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Synthesis and biodistribution study of a chlorotoxin derivative peptide labeled with 131- iodine for tumor therapy
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S.P. Shirmardi   , M. Shamsaei , M. Gandomkar , M. Ghannadi Maragheh |
| , pysham@aut.ac.ir |
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Abstract: (14322 Views) |
| Background: 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.
Thus chlorotoxin derivative was labeled with 131I for
further investigation. Materials and 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. Result of in vitro studies demonstrated
acceptable stability of compound in human
serum and PBS solution. Biodistribution data showed
moderate blood clearance, with concentration of
radioactivity in the kidneys, liver, intestine and
stomach. Conclusion: Results indicates that the
labeled Chlorotoxin derivative might be useful in
determining tumor extent and also, tumor therapy of
gliomas or possibily other cancers. Iran. J. Radiat. Res.,
2011 8(4): 243-248 |
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| Keywords: Cancer, peptide, 131I, labeling, chlorotoxin. |
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Full-Text [PDF 342 kb]
(4024 Downloads)
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Type of Study: Original Research |
Subject:
Radiation Biology
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