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[目的]以肿瘤血管系统为目的靶,以核素标记多肽ATWLPPR为显像剂,探讨核素标记肿瘤血管特异性多肽显像用于肿瘤诊断的可行性。[方法]应用99mTc标记ATWLPPR并鉴定。制作荷人乳腺癌裸鼠模型,实验组于注射99mTc-ATWLPPR后不同时间显像,对照组应用未标记ATWLPPR预处理后显像,勾画感兴趣区,计算两组肿瘤与对侧相应部位放射性比值。荷瘤裸鼠于注射显像剂后180min,取感兴趣器官及肿瘤组织称重并测量放射性计数。[结果]以HYNIC作为双功能螯合剂,99mTc-HYNIC-ATWLPPR标记率可达91.53%±2.39%,放化纯为94.14%±1.75%,标志物体外稳定。实验组荷瘤裸鼠注射显像剂后180min肿瘤部位显影最为清晰,对照组肿瘤部位未见明显显像剂分布,两组肿瘤/对侧上肢的放射性比值分别为2.33±0.40和1.18±0.12(P<0.05)。显像剂在荷乳腺癌裸鼠体内肝脏和肾脏的摄取最高,脑部摄取最低。[结论]制备的99mTc-HYNIC-ATWLPPR方法简单,标记率和放化纯高、稳定性好,主要以肝脏和肾脏排泄;肿瘤组织可以对该显像剂特异性摄取,提示该显像剂可以用于肿瘤诊断。
[Objective] To explore the feasibility of using radionuclide-labeled tumor vascular-specific polypeptide imaging for tumor diagnosis with tumor vascular system as the target and radionuclide labeled peptide ATWLPPR as imaging agent. [Method] The 99mTc labeled ATWLPPR was identified and identified. The nude mouse model of human breast cancer was made. The experimental group was imaged at different time after 99mTc-ATWLPPR injection. The control group was pretreated with unlabeled ATWLPPR, and the region of interest was plotted to calculate the radioactivity ratio . Tumor bearing nude mice 180min after imaging agent injection, organ of interest and tumor tissue were weighed and the radioactivity count was measured. [Result] With HYNIC as a bifunctional chelator, the labeling rate of 99mTc-HYNIC-ATWLPPR reached 91.53% ± 2.39% and the radiochemical purity was 94.14% ± 1.75%. The markers were stable in vitro. The experimental group had the clearest development of the tumor site 180 days after injection of the imaging agent in nude mice, and no obvious imaging agent distribution was found in the tumor site of the control group. The radioactivity ratios of tumor / contralateral limb in the two groups were 2.33 ± 0.40 and 1.18 ± 0.12 P <0.05). Imaging agents in the breast cancer nude mice liver and kidney uptake, brain uptake lowest. [Conclusion] The prepared 99mTc-HYNIC-ATWLPPR method is simple, high labeling rate and high radiochemical purity, and is mainly excreted in the liver and kidney. The tumor tissue can specifically ingest the imaging agent, suggesting that the imaging agent can For cancer diagnosis.