| Apoptosis-inducing activity of new pyrazole emodin derivatives in human hepatocellular carcinoma HepG2 cells. | |
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MedLine Citation:
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PMID: 17541163 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of new pyrazole derivatives from emodin synthesized in our lab have been shown to have much stronger cytotoxicity than emodin against various tumor cell lines. This study was to examine the apoptosis-inducing activity of these new emodin derivatives in human hepatocellular carcinoma HepG2 cell culture for a better understanding of their cytotoxic effects on the cancer cells. Several major events in the induction of cell apoptosis, nuclear chromatin condensation, DNA fragmentation, caspase-3 activation and poly ADP-ribose polymerase (PARP) cleavage were detected in the cells after treatment with the compounds at various concentrations. Of the seven emodin derivatives tested at a dose of 10 microM and within a treatment period of 24 h, only compounds 1 and 3 effectively induced all these apoptotic events in the cancer cells. The apoptosis-inducing activity of the compounds showed a positive correlation to their cytotoxic activity, suggesting a close connection between the growth inhibition and apoptosis induction of the cancer cells by these pyrazole emodin derivatives. |
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Authors:
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Xiao-Dong Wang; Lian-Quan Gu; Jian-Yong Wu |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Biological & pharmaceutical bulletin Volume: 30 ISSN: 0918-6158 ISO Abbreviation: Biol. Pharm. Bull. Publication Date: 2007 Jun |
Date Detail:
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Created Date: 2007-06-01 Completed Date: 2007-07-17 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9311984 Medline TA: Biol Pharm Bull Country: Japan |
Other Details:
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Languages: eng Pagination: 1113-6 Citation Subset: IM |
Affiliation:
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School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Apoptosis
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drug effects* Carcinoma, Hepatocellular / drug therapy*, pathology Caspase 3 / metabolism Cell Line, Tumor Cell Nucleus / drug effects Cell Proliferation / drug effects Cell Survival / drug effects DNA Fragmentation / drug effects Dose-Response Relationship, Drug Emodin / chemistry, metabolism*, toxicity* Enzyme Activation / drug effects Formazans / metabolism Humans Liver Neoplasms / drug therapy*, pathology Molecular Structure Poly(ADP-ribose) Polymerases / metabolism Tetrazolium Salts / metabolism Time Factors |
| Chemical | |
Reg. No./Substance:
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0/Formazans; 0/Tetrazolium Salts; 23305-68-2/MTT formazan; 518-82-1/Emodin; EC 2.4.2.30/Poly(ADP-ribose) Polymerases; EC 3.4.22.-/Caspase 3 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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