Vol 9: Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats.Reportar como inadecuado



 Vol 9: Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats.


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This article is from PLoS ONE, volume 9.AbstractBaicalin has been used as mainly bioactive constituent of about 100 kinds of traditional Chinese medicines in Chinese pharmacopoeia. The effect of baicalin on cytochrome P450 should be paid more attention because baicalin was used widely. The aim of this study was to investigate whether baicalin could inhibit CYP1A2 in pooled human liver microsomes HLMs and in rats in vivo and the gene polymorphisms could affect inter-individual variation in IC50 in 28 human livers. Phenacetin was used as probe of CYP1A2. Kinetic parameter of CYP1A2 and IC50 of baicalin on CYP1A2 to each sample were measured and the common CYP1A2 polymorphisms −3860GA and −163CA were genotyped. The results showed that baicalin exhibited a mixed-type inhibition in pooled HLMs, with a Ki value of 25.4 µM. There was substantial variation in Km, Vmax, CLint of CYP1A2 and IC50 of baicalin on CYP1A2 3∼10-fold. The range was from 26.6 to 114.8 µM for Km, from 333 to 1330 pmol·min−1·mg−1protein for Vmax and from 3.8 to 45.3 µL·min−1·mg−1 protein for CLint in HLMs n = 28. The Mean range value of IC50 in 28 HLMs was 36.3 18.9 to 56.1 µM. The genotypes of −3860GA and −163CA had no significant effect on the inhibition of baicalin on CYP1A2. The animal experiment results showed that baicalin 450 mg-kg, i.v. significantly decreased the Cmax and CL of phenacetin, and increased C60 min, t1-2, Vd and AUC P



Autor: Gao, Na; Qi, Bing; Liu, Fang-jun; Fang, Yan; Zhou, Jun; Jia, Lin-jing; Qiao, Hai-ling

Fuente: https://archive.org/







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