Browsing by Author "Celikezen, Fatih Caglar"

Now showing 1 - 12 of 12

Characterisation of Carbonic Anhydrase Purified From Erythrocytes of Van Cat (Felis Catus)
(Parlar Scientific Publications (p S P), 2013) Soyler, Muhammed; Demir, Halit; Celikezen, Fatih Caglar; Celik, Ismail; Akan, Zafer
Carbonic anhydrase plays different roles in various tissues. It is a key enzyme that regulates the acid-base homeostasis under both normal and pathological conditions. In this study, carbonic anhydrase (CA; E.C 4.2.1.1) was purified from erythrocytes of Van cat (Fells catus) by affinity chromatography. The purification rate was found to be 367.21-fold. SDS-PAGE (sodium dodecyl sulfate-polyacrylamide gel electrophoresis) was used to control the purity of enzyme. Optimal pH, ionic strength, and temperature for enzyme activity were determined. Molecular weight of CA was identified to be about 30 kDa by SDS-PAGE. Optimal pH and temperature were 8.0 and 40 degrees C. The highest activity was found at a concentration of 0.12 M (NH4)(2)SO4 as ionic strength. The Van cat (Fells catus) is a unique and endemic species; therefore, the characterisations of carbonic anhydrase enzyme are crucial. This study will shed light to future studies regarding the Van cat.
Cytoprotective Effects of Boric Acid and Coenzyme Q10 Therapy on Induced Pulmonary Fibrosis in Response To Intratracheal Administration of Bleomycin in Rats
(Parlar Scientific Publications (p S P), 2013) Oto, Gokhan; Ekin, Suat; Celikezen, Fatih Caglar; Yener, Zabit; Tanritanir, Pinar; Ozdeinir, Hulya; Bayramoglu, Mahire
This study was designed to examine cytoprotective effects of boric acid and CoQ(10) on a model of bleomycin-induced lung fibrosis. A total of 32 female Wistar albino rats (200-250 g, n=8) were randomly divided into four groups (control, bleomycin, bleomycin + boric acid, and bleomycin + boric acid + CoQ(10)). Rats in the control group were given equal volumes of saline intratracheally. Lung fibrosis was induced by intratracheal administration of bleomycin hydrochloride (7.5 mg/kg in 0.9% NaCl) to rats under anaesthesia. In the treatment groups, the rats were treated with boric acid (10 mg/kg per day; perorally) and CoQ(10) (4 mg/kg per day; intraperitoneally) for 30 days. All animals were sacrificed at the end of the experiment. The lung, liver, kidney, and spleen tissues were excised, taken for histopathological evaluation, and stored for the measurement of SOD and GSH-Px activities with trace element and minerals. As a result, boric acid and boric acid + CoQ(10) had preventive roles on bleomycin-induced lung fibrosis in rats.
Determination of in Vitro Antioxidant, Antimicrobial Properties and Cox-1/Cox-2 Enzyme Inhibition Activity of Capparis Sicula
(Kahramanmaras Sutcu Imam Univ Rektorlugu, 2023) Acar, Nagihan; Celikezen, Fatih Caglar; Sahin, Ibrahim Halil; Firat, Mehmet; Kocyigit, Recep; Kirecci, Oguz Ayhan
Since synthetic drugs cause many side effects and have a high cost, there has been increasing interest in the development of herbal based drugs that have fewer side effects and are relatively inexpensive. Capparis sicula is traditionally used in the treatment of some diseases among people. For this purpose, the antioxidant and antimicrobial properties of the methanol extract of the Capparis sicula plant and its inhibitory effects on COX-1 and COX-2 enzymes were investigated. In the study, the antioxidant properties of the Capparis sicula plant were determined by DPPH and CUPRAC methods, while its antimicrobial properties were determined by the disk diffusion method. The effect of Capparis sicula on COX-1 and COX-2 enzymes was determined colorimetrically using commercial kits. The results showed that Capparis sicula had a significant antioxidant effect, but did not have any antimicrobial effect on standard strains of Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Candida albicans. In addition, the inhibitory effect on the COX-1 enzyme was 4.23% for the first time, and the inhibition effect on the COX-2 enzyme was determined as 23.21%. As a result, the pharmaceutical, food and cosmetic industries can use Capparis sicula as an important source of natural raw materials.
The Effects of Pretreatment With Lithium Metaborate Dihydrate on Lipid Peroxidation and Ca, Fe, Mg, and K Levels in Serum of Wistar Albino Male Rats Exposed To Cd
(Springer Heidelberg, 2020) Tasdemir, Muhammed; Celikezen, Fatih Caglar; Oto, Gokhan; Ozbey, Fahrettin
Boron and boron compounds have beneficial biological effects. Lithium metaborate dihydrate (LMBDH) is used in many branches of industry. Despite its wide industrial use, there is limited information about its biological effects on antioxidant defense system and trace element homeostasis. Therefore, the aim of this study was to evaluate the in vivo protective effects of LMBDH against CdCl2-induced oxidative stress and imbalance of some bioelements for the first time. In the study, totally 20 Wistar albino male rats were used. The rats were fed with pellet food and water ad libitum and divided into four groups including five rats in each. Group I was control group (standard pellet food + water + normal saline), Group II was CdCl2 (4.58 mg/kg/body weight/intraperitoneally/single dose), Group III was LMBDH (15 mg/kg/body weight/day orally, for 5 days), Group IV was CdCl2 (4.58 mg/kg/body weight/intraperitoneally/single dose in fifth day), and LMBDH (15 mg/kg/body weight/day orally for 5 days). The results showed that CdCl2 treatment increased blood MDA level and decreased antioxidant enzyme activities and the level of blood GSH compared to control group. Pretreatment with LMBDH significantly decreased MDA levels and increased SOD activity (p < 0.05). In addition, Ca, Fe, and K levels decreased in LMBDH pretreatment group in different statistically levels. However, Mg levels showed an increase in LMBDH pretreatment group. As a result, LMBDH pretreatment decreased MDA status and supported antioxidant system by increasing SOD activity. In addition, it did not exhibit an ameliorative effect on measured bioelement homeostasis.
In Vitro Evaluation of Selective Cytotoxic Activity of Chaerophyllum Macropodum Boiss. on Cultured Human Sh-Sy5y Neuroblastoma Cells
(Springer, 2022) Celikezen, Fatih Caglar; Turkez, Hasan; Firat, Mehmet; Arslan, Mehmet Enes; Oner, Sena
Neuroblastoma is the most common solid tumor in children. New treatment approaches are needed because of the harmful side effects and costs of the methods used in the treatment of neuroblastoma. Medicinal and aromatic plants are important for new treatment approaches due to their minimal side effects and economic advantages. Therefore, the present study was carried out to examine the cytotoxic effect of Chaerophyllum macropodum extract on human neuroblastoma (SH-SY5Y) and fibroblast (HDFa) cell lines. 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase release (LDH) assays were used to determine the cytotoxic effect of C. macropodum. The extracts were analyzed for their phenolic content by HPLC-PDA. Major components were determined as 63.600% o-coumaric acid, 15.606% catechine hydrate, 8.713% rosmarinic acid, 4.376% clorogenic acid, and 3.972% salicylic acid. The obtained results from cytotoxicity testing revealed that C. macropodum exerted a significant cytotoxic effect on human neuroblastoma cells at all tested concentrations (p < 0.05). But it did not lead to any cytotoxic potential on human fibroblasts. As a result, the obtained data clearly revealed C. macropodum exerted a selective cytotoxic action on neuroblastoma cells for the first time.
In Vitro Inhibitor Effect and Molecular Docking of Thiamine (Vitamin B1), Riboflavin (Vitamin B2), and Reference Inhibitor Captopril on Angiotensin-Converting Enzyme Purified From Sheep Plasma
(Taylor & Francis Ltd, 2024) Ciftci, Muhammed Haluk; Turkoglu, Vedat; Bas, Zehra; Celikezen, Fatih Caglar
Objective: Angiotensin-converting enzyme (ACE, EC 3.4.15.1) is a very important factor in the regulation of blood pressure. Also, the inhibition of ACE with natural compounds has been a very important research area in the treatment of high blood pressure. ACE was purified and characterized from sheep plasma. Molecular docking studies and the inhibition effect of thiamine, riboflavin, and captopril on ACE were investigated. Methods: Herein, ACE was purified from sheep plasma by affinity chromatography. The effect of thiamine and riboflavin on ACE was researched. Molecular docking studies were performed to understand the molecular interactions between thiamine, riboflavin, and captopril with ACE. Results: The purification coefficient was found to be 8636 fold. The binding energy of thiamine, riboflavin, and captopril was found to be -6.7 kcal/mol, -8.1 kcal/mol, and -5.5 kcal/mol, respectively. Thiamine conformed to three conventional hydrogen bonds with ASP:415, HIS:513, and LYS:454. Riboflavin formed four conventional hydrogen bonds with GLN:281, GLU:376, THR:282, and TYR:520. Captopril formed two conventional hydrogen bonds with ARG:124, one conventional hydrogen bond with TYR:62 and ASN:85, and one carbon-hydrogen bond with ASN:66. Molecular docking results showed that thiamine, riboflavin, and captopril interacted with ACE through hydrogen bonding and hydrophobic interactions. Thiamine and riboflavin indicated significant inhibition effects on ACE. The IC50 values of thiamine, riboflavin, and captopril were found as 960.56 mu M, 11.02 mu M, and 1.60 nM, respectively. K-i values for thiamine, riboflavin, and captopril were determined as 1352.04 mu M, 12.30 mu M, and 1.06 nM, respectively. Conclusion: In this work, it was concluded that thiamine and riboflavin may have preventive and therapeutical impacts against high blood pressure with their ACE inhibitor effect. Thiamine and riboflavin showed a lower inhibitory effect with a higher IC50 than captopril. However, when the inhibitory effect of thiamine and riboflavin vitamins is compared to captopril, it is concluded that they may be natural inhibitors with fewer side effects.
The Investigation of Hawthorn (Crataegus Orientalis) Plant's Inhibition Effect on Angiotensin Converting Enzyme and in Silico Studies
(Taylor & Francis Ltd, 2024) Yavuz, Mahmut; Celikezen, Fatih Caglar; Firat, Mehmet; Bas, Zehra; Turkoglu, Vedat
Hawthorn plant is used among people due to its cardiovascular, anti-inflammatory, and antihistamine properties. But no scientific study has been done about Crataegus orientalis (Mill.) M.Bieb. The presented study was planned to determine the effects of ethanol and n-hexane extracts of Crataegus orientalis leaves on human plasma ACE enzyme. In the study, the effect of plant extracts on ACE was studied by the spectrophotometric method. The chemical composition of the plant extracts was determined by HPLC-DAD analyses. In addition, molecular doking and ADME prediction studies were carried out. As a result, the obtained data showed that Crataegus orientalis could have an important place in the pharmaceutical industry and drug discovery studies, as it supports the traditional use of Crataegus orientalis as hypotensive. The results of the molecular docking studies revealed that the interactions of the selected compounds with the human ACE enzyme caused inhibition. [GRAPHICS]
Investigation of Protective Effects of Lithium Borate on Spermatogenesis and Testes Histopathology Against Cadmium-Induced Acute Toxicity in Rats
(Tubitak Scientific & Technological Research Council Turkey, 2020) Yildirim, Serkan; Celikezen, Fatih Caglar; Belhan, Saadet; Oto, Gokhan; Eser, Gizem; Sengul, Emin; Cinar, Dursunali
In this study, protective effects of lithium borate (LTB) on spermatogenesis as well as histopathological and immunohistochemical findings of testes in experimentally induced acute Cadmium (Cd) toxicity in rats were determined. Twenty-eight male Wistar albino rats, were used, weighing 200-220 g. Rats were randomly divided into 4 groups: Control, Cd, LTB, and LTB + Cd. Rats were anesthetized with ketamine at the end of the sixth day, blood was taken from their hearts, and the rats were decapitated. Typically, the control and LTB groups exhibited similar values. Compared with those observed for the control group, the sperm morphology (i.e. abnormal sperm count) increased for the Cd group, while the FSH, LH, total testosterone levels, sperm motility, and density decreased in a statistically significant manner. Clearly, no adverse effects of LTB on the sperm motility, density, and sperm morphology (i.e. abnormal sperm count) were observed, but LTB decreased the negative effects of Cd toxicity. Abnormal disturbances in the head and tail areas of the sperms increased; thus, the total abnormal sperm rate increases, leading to the decreased fertilization capacity. The histopathological examination of testicular tissues revealed severe haemorrhage and hyperaemia in intertubular intervals, tubule atrophy, severe degenerative and necrotic changes in spermatocytes, tubule wall thinning, and necrosis in basal germ cells. In immunohistochemically Caspase-3, 8-OHdG, and COX-2 staining, changes in the control and LTB groups were not detected, while the Cd toxicity group exhibited severe expression in the testis tissue. Histopathological and immunohistochemical changes were significantly decreased in the LTB + Cd group compared to the Cd group. In conclusion, in this study it was determined that LTB has protective effects on Cd-induced testicular toxicity in rats.
An Investigation of Protective Effects of Litium Borate on Blood and Histopathological Parameters in Acute Cadmium-Induced Rats
(Humana Press inc, 2018) Yildirim, Serkan; Celikezen, Fatih Caglar; Oto, Gokhan; Sengul, Emin; Bulduk, Mehmet; Tasdemir, M.; Cinar, D. Ali
This study was carried out to determine the protective effects of lithium borate (LTB) on blood parameters and histopathological findings in experimentally induced acute cadmium (Cd) toxicity in rats. Twenty-eight male Wistar albino rats were used, weighing 200-220 g, and they were randomly divided into four groups, including one control and the following three experimental groups: a Cd group (0.025 mmol/kg), a LTB group (15 mg/kg/day orally for 5 days), and a LTB + Cd group (15 mg/kg/day orally for 5 days and Cd 0.025 mmol/kg by intraperitoneal injection on the fifth day). All the rats in the study were anesthetized with ketamine at the end of the sixth day, blood was taken from their hearts, and then the rats were decapitated. The values in the control and LTB group were usually close to each other. White blood cell (WBC), neutrophil %, and C-reactive protein (CRP) levels increased in the Cd and LTB + Cd groups while lymphocyte and monocyte levels decreased in a statistically significant manner, in comparison to the other groups. It was determined that the levels of red blood cells (RBCs), hematocrit (Htc), and hemoglobin (Hb) did not change in the groups. The levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) in the Cd and LTB + Cd groups significantly increased, in comparison to the other groups, while the glucose, alkaline phosphatase (ALP), albumin (ALB), and total protein (TP) levels decreased. According to histopathological findings in the control and LTB groups, the liver and kidney tissues were found to have normal histological structures. In the Cd group, severe necrotic hemorrhagic hepatitis, mild steatosis, and mononuclear cell infiltration were detected in the liver. In the LTB + Cd group, degeneration and mild mononuclear cell infiltration were found in the liver. Regarding the kidney tissue in the Cd group, severe intertubular hyperemia in both kidney cortex and medulla, as well as degeneration and necrosis in the tubulus epithelium, was observed. In the LTB + Cd group, mild interstitial hyperemia and mononuclear cell infiltration was detected. Resultantly, it can be said that LTB at this dose has non-toxic effects and some beneficial effects for liver and kidney damage caused by acute Cd toxicity.
Synthesis and Biological Evaluation of Novel Benzylidene Thiazolo Pyrimidin-3(5h) Derivatives
(Taylor & Francis Ltd, 2024) Akbas, Esvet; Othman, Khdir A.; Celikezen, Fatih Caglar; Ejder, Nebahat Aydogan; Turkez, Hasan; Yapca, Omer Erkan; Mardinoglu, Adil
Starting compound 1 was synthesized according to reference.(1) Benzylidene thiazole pyrimidin-3(5H)-ones were synthesized reactions of 1 with bromoacetic acid and various aryl-aldehydes in the same vessel via one-step, unlike studies in the literature. Quantum chemical parameters and full geometry optimizations for all compounds were computed using DFT based on B3LYP. Cytotoxic action potential of synthesized compounds was evaluated using trypan blue dye exclusion and MTT assays in different cell lines including adenocarcinoma alveolar basal epithelial-like adherent A549 cells, the colon adenocarcinoma HT-29 cells, prostate adenocarcinoma DU-145 cells, and diploid ARPE-19 retinal pigment epithelial cells. Embryotoxicity and genotoxicity assessments were performed on pluripotent human embryonal carcinoma NT2 and human lymphocyte cells, respectively. Compound A1 exhibited good anticancer activity on A549 and DU-145 cell lines, and the compounds including A3, 4, 6, and 9 induced cytotoxicity on A549 cells. The compounds A1-10 also showed a good biosafety profile at relatively lower concentrations.
Synthesis of the 3,5-Diphenyl and Cytogenetic and Oxidative Alterations After Exposure of Cultured Human Whole Blood Cells
(Taylor & Francis As, 2017) Akbas, Esvet; Celikezen, Fatih Caglar; Turkez, Hasan; Ozdemir, Ozlem; Ruzgar, Adem; Ergan, Erdem; Sahin, Ertan
The 3,5-diphenyl-1H-pyrazole was obtained by condensation reaction of dibenzoylmethane and thiosemicarbazide in acetic acid under conventional heating and microwave irradiation method. The structure of the 3,5-diphenyl-1H-pyrazole confirmed by IR, H-1, and C-13 NMR and X-ray diffraction and the geometry optimization was carried out using density functional theory (DFT) methods at B3LYP/6-31G, 6-31G(d), 6-31G(d, p), 6-311G(d, p), 6-311G(2d, 2p), 6-31+G(d, p), 6-311++G(d, p) levels. In addition, cytotoxic and oxidative effects were investigated in cultured human peripheral blood cells.
Synthesis, Characterization, Theoretical Studies and in Vitro Embriyotoxic, Genotoxic and Anticancer Effects of Novel Phenyl(1,4,6-Triphenyl
(Taylor & Francis Ltd, 2024) Akbas, Esvet; Othman, Khdir A.; Celikezen, Fatih Caglar; Ejder, Nebahat Aydogan; Turkez, Hasan; Yapca, Omer Erkan; Mardinoglu, Adil
In this study, phenyl (1,4,6-triphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methanone was obtained by using the Biginelli reaction method. The structure of this compound was analyzed using elemental analysis, IR, 1H, and 13C NMR. The quantum chemical calculations (QCC) of this compound were performed density functional theory (DFT) method, 6-31 G (d, p) base set, and B3LYP functions with the Gaussian09W software package. Literature shows that pyrimidine-derived compounds have very active biological properties. For this reason, the biologically active properties of the synthesized compound were also examined. To determine embryotoxic, genotoxic, and cytotoxic effects of compound, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), lactate dehydrogenase (LDH) release, micronucleus (MN) and 8-OH-dG assays were carried out. On the other hand, pharmacokinetic and toxicity properties (ADMET) were predicted in silico via SwissADME and Protox-II web tools. In silico estimates of this compound used in the study showed that the compound has the covetable physicochemical properties for bioavailability. In conclusion, the obtained results of our study clearly showed that this compound exerted strong toxicity potential.