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New approach for screening anti—tumor compounds
作者姓名:PANYuanjiang  ZHANGHong  CHENYaozu
作者单位:[1]DepartmentofChemistry,ZhejiangUniversity,Hangzhou310027,China [2]DepartmentofFoodScience,HangzhouUniversityofCommerce,Hangzhou310035,China
基金项目:国家科学基金,浙江省自然科学基金 
摘    要:A new screening approach for anticancer active compounds is presented.In this method,a target enzyme is incubated with a mixture of compounds,and then the com-plex formed by the target and small molecules is separated from the rest of the mixture by ultra-filtration.The complex that is retained on the membrane is subsequently washed with acid and small molecules that are specifically bound to the target are released and collected,then analyzed by high-performance liquid chromatograph combined with electrospray ionization mass spectrometry (HPLC/ESI-MS) analysis.We have successfully applied this method to screen anti-cancer compounds.DNA topoisomerase Ⅱ is used as a target to capture anti-tumor candidates from a mixture of combinatorial compounds,such as doxorubicin,daunorubi-cin and pravastain.

关 键 词:抗肿瘤化合物  抗癌药物  药物筛选  液相色谱法  药物开发
收稿时间:2002-07-10

New approach for screening anti-tumor compounds
PANYuanjiang ZHANGHong CHENYaozu.New approach for screening anti-tumor compounds[J].Chinese Science Bulletin,2003,48(7):630-633.
Authors:Yuanjiang Pan  Hong Zhang  Yaozu Chen
Institution:PAN Yuanjiang1, ZHANG Hong1,2 & CHEN Yaozu1 1. Department of Chemistry, Zhejiang University, Hangzhou 310027, China; 2. Department of Food Science, Hangzhou University of Commerce, Hangzhou 310035, China
Abstract:A new screening approach for anticancer active compounds is presented. In this method, a target enzyme is incubated with a mixture of compounds, and then the complex formed by the target and small molecules is separated from the rest of the mixture by ultra-filtration. The complex that is retained on the membrane is subsequently washed with acid and small molecules that are specifically bound to the target are released and collected, then analyzed by high-performance liquid chromatograph combined with electrospray ionization mass spectrometry (HPLC/ESI-MS) analysis. We have successfully applied this method to screen anti-cancer compounds. DNA topoisomeraseⅡ is used as a target to capture anti-tumor candidates from a mixture of combinatorial compounds, such as doxorubicin, daunorubicin and pravastain.
Keywords:bio-affinity ultrafiltration  high throughput screening  anticancer active compounds  high-performance liquid chromatography (HPLC)  electrospray ionization mass spectrometry (ESI-MS)
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