一种用于阿尔茨海默病中β-淀粉样斑块近红外成像的半花菁衍生物。
A hemicyanine derivative for near-infrared imaging of β-amyloid plaques in Alzheimer's disease.
机构信息
Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China; School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
出版信息
Eur J Med Chem. 2019 Oct 1;179:736-743. doi: 10.1016/j.ejmech.2019.07.005. Epub 2019 Jul 2.
The formation of amyloid-β (Aβ) plaques in the brain is one of the main pathological features of Alzheimer's disease (AD). The imaging probes, capable of detecting Aβ deposition, are important tools for early diagnosis of AD. In this article, we designed, synthesized and evaluated a cyanine-based near-infrared fluorescence (NIRF) probe ZT-1 for the detection of Aβ deposits in the brain. The probe had excellent fluorescent properties with an emission maximum above 720 nm upon binding to Aβ aggregates with affinity of 445.0 nM (K). Furthermore, ZT-1 exhibited good biostability, photostability, and binding selectivity toward Aβ aggregates by in vitro fluorescence staining experiments. In vivo NIRF imaging result also revealed that our probe could efficiently differentiate transgenic and wild-type mice. All these studies indicated that ZT-1 is a promising fluorescent probe for Aβ plaques in the AD brains.
淀粉样蛋白-β（Aβ）斑块在大脑中的形成是阿尔茨海默病（AD）的主要病理特征之一。能够检测 Aβ 沉积的成像探针是 AD 早期诊断的重要工具。在本文中，我们设计、合成并评价了一种基于菁染料的近红外荧光（NIRF）探针 ZT-1，用于检测大脑中的 Aβ 沉积物。该探针与 Aβ 聚集物结合后具有出色的荧光特性，其发射最大值超过 720nm，对 Aβ 聚集物的亲和力为 445.0nM（K）。此外，通过体外荧光染色实验，ZT-1 表现出良好的生物稳定性、光稳定性和对 Aβ 聚集物的结合选择性。体内 NIRF 成像结果也表明，我们的探针可以有效地区分转基因和野生型小鼠。所有这些研究表明，ZT-1 是一种有前途的 AD 脑内 Aβ 斑块荧光探针。
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