论著(基础研究)

单酰基甘油脂肪酶的新型黄酮类化合物抑制剂的初步筛选及研究

  • 马佳慧 ,
  • 杨若林 ,
  • 沈征武# ,
  • 刘坚华#
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  • 上海交通大学 基础医学院化学教研室,上海200025
马佳慧 ( 1992— ),女,硕士生;电子信箱:judith199212@sjtu.edu.cn。

网络出版日期: 2018-03-09

基金资助

国家自然科学基金(81402775);高等学校博士学科点专项科研基金(20130073120113)

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

摘要

目的· 寻找新型(结构新、靶点新)单酰基甘油脂肪酶(monoacylglycerol lipase,MAGL)抑制剂。方法· 运用计算机辅助虚
拟筛选手段,通过合理的结构分析,再结合生物学评估的方法进行筛选。结果· 发现一系列天然黄酮类MAGL 抑制剂。其中化合物9
(槲皮素)对MAGL 的抑制活性最好,IC50 值达到了36 μmol/L。结论· 成功发现了一系列天然的黄酮类MAGL 抑制剂,有望为发现
新型的MAGL 抑制剂提供新的结构类型。

本文引用格式

马佳慧 , 杨若林 , 沈征武# , 刘坚华# . 单酰基甘油脂肪酶的新型黄酮类化合物抑制剂的初步筛选及研究[J]. 上海交通大学学报(医学版), 2018 , 38(1) : 30 . DOI: 10.3969/j.issn.1674-8115.2018.01.006

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.
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