Journal of Chinese Pharmaceutical Sciences

Phytotherapy in China and Its Prospects

Hai-Jun zhou, Yun-Ru Lu

1992, 1(1): 3-12.

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Isolation and Characterization of Platelet-Activating Factor (PAF) Inhibitors from Zanthoxylum schinifolium

Mei-Fang Hong, Jing-Xian Pan, Tian-Yi Jiang, Chang-Ling Li, Gui-Qiu Han

1992, 1(1): 13-19.

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Two new compounds, schinifolin I and acetoxyschinifolin II, along with five known compounds (auraptenIII, dictamnine IV, scoparone V, skimmianine VI, and β-sitosterol VII) were isolated from the roots of Zanthoxylum schinifolium Sieb.et Zucc.col- lected in Yixing County, Jiangsu Province. The structure determination was based upon spectroscopic analysis(UV, IR, MS, PMR, CMR, ²D NMR).The structures of schinifolin I and acetoxyschinifolin II were elucidated as 7[(3',7'-dimethyl-2',6'-octadienyl)] oxy-8-methoxy-2H-1-benzopyran-2-one, and 7[(3',7'-dimethyl-5'-acetoxy-2',6'-octadienyl)]oxy-8-methoxy-2H-1-benzopyran-2-one, respectively. In the test of platelet aggregation caused by PAF, compounds I, II, III and V showed inhibitory activity.

Dibenzocyclooctadiene Lignans with Platelet-Activating Factor (PAF) Antagonist Activity from Kadsura heteroclita

Gui-Qiu Han, Ping Dai Rong Xue, Byron H.Arison, David C.Lankin, San Bao Hwang

1992, 1(1): 20-27.

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Seven known dibenzocyclooctadiene lignans, tigloylgomisin P(1), angeloylgomisin P(2), gomisin A(3), Schizandrin(4), angeloylgomisin H(5), gomisin B(6) and R(+)-gomisin M1(7) were isolated from Kadsura heteroclita.The conformation of tiglolylgomisin P(1)was established by ²D NMR techniques. Using [³H] platelet activating factor (PAF) binding to human platelet membrane assay, (1), (2) and (7) showed PAF receptor antagonistic activities.

Exploration for a Natural Selenium Supplement-Characterization and Bioactivities of Se-containing Polysaccharide from Garlic

Ming Yang, Kui Wang, Lin Gao, Yu-Ting Han, Jing-Fen Lu, Tong-Tong Zou

1992, 1(1): 28-32.

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A Se-containing polysaccharide (Se-GPS), with average molecular weight of 1.5×10⁴ was isolated from Hubei Enshi garlic (Allium sativum L.) and purified by means of Sephadex G25 to G200 chromatographies. Its chemical homogeneity and composition were studied by optical rotation, HPLC and paper chromatographical methods. The abilities of scavenging active oxygen free radicals and inhibiting the damage of erythrocyte membrane by SiO2 were established by spin trapping ESR studies. Se-GPS was shown to inhibit human cytomegalovirus by plague reduction assays and cytopathogenic effect tests.

Studies on Mitomycin C Dextran-microspheres

Shu-Li Wei, Yi-Chun Sun, Jing-Shi Zhang, Wei-Wei Tan, Jing-Xia Xie, Xuan Li, Jian-Gang Zhu

1992, 1(1): 33-40.

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In this paper, the preparation and properties of mitomycin C dextran-microspheres(MMC-DMS)were reported. The characteristics of pharmacokinetics and embolization effects of MMC-DMS in vivo were studied in dogs. The average diameter of the microspheres was 75±19 μm and the content was 5% of MMC. In vitro experiment, the release rate of drug demonstrated that the microspheres had sustained-release properties. The microspheres and conventional MMC were infused into the hepatic artery of dogs through a catheter for embolization, respectively. The plasma concentration of MMC was determined by HPLC. Results showed that the peak concentration of conventional MMC was 2.6 times as much as MMC-DMS. Angiograms revealed that peripheral blood vessels decreased obviously in liver. The histopathologic examination showed that the microspheres lodged in the hepatic artery and displayed nodular necrosis in the embolized segment. The MMC-DMS were used in clinical trial in 100 patients with hepatic cancer. The tumor reduction and improvement of symptoms in patients were observed after hepatic arterial embolization. The survival duration was prolonged. Results showed that the MMC-DMS is a promising embolic agent for treatment of hepatic cancer. It could aid in the use of intensive chemotherapy with minimum systemic side effect.

Effects of N-(3', 4', 5'-Trimethoxycinnamoyl) ortho-Aminobenzoic Acid on Antigen-induced Contraction of Guinea-pig Ileum and the Degranulation of and Histamine Release from Mast Cells

Jun-Jiang Ma, La-Fu Si, Zhi-Bin Lin

1992, 1(1): 41-45.

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N-(3', 4', 5'-Trimethoxycinnamoyl) ortho-aminobenzoic acid (TOA), at the concentration of 80 μg/ml, significantly inhibited the antigen-induced contraction of ileum isolated from the actively sensitized guinea-pig. At the concentrations of 25 and 50 μg/ml, TOA inhibited homocytotropic antibody-mediated degranulation of mast cells in the rat mesentery, and also inhibited anaphylactic histamine release from rat peritoneal mast cells.

Effects of Lingzhi (Ganoderma lucidum) on Hemorrheology Parameters and Symptoms of Hypertensive Patients with Hyperlipidemia and Sequelae of Cerebral Thrombosis

Zhang-Hua Cheng, Jue-Ying Wang, Yi-De Shao, Zi-Jun Liang, Yi-Hua Ning, Zhi-Juan Bai, Shuang Dong, Yu-Chan Ye, Masao Mori, Wei-Rong Huang

1992, 1(1): 46-50.

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The effects of Lingzhi (Ganoderma lucidum) on hemorrheology parameters and symptoms of hypertensive patients with hyperlipidemia, sequelae of cerebral thrombosis and coronary heart disease are studied. The Lingzhi extract was given to 33 patients (15 male, 18 female, 65±8 years old) in dosage of 110 mg qid po for 2 weeks. The blood viscosity was improved after treatment. The results showed that whole blood viscosity (at high shear rate and low shear rate) and plasma viscosity were significantly decreased(P<0.01). Lingzhi showed the effect of reducing blood pressure simultaneously. Several symptoms were also improved. However, there were no significant changes in haematocrit and erythrocyte sedimentation rate (P>0.05).In a few cases there occurred adverse reactions of palpitation and restlessness.

Studies on the Analytical Method for a New Antiarrhythmic Guanfu Base A in Rabbit Plasma

Li-Li Yang, Xiang-Jing Yang, Jing-Han Liu, Nai-San Li, Ning-Ying Qiu

1992, 1(1): 51-59.

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Guan-fu base A(GFA), a new antiarrhythmic alkaloid with a structure of C20-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride (TFAA) to produce GFA-TFAA of which the structure was identified by GC-MSD. There was a wide linear range of the GC-ECD method from 10 to 20000 ng/ml (r = 0.9984). The average recovery of GFA from the spiked plasma was 97.52%. The coefficients of variation of within-day and between-day were less than 7% and 9%, respectively. The method was used in the preclinical experiment of pharmacology of GFA and the results showed that GFA concentrations in rabbits' plasma within 6 hours after the administration ranged from 0.338±0.014 to 13.459±5.393 μg/ml for dosage 10mg/kg, from 0.133±0.038 to 2.546±0.480 μg/ml for dosage 2 mg/kg and from 45.25±10.34 to 535.86±24.36 ng/ml for dosage 0.4 mg/kg.

Separation and Quantitative Determination of Three Phytoecdysteroids in Rhaponticum uniflorum by High Performance Liquid Chromatograghy

De-An Guo, Zhi-Cen Lou

1992, 1(1): 60-66.

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An anlytical method for the separation and quantitative determination of three phytoecdysteroids in Rhaponticum uniflorum by high performance liquid chromatography has been developed. Three phytoecdysteroids, ecdysterone (I), rhapontisterone (II) and turkesterone (III) were separated and determined quantitatively by using the solvent system MeOH-H2O (40:60) at 242 nm with flow rate of 1.5 ml/min, the operation can be completed in 10 minutes. Using the external standard method, the content of three phytoecdysteroids in the roots and aerial parts of Rhaponticum uniflorum obtained from different localities was determined. It is proved that this method is sensitive and accurate, and with good reproducibility.

Mass Spectrometric Characterization of a Thermolabile Metabolite of Camazepam

Xiang-Lin Lu, Xian-Gui Yang

1992, 1(1): 67-74.

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Incubation of camazepam [3-(N,N-dimethyl) carbamoyloxy-7-chloro-1-methyl-1,3-dihydro-5-phenyl-2H-1, 4-benzodiazepin-2-one] with rat liver microsomes and cofactors produced a 3-(N-methyl-N-hydroxymethyl) carbamoyloxy derivative as the most abundant metabolite. This metabolite was thermally unstable and was isolated from a metabolite mixture by normal-phase High-Performance Liquid Chromatography. Its structure was established by chemical ionization and ²⁵²Cf plasma desorption time-of-flight mass spectral analyses.

Determination of Dehydroepiandrosterone Sulfate with High Performance Liquid Chromatography

Hua Chi Yu-Ling Liu Shi-Jie Gu

1992, 1(1): 75-78.

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Studies on Active Polysaccharides from Ganoderma lucidum

Yun-Qing He, Rong-Zhi Li, Qi Chen, Zhi-Bin Lin, Dong Xin, Li Ma

1992, 1(1): 79-81.

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