The Inhibitory Effect of Flavonoid Aglycones on the Metabolic Activity of CYP3A4 Enzyme

摘要: Flavonoids are natural compounds that have been extensively studied due to their positive effects on human health. There over 4000 flavonoids found in higher plants and beneficial shown vitro as well vivo. However, data pharmacokinetics influence metabolic enzymes is scarce. The aim of this study was focus possible interactions between the 30 most commonly encountered flavonoid aglycones activity CYP3A4 enzyme. 6β-hydroxylation testosterone used marker reaction activity. Generated product determined by HPLC coupled with diode array detector. Metabolism time dependence, direct inhibition, were tested determine if inhibition reversible and/or irreversible. Out tested, 7 significantly inhibited CYP3A4, prominent being acacetin 95% enzyme at 1 µM concentration. Apigenin showed acacetin, chrysin combined irreversible while dimethylether, isorhamnetin, pinocembrin, tangeretin pure inhibition. These results alert flavonoid⁻drug level CYP3A4.