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

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F1TC—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。

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

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.