Isochlorogenic acid A affects P450 and UGT enzymes in vitro and in vivo / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 865-870, 2016.
Article
Dans Anglais
| WPRIM
| ID: wpr-812566
ABSTRACT
Isochlorogenic acid A (ICQA), which has anti-inflammatory, hepatoprotective, and antiviral properties, is commonly presented in fruits, vegetables, coffee, plant-based food products, and herbal medicines. These herbal medicines are usually used in combination with other medicines in the clinic. However, little is known about the regulatory effects of ICQA on drug-metabolizing enzymes and the herb-drug interactions. In the present study, we evaluated the inhibitory potentials of ICQA on CYP1A2, CYP2C9, CYP2C19, CYP3A4, CYP2D6, and CYP2E1 in vitro based on a cocktail approach. The P450 and UGT activities in mice treated with ICQA for a prolonged period were also determined. Our results demonstrated that ICQA exhibited a weak inhibitory effect on CYP2C9 in human liver microsomes with IC being 57.25 μmol·L and Ki being 26.77 μmol·L. In addition, ICQA inhibited UGT1A6 activity by 25%, in the mice treated with ICQA (i.p.) at 30 mg·kg for 14 d, compared with the control group. Moreover, ICQA showed no mechanism-based inhibition on CYP2C9 or UGT1A6. In conclusion, our results further confirm a safe use of ICQA in clinical practice.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Microsomes du foie
/
Cinétique
/
Chimie
/
Acide chlorogénique
/
Glucuronosyltransferase
/
Cytochrome P-450 enzyme system
/
Inhibiteurs des enzymes du cytochrome P-450
/
Métabolisme
/
Souris de lignée C57BL
Limites du sujet:
Animaux
/
Humains
langue:
Anglais
Texte intégral:
Chinese Journal of Natural Medicines (English Ed.)
Année:
2016
Type:
Article
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