摘要
目的:评价连续ig黄连、黄芩提取液及其黄连-黄芩合煎液对大鼠肠黏膜上P-糖蛋白(P-glycoprotein,P-gp)活性的影响,探讨黄连-黄芩药对配伍的机制。方法:将大鼠随机分为5组。连续ig黄连、黄芩提取液及其合煎液1周诱导后,采用非翻转肠囊和翻转肠囊实验,以累计渗透率和表观渗透系数(Papp)为考察指标,体外评价P-gp底物罗丹明123(rhodamine123,R123)和非P-gp底物荧光素钠(fluorescein sodium,FS)经大鼠空肠黏膜吸收方向(M-S)和分泌方向(S-M)的转运变化。结果:黄连提取液能减少R123经空肠M-S方向的转运(P<0.05),对S-M方向转运没有显著影响。黄芩及其黄连-黄芩合煎液均能不同程度的增加R123经空肠M-S方向的转运,同时可不同程度的降低S-M方向的转运。在评价各组药液对旁细胞转运药物FS影响的实验中,黄连、黄芩和黄连-黄芩合煎液(2∶1)组在M-S和S-M双活性方向对FS的透过性均无显著影响,而黄连-黄芩合煎液(1∶1)组可同时降低双方向的透过性。各组的泵出比较生理盐水组无显著差异。结论:黄连提取液连续ig可增加大鼠肠黏膜上P-gp的活性,而黄芩对P-gp的活性具有一定的抑制作用,合煎液与黄芩相似,但抑制作用更强。与生理盐水组相比,三者抑制作用强弱顺序为1∶1合煎组最强,2∶1合煎组次之,黄芩组最弱。
Objective：To investigate the effect of Coptis-scute herb and combined（2∶1,1∶1） use on the P-glycoprotein function in rat jejunum.Method： The rats were randomly divided into five groups.Rhodamine 123（R123） and fluorescein sodium（FS）,a P-gp substrate and a non-P-gp substrate model drug were taken as investigating indicator.After oral administration of four different decoctions of Coptis-scute herb and its combination（2∶1,1∶1） for successive 7 days,the cumulative permeability percentage and the apparent permeability coefficient（Papp） of R123 or FS were evaluated by applying a rat everted gut sac as well as a non everted gut sac method.Result： The absorptive directed permeability（mucosa to serosa,M-S） of R123 can be increased after oral administration of Coptis decoction,and on the other hand,the secretory directed transport（serosa to mucosa,S-M） be decreased,but there is no significant effect.The other three groups can increase M-S of R123 as well as reduce S-M,but there is no significant difference on the S-M after oral administration of Scute decoction.In parietal cells transport of FS,no significant effect can be found in Coptis-scute herb and its combination 2∶1 group on two direction transport but decreased effect can be found in combination1∶1 group.Comparing with the efflux ratios（ER） of physiological saline,there are no significant differences on the four groups.Conclusion： Coptis could increase P-gp activity,and Scute may have opposite effect.The rest of the two groups have stronger inhibition than Scute.1∶1 group was the strongest one,followed by 2∶1,the weakest was the Scute group.
出处
《中国实验方剂学杂志》
CAS
北大核心
2012年第8期141-146,共6页
Chinese Journal of Experimental Traditional Medical Formulae
基金
国家自然科学基金项目(30672585
81073140)
关键词
黄连
黄芩
配伍
P-gp活性
大鼠肠黏膜
Rhizoma Coptidis
Radix Scutellariae
combination
P-glycoprotein function
rat jejunum
