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

中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (10): 1110-1114.

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

李运曼, 康恺, 方伟蓉

中国药科大学生理教研室, 南京 210009 , 江苏

收稿日期:2006-05-16 接受日期:2006-06-29 出版日期:2006-10-26 发布日期:2020-11-05

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

LI Yun-man, KANG Kai, FANG Wei-rong

Department of Physiology , China Pharmaceutical University , Nanjing 210009 , Jiangsu , China

Received:2006-05-16 Accepted:2006-06-29 Online:2006-10-26 Published:2020-11-05
Contact: LI Yun-man ,female , PhD, professor , master supervisor, majoring in cardiovascular pharmacology , anti-inflammation and immunopharmacology.Tel:025-85325383 Email:yvcaoren@sina.com

摘要/Abstract

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。

关键词: 洛美利嗪, P-糖蛋白, 血脑屏障, RT-PCR

Abstract: 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-gPinhibiting agent against multidrug resistance.METHODS: Rhodamine123 (Rh123)was used to examine the activity of P-gPand 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.

Key words: lomerizine, P-glycoprotein, bloodbrain barrier, RT-PCR

中图分类号:

R965.2
R966

李运曼, 康恺, 方伟蓉. 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[J]. 中国临床药理学与治疗学, 2006, 11(10): 1110-1114.

LI Yun-man, KANG Kai, FANG Wei-rong. Lomerizine inhibits activity of P-glycoprotein in primary cultured brain microvessel endothelial cell monolayers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2006, 11(10): 1110-1114.

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