Ediz M.Avcibaşi U.Ünak P.Müftüler F.Z.B.Medine E.I.Yurt Kilçar A.Demiroǧlu H.Gümüşer F.G.Sakarya S.2024-07-222024-07-22201310849785http://akademikarsiv.cbu.edu.tr:4000/handle/123456789/17366The aim of this study is to determine the incorporations of radiolabeled bleomycin (131I-BLM) and bleomycin-glucuronide (131I- BLMGLU) on PC-3 (human prostate carcinoma cell line), Caco-2 (human colon adenocarcinoma cell line), Hutu-80 (Human Duodenum adenocarcinoma cell line), and A549 (Human lung adenocarcinoma epithelial cell line) cancerous cell lines. For this purpose, BLM and BLMGLU enyzmatically synthesized were labeled with 131I, quality control studies were done and the incorporation yields of 131I-BLM and 131I-BLMGLU on these cell lines were measured. Quality-control studies showed that the radiolabeling yields were obtained as 95% and 90% for 131I-BLM and 131I-BLMGLU, respectively. Also, as a result of the cell culture studies, it was found that 131I-BLM and 131I-BLMGLU had higher incorporation on PC-3 cells than that of other cell lines. In addition to this, it was reported that the incorporation yield of 131I-BLMGLU was higher than that 131I-BLM. At the end of the study, cytotoxicities of BLM and BLMGLU on PC-3 cancerous cell line were inspected and fluorescent images of BLM and BLMGLU were taken on PC-3 cells by using fluorescein isothiocyanate. In conclusion, cell culture studies demonstrated that the incorporation values of 131I-BLMGLU on the four cell lines were about five to six times higher than 131I-BLM. Radiolabeled glucuronide derivatives can be used in cancer therapy and tumor imaging, depending on the properties of radioiodine for the β-glucuronidase-rich tissues because glucuronidation leads to rapid and higher incorporation on adenocarcinoma cells. © Mary Ann Liebert, Inc.EnglishAdenocarcinomaAntineoplastic AgentsApoptosisBleomycinCaco-2 CellsCell ProliferationDuodenal NeoplasmsGlucuronidesHumansIodine RadioisotopesLung NeoplasmsMaleOptical ImagingProstatic Neoplasmsbleomycinbleomycin glucuronide i 131bleomycin i 131fluorescein isothiocyanateglucuronideradiopharmaceutical agentunclassified drugantineoplastic agentbleomycinglucuronideradioactive iodineanimal tissueantineoplastic activityapoptosisarticlecancer cell culturecell survivalcell viabilitycolon adenocarcinomaconcentration responsecontrolled studydiagnostic imagingdrug glucuronidationdrug structuredrug synthesishigh performance liquid chromatographyhumanhuman cellin vitro studyisotope labelinglung adenocarcinomamalemicrosomenonhumanpriority journalprostate carcinomaquality controlradiation injuryradiochromatographyradioiodinationratstomach adenocarcinomaadenocarcinomaCACO 2 cell linecell proliferationchemistrydrug effectsduodenum tumorfluorescence imaginglung tumormetabolismProstatic NeoplasmsArticle10.1089/cbr.2012.1316