野黄芩苷对Caco-2细胞中P-gp蛋白表达及活性的影响  

Effect of Scutellarin on the Expression and Activity of P-gp in Caco-2 Cells

作　　者：柳睿[1] 金晶[1] 苟晓莉 周子懿[2] 蔡业峰[2] 黄民[1] 

机构地区：[1]中山大学药学院药物代谢与药动学实验室,广州510006 [2]广东省中医院神经1科

出　　处：《中国药师》2015年第4期529-532,共4页China Pharmacist

基　　金：广东省重点实验室建设项目(编号:2011A060901014);国家科技支撑计划项目(编号:2012BAI29B09);广东省重大科技专项(编号:2012A080202013);十二五重大专项(编号:2012ZX09506-001-004)

摘　　要：目的:研究野黄芩苷对Caco-2细胞中P-糖蛋白(P-gp)表达及活性的影响。方法:野黄芩苷(25,50及100μmol·L-1)与Caco-2细胞共孵育24 h,48 h及72 h后,通过western blot方法检测野黄芩苷对Caco-2细胞中P-gp蛋白表达的影响;通过罗丹明123转运试验,测定罗丹明123在Caco-2细胞内的累积量变化,以考察野黄芩苷对P-gp活性的影响。结果:野黄芩苷对Caco-2细胞中P-gp蛋白表达具有诱导作用,孵育24 h后,野黄芩苷(25,50及100μmol·L-1)对P-gp蛋白的上调倍数分别为2.34,2.65,2.00;孵育48 h后,野黄芩苷上调P-gp蛋白表达2.70,4.66,3.13倍;孵育72 h后,野黄芩苷(25,50及100μmol·L-1)对P-gp蛋白的上调倍数分别为2.82,2.62,1.84。野黄芩苷上调Caco-2细胞中P-gp蛋白表达的同时增加P-gp外排泵活性,孵育24 h后,野黄芩苷(25,50及100μmol·L-1)降低胞内罗丹明123累积量至70.6%,66.6%,76.6%;孵育48 h后,胞内罗丹明123累积量降低至55.6%,37.5%,65.2%;孵育72 h后,胞内罗丹明123累积量降低至45.5%,53.9%,60.3%。结论:野黄芩苷诱导Caco-2细胞中P-gp的蛋白表达,并能增加P-gp外排泵活性。Objective： To investigate the effect of scutellarin on P-gp protein expression and activity in Caco-2 cells. Methods：Scutellarin（ 25,50 and 100 μmol·L^-1） was incubated with Caco-2 cells respectively for 24 h,48 h and 72 h. The expression of Pgp was determined by western blot assay and the activity of P-gp was determined by Rhodamine-123 assay. Results： P-gp protein expression levels were significantly increased by scutelarin. After the incubation for 24 h with scutellarin,P-gp protein expression was upregulated 2. 34-,2. 65- and 2. 00- fold in Caco-2 cells. After the incubation with scutellarin for 48 h,P-gp protein expression was upregulated 2. 70-,4. 66- and 3. 13- fold. After the incubation with scutellarin for 72 h,P-gp protein expression was up-regulated 2. 82-,2. 62- and 1. 84-fold. The intracellular accumulation of rhodamine-123 was significantly decreased by scutellarin,indicating that the efflux transport activity of P-gp was increased by scutellarin in Caco-2 cells. Conclusion： Scutellarin can significantly up-regulate P-gp protein expression and increase the efflux transport activity of P-gp in Caco-2 cells.

关 键 词：野黄芩苷 P-GP 蛋白表达 罗丹明123 CACO-2 

分 类 号：R285.5[医药卫生—中药学]