Inhibitory effects of astaxanthin, ß-cryptoxanthin, canthaxanthin, lutein, and zeaxanthin on cytochrome P450 enzyme activities.
Food Chem Toxicol
; 59: 78-85, 2013 Sep.
Article
em En
| MEDLINE
| ID: mdl-23669408
ABSTRACT
Astaxanthin, ß-cryptoxanthin, canthaxanthin, lutein and zeaxanthin, the major xanthophylls, are widely used in food, medicine, and health care products. To date, no studies regarding the inhibitory effects of these xanthophylls on the nine CYPs isozymes have been reported. This study investigated the reversible and time-dependent inhibitory potentials of five xanthophylls on CYPs activities in vitro. The reversible inhibition results showed that the five compounds had only a weak inhibitory effect on the nine CYPs. Lutein did not inhibit the nine CYPs activities. Astaxanthin weakly inhibited CYP2C19, with an IC50 of 16.2 µM; and ß-cryptoxanthin weakly inhibited CYP2C8, with an IC50 of 13.8 µM. In addition, canthaxanthin weakly inhibited CYP2C19 and CYP3A4/5, with IC50 values of 10.9 and 13.9 µM, respectively. Zeaxanthin weakly inhibited CYP3A4/5, with an IC50 of 15.5 µM. However, these IC50 values were markedly greater than the Cmax values reported in humans. No significant IC50 shift was observed in the time-dependent inhibition screening. Based on these observations, it is unlikely that these five xanthophylls from the diet or nutritional supplements alter the pharmacokinetics of drugs metabolized by CYPs. These findings provide some useful information for the safe use of these five xanthophylls in clinical practice.
Palavras-chave
AS; Astaxanthin; C(max); CA; CYP; Canthaxanthin; IC(50); In vitro CYPs inhibition; LCMS/MS; LU; Lutein; NADP(+); ZE; Zeaxanthin; astaxanthin; canthaxanthin; cytochrome P450; liquid chromatographytandem mass spectrometry; lutein; maximum plasma concentration; the 50% inhibitory concentration; zeaxanthin; ß-Cryptoxanthin; ß-cryptoxanthin; ß-nicotinamide adenine dinucleotide phosphate; ßC
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Microssomos Hepáticos
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Carotenoides
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Xenobióticos
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Inibidores Enzimáticos
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Inibidores das Enzimas do Citocromo P-450
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article