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Titolo:
Role of furanocoumarin derivatives on grapefruit juice-mediated inhibitionof human CYP3A activity
Autore:
Guo, LQ; Fukuda, K; Ohta, T; Yamazoe, Y;
Indirizzi:
Tohoku Univ, Grad Sch Pharmaceut Sci, Div Drug Metab & Mol Toxicol, Aoba Ku, Sendai, Miyagi 9808578, Japan Tohoku Univ Sendai Miyagi Japan 9808578 Ku, Sendai, Miyagi 9808578, Japan Tanabe Seiyaku Co Ltd, Discovery Res Lab, Dept Drug Metab & Pharmacokinet,Toda, Saitama, Japan Tanabe Seiyaku Co Ltd Toda Saitama Japan rmacokinet,Toda, Saitama, Japan Kanazawa Univ, Fac Pharmaceut Sci, Div Pharmacognosy & Chem Nat Prod, Kanazawa, Ishikawa 920, Japan Kanazawa Univ Kanazawa Ishikawa Japan 920 , Kanazawa, Ishikawa 920, Japan
Titolo Testata:
DRUG METABOLISM AND DISPOSITION
fascicolo: 7, volume: 28, anno: 2000,
pagine: 766 - 771
SICI:
0090-9556(200007)28:7<766:ROFDOG>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
DRUG-INTERACTIONS; CYTOCHROME-P450 3A4; ENTEROCYTE CYP3A4; ORAL AVAILABILITY; 6',7'-DIHYDROXYBERGAMOTTIN; FELODIPINE; COMPONENTS; INACTIVATION; MECHANISM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Yamazoe, Y Tohoku Univ, Grad Sch Pharmaceut Sci, Div Drug Metab & Mol Toxicol, Aoba Ku, Sendai, Miyagi 9808578, Japan Tohoku Univ Sendai Miyagi Japan 9808578 Miyagi 9808578, Japan
Citazione:
L.Q. Guo et al., "Role of furanocoumarin derivatives on grapefruit juice-mediated inhibitionof human CYP3A activity", DRUG META D, 28(7), 2000, pp. 766-771

Abstract

With juices of grapefruit and related fruits, possible relationships between contents of six different furanocoumarins and extents of inhibition of microsomal CYP3A activity have been studied in vitro. Microsomal CYP3A-mediated testosterone 6 beta-hydroxylation was inhibited by the addition of a fruit juice (2.5%, v/v) from eight different grapefruit sources, two sweeties, three pomelos, and one sour orange, whereas no clear inhibition was observed with two sweet orange juices. The inhibitory component in grapefruit juice resides mainly in the precipitate rather than in the supernatant after centrifugation. Higher amounts of (R)-6',7'-dihydroxybergamottin (DHB) weredistributed in the supernatant, whereas GF-I-1, GF-I-2, GF-I-4, and the newly isolated GF-I-5, and GF-I-6 were detected predominantly in the precipitate. Mixing of five representative furanocoumarins at their detectable levels in grapefruit juice reproduced roughly the inhibitory potencies of grapefruit juice, but omission of any of the components resulted in decreased potencies. These results suggested that all the major furanocoumarins contributed to the CYP3A inhibitory properties of grapefruit juice. Furthermore, all six furanocoumarins showed stronger CYP3A inhibitory potencies after preincubation in the presence of NADPH, suggesting that both competitive and mechanism-based inhibition occur in a grapefruit juices-drug interaction.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 05:31:39