Sürdürülebilir Kalkınma Amaçları
Yazarlar
- Togar, Basak(3)
- Ağar, Güleray(2)
- Emsen, Bugrahan(2)
- Kızıl, Hamit Emre(2)
- Turkez, Hasan(2)
- Agar, G.(1)
- Anar, M.(1)
- Arslan, Mehmet Enes(1)
- Aslan, Ali(1)
- Aslan, Osman Nuri(1)
- Aydın, Numan(1)
- Bakan, Feray(1)
- Bayram, Sinan(1)
- Bağcı, Yavuz(1)
- Bilginoğlu, Emine(1)
- Cacciatore, Ivana(1)
- Cavusoglu, Seyda(1)
- Ceker, S.(1)
- Demir, Merve(1)
- Demir, Yeliz(1)
- Dertli, Enes(1)
- Ecem Bayram, Nesrin(1)
- Ekincioglu, Yavuz(1)
- Ekincioğlu, Yavuz(1)
- Engin, Tubanur(1)
- Gerçek, Yusuf Can(1)
- Hacimüftüoglu, Ahmet(1)
- Kalay, Erbay(1)
- Karakaş, İbrahim Hakkı(1)
- Karaoğlanoğlu, Serpil(1)
- Kizil, H. E.(1)
- Kizil, Hamit Emre(1)
- Kizil, Hamit Emre(1)
- Mardinoglu, Adil(1)
- Nartop, Dilek(1)
- Ozdemir, Ozlem(1)
- Pezik, Esra(1)
- Stefano, Di Antonio(1)
- Süloğlu, Aysun Kılıç(1)
- Tatar, Abdulgani(1)
Yayınlar
- MakaleAçık Erişim2026Scopus SJRQ2Rhodanine–Sulfonate hybrids targeting aldose reductase: Synthesis, in vitro inhibition, molecular docking, and cytotoxicity studies
Kalay, Erbay; Demir, Yeliz; Türkeş, Cüneyt; Aslan, Osman Nuri; Pezik, Esra; Şahin, Engin
Aldose reductase (ALR2), a key enzyme in the polyol pathway, plays a significant role in the onset and progression of diabetic complications, rendering it a critical pharmacological target. In this study, a novel series of twenty-four sulfonate ester-functionalized rhodanine derivatives (compounds 1–24) were rationally designed, synthesized via Knoevenagel condensation, and comprehensively evaluated for their inhibitory activity against ALR2. Spectroscopic and spectrometric methods confirmed the structural integrity of the synthesized compounds. In vitro enzyme inhibition assays revealed that all compounds acted as competitive inhibitors, with several analogues, particularly compounds 6 and 8, exhibiting stronger ALR2 inhibition (Ki = 0.43 µM and 0.48 µM, respectively) than the reference drug epalrestat (Ki = 0.98 µM). Structure–activity relationship (SAR) analysis highlighted the critical influence of para-substituted electron-donating (e.g., methyl) and electron-withdrawing (e.g., nitro, halogen) groups on binding potency. Molecular docking of the most potent inhibitor (compound 6) demonstrated a stable binding pose supported by key interactions, including hydrogen bonding with His110 and π–π stacking with Phe122. In silico ADME profiling confirmed favorable drug-likeness properties for all derivatives. Cytotoxicity studies on L929, A549, and RG-2 cell lines revealed that most compounds were less toxic than the reference drug at lower concentrations, with compound 8 showing a promising cytotoxic profile. These findings position rhodanine–sulfonate hybrids as promising scaffolds for the development of next-generation ALR2 inhibitors for the treatment of diabetic complications.
AtıfScopus2WoS3
İncele - MakaleYalnız künye2026Scopus SJRQ2Novel heteroaromatic compounds bearing thiosemicarbazone as anti-cancer and anti-bacterial agents: Synthesis, cytotoxic and biological screening, molecular docking and DFT analysis
Nartop, Dilek; Ögütcü, Hatice; Özkan, Elvan Hasanoglu; Yetim, Nurdan Kurnaz; Kizil, Hamit Emre; Ekincioglu, Yavuz
Novel heteroaromatic compounds (Hc1, Hc2, Hc3, Hc4) were obtained, and their structure were confirmed using various spectroscopic methods, including elemental analysis, fourier transform infrared (FT-IR) spectroscopy, proton and carbon nuclear magnetic resonance (1H/13C-NMR) spectroscopy, and molar conductance measurement. The biological activities of the heteroaromatic compounds against several Gram-positive (Micrococcus luteus ATCC9341, Staphylococcus epidermidis ATCC12228, Bacillus cereus RSKK863, Listeria monocytogenes ATCC 19111), and Gram-negative bacterial strains (Pseudomonas aeruginosa ATCC27853, Klebsiella pneumonia ATCC27853, Enterobacter aerogenes ATCC51342, Salmonella typhi H NCTC9018394, Shigella dysenteriae NCTC2966, Proteus vulgaris RSKK96026) were evaluated using the well-diffusion method. In general, the heteroaromatic compounds demonstrated a stronger inhibitory effect against Gram-positive bacteria. Hc1, Hc2 and Hc3 showed the highest inhibitory effect against B. cereus and L. monocytogenes. The compound (Hc4) showed the highest antibacterial activity and antifungal activity against Bacillus cereus and C. albicans, respectively. The cytotoxic activity of the heteroaromatic compounds was assessed against the non-small cell lung cancer cell line (NCI-H460) using the NutriCulture Cell Viability Detection Kit-8 (CVDK-8). Among the synthesized heteroaromatic compounds, Hc3 exhibited significant cytotoxic activity with an IC50 value of 141.3 & micro;g/mL, whereas compounds Hc1, Hc2, and Hc4 did not display significant toxicity at the tested concentrations. The molecular geometry of the heteroaromatic compound (Hc3) was optimized using Gaussian 09 W at the B3LYP/6-311++G (d,p) level of theory. Key structural parameters such as bond lengths, bond angles, and dihedral angles were determined through the same computational framework. Electronic features, including frontier molecular orbitals, global reactivity descriptors, and molecular electrostatic potential surfaces, were analyzed to explore intramolecular charge distribution and predict reactive sites. To evaluate the biological potential of the heteroaromatic compound (Hc3), molecular docking studies were performed. Additionally, drug-likeness assessment based on Lipinski's Rule of Five and ADME profiling revealed favorable pharmacokinetic characteristics. Molecular docking studies revealed that compound Hc3 showed a binding energy of -4.09 kcal/mol against the EGFR target (PDB ID: 1UWH), exhibiting key interactions such as hydrogen bonding and It-interactions with the active site residues. Based on all the results, it can be said that new heteroaromatic compounds have significant potential in the pharmaceutical field.
AtıfScopus1OpenAlex1İncele - MakaleAçık Erişim2025Scopus SJRQ2An Integrated In Vitro and In Silico Investigation of the Bioactive Properties of Wild Glycyrrhiza glabra var. glandulifera
Kızıl, Hamit Emre; Ulcay, Sibel; Ekincioğlu, Yavuz; Öğütçü, Hatice; Ağar, Güleray
This investigation examined methanol extracts obtained from the whole plant (encompassing all organs except roots), flowers, and fruits of wild Glycyrrhiza glabra var. glandulifera, a liquorice cultivar indigenous to the Cappadocia region of Türkiye, constituting the first comprehensive in vitro and in silico analysis of this species within the region. Anatomical identification revealed distinctive structural characteristics, including thick-walled epidermal cells in the stem, organized clusters of collenchyma cells, and well-defined sclerenchyma layers encompassing the vascular bundles. The petiole exhibited a characteristic heart-shaped morphology containing three vascular bundles, while foliar analysis demonstrated the presence of stomata on both adaxial and abaxial surfaces, accompanied by a bifacial mesophyll arrangement. The extracts demonstrated remarkable antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, as well as various fungal species. Furthermore, significant cytotoxic activity was observed against non-small cell lung cancer (H460), with the whole plant extract exhibiting IC50 values of 117.8 µg/mL (24 h) and 105.6 µg/mL (48 h). Flower extracts demonstrated IC50 values of 116.8 µg/mL (24 h) and 112.7 µg/mL (48 h), while fruit extracts displayed superior potency with IC50 values of 104.4 µg/mL (24 h) and 63.09 µg/mL (48 h). Molecular docking analyses, conducted utilizing AutoDock Tools 1.5.6 and BIOVIA Discovery Studio Visualizer 4.5, revealed significant protein-ligand interactions, yielding optimal binding energy and inhibition constant values of -9.57 kcal/mol and 96.92 nM, respectively. The RMSD values were calculated based on structural variations between ligand-protein complexes during re-docking procedures. These findings underscore the substantial biological potential of Glycyrrhiza glabra var. glandulifera from Cappadocia, necessitating further comprehensive investigation.
AtıfScopus6WoS6OpenAlex5İncele - MakaleAçık Erişim2025Scopus SJRQ1Pharmacological Potential and Bioactive Components of Wild Anatolian Sage (Salvia aethiopis L.)
Bilginoğlu, Emine; Kızıl, Hamit Emre; Öğütcü, Hatice; Ağar, Güleray; Bağcı, Yavuz
Salvia aethiopis L., a member of the Lamiaceae family, has gained attention due to its bioactive compounds with potential therapeutic applications. This study investigated the chemical composition and biological activities of S. aethiopis ethanol extract collected from Karaman province, Türkiye. The phenolic profile of the plant was characterized using LC–MS/MS analysis, which revealed substantial amounts of rosmarinic acid, ferulic acid, caffeic acid, and p-coumaric acid. The antimicrobial activity of the extracts was evaluated against various Gram-positive and Gram-negative bacteria, as well as fungal strains, using the agar well diffusion method. The results demonstrated potent antibacterial effects, particularly against Staphylococcus aureus, Micrococcus luteus, and Klebsiella pneumoniae. Furthermore, the cytotoxic potential of S. aethiopis was assessed on H-460 non-small cell lung cancer cells. The extract exhibited a dose-dependent cytotoxic effect, with a significant reduction in cell viability after 24 and 48 h of treatment, yielding IC50 values of 80.08 and 56.19 μg/mL, respectively. These findings suggest that S. aethiopis possesses promising antimicrobial and anticancer properties, which could contribute to the development of novel therapeutic agents.
AtıfScopus8WoS7OpenAlex7İncele - MakaleYayıncıda açık erişim2024Scopus SJRQ1Can Enzymatic Modified Pectin in Mediterranean Fruits Be Therapeutic Against Stomach Cancer?
Üstün, Selime; Kizil, Hamit Emre; Dertli, Enes
The aim of this study was to evaluate the cytotoxic effects of enzymatically modified pectin products derived from grapefruit, jujube, and kumquat on the MKN-45 gastric cancer cell line in vitro. FTIR analysis revealed that the spectra of the pectins produced were comparable to those of commercial pectin and included the characteristic peaks identified in the literature. The galacturonic acid content was measured as 612 mg/g in grapefruit pectin, 544 mg/g in jujube pectin, and 704 mg/g in kumquat pectin. DSC analysis indicated that all pectin samples and their modifications exhibited one endothermic peak and one exothermic peak. Cytotoxicity assessments revealed that the enzymatically modified grapefruit pectin demonstrated significant cytotoxic effects across all tested concentrations, with 0.075 mg/mL being the most effective. For kumquat pectin, all tested concentrations showed cytotoxic properties, with 0.3, 0.15, and 0.075 mg/mL being the most effective. In the case of jujube pectin, cytotoxic effects were observed at all concentrations except for 1.2 mg/mL.
AtıfScopus3WoS3OpenAlex3İncele - MakaleAçık Erişim2024Scopus SJRQ3InvestIgatIon of cytotoxIcIty and antIbacterIal effect of boron-contaInIng nano-hydroxyapatIte
Aydın, Numan; Karaoğlanoğlu, Serpil; Süloğlu, Aysun Kılıç; İdil, Neslihan; Demir, Merve; Karakaş, İbrahim Hakkı
Introduction: Different regenerative materials are used to protect and stimulate pulp tissue. Objectives: This in vitro study aimed to examine the cytotoxicity of different doses of boron-containing nano-hydroxyapatite (B-nHAp) and its antibacterial effect. Material and methods: B-nHAp was synthesized with microwave-assisted chemical precipitation method at different rates, such as 1%, 5%, and 10%. The extracts were prepared in separate tubes: 1%, 5%, 10% B-nHAp, and nHAp 50 mg/ml. Cytotoxicity test was performed on L929 mouse fibroblasts for 24 and 72 hours. Antibacterial analysis was performed with Streptococcus mutans bacteria using micro-dilution method. Cell viability values were evaluated with two-way analysis of variance (ANOVA) test (p < 0.05). Results: B-nHAp was successfully synthesized in XRD and SEM analyses. Nano-hydroxyapatite showed more cell viability than control group at 24 and 72 hours. All B-nHAp extracts demonstrated less cell viability at the end of 24 hrs. than control group. However, 1% B-nHAp cell viability decreased more in the B-nHAp group compared with the control group, while 5% and 10% B-nHAp showed high cell viability after 72 hours of incubation. B-nHAp demonstrated less antibacterial effect on Streptococcus mutans compared with nHAp. Conclusions: According to the results, the addition of boron to nano-hydroxyapatite does not make a significant contribution to increase the regenerative and antibacterial properties of the material.
AtıfScopus4OpenAlex5İncele - MakaleAçık Erişim2022Scopus SJRQ2Synthesis and in Vitro Toxicity Assessment of Different Nano-Calcium Phosphate Nanoparticles
Togar, Basak; Türkez, Hasan; Bakan, Feray; Arslan, Mehmet Enes; Tatar, Abdulgani; Cacciatore, Ivana; Hacimüftüoglu, Ahmet; Çadirci, Kenan; Stefano, Di Antonio; Mardinoglu, Adil
Nanoscale biomaterials are commonly used in a wide range of biomedical applications such as bone graft substitutes, gene delivery systems, and biologically active agents. On the other hand, the cytotoxic potential of these particles hasn't yet been studied comprehensively to understand whether or not they exert any negative impact on the cellular structures. Here, we undertook the synthesis of beta-tricalcium phosphate (beta-TCP) and biphasic tricalcium phosphate (BCP) nanoparticles (NPs) and determine their concentration-dependent toxic effects in human fetal osteoblastic (hFOB 1.19) cell line. Firstly, BCP and beta-TCP were synthesized using a water-based precipitation technique and characterized by X-Ray Diffraction (XRD), Raman Spectroscopy, and Transmission Electron Microscopy (TEM). The cytological effects of beta-TCP and BCP at different concentrations (0-640 ppm) were evaluated by using 3- (4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays. The total oxidative status (TOS) parameter was used for investigating oxidative stress potentials of the NPs. In addition, the study assessed the DNA damage product 8-hydroxy-2'-deoxyguanosine (8-Oxo-dG) level in hFOB 1.19 cell cultures. The results indicated that the beta-TCP (above 320 ppm) and BCP (above 80 ppm) NPs exhibited cytotoxicity effects on high concentrations. It was also observed that the oxidative stress increased relatively as the concentrations of NPs increased, aligning with the cytotoxicity results. However, the NPs concentrations of 160 ppm and above increased the level of 8-OH-dG. Consequently, there is a need for more systematic in vivo and in vitro approaches to the toxic effects of both nanoparticles.
AtıfScopus4WoS1OpenAlex3İncele - MakaleYalnız künye2020Scopus SJRQ2Effects of processing methods and extraction solvents on the chemical content and bioactive properties of propolis
Ecem Bayram, Nesrin; Gerçek, Yusuf Can; Bayram, Sinan; Toğar, Başak
The aim of this study was to evaluate the bioactive properties of propolis extract prepared using different solvents and different extraction methods. The extracts were analyzed by gas chromatography–mass spectrometry (GC–MS) and the differences between their antibacterial activities were evaluated by disc diffusion method. At the same time, bioactive properties of different concentrations of propolis extracts were investigated on human umbilical vein endothelial cells (HUVEC). The proliferative effects and cytotoxic effects of the extracts were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) analyzes, respectively. Total antioxidant capacity (TAC) and total oxidative status (TOS) parameters were used in assessing biochemical effects in the HUVEC cell line. The DNA damage was also analyzed by 8-oxo-2-deoxyguanosine (8-OHdG) level as indicators of genotoxicity. As a result of the MTT analysis conducted within the scope of the present study, the extracts tested were sorted as 95% ethanol extract of propolis (PEE95) > ultrasonic ethanol extract of propolis (PUEE) > 50% ethanol extract of propolis (PEE50) > ultrasonic water extract of propolis (PUWE) in terms of the effectiveness of their cell viabilities. It was observed that high concentrations of PEE95 induced LDH release. In addition to this, our findings have shown that PEE50, PUEE and PUWE increased oxidative stress at high concentrations. According to 8-OH-dG analysis, all tested extracts were found to be non-genotoxic. The results obtained from antibacterial activity and minimum inhibition concentration tests showed that PUEE and PEE95 had stronger antibacterial effects than PEE50 and PUWE. All these results indicated that propolis has beneficial effects for human health and therefore it is a valuable product which can be used as a food supplement.
AtıfScopus23WoS22OpenAlex25İncele - MakaleAçık Erişim2019Scopus SJRQ1Inhibition of growth of U87MG human glioblastoma cells by Usnea longissima Ach.
Emsen, Bugrahan; Ozdemir, Ozlem; Engin, Tubanur; Togar, Basak; Cavusoglu, Seyda; Turkez, Hasan
Herbal medicines are efficient to reduce side effects in the fight against glioblastoma, which plays a critical role within brain cancer species. The recent studies designated for testing the effects of lichens that have shown numerous anticancer activities on glioblastoma so far. In the present study, different concentrations of water extract obtained from Usnea longissima Ach. were used in order to determine cytotoxic (via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and lactate dehydrogenase tests), antioxidant (via total antioxidant capacity test), pro-oxidant (via total oxidant status test) and genotoxic (via 8-hydroxy-2'-deoxyguanosine test) effects of them on human U87MG-glioblastoma cancer cell lines. Primary mixed glial-neuronal non-cancerous cells from Sprague-Dawley rats were also utilized to measure the effects of treatments on non-cancerous cells. Based on median inhibitory concentration values, the data belonged to non-cancerous cells (2486.71 mg/L) showed distinct towering compared to U87MG (80.93 mg/L) cells. The viability of non-cancerous and U87MG cells exposed to extract is decreased in a dose dependent manner. It was also showed that low concentrations of extract notably increased total antioxidant capacity on non-cancerous cells. In addition, various phenolic compounds in extract were detected through high-perfonnance liquid chromatography. The recent results encourage that extract will be able to have therapeutic potential against glioblastoma.
AtıfScopus23WoS20OpenAlex21İncele - MakaleAçık Erişim2018Scopus SJRQ3Effects of two lichen acids isolated from Pseudevernia furfuracea (L.) Zopf in cultured human lymphocytes
Emsen, Bugrahan; Togar, Basak; Turkez, Hasan; Aslan, Ali
The present study aims at assessing the efficacies of olivetoric acid (OA) and physodic acid (PA) isolated from Pseudevernia furfuracea (L.) Zopf (Parmeliaceae) in human lymphocytes (HLs) in vitro. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and lactate dehydrogenase assays were performed to establish cytotoxicity in HLs. Besides, oxidative stress and genotoxicity were monitored by estimating the changes of total oxidative stress (TOS) and 8-hydroxy-2'-deoxyguanosine (8-OH-dG) levels, respectively, in HLs. At the same time, OA- and PA-induced total antioxidant capacity (TAC) levels in HLs were determined. Although especially low concentrations of OA (IC50 = 109.94 mg/L) and PA (IC50 = 665.49 mg/L) did not show cytotoxic effect at high levels in HLs, it was revealed that cytotoxicity was significantly (p < 0.05) associated with oxidative stress and genotoxicity via correlation analysis. While TOS level in HLs did not statistically (p > 0.05) increase in the presence of all treatments (0.5-100 mg/L) of PA, TAC level was increased by PA applications in certain concentrations (0.5-10 mg/L). Overall, the obtained data indicate that OA and especially PA as lichen compounds that do not cause oxidative stress can be a new resource of therapeutics as recognized in the present study with their high antioxidant features.
AtıfWoS20OpenAlex24İncele - BildiriYayıncıda açık erişim2016Scopus SJRQ1Determination of antigenotoxic, proliferative and cytotoxic properties of ellagic acid
Ceker, S.; Agar, G.; Anar, M.; Kizil, H. E.