洛美利嗪抑制原代培养的脑微血管内皮细胞上P-糖蛋白的活性(英文)  

Lomerizine inhibits activity of P-glycoprotein in primary cultured brain microvessel endothelial cell monolayers

作　　者：李运曼[1] 康恺[1] 方伟蓉[1] 

机构地区：[1]中国药科大学生理教研室

出　　处：《中国临床药理学与治疗学》2006年第10期1110-1114,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的研究洛美利嗪对血脑屏障上P-糖蛋白功能活性的影响,寻找新型高效的P-糖蛋白抑制剂。方法使用罗丹明123荧光指示剂研究脑微血管内皮细胞上P-糖蛋白的活性,应用RT-PCR技术分析洛美利嗪对mdr基因mRNA的影响。结果洛美利嗪能够浓度依赖性地增加RBMECs中的罗丹明123水平,对RBMECs上mdr基因mRNA表达无影响。结论洛美利嗪通过抑制P-糖蛋白功能活性而逆转血脑屏障上的多药耐药。AIM： To study the effect of Lomerizine on the activity of P-glycoprotein （P-gp） in the bloodbrain barrier（BBB） and search for novel effective P-gp inhibiting agent against muhidrug resistance. METHODS： Rhodamine123 （Rh123） was used to examine the activity of P-gp and RT-PCR to study the mdr mRNA expression in cultured rat brain microvessel endothelial cells （RBMECs）. RESULTS： Lomerizine could increase the cellular Rh123 in RBMECs in a concentration-dependent manner. RT-PCR indicated that lomerizine could not down-regulate the expression of mdr mRNA. CONCLUSION： Lomerizine can reverse multidrug resistance in the blood-brain barrier by inhibiting the activity of P-gp.

关 键 词：洛美利嗪 P-糖蛋白 血脑屏障 RT-PCR 

分 类 号：R965.2[医药卫生—药理学] R966[医药卫生—药学]