Department of Nuclear Medicine, Peking University First Hospital, 100034, Beijing, P. R. China.
State Key Laboratory of Organic-Inorganic Composites and Beijing Key Lab of Bioprocess, Beijing University of Chemical Technology, 15 Beisanhuan East Road, Chaoyang District, 100029, Beijing, P. R. China.
Chemistry. 2020 Sep 10;26(51):11705-11709. doi: 10.1002/chem.202002415. Epub 2020 Aug 11.
Chemical exchange saturation transfer (CEST) MRI has recently emerged as a versatile molecular imaging approach in which diamagnetic compounds can be utilized to generate an MRI signal. To expand the scope of CEST MRI applications, herein, we systematically investigated the CEST properties of N-aryl amides with different N-aromatic substitution, revealing their chemical shifts (4.6-5.8 ppm) and exchange rates (up to thousands s ) are favorable to be used as CEST agents as compared to alkyl amides. As the first proof-of-concept study, we used CEST MRI to detect the enzymatic metabolism of the drug acebutolol directly by its intrinsic CEST signal without any chemical labeling. Our study implies that N-aryl amides may enable the label-free CEST MRI detection of the metabolism of many N-aryl amide-containing drugs and a variety of enzymes that act on N-aryl amides, greatly expanding the scope of CEST MR molecular imaging.
化学交换饱和转移（CEST）MRI 最近作为一种多功能分子成像方法出现，其中可以使用抗磁性化合物来产生 MRI 信号。为了扩展 CEST MRI 的应用范围，在此，我们系统地研究了具有不同 N-芳基取代的 N-芳酰胺的 CEST 性质，结果表明其化学位移（4.6-5.8ppm）和交换率（高达几千秒）非常适合用作 CEST 试剂，与烷基酰胺相比。作为首个概念验证研究，我们使用 CEST MRI 直接通过其内在的 CEST 信号来检测药物醋丁洛尔的酶代谢，而无需任何化学标记。我们的研究表明，N-芳酰胺可能能够实现对许多含有 N-芳酰胺的药物和作用于 N-芳酰胺的各种酶的代谢的无标记 CEST MRI 检测，从而极大地扩展了 CEST MR 分子成像的范围。
