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Wyniki wyszukiwania dla: mechanism-based inhibition
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublikacjaHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Hyperbaric Storage at Subzero Temperature – the Effect on the Shelf-Life and Selected Quality Characteristics of Raw Pork Sausages
PublikacjaThe aim of this study was to determine the microbiological stability and changes occurring in selected physicochemical properties of raw pork sausages during hyperbaric storage at subzero temperature (HS-ST). It was shown that storage at moderate pressures (up to 111 MPa) led to a reduction in microbial populations. After 21 days of storage under these conditions, no microorganisms were detected in the samples. Additionally, the...
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Novel Cast Polyurethanes Obtained by Using Reactive Phosphorus-Containing Polyol: Synthesis, Thermal Analysis and Combustion Behaviors
PublikacjaPhosphorus-containing polyol applications in polyurethane synthesis can prevent volatilization of flame retardants and their migration on the surface of a material. In this work, novel cast polyurethanes were prepared by a one-step method with the use of different amounts of phosphorus-containing polyol, 4,4′–diphenylmethane diisocyanate and 1,4-butanediol. The chemical structure, thermal, physicochemical and mechanical properties...
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublikacjaNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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The excitation controller with gain scheduling mechanism for synchronous generator control
PublikacjaThe power systems, including the synchronous generators and power systems networks, are complex nonlinear systems with configuration and parameters which change through time. That leads to electromechanical oscillations occurring in that system. Thus synchronous generator excitation controller must be capable of providing appropriate stabilization signal over broad range of operating conditions and disturbances. In this paper,...
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On the durability of the hydraulic satellite motor working mechanism in overload condition
PublikacjaThe paper presents the newest construction of the hydraulic satellite pump/motor. In this study, the fracture of the hydraulic satellite motor working mechanism is investigated. Factors influencing the durability of satellite working mechanism have been described. The durability of the hydraulic satellite motor working mechanism at a load, corresponding to a pressure of 15 MPa supplied with refined rapeseed oil is very low. Analyses...
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Selectivity Tuning by Natural Deep Eutectic Solvents (NADESs) for Extraction of Bioactive Compounds from Cytinus hypocistis—Studies of Antioxidative, Enzyme-Inhibitive Properties and LC-MS Profiles
PublikacjaIn the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. The extracts were found to possess total phenolic and total flavonoid contents in the ranges of 26.47–186.13...
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Inhibition of Polymer Photodegradation by Incorporation of Coffee Silverskin
PublikacjaOver the last years, the trend associated with the incorporation of materials from renewable resources into polymer technology is getting significantly more vital. Researchers are trying to transfer the properties of natural raw materials into the polymer world. Therefore, different natural materials are more often investigated as potential additives for polymers. Such an effect is noted for the coffee industry by-products, such...
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Antibacterial evaluation of bioactive modifiers of bone cements: antibiotics, nanometals and chitosan
PublikacjaModern biomaterials in addition to their basic tasks, can serve as carriers of active substance. The release of a bioactive particles allows to locally fight infection or its prevent it. Bone cements additionally to their basic applications in orthopedic surgery can also serve to deliver locally active substances. Currently, only antibiotics are routinely used as modifiers for bone cements. Bioactive bone cements constitute...
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The Caucasian flora: a still-to-be-discovered rich source of antioxidants
PublikacjaCellular redox homeostasis is a state of balance between the formation of Usually Reactive Oxygen and / or Nitrogen Species (ROS/RNS), endogenous antioxidant defence systems, and exogenous dietary antioxidants. The disturbance of redox homeostasis, by the overproduction of endogenous ROS/RNS, may increase the risk of development of so-called civilisation diseases. The solution seems to be either the increased production of endogenous...
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Characterization of PVDF/Graphene Nanocomposite Membranes for Water Desalination with Enhanced Antifungal Activity
PublikacjaSeawater desalination is a worldwide concern for the sustainable production of drinking water. In this regard, membrane distillation (MD) has shown the potential for effective brine treatment. However, the lack of appropriate MD membranes limits its industrial expansion since they experience fouling and wetting issues. Therefore, hydrophobic membranes are promising candidates to successfully deal with such phenomena that are typical...
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RAAS inhibition – a practice of medical progress
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Glucosamine-6-phosphate synthase with an oligoHis insert
PublikacjaGlucosamine-6-phosphate (GlcN-6-P) synthase known also as L-Glutamine: D-fructose-6-phosphate aminotransferase (EC 2.6.1.16), catalyzes the first committed step in the amino sugar biosynthetic pathway in prokaryotic and eukaryotic organisms. The final product of this pathway is an activated precursor of numerous macromolecules containing amino sugars, including chitin and mannproteins in fungi, peptydoglican and lipopolysaccharides...
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Viscous versus electromagnetic damping – amplification in a neighbourhood of a mechanism singular position
PublikacjaIn the paper, damping of vibrations are considered and compared in a mechanical and in a electromechanical system. In the system, a continuous beam is considered as the main vibrating element. The compared dissipations methods are based on: viscous dampers and DC generators. To increase the possible damping effectiveness, velocity amplification is proposed, i.e., a mechanism is introduced between the beam and the damping element....
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A simple model of the trap-assisted recombination with the excitonic Auger mechanism
PublikacjaWe present a simple model of the trap-assisted recombination combined with the excitonic Auger mechanism. It has been shown that only six independent transitions of electrons and holes should be taken into account to describe a combination of the Shockley–Read–Hall (SRH) recombination with this excitonic process. This is in opposition to a well-known model of the SRH mechanism with the free carriers Auger effect via deep states,...
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Biological Activity of Tea-Chokeberry and Chokeberry Fermented Beverages
PublikacjaFermented beverages, such as kombucha are gaining more and more popularity due to their beneficial effects on human health. These products are obtained by the fermentation of tea infusion using so called tea fungus. This microbial consortium can also be used to prepare fermented fruit beverages. Therefore, the aim of this study was to determine the changes in the antioxidant profile of tea-chokeberry and chokeberry beverages...
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Stone cutting industry waste-supported zinc oxide nanostructures for ultrasonic assisted decomposition of an anti-inflammatory non-steroidal pharmaceutical compound
PublikacjaPowdered stone waste (PSW) obtained from a stone cutting industrial unit was applied as support for the immobilization of nano-sized ZnO to be utilized as an effective catalyst for the catalytic conversion of acetaminophen (ACE) under ultrasonication. The incorporation of ZnO nanostructures into PSW structure enhanced the specific surface area and pore volume of the as-prepared nanocompound. The change in the value of zero point...
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Molecular targets for antifungals in amino acid and protein biosynthetic pathways
PublikacjaFungi cause death of over 1.5 million people every year, while cutaneous mycoses are among the most common infections in the world. Mycoses vary greatly in severity, there are long-term skin (ringworm), nail or hair infections (tinea capitis), recurrent like vaginal candidiasis or severe, life-threatening systemic, multiorgan infections. In the last few years, increasing importance is attached to the health and economic problems...
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Sounding Mechanism of a Flue Organ Pipe—A Multi-Sensor Measurement Approach
PublikacjaThis work presents an approach that integrates the results of measuring, analyzing, and modeling air flow phenomena driven by pressurized air in a flue organ pipe. The investigation concerns a Bourdon organ pipe. Measurements are performed in an anechoic chamber using the Cartesian robot equipped with a 3D acoustic vector sensor (AVS) that acquires both acoustic pressure and air particle velocity. Also, a high-speed camera is employed...
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Mechanism of Li nucleation at graphite anodes and mitigation strategies
PublikacjaLithium metal plating is a critical safety issue in Li-ion cells with graphite anodes, and contributes significantly to ageing, drastically limiting the lifetime and inducing capacity loss. Nonetheless, the nucleation mechanism of metallic Li on graphite anodes is still poorly understood. But in-depth understanding is needed to rationally design mitigation measures. In this work, we conducted FirstPrinciples studies to elucidate...
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Investigation of sensing mechanism of Nasicon electrocatalytic sensors in nitrogen dioxide and ammonia
PublikacjaIn this paper a sensing mechanism of Nasicon electrocatalytic sensor in nitrogen dioxide and ammonia is investigated. Both gases are environmentally hazardous and contain nitrogen atom in the molecule. However, it seems that their sensing mechanism in electrocatalytic sensor could be totally different. Namely, the maximum sensitivity for each gas was obtained at different temperatures. Also, different auxiliary layers are formed...
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Establishing the allosteric mechanism in CRISPR‐Cas9
PublikacjaAllostery is a fundamental property of proteins, which regulates biochemical information transfer between spatially distant sites. Here, we report on the critical role of molecular dynamics (MD) simulations in discovering the mechanism of allosteric communication within CRISPR‐Cas9, a leading genome editing machinery with enormous promises for medicine and biotechnology. MD revealed how allostery intervenes during at least three...
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The methodology of design of satellite working mechanism of positive displacement machine
PublikacjaIn this paper is described a methodology of design of satellite mechanism consisting of two noncircular gears (externally toothed rotor and internally toothed curvature) and circular gears (satellites). In the presented methodology is assumed that the rotor pitch line is known, and the curvature pitch line is necessary to designate. The presented methodology applies to mechanisms for which the number of the curvature humps is at...
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Self-assembled concentric stripes of diamond particles by a pinning-depinning mechanism
PublikacjaWe describe the novel mechanism of spontaneous formation of the concentric stripe patterns of microdiamonds via gradual solvent evaporation from a suspension confined in a teardrop well. The self-organized patterns exhibit a series of arcs with regular spacings varying between hundreds of micrometers and millimeters. They result from an interplay between the directional forced circulation of the solvent and a stick-slip movement...
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Inhibition of cancer antioxidant defense by natural compounds
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The influence of food phytochemicals on cyclic phosphodiesterase 4 (PDE4) activity
PublikacjaCyclic phosphodiesterase 4 (PDE4) belongs to family of cyclic phosphodiesterases, which are expressed predominantly in inflammatory cells, airway smooth muscles, cardiovascular tissues and brain. Inhibitors of this family of enzymes found medicinal applications as antidepressants, antiinflamatory drugs (mainly in airway diseases) or antiasthmatics (Ibudilast). PDE4 inhibitors are also being tested for preventing the development...
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Towards spectral sensitivity curve for two-photon vision mechanism
PublikacjaAbstract Purpose: The perceived brightness of different visible light sources can be compared with photometric units based on the standardized luminosity curves (300-780nm range). As reported previously (PNAS 111(50), pp. E5445-E5454 (2014)), near-infrared (NIR) radiation can cause isomerization of visual pigments by one- or two-photon absorption. The perceived color of the stimulus is red in the case of one-photon vision (1PV)...
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Minimising the Churn Out of the Service by Using a Fairness Mechanism
PublikacjaThe paper proposes an algorithm of bandwidth distribution, ensuring fairness to end-users in computer networks. The proposed algorithm divides users into satisfied and unsatisfied users. It provides fairness in terms of quality of experience (QoE) for satisfied users and quality of service (QoS) for unsatisfied users. In this paper, we present detailed comparisons relevant to service providers to show the advantages of the proposed...
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The extended version of restriction analysis approach for the examination of the ability of low-molecular-weight compounds to modify DNA in a cell-free system
PublikacjaOne of the primary requirements in toxicology is the assessment of ability of chemicals to induce DNA covalent modification. There are several well-established methods used for this purpose such as 32P-Postlabeling or HPLC-MS. However, all of these approaches have difficult to overcome limitations, which prevents their use in genotoxin screening. Here, we describe the simple protocol exploiting specificity of restriction enzymes...
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The influence of moderate pressure and subzero temperature on the shelf life of minced cod, salmon, pork and beef meat
PublikacjaThe effect of moderate pressure at subzero temperature on natural microflora of minced cod, salmony, pork and beef meat was studied. Pressure of 193 MPa at –20 °C caused reduction of total bacterial count in pork and beef meat by 1.1 and 0.6 log cycles, respectively, and by about 1.5 log cycles in fish meat. Under these conditions the psychrophilic and psychrotophic bacteria were below the detection limit (<10CFU/g of sample) in...
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublikacjaThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Biomechanical testing of bioactive bone cements – a comparison of the impact of modifiers: antibiotics and nanometals
PublikacjaApart from its bone filler and fracture stabilizing function, bone cement can be used as a carrier of bioactive substances, and such modified bone cement can protect the implant against microorganisms, treat local infections and combat bacteria introduced during the surgical procedure. In this paper, the effects of modifying antibiotics and nanosilver on the biomechanical properties of bone cement were examined. The following tests...
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The Influence of Co-Fermentation of Agri-Food Waste with Primary Sludge on Biogas Production and Composition of the Liquid Fraction of Digestate
PublikacjaEnergy self-sufficiency is a current trend in wastewater treatment plants. This effect can be achieved by increasing the production of electricity from biogas and by reducing energy consumption for technological processes. One idea, in line with the circular economy concept, is the use of waste rich in organic matter as co-substrates for the fermentation process. The aim of this study was to determine the effect of waste co-fermentation...
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Unexpected Z/E isomerism of N-methyl-O-phosphothioyl benzohydroxamic acids, their oxyphilic reactivity and inertness to amines
PublikacjaThiophosphinoylation of N-methyl p-substituted benzohydroxamic acids using disulfanes (method A) or diphenylphosphinothioyl chloride (method B) provides only one conformer of the respective O-phosphothioyl derivative (Xray and NMR analysis). Undergoing the P-transamidoxylation reaction is an evidence of the reversibility of thiophosphinoylation. Only those products containing strong EWG substituents in the aroyl residue or bulky...
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Synergistic Effects of Propolis Combined with 2-Phenoxyethanol and Antipyretics on the Growth of Staphylococcus aureus
PublikacjaThe present investigation aimed to assess the combinational effect of commonly usedantipyretics and antiseptics with ethanolic extracts of propolis (EEPs) on the growth inhibition ofStaphylococcus aureus. The broth microdilution checkerboard assay revealed synergistic interactionsbetween all investigated antipyretics, namely acetylsalicylic acid, ibuprofen, and acetaminophen,with EEPs samples. The values of the fractional inhibitory...
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Pathogenesis of psoriasis in the “omic” era. Part II. Genetic, genomic and epigenetic changes in psoriasis
PublikacjaPsoriasis is a multifactorial disease in which genetic, environmental and epigenetic factors regulating gene expression play a key role. In the “genomic era”, genome-wide association studies together with target genotyping platforms performed in different ethnic populations have found more than 50 genetic susceptible markers associated with the risk of psoriasis which have been identified so far. Up till now, the strongest association...
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The Chitosan-Based System with Scutellariae baicalensis radix Extract for the Local Treatment of Vaginal Infections
PublikacjaScutellarie baicalensis radix, as a flavone-rich source, exhibits antibacterial, antifungal, an-tioxidant, and anti-inflammatory activity. It may be used as a therapeutic agent to treat various
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Influence of geometrical and operational parameters on tooth wear in the working mechanism of a satellite motor
PublikacjaThis article describes the phenomena affecting the wear of the rotor of the working mechanism in a hydraulic satellite motor. The basic geometrical relationships that allow the calculation of the coordinates of the points of contact between the satellite and the rotor and the curvature are presented. A method for calculating the number of contacts of the satellite teeth with the rotor teeth and of the satellite teeth with the curvature...
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A self-optimization mechanism for generalized adaptive notch smoother
PublikacjaTracking of nonstationary narrowband signals is often accomplished using algorithms called adaptive notch filters (ANFs). Generalized adaptive notch smoothers (GANSs) extend the concepts of adaptive notch filtering in two directions. Firstly, they are designed to estimate coefficients of nonstationary quasi-periodic systems, rather than signals. Secondly, they employ noncausal processing, which greatly improves their accuracy and...
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Validation of Hydraulic Mechanism during Blowout Trauma of Human Orbit Depending on the Method of Load Application
PublikacjaThe more we know about mechanisms of the human orbital blowout type of trauma, the better we will be able to prevent them in the future. As long as the buckling mechanism’s veracity is not in doubt, the hydraulic mechanism is not based on equally strong premises. To investigate the correctness of the hydraulic mechanism’s theory, two different methods of implementation of the hydraulic load to the finite element method (FEM) model...
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Mechanism of Osmolyte Stabilization–Destabilization of Proteins: Experimental Evidence
PublikacjaIn this work, we investigated the influence of stabilizing (N,N,N-trimethylglycine) and destabilizing (urea) osmolytes on the hydration spheres of biomacromolecules in folded forms (trpzip-1 peptide and hen egg white lysozyme─hewl) and unfolded protein models (glycine─GLY and N-methylglycine─NMG) by means of infrared spectroscopy. GLY and NMG were clearly limited as minimal models for unfolded proteins and should be treated with...
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Mass Spectrometric Identification of 13C-Labeled Metabolites DuringAnaerobic Propanoic Acid Oxidation
PublikacjaBiowaste digestion is a possibility to gain biogas as a renewable fuel source. However, the anaerobic food chain may be disrupted by, e.g., substrate overload or by inhibitors, leading to the accumulation of volatile fatty acids (VFAs), predominantly of propanoic acid (PA). VFA Accumulation may cause a rapid pH decrease, less biogas production, or even a total inhibition. To maintain high biogas productivity or to prevent a collapse...
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublikacjaFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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Mass spectrometric identification of 13C-Labeled metaboloites during anaerobic propanoic acid oxidation
PublikacjaBiowaste digestion is a possibility to gain biogas as a renewable fuel source. However, the anaerobic food chain may be disrupted by, e.g., substrate overload or by inhibitors, leading to the accumulation of volatile fatty acids (VFAs), predominantly of propanoic acid (PA). VFA Accumulation may cause a rapid pH decrease, less biogas production, or even a total inhibition. To maintain high biogas productivity or to prevent a collapse...
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Chemical and biological evaluation of antioxidant activity of endogenous redox-active compounds compared to plant-derived exogenous antioxidants
PublikacjaThe research conducted so far has shown that endogenous antioxidants, despite being regarded as the first line of antioxidant defense, may not be sufficient to maintain redox homeostasis in cells exposed to oxidative stress. The results obtained in the doctoral dissertation show that endogenous redox-active compounds were moderate or weak scavengers of ABTS and DPPH radicals, while in cellular setting, their impact on the reducing...
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Chemical Aspects of Biological Activity of Isothiocyanates and Indoles, the Products of Glucosinolate Decomposition
PublikacjaThere is growing evidence that cancer chemoprevention employing natural, bioactive compounds may halt or at least slow down the different stages of carcinogenesis. A particularly advantageous effect is attributed to derivatives of sulfur-organic phytochemicals, such as glucosinolates (GLs) synthesized mainly in Brassicaceae plant family. GLs are hydrolysed enzymatically to bioactive isothiocyanates (ITC) and indoles, which exhibit strong...
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Clays as Inhibitors of Polyurethane Foams’ Flammability
PublikacjaPolyurethanes are a very important group of polymers with an extensive range of applications in different branches of industry. In the form of foams, they are mainly used in bedding, furniture, building, construction, and automotive sectors. Due to human safety reasons, these applications require an appropriate level of flame retardance, often required by various law regulations. Nevertheless, without the proper modifications,...
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Removal of diphenols using pine biochar. Kinetics, equilibrium, thermodynamics, and mechanism of uptake
PublikacjaThermal pyrolysis synthesized activated biochar from the Pinus elliottii sawdust (PS) at 600° C. The obtained activated biochar (PB600) was used for the removal of three diphenols, catechol (CAT), resorcinol (RES), and hydroquinone (HYD), which are utilized mainly in different industries. The PB600 was characterized by several analytical techniques. The BET surface area of 1473 m2.g−1 and a total pore volume of 0.707 cm3 g−1 was...
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Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies
PublikacjaA series of 2-(1H-indol-2-yl)-3-acrylonitrile derivatives, 2a–x, 3, 4a–b, 5a–d, 6a–b, and 7, were synthesized as potential antitumor and antimicrobial agents. The structures of the prepared compounds were evaluated based on elemental analysis, IR, 1H- and 13NMR, as well as MS spectra. X-ray crystal analysis of the representative 2-(1H-indol-2-yl)-3-acrylonitrile 2l showed that the acrylonitrile double bond was Z-configured. All...
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PI3Kδ Inhibition by Idelalisib in Patients with Relapsed Indolent Lymphoma
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