Table of Content

15 March 1997, Volume 6 Issue 1

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Full Papers

Studies on the Antitumour Activities of 8-Chloroadenosine

Li-He Zhang^*, Jia-Chun Fang

1997, 6(1):  1-7. 

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(Sp)-Octyl-8-chloroadenosine-3',5'-cyclophosphate (OCC), a newly synthesized 8-Cl-c-AMP derivative, strongly induced inhibition and differentiation in human leukemia HL 60 cells. In flow cytometry, OCC brought about a block at the G1 phase of HL-60 cell cycle. OCC inhibited strongly the synthesis of DNA without affecting the synthesis of RNA and protein in HL-60 cells and also activated the c-AMP dependent protein kinase in the cytosol of HL-60 cells. 8-Chloroadenosine is the active metabolite of OCC and inhibited significantly the growth of tumour in vitro and in vivo tests. 8-Chloroadenosine can induce differentiation of gastric mucoid adenocarcinoma cell line MGc80-3 and induce apoptosis in the MOLT-4 cells. The mechanism of the antitumour effects of 8 chloroadenosine was discussed.

Alkaloids from the Roots of Aristolochia Triangularis (I)

Wen-Han Lin^*, Hong-Zheng Fu, Yoshio Hano, Taro Nomura

1997, 6(1):  8-13. 

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From the roots of Aristolochia triangularis, two new alkaloids triangularine-A and triangularine-B together with thirteen known alkaloids namely aristololactam AII, AIIIa, AIA, Ia, IIA, BII, CII, cepharadione A, 4,5-dioxodehydroasimilobine; aristolochic acid-D (IVa), magnoflorine; N,N-dimethyllindcarpine and oblongine were isolated, their structures were identified by means of spectral analysis and chemical conversion.

Diterpene Alkaloids of Aconitum kirinense Nakai I Lepe-nine and Kirinine A

Feng Feng^*, Jing-Han Liu

1997, 6(1):  14-17. 

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Two diterpene alkaloids, lepenine and kirinine A were isolated for the first time from the roots of Aconitum kirinense Nakai. Their structures have been established by IR, HRMS, NMR analysis and chemical reactions, and kininine A was found to be a new C20 diterpene alkaloid.

Study on QSAR of Taxol and its Derivatives Based on Stepwise Multivariate Linear Regression Analysis

Ai-Lin Liu^*, Han-Lin Chi

1997, 6(1):  18-22. 

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Using the method of stepwise multivariate linear regression (SMLR), the quantitative structure activity relationships (QSAR) of two isomeric series of taxol and its derivatives have been studied. It was found that the molar refractivity of the C3' substituent of the C13 side chain has significant correlation with its activity. We deduce that structural changes in the C3' substituents may be critical to the anticancer function. It would be useful to the design and synthesis of taxol like compounds with improved activities.

SOD like Activity of Copper Salicylate Complex in Tween Micellar Systems

Yan Liu^*, Xue-Dong Zhang, Si-Qian Ma, Chun-Su Lu

1997, 6(1):  23-27. 

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Copper salicylate complex has been synthesized and its composition was analyzed. The four surfactants (Tween 20, 40, 60, 80) were purified and their critical micelle concentrations(CMC) in phosphate buffer (pH = 7.4) were measured. The SOD like activity of copper salicylate complex was assayed using the cytochrome creduction method in different media. The cooperative effect of the complex with micelles was studied in detail. SOD like activity of the complex was enhanced in the presence of surfactants. The four surfactants themselves display SOD like activities to a certain extent. Similar results were obtained in the experiment for the antilipid peroxidation of red cell membrane. These results might be explained by the fact of micellar catalysis. It was suggested that the copper salicylate Tween system used as a potential antiinflammatory drug might be worthwhile to be further studied.

Synthesis of Sedative hypnotic Zopiclone Analogues

Dai-Shu Zuo, Da Lu, Yu-Lan Liu, Ya-Fang Zhang

1997, 6(1):  28-31. 

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Eight new cyclopyrrolone compounds were synthesized according to the structure activity relationship and action mechanism of Zopiclone, a cyclopyrrolone hypnotic. Their preliminary pharmacodynamics are under investigation.

An Experimental Model for Screening Anti-AIDS Drugs with Bovine Immunodeficiency Virus

Dai Wang, Shu-Hong Liu, Qi-Min Chen, Yun-Qi Geng, Wei-Ren Xu, Yue-Fang Wei

1997, 6(1):  32-36. 

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The assays for bovine immunodeficiency virus (BIV) induced syncytium formation and BIV long terminal repeat (LTR) directed luciferase (Luc) gene expression were applied to screen and evaluate anti AIDS drugs. Frequency of the syncytium formation and BIV LTR directed Luc activity were in proportion to the number of input BIV infected cells. AZT inhibited the syncytium formation and the BIV LTR directed Luc gene expression level. Its inhibitory effects were dosedependent with the IC50 being 0.24 and 0.052 mmol/L, respectively.

Effects of Berbamine on PAF Production in Human Neutrophils and on Platelet Aggregation

Li-Hua Bao, Da-Li Luo, Bao-Feng Yang, Shu-Zhuang He, Wen-Han Li

1997, 6(1):  37-40. 

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The effects of berbamine, an alkaloid of dibenzylisoquinoline, on PAF produc tion in human neutrophils and on platelet aggregation induced by PAF were studied and compared with those of the calcium antagonist verapamil. Preincubation with berbamine (50 mmol/L, 100 mmol/L) or verapamil (10 mmol/L, 100 mmol/L) was shown to significantly inhibit A 23187 stimulated PAF synthesis. Berbamine and verapamil were found to inhibit platelet aggregation induced by PAF 70 pmol/L in a dose dependent manner. These results suggest that the inhibitory effects of berbamine and verapamil on A-23187 stimulated PAF synthesis in human neutrophils and PAF induced platelet aggregation are possibly brought about by inhibiting cellular calcium influx.

Vasodilation Effects of RGD Containing Peptides and Derivatives

Dilinuer Shabituove, Ming Zhao, Shi-Qi Peng^*, Chao-Shu Tang, Qin-Lu Zhou, Qiang Li

1997, 6(1):  41-44. 

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The binding of Fgn to GPIIb/IIIa has confirmed that there are two distinct amino acid sequences within the Fgn molecule that are responsible for mediating its attachment to GPIIb/IIIa receptor. In addition to monoclonal antibodies, the binding function of GPIIb/IIIa can be blocked by synthetic small peptides containing the RGD and APLRV sequence. In our preliminary study it was found that besides inhibition of platelet aggregation and thrombus formation RGDS showed vasodilation effects as well. In an attempt to confirm the vasodilation effect of RGDS related peptides, RGDF, APLRV, APLRVRGDS and APLRVRGDF were investigated. The effects of these synthetic peptides on rat aortic strips pretreated with NE in vitro were observed. The relaxing extents of contracted strips for the peptides at three doses (10^-5 mol/L, 10^-6 mol/L, 10^-7 mol/L) were recorded.

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

1997, 6(1):  45-50. 

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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.

Communication

Resolution of α1-Adrenoceptor Antagonist (±)-DDPH and Pharmacological Activity of (-)-DDPH

Pei-Zhou Ni, Hong-Bin Sun, Jiu-He Pen, Lin Xin, Jia-Qing Qian

1997, 6(1):  51-53. 

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Abstract of Thesis

Transdermal Iontophoresis of Non-steroid Anti-inflammatory Drugs

Jian-Qing Gao, Wen-Quan Liang

1997, 6(1):  54-56. 

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