以微管蛋白为靶的高通量药物筛选方法的建立与应用  

Establishment and application of a high throughput microtubule-targeted screening assay

作　　者：孙婉[1] 李敏[1] 魏少荫[1] 吴军[1] 徐波[1] 崔景荣[1] 

机构地区：[1]北京大学天然药物及仿生药物国家重点实验室,北京100083

出　　处：《中国新药杂志》2006年第21期1828-1831,共4页Chinese Journal of New Drugs

基　　金：国家高技术研究发展(863)计划(2002AA2Z343C)

摘　　要：目的:以微管蛋白为靶建立高通量筛选(HTS)模型,以便有效地发现抗肿瘤化合物。方法:细胞培养与免疫荧光技术。结果:以常规的免疫组化(玻片)方法为基础优化实验条件,在96孔板上建立了以微管蛋白为靶点的高通量药物筛选模型;抗肿瘤药物紫杉醇和秋水仙碱作用于人肝癌HepG2细胞后,细胞的免疫荧光强度发生了明显的可检测的变化,间接反映药物对细胞微管蛋白聚合／解聚作用的影响,与理论预测结果一致。结论:基于人种瘤细胞的以微管蛋白为靶点的高通量筛选方法可用于抗肿瘤化合物的筛选。Objective： To establish a novel high throughput screening （HTS） model targeted on microtubule to efficiently screen anti-cancer drugs. Method： A microtubule-targeted HTS model was developed onto 96-well culture plates. The assay process was optimized by immunofluorescence technology. Results： The change of cellular immunofluorescent intensity was significantly visualized after incubation of palitaxel and colchicine with HepG2 cells for 6 h respectively, which suggested the detectable activities of the drugs on microtubule assembly/disassembly. Conclusion： The microtubule-targeted HTS model to screen anti-cancer agents was achievable.

关 键 词：微管蛋白 免疫荧光 抗肿瘤 高通量筛选 

分 类 号：R965.1[医药卫生—药理学] R979.1[医药卫生—药学]