(P—gP)expressioninMDCK—MDR1 cells,itcouldbeusedasadrugtransportmodeltoscreenP—gpsubstratesorinhibitors,aswellasmodels ofintestinalmucosa,bloodbrainbarrierandkidney.AlthoughtherearesomedisadvantagesinMDCK— MDR1cellmodel,itisaneffectivetoolforimplementingpermeabilityofdruginanoptimalfashion. Keywords:MDCK—MDR1...
inMDCK—MDRl highpolarizedP-glycoprotein(P—gP)expression asmodels couldbeusedasa modeltoscreensubstratesor well cells,it drugtransport P-gP inhibitors,as ofintestinal brainbarrierand therearesome inMDCK- mucosa,blood kidney.Although disadvantages MDRlcell isaneffectivetoolfor of inan fashion. model,...
B ecau se there is h igh po larized Pglycop rotein ( Pgp ) exp re ssion in MDCKMDR 1 cells, it cou ld be u sed a s a drug tran sport model to screen Pgp sub strate s or inh ib itors, a s well a s models of in te stinal m uco sa, b lood b rain barrier and k...
MDCK-MDR1细胞系高表达 P-糖蛋白(P-glycoprotein, P-gp), 且 P-gp呈极性分布, 因而它可以作为药物转运模型快速筛选 P-gp底物和抑制剂, 以及肠道、血脑屏障、肾脏的体外模型。关键词:MDCK-MDR1细胞;P-糖蛋白;药物转运;细胞模型中图分... 文档格式:PDF | 页数:6 | 浏览次数:396 | 上传日期:2018-07-...
MDCK2MDR1细胞模型及其在药物透过研究中的应用进展刘 瑶,曾苏3(浙江大学药学院,浙江杭州310058)摘要:本文介绍了MDCK2MDR1细胞系的特点、模型的建立,药物在其细胞模型上吸收转运的研究进展。概述了国内外关于利用MDCK2MDR1细胞系作为模型进行药物筛选、药物相互作用和研究药物吸收转运机制等方面的内容。MDCK2MDR1细胞系...
方法用表观通透性系数(Papp)测定长春新碱经MDCK-MDR1细胞膜的转运,以观察佛手柑内酯对长春新碱转运的影响。采用分子对接预测佛手柑内酯与P-糖蛋白(P-gp)的结合力。通过罗丹明123(Rho123)的蓄积和活性分析,确定了佛手柑内酯对P-gp功能和P-gp ATP酶活性的影响。以1,6-二苯基-1,3- 5-己三烯(DPH)为研究...
MDCK2 MDR1细胞模型及其在药物透过研究中的应用进展刘 瑶 , 曾 苏3(浙江大学 药学院 , 浙江 杭州 310058)摘要 : 本文介绍了 MDCK2 MDR1细胞系的特点、 模型的建立 ,药物在其细胞模型上吸收转运的研究进展。概述了国内外关于利用 MDCK2 MDR1细胞系作为模型进行药物筛选、 药物相互作用和研究药物吸收转运机制等...
Preparation of MDR1-MDCK Cells Figure 2. Morphology of MDR1-MDCK cells. Method and Results Compounds are applied to the apical or basolateral side of the cell monolayer. The apparent permeability and efflux ratio of the test compounds was determined in duplicate. Compounds were quantified by LC...
Because there is high polarized P-glycoprotein (P-gp) expression in MDCK-MDR1 cells, it could be used as a drug transport model to screen P-gp substrates or inhibitors, as well as models of intestinal mucosa, blood brain barrier and kidney. Although there are some disadvantages in MDCK-...
The polarized efflux activities of P-gp(s) in MDCK-MDR1 cells, MDCK-WT cells, and Caco-2 cells were compared using digoxin as a substrate. Apparent Michaelis-Menten constants (KM,Vmax) for the efflux of vinblastine in these three cell lines were determined. Apparent inhibition constants (KI...