title: Synthesis and biological evaluation of matrine derivatives as anti-hepatocellular cancer agents.
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.
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China.
authors.forename: Lichuan
authors.initials: L
authors.lastname: Wu
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China.
authors.forename: Shuaibing
authors.initials: S
authors.lastname: Liu
authors.affiliation: 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.
authors.forename: Jinrui
authors.initials: J
authors.lastname: Wei
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China.
authors.forename: Dong
authors.initials: D
authors.lastname: Li
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China.
authors.forename: Xu
authors.initials: X
authors.lastname: Liu
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China.
authors.forename: Jianyi
authors.initials: J
authors.lastname: Wang
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China. Electronic address: w_lsheng@163.com.
authors.forename: Lisheng
authors.initials: L
authors.lastname: Wang
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D015820:Cadherins / Q000378:metabolism; D006528:Carcinoma, Hepatocellular / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D050759:Cyclin-Dependent Kinase Inhibitor p21 / Q000378:metabolism; D050760:Cyclin-Dependent Kinase Inhibitor p27 / Q000378:metabolism; D015536:Down-Regulation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects*; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000378:metabolism / Q000473:pathology; D011807:Quinolizines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship; D015854:Up-Regulation / Q000187:drug effects; D000093842:Matrines
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D015820:Cadherins; D050759:Cyclin-Dependent Kinase Inhibitor p21; D011807:Quinolizines; D050760:Cyclin-Dependent Kinase Inhibitor p27; D000093842:Matrines
keywords: Anticancer activity; Cell cycle; Hepatocarcinoma; Matrine derivatives; Migration