Synthesis and Cytotoxicity Evaluation of 13-n-Alkyl Berberine and Palmatine Analogues as Anticancer Agents

文献类型： 外文期刊

第一作者： Zhang, Lei

作者： Zhang, Lei;Li, Jingjing;Li, Naisan;Wang, Jing;Wang, Yongbin;Yao, Qizheng;Ma, Fei;Ma, Fei;Yao, Shining;Wang, Xiuzhen

作者机构：

关键词： berberine;palmatine;alkylation;cytotoxicity;antitumor

期刊名称：MOLECULES （ 影响因子：4.411； 五年影响因子：4.587 ）

ISSN： 1420-3049

年卷期： 2012 年 17 卷 10 期

页码：

收录情况： SCI

摘要： By introducing long carbon-chain alkyl groups at the C-13 position of berberine and palmatine, 13-n-hexyl/13-n-octyl berberine and palmatine chloride analogues 4a-d were synthesized and examined by MTT assays for cytotoxic activity in seven human cancer cell lines (7701QGY, SMMC7721, HepG2, CEM, CEM/VCR, KIII, Lewis), yielding IC50 values of 0.02 +/- 0.01-13.58 +/- 2.84 mu M. 13-n-Octyl palmatine (compound 4d) gave the most potent inhibitor activity, with an IC50 of 0.02 +/- 0.01 mu M for SMMC7721. In all cases, the 13-n-alkyl berberine and palmatine analogues 4a-d were more cytotoxic than berberine and palmatine. In addition, compounds 4a-d also exhibited more potent cytotoxicity than berberine and palmatine in mice with S180 sarcoma xenografted in vivo. The primary screening results indicated that the 13-n-hexyl/13-n-octyl berberine and palmatine analogues might be valuable source for new potent anticancer drug candidates.

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