Browsing by Author "Baspinar, Y"

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    Serum hypoxia-inducible factor-2: A candidate prognostic biomarker for laryngeal cancer
    Eskiizmir, G; Koçal, GÇ; Uysal, T; Ellidokuz, H; Baspinar, Y
    Objectives To determine the serum hypoxia-inducible factor-1, -2 and -3 (HIF-1, -2 and -3) levels in patients with laryngeal neoplasm, and to investigate their role in differential diagnosis, prediction of tumour characteristic and extension, and prognosis and survival. Study Design Prospective, cohort study at a tertiary referral centre. Settings The study was conducted in a tertiary medical centre. Participants Patients with benign, premalignant and malignant laryngeal neoplasms were included. Sixty-four patients with a laryngeal neoplasm were enrolled. Main Outcome Measures Serum HIF-1, -2 and -3 levels were measured from blood samples that were drawn before treatment, using ELISA. Results A statistically significant difference between benign (HIF-1, -2, -3:4046,1 pg/mL; 2581,5 pg/mL; 1321,0 pg/mL), premalignant (HIF-1, -2, -3:3630,3 pg/mL; 3229,7 pg/mL; 2549,8 pg/mL) and malignant (HIF-1, -2, -3:3576,7 pg/mL; 2595,8 pg/mL; 1106,3 pg/mL) laryngeal neoplasms was not detected when serum HIF-1, -2 and -3 levels were compared. However, high serum HIF-2 level adversely affected survival and locoregional control and had more than 7-fold increase in hazard ratio. Moreover, serum HIF-2 was an independent prognostic factor for 2-year overall, disease-free, distant metastasis-free survival and locoregional control. Conclusion This is the first clinical study in which the diagnostic, predictive and prognostic roles of hypoxia-related biomolecules were examined in laryngeal neoplasms. Hypoxia-inducible factor-2 is a prognostic factor in larynx cancer irrespective of treatment modality.
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    Formulation, characterization, cytotoxicity and Salmonella/microsome mutagenicity (Ames) studies of a novel 5-fluorouracil derivative
    Karayildirim, ÇK; Kotmakçi, M; Halay, E; Ay, K; Baspinar, Y
    5-Fluorouracil is one of the first line drugs for the systemic therapy of solid tumors like breast, colorectal, oesophageal, stomach, pancreatic, head and neck. It could be shown that sugars can improve the absorption across cell membranes and can help to bypass some pharmacokinetic problems. Carbohydrates as most common organic molecules are an important issue of plant and animal metabolisms. They are non toxic and have important duties in the body like participating in DNA and RNA synthesis and being responsible for energy production. In addition, they have many hydroxyl, aldehyde and ketone groups that attract attention for synthesis as a potential drug derivative. 1,2,3,-Triazole compounds have also important role in heterocyclic chemistry because of their pharmaceutical properties and their high reactivity, which could be used as a building block for complex chemical compounds. In this study, following the Click Reaction of 5-FU and tetra-O-acetylglycose the 5-fluorouracil derivative 1-[{1'-(2 '',3 '',4 '',6 ''-tetra-O-acetyl-beta-D-glycopyronosyl)-1'H-1',2',3'-triazole-4'-yl} methyl] 5-fluorouracil was synthesized. Following, a micellar formulation of 5-Fluorouracil derivative was prepared and characterized in terms of particle size, polydispersity index, zeta potential, refractive index and pH. Furthermore, the cytotoxicity and mutagenicity of the 5-fluorouracil derivative was investigated using an in vitro cell culture model and the AMES test. According to the results of this study, the novel 5-fluorouracil derivative could be a drug candidate for the therapy of cancer and needs further in vivo investigations. (C) 2018 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
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    Development of a Radiolabeled Folate-Mediated Drug Delivery System for Effective Delivery of Docetaxel
    Çetin, O; Güngör, B; Içhdef, C; Parlak, Y; Bilgin, ES; Üstün, F; Altun, GD; Baspinar, Y; Teksöz, S
    Many preclinical studies are carried out with the aimof developingnew 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 magneticnanoparticle (SLMNP) system was developed by loading superparamagneticiron oxide nanoparticles (MNP) and docetaxel (DTX) into the solidlipid nanoparticles as a drug delivery system that will function bothin cancer treatment and diagnosis. For this purpose, first, SLMNPwas synthesized by the hot homogenization method, and the surfaceof the particles was modified with a folate derivative to carry theparticles to tissues with folate receptors. The synthesized magneticsolid lipid nanoparticles were loaded with DTX, and then radiolabelingwas carried out with technetium-99 m (Tc-99m-DTX-SLMNP).Structural characteristics of these nanoparticles were determinedby characterization methods. According to the TEM images of MNPs,SLN, and SLMNPs, MNPs were observed between 25and 35 nm, SLNs between400 and 500 nm, and SLMNPs between 350 and 450 nm. The drug entrapmentefficiency of SLMNPs loaded with DTX was found to be 19%, and thepercentage efficiency of radiolabeling was found to be 98.0 & PLUSMN;2.0%. The biological behavior of this radiolabeled system was investigated in vitro and in vivo. Folate receptor-positiveSKOV-3 and folate receptor-negative A549 cancer cell lines were studied.The IC50 values of DTX-SLMNP in SKOV-3 and A549 cells were50.21 and 172.27 & mu;M at 48 h, respectively. Gamma camera imagingstudies of Tc-99m-DTX-SLMNP and magnetically applied Tc-99m-DTX-SLMNP compounds were performed on tumor-bearing CD-1nude mice. The uptake in the folate receptor-positive tumor regionwas higher than that in the folate receptor negative tumor region.We proposed that the drug delivery system we prepared in this studybe evaluated for preclinical studies of new drug carrier formulationsof the taxane class of anticancer drugs.