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 VR 1.0
 PT J
 AU Liu, W
 Zhang, B
 Wang, Q
 Xie, ZH
 Yao, WB
 Gao, XD
 Yu, LL
 AF Liu, Wei
 Zhang, Boce
 Wang, Qin
 Xie, Zhouhong
 Yao, Wenbing
 Gao, Xiangdong
 Yu, Liangli (Lucy)
 TI Effects of Sulfation on the Physicochemical and Functional Properties
 of Psyllium
 SO JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
 AB The sulfation of psyllium was carried out with sulfur trioxide-pyridine
 in dimethyl formamide. Three sulfated psyllium derivatives, named SP1,
 SP2, and SP3, were characterized by sulfur content determination,
 elemental analysis, FT-IR, and surface charge analysis. The sulfated
 derivatives were also evaluated for their morphological and
 rheological properties, water uptake capacities, swelling volumes, and
 in vitro bile acid-binding abilities. The results showed that sulfation
 reduced the gelling capacity of psyllium and the viscosity of its
 solution, and significantly increased its bile acid-binding capacity.
 Sulfation might also increase the water uptake ability of psyllium but
 might decrease its swelling capacity. The three sulfated psyllium
 derivatives had in vitro binding capacities against cholic and
 chenodeoxycholic acids comparable to that of cholestyramine resin on
 a per same as it is weight basis. The bile acid-binding capacity of
 SP1 was about 8.4-fold of that observed for the original psyllium
 preparation under the same assay conditions. The results from this
 study suggest that sulfation is a possible approach to obtain novel
 psyllium derivatives with desirable physicochemical, functional, and
 biological properties for utilization in functional foods or
 supplemental and pharmaceutical products.
 SN 0021-8561
 PD JAN 13
 PY 2010
 VL 58
 IS 1
 BP 172
 EP 179
 DI 10.1021/jf902731p
 UT ISI:000273268100023
 PT J
 AU Yan, JL
 Qian, ZY
 Sheng, L
 Zhao, BH
 Yang, LN
 Ji, H
 Han, XY
 Zhang, R
 AF Yan, Junling
 Qian, Zhiyu
 Sheng, Liang
 Zhao, Bohua
 Yang, Lina
 Ji, Hui
 Han, Xiaoyuan
 Zhang, Rong
 TI EFFECT OF CROCETIN ON BLOOD PRESSURE RESTORATION AND SYNTHESIS OF
 INFLAMMATORY MEDIATORS IN HEART AFTER HEMORRHAGIC SHOCK IN
 ANESTHETIZED RATS
 SO SHOCK
 AB Crocetin, a constituent of saffron, has been shown not only to prevent
 reactive oxygen species-induced hepatotoxicity and genotoxicity but
 also to increase whole-body oxygen consumption and survival. The
 present study was to determine whether crocetin has beneficial effects
 on cardiac injury caused by hemorrhagic shock and resuscitation in
 rats. Anesthetized rats were bled to reduce mean arterial pressure
 (MAP) to 35 +/- 5 mmHg for 60 min and then resuscitated with their
 withdrawn shed blood and isotonic sodium chloride solution. Crocetin
 was administered via the duodenum at 50 mg/kg 40 min after bleeding.
 We investigated MAP, serum creatine kinase activity, the activity of
 nuclear factor-kappa B, iNOS, and total superoxide dismutase (T-SOD),
 as well as levels of NO, malondialdehyde, TNF-alpha, and IL-6 in the
 heart at 2 h postresuscitation. Compared with control group, crocetin
 significantly increased MAP from 10 min after administration to the
 end of the protocol except the period between 75 and 90 min after initial
 bleeding, whereas serum creatine kinase activity was dramatically
 decreased at 2 h postresuscitation. Myocardial nuclear factor-kappa
 B activity, iNOS activity, NO, malondialdehyde, TNF-alpha, and IL-6
 were significantly elevated, whereas T-SOD activity was suppressed in
 the control group if compared with those of sham animals. These
 parameters tended to be normalized in rats administered crocetin. These
 results suggest that crocetin blocks inflammatory cascades by
 inhibiting reactive oxygen species production and preserving T-SOD
 activity to ameliorate the cardiac injury caused by
 hemorrhage/resuscitation.
 SN 1073-2322
 PD JAN
 PY 2010
 VL 33
 IS 1
 BP 83
 EP 87
 DI 10.1097/SHK.0b013e3181a98f55
 UT ISI:000272970200014
 PT J
 AU Zhang, J
 Deng, DW
 Qian, ZY
 Liu, F
 Chen, XY
 An, LX
 Gu, YQ
 AF Zhang, Jian
 Deng, Dawei
 Qian, Zhiyu
 Liu, Fei
 Chen, Xinyang
 An, Lianxiao
 Gu, Yueqing
 TI The Targeting Behavior of Folate-Nanohydrogel Evaluated by Near
 Infrared Imaging System in Tumor-Bearing Mouse Model
 SO PHARMACEUTICAL RESEARCH
 AB Purpose. To synthesize
 P[(Folate-Allylamine)-co-(N-isopropylacrylamine)-co-Acrylamide] (P
 (FoAAnco-NIPA- AAm), folate-NHG) with appropriate diameter and lower
 critical solution temperature (LCST) for targeting to folate receptor
 (FR) expressing tumors.
 Methods. Folate-NHG was synthesized by free-radical precipitation
 polymerization method reported in our previous work and other reports.
 LCST, diameter and morphology of folate-NHG were characterized by
 UV-vis spectrophotometer, laser particle size analyzer (LPSA) and
 transmission electron microscope (TEM), respectively. No. 12 near
 infrared dye (NIRD-12) was entrapped into folate-NHG by hydrophobic
 association to trace the in vivo dynamic behavior of folate-NHG. This
 process was evaluated by a homemade near infrared (NIR) imaging system.
 Results. Spherical folate-NHG with diameter of about 50 nm and LCST
 of about 40 C was successfully synthesized. The photo stability of
 NIRD-12 was strengthened after being entrapped into folate-NHG, which
 enabled NIRD-12 to better trace the in vivo dynamic process of
 folate-NHG. Folate-NHG showed good targeting capability for all three
 folate receptor expressing tumor models (SMMC-7721, Bel-7402 and HeLa)
 with different sizes, and this accumulation could last for more than
 96 h. D-folate-NHG, synthesized with double amount of FoAAn, showed
 better targeting effect for SMMC-7721 tumor model than that of
 folate-NHG.
 Conclusions. Folate-NHG could actively accumulate in three models of
 folate receptor positive tumors with different sizes and keep retention
 for more than 96 h, which enables it to be used as a diagnostic reagent
 or anti-tumor drug carrier for tumor therapy.
 SN 0724-8741
 PD JAN
 PY 2010
 VL 27
 IS 1
 BP 46
 EP 55
 DI 10.1007/s11095-009-0005-1
 UT ISI:000272905300005
 PT J
 AU Mu, R
 Lu, N
 Wang, J
 Yin, YH
 Ding, Y
 Zhang, XX
 Gui, H
 Sun, Q
 Duan, HQ
 Zhang, L
 Zhang, YC
 Ke, X
 Guo, QL
 AF Mu, Rong
 Lu, Na
 Wang, Jia
 Yin, Yueheng
 Ding, Yan
 Zhang, Xiaoxuan
 Gui, Huan
 Sun, Qiong
 Duan, Huaqin
 Zhang, Lun
 Zhang, Yuchen
 Ke, Xue
 Guo, Qinglong
 TI An oxidative analogue of gambogic acid-induced apoptosis of human
 hepatocellular carcinoma cell line HepG2 is involved in its anticancer
 activity in vitro
 SO EUROPEAN JOURNAL OF CANCER PREVENTION
 AB The objective of this study was to investigate the apoptosis-inducing
 effect of an oxidative analogue of gambogic acid (GA) on the human
 hepatocellular carcinoma cell line HepG2 and explore the related
 molecular mechanisms. HepG2 cells were treated with the analogue of
 GA and the growth inhibition was analysed by MTT assay. The
 morphological changes in cells were observed under an inverted light
 microscope and a fluorescence microscope. In addition, both the
 cell-cycle arrest and the apoptosis rate were detected by flow
 cytometry. Western blot was used to evaluate the alteration of protein
 expression. The viability of HepG2 cells was markedly inhibited in a
 concentration-dependent manner and obvious morphological changes were
 confirmed, including condensed chromatin and reduced volume. Increased
 percentage of apoptotic cells was displayed and altered expression
 level of several apoptosis-associated proteins, P53, Bcl-2, Bax and
 pro-caspase-3, was obtained. The newly synthesized analogue of GA
 exhibited potential anticancer activity, induced remarkable apoptosis
 in HepG2 cells, probably through the intrinsic mitochondrial pathway,
 and promised to be a new candidate for future cancer therapy. European
 Journal of Cancer Prevention 19:61-67 (C) 2010 Wolters Kluwer Health
 | Lippincott Williams & Wilkins.
 SN 0959-8278
 PD JAN
 PY 2010
 VL 19
 IS 1
 BP 61
 EP 67
 DI 10.1097/CEJ.0b013e328333fb22
 UT ISI:000272952200010
 PT J
 AU Zhao, L
 Chen, Z
 Wang, J
 Yang, L
 Zhao, Q
 Wang, J
 Qi, Q
 Mu, R
 You, QD
 Guo, QL
 AF Zhao, Li
 Chen, Zhen
 Wang, Jun
 Yang, Li
 Zhao, Qing
 Wang, Jia
 Qi, Qi
 Mu, Rong
 You, Qi-Dong
 Guo, Qing-Long
 TI Synergistic effect of 5-fluorouracil and the flavanoid oroxylin A on
 HepG2 human hepatocellular carcinoma and on H-22 transplanted mice
 SO CANCER CHEMOTHERAPY AND PHARMACOLOGY
 AB To investigate the synergistic inhibitory effects of the combination
 of 5-fluorouracil (5-FU) with the natural flavanoid oroxylin A on human
 hepatocellular carcinoma cells HepG2 in vitro and on transplanted
 murine hepatoma 22 (H-22) tumors in vivo and the preliminary
 mechanisms.
 The inhibitory effects of 5-FU combined with the natural flavanoid
 oroxylin A in vitro were detected by MTT assay and the effects in vivo
 were investigated by transplanted H-22 mice model. DAPI staining and
 Annexin V/propidium iodide (PI) double staining were used to detect
 the cell morphological changes and apoptosis. The mRNA levels of
 thymidine synthetase (TS) and dihydropyrimidine dehydrogenase (DPD)
 in HepG2 cells after oroxylin A and 5-FU combination treatment were
 observed by quantitative real-time PCR. Western blotting assay was used
 to reveal the expressions of apoptotic-inducing proteins P53, cleaved
 PARP, COX-2, Bcl-2, and pro-caspase3.
 Oroxylin A in combination with 5-FU presented synergistic effect (CI
 < 1) on HepG2 cells in vitro when the inhibitory rate was higher than
 7.5%. The inhibitory rate on H-22 murine solid tumor in vivo in the
 combination group was higher than monotherapy. 5-FU combined with
 oroxylin A exerted stronger apoptotic induction in HepG2 cells than
 either single drug treatment. Quantitative real-time PCR discovered
 the downregulation of TS mRNA and DPD mRNA in HepG2 cells after
 combination treatment. Western blotting assay revealed oroxylin A
 enhanced 5-FU-induced apoptosis in HepG2 cells by elevating the
 expressions of apoptotic-inducing proteins P53 and cleaved PARP and
 decreasing the expression of apoptotic-inhibitory proteins COX-2,
 Bcl-2, and pro-caspase3.
 The anti-hepatocellular carcinoma effects in vitro and in vivo of 5-FU
 and oroxylin A combinations were synergistic and oroxylin A increased
 the sensitivity of HepG2 cells to 5-FU by modulating the metabolic
 enzymes of 5-FU and apoptotic-related proteins.
 SN 0344-5704
 PD FEB
 PY 2010
 VL 65
 IS 3
 BP 481
 EP 489
 DI 10.1007/s00280-009-1053-2
 UT ISI:000273031400009
 PT J
 AU Zhang, YC
 Zhou, JP
 Pan, WH
 Wu, XM
 Wang, S
 AF Zhang, Yanchun
 Zhou, Jinpei
 Pan, Weihong
 Wu, Xiaoming
 Wang, Shuai
 TI Synthesis and Biological Study of
 3-Butyl-1-(2,6-dichlorophenyl)-1H-[1,2,4]triazol-5(4H)-one
 Derivatives as Anti-hypertension Drugs
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB A series of nitric oxide-donating derivatives of
 [1,2,4]triazol-5(4H)-one (9a-f and 15a-f) as a novel class of
 angiotensin II receptor AT1 antagonists have been designed and
 synthesized by coupling furoxan and nitric oxide with lead compound
 1. The synthesized compounds were evaluated for their antagonism of
 AT1 receptor with induced contraction in the rabbit thoracic aortic
 ring and the results showed that compounds 9b, 15b and 15d exhibited
 potent antagonistic activity of AT1 receptor. Moreover 9b, 15b, 15d,
 15e had good maximum NO release amount of this series.
 SN 1570-1808
 PD JAN
 PY 2010
 VL 7
 IS 1
 BP 18
 EP 22
 UT ISI:000272791000005
 PT J
 AU Shu, XY
 Yu, L
 Tang, YP
 Zhang, L
 Ding, AW
 Luo, D
 Duan, JA
 Shen, XC
 AF Shu, Xiaoyun
 Yu, Li
 Tang, Yuping
 Zhang, Li
 Ding, Anwei
 Luo, Dan
 Duan, Jin-ao
 Shen, Xiangchun
 TI Bioassay-guided separation of the proinflammatory constituents from
 the roots of Euphorbia kansui
 SO JOURNAL OF NATURAL MEDICINES
 AB In view of the toxic inflammatory reaction induced by Euphorbia kansui
 roots, a traditional Chinese medicine used for the treatment of edema,
 ascites, and asthma, the 95% ethanol extract was found to have a
 significant stimulating effect on inflammatory cells. Bioassay-guided
 separation of the 95% ethanol extract from the roots of E. kansui led
 to the isolation of five diterpenoids whose structures were identified
 by H-1, C-13 NMR spectroscopy and HR-ESI-MS as kansuinine B (1),
 kansuinine A (2), kansuiphorin C (3), 3-O-benzoyl-20-deoxyingenol (4),
 and 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (5). The
 proinflammatory effect of compounds 1-5 was evaluated in vitro in
 models of inflammation using exoteric mice splenic lymphocytes (SPL)
 and rat peritoneal macrophages (PM phi). Compounds 1, 2, and 5 markedly
 promoted SPL proliferation and NO production by PM phi at
 concentrations from 0.78 to 12.50 mu g/mL. Hence the three compounds
 are believed to be important proinflammatory components of the roots
 of E. kansui.
 SN 1340-3443
 PD JAN
 PY 2010
 VL 64
 IS 1
 BP 98
 EP 103
 DI 10.1007/s11418-009-0366-0
 UT ISI:000272849000017
 PT J
 AU Shen, J
 Sun, MJ
 Ping, QN
 Ying, Z
 Liu, W
 AF Shen, Jie
 Sun, Minjie
 Ping, Qineng
 Ying, Zhi
 Liu, Wen
 TI Incorporation of liquid lipid in lipid nanoparticles for ocular drug
 delivery enhancement
 SO NANOTECHNOLOGY
 AB The present work investigates the effect of liquid lipid incorporation
 on the physicochemical properties and ocular drug delivery enhancement
 of nanostructured lipid carriers (NLCs) and attempts to elucidate in
 vitro and in vivo the potential of NLCs for ocular drug delivery. The
 CyA-loaded or fluorescein-marked nanocarriers composed of Precifac ATO
 5 and Miglyol 840 (as liquid lipid) were prepared by melting-emulsion
 technology, and the physicochemical properties of nanocarriers were
 determined. The uptake of nanocarriers by human corneal epithelia cell
 lines (SDHCEC) and rabbit cornea was examined. Ex vivo fluorescence
 imaging was used to investigate the ocular distribution of
 nanocarriers. The in vitro cytotoxicity and in vivo acute tolerance
 were evaluated. The higher drug loading capacity and improved in vitro
 sustained drug release behavior of lipid nanoparticles was found with
 the incorporation of liquid lipid in lipid nanoparticles. The uptake
 of nanocarriers by the SDHCEC was increased with the increase in liquid
 lipid loading. The ex vivo fluorescence imaging of the ocular tissues
 indicated that the liquid lipid incorporation could improve the ocular
 retention and penetration of ocular therapeutics. No alternation was
 macroscopically observed in vivo after ocular surface exposure to
 nanocarriers. These results indicated that NLC was a biocompatible and
 potential nanocarrier for ocular drug delivery enhancement.
 SN 0957-4484
 PD JAN 15
 PY 2010
 VL 21
 IS 2
 AR 025101
 DI 10.1088/0957-4484/21/2/025101
 UT ISI:000272641800001
 PT J
 AU Tu, FP
 Chu, WH
 Zhuang, XY
 Lu, CP
 AF Tu, F. P.
 Chu, W. H.
 Zhuang, X. Y.
 Lu, C. P.
 TI Effect of oral immunization with Aeromonas hydrophila ghosts on
 protection against experimental fish infection
 SO LETTERS IN APPLIED MICROBIOLOGY
 AB Aims:
 To investigate whether oral immunization with Aeromonas hydrophila
 ghosts (AHG) vaccine can elicit mucosal and systemic immune responses
 of Carp (Carassius auratus gibelio) compared to conventional
 formalin-killed bacteria (FKC).
 Methods and Results:
 Fish were fed diets coated with AHG, FKC or phosphate buffered saline
 (PBS) alone, after immunization, more antigen-specific antibody was
 significantly detected in serum and intestinal mucus in AHG group than
 FKC group and PBS group. In addition, after challenged with the parent
 strain J-1, the survival of bacterial ghost-vaccinated fish was higher
 than PBS group and FKC group, the relative per cent survival (RPS) being
 76 center dot 8%, 58 center dot 9%, respectively.
 Conclusions:
 Oral immunization with A. hydrophila ghosts can elicit systemic and
 mucosal adaptive immune responses and has higher potential to induce
 protective adaptive immunity than normal vaccine.
 Significance and Impact of the Study:
 Oral immunization with bacterial ghosts is a promising new solution
 with potential application to prevent diseases in fish.
 SN 0266-8254
 PD JAN
 PY 2010
 VL 50
 IS 1
 BP 13
 EP 17
 DI 10.1111/j.1472-765X.2009.02746.x
 UT ISI:000272582600003
 PT J
 AU Du, JL
 Shen, NF
 Zhu, LY
 Wang, JL
 AF Du, Jinli
 Shen, Naifeng
 Zhu, Liyan
 Wang, Jinlan
 TI Emergence of noncollinear magnetic ordering in bimetallic Co6-nMnn
 clusters
 SO JOURNAL OF PHYSICS D-APPLIED PHYSICS
 AB Using spin-polarized density functional calculations, we have studied
 the magnetic states including collinear and noncollinear magnetic
 coupling in bimetallic Co6-nMnn clusters. The ground state of Co6-nMnn
 clusters displays collinear magnetic ordering for n <= 3, whereas a
 magnetic transition to noncollinear ordering occurs at n = 4 and the
 noncollinear magnetic structure remains to be energetically favoured
 afterwards. Moreover, the total magnetic moment of Co6-nMnn increases
 with n by 2 mu(B) for n = 0-3 and decreases sharply from n = 3 to n
 = 4, while the decreasing trend becomes smooth for n = 4-6. The
 competition of ferromagnetic and antiferromagnetic interactions
 between the neighbouring magnetic moments induces the emergence of
 noncollinear magnetic coupling in the small bimetallic clusters.
 SN 0022-3727
 PD JAN 13
 PY 2010
 VL 43
 IS 1
 AR 015006
 DI 10.1088/0022-3727/43/1/015006
 UT ISI:000272702300010
 PT J
 AU Zhang, XY
 Liu, JP
 Qiao, H
 Liu, H
 Ni, JM
 Zhang, WL
 Shi, YB
 AF Zhang, Xiaoyun
 Liu, Jianping
 Qiao, Hua
 Liu, Huan
 Ni, Jingman
 Zhang, Wenli
 Shi, Yanbin
 TI Formulation optimization of dihydroartemisinin nanostructured lipid
 carrier using response surface methodology
 SO POWDER TECHNOLOGY
 AB Response surface methodology (RSM) using the central composite
 rotatable design (CCRD) model was used to optimize formulations of
 dihydroartemisinin nancistructured lipid carrier (DHA-NLC). The CCRD
 consisting of three-factored factorial design with three levels was
 used in this study The drug encapsulation efficiency (EE), drug loading
 (DL) percentage and particle size of DHA-NLC were investigated with
 respect to three independent variables including DHA concentration
 (XI), lipid concentration (X-2) and ratio of liquid lipid to total lipid
 (X-3). The result showed that the optimal formulation could be obtained
 from this response surface methodology The optimal formulation for
 DHA-NLC was composed of DHA concentration (X-1) of 1 g/l, lipid
 concentration (X-2) of 1% and ratio of liquid lipid to total lipid (X-3)
 of 0.1:1. DHA-NLC under the optimized conditions gave rise to the EE
 of (98.97 +/- 2.3)%, DL of (15.61 +/- 1.9) mean diameter of (198 +/4.7) nm, polydispersity index (PI) of 0.146 and zeta potential value
 of (-21.6 +/- 1.3) mV TEM of the optimized NLC showed spherical
 particles. The in vitro experiments proved that DHA in the NLC released
 gradually over the period of 48 h. This study showed that the RSM-CCRD
 could efficiently be applied for the modeling of DHA-NLC. Published
 by Elsevier B.V.
 SN 0032-5910
 PD JAN 10
 PY 2010
 VL 197
 IS 1-2
 BP 120
 EP 128
 DI 10.1016/j.powtec.2009.09.004
 UT ISI:000272125000016
 PT J
 AU Zhang, T
 Liu, H
 Liu, XT
 Xu, DR
 Chen, XQ
 Wang, Q
 AF Zhang, Ting
 Liu, Hai
 Liu, Xue-Ting
 Xu, De-ran
 Chen, Xiao-qing
 Wang, Qiang
 TI Qualitative and quantitative analysis of steroidal saponins in crude
 extracts from Paris polyphylla var. yunnanensis and P. polyphylla var.
 chinensis by high performance liquid chromatography coupled with mass
 spectrometry
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 AB High performance liquid chromatography coupled with electrospray
 ionization multi-stage tandem mass spectrometry (HPLC-ESI-MSn) and
 triple quadrupole mass spectrometric detection (HPLC-ESI-MS/MS),
 respectively, had been employed for the simultaneous identification
 and quantification of steroidal saponins in the rhizomes of Paris
 polyphylla var. yunnanensis and A polyphylla var. chinensis, which are
 the qualified plants of "Chonglou" in Chinese. The HPLC experiments
 were performed by means of a reversed-phase C-18 column and a binary
 mobile phase system consisting of 0.1% aqueous formic acid and
 acetonitrile under gradient elution conditions. The characteristic
 fragmentation patterns of diosgenin- and pennogenin-type steroidal
 saponins were investigated using ESI-MSn in negative ion mode. The MSn
 data of the [M-H](-) ions provided structural information on the sugar
 sequence of the oligosaccharide chains and the aglycones of steroidal
 saponins. As a result, ten and seven saponins were determined in A
 polyphylla var. yunnanensis and P. polyphylla var. chinensis,
 respectively, including four unknown compounds. One unknown compound
 was tentatively identified as
 diosgenin-3-O-alpha-L-rhamnopyranosyl(1 --> 4)
 [alpha-L-rhamnopyranosyl(1 --> 2)]-beta-D-glucopyranoside and the
 aglycones of the other three new compounds were reported from Chonglou
 for the first time. The developed HPLC-ESI-MS/MS method was validated
 and found to be satisfactorily linear, selective and robust. The limits
 of detection (LODs) and quantitation (LOQs) ranged, respectively, from
 0.5 to 10 ng/mL and 2 to 34 ng/mL depending on six various compounds.
 The intra- and inter-day precisions of the method were evaluated and
 were less than 5.0%. Recoveries ranged from 92% to 104% for all
 compounds. The established quality evaluation method was successfully
 used for simultaneous quantification of six predominant steroidal
 saponins in the rhizomes of these two Paris species. (C) 2009 Elsevier
 B.V. All rights reserved.
 SN 0731-7085
 PD JAN 5
 PY 2010
 VL 51
 IS 1
 BP 114
 EP 124
 DI 10.1016/j.jpba.2009.08.020
 UT ISI:000270748100018
 FN ISI Export Format
 VR 1.0
 PT J
 AU Zhang, M
 Liu, K
 Li, L
 Fan, JH
 Song, JN
 Liu, BL
 AF Zhang Min
 Liu Kang
 Li Lin
 Fan Jinghua
 Song Junna
 Liu Baolin
 TI Resveratrol Restores Lysophosphatidylcholine-induced Loss of
 Endothelium-dependent Relaxation in Rat Aorta Tissue Coinciding with
 Inhibition of Extracellular-signal-regulated Protein Kinase
 Activation
 SO PHYTOTHERAPY RESEARCH
 AB To investigate whether resveratrol could restore the
 lysophosphatidylcholine (LPC)-induced loss of endothelium-dependent
 relaxation in in vitro cultured rat aorta tissue, first the effect of
 resveratrol on the loss of EDR was examined in this preparation. The
 results showed that resveratrol effectively attenuated the inhibition
 of LPC (10 mu m) on both endothelium-derived relaxing factor (EDRF)
 and endothelium-derived hyperpolarizing factor (EDHF) in a
 concentration-dependent manner (1, 10, 100 mu m). In addition,
 resveratrol inhibited elevated K+-induced vascular contracture, but
 had no significant effects on ACh (1 mu m)-induced
 endothelium-dependent relaxation (EDR). A similar tendency was also
 observed with PD 98059 (30 mu m), a selective inhibitor of ERK. When
 the cells were exposed to LPC (20 mu M) the mRNA expression of eNOS
 and COX-1 mRNA were down-regulated, followed by a local induction of
 iNOS and COX-2. Resveratrol and PD 98059 successfully reversed the
 effects of LPC on relative mRNA expressions. Both resveratrol and PD
 98059 inhibited the activation of ERK induced by LPC. These findings
 demonstrate that resveratrol can restore the LPC-induced loss of EDR
 in rat aorta and protect the endothelium against LPC-induced injuries
 via the inhibition of the inflammation-like response. Copyright (C)
 2010 John Wiley & Sons, Ltd.
 SN 0951-418X
 PD DEC
 PY 2010
 VL 24
 IS 12
 BP 1762
 EP 1768
 DI 10.1002/ptr.3136
 UT ISI:000285679200004
 PT J
 AU Song, M
 Zhang, SY
 Xu, XY
 Hang, TJ
 Jia, L
 AF Song, Min
 Zhang, Siyun
 Xu, Xiaoyan
 Hang, Taijun
 Jia, Lee
 TI Simultaneous determination of three Panax notoginseng saponins at
 sub-nanograms by LC-MS/MS in dog plasma for pharmacokinetics of
 compound Danshen tablets
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB Compound Danshen tablets are composed of Panax notoginseng, Salvia
 miltiorrhiza and Borneol. The tablets are prescribed for treatment of
 cardiovascular diseases in China. The present study aimed at developing
 a specific and sensitive LC-MS/MS method to simultaneously determine
 three bioactive P. notoginseng saponins, i.e., notoginsenoside R1.
 ginsenoside Rg1 and Rb1, in dogs after a single oral administration
 of the compound tablets in order to obtain the clinically relevant
 saponin-related pharmacodynamics of the tablets in patients. The R1,
 Rg1 and Rb1 were extracted from dog plasma with acetone-methanol
 (80:20, v/v), separated by reversed phase liquid chromatography and
 determined by tandem mass spectrometry (LC-MS/MS) with positive
 electrospray ionization (ESI). The developed method reached lower
 limit of quantitation (LLOQ) at 0.10 ng/ml for the three saponins. The
 method was validated in terms of selectivity, matrix effects,
 linearity, precision and accuracy, and then was applied to a
 pharmacokinetic study of the three bioactive saponins simultaneously
 in dogs after a single oral administration of compound Danshen tablets
 at a clinical equivalent dose. The C-max and AUC((o-infinity)) for R1,
 Rg1 and Rb1 were 1.91, 3.34 and 28.6 ng/ml, and 7.5, 11.0, and 1712
 (h ng/ml), respectively. (c) 2010 Elsevier ay. All rights reserved.
 SN 1570-0232
 PD DEC 15
 PY 2010
 VL 878
 IS 32
 BP 3331
 EP 3337
 DI 10.1016/j.jchromb.2010.10.007
 UT ISI:000285951500001
 PT J
 AU Zhuang, J
 Ping, QN
 Song, YM
 Qi, JP
 Cui, Z
 AF Zhuang, Jie
 Ping, Qineng
 Song, Yunmei
 Qi, Jianping
 Cui, Zheng
 TI Effects of chitosan coating on physical properties and pharmacokinetic
 behavior of mitoxantrone liposomes
 SO INTERNATIONAL JOURNAL OF NANOMEDICINE
 AB The objective of this work was to evaluate the physical properties and
 in vivo circulation of chitosan (CH)-coated liposomes of mitoxantrone
 (MTO). Changes in particle size and zeta potential confirmed the
 existence of a coating layer on the surface of liposomes. The in vitro
 release of adsorbed CH from the liposomes was significantly slower than
 CH solution, indicating the stable interaction between CH and
 liposomes. The physical stability of the CH-coated liposomes was
 evaluated by measuring the change in particle size before and after
 freeze-drying and rehydration. The smallest change was observed when
 saturated adsorption of CH occurred (0.3%). The sustained release in
 vitro of MTO from CH-coated liposomes confirmed the increased stability
 of liposomes. Systemic circulation of CH-coated MTO liposomes was
 examined. The 0.3% CH-coated liposomes showed the longest circulation
 time. It could be concluded that the prolonged retention time of the
 liposomes was closely related with CH coating and its stability effect.
 SN 1176-9114
 PY 2010
 VL 5
 BP 407
 EP 416
 UT ISI:000283715300041
 PT S
 AU Gu, YQ
 Liu, F
 Fang, CS
 Qian, ZY
 Achilefu, S
 AF Gu, Yueqing
 Liu, Fei
 Fang, Chunsheng
 Qian, Zhiyu
 Achilefu, Samuel
 ED Achilefu, S; Raghavachari, R
 TI In vivo investigation of pharmacokinetics of model drug: comparison
 of near infrared technique with high-performance liquid chromatography
 SO REPORTERS, MARKERS, DYES, NANOPARTICLES, AND MOLECULAR PROBES FOR
 BIOMEDICAL APPLICATIONS II
 SE Proceedings of SPIE-The International Society for Optical Engineering
 CT Conference on Reporters, Markers, Dyes, Nanoparticles, and Molecular
 Probes for Biomedical Applications II
 CY JAN 25-27, 2010
 CL San Francisco, CA
 AB Near infrared spectroscopy possess great potential for in vivo
 quantitative monitoring of drugs in animal subject. The accuracy of
 the measurements by near infrared technique should be evaluated by an
 established method. In this study, a near infrared fluorescence dye,
 cypate and its conjugation cypate-PEG were used as model drug for in
 vivo dynamic study. The pharmacokinetics of the model drug in mice
 subjects were investigated by near infrared spectroscopy and high
 performance liquid chromatography, respectively. The results from the
 two techniques were compared. The pharmacokinetic parameters
 calculated based on the acquired data by DAS software showed that there
 were no statistical differences between the two methods. The dynamic
 distribution of the model drugs in mouse model imaged by NIR image
 system indicated that cypate firstly accumulated in liver and was
 cleared from the enteron system, while cypate - PEG clearance from the
 urine system. Results indicated that NIR monitoring technique provide
 a promising quantitative way for in vivo monitoring the dynamics of
 drugs in animal subjects.
 SN 0277-786X
 BN 978-0-8194-7972-3
 PY 2010
 VL 7576
 AR 75760A
 DI 10.1117/12.840332
 UT ISI:000285580600008
 PT S
 AU Deng, DW
 Chen, XY
 Zhang, JA
 Liu, F
 Cao, J
 Gu, YQ
 AF Deng, Dawei
 Chen, Xinyang
 Zhang, Jian
 Liu, Fei
 Cao, Jie
 Gu, Yueqing
 ED Achilefu, S; Raghavachari, R
 TI Aqueous synthesis of PbS quantum dots for noninvasive near-infrared
 fluorescence imaging in a mouse model
 SO REPORTERS, MARKERS, DYES, NANOPARTICLES, AND MOLECULAR PROBES FOR
 BIOMEDICAL APPLICATIONS II
 SE Proceedings of SPIE-The International Society for Optical Engineering
 CT Conference on Reporters, Markers, Dyes, Nanoparticles, and Molecular
 Probes for Biomedical Applications II
 CY JAN 25-27, 2010
 CL San Francisco, CA
 AB In this paper, we present a new facile and environmental friendly method
 to prepare water-soluble near-infrared (NIR)-emitting PbS quantum dots
 (QDs) at room temperature under ambient conditions, using
 dihydrolipoic acid (DHLA) as a stabilizer. The photoluminescence (PL)
 emissions of the prepared DHLA-capped PbS QDs are tunable between 870
 and 1010 nm. A PL quantum yield (QY) of similar to 10% can be achieved
 under optimized conditions without any post-preparative treatment.
 Here, we further use the produced DHLA-capped PbS QDs for NIR
 fluorescence imaging in a mouse model. The obtained experimental
 results showed that the NIR fluorescence of the PbS QDs in living
 tissues generated from the excitation with semiconductor laser
 (lambda(max)=765.9 nm) could penetrate living tissues and be detected
 easily by the noninvasive in vivo NIR fluorescence imaging system. In
 addition, the preliminary studies on the cytotoxicity and in vivo
 toxicity of the QDs also indicates fully that these water-soluble
 DHLA-capped PbS QDs are very lowly toxic, and as such they should have
 greater potential in biological and medical applications especially
 in noninvasive in vivo fluorescence imaging of mice, compared to other
 existing highly toxic aqueous NIR-emitting quantum dots (CdTe, HgTe,
 etc).
 SN 0277-786X
 BN 978-0-8194-7972-3
 PY 2010
 VL 7576
 AR 75761K
 DI 10.1117/12.840136
 UT ISI:000285580600036
 PT J
 AU Zhou, XA
 Li, MA
 Wang, XB
 Wang, T
 Kong, LY
 AF Zhou, Xiang
 Li, Miao
 Wang, Xiao-Bing
 Wang, Tao
 Kong, Ling-Yi
 TI Synthesis of Benzofuran Derivatives via Rearrangement and Their
 Inhibitory Activity on Acetylcholinesterase
 SO MOLECULES
 AB During a synthesis of coumarins to obtain new candidates for treating
 Alzheimer's Disease (AD), an unusual rearrangement of a benzopyran
 group to a benzofuran group occurred, offering a novel synthesis
 pathway of these benzofuran derivatives. The possible mechanism of the
 novel rearrangement was also discussed. All of the benzofuran
 derivatives have weak anti-AChE activities compared with the reference
 compound, donepezil.
 SN 1420-3049
 PD DEC
 PY 2010
 VL 15
 IS 12
 BP 8593
 EP 8601
 DI 10.3390/molecules15128593
 UT ISI:000285709000006
 PT J
 AU Liu, EH
 Qi, LW
 Li, P
 AF Liu, E-Hu
 Qi, Lian-Wen
 Li, Ping
 TI Structural Relationship and Binding Mechanisms of Five Flavonoids with
 Bovine Serum Albumin
 SO MOLECULES
 AB Flavonoids are structurally diverse and the most ubiquitous groups of
 dietary polyphenols distributed in various fruits and vegetables. In
 this study, the interaction between five flavonoids, namely
 formononetin-7-O-beta-D-glucoside, calycosin-7-O-beta-D-glucoside,
 calycosin, rutin, and quercetin, and bovine serum albumin (BSA) was
 investigated by fluorescence and UV-vis absorbance spectroscopy. In
 the discussion, it was proved that the fluorescence quenching of BSA
 by flavonoids was a result of the formation of a flavonoid-BSA complex.
 Fluorescence quenching constants were determined using the
 Stern-Volmer and Lineweaver-Burk equations to provide a measure of the
 binding affinity between the flavonoids and BSA. The binding constants
 ranked in the order quercetin > rutin > calycosin >
 calycosin-7-O-beta-D-glucoside approximate to
 formononetin-7-O-beta-D-glucoside. The results of thermodynamic
 parameters Delta G, Delta H, and Delta S at different temperatures
 indicated that the hydrophobic interaction played a major role in
 flavonoid-BSA association. The distance r between BSA and acceptor
 flavonoids was also obtained according to Forster's theory of
 non-radiative energy transfer.
 SN 1420-3049
 PD DEC
 PY 2010
 VL 15
 IS 12
 BP 9092
 EP 9103
 DI 10.3390/molecules15129092
 UT ISI:000285709000037
 PT J
 AU Wei, LB
 Lu, N
 Dai, QS
 Rong, JJ
 Chen, Y
 Li, ZY
 You, QD
 Guo, QL
 AF Wei, Libin
 Lu, Na
 Dai, Qinsheng
 Rong, Jingjing
 Chen, Yan
 Li, Zhiyu
 You, Qidong
 Guo, Qinglong
 TI Different Apoptotic Effects of Wogonin Via Induction of H2O2 Generation
 and Ca2+ Overload in Malignant Hepatoma and Normal Hepatic Cells
 SO JOURNAL OF CELLULAR BIOCHEMISTRY
 AB Wogonin, a major active constituent of Scutellaria baicalensis,
 possesses potent anticancer activities both in vivo and in vitro. This
 paper describes the different apoptotic effects of wogonin in HepG2
 and L02 cells and the possible mechanism for the differences. Through
 DAPI staining, Annexin-V/PI double-staining assay, JC-1 detection and
 the expressions of the key apoptotic proteins, we find that wogonin
 prefers to induce apoptosis in HepG2 cells through the mitochondrial
 pathway, while has much less effects on L02 cells. Moreover,
 overexpression of Bcl-2 can block wogonin-induced apoptosis in HepG2
 cells. To illustrate the specific selective mechanism of wogonin in
 apoptosis induction, H2O2, O-center dot(2)- and Ca2+ are measured by
 2',7'-dichlorfluorescein-diacetate, dihydroethidium and Flou-3 AM
 assay, respectively. The results show that the different apoptotic
 effects of wogonin in HepG2 and L02 cells are due to the different
 regulations to the redox balance of reactive oxygen species and the
 Ca2+ release from endoplasmic reticulum. IP3R-sensitive Ca2+ channels
 are the key targets of the wogonin-increased H2O2. Besides, the
 activation of PLC gamma 1 plays as a bridge between H2O2 signal
 molecules and Ca2+ release. Taken together, wogonin preferentially
 kills hepatoma cells by H2O2-dependent apoptosis triggered by Ca2+
 overload. The results reveal that wogonin is a competitive anticancer
 drug candidate for the malignant hepatoma therapy. J. Cell. Biochem.
 111: 1629-1641, 2010. (C) 2010 Wiley-Liss, Inc.
 SN 0730-2312
 PD DEC 15
 PY 2010
 VL 111
 IS 6
 BP 1629
 EP 1641
 DI 10.1002/jcb.22898
 UT ISI:000286300700026
 PT J
 AU Guo, P
 Liu, JM
 Li, XK
 Yang, SL
 Yao, QZ
 AF Guo Ping
 Liu Jianmin
 Li Xiaokun
 Yang Shulin
 Yao Qizheng
 TI Chiral Resolution of Curcumol Epoxy Derivatives by Ionic Liquid
 [BMIm]BF4
 SO ACTA CHIMICA SINICA
 AB The isomers of 10,14-epoxycurcumol derivatives were separated by the
 ionic liquid [BMIm]BF4, in which there is a difference in the solubility
 of the complexes formed with the isomers and [BMIm]BF4. The yield 22%
 of (10R)-10,14-epoxycurcumol (E1) with 99% ee and the yield 49% of
 (10S)-10,14-epoxycurcumol (E2) with 92% ee were obtained respectively
 in the resolution. The ionic liquid could be recovered easily and used
 again with the same separation effect.
 SN 0567-7351
 PD DEC 28
 PY 2010
 VL 68
 IS 24
 BP 2619
 EP 2621
 UT ISI:000286352700020
 PT J
 AU Qin, KM
 Cai, H
 Zhang, L
 Shi, Y
 Ping, L
 Cai, BC
 AF Qin Kunming
 Cai Hao
 Zhang Li
 Shi Yun
 Ping, Li
 Cai Baochang
 TI Chemical Constituents and Effective Substances of Traditional Chinese
 Medicinal Formula
 SO PROGRESS IN CHEMISTRY
 AB Traditional Chinese medicinal formula (TCMF) is an important clinic
 guide for application of Chinese medicines. It is a reflection of both
 diagnosis and treatment of traditional Chinese medical theory,
 occupying a pivotal position in the system of Chinese medicine. At
 present, TCMF is facing difficulties because its curative effects are
 largely based on the prescribing doctor's experience and its effective
 constituents and mechanisms of action are unclear, which seriously
 restricts their development in the international market. Chemical
 constituents and effective substance basis of TCMF are two important
 parts of the study of Chinese medicines. In the recent years, the
 development of modern biological and analytical techniques have
 provided new techniques and approaches for the modern studies on
 chemical constituents and effective substances in TCMF. In this paper,
 we reviewed the latest progress of studying the chemical constituents
 and effective substance basis of TCMF, and put forward basic thoughts
 on improving research activities in the area.
 SN 1005-281X
 PD DEC
 PY 2010
 VL 22
 IS 12
 BP 2436
 EP 2449
 UT ISI:000285795300018
 PT J
 AU Zhang, F
 Wang, JS
 Gu, YC
 Kong, LY
 AF Zhang, Feng
 Wang, Jun-Song
 Gu, Yu-Cheng
 Kong, Ling-Yi
 TI Triterpenoids from Aglaia abbreviata and Their Cytotoxic Activities
 SO JOURNAL OF NATURAL PRODUCTS
 AB Six new triterpenoids (1-6), along with 10 known compounds, were
 isolated from the stems of Aglaia abbreviata. The structures of 1-6
 were elucidated on the basis of their spectroscopic data. Compounds
 1-6 were evaluated for their cytotoxic activities against a small panel
 of human tumor cell lines.
 SN 0163-3864
 PD DEC
 PY 2010
 VL 73
 IS 12
 BP 2042
 EP 2046
 DI 10.1021/np100599g
 UT ISI:000285560000013
 PT J
 AU Zhang, WB
 Wang, Z
 Shu, F
 Jin, YH
 Liu, HY
 Wang, QJ
 Yang, Y
 AF Zhang, Wen-bin
 Wang, Zhuo
 Shu, Fei
 Jin, Yong-hua
 Liu, Hong-yi
 Wang, Qiu-juan
 Yang, Yong
 TI Activation of AMP-activated Protein Kinase by Temozolomide Contributes
 to Apoptosis in Glioblastoma Cells via p53 Activation and mTORC1
 Inhibition
 SO JOURNAL OF BIOLOGICAL CHEMISTRY
 AB Methylating drugs such as temozolomide (TMZ) are widely used in the
 treatment of brain tumors including malignant glioblastoma. The
 mechanism of TMZ-induced glioblastoma cell death and apoptosis,
 however, is not fully understood. Here, we tested the potential
 involvement of AMP-activated protein kinase (AMPK) in this process.
 We found that methylating agents TMZ and
 N-methyl-N'-nitro-N-nitrosoguanidine induce AMPK activation in
 primary cultured human glioblastoma and glioblastoma cell lines.
 TMZ-induced O-6-methylguanine production is involved in AMPK
 activation. O-6-benzylguanine, an O-6-methylguanine-DNA
 methyltransferase inhibitor, enhances TMZ-induced O-6-methylguanine
 production, leading to enhanced reactive oxygen species production,
 which serves as an upstream signal for AMPK activation. Activation of
 AMPK is involved in TMZ-induced glioblastoma cell death and apoptosis.
 AMPK inhibitor (Compound C) or AMPK alpha siRNA knockdown inhibits
 TMZ-induced glioblastoma cell death and apoptosis, whereas AMPK
 activator 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside
 enhances it. In further studies, we found that activation of AMPK is
 involved in TMZ-induced p53 activation and subsequent p21, Noxa, and
 Bax up-regulation. Activation of AMPK by TMZ also inhibits mTOR complex
 1 (mTORC1) signaling and promotes anti-apoptosis protein Bcl-2
 down-regulation, which together mediate TMZ-induced pro-cell
 apoptosis effects. Our study suggests that activation of AMPK by TMZ
 contributes to glioblastoma cell apoptosis, probably by promoting p53
 activation and inhibiting mTORC1 signaling.
 SN 0021-9258
 PD DEC 24
 PY 2010
 VL 285
 IS 52
 DI 10.1074/jbc.M110.164046
 UT ISI:000285414400008
 PT J
 AU Zhang, C
 Qin, MJ
 Shu, P
 Hong, JL
 Lue, L
 He, DX
 AF Zhang, Cong
 Qin, Min-Jian
 Shu, Pan
 Hong, Jun-Li
 Lue, Lin
 He, Dan-Xia
 TI Chemical Variations of the Essential Oils in Flower Heads of
 Chrysanthemum indicum L. from China
 SO CHEMISTRY & BIODIVERSITY
 AB The volatile compositions of hydrodistilled essential oils in the
 flower heads of Chrysanthemum indicum L. from eight populations in
 China were analyzed by GC/MS. A total of 169 compounds representing
 88.79-99.53% of the oils were identified, and some remarkable
 differences were found in the constituent percentages of the eight
 populations. The predominant components of the essential oils were
 1,8-cineole (0.62-7.34%), (+)-(1R,4R)-camphor (0.17-27.56%),
 caryophyllene oxide (0.54-5.8%), beta-phellandrene (0.72-1.87%),
 (-)-(1S,2R,4S)-borneol acetate (0.33-8.46%),
 2-methyl-6-(p-tolyl)hept-2-ene (0.3-8.6%),
 4,6,6-trimethylbicyclo[3.1.1]hept-3-en-2-yl acetate (0.17-26.48%),
 and hexadecanoic acid (0.72-15.97%). The chemotaxonomic value of the
 essential-oil compositions was discussed according to the results of
 cluster analysis (CA) and principal-component analysis (PCA). The
 eight populations were divided into five groups as different chemotypes
 (Groups A-E), and the scores together with the loadings revealed
 clearly different chemical properties of each population. In
 conclusion, GC/MS in combination with chemometric techniques provided
 a flexible and reliable method for characterizing the essential oils
 of different populations of C. indicum L.
 SN 1612-1872
 PD DEC
 PY 2010
 VL 7
 IS 12
 BP 2951
 EP 2962
 UT ISI:000285393800014
 PT J
 AU Li, H
 Zhong, WY
 Xu, DK
 AF Li Hui
 Zhong Wen-Ying
 Xu Dan-Ke
 TI Preparation of Biotinylated Silver Nanoparticles and Its Application
 of Visual Detection Method for Protein Chip
 SO CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 AB Biotinylated silver nanoparticles (Bio-AgNPs) were successfully
 prepared using oligonucelotide as coupling molecules. The resulted
 bio-AgNPs could be used for visual detection for protein arrays by a
 catalytical reaction with hydroquinone/AgNO3. To probe the feasibility
 of visual detection, human IgG was used as a model protein sample to
 be immobilized on the glass slides and bio-AgNPs were employed to couple
 with the protein via stripavaidin labeled anti-human IgG. The results
 show that the linear relationship of protein concentration is between
 160 fg and 100 pg and the limit of detection is 160 fg(S/N = 3). Compared
 with the method using SA-labeled gold nanoparticle or silver
 enhancement, the sensitivity of this method is increased about 40 fold.
 The presented method shows its advantages including high sensitivity,
 stability and rapidity.
 SN 0251-0790
 PD NOV 10
 PY 2010
 VL 31
 IS 11
 BP 2184
 EP 2189
 UT ISI:000285538100015
 PT J
 AU Dai, YJ
 Wang, QA
 Zhang, XL
 Jia, SR
 Zheng, H
 Feng, DC
 Yu, P
 AF Dai, Yujie
 Wang, Qiang
 Zhang, Xiuli
 Jia, Shiru
 Zheng, Heng
 Feng, Dacheng
 Yu, Peng
 TI Molecular docking and QSAR study on steroidal compounds as aromatase
 inhibitors
 SO EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 AB In order to develop more potent, selective and less toxic steroidal
 aromatase (AR) inhibitors, molecular docking, 2D and 3D hybrid
 quantitative structure activity relationship (QSAR) study have been
 conducted using topological, molecular shape, spatial, structural and
 thermodynamic descriptors on 32 steroidal compounds. The molecular
 docking study shows that one or more hydrogen bonds with MET374 are
 one of the essential requirements for the optimum binding of ligands.
 The QSAR model obtained indicates that the aromatase inhibitory
 activity can be enhanced by increasing SIC, SC_3_C, Jurs_WNSA_1,
 Jurs_WPSA_1 and decreasing CDOCKER interaction energy (E-CD),
 IAC_Total and Shadow_XZfrac. The predicted results shows that this
 model has a comparatively good predictive power which can be used in
 prediction of activity of new steroidal aromatase inhibitors. (C) 2010
 Elsevier Masson SAS. All rights reserved.
 SN 0223-5234
 PD DEC
 PY 2010
 VL 45
 IS 12
 BP 5612
 EP 5620
 DI 10.1016/j.ejmech.2010.09.011
 UT ISI:000285485000008
 PT J
 AU Zhang, Y
 Wang, JS
 Wei, DD
 Wang, XB
 Luo, J
 Luo, JG
 Kong, LY
 AF Zhang, Yao
 Wang, Junsong
 Wei, Dandan
 Wang, Xiaobing
 Luo, Jun
 Luo, Jianguang
 Kong, Lingyi
 TI Cytotoxic tirucallaneC(26) triterpenoids from the stem barks of
 Aphanamixis grandifolia
 SO PHYTOCHEMISTRY
 AB Five tirucallane type C-26 triterpenoids accompanied by two known
 compounds 3 alpha-hydroxy-24 25 26
 27-tetranortirucall-7-ene-23(21)-lactone and 3-oxo-24 25 26
 27-tetranortirucall-7-ene-23(21)-lactone were isolated from the stem
 barks of Aphanamixis grandifolia Their structures were established
 mainly by means of a combination of 1D and 2D NMR spectroscopic and
 mass spectrometry techniques as 3 alpha-hydroxyl-21 alpha-methoxy-24
 25 26 27-tetranortirucall-7-ene-23(21)-lactone 3 alpha-hydroxy-21
 beta-methoxy-24 25 26 27-tetranortirucall-7-ene-23(21)-lactone
 3-oxo-21 alpha-methoxy-24 25 26
 27-tetranortirucall-7-ene-23(21)-lactone 3-oxo-21 beta-methoxy-24 25
 26 27-tetranortirucall-7-ene-23 (21)-lactone and 3-oxo-21
 alpha-ethoxy-24 25 26 27-tetranortirucall-7-ene-23(21)-lactone All
 Isolates were in vitro evaluated for their cytotoxic activities against
 five tumor cell lines (MCF-7 HeLa HepG2 SGC-7901 and BGC-823) (C) 2010
 Elsevier Ltd All rights reserved
 SN 0031-9422
 PD DEC
 PY 2010
 VL 71
 IS 17-18
 BP 2199
 EP 2204
 DI 10.1016/j.phytochem.2010.08.017
 UT ISI:000285325500031
 PT J
 AU Xu, L
 Sun, H
 AF Xu, L.
 Sun, H.
 TI Pharmacological Manipulation of Brain Glycogenolysis as a Therapeutic
 Approach to Cerebral Ischemia
 SO MINI-REVIEWS IN MEDICINAL CHEMISTRY
 AB Brain ischemia resulting from multiple disease states including
 cardiac arrest, stroke and traumatic brain injury, is a leading cause
 of death and disability. Despite significant resources dedicated to
 developing pharmacological interventions, few effective therapeutic
 options are currently available. The basic consequence of cerebral
 ischemia, characterized by energy failure and subsequent brain
 metabolic abnormalities, enables the protective effects by
 pharmacological manipulation of brain metabolism. We present here the
 important roles of brain glycogen metabolism and propose inhibition
 of glycogenolysis as a therapeutic approach to cerebral ischemia.
 SN 1389-5575
 PD OCT
 PY 2010
 VL 10
 IS 12
 BP 1188
 EP 1193
 UT ISI:000285290000008
 PT J
 AU Qian, S
 Gu, Y
 Xiao, Y
 Mallik, S
 AF Qian, Steven
 Gu, Yan
 Xiao, Ying
 Mallik, Sanku
 TI Characterization of Carbon-Centered Radicals Formed from
 COX-Catalyzed Dihomo-Gamma-Linolenic Acid Peroxidation
 SO FREE RADICAL BIOLOGY AND MEDICINE
 CT 17th Annual Meeting of the Society-for-Free-Radical-Biology-Medicine
 /15th Biennial Meeting of the
 Society-for-Free-Radical-Research-International
 CY NOV 17-21, 2010
 CL Orlando, FL
 SN 0891-5849
 PY 2010
 VL 49
 SU Suppl. 1
 BP S214
 EP S214
 DI 10.1016/j.freeradbiomed.2010.10.624
 UT ISI:000284348000632
 PT J
 AU Chen, ZP
 Sun, J
 Chen, HX
 Xiao, YY
 Liu, D
 Chen, J
 Cai, H
 Cai, BC
 AF Chen, Zhi-peng
 Sun, Jun
 Chen, Hong-xuan
 Xiao, Yan-yu
 Liu, Dan
 Chen, Jun
 Cai, Hao
 Cai, Bao-chang
 TI Comparative pharmacokinetics and bioavailability studies of
 quercetin, kaempferol and isorhamnetin after oral administration of
 Ginkgo biloba extracts, Ginkgo biloba extract phospholipid complexes
 and Ginkgo biloba extract solid dispersions in rats
 SO FITOTERAPIA
 AB The aim of this study was to improve the oral bioavailability of Ginkgo
 biloba extract (GBE) through preparing G. biloba extract phospholipid
 complexes (GBP) and G. biloba extract solid dispersions (CBS). Firstly
 we prepared the GBP and GBS and studied their physicochemical
 properties by differential scanning calorimetry (DSC), powder X-ray
 diffraction (XRD) and dissolution. Then we studied the pharmacokinetic
 characteristics and bioavailability in rats. The results showed that
 the bioavailability of quercetin, kaempferol and isorhamnetin in rats
 was increased remarkably after oral administration of GBP and GBS
 comparing with GBE. The bioavailabilities of GBP increased more than
 that of GBS. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0367-326X
 PD DEC
 PY 2010
 VL 81
 IS 8
 BP 1045
 EP 1052
 DI 10.1016/j.fitote.2010.06.028
 UT ISI:000285281800015
 PT J
 AU Wu, GZ
 Su, X
 AF Wu, Guanzhong
 Su, Xin
 TI Antipruritic activity of extracts of Humulus scandens, the
 combinations of bioactive flavonoids
 SO FITOTERAPIA
 AB The antipruritic effects of the ethanol fractions of Humulus scandens
 on the 4-AP (4-aminopyridine)-induced and chloroquine-induced
 scratching in ICR mice were examined. The 40% ethanol fractions of H.
 scandens suppressed both the 4-AP- and chloroquine-induced scratching
 behavior, which significantly inhibited degranulation of rat
 peritoneal mast cell and antigen-stimulated histamine release. Further
 studies proved that the 40% ethanol fractions of H. scandens decreased
 the content of IL4 in serum of chloroquine-induced scratching ICR mice.
 The results suggest that the 40% ethanol fractions of H. scandens has
 antipruritic effects on both antihistamine-resistant and -sensitive
 pruritus. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0367-326X
 PD DEC
 PY 2010
 VL 81
 IS 8
 BP 1073
 EP 1078
 DI 10.1016/j.fitote.2010.07.003
 UT ISI:000285281800020
 PT J
 AU Xue, M
 Jiang, ZZ
 Liu, JP
 Zhang, LY
 Wang, T
 Wang, H
 Liu, L
 Zhou, ZX
 AF Xue, Mei
 Jiang, Zhen-zhou
 Liu, Ji-ping
 Zhang, Lu-Yong
 Wang, Tao
 Wang, Hao
 Liu, Li
 Zhou, Zhi-xing
 TI Comparative study on the anti-inflammatory and immune suppressive
 effect of Wilforlide A
 SO FITOTERAPIA
 AB Tripterygium Glycosides (TG) is effective in the treatment of patients
 with a variety of inflammatory and autoimmune diseases, especially
 rheumatoid arthritis (RA) in clinical. Wilforlide A (T-1) serves as
 a quality control standard of TG that be listed in Drug Standard of
 Ministry of Public Health of the People's Republic of China. The
 pharmacologic actions of T-1 remain to be unidentified. In this paper,
 we studied the anti-inflammatory and immune suppressive effect of T-1,
 and compared it with Triptolide (TP), which believed to be the major
 active component of TG. Carrageenan-induced rat pedal swelling,
 tampon-induced rat granulation, and mice ear inhibition rate of
 swelling trail results show that high-dose T-1 has obvious
 anti-inflammatory effect. Colorimetric detection contents of
 hemolysin, carbon elimination from plasma of mice, mice delayed
 hypersensitivity immune, and organ index were measured. The results
 show that T-1 has no significant immune suppressive activity, and there
 has a significant difference with TP and TG. Therefore, we think the
 content of TP also should be controlled as a supplement standard in
 order to ensure safe and effective medication. (C) 2010 Elsevier B.V.
 All rights reserved.
 SN 0367-326X
 PD DEC
 PY 2010
 VL 81
 IS 8
 BP 1109
 EP 1112
 DI 10.1016/j.fitote.2010.07.007
 UT ISI:000285281800026
 PT J
 AU Zhang, YM
 Yin, RT
 Jia, RR
 Yang, EH
 Xu, HM
 Tan, NH
 AF Zhang, Yu-Mei
 Yin, Run-Ting
 Jia, Rui-Rui
 Yang, En-Hu
 Xu, Han-Mei
 Tan, Ning-Hua
 TI A new abietane diterpene from Glyptostrobus pensilis
 SO FITOTERAPIA
 AB A new abietane diterpene, glypensin A (1) and four known compounds,
 12-acetoxy-ent-labda-8(17), 13E-dien-15-oic acid (2), quercetin
 3-O-alpha-L-arabinofuranoside (3), quercetin
 3-O-beta-D-galactopyranoside (4), beta-sitosterol (5) were isolated
 from the branches and leaves of Glyptostrobus pensilis (Staut.) Koch.
 Their structures were determined by MS, 1D- and 2D-NMR means. Compound
 1 showed cytotoxicity on human chronic myeloid leukemia cell line K562
 (IC50 = 21.2 mu M). (C) 2010 Elsevier B.V. All rights reserved.
 SN 0367-326X
 PD DEC
 PY 2010
 VL 81
 IS 8
 BP 1202
 EP 1204
 DI 10.1016/j.fitote.2010.08.001
 UT ISI:000285281800041
 PT J
 AU Li, HC
 Chang, JH
 Liu, GG
 AF Li, H. C.
 Chang, J. H.
 Liu, G. G.
 TI MEASUREMENT OF HRQOL USING EQ-5D IN TYPE 2 DIABETES MELLITUS PATIENTS
 TREATED WITH ORAL ANTI-DIABETIC DRUGS IN CHINA
 SO VALUE IN HEALTH
 SN 1098-3015
 PD NOV
 PY 2010
 VL 13
 IS 7
 BP A296
 EP A297
 UT ISI:000282818001287
 PT J
 AU Chang, J
 Sun, F
 Li, H
 AF Chang, J.
 Sun, F.
 Li, H.
 TI EVALUATING THE COST-EFFECTIVENESS OF THERAPY CONVERSION FROM BASAL
 INSULIN TO BIPHASIC INSULIN ASPART 30/70 IN PATIENTS WITH TYPE 2
 DIABETES IN CHINA: A MODELING STUDY OF LONG-TERM COSTS AND HEALTH
 OUTCOMES
 SO VALUE IN HEALTH
 SN 1098-3015
 PD NOV
 PY 2010
 VL 13
 IS 7
 BP A507
 EP A507
 UT ISI:000282818001531
 PT J
 AU Yao, W
 Shao, R
 Chen, Y
 Chang, F
 AF Yao, W.
 Shao, R.
 Chen, Y.
 Chang, F.
 TI RECOMMENDATIONS FOR A BIOLOGICS-SPECIFIC PRICING SYSTEM IN CHINA
 SO VALUE IN HEALTH
 SN 1098-3015
 PD NOV
 PY 2010
 VL 13
 IS 7
 BP A533
 EP A534
 UT ISI:000282818001668
 PT J
 AU Liu, XY
 Zhi, HY
 Du, F
 Ye, ZG
 Wang, NJ
 Qin, WJ
 Li, JR
 AF Liu, Xinyi
 Zhi, Hongying
 Du, Feng
 Ye, Zuguang
 Wang, Naijie
 Qin, Wenjie
 Li, Jianrong
 TI A HPLC-UV method for the determination of puerarin in rat plasma after
 intravenous administration of PEGylated puerarin conjugate
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB A sensitive and reproducible HPLC method for quantitative
 determination of puerarin (PUE) in rat plasma was developed and
 validated using 4-hydroxybenzaldehyde as an internal standard The
 separation of PUE was performed on a CAPCELL PAK C18 column by gradient
 elution with 0 2% aqueous phosphoric acid and acetonitrile as the mobile
 phase The method was validated and found to be linear in the range of
 80-12 000 ng/mL The limit of quantification was 80 ng/mL based on 100
 mu L of plasma The variations for intra- and inter-day precision were
 less than 8 3% and the accuracy values were between 98% and 105 2% The
 extraction recoveries were more than 85% The method was successfully
 applied in the comparative study of pharmacokinetics of PEGylated
 puerarin (PEG-PUE) versus PUE in rats Compared with PUE PEG-PUE showed
 a 5 2-fold increase in half-life of PUE and a 4 7-fold increase in mean
 residence time In addition this method was also successfully applied
 to determine the low plasma concentration of PUE regenerated from
 PEG-PUE in vitro (C) 2010 Elsevier B V All rights reserved
 SN 1570-0232
 PD DEC 1
 PY 2010
 VL 878
 IS 31
 BP 3297
 EP 3302
 DI 10.1016/j.jchromb.2010.10.011
 UT ISI:000285118100014
 A He, TT
 U Zou, QG
 Feng, ZB
 Zhang, ZJ
 A He, Tingting
 F Zou, Qiaogen
 Feng, Zhenbin
 Zhang, Zunjian
 T Study of sodium tanshinone II A sulfonate tissue distribution in rat
 I by liquid chromatography/tandem mass spectrometry
 ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
 A A rapid and sensitive method based on liquid chromatography/tandem mass
 B spectrometry (LC-MS/MS) has been developed and fully validated for the
 quantitative determination of sodium tanshinone HA sulfonate (STS,
 sodium
 (1,6,6-trimethyl-10,11-dioxo-7,8,9-trihydrophenanthro[1,2-b]furan)
 -yl-2- sulfonate) in rat biosamples including plasma and different
 tissues using sodium tanshinone I sulfonate (sodium
 (1,6-dimethyl-10,11-dioxo-phenanthro[1,2-b]furan)-yl-2-sulfonate)
 as internal standard. Simple protein precipitation by acetonitrile was
 utilized for extracting STS from the rat biosamples. Chromatographic
 separation of the sample matrix from the analyte and the internal
 standard was performed using a commercially available analytical
 column with a mobile phase consisting of methanol-5 mmoL/L ammonia
 acetate (70:30, v/v) at a flow rate of 0.2 mL/min. Detection was
 performed on a triple quadrupole tandem mass spectrometer equipped with
 an electrospray ionization source and operated in the negative-ion
 mode. The intra- and inter-day precisions (RSD%) and deviations of the
 assay accuracies were within 10.0% for STS. The extraction recovery
 of STS was more than 86.5%. The limit of detection (LOD) of STS was
 1.0 ng/mL. The method was successfully applied to the tissue
 distribution study of STS intravenously administered to healthy
 Sprague-Dawley rats. The tissue distribution results showed that
 liver, kidney, lung, small intestine and duodenum were the major
 distribution tissues of STS in rats, and that STS had difficulty in
 crossing the blood-brain barrier. After 24 h, STS could be detected
 only in the kidney, stomach and small intestine, indicating that there
 was no long-term accumulation of STS in rat.
 0004-4172
 2010
 ISI:000285034000003
 PT J
 AU Jiao, J
 Xiang, H
 Liao, Q
 AF Jiao, J.
 Xiang, H.
 Liao, Q.
 TI Recent Advancement in Nonsteroidal Aromatase Inhibitors for Treatment
 of Estrogen-Dependent Breast Cancer
 SO CURRENT MEDICINAL CHEMISTRY
 AB Estrogen-dependent breast cancer (EDBC) is a kind of common malignant
 tumor in postmenopausal women with growing tendency in recent years.
 Aromatase (AR) is the key enzyme responsible for estrogen biosynthesis
 and has been considered as an important target for designing inhibitors
 as potent therapeutic agents for EDBC. AR inhibitors (AIs) are divided
 into steroidal and nonsteroidal compounds, and the latter shows high
 inhibitory potency against AR. This review summarizes recent
 advancement in nonsteroidal AIs.
 SN 0929-8673
 PD OCT
 PY 2010
 VL 17
 IS 30
 BP 3476
 EP 3487
 UT ISI:000284654300003
 PT J
 AU Ren, M
 Dong, J
 Xu, YG
 Wen, N
 Gong, GY
 AF Ren, Mei
 Dong, Jin
 Xu, Yungen
 Wen, Nan
 Gong, Guoying
 TI Synthesis of Novel Ligustrazine Derivatives as Na+/H+ Exchange
 Inhibitors
 SO CHEMISTRY & BIODIVERSITY
 AB A novel series of 3,5,6-trimethylpyrazine-2-methoxy (or methylamino)
 substituted benzoylguanidine derivatives were designed and
 synthesized as Na+/H+ exchange (NHE) inhibitors. In this study,
 compounds with electron-withdrawing substituents on the benzene ring
 seemed to improve NHE-1 inhibitory activities. Compounds 6d, 6k, and
 6l were found to be potent inhibitors of NHE-1 (IC50 = 3.0 +/- 1.6,
 3.0 +/- 1.4, and 1.6 +/- 0.4 nmol/l, resp.). Furthermore, they showed
 a remarkable reduction of infarct size in the rat myocardial infarction
 model in vivo.
 SN 1612-1872
 PY 2010
 VL 7
 IS 11
 BP 2727
 EP 2736
 UT ISI:000284967200007
 PT J
 AU Zhang, HJ
 He, H
 Li, SS
 Lu, JR
 Chuong, PH
 AF Zhang Huaijing
 He Hua
 Li Shanshan
 Lu Jinrong
 Chuong, Pham-Huy
 TI Study on the Interactions of Different PAMAM Dendrimers with Bovine
 Serum Albumin
 SO ACTA CHIMICA SINICA
 AB Polyamidoamine (PAMAM) dendrimers have been synthesized by divergent
 with ethylenediamine as core. The interaction between PAMAM including
 amine-terminated generation 4.0 (G4.0), generation 3.0 (G3.0) PAMAM
 and ester-terminated generation 3.5 (G3.5) PAMAM dendrimers and bovine
 serum albumin (BSA) under physiological condition was studied by
 fluorescence spectroscopy. The results showed that the fluorescence
 intensity of BSA decreased with the addition of different PAMAM
 dendrimers, the quenching extent strongly depends on the type and
 amounts of their surface groups. The quenching mechanism was static
 quenching mechanism. The quenching constants of G4.0 PAMAM, G3.5 PAMAM,
 G3.0 PAMAM with BSA were 2.73, 1.69, 1.55 L.mmol(-1), respectively.
 The influence of pH and ionic strength on the interactions was also
 investigated. Furthermore, synchronous fluorescence,
 ultraviolet-visible spectra analysis (UV), and red edge excitation
 shift (REES) showed that PAMAM dendrimers could change the conformation
 of BSA.
 SN 0567-7351
 PD SEP 14
 PY 2010
 VL 68
 IS 17
 BP 1741
 EP 1748
 UT ISI:000284511400012
 A Cai, ZY
 U Yang, Y
 Liu, XH
 Qi, XB
 A Cai, Zheng-Yu
 F Yang, Yang
 Liu, Xin-Hua
 Qi, Xing-Bao
 T Novel
 I 3-(1-acetyl-5-(substituted-phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-7fluoro -2H-chromen-2-one Derivatives: Synthesis and Anticancer
 Activity
 LETTERS IN DRUG DESIGN & DISCOVERY
 A A series of novel coumarin derivatives containing 4,5-dihydropyrazole
 B moiety as potential telomerase inhibitors were synthesized. The
 bioassay tests showed that compound 3b exhibited potentially high
 activity against human gastric cancer cell SGC-7901 with IC50 value
 was 2.98 +/- 0.16. Docking simulation was performed to position
 compound 3b into the telomerase (3DU6) active site to determine the
 probable binding model. The result shows that some coumarin containing
 4,5-dihydropyrazole moiety can combine well with the telomerase active
 site and may have use as potential telomerase inhibitors.
 1570-1808
 2010
 ISI:000284692700003
 PT J
 AU Chen, JQ
 Zha, XM
 Sun, M
 Cai, J
 Zhou, W
 Ji, M
 AF Chen, Junqing
 Zha, Xiaoming
 Sun, Min
 Cai, Jin
 Zhou, Wen
 Ji, Min
 TI Synthesis and In Vivo Acute Antihyperglycemic Evaluation of Novel
 Isosteviol Derivatives
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB Isosteviol is a beyerane tetracyclic diterpenoid with a large variety
 of biological activities. In this article, a series of novel isosteviol
 derivatives containing the modification of C-18 carboxyl group (5-12),
 C-16 carbonyl group (14-16) and heteroatom-containing frameworks fused
 with isosteviol structure (18-19) were synthesized and evaluated for
 their in vivo acute antihyperglycemeric effects. Among them, compound
 8 exhibited the most potent antihyperglycemeric effects. Furthermore,
 primarily, structure-activity relationship (SAR) was also analyzed.
 The structures of all the newly synthesized compounds were determined
 by H-1, (CNMR)-C-13, MS, IR and elementary analysis.
 SN 1570-1808
 PD NOV
 PY 2010
 VL 7
 IS 9
 BP 686
 EP 693
 UT ISI:000284692700011
 PT J
 AU Zhang, JH
 He, MC
 AF Zhang, Jinghuan
 He, Mengchang
 TI Effect of structural variations on sorption and desorption of
 phenanthrene by sediment organic matter
 SO JOURNAL OF HAZARDOUS MATERIALS
 AB Sorption and desorption isotherms of phenanthrene (PHE) on sediment
 organic matter (SOM) prepared at different combustion temperature were
 studied to examine the impact of SOM structure on sorption and
 desorption. With the increase of combustion temperature from 0 to 400
 degrees C, the aromatic groups (-C=C) in SOM samples increased, while
 the aliphatic groups (-CH, -CH2) and polar structures (-C-O, -OH)
 decreased. When the combustion temperature increased to 500 degrees
 C. aliphatic structures, polar structures and most aromatic structures
 were burnt out, and the mineral materials were dominant in the sample.
 The increase of combustion temperature decrease the sorption isotherm
 nonlinearity index n value, and enhanced the adsorption capacity and
 desorption hysteresis for PHE on SOM. However, higher n value, lower
 sorption capacity and sorption irreversibility were presented in the
 sample treated at 500 degrees C (T500). Positive correlations between
 single-point organic carbon-normalized distribution coefficient log
 K-oc values and aromatic carbon (p < 0.01) and negative correlations
 between log K-oc values and aliphaticity or H/C ratios (p < 0.05) were
 observed. There was a negative relation between hysteresis index (HI)
 value and aromatic carbon (p < 0.01) and a negative trend of the sorption
 isotherm nonlinearity index n values and aromatic carbon (p < 0.01).
 The above results indicated the dominance of aromatic structures in
 the sorption nonlinearity, sorption capacity and desorption hysteresis
 of PHE on SOM. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0304-3894
 PD DEC 15
 PY 2010
 VL 184
 IS 1-3
 BP 432
 EP 438
 DI 10.1016/j.jhazmat.2010.08.123
 UT ISI:000284504800057
 PT J
 AU Zhang, L
 Yang, J
 Chen, XQ
 Zan, K
 Wen, XD
 Chen, H
 Wang, QA
 Lai, MX
 AF Zhang, Li
 Yang, Jie
 Chen, Xiao-qing
 Zan, Ke
 Wen, Xiao-dong
 Chen, Hong
 Wang, Qiang
 Lai, Mao-xiang
 TI Antidiabetic and antioxidant effects of extracts from Potentilla
 discolor Bunge on diabetic rats induced by high fat diet and
 streptozotocin
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Aim of the study: Potentilla discolor Bunge, commonly found at the north
 temperate and boreal zone, has been used for diabetes in China for a
 long time. Flavonoids and triterpenoids are two major types of
 compounds in P. discolor. This study was designed primarily to
 investigate the effects of total flavonoids extract (TFE) and total
 triterpenoids extract (TTE) of P. discolor Bunge on blood glucose,
 lipid profiles and antioxidant parameters on diabetic rats induced by
 high fat diet and streptozotocin.
 Materials and methods: High fat diet-fed and streptozotocin-induced
 diabetic rats were treated with the TFE and TTE for 15 days,
 respectively. A range of parameters were tested including fasting blood
 glucose (FBG), serum insulin (SI), blood lipid profile,
 malondialdehyde (MDA), superoxide dismutase (SOD), glutathione (GSH),
 glycosylated serum protein (GSP), and nitric oxide (NO).
 Results: Diabetic rats treated with TFE or TTE had decreased
 concentration of FBG and GSP compared with the control group.
 Meanwhile, the levels of serum total cholesterol (TC), triglycerides
 (TG) and low-density lipoprotein cholesterol (LDL-c) in the TFE or TTE
 treated diabetic rats were lower, and the high-density lipoprotein
 cholesterol (HDL-c) level was higher than in the control diabetic rats.
 Furthermore, the extracts treatment decreased the MDA and NO level,
 while increased SOD and GSH levels in diabetic rats. Histopathologic
 examination also showed that the extracts have protective effects on
 beta-cells in diabetic rats which are supported by the increase of SI.
 Conclusions: All these experimental results highlighted the
 hypoglycemic and hypolipidemic properties of the two extracts from
 Potentilla discolor Bunge on diabetes and its complications, possibly
 through a strong antioxidant activity and a protective action on
 beta-cells. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
 SN 0378-8741
 PD NOV 11
 PY 2010
 VL 132
 IS 2
 BP 518
 EP 524
 DI 10.1016/j.jep.2010.08.053
 UT ISI:000284569200021
 PT J
 AU Feng, Z
 Wenying, L
 AF Feng, Zheng
 Wenying, Liu
 TI Determination of 1,2-bis (2-aminophenoxy)ethane-N,N,N ',N
 '-tetraacetic acid (BAPTA free acid) in rat plasma, urine and feces
 by liquid chromatography with UV and tandem mass spectrometric
 detection
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB BAPTA free acid was identified as the main metabolic product of
 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid
 tetra(actoxymethyl ester) (BAPTA-AM), a neuroprotective agent in
 cerebral ischemia, in rats. In this paper, liquid
 chromatography-ultraviolet (LC-UV) and mass spectrometry/mass
 spectrometry (LC-MS/MS) methods were employed for the determination
 of BAPTA free acid in rat urine and feces and rat plasma, respectively.
 By liquid-liquid extraction and LC-UV analysis, a limit of quantitation
 of 1000 ng/ml using 0.2 ml rat urine for extraction and 250 ng/ml using
 1 ml rat fecal homogenate supernatant for extraction could be reached.
 The assay was linear in the range of 1000-50,000 ng/ml for rat urine
 and 250-10,000 ng/ml for rat fecal homogenate supernatant. Because the
 sensitivity of the LC-UV method was apparently insufficient for
 evaluating the pharmacokinetic profile of BAPTA in rat plasma, a
 LC-MS/MS method was subsequently developed for the analysis of BAPTA
 free acid. By protein precipitation and LC-MS/MS analysis, the limit
 of quantitation was 5 ng/ml using 0.1 ml rat plasma and the linear range
 was 5.0-500 ng/ml. Both methods were validated and can be used to
 support a thorough preclinical pharmacokinetic evaluation of BAPTA-AM
 liposome injection. (C) 2010 Elsevier B.V. All rights reserved.
 SN 1570-0232
 PD NOV 15
 PY 2010
 VL 878
 IS 30
 BP 3052
 EP 3058
 DI 10.1016/j.jchromb.2010.09.008
 UT ISI:000284672300002
 A Lei, J
 U Qian, SH
 Jiang, JQ
 A Lei, Jing
 F Qian, Shi-Hui
 Jiang, Jian-Qin
 Two new flavone glycosides from the seeds of Impatiens balsamina L.
 JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
 A Two new flavone glycosides were isolated from the seeds of Impatiens
 B balsamina L. and their structures were determined as
 quercetin-3-O-[-l-rhamnose-(12)--d-glucopyranosyl]-5-O--d-glucopyr
 anosid e (1), and
 quercetin-3-O-[(6'''-O-caffeoyl)--l-rhamnose-(12)--d-glucopyranosy
 l]-5-O --d-glucopyranoside (2) on the basis of various spectral and
 chemical studies.
 1028-6020
 P 2010
 1033
 1037
 10.1080/10286020.2010.532315
 ISI:000284891600004
 PT J
 AU Liu, K
 Xu, QA
 AF Liu, Kang
 Xu, Qiang
 TI Roxithromycin inhibits the effector phase of delayed-type
 hypersensitivity (Retraction of vol 8, pg 126, 2008)
 SO INTERNATIONAL IMMUNOPHARMACOLOGY
 SN 1567-5769
 PD NOV
 PY 2010
 VL 10
 IS 11
 BP 1477
 EP 1477
 DI 10.1016/j.intimp.2010.08.019
 UT ISI:000284657000022
 PT J
 AU Zhou, P
 Gross, S
 Liu, JH
 Yu, BY
 Feng, LL
 Nolta, J
 Sharma, V
 Piwnica-Worms, D
 Qiu, SX
 AF Zhou, Ping
 Gross, Shimon
 Liu, Ji-Hua
 Yu, Bo-Yang
 Feng, Ling-Ling
 Nolta, Jan
 Sharma, Vijay
 Piwnica-Worms, David
 Qiu, Samuel X.
 TI Flavokawain B, the hepatotoxic constituent from kava root, induces
 GSH-sensitive oxidative stress through modulation of IKK/NF-kappa B
 and MAPK signaling pathways
 SO FASEB JOURNAL
 AB Kava (Piper methysticum Foster, Piperaceae) organic solvent-extract
 has been used to treat mild to moderate anxiety, insomnia, and muscle
 fatigue in Western countries, leading to its emergence as one of the
 10 best-selling herbal preparations. However, several reports of
 severe hepatotoxicity in kava consumers led the U. S. Food and Drug
 Administration and authorities in Europe to restrict sales of
 kava-containing products. Herein we demonstrate that flavokawain B
 (FKB), a chalcone from kava root, is a potent hepatocellular toxin,
 inducing cell death in HepG2 (LD50 = 15.3 +/- 0.2 mu M) and L-02 (LD50
 = 32 mu M) cells. Hepatocellular toxicity of FKB is mediated by
 induction of oxidative stress, depletion of reduced glutathione (GSH),
 inhibition of IKK activity leading to NF-kappa B transcriptional
 blockade, and constitutive TNF-alpha-independent activation of
 mitogen-activated protein kinase (MAPK) signaling pathways, namely,
 ERK, p38, and JNK. We further demonstrate by noninvasive
 bioluminescence imaging that oral consumption of FKB leads to
 inhibition of hepatic NF-kappa B transcriptional activity in vivo and
 severe liver damage. Surprisingly, replenishment with exogenous GSH
 normalizes both TNF-alpha-dependent NF-kappa B as well as MAPK
 signaling and rescues hepatocytes from FKB-induced death. Our data
 identify FKB as a potent GSH-sensitive hepatotoxin, levels of which
 should be specifically monitored and controlled in kava-containing
 herb products.-Zhou, P., Gross, S., Liu, J.-H., Yu, B.-Y., Feng, L.-L.,
 Nolta, J., Sharma, V., Piwnica-Worms, D., Qiu, S. X. Flavokawain B,
 the hepatotoxic constituent from kava root, induces GSH-sensitive
 oxidative stress through modulation of IKK/NF-kappa B and MAPK
 signaling pathways. FASEB J. 24, 4722-4732 (2010). www.fasebj.org
 SN 0892-6638
 PD DEC
 PY 2010
 VL 24
 IS 12
 BP 4722
 EP 4732
 DI 10.1096/fj.10-163311
 UT ISI:000284824400013
 PT J
 AU Yang, GJ
 Yan, JK
 Qi, F
 Sun, C
 AF Yang, Gongjun
 Yan, Jiankang
 Qi, Fen
 Sun, Cheng
 TI High Sensitivity and Reproducibility of a Bismuth/Poly(bromocresol
 purple) Film Modified Glassy Carbon Electrode for Determination of
 Trace Amount of Cadmium by Differential Pulse Anodic Stripping
 Voltammetry
 SO ELECTROANALYSIS
 AB This work described a novel type of bismuth/poly(bromocresol purple)
 film modified glassy carbon electrode (denoted as Bi/Poly(BCP)/GCE)
 for anodic stripping analysis of trace Cd2+. The Bi/Poly(BCP)/GCE was
 fabricated in situ by depositing simultaneously bismuth and cadmium
 by reduction at -1.20 V on the poly(BCP) film using a differential pulse
 voltammetry. Under the optimum conditions, the anodic stripping peak
 current response increased linearly with the Cd2+ concentrations in
 a range of 2.0 x 10(-8)-1.0 x1.0(-7) M and 1.0 x 10(-7)-6.0x10(-6) M
 in 0.1 M NaAc-Ac buffer solution (pH 5.0) with the detection limit of
 6.5 x 10(-9) M (S/N =3). The Bi/poly(BCP)/GCE performed good
 reproducibility and high sensitivity. Finally, this proposed method
 was successfully applied to determine the concentration of Cd2+ in
 water samples.
 SN 1040-0397
 PD NOV
 PY 2010
 VL 22
 IS 22
 BP 2729
 EP 2738
 DI 10.1002/elan.201000260
 UT ISI:000284914800016
 PT J
 AU Li, P
 AF Li, Ping
 TI Plant Natural Products in Drug Discovery
 SO CURRENT ORGANIC CHEMISTRY
 SN 1385-2728
 PD OCT
 PY 2010
 VL 14
 IS 16
 BP 1669
 EP 1669
 UT ISI:000284825800001
 PT J
 AU Chu, C
 Qi, LW
 Li, B
 Gao, W
 Li, P
 AF Chu, Chu
 Qi, Lian-Wen
 Li, Bin
 Gao, Wen
 Li, Ping
 TI Radix Astragali (Astragalus): Latest Advancements and Trends in
 Chemistry, Analysis, Pharmacology and Pharmacokinetics
 SO CURRENT ORGANIC CHEMISTRY
 AB Radix Astragali (Astragalus) has been used in Traditional Chinese
 Medicine for over 2000 years, and still widely used in Asian countries
 to enhance the immune system and to protect the body against various
 stresses. In Europe and the United States, Astragalus is commonly used
 as nutritional dietary supplements and additives to foods and
 beverages. During the last several years, we have witnessed a steady
 expansion in the number of publications made associated with this herb.
 This review focuses on latest advancements and trends in chemistry,
 analysis, pharmacology and pharmacokinetics of Radix Astragali.
 Several types of constituents including triterpene saponins,
 flavonoids and astragalus polysaccharides have been summarized, and
 astragalus polysaccharides are still a challenging issue. With the
 rapid development of analytical techniques, a great number of methods
 have been developed for the identification and quantification of the
 plant material, extracts, and products of Radix Astragali. Separation
 was achieved using thin layer chromatography (TLC), high performance
 liquid chromatography (HPLC), callipary electrophoresis (CE), and
 high-speed counter-current chromatography (HSCCC). Among these
 techniques HPLC and hyphenated methods like HPLC with ultraviolet (UV),
 evaporative light scattering detection (ELSD), or mass spectrometry
 (MS) are by far the most employed. Radix Astragali has attracted
 ever-increasing attention in a variety of biological activity studies;
 its immunomodulatory effects, cardioprotective effects,
 antihyperglycemic effects, hepatoprotective effects and anticancer
 effects were strengthened in this review. Pharmacokinetic studies
 showed that the flavonoids could be absorbed and metabolized in vivo,
 and their major metabolic pathways are glucuronidation and sulfation,
 while the bioavailability of saponins is extremely low.
 SN 1385-2728
 PD OCT
 PY 2010
 VL 14
 IS 16
 BP 1792
 EP 1807
 UT ISI:000284825800010
 PT J
 AU Zheng, JH
 Zhang, G
 Lu, Y
 Fang, F
 He, JK
 Li, N
 Talbi, A
 Zhang, Y
 Tang, Y
 Zhu, JB
 Chen, XJ
 AF Zheng, Jianheng
 Zhang, Ge
 Lu, Yang
 Fang, Fang
 He, Jiake
 Li, Ning
 Talbi, Amer
 Zhang, Ying
 Tang, Yue
 Zhu, Jiabi
 Chen, Xijing
 TI Effect of Pulmonary Surfactant and Phospholipid Hexadecanol Tyloxapol
 on Recombinant Human-Insulin Absorption from Intratracheally
 Administered Dry Powders in Diabetic Rats
 SO CHEMICAL & PHARMACEUTICAL BULLETIN
 AB The purpose of the present study was to evaluate the enhancement effect
 of the natural pulmonary surfactant (PS) or its artificial substitute,
 phospholipid hexadecanol tyloxapol (PHT) on the bioavailability and
 hypoglycemic activity of recombinant human insulin (rh-insulin) in a
 pulmonary delivery system. PS- or PHT-loaded insulin formulation was
 administered to streptozotocin induced diabetic rats, at doses of 5
 U/kg, 10 U/kg and 20 U/kg insulin, respectively. The hypoglycemic
 effect caused by PS or PHT containing rh-insulin was analyzed and the
 area above the curves (AAC) of scrum glucose levels versus time, the
 minimum glucose concentration (C-min), the time to C-min (T-min) and
 the pharmacological availability (PA%) were derived from the serum
 glucose profiles. Results showed that PS and PHT caused significantly
 decrease in serum glucose levels. The decrease in plasma glucose levels
 continued for about 5 h after the nadir. The highest AAC value was
 obtained when 20 U/kg rh-Insulin with PS or PHT as absorption enhancer
 was administered to rats. AAC(0-360min) of PS- or PHT-loaded rh-insulin
 was 2-3 times as much as that without PS or PHT and PA% increased by
 1.3-2 fold. Thus, the extent of oral absorption of insulin from PSor PHT-loaded particles was significantly greater when compared with
 that without them. In addition, PHT as well as PS did not change the
 lactate dehydrogenase (LDH) activity, alkaline phosphatase (AKP)
 activity and N-acetyl-beta-D-glucoaminidase (NAG) activity in bronch
 fluid which are sensitive indicators of acute toxicity to lung cells
 in bronchoalveolar lavage (BAL). It is concluded that PS and PHT is
 a promising absorption enhancer for pulmonary delivery systems of large
 molecule drugs as rh-Insulin.
 SN 0009-2363
 PD DEC
 PY 2010
 VL 58
 IS 12
 BP 1612
 EP 1616
 UT ISI:000284860800011
 PT J
 AU Lai, YS
 Ma, L
 Huang, WX
 Yu, X
 Zhang, YH
 Ji, H
 Tian, JD
 AF Lai, Yisheng
 Ma, Lin
 Huang, Wenxing
 Yu, Xing
 Zhang, Yihua
 Ji, Hui
 Tian, Jide
 TI Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)
 phenyl]methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX
 inhibitors
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB Fourteen new 3-[4-(amino/methylsulfonyl)
 phenyl]methylene-indolin-2-one derivatives were synthesized. Six
 compounds displayed potent inhibitory activities against COX-1/2 and
 5-LOX with IC50 in the range of 0.10-9.87 mu M. Particularly, 10f
 exhibited well balanced inhibitory action on these enzymes (IC50 =
 0.10-0.56 mu M). More importantly, 10f and several other compounds had
 comparable or stronger anti-inflammatory and analgesic activities, but
 better gastric tolerability in vivo, as compared with darbufelone
 mesilate and tenidap sodium. Therefore, our findings may aid in the
 design of new and safe anti-inflammatory reagents for the intervention
 of painful inflammatory diseases, such as rheumatoid arthritis at
 clinic. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0960-894X
 PD DEC 15
 PY 2010
 VL 20
 IS 24
 BP 7349
 EP 7353
 DI 10.1016/j.bmcl.2010.10.056
 UT ISI:000284332900035
 PT J
 AU Zheng, YF
 Qi, LW
 Zhou, JL
 Li, P
 AF Zheng, Yun-Feng
 Qi, Lian-Wen
 Zhou, Jian-Liang
 Li, Ping
 TI Structural characterization and identification of oleanane-type
 triterpene saponins in Glycyrrhiza uralensis Fischer by
 rapid-resolution liquid chromatography coupled with time-of-flight
 mass spectrometry
 SO RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 AB Oleanane-type triterpene saponins (OTS) are major active ingredients
 in Glycyrrhiza uralensis. In this work, a rapid-resolution liquid
 chromatography with time-of-flight mass spectrometry (RRLC/TOF-MS)
 method has been developed to characterize and identify OTS from G.
 uralensis. The major diagnostic ions and fragmentation pathways from
 thirteen OTS have been characterized for the first time. At a low
 fragmentor voltage of 120 V in positive ion mode, the precursor ion
 [M + H](+) or/and [M + Na](+) was obtained for accurate determination
 of molecular formula. When the fragmentor voltage was increased to 425
 V, abundant characteristic fragment ions were observed for structural
 characterization. Neutral losses of sugar moieties, such as glucuronic
 acid (G1cA, 176 Da), glucose (G1c, 162 Da) and rhamnose (Rha, 146 Da),
 were commonly observed in the MS spectra for prediction of the sugar
 number and sequences. Other typical losses included AcOH (60 Da), CH2O
 (30 Da), 2 x H2O (2 x 18 Da) and HCOOH (46 Da) from [Aglycone + H H2O](+)
 (named [B](+)), corresponding to the presence of a C-22-acetyl group,
 C-24-hydroxyl group, C-22-hydroxyl group or C-30-carboxyl group on the
 aglycone moiety, respectively. In particular, characteristic ring
 cleavages of the aglycone moieties on A- and B-rings were observed.
 Based on the fragmentation patterns of reference compounds, nineteen
 OTS have been identified in an extract of G. uralensis, thirteen of
 which were unambiguously identified and the other six were tentatively
 assigned. Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0951-4198
 PD NOV
 PY 2010
 VL 24
 IS 22
 BP 3261
 EP 3270
 DI 10.1002/rcm.4768
 UT ISI:000284023400006
 PT J
 AU Ye, BP
 Rui, Q
 Wu, QL
 Wang, DY
 AF Ye, Boping
 Rui, Qi
 Wu, Qiuli
 Wang, Dayong
 TI Metallothioneins Are Required for Formation of Cross-Adaptation
 Response to Neurobehavioral Toxicity from Lead and Mercury Exposure
 in Nematodes
 SO PLOS ONE
 AB Metallothioneins (MTs) are small, cysteine-rich polypeptides, but the
 role of MTs in inducing the formation of adaptive response is still
 largely unknown. We investigated the roles of metallothionein genes
 (mtl-1 and mtl-2) in the formation of cross-adaptation response to
 neurobehavioral toxicity from metal exposure in Caenorhabditis
 elegans. Pre-treatment with mild heat-shock at L2-larva stage
 effectively prevented the formation of the neurobehavioral defects and
 the activation of severe stress response in metal exposed nematodes
 at concentrations of 50 and 100 mM, but pre-treatment with mild
 heat-shock did not prevent the formation of neurobehavioral defects
 in 200 mM of metal exposed nematodes. During the formation of
 cross-adaptation response, the induction of mtl-1 and mtl-2 promoter
 activity and subsequent GFP gene expression were sharply increased in
 50 mu M or 100 mM of metal exposed Pmtl-1::GFP and Pmtl-2::GFP
 transgenic adult animals after mild heat-shock treatment compared with
 those treated with mild heat-shock or metal exposure alone. Moreover,
 after pre-treatment with mild heat-shock, no noticeable increase of
 locomotion behaviors could be observed in metal exposed mtl-1 or mtl-2
 mutant nematodes compared to those without mild heat-shock
 pre-treatment. The defects of adaptive response to neurobehavioral
 toxicity induced by metal exposure formed in mtl-1 and mtl-2 mutants
 could be completely rescued by the expression of mtl-1 and mtl-2 with
 the aid of their native promoters. Furthermore, overexpression of MTL-1
 and MTL-2 at the L2-larval stage significantly suppressed the toxicity
 on locomotion behaviors from metal exposure at all examined
 concentrations. Therefore, the normal formation of cross-adaptation
 response to neurobehavioral toxicity induced by metal exposure may need
 the enough accumulation of MTs protein in animal tissues.
 SN 1932-6203
 PD NOV 18
 PY 2010
 VL 5
 IS 11
 AR e14052
 DI 10.1371/journal.pone.0014052
 UT ISI:000284356900014
 PT J
 AU Liu, F
 Deng, DW
 Chen, XY
 Qian, ZY
 Achilefu, S
 Gu, YQ
 AF Liu, Fei
 Deng, Dawei
 Chen, Xinyang
 Qian, Zhiyu
 Achilefu, Samuel
 Gu, Yueqing
 TI Folate-Polyethylene Glycol Conjugated Near-Infrared Fluorescence
 Probe with High Targeting Affinity and Sensitivity for In Vivo Early
 Tumor Diagnosis
 SO MOLECULAR IMAGING AND BIOLOGY
 AB The purpose of this study is to synthesize a folate-polyethylene glycol
 (PEG) conjugated near-infrared fluorescence probe (fPI-01) for
 diagnosis of folate receptor (FR)-overexpressed tumors with high
 sensitivity and specificity.
 fPI-01 was synthesized, purified, and characterized. Its cytotoxicity
 and affinity to tumor cells were determined in vitro. The dynamics and
 biodistribution of the probe was monitored in normal nude mice. And
 the tumor-targeting capability was investigated in nude mice bearing
 different tumor xenograft.
 fPI-01 was successfully synthesized with strengthened optical
 properties. Cells experiments showed the probe had high FR affinity
 and without apparent cytotoxicity. Animal experiments indicated the
 probe excreted through urine by kidney. And its tumor-targeting ability
 was demonstrated on different tumor-bearing mice, with high
 sensitivity and tumor-to-normal tissue contrast ratio (10:1).
 fPI-01 is a promising optical agent for diagnosis of FR-positive
 tumors, especially in their early stage.
 SN 1536-1632
 PD DEC
 PY 2010
 VL 12
 IS 6
 BP 595
 EP 607
 DI 10.1007/s11307-010-0305-1
 UT ISI:000284159300005
 PT J
 AU Zhang, JW
 Zhou, F
 Wu, XL
 Gu, Y
 Ai, H
 Zheng, YT
 Li, YN
 Zhang, XX
 Hao, G
 Sun, JG
 Peng, Y
 Wang, GJ
 AF Zhang, Jingwei
 Zhou, Fang
 Wu, Xiaolan
 Gu, Yi
 Ai, Hua
 Zheng, Yuanting
 Li, Yannan
 Zhang, Xiaoxuan
 Hao, Gang
 Sun, Jianguo
 Peng, Ying
 Wang, Guangji
 TI 20(S)-Ginsenoside Rh2 Noncompetitively Inhibits P-Glycoprotein In
 Vitro and In Vivo: A Case for Herb-Drug Interactions
 SO DRUG METABOLISM AND DISPOSITION
 AB P-glycoprotein (P-gp) is an ATP-dependent efflux transporter highly
 expressed in gastrointestinal tract and multidrug resistance tumor
 cells. Inhibition or induction of P-gp can cause drug-drug interactions
 and thus influence the effects of P-gp substrate drugs. Previous
 studies indicated that 20(S)-ginsenoside Rh2 [20(S)-Rh2] could
 synergistically enhance the anticancer effects of conventional
 chemotherapeutic agents at a nontoxic dose. The aim of present study
 was to investigate in vitro and in vivo whether 20(S)Rh2 was a P-gp
 inhibitor and analyze the possible inhibitory mechanisms and potential
 herb-drug interactions. Results showed that in vitro, 20(S)-Rh2
 significantly enhanced rhodamine 123 retention in cells and decreased
 the efflux ratio of digoxin, fexofenadine, and etoposide, which were
 comparable to the effects of the established P-gp inhibitor verapamil.
 However, the transport of 20(S)Rh2 suggested that 20(S)-Rh2 was not
 a P-gp substrate. Further-more, the inhibitory effect persisted for
 at least 3 h after removal of 20(S)-Rh2. Unlike P-gp substrates,
 20(S)-Rh2 inhibited both basal and verapamil-stimulated P-gp ATPase
 activities. It also significantly decreased UIC2 binding fluorescence,
 a marker for conformational change of P-gp. In situ and in vivo
 experiments showed that 20(S)-Rh2 increased the area under the plasma
 concentration-time curve and maximum plasma concentration of digoxin,
 fexofenadine, and etoposide significantly without affecting terminal
 elimination half-time. Long-term treatment with 20(S)-Rh2 failed to
 affect intestinal P-gp expression in vitro and in vivo. In conclusion,
 20(S)-Rh2 is a potent noncompetitive P-gp inhibitor, which indicates
 a potential herb-drug interaction when 20(S)-Rh2 is coadministered
 with P-gp substrate drugs. It could increase the absorption of P-gp
 substrate drugs without long-term induction of P-gp expression in rats.
 SN 0090-9556
 PD DEC
 PY 2010
 VL 38
 IS 12
 BP 2179
 EP 2187
 DI 10.1124/dmd.110.034793
 UT ISI:000284309900014
 PT J
 AU Liu, EH
 Qi, LW
 Li, K
 Chu, C
 Li, P
 AF Liu, E-Hu
 Qi, Lian-Wen
 Li, Kai
 Chu, Chu
 Li, Ping
 TI Recent Advances in Quality Control of Traditional Chinese Medicines
 SO COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
 AB Traditional Chinese medicines (TCMs) have been used for disease
 prevention and therapy in China for a long history and are becoming
 increasingly popular over the world. However, TCMs are complex mixtures
 and contain usually hundreds of chemically different constituents,
 which make the quality control of crude drugs and their medical
 preparations extremely difficult. Therefore, better analytical
 strategies to assure their efficacy, safety and consistency are in
 great demand. The present work provides an overview of the development
 of quality control for TCMs based on microscopic and molecular
 identification, quantitative and qualitative analysis, fingerprint,
 combination of fingerprint and multi-component quantification, as well
 as activity-integrated fingerprint over the last five years. The
 biological fingerprinting analysis of TCMs with targeting absorption,
 distribution, metabolism, excretion by chromatographic and
 chemometric method are also highlighted due to its broad application
 in the quality control of TCMs. The comprehensive methods analyzed with
 modern hyphenated techniques are strongly recommended to assess the
 authenticity, quality consistency and stability of TCMs.
 SN 1386-2073
 PD DEC
 PY 2010
 VL 13
 IS 10
 BP 869
 EP 884
 UT ISI:000284622300006
 PT J
 AU Wang, TC
 Wei, JZ
 Guo, CS
 Zhang, HB
 Fan, HX
 AF Wang, Tian Cai
 Wei, Ju Zhi
 Guo, Chuan Sheng
 Zhang, Hui Bin
 Fan, Hou Xing
 TI Design, synthesis and anti-proliferative studies of a novel series of
 indirubin derivatives
 SO CHINESE CHEMICAL LETTERS
 AB A series of novel derivatives of indirubin were synthesized and
 evaluated for their anti-proliferative activity against human cancer
 cell lines of SGC7901, A549, HL-60, SK-BR-3 and HCT116. Most of the
 compounds displayed more potent activity than Sunitinib. In addition,
 the derivatives showed improved water solubility, which may be
 favorable to their pharmacokinetic performances. (C) 2010 Hui Bin
 Zhang. Published by Elsevier B.V. on behalf of Chinese Chemical
 Society. All rights reserved.
 SN 1001-8417
 PD DEC
 PY 2010
 VL 21
 IS 12
 BP 1407
 EP 1410
 DI 10.1016/j.cclet.2010.05.026
 UT ISI:000284389800005
 PT J
 AU Xi, BM
 Ni, PZ
 Jiang, ZZ
 Wu, DQ
 Zhang, SH
 Zhang, HB
 Wang, T
 Chen, WH
 AF Xi, Bao-Min
 Ni, Pei-Zhou
 Jiang, Zhen-Zhou
 Wu, Dian-Qing
 Zhang, Shou-Hua
 Zhang, Hui-Bin
 Wang, Tao
 Chen, Wen-Hua
 TI Synthesis and Blocking Activities of a New Class of
 alpha(1)-Adrenoceptor Antagonists
 SO CHEMICAL BIOLOGY & DRUG DESIGN
 AB Finding effective chemotherapeutic agents for clinical use is a
 long-lasting goal in medicinal chemistry. In this study, we report a
 new class of alpha(1)-adrenoceptor (alpha(1)-AR) antagonists.
 Specifically, we describe the synthesis and the blocking activities
 toward alpha(1)-AR of
 7-(2-hydroxypropoxy)-3,4-dihydroisoquinolin-1(2H)-one 1 and its
 structurally perturbed analogs 2-11 that were designed according to
 the principle of bioisosterism. Their structures were identified with
 IR, 1H NMR, MS, HRMS and elemental analysis. The blocking activities
 of compounds 1-11 were evaluated on isolated rat anococcygeus muscles.
 The results indicated that these compounds showed moderate to good
 activities. Among them, compound 1 exhibited the highest activity that
 was comparable to those of known alpha(1)-AR antagonists tamsulosin
 and DDPH (1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride) and thus may be
 exploitable as a lead compound for the discovery of promising
 alpha(1)-AR antagonists.
 SN 1747-0277
 PD DEC
 PY 2010
 VL 76
 IS 6
 BP 505
 EP 510
 DI 10.1111/j.1747-0285.2010.01040.x
 UT ISI:000284170000006
 PT J
 AU Yao, J
 Fan, Y
 Du, RH
 Zhou, JP
 Lu, Y
 Wang, W
 Ren, J
 Sun, XJ
 AF Yao, Jing
 Fan, Ying
 Du, Ronghui
 Zhou, Jianping
 Lu, Yun
 Wang, Wei
 Ren, Jin
 Sun, Xiaojing
 TI Amphoteric hyaluronic acid derivative for targeting gene delivery
 SO BIOMATERIALS
 AB The study aimed to develop an amphoteric hyaluronic acid (HA)
 derivative with polyethyleneimine (PEI) chains (HAP) for gene delivery
 to overcome the disadvantages of PEI as gene carrier including the
 cytotoxicity caused by excess of positive charge, non-special
 interaction and aggregation in the blood, and non-target gene delivery.
 The HAP was synthesized by an imine reaction between periodate-oxidized
 HA and PEI. The HAP/DNA complex was prepared, and its characterization
 was investigated. The size of complex with higher molecular weight HA
 in PBS was about 200 nm at optimal charge ratio. No apparent aggregation
 among the particles was observed. The HAPs also showed high protection
 of DNA from nuclease, better dissociation of DNA from the complex and
 lower cytotoxicity. It also exhibited higher transfection efficiency
 in HepG2 cells than the PEI/DNA complex. Among all complexes, the
 HAP50/DNA complex was especially found to be most efficient, yielding
 comparable transfection efficiency with that of Lipofectamine/DNA
 lipoplexes. Moreover, the HAP-IR820 obviously accumulated in tumor
 after i.v. administration as compared to the PEI-IR820, which indicated
 that the HAP could assist the DNA targeting to the tumor. Therefore,
 HAP should be a promising non-viral gene vector. (C) 2010 Elsevier Ltd.
 All rights reserved.
 SN 0142-9612
 PD DEC
 PY 2010
 VL 31
 IS 35
 BP 9357
 EP 9365
 DI 10.1016/j.biomaterials.2010.08.043
 UT ISI:000284393300022
 PT J
 AU Lu, Y
 Sun, YX
 Xiong, QY
 Zhang, Y
 Hou, J
 Mekoo, DJL
 Zhang, F
 Hu, XB
 Ma, YJ
 Liu, JJ
 Li, TM
 AF Lu Yong
 Sun Yunxiao
 Xiong Qiyan
 Zhang Yu
 Hou Jing
 Mekoo, Didier J. L.
 Zhang Fan
 Hu Xiangbing
 Ma Yanjun
 Liu Jingjing
 Li Taiming
 TI Immunization with P277 induces vascular leak syndrome in C57BL/6 mice
 via endothelial damage
 SO AUTOIMMUNITY
 AB Accumulating evidence established a positive association of anti-heat
 shock protein 60 (HSP60) autoantibodies and the presence of
 atherosclerosis. However, whether anti-P277 (HSP60 437-460)
 autoantibodies may lead to the pathological increase in vascular
 permeability, a vascular leak syndrome (VLS), is unknown. In the
 present study, anti-P277 immunity was effectively induced in C57BL/6
 mice, causing a marked increase in VLS in both normal mice and those
 bearing melanoma as well. Further analysis of the pathological role
 of anti-P277 immunity revealed that the B-cell epitopes located in P277
 played a causal role in the development of VLS. Moreover, studies on
 endothelial cells (ECs) showed that the anti-P277 antibodies could
 cross-react with HSP60, highly expressed in both normal and stressed
 ECs, and mediate damage to cells in the presence of complement. These
 data suggested that humoral immune response induced by anti-P277
 immunity mediates EC damage and induces VLS. These negative effects
 may cast shadows on P277, used as a peptide vaccine.
 SN 0891-6934
 PD DEC
 PY 2010
 VL 43
 IS 8
 BP 654
 EP 663
 DI 10.3109/08916931003674683
 UT ISI:000284074300010
 PT J
 AU Qiu, FR
 Zhang, R
 Wang, GJ
 Gao, CL
 Sun, JG
 Jiang, JA
 Ma, YM
 AF Qiu, Furong
 Zhang, Rong
 Wang, Guangji
 Gao, Chenglu
 Sun, Jianguo
 Jiang, Jian
 Ma, Yueming
 TI Activation of CYP3A-mediated testosterone 6 beta-hydroxylation by
 tanshinone IIA and midazolam 1-hydroxylation by cryptotanshinone in
 human liver microsomes
 SO XENOBIOTICA
 AB 1. This study evaluated the in vitro activation of CYP3A-mediated
 midazolam 1-hydroxylation and testosterone 6 beta-hydroxylation by
 tanshinone I, tanshinone IIA, and cryptotanshinone.
 2. The abilities of tanshinones to activate CYP3A-mediated midazolam
 1-hydroxylation and testosterone 6 beta-hydroxylation in human liver
 microsomes (HLMs) were tested. Substrate-and effector-dependent
 activation of CYP3A by tanshinones were both observed.
 3. Cryptotanshinone was shown to activate CYP3A-mediated midazolam
 1-hydroxylation in a concentration-dependent manner. In contrast,
 tanshinone IIA and tanshinone I did not activate this hydroxylation
 reaction. In addition, tanshinone IIA activated CYP3A-mediated
 testosterone 6 beta-hydroxylation, whereas cryptotanshinone and
 tanshinone I did not.
 4. The results from our study enhance the understanding of CYP3A
 activation by tanshinone IIA and cryptotanshinone in HLMs.
 Additionally, these data allow for an accurate prediction of the
 magnitude and likelihood of Danshen-drug interactions.
 SN 0049-8254
 PD DEC
 PY 2010
 VL 40
 IS 12
 BP 800
 EP 806
 DI 10.3109/00498254.2010.519062
 UT ISI:000284003800002
 PT J
 AU Liu, CW
 Lu, YY
 Yang, ZZ
 Xing, YY
 Xi, T
 AF Liu, Cheng-Wei
 Lu, Yuan-Yuan
 Yang, Zhen-Zheng
 Xing, Ying-Ying
 Xi, Tao
 TI Rapid screening and characterization of metabolites from a
 marine-derived actinomycete by high-performance liquid chromatography
 coupled with electrospray ionization quadrupole time-of-flight mass
 spectrometry
 SO RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 AB A rapid and reliable method has been optimized and established for the
 analysis of the metabolites from a marine actinomycete by
 high-performance liquid chromatography coupled with electrospray
 ionization quadrupole time-of-flight mass spectrometry (HPLC/QTOF
 MS/MS). From MS/MS spectra, the product ions of [M+H](+) were recorded
 to provide abundant structural information of the mother nucleus and
 peptide moieties. Using the QTOF MS/MS and in-source collision-induced
 dissociation (in-source CID) techniques, three main metabolites
 including actinomycin D, actinomycin V and actinomycin I were
 determined and characterized by elemental compositions of precursor
 and product ions (<7 ppm). Additionally, this method provided
 information about the compositions of the peptide residues and the
 sequences of the amino acid from a series of fragment ions. It proved
 useful for the identification of the metabolites in marine samples
 which have similar structures especially when there were no reference
 compounds available. Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0951-4198
 PD DEC 15
 PY 2010
 VL 24
 IS 23
 BP 3413
 EP 3418
 DI 10.1002/rcm.4744
 UT ISI:000284037800005
 PT J
 AU Qi, J
 Li, N
 Zhou, JH
 Yu, BY
 Qiu, SX
 AF Qi, Jin
 Li, Na
 Zhou, Jia-Hong
 Yu, Bo-Yang
 Qiu, Samuel X.
 TI Isolation and Anti-Inflammatory Activity Evaluation of Triterpenoids
 and a Monoterpenoid Glycoside from Harpagophytum procumbens
 SO PLANTA MEDICA
 AB A new triterpenoid glycoside, designated harproside (1), and a new
 iridoid glycoside, named pagide (2), along with six known triterpenoids
 (3-8), were obtained from the tubers of Harpagophytum procumbens D.C.
 (devil's claw), and their structures were established through chemical
 methods and spectroscopic analyses. In an in vitro assay, the six
 triterpenoids showed anti-inflammatory activity. Compounds 3, 7, and
 8 showed significant inhibitory activity against neutrophil
 respiratory burst stimulated by PMA, while compounds 4, 5, and 6 showed
 marginal inhibitory activity.
 SN 0032-0943
 PD NOV
 PY 2010
 VL 76
 IS 16
 BP 1892
 EP 1896
 DI 10.1055/s-0030-1250029
 UT ISI:000284144400020
 PT J
 AU Wei, KH
 Gao, SL
 Huang, HP
 AF Wei Kun-Hua
 Gao Shan-Lin
 Huang He-Ping
 TI Tissue culture and generation of autotetraploid plants of Sophora
 flavescens Aiton
 SO PHARMACOGNOSY MAGAZINE
 AB Background: Sophora flavescens Aiton is an important medicinal plant
 in China. Early in vitro researches of S. flavescens were focused on
 callus induction and cell suspension culture, only a few were concerned
 with in vitro multiplication. Objective: To establish and optimize the
 rapid propagation technology of S. flavescens and to generate and
 characterize polyploid plants of S. flavescens. Materials and Methods:
 The different concentrations of 6-benzylaminopurine (BAP),
 indole-3-acetic acid (IAA) and kinetin (KT) were used to establish and
 screen the optimal rapid propagation technology of S. flavescens by
 orthogonal test; 0.2% colchicine solution was used to induce polyploid
 plants and the induced buds were identified by root-tip chromosome
 determination and stomatal apparatus observation. Results: A large
 number of buds could be induced directly from epicotyl and hypocotyl
 explants on the Murashige and Skoog medium (MS; 1962) supplemented with
 1.4-1.6 mg/l 6-benzylaminopurine (BAP) and 0.3 mg/l indole-3-acetic
 acid (IAA). More than 50 lines of autotetraploid plants were obtained.
 The chromosome number of the autotetraploid plantlet was 2n = 4x = 36.
 All tetraploid plants showed typical polyploid characteristics.
 Conclusion: Obtained autotetraploid lines will be of important genetic
 and breeding value and can be used for further selection and plant
 breeding.
 SN 0973-1296
 PD OCT-DEC
 PY 2010
 VL 6
 IS 24
 BP 286
 EP 292
 DI 10.4103/0973-1296.71793
 UT ISI:000283922900008
 PT J
 AU Zhou, JL
 Xin, GZ
 Shi, ZQ
 Ren, MT
 Qi, LW
 Li, HJ
 Li, P
 AF Zhou, Jian-Liang
 Xin, Gui-Zhong
 Shi, Zi-Qi
 Ren, Mei-Ting
 Qi, Lian-Wen
 Li, Hui-Jun
 Li, Ping
 TI Characterization and identification of steroidal alkaloids in
 Fritillaria species using liquid chromatography coupled with
 electrospray ionization quadrupole time-of-flight tandem mass
 spectrometry
 SO JOURNAL OF CHROMATOGRAPHY A
 AB Liquid chromatography coupled with electrospray ionization quadrupole
 time-of-flight tandem mass spectrometry (LC/ESI-QTOF-MS/MS) was
 performed to study the fragmentation behaviors of steroidal alkaloids
 from Fritillaria species the antitussive and expectorant herbs widely
 used in traditional Chinese medicine We propose herein a strategy that
 combining key diagnostic fragment ions and the relative abundances and
 amounts of major fragment ions (the ions exceeding 10% in abundance)
 to distinguish different sub-classes of Fritillaria alkaloids (FAs)
 It was found that hydrogen rearrangement and induction effects result
 in ring cleavage of the basic skeletons occurred in the MS/MS process
 and produced characteristic fragment ions which are useful for
 structural elucidation This method was finally used to investigate the
 primary steroidal alkaloids in the extracts of eight major Fritillaria
 species As a result 41 steroidal alkaloids (29 cevanine type 1 jervine
 type 6 veratramine type and 5 secosolanidine type alkaloids) were
 selectively identified in these Fritillaria species Twenty-six
 compounds were unambiguously identified by comparing with the
 reference compounds and 15 compounds were tentatively identified or
 deduced according to their MS/MS data Logical fragmentation pathways
 for different types of FAs have been proposed and are useful for the
 identification of these types of steroidal alkaloids in natural
 products especially when there are no reference compounds available
 (C) 2010 Elsevier B V All rights reserved
 SN 0021-9673
 PD NOV 5
 PY 2010
 VL 1217
 IS 45
 BP 7109
 EP 7122
 DI 10.1016/j.chroma.2010.09.019
 UT ISI:000283973000014
 PT J
 AU Song, R
 Xu, L
 Xu, FG
 Li, Z
 Dong, HJ
 Tian, YA
 Zhang, ZJ
 AF Song, Ru
 Xu, Lei
 Xu, Fengguo
 Li, Zhe
 Dong, Haijun
 Tian, Yuan
 Zhang, Zunjian
 TI In vivo metabolism study of rhubarb decoction in rat using
 high-performance liquid chromatography with UV photodiode-array and
 mass-spectrometric detection A strategy for systematic analysis of
 metabolites from traditional Chinese medicines in biological samples
 SO JOURNAL OF CHROMATOGRAPHY A
 AB High-performance liquid chromatography with diode-array detection
 (HPLC-DAD) and tandem mass spectrometry (HPLC-MS/MS) was used for
 separation and identification of metabolites in rat urine bile and
 plasma after oral administration of rhubarb decoction Based on the
 proposed strategy 91 of the 113 potential metabolites were tentatively
 identified or characterized Besides anthraquinones metabolites gallic
 acid (-)-epicatechin and (+)-catechin metabolites were also detected
 and characterized in these biological samples Our results indicated
 that glucuronidation and sulfation were the main metabolic pathways
 of anthraquinones while methylation glucuronidation and sulfation were
 the main metabolic pathways of gallic acid (-)-epicatechin and
 (+)-catechin Phase I reactions (e g hydroxylation and reduction) played
 a relatively minor role compared to phase II reactions in metabolism
 of phenolic compounds of rhubarb decoction The identification and
 structure elucidation of these metabolites provided essential data for
 further pharmacological and clinical studies of rhubarb and related
 preparations Moreover the results of the present Investigations
 clearly indicated the relevance and usefulness of the combination of
 chromatographic spectrophotometric and mass-spectrometric analysis to
 detect and identify metabolites (C) 2010 Elsevier BV All rights
 reserved
 SN 0021-9673
 PD NOV 5
 PY 2010
 VL 1217
 IS 45
 BP 7144
 EP 7152
 DI 10.1016/j.chroma.2010.09.028
 UT ISI:000283973000018
 PT J
 AU Chen, JQ
 Du, YX
 Zhu, FX
 Chen, B
 AF Chen, Jiaquan
 Du, Yingxiang
 Zhu, Fenxia
 Chen, Bin
 TI Evaluation of the enantioselectivity of glycogen-based dual chiral
 selector systems towards basic drugs in capillary electrophoresis
 SO JOURNAL OF CHROMATOGRAPHY A
 AB Several chiral reagents including cyclodextrins (CDs) and derivatives
 crown ethers proteins chiral surfactants and polymers have been
 involved in dual selector systems for enantioseparation of a series
 of chiral compounds by capillary electrophoresis (CE) In comparison
 to the chiral reagents above-mentioned there is no report concerning
 the use of polysaccharides in dual chiral CE system In this paper we
 first investigate the enantioselectivity of polysaccharide-based dual
 selector systems towards some chiral drugs During our recent work
 glycogen belonging to the class of branched polysaccharides has been
 used as a novel chiral selector in CE In this study three glycogen-based
 dual chiral CE systems have been established for enantiomeric
 separations of several racemic basic drugs consisting of duloxetine
 cetirizine citalopram sulconazole laudanosine amlodipine propranolol
 atenolol and nefopam These three dual systems combined glycogen
 (neutral polysaccharide) with chondroitin sulfate A (CSA ionic
 polysaccharide) beta-CD and HP-beta-CD respectively It was found that
 the dual system of glycogen/CSA exhibited good enantioselective
 properties toward the tested drugs More importantly compared to the
 single selector systems synergistic effect was observed when glycogen
 was used with CSA for most of the analytes This indicated the
 enhancement of enantioseparation observed for these analytes in
 glycogen/CSA system might be due to some favorable interaction effects
 between glycogen and CSA Moreover in order to evaluate the
 stereoselectivity of glycogen/CSA the influences of buffer pH and
 selector concentration on enantioseparation of the studied drugs were
 also investigated (C) 2010 Elsevier B V All rights reserved
 SN 0021-9673
 PD NOV 5
 PY 2010
 VL 1217
 IS 45
 BP 7158
 EP 7163
 DI 10.1016/j.chroma.2010.09.017
 UT ISI:000283973000020
 PT J
 AU Zan, K
 Shi, SP
 Fu, QA
 Chen, XQ
 Zhou, SX
 Xiao, MT
 Tu, PF
 AF Zan, Ke
 Shi, She-Po
 Fu, Qiang
 Chen, Xiao-Qing
 Zhou, Si-Xiang
 Xiao, Mei-Tian
 Tu, Peng-Fei
 TI New Sesquiterpenoids from Artemisia anomala
 SO HELVETICA CHIMICA ACTA
 AB One new guaianolide, anomalactone A (1), and one new norcadinane
 sesquiterpene, anomallenodiol (2), along with two germacranolides,
 anomalactones B and C (3 and 4, resp.), were isolated from the aerial
 part of Artemisia anomala S. MOORE. Their structures were determined
 on the basis of extensive spectroscopic analyses.
 SN 0018-019X
 PY 2010
 VL 93
 IS 10
 BP 2000
 EP 2006
 UT ISI:000283908200015
 PT J
 AU Xu, GF
 Li, H
 Zhang, C
 Sun, ZY
 Zhong, WY
 Xu, DK
 Chen, HY
 AF Xu Guo-Feng
 Li Hui
 Zhang Cui
 Sun Zi-Yin
 Zhong Wen-Ying
 Xu Dan-Ke
 Chen Hong-Yuan
 TI Research and Application of Visual Detection Based on Quantum Dots
 Coupled with Silver Enhancement
 SO CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
 AB CdTe quantum dot probe modified with streptavidin ( SA) was synthesized
 and prepared. A novel visual detection method based on the quantum dot
 coupled with silver enhancement was successfully established. Combined
 with the protein microarray analysis technique, this novel method did
 well in the detection of the reverse phase protein microarray. To detect
 the analytical performance, human IgG was used as a mode in this
 experiment. First, human IgG was immobilized on Aldehyde slides, then
 the optimized bio-goat anti-human IgG and CdTe-SA probe was added,
 finally silver enhancement coloration was carried out for 15 min. The
 results showed a good linear correlation between the signal gray level
 and the logarithm of human IgG immobilized on slides from 100 pg to
 1.6 ng with a correlation coefficient (R-2) of 0.997 while its lowest
 detectable limit was about 50 pg human IgG. This novel method could
 be used to the sensitive detection of micro-amount protein and showed
 the characteristics of the simple operation, lower request to the
 instruments and the visual results.
 SN 0253-3820
 PD OCT
 PY 2010
 VL 38
 IS 10
 BP 1383
 EP 1387
 DI 10.3724/SP.J.1096.2010.01383
 UT ISI:000283904400001
 PT J
 AU Yao, ZY
 Zhang, H
 Sheng, HM
 Wu, XM
 Bin Sun, H
 AF Yao, Zhang Yu
 Zhang, Hao
 Sheng, Huan Ming
 Wu, Xiao Ming
 Bin Sun, Hong
 TI An unexpected Hoffmann elimination during the alkylation of
 dihydrotetrabenazine
 SO CHINESE CHEMICAL LETTERS
 AB Dihydrotetrabenazine (DTBZ) is the major pharmacologically active form
 of tetrabenazine (TBZ), which was approved by FDA for the treatment
 of chorea associated with Huntington's disease (HD). An unexpected
 Hoffmann elimination was observed during the treatment of DTBZ with
 sodium hydrogen and alkyl halides, leading to the formation of both
 eliminated products (major) and hydroxyl-alkylated products (minor).
 (C) 2010 Xiao Ming Wu. Published by Elsevier B.V. on behalf of Chinese
 Chemical Society. All rights reserved.
 SN 1001-8417
 PD NOV
 PY 2010
 VL 21
 IS 11
 BP 1334
 EP 1337
 DI 10.1016/j.cclet.2010.06.022
 UT ISI:000283899700019
 PT J
 AU Zhang, QH
 Yang, J
 He, Y
 Liu, F
 Wang, JP
 Davey, AK
 AF Zhang, Qing-Hua
 Yang, Jin
 He, Ying
 Liu, Fang
 Wang, Ji-Ping
 Davey, Andrew K.
 TI Food effect on the pharmacokinetics of entecavir from dispersible
 tablets following oral administration in healthy Chinese volunteers
 SO ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
 AB Objective: The aim of the present study was to assess the effect of
 food on the pharmacokinetics of entecavir (CAS 142217-69-4) from
 dispersible tablets.
 Methods: In an open-label, two-way crossover study, 12 healthy Chinese
 volunteers randomly received a single oral dose of 1 mg entecavir
 dispersible tablets under fasted and fed conditions. Blood samples were
 collected and determined for pharmacokinetic analyses. A solid phase
 extraction for sample preparation and a LC/MS method were developed
 and validated for determination of entecavir in human plasma.
 Results: The absorption of entecavir from dispersible tablets was
 altered significantly with food intake, as evidenced by a decrease in
 C m of 63%, a decrease in AUC(0-t) of 22%, and a delay in T-max of 1.5
 h. The calibration curve was linear from 0.2 to 25 ng/mL, with a lower
 limit of quantitation (LLOQ) of 0.2 ng/mL.
 Conclusion: Food intake has an obvious effect on the absorption of
 entecavir from dispersible tablets. It is better to take entecavir
 dispersible tablets on an empty stomach.
 SN 0004-4172
 PY 2010
 VL 60
 IS 10
 BP 640
 EP 644
 UT ISI:000283963500010
 PT J
 AU Zhang, PH
 Zhang, LY
 Jiang, ZZ
 Wang, T
 Chen, HK
 Xiong, YT
 Li, Z
 AF Zhang, Pinghu
 Zhang, Luyong
 Jiang, Zhenzhou
 Wang, Tao
 Chen, Hongkui
 Xiong, Yating
 Li, Zhan
 TI In Vitro Mitochondrial Toxicity of Metacavir, a New Nucleoside Reverse
 Transcriptase Inhibitor for Treatment of Hepatitis B Virus
 SO ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
 AB Therapy with nucleoside reverse transcriptase inhibitors (NRTIs) can
 be associated with mitochondrial toxicity. In vitro studies have been
 used to predict the predisposition for and characterize the mechanisms
 causing mitochondrial toxicity. Metacavir (PNA) is a novel synthetic
 nucleoside analog for oral administration with potent and specific
 antiviral activity against hepatitis B virus (HBV). We assessed the
 potential for mitochondrial toxicity of PNA in long-term cultures of
 HepG2 hepatoma cells by measuring mitochondrial function (through
 lactate secretion), levels of mitochondrial DNA (mtDNA), and the
 activities of respiratory-chain complexes I to IV. Exposure of HepG2
 cells to PNA at concentrations up to 50 mu M for 15 days resulted in
 no deleterious effect on cell proliferation, levels of lactate or
 mtDNA, or enzyme activities of respiratory-chain complexes I to IV.
 In contrast, dideoxycytosine at 10 mu M and zidovudine at 50 mu M have
 significant effects on cell proliferation, levels of lactate and mtDNA,
 and enzyme activities of respiratory-chain complexes I to IV. However,
 PNA at a supratherapeutic concentration of 250 mu M could result in
 significant alterations in the levels of mtDNA and the activities of
 respiratory-chain complex enzymes, revealing evidence of the potential
 mitochondrial toxicity of PNA. In summary, these in vitro results
 indicate that the potential for PNA to interfere with mitochondrial
 functions is low.
 SN 0066-4804
 PD NOV
 PY 2010
 VL 54
 IS 11
 BP 4887
 EP 4892
 DI 10.1128/AAC.00794-10
 UT ISI:000284155000049
 PT J
 AU Yang, R
 Zeng, HJ
 Yu, LL
 Chen, XL
 Qu, LB
 Li, P
 AF Yang Ran
 Zeng Huajin
 Yu Lanlan
 Chen Xiaolan
 Qu Lingbo
 Li Ping
 TI The Interaction of Flavonoid-BSA and the Relationship Between
 Molecular Structure of Flavonoids and Their Binding to BSA
 SO ACTA CHIMICA SINICA
 AB The interactions between eleven flavonoids and BSA were investigated
 by fluorescence spectroscopy The binding parameters, including binding
 constants, binding numbers and binding distance, were calculated By
 a comparison of the structures of flavonoids with their binding
 potency, the structural requirements of flavonoids for the binding were
 obtained Furthermore, to explore the effect of molecular structure on
 the binding, a study on quantitative structure and binding-property
 relationship (QSPR) was performed on SGI workstations
 SN 0567-7351
 PD OCT 14
 PY 2010
 VL 68
 IS 19
 BP 1995
 EP 1999
 UT ISI:000283976300012
 PT J
 AU Cen, JA
 Qi, Y
 Tao, YF
 Deng, Y
 Fang, WR
 Li, YM
 Zhang, LY
 Huang, WL
 AF Cen, Juan
 Qi, Yan
 Tao, Yi-fu
 Deng, Yan
 Fang, Wei-rong
 Li, Yun-man
 Zhang, Lu-yong
 Huang, Wen-long
 TI HZ08, a great regulator to reverse multidrug resistance via cycle
 arrest and apoptosis sensitization in MCF-7/ADM
 SO EUROPEAN JOURNAL OF PHARMACOLOGY
 AB In early studies, it was demonstrated that R-HZ08, S-HZ08 and the
 racemate had strong reverse efficacy of multidrug resistance in vitro
 and in vivo (Yan et al., 2008b). The effect was supposed to have direct
 interaction with multidrug resistance-associated protein (MRP1) in
 MCF-7/ADM and P-glycoprotein in K562/A02. According to our latest
 study, we found HZ08 could enhance chemotherapy induced apoptosis by
 synergistic action on reactive oxygen species generation, GSH
 depletion, mitochondrial membrane potential depolarization,
 cytochrome c release and caspase activation. Moreover, the potential
 selective effect of HZ08 on resistant cells suggested that HZ08 have
 specific targets for resistance reversal via apoptosis regulation.
 Therefore, we traced individual influence of HZ08, not only on
 apoptosis pathway per se but also on apoptosis related intracellular
 regulation systems. Then we found HZ08 could increase cells in
 G(0)/G(1) phase and regulate apoptosis related proteins (Bcl-2, Bax)
 as well as upstream functional molecules (c-Myc and c-Fos), which are
 usually abnormal in malignancy and responsible for multidrug
 resistance in MCF-7/ADM. Thereby, chemotherapy induced apoptosis was
 promoted. R-HZ08 showed better effect than S-HZ08 or the racemate did
 in most of targets above. Furthermore, HZ08 did not change the
 concentration of intracellular Ca2+ which means it would not have side
 effect as verapamil does. Considering multidrug resistance is
 multifactorial, HZ08, especially R-HZ08, which could sensitize
 apoptosis by multiple improvements of upstream malignant characters,
 will be a promising drug to enhance the effect of chemotherapy in the
 treatment of multidrug resistant tumor. (c) 2010 Elsevier B.V. All
 rights reserved.
 SN 0014-2999
 PD NOV 25
 PY 2010
 VL 647
 IS 1-3
 BP 21
 EP 30
 DI 10.1016/j.ejphar.2010.08.013
 UT ISI:000283835400003
 PT J
 AU Fu, RG
 You, QD
 Yang, L
 Wu, WT
 Jiang, C
 Xu, XL
 AF Fu, Rong-geng
 You, Qi-dong
 Yang, Lei
 Wu, Wu-tong
 Jiang, Cheng
 Xu, Xiao-li
 TI Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine
 and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and
 Aurora-A kinase inhibitors for anti-cancer agents
 SO BIOORGANIC & MEDICINAL CHEMISTRY
 AB Four series of dihydropyrazolo[3,4-b]pyridines and
 benzo[4,5]imidazo[1,2-a]pyrimidines were designed and synthesized as
 dual KSP and Aurora-A kinase inhibitors for anti-cancer agents by
 introducing some fragments of Aurora-A kinase inhibitors into our KSP
 inhibitor CPUYL064. A total of 19 target compounds were evaluated by
 two related enzyme inhibition assays and a cytotoxicity assay in vitro.
 The results showed that some target compounds could inhibit both
 enzymes, and several of them showed significant inhibition activity
 against HCT116 cell line. Despite showing moderate KSP and Aurora-A
 kinase inhibition, the lead compounds 6a and 6e displayed significant
 cytotoxic activity in the micromolar range, especially against the
 HCT116 cell line and HepG2 cell line. The results may be useful for
 developing a new class of inhibitors having a dual function, KSP
 inhibition and Aurora-A kinase inhibition, for the treatment of cancer.
 (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0968-0896
 PD NOV 15
 PY 2010
 VL 18
 IS 22
 BP 8035
 EP 8043
 DI 10.1016/j.bmc.2010.09.020
 UT ISI:000283649900040
 PT J
 AU Dong, J
 Yao, SW
 Xu, YG
 AF Dong Jin
 Yao Shuowei
 Xu Yungen
 TI Tumor Angiogenesis Inhibitors
 SO PROGRESS IN CHEMISTRY
 AB At present, drug inhibition of angiogenesis has become a hot topic in
 the treatment of tumor and several tumor angiogenesis inhibitors (TAIs)
 have been marketed. TAIs can suppress tumor growth and metastasis, and
 even induce tumor regression. Research and development on TAIs holds
 the promise of supplying drugs with high potency, low toxicity and
 broad-spectrum antitumor activity for tumor patients. This review
 summarizes recent research progress in TAIs. First of all, indirect
 TAIs are introduced. Among indirect TAIs, VEGF inhibitors are the most
 successful TAIs currently. Secondly, direct TAIs, which are unlikely
 switch on the angiogenic rescue program, are introduced. Thirdly, in
 the miscellaneous TAIs part, thalidomide and its derivatives, whose
 mechanisms of activity have not been defined well, are described in
 detail. Finally, several problems encountered in the research and
 development of TAIs, such as challenge from novel theory of
 anti-angiogenenic therapy and resistance, are analyzed and discussed,
 and future research directions are pointed out.
 SN 1005-281X
 PD OCT
 PY 2010
 VL 22
 IS 10
 BP 1993
 EP 2002
 UT ISI:000283615400013
 PT J
 AU Zhou, CH
 Xiang, M
 He, SY
 Qian, ZY
 AF Zhou, Cheng-Hua
 Xiang, Min
 He, Shu-Ying
 Qian, Zhi-Yu
 TI Protein Kinase C Pathway is Involved in the Inhibition by Crocetin of
 Vascular Smooth Muscle Cells Proliferation
 SO PHYTOTHERAPY RESEARCH
 AB Crocetin is a natural carotenoid compound isolated from Gardenia
 jasminoids Ellis. Our previous study showed that crocetin inhibits
 angiotensin II (Ang II)-induced proliferation of vascular smooth
 muscle cells (VSMCs). The present study investigated the involvement
 of the protein kinase C (PKC) pathway in the growth-inhibitory action
 of crocetin in VSMCs. The findings showed that PKC activity in the
 membrane fraction of VSMCs increased following stimulation with Ang
 II, which was suppressed significantly by pretreating the cells with
 crocetin. Inhibition of PKC activity by crocetin appeared to be
 associated with growth inhibition in VSMCs, because chelerythrine
 chloride, a specific PKC inhibitor, likewise decreased cell
 proliferation. PKC-alpha, a conventional PKC isoform, was detected in
 bovine aorta VSMCs by RT-PCR and western blotting analysis. Crocetin
 inhibited Ang II-induced membrane translocation of PKC-alpha, and the
 inhibition of crocetin on PKC activity in membrane fraction coincided
 with its suppression on membrane translocation of PKC-alpha. In
 addition, Ang II-induced mRNA expressions of c-fos, c-jun and c-myc
 were also decreased by crocetin. Taken together, the data suggest that
 the inhibition by crocetin of PKC activity, at least in part due to
 inactivation of PKC-alpha, and the subsequent suppression of
 proto-oncogene expressions might mediate its inhibitory effect on
 VSMCs proliferation. Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0951-418X
 PD NOV
 PY 2010
 VL 24
 IS 11
 BP 1680
 EP 1686
 DI 10.1002/ptr.3194
 UT ISI:000283794300017
 PT J
 AU Sun, MJ
 Wang, Y
 Shen, J
 Xiao, YY
 Su, ZG
 Ping, QN
 AF Sun, Minjie
 Wang, Yu
 Shen, Jie
 Xiao, Yanyu
 Su, Zhigui
 Ping, Qineng
 TI Octreotide-modification enhances the delivery and targeting of
 doxorubicin-loaded liposomes to somatostatin receptors expressing
 tumor in vitro and in vivo
 SO NANOTECHNOLOGY
 AB Octreotide is believed to be the ligand of somatostatin receptors
 (SSTRs) which are widely used in tumor diagnosis and clinical therapy.
 In the present work, a new targeting conjugate,
 octreotide-polyethylene glycol-phosphatidylethanolamine
 (Oct-PEG-PE), was developed for the assembling of liposome, and the
 effect of octreotide-modification on the enhancement of the delivery
 and targeting of doxorubicin-loaded liposomes was investigated in
 vitro and in vivo. Oct-PEG-PE was synthesized by a three-step reaction
 involving two derivative intermediate formations of bis (p-nitrophenyl
 carbonate)-PEG ((pNP)(2)-PEG) and pNP-PEG-PE. The Oct-modified and
 unmodified liposomes (DOX-OL and DOX-CL) were prepared by the ammonium
 sulfate gradient method. Both drug uptake assay and cell apoptosis
 assay suggested that DOX-OL noticeably increased the uptake of DOX in
 SMMC-7721 cells and showed a more significant cytotoxicity, compared
 with DOX-CL. The effect of DOX-OL was remarkably inhibited by free
 octreotide. In contrast, no significant difference in drug cytotoxicty
 was found between DOX-OL and DOX-CL in CHO cells without obvious
 expression of SSTRs. The study of ex vivo fluorescence tissues imaging
 of BALB/c mice and in vivo tissue distribution of B16 tumor-bearing
 mice indicated that DOX-OL caused remarkable accumulation of DOX in
 melanoma tumors and the pancreas, in which the SSTRs are highly
 expressed.
 SN 0957-4484
 PD NOV 26
 PY 2010
 VL 21
 IS 47
 AR 475101
 DI 10.1088/0957-4484/21/47/475101
 UT ISI:000283673100001
 PT J
 AU Liu, DF
 Ge, YF
 Tang, Y
 Yuan, YB
 Zhang, Q
 Li, R
 Xu, QW
 AF Liu, Dongfei
 Ge, Yifan
 Tang, Yue
 Yuan, Yubing
 Zhang, Qing
 Li, Rui
 Xu, Qunwei
 TI Solid lipid nanoparticles for transdermal delivery of diclofenac
 sodium: preparation, characterization and in vitro studies
 SO JOURNAL OF MICROENCAPSULATION
 AB The aim of this study was to prepare diclofenac sodium (DNa) solid lipid
 nanoparticles (SLNs) by a modified emulsion/solvent evaporation method
 for transdermal delivery. Five independent processing parameters
 including the lipid matrix, emulsifiers, co-emulsifiers,
 water-dispersed phase and organic phase were assessed systematically
 to enhance the entrapment of DNa. The SLNs produced by optimal
 formulation were submicrometre size with low polydispersity index, the
 entrapment efficiency was about 89% and the drug loading was about 9.5%.
 Shape and surface morphology were determined by transmission electron
 microscopy, which revealed the fairly spherical and core-shell shapes
 of the SLNs. The in vitro release of SLNs showed a two-step release
 pattern: one initial burst release followed by a second slow-release
 phase. In the in vitro cutaneous permeation studies, value of flux
 obtained for DNa solution was higher than that of SLNs suspension. SLNs
 had also been shown to improve the dermal localization of DNa.</.
 SN 0265-2048
 PY 2010
 VL 27
 IS 8
 BP 726
 EP 734
 DI 10.3109/02652048.2010.513456
 UT ISI:000283689900007
 A Qu, B
 U Ou, BL
 Chen, DY
 Hu, YZ
 A Qu, Bin
 F Ou, Bei-Li
 Chen, De-Ying
 Hu, Yu-Zhu
 T Identification, Synthesis and Spectral Characterization of a Potential
 I Impurity of Ceftazidime
 JOURNAL OF FOOD AND DRUG ANALYSIS
 A During the process development of ceftazidime, a new impurity which
 B exceeded the limit of 0.1% was detected by a simple HPLC method. The
 molecular weight of the target impurity was determined by LC/MS. This
 suspected impurity was synthesized and purified for characterization.
 When co-injected with ceftazidime in HPLC, the retention time of the
 impurity was the same as the ceftazidime sample containing the
 impurity. The structural determination of the suspected impurity was
 conducted by ER, MS, H-1-NMR and C-13-NMR spectroscopic techniques.
 This new impurity was the methyl ester of ceftazidime, and its structure
 was determined as
 (6R,7R)-7-[[(Z)-2-(2-aminothiazol-4-y1)-2-[(1-methoxycarbonyl-1-me
 thylet hoxy)
 imino]acetyl]amino]-8-oxo-3-[(1-pyridinio)methyl]-5-thia-1-azabicy
 clo[4. 2.0]oct-2-ene-2-carboxylate, with molecular formula of
 C23H24N6O7S2 and molecular weight of 560 Da.
 1021-9498
 P 2010
 ISI:000283694800006
 PT J
 AU Zhao, YR
 Ding, L
 Fan, HW
 Yu, Y
 Qi, XM
 Leng, Y
 Rao, YK
 AF Zhao, Yan-rong
 Ding, Li
 Fan, Hong-wei
 Yu, Yong
 Qi, Xie-min
 Leng, Ye
 Rao, Ya-kun
 TI Determination of the unstable drug otilonium bromide in human plasma
 by LC-ESI-MS and its application to a pharmacokinetic study
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB Otilonium bromide (OB) degrades rapidly in plasma and readily undergoes
 hydrolysis by the plasma esterase. In this paper, an LC-ESI-MS method
 has been developed for the determination of OB in human plasma. The
 rapid degradation of OB in plasma was well prevented by immediate
 addition of potassium fluoride (KF, an inhibitor of plasma esterase)
 to the freshly collected plasma before prompt treatment with
 acetonitrile. The method was validated over the concentration range
 of 0.1-20 ng/ml. The data of intra-run and inter-run precision and
 accuracy were within +/- 15%. The mean extraction recoveries for OB
 and the internal standard were higher than 93.0% and the matrix effects
 were negligible. The method has been successfully used in a
 pharmacokinetic study. (C) 2010 Elsevier B.V. All rights reserved.
 SN 1570-0232
 PD OCT 15
 PY 2010
 VL 878
 IS 28
 BP 2896
 EP 2900
 DI 10.1016/j.jchromb.2010.08.003
 UT ISI:000283687200035
 PT J
 AU Luo, YB
 Liu, M
 Dai, Y
 Yao, XJ
 Xia, YF
 Chou, GX
 Wang, ZT
 AF Luo, Yubin
 Liu, Mei
 Dai, Yue
 Yao, Xiujuan
 Xia, Yufeng
 Chou, Guixin
 Wang, Zhengtao
 TI Norisoboldine Inhibits the Production of Pro-inflammatory Cytokines
 in Lipopolysaccharide-Stimulated RAW 264.7 Cells by Down-Regulating
 the Activation of MAPKs but Not NF-kappa B
 SO INFLAMMATION
 AB Norisoboldine is the main isoquinoline alkaloid occurring in Radix
 Linderae, the dry roots of Lindera aggregata (Lauraceae family). It
 has been previously implicated to be able to ameliorate the synovial
 inflammation and abnormal immune conditions in collagen-induced
 arthritis of mice. To get insight to the potential anti-inflammatory
 mechanisms of this alkaloid compound, the present study was undertaken
 to explore the effects of norisoboldine on the production of
 pro-inflammatory cytokines from macrophages stimulated by
 lipopolysaccharide. In vitro, norisoboldine substantially reduced the
 production of nitric oxide (NO), tumor necrosis factor (TNF)-alpha as
 well as interleukin (IL)-1 beta from RAW264.7 macrophage cells in a
 concentration-dependent manner, whereas it only slightly reduced the
 production of interleukin-6 (IL-6) at both protein and transcription
 levels. Of note, the preventive effects of norisoboldine on the release
 of pro-inflammatory cytokines were correlated with the inhibitory
 action on the phosphorylations of mitogen-activated protein (MAP)
 kinases including p38, extracellular signal-regulated kinase (ERK) and
 c-jun NH2-terminal kinase (JNK), but not on the activation and
 translocation of nuclear factor-kappa B (NF-kappa B). It can be
 therefore concluded that norisoboldine inhibits the macrophage
 activation and the resultant production of pro-inflammatory cytokines
 via down-regulating the activation of MAPKs signaling pathways rather
 than NF-kappa B.
 SN 0360-3997
 PD DEC
 PY 2010
 VL 33
 IS 6
 BP 389
 EP 397
 DI 10.1007/s10753-010-9197-0
 UT ISI:000283572900005
 PT J
 AU Du, YX
 Chen, B
 AF Du, Yingxiang
 Chen, Bin
 TI Recent advances in enantioseparation by capillary electrophoresis
 using antibiotics and polysaccharides as chiral selectors A review
 SO CHIMICA OGGI-CHEMISTRY TODAY
 AB This review gives an overview of the use of antibiotics and
 polysaccharides as chiral selectors in the field of enantioseparation
 by capillary electrophoresis (CE). Antibiotics and polysaccharides are
 two important types of chiral selectors in CE, and have been utilized
 successfully in enantioseparation of various compounds including
 pharmaceuticals, biochemicals, agrochemicals, fine chemicals, etc. In
 this review, recent advances covering literature published from
 January 2006 to April 2010 in chiral CE separation with antibiotics
 and polysaccharides are summarized. These developments focus on the
 introductions of new chiral selectors, investigations in different CE
 modes containing micellar electrokinetic chromatography and
 nonaqueous capillary electrophoresis, studies on separation
 mechanisms and improvements in separation methods.
 SN 1973-8250
 PD SEP-OCT
 PY 2010
 VL 28
 IS 5
 BP 37
 EP 42
 UT ISI:000283581600005
 PT J
 AU Wu, SM
 Tian, ZQ
 Zhang, ZL
 Huang, BH
 Jiang, P
 Xie, ZX
 Pang, DW
 AF Wu, Sheng-Mei
 Tian, Zhi-Quan
 Zhang, Zhi-Ling
 Huang, Bi-Hai
 Jiang, Peng
 Xie, Zhi-Xiong
 Pang, Dai-Wen
 TI Direct fluorescence in situ hybridization (FISH) in Escherichia coli
 with a target-specific quantum dot-based molecular beacon
 SO BIOSENSORS & BIOELECTRONICS
 AB Quantum dots (QDs) are inorganic fluorescent nanocrystals with
 excellent properties such as tunable emission spectra and
 photo-bleaching resistance compared with organic dyes, which make them
 appropriate for applications in molecular beacons. In this work,
 quantum dot-based molecular beacons (QD-based MBs) were fabricated to
 specifically detect beta-lactamase genes located in pUC18 which were
 responsible for antibiotic resistance in bacteria Escherichia coil (E.
 coli) DH5 alpha. QD-based MBs were constructed by conjugating
 mercaptoacetic acid-quantum dots (MAA-QDs) with black hole quencher
 2 (BHQ2) labeled thiol DNA vial metal-thiol bonds. Two types of
 molecular beacons, double-strands beacons and hairpin beacons, were
 observed in product characterization by gel electrophoresis. Using
 QD-based MBs, one-step FISH in tiny bacteria DH5a was realized for the
 first time. QD-based MBs retained their bioactivity when hybridizing
 with complementary target DNA, which showed excellent advantages of
 eliminating background noise caused by adsorption of non-specific
 bioprobes and achieving clearer focus of genes in plasmids pUC18, and
 capability of bacterial cell penetration and signal specificity in
 one-step in situ hybridization. (C) 2010 Elsevier B.V. All rights
 reserved.
 SN 0956-5663
 PD OCT 15
 PY 2010
 VL 26
 IS 2
 BP 491
 EP 496
 DI 10.1016/j.bios.2010.07.067
 UT ISI:000283804400030
 PT J
 AU Wang, Y
 Di, LL
 Lin, GW
 Lu, T
 AF Wang, Yue
 Di, Li Li
 Lin, Guo Wu
 Lu, Tao
 TI Crystal structure of 2-(2-amino-5-chlorophenyl)-1H-benzimidazole,
 C13H10ClN3
 SO ZEITSCHRIFT FUR KRISTALLOGRAPHIE-NEW CRYSTAL STRUCTURES
 AB C13H10ClN3, orthorhombic, Pna2(1) (no. 33), a = 8.685(2) angstrom, b
 = 6.648(1) angstrom, c = 19.264(4) angstrom, v = 1112.3 angstrom(3),
 Z= 4, R-gt(F) = 0.046, wR(ref)(F-2) = 0.149, T = 296 K.
 SN 1433-7266
 PY 2010
 VL 225
 IS 3
 BP 457
 EP 458
 DI 10.1524/ncrs.2010.0200
 UT ISI:000283462300016
 PT J
 AU Hou, ZG
 Luo, JG
 Wang, JS
 Kong, LY
 AF Hou, Zhiguo
 Luo, Jianguang
 Wang, Junsong
 Kong, Lingyi
 TI Separation of minor coumarins from Peucedanum praeruptorum using HSCCC
 and preparative HPLC guided by HPLC/MS
 SO SEPARATION AND PURIFICATION TECHNOLOGY
 AB Two minor coumarins, including a new compound qianhucoumarin J, were
 isolated from Peucedanum praeruptorum by a multi-step separation
 procedure using high-speed counter-current chromatography (HSCCC) and
 preparative high performance liquid chromatography (prep-HPLC)
 monitored by high performance liquid chromatography coupled with mass
 spectrometry (HPLC/MS) analysis. The crude extract was analyzed first
 by HPLC/MS to detect unknown compounds. The target compounds were
 enriched by HSCCC, using a two-phase solvent system of petroleum
 ether-ethyl acetate-methanol-water (5:5:6:4, v/v) and then isolated
 and purified by preparative HPLC monitored by HPLC/MS. The structure
 of the new compound was elucidated mainly by analysis of its 1D and
 2D NMR spectral data. Its absolute configuration was determined by
 chemical degradation followed by chiral HPLC analysis. (C) 2010
 Elsevier B.V. All rights reserved.
 SN 1383-5866
 PD OCT 13
 PY 2010
 VL 75
 IS 2
 BP 132
 EP 137
 DI 10.1016/j.seppur.2010.08.007
 UT ISI:000283402500006
 PT J
 AU Shao, M
 Wang, Y
 Liu, Z
 Zhang, DM
 Cao, HH
 Jiang, RW
 Fan, CL
 Zhang, XQ
 Chen, HR
 Yao, XS
 Ye, WC
 AF Shao, Meng
 Wang, Ying
 Liu, Zhong
 Zhang, Dong-Mei
 Cao, Hui-Hui
 Jiang, Ren-Wang
 Fan, Chun-Lin
 Zhang, Xiao-Qi
 Chen, He-Ru
 Yao, Xin-Sheng
 Ye, Wen-Cai
 TI Psiguadials A and B, Two Novel Meroterpenoids with Unusual Skeletons
 from the Leaves of Psidium guajava
 SO ORGANIC LETTERS
 AB Psiguadials A (1) and B (2), two novel sesquiterpenoid-diphenylmethane
 meroterpenoids with unusual skeletons, along with a pair of known
 epimers, psidial A (3) and guajadial (4), were isolated from the leaves
 of Psidium guajava. Their structures with absolute configurations were
 elucidated by means of NMR, X-ray diffraction, and quantum chemical
 CD calculation. Compounds 1, 2, and 4 exhibited potent inhibitory
 effects on the growth of human hepatoma cells.
 SN 1523-7060
 PD NOV 5
 PY 2010
 VL 12
 IS 21
 BP 5040
 EP 5043
 DI 10.1021/ol102179u
 UT ISI:000283531000085
 PT J
 AU Li, H
 Huo, MR
 Zhou, JP
 Dai, YD
 Deng, YP
 Shi, XJ
 Masoud, J
 AF Li, Hong
 Huo, Meirong
 Zhou, Jianping
 Dai, Yindi
 Deng, Yaping
 Shi, Xiangjie
 Masoud, Jumah
 TI Enhanced Oral Absorption of Paclitaxel in N-Deoxycholic Acid-N,
 O-Hydroxyethyl Chitosan Micellar System
 SO JOURNAL OF PHARMACEUTICAL SCIENCES
 AB The overall goal of this study was to develop a micellar system of
 paclitaxel (PTX) to enhance its oral absorption. An amphiphilic
 chitosan derivative, N-deoxycholic acid-N, O-hydroxyethyl chitosan
 (DHC), was synthesized and characterized by FTIR, H-1 NMR, elemental
 analysis, and X-ray diffraction (XRD) techniques. The degree of
 substitution (DS) of hydroxyethyl group and deoxycholic acid group
 ranged from 89.5-114.5% and 1.11-8.17%, respectively. The critical
 micelle concentration (CMC) values of DHC decreased from 0.26 to 0.16
 mg/mL as the DS of deoxycholic acid group increased. PTX was
 successfully loaded in DHC micelles with a high drug loading (31.68
 +/- 0.14%) and entrapment efficiency (77.57 +/- 0.51%). The particle
 size of PTX-loaded DHC micelles ranged from 203.35 +/- 2.19 to 236.70
 +/- 3.40 nm as the DS of deoxycholic acid group increased. After orally
 administration of PTX-loaded DHC micelles, the bioavailability was
 threefold compared with that of an orally dosed Taxol (R). The
 single-pass intestinal perfusion studies (SPIP) showed that the
 intestinal absorption of micelles was via endocytosis involving a
 saturable process and a p-glycoprotein (P-gp)-independent way. All
 these indicated that the DHC micelles might be a promising tool for
 oral delivery of poorly water-soluble drugs. (C) 2010 Wiley-Liss, Inc.
 and the American Pharmacists Association J Pharm Sci 99:4543-4553, 2010
 SN 0022-3549
 PD NOV
 PY 2010
 VL 99
 IS 11
 BP 4543
 EP 4553
 DI 10.1002/jps.22159
 UT ISI:000283477100012
 PT J
 AU Huang, XF
 Yang, YM
 Zhu, J
 Liu, JH
 AF Huang, Xingfu
 Yang, Yanmin
 Zhu, Jun
 Liu, Jinhan
 TI A Single Ethanoyl Changes the Effects on HERG K+ Channel: Comparative
 Effects of Acehytisine Hydrochloride and Guanfu Base G
 SO CIRCULATION
 CT World Congress of Cardiology Scientific Sessions
 CY JUN 16-19, 2010
 CL Beijing, PEOPLES R CHINA
 SN 0009-7322
 PD JUL 13
 PY 2010
 VL 122
 IS 2
 BP P1106
 UT ISI:000279801703274
 PT J
 AU Xiong, F
 Wang, H
 Geng, KK
 Gu, N
 Zhu, JB
 AF Xiong, Fei
 Wang, Hao
 Geng, Kun-kun
 Gu, Ning
 Zhu, Jia-bi
 TI Optimized Preparation, Characterization and Biodistribution in Heart
 of Breviscapine Lipid Emulsion
 SO CHEMICAL & PHARMACEUTICAL BULLETIN
 AB Breviscapine is a Traditional Chinese Medicine treating cardiovascular
 diseases by promoting blood circulation and removing blood stasis. The
 major active component of breviscapine has low aqueous solubility, poor
 chemical stability, short biological half-life and rapid elimination
 rate from the plasma. The use of a lipid emulsion formulation containing
 breviscapine might improve chemical stability, increase drug loading,
 exhibit sustained release profile. In the present study, we developed
 an optimized formulation and technological method for the preparation
 of sterile and stable breviscapine lipid emulsion (Bre-LE) for
 intravenous infusion. The average particle size, polydispersity index,
 zeta potential, stability constant (K-s) value and content of final
 product were (225.3 +/- 8.8)nm, 0.221 +/- 0.020, (-29.6 +/- 1.5) mV,
 (24.3 +/- 2.9)% and (94.5 +/- 0.6)% respectively (n=3). The results
 of in vitro release experiment suggest that lipid emulsion as
 breviscapine carrier showed a desirable sustained release profile.
 Dilution stability and long-term stability were also researched in the
 present paper. The results show the carrier could protect drug from
 degradation after dilution by phosphate buffered saline and fetal calf
 serum. And Bre-LE was stable for up to 6 months at room temperature
 storage condition. The biodistribution of drug in heart of mice
 increased dramatically after encapsulation into lipid emulsion which
 was beneficial to heart disease therapy.
 SN 0009-2363
 PD NOV
 PY 2010
 VL 58
 IS 11
 BP 1455
 EP 1460
 UT ISI:000283522300006
 PT J
 AU Cao, P
 Yu, JM
 Lu, WG
 Cai, XT
 Wang, ZG
 Gu, ZH
 Zhang, JA
 Ye, TM
 Wang, M
 AF Cao, Peng
 Yu, Jiemiao
 Lu, Wuguang
 Cai, Xueting
 Wang, Zhigang
 Gu, Zhenhua
 Zhang, Juan
 Ye, Tingmei
 Wang, Min
 TI Expression and Purification of an Antitumor-Analgesic Peptide from the
 Venom of Mesobuthus martensii Karsch by Small Ubiquitin-Related
 Modifier Fusion in Escherichia coli
 SO BIOTECHNOLOGY PROGRESS
 AB To prevent protein aggregation, some proteins are usually expressed
 as fusion proteins from which target proteins can be released by
 proteolytic or chemical reagents. In this report, small
 ubiquitin-related modifier (SUMO) linked with a hexa-histidine tag was
 used as a fusion partner for the antitumor-analgesic peptide from the
 venom of Buthus martensii (Karsch) scorpion (AGAP). The optimal
 expression level of the soluble fusion protein, SUMO-AGAP, was up to
 40% of the total cellular protein. The fusion protein was purified by
 Ni-NTA affinity chromatography and cleaved by a SUMO-specific protease
 (Ulp1) to obtain the recombinant AGAP (rAGAP), which was further
 purified by Ni-NTA affinity chromatography. The purified final product
 was >95% pure by SDS-PAGE stained with Coomassie brilliant blue R-250.
 Mass spectroscopic analysis indicated the protein to be 7142.63 Dalton,
 which equaled the theoretically expected mass. N-terminal sequencing
 of rAGAP showed the sequence corresponded to the native protein. MTT
 assay indicated the rAGAP could significantly inhibit the
 proliferation of Jurkat and Hut 78 T lymphoma cell lines. The further
 writhing experiment showed that the rAGAP had an intensive analgesic
 effect. The expression strategy presented in this study allows
 convenient high yield and easy purification of the rAGAP with native
 sequences. (C) 2010 American Institute of Chemical Engineers
 Biotechnol. Prog., 26: 1240-1244, 2010
 SN 8756-7938
 PD SEP-OCT
 PY 2010
 VL 26
 IS 5
 BP 1240
 EP 1244
 DI 10.1002/btpr.433
 UT ISI:000283482100005
 PT J
 AU Li, SS
 He, H
 Chen, Z
 Zha, J
 Chuong, PH
 AF Li Shan-shan
 He Hua
 Chen Zhe
 Zha Jun
 Chuong Pham-Huy
 TI Fluorescence Study on the Interactions between Carbon Nanotubes and
 Bovine Serum Albumin
 SO SPECTROSCOPY AND SPECTRAL ANALYSIS
 AB As a new family of nanomaterials, carbon nanotubes (CNTs) exhibit
 unique properties such as their capacity to penetrate into the cells
 and low immunogenicity, which have attracted increasing attention in
 biomedical field and make their application in drug and gene transfer
 systems being possible. So getting more information about the
 interaction of CNTs with biomacromolecules is crucial for further
 investigation of CNTs in therapeutic applications. The interaction
 between CNTs and BSA under physiological condition was investigated
 by fluorescence quenching, synchronous fluorescence and red edge
 excitation shift (REES)method. The results showed that CNTs could
 significantly decrease the fluorescence intensity of BSA. While the
 results of synchronous fluorescence and REES indicated that CNTs almost
 had no influence on the conformation of BSA. So the authors concluded
 that the mechanism of interaction between CNTs and BSA was non-specific
 adsorption.
 SN 1000-0593
 PD OCT
 PY 2010
 VL 30
 IS 10
 BP 2689
 EP 2692
 DI 10.3964/j.issn.1000-0593(2010)10-2689-04
 UT ISI:000283267900023
 PT J
 AU Li, YJ
 Wei, HL
 Qi, LW
 Chen, J
 Ren, MT
 Li, P
 AF Li, Yan-Jing
 Wei, Huan-Li
 Qi, Lian-Wen
 Chen, Jun
 Ren, Mei-Ting
 Li, Ping
 TI Characterization and identification of saponins in Achyranthes
 bidentata by rapid-resolution liquid chromatography with electrospray
 ionization quadrupole time-of-flight tandem mass spectrometry
 SO RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 AB A rapid-resolution liquid chromatography (RRLC) method coupled with
 electrospray ionization quadrupole time-of-flight tandem mass
 spectrometry (Q-TOF MS/MS) has been developed for analysis of
 oleanane-type triterpenoid saponins in Achyranthes bidentata.
 Collision-induced dissociation techniques were used to fragment the
 precursor molecular ions and the resulting product ions. A
 retro-Diels-Alder rearrangement from the oleanane aglycone skeleton
 in the MS/MS process yielded characteristic fragment ions in positive
 ion mode. These characteristic ions were helpful in predicting the
 aglycone structure. Losses of monosaccharide sequences, presence of
 sugar-chain fragment ions, and cleavage of CO2 were observed for
 important information on sugar types and attachment sequences.
 Fragmentation rules of three major groups of saponins from A. bidentata
 were summarized, and the possible fragmentation pathways were
 proposed. A total of 22 compounds including both the target and unknown
 oleanane-type triterpenoid saponins were rapidly screened and
 predicted in the herbal extract by the developed method. The RRLC-Q-TOF
 MS/MS method has provided a powerful approach for rapid separation,
 target screening and structural elucidation of oleanane-type saponins,
 and also opened perspectives for similar studies on other herbal
 medicines. Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0951-4198
 PD OCT
 PY 2010
 VL 24
 IS 20
 BP 2975
 EP 2985
 DI 10.1002/rcm.4728
 UT ISI:000283103000007
 PT J
 AU Qi, J
 Xu, DR
 Zhou, YF
 Qin, MJ
 Yu, BY
 AF Qi, Jin
 Xu, Deran
 Zhou, Yi-Feng
 Qin, Min-Jian
 Yu, Bo-Yang
 TI New features on the fragmentation patterns of homoisoflavonoids in
 Ophiopogon japonicus by high-performance liquid
 chromatography/diode-array detection/electrospray ionization with
 multi-stage tandem mass spectrometry (vol 24, pg 2193, 2010)
 SO RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 SN 0951-4198
 PD OCT
 PY 2010
 VL 24
 IS 20
 BP 3076
 EP 3077
 DI 10.1002/rcm.4723
 UT ISI:000283103000019
 PT J
 AU Tang, H
 Guo, QA
 Zhang, C
 Zhu, J
 Yang, H
 Zou, YL
 Yan, Y
 Hong, D
 Sou, T
 Yan, XM
 AF Tang, Hui
 Guo, Qiang
 Zhang, Chao
 Zhu, Jun
 Yang, Hui
 Zou, Yun-Lian
 Yan, Yan
 Hong, Dong
 Sou, Tao
 Yan, Xin-Min
 TI Identification of an intermediate signature that marks the initial
 phases of the colorectal adenoma-carcinoma transition
 SO INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE
 AB The colorectal adenoma-carcinoma sequence describes the stepwise
 progression from normal to dysplastic epithelium and then to carcinoma.
 Only a small proportion of colorectal adenomas (CRAs) progress to
 colorectal carcinomas (CRCs). Endoscopic intervention is currently
 being used on patients with high grade dysplasia CRAs, with diameters
 of >1 cm, or villous components of >25% who are at higher risk than
 other CRA sufferers. During the process, biopsy samples are taken for
 conventional histological diagnosis, but poor pathomorphological
 sensitivity and specificity greatly limit the diagnostic accuracy.
 Unfortunately, there are no reliable molecular criteria available that
 can predict the potential development of CRA to CRC. Gene expression
 profiles of normal colorectal mucosa (NOR), CRA and different Dukes'
 stages of CRC biopsy specimens, which represent the gradual progress
 of the CRA to CRC sequence, were determined by Affymetrix technology.
 Representative regulated genes were further analyzed by quantitative
 real-time PCR (qRT-PCR) and immunohistochemistry (IHC).
 Intersectional analyses of discriminative expression signatures of CRC
 vs. CRA and CRA vs. NOR allowed the identification of an intermediate
 signature of 463 probe sets (psets) that mark the NOR -> CRA -> CRC
 progression. This signature represents a reservoir of candidate
 markers for the early diagnosis of higher-risk CRA, thus allowing for
 timely therapeutic intervention and more selective treatment. A
 further 279 CRC-specific psets pointing to the malignant transition
 from CRA to CRC were identified and these could represent potential
 therapeutic targets for CRC. The reliability of the results was further
 confirmed by qRT-PCR and IHC analyses of the 4-gene sets randomly
 selected from the 463 psets.
 SN 1107-3756
 PD NOV
 PY 2010
 VL 26
 IS 5
 BP 631
 EP 641
 DI 10.3892/ijmm_00000508
 UT ISI:000283203200001
 PT J
 AU Xiong, Y
 Shen, L
 Liu, KJ
 Tso, P
 Xiong, YQ
 Wang, GJ
 Woods, SC
 Liu, M
 AF Xiong, Ye
 Shen, Ling
 Liu, Kristina J.
 Tso, Patrick
 Xiong, Yuqing
 Wang, Guangji
 Woods, Stephen C.
 Liu, Min
 TI Antiobesity and Antihyperglycemic Effects of Ginsenoside Rb1 in Rats
 SO DIABETES
 AB OBJECTIVE Obesity and type 2 diabetes are national and worldwide
 epidemics. Because currently available antiobesity and antidiabetic
 drugs have limited efficacy and/or safety concerns, identifying new
 medicinal agents, such as ginsenoside Rb1 (Rb1) as reported here,
 offers exciting possibilities for future development of successful
 antiobesity and antidiabetic therapies.
 RESEARCH DESIGN AND METHODS Changes in feeding behavior after acute
 intraperitoneal administration of Rb1 and the effects of
 intraperitoneal Rb1 for 4 weeks on body weight, energy expenditure,
 and glucose tolerance in high-fat diet (HFD)-induced obese rats were
 assessed. We also examined the effects of Rb1 on signaling pathways
 and neuropeptides in the hypothalamus.
 RESULTS Acute intraperitoneal Rb1 dose-dependently suppressed food
 intake without eliciting signs of toxicity. This inhibitory effect on
 feeding may be mediated by central mechanisms because Rb1 stimulated
 c-Fos expression in brain areas involved in energy homeostasis.
 Consistent with this, Rb1 activated the phosphatidylinositol
 3-kinase/Airt signaling pathway and inhibited NPY gene expression in
 the hypothalamus. Four-week administration of Rb1 significantly
 reduced food intake, body weight gain, and body fat content and
 increased energy expenditure in HFD-induced obese rats. Rb1 also
 significantly decreased fasting blood glucose and improved glucose
 tolerance, and these effects were greater than those observed in
 pair-fed rats, suggesting that although Rb1's antihyperglycemic effect
 is partially attributable to reduced food intake and body weight; there
 may be additional effects of Rb1 on glucose homeostasis.
 CONCLUSIONS These results identify Rb1 as an antiobesity and
 antihyperglycemic agent. Diabetes 59:2505-2512, 2010
 SN 0012-1797
 PD OCT
 PY 2010
 VL 59
 IS 10
 BP 2505
 EP 2512
 DI 10.2337/db10-0315
 UT ISI:000283205700023
 PT J
 AU Lai, YS
 Shen, LH
 Zhang, ZZ
 Liu, WQ
 Zhang, YH
 Ji, H
 Tian, J
 AF Lai, Yisheng
 Shen, Lihong
 Zhang, Zhenzhen
 Liu, Wenqing
 Zhang, Yihua
 Ji, Hui
 Tian, Jide
 TI Synthesis and biological evaluation of furoxan-based nitric
 oxide-releasing derivatives of glycyrrhetinic acid as
 anti-hepatocellular carcinoma agents
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB A series of novel furoxan-based nitric oxide (NO)-releasing
 derivatives of glycyrrhetinic acid (GA) were designed, synthesized,
 and evaluated for their in vitro cytotoxicity against human
 hepatocellular carcinoma (HCC) and non-tumor liver cells. Five
 furoxan/GA hybrids, 7b-d, 7f, and 7g, displayed potent cytotoxicity
 against HCC cells (IC50: 0.25-1.10 mu M against BEL-7402 cells and
 1.32-6.78 mu M against HepG2 cells), but had a little effect on the
 growth of LO2 cells, indicating that these compounds had selective
 cytotoxicity against HCC cells. Furthermore, these compounds produced
 high concentrations of NO in HCC cells, but low in LO2 cells and
 treatment with hemoglobin partially reduced the cytotoxicity of the
 hybrid in HCC cells. Apparently, the high concentrations of NO produced
 by NO donor moieties and the bioactivity of GA synergistically
 contribute to the cytotoxicity, but the NO is a major player against
 HCC cells in vitro. Potentially, our findings may aid in the design
 of new chemotherapeutic reagents for the intervention of human HCC at
 clinic. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0960-894X
 PD NOV 15
 PY 2010
 VL 20
 IS 22
 BP 6416
 EP 6420
 DI 10.1016/j.bmcl.2010.09.070
 UT ISI:000283052900014
 PT J
 AU Hu, R
 Saw, CLL
 Yu, R
 Kong, ANT
 AF Hu, Rong
 Saw, Constance Lay-Lay
 Yu, Rong
 Kong, Ah-Ng Tony
 TI Regulation of NF-E2-Related Factor 2 Signaling for Cancer
 Chemoprevention: Antioxidant Coupled with Antiinflammatory
 SO ANTIOXIDANTS & REDOX SIGNALING
 AB Cancer chemoprevention is a process of using either natural or
 synthetic compounds to reduce the risk of developing cancer.
 Observations that NF-E2-related factor 2 (Nrf2)-deficient mice lack
 response to some chemopreventive agents point to the important role
 of Nrf2 in chemoprevention. Nrf2 is a member of basic-leucine zipper
 transcription factor family and has been shown to regulate gene
 expression by binding to a response element, antioxidant responsive
 element. It is generally believed that activation of Nrf2 signaling
 is an adaptive response to the environmental and endogenous stresses.
 Under homeostatic conditions, Nrf2 is suppressed by association with
 Kelch-like ECH-associated protein 1 (Keap1), but is stimulated upon
 exposure to oxidative or electrophilic stress. Once activated, Nrf2
 translocates into nuclei and upregulates a group of genes that act in
 concert to combat oxidative stress. Nrf2 is also shown to have
 protective function against inflammation, a pathological process that
 could contribute to carcinogenesis. In this review, we will discuss
 the current progress in the study of Nrf2 signaling, in particular,
 the mechanisms of Nrf2 activation by chemopreventive agents. We will
 also discuss some of the potential caveats of Nrf2 in cancer treatment
 and future opportunity and challenges on regulation of Nrf2-mediated
 antioxidant and antiinflammatory signaling in the context of cancer
 prevention. Antioxid. Redox Signal. 13, 1679-1698.
 SN 1523-0864
 PD DEC
 PY 2010
 VL 13
 IS 11
 BP 1679
 EP 1698
 DI 10.1089/ars.2010.3276
 UT ISI:000283053100006
 PT J
 AU Xie, YA
 Hao, HP
 Kang, A
 Liang, Y
 Xie, T
 Sun, SQ
 Dai, C
 Zheng, XA
 Xie, L
 Li, JA
 Wang, GJ
 AF Xie, Yuan
 Hao, Haiping
 Kang, An
 Liang, Yan
 Xie, Tong
 Sun, Shiqing
 Dai, Chen
 Zheng, Xiao
 Xie, Lin
 Li, Juan
 Wang, Guangji
 TI Integral pharmacokinetics of multiple lignan components in normal,
 CCl4-induced hepatic injury and hepatoprotective agents pretreated
 rats and correlations with hepatic injury biomarkers
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Although pharmacokinetic alternations by hepatic injury have been
 extensively studied, little is known about the potential influence of
 hepatoprotective agent's treatment. This study was aimed to
 investigate the holistic pharmacokinetics of multiple lignans, CYP3A
 regulations, and their correlations with hepatic injury biomarkers,
 in hepatic Injured rats pretreated with or without schisandra lignan
 extract (SLE) and dimethyl-diphenyl-bicarboxylate (DDB). Integral
 pharmacokinetics of multiple lignans based on an AUC-weighting
 approach was determined in normal, CCl4 induced hepatic injury rats
 pretreated with or without SLE and DDB Protein expression and
 activities of CYP3A were determined Pharmacokinetic parameters and
 CYP3A activities were correlated with serum alanine aminotransferase
 (ALT) and aspartate aminotransferase (AST) levels. CCl4 induced acute
 hepatic injury resulted in a nearly 8-fold enhancement of integral
 plasma exposures of multiple lignans, which was caused by the
 significant down-regulation of CYP3A. SLE and DDB pretreatment
 exhibited potent hepatoprotective effects, accompanied with the
 restored expression and activity of CYP3A, and the recovery of the
 respective and integral pharmacokinetics of lignans components. The
 integral AUC(0-tn) and CYP3A activities correlated well with ALT and
 AST. This study suggested that the pharmacokinetic regulating effects
 of hepatoprotective agent's on themselves and co-prescribed drugs
 should be of concern, and hepatic injury biomarkers may serve as good
 predictors (C) 2010 Elsevier Ireland Ltd. All rights reserved.
 SN 0378-8741
 PD SEP 15
 PY 2010
 VL 131
 IS 2
 BP 290
 EP 299
 DI 10.1016/j.jep.2010.06.038
 UT ISI:000282709100008
 PT J
 AU Cheng, YW
 Wang, YL
 Zhang, YH
 Peng, SX
 Chiou, GCY
 AF Cheng, Yu-Wen
 Wang, Yu-Liang
 Zhang, Yi-Hua
 Peng, Si-Xun
 Chiou, George C. Y.
 TI Proliferation of retinal pigment epithelial cells induced by
 (R,R)-XY-10 and (S,S)-XY-10 and their action mechanisms
 SO INTERNATIONAL JOURNAL OF OPHTHALMOLOGY
 AB AIM: To investigate the mechanism of proliferation effect induced by
 (R,R)-XY-10 and (S,S)-XY-10 on retinal pigmented epithelial cells
 (ARPE-19).
 METHODS: Human retinal pigmented epithelial cells (ARPE-19) and human
 umbilical vein endothelial cells (HUVECs) were used to investigate the
 effect of (R,R)-XY-10 and (S,S)-XY-10 on cell growth, and their
 mechanisms of proliferative action by using ERK, AKT, PI3K, Protein
 kinase C (PKC) and Nitric oxide synthase (NOS) inhibitors.
 RESULTS: (R,R)-XY-10 and (S,S)-XY-10 dose-dependently increased
 ARPE-19 cell proliferation, but not on HUVECs. When treated with
 proliferative inhibitors, H-7 (5 mu mol/L), hyperidn (20 mu mol/L),
 PD98059 (2 mu mol/L), LY294002 (50 mu mol/L), SH-5 (10 mu mol/L) and
 L-NAME (100 mu mol/L), the proliferative effect was reduced by H-7,
 hyperidn, PD98059 and LY294002, but not by SH-5 and L-NAME.
 CONCLUSION: (R,R)-XY-10 and (S,S)-XY-10 can induce cell proliferation
 through MAPK and PI3K dependent pathway.
 SN 1672-5123
 PD MAR 18
 PY 2010
 VL 3
 IS 1
 BP 9
 EP 13
 UT ISI:000282934100003
 PT J
 AU Ten, SC
 Gu, SY
 Niu, YF
 An, XF
 Yan, M
 He, M
 AF Ten, Shi-Chao
 Gu, Shou-Yong
 Niu, Yun-Fei
 An, Xiao-Fei
 Yan, Ming
 He, Ming
 TI Central Administration of Kisspeptin-10 Inhibits Water and Sodium
 Excretion of Anesthetized Male Rats and the Involvement of Arginine
 Vasopressin
 SO ENDOCRINE RESEARCH
 AB Aim. To investigate the effect of hypothalamus kisspeptin on water and
 sodium excretion and the possible mechanism. Method. The
 intracerebroventricular (icv) administration and radioimmunoassay
 were used to observe the effect of kisspeptin-10 on urine flow, sodium
 and potassium excretion, plasma arginine vasopressin (AVP), and atrial
 natriuretic peptide (ANP) concentrations in anesthetized male rats.
 The mediation of renal sympathetic nerve was also investigated by
 studies conducted on rats with bilateral renal sympathetic
 denervation. Results. The urine flow, sodium excretion, and free water
 clearance decreased significantly by icv injection of 5 nmol
 kisspeptin-10 (p < 0.05) from 30 to 60 min post-injection. Meanwhile,
 plasma AVP concentrations increased significantly 30 min after the icv
 injection of 5 nmol kisspeptin-10 (p < 0.05), whereas the equal dose
 of kisspeptin-10 did not significantly change plasma ANP
 concentrations. The mean arterial blood pressure, heart rate, and
 potassium excretion did not significantly change during the
 experiment. Furthermore, pretreatment with 5 nmol kisspeptin-10 could
 still significantly decrease urine flow and sodium excretion in renal
 sympathetic denervated rats. Conclusion. Central administration of
 kisspeptin-10 could inhibit sodium excretion and urine flow in
 anesthetized male rats, which is probably mediated by increasing the
 plasma AVP concentration and is independent of plasma ANP concentration
 and renal sympathetic nerve activity.
 SN 0743-5800
 PY 2010
 VL 35
 IS 3
 BP 128
 EP 136
 DI 10.3109/07435801003769995
 UT ISI:000282885600004
 PT J
 AU Hao, HP
 Lai, L
 Zheng, CN
 Wang, QO
 Yu, G
 Zhou, XY
 Wu, LA
 Gong, P
 Wang, GJ
 AF Hao, Haiping
 Lai, Li
 Zheng, Chaonan
 Wang, Qiong
 Yu, Guo
 Zhou, Xueyan
 Wu, Liang
 Gong, Ping
 Wang, Guangji
 TI Microsomal Cytochrome P450-Mediated Metabolism of Protopanaxatriol
 Ginsenosides: Metabolite Profile, Reaction Phenotyping, and
 Structure-Metabolism Relationship
 SO DRUG METABOLISM AND DISPOSITION
 AB Although the biotransformation of ginsenosides in the gastrointestinal
 tract has been extensively studied, much less is known about hepatic
 cytochrome P450 (P450)-catalyzed metabolism. The major aims of this
 study were to clarify the metabolic pathway and P450 isoforms involved
 and to explore the structure-metabolism relationship of
 protopanaxatriol (PPT)-type ginsenosides in hepatic microsomes.
 Efficient depletion of ginsenoside Rh1, Rg2, Rf, and PPT was found,
 whereas the elimination of Re and Rg1, characterized by a glucose
 substitution at the C20 hydroxy group, was negligible in microsomal
 incubation systems. Based on high-performance liquid chromatography
 hybrid ion trap and time-of-flight mass spectrometry analysis, the
 oxygenation metabolism on the C20 aliphatic branch chain was identified
 as the predominant metabolic pathway of PPT ginsenosides in both human
 and rat hepatic microsomes. By a comparison with authentic standards,
 the C24-25 double bond was identified as one of the oxygenation sites
 to produce the metabolites of C20-24 epoxide (ocotillol-type
 ginsenosides). Both chemical inhibition and human recombinant P450
 isoform assays indicated that CYP3A4 was the predominant isozyme
 responsible for the oxygenation metabolism of PPT ginsenosides. Enzyme
 kinetic evaluations in rat and human hepatic microsomes and human
 recombinant CYP3A4 isozyme incubation systems showed generally
 consistent results in that the intrinsic clearance ranked as Rf <= Rg2
 < Rh1 < PPT, closely correlating with logP values and the number of
 glycosyl substitutions. Results obtained from this study suggest that
 CYP3A4-catalyzed oxygenation metabolism plays an important role in the
 hepatic disposition of ginsenosides and that glycosyl substitution,
 especially at the C20 hydroxy group, determines their intrinsic
 clearances by CYP3A4.
 SN 0090-9556
 PD OCT
 PY 2010
 VL 38
 IS 10
 BP 1731
 EP 1739
 DI 10.1124/dmd.110.033845
 UT ISI:000281969200015
 PT J
 AU Liang, Y
 Hao, HP
 Xie, L
 Kang, A
 Xie, T
 Zheng, XA
 Dai, C
 Hao, K
 Sheng, LS
 Wang, GJ
 AF Liang, Yan
 Hao, Haiping
 Xie, Lin
 Kang, An
 Xie, Tong
 Zheng, Xiao
 Dai, Chen
 Hao, Kun
 Sheng, Longsheng
 Wang, Guangji
 TI Development of a Systematic Approach to Identify Metabolites for Herbal
 Homologs Based on Liquid Chromatography Hybrid Ion Trap Time-of-Flight
 Mass Spectrometry: Gender-Related Difference in Metabolism of
 Schisandra Lignans in Rats
 SO DRUG METABOLISM AND DISPOSITION
 AB Metabolic research for herbal medicine (HM) is a formidable task, which
 is still in its infancy due to complicated components in HM, complex
 metabolic pathways, and lack of authentic standards. The present work
 contributes to the development of a powerful technical platform to
 rapidly identify and classify metabolites of herbal components based
 on a liquid chromatography hybrid ion trap time-of-flight mass
 spectrometry. Taking Schisandra lignans extract as an example, the
 metabolic studies were completed both in vitro and in vivo. In the in
 vitro study, metabolites for five representative Schisandra lignans
 were identified and structurally characterized. The major metabolic
 pathways were summed as demethylation, hydroxylation, and
 demethylation and hydroxylation. In the in vivo study, 44 metabolites
 were detected in rat urine. These metabolites were identified and
 classified rapidly according to the metabolic rules obtained in the
 in vitro studies, and hydroxylation was confirmed as the primacy
 metabolic pathway for lignans in rat urine. In addition, "relative
 cumulative excretion" (RCE) for the metabolites in female and male rats
 were calculated according to their relative intensities in the urine
 samples collected at 0 to 12, 12 to 24, and 24 to 36 h. As a result,
 great gender-related difference on RCE was observed. For most
 metabolites, RCE in female rats was significantly lower than that in
 male rats. In conclusion, the presently developed methodology and
 approach on metabolic research for Schisandra lignans will find its
 wide use in metabolic studies for herbal medicines.
 SN 0090-9556
 PD OCT
 PY 2010
 VL 38
 IS 10
 BP 1747
 EP 1759
 DI 10.1124/dmd.110.033373
 UT ISI:000281969200017
 PT J
 AU Liu, YT
 Hao, HP
 Xie, HG
 Lai, L
 Wang, QO
 Liu, CX
 Wang, GJ
 AF Liu, Yi-Tong
 Hao, Hai-Ping
 Xie, Hong-Guang
 Lai, Li
 Wang, Qiong
 Liu, Chang-Xiao
 Wang, Guang-Ji
 TI Extensive Intestinal First-Pass Elimination and Predominant Hepatic
 Distribution of Berberine Explain Its Low Plasma Levels in Rats
 SO DRUG METABOLISM AND DISPOSITION
 AB Berberine, one of the most commonly used natural products, exhibits
 a poor plasma concentration-effect relationship whose underlying
 mechanisms remain largely unclear. This study was designed to test the
 hypothesis that extensive first-pass elimination and abundant tissue
 distribution of berberine may be its specific pharmacokinetic
 properties. For that, four different dosing routes, intragastric,
 intraduodenal, intraportal, and intravenous, were used to investigate
 the gastric, intestinal, and hepatic first-pass elimination of
 berberine. After intragastric dosing, approximately half of berberine
 ran intact through the gastrointestinal tract and another half was
 disposed of by the small intestine, leading to an extremely low extent
 of absolute oral bioavailability in rats (0.36%). Moreover, the major
 berberine metabolites were identified and quantified in rat enterocyte
 S9 fractions, portal vein plasma, and intestinal perfusates; plasma
 concentrations and tissue distribution of berberine and its major
 metabolites were determined as well. Data indicated that M1, M2
 glucuronide, and M3 were the major metabolites generated from the small
 intestine and that there was a 70-fold increase in the ratio of the
 area under the concentration-time curve value for berberine (liver
 versus plasma). We conclude that intestinal first-pass elimination of
 berberine is the major barrier of its oral bioavailability and that
 its high extraction and distribution in the liver could be other
 important factors that lead to its low plasma levels in rats.
 SN 0090-9556
 PD OCT
 PY 2010
 VL 38
 IS 10
 BP 1779
 EP 1784
 DI 10.1124/dmd.110.033936
 UT ISI:000281969200020
 PT J
 AU Hao, C
 Zhang, YH
 Jiang, YW
 Ma, DW
 AF Hao Chao
 Zhang Yihua
 Jiang Yongwen
 Ma Dawei
 TI CuBr/N,N-Dimethylglycine-Catalyzed Coupling Reaction of
 2-Chlorotrifluoroacetanilides with Phenols at Mild Conditions
 SO CHINESE JOURNAL OF CHEMISTRY
 AB The ortho-substituent effect directed by the CF3CONH group exists in
 CuBr/N,N-dimethylglycine-catalyzed diaryl ether formation from
 o-chlorotrifluoroacetanilides and phenols, leading to this coupling
 reaction proceeding at 80 degrees C to afford a wide range of diaryl
 ethers. The halogen-exchange also plays an important role in this
 transformation because adding potassium iodide is essential for
 complete conversion.
 SN 1001-604X
 PD SEP
 PY 2010
 VL 28
 IS 9
 BP 1645
 EP 1650
 DI 10.1002/cjoc.201090279
 UT ISI:000282998700022
 PT J
 AU Tian, HY
 Wang, L
 Zhang, XQ
 Wang, Y
 Zhang, DM
 Jiang, RW
 Liu, Z
 Liu, JS
 Li, YL
 Ye, WC
 AF Tian, Hai-Yan
 Wang, Lei
 Zhang, Xiao-Qi
 Wang, Ying
 Zhang, Dong-Mei
 Jiang, Ren-Wang
 Liu, Zhong
 Liu, Jun-Shan
 Li, Yao-Lan
 Ye, Wen-Cai
 TI Bufogargarizins A and B: Two Novel 19-Norbufadienolides with
 Unprecedented Skeletons from the Venom of Bufo bufo gargarizans
 SO CHEMISTRY-A EUROPEAN JOURNAL
 SN 0947-6539
 PY 2010
 VL 16
 IS 36
 BP 10989
 EP 10993
 DI 10.1002/chem.201000847
 UT ISI:000283015500013
 PT J
 AU Jiang, B
 Zeng, Y
 Li, MJ
 Xu, JY
 Zhang, YN
 Wang, QJ
 Sun, NY
 Lu, T
 Wu, XM
 AF Jiang, Bo
 Zeng, Yi
 Li, Meng-Jie
 Xu, Jin-Yi
 Zhang, Yong-Na
 Wang, Qiu-Juan
 Sun, Ni-Yue
 Lu, Tao
 Wu, Xiao-Ming
 TI Design, Synthesis, and Biological Evaluation of
 1,5-Diaryl-1,2,4-triazole Derivatives as Selective Cyclooxygenase-2
 Inhibitors
 SO ARCHIV DER PHARMAZIE
 AB A series of 1,5-diaryl-1,2,4-triazole derivatives were synthesized and
 evaluated as cyclooxygenase-2 (COX-2) inhibitors. The results of the
 preliminary biological assays in vivo showed that eight compounds 5b,
 6b, 6c, 7c, 8b, 8d, 9c, and 9d have potent anti-inflammatory activity
 (P < 0.01), while compounds 6b, 6c, and 9c exhibit marked potency.
 Compound 6c was then selected for further investigation. In the COX
 inhibition assay in vitro, compound 6c was identified as a potent and
 selective inhibitor of COX-2 (COX-2 IC50 = 0.37 mu M; SI = 0.018), being
 equipotent to celecoxib (COX-2 IC50 = 0.26 mu M; SI = 0.015). In a rat
 carrageenan-induced paw edema assay, 6c exhibited moderate
 anti-inflammatory activity (35% inhibition of inflammation) at 2 h
 after administration of 15 mg/kg as an oral dose. A docking study also
 revealed that compound 6c binds in the active site of COX-2 in a similar
 mode to that of the known selective COX-2 inhibitor SC-558.
 SN 0365-6233
 PD SEP
 PY 2010
 VL 343
 IS 9
 BP 500
 EP 508
 DI 10.1002/ardp.200900227
 UT ISI:000282793400002
 PT J
 AU A, JY
 Qian, SX
 Wang, GJ
 Yan, B
 Zhang, SJ
 Huang, Q
 Ni, LN
 Zha, WB
 Liu, LS
 Cao, B
 Hong, M
 Wu, HX
 Lu, H
 Shi, JA
 Li, MJ
 Li, J
 AF A, Jiye
 Qian, Sixuan
 Wang, Guangji
 Yan, Bei
 Zhang, Sujiang
 Huang, Qing
 Ni, Lingna
 Zha, Weibin
 Liu, Linsheng
 Cao, Bei
 Hong, Ming
 Wu, Hanxin
 Lu, Hua
 Shi, Jian
 Li, Mengjie
 Li, Jianyong
 TI Chronic Myeloid Leukemia Patients Sensitive and Resistant to Imatinib
 Treatment Show Different Metabolic Responses
 SO PLOS ONE
 AB The BCR-ABL tyrosine kinase inhibitor imatinib is highly effective for
 chronic myeloid leukemia (CML). However, some patients gradually
 develop resistance to imatinib, resulting in therapeutic failure.
 Metabonomic and genomic profiling of patients' responses to drug
 interventions can provide novel information about the in vivo
 metabolism of low-molecular-weight compounds and extend our insight
 into the mechanism of drug resistance. Based on a multi-platform of
 high-throughput metabonomics, SNP array analysis, karyotype and
 mutation, the metabolic phenotypes and genomic polymorphisms of CML
 patients and their diverse responses to imatinib were characterized.
 The untreated CML patients (UCML) showed different metabolic patterns
 from those of healthy controls, and the discriminatory metabolites
 suggested the perturbed metabolism of the urea cycle, tricarboxylic
 acid cycle, lipid metabolism, and amino acid turnover in UCML. After
 imatinib treatment, patients sensitive to imatinib (SCML) and patients
 resistant to imatinib (RCML) had similar metabolic phenotypes to those
 of healthy controls and UCML, respectively. SCML showed a significant
 metabolic response to imatinib, with marked restoration of the
 perturbed metabolism. Most of the metabolites characterizing CML were
 adjusted to normal levels, including the intermediates of the urea
 cycle and tricarboxylic acid cycle (TCA). In contrast, neither
 cytogenetic nor metabonomic analysis indicated any positive response
 to imatinib in RCML. We report for the first time the associated genetic
 and metabonomic responses of CML patients to imatinib and show that
 the perturbed in vivo metabolism of UCML is independent of imatinib
 treatment in resistant patients. Thus, metabonomics can potentially
 characterize patients' sensitivity or resistance to drug intervention.
 SN 1932-6203
 PD OCT 8
 PY 2010
 VL 5
 IS 10
 AR e13186
 DI 10.1371/journal.pone.0013186
 UT ISI:000282676700005
 PT J
 AU Zhang, HW
 Zhang, J
 Hu, S
 Zhang, ZJ
 Zhu, CJ
 Ng, SW
 Tan, RX
 AF Zhang, Hua-Wei
 Zhang, Jie
 Hu, Sha
 Zhang, Zun-Jian
 Zhu, Cheng-Jian
 Ng, Seik Weng
 Tan, Ren-Xiang
 TI Ardeemins and Cytochalasins from Aspergillus terreus Residing in
 Artemisia annua
 SO PLANTA MEDICA
 AB Three new alkaloids, 15b-dehydro-5-N-acetylardeemin (3),
 10-phenyl-[12]-cytochalasins Z16 (6) andZ17(7), were characterized
 from the liquid culture of the endophytic fungus Aspergillus terreus
 IFB-E030 along with six known derivatives, 5-N-acetylardeemin (1),
 15b-beta-hydroxyl-5-N-acetylardeemin (2), cytochalasin E (4),
 rosellichalasin (5), cytochalasins Z11 (8), and Z13 (9). The structures
 of the new metabolites were established mainly by a combination of their
 1D- and 2D-NMR spectra, single crystal X-ray diffraction, and the
 modified Mosher reaction. Biological assays indicated that
 cytochalasin Z17 (7) had moderate cytotoxicity against human
 nasopharyngeal epidermoid tumor KB cell line with an IC50 value of 26.2
 mu M.
 SN 0032-0943
 PD OCT
 PY 2010
 VL 76
 IS 14
 BP 1616
 EP 1621
 DI 10.1055/s-0030-1249781
 UT ISI:000282366800023
 PT J
 AU Zhang, XY
 Qiao, H
 Liu, JP
 Dong, HJ
 Shen, CL
 Ni, JM
 Shi, YB
 Xu, Y
 AF Zhang, Xiaoyun
 Qiao, Hua
 Liu, Jianping
 Dong, Haijun
 Shen, Chenlin
 Ni, Jingman
 Shi, Yanbin
 Xu, Ying
 TI Dihydroartemisinin loaded nanostructured lipid carriers (DHA-NLC):
 Evaluation of pharmacokinetics and tissue distribution after
 intravenous administration to rats
 SO PHARMAZIE
 AB A simple and rapid LC-MS/MS method was established for the
 determination of dihydroartemisinin (DHA) in plasma and tissues of
 rats. Sample preparation was achieved by liquid liquid extraction with
 aether and analysis was performed on LC-MS/MS in positive ion mode using
 electrospray ionization (ESI) as an interface. Target compounds were
 quantified in a single ion-monitoring (SIM) mode. DHA was monitored
 at m/z 267.1 and the internal standard finasteride at m/z 305.2.
 Chromatography was carried out using a Synergi fusion RP 80 column with
 a mixture of ethanol and 0.1% formic acid mixture (75:25) as the mobile
 phase. The pharmacokinetics and tissue distribution after intravenous
 administration of DHA in nanostructured lipid carrier (NLC) and in
 solution were then compared. The mean residence times (MRT) of the
 DHA-NLC was much longer than that of the DHA solution. In the tested
 organs, the AUC values of the DHA-NLC were higher than that of the DHA
 solution in liver, spleen, lung, brain and muscle, and lower than the
 DHA solution in heart and kidney. DHA-NLC prepared in this study is
 a promising sustained-release and drug-targeting system for antitumor
 drugs. It may also allow a reduction in dosage and a decrease in systemic
 toxicity.
 SN 0031-7144
 PD SEP
 PY 2010
 VL 65
 IS 9
 BP 670
 EP 678
 DI 10.1691/ph.2010.0082
 UT ISI:000282457400007
 PT J
 AU Huang, FJ
 Wu, T
 AF Huang, Feng-Jie
 Wu, Tong
 TI PURIFICATION AND CHARACTERIZATION OF A NEW PEPTIDE (S-8300) FROM SHARK
 LIVER
 SO JOURNAL OF FOOD BIOCHEMISTRY
 AB S-8300, a small (8200.901 Da) antidiabetic peptide, was purified and
 characterized from shark livers (Chiloscyllium plagiosum). It was
 isolated by extraction of the water-soluble fraction, dialysis,
 ultrafiltration and dicthylaminoethyl Sepharose, Bio-Gel P-10 and fast
 protein liquid chromatography monoQ chromatography. The new peptide
 (S-8300) contained 17 amino acids and the 15 N-terminal amino acid
 residues of S-8300 were
 NH2-Met-Leu-Val-Gly-Pro-Ile-Gly-Ala-Ala-Lys-Val-Val-Tyr-Glu-Gln-.
 The new peptide was stable at 95C for 30 min and stable between pH 3.0
 and 9.0. It was not inactivated by DNase and RNase, but totally
 inactivated by trypsin and proteinase K digestion. In addition, S-8300
 could remarkably protect the structure integrity and recover the damage
 of NIT-1 cell after exposure to the toxin of streptozotocin. Homology
 search of NH2-terminal sequence showed that S-8300 was a totally new
 protein.
 PRACTICAL APPLICATIONS
 The experiments suggested that S-8300 could reduce the adverse effect
 of beta-cell toxins and protect the structure integrity and mitigate
 the damage. S-8300 could markedly decrease the level of fasting plasma
 glucose, glycohemoglobin-A1, triglyceride, cholesterol, free fatty
 acid and malondialdehyde, increased the activity of superoxide
 dismutase and attenuated the injury of beta-cell in pancreatic islet.
 Therefore, S-8300 has a significant protective effect on diabetes in
 mice. These might indicate that S-8300 could have clinical therapy
 significance.
 SN 0145-8884
 PD OCT
 PY 2010
 VL 34
 IS 5
 BP 962
 EP 970
 DI 10.1111/j.1745-4514.2010.00336.x
 UT ISI:000282637300005
 PT J
 AU Zhipeng, C
 Jiabi, Z
 Hongxuan, C
 Yan-yu, X
 Jun, C
 Cai, BC
 AF Zhipeng, C.
 Jiabi, Z.
 Hongxuan, C.
 Yan-yu, X.
 Jun, C.
 Cai, Bao-chang
 TI Distribution of liposomal bifendate in liver following intravenous
 injection in mice
 SO JOURNAL OF DRUG TARGETING
 AB The purpose of this study was to develop and study the behaviors of
 bifendate (DDB) liposome in vivo. DDB liposome was prepared by the
 rotary evaporationextrusion method. The particle size,
 zeta-potential, encapsulation efficiency (EE), and in vitro drug
 release from liposome were determined and the in vivo studies were
 tested in mice and rats. The concentrations of DDB in plasma and liver
 at different sampling time points were determined by RP-HPLC. The liver
 concentration time curves of DDB liposome and free drug solution in
 mice were determined, and the pharmacokinetic parameters in rats and
 mice were calculated and compared by statistical analysis. The average
 liposome diameter was 323 +/- 29 nm (n=3) and the EE was 91.52 +/- 2.38%.
 There were significantly different parameters of k10 and area under
 the plasma concentrationtime curve (AUC(0-T)) between liposome and
 solution. The mean residence time (MRT0-T) in plasma of liposomal
 formulation was 3.72 times longer than that of solution. Compared with
 solution, DDB liposome delivered about 2.57 times higher DDB into
 liver. Thus, an optimum intravenous liposonne formulation for DDB could
 be developed as an alternative to the commercial DDB preparations.
 SN 1061-186X
 PD SEP
 PY 2010
 VL 18
 IS 8
 BP 627
 EP 636
 DI 10.3109/10611861003639788
 UT ISI:000281961600006
 PT J
 AU Li, NG
 Shi, ZH
 Tang, YP
 Yang, JP
 Wang, ZJ
 Song, SL
 Lu, TL
 Duan, JA
 AF Li, Nian-Guang
 Shi, Zhi-Hao
 Tang, Yu-Ping
 Yang, Jian-Ping
 Wang, Zhen-Jiang
 Song, Shu-Lin
 Lu, Tu-Lin
 Duan, Jin-Ao
 TI Targeting the Development of Resveratrol as a Chemopreventive Agent
 SO DRUG DEVELOPMENT RESEARCH
 AB Tumor development consists of several separate, but closely linked,
 stages: tumor initiation, promotion, and progression. This long and
 complex process provides opportunities for intervention both in
 preventing cancer initiation and in treating the neoplasm during its
 premalignant stages. Resveratrol, a polyphenolic compound found in
 many plant species, including grapes, peanuts, and various herbs, has
 recently been investigated intensely for its cancer chemopreventive
 property. The present work is an overview of the chemopreventive
 mechanisms of resveratrol in anti-initiation, anti-promotion, and
 anti-progression. These, together with the low toxicity of
 resveratrol, suggest promise for novel chemopreventive agents.
 However, the low bioavailability and rapid clearance of resveratrol
 from the circulation require the design of new resveratrol-like
 chemopreventive agents, the structural modifications and the structure
 activity relationship of which are also discussed in this review. Drug
 Dev Res 71:335-350, 2010. (C) 2010 Wiley-Liss, Inc.
 SN 0272-4391
 PD SEP
 PY 2010
 VL 71
 IS 6
 BP 335
 EP 350
 DI 10.1002/ddr.20380
 UT ISI:000282539900002
 PT J
 AU Chen, YJ
 Tao, JA
 Xiong, F
 Zhu, JB
 Gu, N
 Zhang, YH
 Ding, Y
 Ge, LA
 AF Chen Yue-Jian
 Tao Juan
 Xiong Fei
 Zhu Jia-Bi
 Gu Ning
 Zhang Yi-Hua
 Ding Ye
 Ge Liang
 TI Synthesis, self-assembly, and characterization of PEG-coated iron
 oxide nanoparticles as potential MRI contrast agent
 SO DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
 AB Aim: Investigated the self-assembly and characterization of novel
 antifouling polyethylene glycol (PEG)-coated iron oxide nanoparticles
 as nanoprobes for magnetic resonance imaging (MRI) contrast agent.
 Method: Monodisperse oleic acid-coated superparamagnetic iron oxide
 cores are synthesized by thermal decomposition of iron oleate. The
 self-assembly behavior between iron oxide cores and PEG-lipid
 conjugates in water and their characteristics are confirmed by
 transmission electron microscope, X-ray diffraction,
 thermogravimetric analysis, Fourier transform infrared spectroscopy,
 and vibrating sample magnetometer. Result: Dynamic light scattering
 shows superparamagnetic iron oxide nanoparticles coated with PEG are
 stable in water for pH of 3-10 and ionic strengths up to 0.3 M NaCl,
 and are protein resistant in physiological conditions. Additionally,
 in vitro MRI study demonstrates the efficient magnetic resonance
 imaging contrast characteristics of the iron oxide nanoparticles.
 Conclusion: The result indicates that the novel antifouling PEG-coated
 superparamagnetic iron oxide nanoparticles could potentially be used
 in a wide range of applications such as biotechnology, MRI, and magnetic
 fluid hyperthermia.
 SN 0363-9045
 PD OCT
 PY 2010
 VL 36
 IS 10
 BP 1235
 EP 1244
 DI 10.3109/03639041003710151
 UT ISI:000282523500011
 PT J
 AU Cao, F
 Zhang, XL
 Ping, QN
 AF Cao, Feng
 Zhang, Xiaolin
 Ping, Qineng
 TI New method for ophthalmic delivery of azithromycin by
 poloxamer/carbopol-based in situ gelling system
 SO DRUG DELIVERY
 AB This study focused on preparation and evaluation of a thermosensitive
 and mucoadhesive in situ gelling ophthalmic system of azithromycin
 (ATM). Poloxamer 407 (P407) and poloxamer 188 (P188) were used as
 gelling agents. Addition of Carbopol 974P (CP 974P) to the gelling
 systems could increase the solubility of ATM by salt effect and enhance
 the mucoadhesive property of the systems. Gelation temperature of these
 systems ranged from 31.21-36.31 degrees C depending on the ratio of
 P407 and P188. Mucoadhesion force of the system composed of
 P407/P188/CP 974P (21/5/0.3%, w/v) was 2.3-fold that without carbopol
 974P. Viscosity of the formulation was in a suitable range at 25 degrees
 C and pseudoplastic behavior was observed at 35 degrees C. The
 formulation exhibited a 24-h sustained release of ATM. In vivo resident
 experiments showed AUC(0-12) of ATM in rabbit tears increased by
 1.78-fold for in situ gel compared with eye drop. At 12 h, tear
 concentrations exceeded minimum inhibitory concentration (MIC)
 breakpoint for the most common causative pathogens of bacterial
 conjunctivitis by 2.8-fold. Results in vitro and in vivo indicated that
 this droppable gel performed better than ATM eye drop did.
 SN 1071-7544
 PD SEP-OCT
 PY 2010
 VL 17
 IS 7
 BP 500
 EP 507
 DI 10.3109/10717544.2010.483255
 UT ISI:000282521100003
 PT J
 AU Xia, XF
 Yang, JA
 Li, FH
 Li, Y
 Zhou, XB
 Dai, Y
 Wong, STC
 AF Xia, Xiaofeng
 Yang, Jian
 Li, Fuhai
 Li, Ying
 Zhou, Xiaobo
 Dai, Yue
 Wong, Stephen T. C.
 TI Image-Based Chemical Screening Identifies Drug Efflux Inhibitors in
 Lung Cancer Cells
 SO CANCER RESEARCH
 AB Cancer cells with active drug efflux capability are multidrug resistant
 and pose a significant obstacle for the efficacy of chemotherapy.
 Moreover, recent evidence suggests that high drug efflux cancer cells
 (HDECC) may be selectively enriched with stem-like cancer cells, which
 are believed to be the cause for tumor initiation and recurrence. There
 is a great need for therapeutic reagents that are capable of eliminating
 HDECCs. We developed an image-based high-content screening (HCS)
 system to specifically identify and analyze the HDECC population in
 lung cancer cells. Using the system, we screened 1,280
 pharmacologically active compounds that identified 12 potent HDECC
 inhibitors. It is shown that these inhibitors are able to overcome
 multidrug resistance (MDR) and sensitize HDECCs to chemotherapeutic
 drugs, or directly reduce the tumorigenicity of lung cancer cells
 possibly by affecting stem-like cancer cells. The HCS system we
 established provides a new approach for identifying therapeutic
 reagents overcoming MDR. The compounds identified by the screening may
 potentially be used as potential adjuvant to improve the efficacy of
 chemotherapeutic drugs. Cancer Res; 70(19); 7723-33. (C) 2010 AACR.
 SN 0008-5472
 PD OCT 1
 PY 2010
 VL 70
 IS 19
 BP 7723
 EP 7733
 DI 10.1158/0008-5472.CAN-09-4360
 UT ISI:000282647700036
 PT J
 AU Tian, HL
 Yu, T
 Xu, NN
 Feng, C
 Zhou, LY
 Luo, HW
 Chang, DC
 Le, XF
 Luo, KQ
 AF Tian, Hong-Lei
 Yu, Ting
 Xu, Nai-Ning
 Feng, Chao
 Zhou, Li-Ying
 Luo, Hou-Wei
 Chang, Donald C.
 Le, Xiao-Feng
 Luo, Kathy Qian
 TI A novel compound modified from tanshinone inhibits tumor growth in vivo
 via activation of the intrinsic apoptotic pathway
 SO CANCER LETTERS
 AB A novel compound, acetyltanshinone IIA (ATA) was obtained from chemical
 modifications of tanshinone TIIA (TIIA) isolated from a medicinal
 plant, Salvia miltiorrhiza. ATA exhibited increased water solubility
 and stronger apoptotic activity on multiple cancer cell lines than
 TIIA. ATA displayed a higher growth inhibition ability on breast cancer
 especially HER2 positive cells than normal cells and it inhibited
 xenografted tumor growth in mice. Mechanistic studies showed that ATA
 could induce significant reactive oxygen species (ROS) generation, Bax
 translocation to mitochondria, resulting in mitochondria damage,
 cytochrome c release, caspase-3 activation and apoptotic cell death.
 ATA-mediated ROS production and its downstream apoptotic events could
 be blocked by an antioxidant agent, propyl gallate, indicating the
 prominent role of ROS in ATA-induced apoptosis. Overexpression of Bcl-2
 protein reduced ATA-induced cell death. In conclusion, ATA is a novel
 anticancer agent with potent in vitro and in vivo anticancer ability.
 ROS-mediated Bax activation should be the mechanism by which ATA
 induces apoptosis and inhibits tumor growth. (C) 2010 Elsevier Ireland
 Ltd. All rights reserved.
 SN 0304-3835
 PD NOV 1
 PY 2010
 VL 297
 IS 1
 BP 18
 EP 30
 DI 10.1016/j.canlet.2010.04.020
 UT ISI:000282715000003
 PT J
 AU Wang, L
 Ling, Y
 Chen, Y
 Li, CL
 Feng, F
 You, QD
 Lu, N
 Guo, QL
 AF Wang, Ling
 Ling, Yun
 Chen, Yan
 Li, Cheng-Ling
 Feng, Feng
 You, Qi-Dong
 Lu, Na
 Guo, Qing-Long
 TI Flavonoid baicalein suppresses adhesion, migration and invasion of
 MDA-MB-231 human breast cancer cells
 SO CANCER LETTERS
 AB Baicalein is a widely used Chinese herbal medicine that has been used
 historically in anti-inflammatory and anti-cancer therapy. However,
 the molecular mechanism of its anti-cancer activity remains poorly
 understood and warrants further investigations. The purpose of this
 study is to verify the activity of baicalein to inhibit the invasion
 of MDA-MB-231 human breast cancer cells. The results indicated that
 baicalein suppressed MDA-MB-231 cell adhesion to fibronectin-coated
 substrate, wound healing migration and invasion through the Matrigel
 in a concentration-dependent manner. Western blot and gelatin
 zymography analysis showed that baicalein significantly inhibited the
 expression and secretion of matrix metalloproteinases 2/9 (MMP-2/9)
 in MDA-MB-231 cells. Additionally, treatment of MDA-MB-231 cells with
 baicalein down-regulated the expression of MMP-2/9 involved
 mitogen-activated protein kinases (MAPK) signaling pathway. Taken
 together, baicalein had potential to suppress the adhesion, migration
 and invasion of MDA-MB-231 cancer cells in vitro and it could serve
 as a promising drug for the treatment of cancer metastasis. (C) 2010
 Elsevier Ireland Ltd. All rights reserved.
 SN 0304-3835
 PD NOV 1
 PY 2010
 VL 297
 IS 1
 BP 42
 EP 48
 DI 10.1016/j.canlet.2010.04.022
 UT ISI:000282715000005
 PT J
 AU Zhou, L
 Wang, W
 Feng, YY
 Wei, SH
 Zhou, JH
 Yu, BY
 Shen, JA
 AF Zhou, Lin
 Wang, Wei
 Feng, Yuying
 Wei, Shaohua
 Zhou, Jiahong
 Yu, Boyang
 Shen, Jian
 TI Delivering a hydrophobic anticancer drug for photodynamic therapy by
 amorphous formulation
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB An amorphous formulation of hypocrellin A for photodynamic therapy is
 reported which can provide stable aqueous dispersion of such
 hydrophobic photosensitizers. In vitro studies have demonstrated the
 active uptake of amorphous formulation of hypocrellin A into the
 mitochondria of tumor cells. Compared with Tween-80 micelle embedded
 hypocrellin A, low dark-toxicity but similar light-toxicity of the
 amorphous one to drug impregnated tumor cells was observed. Thus, the
 potential of using amorphous formulation of hypocrellin A as drug
 delivery system for photodynamic therapy has been demonstrated. (C)
 2010 Elsevier Ltd. All rights reserved.
 SN 0960-894X
 PD NOV 1
 PY 2010
 VL 20
 IS 21
 BP 6172
 EP 6174
 DI 10.1016/j.bmcl.2010.08.132
 UT ISI:000282677900001
 PT J
 AU Du, JL
 Wu, GF
 Wang, JL
 AF Du, Jinli
 Wu, Guangfen
 Wang, Jinlan
 TI Density Functional Theory Study of the Interaction of Carbon Monoxide
 with Bimetallic Co-Mn Clusters
 SO JOURNAL OF PHYSICAL CHEMISTRY A
 AB Using spin-polarized density functional calculations, we have studied
 the interaction of carbon monoxide (CO) with bimetallic ConMn (n = 1-6)
 and ConMn6-n (n = 0-6) clusters. Various adsorption sites including
 atop, hollow, and bridge adsorption patterns and different possible
 spin states are considered. The CO molecule prefers to adsorb at the
 Co site rather than at the Mn site. Atop adsorption structure is
 energetically more favored over the hollow and bridge adsorption ones
 for the bimetallic clusters with an exception of Co5Mn. Large
 adsorption energy is found at Co3Mn, Co2Mn4, and Co3Mn3, associating
 with the relative stability of the bare Co Mn clusters and the
 electrostatic interactions as well as adsorption patterns. The
 activation of the C-O bond and the red shift of the C-O stretching
 frequency are sensitive to the adsorption sites and high chemical
 activity is identified for Co-6, Co5Mn, and Mn-6 clusters. More
 interestingly, the adsorption of CO has different influence on the
 magnetism of the clusters: the magnetic moment remains unchanged for
 CoMn and Co2Mn, while it is reduced by 2 mu(B) for ConMn (n = 3-6) and
 Co Mn6-n (n = 0-5) and is enhanced by 2 mu(B) for Mn-6 when a CO molecule
 is loaded to the cluster.
 SN 1089-5639
 PD OCT 7
 PY 2010
 VL 114
 IS 39
 BP 10508
 EP 10514
 DI 10.1021/jp106321s
 UT ISI:000282210000005
 PT J
 AU Yu, LZ
 Jiye, A
 Sun, M
 Xu, J
 Cheng, LP
 Shi, RH
 AF Yu, Lianzhen
 Jiye, A.
 Sun, Min
 Xu, Jin
 Cheng, Liping
 Shi, Ruihua
 TI Research on metabolic phenotype of gastric cancer tissue and plasma
 by gas chromatography-time of flight mass spectrometry
 SO JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY
 SN 0815-9319
 PD SEP
 PY 2010
 VL 25
 SU Suppl. 2
 BP A140
 EP A140
 UT ISI:000282181400458
 PT J
 AU Xu, Y
 Jin, XF
 Ping, QN
 Cheng, JA
 Sun, MJ
 Cao, F
 You, WL
 Yuan, DF
 AF Xu, Ying
 Jin, Xuefeng
 Ping, Qineng
 Cheng, Juan
 Sun, Minjie
 Cao, Feng
 You, Weiliang
 Yuan, Dongfen
 TI A novel lipoprotein-mimic nanocarrier composed of the modified protein
 and lipid for tumor cell targeting delivery
 SO JOURNAL OF CONTROLLED RELEASE
 AB Ursodeoxycholic acid (UA) modified protein-lipid nanocomplex (uP-LNC)
 as a novel biomimetic nanocarrier was developed for tumor-targeting
 delivery. Bovine serum albumin (BSA) was used as a model protein and
 its amino groups were covalently modified by UA. Lipid nanoparticle
 (LNP) composed of phospholipids, triglycerides and octadecylamine was
 prepared by using solvent evaporation method and was used as the core.
 UA modified BSA (uP) was attached onto the surface of LNP by post-insert
 method and generated the protein-lipid nanocomplex. As the control,
 cholesteryl hemiglutarate (CH), a non-targeting ligand was also used
 to modify BSA and then formed CH modified protein-lipid nanocomplex
 (cP-LNC). The combining efficiency of modified BSA with LNP, determined
 by Bradford protein assay, increased with the enhancement of
 substitution degree. The modified BSA and nanocomplex were
 characterized for the substitute degree, average molecular weight,
 surface tension, particle size and zeta potential by various
 physicochemical analyses. In vitro dissolution tests and cell uptake
 studies were performed by loading coumarin-6 as a fluorescent probe.
 The results indicated that the UA modified protein attached on the
 nanoparticles significantly decreased drug release from the
 nanocomplex in pH 7.4 medium, The uptake of uP-LNC was higher in hepatic
 carcinoma cells (HepG2 and Bel 7402) than in normal liver cells (L02).
 Furthermore, the uptake of uP-LNC was significantly higher than that
 of cP-LNC and LNP in these cells. The uptake was dependent on time,
 temperature and concentration, and could be inhibited by free UA. In
 addition, the MTT assay of uP-LNC and u(x)P with various degrees of
 substitution showed very low cytotoxicity at tested concentrations in
 all cells. The UA modification served to facilitate the specific
 receptor and energy mediated endocytosis process of the protein-lipid
 nanocomplex and enabled this nanocomplex to be a potential nanocarrier
 for tumor-targeting drug delivery. (c) 2010 Elsevier B.V. All rights
 reserved.
 SN 0168-3659
 PD SEP 15
 PY 2010
 VL 146
 IS 3
 BP 299
 EP 308
 DI 10.1016/j.jconrel.2010.05.022
 UT ISI:000282398100005
 PT J
 AU Xu, HM
 Wei, J
 Pan, L
 Lin, HY
 Wang, WQ
 Zhang, YH
 Shen, ZL
 AF Xu, Han-Mei
 Wei, Jin
 Pan, Li
 Lin, Hongying
 Wang, Weiqiang
 Zhang, Yihua
 Shen, Zilong
 TI The Mechanism of (R,R) ZX-5 on Increasing NO Release
 SO INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
 AB (R,R) ZX-5 has been proven to have positive effects on choroidal blood
 flow without affecting the sclera and ciliary bodies in New Zealand
 white rabbits. This study was designed to investigate the mechanisms
 of (R,R) ZX-5 on improving the choroidal blood flow and promoting NO
 production. HUVECs (human umbilical vein endothelial cells) were used
 to determine the production of eNOS, p-eNOS, AKT and Erk1/2 by Western
 blot analysis. iNOS and eNOS mRNA levels were investigated by RT-PCR
 and the effect of (R,R) ZX-5 on NO production were determined by eNOS
 activity assay. We found (R,R) ZX-5 upregulated protein expression of
 eNOS and iNOS, increased NO production, and reduced ERK and Akt protein
 level. Therefore, (R,R) ZX-5 may promote the choroidal blood flow in
 New Zealand white rabbits without affecting the blood flow in the iris
 or ciliary bodies via increasing NO production. These results suggest
 that (R,R) ZX-5 may function to cure and prevent Age-related macular
 degeneration (AMD).
 SN 1422-0067
 PD SEP
 PY 2010
 VL 11
 IS 9
 BP 3323
 EP 3333
 DI 10.3390/ijms11093323
 UT ISI:000282223500019
 PT J
 AU Yang, J
 Ding, L
 Hu, LL
 Jin, SH
 Liu, WY
 Wang, ZZ
 Xiao, W
 You, QD
 Guo, QL
 AF Yang, Jing
 Ding, Li
 Hu, Linlin
 Jin, Shaohong
 Liu, Wenyuan
 Wang, Zhenzhong
 Xiao, Wei
 You, Qidong
 Guo, Qinglong
 TI Comparison of electron capture-atmospheric pressure chemical
 ionization and electrospray ionization for the analysis of gambogic
 acid and its main circulating metabolite in dog plasma
 SO EUROPEAN JOURNAL OF MASS SPECTROMETRY
 AB Gambogic acid (GA), a promising anticancer candidate, is a
 polyprenylated xanthone abundant in the resin of Garcinia morella and
 Garcinia hanburyi. Electron capture-atmospheric pressure chemical
 ionization (EC-APCI) and electrospray ionization (ESI) techniques,
 both in the negative ion mode, were evaluated regarding ionization,
 fragmentation patterns and sensitivity for simultaneous liquid
 chromatography-tandem mass spectrometry (LC-MS/MS) analysis of GA and
 its main circulating metabolite, 10-hydroxygambogic acid (10-OHGA) in
 dog plasma. Both analytes underwent extensive in-source fragmentation
 in EC-APCI, which was not desirable for reliable quantification of
 these analytes, whereas the substitution of ESI for EC-APCI almost
 eliminated the source instability of both analytes. Negative ion ESI
 was, therefore, chosen for the development of an LC-MS/MS method for
 simultaneous determination of these analytes. After protein
 precipitation by acetonitrile, all analytes were separated on a Luna
 C18 HST column (50 x 2.0 mm id., 2.5 mu m) with a mobile phase of 20
 mmol L-1 ammonium acetate water solution containing 0.2% acetic
 acid :acetonitrile (18:82, v/v). The detection was performed on a
 tandem mass spectrometer using selective reaction monitoring mode.
 Calibration curves were linear over the range of 10-6000 ng mL(-1) for
 GA and 3-2000 ng mL(-1) for 10-OHGA. The method was successfully applied
 to the pharmacokinetics study of GA injection in six beagle dogs.
 SN 1469-0667
 PY 2010
 VL 16
 IS 5
 BP 605
 EP 617
 DI 10.1255/ejms.1095
 UT ISI:000282257200006
 PT J
 AU Liu, J
 He, T
 Lu, QA
 Shang, J
 Sun, HB
 Zhang, LY
 AF Liu, Jun
 He, Ting
 Lu, Qian
 Shang, Jing
 Sun, Hongbin
 Zhang, Luyong
 TI Asiatic acid preserves beta cell mass and mitigates hyperglycemia in
 streptozocin-induced diabetic rats
 SO DIABETES-METABOLISM RESEARCH AND REVIEWS
 AB Background Type 1 diabetes is a chronic condition in which the pancreas
 produces little or no insulin due to the loss or dysfunction of
 pancreatic beta cells. This study investigated the beneficial effects
 of asiatic acid - a triterpenoid compound - preserved beta mass and
 mitigated hyperglycemia in streptozocin-induced diabetic rats.
 Methods Diabetes mellitus was induced in adult male Wistar rats by a
 single intraperitoneal injection of streptozocin (60 mg/kg body
 weight). The diabetic rats were divided into untreated and asiatic acid
 (25 mg/kg) groups. Controls were intraperitoneal injection with
 citrate buffer. Blood glucose level, plasma insulin, and pancreas
 immunohistochemistry analysis were examined after a 2-week
 experimental period. AKT and Bcl-xL expression in the pancreatic islets
 of rats were evaluated by Western blot methods.
 Results Blood glucose levels were significantly reduced in rats
 receiving asiatic acid after streptozocin administration. Asiatic acid
 concomitantly increased serum insulin levels in diabetic rats.
 Immunohistochemical staining revealed a marked preservation by asiatic
 acid of insulin-producing beta cells in the pancreatic islets of the
 diabetic rats. Furthermore, asiatic acid in vivo induced pro-survival
 Akt kinase activation and Bcl-xL expression in the pancreatic islets
 of diabetic rats.
 Conclusions These results suggest that asiatic acid exerts its
 glucose-lowering effects, in part through influences on beta-cell
 mass. Asiatic acid administration resulted in preservation and
 restoration of beta-cell mass and function in diabetic rodent models.
 Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 1520-7552
 PD SEP
 PY 2010
 VL 26
 IS 6
 BP 448
 EP 454
 DI 10.1002/dmrr.1101
 UT ISI:000282202400003
 PT J
 AU Liu, WY
 Yang, XJ
 Feng, F
 Wu, CY
 Ding, L
 AF Liu, Wenyuan
 Yang, Xiaojing
 Feng, Feng
 Wu, Chunyong
 Ding, Li
 TI SPE and LC for Analysis of the Tissue Distribution of Wogonin and Its
 Metabolite in Tumor-Bearing Nude Mice
 SO CHROMATOGRAPHIA
 AB The tissue distribution of wogonin was investigated for study of its
 anticancer activity. A robust, reliable, and sensitive LC method was
 developed for simultaneous analysis of wogonin and its major
 metabolite, wogonoside, in tissues of tumor-bearing nude mice. To reach
 the required level of detection in different tissues, sample
 pretreatment was by solid-phase extraction. Good LC separation was
 achieved on a C-18 column with methanol-0.5% formic acid 68:32 (v/v)
 as mobile phase. UV detection was performed at 275 nm and calibration
 plots for both analytes were linear over the range 0.16-80.0 mu g g(-1)
 for all the biological samples studied with correlation coefficients >
 0.9980. Inter-day and intra-day precision were no more than 15% at the
 limit of quantification and 10% at other concentrations; recovery from
 all tissues was 92.3-101.4% for wogonin and 66.7-74.3% for wogonoside.
 The method was ideal for this tissue distribution study and results
 obtained reflect the potential of wogonin for further pharmaceutical
 development as an anticancer agent.
 SN 0009-5893
 PD OCT
 PY 2010
 VL 72
 IS 7-8
 BP 753
 EP 757
 DI 10.1365/s10337-010-1714-7
 UT ISI:000282211200027
 PT J
 AU Wang, XJ
 Gu, K
 Xu, JS
 Li, MH
 Cao, RY
 Wu, J
 Li, TM
 Liu, JJ
 AF Wang, Xue Jun
 Gu, Kai
 Xu, Jin Shu
 Li, Ming Hui
 Cao, Rong Yue
 Wu, Jie
 Li, Tai Ming
 Liu, Jing Jing
 TI Immunization with a recombinant GnRH vaccine fused to heat shock
 protein 65 inhibits mammary tumor growth in vivo
 SO CANCER IMMUNOLOGY IMMUNOTHERAPY
 AB Gonadotrophin-releasing hormone (GnRH) is the prime decapeptide
 hormone in the regulation of mammalian reproduction. Active
 immunization against GnRH has been a good treatment option to fight
 against hormone-dependent disease such as breast cancer. We designed
 and purified a novel protein vaccine Hsp65-GnRH(6) containing heat
 shock protein 65 (Hsp65) and six copies of GnRH in linear alignment.
 Immunization with Hsp65-GnRH(6) evoked strong humoral response in
 female mice. The generation of specific anti-GnRH antibodies was
 detected by ELISA and verified by western blot. In addition, anti-GnRH
 antibodies effectively neutralized endogenous GnRH activity in vivo,
 as demonstrated by the degeneration of the ovaries and uteri in the
 vaccinated mice. Moreover, the growth of EMT-6 mammary tumor allografts
 was inhibited by anti-GnRH antibodies. Histological examinations have
 shown that there was increased focal necrosis in tumors. Taken
 together, our results showed that immunization with Hsp65-GnRH(6)
 elicited high titer of specific anti-GnRH antibodies and further led
 to atrophy of reproductive organs. The specific antibodies could
 inhibit the growth of EMT-6 murine mammary tumor probably via an
 indirect mechanism that includes the depletion of estrogen. In view
 of these results, the protein vaccine Hsp65-GnRH(6) appears to be a
 promising candidate vaccine for hormone-dependent cancer therapy.
 SN 0340-7004
 PD DEC
 PY 2010
 VL 59
 IS 12
 BP 1859
 EP 1866
 DI 10.1007/s00262-010-0911-4
 UT ISI:000282184700010
 PT J
 AU Wang, Y
 Lin, GW
 Hong, J
 Li, L
 Yang, YM
 Lu, T
 AF Wang, Yue
 Lin, Guo-Wu
 Hong, Jin
 Li, Li
 Yang, Yu-Mei
 Lu, Tao
 TI Synthesis, structure, DNA binding and cleavage ability of a new copper
 ciprofloxacin complex
 SO JOURNAL OF COORDINATION CHEMISTRY
 AB The structure of 1 consists of [Cu(HCp)(phen)(H2O)]2+ (HCp is
 ciprofloxacin and phen is 1,10-phenanthroline), two acetates, and four
 free water molecules. In each cation, copper displays a distorted
 square pyramid, coordinated to ring 3-carboxylate and 4-oxo oxygen from
 HCp, two nitrogens from phen, and one water molecule. There are five
 water molecules in each discrete complex with one coordinated to Cu
 center, and the other four linked to each other by intermolecular
 hydrogen bonds. Two uncoordinated acetates make the compound neutral.
 The complex exhibits higher DNA binding compared to HCp at the same
 conditions by fluorescence and viscosity measurements. Combining its
 structure with the DNA-binding result, the binding mechanism may be
 explained by intercalation. Moreover, 1 shows significant cleavage of
 DNA in the presence of a reducing agent, such as ascorbate by gel
 electrophoresis using supercoiled pBR322 DNA in Tris-HCl buffer (pH
 7.4). The complex also has a higher activity against Gram-positive
 bacteria Staphylococcus aureus and Gram-negative bacteria Klebsiella
 pneumoniae than HCp.
 SN 0095-8972
 PY 2010
 VL 63
 IS 20
 BP 3662
 EP 3675
 DI 10.1080/00958972.2010.515986
 UT ISI:000282028300014
 PT J
 AU Li, ZY
 Wang, YY
 Tang, CH
 Xu, JY
 Wu, XM
 Yao, HQ
 AF Li Ziyuan
 Wang Yiyun
 Tang Changhua
 Xu Jinyi
 Wu Xiaoming
 Yao Hequan
 TI Synthesis of 3-Benzoyl Acrylates/Acrylamides via Dehydrogenation of
 3-Benzoyl Propionates/Propionamides Using IBX/p-TsOH
 SO CHINESE JOURNAL OF CHEMISTRY
 AB Dehydrogenation by IBX/p-TsOH is applied to the conversion of 3-benzoyl
 propionates/propionamides to 3-benzoyl acrylates/acrylamides in
 moderate to excellent yields. The reaction time for the dehydrogenation
 of 3-benzoyl propionamides was remarkably shorter than that for the
 dehydrogenation of esters.
 SN 1001-604X
 PD JUL
 PY 2010
 VL 28
 IS 7
 BP 1301
 EP 1305
 DI 10.1002/cjoc.201090225
 UT ISI:000282083700040
 PT J
 AU Liu, LS
 Aa, JY
 Wang, GJ
 Yan, B
 Zhang, Y
 Wang, XW
 Zhao, CY
 Cao, B
 Shi, JA
 Li, MJ
 Zheng, TA
 Zheng, YT
 Hao, G
 Zhou, F
 Sun, JG
 Wu, ZM
 AF Liu, Linsheng
 Aa, Jiye
 Wang, Guangji
 Yan, Bei
 Zhang, Ying
 Wang, Xinwen
 Zhao, Chunyan
 Cao, Bei
 Shi, Jian
 Li, Mengjie
 Zheng, Tian
 Zheng, Yuanting
 Hao, Gang
 Zhou, Fang
 Sun, Jianguo
 Wu, Zimei
 TI Differences in metabolite profile between blood plasma and serum
 SO ANALYTICAL BIOCHEMISTRY
 AB In metabolomic research, blood plasma and serum have been considered
 to possess similar compositions and properties. Their perceived
 equivalence has resulted in researchers choosing arbitrarily between
 serum and plasma for analysis. Here, routine serum and plasma were
 prepared and their low-molecular-weight compounds were determined
 using gas chromatography/time-of-flight mass spectrometry. Principal
 components analysis was applied to process the acquired data, and
 marked differences in metabolite profiles were observed between serum
 and plasma. Of the 72 identified compounds, 36 (50%) discriminate serum
 from plasma, with 29 and 7 metabolites showing a significantly higher
 abundance (t test, P < 0.05) in serum and plasma, respectively.
 Incubation of blood had distinct effects on the analyte peak areas,
 with the effects being more pronounced for plasma than for serum and
 more pronounced for a shorter incubation than for a longer incubation.
 These results highlight the importance in choosing serum or plasma as
 the analytical sample and in stipulating the incubation time. Because
 incubation affected the analyte peak areas less in serum than in plasma,
 we recommend serum as the sample of choice in metabolomic studies. (C)
 2010 Elsevier Inc. All rights reserved.
 SN 0003-2697
 PD NOV 15
 PY 2010
 VL 406
 IS 2
 BP 105
 EP 112
 DI 10.1016/j.ab.2010.07.015
 UT ISI:000281925300002
 PT J
 AU Xie, WJ
 Tanabe, G
 Morimoto, H
 Hatanaka, T
 Minematsu, T
 Wu, XM
 Muraoka, O
 AF Xie, Weijia
 Tanabe, Genzoh
 Morimoto, Hiroyuki
 Hatanaka, Takanori
 Minematsu, Toshie
 Wu, Xiaoming
 Muraoka, Osamu
 TI Another mode of heterocyclization of an enantiopure C-2-symmetric
 bis-epoxide leading to the symmetric dialkyl sulfide
 SO TETRAHEDRON
 AB Reexamination of heterocyclization of an enantiopure C-2-symmetric
 bis-epoxide (7) with sodium sulfide is described. In addition to the
 reported processes leading to thiane (4a) and thiepane (6), another
 mode of cyclization was found to occur to a considerable extent,
 affording a symmetric dialkyl sulfide (5), and the structure of the
 main product reported (4a) has been revised. Conditions for the
 chemoselective formation of 6 were established, and effective
 transformation of 6 into 4 was accomplished by the modification of the
 processes. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0040-4020
 PD SEP 18
 PY 2010
 VL 66
 IS 38
 BP 7487
 EP 7491
 DI 10.1016/j.tet.2010.07.064
 UT ISI:000281836300005
 PT J
 AU Tian, HY
 Wang, L
 Zhang, XQ
 Zhang, DM
 Wang, Y
 Liu, JS
 Jiang, RW
 Ye, WC
 AF Tian, Hai-Yan
 Wang, Lei
 Zhang, Xiao-Qi
 Zhang, Dong-Mei
 Wang, Ying
 Liu, Jun-Shan
 Jiang, Ren-Wang
 Ye, Wen-Cai
 TI New bufadienolides and C-23 steroids from the venom of Bufo bufo
 gargarizans
 SO STEROIDS
 AB Six new bufadienolides (1-6) and two new C-23 steroids (7 and 8),
 together with three known compounds (9-11) were isolated from the venom
 of Bufo bufo gargarizans. Their structures were elucidated by
 spectroscopic analysis and single-crystal X-ray diffraction. In vitro
 cytotoxicities of all compounds were evaluated in A549 cancer cell
 line. Compounds 2, 3 and 10 showed significant cytotoxic activities.
 (C) 2010 Elsevier Inc. All rights reserved.
 SN 0039-128X
 PD DEC
 PY 2010
 VL 75
 IS 12
 BP 884
 EP 890
 DI 10.1016/j.steroids.2010.05.013
 UT ISI:000281932500012
 PT J
 AU Zheng, YF
 Qi, LW
 Cui, XB
 Peng, GP
 Peng, YB
 Ren, MT
 Cheng, XL
 Li, P
 AF Zheng, Yun-Feng
 Qi, Lian-Wen
 Cui, Xiao-Bing
 Peng, Guo-Ping
 Peng, Yong-Bo
 Ren, Mei-Ting
 Cheng, Xiao-Lan
 Li, Ping
 TI Oleanane-type Triterpene Glucuronides from the Roots of Glycyrrhiza
 uralensis Fischer
 SO PLANTA MEDICA
 AB Investigation of characteristic constituents of the roots of
 Glycyrrhiza uralensis Fischer led to isolation of four new triterpene
 glucuronides, namely uralsaponins C-F (1-4), an artificial product,
 namely the methyl ester of glycyrrhizin (5), as well as six known
 triterpene glucuronides (611). These new compounds were identified by
 1D and 2D NMR spectroscopic analysis. The cytotoxicity of the selected
 compounds and their aglycones were evaluated against HeLa and MCF-7
 cancer cell lines, and the preliminary structure-activity relationship
 was also elucidated.
 SN 0032-0943
 PD SEP
 PY 2010
 VL 76
 IS 13
 BP 1457
 EP 1463
 DI 10.1055/s-0029-1240907
 UT ISI:000281742700012
 PT J
 AU Wang, F
 Zhou, L
 Zhou, JH
 Gu, XT
 Feng, YY
 AF Wang, Fang
 Zhou, Lin
 Zhou, Jiahong
 Gu, Xiaotian
 Feng, Yuying
 TI Characterization of anticancer hypocrellin A encapsulated with silica
 nanoparticles
 SO JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY
 AB Hypocrellins, natural photosensitizers including hypocrellin A (HA)
 and hypocrellin B (HB), have been used as a traditional Chinese herbal
 medicine to cure various skin diseases. Hypocrellins have excellent
 antiviral activity, which can inhibit the growth of human
 immunodeficiency virus. They also exhibit significant light-induced
 antitumor property. In this article, thermal analysis technologies
 (e.g., differential scanning calorimetry and thermogravimetry) are
 employed to characterize whether the photosensitive hypocrellin A
 could be encapsulated with silica nanoparticle (SN) material or not,
 and evaluate the stability of inclusion complex. The results show that
 the inclusion complex exhibits improved performance in both stability
 and hydrophilicity than natural hypocrellin A. Fluorescence
 spectrophotometry studies have also been performed to verify the
 thermal analysis results. The results suggest that the thermal analysis
 technology could be used as an effective and rapid tool to characterize
 the encapsulation properties of the novel anticancer HA-SN complex.
 SN 1388-6150
 PD OCT
 PY 2010
 VL 102
 IS 1
 BP 69
 EP 74
 DI 10.1007/s10973-009-0630-2
 UT ISI:000281705500012
 A Chen, GH
 U Wang, L
 Yao, XM
 Zhang, ML
 Wu, FH
 A Chen Guohua
 F Wang Li
 Yao Xiumei
 Zhang Mingliang
 Wu Feihua
 T Synthesis and Biological Activity of Dihydropyridine Calcium
 I Antagonists
 CHINESE JOURNAL OF ORGANIC CHEMISTRY
 A Sixteen new dihydropyridine calcium antagonists 4a similar to 4l and
 B 9a similar to 9d were designed and synthesized based on
 5-(methoxycarbonyl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyri
 dine-3 -carboxylic acid (1) or diketene. The structures of the target
 compounds were confirmed by IR,H-1 NMR, ESI-MS techniques and elemental
 analysis. The results of preliminary pharmacological test showed that
 compounds 4e, 4g, 4h, 4i and 4j had obvious relaxation effect on the
 contraction of vascular ring of aorta induced by KCI, which were better
 than positive control (levoamlodipine besylate).
 0253-2786
 2010
 1004
 ISI:000281722600007
 PT J
 AU Liu, XH
 Liu, HF
 Chen, J
 Yang, Y
 Song, BA
 Bai, LS
 Liu, JX
 Zhu, HL
 Qi, XB
 AF Liu, Xin-Hua
 Liu, Hui-Feng
 Chen, Jin
 Yang, Yang
 Song, Bao-An
 Bai, Lin-Shan
 Liu, Jing-Xin
 Zhu, Hai-Liang
 Qi, Xing-Bao
 TI Synthesis and molecular docking study of novel coumarin derivatives
 containing 4,5-dihydropyrazole moiety as potential antitumor agents
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB A series of novel coumarin derivatives containing 4,5-dihydropyrazole
 moiety as potential telomerase inhibitors were synthesized. The
 bioassay tests show that compound 3d exhibited potentially high
 activity against human gastric cancer cell SGC-7901 with IC50 value
 of 2.69 +/- 0.60 mu g/mL. All title compounds were assayed for
 telomerase inhibition by a modified TRAP assay, the results show that
 compounds 3d and 3f can strongly inhibit telomerase with IC50 values
 of 2.0 +/- 0.07 and 1.8 +/- 0.35 mu M, respectively. Docking simulation
 was performed to position compound 3d into the telomerase (3DU6) active
 site to determine the probable binding model. (C) 2010 Elsevier Ltd.
 All rights reserved.
 SN 0960-894X
 PD OCT 1
 PY 2010
 VL 20
 IS 19
 BP 5705
 EP 5708
 DI 10.1016/j.bmcl.2010.08.017
 UT ISI:000281735600022
 PT J
 AU Xiong, Y
 Yang, YQ
 Yang, J
 Chai, HY
 Li, Y
 Yang, J
 Jia, ZM
 Wang, ZR
 AF Xiong, Yu
 Yang, Yuqing
 Yang, Jin
 Chai, Hongyan
 Li, Ying
 Yang, Jing
 Jia, Ziming
 Wang, Zhengrong
 TI Tectoridin, an isoflavone glycoside from the flower of Pueraria lobata,
 prevents acute ethanol-induced liver steatosis in mice
 SO TOXICOLOGY
 AB In traditional Chinese medicine, the flower of Pueraria lobata
 (Puerariae Flos) has been used in therapy to counteract the problems
 associated with alcohol drinking and liver injury. In this study, we
 investigated the hepatoprotective effects and its mechanisms of
 tectoridin, an isoflavone glycoside from the flower of P. lobata
 (Willd.) Ohwi. Ethanol (5 g/kg) was given orally every 12 h for a total
 of three doses. 1 h after the last dose of ethanol, tectoridin (25,
 50 and 100 mg/kg) was given intragastrically five times in three
 consecutive days. The mice were sacrificed at 4 h after tectoridin
 treatment. Peroxisome proliferators-activated receptor alpha (PPAR
 alpha), sterol regulatory element-binding protein (SREBP)-1c and their
 target genes were evaluated by biochemical analysis and quantitative
 real-time polymerase chain reaction (qPCR). Mitochondria were isolated
 for the mitochondrial permeability transition (MPT) and membrane
 potential (Delta Psi(m)) assay. Acute ethanol exposure resulted in the
 significant increase of the alanine aminotransferase (ALT), aspartate
 aminotransferase (AST) and triglyceride (TG) levels and hepatic
 mitochondria dysfunction shown as the increase of MPT and the decrease
 of Delta Psi(m). However, tectoridin treatment dramatically attenuated
 these effects. In addition, tectoridin remarkably alleviated the
 over-production of thiobarbituric acid-reactive substance.
 Furthermore, tectoridin inhibited the decrease of PPAR alpha
 expression and its target genes, including medium-chain acyl-CoA
 dehydrogenase (MCAD), acyl-CoA oxidase (ACO) and cytochrome P450 4A
 (CYP 4A) at mRNA and enzyme activity levels. These data showed that
 tectoridin protected against ethanol-induced liver steatosis mainly
 through modulating the disturbance of PPAR alpha pathway and
 ameliorating mitochondrial function. (C) 2010 Elsevier Ireland Ltd.
 All rights reserved.
 SN 0300-483X
 PD SEP 30
 PY 2010
 VL 276
 IS 1
 BP 64
 EP 72
 DI 10.1016/j.tox.2010.07.007
 UT ISI:000281624800010
 PT J
 AU Zhu, BL
 Xu, HM
 Zhao, LM
 Huang, XF
 Zhang, FG
 AF Zhu, Beili
 Xu, Han-Mei
 Zhao, Liming
 Huang, Xiaofeng
 Zhang, Fengguo
 TI Site-specific modification of anti-angiogenesis peptide HM-3 by
 polyethylene glycol molecular weight of 20 kDa
 SO JOURNAL OF BIOCHEMISTRY
 AB HM-3, an RGD modified endostatin-derived polypeptide, is a potent
 angiogenesis inhibitor synthesized in our laboratory. Its robust
 inhibitory effects on endothelial cell migration and tumour growth have
 been demonstrated by in vivo and in vitro activity assays. However,
 the drug has relatively short half-life in vivo. For the purpose of
 prolonging HM-3 half-life and retaining the safety and efficacy of the
 peptide, the study chose methoxy-polyethylene glycol-Succinimidyl
 Carbonate (SC-mPEG, molecular weight 20 kDa, named SC-mPEG(20k)) to
 specifically modify its N terminus. Compared with HM-3, the
 site-specific mono-PEGylated peptide PEG(20k)-HM-3 was shown the same
 activity in the inhibition of B16F10 tumour in vivo (the inhibitory
 effect of PEG(20k)-HM-3, HM-3 and Taxol were 44.35, 39.68%,
 respectively), while the frequency of drug-administering reduced from
 twice a day to once every 3 days. Its rate of in vitro degradation in
 serum was markedly reduced (72.78% could still be detected after 132
 h). Histochemistry and immunohistochemistry analysis showed that both
 HM-3 and PEG(20k)-HM-3 induced large areas of continuous necrosis
 within tumours and significantly reduced the vessel density compared
 to control. It might be a breakthrough in PEG modification field to
 modify a small peptide with a large PEG and reach a good result.
 SN 0021-924X
 PD SEP
 PY 2010
 VL 148
 IS 3
 BP 341
 EP 347
 DI 10.1093/jb/mvq070
 UT ISI:000281534100010
 PT J
 AU Chen, DQ
 Jiang, XQ
 Huang, YY
 Zhang, C
 Ping, QN
 AF Chen, Daquan
 Jiang, Xiaoqun
 Huang, Yanyu
 Zhang, Can
 Ping, Qineng
 TI pH-Sensitive mPEG-Hz-Cholesterol Conjugates as a Liposome Delivery
 System
 SO JOURNAL OF BIOACTIVE AND COMPATIBLE POLYMERS
 AB Hydrazone (Hz)-based pH-sensitive methoxy(polyethylene glycol)cholesterol conjugates (mPEG-Hz-Chol), were synthesized and used to
 fabricate liposomes. The structures of the mPEG2000-Hz-Chol conjugate
 were confirmed by FT-IR and H-1-NMR; they were stable at pH 7.4 but
 sensitive to mild acid conditions (pH 5.5). Plain liposomes were also
 prepared with S100PC/Chol, and the pH-insensitive liposomes with
 S100PC/Chol/mPEG2000-Chol for comparison; all the liposomes were
 similar in diameter similar to 20 0 nm. In vitro, the pH-sensitive
 liposomes released more of the model drug, paclitaxel (PTX), than the
 plain liposomes. The pH-sensitive liposomes were less toxic than the
 plain liposomes and exhibited higher cellular uptake of PTX compared
 with pH-insensitive liposomes by human breast cancer cells (MCF-7).
 The pH-sensitive mPEG2000-Hz-Chol liposomes are now being investigated
 as a potential new liposome drug delivery system.
 SN 0883-9115
 PD SEP
 PY 2010
 VL 25
 IS 5
 BP 527
 EP 542
 DI 10.1177/0883911510379996
 UT ISI:000281598800007
 PT J
 AU Liu, XP
 Du, YX
 AF Liu, Xiangping
 Du, Yingxiang
 TI Study on the binding of chiral drug duloxetine hydrochloride to human
 serum albumin
 SO EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 AB Duloxetine holds a special promise as an antidepressant, and its effect
 depends on its binding to human serum albumin (HSA). For this reason,
 the binding mechanism of duloxetine with HSA was investigated. The
 specific binding site in HSA was identified and binding constants were
 determined. Duloxetine could compete with dansyl-L-proline (DLP), a
 site II marker for binding to site II. Binding constants between
 duloxetine and HSA were 1.75 x 10(3) L mol(-1) and 3.74 x 10(3) L mol(-1)
 at pH 7.4 and pH 8.5, respectively. The interaction process of
 enantiomers and HSA was susceptible to pH change. It was concluded that
 specific binding position of duloxetine was located in site II, and
 the B conformation of HSA possibly excelled the N conformation in
 identifying and binding to enantiomers. (C) 2010 Elsevier Masson SAS.
 All rights reserved.
 SN 0223-5234
 PD SEP
 PY 2010
 VL 45
 IS 9
 BP 4043
 EP 4049
 DI 10.1016/j.ejmech.2010.05.063
 UT ISI:000281568600064
 PT J
 AU Wang, JX
 Ma, JH
 You, QD
 Zhao, L
 Wang, F
 Li, C
 Guo, QL
 AF Wang, Jinxin
 Ma, Junhai
 You, Qidong
 Zhao, Li
 Wang, Fan
 Li, Chong
 Guo, Qinglong
 TI Studies on chemical modification and biology of a natural product,
 gambogic acid (II): Synthesis and bioevaluation of gambogellic acid
 and its derivatives from gambogic acid as antitumor agents
 SO EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 AB Gambogic acid (GA) has been reported to be a potent apoptosis inducer.
 The fact that it is amenable to chemical modification makes GA an
 attractive molecule for the development of anticancer agents. We
 firstly reported the synthesis of gambogellic acid, which was generated
 under acid catalysis from readily available GA by a base-catalyzed
 diene intramolecular annelation. Sequentially, thirteen new compounds
 were synthesized and their inhibitory activity on HT-29, Bel-7402,
 BGC-823, and A549 cell lines were evaluated in vitro by MTT assay, and
 (38, 40)-epoxy-33-chlorogambogellic acid (4) was identified as a
 BGC-823 cell apoptosis inducer through MTT cell assay, observations
 of morphological changes, and Annexin-V/PI double-staining assay.
 Compound 4 showed significant effects in inducing apoptosis and might
 serve as a potential lead compound for discovery of new anticancer
 drugs. Further structure activity relationships (SARs) of gambogic
 acid derivatives were discussed. (C) 2010 Elsevier Masson SAS. All
 rights reserved.
 SN 0223-5234
 PD SEP
 PY 2010
 VL 45
 IS 9
 BP 4343
 EP 4353
 DI 10.1016/j.ejmech.2010.04.037
 UT ISI:000281568600101
 PT J
 AU He, LQ
 Gu, HX
 Yin, DK
 Zhang, YH
 Wang, XS
 AF He Li-Qin
 Gu Hong-Xia
 Yin Deng-Ke
 Zhang Yi-Hua
 Wang Xiao-Shan
 TI Synthesis and Anti-cancer Activity of Nitric Oxide Donor-based Matrine
 Derivatives
 SO CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 AB Matrine, one of the major active alkaloids isolated from the Sophora
 alopecuroides L which is a useful Chinese herbal drug, possesses
 antipyretic, anti-inflammatory, analgesic, and notable antiviral
 activities, and has been used for the treatment of
 lipopolysaccharide-induced liver injury. Recently, it was reported
 that matrine could inhibit the growth of tumor cells. Nitric oxide(NO),
 a free radical molecule, is involved in numerous physiological and
 pathological processes. High levels of NO usually are toxic to tumor
 cells. It was therefore of interest to determine whether the hybrid
 of matrine and NO donor furoxan would provide a hitherto unknown class
 of matrine derivatives that possess potent anticancer activity. Herein
 furoxan-based matrine compounds 11a-11m were designed and synthesized,
 and their structures were confirmed by MS, IR, H-1 NMR spectra and
 elemental analysis. All target compounds exhibited expectedly much
 more stronger anti human hepatocellular carcinoma cells(HepG2 cells)
 activity than that of parent compound matrine in vivo. Furthermore,
 compounds 11a-11c, 11h and 11i had stronger cytotoxic activities than
 that of control 5-flu-orouracil. The concept of designing NO
 donor-based matrine derivatives that possess potent anticancer
 activity warrants further investigation.
 SN 0251-0790
 PD AUG 10
 PY 2010
 VL 31
 IS 8
 BP 1541
 EP 1547
 UT ISI:000281590200012
 PT J
 AU Xiu, AH
 Kong, Y
 Zhou, MY
 Zhu, B
 Wang, SM
 Zhang, JF
 AF Xiu, Aihui
 Kong, Yi
 Zhou, Mengyi
 Zhu, Bin
 Wang, Shiming
 Zhang, Jianfa
 TI The chemical and digestive properties of a soluble glucan from
 Agrobacterium sp ZX09
 SO CARBOHYDRATE POLYMERS
 AB A salt-tolerant strain Agrobacteriurn sp. ZX09 produced a high
 molecular mass, water-soluble extracellular polysaccharide (EPS)
 composed of D-glucose. By examining periodate oxidation, H-1 NMR and
 C-13 NMR spectra, it was proven that the EPS consisted of the following
 repeating unit: -> 3)-beta-D-Glcp-(1 -> 3)-[beta-D-Glcp-(1 ->
 3)-beta-D-Glcp-(1 -> 3)]3-alpha-D-Glcp-(1 -> 3)-alpha-D-Glcp-(1 -> .
 In vitro the EPS was indigestible by alpha-amylase, and strongly
 inhibited pancreatic alpha-amylase activity. Fasting mice fed on the
 EPS failed to increase blood glucose levels. Experimental diets
 containing the EPS suppressed steep increase in blood glucose
 concentration. These results suggest that the novel water-soluble
 glucan could be potentially useful for decreasing absorption of dietary
 carbohydrate and postprandial blood glucose level. (C) 2010 Elsevier
 Ltd. All rights reserved.
 SN 0144-8617
 PD OCT 15
 PY 2010
 VL 82
 IS 3
 BP 623
 EP 628
 DI 10.1016/j.carbpol.2010.05.027
 UT ISI:000281524900014
 PT J
 AU Dai, J
 Wu, Y
 Chen, SW
 Zhu, S
 Yin, HP
 Wang, M
 Tang, JA
 AF Dai, Jun
 Wu, Yan
 Chen, Shang-wei
 Zhu, Song
 Yin, Hong-ping
 Wang, Min
 Tang, Jian
 TI Sugar compositional determination of polysaccharides from Dunaliella
 salina by modified RP-HPLC method of precolumn derivatization with
 1-phenyl-3-methyl-5-pyrazolone
 SO CARBOHYDRATE POLYMERS
 AB A modified high-performance liquid chromatography method of pre-column
 derivatization with 1-phenyl-3-methyl-5-pyrazolone (PMP) has been
 established for high resolution separation and high sensitivity
 determination of ten monosaccharides simultaneously, which frequently
 occur in algae polysaccharides. The effects of volume proportion of
 acetonitrile and pH value of mobile phase (0.1 M phosphate buffer
 acetonitrile) on retention and separation of the monosaccharide
 derivatives were investigated with Eclipse XPB-C18 column screened
 out. The hydrolyzation condition of polysaccharides and derivatization
 procedure of hydrolysates were also optimized. The modified analysis
 method was used for the determination of monosaccharide compositions
 in five polysaccharide fractions isolated from Duanaliella salina. The
 results showed that PD1 and PD4a were acidic heteropolysaccharide
 mainly containing glucose and galactose respectively, and PD4a
 contained sulfated groups; PD2 and PD3 all were a glucan; while PD4b
 was a complex of polysaccharide linked with nucleic acids by covalent
 bonds. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0144-8617
 PD OCT 15
 PY 2010
 VL 82
 IS 3
 BP 629
 EP 635
 DI 10.1016/j.carbpol.2010.05.029
 UT ISI:000281524900015
 PT J
 AU Wu, JF
 Xiang, BR
 Li, KX
 AF Wu, Jing-Fang
 Xiang, Bing-Ren
 Li, Kui-Xing
 TI Bioequivalence evaluation of menthol after oral administration of
 peppermint oil soft capsules in dogs
 SO ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
 AB A randomized, two-way, crossover, bio-equivalence study in 6 beagle
 dogs was conducted to compare the bioavailability of two peppermint
 oil formulations, soft capsule and hard capsule. The drug was given
 in a single dose of two capsules (total, 200 mg), and blood samples
 were withdrawn during the 12 h after drug administration. Menthol (CAS
 2216-51-5) as the main component of peppermint oil was determined by
 a gas chromatography-tandem mass spectrometry (GC-MS/MS) method after
 cleavage with beta-glocuronidase. The following pharmacokinetic
 variables were computed for the two formulations: maximum
 concentration (C-max), time to maximum concentration (T-max),
 half-life of elimination (t(1/2)), mean residence time (MRT), and areas
 under the plasma concentration-time curve (AUC(0-t), and
 AUC(0-infinity)). For calculation of the 90% confidence interval (CI),
 an analysis of variance (ANOVA) was carried out.
 The results indicated that treatment and subject had statistically
 significant effect on AUC(0-t), AUC(0-infinity) and C-max, and the 90%
 CIs for AUC(0-t), AUC(0-infinity) and C-max were outside the acceptable
 bioequivalence range. The relative bioavailability was 121.4 +/- 10.6%
 for AUC(0-infinity) Therefore, it can be concluded that the two
 formulations are not bioequivalent and the bioavailability of soft
 capsules is significantly higher than that of hard capsules.
 SN 0004-4172
 PY 2010
 VL 60
 IS 8
 BP 479
 EP 482
 UT ISI:000281581900002
 PT J
 AU Wang, XS
 Liao, JM
 Yin, DK
 Zhan, F
 Dai, SF
 Xie, GY
 Sang, XB
 AF Wang, Xingsheng
 Liao, Jianmin
 Yin, Dengke
 Zhan, Fan
 Dai, Sufei
 Xie, Guangyan
 Sang, Xiaobing
 TI Establishment of a Novel Model for Studying the Effects of Extracts
 of Chinese Herb Medicine on Human Type II 5 alpha-Reductase in Vitro
 SO YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN
 AB Human steroid 5 alpha-reductase type II (hSRD5A2) and
 dihydrotestosterone (DHT) play important roles in benign prostatic
 hyperplasia (BPH). The aim of our study was to establish a novel model
 to investigate the inhibitory effects of extracts and compounds of
 Chinese herb medicine on hSRD5A2. The gene, hSRD5A2, was artificially
 synthesized and cloned into pcDNA3.1 (+) vector, which was transfected
 into CHO cells by liposome. Transfected cells were screened through
 G418 and MTX. The expressed protein of hSRD5A2 by cells was purified
 and detected by western blotting. A minim reactive system comprising
 hSRD5A2 and testosterone (T) as substrate together with NADPH as
 hydrogen donor was established for screening inhibitors of hSRD5A2.
 The reaction system was optimized in the concentrations of T, NADPH,
 and hSRD5A2 and reaction temperature, time, and activity of hSRD5A2
 were determined by the production of DHT. Furthermore, we screened some
 extracts and compounds of Chinese herb medicine using this model. The
 concentrations of T, NADPH, and hSRD5A2 were 0.02 mu M, 0.8 mM, and
 0.05 U/mu l, respectively, in the model; maximum activity of hSRD5A2
 was achieved at 37 degrees C and 60 min reaction, and mangiferin had
 significant inhibitory effect on the activity of hSRD5A2. The model
 in this study is convenient and reliable for screening and evaluation
 of inhibitors of hSRD5A2; mangiferin may be a potential medicine for
 the treatment of BPH.
 SN 0031-6903
 PD SEP
 PY 2010
 VL 130
 IS 9
 BP 1207
 EP 1214
 UT ISI:000281433800012
 PT J
 AU Hong, JL
 Qin, XY
 Shu, P
 Wu, G
 Wang, QA
 Qin, MJ
 AF Hong, Jun-Li
 Qin, Xiao-Ying
 Shu, Pan
 Wu, Gang
 Wang, Qiang
 Qin, Min-Jian
 TI Analysis of catalpol derivatives by characteristic neutral losses
 using liquid chromatography combined with electrospray ionization
 multistage and time-of-flight mass spectrometry
 SO RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 SN 0951-4198
 PD SEP
 PY 2010
 VL 24
 IS 17
 BP 2680
 EP 2686
 DI 10.1002/rcm.4676
 UT ISI:000281355000026
 PT J
 AU Ma, C
 Gao, MM
 Liu, WC
 Zhu, J
 Tian, H
 Gao, XD
 Yao, WB
 AF Ma, Chen
 Gao, Mingming
 Liu, Wenchao
 Zhu, Jing
 Tian, Hong
 Gao, Xiangdong
 Yao, Wenbing
 TI Intein-Mediated Expression and Purification of an Analog of
 Glucagon-like Peptide-1 in Escherichia coli
 SO PROTEIN AND PEPTIDE LETTERS
 AB To facilitate expression and purification of an analog of GLP-1
 (mGLP-1), an intein system was employed in this study. A recombinant
 fusion protein, CBD-DnaB-mGLP-1, was constructed and expressed in the
 form of inclusion body. After refolding, the intein-mediated
 self-cleavage was triggered by pH and temperature shift. By using
 chitin beads column followed by single step purification, about 2.58
 mg of mGLP-1 with the purity of up to 98% could be obtained from 1 L
 medium. Tricine-SDS-PAGE, RP-HPLC, and ESI-MS were undertaken to
 determine the purity and molecular weight of mGLP-1. The
 glucose-lowering activity of mGLP-1 was also preliminarily determined.
 SN 0929-8665
 PY 2010
 VL 17
 IS 10
 BP 1245
 EP 1250
 UT ISI:000281430400009
 PT J
 AU Zhou, JP
 Ni, SJ
 Zhang, HB
 Qian, H
 Chi, YS
 Huang, WL
 Yu, L
 Hu, XW
 Chen, W
 AF Zhou, Jinpei
 Ni, Shuaijian
 Zhang, Huibin
 Qian, Hai
 Chi, Yushi
 Huang, Wenlong
 Yu, Lu
 Hu, Xiaowen
 Chen, Wei
 TI Synthesis and Bioactivity Evaluation of Dipeptidyl Peptidase IV
 Resistant Glucagon-like Peptide-1 Analogues
 SO PROTEIN AND PEPTIDE LETTERS
 AB Glucagon-like peptide -1 (GLP-1) is an incretin hormone displaying
 glucose-dependent stimulation of insulin secretion and trophic effects
 on the pancreatic beta-cells. However, GLP-1 is rapidly degraded to
 GLP-1(9-36) by dipeptidyl peptidase-IV (DPP-IV), which removes the
 N-terminal dipeptide His(7)-Ala(8). The rapid inactivation of GLP-1
 in the blood circulation limits its clinical application. Hence, we
 replaced the enzymatic hydrolyzation position Ala(8) with other
 natural amino acids. The GLP-1 analogues were synthesized rapidly and
 efficiently under microwave irradiation, using Fmoc/tBu orthogonal
 protection strategy. Studies on blood-glucose-lowering effect of GLP-1
 analogues in vivo were undertaken using 10-week-old male Kunming mice.
 The metabolic stability was tested by incubation with dipeptidyl
 peptidase-IV (DPP-IV). Generally, Xaa(8)-GLP-1 analogues exhibit
 resistance to DPP-IV degradation in vitro and stronger hypoglycemic
 effect than GLP-1. This may help to understand the structure-activity
 relationship of GLP-1 analogues.
 SN 0929-8665
 PY 2010
 VL 17
 IS 10
 BP 1290
 EP 1295
 UT ISI:000281430400016
 PT J
 AU Wang, X
 Yao, J
 Zhou, JP
 Lu, Y
 Wang, W
 AF Wang, X.
 Yao, J.
 Zhou, J. P.
 Lu, Y.
 Wang, W.
 TI Synthesis and evaluation of chitosan-graft-polyethylenimine as a gene
 vector
 SO PHARMAZIE
 AB The objective of this study was to prepare a series of
 chitosan-graft-polyethylenimine (chitosan-g-PEI) copolymers as gene
 carriers with high transfection efficiency and low cytotoxicity.
 Chitosan-g-PEIs with different molecular weights and segments were
 successfully synthesized by both oxidation and imine reactions and then
 characterized by H-1 NMR, IR, UV and DSC. All types of Chitosan-g-PEIs
 prepared were found to interact efficiently with plasmid DNA
 (pIRES2-EGFP-p53) on DNA retardation assays. The Chitosan-g-PEI/DNA
 complex had a diameter of approximately 200 nm and a surface potential
 of zeta = +10.0 mV when the N/P ratio was 15/1. Optimal transfection
 efficiency of the chitosan-g-PEI/DNA complex was observed at N/P = 45/1
 on HepG2 cells, with significantly lower toxicity compared with the
 gold standard PEI 25 kd. Moreover, the results showed that the toxicity
 increased with increasing molecular weight of the PEI segment in
 chitosan-g-PEI. Based on these results, chitosan-g-PEI with different
 chitosan and PEI segments of could be used for gene expression on
 different levels, and some of them may appear as potential candidates
 for gene delivery systems.
 SN 0031-7144
 PD AUG
 PY 2010
 VL 65
 IS 8
 BP 572
 EP 579
 DI 10.1691/ph.2010.9422
 UT ISI:000281349100003
 PT J
 AU Wu, GQ
 Wu, HB
 Fan, XB
 Zhao, R
 Li, XF
 Wang, SL
 Ma, YH
 Shen, ZL
 Xi, T
 AF Wu, Guoqiu
 Wu, Hongbin
 Fan, Xiaobo
 Zhao, Rui
 Li, Xiaofang
 Wang, Shenglan
 Ma, Yihua
 Shen, Zilong
 Xi, Tao
 TI Selective toxicity of antimicrobial peptide S-thanatin on bacteria
 SO PEPTIDES
 AB S-thanatin, an analog of thanatin, was synthesized by substituting the
 15th amino acid of threonine with serine, which showed a broad
 antimicrobial activity against bacteria. We reported earlier that
 membrane phospholipid was found to be the target for S-thanatin with
 different mechanism from other antimicrobial peptides. In this study,
 we have performed its structural characterization by circular
 dichroism (CD) spectroscopy. The CD analysis showed that S-thanatin
 retained its overall conformation beta-sheet in aqueous buffer,
 beta-turn in 50% trifluoroethanol (TFE) and beta-hairpin in 0.4 mM
 POPC-LUVs. In hemolysis assay, S-thanatin exhibited low hemolytic
 activity and bacteria selectivity. We investigated the effect of the
 presence of 33 mol percent cholesterol on the interactions of the
 antimicrobial peptide S-thanatin with phosphatidylcholine (PC) model
 membrane systems. The results showed that S-thanatin was more potent
 at disrupting cholesterol-free bacterial than cholesterol-containing
 eukaryotic membranes. Thus, in all respects, fluorescence dye leakage
 experiments indicated that cholesterol inhibited the
 S-thanatin-induced permeabilization of PC vesicles. Finally, flow
 cytometry was used to monitor changes in bacterial cell membrane
 potential and cell membrane integrity, with specific fluorescent dyes
 DiBAC(4)(3) and PI. Adding the respiratory poison CCCP seemed to
 prevent peptide-induced membrane damage, which suggested that
 S-thanatin acted at the metabolic level on respiratory chain. These
 findings might explain why S-thanatin was selective toxicity towards
 bacteria, but low toxicity towards erythrocytes. It might be due to
 three factors at least: electrostatic interaction (namely anionic
 phospholipids); cholesterol; respiratory chain. (C) 2010 Elsevier Inc.
 All rights reserved.
 SN 0196-9781
 PD SEP
 PY 2010
 VL 31
 IS 9
 BP 1669
 EP 1673
 DI 10.1016/j.peptides.2010.06.009
 UT ISI:000281368400007
 PT J
 AU Lin, GW
 Wang, Y
 Zhou, QF
 Tang, WF
 Wang, JA
 Lu, T
 AF Lin, Guowu
 Wang, Yue
 Zhou, Qingfa
 Tang, Weifang
 Wang, Jian
 Lu, Tao
 TI A Facile Synthesis of 3-Substituted 9H-Pyrido[3,4-b]indol-1(2H)-one
 Derivatives from 3-Substituted beta-Carbolines
 SO MOLECULES
 AB A mild and efficient two-step synthesis of 3-substituted
 beta-carbolinone derivatives from 3-substituted beta-carboline in
 good yields is described. A possible reaction mechanism for the
 formation of the skeleton of beta-carbolin-1-one is proposed. The
 structures of these compounds were established by IR, H-1-NMR,
 C-13-NMR, mass spectrometry and elemental analysis, as well as X-ray
 crystallographic analysis of 4-2 and 6-2.
 SN 1420-3049
 PD AUG
 PY 2010
 VL 15
 IS 8
 BP 5680
 EP 5691
 DI 10.3390/molecules15085680
 UT ISI:000281481100037
 PT J
 AU Dong, J
 Yao, SW
 Zhou, XD
 Zhang, LJ
 Xu, YG
 AF Dong, Jin
 Yao, Shuowei
 Zhou, Xiaodong
 Zhang, Lijuan
 Xu, Yungen
 TI Synthesis of N-Heteroaroyl Aminosaccharide Derivatives as Fibroblast
 Growth Factor 2 Signaling Modulators
 SO CHEMICAL & PHARMACEUTICAL BULLETIN
 AB Fibroblast growth factor 2 (FGF2) signaling plays an important role
 in angiogenesis. Heparin/heparan sulfate (HS) is required for FGF2
 signaling but heparin mimics either promotes or inhibits FGF2
 signaling. To take advantage such properties of heparin mimics, a
 series of N-heteroaroyl aminosaccharide derivatives were designed and
 synthesized as FGF2 signaling modulators. The bioactivity was
 determined in a FGF2 and heparin-dependent cell proliferation assay
 using FGFR1c expressing BaF3 cells. We found that most of the compounds
 inhibited heparin- and FGF2-dependent BaF3 cell proliferation while
 three compounds promoted the cell proliferation. These results suggest
 that the small molecular heparin mimics approach might be useful in
 developing novel anti-angiogenic agents.
 SN 0009-2363
 PD SEP
 PY 2010
 VL 58
 IS 9
 BP 1210
 EP 1215
 UT ISI:000281436900014
 PT J
 AU Zhang, HW
 Zhang, H
 Zhang, YQ
 Ng, SS
 Ren, FL
 Wang, YY
 Duan, YQ
 Chen, L
 Zhai, YG
 Guo, QL
 Chang, ZJ
 AF Zhang, Haiwei
 Zhang, Hui
 Zhang, Yanquan
 Ng, Ser Sur
 Ren, Fangli
 Wang, Yingying
 Duan, Yaqi
 Chen, Lin
 Zhai, Yonggong
 Guo, Qinglong
 Chang, Zhijie
 TI Dishevelled-DEP domain interacting protein (DDIP) inhibits Wnt
 signaling by promoting TCF4 degradation and disrupting the
 TCF4/beta-catenin complex
 SO CELLULAR SIGNALLING
 AB The TCF4/beta-catenin complex, the executor of canonical
 Wnt/beta-catenin signaling, is regulated by a variety of factors. Among
 these, Dishevelled (Dvl) is a critical regulator that releases
 beta-catenin from degradation and stabilizes TCF4/beta-catenin
 complex. Here, we report that DDIP (Dishevelled-DEP domain Interacting
 Protein, also named as Spats1. spermatogenesis associated, serine-rich
 1), a novel protein that interacts with Dvl, regulates Wnt signaling.
 We provide evidence that DDIP suppresses Lef-1 luciferase reporter
 activity stimulated by Wnt1. Dvl2 or beta-catenin, interacts with the
 TCF4/beta-catenin complex, and disrupts the interaction of TCF4 and
 beta-catenin by promoting TCF4 degradation through the proteasome
 pathway. Our results indicate that DDIP is a negative regulator of the
 canonical Wnt signaling. (C) 2010 Elsevier Inc. All rights reserved.
 SN 0898-6568
 PD NOV
 PY 2010
 VL 22
 IS 11
 BP 1753
 EP 1760
 DI 10.1016/j.cellsig.2010.06.016
 UT ISI:000281463500018
 PT J
 AU Song, M
 Zhao, H
 Wang, L
 Yang, L
 Hang, TJ
 Wen, AD
 AF Song, Min
 Zhao, Hua
 Wang, Li
 Yang, Lin
 Hang, Taijun
 Wen, Aidong
 TI Development and validation of a robust LC-MS-MS with atmospheric
 pressure chemical ionization for quantitation of carbazochrome sodium
 sulfonate in human plasma: application to a pharmacokinetic study
 SO BIOMEDICAL CHROMATOGRAPHY
 AB A highly selective and sensitive liquid chromatography coupled with
 atmospheric pressure chemical ionization tandem mass spectrometry
 (LC-APCI-MS-MS) was developed and validated for the quantitation and
 pharmacokinetic study of carbazochrome sodium sulfonate in human
 plasma. Protein precipitation with 14% perchloric acid solution was
 selected for sample preparation, and amiloride hydrochloride was
 employed as an internal standard. The analytes were separated on a
 Hypersil ODS-2 column by a multiple-step linear gradient elution with
 a mobile phase consisting of 0.2% formic acid solution and methanol
 pumped at a flow rate of 1.0 mL/min. The determination was optimized
 and carried out with positive atmospheric pressure chemical ionization
 by selective reaction monitoring of the ion of m/z 148, the protonated
 thermodegraded fragment of the free acidic form of carbazochrome sodium
 sulfonate selected as the parent, and the ion of m/z 107 as the optimum
 collision induced dissociation (CID) product. The method was fully
 validated over a concentration range of 0.5-50 ng/mL, with the lower
 limit of quantitation of 0.5 ng/mL. The application of the LC-MS-MS
 method was demonstrated for the specific and quantitative analysis of
 carbazochrome sodium sulfonate in human plasma from a pharmacokinetic
 study in 24 healthy male Chinese volunteers after a single oral
 administration of 90 mg carbazochrome sodium sulfonate capsules.
 Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0269-3879
 PD SEP
 PY 2010
 VL 24
 IS 9
 BP 990
 EP 999
 DI 10.1002/bmc.1397
 UT ISI:000281424600012
 PT J
 AU Liu, YD
 Ma, SP
 Qu, R
 AF Liu, Yadong
 Ma, Shiping
 Qu, Rong
 TI SCLM, total saponins extracted from Chaihu-jia-longgu-muli-tang,
 reduces chronic mild stress-induced apoptosis in the hippocampus in
 mice
 SO PHARMACEUTICAL BIOLOGY
 AB Increasing evidence demonstrates that stress or depression can lead
 to atrophy and cell loss in the hippocampus. In contrast,
 antidepressant treatment significantly reduces apoptosis in the
 dentate granule cell layer and subgranular zone in animal models of
 depression. In the present study, we investigated the neuroprotective
 action of SCLM, the total saponins extracted from
 Chaihu-jia-longgu-muli-tang, a traditional Chinese medicinal formula
 which was prescribed 1000 years ago, in the reduction of apoptosis in
 hippocampal neurons using an experimental chronic mild stress (CMS)
 model. Mice were subjected to the CMS procedure for a period of 21
 consecutive days. SCLM (100 mg/kg, p.o.) or fluoxetine (20 mg/kg, p.o.)
 was administered during the stress periods. CMS mice showed a decreased
 sucrose intake over 21 days, and an increase in the number of
 TUNEL-positive neurons as well as up-regulation of the
 apoptotic-related factors, such as Bax and caspase-3 in the
 hippocampus, compared with control mice. On the other hand, the
 administration of SCLM (100 mg/kg) and fluoxetine (20 mg/kg) reversed
 these effects induced by CMS, showing a significant increase of sucrose
 intake and a dramatic reduction of TUNEL-positive neurons and decreased
 expression of Bax and caspase-3 proteins. The present results suggest
 that SCLM possesses a significant antidepressant-like property, and
 this effect may be through protection against stress-induced neuronal
 apoptosis by affecting the expression of Bax and caspase-3 proteins
 in the hippocampus. These findings provide important information that
 the anti-apoptotic effect of herbal medicine therapy may be beneficial
 for the treatment of depression.
 SN 1388-0209
 PD AUG
 PY 2010
 VL 48
 IS 8
 BP 840
 EP 848
 DI 10.3109/13880200903296154
 UT ISI:000281304800001
 PT J
 AU Song, JX
 Kou, JP
 Huang, YL
 Yu, BY
 AF Song, Jiaxi
 Kou, Junping
 Huang, Yalin
 Yu, Boyang
 TI Ruscogenin Mainly Inhibits Nuclear Factor-kappa B but Not Akt and
 Mitogen-Activated Protein Kinase Signaling Pathways in Human Umbilical
 Vein Endothelial Cells
 SO JOURNAL OF PHARMACOLOGICAL SCIENCES
 AB Our previous results suggested that ruscognin inhibited tumor necrosis
 factor alpha (TNF-alpha)-induced leukocyte adhesion, which correlated
 with its suppression of intercellular adhesion molecule-1 (ICAM-1)
 expression in endothelial cells. In the present studies, we further
 examined its effects on the main signaling pathways involved in
 upregulation of ICAM-1 induced by TNF-alpha in human umbilical vein
 endothelial cells (HUVECs). The results showed that ruscogenin
 significantly suppressed p65 phosphorylation, I kappa B-alpha
 phosphorylation and degration, and inhibited I kappa B kinase alpha
 (IKK alpha) and IKK beta activation induced by TNF-alpha. However, it
 exerted weak effects on TNF-alpha-induced phosphorylations of p38,
 JNK, ERK1/2, and Akt. Overall, our results indicated that
 downregulation of ICAM-1 expression by ruscogenin in HUVECs might be
 mediated by nuclear factor-kappa B (NF-kappa B), but not by
 mitogen-activated protein kinase (MAPK) and Akt signaling pathways.
 SN 1347-8613
 PD AUG
 PY 2010
 VL 113
 IS 4
 BP 409
 EP 413
 DI 10.1254/jphs.10076SC
 UT ISI:000281166400017
 PT J
 AU Hong, J
 Jiao, Y
 He, WJ
 Guo, ZJ
 Yu, Z
 Zhang, JF
 Zhu, LG
 AF Hong, Jin
 Jiao, Yang
 He, Weijiang
 Guo, Zijian
 Yu, Zhen
 Zhang, Junfeng
 Zhu, Longgen
 TI His-Oriented Peptide Hydrolysis Promoted by cis-[Pt(en)(H2O)(2)](2+):
 a New Specific Peptide Cleavage Site
 SO INORGANIC CHEMISTRY
 AB The new specific hydrolysis of histidine-containing peptides promoted
 by cis-[Pt(en)(H2O)(2)](2+) was investigated by electrospray
 ionization mass spectrometry (ESI-MS) and nuclear magnetic resonance
 spectrometry (NMR). MS determination demonstrated that
 cis-[Pt(en)(H2O)(2)](2+) anchors to AcGHG with the stoichiometry of
 either 1:1 or 2:1 (Pt/peptide), but only with 1:1 stoichoimetiy to
 AcGHL. Cis-[Pt(en)(H2O)(2)](2+) is able to promote the cleavage of the
 first downstream peptide bond from histidine at 60 degrees C and pH
 2.65, and Pt-anchored peptides are the essential intermediates for the
 promoted hydrolysis. Moreover, the larger amount of Pt(II) complex
 results in higher fragmental yield and higher hydrolysis rate. In the
 presence of 1 equiv of Pt(II) complex, H-1 NMR determination confirmed
 the apparent first-order kinetics of the Pt(II)-promoted hydrolysis
 and the hydrolysis rate for AcGHG and AcGHL is 0.20 day(-1) and 0.14
 day(-1), respectively. Moreover, Pt(II) coordinating to histidine
 imidazole is the key step to form the Pt(II)-anchored peptides. The
 Pt(II)-activating the first His-downstream carbonyl group via synergic
 coordinating to His imidazole and carbonyl O atom has been proposed
 for the Pt(II)-promoted his-oriented peptide hydrolysis. The lower
 rate for AcGHL should be correlated to the steric hindrance of Leu side
 chain to the second Pt(II) coordinating to tripeptide. In addition,
 the newly confirmed specific His-oriented peptide cleavage site
 implies a new potential strategy for target cleavage of peptides or
 proteins.
 SN 0020-1669
 PD SEP 6
 PY 2010
 VL 49
 IS 17
 BP 8148
 EP 8154
 DI 10.1021/ic101191m
 UT ISI:000281231800071
 PT J
 AU Xu, HA
 Gao, XH
 Song, L
 Wang, FY
 Xu, Z
 Lu, D
 Xu, XX
 Xia, YF
 Dai, Y
 AF Xu, Huan
 Gao, Xinghua
 Song, Jie
 Wang, Fengyun
 Xu, Zhao
 Lu, Dan
 Xu, Xianxiang
 Xia, Yufeng
 Dai, Yue
 TI Peoniflorin Prevents the Adhesion Between Inflammatory Endothelial
 Cells and Leukocytes Through Inhibiting the Activation of MAPKs and
 NF-kappa B
 SO DRUG DEVELOPMENT RESEARCH
 AB The vascular endothelium can be activated by multiple factors,
 including lipopolysaccharide (LPS) functioning as a key component of
 the inflammatory response. Activated endothelium promotes the
 recruitment of leukocytes mainly by releasing various adhesion
 molecules and amplifies inflammation via a feedback loop. Peoniflorin,
 the main active constituent of the roots of Paeonia lactiora Pall.,
 possesses anti-inammatory, anti-infective, and anti-platelet
 aggregative properties. To elucidate the anti-inammatory mechanism of
 peoniflorin, the present study was conducted to address its effects
 on the adhesion of inflammatory endothelial cells to leukocytes.
 Peoniflorin substantially reduced adhesion of either human acute
 monocytic leukemia cells (THP-1) or human acute promyelocytic leukemia
 cells (HL-60) to LPS-stimulated human umbilical vein endothelial cells
 (HUVECs). It also markedly down-regulated the expression of E-selectin
 at both the gene and protein levels. However, peoniflorin only slightly
 reduced expression of intercellular adhesion molecule-1 (ICAM-1).
 Signal pathway analysis indicated that peoniflorin reduced
 phosphorylation of c-Jun NH2-terminal kinase (JNK) and p38 kinase, as
 well as the phosphorylation and degradation of I kappa B-alpha in
 HUVECs. These findings suggest that prevention of the adhesion between
 inflammatory endothelial cells and leukocytes contributes, at least
 partially, to the anti-inflammation action of peoniflorin. The
 anti-adhesion mechanisms of peoniflorin were involved in the
 down-regulation of the activation of mitogen-activated protein kinases
 (MAPKs) and nuclear factor-kappa B (NF-kappa B), and a reduction of
 adhesion molecule expressions in endothelial cells. Drug Dev Res
 71:275-284, 2010. (C) 2010 Wiley-Liss, Inc.
 SN 0272-4391
 PD AUG
 PY 2010
 VL 71
 IS 5
 BP 275
 EP 284
 DI 10.1002/ddr.20372
 UT ISI:000281337000001
 PT J
 AU Guo, XA
 Chen, CL
 Yang, QA
 Yin, YM
 You, QD
 Tang, YQ
 AF Guo, Xiang
 Chen, Chun-Lin
 Yang, Qian
 Yin, Yue-Miao
 You, Qi-Dong
 Tang, Yi-Qun
 TI Effects of a Novel Class III Antiarrhythmic Agent, CPUY11018, on Rat
 Atrial Fibrillation
 SO DRUG DEVELOPMENT RESEARCH
 AB CPUY11018 has anti-atrial fibrillation (AF) effects in rats. The
 effects of CPUY11018 on the transient outward K+ current (I-to) and
 ultra-rapid delayed rectifier K+ current (I-Kur) were studied using
 whole-cell patch clamp techniques and an acetylcholine (ACh)-CaCl2
 induced AF model. CPUY11018 inhibited I-to and I-kur in a
 concentration-dependent manner with IC50 values of 18.5 and 1.7 mu M,
 respectively. Inhibition was independent of the depolarizing voltage.
 In the AF ACh-CaCl2 model, AF duration was effectively shortened after
 treatment with 5 mg/kg CPUY11018 for 4 days. These results indicate
 that CPUY11018 is effective in treating AF partly by blocking I-to and
 I-kur. Drug Dev Res 71:303-312, 2010. (C) 2010 Wiley-Liss, Inc.
 SN 0272-4391
 PD AUG
 PY 2010
 VL 71
 IS 5
 BP 303
 EP 312
 DI 10.1002/ddr.20375
 UT ISI:000281337000004
 PT J
 AU Zhang, Y
 Huo, MR
 Zhou, JP
 Xie, SF
 AF Zhang, Yong
 Huo, Meirong
 Zhou, Jianping
 Xie, Shaofei
 TI PKSolver: An add-in program for pharmacokinetic and pharmacodynamic
 data analysis in Microsoft Excel
 SO COMPUTER METHODS AND PROGRAMS IN BIOMEDICINE
 AB This study presents PKSolver, a freely available menu-driven add-in
 program for Microsoft Excel written in Visual Basic for Applications
 (VBA), for solving basic problems in pharmacokinetic (PK) and
 pharmacodynamic (PD) data analysis. The program provides a range of
 modules for PK and PD analysis including noncompartmental analysis
 (NCA), compartmental analysis (CA), and pharmacodynamic modeling. Two
 special built-in modules, multiple absorption sites (MAS) and
 enterohepatic circulation (EHC), were developed for fitting the
 double-peak concentration-time profile based on the classical
 one-compartment model. In addition, twenty frequently used
 pharmacokinetic functions were encoded as a macro and can be directly
 accessed in an Excel spreadsheet. To evaluate the program, a detailed
 comparison of modeling PK data using PKSolver and professional PK/PD
 software package WinNonlin and Scientist was performed. The results
 showed that the parameters estimated with PKSolver were satisfactory.
 In conclusion, the PKSolver simplified the PK and PD data analysis
 process and its output could be generated in Microsoft Word in the form
 of an integrated report. The program provides pharmacokinetic
 researchers with a fast and easy-to-use tool for routine and basic PK
 and PD data analysis with a more user-friendly interface. (C) 2010
 Elsevier Ireland Ltd. All rights reserved.
 SN 0169-2607
 PD SEP
 PY 2010
 VL 99
 IS 3
 BP 306
 EP 314
 DI 10.1016/j.cmpb.2010.01.007
 UT ISI:000281337700008
 PT J
 AU Yang, F
 Du, YX
 Chen, B
 Fan, QF
 Xu, GF
 AF Yang, Fan
 Du, Yingxiang
 Chen, Bin
 Fan, Qingfeng
 Xu, Guangfu
 TI Enantiomeric Separation of Nefopam Hydrochloride by Affinity
 Electrokinetic Chromatography Using Chondroitin Sulfate A as Chiral
 Selector and Its Chiral Recognition Mechanism
 SO CHROMATOGRAPHIA
 AB In this study, a new approach to the enantioseparation of nefopam
 hydrochloride by means of affinity electrokinetic chromatography
 (AEKC) with chondroitin sulfate A belonging to linear ionic
 polysaccharides has been developed. The difference in the
 antinociceptive activity of the enantiomers of nefopam was
 demonstrated in some studies, and the method established in this paper
 allowed complete separation of nefopam. Especially, there are no
 reports concerned with the enantioselective separation of nefopam
 using chondroitin sulfate A as chiral selectors in CE. During the course
 of this work, both migration time and enantioseparation of nefopam were
 influenced by several parameters such as pH of the BGE, selector
 concentration, capillary temperature and applied voltage.
 Consequently, these parameters were systematically optimized in order
 to obtain the optimum enantioseparation of nefopam. Moreover,
 comparison of the influences of the studied parameters was further
 investigated using univariate analysis of variance as a calculation
 method by Statistical Product and Service Solutions (SPSS) in this
 paper. Finally, a mechanism of enantiorecognition in AEKC towards the
 enantiomers of nefopam with chondroitin sulfate A was described.
 SN 0009-5893
 PD SEP
 PY 2010
 VL 72
 IS 5-6
 BP 489
 EP 493
 DI 10.1365/s10337-010-1670-2
 UT ISI:000281174300017
 PT J
 AU Wu, GQ
 Fan, XB
 Wu, HB
 Liu, NF
 Li, XF
 Gou, LX
 Nie, Y
 Zhao, R
 Xi, T
 AF Wu, Guoqiu
 Fan, Xiaobo
 Wu, Hongbin
 Liu, Naifeng
 Li, Xiaofang
 Gou, Lixia
 Nie, Yu
 Zhao, Rui
 Xi, Tao
 TI Bioscreening of phage display antibody library and expression of a
 humanized single-chain variable fragment antibody against human
 connective tissue growth factor (CTGF/CCN2)
 SO BIOTECHNOLOGY AND APPLIED BIOCHEMISTRY
 AB Excessive expression of CTGF (connective tissue growth factor)/CCN2
 has been observed in many fibrotic diseases. The inhibition of the
 CTGF/CCN2 by antibody has been shown to be clinically useful for the
 management of fibrosis. A phage display humanized single-chain Fv
 antibody library was screened using CTGF/C (CTGF/CCN2 C-terminal
 domain) as the target. A phage ELISA was performed after four rounds
 of biopanning, and ten positive clones were further evaluated by ELISA
 and were chosen for DNA sequencing. The DNA encoding scFv (single-chain
 variable fragment) containing a full-length variable domain fragment
 of heavy chain and light chain of human immunoglobulin was inserted
 into pET-32(a)+ vector, and the fusion protein (TrxA-scFv) containing
 a thrombin cleavage site was expressed mainly in soluble form. The scFv
 was obtained by purified fusion protein digested with thrombin and then
 separated from the fusion partner TrxA by gel-filtration
 chromatography. An immunological assay showed that the purified scFv
 reacted with CTGF/CCN2 in a concentration-dependent manner. The result
 of the cell migration assay demonstrated that the scFv at 100 ng/ml
 could effectively inhibit the migration of HUVEC (human umbilical-vein
 endothelial cells) caused by CTGF/C. The number of migratory cells was
 significantly decreased as compared with the negative control (1062
 +/- 92 versus 3269 +/- 288, P < 0.001) and the inhibition rate was 90.5%.
 SN 0885-4513
 PD JUL
 PY 2010
 VL 56
 PN Part 3
 BP 95
 EP 102
 DI 10.1042/BA20100031
 UT ISI:000281317000002
 PT J
 AU Gu, Y
 Wang, GJ
 Wu, XL
 Zheng, YT
 Zhang, JW
 Ai, H
 Sun, JG
 Jia, YW
 AF Gu, Y.
 Wang, G. -J.
 Wu, X. -L.
 Zheng, Y. -T.
 Zhang, J. -W.
 Ai, H.
 Sun, J. -G.
 Jia, Y. -W.
 TI Intestinal absorption mechanisms of ginsenoside Rh2:
 stereoselectivity and involvement of ABC transporters
 SO XENOBIOTICA
 AB 1. This study investigated the absorption mechanism of ginsenoside Rh2
 to clarify the reasons for its poor absorption. Transepithelial
 transport across Caco-2 cell monolayers, cellular uptake, and in situ
 rat intestinal perfusion were examined.
 2. Cellular uptake of Rh2 was linear from 1 to 50 mu M at 4 degrees
 C, whereas it was saturated when the concentration exceeded 10 mu M
 at 37 degrees C. At 37 degrees C, the uptake at 10 mu M was linear in
 60 min. Intracellular exposure in 240 min was 2173.70 and 979.38 ng .
 min/mu g for S and R isomers, respectively.
 3. Transepithelial permeability of Rh2 was about 10(-8) to 10(-7) cm/s.
 Efflux ratios were above 1.5. Sodium dodecyl sulfate, sodium citrate,
 and sodium deoxycholate had no effect on Rh2 permeability.
 4. After intestinal perfusion for 3 h, 9.1% of 20(R)- Rh2 and 15.7%
 of 20(S)- Rh2 were absorbed.
 5. Cyclosporine, quercetin, and probenecid could improve the cellular
 uptake, absorptive permeability, and intestinal absorption.
 Carrier-mediated transport was the major absorption mechanism. Rh2 was
 a substrate of ABC transporters.
 6. The ABC-transporter-mediated efflux and the poor permeability were
 the major reasons for Rh2 poor absorption. 7. The stereoselective
 absorption was significant. R isomer exhibited lower absorption
 profiles in all the experiments, possibly due to more potent efflux.
 SN 0049-8254
 PD SEP
 PY 2010
 VL 40
 IS 9
 BP 602
 EP 612
 DI 10.3109/00498254.2010.500744
 UT ISI:000280993500002
 PT J
 AU Zhao, Q
 Wang, J
 Zou, MJ
 Hu, R
 Zhao, L
 Qiang, L
 Rong, JJ
 You, QD
 Guo, QL
 AF Zhao, Qing
 Wang, Jia
 Zou, Mei-Juan
 Hu, Rong
 Zhao, Li
 Qiang, Lei
 Rong, Jing-Jing
 You, Qi-Dong
 Guo, Qing-Long
 TI Wogonin potentiates the antitumor effects of low dose 5-fluorouracil
 against gastric cancer through induction of apoptosis by
 down-regulation of NF-kappaB and regulation of its metabolism
 SO TOXICOLOGY LETTERS
 AB Traditional Chinese medicines have been recognized as a new source of
 anticancer drugs or chemotherapy adjuvant to enhance the efficacy of
 chemotherapy and to ameliorate the side effects. Wogonin (WOG) has a
 potential for therapeutic use in the treatment of antitumor and
 chemoprophylaxis 5-Fluorouracil (5-FU) is a key systemic chemotherapy
 drug and widely use in the treatment of solid tumors In this study,
 we found that combination of WOG and 5-FU inhibited the viability of
 MGC-803 cells in a concentration-dependent manner and exhibited a
 synergistic anticancer effect (Cl < 1) when 5-FU was used at relatively
 low concentrations. The pro-apoptotic activity of two-drug combination
 was much stronger than single. Furthermore, WOG could decrease the mRNA
 levels of dihydropyrimidine dehydrogenase (DPD), the metabolic enzymes
 of 5-FU WOG could inhibit the NF-kappa B nuclear translocation and
 I-kappa B phosphorylation. Moreover, combined treatment caused
 significantly growth inhibition of human tumor xenografts. in
 addition, WOG markedly enhanced the antitumor activity of low dose 5-FU
 (i p 10 mg/kg/day), however there is no toxicity and influence on diet
 consumption in experimental animals. Taken together, our data's showed
 that WOG increased 5-FU retention for a prolonged catabolism by
 modulating 5-FU metabolic enzymes and sensitized the MGC-803 cells to
 5-FU induced apoptosis by inhibiting the NF-kappa B nuclear
 translocation. The anti-gastric cancer effect of two-drug combination
 was much stronger than that of WOG or 5-FU alone. These results may
 be relevant to design new clinical therapeutic strategies against
 gastric cancer in future (C) 2010 Elsevier Ireland Ltd All rights
 reserved.
 SN 0378-4274
 PD SEP 1
 PY 2010
 VL 197
 IS 3
 BP 201
 EP 210
 DI 10.1016/j.toxlet.2010.05.019
 UT ISI:000281002700008
 PT J
 AU Wu, YL
 Fan, QQ
 Lu, N
 Tao, L
 Gao, YA
 Qi, Q
 Guo, QL
 AF Wu, Yulin
 Fan, Qianqian
 Lu, Na
 Tao, Lei
 Gao, Yuan
 Qi, Qi
 Guo, Qinglong
 TI Breviscapine-induced Apoptosis of Human Hepatocellular Carcinoma Cell
 Line HepG2 was Involved in its Antitumor Activity
 SO PHYTOTHERAPY RESEARCH
 AB Breviscapine is a flavonoid constituent isolated from a traditional
 Chinese herb Erigerin breviscapus (Vant.) Hand-Mazz. To investigate
 the apoptosis-inducing effect of breviscapine on human hepatocellular
 carcinoma cell line HepG2 and explore the relative molecular
 mechanisms. HepG2 cells were treated with breviscapine at different
 concentrations and the inhibitory rate was analyzed by MTT assay. The
 morphological changes in cells were observed under an inverted light
 microscope and a fluorescence microscope and the apoptosis rate were
 detected by flow cytometry. Western blot was used to evaluate the
 protein expression. The viability of HepG2 cells was markedly inhibited
 in a concentration-dependent manner and obvious morphological changes
 were confirmed, including condensed chromatin and reduction in volume.
 The increased percentage of apoptotic cells was displayed by flow
 cytometry and the altered expression level of several
 apoptosis-associated proteins, Bcl-2, Bax and caspase-3, was detected
 by western blot. It is first discovered that breviscapine exhibited
 potential antitumor activity, induces remarkable apoptosis in HepG2
 cells and promises to be a new candidate in future cancer therapy.
 Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0951-418X
 PD AUG
 PY 2010
 VL 24
 IS 8
 BP 1188
 EP 1194
 DI 10.1002/ptr.3002
 UT ISI:000281006500013
 PT J
 AU Zhu, JJ
 Zhang, CF
 Zhang, MA
 Bligh, SWA
 Yang, L
 Wang, ZM
 Wang, ZT
 AF Zhu, Jing-Jing
 Zhang, Chao-Feng
 Zhang, Mian
 Bligh, S. W. Annie
 Yang, Li
 Wang, Zhi-Min
 Wang, Zheng-Tao
 TI Separation and identification of three epimeric pairs of new C-glucosyl
 anthrones from Rumex dentatus by on-line high performance liquid
 chromatography-circular dichroism analysis
 SO JOURNAL OF CHROMATOGRAPHY A
 AB Six C-glucosyl anthrones were characterized as three pairs of epimers
 by on-line high performance liquid chromatography-circular dichroism
 (HPLC-CD) analysis and isolated from the roots of Rumex dentatus by
 column chromatography. Their structures were elucidated by mass
 spectrometry, nuclear magnetic spectroscopy and HPLC-CD analysis. They
 are 10R-C-beta-D-glucosyl-10-hydroxyemodin-9-anthrone (rumejaposide
 E, 1) and 10S-C-beta-D-glucosyl-10-hydroxyemodin-9-anthrone
 (rumejaposide F, 2), 10R-C-beta-D-glucosylemodin-9-anthrone
 (rumejaposide G, 3) and 10S-C-beta-D-glucosylemodin-9-anthrone
 (rumejaposide H. 4).
 10S-C-beta-D-glucosyl-10-hydroxychrysophanol-9-anthrone
 (cassialoin, 5) and
 10R-C-beta-D-glucosyl-10-hydroxychrysophanol-9-anthrone
 (rumejaposide I. 6). Rumejaposides F-I (2-4 and 6) were new C-glucosyl
 anthrones. Rumejaposide E (1) and cassialoin (5) were isolated for the
 first time in Rumex plants. On-line HPLC-UV-CD analysis was a useful
 tool for structure elucidating epimeric C-glycosides anthrones 3-6
 because of the poor stability of the pure isomers (3 and 4) and the
 minute quantity of 5 and 6 in the mixture. (C) 2010 Elsevier B.V. All
 rights reserved.
 SN 0021-9673
 PD AUG 13
 PY 2010
 VL 1217
 IS 33
 BP 5384
 EP 5388
 DI 10.1016/j.chroma.2010.05.039
 UT ISI:000280970500009
 PT J
 AU Gan, L
 Han, S
 Shen, JQ
 Zhu, JB
 Zhu, CL
 Zhang, XX
 Gan, Y
 AF Gan, Li
 Han, Shun
 Shen, Jinqiu
 Zhu, Jiabi
 Zhu, Chunliu
 Zhang, Xinxin
 Gan, Yong
 TI Self-assembled liquid crystalline nanoparticles as a novel ophthalmic
 delivery system for dexamethasone: Improving preocular retention and
 ocular bioavailability
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB The object of this study was to design novel self-assembled liquid
 crystalline nanoparticles (cubosomes) as an ophthalmic delivery system
 for dexamethasone (DEX) to improve its preocular retention and ocular
 bioavailability DEX cubosome particles were produced by fragmenting
 a cubic crystalline phase of monoolein and water in the presence of
 stabilizer Poloxamer 407. Small angle X-ray diffraction (SAXR)
 profiles revealed its internal structure as Pn3m space group,
 indicating the diamond cubic phase. In vitro, the apparent permeability
 coefficient of DEX administered in cubosomes exhibited a 4.5-fold (F1)
 and 3 5-fold (F2) increase compared to that of Dex-Na phosphate eye
 drops Preocular retention studies revealed that the retention of
 cubosomes was significantly longer than that of solution and carbopol
 gel, with AUC(0 -> 180min) of Rh B cubosomes being 2-3-fold higher than
 that of the other two formulations In vivo pharmacokinetics in aqueous
 humor was evaluated by microdialysis, which indicated a 1 8-fold (F1)
 increase in AUC(0 -> 240min) of DEX administered in cubosomes relative
 to that of Dex-Na phosphate eye drops, with about an 8-fold increase
 compared to that of DEX suspension Corneal cross-sections after
 incubation with DEX cubosomes demonstrated an unaffected corneal
 structure and tissue integrity, which indicated the good
 biocompatibility of DEX cubosomes In conclusion, self-assembled liquid
 crystalline nanoparticles might represent a promising vehicle for
 effective ocular drug delivery Crown Copyright (C) 2010 Published by
 Elsevier B V. All rights reserved
 SN 0378-5173
 PD AUG 30
 PY 2010
 VL 396
 IS 1-2
 BP 179
 EP 187
 DI 10.1016/j.ijpharm.2010.06.015
 UT ISI:000280936000025
 PT J
 AU Tong, L
 Xiong, RS
 Jiang, H
 Jiang, XR
 Sun, HB
 Jiang, HL
 Shen, JS
 AF Tong, Ling
 Xiong, Ruisheng
 Jiang, Hong
 Jiang, Xiangrui
 Sun, Hongbin
 Jiang, Hualiang
 Shen, Jingshan
 TI IMPROVED TOTAL SYNTHESIS OF RACEMIC RUTAMARIN
 SO HETEROCYCLES
 AB An improved, convenient and cost-effective process, using
 2,4-dihydroxybenzaldehyde 2 as starting material for (+/-)-rutamarin
 1, is described. The overall yield of 1 is 44% in eight steps, requiring
 no chromatographic purification.
 SN 0385-5414
 PD JUL 1
 PY 2010
 VL 81
 IS 7
 BP 1697
 EP 1702
 DI 10.3987/COM-10-11962
 UT ISI:000281076100009
 PT J
 AU Zha, XM
 Zhang, FR
 Shan, JQ
 Zhang, YH
 Liu, JO
 Sun, HB
 AF Zha, Xiao Ming
 Zhang, Fei Ran
 Shan, Jia Qi
 Zhang, Yi Hua
 Liu, Jun O.
 Sun, Hong Bin
 TI Synthesis and evaluation of in vitro anticancer activity of novel
 solasodine derivatives
 SO CHINESE CHEMICAL LETTERS
 AB Solasodine 11 is a steroidal alkaloid with various biological
 activities. Herein, 8 novel solasodine derivatives were synthesized
 and their effect on prostate cancer cell proliferation was assessed
 in vitro. Significant improvement in antiproliferative activity was
 achieved among some of the synthetic analogs. In particular, 19
 exhibited the most potent inhibitory effect against the proliferation
 of PC-3 cell line (IC50 = 3.91 mu mol/L). (C) 2010 Jun O. Liu. Published
 by Elsevier B.V. on behalf of Chinese Chemical Society. All rights
 reserved.
 SN 1001-8417
 PD SEP
 PY 2010
 VL 21
 IS 9
 BP 1087
 EP 1090
 DI 10.1016/j.cclet.2010.04.020
 UT ISI:000280945100018
 PT J
 AU Yang, QA
 Fedida, D
 Xu, HJ
 Wang, BH
 Du, LP
 Wang, XJ
 Li, MY
 You, QD
 AF Yang, Qian
 Fedida, David
 Xu, Hongjian
 Wang, Binghe
 Du, Lupei
 Wang, Xiaojian
 Li, Minyong
 You, Qidong
 TI Structure-Based Virtual Screening and Electrophysiological Evaluation
 of New Chemotypes of K(V)1.5 Channel Blockers
 SO CHEMMEDCHEM
 AB Atrial fibrillation (AF) is the most prevalent nonfatal cardiac rhythm
 disorder associated with an increased risk of heart failure and stroke.
 Considering the ventricular side effects induced by anti-arrhythmic
 agents in current use, K(v)1.5 channel blockers have attracted a great
 deal of deliberation owing to their selective actions on atrial
 electrophysiology. Herein we report new chemotypes of K(v)1.5 channel
 blockers that were identified through a combination of structure-based
 virtual screening and in silico druglike property prediction including
 six scoring functions, as well as electrophysiological evaluation.
 Among them, five of the 18 compounds exhibited >50% blockade ratio at
 10 mu m, and have structural features different from conventional
 K(v)1.5 channel blockers. These novel scaffolds could serve as hits
 for further optimization and SAR studies for the discovery of selective
 agents to treat AF.
 SN 1860-7179
 PD JUL
 PY 2010
 VL 5
 IS 8
 BP 1353
 EP 1358
 DI 10.1002/cmdc.201000162
 UT ISI:000281061300020
 PT J
 AU Rong, JJ
 Hu, R
 Song, XM
 Ha, J
 Lu, N
 Qi, Q
 Tao, L
 You, QD
 Guo, QL
 AF Rong, Jing-Jing
 Hu, Rong
 Song, Xiu-Ming
 Ha, Jun
 Lu, Na
 Qi, Qi
 Tao, Lei
 You, Qi-Dong
 Guo, Qing-Long
 TI Gambogic acid triggers DNA damage signaling that induces
 p53/p21(Waf1/CIP1) activation through the ATR-Chk1 pathway
 SO CANCER LETTERS
 AB Gambogic acid (GA) has been wildly studied to show potent anti-tumor
 effects in vivo and in vitro. We have confirmed that GA stabilized and
 activated p53 through down-regulating the expression of MDM2 in variety
 of cancer cell lines. However, GA-induced p53 activation could be
 partially reversed by caffeine, a PI3k inhibitor. Therefore, questions
 of whether GA induces post-translational modifications of p53 and
 subsequent activation of p53; and if that is the case, which upstream
 signaling pathway(s) is (are) responsible for that are proposed. Here,
 the relationship between p53 activation and its post-translational
 modifications was investigated in the human cancer cell lines HepG2
 and A549 in response to GA or adriamycin treatment. GA induces p53
 phosphorylation at sites Ser15 and Ser20 in a concentration- or
 time-dependent way, which was a direct result of DNA damage, as
 gamma-HA2X foci and 'comet' DNA fragments were detected. GA induces
 p53 phosphorylation through activation of an ATM- and Rad3-related
 pathway, and GA-induced phosphorylation of Chk1 is also involved. Upon
 treatment with GA, AIR activation is clearly associated with p53
 phosphorylation, as well as activation of its target gene
 p21(Waf/CIP1). Furthermore, we found the dephosphorylation of Cdk1 at
 Thr161 induced by GA was abrogated, followed by a remarkable disruption
 of G2/M arrest when the cells were pre-incubated with caffeine.
 Interestingly, the sensitivity to caffeine enhanced the cytotoxicity
 of GA as well. Taken together, these data showed an important role of
 the DNA damage response mediated by ATR-Chk1 in p53/p21(Waf/CIP1)
 activation and downstream G2/M arrest during GA treatment. (C) 2010
 Elsevier Ireland Ltd. All rights reserved.
 SN 0304-3835
 PD OCT 1
 PY 2010
 VL 296
 IS 1
 BP 55
 EP 64
 DI 10.1016/j.canlet.2010.03.016
 UT ISI:000281025700008
 PT J
 AU Chen, FH
 Zhang, LB
 Qiang, L
 Yang, Z
 Wu, TA
 Zou, MJ
 Tao, L
 You, QD
 Li, ZY
 Yang, Y
 Guo, QL
 AF Chen, Fei-hong
 Zhang, Lin-bo
 Qiang, Lei
 Yang, Zhen
 Wu, Tian
 Zou, Mei-juan
 Tao, Lei
 You, Qi-dong
 Li, Zhi-yu
 Yang, Yong
 Guo, Qing-Long
 TI Reactive oxygen species-mitochondria pathway involved in
 LYG-202-induced apoptosis in human hepatocellular carcinoma HepG(2)
 cells
 SO CANCER LETTERS
 AB Previously, we demonstrated that LYG-202, a newly synthesized
 flavonoid with a piperazine substitution, exhibited obvious antitumor
 activity in vivo and in vitro. The exact mechanism of this new compound
 remains unclear. In the present study, we examined the effects of
 LYG-202 on reactive oxygen species (ROS) production and the downstream
 signaling pathway in the apoptosis of human hepatocellular carcinoma
 HepG2 cells. Pretreatment with NAC (N-acetylcysteine), a ROS
 production inhibitor, partly inhibited the apoptosis induced by
 LYG-202 via blocking the ROS generation. Further data revealed that
 LYG-202 induced ROS accumulation followed by a decrease in
 mitochondrial membrane potential (MMP), release of cytochrome c (Cyt
 c) and apoptosis-inducing factor (AIF) to cytosol, which induced
 apoptosis of the cells. Moreover, the mitogen-activated protein
 kinases (MAPK), the downstream effect of ROS accumulation including
 c-Jun N-terminal kinase (JNK) and p38 MAPK, could be activated by
 LYG-202. Taken together, the generation of ROS might play an important
 role in LYG-202-induced mitochondrial apoptosis pathway, which
 provided further support for LYG-202 as a novel anticancer therapeutic
 candidate. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
 SN 0304-3835
 PD OCT 1
 PY 2010
 VL 296
 IS 1
 BP 96
 EP 105
 DI 10.1016/j.canlet.2010.04.004
 UT ISI:000281025700012
 PT J
 AU Fan, QQ
 Wang, QJ
 Zeng, BB
 Ji, WH
 Ji, H
 Wu, YL
 AF Fan, Qian-Qian
 Wang, Qiu-Juan
 Zeng, Bu-Bing
 Ji, Wen-Hao
 Ji, Hui
 Wu, Yu-Lin
 TI Apoptosis induction of ZBB-006, a novel synthetic diterpenoid, in the
 human hepatocellular carcinoma cell line HepG2 in vitro and in vivo
 SO CANCER BIOLOGY & THERAPY
 AB Diterpenes, present in many medicinal plants, have been the focus of
 continuous studies for the development of new anticancer agents.
 ZBB-006 is a new synthetic diterpenoid derivative which exhibited
 significant anti-proliferation activity against various cancer cell
 lines in our previous study. Here, we investigated the antitumor effect
 of ZBB-006 and its potential mechanisms in the human hepatocellular
 carcinoma cell line HepG2, both in vitro and in vivo. We found that
 oral administration of ZBB-006 effectively suppressed the growth of
 HepG2 xenograft tumor in nude mice without body weight decline,
 compared with the control group. Meanwhile, the growth inhibitory
 effect of ZBB-006 on HepG2 cells was observed with MTT assay. Then
 apoptosis induced by ZBB-006 in HepG2 cells was evidenced by DAPAPI
 staining and Annexin V/PI double staining assay. ZBB-006 also
 dissipated the mitochondrial membrane potential (Delta Psi m)
 apparently as revealed by JC-1 staining. Furthermore, the cleavage of
 PAPARP, activation of caspase-3 and caspase-9 but not caspase-8 was
 demonstrated by western blot assay both in vitro and in vivo.
 Additionally, the proapoptotic protein Bax was markedly elevated,
 while the antiapoptotic protein Bcl-2 was downregulated. Collectively,
 our data indicated that ZBB-006 exerted a strong antitumor effect on
 HepG2 cells by initiating the mitochondrial-dependent apoptosis, and
 it has potential to be explored as a new promising therapeutic agent
 against human hepatoma.
 SN 1538-4047
 PD AUG 1
 PY 2010
 VL 10
 IS 3
 AR 12425
 UT ISI:000281005600011
 PT J
 AU Li, M
 Bao, Z
 Zhou, J
 Luo, N
 AF Li, M.
 Bao, Z.
 Zhou, J.
 Luo, N.
 TI DIMENSIONS CHARACTERIZING GOOD HEALTH BY CHINESE IN CHINA
 SO VALUE IN HEALTH
 SN 1098-3015
 PD MAY
 PY 2010
 VL 13
 IS 3
 BP A17
 EP A17
 UT ISI:000277121900079
 PT J
 AU Wang, XJ
 Gu, K
 Xu, JS
 Cao, RY
 Li, MH
 Wu, J
 Li, TM
 Liu, JJ
 AF Wang, Xue Jun
 Gu, Kai
 Xu, Jin Shu
 Cao, Rong Yue
 Li, Ming Hui
 Wu, Jie
 Li, Tai Ming
 Liu, Jing Jing
 TI Preparation of a peptide vaccine against GnRH by a bioprocess system
 based on asparaginase
 SO VACCINE
 AB GnRH is a promising target in hormone-dependent cancer immunotherapy.
 In our previous study, we have designed and purified a peptide vaccine
 GhM (GnRH3-hinge-MVP) by use of the bioprocess system based on
 asparaginase. Active immunization with GhM in the presence of CFA/IFA
 evoked strong humoral response. In this study, the motif NRLLLTG with
 high affinity to nanoparticle carrier VLP HBc Delta-SBD was fused to
 the C terminus of GhM to form a new peptide vaccine GhMNR
 (GnRH3-hinge-MVP-NRLLLTG). The fusion protein ansB-C-GhMNR was
 controlled by vigorous T7lac promotor and expressed effectively as
 inclusion bodies after induction by lactose and then purified by means
 of cell disruption, washing and cold ethanol fractionation. After
 hydrolyzed for 72 h, GhMNR was liberated from the fusion partner ansB-C
 and purified by CM52 cation exchange chromatography. These results
 suggested that the bioprocess system is suitable for large-scale
 expression and purification of the peptide vaccine GhMNR, and even some
 other proteins or peptides which may be important for industrial or
 laboratory purposes. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0264-410X
 PD JUL 12
 PY 2010
 VL 28
 IS 31
 BP 4984
 EP 4988
 DI 10.1016/j.vaccine.2010.05.026
 UT ISI:000280659600019
 PT J
 AU Huang, XJ
 Wang, Y
 Yin, ZQ
 Ye, WC
 AF Huang, Xiao-Jun
 Wang, Ying
 Yin, Zhi-Qi
 Ye, Wen-Cai
 TI Two new dimeric secoiridoid glycosides from the fruits of Ligustrum
 lucidum
 SO JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
 AB Two new secoiridoid glycosides, ligusides A and B (1 and 2), as well
 as seven known compounds (3-9), were isolated from the fruits of
 Ligustrum lucidum. Their structures were elucidated on the basis of
 spectroscopic and chemical analysis.
 SN 1028-6020
 PY 2010
 VL 12
 IS 8
 BP 685
 EP 690
 DI 10.1080/10286020.2010.490781
 UT ISI:000280817100008
 PT J
 AU Yang, LN
 Qian, ZY
 Ji, H
 Yang, RH
 Wang, YH
 Xi, LA
 Sheng, LA
 Zhao, BH
 Zhang, XM
 AF Yang, Lina
 Qian, Zhiyu
 Ji, Hui
 Yang, Ruhui
 Wang, Yuhuan
 Xi, Liang
 Sheng, Liang
 Zhao, Bohua
 Zhang, Xiaoming
 TI Inhibitory effect on protein kinase C theta by Crocetin attenuates
 palmitate-induced insulin insensitivity in 3T3-L1 adipocytes
 SO EUROPEAN JOURNAL OF PHARMACOLOGY
 AB Epidemiologic and experimental studies have pointed to an etiologic
 role of elevated plasma free fatty acids in insulin resistance, which
 is frequently associated with a state of low-grade inflammation. In
 this study, we investigated the effects of Crocetin, a unique
 carotenoid, on insulin resistance induced by palmitate in 3T3-L1
 adipocytes. Exposure of palmitate led to an increase in insulin
 receptor substrate-1 (IRS-1) serine(307) phosphorylation as well as
 activation of c-Jun NH2-terminal kinase (JNK) and inhibitor kappa B
 kinase 3 (IKK beta), concomitantly with reductions of IRS-1 function
 and glucose metabolism. Interestingly, pretreatment with Crocetin
 almost reversed all of these abnormalities in a dose-dependent manner.
 IRS-1 serine(307) phosphorylation was significantly reduced by JNK or
 IKK beta inhibitor, especially by combination of these two inhibitors.
 Moreover, palmitate treatment induced activation of protein kinase C
 theta (PKC theta) while blocking PKC theta significantly inhibited JNK
 and IKK beta activation induced by palmitate or phorbol 12-myristate
 13-acetate (PKC activator, PMA), and attenuated the palmitate-induced
 defects in insulin action. Crocetin demonstrated an impressive
 suppression in the activation of PKC theta induced not only by palmitate
 but also by PMA in a dose-dependent manner. Taken together, Crocetin
 inhibited JNK and IKK beta activation via suppression of PKC theta
 phosphorylation, attenuating insulin insensitivity induced by
 palmitate in 3T3-L1 adipocytes. (C) 2010 Elsevier B.V. All rights
 reserved.
 SN 0014-2999
 PD SEP 10
 PY 2010
 VL 642
 IS 1-3
 BP 47
 EP 55
 DI 10.1016/j.ejphar.2010.05.061
 UT ISI:000280681500006
 PT J
 AU Gao, MM
 Ma, C
 Liu, WC
 Zhu, J
 Tian, H
 Gao, XD
 Yao, WB
 AF Gao, Mingming
 Ma, Chen
 Liu, Wenchao
 Zhu, Jing
 Tian, Hong
 Gao, Xiangdong
 Yao, Wenbing
 TI Production and purification of an analog of glucagon-like peptide-1
 by auto-induction and on-column cleavage in Escherichia coli
 SO WORLD JOURNAL OF MICROBIOLOGY & BIOTECHNOLOGY
 AB As a promising type 2 anti-diabetic agent, glucagon-like peptide-1
 (GLP-1) is attracting more and more interest. Mutated GLP-1 (mGLP-1)
 is an analog of native GLP-1. To facilitate the production and
 purification of mGLP-1, auto-induction and on-column cleavage was
 employed in this study. By using auto-induction system, after 24 h of
 shaking culture, about 12.6 g wet bacterial cells could be obtained
 from 1 l medium, and this was about 3.6 times more than that of the
 IPTG-induction group. After disruption and centrifugation, the fusion
 protein was directly purified and cleaved on Ni-Sepharose 6 Fast Flow
 column. Then, RESOURCE15 RPC column was used for further purification.
 By using these two steps of purification, about 1.58 mg of mGLP-1 with
 the purity of up to 98% could be obtained from 1 g wet bacterial cells.
 In the bioactivity study, mGLP-1 displayed a significant and
 dose-dependent glucose-lowering activity. These results suggested
 that auto-induction and on-column cleavage could facilitate the
 production and purification of mGLP-1. These methods could also be
 applied to the preparation of other proteins and peptides.
 SN 0959-3993
 PD SEP
 PY 2010
 VL 26
 IS 9
 BP 1675
 EP 1682
 DI 10.1007/s11274-010-0345-3
 UT ISI:000280642800016
 PT J
 AU Yang, L
 Xue, XW
 Zhang, YH
 AF Yang, Lei
 Xue, Xiaowen
 Zhang, Yihua
 TI Simple and Efficient Synthesis of Belinostat
 SO SYNTHETIC COMMUNICATIONS
 AB A novel synthesis of belinostat (1) starting from 3-nitrobenzaldehyde
 has been developed. The key step in this sequence involves the
 conversion of (2E)-3-(3-aminophenyl)acrylic acid methyl ester to
 (2E)-3-(3-chlorosulfonylphenyl)acrylic acid methyl ester via
 diazotization and sulfonylation.
 SN 0039-7911
 PY 2010
 VL 40
 IS 17
 BP 2520
 EP 2524
 DI 10.1080/00397910903277870
 UT ISI:000280662300003
 PT J
 AU Luo, Y
 Liu, M
 Xia, Y
 Dai, Y
 Chou, G
 Wang, Z
 AF Luo, Y.
 Liu, M.
 Xia, Y.
 Dai, Y.
 Chou, G.
 Wang, Z.
 TI Therapeutic effect of norisoboldine, an alkaloid isolated from Radix
 Linderae, on collagen-induced arthritis in mice
 SO PHYTOMEDICINE
 AB The alkaloid fraction of Radix Linderae, the main active component of
 this herb drug, has been proven to exhibit anti-inflammatory,
 analgestic and antimicrobial activities. The present study was
 undertaken to investigate the therapeutic potential of norisoboldine,
 the major isoquinoline alkaloid present in Radix Linderae, in collagen
 II -induced arthritis (CIA) of mice as well as the possible mechanisms.
 CIA was induced in mice by immunization with chicken type II collagen
 (II). After boosted on day 21, mice were treated with norisoboldine
 (10, 20, 40 mg/kg) for twenty consecutive days. The clinical scores,
 body weight changes and joint histopathology were evaluated.
 Norisoboldine treatment significantly alleviated the severity of the
 disease, based on the reduced clinical scores and elevated the lowered
 body weights of model mice. Meanwhile, this alkaloid dose-dependently
 reduced the infiltration of inflammatory cells, synovial hyperplasia
 and protected joint from destruction. Additionally, the serum level
 of anti-CII IgG and the CII-stimulated lymphocyte proliferation were
 remarkably decreased in the groups administered with norisoboldine.
 An assessment of Th1 function using the delayed-type hypersensitivity
 model confirmed that norisoboldine also significantly suppressed the
 enhanced T cell responses in vivo. These findings suggest that
 norisoboldine might be a potential therapeutic agent for rheumatoid
 arthritis, and it functions through protecting joint destruction as
 well as regulating the abnormal immune responses. (C) 2010 Elsevier
 GmbH. All rights reserved.
 SN 0944-7113
 PD AUG
 PY 2010
 VL 17
 IS 10
 BP 726
 EP 731
 DI 10.1016/j.phymed.2010.01.013
 UT ISI:000280538900004
 PT J
 AU Liu, P
 Hu, Y
 Guo, DH
 Wang, DX
 Tu, HH
 Ma, L
 Xie, TT
 Kong, LY
 AF Liu, P.
 Hu, Y.
 Guo, D. -H.
 Wang, D. -X.
 Tu, H. -H.
 Ma, L.
 Xie, T. -T.
 Kong, L. -Y.
 TI Potential antidepressant properties of Radix Polygalae (Yuan Zhi)
 SO PHYTOMEDICINE
 AB Radix Polygalae ("Yuan Zhi", the roots of Polygala tenuifolia Willd.,
 YZ) is an important herb used in traditional Chinese medicine to mediate
 depression. The present study was designed to verify the antidepressant
 effects of the standardized YZ ethanol extract (YZE) and its four
 fractions YZ-30, YZ-50, YZ-70 and YZ-90 on the tail suspension (TST)
 and forced swimming test (FST). Furthermore, the standardization of
 the fractions obtained from the separation procedures was carried out
 by high-performance liquid chromatography (HPLC)-fingerprint. The
 YZ-50 fraction (Oligosaccharide esters - enriched, oral (200 mg/kg)
 showed a significant anti-immobility like effects. The data of YZ-50
 on the corticosterone-induced injure of SH-SY5Y human neuroblastoma
 cell indicated that YZ-50 may have biological effects on
 neuroprotection. Proliferation of cell lines was assessed by
 dimethylthiazoldiphenyltetrazoliumbromide (MTT) and
 5-bromo-2'-deoxyuridine (BrdU) incorporation assays. It was found that
 YZ-50 and its two bioactive compounds, 3,6'-di-o-sinapoyl-sucrose
 (DISS) and tenuifoliside A(TEA) showed protection activities in SY5Y
 cells from the lesion. By using bioassay-screening methods, our results
 indicate that the presence of oligosaccharide esters such as DISS and
 TEA in this herb may be responsible for the cytoprotective activity
 effects. (C) 2010 Elsevier GmbH. All rights reserved.
 SN 0944-7113
 PD AUG
 PY 2010
 VL 17
 IS 10
 BP 794
 EP 799
 DI 10.1016/j.phymed.2010.01.004
 UT ISI:000280538900014
 PT J
 AU Wang, XJ
 Yang, QA
 Li, MY
 Yin, DL
 You, QD
 AF Wang, Xiaojian
 Yang, Qian
 Li, Minyong
 Yin, Dali
 You, Qidong
 TI In silico binding characteristics between human histamine H-1 receptor
 and antagonists
 SO JOURNAL OF MOLECULAR MODELING
 AB It is widely acknowledged that the H-1 receptor antagonists have
 important therapeutic significance in the treatment of various
 allergic disorders, but little was known about the binding mode between
 the receptor and antagonists since the crystal structure of G-protein
 coupling receptors (GPCRs) were hard to obtain. In this paper, a
 theoretical three-dimensional model of human histamine H-1 receptor
 (HHR1) was developed on the basis of recently reported high resolution
 structures of human A(2A) adenosine receptor, human
 beta(2)-adrenoceptor and turkey beta(1)-adrenoceptor. Furthermore,
 three representative H-1 receptor antagonists were chosen for docking
 studies. Subsequently, a qualitative pharmacophore model was developed
 by Hiphop algorithm based on the docking conformations of these three
 antagonists. In this paper, active environment, certain key residues,
 and the corresponding pharmacophore features of H-1 receptor were
 identified by such combinations of receptor-based and ligand-based
 approaches, which would give sufficient guidance for the rational
 design of novel antihistamine agents.
 SN 1610-2940
 PD AUG
 PY 2010
 VL 16
 IS 9
 BP 1529
 EP 1537
 DI 10.1007/s00894-010-0666-z
 UT ISI:000280640700010
 PT J
 AU Wang, MY
 Zhao, FM
 Peng, HY
 Lou, CH
 Li, Y
 Ding, X
 Yu, XY
 Yang, GM
 Xu, DQ
 Jiang, LH
 Zhang, X
 Ye, LH
 Cai, BC
 AF Wang, Ming-Yan
 Zhao, Feng-Ming
 Peng, Hai-Yan
 Lou, Cheng-Hua
 Li, Yu
 Ding, Xia
 Yu, Xiao-Yi
 Yang, Guang-Ming
 Xu, Dong-Qing
 Jiang, Li-Hua
 Zhang, Xu
 Ye, Li-Hong
 Cai, Bao-Chang
 TI Investigation on the morphological protective effect of
 5-hydroxymethylfurfural extracted from wine-processed Fructus corni
 on human L02 hepatocytes
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Aim: To determine the mode of action of 5-hydroxymethylfurfural (5-HMF)
 extracted from wine-processed Fructus corni on hepatoprotective
 activities, the effects of 5-HMF on H2O2-induced human L02 hepatocytes
 injury was examined.
 Mthods: Hepatocytes L02 injured by H2O2 was treated by 5-HMF. The
 morphological changes of the cells were observed under inverted
 phase-contrast, fluorescence, and transmission electron microscopy
 and the activities of caspase-9 and caspase-3 were tested by
 enzyme-linked immunosorbent detector.
 Results: It revealed that 5-HMF improved the morphology of H2O2-treated
 human L02 hepatocytes, and also inhibited the level of caspase-9 and
 caspase-3 of them.
 Conclusions: These results suggested a morphological hepatocyte
 protective effect and the anti-apoptosis mechanism by 5-HMF. (C) 2010
 Elsevier Ireland Ltd. All rights reserved.
 SN 0378-8741
 PD JUL 20
 PY 2010
 VL 130
 IS 2
 BP 424
 EP 428
 DI 10.1016/j.jep.2010.05.024
 UT ISI:000280622400033
 PT J
 AU Liu, XY
 Yu, BY
 Wang, NJ
 Zhang, B
 Du, F
 He, C
 Ye, ZG
 AF Liu, Xinyi
 Yu, Boyang
 Wang, Naijie
 Zhang, Bei
 Du, Feng
 He, Cheng
 Ye, Zuguang
 TI A validated stability-indicating HPLC method for the determination of
 PEGylated puerarin in aqueous solutions
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB The aim of this study was to develop a validated specific
 stability-indicating HPLC method for the quantitative determination
 of PEGylated puerarin (PEG-PUE) in aqueous solutions. The method was
 validated by subjecting PEG-PUE to forced degradation under stress
 conditions of acid, alkali, water hydrolysis, and oxidation. Both
 PEG-PUE and puerarin (PUE) were simultaneously determined and
 separated on CAPCELL PAK C18 column by gradient elution with 0.2%
 aqueous phosphoric acid and acetonitrile as the mobile phase. The flow
 rate was 1.0 mL min(-1) and detection wavelength was set at 250 nm.
 Both calibration curves showed good linear regression (r >= 0.9998)
 within test ranges. The LOD and LOQ of PEG-PUE were determined to be
 3 and 9 mu g mL(-1) respectively. Degradation of PEG-PUE followed
 pseudo-first-order kinetics with t(1/2) of 59 min at pH 9.0 and 17.79
 h at pH 7.4. However, at pH 5.0 and 2.0, there was no significant
 degradation of PEG-PUE over time. In conclusion, the method was
 observed to have the necessary specificity, precision, and accuracy,
 and to be suitable for quantity monitoring the degradation process of
 PEG-PUE during stability studies. The degradation studies may give
 insight into useful information for formulation development of
 PEG-PUE. (C) 2010 Elsevier B.V. All rights reserved.
 SN 1570-0232
 PD AUG 1
 PY 2010
 VL 878
 IS 23
 BP 2061
 EP 2066
 DI 10.1016/j.jchromb.2010.06.001
 UT ISI:000280617400003
 PT J
 AU Wu, XA
 Chen, H
 Sun, JG
 Peng, Y
 Liang, Y
 Wang, GJ
 Wu, JZ
 Zhang, P
 AF Wu, Xiao
 Chen, Hui
 Sun, Jianguo
 Peng, Ying
 Liang, Yan
 Wang, Guangji
 Wu, Jizhou
 Zhang, Peng
 TI Development and validation of a liquid chromatography-mass
 spectrometry method for the determination of verticinone in rat plasma
 and its application to pharmacokinetic study
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB We have developed and validated a sensitive liquid
 chromatography-electrospray ionization-mass spectrometric
 (LC-ESI-MS) method for the quantification of verticinone, a major
 active constituent from Fritillaria hupehensis Hsiao et KC Hsia., in
 rat plasma. Verticinone and the internal standard (IS), hupehenine,
 were extracted from plasma samples by a simple liquid-liquid extraction
 with ethyl acetate after being alkalified by 1 M ammonia hydroxide.
 Chromatographic separation was achieved on a C-18 column using a
 gradient elution program with methanol and water as the mobile phase.
 The detection was performed by selected ion monitoring (SIM) mode via
 positive electrospray ionization (ESI) interface. The lower limit of
 quantification (LLOQ) was 0.1 ng/mL. The calibration curves were linear
 (r(2) > 0.998) over the concentration range of 0.1-200 ng/mL. Withinand between-run precision was less than 6.5% and accuracy was within
 +/- 10.7%. The validated method was applied to the pharmacokinetic
 study of verticinone in rats after a single oral administration of 1
 mg/kg. (C) 2010 Elsevier B.V. All rights reserved.
 SN 1570-0232
 PD AUG 1
 PY 2010
 VL 878
 IS 23
 BP 2067
 EP 2071
 DI 10.1016/j.jchromb.2010.06.004
 UT ISI:000280617400004
 PT J
 AU Xu, M
 Dai, DZ
 Zhang, Q
 Cheng, YS
 Dai, Y
 AF Xu, M.
 Dai, D. Z.
 Zhang, Q.
 Cheng, Y. S.
 Dai, Y.
 TI Upregulated NADPH Oxidase Contributes to Diabetic Testicular
 Complication and is Relieved by Strontium Fructose 1,6-Diphosphate
 SO EXPERIMENTAL AND CLINICAL ENDOCRINOLOGY & DIABETES
 AB Diabetes is frequently associated with declining sexual function
 resulting from oxidative damage. NADPH oxidase is a major resource of
 reactive oxygen species (ROS) in the testes and is likely related to
 an activated endothelin-1 (ET-1) system. An activation of NADPH oxidase
 - ET-1 pathway was hypothesized in diabetic testopathy. We verified
 the hypothesis and tested if strontium fructose 1,6-diphosphate
 (FDP-Sr) could relieve these changes in diabetic testis as compared
 to testosterone propionate (TP) and sildenafil. Diabetes was produced
 in male Sprague-Dawley rats 8 weeks after a single injection of
 streptozotocin (STZ), and interventions with testosterone propionate
 (TP), sildenafil and FDP-Sr were conducted in the last 4 weeks. Blood
 glucose, testosterone, follicle stimulating hormone (FSH),
 luteinizing hormone (LH) and expressions of NADPH oxidase subunits and
 the ET system were measured. Decreased insulin, FSH, LH and
 testosterone in serum were found associating with testicular oxidative
 stress in STZ-injected rats. Additionally, over-expressions of NADPH
 oxidase p22, p47, p67 subunits and the ET pathway were significant in
 the diabetic testis relative to normal and were completely abolished
 by FDP-Sr. Both TP and sildenafil were not beneficial to diabetic
 testopathy except serum androgen raised by TP. Activated NADPH oxidase
 and ET system are significant contributing to testis injury and are
 responded to FDP-Sr only, against both TP and sildenafil, by restoring
 the testis function and the hypothalamus-pituitary-testis axis. It is
 due to its extra-energy supply and an antioxidant activity of FDP-Sr.
 SN 0947-7349
 PD JUL
 PY 2010
 VL 118
 IS 7
 BP 459
 EP 465
 DI 10.1055/s-0030-1248325
 UT ISI:000280643300011
 PT J
 AU Liu, HY
 Wu, SM
 Cheng, F
 Hu, YZ
 Yan, ZY
 AF Liu Hai-Yan
 Wu Sheng-Mei
 Cheng Fang
 Hu Yu-Zhu
 Yan Zheng-Yu
 TI Fluorescence Resonance Energy Transfer Between Quantumn Dots
 SO CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
 AB The fluorescent resonance energy transfer(FRET) between two kinds of
 quantum dots(QDs) with different surface-charge was researched.
 Green-emission QDs was modified with amphiphilic surfactants (CTMAB)
 and red-emission QDs was modified with thiolglycolic acid (TGA)
 separately. The experiments proved that both CTMAB and TGA both could
 well turn the oil-soluble QDs into water-soluble ones, as well as
 opposite electric charges on the surface. Then the water-soluble QDs
 were characterized by agarose gel electrophoresis, fluorescence image
 and quantum yield. Taking advantage of the interaction between the
 opposite charges, fluorescent resonance energy transfer(FRET) was
 detected between two kinds of QDs in phosphate buffer solution(pH 7.5)
 with an excitation wavelength of 400 nm, and the FRET efficiencies were
 satisfied (quenching efficiency was 0.54 and enhance efficiency was
 0.27).
 SN 0253-3820
 PD JUL
 PY 2010
 VL 38
 IS 7
 BP 1036
 EP 1039
 DI 10.3724/SP.J.1096.2010.01036
 UT ISI:000280677000025
 PT J
 AU Liu, J
 Li, HX
 Jiang, XQ
 Zhang, C
 Ping, QN
 AF Liu, Jia
 Li, Hongxia
 Jiang, Xiaoqun
 Zhang, Can
 Ping, Qineng
 TI Novel pH-sensitive chitosan-derived micelles loaded with paclitaxel
 SO CARBOHYDRATE POLYMERS
 AB A series of pH-sensitive graft copolymers,
 N-octyl-N-(2-carboxyl-cyclohexamethenyl) chitosan derivatives were
 synthesized and characterized by FTIR, H-1 NMR and elemental analysis,
 and their physical properties were measured with differential scanning
 calorimetry and X-ray diffraction spectrometry. The critical micelle
 concentrations (CMCs) of the modified chitosan determined by using
 pyrene as a hydrophobic probe in fluorescence spectroscopy were from
 11 to 72 mu g/ml. The graft polymers can form micelles solubilizing
 paclitaxel, with drug-loading rate ranging from 30.47% to 48.10% and
 entrapment efficiency from 42.22% to 59.24%. Cytotoxicities of carrier
 against tumor cells estimated that carriers were nearly non-cytotoxic.
 Additionally, the results of pH-sensitivity and drug release
 experiments showed that the micelles were highly sensitive to mild
 acidic conditions (pH 5.5) while reasonably stable at physiological
 conditions (pH 7.4). Therefore, chitosan-derived micelle may be a
 potential anti-tumor drug delivery system for chemotherapy of cancer.
 (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0144-8617
 PD SEP 5
 PY 2010
 VL 82
 IS 2
 BP 432
 EP 439
 DI 10.1016/j.carbpol.2010.04.084
 UT ISI:000280574600030
 PT J
 AU Wu, QA
 Yuan, QA
 Liu, EH
 Qi, LW
 Bi, ZM
 Li, P
 AF Wu, Qian
 Yuan, Quan
 Liu, E-Hu
 Qi, Lian-Wen
 Bi, Zhi-Ming
 Li, Ping
 TI Fragmentation study of iridoid glycosides and phenylpropanoid
 glycosides in Radix Scrophulariae by rapid resolution liquid
 chromatography with diode-array detection and electrospray ionization
 time-of-flight mass spectrometry
 SO BIOMEDICAL CHROMATOGRAPHY
 AB Rapid resolution liquid chromatography (RRLC) coupled with diode array
 detection (DAD) and electrospray ionization time-of-flight mass
 spectrometry (ESI-TOF MS) method was applied to the mass spectral study
 of a series of naturally occurring iridoid glycosides and
 phenylpropanoid glycosides in Radix Scrophulariae, which provides
 higher speed and increased sensitivity without loss of resolution. With
 dynamic adjustment as the key role of the fragmentor voltage and
 confirmed with authentic standards, valuable structural information
 regarding the nature of both the glycoside skeletons was thus obtained.
 Most compositions were found to possess organic acid moiety such as
 cinnamoyl, caffeoyl and ferulyol. Besides extensive fragmentation of
 the carbohydrate moiety, losses of the hydroxyl and glucose residue
 units showed in the spectra, permitting the exploration of the skeleton
 and the identity of substituents in the molecule. Ten major iridoid
 glycosides and 10 phenylpropanoid glycosides were identified or
 tentatively characterized based on their retention times, UV and TOF
 MS data. The major fragmentation pathways of PGs in Radix Scrophulariae
 obtained through the MS data was schemed systematically for the first
 time, which provides a reference for other PGs derivatives. Copyright
 (C) 2009 John Wiley & Sons, Ltd.
 SN 0269-3879
 PD AUG
 PY 2010
 VL 24
 IS 8
 BP 808
 EP 819
 DI 10.1002/bmc.1368
 UT ISI:000280542700002
 PT J
 AU Aa, JY
 Wang, GJ
 Hao, HP
 Huang, Q
 Lu, YH
 Yan, B
 Zha, WB
 Liu, LS
 Kang, A
 AF Aa, Ji-ye
 Wang, Guang-ji
 Hao, Hai-ping
 Huang, Qing
 Lu, Yi-hong
 Yan, Bei
 Zha, Wei-bin
 Liu, Lin-sheng
 Kang, An
 TI Differential regulations of blood pressure and perturbed metabolism
 by total ginsenosides and conventional antihypertensive agents in
 spontaneously hypertensive rats
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To investigate the regulatory effects of total ginsenosides and
 the conventional antihypertensive agents (captopril, amlodipine,
 terazosin and hydrochlorothiazide) on the blood pressure and perturbed
 metabolism in spontaneously hypertensive rats (SHRs) and to analyze
 the cause-effect relationships between high blood pressure and the
 metabolic disorders of hypertension.
 Methods: SHRs were administrated with total ginsenosides or the
 antihypertensive agents for eight weeks. Systolic blood pressure (SP)
 was measured every week and low-molecular-weight compounds in blood
 plasma were quantitatively analyzed using a nontargeted
 high-throughput metabolomic tool: gas chromatography/time of flight
 mass spectrometry (GC/TOFMS). The metabolic patterns were evaluated
 using principal components analysis and potential markers of
 hypertension were identified.
 Results: Total ginsenosides and the antihypertensive agents
 differentially regulated SP and the metabolic pattern in SHRs. Total
 ginsenosides caused a progressive and prolonged reduction of SP and
 markedly normalized the perturbed metabolism with 14 of 27 (51.8%)
 markers of hypertension which were regulated toward normal. Total
 ginsenosides also reduced free fatty acids' level toward normal levels.
 In contrast, captopril, amlodipine and terazosin efficiently depressed
 SP, but had little effect on metabolic perturbation with only 8 (29.6%),
 4 (14.8%), and 4 (14.8%) markers, respectively, which were regulated.
 Conclusion: The metabolic changes persisted when the blood pressure
 was lowered by the conventional antihypertensive agents, suggesting
 that hypertension may not be the cause of the metabolic perturbation
 in SHRs.
 SN 1671-4083
 PD AUG
 PY 2010
 VL 31
 IS 8
 BP 930
 EP 937
 DI 10.1038/aps.2010.86
 UT ISI:000280617100006
 PT J
 AU Wang, J
 Liu, JH
 Guo, X
 Zhang, JA
 Yu, BY
 AF Wang, Jing
 Liu, Ji-hua
 Guo, Xu
 Zhang, Jian
 Yu, Bo-yang
 TI A sensitive indirect competitive enzyme-linked immunosorbent assay for
 the detection of sarsasapogenin in rat plasma
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To generate a polyclonal antibody against sarsasapogenin and to
 develop an indirect competitive enzyme-linked immunosorbent assay
 (IC-ELISA) method for the pharmacokinetic study of Sarsasapogenin in
 rats.
 Methods: The antigen of sarsasapogenin was produced using an active
 ester method and subsequently used for raising polyclonal antibodies
 in rabbits. The specificity and sensitivity of the antibody were
 measured by IC-ELISA. Using the ELISA method, sarsasapogenin levels
 were measured in the serum of rats after an oral dose of 100 mg/kg.
 Results: Polyclonal antibodies raised against sarsasapogenin-bovine
 serum albumin were generated and showed a high reactivity to
 sarsasapogenin. The antibodies exhibited minor cross-reactivity to
 ruscogenin (23%), diosgenin (22%), 25 (R, S) ruscogenin
 I-O-[beta-D-glucopyranosyl (1-->2)][beta-D-xylopyranosyl
 (1-->3)]-beta-D-fucopyranoside (26%) and no cross-reactivity to
 diammonium glycyrrhizinate and notoginseng R1. The detection range of
 sarsasapogenin by this ELISA method was approximately 2.4-760 ng/mL.
 The recovery rates of 10 ng/mL, 100 ng/mL, and 500 ng/mL were in the
 range of 91.0%-96.2% for intra-assay and 89.0%-92.0% for inter-assay.
 The coefficients of variation (CV%) for intra-and inter-assays at the
 three different sarsasapogenin levels were 3.1%-8.3% (n=6) and
 6.0%-14.1% (n=6), respectively.
 Conclusion: The IC-ELISA method is a sensitive test for the
 determination of sarsasapogenin concentration in rat plasma and for
 pharmacokinetic (PK) studies.
 SN 1671-4083
 PD AUG
 PY 2010
 VL 31
 IS 8
 BP 984
 EP 989
 DI 10.1038/aps.2010.85
 UT ISI:000280617100013
 PT J
 AU Han, S
 Shen, JQ
 Gan, Y
 Geng, HM
 Zhang, XX
 Zhu, CL
 Gan, L
 AF Han, Shun
 Shen, Jin-qiu
 Gan, Yong
 Geng, Hai-ming
 Zhang, Xin-xin
 Zhu, Chun-liu
 Gan, Li
 TI Novel vehicle based on cubosomes for ophthalmic delivery of
 flurbiprofen with low irritancy and high bioavailability
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To develop a novel vehicle based on cubosomes as an ophthalmic
 drug delivery system for flurbiprofen (FB) to reduce ocular irritancy
 and improve bioavailability.
 Methods: FB-loaded cubosomes were prepared using hot and high-pressure
 homogenization. Cubosomes were then characterized by particle size,
 zeta potential, encapsulation efficiency, particle morphology, inner
 cubic structure and in vitro release. Corneal permeation was evaluated
 using modified Franz-type cells. Ocular irritation was then evaluated
 using both the Draize method and histological examination. The ocular
 pharmacokinetics of FB was determined using microdialysis.
 Results: The particle size of each cubosome formulation was about 150
 nm. A bicontinuous cubic phase of cubic P-type was determined using
 cryo-transmission electron microscopy (cryo-TEM) observation and
 small angle X-ray scattering (SAXS) analysis. In vitro corneal
 permeation study revealed that FB formulated in cubosomes exhibited
 2.5-fold (F1) and 2.0-fold (F2) increase in P-app compared with FB PBS.
 In the ocular irritation test, irritation scores for each group were
 less than 2, indicating that all formulations exhibited excellent
 ocular tolerance. Histological examination revealed that neither the
 structure nor the integrity of the cornea was visibly affected after
 incubation with FB cubosomes. The AUC of FB administered as FB cubosome
 F2 was 486.36+/-38.93 ng.mL(-1).min.mu g(-1), which was significantly
 higher than that of FB Na eye drops (P<0.01). Compared with FB Na eye
 drops, the T-max of FB cubosome F2 was about 1.6-fold higher and the
 MRT was also significantly longer (P<0.001).
 Conclusion: This novel low-irritant vehicle based on cubosomes might
 be a promising system for effective ocular drug delivery.
 SN 1671-4083
 PD AUG
 PY 2010
 VL 31
 IS 8
 BP 990
 EP 998
 DI 10.1038/aps.2010.98
 UT ISI:000280617100014
 PT J
 AU Angeli, V
 Chen, HL
 Mester, Z
 Rao, YL
 D'Ulivo, A
 Bramanti, E
 AF Angeli, Valeria
 Chen, Huilun
 Mester, Zoltan
 Rao, Yulan
 D'Ulivo, Alessandro
 Bramanti, Emilia
 TI Derivatization of GSSG by pHMB in alkaline media. Determination of
 oxidized glutathione in blood
 SO TALANTA
 AB Chromatographic determination of glutathione disulfide (GSSG) without
 any preliminary reduction has been presented using GSSG derivatization
 by p-hydroxymercuribenzoate (pHMB) in strong alkaline medium followed
 by the determination of GS-pHMB complex by reversed phase
 chromatography coupled to chemical vapour generation and atomic
 fluorescence detector (RPC-CVGAFS). A detection limit of 35 nM for GSSG
 (corresponding to 1.8 pmol) detected as GS-pHMB species was achieved
 based on a signal-to-noise ratio of 3 in buffer and in blood. The
 proposed method was applied to the determination of GSSG in whole blood
 and validated by the classical determination of GSSG by derivatization
 after reduction with dithiothreitol (DTT). (C) 2010 Elsevier B.V. All
 rights reserved.
 SN 0039-9140
 PD JUL 15
 PY 2010
 VL 82
 IS 2
 BP 815
 EP 820
 DI 10.1016/j.talanta.2010.05.065
 UT ISI:000280375700059
 PT J
 AU Qi, J
 Xu, DR
 Zhou, YF
 Qin, MJ
 Yu, BY
 AF Qi, Jin
 Xu, Deran
 Zhou, Yi-Feng
 Qin, Min-Jian
 Yu, Bo-Yang
 TI New features on the fragmentation patterns of homoisoflavonoids in
 Ophiopogon japonicus by high-performance liquid
 chromatography/diode-array detection/electrospray ionization with
 multi-stage tandem mass spectrometry
 SO RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 AB Homoisoflavonoids, a special class of flavonoids, are mainly
 distributed in the Liliaceae family and have various biological
 activities. Previously, very little research has been reported on the
 gas-phase fragmentation patterns of homoisoflavonoids by electrospray
 ionization mass spectrometry. In this paper, we report the use of
 high-performance liquid chromatography with a diode-array detector
 (HPLC-DAD) and electrospray ionization multi-stage tandem mass
 spectrometry (ESI-MSn) to study the fragmentation behavior of 11
 homoisoflavonoid standards and to analyze homoisoflavonoids in
 Ophiopogon japonicus. In total, 28 homoisoflavonoids (including seven
 novel constituents) were characterized. The deprotonated [M-H](-)
 molecules of the homoisoflavonoids containing a saturated C2-C3 bond
 afforded the A or B product ion (base peak) according to whether the
 B-ring was substituted with a hydroxyl group. For the homoisoflavonoids
 containing a C-2-C-3 double bond, the product ions (A or C ion) were
 created from the precursor [M-H](-) ion as the base peak when the B-ring
 was substituted with a hydroxyl group. The homoisoflavonoids carrying
 a formyl group in the A-ring readily eliminated one molecule of CO to
 form the product ion [M+H-CO](-) (base peak) irrespective whether the
 C-2-C-3 bond was saturated or not. This product ion afforded the
 [M-H-CO-B-ring-CH2+H](-) ion by cleavage of the C3-C9 bond. This latter
 product ion always appeared in tandem mass (MS/MS) spectra of type I
 homoisoflavonoids. The common features of flavonoids observed during
 the gas-phase fragmentation mechanisms were the loss of the following
 groups: 15 Da (CH3), 18 Da (H2O), 28 Da (CO), 44 Da (CO2) and 46 Da
 (CH2O2). A retro-Diels-Alder (RDA)-like cleavage was also observed for
 the homoisoflavonoids. The different gas-phase fragmentation routes
 were characterized for the deprotonated molecules obtained from the
 various homoisoflavonoids and collision-induced dissociation (CID)
 fragmentation differences were noted for the different locations of
 the various substituents. In conclusion, we can say that this study
 allowed us to structurally elucidate and identify homoisoflavonoids
 distributed in related plants and their complex prescriptions.
 Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0951-4198
 PD AUG
 PY 2010
 VL 24
 IS 15
 BP 2193
 EP 2206
 DI 10.1002/rcm.4608
 UT ISI:000280495700003
 PT J
 AU Zhou, CH
 Xiang, M
 He, SY
 Qian, ZY
 AF Zhou, Cheng-Hua
 Xiang, Min
 He, Shu-Ying
 Qian, Zhi-Yu
 TI Crocetin Inhibits Cell Cycle G(1)/S Transition through Suppressing
 Cyclin D1 and Elevating p27(kip1) in Vascular Smooth Muscle Cells
 SO PHYTOTHERAPY RESEARCH
 AB Crocetin is a natural carotenoid compound isolated from Gardenia
 jasminoids Ellis. Our previous study shows that crocetin inhibits
 angiotensin II (Ang II)-induced vascular smooth muscle cells (VSMCs)
 proliferation. To further explore the mechanism by which crocetin
 inhibits VSMCs proliferation, in the present study we examined the
 effect of crocetin on cell cycle progression and cell cycle regulatory
 proteins. Flow cytometry analysis showed that Ang II elicited
 significant increase in the percentage of VSMCs in the S phase, with
 a concomitant decline in the percentage of VSMCs in the G(0)/G(1) phase.
 However, on pretreatment of VSMCs with crocetin, the percentage of
 VSMCs in the S phase decreased, while that in the G(0)/G(1) phase
 increased significantly. In addition, Ang II-induced increase of cell
 proliferation index was also decreased by crocetin. Western blotting
 analysis indicated that crocetin markedly inhibited the protein
 expression of cyclin D1 but not cyclin E. Crocetin also increased the
 level of cyclin-dependent kinase inhibitor (CDKI) p27(kip1) but not
 CDKI p27(waf1/cip1). In conclusion, our present results suggest that
 the inhibition of cell cycle G(1)/S transition in VSMCs by crocetin
 can be attributed, at least in part, to its suppression of cyclin D1
 and elevation of CDKI p27(kip1). Copyright (C) 2009 John Wiley & Sons,
 Ltd.
 SN 0951-418X
 PD JUL
 PY 2010
 VL 24
 IS 7
 BP 975
 EP 981
 DI 10.1002/ptr.3039
 UT ISI:000280142900004
 PT J
 AU Wang, YQ
 Ye, C
 Wu, LH
 Hu, YZ
 AF Wang, Yunqing
 Ye, Chao
 Wu, Liheng
 Hu, Yuzhu
 TI Synthesis and characterization of self-assembled CdHgTe/gelatin
 nanospheres as stable near infrared fluorescent probes in vivo
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 CT 21st International Symposium on Pharmaceutical and Biomedical Analysis
 CY OCT 11-14, 2009
 CL Orlando, FL
 AB This work presented a kind of novel near infrared emitting
 CdHgTe/gelatin nanospheres which were synthesized with Cd(NO3)(2),
 Hg(NO3)(2). NaHTe and a thiol stabilizer in gelatin solution The
 self-assembled nanospheres were megranate-like and nearly 40 nm in
 diameter, with CdHgTe QDs uniformly embedded in gelatin matrix. They
 exhibited strong fluorescence ranging from 580 to 800 nm that could
 be tuned by molar ratios of Hg2+ and gelatin. The full widths at
 half-maximum of the emission spectra were in the range of 60-80 nm.
 Compared with bare CdHgTe QDs, the photostability of this compact
 complex nanostructure remarkably improved. Moreover, the fluorescence
 of CdHgTe/gelatin nanospheres was much more resistant to the
 interference from certain kinds of endogenous biomolecules such as HSA,
 transferrin and hemoglobin Further applications of living cells and
 mouse imaging were demonstrated with an in vivo near infrared
 fluorescence imaging system The Inherent advantages of high stability
 as well as high fluorescence intensity make the nanospheres particular
 interested NIR bioprobe candidates for in vivo imaging studies (C) 2010
 Elsevier B.V. All rights reserved
 SN 0731-7085
 PD NOV 2
 PY 2010
 VL 53
 IS 3
 BP 235
 EP 242
 DI 10.1016/j.jpba.2010.02.028
 UT ISI:000280435800003
 PT J
 AU Li, NG
 Shi, ZH
 Tang, YP
 Ma, HY
 Yang, JP
 Li, BQ
 Wang, ZJ
 Song, SL
 Duan, JA
 AF Li, Nian-Guang
 Shi, Zhi-Hao
 Tang, Yu-Ping
 Ma, Hong-Yue
 Yang, Jian-Ping
 Li, Bao-Quan
 Wang, Zhen-Jiang
 Song, Shu-Lin
 Duan, Jin-Ao
 TI Synthetic Strategies in the Construction of Chromones
 SO JOURNAL OF HETEROCYCLIC CHEMISTRY
 AB Because of important biological applications of chromones, some
 synthetic strategies leading to more complex derivatives have been
 widely explored in the past years. Thus, the purpose of this review
 is to report some recent improvements of the classical synthetic
 methods and of some nonclassical methods to obtain simple oxygenated
 chromones. The strategies for synthesis of heterocycle analogs
 containing phosphorus, nitrogen, and sulfur are also summarized.
 SN 0022-152X
 PD JUL
 PY 2010
 VL 47
 IS 4
 BP 785
 EP 799
 DI 10.1002/jhet.393
 UT ISI:000280450700003
 PT J
 AU Liu, Y
 Zhou, JL
 Liu, P
 Sun, S
 Li, P
 AF Liu, Ying
 Zhou, Jian-Liang
 Liu, Peng
 Sun, Shi
 Li, Ping
 TI Chemical markers' fishing and knockout for holistic activity and
 interaction evaluation of the components in herbal medicines
 SO JOURNAL OF CHROMATOGRAPHY A
 AB A strategy based on chemical markers' fishing and knockout has been
 proposed for holistic activity and interaction evaluation of the
 bioactive components in herbal medicines (HMs). It was devised to
 screen bioactive-compound group that represents the efficacy of HM,
 estimate the bioactivity contribution of each component and elucidate
 the interactions of multi-components. This strategy was accomplished
 through the following steps: (1) screen out the chemical markers
 (target peaks) in a HM fingerprint using online two-dimensional
 turbulent flow chromatography/liquid chromatography-mass
 spectrometry technique, (2) fish target peaks and knockout any
 interested peak, and (3) evaluate the bioactivities of fishing and
 knockout portions. After comparison of the bioactivities of samples
 containing different target peaks, the efficacy of target-peak group,
 bioactivity contribution of each compound, and the interactions of
 multi-components are elucidated. Using Acetylcholinesterase (AChE)
 and Bulbs of Lycoris radiata (L. Herit.) Herb. (BLR) as the experimental
 materials, four target peaks were screened out as the AChE binders.
 By target peaks' fishing and knockout, combined with activity
 evaluation, we observed that the bioactivity of the four-peak mixture
 is similar with the global bioactivity of BLR extract, and there are
 significant suppressive actions among these four target peaks. These
 results indicate that this proposed strategy is a useful approach for
 holistic screening of bioactive-compound group and elucidation of the
 multi-component interactions in HM. (C) 2010 Elsevier B.V. All rights
 reserved.
 SN 0021-9673
 PD AUG 6
 PY 2010
 VL 1217
 IS 32
 BP 5239
 EP 5245
 DI 10.1016/j.chroma.2010.06.039
 UT ISI:000280497300014
 PT B
 AU Sen, Z
 AF Sen, Zhou
 ED Jiang, Y; Cheng, G
 TI Internal stabilizability for a reaction-diffusion system
 SO PROCEEDINGS OF THE 2010 INTERNATIONAL CONFERENCE ON APPLICATION OF
 MATHEMATICS AND PHYSICS, VOL 2 - ADVANCES ON APPLIED MATHEMATICS AND
 COMPUTATION MATHEMATICS
 CT International Conference on Application of Mathematics and Physics
 (AMP2010)
 CY MAY 08-09, 2010
 CL Nanjing, PEOPLES R CHINA
 AB This paper is concerned with the problem of internal stabilizability
 for a 2 x 2 reaction-diffusion system describing interactions between
 a prey population and a predator population. We obtain some results
 of internal zero stabilizability of the predator population.
 BN 978-1-84626-082-7
 PY 2010
 BP 133
 EP 137
 UT ISI:000280135200030
 PT J
 AU Wang, QO
 Hao, HP
 Zhu, XX
 Yu, G
 Lai, L
 Liu, YT
 Wang, YX
 Jiang, S
 Wang, GJ
 AF Wang, Qiong
 Hao, Haiping
 Zhu, Xuanxuan
 Yu, Guo
 Lai, Li
 Liu, Yitong
 Wang, Yuxin
 Jiang, Shan
 Wang, Guangji
 TI Regioselective Glucuronidation of Tanshinone IIa after Quinone
 Reduction: Identification of Human UDP-Glucuronosyltransferases,
 Species Differences, and Interaction Potential
 SO DRUG METABOLISM AND DISPOSITION
 AB We have previously identified that the predominant metabolic pathway
 for tanshinone IIa (TSA) in rat is the NAD(P)H:quinone oxidoreductase
 1 (NQO1)-mediated quinone reduction and subsequent glucuronidation.
 The present study contributes to further research on its
 glucuronidation enzyme kinetics, the identification of human
 UDP-glucuronosyltransferase (UGT) isoforms, and the interaction
 potential with typical UGT substrates. A pair of regioisomers (M1 and
 M2) of reduced TSA glucuronides was found from human, rat, and mouse,
 whereas only M1 was found in dog liver S9 incubations. The overall
 glucuronidation clearance of TSA in human liver S9 was 11.8 +/- 0.8
 mu l/min/mg protein, 0.7-, 0.8-, and 3-fold of that in the mouse, rat,
 and dog, respectively. Using intrinsic clearance M2/M1 as a
 regioselective index, opposite regioselectivity was found between
 human (0.7) and mouse (1.3), whereas no significant regioselectivity
 was found in rat. In a sequential metabolism system, by applying human
 liver cytosol as an NQO1 donor combined with a screening panel of 12
 recombinant human UGTs, multiple UGTs were found involved in the M1
 formation, whereas only UGT1A9 and, to a very minor extent, UGT1A1 and
 UGT1A3 contributed to the M2 formation. Further enzyme kinetics,
 correlation, and chemical inhibition studies confirmed that UGT1A9
 played a major role in both M1 and M2 formation. In addition, TSA
 presented a potent inhibitory effect on the glucuronidation of typical
 UGT1A9 substrates propofol and mycophenolic acid, with an IC50 value
 of 8.4 +/- 1.8 and 8.9 +/- 1.9 mu M, respectively. This study will help
 to guide future studies on characterizing the NQO1-mediated reduction
 and subsequent glucuronidation of other quinones.
 SN 0090-9556
 PD JUL
 PY 2010
 VL 38
 IS 7
 BP 1132
 EP 1140
 DI 10.1124/dmd.109.031864
 UT ISI:000280382100016
 PT J
 AU Chen, YJ
 AF Chen, Yijun
 TI Hot topic: Biotransformation in Drug Discovery and Development
 SO CURRENT ORGANIC CHEMISTRY
 SN 1385-2728
 PD AUG
 PY 2010
 VL 14
 IS 14
 BP 1399
 EP 1399
 UT ISI:000280474000001
 PT J
 AU Liu, JH
 Yu, BY
 AF Liu, Ji-Hua
 Yu, Bo-Yang
 TI Biotransformation of Bioactive Natural Products for Pharmaceutical
 Lead Compounds
 SO CURRENT ORGANIC CHEMISTRY
 AB Biotransfomation has been increasingly utilized as a tool to generate
 pharmaceutical lead compounds from natural products in recent years.
 A wide variety of natural pruducts including aromatics, steroids,
 alkaloids, coumarins, flavonoids and terpenoids can be biotransformed
 by fungi, yeasts, bacteria, plant cells and enzymes derived from these
 sources. The biochemical reactions occurring in microorganisms and
 plant cells are typically regio- and stereo-selective, which is
 difficult to be achieved by chemical methods. In this review we describe
 important biotransformations used for the generation of lead compounds
 with pharmaceutical utilities and further structural diversification
 of complex natural products, especially those from traditional Chinese
 medicines. Such approach will ultimately benefit the advancement of
 biotransformation and potential therapeutics.
 SN 1385-2728
 PD AUG
 PY 2010
 VL 14
 IS 14
 BP 1400
 EP 1406
 UT ISI:000280474000002
 PT J
 AU Wei, MC
 Wang, SZ
 Shang, GD
 AF Wei, Maochen
 Wang, Shuzhen
 Shang, Guangdong
 TI Biosynthetic Pathways and Engineering for Bioactive Natural Products
 SO CURRENT ORGANIC CHEMISTRY
 AB Natural products synthesized by polyketide synthase (PKS),
 non-ribosomal peptide synthetase (NRPS) and the hybrid PKS-NRPS have
 been valuable sources for bioactive compounds due to their structural
 diversity and wide variety of biological activities. Progresses in the
 biosynthetic study of natural products in recent years reinvigorate
 the hope of discovering new compounds for clinical use. This review
 focuses on the elucidation of biosynthetic pathways of PKS and NRPS,
 the more "abnormal" biosynthetic reactions, the manipulation of gene
 cluster to increase product yields, as well as the catalytic
 applications of the enzymes originated from secondary metabolism.
 Genome mining or key regulatory gene activation to obtain "silent" gene
 cluster and the progresses on using sequencing data to predict the
 generation of natural products are also summarized.
 SN 1385-2728
 PD AUG
 PY 2010
 VL 14
 IS 14
 BP 1433
 EP 1446
 UT ISI:000280474000005
 PT J
 AU Huang, Y
 Liu, N
 Wu, XR
 Chen, YJ
 AF Huang, Yan
 Liu, Nan
 Wu, Xuri
 Chen, Yijun
 TI Dehydrogenases/Reductases for the Synthesis of Chiral Pharmaceutical
 Intermediates
 SO CURRENT ORGANIC CHEMISTRY
 AB The increasing trend of chiral drugs in the pharmaceutical industry
 has promoted greatly on the development of numerous biocatalytic routes
 in combination with chemical methods. Because the resulting chiral
 alcohols are particularly valuable intermediates and precursors for
 the synthesis of chiral drugs, dehydrogenases and reductases have been
 extensively used in the synthesis of chiral compounds from ketone
 substrates with high regio- and stereo-selectivities. In this review,
 biocatalytic processes carried out by dehydrogenases and reductases
 are described for the synthesis of chiral intermediates for a wide
 variety of pharmaceuticals, including antidepressants,
 anti-anxieties, anti-asthmatics, anti-hypertensives,
 cholesterol-lowering agents, NK1 antagonists, ACE inhibitors and
 beta-Lactamase inhibitors.
 SN 1385-2728
 PD AUG
 PY 2010
 VL 14
 IS 14
 BP 1447
 EP 1460
 UT ISI:000280474000006
 PT J
 AU Zhang, HJ
 He, H
 Lu, YN
 Gu, Y
 Chuong, PH
 AF Zhang Huaijing
 He Hua
 Lue Yanni
 Gu Yan
 Chuong, Pham-huy
 TI EFFECTS OF PAMAM DENDRIMERS ON THE SOLUBILITY OF KETOPROFEN
 SO ACTA POLYMERICA SINICA
 AB The aim of this study was to study the effect of polyamidoamine (PAMAM)
 dendrimers on the aqueous solubility of ketoprofen and investigate the
 mechanism of solubilization. PAMAM dendrimers of G1. 0, Gl. 5, G2. 0,
 G2. 5, G3. 0 and G3. 5 were used as drug carriers of ketoprofen. The
 effects of pH and concentration of the dendrimers on the solubility
 of ketoprofen were studied by UV spectroscopy. In addition, the
 computational simulation was used to investigate the mechanism of
 interaction between PAMAM dendrimers and ketoprofen. Results showed
 that the pH, generation size, and concentration influenced the
 solubilization of ketoprofen. The solubility of ketoprofen increased
 with the increase of pH, generation size, and concentration of PAMAM
 dendrimers at pH 4.0 similar to 6.0. Both amino and ester terminated
 dendrimers caused the increase in ketoprofen solubility. However, at
 each pH, the solubility of ketoprofen was greater in the presence of
 amino-terminated dendrimers compared to the ester-terminated
 dendrimers possessing the same number of surface functional groups.
 The results of computational simulation show that interaction between
 ketoprofen and PAMAM dendrimers is mainly electrostatic force. Its
 mechanism of solubilization maybe an electrostatic interaction between
 the carboxyl group of ketoprofen and the primary amines or tertiary
 amines of PAMAM dendrimers.
 SN 1000-3304
 PD JUL 20
 PY 2010
 IS 7
 BP 876
 EP 883
 UT ISI:000280431100011
 PT J
 AU Wu, JJ
 Cheng, KW
 Zuo, XF
 Wang, MF
 Li, P
 Zhang, LY
 Wang, H
 Ye, WC
 AF Wu, Jia-Jun
 Cheng, Ka-Wing
 Zuo, Xiao-Feng
 Wang, Ming-Fu
 Li, Ping
 Zhang, Lu-Yong
 Wang, Hao
 Ye, Wen-Cai
 TI Steroidal saponins and ecdysterone from Asparagus filicinus and their
 cytotoxic activities
 SO STEROIDS
 AB Two new spirostanoides, filiasparosides E (1) and F (2), one new
 furostanoside, filiasparoside G (3), and one new ecdysterone,
 stachysterone A-20, 22-acetonide (4), together with six known
 steroidal saponins, asparagusin A (5), filiasparoside A (6),
 filiasparoside B (7), aspafilioside A (8), aspafilioside B (9), and
 filiasparoside C (10) were isolated from the roots of Asparagus
 filicinus Buch.-Ham. Their structures were elucidated on the basis of
 spectroscopic and chemical evidence. Compounds 1-10 were investigated
 for their cytotoxicities against human breast adenocarcinoma
 MDA-MB-231 cell line and compounds 8-10 exhibited cytotoxic activities
 with IC50 values ranging from 3.4 to 6.6 mu M. (C)2010 Elsevier Inc.
 All rights reserved.
 SN 0039-128X
 PD OCT
 PY 2010
 VL 75
 IS 10
 BP 734
 EP 739
 DI 10.1016/j.steroids.2010.05.002
 UT ISI:000280046700016
 PT J
 AU Cao, YA
 Chen, JJ
 Tan, NH
 Wu, YP
 Yang, J
 Wang, QA
 AF Cao, Yuan
 Chen, Ji-Jun
 Tan, Ning-Hua
 Wu, Yong-Ping
 Yang, Jie
 Wang, Qiang
 TI Structure determination of selaginellins G and H from Selaginella
 pulvinata by NMR spectroscopy
 SO MAGNETIC RESONANCE IN CHEMISTRY
 AB Selaginellins G (1) and H (2), two new selaginellin derivatives, were
 isolated from the whole plant of Selaginella pulvinata. Their
 structures were elucidated, and complete assignments of the H-1 and
 C-13 NMR spectroscopic data were achieved by 1D and 2D NMR experiments
 (HSQC, HMBC, COSY and ROESY). Compound 1 displayed good antifungal
 activity against Candida albicans with an IC50 value of 5.3 mu g/ml.
 Copyright (C) 2010 John Wiley & Sons, Ltd.
 SN 0749-1581
 PD AUG
 PY 2010
 VL 48
 IS 8
 BP 656
 EP 659
 DI 10.1002/mrc.2623
 UT ISI:000280218800012
 PT J
 AU Liang, Y
 Hao, HP
 Kang, A
 Xie, L
 Xie, T
 Zheng, XA
 Dai, C
 Wan, LR
 Sheng, LS
 Wang, GJ
 AF Liang, Yan
 Hao, Haiping
 Kang, An
 Xie, Lin
 Xie, Tong
 Zheng, Xiao
 Dai, Chen
 Wan, Leren
 Sheng, Longsheng
 Wang, Guangji
 TI Qualitative and quantitative determination of complicated herbal
 components by liquid chromatography hybrid ion trap time-of-flight
 mass spectrometry and a relative exposure approach to herbal
 pharmacokinetics independent of standards
 SO JOURNAL OF CHROMATOGRAPHY A
 AB To date, the pharmacokinetic research of herbal medicines (HMs) is
 still in its infancy and is facing critical technical challenges on
 the qualitative and quantitative analysis of complicated components
 from biological matrices. Additionally, the lack of authentic
 standards constitutes another bottleneck on assessing herbal
 pharmacokinetics. This present work contributes to the development of
 a powerful technical platform for both qualitative and quantitative
 pharmacokinetic analysis of herbal components, and a strategy of
 relative exposure that provides a practicable pharmacokinetic
 assessment independent of authentic standards, based on the use of
 liquid chromatography hybrid ion trap time-of-flight mass spectrometry
 (LC-IT-TOF/MS). Taking schisandra lignans extract (SLE) as an example,
 the LC-IT-TOF/MS assay was initially applied to the global qualitative
 analysis of components contained in SLE per se and in the rat plasma
 post SLE dosing. Afterwards, this study focused on validating the
 quantitative performance of LC-IT-TOF/MS assay by comparison with a
 well-established LC-Q/MS assay. For the absolute quantification of
 five lignans components with authentic standards, both assays showed
 very similar analytical figures of merit such as linearity, precision,
 accuracy, and pharmacokinetic parameters. Compared with LC-Q/MS, the
 prominent advantage of LC-IT-TOF/MS assay is its much higher
 sensitivity. Moreover, a 'relative exposure approach' (REA) that
 entails the use of sequentially diluted original herbal preparations
 to prepare the 'mixed calibration curves' was developed to assessing
 herbal pharmacokinetics independent of specific authentic compounds
 for each component. Such an approach was found capable of providing
 virtually identical pharmacokinetic parameters as that from the
 typical pharmacokinetic assay calibrated by authentic standards,
 except for the absolute plasma concentrations. The presently developed
 methodology and approach will find its wide use in, but not limited
 to, the qualitative and quantitative pharmacokinetic analysis of
 herbal medicines. (C) 2010 Elsevier By. All rights reserved.
 SN 0021-9673
 PD JUL 23
 PY 2010
 VL 1217
 IS 30
 BP 4971
 EP 4979
 DI 10.1016/j.chroma.2010.05.056
 UT ISI:000280019300012
 PT J
 AU Zhou, XW
 Li, Y
 Jiang, XQ
 Qiu, L
 Liu, JP
 AF Zhou, Xiaowen
 Li, Ying
 Jiang, Xiaoqun
 Qiu, Lu
 Liu, Jianping
 TI Release of copper and indomethacin from intrauterine devices immersed
 in simulated uterine fluid
 SO EUROPEAN JOURNAL OF CONTRACEPTION AND REPRODUCTIVE HEALTH CARE
 AB Objectives To study the release of cupric ions and indomethacin from
 copper-bearing intrauterine devices (Cu-IUDs) and to assess the
 influence of their surface area of copper and the pH of the test medium
 on the release of cupric ions.
 Methods Cu-IUDs were incubated in simulated uterine fluid (SUF). The
 in vitro release of cupric ions and indomethacin was determined by means
 of a flame atomic absorption spectrometer and a UV752
 spectrophotometer, respectively, over a period of 220 days. The effect
 of indomethacin on the pH of the SUF was monitored during the cupric
 ions release study.
 Results The Cu-IUDs released cupric ions in vitro according to a
 biphasic pattern. After an initial burst release, the rate slowed down
 and then became steady. The release of indomethacin from two medicated
 Cu-IUDs was biphasic and, in both cases, in accordance with the in vitro
 dissolution model of the drug. The surface area of copper of Cu-IUDs
 and the pH change induced by indomethacin incorporated in their frame
 affected the release rate of copper (p < 0.05).
 Conclusion The surface area of the copper and the pH of the test medium
 modulate the in vitro release of cupric ions from Cu-IUDs.
 SN 1362-5187
 PD JUN
 PY 2010
 VL 15
 IS 3
 BP 205
 EP 212
 DI 10.3109/13625181003782860
 UT ISI:000280194300007
 PT J
 AU Wang, Y
 Song, M
 Hang, TJ
 Wen, AD
 Yang, L
 AF Wang, Yu
 Song, Min
 Hang, Taijun
 Wen, Aidong
 Yang, Lin
 TI LC-MS-MS Simultaneous Determination of Niacin, Niacinamide and
 Nicotinuric Acid in Human Plasma LC-MS-MS and Its Application to a Human
 Pharmacokinetic Study
 SO CHROMATOGRAPHIA
 AB A highly selective and sensitive liquid chromatographic tandem mass
 spectrometric (LC-MS-MS) method was developed and validated for the
 quantitation and pharmacokinetic study of niacin (NA) and its two
 metabolites niacinamide (NAM) and nicotinuric acid (NUR) in human
 plasma. Protein precipitation with 14% perchloric acid solution was
 selected for sample preparation, and ganciclovir was used as an
 internal standard. Separation was on a Phenomenex Curosil-PFP (250 mm
 x 4.6 mm, 5 mu m) column by a multiple steep steps linear gradient
 elution with mobile phase consisting of water and methanol, both
 containing 0.1% formic acid, pumped at a flow rate of 1 mL min(-1).
 The determination was optimized and carried out with positive
 electrospray ionization by selective multiple reaction monitoring. The
 method was linear in the concentration range of 15-2,000 ng mL(-1) for
 NA, 70-2,000 ng mL(-1) for NAM and 10-2,000 ng mL(-1) for NUR, by
 standard addition calibration. The application of LC-MS-MS was
 demonstrated for the specific and quantitative analysis of NA, NAM and
 NUR in human plasma from a pharmacokinetic study in 12 healthy Chinese
 volunteers treated with three incremental doses of niacin
 extended-release/lovastatin tablets and an additional steady-state
 regime.
 SN 0009-5893
 PD AUG
 PY 2010
 VL 72
 IS 3-4
 BP 245
 EP 253
 DI 10.1365/s10337-010-1645-3
 UT ISI:000280250000008
 PT J
 AU Xu, GF
 Du, YX
 Chen, B
 Chen, JQ
 AF Xu, Guangfu
 Du, Yingxiang
 Chen, Bin
 Chen, Jiaquan
 TI Investigation of the Enantioseparation of Basic Drugs with
 Erythromycin Lactobionate as a Chiral Selector in CE
 SO CHROMATOGRAPHIA
 AB The macrocyclic antibiotics including ansamycins, glycopeptides,
 aminoglycosides and polypeptides have been demonstrated to exhibit
 powerful enantioselectivity towards numerous chiral compounds. By
 comparison with the four classes of antibiotics, macrolides are another
 type of macrocyclic antibiotics. In this study erythromycin
 lactobionate belonging to the group of macrolides is first used as a
 chiral selector in CE for the enantiomeric separations of basic drugs.
 As observed, erythromycin lactobionate allowed excellent separation
 of the enantiomers of
 N,N-dimethyl-3-(2-methoxyphenoxy)-3-propylamine, propranolol and
 duloxetine, as well as partial enantioresolution of primaquine,
 chloroquine and nefopam. In addition, erythromycin lactobionate
 possesses advantages such as high solubility and low viscosity in the
 solvent and very weak UV absorption. Among several experimental factors
 including buffer pH, BGE and erythromycin lactobionate concentrations,
 capillary temperature and applied voltage, we found that the
 enantioseparations of basic drugs above-mentioned strongly depended
 on the pH of BGE and the concentration of the chiral additive. The
 optimum pH was in the neutral or weak basic region but varied among
 drugs. An erythromycin lactobionate concentration of about 10% (w/v)
 and a low capillary temperature of 16 A degrees C were recommended for
 the practical analysis.
 SN 0009-5893
 PD AUG
 PY 2010
 VL 72
 IS 3-4
 BP 289
 EP 295
 DI 10.1365/s10337-010-1647-1
 UT ISI:000280250000013
 PT J
 AU Yin, RT
 Zheng, H
 Xi, T
 Xu, HM
 AF Yin, Runting
 Zheng, Heng
 Xi, Tao
 Xu, Han-Mei
 TI Effect of RGD-4C Position is More Important Than Disulfide Bonds on
 Antiangiogenic Activity of RGD-4C Modified Endostatin Derived
 Synthetic Polypeptide
 SO BIOCONJUGATE CHEMISTRY
 AB ES-2 (IVRRADRAAVP), an endostatin-derived synthetic polypeptide,
 contains the amino acids 50-60 of endostatin from its N terminus, and
 it had no inhibitory effects on tumor growth in vivo. In order to
 increase the targeted delivery of ES-2 to tumors and further enhance
 the activity, the polypeptide RGD-4C (ACDCRGDCFC) was introduced into
 ES-2, and the effects of RGD-4C position and RGD-4C disulfide bonds
 on polypeptides activity were investigated. When RGD-4C polypeptides
 (with or without disulfide bonds) were introduced to the N-terminals
 of synthesized ES-2, the modified ES-2 showed significant antitumor
 activity in vivo. Cell proliferation and chicken chorioallantoic
 membrane (CAM) assay results showed that disulfide bonds had no
 significant effects on RGD-4C-modified ES-2 antiangiogenic activity.
 Furthermore, the target of modified peptides was integrin alpha 5/beta
 1, rather than integrin alpha v beta 3 as previous studies mentioned.
 SN 1043-1802
 PD JUL
 PY 2010
 VL 21
 IS 7
 BP 1142
 EP 1147
 DI 10.1021/bc900292y
 UT ISI:000280028100004
 PT J
 AU Chen, Q
 Liu, QM
 Li, ZM
 Zhong, WY
 He, W
 Xu, DK
 AF Chen, Qing
 Liu, Qiongming
 Li, Zhoumin
 Zhong, Wenying
 He, Wei
 Xu, Danke
 TI A visual chip-based coimmunoprecipitation technique for analysis of
 protein-protein interactions
 SO ANALYTICAL BIOCHEMISTRY
 AB Here we report a visual chip-based coimmunoprecipitation (vChip-coIP)
 platform for analysis of protein-protein interactions (PPIs) by
 combining advantages of an antibody microarray, traditional coIP, and
 a silver enhancement detection method. The chip was fabricated by
 spotting anti-Flag antibody on aldehyde-modified slides, and the
 resulting platform could assay immunoprecipitate from a small amount
 of crude cell lysates containing Flag-bait and Myc-prey. The
 interaction signals are visible using biotinylated anti-Myc antibody
 and colloidal gold-labeled streptavidin followed by a silver
 enhancement detection method. It is shown that vChip-coIP is a simple,
 cost-effective, and highly efficient platform for the comprehensive
 study of PPIs. (C) 2010 Elsevier Inc. All rights reserved.
 SN 0003-2697
 PD SEP 15
 PY 2010
 VL 404
 IS 2
 BP 244
 EP 246
 DI 10.1016/j.ab.2010.05.003
 UT ISI:000280213400022
 PT J
 AU Xu, DH
 Zhang, YH
 Ma, DW
 AF Xu, Danhua
 Zhang, Yihua
 Ma, Dawei
 TI Organocatalytic approach to 3,5,6-trisubstituted and
 4,6-disubstituted tetrahydropyran-2-ones
 SO TETRAHEDRON LETTERS
 AB The diarylprolinol ether-catalyzed Michael addition and subsequent
 cyclization of ethyl 3-methyl-2-oxobut-3-enoate with aldehydes, and
 gamma-substituted beta,gamma-unsaturated-alpha-ketoesters with
 acetaldehyde, afforded the corresponding lactals, which were subjected
 to oxidation and stereocontrolled hydrogenation to provide
 3,5,6-trisubstituted and 4,6-disubstituted tetrahydropyran-2-ones
 with excellent enantioselectivities. (C) 2010 Elsevier Ltd. All rights
 reserved.
 SN 0040-4039
 PD JUL 21
 PY 2010
 VL 51
 IS 29
 BP 3827
 EP 3829
 DI 10.1016/j.tetlet.2010.05.077
 UT ISI:000279864100033
 PT J
 AU Conga, RG
 Zhang, YH
 Tian, WS
 AF Conga, Rigang
 Zhang, Yihua
 Tian, Weisheng
 TI A concise synthesis of the steroidal core of clathsterol
 SO TETRAHEDRON LETTERS
 AB The protected steroidal core of clathsterol, a marine natural product
 with remarkable inhibitory activity against HIV-1 reverse
 transcriptase, was synthesized starting from readily available
 tigogenin. The synthetic strategy involved three key reactions:
 abnormal Baeyer-Villiger rearrangement of the spiroketal of tigogenin,
 xanthation of steroidal 16-hydroxyl-22-carboxylate dianion and
 regioselective epoxide-opening lactonization. (C) 2010 Elsevier Ltd.
 All rights reserved.
 SN 0040-4039
 PD JUL 28
 PY 2010
 VL 51
 IS 30
 BP 3890
 EP 3892
 DI 10.1016/j.tetlet.2010.05.072
 UT ISI:000279817400006
 PT J
 AU He, SJ
 Zhu, JB
 Xie, FM
 AF He, Shengjiang
 Zhu, Jiabi
 Xie, Fuming
 TI Preparation and characterization of tramadol PEG-coated
 multivesicular liposomes for sustained release
 SO PHARMAZIE
 AB The purpose of the present study was to prepare multivesicular
 liposomes (MVL) with a high drug loading capacity for intramuscular
 sustained release and to investigate their potential applicability
 towards tramadol, and to improve the stability of liposomes by coating
 PEG. The basic physiochemical properties of tramadol MVLs and
 PEG-coated MVLs were studied. The average particle sizes of optimum
 preparation were 18.2 mu m and 31.3 mu m. The entrapment efficiency
 was up to 80%. The encapsulation efficiency of tramadol MVLs and
 PEG-coated MVLs was measured. The results confirmed the possibility
 of multivesicular liposomes as a sustained-release delivery system.
 Tramadol was continuously released from MVL formulations in PBS (pH6.8)
 in vitro, and reached a maximum of 80% within 72 h. The results show
 that tramadol PEG-coated MVLs could provide sustained release
 according to the first order kinetic equation.
 SN 0031-7144
 PD JUL
 PY 2010
 VL 65
 IS 7
 BP 467
 EP 470
 DI 10.1691/ph.2010.9357
 UT ISI:000279891200004
 PT J
 AU Chen, YJ
 Tao, J
 Xiong, F
 Zhu, JB
 Gu, N
 Geng, KK
 AF Chen, Y. J.
 Tao, J.
 Xiong, F.
 Zhu, J. B.
 Gu, N.
 Geng, K. K.
 TI Characterization and in vitro cellular uptake of PEG coated iron oxide
 nanoparticles as MRI contrast agent
 SO PHARMAZIE
 AB Monodisperse magnetic iron oxide nanoparticles (MNPs), coated with PEG
 at different molecular weight, were prepared via self-assembly method.
 The particle diameters were measured by dynamic light scattering and
 transmission electron microscope. Increasing the molecular weight of
 PEG in the coating polymer increased the overall particles diameter.
 As coating thickness increased, the saturation magnetization (Ms) and
 T-2 relaxivity decreased. The interactions of these MNPs with
 macrophage cells were also investigated. The results showed that
 cellular uptakes of MNPs depended on nanoparticle concentration and
 surface chemistry. The results of this study will have implications
 on the chemical design of nanomaterials for bio-imaging and
 bio-detection.
 SN 0031-7144
 PD JUL
 PY 2010
 VL 65
 IS 7
 BP 481
 EP 486
 DI 10.1691/ph.2010.9372
 UT ISI:000279891200007
 PT J
 AU Ji, BS
 Li, M
 He, L
 AF Ji, Bian-Sheng
 Li, Ming
 He, Ling
 TI Interaction of CJZ3, a lomerizine derivative, with ATPase activity of
 human P-glycoprotein in doxorubicin-resistant human myelogenous
 leukemia (K562/DOX) cells
 SO PHARMAZIE
 AB P-Glycoprotein, a 170-180 kDa membrane glycoprotein that mediates
 multidrug resistance, hydrolyses ATP to efflux a broad spectrum of
 hydrophobic agents. To observe the interaction of a P-gp reversal agent
 with P-gp ATPase activity should provide further insights into the
 mechanisms of P-gp modulator. In this study, we analysed the effect
 of CJZ3, a lomerizine derivative, on the adenosine triphosphatase
 (ATPase) activity of human P-glycoprotein. The results showed that the
 basal P-gp ATPase activity was increased by CJZ3 with half-maximal
 activity concentration (Km) of 6.8 +/- 1.5 mu M, CJZ3 may interact with
 P-gp with a higher affinity and exhibit a more potent effect than
 verapamil (Ver). Kinetic analysis indicated a noncompetitive
 inhibition of Ver-stimulated P-gp ATPase activity and a competitive
 inhibition of CJX2-stimulated P-gp ATPase activity by CJZ3, moreover,
 the effect of CsA on CJZ3-stimulated and Ver-stimulated P-gp ATPase
 activity showed a non-competitive and a competitive inhibition
 respectively. CJZ3 and CJX2 can bind P-gp either on overlapping sites
 or distinct but interacting sites, while CJZ3 and Ver as well as CsA
 can bind P-gp on separated sites in K562/DOX cells.
 SN 0031-7144
 PD JUL
 PY 2010
 VL 65
 IS 7
 BP 515
 EP 519
 DI 10.1691/ph.2009.9803
 UT ISI:000279891200013
 PT J
 AU Cheng, KG
 Liu, J
 Sun, HB
 Bokor, E
 Czifrak, K
 Konya, B
 Toth, M
 Docsa, T
 Gergely, P
 Somsak, L
 AF Cheng, Keguang
 Liu, Jun
 Sun, Hongbin
 Bokor, Eva
 Czifrak, Katalin
 Konya, Balint
 Toth, Marietta
 Docsa, Tibor
 Gergely, Pal
 Somsak, Laszlo
 TI Tethered derivatives of D-glucose and pentacyclic triterpenes for
 homo/heterobivalent inhibition of glycogen phosphorylase
 SO NEW JOURNAL OF CHEMISTRY
 AB Propargyl esters of the C-28 carboxylic acids of pentacyclic
 triterpenes (oleanolic, ursolic, and maslinic acids) were coupled with
 2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl azide as well as
 N-(omega-azido-[C-2, C-6, and
 C-11]alkanoyl)-beta-D-glucopyranosylamines under conditions of
 copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) to give
 tethered D-glucose-triterpene heteroconjugates. The O-acetyl
 protecting groups were removed by base-catalyzed hydrolysis.
 N-(omega-Azido-[C-2, C-6, C-11, and
 C-16]alkanoyl)-beta-D-glucopyranosylamines were also tethered by
 1,7-octadiyne under CuAAC conditions to furnish D-glucose
 homoconjugates. O-Deacetylation was carried out by the Zemplen
 protocol. The new compounds were assayed against rabbit muscle glycogen
 phosphorylase (RMGP) a or b enzymes. Some of the heteroconjugates
 inhibited the enzyme in the low micromolar range (IC50 values 40-70
 mu M), while the homoconjugates proved inefficient as inhibitors.
 SN 1144-0546
 PY 2010
 VL 34
 IS 7
 BP 1450
 EP 1464
 DI 10.1039/b9nj00602h
 UT ISI:000279911700028
 PT J
 AU Yao, Y
 Li, XB
 Zhao, W
 Zeng, YY
 Shen, H
 Xiang, H
 Xiao, H
 AF Yao, Yao
 Li, Xiao-Bo
 Zhao, Wei
 Zeng, Yan-Yan
 Shen, Hong
 Xiang, Hua
 Xiao, Hong
 TI Anti-obesity effect of an isoflavone fatty acid ester on obese mice
 induced by high fat diet and its potential mechanism
 SO LIPIDS IN HEALTH AND DISEASE
 AB Background: The novel compound 1a is one of the isoflavone fatty acid
 esters. In order to investigate the anti-obesity effect of compound
 1a and its potential mechanism of influence in adipocyte
 differentiation, Obese male C57BL/6J mice induced by high-fat diet
 (HFD) and rat preadipocytes (3T3-L1 cell) were used.
 Methods: After 4-week HFD induction, the obese model was made
 successfully. After treatment with compound 1a, mice plasma
 biochemistry parameters were analyzed. In addition, mice hepatic
 tissue slice was observed. In in vitro research, 3T3-L1 cell
 differentiation by Oil-Red-O staining and adipocyte apoptosis was
 detected by flow cytometry.
 Results: The in vivo results implied that compound 1a significantly
 decreased the body weight, white adipose tissue weight of obesity
 mice(p < 0.05), reduced leptin and TG in plasma(p < 0.05), elevated
 HDL-C in serum(p < 0.05). The in vitro results suggested that compound
 1a could significantly suppress the adipocyte viability and lipid
 accumulation in the differentiation of preadipocyte, and induce
 apoptosis in both preadipocytes and mature adipocytes(p < 0.05).
 Conclusion: Compound 1a regulates serum lipid profiles, decreases
 adipose tissue mass and body weight gain by inducing adipocyte
 apoptosis in high fat diet induced mice. Thus, it may be used to treat
 obese patients with hypercholesterolemia and hypertriglyceridemia.
 SN 1476-511X
 PD MAY 19
 PY 2010
 VL 9
 AR 49
 DI 10.1186/1476-511X-9-49
 UT ISI:000279907200001
 PT J
 AU Cao, RS
 Hu, YQ
 Wang, Y
 Gurley, EC
 Studer, EJ
 Wang, XA
 Hylemon, PB
 Pandak, WM
 Sanyal, AJ
 Zhang, LY
 Zhou, HP
 AF Cao, Risheng
 Hu, Yiqiao
 Wang, Yun
 Gurley, Emily C.
 Studer, Elaine J.
 Wang, Xuan
 Hylemon, Phillip B.
 Pandak, William M.
 Sanyal, Arun J.
 Zhang, Luyong
 Zhou, Huiping
 TI Prevention of HIV Protease Inhibitor-Induced Dysregulation of Hepatic
 Lipid Metabolism by Raltegravir via Endoplasmic Reticulum Stress
 Signaling Pathways
 SO JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
 AB Hyperlipidemia associated with the HIV protease inhibitor (PI), the
 major component of highly active antiretroviral treatment (HAART) for
 HIV infection, has stimulated interest in developing new agents that
 minimize these side effects in the clinic. HIV integrase inhibitor is
 a new class of anti-HIV agents. Raltegravir is a first-in-its-class
 oral integrase inhibitor and has potent inhibitory activity against
 HIV-1 strains that are resistant to other antiretroviral regimens. Our
 previous studies have demonstrated that HIV PI-induced endoplasmic
 reticulum (ER) stress links to dysregulation of lipid metabolism.
 However, little information is available as to whether raltegravir
 would have similar effects as the HIV PIs. In this study, we examined
 the effect of raltegravir on lipid metabolism both in primary rat
 hepatocytes and in in vivo mouse models, and we further determined
 whether the combination of raltegravir with existing HIV PIs would
 potentially exacerbate or prevent the previously observed development
 of dyslipidemia. The results indicated that raltegravir did not induce
 ER stress or disrupt lipid metabolism either in vitro or in vivo.
 However, HIV PI-induced ER stress and lipid accumulation were
 significantly inhibited by raltegravir both in in vitro primary rat
 hepatocytes and in in vivo mouse liver. High-performance liquid
 chromatography analysis further demonstrated that raltegravir did not
 affect the uptake and metabolism of HIV PIs in hepatocytes. Thus,
 raltegravir has less hepatic toxicity and could prevent HIV PI-induced
 dysregulation of lipid metabolism by inhibiting ER stress. These
 results suggest that incorporation of this HIV integrase inhibitor may
 reduce the side effects associated with current HAART.
 SN 0022-3565
 PD AUG 10
 PY 2010
 VL 334
 IS 2
 BP 530
 EP 539
 DI 10.1124/jpet.110.168484
 UT ISI:000279990700019
 PT J
 AU Zheng, H
 Jiang, YY
 Wang, Y
 Jia, XM
 Yan, TH
 Gao, PH
 Yan, L
 Jiang, LH
 Ji, H
 Cao, YB
 AF Zheng, Hao
 Jiang, Yuan-Ying
 Wang, Yan
 Jia, Xin-Ming
 Yan, Tian-Hua
 Gao, Ping-Hui
 Yan, Lan
 Jiang, Ling-Huo
 Ji, Hui
 Cao, Yong-Bing
 TI TOP2 gene disruption reduces drug susceptibility by increasing
 intracellular ergosterol biosynthesis in Candida albicans
 SO JOURNAL OF MEDICAL MICROBIOLOGY
 AB In this study the role of the TOP2 gene in fungal drug susceptibility
 was investigated by disrupting and overexpressing the gene in Candida
 albicans. MIC determination and a spot assay showed that a top2
 Delta/Delta null mutant (strain T2bc) was more resistant to the
 antifungals tested than the wildtype (strain CAI4). Real-time RT-PCR
 and rhodamine 6G efflux examination showed that TOP2 did not influence
 the activity of drug efflux pumps. Sterol analysis with
 GC/high-resolution MS indicated that the intracellular ergosterol
 composition of the top2 Delta/Delta mutant was significantly
 increased. Subsequently, fluorescence polarization measurements also
 revealed that Top2-deprived cells displayed a decrease in membrane
 fluidity, resulting in enhanced passive diffusion of the drugs.
 Quantitative real-time RT-PCR analysis further confirmed that the
 ERG11 gene, an essential gene in ergosterol biosynthesis, was
 upregulated. These results demonstrate a close relationship between
 the TOP2 gene and drug susceptibility in C. albicans.
 SN 0022-2615
 PD JUL
 PY 2010
 VL 59
 IS 7
 BP 797
 EP 803
 DI 10.1099/jmm.0.018325-0
 UT ISI:000279838400008
 PT J
 AU Yu, N
 Xun, Y
 Jin, D
 Yang, H
 Hang, T
 Cui, H
 AF Yu, N.
 Xun, Y.
 Jin, D.
 Yang, H.
 Hang, T.
 Cui, H.
 TI Effect of Sperminated Pullulans on Drug Permeation Through Isolated
 Rabbit Cornea and Determination of Ocular Irritation
 SO JOURNAL OF INTERNATIONAL MEDICAL RESEARCH
 AB The aim of this study was to investigate the effect of two sperminated
 pullulans (SP) with a different number of amino groups (SP-L, amino
 group content 0.124 mmol/g polymer; and SP-H, amino group content 0.578
 mmol/g polymer) on the permeation of drugs through isolated rabbit
 corneas. Determination of corneal hydration levels and Draize eye tests
 were performed to assess the safety of SP both in vitro and in vivo.
 For 0.2% (w/v) SP-L and 0.2% (w/v) SP-H, the enhancement ratios (ERs)
 with dexamethasone of 1.34 and 1.42, respectively, were not
 statistically significant. For ofloxacin, tobramycin and sodium
 fluorescein, the ERs with 0.2% SP-L were 1.37, 2.02 and 2.12,
 respectively, and with 0.2% SP-H the ERs were 1.84, 4.69 and 6.87,
 respectively; these ERs were all statistically significant.
 Enhancement increased with increasing amino group content of the SP.
 The improved transcorneal drug absorption via the paracellular route
 indicated opening of the tight junctions in the corneal epithelium.
 Irritation tests indicated that 0.2% SP-L and 0.2% SP-H did not damage
 the corneal tissues.
 SN 0300-0605
 PD MAR-APR
 PY 2010
 VL 38
 IS 2
 BP 526
 EP 535
 UT ISI:000279877200015
 PT J
 AU Li,
 AF Li, Xiu-Min
 Ma, Hai-Bin
 Ma, Zhan-Qiang
 Lu-Fan
 Chang-Liang
 Rong
 Shi-Ping
 TI Ameliorative and neuroprotective effect in MPTP model of Parkinson's
 disease by Zhen-Wu-Tang (ZWT), a traditional Chinese medicine
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Aim of the study: Traditional Chinese medicine Zhen-Wu-Tang (ZWT) is
 a well-known PentaHerbs formula from "Treatise on Febrile Disease".
 This study is to elucidate its neuroprotective effect and mechanism
 of ameliorative effect of the syndrome of Parkinson's disease (PD).
 Materials and methods:The ameliorative effect of ZWT on symptom of PD
 through behavior tests including: swimming test, the tail suspension
 test and open-field test was investigated. The neuroprotective effect
 of dopaminergic neurons from the striatum and frontal cortex of brain
 was detected by high performance liquid chromatography with
 electrochemical detection (HPLC-ECD).
 Results: This study proved that ZWT could ameliorate the typical
 symptom of PD and protect dopaminergic system.
 Conclusion: These results suggested that ZWT possessed protective and
 ameliorative properties of dopaminergic neurons. (C) 2010 Elsevier
 Ireland Ltd. All rights reserved.
 SN 0378-8741
 PD JUL 6
 PY 2010
 VL 130
 IS 1
 BP 19
 EP 27
 DI 10.1016/j.jep.2010.03.020
 UT ISI:000279886900004
 PT J
 AU Meng, QG
 Yu, M
 Gu, B
 Li, J
 Liu, Y
 Zhan, CY
 Xie, C
 Zhou, JP
 Lu, WY
 AF Meng, Qinggang
 Yu, Mei
 Gu, Bing
 Li, Jin
 Liu, Yu
 Zhan, Changyou
 Xie, Cao
 Zhou, Jianping
 Lu, Weiyue
 TI Myristic acid-conjugated polyethylenimine for brain-targeting
 delivery: in vivo and ex vivo imaging evaluation
 SO JOURNAL OF DRUG TARGETING
 AB To investigate the potential of myristic acid (MC) to mediate brain
 delivery of polyethylenimine (PEI) as a gene delivery system, a
 covalent conjugate (MC-PEI) of MC, and PEI was synthesized. A
 near-infrared fluorescence probe, IR820 was conjugated to MC-PEI to
 explore its in vivo distribution after intravenous (i.v.)
 administration in mice. The brain targeting ability of MC-PEI was
 evaluated by near-infrared fluorescence imaging and analyzed
 semiquantitatively by fluorescence intensity, respectively.
 Significant NIR fluorescent signal was detected in the brain 12 h after
 i.v. administration and further confirmed by imaging the whole brain
 and brain slices. Semiquantitative results from fluorescence intensity
 further supported the successful brain delivery of MC-PEI which led
 to a very significant increase (similar to 200%) in the brain uptake
 after i.v. injection in comparison with unmodified PEI. The capability
 of MC-PEI to condense DNA was further confirmed using agarose gel
 retardation assay, indicating its potential for gene delivery. The
 significant in vivo and ex vivo results suggest that MC-PEI is a
 promising brain-targeting drug delivery system, especially for gene
 delivery.
 SN 1061-186X
 PD JUL
 PY 2010
 VL 18
 IS 6
 BP 438
 EP 446
 DI 10.3109/10611860903494229
 UT ISI:000279926400004
 PT J
 AU Cao, J
 Xue, B
 Li, H
 Deng, DW
 Gu, YQ
 AF Cao, Jie
 Xue, Bing
 Li, Hui
 Deng, Dawei
 Gu, Yueqing
 TI Facile synthesis of high-quality water-soluble
 N-acetyl-L-cysteine-capped Zn1-xCdxSe/ZnS core/shell quantum dots
 emitting in the violet-green spectral range
 SO JOURNAL OF COLLOID AND INTERFACE SCIENCE
 AB In this paper, we report a new facile method to synthesize water-soluble
 Zn1-xCdxSe and core/shell Zn1-xCdxSe/ZnS quantum dots (QDs) emitting
 in the violet-green spectral range, using N-acetyl-L-cysteine (NAC)
 as a stabilizer. The influence of various experimental variables,
 including the precursor Zn/Cd/Se/NAC molar ratios, the pH of original
 solution and the refluxing time on optical properties were explored
 systematically. The obtained aqueous Zn1-xCdxSe QDs exhibit a tunable
 photoluminescence (PL) emission (from similar to 415 nm to 506 nm) and
 a favorable narrow PL bandwidth (FWHM: 27-38 nm). After coating with
 a ZnS shell, the PL emission intensity of the formed core/shell
 Zn1-xCdxSe/ZnS QDs is greatly increased (PL quantum yield (QY): similar
 to 30%). These resulting Zn1-xCdxSe and core/shell Zn1-xCdxSe/ZnS QDs
 were further characterized by transmission electron microscopy (TEM),
 energy disperse spectroscopy (EDS) and X-ray diffraction (XRD). In
 addition, the cytotoxicity and the fluorescence imaging of
 Zn1-xCdxSe/ZnS QDs to MCF-7 cells were preliminarily investigated. The
 experimental results show that the as-prepared violet-green-emitting
 Zn1-xCdxSe/ZnS QDs have low cytotoxicity, which makes them an ideal
 inorganic fluorescent probe for biolabeling and cell imaging. (C) 2010
 Elsevier Inc. All rights reserved.
 SN 0021-9797
 PD AUG 15
 PY 2010
 VL 348
 IS 2
 BP 369
 EP 376
 DI 10.1016/j.jcis.2010.05.007
 UT ISI:000279968700011
 PT J
 AU Yu, Y
 Yu, YL
 Liu, L
 Wang, XT
 Lu, SS
 Liang, Y
 Liu, XD
 Xie, L
 Wang, GJ
 AF Yu, Sen
 Yu, Yunli
 Liu, Li
 Wang, Xinting
 Lu, Shousi
 Liang, Yan
 Liu, Xiaodong
 Xie, Lin
 Wang, Guangji
 TI Increased Plasma Exposures of Five Protoberberine Alkaloids from
 Coptidis Rhizoma in Streptozotocin-Induced Diabetic Rats: Is P-GP
 Involved?
 SO PLANTA MEDICA
 AB Our previous study showed a higher exposure of berberine, palmatine,
 coptisine, epiberberine and jatrorrhizine in 6-week streptozotocin
 (STZ)-induced diabetic rats, after oral administration of Coptidis
 Rhizoma extract. The aim of the present study was to investigate whether
 the function and expression of intestinal P-glycoprotein (P-GP) was
 downregulated in STZ-induced diabetic rats and if the impairment of
 P-GP function and expression contributed to the exposure increase of
 the five protoberberine alkaloids. Plasma concentration-time profiles
 of the drugs in the portal vein were obtained after oral administration
 of Coptidis Rhizoma extract. The effective permeability of the drug
 across duodenum and ileum were measured using in situ single-pass
 intestine perfusion. P-GP function in the rat intestine was assessed
 by measuring the absorption of rhodamine 123 (Rho123). P-GP levels were
 evaluated using Western blots. It was found that the C-max and AUC(0-8)
 values of five alkaloids in the portal vein of diabetic rats were
 significantly higher than those in the control rats. Diabetic rats also
 exhibitd a higher level of Rho123 in the portal vein, which showed
 impairment of P-GP function. A higher effective permeability of the
 tested drug was found in the duodenum of diabetic rats using in situ
 single-pass intestine perfusion, indicating that berberine and Rho123
 transported more easily across the intestinal barrier of diabetic rats.
 A lower level of P-GP protein was found in the duodenum, jejunum and
 ileum of the diabetic rats as compared with age-matched control rats.
 All these results suggested that the function and expression of P-GP
 were impaired in the intestine of STZ-induced diabetic rats which, at
 least partly, contributed to the exposure increase of the five
 protoberberine alkaloids.
 SN 0032-0943
 PD JUN
 PY 2010
 VL 76
 IS 9
 BP 876
 EP 881
 DI 10.1055/s-0029-1240815
 UT ISI:000279668400006
 PT J
 AU Wang, L
 Yin, ZQ
 Wang, Y
 Zhang, XQ
 Li, YL
 Ye, WC
 AF Wang, Lei
 Yin, Zhi-Qi
 Wang, Ying
 Zhang, Xiao-Qi
 Li, Yao-Lan
 Ye, Wen-Cai
 TI Perisesaccharides A-E, New Oligosaccharides from the Root Barks of
 Periploca sepium
 SO PLANTA MEDICA
 AB Five new oligosaccharides, named perisesaccharides A-E (1-5), were
 isolated from the root barks of Periploca sepium. Their structures were
 elucidated by NMR and HRESIMS data. The absolute configurations of
 these compounds were determined by a combination of X-ray diffraction
 analysis, modified Mosher's method, circular dichroism spectroscopy,
 and acid hydrolysis. The boat conformation of oleandronic acid
 delta-lactone was reported for the first time.
 SN 0032-0943
 PD JUN
 PY 2010
 VL 76
 IS 9
 BP 909
 EP 915
 DI 10.1055/s-0029-1240842
 UT ISI:000279668400012
 PT J
 AU Zhou, L
 Ning, YW
 Wei, SH
 Feng, YY
 Zhou, JH
 Yu, BY
 Shen, J
 AF Zhou, Lin
 Ning, Yu-Wei
 Wei, Shao-Hua
 Feng, Yu-Ying
 Zhou, Jia-Hong
 Yu, Bo-Yang
 Shen, Jian
 TI A nanoencapsulated hypocrellin A prepared by an improved microemulsion
 method for photodynamic treatment
 SO JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
 AB A new hypocrellin A (HA) encapsulated silica nanoparticles was prepared
 by an improved microemulsion method based on the unique character of
 cetyl trimethyl ammonium bromide (CTAB). Stable aqueous dispersions
 of the HA-loaded nanoparticles, with the diameter about 50 nm, owned
 superior photo-stability and singlet oxygen generation ability to free
 HA. In vitro studies demonstrated the active uptake of HA-doped
 nanoparticles into the cytosol of HeLa (human cervix epithelioid
 carcinoma) cells. Significant morphology change and phototoxicity to
 such impregnated tumor cells was observed upon irradiation with light.
 Thus, the potential of using this method to prepare silica
 nanoparticles as drug carriers for photodynamic therapy has been
 demonstrated.
 SN 0957-4530
 PD JUL
 PY 2010
 VL 21
 IS 7
 BP 2095
 EP 2101
 DI 10.1007/s10856-010-4067-8
 UT ISI:000279592600011
 PT J
 AU Wang, J
 Dong, SF
 Liu, CH
 Wang, W
 Sun, SH
 Gu, JX
 Wang, YA
 Boraschi, D
 Qu, D
 AF Wang, Jing
 Dong, Shengfu
 Liu, Chunhong
 Wang, Wei
 Sun, Shuhui
 Gu, Jianxin
 Wang, Yuan
 Boraschi, Diana
 Qu, Di
 TI beta-Glucan Oligosaccharide Enhances CD8(+) TCells Immune Response
 Induced by a DNA Vaccine Encoding Hepatitis B Virus Core Antigen
 SO JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY
 AB DNA vaccination can induce specific CD8(+) T cell immune response, but
 the response level is low in large mammals and human beings.
 Coadministration of an adjuvant can optimize protective immunity
 elicited by a DNA vaccine. In this study, we investigated the effect
 of a synthetic glucohexaose (beta-glu6), an analogue of Lentinan basic
 unit, on specific CD8(+) T cell response induced by a DNA vaccine
 encoding HBcAg (pB144) in mice. We found that beta-glu6 promoted the
 recruitment and maturation of dendritic cells, enhanced the activation
 of CD8(+) and CD4(+) T cells and increased the number of specific
 CD8(+)/IFN-gamma(+) T cells in lymphoid and nonlymphoid tissues in mice
 immunized by pB144. Immunization with pB144 and beta-glu6 increased
 the anti-HBc IgG and IgG2a antibody titer. These results demonstrate
 that beta-glu6 can enhance the virus-specific CTL and Th1 responses
 induced by DNA vaccine, suggesting beta-glu6 as a candidate adjuvant
 in DNA vaccination.
 SN 1110-7243
 PY 2010
 AR 645213
 DI 10.1155/2010/645213
 UT ISI:000279791900001
 PT J
 AU Huo, MR
 Zhang, Y
 Zhou, JP
 Zou, AF
 Yu, D
 Wu, YP
 Li, J
 Li, H
 AF Huo, Meirong
 Zhang, Yong
 Zhou, Jianping
 Zou, Aifeng
 Yu, Di
 Wu, Yiping
 Li, Jing
 Li, Hong
 TI Synthesis and characterization of low-toxic amphiphilic chitosan
 derivatives and their application as micelle carrier for antitumor drug
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB A new series of amphiphilically modified chitosan molecules with long
 alkyl chains as hydrophobic moieties and glycol groups as hydrophilic
 moieties (N-octyl-O-glycol chitosan, OGC) was synthesized for use as
 drug carriers. The chemical structure was characterized by Fourier
 transform infrared, H-1 nuclear magnetic resonance, and elemental
 analysis. OGC could easily self-assemble to form nanomicelles in an
 aqueous environment and exhibited a low critical micellar
 concentration of 5.3-32.5 mg/L The biocompatibility and low toxicity
 of OGC as excipient for the dosage forms aimed at iv. administration
 were confirmed by hemolysis, acute toxicity and histopathological
 studies. Furthermore, the possibility of solubilizing paclitaxel
 (PTX), a water-insoluble antitumor drug, with OGC micelles was also
 explored. PTX was successfully loaded into OGC micelles by using a
 simple dialysis process. The drug-loading capacity of OGC and stability
 of drug-loaded micelles were significantly affected by the degree of
 substitution of alkyl chains. Moreover, a series of safety studies
 including hemolysis, hypersensitivity, maximum tolerated dose, acute
 toxicity, and organ toxicity revealed that the PTX-loaded OGC micelles
 had advantages over the commercially available injectable preparation
 of PTX (Taxol (R)), in terms of low toxicity levels and increased
 tolerated dose. Additionally, cytotoxicity studies showed that the
 PTX-loaded OGC micelles were comparable to the commercial formulation,
 but the blank micelles were far less toxic than the Cremophor EL
 vehicle. These results suggest that OGC is a promising carrier for
 injectable Pp( micelles. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0378-5173
 PD JUL 15
 PY 2010
 VL 394
 IS 1-2
 BP 162
 EP 173
 DI 10.1016/j.ijpharm.2010.05.001
 UT ISI:000279720400019
 PT J
 AU Pan, R
 Gao, XH
 Li, Y
 Xia, YF
 Dai, Y
 AF Pan, Rong
 Gao, Xing-Hua
 Li, Ying
 Xia, Yu-Feng
 Dai, Yue
 TI Anti-arthritic effect of scopoletin, a coumarin compound occurring in
 Erycibe obtusifolia Benth stems, is associated with decreased
 angiogenesis in synovium
 SO FUNDAMENTAL & CLINICAL PHARMACOLOGY
 AB Scopoletin is the main constituent of coumarin found in the stems of
 Erycibe obtusifolia Benth, a traditional Chinese medicine used in the
 treatment of rheumatoid arthritis. We have previously demonstrated
 that scopoletin is able to decrease the serum level of uric acid in
 hyperuricemic mice induced by potassium oxonate, and attenuate croton
 oil-induced inflammation. In the present study, we evaluated the
 anti-arthritic effects of scopoletin in rat adjuvant-induced arthritis
 by assessing paw swelling, pathology, and synovial angiogenesis. It
 was found that scopoletin, injected intraperitoneally at doses of 50,
 100 mg/kg, reduced both inoculated and non-inoculated paw swelling as
 well as articular index scores, and elevated the mean body weight of
 adjuvant-induced arthritic rats. Rats treated with higher dose of
 scopoletin showed a near-normal histological architecture of the
 joints and a reduced new blood vessel formation in the synovial tissues.
 Furthermore, scopoletin downregulated the overexpression of vascular
 endothelial growth factor, basic fibroblast growth factor and
 interleukin 6 in the synovial tissues of adjuvant-induced arthritic
 rats. In conclusion, scopoletin is capable of ameliorating clinical
 symptoms of rat adjuvant-induced arthritis, by reducing numbers of new
 blood vessels in the synovium and the production of important
 endogenous angiogenic inducers. Therefore, this compound may be a
 potential agent for angiogenesis-related diseases and could serve as
 a structural base for screening more potent synthetic analogs.
 SN 0767-3981
 PD AUG
 PY 2010
 VL 24
 IS 4
 BP 477
 EP 490
 DI 10.1111/j.1472-8206.2009.00784.x
 UT ISI:000279611400012
 PT J
 AU Du, Y
 Xu, W
 Yao, QZ
 Liu, ZL
 AF Du Yang
 Xu Wen
 Yao Qizheng
 Liu Zuliang
 TI Synthesis and Characterization of 4H-Pyridofuroxan-5-one and Its
 Nucleotide Derivative
 SO CHINESE JOURNAL OF ORGANIC CHEMISTRY
 AB A new compound, 4H-pyridofuroxan-5-one
 (4,5-dihydro-[1,2,5]oxadiazolo[3,4-b]pyridine-5-one 1-oxide), and
 its nucleotide derivative of tetraacetoxy D-ribose, were synthesized,
 and their structures as well as intermediates of each reactions were
 confirmed by H-1 NMR, MS techniques and elemental analysis.
 SN 0253-2786
 PD JUN
 PY 2010
 VL 30
 IS 6
 BP 928
 EP 932
 UT ISI:000279604600023
 PT J
 AU Yuan, YZ
 Zhang, M
 Qian, W
 Zhang, ZX
 AF Yuan Yao-Zuo
 Zhang Mei
 Qian Wen
 Zhang Zheng-Xing
 TI Characterization of Related Substances in Etimicin Sulfate Sample by
 High Performance Liquid Chromatography-Electrospray Ionization-Ion
 Trap-Mass Spectrometry
 SO CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
 AB A high performance liquid chromatography-electrospray ionization-ion
 trap-mass spectrometry (HPLC-ESI-IT-MS") method for the
 identification of related substances in etimicin was established. The
 analytical conditions were as follows; Phenomnex Gemini NX C-18 (150
 mm x 4. 6 mm, 5 mu m) column; the mobile phase; [water-ammonia-glacial
 acetic acid (96: 3. 6:0. 4)]-methanol (70: 30); flow rate of mobile
 phase; 1 mL/min; temperature of ESI ion source: 350 degrees C;
 nebulizing pressure; 275. 8 kPa; dry gas flow; 10 L/min and the analytes
 were detected in the positive mode. Eighteen related substances in a
 etimicin sample were separated and detected by HPLC-ESI-IT-MS" and
 thirteen related substances were deduced, they are gentamicin C-la,
 micronomicin and its three isomers, two etimicin's isomers, two
 degradation products of etimicin, two homologues of etimicin, and two
 other unknown compounds, the other five related substances which MS
 and MS2 data were detected can not be elucidated.
 SN 0253-3820
 PD JUN
 PY 2010
 VL 38
 IS 6
 BP 817
 EP 822
 DI 10.3724/SP.J.1096.2010.00817
 UT ISI:000279604300010
 PT J
 AU Xu, Z
 Wang, XB
 Dai, Y
 Kong, LY
 Wang, FY
 Xu, HA
 Lu, D
 Song, J
 Hou, ZG
 AF Xu, Zhao
 Wang, Xiaobing
 Dai, Yue
 Kong, Lingyi
 Wang, Fengyun
 Xu, Huan
 Lu, Dan
 Song, Jie
 Hou, Zhiguo
 TI (+/-)-Praeruptorin A enantiomers exert distinct relaxant effects on
 isolated rat aorta rings dependent on endothelium and nitric oxide
 synthesis
 SO CHEMICO-BIOLOGICAL INTERACTIONS
 AB Praeruptorin A is a coumarin compound naturally occurring in the roots
 of Peucedanum praeruptorum Dunn., a commonly used traditional Chinese
 medicine for the treatment of certain respiratory diseases and
 hypertension. Although previous studies indicated the relaxant effects
 of (+/-)-praeruptorin A on tracheal and arterial preparations, little
 is known about the functional characteristics of the enantiomers. In
 the present study, the two enantiomers were successfully isolated and
 identified by using a preparative Daicel Chiralpak AD-H column, and
 their relaxant effects on aorta rings were observed and compared.
 (+)-Praeruptorin A showed more potent relaxation than (-)-praeruptorin
 A against KCl- and phenylephrine-induced contraction of rat isolated
 aortic rings with intact endothelium. Removal of the endothelium
 remarkably reduced the relaxant effect of (+)-praeruptorin A but not
 that of (-)-praeruptorin A. Pretreatment of aortic rings with
 N-omega-nitro-L-arginine methyl ester (L-NAME, an inhibitor of nitric
 oxide synthase) or methylene blue (MB, a soluble guanylyl cyclase
 inhibitor) resulted in similar changes of the relaxant effects of the
 two enantiomers to endothelium removal. Molecular docking studies also
 demonstrated that (+)-praeruptorin A was in more agreement to nitric
 oxide synthase pharmacophores than (-)-praeruptorin A. On the other
 hand, the two enantiomers of praeruptorin A could slightly attenuate
 the contraction of rat aortic rings induced by internal Ca2+ release
 from sarcoplasmic reticulum (SR). These findings indicated that
 (+)-praeruptorin A and (-)-praeruptorin A exerted distinct relaxant
 effects on isolated rat aorta rings, which might be mainly attributed
 to nitric oxide synthesis catalyzed by endothelial nitric oxide
 synthase. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
 SN 0009-2797
 PD JUL 30
 PY 2010
 VL 186
 IS 2
 BP 239
 EP 246
 DI 10.1016/j.cbi.2010.04.024
 UT ISI:000279644900016
 PT J
 AU Zhou, L
 Liu, JH
 Ma, F
 Wei, SH
 Feng, YY
 Zhou, JH
 Yu, BY
 Shen, JA
 AF Zhou, Lin
 Liu, Ji-Hua
 Ma, Fei
 Wei, Shao-Hua
 Feng, Yu-Ying
 Zhou, Jia-Hong
 Yu, Bo-Yang
 Shen, Jian
 TI Mitochondria-targeting photosensitizer-encapsulated amorphous
 nanocage as a bimodal reagent for drug delivery and biodiagnose in vitro
 SO BIOMEDICAL MICRODEVICES
 AB The use of ceramic nano-carriers containing anti-cancer drugs for
 targeted delivery that span both fundamental and applied research has
 attracted the interest of the scientific community. In this paper, a
 hydrophobic photodynamic therapy drug, hypocrellin A (HA), was
 successfully encapsulated in water-soluble amorphous silica nanocage
 (HANC) by an improved sol-gel method. These nanocages are of ultrasmall
 size, highly monodispersed, stable in aqueous suspension, and retain
 the optical properties of HA. Moreover, these nanocages can be
 effectively delivered, subsequently taken up by cancer cells and
 finally targeted to mitochondria. In addition, incubation time
 dependent photodynamic efficacy difference between HANC and HA was
 investigated for the first time. Especially, the nanocages, owning
 extremely high stable fluorescence comparing with free HA, also have
 potentials as efficient probes for optical biodiagnose in vitro. All
 these properties of HANC could possibly make it especially promising
 to be used as a bimodal reagent for photodynamic therapy and
 biodiagnose.
 SN 1387-2176
 PD AUG
 PY 2010
 VL 12
 IS 4
 BP 655
 EP 663
 DI 10.1007/s10544-010-9418-1
 UT ISI:000279500200010
 PT J
 AU Zhang, YF
 Ye, BP
 Wang, DY
 AF Zhang, Yanfen
 Ye, Boping
 Wang, Dayong
 TI Effects of Metal Exposure on Associative Learning Behavior in Nematode
 Caenorhabditis elegans
 SO ARCHIVES OF ENVIRONMENTAL CONTAMINATION AND TOXICOLOGY
 AB In the present study, the thermotaxis model was used to evaluate the
 effects of metal exposure at different concentrations on associative
 learning behavior in nematodes. The examined nematodes were cultured
 at 25 or 17A degrees C, and then shifted to 20A degrees C condition.
 Based on the ability of nematodes to trace the temperature of 20A
 degrees C, exposure to 10 mu M of all examined metals and 2.5 mu M Pb
 and Hg caused significant decrease of associative learning behavior
 at time intervals of 5 and 18 h; however, exposure to 2.5 mu M Cu, Zn,
 and Ag did not influence associative learning behavior. Moreover,
 exposure to 2.5 and 10 mu M of examined metals did not influence body
 bend and thermotaxis to cultivation temperature, whereas exposure to
 50 mu M of examined metals caused significant reduction of body bend
 and thermotaxis to cultivation temperature. Furthermore, Pb and Hg were
 the more toxic among the examined metals, with severe toxicity on
 associative learning behavior, thermotaxis, and locomotion behavior
 in nematodes.
 SN 0090-4341
 PD JUL
 PY 2010
 VL 59
 IS 1
 BP 129
 EP 136
 DI 10.1007/s00244-009-9456-y
 UT ISI:000279581100014
 PT J
 AU Wei, MC
 Deng, J
 Feng, K
 Yu, BY
 Chen, YJ
 AF Wei, Maochen
 Deng, Jing
 Feng, Kun
 Yu, Boyang
 Chen, Yijun
 TI Universal Method Facilitating the Amplification of Extremely GC-Rich
 DNA Fragments from Genomic DNA
 SO ANALYTICAL CHEMISTRY
 AB Polymerase chain reaction (PCR) is a basic technique with wide
 applications in molecular biology. Despite the development of
 different methods with various modifications, the amplification of
 GC-rich DNA fragments is frequently troublesome due to the formation
 of complex secondary structure and poor denaturation. Given the fact
 that GC-rich genes are closely related to transcriptional regulation,
 transcriptional silencing, and disease progression, we developed a PCR
 method combining a stepwise procedure and a mixture of additives in
 the present work. Our study demonstrated that the PCR method could
 successfully amplify targeted DNA fragments up to 1.2 Kb with GC content
 as high as 83.5% from different species. Compared to all currently
 available methods, our work showed satisfactory, adaptable, fast and
 efficient (SAFE) results on the amplification of GC-rich targets, which
 provides a versatile and valuable tool for the diagnosis of genetic
 disorders and for the study of functions and regulations of various
 genes.
 SN 0003-2700
 PD JUL 15
 PY 2010
 VL 82
 IS 14
 BP 6303
 EP 6307
 DI 10.1021/ac100797t
 UT ISI:000279727800053
 PT J
 AU Huang, FH
 Zhang, XY
 Zhang, LY
 Li, Q
 Ni, B
 Zheng, XL
 Chen, AJ
 AF Huang, Fang-hua
 Zhang, Xin-yue
 Zhang, Lu-yong
 Li, Qin
 Ni, Bin
 Zheng, Xiao-liang
 Chen, Ai-jun
 TI Mast cell degranulation induced by chlorogenic acid
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To investigate the mechanism of chlorogenic acid (CA)-induced
 anaphylactoid reactions. Methods: Degranulation of peritoneal mast
 cells was assayed by using alcian blue staining in guinea pigs, and
 the degranulation index (DI) was calculated. CA-induced degranulation
 of RBL-2H3 cells was also observed and assayed using light microscopy,
 transmission electron microscopy, flow cytometry, and
 beta-hexosaminidase release.
 Results: CA 0.2, 1.0, and 5.0 mmol/L was able to promote degranulation
 of peritoneal mast cells in guinea pigs in vitro, but it did not increase
 the degranulation of peritoneal mast cells in CA-sensitized guinea pigs
 compared with control (P>0.05). Treatment with CA 0.2, 1.0, and 5.0
 mmol/L for 30, 60, and 120 min induced degranulation in RBL-2H3 cells
 in a dose-and time-dependent manner (P<0.01). Under transmission
 electron microscope typical characteristics of degranulation,
 including migration of granular vesicles toward the plasma membrane
 and integration combined with exocytosis, were observed, after CA or
 C48/80 treatment. Fluorescent microscopy and flow cytometric analysis
 showed that CA induced concentration-dependent translocation of
 phosphatidylserine in RBL-2H3 cells. beta-hexosaminidase release in
 RBL-2H3 cells was significantly increased after incubation with 1
 mmol/L CA for 60 min and 5 mmol/L CA for 30 min (P<0.01).
 Conclusion: CA induces degranulation of peritoneal mast cells and
 RBL-2H3 cells in guinea pigs, which might be one of the mechanisms of
 the generation of anaphylactoid reactions induced by CA.
 SN 1671-4083
 PD JUL
 PY 2010
 VL 31
 IS 7
 BP 849
 EP 854
 DI 10.1038/aps.2010.63
 UT ISI:000279538400011
 PT J
 AU Liu, JJ
 Ma, XA
 Cai, LB
 Cui, YG
 Liu, JY
 AF Liu, Jin-Juan
 Ma, Xiang
 Cai, Ling-Bo
 Cui, Yu-Gui
 Liu, Jia-Yin
 TI Downregulation of both gene expression and activity of Hsp27 improved
 maturation of mouse oocyte in vitro
 SO REPRODUCTIVE BIOLOGY AND ENDOCRINOLOGY
 AB Background: Heat shock protein 27 (Hsp27), a member of the small heat
 shock protein family, is an apoptosis regulator. Our previous proteomic
 study showed that Hsp27 mainly expressed in human oocyte, and that Hsp27
 expression was downregulated in the ovaries derived from women with
 the polycystic ovary syndrome (PCOS), a well known endocrinal disorder
 with abnormal apoptotic activity and folliculogenesis. However, the
 exact effects of Hsp27 downregulation on oocyte development have not
 yet been clarified.
 Methods: The expression of Hsp27 gene was downregulated in the mouse
 oocytes cultured in vitro using siRNA adenovirus infection, while the
 activity of Hsp27 was decreased by microinjection of polyclonal Hsp27
 antibody into the cytoplasm of germinal vesicle (GV) oocytes. Oocyte
 maturation rate was evaluated by morphological observation. Early
 stage of apoptosis was determined using Annexin-V staining analysis
 and some critical apoptotic factors and cytokines were also monitored
 at both mRNA level by real time RT-PCR and protein expression level
 by immunofluorescence and western blot.
 Results: Hsp27 expressed at high level in maturing oocytes. Infection
 with AdshHsp27, and microinjection of Hsp27 antibody into GV oocytes,
 resulted in the improved oocyte development and maturation. Germinal
 vesicle breakdown (GVBD) rates were significantly increased in two
 AdshHsp27-treated groups (88.7%, 86.0%) and Hsp27 antibody-injected
 group (77.0%) when compared with control (76.2% in AdGFP, 64.4% in
 IgG-injected), respectively. In addition, the rates of metaphase II
 (MII) development in two AdshHsp27-treated groups (73.8%, 76.4%) and
 Hsp27 antibody-injected group (67.3%) were higher than that in the
 controls (59.6% in AdGFP, 55.1% in IgG-injected). We also found that
 the rates of early stage of apoptosis in Hsp27 downregulated groups
 (46.5% and 45.6%) were higher than that in control group (34.1%) after
 8 h of IVM. Similarly, downregulation of Hsp27 caused a significantly
 enhanced the expression of apoptotic factors (caspase 8, caspase 3)
 and cytokines (bmp 15 and gdf 9).
 Conclusions: Downregulation of Hsp27 improved the maturation of mouse
 oocytes, while increased early stage of apoptosis in oocytes by
 inducing the activation of extrinsic, caspase 8-mediated pathway.
 SN 1477-7827
 PD MAY 14
 PY 2010
 VL 8
 AR 47
 DI 10.1186/1477-7827-8-47
 UT ISI:000279509200002
 PT J
 AU Cao, X
 Yao, Z
 Shao, M
 Chen, H
 Ye, W
 Yao, X
 AF Cao, X.
 Yao, Z.
 Shao, M.
 Chen, H.
 Ye, W.
 Yao, X.
 TI Pharmacokinetics of methyl protodioscin in rats
 SO PHARMAZIE
 AB Methyl protodioscin (MPD), a natural furostanol saponin, showed
 distinct antitumor activity and is distributed in many traditional
 Chinese medicines. The pharmacokinetics, distribution and excretion
 of MPD were first investigated after i.v. injection to rats in this
 study. The dose-dependent pharmacokinetics of MPD were characterized
 after i.v. injection (20, 40 and 120 mg/kg of MPD) to rats. A good
 linearity (r = 0.9989, P < 0.05) was found in the regression analysis
 of the AUC(0-t) -dose. The plasma concentrations of MPD declined
 rapidly with an elimination half-life (t(1/2)) from 25.56 to 29.32 min.
 The MPD kinetics was in line with one-compartment model after i.v.
 injection. 23.43% and 32.86% of MPD was recovered in urine and bile,
 respectively. The concentrations of MPD in plasma and most examined
 tissues 5 h after injection were close to or below the Low Limit of
 Quantification (LLOQ). This indicated that MPD was distributed and
 eliminated rapidly in rats.
 SN 0031-7144
 PD MAY
 PY 2010
 VL 65
 IS 5
 BP 359
 EP 362
 DI 10.1691/ph.2010.9785
 UT ISI:000279426600010
 PT J
 AU Perera, PK
 Li, YM
 Peng, C
 Fang, WR
 Han, CF
 AF Perera, Pathirage Kamal
 Li, Yunman
 Peng, Cheng
 Fang, Weirong
 Han, Caifeng
 TI Immunomodulatory activity of a Chinese herbal drug Yi Shen Juan Bi in
 adjuvant arthritis
 SO INDIAN JOURNAL OF PHARMACOLOGY
 AB Objective: To investigate the immunomodulating mechanisms of a Chinese
 herbal medicine Yi Shen Juan Bi (YJB) in treatment of adjuvant arthritis
 (AA) in rats. Materials and Methods: Levels of serum tumor necrosis
 factor alpha (TNF-) and interleukin-1 (IL-1) were measured by the
 Enzyme-Linked Immunosorbent Assay (ELISA). Expression of TNF- mRNA and
 IL-1 mRNA in synovial cells was measured with the semi-quantitative
 technique of reverse transcription-polymerase chain reaction
 (RT-PCR), while caspase-3 was examined by western blot analysis.
 Results: The administration of YJB significantly decreased the
 production of serum TNF- and IL-1. It also decreased significantly the
 TNF- mRNA, IL-1 mRNA, and caspase-3 expression in synoviocytes.
 Conclusions: YJB produces the immunomodulatory effects by
 downregulating the over-activated cytokines, while it activates
 caspase-3, which is the key executioner of apoptosis in the immune
 system. This may be the one of the underlying mechanisms that explains
 how YJB treats the rheumatoid arthritis.
 SN 0253-7613
 PD MAR-APR
 PY 2010
 VL 42
 IS 2
 BP 65
 EP 69
 DI 10.4103/0253-7613.64489
 UT ISI:000279251500002
 PT J
 AU Wang, Y
 Yin, HP
 Lv, XB
 Wang, YF
 Gao, HY
 Wang, M
 AF Wang, Ying
 Yin, Hongping
 Lv, Xiaobo
 Wang, Yufeng
 Gao, Hongyan
 Wang, Min
 TI Protection of chronic renal failure by a polysaccharide from Cordyceps
 sinensis
 SO FITOTERAPIA
 AB A water-soluble polysaccharide (CPS-2), isolated from the cultured
 Cordyceps sinensis, was obtained by hot-water extraction,
 anion-exchange and gel permeation chromatography. Its structural
 characteristics were investigated by PMP pre-column derivation,
 periodate oxidation, methylation analysis, FTIR and NMR spectroscopy.
 CPS-2 was found to be mostly of alpha-(1 -> 4)-D-glucose and alpha-(1
 -> 3)-D-mannose, branched with alpha-(1 -> 4,6)-D-glucose every twelve
 residues on average. CPS-2 had a molecular weight of 4.39 x 10(4) Da.
 The protective effect of CPS-2 on the model of chronic renal failure
 was established by fulgerizing kidney. The changes in blood urea
 nitrogen and serum creatinine revealed that CPS-2 could significantly
 relieve renal failure caused by fulgerizing kidney. (C) 2009 Elsevier
 B.V. All rights reserved.
 SN 0367-326X
 PD JUL
 PY 2010
 VL 81
 IS 5
 BP 397
 EP 402
 DI 10.1016/j.fitote.2009.11.008
 UT ISI:000279306700018
 PT J
 AU Xia, ZX
 Qu, W
 Lu, HY
 Fu, JQ
 Ren, YL
 Liang, JY
 AF Xia, Zhengxiang
 Qu, Wei
 Lu, Haiying
 Fu, Juqin
 Ren, Yanli
 Liang, Jingyu
 TI Sesquiterpene lactones from Sonchus arvensis L. and their
 antibacterial activity against Streptococcus mutans ATCC 25175
 SO FITOTERAPIA
 AB Two new sesquiterpene lactones,1 beta-sulfate-5 alpha, 6 beta
 H-eudesma-3-en-12, 6 alpha-olide (1) and 1 beta-(p-hydroxyphenyl
 acetyl)-15-O-beta-D-glucopyranosyl-5 alpha, 6 beta
 H-eudesma-3-en-12, 6 alpha-olide (2) were isolated from Sonchus
 arvensis L (Asteraceae), together with eight known compounds. Their
 structures were elucidated through spectroscopic and chemical methods.
 They were evaluated for antibacterial activity. Among them, compounds
 1 and 7 exhibited antibacterial activity against oral pathogen
 Streptococcus mutans ATCC 25175 with MIC values of 15.6 and 62.5 mu
 g/ml, respectively. (c) 2010 Elsevier B.V. All rights reserved.
 SN 0367-326X
 PD JUL
 PY 2010
 VL 81
 IS 5
 BP 424
 EP 428
 DI 10.1016/j.fitote.2009.12.001
 UT ISI:000279306700022
 PT J
 AU Fu, JH
 Sun, HS
 Wang, Y
 Zheng, WQ
 Shi, ZY
 Wang, QJ
 AF Fu, J. -h.
 Sun, H. -s.
 Wang, Y.
 Zheng, W. -q.
 Shi, Z. -y.
 Wang, Q. -j.
 TI The Effects of a Fat- and Sugar-Enriched Diet and Chronic Stress on
 Nonalcoholic Fatty Liver Disease in Male Wistar Rats
 SO DIGESTIVE DISEASES AND SCIENCES
 AB The pathogenesis of nonalcoholic fatty liver disease (NAFLD) is still
 under debate. The aim of this study was to investigate the effects of
 a long-term fat- and sugar-enriched diet (FSED) and chronic stress (CS)
 on NAFLD.
 Male Wistar rats were fed on either a standard diet or a FSED and given
 CS, a random electric foot shock (2 hr/morning and afternoon per day),
 or not for 12 weeks. After the experimental period, epididymal adipose
 tissue weight, sign of visceral obesity (VO), and hepatic index (HI)
 were measured. At sacrifice blood samples and liver were obtained.
 Histology of the liver was blindly determined by a pathologist.
 Histopathologically, moderate to severe steatosis, ballooning
 hepatocytes, and portal or lobules inflammation were observed in the
 FSED+CS group. However, mild to moderate steatosis with a few portal
 inflammation in the FSED group and mild steatosis or not with a few
 portal inflammation in the CS group were found correspondingly. In
 addition, more severe blood-fat disorder, high HI, fatty metabolic
 dysfunction, oxidative stress, high expressions of C-reactive protein
 mRNA and low expressions of peroxisome proliferator-activated receptor
 alpha mRNA in the liver were also revealed in the FSED+CS group. But,
 the degree of VO was not different between the FSED and FSED+CS groups.
 The observations strongly suggest that chronic stress can aggravate
 fat- and sugar-enriched diet-induced NAFLD from steatosis to
 steatohepatitis in male Wistar rats, although VO is not changed.
 SN 0163-2116
 PD AUG
 PY 2010
 VL 55
 IS 8
 BP 2227
 EP 2236
 DI 10.1007/s10620-009-1019-6
 UT ISI:000279294200014
 PT J
 AU Chen, JQ
 Hu, ZJ
 Wang, D
 Gao, CJ
 Ji, R
 AF Chen, Jian-qiu
 Hu, Zhi-jun
 Wang, Duo
 Gao, Cong-jie
 Ji, Rong
 TI Photocatalytic mineralization of dimethoate in aqueous solutions using
 TiO2: Parameters and by-products analysis
 SO DESALINATION
 AB Photocatalytic mineralization of dimethoate using nanosized TiO2 at
 different conditions has been investigated. The objective of this work
 was to study the influence on the photocatalytic mineralization of
 dimethoate, of various parameters and identify intermediates formed
 during photocatalytic treatment. The mineralization efficiency of
 dimethoate increased with elevated concentration of humic acid up to
 5 mg/L, while the efficiency reduced when the concentration was above
 5 mg/L due to competitive adsorption. The presence of CH3COCH3 can
 significantly inhibit dimethoate mineralization and the half-life of
 mineralization efficiency was increased by about 3 times. The photo
 mineralization efficiency changed with increasing concentrations of
 inorganic ions. With respect to the ions of Fe3+, Cu2+, Zn2+, HCO3and NO3-, the mineralization efficiency increased with increasing
 concentration of ions and reached a maximum at optimal concentrations,
 which was followed by a decrease with a further increase in ion
 concentrations. By contrast, the mineralization of dimethoate was
 strongly inhibited by Cl- and Cr3+ ions. Intermediate products from
 dimethoate were identified by means of GC MS and four possible
 by-products were identified. A proposed mineralization pathway for
 dimethoate is presented. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0011-9164
 PD AUG
 PY 2010
 VL 258
 IS 1-3
 BP 28
 EP 33
 DI 10.1016/j.desal.2010.03.053
 UT ISI:000279229400005
 PT J
 AU Wang, JX
 Yang, Y
 Ma, JH
 Zhang, L
 Guo, QL
 You, QD
 AF Wang Jin-Xin
 Yang Yan
 Ma Jun-Hai
 Zhang Lei
 Guo Qing-Long
 You Qi-Dong
 TI Synthesis of Gambogic Acid Oxidative Analogues and Their Dimension
 Quantity Structure-activity Relationship Analysis
 SO CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 AB 35,40-Dihydroxyl-6-methoxyl-gambogic acid methyl ester(1), 9,
 10-dihydroxy1-6-methoxyl-gambogie acid methyl ester(2) and
 2-deisohexylene-2-(2-formyl)ethy1-6-methoxyl-gambogic acid methyl
 ester(3) were first synthesized. And their antitumour activities on
 several cancer lines were tested. Meanwhile via Tripos Sci QSAR
 software calculation the QSAR equation explains the relationship
 between activity and structure with 2D QSAR method, and the biological
 activities are closely related to polarity volume ratio, the absolute
 value of the total charge, valence connectivity indexes and molecular
 volume. Our research can provide some guide meaning for the following
 research on studies of gambogic acid derivates.
 SN 0251-0790
 PD JUN 10
 PY 2010
 VL 31
 IS 6
 BP 1172
 EP 1178
 UT ISI:000279304500023
 PT J
 AU Gao, YA
 Qian, SA
 Zhang, JJ
 AF Gao, Yuan
 Qian, Shuai
 Zhang, Jianjun
 TI Physicochemical and Pharmacokinetic Characterization of a Spray-Dried
 Cefpodoxime Proxetil Nanosuspension
 SO CHEMICAL & PHARMACEUTICAL BULLETIN
 AB Cefpodoxime proxetil (CP) is a prodrug, the third generation
 cephem-type broad-spectrum antibiotic administered orally. However,
 CP was found to be a poorly water-soluble drug with low bioavailability
 when orally administered. In the present investigation, the
 spray-dried cefpodoxime proxetil nanosuspension (SDN) was prepared.
 The physicochemical properties were characterized by rheological
 evaluation, particle size measurement and its distribution, dynamics
 of reconstitution, in-vitro dissolution testing, surface morphology,
 surface area and pore size measurements. The pharmacokinetic study of
 SDN, in comparison to a marketed cefpodoxime proxetil for oral
 suspension (MS), was also performed in rabbits after a single oral dose.
 It was found that SDN exhibited a significant decrease in t(max), a
 1.60-fold higher area under curve (AUC) and 2.33-fold higher maximum
 plasma concentration (C-max) than MS.
 SN 0009-2363
 PD JUL
 PY 2010
 VL 58
 IS 7
 BP 912
 EP 917
 UT ISI:000279213500006
 PT J
 AU Chen, ND
 Yue, L
 Zhang, JA
 Kou, JP
 Yu, BY
 AF Chen, Nai-Dong
 Yue, Lei
 Zhang, Jian
 Kou, Jun-Ping
 Yu, Bo-Yang
 TI One unique steroidal sapogenin obtained through the microbial
 transformation of ruscogenin by Phytophthora cactorum ATCC 32134 and
 its potential inhibitory effect on tissue factor (TF) procoagulant
 activity
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB With the aim to obtain more effective tissue factor (TF) inhibitors,
 the microbial transformation of three steroidal sapogenins, ruscogenin
 (1), diosgenin (2) and sarsasapogenin (3), was carried out and only
 ruscogenin was selectivity converted to 1-hydroxy-spirost-4-en-3-one
 (4) by Phytophthora cactorum ATCC 32134. The in vitro anti-TF
 procoagulant activity of this metabolite was enhanced almost 10 times
 to an IC50 value of 0.29 mu M. The chemical assignments of compound
 4 were made unambiguously using ESI-MS, IR and 2D NMR spectroscopy.
 (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0960-894X
 PD JUL 15
 PY 2010
 VL 20
 IS 14
 BP 4015
 EP 4017
 DI 10.1016/j.bmcl.2010.05.103
 UT ISI:000279258800003
 PT J
 AU Liu, XH
 Liu, HF
 Shen, X
 Song, BA
 Bhadury, PS
 Zhu, HL
 Liu, JX
 Qi, XB
 AF Liu, Xin-Hua
 Liu, Hui-Feng
 Shen, Xu
 Song, Bao-An
 Bhadury, Pinaki S.
 Zhu, Hai-Liang
 Liu, Jin-Xing
 Qi, Xing-Bao
 TI Synthesis and molecular docking studies of novel 2-chloro-pyridine
 derivatives containing flavone moieties as potential antitumor agents
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB A series of novel 2-chloro-pyridine derivatives containing flavone,
 chrome or dihydropyrazole moieties as potential telomerase inhibitors
 were synthesized. The bioassay tests showed that compounds 6e and 6f
 exhibited some effect against gastric cancer cell SGC-7901 with IC50
 values of 22.28 +/- 6.26 and 18.45 +/- 2.79 mu g/mL, respectively. All
 title compounds were assayed for telomerase inhibition by a modified
 TRAP assay, the results showed that compound 6e can strongly inhibit
 telomerase with IC50 value of 0.8 alpha 0.07 mu M. Docking simulation
 was performed to position compound 6e into the active site of telomerase
 (3DU6) to determine the probable binding model. (C) 2010 Elsevier Ltd.
 All rights reserved.
 SN 0960-894X
 PD JUL 15
 PY 2010
 VL 20
 IS 14
 BP 4163
 EP 4167
 DI 10.1016/j.bmcl.2010.05.080
 UT ISI:000279258800039
 PT J
 AU Liu, K
 Wang, H
 An, YA
 Liu, BL
 Huang, F
 AF Liu Kang
 Wang Heng
 An Yuan
 Liu Baolin
 Huang Fang
 TI Resveratrol modulates adipokine expression and improves insulin
 sensitivity in adipocytes: Relative to inhibition of inflammatory
 responses
 SO BIOCHIMIE
 AB Resveratrol is a potent inhibitor of inflammation and has anti-diabetic
 potentiality, however whether its anti-inflammatory potency
 contributes to the amelioration of diabetes or insulin resistance
 remains to be determined. This study aims at evaluating the effects
 of resveratrol on inflammation-related adipokines expression and
 insulin sensitivity in adipocytes. We stimulated RAW264.7 cells with
 LPS and collected the supernatant as a conditioned medium (CM) for the
 culture of adipocytes. Resveratrol, at concentrations ranging from 0.1
 to 10 mu M, effectively inhibited lipopolysaccharide (LPS)-induced
 INF-alpha and IL-6 production with the downregulation of relative genes
 expression in macrophages. Exposing differentiated 3T3-L1 cells to
 RAW264.7 CM resulted in gene over-expressions of TNF-alpha, IL-6 and
 resistin, however, mRNA expression of adiponectin and PPAR gamma were
 down-regulated. Pretreatment of CM from resveratrol-treated
 macrophages reduced the elevated levels of TNF-alpha and IL-6, and
 significantly reversed inflammation-related changes in adipokine gene
 expression in 3T3-L1 adipocytes. Resveratrol suppressed extracellular
 receptor-activated kinase (ERK) and transcription factor-kappa B
 (NF-kappa B) activation by reducing the phosphorylation of ERK1/2 and
 NF-kappa B p65: moreover, it modulated insulin signaling transduction
 by modification of Ser/Thr phosphorylation of insulin receptor
 substrate-1 (IRS-1) and downstream AKT (T308), and thereby improved
 insulin sensitivity in adiposities. These results demonstrated that
 resveratrol modulated adipokines expression and improved insulin
 sensitivity which relative to inhibition of inflammatory-like response
 in adipocytes. (C) 2010 Elsevier Masson SAS. All rights reserved.
 SN 0300-9084
 PD JUL
 PY 2010
 VL 92
 IS 7
 BP 789
 EP 796
 DI 10.1016/j.biochi.2010.02.024
 UT ISI:000279474800008
 PT J
 AU Zhu, YA
 Yu, JN
 Tong, SS
 Wang, L
 Peng, M
 Cao, X
 Xu, XM
 AF Zhu, Yuan
 Yu, Jiangnan
 Tong, Shanshan
 Wang, Li
 Peng, Min
 Cao, Xia
 Xu, Ximing
 TI Preparation and In Vitro Evaluation of Povidone-Sodium
 Cholate-Phospholipid Mixed Micelles for the Solubilization of Poorly
 Soluble Drugs
 SO ARCHIVES OF PHARMACAL RESEARCH
 AB Mixed micelles made of polyvinylpyrrolidone (PVP), sodium cholate, and
 phospholipids were prepared to improve the solubility of poorly
 water-soluble drugs. Sylibin, a drug used in treating liver diseases,
 was incorporated into the mixed micelles. The formulation of sylibin
 containing PVP-sodium cholate-phospholipid mixed micelles with an
 optimized composition (PVP/sodium cholate/phospholipid/silybin =
 3:3:4:1 similar to 2 by weight) was obtained based on the study of
 pseudoternary phase diagrams. The critical micelle concentration was
 used to evaluate the micellar stability towards dilution. The results
 showed that addition of PVP to sodium-cholate-phospholipid mixed
 micelles increased stability. The solubility of sylibin in PVP-sodium
 cholate-phospholipid mixed micelles was higher than that in pure water
 or in sodium cholate-phospholipid mixed micelles. In a stability study,
 we found that PVP-sodium cholate-phospholipid mixed micelles showed
 good stability. After 3 months storage at 40 degrees C, just 2.6%
 sylibin was lost with only minor changes of the particle size when
 compared to a reference formulation containing sodium cholate and
 phospholipid mixed micelles. In addition, the developed formulation
 significantly improved in vitro drug release. The time required to
 release 50% sylibin (t50%) from sodium cholate and phospholipid mixed
 micelles was 326 h, while the t50% from PVP-sodium cholate-phospholipid
 mixed micelles was only 51.1 h. Our results suggest that these mixed
 micelles might have significant potential application to the
 biomedical field.
 SN 0253-6269
 PD JUN
 PY 2010
 VL 33
 IS 6
 BP 911
 EP 917
 DI 10.1007/s12272-010-0614-6
 UT ISI:000279357300015
 PT J
 AU Li, H
 Sun, ZY
 Zhong, WY
 Hao, N
 Xu, DK
 Chen, HY
 AF Li, Hui
 Sun, Ziyin
 Zhong, Wenying
 Hao, Nan
 Xu, Danke
 Chen, Hong-Yuan
 TI Ultrasensitive Electrochemical Detection For DNA Arrays Based on
 Silver Nanoparticle Aggregates
 SO ANALYTICAL CHEMISTRY
 AB Multiplexed DNA target detection is of great significance in many
 fields including clinical diagnostics, environmental monitoring,
 biothreat detection and forensics. Although the emergence of DNA chip
 technology has accelerated this process, it is still a challenge to
 perform ultrasensitive DNA assay at low attomol concentrations so that
 DNA detection can be directly achieved without a PCR protocol. In this
 work, an oligonucleotide-functionalized silver nanoparticle tag has
 been successfully developed for multiplexed DNA electrochemical
 detection with ultrahigh sensitivity. The multiprobes containing
 oligo(d)A and the reporting probes were anchored onto the silver
 nanopartides, followed by hybridizing with the silver nanoparticle
 conjugate modified with oligo(d)T. The-hybridization-induced tag was
 found to show an aggregated nanostructare 10 times larger than the
 individual nanoparticle, as revealed by TEM. For sandwich-based
 assays, the tag was specifically coupled to a gold electrode surface
 via target DNA. Compared to a single nanoparticle label, this novel
 tag has shown excellent electroactive property and produces 10(3)-fold
 amplification in the differential pulse voltammetric (DPV) method.
 Hepatitis B virus (HBV) sequence was employed as a sample model, and
 we have achieved a detection limit of 5 aM (similar to 120 molecules
 in 40 mu L volume), demonstrating ultrasensitive measurement for DNA.
 The property of the electrochemical process involving silver
 aggregates was further investigated and the integrative oxidation of
 the silver tag was observed. We further demonstrated the multiplexed
 DNA target detection using array chips functionalized with Herpes
 simplex virus (HSV), Epstein Barr-virus (EBV) and cytomegalovirus
 (CMV) sequences, which shows effective recognition of the relative
 sequences individually or simultaneously. The method offers a uniquely
 new approach for DNA detection with ultrahigh sensitivity as well as
 advantages of rapidity, throughput, and miniaturization.
 SN 0003-2700
 PD JUL 1
 PY 2010
 VL 82
 IS 13
 BP 5477
 EP 5483
 DI 10.1021/ac101193e
 UT ISI:000279253300014
 PT J
 AU Li, J
 Zhang, LA
 Jiang, ZZ
 Shu, B
 Li, F
 Bao, QL
 Zhang, LY
 AF Li, Ji
 Zhang, Liang
 Jiang, Zhenzhou
 Shu, Bin
 Li, Fu
 Bao, Qingli
 Zhang, Luyong
 TI Toxicities of aristolochic acid I and aristololactam I in cultured
 renal epithelial cells
 SO TOXICOLOGY IN VITRO
 AB Aristolochic acid nephropathy, a progressive tubulointerstitial renal
 disease, is primarily caused by aristolochic acid I (AA-I)
 intoxication. Aristololactam I (AL-I), the main metabolite of AA-I,
 may also participate in the processes that lead to renal damage. To
 investigate the role and mechanism of the AL-I-mediated cytotoxicity,
 we determined and compared the cytotoxic effects of AA-I and AL-I on
 cells of the human proximal tubular epithelial (HK-2) cell line. To
 this end, we treated HK-2 cells with AA-I and AL-I and assessed the
 cytotoxicity of these agents by using the
 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MU)
 assay, flow cytometry, and an assay to determine the activity of caspase
 3. The proliferation of HK-2 cells was inhibited in a concentrationand time-dependent manner. Cell-cycle analysis revealed that the cells
 were arrested in the S-phase. Apoptosis was evidenced by the results
 of the annexin V/propidium iodide (PI) assay and the occurrence of a
 sub-G1 peak. In addition, AA-I and AL-I increased caspase 3-like
 activity in a concentration-dependent manner. These results also
 suggested that the cytotoxic potency of AL-I is higher than that of
 AA-I and that the cytotoxic effects of these molecules are mediated
 through the induction of apoptosis in a caspase 3-dependent pathway.
 (C) 2010 Published by Elsevier Ltd.
 SN 0887-2333
 PD JUN
 PY 2010
 VL 24
 IS 4
 BP 1092
 EP 1097
 DI 10.1016/j.tiv.2010.03.012
 UT ISI:000279124900006
 PT J
 AU Zhong, QF
 Sun, LP
 AF Zhong, Qi-Fei
 Sun, Li-Ping
 TI An efficient synthesis of 6,9-disubstituted purin-8-ones via
 copper-catalyzed coupling/cyclization
 SO TETRAHEDRON
 AB An efficient and novel synthesis of 6,9-disubstituted purin-8-ones has
 been developed. Starting from dichloropyrimidin-5-ylcarbamate,
 CuCl/amino acid catalyzed coupling/cyclization reaction with amines
 was achieved to afford 9-substituted 6-chloropurin-8-ones. Then a
 microwave-assisted amination procedure was carried out for the
 synthesis of 6,9-disubstituted purin-8-ones in moderate to good
 yields. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0040-4020
 PD JUL 3
 PY 2010
 VL 66
 IS 27-28
 BP 5107
 EP 5111
 DI 10.1016/j.tet.2010.04.106
 UT ISI:000279126700026
 PT J
 AU Cirioni, O
 Wu, GQ
 Li, LX
 Orlando, F
 Silvestri, C
 Ghiselli, R
 Shen, ZL
 Scalise, A
 Gabrielli, E
 Scuppa, D
 Romiti, C
 Provinciali, M
 Guerrieri, M
 Giacometti, A
 AF Cirioni, Oscar
 Wu, Guoqiu
 Li, Linxian
 Orlando, Fiorenza
 Silvestri, Carmela
 Ghiselli, Roberto
 Shen, Zilong
 Scalise, Alessandro
 Gabrielli, Eleonora
 Scuppa, Daniele
 Romiti, Chiara
 Provinciali, Mauro
 Guerrieri, Mario
 Giacometti, Andrea
 TI S-thanatin enhances the efficacy of tigecycline in an experimental rat
 model of polymicrobial peritonitis
 SO PEPTIDES
 AB We investigated the efficacy of the peptide s-thanatin alone and in
 combination with tigecycline in an animal model of sepsis induced by
 cecal ligation and puncture. Adult male Wistar rats were randomized
 to receive intravenously isotonic sodium chloride solution, 5 mg/kg
 s-thanatin, 2 mg/kg tigecycline, 5 mg/kg s-thanatin combined with 2
 mg/kg tigecycline. The experiment was also performed with
 administration of the drugs 360 min after the surgical procedure to
 better investigate the clinical situation where there is an interval
 between the onset of sepsis and the initiation of therapy. Lethality,
 bacterial growth in blood, peritoneum, spleen and liver, and NO indices
 were evaluated. All compounds reduced the lethality when compared to
 control. In all experiments, the compounds reduced significantly
 bacterial growth and lethality compared with saline treatment.
 Treatment with s-thanatin resulted in significant decrease in plasma
 NO levels compared to tigecycline and control group. The combination
 between s-thanatin and tigecycline proved to be the most effective
 treatment in reducing all variables measured. S-thanatin may have
 potential therapeutic usefulness alone and when associated to
 tigecycline in polymicrobial peritonitis. (C) 2010 Elsevier Inc. All
 rights reserved.
 SN 0196-9781
 PD JUL
 PY 2010
 VL 31
 IS 7
 BP 1231
 EP 1236
 DI 10.1016/j.peptides.2010.03.034
 UT ISI:000279078700002
 PT J
 AU Geng, Y
 Xiang, BR
 AF Geng, Ying
 Xiang, Bingren
 TI Net analyte signal based two-dimensional (NAS 2D) correlation near
 infrared spectroscopy
 SO JOURNAL OF MOLECULAR STRUCTURE
 CT 5th International Symposium on Two Dimensional Correlation
 Spectroscopy
 CY AUG 05-07, 2009
 CL Wroclaw, POLAND
 AB A new method of analysis, based on the net analyte signal presented
 by Lorber is proposed for the two-dimensional correlation near infrared
 spectroscopy. A spectra data set under the static perturbation of
 concentration was collected. NAS is manipulated for removing the
 information that was unrelated to a certain analyte. To demonstrate
 the potential of NAS 2D correlation spectroscopy, a set of
 concentration-dependent near infrared spectra of Sinomenine
 Hydrochloride in methanol was used as an example. The results show that
 NAS 2D, reconstructed from a series of principal factors can extract
 more subtle and useful spectra features, and make the band assignment
 explicable for structure analysis. (C) 2010 Elsevier B.V. All rights
 reserved.
 SN 0022-2860
 PD JUN 16
 PY 2010
 VL 974
 IS 1-3
 SI Sp. Iss. SI
 BP 173
 EP 178
 DI 10.1016/j.molstruc.2010.03.023
 UT ISI:000279029300027
 PT J
 AU Sun, W
 Du, YX
 Wang, YQ
 AF Sun, Wen
 Du, Yingxiang
 Wang, Yunqing
 TI Study on fluorescence properties of carbogenic nanoparticles and their
 application for the determination of ferrous succinate
 SO JOURNAL OF LUMINESCENCE
 AB A new type of fluorescent nanomaterial named carbogenic nanoparticles
 (NPs) has drawn considerable attention recently. In this study, we
 adopted a direct and simple synthetic method to produce the carbogenic
 NPs and investigated the fluorescence properties of the as-prepared
 carbogenic NPs in detail. It was found that the fluorescence of
 carbogenic NPs was stable with the variance of environmental conditions
 such as pH, temperature and UV irradiation. More interestingly, we
 found carbogenic NPs exhibited high selectivity and sensitivity
 towards ferric ions. Under optimum conditions, a good linear
 relationship could be obtained between the fluorescence intensity and
 concentration of ferric ions in the range of 5.0 x 10(-5)-5.0 x 10(-4)
 mol L-1, and the limit of detection is 11.21 mu mol L-1. Based on the
 fluorescence quenching of carbogenic NPs, a rapid and specific
 quantitative method was proposed for the determination of ferrous
 succinate. The content of ferrous succinate in commercial tablets
 determined by the present method was agreed with the spectrophotometric
 method results and the reproducibility and the recovery of the proposed
 method were satisfactory. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0022-2313
 PD AUG
 PY 2010
 VL 130
 IS 8
 BP 1463
 EP 1469
 DI 10.1016/j.jlumin.2010.03.013
 UT ISI:000279139300024
 PT J
 AU Wu, Y
 Li, XD
 Lin, RC
 Jin, SH
 AF Wu, Yi
 Li, Xiao D.
 Lin, Rui C.
 Jin, Shao H.
 TI Development of a Size-Exclusion HPLC Method with Evaporative
 Light-Scattering Detection for the Quantitation of Polysorbate 80 in
 Houttuynia cordata Injection
 SO JOURNAL OF AOAC INTERNATIONAL
 AB A rapid and accurate size-exclusion HPLC method for the quantitation
 of polysorbate 80 (PS80) in Houttuynia cordata injection, a Chinese
 traditional medicine, was developed and validated. The assay was
 conducted on an Agilent 1100 HPLC system with a TosoHaas TSKgel G2000
 SWXL column (30 cm x 7.8 mm, 5 mu m particle size) and an Alltech
 evaporative light-scattering detector (ELSD) 2000. The mobile phase
 was 20 mmoL/L ammonium acetate-acetonitrile (90 + 10, v/v) delivered
 at a flow rate of 0.6 mL/min under isocratic conditions. The ELSD was
 operated in the impactor "off" mode, the drift tube temperature was
 set at 110 degrees C, and nitrogen flow was maintained at 2.3 L/min.
 The LOD was 0.25 mg/mL. Linearity was obtained between the log of
 concentration (C) and the log of peak area (Y) of PS80 in the range
 of 0.5-20 mg/mL according to the equation: Log Y = 1.4529 Log C 0.8232
 (r(2) = 0.9976). An RSD of 1.6% (n = 6) for the determination
 demonstrated the good precision of the optimized method. PS80 content
 in several commercial H. cordata injection products from different
 manufacturers was determined. The data for PS80 content is useful in
 evaluation of the safety of the products from different manufacturers.
 SN 1060-3271
 PD MAY-JUN
 PY 2010
 VL 93
 IS 3
 BP 917
 EP 921
 UT ISI:000279140000026
 PT J
 AU Zhou, YY
 Du, YZ
 Wang, L
 Yuan, H
 Zhou, JP
 Hu, FQ
 AF Zhou, Yue-Yu
 Du, Yong-Zhong
 Wang, Ling
 Yuan, Hong
 Zhou, Jian-Ping
 Hu, Fu-Qiang
 TI Preparation and pharmacodynamics of stearic acid and poly
 (lactic-co-glycolic acid) grafted chitosan oligosaccharide micelles
 for 10-hydroxycamptothecin
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB Stearic acid (SA) and poly (lactic-co-glycolic acid) (PLGA) grafted
 chitosan oligosaccharide (SA-CSO-PLGA SCP) tripolymer was synthesized
 via the reaction between the carboxyl group of SA or PLGA with
 carboxylic side group, and the amine group of CSO in the presence of
 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC). The degrees of
 amino-substitution for SA and PLGA were assayed through 2, 4,
 6-trinitrobenzene sulfonic acid (TNBS) test and C-13 NMR spectrum,
 which were 8.15% and 5.82%, respectively; the critical micelle
 concentrations of SCP in PBS (pH 7.4) and deionized water (DI water)
 were about 34.9 and 14.5 mu g/ml, respectively. Using
 10-hydroxycamptothecin (HCPT) as a model drug, the drug-loaded
 micelles showed above 86% encapsulation efficiency, which not only
 enhanced the solubility of HCFT in aqueous medium markedly, but also
 protected the lactone ring of HCPT. Cellular uptakes of SCP micelles
 against A549, MCF-7 and HepG-2 tumor cells showed a faster cellular
 internalization. Comparing to the commercial HCFT injection,
 HCPT-loaded micelles showed higher cytotoxicities against A549, MCF-7
 and HepG-2 cells. The increased folds were 22, 18 and 15, respectively.
 These results suggested the SCP could be applied as a carrier for
 hydrophobic drugs. (c) 2010 Elsevier B.V. All rights reserved.
 SN 0378-5173
 PD JUN 30
 PY 2010
 VL 393
 IS 1-2
 BP 143
 EP 151
 DI 10.1016/j.ijpharm.2010.04.025
 UT ISI:000279208700018
 PT J
 AU Luo, YD
 Wu, SS
 Li, XY
 Li, P
 AF Luo, Yongdong
 Wu, Shuisheng
 Li, Xiaoyan
 Li, Ping
 TI LC-ESI-MS-MS Determination of Rat Plasma Protein Binding of Major
 Flavonoids of Flos Lonicerae Japonicae by Centrifugal Ultrafiltration
 SO CHROMATOGRAPHIA
 AB Centrifugal ultrafiltration (CU) and a fast liquid chromatography with
 electrospray ionization tandem mass spectrometric (LC-ESI-MS-MS)
 method have been developed for drug-protein binding analysis of four
 flavonoids of Flos Lonicerae Japonicae (FLJ). A rapid separation of
 free drug from the plasma was achieved by CU and the simultaneous
 analysis of four flavonoids of FLJ in rat plasma was by fast
 LC-ESI-MS-MS. The chromatographic analytical time decreased to 6.5 min
 without sacrificing resolution using a 4.6 mm x 50 mm, 1.8 mu m particle
 size reverse phase column and MS-MS mode performed for multiple
 reaction monitoring (MRM). The protein binding rates of four flavonoids
 were in the range of 66.8 +/- A 7.4 to 81.3 +/- A 5.1% after oral
 administration of the flavonoid fraction of FLJ. All values were almost
 similar to 70.0% at 30, 45 and 80 min. Its result suggests that these
 flavonoids in rat plasma perform high protein binding rates and present
 a stable binding in a longer time. Meanwhile, it reveals that the
 elimination of these flavonoids may be relatively moderate in the body,
 the performance of a certain degree of accumulation may be speculated
 and make further impacts on the pharmacokinetic parameters.
 SN 0009-5893
 PD JUL
 PY 2010
 VL 72
 IS 1-2
 BP 71
 EP 77
 DI 10.1365/s10337-010-1618-6
 UT ISI:000279026300010
 PT J
 AU Zhang, Q
 Liang, JY
 Li, QS
 Min, ZD
 AF Zhang, Qiong
 Liang, Jing Yu
 Li, Qing Shan
 Min, Zhi Da
 TI New limonoids from the fruits of Melia toosendan
 SO CHINESE CHEMICAL LETTERS
 AB Two new limonoids, 1 alpha-Tigloyloxy-3 alpha-acetoxyl-7
 alpha-hydroxyl-12 alpha-ethoxyl nimbolinin (1) and1
 alpha-Benzoyloxy-3 alpha-acetoxyl-7 alpha-hydroxyl-12 alpha-ethoxyl
 (2), were isolated from the fruits of Melia toosendan. Their structures
 were established on the basis of various NMR spectroscopic analyses,
 including 2D-NMR techniques (HSQC, HMBC, NOESY) and HR-ESI-MS. (C) 2010
 Qiong Zhang. Published by Elsevier B.V. on behalf of Chinese Chemical
 Society. All rights reserved.
 SN 1001-8417
 PD JUL
 PY 2010
 VL 21
 IS 7
 BP 838
 EP 841
 DI 10.1016/j.cclet.2010.02.018
 UT ISI:000279039000022
 PT J
 AU Zhang, F
 Fang, CG
 Wu, YT
 Wang, YT
 Li, AM
 Zhang, ZB
 AF Zhang Feng
 Fang Cheng-Gang
 Wu You-Ting
 Wang Yuan-Tao
 Li Ai-Min
 Zhang Zhi-Bing
 TI Absorption of CO2 in the aqueous solutions of functionalized ionic
 liquids and MDEA
 SO CHEMICAL ENGINEERING JOURNAL
 AB Four ionic liquids (ILs) tetramethylammonium glycinate (=[Gly]),
 tetraethylammonium glycinate ([N-2222][Gly])), tetramethylammonium
 lysinate ([N-1111][Lys]) and tetraethylammonium lysinate
 ([N-2222][Lys]) were synthesized and mixed with water or
 N-methyldiethanolamine (MDEA) aqueous solutions to form a new type of
 solvents for the uptake of CO2. The solubility or absorption of CO2
 in these IL+MDEA aqueous solutions was investigated over a wide range
 of IL concentrations (5-100%), temperature (298-318 K) and partial
 pressure of CO2 (4-400 kPa). The results indicated that ionic liquid
 could greatly enhance the absorption and increased the absorption rate
 of CO2 in MDEA aqueous solutions. It had been found that the aqueous
 solutions of 15% IL and 15% MDEA had higher absorption rate and larger
 uptake than other IL+MDEA solutions of 30% total amines. Temperature
 (298-318 K) seemed to have some influence on the absorption of CO2 in
 IL+MDEA aqueous solutions. Noticeably, due to the two amino groups in
 a molecular, the mole absorption of the 30% lysine based ionic liquids
 aqueous solutions was 0.98 ([N-1111][Lys]) and 1.21 ([N-2222][Lys])
 mole CO2, being about 2-3 times the absorption capacity of MDEA under
 the same condition. Regeneration under the condition of temperature
 353 K. 4 kPa for 240 min showed that aqueous solution of 15% IN, 15%
 MDEA had significant regeneration efficiency (over 98%). (c) 2010
 Elsevier B.V. All rights reserved.
 SN 1385-8947
 PD JUN 1
 PY 2010
 VL 160
 IS 2
 BP 691
 EP 697
 DI 10.1016/j.cej.2010.04.013
 UT ISI:000279137900037
 PT J
 AU Chen, JH
 Zhang, XG
 Jiang, YT
 Yan, LY
 Tang, L
 Yin, YW
 Cheng, DS
 Chen, J
 Wang, M
 AF Chen, Jian-Hua
 Zhang, Xin-Guo
 Jiang, Yu-tao
 Yan, Lu-Ying
 Tang, Li
 Yin, Yi-Wei
 Cheng, Dai-Shuang
 Chen, Jing
 Wang, Min
 TI Bioactivity and pharmacokinetics of two human serum albumin-thymosin
 alpha 1-fusion proteins, rHSA-T alpha 1 and rHSA-L-T alpha 1, expressed
 in recombinant Pichia pastoris
 SO CANCER IMMUNOLOGY IMMUNOTHERAPY
 AB Thymosin-alpha 1 (T alpha 1) is indicated for the treatment of certain
 viral infections, including hepatitis B and C, and cancers, such as
 melanoma. In this paper, the fusion genes encoding human serum albumin
 (HSA) and T alpha 1 with (rHSA-L-T alpha 1) and without a linker peptide
 (rHSA-T alpha 1) were constructed and overexpressed in P. pastoris.
 Through the process of ion interaction chromatography (Q-Sepharose
 F.F), hydrophobic interaction chromatography (Phenyl Sepharose HP) and
 affinity chromatography (Blue Sepharose F.F), the purity of fusion
 proteins was greater than 97%. In contrast to the reactivity of normal
 spleen cells to Con A, the data of in vitro murine spleen lymphocytes
 proliferation experiment suggested that spleen cells achieved a higher
 degree of T cell maturation after rHSA-L-T alpha 1, rHSA-T alpha 1 and
 T alpha 1 treatments, respectively. Moreover, rHSA-L-T alpha 1, rHSA-T
 alpha 1 and T alpha 1 can also antagonize dexamethasone-induced
 apoptosis of thymocyte sub-populations. In hydrocortisone-induced
 immunosuppression mice (in vivo experiments), after subcutaneous
 injections with two fusion proteins and T alpha 1 for seven consecutive
 days, the net increment of body weight, the spleen index and the thymus
 index were significantly improved. Simultaneously, the increase in SOD
 level and the decrease in MDA level in plasma were observed. The
 pharmacokinetic data of rHSA-L-T alpha 1 and rHSA-T alpha 1
 administered in rats showed an improved pharmacokinetic profile with
 a conspicuous prolonged half life. The analysis of bioactivity and
 pharmacokinetics suggested that fusion proteins rHSA-L-T alpha 1 and
 rHSA-T alpha 1 were new drug candidates.
 SN 0340-7004
 PD SEP
 PY 2010
 VL 59
 IS 9
 BP 1335
 EP 1345
 DI 10.1007/s00262-010-0862-9
 UT ISI:000279198000004
 PT J
 AU Ma, L
 Ji, JL
 Ji, H
 Yu, X
 Ding, LJ
 Liu, K
 Li, YQ
 AF Ma, L.
 Ji, J. L.
 Ji, H.
 Yu, X.
 Ding, L. J.
 Liu, K.
 Li, Y. Q.
 TI Telmisartan alleviates rosiglitazone-induced bone loss in
 ovariectomized spontaneous hypertensive rats
 SO BONE
 AB In the present study, we systematically examined telmisartan, an
 angiotensin AT(1) receptor antagonist, on rosiglitazone-induced bone
 loss in ovariectomized spontaneously hypertensive rats. Telmisartan
 (5 mg/kg/d, 90 days) was found to be able to significantly alleviate
 rosiglitazone (10 mg/kg/d, 90 days)-induced decrease in BMD of femur
 and lumbar vertebrae. The BMD changes were associated with positive
 biomechanical changes of lumbar vertebrae, improvements in
 microarchitecture of tibial metaphysic and normalized serum
 osteocalcin (OC) levels and urinary deoxypyridinoline/creatinine
 (DPD/Cr) ratio. MicroCT analysis of the tibial metaphysis showed that
 telmisartan significantly prevented the decreases in bone
 volume/tissue volume (BV/TV), connect density (Conn. D.), trabecular
 number (Tb. N.) and trabecular thickness (Tb. Th.), and increase in
 trabecular separation (Tb. Sp.) induced by rosiglitazone.
 Histomorphometric analysis also showed that telmisartan had protective
 effects on rosiglitazone-reduced bone formation indices such as
 histomorphometric bone volume fraction (BV/TV-Histo), mineralizing
 surface/bone surface (MS/BS), mineral apposition rate (MAR) and bone
 formation rate (BFR/BS). Our study clearly showed that telmisartan
 alleviated rosiglitazone-induced bone loss in ovariectomized
 spontaneous hypertensive rats. The relief of bone loss provides a
 possible therapeutic application of telmisartan with rosiglitazone for
 the treatment of elderly women patients afflicted with metabolic
 syndrome. (C) 2010 Elsevier Inc. All rights reserved.
 SN 8756-3282
 PD JUL
 PY 2010
 VL 47
 IS 1
 BP 5
 EP 11
 DI 10.1016/j.bone.2010.03.016
 UT ISI:000279150400001
 PT J
 AU Sun, L
 Lin, SS
 Zhao, RP
 Yu, BY
 Yuan, ST
 Zhang, LY
 AF Sun, Li
 Lin, Sensen
 Zhao, Renping
 Yu, Boyang
 Yuan, Shengtao
 Zhang, Luyong
 TI The Saponin Monomer of Dwarf Lilyturf Tuber, DT-13, Reduces Human
 Breast Cancer Cell Adhesion and Migration during Hypoxia via Regulation
 of Tissue Factor
 SO BIOLOGICAL & PHARMACEUTICAL BULLETIN
 AB Adhesion and migration of tumor cells are crucial steps in tumor
 invasion and metastasis. In the present study, we investigated the
 effects of saponin monomer 13 of dwarf lilyturf tuber (DT-13) on
 metastasis of human breast cancer cells (MDA-MB-435) during hypoxia.
 The effects and molecular mechanisms of DT-13 on MDA-MB-435 cells
 metastatic phenotype in vitro and in vivo were evaluated by RNA
 interference; quantitative real-time polymerase chain reaction
 (qRT-PCR) and Western blot assays. DT-13 had no significant effects
 on cell adhesion and migration under normoxia conditions. Under hypoxic
 conditions, IVIDA-MB-435 adhesion to vitronectin was inhibited by
 about 43.5% or 60.8% after exposure of the cells to DT-13 at 1 mu M
 or 10 mu M, respectively. DT-13 decreased the migratory response by
 hypoxia at 1 or 10 mu M, and inhibition ratios were 20% and 30%,
 respectively. DT-13 inhibited hypoxia-induced expression of alpha v
 beta 3 integrin, tissue factor (TF) and early growth response gene-1
 (Egr-1) and decreased excretion of matrix metalloproteinase 9 (MMP-9)
 of MDA-MB-435 cells under hypoxic conditions. After Egr-1 short
 interference RNA (siRNA) treatment, DT-13 could still inhibit the
 up-regulation of TF mRNA and protein levels and its pro-coagulant
 activity (PCA) under hypoxia. In nude mice, DT-13 decreased
 extravasation of MDA-MB-435 cells in the lung after tail vein
 injection. Our data suggest that DT-13 inhibits MDA-MB-435 cells
 metastasis during hypoxia via regulation of TF, and the effect of DT-13
 on TF is partly mediated by Egr-1.
 SN 0918-6158
 PD JUL
 PY 2010
 VL 33
 IS 7
 BP 1192
 EP 1198
 UT ISI:000279199800019
 PT J
 AU Lu, ML
 Cao, X
 Yang, X
 Zheng, H
 Liu, N
 Jiang, Y
 Lin, DH
 Chen, YJ
 AF Lu, Meiling
 Cao, Xu
 Yang, Xin
 Zheng, Heng
 Liu, Nan
 Jiang, Yun
 Lin, Donghai
 Chen, Yijun
 TI A diketoreductase exhibits unique renaturation profile from
 thermal-induced protein unfolding
 SO AMINO ACIDS
 AB Proteins can refold from thermal-induced denaturation.
 Apo-diketoreductase exhibited a unique refolding profile, in which the
 degree of refolding from higher temperature was more complete. Partial
 aggregation and structural change may provide possible explanation on
 this phenomenon.
 SN 0939-4451
 PD JUL
 PY 2010
 VL 39
 IS 2
 BP 609
 EP 613
 DI 10.1007/s00726-010-0491-9
 UT ISI:000279190400032
 PT J
 AU Cheng, YS
 Dai, DZ
 Dai, Y
 AF Cheng, Yu-Si
 Dai, De-Zai
 Dai, Yin
 TI Testis dysfunction by isoproterenol is mediated by upregulating
 endothelin receptor A, leptin and protein kinase C epsilon and is
 attenuated by an endothelin receptor antagonist CPU0213
 SO REPRODUCTIVE TOXICOLOGY
 AB This study has examined whether upregulation of endothelin receptor
 A, leptin and phosphorylated protein kinase C epsilon contributes to
 stress-induced testicular damaged and its possible reversal by
 endothelial (ET) antagonism. Adult male Sprague-Dawley rats were
 randomly divided into control and isoproterenol (ISO 1 mg/kg,
 subcutaneous (s.c.), 10 days) groups, and intervened with the ET
 receptor antagonist CPU0213 (20 mg/kg, s.c.), on days 6-10. In ISO
 group, testicular succinate dehydrogenase, lactate dehydrogenase,
 acid phosphotase, and gamma-glutamyl transpeptidase, and serum
 testosterone decreased, whereas FSH increased, relative to control.
 The seminiferous tubules were damaged in association with testicular
 upregulation of protein abundance of leptin and pPKC epsilon, and mRNA
 and protein expression of leptin receptor (OBRb) and ETA. CPU0213 was
 effective in ameliorating these abnormalities. Over-expression of ETA
 and leptin accounting for the testis dysfunction is likely to be
 mediated by pPKC epsilon in the ISO treated rats. The upregulated ET
 pathway appears to be critical in pathologies of the testis. (C) 2010
 Elsevier Inc. All rights reserved.
 SN 0890-6238
 PD JUL
 PY 2010
 VL 29
 IS 4
 BP 421
 EP 426
 DI 10.1016/j.reprotox.2010.03.001
 UT ISI:000278951900006
 PT J
 AU Xu, FG
 Liu, Y
 Song, R
 Dong, HJ
 Zhang, ZJ
 AF Xu, Fengguo
 Liu, Ying
 Song, Rui
 Dong, Haijuan
 Zhang, Zunjian
 TI HPLC/DAD Comparison of Sixteen Bioactive Components Between
 Da-Cheng-Qi Decoction and its Parent Herbal Medicines
 SO NATURAL PRODUCT COMMUNICATIONS
 AB Differences in the contents of sixteen bioactive components (three
 tannins, five anthraquinones, six flavonoids and two neolignans)
 between Da-Cheng-Qi decoction (DCQD) and its three constitutional
 herbal medicines (Radix et Rhizoma Rhei, Cortex Magnoliae officinalis,
 and Fructus Aurantii Immaturus) were compared using validated HPLC/DAD
 methods. The results indicated that there existed some kinds of
 interactions between these constitutional natural medicines during the
 DCQD preparation procedure, which could either enhance or depress the
 extractive rates of bioactive components.
 SN 1934-578X
 PD JUN
 PY 2010
 VL 5
 IS 6
 BP 893
 EP 896
 UT ISI:000278891800014
 PT J
 AU Liang, Y
 Kang, A
 Xie, T
 Zheng, XA
 Dai, C
 Hao, HP
 A, JY
 Sheng, LS
 Xie, L
 Wang, GJ
 AF Liang, Yan
 Kang, An
 Xie, Tong
 Zheng, Xiao
 Dai, Chen
 Hao, Haiping
 A, Jiye
 Sheng, Longsheng
 Xie, Lin
 Wang, Guang-ji
 TI Influence of segmental and selected ion monitoring on quantitation of
 multi-component using high-pressure liquid chromatography-quadrupole
 mass spectrometry: Simultaneous detection of 16 saponins in rat plasma
 as a case
 SO JOURNAL OF CHROMATOGRAPHY A
 AB Quadrupole (Q) mass spectrometers are the most popular analytical tools
 due to their reliability, effectiveness, and low cost. However, they
 are not suitable for quantitative analysis of multi-component since
 the sensitivity will get worse rapidly with the increasing number of
 m/z detected. The present work, for the first time, attempted to analyze
 of 16 saponins simultaneously using an approach of segmental and
 selected ion monitoring (SSIM) based on LC-Q/MS, and systematically
 investigated the influence of different SSIM modes on signal
 level/noise level (S/N), lower limits of quantification (LLOQ), upper
 limits of quantification (ULOQs), etc. Our results showed that a proper
 SSIM mode could not only provide much higher sensitivity for all the
 targeting analytes, but also dramatically broadened their dynamic
 ranges. The developed methodology could effectively break the
 application bottleneck on the quantitative analysis of multi-component
 with LC-Q/MS, and would be applied widely in related fields for
 multi-component analysis, such as environmental monitoring,
 metabonomics, Chinese herbal medicine research. (C) 2010 Elsevier B.V.
 All rights reserved.
 SN 0021-9673
 PD JUN 25
 PY 2010
 VL 1217
 IS 26
 BP 4501
 EP 4506
 DI 10.1016/j.chroma.2010.04.054
 UT ISI:000278920900033
 PT J
 AU Chen, X
 Luo, JG
 Kong, LY
 AF Chen, Xia
 Luo, Jian-Guang
 Kong, Ling-Yi
 TI Two new triterpenoid saponins from Dianthus superbus L.
 SO JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
 AB Two new triterpenoid saponins (1 and 2) were isolated from the dried
 aerial parts of Dianthus superbus L. (Caryophyllaceae). Their
 structures were elucidated on the basis of spectral data to be
 3-O--D-glucopyranosyl olean-9(11),12-diene-23,28-dioic acid
 28-O--D-glucopyranoside (1) and 3-O--D-glucopyranosyl
 olean-11,13(18)-diene-23,28-dioic acid 28-O--D-glucopyranoside (2).
 SN 1028-6020
 PY 2010
 VL 12
 IS 6
 BP 458
 EP 463
 DI 10.1080/10286020.2010.493326
 UT ISI:000278787000007
 PT J
 AU Zan, K
 Zhou, SX
 Chen, XQ
 Fu, Q
 Tu, PF
 AF Zan, Ke
 Zhou, Si-Xiang
 Chen, Xiao-Qing
 Fu, Qiang
 Tu, Peng-Fei
 TI Prostaglandin-like fatty acid derivatives from Artemisia anomala
 SO JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
 AB Four prostaglandin-like fatty acid derivatives anomalone A-D (1-4)
 were isolated from the aerial part of Artemisia anomala S. Moore. Their
 structures were determined on the basis of extensive spectroscopic
 analyses.
 SN 1028-6020
 PY 2010
 VL 12
 IS 6
 BP 492
 EP 497
 DI 10.1080/10286020.2010.489825
 UT ISI:000278787000012
 PT J
 AU Xu, D
 Wang, F
 Gu, HY
 Wang, J
 Guo, QL
 Zhang, YL
 Wang, ZY
 AF Xu, Dan
 Wang, Feng
 Gu, Hongyan
 Wang, Jia
 Guo, Qinglong
 Zhang, Yanli
 Wang, Ziyu
 TI Hybrid cells differentiate to hepatic lineage cells and repair
 oxidative damage
 SO CELLULAR & MOLECULAR BIOLOGY LETTERS
 AB Hybrid cells derived from stem cells play an important role in
 organogenesis, tissue regeneration and cancer formation. However, the
 fate of hybrid cells and their range of function are poorly understood.
 Fusing stem cells and somatic cells induces somatic cell reprogramming,
 and the resulting hybrid cells are embryonic stem cell-like cells.
 Therefore, we hypothesize that fusion-induced hybrid cells may behave
 like ES cells in certain microenvironments. In this study, human
 hepatic cells were induced to apoptosis with H2O2, and then co-cultured
 with hybrid cells that had been derived from mouse ES cells and human
 hepatic cells using a transwell. After co-culturing, the degree of
 apoptosis was evaluated using Annexin-V/PI double-staining analysis,
 flow cytometry and Western-blot. We observed that H2O2-induced cell
 apoptosis was inhibited by co-culture. In addition, the activity of
 injury-related enzymes (GSH-Px, LDH and SOD) and the level of albumin
 release in the co-culture system trended toward the level of normal
 undamaged hepatic cells. The stably increased levels of secretion of
 ALB in the co-culture system also confirmed that co-culture with hybrid
 cells helped in recovery from injury. The fate of the hybrid cells was
 studied by analyzing their gene expression and protein expression
 profiles. The results of RT-PCR indicated that during co-culturing,
 like ES cells, hybrid cells differentiated into hepatic lineage cells.
 Hybrid cells transcripted genes from both parental cell genomes. Via
 immunocytochemical analysis, hepatic directional differentiation of
 the hybrid cells was also confirmed. After injecting the hybrid cells
 into the mouse liver, the GFP-labeled transplanted cells were
 distributed in the hepatic lobules and engrafted into the liver
 structure. This research expands the knowledge of fusion-related
 events and the possible function of hybrid cells. Moreover, it could
 indicate a new route of differentiation from pluripotent cells to
 tissue-specific cells via conditional co-culture.
 SN 1425-8153
 PD SEP
 PY 2010
 VL 15
 IS 3
 BP 451
 EP 472
 DI 10.2478/s11658-010-0018-0
 UT ISI:000278930100007
 PT J
 AU Shao, L
 Huang, J
 Jing, L
 Chen, JY
 Kan, SD
 Wang, M
 Li, JA
 Chen, DJ
 AF Shao, Lei
 Huang, Jia
 Jing, Lan
 Chen, Ji-Ye
 Kan, Shi-Dong
 Wang, Min
 Li, Ji-An
 Chen, Dai-Jie
 TI Overexpression of aveBIV leading to the improvement of
 4'-epidaunorubicin production in Streptomyces coeruleorubidus strain
 SIPI-A0707
 SO APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
 AB The 4'-epidaunorubicin is the semisynthesis precursor of epirubicin
 which is a clinically useful antitumor drug thought to have slightly
 less cardiotoxicity than doxorubin. The 4'-epidaunorubicin was formed
 by overexpression of heterologous Streptomyces avermitilis aveBIV in
 Streptomyces coeruleorubidus SIPI-A0707 dnmV mutant blocked in the
 biosynthesis of daunosamine, the deoxysugar component of daunorubicin.
 But there was a low-yield production of 4'-epidaunorubicin. In our
 study, product yields were enhanced considerably by increasing aveBIV
 gene copy number or changing means of aveBIV integration. The
 4'-epidaunorubicin titer was improved by around threefold in the
 recombinant strain DYG1006 with the aveBIV increased threefold copy
 numbers. The transcript levels of aveBIV gene meet the expectation of
 fermentation levels of 4'-epidaunorubicin. The method described here
 provides the means to produce 4'-epidaunorubicin efficiently on an
 industrial scale.
 SN 0175-7598
 PD JUL
 PY 2010
 VL 87
 IS 3
 BP 1057
 EP 1064
 DI 10.1007/s00253-010-2541-3
 UT ISI:000278810200022
 PT J
 AU Cui, YX
 Wu, ZM
 Liu, XX
 Ni, R
 Zhu, XX
 Ma, LL
 Liu, JP
 AF Cui, Yanxia
 Wu, Zimei
 Liu, Xiaoxu
 Ni, Rui
 Zhu, Xuanxuan
 Ma, Lulu
 Liu, Jianping
 TI Preparation, Safety, Pharmacokinetics, and Pharmacodynamics of
 Liposomes Containing Brucea javanica Oil
 SO AAPS PHARMSCITECH
 AB Brucea javanica oil-loaded liposomes (BJOL) were prepared through thin
 film hydration method and characterized by transmission electron
 microscope, dynamic light scattering, and differential scanning
 calorimetry. Acute toxicity of B. javanica oil (BJO) in liposomes was
 assessed by determining the number of deaths of Kunming mice over
 intravenous treatment for 2 weeks. The pharmacokinetic behavior of the
 main active component (oleic acid) was studied in SD rats. The
 pharmacodynamics of BJOL was investigated using MMC-7721 cell lines
 and mice with Lewis lung cancer. The commercial emulsion of BJO (BJOE)
 was used as a reference. The data showed that BJOL had an average
 diameter of 108.2 nm with a zeta potential of -57.0 mV, drug loading
 of 3.60%, and entrapment efficiency of 92.40%. The area under curve
 of BJO in liposomes and emulsions were 2.31 and 1.15 mg min/ml,
 respectively. Compared with BJOE, mean residence time and elimination
 half-time (t (1/2)) increased 2.8- and 4.0-fold, respectively, and the
 clearance (CL) decreased 0.5-fold. In the acute toxicity test, the
 median lethal dose (LD50) of BJOE was 7.35 g/kg. In contrast, all mice
 treated with liposomes survived even at the highest dosage (12.70
 g/kg). The IC50 value of BJOL group was one third of that of BJOE group
 (p < 0.01), and a less weight loss was observed in the BJOL-treated
 animals (p < 0.05). In conclusion, the present study suggests that BJOL
 significantly decreased toxicity of BJO and enhance the antitumor
 activity. Therefore, liposomes may be a potential effective delivery
 vehicle for this lipophilic antitumor drug.
 SN 1530-9932
 PD JUN
 PY 2010
 VL 11
 IS 2
 BP 878
 EP 884
 DI 10.1208/s12249-010-9454-4
 UT ISI:000278921400044
 PT J
 AU Shang, JH
 Cai, XH
 Feng, T
 Zhao, YL
 Wang, JK
 Zhang, LY
 Yan, M
 Luo, XD
 AF Shang, Jian-Hua
 Cai, Xiang-Hai
 Feng, Tao
 Zhao, Yun-Li
 Wang, Jing-Kun
 Zhang, Lu-Yong
 Yan, Ming
 Luo, Xiao-Dong
 TI Pharmacological evaluation of Alstonia scholaris: Anti-inflammatory
 and analgesic effects
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Ethnopharmacological relevance: Alstonia scholaris (Apocynaceae) has
 been historically used in "dai" ethnopharmacy to treat chronic
 respiratory diseases. The leaf extract, developed as a commercially
 available traditional Chinese medicine, used to release tracheitis and
 cold symptom, has also been prescribed in hospitals and sold over the
 counter in drug stores.
 Aim of the study: The investigation evaluated the anti-inflammatory
 and analgesic activities of the ethanolic extract, fractions and main
 alkaloids of Alstonia scholaris leaf to provide experimental evidence
 for its traditional and modern clinical use. Besides, to discover the
 active fraction and components for further better use in Chinese
 medicine is hopeful.
 Materials and methods: The leaf of Alstonia scholaris was extracted
 with ethanol and then separated into different fractions. Furthermore,
 alkaloids were isolated by phytochemical method. The analgesic
 activities were investigated using acetic acid-induced writhing,
 hot-plate and formalin tests in mice. The anti-inflammatory activities
 were carried out in vivo and in vitro, including xylene-induced ear
 edema and carrageenan-induced air pouch formation in mice, and COX-1,
 -2 and 5-LOX inhibition.
 Results: It has been exhibited that the EtOAc and alkaloid fractions
 reduced acetic acid-induced writhing response in mice, significantly.
 The ethanolic extract, Et0Ac and alkaloid fractions remarkably
 inhibited xylene-induced ear edema. Further investigation was focused
 on the alkaloids fraction and three main alkaloids isolated from the
 alkaloids fraction, in different animal models. Alkaloids reduced
 acetic acid-induced writhing response, and xylene-induced ear edema
 in mice. In the hot-plate test, alkaloids did not increase the latency
 period of mice obviously. In the formalin test, alkaloids did not
 inhibit the licking time in first phase, but significantly inhibited
 the licking time in second phase of mice. Alkaloids increased
 significantly SOD activity and decreased levels of NO. PGE2 and MDA
 significantly, in air pouch mice model. Moreover, some alkaloids
 isolated from the leaf of Alstonia scholaris exhibited inhibition of
 COX-1, COX-2 and 5-LOX in vitro anti-inflammatory assay, which
 supported alkaloids as the bioactive fraction.
 Conclusions: The alkaloids fraction of Alstonia scholaris leaf, three
 main alkaloids, picrinine, vallesamine and scholaricine, may produce
 the anti-inflammatory and analgesic effect peripherally based on
 several in vivo assays. In in vitro tests, alkaloids exhibited
 inhibition of inflammatory mediators (COX-1, COX-2 and 5-LOX), which
 is accordant with results on animal models. Besides, COX-2/5-LOX dual
 inhibitors found in the experiment, such as 16-formyl-5
 alpha-methoxystrictamine, picralinal, and tubotaiwine might be
 valuable for further attention. (C) 2010 Published by Elsevier Ireland
 Ltd.
 SN 0378-8741
 PD MAY 27
 PY 2010
 VL 129
 IS 2
 BP 174
 EP 181
 DI 10.1016/j.jep.2010.02.011
 UT ISI:000278651300004
 PT J
 AU Liu, W
 Xu, J
 Jing, P
 Yao, WB
 Gao, XD
 Yu, LL
 AF Liu, Wei
 Xu, Jing
 Jing, Pu
 Yao, Wenbing
 Gao, Xiangdong
 Yu, Liangli (Lucy)
 TI Preparation of a hydroxypropyl Ganoderma lucidum polysaccharide and
 its physicochemical properties
 SO FOOD CHEMISTRY
 AB A hydroxypropyl Ganoderma lucidum polysaccharide (H-GLP) was prepared
 from a low-value water-insoluble polysaccharide from G. lucidum (GLP)
 using propylene oxide under an alkaline condition. The H-GLP was
 characterised for its chemical structure with IR and C-13 NMR spectra
 and analysed for its mono-sugar composition, molecular weight, and
 hydroxypropyl content. H-GLP contained mannose, glucose, and galactose
 in a mole ratio of 1.0:36.5:3.59, respectively, with an average
 molecular weight of 788 kDa and a hydroxypropyl content of 12.05%. H-GLP
 also had an excellent water solubility of more than 50 mg/mL, suggesting
 that hydroxypropylation might serve as an effective approach to enhance
 water solubility of GLP. H-GLP was also compared to the original GLP
 and ascorbic acid for antioxidant properties. H-GLP showed much
 stronger free radical scavenging capacity against hydroxyl and
 superoxide anion radicals and hydrogen peroxide than GLP. These results
 suggested the potential of hydroxypropylation in developing
 water-soluble antioxidative polysaccharides from GLP to enhance the
 profitability of G. lucidium production and processing industries. (C)
 2010 Elsevier Ltd. All rights reserved.
 SN 0308-8146
 PD OCT 15
 PY 2010
 VL 122
 IS 4
 BP 965
 EP 971
 DI 10.1016/j.foodchem.2009.11.087
 UT ISI:000278582400005
 PT J
 AU Liu, F
 Yu, LQ
 Jiang, C
 Yang, L
 Wu, WT
 You, QD
 AF Liu, Fei
 Yu, Li-Qin
 Jiang, Cheng
 Yang, Lei
 Wu, Wu-Tong
 You, Qi-Dong
 TI Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic
 kinesin KSP
 SO BIOORGANIC & MEDICINAL CHEMISTRY
 AB Inhibitors of kinesin spindle protein (KSP) are a promising class of
 anticancer agents that cause mitotic arrest in cells from a failure
 to form functional bipolar mitotic spindles. Here, we report the
 synthesis and biological evaluation of a novel series of
 tetrahydro-beta-carboline analogs based on the structure of the known
 KSP inhibitor HR22C16. Preferred compounds 11b, 12a and 19b were
 identified as potent inhibitors in a KSP ATPase assay with good
 anti-proliferative activity in A549 cells. (C) 2010 Elsevier Ltd. All
 rights reserved.
 SN 0968-0896
 PD JUN 15
 PY 2010
 VL 18
 IS 12
 BP 4167
 EP 4177
 DI 10.1016/j.bmc.2010.05.024
 UT ISI:000278480900001
 PT J
 AU Zan, M
 Chen, XQ
 Fu, Q
 Shi, SP
 Zhou, SX
 Xiao, MT
 Tu, PF
 AF Zan, Me
 Chen, Xiao-Qing
 Fu, Qiang
 Shi, She-Po
 Zhou, Si-Xiang
 Xiao, Mei-Tian
 Tu, Peng-Fei
 TI 1, 10-Secoguaianolides from Artemisia anomala (Asteraceae)
 SO BIOCHEMICAL SYSTEMATICS AND ECOLOGY
 SN 0305-1978
 PD JUN
 PY 2010
 VL 38
 IS 3
 BP 431
 EP 434
 DI 10.1016/j.bse.2010.01.015
 UT ISI:000278709900022
 PT J
 AU Wang, L
 Yin, ZQ
 Cai, Y
 Zhang, XQ
 Yao, XS
 Ye, WC
 AF Wang, Lei
 Yin, Zhi-Qi
 Cai, Yan
 Zhang, Xiao-Qi
 Yao, Xin-Sheng
 Ye, Wen-Cai
 TI Amaryllidaceae alkaloids from the bulbs of Lycoris radiata
 SO BIOCHEMICAL SYSTEMATICS AND ECOLOGY
 SN 0305-1978
 PD JUN
 PY 2010
 VL 38
 IS 3
 BP 444
 EP 446
 DI 10.1016/j.bse.2010.02.005
 UT ISI:000278709900026
 PT J
 AU Wu, XR
 Wang, LL
 Wang, SZ
 Chen, YJ
 AF Wu, Xuri
 Wang, Lili
 Wang, Shuzhen
 Chen, Yijun
 TI Stereoselective introduction of two chiral centers by a single
 diketoreductase: an efficient biocatalytic route for the synthesis of
 statin side chains
 SO AMINO ACIDS
 AB Statins, including atorvastatin (Lipitor(A (R))), are the top-selling
 drugs in the world. The biocatalytic production of chiral side chains
 of statin drugs is of great interest to academia and industry.
 Stereoselective double reduction of a beta,delta-diketo ester
 catalyzed by a diketoreductase offers a simple and efficient route for
 the preparation of statin side chains. Comparison of different cofactor
 regeneration systems resulted in an easy and cost-effective process
 for this enzymatic reduction.
 SN 0939-4451
 PD JUN
 PY 2010
 VL 39
 IS 1
 BP 305
 EP 308
 DI 10.1007/s00726-009-0390-0
 UT ISI:000278519200027
 PT J
 AU Fu, MJ
 Zhuang, JJ
 Hou, FZ
 Ning, XB
 Zhan, QB
 Shao, Y
 AF Fu Mao-Jing
 Zhuang Jian-Jun
 Hou Feng-Zhen
 Ning Xin-Bao
 Zhan Qing-Bo
 Shao Yi
 TI Extracting human gait series based on the wavelet transform
 SO ACTA PHYSICA SINICA
 AB The wavelet transform was applied to process the accelerometer signals
 derived from human walking. The accelerometer signals were first
 decomposed at different levels utilizing the multi-scale and
 multi-resolution characteristics of the discrete wavelet transform
 After the determination of both the mother wavelet and the optimal
 decomposition level, human gait series can thus be extracted from the
 eigen scale of the accelerometer signal Compared with the method that
 detects peak values directly from accelerometer signals by
 thresholding, the wavelet transform gives higher detection rate of peak
 values on the eigen scale of the accelerometer signals Even when the
 accelerometer signals are exposed to serious noise, experimental
 results still demonstrate that the wavelet approach can guarantee the
 precision of the extracted gait series, which is of vital importance
 for the subsequent analyses It can be concluded that wavelet transform
 is an effective tool for the extraction of gait rhythmicity. The wavelet
 transform will be helpful in identifying the characteristics of other
 physiological signals.
 SN 1000-3290
 PD JUN
 PY 2010
 VL 59
 IS 6
 BP 4343
 EP 4350
 UT ISI:000278672300104
 PT J
 AU Wang, Y
 Li, ZH
 Zhong, WY
 Li, H
 Xu, DK
 Chen, HY
 AF Wang Ying
 Li ZhongHui
 Zhong WenYing
 Li Hui
 Xu DanKe
 Chen HongYuan
 TI Rhodamine B doped silica nanoparticle labels for protein microarray
 detection
 SO SCIENCE CHINA-CHEMISTRY
 AB A core-shell Rhodamine B-doped SiO2 nanoparticle was synthesized and
 its fluorescent intensity was found to be 1000 times higher than that
 of individual Rhodamine B molecule. The doped nanoparticles were
 further conjugated with streptavidin and the resulting nanoparticles
 were used in the detection of reverse-phase protein microarrays, in
 which human IgG of various concentrations was first immobilized on
 aldehyde-modified glass slides and then biotinlyated goat anti human
 IgG as well as the labeled nanoparticles were sequentially conjugated.
 The calibration curve is linear over the range from 800 fg to 500 pg
 and the limit of detection is 100 fg, which is 8 times lower than that
 of streptavidin-labeled Cy3 fluorescent dyes. The dye-doped SiO2
 nanoparticles show potentials for the protein array detection.
 SN 1674-7291
 PD APR
 PY 2010
 VL 53
 IS 4
 BP 747
 EP 751
 DI 10.1007/s11426-010-0104-1
 UT ISI:000278263400007
 PT J
 AU Liu, H
 Xu, JP
 Qu, LB
 Xiang, BR
 AF Liu Hao
 Xu JianPing
 Qu LingBo
 Xiang BingRen
 TI Generalized two-dimensional correlation near-infrared spectroscopy
 and principal component analysis of the structures of methanol and
 ethanol
 SO SCIENCE CHINA-CHEMISTRY
 AB Liquid state methanol and ethanol under different temperatures have
 been investigated by FT-NIR (Fourier transform near-infrared)
 spectroscopy, generalized two-dimensional (2D) correlation
 spectroscopy, and PCA (principal component analysis). First, the
 FT-NIR spectra were measured over a temperature range of 30-64 (or
 30-71) degrees C, and then the 2D correlation spectra were computed.
 Combining near-infrared spectroscopy, generalized 2D correlation
 spectroscopy, and references, we analyzed the molecular structures
 (especially the hydrogen bond) of methanol and ethanol, and performed
 the NIR band assignments. The PCA method was employed to verify the
 results of the 2D analysis. This study will be helpful to the
 understanding of these reagents.
 SN 1674-7291
 PD MAY
 PY 2010
 VL 53
 IS 5
 BP 1155
 EP 1160
 DI 10.1007/s11426-010-0172-2
 UT ISI:000278263500027
 PT J
 AU Gao, YA
 Zu, HI
 Zhang, JJ
 AF Gao Yuan
 Zu Hui
 Zhang Jianjun
 TI Pharmaceutical Cocrystals
 SO PROGRESS IN CHEMISTRY
 AB Different solid forms of identical drug may have diverse
 physicochemical properties, therapeutic/toxicological effects and
 formulation profiles. Compared to solvates and salts which are limited
 to small numbers of nontoxic solvents and ionizable drugs, cocrystals
 represent the very promising designable solid forms of active
 pharmaceutical ingredients, due to their extensive species and wide
 application scope. In this article, progress on pharmaceutical
 cocrystals, including the formation principles, cocrystal design,
 physicochemical properties and preparation techniques, is addressed.
 Cocrystals have great potentials in pharmaceutical sciences.
 SN 1005-281X
 PD MAY
 PY 2010
 VL 22
 IS 5
 BP 829
 EP 836
 UT ISI:000278187300007
 PT J
 AU Lei, BK
 Zha, WB
 Wang, Y
 Wen, C
 Studer, EJ
 Wang, XA
 Jin, F
 Wang, GJ
 Zhang, LY
 Zhou, HP
 AF Lei, Bokai
 Zha, Weibin
 Wang, Yun
 Wen, Cong
 Studer, Elaine J.
 Wang, Xuan
 Jin, Fang
 Wang, Guangji
 Zhang, Luyong
 Zhou, Huiping
 TI Development of a Novel Self-Microemulsifying Drug Delivery System for
 Reducing HIV Protease Inhibitor-Induced Intestinal Epithelial Barrier
 Dysfunction
 SO MOLECULAR PHARMACEUTICS
 AB The development of HIV protease inhibitors (Pis) has been one of the
 most significant advances of the past decade in controlling HIV
 infection. Unfortunately, the benefits of HIV Pis are compromised by
 serious side effects. One of the most frequent and deleterious side
 effects of HIV Pls is severe gastrointestinal (GI) disorders including
 mucosal erosions, epithelial barrier dysfunction, and leak-flux
 diarrhea, which occurs in 16-62% of patients on HIV Pls. Although the
 underlying mechanisms behind HIV Pl-associated serious adverse side
 effects remain to be identified, our recent studies have shown that
 activation of endoplasmic reticulum (ER) stress response plays a
 critical role in HIV Pl-induced GI complications. The objective of this
 study was to develop a novel self-microemulsifying drug delivery system
 (SMEDDS) using various antioxidants as surfactants and cosurfactants
 to reduce the GI side effects of the most commonly used HIV PI,
 ritonavir. The biological activities of this SMSDDS of ritonavir were
 compared with that of Norvir, which is currently used in the clinic.
 Rat normal intestinal epithelial cells (IEC-6) and mouse Raw 264.7
 macrophages were used to examine the effect of new SMEDDS of ritonavir
 on activation of ER stress and oxidative stress. Sprague-Dawley rats
 and C571BL6 mice were used for pharmacokinetic studies and in vivo
 studies. The intracellular and plasma drug concentrations were
 determined by HPLC analysis. Activation of ER stress was detected by
 Western blot analysis and secreted alkaline phosphatase (SEAP)
 reporter assay. Reactive oxygen species (ROS) was measured using
 dichlorodihydrofluorescein diacetate as a probe. Cell viability was
 determined by Roche's cell proliferation reagent WST-1. Protein levels
 of inflammatory cytokines (TNF-alpha and IL-6) were determined by
 enzyme-linked immunosorbent assays (ELISA). The intestinal
 permeability was assessed by luminal enteral administration of
 fluorescein isothiocyanate conjugated dextran (FITC-dextran, 4 kDa).
 The pathologic changes in intestine were determined by histological
 examination. The results indicated that incorporation of antioxidants
 in this new SMEDDS not only significantly reduced ritonavir-induced
 ER stress activation, ROS production and apoptosis in intestinal
 epithelial cells and macrophages, but also improved the solubility,
 stability and bioavailability of ritonavir, and significantly reduced
 ritonavir-induced disruption of intestinal barrier function in vivo.
 In conclusion, this new SMEDDS of ritonavir has less GI side effects
 compared to Norvir. This new SMEDDS can be used for other HIV Pls and
 any insoluble antiviral drug with serious GI side effects.
 SN 1543-8384
 PD MAY-JUN
 PY 2010
 VL 7
 IS 3
 BP 844
 EP 853
 DI 10.1021/mp100003r
 UT ISI:000278452100022
 PT J
 AU Wang, Q
 Wu, XM
 Zhang, DY
 AF Wang, Quan
 Wu, Xiao Ming
 Zhang, Da Yong
 TI RESEARCH PROGRESS ON PREDICTION MODELS FOR PHYSICAL PROPERTIES OF IONIC
 LIQUID
 SO MODERN PHYSICS LETTERS B
 CT 3rd International Symposium on Physics of Fluids
 CY JUN 15-18, 2009
 CL Jiuzhaigou, PEOPLES R CHINA
 AB The field of ionic liquid has gained rapid growth in recent years and
 occupied a forefront in green chemistry. As a useful instrument to the
 research and development of novel ionic liquids, the physical
 properties are of utmost importance. Thus, great efforts have been made
 to obtain these important data, as it is far from getting sufficient
 physiochemical information for intensive and extensive investigation
 which consequently becomes a bottleneck for the theoretical and
 applicable research of ionic liquids. Additionally, with the given
 immeasurable possible ionic liquids by various cation and anion
 combinations, it is an impossible task to find an ideal ionic liquid
 with desired physical properties using conventionally "try and error"
 process. For these reasons, exploration of novel prediction models for
 physical properties of ionic liquid is imperative. This paper gives
 an overview of recent progress of various prediction models.
 SN 0217-9849
 PD MAY 30
 PY 2010
 VL 24
 IS 13
 BP 1487
 EP 1490
 DI 10.1142/S0217984910023931
 UT ISI:000278194400054
 PT J
 AU Ni, SJ
 Zhang, HB
 Huang, WL
 Zhou, JP
 Qian, H
 Chen, W
 AF Ni, Shuaijian
 Zhang, Huibin
 Huang, Wenlong
 Zhou, Jinpei
 Qian, Hai
 Chen, Wei
 TI The application of an aryl hydrazine linker prevents beta-elimination
 side products in the SPPS of C-terminal cysteine peptides
 SO JOURNAL OF PEPTIDE SCIENCE
 AB Solid-phase synthesis allows for the preparation of some complex
 cysteine-containing peptides with both a high yield and purity.
 However, side reactions during chain elongation such as modification
 of amino acid residues have been found in C-terminal cysteine peptides.
 We identified 3-(1-piperidinyI)-alanine peptides, corroborated the
 mechanism of the side reaction, and introduced an efficient approach
 for the Fmoc-based synthesis of C-terminal cysteine peptides using an
 aryl hydrazine linker. Copyright (C) 2010 European Peptide Society and
 John Wiley & Sons, Ltd.
 SN 1075-2617
 PD JUN
 PY 2010
 VL 16
 IS 6
 BP 309
 EP 313
 DI 10.1002/psc.1240
 UT ISI:000278392200008
 PT J
 AU Fan, JH
 Liu, K
 Zhang, ZA
 Luo, TJ
 Xi, ZL
 Song, JN
 Liu, BL
 AF Fan, Jinghua
 Liu, Kang
 Zhang, Zhongai
 Luo, Tianjiong
 Xi, Zhilei
 Song, Junna
 Liu, Baolin
 TI Modified Si-Miao-San extract inhibits the release of inflammatory
 mediators from lipopolysaccharide-stimulated mouse macrophages
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Ethnopharmacological relevance: Modified Si-Miao-San (mSMS) is a
 prescription modified from Si-Miao-San which is an ancient Chinese
 prescription used to treat various ailments.
 Aim of the study: Modified Si-Miao-San (mSMS) has been used for the
 treatment of infectious and inflammatory disorders in the clinic. This
 study was aimed to investigate its anti-inflammatory activity and
 underlying mechanism at cellular and molecular levels.
 Materials and methods: We stimulated RAW264.7 cells with
 Lipopolysaccharide (LPS) and observed effects of mSMS on the release
 of inflammatory mediators such as: tumor necrosis factor-alpha
 (TNF-alpha), interleukin-6 (IL-6), NO, and relative gene expressions.
 Meanwhile, we also investigated the modulation of mSMS in inflammatory
 signal transduction mediated through extracellular signal-regulated
 protein kinase (ERK) and nuclear factor-kappa B (NF-kappa B) pathway.
 Results: Our findings demonstrated that mSMS significantly inhibited
 the excessive production of NO, TNF-alpha and IL-6 and the over
 expression of relative genes in LPS-stimulated macrophages. In
 addition, mSMS suppressed LPS-induced ERK1/2-phosphorylation and
 inhibited the activation of NF-kappa B by attenuation of I kappa B-alpha
 degradation.
 Conclusions: Our results suggest that the anti-inflammatory properties
 of mSMS might result from the inhibition of inflammatory mediators,
 such as NO, TNF-alpha and IL-6, via suppression of ERK and NF-kappa
 B dependent pathways. (C) 2010 Elsevier Ireland Ltd. All rights
 reserved.
 SN 0378-8741
 PD MAY 4
 PY 2010
 VL 129
 IS 1
 BP 5
 EP 9
 DI 10.1016/j.jep.2010.02.002
 UT ISI:000278239600002
 PT J
 AU Du, YZ
 Lu, P
 Zhou, JP
 Yuan, H
 Hu, FQ
 AF Du, Yong-Zhong
 Lu, Ping
 Zhou, Jian-Ping
 Yuan, Hong
 Hu, Fu-Qiang
 TI Stearic acid grafted chitosan oligosaccharide micelle as a promising
 vector for gene delivery system: Factors affecting the complexation
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB Stearic acid (SA) grafted chitosan oligosaccharide (CSO-SA) with
 different molecular weight of chitosan oligosaccharide (CSO) and graft
 ratio of stearic acid were synthesized by coupling reaction of SA and
 CSO. The cationic polymeric micelles of CSO-SA via self-assemble formed
 and used for gene delivery of fish sperm DNA. Factors affecting
 complexation and stability of the complexes of CSO-SA micelles and DNA
 were investigated. The results indicated that pKa of CSO-SA with 3 kDa
 of CSO decreased from 8.16 to 6.02 as the substitution degree of amino
 groups of CSO in CSO-SA increased from 9.79% to 63.41%, whereas the
 molecular weight (M-W) of CSO less affected the pKa. As for the
 stability of complexes, ethidium bromide assay data demonstrated that
 the complexes consisting of CSO-SA with lower amino substitution degree
 or smaller molecular weight of CSO were more stable than that with the
 higher amino substitution degree or molecular weight of CSO. The
 results also presented that the low pH and ionic strength environment
 were in favor for the stability of complexes. (C) 2010 Elsevier B.V.
 All rights reserved.
 SN 0378-5173
 PD MAY 31
 PY 2010
 VL 391
 IS 1-2
 BP 260
 EP 266
 DI 10.1016/j.ijpharm.2010.02.017
 UT ISI:000278342900032
 PT J
 AU Zhang, WL
 Gu, XA
 Bai, H
 Yang, RH
 Dong, CD
 Liu, JP
 AF Zhang, Wen-Li
 Gu, Xiao
 Bai, Hui
 Yang, Ru-Hui
 Dong, Chen-Dong
 Liu, Jian-Ping
 TI Nanostructured lipid carriers constituted from high-density
 lipoprotein components for delivery of a lipophilic cardiovascular
 drug
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB To investigate the possibility of reconstituted protein-free
 high-density lipoprotein (HDL) being a carrier for delivering a
 lipophilic cardiovascular drug, Tanshinone IIA-loaded HDL-like
 nanostructured lipid carriers (TA-NLC) were prepared by a
 nanoprecipitation/solvent diffusion method. The physicochemical
 parameters of TA-NLC were characterized in terms of particle size, zeta
 potential, morphology, entrapment efficiency, differential scanning
 calorimetry (DSC) and stability. A novel two-step method has been
 employed to determine entrapment efficiency of TA-NLC. The binding
 properties of TA-NLC to apolipoproteins were investigated by in vitro
 incubation competition assay in the presence of native HDL and
 electrophoresis test. Phagocytosis and cytotoxicity was evaluated
 using mouse macrophage cell line RAW 264.7 with TA-NLC and incubated
 TA-NLC with native HDL (TA-NLC-apo). The results showed that TA-NLC
 had an average diameter of 8.0 +/- 1.2 nm, zeta potential of -29.0 +/0.0 mV, drug loading of 6.17 +/- 0.3% and entrapment efficiency of 97.84
 +/- 1.2%. TA-NLC were demonstrated spheres with drug incorporated in
 lipid core forming a shell-core structure. DSC analysis showed that
 TA was dispersed in NLC in an amorphous state. The incorporation of
 glycerol trioleate to NLC led to crystal order disturbance. Agarose
 gel electrophoresis and sodium dodecyl sulfate polyacrylamide gel
 electrophoresis (SDS-SPAGE) patterns indicated that TA-NLC could bind
 to apolipoprotein A-I (apoA-I) specifically in vitro. Phagocytosis
 studies showed significant differences in uptake between TA-NLC and
 TA-NLC-apo and demonstrated that TA-NLC incubated with native HDL could
 turn endogenous by association to apolipoproteins, which cannot
 trigger immunological responses and could escape from recognition by
 macrophages. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0378-5173
 PD MAY 31
 PY 2010
 VL 391
 IS 1-2
 BP 313
 EP 321
 DI 10.1016/j.ijpharm.2010.03.011
 UT ISI:000278342900038
 PT J
 AU Hu, GQ
 Zhang, ZQ
 Xie, SQ
 Huang, WL
 AF Hu, Guo Qiang
 Zhang, Zhong Quan
 Xie, Song Qiang
 Huang, Wen Long
 TI Synthesis and antitumor evaluation of C3/C3 fluoroquinolone dimers
 (I): Tethered with a fused heterocyclic
 s-triazolo[2,1-b][1,3,4]thiadiazole
 SO CHINESE CHEMICAL LETTERS
 AB Five C3/C3 fluoroquinolone dimers tethered with a fused heterocyclic
 ring of s-triazolo[2,1-b][1,3,4]thiadiazole derived from
 antibacterial quinolones were synthesized and characterized, and their
 in vitro antitumor activity against L1210, CHO cell lines was evaluated
 via the respective IC50 values. (C) 2010 Guo Qiang Hu. Published by
 Elsevier B.V. on behalf of Chinese Chemical Society. All rights
 reserved.
 SN 1001-8417
 PD JUN
 PY 2010
 VL 21
 IS 6
 BP 661
 EP 663
 DI 10.1016/j.cclet.2010.01.037
 UT ISI:000278442300007
 A Qian, Y
 U Liang, JY
 Qu, W
 Che, YY
 A Qian, Yong
 F Liang, Jing Yu
 Qu, Wei
 Che, YanYun
 Two new homoisoflavanones from Polygonatum odoratum (Mill.) Druce
 CHINESE CHEMICAL LETTERS
 A Two new homoisoflavanones were isolated from the rhizomes of
 B Polygonatum odoratum (Mill.) Druce and their structures were
 elucidated as
 (3R)-5,7-dihydroxy-8-methoxy-3-(4-methoxybenzyl)-6-methylchrom-an4-one (1) and
 (3R)-5,7,8-trihydroxy-3-(4-hydroxybenzyl)-6-methylchroman-4-one
 (2), on the basis of sp-ectral analysis. (C) 2010 Jing Yu Liang.
 Published by Elsevier B.V. on behalf of Chinese Chemical Society. All
 rights reserved.
 1001-8417
 2010
 10.1016/j.cclet.2010.01.040
 ISI:000278442300019
 PT J
 AU Ou, Y
 Zheng, S
 Lin, L
 Jiang, QH
 Yang, XG
 AF Ou, Yu
 Zheng, Shan
 Lin, Lin
 Jiang, Qizhou
 Yang, Xuegan
 TI Protective effect of C-phycocyanin against carbon
 tetrachloride-induced hepatocyte damage in vitro and in vivo
 SO CHEMICO-BIOLOGICAL INTERACTIONS
 AB This study focused on the hepatoprotective activity of C-phycocyanin
 (C-PC) against carbon tetrachloride-induced hepatocyre damage in vitro
 and in vivo. In in vitro study, human hepatocyte cell line L02 was used.
 C-PC showed its capability to reverse CCl4-induced L02 cells viability
 loss, alanine transaminase (ALT) leakage and morphological changes.
 C-PC also showed the following positive effects: prevent the
 CCl4-induced overproduction of intracellular reactive oxygen species
 (ROS) and malondialdehyde (MDA); prevent changes in superoxide
 dismutase (SOD) activity; and reduce glutathione (GSH) level. In vivo,
 CPC showed its capability to decrease serum ALT and aspartate
 transaminase (AST) levels in CCl4-induced liver damage in mice. The
 histological observations supported the results obtained from serum
 enzymes assays. C-PC also showed the following effects in mice liver:
 prevent the CCl4-induced MDA formation and GSH depletion; prevent SOD
 and glutathione peroxidase (GSH-Px) activity; and prevent the
 elevation of transforming growth factor-beta1 (TGF-beta(1)) and
 hepatocyte growth factor (HGF) mRNAs. Both the in vitro and in vivo
 results suggested that C-PC was useful in protecting against
 CCl4-induced hepatocyte damage. One of the mechanisms is believed to
 be through C-PCs scavenging ability to protect the hepatocytes from
 free radicals damage induced by CCl4. In addition, C-PC may be able
 to block inflammatory infiltration through its anti-inflammatory
 activities by inhibiting TGF-beta 1 and HGF expression. (C) 2010
 Elsevier Ireland Ltd. All rights reserved.
 SN 0009-2797
 PD APR 29
 PY 2010
 VL 185
 IS 2
 BP 94
 EP 100
 DI 10.1016/j.cbi.2010.03.013
 UT ISI:000278440300002
 PT J
 AU Yu, LY
 Deng, HS
 Xiang, BR
 AF Yu, Liyan
 Deng, Haishan
 Xiang, Bingren
 TI Liquid chromatography-tandem mass/mass spectrometry method for the
 quantification of rabeprazole in human plasma and application to a
 pharmacokinetic study
 SO ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
 AB A rapid, simple and sensitive reversed-phase high-performance liquid
 chromatographic-tandem mass/mass spectrometry (HPLC/MS/MS) method has
 been developed for the measurement of rabeprazole (CAS 117976-89-3)
 concentrations in human plasma and its use in bioavailability studies
 has been evaluated. The method was linear in the concentration range
 of 0.05-2.5 mu g/ml. The lower limit of quantification (LLOQ) was 0.05
 mu g/ml in 1 ml plasma sample. The intra- and inter-day relative
 standard deviation across three validation runs over the entire
 concentration range was less than 8.2% and 7.53%, respectively. This
 method was successfully applied for the evaluation of pharmacokinetic
 profiles of rabeprazole tablet in 18 healthy volunteers. The main
 pharmacokinetic parameters obtained were: AUC(0-t) 1415.88 +/- 505.46
 and 1457.44 +/- 524.40 ng . h/ml, AUC(0-infinity) 1439.10 +/- 507.47
 and 1479.81 +/- 527.83 ng h/ml, C-max 678.24 +/- 278.93 and 657.83 +/250.86 ng/ml, t(1/2) 1.48 +/- 0.19 and 1.38 +/- 0.24 h, t(max) 3.8 +/0.8 and 3.7 +/- 0.5 h for the test and reference formulations,
 respectively. No statistical differences were observed for C-max and
 the area under the plasma concentration time curve for rabeprazole.
 90% confidence limits calculated for C-max and AUC from zero to infinity
 (AUC(0-infinity)) of rabeprazole were included in the bioequivalence
 range (0.8-1.25 for AUC).
 SN 0004-4172
 PY 2010
 VL 60
 IS 5
 BP 262
 EP 266
 UT ISI:000278351000006
 PT J
 AU Yu, JN
 Zhu, YA
 Wang, L
 Peng, M
 Tong, SS
 Cao, X
 Qiu, H
 Xu, XM
 AF Yu, Jiang-nan
 Zhu, Yuan
 Wang, Li
 Peng, Min
 Tong, Shan-shan
 Cao, Xia
 Qiu, Hui
 Xu, Xi-ming
 TI Enhancement of oral bioavailability of the poorly water-soluble drug
 silybin by sodium cholate/phospholipid-mixed micelles
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To evaluate a mixed micellar drug delivery system composed of
 sodium cholate and phospholipid for oral administration of silybin,
 a promising hepatoprotectants.
 Methods: The optimum formulation of sodium cholate/phospholipid-mixed
 micelles containing silybin was obtained based on the study of
 pseudo-ternary phase diagram. The dissolution of silybin-mixed
 micelles was investigated. The pharmacokinetic characteristics and
 bioavailability after oral administration of silybin-mixed micelles
 and silybin-N-methylglucamine were compared in dogs.
 Results: The mean particle size of prepared mixed micelles was 75.9
 +/- 4.2 nm. The largest solubility of silybin was found to be 10.0 +/1.1 mg/mL in the optimum formulation of mixed micelles. The
 silybin-sodium cholate/phospholipid-mixed micelles showed a very slow
 release of silybin 17.5% (w/w) within 72 h in phosphate buffer (pH 7.4)
 and 15.6% (w/w) in HCl solution (pH 1.2). After oral administration
 to dogs, the relative bioavailability of mixed micelles versus
 silybin-N-methylglucamine in dogs was 252.0%.
 Conclusion: Sodium cholate/phospholipid-mixed micelles are promising
 carriers in orally delivery of silybin, considering their capability
 of enhancing bioavailability and large-scale production.
 SN 1671-4083
 PD JUN
 PY 2010
 VL 31
 IS 6
 BP 759
 EP 764
 DI 10.1038/aps.2010.55
 UT ISI:000278341900015
 PT J
 AU Di, LL
 Wang, Y
 Lin, GW
 Lu, T
 AF Di, Li Li
 Wang, Yue
 Lin, Guo Wu
 Lu, Tao
 TI Aquabis(1H-benzimidazole-2-carboxylato-kappa O-2,N-3)zinc(II)
 SO ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE
 AB In the title compound, [Zn(C8H5N2O2)(2)(H2O)], the Zn-II ion is
 coordinated in each case by a carboxylate O atom and an imidazole N
 atom from two different benzimidazole-2-carboxylate (BIC) ligands and
 one water O atom in a trigonal-bipyramidal geometry. In the complex
 molecule, the two benzimidazole planes are twisted, making a dihedral
 angle of 55.93 (11)degrees. The three-dimensional framework is
 organized by intermolecular N-H center dot center dot center dot O
 hydrogen bonding and OH center dot center dot center dot O interactions
 and pi-pi interactions between adjacent benzimidazole rings
 [centroid-centroid distance = 3.586 (3) angstrom].
 SN 1600-5368
 PD JUN
 PY 2010
 VL 66
 PN Part 6
 BP M610
 EP U193
 DI 10.1107/S1600536810015631
 UT ISI:000278263300009
 PT J
 AU Qi, JP
 Sun, MJ
 Ping, QE
 Zhuang, JE
 Li, JR
 Peddie, F
 Song, YM
 AF Qi, Jianping
 Sun, Minjie
 Ping, Qineng
 Zhuang, Jie
 Li, Jiangran
 Peddie, Frank
 Song, Yunmei
 TI The Mechanisms for Enhanced Oral Absorption of Hydroxysafflor Yellow
 A by Chuanxiong Volatile Oil
 SO PLANTA MEDICA
 AB The aims of this study were to investigate the effect of Ligusticum
 chuanxiong volatile oil (CVO) on the oral absorption of hydroxysafflor
 yellow A (HSYA). The effects were studied both in vitro and in vivo.
 The contents of CVO were measured by GC-MS. The Caco-2 cell model was
 used to evaluate HSYA permeation with or without the presence of CVO.
 Transepithelial electrical resistance (TEER) of the Caco-2 cell
 monolayers was monitored and the alteration in the subcellular
 localization of claudin-1, the tight junction protein, was observed
 by immunofluorescence. The irritation of CVO on rat intestine was
 studied by paraffin slice technology. Our results demonstrated that
 CVO mainly contained ligustilide (47.82%). The Papp of HSYA was
 improved by 5.34-fold and 4.62-fold in the presence of 0.02 mg/mL and
 0.01 mg/mL of CVO, respectively. After opening of the tight junctions
 of the Caco-2 cell monolayer, TEER decreased, the position of claudin-1
 changed, and its expression increased. CVO at different concentrations
 10, 25, 100 and 200 mg/kg) caused no significant irritation on rat
 intestine. The bioavailability of HSYA in rats was increased by
 6.48-fold and 4.91-fold when 100 and 25mg/kg of CVO were
 co-administrated, respectively. CVO was an effective absorption
 enhancer for oral delivery of BCS III drugs. It can cause redistribution
 of claudin-1 proteins and open the tight junctions.
 SN 0032-0943
 PD MAY
 PY 2010
 VL 76
 IS 8
 BP 786
 EP 792
 DI 10.1055/s-0029-1240705
 UT ISI:000278064200005
 PT J
 AU Chen, YQ
 Zhang, WD
 Kong, LY
 Lu, T
 Shen, YH
 AF Chen, Y. Q.
 Zhang, W. D.
 Kong, L. Y.
 Lu, T.
 Shen, Y. H.
 TI Delavayol, a novel sesquiterpene from Incarvillea delavayi Bureau et
 Franchet
 SO NATURAL PRODUCT RESEARCH
 AB To investigate the chemical constituents from Incarvillea delavayi
 Bureau et Franchet, a new sesquiterpene, named delavayol, together with
 three known ones, was isolated by column chromatography. Spectroscopic
 and chemical evidence revealed the structures to be
 8,9-dihydroxy-1(10)-eremophiliene-11,12-diol (1), oleanolic acid
 (2), myrianthic acid (3), and sitoindoside I (4). Compounds 3 and 4
 were isolated from the genus Incarvillea for the first time.
 SN 1478-6419
 PY 2010
 VL 24
 IS 10
 BP 915
 EP 919
 DI 10.1080/14786410802421026
 UT ISI:000278007000003
 PT J
 AU Yang, MH
 Luo, JG
 Huang, XF
 Kong, LY
 AF Yang, Ming Hua
 Luo, Jian Guang
 Huang, Xue Feng
 Kong, Ling Yi
 TI Flavonol glycosides with -D-aldohexoses from Rhododendron irroratum
 SO NATURAL PRODUCT RESEARCH
 AB Two new flavonol glycosides which contain rare -D-galactose or
 -D-glucose were obtained from the flowers of Rhododendron irroratum
 Franch., namely myricetin 3-O--D-galactoside-3'-O--D-glucoside (1)
 and myricetin 3-O--D-galactoside-3'-O--D-galactoside (2). Their
 structures were determined by UV, IR, HR-ESI-MS, ESI-MS, 1D- and 2D-NMR
 techniques.
 SN 1478-6419
 PY 2010
 VL 24
 IS 10
 BP 920
 EP 925
 DI 10.1080/14786410802425811
 UT ISI:000278007000004
 PT J
 AU Yin, RJ
 Huang, XF
 Kong, LY
 AF Yin, Ren-Jie
 Huang, Xue-Feng
 Kong, Ling-Yi
 TI Constituents from the heartwoods of Osmanthus armatus
 SO NATURAL PRODUCT RESEARCH
 AB A new ester, armatuside (1), along with 13 known compounds (2-14), were
 obtained from the ethanolic extract of the heartwoods of Osmanthus
 armatus. The structures of all compounds were deduced using 1D, and
 2D NMR spectroscopic methods. The absolute configuration of 1 was
 deduced by chemical correlation with a known compound. Compounds 2-14
 were isolated from the plant for the first time.
 SN 1478-6419
 PY 2010
 VL 24
 IS 10
 BP 948
 EP 952
 DI 10.1080/14786410802689713
 UT ISI:000278007000008
 PT J
 AU Zheng, YF
 Dai, DZ
 Dai, Y
 AF Zheng, Yu-Fen
 Dai, De-Zai
 Dai, Yin
 TI NaHS ameliorates diabetic vascular injury by correcting depressed
 connexin 43 and 40 in the vasculature in streptozotocin-injected rats
 SO JOURNAL OF PHARMACY AND PHARMACOLOGY
 AB Objectives Cardiovascular complication contributes an important role
 to morbidity and mortality in patients with diabetes. We hypothesized
 that these abnormalities are mainly mediated by oxidative stress,
 endothelial dysfunction and impaired intracellular communications.
 Thus, we examined vasoactivity and expression of connexin (Cx) 43 and
 40, protein kinase C-epsilon (PKC epsilon) and NADPH oxidase of the
 vasculature of thoracic aorta in streptozotocin (STZ)-injected rats,
 and whether NaHS could reverse these abnormalities compared with
 aminoguanidine.
 Methods Male Sprague-Dawley rats were administered with STZ (60 mg/kg,
 i.p.) to induce diabetes. Diabetic rats were divided into untreated
 and treated groups in the 5th-8th week and intervention with either
 NaHS (5 mg/kg daily, s.c.) or aminoguanidine (100 mg/kg daily, p.o.)
 was made.
 Key findings In rats with untreated diabetes, hyperglycaemia,
 increased activity of inducible nitric oxide (NO) synthase, increased
 NO, mild vascular spasm, reduced NO bioavailability and diminished
 vasorelaxation were found. These findings were accompanied by
 downregulated Cx43 and Cx40, and upregulated PKC epsilon and NADPH
 oxidase subunits p22(phox)/p47(phox)/p67(phox) in the thoracic aorta.
 NaHS appears to be as effective as aminoguanidine in attenuating these
 abnormalities.
 Conclusions NaHS shows promise in relieving diabetic vascular
 abnormality by upregulating junctional connexin Cx40 and Cx43, via
 normalizing NADPH oxidase and PKC epsilon in the vasculature.
 SN 0022-3573
 PD MAY
 PY 2010
 VL 62
 IS 5
 BP 615
 EP 621
 DI 10.1211/jpp.62.05.0009
 UT ISI:000278158000009
 PT J
 AU Luo, J
 Wang, JS
 Wang, XB
 Luo, JG
 Kong, LY
 AF Luo, Jun
 Wang, Jun-Song
 Wang, Xiao-Bing
 Luo, Jian-Guang
 Kong, Ling-Yi
 TI Chuktabularins E-T, 16-Norphragmalin Limonoids from Chukrasia
 tabularis var. velutina
 SO JOURNAL OF NATURAL PRODUCTS
 AB Chuktabularins E-T (1-16), 16 new 16-norphragmalin limonoids, together
 with four known compounds, chuktabularins A D, were isolated from the
 stem bark of Chukrasia tabularis var. veltaina. These compounds possess
 a biosynthetically extended propionyl or acetyl group at C-15 and a
 characteristic ketal moiety between the limonoid skeleton and the acyl
 substituent at C-15. The structures of these compounds were established
 on the basis of detailed spectroscopic analysis, and that of 1 was
 confirmed by a single-crystal X-ray diffraction experiment,
 representing the first verification of the skeleton of
 16-norphragmalin limonoids. Chuktabularins K-O (7-11) were found to
 be the first 19-acetoxylated 16-norphragmalin limonoids.
 Variable-temperature H-1 NMR experiments suggested that 7 exists as
 an equilibrium mixture of conformational isomers in solution. The
 absolute configuration of 5 was determined by the CD exciton chirality
 method on its 11,12-di-p-chlorobenzoate (5a), and those of 1-4 and 6-16
 were proposed by correlating with 5 spectroscopically and
 biogenetically.
 SN 0163-3864
 PD MAY
 PY 2010
 VL 73
 IS 5
 BP 835
 EP 843
 DI 10.1021/np900734c
 UT ISI:000278080900009
 PT J
 AU Chen, XM
 Lu, T
 Lu, SA
 Li, HF
 Yuan, HL
 Ran, T
 Liu, HC
 Chen, YD
 AF Chen, Xiu-Mei
 Lu, Tao
 Lu, Shuai
 Li, Hui-Fang
 Yuan, Hao-Liang
 Ran, Ting
 Liu, Hai-Chun
 Chen, Ya-Dong
 TI Structure-based and shape-complemented pharmacophore modeling for the
 discovery of novel checkpoint kinase 1 inhibitors
 SO JOURNAL OF MOLECULAR MODELING
 AB Checkpoint kinase 1 (Chk1), a member of the serine/threonine kinase
 family, is an attractive therapeutic target for anticancer combination
 therapy. A structure-based modeling approach complemented with shape
 components was pursued to develop a reliable pharmacophore model for
 ATP-competitive Chk1 inhibitors. Common chemical features of the
 pharmacophore model were derived by clustering multiple
 structure-based pharmacophore features from different Chk1-ligand
 complexes in comparable binding modes. The final model consisted of
 one hydrogen bond acceptor (HBA), one hydrogen bond donor (HBD), two
 hydrophobic (HY) features, several excluded volumes and shape
 constraints. In the validation study, this feature-shape query yielded
 an enrichment factor of 9.196 and performed fairly well at
 distinguishing active from inactive compounds, suggesting that the
 pharmacophore model can serve as a reliable tool for virtual screening
 to facilitate the discovery of novel Chk1 inhibitors. Besides, these
 pharmacophore features were assumed to be essential for Chk1
 inhibitors, which might be useful for the identification of potential
 Chk1 inhibitors.
 SN 1610-2940
 PD JUL
 PY 2010
 VL 16
 IS 7
 BP 1195
 EP 1204
 DI 10.1007/s00894-009-0630-y
 UT ISI:000278027600003
 PT J
 AU Zheng, YT
 Zhou, F
 Wu, XL
 Wen, XZ
 Li, YN
 Yan, B
 Zhang, JW
 Hao, G
 Ye, WC
 Wang, GJ
 AF Zheng, Yuanting
 Zhou, Fang
 Wu, Xiaolan
 Wen, Xiaozhou
 Li, Yannan
 Yan, Bei
 Zhang, Jingwei
 Hao, Gang
 Ye, Wencai
 Wang, Guangji
 TI 23-Hydroxybetulinic acid from Pulsatilla chinensis (Bunge) Regel
 synergizes the antitumor activities of doxorubicin in vitro and in vivo
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Ethnopharmacological revelance: Pulsatilla chinensis (Bunge) Regel
 has been used as adjuvant in chemotherapy in traditional Chinese
 medicine. 23-Hydroxybetulinic acid, an isolated pentacyclic
 triterpene, is the major active constituent of Pulsatilla chinensis
 (Bunge) Regel.
 Aim of this study: To evaluate the combinational anticancer effect of
 23-hydroxybetulinic acid and doxorubicin in vitro and in vivo.
 Materials and methods: The effect of combination treatment with
 23-hydroxybetulinic acid and doxorubicin was evaluated with a
 quantitative combination index method based on the median-effect
 analysis in various cancer cell lines. And in vivo efficacy of
 combination chemotherapy was also evaluated using ICR mice bearing
 sarcoma 180 carcinoma tumors.
 Results: 23-Hydroxybetulinic acid showed a synergistic cytotoxic
 effect on multiple cancer cell lines by combined use with doxorubicin.
 In vivo studies further demonstrated that co-administration of 23-HBA
 significantly improved the sensitivity of the tumor to doxorubicin
 through increasing intra-tumor doxorubicin concentration and
 inhibiting doxorubicin-induced up-regulation of P-gp in tumor.
 Conclusion: These results suggest that the combined therapy with
 23-hydroxybetulinic acid and doxorubicin may be a new promising
 strategy to promote the clinical chemotherapy, which needs further
 verification. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
 SN 0378-8741
 PD APR 21
 PY 2010
 VL 128
 IS 3
 BP 615
 EP 622
 DI 10.1016/j.jep.2010.02.004
 UT ISI:000278160200011
 PT J
 AU Chang, JS
 Huypens, P
 Zhang, YB
 Black, C
 Kralli, A
 Gettys, TW
 AF Chang, Ji Suk
 Huypens, Peter
 Zhang, Yubin
 Black, Chelsea
 Kralli, Anastasia
 Gettys, Thomas W.
 TI Regulation of NT-PGC-1 alpha Subcellular Localization and Function by
 Protein Kinase A-dependent Modulation of Nuclear Export by CRM1
 SO JOURNAL OF BIOLOGICAL CHEMISTRY
 AB Peroxisome proliferator-activated receptor gamma co-activator-1 alpha
 (PGC-1 alpha) plays a central role in the regulation of cellular energy
 metabolism and metabolic adaptation to environmental and nutritional
 stimuli. We recently described a novel, biologically active splice
 variant of PGC-1 alpha (NT-PGC-1 alpha, amino acids 1-270) that retains
 the ability to interact with and transactivate nuclear hormone
 receptors through its N-terminal transactivation domain. Whereas PGC-1
 alpha is an unstable nuclear protein sensitive to ubiquitin-mediated
 targeting to the proteasome, NT-PGC-1 alpha is relatively stable and
 predominantly cytoplasmic, suggesting that its ability to interact
 with and activate nuclear receptors and transcription factors is
 dependent upon regulated access to the nucleus. We provide evidence
 that NT-PGC-1 alpha interacts with the nuclear exportin, CRM1, through
 a specific leucine-rich domain (nuclear export sequence) that
 regulates its export to the cytoplasm. The nuclear export of NT-PGC-1
 alpha is inhibited by protein kinase A-dependent phosphorylation of
 Ser-194, Ser-241, and Thr-256 on NT-PGC-1 alpha, which effectively
 increases its nuclear concentration. Using site-directed mutagenesis
 to prevent or mimic phosphorylation at these sites, we show that the
 transcriptional activity of NT-PGC-1 alpha is regulated in part through
 regulation of its subcellular localization. These findings suggest
 that the function of NT-PGC-1 alpha as a transcriptional co-activator
 is regulated by protein kinase A-dependent inhibition of CRM1-mediated
 export from the nucleus.
 SN 0021-9258
 PD JUN 4
 PY 2010
 VL 285
 IS 23
 BP 18039
 EP 18050
 DI 10.1074/jbc.M109.083121
 UT ISI:000278133400079
 PT J
 AU Shen, Y
 Li, YQ
 Li, SP
 Ma, L
 Ding, LJ
 Ji, H
 AF Shen, Yang
 Li, Yong-Qi
 Li, Shao-Ping
 Ma, Lin
 Ding, Li-Ju
 Ji, Hui
 TI Alleviation of ovariectomy-induced osteoporosis in rats by Panax
 notoginseng saponins
 SO JOURNAL OF NATURAL MEDICINES
 AB To examine the effects of Panax notoginseng saponins (PNS), the main
 active components of Panax notoginseng, on ovariectomy-induced
 osteoporosis in rats. A total of 72 six-month-old female rats were
 randomly assigned to sham-operated group and five ovariectomized (OVX)
 groups: OVX with distilled water (5 ml/kg/day, p.o.), OVX with graded
 doses of PNS (75, 150, 300 mg/kg/day, p.o.), and OVX with nilestriol
 (1 mg/kg/week, p.o.). Animals were sacrificed after a 13-week treatment
 course. Compared with the OVX group, PNS administration prevented
 OVX-induced decrease in bone mineral density (BMD) of lumbar vertebrae
 and total femur, and significantly increased bone structural
 biomechanical properties. Improvements of BMD and biomechanical
 properties were accompanied by the beneficial changes of PNS on
 trabecular microarchitecture in the tibial metaphysis. PNS at the
 highest dose significantly prevent decrease in trabecular bone volume
 over bone total volume, trabecular number, trabecular thickness,
 connectivity density, and increase in trabecular separation and
 structure model index in OVX rats. The bone-modulating effects of PNS
 may be due to the increased bone formation and decreased bone
 resorption, as was evidenced by the elevated level of serum alkaline
 phosphatase and decreased level of urinary deoxypyridinoline. PNS
 treatment is able to enhance BMD, bone strength, and prevent the
 deterioration of trabecular microarchitecture without hyperplastic
 effect on uterus. Therefore, PNS might be a potential alternative
 medicine for the prevention and treatment of postmenopausal
 osteoporosis.
 SN 1340-3443
 PD JUL
 PY 2010
 VL 64
 IS 3
 BP 336
 EP 345
 DI 10.1007/s11418-010-0416-7
 UT ISI:000278134500013
 A Chen, ZP
 U Zhu, JB
 Chen, HX
 Xiao, YY
 Feng, MS
 Cai, H
 Chen, J
 Cai, BC
 A Chen, Zhi-Peng
 F Zhu, Jia-Bi
 Chen, Hong-Xuan
 Xiao, Yan-Yu
 Feng, Ming-Sheng
 Cai, Hao
 Chen, Jun
 Cai, Bao-Chang
 T Synthesis of a novel polymer bile salts-(polyethylene
 I glycol)(2000)-bile salts and its application to the liver-selective
 targeting of liposomal DDB
 DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
 A Purpose: The objective of this study was to achieve a sustained and
 B targeted delivery of liposome to the liver, by modifying the
 phospholipid [phosphatidylcholine (PC)/cholesterol (10 : 1) liposomes
 with a novel polymer bile salts-(polyethylene glycol)(2000)-bile salts
 (BP2B). Methods: First, we generated a novel BP2B by
 N,N'-dicyclohexylcarbodiimide/4-dimethylaminopyridine
 esterification method and confirmed by Fourier transform infraredand
 H-1-NMR spectra. Second, we prepared the BP2B-modified liposomes
 (BP2BL) that included BP2B, and the effect of the weight ratios of
 BP2B/PC on entrapment efficiency was investigated and BP2B/PC = 3%
 (w/w) was determined as the optimum ratio for the
 4,4'-dimethoxy-5,6,5',6'-bi(methylenedioxy)-2,2'-bicarbomethoxybip
 henyl liposomes. And then, the ability of the liver target of BP2BL
 was studied by calculating the targeted parameters. Results and
 Discussion: All the results revealed that the introduction of
 polyoxyethylene chains could control interactions of bile salt
 moieties on liposome surfaces with the receptor compared with
 traditional liposomes (CL), marking BP2BL as a suitable carrier for
 hepatic parenchymal cell-specific and sustained targeting. It was
 suggested that liposomes containing such novel BP2B have great
 potential as drug delivery carriers for the liver-selective targeting
 that has targeted and sustained drug delivery.
 0363-9045
 2010
 10.3109/03639040903410342
 ISI:000278127500005
 PT J
 AU Chen, GH
 Luo, XC
 Zhang, JB
 Huang, WL
 AF Chen Guo-Hua
 Luo Xiao-Chuan
 Zhang Jiang-Bo
 Huang Wen-Long
 TI Synthesis and Biological Activities of 1-Acetyl-5-substituted
 Indoline Compounds
 SO CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 AB As benign prostate hyperplasia(BPH) is a common disease in elderly men,
 it is urgent to find new alpha(1)-adrenoceptor(AR) antagonists, the
 first choice for the therapy of BPH. On the basis of hybridization
 principle with 1-acetylindoline as the starting compound, two series
 of indoline derivatives 1-acetyl-5-{2-[4-(substituted phenoxy) ethyl]
 piperazin-l-yl} alkyl indoline and 1-acetyl-5-{2-[4-(substituted
 phenyl) piperazin-1-yl] alkyl} indoline were designed and synthesized.
 The structures of the target compounds were confirmed by H-1 NMR,
 elemental analysis, IR and MS. Preliminary pharmacological test show
 all the target compounds exhibit certain antagonism of alpha(1)-AR.
 Compounds 9h and 12l perform better than piperazine, and are worth of
 further research.
 SN 0251-0790
 PD MAY 10
 PY 2010
 VL 31
 IS 5
 BP 970
 EP 975
 UT ISI:000278159700022
 PT J
 AU Deng, J
 Wei, MC
 Yu, BY
 Chen, YJ
 AF Deng, Jing
 Wei, Maochen
 Yu, Boyang
 Chen, Yijun
 TI Efficient amplification of genes involved in microbial secondary
 metabolism by an improved genome walking method
 SO APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
 AB Genome walking is a commonly used technique for the identification of
 DNA sequences adjacent to known regions. Despite the development of
 various genome walking methods, nonspecific products are often
 produced in certain circumstances, especially when GC-rich DNA
 sequences are dealt with. To effectively resolve such technical issues,
 a simple nested polymerase chain reaction-based genome walking method
 has been developed by implementing a progressively decreased annealing
 temperature from 70A degrees C to 47.5A degrees C in the first round
 of amplification and a high annealing temperature of 65A degrees C in
 the second round of amplification. During the entire process, a lower
 ramp rate of 1.5A degrees C s(-1) and cooling rate of 2.5A degrees C
 s(-1) are performed to reach the annealing temperature. Using this
 method, we successfully obtained the upstream and downstream sequences
 of three GC-rich genes involved in the biosynthetic pathways of
 secondary metabolites from two bacterial genomes. The efficient
 amplification of DNA target longer than 1.5 Kb with GC content up to
 75.0% indicates that the present technique could be a valuable tool
 for the investigation of biosynthetic pathways of various secondary
 metabolites.
 SN 0175-7598
 PD JUN
 PY 2010
 VL 87
 IS 2
 BP 757
 EP 764
 DI 10.1007/s00253-010-2569-4
 UT ISI:000277959500036
 PT J
 AU Song, QX
 Jing, H
 Wu, HP
 Zhou, GH
 Kajiyama, T
 Kambara, H
 AF Song, Qinxin
 Jing, Hua
 Wu, Haiping
 Zhou, Guohua
 Kajiyama, Tomoharu
 Kambara, Hideki
 TI Gene expression analysis on a photodiode array-based bioluminescence
 analyzer by using sensitivity-improved SRPP
 SO ANALYST
 AB Most methods used for gene expression analysis are based on
 dye-labeling, which requires costly instruments. Recently a dye-free
 gene expression analysis method-SRPP (Sequence-tagged
 reverse-transcription polymerase chain reaction coupled with
 pyrosequencing) was developed to compare relative gene expression
 levels in different tissues, but the throughput of the SRPP assay is
 very limited due to the use of a photomultiplier tube (PMT)-based
 pyrosequencer for the detection. To increase the throughput of the SRPP
 assay, an inexpensive photodiode (PD) array-based bioluminescence
 analyzer (termed as "PD-based pyrosequencer'') was coupled to SRPP;
 however the low sensitivity of PD limited the wide application of SRPP.
 To enable SRPP analyzing low abundance genes in clinical samples,
 sequence-tagged gene-specific primers instead of sequence-tagged poly
 (T)(n) primers were used for reverse-transcription, and the SRPP
 sensitivity was thus improved more than 10 times. This improvement
 compensates the sensitivity loss due to the use of PD in a
 pyrosequencer. The accurate determination of the expression levels of
 ten prognostic marker genes (AL080059, MMP9, EXT1, ORC6L, AF052162,
 C9orf30, FBXO31, IGFBP5, ESM1, and RUNDC1) differing between normal
 tissues and tumor tissues of breast cancer patients demonstrated that
 SRPP using gene-specific RT primers coupled with the PD array-based
 bioluminescence analyzer is reliable, inexpensive, and sensitive in
 gene expression analysis.
 SN 0003-2654
 PY 2010
 VL 135
 IS 6
 BP 1315
 EP 1319
 DI 10.1039/c0an00012d
 UT ISI:000278011800020
 PT J
 AU Zhang, Y
 Chen, YD
 You, QD
 Zou, LY
 Yang, Y
 AF Zhang Yuan
 Chen Ya-Dong
 You Qi-Dong
 Zou Li-Yun
 Yang Yan
 TI Homology Modeling and Molecular Docking Studies on the Selectivity of
 HDAC1/HDAC8
 SO ACTA PHYSICO-CHIMICA SINICA
 AB Histone deacetylases (HDACs) have emerged as important anti. tumor
 targets in recent years. As HDACs comprise multiple isoforms and there
 are different physiological functions among various isoforms, the
 development of selective HDAC inhibitors has attracted a great deal
 of attention. This study focused on the discovery of selective HDAC1,
 HDAC8 inhibitors and specifically a homology model for HDAC1 was
 generated. A comparison was made between the HDAC1 homology model and
 the crystal structure of HDAC8, which showed that some active site
 residues were different from each other and these residues played
 important roles in the selectivity between HDAC1 and HDAC8. Two linear
 regression models were established based on the inhibitory activities
 against HDAC1, HDAC8 and the docking scores of 52 compounds. The
 developed linear regression models for HDAC1 and HDAC8 have non. cross
 validated correlation coefficients R-2 of 0.82 and 0.80, respectively,
 which indicates that the results are statistically significant. These
 models were used to predict the activities of the synthesized compounds
 and these prediction results can provide further insights into the
 selectivity of HDAC1, HDAC8.
 SN 1000-6818
 PD JUN
 PY 2010
 VL 26
 IS 6
 BP 1676
 EP 1686
 UT ISI:000278106600033
 PT J
 AU Liu, R
 Wang, M
 Duan, JA
 Guo, JM
 Tang, YP
 AF Liu, Rui
 Wang, Min
 Duan, Jin-ao
 Guo, Jian-ming
 Tang, Yu-ping
 TI Purification and identification of three novel antioxidant peptides
 from Cornu Bubali (water buffalo horn)
 SO PEPTIDES
 AB Cornu Bubali (water buffalo horn, WBH) has been used in Traditional
 Chinese Medicine (TCM) for thousands of years. In the present study,
 three peptides with antioxidant properties were purified from aqueous
 extract of Cornu Bubali (water buffalo horn, WBH) by consecutive
 chromatographic methods including gel filtration chromatography,
 ion-exchange chromatography and high performance liquid
 chromatography. The sequences of the three peptides were identified
 to be Gln-Tyr-Asp-Gln-Gly-Val (WBH-1, 708 Da),
 Tyr-Glu-Asp-Cys-Thr-Asp-Cys-Gly-Asn (WBH-2, 1018 Da) and
 Ala-Ala-Asp-Asn-Ala-Asn-Glu-Leu-Phe-Pro-Pro-Asn (WBH-3, 1271 Da) by
 matrix assisted laser desorption ionization
 time-of-flight/time-of-flight mass spectrometry (MALDI-LIFT-TOF/TOF
 MS). The antioxidant activity of these peptides was tested using
 1-dipheny1-2-picrylhydrazyl (DPPH) scavenging assay directly.
 Methylthiazol tetrazolium (MTT) assay and lactate dehydrogenase (LDH)
 release assay were also used to evaluate the protection of peptides
 against hydrogen peroxide (H2O2) induced injury. The results showed
 that these peptides could reduce the DPPH radical and protect rat
 cerebral microvascular endothelial cells (rCMECs) against
 H2O2-induced injury, thus demonstrating that these peptides had
 antioxidant activity. These results suggest that WBH-1, WBH-2 and
 WBH-3, isolated from the aqueous extract of water buffalo horn are
 natural antioxidants and may contribute to the efficacy of WBH. (C)
 2010 Elsevier Inc. All rights reserved.
 SN 0196-9781
 PD MAY
 PY 2010
 VL 31
 IS 5
 BP 786
 EP 793
 DI 10.1016/j.peptides.2010.02.016
 UT ISI:000277768400002
 PT J
 AU Xu, FG
 Liu, Y
 Song, R
 Dong, HJ
 Zhang, ZJ
 AF Xu, Fengguo
 Liu, Ying
 Song, Rui
 Dong, Haijuan
 Zhang, Zunjian
 TI Constituents of Da-Cheng-Qi Decoction and its Parent Herbal Medicines
 Determined by LC-MS/MS
 SO NATURAL PRODUCT COMMUNICATIONS
 AB Da-Cheng-Qi decoction (DCQD) is a purgative prescription used in China
 and East Asia. To profile the constituents of this complex traditional
 Chinese medicine (TCM), a high-performance liquid chromatographic,
 electrospray ionization, tandem mass spectrometric (HPLC-ESI/MS/MS)
 analytical method was developed. After separation on a reversed-phase
 C18 analytical column using gradient elution, samples were analyzed
 by ESI-MS/MS in negative mode. As a result, a total of 37 compounds
 were detected, of which two tannins, three anthraquinones, two
 sennosides, Five flavonoids and two lignans were unambiguously
 identified by comparison with standard compounds, and sixteen
 compounds were either tentatively identified or deduced according to
 their MS/MS data. The fragmentation pathways of many of the observed
 compounds, such as the tannins and lignans are reported for the first
 time. In addition, the identity of each peak in DCQD was explored by
 comparison with those of its three constituent herbs. The results
 indicated that tannins, anthraquinones and sennosides in DCQD
 originated from Radix et Rhizoma Rhei, flavonoids from Fructus Aurantii
 Immaturus, and lignans from Cortex Magnoliae officinalis. The present
 study provides an example of chemical constitution profiling in complex
 TCM systems using LC/MS/MS.
 SN 1934-578X
 PD MAY
 PY 2010
 VL 5
 IS 5
 BP 789
 EP 794
 UT ISI:000277750200023
 PT J
 AU Xu, FG
 Liu, Y
 Dong, HJ
 Song, R
 Zhang, ZJ
 AF Xu, Fengguo
 Liu, Ying
 Dong, Haijuan
 Song, Rui
 Zhang, Zunjian
 TI Pharmacokinetic Comparison in Rats of Six Bioactive Compounds Between
 Da-Cheng-Qi Decoction and its Parent Herbal Medicines
 SO NATURAL PRODUCT COMMUNICATIONS
 AB Da-Cheng-Qi decoction (DCQD) is a purgative compound prescription used
 in China and East Asia. In this paper, pharmacokinetic differences of
 six major active components (rhein, emodin, aloe-emodin, magnolol,
 naringenin and hesperetin) between DCQD and its three constitutional
 herbal medicines i.e. Radix et Rhizoma Rhei, Cortex Magnoliae
 officinalis and Fructus Aurantii Immantrus were investigated in rats
 after oral administration. Plasma samples were analyzed for the
 quantification of the six active components using validated LC-MS/MS
 methods. Unpaired Student's t-test was used for statistical
 comparison. Significant differences (p<0.05) in the main
 pharmacokinetic parameters for rhein, emodin, aloe-emodin, magnolol,
 naringenin and hesperetin were found between DCQD and the decoction
 of its constitutional single herbal medicines, which demonstrated the
 presence of drug-drug interactions between these constitutional raw
 materials of DCQD occurring either in the procedure of decoction or
 during ADME process.
 SN 1934-578X
 PD MAY
 PY 2010
 VL 5
 IS 5
 BP 795
 EP 800
 UT ISI:000277750200024
 PT J
 AU Zhou, JP
 Qian, H
 Zhang, HB
 Gao, H
 Huang, WL
 Zhu, XY
 Ni, SAJ
 Zhang, CT
 AF Zhou, Jinpei
 Qian, Hai
 Zhang, Huibin
 Gao, Hui
 Huang, Wenlong
 Zhu, Xiaoyun
 Ni, Shuaijian
 Zhang, Chuntao
 TI Design, Synthesis and Biological Evaluation of Benzopyran Derivatives
 as K-ATP Channel Openers
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB In order to complete the SAR and discover new potent and selective PCOs,
 some changes were made to the C-4 and C-2 substitutions of cromakalim.
 A series of 4 -amino acid substituted -2, 2-dialkylchromans
 structurally related to cromakalim were synthesized and evaluated, as
 ATP-sensitive potassium channel openers (8a-l). Preliminary
 biological tests suggested that these compounds exhibited potent to
 mild relaxation activity of the KCl-contracted rat aortic strips.
 Compounds 8b (IC50 = 0.25 mu M), 8f (IC50 = 6.44 mu M) and 8j (IC50
 = 8.65 mu M) exhibited commendable opening activity of potassium
 channels. In addition to anti-hypertension, these compounds can also
 be considered as lead candidates for the further development of
 myocardial antiischemic drugs.
 SN 1570-1808
 PD JUL
 PY 2010
 VL 7
 IS 6
 BP 415
 EP 420
 UT ISI:000277887000005
 PT J
 AU Dong, Y
 Xiang, BR
 Wang, T
 Liu, H
 Qu, LB
 AF Dong, Ying
 Xiang, Bingren
 Wang, Teng
 Liu, Hao
 Qu, Lingbo
 TI Rough set-based SAR analysis: An inductive method
 SO EXPERT SYSTEMS WITH APPLICATIONS
 AB Rough set algorithm was used as a new methodology to build
 structure-activity relationship (SAR) models in this paper. It acted
 as feature selector and nonlinear rule generator. The SAR model
 expressed as human readable if-then rules was developed for the
 inhibition of the serine/threonine kinase CDK1/cyclinB by compounds
 from the indirubin inhibitor family. The feature selection ability of
 rough set algorithm was compared with the build-in approaches
 (CfsSubsetEval and ConsistencySubsetEval) in Weka under leave-one-out
 (LOO) and 10-fold cross-validation. Through training a set of 31
 objects, a rule-based SAR model had been built with a reduct generated
 by rough set. The predictability of the model was evaluated by an
 external test set of 16 compounds. The existing powerful approaches,
 such as the decision tree learners, neural network, support vector
 classifier and LogitBoost approaches, were used to verify the
 performance of rough set method. It revealed that rough set method
 should play important role in data preprocessing and model building
 of nonlinear SAR analysis. The advantages and limitations of rough
 set-based SAR analysis were discussed. The results were satisfactorily
 in accordance with the available understanding of cocrystal structures
 and 3D QSAR models. (C) 2009 Elsevier Ltd. All rights reserved.
 SN 0957-4174
 PD JUL
 PY 2010
 VL 37
 IS 7
 BP 5032
 EP 5039
 DI 10.1016/j.eswa.2009.12.008
 UT ISI:000277726300036
 PT J
 AU Zhou, YQ
 Li, WZ
 Chen, LY
 Ma, SW
 Ping, L
 Yang, ZL
 AF Zhou, Yongqiang
 Li, Weize
 Chen, Lvyi
 Ma, Shuwei
 Ping, Li
 Yang, Zhonglin
 TI Enhancement of intestinal absorption of akebia saponin D by borneol
 and probenecid in situ and in vitro
 SO ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
 AB Akebia saponin D is a typical bioactive triterpenoid saponin isolated
 the rhizome of Dipsacus asper Wall. Our previous studies demonstrated
 that the oral bioavailability of akebia saponin D was very low, but
 the underlying mechanisms remained unknown. The present study aims to
 investigate the intestinal absorptive characteristics of akebia
 saponin D as well as the absorptive transport behavior influenced by
 co-administration of three absorption-enhancing agents and three
 efflux protein inhibitors using an in vitro everted gut sac method and
 an in situ intestinal perfusion model. The results showed that akebia
 saponin D had a quite limited intestinal permeability, and there was
 a non-linear increase in transepithelial transportation with
 increasing concentrations of akebia saponin D. The absorption of akebia
 saponin D was intestinal segment selective and the small intestine was
 the best absorptive site. Among three absorption promoters, borneol
 could significantly improve the permeability of akebia saponin D across
 ileum, while Tween-80 and DMSO had almost no absorption-enhancing
 effect. In addition, verapamil, probenecid and pantoprazole in the
 perfusates were used in this study as modulators of transporters such
 as P-glycoprotein, MRPs and BCRP in the intestinal mucosa,
 respectively. The results exhibited that the ileal permeability of
 akebia saponin D was markedly elevated by the co-administration of
 probenecid, indicating that akebia saponin D may be likely a substrate
 of MRPs. The above-mentioned results suggest that akebia saponin D has
 a poor intestinal absorption not only due to its poor transepithelial
 permeability but also owing to the contribution of efflux transporters
 such as MRPs in the intestine. (C) 2010 Elsevier B.V. All rights
 reserved.
 SN 1382-6689
 PD MAY
 PY 2010
 VL 29
 IS 3
 BP 229
 EP 234
 DI 10.1016/j.etap.2010.01.004
 UT ISI:000277906800006
 PT J
 AU Gao, F
 Ding, L
 Ma, PC
 Wu, F
 AF Gao, Fang
 Ding, Li
 Ma, Pengcheng
 Wu, Fei
 TI Simultaneous Analysis of Zofenopril and Its Active Metabolite
 Zofenoprilat in Human Plasma by LC-ESI-MS Using Pre-Column
 Derivatization with p-Bromophenacyl Bromide
 SO CHROMATOGRAPHIA
 AB Zofenoprilat is an active metabolite of zofenopril, which is very
 unstable in plasma because of oxidative degradation of its thiol group.
 In this method, p-bromophenacyl bromide was used as derivatization
 reagent, immediately after plasma separation, to react with the free
 thiol group of zofenoprilat and form the derivative
 zofenoprilat-p-BPB. After acidification with 50% acetic acid, the
 derivatized plasma samples were extracted with methyl tert-butyl ether
 and separated on a C-18 column with 40:60 (v/v) 10 mM ammonium acetate
 buffer solution containing 0.1% formic acid-acetonitrile as mobile
 phase. Calibration plots were linear over the concentration range 1-500
 ng mL(-1) for zofenopril and 2-1,800 ng mL(-1) for zofenoprilat. The
 method was successfully used to study the bioavailability of zofenopril
 calcium capsules relative to that of zofenopril calcium tablets in
 healthy Chinese volunteers.
 SN 0009-5893
 PD JUN
 PY 2010
 VL 71
 IS 11-12
 BP 1007
 EP 1014
 DI 10.1365/s10337-010-1606-x
 UT ISI:000277936600006
 PT J
 AU Song, R
 Xu, L
 Zhang, ZJ
 Tian, Y
 Xu, FG
 Dong, HJ
 AF Song, Rui
 Xu, Lei
 Zhang, Zunjian
 Tian, Yuan
 Xu, Fengguo
 Dong, Haijuan
 TI Determination of Gallic Acid in Rat Plasma by LC-MS-MS
 SO CHROMATOGRAPHIA
 AB Liquid chromatography-electrospray ionization tandem mass
 spectrometry has been used for rapid, selective, and sensitive
 quantitative analysis of gallic acid in rat plasma. Sample pretreatment
 involved a one-step extraction using ethyl acetate with protocatechic
 acid as internal standard. Separation was on a C-18 column using an
 isocratic mobile phase, consisting of methanol-0.1% aqueous formic
 acid (40:60, v/v) at 0.2 mL min(-1). The stability of gallic acid was
 evaluated in acidified and non-acidified plasma. The method was
 validated then successfully applied to a pharmacokinetic study in rats
 after oral administration of rhubarb extract.
 SN 0009-5893
 PD JUN
 PY 2010
 VL 71
 IS 11-12
 BP 1107
 EP 1111
 DI 10.1365/s10337-010-1565-2
 UT ISI:000277936600020
 PT J
 AU Xie, HT
 Wang, GJ
 Xu, MJ
 Jia, YW
 Li, H
 Sun, JG
 Li, P
 AF Xie, Hai-Tang
 Wang, Guang-Ji
 Xu, Mei-Juan
 Jia, Yuan-Wei
 Li, Hao
 Sun, Jian-Guo
 Li, Peng
 TI A New LC-MS-MS Method for Quantitative Analysis of Adefovir, and Its
 Use for Pharmacokinetic Studies in Healthy Chinese Volunteers
 SO CHROMATOGRAPHIA
 AB A rapid and sensitive liquid chromatographic-tandem mass spectrometric
 method for analysis of adefovir in human plasma has been developed and
 validated. After protein precipitation and evaporation, 10 mu L
 supernatant was injected for reversed-phase LC separation. Adefovir
 and the internal standard (acyclovir) were monitored in selected
 reaction monitoring (SRM) mode at m/z 274.10 -> 256.00 and 226.10 ->
 152.00, respectively. The calibration plot was linear over the
 concentration range 0.5-100 ng mL(-1), and correlation coefficients
 were > 0.999. Mean intra-day and inter-day accuracy ranged from 89.43
 to 93.20% and from 91.40 to 95.57%, respectively, and mean intra-day
 and inter-day precision was between 2.40 and 7.66% and between 5.60
 and 10.47%, respectively. The method was successfully applied to a
 Phase I pharmacokinetic study of adefovir after oral administration
 of adefovir dipivoxil capsules at doses of 5, 10, and 20 mg to
 twenty-four healthy Chinese volunteers.
 SN 0009-5893
 PD APR
 PY 2010
 VL 71
 IS 7-8
 BP 587
 EP 593
 DI 10.1365/s10337-010-1474-4
 UT ISI:000277710400005
 PT J
 AU Fan, XM
 Ji, YB
 Zhu, DN
 AF Fan, Xiao-Mei
 Ji, Yi-Bing
 Zhu, Da-Ni
 TI An Integrated Approach Based on Experimental Designs for Fingerprint
 Development of the Complex Herbal Prescription Sheng-Mai-San by MEKC
 SO CHROMATOGRAPHIA
 AB An integrated strategy based on experimental designs for the
 development, optimization and validation of the fingerprint method of
 Sheng-Mai-San by MEKC has been described. Orthogonal and sequential
 uniform designs were employed to select important experimental
 parameters and optimize CE conditions. Method validation was performed
 in terms of injection precision, sample stability test and robustness
 testing. Additionally, conventional modeling method was used to
 predict the optimum separation conditions for comparative purpose. The
 strategy described can also be utilized for fingerprint development
 in the quality control of other herbal medicines.
 SN 0009-5893
 PD APR
 PY 2010
 VL 71
 IS 7-8
 BP 667
 EP 677
 DI 10.1365/s10337-010-1519-8
 UT ISI:000277710400016
 A Liu, B
 U You, QD
 Li, ZY
 A Liu, Bao
 F You, Qi Dong
 Li, Zhi Yu
 T Design, synthesis and antitumor activity of
 I 6,7-disubstituted-4-(heteroarylamino)quinoline-3-carbonitrile
 derivatives
 CHINESE CHEMICAL LETTERS
 A A series of new
 B 6,7-disubstituted-4-(benzothiazol-6-ylamino)quinoline-3-carbonitri
 le derivatives (12a-I) were synthesized. The cytotoxicity of 12 new
 compounds was evaluated in AGS, HepG2 and HT-29 cell lines The results
 showed that compounds 12g, 12h, 12i, 12k and 121 displayed more potent
 cytotoxic activities than Bosutinib, compound 121 exhibited the most
 potent antitumor activity among the tested compounds. (C) 2010 Qi Dong
 You Published by Elsevier B V. on behalf of Chinese Chemical Society.
 All rights reserved.
 1001-8417
 2010
 10.1016/j.cclet.2010.01.016
 ISI:000277862400012
 PT J
 AU Wang, QZ
 Liang, JY
 Feng, X
 AF Wang, Qi Zhi
 Liang, Jing Yu
 Feng, Xu
 TI Evodiagenine and dievodiamine, two new indole alkaloids from Evodia
 rutaecarpa
 SO CHINESE CHEMICAL LETTERS
 AB Two new indole alkaloids, evodiagenine 1 and dievodiamine 2 were
 isolated from the fruits of Evodia rutaecarpa (Juss) Benth. The
 structure of compounds 1 and 2 were elucidated by comprehensive
 spectroscopic analysis and compound 1 was confirmed by X-ray
 crystallographic analysis (C) 2009 Xu Feng. Published by Elsevier B.V.
 on behalf of Chinese Chemical Society. All rights reserved.
 SN 1001-8417
 PD MAY
 PY 2010
 VL 21
 IS 5
 BP 596
 EP 599
 DI 10.1016/j.cclet.2009.12.002
 UT ISI:000277862400023
 PT J
 AU Ye, XL
 Zhou, W
 Li, YQ
 Sun, YH
 Zhang, YH
 Ji, H
 Lai, YS
 AF Ye, Xiaolei
 Zhou, Wu
 Li, Yongqi
 Sun, Yihua
 Zhang, Yihua
 Ji, Hui
 Lai, Yisheng
 TI Darbufelone, a novel anti-inflammatory drug, induces growth inhibition
 of lung cancer cells both in vitro and in vivo
 SO CANCER CHEMOTHERAPY AND PHARMACOLOGY
 AB Inflammation plays a crucial role in the development of lung cancer.
 Accumulated studies have proved that non-steroidal anti-inflammatory
 drugs (NSAIDs) which block inflammation by their actions on arachidonic
 acid (AA) metabolism have a potential role in cancer chemotherapy and
 chemoprevention. The aim of our study was to investigate whether
 darbufelone, a novel anti-inflammatory drug, has anticancer effects
 in lung cancer.
 Human non-small cell lung cancer cell lines were treated with
 darbufelone at various doses and time points for analysis of cell
 viability, cell cycle, and apoptosis in vitro. The in vivo effect of
 darbufelone was assessed in Lewis lung carcinoma mice model.
 Darbufelone inhibited the proliferation of non-small cell lung cancer
 cell lines in a dose-dependent manner, and induced cell cycle arrest
 at G0/G1 phase through up-regulation of p27 expression. Treatment with
 darbufelone also induced apoptosis by activating caspase-3 and
 caspase-8. Lewis lung carcinoma growth was also significantly
 inhibited by darbufelone treatment at daily dose of 80 mg/kg.
 Taken together, these studies suggested that darbufelone, an
 anti-inflammation drug, might represent a novel therapeutic approach
 for lung cancer treatment.
 SN 0344-5704
 PD JUL
 PY 2010
 VL 66
 IS 2
 BP 277
 EP 285
 DI 10.1007/s00280-009-1161-z
 UT ISI:000277785600009
 PT J
 AU Jin, L
 Zhu, AH
 Wang, Y
 Lu, Y
 Liu, JJ
 AF Jin Liang
 Zhu Aihua
 Wang Yu
 Lu Yong
 Liu Jingjing
 TI HSP65 serves as an immunogenic carrier for a diabetogenic peptide P277
 inducing anti-inflammatory immune response in NOD mice by nasal
 administration
 SO VACCINE
 AB Mucosal administration of autoantigen 1451,65 can induce
 anti-inflammatory immune response and decrease organ-specific
 inflammation and disease in several models of autoimmunity, such as
 arthritis and atherosclerosis We have been interested in whether the
 HSP65 serves as an immunogenic carrier for a diabetogenic peptide P277
 can also Induce anti-inflammatory immune response in NOD mice by
 mucosal administration Thus, the dual functions of anti-type 1 diabetes
 of HSP65 and P277 will be obtained To test this hypothesis, we examined
 the effect of intranasal vaccination with P277 tandem repeat sequences
 carried by HSP65 in the absence of adjuvants on autoimmune diabetes
 in NOD mice. We found a significant decrease in the incidence of
 diabetes, inhibition of insulitis, reduction in IgG2a isotype
 antibodies to P277 and proinflammatory cytokines IFN-gamma and IL-2
 secretion, increased IgG1, IgG2b subclass antibodies to P277 and
 anti-inflammatory cytokmes IL-10 and IL-4 secretion, and reduced
 proliferation in nasal administration of the fusion protein HSP65-6
 x P277 Our results demonstrate that HSP65 may serve as a particularly
 advantageous carrier for P277-based vaccines and mucosal
 administration may be a therapeutic approach for treatment of type 1
 diabetes. (C) 2010 Elsevier Ltd. All rights reserved
 SN 0264-410X
 PD APR 26
 PY 2010
 VL 28
 IS 19
 BP 3312
 EP 3317
 DI 10.1016/j.vaccine.2010.02.100
 UT ISI:000277677000008
 PT J
 AU Liu, L
 Jiang, ZZ
 Liu, J
 Huang, X
 Wang, T
 Liu, J
 Zhang, Y
 Zhou, ZX
 Guo, JL
 Yang, LN
 Chen, Y
 Zhang, LY
 AF Liu, Li
 Jiang, Zhenzhou
 Liu, Jing
 Huang, Xin
 Wang, Tao
 Liu, Jun
 Zhang, Yun
 Zhou, Zhixing
 Guo, Jianlu
 Yang, Lina
 Chen, Yun
 Zhang, Luyong
 TI Sex differences in subacute toxicity and hepatic microsomal metabolism
 of triptolide in rats
 SO TOXICOLOGY
 AB Triptolide, a major active component of Tripterygium wilfordii Hook
 F (TWHF), has multiple pharmacological activities. However, its
 clinical use is often limited by its severe toxicity. In the present
 study, we evaluated the oral toxicity of triptolide in Sprague-Dawley
 rats for 28 days at the dosages of 0, 200 and 400 mu g/kg/day,
 respectively. Significant difference in the toxicity of triptolide at
 400 mu g/kg was found between different sexes. The triptolide-treated
 female rats showed many abnormalities, including anorexia, diarrhea,
 leanness, suppression of weight gain and food intake, fatty liver,
 splenomegaly and atrophy of ovaries. In contrast, no such abnormalities
 were observed in male rats except for the significant reproductive
 toxicity. Furthermore, the metabolism of triptolide in liver
 microsomes from both sexes was investigated by HPLC. A greater rate
 of triptolide metabolism was observed in male rat hepatic microsomes,
 suggesting that one of the cytochrome P450s (CYPs) responsible for
 triptolide metabolism is male-specific or predominant at least. The
 inhibition experiments with CYP inhibitors showed that CYP3A and CYP2B
 were mainly involved in the metabolism of triptolide. In addition,
 since CYP3A2 is a male-predominant form in rats, significant sex
 difference in the metabolism of triptolide disappeared in vitro after
 anti-rat CYP3A2 antibody pretreatment. Results suggested that CYP3A2
 made an important contribution to the sex-related metabolism of
 triptolide, which may result in the sex differences in triptolide
 toxicity. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
 SN 0300-483X
 PD APR 30
 PY 2010
 VL 271
 IS 1-2
 BP 57
 EP 63
 DI 10.1016/j.tox.2010.03.004
 UT ISI:000277739900009
 PT J
 AU Yue, L
 Zhang, F
 Wang, ZX
 AF Yue, Long
 Zhang, Feng
 Wang, Zhixiang
 TI Study on Ultrasonic Extraction of Gastrodin from Gastrodia elata Bl.
 SO SEPARATION SCIENCE AND TECHNOLOGY
 AB Gastrodin, a pharmacologically active constituent, was ultrasonically
 extracted from gastrodia elata Bl. in the aqueous solution. The effects
 of six parameters including ethanol-water compositions, extraction
 time, extraction temperature, particle size, solvent volume, and
 ultrasonic power on the extraction yield of gastrodin were
 investigated. According to the orthogonal design, the optimal
 extraction conditions was explored as extraction temperature 60
 degrees C, extraction time 50 minutes, ultrasonic power 126W, solvent
 volume 8mL center dot g-1, ethanol-water compositions 70%, and particle
 size 10-20 mesh. Though the yield of gastrodin via ultrasonic
 extraction was about 0.01% lower than that from the reflux extraction,
 the extraction time of the ultrasonic extraction was greatly shortened.
 Therefore, ultrasonic extraction has high efficiency and is proved to
 be very valuable in the extraction of gastrodin from gastrodia elata
 SN 0149-6395
 PY 2010
 VL 45
 IS 6
 BP 832
 EP 838
 DI 10.1080/01496390903566671
 UT ISI:000277727800014
 PT J
 AU Ya, J
 Zhang, XQ
 Wang, Y
 Zhang, QW
 Chen, JX
 Ye, WC
 AF Ya, Ji
 Zhang, Xiao-Qi
 Wang, Ying
 Zhang, Qing-Wen
 Chen, Jian-Xin
 Ye, Wen-Cai
 TI Two new phenolic compounds from the roots of Ficus hirta
 SO NATURAL PRODUCT RESEARCH
 AB A new prenylcoumarin, 5-methoxyl-4,2'-epoxy-3-(4',
 5'-dihydroxyphenyl)-linear pyranocoumarin (1), and a new flavonoid,
 3-acetyl-3,5,4'-trihydroxy-7-methoxylflavone (2), were isolated from
 the roots of Ficus hirta. Their structures were elucidated by
 spectroscopic methods including 1D-, 2D- NMR and HR-ESI-MS.
 SN 1478-6419
 PY 2010
 VL 24
 IS 7
 BP 621
 EP 625
 DI 10.1080/14786410902847377
 UT ISI:000277661200003
 PT J
 AU Zhang, ZB
 Li, ZC
 Tian, J
 Jiang, W
 Wang, Y
 Zhang, XJ
 Li, ZR
 You, QD
 Shapiro, JI
 Si, SY
 Xie, ZJ
 AF Zhang, Zhongbing
 Li, Zhichuan
 Tian, Jiang
 Jiang, Wei
 Wang, Yin
 Zhang, Xiaojin
 Li, Zhuorong
 You, Qidong
 Shapiro, Joseph I.
 Si, Shuyi
 Xie, Zijian
 TI Identification of Hydroxyxanthones as Na/K-ATPase Ligands
 SO MOLECULAR PHARMACOLOGY
 AB We have screened a chemical library and identified several novel
 structures of Na/K-ATPase inhibitors. One group of these inhibitors
 belongs to polyphenolic xanthone derivatives. Functional
 characterization reveals the following properties of this group of
 inhibitors. First, like ouabain, they are potent inhibitors of the
 purified Na/K-ATPase. Second, their effects on the Na/K-ATPase depend
 on the number and position of phenolic groups. Methylation of these
 phenolic groups reduces the inhibitory effect. Third, further
 characterization of the most potent xanthone derivative, MB7
 (3,4,5,6-tetrahydroxyxanthone), reveals that it does not change either
 Na+ or ATP affinity of the enzyme. Finally, unlike that of ouabain,
 the inhibitory effect of MB7 on Na/K-ATPase is not antagonized by K+.
 Moreover, MB7 does not activate the receptor Na/K-ATPase/Src complex
 and fails to stimulate protein kinase cascades in cultured cells. Thus,
 we have identified a group of novel Na/K-ATPase ligands that can inhibit
 the pumping function without stimulating the signaling function of
 Na/K-ATPase.
 SN 0026-895X
 PD JUN
 PY 2010
 VL 77
 IS 6
 BP 961
 EP 967
 DI 10.1124/mol.110.063974
 UT ISI:000277751600009
 PT J
 AU Feng, X
 Wang, JS
 Luo, J
 Kong, LY
 AF Feng, Xin
 Wang, Jun-Song
 Luo, Jun
 Kong, Ling-Yi
 TI A pair of sesquiterpene glucosides from the leaves of Nicotiana tabacum
 SO JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
 AB A pair of sesquiterpene glucosides,
 3-hydroxysolavetivone--d-glucoside A (1) and
 3-hydroxysolavetivone--d-glucoside B (2), have been isolated from the
 leaves of Nicotiana tabacum. The former is a new compound, while the
 latter is a known one. Their structures were established by
 spectroscopic methods including 1H, 13C, and 2D NMR. The relative
 configuration of C-3 in compound 2 was revised by NOESY experiment.
 SN 1028-6020
 PY 2010
 VL 12
 IS 3
 BP 252
 EP 256
 DI 10.1080/10286020903550947
 UT ISI:000277569900013
 PT J
 AU Liu, W
 Wang, HY
 Pang, XB
 Yao, WB
 Gao, XD
 AF Liu, Wei
 Wang, Hengyu
 Pang, Xiubing
 Yao, Wenbing
 Gao, Xiangdong
 TI Characterization and antioxidant activity of two low-molecular-weight
 polysaccharides purified from the fruiting bodies of Ganoderma lucidum
 SO INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
 AB Two low-molecular-weight polysaccharides, GLP(L)1 and GLP(L)2,
 purified from a crude Ganoderma lucidum polysaccharide preparation
 GLPP were investigated for their physicochemical properties. structure
 characterization and antioxidant activities The results indicated that
 GLP(L)1 was a glucan with an average molecular weight of 5 2 kDa, while
 GLP(L)2 was composed of glucose, galactose and mannose in a ratio of
 29 1 8 1.0 with the average molecular weight of 15.4 kDa GLP(L)1 and
 GLP(L)2 had similar structure characteristic which contained linkages
 such as -> 3)-Glcp-(1 ->,-> 4)-Glcp-(1 ->,-> 6)-Glcp-(1 ->,->
 3,6)-Glcp-(1 ->, and -> 4,6 )-Glcp-(1 -> in the percentage ratio of
 21.9 20 3 23.7 24 0 3 7 and 23 0 34 6 7 0 14.1 3.0 in the backbone or
 branches, respectively Antioxidant results showed that both GLP(L)1
 and GLP(L)2 exhibited antioxidant activities while GLP(L)1 was more
 effective in free radicals scavenging and Fe2+ chelating.
 Low-molecular-weight polysaccharide seems to play an important role
 in the exploration of natural antioxidants in food industry and
 pharmaceuticals (C) 2010 Elsevier B V All rights reserved
 SN 0141-8130
 PD MAY 1
 PY 2010
 VL 46
 IS 4
 BP 451
 EP 457
 DI 10.1016/j.ijbiomac.2010.02.006
 UT ISI:000277676700011
 PT J
 AU Cao, Y
 Tan, NH
 Chen, JJ
 Zeng, GZ
 Ma, YB
 Wu, YP
 Yan, H
 Yang, J
 Lu, LF
 Wang, Q
 AF Cao, Yuan
 Tan, Nin-Hua
 Chen, Ji-Jun
 Zeng, Guang-Zhi
 Ma, Yun-Bao
 Wu, Yong-Ping
 Yan, He
 Yang, Jie
 Lu, Lai-Feng
 Wang, Qiang
 TI Bioactive flavones and biflavones from Selaginella moellendorffii
 Hieron
 SO FITOTERAPIA
 AB Three new flavones named 5-carboxymethyl-4',7-dihydroxyflavone (1),
 its ethyl ester (2) and butyl ester (3) were isolated from the herb
 Selaginella moellendorffii Hieron., together with ten known compounds.
 Their structures were elucidated on the basis of spectroscopic and
 chemical analysis. Selected compounds were evaluated for their
 anti-HBV and cytotoxic activity. Among them, compounds 2 and 3
 displayed inhibitory activity in vitro on hepatitis B virus (HBV)
 surface antigen (HBsAg) secretion of the Hep G2.2.15 cell line with
 IC50 values of 0.17 mg/ml and 0.46 mg/ml, and on HBV e antigen (HBeAg)
 secretion with IC50 values of 0.42 mg/ml and 0.42 mg/ml, respectively.
 Compounds 7.8. 10 and 12 exhibited selective cytotoxicity against the
 three human cancer cell lines tested. (C) 2009 Elsevier By. All rights
 reserved.
 SN 0367-326X
 PD JUN
 PY 2010
 VL 81
 IS 4
 BP 253
 EP 258
 DI 10.1016/j.fitote.2009.09.007
 UT ISI:000277699400006
 PT J
 AU Peng, HJ
 Dai, DZ
 Ji, H
 Dai, Y
 AF Peng, Hong-Jun
 Dai, De-Zai
 Ji, Hui
 Dai, Yin
 TI The separate roles of endothelin receptors participate in remodeling
 of matrix metalloproteinase and connexin 43 of cardiac fibroblasts in
 maladaptive response to isoproterenol
 SO EUROPEAN JOURNAL OF PHARMACOLOGY
 AB Stress may affect gap junction connexin 43 and matrix
 metalloproteinase-2/9 (MMP-2/9) in cardiac fibroblasts, potentially
 contributing to worsening cardiac function and arrhythmias. Cardiac
 fibroblasts isolated from neonatal rat were incubated with
 isoproterenol at 3 x 10(-7) M to mimic stress and were treated with
 either PD156707 or IRL-1038 (selective antagonists for endothelin A
 and B receptor respectively) and CPU0213 (a dual endothelin A/B
 receptor antagonist) at 1 x 10(-8) M, 3 x 10(-8) M or 1 x 10(-7) M.
 RT-PCR and Western blotting were conducted. Upregulation of the two
 endothelin receptors, MMP-2/9 and NADPH oxidase subunits (p22phox and
 p47phox), and downregulation of connexin 43 in cardiac fibroblasts were
 found in the presence of isoproterenol and were attenuated by the
 selective blockers PD156707 and IRL-1038 in a dose-dependent manner.
 IRL-1038 was less effective. CPU0213 appeared to be more effective than
 the two selective blockers in blocking these changes. Changes in
 cardiac fibroblasts in response to isoproterenol mediated by
 upregulation of the endothelin-NADPH oxidase pathway may play a role
 in deteriorating cardiac function and arrhythmias. The endothelin A
 receptor has a major role, relative to the endothelin B receptor, in
 the remodeling of cardiac fibroblasts during isoproterenol
 stimulation. CPU0213, a dual endothelin receptor A/B blocker, seems
 to be more effective in normalizing these changes than do the selective
 endothelin receptor antagonists. (C) 2010 Elsevier B.V. All rights
 reserved.
 SN 0014-2999
 PD MAY 25
 PY 2010
 VL 634
 IS 1-3
 BP 101
 EP 106
 DI 10.1016/j.ejphar.2010.02.001
 UT ISI:000277554900015
 PT J
 AU Zou, S
 Zhang, X
 Yao, WB
 Niu, YG
 Gao, XD
 AF Zou, Shan
 Zhang, Xian
 Yao, Wenbing
 Niu, Yuge
 Gao, Xiangdong
 TI Structure characterization and hypoglycemic activity of a
 polysaccharide isolated from the fruit of Lycium barbarum L.
 SO CARBOHYDRATE POLYMERS
 AB An acidic polysaccharide LBP-1 isolated from the fruit of Lycium
 barbarum L. was purified by ion-exchanged column. Structure
 characterization and in vitro hypoglycemic activity of LBP-1 were
 determined. Chemical analysis indicated LBP-1 was composed with
 rhamnose, arabinose, xylose, galactose, mannose, galacturonic acid =
 1.00:7.85:0.37:0.65:3.01:8.16 with average molecular weight of 2.25
 x 10(6) Da. The structure features of LBP-1 were investigated by FT-IR,
 GC-MS, H-1-NMR and C-13-NMR. The backbone were mainly composed of
 (1,5)-linkage arabinose, (1,4)-linkage galacturonic acid,
 -(1)-mannose-(3,6)-linkage and terminated with -(1)-mannose. LBP-1
 protected the pancreatic islets cells from oxidative damage and
 enhanced cell survival ratio significantly. Moreover, its application
 inhibited the development of insulin resistance in HepG2 cells. This
 paper indicates the beneficial effect of LBP-1 and explores a potential
 hypoglycemic functional food and pharmaceuticals with definitely
 structure. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0144-8617
 PD MAY 16
 PY 2010
 VL 80
 IS 4
 BP 1161
 EP 1167
 DI 10.1016/j.carbpol.2010.01.038
 UT ISI:000277636200020
 PT J
 AU Qiu, FR
 Wang, GJ
 Zhang, R
 Sun, JG
 Jiang, J
 Ma, YM
 AF Qiu, Furong
 Wang, Guangji
 Zhang, Rong
 Sun, Jianguo
 Jiang, Jian
 Ma, Yueming
 TI Effect of danshen extract on the activity of CYP3A4 in healthy
 volunteers
 SO BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
 AB center dot Many cytochrome P450 mediated interactions have been
 reported between drug and herbal medicines. In particular, CYP3A4 is
 known to play a critical role in several clinically relevant herb-drug
 interactions. Midazolam has been reported to be one of the preferred
 in vivo CYP3A probes.
 center dot It has been reported that the lipophilic components of
 danshen could induce CYP3A in C57BL/6J mice, that cryptotanshinone and
 tanshinone IIA of danshen extract could activate human PXR and
 consequently induce the expression of the CYP3A4 gene.
 WHAT THIS STUDY ADDS
 center dot Co-administration of multiple doses of danshen tablets
 caused an increase in apparent oral clearance of midazolam by 35.4%,
 a corresponding decline in C-max by 31.1% and a decline in
 AUC(0,infinity) by 27.0% in human volunteers. The t(1/2) of midazolam
 and 1-hydroxymidazolam were not changed, and the C-max and
 AUC(0,infinity) ratio of midazolam to 1-hydroxymidazolam were not
 affected. The results suggested that multiple dose administration of
 danshen tablets could induce CYP3A4 in the gut, thereby increasing the
 clearance of midazolam. Therefore, caution should be taken when danshen
 products containing lipophilic components are used in combination with
 therapeutic drugs metabolized by CYP3A.
 AIMS
 To assess the effect of danshen extract on CYP3A4 activity using
 midazolam as an in vivo probe.
 METHODS
 A sequential, open-label, two-period pharmacokinetic interaction
 study design was used to compare midazolam pharmacokinetic parameters
 before and after 14 days of administration of danshen tablets. Twelve
 healthy volunteers received a single oral dose (15 mg) of midazolam
 followed by danshen tablets (four tablets orally, three times a day)
 for 14 days. On the last day of the study they received four danshen
 tablets with a 15 mg midazolam tablet and plasma concentrations of
 midazolam and its corresponding metabolite 1-hydroxylmidazolam were
 measured prior to and after the administration of danshen tablets
 periodically for 12 h.
 RESULTS
 The 90% confidence intervals of C(max,)t(1/2), CL/F and
 AUC(0,infinity) of midazolam before and after administration of
 danshen tablets were (0.559, 0.849), (0.908, 1.142), (1.086, 1.688)
 and (0.592, 0.921), respectively; and those of C-max, t(1/2) and
 AUC(0,infinity) of 1-hydroxylmidazolam after vs. before
 administration of danshen tablets were (0.633, 0.923), (0.801, 1.210)
 and (0.573, 0.980), respectively. Ratios of geometric LS means of
 C-max(1OHMid) : C-max(Mid) and AUC(max(1OHMid)) : AUC(max(Mid)) (after
 vs. before 14-day danshen) were 1.072 and 1.035, respectively.
 CONCLUSIONS
 Our findings suggest that multiple dose administration of danshen
 tablets may induce CYP3A4 in the gut. Accordingly, caution should be
 taken when danshen products are used in combination with therapeutic
 drugs metabolized by CYP3A.
 SN 0306-5251
 PD JUN
 PY 2010
 VL 69
 IS 6
 BP 656
 EP 662
 DI 10.1111/j.1365-2125.2010.03624.x
 UT ISI:000277522100011
 PT J
 AU Ling, Y
 Ye, XL
 Ji, H
 Zhang, YH
 Lai, YS
 Peng, SX
 Tian, JD
 AF Ling, Yong
 Ye, Xiaolei
 Ji, Hui
 Zhang, Yihua
 Lai, Yisheng
 Peng, Sixun
 Tian, Jide
 TI Synthesis and evaluation of nitric oxide-releasing derivatives of
 farnesylthiosalicylic acid as anti-tumor agents
 SO BIOORGANIC & MEDICINAL CHEMISTRY
 AB Novel furoxan-based nitric oxide (NO)-releasing derivatives (11a-p)
 of farnesylthiosalicylic acid (FTA) were synthesized. Compounds 11d,
 11f, 11k, and 11m-o displayed anti-tumor activities superior to FTA
 and sorafenib in most cancer cells tested. Analysis of six compounds
 revealed that 11d, 11f, 11n, 11o, and 11p, but not 11a that had low
 anti-tumor activity, produced high levels of NO, associated with their
 strong anti-tumor activity. Furthermore, the anti-tumor activity of
 11f was partially mimicked by the furoxan moiety, but reduced by
 pre-treatment with hemoglobin. Importantly, treatment with 11f
 inhibited Ras-related signaling in cancer cells. Apparently, the high
 anti-tumor activity of 11f was attributed to the synergic effect of
 high levels of NO production and inhibition of Ras-related signaling
 in cancer cells. Our findings suggest that the furoxan/FTA hybrids may
 hold greater promise as therapeutic agents for the intervention of
 human cancers. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0968-0896
 PD MAY 15
 PY 2010
 VL 18
 IS 10
 BP 3448
 EP 3456
 DI 10.1016/j.bmc.2010.03.077
 UT ISI:000277545900009
 PT J
 AU Liang, RM
 Cao, YB
 Zhou, YJ
 Xu, Y
 Gao, PH
 Dai, BD
 Yang, F
 Tang, H
 Jiang, YY
 AF Liang, Rong-mei
 Cao, Yong-bing
 Zhou, You-jun
 Xu, Yi
 Gao, Ping-hui
 Dai, Bao-di
 Yang, Feng
 Tang, Hui
 Jiang, Yuan-ying
 TI Transcriptional response of Candida albicans biofilms following
 exposure to 2-amino-nonyl-6-methoxyl-tetralin muriate
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To identify changes in the gene expression profile of Candida
 albicans (C albicans) biofilms following exposed to
 2-amino-nonyl-6-methoxyl-tetralin muriate(10b) and clarify the
 mechanism of 10b against C albicans biofilms.
 Methods: Anti-biofilm activity of 10b was assessed by tetrazolium (XTT)
 reduction assay and the action mechanism against biofilms was
 investigated by cDNA microarray analysis and real-time RT-PCR assay.
 Results: Ten differentially expressed genes were directly linked to
 biofilm formation and filamentous or hyphal growth (eg, NRG1, ECE1 and
 CSA1). Decreased gene expression was involved in glycolysis (eg, HXK2
 and PFK1) and antioxidant defense (eg, SOD5), while increased gene
 expression was associated with enzymes that specifically hydrolyzed
 beta-1,3 glucan (XOG1), and with lipid, fatty acid and sterol
 metabolism (eg, SLD1, ERG6 and ERG2). Functional analysis indicated
 that addition of anti-oxidant ascorbic acid reduced inhibitory
 efficiency of 10b on mature biofilm.
 Conclusion: Inhibition of 10b on biofilm formation possibly depends
 on impairing the ability of C albicans to change its morphology via
 altering the expression of biofilm formation genes. Mitochondrial
 aerobic respiration shift and endogenous ROS augmentation might be a
 major contribution to reduce mature biofilm metabolic activity. The
 data may be useful for the development of new strategies to reduce the
 incidence of device-associated infections.
 SN 1671-4083
 PD MAY
 PY 2010
 VL 31
 IS 5
 BP 616
 EP 628
 DI 10.1038/aps.2010.33
 UT ISI:000277661600013
 PT J
 AU Chang, BB
 Zhang, L
 Cao, WW
 Cao, Y
 Yang, WL
 Wang, Y
 Chen, YC
 Liu, XQ
 AF Chang, Bo-bo
 Zhang, Lin
 Cao, Wan-wen
 Cao, Yuan
 Yang, Wen-liang
 Wang, Yan
 Chen, Yuan-cheng
 Liu, Xiao-quan
 TI Pharmacokinetic interactions induced by content variation of major
 water-soluble components of Danshen preparation in rats
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To investigate the pharmacokinetic interactions induced by
 content variation of the main water-soluble components of Danshen
 injection in rats.
 Methods: Intravenous Danshen injection (control) or Danshen injection
 with danshensu (DSS), protocatechuic aldehyde (PAL), salvianolic acid
 A (Sal A) or salvianolic acid B (Sal B) were administered to female
 Sprague Dawley rats. Plasma concentrations of DSS, Sal A, PAL and its
 oxidative metabolite protocatechuic acid (PA) were analyzed
 simultaneously with LC-MS/MS; concentrations of Sal B were determined
 by the LC-MS method. Non-compartmental pharmacokinetic parameters were
 calculated and compared for identifying the pharmacokinetic
 interactions among these components.
 Results: Compared with the control group, the DSS, Sal A, and Sal B
 groups had significant increases in AUC(0-infinity) in response to
 elevated concentrations of PAL (by 78.1%, 51.0%, and 82.9%,
 respectively), while the clearances (CL) were markedly reduced (by
 42.5%, 32.9%, and 46.8%, respectively). Similarly, Sal A increased the
 AUC(0-infinity) of DSS and Sal B (26.7% and 82.4%, respectively) and
 substantially decreased their clearances (21.4% and 45.6%,
 respectively). In addition, the pharmacokinetics of DSS and Sal B were
 significantly affected by the content variation of the other major
 components; the AUC(0-infinity) increased by 45.1% and 52.1%,
 respectively, the CL dropped by 29.6% and 27.1%, respectively, and the
 T-1/2 was decreased by 22.0% and 19.6%, respectively.
 Conclusion: Complex, extensive pharmacokinetic interactions were
 observed among the major water-soluble constituents in the Danshen
 injection. The content variation of PAL had the most significant effect
 on the pharmacokinetic behaviors of other major constituents.
 Furthermore, the pharmacokinetics of DSS and Sal B were the most
 susceptible to the content change of other components.
 SN 1671-4083
 PD MAY
 PY 2010
 VL 31
 IS 5
 BP 638
 EP 646
 DI 10.1038/aps.2010.27
 UT ISI:000277661600015
 PT J
 AU Chu, WH
 Zhu, W
 AF Chu, W. -H.
 Zhu, W.
 TI Isolation of Bdellovibrio as Biological Therapeutic Agents Used For
 the Treatment of Aeromonas hydrophila Infection in Fish
 SO ZOONOSES AND PUBLIC HEALTH
 AB P>Fourteen strains of Bdellovibrio-like organisms were isolated from
 cultured fish ponds using Aeromonas hydrophila J-1 as host, one of them
 formed large plaques after 48 h of incubation at 28 degrees C on a double
 layer plate, designated as Bdellovibrio C-1. The Bdellovibrio was
 confirmed by electron microscopy and PCR amplification of
 Bdellovibrio-specific 16S rDNA. The optimum temperature for the growth
 of BdC-1 was between 15-37 degrees C and with optimal activity at
 temperatures of 25-30 degrees C. The ability of BdC-1 to lyse A.
 hydrophila was similar in the pH range of 6.5 to 8.5. It can lyse 23
 Gram-negative bacterial strains comprising three genera of fish
 pathogens and one strain of Escherichia coli but cannot lyse
 Gram-positive bacteria such as Bacillus subtillis and Staphylococcus
 aureus. Immersion of fish in water containing different concentrations
 of BdC-1 was used in protection against an experimental infection of
 A. hydrophila J-1. Results show that the mortality of groups immersed
 with BdC-1 was lower than the group without BdC-1. These results suggest
 that it may be possible to use Bdellovibrio to control the disease
 caused by A. hydrophila.
 SN 1863-1959
 PD JUN
 PY 2010
 VL 57
 IS 4
 BP 258
 EP 264
 DI 10.1111/j.1863-2378.2008.01224.x
 UT ISI:000277416200005
 PT J
 AU Qi, SH
 Liu, Y
 Hao, LY
 Guan, QH
 Gu, YH
 Zhang, J
 Yan, H
 Wang, M
 Zhang, GY
 AF Qi, S. -H.
 Liu, Y.
 Hao, L. -Y.
 Guan, Q. -H.
 Gu, Y. -H.
 Zhang, J.
 Yan, H.
 Wang, M.
 Zhang, G. -Y.
 TI NEUROPROTECTION OF ETHANOL AGAINST ISCHEMIA/REPERFUSION-INDUCED BRAIN
 INJURY THROUGH DECREASING c-Jun N-TERMINAL KINASE 3 (JNK3) ACTIVATION
 BY ENHANCING GABA RELEASE
 SO NEUROSCIENCE
 AB Our latest study indicated that ethanol could attenuate cerebral
 ischemia/reperfusion-induced brain injury through activating
 Ionotropic glutamate receptors Kainate Family (Gluk1)-kainate (KA)
 receptors and gamma-aminobutyric acid (GABA) receptors. However, the
 possible mechanism of the neuroprotective effects of ethanol remains
 unclear. In this study we report that ethanol shows neuroprotective
 effects against ischemic brain injury through enhancing GABA release
 and then decreasing c-Jun N-terminal kinase 3 (JNK3) activation.
 Electrophysiologic recording indicated that ethanol enhances GABA
 release from presynaptic neurons and the released GABA subsequently
 inhibits the KA receptor mediated whole-cell currents. Moreover, our
 data show that ethanol can inhibit the increased assembly of the
 Gluk2-PSD-95-MLK3 (postsynaptic density protein-95, PSD-95 and
 mixed-lineage kinase 3, MLK3) module induced by cerebral ischemia and
 the activation of the MLK3-MKK4/7-JNK (mitogen-activated protein
 kinase kinase 4/7, MKK4/7) cascade. Pretreatment of the GABA(A)
 receptor antagonist bicuculline and antagonist of VGCC (a
 broad-spectrum blocker of the voltage-gated calcium channel [VGCC])
 Chromic (CdCl2) can demolish the neuroprotective effects of ethanol.
 The results suggest that during ischemia-reperfusion, ethanol may
 activate presynaptic Gluk1-KA and facilitate Ca2+-dependent GABA
 release. The released GABA activates postsynaptic GABAA receptors,
 which suppress the ischemic depolarization and decrease the
 association of signaling module Gluk2-PSD-95-MLK3 induced by the
 activation of postsynaptic Gluk2-KA receptors. There is a raised
 possibility that ethanol inhibiting the JNK3 apoptotic pathway
 (MLK3/MKK4/7/JNK3/c-Jun/Fas-L) performs a neuroprotective function
 against ischemic brain injury. (C) 2010 IBRO. Published by Elsevier
 Ltd. All rights reserved.
 SN 0306-4522
 PD JUN 2
 PY 2010
 VL 167
 IS 4
 BP 1125
 EP 1137
 DI 10.1016/j.neuroscience.2010.02.018
 UT ISI:000277434800016
 PT J
 AU Shao, H
 Ren, XM
 Liu, NF
 Chen, GM
 Li, WL
 Zhai, ZH
 Wang, DW
 AF Shao, H.
 Ren, X. M.
 Liu, N. F.
 Chen, G. M.
 Li, W. L.
 Zhai, Z. H.
 Wang, D. W.
 TI Influence of CYP2C9 and CYP2C19 genetic polymorphisms on
 pharmacokinetics and pharmacodynamics of gliclazide in healthy Chinese
 Han volunteers
 SO JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS
 AB P>Background and objective:
 CYP2C9 is the major contributor to gliclazide metabolic clearance in
 vitro, while the pharmacokinetics of gliclazide modified release are
 affected mainly by CYP2C19 genetic polymorphisms in vivo. This study
 aims to investigate the influence of CYP2C9 and CYP2C19 genetic
 polymorphisms on the pharmacokinetics and pharmacodynamics of
 gliclazide in healthy Chinese Han volunteers.
 Methods:
 Eighteen healthy Han subjects with various combinations of CYP2C9 and
 CYP2C19 genotypes received 80 mg gliclazide. Plasma gliclazide
 concentrations were measured by a liquid chromatography-tandem mass
 spectrometry method for 84 h and plasma glucose and insulin levels were
 measured up to 15 h post-dose.
 Results and discussion:
 There was no difference in either pharmacokinetic and or
 pharmacodynamic parameters of gliclazide when group A (CYP2C9*1/*1,
 CYP2C19 extensive metabolizers) was compared with group B
 (CYP2C9*1/*3, CYP2C19 *1/*1). When group C (CYP2C9*1/*1 and CYP2C19
 poor metabolizers) was compared with group A, the AUC(0-infinity) and
 C-max in group C were significantly higher [83 center dot 94 +/- 40
 center dot 41 vs. 16 center dot 39 +/- 5 center dot 10 mu g center dot
 h/mL (P = 0 center dot 000) and 1 center dot 50 +/- 0 center dot 85
 vs. 0 center dot 45 +/- 0 center dot 18 mu g/mL (P = 0 center dot 000)],
 and the oral clearance was significantly lower [1 center dot 17 +/0 center dot 63 vs. 5 center dot 38 +/- 1 center dot 86 L/h (P = 0 center
 dot 000)]. The half-life of gliclazide was also significantly prolonged
 in group C subjects when compared with that of group A (33 center dot
 47 +/- 12 center dot 39 vs. 19 center dot 34 +/- 10 center dot 45 h),
 but the difference was not significant (P = 0 center dot 052). The
 increase in serum glucose level at 11 h after dosing (Delta C-glu11)
 in group C was significantly higher than that of group A (-1 center
 dot 08 +/- 0 center dot 42 vs. 0 center dot 22 +/- 1 center dot 01 mmol/L,
 P = 0 center dot 022). The corresponding insulin levels showed no
 difference between the two groups.
 Conclusion:
 CYP2C9*3 was not associated with any change in the disposition of
 gliclazide. CYP2C19 polymorphisms appear to exert the dominant
 influence on the pharmacokinetics of gliclazide in healthy Chinese Han
 subjects, and may also affect the observed pharmacodynamics of the drug
 as a result.
 SN 0269-4727
 PD JUN
 PY 2010
 VL 35
 IS 3
 BP 351
 EP 360
 DI 10.1111/j.1365-2710.2009.01134.x
 UT ISI:000277413000011
 PT J
 AU Wei, MC
 Wang, SZ
 He, YM
 Fang, YL
 Chen, YJ
 AF Wei, Maochen
 Wang, Suzhen
 He, Yunmian
 Fang, Yongliang
 Chen, Yijun
 TI Separation of structurally similar nocathiacin analogues by reversed
 phase chromatography
 SO JOURNAL OF CHROMATOGRAPHY A
 AB The complete separation of structurally similar compounds has been a
 challenge due mainly to their similarity on physical and chemical
 properties. In the present study, a simple and effective
 chromatographic method to separate and purify nocathiacin acid from
 its structural analogue nocathiacin I was developed. After evaluating
 mobile phase compositions on the retention characteristics by reversed
 phase high-performance liquid chromatography (HPLC), the elution order
 of nocathiacin land nocathiacin acid was completely reversed, and the
 resolution value between the two analogues was improved, by varying
 pH value and ionic strength, to greater than 10 from merged peaks under
 initial conditions. In addition, a preparative isolation of
 nocathiacin acid was performed by reversed phase column chromatography
 under the guidance of the HPLC study. This chromatographic method
 resulted in an efficient process to obtain pure nocathiacin acid with
 a recovery rate of 83%. The present approach offers a new methodology
 for the separation of structurally closely related secondary
 metabolites. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0021-9673
 PD APR 30
 PY 2010
 VL 1217
 IS 18
 BP 3038
 EP 3043
 DI 10.1016/j.chroma.2010.02.079
 UT ISI:000277373800005
 PT J
 AU Ni, B
 Zhang, JR
 Zou, JJ
 Zhao, W
 Li, JH
 AF Ni, Bin
 Zhang, Junren
 Zou, JianJun
 Zhao, Wei
 Li, JianHua
 TI A Simple and Sensitive HPLC Method For Quantification of the Metabolin
 of Meclofenoxate In Human Plasma
 SO JOURNAL OF CHROMATOGRAPHIC SCIENCE
 SN 0021-9665
 PD MAY-JUN
 PY 2010
 VL 48
 IS 5
 BP 353
 EP 357
 UT ISI:000277431900006
 PT J
 AU Zhao, LH
 Xiang, BR
 Tan, XY
 AF Zhao, Luhua
 Xiang, Bingren
 Tan, Xiying
 TI Fingerprinting of Marsdenia tenacissima by Capillary Electrophoresis
 Compared to HPLC
 SO JOURNAL OF CHROMATOGRAPHIC SCIENCE
 SN 0021-9665
 PD MAY-JUN
 PY 2010
 VL 48
 IS 5
 BP 417
 EP 420
 UT ISI:000277431900018
 PT J
 AU Yang, J
 Chen, H
 Zhang, L
 Wang, Q
 Lai, MX
 AF Yang, Jie
 Chen, Hong
 Zhang, Li
 Wang, Qiang
 Lai, Mao-Xiang
 TI Anti-Diabetic Effect of Standardized Extract of Potentilla discolor
 Bunge and Identification of its Active Components
 SO DRUG DEVELOPMENT RESEARCH
 AB Potentilla discolor Bunge, a Chinese folk medicine, has been used for
 the treatment of diabetes for many years. Unfortunately, little
 information is available on its bioactive components and mechanism of
 action. We report the anti-diabetic effect of P. discolor on normal
 and alloxan-induced diabetic mice, as well as the possible constituents
 and mechanism responsible for this activity. We found that the
 standardized extract of P. discolor (EPD) had little effect on the
 glucose levels of normal mice, while a dose-dependent hypoglycemic
 effect was observed in diabetic mice. Glucose tolerance test data
 indicated that there was a significantly higher rate of glucose
 disposal after EPD treatment. Phytochemical characterization
 indicated that the major components of EPD were triterpenes and
 flavonoids that could inhibit the activity of glycogen phosphorylase
 (GP) in vitro. Tormentic acid, asiatic acid, and potengriffioside A
 exhibited inhibitory effects on GP (IC50 = 90.6, 65.4, and 85.9 mu M,
 respectively). The inhibition on GP may be one molecular mechanism
 through which EPD ameliorates hyperglycemia. These results suggest P.
 discolor extract may offer an alternate treatment for diabetes. Drug
 Dev Res 71:127-132, 2010. (C) 2009 Wiley-Liss, Inc.
 SN 0272-4391
 PD APR
 PY 2010
 VL 71
 IS 2
 BP 127
 EP 132
 DI 10.1002/ddr.20340
 UT ISI:000277327600005
 PT J
 AU Guo, DL
 Liu, GN
 Zhou, Y
 Li, J
 Xu, JY
 Jiang, HL
 Chen, KX
 Liu, H
 AF Guo Diliang
 Liu Guannan
 Zhou Yu
 Li Jian
 Xu Jinyi
 Jiang Hualiang
 Chen Kaixian
 Liu Hong
 TI Research Progress in HIV Integrase Inhibitors
 SO CHINESE JOURNAL OF ORGANIC CHEMISTRY
 AB HIV integrase is one of the three essential enzymes for viral DNA
 replication and the molecular target of the newly approved anti-AIDS
 drug raltegravir (MK-0518, Isentress). HIV integrase inhibitors have
 emerged as a new class of drugs for the treatment of AIDS. In this
 article, the recent progress of HIV integrase inhibitors is reviewed
 to provide some useful information for the further research and
 development of HIV integrase inhibitors.
 SN 0253-2786
 PD APR
 PY 2010
 VL 30
 IS 4
 BP 477
 EP 485
 UT ISI:000277485200001
 PT J
 AU Zhu, SH
 Zou, BJ
 Wu, HP
 Ma, YJ
 Chen, Y
 Zhou, GH
 AF Zhu Shu-Hui
 Zou Bing-Jie
 Wu Hai-Ping
 Ma Yin-Jiao
 Chen Ying
 Zhou Guo-Hua
 TI Preparation of Thermostable Biotinlyted Firefly Luciferase and Its
 Application to Pyrosequencing
 SO CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
 AB The next generation pyrosequencing system requires stable and
 immobilized luciferase. In order to get stable and immobilized
 luciferase(LUC) for the large-scale pyrosequeneing platform, the genes
 coding the Photinus pyralis firefly luciferase and 87 C-terminal
 residues of biotin carboxyl carrier protein(BCCP87) were inserted into
 plasmid to express biotinylated fussion protein in E. coli BL21 (DE3),
 and the gene of luciferase was mutated to get thermostable biotinylated
 luciferase. The fusion protein was immobilized on streptavidin-coated
 Beads and applied to pyrosequencing. The results of activity detection
 showed that mutant luciferase had a good tolerance to heat, and still
 showed activities at 50 degrees C. The mutant LUG remains 80% activities
 after incubated at 43 degrees C for 10 min. Western blot analysis
 indicated that the fusion protein was successfully biotinylated in E.
 coli. The biotinylated luciferase immobilized on magnetic beads coated
 with streptavidin showed catalytic activity of 2.1 X 10(5) RLU/mu L
 beads and the activity remained nearly constant even if bead-LUC
 suffered from multiple washing processes. The DNA was accurately and
 quantitatively sequenced by using luciferase and adenosine
 triphosphate (ATP) sulfurylase co-immobilized on magnetic beads. This
 study provides an efficient and thermostable enzyme for the large-scale
 chip-based pyrosequencing system.
 SN 0253-3820
 PD APR
 PY 2010
 VL 38
 IS 4
 BP 458
 EP 463
 DI 10.3724/SP.J.1096.2010.00458
 UT ISI:000277393500002
 PT J
 AU Chen, GH
 Wang, S
 Wu, FH
 AF Chen, Guo Hua
 Wang, Sheng
 Wu, Fei Hua
 TI A practical synthesis of sarpogrelate hydrochloride and in vitro
 platelet aggregation inhibitory activities of its analogues
 SO CHINESE CHEMICAL LETTERS
 AB A convenient approach for the preparation of sarpogrelate
 hydrochloride was developed. Two series of sarpogrelate hydrochloride
 analogues were designed and synthesized in order to improve their
 platelet aggregation inhibitory activities, biological tests
 suggested that these compounds have platelet aggregation inhibitory
 activities to some extent. (C) 2009 Guo Hua Chen. Published by Elsevier
 B.V. on behalf of Chinese Chemical Society. All rights reserved.
 SN 1001-8417
 PD MAR
 PY 2010
 VL 21
 IS 3
 BP 287
 EP 289
 DI 10.1016/j.cclet.2009.11.030
 UT ISI:000277378700010
 PT J
 AU Wang, ZH
 Dong, Y
 Wang, T
 Shang, MH
 Hua, WY
 Yao, QZ
 AF Wang, Zhao Hui
 Dong, Ying
 Wang, Tao
 Shang, Ming Hong
 Hua, Wei Yi
 Yao, Qi Zheng
 TI Synthesis and CDK2 kinase inhibitory activity of 7/7 '-azaindirubin
 derivatives
 SO CHINESE CHEMICAL LETTERS
 AB A series of novel 7'-azaindirubin (1a-g) and 7-azaindirubin (2a, 2c,
 2e and 2f) derivatives were designed and synthesized. Their structures
 were characterized by H-1 NMR and MS spectroscopy as well as by
 elemental analysis. Their inhibitory properties against CDK2/cylinA
 were evaluated in vitro. In contrast to indirubin, some of the described
 azaindirubins emerged as potent inhibitors of CDK2/cylinA and compound
 2b had more potent activity. Biological tests also showed that nitrogen
 atom at 7-position of azaindirubin was more beneficial to enhance the
 kinase inhibitory activity. (C) 2009 Qi Zheng Yao. Published by
 Elsevier B.V. on behalf of Chinese Chemical Society. All rights
 reserved.
 SN 1001-8417
 PD MAR
 PY 2010
 VL 21
 IS 3
 BP 297
 EP 300
 DI 10.1016/j.cclet.2009.11.029
 UT ISI:000277378700013
 PT J
 AU Li, ZL
 Qian, SH
 Pu, SB
 AF Li, Zhen Lin
 Qian, Shi Hui
 Pu, She Ban
 TI Two new taraxastane-type triterpenoids from the fruit of Cicuta virosa
 L. var latisecta Celak
 SO CHINESE CHEMICAL LETTERS
 AB Two new taraxastane-type triterpenoids, 20-taraxastene-3 beta,12
 beta,16 beta-triol 1 and 3 beta-feruloyloxy-20-taraxastene-16
 beta,28-diol 2, were isolated from the fruit of Cicuta virosa L. var
 latisecta Celak. There structures were elucidated by ESI-MS, 1D- and
 2D-NMR spectroscopic methods. (C) 2009 Shi Hui Qian. Published by
 Elsevier B.V. on behalf of Chinese Chemical Society. All rights
 reserved.
 SN 1001-8417
 PD MAR
 PY 2010
 VL 21
 IS 3
 BP 317
 EP 321
 DI 10.1016/j.cclet.2009.11.001
 UT ISI:000277378700018
 PT J
 AU Fu, MJ
 Zhuang, JJ
 Hou, FZ
 Zhan, QB
 Shao, Y
 Ning, XB
 AF Fu Mao-Jing
 Zhuang Jian-Jun
 Hou Feng-Zhen
 Zhan Qing-Bo
 Shao Yi
 Ning Xin-Bao
 TI A method for extracting human gait series from accelerometer signals
 based on the ensemble empirical mode decomposition
 SO CHINESE PHYSICS B
 AB In this paper, the ensemble empirical mode decomposition (EEMD) is
 applied to analyse accelerometer signals collected during normal human
 walking. First, the self-adaptive feature of EEMD is utilised to
 decompose the accelerometer signals, thus sifting out several
 intrinsic mode functions (IMFs) at disparate scales. Then, gait series
 can be extracted through peak detection from the eigen IMF that best
 represents gait rhythmicity. Compared with the method based on the
 empirical mode decomposition (EMD), the EEMD-based method has the
 following advantages: it remarkably improves the detection rate of peak
 values hidden in the original accelerometer signal, even when the
 signal is severely contaminated by the intermittent noises; this method
 effectively prevents the phenomenon of mode mixing found in the process
 of EMD. And a reasonable selection of parameters for the stop-filtering
 criteria can improve the calculation speed of the EEMD-based method.
 Meanwhile, the endpoint effect can be suppressed by using the auto
 regressive and moving average model to extend a short-time series in
 dual directions. The results suggest that EEMD is a powerful tool for
 extraction of gait rhythmicity and it also provides valuable clues for
 extracting eigen rhythm of other physiological signals.
 SN 1674-1056
 PD MAY
 PY 2010
 VL 19
 IS 5
 AR 058701
 DI 10.1088/1674-1056/19/5/058701
 UT ISI:000277372200088
 PT J
 AU Li, K
 Ding, L
 Yang, ZL
 Liu, EH
 Qi, LW
 Li, P
 Hu, YZ
 AF Li, Kai
 Ding, Li
 Yang, Zhong-Lin
 Liu, E-Hu
 Qi, Lian-Wen
 Li, Ping
 Hu, Yu-Zhu
 TI Determination of asperosaponin VI in rat plasma by HPLC-ESI-MS and its
 application to preliminary pharmacokinetic studies
 SO BIOMEDICAL CHROMATOGRAPHY
 AB Asperosaponin VI (also named akebia saponin D) is a typical bioactive
 triterpenoid saponin isolated from the rhizome of Dipsacus asper Wall
 (Dipsacaceae). In this work, a sensitive high-performance liquid
 chromatography-electrospray ionization-mass spectrometry
 (HPLC-ESI-MS) assay has been established for determination of
 asperosaponin VI in rat plasma. With losartan as the internal standard
 (IS), plasma samples were prepared by protein precipitation with
 methanol. Chromatographic separation was performed on a C-18 column
 with a mobile phase of 10 mm ammonium acetate buffer containing 0.05%
 formic acid-methanol (32:68, v/v). The analysis was performed on an
 ESI in the selected ion monitoring mode using target ions at m/z 951.4
 for asperosaponin VI and miz 423.2 for the IS. The calibration curve
 was linear over the range 3-1000 ng/mL and the lower limit of
 quantification was 3.0 ng/mL. The intra- and inter-assay variability
 values were less than 9.5 and 7.8%, respectively. The accuracies
 determined at the concentrations of 3.0, 100.0, 300.0 and 1000 ng/mL
 for asperosaponin VI were within 15.0%. The validated method was
 successfully applied to a pharmacokinetic study in rats after oral
 administration of asperosaponin VI. Copyright (C) 2009 John Wiley &
 Sons, Ltd.
 SN 0269-3879
 PD MAY
 PY 2010
 VL 24
 IS 5
 BP 550
 EP 555
 DI 10.1002/bmc.1325
 UT ISI:000277335200014
 PT J
 AU Wu, GQ
 Wu, HB
 Li, LX
 Fan, XB
 Ding, JX
 Li, XF
 Xi, T
 Shen, ZL
 AF Wu, Guoqiu
 Wu, Hongbin
 Li, Linxian
 Fan, Xiaobo
 Ding, Jiaxuan
 Li, Xiaofang
 Xi, Tao
 Shen, Zilong
 TI Membrane aggregation and perturbation induced by antimicrobial peptide
 of S-thanatin
 SO BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
 AB Thanatin, a 21-residue peptide, is an inducible insect peptide. In our
 previous study, we have identified a novel thanatin analog of
 S-thanatin, which exhibited a broad antimicrobial activity against
 bacteria and fungi with low hemolytic activity. This study was aimed
 to delineate the antimicrobial mechanism of S-thanatin and identify
 its interaction with bacterial membranes. In this study, membrane
 phospholipid was found to be the target for S-thanatin. In the presence
 of vesicles, S-thanatin interestingly led to the aggregation of anionic
 vesicles and sonicated bacteria. Adding S-thanatin to Escherichia coli
 suspension would result in the collapse of membrane and kill bacteria.
 The sensitivity assay of protoplast elucidated the importance of outer
 membrane (OM) for S-thanatin's antimicrobial activity. Compared with
 other antimicrobial peptide, S-thanatin produced chaotic membrane
 morphology and cell debris in electron microscopic appearance. These
 results supported our hypothesis that S-thanatin bound to negatively
 charged LPS and anionic lipid, impeded membrane respiration, exhausted
 the intracellular potential, and released periplasmic material, which
 led to cell death. (C) 2010 Elsevier Inc. All rights reserved.
 SN 0006-291X
 PD APR 23
 PY 2010
 VL 395
 IS 1
 BP 31
 EP 35
 DI 10.1016/j.bbrc.2010.03.107
 UT ISI:000277298000006
 PT J
 AU Liu, R
 Wang, M
 Duan, JA
 AF Liu, Rui
 Wang, Min
 Duan, Jin-Ao
 TI Antipyretic and Antioxidant Activities of the Aqueous Extract of Cornu
 Bubali (Water Buffalo Horn)
 SO AMERICAN JOURNAL OF CHINESE MEDICINE
 AB Cornu Bubali (water buffalo horn, WBH) is an animal-derived product
 which is widely used in Traditional Chinese Medicine (TCM) for
 dispelling heat, relieving convulsions and cooling blood. The purpose
 of this study was to investigate the antipyretic activity of WBH aqueous
 extract and its potential mechanism. Two hyperthermia models,
 yeast-induced (infectious) and skimmed milk-induced (noninfectious)
 hyperthermia were employed to evaluate the antipyretic effect and the
 results showed that rectal temperature of hyperthermia animals was
 decreased significantly after oral administration of WBH extract. The
 production of tumor necrosis factor-alpha (TNF-alpha)-induced
 prostaglandin E-2 (PGE(2)) in rat cerebral microvascular endothelial
 cells (rCMECs) was inhibited by WBH extract in the concentrations of
 10 mu g/ml and 100 mu g/ml. The WBH extract protected rCMECs survival
 from hydrogen peroxide (H2O2)-induced toxicity and inhibited the
 H2O2-induced leakage of lactate dehydrogenase (LDH) enzyme release at
 a dose ranging from 5 mu g/ml to 100 mu g/ml. It could also increase
 the superoxide dismutase (SOD) and catalase (CAT) enzyme activities.
 The results suggest that Cornu Bubali exhibits antipyretic activity
 on both infectious and noninfectious hyperthermia. The antipyretic
 activity of WBH may be due to the effects on enhancing antioxidation
 enzyme activities, decreasing PGE(2) production, and protecting the
 rCMECs against H2O2-induced injury.
 SN 0192-415X
 PY 2010
 VL 38
 IS 2
 BP 293
 EP 306
 DI 10.1142/S0192415X10007853
 UT ISI:000277510100007
 PT J
 AU Liu, L
 Yu, YL
 Yang, JS
 Li, Y
 Liu, YW
 Liang, Y
 Liu, XD
 Xie, L
 Wang, GJ
 AF Liu, Li
 Yu, Yun-Li
 Yang, Jian-Song
 Li, Yang
 Liu, Yao-Wu
 Liang, Yan
 Liu, Xiao-Dong
 Xie, Lin
 Wang, Guang-Ji
 TI Berberine suppresses intestinal disaccharidases with beneficial
 metabolic effects in diabetic states, evidences from in vivo and in
 vitro study
 SO NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
 AB Clinical reports have demonstrated that berberine is a potential
 antidiabetic agent, but the underlying mechanism is unclear. The
 purpose of this study was to investigate if berberine exerts its
 hypoglycemic action via inhibiting intestinal disaccharidases using
 in vivo and in vitro experiments. Streptozotocin-induced diabetic rats
 received berberine (100 or 200 mg/kg) orally once daily or acarbose
 (40 mg/kg) orally twice daily for 5 weeks. Disaccharidase activities
 and sucrase-isomaltase (SI) complex messenger RNA (mRNA) expression
 in intestinal regions were assessed. The same treatment was operated
 in normal rats. Sucrose and maltose loading tests were also documented.
 In addition, Caco-2 cells were cultured in medium containing berberine
 or berberine plus chelerythrine. Compound C or H-89 for 5 days,
 disaccharidase activities, and SI complex mRNA levels were measured.
 The animal experiments showed that berberine significantly decreased
 the disaccharidase activities and SI complex mRNA expression both in
 diabetic rats and normal rats. Berberine can also significantly lower
 postprandial blood glucose levels induced by sucrose or maltose loading
 in normal rats. The cellular results showed that berberine may suppress
 disaccharidase activities and downregulate SI complex mRNA expression
 in a concentration-dependent manner. Only H-89, an inhibitor of protein
 kinase A (PKA), may reverse the decrease in disaccharidase activities
 and SI complex mRNA expression induced by berberine. In conclusion,
 berberine suppresses disaccharidase activities and SI complex mRNA
 expression with beneficial metabolic effects in diabetic states. The
 inhibitory effect, at least partly, involves the PKA-dependent
 pathway.
 SN 0028-1298
 PD APR
 PY 2010
 VL 381
 IS 4
 BP 371
 EP 381
 DI 10.1007/s00210-010-0502-0
 UT ISI:000277181700010
 PT J
 AU Lu, XY
 You, QD
 Chen, YD
 AF Lu, X. Y.
 You, Q. D.
 Chen, Y. D.
 TI Recent Progress in the Identification and Development of InhA Direct
 Inhibitors of Mycobacterium tuberculosis
 SO MINI-REVIEWS IN MEDICINAL CHEMISTRY
 AB The InhA-related enoyl-ACP reductase, an enzyme involved in fatty acid
 synthesis, is one of the best validated targets for the development
 of anti-tubercular agents. However, the majority of isoniazid
 (INH)-resistant clinical strains are observed mainly due to the
 emergence of KatG mutants that do not form an INH-NAD adduct. Thus
 compounds that directly inhibit InhA avoiding activation by KatG would
 be promising candidates for combating MDR-TB. Herein, some predominant
 examples of InhA direct inhibitors recently developed are reviewed and
 special attention is paid to 3D-structures of InhA in drug design
 process.
 SN 1389-5575
 PD MAR
 PY 2010
 VL 10
 IS 3
 BP 182
 EP 193
 UT ISI:000277156300001
 PT J
 AU Xie, SS
 Hu, N
 Jing, XY
 Liu, XD
 Xie, L
 Wang, GJ
 Liu, CH
 AF Xie, Shan-Shan
 Hu, Nan
 Jing, Xin-Yue
 Liu, Xiao-Dong
 Xie, Lin
 Wang, Guang-Ji
 Liu, Chang-Hui
 TI Effect of Huang-Lian-Jie-Du-Decoction on pharmacokinetics of
 verapamil in rats
 SO JOURNAL OF PHARMACY AND PHARMACOLOGY
 AB Objectives The aim was to investigate the effect of
 Huang-Lian-Jie-Du-Decoction (HLJDD) on the pharmacokinetic behaviour
 of verapamil in rats.
 Methods Rats orally received 3.33 g/kg of HLJDD extract for 14 days,
 and pharmacokinetics of verapamil was investigated after oral and
 intravenous verapamil. Norverapamil formation for assessing
 cytochrome P450 3A activity in hepatic and intestinal microsomes of
 the HLJDD-treated rats was investigated. The inhibitory effect of
 berberine on the formation of norverapamil in intestinal and hepatic
 microsomes was also evaluated.
 Key findings HLJDD treatment increased the plasma concentration of
 verapamil and decreased the plasma concentration of norverapamil,
 resulting in a 24% increase in the AUC(0-480) of verapamil and a 25%
 reduction in the AUC(0-480) of norverapamil after oral administration.
 However, HLJDD did not alter the pharmacokinetic behaviour of verapamil
 after intravenous administration. Norverapamil formation showed
 biphasic kinetics in both intestinal and hepatic microsomes. HLJDD
 treatment significantly decreased the intrinsic clearance of verapamil
 in intestinal microsomes, but had no effect on the hepatic metabolism
 of verapamil. Berberine also inhibited norverapamil formation in both
 intestinal and hepatic microsomes; the extent of inhibition was larger
 in intestinal microsomes.
 Conclusions HLJDD displayed a route-dependent effect on the
 pharmacokinetics of verapamil in rats. HLJDD treatment increased the
 bioavailability of verapamil partly via inhibiting first-pass
 verapamil metabolism in the intestine.
 SN 0022-3573
 PD APR
 PY 2010
 VL 62
 IS 4
 BP 440
 EP 447
 DI 10.1211/jpp/62.04.0005
 UT ISI:000277102200005
 PT J
 AU Wang, H
 Qi, J
 Xu, T
 Liu, JH
 Qin, MJ
 Zhu, DN
 Yu, BY
 AF Wang, Hui
 Qi, Jin
 Xu, Tian
 Liu, Ji-Hua
 Qin, Min-Jian
 Zhu, Dan-Ni
 Yu, Bo-Yang
 TI Effects of Storage Condition Factors on Fungal Invasion of Radix
 Ophiopogonis
 SO JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
 AB Fungal invasion is a main factor leading to the loss of postharvest
 herbs during storage. To prevent fungal invasion and clarify the
 favorable conditions for the stability of herbs during the storage
 period, uniform design and three-dimensional response surfaces were
 applied to investigate the relationship of the mildew degree of Radix
 Ophiopogonis induced by prevalent fungal isolates and the storage
 factors including air relative humidity (X-1), temperature (X-2), and
 moisture content (X-3), in laboratory studies. Mildew degree was
 evaluated by ergosterol assay of mold isolates through a
 high-performance liquid chromatography diode array detector
 (HPLC-DAD) technique. As a result, storage conditions, which satisfied
 the following correlation equations established by the relationships
 between the storage factors and the biomass of mildew (Y), could
 effectively prevent fungal spoilage: Y = -0.2484084028 +
 0.00030711966572 x X-3 x X-3 + 0.00018881361186 x X-1 x X-2 0.00029473040679 x X-2 x X-3 <= 0; Y=-0.2697457586 + 0.004127756022
 x X-1 - 0.000015977780492 x X-1 x X-1 + 0.00021906984606 x X-2 x X-3
 <= 0; Y = -0.325655811 + 0.015464432582 x X-2 + 0.00004779394354 x X-1
 x X-1 - 0.00021743815482 x X-2 x X-2 <= 0. This compositive methodology
 might be useful to predict the occurrence of fungal invasion.
 SN 0021-8561
 PD MAY 12
 PY 2010
 VL 58
 IS 9
 BP 5432
 EP 5437
 DI 10.1021/jf9044588
 UT ISI:000277237500033
 PT J
 AU Xu, XX
 Gao, XH
 Pan, R
 Lu, D
 Dai, Y
 AF Xu, Xian-xiang
 Gao, Xing-hua
 Pan, Rong
 Lu, Dan
 Dai, Yue
 TI A simple adhesion assay for studying interactions between platelets
 and endothelial cells in vitro
 SO CYTOTECHNOLOGY
 AB Cell adhesion plays a key role during various physiological and
 pathological processes. Many studies have been performed to understand
 the interaction of platelets with endothelial cells (ECs) during the
 past decades. Modulation of their interaction has been shown to be
 therapeutically useful in thrombotic diseases. Some methods of
 labeling platelets such as counting and radiolabeling have been applied
 in the study of the platelets-ECs interaction, but these methods did
 not obtain full approval. A rapid, simple and sensitive assay for
 platelets-ECs interaction was developed in this paper. Platelets were
 labeled with Sudan Black B (SBB) before adding to confluent ECs
 monolayer. Non-adherent platelets were removed by washing with PBS.
 The adherent platelets were lysed with dimethylsulfoxide (DMSO) and
 the absorbance was recorded at 595 nm by spectrophotometer. A linear
 correlation was observed between the absorbance of SBB and the number
 of platelets. By employing the SBB method, the influence of heparin
 on platelets-ECs interactions was observed. Heparin (3-100 units/mL)
 obviously reduced platelets adhering to ECs in a
 concentration-dependent manner.
 SN 0920-9069
 PD JAN
 PY 2010
 VL 62
 IS 1
 BP 17
 EP 22
 DI 10.1007/s10616-010-9256-2
 UT ISI:000277137600002
 PT J
 AU Li, HF
 Chen, YD
 Rao, SS
 Chen, XM
 Liu, HC
 Qin, JH
 Tang, WF
 Yue-Wang
 Zhou, X
 Lu, T
 AF Li, Hui-Fang
 Chen, Yadong
 Rao, Sha-Sha
 Chen, Xiu-Mei
 Liu, Hai-Chun
 Qin, Ji-Hong
 Tang, Wei-Fang
 Yue-Wang
 Zhou, Xiang
 Lu, Tao
 TI Recent Advances in the Research and Development of B-Raf Inhibitors
 SO CURRENT MEDICINAL CHEMISTRY
 AB Oncogenic B-Raf has been identified in a variety of cancers with high
 incidence, especially in malignant melanoma and thyroid cancer. Most
 B-Raf mutations elicit elevated kinase activity and the constitutive
 activation of Ras/Raf/MEK/ERK pathway, which induces proliferation and
 promotes malignant transformation. Therefore, B-Raf inhibitors,
 targeting B-Raf or mutated B-Raf, have received increasing momentum
 in oncology drug discovery arena. This review focuses on the diverse
 small-molecule inhibitors of B-Raf kinase recently reported in the
 literature, including those currently in clinical and preclinical
 phase. They are described as two categories, type I or type II kinase
 inhibitors, based on their different mechanism of action with active
 or inactive conformations of the B-Raf kinase derived from the
 available crystal structures or molecular docking analysis. A
 particular emphasis is placed on their binding modes and the
 structure-activity relationship (SAR) of each chemical structure
 class.
 SN 0929-8673
 PD JUN
 PY 2010
 VL 17
 IS 16
 BP 1618
 EP 1634
 UT ISI:000277120200001
 PT J
 AU Wong, I
 Liao, H
 Bai, XS
 Zaknic, A
 Zhong, JH
 Guan, Y
 Li, HY
 Wang, YJ
 Zhou, XF
 AF Wong, Ira
 Liao, Hong
 Bai, Xianshu
 Zaknic, Antony
 Zhong, Jinhua
 Guan, Yue
 Li, Hong-Yun
 Wang, Yan-Jiang
 Zhou, Xin-Fu
 TI ProBDNF inhibits infiltration of ED1+macrophages after spinal cord
 injury
 SO BRAIN BEHAVIOR AND IMMUNITY
 AB The central nervous system (CNS) does not regenerate partly clue to
 the slow clearance of debris from the degenerated myelin sheath by
 Wallerian degeneration. The mechanism underlying the inefficiency in
 myelin clearance is not clear. Here we showed that endogenous proBDNF
 may inhibit the infiltration of ED1+ inflammatory cells after spinal
 cord injury. After injury, proBDNF and its receptors sortilin and
 p75NTR are expressed in the spinal cord as determined by Western blots
 and immunocytochemistry. ProBDNF and mature BDNF were released from
 macrophages in vitro. Macrophages in vivo (ED1+) and isolated in vitro
 (CD11b+) express moderate levels of proBDNF, sortilin and p75NTR.
 ProBDNF suppressed the migration of isolated macrophages in vitro and
 the antibody to proBDNF enhanced the migration. Suppression of proBDNF
 in vivo by administering the antiserum to the prodomain of BDNF after
 spinal cord injury (SCI) increased the infiltration of macrophages and
 increased number of neurons in the injured cord. BBB tests showed that
 the treatment of the antibody to proBDNF improved the functional
 recovery after spinal cord injury. Our data suggest that proBDNF is
 a suppressing factor for macrophage migration and infiltration and may
 play a detrimental role after SCI. (C) 2010 Elsevier Inc. All rights
 reserved.
 SN 0889-1591
 PD MAY
 PY 2010
 VL 24
 IS 4
 BP 585
 EP 597
 DI 10.1016/j.bbi.2010.01.001
 UT ISI:000277206600011
 PT J
 AU Xiang, H
 Zhao, W
 Xiao, H
 Qian, L
 Yao, Y
 Li, XB
 Liao, QJ
 AF Xiang, Hua
 Zhao, Wei
 Xiao, Hong
 Qian, Lei
 Yao, Yao
 Li, Xiao-Bo
 Liao, Qing-Jiang
 TI Synthesis and biological evaluation of isoflavone fatty acid esters
 with potential weight loss and hypolipidemic activities
 SO BIOORGANIC & MEDICINAL CHEMISTRY
 AB A series of isoflavone fatty acid esters were designed on the basis
 of endogenous oleoyl-estrone using estrogen moiety modification
 strategy. Ten new compounds were synthesized, and their body weight
 loss and hypolipidemic bioactivities were assayed. Some of these novel
 compounds could effectively inhibit the differentiation of 3T3-L1
 preadipocytes in vitro. The most potent compound 1a significantly
 decreased the body weight and white adipose tissue weight in a high-fat
 diet-induced rat model. Also, compound 1a showed good hypolipidemic
 activity and low toxicity. (c) 2010 Elsevier Ltd. All rights reserved.
 SN 0968-0896
 PD MAY 1
 PY 2010
 VL 18
 IS 9
 BP 3036
 EP 3042
 DI 10.1016/j.bmc.2010.03.055
 UT ISI:000277083400006
 PT J
 AU Chen, DQ
 Jiang, XQ
 Liu, J
 Jin, X
 Zhang, C
 Ping, QN
 AF Chen, Daquan
 Jiang, Xiaoqun
 Liu, Jia
 Jin, Xiang
 Zhang, Can
 Ping, Qineng
 TI In Vivo Evaluation of Novel pH-sensitive mPEG-Hz-Chol Conjugate in
 Liposomes: Pharmacokinetics, Tissue Distribution, Efficacy Assessment
 SO ARTIFICIAL CELLS BLOOD SUBSTITUTES AND BIOTECHNOLOGY
 SN 1073-1199
 PD MAY
 PY 2010
 VL 38
 IS 3
 BP 136
 EP 142
 DI 10.3109/10731191003685481
 UT ISI:000277264800004
 PT J
 AU Chen, HM
 Wang, DP
 Wang, XY
 Huang, WL
 Cai, Q
 Ding, K
 AF Chen, Huaming
 Wang, Deping
 Wang, Xianyang
 Huang, Wenlong
 Cai, Qian
 Ding, Ke
 TI Mild Conditions for Copper-Catalyzed N-Arylation of Imidazoles
 SO SYNTHESIS-STUTTGART
 AB An efficient copper(I) bromide catalyzed N-arylation of azoles with
 a variety of aromatic bromides and iodides under mild conditions is
 reported. This reaction displayed great functional group compatibility
 and excellent reactive selectivity.
 SN 0039-7881
 PD MAY
 PY 2010
 IS 9
 BP 1505
 EP 1511
 DI 10.1055/s-0029-1218691
 UT ISI:000276909600015
 PT J
 AU Huang, HP
 Gao, SL
 Chen, LL
 Wei, KH
 AF Huang, He-Ping
 Gao, Shan-Lin
 Chen, Lan-Lan
 Wei, Kun-Hua
 TI In vitro tetraploid induction and generation of tetraploids from
 mixoploids in Dioscorea zingiberensis
 SO PHARMACOGNOSY MAGAZINE
 AB This article describes an efficient colchicine-mediated technique for
 the in vitro induction of tetraploids in Dioscorea zingiberensis and
 its confirmation by flow cytometry. Buds immersed in 0.2% colchicine
 solution for 36 hours prior to culture induced as high as 35.6%
 tetraploid plants. Colchicine-induced tetraploids remained stable
 after six months in soil. Leaf characteristics of diploids and
 tetraploids in D. zingiberensis were compared. It was determined that
 the leaf sizes of glasshouse-grown plants and stomatal sizes of both
 in vitro and glasshouse-grown plants were suitable parameters for
 identifying putative tetraploids in D. zingiberensis. Besides
 generating tetraploids, this technique generated mixoploids in D.
 zingiberensis. Calli derived from mixoploid leaves were induced to form
 buds and shoots. Individual shoots were classed as diploid, mixoploid,
 and tetraploid by flow cytometry. This callus-based technique could
 be employed when a genome-doubling agent generated mixoploids, but no
 tetraploids.
 SN 0973-1296
 PD JAN-MAR
 PY 2010
 VL 6
 IS 21
 BP 51
 EP 56
 DI 10.4103/0973-1296.59966
 UT ISI:000276883000009
 PT J
 AU Zhang, H
 Yang, F
 Qi, J
 Song, XC
 Hu, ZF
 Zhu, DN
 Yu, BY
 AF Zhang, Hong
 Yang, Fan
 Qi, Jin
 Song, Xiao-Chen
 Hu, Zheng-Fang
 Zhu, Dan-Ni
 Yu, Bo-Yang
 TI Homoisoflavonoids from the Fibrous Roots of Polygonatum odoratum with
 Glucose Uptake-Stimulatory Activity in 3T3-L1 Adipocytes
 SO JOURNAL OF NATURAL PRODUCTS
 AB The EtOAc-soluble fraction of a 90% MeOH extract of the fibrous roots
 of Polygonatum ocloratum was found to potentiate insulin-stimulated
 glucose uptake in differentiated 3T3-L1 adipocytes. Bioassay-guided
 fractionation yielded nine homoisoflavonoids (1-9), four of which were
 new (1-4), together with an isoflavone glycoside (10) and a flavanone
 glycoside (11). The structures of new compounds were elucidated on the
 basis of extensive 1D and 2D NMR spectroscopy, and the absolute
 configurations were deduced by CD spectra. All 11 compounds showed
 effects of sensitizing adipocytes for insulin in a cell-based glucose
 uptake assay using 3T3-L1 adipocytes. The results indicate that
 homoisoflavonoids may be potential insulin sensitizers.
 SN 0163-3864
 PD APR
 PY 2010
 VL 73
 IS 4
 BP 548
 EP 552
 DI 10.1021/np900588q
 UT ISI:000276950000007
 PT J
 AU Sun, SX
 Li, YM
 Fang, WR
 Cheng, P
 Liu, LF
 Li, FW
 AF Sun, Shi-xue
 Li, Yun-man
 Fang, Wei-rong
 Cheng, Peng
 Liu, Lifang
 Li, Fengwen
 TI Effect and mechanism of AR-6 in experimental rheumatoid arthritis
 SO CLINICAL AND EXPERIMENTAL MEDICINE
 AB The root of Clematis chinensis Osbeck has been used widely in rheumatoid
 arthritis in Chinese traditional medicine and AR-6 is a triterpene
 saponin isolated from it. In this present study, we investigated in
 vivo effects of oral AR-6 in chronic rat adjuvant-induced arthritis
 (AA) and in vitro effect in macrophage and synoviocytes cells.
 Arthritic scores and serum inflammatory mediators were evaluated 19
 days after AA induction by endermic injection of Freund's complete
 adjuvant in Sprague-Dawley(S-D) rats. Oral administration of AR-6 to
 arthritic rats resulted in a clear decrease of clinical signs compared
 to untreated controls. The synoviocyte and macrophage response ex vivo
 were then analyzed. Anti-arthritic effects of AR-6 correlated with
 significant decrease of NO and TNF-alpha produced by peritoneal
 macrophages, ex vivo and in vitro. AR-6 also significant decreased the
 proliferation of synoviocyte. These data indicate that AR-6 is a
 potential anti-inflammatory therapeutic and preventive agent.
 SN 1591-8890
 PD JUN
 PY 2010
 VL 10
 IS 2
 BP 113
 EP 121
 DI 10.1007/s10238-009-0075-8
 UT ISI:000276963700005
 PT J
 AU He, LQ
 Liu, J
 Yin, DK
 Zhang, YH
 Wang, XS
 AF He, Li Qin
 Liu, Jing
 Yin, Deng Ke
 Zhang, Yi Hua
 Wang, Xiao Shan
 TI Synthesis and biological evaluation of nitric oxide-releasing matrine
 derivatives as anticancer agents
 SO CHINESE CHEMICAL LETTERS
 AB A series of furoxan-based nitric oxide-releasing matrine derivatives
 (10a-f) were synthesized. The biological evaluation showed that
 compounds 10a, 10b, 10e and 10f had stronger cytotoxic activities than
 5-fluorouracil against human hepatoma cells (HepG2) in vitro. (C) 2009
 Yi Hua Zhang. Published by Elsevier B.V. on behalf of Chinese Chemical
 Society. All rights reserved.
 SN 1001-8417
 PD APR
 PY 2010
 VL 21
 IS 4
 BP 381
 EP 384
 DI 10.1016/j.cclet.2009.11.033
 UT ISI:000276917900001
 PT J
 AU Qian, H
 Chen, W
 Zhou, JP
 Huang, WL
 Zhang, HB
 Jin, J
 AF Qian, Hai
 Chen, Wei
 Zhou, Jin Pei
 Huang, Wen Long
 Zhang, Hui Bin
 Jin, Jing
 TI Total synthesis of endothelin 1 by microwave-assisted solid phase
 method
 SO CHINESE CHEMICAL LETTERS
 AB A microwave-assisted solid phase synthesis for endothelin 1 is
 presented. Reduced endothelin I was synthesized efficiently on Wang
 resin under microwave irradiation using Fmoc/tBu orthogonal protection
 strategy. The whole peptide was cleaved from the resin and two
 disulphide bridges were formed under air oxidation at room temperature.
 The purity and efficiency of synthesizing the peptide is much higher
 than other methods used before. (C) 2009 Jin Pei Zhou. Published by
 Elsevier B.V. on behalf of Chinese Chemical Society. All rights
 reserved.
 SN 1001-8417
 PD APR
 PY 2010
 VL 21
 IS 4
 BP 388
 EP 390
 DI 10.1016/j.cclet.2009.12.016
 UT ISI:000276917900003
 PT J
 AU Chen, XM
 Qian, SH
 Feng, F
 AF Chen, Xiu Mei
 Qian, Shi Hui
 Feng, Feng
 TI Two new tetrahydronaphthalenes from the stem of Impatiens balsamina
 SO CHINESE CHEMICAL LETTERS
 AB Two new tetrahydronaphthalenes, 1 alpha, 2 alpha-diol-4
 alpha-ethoxy-1, 2, 3, 4-tetrahydronaphthalene (1) and 1 alpha, 2 alpha,
 4 beta-triol-1, 2, 3, 4-tetrahydronaphthalene (2), were isolated from
 the stem of Impatiens balsamina L. Their structures were elucidated
 by various spectroscopic methods. (C) 2009 Feng Feng. Published by
 Elsevier B.V. on behalf of Chinese Chemical Society. All rights
 reserved.
 SN 1001-8417
 PD APR
 PY 2010
 VL 21
 IS 4
 BP 440
 EP 442
 DI 10.1016/j.cclet.2009.12.019
 UT ISI:000276917900016
 PT J
 AU Zhao, LY
 Dong, YH
 Chen, GT
 Hu, QH
 AF Zhao, Liyan
 Dong, Yanhong
 Chen, Guitang
 Hu, Qiuhui
 TI Extraction, purification, characterization and antitumor activity of
 polysaccharides from Ganoderma lucidum
 SO CARBOHYDRATE POLYMERS
 AB Ultrasonic-aid extraction (UAE) was applied to the extraction of
 polysaccharides from Ganoderma lucidum and then the crude
 polysaccharides were purified by filtration, DEAE cellulose-52
 chromatography and Sephadex G-100 size-exclusion chromatography in
 that order. Two main fractions, GP-1 and GP-2, were obtained through
 the extraction and purification steps. The characterizations, such as
 molecular weight, monosaccharides composition, ultraviolet spectrum
 and infrared spectrum of the two fractions were analyzed in this study.
 Furthermore, the influence of G. lucidum polysaccharides fractions
 upon activation of macrophage cell (RAW 264.7) and antitumor activities
 to the human breast cancer cell (MDA-MB-231) in vitro were evaluated
 by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium
 bromide) assay. The results indicated that GP-1 and GP-2 can increase
 the proliferation and pinocytic activity of macrophage significantly
 and play an inhibited effect on the cancer cell, moreover, the antitumor
 activity of the GP-1 and GP-2 increased with the participation of the
 antitumor factors induced from macrophage by polysaccharides
 fractions. (C) 2009 Elsevier Ltd. All rights reserved.
 SN 0144-8617
 PD MAY 5
 PY 2010
 VL 80
 IS 3
 BP 783
 EP 789
 DI 10.1016/j.carbpol.2009.12.029
 UT ISI:000276987800023
 PT J
 AU Zhang, Q
 Wang, GJ
 Jiye, A
 Ma, B
 Dua, Y
 Zhu, LL
 Wu, D
 AF Zhang, Qi
 Wang, Guangji
 Jiye A
 Ma, Bo
 Dua, Yu
 Zhu, Lingling
 Wu, Di
 TI Metabonomic profiling of diet-induced hyperlipidaemia in a rat model
 SO BIOMARKERS
 AB This study describes the metabolic profiles of the development of
 hyperlipidaemia in a rat model, utilizing metabonomics by gas
 chromatography-mass spectrometry (GC-MS) determination coupled with
 multivariate statistical analysis. Rat plasma samples were collected
 before and during a high-lipid diet at days 0, 7, 14, 21 and 28, and
 were analysed for lipid levels using kit assays or metabonomics using
 GC-MS. Forty-one endogenous metabolites were separated, identified and
 quantified using GC-MS. The data matrix was processed by principal
 component analysis or partial least squares discriminant analysis.
 Dynamic modification of the rat metabonome can be clearly identified
 and tracked at different stages of hyperlipidaemia in the rat model.
 Potential biomarkers, including beta-hydroxybutyrate, tyrosine and
 creatinine, were identified. The current work suggests that
 metabonomics is able to provide an overview of biochemical profiles
 of disease progress in animal models. Using a metabonomic approach to
 identify physiopathological states promises to establish a new
 methodology for the early diagnosis of human diseases.</.
 SN 1354-750X
 PD MAY
 PY 2010
 VL 15
 IS 3
 BP 205
 EP 216
 DI 10.3109/13547500903419049
 UT ISI:000276898100002
 PT J
 AU Yue, ZB
 Zhang, ML
 Sheng, GP
 Liu, RH
 Long, Y
 Xiang, BR
 Wang, J
 Yu, HQ
 AF Yue, Zheng-Bo
 Zhang, Meng-Lin
 Sheng, Guo-Ping
 Liu, Rong-Hua
 Long, Ying
 Xiang, Bing-Ren
 Wang, Jin
 Yu, Han-Qing
 TI Determination of main components and anaerobic rumen digestibility of
 aquatic plants in vitro using near-infrared-reflectance spectroscopy
 SO WATER RESEARCH
 AB A near-infrared-reflectance (NIR) spectroscopy-based method is
 established to determine the main components of aquatic plants as well
 as their anaerobic rumen biodegradability. The developed method is more
 rapid and accurate compared to the conventional chemical analysis and
 biodegradability tests. Moisture, volatile solid, Klason lignin and
 ash in entire aquatic plants could be accurately predicted using this
 method with coefficient of determination (r(2)) values of 0.952, 0.916,
 0.939 and 0.950, respectively. In addition, the anaerobic rumen
 biodegradability of aquatic plants, represented as biogas and methane
 yields, could also be predicted well. The algorithm of continuous
 wavelet transform for the NIR spectral data pretreatment is able to
 greatly enhance the robustness and predictive ability of the NIR
 spectral analysis. These results indicate that NIR spectroscopy could
 be used to predict the main components of aquatic plants and their
 anaerobic biodegradability. (C) 2010 Elsevier Ltd. All rights
 reserved.
 SN 0043-1354
 PD APR
 PY 2010
 VL 44
 IS 7
 BP 2229
 EP 2234
 DI 10.1016/j.watres.2009.12.049
 UT ISI:000276668700015
 PT J
 AU Wu, WJ
 Xu, XX
 Dai, Y
 Xia, LZ
 AF Wu, Wenjun
 Xu, Xianxiang
 Dai, Yue
 Xia, Lunzhu
 TI Therapeutic Effect of the Saponin Fraction from Clematis chinensis
 Osbeck Roots on Osteoarthritis Induced by Monosodium Iodoacetate
 through Protecting Articular Cartilage
 SO PHYTOTHERAPY RESEARCH
 AB The objective of the present study was to investigate the effect of
 the saponin fraction from Clematis chinensis Osbeck roots (SFC) on an
 osteoarthritis model in rats and to explore its underlying mechanisms.
 Osteoarthritis was induced by intraarticular injection of monosodium
 iodoacetate (MIA) into knee joints of rats, and SEC and diclofenac were
 orally administered once a day for 28 consecutive days. Joint swelling,
 macroscopic observation, histological assessment and proteoglycan
 (PG) degradation were examined. In vitro, cultured rabbit chondrocytes
 were stimulated with MIA and sodium nitroprusside (SNP), respectively.
 The effects of SFC on MIA- and SNP-induced chondrocyte injury were
 examined by MTT assay. It was shown that SFC (50, 100, 200 mg/kg)
 dose-dependently reduced cartilage injury and PG degradation induced
 by MIA. Diclofenac (4 mg/kg) only slightly alleviated cartilage injury
 and PG degradation. SFC also prevented SNP- or MIA-induced rabbit
 chondrocyte impairment. These results indicate that SEC is effective
 in ameliorating joint destruction and cartilage erosion in MIA-induced
 osteoarthritic in rats, and the mechanisms of action for protecting
 articular cartilage are through preventing extracellular matrix
 degradation and chondrocyte injury. Copyright (C) 2009 John Wiley &
 Sons, Ltd.
 SN 0951-418X
 PD APR
 PY 2010
 VL 24
 IS 4
 BP 538
 EP 546
 DI 10.1002/ptr.2977
 UT ISI:000276802500012
 PT J
 AU Chu, C
 Cai, HX
 Ren, MT
 Liu, EH
 Li, B
 Qi, LW
 Li, P
 AF Chu, Chu
 Cai, Hai-Xia
 Ren, Mei-Ting
 Liu, E-Hu
 Li, Bin
 Qi, Lian-Wen
 Li, Ping
 TI Characterization of novel astragaloside malonates from Radix Astragali
 by HPLC with ESI quadrupole TOF MS
 SO JOURNAL OF SEPARATION SCIENCE
 AB A structurally identified new compound named malonylastragaloside I
 was isolated and obtained from Radix Astragali. This novel compound
 was found to be unstable especially under high temperature and pH value.
 Using sonication extraction, addition of formic acid, and an efficient
 medium pressure ODS C-18 column chromatography method, a high yield
 of 40 mg of this compound was obtained from 150 g of powdered crude
 herbal medicine. Malonylastragaloside I was structurally
 characterized by NMR and ESI quadrupole TOF MS. With the strategy of
 target precursor ions scan, a total of 22 astragalosides including 8
 astragaloside malonates were screened and characterized from the
 methanolic extract of Radix Astragali by HPLC-Q-TOF/MS. The eight
 astragaloside malonates were found in both Astragalus membranaceus
 var. mongholicus and A. membranaceus. The results provided a real
 profile of various triterpene saponins in Radix Astragali. It is a first
 report regarding isolation and characterization of astragaloside
 malonates in Astragalus species.
 SN 1615-9306
 PD MAR
 PY 2010
 VL 33
 IS 4-5
 BP 570
 EP 581
 DI 10.1002/jssc.200900687
 UT ISI:000276573800015
 PT J
 AU Chen, JZ
 Chou, GX
 Wang, CH
 Yang, L
 Bligh, SWA
 Wang, ZT
 AF Chen, Jian-Zhong
 Chou, Gui-Xin
 Wang, Chang-Hong
 Yang, Li
 Bligh, S. W. Annie
 Wang, Zheng-Tao
 TI Characterization of new metabolites from in vivo biotransformation of
 norisoboldine by liquid chromatography/mass spectrometry and NMR
 spectroscopy
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 AB Nolisoboldine (1,9-dihydroxy-2,10-dimethoxynoraporphine) is one of
 the major bioactive isoquinoline alkaloids in Linderae Radix, a
 commonly used Chinese herbal medicine The aim of this study is to
 isolate and characterize metabolites of norisoboldine after gavage
 feeding in rats High-performance liquid chromatography coupled with
 electrospray ionization and ion-trap mass spectrometry (HPLC-ESI/MS")
 was used to identify metabolites of norisoboldine in rat urine and bile
 samples A total of five metabolites of norisoboldine were characterized
 by comparing retention time and UV absorption in HPLC, and by molecular
 mass and fragmentation pattern of the analytes by mass spectrometry
 with those of norisoboldine Two new glucuronide conjugates of
 norisoboldine, noriosboldine-1-O-beta-D-glucuionide and rim
 isobolchne-9-O-alpha-D-glucuromde, were isolated from rat urine
 samples and their structures were ;confirmed by NMR spectioscopy ((1H),
 C-13, HMBC and HSQC) for the fiist time The iesults suggested that
 glucuromdation and sulfation were involved in metabolic pathways of
 nonsobolchne in rat (C) 2010 Elsevier B V All tights ieseived
 SN 0731-7085
 PD SEP 5
 PY 2010
 VL 52
 IS 5
 BP 687
 EP 693
 DI 10.1016/j.jpba.2010.02.008
 UT ISI:000276785400007
 PT J
 AU Lin, YN
 Zhu, DN
 Qi, J
 Qin, MJ
 Yu, BY
 AF Lin, Yining
 Zhu, Danni
 Qi, Jin
 Qin, Minjian
 Yu, Boyang
 TI Characterization of homoisoflavonoids in different cultivation
 regions of Ophiopogon japonicus and related antioxidant activity
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 AB Homoisoflavonoids were identified in Ophiopogon japonicas of two
 cultivation regions in China Hangmaidong (grown in Zhejiang province)
 and Chuan-maidong (grown in Sichuan province). Liquid chromatography
 (LC). coupled with electrospray ionization (ESI) tandem mass
 spectrometry (MS), was developed to analyze homoisoflavonoids in these
 two areas. Based on LC-MS/MS data, 24 homoisoflavonoid compounds-19
 in Hang-maidong and 17 in Chuan-maidong were identified or tentatively
 characterized The homoisoflavonoids in the two regions were similar
 in chemical profile, but distinctive in their combination and ratio
 Methylophiopogonanone A and methylophiopogonanone B were the major
 contributors to the total homoisoflavonoid content Hang-maidong had
 a higher total homoisoflavonoid content and better DPPH
 (2,2-diphenyl-1-pieryl-hydrazyl) radical-scavenging activity than
 that of Chuan-maidong. The total phenolic content showed no significant
 difference between the two regions. This study allows a clear chemical
 differentiation of Hang-maidong from Chuan-maidong (C) 2010 Elsevier
 B V All rights reserved
 SN 0731-7085
 PD SEP 5
 PY 2010
 VL 52
 IS 5
 BP 757
 EP 762
 DI 10.1016/j.jpba.2010.02.016
 UT ISI:000276785400018
 PT J
 AU Luo, XG
 Zou, JN
 Wang, SZ
 Zhang, TC
 Xi, T
 AF Luo, Xue-Gang
 Zou, Jia-Ning
 Wang, Shu-Zhen
 Zhang, Tong-Cun
 Xi, Tao
 TI Novobiocin Decreases SMYD3 Expression and Inhibits the Migration of
 MDA-MB-231 Human Breast Cancer Cells
 SO IUBMB LIFE
 AB SET and MYND domain-containing protein 3 (SMYD3) is a histone
 methyltransferase that plays an important role in transcriptional
 regulation in human carcinogenesis, and heat-shock protein HSP90A has
 been shown to increase the activity of SMYD3. We previously reported
 that overexpression of SMYD3 stimulated the migration of cells. In this
 study, we further found that novobiocin, a HSP90 inhibitor, could
 decrease the expression of SMYD3 and dose dependently inhibit the
 proliferation and migration of MDA-MB-231 human breast cancer cells.
 As a control, the short hairpin RNA (shRNA) targeting SMYD3 gene also
 showed similar effects with novobicin. This study is the first to show
 that novobiocin can inhibit the migration of breast cancer cells and
 such event may involve the downregulation of SMYD3. These findings
 might throw light on the development of novel therapeutic approaches
 to human cancers, and lend further understanding to the potential role
 of SMYD3 in human carcinogenesis. (C) 2009 IUBMB IUBMB Life, 62(3):
 194-199, 2010
 SN 1521-6543
 PD MAR
 PY 2010
 VL 62
 IS 3
 BP 194
 EP 199
 DI 10.1002/iub.288
 UT ISI:000276585200005
 PT J
 AU Zhu, Y
 Li, HF
 Lu, S
 Zheng, YX
 Wu, Z
 Tang, WF
 Zhou, X
 Lu, T
 AF Zhu, Yong
 Li, Hui-Fang
 Lu, Shuai
 Zheng, Yi-Xuan
 Wu, Zeng
 Tang, Wei-Fang
 Zhou, Xiang
 Lu, Tao
 TI Investigation on the isoform selectivity of histone deacetylase
 inhibitors using chemical feature based pharmacophore and docking
 approaches
 SO EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 AB A three dimensional (3D) chemical feature based pharmacophore model
 was developed for selective histone deacetylase 1 (HDAC1) inhibitors,
 which provides an efficient way to discuss the isoform selectivity of
 HDAC inhibitors. In contrast to the classical pan-HDAC pharmacophore,
 two hydrophobic features (HY and HYAr2) were found in the chemical
 feature based pharmacophore model, which might be responsible for the
 selectivity of HDAC1 inhibitions. Molecular docking also highlighted
 the two hydrophobic features, which are located in the internal cavity
 adjacent to the active site. The results contribute to our
 understanding of the molecular mechanism underlying the selectivity
 of HDAC1 inhibitors and suggest a possible target region to design novel
 selective HDAC1 inhibitors. (C) 2010 Elsevier Masson SAS. All rights
 reserved.
 SN 0223-5234
 PD MAY
 PY 2010
 VL 45
 IS 5
 BP 1777
 EP 1791
 DI 10.1016/j.ejmech.2010.01.010
 UT ISI:000276695200012
 PT J
 AU Chen, JQ
 Du, YX
 Zhu, FX
 Chen, B
 AF Chen, Jiaquan
 Du, Yingxiang
 Zhu, Fenxia
 Chen, Bin
 TI Glycogen: A novel branched polysaccharide chiral selector in CE
 SO ELECTROPHORESIS
 AB Various chiral selectors have been employed in CE and among them linear
 polysaccharides exhibited powerful enantioselective properties
 Different from linear polysaccharides, the use of branched
 polysaccharides as chiral selectors in CE has not been reported
 previously. In this study glycogen belonging to the class of branched
 polysaccharides was used as a novel chiral selector for the
 enantiomeric separations for the first time. Since glycogen is
 electrically neutral, the method is applicable to ionic compounds.
 Eighteen chiral compounds including 12 basic drugs and six acidic drugs
 have been tested to demonstrate the potential of this chiral selector
 BGE and selector concentrations and buffer pH were systematically
 optimized in order to obtain successful chiral separations Among the
 tested compounds, the enantiomers of ibuprofen, which is an acidic
 drug, were successfully recognized by 3.0% w/v glycogen with 90 mM
 Tris-H3PO4 buffer (pH 7 0). The enantiomers of basic drugs such as
 citalopram, cetirizine and nefopam were also baseline-resolved with
 50 mM Tris-H3PO4 buffer (pH 3 0) containing 3.0% glycogen Amlodipine
 belonging to basic compound only gave partial enantioseparation under
 the above-mentioned condition.
 SN 0173-0835
 PD MAR
 PY 2010
 VL 31
 IS 6
 BP 1044
 EP 1050
 DI 10.1002/elps.200900534
 UT ISI:000276807300008
 PT J
 AU Li, N
 Jia, N
 Dai, DZ
 Hu, C
 Dai, Y
 AF Li, Na
 Jia, Nan
 Dai, De-Zai
 Hu, Chen
 Dai, Yin
 TI Role of endothelin in the effects of isoprenaline on potassium currents
 and calsequestrin 2 expression in the heart
 SO CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY
 AB P>1. Activation of beta-receptors may modulate potassium channels and
 calcium handling proteins and serve as a basis for arrhythmogenesis.
 We determined whether an endothelin (ET) receptor antagonist CPU0213
 could relieve the isoprenaline-(ISO) induced changes in I-Kr and I-Ks
 and calsequestrin 2 (CASQ2) in the heart.
 2. In isolated ventricular myocytes, the I-Kr and I-Ks currents and
 expression for CASQ2, FKBP12.6, SERCA2a and ETAR were measured in the
 presence of ISO and either propranolol or CPU0213.
 3. In the presence of ISO, I-Kr and I-Ks currents were significantly
 exaggerated and FKBP12.6, SERCA2a and CASQ2 were downregulated
 together with upregulation of ETAR in the myocardium. Interestingly,
 endothelin-1 was also effective in downregulating the expression of
 CASQ2. These changes were partially relieved by either CPU0213 or
 propranolol.
 4. I-Kr and I-Ks currents can be separated into exaggerated/induced
 and basic components in the presence of ISO. The former, induced by
 ISO, is pathological and sensitive to either CPU0213 or propranolol.
 5. Exaggerated I-Kr and I-Ks and downregulated CASQ2 by ISO are relevant
 to stress-related events in which the ET pathway is actively involved.
 By suppressing the ISO-exaggerated I-Kr and I-Ks and normalizing the
 expression of CASQ2, endothelin receptor antagonism is likely
 promising in dealing with stress-related cardiac arrhythmias.
 SN 0305-1870
 PD MAY-JUN
 PY 2010
 VL 37
 IS 5-6
 BP 557
 EP 563
 DI 10.1111/j.1440-1681.2010.05349.x
 UT ISI:000276776700006
 PT J
 AU Zhang, LP
 Wang, YL
 AF Zhang Lan-ping
 Wang Ya-lou
 TI Facile Synthesis of 5-Hydroxy-2-(2-phenylethyl)chromone
 SO CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
 AB 5-Hydroxy-2-(2-phenylethyl)chromone(1) was synthesized from
 2,6-dihydroxyacetophenone(7) obtained via four-steps
 resorcinol-reacting with phenylpropionic acid, the procedures
 involved are Baker-Venkataraman rearrangement and cyclization which
 are easy to conduct, the overall yield is 32%.
 SN 1005-9040
 PD MAR 25
 PY 2010
 VL 26
 IS 2
 BP 245
 EP 248
 UT ISI:000276590500018
 PT J
 AU Wu, FW
 Xu, ZH
 Wang, ZX
 Shi, YQ
 Li, L
 Zhang, ZB
 AF Wu, Fawen
 Xu, Zhihong
 Wang, Zhixiang
 Shi, Yiqiang
 Li, Lei
 Zhang, Zhibing
 TI Membrane-based air separation for catalytic oxidation of
 isolongifolene
 SO CHEMICAL ENGINEERING JOURNAL
 AB Oxygen-enriched air (OEA) from membrane-based air separation has been
 widely used in the industrial field in the past two decades.
 Isolongifolenone, an oxygenated derivative of isolongifolene, is an
 important perfume ingredient in the perfumery industry. In this paper,
 the DEA produced by the membranes was employed as oxidant to convert
 isolongifolene into isolongifolenone with cobaltous acetate as
 catalyst. The effects of the reaction conditions on the conversion and
 the yield were investigated thoroughly. It was found that the
 conversion of isolongifolene increased with the oxygen concentration
 of the OEA and the reaction temperature. The maximum yield was obtained
 under the conditions of the oxygen concentration of 33.1% and the
 temperature of 60 degrees C. Both the conversion and the yield increased
 with the flux of IDEA. In addition, the solvent-free reaction process
 not only facilitated the catalyst recovery, but also minimized the
 effluent discharge. (C) 2010 Elsevier B.V. All rights reserved.
 SN 1385-8947
 PD APR 15
 PY 2010
 VL 158
 IS 3
 BP 426
 EP 430
 DI 10.1016/j.cej.2010.01.012
 UT ISI:000276783300008
 PT J
 AU Wang, YH
 Sun, JF
 Tao, YM
 Xu, XJ
 Chi, ZQ
 Liu, JG
 AF Wang, Yu-hua
 Sun, Jian-feng
 Tao, Yi-min
 Xu, Xue-jun
 Chi, Zhi-qiang
 Liu, Jing-gen
 TI Paradoxical relationship between RAVE (relative activity versus
 endocytosis) values of several opioid receptor agonists and their
 liability to cause dependence
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To examine the relationship between the RAVE (relative activity
 versus endocytosis) values of opiate agonists and their dependence
 liability by studying several potent analgesics with special profiles
 in the development of physical and psychological dependence.
 Methods: The effects of (-)-cis-(3R, 4S, 2'R) ohmefentanyl (F9202),
 (+)-cis-(3R, 4S, 2'S) ohmefentanyl (F9204), dihydroetorphine (DHE) and
 morphine on [S-35] GTP gamma S binding, forskolin-stimulated cAMP
 accumulation, and receptor internalization were studied in CHO cells
 stably expressing HA-tagged mu-opioid receptors (CHO-HA-MOR). cAMP
 overshoot in response to the withdrawal of these compound treatments
 was also tested.
 Results: All four agonists exhibited the same rank order of activity
 in stimulation of [S-35]GTP gamma S binding, inhibition of adenylyl
 cyclase (AC) and induction of receptor internalization:
 DHE>F9204>F9202> morphine. Based on these findings and the previous
 in vivo analgesic data obtained from our and other laboratories, the
 RAVE values of the four agonists were calculated. The rank order of
 RAVE values was morphine>F9202>F9204>DHE. For the induction of cAMP
 overshoot, the rank order was F9202 >= morphine>F9204 >= DHE.
 Conclusion: Taken in combination with previous findings of these
 compounds' liability to develop dependence, the present study suggests
 that the agonist with the highest RAVE value seems to have a relatively
 greater liability to develop psychological dependence relative to the
 agonist with the lowest RAVE value. However, the RAVE values of these
 agonists are not correlated with their probability of developing
 physical dependence or inducing cAMP overshoot, a cellular hallmark
 of dependence.
 SN 1671-4083
 PD APR
 PY 2010
 VL 31
 IS 4
 BP 393
 EP 398
 DI 10.1038/aps.2010.19
 UT ISI:000276834300002
 PT J
 AU Wang, ZQ
 Chen, S
 Lu, YN
 Ni, KY
 He, H
 AF Wang Zhiqun
 Chen Shi
 Lue Yanni
 Ni Kunyi
 He Hua
 TI Molecular Modeling of the Interaction Between Mitoxantrone and B-DNA
 SO ACTA CHIMICA SINICA
 AB Molecular modeling methods have been applied to characterization of
 the intercalation mode of the anticancer drug mitoxantrone (MTX) into
 B-DNA fragments for controversies. The results show that there are
 groove selectivity and base pairs specificity recognition between MTX
 and B-DNA, MTX prefers to intercalate into DNA from the minor groove
 for the base pair 5'-CG. Through analyzing the detailed energy terms
 of DNA-MTX, the steric interactions, especially the electrostatic
 interactions were found to be the main factors to the primary drive
 of intercalation and base pairs specificity. The conformation of
 MTX-DNA at the best action site shows that only a portion of the
 chromophore of MTX was involved in the intercalation into DNA base pairs
 and the binding of MTX to DNA was potentially enhanced by the presence
 of side chains which could bind electrostatically to the phosphate
 groups spreading along 3'-5' of the B-DNA.
 SN 0567-7351
 PD MAR 28
 PY 2010
 VL 68
 IS 6
 BP 551
 EP 556
 UT ISI:000276585500015
 PT J
 AU Lu, D
 Huang, WL
 AF Lu, Dong
 Huang, Wenlong
 TI Overview of drug evaluation system in China
 SO SCIENTIFIC RESEARCH AND ESSAYS
 AB Developing a drug requires great amount of research work in chemistry,
 manufacturing, controls (CMC), preclinical science and clinical
 trials. Drug reviewers in regulatory agencies around the world bear
 the responsibility of evaluating whether the research data support the
 safety, effectiveness and quality control of a new drug product to serve
 the public health. This article provides an overview of the drug
 evaluation procedure implemented in China's drug regulatory agency,
 State Food and Drug Administration (SFDA). Several unique features are
 discussed in details. This article provides insight into the drug
 evaluation system and requirements in China. As a developing country,
 China developed its own unique drug evaluation system along its drug
 development history while learning from those systems established in
 developed countries. China uses this system to reach a goal: ensuring
 safe and effective drug products for patients around the world.
 SN 1992-2248
 PD MAR 18
 PY 2010
 VL 5
 IS 6
 BP 514
 EP 518
 UT ISI:000276344700002
 PT J
 AU Zheng, YW
 Vagal, S
 Zhu, XX
 de Waele, C
 Smith, PF
 Wang, GJ
 Zhang, M
 Darlington, CL
 AF Zheng, Yiwen
 Vagal, Shweta
 Zhu, Xuan-xuan
 de Waele, Catherine
 Smith, Paul F.
 Wang, Guangji
 Zhang, Ming
 Darlington, Cynthia L.
 TI The effects of the Chinese herbal medicine EMF01 on salicylate-induced
 tinnitus in rats
 SO JOURNAL OF ETHNOPHARMACOLOGY
 AB Aim of the study. Traditional Chinese medicine (TCM) has been reported
 to successfully alleviate tinnitus. although well-controlled studies
 have not been conducted. In this study, we attempted to test a TM Er
 Ming Fang (EMF01) containing Rehmannia glutinosa, Cornus officinalis,
 Salvia mittiorrhiza, Pueraria, Schisandra chinensis, Porto cocos and
 Platycodon grandiflorum, on salicylate-induced tinnitus in rats, using
 a conditioned lick suppression paradigm
 Materials and methods. A pilot study examined the effect of 8.75 g/kg
 and 17.5 g/kg EMF01 (delivered by oral gavage for 20 days) and showed
 a slight decrease in the suppression ratio (SR) in the 8 75 g/kg group
 In order to confirm the possible effect of EMF01 on [Humus at 8 75 g/kg,
 a further study was carried out with a larger sample size
 Results While there were statistically significant differences between
 the treatment groups, post hoc tests revealed that EMF01 did not have
 any significant effect on salicylate-induced tinnitus
 Conclusions While this study does not support the efficacy of EMF01
 in the treatment of salicylate-induced tinnitus, further studies
 should be conducted to determine if it alleviates tinnitus associated
 with acoustic trauma (C) 2010 Elsevier Ireland Ltd. All rights reserved
 SN 0378-8741
 PD MAR 24
 PY 2010
 VL 128
 IS 2
 BP 545
 EP 548
 DI 10.1016/j.jep.2010.01.053
 UT ISI:000276429000037
 PT J
 AU Tong, Y
 Zhong, K
 Tian, H
 Gao, XD
 Xu, XY
 Yin, XJ
 Yao, WB
 AF Tong, Yue
 Zhong, Kai
 Tian, Hong
 Gao, Xiangdong
 Xu, Xiangyang
 Yin, Xiaojin
 Yao, Wenbing
 TI Characterization of a monoPEG20000-Endostar
 SO INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
 AB In this study, we investigated the PEG attachment site of
 mono-PEGylated Endostar, a modified recombinant human endostatin
 approved in China for lung cancer N-terminal site-dilected
 mono-PEGylation of Endostar was accomplished using
 mPEG-propionaldehyde derivatives (Mw = 20 kDa) under slightly acidic
 pH conditions (pH 5 5) One-step cation exchange chromatography was used
 to purify the mono-PEGylated Endostar Following tryptic digestion, the
 peptide fragment containing PEG was separated by SDS-PAGE Barium iodide
 staining and Western blotting were used to detect the PEG moiety and
 the N-terminus of Endostar. respectively The peptide fragment stained
 by barium iodide showed a positive response to anti-(His) 6 mAb,
 demonstrating that PEG was located at the N-terminus of Endostar LC/MS
 was applied to verify the occurrence of mono-PEGylation at the
 N-terminus of Endostar. (C) 2010 Elsevier B V All rights reserved
 SN 0141-8130
 PD APR 1
 PY 2010
 VL 46
 IS 3
 BP 331
 EP 336
 DI 10.1016/j.ijbiomac.2010.01.017
 UT ISI:000276381300009
 PT J
 AU Lu, Y
 Zhang, HY
 Hou, J
 Wang, HQ
 Hu, XB
 Ma, YJ
 Ge, XY
 Huang, L
 Yang, YA
 Cao, RY
 Fan, H
 Liu, JJ
 Wu, J
 AF Lu Yong
 Zhang Huiyong
 Hou Jing
 Wang Huaqian
 Hu Xiangbing
 Ma Yanjun
 Ge Xiaoyu
 Huang Li
 Yang Yanan
 Cao Rongyue
 Fan Hao
 Liu Jingjing
 Wu Jie
 TI Vaccination with a potent DNA vaccine targeting B-cell epitopes of hGRP
 induces prophylactic and therapeutic antitumor activity in vivo
 SO GENE THERAPY
 AB Gastrin-releasing peptide (GRP), a bombesin-like peptide, is an
 autocrine or paracrine growth factor that can stimulate the growth of
 various cancer cells, making it an ideal target antigen to develop
 vaccines against cancer. In this study, we developed a novel DNA vaccine
 that encodes six tandem repeats of B-cell epitope GRP(18-27) (GRP6)
 flanked by HSP65 as carrier and four tandem repeats of mycobacterial
 HSP70(407-426) (M4) as helper T-cell epitopes for enhancement of
 immunogenicity. When intramuscularly immunized to mice, this anti-GRP
 DNA vaccine-induced GRP-specific antibody ( Ab) responses that were
 at least 10-fold higher in magnitude compared with HSP65-GRP6 protein
 vaccine. Both prophylactic and therapeutic antitumor immunities
 induced by vaccination significantly suppressed the growth of
 GRP-dependent prostate carcinoma RM-1 in vivo and prolonged the
 survival of tumor-inoculated mice. Out results also showed that the
 immune sera with high titer of GRP-specific Abs effectively inhibited
 the growth of tumor in mice and dose dependently inhibited
 proliferation of cultured RM-1 cells in vitro, suggesting that the GRP
 neutralizing Ab is responsible for the protective and therapeutic
 antitumor activity of vaccination. These findings may be of great
 importance in the further exploration of the applications of growth
 factors identified in human in cancer therapy. Gene Therapy (2010) 17,
 459-468; doi: 10.1038/gt.2009.165; published online 4 February 2010
 SN 0969-7128
 PD APR
 PY 2010
 VL 17
 IS 4
 BP 459
 EP 468
 DI 10.1038/gt.2009.165
 UT ISI:000276425800003
 PT J
 AU Guo, DH
 Deng, XJ
 Zhao, SZ
 Zhu, J
 Xia, CF
 Chen, SS
 Song, Y
 AF Guo De-Hua
 Deng Xiao-Jun
 Zhao Shan-Zhen
 Zhu Jian
 Xia Chong-Fei
 Chen Shun-Sheng
 Song Yue
 TI Simultaneous Determination of 76 Veterinary Drug Residues in
 Foodstuffs of Animal Origin by Solid Phase Extraction-Liquid
 Chromatography-Tandem Mass Spectrometry
 SO CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
 AB A method based on solid phase extraction-liquid chromatography-tandem
 mass spectrometry for the simultaneous determination of 76 veterinary
 drugs in foodstuffs of animal origin was presented. The residues
 derived from pork, shrimp, milk, liver and egg were extracted by
 acetonitrile combined with citrate buffer containing magnesium cation.
 The extracts were distilled and redissolved with citrate buffer
 followed by a further cleanup procedure using polymer connected with
 cation exchange SPE column. The residues retained in column were rinsed
 with methanol and mixture of methanol and ammonium hydroxide (95:5,
 V/V). Sample matrix-matched calibration was used to determine the
 residue contents by external standard. The method provided a LOQ of
 0.5 mu g/kg (beta-agonist and triphenylmethane), 1.0 mu g/kg
 (benzodiazepine and nitroimdazole), 5.0 mu g/kg( benzimidazole) and
 20.0 mu g/kg( sulfanilamide), linear relationship more than 0.907 and
 a recovery ranged from 59.4% to 115.3% with a RSD between 2.6% and 27.3%
 in sample matrix. The practical inspection using the method offered
 two positive samples for ractopamine and diazepam with a residual
 concentration of 0.92 and 6.5 mu g/kg.
 SN 0253-3820
 PD MAR
 PY 2010
 VL 38
 IS 3
 BP 318
 EP 324
 DI 10.3724/SP.J.1096.2010.00318
 UT ISI:000276536700004
 PT J
 AU Ren,
 Yan,
 Yao,
 Jin,
 Gao,
 AF Ren,
 Yan,
 Yao,
 Jin,
 Gao,
 Wenbing
 Xiangdong
 TI Enzymatic degradation products from a marine polysaccharide YCP with
 different immunological activity and binding affinity to macrophages,
 hydrolyzed by alpha-amylases from different origins
 SO BIOCHIMIE
 AB YCP is a marine polysaccharide with anti-tumor and immune-modulating
 effects. This study evaluated the effect of enzymatic degradation of
 YCP by alpha-amylases from different origins on its immunological
 activity and binding ability to the macrophages. YCP was hydrolyzed
 by alpha-amylases isolated from Aspergillus oryzae, Bacillus
 licheniformis, Barley malt, and Porcine pancreas respectively, then
 four fragments with unique molecular weight (termed: YCP-Ao, YCP-Bl,
 YCP-Bm, and YCP-Pp, respectively) were obtained. The four fragments
 showed different immunological activity and the ability to bind to
 macrophages. Among them, YCP-Ao possessed almost equivalent
 immunological activity compared to the original YCP, while such
 properties were not retained in YCP-Bl. Our further study showed that
 YCP-Ao prevented YCP from binding to macrophages. In conclusion, YCP-Ao
 and YCP might have similar active regions. Crown Copyright (C) 2009
 Published by Elsevier Masson SAS. All rights reserved.
 SN 0300-9084
 PD APR
 PY 2010
 VL 92
 IS 4
 BP 411
 EP 417
 DI 10.1016/j.biochi.2009.11.003
 UT ISI:000276375100012
 PT J
 AU Lin, H
 Tian, YA
 Zhang, ZJ
 Wu, LL
 Chen, Y
 AF Lin, Hui
 Tian, Yuan
 Zhang, Zunjian
 Wu, Lili
 Chen, Yun
 TI Quantification of piperazine phosphate in human plasma by
 high-performance liquid chromatography-electrospray ionization
 tandem mass spectrometry employing precolumn derivatization with
 dansyl chloride
 SO ANALYTICA CHIMICA ACTA
 AB This paper describes a novel method that combines dansyl chloride
 (DNS-CL) derivatization with high-performance liquid
 chromatography-electrospray ionization tandem mass spectrometry
 (LC-ESI/MS/MS) for the sensitive and selective determination of
 piperazine phosphate in human plasma. After addition of ondansetron
 hydrochloride as internal standard (IS), piperazine phosphate was
 derivatized and then extracted with ethyl acetate. After being
 evaporated and reconstituted, the sample was analyzed using
 LC-ESI/MS/MS. Separation was achieved using an Agilent ZORBAX SB-C-18
 (150 mm x 2.1 mm I.D., 3.5 mu m) column and isocratic elution with 10
 mM ammonium acetate solution (pH 3.0)-methanol (50: 50, v/v). Detection
 was performed on a triple-quadrupole mass spectrometer utilizing
 electrospray ionization (ESI) interface operating in positive ion and
 selected reaction monitoring (SRM) mode with the precursor to product
 ion transitions m/z 320 -> 171 for DNS-CL-piperazine phosphate and m/z
 294 170 for the IS. The method was fully validated for its selectivity,
 sensitivity, linearity, precision, accuracy, recovery, matrix effect
 and stability. The coefficient (r) of piperazine phosphate with a
 linear range of 0.1-15 mu g mL(-1) was 0.9974-0.9995. The limit of
 detection and lower limit of quantification in human plasma were 0.01
 and 0.1 mu g mL(-1), respectively. The validated LC-ESI/MS/MS method
 has been successfully applied to a bioequivalence study of piperazine
 phosphate trochiscus in Chinese healthy male volunteers. (C) 2010
 Elsevier B.V. All rights reserved.
 SN 0003-2670
 PD APR 1
 PY 2010
 VL 664
 IS 1
 BP 40
 EP 48
 DI 10.1016/j.aca.2010.02.003
 UT ISI:000276372700005
 PT J
 AU Chen, YJ
 AF Chen, Yijun
 TI PhD: routine technical work of sequencing is no substitute
 SO NATURE
 SN 0028-0836
 PD APR 8
 PY 2010
 VL 464
 IS 7290
 BP 831
 EP 831
 DI 10.1038/464831a
 UT ISI:000276397300012
 PT J
 AU Wu, L
 Ding, XP
 Zhu, DN
 Yu, BY
 Yan, YQ
 AF Wu, Lei
 Ding, Xiao-Ping
 Zhu, Dan-Ni
 Yu, Bo-Yang
 Yan, Yong-Qing
 TI Study on the radical scavengers in the traditional Chinese medicine
 formula Shengmai San by HPLC-DAD coupled with chemiluminescence (CL)
 and ESI-MS/MS
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 AB Shengmai San (SMS) has been used for the treatment of cardiovascular
 disease in Asia for long-time. It has been reported that SMS can protect
 against oxidative stress and tune immune response in patients. In this
 paper, a high performance liquid chromatography-diode array
 detection-chemiluminescence (HPLC-DAD-CL) method for on-line
 detection was successfully applied to screen antioxidants in complex
 SMS extracts. The H2O2 scavenging activity of every fraction of SMS
 extracts was measured to evaluate each contribution to the total
 anti-oxidative activities of the prescription, followed by structures
 identification of the main active components by LC/MS/MS. HPLC-DAD-CL
 method was also applied for comparing the scavenging rates of main
 active components between the individual herbs and SMS. Interestingly,
 we found that the scavenging activities of main components detected
 in the individual herbs were different from those in SMS. The
 experimental data indicated that drug interactions during decocting
 process could result in the changes of the antioxidants' solubility.
 This study demonstrated that HPLC-DAD-CL on-line assay was a useful
 technique for rapidly screening and identifying bioactive components
 from complex multi-herbal prescription. (C) 2010 Elsevier By. All
 rights reserved.
 SN 0731-7085
 PD AUG 1
 PY 2010
 VL 52
 IS 4
 BP 438
 EP 445
 DI 10.1016/j.jpba.2010.01.021
 UT ISI:000276057300003
 A Liu, WY
 U Li, P
 Feng, F
 Mao, LS
 A Liu, Wenyuan
 F Li, Ping
 Feng, Feng
 Mao, Lishun
 T Isolation and structure characterization of related impurities in
 I 10-O-(N,N-dimethylaminoethyl)-ginkgolide B methanesulfonate (XQ-1H)
 bulk drug and quantitation by a validated RP-LC
 JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 A 10-O-(N,N-dimethylaminoethyl)-ginkgolide B methanesulfonate (XQ-1H),
 B a novel active derivative of ginkgolide B, is a platelet-activating
 factor antagonist which is being under clinical trial. Two unknown
 related impurities were observed in analysis of XQ-1H bulk drug. A
 scaling up preparative liquid chromatography (Prep LC) was used for
 isolation of the two impurities. Based on LC-MS/MS and nuclear magnetic
 resonance (NMR) spectra, they were characterized as
 10-O-(N,N-dimethylaminoethyl)-11,12-seco-ginkgolide B (imp-1)and
 10-O-(N,N-dimethylaminoethyl)-11,12,2,15-diseco-3,14-dehydroginkgo
 lide B (imp-2), respectively. A reversed-phase liquid chromatography
 (RP-LC) was developed for simultaneous determination of XQ-1H as well
 as imp-1 and imp-2. Main variables that significantly influence the
 chromatographic procedure were optimized and efficient
 chromatographic separation was achieved on a CN column with mobile
 phase consisting of 5 mM dipotassium hydrogen phosphate (pH 7.5) and
 methanol delivered in a gradient mode at the flow rate of 1.0 mL min(-1).
 The method was validated and found to be suitable to check the quality
 of bulk samples of XQ-1H at test concentration of 5.0 mg mL(-1) for
 a 20 mu L injection volume. (C) 2010 Elsevier B.V. All rights reserved.
 0731-7085
 AUG 1
 2010
 10.1016/j.jpba.2010.01.019
 ISI:000276057300023
 PT J
 AU Jia, YW
 Xie, HT
 Wang, GJ
 Sun, JG
 Wang, W
 Qing, H
 Wang, X
 Yang, H
 Xu, MJ
 Gu, Y
 Yao, C
 Shen, J
 AF Jia, Yuanwei
 Xie, Haitang
 Wang, Guangji
 Sun, Jianguo
 Wang, Wei
 Qing, Huang
 Wang, Xuan
 Yang, Hao
 Xu, Meijuan
 Gu, Yi
 Yao, Chen
 Shen, Jie
 TI Quantitative determination of helicid in rat biosamples by liquid
 chromatography electrospray ionization mass spectrometry
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB A simple liquid chromatography electrospray ionization mass
 spectrometry (LC-ESI-MS) method with highly improved sensitivities for
 the determination of helicid in rat bile, urine, feces and most tissues
 was developed. The tissues and feces were firstly homogenized
 mechanically using deionized water as the media. Bile, urine, tissues
 and feces homogenates were extracted by liquid-liquid extraction with
 n-butyl alcohol for sample preparation. The subsequent analysis
 procedures were performed on a Shimadzu LCMS2010A system (electrospray
 ionization single quadrupole mass analyzer). A Luna C-18 column (150
 mm x 2.00 mm, 5 mu m) was used as the analytical column, while a mixture
 of acetonitrile and ammonium chloride water solution was used as the
 mobile phase. The proportions of mobile phase were changed timely
 according to gradient programs. Chlorinated adducts of molecular ions
 [M+Cl-] at m/z 319.00 and 363.05 were used to quantify helicid and
 bergeninum (internal standard), respectively. The method was validated
 to be accurate, precise and rugged with good linearity. The proposed
 method was successfully applied to the preclinical tissue distribution
 and excretion studies of helicid in rats. (C) 2010 Elsevier B.V. All
 rights reserved.
 SN 1570-0232
 PD MAR 15
 PY 2010
 VL 878
 IS 9-10
 BP 791
 EP 797
 DI 10.1016/j.jchromb.2010.01.038
 UT ISI:000276125100010
 PT J
 AU Wei-Ze, L
 Mei-Rong, H
 Jian-Ping, Z
 Yong-Qiang, Z
 Bao-Hua, H
 Ting, L
 Yong, Z
 AF Wei-Ze, Li
 Mei-Rong, Huo
 Jian-Ping, Zhou
 Yong-Qiang, Zhou
 Bao-Hua, Hao
 Ting, Liu
 Yong, Zhang
 TI Super-short solid silicon microneedles for transdermal drug delivery
 applications
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB In this study, the super-short microneedles with a length of 70-80 mu
 m were fabricated using silicon wet etching technology. As evident from
 the visual inspection of pierced human skin, appearance of blue spots
 array after Evans Blue (EB) application indicated that the super-short
 microneedles were able to pierce into skin by pressing and swaying
 against the microneedles backing layer continually with a finger. The
 micro-conduits created in skin were validated by histological
 examination.
 Transport studies revealed that: (i) skin pretreated with super-short
 microneedles resulted in a remarkable enhancement of the galanthamine
 (GAL) transport, and the permeated amount increased as the insertion
 force increased; (ii) the super-short microneedles with flat tips were
 better than that with sharp tips for enhancing skin permeability; (iii)
 the longer time of super-short microneedles detained in skin resulted
 in a higher increase of skin permeability; (iv) there was no linear
 correlation between the GAL permeated through skin and the number of
 microneedles. The EIIIA(+) (526 bp) segment, a very sensitive marker
 of tissue injury, did not expressed in the skin pierced by super-short
 microneedles. Meanwhile, the skin pretreated with super-short
 microneedles did not infected after incubation with the Staphylococcus
 aureus. These results suggest that super-short microneedles may be a
 safe and efficient alternative for transdermal drug delivery of
 hydrophilic molecules. (C) 2010 Elsevier B.V. All rights reserved.
 SN 0378-5173
 PD APR 15
 PY 2010
 VL 389
 IS 1-2
 BP 122
 EP 129
 DI 10.1016/j.ijpharm.2010.01.024
 UT ISI:000276219200015
 PT J
 AU Chen, ND
 Zhang, J
 Liu, JH
 Yu, BY
 AF Chen Naidong
 Zhang Jian
 Liu Jihua
 Yu Boyang
 TI Highly Efficient and Regio-selective Glucosylation of 25(S) Ruscogenin
 by Gliocladium deliquescens NRRL1086
 SO CHINESE JOURNAL OF CHEMISTRY
 AB A new steroidal glycoside, 25(S) ruscogenin
 1-O-beta-D-glucopyranoside (2) was obtained through the microbial
 transformation of 25(S) ruscogenin (1) by G. deliquescens NRRL1086 in
 54% isolated yield. The structure of the product was elucidated by IR,
 MS and NMR spectra. This is the first report on the preparation of
 steroidal saponins by microbial transformation.
 SN 1001-604X
 PD MAR
 PY 2010
 VL 28
 IS 3
 BP 439
 EP 442
 UT ISI:000276327400018
 PT J
 AU Wang, XJ
 Lu, N
 Yang, Q
 Dai, QS
 Tao, L
 Guo, XK
 Guo, QL
 You, QD
 AF Wang, Xiaojian
 Lu, Na
 Yang, Qian
 Dai, Qinsheng
 Tao, Lei
 Guo, Xiaoke
 Guo, Qinglong
 You, Qidong
 TI Spectacular modification of Gambogic acid on microwave irradiation in
 methanol: Isolation and structure identification of two products with
 potent anti-tumor activity
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB Treatment of gambogic acid with methanol in acidic condition under
 microwave irradiation led to the formation of two new products bearing
 spectacular A ring systems which were different from reported Garcinia
 natural products. The chemical structures of these two compounds were
 elucidated by extensive NMR and MS spectroscopic analysis as well as
 crystallographic study. Both of the two products could significantly
 inhibit the growth of various tumor cell lines in vitro with IC50 values
 at mu M level through apoptotic pathway. (C) 2010 Elsevier Ltd. All
 rights reserved.
 SN 0960-894X
 PD APR 15
 PY 2010
 VL 20
 IS 8
 BP 2438
 EP 2442
 DI 10.1016/j.bmcl.2010.03.021
 UT ISI:000276291500008
 PT J
 AU Cao, Y
 Chen, JJ
 Tan, NH
 Oberer, L
 Wagner, T
 Wu, YP
 Zeng, GZ
 Yan, H
 Wang, Q
 AF Cao, Yuan
 Chen, Ji-Jun
 Tan, Ning-Hua
 Oberer, Lukas
 Wagner, Trixie
 Wu, Yong-Ping
 Zeng, Guang-Zhi
 Yan, He
 Wang, Qiang
 TI Antimicrobial selaginellin derivatives from Selaginella pulvinata
 SO BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 AB Six selaginellin derivatives, including three new analogues
 selaginellins D-F (1-3), were isolated from the EtOAc extract of the
 whole plant of Selaginella pulvinata (Hook. et Grev.) Maxim. Their
 structures were determined on the basis of extensive physical and
 chemical evidence. Compounds 1 and 4 demonstrated antifungal
 activities against Candida albicans; compounds 4-6 exhibited
 significant antibacterial activity against Staphylococcus aureus. (C)
 2010 Elsevier Ltd. All rights reserved.
 SN 0960-894X
 PD APR 15
 PY 2010
 VL 20
 IS 8
 BP 2456
 EP 2460
 DI 10.1016/j.bmcl.2010.03.016
 UT ISI:000276291500012
 A Gu, P
 U Ding, Y
 Sun, DZ
 Hang, TJ
 Liu, WY
 Ding, L
 A Gu, Ping
 F Ding, Ying
 Sun, Dezhu
 Hang, Taijun
 Liu, Wenying
 Ding, Li
 T Quantification of henatinib maleate, a novel potent inhibitor of VEGF
 I receptors, in rat plasma by LC-MS/MS
 BIOMEDICAL CHROMATOGRAPHY
 A Henatinib maleate
 B (R,Z)-2[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)
 methyl]-5-(2-hydroxy-3morpholinopropy1)-3-methyl-5,6,7,8-tetrahydr
 o-1H-p yrrolo[3,2-0 azepin-4-ketone maleate is a potent inhibitor of
 vascular endothelial growth factor receptors, and is currently under
 preclinical evaluation as an anticancer drug. A novel method for the
 quantification of henatinib maleate in rat plasma using high
 performance liquid chromatography-tandem mass spectrometry has been
 developed. The analyte (henatinib maleate) and internal standard
 (papaverine hydrochloride) were extracted from 50 ta of rat plasma by
 protein precipitation and separated on a C-18 column using a mixture
 of 25 mm ammonium acetate buffer:methanol :acetonitrile (35:50:15,
 v/v/v) as mobile phase with a run time of 4.5 min. The detection was
 performed by means of triple quadrupole mass spectrometer equipped with
 an ESI interface operating in the multiple-reaction monitoring mode.
 A linear response was observed over the concentration range 5.0-1000
 ng/mL. The limit of quantification was 5.0 ng/mL. Both intra- and
 inter-day precision, defined as relative standard deviation, were
 within 9.7%. Accuracy, defined as relative error, was within 3.1%. The
 developed method was successfully applied to preclinical
 pharmacokinetic studies of henatinib maleate in rat after a single oral
 administration of the drug. Copyright (C) 2009 John Wiley & Sons, Ltd.
 0269-3879
 2010
 10.1002/bmc.1308
 ISI:000276169100012
 PT J
 AU Hu, YM
 Su, GH
 Sze, SCW
 Ye, WC
 Tong, Y
 AF Hu, Yong Mei
 Su, Guang Hai
 Sze, Stephen Cho-Wing
 Ye, Wencai
 Tong, Yao
 TI Quality assessment of Cortex Phellodendri by high-performance liquid
 chromatography coupled with electrospray ionization mass spectrometry
 SO BIOMEDICAL CHROMATOGRAPHY
 AB A simple method based on liquid chromatography coupled with diode array
 detection and electrospray ionization mass spectrometry
 (LC-DAD-ESI-MS) was developed for the quality assessment of Cortex
 Phellodendri (CP), which was mainly derived from two species of
 Phellodendron chinense Schneid and Phellodendron amurense Rupr. Total
 41 compounds, including 14 phenols, 24 alkaloids and three liminoidal
 triterpenes were identified or tentatively characterized from the 75%
 methanol extract of CP samples by online ESI-MSn fragmentation and UV
 spectra analysis. Among them, two phenols and six alkaloids were
 simultaneously quantified using HPLC-DAD method. The validated
 HPLC-DAD method showed a good linearity, precision, repeatability and
 accuracy for the quantification of eight marker compounds.
 Furthermore, the plausible fragmentation pathway of the representative
 compounds were proposed in the present study. The differences of the
 chemical constituents content and the comprehensive HPLC profiles
 between the two CP species using LC-DAD-ESI-MS method are reported for
 the first time, indicating that the CP drugs from different resources
 should be used separately in the clinic. Copyright (C) 2009 John Wiley
 & Sons, Ltd.
 SN 0269-3879
 PD APR
 PY 2010
 VL 24
 IS 4
 BP 438
 EP 453
 DI 10.1002/bmc.1311
 UT ISI:000276169100015
 PT J
 AU Zhang, HM
 Wang, W
 Jiang, ZZ
 Shang, J
 Zhang, LY
 AF Zhang, Hongmei
 Wang, Wei
 Jiang, Zhenzhou
 Shang, Jing
 Zhang, Luyong
 TI Differential involvement of 5-HT1A and 5-HT1B/1D receptors in human
 interferon-alpha-induced immobility in the mouse forced swimming test
 SO ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
 AB Although Interferon-alpha (IFN-alpha, CAS 9008-11-1) is a powerful
 drug in treating several viral infections and certain tumors, a
 considerable amount of neuropsychiatric side-effects such as
 depression and anxiety are an unavoidable consequence. Combination
 with the selective serotonin (5-HT) reuptake inhibitor (SSRI)
 fluoxetine (CAS 56296-78-7) significantly improved the situation.
 However, the potential 5-HT1A receptor- and 5-HT1B receptor-signals
 involved in the antidepressant effects are still unclear. The effects
 of 5-HT1A receptor- and 5-HT1B receptor signals were analyzed by using
 the mouse forced swimming test (FST), a predictive test of
 antidepressant-like action. The present results indicated that (1)
 fluoxetine (administrated intragastrically, 30 mg/kg; not subactive
 dose: 15 mg/kg) significantly reduced IFN-alpha-induced increase of
 the immobility time in the forced swimming test; (2) 5-HT1A receptorand 5-HT1B receptor ligands alone or in combination had no effects on
 IFN-alpha-induced increase of the immobility time in the FST; (3)
 surprisingly, WAY 100635 (5-HT1A receptor antagonist, 634908-75-1) and
 8-OH-DPAT(5-HT1A receptor agonist, CAS 78950-78-4) markedly enhanced
 the antidepressant effect of fluoxetine at the subactive dose (15
 mg/kg, i.g.) on the IFN-alpha-treated mice in the FST. Further
 investigations showed that fluoxetine combined with WAY 100635 and
 8-OH-DPAT failed to produce antidepressant effects in the FST. (4)
 Co-application of CGS 12066A (5-HT1B receptor agonist, CAS
 109028-09-3) or GR 127935 (5-HT1B/1D receptor antagonist, CAS
 148642-42-6) with fluoxetine had no synergistic effects on the
 IFN-alpha-induced increase of immobility time in FST. (5)
 Interestingly, co-administration of GR 127935, WAY 100635 and
 fluoxetine significantly reduced the IFN-alpha-induced increase in
 immobility time of FST, being more effective than co-administration
 of WAY 100635 and fluoxetine. All results suggest that (1) compared
 to the 5-HT1B receptor, the 5-HT1A receptor signal plays the dominant
 role in improving the anti-immobility effect of fluoxetine in the
 IFN-alpha-induced depression; (2) combination of the 5-HT(1)A
 antagonist with subactive fluoxetine can be helpful in
 IFN-alpha-induced depression treatment.
 SN 0004-4172
 PY 2010
 VL 60
 IS 3
 BP 109
 EP 115
 UT ISI:000276272600001
 PT J
 AU Lin, H
 Tian, Y
 Tian, JX
 Zhang, ZJ
 Mao, GG
 AF Lin, Hui
 Tian, Yuan
 Tian, Ji-Xin
 Zhang, Zun-Jian
 Mao, Guo-Guang
 TI Pharmacokinetics and bioequivalence study of valacyclovir
 hydrochloride capsules after single dose administration in healthy
 Chinese male volunteers
 SO ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
 AB The aim of the present study was to compare the bioavailability of
 valacyclovir (CAS 124832-26-4; INN: valaciclovir) from two
 valacyclovir hydrochloride (CAS 214832-27-5) capsules (150 mg/capsule
 as test preparation and 150 mg/capsule commerciallty available
 original capsule of the drug as reference preparation) in 20 Chinese
 healthy male volunteers, aged between 20 and 27. The study was conducted
 according to an open randomized, single blind, 2-way crossover study
 design with a wash-out phase of 7 days. Blood samples for
 pharmacokinetic profiling were taken up to 24 h post-dose. Valacyclovir
 hydrochloride is rapidly converted to acyclovir (CAS 59277-89-3) after
 oral administration, so the pharmacokinetcis and bioequivalence of
 valacyclovir hydrochloride can be studied by determining the plasma
 concnetratio of acyclovir. Plasma concentrations of acyclovir were
 determined witha validated liquid chromatography, tandem mass
 spectrometry (LC-MS/MS) method. The pharmacokinetic parameters of test
 and reference formulations were estimated as follows: the maximum
 plasma concentrations (C-max) were 2.04 +/- 0.43 mu g mL and 2.01 +/0.50 mu g/mL; the median T-max were 1.1 +/- 0.3 h and 1.0 +/- 0.3 h;
 plasma elimination half-lives (t(1/2)) were 2.94 +/- 0.42 h and 2.85
 +/- 0.28 h Values of AUC(0-t) demonstrate nearly identical
 bioavailability of valacyclovir hydrochloride from the examined
 formulations. AUC(0-15) were 6.70 +/- 1.26 mu g.h/mL and 6.96 +/- 1.25
 g.h/mL. Areas under the plasma concentration-time curve
 (AUC(0-infinity)) were 6.90 +/- 1.36 mu g.h/ml and 7.15 +/- 1.31 mu
 g.h/mL. Both primary target parameters , AUC(0-infinity) and AUC(0-t)
 wre tested parametrically by analysis of variaance (ANOVA) and relative
 bioavailabilities were 96.69 7.89% for AUC(0-infinity) , 96.40 8.0%
 for AUC(0-15). Bioequivalence between test and reference preparation
 was demonstated fro both parameters AUC(0-infinity) and AUC(0-t). The
 90% confidence intervals of the T/R-ratios of logarithmically
 transformed data were in the generally accepted range of 80-125%. It
 meant that the test formualtion was bioequivalnet to the reference
 formulation for valacyclovir hydrochloride.
 SN 0004-4172
 PY 2010
 VL 60
 IS 3
 BP 162
 EP 167
 UT ISI:000276272600009
 PT J
 AU Wang, ZH
 Wang, T
 Yao, SN
 Chen, JC
 Hua, WY
 Yao, QZ
 AF Wang, Zhao-Hui
 Wang, Tao
 Yao, Shi-Ning
 Chen, Jing-cai
 Hua, Wei-Yi
 Yao, Qi-Zheng
 TI Synthesis and Biological Evaluation of 7-Azaisoindigo Derivatives
 SO ARCHIV DER PHARMAZIE
 AB A series of novel 7-azaisoindigo derivatives 3-14 were designed,
 synthesized, and structurally characterized by IR, H-1-NMR, C-13-NMR,
 mass spectra, and elemental analyses. Their antiproliferative
 activities were evaluated in a hormone-independent prostate cancer
 cell line DU145. Among them, compounds 8, 9, 14 showed the highest
 activities. Our study also showed that compounds 7, 11, 12 exhibited
 higher inhibitory activities on CDK2/cyclin A than that of the positive
 control meisoindigo. Western blot analysis on DU145 cells treated with
 compounds 7 and 9 demonstrated that 7-azaisoindigo derivatives could
 decrease the level of CDK2 activity (phosphorylation) and the
 expression of cyclin D1, and increase the expression of endogenous
 cyclin-dependent inhibitor p27.
 SN 0365-6233
 PD MAR
 PY 2010
 VL 343
 IS 3
 BP 160
 EP 166
 DI 10.1002/ardp.200900268
 UT ISI:000276274500004
 PT J
 AU Gao, MM
 Tian, H
 Ma, C
 Gao, XD
 Guo, W
 Yao, WB
 AF Gao, Mingming
 Tian, Hong
 Ma, Chen
 Gao, Xiangdong
 Guo, Wei
 Yao, Wenbing
 TI Expression, Purification, and C-terminal Site-Specific PEGylation of
 Cysteine-Mutated Glucagon-Like Peptide-1
 SO APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY
 AB Glucagon-like peptide-1 (GLP-1) is attracting increasing interest on
 account of its prominent benefits in type 2 diabetes. However, its
 clinical application is limited because of short biological half-life.
 This study was designed to produce a C-terminal site-specific PEGylated
 analog of cysteine-mutated GLP-1 (cGLP-1) to prolong its action. The
 gene of cGLP-1 was inserted into pET32a to construct a thioredoxinA
 fusion protein. After expression in BL21 (DE3) strain, the fusion
 protein was purified with Ni-affinity chromatography and then was
 PEGylated with methoxy-polyethylene glycol-maleimide
 (mPEG(10K)-MAL). The PEGylated fusion protein was purified with anion
 exchange chromatography and then was cleaved by enterokinase. The
 digested product was further purified with reverse-phase
 chromatography. Finally, 8.7 mg mPEG(10K)-cGLP-1 with a purity of up
 to 98% was obtained from the original 500 ml culture. The circular
 dichroism spectra indicated that mPEG(10K)-cGLP-1 maintained the
 secondary structure of native GLP-1. As compared with that of native
 GLP-1, the plasma glucose lowering activity of mPEG(10K)-cGLP-1 was
 significantly extended. These results suggest that our method will be
 useful in obtaining a large quantity of mPEG(10K)-cGLP-1 for further
 study and mPEG(10K)-cGLP-1 might find a role in the therapy of type
 2 diabetes through C-terminal site-specific PEGylation.
 SN 0273-2289
 PD SEP
 PY 2010
 VL 162
 IS 1
 BP 155
 EP 165
 DI 10.1007/s12010-009-8725-6
 UT ISI:000276252600015
 PT J
 AU Ding, CY
 Tu, SH
 Yao, QZ
 Li, FL
 Wang, YX
 Hu, WX
 Zhang, A
 AF Ding, Chunyong
 Tu, Shanghui
 Yao, Qizheng
 Li, Fulong
 Wang, Yuanxiang
 Hu, Wenxiang
 Zhang, Ao
 TI One-Pot Three-Step Synthesis of Naphtho[2,3-a]carbazole-5,13-diones
 using a Tandem Radical Alkylation-Cyclization-Aromatization Reaction
 Sequence
 SO ADVANCED SYNTHESIS & CATALYSIS
 AB A three-step, one-pot tandem reaction including radical nucleophilic
 alkylation/cyclization/aromatization was developed using 0.3
 equivalents of silver(I) acetate (AgOAc) as the catalyst and 2
 equivalents of ammonium persulfate as the oxidant. This strategy is
 highly efficient for the assembly of pentacyclic complex carbazoles
 from aryl-fused bromobenzoquinones and indol-3-ylpropanoic acid acids
 in 52-72% overall yields (three steps). This new approach provides a
 significant improvement over the previously reported methods and would
 greatly facilitate analog library construction of pentacyclic complex
 carbazoles and benefit further biological evaluation of these
 compounds.
 SN 1615-4150
 PD MAR
 PY 2010
 VL 352
 IS 5
 BP 847
 EP 853
 DI 10.1002/adsc.200900789
 UT ISI:000276317800007
 PT J
 AU Song, JN
 Liu, K
 Yi, JL
 Zhu, DQ
 Liu, GL
 Liu, BL
 AF Song, Junna
 Liu, Kang
 Yi, Jiali
 Zhu, Deqiu
 Liu, Gaolin
 Liu, Baolin
 TI Luteolin Inhibits Lysophosphatidylcholine-Induced Apoptosis in
 Endothelial Cells by a Calcium/Mithocondrion/Caspases-Dependent
 Pathway
 SO PLANTA MEDICA
 CT 9th Annual Oxford International Conference on Science of Botanicals
 CY APR 12-15, 2010
 CL Oxford, MS
 HO Univ Mississippi
 AB Luteolin, a naturally occurring polyphenol flavonoid, has demonstrated
 some beneficial modulation toward the endothelium. This study aims to
 investigate the effects of luteolin on lysophosphatidylcholine
 (LPC)-induced apoptosis, a key event in the pathogenesis of
 atherosclerosis, in endothelial cells. Luteolin reduced not only
 LPC-induced cell death but also lactate dehydrogenase (LDH) leakage.
 Luteolin inhibition of LPC-induced apoptosis in endothelial cells
 demonstrated its protection against the cytotoxicity of LPC.
 LPC-induced apoptosis is characterized by a calcium-dependent
 mitochondrial pathway, involving calcium influx, activation of
 calpains, cytochrome C release and caspases activation. Luteolin
 reduced calcium influx. It also inhibited calpains activation and
 prevented the release of cytochrome C from mitochondrion. The
 inhibition of cytochrome C release by luteolin blocked the activation
 of caspase-3 and thus prevented subsequent endothelial cell apoptosis.
 These results suggested that luteolin inhibits LPC-induced apoptosis
 in endothelial cells through the blockage of the calcium-dependent
 mitochondrial pathway.
 SN 0032-0943
 PD MAR
 PY 2010
 VL 76
 IS 5
 BP 433
 EP 438
 DI 10.1055/s-0029-1186197
 UT ISI:000275939800005
 PT J
 AU Qian, H
 Chen, W
 Zhang, XY
 Zhang, HB
 Zhou, JP
 Huang, WL
 Jin, J
 Dai, DY
 AF Qian, Hai
 Chen, Wei
 Zhang, Xiaoyan
 Zhang, Huibin
 Zhou, Jinpei
 Huang, Wenlong
 Jin, Jing
 Dai, Dongyan
 TI Synthesis and Biological Evaluation of
 Dihydroisoquinoline-2(1H)-Carbothioamide Derivatives as TRPV1
 Antagonists
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB TRPV1 receptor is an important analgesia target. Its antagonists are
 expected to prevent pain perception by blocking the receptor directly.
 In this letter, eight dihydroisoquinoline-2(1H)-carbothioamide
 derivatives were designed and synthesized as TRPV1 antagonists. The
 benzene ring was modified with different substitutional groups.
 Preliminary biological tests suggested that the new compounds
 exhibited TRPV1 antagonist activity and different analgesia effects,
 some of which were promising as analgesia drugs.
 SN 1570-1808
 PD MAY
 PY 2010
 VL 7
 IS 4
 BP 235
 EP 237
 UT ISI:000275929300002
 PT J
 AU Li, YT
 Zhang, JM
 Li, HW
 Hu, YZ
 Wei, Y
 AF Li, Yanting
 Zhang, Jianmin
 Li, Huiwan
 Hu, Yuzhu
 Wei, Yu
 TI Highly Stable Dispersibility in Water Induced by Surface Hydration
 Force of TiO2 Nanocrystalline Mixtures During Phase Transformation
 SO JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY
 AB Titania (TiO2) nanoparticles were prepared by the alcohothermal method
 using tetra-n-butyl titanate [Ti(OC4H9n)(4)] as a precursor. The phase
 transformation from anatase to rutile happened when the nanoparticles
 were calcined at 800 degrees C and 900 degrees C in an oven,
 respectively. TiO2 nanocrystalline mixtures had the highly stable
 dispersibility when they were dispersed in water medium. The zeta
 potentials of the different TiO2 nanoparticles showed that the surface
 electrostatic forces were not crucial factors in such stable
 dispersibility. Other characterizations, including x-ray diffraction
 (XRD) and Fourier-transform infrared spectroscopy (FT-IR), indicated
 that the phase transformation was favor of the adsorption of water on
 TiO2 surface. A visual model was presented to illustrate that the strong
 repulsive surface hydration force prevented TiO2 nanoparticles from
 aggregation.
 SN 0193-2691
 PY 2010
 VL 31
 IS 2
 BP 260
 EP 263
 DI 10.1080/01932690903119716
 UT ISI:000275860400015
 PT J
 AU Yuan, DC
 Ju, CY
 Ding, S
 Jing, X
 Zhang, C
 AF Yuan, Dechuang
 Ju, Caoyun
 Ding, Song
 Jing, Xiang
 Zhang, Can
 TI Synthesis of 1-Octadecanol-Modified Water-Swelling Polyurethane
 Hydrogels as Vaginal Drug-Delivery Vehicle
 SO JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
 AB The purpose of this work was to develop a novel polyurethane hydrogel
 system for sustained drug release, which could be used as a vaginal
 drug-delivery vehicle. The blank polyurethane hydrogels were
 synthesized by a polyol oligomeric, a diisocyanate and a triol (used
 as cross-linking agent). In order to improve the swelling ability of
 a polyurethane hydrogel, a small amount of 1-octadecanol was added.
 Additionally, the structure, mechanical properties and thermal
 properties of polymers were assessed by FT-IR, WAXD, DSC and mechanical
 tests. The results show that no more than 2.5 wt% of 1-octadecanol
 additives is sufficient to affect the release profile without changing
 the structure and mechanical properties of the polyurethane hydrogels
 obviously. Tinidazole was chosen as a model drug, the release data of
 drug from polyurethane hydrogels were fitted using the Ritger-Peppas
 equation and the result showed that it was non-Fickian diffusion, which
 means that the drug release was controlled by both swollen control and
 diffusion control. In conclusion, our work proves that the synthesized
 polyurethane hydrogel modified by 1-octadecanol may be a promising
 sustained release drug carrier. (C) Koninklijke Brill NV, Leiden, 2010
 SN 0920-5063
 PY 2010
 VL 21
 IS 4
 BP 493
 EP 505
 DI 10.1163/156856209X427032
 UT ISI:000275981600006
 PT J
 AU Qi, LW
 Liu, EH
 Chu, C
 Peng, YB
 Cai, HX
 Li, P
 AF Qi, Lian-Wen
 Liu, E-Hu
 Chu, Chu
 Peng, Yong-Bo
 Cai, Hai-Xia
 Li, Ping
 TI Anti-Diabetic Agents from Natural Products-An Update from 2004 to 2009
 SO CURRENT TOPICS IN MEDICINAL CHEMISTRY
 AB Diabetes mellitus (DM), the third killer of the mankind health along
 with cancer, cardiovascular and cerebrovascular diseases, is one of
 the most challenging diseases facing health care professionals today.
 The World Health Organization (WHO) has declared that a DM epidemic
 is underway. Primary DM and its complications are costly to manage,
 not only for affected individuals, but also for healthcare systems
 around the world. Screening of anti-diabetic agents has been
 extensively investigated in the past decades. Natural products (NPs)
 have served as a major source of drugs for centuries, and about half
 of the pharmaceuticals in use today are derived from natural
 substances. Many natural products especially plants-derived medicines
 have been recommended for the treatment of DM. The present paper reviews
 NPs appeared in the literature with potential for DM and also identifies
 the research needs in this area. It mainly covers the time period from
 January 2004 to June 2009. The current review is divided into three
 major sections based on classification of the natural materials
 involved. The first part focuses on known and some new chemical entities
 isolated mainly from medicinal plants possessing anti-diabetic
 properties, including saponins, flavonoids, alkaloids,
 anthraquinones, terpenes, coumarins, phenolics, polysaccharides, and
 some other compounds. The second part summarizes crude extract of
 medicinal plants which are commonly used in the traditional Chinese
 medical system and have been demonstrated experimental or/and clinical
 anti-diabetic effectiveness, mainly including Leguminosae,
 Cucurbitaceae, Araliaceae, Liliaceae, Chenopodiaceae, Solanaceae,
 Compositae, Campanulaceae, Cornaceae, Rhamnaceae, Scrophulariaceae,
 Euphorbiaceae, Ginkgoceae, Gramineae, Myrtaceae, Sterculiaceae,
 Annonaceae, Labiatae, Crassulaceae, and Miscellaneous. The third part
 lists some compound formulae consisting of extracts of several plants
 that have been reported as beneficial for the treatment of DM, major
 involving Xiaokeling tablet, Huang-Lian-Jie-Du-Decoction,
 Ba-Wei-Di-Huang-Wan and Formula 1.
 SN 1568-0266
 PD MAR
 PY 2010
 VL 10
 IS 4
 BP 434
 EP 457
 UT ISI:000275929700006
 PT J
 AU Cheng, KG
 Liu, J
 Sun, HB
 Xie, J
 AF Cheng, Keguang
 Liu, Jun
 Sun, Hongbin
 Xie, Juan
 TI Synthesis of Oleanolic Acid Dimers as Inhibitors of Glycogen
 Phosphorylase
 SO CHEMISTRY & BIODIVERSITY
 AB Recently, oleanolic acid was found to be an inhibitor of glycogen
 phosphorylase. For further structural modification, we have
 synthesized several dimers of oleanolic acid by using amide, ester,
 or triazole linkage with click chemistry. The click chemistry was shown
 to be the most efficient method for the dimer synthesis. Nearly
 quantitative yield of triazole-linked dimers was obtained. Biological
 evaluation of the synthesized dimers as inhibitors of glycogen
 phosphorylase has been described. Four of six dimers exhibited
 inhibitory activity against rabbit muscle glycogen phosphorylase a
 (RMGPa), with compounds 2 and 7 as the most potent inhibitors, which
 displayed an IC50 value (ca. 3 mu M) lower than that of oleanolic acid
 (IC50=14 mu M).
 SN 1612-1872
 PY 2010
 VL 7
 IS 3
 BP 690
 EP 697
 UT ISI:000276059600014
 PT J
 AU Jing, XY
 Liu, X
 Wen, T
 Xie, SS
 Yao, D
 Liu, XD
 Wang, GJ
 Xie, L
 AF Jing, Xinyue
 Liu, Xiang
 Wen, Tao
 Xie, Shanshan
 Yao, Dan
 Liu, Xiaodong
 Wang, Guangji
 Xie, Lin
 TI Combined effects of epileptic seizure and phenobarbital induced
 overexpression of P-glycoprotein in brain of chemically kindled rats
 SO BRITISH JOURNAL OF PHARMACOLOGY
 AB Background and purpose:
 The multidrug resistance of epilepsy may result from the overexpression
 of P-glycoprotein, but the mechanisms are unclear. We investigated
 whether the overexpression of P-glycoprotein in the brains of subjects
 with pharmacoresistant epilepsy resulted from both drug effects and
 seizure activity.
 Experimental approach:
 Kindled rats were developed by injecting a subconvulsive dose of
 pentylenetetrazole (33 mg center dot kg-1 center dot day-1, i.p.) for
 28 days. Groups were then treated with an oral dose of phenobarbital
 (45 mg center dot kg-1 center dot day-1) for 40 days. In accord with
 behavioural observations, P-glycoprotein activity in brain was
 assessed using brain-to-plasma concentration ratios of rhodamine 123.
 P-glycoprotein levels in the brain regions were further evaluated using
 RT-PCR and Western blot analysis. The distribution of phenobarbital
 in the brain was assessed by measuring phenobarbital concentrations
 1 h following its oral administration.
 Key results:
 The kindling significantly increased P-glycoprotein activity and
 expression. Good associations were found among P-glycoprotein
 activity, expression and phenobarbital concentration in the
 hippocampus. Short-term treatment with phenobarbital showed good
 anti-epileptic effect; the maximum effect occurred on day 14 when
 overexpression of P-glycoprotein was reversed. Continuous treatment
 with phenobarbital had a gradually reduced anti-epileptic effect and
 on day 40, phenobarbital exhibited no anti-epileptic effect; this was
 accompanied by both a re-enhancement of P-glycoprotein expression and
 decreased phenobarbital concentration in the hippocampus.
 P-glycoprotein function and expression were also increased in
 age-matched normal rats treated with phenobarbital.
 Conclusions and implications:
 The overexpression of P-glycoprotein in the brain of subjects with
 pharmacoresistant epilepsy is due to a combination of drug effects and
 epileptic seizures.
 SN 0007-1188
 PD APR
 PY 2010
 VL 159
 IS 7
 BP 1511
 EP 1522
 DI 10.1111/j.1476-5381.2009.00634.x
 UT ISI:000275873700014
 PT J
 AU Yang, LM
 Ge, WH
 Yu, F
 Zhu, HJ
 AF Yang, Limei
 Ge, Weihong
 Yu, Feng
 Zhu, Huaijun
 TI Impact of VKORC1 gene polymorphism on interindividual and interethnic
 warfarin dosage requirement- A systematic review and meta analysis
 SO THROMBOSIS RESEARCH
 AB Introduction: Warfarin is the most widely used oral anticoagulant. It
 has been suggested that anticoagulation effect of warfarin is
 significantly associated with the polymorphism of certain genes,
 including Cytochrome P450 complex subunit 2C9 (CYP2C9), Vitamin K
 Epoxide Reductase Complex Subunit 1 (VKORC1), Gamma-Glutamyl
 Carboxylase (GGCX) and Apolipoprotein E (APOE) etc. The purpose of the
 present study was to conduct a systemic review and meta-analysis to
 investigate the relationship between mean daily warfarin dose (MDWD)
 and VKORC1 single nucleotide polymorphisms (SNPs).
 Materials and Methods: Inclusion and exclusion criteria were made, and
 the studies between 2004 and present were searched. References were
 examined, and experts were consulted for additional information. Data
 were extracted. Revman 4.2.10 software was applied to analyze the
 relationship between MDWD and VKORC1 SNPs.
 Results: Total 19 studies were included in the meta-analysis. The
 frequencies of 1173TT and -1639 AA in Asian patients were higher than
 those in Caucasian and African populations. Patients with VKORC1 1173
 CT and 1173 CC required 44% [95% Confidence Interval (CI); 32%, 56%]
 and 97% [73%, 122%] higher MDWD than 1173 TT carriers, -1639GA and
 -1639GG carriers required 52% [41%, 64%] and 102% [85%, 118%] higher
 MDWD than -1639AA carriers, 3730GA and 3730AA carriers required 27%
 [3%, 58%] and 52% [3%, 109%] higher MDWD than 3730GG carriers. In
 addition, 1173C, -1639 G and 3730 A carriers required 63% [44%, 82%],
 61% [49%, 73%] and 32% [4%, 59%] higher MDWD than 1173TT, -1639 AA and
 3730GG, respectively. Sensitive analyses demonstrated that the impacts
 of gene polymorphism on warfarin dosage requirement were significantly
 different between Caucasian and Asian population, and the results of
 meta-analyses were stable and reliable.
 Conclusion: This is the first meta-analysis about the impact of VKORC1
 gene polymorphism on warfarin dose requirement. Our studies showed that
 gene polymorphisms of VKORC1 significantly associated with the
 variation of interindividual warfarin dose requirement variation, and
 the effects are different in ethnicities. (C) 2009 Elsevier Ltd. All
 rights reserved.
 SN 0049-3848
 PD APR
 PY 2010
 VL 125
 IS 4
 BP E159
 EP E166
 DI 10.1016/j.thromres.2009.10.017
 UT ISI:000275786000027
 PT J
 AU Su, CH
 Ji, H
 Su, YX
 AF Su, Changhai
 Ji, Hui
 Su, Yixin
 TI Hospital pharmacists' knowledge and opinions regarding adverse drug
 reaction reporting in Northern China
 SO PHARMACOEPIDEMIOLOGY AND DRUG SAFETY
 AB Purpose This study was designed to investigate the knowledge and
 opinions of hospital pharmacists about the spontaneous reporting of
 adverse drug reactions (ADRs) in Inner Mongolia, a nor-them region of
 China.
 Methods A face-to-face questionnaire survey of hospital pharmacists
 was conducted in five tertiary general hospitals in Inner Mongolia
 between July and December 2007. The structured questionnaire consisted
 of questions about the demographic details of the pharmacists, their
 knowledge of pharmacovigilance and their opinions on pharmacists'
 involvement in ADR reporting.
 Results Of the 288 pharmacists visited, 246 responded giving a total
 response rate of 85.4%. An amount of 70% of the pharmacists could define
 ADR correctly and 78.0% knew how to report ADRs. However, only one-third
 were clear as to what should be reported. The majority of pharmacists
 (92.7%) considered ADR reporting to be a professional obligation.
 However, only 36 (14.6%) claimed to have reported an ADR in their
 career, 25 of these 36 pharmacists (69.4%) were clinical pharmacists.
 Younger pharmacists and those who had received ADR training were more
 likely to report an ADR. The three major reasons for not reporting were:
 uncertain association (81.9%), insufficient clinical knowledge
 (68.6%) and lack of time (45.7%). The most frequently mentioned
 suggestion for improvement included more education on ADR reporting
 (66.7%), participation in ward rounds (43.9%) and encouragement from
 the pharmacy department (32.9%).
 Conclusion Our investigation showed hospital pharmacists in it
 northern region of China had a reasonable knowledge of and positive
 attitudes towards pharmacovigilance. However, the majority of
 pharmacists had never reported an ADR in their career. Pharmacists'
 ADR education and increasing involvement in patient care would be
 important in improving ADR reporting in hospitals. Copyright (C) 2009
 John Wiley & Sons, Ltd.
 SN 1053-8569
 PD MAR
 PY 2010
 VL 19
 IS 3
 BP 217
 EP 222
 DI 10.1002/pds.1792
 UT ISI:000275693700001
 PT J
 AU Zhao, XQ
 Li, F
 Zhuang, WP
 Xue, XW
 Lian, YY
 Fan, JH
 Fang, DS
 AF Zhao, Xueqing
 Li, Fei
 Zhuang, Weiping
 Xue, Xiaowen
 Lian, Yuanyang
 Fan, Jianhui
 Fang, Dongsheng
 TI A New Method for Synthesis of Nolatrexed Dihydrochloride
 SO ORGANIC PROCESS RESEARCH & DEVELOPMENT
 AB A new synthetic method for nolatrexed dihydrochloride (thymitaq) has
 been developed. The synthesis was accomplished in three steps featuring
 the direct conversion of the starting 4-bromo-5-methylisatin into the
 methyl anthranilate by potassium peroxydisulfate/sodium methoxide. In
 the final Ullmann reaction potassium carbonate was employed in place
 of sodium hydride, and the amount of copper catalysts was significantly
 reduced. Moreover, sodium sulfide solution was utilized to efficiently
 remove copper under approximately neutral conditions instead of
 hydrogen sulfide/methanol under strongly acidic conditions. By means
 of these modifications, nolatrexed dihydrochloride was ensured to be
 prepared in good yield and high purity.
 SN 1083-6160
 PD MAR-APR
 PY 2010
 VL 14
 IS 2
 BP 346
 EP 350
 DI 10.1021/op9002517
 UT ISI:000275711900005
 PT J
 AU Xu, XX
 Dai, Y
 AF Xu, Xianxiang
 Dai, Yue
 TI Heparin: an intervenor in cell communication
 SO JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
 AB Introduction
 Effects of heparin beyond anticoagulant
 Non-anticoagulant heparins
 Cells adhere to communicate
 Anti-adhesion activity of heparin
 Heparin and cell adhesion molecules
 Heparin binds to messengers in cell communication
 What makes cells sticky?
 Heparin and heparanase
 Conclusion
 It was nearly 100 years since heparin was discovered, but the role of
 this widely used anticoagulant is still remarkably thought provoking
 now. During pathological processes such as atherosclerosis,
 inflammation, cancer and infection, phenomena of cell adhesion are
 ubiquitous and complicated. Heparin exerts anti-adhesion activity
 appearing as a common mechanism of its potential polypharmacology in
 those diseases. Furthermore, heparin can bind a variety of signalling
 molecules such as growth factors, cell surface proteins of pathogens
 and most notably, cell adhesion molecules. These signalling molecules
 are involved in cell communication, acting as ligands, receptors and
 second messengers. Considering that heparan sulphate
 glycosaminoglycan is increasingly recognized as a key mediator in many
 cellular processes, the structural similarity with heparan sulphate
 suggests that heparin is a multifunctional intervenor in cell
 communication.
 SN 1582-1838
 PD JAN-FEB
 PY 2010
 VL 14
 IS 1-2
 BP 175
 EP 180
 DI 10.1111/j.1582-4934.2009.00871.x
 UT ISI:000275639700015
 PT J
 AU Gao, Y
 Lu, N
 Ling, Y
 Chen, Y
 Wang, L
 Zhao, Q
 Qi, Q
 Liu, W
 Zhang, HW
 You, QD
 Guo, QL
 AF Gao, Ying
 Lu, Na
 Ling, Yun
 Chen, Yan
 Wang, Ling
 Zhao, Qing
 Qi, Qi
 Liu, Wei
 Zhang, Haiwei
 You, Qidong
 Guo, Qinglong
 TI Oroxylin A inhibits angiogenesis through blocking vascular endothelial
 growth factor-induced KDR/Flk-1 phosphorylation
 SO JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
 AB In this study, we examined the antiangiogenic effect of oroxylin A in
 vitro and in vivo and explored the potential mechanisms for this effect.
 Transwell assay and tube formation assay were used to evaluate the
 effects of oroxylin A on vascular endothelial growth factor
 (VEGF)-induced migration and tube formation of human umbilical vein
 endothelial cells (HUVECs). Rat aortic ring assay was also employed
 to assess the effect of oroxylin A on microvessel outgrowth from rat
 aorta. Human tumor xenografts model in nude mice was further used to
 investigate the antiangiogenic activity of oroxylin A in vivo. Western
 blot analysis was used to investigate the related mechanism.
 Oroxylin A remarkably suppressed the VEGF-stimulated migration and
 tube formation of HUVECs. It also inhibited microvessel sprouting from
 rat aortic ring in vitro. In addition, it suppressed the angiogenesis
 of xenograft tumor in nude mice, which concurred with the inhibition
 of tumor growth. Moreover, oroxylin A blocked VEGF-induced
 phosphorylation of KDR/Flk-1 and related downstream signaling
 molecules, including p38 mitogen-activated protein kinase,
 extracellular signal-regulated kinase and Akt.
 Oroxylin A possessed antiangiogenic activities in vitro and in vivo,
 which could be an underlying mechanism of its anticancer effect.
 SN 0171-5216
 PD MAY
 PY 2010
 VL 136
 IS 5
 BP 667
 EP 675
 DI 10.1007/s00432-009-0705-2
 UT ISI:000275754200004
 PT J
 AU Liu, W
 Wang, HY
 Yao, WB
 Gao, XD
 Yu, LL
 AF Liu, Wei
 Wang, Hengyu
 Yao, Wenbing
 Gao, Xiangdong
 Yu, Liangli (Lucy)
 TI Effects of Sulfation on the Physicochemical and Functional Properties
 of a Water-Insoluble Polysaccharide Preparation from Ganoderma lucidum
 SO JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
 AB The sulfation of a water-insoluble Ganoderma lucidum polysaccharide
 (GLP) was successfully carried out with chlorosulfonic acid-pyridine
 in dimethyl formamide to prepare three sulfated GLP derivatives, named
 sGLP1, sGLP2, and sGLP3. The chemical structure of the sulfated GLIP
 was confirmed by Fourier transform infrared and C-13 NMR analyses. The
 sGLPs were evaluated for their water solubility, degree of substitution
 (DS), antioxidant properties, and bile acid-binding capacities. The
 results showed that sulfation improved the water solubility of GLP and
 increased its scavenging capacities against hydroxyl and superoxide
 anion radicals, hydrogen peroxide-scavenging activity, Fe(II)
 chelating ability, reducing power, and bile acid-binding capacities.
 It was also observed that the DS may influence the physicochemical and
 functional properties of sGLPs. For instance, the sulfated GLP with
 the lowest DS had the greatest bile acid-binding capacity, and the sGLP
 that had the highest DS showed the lowest bile acid-binding ability
 under the experimental conditions. The results from this study
 suggested that sulfation is a possible approach to obtain novel
 water-soluble derivatives of GLP with improved physicochemical,
 functional, and biological properties for potential utilization in
 functional foods or supplemental products.
 SN 0021-8561
 PD MAR 24
 PY 2010
 VL 58
 IS 6
 BP 3336
 EP 3341
 DI 10.1021/jf903395g
 UT ISI:000275710700015
 PT J
 AU An, JJ
 Zhou, JL
 Li, HJ
 Jiang, Y
 Li, P
 AF An, Jing-Jing
 Zhou, Jian-Liang
 Li, Hui-Jun
 Jiang, Yan
 Li, Ping
 TI Puqienine E: An angiotensin converting enzyme inhibitory steroidal
 alkaloid from Fritillaria puqiensis
 SO FITOTERAPIA
 AB Eight steroidal alkaloids, puqienine A, puqienine B, puqienine C,
 puqienine D, puqienine E, puqietinone, puqiedine and peimisine were
 isolated from Fritillaria puqiensis G D Yu et G Y Chen, and their
 anti-hypertensive effect were assessed in vitro based oil the
 inhibition of the Purified angiotensin converting enzyme (ACE) Using
 high-performance liquid chromatography assay The results showed that
 puqienine E, puqienine B and puqienine A exhibited better inhibitory
 activity against ACE than others, with inhibition ratios of 70 2 +/0 5%, 24 7 +/- 0 5% and 20 4 +/- 2 8%. respectively at the concentration
 of 200 mu M The 50% inhibiting concentration of puqienine E was
 determined to be 68 mu M (C) 2009 Elsevier B V All rights reserved
 SN 0367-326X
 PD APR
 PY 2010
 VL 81
 IS 3
 BP 149
 EP 152
 DI 10.1016/j.fitote.2009.08.012
 UT ISI:000275599200001
 A Sun, ZX
 U Huang, XF
 Kong, LY
 A Sun, Zhouxuan
 F Huang, Xuefeng
 Kong, Lingyi
 T A new steroidal saponin from the dried stems of Asparagus officinalis
 FITOTERAPIA
 A Yamnogenin II (1), a new steroidal saponin with a unique aglycone
 B moiety, and (25S)-spirostan-5-ene-3
 beta-ol-3-O-alpha-L-rhamnopyranosyl-(1,2)-[alpha-L-rhamnopyranosyl(1,4) ]-beta-D-glucopyranoside (2), were isolated from the dried stems
 of Asparagus officinalis L The structure of 1 was assessed by
 spectroscopial analysis as (25S)-spirostan-5-ene-3
 beta,21-diol-3-O-alpha-L-rhamnopyranosyl-(1,2)-[alpha-L-rhamnopyran
 osyl- (1,4)]-beta-D-glucopyranoside Crown Copyright (C) 2009 Published
 by Elsevier B V All rights reserved
 0367-326X
 2010
 10.1016/j.fitote.2009.09.002
 ISI:000275599200013
 PT J
 AU Ding, XP
 Wang, XT
 Xu, T
 Qi, J
 Wang, H
 Yu, BY
 AF Ding, Xiao-Ping
 Wang, Xin-Tang
 Xu, Tian
 Qi, Jin
 Wang, Hui
 Yu, Bo-Yang
 TI Comparison of Two On-Line Analysis Techniques Used for the Screening
 of Antioxidants in EGb 761
 SO CHROMATOGRAPHIA
 AB In order to perform on-line screening procedures for antioxidants in
 the Ginkgo biloba extract (EGb761), a comparison was carried out
 between LC-DAD-DPPH analysis used for the determination of DPPH center
 dot bleaching and LC-DAD-CL determination applied for the detection
 of H2O2 and O (2) (-center dot) scavenging activities. The results
 demonstrated that 15 antioxidants in EGb 761 could be identified by
 LC-DAD-CL, while only 10 antioxidants were detected under LC-DAD-DPPH
 conditions. Furthermore, it was found that both sensitivity and
 reproducibility of the LC-DAD-CL method were superior. The results
 indicated that the combination of the two methods might provide useful
 information for the prediction of antioxidants in herbal medicines.
 SN 0009-5893
 PD MAR
 PY 2010
 VL 71
 IS 5-6
 BP 493
 EP 497
 DI 10.1365/s10337-010-1470-8
 UT ISI:000275787900020
 PT J
 AU Lu, XY
 Chen, YD
 You, QD
 AF Lu, Xiaoyun
 Chen, Yadong
 You, Qidong
 TI 3D-QSAR, molecular docking studies, and binding mode prediction of
 thiolactomycin analogs as mtFabH inhibitors
 SO JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
 AB Mycobacterium tuberculosis beta-ketoacyl-acyl carrier protein
 synthase III (mtFabH) has been identified as a novel target for treating
 tuberculosis. The aim of this study was to understand the binding
 affinities of thiolactomycin (TLM) analogs for mtFabH based on 3D
 quantitative structure-activity relationship (3D-QSAR) analysis and
 molecular docking studies. The 3D-QSAR models produced statistically
 significant results (comparative molecular field analysis (CoMFA) r2
 cv = 0.701, r<SU2</SU = 0.988; comparative molecular similarity indices
 analysis (CoMSIA) r2 cv = 0.625, r<SU2</SU = 0.969) with 40 TLM analogs.
 In particular, compounds possessing hydrogen bond acceptors attached
 to the end of side chains at the C5 position of TLM analogs may enhance
 their activity. The results of 3D-QSAR models were further compared
 with structure-based analysis using docking studies with the crystal
 structure of mtFabH. A plausible binding mode between TLM analogs and
 mtFabH is proposed.</.
 SN 1475-6366
 PD APR
 PY 2010
 VL 25
 IS 2
 BP 240
 EP 249
 DI 10.3109/14756360903049059
 UT ISI:000275467200011
 PT J
 AU Yang, J
 Ding, L
 Jin, SH
 Liu, XX
 Liu, WY
 Wang, ZZ
 AF Yang, Jing
 Ding, Li
 Jin, Shaohong
 Liu, Xiaoxue
 Liu, Wenyuan
 Wang, Zhenzhong
 TI Identification and quantitative determination of a major circulating
 metabolite of gambogic acid in human
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB Gambogic acid (GA), a promising anticancer candidate, is a
 polyprenylated xanthone abundant in the resin of Garcinia morella and
 Garcinia hanburyi. The major circulating metabolite of CA in human,
 10-hydroxygambogic acid (10-OHGA), was identified by comparison of the
 retention time and mass spectra with those of reference standard using
 liquid chromatography-tandem mass spectrometry. The reference
 standard of 10-OHGA was isolated from bile samples of rats after
 intravenous injection of GA injection, and its structure was confirmed
 by NMR. Then, a selective and sensitive method was developed for the
 quantitative determination of this metabolite in human plasma. After
 liquid-liquid extraction by ethyl acetate, the analyte and the internal
 standard were separated on a Sepax HPC18 column (100mm x 2.1 mm i.d.,
 3.0 mu m) with a mobile phase of 10mM ammonium acetate water solution
 containing 0.1% formic acid-acetonitrile (20:80, v/v). The detection
 was performed on a single quadrupole mass spectrometer equipped with
 electrospray ionization (ESI) source. The calibration curve was linear
 over the range of 3-2000ng/mL for 10-OHGA. The developed quantification
 method can now be used for the pharmacokinetic and pharmacological
 Studies of 10-OHGA after intravenous infusion of CA injection in human.
 (C) 2010 Elsevier B.V. All rights reserved.
 SN 1570-0232
 PD MAR 1
 PY 2010
 VL 878
 IS 7-8
 BP 659
 EP 666
 DI 10.1016/j.jchromb.2010.01.032
 UT ISI:000275565200006
 PT J
 AU Chen, B
 Du, YX
 AF Chen, Bin
 Du, Yingxiang
 TI Evaluation of the enantioseparation capability of the novel chiral
 selector clindamycin phosphate towards basic drugs by micellar
 electrokinetic chromatography
 SO JOURNAL OF CHROMATOGRAPHY A
 AB To date, a series of chiral selectors have been utilized successfully
 in capillary electrophoresis (CE) Among these Various chiral
 selectors, macrocyclic antibiotics have been demonstrated to represent
 powerful enantioselectivity towards many chiral compounds. Differing
 from macrocyclic antibiotics, the use of lincosamide antibiotics as
 chiral selectors has not been reported previously. In our recent work,
 clindamycin phosphate belonging to the group of lincosamides has been
 first used as a chiral selector in capillary zone electrophoresis (CZE)
 In this paper, a micellar electrokinetic chromatography (MEKC) method
 has been developed for the evaluation of enantioseparation capability
 of this novel chiral selector towards several racemic basic drugs As
 observed during the Course of this work, clindamycin phosphate allowed
 excellent separation of the enantiomers of nefopam, citalopram,
 tryptophan, chlorphenamine, propranolol and metoprolol, as well as
 partial enantioresolution of tryptophan methyl ester and cetirizine
 In this MEKC chiral separation system, different types of anionic
 surfactants. organic additives and background electrolytes were
 tested. and satisfactory enantioseparations of basic drugs
 above-mentioned were achieved using sodium dodecyl sulfate (SDS) as
 the surfactant, isopropanol as the organic additive, and phosphate as
 the background electrolyte Furthermore, both migration times and
 enantioseparation of the analytes were influenced by several
 experimental parameters such as pH of the BGE, clindamycin phosphate
 and SDS concentrations, phosphate and isopropanol concentrations, and
 applied voltage Consequently, the effects of these factors on
 enantioseparations of the studied basic drugs were systematically
 investigated in order to evaluate the stereoselectivity of clindamycin
 phosphate in MEKC (C) 2010 Elsevier B V All rights reserved
 SN 0021-9673
 PD MAR 12
 PY 2010
 VL 1217
 IS 11
 BP 1806
 EP 1812
 DI 10.1016/j.chroma.2010.01.043
 UT ISI:000275353800011
 PT J
 AU Hu, XB
 Zhang, YK
 Lin, M
 Lu, Y
 Zhang, Y
 Zhang, HY
 Chen, YY
 Hou, J
 Xing, Y
 Jin, L
 Cao, RY
 Liu, JJ
 AF Hu Xiangbing
 Zhang Yankai
 Lin Ming
 Lu Yong
 Zhang Yu
 Zhang Huiyong
 Chen Yingying
 Hou Jing
 Xing Yun
 Jin Liang
 Cao Rongyue
 Liu Jingjing
 TI The fusion protein of HSP65 with tandem repeats of beta-hCG acting as
 a potent tumor vaccine in suppressing hepatocarcinoma
 SO INTERNATIONAL IMMUNOPHARMACOLOGY
 AB It has been demonstrated that the beta-subunit of human chorionic
 gonadotropin (beta-hCG) is ectopically expressed on a variety of human
 cancers of different histological types and has been used as an
 antigenic target in anti-cancer vaccines. We engineered a fusion
 protein by fusing 10 tandemly repeated copies of the 10-residue
 sequence of beta-hCG (109-118) (in CTP37) combined with beta-hCG
 C-terminal 37 peptides to mycobacterial heat-shock protein 65 and
 immunized mice via subcutaneous injection. Humoral immune and cellular
 immune responses were effectively elicited. High titer of
 anti-beta-hCG antibody was detected in immunized mice sera by ELISA
 and verified by Western blot analyses. The fusion protein of
 HSP65-X10-beta-hCGCTP37 effectively inhibited the growth of tumor both
 protective and therapeutic anti-tumor immunity in hepatocellular
 carcinoma tumor models in mice. Meanwhile, it also attenuated
 tumor-induced angiogenesis in intradermal tumor model in mice. Taken
 together, these results demonstrate that immune responses are
 effectively induced by a novel fusion protein vaccine targeting
 beta-hCG, suppressing the growth of hepatocellular carcinoma in mice.
 The beta-hCG-targeted vaccine holds promise for the treatment of a
 number of cancers and merits further study. (C) 2009 Elsevier B.V. All
 rights reserved.
 SN 1567-5769
 PD FEB
 PY 2010
 VL 10
 IS 2
 BP 230
 EP 238
 DI 10.1016/j.intimp.2009.11.006
 UT ISI:000275381400013
 PT J
 AU Zhao, L
 Liang, JY
 Zhang, JY
 Chen, Y
 AF Zhao, Ling
 Liang, Jing Yu
 Zhang, Jing Yu
 Chen, Yun
 TI A novel diarylheptanoid bearing flavonol moiety from the rhizomes of
 Alpinia officinarum Hance
 SO CHINESE CHEMICAL LETTERS
 AB A novel diarylheptanoid bearing flavonol moiety, named officinin A (1),
 along with two known compounds galangin and kaempferide were isolated
 from the rhizomes of Alpina officinarum Hance. The structure
 elucidation was accomplished by HR-ESI-MS, 1D and 2D NMR methods. (C)
 2009 Jing Yu Liang. Published by Elsevier B.V. on behalf of Chinese
 Chemical Society. All rights reserved.
 SN 1001-8417
 PD FEB
 PY 2010
 VL 21
 IS 2
 BP 194
 EP 196
 DI 10.1016/j.cclet.2009.09.011
 UT ISI:000275396700018
 PT J
 AU Wei, MC
 Wang, SZ
 Fang, YL
 Chen, YJ
 AF Wei, Maochen
 Wang, Shuzhen
 Fang, Yongliang
 Chen, Yijun
 TI Microbial generation of nocathiacin acid from nocathiacin I
 SO BIORESOURCE TECHNOLOGY
 AB Microbial generation of nocathiacin acid from nocathiacin I by
 manipulating enzymatic activities related to C-terminal
 dehydroalanine hydrolysis in Amycolatopsis fastidiosa LCB1001 was
 investigated by comparing the effects of various factors including
 metal ions, amino acid precursors and starting pH on the
 transformation. CuCl2 and cysteine significantly increased
 bioconversion yields, and starting pH and time were also major factors
 affecting the product yield. Under optimal conditions, the yield of
 nocathiacin acid was increased from 10.4 mg/L to greater than 45.0 mg/L
 after 6 days of fermentation. The use of protease inhibitors indicated
 that enzymes such as peptidylglycine monooxygenase and alcylase I are
 likely involved in the bioconversion. This is the first report on the
 generation of nocathiacin acid through microbial conversion in situ.
 Compared to chemical methods, the present approach is more effective
 and could be broadly applied in the production of novel derivatives
 of microbial secondary metabolites. (c) 2009 Elsevier Ltd. All rights
 reserved.
 SN 0960-8524
 PD MAY
 PY 2010
 VL 101
 IS 10
 BP 3617
 EP 3622
 DI 10.1016/j.biortech.2009.12.060
 UT ISI:000275563200044
 PT J
 AU Tan, DP
 Chou, GX
 Wang, ZT
 AF Tan, Dao-peng
 Chou, Gui-xin
 Wang, Zheng-tao
 TI Phenolic compounds from Senecio scandens
 SO BIOCHEMICAL SYSTEMATICS AND ECOLOGY
 SN 0305-1978
 PD FEB
 PY 2010
 VL 38
 IS 1
 BP 122
 EP 124
 DI 10.1016/j.bse.2009.12.032
 UT ISI:000275581200016
 PT J
 AU Wang, Y
 Feng, F
 Wang, Z
 AF Wang, Ya
 Feng, Fang
 Wang, Zhe
 TI DETERMINATION OF SELECTED ELEMENTS IN AQUEOUS EXTRACTIONS OF A
 TRADITIONAL CHINESE MEDICINE FORMULA BY ICP-MS AND FAAS: EVALUATION
 OF FORMULA RATIONALITY
 SO ANALYTICAL LETTERS
 AB Eight elements (Mg, Fe, Al, Ti, Mn, Co, Cu, and Zn) in Bai-Hu-Tang,
 an aqueous extraction of a traditional Chinese medicine formula
 consists of four crude drugs, were analyzed quantitatively by
 inductively coupled plasma mass spectrometry and flame atomic
 absorption spectrometry. The method was validated and the rationality
 of this formula was confirmed for enhancing dissolution of Mg, Fe, Cu,
 Mn, and Zn in the extraction while reducing that of Al and Co. By
 employing multivariate statistical techniques, data were classified
 and relationships among elements content in samples of different
 composition were revealed.
 SN 0003-2719
 PY 2010
 VL 43
 IS 6
 BP 983
 EP 992
 DI 10.1080/00032710903491138
 UT ISI:000275436100009
 PT J
 AU Huang, Y
 Gan, HF
 Li, S
 Xu, JY
 Wu, XM
 Yao, HQ
 AF Huang, Yue
 Gan, Haifeng
 Li, Shang
 Xu, Jinyi
 Wu, Xiaoming
 Yao, Hequan
 TI Oxidation of 4-carboxylate thiazolines to 4-carboxylate thiazoles by
 molecular oxygen
 SO TETRAHEDRON LETTERS
 AB A facile and environment-benign oxidation by molecular oxygen was
 applied for the conversion of 4-carboxylate thiazolines to
 4-carboxylate thiazoles. The substituent effect on thiazoline ring was
 investigated. it was found that electron-poor group on the thiazoline
 ring could facilitate the oxidation. (C) 2010 Elsevier Ltd. All rights
 reserved.
 SN 0040-4039
 PD MAR 31
 PY 2010
 VL 51
 IS 13
 BP 1751
 EP 1753
 DI 10.1016/j.tetlet.2010.01.091
 UT ISI:000275292800035
 PT J
 AU Cheng, KG
 Liu, J
 Sun, HB
 Xie, J
 AF Cheng, Keguang
 Liu, Jun
 Sun, Hongbin
 Xie, Juan
 TI Synthesis of Nucleoside Conjugates as Potential Inhibitors of Glycogen
 Phosphorylase
 SO SYNTHESIS-STUTTGART
 AB Click chemistry has been successfully used for the synthesis of novel
 nucleoside conjugates between uridine and N-acetylglucosamine or
 oleanolic acid derivatives. These molecules displayed micromolar
 inhibition towards glycogen phosphorylase.
 SN 0039-7881
 PD MAR
 PY 2010
 IS 6
 BP 1046
 EP 1052
 DI 10.1055/s-0029-1218629
 UT ISI:000275197300024
 PT J
 AU Xie, SF
 Xiang, BR
 Zhang, M
 Deng, HS
 AF Xie, Shaofei
 Xiang, Bingren
 Zhang, Ming
 Deng, Haishan
 TI Determination of medroxyprogesterone in water samples using dispersive
 liquid-liquid microextraction with low solvent consumption
 SO MICROCHIMICA ACTA
 AB A simple, rapid and efficient extraction procedure, dispersive
 liquid-liquid microextraction with low solvent consumption, has been
 developed in combination with high-performance liquid
 chromatography-ultraviolet detection for the extraction and
 determination of medroxyprogesterone from aqueous samples. For this
 technique, 120 mu L of the mixture of extraction solvent and dispersive
 solvent at a ratio of 3:7 was injected into the aqueous sample with
 a syringe. Then a cloudy solution forms while manually shaking the
 conical centrifuge tube. After centrifuging, the extractant settled
 at the bottom of the conical centrifuge tube and part of it was
 introduced into the HPLC system. Some key parameters, including the
 type and volume of extraction solvent and dispersive solvent,
 extraction time and salt effect were investigated. Under optimum
 conditions, good linear behavior (R > 0.9982) over the investigated
 concentration ranges were obtained. The method was successfully
 applied to tap water, farm water and river water samples.
 SN 0026-3672
 PD MAR
 PY 2010
 VL 168
 IS 3-4
 BP 253
 EP 258
 DI 10.1007/s00604-010-0291-7
 UT ISI:000275123000009
 PT J
 AU Fang, L
 Jumpertz, S
 Zhang, YH
 Appenroth, D
 Fleck, C
 Mohr, K
 Trankle, C
 Decker, M
 AF Fang, Lei
 Jumpertz, Sabine
 Zhang, Yihua
 Appenroth, Dorothea
 Fleck, Christian
 Mohr, Klaus
 Traenkle, Christian
 Decker, Michael
 TI Hybrid Molecules from Xanomeline and Tacrine: Enhanced Tacrine Actions
 on Cholinesterases and Muscarinic M-1 Receptors
 SO JOURNAL OF MEDICINAL CHEMISTRY
 AB A set of amide- and amine-linked hybrid molecules comprising moieties
 of the orthosteric M-1 muscarinic receptor agonist xanomeline and the
 cholinesterase inhibitor and allosteric receptor modulator tacrine
 were prepared with varying spacer length of 10-17 atoms. The hybrids
 inhibited acetylcholinesterase with similar or higher potency compared
 to tacrine. M, receptor binding affinity was similar or higher relative
 to xanomeline and far higher relative to tacrine. Affinities hardly
 changed when the receptors' orthosteric site was Occupied by all
 inverse agonist ligand. When Occupied by the orthosteric activator
 acetylcholine, affinity for the hybrids declined to unmeasureably low
 levels. Hybrids did not activate M-1 receptors. In vivo studies
 assaying cognition impairment in rats induced by scopolamine revealed
 pronounced enhancement of scopolamine action. Taken together, instead
 of dualsteric (simultaneous allosteric/orthosteric) binding, the
 hybrids seem to prefer purely allosteric binding at the inactive M-1
 receptor.
 SN 0022-2623
 PD MAR 11
 PY 2010
 VL 53
 IS 5
 BP 2094
 EP 2103
 DI 10.1021/jm901616h
 UT ISI:000275087000017
 PT J
 AU Yao, WR
 Zhang, YZ
 Chen, Y
 Yang, ZP
 AF Yao, Wei-Rong
 Zhang, Yin-Zhu
 Chen, Yi
 Yang, Zhi-Ping
 TI Aroma Enhancement and Characterization of the Absolute Osmanthus
 fragrans Lour.
 SO JOURNAL OF ESSENTIAL OIL RESEARCH
 AB In this paper, beta-glucosidase hydrolysis approach was applied on
 Osmanthus fragrans Lour. flowers for the aroma enhancement of the
 extract. The hydrolysis and extraction conditions, including enzyme
 amount, temperature, time, rate of agitation, buffer pH, buffer volume,
 extraction time, extraction temperature and petroleum ether volume,
 were optimized. The crude extract (concrete) and refined extract
 (absolute) under optimum conditions had increased yields of 0.42% and
 0.25%, which were 147.1% and 177.8%, respectively, as compared with
 the procedure without the beta-glucosidase hydrolysis. Analyses showed
 no obvious qualitative differences in the volatiles produced with and
 without enzymatic hydrolysis. However, the amount of typical aroma
 components significantly increased in the hydrolysis sample, As
 compared with the no-hydrolysis control, the first four aroma
 components with the most increase were
 6,10,14-trimethyl-2-pentadecan-2-one, nonanal, dihydro-beta-ionol
 and (E)-beta-ionone in the hydrolysis sample.
 Megastigma-4,6(E),8(E)-triene was only found in the hydrolysis sample,
 but the amount of trans-linalool oxide, cis-linalool oxide and
 dihydro-3-oxo-ionol decreased. Organoleptic assessment supported that
 the hydrolysis sample produced a stronger fragrance.
 SN 1041-2905
 PD MAR-APR
 PY 2010
 VL 22
 IS 2
 BP 97
 EP 102
 UT ISI:000275213100001
 PT J
 AU Guo, Q
 Deng, M
 Yu, BY
 Tan, L
 AF Guo, Qing
 Deng, Ming
 Yu, Boyang
 Tan, Li
 TI Analysis of the Residues of 20 Organochlorine Pesticides in Herba
 epimedii, a Chinese Herbal Medicine, by Solid-Phase Extraction with
 Gas Chromatography/Negative Chemical Ionization-Mass Spectrometry
 SO JOURNAL OF AOAC INTERNATIONAL
 AB A multiresidue analytical method has been developed to simultaneously
 determine the residues of 20 organochlorine pesticides in Herba
 epimedii, a traditional Chinese medicine. The 20 pesticides are
 included in the list of regulated substances by the Food and
 Environmental Hygiene Department in Hong Kong. The method consists of
 solid-phase extraction for cleanup of samples and GC coupled on-line
 with negative chemical ion-MS to analyze the target pesticides. The
 chromatographic separation of the compounds was carried out on a
 DB-1701 column by using an optimal temperature program, and the
 quantitative analysis was conducted by selected ion monitoring. The
 LOD and LOQ values fell in the range of 0.0555-5.8821 and 0.1241-17.9333
 ng/g, respectively. The average recoveries were between 75.4 and 90.7%
 (n = 5) for the 20 organochlorine pesticides. The developed method
 proved to be reliable and accurate, and permits rapid determination
 of the 20 organochlorine pesticides in one run.
 SN 1060-3271
 PD JAN-FEB
 PY 2010
 VL 93
 IS 1
 BP 295
 EP 305
 UT ISI:000275096600035
 PT J
 AU Yao, S
 Ma, L
 Luo, JG
 Wang, JS
 Kong, LY
 AF Yao, Shun
 Ma, Li
 Luo, Jian-Guang
 Wang, Jun-Song
 Kong, Ling-Yi
 TI New Triterpenoid Saponins from the Roots of Gypsophila paniculata L.
 SO HELVETICA CHIMICA ACTA
 AB The seven new triterpenoid saponins 1-7 were isolated from the roots
 of Gypsophila paniculata L. Their structures were established by 1Dand 2D-NMR techniques, HR-MS, and acid hydrolysis. The isolated
 compounds include 3,28-O-bidesmosides with or without a
 4-methoxycinnamoyl group (see 1 vs. 2 and 3), and 3-O-monoglucosides
 4-7. All isolated saponins 1-7 and their aglycones were evaluated for
 their alpha-glucosidase inhibition activity. Compound 1 showed
 inhibitor activity against yeast alpha-glucosidase with an IC50 value
 of 100.9 +/- 3.3 mu M, whereas compounds 2-7 were inactive.
 SN 0018-019X
 PY 2010
 VL 93
 IS 2
 BP 361
 EP 374
 UT ISI:000275157100026
 PT J
 AU Ding, XP
 Wang, XT
 Chen, LL
 Qi, J
 Xu, T
 Yu, BY
 AF Ding, Xiao-Ping
 Wang, Xin-Tang
 Chen, Lin-Lin
 Qi, Jin
 Xu, Tian
 Yu, Bo-Yang
 TI Quality and antioxidant activity detection of Crataegus leaves using
 on-line high-performance liquid chromatography with diode array
 detector coupled to chemiluminescence detection
 SO FOOD CHEMISTRY
 AB An on-line high-performance liquid chromatography-diode array
 detector combined with chemiluminescence detection (HPLC-DAD-CL)
 method was developed to evaluate the antioxidant activity and quality
 of Crotaegus leaves derived from different species and habitats. The
 chromatographic fingerprint and active profiles of Crataegus leaves
 were simultaneously achieved by HPLC-DAD-CL. Main antioxidants in
 Crataegus leaves were identified by HPLC-DAD-CL and HPLC/ESI/MS. Data
 analysis based on the total antioxidant activities of 10 batches of
 samples indicated that there were obvious differences among samples
 from different species and habitats. Good precision and
 reproducibility were obtained for DAD and CL detection with relative
 standard deviations less than 1.0% for retention time and 4.0% for intra
 and inter-day variations. The results suggested that the on-line method
 might provide potential information for the identification and
 quantitation of active markers, which were directly associated with
 the quality of herbal medicines. (C) 2009 Elsevier Ltd. All rights
 reserved.
 SN 0308-8146
 PD JUN 1
 PY 2010
 VL 120
 IS 3
 BP 929
 EP 933
 DI 10.1016/j.foodchem.2009.11.014
 UT ISI:000275014200043
 PT J
 AU Lu, XY
 You, QD
 AF Lu, Xiaoyun
 You, Qidong
 TI Recent Advances on Platensimycin: A Potential Antimicrobial Agent
 SO CURRENT MEDICINAL CHEMISTRY
 AB Platensimycin, an active metabolite of Streptomyces platensis, was
 initially discovered by a combination of RNA interferin induced
 gene-silencing and library screening to microbial extracts.
 Platensimycin selectively inhibits beta-ketoacyl-acyl carrier protein
 (ACP) synthase II (FabF) that is recognized as an effective
 broad-spectrum antibiotic against drug-resistant microorganism
 strains. Its novel scaffold and extraordinary antibacterial activity
 have drawn great attentions in recent years. So far, a number of
 synthetic strategies have been explored for the total synthesis of
 platensimycin. Moreover, many analogues have been investigated in
 terms of structure-activity relationships (SAR). This review provides
 a detailed overview of updated studies on platensimycin, focusing on
 various total and formal synthetic strategies, development of
 analogues, and the structure-activity relationships.
 SN 0929-8673
 PD APR
 PY 2010
 VL 17
 IS 12
 BP 1139
 EP 1155
 UT ISI:000275151500003
 PT J
 AU Chen, Q
 Luo, JG
 Kong, LY
 AF Chen, Qing
 Luo, Jian-Guang
 Kong, Ling-Yi
 TI Triterpenoid Saponins from Gypsophila altissima L.
 SO CHEMICAL & PHARMACEUTICAL BULLETIN
 AB Two new triterpenoid saponins (1, 2) were isolated from the roots of
 Gypsophila altissima L. (Caryophyl-laceac), together with a known
 compound (3). The structures of new, saponins were established as
 quillaic acid 3-O-beta-D-xylopranosyl-(1 ->
 3)-beta-D-glucuronopyranoside (1), and 3-O-beta-D-galactopyransyl-(1
 -> 2)-1 beta-D-xylopyranosyl-(1 -> 3)]-beta-D-glucuronopyranosyl
 quillaic acid 28-O-(6-O-acetyl)-beta-D-glucopyranosyl-(1 ->
 2)[beta-D-glucopyranosyl-(1 -> 3)-[beta-D-xylopyranosyl-(1 ->
 4)]-alpha-L-rhamnopyranosyl-(1 -> 2)beta-D-fucopyranoside (2), on the
 basis of various (2), on the basis of various spectroscopic analyses
 (including heteronuclear single quantum correlation (HSQC).
 heteronuclear multiple bond correlation (HMBC), nuclear Overhauser
 effect spectroscopy (NOESY), total correlation spectroscopy (TOCSY),
 and high-resolution electrospray ionization mass spectrometry
 (IIR-ESI-MS)) and chemical degradations.
 SN 0009-2363
 PD MAR
 PY 2010
 VL 58
 IS 3
 BP 412
 EP 414
 UT ISI:000275047200025
 PT J
 AU Chen, JQ
 Zha, XM
 AF Chen, Junqing
 Zha, Xiaoming
 TI 4 '-Bromobutyl ent-16-oxobeyeran-19-oate
 SO ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE
 AB The title compound, C24H37BrO3, is a tetracyclic diterpenoid with a
 beyerane skeleton, synthesized by esterification of isosteviol. It
 comprises a fused four-ring system A/B/C/D. Rings A and B have a chair
 conformation, whereas ring C is an unsymmetrical distorted chair; the
 remaining five-membered ring D adopts an envelope conformation. The
 stereochemistry of the A/B and B/C ring junctions are trans, while the
 C/D junction is cis.
 SN 1600-5368
 PD MAR
 PY 2010
 VL 66
 PN Part 3
 BP O607
 EP U4927
 DI 10.1107/S1600536810005167
 UT ISI:000275126500172
 PT J
 AU Zhou, L
 Liu, JH
 Zhang, J
 Wei, SH
 Feng, YY
 Zhou, JH
 Yu, BY
 Shen, J
 AF Zhou, Lin
 Liu, Ji-Hua
 Zhang, Jian
 Wei, Shao-Hua
 Feng, Yu-Ying
 Zhou, Jia-Hong
 Yu, Bo-Yang
 Shen, Jian
 TI A new sol-gel silica nanovehicle preparation for photodynamic therapy
 in vitro
 SO INTERNATIONAL JOURNAL OF PHARMACEUTICS
 AB We report a facile silica nanovehicle preparation procedure for
 hydrophobic drug delivery, which is carried out in water without adding
 any surfactant and additional catalyst. This strategy includes
 hydrophobic drug nanopaticle preparation by reprecipitation method and
 in situ hydrolyzation and polymerization to encapsulate this
 naoparticle using only
 N-(beta-amimoethyl)-gamma-aminopropyltyiethoxysilane (AETPS). To
 demonstrate this technique hypocrellin A (HA), a hydrophobic
 photosensitizing anticancer drug, is embedded into silica nanovehicle
 using this simple method. The resulting HA encapsulated nanovehicles
 (HANV) are monodisperse and stable in aqueous solution. Comparative
 studies with free HA and entrapped HA have demonstrated that the
 encapsulation effect on the embedded photosensitizer nanoparticle
 significantly enhances the efficacy of singlet oxygen generation and,
 thereby, the in vitro photodynamic efficacy. (C) 2009 Elsevier B.V.
 All rights reserved.
 SN 0378-5173
 PD FEB 15
 PY 2010
 VL 386
 IS 1-2
 BP 131
 EP 137
 DI 10.1016/j.ijpharm.2009.11.010
 UT ISI:000274876400016
 PT J
 AU Mao, YF
 Li, YQ
 Zong, L
 You, XM
 Lin, FQ
 Jiang, L
 AF Mao, Yan-Fei
 Li, Yong-Qi
 Zong, Lin
 You, Xin-Min
 Lin, Fu-Qing
 Jiang, Lai
 TI Methanol extract of Phellodendri cortex alleviates
 lipopolysaccharide-induced acute airway inflammation in mice
 SO IMMUNOPHARMACOLOGY AND IMMUNOTOXICOLOGY
 AB Materials and methods: At 2 h after LPS exposure, mice were treated
 orally with methanol extract of Phellodendri cortex (100, 200 and 400
 mg/kg). At the end of this study, bronchoalveolar lavage fluids (BALF)
 were collected and number of total cells, macrophages and neutrophils,
 protein concentration were analyzed. Tumor necrosis factor-alpha
 (TNF-alpha), macrophage inflammatory protein (MIP-2), IL-10 levels and
 nitric oxide (NO) production in BALF were also determined.
 Results: Methanol extract of Phellodendri cortex dose-dependently
 alleviated LPS-induced acute airway inflammation via decreasing the
 infiltration of inflammatory cells and the release of inflammatory
 mediators.
 Conclusion: The relief of airway inflammation provides a possible
 therapeutic application of Phellodendri cortex for the treatment of
 infectious pulmonary diseases.
 SN 0892-3973
 PD MAR
 PY 2010
 VL 32
 IS 1
 BP 110
 EP 115
 DI 10.3109/08923970903193325
 UT ISI:000274909100015
 PT J
 AU Cheng, J
 Wu, ZH
 Ping, QNN
 Wang, BG
 Lu, JJ
 AF Cheng, Juan
 Wu, Zheng Hong
 Ping, Qineng Neng
 Wang, Bogang
 Lu, Junjun
 TI The absorption characteristics of bifendate solid dispersion in rat
 intestinal tissue
 SO DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
 AB Aim: Research on bifendate intestinal absorption. Method: The single
 passed intestinal backflow method was used. Bifendate with different
 concentrations, bifendate with and without 2,4-dinitrophenol,
 verapamil, and probenecid, and solid state of bifendate in different
 systems were studied. Result: Change of concentration and the presence
 of energy inhibitor, P-glycoprotein inhibitor and multidrug-resistant
 protein inhibitor did not affect the K-a of bifendate intestinal
 absorption; there were obvious differences among intestinal absorption
 of native drug, solid dispersion, and physical mixtures. Conclusion:
 The result indicated that the intestinal absorption mechanism of
 bifendate is passive transport. Solid state of bifendate in different
 systems could affect the intestinal absorption.
 SN 0363-9045
 PD MAR
 PY 2010
 VL 36
 IS 3
 BP 283
 EP 291
 DI 10.3109/03639040903140571
 UT ISI:000274905900003
 PT J
 AU Wu, L
 Zhang, G
 Lu, Q
 Sun, Q
 Wang, ML
 Li, N
 Gao, ZD
 Sun, Y
 Li, TT
 Han, DE
 Yu, X
 Wang, L
 Sun, W
 Zhao, D
 Wu, YN
 Lu, Y
 Chen, XJ
 AF Wu, Lei
 Zhang, Ge
 Lu, Qin
 Sun, Qian
 Wang, Mulan
 Li, Na
 Gao, Zidong
 Sun, Ya
 Li, Tingting
 Han, Deen
 Yu, Xue
 Wang, Lei
 Sun, Wei
 Zhao, Di
 Wu, Yaning
 Lu, Yang
 Chen, Xijing
 TI Evaluation of salmon calcitonin (sCT) enteric-coated capsule for
 enhanced absorption and GI tolerability in rats
 SO DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
 AB Background: Considering the chronic and repeated nature of salmon
 calcitonin (sCT) therapy, the oral route is a preferred route of
 administration. But, the oral bioavailability of sCT is very low due
 to enzymatic degradation and poor permeation across intestinal
 epithelial cells. It was the aim of this study to investigate the
 pharmacodynamic (PD), pharmacokinetic (PK), and mucosal injury
 characteristic of sCT oral delivery system. Method: In this study, PD
 experiments were performed to find a suitable releasing region of sCT,
 an effect absorption enhancer, and an optimal mass ratio of
 sCT/enhancer. In addition, the PK experiments were designed to validate
 the absorption enhancement of this oral delivery system.
 Histopathological evaluations on the intestinal mucosa were carried
 out to assess any potential toxicity of the absorption enhancer.
 Results: Through the PD research, we determined that oral sCT
 enteric-coated capsules containing sCT and citric acid (CA) with a
 ratio of 1:20 may be an adaptable delivery. PK study further proved
 that the oral absorption of sCT was enhanced from this delivery system.
 Finally, no damage on intestinal mucosa was observed when rats received
 the delivery system containing CA for up to 7 days. Conclusion: These
 results suggested that enteric-coated capsules with a certain amount
 of CA might give enhanced oral delivery of peptide drugs like sCT.</.
 SN 0363-9045
 PD MAR
 PY 2010
 VL 36
 IS 3
 BP 362
 EP 370
 DI 10.3109/03639040903173580
 UT ISI:000274905900012
 PT J
 AU Zhuang, P
 Ji, H
 Zhang, YH
 Min, ZL
 Ni, QG
 You, R
 AF Zhuang, Pei
 Ji, Hui
 Zhang, Yi-Hua
 Min, Zhen-Li
 Ni, Qing-Gui
 You, Ran
 TI ZJM-289, a novel nitric oxide donor, alleviates the cerebral
 ischaemic-reperfusion injury in rats
 SO CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY
 AB P>1. Current studies indicate that nitric oxide (NO) plays a dual role
 as both a protective and pathogenic factor in focal cerebral ischaemia
 depending on the level, location, source and environment. The present
 study hypothesized that the NO donor ZJM-289 could inhibit cerebral
 ischaemia-reperfusion (I/R) injury and investigated the mechanism of
 the beneficial events.
 2. Adult male rats were randomly divided into four groups: (i) sham
 operated; (ii) I/R (ischaemia for 90 min and reperfusion for 24 h)
 treated with vehicle; (iii) I/R treated with 0.1 mmol/kg body weight
 ZJM-289; and (iv) I/R treated with 0.2 mmol/kg body weight ZJM-289.
 We evaluated the changes in brain infarction, brain-water content,
 neurological deficits and histopathology. Western blot analysis was
 used to study the expression of endothelial nitric oxide synthase
 (eNOS) and neuronal nitric oxide synthase (nNOS) in the brain after
 I/R. The levels of NO and cyclic guanosine monophosphate (cGMP) were
 also determined.
 3. ZJM-289 reduced infarct volume and brain-water content in ischemic
 brains and promoted functional recovery. Western blotting showed
 significant inhibition of nNOS in ZJM-289 treated rats compared with
 untreated rats. However, eNOS expression in the ischemic brain was
 enhanced in the ZJM-289 groups. The cGMP and NO levels increased in
 the ZJM-289 groups after I/R. The study showed that ZJM-289 could
 alleviate cerebral injury after I/R through inhibition of nNOS and
 stimulation of the NO/soluble guanylate cyclase/cGMP pathway.
 Therefore, a suitable NO donor might be an effective candidate for the
 treatment of acute stroke by neuroprotection.
 SN 0305-1870
 PD MAR
 PY 2010
 VL 37
 IS 3
 BP e121
 EP e127
 DI 10.1111/j.1440-1681.2010.05353.x
 UT ISI:000274908000002
 PT J
 AU Han, DE
 Zheng, Y
 Li, N
 Zhao, D
 Zhang, G
 Yan, HF
 Zhang, LL
 Sun, W
 Wu, YN
 Lu, Y
 Chen, XJ
 AF Han, De-En
 Zheng, Yi
 Li, Ning
 Zhao, Di
 Zhang, Ge
 Yan, Hefeng
 Zhang, Lingli
 Sun, Wei
 Wu, Ya-Ning
 Lu, Yang
 Chen, Xijing
 TI Determination of Nateglinide in Human Plasma by LC-ESI-MS and Its
 Application to Bioequivalence Study
 SO CHROMATOGRAPHIA
 AB To evaluate the bioequivalence of nateglinide, a rapid and specific
 liquid chromatographic-electrospray ionization mass spectrometric
 method was developed and validated to determine nateglinide for human
 plasma samples. The analyte was detected using electrospray positive
 ionization mass spectrometry in the selected ion monitoring mode.
 Tinidazole was used as the internal standard. A good linear
 relationship obtained in the concentration ranged from 0.05 to 16 mu
 g mL(-1) (r (2) = 0.9993). Lower limit of quantification was 0.05 mu
 g mL(-1) using 100 mu L of plasma sample. Intra- and inter-day relative
 standard deviations were 2.1-7.5 and 4.7-8.9%, respectively. Among the
 pharmacokinetic data obtained, T (max) was 2.09 +/- A 1.06 h for
 reference formulation and 2.40 +/- A 0.97 h for test formulation. C
 (max) was 4.17 +/- A 1.31 mu g mL(-1) for reference formulation and
 4.37 +/- A 1.53 mu g mL(-1) for test formulation. The half-life (t
 (A1/2)) was 1.93 +/- A 0.44 h for reference formulation and 1.92 +/A 0.29 h for test formulation. AUC(0-10h) was 13.67 +/- A 4.36 mu g
 h mL(-1) for reference formulation and 13.21 +/- A 4.09 mu g h mL(-1)
 for test formulation. This method was successfully applied to the
 pharmacokinetic study in human plasma samples.
 SN 0009-5893
 PD FEB
 PY 2010
 VL 71
 IS 3-4
 BP 299
 EP 304
 DI 10.1365/s10337-009-1405-4
 UT ISI:000274903300018
 PT J
 AU Ye, DJ
 Zhang, Y
 Wang, F
 Zheng, MF
 Zhang, X
 Luo, XM
 Shen, X
 Jiang, HL
 Liu, H
 AF Ye, Deju
 Zhang, Yu
 Wang, Fei
 Zheng, Mingfang
 Zhang, Xu
 Luo, Xiaomin
 Shen, Xu
 Jiang, Hualiang
 Liu, Hong
 TI Novel thiophene derivatives as PTP1B inhibitors with selectivity and
 cellular activity
 SO BIOORGANIC & MEDICINAL CHEMISTRY
 AB A series of novel thiophene derivatives was designed, synthesized and
 their activities as competitive inhibitors of protein tyrosine
 phosphatase (PTPs) 1B (PTP1B) inhibitors were evaluated. All the
 compounds showed inhibitory potencies, and 10 of these exhibited
 moderate inhibitory activities with IC50 values less than 10 mu M. The
 activity of the most potent compound P28 (IC50 = 2.1 mu M) was 15 times
 higher than that of the hit compound P01. Further, four representative
 compounds (P19, P22, P28, and P31) demonstrated remarkably high
 selectivities against other PTPs (e. g., PTP alpha, LAR, CD45, and
 TCPTP); P19 exhibited greater than sixfold selectivity over highly
 homologous TCPTP. More importantly, these compounds are permeable to
 cell membranes. The treatment of CHO-K1 cells with P28 (10 mu M)
 resulted in increased phosphorylation of AKT, which suggested
 extensive cellular activity of this compound. The novel chemical
 entities reported in this study could be used for overcoming the poor
 selectivity and low cellular activity of PTP1B inhibitors and might
 represent a starting point for development of therapeutic PTP
 inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.
 SN 0968-0896
 PD MAR 1
 PY 2010
 VL 18
 IS 5
 BP 1773
 EP 1782
 DI 10.1016/j.bmc.2010.01.055
 UT ISI:000274957100003
 PT J
 AU Gu, SH
 Jiye, A
 Wang, GJ
 Zha, WB
 Yan, B
 Zhang, Y
 Ren, HC
 Cao, B
 Liu, LS
 AF Gu, Shenghua
 Jiye, A.
 Wang, Guangji
 Zha, Weibin
 Yan, Bei
 Zhang, Ying
 Ren, Hongcan
 Cao, Bei
 Liu, Linsheng
 TI Metabonomic profiling of liver metabolites by gas chromatography-mass
 spectrometry and its application to characterizing hyperlipidemia
 SO BIOMEDICAL CHROMATOGRAPHY
 AB The measurement of metabolites in tissues is of great importance in
 metabonomic research in the biomedical sciences, providing more
 relevant information than is available from systemic biofluids. The
 liver is the most important organ/tissue for most biochemical
 reactions, and the metabolites in the liver are of great interest to
 scientists. To develop an optimized extraction method and
 comprehensive profiling technique for liver metabolites, organic
 solvents of various compositions were designed using design of
 experiments to extract metabolites from the liver, and the metabolites
 were profiled by gas chromatography/time-of-flight mass spectrometry
 (GC/TOF-MS). The resolved peak areas were processed by principle
 components analysis, partial least-squares projections to latent
 structures, and discriminant analysis. The results suggest the highest
 extraction efficiency was for methanol-water, which maximized the
 majority of GC/TOF-MS responses. The optimal solvent was applied to
 extract metabolites in liver of hyperlipidemia hamster and the control.
 The GC/TOF-MS profiles of liver metabolites showed obvious differences
 between hyperlipidemic hamsters and controls. A comparison of liver
 and serum data from the same animals identified common biomarkers and
 presented complementary information. Our results suggest that liver
 metabonomics is a valuable technique and that the combined analysis
 of systematic biofluids and local tissues is meaningful and
 complementary, recovering more comprehensive metabonomic data than
 either analysis alone. Copyright (C) 2009 John Wiley & Sons, Ltd.
 SN 0269-3879
 PD MAR
 PY 2010
 VL 24
 IS 3
 BP 245
 EP 252
 DI 10.1002/bmc.1279
 UT ISI:000274938500003
 PT J
 AU Tang, Y
 Ni, MX
 Wu, WT
 Sun, J
 Zhou, CL
 AF Tang, Ying
 Ni, Mengxiang
 Wu, Wutong
 Sun, Jin
 Zhou, Changlin
 TI Biotransformation of the antitumor intermediate 5-fluorouridine by
 recombinant Escherichia coli with high pyrimidine nucleoside
 phosporylase activity
 SO BIOCATALYSIS AND BIOTRANSFORMATION
 AB 5-Fluorouridine (5-FUrd) is a precursor of the widely used antitumor
 drug doxifluridine. We have produced 5-FUrd by biotransformation by
 cloning the gene encoding pyrimidine nucleoside phosphorylase
 (PyNPase) from Enterobacter aero-genes CMCC (B) 45103 and expression
 in Escherichia coli BL21 (DE3), resulting in recombinant E. coli BL21
 (DE3)/ pET28a-PyNPase. After medium optimization, the PyNPase activity
 in the fermentation broth was 1613 U mg<SU-1</SU, which was 54-fold
 that of E. aerogenes. Under optimal conditions (cell concentration,
 0.5 g L<SU-1</SU; uridine, 10 mM; 5-fluorouracil, 45 mM; temperature,
 50 degrees C; pH, 7.8), more than 90% of uridine was converted to 5-FUrd,
 suggesting that this is a valuable tool for application in the
 preparation of antiviral and antitumor drugs.
 SN 1024-2422
 PD MAR
 PY 2010
 VL 28
 IS 2
 BP 130
 EP 136
 DI 10.3109/10242420903505842
 UT ISI:000274855300005
 PT J
 AU Yu, LY
 Zhang, W
 Xiang, BR
 Xie, SF
 Deng, HS
 Sun, RM
 AF Yu, Liyan
 Zhang, Wei
 Xiang, Bingren
 Xie, Shaofei
 Deng, Haishan
 Sun, Rongmei
 TI SIMPLEX-STOCHASTIC RESONANCE ALGORITHM APPLIED TO DETECTION OF WEAK
 CHROMATOGRAPHIC PEAKS
 SO ANALYTICAL LETTERS
 AB The simplex-stochastic resonance algorithm (SSRA) was applied to
 amplification and detection of the weak High Performance Liquid
 Chromatography (HPLC) chromatographic signals of coumatetralyl in
 plasma. In this algorithm, modified simplex algorithm was embedded to
 greatly enhance the signal-to-noise ratio of chromatographic signals.
 The application of SSRA to detect HPLC/UV weak signals of coumatetralyl
 showed an excellent quantitative relationship between different
 concentrations and responses. The assay was linear over the
 concentration range of 3-100 ng/mL, r = 0.9997, and RSD < 10%. The good
 linearity and precision demonstrated that it is an effective algorithm
 for detecting weak chromatographic peaks.
 SN 0003-2719
 PY 2010
 VL 43
 IS 5
 BP 851
 EP 857
 DI 10.1080/00032710903486344
 UT ISI:000274995000012
 PT J
 AU Song, QX
 Wu, HP
 Feng, F
 Zhou, GH
 Kajiyama, T
 Kambara, H
 AF Song, Qinxin
 Wu, Haiping
 Feng, Fang
 Zhou, Guohua
 Kajiyama, Tomoharu
 Kambara, Hideki
 TI Pyrosequencing on Nicked dsDNA Generated by Nicking Endonucleases
 SO ANALYTICAL CHEMISTRY
 AB Although the pyrosequencing method is simple and fast, the step of ssDNA
 preparation increases the cost, labor, and cross-contamination risk.
 In this paper, we proposed a method enabling pyrosequencing directly
 on dsDNA digested by nicking endonucleases (NEases). Recognition
 sequence of NEases was introduced using artificially mismatched bases
 in a PCR primer (in the case of genotyping) or a reverse-transcription
 primer (in the case of gene expression analysis). PCR products were
 treated to remove excess amounts of primers, nucleotides, and
 pyrophosphate (PPi) prior to sequencing. After the nicking reaction,
 pyrosequencing starts at the nicked 3' end, and extension reaction
 occurs when the added dNTP is complementary to the non-nicked strand.
 Although the activity of strand displacement by Klenow is limited,
 similar to 10 bases are accurately sequenced; this length is long enough
 for genotyping and SRPP-based differential gene expression analysis.
 It was observed that the signals of two allele-specific bases in a
 pyrogram from nicked dsDNA are highly quantitative, enabling
 quantitative determination of allele-specific templates; thus, Down's
 Syndrome diagnosis as well as differential gene expression analysis
 was successfully executed. ne results indicate that pyrosequencing
 using nicked dsDNA as templates is a simple, inexpensive, and reliable
 way in either quantitative genotyping or gene expression analysis.
 SN 0003-2700
 PD MAR 1
 PY 2010
 VL 82
 IS 5
 BP 2074
 EP 2081
 DI 10.1021/ac902825r
 UT ISI:000274841300070
 PT J
 AU Peng, KF
 Kong, Y
 Zhai, L
 Wu, XF
 Jia, P
 Liu, JZ
 Yu, HN
 AF Peng, Kanfu
 Kong, Yi
 Zhai, Lei
 Wu, Xiongfei
 Jia, Peng
 Liu, Jingze
 Yu, Haining
 TI Two novel antimicrobial peptides from centipede venoms
 SO TOXICON
 AB Centipede venoms are complex mixtures of biochemically and
 pharmacologically active components such as peptides and proteins.
 Very few are known about their pharmacological actions. The present
 work reports the structural and functional characterization of two
 antimicrobial peptides (scolopin 1 and -2) identified from centipede
 venoms of Scolopendra subspinipes mutilans by Sephadex gel filtration
 and reverse-phase high-performance liquid chromatography (RP-HPLC).
 The amino acid sequences of scolopin 1 and -2 were
 FLPKMSTKLRVPYRRGTKDYH and GILKKFMLHRGTKVYKMRTLSKRSH determined by
 Edman degradation and matrix assisted laser desorption ionization time
 of flight mass spectrometry (MALDI-TOF MS). Both scolopin I and -2
 showed strong antimicrobial activities against tested microorganisms
 including Gram-positive/negative bacteria and fungi. They also showed
 moderate hemolytic activity against both human and rabbit red cells.
 This is the first report of antimicrobial peptides from centipedes.
 (C) 2009 Elsevier Ltd. All rights reserved.
 SN 0041-0101
 PD FEB-MAR
 PY 2010
 VL 55
 IS 2-3
 BP 274
 EP 279
 DI 10.1016/j.toxicon.2009.07.040
 UT ISI:000274579100014
 PT J
 AU Luo, XQ
 Yang, HX
 Liang, CG
 Jin, SH
 AF Luo, Xiaoqing
 Yang, Huaxin
 Liang, Chenggang
 Jin, Shaohong
 TI Structural characterization of N-linked oligosaccharides of Defibrase
 from Agikistrodon acutus by sequential exoglycosidase digestion and
 MALDI-TOF mass spectrometry
 SO TOXICON
 AB Detailed structures of N-linked oligosaccharides of Defibrase, a
 highly active thrombin like enzyme (TLE) purified from the venom of
 Agkistrodon acutus, were successfully characterized using MALDI-TOF
 mass spectrometry in combination with sequential exoglycosidase
 digestion. Monosaccharide composition analysis was performed by high
 performance anion-exchange chromatography with pulsed amperometric
 detection (HPAEC-PAD). Galactose(Gal), mannose(Man), fucose(Fuc),
 N-acetylglucosamine (GlcNAc), and sialic acid (Neu5Ac) was detected
 and the total carbohydrate content was about 19.4% (w/w). The N-linked
 oligosaccharides were released by treatment with PNGase F, fluorescent
 labeled with 2-aminobenzamide, and fractionated by high performance
 liquid chromatography (HPLC). The main oligosaccharide fractions were
 collected and further digested with an array of exoglycosidase
 mixtures, and subsequent MALDI TOF MS analysis of the resulting
 products yielded information about structural features of the
 oligosaccharide. The combined data revealed the presence of five
 distinct oligosaccharide structures in Defibrase, which are mainly
 complex or hybrid type, with a small amount of oligomannosidic type.
 The complex type oligosaccharides are mostly tri-or bi-antennary and
 the hybrid oligosaccharides are all bi-antennary. Most
 oligosaccharides are also found to be fucosylated. (C) 2009 Elsevier
 Ltd. All rights reserved.
 SN 0041-0101
 PD FEB-MAR
 PY 2010
 VL 55
 IS 2-3
 BP 421
 EP 429
 DI 10.1016/j.toxicon.2009.09.007
 UT ISI:000274579100032
 PT J
 AU Fang, WR
 Deng, Y
 Li, YM
 Shang, EX
 Fang, F
 Lv, P
 Bai, L
 Qi, Y
 Yan, F
 Mao, LS
 AF Fang, Weirong
 Deng, Yan
 Li, Yunman
 Shang, Erxin
 Fang, Fang
 Lv, Peng
 Bai, Li
 Qi, Yan
 Yan, Fang
 Mao, Lishun
 TI Blood brain barrier permeability and therapeutic time window of
 Ginkgolide B in ischemia-reperfusion injury
 SO EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
 AB The goal of this study was to estimate the blood brain barrier (BBB)
 permeability of Ginkgolide B in normal condition and models of ischemia
 both in vivo and in vitro. A sensitive LC-MS/MS analytical method was
 developed to determinate accurately the concentration of Ginkgolide
 B in cell, plasma and brain tissue. The injured rat brain microvessel
 endothelial cells (RBMECs) induced by Na2S2O4 served as a
 hypoxia/reoxygenation model in vitro. Intracellular concentration of
 Ginkgolide B increased in injured cells in a concentration-dependent
 manner. As a model of in vivo-ischemia/reperfusion, we performed middle
 cerebral artery occlusion (MCAC)in rats. Concentration of Ginkgolide
 B in the brain tissues showed higher in cerebral ischemia-reperfused
 animals than that in normal rats. To evaluate potential clinical effect
 of Ginkgolide B, we determined therapeutic time window in MCAO rats.
 Up to i.v. administration at 2 h after reperfusion of rats, Ginkgolide
 B Could decrease infarction volume and brain edema, exerting
 significant protective effect in cerebral ischemia injury. In
 conclusion, Ginkgolide B could pass through BBB, especially after
 ischemia-reperfusion injury of brain, and might be therapeutically
 effective for ischemia/reperfusion injury of human brain. (C) 2009
 Elsevier B.V. All rights reserved.
 SN 0928-0987
 PD JAN 31
 PY 2010
 VL 39
 IS 1-3
 BP 8
 EP 14
 DI 10.1016/j.ejps.2009.10.002
 UT ISI:000274672300002
 PT J
 AU Zhao, L
 Zhen, C
 Wu, ZQ
 Hu, R
 Zhou, CL
 Guo, QL
 AF Zhao, Li
 Zhen, Chen
 Wu, Zhaoqiu
 Hu, Rong
 Zhou, Changlin
 Guo, Qinglong
 TI General pharmacological properties, developmental toxicity, and
 analgesic activity of gambogic acid, a novel natural anticancer agent
 SO DRUG AND CHEMICAL TOXICOLOGY
 AB In this article, the general pharmacological toxicity of gambogic acid
 (GA), a new anticancer agent, on the dog cardiovascular and respiratory
 system and the mouse central nervous system (CNS) were observed. The
 developmental toxicity and analgesic activities of GA were also
 investigated in rats and mice. Results showed that GA did not cause
 any toxic symptoms on blood pressure (i.e., mean arterial pressure),
 heart rate (HR), and respiratory frequency. However, a high dose of
 GA showed slight side effects on the mouse CNS. Further, evidence of
 maternal and developmental toxicity was observed in a dose-dependent
 manner. The maternal body-weight gain, as well as the birth weights
 and live birth index, were decreased significantly in the treatment
 groups. The inhibitory effects of GA on fetal skeletal development were
 also found. No obvious effects of GA on external alterations and
 visceral alterations were shown. In the analgesic experiments, GA
 showed significant analgesic activity in the acetic-acid-induced
 writhing study in a dose-dependent manner. This mechanism might be
 related to its anti-inflammation properties.
 SN 0148-0545
 PD JAN
 PY 2010
 VL 33
 IS 1
 BP 88
 EP 96
 DI 10.3109/01480540903173534
 UT ISI:000274742400012
 PT J
 AU Huang, DC
 Liu, W
 Zhao, SK
 Shi, YQ
 Wang, ZX
 Sun, YM
 AF Huang, D. C.
 Liu, W.
 Zhao, S. K.
 Shi, Y. Q.
 Wang, Z. X.
 Sun, Y. M.
 TI Quantitative design of seed load for solution cooling crystallization
 based on kinetic analysis
 SO CHEMICAL ENGINEERING JOURNAL
 AB Seed load of crystallization has a direct effect on the product
 qualities. To further reveal the effects of seed load on
 crystallization kinetics and improve the product size distribution,
 the aqueous solution of potassium nitrate (KNO3-H2O) is employed as
 a model system and the relevant kinetic experiments are conducted in
 a batch cooling crystallizer. The crystal nucleation and growth rate
 parameters are firstly estimated with the concentration and
 transmittance data using a mathematical model reported in our lab, and
 then the backward calculations with the help of the model parameters
 are successfully performed. It is found that the nucleation capacity
 decreases and growth capacity increases with increasing seed load, and
 the size distribution of crystal products tends to be more uniform.
 However, with the increasing of seed load, the linear growth rate of
 single crystal and the mean size of products both reduce accordingly.
 Based on the calculational and experimental results, a quantitative
 design scheme concerning seed load is proposed by further kinetic
 analyses, and the corresponding verification experiments are carried
 out. The results show that under the guidance of the proposed scheme,
 the size distribution of crystal products is more concentrated and the
 mean size of final particles can also escape from reducing obviously.
 (C) 2009 Elsevier B.V. All rights reserved.
 SN 1385-8947
 PD JAN 15
 PY 2010
 VL 156
 IS 2
 BP 360
 EP 365
 DI 10.1016/j.cej.2009.09.029
 UT ISI:000274771400017
 PT J
 AU Yu, YL
 Liu, L
 Wang, XT
 Liu, X
 Liu, XD
 Xie, L
 Wang, GJ
 AF Yu, Yunli
 Liu, Li
 Wang, Xinting
 Liu, Xiang
 Liu, Xiaodong
 Xie, Lin
 Wang, Guangji
 TI Modulation of glucagon-like peptide-1 release by berberine: In vivo
 and in vitro studies
 SO BIOCHEMICAL PHARMACOLOGY
 AB Glucagon-like peptide (GLP)-1 is a potent glucose-dependent
 insulinotropic gut hormone released from intestinal L cells. Our
 previous studies showed that berberine increased GLP-1 secretion in
 streptozotocin-induced diabetic rats. The aim of this study was to
 investigate whether berberine affected GLP-1 release in normal rats
 and in NCI-H716 cells. Proglucagon and prohormone convertase 3 genes
 regulating GLP-1 biosynthesis were analyzed by RT-PCR. Effects of
 pharmacological inhibitors on berberine-mediated GLP-1 release were
 studied. In vivo,5-week treatment of berberine enhanced GLP-1
 secretion induced by glucose load and promoted proglucagon mRNA
 expression as well as L cell proliferation in intestine. In vitro,
 berberine concentration-dependently stimulated GLP-1 release in
 NCI-H716 cells. Berberine also promoted both prohormone convertase 3
 and proglucagon mRNA expression. Chelerythrine (inhibitor of PKC)
 concentration-dependently suppressed berberine-mediated GLP-1
 secretion. Compound C (inhibitor of AMPK) also inhibited
 berberine-mediated GLP-1 secretion. But only low concentrations of H89
 (inhibitor of PKA) showed inhibitory effects on berberine-mediated
 GLP-1 release. The present results demonstrated that berberine showed
 its modulation on GLP-1 via promoting GLP-1 secretion and GLP-1
 biosynthesis. Some signal pathways including PKC-dependent pathway
 were involved in this process. Elucidation of mechanisms controlling
 berberine-mediated GLP-1 secretion may facilitate the understanding
 of berberine's antidiabetic effects. (C) 2009 Elsevier Inc. All rights
 reserved.
 SN 0006-2952
 PD APR 1
 PY 2010
 VL 79
 IS 7
 BP 1000
 EP 1006
 DI 10.1016/j.bcp.2009.11.017
 UT ISI:000274665800008
 PT J
 AU Chen, ND
 Zhang, J
 Liu, JH
 Yu, BY
 AF Chen, Nai-Dong
 Zhang, Jian
 Liu, Ji-Hua
 Yu, Bo-Yang
 TI Microbial conversion of ruscogenin by Gliocladium deliquescens
 NRRL1086: glycosylation at C-1
 SO APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
 AB The glycosylation of ruscogenin (1) by Gliocladium deliquescens NRRL
 1086 was observed and gave a regioselectively glycosylated product
 identified as ruscogenin 1-O-beta-D-glucopyranoside (2) by infrared,
 mass spectrometry, and nuclear magnetic resonance spectra. Time-course
 studies indicated that it appeared to be favorable to accumulate 2 when
 ruscogenin was added to the 24-h-old stage II culture, and the yield
 of 2 was about 20.1% during 120 similar to 168 h. It was noted that
 additional carbohydrates could significantly increase glycoside
 formation and the yield of 2 even reached as high as 68% compared with
 the control 20.1%. The primary investigation about the characteristics
 of the enzyme resulted that the reaction was blocked by
 beta-glycosidase inhibitor imidazole, however, was enhanced
 remarkably by glycosyltransferase inhibitor sodium dodecyl sulfate.
 To our knowledge, this is the first reported case of producing steroidal
 saponin by microbial transformation, and G. deliquescens NRRL1086
 would be a practical and highly efficient tool in producing natural
 ruscogenin monoside.
 SN 0175-7598
 PD MAR
 PY 2010
 VL 86
 IS 2
 BP 491
 EP 497
 DI 10.1007/s00253-009-2315-y
 UT ISI:000274707600008
 PT J
 AU Xie, SF
 Xiang, BR
 Deng, HS
 Wu, JF
 AF Xie, Shaofei
 Xiang, Bingren
 Deng, Haishan
 Wu, Jingfang
 TI Coupled stochastic resonance to improve chromatography determinations
 SO ANALYTICAL AND BIOANALYTICAL CHEMISTRY
 AB Traditional bistable stochastic resonance has been demonstrated as an
 effective tool to detect the weak signal in a strong noise background.
 To achieve a better signal-to-noise ratio for the output signal, a
 coupled stochastic resonance was developed by nonlinearly coupling two
 double-well potential systems. The response characteristics of coupled
 stochastic resonance subjected to analytical signals have been
 investigated and compared with those of bistable stochastic resonance.
 The improvement of chromatographic determination with the proposed
 coupled stochastic resonance was validated by both simulated signals
 and chromatographic signals. The weak signals from both simulated data
 and plasma samples with different concentrations were all amplified
 significantly and the quantitative relationship between different
 concentrations and responses was kept well. It is reasonable to believe
 that coupled stochastic resonance could play an important role in
 applications where quantitative determination of low-concentration
 samples is crucial.
 SN 1618-2642
 PD MAR
 PY 2010
 VL 396
 IS 5
 BP 1921
 EP 1927
 DI 10.1007/s00216-009-3350-3
 UT ISI:000274742900033
 PT J
 AU Zha, WB
 Liang, G
 Xiao, J
 Studer, EJ
 Hylemon, PB
 Pandak, WM
 Wang, GJ
 Li, XK
 Zhou, HP
 AF Zha, Weibin
 Liang, Guang
 Xiao, Jian
 Studer, Elaine J.
 Hylemon, Phillip B.
 Pandak, William M., Jr.
 Wang, Guangji
 Li, Xiaokun
 Zhou, Huiping
 TI Berberine Inhibits HIV Protease Inhibitor-Induced Inflammatory
 Response by Modulating ER Stress Signaling Pathways in Murine
 Macrophages
 SO PLOS ONE
 AB Background: HIV protease inhibitor (PI)-induced inflammatory response
 plays an important role in HIV PI-associated dyslipidemia and
 cardiovascular complications. This study examined the effect of
 berberine, a traditional herb medicine, on HIV PI-induced inflammatory
 response and further investigated the underlying cellular/molecular
 mechanisms in macrophages.
 Methodology and Principal Findings: Cultured mouse J774A.1 macrophages
 and primary mouse macrophages were used in this study. The expression
 of TNF-alpha and IL-6 were detected by real-time RT-PCR and ELISA.
 Activations of ER stress and ERK signaling pathways were determined
 by Western blot analysis. Immunofluorescent staining was used to
 determine the intracellular localization of RNA binding protein HuR.
 RNA-pull down assay was used to determine the association of HuR with
 endogenous TNF-alpha and IL-6. Berberine significantly inhibited HIV
 PI-induced TNF-alpha and IL-6 expression by modulating ER stress
 signaling pathways and subsequent ERK activation, in turn preventing
 the accumulation of the RNA binding protein HuR in cytosol and
 inhibiting the binding of HuR to the 3'-UTRs of TNF-alpha and IL-6 in
 macrophages.
 Conclusions and Significance: Inhibition of ER stress represents a key
 mechanism by which berberine prevents HIV PI-induced inflammatory
 response. Our findings provide a new insight into the molecular
 mechanisms of berberine and show the potential application of berberine
 as a complimentary therapeutic agent for HIV infection.
 SN 1932-6203
 PD FEB 9
 PY 2010
 VL 5
 IS 2
 AR e9069
 DI 10.1371/journal.pone.0009069
 UT ISI:000274442600004
 PT J
 AU Li, J
 Huang, WL
 Zhang, HB
 Zhou, HP
 AF Li, Jing
 Huang, Wenlong
 Zhang, Huibin
 Zhou, Huiping
 TI Synthesis and Preliminary COX-2 Expression Inhibitory Activities of
 Andrographolide Derivatives
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB The synthesis of a series of andrographolide derivatives was described
 and their inhibitory effects on COX-2 expression in mouse macrophages
 were also evaluated. Some of the tested compounds showed better
 inhibitory potency than andrographolide, and compound (5d) was the best
 one.
 SN 1570-1808
 PD MAR
 PY 2010
 VL 7
 IS 3
 BP 176
 EP 181
 UT ISI:000274432900005
 PT J
 AU Hamed, KH
 Hu, C
 Dai, DZ
 Yu, F
 Dai, Y
 AF Hamed, Khan Hussien
 Hu, Chen
 Dai, De-Zai
 Yu, Feng
 Dai, Yin
 TI CPU228, a derivative of dofetilide, relieves cardiac dysfunction by
 normalizing FKBP12.6, NADPH oxidase and protein kinase C epsilon in
 the myocardium
 SO JOURNAL OF PHARMACY AND PHARMACOLOGY
 AB Objectives The aim of this study was to determine if CPU228, a
 derivative of dofetilide, is more effective than dofetilide in
 attenuating isoproterenol-induced heart failure by recovering
 downregulated FK506 binding protein (FKBP12.6), and suppressing
 oxidative stress, upregulated NADPH oxidase and protein kinase C
 epsilon (PKC epsilon) hyperphosphorylation in the myocardium.
 Methods Heart failure was induced by isoproterenol (1 mg/kg s.c. for
 5 days) in male Sprague-Dawley rats. Intervention with either CPU228
 or dofetilide (2 mg/kg on Days 3-5) was then conducted in vivo and in
 vitro.
 Key findings Isoproterenol produced compromised left ventricular
 systolic pressure, left ventricular pressure rise (dp/dt(max)) and
 fall (dp/dt(min)), and left ventricular end-diastolic pressure,
 associated with oxidative stress, abnormal FKBP12.6, NADPH oxidase
 p67phox and PKC epsilon in the rnyocardium. CPU228 was more effective
 in attenuating these changes than dofetilide in vivo. Dofetilide
 produced a prolonged QTc to replace a shortened one. In primary neonatal
 cardiomyocytes, cultured with isoproterenol and treated with either
 CPU228 or dofetilide at 10(-8), 10(-7) and 10(-6) mol/l, isoproterenol
 produced a hyperadrenergic state characterized by downregulated
 FKBP12.6, upregulated NADPH oxidase p67phox and PKC epsilon in vitro.
 CPU228 was more effective than dofetilide in recovering these changes
 in a dose-dependent manner without a prolonged QTc.
 Conclusions CPU228 was more effective than dofetilide in attenuating
 heart failure by normalizing isoproterenol-induced changes, including
 downregulation of FKBP12.6, upregulation of NADPH oxidase and PKC
 epsilon hyperphosphorylation in vivo and in vitro.
 SN 0022-3573
 PD JAN
 PY 2010
 VL 62
 IS 1
 BP 77
 EP 83
 DI 10.1211/jpp/62.01.0008
 UT ISI:000274470700008
 PT J
 AU Xin, GZ
 Zhou, JL
 Qi, LW
 Li, CY
 Liu, P
 Li, HJ
 Wen, XD
 Li, P
 AF Xin, Gui-Zhong
 Zhou, Jian-Liang
 Qi, Lian-Wen
 Li, Chang-Yin
 Liu, Peng
 Li, Hui-Jun
 Wen, Xiao-dong
 Li, Ping
 TI Turbulent-flow chromatography coupled on-line to fast
 high-performance liquid chromatography and mass spectrometry for
 simultaneous determination of verticine, verticinone and isoverticine
 in rat plasma
 SO JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL
 AND LIFE SCIENCES
 AB A method based on the on-line turbulent-flow chromatography and fast
 high-performance liquid chromatography/mass spectrometry (TFC-LC/MS)
 was developed for sensitive and high throughput pharmacokinetic Study
 of traditional Chinese medicines (TCMs). In this method, an on-line
 extraction column (Waters Oasis HLB) and a fast HPLC Column with sub-2
 mu m particle size (Agilent Zorbax StableBond-C-18, 4.6 mm x 50 mm,
 1.8 mu m) in a column-switching set-up were utilized. HLB is a
 reversed-phase extraction column with hydrophilic-lipophilic balanced
 copolymer (2.1 mm x 20mm, 25 mu m particle size), which will exhibit
 some turbulent-flow properties at a high-flow rate. The method combines
 the speed and robustness of turbulent-flow extraction and the
 sensitivity and separation efficiency of fast HPLC-MS to analyze
 multiple and trace constituents of TCMs in plasma matrix. This method
 was successfully applied for pharmacokinetic Study of verticine,
 verticinone and isoverticine, the chemical markers of Fritillaria
 thunbergii, after oral administration of total steroidal alkaloids
 extract of F. thunbergii to rats. Each plasma sample was analyzed within
 7 min. The method demonstrated good linearity (R > 0.999) ranged from
 0.505 to 96.0 ng/mL with satisfactory accuracy and precision, and the
 lower limit of quantifications of verticine, verticinone and
 isoverticine were estimated to be 0.120. 0.595 and 0.505 ng/mL,
 respectively. These results indicate that the proposed method is fast,
 sensitive, and feasible for pharmacokinetic Study of TCMs. (C) 2009
 Elsevier B.V. All rights reserved.
 SN 1570-0232
 PD FEB 1
 PY 2010
 VL 878
 IS 3-4
 BP 435
 EP 441
 DI 10.1016/j.jchromb.2009.12.027
 UT ISI:000274414500022
 PT J
 AU Hong, J
 Jiao, Y
 Yan, JB
 He, WJ
 Guo, ZJ
 Zhu, LG
 Zhang, JF
 AF Hong, Jin
 Jiao, Yang
 Yan, Jianbin
 He, Weijiang
 Guo, Zijian
 Zhu, Longgen
 Zhang, Junfeng
 TI DNA cleavage promoted by trigonal-bipyramidal zinc(II) and copper(II)
 complexes formed by asymmetric tripodal tetradendate
 2-[bis(2-aminoethyl)amino]ethanol
 SO INORGANICA CHIMICA ACTA
 AB Asymmetric trigonal-bipyramidal Zn(II) complex 1 formed by
 2-[bis(2-aminoethyl) amino]ethanol (L) was found to be able to promote
 the cleavage of supercoiled plasmid DNA pBR322 to the nicked and linear
 DNA via a hydrolytic manner but only in neutral Tris-HCl buffer, no
 cleavage was observed in HEPES or NaH2PO4/Na2HPO4 buffer. However, the
 copper complex 2 of L, possessing the similar coordination geometry,
 can only promote DNA cleavage via an oxidative mechanism in the presence
 of ascorbic acid. ESI-MS study implies that complex 1 exist mainly as
 [Zn(L)](2+)/[Zn(L-H)](+) in neutral Tris-HCl buffer. Moreover, there
 is no discriminable species for complex 1 in HEPES or NaH2PO4/Na2HPO4
 buffer. A phosphate activation mechanism via phosphate coordinating
 to Zn(II) center of [Zn(L)](2+)/[Zn(L-H)](+) to form the stable
 trigonal-bipyramidal structure is proposed for the hydrolytic cleavage
 promote by complex 1. For complex 2, the abundance of [Cu(L)Cl](+) is
 higher than that of [Cu(L)](2+)/[Cu(L-H)](+) in Tris-HCl buffer. The
 lower phosphate binding/activating ability of Cu(II) in complex 2 may
 be the origin for its incapability to promote the hydrolytic DNA
 cleavage. However, the readily accessible redox potential of Cu(II)
 makes complex 2 promote the oxidative DNA cleavage. Although the DNA
 cleavage promoted by complex 1 has no specificity,
 trigonal-bipyramidal Zn(II) complexes formed by asymmetric tripodal
 polyamine with ethoxyl pendent should be a novel potential model for
 practical artificial nuclease. (C) 2009 Elsevier B. V. All rights
 reserved.
 SN 0020-1693
 PD MAR 1
 PY 2010
 VL 363
 IS 4
 BP 793
 EP 798
 DI 10.1016/j.ica.2009.12.004
 UT ISI:000274414700022
 PT J
 AU Chen, B
 Du, YX
 Wang, H
 AF Chen, Bin
 Du, Yingxiang
 Wang, Hao
 TI Study on enantiomeric separation of basic drugs by NACE in
 methanol-based medium using erythromycin lactobionate as a chiral
 selector
 SO ELECTROPHORESIS
 AB A wide variety of chiral selectors have been employed in CZE, and among
 them macrocyclic antibiotics including glycopeptides, ansamycins,
 aminoglycosides and polypeptides exhibited prominent enantioselective
 properties toward abundant racemic compounds. Compared with CZE, the
 use of macrocyclic antibiotic! as chiral selectors in NACE has not been
 reported previously. In this study, an approach to the
 enantioseparation of basic drugs by means of NACE with erythromycin
 lactobionate (EL) belonging to the group of macrolide antibiotics has
 been investigated. Especially different from the above four classes
 of antibiotics, there are no reports concerned with the use of
 macrolides which belong to macrocyclic antibiotics as chiral selectors
 in CE. In this work EL is first used as a chiral selector in NACE for
 the enantiomeric separations of two racemic basic drugs that possess
 high separability consisting of propranolol and duloxetine.
 Furthermore, EL possesses advantages such as high solubility and low
 viscosity in the solvent and very weak UV absorption. The chiral
 separations were achieved using Tris-boric acid as the BGE and methanol
 as the organic medium. In the course of this work we observed that both
 migration time and enantioseparation were influenced by several
 parameters such as the pH and composition of the BGE, EL concentration,
 capillary temperature and applied voltage. Consequently, these
 parameters were systematically optimized in order to obtain the optimum
 enantioseparations.
 SN 0173-0835
 PD JAN
 PY 2010
 VL 31
 IS 2
 BP 371
 EP 377
 DI 10.1002/elps.200900343
 UT ISI:000274431700013
 PT J
 AU Han, X
 Yan, M
 An, XF
 He, M
 Yu, JY
 AF Han, Xu
 Yan, Ming
 An, Xiao-fei
 He, Ming
 Yu, Jiang-yi
 TI Central administration of kisspeptin-10 inhibits natriuresis and
 diuresis induced by blood volume expansion in anesthetized male rats
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To investigate the possible role of hypothalamic kisspeptin in
 the regulation of body fluid metabolism and maintenance of internal
 homeostasis.
 Methods: Natriuresis and diuresis were induced by blood volume
 expansion (VE) in anesthetized male rats and kisspeptin-10 was
 intracerebroventricularly (icv) administered. Radioimmunoassay (RIA)
 was used to measure the plasma arginine vasopressin (AVP) and atrial
 natriuretic peptide (ANP) concentrations during the VE. The mediation
 of the renal sympathetic nerve was also investigated in rats with
 bilateral renal sympathetic denervation.
 Results: The increased urine flow and sodium excretion induced by VE
 were significantly inhibited by icv injection of 5 nmol kisspeptin-10
 (P < 0.05), which peaked 20 min after the decrease in VE. The mean
 arterial blood pressure and heart rate did not change during the
 experiment. Plasma AVP concentrations were significantly increased 20
 min after icv injection of 5 nmol kisspeptin-10 during VE (P < 0.05),
 while pretreatment with 5 nmol kisspeptin-10 did not significantly
 change plasma ANP concentrations. Furthermore, pretreatment with 5
 nmol kisspeptin-10 could significantly inhibit VE-induced natriuresis
 and diuresis in renal sympathetic denervated rats (P < 0.05).
 Conclusion: Central administration of kisspeptin-10 inhibited
 VE-induced natriuresis and diuresis. This effect was likely mediated
 by increasing AVP release independent of plasma ANP concentration and
 renal sympathetic nerve activity.
 SN 1671-4083
 PD FEB
 PY 2010
 VL 31
 IS 2
 BP 145
 EP 149
 DI 10.1038/aps.2009.179
 UT ISI:000274578400002
 PT J
 AU Qi, MY
 Feng, Y
 Dai, DZ
 Li, N
 Cheng, YS
 Dai, Y
 AF Qi, Min-you
 Feng, Yu
 Dai, De-zai
 Li, Na
 Cheng, Yu-si
 Dai, Yin
 TI CPU86017, a berberine derivative, attenuates cardiac failure through
 normalizing calcium leakage and downregulated phospholamban and
 exerting antioxidant activity
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To investigate whether CPU86017, a berberine derivative,
 attenuates heart failure by blocking calcium influx and exerting its
 antioxidant activity.
 Methods: Myocardial infarction was induced in male Sprague-Dawley rats
 for 17 d followed by isoproterenol (ISO) (5 mg/kg, sc) treatment for
 5 d to reduce cardiac function. The rats were divided into 5 groups:
 sham operation, myocardial infarction (MI), MI plus ISO, and co-treated
 (in mg/kg, po) with either propranolol (PRO, 10) or CPU86017 (80).
 Hemodynamic measurements were conducted, and measurements of the redox
 system, calcium handling proteins and endothelin (ET) system in vivo
 were done. Furthermore, calcium flux studies and PLB
 immunocytochemistry were conducted in vitro.
 Results: Compared to sham operation, HF was evident following MI and
 further worsened by ISO treatment. This occurred in parallel with
 downregulated mRNA and protein production of SERCA2a, PLB, and
 FKBP12.6, and was associated with upregulation of preproET-1,
 endothelin converting enzyme, and PKA mRNA production in the myocardium
 in vivo. Calcium leakage was induced by ISO treatment of isolated
 beating myocytes in vitro. These changes were attenuated by treatment
 with either PRO or CPU86017. PLB fluorescence in myocytes was
 downregulated by ISO treatment, and was relieved significantly by
 treatment with antioxidant aminoguanidine, ascorbic acid or CPU86017
 in vitro.
 Conclusion: HF, calcium leakage, downregulated PLB, FKBP12.6, SERCA2a
 production, and upregulated PKA were caused by ISO treatment, and were
 abolished by CPU86017 treatment. The beneficial effects of CPU86017
 are attributable to its antioxidant and calcium influx blocking
 effects.
 SN 1671-4083
 PD FEB
 PY 2010
 VL 31
 IS 2
 BP 165
 EP 174
 DI 10.1038/aps.2009.180
 UT ISI:000274578400005
 PT J
 AU Wang, W
 Wang, J
 Dong, SF
 Liu, CH
 Italiani, P
 Sun, SH
 Xu, J
 Boraschi, D
 Ma, SP
 Qu, D
 AF Wang, Wei
 Wang, Jing
 Dong, Sheng-fu
 Liu, Chun-hong
 Italiani, Paola
 Sun, Shu-hui
 Xu, Jing
 Boraschi, Diana
 Ma, Shi-ping
 Qu, Di
 TI Immunomodulatory activity of andrographolide on macrophage activation
 and specific antibody response
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To investigate the immunomodulatory effects of andrographolide
 on both innate and adaptive immune responses.
 Methods: Andrographolide (10 mu g/mL in vitro or 1 mg/kg in vivo) was
 used to modulate LPS-induced classical activated (M1) or IL-4-induced
 alternative activated (M2) macrophages in vitro and humor immune
 response to HBsAg in vivo. Cytokine gene expression profile (M1 vs M2)
 was measured by real-time PCR, IL-12/IL-10 level was detected by ELISA,
 and surface antigen expression was evaluated by flow cytometry, whereas
 phosphorylation level of ERK 1/2 and AKT was determined by Western blot.
 The level of anti-HBs antibodies in HBsAg immunized mice was detected
 by ELISA, and the number of HBsAg specific IL-4-producing splenocyte
 was enumerated by ELISPOT.
 Results: Andrographolide treatment in vitro attenuated either LPS or
 IL-4 induced macrophage activation, inhibited both M1 and M2 cytokines
 expression and decreased IL-12/IL-10 ratio (the ratio of M1/M2
 polarization). Andrographolide down-regulated the expression of
 mannose receptor (CD206) in IL-4 induced macrophages and major
 histocompability complex/costimulatory molecules (MHC I, CD40, CD80,
 CD86) in LPS-induced macrophages. Correspondingly, anti-HBs antibody
 production and the number of IL-4-producing splenocytes were reduced
 by in vivo administration of andrographolide. Reduced phosphorylation
 levels of ERK1/2 and AKT were observed in macrophages treated with
 andrographolide.
 Conclusion: Andrographolide can modulate the innate and adaptive
 immune responses by regulating macrophage phenotypic polarization and
 Ag-specific antibody production. MAPK and PI3K signaling pathways may
 participate in the mechanisms of andrographolide regulating macrophage
 activation and polarization.
 SN 1671-4083
 PD FEB
 PY 2010
 VL 31
 IS 2
 BP 191
 EP 201
 DI 10.1038/aps.2009.205
 UT ISI:000274578400008
 PT J
 AU Wu, GQ
 Liu, NF
 Van, XB
 Li, LX
 Zhang, C
 Gou, LX
 Liu, Z
 AF Wu Guo-Qiu
 Liu Nai-Feng
 Van Xiao-Bo
 Li Linxian
 Zhang Chen
 Gou Lixia
 Liu Zhao
 TI The Level of Connective Tissue Growth Factor in Sera of Patients with
 Hepatitis B Virus Strongly Correlates with Stage of Hepatic Fibrosis
 SO VIRAL IMMUNOLOGY
 AB Connective tissue growth factor (CTGF) plays a crucial role in the
 formation and development of hepatic fibrosis. The aim of this study
 was to establish a method for CTGF determination in order to investigate
 the level of CTGF in the sera of patients with hepatitis B virus, and
 to assess the correlation between CTGF concentration and stage of
 hepatic fibrosis. A CTGF C-terminal region gene was obtained by RT-PCR
 of human mesangial kidney cells and inserted into pET-32a((+)) vector.
 Recombinant protein was obtained by expression and purification of the
 fused protein. Polyclonal and monoclonal antibodies were prepared to
 establish a sandwich ELISA method. CTGF levels in 18 healthy serum
 samples and 83 serum samples from patients with hepatitis B virus were
 assessed. A simple, sensitive, and noninvasive method of determining
 CTGF levels was successfully established. CTGF levels in the sera of
 patients with hepatitis B were significantly increased compared
 controls (p<0.001). There was a strong correlation between CTGF
 concentration and fibrotic stage (r - 0.8906, p<0.005). No significant
 association was found between CTGF level and the grade of hepatic
 inflammation (p>0.05). The area under the receiver operating
 characteristic (ROC) curves of CTGF was 0.681 for identification of
 significant fibrosis, and 0.759 for the diagnosis of middle-and
 late-stage fibrosis. Accuracy of CTGF assessment was independent of
 age, renal function, liver function, platelet count, or other
 biochemical markers of liver fibrosis (all p>0.05). No significant
 correlation was found between CTGF and several humoral factors
 associated with liver fibrosis (all p>0.05). The levels of CTGF in the
 sera of patients with hepatitis B were strongly associated with the
 stages of hepatic fibrosis, and CTGF may become a useful diagnostic
 aid in assessing hepatic fibrosis.
 SN 0882-8245
 PD FEB
 PY 2010
 VL 23
 IS 1
 BP 71
 EP 78
 DI 10.1089/vim.2009.0067
 UT ISI:000274157900008
 PT J
 AU Zhou, QF
 Zhu, Y
 Tang, WF
 Lu, T
 AF Zhou, Qing-Fa
 Zhu, Yong
 Tang, Wei-Fang
 Lu, Tao
 TI Michael Addition-Lactonization Reaction of Electron-Deficient Alkynes
 with N-(Diphenylmethylene)glycinates: An Efficient Synthesis of
 3-Amino-2-pyrone Derivatives
 SO SYNTHESIS-STUTTGART
 AB A mild and efficient process for the synthesis of 3-amino-2-pyrone
 derivatives has been developed. This approach is based on the Michael
 addition of N-(diphenylmethylene)glycinates to various alkynyl
 ketones, followed by lactonization using 10 mol% sodium hydroxide as
 catalyst. Aromatic and aliphatic alkynyl ketones were converted into
 the corresponding 3-amino-2-pyrone derivatives in moderate to high
 yields. When methyl propiolate was submitted to the reaction,
 alpha,beta-dehydroamino acids were formed in good yields.
 SN 0039-7881
 PD JAN
 PY 2010
 IS 2
 BP 211
 EP 216
 DI 10.1055/s-0029-1217098
 UT ISI:000274245900004
 PT J
 AU Xin, MH
 You, QD
 Xiang, H
 AF Xin, Minhang
 You, Qidong
 Xiang, Hua
 TI An efficient, practical synthesis of 2-methoxyestradiol
 SO STEROIDS
 AB An efficient and practical scheme to synthesize 2-methoxyestradiol has
 been developed. The key step was the copper-mediated methoxylation
 using ethyl acetate as a co-catalyst to introduce a methoxyl group.
 These synthetic procedures of four steps from 17 beta-estradiol as
 starting material gave 2-methoxyestradiol with a 61% overall yield.
 (C) 2009 Elsevier Inc. All rights reserved.
 SN 0039-128X
 PD JAN
 PY 2010
 VL 75
 IS 1
 BP 53
 EP 56
 DI 10.1016/j.steroids.2009.09.013
 UT ISI:000274083000006
 PT J
 AU Jiang, C
 Zhang, XJ
 Shen, Z
 You, QD
 AF Jiang Cheng
 Zhang Xiaojin
 Shen Zheng
 You Qidong
 TI Kinesin Spindle Protein Inhibitors
 SO PROGRESS IN CHEMISTRY
 AB Inhibition of kinesin spindle protein (KSP) represents a novel and
 specific mechanism to target the mitotic spindle that may be devoid
 of the neuropathy-associated side effects common to the agents that
 target microtubules. Since the discovery of monastrol, the first
 selective small molecular inhibitor of KSP, many types of KSP
 inhibitors have been reported. In this review we describe the
 development of different types of KSP inhibitors. The structures and
 functions of KSP and the use of which as a novel target in the research
 of anticancer agents are introduced. The structure-activity
 relationship of some KSP inhibitors and the perspective of the study
 on KSP inhibitors are also discussed.
 SN 1005-281X
 PD JAN
 PY 2010
 VL 22
 IS 1
 BP 153
 EP 162
 UT ISI:000274279900019
 PT J
 AU Xia, CH
 Sun, JG
 Wang, GJ
 Shang, LL
 Zhang, XX
 Zhang, R
 Peng, Y
 Wang, XJ
 Hao, HP
 Xie, L
 Roberts, MS
 AF Xia, Chun-hua
 Sun, Jian-guo
 Wang, Guang-ji
 Shang, Li-li
 Zhang, Xiao-xuan
 Zhang, Rong
 Peng, Ying
 Wang, Xiao-jin
 Hao, Hai-ping
 Xie, Lin
 Roberts, Michael S.
 TI Herb-Drug Interactions: In Vivo and In Vitro Effect of Shenmai
 Injection, a Herbal Preparation, on the Metabolic Activities of Hepatic
 Cytochrome P450 3A1/2, 2C6, 1A2, and 2E1 in Rats
 SO PLANTA MEDICA
 AB Shenmai injection (SMI), a mixture of Radix Ginseng and Radix
 Ophiopogonis, is one of the most popular herbal medicinal products and
 is widely used for the treatment of coronary atherosclerotic
 cardiopathy and viral myocarditis. The purpose of this study was to
 investigate the effect of SMI, in vivo and in vitro, on the metabolic
 activities of hepatic cytochrome CYP450 3A1/2, 2C6, 2E1, and 1A2 in
 rats. After a single or multiple pretreatment with SMI, the rats were
 administrated intravenously a cocktail containing midazolam (1 mg/kg),
 diclofenac (0.5 mg/kg), theophylline (1 mg/kg), and chlorzoxazone (0.5
 mg/kg) as probe substrates of rat CYP450 3A1/2, 2C6, 1A2, and 2E1,
 respectively. Single and multiple SMI pretreatment to rats resulted
 in a rise of 33.8% (p < 0.01) and 25.6% (p < 0.01) in AUC for midazolam,
 and an increase in AUC for diclofenac by 14.7% (p < 0.05) and 31.2%
 (p < 0.01), respectively. However, the pharmacokinetics of
 chlorzoxazone and theophylline in rats was not altered markedly. In
 rat liver microsomes, linear mixed-type inhibition of SMI against the
 enzyme activities of CYP3A1/2, CYP2C6, and CYP1A2 was shown with IC50
 values of 3.3%, 2.0%, and 3.1% and K-i values of 3.8%, 1.5%. and 1.9%,
 respectively. These in vivo and in vitro results demonstrated that SMI
 had the potential to inhibit the activities of hepatic CYP3A1/2 and
 CYP2C6, but might not significantly affect CYP1A2 and CYP2E1-mediated
 metabolism in rats.
 SN 0032-0943
 PD FEB
 PY 2010
 VL 76
 IS 3
 BP 245
 EP 250
 DI 10.1055/s-0029-1186082
 UT ISI:000274392700007
 PT J
 AU Yang, M
 Xu, YP
 Pan, DH
 Din, H
 Wang, LZ
 Wang, GJ
 AF Yang, Min
 Xu, Yu-pin
 Pan, Dong-hui
 Din, Hong
 Wang, Li-zhen
 Wang, Guang-ji
 TI Potential of radioiodinated anticancer compounds of traditional
 Chinese medicine for cancer therapy
 SO JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
 AB 23-Hydroxybetulinic acid (23-HBA) is the efficient antitumor compound
 extracted from the roots of a Chinese Medicinal Herb, Pulsatilla
 chinensis (Bge) Regel. To evaluate the effect of radioiodination on
 cytotoxicity, 23-HBA was radioiodinated with I-125. I-125-23-HBA could
 be prepared in high yields and good radiochemical purity and was
 characterized using reverse phase HPLC. In ICR mice bearing Liver
 Cancer HepA tumor, I-125-23-HBA showed a tumor uptake of 2.1% ID/g at
 2 hp.i. and 0.15% ID/g at 48 hp.i on i.v. injection. When injected
 intratumorally, greater tumor uptake and retention was observed (20%
 ID/g at 2 hp.i. and 4.6% ID/g at 48 hp.i. respectively).
 SN 0236-5731
 PD JAN
 PY 2010
 VL 283
 IS 1
 BP 189
 EP 191
 DI 10.1007/s10967-009-0192-6
 UT ISI:000274333000026
 PT J
 AU Shen, Y
 Yin, C
 Su, MX
 Tu, JS
 AF Shen, Yan
 Yin, Chun
 Su, Mengxiang
 Tu, Jiasheng
 TI Rapid, sensitive and selective liquid chromatography-tandem mass
 spectrometry (LC-MS/MS) method for the quantification of topically
 applied azithromycin in rabbit conjunctiva tissues
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 AB A simple, rapid, sensitive and selective liquid chromatography-tandem
 mass spectrometry method was developed and validated for the
 quantification of azithromycin in rabbit conjunctiva tissues using
 roxithromycin as internal standard. Following a deproteinization
 procedure, the samples were eluted isocratically at a flow rate of 0.3
 mL/min utilizing a mobile phase containing of 10 mM ammonium acetate
 (adjusted pH to 5.2 with 0.1% acetic acid)-methanol (18:82, v/v) and
 a SHISEIDO CAPCELL PAK C-18 (3.0 mm x 75 mm, 3 mu m). Azithromycin and
 its internal standard were measured by a triple-quadrupole mass
 spectrometer in the selected reaction monitoring (SRM) mode with
 precursor-to-product qualifier transition m/z 375 [M+2H](2+) -> 591
 and m/z 837 [M+H](+) -> 679 respectively. The method demonstrated that
 good linearity ranged from 10 to 2000 ng/mL with r = 0.9998. The lower
 limit of quantification for azithromycin in conjunctiva tissues was
 10 ng/mL with good accuracy and precision. The intra- and inter-day
 precision (RSD) values were below 15% and accuracy (%) ranged from 90%
 to 110% at all QC levels. The method was applicable to ocular
 pharmacokinetic studies of azithromycin. (C) 2009 Elsevier B.V. All
 rights reserved.
 SN 0731-7085
 PD MAY 1
 PY 2010
 VL 52
 IS 1
 BP 99
 EP 104
 DI 10.1016/j.jpba.2009.12.001
 UT ISI:000274358900014
 PT J
 AU Zhao, Y
 Zhai, DS
 Chen, XJ
 Yu, QL
 He, H
 Sun, Y
 Gao, ZD
 Wang, L
 Wang, HH
 Han, DE
 Ji, H
 AF Zhao, Ying
 Zhai, Desheng
 Chen, Xijing
 Yu, Qiaoling
 He, Hui
 Sun, Ya
 Gao, Zidong
 Wang, Lei
 Wang, Huanhuan
 Han, De'en
 Ji, Hui
 TI Determination of Nimodipine in Human Plasma by HPLC-ESI-MS and Its
 Application to a Bioequivalence Study
 SO JOURNAL OF CHROMATOGRAPHIC SCIENCE
 SN 0021-9665
 PD FEB
 PY 2010
 VL 48
 IS 2
 BP 81
 EP 85
 UT ISI:000274116700001
 PT J
 AU Rao, YL
 Xiang, BR
 Bramanti, E
 D'Ulivo, A
 Mester, Z
 AF Rao, Yulan
 Xiang, Bingren
 Bramanti, Emilia
 D'Ulivo, Alessandro
 Mester, Zoltan
 TI Determination of Thiols in Yeast by HPLC Coupled with LTQ-Orbitrap Mass
 Spectrometry after Derivatization with p-(Hydroxymercuri)benzoate
 SO JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
 AB A liquid chromatography method with mass spectrometric detection has
 been developed for the simultaneous determination of six thiols in the
 sulfur metabolic pathway, including cysteine (Cys), homocysteine
 (HCys), glutathione (GSH), cysteinyl-glycine (Cys-Gly),
 gamma-glutamyl-cysteine (Glu-Cys), and S-adenosyl-homocysteine
 (AdoHcy). Tris(2-carboxyethyl)phosphine (TCEP) was used as the
 reducing reagent and p-(hydroxymercuri)benzoate (PHMB) as the
 derivatization reagent. Thiols were extracted from 3 mg of yeast using
 water in an ultrasonic bath. The absolute detection limits for the
 compounds studied were in the subpicomole range. It was found that
 AdoHcy, Cys, GSH, Cys-Gly, Glu-Cys, and very little HCys were present
 in the selenium-enriched yeast sample studied, and GSH, Glu-Cys, very
 little AdoHcy, Cys, and Cys-Gly were present in three bakery yeasts.
 SN 0021-8561
 PD FEB 10
 PY 2010
 VL 58
 IS 3
 BP 1462
 EP 1468
 DI 10.1021/jf903485k
 UT ISI:000274269000014
 PT J
 AU Liu, W
 Xie, ZH
 Zhang, BC
 Wang, Q
 Yao, WB
 Gao, XD
 Yu, LL
 AF Liu, Wei
 Xie, Zhuohong
 Zhang, Boce
 Wang, Qin
 Yao, Wenbing
 Gao, Xiangdong
 Yu, Liangli (Lucy)
 TI Effects of Hydroxypropylation on the Functional Properties of Psyllium
 SO JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
 AB The hydroxypropylated psyllium derivatives were successfully prepared
 with propylene oxide under the alkaline condition for the first time.
 Four hydroxypropylated psyllium derivatives, denoted as HP1, HP2, HP3,
 and HP4, were characterized for their hydroxypropyl content, molar
 substitution, and IR spectra. The hydroxypropyl derivatives were also
 evaluated for their surface structure, gelling properties, water
 uptake capacities, swelling volumes, and in vitro bile acid-binding
 abilities. The results showed that hydroxypropylation significantly
 reduced the gelling properties of psyllium. Psyllium derivatives with
 a relatively low hydroxypropyl substitution degree had greater in vitro
 binding capacities against cholic and chenodeoxycholic acids and
 higher swelling ability. The results from this study suggested that
 hydroxypropylation may be a possible approach for obtaining novel
 psyllium derivatives with improved physicochemical, functional, and
 biological properties for utilization in functional foods or
 supplemental and pharmaceutical products.
 SN 0021-8561
 PD FEB 10
 PY 2010
 VL 58
 IS 3
 BP 1615
 EP 1621
 DI 10.1021/jf903691z
 UT ISI:000274269000034
 PT J
 AU Yang, NY
 Xu, XH
 Ren, DC
 Duan, JA
 Xie, N
 Tian, LJ
 Qian, SH
 AF Yang, Nian-Yun
 Xu, Xiao-Hua
 Ren, Dong-Chun
 Duan, Jin-Ao
 Xie, Ning
 Tian, Li-Juan
 Qian, Shi-Hui
 TI Secoiridoid Constituents from the Fruits of Ligustrum lucidum
 SO HELVETICA CHIMICA ACTA
 AB Four new secoiridiod glucosides, p-hydroxyphenethyl
 7-beta-D-glucosideelenolic acid ester (1), 6'-elenolylnicotiflorine
 (2), 6'''-acetylnicotiflorine (3), and oleoside 7-ethyl 11-methyl
 ester (4), as well as six known glucosides, nuezhenide (5), GI-3 (6),
 nicotiflorine (7), isoneuzhenide (8), neonuezhenide (9), and oleoside
 11-methyl ester (10) were isolated from the fruits of Ligustrum
 lucidum. Their structures were elucidated by spectroscopic methods.
 Compound 4 was an artifact produced during extraction.
 SN 0018-019X
 PY 2010
 VL 93
 IS 1
 BP 65
 EP 71
 UT ISI:000274284000008
 PT J
 AU Guo, DL
 Huang, H
 Zhou, Y
 Xu, JY
 Jiang, H
 Chen, KX
 Liu, H
 AF Guo, Diliang
 Huang, He
 Zhou, Yu
 Xu, Jinyi
 Jiang, Hualiang
 Chen, Kaixian
 Liu, Hong
 TI Ligand-free iron/copper cocatalyzed N-arylations of aryl halides with
 amines under microwave irradiation
 SO GREEN CHEMISTRY
 AB Ligand-free iron/copper cocatalyzed cross-coupling reactions of aryl
 halides with amines were carried out to provide the corresponding
 coupling products in good yields. It is worth noting that the method
 displays a broad substrate scope, and is convenient, rapid, low-cost
 and environmentally friendly.
 SN 1463-9262
 PY 2010
 VL 12
 IS 2
 BP 276
 EP 281
 DI 10.1039/b917010c
 UT ISI:000274396800015
 PT J
 AU Yin, H
 Wang, Y
 Wang, Y
 Chen, T
 Tang, H
 Wang, M
 AF Yin, Hongping
 Wang, Ying
 Wang, Yufeng
 Chen, Tao
 Tang, Huiling
 Wang, Min
 TI Purification, Characterization and Immuno-Modulating Properties of
 Polysaccharides Isolated from Flammulina velutipes Mycelium
 SO AMERICAN JOURNAL OF CHINESE MEDICINE
 AB To investigate the immuno-modulating activity of Flammulina velutipes
 mycelium, three different Flammulina velutipes polysaccharides (FVPs)
 were isolated by fractionation using gel filtration and were identified
 as the immunomodulators of murine peritoneal macrophages. Based on the
 results of fourier transform infrared spectroscopy (FTIR), high
 performance liquid chromatography (HPLC), NMR spectroscopy,
 methylation analysis and gas chromatography-mass spectrogram (GC-MS),
 FVP2C was identified as glucose, galactose, mannose and fucose in molar
 ratio of 100: 14: 7: 4. FVP2C, molecular weight of 27.3 x 10(3) Da,
 was characterized as alpha-D-(1 -> 4)-glucan which was highly branched
 with alpha-D-(1 -> 6)-glucosyl residues, a single galactose or small
 amounts of mannoses and fucose at the C-6 position every twelve
 residues, on average, along the main chain. In the present study, it
 was found that three FVPs induced a significant increase in cellular
 nitric oxide formation, interleukin-1 production and tumor necrosis
 factor-alpha secretion in macrophages in vitro. The immuno-modulating
 activity of FVP2A, FVP2B and FVP2C was dose-dependent.
 SN 0192-415X
 PY 2010
 VL 38
 IS 1
 BP 191
 EP 204
 DI 10.1142/S0192415X10007750
 UT ISI:000274268300015
 PT J
 AU Tang, SS
 Du, MH
 Zhang, JH
 Kong, X
 Liu, JJ
 AF Tang, Song-Shan
 Du, Ming-Hua
 Zhang, Juan-Hui
 Kong, Xin
 Liu, Jing-Jing
 TI Structure and function relationships of three novel hGHRH-GGC analogs
 SO REGULATORY PEPTIDES
 AB Growth hormone releasing hormone (GHRH) is one of the hypothalamus
 hormones. For its potential applications in agriculture and medicine,
 GHRH analog with higher activity and longer half-life has been looked
 for. By using the fusion expression with unique acid labile linker
 Asp-Pro and biochemical purification, the three novel GHRH peptides,
 Pro-Pro-hGHRH(1-44)-Gly-Gly-Cys, Pro-hGHRH(1-44)-Gly-Gly-Cys, and
 (1)Pro-GHRH(2-44)-Gly-Gly-Cys, were obtained. The peptide molecular
 weight with 5,455, 5,373 or 5,210 Da measured by EIS-MS is coincident
 with the actual values. The peptides at 0.1-10 mu g/ml increased rat
 pituitary GH releases in a dose-dependent manner and at 5 mu g/ml
 increased human pituitary GH releases. The activity comparisons showed
 that at 10 mu g/ml there were significant between
 (1)Pro-hGHRH(2-44)-Gly-Gly-Cys and Pro-Pro-hGHRH(1-44)-Gly-Gly-Cys
 or Pro-hGHRH(1-44)-Gly-Gly-Cys, (1)Pro-hGHRH(2-44) (P<0.05). The
 (1)Pro-hGHRH(2-44)-Gly-Gly-Cys showed the highest GH release from rat
 pituitary. The activity results showed that the N-terminal Pro
 modulations and the C-terminal Gly-Gly-Cys extension regulate GH
 release from pituitary. The results showed that the three peptides had
 good GH release, function-selectivity and species specificity.
 Published by Elsevier B.V.
 SN 0167-0115
 PD JAN 8
 PY 2010
 VL 159
 IS 1-3
 BP 87
 EP 92
 DI 10.1016/j.regpep.2009.09.010
 UT ISI:000273920500014
 PT J
 AU Cheng, KG
 Wang, C
 Liu, J
 Xie, J
 Sun, HB
 AF Cheng, Keguang
 Wang, Chao
 Liu, Jun
 Xie, Juan
 Sun, Hongbin
 TI Synthesis and Evaluation of C-28 Oleanolic Acid Derivatives as
 Inhibitors of Glycogen Phosphorylase
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB Synthesis and evaluation of C-28 oleanolic acid derivatives as novel
 inhibitors of glycogen phosphorylase have been described. The results
 of glycogen phosphorylase inhibition assay and structure-activity
 relationship (SAR) analysis are also discussed.
 SN 1570-1808
 PD FEB
 PY 2010
 VL 7
 IS 2
 BP 116
 EP 121
 UT ISI:000274066100007
 PT J
 AU Qian, H
 Fu, ZX
 Zhang, HB
 Zhou, JP
 Huang, WL
 Jin, J
 Chen, W
 Dai, DY
 AF Qian, Hai
 Fu, Zhixian
 Zhang, Huibin
 Zhou, Jinpei
 Huang, Wenlong
 Jin, Jing
 Chen, Wei
 Dai, Dongyan
 TI Synthesis and Biological Evaluation of Capsaicin Derivatives as
 Analgesia Drugs
 SO LETTERS IN DRUG DESIGN & DISCOVERY
 AB TRPV1 is an important analgesia target. Capsaicin, the prototypical
 TRPV1 agonist, has a clear therapeutic potential. But the highly
 pungency limited its use. In this letter, for lowering its pungency,
 a series of capsaicin derivatives were designed and synthesized,
 including 10 compounds which were the direct combination of capsaicin
 and dihydro capsaicin with various NSAIDs. Preliminary biological
 tests suggested that some compounds had both anti-inflammatory
 activity and analgesic activity and their pungency was lower. Based
 on these results, some of these molecules can be considered as lead
 candidates for the further development of analgesic drugs.
 SN 1570-1808
 PD FEB
 PY 2010
 VL 7
 IS 2
 BP 122
 EP 127
 UT ISI:000274066100008
 PT J
 AU Chen, Y
 Lu, N
 Ling, Y
 Wang, L
 You, QD
 Li, ZY
 Guo, QL
 AF Chen, Yan
 Lu, Na
 Ling, Yun
 Wang, Ling
 You, Qidong
 Li, Zhiyu
 Guo, Qinglong
 TI LYG-202, a Newly Synthesized Flavonoid, Exhibits Potent
 Anti-angiogenic Activity In Vitro and In Vivo
 SO JOURNAL OF PHARMACOLOGICAL SCIENCES
 AB LYG-202 (C25H30N2O5) is a newly synthesized flavonoid that has been
 confirmed to possess an antitumor effect, but the mechanism is unclear.
 Our present study was performed to identify the anti-angiogenic
 activity of this novel compound in vitro and in vivo. LYG-202 inhibited
 vascular endothelial growth factor (VEGF) Stimulated migration and
 tube formation of human umbilical vein endothelial cells and arrested
 microvessel outgrowth from rat aortic rings in vitro. Meanwhile,
 LYG-202 suppressed the neovascularization of Chicken Chorioallantoic
 Membrane in vivo. Mechanistic studies revealed that LYG-202 suppressed
 the VEGF-induced tyrosine phosphorylation of KDR/Flk-1 (VEGFR-2) as
 well as its downstream protein kinases activation, by decreasing
 phosphorylated forms of serine/threonine kinase Akt, extracellular
 signal-regulated kinase, and p38 mitogen-activated protein kinase.
 LYG-202 exerts anti-angiogenic activity both in vitro and in vivo, and
 these results suggest that it deserves further investigation as a
 promising anti-tumor angiogenesis compound.
 SN 1347-8613
 PD JAN
 PY 2010
 VL 112
 IS 1
 BP 37
 EP 45
 DI 10.1254/jphs.09213FP
 UT ISI:000273997000008
 PT J
 AU Mi, XH
 Yu, HN
 Jia, P
 Zhang, ZZ
 Zhang, LY
 Liu, JZ
 AF Mi, Xuhua
 Yu, Haining
 Jia, Peng
 Zhang, Zhenzhou
 Zhang, Luyong
 Liu, Jingze
 TI Two tachykinin-like peptides from skin secretions of Danio rerio
 SO JOURNAL OF PEPTIDE SCIENCE
 AB Tachykinin perform multiple physiological functions such as smoothing
 muscle contraction, vasodilation, inflammation, the processing of
 nerve signal, neuroprotection and neurodegeneration. Two novel
 tachykinin-like peptides named tachykinin-DR1 and -DR2 were identified
 from skin secretions of Danio rerio in current work. Their amino acid
 sequences were determined as SKSQHFHGLM-NH2 and NKGEIFVGLM-NH2,
 respectively. They share a conserved FXGLM-NH2 C-terminal consensus
 motif. By cDNA cloning, the precursor encoding both tachykinin-DR1 and
 -DR2 was screened from the skin cDNA library of D. rerio. Tachykinin-DR1
 and -DR2 share the same precursor, which is composed of 108 amino acid
 (aa) residues. Regarding the biological activity, tachykinin-DRs could
 induce the contraction of isolated strips of guinea pig ileum just like
 other tackykinins. To our best knowledge, this is the first report of
 tachykinin from fish skin. Copyright (C) 2009 European Peptide Society
 and John Wiley & Sons, Ltd.
 SN 1075-2617
 PD FEB
 PY 2010
 VL 16
 IS 2
 BP 81
 EP 84
 DI 10.1002/psc.1194
 UT ISI:000273993200001
 PT J
 AU Liu, EH
 Qi, LW
 Cheng, XL
 Peng, YB
 Li, P
 AF Liu, E-Hu
 Qi, Lian-Wen
 Cheng, Xiao-Lan
 Peng, Yong-bo
 Li, Ping
 TI Simultaneous determination of twelve bioactive constituents in Buyang
 Huanwu decoction by HPLC-DAD-ELSD and HPLC-TOF/MS
 SO BIOMEDICAL CHROMATOGRAPHY
 AB Buyang Huanwu Decoction (BYHYD) is a classical traditional Chinese
 medicinal prescription that has been widely used for treating
 cerebrovascular illnesses for hundreds of years. In this study, a
 comprehensive analytical method has been developed for quantitative
 analysis of the major constituents in BYHWD. This method was based on
 high-performance liquid chromatography coupled to a diode array and
 evaporative light scattering detectors (HPLC-DAD-ELSD) on a common
 reverse-phase C-18 column. HPLC coupled with on-line time-of-flight
 mass spectrometry (HPLC-TOF/MS) was additionally adopted to provide
 further validation for the constituents. It was found that 0.3% aqueous
 formic acid and acetonitrile was the optimum mobile phase for gradient
 elution. This method, which showed excellent precision and accuracy,
 was successfully applied to quantify the bioactive constituents in six
 BYHWD products. The validated HPLC-DAD-ELSD method, together with the
 HPLC-TOF/MS analysis, provided a new basis for assessing the quality
 of traditional Chinese medicinal prescription consisting of many
 bioactive components. Copyright (C) 2009 John Wiley & Sons, Ltd.
 SN 0269-3879
 PD FEB
 PY 2010
 VL 24
 IS 2
 BP 125
 EP 131
 DI 10.1002/bmc.1269
 UT ISI:000273972600001
 PT J
 AU Xu, G
 Dou, J
 Zhang, L
 Guo, QL
 Zhou, CL
 AF Xu, Ge
 Dou, Jie
 Zhang, Lei
 Guo, Qinglong
 Zhou, Changlin
 TI Inhibitory Effects of Baicalein on the Influenza Virus in Vivo Is
 Determined by Baicalin in the Serum
 SO BIOLOGICAL & PHARMACEUTICAL BULLETIN
 AB Baicalein, an extract from Scutellaria baicalensis, was evaluated for
 its ability to inhibit the influenza virus in vivo. Oral administration
 of baicalein to BALB/c mice infected with the influenza
 A/FM1/1/47(H1N1) virus showed significant effects in preventing death,
 increasing the mean time to death, inhibiting lung consolidation, and
 reducing the lung virus titer in a dose-dependent manner. These effects
 are believed to be due to baicalin, the metabolite of baicalein in the
 serum. At a concentration of baicalin 2 mu g/ml in overlay medium, it
 showed significant inhibition in the plaque assay, and the mean IC50
 value of baicalin was calculated as 1.2 mu g/ml in the cytopathic effect
 assay. Our results showed that baicalein warrants further research as
 a potential antiinfluenza viral agent.
 SN 0918-6158
 PD FEB
 PY 2010
 VL 33
 IS 2
 BP 238
 EP 243
 UT ISI:000274005600013
 PT J
 AU Yang, YJ
 Song, DM
 Jiang, WM
 Xiang, BR
 AF Yang, Y. J.
 Song, D. M.
 Jiang, W. M.
 Xiang, B. R.
 TI RAPID RESOLUTION RP-HPLC-DAD METHOD FOR SIMULTANEOUS DETERMINATION OF
 SILDENAFIL, VARDENAFIL, AND TADALAFIL IN PHARMACEUTICAL PREPARATIONS
 AND COUNTERFEIT DRUGS
 SO ANALYTICAL LETTERS
 AB A novel and Rapid Resolution Reversed-Phase High-Performance Liquid
 Chromatography-Diode Array Detector method has been developed and
 validated for the simultaneous determination of sildenafil,
 vardenafil, and tadalafil in pharmaceutical preparations and
 counterfeit drugs. An Agilent Zorbax SB C8 column (50 x 4.6 mm i.d.,
 1.8 mu m particle size) was used. The mobile phase consisted of a mixture
 of 0.030 M of ammonium formate (adjusted to pH 3.0 with formic acid)
 and acetonitrile in the ratio 70:30. Ultraviolet (UV) detection was
 performed at 230 nm. Total run time was 7 min; these three drugs were
 eluted at the retention times of 1.654, 2.032, and 5.067 min for
 vardenafil, sildenafil, and tadalafil, respectively. The method was
 validated for accuracy, precision, linearity, specificity, and
 sensitivity. From the validation study, it was found that the method
 is specific, rapid, accurate, precise, and reproducible. Calibration
 curves were linear over the concentration ranges of 0.2-200 mu g ml(-1)
 for sildenafil, vardenafil, and tadalafil. The limits of detection
 (LOD) values were 1.0, 1.1, and 1.0 ng and the limit of quantification
 (LOQ) values were 2.0, 2.1, and 2.0 ng for sildenafil, vardenafil, and
 tadalafil, respectively. The method is rapid both for routine
 quantitative analysis of sildenafil, vardenafil, and tadalafil in
 pharmaceutical preparations and screening their suspected counterfeit
 drugs.
 SN 0003-2719
 PY 2010
 VL 43
 IS 3
 BP 373
 EP 380
 DI 10.1080/00032710903402283
 UT ISI:000274033200001
 PT J
 AU Dai, L
 Ji, H
 Kong, XW
 Zhang, YH
 AF Dai, Li
 Ji, Hui
 Kong, Xiang-wen
 Zhang, Yi-hua
 TI Antifibrotic effects of ZK(14), a novel nitric oxide-donating
 biphenyldicarboxylate derivative, on rat HSC-T6 cells and CCl4-induced
 hepatic fibrosis
 SO ACTA PHARMACOLOGICA SINICA
 AB Aim: To study the pharmacologic effect of ZK(14), a novel nitric
 oxide-donating biphenyldicarboxylate (DDB) derivative, on HSC-T6
 cells and on CCl4-induced hepatic fibrosis.
 Methods: Inhibition of HSC-T6 cell growth by ZK(14) was evaluated by
 MTT assay. The effect of ZK(14) on the percentage of HSC-T6 cells
 undergoing apoptosis was measured using Annexin-V/PI double-staining
 and TUNEL assay. Mitochondrial membrane potential (MMP) and caspase
 activities were tested. Hepatic fibrosis was induced in Sprague-Dawley
 rats by intraperitoneal injection with 14% CCl4. Rats with hepatic
 fibrosis were randomly divided into four groups: model control, ZK(14)
 (20 mg/kg), ZK(14) (10 mg/kg) and DDB (5 mg/kg). Levels of aspartate
 aminotransferase (AST), alanine aminotransferase (ALT), hyaluronic
 acid (HA), type III collagen (PCIII), and nitric oxide (NO) were
 assessed, and liver samples were stained with hematoxylin-eosin. The
 NO level in cells treated with ZK(14) in vitro was also measured.
 Results: The effect of ZK(14) on HSC-T6 cell apoptosis was
 concentration-and time-dependent, with up to 50% of cells becoming
 apoptotic when exposed to 100 mu mol/L ZK(14) for 18 h. ZK(14) treatment
 resulted in mitochondrial membrane depolarization and activation of
 caspases 3 and 9. At a dose of 20 mg/kg, ZK(14) significantly decreased
 serum transaminase (AST, ALT) activities and fibrotic index (HA, PCIII)
 levels and significantly inhibited fibrogenesis.
 Conclusion: These data indicate that ZK(14), a novel NO-donating DDB
 derivative, promotes HSC-T6 apoptosis in vitro through a signaling
 mechanism involving mitochondria and caspase activation and it
 inhibits CCl4-induced hepatic fibrosis in vivo. The results suggest
 that ZK(14) has potential therapeutic value in the treatment of hepatic
 fibrosis.
 SN 1671-4083
 PD JAN
 PY 2010
 VL 31
 IS 1
 BP 27
 EP 34
 DI 10.1038/aps.2009.170
 UT ISI:000273994600004
 PT J
 AU Liu, L
 Deng, YX
 Liang, Y
 Pang, XY
 Liu, XD
 Liu, YW
 Yang, JS
 Xie, L
 Wang, GJ
 AF Liu, Li
 Deng, Yuan-Xiong
 Liang, Yan
 Pang, Xiao-Yan
 Liu, Xiao-Dong
 Liu, Yao-Wu
 Yang, Jian-Song
 Xie, Lin
 Wang, Guang-Ji
 TI Increased Oral AUC of Baicalin in Streptozotocin-Induced Diabetic Rats
 due to the Increased Activity of Intestinal beta-Glucuronidase
 SO PLANTA MEDICA
 AB The purpose of the study was to investigate the pharmacokinetics of
 baicalin, a major bioactive component of Scutellariae radix, in
 diabetic conditions. The 4-week diabetic rats were induced by
 intraperitoneal administration of streptozotocin. Plasma
 concentrations of baicalin were measured following oral (200 mg/kg)
 or intravenous (12 mg/kg) administration. Everted intestinal
 transport, intestinal mucosal metabolism of baicalin and intestinal
 beta-glucuronidase activity were also investigated. It was found that
 the diabetic condition significantly increased the exposure of
 baicalin following oral doses (AUC 100.77 +/- 4.16 mu g . h/mL in
 diabetic rats vs. 48.48 +/- 7.94 mu g . h/mL in normal rats). In
 contrast, the diabetic condition significantly decreased the exposure
 of baicalin following intravenous doses (AUC 11.20 +/- 2.28 mu g . h/mL
 in diabetic rats vs. 18.02 +/- 3.45 mu g . h/mL in normal rats). We
 also found lower apparent permeability coefficients of baicalin in the
 ileum of diabetic rats (8.43 x 10(-6) +/- 2.40 x 10(-6) cm/s in diabetic
 rats vs. 5.21 x 10(-5) +/- 1.55 x 10(-5) cm/s in normal rats). Further
 studies showed that the diabetic condition enhanced the hydrolysis of
 baicalin to baicalein in intestinal mucosal, accompanied by an increase
 of beta-glucuronidase activity. All these results suggested that the
 higher oral exposure of baicalin in diabetic rats did not result from
 the decreased hepatic metabolism or increased intestinal absorption
 of baicalin. The enhancement of intestinal beta-glucuronidase activity
 may partly account for the higher exposure of baicalin in diabetic rats
 after oral administration.
 SN 0032-0943
 PD JAN
 PY 2010
 VL 76
 IS 1
 BP 70
 EP 75
 DI 10.1055/s-0029-1185946
 UT ISI:000273762100009
 PT J
 AU Huang, ZJ
 Zhang, YH
 Zhao, L
 Jing, YW
 Lai, YS
 Zhang, LY
 Guo, QL
 Yuan, ST
 Zhang, JJ
 Chen, L
 Peng, SX
 Tian, JD
 AF Huang, Zhangjian
 Zhang, Yihua
 Zhao, Li
 Jing, Yongwang
 Lai, Yisheng
 Zhang, Luyong
 Guo, Qinglong
 Yuan, Shengtao
 Zhang, Jianjun
 Chen, Li
 Peng, Sixun
 Tian, Jide
 TI Synthesis and anti-human hepatocellular carcinoma activity of new
 nitric oxide-releasing glycosyl derivatives of oleanolic acid
 SO ORGANIC & BIOMOLECULAR CHEMISTRY
 AB A series of nitric oxide (NO)-releasing glycosyl derivatives (2-14)
 of oleanolic acid were synthesized to improve the aqueous solubility
 and cytotoxicity of the parent compound 1. Derivative 3 exhibited
 better solubility and strong cytotoxicity against human hepatocellular
 carcinoma (HCC) in vitro. Furthermore, 3 displayed low acute toxicity
 to mice and significantly inhibited the growth of HCC tumors in vivo,
 indicating that 3 may be a promising candidate for the treatment of
 human HCC.
 SN 1477-0520
 PY 2010
 VL 8
 IS 3
 BP 632
 EP 639
 DI 10.1039/b918846k
 UT ISI:000273745100020
 PT J
 AU Li, J
 Yu, H
 Li, SA
 Wang, GJ
 AF Li, Juan
 Yu, Hua
 Li, Shuai
 Wang, Guang Ji
 TI Enhanced distribution and extended elimination of glycyrrhetinic acid
 in mice liver by mPEG-PLA modified (mPEGylated) liposome
 SO JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
 AB A rapid and simple method of high-performance liquid chromatography
 with UV detector for the quantification of glycyrrhetinic acid (GA)
 in mice plasma and tissues has been developed and validated. With the
 established assay method, the pharmacokinetic profiles and tissue
 distribution of GA in different formulations are compared in mice after
 intravenous administration of the drug(25 mg/kg). The results showed
 that mPEG-PLA modified (mPEGylated) GA liposome (PL-GA) significantly
 prolonged the mean residence time (MRT) of GA in mice plasma and liver
 (MRT: 0.43 +/- 0.13 and 1.72 +/- 0.11 h, respectively) than the normal
 GA liposome (L-GA) (MRT: 0.23 +/- 0.01 and 1.07 +/- 0.31 h,
 respectively) and GA sodium injection (S-GA) (MRT: 0.13 +/- 0.01 and
 0.95 +/- 0.08 h, respectively). Moreover, PL-GA specifically increased
 GA uptake in liver (AUC(0-infinity,) (liver) value of 1.6-fold and
 1.3-fold higher than that for S-GA and L-GA, respectively) and reduced
 its distribution into other tissues after dosing. Due to these
 pharmacokinetic properties, it may be promising to develop PL-GA
 further as a new pharmaceutical preparation for GA on the treatment
 of various chronic hepatic diseases. (C) 2009 Published by Elsevier
 B.V.
 SN 0731-7085
 PD APR 6
 PY 2010
 VL 51
 IS 5
 BP 1147
 EP 1153
 DI 10.1016/j.jpba.2009.11.005
 UT ISI:000273835100022
 PT J
 AU Wu, GQ
 Fan, XB
 Li, LX
 Wang, HL
 Ding, JX
 Wu, HB
 Zhao, R
 Gou, LX
 Shen, ZL
 Xi, T
 AF Wu, Guoqiu
 Fan, Xiaobo
 Li, Linxian
 Wang, Hailiang
 Ding, Jiaxuan
 Wu Hongbin
 Zhao, Rui
 Gou, Lixia
 Shen, Zilong
 Xi, Tao
 TI Interaction of antimicrobial peptide s-thanatin with
 lipopolysaccharide in vitro and in an experimental mouse model of
 septic shock caused by a multidrug-resistant clinical isolate of
 Escherichia coli
 SO INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
 AB s-thanatin, an analogue of thanatin, was synthesised by substituting
 the fifteenth amino acid threonine with serine and showed broad
 antimicrobial activity against Gram-negative and Gram-positive
 bacteria. To evaluate its antimicrobial activity against a
 multidrug-resistant (MDR) clinical isolate as well as its
 anti-endotoxin activity, its lipopolysaccharide (LPS)-binding and
 -neutralising activity in vitro and its therapeutic efficacy in an
 experimental model of septic shock caused by a MDR clinical isolate
 of Escherichia coli were studied. The ability of s-thanatin to bind
 or neutralise LPS from E. coli O111:B4 was determined using a
 quantitative assay kit. Male ICR mice were given an intraperitoneal
 (i.p.) administration of 2 x 1010 colony-forming units of E. coli
 E79466. Following bacterial challenge, all animals were randomised to
 receive i.p. administration of saline, 40 mg/kg ceftazidime (CAZ), or
 40 mg/kg CAZ + s-thanatin (10, 20 or 40 mg/kg). The results showed that
 s-thanatin not only completely bound to the LPS (median effective
 concentration of 17.5 mu g/mL) but also improved the survival and
 reduced the number of inoculated bacteria in a mouse model of septic
 shock. s-thanatin may be an attractive candidate to develop as an
 anti-MDR bacterial agent. (C) 2009 Elsevier B.V. and the International
 Society of Chemotherapy. All rights reserved.
 SN 0924-8579
 PD MAR
 PY 2010
 VL 35
 IS 3
 BP 250
 EP 254
 DI 10.1016/j.ijantimicag.2009.11.009
 UT ISI:000273720300007
 PT J
 AU Ni, SH
 Zhang, HB
 Huang, WL
 Zhou, JP
 Qian, H
 AF Ni, Shuai Han
 Zhang, Hui Bin
 Huang, Wen Long
 Zhou, Jin Pei
 Qian, Hai
 TI Solid phase synthesis of fatty acid modified glucagon-like peptide-1
 (7-36) amide under thermal and controlled microwave irradiation
 SO CHINESE CHEMICAL LETTERS
 AB Fatty acid modified glucagon-like peptide-1 (7-36) amide was
 synthesized efficiently on Rink-Amide-MBHA resin by
 microwave-assisted solid phase method. The method of thermal and
 controlled microwave irradiation provided impressive enhancements in
 product yield, selectivity, and reaction rate. The coupling time was
 dramatically decreased to 6 min, and the desired products were obtained
 in high yield and purity. (C) 2009 Wen Long Huang. Published by Elsevier
 B.V. on behalf of Chinese Chemical Society. All rights reserved.
 SN 1001-8417
 PD JAN
 PY 2010
 VL 21
 IS 1
 BP 27
 EP 30
 DI 10.1016/j.cclet.2009.08.007
 UT ISI:000273898200007
 PT J
 AU Ji, JF
 Zhang, HB
 Huang, WL
 Qian, H
 Zhou, JP
 AF Ji, Jian Feng
 Zhang, Hui Bin
 Huang, Wen Long
 Qian, Hai
 Zhou, Jin Pei
 TI A convenient synthesis of ezetimibe analogs as cholesterol absorption
 inhibitors
 SO CHINESE CHEMICAL LETTERS
 AB A convenient method for the synthesis of ezetimibe analogs as
 cholesterol absorption inhibitors was described. The key step in the
 synthesis was the intramolecular ring formation through Mitsunobu
 reaction. Furthermore, a new series of analogs was designed and
 synthesized. (C) 2009 Wen Long Huang. Published by Elsevier B.V. on
 behalf of Chinese Chemical Society. All rights reserved.
 SN 1001-8417
 PD JAN
 PY 2010
 VL 21
 IS 1
 BP 67
 EP 69
 DI 10.1016/j.cclet.2009.08.009
 UT ISI:000273898200017
 PT J
 AU Geng, D
 Shi, Y
 Min, ZD
 Liang, JY
 AF Geng, Di
 Shi, Yao
 Min, Zhi Da
 Liang, Jing Yu
 TI A new diterpenoid from Euphorbia helioscopia
 SO CHINESE CHEMICAL LETTERS
 AB A new jatrophane-type diterpenoid, 7 beta,14 beta,15 beta-triacetoxy-3
 beta-benzoyloxy-9-oxojatropha-5E,11E-diene, named euphornin N was
 isolated from Euphorbia helioscopia L. The structure and relative
 stereochemistry of the new compound was elucidated by spectroscopic
 methods. (C) 2009 Jing Yu Liang. Published by Elsevier B.V. on behalf
 of Chinese Chemical Society. All rights reserved.
 SN 1001-8417
 PD JAN
 PY 2010
 VL 21
 IS 1
 BP 73
 EP 75
 DI 10.1016/j.cclet.2009.09.013
 UT ISI:000273898200019
 PT J
 AU Nie, W
 Luo, JG
 Kong, LY
 AF Nie, Wei
 Luo, Jian-Guang
 Kong, Ling-Yi
 TI New triterpenoid saponins from the roots of Gypsophila pacifica Kom.
 SO CARBOHYDRATE RESEARCH
 AB Six new triterpenoid saponins (1-6) have been isolated from the roots
 of Gypsophila pacifica Kom. Their structures were established on the
 basis of extensive NMR (H-1, C-13, TOCSY, HSQC, and HMBC) and ESIMS
 studies. (C) 2009 Published by Elsevier Ltd.
 SN 0008-6215
 PD JAN 11
 PY 2010
 VL 345
 IS 1
 BP 68
 EP 73
 DI 10.1016/j.carres.2009.08.015
 UT ISI:000273865100010
 PT J
 AU Hou, FZ
 Zhuang, JJ
 Bian, CH
 Tong, TJ
 Chen, Y
 Yin, J
 Qiu, XJ
 Ning, XB
 AF Hou, Fengzhen
 Zhuang, Jianjun
 Bian, Chunhua
 Tong, Tangji
 Chen, Ying
 Yin, Jie
 Qiu, Xiaojun
 Ning, Xinbao
 TI Analysis of heartbeat asymmetry based on multi-scale time
 irreversibility test
 SO PHYSICA A-STATISTICAL MECHANICS AND ITS APPLICATIONS
 AB We investigate the asymmetry of heart rate control system and suggest
 a simple index to quantify this asymmetry by performing
 high-dimensional time irreversibility tests to heartbeat interval time
 series over Multiple scales. The results provide strong evidence to
 the concept that the asymmetry is an intrinsic property of heart rate
 control system. As a simple and visual method, it is proved to be
 effective in classifying physiologic and synthetic subjects while the
 maximum scale is selected within a proper range, and also provides a
 new way to analyze the time irreversibility for other high-dimensional
 systems. (C) 2009 Elsevier B.V. All rights reserved.
 SN 0378-4371
 PD FEB 15
 PY 2010
 VL 389
 IS 4
 BP 754
 EP 760
 DI 10.1016/j.physa.2009.10.003
 UT ISI:000273694300012
 PT J
 AU Liu, WY
 Feng, F
 Yu, CX
 Xie, N
 AF Liu, Wen-Yuan
 Feng, Feng
 Yu, Cheng-Xia
 Xie, Ning
 TI Qualitative and Quantitative Analysis of the Main Constituents of Radix
 Ilicis Pubescentis by LC-Coupled with DAD and ESI-MS Detection
 SO NATURAL PRODUCT COMMUNICATIONS
 AB A sensitive and selective high performance liquid chromatographic
 method coupled with DAD detection is presented for quality control of
 Radix Ilicis Pubescentis. By means of this analytical procedure the
 major individual constituents (ilexoside O, ilexgenin A, ilexsaponin
 A,, ilexsaponin B-1, liriodendin and acanthoside B) could be quantified
 simultaneously. LC-ESI-MS was applied for identification of the six
 compounds in the plant by comparing their m/z value and retention times
 with those of selected standards. For quantitative analysis, the
 extraction procedure and the extraction solvent were optimized in order
 to ensure the exhaustive extraction of the plant material. The HPLC
 conditions were evaluated and optimized for the exact quantification
 of all six individual compounds. Chromatographic separation was
 carried out on a C-18 column using gradient elution with acetonitrile
 and 0.1% phosphoric acid as the mobile phase. Detection was carried
 out using a photodiode array detector. The calibration curves for
 determination of the six constituents showed good linearity over the
 investigated ranges (r(2)>0.999). Measurement of intra-day and
 inter-day variability (expressed as RSD value) was conducted to assess
 precisions of the method, and RSD (%) of intra- and inter-day variation
 were between 1.56-3.36% and 1.61-3.58%, respectively. The recoveries
 of the six compounds were between 96.4-102.2%, with RSD (%) values
 ranging from 1.7-3.8%. These validation results demonstrated the
 suitability of the method for the precise and accurate determination
 of the main constituents in Radix Ilicis Pubescentis. The method was
 successfully applied for quality evaluation of 12 batches of Radix
 Ilicis Pubescentis obtained from different regions of southern China.
 The contents of the six major constituents varied significantly due
 to their different origins, which can be used as an aid to assessing
 the quality of Radix Ilicis Pubescentis.
 SN 1934-578X
 PD JAN
 PY 2010
 VL 5
 IS 1
 BP 23
 EP 26
 UT ISI:000273519200006
 PT J
 AU Lu, XY
 Chen, YD
 Sun, NY
 Jiang, YJ
 You, QD
 AF Lu, Xiao-Yun
 Chen, Ya-Dong
 Sun, Ni-yue
 Jiang, Yong-Jun
 You, Qi-Dong
 TI Molecular-docking-guided 3D-QSAR studies of substituted
 isoquinoline-1,3-(2H,4H)-diones as cyclin-dependent kinase 4 (CDK4)
 inhibitors
 SO JOURNAL OF MOLECULAR MODELING
 AB The cyclin-dependent kinases (CDKs) are critical regulators of cell
 cycle progression, and are involved in uncontrolled cell
 proliferation-a hallmark of cancer. This suggests that small molecular
 inhibitors of CDKs might be attractive as prospective antitumor agents.
 To explore the relationship between the structures of substituted
 isoquinoline-1,3-(2H, 4H)-diones and their inhibition of CDK4, 3D-QSAR
 studies were performed on a dataset of 48 compounds. The bioactive
 conformation of template compound 34 was obtained by performing
 molecular docking into the ATP binding site of the homology model of
 CDK4 and ranking by highest consensus score, which was then used to
 build and align the rest of the molecules in the series. The constructed
 comparative molecular similarity indices analysis (CoMSIA) produces
 significantly better results than comparative molecular field analysis
 (CoMFA), with r(cv)(2) = 0.707 and r(2) = 0.988. The contours analysis
 provides useful information about the structural requirements for
 substituted isoquinoline-1,3-(2H, 4H)-diones for CDK4 inhibitory
 activity.
 SN 1610-2940
 PD FEB
 PY 2010
 VL 16
 IS 2
 BP 163
 EP 173
 DI 10.1007/s00894-009-0529-7
 UT ISI:000273668800001
 PT J
 AU Sun, RH
 Zheng, H
 Fang, ZZ
 Yao, WB
 AF Sun, Renhua
 Zheng, Heng
 Fang, Zhengzhi
 Yao, Wenbing
 TI Rational design of aminoacyl-tRNA synthetase specific for
 p-acetyl-L-phenylalanine
 SO BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
 AB The Methanococcus jannaschii tRNA(Tyr)/tyrosyl-tRNA synthetase pair
 has been engineered to incorporate unnatural amino acids into proteins
 in Escherichia coli site-specifically In older to acid other unnatural
 amino acids into proteins by this approach. the amino acid binding site
 of M jannaschn tyrosyl-tRNA synthetase need to be mutated The crystal
 structures of M.jannaschii tyrosyl-tRNA synthetase and Its maturation
 were determined, which provided all opportunity to design
 aminoacyl-tRNA synthetases specific for Unnatural amino acids In our
 Study. we attempted to design aminoacyl-tRNA synthetases being able
 to deliver p-acetyl-L-phenylalanine into proteins
 p-Acetyl-L-phenylalanine was Superimposed oil tyrosyl in M jannaschn
 tyrosyl-tRNA synthetase-tyrosine complex Tyr32 needed to be changed
 to non-polar amino acid with shorter side chain, Val, Leu, Ile, Gly
 or Ala, in order to reduce steric clash and provide hydrophobic
 environment to acetyl oil p-acetyl-L-phenylalanine Asp158 and Ile 159
 Would be changed to specific amino acids for the same reason So we
 designed 60 aminoacyl-rRNA synthetases. Binding of these
 aminoacyl-tRNA synthetases with p-acetyl-L-phenylalanine indicated
 that only 15 of them turned Out to be able to bind
 p-acetyl-L-phenylalanine with reasonable poses Binding affinity
 computation proved that the mutation of Tyr32Leu and Asp158Gly
 benefited p-acetyl-L-phenylalanine binding And two of the designed
 aminoacyl-tRNA synthetases had considerable binding affinities. They
 seemed to be very promising to be able to incorporate
 p-acetyl-L-phenylalanine into proteins in E coli The results show that
 the combination of homology modeling and molecular docking is a
 feasible method to filter inappropriate mutations in molecular design
 and Point out beneficial Mutations (C) 2009 Elsevier Inc All rights
 reserved
 SN 0006-291X
 PD JAN 1
 PY 2010
 VL 391
 IS 1
 BP 709
 EP 715
 DI 10.1016/j.bbrc.2009.11.125
 UT ISI:000273624500124
 PT J
 AU Wu, XD
 Sun, LX
 Zha, WB
 Studer, E
 Gurley, E
 Chen, L
 Wang, X
 Hylemon, PB
 Pandak, WM
 Sanyal, AJ
 Zhang, LY
 Wang, GJ
 Chen, J
 Wang, JY
 Zhou, HP
 AF Wu, Xudong
 Sun, Lixin
 Zha, Weibin
 Studer, Elaine
 Gurley, Emily
 Chen, Li
 Wang, Xuan
 Hylemon, Phillip B.
 Pandak, William M., Jr.
 Sanyal, Arun J.
 Zhang, Luyong
 Wang, Guangji
 Chen, Jie
 Wang, Jian-Ying
 Zhou, Huiping
 TI HIV Protease Inhibitors Induce Endoplasmic Reticulum Stress and
 Disrupt Barrier Integrity in Intestinal Epithelial Cells
 SO GASTROENTEROLOGY
 AB BACKGROUND & AIMS: Human immunodeficiency virus (HIV) protease
 inhibitor (PI)-induced adverse effects have become a serious clinical
 problem. In addition to their metabolic and cardiovascular
 complications, these drugs also Frequently cause severe
 gastrointestinal disorders, including mucosal erosions, epithelial
 barrier dysfunction, and diarrhea. However, the exact mechanisms
 underlying gastrointestinal adverse effects of HIV Pis remain unknown.
 This study investigated whether HIV Pis disrupt intestinal epithelial
 barrier integrity by activating endoplasmic reticulum (ER) stress.
 METHODS: The most commonly used HIV Pis (lopinavir, ritonavir, and
 amprenavir) were used; their effects on ER stress activation and
 epithelial paracellular permeability were examined in vitro as well
 as in vivo using wild-cype and CHOP-/- mice. RESULTS: Treatment with
 lopinavir and ritonavir, but not amprenavir, induced ER stress, as
 indicated by, I decrease in secreted alkaline phosphatase activities
 and an increase in the unfolded protein response. This activated ER
 stress partially impaired the epithelial barrier integrity by
 promoting intestinal epithelial cell apoptosis. CHOP silencing by
 specific small hairpin RNA prevented lopinavir- and ritonavir-induced
 barrier dysfunction In Cultured intestinal epithelial cells, whereas
 CHOP-/- mice exhibited decreased mucosal injury after exposure to
 lopinavir and ritonavir. CONCLUSIONS: HIV PIs induce ER stress and
 activate the unfolded protein response in intestinal epithelial cells,
 thus resulting in disruption of the epithelial barrier integrity.
 SN 0016-5085
 PD JAN
 PY 2010
 VL 138
 IS 1
 BP 197
 EP 209
 DI 10.1053/j.gastro.2009.08.054
 UT ISI:000273427700030
 PT J
 AU Lu, XY
 Chen, YD
 You, QD
 AF Lu, Xiao-Yun
 Chen, Ya-Dong
 You, Qi-Dong
 TI 3D-QSAR Studies of Arylcarboxamides with Inhibitory Activity on InhA
 using Pharmacophore-Based Alignment
 SO CHEMICAL BIOLOGY & DRUG DESIGN
 AB Enoyl acyl carrier protein reductase (InhA) is a promising target for
 the development of antituberculosis drugs. The InhA-bound conformation
 of an indole-5-amide inhibitor (Genz 10850) (PDB code: IP44) was used
 to build a pharmacophore model by LigandScout. This model was then
 successfully used to identify the bioactive conformation and align 40
 structurally diverse arylcarboxamide derivatives. Comparative
 molecular field analysis (CoMFA) and comparative molecular similarity
 indices analysis (CoMSIA) were performed on arylcarboxamides-based
 InhA inhibitors based on pharmacophore alignment. The best prediction
 was obtained with CoMSIA model combining steric and electrostatic
 fields (r(cv)(2) = 0.729, r(2) = 0.972). The model was validated by
 an external test set, which gave a good predictive value (r(pred)(2)
 = 0.826). Graphical interpretation of the results revealed important
 structural features of the zarylcarboxamides related to the active site
 of InhA. The results may be exploited for further design and virtual
 screening for some novel InhA inhibitors.
 SN 1747-0277
 PD FEB
 PY 2010
 VL 75
 IS 2
 BP 195
 EP 203
 DI 10.1111/j.1747-0285.2009.00926.x
 UT ISI:000273396900007