槲皮素对小肠吸收阿昔洛韦的促进作用

目的: 研究槲皮素抑制P-糖蛋白(P-Glycoprotein P-gp)对小肠吸收阿昔洛韦的影响.方法: 采用小肠翻转实验和离体小肠吸收实验考察槲皮素促进阿昔洛韦的吸收.结果:小肠翻转实验结果表明,经不同浓度的槲皮素溶液孵育后,阿昔洛韦由小肠黏膜侧到浆膜侧的转运量随槲皮素浓度的增加而增加,经拟合符合Boltzmann 方程;离体小肠吸收实验结果表明,经不同浓度的槲皮素溶液孵育后,阿昔洛韦由小肠浆膜侧到黏膜侧的转运量随槲皮素浓度的增加而减少.结论:槲皮素为P-gp抑制剂,其多药耐药逆转作用有利于促进阿昔洛韦的吸收.

Effect of quercetin on the acyclovir intestinal absorption

Objective: To study the effect of quercetin on acyclovir intestinal absorption. Methods: The everted gut sac and in vitro intestinal absorption tests were performed. The acyclovir transport quantity was determined by HPLC method. Results: The everted gut sac study showed that quercetin significantly inhibited the function of intestinal P-glycoprotein (P-gp). The acyclovir transport quantities from mucosa to serosa space, which incubated with 5,10,80 mg/L quercetin solution or 10 mg/L verapamil solution, were increased 0.3, 0.6, 1.0 and 1.0-fold higher than acyclovir alone, respectively. The transport quantity caused by inhibition of intestinal P-gp function fitted with Boltzmann equation. The in vitro intestinal absorption test indicated that the transported acyclovir from serosa to mucosa, incubated with 2,5,10 mg/L quercetin solution, was significantly decreased compared with acyclovir alone. Conclusion: Quercetin can enhance acyclovir intestinal absorption by inhibiting the function of P-gp.