以Caco-2细胞模型研究远志皂苷水解物的肠吸收特性

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(PMCA)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.

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

Objective To determine the transportation of active components of Polygala saponin hydrolysate(PSH),3,4,5-trimethoxycinnamylic acid(TMCA),p-methoxycinnamylic acid(PMCA) and tenuifolin(TF),in the intestinal 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 1×10-6cm·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.