Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 6, Pages 2611-2620Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.09.034
Keywords
Gambogic acid derivatives; Anti-tumor; Apoptosis inducer; Structure-activity relationship
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Funding
- 863 High-Tech Project of China [2002AA2Z3112, 2004AA2Z3A10]
- Key Projects of Science and Technology Research of Ministry of Education of PRC [2006-106094]
- Projects of Natural Science Foundation of Jiangsu Province [BK2006149]
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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 CA derivatives, 11 oxidized derivatives of CA 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 CA 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. (C) 2008 Elsevier Masson SAS. All rights reserved.
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