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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)
Abstract
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...
  • References (26)
  • Citations (150)
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References26
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Flavonoids are widely occurring in our diet. In this study, the effects of nine flavonoids on acetaminophen (APAP) oxidation and related cytochrome P450 (P450) enzyme activities were investigated. With rat liver microsomes, APAP oxidation was stimulated 2- to 4-fold by 50 microM flavone or tangeretin and inhibited 65% by myricetin or quercetin. Only a slight inhibition of APAP oxidation was caused by naringenin. All the effects cited herein were from experiments with 50 microM flavonoids. With h...
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The content of the potentially anticarcinogenic flavonoids quercetin, kaempferol, myricetin, apigenin, and luteolin of commonly consumed beverages was determined by RP-HPLC with UtT detection. Flavonoid levels in beer, coffee, chocolate milk, and white wine were below 1 mg/L. Twelve types of tea infusion, six types of wine, apple juice, tomato juice, grape juice, orange juice, grapefruit juice, and lemon juice were analyzed. No luteolin or apigenin were detected in any of the beverages. In red w...
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