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Synthesis and biodistribution study of a chlorotoxin derivative peptide labeled with Iodine-131 for tumor therapy

Author(s): Seyed Pezhman Shirmardi | Mojtaba Shamsaei | Mostafa Gandomkar | Mohammad Ghannadi Maragheh

Journal: Iranian Journal of Nuclear Medicine
ISSN 1681-2824

Volume: 18;
Issue: Suppl 1;
Start page: 114;
Date: 2010;
Original page

Keywords: Cancer | Peptide | 131I | Labeling | Chlorotoxin

Introduction: Chlorotoxin is a 36-amino acid peptide found in the venom of the Leiurus quinquestriatus which blocks small-conductance chloride channels. Chlorotoxin binds preferentially to glioma cells that allow development of new methods for the treatment and diagnosis of several types of cancer. Due to this a chlorotoxin derivative was labeled with 131I and investigated further. Methods: A chlorotoxin derivative was synthesized on a solid phase using a standard Fmoc strategy. Labeling with iodine-131 was performed through chloramine-T method and radiochemical analysis involved sephadex G-25 and HPLC methods. The stability of radiopeptide was checked in the presence of PBS and human serum at 37 °C up to 24 h. The biodistribution was studied in mice. Results: The chemical purity of synthesized peptide as assessed by analytical RP-HPLC was 95%. Labeling of peptide resulted in a radiochemical yield of 80% with radiochemical purity of > 95% with specific activity of 0.740 GBq/μmol. Results of In vitro studies demonstrated acceptable stability of compound in human serum and PBS solution. Conclusion: Biodistribution data showed moderate blood clearance, with concentration of radioactivity in the kidneys, liver, intestine and stomach.
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