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    CYTOTOXIC AND GENOTOXIC EVALUATION OF SOME NEWLY SYNTHESIZED SULFONAMIDE DERIVATIVES
    (Parlar Scientific Publications (P S P), 2017) Sen, Selen; Berber, Ahmet Ali; Demirci, Tuna; Arslan, Mustafa; Aksoy, Huseyin
    In the present study, it was aimed to assess the genotoxic potentials of [4,4-Dimethyl-2,6dioxocyclohexylidene) methylamino) benzene sulfonamide] (2b) and [4-((1,3-Dimethy1-2,4,6trioxo-tetrahydropyrimidin-5(6H)-ylidene) methyla mino) benzenesulfonamide] (2e) compounds which were synthesized considering that they may be used as drug raw materials and detected to inhibit human carbonic anhydrase I, II isoenzymes. For this purpose, chromosomal aberration, micronucleus and comet tests were implemented in human peripheral blood lymphocytes. 2b was used at the concentrations of 2.12, 1.06, 0.53 mu g/mL. 2e was used at the concentrations of 2.52, 1.26, 0.63 mu g/mL for these in vitro assays. We observed that 2b and 2e had no significant difference in all our application doses for chromosomal abnormalities and micronucleus assay. 2b and 2e showed different responses for tail length, tail intensity and tail moment in Comet assay. 2b reduced the mitotic index in all concentrations in 48 h application compared to both control groups, whereas 2e only reduced mitotic index at 2.52 mu g/mL compared to negative control and in all concentrations compared to the solvent control. According to the obtained results, the test substances are cytotoxic at high concentrations and long-term exposure but they are not genotoxic in human peripheral lymphocytes.
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    Kinesin-5 inhibitörü olan Monastrol bileşiğinin sentezi ve yük transferi kompleks etkileşmelerinin incelenmesi
    (2016) Berber, Nurcan; Arslan, Mustafa
    Kinesin-5 inhibitörü olarak kullanılan Monastrol, çözücüsüz ortamda alümina sülfonik asit (ASA) katalizörü varlığında 3-hidroksibenzaldehit, tiyoüre ve etilasetoasetat kullanılarak sentezlenmiştir. Elektron verici (Donör, D) olarak monastrol, elektron alıcı (Akseptör, A) olarak tetrasiyanoquinometan (TCNQ) kullanılmış ve bunlar ile 2,3dikloro-5,6-disiyano-p-benzokinon (DDQ) bileşikleri arasındaki yük transfer kompleksleri asetonitril içinde 21 °C'de spektrofotometrik olarak incelenmiştir. Komplekslerin stokiyometrisi, Job yöntemi kullanılarak incelenmiş, elektron verici ve alıcılar arasında TCNQ ile 742 nm ve DDQ ile 546 nm dalga boyunda maksimum absorbsiyon bandında 1:1 oranında olduğu bulunmuştur. Komplekslerin denge sabiti Benesi-Hildebrand ve termodinamik parametreleri Van't Hoff denklemi ile belirlenmiştir.
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    Preparation and Characterization of Some Schiff Base Compounds
    (Adiyaman University, 2020) Berber, Nurcan; Arslan, Mustafa
    Schiff bases (imines) have been frequently used in various fields such as medicine, pharmaceutical purposes due to their various biological properties. In this study, nine new imine compounds (3a-h) were synthesized from 1-naphthyl amine with aromatic aldehydes in MeOH and their chemical structures were defined by 1H/13C NMR, IR and elemental analysis studies. We observed a singlet one hydrogen of the imines (–CH=N–) at 8.56–8.86 ppm in the 1H NMR spectra and also carbon of the Schiff bases (–CH=N–) at 158.2-163.4 ppm in the 13C NMR spectra. Also the IR spectra displayed the (–C=N–) characteristic absorption band at around 1600 cm-1. The obtained characteristic peaks at the expected locations proved the structural accuracy of the synthesized new derivative Schiff bases. © 2020, Adiyaman University. All rights reserved.
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    Synthesis of new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives as carbonic anhydrase inhibitors
    (Wiley, 2020) Berber, Nurcan; Arslan, Mustafa; Vural, Firat; Ergun, Adem; Gencer, Nahit; Arslan, Oktay
    Human carbonic anhydrase I and II isoenzymes (hCA I and II) are important metabolic enzymes. In this study, a new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives were synthesized and also some inhibition parameters including IC50(hydratese) and inhibition constant values (K-i, esterase) were determined. All studied compounds exhibited potent inhibition against these enzymes. They inhibited carbonic anhydrases (CAs) with the IC(50)values of 113 to 395.8 nM (K-i = 77.38-319.59 nM) for hCA I and 91.9 to 516 nM (K-i = 62.79-425.89 nM) for hCA II. Among the compounds,5cwas found to be the most active one (K-i: 77.38 nM) for hCA I and5gwas found for hCA II with the value of 62.79 nM.
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    The effect of dexmedetomidine on myocardial ischemia reperfusion injury in streptozotocin induced diabetic rats
    (Anaesthesia Pain & Intensive Care, 2015) Arslan, Mustafa; Poyraz, Fatih; Kiraz, Hasan Ali; Alkan, Metin; Kip, Gulay; Erdem, Ozlem; Ozer, Abdullah
    Objective: Ischemia/reperfusion (I/R) injury is an important cause of myocardial damage by means of oxidative, inflammatory, and apoptotic mechanisms. The aim of the present study was to examine the potential cardio-protective effects of dexmedetomidine in a diabetic rat model of myocardial I/R injury. Methodology: A total of 18 streptozotocin (55 mg/kg) induced diabetic Wistar Albino rats were randomly divided into three equal groups as follows: the diabetic I/R group (DIR) in which myocardial I/R was induced by ligating the left anterior descending (LAD) coronary artery for 30 min, followed by 2 hours of reperfusion following left thoracotomy, the diabetic I/R dexmedetomidine group (DIRD) which were given 100 mu g/kg dexmedetomidine intraperitoneally 30 min before I/R induction by the same method and the diabetic control group (DC) which underwent sham operations without tightening of the coronary sutures. As a control group (C), 6 healthy age-matched Wistar Albino rats underwent sham operations similar to DC group. After the operation the rats were sacrificied and the myocardial tissues were histopathologically examined. Results: Microscopic myonecrosis findings were significantly different among groups (p= 0.008). Myonecrosis findings were significantly higher in DIR compared to C, DC and DIRD groups (p= 0.001, p=0.007 and p=0.037 respectively). Similarly microscopic inflammatory cell infiltration degrees showed significant differences among groups (p<0.0001). Compared to C, DC and DIRD groups, the microscopic inflammatory cell infiltration was significantly higher among DIR group (p<0.0001, p<0.0001 and p=0.009 respectively). Also myocardial tissue edema was significantly different among groups (p=0.002). The microscopic myocardial tissue edema levels were significantly higher in DIR group than C and DIRD groups (p<0.0001 and p=0.022 respectively). Tissue edema was also more prominent in DC compared to C group (p=0.022) Conclusion: Taken together our data indicate that dexmedetomidine may be helpful in reducing myocardial necrosis, myocardial inflammation and myocardial tissue edema resulting from ischemia/reperfusion injury.
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    The effect of levosimendan on myocardial ischemia[1] reperfusion injury in streptozotocin-induced diabetic rats
    (Co-Action Publishing, 2015) Kiraz, Hasan Ali; Poyraz, Fatih; Kip, Gülay; Erdem, Özlem; Alkan, Metin; Arslan, Mustafa; Özer, Abdullah
    Objective: Ischemia/reperfusion (I/R) injury is an important cause of myocardial damage by means of oxidative, inflammatory, and apoptotic mechanisms. The aim of the present study was to examine the potential cardio protective effects of levosimendan in a diabetic rat model of myocardial I/R injury. Methods: A total of 18 streptozotocin-induced diabetic Wistar Albino rats (55 mg/kg) were randomly divided into three equal groups as follows: the diabetic I/R group (DIR) in which myocardial I/R was induced following left thoracotomy, by ligating the left anterior descending coronary artery for 60 min, followed by 2 h of reperfusion; the diabetic I/R levosimendan group (DIRL), which underwent I/R by the same method while taking levosimendan intraperitoneal 12 mg kg-1; and the diabetic control group (DC) which underwent sham operations without tightening of the coronary sutures. As a control group (C), six healthy age-matchedWistar Albino rats underwent sham operations similar to the DC group. Two hours after the operation, the rats were sacrificed and the myocardial tissue samples were examined by light microscopy for evidence of myonecrosis and inflammatory cell infiltration. Results: Myonecrosis findings were significantly different among groups (p = 0.008). Myonecrosis was more pronounced in the DIR group compared with the C, DC, and DIRL groups (p = 0.001, p = 0.007 and p = 0.037, respectively). Similarly, the degree of inflammatory cell infiltration showed significant difference among groups (p<0.0001). Compared with C, DC, and DIRL groups, the inflammatory cell infiltration was significantly higher among the DIR group (p<0.0001, p<0.0001, and p=0.020, respectively). Also, myocardial tissue edema was significantly different among groups (p=0.006). The light microscopic myocardial tissue edema levels were significantly higher in the DIR group than the C, DC, and DIRL groups (p=0.001, p=0.037, and p=0.014, respectively). Conclusion: Taken together, our data indicate that levosimendan may be helpful in reducing myocardial necrosis, myocardial inflammation, and myocardial tissue edema resulting from ischemia-reperfusion injury. © 2015 Hasan Ali Kiraz et al.
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    The effect of levosinnendan on myocardial ischemia reperfusion injury in streptozotocin-induced diabetic rats
    (Co-Action Publishing, 2015) Kiraz, Hasan Ali; Poyraz, Fatih; Kip, Gulay; Erdem, Ozlem; Alkan, Metin; Arslan, Mustafa; Ozer, Abdullah
    Objective: Ischemia/reperfusion (I/R) injury is an important cause of myocardial damage by means of oxidative, inflammatory, and apoptotic mechanisms. The aim of the present study was to examine the potential cardio protective effects of levosimendan in a diabetic rat model of myocardial I/R injury. Methods: A total of 18 streptozotocin-induced diabetic Wistar Albino rats (55 mg/kg) were randomly divided into three equal groups as follows: the diabetic I/R group (DIR) in which myocardial I/R was induced following left thoracotomy, by ligating the left anterior descending coronary artery for 60 min, followed by 2 h of reperfusion; the diabetic I/R levosimendan group (DIRL), which underwent I/R by the same method while taking levosimendan intraperitoneal 12 mu g kg(-1); and the diabetic control group (DC) which underwent sham operations without tightening of the coronary sutures. As a control group (C), six healthy age-matched Wistar Albino rats underwent sham operations similar to the DC group. Two hours after the operation, the rats were sacrificed and the myocardial tissue samples were examined by light microscopy for evidence of myonecrosis and inflammatory cell infiltration. Results: Myonecrosis findings were significantly different among groups (p = 0.008). Myonecrosis was more pronounced in the DIR group compared with the C, DC, and DIRL groups (p = 0.001, p = 0.007 and p = 0.037, respectively). Similarly, the degree of inflammatory cell infiltration showed significant difference among groups (p < 0.0001). Compared with C, DC, and DIRL groups, the inflammatory cell infiltration was significantly higher among the DIR group (p < 0.0001, p < 0.0001, and p = 0.020, respectively). Also, myocardial tissue edema was significantly different among groups (p = 0.006). The light microscopic myocardial tissue edema levels were significantly higher in the DIR group than the C, DC, and DIRL groups (p = 0.001, p = 0.037, and p = 0.014, respectively). Conclusion: Taken together, our data indicate that levosimendan may be helpful in reducing myocardial necrosis, myocardial inflammation, and myocardial tissue edema resulting from ischemia reperfusion injury.