P-gp蛋白功能抑制剂高通量筛选模型的建立与应用  

A high throughput screening model for P-gp functional inhibitors

作　　者：郎廷元[1] 晏菊芳 胡昌华[1] 

机构地区：[1]西南大学药学院现代生物医药研究所,重庆400716 [2]成都地奥制药集团药物研究所,四川成都610041

出　　处：《中国药理学通报》2007年第10期1396-1399,共4页Chinese Pharmacological Bulletin

基　　金：重庆市科技攻关项目基金资助(No2003-8110)

摘　　要：目的建立高通量筛选模型,寻找疗效好、毒副作用小的肿瘤多药耐药逆转剂。方法以罗丹明123荧光染料胞内积累实验为基础,建立基于细胞水平的高通量筛选模型,对480个中药样品进行了高通量筛选,并采用剂量—活性依赖实验和抗性增敏实验验证阳性样品。结果模型Z′因子为0.72,筛选得到2个中药样品。结论建立的P-gp蛋白功能抑制剂高通量筛选模型稳定性好,灵敏度高,筛选得到的2种中药样品具有较好的P-gp蛋白功能抑制活性。Aim To establish a cell model for high throughput screening and search for novel inhibitors of P-gp. Methods A fluorescent cell-based assay was developed for application in high throughput screening. A library of 480 traditional Chinese medicine samples was screened. Results The value of Z＇ was 0. 72. Screening of a library of 480 traditional Chinese medicine identified 2 positive samples. Conclusions This HTS model for screening P-gp inhibitors was stable and sensitive. The 2 positive samples had good P-gp inhibitory activities.

关 键 词：P糖蛋白 抑制剂 高通量筛选 中药样品 

分 类 号：R556[医药卫生—血液循环系统疾病] R965.1[医药卫生—内科学]