Effects of bioflavonoids on hepatic P450 activities

Published on Jan 1, 1995in Xenobiotica1.902
· DOI :10.3109/00498259509061876
M. T. Obermeier1
Estimated H-index: 1
(BMS: Bristol-Myers Squibb),
R. E. White1
Estimated H-index: 1
(BMS: Bristol-Myers Squibb),
C. S. Yang6
Estimated H-index: 6
(RU: Rutgers University)
1. The effects of tangeretin, green tea flavonoids, and other flavonoids on 7-ethoxyre-sorufin-O-deethylase (EROD; 450 1A), 7-pentoxyresorufin-O-dealkylase (PROD; P450 2B), p-nitrophenol hydroxylase (PNPH, P450 2E1), and erythromycin-N-demethylase (ERDM; P450 3A) were examined in induced rat liver microsomes. EROD, PNPH, ERDM, and nifedipine oxidase (NIFO; P450 3A4) were examined in human liver microsomes.2. All flavonoids tested inhibited EROD activity at higher concentrations in liver microsomes. Flavone and tangeretin were potent inhibitors of EROD, with IC50's of 0 ± 7 and 0 ± 8 μM respectively in rat liver microsomes and 0 ± 15 and 16 μM respectively in human liver microsomes. The green tea flavonoid (—)-epicatechin-3-gallate (ECG) was the most potent inhibitor of EROD in human liver microsomes (IC50 = 75μM). The effect of the green tea flavonoids on EROD was complex; in addition to inhibition at high concentrations of flavonoid, moderate activation was seen at lower concentrations.3. 450 2B-, 2E1- a...
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