title: Development of fluorescent probes that bind and stain amyloid plaques in Alzheimer's disease.
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.
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Seung-Jin
authors.initials: SJ
authors.lastname: Jung
authors.affiliation: Department of Nuclear Medicine, Chonnam National University Hwasun Hospital, Hwasun, Republic of Korea.
authors.forename: Seung-Hwan
authors.initials: SH
authors.lastname: Park
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Eun Je
authors.initials: EJ
authors.lastname: Lee
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Jeong Hoon
authors.initials: JH
authors.lastname: Park
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Young Bae
authors.initials: YB
authors.lastname: Kong
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Jong Kook
authors.initials: JK
authors.lastname: Rho
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Min Goo
authors.initials: MG
authors.lastname: Hur
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea.
authors.forename: Seung Dae
authors.initials: SD
authors.lastname: Yang
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup, 580-185, Republic of Korea. ydpark@kaeri.re.kr.|Department of Nuclear Medicine, Chonnam National University Hwasun Hospital, Hwasun, Republic of Korea. ydpark@kaeri.re.kr.
authors.forename: Yong Dae
authors.initials: YD
authors.lastname: Park
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis* / Q000473:pathology; D016229:Amyloid beta-Peptides / Q000032:analysis*; D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism; D001921:Brain / Q000473:pathology; D047188:Chalcones / Q000737:chemistry; D004195:Disease Models, Animal; D018450:Disease Progression; D005260:Female; D005456:Fluorescent Dyes / Q000737:chemistry*; D051379:Mice; D008822:Mice, Transgenic; D010446:Peptide Fragments / Q000032:analysis*; D058225:Plaque, Amyloid / Q000175:diagnosis* / Q000473:pathology
chemical_list: D016229:Amyloid beta-Peptides; D047188:Chalcones; D005456:Fluorescent Dyes; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42)
keywords: Alzheimer’s disease (AD); Aβ plaques; Chalcone-mimic probes; Fluorescent probe