Zhang Xuran, Ruan Qing, Jiang Yuhao, Gan Qianqian, Zhang Junbo
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.
Transl Oncol. 2021 Jan;14(1):100966. doi: 10.1016/j.tranon.2020.100966. Epub 2020 Nov 24.
Previously, we reported a [Tc(ǀ)] labeled d-glucoamine derivative (Tc-CN5DG) and evaluated it as a tumor imaging agent in mice bearing A549 tumor xenografts. In this paper, Tc-CN5DG was further studied in U87 MG (human glioma cells), HCT-116 (human colon cancer cells), PANC-1 (human pancreatic cancer cells) and TE-1 (human esophageal cancer cells) tumor xenografts models to verify its potential application for imaging of different kinds of tumors. The biodistribution data showed that Tc-CN5DG had a similar biodistribution pattern in four tumor models at 2 h post-injection with high accumulation in tumors and kidneys. The tumor/muscle ratios (from 4.08 ± 0.42 to 9.63 ± 3.53) and tumor/blood ratios (from 17.18 ± 7.40 to 53.17 ± 16.16) of Tc-CN5DG in four tumor models were high. All four kinds of tumors could be clearly seen on their corresponding SPECT/CT images. Pharmacokinetic study in healthy CD-1 mice demonstrated that Tc-CN5DG cleared fast from blood (2 min, 12.97 ± 0.88%ID/g; 60 min, 0.33 ± 0.06%ID/g) and the blood distribution, elimination half-life was 5.81 min and 21.16 min, respectively. No abnormality was observed through the abnormal toxicity study. All of the above results demonstrated that Tc-CN5DG could be a broad-spectrum SPECT probe for tumor imaging and its further clinical application is warranted.
此前，我们报道了一种[锝（ǀ）]标记的d - 葡糖胺衍生物（Tc - CN5DG），并在携带A549肿瘤异种移植瘤的小鼠中对其作为肿瘤成像剂进行了评估。在本文中，对Tc - CN5DG在U87 MG（人胶质瘤细胞）、HCT - 116（人结肠癌细胞）、PANC - 1（人胰腺癌细胞）和TE - 1（人食管癌细胞）肿瘤异种移植瘤模型中进行了进一步研究，以验证其在不同类型肿瘤成像中的潜在应用。生物分布数据表明，注射后2小时，Tc - CN5DG在四种肿瘤模型中的生物分布模式相似，在肿瘤和肾脏中具有高蓄积。Tc - CN5DG在四种肿瘤模型中的肿瘤/肌肉比（从4.08±0.42到9.63±3.53）和肿瘤/血液比（从17.18±7.40到53.17±16.16）都很高。在相应的SPECT/CT图像上可以清晰地看到所有四种肿瘤。在健康的CD - 1小鼠中进行的药代动力学研究表明，Tc - CN5DG从血液中清除迅速（2分钟时，12.97±0.88%ID/g；60分钟时，0.33±0.06%ID/g），血液分布、消除半衰期分别为5.81分钟和21.16分钟。通过异常毒性研究未观察到异常。上述所有结果表明，Tc - CN5DG可能是一种用于肿瘤成像的广谱SPECT探针，值得进一步临床应用。
