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.