基甘向标 [F]3,3,3-三-d-alanine 标记剂用于成像细菌感染
Alexandre M Sorlin1, Marina López-Álvarez1, Jacob Biboy2
1Department of Radiology, Biomedical Imaging University of California, San Francisco, San Francisco, California 94158, United States.
JACS Au
|April 1, 2024
概括
一种新的PET标记物,d-[18F]-CF3-ala,在细菌中显示出高积累,特别是大肠杆菌. 这种辐射追踪器显示出特定细菌感染的潜力,可用低背景信号进行成像.
科学领域:
- 核医学就是核医学.
- 放射化学 放射化学是指辐射化学.
- 微生物学 微生物学
- 感染成像 感染成像
背景情况:
- 目前用于细菌感染的成像技术缺乏病原体特异性.
- 针对细菌代谢的正子发射断层扫描 (PET) 追踪剂正在开发中.
- 以前的d-氨基酸衍生PET标记剂显示细菌积累,但需要优化用于临床使用.
研究的目的:
- 开发一种用-18标记的PET追踪剂,d-[18F]-CF3-ala,用于细菌感染成像.
- 评估d-[18F]-CF3-ala. 的稳定性,新陈代谢和细菌的结合.
- 评估d-[18F]-CF3-ala在检测细菌感染中的体外和体内性能.
主要方法:
- -19母化合物d-[19F]-CF3-ala的合成和表征.
- 对d-氨基酸氧化酶的血清稳定性和敏感性的评估.
- 使用HPLC/质谱测量对*Escherichia coli*中丁糖的结合的评估.
- 对d-[18F]-CF3-ala和*in vitro*细菌积累研究的放射合成.
- 在急性细菌感染的小鼠模型中的体内成像研究.
主要成果:
- 基因化合物d-[19F]-CF3-ala在血清中稳定,并且通过d-氨基酸氧化酶代谢不良.
- d-[19F]-CF3-ala在大肠杆菌中被强有力的纳入. peptidoglycan.
- d-[18F]-CF3-ala在格拉姆阴性病原体,特别是大肠杆菌中显示出优先积累.
- 在体内研究成功地区分了热杀死的大肠杆菌和低背景信号的热杀死大肠杆菌.
结论:
- d-[18F]-CF3-ala是用于细菌感染成像的有前途的PET追踪剂.
- [18F]修改的d-氨基酸方法为细菌代谢提供了更好的特异性.
- 这种追踪剂有可能提高细菌感染的检测和监测.
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