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Search results for: MIC, ANTIMICROBIAL ACTIVITY, MURAMYL DIPEPTIDE DERIVATIVES, ANALOGUES OF ANTHRAQUINONES, RETRO-TUFTSIN DERIVATIVES
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Influence of S-Oxidation on Cytotoxic Activity of Oxathiole-Fused Chalcones
PublicationSynthesis, in vitro cytotoxic activity, and interaction with tubulin of oxidized, isomeric 1-(5-alkoxybenzo[d] [1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-ones and 1-(6- alkoxybenzo[d][1,3]oxathiol-5-yl)-3-phenylprop-2-en-1- ones are described. Most of the compounds demonstrated cytotoxic activity at submicromolar concentrations. It was found that oxidation of sulfur atom of the oxathiole-fused chalcones strongly influenced activity...
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The Physical Activity Environment Policy Index for monitoring government policies and actions to improve physical activity
PublicationBackground A multifaceted response, including government action, is essential to improve population levels of physical activity (PA). This article describes the development process of the ‘Physical Activity Environment Policy Index’ (PA-EPI) monitoring framework, a tool to assess government policies and actions for creating a healthy PA environment. Methods An iterative process was undertaken. This involved a review of policy...
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Photosensitive and pH-dependent activity of pyrazine-functionalized carbazole derivative as promising antifungal and imaging agent
PublicationCarbazole skeleton plays a significant role as a structural scaffold of many pharmacologically active compounds. Pyrazine-functionalized carbazole derivative was constructed by coupling 2-amino-5-bromo-3-methylaminepyrazine (ABMAP) into 3 and 6 positions of the carbazole ring. Multi-experimental methods were used, e.g., potentiometric, spectroscopic (ATR, UV, XRD powder,1H and13C NMR), electrochemical (cyclic voltammetry), and...
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublicationGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
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Antifungal Activity and Synergism with Azoles of Polish Propolis
PublicationThe aim of our work was to check if one of the products of natural origin, namely honey 19 bee propolis may be an alternative or supplement to currently used antifungal agents. The activity 20 of 50 ethanolic extracts of propolis (EEPs), harvested in Polish apiaries, was tested on a group of 69 21 clinical isolates of C. albicans. Most of the EEPs showed satisfactory activity, with minimum 22 fungicidal concentrations (MFC) mainly...
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Study of the Anti-Staphylococcal Potential of Honeys Produced in Northern Poland
PublicationThe antimicrobial activity of 144 samples of honeys including 95 products from apiaries located in Northern Poland was evaluated. The antibacterial activity of those natural products, their thermal stability, and activity in the presence of catalase was investigated by microdilution assays in titration plates. The MTT assay was performed for the determination of anti-biofilm activity. Spectrophotometric assays were used for the...
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Knowledge representation of motor activity of patients with Parkinson’s disease
PublicationAn approach to the knowledge representation extraction from biomedical signals analysis concerning motor activity of Parkinson disease patients is proposed in this paper. This is done utilizing accelerometers attached to their body as well as exploiting video image of their hand movements. Experiments are carried out employing artificial neural networks and support vector machine to the recognition of characteristic motor activity...
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Supramolecular structures formed by 2-aminopyridine derivatives. Part I. Hydrogenbonding networks via N-H...N interactions and the conformational polymorphism of N,N´-bis(2-piridyl)aryldiamines
PublicationOtrzymano serię N,N´-bis(2-pirydylo)arylodiamin w postaci monokryształów. Zgodnie z oczekiwaniami, powstawały dwie odmiany polimorficzne. Forma EE z układem wiązań R22(8) figuruje jako jednowymiarowe taśmy. Stwierdzono, że ugrupowanie 2-aminopirydylowe stanowi synton supramolekularny za pomocą którego można projektować struktury w ciele stałym. Właściwości tego syntonu były badane z wykorzystaniem metod dyfrakcyjnych oraz spektroskopii...
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Synthesis and biological evaluation of 2,7-Dihydro-3H-dibenzo[de,h]cinnoli- ne-3,7-done derivatives a novel group of anticancer agents active on a multidrug resistance cell line.
PublicationZsyntezowano serię pochodnych pirydazonu z jednym lub dwoma łańcuchami bocznymi w różnych pozycjach chromoforu tetracyklicznego. Związki wykazały aktywność cytoksyczną na mysią białaczkę L1210 i ludzką k562 oraz na linii komórkowej oporności krzyżowej MDR (k562/DX). Dwa najbardziej aktywne związki przetestowano in vivo na mysiej białaczce P388. Wykazały one aktywność przeciwnowotworową porównywalną z aktywnością Mitoxantronu.
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Lower rim substituted tert-butyl calix[4]arene (part VII): ionophoric properties of calix[4]arene-crown-6 derivatives in plasticized PVC-membrane electrodes and in solution.
PublicationW pracy przedstawiono syntezę i charakterystykę otrzymanych produktów (2-9), pochodnych p-tert-butylokaliks[4]-korony-6. Zdolności kompleksujące tych związków badano w elektrodach jonoselektywnych, stosując te związki jako jonofory w plastyfikowanej membranie PCW.Wyznaczono wartości stałych trwałości kompleksów z jonami metali I grupy. Stwierdzono, że selektywność kompleksowania zależy od rozmiaru i natury podstawnika wprowadzonego...
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Pathological brain network activity: memory impairment in epilepsy
PublicationOur thinking, memory and cognition in general, relies upon precisely timed interactions among neurons forming brain networks that support cognitive processes. The surgical evaluation of drug-resistant epilepsy using intracranial electrodes provides a unique opportunity to record directly from human brain and to investigate the coordinated activity of cognitive networks. In this issue of Neurology®, Kleen and colleagues1 implicate...
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Differential antitumor effects of vitamin D analogues on colorectal carcinoma in culture
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Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule
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Awareness of patients suffering from selected chronic diseases of the importance of physical activity in treating their disorders
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Development of Antimicrobial Phototreatment Tolerance: Why the Methodology Matters
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Kalanchoe sp. Extracts—Phytochemistry, Cytotoxic, and Antimicrobial Activities
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New conjugates of mycophenolic acid and their antiproliferative activity
PublicationThe new conjugates of mycophenolic acid (MPA) were obtained in the reaction of N6-(ω-aminoalkyl)adenosines with MPA in the presence of EDCI as a coupling reagent. New compounds 4a–h were evaluated on leukemia cell line (Jurkat) and PBMC from healthy donors. Length of the linker influenced observed activity. The compound 4b possessing 1,3-diamine spacer exhibited the most promising results and can be considered to further investigations.
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The Relation Between Art and Physical Activity in the Public Space of the Contemporary City
PublicationArt has always been and still is a mirror in which human activity is reflected. One of the basic human activities is physical activity, thanks to which humans are able to satisfy their needs, improve health and also function in society. Therefore, there are different relationships between physical activity and art. Both of them are present in the public space of cities and this aspect of connection is addressed in the article. The...
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Validated HPTLC method for determination of ledol and alloaromadendrene in the essential oil fractions of Rhododendron tomentosum plants and in vitro cultures and bioautography for their activity screening
PublicationRhododendron tomentosum (Ledum palustre) is a bog shrub used in traditional medicine for treatment of respiratory and rheumatic diseases. Due to the large variability of the chemical composition of its essential oil, depending on the habitat, the in vitro cultures were established as the alternative source of the volatile fraction. There is a need to monitor a quality of the field grown as well as in vitro plant material, especially...
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The influence of food phytochemicals on cyclic phosphodiesterase 4 (PDE4) activity
PublicationCyclic 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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Detection of person presence and its activity in the bathtub
PublicationA practical application of a bioimpedance technique for a detection of a bathing person is presented in the paper. It addresses the possibility of supervising people in the bathtub without voiding of their intimacy. The measurement system installed in a fiber-glass or a plastic bathtub is able to detect a presence of the bathing person, to estimate its activity and thus to detect potentially dangerous events. In the paper a principle...
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Comparison of Acoustic and Visual Voice Activity Detection for Noisy Speech Recognition
PublicationThe problem of accurate differentiating between the speaker utterance and the noise parts in a speech signal is considered. The influence of utilizing a voice activity detection in speech signals on the accuracy of the automatic speech recognition (ASR) system is presented. The examined methods of voice activity detection are based on acoustic and visual modalities. The problem of detecting the voice activity in clean and noisy...
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Essential oils as potential anti-staphylococcal agents
PublicationAntibiotic therapy of staphylococcal mastitis is characterized by significantly lower cure rates compared to infections caused by other microorganisms. Thus, it is necessary to search for new, alternative, non-antibiotic agents that are effective in the eradication of these bacteria. The aim of our research was to investigate the antimicrobial, especially anti-staphylococcal potential of a large collection (n=36) of essential oils...
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Obtaining and Characterization of the PLA/Chitosan Foams with Antimicrobial Properties Achieved by the Emulsification Combined with the Dissolution of Chitosan by CO2 Saturation
PublicationA new method of obtaining functional foam material has been proposed. The materials were created by mixing the poly lactic acid (PLA) solution in chloroform, chitosan (CS) dissolved in water saturated with CO2 and polyethylene glycol (PEG), and freeze-dried for removal of the solvents. The composite foams were characterized for their structural (SEM, FT-IR, density, porosity), thermal (DSC), functional (hardness, elasticity, swelling...
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Obtaining and Characterization of the PLA/Chitosan Foams with Antimicrobial Properties Achieved by the Emulsification Combined with the Dissolution of Chitosan by CO2 Saturation
PublicationA new method of obtaining functional foam material has been proposed. The materials were created by mixing the poly lactic acid (PLA) solution in chloroform, chitosan (CS) dissolved in water saturated with CO2 and polyethylene glycol (PEG), and freeze-dried for removal of the solvents. The composite foams were characterized for their structural (SEM, FT-IR, density, porosity), thermal (DSC), functional (hardness, elasticity, swelling...
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Influence of temperature on the activity of anammox granular biomass.
PublicationThe aim of this study was to determine a short-term and long-term effect of temperature on the anammox rate and determination of temperature coefficients in the Arrhenius and Ratkowsky equations. The short-term effects of temperature on the anammox granular biomass were investigated in batch tests at ten different temperatures in the range of 10–55 °C. The maximum overall nitrogen removal rate of 1.3 gN gVSS−1·d−1 was observed...
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Territorial Aspects of Entrepreneurial Activity in Polish Suburban Zones
PublicationGlobalization has led to an increased correlation and integration of various fields in modern civilization, including those connected with allocation of entrepreneurial functions. Connection, on a global scale, has shown an increased significance of worldwide corporations. Territorial allocation of the entrepreneurial function has become the subject of translocation and revaluation. Translocation can be understood as the change...
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Optimal placement of IMU sensor for the detection of children activity
PublicationIn this paper an investigation to determine the optimal placement of IMU sensors for the purpose of children characteristic activity detection is presented. The article compares four different placement of two IMU sensors on human body. Ten healthy volunteers participated within the study. Data were collected firstly from two wireless 9-axial IMU sensors placed at the left and right wrists, then sensors were placed at lower back...
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Elderly persons professional activity - substantive issues and methodical challenges
PublicationPopulation ageing and mass withdrawal of persons around retirement age from the labour market constitutes a serious threat for European Union economy, especially in the so-called new member states. The coming years are expected to bring a considerable increase in public spending on pensions and health care, as well as changes in the structure and size of consumer demand and an increase in the number of socially excluded individuals....
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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublicationAbstract: Background: It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective: The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian vitro toxicity of thus prepared AmB derivatives. Methods:...
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The microbial community, its biochemical potential, and the antimicrobial resistance of Enterococcus spp. in Arctic lakes under natural and anthropogenic impact (West Spitsbergen)
PublicationThe sustainable management of small human communities in the Arctic is challenging. In this study, both a water supply system (Lake 1) under the natural impact of a bird-nesting area, and a wastewater receiver (Lake 2) were analysed in the vicinity of the Polish Polar Station on West Spitsbergen. Microbial community composition, abundance and activity were assessed in samples of the treated wastewater, lake water and sediments...
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Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin
PublicationSynthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol- 5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site. Interaction of selected derivatives with tubulinwas evaluated using molecular modeling,...
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Biological Activity of Tea-Chokeberry and Chokeberry Fermented Beverages
PublicationFermented 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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Peptomeric analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds
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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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Conformational studies of cyclic enkephalin analogues withL- orD-proline in position 3
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Theoretical Study on Interactions of Bicyclic Vasopressin Analogues with Human Neurohypophyseal Hormone Receptors
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SYNTHESIS AND FLUORESCENT PROPERTIES OF THE TRICYCLIC ANALOGUES OF ACYCLOVIR LINKED WITH NITROGEN HETBROCYCLIC UNITS
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Stereochemical Assingment of β -lactam Antibiotics and their Analogues by Electronic Circular Dichroism Spectroscopy
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The Advancement of Biodegradable Polyesters as Delivery Systems for Camptothecin and Its Analogues—A Status Report
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Solid-phase synthesis and characterization of N-acetylated Gly-His-Lys analogues
PublicationZaprezentowano nowe analogi tripeptydu Gly-His-Lys (GHK), stanowiącego sekwencję naturalnie występującą w -II-łańuchu kolagenu, skąd jest uwalniany w stanach zapalnych i w procesach gojenia się ran. Gly-His-Lys jest szeroko stosowany na rynku kosmetycznym w połączeniu z kwasem palmitynowym, który ułatwia jego wnikanie w głąb skóry. Zaplanowane modyfikacje zawierały fragment Gly-X-Y (X=Met, Hyp, Hyp-Met, Gly-Hyp; Y=Lys, D-Lys) i...
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The ability of new sugar-modified derivatives of antitumour anthracycline, daunorubicin, to stimulate NAD(P)H Oxidation in Different Cellular Oxidoreductase Systems: NADH Dehydrogenase, NADPH Cytochrome P450 Reductase, and Xanthine Oxidase.
PublicationUboczne działanie cytostatyków z grupy antracyklin prowadzi do uszkodzenia serca (kardiotoksyczność) w wyniku pośredniczenia przez te związki przeniesienia jednoelektronowego ze zredukowanych nukleotydów do tlenu i powstania reaktywnych anionorodników tlenowych. Proces ten jest katalizowany głównie przez trzy enzymy: dehydrogenazę NADH, reduktazę NADPH/cytochrom P450 oraz oksydazę ksantynową. W publikacji przedstawione są wyniki...
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Helicity discrimination in N,N'-dibenzoyl-1,2,3,4,7,8,9,10-octahydro-1,10-phenanthrolines and their thiono- and selenocarbonyl analogues by inclusion complexation with chiral diols
PublicationX-ray crystallographic analysis of the title compounds revealed that they assume a folded helical con- formation of an approximate C2 symmetry in the solid state. Dithioamide, diselenoamide and monoselenoamide were resolved to enantiomers by inclusion crystallization with optically active diols (TADDOLs). The absolute configuration of the guest molecules in the complexes was assigned as P. The optical activity of the resolved compounds...
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Method for Clustering of Brain Activity Data Derived from EEG Signals
PublicationA method for assessing separability of EEG signals associated with three classes of brain activity is proposed. The EEG signals are acquired from 23 subjects, gathered from a headset consisting of 14 electrodes. Data are processed by applying Discrete Wavelet Transform (DWT) for the signal analysis and an autoencoder neural network for the brain activity separation. Processing involves 74 wavelets from 3 DWT families: Coiflets,...
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The effect of freeze-drying and storage on lysozyme activity, lactoferrin content, superoxide dismutase activity, total antioxidant capacity and fatty acid profile of freeze-dried human milk
PublicationPooled human milk samples were freeze-dried and stored for 6 weeks at a temperature of 5 C and 25 C. Freeze-drying decreased the water content of milk by 86.5%, and the obtained lyophilizate was readily soluble in water. The freeze-drying process did not affect superoxide dismutase (SOD) activity, fatty acid (FA) profile or lactoferrin (LF) content, but it decreased total antioxidant capacity (TAC) of human milk by 22.1% and induced...
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Pr-doped TiO2: The effect of metal content on photocatalytic activity
PublicationThe Pr-TiO2 nanoparticles were prepared by using the sol-gel method. As-prepared samples were characterized by BET measurements, X-ray powder diffraction analysis (XRD) and UV-Vis spectra. Visible and ultraviolet light photocatalytic activity of the sample was studied by photodegradation of phenol while considering the influence of the dopant concentration. TiO2 doped with 0.25 mol% of praseodymium showed the highest photocatalytic...
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Accelerometer signal pre-processing influence on human activity recognition
PublicationA study of data pre-processing influence on accelerometer-based human activity recognition algorithms is presented. The frequency band used to filter-out the accelerometer signals and the number of accelerometers involved were considered in terms of their influence on the recognition accuracy.
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Ionic liquid as morphology-directing agent of two-dimensional Bi2WO6: New insight into photocatalytic and antibacterial activity
PublicationAn efficient and durable utilization of light to drive photocatalytic reactions still requires the overcoming of barriers. Herein, two-dimensional (2D) ultrathin IL_Bi2WO6 (IL_BWO) photocatalysts were prepared for the first time via ionic liquid-assisted hydrothermal route by adjusting the amount of tetrabutylammonium chloride [TBA][Cl], synthesis temperature and duration. IL played the role of morphology-directing agent given...
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Induction of the Stringent Response Underlies the Antimicrobial Action of Aliphatic Isothiocyanates
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Antimicrobial properties of protective coatings produced by plasma spraying technique
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