Development of ¹⁵³Sm-bleomycin as a possible therapeutic complex

Development of 153 Sm-bleomycin as a possible therapeutic complex 1 first-author 2 2 corresp Corresponding author. E-mail address: ajalilian@nrcam.org Corresponding author. E-mail address: ajalilian@nrcam.org ajalilian@nrcam.org 2 2 2 Faculty of Nuclear Engineering and Physics, Amir Kabir University, Tehran, Iran Faculty of Nuclear Engineering and Physics, Amir Kabir University, Tehran, Iran Radiopharmaceutical Research and Development Laboratories, Nuclear Science and Technology Research Institute, Tehran, Iran Radiopharmaceutical Research and Development Laboratories, Nuclear Science and Technology Research Institute, Tehran, Iran Due to interesting therapeutic properties of 153 Sm and antineoplastic antibiotic, bleomycin (BLM), 153 Sm-bleomycin ( 153 Sm-BLM) was developed as a possible therapeutic compound using 153 SmCl 3 and BLM. The 153 SmCl 3 was obtained by thermal neutron flux (5×10 13 n·cm –2 ·s –1 ) of an enriched 152 Sm 2 O 3 sample, dissolved in acidic media. Under optimized conditions (room temperature, 45 min, 0.1 mg bleomycin for 740–3700 MBq 153 SmCl 3 ) a radiochemical purity over 98 % was obtained shown by HPLC (Specific activity = 55 TBq/mM). The 153 SmCl 3 and 153 Sm-BLM were administered into wild-type rats up to 96 h followed by biodistribution. The SPECT imaging of labeled compound in wild-type rats was performed and significant image pattern was observed for a radiolabeled bleomycin compound. The 153 Sm-BLM is a potential therapeutic compound and our experiments on this compound have shown satisfactory quality, and stability suitable for future therapeutic studies. Bleomycin Sm-153 Biodistribution Radiolabeling References Zhao G , Li F , Lin H , Lin H . Bioorg Med Chem , 2007 , 15 : 533 - 40 . Bioorg Med Chem Heffeter P , Jakupec MA , Körner W . Biochem Pharmacol , 2007 , 73 : 1873 - 86 . Biochem Pharmacol Firestone R B , Shirley V S , Baglin C M , Zipkin, J . Table of isotopes, 8th edition (CDROM) , Version 1.0 . Wiley-Interscience , New York , 1996 . Table of isotopes, 8th edition (CDROM) Misra S N , Gagnani M A , Shukla R S . Bioinorg Chem Appl , 2004 , 2 : 155 - 92 . Bioinorg Chem Appl Kostova I . Curr Med Chem Anticancer Agents , 2005 , 5 : 591 - 602 . Review . Curr Med Chem Anticancer Agents Umezawa H T , Takeuchi S , Hori T J . Antibiot , 1972 , 7 : 409 - 420 . Antibiot Korppi-Tommola T , Huhmar H , Aronen HJ . Nucl Med Commun , 1999 , 20 : 145 - 152 . Nucl Med Commun Jalilian A R , Yari Kamrani Y , Sadeghi M . Nukleonika , 2006 , 51 : 119 - 123 . Nukleonika Jalilian A R , Shirazi B , Aboudzadeh R . Radiochim Acta , 2006 , 94 : 453 - 459 . Radiochim Acta Jalilian A R , Rowshanfarzad P , Sabet M . J Radioan Nucl Chem , 2005 , 264 : 617 - 621 . J Radioan Nucl Chem Ferro-Flores G , De Mara Ramrez F , Tendilla J I . Bio-conjugate Chem , 1999 , 10 : 726 - 734 . Bio-conjugate Chem Jalilian A R , Fateh B , Ghergherehchi M . Nukleonika , 2005 , 50 : 143 - 148 . Nukleonika Jalilian A R , Zandi H , Sardari D . Nukleonika , 2009 , 54 ( 2 ) 135 - 141 . Nukleonika Melnyk D L , Horwitz S B , Peisach . J Inorganica Chimica Acta , 1987 , 138 : 75 - 78 . J Inorganica Chimica Acta Anthoiine W E , Soiaiman D , Saryan L A . J Inorg Biochem , 1982 , 11 : 7544 . J Inorg Biochem Bereman RD , Winkler ME . J Inorg Biochem , 1980 , 13 : 95 - 104 . J Inorg Biochem Reynolds J E , Martindale, the extra pharmacopoeia , 31 st edn.: London , Royal Pharmaceutical Society , 1996 , 546 - 547 . Martindale, the extra pharmacopoeia Takita T , Umezawa Y , Saito SI . Tet Lett , 1982 , 123 : 521 - 524 . Tet Lett Welwyn H , Proceedings of First International Symposium on Bleomycin , London, Lundbeck Ltd . 1973 , 1972 - 1974 . Jalilian A R , Mirzaii M , Karimian A . Iran J Nucl Med , 2005 , 23 : 19 - 26 . Iran J Nucl Med 10.13538/j.1001-8042/nst.21.165-170 2009-06-31 2010-06-20 2021-01-19 2010 Nuclear Science and Techniques 03 21