胡桃醌经大鼠肠道及Caco-2细胞模型转运特征的研究

Absorption mechanism of juglone across rat intestine and Caco-2 monolayer model

目的研究胡桃醌经大鼠肠道及Caco-2细胞的转运特征。方法应用Caco-2细胞模型和翻转肠囊法考察转运时间、药物浓度对胡桃醌吸收的影响,采用高效液相色谱法测定胡桃醌浓度,计算其表观渗透系数(Papp)。结果随着浓度增加和时间延长,胡桃醌累积通透量逐渐增加;胡桃醌浓度为100μmol L-1时,在Caco-2细胞模型表观渗透系数为1.4×10-7cm s-1;在翻转肠囊模型表观渗透系数2.0×10-7cm s-1。结论胡桃醌的转运符合被动扩散的性质,经肠道吸收率较低。

Objective To investigate the transport characteristics of juglone across rat intestine and Caco-2 monolayer model.Methods Caco-2 cells and everted-gut technique were used to explore the effect of time and drug concentration on the absorption of juglone.The drug concentration was measured by HPLC and the apparent permeability coefficient（Papp） was calculated.Results The collective transport of juglone was positively correlated with the time and concentration.At the concentration of 100 μmol L-1,the Papp was 1.4×10-7cm s-1in the Caco-2 monolayer model and 2×10-7cm s-1 in the rat intestine model.Conclusion The main mechanism of juglone absorption is passive transference,and the absorption rate is very low.