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    Recent progress in the research on lamellarins and related pyrrole-derived alkaloids from marine organisms
    Ai-Li Fan, Wen-Han Lin, Yan-Xing Jia *
       DOI: 10.5246/jcps.2011.05.054
    Abstract1434)      PDF (1033KB)(901)       Save
    Lamellarins and related pyrrole-derived alkaloids are a large family of marine alkaloids with novel structures and promising bioactivities. They have been isolated from diverse marine organisms and all of them feature a 3,4-diarylpyrrole 2-carboxylic acid ester or amide moiety. This article provides an overview of recent literatures on lamellarins and related pyrrole-derived alkaloids, including their isolation, total synthesis, biological and structure activity relationship (SAR) studies.
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    Cited: Baidu(331)
    Protective effects of icariin on human umbilical vein endothelial cell injured by angiotensin II
    Qiu-Juan Wang *, Zhi-Wei Pan, Yu Wang, Juan Yang, Ying Jia, Ling-Yi Kong
    Abstract1391)      PDF (670KB)(534)       Save

    To investigate the effects of icariin (ICA) on angiotensin II(Ang II)-induced injury in human umbilical vein endothelial cells line (ECV-304). The ECV-304 cells were cultured in vitro. After 24 h incubating with icariin, the model of AngII-induced injury in ECV-304 was established. The cell viability (MTT method), Lactate dehydrogenase (LDH) release and Nitric oxide (NO) production in the medium, the capacity of scavenging superoxide anion radicals (O2·–) and hydroxyl radicals (·OH) were measured. The activities of superoxide dismutase (SOD), total nitric oxide synthase (T-NOS), inducible nitric oxide synthase (iNOS) and constitutive nitric oxide synthase (cNOS) in the cells were determined. Compared with the Ang II-treated group, ICA can significantly raise the viability of EC, increase the activities of SOD, T-NOS and cNOS, increase the production of NO, enhance the capacity of scavenging superoxide anion radicals (O2·–) and hydroxyl radicals(·OH), and lower LDH leakage and iNOS activity. The results suggest that ICA can protect endothelial cells (ECV-304) from Ang II-induced injury.

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    Effects of PVP K30 on Aqueous Solubility and Dissolution Properties of Daidzein
    GUO Sheng-rong *, GUO Li
    Abstract1820)      PDF (389KB)(884)       Save
    Aim To study effects of PVP K30 on the aqueous solubility and dissolution properties of daidzein. Methods To measure the aqueous solubility and dissolution rates of daidzein in three different states (within solid dispersions, physical mixtures and as a pure drug) and investigate drug-polymer interactions in the solid state using X-ray powder diffraction and fourier-transform infrared spectroscopy. Results The negative values of the Gibbs free energy and enthalpy of transfer explained the spontaneous transfer of daidzein from phosphate buffer solution (PBS) to a solution of PVP in PBS.X-ray powder diffraction patterns showed that the drug was in the amorphous state (ratio of the drug:PVP<1:5) when dispersed in PVP K30.The infrared spectra indicated there exist interactions between the OH of daidzein and the C=O of PVP K30. Conclusion the dispersion of daidzein in PVP K30 considerably enhances the solubility and dissolution rate.
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    Cited: Baidu(73)
    Kiridine, A C18-Diterpene Alkaloid from Aconitum kirinense
    Feng Feng, Ye Wencai, Liu Jinghan, Zhao Shouxun, Ian D. Williams, Che Chuntao
    Abstract1225)      PDF (264KB)(564)       Save
    Kiridine, a new C 18 -diterpenoid alkaloid, was isolated from the roots of Aconitum kirinense. Its structure was elucidated by MS, 1D- and 2D- NMR, and mono-crystal X-ray analysis. It is the first norditerpene alkaloid containing a 9,14-methylenedioxy group and the substituent at C-14 is β-configuration.
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    Cited: Baidu(66)
    A Novel Minor Saponin from the Leaves of Panax Ginseng. C. A. Meyer
    De-Qing Dou *, Ying-Jie Chen, Zhong-ZeMa, Ye Wen, Min-Hua weng, Yu-Ping Pei, Zhi-Xue Wang, Hiroyki, Hideaki, Yasvnobu Murakami
    Abstract952)      PDF (318KB)(472)       Save
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    Cited: Baidu(61)
    Three Anthraquinones Isolated from Aster tataricus L.f
    LU Yan-hua, WANG Zheng-tao *, XU Luo-shan, WU Zi-bin
    Abstract216)      PDF (343KB)(877)       Save
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    Cited: Baidu(55)
    HPLC Determination of Harpagoside and Cinnamic Acid in Radix Scrophulariae
    Xie Lihua, Liu Hongyu, Xu Bingjiu, Wang Xuan, Wang Jianhua, Xu Feng, Cai Shaoqing
    Abstract1314)      PDF (258KB)(999)       Save
    A gradient HPLC method was established for the determination of harpagoside and cinnamic acid in Radix Scrophulariae (Xuanshen) and a proposition was put forward for the lowest content of the characteristic and active constituent (harpagoside) for qualified Radix Scrophulariae. The experimental conditions were as follows: Ultrasphere ODS column (250 mm × 4.6 mm, 5 mm), mobile phase: acetonitrile-water (containing 1.0% acetic acid) (20:80→50:50) (20 min), flow-rate 1 mL·min-1, room temperature, detection wavelength 278 nm. Twenty-eight samples of Xuan-shen (Radix Scrophulariae) from different districts of China were analyzed and the contents of harpagoside and cinnamic acid in Xuan-shen were 0.041~0.244% and 0.012~0.068% respectively. The recoveries (±RSD)% were 97.13(±0.80)% for harpagoside and 99.38(±0.51)% for cinnamic acid. The method is simple and accurate. It can be used for the quality control of Radix Scrophulariae. We propose that the content of harpagoside in qualified Radix Scrophularia should be no less than 0.05%.
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    Cited: Baidu(52)
    FDA approves weight-management drug Contrave
    Journal of Chinese Pharmaceutical Sciences    2014, 23 (9): 662-662.  
    Abstract210)   HTML98)    PDF (406KB)(120)       Save
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    Cited: Baidu(50)
    Effects of Matrine on Aconitine-Induced Electrophysiological Changes in Rat Ventricular Myocytes
    SHAN Hong-li, YANG Bao-feng *, ZHOU Yu-hong, WANG He, LI Bao-xin
    Abstract213)      PDF (407KB)(728)       Save
    Aim To explore the reason that the antiarrhythmic effect of the extract of traditional Chinese medicinal herb, matrine, is weaker than quinidine and verapamil by comparision of the effect and efficacy of matrine on various kinds of transmembrane ionic currents with those of quinidine and verapamil; and to demonstrate the best targets for antiarrhythmic drugs. Methods Whole-cell patch-clamp techniques were used to record the action potential and ionic currents in single cells of rat ventricular myocytes. Aconitine was used to induce the changes of ionic currents, then study the effects of matrine and quinidine, verapamil on aconitine-induced imbalanced channel currents and action potential. Results Aconitine 1 μmol·L -1 induced significant changes in transmembrane currents and action potential in single cells of rat ventricular myocytes. APD was significantly prolonged by aconitine. Simultaneously, aconitine increased sodium, L-type calcium and inward rectifier potassium currents. Matrine 100 μmol·L -1 reversed the aconitine-induced changes of sodium current (INa) from (-70.2±10.5) pA/pF to (-39.6±4.0) pA/pF (n=5, P<0.05 vs aconitine); L-type calcium current (ICa-L) from (20.4±3.8) pA/pF to (-12.9±2.9) pA/pF (n=6, P<0.01); the inward rectifier potassium current (Ik1) from (-32.2±1.08) pA/pF to (-24.0±3.4) pA/pF (n=6, P<0.01), and action potential duration. The reversal effects of quinidine and verapamil on aconitine-induced changes of APD and ionic currents were more marked than matrine. Conclusion Aco-nitine significantly disturbs the normal equilibrium of ion channels in ventricular myocytes. It induces changes of INa, ICa-L, Ik1 and prolongation of action potential duration. Matrine at concentration 50 or 100 μmol·L-1 statistically significantly suppresses aconitine-induced changes of APD and ionic currents. The potency and efficacy of inhibitory effect of matrine are markedly weaker than those of commonly used verapamil and quinidine.
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    Cited: Baidu(49)
    Pharmacokinetics of Scutellarin in Dogs
    LI Su-hua, JIANG Xue-hua *, LAN Ke, YANG Jun-yi, ZHOU Jing
    Abstract1866)      PDF (360KB)(594)       Save
    Aim To establish an RP-HPLC method for the determination of scutellarin in plasma and study its pharmacokinetics in dogs. Methods Scutellarin was given to dogs by intravenous injection and determined by RP-HPLC, the mean plasma concentration-time curve was plotted and pharmacokinetic parameters were calculated by program 3p87. Results The concentration-time curve of scutellarin could be fitted to three-compartment model with T 1/2pi , T 1/2α and T 1/2β being 1.05±0.80 min, 6.99±2.76 min and 51.61±28.78 min, respectively, V c being 880.1±508.3 mL, CL being 189.6±53.8 mL·min -1 , and AUC 0-90 and AUC 0-∞ being 574.43±133.95 μg·min·mL -1 and 599.34±132.00μg·min·mL -1 , respectively. Conclusion The fact that the concentrations of scutellarin in plasma declined rapidly after the medication suggested that the T 1/2 of scutellarin should be taken into account in drug administration and preparation development.
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    Cited: Baidu(44)
    Preliminary Study of Dual Characteristics of Antioxidation and Prooxidation of Flavonoids
    Lu Jingfen, Li Ting, Jin Duo, Shen Chuanyong, Wang Kui, Yin Junjie
    Abstract805)      PDF (615KB)(517)       Save
    Flavonoids were comparatively studied as the scavengers of hydroxyl and superoxide flee radicals by means of spin trapping-electron spin resonance(ESR) method. The relative activity is related to molecular structures, i.e., the number and position of hydroxyl groups. With molecular modeling and quantum chemistry calculation methods, the relationships were also revealed from the structural analysis of the flavonoids and the products of their single electron oxidation. The spin labeling ESR results indicate that some flavonoids Can influence the conformation of membrane protein, which is likely due to oxidative damage. Both antioxidation and prooxidation characteristics of flavdnoids are worth further studying in detail.
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    Cited: Baidu(44)
    Studies on Chemical Constituents of Dendrobium chryseum
    Guo-Xiang Ma, Tian-Shan Wang *, Li Yin, Yang Pan, Guo-Jun Xu, Luo-Shan Xu
    Abstract1113)      PDF (291KB)(649)       Save
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    Cited: Baidu(41)
    Metabolism of Shikonin in Rats
    Li Huiyi, Luo Shurong, Zhou Tonghui
    Abstract197)      PDF (547KB)(502)       Save
    The metabolism of shikonin in rats was studied. Shikonin was administered (i.p.) to healthy, male Wistar rats pretreated with phenobarbital (PB, i.p., 60 mg·kg-1, once a day, 3 d) by asingle dose of 20 mg·kg-1, urine and bile were collected. The bile and urine samples wererespectively hydrolyzed with β-glucuronidase, extracted with ethyl acetate and the extractive concentrated in vacuum. The residues were dissolved in methanol and analyzed by a RP-HPLC/DADsystem for identification of shikonin metabolites. It has been proved that shikonin is metabolizedvery fast in the body and the metabolites are excreted mainly throngh the bile. The chromatograms and spectra showed that there were ten shikonin metabolites with similar UV spectra in the bile andurine respectively. The difference between in vivo and in vitro metabolic profiles of shikonin wasalso discussed.
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    Cited: Baidu(39)
    Synthesis of Hydroxyethylene-based β-Secretase Inhibitors
    YANG Xiao-ming, ZOU Xiao-min, FU Yi-qiu, MOU Ke, XU Ping *
    Abstract817)      PDF (350KB)(648)       Save
    Aim To discuss in depth the synthesis of hydroxyethylene dipeptide-based β-secretase inhibitors; Methods Organic reactions such as nucleophilic addition and substitution assisted by organometallic agents, catalytic hydrogenation, and classic peptide coupling were used to synthesize peptidomimetic β-secretase inhibitors. Results Ideal reaction conditions and potential problems were investigated, and one of the designed β-secretase inhibitors 13 (as a model) was synthesized successfully; Conclusion This approach might be used to build up the β-secretase inhibitor library and to search for new molecular candidates.
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    Cited: Baidu(39)
    A New Fluorenone Derivative from Dendrobium Chrysotoxum
    Guo-Xiang Ma **, Zheng-Tao Wang ***, Luo-Shan Xu, Guo-Jun Xu
    Abstract1188)      PDF (342KB)(793)       Save
    A new fluorenone derivative, named chrysotoxone (3) was isolated from the ethanolic extract of the stems of Dendrobium chrysotoxum (Orchidaceae), along with three known compounds. The structure of the new fluorenone was elucidated as 2,5,8-trihydroxy-1,4-dimethoxy-9-fluorenone.
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    Cited: Baidu(35)
    Trichostatin A Induces Apoptosis by Inhibiting Telomerase Activity and Expression of Telomerase Reverse Transcriptase in HL-60 Cells
    ZHOU Yong-ming, GUO Wei, ZHOU Hao, LI Hui-yu, LIU Li-qiong, YAO Jun-xia, ZHENG Jin-e, GUO Tian-nan, HUANG Shi-ang *
    Abstract2204)      PDF (455KB)(485)       Save
    Aim To investigate the effects of trichostatin A (TSA) on telomerase activity and the expression of human telomerase reverse transcriptase (hTERT) during apoptosis in vitro and the mechanisms in HL-60 cells. Methods The proliferative activity of HL-60 cells was assessed by MTT assay. Cell apoptosis was analyzed by flow cytometry. Telomerase activity was examined by TRAP-ELISA. The expression of telomerase subunits was analyzed by RT-PCR. Results A time- and dose-dependent inhibition was detected in HL-60 cells treated with TSA. After treatment with 600 nmol·L -1 TSA for 48 h, the apoptosis rate in HL-60 cells was 42.6% and telomerase activity decreased 1.95±0.25, 1.73±0.12 and 1.52±0.09 for 12, 24 and 48 h, respectively. The expression of hTERTmRNA decreased. No significant changes were observed in the expression of hTRmRNA and hTP1mRNA. Conclusion TSA inhibits telomerase activity and induces apoptosis in HL-60 cells. The underlying mechanism may be related to the down-regulation of hTERT transcription.
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    Cited: Baidu(33)
    Improvement of Similarity Measure: Pearson Product-Moment Correlation Coefficient
    LIU Yong-suo, MENG Qing-hua, CHEN Rong, WANG Jian-song, JIANG Shu-min, HU Yu-zhu *
    Abstract1090)      PDF (375KB)(744)       Save

    Aim To study the reason of the insensitiveness of Pearson product-moment correlation coefficient as a similarity measure and the method to improve its sensitivity. Methods Experimental and simulated data sets were used. Results The distribution range of the data sets influences the sensitivity of Pearson product-moment correlation coefficient. Weighted Pearson product-moment correlation coefficient is more sensitive when the range of the data set is large. Conclusion Weighted Pearson product-moment correlation coefficient is necessary when the range of the data set is large.

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    Cited: Baidu(32)
    Effects of Breviscapine on the Changes in Antioxidant Enzyme Activity Induced by Cerebral Ischemia-reperfusion in Rats
    Xiao-Xia Chen, Bing He
    Abstract1248)      PDF (302KB)(447)       Save
    Effects of breviscapine, the active ingredient isolated from Erigeron breviscapus (Vant) Hand-mazz, on the changes in antioxidant enzyme activity induced by cerebral ischemia-reperfusion in rats were explored. It was found that breviscapine improved the activities of superoxide dismutase (SOD), GSH-peroxidase and catalase, while decreasing the malondialdehyde (MDA) content in the brain, which was benificial in reducing the damage from cerebral ischemia-reperfusion.
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    Cited: Baidu(32)
    Preparation of Bovine Serum Albumin Microspheres by an Acetone-ethanol Heat Denaturation Method
    Lin He, Guo-Qiang Chen *, Ying-Jie Lu, Jin-Chun Chen
    Abstract896)      PDF (434KB)(574)       Save
    Stable sub 500 nm bovine serum albumin (BSA) microsphere suspensions were produced by controlled addition of acetone and ethanol to an aqueous solution of BSA, followed by stabilization process of the formed microspheres at an elevated temperature. Microspheres produced by this acetone-ethanol heat denaturation method were stabilized at relatively low temperatures (70~75 º C) over a short period of time (20 min). The acetone-ethanol heat denaturation method, in comparison with the traditional oil/water technique for preparation of albumin microspheres, which requires high temperature (over 100 º C) and longer heating time (more than 30 min) for stabilization, offers a number of advantages. This report describes the influence of process conditions, such as ratios of acetone to ethanol to BSA aqueous solution, heating time and heating temperature, on microsphere formation and their stability. A loading efficiency of 40% rose bengal was achieved. Rose bengal release rates from these microspheres in phosphate buffered saline medium at 37 º C were dependent on microsphere stabilities and 25% to 60% of initial loading drug were released in 15 days.
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    Cited: Baidu(31)
    Homoerydictyl-7-O-β-D-glycoside-A Receptor Antagonist of Platelet-activating Factor (PAF)
    Guan Zengwei, Wang Yinye, Yang Xiuwei, Cui Yuxin
    Abstract838)      PDF (255KB)(565)       Save
    Homoeriodictyl-7-O-β-D-glycoside, a flavonoid compound isolated from the Chinese medicinal herb, viscum coloratum inhibited platelet aggregation induced by platelet-activating factor(PAF), but it had no inhibitory activity on adenosine diphosphate-induced platelet aggregation. In the present study, we intended to get an insight into the mechanism of its anti-PAF action. Using [ 3 H]PAF receptor binding assay we found that the compound exhibited inhibitory activity. The inhibitory rate was 18.5%, 28.4%, 58.7%, 78% and 78%, respectively, at concentrations of 10 -8 , 10 -7 , 10 -6 , 10 -5 and 10 -4 mol·L -1 , There was a visible dose-effect relationship as well as a correlation between different concentrations and their inhibitory rates (γ = 0.985, P<0.05) when the dose was equal to or less than 1×10 -5 mol·L -1 , and its IC 50 was 8.0×10 -7 mol·L -1 . The inhibitory rate didn't increase with increasing concentration of the compound when it went beyond 1×10 -5 mol·L -1 indicating competitive inhibition of binding of [ 3 H]PAF to PAF receptor reached saturation.
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    Cited: Baidu(30)
    The Activity of Erianin and Chrysotoxine from Dendrobium chrysotoxum to Reverse Multidrug Resistance in B16/h MDR-1 Cells
    Guo-Xiang Ma *, Gerald A. LeBlanc
    Abstract211)      PDF (302KB)(496)       Save
    The ability of two dihydrostilbene derivatives erianin and chrysotoxine from Dendrobium chrysotoxum to reverse multidrug resistant (MDR) cells was investigated using murine B16 melanoma cells transfected with the human MDR-1 gene and crossresistant to vinblastine and adriamycin (B16/h MDR-1 cells). Both of the two compounds were shown to increase the accumulation of adriamycin, the P-glycoprotein (P-gp) substrate, in B16/h MDR-1 transfectants.
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    Cited: Baidu(30)
    Interaction Between Gatifloxacin and Bovine Serum Albumin
    YAN Zheng-yu *, SHAO Xiu-fen, YAN Lin, HU Yu-zhu
    Abstract1835)      PDF (320KB)(676)       Save
    Aim To study the reaction mechanism between gati fl oxacin and bovine serum albumin (BSA) at different pHs. Methods Fluorescence spectra and UV absorbance spectra were used. Results The binding constants were determined from a double reciprocal Lineweaver- Burk curves at different pHs. The binding distance r under normal physiologi cal condition was obtained according to Foster theory of non-radiative energy transfer. The binding force between gatifloxacin and BSA was inferred by thermody namical coordination. Conclusion The interaction between gatifl oxacin and BSA seems to be strong and the main binding force is electrostatic fo rce.
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    Cited: Baidu(29)
    Application of L-Cys-Capped CdS Nanoparticles in Determination of Nucleic Acid by Resonance Light-Scattering Technique
    DAI Mei-ling, YAN Zheng-yu *, QU Ping, SHAO Xiu-fen
    Abstract1798)      PDF (474KB)(606)       Save
    Aim To determine nucleic acid (DNA) using Nanometer-sized L-cysteine-capped CdS particles by resonance light scattering (RLS) method. Methods The nano-particles synthesized by a colloidal aqueous method were water-soluble, stable, and highly luminescent. The RLS of L-Cys-CdS particles were greatly quenched by DNA in Tris-HCl solutions. The intensity of RLS at 344 nm was proportional to the concentration of DNA. Results The linearity range of the calibration curve was 0.01-1.0 μg·mL -1 for calf thymus DNA and 0.04-1.5 μg·mL -1 for salmon sperm DNA. The detection limits (3 δ) were 8 ng·mL -1 for calf thymus DNA and 10 ng·mL -1 for salmon sperm DNA. Conclusion This method is simple, sensitive, and capable of avoiding the use of toxic dyes.
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    Cited: Baidu(29)
    Chemical synthesis and biological activities of Securinega alkaloids
    Wen Zhang, Jun-Yong Li, Ping Lan, Ping-Hua Sun, Ying Wang, Wen-Cai Ye, Wei-Min Chen *
       DOI: 10.5246/jcps.2011.03.026
    Abstract1687)      PDF (1037KB)(1033)       Save
    The Securinega alkaloids are a group of compounds isolated from the plants of Securinega, Phyllanthus and Flueggea genera belonging to the Euphorbiaceae family. Most of these compounds exhibit a wide range of biological activities, such as GABA receptor antagonist, antimalarial and antibacterial activity. Due to the special structural features of Securinega alkaloids, the synthesis strategies for their different structural skeletons are challenging for organic and medicinal chemists. In the review, we will provide an overview of the total synthesis of several Securinega alkaloids and their biological activities.
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    Cited: Baidu(27)
    Chemistry of the Chinese herbal medicine Puerariae Radix (Ge-Gen): A review
    Wei Song, Yanjiao Li, Xue Qiao, Yi Qian, Min Ye
    Journal of Chinese Pharmaceutical Sciences    2014, 23 (6): 347-360.   DOI: 10.5246/jcps.2014.06.048
    Abstract518)   HTML78)    PDF (955KB)(1088)       Save
    Puerariae Radix (Ge-Gen in Chinese) is a popular traditional Chinese herbal medicine derived from the dried roots of Pueraria lobata (Willd.) Ohwi or P. thomsonii Benth. It shows significant pharmacological activities in the treatment of cardiovascular diseases, hypertension, and diabetes. This review summarizes progress in the chemistry study of Pueraria species, mainly covering the classes of flavonoids, puerosides, coumarins, triterpenoids, and triterpene saponins. Qualitative and quantitative chemical analyses are also covered.
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    Cited: Baidu(25)
    A New Quinazolone Alkaloid from Leaves of Dichroa febrifuga
    Deng Yonghong, Xu Rensheng, Ye Yang *
    Abstract1792)      PDF (253KB)(993)       Save
    A new alkaloid, neodichroine, along with several known alkaloids, a coumarin, a flavanone and vanillin were isolated from leaves of Dichroa febrifuga. Its structure was elucidated by spectral analyses and semi-synthesis from β -dichrone.
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    Cited: Baidu(25)
    Survey on Natural Radiosensitizing Agents Since 2000
    LU Jia, SHAO Hong *
    Abstract741)      PDF (364KB)(659)       Save
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    Cited: Baidu(23)
    New Tannins from Lythrum Salicaria L.
    Xiu-Jing Ma *, Chun-Ru Ji, Yu-Ming Wang, Guang-Qiang Zhang, Yan-Ze Liu
    Abstract688)      PDF (241KB)(472)       Save
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    Cited: Baidu(23)
    Ocotillone-type Ginsenoside from Leaves of Panax ginseng
    Dou Deqiang, Chen Ying, Ren Jie, Pei Yuping, Chen Yingjie *
    Abstract861)      PDF (337KB)(520)       Save
    An ocotillone-type ginsenoside, together with 2 known ginsenosides was isolated from leaves of Panax ginseng and identified as pseudoginsenoside RT5 on the basis of chemical and physicochemical evidences. It has been so far the first example of ocotillone type ginsenoside discovered in Panax ginseng and its plausible biotransformation pathway also discussed.
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    Cited: Baidu(22)
    Synergistic effect of pinellia total alkaloids and uncaria total alkaloids on anticonvulsant action in mice and rats
    Yin-Xia Cheng, Ming-Zheng Wang *, Jing-Jing Chen, Rong Yang, Xin-Gu He,
    Yong-Gang Ma, Li-Hua Yang, Ming-Sheng Zhang
    Abstract2336)      PDF (732KB)(1272)       Save

    Aim To investigate the synergistic effect of the combination of pinellia total alkaloid (PTA) and uncaria total alkaloid (UTA), and explore the mechanism of anticonvulsant action. Methods Anticonvulsant and toxic effect profiles of combinations of PTA with UTA, alone and at three fixed ratios of 1:4, 1:1, 4:1, were evaluated in maximal electroshock (MES)-induced seizures and acute toxicity test in mice. Respective ED50 and LD50 were calculated with Bliss’s method. Their synergistic effect were evaluated by isobolographic analysis and allowed the determination of benefit indices (BI) for respective combinations. The model of convulsive rats kindled by penicillin topically injected into cortex was used to investigated the content of Glu, Asp, Gly and GABA in hippocampus using high performance liquid chromatography (HPLC). Results Combinations of PTA and UTA at the ratio of 4:1 were synergistic in MES test and antagonistic in acute toxicity test, showing the best profile for combinations of PTA with UTA. In contrast, the ratios of 1:4 and 1:1, despite synergistic in MES test, were additive in acute toxicity test. The 4:1 combination and two drugs alone significantly decreased Glu level and increased GABA level in the hippocampusbut the GABA level in the 4:1 combination group was higher than that in the two drugs alone groups. They did not have significant influence on the levels of Asp and Gly. Conclusion Combinations of PTA and UTA at 4:1 ratio demonstrated synergistic effect in anticonvulsant action and antagonistic effect in toxicity. The anticonvulsant mechanism might be related to decreasing the excitability of Glutamatergic neurons and increasing the inhibition of GABAergic neurons.

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    Cited: Baidu(21)
    Protective Effect of Tetrandrine and Fructose-1,6-diphosphate on the Model of Focal Cerebral Ischemia in Rats
    Zhi Dong, Chun-Sheng Xue, Qi-Xin Zhou
    Abstract1142)      PDF (359KB)(599)       Save
    The effect of tetrandrine (Tet) on the infarction area and volume of rat brain induced by middle cerebral artery occlusion (MCAO) was investigated. The treatment with Tet 7.5, 12.0 or 15.0 mg·kg -1 , or with fructose-1,6-diphosphate (FDP) 200 and 350 mg·kg -1 ip immediately after MCAO, respectively, significantly reduced the infarction area and volume in a dose dependent manner. MK801 and FDP also displayed a protective effect on brain ischemia. A combination of Tet and FDP administered immediately after MCAO, produced a more potent protective effect than those treated with Tet or FDP alone. When Tet or FDP was administered 1 h and 2 h after MCAO, respectively, they could still significantly reduce the infarction area and volume of brain tissue. But, there was no significant protective effect when these two compounds were given 3 h after MCAO.
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    Cited: Baidu(21)
    Studies on the Anti-lipid Peroxidative Actions of the Methanolic Extract of the Root of Aegle marmelos and Its Constituents In Vivo and In Vitro
    Xiu-Wei Yang, Masao Hattori, Tsuneo Namba
    Abstract1118)      PDF (410KB)(523)       Save
    The inhibitory effect of the methanolic extract of the root of Aegle marmelos (MERA) and its constituents on the lipid peroxidation in vivo and in vitro were studied. The results suggested that MERA increased the activities of superoxide dismutase (SOD) and GSH-peroxidase in the liver cytosol of mice, but showed no significant effect on the activity of catalase, and one of its major constituents, 4-methoxy-1-methyl-2-quinolone (MMQ) increased the activity of SOD in liver tissue of mice intoxicated with FeCl 2 -ascorbic acid (AA)-ADP in vivo. Various constituents isolated from the root of title plant inhibited the lipid peroxidation in rat liver homogenate, which was in vitro induced by FeCl 2 -ascorbic acid, CCl 4 -NADPH, or ADP-NADPH. Of the test compounds, MMQ and its derivatives integriquinolone were similar to (-tocopherol in inhibiting MDA production in rat liver microsomes induced by Fe 2+ -ascorbate, CCl 4 -NADPH, or ADP-NADPH.
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    Cited: Baidu(21)
    Quantitative Analysis of Flavonoids in Scutellariae Radix of Different Sources and Seasonal Variation by HPLC
    Yong-Yu Zhang, Yun-Zhen Guo, Hiroyuki Ageta, Yoshihiro Harigaya, Masayuki Onda, Kadsunori Hashimoto, Yukinobu Ikeya, Minoru Okada, Masao Maruno
    Abstract754)      PDF (301KB)(440)       Save
    The seasonal and source variations of flavonoid contents in Scutellariae Radix were investigated by using the materials collected at the same place in Liaoning Province, China, during three years, 1990-1992, and in seven other provinces in China. Four principal flavonoids in the plant roots, i.e., baicalin, baicalein, wogonin-7-O-glucuronide and wogonin were analyzed by using a reversed-phase chromatographic system with a chemically bonded ODS silica gel column and phosphate buffer-methanol (68:32 and 1:1) as mobile phase. The contents of the four compounds combined in the herb collected at Chengde, Hebei Province are the highest. The results show that the best time for harvesting the roots in Liaoning Province is the end of August.
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    Cited: Baidu(20)
    A New Amino Acid Derivative from Red Ginseng
    Yi-Nan Zheng, H Okuda, Li-Kun Han, Lan Xiang, Y Matsuura, T Takaku, K Kameda
    Abstract1168)      PDF (359KB)(468)       Save
    Five ninhydrin-positive compounds were isolated from the water extract of red ginseng through the Bio-gel P-2 column chromatography. One compound is known as arginine. Another compound is a new substance which is determined as 1'-Nα-arginine-1'-deoxy-4'-O-(α-D-glucopyranosyl)-D-fructose (AFG) through the analysis of 13 C NMR, 1 H NMR, IR and UV spectra. Its structure is also verified through the reaction of maltose and arginine. The structures of compounds 3, 4 and 5 are being researched.
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    Cited: Baidu(20)
    Preparation and Characterization of Solid Dispersions of Silymarin with Polyethylene Glycol 6000
    LI Feng-qian *, HU Jin-hong, JIANG Yuan-ying
    Abstract963)      PDF (425KB)(687)       Save
    Aim To prepare and characterize solid dispersions of silymarin with the intention of improving their dissolution properties. Methods The solid dispersions were prepared by the fusion method with polyethylene glycol 6000 (PEG 6000) as the carrier. Evaluation of the properties of the dispersions was performed using dissolution studies, X-ray powder diffraction and Fourier-transform infrared (FT-IR) spectroscopy. Results The rate of dissolution of silymarin was considerably improved as compared with pure silymarin when formulated in solid dispersions with PEG 6000. The data of the X-ray diffraction showed some changes in the parameters of lattice spacing [d], peak position and relative intensities. FT-IR together with those from X-ray diffraction showed the absence of well-defined drug-polymer interactions. Conclusion The dissolution improvement of poorly soluble silymarin could be illuminated by the changes of the lattice parameters of PEG 6000 and the drug.
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    Cited: Baidu(20)
    Development of new solid phase extraction techniques in the last ten years
    Huixia Fan, Zhipeng Deng, Hao Zhong, Qingqiang Yao *
       DOI: 10.5246/jcps.2013.04.043
    Abstract798)      PDF (875KB)(809)       Save
    Solid phase extraction (SPE) is a widely used sample pretreatment method for separation, purification and enrichment, which has been established due to its significant advantages of time-saving, low consumption of solvent, high enrichment factor, high accuracy, etc. In recent years, a variety of new SPE methods such as molecularly imprinted solid phase extraction (MISPE), magnetic solid phase extraction (MSPE), solid phase micro-extraction (SPME), etc., which are superior to the conventional SPE, have been developed and been widely applied to food, drugs, and environmental monitoring. In this paper, the basic principles and methods of SPE and its new applications in different areas are reviewed.
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    Cited: Baidu(19)
    Chemical constituents of Pseudolarix kaempferi Gord
    Tianzhi Cai, Wen Qi, Lianmei Yang, Guangzhong Tu, Rong Yang, Kehui Xie, Hongzheng Fu *
       DOI: 10.5246/jcps.2012.05.057
    Abstract789)      PDF (933KB)(476)       Save
    Phytochemical investigations of Pseudolarix kaempferi Gord led to the isolation of 26 known compounds. They were identified as follows: pseudolaric acid D (1), pseudolaric acid A (2), pseudolaric acid B (3), pseudolaric acid C (4), oleana-&#8710;11,13(18)-dien-3β-O-acetyl (5), oleana-&#8710;9(11),12-dien-3β-O-acetyl (6), oleana-&#8710;11,13(18)-dien-3β-hydroxyl (7), oleana-&#8710;9(11),12-dien-3β-hydroxyl (8), celangulatin C (9), celangulatin E (10), 17β-tenacigenin B (11), 11α-O-2-methyl butyryl-12β-O-acetyl tenacigenin B (12), 11α-O-2-methyl butyryl-12β-O-tigloyl tenacigenin B (13), β-sitosterol acetate (14), umbelliferone (15), 5,7-dihydroxyl coumarin (16), xanthotoxin (17), isopimpinellin (18), formononetin (19), calycosin (20), cnidimol B (21), thymine (22), 3-furoic acid (23), 2-furoic acid (24), vanillic acid (25), protocatechuic acid (26). Compounds 524 were isolated from P. kaempferi for the first time. And the 1H and 13C NMR spectra of compound 1 were completely assigned for the first time.
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    Cited: Baidu(18)
    High-Performance Liquid Chromatographical Analysis of Ginsenosides in Panax ginseng, P.quinquefolium and P.notoginseng
    Wen-Sheng Lang, Zhi-Cen Lou, Paul Pui-Hay But
    Abstract1167)      PDF (692KB)(491)       Save
    The compositions and contents of ginsenbsides in Panax ginseng, P.quinquefolium and P.notoginseng were determined and compared by reversed-phase High-Performance Liquid Chromatography(HPLC).The method was performed on an Alltech Adsorbosphere HS C 18 column, using 5×10 -3 M NaH 2 PO 4 -H 3 PO 4 buffer solution(pH 3.0)and acetonitrile-water(50:50) as gradient eluents. The baseline separation of ginsenosides Rb 1 , Rb 2 , Rb 3 , Rc, Rd, Rf, Ro, and Re+Rg 1 was obtained in one analytical run.The ginsenosides are directly detected at 203 nm. The detection limit is 40μg at a signal to noise ratio of 3:1.The improved sample preparation and clean-up prior to injection with SEP-PAK C 18 cartridge strongly reduced the front peaks caused by the impurities in the methanolic extracts of samples to afford a smooth baseline and clear background. The HPLC patterns of methanolic extracts mainly including the ginsenosides were found capable of serving as chemical fingerprints to differentiate the three species from each other. It was also found that there are no significant differences of the HPLC patterns between the wild Panax ginseng and the cultivated, the white and the red ginsengs, Chinese and Korean red ginsengs, and the tap roots of Panax ginseng collected in four consecutive months, only certain differences in contents of ginsenosides do exist. The contents of the nine major ginsenosides present in the rhizome, tap root and rootlet as well as the leaf of Panax quinquefolium were also determined and compared.
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    Cited: Baidu(18)
    A New Method of Receptor Mapping to Predict Bioactivity
    Hong-Ming Chen, Tian-Rui Ren, Jia-Ju Zhou
    Abstract741)      PDF (361KB)(369)       Save
    We used genetic algorithm to construct pseudoreceptor site models and made use of the high correlation between interaction energy, which was between the models and the ligands, and bioactivity data of known molecules to predict the bioactivity of unknown molecules. For the system of ALS enzyme inhibitor, this emthod can give reasonable predictions of the bioactivity of ALS enzyme inhibitor.
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    Cited: Baidu(17)
    Pharmacokinetics of Oxiracetam in Healthy Volunteers
    WEI Chun-min *, WANG Ben-jie, GUO Rui-chen **
    Abstract254)      PDF (305KB)(717)       Save
    Aim To study the pharmacokinetics of oxiracetam after single and multiple intravenous administrations in healthy volunteers. Method A HPLC method was used to determine the serum concentration of oxiracetam after intravenous single dose and daily dose of 2 000 mg for 7 d in ten Chinese healthy volunteers. Pharmacokinetic analysis was carried out using Drug And Statistic software. Results The AUC 0 ~ 12 , AUC 0~∞ , K e , t 1/2 , MRT after a single dose of 2 000 mg oxiracetam were 256.26±16.84 μg·mL -1 ·h -1 , 276.74±18.11 μg·mL -1 ·h -1 , 0.18±0.03 h -1 , 3.84±0.64 h, and 4.39±0.39 h, and after multiple doses of oxiracetam were 259.36±25.43 μg·mL -1 ·h -1 , 285.59±27.38 μg·mL -1 ·h -1 , 0.17±0.04 h -1 , 4.14±0.82 h, and 4.87±0.69 h, respectively. Conclusion The pharmacokinetic parameters of oxiracetam do not differ remarkably after single and multiple intravenous administration and there is accumulation in serum after 2000 mg multiple intravenous administration once a day for 7 d.
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    Cited: Baidu(17)