Gao Weijie, Shi Anyang, Hou Yunzhuo, Zhang Peng, Zhang Qian, Ding Caifeng
Key Laboratory of Optic-Electric Sensing and Analytical Chemistry for Life Science, MOE, Shandong Key Laboratory of Biochemical Analysis, Key Laboratory of Analytical Chemistry for Life Science in Universities of Shandong, College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology, Qingdao, 266042, PR China.
Key Laboratory of Optic-Electric Sensing and Analytical Chemistry for Life Science, MOE, Shandong Key Laboratory of Biochemical Analysis, Key Laboratory of Analytical Chemistry for Life Science in Universities of Shandong, College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology, Qingdao, 266042, PR China.
Talanta. 2025 Aug 1;290:127804. doi: 10.1016/j.talanta.2025.127804. Epub 2025 Feb 24.
Nitroreductase (NTR) is an endogenous reductase overexpressed in hypoxic tumors, with its levels closely correlated to the degree of hypoxia. This correlation has significant clinical implications for the analysis of tumor hypoxia, as it allows for the indirect detection of nitroreductases. Due to their simplicity, noninvasive nature, and excellent spatiotemporal resolution, various fluorescence methods have been developed for the analysis of nitroreductase and tumor hypoxia. In this study, we present the design, synthesis, in vitro evaluation, and biological application of an NTR-activated fluorescent probe, F-NTR. Utilizing an oxanthrene fluorophore as the core component, F-NTR incorporates a 4-nitrobenzene recognition group. This innovative probe, which introduces a nitro group, demonstrates high selectivity and reactivity towards nitroreductase (NTR) due to its reducing properties. Furthermore, probe F-NTR is capable of accurately identifying hypoxic environments, which provides a basis for precise detection and localization of tumors. This work lays the groundwork for future investigations into cell metabolism, tumor metabolism, and the surgical management of solid tumors under hypoxic conditions.
硝基还原酶（NTR）是一种在缺氧肿瘤中过表达的内源性还原酶，其水平与缺氧程度密切相关。这种相关性对肿瘤缺氧分析具有重要的临床意义，因为它可以间接检测硝基还原酶。由于其简单性、非侵入性和出色的时空分辨率，已开发出各种荧光方法用于分析硝基还原酶和肿瘤缺氧。在本研究中，我们展示了一种NTR激活的荧光探针F-NTR的设计、合成、体外评估及生物学应用。F-NTR以呫吨荧光团作为核心成分，并结合了一个4-硝基苯识别基团。这种引入硝基的创新探针，由于其还原特性，对硝基还原酶（NTR）表现出高选择性和反应活性。此外，探针F-NTR能够准确识别缺氧环境，为肿瘤的精确检测和定位提供了依据。这项工作为未来对细胞代谢、肿瘤代谢以及缺氧条件下实体瘤手术管理的研究奠定了基础。
