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Due to interesting therapeutic properties of 177Lu and antineoblastic antibiotic, bleomycin (BLM), 177Lu-bleomycin (177Lu-BLM) was developed as a possible therapeutic compound. Lu-177 of 2.6-3 GBq/mg specific activity was obtained by irradiation of a natural Lu2O3 sample with a thermal neutron flux of 4 × 1013 nźcm-2źs-1. The product was converted into chloride form which was further used for labeling of BLM. In optimized conditions a radiochemical purity of 98% was obtained for 177Lu-BLM shown by instant thin-layer chromatography (ITLC) (specific activity, 740 GBq/mmole). Biodistribution studies of Lu-177 chloride and 177Lu-BLM were performed in wild-type rats. The accumulation of the radiolabeled compound in lungs, liver and spleen demonstrates a pattern similar to the other radiolabeled bleomycins. Lu-BLM is a possible therapeutic agent in human malignancies and the efficacy of the compound should be tested in various tumor-bearing models.
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285--291
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Bibliogr. 21 poz., rys.
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autor
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autor
- Radiopharmaceutical Research and Development Laboratory (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Postal code: 14155-1339, Tehran, Iran, Tel.: +98 21 8822 1103, Fax: +98 21 8822 1105, ajalilian@nrcam.org
Bibliografia
- 1. Bahrami-Samani A, Ghannadi-Maragheh M, Jalilian AR, Mazidi M (2010) Biological studies of samarium-153 bleomycin complex in human breast cancer murine xenografts for therapeutic applications. Radiochim Acta 98:237–242
- 2. Bodei L, Ferone D, Grana CM et al. (2009) Peptide receptor therapies in neuroendocrine tumors. J Endocrinol Invest 2;4:360–369
- 3. Brooks RC, Canochan P, Vollano JF, Powel NA, Zwiet J (1999) Metal complexes of bleomycin: evaluation of [Rh-105]-Bleomycin for use in targeted radiotherapy. Nucl Med Biol 26:421–430
- 4. Chakraborty S, Das T, Banerjee S et al. (2008) 177Lu-EDTMP: a viable bone pain palliative in skeletal metastasis. Cancer Biother Radiopharm 23;2:202–213
- 5. Chakraborty S, Das T, Banerjee S, Sarma HD, Venkatesh M (2006) Preparation and preliminary biological evaluation of 177Lu-labelled hydroxyapatite as a promising agent for radiation synovectomy of small joints. Nucl Med Commun 27;8:661–668
- 6. Chakraborty S, Das T, Sarma HD, Venkatesh M, Banerjee S (2008) Preparation and preliminary studies on 177Lu-labeled hydroxyapatite particles for possible use in the therapy of liver cancer. Nucl Med Biol 35;5:589–597
- 7. IAEA (2003) Manual for reactor produced radioisotopes.IAEA-TECDOC-1340. International Atomic Energy Agency, Vienna
- 8. Jalilian AR, Fateh B, Ghergherehchi M, Karimian A (2005) Development of [62Zn]bleomycin as a possible PET tracer. Nukleonika 50:143–148
- 9. Jalilian AR, Rowshanfarzad P, Sabet M, Novinrooz A, Raisali G (2005) Preparation of [66Ga]Bleomycin complex as a possible PET radiopharmaceutical. J Radioanal Nucl Chem 264:617–621
- 10. Jalilian AR, Shirazi B, Aboudzadeh R et al. (2006) [201Tl] (III)-Bleomycin for tumor imaging. Radiochim Acta 94:453–459
- 11. Jalilian AR, Zandi H, Sardari D et al. (2009) Preparation and biological evaluation of [Cu-61]bleomycin complex as a possible PET radiopharmaceutical. Nukleonika 54:135–141
- 12. Korppi-Tommola T, Huhmar H, Aronen HJ et al. (1999) 111In-labelled bleomycin complex for the differentiation of high- and low-grade gliomas. Nucl Med Commun 20:145–152
- 13. Lenkinski RE, Peerce, BE, Pillai MRI, Glickson JD (1980) Calcium(II) and the trivalent lanthanide ion complexes of the bleomycin antibiotics. Potentiometric, fluorescence and proton NMR studies. J Am Chem Soc 102:7088–7093
- 14. Melnyk DL, Horwitz SB, Peisach T (1987) The oxidation-reduction potential of copper-bleomycin. Inorg Chim Acta 138:75–78
- 15. Michael RB, Andrews PM, Rosario AV, Goldenberg DM, Mattes MJ (2005) 177Lu-antibody conjugates for single-cell kill of B-lymphoma cells in vitro and for therapy of micrometastases in vivo. Nucl Med Biol 32:269–278
- 16. Reynolds JE, Martindale I (ed) (1996) The extra pharmacopoeia, 31st ed. Royal Pharmaceutical Society, London, pp 546–547
- 17. Stern PH, Halpern SE, Hagan PL, Howell SB, Dabbs JE, Gordon RM (1981) Cytotoxic activity, tumor accumulationand tissue distribution of ruthenium-103-labeled-bleomycin. J Nat Cancer Inst 66:807–811
- 18. Sullivan JC, Friedman AM, Rayudu GVS, Fordham EW,Ramachandran PC (1075) Tumor localization studies with radioactive lanthanide and actinide complexes. J Nucl Med Biol 2:44–45
- 19. Takita T, Umezawa Y, Saito SI et al. (1982) Retrosynthetic manipulation of bleomycins. Tetrahedron Lett 123:521–524
- 20. Umezawa HT, Takeuchi S, Hori T (1972) Studies on the mechanisms of anti-tumor effects of bleomycin on squamous cell carcinoma. J Antibiot 7:409–420
- 21. Wenzel TJ, Zomlefer K, Rapkin SA, Keith RH (1995) Lanthanide luminescence detection of bleomycins and nalidixic acid. J Liquid Chromat Rel Technol 18:1473–1486
Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BUJ7-0014-0045