Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Bioorg Med Chem Lett. 2021 Jul 1;43:128102. doi: 10.1016/j.bmcl.2021.128102. Epub 2021 May 10.
In order to find a Tc-labeled deferoxamine radiotracer for bacterial infection imaging, deferoxamine dithiocarbamate (DFODTC) was successfully synthesized and it was radiolabeled with [TcN] core to prepare the TcN(DFODTC) complex. TcN(DFODTC) was obtained with high radiochemical purity without further purification. The complex was lipophilic and exhibited good in vitro stability. According to the result of bacterial binding study, the binding of TcN(DFODTC) to bacteria was specific. Biodistribution in mice study indicated that TcN(DFODTC) had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses at 120 min after injection, which showed that the radiotracer could differentiate between bacterial infection and sterile inflammation. SPECT/CT images showed that there was a clear accumulation in infection sites, suggesting that TcN(DFODTC) could be a potential bacterial infection imaging radiotracer.
为了寻找用于细菌感染成像的 Tc 标记的去铁胺放射性示踪剂，成功合成了去铁胺二硫代氨基甲酸盐（DFODTC），并用 [TcN] 核标记制备了 TcN(DFODTC) 络合物。TcN(DFODTC) 不经进一步纯化即可获得高放射化学纯度。该络合物具有亲脂性，并表现出良好的体外稳定性。根据细菌结合研究的结果，TcN(DFODTC)与细菌的结合是特异性的。在小鼠的生物分布研究中，与在松节油诱导的脓肿相比，注射后 120 分钟，TcN(DFODTC)在细菌感染组织中的摄取更高，这表明该示踪剂可区分细菌感染和无菌性炎症。SPECT/CT 图像显示在感染部位有明显的积聚，表明 TcN(DFODTC)可能是一种有潜力的细菌感染成像放射性示踪剂。
