A direct assay of butyrylcholinesterase activity using a fluorescent substrate

被引:27
作者
Kang, Seungyoon [1 ]
Lee, Suji [1 ]
Yang, Woojin [1 ]
Seo, Jiwon [1 ]
Han, Min Su [1 ]
机构
[1] Gwangju Inst Sci & Technol, Dept Chem, 123 Cheomdangwagi Ro, Gwangju 61005, South Korea
关键词
ACETYLCHOLINESTERASE; INHIBITOR; GLUCOSE; CPT-11;
D O I
10.1039/c6ob01360k
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In this study, we report a direct fluorometric assay for butyrylcholinesterase (BChE) activity and screening of its inhibitor, using a fluorescent substrate. 2-(2-(5,6-Dimethoxy-1,3-dioxoisoindolin-2-yl) acetoxy)N, N, N-trimethylethan-1-ammonium iodide (1) was hydrolyzed by BChE, and its fluorescence was quenched by an intramolecular photoinduced electron transfer process. The resulting change in fluorescence provided a facile method for real-time BChE activity testing. Remarkably, 1 was selectively hydrolyzed by BChE, even in the presence of excess acetylcholinesterase, thereby facilitating the specific monitoring of BChE activity. This assay method is also useful for screening potential BChE inhibitors. Given its simplicity, selectivity, and higher assay speed, this method may be extended to high-throughput screening of BChE inhibitors and relevant drug discovery.
引用
收藏
页码:8815 / 8820
页数:6
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