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Paper | Regular issue | Vol 94, No. 7, 2017, pp.1280-1287
Published online, 7th June, 2017
DOI: 10.3987/COM-17-13733
Inhibitory Activity of Hispidin Derivatives Isolated from Inonotus obliquus on Amyloid β Aggregation

Yukine Aihara, Ayumi Kawaguchi, Mizuho Hanaki, Kazuma Murakami, Kazuhiro Irie, and Hideyuki Shigemori*

*Faculty of Life and Environmental Sciences, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki, 305-8572, Japan

Abstract

Alzheimer’s disease (AD), the most common neurodegenerative disease, is characterized by the aggregation of the 42-mer amyloid β-protein (Aβ42). The inhibition of Aβ aggregation is one of the therapeutic strategies for AD. We recently reported that caffeoylquinic acids and phenylethanoid glycosides possessing two or more catechol moieties strongly inhibit the aggregation of Aβ. We report on the inhibitory effect of hispidin derivatives, which were isolated from Inonotus obliquus, on the aggregation of Aβ42. Hispidin derivatives exhibited anti-aggregation activity in a dose-dependent manner. The structure–activity relation of hispidin derivatives validated that the presence of a catechol moiety is essential for the inhibitory activity.