化学
溶剂变色
罗非昔布
荧光团
荧光
聚集诱导发射
生物物理学
赫拉
光化学
环氧合酶
生物化学
酶
体外
物理
生物
量子力学
溶剂
作者
Lijun Xie,Renfu Li,Bi-Yun Zheng,Zuoxu Xie,Xuefen Fang,Yanqi Wang,Gregory D. Cuny,Zhen-Li Li,Bin Lin,Xueyuan Chen,Ming Hu
标识
DOI:10.1021/acs.analchem.1c01978
摘要
Cyclooxygenase-2 (COX-2) fluorescent probes are promising tools for early diagnosis of cancer. Traditionally, COX-2 probes were designed by connecting two parts, a fluorophore and a COX-2 binding unit, via a flexible linker. Herein, a new class of COX-2-specific fluorescent probes have been developed via one-step modification from rofecoxib by an integrative approach to combine the binding unit and the fluorophore into one. Among them, several new rofecoxib analogues not only exhibited still potent COX-2 binding ability but also exhibited attractive fluorescence properties, such as tunable blue-red emission, solvatochromism, aggression-induced emission behavior, and mechanochromism. Notably, the emission of 2a16 can be switched between green-yellow in the crystalline state and red-orange in the amorphous state by grinding and fuming treatments. Furthermore, the highly fluorescent compound 2a16 (Φf = 0.94 in powder) displayed a much stronger fluorescence imaging of COX-2 in HeLa cancer cells overexpressing COX-2 than RAW264.7 normal cells with a minimal expression of COX-2. Most importantly, 2a16 can light up human cancer tissues from adjacent normal tissues with a much brighter fluorescence by targeting the COX-2 enzyme. These results demonstrated the potential of 2a16 as a new red fluorescent probe for human cancer imaging in clinical applications.
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