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Bioorg Med Chem Lett. 2014 Jan 15;24(2):552-5. doi: 10.1016/j.bmcl.2013.12.019. Epub 2013 Dec 10.

Colorimetric and fluorometric assays for acetylcholinesterase and its inhibitors screening based on a fluorescein derivate.

Author information

1
State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemistry and Chemical Engineering, Nanjing University of Technology, Nanjing 210009, China.
2
State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemistry and Chemical Engineering, Nanjing University of Technology, Nanjing 210009, China. Electronic address: chenxq@njut.edu.cn.

Abstract

A fluorescein-based sensor was developed for the AChE activity assay and the inhibitor screening. The sensor provided the dual assay methods for the screening of AChE activity in the presence or absence of inhibitor. The colorimetric and fluorometric assays were based on the following processes: (1) owing to the hydrolysis of acetylthiocholine in the presence of AChE, the fluorescein-based probe can rapidly induce 1,4-addition of the hydrolysis product thiocholine to α,β-unsaturated ketone in the compound 1, resulting in strong fluorescence and absorption changes; (2) in the presence of the corresponding inhibitor, the fluorescence enhancement or the absorption change would be inhibited in that the formation of thiocholine was hindered.

KEYWORDS:

AChE activity; Acetylthiocholine; Fluorescein-based sensor; Inhibitor

PMID:
24360998
DOI:
10.1016/j.bmcl.2013.12.019
[Indexed for MEDLINE]
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