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Baicalin 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 IC 50  in 28 human livers. Phenacetin was used as probe of CYP1A2. Kinetic parameter of CYP1A2 and IC 50  of baicalin on CYP1A2 to each sample were measured and the common CYP1A2 polymorphisms (−3860G>A and −163C>A) were genotyped. The results showed that baicalin exhibited a mixed-type inhibition in pooled HLMs, with a K i  value of 25.4 µM. There was substantial variation in K m , V max , CL int  of CYP1A2 and IC 50  of baicalin on CYP1A2 (3∼10-fold). The range was from 26.6 to 114.8 µM for K m , from 333 to 1330 pmol·min −1 ·mg −1 protein for V max  and from 3.8 to 45.3 µL·min −1 ·mg −1  protein for CL int  in HLMs (n = 28). The Mean (range) value of IC 50  in 28 HLMs was 36.3 (18.9 to 56.1) µM. The genotypes of −3860G>A and −163C>A 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 C max  and CL of phenacetin, and increased C 60 min , t 1/2 , V d  and AUC ( P <0.05). There were significant correlations between percentage of control in C 60 min , t 1/2 , CL, AUC of phenacetin and C max  of baicalin in 11 rats ( P <0.05). Protein binding experiments in vitro showed that baicalin (0–2000 mg/L) increased the unbound phenacetin from 14.5% to 28.3%. In conclusion, baicalin can inhibit the activity of CYP1A2 in HLMs and exhibit large inter-individual variation that has no relationship with gene polymorphism. Baicalin can change the pharmacokinetics of phenacetin in rats.

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