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    A new affinity method for purification of bovine testicular hyaluronidase enzyme and an investigation of the effects of some compounds on this enzyme
    (Taylor & Francis Ltd, 2015) Kaya, Mustafa Oguzhan; Arslan, Oktay; Guler, Ozen Ozensoy
    In this study, a new affinity gel for the purification of bovine testicular hyaluronidase (BTH) was synthesized. L-Tyrosine was added as the extension arm to the Sepharose-4B activated with cyanogen bromide. m-Anisidine is a specific inhibitor of BTH enzyme. m-Anisidine was clamped to the newly formed Sepharose-4B-L-tyrosine as a ligand. As a result, an affinity gel having the chemical structure of Sepharose-4B-L-tyrosine-m-anisidine was obtained. BTH purified by ammonium sulfate precipitation and affinity chromatography was obtained with a 16.95% yield and 881.78 degree of purity. The kinetic constants K-M and V-Max for BTH were determined by using hyaluronic acid as a substrate. K-M and V-Max values obtained from the Lineweaver-Burk graph were found to be 2.23mM and 19.85 U/mL, respectively. In vitro effects of some chemicals were determined on purified BTH enzyme. Some chemically active ingredients were 1,1-dimethyl piperidinium chloride, beta-naphthoxyacetic acid and gibberellic acid. Gibberellic acid showed the best inhibition effect on BTH.
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    Bovine carbonic anhydrase (bCA) inhibitors: Synthesis, molecular docking and theoretical studies of bisoxadiazole-substituted sulfonamide derivatives
    (Elsevier, 2024) Eybek, Abdulbaki; Kaya, Mustafa Oguzhan; Gulec, Ozcan; Demirci, Tuna; Musatat, Ahmad Badreddin; Ozdemir, Oguzhan; Oner, Mine Nazan Kerimak
    This paper describes the in vitro inhibition potential of bisoxadiazole-substituted sulfonamide derivatives (6a-t) against bovine carbonic anhydrase (bCA) after they were designed through computational analyses and evaluated the predicted interaction via molecular docking. First, in silico ADMET predictions and physicochemical property analysis of the compounds provided insights into solubility and permeability, then density functional theory (DFT) calculations were performed to analyse their ionization energies, nucleophilicity, in vitro electron affinity, dipole moments and molecular interactions under vacuum and dimethyl sulfoxide (DMSO) conditions. After calculating the theoretical inhibition constants, IC50 values determined from enzymatic inhibition were found between 12.93 and 45.77 mu M. Molecular docking evaluation revealed favorable hydrogen bonding and pi-interactions of the compounds within the bCA active site. The experimentally most active compound, 6p, exhibited the strongest inhibitory activity with a theoretical inhibition constant value of 9.41 nM and H-bonds with Gln91, Thr198, and Trp4 residues and His63 Pi-cation interactions with His63 residues. Overall, the study reveals promising bCA blocking potential for the synthesized derivatives, similar to acetazolamide.
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    Carbonic Anyhdrase Enzyme From The Siirt Mohair Goat Liver :Purification, Characterization and Assessment of Enzyme Kinetics Against Metal Toxicity
    (2017) Yerlikaya, Emrah; Karagecili, Hasan; Demirdag, Ramazan; Kaya, Mustafa Oguzhan
    Because of their physiological and clinical roles, carbonic anhydrases (CAs) are the most studied enzymes. In earlier studies; CA enzymes have been purified and characterized from the tissues and erythrocytes of many organisms such as; dog, swine, sheep, chicken, bee, fish, bovine, bacteria and human. In this study, the CA enzyme has purified from Siirt Mohair Goat liver tissue with 1930.84 EU x mg-1 of specific activity, 57.28% of purification yield and 80.55 of purification folds. The purity of the purified enzyme has confirmed by SDS-PAGE. As the characterization of CA enzyme’s in Siirt Mohair Goat liver has been done; the optimum ionic strength=25 mM, the optimum pH= 8.0, the optimum temperature= 40ºC and the stable pH= 7.0 has been determined. Inhibitory effects of some metal ions have been examined on the purified CA enzyme. IC50 values of inhibiting metal ions were found as 2.24, 2.76, 2.36, 3.20, 2.55, 2.25, 3.28, 2.13, 3.10, 1.75, 2.16 and 3.50 mM for Al3+, Ni2+, Cd2+, Cu2+, Pb2+, Ba2+, Zn2+, B3+, Fe3+, Se2+, Ag+ and Co2+ respectively. As a result, CA enzyme was first purified from the
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    Comparison of Creatine Kinase Myocardial Band (CK-MB) and high sensitive Troponin I (hsTnI) values between athletes and sedentary people
    (Mattioli 1885, 2020) Cakaroglu, Deniz; Kaya, Mustafa Oguzhan
    Study Objectives: This study was conducted to examine and compare CK-MB and hsTnI values between people who exercise regularly and actively and those who do not, considering that men have a higher muscle mass than women, but also the higher amount of estrogen secreted in women. Methods: The test group was composed of 18 men, 17 women, a total of 35 (23.28 +/- 4.09 years) persons who engaged in active sports with no problems in terms of blood measurement. The control group was formed from a total of 34 (24.50 +/- 5.60 years) persons, including 17 men and 17 women with a sedentary lifestyle that do not engage any sport. Statistical analyses were evaluated in the SPSS program and the Independent Samples t Test was used to determine the difference between the groups. Results: The CK-MB values of active athletes were found to be less than 5 U/L (1.95 +/- 1.04), which is the mean value, and higher values than the control group. hsTnI values have a significant difference between the test group and the control group and this difference was found to below the middle level. The mean CK-MB and hsTnI values of men participants were found to be statistically significant, with more than the mean value of women participants. The men test group CK-MB values were found to be higher than the control group and there was a significant difference (p<0.05). There was no statistically significant difference in hsTnI values between men's test and control groups. Conclusion: As a result of CK-MB and hsTnI measurements of the women test and control groups, it was observed that there was no significant difference between them. Herewith, it has been revealed that there are differences in CK-MB and hsTnI values among those who do active sports compared to those who do not, but also among women and men.
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    Differential in vitro inhibition studies of some cerium vanadate derivatives on xanthine oxidase
    (Taylor & Francis Ltd, 2015) Kaya, Mustafa Oguzhan; Kaya, Yesim; Celik, Gulsah; Kurtulus, Figen; Arslan, Oktay; Guler, Ozen Ozensoy
    In this preliminary study, a new series of some cerium vanadate derivatives have been investigated as new type of inhibitors of xanthine oxidase (XO; E.C 1.17.3.2). XO is a superoxide-producing enzyme found normally in serum and the lungs, and its activity is concerned with several important health problems such as gout, severe liver damage, vascular dysfunction and injury, oxidative eye injury and renal failure. In this study, we present a critical overview of the effects of these novel type agents on XO with comparing the efficacy and safety profiles of allopurinol, the efficient classical inhibitor of XO.
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    In vitro effects of 2, 4-Dichlorophenoxy acetic acid dimethylamine salt and enrofloxacin on BTH
    (Agricultural Research Communication Centre, 2018) Kaya, Mustafa Oguzhan
    In this study, the in vitro effects of enrofloxacin, a broad spectrum antibiotic, and 2, 4-Dichlorophenoxy acetic acid dimethylamine salt that, a herbicide, on the bovine testicular hyaluronidase (BTH) were analyzed. BTH was purified using the method of ammonium sulfate precipitation and using affinity gel (Sepharose-4B-L-tyrosine-m-anisidine). Then the inhibiting effects of enrofloxacin and 2, 4-Dichlorophenoxy acetic acid dimethylamine salt on the purified BTH enzyme were identified. IC50 values of these chemical substances were found to be 0.3101 and 0.4276 mM, respectively.
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    IN VITRO EFFECTS OF NEW GENERATION BISOXADIAZOLE SUBSTITUTED SULFONAMIDE DERIVATIVES ON HUMAN SERUM PARAOXONASE1 (PON1)
    (Parlar Scientific Publications (P S P), 2018) Kaya, Mustafa Oguzhan; Gulec, Ozcan; Arslan, Mustafa
    In this study, new bisoxadiazole substituted sulfonamide compounds were synthesized and in vitro inhibition effects of the compouds on purified human serum paraoxonase 1 (PON I) were investigated by using the method of Gan et al. The results showed that all the synthesized compounds inhibited the paraoxonase 1 enzyme activity. The compounds 6d and 6e were found to be most active compounds (IC50=26.5 mu M and 28.6 mu M) for PON1, respectively.
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    In vitro effects of novel type M-V-O derivatives on Xanthine Oxidase
    (C M B Assoc, 2017) Kaya, Mustafa Oguzhan; Gul, Gulsah Celik; Kurtulus, Figen
    Xanthine Oxidase (XO) is related with different diseases such as vascular, gout, nephropathy and renal stone diseases that are relevant to high uric acid levels and oxidative stress. Some common natural inhibitors of xanthine oxidase are known as rosmarinic acid and apigenin. With this study, we aimed to determine inhibitory effects of originally synthesized new generation transition metal vanadates on Xanthine Oxidase (XO) from bovine milk. Because, Xanthine oxidase inhibitors are typically used in the treatment of gout and nephropathy and renal stone diseases linked to hyperuricaemia. We found considerable IC50 constants for inhibition of XO. Among the synthesized compounds, Cu-V-O was found to be the most active (IC50 = 7.119 mM) for inhibition of XO.
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    In vitro inhibition of purified human carbonic anhydrase I and II by novel fluorene derivatives
    (Macedonian Journal of Chemistry and Chemical Engineering, 2014) Demirhan, Hulya; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Kaya, Yesim; Gencer, Nahit; Arslan, Oktay
    In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 ?M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 ?M) for inhibition of hCA II.
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    IN VITRO INHIBITION OF PURIFIED HUMAN CARBONIC ANHYDRASE I AND II BY NOVEL FLUORENE DERIVATIVES
    (Soc Chemists Technologists Madeconia, 2014) Demirhan, Hulya; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Kaya, Yesim; Gencer, Nahit; Arslan, Oktay
    In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 mu M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 mu M) for inhibition of hCA II.
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    Is there a relation between genetic susceptibility with cancer? A study about paraoxanase (PON1) enzyme activity in breast cancer cases
    (Taylor & Francis Ltd, 2016) Kaya, Mustafa Oguzhan; Sinan, Selma; Guler, Ozen Ozensoy; Arslan, Oktay
    Human serum paraoxonase 1 (PON1, EC 3.1.1.2) is a high density lipoprotein (HDL)-associated antioxidant enzyme that not only decreases oxidative stress, but it is also implicated in development of many cancers. Genetic information provides a means of identifying people who have an increased risk of cancer, thus this knowledge of cancer genetics helps to identify the ability to characterize malignancies leading to the development of new therapeutic approaches. Because of this reason, in this preliminary study we aimed to investigate the role of human serum PON1 enzyme activity and phenotypic distribution in 32 breast cancer (BC) patients (age range 28-82) and 35 cancer free (CF) control group (age range 21-67). PON1 enzyme was prepared from the serum pool of BC patients using hydrophobic interaction chromatography on L-tyrosine-9-aminophenanthrene-coupled Sepharose 4Bgel. The PON1 enzyme activity towards paraoxon substrate was quantified spectrophotometrically. The basal activity of PON1 was statistically decreased in cancer cases compared to the control group. In addition, individuals were classified according to phenotyping of human PON1 Q and R types. In the cohort of BC patients, an increase in the frequency of the PON homozygote Q (AA) genotype was observed (31% in the BC group versus 14% in the CF controls). The frequency of the PON heterozygote QR (AB) genotype was 34.5% in the patients with BC and 37% in the CF group. The same trend was observed in PON homozygote R (BB) genotype frequency (BC cases 34.5% versus controls 49%). We determined that the kinetic parameters of the purified enzyme by Lineweaver-Burk method. We obtained K-m and V-max values of 0.227mM and 62 U/mL min for the BC enzyme, compared with 0.775 mM and 206 U/mL min for the CF control enzyme. As a conclusion, it is clear from our results that while the PON1 AA allele frequency in BC cases is much higher, that of BB allele is much lower, in comparison with the control group. The most significant finding of this study is AA allele activity which is low in BC cases was found high. We concluded that decreased AA allele PON1 activity might have a relation with BC.
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    Oxidant/Antioxidant Status, PON1 and ARES Activities, Trace Element Levels, and Histological Alterations in Sheep with Cystic Echinococcosis
    (Iranian Scientific Society Medical Entomology, 2018) Irak, Kivanc; Celik, Burcak Aslan; Karakoc, Zelal; Celik, Ozgur Yasar; Mert, Handan; Mert, Nihat; Kaya, Mustafa Oguzhan
    Background: Total antioxidant status (TAS), total oxidant status (TOS) and oxidative stress index (OSI), nitric oxide (NO), zinc (Zn), copper (Cu) levels, paraoxonase (PON1), arylesterase (ARES) activities, and biochemical changes were studied on sheep with cystic echinococcosis. Methods: The materials were taken from 2-3 yr old sheep slaughtered in Van Province, Turkey in 2017. Before the slaughter, blood samples were collected from the healthy sheep, while various organs of animals were examined for hydatid cysts after the slaughter. Thirty sheep were protoscolex positive, hydatic group, while 30 sheep that did not have any pathological lesions in organ examinations were accepted as the control group. TOS levels, PON1 and ARES activities, and Zn levels were determined by commercial kits, while Cu levels were determined by atomic absorption spectrophotometer. The collected data were then statistically analyzed. Results: Serum TOS and OSI levels were significantly higher in sheep with cystic echinococcosis compared to the control group (P<0.001). TAS levels (P<0.01), PON1 and ARES activities, on the other hand, were significantly higher in control group compared to the cystic echinococcosis group (P<0.001). There were no significant differences in Zn, NO and Cu levels between the groups. Conclusion: PON1 and ARES activities increased in sheep infected with cyst hydatid. The decline of antioxidant reserves in the metabolism results in excessive amounts of free radicals, along with alterations of the normal histological structure of the cystic organ and changes in trace element metabolism.
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    Siirt Tiftik Keçisi Böbrek Dokusundan Karbonik Anhidraz Enziminin Saflaştırılması, Karakterizasyonu ve Bazı Biyokimyasal Özelliklerinin Araştırılması
    (2016) Yerlikaya, Emrah; Karagecili, Hasan; Demirdag, Ramazan; Kaya, Mustafa Oguzhan
    Carbonic anhydrase (CA) (E.C:4.2.1.1) is a group of metalloenzyme containing zinc widely distributed from the simplest organisms such as bacteria to the most complex organisms such as plants and animals. CA inhibitors are some of the principal drugs used in the management of canine and feline glaucoma. In earlier studies; CA enzymes successfully have been purified and characterized from many living things such as; sheep, chicken, fish, bovine and human. In this study, the CA enzyme has purified from Siirt Mohair Goat kidney tissue with 902.9 EU x mg-1 of specific activity, 50.19% of purification yield and 83.54 of purification folds by using Sepharose-4B-L-tyrosine-sulfonamide affinity column. The purity of the purified enzyme has confirmed by SDS-PAGE. As the characterization of CA enzyme’s in Siirt Mohair Goat kidney has been done; the optimum ionic strength=25mM, the optimum pH=8.5, the optimum temperature=45ºC and the stable pH=7.0 has been determined. Inhibitory effects of Al3+, Ni2+, Cd2+, Pb2+, Ba2+, Zn2+, B3+, Fe3+, Se2+, Ag+ and Co2+ metal ions have been examined on the purified CA enzyme. Inhibition graphics have been drawn in order to find the IC50 values of metals showing inhibition.
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    Synthesis and carbonic anhydrase inhibitory properties of tetrazole- and oxadiazole substituted 1,4-dihydropyrimidinone compounds
    (Informa Healthcare, 2014) Celik, Fatma; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Yavuz, Emre; Gencer, Nahit; Arslan, Oktay
    A new series of tetrazole-, oxadiazole-and cyanosubstituted 1,4-dihydropyrimidinone compounds were synthesized, and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I were evaluated. 4-Cyanophenyl-1,4- dihydropyrimidinone compounds were prepared with 1,3-diketone, cyanobenzaldehyde and urea. The compounds were reacted with sodium azide and then with anhydride to get the final products. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. The compound 4-(1,7,7-trimethyl-2,5-dioxo-1,2,3,4,5,6,7,8-octahydroquinazoline- 4-yl) benzonitrile 6c (IC50 = 0.0547 mM) has the most inhibitory effect.
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    Synthesis, activatory effects, molecular docking and ADME studies as rabbit muscle pyruvate kinase activators of ureido phenyl substituted 1,4-dihydropyridine derivatives
    (Springer, 2024) Kaya, Mustafa Oguzhan; Demirci, Tuna; Calisir, Umit; Ozdemir, Oguzhan; Kaya, Yesim; Arslan, Mustafa
    In this study, the activation of pyruvate kinase enzyme in vitro via different urea substituents in the para position as functional groups of 1,4-dihydropyridine derivatives synthesized by Hantzsch reaction method was investigated. Elemental analysis, 1H-NMR, 13C-NMR and FT-IR spectroscopy were used to identify the ureido phenyl substituted 1,4-dihydropyridine derivatives. Virtual screening based on molecular docking supported the results of possible in vitro pyruvate kinase (PK) activators among the synthesized substances. The results showed that all compounds successfully activated PK. The strongest activator effect was shown by ethyl-4-(4-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,7,8-hexahydroquinolin-3 (7) with an AC50 value of 87.70 mu M. In molecular docking studies, full compatibility (- 3016.93 FF), binding affinities (Delta G = - 8.58 kcal/mol), LUMO-HOMO energy gap (Delta E = 7.85 eV) in Density functional theory (DFT) studies and drug similarity score of the compounds were found to be 0.69. These results shed light on the therapeutic potential of the produced compounds to treat PK-related diseases.
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    Synthesis, inhibition effects, molecular docking and theoretical studies as Paraoxonase 1 (PON1) inhibitors of novel 1,4-dihydropyridine substituted sulfonamide derivatives
    (Springer Birkhauser, 2023) Kaya, Mustafa Oguzhan; Demirci, Tuna; Ozdemir, Oguzhan; Calisir, Umit; Sonmez, Fatih; Arslan, Mustafa
    The novel sulfonamide substitute 1,4-dihydropyridine derivatives were synthesized by the method of Hantzsch reaction. They have been characterized by FT-IR spectroscopy, H-1-NMR, C-13-NMR, and elemental analysis. PON1 which is an antioxidant enzyme has important functions in cardiovascular systems. The enzyme has been purified using a two-step method such as ammonium sulfate precipitation and sepharose-4B-l-tyrosine-9-aminophenanthrene hydrophobic interaction chromatography. The results demonstrated that all the synthesized compounds inhibited PON1 enzyme. The best inhibition effect was observed in compound (1) for PON1 enzyme (IC50: 8.04 mu M, K-i: 5.43 mu M). The free radical scavenging for PON1 was discovered as 20.16 mg/mL, while drug score value was reported as 0.13 for compound (1). Furthermore, the lowest binding energy (-1.31 kcal/mol) determined by molecular docking for PON1 enzyme and the lowest LUMO-HOMO gap ( increment E = 3.12 eV) were calculated for compound (1).