Journal of Chinese Pharmaceutical Sciences

Studies on the Triterpenoid Constituents of the Spores from Ganoderma lucidum Karst

Ruo-Yun Chen, De-Quan Yu

1993, 2(2): 91-96.

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Five compounds were isolated from the ether-soluble fraction of the spores of Ganoderma lucidum. On the basis of their chemical properties and spectral data(MS, UV, IR, ¹H and ¹³C NMR), they were identified as 3, 7, 11, 12, 15, 23-hexaoxo-5α-lanosta-8-en-26-oic acid (I), ganoderic acid B (II), C (III), D (IV)and ganodermanontriol(Ⅴ).Compound I is a new natural product, named ganosporeric acid A. Compounds II, III, IV and V are known compounds and were obtained for the first time from the spores of Ganoderma lucidum.Pharmacological experiments showed that ganosporeric acid A has an activity for lowering the levels GPT in mice with liver injury by CCl4 and GaNI and exhibits heptoprotective effects.

Cyclohexene Epoxides from Piper polysyphorum

Ying Ma, Gui-Qiu Han

1993, 2(2): 97-101.

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Three new cyclohexene epoxides, polysyphoside A, B and C, along with a known compound crotepoxide (4), were isolated from Piper polysyphorum C. DC. Based on spectroscopic analysis, their structures were established as 1-benzoyloxymethylene-2-hydroxy-3-benzoyloxy-1, 6- epoxycyclohex-4-ene (1), 1-benzoyloxymethylene-2-hydroxy-5-benzoyloxy-1, 6-epoxycyclohex-3-ene (2) and 2-hydroxy-3-benzoyloxymethylene-5-benzoyloxy-1, 6-epoxycyclohex-3-ene (3), respectively. It was the first time that(1), (2) and (3) had been isolated from a natural source.

The Synthesis of Vasoactive Protected L-Arginine

Ming-Di Gu, Shi-Qi Peng, Xue-Min Yu, Meng-Shen Cai, Xue-Qing Guo, Lian-Yuan Zhang, Shu-Yun Dong, Yue Zhang, Chao-Shu Tang

1993, 2(2): 102-108.

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Under the catalysis of dioxygenase L-arginine is converted to L-citrulline and nitric oxide, the latter exhibits endothelium derived relaxing factor(EDRF)-like actions.N^G-nitro-L-arginine has an inhibitory effect on the biosynthesis of EDRF in vitro and in vivo, hence it is an EDRF antagonist.The results of the present work indicate that both N^G-NO2-L-Arg-OH and HCl·N^G-NO2-L-Arg-OCH3 have vasodilating effect in vitro, but produced dose-depending increase in mean arterial blood pressure (MAP) in vivo.In vitro HCl·N^G-NO2-L-Arg-N^G-NO2-L-Arg-OCH3 relaxed rat aortic strip pretreated with noradrenaline(NE).In vivo, however, it produced biphasic effect, i.e, decreased MAP at lower dose and increases MAP at higher dose, N^G-Tos-L-Arg-N^G-Tos-L-Arg-OH produced dose-depending vasodilating and hypotensive actions.

Effect of J-894 on Cytoplasmic Free Calcium Concentration in Human Platelet Activation

Jian-Ping Bai^*, Hong Zhang, Zhong Wang

1993, 2(2): 109-113.

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The intracellular free calcium concentration plays a key role as the second messenger in the regulation of cellular reaction.The changes of cytoplasmic free calcium concentration([Ca²⁺]i) in human platelets loaded with the fluorescent calcium indicator quin-2 were measured in this study. The result showed that thrombin (0.3 U/ml)raised the [Ca²⁺]i of platelets four to five times in the presence of 1 mmol/L external calcium, but there was a much smaller increase in [Ca²⁺]i in the absence of external calcium. It seems that thrombin increased[Ca²⁺]i partly by release of internal Ca²⁺, but mainly by stimulating influx.J-894 markedly inhibited the rise of [Ca²⁺]i in platelets induced by thrombin in a dose dependent manner through decreasing both calcium influx and calcium release. This suggests that J-894 may be a calcium channel blocker.

The Effects of Captopril and Cicaprost on Changes of Cardiac Membrane Fluidity and Lipid Peroxidation

Zhi Su, Yuan-Jian Li, Xiu Chen

1993, 2(2): 114-120.

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The main purpose of this study was to investigate the protective actions of captopril and cicaprost on changes of membrane fluidity of cultured neonatal rat myocardial cells exposed to anoxia and sugar deprivation. Lipid peroxidation level estimated by determining the thiobarbituric acid reactive substance(TBARS)content and lactate dehydrogenase (LDH) released in culture medium was also observed in order to examine other membrane-related changes due to anoxia. Membrane fluidity was monitored by measuring changes in the steady state fluorescence anisotropy (rs) by fluorescence spectroscopy. The rs value, TBARS level and LDH release were significantly increased after 3 h anoxia. Captopril (180 μmol/L), cicaprost (30 nmol/L) and indomethacin (1 μmol/L) did not alter rs, TBARS level and LDH activity of normal cultured neonatal rat myocardial cells. However, both captopril and cicaprost significantly prevented the increases of rs, TBARS content and LDH release in those cells exposed to anoxia and sugar deprivation. Indomethacin abolished the actions of captopril on TBARS production and LDH release, but maintained its membrane fluidity protection. These results indicate that captopril and cicaprost protect membrane fluidity and lipid peroxidation changes in anoxia- injured myocardial cells. The action mechanism of captopril may be due, in part, to stimulation of prostacyclin synthesis and/or release.

Immunopotentiating Effects of Cucurbitacin B in Mice

Ying-Ju Liu, Wen-Qing Liu

1993, 2(2): 121-126.

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Cucurbitacin B (CUB) is a major active principle contained in the calyx melo of Cucumis melo L. The immunopotentiating effects of CuB (im, qd×5) were studied.At lower doses, CuB increased the number of peripheral blood T lymphocytes (0.1 mg/kg), the rate of PHA-induced lymphocyte transformation (0.2 mg/kg), the number of plaque forming cells(PFC)of the spleen(0.2 mg/kg) and the level of serum hemolysin (0.4 mg/kg). The phagocytosis of macrophages and the clearance rate of charcoal particles were enhanced only by a large dose(0.8 mg/kg). The results indicate that CuB can potentiate both cellular and humoral immune function.

Reduction of Praziquantel Elimination by Cimetidine in Rats

Ping Yi, Yu-Zhu Quan

1993, 2(2): 127-132.

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The effect of cimetidine on the elimination of praziquantel (PQT) in rats was studied. The results showed that cimetidine 100 mg/kg, ip 2 reduced the clearances of intravenous and oral PQT by 60 and 69 percent respectively. Cimetidine also markedly reduced liver blood flow of rats (a reduction of 58%) and inhibited PQT metabolism in hepatic microsomes of rats (an inhibition of 55%). The reduction in clearance of intravenous PQT could be attributed to the result of cimetidine lowering liver blood flow, whereas the reduction in clearance of oral PQT might be related mainly to the inhibition of cimetidine on the activity of hepatic drug-metabolizing enzymes.

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

1993, 2(2): 133-143.

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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 C18 column, using 5×10^-3 M NaH2PO4-H3PO4 buffer solution(pH 3.0)and acetonitrile-water(50:50) as gradient eluents. The baseline separation of ginsenosides Rb1, Rb2, Rb3, Rc, Rd, Rf, Ro, and Re+Rg1 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 C18 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.

Studies on the Male Antiferility Constituents of tripterygum hypoglaucum (Levl.) Hutch

Zheng-xing zhang, Li Ding, Shao-zhen qian, Deng-kui An

1993, 2(2): 144-147.

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Mono-Feruloyl-R, R-(+)-tartaric Acid form Salvia

Tian-Xiu Qian, Zhao-Hui Yan, Lian-Niang Li^*

1993, 2(2): 148-150.

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