A highly selective fluorescent ESIPT probe for the detection of Human carboxylesterase 2 and its biological applications

被引：104

作者：

Feng, Lei ^{[1
,2
]}

Liu, Zhao-Ming ^{[2
]}

Hou, Jie ^{[3
]}

Lv, Xia ^{[2
]}

Ning, Jing ^{[2
,3
]}

Ge, Guang-Bo ^{[1
,2
]}

Cui, Jing-Nan ^{[1
]}

Yang, Ling ^{[2
]}

机构：

[1] Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116024, Peoples R China

[2] Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

[3] Dalian Med Univ, Dalian 116044, Peoples R China

来源：

BIOSENSORS & BIOELECTRONICS | 2015年 / 65卷

基金：

中国国家自然科学基金;

关键词：

Human carboxylesterase 2; Ratiometric fluorescent probe; 3-Hydroxylflavone; Bioimaging; MAMMALIAN CARBOXYLESTERASES; CATALYTIC-PROPERTIES; HYDROGEN-SULFIDE; TUMOR-TISSUE; LIVING CELLS; ACTIVATION; IRINOTECAN; PRODRUG; CPT-11; SENSITIVITY;

D O I：

10.1016/j.bios.2014.10.002

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

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.

引用

页码：9 / 15

页数：7

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