Journal of Shanghai Jiao Tong University (Medical Science) >

2018 , Vol. 38 >Issue 1: 30

DOI: https://doi.org/10.3969/j.issn.1674-8115.2018.01.006

Original article (Basic research)

Preliminary screening and study of novel flavonoid monoacylglycerol lipase inhibitors

  • MA Jia-hui ,
  • YANG Ruo-lin ,
  • SHEN Zheng-wu# ,
  • LIU Jian-hua#
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  • Department of Chemistry, Shanghai Jiao Tong University College of Basic Medical Sciences, Shanghai 200025, China

Online published: 2018-03-09

Supported by

National Natural Science Foundation of China, 81402775; Special Research Fund for Doctoral Programs in Colleges and Universities, 20130073120113

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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

Cite this article

MA Jia-hui , YANG Ruo-lin , SHEN Zheng-wu# , LIU Jian-hua# . Preliminary screening and study of novel flavonoid monoacylglycerol lipase inhibitors[J]. Journal of Shanghai Jiao Tong University (Medical Science), 2018 , 38(1) : 30 . DOI: 10.3969/j.issn.1674-8115.2018.01.006

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