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乙酰胆碱酯酶(AChE)抑制作用:治疗阿尔茨海默病的潜在治疗靶点

Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease.

作者信息

Li Yong, Zhang Xiao-Xiao, Jiang Li-Juan, Yuan Li, Cao Ting-Ting, Li Xia, Dong Lin, Li Ying, Yin Shu-Fan

机构信息

School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.

College of Life Sciences, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.

出版信息

Chem Biol Drug Des. 2015 Oct;86(4):776-82. doi: 10.1111/cbdd.12550. Epub 2015 Mar 28.

Abstract

A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50  = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).

摘要

合成了一系列新的淫羊藿苷衍生物,并对其体外乙酰胆碱酯酶(AChE)抑制活性进行了评估。大多数测试化合物表现出高AChE抑制活性和低毒性,其中化合物1、2和10活性最强(IC50分别为71.52±22.43、8.28±1.45、5.830±1.78 nM)。

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