Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
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发表时间：
2005
影响因子：
7.3
通讯作者：
M. Ono;N. Yoshida;Kenichi Ishibashi;M. Haratake;Y. Arano;H. Mori;M. Nakayama
中科院分区：
文献类型：
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作者：
M. Ono;N. Yoshida;Kenichi Ishibashi;M. Haratake;Y. Arano;H. Mori;M. Nakayama
脑中β-淀粉样蛋白（A β）肽聚集体的体内成像可能导致阿尔茨海默病（AD）的早期检测和AD治疗进展和有效性的监测。本研究旨在开发以黄酮为核心结构的新型淀粉样蛋白显像剂。设计并合成了放射性碘标记的黄酮衍生物。黄酮衍生物对A β聚集体的结合亲和力从13到77 nM不等。当使用死后AD脑切片进行体外斑块标记时，所有黄酮不仅强烈染色淀粉样斑块，而且还染色脑血管淀粉样蛋白。在使用正常小鼠的生物分布研究中，它们在注射后2分钟显示出3.2至4.1%ID/g的高脑摄取。放射性迅速从脑中洗出（30分钟时为0.5- 1.9%ID/g），这是淀粉样蛋白成像剂非常需要的。这项研究的结果表明，这些类别的放射性碘标记的黄酮可能是有用的候选人作为淀粉样斑块的潜在成像剂。
In vivo imaging of beta-amyloid (A beta) peptide aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of AD treatment. The purpose of this study was to develop novel amyloid imaging agents based on flavone as a core structure. Radioiodinated flavone derivatives were designed and synthesized. The binding affinities of flavone derivatives for A beta aggregates varied from 13 to 77 nM. When in vitro plaque labeling was carried out using post-mortem AD brain sections, all flavones intensely stained not only amyloid plaques but also cerebrovascular amyloids. In biodistribution studies using normal mice, they displayed high brain uptakes ranging from 3.2 to 4.1% ID/g at 2 min postinjection. The radioactivity washed out from the brain rapidly (0.5-1.9% ID/g at 30 min), which is highly desirable for amyloid imaging agents. The results in the study suggest that these classes of radioiodinated flavones may be useful candidates as potential imaging agents for amyloid plaques.