Yazar "Tekin, Suat" seçeneğine göre listele
Listeleniyor 1 - 12 / 12
Sayfa Başına Sonuç
Sıralama seçenekleri
Öğe An Experimental Insight Into the Role of Agomelatine in Renal Ischemia/Reperfusion Injury(Wiley, 2024) Aykora, Damla; Bahar, Mehmet Refik; Tanbek, Kevser; Ozturk, Dilara Altay; Karaca, Elif; Sandal, Suleyman; Tekin, SuatAcute kidney injury (AKI) is one of the leading causes of chronic kidney disease and accounts for 50%-75% of mortality following renal pathologies or organ transplantation. Ischemia-reperfusion injury (IRI) involves an interrupted blood supply to organs and the kidney; IRI exacerbates AKI development. Owing to several pharmacological treatment methods, AKI still has a poor prognosis, and novel therapeutic options are needed. Agomelatine (AGM) is a melatonin receptor agonist (MT1 and MT2) with increased bioavailability and lipophilicity. In this study, we aimed to investigate the antioxidant and anti-inflammatory effects of AGM in experimental renal IRI via long-term and short-term applications. Sixty male Sprague-Dawley rats were randomly divided into six groups (n = 10): the control, I/R, AGM20S, AGM40S, AGM20L, and AGM40L groups. Following the establishment of the renal IRI model, the rats received agomelatine at 20 and 40 mg/kg orally, and agomelatine solvent (hydroxyethylcellulose) was used as a vehicle. At the end of the experiment, blood samples and renal tissues were harvested for histopathological and biochemical analysis. Urea, creatinine, tumor necrosis factor (TNF-alpha), and interleukin-1 beta (IL-1 beta) levels were measured in blood serum samples. Malondialdehyde (MDA) levels and increased superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSHPx), and total glutathione (GSH) levels were measured in renal tissue supernatants. Our biochemical results indicated that AGM reduced creatinine, TNF-alpha, IL-1 beta, and malondialdehyde levels and increased SOD, CAT, GSHPx, and total GSH levels. Agolematine reduced infiltration, intratubular hemorrhage, and intratubular cast formation histopathologically. Our results suggest that AGM could be a potential therapeutic adjuvant agent for ischemia-reperfusion injury in the kidney and several other organs.Öğe Antioxidant and cytotoxic properties of some new dipeptide-indole conjugates(Wiley, 2023) Gonul, Zeynep; Ozturk, Dilara Altay; Kucukbay, Fatumetuzzehra; Tekin, Suat; Tekin, Zehra; Kucukbay, HasanIn this study, 10 new indole-dipeptide conjugates were synthesized, and their anticancer activity was determined against on A2780 (ovarian cancer cell line) and MCF-7 (breast cancer cell line) cells. Among compounds, 5 and 10 showed better activity against A2780 cell lines than the standard drug docatexel at 0.1 and 1 mu M concentrations, while only compound 5 showed better activity than docatexel, the MCF-7 cell line at 0.1 and 1 mu M concentrations. The antioxidant potencies of the compounds were low in both the DPPH and iron reducing power methods tested when compared to standard antioxidants used in this work.Öğe Central MOTS-c infusion affects reproductive hormones in obese and non-obese rats(Elsevier Ireland Ltd, 2024) Ozturk, Dilara Altay; Erden, Yavuz; Tekin, SuatMOTS-c, a mitochondrial-derived peptide, acts as a systemic hormone and MOTS-c level is inversely correlated with markers of obesity. Obesity is a risk factor for male reproductive physiology and is expressed as an important cause of infertility. In this study, we aimed to determine the effects of MOTS-c, which has been proven in the hypothalamus and testicles, on the actors involved in the reproductive axis. In the study, 80 male Wistar-Albino rats were divided into two main groups, obese and non-obese (n = 40). Rats in the first main group were fed with fatty diet feed and obesity was induced. The second main group was fed with normal diet feed. Each main group was divided into 4 subgroups (Control, Sham, 10 and 100 mu M MOTS-c). The lateral ventricles of the animals in the treatment groups were infused with 10 and 100 mu M MOTS-c (solvent in Sham group) for 14 days. At the end of the experiment, hypothalamic Gonadotropin-Releasing Hormone (GnRH) gene expression level, serum testosterone, Luteinizing hormone (LH) and Follicle stimulating hormone (FSH) levels were determined. MOTS-c infusion caused an increase in GnRH mRNA, protein expression levels and serum testosterone, LH and FSH levels in obese and non-obese rats (p < 0.05). MOTS-c administration more significantly upregulated hormone levels in non-obese rats (p < 0.05). MOTS-c administration increases these hormones, suggesting that MOTS-c may stimulate the reproductive axis. Our results reveal that MOTS-c plays a role in the central regulation of reproduction, as well as causes increased LH, FSH and testosterone release.Öğe Effects of gallic acid and quercetin on the structural, thermal, spectroscopic, in vitro biocompatibility and electronic properties of Au-based hydroxyapatite structure(Elsevier Science Sa, 2024) Keser, Serhat; Dogan, Ahmet; Ates, Tankut; Barzinjy, Azeez A.; Ates, Burhan; Tekin, Suat; Kaygili, OmerThe aim of this study is investigating the structural, thermal, spectroscopic, electronic and biocompatibility properties of the Au-based hydroxyapatites containing quercetin (Q) or gallic acid (GA) at various concentration. Different characterization techniques including; XRD analysis, FTIR and Raman spectroscopies, differential thermal analysis, SEM and EDX analysis were utilized. Cell cytotoxicity test was conducted with the cells of MG63 human bone cancer, hFOB 1.19 human osteoblast and Caco-2 human colon cancer. It has been shown that the utilized samples had no cytotoxic activity on the L-929, hFOB 1.19 and MG-63 cells. However, these samples had cytotoxic activity on Caco-2. The current study showed that the bandgap of the un-doped HAp structure was 4.976 eV. The crystallite size is also affected by Au-doping, type of the as-used biological additive and its amount. Also, the as-produced samples were thermally stable in the range from room temperature to 1000 degrees C. The particle size distributions of the samples were found at variable ranges. The molar ratios were close to the stoichiometric value of 1.667. These novel findings not only expand our appreciation for the role of dopants in materials science but also opens avenues for deliberate engineering of electronic properties for enhanced performance in various applications.Öğe Effects of intracerebroventricular MOTS-c infusion on thyroid hormones and uncoupling proteins(Springer Heidelberg, 2023) Bahar, Mehmet Refik; Tekin, Suat; Beytur, Asiye; Onalan, Ebru Etem; Ozyalin, Fatma; Colak, Cemil; Sandal, SuleymanThis study was conducted to determine the possible effects of intracerebroventricular MOTS-c infusion on thyroid hormones and uncoupling proteins (UCPs) in rats. Forty male Wistar Albino rats were divided into 4 groups with 10 animals in each group: control, sham, 10 and 100 mu M MOTS-c. Hypothalamus, blood, muscle, adipose tissues samples were collected for thyrotropin-releasing hormone (TRH), UCP1 and UCP3 levels were determined by the RT-PCR and western blot analysis. Serum thyroid hormone levels were determined by the ELISA assays. MOTS-c infusion was found to increase food consumption but it did not cause any changes in the body weight. MOTS-c decreased serum TSH, T3, and T4 hormone levels. On the other hand, it was also found that MOTS-c administration increased UCP1 and UCP3 levels in peripheral tissues. The findings obtained in the study show that central MOTS-c infusion is a directly effective agent in energy metabolism.Öğe Exploring the anticancer potential of new 3-cyanopyridine derivatives bearing N-acylhydrazone motif: Synthesis, DFT calculations, cytotoxic evaluation, molecular modeling, and antioxidant properties(Wiley, 2024) Kadi, Ibtissem; Sekerci, Guldeniz; Boulebd, Houssem; Zebbiche, Zineddine; Tekin, Suat; Benarous, Khedidja; Boumoud, Taoues3-Cyanopyridine derivatives are known for exhibiting excellent anticancer activity due to their strong capability to inhibit various biological targets, including Pim-1 kinase, survivin, and tubulin polymerization. On the other hand, N-acylhydrazones (NAH) are known to be a very versatile motif in medicinal chemistry and drug design. Based on these data, we report in this paper, the synthesis of novel 3-cyanopyridines incorporating N-acyl hydrazine scaffold, the evaluation of their cytotoxicity on the breast (MCF-7) and ovarian (A-2780) cancer cell lines and their antioxidant properties. Excluding 4a and 4d, all tested molecules exhibited high cytotoxicity against A-2780, with IC50 values ranging from 1.14 to 1.76 mu M. Conversely, only four molecules 3d, 4b, 4c, and 4d demonstrated cytotoxicity against MCF-7, with IC50 values ranging from 1.14 to 3.38 mu M. On the other hand, all the tested molecules exhibited a moderate antioxidant capacity in both the DPPH and metal chelation assays. Docking and molecular dynamics studies revealed that 2d, 3d, and 4d are potential inhibitors of tubulin and the oe strogen receptor, which may explain their high cytotoxicity. These results are promising to study these newly synthesized 3-cyanopyridine-N-acylhydrazones in depth for use as potential anticancer candidates. A series of novel N-acetylhydrazone motifs-containing 3-cyanopyridine derivatives were synthesized, and their anticancer properties against MCF-7 and A2780 cancer cell lines, along with their antioxidant capacities, were investigated under in vitro conditions. Additionally, density functional theory (DFT) calculations and molecular modeling were conducted in silico. imageÖğe Silyl-functionalised silver rhodium and iridium N-heterocyclic carbene complexes with promising cytotoxicity and antimicrobial potential(Elsevier, 2022) Karatas, Mert Olgun; Keskin, Tuba; Ozdemir, Namik; Kucukbay, Hasan; Tekin, Suat; Mansur, Ahmet; Sandal, SuleymanIn the present study, we have synthesized Ag, Rh, and Ir complexes of a silyl-substituted NHC ligand in order to investigate their biological properties. Firstly, Ag-NHC (2) complex was synthesized by the interaction of Ag2O with benzimidazolium iodide (1). Rh-(3) and Ir-NHC (4) complexes were synthesized by the transmetalation reaction between Ag-NHC and [M(cod)Cl]2 (M = Rh or Ir) dimers. The complexes were characterised by NMR spectroscopy and elemental analyses, and crystal structures of Rh-and Ir-NHC (3 and 4) were also reported. The cytotoxic effects of the complexes were tested on four human cancer cell lines and the antimicrobial activities of the complexes were tested against a panel of nine pathogenic microorganisms. The complexes performed com-parable or better activity than standards, cisplatin and AgNO3.Öğe Synthesis and evaluation of anticancer properties of novel benzimidazole ligand and their cobalt(II) and zinc(II) complexes against cancer cell lines A-2780 and DU-145(Elsevier, 2019) Yılmaz, Ülkü; Tekin, Suat; Buğday, Nesrin; Yavuz, Kemal; Küçükbay, Hasan; Sandal, SüleymanEighteen new cobalt(II) or zinc(II) complexes of benzimidazole bearing 1-benzyl and 2-phenyl moieties were synthesized from the reaction of appropriate benzimidazole ligands and CoCl2 or ZnCl2. Their structural characterizations were done by IR, NMR (1H, 13C) and UV–VIS spectrometers. Cytotoxic activities of eighteen new complexes and three benzimidazole ligands were determined using A-2780 (human ovarian) and DU-145 (human prostate) cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell viability assay for the tested benzimidazole derivatives was performed and the LogIC50 values of the compounds were calculated after a 24-hour treatment. All tested benzimidazole derivatives showed higher or comparable antitumor activity against A-2780 cell lines compared to the standard drug docetaxel with a LogIC50 value of ?0.81?µM (p?Öğe Synthesis of New Cinnamoyl-Amino Acid Conjugates and in Vitro Cytotoxicity and Genotoxicity Studies(Wiley-V C H Verlag Gmbh, 2022) Caliskan, Eray; Ozturk, Dilara Altay; Koran, Kenan; Tekin, Suat; Sandal, Suleyman; Erkan, Sultan; Gorgulu, Ahmet OrhanAmino acid conjugates are described by the reaction of amino acids with bioactive organic groups such as vitamins, hormones, flavonoids, steroids, and sugars. In this study, 12 new conjugates were synthesized by reaction of cinnamic acid derivatives with various amino acids. Cytotoxic studies against four different human cancer cells (MCF7, PC-3, Caco-2, and A2780) were carried out by MTT assay method at five different concentrations. The structure-activity relationships based on the cell viability rates were evaluated. To compare the anticancer activities of the compounds using computational chemistry methods, they were docked against A2780 human ovarian cancer, Michigan Cancer Foundation-7 (MCF7), human prostate cancer (PC-3) and human colon epidermal adenocarcinoma (Caco-2) cell lines and compared with the standard 5-Fluorouracil. The results indicate that the efficacy of cinnamic acid derivatives increases with the presence of amino acids. Comet assay was conducted to understand whether the cell deaths occur through DNA damage mechanism and the results exhibit that the changes in the specified parameters were statistically significant (p<0.05). Our study demonstrated that the compounds cause cell death through the formation of DNA damage mechanism.Öğe Synthesis, Cytotoxicity, Antioxidant Activity, DFT Calculations, and Docking Studies of New Pyridine-Malonate Derivatives as Potential Anticancer Agents(Taylor & Francis Ltd, 2024) Kadi, Ibtissem; Guldeniz, Sekerci; Boulebd, Houssem; Zebbiche, Zineddine; Tekin, Suat; Kucukbay, Fatumetuzzehra; Boumoud, TaouesA series of new pyridine-malonate derivatives were synthesized and fully characterized by 1HNMR, 13CNMR, FTIR, and elemental analysis. Their molecular geometry and chemical reactivity have been investigated using DFT calculations. The cytotoxicity of all synthesized compounds was assessed against two human cancer cell lines (MCF-7 and A-2780) using the MTT assay. Among them, compounds 2a, 2c, 2e, and 2g showed comparable or more potent cytotoxicity toward the MCF-7 cells than the reference drug docetaxel (IC50 = 0.34-0.47 vs. 0.50 mu M). In contrast, only compound 2g showed more potent cytotoxicity against the A-2780 cell line compared to the standard (IC50 = 0.36 vs. 0.42 mu M). The docking study revealed a good affinity for the active site of the human topoisomerase-II beta enzyme, which may explain the promising cytotoxicity of these classes of molecules. The radical scavenging activity of the respective compounds was studied using DPPH radical scavenging assay and it was found that most of the compounds are moderate DPPH radical scavengers compared to the standard drugs BHA and BHT.Öğe Synthesis, in vitro, and in silico studies of novel poly-heterocyclic compounds bearing pyridine and furan moieties as potential anticancer agents(Elsevier, 2023) Kadi, Ibtissem; Sekerci, Güldeniz; Boulebd, Houssem; Zebbiche, Zineddine; Tekin, Suat; Kucukbay, Hasan; Boumoud, TaouesThirteen novel poly-heterocyclic compounds containing pyridine and furan moieties were synthesized and fully characterized by H-1 NMR, 1(3)C NMR, FTIR, and elemental analysis. The optimized geometry of the most stable conformation of the synthesized compounds was determined at the DFT/B3LYP level of theory. Frontier molecular orbitals, molecular electrostatic potential, and atoms in molecules analysis were performed to better understand the electronic properties, reactivity, and intermolecular interactions. The cytotoxicity of all compounds was assessed In vitro against MCF-7 and A-2780 cell lines using the MTT assay. Among them, compounds 2c, 3c, 3d, 4a, and 4c at 0.1 mu M concentration showed more potent cytotoxicity against the MCF-7 cells than the reference drug docetaxel. On the other hand, compounds 2c, 3a, 3c, and 4c are more cytotoxic against the A-2780 cell line compared to the standard at the same concentration. The docking studies revealed an excellent affinity for the active site of the human topoisomeraseII ss enzyme, which may explain the promising cytotoxicity of these classes of molecules. The in silico evaluation of ADMET parameters indicated good pharmacokinetic properties of all the investigated compounds. (c) 2022 Elsevier B.V. All rights reserved.Öğe The first peptide derivatives of dioxybiphenyl-bridged spiro cyclotriphosphazenes: In vitro cytotoxicity activities and DNA damage studies(Academic Press Inc Elsevier Science, 2023) Koran, Kenan; Caliskan, Eray; Ozturk, Dilara Altay; Capan, Irfan; Tekin, Suat; Sandal, Suleyman; Gorgulu, Ahmet OrhanIn this study, we aimed to synthesize new peptide-substituted cyclotriphosphazenes from a series of tyrosine -based peptides and dioxyphenyl-substituted spirocyclotriphosphazenes, and to evaluate their in vitro cytotox-icity and genotoxicity activities. Genotoxicity studies were conducted to understand whether the cytotoxic compounds cause cell death through DNA damage. The structures of the novel series of phosphazenes were characterized by FT-IR, elemental analysis, MS, 1D (31P, 1H, and 13C-APT NMR), and 2D (HETCOR) NMR spectroscopic techniques. In vitro cytotoxic activities were carried out against human breast (MCF-7), ovarian (A2780), prostate (PC-3), colon (Caco-2) cancer cell lines and human normal epithelial cell line (MCF-10A) at different concentrations by using an MTT assay. The compounds showed considerable reductions in cell viability against all human cancer cell lines. Especially, the compounds exhibited notable effects in A2780 cell lines (p < 0.05). The IC50 values of the compounds in the A2780 cell line were calculated to be 1.914 mu M for TG, 20.21 mu M for TV, 20.45 mu M for TA, 4.643 mu M for TP, 5.615 mu M for BTG, 1.047 mu M for BTV, 27.02 mu M for BTA, 0.7734 mu M for BTP, 21.5 mu M for DTG, 1.65 mu M for DTV, 2.89 mu M for DTA and 4.599 mu M for DTP. DNA damage studies of the compounds were conducted by the comet assay method using tail length, tail density, olive tail moment, head length, and head density parameters, and the results showed that the cell death occurred through DNA damage mechanism. In a nutshell, these compounds show promising cytotoxic effects and can be considered powerful candidate molecules for pharmaceutical applications.
