Preliminary screening and study of novel flavonoid monoacylglycerol lipase inhibitors

doi:10.3969/j.issn.1674-8115.2018.01.006

›› 2018, Vol. 38 ›› Issue (1): 30-.doi: 10.3969/j.issn.1674-8115.2018.01.006

• Original article (Basic research) • Previous Articles Next Articles

Preliminary screening and study of novel flavonoid monoacylglycerol lipase inhibitors

MA Jia-hui, YANG Ruo-lin, SHEN Zheng-wu#, LIU Jian-hua#

Department of Chemistry, Shanghai Jiao Tong University College of Basic Medical Sciences, Shanghai 200025, China

Online:2018-01-28 Published:2018-03-09
Supported by:
National Natural Science Foundation of China, 81402775; Special Research Fund for Doctoral Programs in Colleges and Universities, 20130073120113

Abstract

Abstract: Objective · To discover and develop novel monoacylglycerol lipase (MAGL) inhibitors. Methods · Computational screening, rational structure analysis and biological assessment was used. Results · A series of natural flavonoid MAGL inhibitors were identified. Compound 9 (quercetin) presented the highest activity with an IC50 value of 36 μmol/L. Conclusion · Several natural flavonoid MAGL inhibitors were identified, which are expected to bring novel hits for discovery of MAGL inhibitors.

Key words: monoacylglycerol lipase, flavonoids, inhibitor

MA Jia-hui, YANG Ruo-lin, SHEN Zheng-wu#, LIU Jian-hua#. Preliminary screening and study of novel flavonoid monoacylglycerol lipase inhibitors[J]. , 2018, 38(1): 30-.

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Preliminary screening and study of novel flavonoid monoacylglycerol lipase inhibitors

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