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Search results for: IN VITRO METABOLIZM
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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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Raman spectroscopic investigation of blood and related materials
PublicationThis paper reports preliminary studies on use of Raman spectroscopy for investigation of blood. High quality blood spectra were recorded in-vitro with excitation wavelengths of 830 nm. Because of complex composition of the blood as well as by light attenuation and scattering in the tissues, spectra set up from wide, low-intensive Raman bands and intensive optical background. To get information about origin of bands in Raman spectra...
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Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity
PublicationSeven conjugates composed of well-known fluoroquinolone antibacterial agents, ciprofloxacin (CIP) or levofloxacin (LVX), and a cell-penetrating peptide transportan 10 (TP10-NH2) were synthesised. The drugs were covalently bound to the peptide via an amide bond, methylenecarbonyl moiety, or a disulfide bridge. Conjugation of fluoroquinolones to TP10-NH2 resulted in congeners demonstrating antifungal in vitro activity against human...
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Synthesis, Chemical Characterization and Multiscale Biological Evaluation of a dimericcRGD Peptide for Targeted Imaging of αVβ3 Integrin Activity
PublicationCyclic peptides containing the Arg-Gly-Asp (RGD) sequence have been shown to specifically bind the angiogenesis biomarker α V β3 integrin. We report the synthesis, chemical characterization, and biological evaluation of two novel dimeric cyclic RGD-based molecular probes for the targeted imaging of α V β3 activity (a radiolabeled version, 64Cu-NOTA-PEG4-cRGD2, for PET imaging, and a fluorescent version, FITC-PEG4-cRGD2, for in...
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Instrumental techniques used in the analysis of exhaled air
PublicationExhaled air composition changes depending on the health status of the patient, making it possible to use breath analysis for diagnosis and monitoring purposes. Despite the fact that it is not yet used in every day medical practice, it potential application could facilitate the diagnostics of various diseases such as metabolic disorders, respiratory tract and gastrointestinal diseases. Described in this paper are different application...
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Spatial development in the EU in the global context
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The interaction of antitumor 1-nitroacridines with DNA in cell-free systems
PublicationUzyskano 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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Posadowienie obiektów mostowych na palach przemieszczeniowych formowanych w gruncie
PublicationPraca dotycząca posadowienia obiektów mostowych na palach przemieszczeniowych formowanych w gruncie. W pracy omówiono technologie pali Franki, Vibro-Fundex, Vibrex, Tubex i FDP oraz podano przykłady realizacji obiektów mostowych na tych palach.
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Gracjana Klein-Raina dr hab.
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Cardinal regenerative features of the MRL mouse
PublicationIn this review, we discuss recent studies relating to major features of adult MRL mouse biology that contribute to the regenerative responses seen. These include an increased inflammatory cell profile, a unique glycolytic metabolic state typically found during embryogenesis, and a cell cycle phenotype of DNA damage and G2/M arrest. These traits have been found in other mammalian and non-mammalian regenerative systems. How these...
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Efficient synthesis and antifungal investigation of nucleosides’ quaternary ammonium salt derivatives
PublicationQuaternary ammonium salts are a group of compounds with diverse biological properties, the most important of which are their antiviral, antibacterial, and antifungal activities. The quaternization reactions of 5'-O-tosyl derivatives of uridine and thymidine with triethylamine, trimethylamine, 4-(N ,N -dimethylamino)pyridine, 2-methylpyridine, and pyridine are described in this article. Two of the synthesized compounds are exceptional...
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Voriconazole and multidrug resistance in Candida albicans
PublicationPorównano aktywność grzybostatyczną in vitro worikonazolu, flukonazolu, ketokonazolu i klotrimazolu wobec opornych na flukonazol szczepów klinicznych Candida albicans oraz rekombinowanych szczepów Saccharomyces cerevisiae eksprymujących jeden z genów kodujących białka oporności wielolekowej (MDR) C. albicans: Cdr1p. Cdr2p lub CaMdr1p. Stwierdzono, że nadekspresja genów MDR czyni komórki drożdżaków mniej wrażliwymi na działanie...
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Initial Report on Numerical Modeling of Blood Flow in Myocardial Bridge Region of Coronary Artery: Concept of Model Validation
PublicationThe paper presents a numerical method of blood flow simulation within the coronary artery covered by the myocardial bridge. The myocardial bridge is a congenital coronary abnormality caused by the blood vessel location under one of the heart muscles. In this case, the blood flow within the vessel is partially disturbed which can cause several consequences. The presented numerical simulation allowed us to estimate the blood flow...
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Modulating D-amino acid oxidase (DAAO) substrate specificity through facilitated solvent access
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Histaminol and Its Complexes with Copper(II) - Studies in Solid State and Solution
PublicationHistaminol [4(5)-(B-hydroxyethyl)imidazole, 4-(1H-imidazol-2-yl)ethanol, L] is an analogue of histamine and its minor metabolite. So far its properties have not been studied in detail due to the synthetic difficulties. Here, the structure and acid-base properties of histaminol, as well as the results of studies on its copper(II) complexes in solid state and aqueous solution are reported. Stability constants of the histaminol–CuII...
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Chemometric methods for determination of mechanisms of action of anticancer compounds
PublicationW 1990 amerykański Narodowy Instytut Raka (NCI) wprowadził szeroki test przesiewowy in vitro mający na celu poszukiwanie nowych związków przeciwnowotworowych. Test został wdrożony po przebadaniu 171 standardowych związków przeciwnowotworowych. Przedmiotem niniejszej pracy jest próba stworzenia reguł klasyfikacji związków standardowych ze względu na ich mechanizm działania przeciwnowotworowego na podstawie wyników z testu NCI. Potwierdzono...
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Wyniki sulfammox (SRAO)
Open Research DataTwo granular sequencing batch reactors were operated for 160 days under anammox conditions, comparing the Anammox process and Sulfate Reduction Ammonium Oxidation process. The study aimed to investigate whether increasing the concentration of SO42- could enhance N removal rates under anaerobic conditions, and whether SO42- reduction and anammox processes...
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Mission impossible for cellular internalization: When porphyrin alliance with UiO-66-NH2 MOF gives the cell lines a ride
PublicationIs it possible to accelerate cell internalization by hybridization of nanomaterials? Herein we support the realization of using metal-organic frameworks (MOFs) with the assistance of rigid porphyrin structure (H2TMP) aimed at drug loading, drug release, relative cell viability, and targeted in vitro drug delivery. There are several MOFs, i.e., UiO-66-NH2 (125 ± 12.5 nm), UiO-66-NH2 @H2TMP (160 ± 14 nm), UiO-66-NH2 @H2TMP@DOX, and...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublicationBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Spatial development in EU in a global context (2022/2023).
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Izabela Sinkiewicz dr inż.
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Effect of Maximal Breath Hold Apnea on Pial Artery Pulsation and Subarachnoid Width in Human
PublicationLittle is known about intracranial pressure (ICP)-cerebral hemodynamic interplay during maximal breath-hold apnea. A recently developed method based on near-infrared transillumination/backscattering sounding (NIR-T/BSS) noninvasively measures changes in pial artery pulsation (cc-TQ) as well as subarachnoid width (sas-TQ) in humans. Changes in sas-TQ correlate with ICP to a considerable extent, whereas cc-TQ reflects the functional...
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Computational studies of friction forces for hard tissue cultivation in bioreactor.
PublicationPonieważ wymiana naturalego stawu na endoprotezę może być dokonywana 2-3 razy w życiu, problem leczenia przez transplantację tkanek chrzęstnych nabiera dużego znaczenia. Przeszczepów tkanki można dokonywać z sukcesem wiele razy. W bioreaktorach, środowisko hydrodynamiczne kształtuje hodowlę tkanek in vitro w obecności sił tarcia, poprzez bezpośrednie działanie na morfologię komórek a także poprzez pośrednie działanie na tkankę...
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The activity of latent benzoperimidine esters to inhibit P-glycoprotein and multidrug resistance-associated protein 1 dependent efflux of pirarubicin from several lines of multidrug resistant tumor cells.
PublicationZaprezentowano wyniki badań biologicznych przeprowadzonych dla nowej grupy związków: estrów benzoperymidyny z zastosowaniem wybranych linii komórek nowotworowych: wrażliwych i opornych o oporności P-gp-zależnej, MRP1-zależnej i o oporności związanej z nadekspresją białek MRP1/LRP. Metodą spektrofluorymetryczną zbadano zdolność estrów benzoperymidyny do hamowania eksportu aktywnego pirarubicyny z komórek opornych. Estry benzoperymidyny...
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A Convenient Way to Methylated 2-Imidazolines. Syntheses of Fluorene and Triazine Cyclic Diamidines
PublicationOne N-methyl- and 4-substituted 2-imidazolines are described. Fluorene bisimidazolines were obtained in good yield (64-92%), starting from 2,7-dicyanofluorene and ammonium sulfide. In a two-step procedure the crude bisthioamide was reacted with excess diaminoalkane-ethanol (1:1 mixt.) in an oil bath. This new procedure is superior over std. methods. For the sake of comparison, a new triazine bisimidazoline (I) was prepd. by...
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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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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublicationDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Modeling in Machine Design
e-Learning CoursesThe course is meant to show the students how to build calculation models in machine design
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Internet Technologies in Infosystems
e-Learning CoursesThe aim of the course "Internet technologies in infosystems" is to familiarize students with issues related to the use of Internet technologies in the implementation of infosystems, including languages and web development tools, as well as application and transmission protocols.
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Management in modern organizations_2022_2023
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Image Processing in Robotics
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CAE in design calculations
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ICT in Management 2020
e-Learning CoursesICT in Management for Bachelor in Management students
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Management in modern organizations_2024_2025
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Contemporary Theories in Architecture
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CAE in Design Calculations
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Advances in Human Genetics
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Conthemporary Theories in Architecture
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Mathematical methods in engineering
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Microscopy methods in nanotechnology
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Management in modern organizations_2023_24
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LAW IN INVESTMENT PROCESS
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Laboratory in organic chemistry
e-Learning CoursesSupport for the laboratory in organic chemistry.
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Microscopy methods in nanotechnology
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Models in Spatial Development
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Image Processing in Robotics
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Wpływ sfunkcjonalizowanych nanocząstek typu rdzeń-powłoka (Fe3O4@SiO2) na zahamowanie enzymów grzybiczych w systemach in vitro
ProjectsProject realized in Department of Pharmaceutical Technology and Biochemistry according to UMO-2015/17/N/NZ7/01087 agreement from 2016-03-17
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The ability to overcome multidrug resistance of tumor cell lines by novel acridine cytostatics with condensed heterocyclic rings
PublicationZbadano aktywność cytotoksyczną, in vitzo dwóch nowych grup cytostatyków akrydynowych zawierających skondensowane pierścienie heterocykliczne w stosunku do komórek nowotworowych linii wrażliwych i opornych. Otrzymane wyniki potwierdziły naszą wcześniejszą hipotezę o istotnej roli pierścieni hetero-cyklicznych w pokonywaniu krzyżowej oporności wielolekowej.
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Biochemia
e-Learning Courses1. Budowa komórek prokariotycznych i eukariotycznych2. Biocząsteczki – aminokwasy, peptydy i białka3. Biocząsteczki – cukry i polisacharydy4. Biocząsteczki – lipidy. Budowa błon biologicznych5. Biocząsteczki – kwasy nukleinowe6. Enzymy – budowa, mechanizmy działania i regulacji aktywności7. Główne szlaki kataboliczne – glikoliza, cykl Krebsa, łańcuch oddechowy, utlenianie kwasów tłuszczowych8. Przykłady szlaków anabolicznych9....
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Cząsteczki mikroRNA - nowy biologicznie aktywny składnik mleka kobiecego
PublicationCząsteczki mikroRNA są krótkimi, niekodującymi oligonukleotydami odpowiadającymi za potranskrypcyjną regulację ekspresji genów. W wyniku ich aktywności kontrolowanych jest wiele procesów komórkowych oraz szlaków sygnalizacyjnych. Od 2010 roku wiadomo, że wchodzą one w skład mleka kobiecego, które obecnie uznaje się za jedno z najbogatszych pokarmowych źródeł mikroRNA. Funkcje tych cząsteczek w organizmie karmionego mlekiem matki...