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Search results for: Α-AMYLASE INHIBITION
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Carboxylic acids as efficient corrosion inhibitors of aluminium alloys in alkaline media
PublicationThe efficiency of AA5754 aluminium alloy corrosion inhibition achieved with maleic, malic, succinic, tartaric, citric, tricarballylic acids and serine in alkaline environment (pH 11) was examined. Selected corrosion inhibitors are characterized by different numbers and distribution of carbonyl and hydroxyl groups within their molecules. We have proposed and verified a novel approach for determining the adsorption isotherms based...
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Positive solutions to second-order differential equations with dependence on the first-order derivative and nonlocal boundary conditions
PublicationIn this paper, we consider the existence of positive solutions for second-order differential equations with deviating arguments and nonlocal boundary conditions. By the fixed point theorem due to Avery and Peterson, we provide sufficient conditions under which such boundary value problems have at least three positive solutions. We discuss our problem both for delayed and advanced arguments α and also in the case when α(t)=t, t∈[0,1]....
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Salicylaldimine-based receptor as a material for iron(III) selective optical sensing
Publicationα,α-Bis(salicylimino)-m-xylene (L) was prepared using both conventional and microwave-assisted procedure. The compound exhibits ability to colorimetric recognition of iron(III) ions in aqueous environment, what is shown by significant color change from yellow to purple. In DMSO : water (9:1 v/v) solvent system receptor creates with iron(III) cations complexes of 2:1 stoichiometry (L:Fe3+) with stability constant (log K) 7.54±0.21....
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Experimental and Quantum Chemical Evaluation of 8-Hydroxyquinoline as a Corrosion Inhibitor for Copper in 0.1 M HCl
PublicationThe corrosion inhibition properties of 8-hydroxyquinoline (8-HQ) in 0.1 M HCl for copper have been investigated by using experimental (electrochemical impedance spectroscopy (EIS), dynamic electrochemical impedance spectroscopy (DEIS), and potentiodynamic polarization) and theoretical methods complemented by surface morphological examination with the aid of scanning electron microscopy (SEM) and electron dispersive X-ray spectroscopy...
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Effect of microwave and convection heating on selected nutrients of human milk
PublicationThe aim of this study was to determine the influence of the microwave heating method (MWH) on selected determinants of the nutritional value of human milk (HM) and compare to the effect exerted by the standard convection heating (CH) method, including holder pasteurization (HoP). It was showed that using MWH under conditions assumed to ensure microbiological safety, changes in the level of the nutrients were not observed. In these...
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Application of the 2-deoxyglucose scaffold as a new chiral probe for elucidation of the absolute configuration of secondary alcohols
PublicationHerein, we present the application of 2-deoxy-D-glucose derivatives as chiral probes for elucidation of the absolute configuration of chiral secondary alcohols. The probes are attached to the studied molecules via glycosylation reaction and the resulting products are examined by a set of standard 2D NMR experiments. The absolute configuration of an oxymethine carbon atom binding the probe is established on a basis of a set of diagnostic...
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Improved Performance of 1-Ethyl-3-Methylimidazolium Tetrafluoroborate at Steel/HCl Interface by Iodide Ions
PublicationThe corrosion and corrosion inhibition of St37 steel in 0.1 M HCl solution by 1-ethyl-3-methylimidazolium tetrafluoroborate (EMITFB) and the effect of addition of KI on the inhibitive performance of EMITFB have been examined by electrochemical [electrochemical impedance spectroscopy, potentiodynamic polarization, and dynamic electrochemical impedance spectroscopy (DEIS)] and surface examination [scanning electron microscope (SEM)...
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Relationships between concentrations of selected organohalogen contaminants and thyroid hormones and vitamins A, E and D in Faroese pilot whales
PublicationPilot whales (Globicephala melas) from the Faroe Islands, North-East Atlantic, have high body concentrations of organohalogenated compounds (OHCs), such as polychlorinated biphenyls (PCBs), organochlorinated pesticides (OCPs) and brominated flame retardants (BFRs). The aim of the present study was to examine if and to what extent blood plasma and liver concentrations of several groups of these OHCs are related to concentrations...
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Bioactivities of Phenolic Compounds from Kiwifruit and Persimmon
PublicationFruit used in the common human diet in general, and kiwifruit and persimmon particularly, displays health properties in the prevention of heart disease. This study describes a combination of bioactivity, multivariate data analyses and fluorescence measurements for the differentiating of kiwifruit and persimmon, their quenching and antioxidant properties. The metabolic differences are shown, as well in the results of bioactivities...
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Unassisted formation of hemiaminal ether from 4-aminopyridine and o-vanillin - experimental and theoretical study
PublicationThe reactions between o-vanillin and three isomeric aminopyridines lead to imines of diverse spatial conformation and reactivity. The direct products of these simple reactions carried out in methanol are either imine compounds formed in the reactions of 2- amino- and 3-aminopyridine with o-vanillin or the α-aminoether formed in the reaction of o-vanillin with 4-aminopyridine. The Schiff-type derivative of 4-aminopyridine and o-vanillin,...
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Phenotypic consequences of LYS4 gene disruption in Candida albicans
PublicationA BLAST search of the Candida Genome Database with the Saccharomyces cerevisiae LYS4 sequence known to encode homoaconitase (HA) revealed ORFs 19.3846 and 19.11327. Both alleles of the LYS4 gene were sequentially disrupted in Candida albicans BWP17 cells using PCR-based methodology. The null lys4Δ mutant exhibited lysine auxotrophy in minimal medium but was able to grow in the presence of L-Lys and α-aminoadipate, an intermediate...
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Residual MobileNets
PublicationAs modern convolutional neural networks become increasingly deeper, they also become slower and require high computational resources beyond the capabilities of many mobile and embedded platforms. To address this challenge, much of the recent research has focused on reducing the model size and computational complexity. In this paper, we propose a novel residual depth-separable convolution block, which is an improvement of the basic...
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The Effect of Hyperbaric Storage on the Nutritional Value and Retention of Certain Bioactive Proteins in Human Milk
PublicationHuman milk (HM) contains the essential macronutrients and bioactive compounds necessary for the normal growth and development of newborns. The milk collected by human milk banks is stored frozen and pasteurized, reducing its nutritional and biological value. The purpose of this study was to determine the effect of hyperbaric storage at subzero temperatures (HS-ST) on the macronutrients and bioactive proteins in HM. As control samples,...
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The effect of surfactants mixtures composition on wetting of different solid materials
PublicationThe wetting properties of surfactants mixtures were investigated. Three types of compounds were used: nonionic gemini α, α'-[2,4,7,9-tetramethyl-5-decyne-4,7-diyl]bis[ω-hydroxyl-olioxyethylene] (S-10), anionic sodium dodecyl sulphates (SDS) and cationic dodecyl trimethyl ammonium bromide (DTAB). The materials used in wetting experiments were steel and methyl polymethacrylate. These materials differ...
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Formation of carbon monoxide by radiative association: a quantum dynamical study
PublicationRate coefficients for the formation of carbon monoxide (CO) by radiative association of carbon and oxygen atoms are computed using quantum dynamical simulations. At temperatures above 10 K CO radiative association is dominated by C(3P) and O(3P) approaching on the A1Π potential energy curve. The rate coefficient is estimated as k=A(T/300 K)αexp−β/T with A= 1.39 × 10−18 cm3 s−1, α=−0.016 and β= 92.2 for temperatures between 6 and...
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The carbohydrate glycosylphosphatidylinositol anchor chain under mechanical stress
PublicationCarbohydrates have quite complicated micro heterogenic structure which may undergo different structural transitions. Due to their extreme flexibility it is very difficult to investigate such structural changes experimentally. In these studies we want to predict what structural and conformational changes are possible in the carbohydrate
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ANALYSIS OF THE p53 PROTEIN GENE EXPRESSION MODEL
PublicationWe study the asymptotic behaviour of the solutions of the p53-Mdm2 model proposed by Monk (2003). The p53 gene is crucial for cellular inhibition of the angiogenesis process, while Mdm2 is a negative regulator of the p53 tumor-suppressor. We investigate the stability of the positive steady state and perform some numerical experiments.
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Towards β-selectivity in functional estrogen receptor antagonists
PublicationBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublicationResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Chemometric Evaluation of WWTPs’ Wastewaters and Receiving Surface Waters in Bulgaria
PublicationWastewater treatment plant (WWTP) installations are designed and operated to reduce the quantity of pollutants emitted to surface waters receiving treated wastewaters. In this work, we used classical instrumental studies (to determine chemicals and parameters under obligations put with Directive 91/271/EEC), ecotoxicological tools (Sinapis alba root growth inhibition (SA-RG) and Heterocypris incongruens mortality (MORT) and growth...
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The noise macromodel of an optocoupler including 1/(f^alfa) noise source
PublicationThe course of design of an optocoupler's PSpice macromodel including noise sources is described. The PSpice macromodel is proposed for the low frequency range. The PSpice model of a MOSFET transistor was applied as the noise source type 1/(f^alfa) in an optocoupler PSpice macromodel. In the enhanced macromodel the value of an exponent α can be changed in the range of 0.8 - 1.25.
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublicationWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
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In vitro and in silico assessment of anti-inflammatory activity of cocoa powders
PublicationPlants are considered the major sources of biologically active compounds, which provide unlimited opportunities for their use either as medical treatments or as novel drug formulations. Cocoa powder is frequently used in nutrition and is known to have many benefits thanks to its wide range of biological activities. The presented study was focused on th evaluation of the anti-inflammatory potential of extracts obtained from cocoa...
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Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublicationOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
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Imidazoacridinone antitumor agent C-1311 as a selective mechanism- based inactivator of human cytochrome P450 1A2 and 3A4 isoenzymes.
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311), a promising antitumor agent that is also active against autoimmune diseases, was determined to be a selective inhibitor of the cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1311 might modulate the effectiveness of other drugs used in multidrug therapy. The present work aimed to identify the mechanism of the observed C-1311-mediated inactivation of CYP1A2...
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Positive solutions to Sturm–Liouville problems with non-local boundary conditions
PublicationIn this paper, the existence of at least three non-negative solutions to non-local boundary-value problems for second-order differential equations with deviating arguments α and ζ is investigated. Sufficient conditions, which guarantee the existence of positive solutions, are obtained using the Avery–Peterson theorem. We discuss our problem for both advanced and delayed arguments. An example is added to illustrate the results.
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Synthesis and crystal structure of ferrocenyl benzothiazole derivatives
PublicationNovel ferrocenyl-containing benzothiazole derivatives were synthesised in moderate yields by one-pot α-amidoalkylation of ferrocene. The reaction conditions were critically evaluated and the crystal structure of one of the amidoalkylated ferrocenes was resolved. Oxidation of the obtained compounds led to known fully aromatic 2-ferrocenylbenzothiazole in 81 % yield, which represents a convenient alternative to earlier methods utilizing...
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Synergistic effects in micellization and surface tension reduction in nonionic gemini S-10 and cationic RTAB surfactants mixtures
PublicationMixtures of nonionic gemini surfactant S-10 (α,α′-[2,4,7,9-tetrametyl-5-decyne-4,7-diyl]bis[ω-hydroxy -polioxyetylene] with cationic alkyltrimethylammonium bromides of different alkyl chain length (RTAB) were investigated. Basing on surface tension measurements the cmc values and other adsorption parameters were found. The Clint, Rubing’s and Rosen theories were applied for evaluation of the synergistic effects in mixed films and...
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The effect of alkyl chain length on synergistic effects in micellization and surface tension reduction in nonionic gemini (S-10) and anionic surfactants mixtures
PublicationMixtures of nonionic gemini surfactant S-10 ( α, α'-[2,4,7,9-tetrametyl-5-decyne-4,7-diyl]bis[ω-hydroxy -polioxyetylene] with anionic SRS (sodium alkylsulfates) and SRSO3 (sodium alkylsulfonates) of different alkyl chain length (from 10 to 14 carbon atoms) were investigated. Surface tension measurements were used to find the cmc values and other adsorption parameters. The Clint, Rubingh’s and Rosen theories were applied for evaluation...
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Corrosion mechanisms in columns for atmospheric distillation of crude oil
PublicationThe paper presents the most common corrosion processes occurring in the columns for atmospheric distillation of crude oil. It describes the mechanisms leading to formation of the chemical compounds, which contribute to corrosion phenomena. The main technological factors influencing corrosion processes have been indicated. The paper also presents the interactions between particular corrosion mechanisms resulting in acceleration...
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Oxidation step in the preparation of benzocamalexin: The crystallographic evidence
PublicationThe study of oxidation step in the preparation of benzocamalexin by the α-amidoalkylation–oxidation sequence revealed the formation of perchloro-1,2-phenylene dibenzoate as the product of transformation of tetrachloro- 1,2-benzoquinone applied as the oxidant. The structures of benzocamalexin and perchloro-1,2-phenylene dibenzoate were confirmed by X-ray diffraction analysis. The extraction step in the final isolation of benzocamalexin...
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Screening evaluation of the quality of commercially available cigars, cigarillos, and bidis based on emission levels of selected terpenes and terpenoids
PublicationThe aim of the research was to verify the use of the solvent-free, non-destructive and easy to operate analytical method to study and compare the emissions of 16 representatives of terpenes and terpenoids from commercially available cigars, cigarillos and bidis − a potential screening analysis for the quality of combustible tobacco products. To assess the amount of organic compounds emitted to the gaseous phase from investigated...
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Two small RNAs conserved in Enterobacteriaceae provide intrinsic resistance to antibiotics targeting the cell wall biosynthesis enzyme glucosamine-6-phosphate synthase
PublicationFormation of glucosamine-6-phosphate GlcN6P) by enzyme GlcN6P synthase (GlmS) represents the first step in bacterial cell envelope synthesis. In Escherichia coli, expression of glmS is controlled by small RNAs (sRNAs) GlmY and GlmZ. GlmZ activates the glmS mRNA by base-pairing. When not required, GlmZ is bound by adapter protein RapZ and recruited to cleavage by RNase E inactivating the sRNA. The homologous sRNA GlmY activates...
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Analytical Steady-State Model of the Pipeline Flow Process
PublicationThe paper addresses the issue of modeling the flow process in transmission pipelines. A base model used for numerical simulation is introduced. Under certain assumptions concerning steady state analysis, the differential equations describing the process are solved analytically for two cases: zero and nonzero inclination angle α. These equations describe a constant flow rate and a corresponding distribution of the pressure along...
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Evaluation of Terpene Decomposition in Kaffir Lime Juice during Storage Using Gas Chromatography–Mass Spectrometry and Proton Transfer Reaction–Mass Spectrometry
PublicationKaffir lime juice, often treated as production waste, can be a good source of terpenes. These compounds undergo various decomposition processes under the influence of external factors, especially during transportation and storage. In this paper, it was possible to monitor changes in the terpene profile of kaffir lime juice under different storage conditions, namely, 4 ◦C, 20 ◦C, and 35 ◦C. The identification of key decomposition...
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Galvanostatic impedance measurements for the efficient adsorption isotherm construction in corrosion inhibitor studies
PublicationWe present an approach towards an accurate and time-efficient adsorption isotherm determination to evaluate the corrosion inhibitor interaction in electrolytic environments. The approach is based on dynamic impedance spectroscopy measurements in galvanostatic mode (g-DEIS). The studied corrosion inhibitor is continuously injected between the secondary cell and the corrosion cell. The efficiency corresponding to instantaneous inhibitor...
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A comprehensive evaluation of mimosa extract as a corrosion inhibitor on AA6060 alloy in acid rain solution: part I. Electrochemical AC methods
PublicationThe inhibition effect of mimosa extract on the corrosion of AA6060 aluminum alloy in acid rain solution was investigated by electrochemical impedance spectroscopy and dynamic electrochemical impedance spectroscopy (DEIS). All the studied electrochemical parameters showed good corrosion inhibitive characteristics with respect to the aluminum alloy in the tested solution. Inhibitor efficiency increased with the concentration and...
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Spin and Orbital Effects on Asymmetric Exchange Interaction in Polar Magnets: M(IO3)2 (M = Cu and Mn)
PublicationMagnetic polar materials feature an astonishing range of physical properties, such as magnetoelectric coupling, chiral spin textures, and related new spin topology physics. This is primarily attributable to their lack of space inversion symmetry in conjunction with unpaired electrons, potentially facilitating an asymmetric Dzyaloshinskii–Moriya (DM) exchange interaction supported by spin–orbital and electron–lattice coupling. However,...
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Bacterial community succession in an Arctic lake–stream system (Brattegg Valley, SW Spitsbergen)
PublicationThe factors affecting prokaryotic and virus structure dynamics and bacterial commu-nity composition (BCC) in aquatic habitats along a ca. 1500 m of the Brattegg Valley lake–stream system (SW Spitsbergen) composed of three postglacial lakes created by Brattegg Glacier meltwater were examined. A high number of small-volume prokaryotic cells were found in the recently-formed, deep, upper,...
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Advanced Scalar-valued Intensity Measures for Residual Drift Prediction of SMRFs with Fluid Viscous Dampers
PublicationMaximum Residual Inter-story Drift Ratio (RIDRmax) plays an important role to specify the state of a structure after severe earthquake and the possibility of repairing the structure. Therefore, it is necessary to predict the RIDRmax of Steel Moment-Resisting Frames (SMRFs) with high reliability by employing powerful Intensity Measures (IMs). This study investigates the efficiency and sufficiency of scalar-valued IMs for predicting...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublicationDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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Sonocatalytic degradation of tetracycline antibiotic using zinc oxide nanostructures loaded on nano-cellulose from waste straw as nanosonocatalyst
PublicationThe aim of the present investigation was the combination of ZnO nanostructures with nano-cellulose (NC) for the efficient degradation of tetracycline (TC) antibiotic under ultrasonic irradiation. The removal efficiency of 12.8% was obtained by the sole use of ultrasound (US), while the removal efficiency increased up to 70% by the US/ZnO treatment process. Due to the integration of ZnO nanostructures with NC, the removal efficiency...
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The properties of reduced Ge-Sb-O glasses for thermoelectric devices
PublicationThe structural and electrical properties of germanium-antimonate glasses after heat treatment in hydrogen have been determined. In the case of 50GeO2-50Sb2O3 glass reduced at 340°C even for less than 1 hour a continuous layer of antimony granules is formed and its electrical properties determine the surface conductivity of the reduced sample. The bulk electrical conductivity at 100°C of this sample was determined as 1000 Scm-1...
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Wpływ obecności chlorku trimetylosililu na reakcję syntezy niesymetrycznych malonoamidów
PublicationW trakcie badań nad syntezą niesymetrycznych malonoamidów, optymalizowaliśmy metodę zaproponowaną przez Pak1. Związki te otrzymywaliśmy używając jako substratów 5-(α-amino-α'-hydroksy)-metyleno-pochodnych kwasu Meldruma oraz szeregu różnych amin. W trakcie badań okazało się, że przeprowadzenie syntezy jest możliwe, jeśli jako substrat zastosuje się słabą zasadę. Przy użyciu mocniejszych zasad wydajności reakcji były niskie. Postanowiliśmy...
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Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Publication5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1 receptor (CB1). Here, we reveal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critical chain length at the C3-position, an electron withdrawing group at the C5-position, the length of the linker between the amide bond and the phenyl ring...
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Ground Tire Rubber Modified by Elastomers via Low-Temperature Extrusion Process: Physico-Mechanical Properties and Volatile Organic Emission Assessment
PublicationIn this paper, low-temperature extrusion of ground tire rubber was performed as a proecological waste tires recycling method. During this process, ground tire rubber was modified with constant content of dicumyl peroxide and a variable amount of elastomer (in the range: 2.5–15 phr). During the studies, three types of elastomers were used: styrene-butadiene rubber, styreneethylene/butylene-styrene grafted with maleic anhydride and...
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c-Myc Protein Level Affected by Unsymmetrical Bisacridines Influences Apoptosis and Senescence Induced in HCT116 Colorectal and H460 Lung Cancer Cells
PublicationUnsymmetrical bisacridines (UAs) are highly active antitumor compounds. They contain in their structure the drugs previously synthesized in our Department: C-1311 and C-1748. UAs exhibit different properties than their monomer components. They do not intercalate to dsDNA but stabilize the G-quadruplex structures, particularly those of the MYC and KRAS genes. Since MYC and KRAS are often mutated and constitutively expressed in cancer...
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New clicked full agonists of the estrogen receptor β
PublicationA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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Multiple Solutions to Third-Order Differential Equations with Derivative Dependence and Deviating Arguments
PublicationIn this paper, we give some new results for multiplicity of positive (nonnegative) solutions for third-order differential equations with derivative dependence, deviating arguments and Stieltjes integral boundary conditions. We discuss our problem with advanced argument α and arbitrary β ∈ C([0,1],[0,1]), see problem (2). It means that argument β can change the character on [0,1], so β can be delayed in some set J ⊂ [0,1] and advanced...