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观察辛热药附子、仙茅水提物对正常人肝脏细胞L02细胞药物代谢酶细胞色素P4503A(Cytochrome P4503A,CYP3A)的影响,进而探讨体内cAMP-PKA信号通路与药性表达的相关性。方法:200μg生药/mL的附子、仙茅水提物作用于L02细胞,以cAMP-PKA信号通路激动剂8-Br-cAMP作为阳性对照。应用免疫组化法检测各组细胞蛋白激酶A(protein kinase A,PKA)表达,应用Western blot法检测孕烷X受体(pregnane x receptor,PXR)表达,应用红霉素-N脱甲基法检测CYP3A活性。结果:与空白对照组比较,附子、仙茅水提物组细胞的PKA、PXR表达增强,CYP3A活性增加。结论:附子、仙茅可增强CYP3A活性,调控cAMP-PKA信号通路是其药性表达机制之一。
To observe the effect of Acridus aconitum and Curculigo laevigata on cytochrome P4503A and CYP3A in normal human L02 cells, and to explore the correlation between cAMP-PKA signaling pathway and drug-induced expression in vivo. Methods: 200μg crude drug / mL aconite, Curcuma longa aqueous extract on L02 cells with cAMP-PKA signal pathway agonist 8-Br-cAMP as a positive control. Immunohistochemistry was used to detect the expression of protein kinase A (PKA) in each group. Western blot was used to detect the expression of pregnane x receptor (PXR). Erythromycin-N demethylation CYP3A activity was measured. Results: Compared with the blank control group, the expression of PKA and PXR increased and the activity of CYP3A increased. Conclusion: Aconite, Curculigo can enhance the activity of CYP3A and regulate the cAMP-PKA signaling pathway is one of the mechanisms of its expression.