Rhizolutin, a Novel 7/10/6-Tricyclic Dilactone, Dissociates Misfolded Protein Aggregates and Reduces Apoptosis/Inflammation Associated with Alzheimer's Disease

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26
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31

초록

Rhizolutin (1) was discovered as a natural product of ginseng-rhizosphericStreptomycessp. WON17. Its structure features an unprecedented 7/10/6-tricyclic dilactone carbon skeleton composed of dimethylcyclodecatriene flanked by a 7-membered and a 6-membered lactone ring based on spectroscopic analysis. During an unbiased screening of natural product libraries, this novel compound was found to dissociate amyloid-beta (A beta) plaques and tau tangles, which are key pathological hallmarks of Alzheimer's disease (AD). Rhizolutin treatment of APP/PS1 double transgenic mice with AD significantly dissociated hippocampal plaques. In vitro, rhizolutin substantially decreased A beta-induced apoptosis and inflammation in neuronal and glial cells. Our findings introduce a unique chemical entity that targets A beta and tau concurrently by mimicking misfolded protein clearance mechanisms of immunotherapy, which is prominently investigated in clinical trials.

키워드

Alzheimer's diseaseamyloid betalactonesnatural productstau proteinTHERMOCHEMISTRY
제목
Rhizolutin, a Novel 7/10/6-Tricyclic Dilactone, Dissociates Misfolded Protein Aggregates and Reduces Apoptosis/Inflammation Associated with Alzheimer's Disease
저자
Kwon, YunShin, JisuNam, KwanghoAn, Joon SooYang, Seung-HoonHong, Seong-HeonBae, MunhyungMoon, KyuhoCho, YakdolWoo, JiwanPark, KeunwanKim, KyeonghwanShin, JongheonKim, Byung-YongKim, YoungSooOh, Dong-Chan
DOI
10.1002/anie.202009294
발행일
2020-12-14
유형
Article
저널명
Angewandte Chemie - International Edition
59
51
페이지
22994 ~ 22998