Proflavine derivatives as fluorescent imaging agents of amyloid deposits

被引：8

作者：

Garin, Dominique ^{[1
]}

Oukhatar, Fatima ^{[2
,3
]}

Mahon, Andrew B. ^{[4
]}

Try, Andrew C. ^{[4
]}

Dubois-Dauphin, Michel ^{[5
]}

Laferla, Frank M. ^{[6
]}

Demeunynck, Martine ^{[2
,3
]}

Sallanon, Marcelle Moulin ^{[1
]}

Chierici, Sabine ^{[2
,3
]}

机构：

[1] Univ Grenoble 1, INSERM, Unit U877, La Tronche, France

[2] Univ Grenoble 1, Dept Chim Mol, UMR 5250, F-38041 Grenoble 9, France

[3] Univ Grenoble 1, CNRS, ICMG FR 2607, F-38041 Grenoble 9, France

[4] Macquarie Univ, Dept Chem & Biomol Sci, N Ryde, NSW 2109, Australia

[5] Univ Geneva, CMU, Dept Pathol & Immunol, Geneva 4, Switzerland

[6] Univ Calif Irvine, Inst Memory Impairments & Neurol Disorders, Irvine, CA USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 08期

关键词：

Proflavine; Click chemistry; Fluorescent markers; Amyloid deposits imaging; ALZHEIMERS-DISEASE; LIPOIC ACID; IN-VIVO; BETA; CURCUMIN; FIBRILS; PLAQUES;

D O I：

10.1016/j.bmcl.2011.03.010

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A series of proflavine derivatives for use to further image A beta amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23 months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on A beta(40) fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new A beta imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2203 / 2206

页数：4

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