天然产物研究与开发 ›› 2021, Vol. 33 ›› Issue (5): 892-897.doi: 10.16333/j.1001-6880.2021.5.021

• 综述 • 上一篇    

天然来源的乙酰胆碱酯酶抑制剂的筛选方法综述

薛欣怡,张翼,刘亚月*   

  1. 广东海洋大学食品与科技学院,广东省水产品加工与安全重点实验室,水产品深加工广东普通高等学校重点实验室,湛江市脑健康海洋药物与营养品重点实验室,广东海洋大学海洋药物研究所,湛江 524088

  • 出版日期:2021-05-28 发布日期:2021-06-01
  • 基金资助:
    国家自然科学基金(21807015);广东海洋大学博士启动项目(R18008);深圳市科创委基础研究面上项目(JCYJ20190813105005619);广东省自然科学基金(2018A030307046)

A review of screening methods for acetylcholinesterase inhibitors from natural sources

XUE Xin-yi,ZHANG Yi,LIU Ya-yue*   

  1. 1College of Food and Technology,Guangdong Ocean University,Key Laboratory of Aquatic Product Processing and Safety in Guangdong Province,Key College of Aquatic Product Deep Processing in Guangdong Province Laboratory,Zhanjiang Key Laboratory of Marine Medicine and Nutrition for Brain Health,Institute of Marine Materia Medica,Guangdong Ocean University,Zhanjiang 524088,China

  • Online:2021-05-28 Published:2021-06-01

摘要: 乙酰胆碱酯酶抑制剂是目前临床上用于治疗阿尔茨海默症(AD)的首选药物。随着科学技术的提高,其筛选方法也在不断创新。本文介绍了基于“胆碱酯能损伤学说”的AD治疗靶点的研究及药物研究进展,并对目前可用于乙酰胆碱酯酶抑制剂筛选方法的原理及优缺点进行了重点阐述,主要包括基于紫外分光光度计的Ellmans比色法、薄层生物自显影法、荧光分析法和超高效液相色谱-质谱联用法。总结经验,不断创新,以期能更有效、更快速的从天然产物中筛选出新型的乙酰胆碱酯酶抑制剂。


关键词: 阿尔茨海默症, 乙酰胆碱酯酶抑制剂, 天然产物, 活性筛选模型

Abstract:

Acetylcholinesterase inhibitors are currently the first choice for the clinical treatment of AD.With the improvement of science and technology,the screening methods are also in constant innovation.This article introduced the research progress of AD therapeutic targets and drug research based on the"cholinergic damage theory",and then emphatically expounded the current methods that could be used for acetylcholinesterase inhibitors’screening,which including Ellman's colorimetric method based on ultraviolet spectrophotometer,thin layer biological autoradiography method,fluorescence analysis method,and ultra-high performance liquid chromatography-mass spectrometry combined with their principles and advantages or disadvantages.We hoped that it would be more effectively and quickly to screen new acetylcholinesterase inhibitors from natural products by summarizing the experience and keeping innovating.

Key words: Alzheimer's disease, acetylcholinesterase inhibitors, natural product, activity screening model

中图分类号:  TQ041