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Journal Article
Research Support, Non-U.S. Gov't
Synthesis and evolution of neuroprotective effects of oxymatrine derivatives as anti-Alzheimer's disease agents.
Chemical Biology & Drug Design 2021 July
While screening for natural product scaffolds as potential anti-Alzheimer's disease (AD), oxymatrine (OMT) was found to relieve symptoms of AD through diminishing death of neuronal cells caused by microglia-induced inflammation. In this study, 13 derivatives of OMT were synthesized and their neuroprotective effects were evaluated on Aβ1-42 -induced PC12 cells using MTT method. In addition, the best neuroprotective potencies were obtained with compounds 4, 6e, and 6f, which were selected for evaluation of decrease in IL-1β and TNF-α in Aβ1-42 -treated PC12 cells. Collectively, these data reveal that derivatives 6e and 6f possess the best ability of diminish IL-1β production and reverse cell damage in all compounds, which are possible to develop as therapeutic agents for AD.
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