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Öğe A Comparative Study of Three Brassicaceae Vegetables Grown in Canakkale: Determination of Total Phenolic Content and Antioxidant Activity of Pulp and Juice Samples of Radish (Raphanus sativus L.), Cabbage (Brassica oleracea L. var capitata L) and Cauliflower (Brassica oleracea L.)(2020) Önder, Ferah Cömert; Doğrular, Nuriye; Gündüzalp, Ecem; Barlak, Sedef; Ay, MehmetBrassicaceae that contains well known species from genus Brassica is an important family for crucifers, cabbage etc. The main goal of this study was to investigate the total phenolic contents and antioxidant activities of 25% aqueous ethanol and methanol extracts of selected vegetable pulps such as radish, cabbage, and cauliflower. These analyses were also applied to the freshly prepared juices. For this purpose, studied vegetables which were grown in villages of Canakkale were obtained from district bazaar in Canakkale. Antioxidant activities of selected vegetables have been determined by using DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) free radical, ABTS ((2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging assay and CUPRAC (cupric reducing antioxidant capacity) method. Total phenolic content was determined by using Folin-Ciocalteu reagent. The results show that total phenolic contents in pulp extracts of 25% aqueous ethanol of red cabbage (1071 ± 25.12 mg FAE/100 g) and brussels sprout (594.00 ± 13.93 mg FAE/100 g) have higher than the other used vegetables. The 25% aqueous ethanol extracts of white and red radish pulps showed the greatest IC50 value with DPPH assay (50.00 µg/mL). The higher phenolic content in the ethanol and methanol extracts of red cabbage may contribute to its increasing CUPRAC activity (4.73 ± 0.11 and 4.78 ± 0.11 quercetin equivalent of flavonoid concentration). In addition, black radish juice showed the highest inhibition value with ABTS assay (70.83 ± 1.83%). This study which may be important for food and health applications, also emphasizes the importance of the cultivation area and the valuable parts of vegetables.Öğe A drug repurposing study identifies novel FOXM1 inhibitors with in vitro activity against breast cancer cells(Humana Press Inc, 2024) Abusharkh, Khaled A. N.; Onder, Ferah Comert; Cinar, Venhar; Hamurcu, Zuhal; Ozpolat, Bulent; Ay, MehmetFOXM1, a proto-oncogenic transcription factor, plays a critical role in cancer development and treatment resistance in cancers, particularly in breast cancer. Thus, this study aimed to identify potential FOXM1 inhibitors through computational screening of drug databases, followed by in vitro validation of their inhibitory activity against breast cancer cells. In silico studies involved pharmacophore modeling using the FOXM1 inhibitor, FDI-6, followed by virtual screening of DrugBank and Selleckchem databases. The selected drugs were prepared for molecular docking, and the crystal structure of FOXM1 was pre-processed for docking simulations. In vitro studies included MTT assays to assess cytotoxicity, and Western blot analysis to evaluate protein expression levels. Our study identified Pantoprazole and Rabeprazole as potential FOXM1 inhibitors through in silico screening and molecular docking. Molecular dynamics simulations confirmed stable interactions of these drugs with FOXM1. In vitro experiments showed both Pantoprazole and Rabeprazole exhibited strong FOXM1 inhibition at effective concentrations and that showed inhibition of cell proliferation. Rabeprazole showed the inhibitor activity at 10 mu M in BT-20 and MCF-7 cell lines. Pantoprazole exhibited FOXM1 inhibition at 30 mu M and in BT-20 cells and at 70 mu M in MCF-7 cells, respectively. Our current study provides the first evidence that Rabeprazole and Pantoprazole can bind to FOXM1 and inhibit its activity and downstream signaling, including eEF2K and pEF2, in breast cancer cells. These findings indicate that rabeprazole and pantoprazole inhibit FOXM1 and breast cancer cell proliferation, and they can be used for FOXM1-targeted therapy in breast or other cancers driven by FOXM1.Öğe A new flavone from antioxidant extracts of Pistacia terebinthus(Elsevier Sci Ltd, 2007) Topcu, Gulacti; Ay, Mehmet; Bilici, Ali; Sarikurkcu, Cengiz; Ozturk, Mehmet; Ulubelen, AyhanAcetone and methanol extracts of the fruits of Pistacia terebinthus L. subsp. terebinthus L. were studied for their antioxidant activity by investigating their total phenolic and flavonoid contents, P-carotene bleaching potential, DPPH radical scavenging effect, scavenging activity on superoxide anion radical, reducing power, and metal chelating effect on ferrous ion. Both extracts showed very similar chemical profile by checking on TLC plates, and exhibited high scavenging activity on superoxide anion radical and DPPH radical. Due to these similarities they were combined and fractionated on a silica gel column for their constituents, and the most active three fractions in DPPH assay were purified to afford a new flavone 6'-hydroxyhypolaetin 3'-methyl ether (1) besides a group of known flavonoids apigenin, luteolin, luteolin 7-O-glucoside, quercetin, quercetagetin 3-methyl ether 7-O-glucoside, isoscutellarein 8-O-glucoside. Their structures were established by UV, UV shift reagents, and H-1 NMR spectroscopic techniques. Antioxidant activity of the new flavone was investigated by P-carotene bleaching and DPPH radical scavenging activity methods, and it showed a high activity in the first system, but not so good in the latter. (c) 2006 Elsevier Ltd. All rights reserved.Öğe Antioxidant activity of Erica arborea(Elsevier, 2007) Ay, Mehmet; Bahadori, Fatemeh; Ozturk, Mehmet; Kolak, Ufuk; Topcu, GuelactiThe antioxidant properties of the methanol extract of leaves and flowers of Erica arborea and the ethyl acetate, butanol and water soluble fractions were investigated. The ethyl acetate extract was found to be the richest for phenolic and flavonoid content which showed the highest antioxidant activity. (c) 2007 Elsevier B.V. All rights reserved.Öğe Antioxidant phenolic compounds from the leaves of Erica Arborea (Ericaceae)(Taylor & Francis Ltd, 2008) Nazemiyeh, Hossein; Bahadori, Fatemeh; Delazar, Abbas; Ay, Mehmet; Topcu, Guelacti; Nahar, Lutfun; Majinda, Runner R. T.Reversed-phase HPLC analyses of the methanol extract of the leaves of Erica arborea afforded a novel phenylpropanoid glucoside, named ericarborin, together with five flavonoids, dihydromyricetin 3-O-alpha-L-rhamnopyranoside, quercetin 3-O-beta-D-glucopyranoside, quercetin 3-O-alpha-L-rhamnopyranoside, apigenin 7-O-beta-D-glucopyranoside and apigenin 7-O-beta-D-(6-O-acetyl-glucopyranoside). While the structure of ericarborin was determined by extensive 1D and 2D NMR analyses, the structures of all known flavonoids were determined by direct comparison of their spectroscopic data with respective literature data. The antioxidant properties of these compounds were assessed by the DPPH assay. The chemotaxonomic significance of these phenolic compounds has been discussed.Öğe Antiproliferative activity of Humulus lupulus extracts on human hepatoma (Hep3B), colon (HT-29) cancer cells and proteases, tyrosinase, ?-lactamase enzyme inhibition studies(Taylor & Francis Ltd, 2016) Onder, Ferah Comert; Ay, Mehmet; Turkoglu, Sumeyye Aydogan; Kockar, Feray Tura; Celik, AyhanThe aims of this study were to examine the antiproliferation of Humulus lupulus extracts on human hepatoma carcinoma (Hep3B) and human colon carcinoma (HT-29) cell lines along with enzyme inhibitory effects of the crude extracts. Potential cell cytotoxicity of six different H. lupulus extracts were assayed on various cancer cells using MTT assay at 24, 48 and 72h intervals. Methanol-1 extract has inhibited the cell proliferation with doses of 0.6-1mg/mL in a time dependent (48 and 72 hours) manner in Hep3B cells with 70% inhibition, while inhibitory effect was not seen in colon cancer cells. Acetone extract has increased the cell proliferation at low doses of 0.1mg/mL for 72h in Hep3B cells and 0.1-0.2mg/mL for 48 and 72h in HT29 cells. The inhibitory effects of the extracts were compared by relative maximum activity values (V-max) using proteases such as -chymotrypsin, trypsin and papain, tyrosinase and -lactamase (penicillinase).Öğe Comparative Study of Antioxidant Properties and Total Phenolic Content of the Extracts of Humulus lupulus L. and Quantification of Bioactive Components by LC-MS/MS and GC-MS(Amer Chemical Soc, 2013) Onder, Ferah Comert; Ay, Mehmet; Sarker, Satyajit D.In this research, antioxidant activities of various extracts obtained from Humulus lupulus L. were compared by DPPH, ABTS, FRAP, and CUPRAC assays. The amount of total phenolic components determined by the Folin-Ciocalteu reagent was found to be highest for 25% aqueous ethanol (9079 +/- 187.83 mg Ferulic acid equivalent/100 g extract) and methanol-1 (directly) (8343 +/- 158.39 mg Ferulic acid equivalent/100 g extract) extracts. The n-hexane extract of H. lupulus exhibited the greatest with DPPH (14.95 +/- 0.03 mu g Trolox equivalent/g sample). The highest phenolic content in the ethanolic extract could be the major contributor to its highest CUPRAC activity (3.15 +/- 0.44 mmol Trolox equivalent/g sample). Methanol-2 (n-hexane, acetone, and methanol) and methanol-3 (n-hexane, dichloromethane, ethylacetate, and methanol) extracts, respectively, exhibited the most potent ABTS (7.35 +/- 0.03 mM Trolox equivalent) and FRAP (1.56 +/- 0.35 mmol Fe2+/g sample) activities. Some of the components from the crude extracts were determined by LC-MS/MS and GC-MS analyses. Comparative screening of antioxidant activities of H. lupulus extracts and quantification of some major components by LC-MS/MS, qualitatively analysis of the reported ones which were optimal under negative ion SIM mode and coinjection, are going to be valuable for food and health applications.Öğe Delivery of Small Molecule EF2 Kinase Inhibitor for Breast and Pancreatic Cancer Cells Using Hyaluronic Acid Based Nanogels(Springer/Plenum Publishers, 2020) Cömert Önder, Ferah; Sağbaş Suner, Selin; Şahiner, Nurettin; Ay, Mehmet; Özpolat, BülentPurpose To evalauted natural polymeric biomaterials including hyaluronic acid (HA) and its copolymeric form HA:Suc nanoparticles (NPs) as drug carrier systems for delivery of hydrophobic small molecule kinase EF2-kinase inhibitor in breast and pancreatic cancer cells. Methods In vitro cellular uptake studies of Rhodamine 6G labaled HA:Suc nanoparticles were evaluated by using flow cytometry analysis and fluorescent microscopy in breast (MDA-MB-231 and MDA-MB-436) and pancreatic cancer cells (PANC-1 and MiaPaca-2). Besides, in vitro release study of compound A (an EF2-kinase inhibitor) as a model hydrophobic drug was performed in the cancer cells. Results These biological evaluation studies indicated that HA and HA:Suc NPs provided a highly effective delivery of compound A were into breast and pancreatic cancer cells, leading to significant inhibition of cell proliferation and colony formation of breast and pancreatic cancer cells. Conclusion HA-sucrose NPs incorporating an EF2-Kinase inhibitor demonstrate significant biologic activity in breast and pancreatic cancer cells. This is the first study that shows natural polymeric drug carriers succesfully deliver a hydrofobic cancer drug into cancer cells. Nanoparticles based on HA:Suc are effective in delivering hydrofobic cancer drugs in breast and pancreatic cancers.Öğe Design, Synthesis, and Molecular Modeling Studies of Novel Coumarin Carboxamide Derivatives as eEF-2K Inhibitors(Amer Chemical Soc, 2020) Onder, Ferah Comert; Durdagi, Serdar; Sahin, Kader; Ozpolat, Bulent; Ay, MehmetEukaryotic elongation factor-2 kinase (eEF-2K) is an unusual alpha kinase commonly upregulated in various human cancers, including breast, pancreatic, lung, and brain tumors. We have demonstrated that eEF-2K is relevant to poor prognosis and shorter patient survival in breast and lung cancers and validated it as a molecular target using genetic methods in related in vivo tumor models. Although several eEF-2K inhibitors have been published, none of them have shown to be potent and specific enough for translation into clinical trials. Therefore, development of highly effective novel inhibitors targeting eEF-2K is needed for clinical applications. However, currently, the crystal structure of eEF-2K is not known, limiting the efforts for designing novel inhibitor compounds. Therefore, using homology modeling of eEF-2K, we designed and synthesized novel coumarin-3-carboxamides including compounds A1, A2, and B1-B4 and evaluated their activity by performing in silico analysis and in vitro biological assays in breast cancer cells. The Molecular Mechanics/Generalized Born Surface Area (MM/GBSA) area results showed that A1 and A2 have interaction energies with eEF-2K better than those of B1-B4 compounds. Our in vitro results indicated that compounds A1 and A2 were highly effective in inhibiting eEF-2K at 1.0 and 2.5 mu M concentrations compared to compounds B1-B4, supporting the in silico findings. In conclusion, the results of this study suggest that our homology modeling along with in silico analysis may be effectively used to design inhibitors for eEF-2K. Our newly synthesized compounds A1 and A2 may be used as novel eEF-2K inhibitors with potential therapeutic applications.Öğe Effects of Pleurotus Eryngii (DC.) Quél. Mushroom Extracts on Cell Proliferation in Breast and Colon Cancer Cell Lines(2024) Önder, Ferah Cömert; Davutlar, Gülce; Önder, Alper; Allı, Hakan; Ay, MehmetThis study was aimed to collect Pleurotus eryngii (DC.) Quél. edible/medicinal mushroom from Çanakkale/Kumkale and to evaluate the antiproliferative effects of alcoholic extracts on breast and colon cancer cell lines. For this purpose, the Soxhlet method prepared methanol and ethanol:H2O (70:30) extracts by gradually increasing solvent polarities. Then, breast (MDA-MB-231, BT-549, BT-20, MCF-7) and colon (HT-29) cancer cell lines were treated with the extracts in increasing concentrations (0.05-0.5 mg/mL) for 48 h. In conclusion, methanol and aqueous ethanol extracts exhibited significant antiproliferative effects in cancer cell lines, according to the MTT assay. The cell viability in the triple-negative breast cancer (TNBC) MDA-MB-231 cell line was highly decreased by methanol extract at a very low concentration (0.1 mg/mL). Furthermore, methanol extract at 0.3 mg/mL reduced the percentage of cell viability in the HT-29 cell line. Aqueous ethanol extract showed antiproliferative activity in breast and colon cancer cell lines at 0.25 mg/mL concentration for 48 h applications. In addition, some bioactive components such as 4-hydroxy flavone, chrysin, and tannic acid of aqueous ethanol extract have been determined by High-Performance Liquid Chromatography (HPLC) analysis. As a result, this study may increase interest in the studies on the anti-cancer activities and the mechanisms of P. eryngii mushroom.Öğe Electrochemical behavior and voltammetric determination of some nitro-substituted benzamide compounds(Tubitak Scientific & Technological Research Council Turkey, 2018) Saglam, Ozlem; Comert Onder, Ferah; Gungor, Tugba; Ay, Mehmet; Dilgin, YusufVoltammetric behaviors of six nitro-substituted benzamides, which are potential prodrug candidates for nitroreductase-based cancer therapy, were investigated using cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The electrochemical behavior of aromatic nitro (ArNO2) compounds by CV indicates that compounds involve various reduction/oxidation steps including the formation of aromatic nitro radical, nitroso, hydroxylamine, and amine groups. Applicability of the voltammetric determination of these prodrug candidates was studied by recording their DPVs, carried out in mixed media (Britton Robinson buffer solution + DMF) at various pH values on a pencil graphite electrode (PGE). Results show that the PGE can offer a disposable, low-cost, and sensitive electrochemical determination method for identifying nitro benzamide compounds. Under the experimental conditions, the PGE had a linear response range from 0.5 to 100 mu M 4-nitro- N-(2-nitrophenyl)benzamide (compound 2). This voltammetric procedure indicates that nitro-substituted benzamide drugs can be successfully determined in pharmaceutical samples.Öğe Humidity effect on real-time response of tetranitro-oxacalix[4] arene-based surface plasmon resonance (SPR) acetone sensor at room temperature(Elsevier Gmbh, 2023) Sen, Sibel; Onder, Ferah Comert; Capan, Rifat; Ay, Mehmet; Erdogan, Cansu OzkayaWe report the effect of humidity on the acetone sensitivity of nano-sized thin films obtained by spin coating the oxacalix[4]arenes(1,3) molecules on suitable substrates in this work. The surface morphologies and volatile organic compound (VOC) sensor properties of spin-coated thin films were examined using atomic force microscopy (AFM) and surface plasmon resonance (SPR), respectively. It was determined that the sensitivities calculated from the measurements performed using a mixture of acetone and water vapor were 14% and 11% incorrect for the 1 and 3 thin film sensors, respectively, compared to those performed with dry air and acetone mixture.Öğe Hyaluronic acid and hyaluronic acid: Sucrose nanogels for hydrophobic cancer drug delivery(Elsevier Science Bv, 2019) Sağbaş Suner, Selin; Ari, Betül; Cömert Önder, Ferah; Özpolat, Bülent; Ay, Mehmet; Şahiner, NurettinPorous and biodegradable hyaluronic acid (HA) nanogel and their copolymeric forms with sucrose (Suc), HA:Sucrose (HA:Suc) nanogels, were synthesized by employing glycerol diglycidyl ether (GDE) as crosslinker with a single step reaction in surfactant-free medium. The size of the nanogels was determined as 150 +/- 50 nm in dried state from SEM images and found to increase to about 540 +/- 47 nm in DI water measured with DLS measurements. The surface areas of HA and HA:Suc nanogels were measured as 18.07 +/- 2.4 and 32.30 +/- 6.1 m(2)/g with porosities of 3.58 +/- 1.8, and 9.44 +/- 3.1 nm via BET analysis, respectively. The zeta potentials for HA and HA:Suc nanogels were measured as -33 +/- 1.4 and -30 +/- 1.2 mV, respectively. The thermal degradation of both types of nanogels revealed similar trends, while hydrolytic degradation of the nanogels was about 22.7 +/- 02 wt% in 15 days. Both HA and HA:Suc nanogels were stable in blood up to 250 mu g/mL concentration with approximately 0.5 +/- 0.1% hemolysis ratio and 76 +/- 12% blood clotting indices, respectively. Finally, these nanogels were used as a sustained slow-release or long-term delivery system over 2 days for a hydrophobic cancer drug, 3-((E)-3-(4-hydroxyphenyl)acryloyl)-2H-chromen-2-on (A(#)) established by our group. The nanogels successfully delivered the model drug A at 10.43 +/- 2.12 mg/g for 2 days. (C) 2019 Elsevier B.V. All rights reserved.Öğe Identifying highly effective coumarin-based novel cholinesterase inhibitors by in silico and in vitro studies(Elsevier Science Inc, 2022) Onder, Ferah Comert; Sahin, Kader; Senturk, Murat; Durdagi, Serdar; Ay, MehmetInhibition of high cholinesterase levels including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), is one of the most important strategies for the treatment of Alzheimer's disease (AD). Clinically limited drugs are used in the treatment of AD, so there is a need to find new effective inhibitors today. Therefore, in this study, synthesized six coumarin carboxamides (A1, A2, B1-B4) were evaluated against AChE and BChE by combined in silico and in vitro studies. The in vitro assessment of studied compounds revealed that A1, A2, B3, and B4 showed highest inhibition potential against AChE and BChE. As demonstrated with our structure activity relationship (SAR) study, the promising inhibition result of AChE at nanomolar concentrations was obtained with heterocyclic amines including pyrrolidine and N-methyl piperazine moieties for tertiary amide substituted coumarin compounds B3 and B4, displaying K-1 values of 9.78 nM and 8.07 nM, respectively. Thus, compounds B3 and B4 had around 5.7- and 6.9-fold more potency compared to the reference molecule, neostigmine. Moreover, coumarin-3-carboxamide derivative A1 bearing benzylmorpholine moiety on coumarin scaffold at position 3 displayed stronger inhibition potential against BChE. Furthermore, in order to better understand their molecular mechanisms in these targets, we conducted molecular docking and MD simulations. Our promising preclinical results show that the lead compounds A1, A2, B3 and B4 have high potential as effective inhibitors for the treatment of AD.Öğe In vitro and in silico studies of nitrobenzamide derivatives as potential anti-neuroinflammatory agents(Taylor & Francis Inc, 2020) Kulabas, Seda Savranoglu; Onder, Ferah Comert; Yilmaz, Yakup Berkay; Ozleyen, Adem; Durdagi, Serdar; Sahin, Kader; Ay, MehmetCommunicated by Ramaswamy H. SarmaÖğe In vitro drug release studies for the treatment of TNBC and pancreatic cancers from natural derivated polymeric micro- and nano-particles(Amer Chemical Soc, 2018) Cömert Önder, Ferah; Sağbaş, Selin; Ay, Mehmet; Özpolat, Bülent; Şahiner, Nurettin[Anstract Not Available]Öğe Investigation of antioxidant, enzyme inhibition and antiproliferative activities of blackthorn (Prunus spinosa L.) extracts(International Society of Academicians, 2023) Sönmez, Merve; Önder, Ferah Cömert; Tokay, Esra; Celık, Ayhan; Köçkar, Feray; Ay, MehmetNatural products have a key role in drug discovery in pharmacology and medicine. Prunus spinosa L. (blackthorn) grown in Çanakkale province in western Turkey, is known as a medicinal plant, a rich source of biologically active compounds such as phenolics, flavonoids and anthocyanidins. The flower and fruit extracts of the plant are subjects of many studies, but they usually lack in details of its potential for bio-inhibition studies. Thus, this study aimed to investigate the antioxidant, enzyme inhibition and antiproliferative activity studies of the methanol, ethyl acetate, dichloromethane, and n-hexane extracts of the plant. The ethyl acetate and methanol extracts demonstrated more better antioxidant activity with DPPH, FRAP, CUPRAC, and TEAC assays. Enzyme inhibition studies of the extracts were performed using β-lactamase and various proteases. The methanol (FL) and ethyl acetate (FL and L) extracts at the concentration of 10 mg/mL, showed good inhibition against α-chymotrypsin, trypsin, and papain with values of 22.6%, 34.7% and 92.1%, respectively. Furthermore, the methanol and ethyl acetate extracts have displayed higher cytotoxic effect against cancer cells such as Hep3B and HT29 when compared to healthy cells (HUVEC) using MTT assay. The findings suggest that P. spinosa L. extracts and their components may be potential for further investigations of novel drug candidatesÖğe Kanser Tedavisinde Sfingozin Kinaz 1 İnhibitörleri Olarak Potansiyel Fitokimyasallar Üzerine Sanal Tarama, Moleküler Yerleştirme ve Moleküler Dinamik Simülasyon Çalışmaları(International Society of Academicians, 2024) Önder, Alper; Davutlar, Gülce; Ay, Mehmet; Önder, Ferah CömertLipid kinazlar olarak sfingozin kinazlar (SphK), sfingozinin (Sph) sfingozin-1-fosfata (S1P) fosforilasyonunu katalize eder. S1P sinyal yolunu hedeflemek birçok insan hastalığı için önemli bir stratejidir. Burada, tıbbi bir bitkinin ana prenillenmiş biyoaktif bileşenlerini değerlendirdik ve flavonoid bileşiklerle sanal bir tarama çalışması ve ardından hedefe yönelik kanser tedavisi için moleküler yerleştirme ve moleküler dinamik (MD) simülasyonu gerçekleştirdik. In silico ADMET ve ilaca benzerlik sonuçları BIOVIA Discovery Studio (DS) tarafından belirlendi. Moleküler yerleştirme ve moleküler dinamik (MD) simülasyonları, filtrelenmiş ligandlarla birlikte Glide/SP ve Maestro Desmond kullanılarak gerçekleştirildi. Glide/SP yerleştirme sonuçları, ksantohumol (XN), 8-prenilnaringenin (8-PN) ve neobavaizoflavon ile SphK1'e karşı daha yüksek bağlanma ilgisi gösterdi. SphK1'i hedefleyen spesifik amino asit kalıntıları arasında üç molekül güçlü hidrojen bağlanması gösterdi. GROMACS tarafından gerçekleştirilen 200 ns MD simülasyon analizi sırasında SphK1-XN ve SphK1-neobavaizoflavon kompleksleri arasında önemli yapısal değişiklikler görülmedi. XN- ve neobavaizoflavon-protein komplekslerinin ortalama kare sapma (RMSD) ortalama değerleri, serbest SphK1 ile karşılaştırıldığında sırasıyla 0,2626 nm, 0,2589 nm ve 0,2508 nm olarak bulundu. Sonuç olarak XN ve 8-PN ile neobavaizoflavon, daha ileri in vitro ve in vivo çalışmalar için incelenmek üzere SphK1'in potansiyel inhibitör adayları olarak belirlendiÖğe Major Bioactive Prenylated Flavonoids from Humulus lupulus L., Their Applications in Human Diseases and Structure-Activity Relationships (SAR) - A Review(Tabriz University of Medical Sciences, 2024) Cömert Önder, Ferah; Kalın, Sevil; Şahin, Nebahat; Davutlar, Gülce; Abusharkh, Khaled A.N.; Maraba, Özlem; Ay, Mehmet; Hal, Rabia SelinaIn recent years, the incidence of cancers, inflammatory diseases, Alzheimer's disease, glucose metabolism disorder and diabetes has increased alarmingly which demands more research into the discovery of new drug candidates to treat these human diseases. Main phytochemicals from Humulus lupulus L. (hops) have been demonstrated to have positive impacts on human health, and prenylated flavonoids are one of the major groups of bioactive phytochemicals found in this plant. Thus, this review summarizes the role of major prenylated components in hops in human diseases including cancer, inflammation and viral infections. In silico studies of prenylated bioactive compounds against various drug targets such as histone deactylases (HDACs), sirtuins (SIRTs), and acetylcholinesterase (AChE), and the molecular molecular interactions between protein and ligand have also been included. Furthermore, the structure-activity relationships (SAR) studies on these compounds are highlighted. This review concludes that the prenylated phytochemicals from H. lupulus L., including xanthohumol (XN), isoxanthohumol (IXN), 8-prenylnaringenin (8-PN) and 6-prenylnaringenin (6-PN), have promising roles in human health and may contribute to new drug discovery and development.Öğe Modification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogen(Pergamon-Elsevier Science Ltd, 2016) Celik, Ayhan; Yetis, Gulden; Ay, Mehmet; Gungor, TugbaThe use of existing antibiotics in the form of prodrug followed by activation using enzymes of pathogenic origin could be a useful approach for antimicrobial therapy. To investigate this idea, a common antibiotic, sulfamethoxazole has been redesigned in the form of a prodrug by simple functional group replacement. Upon reductive activation by a type I nitroreductase from a pathogen, the drug displayed enhanced antimicrobial capacity. This strategy could improve the efficacy and selectively of antibiotics and reduce the incidence of resistance. (C) 2016 Elsevier Ltd. All rights reserved.
