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Öğe CARDIOPROTECTIVE AND ANTIOXI DAN ACTIVITY OF BLUEBERRY ANTHOCYANINE AND POLYPHENOLS IN RATS(Elsevier Science Bv, 2009) Karakurt, Cemsit; Gursoy, Sule; Alagoz, Mehmet Abdullah; Karakurt, Arzu; Aktays, Goknur; Kocak, Gulendam[Abstract Not Available]Öğe Design and synthesis of some thiazolotriazolyl esters as anti-inflammatory and analgesic agents(Springer Birkhauser, 2012) Tozkoparan, Birsen; Aytac, S. Peri; Gursoy, Sule; Aktay, GoknurIn order to develop potent analgesic/anti-inflammatory compounds with reduced ulcerogenic risk, a series of thiazolotriazolyl-carboxylic and acetic acid esters were synthesized and characterized by spectral and elementary analysis. All synthesized compounds were screened for in vivo anti-inflammatory activities in mice by carregeenan-induced paw edema model. The compounds showing 20% reduction in paw edema were also evaluated for their analgesic activities by acetic acid-induced writhing test and the gastric ulceration risk by determining the lipid peroxidation level in stomachs. Among the compounds tested, compounds 1, 4, 6, 7, 8, 1a, 2a, 3a, 4a, 7a, 2b, and 8b showed moderate-to-good anti-inflammatory activity at various doses in any of the measurement intervals. Compounds 7a, 2b, and 8b were the most actives of the series in analgesic activity test. Moreover, compounds 1, 4, and 8 were found to be safe in stomach in respect of free radical production.Öğe The effects of apricot on serum proteins and liver enzymes in rats(Vup Food Research Inst, Bratislava, 2013) Yilmaz, Ismet; Temel, Ismail; Gursoy, Sule; Dogan, ZumrutThis study aimed to investigate the effects of different rates and feeding periods of sun-dried organic apricot (SDOA) supplementation on serum proteins and liver enzymes in rats. Numbers of 120 male and 120 female rats were randomly divided into five groups. The control group was fed with normal rat chow, and the others with 1%, 2.5%, 5% and 10% SDOA-supplemented diet, respectively. At the end of the 30th day of feeding periods, blood samples of 8 rats from each gender of every group were taken. Serum samples were used for measurements of albumin (ALB), total protein (TP), alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) levels. This procedure was repeated on the 60th and 120th days. Effects of rates and periods on parameters and interactions were investigated by two-way ANOVA. As the rates of SDOA in diet increased, decreases were observed in all parameters of males, and in ALP, AST and TP parameters of females. Considering periods, an effective role was observed on ALB, ALT and TP levels in genders. However, there were no significant interactions between rates and periods. The rate of 1% had beneficial effect on parameters in genders. However, the optimal period was not determined.Öğe Effects of Rifaximin on Bacterial Translocation in Thioacetamide-Induced Liver Injury in Rats(Springer/Plenum Publishers, 2012) Harputluoglu, Murat M. M.; Demirel, Ulvi; Gul, Mehmet; Temel, Ismail; Gursoy, Sule; Selcuk, Engin Burak; Aladag, MuratIntestinal bacterial overgrowth (IBO) and increased mucosal permeability are suggested to increase bacterial translocation (BT) in liver injury. Rifaximin (RIF) is a minimally absorbed oral antimicrobial agent that restores gut microflora imbalance. The aim of the present study was to investigate the effects of RIF on BT frequency in thioacetamide (TAA)-induced liver injury. Group 1 was the control. In group 2 (TAA), rats received TAA daily for 3 days. In group 3 (TAA + RIF), RIF was commenced on the same day as the first dose of TAA. In group 4 (RIF), rats received only RIF. Ileal aspirate Escherichia coli counts were significantly lower in the TAA + RIF group than in TAA group. There was no difference in BT frequency between the TAA and TAA + RIF groups. Our results suggest that factors such as intestinal barrier dysfunction and impaired host immune shield, apart from IBO, play an important role in BT in this model.Öğe The effects of sebum configuration on Demodex spp. density(Tubıtak scıentıfıc & technıcal research councıl turkey, ataturk bulvarı no 221, kavaklıdere, ankara, 00000, turkey, 2016) Demirdag, Hatice Gamze; Ozcan, Hamdi; Gursoy, Sule; Beker Akbulut, GulcinBackground/aim: Demodex spp. are ectoparasites living in the pilosebaceous units, which feed on the host's sebum and cellular proteins. The protective barrier of the skin consists of sebum secretion, moisture, and the acid mantle. In this study, we aimed to determine the effects of skin sebum, moisture, pH levels, and sebum configuration on Demodex spp. density Materials and methods: Forty-five patients who had demodicosis were enrolled in the study group, while the control group consisted of 40 subjects without demodicosis. Body fat percentage, serum triglyceride and cholesterol levels, skin sebum, moisture, and pH levels were measured. Demodex spp. density was determined with a standardized skin surface biopsy. Sebum samples were taken from the forehead and a high-performance thin-layer chromatography (HPTLC) method was performed on these samples. Subsequently, densitometric analyses were applied to the HPTLC plates. Results: Demodex spp. were found on the cheeks and lived in an alkali environment. Skin sebum and moisture levels were low in all groups. The skin pH levels and cholesterol ester in the sebum configuration were determined to be significantly higher in the group with demodicosis. Conclusion: We suggest that Demodex spp. may use cholesterol ester in the sebum as nutriment. In other words, cholesterol ester may be a suitable growth medium for the proliferation of Demodex spp.Öğe Identification of some novel amide conjugates as potent and gastric sparing anti-inflammatory agents: In vitro, in vivo, in silico studies and drug safety evaluation(Elsevier, 2023) Kulabas, Necla; Set, Irem; Aktay, Goeknur; Gursoy, Sule; Danis, Oezkan; Ogan, Ayse; Erdem, Safiye SagToday, usage of NSAIDs (nonsteroidal anti-inflammatory drugs) is very common. However, it has been proven by many studies that NSAIDs with free carboxylic acid group damage the GI (gastrointestinal) system. Our aim was to mask the acidic groups of NSAIDs to prevent or reduce their side effects while preserving their pharmacological effects. In this study, new amide derivatives of known NSAIDs, compounds 11 -20 , were synthesized to investigate their analgesic and anti-inflammatory effects using in vivo models. While compound 11 showed the most remarkable anti-inflammatory activity by 60.9% inhibition value at 200 mg/kg dose, compounds 11, 12, 15 and 18 had almost the same analgesic activity to that of acetylsalicylic acid (100 mg/kg) and flurbiprofen (100 mg/kg). In addition, all test compounds used at high dose (200 mg/kg, p.o) did not show any acute toxicity. COX-1 and COX-2 inhibition properties of all compounds were measured by biochemical methods and the interaction of the most active compounds with COX enzymes is elucidated by computer-assisted virtual screening methods. It was determined by in vitro enzyme inhibition studies that compound 11 and 13 , synthesized from selective COX-1 inhibitors dexketoprofen and flurbiprofen, are selective COX-2 inhibitors. Moreover, compounds 11 -13 were found to be non-mutagenic according to the mutagenicity assay using Salmonella TA98 and TA10 0 strains with and without metabolic activation. Finally, the prediction of ADMET profile and drug-likeness properties of compounds 11 -20 were examined and the obtained results were evaluated. & COPY; 2023 Elsevier B.V. All rights reserved.Öğe Novel 1,2,4-Triazolo[3,4-b]-1,3,4-thiadiazole Derivatives as Dual Analgesic/Anti-inflammatory and Antimicrobial Agents(Bentham Science Publ Ltd, 2012) Tozkoparan, Birsen; Aytac, Sevim Peri; Gursoy, Sule; Gunal, Selami; Aktay, GoknurFor this study, a series of 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles (1-12) were synthesized by condensation of 4-amino-5-substituted-3-mercapto-1,2,4-triazoles with various benzoic acids through a one-pot reaction. The anti-inflammatory and analgesic activities as well as gastrointestinal irritation liability of the obtained compounds were evaluated. Several of the synthesized compounds showed noticeable analgesic and anti-inflammatory activity. For the active compounds a very low ulcerogenic index and diminished oxidative damage in stomach were observed. Moreover, title compounds were screened for their antifungal and antibacterial activities. Antifungal activity of the compounds was found better than that of their antibacterial activity.Öğe Synthesis and Characterization of Celecoxib Derivatives as Possible Anti-Inflammatory, Analgesic, Antioxidant, Anticancer and Anti-HCV Agents(Mdpi, 2013) Kucukguzel, S. Guniz; Coskun, Inci; Aydin, Sevil; Aktay, Goknur; Gursoy, Sule; Cevik, Ozge; Ozakpinar, Ozlem BingolA series of novel N-(3-substituted aryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides 2a-e were synthesized by the addition of ethyl alpha-bromoacetate and anhydrous sodium acetate in dry ethanol to N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)-3-(trifluoro-methyl)- 1H-pyrazol-1-yl] benzene sulfonamides 1a-e, which were synthesized by the reaction of alkyl/aryl isothiocyanates with celecoxib. The structures of the isolated products were determined by spectral methods and their anti-inflammatory, analgesic, antioxidant, anticancer and anti-HCV NS5B RNA-dependent RNA polymerase (RdRp) activities evaluated. The compounds were also tested for gastric toxicity and selected compound 1a was screened for its anticancer activity against 60 human tumor cell lines. These investigations revealed that compound 1a exhibited anti-inflammatory and analgesic activities and further did not cause tissue damage in liver, kidney, colon and brain compared to untreated controls or celecoxib. Compounds 1c and 1d displayed modest inhibition of HCV NS5B RdRp activity. In conclusion, N-(ethylcarbamothioyl)-4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide (1a) may have the potential to be developed into a therapeutic agent.
