Department of Chemistry and Nanoscience, Ewha Womans University, Seoul, 03760, Korea.
State Key Laboratory of Fine Chemicals, Dalian University of Technology, 2 Linggong Road, Dalian, 116024, P. R. China.
Angew Chem Int Ed Engl. 2020 Jun 15;59(25):10186-10195. doi: 10.1002/anie.202001675. Epub 2020 Mar 10.
Monitoring fluctuations in enzyme overexpression facilitates early tumor detection and excision. An AIEgen probe (DQM-ALP) for the imaging of alkaline phosphatase (ALP) activity was synthesized. The probe consists of a quinoline-malononitrile (QM) core decorated with hydrophilic phosphate groups as ALP-recognition units. The rapid liberation of DQM-OH aggregates in the presence of ALP resulted in aggregation-induced fluorescence. The up-regulation of ALP expression in tumor cells was imaged using DQM-ALP. The probe permeated into 3D cervical and liver tumor spheroids for imaging spatially heterogeneous ALP activity with high spatial resolution on a two-photon microscopy platform, providing the fluorescence-guided recognition of sub-millimeter tumorigenesis. DQM-ALP enabled differentiation between tumor and normal tissue ex vivo and in vivo, suggesting that the probe may serve as a powerful tool to assist surgeons during tumor resection.
监测酶过表达的波动有助于早期肿瘤的检测和切除。本文合成了一种用于碱性磷酸酶（ALP）活性成像的 AIEgen 探针（DQM-ALP）。该探针由喹啉-丙二腈（QM）核心组成，表面修饰有作为 ALP 识别单元的亲水磷酸盐基团。在 ALP 的存在下，DQM-OH 聚集物迅速释放，导致聚集诱导荧光。利用 DQM-ALP 对肿瘤细胞中 ALP 表达的上调进行成像。该探针渗透到 3D 宫颈和肝肿瘤球体中，在双光子显微镜平台上以高空间分辨率对空间异质的 ALP 活性进行成像，提供了对亚毫米肿瘤发生的荧光引导识别。DQM-ALP 能够在体外和体内区分肿瘤和正常组织，表明该探针可能成为协助外科医生进行肿瘤切除的有力工具。
