维生素E聚乙二醇1000琥珀酸酯对Caco-2细胞模型转运宝藿苷Ⅰ的影响  

Influence of vitamin E tocopherol polyethylene glycol succinate 1000 on baohuoside Ⅰ across membrane transport of Caco-2 monolayer model

作　　者：金鑫[1,2] 张振海[1] 陈玲玲[1] 贾晓斌[1,2] 谭晓斌[1] 陈彦[1] 

机构地区：[1]江苏省中医药研究院国家中医药管理局中药释药系统重点研究室,江苏南京210028 [2]南京中医药大学药学院,江苏南京210046

出　　处：《中草药》2011年第12期2474-2478,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(30973944)

摘　　要：目的考察非离子表面活性剂维生素E聚乙二醇1000琥珀酸酯(TPGS)对宝藿苷I在Caco-2细胞模型转运的影响。方法采用Caco-2细胞模型研究不同浓度的TPGS对宝藿苷Ⅰ细胞转运行为的影响,以超高压液相色谱(UPLC)法测定细胞样品溶液中宝藿苷I的浓度,计算表观渗透系数(Papp)。结果在应用TPGS后,宝藿苷Ⅰ从细胞绒毛面供给侧(AP)→基底面外侧(BL)的跨膜转运量明显增高(P<0.05),外排比率显著下降(P<0.05)。当宝藿苷Ⅰ与TPGS比例分别为1∶1、1∶3、1∶9时,宝藿苷Ⅰ的外排比率分别为1.978 8、1.779 8、1.609 0,与仅用宝藿苷Ⅰ相比分别下降了73%、76%、78%。结论在Caco-2细胞模型上,TPGS可显著促进宝藿苷Ⅰ的吸收。Objective To investigate the effect of non-ionic surfactant vitamin E tocopherol polyethylene glycol succinate 1000（TPGS） on the intestinal absorption of baohuoside Ⅰ across membrane transport of Caco-2 monolayer model.Methods The membrane transport of Caco-2 monolayer model was carried out to examine the effects of TPGS on the intestinal absorption of baohuoside Ⅰ.The baohuoside Ⅰ was determined by UPLC and the apparent permeability coefficients（Papp） were calculated.Results Papp values of membrane transport capacity from the apical（AP） to basolateral（BL） of baohuoside Ⅰ were significantly increased（P0.05） and its efflux ratios were markedly reduced（P0.05） in the presence of the TPGS.The efflux of baohuoside Ⅰ was 1.978 8,1.779 8,and 1.609 0,respectively,when the proportion of baohuoside Ⅰ and TPGS was 1：1,1：3,and 1：9.The ratio decreased 73%,76%,and 78% by using baohuoside Ⅰ only.Conclusion TPGS could obviously promote the absorption of baohuoside Ⅰ on Caco-2 monolayer model.

关 键 词：宝藿苷Ⅰ CACO-2细胞模型 维生素E聚乙二醇1000琥珀酸酯 跨膜转运 肠道吸收 

分 类 号：R282.710.5[医药卫生—中药学]