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Titolo:
DIFFERENTIAL INHIBITION OF AFLATOXIN B-1 OXIDATION BY GESTODENE ACTION ON HUMAN LIVER-MICROSOMES
Autore:
KIM BR; OH HS; KIM DH;
Indirizzi:
KOREA ADV INST SCI & TECHNOL,DOPING CONTROL CTR SEOUL SOUTH KOREA KOREA ADV INST SCI & TECHNOL,DOPING CONTROL CTR SEOUL SOUTH KOREA WON KWANG JR COLL,DEPT CLIN PATHOL IKSAN SOUTH KOREA WON KWANG UNIV,SCH MED,DEPT BIOCHEM IKSAN SOUTH KOREA
Titolo Testata:
Biochemistry and molecular biology international
fascicolo: 4, volume: 43, anno: 1997,
pagine: 839 - 846
SICI:
1039-9712(1997)43:4<839:DIOABO>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN CYTOCHROME-P450 3A4; ALFENTANIL METABOLISM; RAT-LIVER; CYTOCHROME-P-450-IIIA4; 7,8-BENZOFLAVONE; IDENTIFICATION; ACTIVATION; BINDING;
Keywords:
AFLATOXIN B-1; GESTODENE; P450 3A4; INHIBITION;
Tipo documento:
Article
Natura:
Periodico
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
B.R. Kim et al., "DIFFERENTIAL INHIBITION OF AFLATOXIN B-1 OXIDATION BY GESTODENE ACTION ON HUMAN LIVER-MICROSOMES", Biochemistry and molecular biology international, 43(4), 1997, pp. 839-846

Abstract

Human cytochrome P450 (P450) 3A is known to be involved in the formation of both aflatoxin B-1-exo-8,9-epoxide (exo-epoxidation) and aflatoxin Q(1)(3 alpha-hydroxylation). Gestodene, a known inactivator of P450 3A4, inhibited the formation of AFB(1) metabolites in a variety of ways depending on the incubation condition. Preincubation of gestodene with human liver microsomes prior to the addition of AFB(1) inhibited both exo-epoxidation and 3 alpha-hydroxylation whereas simultaneous incubation of gestodene with AFB(1) only inhibited 3 alpha-hydroxylation. These results suggest that two independent substrate binding sites exist in P450 3A4, and AFB(1) binds to both of the binding sites. Gestodene selectively binds to one of the binding sites leading to the formation of AFQ(1), whereas it does not affect the formation of exo-epoxide via the other binding site.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/01/20 alle ore 21:29:59