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Search results for: antitumor drug resistance
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Rational design, synthesis and biological evaluation of thiadiazinoacridines: a new class of antitumor agents.
PublicationZsyntetyzowano serię związków o potencjalnej zdolności do wiązania się z DNA z grupy tiadiazinoakrydyn poprzez cyklizację odpowiednich pochodnych 9-imino-4-nitro-9,10-dihydroakrydyny. Zbadano ich zdolność do wiązania się z DNA oraz cytotoksyczność względem kilku linii komórek nowotworwych. Badania aktywności przeciwnowotworowej wobec białaczki P388 wskazały na zgodność tych wyników z wynikami cytotoksyczności in vitro. Wykazano,...
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Optimization of biocorrosion resistance and mechanical properties of PM Ti–XAl–2Fe–3Cu alloys by response surface methodology
PublicationIn the current study, the biocorrosion resistance and mechanical properties of the Ti–XAl–2Fe–3Cu (wt%) (X = 6, 4, 2 wt%) alloy produced by powder compact extrusion of blended elemental powders were optimized by using the response surface methodology in order to gain the best combination of processing parameters. To run the optimization process, central composite design with three equal levels of oxygen, hydrogen and aluminum was...
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Recent Advances in Polymer-Based Vaginal Drug Delivery Systems
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Filling of Carbon Nanotubes: Containers for Magnetic Probes and Drug Delivery
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Controlled Drug Release by the Pore Structure in Polydimethylsiloxane Transdermal Patches
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Chemometrics of bi-heterocyclic kind of drug specimens in the THz domain
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Chitosan-Based Nanoparticles as Effective Drug Delivery Systems—A review
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Mesoporous silica nanoflakes – Biocompatibility, cellular uptake and drug transport
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Effect of microstructure on mechanical properties and corrosion resistance of 2205 duplex stainless steel
PublicationThis paper presents results of the research on impact of microstructure of austenitic-ferritic steel of duplex type on its mechanical properties and susceptibility to stress corrosion cracking. As showed, improper processing technologies more and more often used in shipbuilding industry for plates and other half-finished products made of duplex steel may cause significant lowering their properties, which frequently makes their...
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Dynamic mechanical properties and flexing fatigue resistance of tire sidewall rubber as function of waste tire rubber reclaiming degree
PublicationA stepwise downsizing method of gel particles in reclaimed rubber to a micro-nano scale and its excellent dynamic performance in tire sidewall were introduced by this work. The results showed that the size of gel particles decreased from several micrometers to micro-nanometers with the increase of reclaiming degree, accompanied by reduced molecular weight and widened molecular weight distribution of sol fraction. The addition of...
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Experimental verification of a new method of loop resistance testing in low voltage systems with residual current devices
PublicationA periodical verification of the effectiveness of protection against electric shock shall be performed in low voltage systems. The scope of this verification includes loop impedance/resistance testing. If a residual current device is installed in a tested circuit, this testing is problematic. A residual current device trips out during the test, because of the high value of measurement current. This precludes the execution of the...
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The abrasive wear resistance of coatings manufactured on high-strength low-alloy (HSLA) offshore steel in wet welding conditions
PublicationSome marine and offshore structure elements exploited in the water cannot be brought to the surface of the water as this will generate high costs, and for this reason, they require in-situ repairs. One of the repair techniques used in underwater pad welding conditions is a wet welding method. This paper presents an investigation of the abrasive wear resistance of coatings made in wet welding conditions with the use of two grades...
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Successive cytotoxicity control by evolutionary surface decorated electronic push-pull green ZnCr-LDH nanostructures: Drug delivery enlargement for targeted breast cancer chemotherapy
PublicationThe reason for the increasing bioavailability and biocompatibility of the porous nanomaterials in the presence of different (bio)molecules is still unknown. The role of difference functional groups and their interactions with the potential bioavailability and biocompatibility is of great importance. To investigate the potential contribution of the electronic effects (especially on the surface of the porous nanomaterials) on their...
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Corrosion Resistance and Surface Bioactivity of Ti6Al4V Alloy after Finish Turning under Ecological Cutting Conditions
PublicationThe influence of cooling conditions and surface topography after finish turning of Ti6Al4V titanium alloy on corrosion resistance and surface bioactivity was analyzed. The samples were machined under dry and minimum quantity lubrication (MQL) conditions to obtain different surface roughness. The surface topographies of the processed samples were assessed and measured using an optical profilometer. The produced samples were subjected...
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Bortezomib induces methylation changes in neuroblastoma cells that appear to play a significant role in resistance development to this compound
PublicationThe anticancer activity of bortezomib (BTZ) has been increasingly studied in a number of indications and promising results for the use of this treatment have been shown in neuroblastoma. As BTZ treatment is usually administered in cycles, the development of resistance and side effects in patients undergoing therapy with BTZ remains a major challenge for the clinical usage of this compound. Common resistance development also means...
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Relieving the Measuring System of the Trailer for Tyre/Road Rolling Resistance Measurements from the Inertia Force
PublicationIn the article the principle of measuring of tyre/road rolling resistance tyres in road conditions applied in a special measuring trailer is presented. This trailer was built in Faculty of Mechanical Engineering at Gdansk University of Technology. The construction of two special devices used in this trailer was discussed. These devices eliminate the influence of some chosen confounding measurements factors such as: the inertia...
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Evaluation of the resistance of steel–concrete adhesive connection in reinforced concrete beams using guided wave propagation
PublicationThe development of the nondestructive diagnostic methods is of significant importance in the last decades. A special attention is paid to diagnostics of reinforced concrete structures, which are very popular in the civil engineering field. A possible use of the guided waves in the estimation of the resistance of steel–concrete adhesive connection is studied in the following paper. The relationships relating adhesive connection...
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Functionalization of graphene oxide coatings with phosphorus atoms and their corrosion resistance in sodium chloride environment
PublicationIn this work, we compared corrosion resistance of graphene oxide, and phosphorus functionalized reduced graphene oxide coatings obtained as a result of electrophoretic deposition on the copper substrate. Doping graphene oxide with phosphorus atoms was performed by a hydrothermal method in the presence of different amounts of phosphoric acid. Structural studies confirmed the insertion of phosphorus atoms into the graphene oxide...
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Enhancing the Seismic Resistance of Columns by GFRP Confinement Using Flexible Adhesive-Experimental Study
PublicationIn this paper, the results of two experiments, focused on testing the effectiveness of a method of enhancing the seismic (dynamic) resistance of masonry columns with the use of flexible polymer adhesive, are shown. The first experiment was devoted to investigate the damping properties of a polymer working between two stiff layers, whereas the aim of the second one was to verify if the identified damping properties of the polymer...
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A strong preference for the TA/TA dinucleotide step discovered for an acridine-based, potent antitumor dsDNA intercalator, C-1305: NMR-driven structural and sequence-specificity studies
PublicationTriazoloacridinone C-1305, a potent antitumor agent recommended for Phase I clinical trials, exhibits high activity towards a wide range of experimental colon carcinomas, in many cases associated with complete tumor regression. C-1305 is a well-established dsDNA intercalator, yet no information on its mode of binding into DNA is available to date. Herein, we present the NMR-driven and MD-refined reconstruction of the 3D structures...
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The treatment of wastewater containing pharmaceuticals in microcosm constructed wetlands: the occurrence of integrons (int1–2) and associated resistance genes (sul1–3, qacEΔ1)
PublicationThe aim of this study was to analyze the occurrence of sulfonamide resistance genes (sul1–3) and other genetic elements as antiseptic resistance gene (qacEΔ1) and class 1 and class 2 integrons (int1–2) in the upper layer of substrate and in the effluent of microcosm constructed wetlands (CWs) treating artificial wastewater containing diclofenac and sulfamethoxazole (SMX), which is a sulfonamide antibiotic. The bacteria in the substrate...
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Antibiotic Resistance of Uropathogens Isolated from Patients Hospitalized in District Hospital in Central Poland in 2020
PublicationThe aim of this study was to determine antibiotic resistance patterns and the prevalence of uropathogenes causing urinary tract infections (UTIs) in patients hospitalized in January–June 2020 in central Poland. Antimicrobial susceptibility testing was performed using the disk-diffusion method. Escherichia coli (52.2%), Klebsiella pneumoniae (13.7%), Enterococcus faecalis (9.3%), E. faecium (6.2%), and Proteus mirabilis (4,3%) were...
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Antibiotic resistance in Staphylococcus aureus strains isolated from cows with mastitis in the eastern Poland and analysis of susceptibility of resistant strains to alternative non-antibiotic agents: lysostaphin, nisin and polymyxin B.
PublicationThe aim of the studies was analysis of resistance of Staphylococcus aureus isolates from bovine mastitis in eastern part of Poland to a set of 20 antibiotics and three alternative agents: lysostaphin, nisin and polymyxin B. Eighty-six out of 123 examined isolates were susceptible to all of 20 tested antibiotics (70 %). The highest percentage of resistance was observed in the case of β-lactam antibiotics: amoxicillin (n=22, 17.9...
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CYP3A4 overexpression enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
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Metabolic transformations of antitumor imidazoacridinone, C-1311, with microsomal fractions of rat and human liver
PublicationWykazano, że enzymatyczna aktywacja jest konieczna dla aktywności biologicznej pochodnej C-1311 (Symadex R), która znajduje się w II fazie badań klinicznych. Zbadano przemiany enzymatyczne tego związku w obecności frakcji enzymatycznych mikrosomalnych komórek wątroby szczura i ludzkiej. Badania te wykazały, że związek C-1311 jest bardziej podatny na przemiany w obecności frakcji mikrosomalnej niż S9 i cytozolowej. Inkubacja związku...
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The role of cytochrome P450 reductase (CPR) in metabolism of potent nitroacridine antitumor, C-1748
PublicationCelem pracy było poznanie molekularnego mechanizmu działania pochodnych 9-amino-1-nitroakrydyny. Zbadano przemiany enzymatyczne tych związków w różnych układach enzymatycznych: I. Szczurza frakcja mikrosomalna z reduktazą cytochromu P450. II. Rekombinantowe izoenzymy cytochromu P450 z wysokim i niskim poziomem reduktazy cytochromu P450. III. Frakcje mikrosomalne dzikiego typu oraz pozbawione genu kodującego reduktazę cytochromu...
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Metabolic transformations of antitumor imidazoacridinone, C-1311, with microsomal fractions of rat and human liver
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CYP3A4 overexpressin enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
PublicationW pracy badano wpływ nadekspresji izoenzymu CYP3A4 na cytotoksyczność i odpowiedź komórkową indukowaną przez przeciwnowotworową pochodną triazoloakrydonu w modelowym układzie komórek CHO: dzikego typu, z nadekspresją reduktazy cytochromu P450 (CHO-HR) oraz z koekspresją reduktazy i izoenzymu CYP3A4 (CHO-HR-3A4). Wykazano, że komórki CHO wykazywały różną wrażliwość na badany związek, a linia CHO-HR okazała się najbardziej wrażliwa,...
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The products of electro- and photochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinone derivatives
PublicationBadano reakcje elektrochemicznego utleniania 2-hydroksyakrydonu, związku modelowego aktywnych przeciwnowotworowo pochodnych imidazoakrydonu. Do badań zastosowano metody woltamperometrii cyklicznej, metodę spektroelektrochemiczną oraz elektrolizę przy kontrolowanym potencjale. Badano też reakcje fotochemicznego utleniania. Badania prowadzono w ramach szerszego problemu poznania przemian aktywacji metabolicznej pochodnych hydroksyakrydonu...
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Electrochemical formation of the adduct between antitumor agent C_1311 and DNA nucleoside dG. 75.
PublicationPrzyjmuje się, że metaboliczna aktywacja przeciwnowotworowej pochodnej C_1311 jest procesem koniecznym dla jej aktywności przeciwnowotworowej. Wykazano wcześniej, że taka aktywacja prowadzi do kowalencyjnego wiązania się leku z DNA w komórce nowotworowej. Aby zbadać molekularny mechanizm powyższej reakcji metabolicznej przeprowadzono badania elektrochemicznego utleniania pochodnej C_1311. Wykazano w pracy, że dwa produkty elektrochemicznego...
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The effect of new non-cross resistant antitumor agents on the energy state of human erythrocytes
PublicationPrzebadano pochodne benzoperimidynowe i antrapirydonowe odnośnie ich wpływu na stan energetyczny ludzkich erytrocytów. Stwierdzono, że poziom nukleotydów jak i wartość AEC erytrocytów nie zmienił się w ciągu 24 h inkubacji z powyższymi związkami. Jest to wynik obiecujący w odniesieniu do ich zastosowania jako związków aktywnych w pokonywaniu oporności wielolekowej.
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Natural carbon-based quantum dots and their applications in drug delivery: A review
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The significance of lumican expression in ovarian cancer drug-resistant cell lines
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Magnetic Silica Nanotubes: Synthesis, Drug Release, and Feasibility for Magnetic Hyperthermia
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Multi‐wall carbon nanotubes – a vehicle for targeted Irinotecan drug delivery
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Antimicrobial peptides (AMPs) as drug candidates: a patent review (2003–2015)
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Chemometric Evaluation of THz Spectral Similarity for the Selection of Early Drug Candidates
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The impact of lipophilicity on environmental processes, drug delivery and bioavailability of food components
PublicationLipophilic properties of the compound allow to predict its fate in living organisms and to propose the models of chemicals transport and accumulation in the ecosystem. Lipophilicity is also useful as the characteristic of chemicals in respect to their optimal attributes for specific biological and non-biological tasks. The lipophilicity descriptors define the potency of endo- and xenobiotics to metabolic transformations and their...
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pH-dependent composite coatings for controlled drug delivery system - Review
PublicationNowadays in case of long-term implants, the most common postoperative complications are bacterial infections, which in consequence may provoke loos- ening of the implants in the primary phase of stabilization. Bacterial infections are currently the most frequent cause of revision surgery of the implants such as hip joint endoprosthesis, knee joint endoprosthesis and dental implants. In order to provide the local and long-term antibacterial...
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Single-wall carbon nanotubes based anticancer drug delivery system
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Influence of Escherichia coli on Expression of Selected Human Drug Addiction Genes
PublicationThe impact of enteric microflora on the expression of genes associated with cocaine and amphetamine addiction was described. Human genome-wide experiments on RNA transcripts expressed in response to three selected Escherichia coli strains allowed for significant alteration (p > 0.05) of the linear regression model between HT-29 RNA transcripts associated with the KEGG pathway:hsa05030:Cocaine addiction after 3 h stimulation with...
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Improvement of the resistance to oxidation of the ecological greases by the additives
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A parametric method for evaluation of resistance of swath ships
PublicationArtykuł zawiera sformułowania metody parametrycznej służącej do wyznaczania oporu kadłuba statku o konfiguracji swath. Metodę opracowano opierając się na rezultatach obliczeń numerycznych, uzyskanych metodami strukturalnymi, wywiedzionymi ze sformułowań teoretycznej hydromechaniki okrętu, wykonanych na dostatecznie licznej serii kształtów kadłuba, o systematycznie uzmiennianych parametrach kształtu. Następnie przedstawiono rezultaty...
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Tire rolling resistance measurements on the road and in the laboratory
PublicationW pracy przedstawiono stanowisko bębnowe do badania oporu toczenia opon samochdowych w warunkach laboratoryjnych. Zaprezentowano także przyczepę dynamometryczną do badania oporu toczenia opon samochodowych w warunkach drogowych. Stanowisko bębnowe i przyczepa zosały zbudowane w Katedrze Pojazdów i Maszyn Roboczych Politechniki Gdańskiej. Omówiono wpływ wzdłużnego pochylenia drogi i naporu powietrza na badane koło na dokładność...
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Static puncture resistance of non-woven geotextiles
PublicationBadania cech fizycznych i wytrzymałościowych geowóknin separcyjnych i osłonowych. Analiza wyników badań oporu na przebicie statycze metodą CBR, dla różnych rodzajów geowłóknin, próbek pozyskanych z terenu (po wbudowaniu w nasyp)i kontrolnych.
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Determination of the transverse resistance characteristics in railway track
PublicationW pracy przedstawiono problem oporów poprzecznych podsypki z punktu widzenia budowy, utrzymania oraz bezpieczeństwa w eksploatacji toru kolejowego. Zaprezentowano różne sposoby analitycznego podejścia do badanego zjawiska na przykładzie modeli matematycznych spotykanych w literaturze. Scharakteryzowano aktualny stan badań doświadczalnych związanych z oporami poprzecznymi. Omówiono różne sposoby prowadzenia takich badań w eksploatowanych...
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The Resistance of Polyethersulfone Membranes on the Alkaline Cleaning Solutions
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“The Guardians of the Truth”: Journalists’ Resistance to the Algorithmization of Journalism
PublicationRegardless of the term used, be it “robot journalism,” “automated journalism,” “algorithmic journalism” or “machine-written journalism,” the process of automatic content creation and distribution is progressing in the newsrooms. Meanwhile, exercising control over the creation and distribution of news is considered a fundamental element of journalists’ professional identity. The article presents the results of research on the perception...
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Examination of the epoxy coating system's resistance to Corrobill
PublicationThe tests of the influence of the surface cleaning agent on the epoxy coating were carried out. Electrochemical and corrosion tests were carried out. The effect of the preparation on the adhesion and hardness of the tested coating was tested.
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Comparison of selected parametric methods for prediction of inland waterways ship hull resistance in towing tank test
PublicationIn the paper selected approximate methods for calculation of inland waterways ship resistance and their verification by towing tests, compared on the example of a small urban ferry, are presented. The test results are made for both the bare hull and the hull with appendages (skeg, azimuthal propeller). Significant differences between results of the theoretical methods and experimental ones, especially in the case of the model with...