Syntheses and neuroprotective effects evolution of oxymatrine derivatives as anti-Alzheimer's disease agents

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 Aβ 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 of IL-1β and TNF-α in Aβ -treated PC12 cells. Collectively, these data reveal that derivatives 6e and 6f possess best ability of diminish IL-1β production and reverse cell damage in all compounds, which are possible to developed as therapeutic agents for AD.