Proflavine derivatives as fluorescent imaging agents of amyloid deposits

Dominique Garin; Fatima Oukhatar; Andrew B. Mahon; Andrew C. Try; Michel Dubois-Dauphin; Frank M. Laferla; Martine Demeunynck; Marcelle Moulin Sallanon; Sabine Chierici

doi:10.1016/j.bmcl.2011.03.010

Proflavine derivatives as fluorescent imaging agents of amyloid deposits

Dominique Garin, Fatima Oukhatar, Andrew B. Mahon, Andrew C. Try, Michel Dubois-Dauphin, Frank M. Laferla, Martine Demeunynck, Marcelle Moulin Sallanon, Sabine Chierici

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

A series of proflavine derivatives for use to further image Aβ 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 Aβ₄₀ fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.

Original language	English
Pages (from-to)	2203-2206
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2011.03.010
Publication status	Published - 15 Apr 2011

Keywords

proflavine
click chemistry
fluorescent markers
amyloid deposits imaging

Access to Document

10.1016/j.bmcl.2011.03.010

Cite this

@article{13391242d1824a9eabda2a22680d1323,

title = "Proflavine derivatives as fluorescent imaging agents of amyloid deposits",

abstract = "A series of proflavine derivatives for use to further image Aβ 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 Aβ40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.",

keywords = "proflavine, click chemistry, fluorescent markers, amyloid deposits imaging",

author = "Dominique Garin and Fatima Oukhatar and Mahon, \{Andrew B.\} and Try, \{Andrew C.\} and Michel Dubois-Dauphin and Laferla, \{Frank M.\} and Martine Demeunynck and Sallanon, \{Marcelle Moulin\} and Sabine Chierici",

year = "2011",

month = apr,

day = "15",

doi = "10.1016/j.bmcl.2011.03.010",

language = "English",

volume = "21",

pages = "2203--2206",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier",

number = "8",

}

TY - JOUR

T1 - Proflavine derivatives as fluorescent imaging agents of amyloid deposits

AU - Garin, Dominique

AU - Oukhatar, Fatima

AU - Mahon, Andrew B.

AU - Try, Andrew C.

AU - Dubois-Dauphin, Michel

AU - Laferla, Frank M.

AU - Demeunynck, Martine

AU - Sallanon, Marcelle Moulin

AU - Chierici, Sabine

PY - 2011/4/15

Y1 - 2011/4/15

N2 - A series of proflavine derivatives for use to further image Aβ 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 Aβ40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.

AB - A series of proflavine derivatives for use to further image Aβ 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 Aβ40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.

KW - proflavine

KW - click chemistry

KW - fluorescent markers

KW - amyloid deposits imaging

UR - https://www.scopus.com/pages/publications/79953290815

U2 - 10.1016/j.bmcl.2011.03.010

DO - 10.1016/j.bmcl.2011.03.010

M3 - Article

C2 - 21435875

AN - SCOPUS:79953290815

SN - 0960-894X

VL - 21

SP - 2203

EP - 2206

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Proflavine derivatives as fluorescent imaging agents of amyloid deposits

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this