原小檗碱型生物碱的体外细胞毒性。

In vitro cytotoxicity of the protoberberine-type alkaloids.

作者信息

Iwasa K, Moriyasu M, Yamori T, Turuo T, Lee D U, Wiegrebe W

机构信息

Kobe Pharmaceutical University, 4-19-1 Motoyamakita, Higashinada-ku, Kobe 658-8558, Japan.

出版信息

J Nat Prod. 2001 Jul;64(7):896-8. doi: 10.1021/np000554f.

DOI:10.1021/np000554f

PMID:11473418

Abstract

In vitro cytotoxic activities of 24 quaternary protoberberine alkaloids related to berberine have been evaluated using a human cancer cell line panel coupled with a drug sensitivity database. Extending the alkyl chain at position 8 or 13 strongly influenced the cytotoxic activity, that is, relative lipophilicity as well as the size of the substituent affects cytotoxicity. The highest level of activity was observed in 8- or 13-hexyl-substituted derivatives of berberine. Structure-activity relationships are described.

摘要

利用一组人类癌细胞系并结合药物敏感性数据库，对24种与小檗碱相关的季铵原小檗碱生物碱的体外细胞毒性活性进行了评估。在8位或13位延长烷基链对细胞毒性活性有强烈影响，也就是说，相对亲脂性以及取代基的大小会影响细胞毒性。在小檗碱的8-或13-己基取代衍生物中观察到最高水平的活性。描述了构效关系。