Abstract:

Structural modifications on 3-OH and 17-COOH were performed with ursolic acid as the starting compound. Nine compounds were synthesized and their structures were confirmed by IR, ¹H NMR and MS. Cell growth inhibitory effects of the derivatives against human hepato carcinoma cell HepG2 were evaluated by MTT assay. The results demonstrate that all the tested compounds exhibited certain antitumor activities in vitro and showed a dose-dependent manner. Derivative 9 had the best anti-cancer activity. Cell apoptosis changes were observed by Hoechst 33342/PI fluorescent stain after derivative 9 interacted with cell for 24 h. The dark blue/light red fluorescence images were taken by a laser scanning confocal microscope. Cell cycles were analyzed by flow cytometry that the cells were blocked in the S phase, and the effects were enhanced gradually with the increment of concentration.

Key words: Ursolic acid, derivatives, synthesize, apoptosis