黄山毛峰茶多酚提取物对肝药酶Cyp3a11的调控作用

Regulatory Effect of Tea Polyphenol Extracts from Huangshan Maofeng Tea on the Drug-Metabolizing Enzyme Cyp3a11

以黄山毛峰为原料,采用实时荧光定量反转录聚合酶链式反应法和蛋白免疫印迹法研究其茶多酚提取物对肝药酶Cyp3a11及孕烷X受体(pregnane X receptor,PXR)的mRNA和蛋白表达影响,在此基础上采用瞬时共转染报告基因技术进一步验证是否通过PXR实现对Cyp3a11表达调控。结果表明:黄山毛峰茶多酚提取物各剂量组(75、150、300 mg/(kg·d))均能显著调控小鼠肝Cyp3a11、PXR m RNA及其蛋白表达;报告基因实验结果显示,100、200、300μg/m L黄山毛峰茶多酚提取物经PXR通路使细胞色素P4503A4基因荧光素酶活力分别增加(3.86±0.05)、(4.82±0.72)、(5.38±0.11)倍。研究表明黄山毛峰茶多酚提取物可激活PXR通路调控肝药酶Cyp3a11的表达。

In this paper,we explored the effect of tea polyphenols from Huangshan Maofeng tea on the mRNA and protein expression levels of the drug-metabolizing enzyme Cyp3a11 and pregnane X receptor(PXR)by real-time reverse transcription polymerase chain reaction(real-time RT-PCR)and Western blot.We further used the transient co-transfection reporter gene assay to verify the role of PXR in regulating Cyp3a11 expression.The results showed that the tea polyphenols at doses of 75,150 and 300 mg/(kg·d)could significantly induce the mRNA and protein expression of PXR and Cyp3a11.Reporter gene screening showed that the tea polyphenols at doses of 100,200 and 300μg/mL could significantly enhance cytochrome P4503A4(CYP3A4)luciferase activity by(3.86±0.05),(4.82±0.72)and(5.38±0.11)folds through the PXR pathway as compared to the solvent control group.Therefore,tea polyphenols from Huangshan Maofeng tea can significantly upregulate CYP3A4 expression via activating the PXR-CYP3A4 pathway.