以Caco-2细胞模型研究远志皂苷水解物的肠吸收特性  

Transportation of Polygala saponin hydrolysates in the small intestine in Caco-2 cell monolayer model

作　　者：王倩[1] 潘瑞乐[1] 肖冰心[1] 刘新民[1] 孔令提[1] 叶林虎[1] 常琪[1] 

机构地区：[1]中国医学科学院北京协和医学院药用植物研究所中草药物质基础与资源利用教育部重点实验室,北京100193

出　　处：《中南药学》2012年第6期405-408,共4页Central South Pharmacy

基　　金：科技部对欧盟科技合作专项(No.0901和1108)

摘　　要：目的通过研究远志皂苷水解物主要活性成分3,4,5-三甲氧基肉桂酸(TMCA)、对甲氧基肉桂酸(PM-CA)和细叶远志皂苷(TF)的肠转运特性,预测其口服生物利用度。方法利用Caco-2细胞模型,以及所建立的LC-MS/MS分析方法,研究上述3个成分在不同浓度下从顶侧(AP)到基底侧(BL)以及从BL到AP2个方向的转运特性。结果 TMCA和PMCA 2个酚酸化合物具有较好的膜通透性,在不同浓度下从AP到BL的表观渗透系数(Papp)均>10×10-6cm.s-1,而三萜皂苷TF的通透性较差,Papp值均<1×10-6cm.s-1。3个化合物的转运量均随浓度的增加而增加,但Papp值保持基本一致,且各自2个方向的Papp值无明显差异。结论 TMCA和PMCA具有良好的肠通透性,属吸收较好的化合物,而TF则通透性较差,口服吸收可能很有限;3个化合物均以被动扩散形式转运,且无外排转运机制。Objective To determine the transportation of active components of Polygala saponin hydrolysate （PSH）, 3, 4, 5-trimethoxyeinnamylic acid （TMCA）, p-methoxycinnamylic acid （PMCA） and tenuifolin （TF）, in the intesti- nal epithelium. Methods The Caco-2 cell monolayer model and the LC-MS/MS method were used to determine the permeabilities of the 3 components transported either from apical side to basolateral side or from basolateral side to apical side. Results The apparent permeability coefficient （Papp） values of TMCA and PMCA were higher than 10×10^-6 cm·S^-1 in the bidirectional transport at different concentrations. The Papp value of TF was lower than 1×10^-6 cm·S^-1. The transported amounts of the 3 components all increased with concentrations, with no changes in the Papp values. The Papp value of each component was not significantly different in the 2 directional transports. Conclusion The 3 active components of PSH can be transported across the intestinal epithelium by passive diffusion. TMCA and PMCA are well absorbed components and might be responsible for PSH activities.

关 键 词：远志皂苷水解物 3 4 5-三甲氧基肉桂酸 对甲氧基肉桂酸 细叶远志皂苷 CACO-2细胞模型 表观渗透系数 

分 类 号：R966[医药卫生—药理学]