Browsing by Author "Karatay, KB"

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    Radiolabeling fingolimod with technetium-99 m and evaluating its biological affinity by in vitro method
    Uygur, E; Parlak, Y; Karatay, KB; Sezgin, C; Gümüser, FG; Müftüler, FZB
    Fingolimod (FTY-720) is the first oral medication approved by the food and drug administration (FDA) for the treatment of multiple sclerosis. It acts on the central nervous system by crossing the blood-brain barrier and binding to sphingosine-1-phosphate receptors (S1PRs). FTY-720 protects against neural damage caused by mitochondrial dysfunction and cytotoxicity by modulating S1PR1. In this study, FTY-720 was radiolabeled with technetium-99 m [Tc-99m]Tc and the biological affinity of [Tc-99m]Tc-FTY-720 was assessed using in vitro methods. The radiochemical yield and stability of [Tc-99m]Tc-FTY-720 was over 95% during 4 h. [Tc-99m]Tc-FTY-720 showed uptake on the SH-SY5Y cell line.
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    Investigation of the Radiolabelling Potential of the Aurora A Kinase Inhibitor Alisertib with Iodine-123 [123I]
    Uygur, E; Sezgin, C; Akdag, BY; Özbey, T; Parlak, Y; Karatay, KB; Gümüser, FG; Müftüler, FZB
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    Investigation of Bioactivity of Estragole Isolated from Basil Plant on Brain Cancer Cell Lines Using Nuclear Method
    Avcibasi, U; Dewa, MT; Karatay, KB; Kilcar, AY; Muftuler, FZB
    Background In recent years, there has been a significant increase in studies investigating the potential use of plant-origin products in the treatment and diagnosis of different types of cancer. Methods In this study, Estragole (EST) was isolated from basil leaves via ethanolic extraction using an 80% ethanol concentration. The isolation process was performed using the High Performance Liquid Chromatography (HPLC) method. The EST isolated from the basil plant was radiolabeled with I-131 using the iodogen method. Quality control studies of the radiolabeled EST (I-131-EST) were carried out by using Thin Layer Radio Chromatography (TLRC). Next, in vitro cell, culture studies were done to investigate the bio-affinity of plant-originated EST labeled with I-131 on human medulloblastoma (DAOY) and human glioblastoma-astrocytoma (U-87 MG) cell lines. Finally, the cytotoxicity of EST was determined, and cell uptake of I-131-EST was investigated on cancer cell lines by incorporation studies. Results As a result of these studies, it has been shown that I-131-EST has a significant uptake on the brain cells. Conclusion This result is very satisfying, and it has encouraged us to do in vivo studies for the molecule in the future.
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    Synthesis of Novel Plant-Derived Encapsulated Radiolabeled Compounds for the Diagnosis of Parkinson's Disease and the Evaluation of Biological Effects with In Vitro/In Vivo Methods
    Uygur, E; Karatay, KB; Dervis, E; Evren, V; Kilçar, AY; Güldü, OK; Sezgin, C; Çinleti, BA; Tekin, V; Muftuler, FZB
    Parkinson's disease (PD) is a neurodegenerative disorder that affects millions of individuals globally. It is characterized by the loss of dopaminergic neurons in Substantia Nigra pars compacta (SNc) and striatum. Neuroimaging techniques such as single-photon emission computed tomography (SPECT), positron emission tomography (PET), and magnetic resonance imaging (MRI) help diagnosing PD. In this study, the focus was on developing technetium-99 m ([Tc-99m]Tc) radiolabeled drug delivery systems using plant-derived compounds for the diagnosis of PD. Madecassoside (MA), a plant-derived compound, was conjugated with Levodopa (L-DOPA) to form MA-L-DOPA, which was then encapsulated using Poly Lactic-co-Glycolic Acid (PLGA) to create MA-PLGA and MA-L-DOPA-PLGA nanocapsules. Extensive structural analysis was performed using various methods such as Fourier-transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectroscopy (NMR), liquid chromatography-mass spectrometry (LC-MS), thin layer chromatography (TLC), high performance liquid chromatography (HPLC), dynamic light scattering (DLS), and scanning electron microscopy (SEM) to characterize the synthesized products. Radiochemical yields of radiolabeled compounds were determined using thin layer radio chromatography (TLRC) and high performance liquid radio chromatography (HPLRC) methods. In vitro cell culture studies were conducted on human neuroblastoma (SH-SY5Y) and rat pheochromocytoma (PC-12) cell lines to assess the incorporation of [Tc-99m]Tc radiolabeled compounds ([Tc-99m]Tc-MA, [Tc-99m]Tc-MA-L-DOPA, [Tc-99m]Tc-MA-PLGA and [Tc-99m]Tc-MA-L-DOPA-PLGA) and the cytotoxicity of inactive compounds (MA and MA-L-DOPA compounds and encapsulated compounds (MA-PLGA and MA-L-DOPA-PLGA). Additionally, the biodistribution studies were carried out on healthy male Sprague-Dawley rats and a Parkinson's disease experimental model to evaluate the compounds' bioactivity using the radiolabeled compounds. The radiochemical yields of all radiolabeled compounds except [Tc-99m]Tc-L-DOPA-PLGA were above 95% and had stability over 6 h. The cytotoxic effects of all substances on SH-SY5Y and PC-12 cells increase with increasing concentration values. The uptake values of PLGA-encapsulated compounds are statistically significant in SH-SY5Y and PC-12 cells. The biodistribution studies showed that [Tc-99m]Tc-MA is predominantly retained in specific organs and brain regions, with notable uptake in the prostate, muscle, and midbrain. PLGA-encapsulation led to higher uptake in certain organs, suggesting its biodegradable nature may enhance tissue retention, and surface modifications might further optimize brain penetration. Overall, the results indicate that radiolabeled plant-derived encapsulated drug delivery systems with [99mTc]Tc hold potential as diagnostic agents for PD symptoms. This study contributes to the advancement of drug delivery agents in the field of brain research.
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    The radiolabeling of [161Tb]Tb-PSMA-617 by a novel radiolabeling method and preclinical evaluation by in vitro/in vivo methods
    Uygur, E; Sezgin, C; Parlak, Y; Karatay, KB; Arikbasi, B; Avcibasi, U; Toklu, T; Barutça, S; Harmansah, C; Sözen, TS; Maus, S; Scher, H; Aras, O; Gümüser, FG; Muftuler, FZB
    Prostate cancer (PC) is the most prevalent cancer in elderly men, exhibiting a positive correlation with age. As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapies have emerged. Recently introduced for treating micrometastatic foci, Terbium-161 ([Tb-161]) has shown great promise in prostate cancer treatment. This study investigated the in vitro and in vivo cytotoxicity of Terbium-161 ([Tb-161])-radiolabeled prostate-specific membrane antigen (PSMA)-617. [Tb-161]Tb-PSMA-617 (7.4 MBq/nmol) demonstrated a radiochemical yield of 97.99 +/- 2.01% and hydrophilicity. [Tb-161]Tb-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 h. In vitro, [Tb-161]Tb-PSMA-617 exhibited cytotoxicity on LNCaP cells but not on PC3 cells. In vivo, scintigraphy imaging visualized the accumulation of [Tb-161]Tb-PSMA-617 in the prostate, kidneys, and bladder. The results suggest that [Tb-161]Tb-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.