Investigation of Therapeutic Efficiency of Bleomycin and Bleomycin-Glucuronide Labeled with I-131 on the Cancer Cell Lines

Ediz M., Avcibasi U., ÜNAK P. , MUFTULER F. Z. B. , MEDİNE E. İ. , Kilcar A. Y. , ...More

CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS, vol.28, no.4, pp.310-319, 2013 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 28 Issue: 4
  • Publication Date: 2013
  • Doi Number: 10.1089/cbr.2012.1316
  • Page Numbers: pp.310-319
  • Keywords: A549, bleomycin, bleomycin-glucuronide, Caco-2, Hutu-80, I-131, PC-3, BETA-GLUCURONIDASE, TELOMERASE ACTIVITY, IN-VITRO, EXPRESSION, PRODRUGS


The aim of this study is to determine the incorporations of radiolabeled bleomycin (I-131-BLM) and bleomycin-glucuronide (I-131-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 I-131, quality control studies were done and the incorporation yields of I-131-BLM and I-131-BLMGLU on these cell lines were measured. Quality-control studies showed that the radiolabeling yields were obtained as 95% and 90% for I-131-BLM and I-131-BLMGLU, respectively. Also, as a result of the cell culture studies, it was found that I-131-BLM and I-131-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 I-131-BLMGLU was higher than that I-131-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 I-131-BLMGLU on the four cell lines were about five to six times higher than I-131-BLM. Radiolabeled glucuronide derivatives can be used in cancer therapy and tumor imaging, depending on the properties of radioiodine for the beta-glucuronidase-rich tissues because glucuronidation leads to rapid and higher incorporation on adenocarcinoma cells.