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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 establish a method for detecting the binding of aminopeptidase inhibitors and tumor cells by fluorescent labeling. Methods: FITC-LYRM03 and FITC-Bestatin were prepared by labeling aminopeptidase N inhibitors LYRM03 and Bestatin with fluorescein isothiocyanate (FITC). Fluorescence microscopy and flow cytometry were used to detect the FITC-LYRM03 and FITC- -LYRM03, FITC-Bestatin on tumor cells and aminopeptidase N inhibitory activity. Results: The compounds LYRM03 and Bestatin had the activity of inhibiting aminopeptidase N of tumor cells. The fluorescent labeled compounds FITC-LYRM03 and FITC-Bestatin had different degrees of binding with tumor cells. CONCLUSION: The binding of the labeled compounds FITC-LYRM03, FITC-Bestatin and tumor cells is consistent with the aminopeptidase N inhibitory activity on tumor cells.