Fang Si'an, Jiang Yuhao, Xiao Di, Zhang Xuran, Gan Qianqian, Ruan Qing, Zhang Junbo
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
Pharmaceutics. 2021 Apr 9;13(4):518. doi: 10.3390/pharmaceutics13040518.
To develop potential technetium-99m single-photon emission computed tomography (SPECT) imaging agents for bacterial infection imaging, the novel norfloxacin isonitrile derivatives CN4NF and CN5NF were synthesized and radiolabeled with a [Tc][Tc(I)] core to obtain [Tc]Tc-CN4NF and [Tc]Tc-CN5NF. These compounds were produced in high radiolabeling yields and showed hydrophilicity and good stability in vitro. The bacterial binding assay indicated that [Tc]Tc-CN4NF and [Tc]Tc-CN5NF were specific to bacteria. Compared with [Tc]Tc-CN4NF, biodistribution studies of [Tc]Tc-CN5NF showed a higher uptake in bacteria-infected tissues than in turpentine-induced abscesses, indicating that [Tc]Tc-CN5NF could distinguish bacterial infection from sterile inflammation. In addition, [Tc]Tc-CN5NF had higher abscess/blood and abscess/muscle ratios. SPECT image of [Tc]Tc-CN5NF showed that there was a clear accumulation in the infection site, suggesting that it could be a potential bacterial infection imaging radiotracer.
为开发用于细菌感染成像的潜在锝-99m单光子发射计算机断层扫描（SPECT）显像剂，合成了新型诺氟沙星异腈衍生物CN4NF和CN5NF，并用[Tc][Tc(I)]核进行放射性标记，得到[Tc]Tc-CN4NF和[Tc]Tc-CN5NF。这些化合物的放射性标记产率很高，在体外表现出亲水性和良好的稳定性。细菌结合试验表明，[Tc]Tc-CN4NF和[Tc]Tc-CN5NF对细菌具有特异性。与[Tc]Tc-CN4NF相比，[Tc]Tc-CN5NF的生物分布研究表明，其在细菌感染组织中的摄取高于松节油诱导性脓肿，这表明[Tc]Tc-CN5NF可以区分细菌感染和无菌性炎症。此外，[Tc]Tc-CN5NF具有更高的脓肿/血液和脓肿/肌肉比值。[Tc]Tc-CN5NF的SPECT图像显示感染部位有明显的聚集，表明它可能是一种潜在的细菌感染成像放射性示踪剂。
