Synthesis and anti-tumor activity of NO-donating derivatives of gambogic acid

AIM:To find a potent apoptosis inducer from gambogic acid and its derivatives.METHODS:Eight new NO-donating derivatives of gambogic acid were synthesized as potential anti-tumor lead compounds and their inhibitory activity on the HT-29,Bel-7402,BGC-823,and A549 cell lines were evaluated in vitro by the MTT assay.RESULTS:Among these compounds,4 with a hydroxyl group at C35 of the gambogic acid moiety was identified as a SKOV3 cell apoptosis inducer through the MTT cell assay,observations of morphological changes,and Annexin-V/PI double staining assay.CONCLUSION:Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for the discovery of new anticancer drugs.