Inhibition of ethoxyresorufin deethylase activity by natural flavonoids in human and rat liver microsomes.
Several flavones and flavonols (chrysin, quercetin, luteolin, flavone and 7, 8-benzoflavone) were found to inhibit ethoxyresorufin deethylase (EROD) activity in human and rat liver microsomes. In man, molecules without hydroxyl groups are more powerful inhibitors than polyhydroxylated flavonoids (7, 8-benzoflavone greater than flavone greater than chrysin greater than luteolin greater than quercetin greater than morin). In rat, chrysin was the strongest inhibitor and the less effective were morin and 7,8-benzoflavone. For all molecules human microsomes were more sensitive than rat microsomes. The most important difference concerned 7,8-benzoflavone which was 10,000-fold more potent in man.
Siess
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MH
Station de Recherches sur la Qualité des Aliments de l'Homme, INRA, Dijon, France.
Le Bon
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AM
Suschetet
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M
Rat
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P
D000818:Animals; D019363:Cytochrome P-450 CYP1A1; D065607:Cytochrome P-450 Enzyme Inhibitors; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology*; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity; D013329:Structure-Activity Relationship
D065607:Cytochrome P-450 Enzyme Inhibitors; D005419:Flavonoids; D010088:Oxidoreductases; D019363:Cytochrome P-450 CYP1A1