Modulation of green tea extract on activities and mRNA expressions of cytochrome P450 enzymes in rats
1.Department of Pharmacy, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou, 325015; 2.Testing and Analysis Center, Wenzhou Medical University, Wenzhou, 325035
ZHOU Ziye1,JIN Hui1,WANG Chenxiang1, et al. Modulation of green tea extract on activities and mRNA expressions of cytochrome P450 enzymes in rats[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2015, 45(7): 502-.
Abstract：Objective: To investigate the potential effects of green tea extract on activities and mRNA expressions of cytochrome P450 (CYP450) enzymes in rats. Methods: After treatment with tea extract or water for 14 days, treatment group rats and control group rats were given the mixture of 4 probe substrates including phenacetin, bupropion, tolbutamide and midazolam. The plasma concentrations of probes at a series of time-points were determined with liquid chromatography tandom mass spectrometry. The activities of CYP450s were evaluated according to the pharmacokinetic parameters of corresponding substrates. Real-time PCR was applied to assess the mRNA expression levels of CYP450s. Results: The pharmacokinetic parameters of bupropion and tolbutamide from treatment group showed significant differences compared with control group, which indicated that green tea extract induced CYP2B1 activity and inhibited CYP2C11 activity. And no significant difference was found in pharmacokinetic parameters of phenacetin or midazolam from treatment group and control group. In addition, treatment with green tea extract significantly up-regulated the mRNA expression of CYP2B1 and down-regulated the mRNA expression of CYP2C11, whereas it had no impact on CYP1A2 and CYP3A1. Conclusion: Continuous ingestion of green tea can modulate the activities and mRNA expressions of CYP2B1 and CYP2C11, which may lead to an undesired interaction.
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