S. Özkorucuklu, Besnik Uka, Gizem Yıldırım Baştemur
In this study, the electrochemical behaviors of cephalexin and cefazoline on disposable pencil graphite electrode were investigated in phosphate buffer at pH of 4.5 to 6.0 by differential pulse voltammetry. Sample analysis was performed in phosphate buffer at the optimum medium determined for each sample. Validation parameters were studied to show the correctness, sensitivity, and consistency of the method developed for the cephalosporins. It was concluded that disposable pencil graphite electrode could be used effectively in the determination of cephalosporins. The limits of detection (S/N=3) were found to be 0.115 mM and 0.303 mM, for cephalexin and cefazoline, respectively. The analysis of these compounds in pharmaceutical formulations and biological samples was carried out at defined optimum conditions. The recovery values were around 100%.
{"title":"Voltammetric Analysis of Cephalexin and Cefazoline in Pharmaceutical Formulation and Biological Samples","authors":"S. Özkorucuklu, Besnik Uka, Gizem Yıldırım Baştemur","doi":"10.18596/JOTCSA.469028","DOIUrl":"https://doi.org/10.18596/JOTCSA.469028","url":null,"abstract":"In this study, the electrochemical behaviors of cephalexin and cefazoline on disposable pencil graphite electrode were investigated in phosphate buffer at pH of 4.5 to 6.0 by differential pulse voltammetry. Sample analysis was performed in phosphate buffer at the optimum medium determined for each sample. Validation parameters were studied to show the correctness, sensitivity, and consistency of the method developed for the cephalosporins. It was concluded that disposable pencil graphite electrode could be used effectively in the determination of cephalosporins. The limits of detection (S/N=3) were found to be 0.115 mM and 0.303 mM, for cephalexin and cefazoline, respectively. The analysis of these compounds in pharmaceutical formulations and biological samples was carried out at defined optimum conditions. The recovery values were around 100%.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42610048","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present work consists the elaboration and the rheological behaviors of nanocomposite (NGTHTPTBAE/MDA/TSP) in the presence of the epoxy resin nanoglycidyl trihydrazine 4.4.4-tripropoxy tribisphenol A of ethylene (NGTHTPTBAE), methylene dianiline (MDA) and trisodium phosphate (TSP) used as filler. Furthermore, we have studied the performance of nanocomposites (NGTHTPTBAE/MDA/TSP) crosslinked by methylene dianiline and formulated by trisodium phosphate at different percentages. Then, the storage modulus G' and the loss modulus G'' (or tanδ = G''/G') are established as a function of the temperature. From these dependencies, we determined the glass transition temperature or tanδ maximum. Moreover, tan δ > 1 for liquid-like materials and it becomes lower than unity for solid-like materials. Finally, the dispersion of the trisodium phosphate incorporated into various prepared nanocomposite (NGTHTPTBAE/MDA/TSP) was determined using the scanning electron microscope (SEM).
{"title":"Morphological and rheological study of the epoxy polymer and their nanocomposite (NGTHTPTBAE/MDA/TSP) crosslinked by methylene dianiline and formulated by trisodium phosphate","authors":"R. Hsissou, M. Berradi, M. E. Bouchti, A. Harfi","doi":"10.18596/JOTCSA.477191","DOIUrl":"https://doi.org/10.18596/JOTCSA.477191","url":null,"abstract":"The present work consists the elaboration and the rheological behaviors of nanocomposite (NGTHTPTBAE/MDA/TSP) in the presence of the epoxy resin nanoglycidyl trihydrazine 4.4.4-tripropoxy tribisphenol A of ethylene (NGTHTPTBAE), methylene dianiline (MDA) and trisodium phosphate (TSP) used as filler. Furthermore, we have studied the performance of nanocomposites (NGTHTPTBAE/MDA/TSP) crosslinked by methylene dianiline and formulated by trisodium phosphate at different percentages. Then, the storage modulus G' and the loss modulus G'' (or tanδ = G''/G') are established as a function of the temperature. From these dependencies, we determined the glass transition temperature or tanδ maximum. Moreover, tan δ > 1 for liquid-like materials and it becomes lower than unity for solid-like materials. Finally, the dispersion of the trisodium phosphate incorporated into various prepared nanocomposite (NGTHTPTBAE/MDA/TSP) was determined using the scanning electron microscope (SEM).","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43722744","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The conductive poly( o -anisidine) (POA) and noble Ag particles were simultaneously deposited on wool fabrics, by the polymerization of o -anisidine with the oxidant mixtures of silver nitrate and ammonium persulfate in different sulfonic acids media. The effect of concentrations of sulfonic acids was investigated on the contents of conductive components (POA/Ag%) and the volume resistivity of the composites. The change in the surface morphology of POA coating, distribution of Ag particles and conformance of noble Ag particles were identified with SEM, EDX, and XRD techniques, respectively. It was observed that the usage of sulfonic acids significantly increased the coating density of the POA/Ag, compared to a control sample prepared in 1.0 M HNO 3 solution. The composites were tested in the catalytic reduction of a dye molecule (methylene blue) with the existence of excess sodium borohydride, and a relatively high catalytic activity (70%) was obtained at 75 min compared to a control POA/wool sample.
在不同的磺酸介质中，用氧化剂硝酸银和过硫酸铵将o -茴香胺聚合，制备出导电聚o -茴香胺(POA)和银同时沉积在羊毛织物上。研究了磺酸浓度对复合材料导电组分POA/Ag%含量和体积电阻率的影响。利用SEM、EDX和XRD技术分别对POA涂层表面形貌的变化、银粒子的分布和贵金属银粒子的一致性进行了表征。结果表明，与在1.0 M hno3溶液中制备的对照样品相比，磺酸的使用显著提高了POA/Ag的包覆密度。在过量硼氢化钠存在的情况下，对复合材料进行了催化还原染料分子(亚甲基蓝)的测试，与对照POA/羊毛样品相比，在75分钟内获得了相对较高的催化活性(70%)。
{"title":"Simultaneous Deposition of Poly(o-anisidine) and Noble Ag Particles on Wool Fabric and The Evaluation of Its Performance as Catalyst in Dye Reduction","authors":"M. K. Erdoğan, M. Karakışla","doi":"10.18596/JOTCSA.512360","DOIUrl":"https://doi.org/10.18596/JOTCSA.512360","url":null,"abstract":"The conductive poly( o -anisidine) (POA) and noble Ag particles were simultaneously deposited on wool fabrics, by the polymerization of o -anisidine with the oxidant mixtures of silver nitrate and ammonium persulfate in different sulfonic acids media. The effect of concentrations of sulfonic acids was investigated on the contents of conductive components (POA/Ag%) and the volume resistivity of the composites. The change in the surface morphology of POA coating, distribution of Ag particles and conformance of noble Ag particles were identified with SEM, EDX, and XRD techniques, respectively. It was observed that the usage of sulfonic acids significantly increased the coating density of the POA/Ag, compared to a control sample prepared in 1.0 M HNO 3 solution. The composites were tested in the catalytic reduction of a dye molecule (methylene blue) with the existence of excess sodium borohydride, and a relatively high catalytic activity (70%) was obtained at 75 min compared to a control POA/wool sample.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46976695","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
BisPMB (1,8-(bis- p -methoxyphenyl)-2,3,7-trithiaocta-4-ene 7-oxide) is a synthetic analogue of the natural compound ajoene, which is a bioactive natural product obtained from rearrangement of the unstable and reactive organosulfur compound allicin produced when garlic is freshly crushed. BisPMB has been shown to have superior cancer-cell cytotoxicity compared with ajoene and a modest selectivity towards cancer cells over non-cancerous ones. In this study, the inhibition effects of E / Z -bisPMB and Z -bisPMB against human carbonic anhydrase isozymes I and II (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were investigated in which E / Z -bisPMB and Z -bisPMB showed similar inhibition profiles against the four enzymes tested, with the IC 50 values ranging from 10.9 to 439.7 nM and the K i values ranging from 5.4 to 195.4 nM. Furthermore, bisPMB was more potent at inhibiting CA I, CA II and AChE compared with commercially available inhibitors.
BisPMB(1,8-(双-对-甲氧基苯基)-2,3,7-三硫辛-4-烯7-氧化物)是天然化合物ajoene的合成类似物，ajoene是一种生物活性天然产物，由不稳定的活性有机硫化合物大蒜素在新鲜粉碎时重排而成。与阿约烯相比，BisPMB已被证明具有优越的癌细胞细胞毒性，并且对癌细胞比非癌细胞有适度的选择性。本研究考察了E / Z -bisPMB和Z -bisPMB对人碳酸酐酶同工酶I和II (hCA I和II)、乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BuChE)的抑制作用，结果表明E / Z -bisPMB和Z -bisPMB对4种酶的抑制作用相似，ic50值为10.9 ~ 439.7 nM, K I值为5.4 ~ 195.4 nM。此外，与市售抑制剂相比，bisPMB在抑制CA I, CA II和AChE方面更有效。
{"title":"Inhibition of Carbonic Anhydrase, Acetylcholinesterase and Butyrylcholinesterase by BisPMB, A Synthetic Analogue of Ajoene","authors":"N. Stellenboom","doi":"10.18596/JOTCSA.484444","DOIUrl":"https://doi.org/10.18596/JOTCSA.484444","url":null,"abstract":"BisPMB (1,8-(bis- p -methoxyphenyl)-2,3,7-trithiaocta-4-ene 7-oxide) is a synthetic analogue of the natural compound ajoene, which is a bioactive natural product obtained from rearrangement of the unstable and reactive organosulfur compound allicin produced when garlic is freshly crushed. BisPMB has been shown to have superior cancer-cell cytotoxicity compared with ajoene and a modest selectivity towards cancer cells over non-cancerous ones. In this study, the inhibition effects of E / Z -bisPMB and Z -bisPMB against human carbonic anhydrase isozymes I and II (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were investigated in which E / Z -bisPMB and Z -bisPMB showed similar inhibition profiles against the four enzymes tested, with the IC 50 values ranging from 10.9 to 439.7 nM and the K i values ranging from 5.4 to 195.4 nM. Furthermore, bisPMB was more potent at inhibiting CA I, CA II and AChE compared with commercially available inhibitors.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46727633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
In this study, iron oxyborate (Fe 3 BO 6 ) was first synthesized through solution combustion method as a potential anode material for lithium-ion batteries. Urea, glycine, citric acid, carbohydrazide, hexamethylene tetramine, and starch were used as fuel sources and the effects of fuels were investigated. The obtained materials were structurally characterized by FT-IR, powder-XRD and solid UV-Vis. The pure crystalline Fe 3 BO 6 was synthesized at low temperature and short reaction time using glycine assisted solution combustion method. It was thermally stable up to 945 °C with non-uniform morphology and a highly porous structure. The magnetic properties were also studied and Fe 3 BO 6 show antiferromagnetic behavior.
{"title":"Solution Combustion Synthesis of Iron Oxyborate (Fe3BO6)","authors":"D. Ozer, O. Icten","doi":"10.18596/JOTCSA.500355","DOIUrl":"https://doi.org/10.18596/JOTCSA.500355","url":null,"abstract":"In this study, iron oxyborate (Fe 3 BO 6 ) was first synthesized through solution combustion method as a potential anode material for lithium-ion batteries. Urea, glycine, citric acid, carbohydrazide, hexamethylene tetramine, and starch were used as fuel sources and the effects of fuels were investigated. The obtained materials were structurally characterized by FT-IR, powder-XRD and solid UV-Vis. The pure crystalline Fe 3 BO 6 was synthesized at low temperature and short reaction time using glycine assisted solution combustion method. It was thermally stable up to 945 °C with non-uniform morphology and a highly porous structure. The magnetic properties were also studied and Fe 3 BO 6 show antiferromagnetic behavior.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45456720","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pollution with the heavy metals of Kosovo's rivers has been and continues to be a serious concern not only for the population, but also for responsible institutions that deal with environmental protection in our country. Based on this fact and our doubts regarding the quality of the river waters of the Municipality of Gjilan, we were motivated to conduct a study of the quality of the Mirusha, Stanishor and Morava river waters. During our research, we have set eight monitoring points for determining the exact level of concentration of heavy metals in the river waters quoted above. The heavy metals analyzed in this study were: Pb, Hg, Mn, Cu, Fe, Ni, Cr, Cd, Zn and Ba. The analytical technique used to determine the concentration of heavy metals was ICP-OES. The obtained results show that Fe, Mn and Ba exceed the allowed level at several monitoring points of the Mirusha and Stanishor rivers and appears in the degree of pollution with these metals of Morava river waters. The presence of heavy metals in the waters of these rivers negatively affects habitat waters and indirectly human health. Therefore, the identification and then suggestions regarding elimination of polluting sources are the subject of this study.
{"title":"Concentration of heavy metals in Mirusha and Stanishor rivers of Gjilan municipality and their impact on pollution of the Morava river, Kosovo","authors":"V. Beluli, Ismet Mulliqi","doi":"10.18596/JOTCSA.489098","DOIUrl":"https://doi.org/10.18596/JOTCSA.489098","url":null,"abstract":"Pollution with the heavy metals of Kosovo's rivers has been and continues to be a serious concern not only for the population, but also for responsible institutions that deal with environmental protection in our country. Based on this fact and our doubts regarding the quality of the river waters of the Municipality of Gjilan, we were motivated to conduct a study of the quality of the Mirusha, Stanishor and Morava river waters. During our research, we have set eight monitoring points for determining the exact level of concentration of heavy metals in the river waters quoted above. The heavy metals analyzed in this study were: Pb, Hg, Mn, Cu, Fe, Ni, Cr, Cd, Zn and Ba. The analytical technique used to determine the concentration of heavy metals was ICP-OES. The obtained results show that Fe, Mn and Ba exceed the allowed level at several monitoring points of the Mirusha and Stanishor rivers and appears in the degree of pollution with these metals of Morava river waters. The presence of heavy metals in the waters of these rivers negatively affects habitat waters and indirectly human health. Therefore, the identification and then suggestions regarding elimination of polluting sources are the subject of this study.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41501250","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The antimicrobial properties of silver compounds and biological properties of benzimidazole derivatives have been well known for many years. In the present study, in terms of their biological potential, six novel silver(I)-N-alkylbenzimidazole derivatives were synthesized in order to examine their carbonic anhydrase (CA) inhibitory properties. All complexes were characterized by the combination of 1H NMR, 13C NMR, mass, FT-IR spectroscopic methods and elemental analyses. The inhibitory properties of all complexes were tested on the esterase activity of human CA I and II (hCA I and hCA II). Acetazolamide was used as a standard. All complexes inhibited the hCA I and hCA II activity in the range of 27.37-29.58 µM and 20.93-27.25 µM, respectively.
{"title":"Synthesis, Characterization, and Carbonic Anhydrase Inhibitory Properties of Silver(I) Complexes of Benzimidazole Derivatives","authors":"Mert Ogun Karataş, Adem Ergün","doi":"10.18596/JOTCSA.546960","DOIUrl":"https://doi.org/10.18596/JOTCSA.546960","url":null,"abstract":"The antimicrobial properties of silver compounds and biological properties of benzimidazole derivatives have been well known for many years. In the present study, in terms of their biological potential, six novel silver(I)-N-alkylbenzimidazole derivatives were synthesized in order to examine their carbonic anhydrase (CA) inhibitory properties. All complexes were characterized by the combination of 1H NMR, 13C NMR, mass, FT-IR spectroscopic methods and elemental analyses. The inhibitory properties of all complexes were tested on the esterase activity of human CA I and II (hCA I and hCA II). Acetazolamide was used as a standard. All complexes inhibited the hCA I and hCA II activity in the range of 27.37-29.58 µM and 20.93-27.25 µM, respectively.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41675876","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zeliha Ustun Argon, N. Ilhan, A. Gökyer, S. Öztürk, Beril Koparal
This study has focused on Morus alba, which is grown in Turkey mostly for fruit production. M. alba seeds’ analysis results showed that oil, protein, ash, ash insoluble in hydrochloric acid, total carbohydrate were 21%, 21.58±0.13g, 3.99±0.13g, 0.9±0.00g, 54.76±2.42 g/100g respectively, main minerals were calcium, phosphorus and potassium. Dominated fatty acids were linoleic acid (80.56±0.22), palmitic acid (7.96±0.06), oleic acid (7.11±0.05). The primary volatiles were l-limonene, 2,2-dimethyldecane, hexanal. Sterol components were found as beta-sitosterol>delta-5-avenasterol>campesterol>cholestanol with 5501.49±44.26 mg/kg total sterols. Tocopherols were δ-tocopherol, γ-tocopherol, β-tocopherol, α-tocopherol, total phenolic content, the radical scavenging activity were 257.67 ± 4.51, 18.23 ± 0.11, 6.71 ± 0.13, 3.23 ± 0.06 mg/kg, 137.1±0.36 mgGAE/100goil, 19.9±0.46% respectively. Other physicochemical properties were free fatty acid (1.55±0.89% oleic acid), peroxide value (3.23±0.55 meqO 2 /kg oil), p-anisidine value (1.18±0.55) and refractive index (40 0 C) (1.4687±0.00). As a result, M. alba seeds and oil with its fatty acid, tocopherol, sterol and mineral composition can be used as nutritional supplements.
{"title":"Phytochemical Evaluation of Morus alba Seeds and Cold Pressed Oil","authors":"Zeliha Ustun Argon, N. Ilhan, A. Gökyer, S. Öztürk, Beril Koparal","doi":"10.18596/JOTCSA.470279","DOIUrl":"https://doi.org/10.18596/JOTCSA.470279","url":null,"abstract":"This study has focused on Morus alba, which is grown in Turkey mostly for fruit production. M. alba seeds’ analysis results showed that oil, protein, ash, ash insoluble in hydrochloric acid, total carbohydrate were 21%, 21.58±0.13g, 3.99±0.13g, 0.9±0.00g, 54.76±2.42 g/100g respectively, main minerals were calcium, phosphorus and potassium. Dominated fatty acids were linoleic acid (80.56±0.22), palmitic acid (7.96±0.06), oleic acid (7.11±0.05). The primary volatiles were l-limonene, 2,2-dimethyldecane, hexanal. Sterol components were found as beta-sitosterol>delta-5-avenasterol>campesterol>cholestanol with 5501.49±44.26 mg/kg total sterols. Tocopherols were δ-tocopherol, γ-tocopherol, β-tocopherol, α-tocopherol, total phenolic content, the radical scavenging activity were 257.67 ± 4.51, 18.23 ± 0.11, 6.71 ± 0.13, 3.23 ± 0.06 mg/kg, 137.1±0.36 mgGAE/100goil, 19.9±0.46% respectively. Other physicochemical properties were free fatty acid (1.55±0.89% oleic acid), peroxide value (3.23±0.55 meqO 2 /kg oil), p-anisidine value (1.18±0.55) and refractive index (40 0 C) (1.4687±0.00). As a result, M. alba seeds and oil with its fatty acid, tocopherol, sterol and mineral composition can be used as nutritional supplements.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44970727","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
DNA topoisomerases are proved therapeutic targets of anticancer and antibacterial drugs. Structures of topoisomerase–DNA and inhibitor ternary complexes have revealed the exact binding sites and mechanisms of topoisomerase poisons. There are two isoforms of Human Topoisomerase II; α and β. Both of them perform similar functions and their levels differ depending on the replicative activity and type of tissue. Topo IIα is preferentially expressed in proliferating cells. Thus selective Topo IIα inhibitors have been of particular interest in cancer therapy, as they may represent a more targeted approach to highly proliferative cells. In this study, we use structure based virtual screening method with molecules which are commercially available in the ZINC database. Docking studies were performed by Glide module available in Schrodinger software, Ligand filtration was also done to obtain an efficient collection of hit molecules by employing Lipinski “rule of five” and pharmacokinetic properties of the compounds were tested using Qikprop module. From approximately ten thousand compounds from Zinc database it was possible to select 4 top chemical structures with good inhibiting profile for topo II, with suitable ADME/Tox properties, thus comp. 1-4 could be the promising inhibitors of human topo IIα enzyme.
{"title":"Discovery of New DNA Topoisomerase II Inhibitors using Structure Based Virtual Screening Method","authors":"T. Ertan-Bolelli, K. Bolelli","doi":"10.18596/JOTCSA.466457","DOIUrl":"https://doi.org/10.18596/JOTCSA.466457","url":null,"abstract":"DNA topoisomerases are proved therapeutic targets of anticancer and antibacterial drugs. Structures of topoisomerase–DNA and inhibitor ternary complexes have revealed the exact binding sites and mechanisms of topoisomerase poisons. There are two isoforms of Human Topoisomerase II; α and β. Both of them perform similar functions and their levels differ depending on the replicative activity and type of tissue. Topo IIα is preferentially expressed in proliferating cells. Thus selective Topo IIα inhibitors have been of particular interest in cancer therapy, as they may represent a more targeted approach to highly proliferative cells. In this study, we use structure based virtual screening method with molecules which are commercially available in the ZINC database. Docking studies were performed by Glide module available in Schrodinger software, Ligand filtration was also done to obtain an efficient collection of hit molecules by employing Lipinski “rule of five” and pharmacokinetic properties of the compounds were tested using Qikprop module. From approximately ten thousand compounds from Zinc database it was possible to select 4 top chemical structures with good inhibiting profile for topo II, with suitable ADME/Tox properties, thus comp. 1-4 could be the promising inhibitors of human topo IIα enzyme.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49567362","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Electrochemical behavior of naphazoline hydrochloride on a carbon paste electrode that was modified with aluminium oxide nanoparticles (Al 2 O 3 NPs) was investigated in a Britton-Robinson (BR) buffer (pH 7.0) using various voltammetric techniques. The results support the presence of an irreversible and diffusion-controlled electrochemical oxidation signal of naphazoline hydrochloride which is approximately at 0.9 V vs. Ag/AgCl. A selective, accurate, and simple square-wave anodic adsorptive stripping voltammetric method was purposed for naphazoline hydrochloride detection. The linear response was within the range of 5.0 × 10 -8 - 3.0 × 10 -5 mol L -1 with a detection limit of 2.6 × 10 –8 mol L –1 (0.0064 mg L –1 ). In addition, the purposed method was also utilized for naphazoline hydrochloride determination in human serum sample.
在pH 7.0的布里顿-罗宾逊(BR)缓冲液中，采用不同伏安技术研究了盐酸萘唑啉在氧化铝纳米粒子修饰的碳糊电极上的电化学行为。结果支持盐酸萘唑啉存在不可逆的扩散控制电化学氧化信号，该信号约为0.9 V /Ag /AgCl。建立了一种选择性好、准确度高、简便的方波阳极吸附溶出伏安法检测盐酸萘唑啉。线性响应范围为5.0 × 10 -8 ~ 3.0 × 10 -5 mol L -1，检出限为2.6 × 10 -8 mol L -1 (0.0064 mg L -1)。此外，该方法还可用于人血清样品中盐酸萘唑啉的测定。
{"title":"Doping Agent Naphazoline Hydrochloride: Development of Simple and Fast Voltammetric Method for Its Determination in Human Serum","authors":"Tuğçe Çetinkol, F. Öztürk, P. Erden","doi":"10.18596/JOTCSA.450793","DOIUrl":"https://doi.org/10.18596/JOTCSA.450793","url":null,"abstract":"Electrochemical behavior of naphazoline hydrochloride on a carbon paste electrode that was modified with aluminium oxide nanoparticles (Al 2 O 3 NPs) was investigated in a Britton-Robinson (BR) buffer (pH 7.0) using various voltammetric techniques. The results support the presence of an irreversible and diffusion-controlled electrochemical oxidation signal of naphazoline hydrochloride which is approximately at 0.9 V vs. Ag/AgCl. A selective, accurate, and simple square-wave anodic adsorptive stripping voltammetric method was purposed for naphazoline hydrochloride detection. The linear response was within the range of 5.0 × 10 -8 - 3.0 × 10 -5 mol L -1 with a detection limit of 2.6 × 10 –8 mol L –1 (0.0064 mg L –1 ). In addition, the purposed method was also utilized for naphazoline hydrochloride determination in human serum sample.","PeriodicalId":17402,"journal":{"name":"Journal of the Turkish Chemical Society, Section A: Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42532357","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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