Abstract
Twenty-six emodin derivatives (17 novel) which attach quaternary ammonium salt were synthesized and evaluated for their anticancer activities in vitro and in vivo. Compounds 11g + 12g and 11h + 12h had more significant antiproliferative ability against three cancer cell lines and low cytotoxicity to HELF. 11g + 12g and 11h + 12h induced AGS cell apoptosis and arrested cell cycle at the G(0)/G(1) phase in a dose-dependent manner. Furthermore, the activities of the caspase-3, -9 enzymes were increased in the treated cells. In vivo studies revealed that compounds 11g + 12g and 11h + 12h showed significant anti-tumor activity compared with controlled group.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects
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Cell Cycle / drug effects
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Emodin / chemical synthesis
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Emodin / chemistry
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Emodin / pharmacology*
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Hep G2 Cells
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Humans
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Liver Neoplasms, Experimental / drug therapy*
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Mice
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Mice, Inbred Strains
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Molecular Structure
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Quaternary Ammonium Compounds / chemical synthesis
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Quaternary Ammonium Compounds / chemistry
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Quaternary Ammonium Compounds / pharmacology*
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Salts / chemical synthesis
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Salts / chemistry
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Salts / pharmacology
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Quaternary Ammonium Compounds
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Salts
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Emodin