| 王芳,臧小豪,周渭.化学通报,2026,89(6):717-726. |
| 尼罗蓝类靶向TSPO的神经炎症近红外荧光分子探针的研究 |
| Study on Near-infrared Fluorescent Molecular Probes with Nile Blue Targeted to TSPO |
| 投稿时间：2025-12-11 修订日期：2026-01-14 |
| DOI： |
| 中文关键词: 神经炎性 近红外荧光成像探针 TSPO 尼罗蓝 |
| 英文关键词:Neuroinflammation, near-infrared fluorescence imaging probe, TSPO, Nile blue fluorophore |
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| 摘要点击次数: 30 |
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| 中文摘要: |
| 神经炎症在阿尔茨海默病、帕金森病等中枢神经系统退行性疾病中发挥关键作用，其早期诊断对疾病干预至关重要。在神经炎症标志性蛋白中，转运蛋白18 kDa（TSPO）的研究最为广泛深入。近红外荧光成像凭借操作简便、组织穿透性强，以及背景干扰小等优势，在活体检测应用方面展现出极大潜力。尼罗蓝作为噁嗪类荧光染料，因具有细胞毒性低、生物相容性好等优点作为理想的荧光团广泛应用于生物成像。本研究以TSPO为靶点，采用异喹啉类、吲哚乙酰胺类和喹唑啉类这三种具有靶向识别功能的基团，引入尼罗蓝荧光团，合成了三种探针（ZXH-01、ZXH-02、ZXH-03），完成合成、表征与性能评估。结果表明：探针ZXH-01光学特性良好，与TSPO高特异性结合。该探针的荧光信号强度会随神经炎症程度变化而相应改变，两者呈正相关关系。综合评价，ZXH-01具备发展为为神经炎症检测试剂的潜力，为神经炎症及相关神经退行性疾病的可视化检测提供了新策略。 |
| 英文摘要: |
| Neuroinflammation plays a pivotal role in central nervous system degenerative diseases such as Alzheimer"s disease and Parkinson"s disease, making its early diagnosis crucial for disease intervention. Among neuroinflammatory biomarker proteins, the 18 kDa translocator protein (TSPO) has been the most extensively studied. Near-infrared fluorescence imaging demonstrates significant potential for in vivo detection applications due to its operational simplicity, strong tissue penetration, and minimal background interference. Nile blue, as an oxazine fluorescent dye, has emerged as an ideal fluorophore owing to its low cytotoxicity and excellent biocompatibility. This study synthesized three probes (ZXH-01, ZXH-02, ZXH-03) targeting TSPO by incorporating the Nile blue fluorophore and conjugating it with three distinct recognition moieties: isoquinoline, indoleacetamide, and quinazoline derivatives. The design, synthesis, and performance evaluation of these probes were systematically investigated. Results demonstrate that probe ZXH-01 exhibits favorable optical properties and high specificity for TSPO binding. Its fluorescence signal intensity shows positive correlation with neuroinflammatory severity. These characteristics indicate ZXH-01"s potential as a neuroinflammation detection reagent, providing a novel strategy for visualizing neuroinflammation and related neurodegenerative diseases. |
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