Li Wenjin, Luo Yihui, Hua Yuqi, Shen Qiaoling, Chen Liping, Xu Yu, Fu Haitian, Yu Chunjing
Department of Nuclear Medicine, Affiliated Hospital of Jiangnan University, No. 1000, Hefeng Road, Wuxi 214000, China.
Wuxi School of Medicine, Jiangnan University, No. 1800, Lihu Avenue, Wuxi 214000, China.
Tomography. 2025 Mar 7;11(3):29. doi: 10.3390/tomography11030029.
Prostate-specific membrane antigen (PSMA)-targeted radioligands are promising diagnostic tools for the targeted positron emission tomography (PET) imaging of prostate cancer (PCa). In present work, we aimed to develop a novel PSMA tracer to provide an additional option for prostate cancer diagnosis. Our team designed a new structure of the PSMA tracer and evaluated it with cellular experiments in vitro to preliminarily verify the targeting and specificity of Ga-NOTA-GC-PSMA. PET/CT imaging of PSMA-positive xenograft-bearing models in vivo to further validate the in vivo specificity and targeting of the radiotracer. Pathological tissue sections from prostate cancer patients were compared with pathological immunohistochemistry and pathological tissue staining results by radioautography experiments to assess the targeting-PSMA of Ga-NOTA-GC-PSMA on human prostate cancer pathological tissues. The novel tracer showed high hydrophilicity and rapid clearance rate. Specific cell binding and micro-PET imaging experiments showed that Ga-NOTA-GC-PSMA displayed a high specific LNCaP tumor cell uptake (1.70% ± 0.13% at 120 min) and tumor-to-muscle (T/M) and tumor-to-kidney (T/K) ratio (13.87 ± 11.20 and 0.20 ± 0.08 at 60 min, respectively). The novel tracer Ga-NOTA-GC-PSMA is promising radionuclide imaging of PCa.
前列腺特异性膜抗原（PSMA）靶向放射性配体是用于前列腺癌（PCa）靶向正电子发射断层扫描（PET）成像的有前景的诊断工具。在本研究中，我们旨在开发一种新型PSMA示踪剂，为前列腺癌诊断提供额外选择。我们团队设计了一种新结构的PSMA示踪剂，并通过体外细胞实验对其进行评估，以初步验证Ga-NOTA-GC-PSMA的靶向性和特异性。对PSMA阳性异种移植荷瘤模型进行体内PET/CT成像，以进一步验证该放射性示踪剂的体内特异性和靶向性。通过放射自显影实验，将前列腺癌患者的病理组织切片与病理免疫组织化学和病理组织染色结果进行比较，以评估Ga-NOTA-GC-PSMA在人前列腺癌病理组织上对PSMA的靶向性。该新型示踪剂显示出高亲水性和快速清除率。特异性细胞结合和微型PET成像实验表明，Ga-NOTA-GC-PSMA在LNCaP肿瘤细胞摄取方面具有高特异性（120分钟时为1.70%±0.13%），肿瘤与肌肉（T/M）和肿瘤与肾脏（T/K）的比值分别为（60分钟时为13.87±11.20和0.20±0.08）。新型示踪剂Ga-NOTA-GC-PSMA在前列腺癌放射性核素成像方面具有前景。
