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Wyniki wyszukiwania dla: inhibitory endopeptydazy prolinowej
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Phospholipids as potential prevention factor in carcinogenesis
PublikacjaPhospholipids are a group of complex lipids, which can be used in cancer chemoprevention. Glicerophospholipids are composed of fatty acids esterified to a glycerol backbone, a phosphate group and a hydrophilic residue such as: cho- line, ethanoloamine, serine or inositol. In the sn-2 position of glicerophospholipid usually there are unsaturated fatty acids, i.e. linolenic acid, while in the sn-1 position more typi- cal are saturated...
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Down-regulation of DNA topoisomerase IIalpha leads to prolonged cell cycle transit in G2 and early M phases and increased survival to microtubule-interacting agents
PublikacjaInhibitory polimeryzacji mikrotubul wykazują preferencyjną toksyczność wobec komórek mitotycznych. W ramach tego projektu badaliśmy czy oporność komórek ludzkich białaczek na inhibitor mikrotubul, winkrystynę, prowadzi do zmian w regulacji progresji cyklu komórkowego. Nasze wyniki wskazują, że oporności na winkrystynę towarzyszą zmiany w długości fazy G2 i M w nieobecności i obecności inhibitora wrzeciona mitotycznego, nokodazolu....
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublikacjaResearch 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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The effect of microemulsion composition on the morphology of Pd nanoparticles deposited at the surface of TiO2 and photoactivity of Pd-TiO2
PublikacjaA series of microemulsion (ME) system, constituted by different water to surfactant molar ratios (Wo) and oil to surfactant mass ratios (S), have been applied for Pd-TiO2 preparation. The effect of ME properties on the morphology of Pd nanoparticles formed at TiO2 surface and an effect of Pd size and distribution on the surface and photocatalytic properties of Pd-TiO2 were investigated. Microemulsion systems were characterized...
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Synthesis of Cyano-Benzylidene Xanthene Synthons Using a Diprotic Brønsted Acid Catalyst, and Their Application as Efficient Inhibitors of Aluminum Corrosion in Alkaline Solutions
PublikacjaNovel cyano-benzylidene xanthene derivatives were synthesized using one-pot and condensation reactions. A diprotic Brønsted acid (i.e., oxalic acid) was used as an effective catalyst for the promotion of the synthesis process of the new starting xanthene–aldehyde compound. Different xanthene concentrations (ca. 0.1–2.0 mM) were applied as corrosion inhibitors to control the alkaline uniform corrosion of aluminum. Measurements were...
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O07 Filaggrin insufficiency renders keratinocyte-derived small extracellular vesicles capable of affecting CD1a-mediated T-cell responses and promoting allergic inflammation
PublikacjaThe association between FLG loss-of-function mutations and the development of atopic dermatitis (AD) indicates that filaggrin is critical to skin barrier function; the mutations are also linked to additional allergic manifestations, but it is unknown how the skin may influence inflammation in distant tissues. Here we investigated the impact of filaggrin insufficiency on keratinocyte-derived exosome-enriched small extracellular...
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Type III Responses to Transient Inputs in Hybrid Nonlinear Neuron Models
PublikacjaExperimental characterization of neuronal dynamics involves recording both of spontaneous activity patterns and of responses to transient and sustained inputs. While much theoretical attention has been devoted to the spontaneous activity of neurons, less is known about the dynamic mechanisms shaping their responses to transient inputs, although these bear significant physiological relevance. Here, we study responses to transient...
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Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublikacjaIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
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Toward better understanding of phosphoryl transfer reaction: the use of phosphoroorganic biocides in research studies
PublikacjaZamierzeniem autora było nakreślenie potencjalnych kierunków rozwoju badań z wykorzystaniem biocydów fosforoorganicznych (BFO) i związanej z nimi reakcji przeniesienia grupy fosforylowej (reakcja FT). Projektowane są nowe, wysoce selektywne inhibitory enzymów, które w pełni wyjaśniają rolę enzymów w warunkach normalnego funkcjonowania i w procesach patologicznych. Pozwoli to w konsekwencji na wyselekcjonowanie nowych terapeutyków...
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Antibiotic-Based Conjugates Containing Antimicrobial HLopt2 Peptide: Design, Synthesis, Antimicrobial and Cytotoxic Activities
PublikacjaRecent 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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Activity of isavuconazole and other triazole derivatives against clinical isolates of Aspergillus fumigatus
PublikacjaAspergillus fumigatus is the most frequent pathogen of the genus Asperillus, which is highly susceptible to triazole derivatives, especially to isavuconazole and voriconazole. Many countries face a growing problem of infections due to A. fumigatus showing acquired resistance to one or several triazoles. In medical centres, monitoring the susceptibility of isolated Aspergillus spp. is recommended. The aim of this study was to collect...
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Characterization of recombinant homocitrate synthase from Candida albicans
PublikacjaLYS21 and LYS22 genes from Candida albicans encoding isoforms of homocitrate synthase (HCS), an enzyme catalyzing the first committed step in the L-lysine biosynthetic pathway, were cloned and expressed as NoligoHistagged fusion proteins in Escherichia coli. The purified gene products revealed HCS activity, i.e. catalyzed the condensation of α-ketoglutarate with acetyl-coenzyme A to yield homocitrate. The recombinant enzymes were purified...
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Cross-talk between DNA damage and cell survival checkpoints during G2 and mitosis: pharmacological implications
PublikacjaW pracy wyjaśnialiśmy rolę surwiwiny w ochronie komórek w czasie przejścia między G2 i mitozą, traktowanych związkiem uszkadzającym DNA. Jako model komórkowy wybraliśmy komórki ludzkiej białaczki MOLT-4, które wykazują zwiększoną ekspresję białka surwiwiny i niefunkcjonalnym p53. Ekspozycja tych komórek na melfalan, klasyczny związek uszkadzający DNA, prowadzi do uruchomienia punktu kontrolnego w G2 i zablokowania progresji cyklu...
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Elucidation of chemical compounds in different extracts of two Lavandula taxa and their biological potentials: Walking with versatile agents on the road from nature to functional applications
PublikacjaDue to their health-promoting and nutraceutical properties, lavenders are frequently employed in the food and pharmaceutical industries. Here, we focused on investigate the chemical profile of hexane, MeOH, and water extracts of leaf, flower, and root of L. pedunculata and L. stoechas and to assess their antioxidant, enzyme inhibitory, and antibacterial properties. The highest total polyphenolic and flavonoids contents were recorded...
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Actions of a nitric oxide donor on prostaglandin production and angiogenic activity in the equine endometrium
PublikacjaNitric oxide (NO) plays an important role in prostaglandin secretion and angiogenesis in the reproductive system. In the present study, the roles of the NO donor spermine NONOate and tumour necrosis factor-alpha (TNF; as a positive control) in prostaglandin production and angiogenic activity of equine endometria during the oestrous cycle were evaluated. In addition, the correlation between NO production...
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Activated sodium percarbonate-ozone (SPC/O3) hybrid hydrodynamic cavitation system for advanced oxidation processes (AOPs) of 1,4-dioxane in water
PublikacjaHydrodynamic cavitation (HC) was employed to activate sodium percarbonate (SPC) and ozone (O3) to degrade recalcitrant 1,4-dioxane. The degradation efficiency > 99 % with a rate constant of 4.04 × 10−2 min−1 was achieved in 120 min under the optimal conditions of cavitation number (Cv) 0.27, pH 5, molar ratio of oxidant to pollutant (rox) 8, ozone dose of 0.86 g h−1 under 25 ± 2 °C with initial concentration of 1,4-dioxane 100...
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Increased susceptibility of PARP-1 KO cells to antitumor triazoloacridone C-1305 is associated with permanent G2 cell cycle arrest.
PublikacjaTriazoloakrydon C-1305 jest nowym inhibitorem topoizomerazy II wykazującym wysoką aktywność przeciwnowotworową. W tej pracy badaliśmy działanie cytotoksyczne pochodnej C-1305 i jej analogu strukturalnego C-1533 wobec komórek fibroblastów mysich i dwóch mutantów, w których uszkodzono gen PARP-1. Jak wykazaliśmy, komórki z uszkodzonym genem PARP-1 są nadwrażliwe na działanie związku C-1305 w porównaniu z komórkami PARP-1 +/+ podczas...
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Synthesis and Structure of Novel Hybrid Compounds Containing Phthalazin-1(2H)-imine and 4,5-Dihydro-1H-imidazole Cores and Their Sulfonyl Derivatives with Potential Biological Activities
PublikacjaA novel hybrid compound—2-(4,5-dihydro-1H-imidazol-2-yl)phthalazin-1(2H)-imine (5) was synthesized and converted into di-substituted sulfonamide derivatives 6a–o and phthalazine ring opening products—hydrazonomethylbenzonitriles 7a–m. The newly prepared compounds were characterized using elemental analyses, IR and NMR spectroscopy, as well as mass spectrometry. Single crystal X-ray diffraction data were collected for the representative...
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Kinetics of Cross-Linking Reaction of Epoxy Resin with Hydroxyapatite-Functionalized Layered Double Hydroxides
PublikacjaThe cure kinetics analysis of thermoset polymer composites gives useful information about their properties. In this work, two types of layered double hydroxide (LDH) consisting of Mg2+ and Zn2+ as divalent metal ions and CO32− as an anion intercalating agent were synthesized and functionalized with hydroxyapatite (HA) to make a potential thermal resistant nanocomposite. The curing potential of the synthesized nanoplatelets in the...
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Efficient Extraction of Fermentation Inhibitors by Means of Green Hydrophobic Deep Eutectic Solvents
PublikacjaThe methods for hydrogen yield efficiency improvements, the gaseous stream purification in gaseous biofuels generation, and the biomass pretreatment are considered as the main trends in research devoted to gaseous biofuel production. The environmental aspect related to the liquid stream purification arises. Moreover, the management of post-fermentation broth with the application of various biorefining techniques gains importance....
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Urinary Tract Infections of Escherichia coli Strains of Chaperone-Usher System
PublikacjaZakażenia dróg moczowych stanowią bardzo poważny problem zdrowotny i ekonomiczny dotyczący milionów ludzi, każdego roku na całym świecie. Najbardziej rozpowszechnionym czynnikiem etiologicznym tego typu infekcji bakteryjnych, obejmujących górne i dolne drogi moczowe, są szczepy E. coli, reprezentujące około 80% przypadków. Uropatogenne szczepy E. coli produkują kilka czynników urowirulentncyh, które można podzielić na dwa główne...
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Anticancer imidazoacridinone C-1311 inhibits hypoxia-inducible factor-1α (HIF-1α), vascular endothelial growth factor (VEGF) and angiogenesis
PublikacjaAntitumor imidazoacridinone C-1311 is a DNA-reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor. Here, we demonstrate the mechanism of C-1311 inhibitory action on novel targets: hypoxia-inducible factor-1α (HIF-1α), vascular-endothelial growth factor (VEGF), and angiogenesis. In a cell-free system, C-1311 prevented HIF-1α binding to an oligonucleotide encompassing a canonical hypoxia-responsive element (HRE),...
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Optimised five-hour multiplex PCR test for the detection of Tinea ungium: performance in a routine PCR laboratory
PublikacjaWe recently published the development of a 5-hour multiplex PCR test for the detection of dermatophyte nail infection. We have optimized this test by inclusion of an inhibition control and evaluated the test in a routine laboratory when compared to the conventional microscopy and culture. A total of 109 clinical samples received at the mycology reference lab at Statens Serum Institute were included. The samples were divided equally...
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L1 Cell Adhesion Molecule Overexpression Down Regulates Phosphacan and Up Regulates Structural Plasticity-Related Genes Rostral and Caudal to the Complete Spinal Cord Transection
PublikacjaL1 cell adhesion molecule (L1CAM) supports spinal cord cellular milieu after contusion and compression lesions, contributing to neuroprotection, promoting axonal outgrowth, and reducing outgrowth-inhibitory molecules in lesion proximity. We extended investigations into L1CAM molecular targets and explored long-distance effects of L1CAM rostral and caudal to complete spinal cord transection (SCT) in...
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The influence of food phytochemicals on cyclic phosphodiesterase 4 (PDE4) activity
PublikacjaCyclic phosphodiesterase 4 (PDE4) belongs to family of cyclic phosphodiesterases, which are expressed predominantly in inflammatory cells, airway smooth muscles, cardiovascular tissues and brain. Inhibitors of this family of enzymes found medicinal applications as antidepressants, antiinflamatory drugs (mainly in airway diseases) or antiasthmatics (Ibudilast). PDE4 inhibitors are also being tested for preventing the development...
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A novel approach to enhance high optically active L-lactate production from food waste by landfill leachate
PublikacjaThe recycling of food waste (FW) through anaerobic fermentation into lactic acid (LA), with two isomers L-LA and D-LA, aligns with the principles of a bio-based circular economy. However, FW fermentation is often limited by competing pathways, acidification inhibition, and trace metals deficiency. This study investigates the introduction of landfill leachate, containing buffering agents (ammonia) and trace metals, into FW fermentation....
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The antitumor compound triazoloacridinone C-1305 inhibits FLT3 kinase activity and potentiates apoptosis in mutant FLT3-ITD leukemia cells.
PublikacjaAim: FMS-like receptor tyrosine kinase (FLT3) is expressed in some normal hematopoietic cell types and plays an important role in the pathogenesis of acute myeloid leukemia (AML). In this study, we examined the effects of triazoloacridinone C-1305, an antitumor compound, on AML cells with different FLT3 status in vitro. Methods: A panel of human leukemic cell lines with different FLT3 status was used, including FLT3 internal tandem...
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The Antimicrobial Potential of Bacteria Isolated from Honey Samples Produced in the Apiaries Located in Pomeranian Voivodeship in Northern Poland
PublikacjaThe principal objective of this study was to determine whether the honeys produced in apiaries located in Pomeranian Voivodeship (Northern Poland) contain bacteria producing metabolites with growth inhibition potential against important human and animal pathogens. The pathogens included Staphylococcus aurues, Staphyloccocus epidermidis, Escherichia coli, Listeria monocytogenes, Pseudomonas aeruginosa, and Candida albicans. From...
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Essential oils as potential anti-staphylococcal agents
PublikacjaAntibiotic therapy of staphylococcal mastitis is characterized by significantly lower cure rates compared to infections caused by other microorganisms. Thus, it is necessary to search for new, alternative, non-antibiotic agents that are effective in the eradication of these bacteria. The aim of our research was to investigate the antimicrobial, especially anti-staphylococcal potential of a large collection (n=36) of essential oils...
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Peptide Permeases in Candida albicans
PublikacjaAims: The aim of this work was to characterize oligopeptide uptake in Candida albicans mutants in which the genes encoding putative peptide permeases were selectively disrupted. Initial velocities of transport of model oligopeptides, (Ala)2, (Ala)3, (Ala)4, and sensitivity of mutants to antifungal oligopeptides containing N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP) were determined and compared to those of the wild-type...
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Composition and antimicrobial activity of fatty acids detected in the hygroscopic secretion collected from the secretory setae of larvae of the biting midge Forcipomyia nigra (Diptera: Ceratopogonidae)
PublikacjaThe hygroscopic secretion produced by the secretory setae of terrestrial larvae of the biting midge Forcipomyia nigra (Winnertz) was analysed using gas chromatography coupled with mass spectrometry (GC-MS). The viscous secretion is stored at the top of each seta and absorbs water from moist air. GC-MS analyses (four independent tests) showed that the secretion contained 12 free fatty acids, the most abundant of which were oleic...
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublikacjaNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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Techniki amplifikacji kwasów nukleinowych -2024-2025 - Nowy
Kursy OnlineSpecjalność: Biotechnologia molekularna (WCh), II stopnia, stacjonarne Prowadzący wykład: dr hab. Beata Krawczyk, prof. uczelni - stacjonarnie na uczelni Prowadzący laboratoria: dr hab. Beata Krawczyk, prof. uczelni - zajęcia stacjonarne na PG, sala 304 WCH B. Kontakt: (58) 347-23-83 Beata Krawczyk (wykłady): e-mail: beata.krawczyk@pg.edu.pl; WCH B; p.217; Konsultacje: stacjonarnie we wtorki o godzinie 13. Opis kursu Kurs...
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Techniki amplifikacji kwasów nukleinowych -2022-2023
Kursy OnlineSpecjalność: Biotechnologia molekularna (WCh), II stopnia, stacjonarne Prowadzący wykład: dr hab. Beata Krawczyk, prof. uczelni - forma stacjonarna Prowadzący laboratoria: mgr inż. Bartosz Ostrowski - zajęcia stacjonarne na PG, sala 17 WCH C. Kontakt: (58) 347-23-83 Beata Krawczyk (wykłady): e-mail: beata.krawczyk@pg.edu.pl; WCH B; p.218; Bartosz Ostrowski, WCH B, p.218 tel. (58) 347-13-83 Konsultacje: stacjonarnie we wtorki ...
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Techniki amplifikacji kwasów nukleinowych -2021-2022
Kursy OnlineSpecjalność: Biotechnologia molekularna (WCh), II stopnia, stacjonarne Prowadzący wykład: dr hab. Beata Krawczyk, prof. uczelni - stacjonarnie na uczelni Prowadzący laboratoria: mgr inż. Magdalena Fordon - zajęcia stacjonarne na PG, sala 17 WCH C. Kontakt: (58) 347-23-83 Beata Krawczyk (wykłady): e-mail: beata.krawczyk@pg.edu.pl; WCH B; p.218; Magdalena Fordon (laboratoria): magda.fordon@gmail.com; WCH B; p.218 Konsultacje:...
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Techniki Amplifikacji Kwasów Nukleinowych -2024-2025
Kursy OnlineSpecjalność: Biotechnologia molekularna (WCh), II stopnia, stacjonarne Prowadzący wykład: dr hab. Beata Krawczyk, prof. uczelni - forma stacjonarna Prowadzący laboratoria: dr hab. Beata Krawczyk, prof. uczelni- zajęcia stacjonarne na PG, sala 304 WCH B (bud.7); III piętro. Kontakt: (58) 347-23-83 Beata Krawczyk (wykłady): e-mail: beata.krawczyk@pg.edu.pl; WCH B; p.217;tel. (58) 347-23-83 Bartosz Ostrowski, WCH B, p.218 tel....
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Nanoparticles preparation using microemulsion systems
PublikacjaMetallic nanoparticles become of current interests because they exhibit unique properties compared with those of metal atoms or bulk metal due to the quantum size effect and their large surface area, which make them attractive for applications in optics, electronics, catalysis biology and medicine. TiO2 has been used for environmental remediation purposes such as in the purification of water and air and also solar-to chemical energy...