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Titolo:
Inhibition of human CYP3A4 activity by grapefruit flavonoids, furanocoumarins and related compounds
Autore:
Ho, PC; Saville, DJ; Wanwimolruk, S;
Indirizzi:
Western Univ Hlth Sci, Coll Pharm, Pomona, CA 91766 USA Western Univ Hlth Sci Pomona CA USA 91766 oll Pharm, Pomona, CA 91766 USA Univ Otago, Sch Pharm, Dunedin, New Zealand Univ Otago Dunedin New Zealand v Otago, Sch Pharm, Dunedin, New Zealand
Titolo Testata:
JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES
fascicolo: 3, volume: 4, anno: 2001,
pagine: 217 - 227
SICI:
1482-1826(200109/12)4:3<217:IOHCAB>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN-LIVER-MICROSOMES; MECHANISM-BASED INACTIVATION; CYTOCHROME-P450 3A4; 11-BETA-HYDROXYSTEROID DEHYDROGENASE; MONOOXYGENASE ACTIVITIES; FELODIPINE INTERACTION; ORAL AVAILABILITY; DRUG METHOXSALEN; JUICE; METABOLISM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
48
Recensione:
Indirizzi per estratti:
Indirizzo: Wanwimolruk, S Western Univ Hlth Sci, Coll Pharm, 309 E 2nd St, Pomona, CA91766 USA Western Univ Hlth Sci 309 E 2nd St Pomona CA USA 91766 USA
Citazione:
P.C. Ho et al., "Inhibition of human CYP3A4 activity by grapefruit flavonoids, furanocoumarins and related compounds", J PHARM P S, 4(3), 2001, pp. 217-227

Abstract

PURPOSE. To evaluate the inhibition of CYP3A4 activity in human liver microsomes by flavonoids, furanocoumarins and related compounds and investigatepossibly more important and potential inhibitors of CYP3A4 in grapefruit juice. METHODS. The effects of various flavonoids and furanocoumarin derivatives on CYP3A4 activity in two human liver microsomal samples was determined using quinine as a substrate. All flavonoids and furanocoumarin derivatives were dissolved in DMSO. In all cases, inhibition activities were compared with activities in control incubations containing 0.2% (v/v) DMSO. RESULTS. The results showed that the inhibition of quinine 3-hydroxylation (CYP3A4 activity) by bergapten (67%), and quercetin (55%) was greater than naringenin (39%) and naringin (6%), at the same inhibitor concentration of 100 . The results also demonstrated that the furan ring in the furanocoumarins enhanced the inhibitory effect on CYP3A4 activity. Flavonoids with more phenolic hydroxyl (-OH) groups produced stronger inhibition than those with lesshydroxyl groups. Of all the chemicals studied, bergapten (5-methoxypsoralen) with the lowest IC50 value (19-36 muM) was the most potent CYP3A4 inhibitor. CONCLUSIONS. These results suggest that more than one component present in grapefruit juice may contribute to the inhibitory effect on CYP3A4. Bergapten appears to be a potent inhibitor of CYP3A4, and may therefore be primarily responsible for the effect of grapefruit juice on CYP3A4 activity.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 04:42:16