盐酸度洛西汀对Caco-2细胞P-糖蛋白功能及表达的影响  

Effects of duloxetine on p-glycoprotein function and expression in Caco-2 cells

作　　者：陈芳[1] 赵瑞柯[1] 

机构地区：[1]南京医科大学附属苏州医院药剂科,江苏省215001

出　　处：《江苏医药》2013年第5期517-519,共3页Jiangsu Medical Journal

摘　　要：目的研究盐酸度洛西汀(DLX)对Caco-2细胞上P-糖蛋白(P-gp)功能和表达的影响。方法将Caco-2细胞分为阴性对照组、维拉帕米10μmol/L阳性对照组(VER组)和DLX 0.2、5、10μmol/L不同浓度处理组。采用流式细胞术检测DLX干预后Caco-2细胞内罗丹明-123的荧光强度和细胞膜上P-gp的表达量。结果与阴性对照组相比,DLX 0.2、5、10μmol/L均显著抑制罗丹明-123从Caco-2细胞的外排(96.3±4.5vs.129.5±14.5、131.2±7.0、135.6±17.1)(P<0.05),而对P-gp阳性率无明显改变(90%vs.94%、91%、89%)(P>0.05)。结论 DLX能抑制Caco-2细胞上P-gp的功能,降低罗丹明-123从Caco-2细胞中的外排,但并不影响P-gp的表达。Objective To investigate the effects of duloxetine（DLX） on P-glycoprotein（P-gp） function and expression in Caco-2 cells. Methods Caco-2 cells were incubated in vitro and divided into three groups of A（negative controls）, B（treated with verapamil 10 μmo1/L as positive controls） and C （treated with different concentrations of DLX 0.2, 5, 10 μmo1/L）. The fluorescence intensity of intracellular rhodamine-123 and P-gp expression in cell membrane after DLX intervention were detected by flow cytometry. Results Compared with group A, DLX 0. 2,5,10μmo1/L significantly inhibited the efflux of rhodamine-123 from Caco-2 cells （96.3±4.5 vs. 129.5±14. 5,131.2±7.0, 135.6±17.1）（P〈0. 05）, but did not obviously change the positive rate of P-gp（90 % vs. 94 %, 91%, 89%） （P〉0. 05）. Conclusion DLX can inhibit P-gp function and decrease the efflux of rhodamine- 123, but does not affect P-gp expression.

关 键 词：盐酸度洛西汀 P-糖蛋白 CACO-2细胞 罗丹明-123 

分 类 号：R969[医药卫生—药理学]