German Center for Neurodegenerative Diseases (DZNE) Rostock, Rostock, Germany.
J Alzheimers Dis. 2012;30(3):651-64. doi: 10.3233/JAD-2012-112168.
The development of early diagnostic and prognostic tools for the visualization of amyloid-β (Aβ) deposits is one important focus of current imaging research. In patients with Alzheimer's disease (AD), non-invasive and efficient detection of soluble and aggregated Aβ is important to determine the immediate success of intervention trails. The novel near infrared-fluorescence (NIRF) probe THK-265 efficiently penetrates the blood-brain barrier and has a strong and efficient binding to cerebral Aβ. Ex vivo microscopy of i) THK-265-labeling of plaques in paraffin-embedded tissue and ii) cerebral cryo-sections after intravenous injection of THK-265 confirmed a systematic increase of the NIRF signal corresponding to Aβ plaque number and size during disease progression. Furthermore, we investigated different stages of plaque formation in amyloid-β protein precursor transgenic mice in vivo after intravenous application of THK-265 to evaluate different aggregation levels with NIRF signals. The intensity of the NIRF signal correlated well with the plaque burden, indicating its utility for direct monitoring of Aβ aggregation progression. In summary, our results support the use of the NIRF probe THK-265 for the diagnosis and direct visualization of amyloid deposits and open the possibility for efficient, pre-symptomatic monitoring of Aβ deposition in the aging brain.
开发用于可视化淀粉样蛋白-β (Aβ) 沉积的早期诊断和预后工具是当前成像研究的一个重要焦点。在阿尔茨海默病(AD)患者中,非侵入性和有效的可溶性和聚集 Aβ 的检测对于确定干预试验的即时成功非常重要。新型近红外荧光(NIRF)探针 THK-265 能够有效地穿透血脑屏障,并且与大脑 Aβ 具有强烈而有效的结合。离体显微镜研究 i)THK-265 标记石蜡包埋组织中的斑块和 ii)THK-265 静脉注射后的脑冷冻切片证实,随着疾病进展,与 Aβ 斑块数量和大小相对应的 NIRF 信号呈系统增加。此外,我们在淀粉样蛋白-β蛋白前体转基因小鼠体内静脉应用 THK-265 后研究了斑块形成的不同阶段,以评估 NIRF 信号与不同的聚集水平。NIRF 信号的强度与斑块负担密切相关,表明其可用于直接监测 Aβ 聚集的进展。总之,我们的结果支持使用 NIRF 探针 THK-265 进行淀粉样蛋白沉积的诊断和直接可视化,并为衰老大脑中 Aβ 沉积的有效、早期无症状监测开辟了可能性。