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Search results for: DRUK%203D
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Effects of an immunosuppressive treatment on the rat prostate
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Lampa nienaftowa - FreeCAD
e-Learning CoursesFreeCAD jest uniwersalnym parametrycznym programem modelującym w przestrzeni 3D CAD, którego rozwój odbywa się wyłącznie według zasad Open Source (licencja LGPL) .FreeCAD jest przeznaczony bezpośrednio dla inżynierii mechanicznej i projektowania detali i produktów, ale mieści się również w szerszym zakresie zastosowań związanych z inżynierią, takich jak architektura, analiza elementów ukończonych, druk 3D i wiele pokrewnych. PS Kurs...
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved 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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Drukowanie trwałych elementów z tworzyw termoplastycznych w technologii FDM/FFF
PublicationDrukowanie detali z tworzyw sztucznych stanowi aktualnie jedną z najczęściej wykorzystywanych form druku 3D, która znajduje szerokie zastosowanie zarówno w obszarze amatorskim, jak i również przemysłowym. Omawiane w pracy zagadnienia dotyczą zasady działania oraz charakterystyki najważniejszych czynników technologii FDM/FFF. Przedstawiono najczęściej występujące błędy oraz defekty drukowanych elementów. Wskazano ponadto najważniejsze...
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Dietary intervention with beetroot juice during doxorubicin cancer chemotherapy in vivo reduces markers of oxidative stress
PublicationCancer chemotherapy with doxorubicin, despite high antitumor activity and broad spectrum of this drug, is on decline due to toxic side effects. The clinical efficacy of anthracyclines have continuously prompted the search for new adjuvants to alleviate undesirable side toxicity incurred by this group of cytostatics. The recent approaches involve the application of synthetic or purified natural antioxidants in combination with doxorubicin...
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublicationResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Intermolecular Interactions as a Measure of Dapsone Solubility in Neat Solvents and Binary Solvent Mixtures
PublicationDapsone is an effective antibacterial drug used to treat a variety of conditions. However, the aqueous solubility of this drug is limited, as is its permeability. This study expands the available solubility data pool for dapsone by measuring its solubility in several pure organic solvents: N-methyl-2-pyrrolidone (CAS: 872-50-4), dimethyl sulfoxide (CAS: 67-68-5), 4-formylmorpholine (CAS: 4394-85-8), tetraethylene pentamine (CAS:...
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Sustainable polymers targeted at the surgical and otolaryngological applications: Circularity and future
PublicationThe ongoing climate changes, high air and noise pollution have significant impact on humans’ health. This influence is especially visible in otolaryngology, which focuses on respiratory and hearing systems disfunctions. However, even though surgeries are done in response to diseases related to climate changes, they also have a negative impact on the environment, mostly connected with the inherence of single-use fossil fuel derived...
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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublicationProliferation and expansion of leukemia is driven by leukemic stem cells (LSCs). Multidrug resistance (MDR) of LSCs is one of the main reasons of failure and relapses in acute myeloid leukemia (AML) treatment. In this study, we show that maintaining HL-60 at low cell culture density or applying a 240-day treatment with anthrapyridazone (BS-121) increased the percentage of primitive cells, which include LSCs determining the overall...
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Activation Energy and Inclination Magnetic Dipole Influences on Carreau Nanofluid Flowing via Cylindrical Channel with an Infinite Shearing Rate
PublicationThe infinite shear viscosity model of Carreau fluid characterizes the attitude of fluid flow at a very high/very low shear rate. This model has the capacity for interpretation of fluid at both extreme levels, and an inclined magnetic dipole in fluid mechanics has its valuable applications such as magnetic drug engineering, cold treatments to destroy tumors, drug targeting, bio preservation, cryosurgery, astrophysics, reaction kinetics,...
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Peptydy penetrujące – rodzaje i mechanizmy przenikania przez błony komórkowe
PublicationPeptydy penetrujące z pewnością są wyjątkową i ciekawą grupą związków peptydowych. Zostały odkryte ponad dwadzieścia lat temu, ale wiedza na ich temat wciąż jest rozbudowywana. Liczne badania nad mechanizmami ich przenikania do wnętrza komórek pozwalają zrozumieć jakie cechy strukturalne warunkują ich zdolność do penetracji komórek. Wiedza ta pozwala na projektowanie nowych, bardziej efektywnych peptydów penetrujących., które mogą...
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Synthesis, structure characterization and thermal propertiesof [Zr<sub>6</sub>(μ<sub>3</sub>-O)<sub>4</sub>(μ<sub>3</sub>-OH)<sub>4</sub>(OOCCH<sub>2</sub><sup>t</sup>Bu)<sub>9</sub>(μ<sub>2</sub>-OH)<sub>3</sub>]<sub>2</sub>
PublicationTytułowy związek otrzymano w reakcji Zr(OiPr)4 z nadmiarem kwasu 3,3-dimetylobutyrowego. Rentgenowska analiza strukturalna została wykonana w temperaturze 103 i 153K. Struktury zawierają dimery podjednostek o wzorze: [Zr6(μ3-O)4(μ3-OH)4-(OOCCH2tBu)9] połączonych 6 mostkującymi grupami μ2-OH. Analiza zmiennotemperaturowych...
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Hel 2019 - video data - pedestrian, bicycles, vehicles
Open Research DataHel 2019 - video data - pedestrian, bicycles, vehicles
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Modelowanie polskiego podsystemu wytwarzania energii elektrycznej w programie MARKAL ze szczególnym uwzględnieniem Europejskiego Systemu Handlu Emisjami
PublicationArtykuł dotyczy problematyki emisji gazów cieplarnianych w Unii Europejskiej oraz działań mających na celu ich redukcję, w szczególności Europejskiego Systemu Handlu Emisjami (EU ETS). Model polskiego podsystemu wytwarzania energii elektrycznej, uwzględniający mechanizmy EU ETS, został opracowany za pomocą pakietu optymalizacyjnego MARKAL. Do modelu wprowadzono dane zebrane na podstawie dostępnych projektów, rozporządzeń i danych...
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Risking It All or Here Comes the Flood
PublicationThe professional reality is interdisciplinary! When city transformation and evolution starts, what are the tools for successful strategies for urban interventions? How does digital planning for digital fabrication processes look like? How dedicated are the new professionals? And how does this all influence the future of bridge design? More than 60 students representing various disciplines of built environment and working together...
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The youth in polish legations and government
PublicationUntil the 2015 elections, youth policy in Poland was treated as a separate domain. There is no uniform legal basis concerned with the matters of young people. Youth rights are dealt with in several articles of the Constitution of the Republic of Poland as well as a number of Acts: on Public Administration Branches, on the Education System, on Higher Education, on Employment Promotion and Labour Market Institutions, on NFZ General...
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Potential reduction of traffic noise by the means of increased fleet of electric vehicles using a combination of low-noise tyres and low-noise road surfaces
PublicationIn the future, the number of zero-emission vehicles like electric and plug-in hybrid vehicles (in electric mode) is expected to be a substantial part of the vehicle fleet. In Norway, such vehicles already account for approximately 20 % of all new cars sold. Since these vehicles emit negligible noise related to the power-train, the tyre/road noise is the dominating noise source. In the LEO project, tyres designed for such cars have...
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Analytical procedures for determination of cocaine and its metabolites in biological samples
PublicationThe dangerous effects and increased usage of illicit drugs have inspired the development of analytical methodologies. We based our review of analytical procedures for determination of cocaine (COC) and its metabolites on literature from the past two decades. Our main aim was to compare the capabilities of different analytical techniques. The diversity of matrices from which COC is determined (e.g., blood, hair, saliva, plasma,...
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Physical and Mechanical Evaluation of Silicone-Based Double-Layer Adhesive Patch Intended for Keloids and Scar Treatment Therapy
PublicationGrowing interest in silicone elastomers for pharmaceutical purposes is due to both theirbeneficial material effect for scar treatment and their potential as drug carriers. Regarding their morphological structure, silicone polymers possess unique properties, which enable a wide range of applicability possibilities. The present study focused on developing a double-layer adhesive silicone film (DLASil) by evaluating its physical...
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Damian Kuźniewski mgr inż.
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Influence of the addition of citric acid on the physico-chemical properties of poly(sorbitol sebacate-co- butylene sebacate)
PublicationThe article presents the results of the physicochemical properties of poly(sorbitol sebacate- co-butylene sebacate) (PSBS) obtained with 0.25; 0.5; 0.75; 1 mol of citric acid (KC). It was shown that PSBS obtained with 0.25 and 0.5 mol KC is characterized by the most optimal mechanical and thermal properties. As a result of the study, it was found that the use of sorbitol and citric acid allows obtaining ester materials with...
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Molecular dynamics and verisimilitude - to what extent can one trust a computational simulation?
PublicationFor the last several tens of years, computer simulations have become of undeniable importance. Molecular Dynamics (MD) simulation techniques are used to examine the phenomena which occur at the level that cannot be observed directly. Thus, they can be successfully exploited in many different scientific fields such as: materials science, applied mathematics and theoretical physics, biochemistry, biophysics or drug design. Despite...
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Development of polyurethanes for bone repair
PublicationThe purpose of this paper is to review recent developments on polyurethanes aimed at the design, synthesis, modifications, and biological properties in the field of bone tissue engineering. Different polyurethane systems are presented and discussed in terms of biodegradation, biocompatibility and bioactivity. A comprehensive discussion is provided of the influence of hard to soft segments ratio, catalysts, stiffness and hydrophilicity...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublicationHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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Zmiany struktury demograficznej ludności i ich wpływ na gospodarkę narodową
PublicationProblem zmian struktury demograficznej i alokacji zasobów ludności w kontekście rozwoju ekonomicznego państwa należy rozważań w ramach redystrybucji dochodów, co odbywa się w oparciu o trzy zasadnicze płaszczyzny, a mianowicie: makroekonomiczną, system emerytalny oraz prywatne transfery dochodów w przypadku sektora gospodarstw domowych. Ogromne znaczenie w ramach wyżej wymienionych powiązań ma czynnik starzenia się społeczeństwa,...
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Scenariusz rozwoju dla obszaru Bezpieczeństwo żywności
PublicationOpracowanie jest częścią foresightu technologicznego: Żywność i żywienie w XXI wieku - wizja rozwoju polskiego sektora spożywczego, wykonanego w ramach projektu, realizowanego w latach 2009-2011 przez konsorcjum: Instytut Ogrodnictwa (dawniej Instytut Sadownictwa i Kwiaciarstwa) w Skierniewicach, Instytut Badań nad Przedsiębiorczością i Rozwojem Ekonomicznym EEDRI przy Społecznej Wyższej Szkole Przedsiębiorczości i Zarządzania...
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Imidazoacridinone antitumor agent C-1311 as a selective mechanism- based inactivator of human cytochrome P450 1A2 and 3A4 isoenzymes.
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311), a promising antitumor agent that is also active against autoimmune diseases, was determined to be a selective inhibitor of the cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1311 might modulate the effectiveness of other drugs used in multidrug therapy. The present work aimed to identify the mechanism of the observed C-1311-mediated inactivation of CYP1A2...
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Diminshed toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
PublicationThe narrow "therapeutic window" of anti-tumour therapy may be the result of drug metabolism leading to the activation or detoxification of antitumour agents. The aim of this work is to examine (i) whether the diminished toxicity of a potent antitumour drug, C-1748, 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine, compared with its 4-demethyl analogue, C-857, results from the differences between the metabolic pathways for the...
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The Metal-Free Regioselective Deuteration of 2-Methylquinolin-8-ol and 2,5-Dimethylquinolin-8-ol, Spectroscopic and Computational Studies
PublicationAbstract: Aim and Background: Introducing deuterium to a molecule is of interest to a wide variety of research, including investigation of reaction mechanisms or kinetics, analysis of drug metabolism, structural elucidation of molecules, and syntheses of isotopically labeled materials used for NMR spectroscopy and medicinal research. Objective: The transition-metal-free regioselective deuteration of 2-methylquinolin-8-ol...
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Removal of selected sulfonamides and sulfonamide resistance genes from wastewater in full-scale constructed wetlands
PublicationSulfonamides are high-consumption antibiotics that reach the aquatic environment. The threat related to their presence in wastewater and the environment is not only associated with their antibacterial properties, but also with risk of the spread of drug resistance in bacteria. Therefore, the aim of this work was to evaluate the occurrence of eight commonly used sulfonamides, sulfonamide resistance genes (sul1–3) and integrase genes...
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Antibiotic-Based Conjugates Containing Antimicrobial HLopt2 Peptide: Design, Synthesis, Antimicrobial and Cytotoxic Activities
PublicationRecent studies have shown that modified human lactoferrin 20−31 fragment, named HLopt2, possesses antibacterial and antifungal activity. Thus, we decided to synthesize and evaluate the biological activity of a series of conjugates based on this peptide and one of the antimicrobials with proven antibacterial (ciprofloxacin, CIP, and levofloxacin, LVX) or antifungal (fluconazole, FLC) activity. The drugs were covalently connected...
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Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublicationUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
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Optoelectronic investigation of nanodiamond interactions with human blood
PublicationWe present optoelectronic investigation of in vitro interactions of whole human blood with different nanodiamond biomarkers. Plasmo-chemical modifications of detonation nanodiamond particles gives the possibility for controlling their surface for biological applications. Optical investigations reveal the biological activity of nanodiamonds in blood dependent on its surface termination. We compare different types of nanodiamonds:...
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Molecular dynamics studies of polyurethane nanocomposite hydrogels
PublicationPolyurethane PEO-based hydrogels have a broad range of biomedical applicability. They are attractive for drug-controlled delivery systems, surgical implants and wound healing dressings. In this study, a PEO based polyurethane hydrogels containing Cloisite R 30B, an organically modified clay mineral, was synthesized. Structure of nanocomposite hydrogels was determined using XRD technique. Its molecular dynamics was studied by means...
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Determination of impurities in pharmaceutical products using LC-MS
PublicationPharmaceutical products can be contaminated by residues of solvents, reagents (used for the synthesis) or degradation products. Impurities in drug may pose a risk to human health and life, therefore analysis and identification of impurities in pharmaceutical products is veryimportant and inevitable.High performance liquid chromatography coupled with mass spectrometry (MS) is very useful technique for identification impurities in...
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Multimateriałowe oraz wielokolorowe drukowanie wysokiej jakości części z żywic utwardzanych światłem UV w technologii PolyJet
PublicationMożliwość budowania multimateriałowych oraz wielokolorowych elementów stanowi ważny trend w rozwoju technologii żywicznych druku 3D. W niniejszym opracowaniu skupiono się na charakterystyce podstawowej metody przetwarzającej ciekłe fotopolimery – technologii PolyJet. Omówiono zasadę jej działania oraz najważniejsze aspekty procesu dotyczące m.in. parametrów drukarki, stosowanych struktur podporowych oraz rodzaju uzyskiwanej powierzchni...
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Selected Methods for the Chemical Phosphorylation and Thiophosphorylation of Phenols
PublicationThis Focus Review gathers together a selection of methods for the chemical phosphorylation of phenols that employ three‐ and four‐coordinate phosphorus compounds. Phosphorylated scaffolds can exhibit enhanced properties compared to their non‐phosphorylated analogues, such as increased biological activity and increased/decreased solubility; as such, phosphorus compounds have gained more and more interest in organic and medicinal...
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Efektywna komunikacja dla kadry administracyjnej Politechniki Gdańskiej
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Application of bioassays in studies on the impact of pharmaceuticals on the environment
PublicationDrug interactions are often desirable particularly in medicine, when treatment of a patient requires using a mixture of drugs in specific doses to produce the adequate therapeutic effect. Unfortunately, interactions between drugs in the environment are not as desirable, despite the fact that drugs are present in the environment at low concentration levels [1]. Pharmaceuticals are present in the environment in a mixture of compounds,...
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Low frequency of itraconazole resistance found among avian Aspergillus fumigatus isolates
PublicationAspergillus fumigatus is the most frequent etiological factor of invasive aspergillosis in human as well as animals, including birds. Aspergillosis caused by drug-resistant strains poses a significant therapeutic issue, especially if resistance pattern includes insensitivity to triazoles, i.e. drugs recommended for the primary therapy purposes. Majority of resistant isolates hold the TR34/L98H...
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublicationThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Determination of Toxicological Parameters of Selected Bioactive Organic Chemicals Using the Ostracodtoxkit FTM
PublicationAssessment of the impact of pharmaceutical residues on living organisms is very complex subject. Apart from taking into account the toxicity of individual compounds also their presence in mixtures should be taken into account. In this work, attempts were made to assess the ecotoxicity of biologically active substances (with 50 % effective concentration (EC50) values growing from fluoxetine (EC50 = 4.431 nM) >> gemfibrozil ≈ 17α-ethinylestradiol...
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Voriconazole-Based Salts Are Active against Multidrug-Resistant Human Pathogenic Yeasts
PublicationVoriconazole (VOR) hydrochloride is unequivocally converted into VOR lactates and valinates upon reaction with silver salts of organic acids. This study found that the anticandidal in vitro activity of these compounds was comparable or slightly better than that of VOR. The Candida albicans clinical isolate overexpressing CaCDR1/CaCDR2 genes, highly resistant to VOR, was apparently more susceptible to VOR salts. On the other hand,...
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Urinary Tract Infections Caused by K. pneumoniae in Kidney Transplant Recipients – Epidemiology, Virulence and Antibiotic Resistance
PublicationUrinary tract infections are the most common complication in kidney transplant recipients, possibly resulting in the deterioration of a long-term kidney allograft function and an increased risk of recipient’s death. K. pneumoniae has emerged as one of the most prevalent etiologic agents in the context of recurrent urinary tract infections, especially with multidrug resistant strains. This paper discusses the epidemiology and risk...
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Glucosamine-6-phosphate synthase with an oligoHis insert
PublicationGlucosamine-6-phosphate (GlcN-6-P) synthase known also as L-Glutamine: D-fructose-6-phosphate aminotransferase (EC 2.6.1.16), catalyzes the first committed step in the amino sugar biosynthetic pathway in prokaryotic and eukaryotic organisms. The final product of this pathway is an activated precursor of numerous macromolecules containing amino sugars, including chitin and mannproteins in fungi, peptydoglican and lipopolysaccharides...
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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the antitumor imidazoacridinone C-1311 in human hepatoma cells
PublicationThere is increasing evidence that the expression level of drug metabolic enzymes affects the final cellular response following drug treatment. Moreover, anti-tumour agents may modulate enzymatic activity and/or cellular expression of metabolic enzymes in tumour cells. We investigated the influence of CYP3A4 overexpression on the cellular response induced by the anti-tumour agent C-1311 in hepatoma cells. C-1311-mediated CYP3A4...
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Development and evaluation of RADA-PDGF2 self-assembling peptide hydrogel for enhanced skin wound healing
PublicationBackground: Wound healing complications affect numerous patients each year, creating significant economic and medical challenges. Currently, available methods are not fully effective in the treatment of chronic or complicated wounds; thus, new methods are constantly sought. Our previous studies showed that a peptide designated as PDGF2 derived from PDGF-BB could be a promising drug candidate for wound treatment and that RADA16-I...
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Application of the near-infrared spectroscopy in the pharmaceutical technology
PublicationNear-infrared (NIR) spectroscopy is currently the fastest-growing and the most versatile analytical method not only in the pharmaceutical sciences but also in the industry. This review focuses on recent NIR applications in the pharmaceutical technology. This article covers monitoring, by NIR, of many manufacturing processes, such as granulation, mixing or drying, in order to determine the end-point of these processes. In this...