Caco-2单层细胞模型上士的宁的体外吸收机制及其与甘草苷的转运相互作用
In vitro absorption mechanism of strychnine and the transport interaction with liquiritin in Caco-2 cell monolayer model
-
摘要:
利用人结肠癌细胞系Caco-2细胞单层模型, 分别考察了转运时间、药物作用浓度、P-糖蛋白抑制剂维拉帕米、溶液pH值对士的宁表观渗透系数 (Papp) 和累积转运浓度 (TRcum) 的影响, 探讨了士的宁的体外肠吸收机制及甘草苷对士的宁吸收与转运的影响。结果表明, 士的宁在Caco-2细胞中的转运主要为被动转运, 吸收较好。甘草苷能显著促进士的宁的吸收, 且当士的宁与甘草苷的配伍比例为1∶1时, 对士的宁吸收的促进作用最强。同时实验还发现, 士的宁可能是P-糖蛋白的作用底物, 环境pH值对士的宁的外排作用有重要影响。
Abstract:To study the effect of liquiritin (Liq) on the transport of strychnine (Str) in Caco-2 cell monolayer model, the transport parameters of Str, such as apparent permeability coefficient (Papp (B→A) and Papp (A→B) ) and cumulative transport amount (TRcum), were determined and comparatively analyzed when Str was used solely and co-used with Liq. The effect of drug concentrations, conveying times, P-glycoprotein (P-gp) inhibitor verapamil and conveying liquor pH values on the transport of Str were also investigated. The results indicated that the absorption of Str in Caco-2 cell monolayer model was well and the passive transference was the main intestinal absorption mechanism of Str in the Caco-2 monolayer model, along with the excretion action mediated by P-gp. Liq enhanced the absorption of Str. Meanwhile, conveying liquor pH value had significant influence on the excretion transport of Str.
下载: