功能性D和L纳夫他林二胺:微波驱动合成,超分子聚合和多光子光终身成像显微镜在活细胞中
Simone G Giuffrida1, David G Calatayud2, Fernando Cortezon-Tamarit1
1Department of Chemistry, University of Bath, Claverton Down, Bath BA2 7AY, U.K.
ACS bio & med chem Au
|December 22, 2025
概括
我们开发了新的联光学成像探针,使用bombesin碎片向癌细胞. 奇拉性显著影响探针吸收和定位,为癌症生物标志物检测和成像提供了新的途径.
科学领域:
- 生物结合化学 生物结合化学
- 光学成像探测器 探测器
- 分子成像学分子成像学
背景情况:
- 胃蛋白释放受体 (GRPR) 是癌细胞中的一个标.
- 在设计有效的成像探头时,奇拉性至关重要.
- 纳夫他二胺 (NDI) 和BODIPY是有用的光标签.
研究的目的:
- 合成和评估新型联光学成像探头,其中包括L-[7,13] bombesin片段 (L-[7,13]-BBN).
- 为了研究性 (L-vs. D-氨基酸) 对探针特性和细胞行为的影响.
- 为这些生物结合物开发微波辅助合成方法.
主要方法:
- 基于NDI的单和双联体的微波辅助合成.
- 使用NMR,光谱学,质谱学,SEM和TCSPC进行表征.
- 使用共聚焦显微镜和MP FLIM在PC-3和A431细胞中的细胞吸收和局部化研究.
主要成果:
- 成功合成和描述了具有可调节光谱和水溶性的新型L-[7,13]-BBN结合的NDI探针.
- 展示了依赖于立体化学的自我组装和聚合行为.
- 观察到不同的细胞吸收和溶酶体局部化L-vs. D-立体异构体;BODIPY含有探针局部化到内分泌网膜.
结论:
- L-[7,13]-BBN片段的性对于调节探头吸收和亚细胞局部化至关重要.
- 开发的探针是无毒的,适合活细胞成像.
- 这些发现为设计用于癌症生物标志物成像的向配体提供了基础.
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