Synthesis, Radiosynthesis and Metabolism of 131I-Y-c(CGRRAGGSC)

Title:Synthesis, Radiosynthesis and Metabolism of 131I-Y-c(CGRRAGGSC)

Volume: 17 Issue: 13

Author(s): Jilai Xie, Donghui Pan, Mudan Lu, Xuan Chen, Yu Chen, Ting Zhang, Yan Xie, Huan Zhou, Lu Liu*, Min Yang*, Jiajun Wang*Daozhen Chen*

Affiliation:

• School of Medicine of Southeast University, Nanjing, Jiangsu 210009,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

• Wuxi Hospital for Maternal and Child Health Care Affiliated to Nanjing Medical University, Wuxi, Jiangsu 214002,China

• Wuxi Hospital for Maternal and Child Health Care Affiliated to Nanjing Medical University, Wuxi, Jiangsu 214002,China

Keywords: c(CGRRAGGSC), interleukin 11, ovarian cancer, SPECT, radiosynthesis, receptor.

Abstract: 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.

Cite this article as:

Xie Jilai , Pan Donghui , Lu Mudan , Chen Xuan , Chen Yu , Zhang Ting , Xie Yan , Zhou Huan , Liu Lu *, Yang Min *, Wang Jiajun *, Chen Daozhen *, Synthesis, Radiosynthesis and Metabolism of 131I-Y-c(CGRRAGGSC), Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (13) . https://dx.doi.org/10.2174/1871520617666170713151647