毛茛甙体外细胞毒活性及其机制  

THE CYTOTOXICITY AND ACTION MECHANISM OF RANUNCULIN IN VITRO

作　　者：李润沼[1] 籍秀娟[1] 

机构地区：[1]中国医学科学院药物研究所

出　　处：《药学学报》1993年第5期326-331,共6页Acta Pharmaceutica Sinica

摘　　要：研究表明,毛茛甙对KB细胞、Bel_(7402)细胞的IC_(50)分别为0.21和0.35 μmol/L;对细胞大分子物质的生物合成以抑制DNA合成最强(IC_(50)=0.35μmol/L)。作用机制研究表明,至少有两种机制参与毛茛甙的体外细胞毒作用:抑制DNA聚合酶作用下的DNA合成;促进超氧阴离子自由基的生成。This paper describes the cytotoxicity of ranunculin(RAN) and its mechanism of action. The IC_(50) of RAN against the KB and Bel_(7402) cells in colony test were found to be 0. 21 and 0. 35μmol/L respectively. RAN inhibited the incorporation of ~3H-labeled precursors into DNA and RNA of L_(1210) cells. RAN (15 μmol/L) markedly decreased DNA synthesis catalyzed by DNA ploymerase Ⅰ and promoted the generation of superoxide anions in DMSO/KO_2 system. In the meantime, SOD and CAT were shown to partly revoke the inhibitory effects of RAN upon the incorporation of ~3H-TdR into DNA. No direct reaction between RAN and DNA template was observed and no effect of RAN on DNA TOPO Ⅱ or RNA polymerase Was found. Our results suggest that the cytotoxicity of RAN in vitro may be due to inhibition of DNA polymerase and increase of oxygen free radicals.

关 键 词：毛莨甙 抗肿瘤作用 合成 细胞毒性 

分 类 号：R914.5[医药卫生—药物化学]