Development of fluorescent probes that bind and stain amyloid plaques in Alzheimer’s disease View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2015-11

AUTHORS

Seung-Jin Jung, Seung-Hwan Park, Eun Je Lee, Jeong Hoon Park, Young Bae Kong, Jong Kook Rho, Min Goo Hur, Seung Dae Yang, Yong Dae Park

ABSTRACT

β-amyloid (Aβ) plaques in the brain are composed of Aβ40 and Aβ42 peptides, and are the defining pathological feature of Alzheimer's disease (AD). Fluorescent probes that can detect Aβ plaques have gained increasing interest as potential tools for in vitro and in vivo monitoring of the progression of AD. In this study, chalcone-mimic fluorescent probe 5 was designed and prepared. Probe 5 exhibited an approximately 50-fold increase in emission intensity after mixing with Aβ42 aggregates, a high affinity for Aβ42 aggregates (K D = 1.59 μM), and reasonable lipophilicity (log P value = 2.55). Probe 5 also exhibited specific staining of Aβ plaques in the transgenic mice (APP/PS1) brain sections. Ex vivo fluorescence imaging of the brain from normal and TG mice revealed that probe 5 was able to penetrate the BBB and stain the Aβ plaques. These results suggest that chalcone-mimic probe 5 possessed the requirements of a fluorescent probe for Aβ plaques and may be useful in AD research. More... »

PAGES

1992-1998

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s12272-015-0617-4

DOI

http://dx.doi.org/10.1007/s12272-015-0617-4

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1048931141

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/26012373


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39 schema:description β-amyloid (Aβ) plaques in the brain are composed of Aβ40 and Aβ42 peptides, and are the defining pathological feature of Alzheimer's disease (AD). Fluorescent probes that can detect Aβ plaques have gained increasing interest as potential tools for in vitro and in vivo monitoring of the progression of AD. In this study, chalcone-mimic fluorescent probe 5 was designed and prepared. Probe 5 exhibited an approximately 50-fold increase in emission intensity after mixing with Aβ42 aggregates, a high affinity for Aβ42 aggregates (K D = 1.59 μM), and reasonable lipophilicity (log P value = 2.55). Probe 5 also exhibited specific staining of Aβ plaques in the transgenic mice (APP/PS1) brain sections. Ex vivo fluorescence imaging of the brain from normal and TG mice revealed that probe 5 was able to penetrate the BBB and stain the Aβ plaques. These results suggest that chalcone-mimic probe 5 possessed the requirements of a fluorescent probe for Aβ plaques and may be useful in AD research.
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