P-糖蛋白抑制剂对蝙蝠葛碱跨膜转运的影响  

Effects of P-glycoprotein inhibitors on the transport of dauricine through membrane

作　　者：高秀蓉[1] 蒋学华[2] 杜青青[2] 宋林[2] 

机构地区：[1]成都医学院药学院药剂教研室,四川成都610083 [2]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2013年第2期135-139,共5页West China Journal of Pharmaceutical Sciences

基　　金：成都医学院院级科研课题(编号:CYZ09-008)

摘　　要：目的研究Caco-2细胞模型中P-糖蛋白抑制剂对蝙蝠葛碱跨膜转运的影响。方法采用HPLC法测定转运液中蝙蝠葛碱的含量;采用Caco-2细胞模型双向转运实验,考察不同浓度维拉帕米、环孢素A和醋酸地塞米松3种P-糖蛋白抑制剂对蝙蝠葛碱跨膜转运的影响。结果加入3种P-糖蛋白抑制剂后,蝙蝠葛碱的Papp(A-B)均有一定程度增加,而Papp(B-A)均有显著降低(P<0.05),即均抑制了蝙蝠葛碱的外排转运。结论外排转运体P-糖蛋白对蝙蝠葛碱有外排作用,蝙蝠葛碱可能为P-糖蛋白底物。OBJECTIVE To investigate the effect of P - gp inhibitors on the transport of dauricine through membrane in Caco - 2 cell line. METHODS HPLC was used to determine the concentration of dauricine ; bidirectional transport of dauricine in Caco - 2 cell model was used, and the effect of P - gp inhibitors Ver, CsA and Dex on the bidirectional transport of dauricine were studied. RESULTS P -gp inhibitors,Ver, CsA and Dex all could promote Papp（A- B） and reduce Papp（B-A） of dauricine in Caco -2 cell line. CONCLUSION P - gp can excrete dauricine, and dauricine maybe the substrate of P - gp.

关 键 词：蝙蝠葛碱 CACO-2细胞模型 P-糖蛋白 底物 多药耐药 北豆根 

分 类 号：R979.1[医药卫生—药品]