Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease.
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).
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Yong
Y
Li
College of Life Sciences, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Xiao-Xiao
XX
Zhang
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Li-Juan
LJ
Jiang
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Li
L
Yuan
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Ting-Ting
TT
Cao
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Xia
X
Li
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Lin
L
Dong
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Ying
Y
Li
School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, China.
Shu-Fan
SF
Yin
D000110:Acetylcholinesterase / Q000737:chemistry / Q000378:metabolism*; D000544:Alzheimer Disease / Q000188:drug therapy / Q000201:enzymology*; D002460:Cell Line; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology; D034181:Epimedium / Q000737:chemistry; D005419:Flavonoids / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D000110:Acetylcholinesterase; C056599:icariin
AChE inhibition; Alzheimer's disease; derivatives; icariin; synthesis