%0 Journal Article
%T Synthesis and Cytotoxicity Evaluation of 13-n-Alkyl Berberine and Palmatine Analogues as Anticancer Agents
%A Lei Zhang
%A Jingjing Li
%A Fei Ma
%A Shining Yao
%A Naisan Li
%A Jing Wang
%A Yongbin Wang
%A Xiuzhen Wang
%A Qizheng Yao
%J Molecules
%D 2012
%I MDPI AG
%R 10.3390/molecules171011294
%X 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¨Cd 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 ¡À 0.01¨C13.58 ¡À 2.84 ¦ÌM. 13-n-Octyl palmatine (compound 4d) gave the most potent inhibitor activity, with an IC50 of 0.02 ¡À 0.01 ¦ÌM for SMMC7721. In all cases, the 13-n-alkyl berberine and palmatine analogues 4a¨Cd were more cytotoxic than berberine and palmatine. In addition, compounds 4a¨Cd 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.
%K berberine
%K palmatine
%K alkylation
%K cytotoxicity
%K antitumor
%U http://www.mdpi.com/1420-3049/17/10/11294