Yazar "Kocyigit, Umit Muhammet" seçeneğine göre listele
Listeleniyor 1 - 13 / 13
Sayfa Başına Sonuç
Sıralama seçenekleri
Öğe ANTIDIABETIC PROPERTIES OF QUEBECOL AS NATURAL PHENOLIC COMPOUND: alpha -GLYCOSIDASE AND alpha -AMYLASE METABOLIC ENZYMES INHIBITION PROPERTIES(PARLAR SCIENTIFIC PUBLICATIONS (P S P), 2019) Kocyigit, Umit MuhammetThis study aims to examine the inhibitory effect of Quebecol on alpha-glycosidase and alpha-amylase enzyme activities in comparison with acarbose as a standard. IC50 amounts were obtained by using the Quebecol-Induced Activity (%) - [Quebecol] graph and the Lineweaver-Burk graph. The IC50 values obtained with Quebecol were 28.56 nM for alpha-glycosidase and 211.82 nM for alpha-amylase, while the mean K-i value was 8.04 nM for alpha-glycosidase. The results of our study are expected to contribute to pharmaceutical research and pharmacological applications by providing insight into the biological effects of Quebecol.Öğe BIOLOGICAL EVALUATION OF 1-(4-(HYDROXY(1-OXO-1,3-DIHYDRO-2H-INDEN-2-YLI-DENE)METHYL)PHENYL)-3-PHENYLUREA DERIVATIVES: ANTICHOLINERGICS AND ANTIEPILEPTIC POTENTIALS(PARLAR SCIENTIFIC PUBLICATIONS (P S P), 2019) Kocyigit, Umit MuhammetIn this work, a class of phenylurea compounds containing 2-benzoylindan-1-one molecules 3a-3j was designed and synthesized from the reaction of phenylurea-substituted acetophenone compounds with phthalaldehyde molecule under mild action situations in good yields. The inhibitory effect of these compounds on some metabolic enzymes was examined and compared with a standard compound. IC50 values were obtained from the phenylurea-Induced Activity (%)-[phenylurea compounds] graph and from the Lineweaver-Burk graph. According to the results, the IC50 values of these molecules were in the range 18.23-63.01 nM for hCA I, while the mean K-i values were in the range 7.79 +/- 0.94-122.64 +/- 32.15 nM for this enzyme. The results obtained are expected to make an important contribution to drug design and pharmacological applications. Additionally, these compounds demonstrated well inhibitory effects against acetylcholineesterase (AChE) enzyme. Finally, the K-i values of hCA II were in the range 15.09 +/- 4.48-65.72 +/- 6.64 nM and 1.54 +/- 0.21-22.44 3.83 nM against AChE, respectively.Öğe Design and Synthesis of Pyrazole Carboxamide Derivatives as Selective Cholinesterase and Carbonic Anhydrase Inhibitors: Molecular Docking and Biological Evaluation(Wiley-V C H Verlag Gmbh, 2024) Durgun, Mustafa; Akocak, Suleyman; Lolak, Nebih; Topal, Fevzi; Kocyigit, Umit Muhammet; Turkes, Cueneyt; Isik, MesutThe present study focused on the synthesis and characterization of novel pyrazole carboxamide derivatives (SA1-12). The inhibitory effect of the compounds on cholinesterases (ChEs; AChE and BChE) and carbonic anhydrases (hCAs; hCA I and hCA II) isoenzymes were screened as in vitro. These series compounds have been identified as potential inhibitors with a KI values in the range of 10.69 +/- 1.27-70.87 +/- 8.11 nM for hCA I, 20.01 +/- 3.48-56.63 +/- 6.41 nM for hCA II, 6.60 +/- 0.62-14.15 +/- 1.09 nM for acetylcholinesterase (AChE) and 54.87 +/- 7.76-137.20 +/- 9.61 nM for butyrylcholinesterase (BChE). These compounds have a more effective inhibition effect when compared to the reference compounds. In addition, the potential binding positions of the compounds with high affinity for ChE and hCAs were demonstrated by in silico methods. The results of in silico and in vitro studies support each other. As a result of the present study, the compounds with high inhibitory activity for metabolic enzymes, such as ChE and hCA were designed. The compounds may be potential alternative agents used as selective ChE and hCA inhibitors in the treatment of Alzheimer ' s disease and glaucoma. imageÖğe The effects of wireless electromagnetic fields on the activities of carbonic anhydrase and acetylcholinesterase enzymes in various tissues of rats(WILEY, 2018) Kocyigit, Umit Muhammet; Taslimi, Parham; Gurses, Fatih; Soylu, Sinan; Dastan, Sevgi Durna; Gulcin, IlhamiThe purpose of our study is to assist in understanding the effects of wireless electromagnetic waves on carbonic anhydrase (CA) and acetylcholinesterase (AChE) enzymes activities in the different tissues of the rats. For this purpose, two different groups each of which contains eight rats (n=8) were formed as being control group and wireless electromagnetic wave-administered group. The rats were necropsied after 60min from the injection of chemicals into the rats intraperitoneally. The different tissues of the rats were extracted. CA and AChE enzymes activities were measured for each tissue. All the experimental results were provided in mean +/- S.D. Statistical significance was identified to be P<0.05. It was observed that there were significant changes of enzyme activities in wireless-administered group in salivary gland, stomach, colon, liver, and striated muscle tissues.Öğe Evaluation of Anticholinergic, Antidiabetic and Antioxidant Activity of Astragalus dumanii, an Endemic Plant(Kahramanmaras Sutcu Imam Univ Rektorlugu, 2022) Kocyigit, Umit Muhammet; Eruygur, Nuraniye; Atas, Mehmet; Tekin, Mehmet; Taslimi, Parham; Gokalp, Faik; Gulcin, IlhamiThe research was conducted to separately evaluate and detect the possible in vitro antioxidant, antimicrobial activity of ethanol extracts prepared from aerial parts and roots of Astragalus dumanii and anti-cholinesterase and alpha-glucosidase inhibitory activity from only aerial parts of its The antioxidant capacity was tested by scavenging of DPPH and ABTS free radicals. Compared with the standard antioxidant compound gallic acid; Root and aerial part extract showed lower DPPH radical scavenging activity, however aerial part extract demonstrated higher ABTS radical scavenging activity. The phenolic contents were detected as 5.31 +/- 0.03 and 13.23 +/- 0.05 mg gallic acid equivalent g-1 extract, flavonoid contents were found as 8.26 +/- 0.004 and 7.93 +/- 0.005 mg Qercetin equivalent g-1 extract. In addition, the effects of the extracts obtained from aerial parts of the plant on acetylcholinesterase, butyrylcholinesterase and a-glycosidase enzymes were investigated in vitro and IC50 values were obtained as 1.47, 0.83 and 0.48 mu g mL-1, respectively. When these values were compared with standard substances, it was seen that Astragalus dumanii could be a good enzyme inhibitory agent. Antimicrobial activity of the plant extracts were determined using the microdilution method and the extracts was not observed to have any antimicrobial activities..Öğe Exploring the Antioxidant, Antimicrobial, Antidiabetic, and Anticancer Properties of Capsicum annuum L. (Samandağ Pepper): Biochemical and In Silico Insights(Wiley-V C H Verlag Gmbh, 2024) Tunc, Tutku; Ozpinar, Hulya; Kocyigit, Umit Muhammet; Erkan, SultanCapsicum annuum L. species from the Samanda & gbreve; district of Hatay/Turkey was used in our study. Phytochemical analysis of seed and fruit ethanol extracts of this plant was carried out by GC-MS method. Total Antioxidant Status (TAS) and Total Oxidant Status (TOS) levels were determined to calculate the Oxidative Stress Index to determine antioxidant activity. MIC method was used to evaluate antimicrobial properties against pathogenic bacteria and fungi. Anticancer activity was determined by the XTT assay on breast (MCF-7), lung (A549) and brain (C6) cancer cells and healthy fibroblast (WI-38) cell lines. The effects of the extracts on acetylcholinesterase and alpha-amylase activities were investigated. It was found that C. annuum fruit extract had a lower OSI value than the seed extract. Fruit and seed extracts showed antimicrobial activity on microorganisms at MIC values of 200 mu g/mL. Molecular docking studies were conducted to analyze the antibacterial properties of plant active ingredients. These studies are chemical components that are determined to be more abundant in the plant extract. Thus, it aimed to evaluate the effects of active compounds on various bacterial species. The results revealed the potential antibacterial properties of plants and provided important data that these ingredients can be used in future treatment methods. The anticancer activity in all cancer cell lines was very high in both seed and fruit extracts with a selectivity index (SI) well above SI >= 3. Furthermore, no deleterious effect on healthy fibroblast (WI-38) cells was observed. The extracts were found to decrease acetylcholinesterase activity but increase alpha-amylase activity. As a result, these plant extracts were found to have anticholinergic potential.Öğe Investigation of Antiepileptic and Anticancer Properties of Some Plant Species Traditionally Used in Turkey(Colegio de Farmaceuticos de la Provincia de Buenos Aires, 2024) Ozpinar, Hulya; Bostanci, Hayrani Eren; Hurmet, Melahat; Kocyigit, Umit MuhammetThe study investigated the antiepileptic and anticancer properties of water and ethanol extracts from plant species traditionally used in Turkey, including Centaurea solstitialis subsp. solstitialis (CSS), Tragopogon reticulatus (TR), Erodium cicutarium subsp. cicutarium (ECC), Alyssum alyssoides (AA) and Leontice leontopetalum subsp. leontopetalum (LLL) using apoptosis and cell cycle studies. In the investigation of the antiepileptic properties of plant extracts, the effects on the activities of carbonic anhydrase I and II isoenzymes were measured spectrophotometrically. In anticancer studies, all extracts were applied to human stomach cancer cell line (AGS), human breast cancer cell line (MCF7) and rat glioma cell line (C6) and their cytotoxicity in healthy mouse fibroblast cell line (L929) was compared using the MTT method. All extracts of ECC inhibited carbonic anhydrase I and II isoenzymes at lower concentrations than the standard substance. However, aqueous extracts of all plants had a highly toxic effect on rat glioma cell line (C6), without damaging healthy cells. © 2024, Colegio de Farmaceuticos de la Provincia de Buenos Aires. All rights reserved.Öğe Novel piperazine and morpholine substituted quinolines: Selective synthesis through activation of 3,6,8-tribromoquinoline, characterization and their some metabolic enzymes inhibition potentials(Elsevier, 2020) Cakmak, Osman; Okten, Salih; Alimli, Dilek; Ersanli, Cem Cuneyt; Taslimi, Parham; Kocyigit, Umit MuhammetRegioselective routes are described for convenient preparation of novel piperazine/morpholine substituted quinoline derivatives at C-3, C-6 and C-8 starting with 3,6,8-tribromoquinoline (6) by nucleophilic substitution via conventional heating or microwave assisted reaction conditions. 3,6,8-Tribromoquinoline (6) was treated with piperazine and morpholine under microvawe irradiation, which selectively furnished 3-mopholinyl and 3-piperazinyl quinoline derivatives 7 and 8 in yields of 58% and 60%, respectively. On the other hand, the activation of benzene cycle of quinoline by nitration of 3,6,8-tribromoquinoline, giving 5-nitro-3,6,8-tribromoquinoline (18) in quantitative yield, was enabled. Then, the bromines at C-6 and C-8 were selectively exchanged by morpholine and piperazine via SNAr reactions. Thus, 6,8-dimopholinylquinoline (22) and 5-nitro-6,8-dipiperazinylquinoline (24), biologically valuable derivatives, were prepared in high yields (82% and 72%, respectively). The synthesized compounds were fully characterizated by H-1 NMR, C-13 NMR, 2D NMR, XRD, HRMS and IR spectra. The novel molecules had effective inhibition profiles against some metabolic enzymes. Also, they have the potential of drug candidates to treat of some diseases including glaucoma, epilepsy, Alzheimer's disease (AD), leukemia, and type-2 diabetes mellitus (T2DM). (C) 2020 Elsevier B.V. All rights reserved.Öğe SAR Evaluation of Disubstituted Tacrine Analogues as Promising Cholinesterase and Carbonic Anhydrase Inhibitors(ASSOC PHARMACEUTICAL TEACHERS INDIA, 2019) Okten, Salih; Ekiz, Makbule; Tutar, Ahmet; Butun, Burcu; Kocyigit, Umit Muhammet; Topcu, Gulacti; Gulcin, IlhamiBackground: The inhibition of both hydrolysis products of acetylcholine (ACh), Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE), is essential for successful treatment of Alzhemier patients. Objectives: This study was investigated inhibition potentials of recently synthesized disubstituted tacrines derivatives on going our research against AChE, BChE and carbonic anhydrase cyctosolic (hCA I and H) enzymes to explore the Structure activity relationship (SAR). Methods: Inhibitory activities of tested compounds against AChE and BChE were measured by spectrophotometric method, developed by Ellman et al. Furthermore, the disubstituted tacrines were determined as inhibitors of two physiologically relevant CA isoforms, the cytosolic hCA I and H by an esterase assay method. Results: The silyl, thiomethyl and cyano substituted seven membered hydrocycle tacrines (9, 11 and 14) significantly inhibited AChE, compared with starting compound 3 (6,8-dibromo-2,3,4,5-teytrahydro-1H-cyclohepta[1,2-b] quinoline) and reference compounds, galantamine and tacrine, while methoxy substituted seven membered hydrocycle tacrine derivative 10 showed selective inhibition against BChE (IC50 = 563 nM). Interestingly, disubstituted tacrines displayed higher or parallel inhibition to galantamine. Additionally, all these tacrine analogues were recorded to be powerful inhibitor compounds of the cytosolic isoenzyme hCA I with K-i in the range of 43.81-471.67 nM, as well as a moderate selectivity toward hCA II isoenzyme with K-i in the range from 87.14 to 614.68 nM compared with AZA, as standard. Conclusion: The disubstituted seven membered hydrocycle tacrine analogues 9-12 and 14 may have promising anti Alzhemier drug candidate and dibromo six membered hydrocycle 2 and dibromo seven membered hydrocycle 3 derivatives may be novel hCA I and II enzyme inhibitors.Öğe Sulfonamide-Bearing Pyrazolone Derivatives as Multitarget Therapeutic Agents: Design, Synthesis, Characterization, Biological Evaluation, In Silico ADME/T Profiling and Molecular Docking Study(John Wiley & Sons Ltd, 2025) Lolak, Nebih; Akocak, Suleyman; Topal, Meryem; Kocyigit, Umit Muhammet; Isik, Mesut; Turkes, Cuneyt; Topal, FevziThe research and design of new inhibitors for the treatment of diseases such as Alzheimer's disease and glaucoma through inhibition of cholinesterases (ChEs; acetylcholinesterase, AChE and butyrylcholinesterase, BChE) and carbonic anhydrase enzymes are among the important targets. Here, a series of novel sulfonamide-bearing pyrazolone derivatives (1a-f and 2a-f) were successfully synthesized and characterized by using spectroscopic and analytical methods. The inhibitory activities of these newly synthesized compounds were evaluated both in vitro and in silico for their effect on carbonic anhydrases (hCA I and hCA II isoenzymes) and ChEs. The in vitro studies showed that these novel compounds demonstrated potential inhibitory activity, with K-I values covering the following ranges: 18.03 +/- 2.86-75.54 +/- 4.91 nM for hCA I, 24.84 +/- 1.57-85.42 +/- 6.60 nM for hCA II, 7.45 +/- 0.98-16.04 +/- 1.60 nM for AChE, and 34.78 +/- 5.88-135.70 +/- 17.39 nM for BChE. Additionally, many of these compounds showed promising inhibitory activity, and some showed higher potency than reference compounds. While the in silico studies have also identified the potential binding positions of these compounds, using the crystal structures of hCA I, II, AChE and BChE receptors. The varying affinities demonstrated by these designed compounds for ChEs and hCA isoenzymes show that these compounds could hold promise as potential alternative agents for selectively inhibiting ChEs and hCAs in the treatment of diseases such as Alzheimer's disease and glaucoma.Öğe Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles(TAYLOR & FRANCIS LTD, 2018) Kocyigit, Umit Muhammet; Budak, Yakup; Gurdere, Meliha Burcu; Erturk, Fatih; Yencilek, Belkiz; Taslimi, Parham; Gulcin, Ilhami; Ceylan, MustafaThe new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06-67.46 mu M. IC50 value of 5-fluorouracil (5-FU) was 90.36 mu M. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 +/- 227.4nM against CA I, and 904.47 +/- 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 +/- 58.33 nM.Öğe Synthesis of Nanoparticles Loading Indenopyrazole Derivatives and Evaluation of Biological Features(Marmara Univ, Inst Health Sciences, 2022) Dogan, Murat; Kocyigit, Umit Muhammet; Gezegen, HayreddinObjective: In this study, it was aimed to prepare nanoparticle formulations using chitosan, a cationic natural polymer, and tripoly phosphate, and to perform mechanical characterization and in vitro cell culture studies. In addition, the cytotoxic effects of nanoparticles containing indenopyrazol derivatives against human glioma cells (C6) and human cervical cancer cells (HeLa) were investigated. Methods: Within the scope of the study, nanoparticles containing indenopyrazole derivative were prepared and characterization of particle size, zeta potential and morphological properties were performed. XTT cytotoxicity test was applied to evaluate the antiproliferative activities of nanoparticles containing these components. Results: Particle size, zeta potential and morphological properties of nanoparticles were observed to be suitable for application. In vitro cell culture studies showed that nanoparticles containing indenopyrazol derivatives showed better cytotoxic effects in both cell lines. Conclusion: The results showed that the mechanical properties of nanoparticles containing indenopyrazol derivatives are suitable and can be applied in anticancer activity studies.Öğe Synthesis, characterization, crystal structures, theoretical calculations and biological evaluations of novel substituted tacrine derivatives as cholinesterase and carbonic anhydrase enzymes inhibitors(ELSEVIER SCIENCE BV, 2019) Okten, Salih; Ekiz, Makbule; Kocyigit, Umit Muhammet; Tutar, Ahmet; Celik, Ismail; Akkurt, Mehmet; Gokalp, Faik; Taslimi, Parham; Gulcin, IlhamiThe six and seven hydrocycle membered disilylanilino acridine (tacrine) analogues (9-11) were synthesized by one-pot procedures. The structures of novel silyl tacrine derivatives were characterized by NMR spectroscopy, elemental analysis and XRD investigations. The silyl substituted novel tacrine derivatives (9-11) were investigated as cholinesterase inhibitors and defined the relative role of AChE (Acetylcholinesterase) versus BChE (Butyrylcholinesterase) inhibition. Novel substituted tacrine derivatives are known as important inhibitors of Carbonic anhydrase (CA) isoenzymes I, and II (hCA I and II), therefore, the synthesized compounds (9-11) were investigated for inhibitory effects on the both CA isoenzymes. Additionally, we evaluated four different enzymes, which were inhibited in the very low nanomolar (nM) range by these compounds. According to the present studies, for AChE, BChE, hCA I and II, the ranges of results are recorded as 30.26 +/- 6.71-117.54 +/- 42.22 nM, 22.45 +/- 5.81-77.41 +/- 4.02 nM, 57.28 +/- 22.16-213.41 +/- 82.75 nM and 46.95 +/- 11.32-274.94 +/- 62.15 nM, respectively. (C) 2018 Elsevier B.V. All rights reserved.
