Role of rat cytochromes P450 in the oxidation of 17?-ethinylestradiol

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F14%3A10283266" target="_blank" >RIV/00216208:11310/14:10283266 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.etap.2014.10.004" target="_blank" >http://dx.doi.org/10.1016/j.etap.2014.10.004</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.etap.2014.10.004" target="_blank" >10.1016/j.etap.2014.10.004</a>

Result language
angličtina
Original language name
Role of rat cytochromes P450 in the oxidation of 17?-ethinylestradiol
Original language description
17?-Ethinylestradiol (EE2) is an endocrine disruptor (ED) used as an ingredient of oral contraceptives. Rat hepatic microsomes metabolize EE2 to three products; two of them are hydroxylated EE2 derivatives. Of the hydroxylation reactions, 2-hydroxylation, is the major reaction. Cytochrome P450 (CYP) plays a major role in EE2 hydroxylation. To resolve which rat CYPs are responsible for EE2 oxidation, three approaches were used: induction of specific CYPs, selective inhibition of CYPs, and recombinant ratCYPs. The results demonstrate that EE2 is hydroxylated by several rat CYPs, among them CYP2C6 and 2C11 are most efficient in 2-hydroxy-EE2 formation, while CYP2A and 3A catalyze EE2 hydroxylation to the second product. EE2 is also an inhibitor of CYP2C-and CYP3A-catalyzed hydroxylation of endogenous EDs progesterone and testosterone. EE2 acts as a reversible inhibitor of CYP3A-mediated progesterone 6?-hydroxylation and inactivates CYP3A- and CYP2C-catalyzed testosterone 6?-hydroxylatio
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
<a href="/en/project/GA14-18344S" target="_blank" >GA14-18344S: Development of nanoparticle-based cytostatics and enzymes for enhanced chemotherapy of human neuroblastomas and study of mechanisms of their action</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2014
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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