甘草次酸在Caco-2细胞模型中的转运机制

Transport Mechanism of Glycyrrhetinic Acid in Human Intestinal Epithelial Caco-2 Cells

采用液相-质谱检测甘草次酸在HBSS磷酸盐缓冲液中的转运量,结果表明:甘草次酸的转运量受时间、浓度以及P-糖蛋白抑制剂维拉帕米和汉防己甲素的影响,表观渗透系数P(appBL-AP)为(17.1±4.2)×10-6～(54.3±6.3)×10-6cm.s-1、P(appAP-BL)为(15.6±3.4)×10-6cm.s-1;甘草次酸在小肠内的吸收主要是被动扩散,口服吸收较好并且存在P-糖蛋白的外排机制。

An experiment was conducted to determine the transferred amount of glycyrrhetinie acid in phosphate buffered solution by HPLC-MS/MS, in order to study the transport mechanism of glycyrrhetinic acid with Caco-2 cell monolayers. Results showed that the transferred amount of glycyrrhetinic acid was affected by culture time, drug concentration and P-glycoprorein inhibitor verapamil and Tetrandrine. The apparent permeability coefficients of glycyrrhetinic acid were （ 17.1 ±4.2 ） ×10^-6 （ 54.3±6.3 ） × 10^4 cm· s^-1 for PappBL-AP, and （15.6±3.4） ×10^-4 cm · s^-1 for PappAP-BL, and the bidirectional transport characteristics were different. It indicated that both active transport and passive diffusion contributed to the ab- sorption of glycyrrhetinic acid in Caco-2 cell monolayers, but the passive diffusion was the dominant process. The P-glycoprotein may play an important role in the effiux of glycyrrhetinic acid.