Person: GAZİOĞLU, IŞIL
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Publication Metadata only Synthesis, anticholinesterase activity and molecular modeling study of novel carbamate-substituted thymol/carvacrol derivatives(2017-02-15) KURT, Belma Zengin; Gazioglu, IŞIL; Dag, AYDAN; Salmas, Ramin Ekhteiari; Kayik, Gulru; Durdagi, Serdar; Sonmez, Fatih; ZENGİN KURT, BELMA; GAZİOĞLU, IŞIL; DAĞ, AYDANNew thymol and carvacrol derivatives with the carbamate moiety were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 5-isopropyl-2-methylphenyl(3-fluorophenyl)carbamate (29) was found to be the most potent AChE inhibitor with IC50 values of 2.22 mu M, and 5-isopropyl-2-methylphenyl (4-fluorophenyl)carbamate (30) exhibited the strongest inhibition against BuChE with IC50 value of 0.02 mu M. Additionally, the result of H4IIE hepatoma cell toxicity assay for compounds 18, 20, 29, 30 and 35 showed negligible cell death at 0.07-10 mu M. Moreover in order to better understand the inhibitory profiles of these molecules, molecular modeling studies were applied. Binding poses of studied compounds at the binding pockets of AChE and BuChE targets were determined. Predicted binding energies of these compounds as well as structural and dynamical profiles of molecules at the target sites were estimated using induced fit docking (IFD) algorithms and post-processing molecular dynamics (MD) simulations methods (i.e., Molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) approaches). (C) 2016 Elsevier Ltd. All rights reserved.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 Metadata only Comparison of antioxidant, anticholinesterase, and antidiabetic activities of three curcuminoids isolated from Curcuma longa L.(2017-01-01) Kalaycıoğlu, Zeynep; Gazioglu, IŞIL; Erim, F. Bedia; GAZİOĞLU, IŞILAntioxidant, anticholinesterase and antidiabetic activities of three curcuminoids isolated from the Curcuma longa were simultaneously tested and compared in this study. The highest antioxidant power was detected for curcumin with the applied methods. The drug potentials of curcuminoids for Alzheimer-s disease were controlled. Bisdemethoxycurcumin (BDMC) showed substantial inhibitory activity. The activity of demethoxycurcumin (DMC) followed BDMC, whereas curcumin showed very little acetylcholinesterase inhibition activity. Antidiabetic activity of curcuminoids was evaluated by their -glucosidase inhibitory activities. All curcuminoids show activities with decreasing order as BDMC>curcumin>DMC. The significant activities of BDMC compared to its isomers and examination of chemical structures of isomers might be a starting point in designing new drugs for Alzheimer-s and Diabetes Mellitus.Publication Metadata only Fatty Acid, Essential Oil and Phenolic Compositions of Alcea pallida and Alcea apterocarpa with Antioxidant, Anticholinesterase and Antimicrobial Activities(2016-01-01) Ertas, Abdulselam; Boga, Mehmet; Gazioglu, IŞIL; Yesil, Yeter; Hasimi, Nesrin; Ozaslan, Cumali; YILMAZ, Hasibe; KAPLAN, Muammer; GAZİOĞLU, IŞILThis study was the first phytochemical and biological activity report on Alcea pallida and Alcea apterocarpa extracts. The main constituents of the essential oils were identified as arachidic acid (34.2%) for A. pallida, and hexatriacontane (25.3%) for A. apterocarpa. The main constituents of the fatty acids obtained from petroleum ether extracts of A. pallida and A. apterocarpa were identified as palmitic acid (31.2%) and oleic acid (25.6%), respectively. The phenolic compositions of the samples were determined using HPLC (LC-20 liquid chromatographic system). A. pallida and A. apterocarpa showed the same peaks which were ascorbic, caffeic, salicylic and p-hydroxybenzoic acids and quercetin, respectively. Salicylic acid showed the highest abundance. Among the eight extracts, the acetone extract of A. pallida possessed the best ABTS cation radical scavenging activity and moderate butyryl-cholinesterase activity at 200 mu g/mL. The A. pallida acetone extract exhibited 53.12% inhibition in DPPH free radical scavenging activity method at 100 mu g/mL concentration. The acetone extract of A. pallida showed weak antimicrobial activity against Escherichia coli, Streptococcus pyogenes, Staphylococcus aureus, Pseudomonas aeruginosa and moderate activity against Candida albicans (inhibition zone diameter 16 mm). The acetone extract of A. apterocarpa showed moderate activity against C. albicans (inhibition zone diameter 14 mm) and S. aureus (inhibition zone diameter 13 mm); weak activity against E. coli., S0 pyogenes, and P. aeruginosa.Publication Open Access Development and validation of a HPLC method for the determination of benzo(a)pyrene in human breast milk(2017-04-01) Tekkeli, Serife Evrim Kepekci; Gazioglu, IŞIL; GAZİOĞLU, IŞIL; TEKKELİ, ŞERİFE EVRİMA simple analytical procedure was developed for the quantitation of benzo(a)pyrene in human breast milk using solid phase extraction (SPE) combined with high performance liquid chromatography. Before the chromatographic process, SPE, including C18 functional groups in silicagel cartridges, was conducted for sample preparation. A C18 column (100×4.6 mm id, 3 μm particle size) was used with acetonitrile:water (80:20) as the mobile phase at a flow rate 1mL/min at 30°C. Fluorimetric detection was performed for excitation and emission at 290 and 406 nm, respectively. It was observed that the calibration curve was linear over the range of 0.5-80 ng/mL. The limit of detection and limit of quantitation were found to be 0.5 and 1.07 ng/mL, respectively. Intraday and interday relative standard deviation values were less than 5.15%. Moreover, the newly developed method provides a fast, simple, cost effective, and sensitive assay to detect an important carcinogen substance, benzo(a)pyrene, in human breast milk.Publication Metadata only Synthesis, Anticholinesterase, Antioxidant, and Anti-Aflatoxigenic Activity of Novel Coumarin Carbamate Derivatives(2018-04-17) KURT, Belma Zengin; Gazioglu, IŞIL; KANDAS, Nur Ozten; Sonmez, Fatih; ZENGİN KURT, BELMA; GAZİOĞLU, IŞILNew coumarin derivatives with the carbamate moiety were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 4-methyl-2-oxo-2H-chromen-7-yl cycloheptylcarbamate (4h) showed the strongest inhibition against AChE with IC50 values of 2.30 mu M, and 2-oxo-2H-chromen-7-yl-(cyclohexylmethyl)carbamate (4c) and 4-methyl-2-oxo-2H-chromen-7-yl-(cyclohexylmethyl)carbamate (4g) were found to be the most potent BuChE inhibitors with IC50 value of 0.003 mu M and 0.004 mu M, respectively. Moreover antioxidant, anti-aflatoxigenic activities, protective effects against aflatoxin-B1 (AFB1) in H4IIE-C3 cells and effects on glutathione s-transferase of the synthesized compounds were investigated. The synthesized coumarin carbamates inhibited AFB1 in H4IIE-C3 cells. Western blot analyses confirmed that GST alpha protein was induced in cells treated with coumarin carbamates and AFB1. These results showed that the synthesized coumarin carbamates possess a potent protective effect against AFB1.Publication Metadata only Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer-s disease(2015-09-18) Kurt, BELMA; Gazioglu, IŞIL; BASILE, Livia; Sonmez, Fatih; GINEX, Tiziana; Kucukislamoglu, Mustafa; GUCCIONE, Salvatore; ZENGİN KURT, BELMA; GAZİOĞLU, IŞILNew benzofuranylthiazole derivatives containing the aryl urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. The result showed that all the synthesized compounds exhibited inhibitory activity on both AChE and BuChE with 1-(4-(5-bromobenzofuran-2-yl)thiazol-2-yl)-3-(2fluorophenyl)urea (e25, IC50 value of 3.85 mu M) and 1-(4-iodophenyl)-3-(4-(5-nitrobenzofuran-2-yl) thiazol-2-yl)urea (e38, IC50 value of 2.03 mu M) as the strongest inhibitors against AChE and BuChE, respectively. Compound e38 was 8.5-fold more potent than galanthamine. The selectivity index of e25 and e38 was 2.40 and 0.37 against AChE and BuChE, respectively. Compound e2, e4 and ell (IC50 = 0.2, 0.5 and 1.13 mu M, respectively) showed a better ABTS cation radical scavenging ability than the standard quercetin (IC50 = 1.18 AM). Best poses of compounds e38 on BuChE and e25 on AChE indicate that the thiazole ring and the amidic moiety are important sites of interaction with both ChEs. In addition, the benzofuran ring and phenyl ring are anchored to the side chains of both enzymes by pi-pi(pi-pi) interactions. (C) 2015 Elsevier Masson SAS. All rights reserved.Publication Metadata only Capparis ovata treatment suppresses inflammatory cytokine expression and ameliorates experimental allergic encephalomyelitis model of multiple sclerosis in C57BL/6 mice(2016-09-15) Ozgun-Acar, Ozden; Celik-Turgut, Gurbet; Gazioglu, IŞIL; Kolak, Ufuk; Ozbal, Seda; Ergur, Bekir U.; Arslan, Sevki; Sen, Alaattin; Topcu, GÜLAÇTI; GAZİOĞLU, IŞIL; TOPÇU, GÜLAÇTISince ancient times, Capparis species have been widely used in traditional medicine to treat various diseases. Our recent investigations have suggested Capparis ovata-s potential anti-neuroinflammatory application for the treatment of multiple sclerosis (MS). The present study was designed to precisely determine the underlying mechanism of its anti-neuroinflammatory effect in a mouse model of MS. C. ovata water extract (COWE) was prepared using the plant-s fruit, buds, and flower parts (Turkish Patent Institute, PT 2012/04,093). We immunized female C57BL/6 J mice with MOG(35_55)/CFA. COWE was administered at a daily dose of 500 mg/Kg by oral gavage either from the day of immunization (T1) or at disease onset (12) for 21 days. Gene expression analysis was performed using a Mouse Multiple Sclerosis RT2 Profiler PCR Array, and further determinations and validations of the identified genes were performed using qPCR. Whole-genome transcriptome profiling was analyzed using Agilent SurePrint G3 Mouse GE 8X60K microarrays. Immunohistochemical staining was applied to brain sections of the control and treated mice to examine the degree of degeneration. COWE was further fractionated and analyzed phytochemically using the Zivak Tandem Gold Triple Quadrupole LC/MS-MS system. COWE remarkably suppressed the development of EAE in T1, and the disease activity was completely inhibited. In the T2 group, the maximal score was significantly reduced compared with that of the parallel EAE group. The COWE suppression of EAE was associated with a significantly decreased expression of genes that are important in inflammatory signaling, such as TNF alpha, IL6, NF-kappa B, CCL5, CXCL9, and CXCK10. On the other hand, the expression of genes involved in myelination/remyelination was significantly increased. Immunohistochemical analysis further supported these effects, showing that the number of infiltrating immune cells was decreased in the brains of COWE-treated animals. In addition, differential expression profiling of the transcriptome revealed that COWE treatment caused the down regulation of a group of genes involved in the immune response, inflammatory response, antigen processing and presentation, B-cell-mediated immunity and innate immune response. Collectively, these results suggest anti-neuroinflammatory mechanisms by which COWE treatment delayed and suppressed the development of EAE and ameliorated the disease in mice with persistent clinical signs. (C) 2016 Elsevier B.V. All rights reserved.Publication Metadata only A detailed study on the chemical and biological profiles of essential oil and methanol extract of Thymus nummularius (Anzer tea): Rosmarinic acid(2015-05-01) Ertas, Abdulselam; Boga, Mehmet; Yilmaz, Mustafa Abdullah; Yesil, Yeter; Tel, Gulsen; Temel, Hamdi; Hasimi, Nesrin; Gazioglu, IŞIL; Ozturk, Mehmet; Ugurlu, Pelin; GAZİOĞLU, IŞILThe aim of this study was to determine the chemical profile of Thymus nummularius by LC-MS/MS and GC/MS. Additionally, the methanol extract, essential oil and some individual main compounds of Thymus nummularius were tested for antioxidant, anticholinesterase and antimicrobial activities. Besides, HPLC-FLD was used to determine total aflatoxin in the plant material. Among the twenty-seven compounds studied by LC-MS/MS, rosmarinic acid (131,898.9 +/- 6463.0 mu g/g dry-extract) was found to be the most abundant compound in the methanol extract. On the other hand, thymol (60.38%) and terpinyl-acetate (10.49%) were found to be the major compounds of the essential oil. Both the essential oil and the methanol extract of T. nummularius exhibited strong antioxidant activity in the four tested methods. Furthermore, the essential oil showed high inhibitory activity against acetyl-,butyryl-cholinesterase enzymes and very strong antimicrobial activity against all tested microorganisms. Besides, T. nummularius can be used both as rosmarinic acid source and as food supplement due to its non-aflatoxin content and high antioxidant, anticholinesterase and antimicrobial activities. (C) 2015 Elsevier B.V. All rights reserved.Publication Metadata only Chemical Profile of Malva Neglecta and Malvella Sherardiana by LC-MS/MS, GC/MS and Their Anticholinesterase, Antimicrobial and Antioxidant Properties With Aflatoxin-Contents(2017-01-01) Hasimi, Nesrin; Ertas, Abdulselam; Oral, Elif Varhan; Alkan, Huseyin; Boga, Mehmet; Yilmaz, Mustafa Abdullah; Yener, Ismail; Gazioglu, IŞIL; Ozaslan, Cumali; AKDENIZ, Mehmet; Kolak, Ufuk; GAZİOĞLU, IŞILThe purpose of the present work was to determine the phenolic and the fatty acids profiles by LC-MS/MS and GC/MS with their antioxidant, anticholinesterase and antimicrobial activities, and aflatoxin contents of Malva neglecta and Malvella sherardiana. The phenolic contents of M. neglecta and M. sherardiana were determined by LC-MS/MS. Malic and 4-OH benzoic acids were found to be the most abundant compounds in M. neglecta and M. sherardiana, respectively. On the other hand, essential oil and fatty acid compositions were determined by GC/MS analysis. The methanol extracts of the plants showed the highest effect in all antioxidant assays in this study. The methanol extract of M. neglecta showed the highest activity among the petroleum ether, acetone, methanol and water extracts against acetyl-and butyryl-cholinesterase enzymes (53.68% and 63.95% inhibition ratio, respectively). The acetone extracts of M. neglacta and M. sherardiana exhibited moderate activity against C. albicans with 18 and 17 mm inhibion zone diameter, respectively. The results of the present study is also showed that the M. neglecta and M. sherardiana can also be used as a food source due to its high phenolic acid content and good antioxidant property. Also, the samples were aflatoxin free.