Design, synthesis and evaluation of curcumin-based fluorescent probes to detect Aβ fibrils

被引：19

作者：

Sato, Taki ^{[1
]}

Hotsumi, Mayumi ^{[1
]}

Makabe, Koki ^{[1
]}

Konno, Hiroyuki ^{[1
]}

机构：

[1] Yamagata Univ, Grad Sch Sci & Technol, Dept Biol Engn, Yonezawa, Yamagata 9928510, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2018年 / 28卷 / 22期

基金：

日本学术振兴会;

关键词：

Alzheimer's disease; Amyloid beta; Curcumin; Inhibitor; Probe; ALZHEIMERS-DISEASE; MECHANISM; PRODUCTS; MEDICINE; ANALOGS; ASSAY;

D O I：

10.1016/j.bmcl.2018.10.002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amyloid beta 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 beta fibril activity in Alzheimer's disease. In this study, we found that curcumin analogues with the fluorescence property instead of non-inhibition of amyloid beta fibrils. The development of new curcumin analogue, Me-CUR (9), as fluorescent switchable probe to detect amyloid beta fibrils is described. Me-CUR (9) shows excellent fluorescence, especially higher than ThT (4), in the presence of amyloid beta fibrils. These results suggest that Me-CUR (9) can become a useful in vitro amyloid fluorescence sensor for diagnosis of Alzheimer's disease.

引用

页码：3520 / 3525

页数：6

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