Free-B-Ring flavonoids as potential lead compounds for colon cancer therapy.

Although flavonoids have been identified as a versatile source of anticancer agents, to the best of our knowledge, no study has yet investigated their anticolon cancer activity in depth. Therefore, the aim of this study was to investigate the association between the structural characteristics of flavonoids and their anticolon cancer activity in the Caco-2 human colon cancer cell line. Our findings demonstrated that the hydroxylation of C5 and C7 in ring A significantly enhanced the anticolon cancer activity of flavonoids over that of 5-fluorouracil, the classic reference cytotoxic agent. By contrast, the glycosylation or the presence of hydroxyl groups in ring B significantly decreased flavonoid anticancer activity. Collectively, these findings suggest a novel, rational design of flavonoid-related compounds that may improve the treatment of colorectal cancer.