洛美利嗪对大鼠脑微血管内皮细胞上P-糖蛋白功能的影响

Effect of Lomerizine on the Activity of P-glycoprotein in Primary Cultured Rat Brain Microvessel Endothelial Cells

目的 :研究洛美利嗪对大鼠脑微血管内皮细胞上P 糖蛋白功能的影响。方法 :使用荧光分光光度计和流式细胞术分析大鼠脑微血管内皮细胞内P 糖蛋白底物 罗丹明 12 3的荧光强度。结果 :环孢素A和洛美利嗪与大鼠脑微血管内皮细胞孵育后能明显提高胞内罗丹明 12 3的荧光强度。人脐静脉内皮细胞内荧光强度则不受环孢素A和洛美利嗪的影响。结论 :洛美利嗪能显著地抑制大鼠脑微血管内皮细胞上P 糖蛋白的活性 ,提高P 糖蛋白底物的胞内浓度。

AIM:To study the effect of lomerizine on the activity of P-glycorprotein(P-gp) in primary cultured rat brain microvessel endothelial cells. METHOD: Fluorescence of Rhodamine123(Rh123) in RBMECs was measured by fluorescence spectrophotometry and flow cytometry. RESULT:Cellular fluorescence of Rh123 in RBMECs increased significantly after incubation with CsA and lomerizine. As a negative control, CsA and lomerizine have no effect on accumulation of Rhodamine123 in HUVECs. CONCLUTION:Lomerizine has a concentration-dependent inhibitory effect on the activity of P-glycoprotein in RBMECs and results in increases in the accumulation of P-glycoprotein substrates.