A novel drug candidate for Alzheimer's disease treatment: gx-50 derived from Zanthoxylum bungeanum.
作者： Maoping Tang , Zhaoxia Wang , Ying Zhou , Wangjie Xu , Shengtian Li
DOI: 10.3233/JAD-121831
关键词:
摘要: This study focused on a promising drug candidate, N-[2-(3,4-dimethoxyphenyl)ethyl]-3-phenyl-acrylamide (gx-50), compound extracted from Sichuan pepper (Zanthoxylum Bungeanum), to determine whether it would be an effective therapeutic for Alzheimer's disease (AD) via biological experiments. In vivo, we determined the pharmacokinetic profile of gx-50 and evaluated effect cognitive abilities amyloid-β protein precursor transgenic (AβPP-Tg) mice by Morris water maze testing. addition, examined effects (Aβ) oligomers in brains AβPP-Tg immunohistochemistry. vitro, observed direct Aβ atomic force microscopy, detected neuroprotective western blotting cell apoptosis assays, measured its intracellular calcium currents laser confocal microscopy. Experiments vivo showed that could penetrate blood brain barrier improve mice. Moreover, treatment decreased accumulation cerebral cortex. The results vitro demonstrated disassemble oligomers, inhibit Aβ-induced neuronal apoptotic gene expression, reduce toxicity. These strongly suggest is potential candidate treating AD.
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