中国临床药理学杂志2012，Vol.28Issue(1)：53-55,3.
流式细胞仪筛选P-糖蛋白的底物或抑制剂
Screening substrates or inhibitor of P- glycoprotein using flow cytometer
贾超 1魏敏吉 2邵克花 2赵秀丽1
作者信息
- 1. 首都医科大学附属北京同仁医院药物临床试验机构,北京100730
- 2. 北京大学第一医院临床药理研究所,北京100191
- 折叠
摘要
Abstract
Objective To study on screening tosufloxacin, sparfloxacin and simvastatin whether are substrates of P - glycoprotein ( P - gp) . Methods Compared with ketoconazole and lansoprazole, tosufloxacin, sparfloxacin and simvastatin's influence on P - glycoprotein's transportation of rhodamine - 123 will be measured by flow cytometer and we can find which are likely the substrates of P - glycoprotein. Then the likely substrates of P - glycoprotein will be test by transportation experiment using human colon adenocarcinoma line Caco - 2 cell mono-layer model. Results Tosufloxacin and sparfloxacin can significantly rendue the transportation of rhodamine - 123 by P - glycoprotein. When incubated by ketoconazole, the PappBL→Ap/PappAP→.BL of tosufloxacin decreased from 10. 03 ± 0. 47 to 0. 93 ± 0. 19 and the Papp. Bu→Ap/PaPPAp→Blof sparfloxacin decreased from 2. 54 ±0. 12 to 1. 02 ± 0.04. Conclusion Active transportation play a major role in the transportation of tosufloxacin and sparfloxacin in Caco - 2 cell mono-layer model. Tosufloxacin and sparfloxacin are likely substrates of P -glycoprotein.关键词
Caco-2细胞/P-gp底物/流式细胞仪/药物转运Key words
Caco - 2 cell/ substrates of P - glycoprotein/ flow cytometer/transportation of drugs分类
医药卫生引用本文复制引用
贾超,魏敏吉,邵克花,赵秀丽..流式细胞仪筛选P-糖蛋白的底物或抑制剂[J].中国临床药理学杂志,2012,28(1):53-55,3.
