ABSTRACT
Objective: To study the antitumor activity of berberine which was alkylated based on the development of new antitumor drug. Methods: The alkylation and bromination of berberine were performed with Grignard reagent and bromine respectively to give 8-alkyl-13-bromo-berberine derivatives in good to excellent yields. The chemical structures of the derivatives were identified by UV, IR, 1H-NMR, and elemental analysis. The antiproliferative effect of the derivatives on human hepatoma cell line HepG2 was evaluated by MTT after 48 h incubation. Results: The results showed that the length of carbon chain of the derivatives was highly correlated with the tumor cell sensitivity and 8-octyl-13-bromo-berberine showed the remarkable activity. Its inhibitory rate was 96. 82% at the concentration of 32 μg/mL and IC50 was 3.33 μg/mL. Conclusion: Known from IC50, the antitumor activity could be enhanced within eight carbon atoms as the bromide side chain extension.