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。
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.
作者
薛欣怡
张翼
刘亚月
XUE Xin-yi;ZHANG Yi;LIU Ya-yue(College 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 ProvinceLaboratory,Zhanjiang Key Laboratory of Marine Medicine and Nutrition for Brain Health,Institute of Marine Materia Medica,Guangdong Ocean University,Zhanjiang 524088,China)
出处
《天然产物研究与开发》
CAS
CSCD
2021年第5期892-897,867,共7页
Natural Product Research and Development
基金
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)。
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
Alzheimer's disease
acetylcholinesterase inhibitors
natural product
activity screening model