Browsing by Author "Medine E.I."

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    Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)
    (2012) Ünak P.; Biber Müftüler F.Z.; Içhedef Ç.; Medine E.I.; Özmen K.; Ünak T.; Kilçar A.Y.; Gümüşer F.G.; Parlak Y.; Bilgin E.S.
    Diethylstilbestrol (DES) is a well known, nonsteroidal estrogen with high affinity for the estrogen receptor (ER). Today DES is used to treat breast and prostate cancers. A phosphate derivative of DES [Diethylstilbestrol diphosphate (DES-P)] which is specific to tumor cells consisting alkaline phosphatase enzyme was synthesized and labeled with 99mTc using tin chloride as reducing agent. In vivo biological activity of 99mTc labeled diethylstilbestrol phosphate compound ( 99mTc-DES-P) was examined by biodistribution studies on Wistar Albino rats. Statistical evaluation was performed using SPSS 13 program. The percentage (%) radiolabeling yield of 99mTc-DES-P and quality control studies were done by Thin Layer Radio Chromatography (TLRC). Results showed that, 99mTc-DES-P may be proposed as an imaging agent for ER enriched tumors such as uterus and prostate and their metastases in bones. © 2012 Akadémiai Kiadó.
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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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    Synthesis, characterization and radiolabeling of folic acid modified nanostructured lipid carriers as a contrast agent and drug delivery system
    (Elsevier Ltd, 2017) Ucar E.; Teksoz S.; Ichedef C.; Kilcar A.Y.; Medine E.I.; Ari K.; Parlak Y.; Sayit Bilgin B.E.; Unak P.
    Nanostructured lipid carriers (NLCs) are the new generation of solid lipid drug delivery systems. Their suitability as contrast agents for gamma scintigraphy is an attracting major attention. The aim of current study was to prepare surface modified nanostructured lipid carrier system for paclitaxel (PTX) with active targeting and imaging functions. In accordance with the purpose of study, PTX loaded nanostructured lipid carriers (NLCs) prepared, modified with a folate derivative and radiolabeled with technetium-99 m tricarbonyl complex (99 mTc(CO)3 +). Cellular incorporation ratios of radiolabeled nanoparticles (99 mTc(CO)3-PTX-NLC) were investigated in vitro on three cancer cell lines. Additionally in vivo animal studies conducted to evaluate biological behavior of 99 mTc(CO)3-PTX-NLC on female Wistar Albino rats. Biodistribution results showed that the folate derivative modified 99 mTc(CO)3-PTX-NLC had considerably higher uptake in folate receptor positive organs. The data obtained from present study could be useful in the design of biodegradable drug carriers of PTX and folate receptor based tumor imaging agents. © 2016 Elsevier Ltd
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    Multifunctional molecular imaging probes for estrogen receptors: 99mTc labeled diethylstilbestrol (DES) conjugated, cuinp quantum dot nanoparticles (DESCIP)
    (Springer Netherlands, 2017) Moharrami P.; Unak P.; Guldu O.K.; Medine E.I.; Gumuser G.; Bilgin E.S.; Aras O.
    A theranostic nanoparticle was synthesized based on diethylstilbestrol conjugated with phosphate, copper, and indium (DESCIP) and labelled with 99mTc which can be used for SPECT imaging of ER-enriched cancers. In vitro biological activity of 99mTc-DESCIP was examined in breast adenocarcinoma cells (MCF-7), prostatic carcinoma cells (PC-3), and pulmonary epithelial cells (A-549). In vivo lymph node imaging was performed in normal and receptor blocked female New Zealand rabbits. Results demonstrated that 99mTc-DESCIP and DESCIP has potential for imaging ER-enriched tumors such as breast and prostate tumors, and their metastases in the lung, as well as improving management for their therapies. © 2017, Akadémiai Kiadó, Budapest, Hungary.