天麻素在Caco-2细胞及Bcap37、Bcap37/MDR1细胞模型中的转运和摄取(英文)

The transport of gastrodin in Caco-2 cells and uptake in Bcap37 and Bcap37/MDR1 cells

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 （GAS） is the major bioactive component of the extracts from the rhizome of Gastrodia elata Blume. The aim of this study is to investigate the transport of GAS in Caco-2 cells and the interaction of P-glycoprotein and GAS. The apparent permeability coefficients （Papp） of GAS were measured as a function of directions and concentrations. It was demonstrated that the efflux ratio was 2.0 over the range of 50？500 μmol.L？1 of GAS from bi-directional transport studies. The transport rate of GAS was dependent on the concentrations. Papp of GAS was not affected by transport directions, GAS concentration or the classical inhibitors of P-glycoprotein （verapamil and GF 120918）. The cellular accumulation of GAS in Bcap37/MDR1 cells transected with hMDR1 gene, was similar to that in Bcap37 cells. The accumulation in both cell lines was concentration dependent. GAS did not affect the accumulation of Rhodamine 123 in Bcap37/MDR1 cells over the range of 50？500 μmol.L？1. It indicated that the transport of GAS in Caco-2 cell monolayers mainly is by passive paracellular transport pathway. P-glycoprotein did not participate in the absorption of GAS in the intestine or the transport across the blood-brain barrier.