NWIPB OpenIR
N-salicyloyl tryptamine derivatives as potential therapeutic agents for Alzheimer's disease with neuroprotective effects
Bai, Yinliang; Liu, Dan; Zhang, Honghua; Wang, Yuying; Wang, Degui; Cai, Hongbin; Wen, Huaixiu; Yuan, Guoqiang; An, Hui; Wang, Yali; Shi, Tao; Wang, Zhen
2021
发表期刊BIOORGANIC CHEMISTRY
卷号115
摘要Alzheimer's disease (AD) has become a serious threat to the developed nations with burgeoning patients and annual costs on health care system in modern society. Neuroinflammation, as one of the specific biochemical factors in the progress of neurodegeneration diseases, performs a crucial role in the pathogenesis and development of AD. Therefore, it is of great significance to develop effective anti-neuroinflammatory strategies for the treatment of AD. N-salicyloyl tryptamine derivatives were previously reported and demonstrated that possessed great potential anti-neuroinflammatory effects and favorable blood-brain barrier (BBB) permeation. Herein, a series of novel N-salicyloyl tryptamine derivatives were synthesized and their anti-AD potential was evaluated both in vitro and in vivo. Among them, L7 performed well anti-neuroinflammatory effects and excellent neuroprotective effects, as well as little toxicity. To lucubrate its potential for the treatment of AD, behavior tests including morris water maze (MWM), eight-arm radial maze, open field test and novel object recognition (NOR) test were carried out and the results showed that L7 could remarkably improve A beta-induced cognitive impairment. Moreover, the mechanism of action of L7 on improving A beta-induced AD was preliminarily investigated, and the results uncovered that the neuroprotective effects of L7 was might exerte via intervening A beta-induced pyroptosis through NLRP3-caspase-1-GSDMD axis and ameliorating neuronal apoptosis by mitochondrial apoptosis pathway. Besides, the distribution of A beta plaques in brain tissues were detected by immunohistochemical (IHC) assay and the results indicated that L7 could significantly attenuate the deposition of A beta plaques in the brain.
关键词Alzheimer's disease (AD) N-salicyloyl tryptamine derivatives Neuroprotection Pyroptosis Apoptosis
文献类型期刊论文
条目标识符http://210.75.249.4/handle/363003/60699
专题中国科学院西北高原生物研究所
推荐引用方式
GB/T 7714
Bai, Yinliang,Liu, Dan,Zhang, Honghua,et al. N-salicyloyl tryptamine derivatives as potential therapeutic agents for Alzheimer's disease with neuroprotective effects[J]. BIOORGANIC CHEMISTRY,2021,115.
APA Bai, Yinliang.,Liu, Dan.,Zhang, Honghua.,Wang, Yuying.,Wang, Degui.,...&Wang, Zhen.(2021).N-salicyloyl tryptamine derivatives as potential therapeutic agents for Alzheimer's disease with neuroprotective effects.BIOORGANIC CHEMISTRY,115.
MLA Bai, Yinliang,et al."N-salicyloyl tryptamine derivatives as potential therapeutic agents for Alzheimer's disease with neuroprotective effects".BIOORGANIC CHEMISTRY 115(2021).
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