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 (1–20) 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 1–20 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.
Highlights
Alzheimer’s disease (AD) is a neurodegenerative disorder that mainly occurs in the elderly.It is characterized by intelligence decline and memory loss, as well as changes in emotions and personality [1]
Oxidative stress plays an important role in the development and progress of AD, and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay is one of the most common methods to evaluate the anti-oxidative activity of compounds [8,9]
The synthesis of the gx-50 derivatives is described in Schemes 1 and 2
Summary
Alzheimer’s disease (AD) is a neurodegenerative disorder that mainly occurs in the elderly. It is characterized by intelligence decline and memory loss, as well as changes in emotions and personality [1]. N-methyl-D-aspartate (NMDA) receptor antagonist, that is memantine. These drugs could alleviate cognitive symptoms in this disease. Oxidative stress plays an important role in the development and progress of AD, and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay is one of the most common methods to evaluate the anti-oxidative activity of compounds [8,9]. The DPPH assay and thioflavin T (ThT) assay were employed to evaluate their anti-oxidative activity and their inhibition and disaggregation on Aβ aggregation. We will report the design, synthesis, and anti-AD bioactivity of these gx-50 derivatives
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