Abstract
A series of new emodin derivatives modified at the C-3 and the C-6 positions were synthesized, and evaluated for their anticancer activities in vitro and in vivo. Among them, Compounds 5g and 5h had more significant antiproliferative ability against HepG2, BGC-823, AGS cancer cell lines and low cytotoxicity to HELF normal cell line, respectively. Compounds 5g and 5h induced AGS cell cycle arrest at G0/G1 phase and induce apoptosis via activation of caspase-3 and caspase-9 enzyme. In vivo studies using H22 xenografts in Kunming mice were conducted with 5g and 5h. The results revealed that the medium dosage group (10 mg/kg) of 5g and the high dosage group (25 mg/kg) of 5h showed significant antitumor activity compared to the control 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