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目的:明确仙茅水提液及其有效成分苔黑酚葡萄糖苷对正常、虚寒状态L02细胞中PXR-CYP3A的影响,为探讨仙茅在不同状态下药效表达差异的机制奠定基础。方法:分别用正常、虚寒大鼠血清培养L02细胞,诱导正常、虚寒2种状态细胞。仙茅水提液及其有效成分苔黑酚葡萄糖苷作用于不同状态细胞后,检测不同状态L02细胞PXR蛋白表达和CYP3A活性。结果:MTT法结果显示,仙茅水提液和苔黑酚葡萄糖苷能使L02细胞活力明显增强;仙茅水提液能使正常组L02细胞PXR蛋白表达水平显著降低,苔黑酚葡萄糖苷能使正常组L02细胞CYP3A活性和PXR蛋白表达水平均显著降低;而仙茅水提液能使虚寒组L02细胞CYP3A活性和PXR蛋白表达升高,苔黑酚葡萄糖苷能使虚寒组L02细胞CYP3A活性水平显著降低,使虚寒组细胞PXR蛋白表达水平升高。结论:仙茅作用于虚寒状态L02细胞,能激活PXR诱导CYP3A活性,但对正常L02细胞的PXR及其介导的CYP3A活性没影响或作用相反。
OBJECTIVE: To clarify the effects of Cortex miltiorrhizae water extract and its active ingredient anisole glucoside on PXR-CYP3A in normal and Deficiency L02 cells, and to lay a foundation for exploring the mechanism of action difference of Curculigo orchids in different states. Methods: Normal and Deficiency rat serum were cultured L02 cells, induced normal and Deficiency two state cells. Curculigo lactea extract and its active ingredient orghenol glucoside role in different states of cells, the detection of different states L02 cells PXR protein expression and CYP3A activity. Results: The results of MTT assay showed that the activity of PXR protein in L02 cells in normal group was significantly lower than that in normal group, while the activity of PXR protein in L02 cells of normal group was significantly lower than that of norcinol glucoside The activity of CYP3A and the expression of PXR protein in L02 cells of normal group were significantly decreased; while the extract of Cortex miltiorrhizae could increase the activity of CYP3A and the expression of PXR protein in L02 cells of asthenia cold group, while cethenol glucoside induced L02 cells The level of CYP3A activity was significantly decreased, so that the expression of PXR protein in Deficiency group increased. CONCLUSION: The effect of Curculigo on the hypoxic-cold state L02 cells can activate the PXR-induced CYP3A activity, but has no effect on the normal L02 cells and PXR-mediated CYP3A activity.