Aurones serve as probes of beta-amyloid plaques in Alzheimer's disease.
Biochemical and biophysical research communications 2007 Jul 10; 361(1):116-21
Ono M M, Maya Y Y, Haratake M M, Ito K K, Mori H H, Nakayama M M
Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14
A novel series of aurone derivatives for in vivo imaging of beta-amyloid plaques in the brain of Alzheimer's disease (AD) were synthesized and characterized. When in vitro binding studies using Abeta(1-42) aggregates were carried out with aurone derivatives, they showed high binding affinities for Abeta(1-42) aggregates at the K(i) values ranging from 1.2 to 6.8nM. When in vitro plaque labeling was carried out using double transgenic mice brain sections, the aurone derivatives intensely stained beta-amyiloid plaques. Biodistribution studies in normal mice after i.v. injection of the radioiodinated aurones displayed high brain uptake (1.9-4.6% ID/g at 2min) and rapid clearance from the brain (0.11-0.26% ID/g at 60min), which is highly desirable for amyloid imaging agents. The results in this study suggest that novel radiolabeled aurones may be useful amyloid imaging agents for detecting beta-amyloid plaques in the brain of AD.