In vitro effects of the citrus flavonoids diosmin, naringenin and naringin on the hepatic drug-metabolizing CYP3A enzyme in human, pig, mouse and fish

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60076658%3A12520%2F16%3A43890497" target="_blank" >RIV/60076658:12520/16:43890497 - isvavai.cz</a>
Result on the web
<a href="http://www.sciencedirect.com/science/article/pii/S000629521630065X" target="_blank" >http://www.sciencedirect.com/science/article/pii/S000629521630065X</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bcp.2016.04.011" target="_blank" >10.1016/j.bcp.2016.04.011</a>

Result language
angličtina
Original language name
In vitro effects of the citrus flavonoids diosmin, naringenin and naringin on the hepatic drug-metabolizing CYP3A enzyme in human, pig, mouse and fish
Original language description
Flavonoids are known to have effects on cytochrome P450 enzymatic activity. However, little effort has been made to examine species differences and the relevance of studies on mammalian and fish microsomes so that extrapolations can be made to humans. Therefore, the effects of several naturally occurring flavonoids on the activity of CYP3A-dependent 7-benzyloxy-4-trifluoromethylcoumarin O-debenzylase (BFCOD) were evaluated in human, pig, mouse, and juvenile rainbow trout sources of hepatic microsomes. Each was exposed to three concentrations (1, 10, and 100 mu M) of diosmin, naringin, and naringenin. Naringenin competitively inhibited BFCOD activity (K-i values were 24.6 mu M in human, 15.6 mu M in pig, and 19.6 mu M in mouse microsomes). In fish, BFCOD activity was inhibited in a noncompetitive manner (K-i = 7 mu M). Neither diosmin nor naringenin affected BFCOD activity in hepatic microsomes from the studied model organisms. These results suggest that dietary flavonoids potentially inhibit the metabolism of clinical drugs.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
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Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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