Beijing Engineering Research Center of Radiographic Techniques and Equipment, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, China.
CAS Key Laboratory for Biological Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, China.
J Nanosci Nanotechnol. 2020 Mar 1;20(3):1375-1382. doi: 10.1166/jnn.2020.17169.
This work reports the synthesis, radiolabeling and imaging studies of iodine-124 labeled peptide modified gold nanoclusters (AuNCs) as positron emission tomography (PET) tracer for lung cancer. The novel modified Au nanoclusters were successfully synthesized by conjugation of tumortargeting peptide luteinizing hormone releasing hormone (LHRH) to human serum albumin (HAS) as a scaffold, resulting in 73% labeling yield of 124I-LHRH-HSA AuNCs. After rapid purification, the radiochemical purity was above 98%. Dynamic PET study in normal rats showed high liver accumulation and rapid lung clearance. Both the PET and fluorescence imaging in A549 xenografted tumor model demonstrated certain amount of tumor uptake. In orthotopic lung cancer model, the tumor sites could be clearly visualized between 2 to 5 hours in PET images. The higher radioactivity concentration in the left lung which inoculated orthotopic tumor than right lung also exhibited the targeting properties. The biological properties of this iodine-124 labeled nanoclusters afford potential applications for early diagnosis of lung cancer with PET.
本工作报道了碘-124 标记的肽修饰金纳米簇（AuNCs）作为正电子发射断层扫描（PET）示踪剂用于肺癌的合成、放射性标记和成像研究。新型修饰的 Au 纳米簇通过将肿瘤靶向肽促黄体激素释放激素（LHRH）与人血清白蛋白（HAS）偶联作为支架成功合成，导致 124I-LHRH-HSA AuNCs 的标记产率达到 73%。快速纯化后，放射化学纯度高于 98%。正常大鼠的动态 PET 研究显示肝脏摄取高，肺部清除快。A549 异种移植肿瘤模型的 PET 和荧光成像均显示出一定量的肿瘤摄取。在原位肺癌模型中，PET 图像在 2 至 5 小时之间可清晰显示肿瘤部位。左肺（接种原位肿瘤）的放射性活度浓度高于右肺，也表现出了靶向性。这种碘-124 标记纳米簇的生物学特性为使用 PET 进行肺癌的早期诊断提供了潜在的应用。
