文献类型：期刊文献

中文题名：一种硝基还原酶探针的合成与研究

英文题名：Synthesis and characterization of a nitroreductase probe

作者：黄微[1];吴君臣[1]

机构：[1]华东理工大学化学与分子工程学院,上海200237

年份：2018

卷号：13

期号：6

起止页码：649

中文期刊名：中国科技论文

外文期刊名：China Sciencepaper

收录：北大核心:【北大核心2017】；

基金：国家自然科学基金资助项目(21778017)

语种：中文

中文关键词：生物化学;荧光探针;硝基还原酶;RGD环肽;肿瘤

外文关键词：biochemistry;fluorescence probe;nitroreductase;cRGD;tumor

摘要：硝基还原酶(nitroreductase,NTR)通常在缺氧肿瘤细胞中过表达,其含量与细胞缺氧程度直接相关,因此有效检测NTR对肿瘤的诊断显得尤为重要。本研究设计合成了一种将环状精氨酸-甘氨酸-天冬氨酸(cRGD)与小分子硝基还原酶探针相结合的新型探针,该探针能通过检测细胞内NTR的含量进而研究肿瘤细胞的缺氧情况。紫外-可见吸收光谱、荧光光谱和细胞毒性实验证实了该探针具有很好的生物相容性,对NTR的检测具有高灵敏度、高选择性和高信噪比。细胞共聚焦成像实验证实探针可以与癌细胞特异性结合,为开发硝基还原酶探针提供了一种新的思路。
Nitroreductase（NTR）can be overexpressed in hypoxic tumors and the NTR level is directly related to the degree of hypoxia,thus the effective detection of NTR is particularly important.In this paper,we have designed and synthesized a novel probe which combines a cyclic RGD peptide with a small molecule nitro reductase probe.It can detect hypoxia by detecting the content of nitroreductase.The probe exhibits good sensitivity,excellent selectivity,high signal-noise ratio and good biocompatibility which are evidenced by UV-vis spectroscopy,fluorescence spectroscopy and cytotoxicity assay.Confocal laser scanning microscopy experiments confirm that the probe can specifically bind to cancer cells.This study provides a new idea for the development of nitroreductase probes.