DNA拓扑异构酶Ⅰ抑制剂的研究  

A Study on the Inhibitors of DNA Topoisomerase Ⅰ

作　　者：唐宝书[1] 王理开[1] 徐晓利[1] 

机构地区：[1]中山医科大学生物化学教研室

出　　处：《中山大学学报（医学科学版）》1989年第4期1-4,2,共5页Journal of Sun Yat-Sen University:Medical Sciences

摘　　要：测试了172种化合物对拓扑酶Ⅰ的抑制作用,发现聚阴离子DIVEMA、FMA、FMAHA及中药盐酸小檗碱、槲皮素、黄岑素甙、楤木皂甙A及昆明山海棠总提出物对拓扑酶Ⅰ有抑制作用,其中聚阴离子的抑制作用特别强烈,DNA Topoisomerases are the enzymes that catalyse the interconversion of the three dimensional conformation of DNA. They play important roles on the biological functions related to DNA. The specific inhibitors of DNA topoisomerases are the useful tool in studying their biological functions. In this experiment, we collected 172 natural compounds or synthetic drugs and carried out the test of inhibition on DNA topoisomerase Ⅰ We found that DIVEMA, FMA, FMAHA, Berberine, Quercetin, Scutellarin, Araloside A and the extract of total hypoglaucum inhibited the activity of DNA topoisomerase Ⅰ The lowest concentrations which completely inhibited the activity of DNA topoisomerase Ⅰ were 0.08μg/ml, o.6μg/ml, 0.5μg/ml, 75 nmol, 100μmol, 540μmol, 540μmol and 15.6μg/ml respectively. DIVEMA in concentration below 10 [tg/ml had no effect on DNA topoisomerase Ⅱ and also no effect on DNase Ⅰ in concentration of 1 mg/ml. Berberine in concentration of 1 mg/ml had no effect on DNA topoisomerase Ⅱ and DNase Ⅰ.

关 键 词：DNA拓扑异构酶Ⅰ 抑制作用 聚阴离子 

分 类 号：R[医药卫生]