大鼠单向灌流模型研究田蓟苷的在体肠吸收

Study on intestinal absorption of tilianin in rats of single-pass perfusion model

目的:研究田蓟苷的大鼠小肠吸收机制。方法:采用大鼠单向灌流模型,高效液相色谱法测定在体肠灌流田蓟苷的浓度变化,考察加入维拉帕米、利血平、根皮苷及利福平对田蓟苷在大鼠空肠段的Ka,Papp的影响。结果:与对照组相比,加入维拉帕米、利血平后,田蓟苷在大鼠空肠段的Ka,Papp有显著性增加(P<0.05);加入根皮苷后,田蓟苷在大鼠空肠段的Papp显著性降低(P<0.05);加入利福平,田蓟苷在大鼠空肠段的Ka,Papp没有显著性增加。结论:田蓟苷是P-糖蛋白(P-gp)、乳腺癌多药耐药蛋白(BCRP)及Na+依赖葡萄糖转运载体1(SGLT1)的底物,P-gp与BCRP外排作用是田蓟苷小肠吸收的主要外排机制,田蓟苷能够依赖SGLT1实现在小肠的吸收转运;田蓟苷不是胆盐转运蛋白的底物。

Objective： To study the intestinal absorption mechanism of tilianin in rats. Method： The single-pass perfusion model was established in rats. The concentrations of tilianin with in situ intestinal perfusion were determined by HPLC. The impact factors, such as verapamil, reserpine, phloridzin and rifampicin, on Kaand Papp of tilianin in rat jejunum were investigated. Result： Compared with the control group, Ka and Papp in rat jejunum were significantly higher after being added with verapamil and reserpine （ P 〈 0. 05 ）. P,pp of tilianin in rat jejunum was significantly lower after being added with phloridzin （ P 〈 0. 05 ）. Compared with the control group, both Ka and Papp of tilianin in rat jejunum were not significantly higher after being added with rifampicin. Conclusion： Tilianin is the substrate of P-gp, BCRP and SGLT1. The effluent effect of P-gp and BCRP is the main mechanism of tilianin in intestinal absorption, indicating that tilianin can realize intestinal absorption and transport by relying on SGLT1. Tilianin is not the substrate of bile salt transporter protein.