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黄连黄芩配伍对大鼠肠黏膜P-gp活性的影响
  • ISSN号:1005-9903
  • 期刊名称:中国实验方剂学杂志
  • 时间:2012
  • 页码:141-146
  • 分类:R285.5[医药卫生—中药学;医药卫生—中医学]
  • 作者机构:[1]北京中医药大学中药学院,北京100102, [2]北京积水潭医院中药房,北京100035, [3]哈尔滨商业大学生命科学与环境研究中心,哈尔滨150028
  • 相关基金:国家自然科学基金项目(30672585,81073140)
  • 相关项目:基于ADME过程相关靶点系统调控的经方黄连药对配伍机理研究
中文摘要:

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。

英文摘要:

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.

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期刊信息
  • 《中国实验方剂学杂志》
  • 北大核心期刊(2011版)
  • 主管单位:国家中医药管理局
  • 主办单位:中国中医科学院中药研究所 中华中医药学会
  • 主编:吴以岭
  • 地址:北京东直门内南小街16号中国中医科学院中药研究所304室
  • 邮编:100700
  • 邮箱:syfjx_2010@188.com
  • 电话:010-84076882
  • 国际标准刊号:ISSN:1005-9903
  • 国内统一刊号:ISSN:11-3495/R
  • 邮发代号:2-417
  • 获奖情况:
  • 全国中医药优秀期刊三等奖,首届《CAJ-CD规范》执行优秀奖
  • 国内外数据库收录:
  • 美国化学文摘(网络版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版)
  • 被引量:59476