Sürdürülebilir Kalkınma Amaçları
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- MakaleAçık Erişim2023MW Assisted Synthesis of New 4,6-diaryl-3,4-Didhydropyrimidines-2(1H)-thione Derivatives: Tyrosinase Inhibition, Antioxidant, and Molecular Docking Studies
Yucel, Tayyibe Beyza; Fandaklı, Seda; Yayli, Nurettin; Barut, Burak; Uzuner, Ugur; Öztürk, Elif; Ates, Fatih
A number of new methoxy-substituted 4,6-diaryl-3,4-dihydropyrimidine-2(1H)-thiones (DH-Pyr-S, 17-28) were designed and synthesized by the reaction of methoxy-substituted chalcones (1–14) with thiourea using solid-phase microwave method (MW) in view of the structural requirements as suggested in the pharmacophore model for tyrosinase inhibition (TI). Synthesized compounds were assessed for their in vitro TI potential and compounds 16, 17, and 21 exhibited notable tyrosinase inhibitory properties at the concentrations of 31.86 ± 2.45 µM, 44.58 ± 0.46 µM, and 48.47 ± 0.66 µM, respectively. Compounds (16, 17, and 21) were exhibited experimentally more potent TI than the standard used in terms of the IC50 value (Kojic acid, 55.38 ± 2.30 µM; p<0.0001). Additionally, DPPH activity of 15-28 were evaluated and compound 17 showed the moderate DPPH activity (45.64 ± 0.34%). Binding affinities of synthesized molecules to the tyrosinase catalytic core were further investigated through in silico molecular docking studies using AutoDock Vina (version 1.2.5), discovery studio accelyrs (BIOVIA, Dassault Systèmes) and predicting small-molecule pharmacokinetic properties using graph-based signatures (pkCSM) programs were used for ADMET calculations. Among synthesized compounds 15, 21, and 24 revealed high binding affinity to tyrosinase active site with lowest binding free energy (ΔG) values of -7.9 kcal/mol, thereby outperformed kojic acid affinity. In conclusion most modeling results were in agreement with their experimental data, suggesting the TI potential of lead compounds.
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İncele - MakaleAçık Erişim2022Farklı substratlar, Pleurotus ostreatus'un antioksidan özelliklerini ve antimikrobiyal aktivitesini etkiler mi?
Karaoğlu, Şengül Alpay; Peksen, Aysun; Can, Zehra; Bozdeveci, Arif; Avcı, Sibel
Öz: Bu çalışmanın amacı, yetiştirme ortamının Pleurotus ostreatus (Jacq. ex Fr.) P. Kumm.'un antioksidan özellikleri ve antimikrobiyal aktiviteleri üzerindeki etkisini belirlemektir. Çalışmada beş adet talaş (%80) ve atık (%20 Çay Atığı veya Buğday Kepeği) ile farklı oranlarda (%80 Talaş + %20 TW, %80 Talaş + 20% GW) yetiştirme substratları hazırlanmıştır. Toplam 19 farklı ortamda yetiştirilen P. ostreatus'tan elde edilen metanol ekstraktların, mikroorganizmalara karşı antimikrobiyal aktiviteleri agar kuyu difüzyon tekniği ile test edildi. Toplam fenolik içerik, Folin-Ciocalteau prosedürü kullanılarak ölçülmüştür. Antioksidan kapasitesi, DPPH'nin ferrik indirgeyici antioksidan gücü (FRAP) ve serbest radikal süpürücü aktivitesi kullanılarak belirlendi.. 80QS+20TW substratından elde edilen mantarların metanol ekstraktının bu çalışmada incelenen tüm mikrooganizmalara karşı en etkili ekstrakt olduğu belirlendi. Farklı substratlar üzerinde yetiştirilen mantar ekstraktlarının antioksidan içerikleri arasında önemli farklılıklar (P
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İncele - Derleme MakaleAçık Erişim2018Mutual Interaction Between Phenolic Compounds and Intestinal Bacteria
Erdogan, Ummugulsum; Talay, Rabia
The intestinal bacterial populations constitute the anaerobic bacteria Clostridium, Bifidobacterium, Peptococcus, Eubacterium, Fusobacterium, Peptostreptococcus, Bacteroides, E. coli, Lactobacillus, Klebsiella, Staphylococcus, Streptococcus and Bacillus species. It is known that the bacteria that make up this population are affecting human health. Therefore, any change in the population causes various diseases (obesity, diabetes, hypertension etc.). Prebiotics are needed to restore this disrupted balance and to protect it from diseases. A diet made from natural foods such as fruit and vegetables plays an important role in the regulation of intestinal microbiota. Many fruit and vegetables rich in phenolic components such as corn, rosehip, trabzon, tomato, carrot, soybean, walnut, grapefruit are important in this sense. The purpose of this compilation is; phenolic compounds, general microbiota and intestinal microbiota and explain the effect of intestinal microbiota on phenolic compounds and phenolic compounds on intestinal microbiota.
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