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Wyniki wyszukiwania dla: IN VIVO MEASUREMENTS
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Successive cytotoxicity control by evolutionary surface decorated electronic push-pull green ZnCr-LDH nanostructures: Drug delivery enlargement for targeted breast cancer chemotherapy
PublikacjaThe reason for the increasing bioavailability and biocompatibility of the porous nanomaterials in the presence of different (bio)molecules is still unknown. The role of difference functional groups and their interactions with the potential bioavailability and biocompatibility is of great importance. To investigate the potential contribution of the electronic effects (especially on the surface of the porous nanomaterials) on their...
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Synthesis, Chemical Characterization and Multiscale Biological Evaluation of a dimericcRGD Peptide for Targeted Imaging of αVβ3 Integrin Activity
PublikacjaCyclic 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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Honey antibacterial activity: A neglected aspect of honey quality assurance as functional food
PublikacjaBackground Honey is considered as a functional food with health-promoting properties. Its potent antibacterial and antibiofilm effects are the major attributes of so called ‘medical-grade honey’ which is topically used for the treatment of burns, wounds and skin disorders. Nevertheless, the current set of honey quality parameters adopted in the European Union do not include its biological properties. Furthermore, in light of the...
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Determination of estrogenic endocrine disruptors in environmental samples - a review of chromatographic methods
PublikacjaWśród związków endokrynnych to estrogeny zarówno naturalne jak i syntetyczne zostały wskazane i opisane jako związki niosące ze sobą największy potencjał aktywności estrogennej. Wysoki potencjał estrogenny jaki posiadają związki z grupy hormonów płciowych potwierdziły badania przeprowadzone zarówno in vitro jak i in vivo. W dużej części (50-95%) próbek ścieków pochodzących z oczyszczalni ścieków zostały wykryte związki z grupy...
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Generation and Characterization of a DNA-GCN4 Oligonucleotide-Peptide Conjugate: The Impact DNA/Protein Interactions on the Sensitization of DNA
PublikacjaRadiotherapy, the most common therapy for the treatment of solid tumors, exerts its effects by inducing DNA damage. To fully understand the extent and nature of this damage, DNA models that mimic the in vivo situation should be utilized. In a cellular context, genomic DNA constantly interacts with proteins and these interactions could influence both the primary radical processes (triggered by ionizing radiation) and secondary reactions,...
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Molecular basis for the DNA damage induction and anticancer activity of asymmetrically substituted anthrapyridazone PDZ-7
Publikacjanthrapyridazones, imino analogues of anthraquinone, constitute a family of compounds with remarkable anti-cancer activity. To date, over 20 derivatives were studied, of which most displayed nanomolar cytotoxicity towards broad spectrum of cancer cells, including breast, prostate and leukemic ones. BS-154, the most potent derivative, had IC50 values close to 1 nM, however, it was toxic in animal studies. Here, we characterize another...
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A standardised static in vitro digestion method suitable for food – an international consensus
PublikacjaSimulated gastro-intestinal digestion is widely employed in many fields of food and nutritional sciences, as conducting human trials are often costly, resource intensive, and ethically disputable. As a consequence, in vitro alternatives that determine endpoints such as the bioaccessibility of nutrients and non-nutrients or the digestibility of macronutrients (e.g. lipids, proteins and carbohydrates) are used for screening and building...
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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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Teloxantron inhibits the processivity of telomerase with preferential DNA damage on telomeres
PublikacjaTelomerase reactivation is one of the hallmarks of cancer, which plays an important role in cellular immortalization and the development and progression of the tumor. Chemical telomerase inhibitors have been shown to trigger replicative senescence and apoptotic cell death both in vitro and in vivo. Due to its upregulation in various cancers, telomerase is considered a potential target in cancer therapy. In this study, we identified...
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Instrument detection and pose estimation with rigid part mixtures model in video-assisted surgeries
PublikacjaLocalizing instrument parts in video-assisted surgeries is an attractive and open computer vision problem. A working algorithm would immediately find applications in computer-aided interventions in the operating theater. Knowing the location of tool parts could help virtually augment visual faculty of surgeons, assess skills of novice surgeons, and increase autonomy of surgical robots. A surgical tool varies in appearance due to...
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Activation of endogenous regenerative potential in mammals using epigenetic inhibitor zebularine
PublikacjaIn this work, a nucleoside inhibitor of DNA methyltransferases, zebularine, was investigated as a wound healing and regeneration promoting agent. It was found that a high dose of intraperitoneally delivered zebularine improved punch wound closure in the ear pinna in mice. Both cytidine, a zebularine analogue, and uridine, a zebularine metabolite, did not promote ear pinna hole closure. The effect of zebularine on ear pinna healing...
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NUTRITIONAL AND PHARMACEUTICAL APPLICATIONS OF BIOACTIVE COMPOUNDS IN TROPICAL FRUITS
PublikacjaDuring the past two decades our international scientific group investigated in vitro the physicochemical and nutritional characteristics of some cultivars of durian at various stages of ripening, mangosteen and new cultivars of snake fruit in comparison with widely used avocado, kiwifruit and mango, and in vivo their influence on laboratory animals. The main objective of the present study was to screen and compare the properties...
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Techniki elektroimpedancyjne w medycynie.Monografie nr 43.
PublikacjaPierwsze aplikacje techniki elektroimpedancyjnej w warunkach klinicznych mają miejsce w latach pięćdziesiątych poprzedniego wieku. Były one związane z próbami oceny przepływu kończynowego za pomocą pletyzmografii impedancyjnej.Od tego czasu technika elektroimpedancyjna, z różnym powodzeniem, była wprowadzana do różnych działów medycyny, np. kardiologii, kardiochirurgii, czy intensywnej opieki medycznej. W znakomitej większości...
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Molecular basis of lipopolysaccharide heterogeneity in Escherichia coli: envelope stress-responsive regulators control the incorporation of glycoforms with a third 3-deoxy-α-D-manno-oct-2-ulosonic acid and rhamnose.
PublikacjaMass spectrometric analyses of lipopolysaccharide (LPS) from isogenic Escherichia coli strains with nonpolar mutations in the waa locus or overexpression of their cognate genes revealed that waaZ and waaS are the structural genes required for the incorporation of the third 3-deoxy-α-D-manno-oct-2-ulosonic acid (Kdo) linked to Kdo disaccharide and rhamnose, respectively. The incorporation of rhamnose requires prior sequential incorporation...
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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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Nowe rozwiązania metodyczne i techniczne w zakresie techniki mikroekstrakcji do fazy stracjonarnej
PublikacjaSample preparation has been recognized as a critical step of the analytical process, being even considered as the bottleneck of the overall process. Enrichment of target compounds, transfer of the analytes into a solvent compatible with the analytical instrumentation, minimization of potential interferences, and efficient sample clean-up, are among the main aims of sample preparation techniques. In this regard, liquid-liquid extraction...
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publikacja5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Electrochemical simulation of metabolic reduction and conjugation reactions of unsymmetrical bisacridine antitumor agents, C-2028 and C-2053
PublikacjaElectrochemistry (EC) coupled with analysis techniques such as liquid chromatography (LC) and mass spectrometry (MS) has been developed as a powerful tool for drug metabolism simulation. The application of EC in metabolic studies is particularly favourable due to the low matrix contribution compared to in vitro or in vivo biological models. In this paper, the EC(/LC)/MS system was applied to simulate phase I metabolism of the representative...
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Electrophoretic deposition and characterization of composite chitosan/Eudragit E 100 or poly(4-vinylpyridine)/mesoporous bioactive glass nanoparticles coatings on pre-treated titanium for implant applications
PublikacjaTitanium implants are surface-modified to achieve bioactivity and often antibacterial properties. Such surface coatings may increase corrosion degradation and be weakly attached to the substrate. In the present research, biodegradable composite coatings, investigated so far as smart environment-sensitive, slowly releasing silver to the implant neighborhood, were produced as a combination of chitosan (CS) with Eudragit E 100 (EE100)...
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Escherichia coli K-12 suppressor-free mutants lacking early glycosyltransferases and late acyltransferases. Minimal lipopolysaccharide structure and induction of envelope stress response.
PublikacjaTo elucidate the minimal lipopolysaccharide (LPS) structure needed for the viability of Escherichia coli, suppressor-free strains lacking either the 3-deoxy-d-manno-oct-2-ulosonic acid transferase waaA gene or derivatives of the heptosyltransferase I waaC deletion with lack of one or all late acyltransferases (lpxL/M/P) and/or various outer membrane biogenesis factors were constructed. Δ(waaC lpxL lpxM lpxP) and waaA mutants exhibited...
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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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Covalent DNA modification by products of myrosinase catalysed glucosinolate degradation in cell-free system
PublikacjaThe bioactive phytochemicals found in Brassica vegetables belonging to glucosinolates (GLS) and especially the products of their degradation isothiocyanates (ITC) and indoles are regarded as the most promising cancer chemopreventive compounds. These secondary metabolites constitute defence system repelling or preventing the development of agrophages attacking brassica plants. The antibiological properties of these compounds suggest...
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Electrochemistry meets enzymes: Investigation of the biotransformation pathway of C-1311 based on electrochemical simulation in comparison to in vitro methods.
PublikacjaThe knowledge of the metabolic pathways and the biotransformation of new drugs is one of the major challenges in pharmaceutical research. It is crucial for elucidation of degradation routes of the new biologically active compounds, especially in the area of possible toxicity. Conventional in vitro drug metabolism studies are based on incubating drug candidate with e.g. hepatocytes or, most importantly, liver cell microsomes and...