Person:
ZENGİN KURT, BELMA

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Organizational Unit

Eczacılık Fakültesi

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BELMA

Last Name

ZENGİN KURT

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Now showing 1 - 10 of 10

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, AYDAN
New 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.
Open Access
Biological activities and chemical composition of Turkish sweetgum balsam (Styrax liquidus) essential oil
(2022-01-01T00:00:00Z) BÜYÜKKILIÇ ALTINBAŞAK, BETÜL; İSSA, GHASSAN; ZENGİN KURT, BELMA; DEMİRCİ, BETÜL; BÜYÜKKILIÇ ALTINBAŞAK, BETÜL; ZENGİN KURT, BELMA
Objective: The purpose of this present study was to make a chemical analysis of the composition of essential oil obtained from sweetgum balsam and to examine its antimicrobial, anticholinesterase, α-glucosidase inhibition, and antioxidant activities. Methods: The essential oil obtained by the hydrodistillation method was analyzed by gas chromatography-mass spectrometry systems. The antimicrobial activities of the essential oil were evaluated by disc diffusion and resazurin microplate methods, the anticholinesterase effect was determined by using in vitro AChE and BChE enzymes inhibition assays, and the antioxidant effect was evaluated by ABTS and CUPRAC methods. Results: The main components of the essential oil were determined as styrene (92.6%) and α-pinene (2.2%). The essential oil showed weak antimicrobial activity against K. pneumoniae, S. epidermidis but strong antimicrobial activity against A. baumannii, C. glabrata. It showed moderate inhibitory activity to AChE and BChE enzymes, and IC50 values were calculated as 36.5 μg/mL and 69.5 μg/mL, respectively. It also showed low inhibition of α-glucosidase (IC50 value was 637.2 μg/mL) and a similar antioxidant effect in the CUPRAC and ABTS method (A0.5 value was 637.2 μg/mL and IC50 value was 632.2 μg/mL, respectively). Conclusion: Styrax Liquidus essential oil can be considered a natural antimicrobial agent due to its strong antimicrobial activity capacity against A. baumannii and C. glabrata strains
Open Access
Structural and mechanical analysis of three orthodontic adhesive composites cured with different light units
(2020-04-01T00:00:00Z) YILMAZ, BERZA; BAKKAL, MELTEM; Kurt, BELMA; YILMAZ, BERZA; BAKKAL, MELTEM; ZENGİN KURT, BELMA
Objective: To evaluate the effects of three different curing units on the physical and mechanical features of three different orthodontic adhesive resin materials. Material and Methods: 45 specimens (5 mm in diameter, and 2 mm in thickness) of each of the three different adhesive composite resin materials (Transbond XT, Grēngloo™ Adhesive and Light Bond Paste) were cured with three different light units (a polywave third generation (Valo), a monowave (DemiUltra), and a second-generation LED (Optima 10)). To quantify degree of conversion (DC), the Attenuated Total Reflectance Fourier Transform Infrared Spectroscopy was used in transmission mode (ALPHA FT-IR Spectrometer, Bruker Optics, Germany). Vickers hardness value was recorded under constant load 100 g for 10 s with a microhardness tester (HMV M-1, Shimadzu Corp., Kyoto, Japan). The data were statistically analyzed using Kruskal-Wallis and chi-square tests. The level of significance was considered p<0.05. Results: The highest DC values were obtained as a result of curing with Optima 10. This rate was followed by Demi Ultra and Valo, respectively. Transbond XT samples showed a lower level of conversion than the samples of Light Bond Paste and Grēngloo™ Adhesive. The top surfaces of each material showed higher hardness values than the bottom surfaces (p<0.05). The Light Bond Paste showed the highest hardness values both on the top and bottom surfaces among the three materials, followed by Grēngloo™ Adhesive. While the hardness values of the top surfaces of the samples cured with Demi Ultra and Valo light units were similar, higher hardness values are recorded with Valo on the bottom surfaces (Valo; 85.200/75.200 (top/bottom) versus Demi Ultra; 86.100/66.000 (top/bottom)). Conclusions: The different DC and the surface hardness properties were recorded for the resin as orthodontic adhesives depending on different light units. Shorter radiation time caused lower DC and surface hardness values.
Open Access
Anticholinesterase, antioxidant, antiaflatoxigenic activities of ten edible wild plants from Ordu area, Turkey
(2018-06-01) Kurt, BELMA; GAZİOĞLU, IŞIL; SEVGİ, ECE; Sönmez, Fatih; ZENGİN KURT, BELMA; GAZİOĞLU, IŞIL; SEVGİ, ECE
Turkey has highly rich floras of medicinal and aromatic plants because of having various climate conditions in different regions. One of these regions is Middle Black Sea Region, especially Ordu Province. Extracts of 10 edible plants (Arum maculatum L., Hypericum orientale L., Ornithogalum sigmoideum Freyn et Sint., Silene vulgaris Garcke var. macrocarpa, Plantago lanceolata L., Achillea millefolium L. subsp. pannonica, Rumex crispus L., Rumex acetosella L., Capsella bursa-pastoris L., Coronopus squamatus Asch.), grown in Ordu, Turkey, were prepared with different solvents (hexane, ethanol and water, separately) and their anticholinestrase and antiaflatoxigenic activities were evaluated. Additionally, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the extracts were assayed. The ethanol extract of R. acetosella exhibited the highest antioxidant activity (A0.5 value of 25.31 µg/mL, for CUPRAC activity; IC50 value of 23.73 µg/mL, for ABTS activity). The hexane extract of C. bursa-pastoris showed the strongest inhibition against AChE enzyme with IC50 value of 7.24 µg/mL, and the hexane extract of A. millefolium subsp. pannonica had the highest BChE activity with IC50 value of 6.40 µg/mL. The ethanol extract of P. lanceolata exhibited the strongest inhibition against aflatoxin with 88% inhibition.
Open Access
Synthesis, Biological Activity and Multiscale Molecular Modeling Studies for Coumaryl-carboxamide Derivatives as Selective Carbonic Anhydrase IX Inhibitors
(2017-08-01) Supuran, Claudiu T.; ZENGİN KURT, BELMA; Sonmez, Fatih; Durdağı, Serdar; Aksoydan, Busecan; Angeli, Andrea; Küçükislamoğlu, Mustafa; ZENGİN KURT, BELMA
New coumaryl-carboxamide derivatives with the thiourea moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and their inhibitory activity against the human carbonic anhydrase (hCA) isoforms hCA I, II, VII and IX were evaluated. While the hCA I, II and VII isoforms were not inhibited by the investigated compounds, the tumour-associated isoform hCA IX was inhibited in the high nanomolar range. 2-Oxo-N-((2-(pyrrolidin-1-yl)ethyl)carbamothioyl)-2H-chromene-3-carboxamide (e11) exhibited a selective inhibitory action against hCA IX with the Ki of 107.9 nM. In order to better understand the inhibitory profiles of studied molecules, multiscale molecular modeling approaches were used. Different molecular docking algorithms were used to investigate binding poses and predicted binding energies of studied compounds at the active sites of the CA I, II, VII and IX isoforms.
Open Access
Electrical and optical characterization of Os-substituted rare-earth orthoferrite YbFeO3-gamma powders
(2021-01-01T00:00:00Z) Polat, O.; Coskun, M.; Sobola, D.; ZENGİN KURT, BELMA; Caglar, M.; Turut, A.; ZENGİN KURT, BELMA
The electrical properties of Os-doped YbFeO3 (YbFO) powders prepared by solid-state reaction have been studied by Impedance Spectrometer/Impedance Spectrometer. SEM, XPS and Raman spectroscopy were utilized for understanding chemical and structured analysis of the synthesized compounds. SEM images have revealed the void nature of the pellets. Furthermore, XPS studies have exhibited that Yb has 3+valance state. It is also revealed that the oxygen vacancies concentration drops as the Os doping level raises by XPS analysis. The frequency dependency of loss-tan(delta) examination has demonstrated that the 5 mol% Os-substituted sample has the lowest loss-tan(delta) values at high frequency regions at 100 degrees C. It has been also realized that the 5 mol% Os-doped compound exhibits the highest resistivity among the samples. Raman spectroscopy examination has unveiled that the samples have similar space group. In addition, the optical band gap of the synthesized powders was also extracted via utilizing the Kubelka-Munk technique. It was realized that the band gap of YbFO slightly increases as the Os dopant ratio advances.
Open Access
Synthesis, spectral properties, α-glucosidase inhibition, second-order and third-order NLO parameters and DFT calculations of Cr(III) and V(IV) complexes of 3-methylpicolinic acid
(2020-11-15T00:00:00Z) Avcı, Davut; Altürk, Sümeyye; Sönmez, Fatih; Tamer, Ömer; Başoğlu, Adil; Atalay, Yusuf; Kurt, BELMA; Dege, Necmi; ZENGİN KURT, BELMA
The Cr(III) and V(IV) complexes of 3-methylpicolinic acid (3-mpaH) were synthesized. The XRD and LC-MS/MS were performed to determine experimental geometric structure of the synthesized complexes. Their experimental spectral analyses were carried out by FT-IR and UV-Vis spectra. Their alpha-glucosidase activities were also evaluated. The synthesized Cr(III) and V(IV) complexes exhibited alpha-glucosidase inhibitory activity with the IC50 values of >600 mu M. Furthermore, the optimal molecular structure geometries, vibrational frequencies, electronic spectral properties, refractive index, band gap, second- and third-order nonlinear optical (NLO) parameters of these complexes were obtained by using DFT/HSEh1PBE/6-311G (d,p)/LanL2DZ level. NLO results demonstrate that the complex 1 is a promising candidate to materials with the high first- and second-order hyperpolarizability values obtained at 55.3 x 10(-30) and 251.0 x 10(-36) esu in ethanol solvent. The experimental refractive index and band gap parameters were comparatively presented. Lastly, NBO analysis was fulfilled to investigate inter- and intra-molecular bonding and the definition of coordination geometries around the central metal ions, as well as the electronic charge transfer interactions in the Cr(III) and V(IV) complexes. (C) 2020 Elsevier B.V. All rights reserved.
Open Access
Synthesis and biological evaluation of novel coumarin-chalcone derivatives containing urea moiety as potential anticancer agents
(2020-01-01T00:00:00Z) Kurt, BELMA; Kandas, Nur Ozten; DAĞ, AYDAN; Sonmez, Fatih; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA; DAĞ, AYDAN
The increasing interest on new drug discovery is constantly up to date as drugs do not increase survival adequately against increasing cancer cases worldwide. Based on the reported anticancer activity of coumarin, chalcone and urea derivatives, the present investigation dealt with the design and synthesis of coumarin derivatives bearing diversely substituted chalcone-urea moieties 5a-k. Through a structure-based molecular hybridization approach, a series of novel coumarin-chalcone derivatives containing urea moiety was synthesized and screened for their in vitro antiproliferative activities against the cancer cell lines (H4IIE and HepG2). In addition, the synthesized compounds were tested on a cell line that was not cancerous (CHO) and the damage, it could give to normal cells was determined. Among the synthesized compounds, 5k exhibited better inhibition of H4IIE compared to Sorafenib. 5j also showed better inhibition against HepG2 than Sorafenib. In particular, 5k induced H4IIE apoptosis, arrested cell cycle at the S phase. Therefore, 5k and 5j may be potent antitumor agents, representing a promising lead for further optimization. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
Open Access
Fungal biotransformation of carvone and camphor by Aspergillus flavus and investigation of cytotoxic activities of naturally obtained essential oils
(2022-01-01T00:00:00Z) Gazioglu, Isil; Zengin, Ozge Sultan; Gunaydin Akyildiz, AYŞENUR; Zengin Kurt, BELMA; GÜNAYDIN AKYILDIZ, AYŞENUR; ZENGİN KURT, BELMA
In this study, the biotransformation of carvone and camphor by Aspergillus flavus and the products were investigated. The biotransformation reaction of carvone by A. flavus resulted in the production of neodihydrocarveol, dihydrocarvone, 2-cyclohexene-1-one,2-methyl-5-(1-methylethenyl), limonene-1,2-diol, trans-p-mentha-1(7),8-dien-2-ol, p-menth-8(10)-ene-2,9-diol, and the biotransformation reaction of camphor resulted in the production of 2 -campholenic acid, 2-cyclohexene-1-one,2-hydroxy-4,4,6,6-tetramethyl, α-campholene aldehyde. The naturally produced essential oils by biotransformation of carvone and camphor were observed to be cytotoxic to breast cancer cells while no significant inhibition was seen in the healthy cell line. Additionally, biotransformation products had the highest inhibition (74%) against aflatoxin B1. The bioactivities of biotransformation products are promising, and they can be further investigated for their therapeutic potential as active agents.
Open Access
Tail-Approach-Based Design and Synthesis of Coumarin-Monoterpenes as Carbonic Anhydrase Inhibitors and Anticancer Agents
(2023-02-01) Kurt B. Z.; Celebi G.; Öztürk Civelek D.; Angeli A.; Akdemir A.; Sonmez F.; Supuran C. T.; ÖZTÜRK CİVELEK, DİLEK; AKDEMİR, ATİLLA; ZENGİN KURT, BELMA
In this study, sixty novel coumarin-monoterpene compounds were synthesized in two series [thirty-two compounds (12-43) bearing a triazole ring in the first series, and twenty-eight compounds (44-71) bearing an alkyl chain in the second one]. Their inhibitory effects on the human carbonic anhydrase (hCA) isoforms I, II, IX, and XII and anticancer potentials were determined. All synthesized molecules selectively inhibited CA IX and XII. 23 and 42 were found to be the strongest inhibitors, with K i values of 1.9 nM against hCA IX. Also, 70 showed the highest inhibitory activity with a K i value of 4.9 nM against hCA XII. Moreover, their cytotoxic effects on colon adenocarcinoma (HT-29), prostate adenocarcinoma (PC-3), and breast adenocarcinoma (MCF-7) cell lines were evaluated. According to the cytotoxicity results, 14 (IC50 = 2.48 μM) and 63 (IC50 = 3.91 μM) exhibited the highest cytotoxicity on the MCF-7 cells, while 23 showed the strongest cytotoxic effect on both PC-3 (IC50 = 9.40 μM) and HT-29 (IC50 = 12.10 μM) cell lines. 14, 23, and 66 decreased CA IX and CA XII protein expression in HT-29 cells, while 23 and 66 showed the strongest reduction of both CA IX and CA XII in MCF-7 cells. All of the selected compounds increased total apoptosis in a concentration-dependent manner in HT-29 and MCF-7 cells. 14 has the strongest apoptotic effect in MCF-7 cells. 23 increased early apoptosis primarily, while 14 and 66 increased total apoptosis in HT-29. In addition, PI/Hoechst staining proves that apoptotic cells are increased in HT-29 with an effect of 14, 23, and 66. As a result of the modeling studies, it has been shown that only the open coumarin form of the compounds can interact directly with the active-site Zn2+ ion. It has been shown that coumarin-monoterpene structures with different alkyl and monoterpene groups both specifically inhibit CA IX and XII and exhibit specific cytotoxicity in different cell lines.