Synthesis of 8-alkyl-13-bromo-berberine hydrochloride derivatives and their effect on proliferation of human HepG2 cell line / 中草药
Chinese Traditional and Herbal Drugs
;
(24): 1765-1770, 2010.
Article
in Chinese
| WPRIM
| ID: wpr-855740
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Chinese Traditional and Herbal Drugs
Year:
2010
Type:
Article
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