| 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 |
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| 引用本文： | 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 |
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| 作者姓名： | 李运曼 康恺 方伟蓉 |
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| 作者单位： | 中国药科大学生理教研室,南京,210009,江苏 |
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| 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。
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| 关 键 词： | 洛美利嗪 P-糖蛋白 血脑屏障 |
| 文章编号： | 1009-2501(2006)10-1110-05 |
| 收稿时间： | 2006-05-16 |
| 修稿时间： | 2006-06-29 |
Lomerizine inhibits activity of P-glycoprotein in primary cultured brain microvessel endothelial cell monolayers |
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| 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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| Authors: | LI Yun-man KANG Kai FANG Wei-rong |
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| Affiliation: | Department of Physiology, China Pharmaceutical University, Nanjing 210009, Jiangsu, China |
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| Abstract: | AIM: To study the effect of Lomerizine on the activity of P-glycoprotein (P-gp) in the blood-brain barrier(BBB) and search for novel effective P-gp inhibiting agent against multidrug 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. |
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| Keywords: | RT-PCR |
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