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Titolo:
Resveratrol, a red wine constituent, is a mechanism-based inactivator of cytochrome P450 3A4
Autore:
Chan, WK; Delucchi, AB;
Indirizzi:
Univ Pacific, Dept Pharmaceut & Med Chem, Sch Pharm & Hlth Sci, Stockton, CA 95211 USA Univ Pacific Stockton CA USA 95211 arm & Hlth Sci, Stockton, CA 95211 USA
Titolo Testata:
LIFE SCIENCES
fascicolo: 25, volume: 67, anno: 2000,
pagine: 3103 - 3112
SICI:
0024-3205(20001110)67:25<3103:RARWCI>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
ARYL-HYDROCARBON RECEPTOR; GRAPEFRUIT JUICE; IN-VITRO; ERYTHROMYCIN; TRANSCRIPTION; ACTIVATION; INHIBITOR; GRAPES; CYP3A4; HUMANS;
Keywords:
resveratrol; red wine; cytochrome P450 3A4; mechanism-based inhibition;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Chan, WK Univ Pacific, Dept Pharmaceut & Med Chem, Sch Pharm & Hlth Sci, Stockton, CA 95211 USA Univ Pacific Stockton CA USA 95211 h Sci, Stockton, CA 95211 USA
Citazione:
W.K. Chan e A.B. Delucchi, "Resveratrol, a red wine constituent, is a mechanism-based inactivator of cytochrome P450 3A4", LIFE SCI, 67(25), 2000, pp. 3103-3112

Abstract

Resveratrol, a phytoalexin found in red wine, has been shown to possess antioxidant and antimutagenic properties. Incubation of resveratrol with Sf9 insect microsomes containing baculovirus-derived human cytochrome P450 3A4 (CYP3A4) and NADPH-cytochrome P450 reductase showed that resveratrol inactivated CYP3A4 in a time- and NADPH-dependent manner. Resveratrol, erythromycin and troleandomycin inactivated CYP3A4 at a similar rate (as reflected byk(inact)) whereas the binding affinity to CYP3A4 (as reflected by K-I) wasin the order of: troleandomycin > erythromycin > resveratrol, (K-I and k(inact) for CYP3A4 inactivation by resveratrol, erythromycin and troleandomycin are 20 muM and 0.20 min(-1), 5.3 muM and 0.12 min(-1) and 0.18 muM and 0.15 min(-1), respectively. ) Fractionation studies of red wine showed that fractions that did not contain resveratrol inactivated CYP3A4 significantly. In addition, the resveratrol content in red wine used in the study was toolow to account for the degree of CYP3A4 inactivation observed after red wine treatment. Inactivation studies using a variety of red wine types showedthat the CYP3A4 inactivation did not correlate to their resveratrol content. In summary, data here showed that resveratrol is an effective mechanism-based inactivator of CYP3A4; however, it is not one of the main red wine constituents that are responsible for CYP3A4 inactivation by red wine. Nevertheless, inactivation of CYP3A4 by resveratrol may cause clinically relevantdrug interactions with CYP3A4 substrates. (C) 2000 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 21:40:54