Journal
BIOSENSORS & BIOELECTRONICS
Volume 65, Issue -, Pages 9-15Publisher
ELSEVIER ADVANCED TECHNOLOGY
DOI: 10.1016/j.bios.2014.10.002
Keywords
Human carboxylesterase 2; Ratiometric fluorescent probe; 3-Hydroxylflavone; Bioimaging
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Funding
- National S&T Major Projects of China [2012ZX09501001, 2012ZX09506001]
- National Basic Research Program of China [2013CB531800]
- National Natural Science Foundation of China [81473181, 81273590, 81302793]
- State Key Laboratory of Fine Chemicals [KF1304]
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A new ratiometric florescence probe derived from 3-hydroxyflavone (3-HF) has been developed for selective and sensitive detection of human carboxylesterase 2 (CE2). The probe is designed by modulating the excited state intramolecular proton transfer (ESIPT) emission of 3-HF via introducing of 4-ethylbenzoyloxy group. Under physiological conditions, probe 1 displays satisfying stability with very low background signal, but it can be selectively hydrolyzed by CE2 to release free 3-HF which brings remarkable changes in fluorescence spectrum. Both reaction phenotyping and chemical inhibition assays demonstrate that probe 1 is highly selective for CE2 over other human hydrolases including carboxylesterase 1, cholinesterases and paraoxonases. Probe 1 has been applied successfully to measure the real activities of CE2 in human biological samples, as well as to screen CE2 inhibitors by using tissue preparations as the enzymes sources. Additionally, probe 1 is cell membrane permeable and can be used for cellular imaging of endogenous CE2 in living cells. All of these features make it possible to serve as a promising tool for exploring the individual differences in biological function of CE2, as well as for rapid screening of selective and potent inhibitors of CE2 for further clinical use. (C) 2014 Elsevier B.V. All rights reserved.
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