文献类型：期刊文献

英文题名：Fluorogenic Labeling Probe for the Imaging of Endogenous β-Galactosidase Activity in Cancer and Senescent Cells

作者：Wang, Jing-Bo[1,2];Zhao, Xue-Ru[1,2,4];Hu, Xi-Le[1,2];Zang, Yi[5];Li, Jia[4];He, Xiao-Peng[1,2,3]

机构：[1]East China Univ Sci & Technol, Key Lab Adv Mat, Sch Chem & Mol Engn, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Feringa Nobel Prize Scientist Joint Res Ctr, Sch Chem & Mol Engn, Joint Int Res Lab Precis Chem & Mol Engn, Shanghai 200237, Peoples R China;[3]Eastern Hepatobiliary Surg Hosp, Natl Ctr Liver Canc, Int Cooperat Lab Signal Transduct, Shanghai 200438, Peoples R China;[4]Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Chem Biol, Shanghai 201203, Peoples R China;[5]Lingang Lab, Shanghai 201203, Peoples R China

年份：2024

卷号：16

期号：50

起止页码：68918

外文期刊名：ACS APPLIED MATERIALS & INTERFACES

收录：;EI(收录号：20245017524469);WOS:【SCI-EXPANDED(收录号:WOS:001372905300001)】；

基金：The authors thank the Natural National Science Foundation of China (NSFC) (nos. 92253306, 82130099, and 22108077), the International Cooperation Program of Shanghai Science and Technology (no.23490711600), the Fundamental Research Funds for the Central Universities (222201717003), the Programme of Introducing Talents of Discipline to Universities (B16017), the Open Funding Project of the State Key Laboratory of Bioreactor Engineering, State Key Laboratory of Drug Research (SKLDR-2023-KF-10), State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan University, Changsha 410082, P. R. China, and Ministry of Education Key Laboratory on Signaling Regulation and Targeting Therapy of Liver Cancer (Naval Medical University) (grant no. 2023-MEKLLC-MS/ZD-00*) for financial support. The Research Center of Analysis and Test of East China University of Science and Technology is gratefully acknowledged for assistance in analytical experiments.

语种：英文

外文关键词：fluorogenic probe; labeling; glycosidases; cell imaging; cancer; senescence

摘要：The sensitive detection of glycosidases in live cells is crucial to understanding their functional roles in disease progression. Here, we develop a fluorogenic labeling probe for beta-galactosidase (beta-Gal) based on a bright green-emitting fluorescent dye, fluorescein. Galactose was introduced to a fluoromethyl-substituted fluorescein derivative through a benzyl spacer, resulting in a quenched fluorescence due to spirocyclization of the dye. After removal of the galactosyl residue by beta-Gal, an similar to 210-fold enhanced green fluorescence (emission maximum at 524 nm) was detected, and the presence of other glycosidases and hydrolases did not produce false-positive signals. The probe was successfully used for imaging of the endogenous beta-Gal activity in cancer and senescent cells, and the imaging results agree with the beta-Gal expression level of the cells, as determined by Western blotting and polymerase chain reaction. Importantly, we demonstrated that upon hydrolysis of galactose, the fluoromethyl-substituted fluorescein derivative is covalently attached to adjacent proteins, both in solution and in live cells. This study offers a small-molecule probe for the sensitive monitoring of endogenous glycosidase activity.