Design, synthesis and evaluation of curcumin-based fluorescent probes to detect Aβ fibrils. Issue 22 (1st December 2018)

• Record Type: Journal Article
• Authors: Sato, Taki; Hotsumi, Mayumi; Makabe, Koki; Konno, Hiroyuki
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 22(2018)
• Page Start: 3520
• Page End: 3525
• Publication Date: 2018-12-01
• Subjects: Alzheimer's disease -- Amyloid β -- Curcumin -- Inhibitor -- Probe; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.10.002
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: Me-CUR is a fluorescent switchable probe to detect amyloid β fibrils with high sensitivity. Me-CUR can be employed as the detecting agent of Aβ fibrils in vitro experiment instead of ThT. Me-CUR has high molecular planarity and thus it could strongly bind with the Aβ fibrils. Abstract: Amyloid β fibrillation is an early event in Alzheimer's disease, so its detection is important to understand its roles in Alzheimer's disease. Curcumin, which has poor water solubility, has been reported to have many pharmacological activities including potent anti-amyloid β fibril activity in Alzheimer's disease. In this study, we found that curcumin analogues with the fluorescence property instead of non-inhibition of amyloid β fibrils. The development of new curcumin analogue, Me-CUR (9 ), as fluorescent switchable probe to detect amyloid β fibrils is described. Me-CUR (9 ) shows excellent fluorescence, especially higher than ThT (4 ), in the presence of amyloid β fibrils. These results suggest that Me-CUR (9 ) can become a useful in vitro amyloid fluorescence sensor for diagnosis of Alzheimer's disease.