Sun Qian, Liu Hang, Yang Ying, Yao Shankun, Liu Zhipeng, Guo Zijian
Chemistry and Biomedicine Innovation Center (ChemBIC), State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023 China.
College of Materials Science and Engineering, College of Science, Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, Nanjing Forestry University, Nanjing 210037, China.
Chem Biomed Imaging. 2025 Mar 3;3(4):260-266. doi: 10.1021/cbmi.4c00115. eCollection 2025 Apr 28.
Cu(II) ions play a critical role in tumor growth and metastasis, making in vivo high-resolution imaging of Cu(II) crucial for understanding its role in tumor pathophysiology. However, designing suitable molecular probes for this purpose remains challenging. Herein, we report the development of a photoacoustic probe for specific in vivo imaging of Cu(II) in tumors. This probe utilizes β-galactoside as a targeting group and incorporates a unique self-immobilization strategy. Upon β-galactosidase-mediated cleavage, the probe generates a reactive quinone methide intermediate that covalently binds to intracellular proteins, enabling selective tumor accumulation. The probe exhibits a ratiometric photoacoustic response to Cu(II) with high selectivity over that of other biological species. In vitro and in vivo studies demonstrated the efficacy of the probe for Cu(II) imaging in tumors. This research provides valuable insights into the role of Cu(II) in tumorigenesis and may facilitate the development of diagnostic and therapeutic approaches for cancer.
铜（II）离子在肿瘤生长和转移中起着关键作用，因此对铜（II）进行体内高分辨率成像对于理解其在肿瘤病理生理学中的作用至关重要。然而，为此目的设计合适的分子探针仍然具有挑战性。在此，我们报告了一种用于肿瘤中铜（II）特异性体内成像的光声探针的开发。该探针利用β-半乳糖苷作为靶向基团，并采用了独特的自固定策略。在β-半乳糖苷酶介导的裂解作用下，该探针产生一种反应性醌甲基化物中间体，该中间体与细胞内蛋白质共价结合，从而实现肿瘤的选择性积累。该探针对铜（II）表现出比率光声响应，对其他生物物种具有高选择性。体外和体内研究证明了该探针在肿瘤中进行铜（II）成像的有效性。这项研究为铜（II）在肿瘤发生中的作用提供了有价值的见解，并可能促进癌症诊断和治疗方法的发展。
