title: Metabolic comparison of radiolabeled bleomycin and bleomycin-glucuronide labeled with 99mTc.
abstract: The metabolic comparison of bleomycin (BLM) and bleomycin-glucuronide (BLMG) radiolabeled with (99m)Tc ((99m)Tc-BLM and (99m)Tc-BLMG, respectively) has been investigated in this study. Quality control procedures were carried out using thin-layer radiochromatography and high-performance liquid chromatography. To compare the metabolic behavior of BLM and its glucuronide conjugate radiolabeled with (99m)Tc, scintigraphic, and biodistributional techniques were applied using male New Zealand rabbits and Albino Wistar rats. The results obtained have shown that these compounds were successfully radiolabeled with a labeling yield of about 100%. Maximum uptakes of (99m)Tc-BLM and (99m)Tc-BLMG metabolized as N-glucuronide were observed within 2 hours in the liver, the bladder, and the spinal cord for (99m)Tc-BLM and the lung, the liver, the kidney, the large intestine, and the spinal cord for (99m)Tc-BLMG, respectively. Scintigraphy and biodistributional studies performed on the experimental animals have shown that radiopharmaceutical potentials of these compounds are completely different. At the same time, uptake of the (99m)Tc-BLMG was found to be better than that of (99m)Tc-BLM.
authors.affiliation: Department of Chemistry, Faculty of Art and Science, Celal Bayar University, Manisa, Turkey.
authors.forename: Feray
authors.initials: F
authors.lastname: Koçan
authors.forename: Ugur
authors.initials: U
authors.lastname: Avcıbaşı
authors.forename: Perihan
authors.initials: P
authors.lastname: Unak
authors.forename: Fazilet Zümrüt Biber
authors.initials: FZ
authors.lastname: Müftüler
authors.forename: Cigdem A
authors.initials: CA
authors.lastname: Içhedef
authors.forename: Hasan
authors.initials: H
authors.lastname: Demiroğlu
authors.forename: Fikriye G
authors.initials: FG
authors.lastname: Gümüşer
mesh_terms: D000818:Animals; D001761:Bleomycin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D020719:Glucuronides / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: D020719:Glucuronides; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D001761:Bleomycin