设计、制备及评价新型环丙沙星黄原酸 TcN 配合物作为潜在的细菌性感染成像剂。

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.

Molecules. 2020 Dec 10;25(24):5837. doi: 10.3390/molecules25245837.

In order to seek novel technetium-99m bacterial infection imaging agents, a ciprofloxacin xanthate (CPF2XT) was synthesized and radiolabeled with [TcN] core to obtain the TcN-CPF2XT complex, which exhibited high radiochemical purity, hydrophilicity, and good stability in vitro. The bacteria binding assay indicated that TcN-CPF2XT had specificity to bacteria. A study of biodistribution in mice showed that TcN-CPF2XT had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses, indicating that it could distinguish bacterial infection from sterile inflammation. Compared to TcN-CPFXDTC, the abscess/blood and abscess/muscle ratios of TcN-CPF2XT were higher and the uptakes of TcN-CPF2XT in the liver and lung were obviously decreased. The results suggested that TcN-CPF2XT would be a potential bacterial infection imaging agent.

为了寻找新型锝-99m 细菌感染显像剂，合成了环丙沙星黄原酸酯（CPF2XT）并与 [TcN] 核标记，得到 TcN-CPF2XT 复合物，该复合物表现出高放射化学纯度、亲水性和良好的体外稳定性。细菌结合实验表明 TcN-CPF2XT 对细菌具有特异性。在小鼠的生物分布研究中发现，TcN-CPF2XT 在细菌感染组织中的摄取量高于松节油诱导的脓肿，表明它可以区分细菌感染和无菌性炎症。与 TcN-CPFXDTC 相比，TcN-CPF2XT 的脓肿/血液和脓肿/肌肉比值更高，肝和肺中的摄取量明显降低。结果表明，TcN-CPF2XT 可能成为一种有潜力的细菌感染显像剂。