Park, Ji-won published the artcileRole of kaempferol to increase bioavailability and pharmacokinetics of nifedipine in rats, Formula: C17H18N2O6, the main research area is Bioavailability; CYP3A4; Kaempferol; Nifedipine; P-gp; Pharmacokinetics.
Herein, the purpose of this study is to evaluate the effects of kaempferol on bioavailability and pharmacokinetics of nifedipine and its metabolite dehydronifedipine in rats. The exptl. design is based on with or without kaempferol in the oral and i.v. administration of nifedipine in rats. Moreover, the pharmacokinetic parameters including nifedipine and dehydronifedipine were evaluated in rats. The in vitro studies of kaempferol were investigated on P-glycoprotein (P-gp) and cytochrome P 450 (CYP) 3A4 activity. Kaempferol reduced a 50% inhibitory concentration (IC50) of 8.6 μmol·L-1 on CYP3A4 enzyme activity. Moreover, kaempferol clearly improved the cell internalization of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp. Depending on increased concentrations of kaempferol, the areas under the plasma concentration-time curve (AUC0-â? and the peak concentration (Cmax) of nifedipine were increased after oral and i.v. administration. Moreover, the absolute bioavailability (AB) and relative bioavailability (RB) of nifedipine in the presence of kaempferol was significantly higher than those of the control group after oral and i.v. administration. Improvement of bioavailability of nifedipine by kaempferol may be mainly because of the inhibition of the P-gp-mediated efflux transporter in the small intestine and CYP3A4-mediated metabolism in the small intestine or liver, or both.
Chinese Journal of Natural Medicines (Amsterdam, Netherlands) published new progress about Bioavailability; CYP3A4; Kaempferol; Nifedipine; P-gp; Pharmacokinetics. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Formula: C17H18N2O6.