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天麻素是传统中药天麻的有效活性成分。本研究以Caco-2细胞、Bcap37和Bcap37/MDR1为模型,体外评价天麻素在Caco-2细胞模型上的转运过程以及天麻素与P-糖蛋白之间的相互作用。在50～500μmol.L?1浓度内,天麻素的表观渗透系数(Papp)比值<2.0,与转运方向无关,且不受P-糖蛋白的经典抑制剂(维拉帕米和GF120918)的影响。天麻素在Bcap37、Bcap37/MDR1细胞中的积聚呈浓度依赖性,且不干扰罗丹明123在Bcap37/MDR1细胞中的积聚。结果表明,天麻素在Caco-2细胞模型上的转运方式以被动转运为主,天麻素不是P-糖蛋白的底物和抑制剂。
Gastrodin is an effective active ingredient of traditional Chinese medicine Tianma. In this study, Caco-2 cells, Bcap37 and Bcap37 / MDR1 as a model, in vitro evaluation of gastrodin transport in Caco-2 cell model and gastrodin and P-glycoprotein interaction. In the concentration range of 50 ~ 500μmol.L ~ 1, gastrodin has an apparent permeability coefficient (Papp) ratio <2.0, which is independent of the transport direction and not affected by the classical inhibitor of P-glycoprotein (verapamil and GF120918) influences. Gastrodin accumulation in Bcap37, Bcap37 / MDR1 cells was concentration-dependent and did not interfere with the accumulation of rhodamine 123 in Bcap37 / MDR1 cells. The results showed that the transport mode of gastrodin on Caco-2 cells was mainly passive, and gastrodin was not the substrate and inhibitor of P-glycoprotein.