一种利用荧光标记检测氨肽酶N抑制剂与肿瘤细胞结合的方法  

A method for Detecting the Binding Activities of Aminopeptidase N Inhibitors to Tumor Cell by Fluorescein

作　　者：王婷[1] 阮林高[1] 戈梅[2] 钱秀萍[1] 

机构地区：[1]上海交通大学药学院,上海200240 [2]上海来益生物药物研发中心,上海201203

出　　处：《现代生物医学进展》2014年第4期634-638,共5页Progress in Modern Biomedicine

基　　金：国家重大新药创制专项(2010zx09401-403)

摘　　要：目的:建立利用荧光标记法检测氨肽酶抑制剂和肿瘤细胞结合的方法。方法:以异硫氰酸荧光素(FITC)标记氨肽酶N抑制剂LYRM03和Bestatin,制备荧光探针FITC-LYRM03、FITC-Bestatin,应用荧光显微成像观察和流式细胞仪检测标记化合物FITC-LYRM03、FITC-Bestatin对肿瘤细胞的结合与氨肽酶N抑制活性的相关性。结果:化合物LYRM03和Bestatin具有肿瘤细胞的氨肽酶N抑制活性,荧光标记化合物FITC-LYRM03、FITC-Bestatin能与肿瘤细胞有不同程度的结合。结论:标记化合物FITC-LYRM03、FITC-Bestatin和肿瘤细胞的结合与对肿瘤细胞的氨肽酶N抑制活性相一致。Objective： To build a fluorescein labeling method to detect the bingding of aminopeptidase N inhibitors with tumor cells. Methods： Aminopeptidase N inhibitors LYRM03 and Bestatin were labeled with fluorescein isothiocyanate （FITC）, and fluorescein -labeled compounds of FITC-LYRM03 and FITC-Bestatin were purified. The relationship between binding activities to tumor cells and inhibitory activities of aminopeptidase N inhibitors was detected by using fluorescence microscope and flow cytometer. Results： Compounds of LYRM03 and Bestatin had inhibitory activities to aminopeptidase N of tumor cells. Fluorescein-labeled FITC-LYRM03 and FITC-Bestatin had different binding activities to tumor cells. Conclusion： There was consistency between binding activities of tumor cells and inhibitory activities of aminopeptidase N inhibitors.

关 键 词：氨肽酶N抑制剂 LYRM03 BESTATIN 异硫氰酸荧光素 

分 类 号：R730.231[医药卫生—肿瘤] R730.5[医药卫生—临床医学]