灯盏花素对Caco-2细胞中P-gp蛋白外排活性的影响  

Effect of Breviscapin on the Efflux Activity of P-gp in Caco-2 Cells

作　　者：周玄 曹昌娥 杨娇 阳美松 邵明园 高洋洋 赖泳 Zhou Xuan;Cao Chang-e;Yang Jiao;Yang Meisong;Shao Mingyuan;Gao Yangyang;Lai Yong(College of Pharmacy and Chemistry, Dali University, Dali, Yunnan 671000, China;Key Laboratory of Pharmaceutical R & D of Insects in Yunnan Province, Dali, Yunnan 671000, China)

机构地区：[1]大理大学药学与化学学院,云南大理671000 [2]云南省昆虫医药研发重点实验室,云南大理671000

出　　处：《大理大学学报》2017年第4期20-23,共4页Journal of Dali University

基　　金：国家自然科学基金资助项目(81241139;81360511);云南省教育厅科学研究基金资助项目(2013J118)

摘　　要：目的:研究灯盏花素对Caco-2细胞中P-糖蛋白(P-gp)外排活性的影响。方法:采用MTT法检测灯盏花素对Caco-2细胞存活率的影响,以确定其试验剂量;通过BCA法测定灯盏花素对Caco-2细胞中总蛋白量的影响,罗丹明123(Rh123)转运试验评价灯盏花素作用后时间对P-gp外排活性的影响。结果:灯盏花素浓度<577.95μg/m L时,Caco-2细胞的存活率>90%;灯盏花素能增加Caco-2细胞中P-gp的外排活性,加入Rh123后,Rh123在Caco-2细胞内的累积量先增加再减少;作用60 min后,灯盏花素(120、240μg/m L)对Caco-2细胞内总蛋白量分别上调222.87%,154.23%。结论:灯盏花素能增加P-gp的外排活性,并上调Caco-2细胞中的总蛋白量。Objective:To investigate the effect of breviscapin on the efflux activity of P-gp in Caco-2cells.Methods:Cell survival rate of Caco-2cells with different breviscapin concentrations were measured by MTT assay.The BCA assay was used to determine the total protein level of Caco-2cells and the efflux activity of P-gp was determined by Rhodamine-123assay after the incubation with breviscapin.Results:The cell survival rate of Caco-2cells was higher than90%when the concentration of breviscapin was less than577.95μg/mL.The efflux activity of P-gp was increased by breviscapin(120μg/mL,240μg/mL)in Caco-2cells.The intracellular accumulation of rhodamine-123was increased and then decreased after the addition of rhodamine-123.After the incubation for60min with breviscapin(120μg/mL,240μg/mL),total protein level in Caco-2cells was up-regulated222.87%,154.23%respectively.Conclusion:Breviscapin can up-regulate total protein level and increase the efflux activity of P-gp in Caco-2cells.

关 键 词：灯盏花素 P-糖蛋白 CACO-2细胞 罗丹明123 

分 类 号：R285[医药卫生—中药学]