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Wyniki wyszukiwania dla: CYP3A4 INHIBITION
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Therapeutic Potential of Multifunctional Tacrine Analogues
PublikacjaTacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as a model inhibitor of cholinesterases in the therapy of Alzheimer’s disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we...
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Instantaneous Impedance Analysis of Non-Stationary Corrosion Process: a Case Study of Carbon Steel in 1M HCl
PublikacjaThe paper concerns the problem of evaluation of stationarity of carbon steel corrosion in 1M HCl. Comparison of corrosion rate with addition of corrosion inhibitor to the reference measurement is the most often used way of evaluating inhibitor efficiency. Such an approach is valid only if corrosion rate is a stationary process. Two complementary techniques were used simultaneously: volumetric analysis of evolved hydrogen and instantaneous...
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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
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Flavonoids as inhibitors of human neutrophil elastase
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Chemical reactivity and antimicrobial activity of N-substituted maleimides
PublikacjaZsyntezowano kilkanaście N-podstawionych maleimidów, zawierających w swojej strukturze podstawniki o różnej wielkości i polarności.Maleimidy o charakterze obojętnym wykazywały silny efekt przeciwgrzybowy; ich aktywność przeciwbakteryjna była zróżnicowana. Niską aktywność przeciwbakteryjną, ale wysoką aktywność cytostatyczną stwierdzono dla maleimidów o charakterze zasadowym. Reaktywność chemiczna i lipofilowość miały wpływ na aktywność...
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublikacjaIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublikacjaIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublikacjaAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublikacjaIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublikacjaIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublikacjaGlucosamine-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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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublikacjaThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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Sulfonamides with hydroxyphenyl moiety: Synthesis, structure, physicochemical properties, and ability to form complexes with Rh(III) ion
PublikacjaSulfonamides are the first successfully synthesized antimicrobial drugs. The mechanism of sulfonamides’ antimicrobial action involves competitive inhibition of folic acid synthesis and prevention of the growth and reproduction of bacteria. Even though they have been applied in therapy for more than 75 years, sulfonamides are still the drugs of choice for the treatment of various diseases. The aim of this work was to synthesize...
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Aromatic heptaene antibiotics as an alternative for synthetic triazole fungicides in plant protection
PublikacjaAn in vitro antifungal activity of candicidin and ascosin antibiotics (0,01-10 μg/mL) towards representative strains of phytopathogenic fungi was detd. Both compds. exhibited similar half max. effective concns. inhibiting growth of the fungi as that of tebuconazole used for comparison.
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The impact of training and neurotrophins on functional recovery after spinal cord transection: cellular and molecular mechanisms contributing to motor improvement
PublikacjaBeneficial effects of locomotor training on the functional recovery after complete transection of the spinal cord indicate that in chronic spinal animals spontaneous recovery processes are enhanced and shaped by the training. The mechanisms of that use-dependent improvement are still not fully understood. This review tackles three aspects of this issue: (1) neurochemical attributes of functional improvement...
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ADAPTATION OF THE ACTIVATED SLUDGE TO THE DIGESTATE LIQUORS DURING THE NITRIFICATION AND DENITRIFICATION PROCESSES
PublikacjaThe activated sludge process of the digestate liquors after chemical separation was conducted using a 10 L lab-scale sequencing batch reactor (SBR) and a 0.50 m3 pilotscale SBR independently (with pH control). Due to the relatively high concentration of free ammonia (FA), clear inhibitory effects of the digestate liquors on the nitrifying bacteria were observed. The adaptation of the activated sludge to the toxicity was evaluated...
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Modelling AOB-NOB competition in shortcut nitrification compared with conventional nitrification-denitrification process
PublikacjaIn particular, mainstream deammonification and/or shortened nitrificationdenitrification via nitrite (so-called “nitrite shunt”) is a promising new treatment concept that has the potential to revolutionise how nitrogen removal is achieved at WWTPs. Understanding the role of the AOB/NOB competition in the nitrogen cycle in wastewater treatment systems will change operational strategies of the novel nitrogen removal processes. The...
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Architektoniczne tożsamości miasta portowego - na przykładach Gdańska i Gdyni oraz Hamburga i Altony
PublikacjaHarbour cities of Northern Europe, especially those growing in the circle of influence of Hanseatic League, were formed in a way, which allows to identify them as the cities of a specific identity considering architecture and urban planning. Industrial revolution of 19-th and early 20-th century brought the radical change in the field of spatial development of the cities. Economical, political, cultural influences, also social...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublikacjaCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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Structural features responsible for control of the eukaryotic GlcN-6-P synthase activity
PublikacjaGlucosamine-6-phosphate (GlcN-6-P) synthase is responsible for catalysis of the first and practically irreversible step in hexosamine metabolism. As UDP-GlcNAc, the final product of the hexosamine path, constitutes one of the essential substrates for assembly of bacterial and fungal cell walls, the enzyme is an interesting target for antimicrobial therapy.The structure of E. coli enzyme, known since 2001, forms a dimer of two identical...
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublikacjaBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Chemical and biological characterization of Ocimum basilicum L. phenolic extract and essential oil derived through ultrasound and microwave-assisted extraction techniques
PublikacjaPlant-derived bioactive molecules are increasingly utilized in food processing as natural additives, driven by a growing interest in healthier lifestyles. This trend has spurred industries to reformulate products to meet the demands of health-conscious consumers. This study investigates the phenolic extract and essential oil of O. basilicum L. obtained via ultrasound-assisted extraction and microwave-assisted extraction, respectively. Characterization...
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Elucidation of chemical compounds in different extracts of two Lavandula taxa and their biological potentials: Walking with versatile agents on the road from nature to functional applications
PublikacjaDue to their health-promoting and nutraceutical properties, lavenders are frequently employed in the food and pharmaceutical industries. Here, we focused on investigate the chemical profile of hexane, MeOH, and water extracts of leaf, flower, and root of L. pedunculata and L. stoechas and to assess their antioxidant, enzyme inhibitory, and antibacterial properties. The highest total polyphenolic and flavonoids contents were recorded...
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REVIEW ON COMPETITION АОB AND NОВ AS AN IMPORTANT ELEMENT FOR COST EFFECTIVE METHODS OF REMOVING NITROGEN FROM WASTEWATER
PublikacjaThe aim of this paper is analysis of process principles and possible factors used to induce inhibition of nitrite oxidation by NOB (Nitrite Oxidizing Bacteria) which could be obtained during not very well understood processes: so called “shortcut” or “partial” nitrification as well deammonification, by qualitative/quantitative studies of AOB (Ammonium Oxidizing Bacteria) and NOB populations in activated...
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Application of Extreme Doses of Aluminium for Growth Control of Filmentous Bacteria Microthrix Parvicella in an Activated Sludge System - Laboratory Investigations
PublikacjaLaboratory investigations of aluminium (PAX-16) application for control of population of filamentous bacteria Microthrix Parvicella in a three-phase bioreactor in lab-scale were performed. Dosing of small aluminium doses (approximately 0.5 mgAl/gMLSS·d) in the period preceding seasonal growth of M.Parvicella failed to prevent mass growth of this microorganism leading to activated sludge bulking phenomenon (SVI-250 ml/gMLSS)...
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublikacjaThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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Novel fast non-linear electrochemical impedance method for corrosion investigations
PublikacjaThe paper presents a novel approach to corrosion rate monitoring using non-linear electrochemical impedance spectroscopy. The authors propose a new variant of non-linear impedance measurement using amplitude-modulated multi-frequency ac perturbation signal. It allows shortening of measurement duration so it is possible to monitor corrosion rate of the systems experiencing rapid changes. In this way a limitation resulting from lack...
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Estimation of the effectiveness of nbpt for limiting ammonia emission from urea based on the field experiments
PublikacjaThe efectiveness of the ammonia emission reduction from NBPT-stabilized urea was investigating in 2011 during a field experiment on a grassland plot fertilized with a one-time dose of 60 kgN/ha. The obtained reduction coefficient of ammonia emission equaled 73% and 39-51% relative to erea without the inhibitor and ammonium nitrate, respectively.
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Drug-Eluting Biopsy Needle as a Novel Strategy for Antimicrobial Prophylaxis in Transrectal Prostate Biopsy
PublikacjaOBJECTIVES: To preclinically evaluate drug-eluting biopsy needles (patent pending WO2016118026) as a new potential way of antimicrobial prophylaxis for transrectal prostate biopsy. METHODS: Twenty steel biopsy needles have been coated with polyvinyl alcohol, ciprofloxacin, and amikacin. Modified biopsy needles have been randomly divided into 3 groups (1:2:1 ratio). Needles from group I were immersed for 30 minutes in dedicated...
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Micro-Raman spectroscopy in the studies of multiphase separated polyurethanes. [online] W: [Proc.] UTECH Europe 2003 . The International Polyurethane Industry Conference and Exhibition. 25/26/27 March 2003, The Hague, Netherlands. London: Crain Communications Ltd. Dostępny w World Wide Web: http://UTECH-2003.com + wydruk.**2003 [s. 123-130 bibliogr. 41 poz.]Mikro-Ramanowska spektroskopia w badaniach poliuretanów wykazujących separację wielofazową.
PublikacjaPrzedmiotem badań były trzy próbki poliuretanowe o zawartości 30% segmentówsztywnych otrzymanych z politlenku propylenu, diizocyjanianu difenylometanui butanodiolu. Próbki te wykazują morfologię wielofazową, w której można wy-różnić globule i sferolity rozproszone w matrycy polimerowej.Za pomocą spek-troskopii mikro-Ramana przeprowadzono mikroanalizę chemiczną wszystkich ele-mentów morfologicznych. Stwierdzono odmienny skład...
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The role of epigenetics in regeneration
PublikacjaComplex changes in chromatin structure and at the transcriptional level occur from the creation of a single parental gamete throughout fertilization, embryo development and the life of an adult organism. Epigenetic changes, such as methylation and hydroxymethylation of DNA or histone methylation and acetylation, are an important part of these processes. Epigenetic regulation has an essential influence on gene expression level. DNA...
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Biologically active compounds based on the carbazole scaffold - synthetic and mechanistic aspects
PublikacjaDoctoral dissertation is divided into three main parts: introduction, results and discussion and experimental. The introduction is divided into four main parts which describe: 5-hydroxytryptamine receptors, the most popular antidepressants, new compounds based on the carbazole structure with affinity for serotonin receptors, telomeres and telomerase with their functions, telomerase inhibition strategies, carbazoles approved in...
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Ogród muz I
PublikacjaNiniejsza książka składa się z dwóch części. W pierwszej znajdują się eseje wprowadzające Czytelnika w tematykę obecności tradycji antycznej w Gdańsku wczesnonowożytnym. Ich autorami są młodzi badacze z różnych ośrodków akademickich. Część druga to katalog wystawy, która miała miejsce w siedzibie Polskiej Akademii Nauk Biblioteki Gdańskiej (19 czerwca do 31 lipca 2015 roku). Na ekspozycji zaprezentowano stare druki i rękopisy...
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W gdańskim ogrodzie muz. Gimnazjum Akademickie w Gdańsku wobec kultury starożytnych Greków i Rzymian: idee, teksty, artefakty.
PublikacjaNiniejsza książka składa się z dwóch części. W pierwszej znajdują się eseje wprowadzające Czytelnika w tematykę obecności tradycji antycznej w Gdańsku wczesnonowożytnym. Ich autorami są młodzi badacze z różnych ośrodków akademickich. Część druga to katalog wystawy, która miała miejsce w siedzibie Polskiej Akademii Nauk Biblioteki Gdańskiej (19 czerwca do 31 lipca 2015 roku). Na ekspozycji zaprezentowano stare druki i rękopisy...
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Protective and Suppressing Electromagnetic Interference Properties of Epoxy Coatings Containing Nano-Sized NiZn Ferrites
PublikacjaNano-crystalline ferrites with the chemical formula NixZn(1−x)Fe2O4, where x = 0, 0.2, 0.4, 0.6, 0.8, 1.0, were synthesized using a co-precipitation method. The obtained ferrites were investigated by X-ray diffraction (XRD). The corrosion inhibiting behavior of nano-sized ferrites was tested using carbon steel samples and 10% aqueous ferrite extracts. Results were compared with previous data obtained for micro-sized ceramic ferrites....
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Architectural expression in designing museums as places of remembrance
PublikacjaMuseums commemorating tragic historic events require the application of particular means of architectural expression. Both the form of the building, the interior design, lighting and materials and its surroundings became a part of the exhibition. In this article the narrative role of architectural components is discussed based on three museums located in different cultural and geographical areas. These are: the Nanjing Massacre...
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Strontium-based nanosized phosphates as anticorrosive fi llers of epoxy and polyurethane coating compositions
PublikacjaAnticorrosive epoxy and polyurethane coatings were compounded using zinc-free nanosized phosphates of strontium (SP) or strontium and aluminum (SAP). For comparison, a nanosized calcium aluminum ammonium phosphate (CAP) and a microsized zinc phosphate (ZP) were tested. Results of salts spray and cyclic corrosion tests revealed better anticorrosive properties of the SAP-based coatings...
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Chiral Pyrazolo[4,3-e][1,2,4]triazine Sulfonamides—Their Biological Activity, Lipophilicity, Protein Affinity, and Metabolic Transformations
PublikacjaReferring to our previous laboratory results related to the tyrosinase and urease inhibition by pyrazolo[4,3-e][1,2,4]triazine sulfonamides, we examined here in silico the mechanism of action at the molecular level of the investigated pyrazolotriazine sulfonamides by the molecular docking method. The studied compounds being evaluated for their cytotoxic effect against cancer cell lines (MCF-7, K-562) and for recombinant Abl and...
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Azymutalny pędnik podowy z napędem hydraulicznym do małych statków
PublikacjaW artykule przedstawiono opis konstrukcji wraz z rysunkiem złożeniowym oraz rysunkami trójwymiarowymi oryginalnego podowego pędnika azymutalnego dla małego statku rybackiego. Pędnik ten z napędem hydraulicznym zaprojektowany na Politechnice Gdańskiej został wykonany i częściowo przebadany. Wystawiony na 16th International Maritime Exhibition BALTEXPO-2011, spotkał się z dużym zainteresowaniem zwłaszcza armatorów małych statków...
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Enhanced aging resistance of poly(ε-caprolactone)/brewers’ spent grain composites
PublikacjaThe presented paper investigated the influence of brewers’ spent grain (BSG) extrusion pa-rameters on the photo-oxidative resistance of poly(ε-caprolactone)-based wood polymer composites. Filler samples characterized by the higher melanoidin content were more efficient in hindering of poly-mer degradation, inhibiting the decomposition of the polymer amorphous phase. As aresult, deteriora-tion of mechanical performance was limited,...
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The Antibacterial and Antifungal Textile Properties Functionalized by Bimetallic Nanoparticles of Ag/Cu with Different Structures
PublikacjaWe reported a preparation and characterization of five kinds of impregnation solutions, containing Ag/Cu in the formof bimetallic nanoparticles (alloy and core-shell) as well as ionic species. The cotton-polyester textiles were successfully impregnated during the washing and ironing process by as-prepared solutions to have antibacterial and antifungal properties against to Escherichia coli, Staphylococcus aureus, and Candida albicans....
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Chemical composition, antioxidant and anticancer effects of the seeds and leaves and indigo (polygonum tinctorium Ait.) Plant
PublikacjaSeeds and leaves of indigo (Polygonum tinctorium Ait.) plant were investigated and compared with another medicinal plant named prolipid for their properties such as chemical composition, antioxidant, and anticancer effects by Fourier transform infrared, three-dimensional fluorescence spectroscopy, and electrospray ionization-MS in negative mode. It was found that polyphenols, flavonoids, and flavanols were significantly higher...
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Genetic predisposition to inflammatory bowel disease
PublikacjaInflammatory bowel disease (IBD) is a chronic, incurable inflammatory disease of the digestive system. The two main disease entities included in the IBD are ulcerative colitis and Crohn's disease. According to epidemiological studies there are more and more new cases every year. In especially among the youngest patients with symptoms of malnutrition and growth inhibition to land up in hospitalwith cancer suspected. The purpose...
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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...