Search results for: BIOLOGICAL ACTIVITY, CANCER THERAPY.
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A novel in vitro assay for assessing efficacy and toxicity of antifungals using human leukaemic cells infected with Candida albicans
PublicationAims: This study describes a novel in vitro assay that simultaneously determines antifungal efficiency and host cell toxicity using suspensions of human leukaemic cells (HL-60) infected with Candida albicans. Methods and Results: The effect of Candida infection on host cell viability was evaluated by the microscopy of trypan blue-stained cells and lactate dehydrogenase (LDH) activity. The in vitro ‘drug potency assay’ utilized...
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublicationNew 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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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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Crystal structures of (E)-3-(4-hydroxybenzylidene)chroman-4-one and (E)-3-(3-hydroxybenzylidene)-2-phenylchroman-4-one
PublicationThe synthesis and crystal structures of (E)-3-(4-hydroxybenzylidene)chroman-4-one, C16H12O3,I, and (E)-3-(3-hydroxybenzylidene)-2-phenylchroman-4-one,C22H16O3,II, are reported. These compounds are of interest with respect to biological activity. Both structures display intermolecular C—H---O and O—H---O hydrogen bonding, forming layers in the crystal lattice. The crystal structure of compound I is consolidated...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis of functionalized new conjugates of batracylin with tuftsin/ retro-tuftsin derivatives and their biological evaluation
PublicationNew batracylin conjugates with tuftsin/retro-tuftsin derivatives were designed and synthesized using T3P as a coupling agent. The conjugates possess an amide bond formed between the carboxyl group of heterocyclic molecule and the N-termini of the tuftsin/retro-tuftsin chain. The in vitro cytotoxic activity of the new analogues and their precursors was evaluated using a series of human and murine tumor cells. BAT conjugates containing...
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PVA-Based Films with Strontium Titanate Nanoparticles Dedicated to Wound Dressing Application
PublicationBioactive materials may be applied in tissue regeneration, and an example of such materials are wound dressings, which are used to accelerate skin healing, especially after trauma. Here, we proposed a novel dressing enriched by a bioactive component. The aim of our study was to prepare and characterize poly(vinyl alcohol) films modified with strontium titanate nanoparticles. The physicochemical properties of films were studied,...
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Bioavailability of Tannins and Other Oligomeric Polyphenols: a Still to Be Studied Phenomenon
PublicationPurpose of Review Polyphenols are a group of plant secondary metabolites characterized with the presence ofmultiples of phenol structural units. Tannins are plant originated phenolic substances, which play an important role in plant defense system as well as have found applications in medicine, industry, and other fields of human activity. Despite these, the mechanisms of bioavailability of these substances are poorly studied and...
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Invasive micropapillary carcinoma of breast - Female, 57 - Tissue image [3160630004749761]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Invasive micropapillary carcinoma of breast - Female, 57 - Tissue image [3150630005268201]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Anticancer Imidazoacridinone C-1311 is Effective in Androgen-Dependent and Androgen-Independent Prostate Cancer Cells
PublicationAndrogen receptor (AR) plays a crutial role in prostate cancer (PCa) development and metastasis. Here, we reported potent anti-PCa activity of a small molecule imidazoacridinone C-1311. In AR-positive PCa cells, C-1311 was found to inhibit the transcriptional activity of AR uncovering a novel mechanism that may be relevant for its anticancer effect. Mechanistically, C-1311 decreased AR binding to prostate-specific antigen (PSA)...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Metabolic activity of tree saps of different origin towards cultured human cells in the light of grade correspondence analysis and multiple regression modeling
PublicationTree saps are nourishing biological media commonly used for beverage and syrup production. Although the nutritional aspect of tree saps is widely acknowledged, the exact relationship between the sap composition, origin, and effect on the metabolic rate of human cells is still elusive. Thus, we collected saps from seven different tree species and conducted composition-activity analysis. Saps from trees of Betulaceae, but not from...
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublicationFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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Selected Methods for the Chemical Phosphorylation and Thiophosphorylation of Phenols
PublicationThis Focus Review gathers together a selection of methods for the chemical phosphorylation of phenols that employ three‐ and four‐coordinate phosphorus compounds. Phosphorylated scaffolds can exhibit enhanced properties compared to their non‐phosphorylated analogues, such as increased biological activity and increased/decreased solubility; as such, phosphorus compounds have gained more and more interest in organic and medicinal...
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Quantum dots conjugates with unsymmetrical bisacridines enhance cytotoxicity of these antitumor compounds in lung cancer cells and have protecting effects on normal cells
PublicationBackground: In recent years, with the rapid development of nanotechnology and its extensive applications in the medicine, nanocarriers for anticancer drug delivery have gained a great importance. Spherical semiconductor nanocrystals, frequently called quantum dots (QDs) are very attractive nanomaterials for bioimaging applications and they possess properties as potential candidates for drug carrier. Unsymmetrical bisacridines (UAs),...
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Isothiocyanates may chemically detoxify mutagenic amines formed in heat processed meat
PublicationMeat consumption represents a dietary risk factor increasing the incidence of common cancers, probably due to carcinogenic amines (HAAs) formed upon meat heating. Interestingly, cancers whose incidence is increased by meat consumption, are decreased in populations consuming brassica vegetables regularly. This inverse correlation is attributed to brassica anticarcinogenic components, especially isothiocyanates (ITCs) that stimulate...
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Adipokine and cytokine levels in patients with adrenocortical cancer, subclinical Cushing's syndrome and healthy controls
PublicationIntroduction In recent years researchers have focused at hormonal activity in Cushing’s syndrome (CS) in connection with metabolic disorders and the role of adipokines and cytokines secreted by the adipose tissue. The aim of the study was to investigate levels of adipokines and cytokines in patients with: subclinical CS (SCS) – in relation to hormonal parameters of hypercortisolemia, and, adrenocortical cancer (ACC). Materials...
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Determination of COD Fractionation as a Key Factor for Appropriate Modelling and Monitoring of Activated Sludge Processes
PublicationAn operation of wastewater treatment plant is usually controlled by global parameters such as flow, solids retention time, sludge age, concentration of ammonia and dissolved oxygen, etc. It is considered that, together with the chemical and biological oxygen demand (COD and BOD), those parameters indirectly exhibit the effectiveness of activated sludge processes. Especially the BOD indicate the amount of organic pollution that...
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ANTIOXIDANT POWER SERIES (APS) AS A TOOL FOR RATIONAL DESIGN AND ASSESSMENT OF HEALTH PROMOTING PROPERTIES OF FUNCTONAL FOODS BASED ON ANTIOXIDANT PHYTOCHEMICALS
PublicationOver past decades, plantborne antioxidants dominated so called "translational research" in the area of food, nutrition, and disease prevention. Among consumers and producers, such phytochemicals are synonyms of nutriceuticals. Popularity and commercial success of antioxidants stems from mechanistic studies suggesting the involvement of reactive oxygen species in etiology of chronic diseases. However, epidemiology failed to provide...
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Biological and mechanical research of titanium implants covered with bactericidal coating
PublicationThe paper concerns the biological and mechanical properties of titanium implants with an antibacterial coating. The Ti13Zr13Nb alloy samples were coated with hydroxyapatite (HAp) coatings using the electrophoretic deposition technique (EPD). Subsequently, the surface of the samples was modified with silver, copper, and nickel nanoparticles by the immersion method. Different titanium sample types (i.e. HAp-only and nanometals-enriched...
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Evaluating Gelatin-Based Films with Graphene Nanoparticles for Wound Healing Applications
PublicationIn this study, gelatin-based films containing graphene nanoparticles were obtained. Nanoparticles were taken from four chosen commercial graphene nanoplatelets with different surface areas, such as 150 m2/g, 300 m2/g, 500 m2/g, and 750 m2/g, obtained in different conditions. Their morphology was observed using SEM with STEM mode; porosity, Raman spectra and elemental analysis were checked; and biological properties, such as hemolysis...
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Blue-berried honeysuckle a promising cancer preventing fruit; Polish genotypes as a source of bioactive phytochemicals
PublicationFrom the ancient times, plants containing health-oriented compounds in their matrices are used in the treatment of different complaints and diseases. One of these groups are plant secondary metabolites (PSM), especially phenolic compounds, terpenes and terpenoids. A large number of PSM exhibit cytotoxicity against a variety of tumor cells, as well as cancer preventive and anticancer efficacy in preclinical animal models. For this...
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The relationship between standard reduction potentials of catechins and biological activities involved in redox control
PublicationRedox homeostasis involves factors that ensure proper function of cells. The excess reactive oxygen species (ROS) leads to oxidative stress and increased risk of oxidative damage to cellular components. In contrast, upon reductive stress, insufficient ROS abundance may result in faulty cell signalling. It may be expected that dietary antioxidants, depending on their standard reduction potentials (E°), will affect both scenarios....
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Bioreactors and biophoton-driven biohydrogen production strategies
PublicationGiven the current issues with global warming and rising greenhouse gas emissions, biohydrogen is a viable alternative fuel option. Technologies to produce biohydrogen include photo fermentation, dark fermentation, direct and indirect bio-photolysis, and two-stage fermentation. Biological hydrogen generation is a green and promising technique with mild reaction conditions and low energy consumption compared to thermochemical and...
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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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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Seasonal variability and morphological structure of bacteria in the Admiralty Bay (King George Island, Antarctic).
PublicationIntroduction: The aim of investigations was to state whether melting glaciers cause mass mortality of the sea stenohalyne organisms, what in consequence can lead to an increase of accumulation and growth of psychrophilic bacteria. It may be also that fresh melting water is unfavourable to the sea bacteria and front glacier's regions are not the areas of their intensive development. Methods: Field investigations were done in Admiralty...
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Properties and applications of thermostable proteases sourced from Deinococcus geothermalis.
PublicationThe growing interest of extremophiles results from the fact that their enzymes arestable and active under harsh environment conditions. These type of biocatalysts are attractivedue to the fact that can be used in industrial processes that were previously regarded asincompatible with biological materials. Among extremozymes the largest group constitutethermozymes. Currently it is estimated that approximately 40% of enzymes used...
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Wytwarzanie i modyfikacja powierzchni porowatych struktur tytanowych przeznaczonych na implanty
PublicationCelem pracy było wytworzenie stopu Ti-13Nb-13Zr z wykorzystaniem technologii selektywnego topienia laserowego (SLM) oraz jego biofunkcjonalizacja za pomocą utleniania mikrołukowego (MAO), a następnie określenie wpływu parametrów procesowych na właściwości otrzymanych materiałów pod kątem ich zastosowania na implanty. Oceniono wpływ napięcia, natężenia i czasu procesu MAO przeprowadzanego w elektrolicie zawierającym wapń i fosfor...
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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublicationChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublicationNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...
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Estimating the Impact of Inflow on the Chemistry of Two Different Caldera Type Lakes Located on the Bali Island (Indonesia)
PublicationThis paper is a preliminary attempt to assess the composition of pollutants in two different caldera lakes situated in the Indonesian Archipelago: Batur and Bratan. Both lakes are characterized by largely different physico-chemical regimes; Batur Lake is located in an area that is currently volcanically active, unlike Bratan Lake. The latter is much smaller and shallower than Batur Lake. The concentration of pollutants in the Indonesian...
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The occurrence and role of Nitrospira in nitrogen removal systems
PublicationApplication of the modern microbial techniques changed the paradigm about the microorganisms performing nitrification. Numerous investigations recognized representatives of the genus Nitrospira as a key and predominant nitrite-oxidizing bacteria in biological nutrient removal systems, especially under low dissolved oxygen and substrate conditions. The recent discovery of Nitrospira capable of performing complete ammonia oxidation...
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The role of analytical chemistry in the study of the Anthropocene
PublicationThe term “Anthropocene” refers to not yet formalized epoch of geologic time during which geologic processes have been dominated by the human impact. This impact takes on many forms. Biological, physical and chemical changes to the Earth System caused by anthropogenic activity are recorded in natural archives either as new fossil assemblages (neobiota), anthropogenic deposits or a wide variety of pollutants emitted to the environment....
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Sathwik Prathapagiri
PeopleSathwik was born in 2000. In 2022, he completed his Master’s of Science in Biological Sciences and Bachelor’s of Engineering in Chemical Engineering in an integrated dual degree program from Birla Institute Of Technology And Science, Pilani, India. During his final year, he worked as a research intern under Dr Giri P Krishnan at Bazhenov lab, University of California San Diego school of medicine to pursue his Master’s Thesis on...
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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
PublicationHypoxia-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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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublicationAbstract: 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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In Vitro Studies on Nanoporous, Nanotubular and Nanosponge-Like Titania Coatings, with the Use of Adipose-Derived Stem Cells
PublicationIn vitro biological research on a group of amorphous titania coatings of different nanoarchitectures (nanoporous, nanotubular, and nanosponge-like) produced on the surface of Ti6Al4V alloy samples have been carried out, aimed at assessing their ability to interact with adipose-derived mesenchymal stem cells (ADSCs) and affect their activity. The attention has been drawn to the influence of surface coating architecture and its physicochemical...
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublicationThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Structural, functional, and stability change predictions in human telomerase upon specific point mutations,
PublicationOverexpression of telomerase is one of the hallmarks of human cancer. Telomerase is important for maintaining the integrity of the ends of chromosomes, which are called telomeres. A growing number of human disease syndromes are associated with organ failure caused by mutations in telomerase (hTERT or hTR). Mutations in telomerase lead to telomere shortening by decreasing the stability of the telomerase complex, reducing its accumulation,...
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A Perspective on Missing Aspects in Ongoing Purification Research towards Melissa officinalis
PublicationMelissa officinalis L. is a medicinal plant used worldwide for ethno-medical purposes. Today, it is grown everywhere; while it is known to originate from Southern Europe, it is now found around the world, from North America to New Zealand. The biological properties of this medicinal plant are mainly related to its high content of phytochemical (bioactive) compounds, such as flavonoids, polyphenolic compounds, aldehydes, glycosides...
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Invasive breast carcinoma of no special type - Female, 64 - Tissue image [4120730022879511]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 64 - Tissue image [4120730022873711]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 64 - Tissue image [4120730022875471]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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SZTUKA WIZUALNA W OBIEKTACH MEDYCZNYCH = VISUAL ARTS IN MEDICAL FACILITIES
PublicationWspółczesna architektura obiektów służby zdrowia podlega dynamicznym przeobrażeniom formalnym wynikającym zarówno z rozwoju technologii medycznych, zmian zachodzących w podejściu wobec pacjenta. Narastający w naukach medycznych kierunek holistyczny ustawia pacjenta jako użytkownika w trzech wymiarach: biologicznym, społecznym i psychologicznym. Stąd pojawiające się w procesie projektowym dotyczącym szpitali czy przychodni nowe...
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Spatio-Temporal Validation of GNSS-Derived Global Ionosphere Maps Using 16 Years of Jason Satellites Observations
PublicationExisting ionospheric models perform very well in mapping the calm state of the ionosphere. However, the problem is accurately determining the total electron content (TEC) for disturbed days. Knowledge of the exact electron density is essential for single−frequency receivers, which cannot eliminate the ionospheric delay. This study aims to investigate temporal and spatial variability in the distribution of TEC based on differences...
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Two-Level Multivariable Control System of Dissolved Oxygen Tracking and Aeration System for Activated Sludge Processes
PublicationThe problem of tracking dissolved oxygen is one of the most complex and fundamental issues related to biological processes. The dissolved oxygen level in aerobic tanks has significant influence on behaviour and activity of microorganism inhabiting the plant. Aerated tanks are supplied with air from an aeration system (blowers, pipes, throttling valves, diffusers). It is a complex dynamic system governed by nonlinear hybrid dynamics....
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"Food Oxidants and Antioxidants" Book review
PublicationThe book is the 14th title in the CRC series Chemical and Functional Properties of Food Components, edited since 2001 by Zdzisław E. Sikorski. The editor of the book, a professor in the University of Łódź and member of the Polish Academy of Sciences, is an internationally recognized authority in biochemistry and biophysics of reactive oxygen species. In Poland Grzegorz Bartosz has a reputation as the author of his most interesting...
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Self-standing Nanoarchitectures
PublicationDespite there are structures invisible for the human eye, they mastered the world of advanced electronic devices, sensors, novel cosmetics or drugs. When the dimensions of the materials go down to the nanometres scale, their properties change dramatically comparing to the observable objects. Because of their tiny size, they gained the name of nanomaterials but simultaneously their importance has significantly grown up. Nanomaterials...