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Inhibition of amyloid fibril formation and cytotoxicity by caffeic acid-conjugated amyloid-β C-terminal peptides.

Abstract：

:Amyloid-β (Aβ) deposition and oxidative stress observed in the brains of patients with Alzheimer's disease (AD) are important targets for therapeutic intervention. In this study, we conjugated the antioxidants caffeic acid (CA) and dihydrocaffeic acid (DHCA) to Aβ1-42 C-terminal motifs (Aβx-42: x=38, 40) to synthesize CA-Aβx-42 and DHCA-Aβx-42, respectively. Among the compounds, CA-Aβ38-42 exhibited potent inhibitory activity against Aβ1-42 aggregation and scavenged Aβ1-42-induced intracellular oxidative stress. Moreover, CA-Aβ38-42 significantly protected human neuroblastoma SH-SY5Y cells against Aβ1-42-induced cytotoxicity, with an IC50 of 4μM. These results suggest that CA-Aβ38-42 might be a potential lead for the treatment of AD.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Arai T,Ohno A,Mori K,Kuwata H,Mizuno M,Imai K,Hara S,Shibanuma M,Kurihara M,Miyata N,Nakagawa H,Fukuhara K

doi

10.1016/j.bmcl.2016.10.027

subject

Has Abstract

pub_date

2016-11-15 00:00:00

pages

5468-5471

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)31055-1

journal_volume

26

pub_type

杂志文章

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