Yazar "Usanmaz, Hande" seçeneğine göre listele

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    Biological, computational evaluation of novel benzofuranyl derivatives as acetylcholinesterase and butyrylcholinesterase
    (Taylor & Francis Ltd, 2024) Usanmaz, Hande; Tas, Omer; Ekinci, Deniz; Uba, Abdullahi Ibrahim; Atmaca, Ufuk
    Aim: A highly efficient one-step method has been developed for the synthesis of benzofuranyl derivatives from 2-benzoylcyclohexane-1-carboxylic acid derivatives using chlorosulfonyl isocyanate. This novel method provides a practical, cost-effective and efficient approach. Materials & methods: The inhibitory effects of benzofuranyl derivatives on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes were investigated. Ki values were determined to range from 0.009 to 0.61 mu M for AChE and 0.28 to 1.60 mu M for BChE. Molecular docking analysis provided insights into the interaction modes and binding patterns of these compounds with AChE and BChE. Conclusion: Kinetic findings of our study suggest that some of our compounds exhibited more effective low micromolar inhibition compared with the reference, and these derivatives could be to design more powerful agents.
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    Improved chromatographic method for purification of lactoperoxidase from different milk sources
    (Taylor & Francis Inc, 2017) Koksal, Zeynep; Usanmaz, Hande; Bayrak, Songul; Ozdemir, Hasan
    Our previous studies showed that sulfanilamide is a new competitive inhibitor of and can be used in the purification of lactoperoxidase (LPO, EC1.11.1.7) from milk. However, this method has some disadvantages like a lower purification factor. The aim of the present study is to improve the purification process of milk LPO from different sources. For this purpose, 16 commercial sulfanilamide derivatives were selected for inhibition studies to determine the best inhibitor of bovine LPO by calculating kinetic parameters. A cyanogen bromide-activated Sepharose 4B affinity matrix was synthesized by coupling with each competitive inhibitor. Among the inhibitors, 5-amino-2-methylbenzenesulfonamide and 2-chloro-4-sulfamoylaniline were used as ligands for the purification of LPO from bovine, buffalo, cow, and goat milks with 1059.37, 509.09, 232.55, and 161.90, and 453.12-, 151.86-, 869.00-, and 447.57-fold, respectively. Our results show that 5-amino-2-methylbenzenesulfonamide, 2-chloro-4sulfamoylaniline, and 5-amino-1-naphthalenesulfonamide are the best inhibitors for one-step purification of the enzyme.
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    Investigating Anxiety, Depression and Obsessive-Compulsive Disorders (OCD) among healthcare workersin COVID-19 unit and the control group
    (2020) Ergenç, Hasan; Ertürk, Zeynep; Usanmaz, Mustafa; Tor, Ibrahim Hakki; Usanmaz, Hande; Akçay, Emine Ülkü
    To investigate anxiety, depression, and Obsessive-Compulsive Disorders (OCDs) among the healthcare workers (HCWs) to compare the healthcare workers in COVID positive services with the control group. This cross-sectional study was conducted on 198 subjects participating in the study. To test the difference between the two groups involved in COVID-19 hospitalization section and normal section in Anxiety, Depression, and Obsessive-Compulsive Disorders Scale, two sample independent t-tests, however, Welch–Satterthwaite P Values were considered for test significance. The categorical variables (sex, branch type, etc.) were also tested using the Chi-Square test to make sure that the two samples were not influenced by the demographics of the population. 198 subjectspartici pated in the study, among whom 72% were female and 28.3% were male. 130 participants (66%) worked in COVID and 68 participants (35%) worked in other sections.The mean age of the two samples was close to 35 and most of them (~45%) were nurses. 57% of the pooled samples had Emergency Response Experience (ERE).There was no significant difference between the two groups regarding sex, education, marital status, and ERE, however, the branch type showed major differences between the two groups(P-value < 0.08). The age difference between the two groups was also insignificant. Working in the COVID-19 section significantly increased anxiety scores from 9.62 to 13.15 with a P-value of <0.03. Obsessive-Compulsive Disorders Scale also significantly increased from 19.72 to 26.6. Working in the COVID-19 section roughly doubled the depression score from 7.49 to 14.71 with a p-value of <0.0001. It is concluded that the health care workers in the COVID-19 section had significantly increased obsessive-compulsive disorders, depression, and anxiety as compared to the control group. Both groups showed no significant difference in terms of age, sex, education, marital status, and ERE. The psychological impact of the COVID-19 pandemic among the frontline HCWs should be understood well. The important public health measure is to protectthem to overcome this global pandemic.
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    Laktoperoksidaz Enziminin Sülfamat Türevleri Bileşikleri Üzerineİnhibisyon Profili
    (2020) Usanmaz, Hande; Atmaca, Ufuk
    Sülfamat iskeleti içeren birçok doğal ürün ve ilaç etken maddelerinde bulunmaktadırlar. Son zamanlarda, sülfamatlar bileşiklerininbulundurdukları fonksiyonel gruplarından dolayı malzeme bilimcisi ve farmakolog tarafından daha fazla ilgi görmektedirler.Peroksidazlar (POD), metabolik fonksiyonlarından dolayı gıda ve ilaç endüstrisinde enzimatik reaksiyonlarda ve klinik teşhislerdeönemli kullanım alanında yer alırlar. Laktoperoksidaz (LPO, EC 1.11.1.7 ) peroksidaz ailesinin bir üyesidir. Bu enzim sütte, tükürükteve gözyaşında bulunan bir oksidoredüktaz olup, patojen mikroorganizmalara karşı yeni doğanların bağırsak sistemlerini ve meme bezlerini korumada önemli bir role sahip olmaktadır. Memeli sütlerinden edilen LPO enzimi, bakterilerin büyümesinin baskılanmasındave bakteri inhibisyonunun desteklenmesinde oldukça önemlidir. Sığır LPO’sunun bakteriyal büyümeyi inhibe etmesi, H2O2 vetiyosiyanat içeren peroksidaz sistemine atfedilir. Bu sistemin antimikrobiyal etkisi sütte doğal olarak oluşmuştur. LPO enzimi üzerineyapılan antibakteriyal çalışmalarda LPO-tiyosiyanat ve peroksit sisteminin patajonik bakterilerde önemli derecede inhibisyona sebepolduğu tespit edilmiştir. LPO’nun birçok uygulama alanı vardır. Peroksidazlar hem gıdalarda hem de farmakolojik uygulamalardakoruyucu olarak kullanılır ve süt işleme tesislerinde nakil esnasında sütün muhafazası amacıyla süt endüstrisinde kullanılmaktadır. Buçalışmanın amacı, LPO enzimi üzerine Metil benzoilsülfamat, Metil (2-bromobenzoil) sülfamat, Metil (3-fenilpropanoil) sülfamat,Metil (1-naphthoil) sülfamat, Metil (2-metilbenzoil) sülfamat, Metil (2-iyodobenzoil) sülfamat, Metil (2-fenilbutanoil) sülfamat, Metil(4-isopropilbenzoil) sülfamat, Metil (4-metoksibenzoil) sülfamat ve Metil (isoquinoline-1-karbonil) sülfamat bileşilklerinin in vitroetkilerini belirlemektir. Bu sülfamat türevi bileşiklerinin LPO enzimi üzerindeki inhibisyon etkisini belirlemek için, enzim aktiviteleriölçülerek her bir inhibitör için Lineweaver-Burk grafikleri çizildi; Ki sabiti ve inhibisyon tipleri bu çizilen grafiklerden bulnunarakhesaplanıldı. Ki değerleri sırasıyla Metil benzoilsülfamat 0,70 μM, Metil (2-bromobenzoil) sülfamat 0,025 μM, Metil (3-fenilpropanoil) sülfamat 0,018 μM, Metil (1-naphthoil) sülfamat 0,047 μM, Metil (2-metilbenzoil) sülfamat 0,043 μM, Metil (2-iyodobenzoil) sülfamat0,19 μM, Metil (2-fenilbutanoil) sülfamat 0,39 μM, Metil (4-isopropilbenzoil) sülfamat 0,42 μM, Metil (4-metoksibenzoil) sülfamat0,078 μM, Metil (isoquinoline-1-karbonil) sülfamat 0,075 μM olarak belirlendi. Metil (4-isopropilbenzoil)sülfamat bileşiği yarışmasızinhibisyon ve diğer maddeler yarışmalı inhibisyon gösterdiği kaydedildi. Metil (2-metilbenzoil)sülfamat bileşiği ise en etkili inhibitörözelliğini yarışmalı inhibisyon tipi LPO enzimi üzerine 0.018 ± 0.024 μM Ki değeri ile göstermiştir.
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    Molecular docking and inhibition profiles of some antibiotics on lactoperoxidase enzyme purified from bovine milk
    (Taylor & Francis Inc, 2022) Kalin, Ramazan; Koksal, Zeynep; Bayrak, Songul; Gerni, Serpil; Ozyurek, Isil Nihan; Usanmaz, Hande; Karaman, Muhammet
    Antibiotics are generally used for human and veterinary applications to preserve and to control microbial diseases. Milk has a biologically significant enzyme known as lactoperoxidase (LPO) that is a member of peroxidase family. In metabolism, LPO has ability to catalyze the transformation of thiocyanate (SCN-) to hypothiocyanite (OSCN-) that is an antibacterial agent and the reaction occurs with hydrogen peroxide. In this work, LPO inhibition effects of some antibiotics including cefazolin, oxytetracycline, flunixin meglumine, cefuroxime, tylosin, vancomycin, chloramphenicol and lincomycin were tested. Among the antibiotics cefazolin was indicated the strongest inhibitory efficacy. The half maximal inhibitory concentration (IC50) and the inhibition constant (K-i) values of cefazolin were found as 8.19 and 34.66 mu M, respectively. It was shown competitive inhibition. 5-Methyl-1,3,4-thiadiazol-2-yl moiety activity plays a key role in the inhibition mechanism of cefazolin. Communicated by Ramaswamy H. Sarma
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    Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors
    (Mdpi, 2017) Koksal, Zeynep; Kalin, Ramazan; Camadan, Yasemin; Usanmaz, Hande; Almaz, Zuleyha; Gulcin, Ilhami; Gokcen, Taner
    Secondary sulfonamides (4a-8h) incorporating acetoxybenzamide, triacetoxybenzamide, hydroxybenzamide, and trihydroxybenzamide and possessing thiazole, pyrimidine, pyridine, isoxazole and thiadiazole groups were synthesized. Lactoperoxidase (LPO, E.C.1.11.1.7), as a natural antibacterial agent, is a peroxidase enzyme secreted from salivary, mammary, and other mucosal glands. In the present study, the in vitro inhibitory effects of some secondary sulfonamide derivatives (4a-8h) were examined against LPO. The obtained results reveal that secondary sulfonamide derivatives (4a-8h) are effective LPO inhibitors. The K-i values of secondary sulfonamide derivatives (4a-8h) were found in the range of 1.096 x 10(-3) to 1203.83 mu M against LPO. However, the most effective inhibition was found for N-(sulfathiazole)-3,4,5-triacetoxybenzamide (6a), with K-i values of 1.096 x 10(-3) +/- 0.471 x 10(-3) mu M as non-competitive inhibition.
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    Synthesis, characterization, biological activity and molecular docking studies of novel schiff bases derived from thiosemicarbazide: Biochemical and computational approach
    (Elsevier, 2021) Tokali, Feyzi Sinan; Taslimi, Parham; Usanmaz, Hande; Karaman, Muhammet; Sendil, Kivilcim
    In this study, eight new Schiff base derivatives (2a-h) were synthesized and their inhibition activities against Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), alpha-Glucosidase and Lactoperoxidase (LPO) were investigated. Structures of the synthesized compounds were characterized using H-1 and C-13 nuclear magnetic resonance (NMR), infrared spectroscopy (IR), and high-resolution mass spectrometry (HRMS) spectroscopic methods. AChE was inhibited by these novel Schiff bases (2a-h) in low nanomolar levels, the K-i of which differed between 592.66 +/- 57.04 and 810.78 +/- 84.06 nM. Against BChE, the novel compounds demonstrated Kis varying from 358.31 +/- 37.88 to 577.24 +/- 59.91 nM. Also, these novel Schiff bases effectively inhibited alpha-glucosidase, with K-i values in the range of 1.56 +/- 0.32 to 14.78 +/- 2.57 nM. For LPO, K-i values were in the range of 3.96 +/- 0.37 to 12.75 +/- 0.06 nM. For alpha-glucosidase, the most effective molecules were 2b and 2 g with K-i values of 1.56 +/- 0.32 and 14.78 +/- 2.57 nM, respectively. Molecular docking results showed that the compounds have binding affinity with -5.559,-9.698, -7.606, and -6.971 kcal/mol against LPO, AChE, BChE, and alpha-glucosidase enzyme, respectively. It has been observed that the furan and thiosemicarbazone moieties play an important role in the inhibition of these enzymes. (C) 2020 Elsevier B.V. All rights reserved.