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Wyniki wyszukiwania dla: antitumor drug resistance
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Impact resistance of plain and twill fabric in GFRP measured by active thermography
PublikacjaThis paper discusses the impact resistance of glass-fibre reinforced polymer (GFRP) composites depending on the type of reinforcement – plain or twill weave. The values of impact energy were: 3J, 10J and 15J. Specimens featuring twill weave transferred higher force during the impact as compared with plain weave specimens. It was observed that an increase of impact energy was accompanied by an increase of the disproportion in...
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Journal of Global Antimicrobial Resistance
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Mechanisms of azole resistance among clinical isolates of Candida glabrata in Poland
PublikacjaCandida glabrata is currently ranked as the second most frequently isolated aetiological agent of human fungal infections, next only to Candida albicans. In comparison with C. albicans, C. glabrata shows lower susceptibility to azoles, the most common agents used in treatment of fungal infections. Interestingly, the mechanisms of resistance to azole agents in C. albicans have been much better investigated than those in C. glabrata....
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Antibiotic resistance, virulence, and phylogenetic analysis of Escherichia coli strains isolated from free-living birds in human habitats
PublikacjaWild birds can be colonized by bacteria, which are often resistant to antibiotics and have various virulence profiles. The aim of this study was to analyze antibiotic resistance mechanisms and virulence profiles in relation to the phylogenetic group of E. coli strains that were isolated from the GI tract of wildfowl. Out of 241 faecal samples, presence of E. coli resistant to a cephalosporin (ESBL/AmpC) was estimated for 33 isolates...
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Evaluation of Wear Resistance of Ti alloys used for elements friction of knee endoprosthesis
PublikacjaThe paper presents research results of resistance to abrasive wear of titanium alloys: Ti6Al4V (commonly used) and Til3Nb13Zr (alloy of new generation) in association with polyethylene (UHMW-PE) predisposed for elements on pair of the knee endoprosthesis. The results were analysed from the point of possibility of an use of new generation titanium alloys as components of such implants. The tests of resistance to abrasive wear of...
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Drug Research
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DRUG DELIVERY
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DRUG SAFETY
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Drug Topics
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Field Evaluation of High Modulus Asphalt Concrete Resistance to Low-Temperature Cracking
PublikacjaHigh-modulus asphalt concrete has numerous advantages in comparison to conventional asphalt concrete, including increased resistance to permanent deformations and increased pavement fatigue life. However, previous studies have shown that the construction of road pavements with High Modulus Asphalt Concrete (HMAC) may significantly increase the risk of low-temperature cracking. Those observations were the motivation for the research...
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Thin layer chromatography in drug discovery process
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Transport deficiency is the molecular basis of Candida albicans resistance to antifungal oligopeptides
Publikacja(FMDP), an inhibitor of glucosamine-6-phosphate synthase, exhibited growth inhibitory activity against Candida albicans, with minimal inhibitory concentration values in the 0.05–50 mg/L range. Uptake by the peptide permeases was found to be the main factor limiting an anticandidal activity of these compounds. Di- and tripeptide containing FMDP (F2 and F3) were transported by Ptr2p/Ptr22p peptide transporters (PTR) and FMDP-containing...
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The Effect of Posaconazole, Itraconazole and Voriconazole in the Culture Medium on Aspergillus fumigatus Triazole Resistance
PublikacjaTriazoles are the only compounds used as antibiotics in both medicine and agriculture. The presence of triazoles in the environment can contribute to the acquisition of azole resistance among isolates of Aspergillus fumigatus. The objective of this study was to investigate the effect of A. fumigatus exposure to triazoles on susceptibility to these compounds. Seventeen triazole-resistant and 21 triazole-sensitive A. fumigatus isolates...
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Intercalation of imidazoacridinones to DNA and its relevance to cytotoxicand antitumor activity
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The interaction of antitumor 1-nitroacridines with DNA in cell-free systems
PublikacjaUzyskano nowe pochodne 1-nitro i 3-nitroakrydyny wykazujące zdolność do specyficznego cięcia DNA w miejscach bezzasadowych. Z użyciem oligonukleotydu z indukowanym miejscem bezzasadowym potwierdzono taką aktywność u obu otrzymanych pochodnych.
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Covalent conjugation of graphene oxide with methotrexate and its antitumor activity
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Akrydyny jako związki aktywne przeciwnowotworowo = Acridines as antitumor drugs
PublikacjaAkrydyny należą do grupy policyklicznych związków heteroaromatycznych. Wykazują szeroki zakres aktywności biologicznej obejmujący aktywność przeciwpierwotniakową, przeciwbakteryjną,przeciwwirusową i przeciwnowotworową. Pochodne akrydyny o działaniu przeciwnowotworowym wykazują zróżnicowany mechanizm działania na poziomie molekularnym. Z uzyskanych dotychczas danych wynika, że jednym z podstawowych etapów działania jest tworzenie...
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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublikacjaChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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The Interaction of Heptakis (2,6-di-O-Methyl)-β-Cyclodextrin with Mianserin Hydrochloride and Its Influence on the Drug Toxicity
PublikacjaOne tetracyclic antidepressant, mianserin hydrochloride (MIA), has quite significant side effects on a patients’ health. Cyclodextrins, which are most commonly used to reduce the undesirable features of contained drugs within their hydrophobic interior, also have the potential to alter the toxic behavior of the drug. The present paper contains investigations and the characteristics of interaction mechanisms for MIA and the heptakis...
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Resistance of Escherichia coli and Enterococcus spp. to selected antimicrobial agents present in municipal
PublikacjaIn this study, the susceptibility to erythromycin (E) and to trimethoprim/sulfamethoxazole (SXT) among isolates of Enterococcus spp. and Escherichia coli was tested, respectively. Both fecal indicators were detected and isolated from raw(RW) and treated wastewater (TW) as well as from samples of activated sludge (AS) collected in a local wastewater treatment plant (WWTP). Biodiversity of bacterial community in AS was also monitored...
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Effects of the preheating laser treatment on microstructure and corrosion resistance of Ti6Al4V bioalloy
PublikacjaThe laser remelting of the Ti6Al4V alloy was made on specimens pre-heated at elevated temperatures. The laser treatment effected in change of microstructures of surface layers and an appearance of blisters and numerous cracks. The corrosion tests demonstrated the decrease in corrosion resistance for each preheating temperature. The observed effects were attributed to negative influence of excessive compressive stresses with no...
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Effect of the Post-Weld Surface Condition on the Corrosion Resistance of Austenitic Stainless Steel AISI 304
PublikacjaSurfaces of welded elements made of corrosion-resistant (stainless) steels develop temper colours. The removal of thickened oxide layers off steels exposed to temperatures below 300°C is necessary and entails the restoring of high corrosion resistance of the stainless steel. The article presents tests concerned with the effect of a method applied to remove post-weld temper on the corrosion resistance of austenitic stainless steel...
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Influence of bitumen type on cracking resistance of asphalt mixtures used in pavement overlays
PublikacjaCracking is one of the predominant distresses occurring in flexible pavements, especially in old pavements that were rehabilitated with an asphalt overlay. In such cases asphalt mixtures should be designed to ensure high resistance to reflective cracking because new asphalt layers are exposed to existing cracks of the old pavement. The nature of these cracks can be various (transverse, longitudinal as well as crazy cracking). One...
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Using anticipatory and drug-evoked appetitive ultrasonic vocalization for monitoring the rewarding effect of amphetamine in a rat model of drug self-administration
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The Significance of MicroRNAs Expression in Regulation of Extracellular Matrix and Other Drug Resistant Genes in Drug Resistant Ovarian Cancer Cell Lines
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Function and Frustration of Multi-Drug ABC Exporter Protein and Design of Model Proteins for Drug Delivery Using Protein Hydration Thermodynamics
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Multi-objective weather routing of sailboats considering wave resistance
PublikacjaThe article presents a method to determine the route of a sailing vessel with the aid of deterministic algorithms. The method assumes that the area in which the route is to be determined is limited and the basic input data comprise the wind vector and the speed characteristic of the vessel. Compared to previous works of the authors, the present article additionally takes into account the effect of sea waves with the resultant resistance...
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The influence of inflation pressure and ambient temperature on the value of the truck tires rolling resistance
PublikacjaThe articlediscusses the effect of inflation pressure and the ambient temperature on the value of the rolling resistance of truck tires which directly translates into fuel consumption. For this purpose, a series of measurements was made at two ambient temperatures (at 25°C and -15°C), using different pumping pressures.
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Diversity of fecal coliforms and their antimicrobial resistance patterns in wastewater treatment model plant.
PublikacjaThe occurrence of resistance patterns among wastewater fecal coliforms was determined in the study. Susceptibility of the isolates was tested against 19 antimicrobial agents: aminoglycosides, aztreonam, carbapenems, cephalosporines, b-lactam/b-lactamase inhibitors, penicillines, tetracycline, trimethoprim/sulfamethoxazole, and fluoroquinolones. Additionally the removal of resistant isolates was evaluated in the laboratory-scale...
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An Influence of Factors of Flow Condition, Particle and Material Properties on Slurry Erosion Resistance
PublikacjaThe degradation of materials due to slurry erosion is the serious problem which occurs in the power industries. The paper presents actual knowledge about an influence of individual factors connected with flow conditions, particles and material properties on the slurry erosion resistance. Among the factors connected with operating conditions, an influence of impact angle, and velocity of impact, particle concertation and liquid...
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A new method of fault loop resistance measurement in low voltage systems with residual current devices
PublikacjaThis paper presents a new method of fault loop resistance measurement in low voltage systems with residual current devices. The method enables measuring fault loop resistance without nuisance tripping of residual current devices, by application an unconventional waveform of measurement current. It is important for proper verification of the effectiveness of protection against electric shock.
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublikacjaDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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Effect of annealing temperature on slurry erosion resistance of ferritic X10CrAlSi18 steel
PublikacjaIn the present work, the slurry erosion tests were carried out to investigate the influence of heat treatment on slurry erosion process of ferritic X10CrAlSi18 stainless steel using a slurry pot test rig. X10CrAlSi18 stainless steel was tested in as-received condition and after annealing at three different temperatures: 600°C, 800°C and 1000°C. Degradation of materials due to slurry erosion depends on many factors connected with...
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Effect of Processing Parameters on Strength and Corrosion Resistance of Friction Stir-Welded AA6082
PublikacjaThe friction stir welding method is increasingly attracting interest in the railway sector due to its environmental friendliness, low cost, and ease of producing high-quality joints. Using aluminum alloys reduces the weight of structures, increasing their payload and reducing fuel consumption and running costs. The following paper presents studies on the microstructure, strength, and corrosion resistance of AA6082 aluminum alloy...
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Acid–Base Equilibrium and Self-Association in Relation to High Antitumor Activity of Selected Unsymmetrical Bisacridines Established by Extensive Chemometric Analysis
PublikacjaUnsymmetrical bisacridines (UAs) represent a novel class of anticancer agents previously synthesized by our group. Our recent studies have demonstrated their high antitumor potential against multiple cancer cell lines and human tumor xenografts in nude mice. At the cellular level, these compounds affected 3D cancer spheroid growth and their cellular uptake was selectively modulated by quantum dots. UAs were shown to undergo metabolic...
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Buckling resistance of a metal column in a corrugated sheet silo - experiments and non-linear stability calculations
PublikacjaThe results of experimental and numerical tests of a single corrugated sheet silo column’s buckling resistance are presented in this study. The experiments were performed in a real silo with and without bulk solid (wheat). A very positive impact of the bulk solid on the column buckling resistance occurred. The experimental results were first compared to the buckling resistance calculated by Eurocode 3 formulae. The comparison revealed that...
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The influence of applying supplementary web plates on structural joint moment resistance and rotational stiffness
PublikacjaContinual trend to simplify structural elements and find less time-consuming solutions on construction site as well as inevitable increase in labour costs determine for instance elimination of those technological steps that are difficult to automation. Welding additional reinforcements and web stiffeners is a great example of such a step. The method presented in EN 1993-1-8 [8] is a result of long-term studies focused on calculating...
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Induction of G2/M phase arrest and apoptosis of human pancreatic cancer BxPC-3 cells by potenet antitumor 1-nitroacridine derivative C-1748
PublikacjaPancreatic ductal adenocarcinoma (PDA) is among the most lethal human cancers, in part because it is insensitive to many chemotherapeutic drugs. Gemcitabine still remains the best chemotherapeutic agent available for the treatment of advanced pancreatic cancer. However, gemcitabine treatment results in only a marginal survival advantage. Thus, there is a strong need for the continuous development of novel therapeutic agents...
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Acridinone antitumor agents: C-1311, C-1330 and C-1305 are metabolized by flavin-containing monooxygenase isoenzymes: FMO1, FMO3 and FMO5 with different rates
PublikacjaRekombinantowe ludzkie monooksygenazy flawinowe: FMO1, FMO3, FMO5 indukują przemiany metaboliczne wybranych do badań pochodnych akrydonu. Biotransformacja związków C-1311, C-1330 i C-1305 przez FMO prowadzi do jednego produktu o strukturze N-tlenku. Wyniki badań wskazują, że najbardziej podatna na przemiany wobec FMO jest pochodna triazoloakrydonu C-1305. Wydaje się więc, że głównymi enzymami pierwszej fazy przemian metabolicznych...
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Determination of amikacin and ciprofloxacin by liquid chromatography with pre-column derivatization to evaluate sustained delivery of antibiotics from Drug-Eluting Biopsy Needle
PublikacjaDetermination of chosen antibacterial antibiotics: amikacin and ciprofloxacin was carried out by HPLC-UV after derivatization with 9-fluorenylmethyl chloroformate and in their native form by HPLC-MS/MS. Developed methods have been applied to control the kinetics of antibiotic release from polymer-based controlled drug delivery system.
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Feasibility study of a Raman spectroscopic route to drug detection
PublikacjaWe present an surface-enhanced Raman spectroscopy (SERS) approach for detection of drugs of abuse in whole human blood. We utilize a near infrared laser with 830 nm excitation wavelength in order to reduce the influence of fluorescence on the spectra of blood. However, regular plasmon resonance peak of plasmonic nanoparticles, such as silver or gold fall in a much lower wavelength regime about 400 nm. Therefore, we have shifted...
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SAMPLE-AND-HOLDING METHOD FOR GAS SENSING APPLIED FOR RESISTANCE GAS SENSORS
PublikacjaThe DC resistance of a Taguchi gas sensor is influenced by the ambient gas. To improve the selectivity and sensitivity of a sensor the fluctuation enhanced sensing (FES) was used. The paper proposes a novel methodology of utilizing FES technique that sample composition of an ambient atmosphere and hold it for further processing (sample-and-holding technique). The method uses the heated gas sensor to sample an ambient atmosphere...
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Metabolic transformation of antitumor agent C1311 with various fractions of rat liver.
PublikacjaWykazano, że enzymatyczna aktywacja jest konieczna dla aktywności bilogicznej pochodnej C-1311. Zbadano przemiany związku w obecności różnych frakcji enzymatycznych mikrosomalnych komórek wątroby szczura.Badania te wykazały, że związek C-1311 jest bardziej podatny na transformację pod wpływem frakcji aktywowanych enzymów mikrosomalnych (CYP1A, CYP2B, CYP3A i CYP4A) niż frakcji S9, cytozolowej czy mikrosomów nieaktywowanych. Związek...
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Synthesis and antitumor activity of conjugates of muramyldipeptide or normuramyldipeptide with hydroxyacridine/acridone derivatives
PublikacjaOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej pochodnymi hydroksyakrydyny/akrydonu i dwóch analogów modyfikowanych pochodnymi 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny. Tylko związki zawierające pochodne 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny wykazały wysoką aktywność cytotoksyczną badaną na 60 liniach ludzkich komórek nowotworowych, na nowotwór prostaty i AIDS-related lymphoma (ARL). Związek...
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Differential antitumor effects of vitamin D analogues on colorectal carcinoma in culture
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Interaction of antitumor triazoloacridone C-1305 and its analogs with telomeric DNA
PublikacjaBadaliśmy oddziaływanie pochodnej triazoloakrydonu C-1305 i jego bliskich analogów strukturalnych z oligonukleotydami zawierającycmi sekwencje telomerowe TTAGGG oraz oligonukleotydami sfałdowanymi w strukturę G-kwadrupleksu. Wykazaliśmy, że spośród badanych związków pochodna C-1305 wykazała największą specyficzność w stosunku do telomerowego DNA. Związek ten stabilizował także strukturę G-kwadrupleksu, podczas gdy jego analogi...
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Effect of Thermal Treatment and Erosion Aggressiveness on Resistance of S235JR Steel to Cavitation and Slurry
PublikacjaS235JR steel is used in many applications, but its resistance to the erosion processes has been poorly studied. To investigate this resistance, cavitation, and slurry erosion tests were conducted. These tests were carried out at different erosion intensities, i.e., different flow rates in the cavitation tunnel with a system of barricades and different rotational speeds in the slurry pot. The steel was tested as-received and after...
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Support for Employees with ASD in the Workplace Using a Bluetooth Skin Resistance Sensor–A Preliminary Study
PublikacjaThe application of a Bluetooth skin resistance sensor in assisting people with Autism Spectrum Disorders (ASD), in their day-to-day work, is presented in this paper. The design and construction of the device are discussed. The authors have considered the best placement of the sensor, on the body, to gain the most accurate readings of user stress levels, under various conditions. Trial tests were performed on a group of sixteen...
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Corrosion resistance examinations of Ti6Al4V alloy with the use of potentiodynamic method in Ringer`s and artificial saliva solutions
PublikacjaThe research results of corrosion resistance of the Ti6Al4V alloy in the simulated body fluids (SBF) are presented. The polished specimens have shown better corrosion resistance than grinded surfaces in both liquids. The artificial saliva has revealed more aggressive test solution than Ringer`s solution. The pitting tendency has been observed in Ringer`s solution for grinded specimens.
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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,...