Novel chalcones as probes for in vivo imaging of β-amyloid plaques in Alzheimer's brains
Novel chalcones as probes for in vivo imaging of β-amyloid plaques in Alzheimer's brains
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DOI：
10.1016/j.bmc.2007.07.052
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发表时间：
2007-11-01
影响因子：
3.5
通讯作者：
Nakayama, Morio
中科院分区：
文献类型：
--
作者：
Ono, Masahiro;Haratake, Mamoru;Nakayama, Morio
合成并表征了一系列新的查尔酮衍生物，用于阿尔茨海默病（AD）脑中β-淀粉样斑块的体内成像。当使用A β聚集体与查耳酮衍生物进行体外结合研究时，A聚集体的结合亲和力在3至105 nM之间变化。以三丁基锡衍生物为原料，过氧化氢为氧化剂，通过碘脱锡反应，成功地制备了高收率、高放化纯度的碘标记查尔酮。静脉注射放射性碘标记的查耳酮后，在正常小鼠中的生物分布研究显示高脑摄取（2分钟时为2.0-4.7%ID/g）和从脑中快速清除（30分钟时为0.2-0.6%ID/g），这是非常理想的淀粉样蛋白成像剂。本研究的结果表明，新的放射性碘标记的查耳酮可能是有用的淀粉样蛋白成像剂，用于检测AD脑中的P-淀粉样蛋白斑块。(C)2007爱思唯尔有限公司保留所有权利。
A novel series of chalcone derivatives for in vivo imaging beta-amyloid plaques in the brain of Alzheimer's disease (AD) were synthesized and characterized. When in vitro binding studies using A beta aggregates were carried out with chalcone derivatives, the binding affinities for A aggregate varied from 3 to 105 nM. The radioiodinated chalcones were successfully prepared through an iododestannylation reaction from the corresponding tributyltin derivatives using hydrogen peroxide as the oxidant in high yields and with high radiochemical purities. Biodistribution studies in normal mice after iv injection of the radioiodinated chalcones displayed high brain uptake (2.0-4.7%ID/g at 2 min) and rapid clearance from the brain (0.2-0.6%ID/g at 30 min), which is highly desirable or amyloid imaging agents. The results in this study suggest that the novel radioiodinated chalcones may be useful amyloid imaging agents for detecting P-amyloid plaques in the brain of AD. (C) 2007 Elsevier Ltd. All rights reserved.