乙基化物和乙基化物作为高性能化学物质交换和转移MRI对比剂
Shaowei Bo1, Dong Zhang2, Mengjie Ma2
1Department of Medical Imaging, The Affiliated Guangdong Second Provincial General Hospital of Jinan University, Guangzhou 510317, China.
Pharmaceuticals (Basel, Switzerland)
|May 27, 2023
概括
新的二磁CEST (diaCEST) 剂,包括乙烯基化物和乙烯基化物,为增强的MRI对比提供了改进的化学转移. 亚酸二化物 (ADH) 在小鼠模型中展示了瘤可视化,扩大了癌症成像的选择.
科学领域:
- 生物医学成像技术 生物医学成像技术
- 化学生物学 化学生物学
- 分子成像学分子成像学
背景情况:
- 化学交换和转移 (CEST) MRI是一种有前途的分子成像技术.
- 电磁CEST (diaCEST) 剂提供生物相容性,但由于微小的化学变化,通常具有有限的敏感性.
- 扩大diaCEST剂的范围对于推进MRI应用至关重要.
研究的目的:
- 通过多种替代物研究乙烯化的CEST特性.
- 开发具有更大的化学转移的新型diaCEST剂,以改善MRI对比度.
- 评估这些药物在癌症成像中的潜力.
主要方法:
- 系统地研究与不同芳香和异性替代剂的乙烯基化物.
- 在生理pH (7.2) 时调整不稳定的质子化学转移和汇率 (7.2).
- 在3T核磁共振扫描仪上评估CEST对比度,并在乳腺癌小鼠模型上进行体内测试.
主要成果:
- 乙基化物表现出可调节的可变质子化学转移从2.85.0 ppm和6802340 s-1的交换率.
- 亚酸二化物 (ADH) 在小鼠乳腺癌模型中显示出显著的对比.
- 一种乙基化衍生物在6.4ppm时表现出最远移位的可变质子,具有出色的对比性.
结论:
- 这项研究扩展了diaCEST剂的目录,增加了化学转移.
- 开发的药物,特别是ADH和acylhydrazones,显示了通过MRI改善癌症诊断的潜力.
- 这些发现有助于分子成像技术的进步,用于临床翻译.
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