Source:http://linkedlifedata.com/resource/pubmed/id/18996626
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
2009-4-20
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pubmed:abstractText |
Gambogic acid (GA), a natural product, exhibits high potency in inhibiting cancer cell growth through the effective induction of apoptosis. In order to investigate the structure-activity relationships of GA derivatives, 11 oxidized derivatives of GA were synthesized. Some of them showed strong inhibitory effects on HT-29, Bel-7402, BGC-823, A549, and SKOV 3 cell lines. Moreover, in this paper the cellular growth inhibitor 39-hydroxy-6-methoxy-gambogic acid methyl ester (10) was identified as a HepG2 cell apoptosis inhibitor through Annexin-V/PI double staining assay and the expression of the related apoptotic proteins (Bax and Bcl-2). Compound 10 may serve as a potential lead compound for the development of new anticancer drugs. Further SAR studies of GA derivatives indicated that modification of carbon-carbon double bond at C-32/33 or C-37/38 and of the methyl groups at C-39/C-35 can improve antitumor activity.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1768-3254
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2611-20
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pubmed:meshHeading |
pubmed-meshheading:18996626-Apoptosis,
pubmed-meshheading:18996626-Biological Factors,
pubmed-meshheading:18996626-Cell Line, Tumor,
pubmed-meshheading:18996626-Cell Proliferation,
pubmed-meshheading:18996626-Cell Survival,
pubmed-meshheading:18996626-Dose-Response Relationship, Drug,
pubmed-meshheading:18996626-Drug Design,
pubmed-meshheading:18996626-Drug Screening Assays, Antitumor,
pubmed-meshheading:18996626-Humans,
pubmed-meshheading:18996626-Molecular Structure,
pubmed-meshheading:18996626-Stereoisomerism,
pubmed-meshheading:18996626-Structure-Activity Relationship,
pubmed-meshheading:18996626-Xanthones
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pubmed:year |
2009
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pubmed:articleTitle |
Studies on chemical structure modification and biology of a natural product, gambogic acid (I): Synthesis and biological evaluation of oxidized analogues of gambogic acid.
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pubmed:affiliation |
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Evaluation Studies
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