In vitro cytotoxicity of the protoberberine-type alkaloids
In vitro cytotoxicity of the protoberberine-type alkaloids
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DOI：
10.1021/np000554f
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发表时间：
2001-07-01
影响因子：
5.1
通讯作者：
Wiegrebe, W
中科院分区：
文献类型：
--
作者：
Iwasa, K;Moriyasu, M;Wiegrebe, W
在体外，24个与黄连素相关的四元原黄连素生物碱的细胞毒活性已经用一个与药物敏感性数据库相结合的人类癌细胞系进行了评估。在第8位或第13位延伸烷基对细胞毒活性有很大影响，即相对亲脂性和取代基的大小影响细胞毒活性。黄连素的8-或13-己基取代衍生物的活性最高。描述了结构-活性关系。
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.