Synthesis and biological evaluation of matrine derivatives as anti-hepatocellular cancer agents

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4267-71. doi: 10.1016/j.bmcl.2016.07.045.

Lichuan Wu ¹, Shuaibing Liu ¹, Jinrui Wei ², Dong Li ¹, Xu Liu ¹, Jianyi Wang ¹, Lisheng Wang ³

Affiliations

1 School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China.
2 School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China; Guangxi Scientific Research Center of Traditional Chinese Medicine, Guangxi University of Chinese Medicine, Nanning, Guangxi 530200, PR China.
3 School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China. Electronic address: w_lsheng@163.com.

PMID: 27481558 DOI: 10.1016/j.bmcl.2016.07.045

Abstract

We delineate herein the synthesis and anti-cancer effects of 15 matrine derivatives. The in vitro growth inhibitory assays showed that most of the prepared compounds exhibited improved anti-proliferative activities towards Cancer cells with IC50 17-109 times lower than that of matrine. Compounds CH6 showed the most potent anti-proliferative activities in the four tested Cancer cell lines. Moreover, compound CH6 could induce G1 cell cycle arrest and inhibit cell migration in human hepatocellular Cancer cell lines Bel-7402 and HepG2 through up-regulation of P21, P27 and E-cadherin and down-regulation of N-Cadherin.

Keywords

Anticancer activity; Cell cycle; Hepatocarcinoma; Matrine derivatives; Migration.

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