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首页> 美国卫生研究院文献>other >The Diarylheptanoid (+)-aR11S-Myricanol and Two Flavones from Bayberry (Myrica cerifera) Destabilize the Microtubule Associated Protein Tau
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The Diarylheptanoid (+)-aR11S-Myricanol and Two Flavones from Bayberry (Myrica cerifera) Destabilize the Microtubule Associated Protein Tau

机译：该二芳基庚（+） - aR从杨梅11s-myricanol和双黄酮（蜡果杨梅）叫板微管相关蛋白头

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Target-based drug discovery for Alzheimer's disease (AD) centered on modulation of the amyloid ß peptide has met with limited success. Therefore, recent efforts have focused on targeting the microtubule-associated protein tau. Tau pathologically accumulates in more than 15 neurodegenerative diseases and is most closely linked with post-symptomatic progression in AD. We endeavored to identify compounds that decrease tau stability rather than prevent its aggregation. An extract from Myrica cerifera (bayberry/southern wax myrtle) potently reduced both endogenous and over-expressed tau protein levels in cells and murine brain slices. The bayberry flavonoids myricetin and myricitrin were confirmed to contribute to this potency but a diarylheptanoid, myricanol, was the most effective anti-tau component in the extract with potency approaching the best targeted lead therapies. (+)-aR,11S-myricanol, isolated from M. cerifera and reported here for the first time as the naturally occurring aglycone, was significantly more potent than commercially available (±)-myricanol. Myricanol may represent a novel scaffold for drug development efforts targeting tau turnover in AD.

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