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Search results for: anti-staphylococcus aureus agents
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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The Influence of the Co-Dopant Dexamethasone Phosphate on the Electrodeposition Process and Drug-Release Properties of Polypyrrole-Salicylate on Iron
PublicationIn this work, the influence of incorporation of two anti-inflammatory drugs dexamethasone phosphate and sodium salicylate on the electrodeposition process of polypyrrole (PPy) film on iron has been studied. The incorporation of the agents into PPy has been carried out in a one-step electropolymerization process on oxidizable iron. The role of each drug agent during the deposition process has been discussed. The morphological and...
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Thermal Instability of Choline Chloride-Based Deep Eutectic Solvents and Its Influence on Their Toxicity─Important Limitations of DESs as Sustainable Materials
PublicationDeep eutectic solvents (DESs) have become a hot topic in many branches of science due to their remarkable properties. They have been studied in a wide variety of applications. In particular, choline chloride (ChCl)-based DESs are one of the most commonly used representatives of these fluids. Nevertheless, in order to apply DESs in some fields, it is essential to guarantee their stability, reusability, and biocompatibility. In this...
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The effect of nanoparticles size on photocatalytic and antimicrobial properties of Ag-Pt/TiO2 photocatalysts
PublicationAg-Pt-modified TiO2 nanocomposites were synthesized using the sol–gel method. Bimetallic modified TiO2 nanoparticles exhibited improved photocatalytic activity under visible-light irradiation, better than monometallic Ag/TiO2 and Pt/TiO2 nanoparticles (NPs). All modified powders showed localized surface plasmon resonance (LSPR) in visible region. The photocatalysts’ characteristics by X-ray diffractometry (XRD), scanning transmission...
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Efficient production of Staphylococcus simulans lysostaphin in a benchtop bioreactor by recombinant Escherichia coli.
PublicationLysostaphin is an enzyme with bactericidal activity against Staphylococcus aureus and other staphylococcal species. In spite of many advantages and promising results of preliminary research, the enzyme is still not widely used in medicine, veterinary or as a food preservative. One of the most important factors limiting application of the enzyme in clinical or technological practice is the high costs of its production. In the present...
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Pharmaceuticals and another groups of emerging contaminants: Occurrence and sources in Admiralty Bay (King George Island, Maritime Antarctica)
PublicationEveryday live activities may introduce a wide range of chemicals into wastewater systems. In this study presence of selected types of pharmaceuticals from cardiovascular system group, nervous and muscolo-skeleton system group, antimicrobial agents, genitourinary and sex hormones were tested in the wastewater from H. Arctowski Antarctic station. Moreover, the receiver of discharged wastewater (Admiralty Bay) were also studied. Considering...
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Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)
PublicationThe aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA−PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro...
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Polyurethane porous scaffolds (PPS) for soft tissue regenerative medicine applications
PublicationTissue engineering requires suitable polymeric scaffolds, which act as a physical support for regenerated tissue. A promising candidate might be polyurethane (PUR) scaffold, due to the ease of the PUR properties design, which can be adjusted directly to the intended purpose. In this study, we report a successful fabrication of porous polyurethane scaffolds (PPS) using solvent casting/particulate leaching technique combined with...
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May Staphylococcus lugdunensis Be an Etiological Factor of Chronic Maxillary Sinuses Infection?
PublicationStaphylococcus lugdunensis is an opportunistic pathogen found in the healthy human skin microbiome bacterial community that is able to cause infections of diverse localization, manifestation, and course, including laryngological infections, such as necrotizing sinusitis. Chronic maxillary sinusitis is a disease present in up to one third of European and American populations, and its etiology is not fully described. Within this...
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Otzrymywanie i charakterystyka nowych biomateriałów o aktywności przeciwdrobnoustrojowej na bazie chitozanu, kolagenu i żelatyny
PublicationW niniejszej pracy przedstawiono opis wyników badań poświęconych otrzymywaniu i charakterystyce biomateriałów zbudowanych z chitozanu, kolagenu i żelatyny, o strukturze i właściwościach wymaganych od nowoczesnego materiału opatrunkowego, stanowiącego jednocześnie dogodną matrycę do inkorporacji związków biologicznie czynnych, zwłaszcza lizostafyny. Opracowane materiały stanowią także próbę odpowiedzi na potrzeby medyczne dotyczące...
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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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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublicationAcquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is one of the most challenging diseases in recent decades. Nevertheless the shortcomings of chemical drugs such as toxicity, lack of curative effects, the search for more potent anti-HIV agents have been focused in our study. In current study, novel scaffold was designed having a benzyl and imidazole in it which are very...
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublicationTelomerase plays a pivotal role in cell proliferation, homeostasis, and neoplastic transformation, making it a promising molecular target for cancer chemotherapy. Of note, although hTERT has been explored thoroughly as a target, none of the promising molecules has been approved as a drug until now. The subject of research conducted as part of my doctoral dissertation is explaining the cellular and molecular mechanism of action...
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublicationThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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Emerging anticancer activity of candidal glucoseamine-6-phosphate synthase inhibitors upon nanoparticle-mediated delivery
PublicationNumerous glutamine analogues have been reported as irreversible inhibitors of the glucosamine-6-phosphate (GlcN-6-P) synthase in pathogenic Candida albicans in the last 3.5 decades. Among the reported inhibitors, the most effective N3-(4-methoxyfumaroyl)-L-2,3- diaminopropanoic acid (FMDP) has been extensively studied in order to develop its more active analogues. Several peptide−FMDP conjugates were tested to deliver FMDP to its...
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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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Anti-cancer effect of Rumex obtusifolius in combination with arginase/nitric oxide synthase inhibitors via downregulation of oxidative stress, inflammation, and polyamine synthesis
PublicationCancer continues to be a leading cause of death worldwide, making the development of new treatment methods crucial in the fight against it. With cancer incidence rates increasing worldwide, ongoing research must focus on identifying new and effective ways to prevent and treat the disease. The combination of herbal extracts with chemotherapeutic agents has gained much interest as a novel strategy to combat cancer. Rumex obtusifolius...
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Experimental and Theoretical Insights into the Intermolecular Interactions in Saturated Systems of Dapsone in Conventional and Deep Eutectic Solvents
PublicationSolubility is not only a crucial physicochemical property for laboratory practice but also provides valuable insight into the mechanism of saturated system organization, as a measure of the interplay between various intermolecular interactions. The importance of these data cannot be overstated, particularly when dealing with active pharmaceutical ingredients (APIs), such as dapsone. It is a commonly used anti-inflammatory and...
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Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions
PublicationBackground. Dapsone (DAP) is an anti-inflammatory and antimicrobial active pharmaceutical ingredient used to treat, e.g., AIDS-related diseases. However, low solubility is a feature hampering its efficient use. Objectives. First, deep eutectic solvents...