Department of Chemistry, University of York, Heslington, York, YO10 5DD, UK.
School of Biological Sciences, University of Southampton, Southampton, UK.
ChemMedChem. 2018 Feb 20;13(4):352-359. doi: 10.1002/cmdc.201700725. Epub 2018 Jan 18.
Production of a biocompatible hyperpolarized bolus for signal amplification by reversible exchange (SABRE) could open the door to simple clinical diagnosis via magnetic resonance imaging. Essential to successful progression to preclinical/clinical applications is the determination of the toxicology profile of the SABRE reaction mixture. Herein, we exemplify the cytotoxicity of the SABRE approach using in vitro cell assays. We conclude that the main cause of the observed toxicity is due to the SABRE catalyst. We therefore illustrate two catalyst removal methods: one involving deactivation and ion-exchange chromatography, and the second using biphasic catalysis. These routes produce a bolus suitable for future in vivo study.
生产用于通过可逆交换（SABRE）进行信号放大的生物相容性超极化 bolus 可以为通过磁共振成像进行简单的临床诊断打开大门。成功推进到临床前/临床应用的关键是确定 SABRE 反应混合物的毒理学概况。在这里，我们使用体外细胞测定法说明了 SABRE 方法的细胞毒性。我们得出结论，观察到的毒性的主要原因是由于 SABRE 催化剂。因此，我们说明了两种催化剂去除方法：一种涉及失活和离子交换层析，另一种使用两相催化。这些路线产生适合未来体内研究的 bolus。
