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: [email protected].
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.