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Öğe 4-Vinylbenzyl and 2-morpholinoethyl substituted ruthenium (II) complexes: Design, synthesis, and biological evaluation(Elsevier, 2020) Sari, Yakup; Gurses, Canbolat; Celepci, Duygu Barut; Kelestemur, Unzile; Aktas, Aydin; Yuksel, Sengul; Ates, BurhanRecently, the medical applications of organoruthenium complexes have attention attracted to organometallic chemists and biochemists. In this study, 4-vinylbenzyl and 2-morpholinoethyl substituted (NHC) Ru(II)(eta(6)-p-cymene) complexes were synthesized and in vitro DNA binding, cell cytotoxicity (anticancer activity) and genotoxicity properties were determined in order to understand the biological activities. These complexes have been prepared from the 4-vinylbenzyl and 2-morpholinoethyl substituted Ag(I) NHC complexes via transmetallation method. The characterization of the new (NHC)Ru(II)(eta(6)-p-cymene) complexes was performed by using H-1 NMR, C-13 NMR, FTIR spectroscopy and elemental analysis techniques. Also, molecular structure of complex 1b was obtained with single-crystal X-ray diffraction method. IC50 value of 1b against MCF-7 cell line was determined as 3.61 mu M and for 1b, an oxidation effect was observed in the concentrations higher than 50 mu g/mL. Comet assay unlike sister chromatid exchange (SCE) analysis data showed correlated results with cytotoxicity as well as DNA binding properties of the complexes. (C) 2019 Elsevier B.V. All rights reserved.Öğe Aliphatic Polyurethane Films Based on Hexamethylene Diisocyanate and Saccharides for Biocompatible Transparent Coating on Optic Medical Devices(Wiley-V C H Verlag Gmbh, 2022) Gurses, Canbolat; Karaaslan-Tunc, Merve Goksin; Kelestemur, Unzile; Balcioglu, Sevgi; Gulgen, Selam; Koytepe, Suleyman; Ates, BurhanPolyurethanes are widely used in daily life, from the textile industry to medical applications. In this study, a biocompatible and transparent coating from polyethylene glycol-based polyurethanes including different type of saccharide (xylose as monosaccharide, sucrose as disaccharide, or starch as polysaccharide) is prepared. Prepared optically transparent polyurethanes are characterized with different instrumental analysis techniques and contact-angle measurements. Thermogravimetric analysis data allow understanding that the synthesized saccharide based polyurethanes are resistant to high temperatures, which means that medical devices can be easily coated with one of the saccharide-based polymers during the manufacturing process. The study results also show that synthesized polyurethane samples having a different kind of saccharides present high biocompatibility and transparency properties via In vitro cytotoxicity analysis and optic transparency tests. For xylose, sucrose, or starch containing polyurethanes, the tranmittance values are 97.72%, 85.20%, and 89.23%, respectively. In addition, scanning electron microscope images show that the samples also have smooth surfaces which can be used for proper coating of medical devices. Consequently, this manuscript addresses synthesis and characterization of the optically transparent polyurethanes based on specific saccharides for biocompatible and transparent surfaces especially in optic medical devices such as colonoscopy applications and laparoscopic detection probes.Öğe Benzotriazole functionalized N-heterocyclic carbene-silver(I) complexes: Synthesis, cytotoxicity, antimicrobial, DNA binding, and molecular docking studies(Pergamon-Elsevier Science Ltd, 2018) Onar, Gulnihan; Karatas, Mert Olgun; Balcioglu, Sevgi; Tok, Tugba Taskin; Gurses, Canbolat; Kilic-Cikla, Isin; Ozdemir, NamikIn this study, six [Ag(NHC)(2)](+)[AgCl2](-) type silver complexes were synthesized by the reaction of corresponding carbene precursor and Ag2O. One [Ag(NHC)(2)]+NO3- type complex was synthesized by the anion exchange reaction of corresponding silver-NHC and NaNO3. The synthesized complexes were characterized by H-1 NMR, C-13 NMR and IR spectroscopic methods, and elemental analysis. X-ray crystal structure of 5a was also reported. Cytotoxicities of all compounds were evaluated against human breast (MCF-7) and colorectal (Caco-2) cancer cell lines and non-cancer mouse fibroblast (L-929) cell lines. All complexes performed stronger activity against both cancer cell lines than standard compound cisplatin while complex 3b performed nearly equal cytotoxicity to cisplatin against non-cancer L-929. Antimicrobial effects of all compounds were evaluated against Escherichia coli, Bacillus subtilis and Candida albicans and good activities were observed. The docking results indicated that complex 3b might be classified as druggable molecule in drug design. DNA binding study also demonstrates that 3b complex has an interaction ability to DNA. Combination of experimental and molecular docking results revealed that reported complexes are promising structures and deserve further research as anticancer drugs. (C) 2018 Elsevier Ltd. All rights reserved.Öğe Biomedical applications of hybrid polymer composite materials(Woodhead Publ Ltd, 2017) Ates, Burhan; Koytepe, Suleyman; Balcioglu, Sevgi; Ulu, Ahmet; Gurses, Canbolat[Abstract Not Available]Öğe Chemistry, structure, and biological roles of Au-NHC complexes as TrxR inhibitors(Academic Press Inc Elsevier Science, 2020) Karaaslan, Merve Goksin; Aktas, Aydin; Gurses, Canbolat; Gok, Yetkin; Ates, BurhanIn recent years, the preparation of metal complexes and the introduction of biologically active organometalic compounds are new strategies in drug development. For this purpose, generally N-heterocyclic pharmaceutical agents have been used as promising nuclei. Au-containing N-heterocyclic carbene (Au-NHC) derivatives are among the compounds used for this purpose, and their enzyme inhibition, antioxidant activity, antimicrobial and anticancer properties are widely studied. In these studies, the anticancer property of Au-NHC complexes is the most widely studied area. The common result in different studies has been revealed that mitochondrial thioredoxin reductases (TrxR) inhibition is the main pathway in the powerful anticancer effect of many Au-NHC complexes. In TrxR inhibition, the high affinity of gold to sulfur is considered to be the main component of the effect. This review includes the discussions releated to the anticancer activities and TrxR inhibition properties of Au-NHC compounds.Öğe Chemistry, Structures, and Advanced Applications of Nanocomposites from Biorenewable Resources(Amer Chemical Soc, 2020) Ates, Burhan; Koytepe, Suleyman; Ulu, Ahmet; Gurses, Canbolat; Thakur, Vijay KumarResearchers have recently focused on the advancement of new materials from biorenewable and sustainable sources because of great concerns about the environment, waste accumulation and destruction, and the inevitable depletion of fossil resources. Biorenewable materials have been extensively used as a matrix or reinforcement in many applications. In the development of innovative methods and materials, composites offer important advantages because of their excellent properties such as ease of fabrication, higher mechanical properties, high thermal stability, and many more. Especially, nanocomposites (obtained by using biorenewable sources) have significant advantages when compared to conventional composites. Nanocomposites have been utilized in many applications including food, biomedical, electroanalysis, energy storage, wastewater treatment, automotive, etc. This comprehensive review provides chemistry, structures, advanced applications, and recent developments about nanocomposites obtained from biorenewable sources.Öğe Chitosan/Polyvinylpyrrolidone/MCM-41 Composite Hydrogel Films: Structural, Thermal, Surface, and Antibacterial Properties(Wiley-V C H Verlag Gmbh, 2018) Ulu, Ahmet; Noma, Samir A. A.; Gurses, Canbolat; Koytepe, Suleyman; Ates, BurhanThe aim of this study is to characterize and investigate the effects of the Mobil Composition of Matter No. 41 (MCM-41) concentrations (0.5, 1, 3, 5, and 10 wt%) on structural, thermal, wettability, water content, oxygen (O-2) permeability, and swelling properties as well as morphological characteristics of chitosan/polyvinylpyrrolidone/MCM-41 (CH/PVP/MCM-41) composite hydrogel films. In addition, hydrolytic degradability, optic transmittance, and antibacterial properties of composite hydrogels films are determined as in vitro. With increasing of MCM-41 content, the composite hydrogels showed higher thermal stability, as expected. The morphologic properties of the composite hydrogel films are studied using scanning electron microscope (SEM) technique that provide evidence for good miscibility of CH, PVP, and MCM-41. The swelling and water-absorbing properties of the composite hydrogel films are significantly improved because of enhanced hydrophilic profile. Furthermore, the antimicrobial properties of the prepared composite hydrogel films are studied against Bacillus subtilis, Escherichia coli, and Candida albicans yeast. The results showed excellent antibacterial behavior of the composite hydrogel films. The study clearly demonstrates that the prepared CH/PVP/MCM-41 composite hydrogel films may be used as a promising candidate material in various fields such as drug delivery, wound healing material, and adsorbent materials.Öğe The Cytotoxicity, DNA Fragmentation, and Decreasing Velocity Induced By Chromium(III) Oxide on Rainbow Trout Spermatozoa(Springernature, 2023) Ozgur, Mustafa Erkan; Ulu, Ahmet; Gurses, Canbolat; Ozcan, Imren; Noma, Samir Abbas Ali; Koytepe, Suleyman; Ates, BurhanThe present study aimed to determine the cytotoxicity of chromium(III) oxide micro particles (Cr2O3-Ps) in rainbow trout (Oncorhynchus mykiss) spermatozoa. Firstly, Cr2O3-Ps were synthesized and structurally characterized the surface, morphological for particle size and thermal properties. In addition, its structural and elemental purity was determined using energy-dispersive X-ray (EDX) spectrum and elemental maps. Structural purity, thermal properties, and stability of Cr2O3 -Ps were also examined in detail by performing thermal analysis techniques. The cytotoxicity of Cr2O3-Ps was measured by the observation of velocities, antioxidant activities, and DNA damages in rainbow trout spermatozoa after exposure during 3 h in vitro incubation. The straight line velocity (VSL), the curvilinear velocity (VCL), and the angular path velocity (VAP) of spermatozoa decreased after exposure to Cr2O3-Ps. While the superoxide dismutase (SOD) and the catalase (CAT) decreased, the lipid peroxidation increased in a dose-dependent manner. However, the total glutathione (tGSH) was not affected in this period. DNA damages were also determined in spermatozoa using Comet assay. According to DNA in tail (%) data, DNA damages have been detected with gradually increasing concentrations of Cr2O3-Ps. Furthermore, all of class types which are categorized as the intensity of DNA fragmentation has been observed between 50 and 500 mu g/L concentrations of Cr2O3-Ps exposed to rainbow trout spermatozoa. At the end of this study, we determined that the effective concentrations (EC50) were 76.67 mu g/L for VSL and 87.77 mu g/L for VCL. Finally, these results about Cr2O3-Ps may say to be major risk concentrations over 70 mu g/L for fish reproduction in aquatic environments.Öğe Effects of strontium - erbium co-doping on the structural properties of hydroxyapatite: An Experimental and theoretical study(Elsevier Sci Ltd, 2020) Mahmood, Bahroz Kareem; Kaygili, Omer; Bulut, Niyazi; Dorozhkin, Sergey, V; Ates, Tankut; Koytepe, Suleyman; Gurses, CanbolatFive different samples of Sr-based Er-doped hydroxyapatites (HAps) in the dissimilar quantities like 0, 0.35, 0.70, 1.05 and 1.40 at% were produced via a wet chemical process. The prepared samples were investigated experimentally by powder X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive X-ray (EDX), Fourier transform infrared (FTIR) spectroscopy, differential thermal analysis (DTA), and in vitro biocompatibility tests. In addition, the density of states (DOS) and band structures were investigated theoretically. It was found that the presence of Er as a dopant affected the lattice parameters, while the EDX measurements confirmed that the presence of Er at various concentrations caused a Ca-deficiency because the addition of Er decreased the Calcium/Phosphorus molar ratio from 1.67 to 1.61. For all samples, the single-phase distribution of HAp was observed. The crystallinity percentage of the samples was found to be 89% or more according to two different methods. The calculations with respect to Scherrer and Williamson-Hall methods showed that the crystallite sizes of the samples were found to be in the ranges of 29-34 nm and 25-42 nm, respectively. DTA investigations revealed that all samples exhibited thermal stability in the temperature range of 25 degrees C - 1000 degrees C. No remarkable morphological alterations were observed. Furthermore, the theoretical studies confirmed that the band structures narrowed with an increase in Er concentration.Öğe Fabrication and characterization of high molecular mass tmpe-based polyurethane wound dressing materials containing allantoin and gentamicin by electrospinning(Eurasia Acad Publ Group (Eapg), 2023) Cakmen, Ayse Basak; Noma, Samir Abbas Ali; Gurses, Canbolat; Koytepea, Suleyman; Ates, Burhan; Yilmaz, IsmetIn this study, biocompatible, antibacterial and high mechanical strength polyurethane-based wound dressing materials were prepared by using the electrospinning technique. In addition, allantoin and gentamicin which will contribute to wound healing, were incorporated into these fiber materials. Polyurethane structures containing trimethylolpropane ethoxylate (TMPE) with 2 different molecular weights were synthesized. TMPE-based polyurethanes/polycaprolactone (1:3) blends were also prepared by adding 1% gentamicin and 10% allantoin and they were knitted by the electrospinning method and turned into a wound dressing material. After this stage, chemical structure, morphological, thermal and mechanical properties, flexibility, antibacterial effect, in vitro biocompatibility, cell adhesion tests, allantoin release level, and biodegradability of the prepared wound dressing materials were performed. The prepared fiber materials exhibited antibacterial properties and 80% cell viability, approximately. In addition, the obtained wound dressing materials showed high mechanical strength and ideal gas permeability. For this reason, it offers an ideal alternative for closing wounds.Öğe Fabrication, thermal and in vitro behaviors of ciprofloxacin loaded ?-cyclodextrin-PEG based polyurethanes as potential biomaterial for wound dressing applications(Taylor & Francis Inc, 2022) Kantarcioglu, Melike; Tunc, Merve Goksin Karaaslan; Gurses, Canbolat; Ates, Burhan; Koytepe, SuleymanAntibacterial polyurethanes as wound-dressing material with high biocompatibility and thermal stability were developed from polyethylene glycol-200 (PEG200), 4,4'-methylenebis(cyclohexyl isocyanate) (HMDI) and beta-cyclodextrin (beta CD). beta CD was preferred in this material because of providing biocompatibility and supporting the absorption/desorption characteristics of ciprofloxacin due to its hydrophobic gap. The beta-cyclodextrin-PEG based polyurethane structures (PU-200-beta CDs) was synthesized with different beta-cyclodextrin:PEG:HMDI ratios. PU-200-beta CDs were characterized by FTIR spectroscopy, thermal analysis, SEM, and water contact angle techniques. The biocompatibility property of polyurethane materials was determined according to the indirect cytotoxicity assay results and the PU-200-beta CDs exhibited cell viability ranging from, 83.04 +/- 7.28% to 99.73 +/- 10.3% against L-929 cells. The hydrolytic degradability test was applied to the highest biocompatible PU-200-beta CD3 structure. The mass loss of PU-200-beta CD3 was determined 4.75 +/- 0.86% at the end of the 28-day. Antibacterial properties of ciprofloxacin doped PU-200-beta CD3 were investigated using Escherichia coli and Bacillus subtilis. The ideal polyurethane structure was selected according to its biocompatibility and antibacterial properties. This polyurethane structure was converted into wound dressing material via electrospinning technique. The obtained dressing material showed mechanical stable fiber structure. Therefore, prepared beta-cyclodextrin-PEG-based polyurethane structure can be suitable for the production of wound-dressing material due to its good ciprofloxacin release properties, high stability and biocompatibility.Öğe Near-infrared inducible supports in bio-catalysts design: A useful and versatile tool in enhancement of enzyme activity(Elsevier, 2024) Noma, Samir Abbas Ali; Dik, Gamze; Gurses, Canbolat; Kurucay, Ali; Topel, Seda Demirel; Ulu, Ahmet; Asiltuerk, MeltemImmobilized enzymes have encountered two main challenges: Reduced enzyme activity compared to free enzymes and exhausted immobilized enzymes due to reusability. Herein, we suggested a promising activity enhancement strategy to overcome these challenges. The emission from upconversion nanoparticles (UCNPs) under near-infrared (NIR) excitation can increase the activity of PEG-L-ASNase due to Forster Resonance Energy Transfer. For this purpose, UCNPs were initially synthesized using the hydrothermal method. Subsequently, these UCNPs were functionalized with a polycationic polymer, branched polyethyleneimine (PEI), and the immobilization of PEG-L-ASNase was achieved through adsorption. We preliminarily explored the parameters such as enzyme concentration, incubation time, pH, temperature, reusability, storage stability, and kinetic study, etc. Further, the in vitro biocompatibility, hemolytic behavior, and anticancer activity of the produced UCNPs were also analyzed as crucial parameters. The results showed the pH durance, thermal and storage stability of the immobilized PEG-L-ASNases were enhanced. The immobilized PEG-L-ASNases maintained their activity to >= 55 % after 20 cycles. Enzyme immobilization led to a decrease in Km and Vmax compared to PEG-L-ASNase. In vitro assays revealed that immobilized enzyme further reduced the proliferation of human leukemia cell line (HL-60) upon NIR irradiation exposure but did not cause toxicity. This research may provide a new strategy to promote the catalytic activity of L-ASNase and demonstrates its potential application on human leukemia cells. Finally, these outcomes are valuable for the use of NIR induction in enzymatic reactions.Öğe New morpholine-liganded palladium(II) N-heterocyclic carbene complexes: Synthesis, characterization, crystal structure, and DNA-binding studies(Wiley-V C H Verlag Gmbh, 2019) Turker, Ferhat; Gurses, Canbolat; Celepci, Duygu Barut; Aktas, Aydin; Ates, Burhan; Gok, YetkinA series of the morpholine-liganded palladium(II) complexes (1a-e) bearing N-heterocyclic carbene (NHC) functionalized by benzonitrile were synthesized. These complexes were synthesized from (NHC)Pd(II)(pyridine) complexes (PEPPSI) and morpholine. The new complexes were fully characterized by using H-1 NMR, C-13 NMR, Fourier-transform infrared spectroscopy, and elemental analysis techniques. Single-crystal X-ray diffraction was used to determine the structure of a derivative. The DNA-binding studies of the new (NHC)Pd(II)morpholine complexes were examined using the pBR322 plasmid. The 2,4,6-trimethylbenzyl derivative compound has the most DNA binding activity. In addition, for the 3-methylbenzyl derivative compound, oxidation effects were observed at concentrations higher than 100 mu g/ml. Also, the molecular and crystal structures of the complex 3-methylbenzyl derivative compound were recorded by using a single-crystal X-ray diffraction method.Öğe Palladium(II) and ruthenium(II) complexes of benzotriazole functionalized N-heterocyclic carbenes: Cytotoxicity, antimicrobial, and DNA interaction studies(Elsevier Science Sa, 2019) Onar, Gulnihan; Gurses, Canbolat; Karatas, Mert Olgun; Balcioglu, Sevgi; Akbay, Nuriye; Ozdemir, Namik; Ates, BurhanIn the present study, four palladium and four ruthenium complexes were synthesized with benzotriazole substituted N-heterocyclic carbene ligands. The structures of complexes were established by appropriate spectroscopic methods and elemental analyses. In addition, the crystal structure of a Pd-NHC complex (1c) was reported. Anticancer, antimicrobial and DNA interaction properties of the complexes were examined. Antimicrobial effects of the complexes were tested against two bacteria strains and one fungi strain. Cytotoxic effects of the complexes were tested against human breast (MCF-7) and colorectal (Caco-2) cancer cell lines and non-cancer mouse fibroblast (L-929) cell lines. Ruthenium complexes were found as more cytotoxic than palladium complexes against cancer cell lines. Especially, benzyl containing, benzimidazole-based ruthenium complexes (3c and 3d) were found as non-cytotoxic against non-cancer L-929 cell lines while performing comparable cytotoxicity against Caco-2 cancer cell lines with cisplatin. In addition, DNA interaction studies were performed with pBR322 plasmid DNA and ctDNA and results showed that both palladium and ruthenium complexes have weaker ability to interact with DNA than cisplatin. The results from this study showed that although the cytotoxic properties of the complexes are not stronger than cisplatin, selectivity of benzyl containing benzimidazole-based ruthenium-NHC complexes against Caco-2 cell lines provides them an advantage, and they deserve further research in the treatment of human colorectal cancer. (c) 2019 Elsevier B.V. All rights reserved.Öğe Photocrosslinkable gelatin/collagen based bioinspired polyurethane-acrylate bone adhesives with biocompatibility and biodegradability(Elsevier, 2021) Balcioglu, Sevgi; Gurses, Canbolat; Ozcan, Imren; Yildiz, Azibe; Koytepe, Suleyman; Parlakpinar, Hakan; Vardi, NigarHard or soft tissue adhesives have been presented as a promising candidate to replace traditional wound closure methods. However, there are mechanical strength problems in biological adhesives and biocompatibility problems in synthetic-based adhesives. At this point, we aimed to remove all these disadvantages and produce a single adhesive that contains all the necessary features and acrylate functionalized UV-curable polyurethane formulations were produced with high crosslink density, high adhesion strength, biocompatibility and injectable property for easy application as potential biomedical adhesives. Aliphatic isophorone diisocyanate (IPDI) was used as the isocyanate source and beta-cyclodextrin was used for host-guest relationship with gentamicin by crosslinking. Proteins (gelatin (GEL), collagen (COL)) and PEGs of various molecular weight ranges (P200, P400, P600) were selected as the polyol backbone for polyurethane synthesis due to their multiple biological activities such as biocompatibility, biodegradability, biomimetic property. Several techniques have been used to characterize the structural, thermal, morphological, and various other physicochemical properties of the adhesive formulations. Besides, the possibility of its use as a hard tissue adhesive was investigated by evaluating the tissue adhesion strength in vitro and ex vivo via a universal testing analyzer in tensile mode. Corresponding adhesive formulations were evaluated by in vitro and in vivo techniques for biocompatibility. The best adhesion strength results were obtained as 3821.0 +/- 214.9, and 3722.2 +/- 486.8 kPa, for IPDI-COL-P200 and IPDI-GEL-P200, respectively. Good antibacterial activity capability toward Escherichia coli Pseudomonas aeruginosa, and Staphylococcus aureus were confirmed using disc diffusion method. Moreover, cell viability assay demonstrated that the formulations have no significant cytotoxicity on the L929 fibroblast cells. Most importantly, we finally performed the in vivo biodegradability and in vivo biocompatibility evaluations of the adhesive formulations on rat model. Considering their excellent cell/tissue viability, fast curable, strong adhesion, high antibacterial character, and injectability, these adhesive formulations have significant potential for tissue engineering applications.Öğe Protonated water-soluble N-heterocyclic carbene ruthenium(II) complexes: Synthesis, cytotoxic and DNA binding properties and molecular docking study(Elsevier Science Sa, 2018) Akkoc, Mitat; Balcioglu, Sevgi; Gurses, Canbolat; Tok, Tugba Taskin; Ates, Burhan; Yasar, SedatNew benzimidazolium salts 1a-d having methylpyridine group on the side chain, have been synthesized and reacted with Ag2O to produce Ag(I)-N-heterocyclic carbene (NHC) complexes 2a-d. Ag(I)-N-heterocyclic carbene (NHC) complexes were used as a carben transfer agents to synthesize water-soluble ruthenium(II)-NHC complexes 4a-d. All synthesized compounds were fully characterized by H-1 and C-13 NMR and HRMS spectroscopic techniques. Anticancer potential and IC50 values of ruthenium(II)-NHC complexes were evaluated by MTT assay against human colorectal cancer (Caco-2) and breast cancer (MCF-7) cell lines. The IC50 value of water-soluble ruthenium(II)-NHC complex 4d demonstrated remarkable cytotoxic activity against Caco-2 (18.0 +/- 1) and MCF-7 (23.8 +/- 0.5) cell lines. Also, 4d has better DNA binding capacity than 4a-c. DS 2017 R2 was used to exert molecular docking for understanding interactions between the water-soluble ruthenium(II)-NHC complexes and DNA. These complexes have been highlighted as a new type of drug. (C) 2018 Elsevier B.V. All rights reserved.Öğe Synthesis and biological evaluation of Au-NHC complexes(Wiley, 2022) Ekinci, Orhan; Akkoc, Mitat; Khan, Siraj; Yasar, Sedat; Gurses, Canbolat; Noma, Samir; Balcioglu, SevgiNew seven Au-N-heterocyclic carbene (NHC) complexes have been synthesized via transmetalation from Ag-NHC complexes. NHC salts, Ag-NHC, and Au-NHC complexes were fully characterized by widely used spectroscopic techniques. The molecular and crystal structures of 3b and 3f Au-NHC complexes were clarified through the single-crystal X-ray diffraction method. According to X-ray diffraction analysis results, the coordination geometry around Au(I) atoms in the complexes are revealed to be almost linear with C-Au-Cl angle. Anticancer activity, DNA binding, xanthine oxidase (XO) inhibitory activity studies, and molecular docking studies were evaluated for all Au-NHC complexes to explore the binding mechanism at the active site. The IC50 value of Au-NHC complexes against human colorectal cancer (Caco-2) and breast cancer (MCF-7) cell lines was defined by MTT assay. The IC50 values for MCF-7 in the range of 5.2 +/- 2 to 152.4 +/- 1 mu M and Caco-2 5.2 +/- 1 to 152.7 +/- 2 mu M showed that 3a, 3b, 3c, 3d, and 3g have better anticancer activity than Cisplatin incredibly complex 3a against both cancer cell line. All Au-NHC complexes showed excellent antimicrobial activity against different bacteria and fungi. 3a was the complex that exhibited the best antimicrobial activity here as well. The XO inhibitory activity experimental results indicated that all gold complexes showed remarkable inhibition activity against XO compared to the generally used standard, allopurinol. The range of IC50 value was determined from 0.407 to 2.681 mu M. 3d complex showed the lowest IC50 value at 0.407 mu M. DNA binding experiments were performed using agarose gel electrophoresis to observe the ability of synthesized Au-NHC complexes to interact with the supercoiled pUC19 plasmid DNA. Molecular docking studies were performed to determine the binding mode of all active compounds against the XO enzyme, antibacterial, antifungal, and MCF-7 cell lines.Öğe Synthesis, characterization, DNA binding and anticancer activities of the imidazolidine-functionalized (NHC)Ru(II) complexes(Elsevier, 2022) Gurses, Canbolat; Aktas, Aydin; Balcioglu, Sevgi; Fadhilah, Araniy; Gok, Yetkin; Ates, BurhanHere, we present a study on the synthesis and biological properties of the ruthenium complexes having naphthyl substituted NHC ligands, which are of great importance for drug development studies. For this purpose, in our study, imidazolidine-functionalized Ru(II)NHC complexes containing naphthyl substitute group were synthesized and in vitro anticancer activity as well as DNA binding properties using agarose gel electrophoresis and ethidium bromide fluorescence quenching assay methods were determined in order to understand the biological activities. The Ru(II)NHC complexes were prepared from naphthyl-substituted Ag(I)NHC complexes and [RuCl2(p-cymene)](2) via the transmetallation method. These new complexes were characterized by using H-1 NMR, C-13 NMR, FTIR spectroscopic method and elemental analysis techniques. Consequently, complex 1d showed the highest anticancer activity in terms of IC30 and IC50 values against HepG2 cell line as 23.9 and 32.84 mu M, respectively. Moreover, depending on the data obtained from agarose gel electrophoresis and fluorescence spectrophotometry techniques, 1b had the highest DNA binding property, which means that 1b behaved binding DNA in the cell as an intercalative manner rather than disrupting the integrity of cell membrane like 1d (C) 2021 Elsevier B.V. All rights reserved.Öğe Water Soluble Coumarin Quaternary Ammonium Chlorides: Synthesis and Biological Evaluation(Wiley-V C H Verlag Gmbh, 2020) Karatas, Mert O.; Noma, Samir A. A.; Gurses, Canbolat; Balcioglu, Sevgi; Ates, Burhan; Alici, Bulent; Cakir, UmitIn the present study, coumarin-bearing three pyridinium and three tetra-alkyl ammonium salts were synthesized. The compounds were fully characterized by(1)H- and(13)C-NMR, LC/MS and IR spectroscopic methods and elemental analyses. The cytotoxic properties of all compounds were tested against human liver cancer (HepG2), human colorectal cancer (Caco-2) and non-cancer mouse fibroblast (L-929) cell lines. Some compounds performed comparable cytotoxicity with standard drug cisplatin. Antibacterial properties of the compounds were tested against Gram-negativeEscherichia coliand Gram-positiveBacillus subtilisbacteria, but the compounds did not have any antibacterial effect against both bacteria. Enzyme inhibitory properties of all compounds were tested on the activities of human carbonic anhydrase I and II, and xanthine oxidase. All compounds inhibited both enzymes more effectively than standard drugs, acetazolamide and allopurinol, respectively. The biological evaluation results showed that ionic and water soluble coumarin derivatives are promising structures for further investigations especially on enzyme inhibition field.
