Research progress in characterizing multiple-target mechanisms of novel anti-Alzheimer's dimers
10.3969/j.issn.1001-1978.2014.09.005
- VernacularTitle:新型益脑双联体防治阿尔采末病作用及机制研究进展
- Author:
Wei SU
;
Longjun ZHU
;
Daping XU
;
Wei CUI
;
Zaijun ZHANG
;
Shengquan HU
;
Shinghung MAK
;
Yifan HAN
- Publication Type:Journal Article
- Keywords:
Alzheimer's disease;
bis ( n )-Cognitin;
multiple targets;
neuroprotection;
molecular mechanisms;
acetylcholinest-erase;
β-amyloid
- From:
Chinese Pharmacological Bulletin
2014;(9):1201-1204,1205
- CountryChina
- Language:Chinese
-
Abstract:
Alzheimer's disease ( AD ) is a complex disease caused by environmental and genetic factors. Therefore, one-drug-multiple-target compounds represent the most promising pharmacological approaches to preventing and treating this dis-ease. We have previously designed and synthesized bis( n)-Cog-nitin, novel anti-Alzheimer's dimers derived from tacrine. Bis ( n)-Cognitin have been proven to act on multiple important AD targets, including acetylcholinesterase, β-secretase, N-methyl-D-aspartic acid receptor and neuronal nitric oxide synthase, con-currently. Moreover, Bis(n)-Cognitin could inhibit β-amyloid-induced neurotoxicity, decrease glutamate-induced excitotoxici-ty, reduce oxidative stress, improve learning and memory, and protect against neuronal apoptosis in various in vitro and in vivo models, suggesting that bis ( n )-Cognitin are potential anti-AD drug candidates.