KMID : 0043320150380111992
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Archives of Pharmacal Research 2015 Volume.38 No. 11 p.1992 ~ p.1998
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Development of fluorescent probes that bind and stain amyloid plaques in Alzheimer¡¯s disease
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Jung Seung-Jin
Park Seung-Hwan Lee Eun-Je Park Jeong-Hoon Kong Young-Bae Rho Jong-Kook Hur Min-Goo Yang Seung-Dae Park Yong-Dae
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Abstract
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¥â-amyloid (A¥â) plaques in the brain are composed of A¥â40 and A¥â42 peptides, and are the defining pathological feature of Alzheimer¡¯s disease (AD). Fluorescent probes that can detect A¥â 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 A¥â42 aggregates, a high affinity for A¥â42 aggregates (KD = 1.59 ¥ìM), and reasonable lipophilicity (log P value = 2.55). Probe 5 also exhibited specific staining of A¥â 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 A¥â plaques. These results suggest that chalcone-mimic probe 5 possessed the requirements of a fluorescent probe for A¥â plaques and may be useful in AD research.
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KEYWORD
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Alzheimer¡¯s disease (AD), A¥â plaques, Fluorescent probe, Chalcone-mimic probes
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