Zhang Hongxing, Lao Guanlin, Liu Mengxing, Jia Zhihui, Liu Jing, Guo Wei
School of Chemistry and Chemical Engineering, Shanxi University, Taiyuan 030006, China.
Chem Biomed Imaging. 2024 Jan 5;2(6):432-441. doi: 10.1021/cbmi.3c00107. eCollection 2024 Jun 24.
Fluorogenic probes have shown great potential in imaging biological species as well as in diagnosing diseases, especially cancers. However, the fluorogenic mechanisms are largely limited to a few photophysical processes to date, typically including photoinduced electron transfer (PeT), fluorescence resonant energy transfer (FRET), and intramolecular charge transfer (ICT). Herein, by calculations and experiments, we set forth that the inhibition of the excited-state π-conjugation in -ester Si-rhodamine or the de-π-conjugation in -ester cyanine 5 via the "" conversion can operate as a general fluorogenic mechanism to fabricate fluorogenic probes. Based on the mechanism and considering the higher chemical stability of than that of , we developed, as a proof-of-concept, three fluorogenic probes , , and on the basis of the platform for sensing cancer biomarkers aminopeptidase N (APN), γ-glutamyltranspeptidase (GGT), and nitroreductase (NTR), respectively, and demonstrated their outstanding performances in distinguishing between cancerous and normal tissues with the high tumor-to-normal tissue ratios in the range of 9-14.
荧光探针在生物物种成像以及疾病诊断，尤其是癌症诊断方面已显示出巨大潜力。然而，迄今为止，荧光机制在很大程度上局限于少数光物理过程，通常包括光致电子转移（PeT）、荧光共振能量转移（FRET）和分子内电荷转移（ICT）。在此，通过计算和实验，我们提出通过“”转化抑制 - 酯基硅罗丹明中的激发态π共轭或 - 酯基花菁5中的去π共轭可作为制造荧光探针的通用荧光机制。基于该机制，并考虑到 比 具有更高的化学稳定性，作为概念验证，我们分别基于 平台开发了三种用于检测癌症生物标志物氨肽酶N（APN）、γ-谷氨酰转肽酶（GGT）和硝基还原酶（NTR）的荧光探针 、 和 ，并证明它们在区分癌组织和正常组织方面具有出色性能，肿瘤与正常组织的高比率在9至14范围内。
