131I-Y-c（CGRRAGGSC）的合成、放射性合成及代谢
Synthesis, Radiosynthesis and Metabolism of 131I-Y-c(CGRRAGGSC).
作者信息
Xie Jilai, Pan Donghui, Lu Mudan, Chen Xuan, Chen Yu, Zhang Ting, Xie Yan, Zhou Huan, Liu Lu, Yang Min, Wang Jiajun, Chen Daozhen
机构信息
Wuxi Hospital for Maternal and Child Health Care Affiliated to Nanjing Medical University, Wuxi, Jiangsu 214002. China.
Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu, 214063. China.
出版信息
Anticancer Agents Med Chem. 2017;17(13):1769-1776. doi: 10.2174/1871520617666170713151647.
BACKGROUND
The formation of the complex interleukin-11(IL-11) and IL-11 receptor (IL-11R) is closely related with tumor progression. Binding of IL-11 to the IL-11 receptor α-chain (IL-11Rα) has been suggested as a target for human cancer. The cyclic peptide c(CGRRAGGSC) is a mimic of IL-11.
OBJECTIVE
To explore 131I-Y-c(CGRRAGGSC) synthesis and radiosynthesis, and metabolism in SKOV3 tumorbearing mice.
METHOD
In this study, 131I labeled c(CGRRAGGSC) was designed and characterized. For radiolabeling, tyrosine was used as a linker to connect c(CGRRAGGSC) and 131I. Balb/c nude mice bearing SKOV3 human ovarian carcinoma were used for in vivo studies. Uptake of 131I-cyclic nonapeptide by the tumor was visualized by single photon emission computerized tomography (SPECT).
RESULTS
The entire labeling process, which took 15 min by chloramine-T method, resulted in a high labeling yield (93.03±6.78%), and high radiochemical purity (RCP) (>95%). SPECT imaging showed that accumulation of the probe in the tumor was close to background levels. In addition, biodistribution studies showed that the accumulation of 131I-Y-c(CGRRAGGSC) in normal mice was similar to that of Na131I.
CONCLUSION
Tyrosine is a suitable chelating agent for the use of radioiodine labeling, however the bioactivity of the conjugate needs further investigation.
背景
白细胞介素 -11（IL -11）与IL -11受体（IL -11R）复合物的形成与肿瘤进展密切相关。IL -11与IL -11受体α链（IL -11Rα）的结合被认为是人类癌症的一个靶点。环肽c（CGRRAGGSC）是IL -11的模拟物。
目的
探索131I - Y - c（CGRRAGGSC）的合成、放射性合成及其在荷SKOV3肿瘤小鼠体内的代谢情况。
方法
本研究设计并表征了131I标记的c（CGRRAGGSC）。在放射性标记过程中，使用酪氨酸作为连接子连接c（CGRRAGGSC）和131I。采用荷SKOV3人卵巢癌的Balb/c裸鼠进行体内研究。通过单光子发射计算机断层扫描（SPECT）观察肿瘤对131I - 环九肽的摄取情况。
结果
采用氯胺 - T法的整个标记过程耗时15分钟，标记产率高（93.03±6.78%），放射化学纯度（RCP）高（>95%）。SPECT成像显示探针在肿瘤中的蓄积接近本底水平。此外，生物分布研究表明，131I - Y - c（CGRRAGGSC）在正常小鼠体内的蓄积情况与131I - 碘化钠相似。
结论
酪氨酸是用于放射性碘标记的合适螯合剂，然而偶联物的生物活性有待进一步研究。
Zotero 插件