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.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids / chemical synthesis
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Alkaloids / chemistry*
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Alkaloids / toxicity
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / toxicity*
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Cadherins / metabolism
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Carcinoma, Hepatocellular / metabolism
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Carcinoma, Hepatocellular / pathology
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Cell Line, Tumor
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Cell Movement / drug effects
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Cell Proliferation / drug effects*
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Cell Survival / drug effects
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Cyclin-Dependent Kinase Inhibitor p21 / metabolism
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Cyclin-Dependent Kinase Inhibitor p27 / metabolism
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Down-Regulation / drug effects
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Drug Screening Assays, Antitumor
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G1 Phase Cell Cycle Checkpoints / drug effects*
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Hep G2 Cells
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Humans
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Liver Neoplasms / metabolism
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Liver Neoplasms / pathology
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Matrines
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Quinolizines / chemical synthesis
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Quinolizines / chemistry*
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Quinolizines / toxicity
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Structure-Activity Relationship
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Up-Regulation / drug effects
Substances
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Alkaloids
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Antineoplastic Agents
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Cadherins
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Cyclin-Dependent Kinase Inhibitor p21
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Quinolizines
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Cyclin-Dependent Kinase Inhibitor p27
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Matrines