Browsing by Subject "radiochromatography"

Now showing 1 - 7 of 7
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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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    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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    Synthesis and biodistribution of novel magnetic-poly(HEMA-APH) nanopolymer radiolabeled with iodine-131 and investigation its fate in vivo for cancer therapy
    (Kluwer Academic Publishers, 2013) Avcibaşi U.; Avcibaşi N.; Akalin H.A.; Ediz M.; Demiroǧlu H.; Gümüşer F.G.; Özçalişkan E.; Türkcan C.; Uygun D.A.; Akgöl S.
    Herein, we investigated the biological uptake, distribution, and radiopharmaceutical potential of a novel molecule based on 2-hydroxyethyl methacrylate (HEMA) and anilinephtalein (APH) in the metabolism of Albino Wistar rats. In order to achieve this, we synthesized APH using organic synthesis methods and copolymerized APH with HEMA using a common polymerization method, surfactant-free emulsion polymerization. In the presence of Fe3O 4 particles, we obtained a new generation magnetic-nano-scale polymer, magnetic-poly(HEMA-APH). This new molecule was chemically identified and approved by several characterization methods using Fourier transform infrared spectroscopy, scanning electron microscope, energy dispersive X-ray spectroscopy, electron spin resonance, atomic force microscope, and Zeta particle-size analysis. To evaluate the biological activity in live metabolism and anti-cancer potential of mag-poly(HEMA-APH), molecule was radioiodinated by a widely used labeling technique, iodogen method, with a gamma diffuser radionuclide, 131I. Thin-layer radiochromatography experiments demonstrated that 131I binded to nanopolymer with the labeling yield of 90 %. Lipophilicity and stability experiments were conducted to determine the condition of cold and labeled mag-poly(HEMA-APH) in rat blood and lipid medium. Results demonstrated that radioiodinated molecule stayed as an intact complex in rat metabolism for 24 h and experimental lipophilicity was determined as 0.12 ± 0.02. In vivo results obtained by imaging and biological distribution experiments indicated that mag-poly(HEMA-APH) labeled with 131I [131I-mag-poly(HEMA-APH)] highly incorporated into tissues of the uterus, the ovarian, the prostate, and the lungs in rat metabolism. Based on these results, it may be evaluated that novel mag-poly(HEMA-APH) molecule labeled with 131I is a compound which has a significant potential for being used as an anti-cancer agent. Certain results can only be obtained whether this molecule is applied to adenocarcinoma cell models and tumor-bearing animals. © 2013 Springer Science+Business Media Dordrecht.
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    Radiolabeling of new generation magnetic poly(HEMA-MAPA) nanoparticles with 131I and preliminary investigation of its radiopharmaceutical potential using albino Wistar rats
    (John Wiley and Sons Ltd, 2013) Avcibaşi U.; Demiroǧlu H.; Ediz M.; Akalin H.A.; Özçalişkan E.; Şenay H.; Türkcan C.; Özcan Y.; Akgöl S.; Avcibaşi N.
    In this study, N-methacryloyl-l-phenylalanine (MAPA) containing poly(2-hydroxyethylmethacrylate) (HEMA)-based magnetic poly(HEMA-MAPA) nanobeads [mag-poly(HEMA-MAPA)] were radiolabeled with 131I [ 131I-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of 131I-mag-poly(HEMA-MAPA) was investigated. Quality control studies were carried out by radiochromatographic method to be sure that 131I binded to mag-poly(HEMA-MAPA) efficiently. In this sense, binding yield of 131I-mag-poly(HEMA-MAPA) was found to be about 95-100%. In addition to this, optimum radiodination conditions for 131I-mag-poly(HEMA- MAPA) were determined by thin-layer radiochromatography studies. In addition to thin-layer radiochromatography studies, lipophilicity (partition coefficient) and stability studies for 131I-mag-poly(HEMA-MAPA) were realized. It was determined that lipophilicities of mag-poly(HEMA-MAPA) and 131I-mag-poly(HEMA-MAPA) were 0.12 ± 0.01 and 1.79 ± 0.76 according to ACD/logP algorithm program, respectively. Stability of the radiolabeled compound was investigated in time intervals given as 0, 30, 60, 180, and 1440 min. It was found that 131I-mag-poly(HEMA-MAPA) existed as a stable complex in rat serum within 60 min. After that, biodistribution and scintigraphy studies were carried out by using albino Wistar rats. It was determined that the most important 131I activity uptake was observed in the breast, the ovary, and the pancreas. Scintigraphy studies well supported biodistribution results. Copyright © 2013 John Wiley & Sons, Ltd.
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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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    Radiosynthesis and biodistribution of 99mTc-trimethoprim: A novel radiolabeled antibiotic for bacterial infection imaging using experimental animals; [ 99mTc-Trimethoprim’in radyosentezi ve biyodağılımı: Deney hayvanları kullanılarak bakteriyel enfeksiyon görüntüleme için yeni bir radyoişaretli antibiyotik]
    (Veteriner Fakultesi Dergisi, 2018) Demiroğlu H.; Topal G.; Parlak Y.; Gümüşer F.G.; Türköz E.U.; Tekin V.; Ateş B.; Ünak P.; Avcibaşi U.
    In the present article, we focused on the radiolabeling and evaluation of 99mTc–TMH complex as a potential candidate for infection imaging in vivo. For this; Trimethoprim (TMH) used to treat bacterial infections was investigated to label with99mTc. Labeling was performed using thin (II) chloride as a reducing agent at room temperature for 1 h and radiochemical analysis involved thin layer radiochromatography (TLRC) and high pressure liquid radiochromatograpy (HPLRC) methods. The stability of labeled antibiotic was checked in the presence of rat blood serum at 37.C up to 180 min. The maximum radiolabeling yield was found to be 96±2% and remained constant at more than 85±1% even in rat serum for 180 min after radiolabeling. Static image of 99mTc-TMH in male rats demonstrated that important radiation signals are present in the infected site at first glance in 30 min. After 30 min the uptake of the 99mTc-TMH as ID/g% in the infected muscle (INM) and normal muscle (NM) of the rats were 7.5±1.5% and 5.00±1.2%, respectively. In the INM/NM ratio a desirable behavior was observed as the values for the INM/ NM increased up to 10.6. 99mTc-TMH prepared with high yield is able to localize well in the bacterially infected muscle of the rats. As a result,99mTc-TMH may be developed as a radiopharmaceutical agent to distinguish infection from inflammation by nuclear imaging. © 2018, Veteriner Fakultesi Dergisi. All rights reserved.
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    Evaluation of new 99mTc(CO)3 + radiolabeled glycylglycine In Vivo
    (Bentham Science Publishers, 2019) Şenışık A.M.; İçhedef Ç.; Kılçar A.Y.; Uçar E.; Arı K.; Parlak Y.; Bilgin E.S.; Teksöz S.
    Background: Peptide-based agents are used in molecular imaging due to their unique properties, such as rapid clearance from the circulation, high affinity and target selectivity. Many of the radiolabeled peptides have been clinically experienced with diagnostic accuracy. The aim of this study was to investigate in vivo biological behavior of [99mTc(CO)3(H2O)3]+ radiolabeled glycylglycine (GlyGly). Methods: Glycylglycine was radiolabeled with a high radiolabeling yield of 94.69±2%, and quality control of the radiolabeling process was performed by thin layer radiochromatography (TLRC) and High-Performance Liquid Radiochromatography (HPLRC). Lipophilicity study for radiolabeled complex (99mTc(CO)3-Gly-Gly) was carried out using solvent extraction. The in vivo evaluation was performed by both biodistribution and SPECT imaging. Results: The high radiolabelling yield of 99mTc(CO)3-GlyGly was obtained and verified by TLRC and HPLRC as well. According to the in vivo results, SPECT images and biodistribution data are in good accordance. The excretion route from the body was both hepatobiliary and renal. Conclusion: This study shows that 99mTc(CO)3-GlyGly has the potential to be used as a peptide-based imaging agent. Further studies, 99mTc(CO)3-GlyGly can be performed on tumor-bearing animals. © 2019 Bentham Science Publishers.