Regioselective Hydroxylation of Phloretin, a Bioactive Compound from Apples, by Human Cytochrome P450 Enzymes
نویسندگان
چکیده
منابع مشابه
Characterization of human cytochrome P450 enzymes.
Many biochemical approaches have been applied to the human cytochrome P450 enzymes, and more than 20 different gene products have been characterized with regard to their properties and catalytic specificities. The complement of the various cytochrome P450 enzymes in a given individual varies markedly, and dramatic differences may be seen in drug metabolism, pharmacological response, and suscept...
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This study demonstrates the stereoselective metabolism of the optical isomers of omeprazole in human liver microsomes. The intrinsic clearance (CL(int)) of the formation of the hydroxy metabolite from S-omeprazole was 10-fold lower than that from R-omeprazole. However, the CL(int) value for the sulfone and 5-O-desmethyl metabolites from S-omeprazole was higher than that from R-omeprazole. The s...
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The stereoselective metabolism of lansoprazole enantiomers was evaluated by incubation of human liver microsomes and cDNA-expressed cytochrome p450 (p450) enzymes to understand and predict their stereoselective disposition in humans in vivo. The intrinsic clearances (Clint) of the formation of both hydroxy and sulfone metabolites from S-lansoprazole were 4.9- and 2.4-fold higher than those from...
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The metabolism of clozapine was studied in vitro using cDNA-expressed human cytochrome P450 (CYP) enzymes 1A2, 3A4, 2C9, 2C19, 2D6, and 2E1. CYP1A2, 3A4, 2C9, 2C19, and 2D6 were able to N-demethylate clozapine. N-Oxide formation was exclusively catalyzed by CYP3A4. CYP2E1 did not metabolize clozapine. With regard to quantitative relationships, CYP1A2, 2C9, 2C19, and 2D6 displayed KM values rang...
متن کاملAn analysis of the regioselectivity of aromatic hydroxylation and N-oxygenation by cytochrome P450 enzymes.
Quinoline was used to probe the steric and electronic contributions to rates of aromatic oxidation of nitrogen-containing, multiring substrates by cytochrome P450 (P450) enzymes. The regioselectivity of the P450 oxidation of quinoline was determined experimentally by identifying and measuring the ratios of metabolites. The laboratory results were compared with those obtained computationally by ...
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ژورنال
عنوان ژورنال: Pharmaceuticals
سال: 2020
ISSN: 1424-8247
DOI: 10.3390/ph13110330