矢车菊黄素在Caco-2细胞模型中的吸收机制研究

目的 研究矢车菊黄素（centaureidin）在Caco-2细胞单层模型中的吸收机制。方法 以HPLC分析矢车菊黄素浓度，用Caco-2 细胞单层模型评价吸收时间、药物浓度、介质pH值、抑制剂等对矢车菊黄素吸收的影响，研究矢车菊黄素的吸收机制，计算表观渗透系数（apparent permeability coefficient, Papp）。结果 药物的吸收与药物浓度和吸收时间正相关；弱酸性介质条件下有利于药物的吸收；2,4-二硝基酚（DNP）对药物吸收无影响，但异博定（verapamil）可增加药物的吸收；从肠腔侧到基底侧的转运小于基底侧到肠腔侧的转运。结论 矢车菊黄素在Caco-2细胞模型中的吸收主要是被动转运，受P-糖蛋白的外排作用。

Transepithelial Transport of Centaureidin Across Caco-2 Cell Monolayers

OBJECTIVE To investigate the transepithelial transport of centaureidin across Caco-2 cell monolayers. METHODS The permeated amounts of centaureidin across Caco-2 cell momnolayers were measured by HPLC to calculate the permeation rate and the apparent permeability coefficient (P_app), based on the effect of absorption time, drug concentration, pH in apical side, and inhibitors, the Papp was determined. RESULTS Transport of centaureidin was concentration-dependent and time-dependent and nonsatuable. The acidic pH in apical side conduced to transepithelial transport of centaureidin. Though 2,4-dinitrophenol had no effect on transport of centaureidin, verapamil improved it. And the apical-to-basolateral P_app was less than the basolateral-to-apical P_app. CONCLUSION Transport of centaureidin across Caco-2 cell monolayers is via passive diffusion with efflux by P-glycoprotein.