Design, Synthesis of N-phenethyl Cinnamide Derivatives and Their Biological Activities for the Treatment of Alzheimer’s Disease: Antioxidant, Beta-amyloid Disaggregating and Rescue Effects on Memory l
Department中科院西北特色植物资源化学重点实验室/甘肃省天然药物重点实验室
Tian Chai1; Xiao-Bo Zhao2; Wei-Feng Wang2; Yin Qiang1; Xiao-Yun Zhang1; Jun-Li Yang2
2018
Source PublicationMolecules
Volume23Issue:10Pages:2663
Abstract

Gx-50 is a bioactive compound for the treatment of Alzheimer’s disease (AD) found in Sichuan pepper (Zanthoxylum bungeanum). In order to find a stronger anti-AD lead compound, 20 gx-50 (120) analogs have been designed and synthesized, and their molecular structures were determined based on nuclear magnetic resonance (NMR) and mass spectrometry (MS) analysis, as well as comparison with literature data. Compounds 120 were evaluated for their anti-AD potential by using DPPH radical scavenging assay for considering their anti-oxidant activity, thioflavin T (ThT) fluorescence assay for considering the inhibitory or disaggregate potency of Aβ, and transgenic Drosophila model assay for evaluating their rescue effect on memory loss. Finally, compound 13 was determined as a promising anti-AD candidate.

KeywordAlzheimer’s Disease Gx-50 Dpph Assay Tht Assay Transgenic Drosophila Model Assay
MOST Discipline Catalogue理学::化学
DOI10.3390/molecules23102663
If3.098
Language英语
compositor第二作者单位
Citation statistics
Cited Times:8[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.licp.cn/handle/362003/24247
Collection中科院西北特色植物资源化学重点实验室/甘肃省天然药物重点实验室
Corresponding AuthorJun-Li Yang
Affiliation1.Lanzhou University
2.Lanzhou Institute of Chemical Physics (LICP), Chinese Academy of Sciences (CAS)
Recommended Citation
GB/T 7714
Tian Chai,Xiao-Bo Zhao,Wei-Feng Wang,等. Design, Synthesis of N-phenethyl Cinnamide Derivatives and Their Biological Activities for the Treatment of Alzheimer’s Disease: Antioxidant, Beta-amyloid Disaggregating and Rescue Effects on Memory l[J]. Molecules,2018,23(10):2663.
APA Tian Chai,Xiao-Bo Zhao,Wei-Feng Wang,Yin Qiang,Xiao-Yun Zhang,&Jun-Li Yang.(2018).Design, Synthesis of N-phenethyl Cinnamide Derivatives and Their Biological Activities for the Treatment of Alzheimer’s Disease: Antioxidant, Beta-amyloid Disaggregating and Rescue Effects on Memory l.Molecules,23(10),2663.
MLA Tian Chai,et al."Design, Synthesis of N-phenethyl Cinnamide Derivatives and Their Biological Activities for the Treatment of Alzheimer’s Disease: Antioxidant, Beta-amyloid Disaggregating and Rescue Effects on Memory l".Molecules 23.10(2018):2663.
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