In vitro inhibition of human CYP2E1 and CYP3A by quercetin and myricetin in hepatic microsomes is not gender dependent
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60076658%3A12520%2F17%3A43895289" target="_blank" >RIV/60076658:12520/17:43895289 - isvavai.cz</a>
Result on the web
<a href="http://www.sciencedirect.com/science/article/pii/S0300483X17300586" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0300483X17300586</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.tox.2017.02.012" target="_blank" >10.1016/j.tox.2017.02.012</a>
Alternative languages
Result language
angličtina
Original language name
In vitro inhibition of human CYP2E1 and CYP3A by quercetin and myricetin in hepatic microsomes is not gender dependent
Original language description
This is the first in vitro study to investigate gender-related differences in the regulation of human cytochrome P450 by the flavonoids. Activities of CYP2E1 and CYP3A were measured in the presence of quercetin, myricetin, or isorhamnetin in hepatic microsomal pools from male and female donors. Hydroxylation of p-nitrophenol (PNPH) was measured to determine CYP2E1 activity, and O-dealkylation of 7-benzyloxy-4-trifluoromethylcoumarin (BFC) was measured to determine CYP3A activity. Quercetin, but not myricetin or isorhamnetin, competitively inhibited PNPH activity in human recombinant cDNAexpressed CYP2E1 with the Ki = 52.1 +/- 6.31 mu M. In the human microsomes, slight inhibition of PNPH activity by quercetin was not considered as physiologically relevant. Quercetin inhibited BFC activity in human recombinant cDNA-expressed CYP3A4 competitively with the Ki = 15.4 +/- 1.52 mu M, and myricetin noncompetitively with the Ki = 74.6 +/- 7.99 mu M. The degree of inhibition by quercetin was similar between genders. Myricetin showed somewhat stronger inhibition in female pools, but the Ki values were higher than physiologically relevant concentrations. Isorhamnetin did not affect either PNPH or BFC activity. We concluded that observed inhibition of CYP2E1 and CYP3A by some flavonols were not gender dependent.
Czech name
—
Czech description
—
Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
30304 - Public and environmental health
Result continuities
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)
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Toxicology
ISSN
0300-483X
e-ISSN
—
Volume of the periodical
381
Issue of the periodical within the volume
15 April 2017
Country of publishing house
IE - IRELAND
Number of pages
9
Pages from-to
10-18
UT code for WoS article
000398651600002
EID of the result in the Scopus database
2-s2.0-85013830851