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Development of 68Ga-NOTA-cRGD Probe Mediated by Sulfenic Acid for Prolonging Tumor Imaging

  • 0Department of Nuclear Medicine, The Affiliated Wuxi People's Hospital of Nanjing Medical University, Wuxi People's Hospital, Wuxi Medical Center, Nanjing Medical University, Wuxi, Jiangsu 214023, P. R. China.
Analytical Chemistry +

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June 9, 2025

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June 9, 2025

View abstract on PubMed

Summary

This summary is machine-generated.

This study introduces a new diagnostic probe, <sup>68</sup>Ga-NOTA-cRGD, which uses 1,3-cyclohexanedione to improve tumor targeting and imaging. The enhanced probe shows better cell uptake and longer imaging times in tumors.

Area Of Science

  • Biomedical Imaging
  • Radiochemistry
  • Oncology

Background

  • Reactive oxygen species (ROS) are key signaling molecules in the tumor microenvironment, influencing tumor growth, drug resistance, and metastasis.
  • 1,3-cyclohexanedione-based probes offer potential for real-time monitoring of ROS in tumors.

Purpose Of The Study

  • To synthesize and evaluate a novel tumor diagnostic probe, <sup>68</sup>Ga-NOTA-cRGD, incorporating a 1,3-cyclohexanedione moiety.
  • To investigate the probe's ability to enhance tumor targeting and prolong imaging time by cross-linking with sulfenic acid.

Main Methods

  • Synthesis of <sup>68</sup>Ga-NOTA-cRGD probe featuring a 1,3-cyclohexanedione group linking NOTA and cRGD peptide.
  • In vitro and in vivo evaluation of the probe's radiolabeling efficiency, stability, cell uptake, and biodistribution compared to a control probe lacking the 1,3-cyclohexanedione group.

Main Results

  • Efficient and stable radiolabeling with excellent physiological stability was achieved.
  • The 1,3-cyclohexanedione-containing probe (<sup>68</sup>Ga-NOTA-cRGD-2) showed superior cell uptake, tumor imaging contrast, and biodistribution compared to the control (<sup>68</sup>Ga-NOTA-cRGD-1).
  • Enhanced cell affinity and a prolonged in vivo biological half-life were observed, with higher uptake in A549 tumor cells.

Conclusions

  • The 1,3-cyclohexanedione moiety significantly enhances tumor-targeting capability and prolongs the retention of the diagnostic probe in tumors.
  • This finding provides a foundation for developing more effective tumor diagnostic probes utilizing this chemical group.