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设计、合成 - 苯乙基肉桂酰胺衍生物及其治疗阿尔茨海默病的生物活性：抗氧化、β-淀粉样蛋白解聚及对记忆缺失的挽救作用。

Design, Synthesis of -phenethyl Cinnamide Derivatives and Their Biological Activities for the Treatment of Alzheimer's Disease: Antioxidant, Beta-amyloid Disaggregating and Rescue Effects on Memory Loss.

机构信息

School of Pharmacy, Lanzhou University, Lanzhou 730000, China.

CAS Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics (LICP), Chinese Academy of Sciences (CAS), Lanzhou 730000, China.

出版信息

Molecules. 2018 Oct 16;23(10):2663. doi: 10.3390/molecules23102663.

DOI:10.3390/molecules23102663
PMID:30332835
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6222358/
Abstract

Gx-50 is a bioactive compound for the treatment of Alzheimer's disease (AD) found in Sichuan pepper (). In order to find a stronger anti-AD lead compound, 20 gx-50 (⁻) 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 ⁻ 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 A, and transgenic model assay for evaluating their rescue effect on memory loss. Finally, compound was determined as a promising anti-AD candidate.

摘要

Gx-50 是一种从四川花椒（）中提取的治疗阿尔茨海默病（AD）的生物活性化合物。为了寻找更强的抗 AD 先导化合物，设计并合成了 20 种 Gx-50（⁻）类似物，根据核磁共振（NMR）和质谱（MS）分析以及与文献数据的比较，确定了它们的分子结构。通过 DPPH 自由基清除实验评估化合物 ⁻ 的抗氧化活性，通过噻唑蓝（ThT）荧光实验评估化合物对 A 的抑制或解聚能力，通过转基因 模型实验评估化合物对记忆丧失的挽救作用，从而评估其抗 AD 潜力。最终，化合物 被确定为有希望的抗 AD 候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/ebe4099d4f85/molecules-23-02663-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/4c48e42a6ae6/molecules-23-02663-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/50d96eaed3af/molecules-23-02663-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/e4e451d8b061/molecules-23-02663-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/ebe4099d4f85/molecules-23-02663-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/4c48e42a6ae6/molecules-23-02663-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/50d96eaed3af/molecules-23-02663-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/e4e451d8b061/molecules-23-02663-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce7c/6222358/ebe4099d4f85/molecules-23-02663-g002.jpg

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