并行传输
多药耐药蛋白2
药理学
碳酸钙-2
Abcg2型
化学
维拉帕米
流出
吸收(声学)
生物利用度
体外
生物化学
生物
运输机
ATP结合盒运输机
材料科学
基因
磁导率
复合材料
有机化学
钙
膜
作者
Hui Yang,Bingtao Zhai,Yu Fan,Jing Wang,Jing Sun,Yajun Shi,Deliang Guo
标识
DOI:10.1016/j.biopha.2018.07.117
摘要
Araloside A is a triterpenoid saponin,which exhibits a broad spectrum of pharmacological activities, such as stimulating fibrinolysis, preventing coagulant, inhibiting renin, and decreasing blood pressure. Our previous report found that the compound exhibits a poor absolute bioavailability. However the underlying mechanisms of its absorption have not been investigated in the small intestine or in a Caco-2 cell model. In this study, the absorption mechanisms of araloside A were investigated in a Caco-2 cell monolayer and in a single-pass intestinal perfusion in situ model with Sprague-Dawley rats. The effects of basic parameters, such as compound concentration, time, temperature, paracellular pathway, different intestinal segments were analyzed, and the susceptibility of araloside A absorption process to treatment with various inhibitors, such as the P-gp inhibitor verapamil, the multidrug resistance protein2 inhibitors (MRP2) MK571 and indomethacin, the breast cancer resistance protein (BCRP) inhibitors Ko143 and reserpine, and endocytosis inhibitor chlorpromazine were assessed. It can be found that the mechanisms of intestinal absorption of araloside A may involve multiple transport pathways, such as passive diffusion, the paracellular pathway, as well as the participation of efflux transporters.
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