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Table of Content

    15 December 2002, Volume 11 Issue 4
    Contents
    Contents list
    Journal of Chinese Pharmaceutical Sciences
    2002, 11(4):  1-01. 
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    Full Papers
    Ocotillone-type Ginsenoside from Leaves of Panax ginseng
    Dou Deqiang, Chen Ying, Ren Jie, Pei Yuping, Chen Yingjie*
    2002, 11(4):  119-121. 
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    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.
    Biotransformation of Artemisinin by Hairy Root Cultures of Rheum palmatum L.
    Li Lixin, Su Yanfang, Liu Xiaofeng, Guo Dean*
    2002, 11(4):  122-124. 
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    The biotransformation of artemisinin by hairy root cultures of Rheum palmatum L. was investigated for the first time. The main product, deoxyartemisinin, was isolated and characterized on the basis of its spectral data.
    Cobalt (II) Complex of 6,7-Dicycanodipyridoquinoxaline with Antitumor Activities: Synthesis, Crystal Structure and Binding with DNA
    Xu Zhidong, Liu He, Wang Min, Xiao Sulong, Yang Ming*, Bu Xianhe
    2002, 11(4):  125-131. 
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    A novel complex Co (II) with the planar ligand 6,7-dicycanodipyrido[2,2-d:2',3'-f]quinoxaline (L), [CoL(NO3)2(CH3CN)] (1) has been synthesized and characterized. The crystal structure of the complex was determined by X ray diffraction analysis. The cobalt atom was heptacoordinated to form a distorted pentagonal bipyramid geometry by three nitrogen atoms of L and a CH3CN, four oxygen atoms of two NO3- in complex 1. Biological tests against four different cell lines (HL-60, KB, Hela and BGC-823) showed that the complex had strong antitumor properties with the 50% inhibition concentrations (IC50) of the complex were in a μmol·L-1 range. For understanding the antitumor mechanism of the complex, the binding modes of the complex with calf thymus DNA had also been investigated with spectrophotometric methods, viscosity and thermal denaturation measurements. The experimental results indicated that complex 1 intercalated into DNA base pairs. The intrinsic binding constant Kb values for 1 (4.43×105mol·L-1) and L (1.65×105mol·L-1) were determined by absorption titration and calculated with the model of McGhee and Von Hippel.
    Effects of BYHW Decoction and Its Effective Constituents on the Fluidity of the Cell Membrane in a Stroke-Modeled Rat Brain
    Lu Jingfen, Li Chenxu , Muteliefu Gulinuer, Li Tingfeng, Tu Pengfei, Yin Junjie, Cai Shaoqing*
    2002, 11(4):  132-136. 
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    With in vitro spin labeling electron spin resonance (ESR) spectroscopy, we have studied the effects of Bu Yang Huan Wu (BYHW) decoction and its effective constituents such as astragaloside IV ferulic acid, chuanxiongzine, rutin, chlorogenic acid, 9,10 dimethoxy pterocarpane-7-O-β-D-glucoside, calycosin, formononetin, calycosin-7-O-glucoside, paeoniflorin, paeonal and quercein on the cell membrane fluidity of a rat brain which was modeled after the dual cervical arteries were intercepted and released for realizing an ischemia reperfusion injury which was selected as a brain stroke model. Our results indicated that the cell membrane fluidity in the model group decreased approximately 8% compared with the control group, and after brain cells were incubatied with species, the membrane fluidity could be recovered closely to the control level depending on the BYHW decoction and its different constituents. As the membrane fluidity is a very sensitive biological index which reflectsd the cell status, our method will be useful to study the molecular mechanism of tradition Chinese medicine (TCM) and its combination recipe.
    Determination of Loratadine in Human Plasma by High Performance Liquid Chromatography-Electrospray Mass Spectrometry and Studies on Its Pharmacokinetics and Relative Bioavailability
    Chen Jun, Gao Kepan, Shi Zhengqi, Lu Wei, Jiang Xinguo*, Rong Zhengxing, Huang Xia, Chen Hongzhuan
    2002, 11(4):  137-141. 
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    A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4~100 ng·mL-1 with r = 0.9995. The recovery of this method was within 95%~104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The Cmax, AUC0-t and Tmax values of the two formulations were 51.89±20.18 ng·mL-1 and 52.48±22.35 ng·mL-1; 140.75±88.42 ng·h·mL-1 and 147.24±92.33 ng·h·mL-1; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the Cmax, AUC0-t and Tmax values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC0-t measurement. Bioequivalance was observed between the two tablets.
    Pharmacokinetics of Recombinant E. coli L-asparaginase in Rats

    Chen Jianhua, Wu Wutong*, Hirano Kazuyuki

    2002, 11(4):  142-147. 
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    The distribution of 125I recombinant E .coli L-asparaginase in tissues or organs and the excretion in urine, feces and bile were studied with in vivo radioactive tracer technique. The amount of radioactivity excreted in urine, feces and bile within 24 h after intravenous administration of 125I recombinant E .coli L-asparaginase to rats was 68.95%,4.44% and 5.36% of the dose respectively.125I recombinant E .coli L-asparaginase in plasma samples was determined. The levels of structural intact molecule in plasma samples were evaluated by SDS-PAGE and bio-imaging analyzer system. Pharmacokinetic parameters were assessed with a model dependent method. The concentration time curves of recombinant E .coli L-asparaginase after intravenous injection at 1250 IU·kg-1, 2500 IU·kg-1, 5000 IU·kg-1 to rats were consistent with the two compartment model. The first and terminal elimination t1/2 were 0.52~0.63h and 2.39~2.76h respectively. AUC was linearly related to the doses. The results of distribution in tissues or organs and excretion in urine suggested that the metabolites of the enzyme were cleared by mechanisms of urinary excretion. Pharmacokinetics parameters of recombinant E .coli L asparaginase in rats are warranted for the design of future clinical trials.
    High-Performance Liquid Chromatographic Determination of Nine Major Constituents in Roots of Salvia
    Wang Hong, Wang Qiang
    2002, 11(4):  148-152. 
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    A method of gradient elution HPLC with UV detection was developed for the analysis of nine major constituents of Salvia species, a commonly used TCM herb, namely danshensu, protocatechuic acid, protocatechualdehyde, salviano lic acid B, methyltanshinone, dihydrotanshinone, cryptotanshinone, tanshinone I and tanshinone II A. In the present study, a Shimadzu CLC-ODS column (150 mm×6 mm, 5 μm) was utilized and 0.5% formic acid (A) and acetonitrile (B) were used for gradient elution at a total flow rate of 0.8 mL·min-1. All calibration curves showed good linear regression (r>0.999) within test ranges. Extraction was conducted by refluxing methanol (10 mL) with dried herb (0.5 g) for 1.0 h.The assay was simple, convenient and reproducible. The proposed method was successfully applied to the determination of nine major constituents in thirteen Salvia species and the results showed that the contents of Salvia components vary in different species and origin. Tanshinone was hardly detected in S.yunnanensis and S. prionitis, therefore they are not suitable for clinical use as Danshen.
    Determination of Chlordiazepoxide by Sodium Tetraphenylboron Method
    Li Yanwei*, Wei Wenlong, Wang Zhizhong, Wang Jinhui
    2002, 11(4):  153-156. 
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    This paper describes an effective method for determining chlordiazepoxide. An excess of sodium tetraphenylboron is added to precipitate chlordiazepoxide in HAc-NaAc buffer solution (pH = 4.0). After filtering off the precipitate, the excessive sodium tetraphenylboron in the filtrate is titrated with cetyltrimethylammonium bromide standard solution, with bromophenol blue as indicator. The method is simple and rapid, it has been applied for the determination of chlordiazepoxide raw materials with satisfactory results. The recovery is between 99.58% and 100.4%, the relative error is less than ±0.50%. Experiments show that the method gives the same results as the approach using nonaqueous titration (ChP).
    Protective Effects of Tea Polyphenol on Cerebral Ischemia-Reperfusion Injury in Rats and Its Scavenging Oxy-radical and Anticerebral Lipid Peroxidation Effects
    He Bing, Chen Xiaoxia, Chen Yiyue
    2002, 11(4):  157-161. 
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    AIM To study the protective effects of tea polyphenol (TP) on cerebral ischemia reperfusion injury in rats and its scavenging oxygen free radical(OFR) activities and antilipid peroxidation in vitro. METHODS Cerebral ischemia reperfusion injury was produced by bilateral ligation of the common carotid arteries with vagus nerves and reperfusion for 45 min. The mitochondrial lipid peroxidation of rat brain induced by oxygen free radical was measured by thiobarbituric acid spectrophotometry. Superoxide anion (O2-) from xanthine-xanthine oxidase system and hydroxyl radical (·OH) from Fe2+-H2O2 system were determined with spectrophotometry. RESULTS During Cerebral ischemia reperfusion,TP improved the activities of superoxide dismutase (P<0.05), GSH peroxidase(P<0.01) and catalase(P<0.01), while decreasing the maiondialdchyde content in the brain(P<0.05) and brain water content (P<0.01). Tea polyphenol possessed significantly scavenging effects on ·OH produced by Fenton reaction and O2- produced by xanthine-xanthine oxidase system (the IC50 were 2.2 mmol·L-1 and 1.9 mmol·L-1 respectively). Tea polyphenol could significant inhibit the lipid peroxidation of cerbral mitochondrial membrane induced by ·OH in a concentration dependent manner. CONCLUSION The results indicate that tea polyphenol could protect the injury on cerebral ischemia reperfusion in rats for OFR, these effects may be related to its scavenging effects on oxygen free radicals and antilipid peroxidant.
    Communication
    N-nitro-L-arginine Attenuates Morphine and Dihydroetorphine-induced Place Preference in Mice
    Wan Xingwang, Huang Mao, He Yaqin, Li Wanhai, Wan Li, You Zhendong, Lu Changlin
    2002, 11(4):  162-165. 
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    CONTENTS OF VOLUME 11
    AUTHOR INDEX

    2002, 11(4):  166-170. 
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