Browsing by Author "Müftüler F.Z.B."

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    In vivo biodistribution of 131I labeled bleomycin (BLM) and isomers (A2 and B2) on experimental animal models
    (2010) AvcIbaşI U.; Demiroǧlu H.; Ünak P.; Müftüler F.Z.B.; Içhedef Ç.A.; Gümüşer F.G.
    Bleomycins (BLMs; BLM, A2, and B2) were labeled with 131I and radiopharmaceutical potentials were investigated using animal models in this study. Quality control procedures were carried out using thin layer radiochromatography (TLRC), high performance liquid chromatography (HPLC), and liquid chromatography (LC/MS/MS). Labeling yields of radiolabeled BLMs were found to be 90, 68, and 71%, respectively. HPLC chromatograms were taken for BLM and cold iodinated BLM (127I-BLM). Five peaks were detected for BLM and three peaks for 127I-BLM in the HPLC studies. Two peaks belong to isomers of BLM. The isomers of BLM were purified with using HPLC. Biological activity of BLM was determined on male Albino Wistar rats by biodistribution and scintigraphic studies were performed for BLMs by using New Zelland rabbits. The biodistribution results of 131I-BLM showed high uptake in the stomach, the bladder, the prostate, the testicle, and the spinal cord in rats. Scintigraphic results on rabbits agrees with that of biodistributional studies on rats. The scintigraphy of radiolabeled isomers (131I-A2 and 131I-B2) are similiarly found with that of 131I-BLM. © 2010 Akadémiai Kiadó, Budapest, Hungary.
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    Metabolic comparison of radiolabeled bleomycin and bleomycin-glucuronide labeled with 99mTc
    (2011) Koçan F.; Avcíbaşí U.; Ünak P.; Müftüler F.Z.B.; Içhedef Ç.A.; Demiroǧlu H.; Gümüşer F.G.
    The metabolic comparison of bleomycin (BLM) and bleomycin-glucuronide (BLMG) radiolabeled with 99mTc ( 99mTc-BLM and 99mTc-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 99mTc, 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 99mTc-BLM and 99mTc-BLMG metabolized as N-glucuronide were observed within 2 hours in the liver, the bladder, and the spinal cord for 99mTc-BLM and the lung, the liver, the kidney, the large intestine, and the spinal cord for 99mTc-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 99mTc-BLMG was found to be better than that of 99mTc-BLM. © 2011, Mary Ann Liebert, Inc.
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    Radiolabeling of bleomycin-glucuronide with 131I and biodistribution studies using xenograft model of human colon tumor in Balb/C mice
    (2012) Demiroǧlu H.; Avcibaşi U.; Ünak P.; Müftüler F.Z.B.; Içhedef Ç.A.; Gümüşer F.G.; Sakarya S.
    Bleomycin-glucuronide (BLMG) is the glucuronide conjugate of BLM. In the present study, BLMG was primarily enzymatically synthesized by using a microsome preparate separated from rat liver, labeled with 131I by iodogen method with the aim of generating a radionuclide-labeled prodrug, and investigated its bioaffinities with tumor-bearing Balb/C mice. Quality control procedures were carried out using thin-layer radiochromatography and high-performance liquid chromatography. Tumor growing was carried out by following Caco-2 cell inoculation into mice. Radiolabeling yield was found to be about 65%. Results indicated that 131I-labeled BLMG ( 131I-BLMG) was highly stable for 24 hours in human serum. Biodistribution studies were carried out with male Albino Wistar rats and colorectal adenocarcinoma tumor-bearing female Balb/C mice. The biodistribution results in rats showed high uptake in the prostate, the large intestine, and the spinal cord. In addition to this, scintigraphic results agreed with those of biodistributional studies. Xenography studies with tumor-bearing mice demonstrated that tumor uptakes of 131I-BLM and 131I-BLMG were high in the first 30 minutes postinjection. Tumor-bearing animal studies demonstrated that 131I-BLMG was specially retained in colorectal adenocarcinoma with high tumor uptake. Therefore, 131I-BLMG can be proven to be a promising imaging and therapeutic agent, especially for colon cancer in nuclear medical applications. © Copyright 2012, Mary Ann Liebert, Inc. 2012.
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    Investigation of therapeutic efficiency of bleomycin and bleomycin-glucuronide labeled with 131I on the cancer cell lines
    (Mary Ann Liebert Inc., 2013) Ediz M.; Avcibaşi U.; Ünak P.; Müftüler F.Z.B.; Medine E.I.; Yurt Kilçar A.; Demiroǧlu H.; Gümüşer F.G.; Sakarya S.
    The 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.
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    Investigation of therapeutic efficiency of phenytoin (PHT) labeled with radioactive 131I in the cancer cell lines
    (Springer Netherlands, 2016) Uzaras C.; Avcıbaşı U.; Demiroğlu H.; Medine E.İ.; Kılçar A.Y.; Müftüler F.Z.B.; Ünak P.
    The aim of this study is to determine the incorporations of PHT radiolabeled with 131I (131I-PHT) on U-87 MG, Daoy and A549 cancerous cell lines. For this, cold and radio-labeling studies were carried out. The radio-labeling yield of 131I-PHT was obtained about 95 %. Subsequently, cell culture studies were carried out and radio-labeling yields of 131I, 131I-PHT on U-87 MG, Daoy and A549 cancerous cells were investigated. Cell culture studies demonstrated that the incorporation values of 131I-PHT on the three cell lines decreased with increasing radioactivity. Consequently, 131I-PHT may be a good radiopharmaceutical for targeting radionuclide therapy of Central Nervous System Tumors. © 2015, Akadémiai Kiadó, Budapest, Hungary.
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    Preparation of a 99mTc-labeled graft polymer and its in vitro and in vivo evaluation
    (Springer Science and Business Media B.V., 2021) Avcıbaşı U.; Türkyarar T.; Karadağ A.; Bakan B.; Yavaşoğlu N.Ü.K.; Kuşat K.; Akgöl S.; Gülcemal D.; Tekin V.; Müftüler F.Z.B.; Topal G.; Parlak Y.; Gümüşer F.G.
    The aim of this study is the synthesis of a novel 99mTc-labeld graft polymer and the biological evaluation of its in vitro and in vivo properties. To this end, a L-proline-graft-poly(HEMA) was prepared and labeled with 99mTc. The radiochemical yield of approximately the 99mTc-labeled compound amounted to 97 ± 2.3%. The cytotoxicity test revealed no cytotoxic effect after a 24- and 48-h incubation. The results of the hemolysis test showed that hemolysis was non-toxic with an effect level of less than 2%. Subsequently, the biodistribution in healthy rats was determined. High accumulation of the polymer was observed in the pancreas, thyroid and prostate. © 2021, Akadémiai Kiadó, Budapest, Hungary.