Person: DAĞ, AYDAN
6 results
Search Results
Now showing 1 - 6 of 6
Publication Open Access Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors(2017-01-01) Sonmez, Fatih; KURT, Belma Zengin; Gazioglu, IŞIL; BASILE, Livia; Dag, AYDAN; CAPPELLO, Valentina; GINEX, Tiziana; Kucukislamoglu, Mustafa; GUCCIONE, Salvatore; ZENGİN KURT, BELMA; GAZİOĞLU, IŞIL; DAĞ, AYDANNew coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and in vitro tested as acetylcholinesterase (AChE) inhibitors. 2-(diethylamino)-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)acetamide (6c, IC50 value of 43 nM) was the best AChE inhibitor with a selectivity index of 4151.16 over BuChE. Kinetic study of AChE inhibition revealed that 6c was a mixed-type inhibitor. Moreover, the result of H4IIE hepatoma cell toxicity assay for 6c showed negligible cell death. Molecular docking studies were also carried out to clarify the inhibition mode of the more active compounds. Best pose of compound 6c is positioned into the active site with the coumarin ring wedged between the residues of the CAS and catalytic triad of AChE. In addition, the coumarin ring is anchored into the gorge of the enzyme by H-bond with Tyr130.Publication Open Access Assessment of in vitro cytotoxic and genotoxic activities of some trimethoprim conjugates(2018-06-01) Bayulken, Devrim Guzel; Bostancioglu, R. Beklem; Koparal, A. Tansu; Tuylu, Berrin Ayaz; Dag, AYDAN; Benkli, KADRİYE; DAĞ, AYDAN; BENKLİ, KADRIYETrimethoprim, a commonly used antibacterial agent, is widely applied in the treatment of variety of infections in human. A few studies have demonstrated an extensive exposure of man to antibiotics, but there is still a lack of data for cytotoxic effects including nephrotoxicity, gastrointestinal toxicity, hematotoxicity, neurotoxicity and ototoxicity. The main purpose behind this study was to determine cytotoxic and genotoxic activities of trimethoprim (1), trimethoprim with maleic acid (2) and trimethoprim in conjugation with oxalic acid dihydrate (3). The cytotoxic effects of these three conjugates were elucidated by employing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoium bromide (MTT) assay using embryonic rat fibroblast-like cell line (F2408) and H-ras oncogene activated embryonic rat fibroblast-like cancer cell line (5RP7). Additionally, determination of genotoxic activity of these three compounds were studied by using cytokinesis blocked micronucleus assay (CBMN) in human lymphocytes. The results demonstrated that trimethoprim alone and its combination with other compounds are able to induce both cytotoxic and genotoxic damage on cultured cells (F2408, 5RP7, human lymphocytes).Publication Open Access Cytotoxic, Apoptotic and Genotoxic Effects of Lipid-Based and Polymeric Nano Micelles, an In Vitro Evaluation(2017-11-01) BAHADORİ, FATEMEH; KOÇYİĞİT, ABDÜRRAHİM; DAĞ, AYDAN; TOPÇU, GÜLAÇTI; BAHADORİ, FATEMEH; KOÇYİĞİT, ABDÜRRAHİM; DAĞ, AYDAN; TOPÇU, GÜLAÇTISelf-assembly systems (SAS) mainly consist of micelles, and liposomes are the classes of Nano Drug Delivery Systems with superior properties compared to traditional therapeutics in targeting cancer tumors. All commercially available nano-formulations of chemotherapeutics currently consist of SAS. According to our knowledge, a specific toxicity comparison based on material differences has not yet been performed. The purpose of this study was to evaluate and compare the toxicity of two SAS consisting of Sterically Stabilized Micelles (SSM) made of a lipid-based amphiphilic distearoyl-sn-glycero-phosphatidylethanolamine-polyethylene glycol (PEG)-2000 and a polymeric micelle (PM) consisting of Y-shape amphiphilic block copolymer, synthesized using poly ε-caprolactone and PEG. The mechanism of cytotoxicity and genotoxicity of micelles on L-929 healthy mouse fibroblast cells was assessed using Sulforhodamine-B, WST-1, Acridine Orange/Ethidium Bromide and alkaline single-cell gel electrophoresis assays. Results showed that SSM in conc. of 40 mg/mL shows very low cytotoxicity at the end of 24, 48 and 72 h. The DNA damage caused by SSM was much lower than PM while the latter one showed significant toxicity by causing apoptosis with the ED50 value of 3 mg/mL. While the DNA damage caused by SSM was ignorable, some DNA chain breaks were detected on cells treated with PM.Publication Metadata only Synthesis and initial evaluation of efficacy of olean-12-en-28-ol, 3 beta-pentacosanoate for the symptomatic treatment of multiple sclerosis(2019-07-01) DAĞ, AYDAN; Sen, A.; ŞENOL, HALİL; Kale, E.; TOPÇU, GÜLAÇTI; ŞENOL, HALIL; DAĞ, AYDAN; TOPÇU, GÜLAÇTIPublication Metadata only Controlling the morphology of glyco-nanoparticles in water using block copolymer mixtures: the effect on cellular uptake(2015-01-01) Dag, AYDAN; Lu, Hongxu; STENZEL, Martina; DAĞ, AYDANBackground/purpose: Usage of barrier materials is an important step in revascularization procedure. One of the undesired properties of these barrier materials is to cause coronal tooth discoloration. The aim of this in vitro study was to evaluate the tooth discoloration induced by ProRoot MTA (PMTA), Biodentine, and MM-MTA, as well as the efficacy of internal bleaching on this discoloration. Materials and methods: Forty-two maxillary incisor teeth were prepared. Triple antibiotic paste (TAP) was placed in the root canals and incubated for 3 weeks. After removing the TAP, blood embedded spongostans were inserted into the root canals, and PMTA, Biodentine, or MM-MTA was placed over them. The teeth were incubated for 4 weeks at 37 C; then, the internal bleaching agent was sealed for one week. The tooth color was measured throughout the study and the color change values (DE) of each specimen were calculated, and the data was statistically analyzed using the one-way ANOVA and Tamhane’s T2 tests. Results: The TAP significantly decreased the luminosity of the teeth (p < 0.05); however, no significant differences were observed between the tooth discolorations induced by the PMTA, Biodentine, and MM-MTA (p > 0.05). The teeth in the Biodentine group were more whitened than those of the PMTA and MM-MTA groups (p < 0.05).Publication Metadata only Origami with ABC Triblock Terpolymers Based on Glycopolymers: Creation of Virus-Like Morphologies(2015-05-01) Dag, AYDAN; ZHAO, Jiacheng; STENZEL, Martina H.; DAĞ, AYDANMorphologies, that resemble viruses, were created using a single ABC triblock terpolymer poly(2-acryloylethyl-alpha-D-mannopyranoside)-b-poly(n-butyl acrylate)-b-poly(4-vinylpyridine) (PAcManA(70)-b-PBA(369)-b-PVP370). Morphologies ranging from flower-like micelles, cylindrical micelles, raspberry-like morphologies to nanocaterpillars were obtained by adjusting the pH value during the self-assembly process. The resulting nanoparticles had an abundance of mannose on the surface, which were recognized by the mannose receptors of RAW264.7, a macrophage cell line that can be used as a model for virus entry.