Table of Content

15 June 1993, Volume 2 Issue 1

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Review

Development of Cardiovascular Drugs Based on Isoquinoline Compounds from Chinese Medicinal Materials

Si-Xun Peng, Wei-Yi Hua, Wen-Long Huang, Zhen-Ya Huang, Hui-Ming Cai

1993, 2(1):  3-10. 

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By using active principles of Chinese medicinal materials as lead compounds soquinoline derivatives have been designed and synthesized. Their chemical structures include bisbenzylisoquinoline, benzyl-isoquinoline and protoberberine. Their cardiovascular effects were studied involving α-adrenoceptor, adenosine A1, A2 and DPH-calcium channel radioreceptor assays.In addition, calmodulin inhibiting, calcium antagonistic potassium channel blocking and antiplatelet aggregation activities were also performed.It was found that compound VI19 was a new potassium channe blocker with α-adrenoceptor antagonism, compound V9, and V21 lowered blood pressure on various animal models with negative chronotropic action, compound VI13 possessed antiarrhythmic and antifi- brillation action, and it may be a candidate tot clinic evaluation.The structure-activity relationships deduced may provide a theoretical basis for further development of new agents.

Full Papers

Carbon-13 Nuclear Magnetic Resonance Spectra of Some Protoilludane Sesquiterpenoid Aromatic Esters from Armillaria mellea (Vahl.ex Fr.) Quel.

Jun-Shan Yang^*, Ya-Lun Su, De-Quan Yu, Xiao-Tian Liang

1993, 2(1):  11-17. 

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The carbon-13 nuclear magnetic resonance spectra of seventeen protoilludane sesquiterpenoid aromatic esters from the artificially cultured mycelium of Armillaria mellea (Vahl. ex Fr.) Quel.have been analysed and assigned. All the 11CNMR signals of the model compounds melleolide 5 and compounds 8, 10, 11, 13, 14, 15, and 16 can be assigned on the basis of the multiplicity of the signals in the off-resonance decoupled spectra or INEPT spectra, ¹³C-¹H COSY and long-range ¹³C-¹¹H COSY. The assignments of the ¹³C NMR spectra of other protoilludane sesquiterpenoid aromatic esters were completed by comparison with the model compounds as well as the electronic effects of substituted group on the molecules. The present results indicate that 11CNMR spectroscopy provides an effective method for characterizing the protoilludane sesquiterpenoid aromatic esters.

Antiplatelet Aggregation and Vasodilation Effects of RGDS

Ming Zhao, Shi-Qi Peng, Meng-Shen Cai, Chao-Shu Tang, Chang-Ling Li, Xue-Min Yu, Zhen-Nan Wang

1993, 2(1):  18-23. 

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In an attempt to demonstrate the biological activities of a short peptide. Arg-Gly-Asp-Ser (RGDS) was synthesized and used for bioassay, The data obtained here proved that RGDS obviously inhibited PAF- and/or ADP-induced platelet aggregation. The present paper revealed that RG-DS had vasodilative action and the cGMP accumulation may be one of the mechanisms of RGDS exerting bioactivities.

Application of Microcalorimetric Technique for the Screening and Examination of Medicines

You-Min Zhang, Bao-Huai Wang

1993, 2(1):  24-32. 

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According to the heating effect caused by interaction between matters, a series of experiments on the interaction between drugs and cells from human bodies, DNA and physiological saline have been carried out with a MS-80 standard Calvet microcalorimeter. The experiments include: (1) Thermokinetic studies of the effect of anticancer drugs [sodium norcantharidate (ASN), the bioactire materials (Sp.P and Sp.S) from algae etc.]on the cancer cells [Hela, human breast carcinoma (Bcap-37), human adenocarcinoma gastric cells (SGc-7901 and MCF-7) etc.] and the normal cells from human bodies [diploid fibroblasts from human fetal lung (2BS) etc.] at 310.15 K:(2) Studies of the in- tercalation binding of some alkaloidal drugs with the bioactivity to inhibit monoamine oxidase (harmalinc and harmine etc.) to call thymus DNA in neutral aqueous solution at 298.15 K:(3) Studies of the interaction between long acting drugs (long acting oral contraceptive-norgestrel etc.) and slowreleasing drug (Contac) and aqueous solution of 0.9% NaCl at 310.15 K. All the experimental results have given their characteristic thermograms and the interaction enthalpy changes. On the analysis of all the results, the authors put forward a method on application of microcalorimetric technique for screening and examination of medicines. The principle of application and the experimental operation of this method have been expounded, and some results of the above experiments have been discussed. As one of the methods for screening and examining medicines, the microcalorimctric method has some distinguished features and advantages over other methods.

Bovine Serum Albumin (BSA) Microspheres Containing Methotrexate (MTX) I. Pharmaceutical Aspects

Ting-Sen Shi, Xiao-Ping Chen

1993, 2(1):  33-38. 

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Microspheres I, II and III were produced by emulsion technique.Microsphere I was solidified by glutaraldehyde crosslinking, microsphere II was solidified by glutaraldehyde crosslinking and further treated with glycine solution and microsphere Illwas solidified by heating denaturation only.The results showed that the microsphere diameter produced by cross[inking was bigger than that prepared by heating.The microsphere II had higher hydrophilicity than Microsphere I had.The methotrexate (MTX) contents in microspheres I and II were 2.73±0.053%, 2.87±0.119% respectively. microsphere III was only blank microspheres with MTX adsorbed on their surfaces.In vitro release studies, microspheres I and I have maintained sustained release of MTX till the next day, it was found that the drug releases from microspheres I and II were governed by Higuchi diffusion law.

Investigation and Exploitation of New Medicinal Resources of Genus Bupleurum (Umbelliferae) in Qinghai Province and Xizhang (Tibet) Autonomous Region in China

Ying Li, Ji-Xian Guo, Sheng-Li Pan, Da-Shang Luo

1993, 2(1):  39-44. 

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In China, some species of Bupleurum (family Umbelliferae) have been used as Chinese traditional medicine under the name “Chai-Hu” for the treatment of fevers and influenza.In the present paper, the authors report a study on the investigation and exploitation of new medicinal resources of “Chai-Hu” in Qinghai Province and Xizang (Tibet) Autonomous Region where no one has studied this hitherto.18 species, 7 varieties, I form of Bupleurum and a new species (Bupleurum qinghaiense) have been discovered.The taxonomy and preliminary phytochemical studies of the roots of three medicinal plants, B. qinghaiense, B. rnarginatum var.stenophyllum and B.smithii var.parvifolium.are reported in this paper.

Investigation on the Antitumor Activity of Organotin Compound

Jun-Jun Xiao, Jing-Rong Cui, Ya-Xian Su, Jie He, Jun-En Yao

1993, 2(1):  45-52. 

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Changes in the surface structure of cell membrane and the contents of membrane proteins and nuclear DNA of human gastric cancer (BGC-823) cells treated with organotin compound (Et2SnCl2phen) were studied with a scanning electron microscope (SEM), a scanning tunneling, microscope (STM), and a cytofluorophotometer. It was found that Et2SnCl2Phen not only inhibited the cell growth but also remarkably changed the surface structure of the membrane of cancer cells. The surface of Et2SnCl2phen treated cancer cells was relatively smooth and showed fewer microvilli under SEM. STM images showed an uneven and loose distribution of the surface of the cell. In comparison with the untreated cancer cells, there was an evident decrease in the content of membrane proteins and nuclear DNA in Et_2SnCl2phen treated cells.

Effect of Triptolide on Reproductive Endocrinology and Dihydrotestosterone Receptors in Rats

Ying Wang, Yi-Bin Sun, Qiao-Qin Chen, Chun-Yan Lu, Shu-Dong Zong, Zhi-Jian Qian

1993, 2(1):  53-58. 

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Triptolide was given orally to adult male Sprague-Dawley rat sat a dosage of 75 μg/kg for 35 days. After 28 days of treatment, the result of mating tests showed that all the drug treated rats were infertile. At the end of drug treatment, the density of caudal spermatozoa and the weight of cpididymis were reduced significantly. All the spermatozoa were immobile.There was no detectable damage of spermatogenesis and epididymal epithelia in triptolide treated rats under microscopical examination. However, modcrate and severe damage of spermatozoa were seen in the corpus and caudal epididymis. The content of cytosolic and nuclear dihydrotestosterone (DHT) receptors in the caput and caudal epididymides was increased but insignificantly as compared with that of the controls. However, the content of DHT receptor in the cytosal of the ventral prostate was elevated very, significantly (P<0.01). This result suggests that one of the sitcs of action of triptolide might be the epididymis.

Inhibitory Effects of Flufenamic Acid and Mefenamic Acid on Experimental Uveitis in Rabbits

Zhu-Fang Shen, George C.Y.Chiou

1993, 2(1):  59-63. 

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The experimental uveitis was induced by injecting lens protein into the antertor cham- ber of rabbit's eye. A special fluorophotometer was used for objectively measuring the flaoreseein level in the anterior chamber of the eve to rellect the degree of inflammation. When administered intravenously. The inhibitory effects of flufenamic acid and mefenamic acid on experimental uveius showed a dose-dependent relationship, The former at dosages 5.0.12.5 and 250 mg kg decreased the areas under the time-response curve to 22.3%.11.5% and 9.3% of the control, respectively: however the latter at dosages 6.2.12.5 and 25.0 mg/kg decreased the areas under the curve to 35.5%.21.0% and 8.6% of the control, respectively. When instilled by ocular route.50μl of 1% eye-drops of flufenmic acid or mefenamic acid lowered the fluoreseein levels of treated eyes as well as contra-lateral eyes. The areas under the time-response curve for treated eyes were decreased to 20.3% of the control and those of contra-lateral eyes to about 50% of the control. The results indicate that both flufenamic and mefenamic acids, applied intravenously or topically, can inhibit ocular inflammation.

Selective Effect of Qinghaosu on Different Stages of Plasmodium falciparum in Vitro

Zu-Guang Ye, Carolyn Doak, Knox Van Dyke

1993, 2(1):  64-68. 

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Using highly synchronous cultures of Plasmodium falciparum in vitro, the susceptibility of the different stages of the intraerythrocytic parasites to Qinghaosu (QHS) was assessed. The anti-parasitic effect of QHS was measured by comparing the changes of irradiation of 3 H-hypoxanthine incorporated into the nucleic acids of parasites exposed to various concentrations of QHS at different stages of growth. It was found that the trophozoite stage of the parasite was the most sensitive to QHS, whereas the early ring stage was the least sensitive, and the sensitivities of the late ring and schizont stages fell between those of the early ring and trophozoite stages. The results revealed the correlation of stage-dependent effects of QHS with the blockade of the protein metabolism of the parasite.

Effects of Oleanolic Acid on the Immune Complex Allergic Reaction and Inflammation

Chong-Chu Zhou, Xiao-Bo Sun, Wei Liu, Hai-Bo Shi, Hong-Bo Gao, Yan-Bo Miao

1993, 2(1):  69-79. 

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When oleanolic acid (OA) was administered ig before and after sensitization on d 1 to d 5 and d 11 to d 17, it had no apparent effect on Arthus reaction. When it was administered at 48, 24 and 1 h before challenge, however, Arthus reaction was significantly inhibited. OA showed markedly suppressive effects on reversible passive Arthus reaction and leukocyte migratory response. It could significantly stabilize erythrocyte membrane, inhibit the swelling of the rat's hind paw induced by injecting mycostatin, reduce the acid phosphatase content in the inflammatory exudate, suppress the synthesis or release of PGE, histamine, LTB4 and kinin, and the phlogistic action of PGE2, histamine, 5-HT and kinin. In addition, it could decrease the content of malonyldialdehyde (MDA) in hepatic tissue of alcohol-intoxicated mice, and increase the activity of catalase (CAT) in hepatic tissue of mice. OA had no apparent effect on the activity of super-oxide dismutase (SOD) in rat serum, on the content of immune complex in serum of rat with Arthus reaction, on the phagocytosis of monocytc-macrophage system, on the clearance of enzyme-containing immune complex by macrophage, or on the activity of total complement.

Communications

Studies on Biologically Active Principles of Huangqi, Root of Astragalus membranaceous, Isolation and Detection of Constituents Scavenging Superoxide Anion

Xing-Jie Liu, Ming-Hua Jiang, Zheng-Kun Yu, Ji-Mong Zheng, Zhi-Ming Gong, Jing-Hua Zhang, Rui-Hong Dai

1993, 2(1):  80-84. 

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Sudieson Trasitional Chinese Medical Prescripition Ma Xing Shi Gan Tang by Bio-coordination Chemistry

Qiu-Hao Chen, Bing-fu Wu, Wan-Jun Cui

1993, 2(1):  85-87. 

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Characterization of Platelet Activaing Factor (PAF) Binding Sites in Rabbit Platelet Membranes

Yin-Ye Wang, Chang-Ling Li, Ying Ma, Gui-Qiu Han

1993, 2(1):  88-90. 

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