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目的:研究左金丸类方中4种生物碱的转运特征并比较其差异。方法:采用LC-MS/MS法测定左金丸类方中4种生物碱在Caco-2细胞上的转运特征,研讨其转运差异的机制。结果:环孢素A和维拉帕米均可增加4种生物碱的Papp(AP-BL),降低其Papp(BL-AB);MK-571对其转运均无影响;左金丸中的4种生物碱的Papp(AP-BL)均较黄连组增大;甘露散、茱萸丸中的药根碱、黄连碱和小檗碱的Papp(BL-AP)均较黄连减小。结论:小檗碱、黄连碱、药根碱和巴马汀均为P-gp底物,而非MRP2底物;吴茱萸可能具有抑制P-gp活性的作用。
Objective: To study the transport characteristics of four alkaloids in Zuojinwan decoction and to compare their differences. Methods: The transport characteristics of four alkaloids in Zuojinwan decoction on Caco-2 cells were determined by LC-MS / MS, and the mechanism of their transport differences was studied. Results: Both cyclosporin A and verapamil could increase Papp (AP-BL) and decrease Papp (BL-AB) of four alkaloids; MK-571 had no effect on its transport; Papp (AP-BL) of the alkaloids increased compared with the Coptis group. Papp (BL-AP) of jatrorrhizine, rhizome alkali and berberine in the Ganluosan and Zhugu pill decreased compared with Coptis. Conclusion: Berberine, Coptis, jatrorrhizine and palmatine are P-gp substrate, but not MRP2 substrate; Evodia may inhibit the activity of P-gp.