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Search results for: antitumor drug resistance
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Novel Nystatin A1 derivatives exhibiting low host cell toxicity and antifungal activity in an in vitro model of oral candidosis
PublicationOpportunistic oral infections caused by Candida albicans are frequent problems in immunocompromised patients. Management of such infections is limited due to the low number of antifungal drugs available, their relatively high toxicity and the emergence of antifungal resistance. Given these issues, our investigations have focused on novel derivatives of the antifungal antibiotic Nystatin A1, generated by modifications at the amino...
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Deep slot effect in the squirrel-cage induction motors with scalar (V/F) control
PublicationQualitative characteristics of the electrical drive considerably depend on identification accuracy of math model parameters. In particular, it is depend on detection accuracy of stator active resistance r1 that is used in calculation of flux linkages, rotary speed in sensorless control systems. Paper provides analysis of influence of stator deep slot effect to stator active resistance value
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Synthesis, characterization, and interactions of single-walled carbon nanotubes modified with doxorubicin with Langmuir–Blodgett biomimetic membranes
PublicationThe synthesis, characterization, and the influence of single-walled carbon nanotubes (SWCNTs) modified with an anticancer drug doxorubicin (DOx) on the properties of model biological membrane as well as the comparison of the two modes of modification has been presented. The drug was covalently attached to the nanotubes either preferentially on the sides or at the ends of the nanotubes by the formation of hydrazone bond. The efficiency...
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In vivoevaluation of the CB1allosteric modulator LDK1258 reveals CB1-receptor independent behavioral effects
PublicationIn the present study, we examined whether LDK1258, which produces strong CB1receptor allosteric effects ininvitroassays, would elicitin vivoeffects consistent with allosteric activity. In initial studies, LDK1258 reducedfood consumption and elicited delayed antinociceptive effects in the chronic constrictive injury of the sciaticnerve (CCI) model of neuropathic pain, which unexpectedly emerged 4 h post-injection. UPLC-MS/MS analysisquantified...
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Electrochemistry/mass spectrometry (EC/MS) for fast generation and identification of novel reactive metabolites of two unsymmetrical bisacridines with anticancer activity.
PublicationThe development of a new drug requires knowledge about its metabolic fate in a living organism, regarding the comprehensive assessment of both drug therapeutic activity and toxicity profiles. Electrochemistry (EC) coupled with mass spectrometry (MS) is an efficient tool for predicting the phase I metabolism of redox-sensitive drugs. In particular, EC/MS represents a clear advantage for the generation of reactive drug transformation...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublicationThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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Simple Measurement Method for Resistive Sensors Based on ADCs of Microcontrollers
PublicationA new, complete measurement method for resistance measurement of resistive sensors for systems based on microcontrollers equipped with analog-to-digital converters (ADCs) is proposed. The interface circuit consists of only four resistors, including a resistive sensor and a reference resistor, connected directly to the microcontroller pins. It is activated only during measurements, which significantly reduces power consumption....
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Fluctuation-enhanced and conductometric gas sensing with nanocrystalline NiO thin films: A comparison
PublicationNanocrystalline thin films of NiO were prepared by advanced reactive gas deposition, and their responses to formaldehyde, ethanol and methane gases were studied via fluctuation-enhanced and conductometric methods Thin films with thicknesses in the 200–1700-nm range were investigated in as-deposited form and after annealing at 400 and 500 °C. Morphological and structural analyses showed porous deposits with NiO nanocrystals having...
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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublicationA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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Development of different methods for drugs and psychoactive substances extraction from hair samples and their identification based on HPLC-ESI-QTOF analysis
PublicationOver the past decade, the use of non-controlled designer drugs and drug of abuse has rapidly increased. Hair, as a human matrix, enables detection of drugs incorporated into its structure. Studies of presence and identification of drug metabolites in human hair samples has been performed using liquid chromatography electrospray ionization quadrupole time of flight mass spectrometry (HPLC-ESI-QTOF-MS) with steady alternation of...
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Self-Association of Amphotericin B: Spontaneous Formation of Molecular Structures Responsible for the Toxic Side Effects of the Antibiotic
PublicationAmphotericin B (AmB) is a lifesaving antibiotic used to treat deep-seated mycotic infections. Both the pharmaceutical activity and highly toxic side effects of the drug rely on its interaction with biomembranes, which is governed by the molecular organization of AmB. In the present work we present detailed analysis of self-assembly of AmB molecules in different environments, interesting from the physiological standpoint, based...
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Determination of Earth Pressure and Displacement of the Retaining Structure According to the Eurocode 7-1
PublicationComparative analysis of standard guidelines and findings given in EC7-1 and in Polish Standard PN-83/B-03010. Discussed guidelines concerning active and passive earth pressure as well as at rest pressure state. Wall displacement causing limit states of earth pressure and resistance. Interactive assumptions concerning intermediate earth pressure and resistance values. Conclusions and final remarks.
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High performance LaNi1-xCoxO3-δ (x = 0.4 to 0.7) infiltrated oxygen electrodes for reversible solid oxide cells
PublicationOxygen electrodes prepared by infiltration of yttria stabilized zirconia backbone with Ce0.8Gd0.2O1.95 barrier layer and LaNi1-xCoxO3-δ (x=0.4 to 0.7) catalyst for application in reversible solid oxide cells have been studied. The effect of temperature and Ni:Co ratio on their phase composition, microstructure and electrochemical properties are discussed. It was shown that oxygen electrodes infiltrated with LaNi0.5Co0.5O3-δ had...
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Determination of bromhexine and its metabolites in equine serum samples by liquid chromatography – Tandem mass spectrometry: Applicability to the elimination study after single oral dose
PublicationBromhexine (BH), expectorant used in the treatment of respiratory disorders associated with viscid or excessive mucus, is not permitted for use in the competing horse by many authorities in horseracing and Olympic disciplines. Metabolic studies are of the great importance in anti-doping field because they allow for updating the selection of the most appropriate markers for prohibited substances, such as metabolites present at higher...
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Highly Conserved Homotrimer Cavity Formed by the SARS-CoV-2 Spike Glycoprotein: A Novel Binding Site
PublicationAn important stage in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) life cycle is the binding of the spike (S) protein to the angiotensin converting enzyme-2 (ACE2) host cell receptor. Therefore, to explore conserved features in spike protein dynamics and to identify potentially novel regions for drugging, we measured spike protein variability derived from 791 viral genomes and studied its properties by molecular...
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Effect of MAO coatings on cavitation erosion and tribological properties of 5056 and 7075 aluminum alloys
PublicationTwo ceramic coatings have been applied on 5056 and 7075 aluminum alloy by microarc oxidation (MAO) technology. The mass losses, surface morphologies and the phase constituents of the MAO coatings before and after cavitation tests were examined by means of digital scales, scanning electron microscopy (SEM) and X-ray diffraction (XRD), respectively. In order to assess the impact of the mechanical properties of the surface layer on...
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Hydrogen effects in duplex stainless steel welded joints - electrochemical studies
PublicationIn this work results on the influence of hydrogen on passivity and corrosion resistance of 2205 duplex stainless steel (DSS) welded joints are described. The results were discussed by taking into account three different areas on the welded joint: weld metal (WM), heat-affected zone (HAZ) and parent metal. The corrosion resistance was qualified with the polarization curves registered in a synthetic sea water. The conclusion is that,...
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Review on Current Status of Echinocandins Use
PublicationFungal infections are rising all over the world every year. There are only five medical compound classes for treatment: triazoles, echinocandins, polyenes, flucytosine and allylamine. Currently, echinocandins are the most important compounds, because of their wide activity spectrum and much lower sides effects that may occur during therapy with other drugs. Echinocandins are secondary metabolites of fungi, which can inhibit the...
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Pharmaceutical applications of surfactants
PublicationIn this study we focused on biological activity of various surfactants. According to our research, they con act both as carriers as well as therapeutic agents. Depending on their concentration, they can create different structures in a solution, which influence their properties. Liposomes have a significant role in drug delivery system. Surfactants in from of bilayer are analogous to natural biological cell membrane.
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Further development of the poroelastic road surface within the new Polish project SEPOR
PublicationRoad surfaces have a direct impact on noise generated by rolling tyres, the main and dominant source of noise of moving vehicles. Road surface texture, porosity and stiffness/elasticity govern the pavement contribution to tyre/road noise the most. An experimental PoroElastic Road Surface (PERS) is a wearing course with a high content of interconnected voids (pores) and with an elastic behavior due to the use of small particles...
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The retrofitting of ships by applying retractable bow hydrofoils: a case study
PublicationIncreasing environmental requirements and a relatively long ship life of 30 years mean more attention is needed to retrofit existing ships. One possibility is using hydrofoils to reduce the ship’s resistance and improve comfort and safety in rough sea conditions. This study investigates the influence of retractable bow hydrofoils on the seakeeping performance and operational conditions of a selected case study vessel (V-shaped...
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Usage of Two-Center Basis Function Neural Classifiers in Compact Smart Resistive Sensors
PublicationA new solution of the smart resistance sensorwith the Two-Center Basis Function (TCBF) neuralclassifier, for which the resistance sensor is a component ofan anti-aliasing filter of an ADC is proposed. Thetemperature measurement procedure is based on excitationof the filter by square impulses, sampling time response ofthe filter and processing measured voltage values by theTCBF classifier. All steps of the measurement procedure...
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UV-Light-Induced Fluctuation Enhanced Sensing by WO3-Based Gas Sensors
PublicationWO3-based gas sensors were investigated under UV-light irradiation and at different working temperatures with the object of achieving superior sensitivity and selectivity. Resistance fluctuations in the WO3 layer were studied together with dc resistance measurements. The data were taken in synthetic air, ethanol, nitrogen dioxide, and mixtures of these gases. We conclude that UV irradiation can easily be applied to enhance the...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublicationZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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Potential of Liquid Biopsy in Papillary Thyroid Carcinoma in Context of miRNA, BRAF and p53 Mutation
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Genetic Determinants of Vitamin D-Related Disorders; Focus on Vitamin D Receptor
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Morphine and methadone pre-exposures differently modify brain regional Fos protein expression and locomotor activity responses to morphine challenge in the rat
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Population analysis to assess the influence of age and body weight on pharmacokinetics and pharmacodynamics of dexmedetomidine in New Zealand White rabbits
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Acute and subacute (28-Day) toxicity studies of ionic liquid, didecyldimethyl ammonium acesulfamate, in rats
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The pharmacokinetics of propofol in ICU patients undergoing long-term sedation
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The quantification of reticulocyte maturation and neocytolysis in normal and erythropoietin stimulated rats
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Targeting shelterin proteins for cancer therapy.
PublicationAs a global health challenge, cancer prompts continuous exploration for innovative therapies that are also based on new targets. One promising avenue is targeting the shelterin protein complex, a safeguard for telomeres crucial in preventing DNA damage. The role of shelterin in modulating ataxia- telangiectasia mutated (ATM) and ataxia-telangiectasia and Rad3-related (ATR) kinases, key players in the DNA damage response (DDR),...
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Complexation of Bioelements and Toxic Metals by Polyphenolic Compounds - Implications for Health
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Protective Effect of Aronia Melanocarpa Polyphenols on Cadmium Accumulation in the Body: A Study in a Rat Model of Human Exposure to this Metal
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Aqueous Extracts of Selected Potentilla Species Modulate Biological Activity of Human Normal Colon Cells
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New Insights into Dietary Supplements Used in Sport: Active Substances, Pharmacological and Side Effects
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Antioxidants as a Potential Preventive and Therapeutic Strategy for Cadmium
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Prolonged Quercetin Administration Diminishes the Etoposide-Induced DNA Damage in Bone Marrow Cells of Rats
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Rheological Characteristics of Novel Meloxicam-Loaded Complex Organogels Based on Fumed Silica and Poloxamer
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Current status of liposomal porphyrinoid photosensitizers
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Vitamin D Metabolism Gene Polymorphisms and Their Associated Disorders: A Literature Review
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Genotoxicity of selected pharmaceuticals, their binary mixtures, and varying environmental conditions – study with human adenocarcinoma cancer HT29 cell line
PublicationPharmaceutical residues are present in the environment in mixtures and their adverse effects may also result from interactions that occur between compounds. Studies presented in this work focus on genotoxicity of pharmaceuticals from different therapeutic groups in mixtures and in individual solutions impacted with different environmental conditions assessed using comet assay (alkaline approach). Binary mixtures of pharmaceuticals...
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublicationCarnosine, 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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Essential Oils, Silver Nanoparticles and Propolis as Alternative Agents Against Fluconazole Resistant Candida albicans, Candida glabrata and Candida krusei Clinical Isolates
PublicationDevelopment of effective and safe therapeutic treatment of fungal infections remains one of the major challenge for modern medicine. The aim of presented investigation was to analyze the in vitro antifungal activity of selected essential oils, ethanolic extracts of propolis and silver nanoparticles dropped on TiO2 against azole-resistant C. albicans (n = 20), C. glabrata (n = 14) and C. krusei (n = 10) clinical isolates. Among...
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Cavitation Erosion – Phenomenon and Test Rigs
PublicationThe cavitation and cavitation erosion phenomenon have been shortly presented. The main four types of test rigs to investigate the cavitation erosion resistance have been shown. Each type of test design is described and an example of a design is shown. A special attention has been payed to the designs described in the International ASTM Standards: a vibratory design and a cavitating jet cell. There was shown that the design of a...
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A measurement method for lossy capacitive relative humidity sensors based on a direct sensor-to-microcontroller interface circuit
PublicationA new time-domain measurement method for determining the capacitance and resistance values of lossy relative humidity capacitive sensors is presented. The method is based on a direct sensor-to-microcontroller interface for microcontrollers with internal analog comparators and timers. The interface circuit consists only of four reference resistors (two reference resistors if a microcontroller includes a voltage reference source),...
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Impact of selected drugs and their binary mixtures on the germination of Sorghum bicolor (sorgo) seeds
PublicationThe aim of this study was to assess the toxicological potential of binary drug mixtures and individual drugs under different pH conditions with different inorganic ion additions on the germination of Sorghum bicolor (sorgo) seeds. To assess whether the given drug mixtures were more phytotoxic than the individual compounds, concentration addition (CA) and independent action (IA) approaches were applied to estimate the predicted...
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Analytical approach for membrane action in laterally-restrained reinforced concrete square slabs under uniformly distributed loads
PublicationLaterally-restrained reinforced concrete slabs can mobilise compressive membrane action and subsequent tensile membrane action under extreme loading conditions, thereby enhancing the load resistance under uniformly distributed loads. Previous analytical study focuses primarily on tensile membrane action in simply-supported slabs. This paper describes an analytical approach for membrane action in laterally-restrained square slabs....