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Wyniki wyszukiwania dla: IN VITRO PROTEOLYSIS
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The crystal structure of (1RS,4RS,5RS,6SR)-5-cyano-5-nitro-6-phenyl-bicyclo[2.2.1]hept-2-ene
PublikacjaStructure of nitronorbornene derivative C14H12N2O2 synthesized in the reaction of cyclopentadiene with E-2-phenyl-1-cyano-1-nitroethene was determined by single crystal X-ray diffraction analysis. It was found that in analyzed molecule the nitro group is in endo-position whereas phenyl group have exo-ori-entation.
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New Molecular Markers Involved in Regulation of Ovarian Granulosa Cell Morphogenesis, Development and Differentiation during Short-Term Primary In Vitro Culture—Transcriptomic and Histochemical Study Based on Ovaries and Individual Separated Follicles
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Rational design, synthesis and biological evaluation of thiadiazinoacridines: a new class of antitumor agents.
PublikacjaZsyntetyzowano serię związków o potencjalnej zdolności do wiązania się z DNA z grupy tiadiazinoakrydyn poprzez cyklizację odpowiednich pochodnych 9-imino-4-nitro-9,10-dihydroakrydyny. Zbadano ich zdolność do wiązania się z DNA oraz cytotoksyczność względem kilku linii komórek nowotworwych. Badania aktywności przeciwnowotworowej wobec białaczki P388 wskazały na zgodność tych wyników z wynikami cytotoksyczności in vitro. Wykazano,...
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HR-CS FAAS based method for direct determination of total concentrations of Ca, Fe, Mg and Mn in functional apple beverages and evaluation of contributions of the bioaccessible fraction of these elements by in vitro gastrointestinal digestion and chemical fractionation
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In vitro effect of three-dimensional (3D) titanium mini-plate systems used for surgical treatment of condylar fractures on interleukin 1 (IL-1) and interleukin 6 (IL-6) concentration in THP-1 macrophages
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In vitro enzyme kinetics and NMR-based product elucidation for glutathione S-conjugation of the anticancer unsymmetrical bisacridine C-2028 in liver microsomes and cytosol: major role of glutathione S-transferase M1-1 isoenzyme
PublikacjaThis work is the next step in studying the interplay between C-2028 (anticancer-active unsymmetrical bisacridine developed in our group) and the glutathione S-transferase/glutathione (GST/GSH) system. Here, we analyzed the concentration- and pH-dependent GSH conjugation of C-2028 in rat liver microsomes and cytosol. We also applied three recombinant human GST isoenzymes, which altered expression was found in various tumors. The...
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Effects of Surface Energy and Surface Residual Stresses on Vibro-Thermal Analysis of Chiral, Zigzag, and Armchair Types of SWCNTs Using Refined Beam Theory
PublikacjaIn this article, vibration characteristics of three different types of Single-Walled Carbon Nanotubes (SWCNTs) such as armchair, chiral, and zigzag carbon nanotubes have been investigated considering the effects of surface energy and surface residual stresses. The nanotubes are embedded in the elastic substrate of the Winkler type and are also exposed to low and high-temperature environments. A new refined beam theory namely, one-variable...
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Fluoride as a factor initiating and potentiating inflammation in THP1 differentiated monocytes/macrophages
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Synthetic analogues of cyanobacterial alkaloid cylindrospermopsin and their toxicological activity
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The role of the enzymatic antioxidant system in cylindrospermopsin-induced toxicity in human lymphocytes
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Toxicity of cylindrospermopsin in human lymphocytes: Proliferation, viability and cell cycle studies
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Combination of ABT-737 and resveratrol enhances DNA damage and apoptosis in human T-cell acute lymphoblastic leukemia MOLT-4 cells
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Lifespan of etoposide-treated human neutrophils is affected by antioxidant ability of quercetin
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A rapid assay of human thyroid peroxidase activity
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Improved cytotoxicity and preserved level of cell death induced in colon cancer cells by doxorubicin after its conjugation with iron-oxide magnetic nanoparticles
PublikacjaA promising strategy for overcoming the problem of limited efficacy in antitumor drug delivery and in drug release is the use of a nanoparticle-conjugated drug. Doxorubicin (Dox) anticancer chemotherapeutics has been widely studied in this respect, because of severe cardiotoxic side effects. Here, we investigated the cytotoxic effects, the uptake process, the changes in cell cycle progression and the cell death processes in the...
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Room temperature solvent extraction for simple and fast determination of total concentration of Ca, Cu, Fe, Mg, Mn, and Zn in bee pollen by FAAS along with assessment of the bioaccessible fraction of these elements using in vitro gastrointestinal digestion
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Characteristic and specificity of protease activity of thermophilic bacteria Meiothermus ruber
PublikacjaThe primary purpose of research was to establish the possibility of using thermophilic bacteria Meiothermus ruber as a source of proteolytic enzymes. The main reason of searching new proteases is their commercial value especially in production of detergents, food, pharmaceuticals, leather, diagnostics or waste management. The development of this type processes will be possible by utilization of enzymes which have unique characteristics...
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Comparison of hydrogen bonds and diverse weak interactions of the nitro group in 2-methyl-4-nitroanilinium nitrate, bisulfate and two hexafluoridosilicates: elementary graph-set approach
PublikacjaCrystal structures of (H2m4na)NO3 (1), (H2m4na)HSO4 (2), (H2m4na)2SiF6 (3) and (H2m4na)2SiF6*2H2O (4), where 2m4na = 2-methyl-4-nitroaniline, are presented. Two layers of interactions occur in the structures, N—H...O/F hydrogen bonds and interactions with the nitro group. Although diverse, hydrogen-bonding patterns are compared with each other by means of interrelations among elementary graph-set descriptors and descriptors of hydrogen-bonding...
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2-Methoxyestradiol and Hydrogen Peroxide as Promising Biomarkers in Parkinson’s Disease
PublikacjaEstrogens function in numerous physiological processes including controlling brain cell growth and differentiation. 2-Meth- oxestradiol (2-ME2), a 17β-estradiol (E2) metabolite, is known for its anticancer effects as observed both in vivo and in vitro. 2-ME2 affects all actively dividing cells, including neurons. The study aimed to determine whether 2-ME2 is a potentially cancer-protective or rather neurodegenerative agent in a...
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Double layer adhesive silicone dressing as a potential dermal drug delivery film in scar treatment
PublikacjaThe present studies focused on the evaluation of design of an adhesive silicone film intended for scar treatment. Developed silicone double layer film was examined in terms of its future relevance to therapy and applicability on the human skin considering properties which included in vitro permeability of water vapor and oxygen. In order to adapt the patches for medical use in the future there were tested such properties as...
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Degradation of tetracycline antibiotic utilizing light driven-activated oxone in the presence of g-C3N4/ZnFe LDH binary heterojunction nanocomposite
PublikacjaIn the present study, a binary heterojunction nanocomposite composed of graphitic carbon nitride (g-C3N4) and Zn/Fe-contained layered double hydroxide (ZnFe LDH) was employed as heterogeneous catalyst for the decomposition of tetracycline (TC) antibiotic utilizing Oxone and UV light irradiation. The sole use of g-C3N4/ZnFe LDH as adsorbent led to the negligible elimination of TC. In addition, the sole use of Oxone or UV (photolysis)...
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On the electronic structure of methyl butyrate and methyl valerate
PublikacjaWe present novel results of the analysis of the electronic structure of two aliphatic esters: methyl butyrate and methyl valerate. High-resolution photoabsorption spectra were collected and analyzed over the energy range 4.0–10.8 eV and showed for both the molecules not only a clear band of the HOMO to LUMO transition, but also vibronic structure associated with the first Rydberg-valence transition. Photoelectron spectra recorded...
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Antitumor Activity of Triazine Mimic Antibiotics for DNA-binding Implications (Impressive Activity in Vitro Against a Variety of Tumor Types in the NCI-60 Screen): NSC 710607 To Fight HCT-116 Human Colon Carcinoma Cell Lines in Vivo Using the Hollow Fiber Assay and Xenograft Mouse Models
PublikacjaPurpose Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. Methods The NCI initial hollow...
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Advanced oxidation processes (AOPs) based wastewater treatment - unexpected nitration side reactions - a serious environmental issue: A review
PublikacjaChemical compounds containing nitro group (nitro-products) are a one of toxic by-products, that can be formed during wastewater treatment processes. In case of presence of nitrite or nitrate ions, the formation of nitro-products during advanced oxidation processes (AOPs) is very common. It is caused by the reactive nitrogen species (RNs) such as nitrate radical (NO3•), nitrite radical (NO2•), nitrogen oxide radical (NO•) and peroxynirite...
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Nitrofurazone Removal from Water Enhanced by Coupling Photocatalysis and Biodegradation
Publikacja(1) Background: Environmental contamination with antibiotics is particularly serious because the usual methods used in wastewater treatment plants turn out to be insufficient or ineffective. An interesting idea is to support natural biodegradation processes with physicochemical methods as well as with bioaugmentation with efficient microbial degraders. Hence, the aim of our study is evaluation of the effectiveness of different...
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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
PublikacjaCancer 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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DNAffinity: a machine-learning approach to predict DNA binding affinities of transcription factors
PublikacjaWe present a physics-based machine learning approach to predict in vitro transcription factor binding affinities from structural and mechanical DNA properties directly derived from atomistic molecular dynamics simulations. The method is able to predict affinities obtained with techniques as different as uPBM, gcPBM and HT-SELEX with an excellent performance, much better than existing algorithms. Due to its nature, the method can...
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Changes in enzymatic activity of fish and slaughter animals meat after high pressure treatment at subzero temperatures
PublikacjaThe aim of this study was to determine changes in the activity of proteolytic enzymes and transglutaminase of fish and mammal meat after pressurization at subzero temperatures. The activity was measured at the optimal pHs determined for enzymes from particular types of tested meat. It was found that increasing the pressure in the range of 60–193 MPa, did not change significantly the activity of acidic proteases of cod flesh, while...
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Absolute Photoabsorption Cross-Sections of Methanol for Terrestrial and Astrophysical Relevance
PublikacjaWe investigate the methanol absorption spectrum in the range 5.5–10.8 eV to provide accurate and absolute cross-sections values. The main goal of this study is to provide a comprehensive analysis of methanol electronic-state spectroscopy by employing high-resolution vacuum ultraviolet (VUV) photoabsorption measurements together with state-of-the-art quantum chemical calculation methods. The VUV spectrum reveals several new features...
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Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals
PublikacjaAntifungal polyene macrolide antibiotics Amphotericin B (AmB) and Nystatin (NYS) were conjugated through the ω-amino acid linkers with diwalled “molecular umbrellas” composed of spermidine-linked deoxycholic or cholic acids. The presence of “umbrella” substituents modulated biological properties of the antibiotics, especially their selective toxicity. Some of the AmB-umbrella conjugates demonstrated antifungal in vitro activity...
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublikacjaHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Immunomodulation of macrophages activity in murine bacteremia model
PublikacjaZaprezentowano wyniki badań in vitro i in vivo połączeń muramylodipeptydu (MDP) z tetrapeptydem jakim jest tuftsyna. Otrzymane rezultaty pokazują, że badane związki modulują fagocytarne możliwości makrofagów w mysim modelu bakteryjnym.
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublikacjaNew unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of tumor cell lines but also against human tumor xenografts in nude mice. Representative UA compounds, named C-2028, C-2045 and C-2053, were characterized in respect to their physicochemical properties and the following studies aimed to elucidate the role of metabolic transformations in UAs action. We demonstrated with phase I and phase II enzymes...
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Synthesis and antitumor activity of conjugates of muramyldipeptide or normuramyldipeptide with hydroxyacridine/acridone derivatives
PublikacjaOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej pochodnymi hydroksyakrydyny/akrydonu i dwóch analogów modyfikowanych pochodnymi 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny. Tylko związki zawierające pochodne 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny wykazały wysoką aktywność cytotoksyczną badaną na 60 liniach ludzkich komórek nowotworowych, na nowotwór prostaty i AIDS-related lymphoma (ARL). Związek...
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Aromatic heptaene antibiotics as an alternative for synthetic triazole fungicides in plant protection
PublikacjaAn in vitro antifungal activity of candicidin and ascosin antibiotics (0,01-10 μg/mL) towards representative strains of phytopathogenic fungi was detd. Both compds. exhibited similar half max. effective concns. inhibiting growth of the fungi as that of tebuconazole used for comparison.
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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublikacjaAbstract: Background: It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective: The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian vitro toxicity of thus prepared AmB derivatives. Methods:...
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Synthesis of parametric images in the medical active thermography
PublikacjaArtykuł przedstawia zastosowanie nowej metody syntezy obrazów w termografii dla potrzeb opisu ilościowego właściwości termicznych tkanek. opis taki umożliwia różnicowanie przypadków medycznych. Metodę zastosowania dla licznych pomiarów fantomowych oraz in vitro. Przedstawiono i omówiono rezultaty prac.
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The extracts from Panax quinquefolium shoots derived from somatic embryos accumulate ginsenosides and have the antioxidant properties
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Phototransformation of three selected pharmaceuticals, naproxen, 17α-Ethinylestradiol and tetracycline in water: Identification of photoproducts and transformation pathways
PublikacjaTransformation products (TPs) may be formed during various processes, however, it was proved that one of the main mechanisms responsible for degradation of pharmaceuticals in natural waters is photolysis. Three compounds were selected, tetracycline (TC), 17-α-ethinylestradiol (EE2) and naproxen (NAP), for degradation experiments which were performed using a xenon lamp emitting light with a spectrum closely approximating that of...
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Chemical variability of Rhododendron tomentosum (Ledum palustre) essential oils and their pro-apoptotic effect on lymphocytes and rheumatoid arthritis synoviocytes
PublikacjaRhododendron tomentosum (Ledum palustre) is an aromatic plant traditionally used for alleviating rheumatic complaints which makes it a potential candidate for a natural drug in rheumatoid arthritis (RA) treatment. However, the effects of plants’ volatiles on apoptosis of synovial fibroblasts and infiltrating leucocytes of RA synovia, have not been reported. Volatile fraction of R. tomentosum is chemically variable and chemotypes...
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Combined anticancer therapy with imidazoacridinone analogue C‐1305 and paclitaxel in human lung and colon cancer xenografts—Modulation of tumour angiogenesis
PublikacjaThe acridanone derivative 5-dimethylaminopropylamino- 8- hydroxytriazoloacridinone (C-1305) has been described as a potent inhibitor of cancer cell growth. Its mechanism of action in in vitro conditions was attributed, among others, to its ability to bind and stabilize the microtubule network and subsequently exhibit its tumour- suppressive effects in synergy with paclitaxel (PTX). Therefore, the objective of the present study...
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Induction of napthoquinone and flavonoid production in Dionaea muscipula and Drosera capensis
PublikacjaMetabolity (naftochinony: plumbagina i ramantaceon, flawonoidy: mirecytyna i kwercetyna) z roślin Droseraceae: Dionaea muscipula i Drosera capensis są używane jako leki przeciwnowotworowe i przeciwkurczowe. Przedstawiono zdolności indukowania produkcji tych metabolitów, przez odpowiednie warunki elicytacji w hodowli in vitro.
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Nutraceutical value of persimmon (Diospyros kaki Thunb.) and its influence on some indices of atherosclerosis in an experiment on rats fed cholesterol-containing diet
PublikacjaThe nutraceutic value of persimmon (Diospyros kaki Thunb. cv. Triumph) and its influence on some indices of atherosclerosis were studied in vitro and in experiment on rats fed cholesterol-containing diet. It was found that persimmon possesses a high nutraceutical value: it contains soluble fibers, total polyphenols and phe - nolic acids. The content of dietary fiberwas 1.83 ± 0.11, 0.69 ± 0.07 and 1.14 ± 0.12 g/100 g fresh weight...
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Multilayer thermal model of healty and burned skin
PublikacjaW pracy przedstawiono spójny model cieplny skóry wraz z tkankami podskórnymi, na podstawie pomiarów "in vitro" na świni domowej. Model uwzględnia rozkład temperatury, przewodności cieplnej oraz efuzyjności i dyfuzyjności cieplnej w funkcji głębokości, zarówno dla skóry zdrowej jak i oparzonej.
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Role of thermographic inspection in cardiosurgery.
PublikacjaArtykuł przedstawia zastosowanie nowych metod diagnostyki i monitoringu śródoperacyjnego serca bazujących na pomiarach termograficznych oraz elektroimpedancyjnych. Metodę aktywnej termografii dynamicznej zastosowano in vitro w eksperymentach na zwierzętach (świnia domowa) podczas rozwijającego się zawału mięśnia serca. Przedstawiono i omówiono rezultaty prac.
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Cancer stem cells in drug resistance and drug screening: can we exploit the cancer stem cell paradigm in search for new antitumor agents?
PublikacjaPraca przedstawia przegląd literatury dotyczącej hipotezy komórek pierwotnych nowotworu, w szczególności w ich oporności na istniejące terapie. Dyskutowane jest także zagadnienie możliwości wykorzystania wiedzy o tych komórkach do konstrukcji nowych testów do badań przesiewowych in vitro w celu poszukiwania nowych leków przeciwnowotworowych.
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Data processing methods for dynamic medical thermography.
PublikacjaArtykuł przedstawia zastosowanie nowej metody syntezy obrazów w termografii dla potrzeb opisu ilościowego właściwości termicznych tkanek. Opis taki umożliwia różnicowanie przypadków medycznych. Metodę zastosowania dla licznych pomiarów fantomowych i in vitro w eksperymentach na zwierzętach (świnia domowa). Przedstawiono i omówiono rezultaty prac.
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Effect of modification of 6-[(aminoalkyl)amino]-7H-benzo[e]-perimidin-7-ones on their cytotoxic activity toward sensitive and multidrug resistant tumor cell lines. Synthesis and biological evaluation
PublikacjaPrzeprowadzono syntezę szeregu nowych pochodnych benzoperimidynowych, a mianowicie: monohydroksybenzoperimidyny i 2-aminobenzoperimidyny. Oznaczono aktywność przeciwnowotworową in vitro powyższych związków względem komórek nowotworowych bez oporności oraz z wykształconą opornością wielolekową. Wyznaczono również powinowactwo pochodnych do błony komórkowej, na kolumnie HPLC z odpowiednim wypełnieniem.
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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublikacjaThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
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Wpływ zmiany parametrów geometrycznych na wydajność i efektywność protezy zastawki aortalnej Human Aortic Bioprosthesis
PublikacjaW pracy wykazano na podstawie rezultatów badań in vitro, że konstrukcja wykonana z nanocelulozy bakteryjnej, posiada wszelkie cechy protezy zastawki aortalnej możliwe do wykazania na drodze ww. badań oraz że określone cechy geometrii protezy wpływają na jej efektywność i funkcjonalność. W szczególności, w pracy przedstawiono wyniki badań in vitro trzech modeli konstrukcji protezy zastawki aortalnej, oznaczonych M2, M4’ i M4. Badania...