Inhibition of methoxyresorufin demethylase activity by flavonoids in human liver microsomes

Flavonoids are a class of dietary phytochemicals with anticarcinogenic properties. A Series of ten structurally related flavonoids were evaluated for their effect on methoxyresorufin O-demethylase (MROD) activity in human liver microsomes. All compounds inhibited this cytochrome P450 1A2 (CYP1A2) me...

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Bibliographic Details
Published in:Life sciences (1973) 1998, Vol.63 (8), p.PL119-PL123
Main Authors: Zhai, Suoping, Dai, Renke, Wei, Xiaoxiong, Friedman, Fred K., Vestal, Robert E.
Format: Article
Language:English
Subjects:
Adult
CYP1A2
Cytochrome P-450 CYP1A2 Inhibitors
Cytochrome P-450 Enzyme Inhibitors
Cytochrome P-450 Enzyme System
Enzyme Inhibitors - pharmacology
Female
Flavones
flavonoids
Flavonoids - pharmacology
galangin
human liver microsomes
Humans
inhibition
Isoenzymes - antagonists & inhibitors
methoxyresorufin
Microsomes, Liver - enzymology
Oxidoreductases - antagonists & inhibitors
phytochemicals
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Summary:Flavonoids are a class of dietary phytochemicals with anticarcinogenic properties. A Series of ten structurally related flavonoids were evaluated for their effect on methoxyresorufin O-demethylase (MROD) activity in human liver microsomes. All compounds inhibited this cytochrome P450 1A2 (CYP1A2) mediated activity. 3,5,7-Trihydoxyflavone (galangin) was the most potent inhibitor, followed by 3-hydroxyflavone and flavone. The relative inhibitory potency of flavonoids is related to their structures. The results suggest that flavonoids may modulate pharmacological and toxicological effects mediated by CYP1A2.
ISSN:0024-3205
1879-0631
DOI:10.1016/S0024-3205(98)00323-3