汉防己甲素抑制大鼠肠道内P-糖蛋白功能调节药物吸收的机制研究  

Mechanism of tetrandrine inhibiting P-glycoprotein function and regulating drug absorption in rat intestine

作　　者：余潜[1] 曹平 瞿庄茵 赵静[2] 高坤[2] YU Qian;CAO Ping;QU Zhuangyin;ZHAO Jing;GAO Kun(Department of Pharmacy,Nanjing First Hospital,Nanjing Medical University,Nanjing,Jiangsu 210006,China;Department of Nephrology,Jiangsu Province Hospital of Traditional Medicine,Nanjing,Jiangsu 210029)

机构地区：[1]南京医科大学附属南京医院(南京市第一医院)药学部,江苏南京210006 [2]江苏省中医院肾内科,江苏南京210029

出　　处：《徐州医科大学学报》2020年第11期786-789,共4页Journal of Xuzhou Medical University

基　　金：国家自然科学基金(81673912)。

摘　　要：目的研究汉防己甲素(TET)通过调节P-糖蛋白(P-gp)功能影响肠道药物吸收的作用。方法使用体外扩散池法(ussing chamber)测定评价P-gp底物罗丹明123(Rho123)在肠道内吸收方向和排出方向的透过量和透过系数(Papp),以及TET对Rho123和5(6)-羧基荧光素(CF)经离体大鼠肠黏膜透过性的影响。结果TET可以促进Rho123的吸收,抑制其排出,且这一功能与细胞旁路转运无关。结论TET可能具有抑制肠道内P-gp活性的作用。其可促进口服肿瘤药物的吸收并抑制多药耐药的发生,起到解毒增效的作用。Objective To investigate the effect of tetrandrine(TET)on intestinal absorption by regulating the function of P-glycoprotein(P-gp).Methods The permeability volume and coefficient of a P-glycoprotein substrate,rhodamine123(Rho123)on the intestinal absorption and emptying directions were determined by an in vitro diffusion chamber system.The effects of TET on Rho123 and 5(6)-carboxy fluorescein(CF)on in vitro permeability of rate intestinal mucosa were detected.Results TET could stimulate the absorption of Rho123 and inhibit its emptying,which was not related to the paracellular pathway.Conclusions TET may inhibit the activity of P-gp in the intestine.TET can promote the absorption of oral tumor drugs and inhibit multidrug resistance,so as to reduce toxicity and enhance effectiveness.

关 键 词：汉防己甲素 P-糖蛋白 罗丹明123 体外扩散池法 

分 类 号：R73-361[医药卫生—肿瘤]