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目的:通过经典的体外细胞模型探讨五味子乙素对P-糖蛋白的影响。方法:以Caco-2细胞模型为载体,选取罗丹明123和环孢素-为P-gp底物,采用高效液相色谱法(HPLC)和液体闪烁计数法检测不同条件下五味子乙素、罗丹明123及环孢素-跨膜转运的变化,计算表观渗透系数、表观渗透率等参数。结果:五味子乙素浓度在20,40,80μg·ml~(-1)时双向跨膜转运的速率相似,无选择性差异。五味子乙素浓度为20~160μg·ml~(-1)时可显著抑制罗丹明123和环孢素A在Caco-2细胞模型中BL→AP定向转运(P<0.05),且呈剂量相关性。结论:五味子乙素为P-gp抑制药,但不是P-gp底物。
OBJECTIVE: To investigate the effect of Schisandrin B on P-glycoprotein through a classical in vitro cell model. Methods: The Caco-2 cell model was used as the carrier. Rhodamine 123 and cyclosporin were selected as substrates of P-gp. High performance liquid chromatography (HPLC) and liquid scintigraphy Ming 123 and cyclosporine - transmembrane transport changes, calculate the apparent permeability coefficient, apparent permeability and other parameters. Results: The bi - directional transmembrane transport rates of Schizandrin B2 at 20,40,80μg · ml ~ (-1) were similar with no selective difference. Schisandrin B at a concentration of 20 ~ 160μg · ml ~ (-1) significantly inhibited the BL-AP directional transport (P <0.05) of rhodamine 123 and cyclosporin A in Caco-2 cell model with dose-dependent . Conclusion: Schisandrin B is P-gp inhibitor, but not P-gp substrate.