体外筛选中药胆碱酯酶抑制剂  

Screening of Traditional Chinese Medicine Cholinesterase Inhibitors in vitro

作　　者：郑燕 缪雨静 江媛 冯展 曾铁鑫 张敏 刘德旺[5] 黄林芳[1,2] ZHENG Yan;MIAO Yu-jing;JIANG Yuan(Key Laboratory of Chinese Medicine Resources Conservation,State Administration of Traditional Chinese Medicine of China,Institute of Medicinal Plant Development,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100193;Engineering Research Center of Chinese Medicine Resource,Ministry of Education,Beijing 100193;Dali University,Dali,Yunnan 671000)

机构地区：[1]中国医学科学院北京协和医学院药用植物研究所,国家中医药管理局中药资源保护重点研究室,北京100193 [2]中药资源教育部工程研究中心,北京100193 [3]大理大学,云南大理671000 [4]江西中医药大学,江西南昌330000 [5]内蒙古医科大学,内蒙古呼和浩特010107

出　　处：《安徽农业科学》2022年第6期149-152,共4页Journal of Anhui Agricultural Sciences

基　　金：北京市自然科学基金项目(7202135)。

摘　　要：[目的]从中药中发现新颖的胆碱酯酶抑制剂(ChEI)。[方法]采用4种溶媒从14种中药中提取了56种粗提物,并对14种中药的56种中药提取物进行乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BuChE)抑制活性筛选。[结果]虎杖乙酸乙酯提取物和云木香石油醚提取物表现出AChE和BuChE双重抑制作用,这2种提取物为阿尔兹海默氏症的治疗提供了巨大的潜力。大多数中药乙酸乙酯提取物均显示出较强的BuChE抑制活性。提取物抑制AChE和BuChE的IC_(50)分别为16.00~42.03和11.29~41.92μg/mL。[结论]中药可以作为胆碱酯酶抑制剂的潜在来源。[Objective]To discover a novel cholinesterase inhibitor(ChEI)from traditional Chinese medicine.[Method]56 kinds of crude extracts were extracted from 14 kinds of traditional Chinese medicines using 4 kinds of solvents,and 56 kinds of traditional Chinese medicine extracts from 14 kinds of traditional Chinese medicines were screened for acetylcholinesterase(AChE)and butyrylcholinesterase(BuChE)inhibitory activities.[Result]The ethyl acetate extract of Polygonum cuspidatum and the petroleum ether extract of Carmelia serrata exhibited dual inhibitory effects on AChE and BuChE,and these two extracts provided great potential for the treatment of Alzheimer′s disease.Most of the traditional Chinese medicine ethyl acetate extracts showed strong BuChE inhibitory activity.The IC_(50) of the extracts against AChE and BuChE were 16.00-42.03 and 11.29-41.92μg/mL,respectively.[Conclusion]Traditional Chinese medicine can be a potential source of cholinesterase inhibitors.

关 键 词：胆碱酯酶抑制 阿尔茨海默氏症 中药 体外筛选 

分 类 号：R96[医药卫生—药理学]