Browsing by Author "Bilgin E.S."

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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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    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.
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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.
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    Thymoquinone glucuronide conjugated magnetic nanoparticle for bimo-dal imaging and treatment of cancer as a novel theranostic platform
    (Bentham Science Publishers, 2021) İnce İ.; Müftüler Z.B.; Medine E.İ.; Güldü Ö.K.; Takan G.; Ergönül A.; Parlak Y.; Yıldırım Y.; Çakar B.; Bilgin E.S.; Aras Ö.; Göker E.; Ünak P.
    Background: Theranostic oncology combines therapy and diagnosis and is a new field of medicine that specifically targets the disease by using targeted molecules to destroy the cancer-ous cells without damaging the surrounding healthy tissues. Objective: We aimed to develop a tool that exploits enzymatic TQ release from glucuronide (G) for the imaging and treatment of lung cancer. We added magnetic nanoparticles (MNP) to enable magnetic hyperthermia and MRI, as well as 131I to enable SPECT imaging and radionuclide thera-py. Methods: A glucuronide derivative of thymoquinone (TQG) was enzymatically synthesized and conjugated with the synthesized MNP and then radioiodinated with 131I. New Zealand white rab-bits were used in SPECT and MRI studies, while tumor modeling studies were performed on 6–7-week-old nude mice utilized with bioluminescence imaging. Results: Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR) spectra confirmed the expected structures of TQG. The dimensions of nanoparticles were below 10 nm and they had rather polyhedral shapes. Nanoparticles were radioiodinated with 131I with over 95% yield. In imaging studies, in xenograft models, tumor volume was significantly reduced in TQGMNP-treated mice but not in non-treated mice. Among mice treated intravenously with TQGMNP, xenograft tumor models disappeared after 10 and 15 days, respectively. Conclusion: Our findings suggest that TQGMNP in solid, semi-solid and liquid formulations can be developed using different radiolabeling nuclides for applications in multimodality imaging (SPECT and MRI). By altering the characteristics of radionuclides, TQGMNP may ultimately be used not only for diagnosis but also for the treatment of various cancers as an in vitro diagnostic kit for the diagnosis of beta glucuronidase-rich cancers. © 2021 Bentham Science Publishers.
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    Development of a Radiolabeled Folate-Mediated Drug Delivery System for Effective Delivery of Docetaxel
    (American Chemical Society, 2023) Çetin O.; Güngör B.; İçhedef C.; Parlak Y.; Bilgin E.S.; Üstün F.; Durmuş Altun G.; Başpınar Y.; Teksöz S.
    Many preclinical studies are carried out with the aim of developing new formulations for the effective delivery of taxane class drugs, one of the most important anticancer drugs used clinically today. In this study, a radiolabeled folate-mediated solid lipid magnetic nanoparticle (SLMNP) system was developed by loading superparamagnetic iron oxide nanoparticles (MNP) and docetaxel (DTX) into the solid lipid nanoparticles as a drug delivery system that will function both in cancer treatment and diagnosis. For this purpose, first, SLMNP was synthesized by the hot homogenization method, and the surface of the particles was modified with a folate derivative to carry the particles to tissues with folate receptors. The synthesized magnetic solid lipid nanoparticles were loaded with DTX, and then radiolabeling was carried out with technetium-99 m (99mTc-DTX-SLMNP). Structural characteristics of these nanoparticles were determined by characterization methods. According to the TEM images of MNPs, SLN, and SLMNPs, MNPs were observed between 25and 35 nm, SLNs between 400 and 500 nm, and SLMNPs between 350 and 450 nm. The drug entrapment efficiency of SLMNPs loaded with DTX was found to be 19%, and the percentage efficiency of radiolabeling was found to be 98.0 ± 2.0%. The biological behavior of this radiolabeled system was investigated in vitro and in vivo. Folate receptor-positive SKOV-3 and folate receptor-negative A549 cancer cell lines were studied. The IC50 values of DTX-SLMNP in SKOV-3 and A549 cells were 50.21 and 172.27 μM at 48 h, respectively. Gamma camera imaging studies of 99mTc-DTX-SLMNP and magnetically applied 99mTc-DTX-SLMNP compounds were performed on tumor-bearing CD-1 nude mice. The uptake in the folate receptor-positive tumor region was higher than that in the folate receptor negative tumor region. We proposed that the drug delivery system we prepared in this study be evaluated for preclinical studies of new drug carrier formulations of the taxane class of anticancer drugs. © 2023 The Authors. Published by American Chemical Society.