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目的:探讨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Caco-2细胞PXR-CYP3A活性的影响。方法:肌注氢化可的松琥珀酸钠20mg·kg-1·d-1制造虚寒大鼠模型;分别用正常、虚寒大鼠血清培养Caco-2细胞,诱导正常、虚寒两种状态细胞。仙茅水提液(生药0.75mg/m L)及其有效成分苔黑酚葡萄糖苷(1×10-5mol/L)作用于不同状态细胞后,检测不同状态Caco-2细胞PXR和P-gp蛋白表达。结果:MTT法结果显示,仙茅水提液各浓度(1 000、750、500、250、100μg/m L)及其有效成分苔黑酚葡萄糖苷各浓度(10-3、10-4、10-5、10-6、10-7mol/L)对Caco-2细胞没有明显细胞毒性。虚寒组细胞的P-gp蛋白表达较正常组明显降低(P<0.05);PXR蛋白表达水平有降低趋势,但无统计学意义。仙茅水提液与苔黑酚葡萄糖苷均能使正常和虚寒组细胞P-gp蛋白水平显著升高(P<0.01),而对PXR蛋白水平没有显著影响。结论:仙茅能使正常及虚寒状态Caco-2细胞P-gp高表达,说明仙茅对Caco-2细胞P-gp有诱导作用。
OBJECTIVE: To investigate the effects of Curculigo celandica extract and its active ingredient anisole glucoside on PXR-CYP3A activity in Caco-2 cells in normal / Deficiency state. Methods: Cox-2 cells were induced by intraperitoneal injection of hydrocortisone sodium succinate 20 mg · kg-1 · d-1 in normal rats. cell. Curculigo laevigata aqueous extract (crude drug 0.75mg / m L) and its active ingredient anisole glucoside (1 × 10-5mol / L) in different states of cells, the detection of different states of Caco-2 cells PXR and P-gp Protein. Results: The results of MTT assay showed that each concentration (1 000, 750, 500, 250 and 100 μg / mL) of C. sinensis aqueous extract and each concentration of anisole glucoside (10-3, 10-4, -5,10-6,10-7 mol / L) had no obvious cytotoxicity on Caco-2 cells. The expression of P-gp protein in Deficiency group was significantly lower than that in normal group (P <0.05), and the expression of PXR protein was decreased, but there was no statistical significance. Cortex miltiorrhizae and orcinol glucoside both increased the P-gp protein level in normal and asthenic group (P <0.01), but had no significant effect on PXR protein level. CONCLUSION: Curculigine can promote the expression of P-gp in Caco-2 cells in normal and asthenic states, indicating that Curculigo oryzae can induce P-gp in Caco-2 cells.