title: The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats.
abstract: The purpose of this study was to determine the effect of apigenin on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats. Healthy male SD rats were randomly divided into four groups: A group (the control group), B group (the long-term administration of 165 mg/kg apigenin for 15 days), C group (a single dose of 165 mg/kg apigenin), and D group (a single dose of 252 mg/kg apigenin). The serum concentrations of imatinib and N-desmethyl imatinib were measured by HPLC, and pharmacokinetic parameters were calculated using DAS 3.0 software. The parameters of AUC(0-t), AUC(0-∞), Tmax, V(z)/F, and CL(z)/F for imatinib in group B were different from those in group A (P < 0.05). Besides, MRT(0-t) and MRT(0-∞) in groups C and D differed distinctly from those in group A as well. The parameters of AUC(0-t) and Cmax for N-desmethyl imatinib in group C were significantly lower than those in group A (P < 0.05); however, compared with groups B and D, the magnitude of effect was modest. Those results indicated that apigenin in the short-term study inhibited the metabolism of imatinib and its metabolite N-desmethyl imatinib, while in the long-term study the metabolism could be accelerated.
authors.affiliation: The First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325000, China.
authors.forename: Xian-yun
authors.initials: XY
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Xu
authors.affiliation: Ningbo Municipal Hospital of Traditional Chinese Medicine, Ningbo 315010, China.
authors.forename: Wan-shu
authors.initials: WS
authors.lastname: Li
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Luo
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Pei-wu
authors.initials: PW
authors.lastname: Geng
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Li
authors.initials: L
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Meng-ming
authors.initials: MM
authors.lastname: Xia
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Meng-chun
authors.initials: MC
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Yu
authors.affiliation: School of Pharmacy, Wenzhou Medical University, Wenzhou 325035, China.
authors.forename: Guo-Xin
authors.initials: GX
authors.lastname: Hu
mesh_terms: D000818:Animals; D047310:Apigenin / Q000008:administration & dosage*; D001549:Benzamides / Q000037:antagonists & inhibitors / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D000068877:Imatinib Mesylate; D010879:Piperazines / Q000037:antagonists & inhibitors / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics*; D011743:Pyrimidines / Q000037:antagonists & inhibitors / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics*; D051381:Rats
chemical_list: D001549:Benzamides; D010879:Piperazines; D011743:Pyrimidines; D047310:Apigenin; D000068877:Imatinib Mesylate