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Wyniki wyszukiwania dla: UGT METABOLIC TRANSFORMATIONS
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Adenylate Kinase 4—A Key Regulator of Proliferation and Metabolic Shift in Human Pulmonary Arterial Smooth Muscle Cells via Akt and HIF-1α Signaling Pathways
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Glukuronidacja leków przeciwnowotworowych – detoksyfikacja, mechanizm oporności czy sposób na formę proleku?*
PublikacjaKsenobiotyki podlegają w organizmie biotransformacji I i II fazy, której celem jest ich detoksyfikacja i ułatwienie wydalania. UDP-glukuronylotransferazy (UGT) – enzymy należące do II fazy metabolizmu katalizują przyłączenie kwasu glukuronowego do lipofilowego substratu zawierającego nukleofilową grupę funkcyjną. Nadrodzina UGT składa się z izoenzymów o różnej swoistości substratowej oraz odmiennym profilu ekspresji w poszczególnych tkankach....
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The role of glucuronidation in drug resistance
PublikacjaThe final therapeutic effect of a drug candidate, which is directed to a specific molecular target strongly depends on its absorption, distribution, metabolism and excretion (ADME). The disruption of at least one element of ADME may result in serious drug resistance. In this work we described the role of one element of this resistance: phase II metabolism with UDP-glucuronosyltransferases (UGTs). UGT function is the transformation...
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublikacjaBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Sex hormone-binding globulin (SHBG) mitigates ER stress and improves viability and insulin sensitivity in adipose-derived mesenchymal stem cells (ASC) of equine metabolic syndrome (EMS)-affected horses
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UDP-glukuronylotransferazy - białka siateczki śródplazmatycznej. Struktura i mechanizm działania
PublikacjaIzoenzymy UDP-glukuronylotransferazy (EC. 2.4.1.17), UGT, katalizują w organizmach ssaków reakcję koniugacji grupy glikozylowej pochodzącej z nukleotydu UDPGA z aglikonem. UDPGA jest przyłączany do odpowiedniej grupy funkcyjnej metabolitu I fazy, rzadziej związku wyjściowego, przez co polarność aglikonu i zdolność jego wydalania z komórki zwiększa się, a to w konsekwencji obniża efekt toksyczny.Struktura UGT zawiera 2 domeny. Domena...
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OPTIMAL FARM SIZE AND EFFECTIVENESS OF AGRICULTURE IN THE EU: THE CASE OF WHEAT YIELDS
PublikacjaThe article concentrates on the relationship between the size of a farm and its efficiency in relation to wheat production in the European Union (EU). The issue is not new, however fundamental from the point of view of the agricultural policy, as the appropriate shape of the agrarian structure affects the economic rationality in agriculture and significantly improves the productivity. We analysed data for the period between 2004...
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Mechanism of Isomerization and Acid-Induced Transformations of 3-Hydroxy-4,4'-dimethoxy-3'-methyl-3-oxo-7,7'-bis(piperidino-carbonyloxy)-2,2'-spirobi-[2H,2'H,3H,3'H-benzo[b]thiophene]. Unusual Equilibrium between the Spiro and 3-Hydroxy-benzothiophene Systems.
PublikacjaStwierdzono, że 3'-hydroksy-4,4'-dimetoksy-3'-metylo-3-okso-7,7'-bis(piperydynokarbonyloksy)-2,2'-spirobi[2H,2'H,3H,3'H-benzo[b]tiofen] występuje w roztworach postaci mieszaniny dwóch diastereoizomerów pozostających w dynamicznej równowadze. Mechanizm tej równowagi oparty jest na odwracalnym otwarciu pierścienia z 1,5 przeniesieniem protonu i utworzeniu przjściowej formy 3-hydroksybenzotiofenu.
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Prediction of Overall In Vitro Microsomal Stability of Drug Candidates Based on Molecular Modeling and Support Vector Machines. Case Study of Novel Arylpiperazines Derivatives
PublikacjaOther than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline. The ideal drug candidate should be stable enough to reach its therapeutic site of action. Despite many recent excellent achievements in the field of computational methods supporting drug metabolism studies, a well-recognized procedure to model...
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Human UDP-Glucuronosyltransferases: Effects of altered expression in breast and pancreatic cancer cell lines.
PublikacjaIncreased aerobic glycolysis and de novo lipid biosynthesis are common characteristics of invasive cancers. UDP-glucuronosyltransferases (UGTs) are phase II drug metabolizing enzymes that in normal cells possess the ability to glucuronidate these lipids and speed their excretion; however, de-regulation of these enzymes in cancer cells can lead to an accumulation of bioactive lipids, which further fuels cancer progression. We hypothesize...
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The role of intestine and liver in glucuronidation of the imidazo- and triazoloacridinone antitumor agents, C-1311 and C-1305: High affinity substrates for UGT1A10
PublikacjaCelem przeprowadzonych badań było określenie roli poszczególnych izoform UDP-glukuronylotransferazy (UGT)oraz mikrosomów jelita(HIM)i wątroby (HLM) wyizolowanych od różnych pacjentów w metabolizmie pochodnych akrydonu, związków C-1311 i C-1305. Wykazano, że rodziną UGT katalizującą przemiany C-1305 i C-1311 jest UGT1A, z najwyższą aktywnością wykazywaną przez pozawątrobowy izoenzym UGT1A10. Rozkład aktywności frakcji mikrosomalnych...
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Eigenfaces, Fisherfaces, Laplacianfaces, Marginfaces – How to Face the Face Verification Task
PublikacjaThis paper describes the exhaustive tests of four known methods of linear transformations (Eigenfaces, Fisherfaces, Laplacianfaces and Marginfaces) in the context of face verification task. Additionally, we introduce a new variant of the transformation (Laplacianface + LDA), and the specific interval-based decision rule. Both of them improve the performance of face verification, in general, however, our experiments show that the...
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UDP-glukuronylotranferazy w metabolizmie detoksykacyjnym i aktywacyjnym związków endogennych oraz ksenobiotyków
PublikacjaGlukuronidacja jest główną drogą koniugacji w szlakach metabolizmu i wydalania związków endogennych oraz ksenobiotyków. Reakcja ta jest katalizowana przez UDP-glukuronylotransferazy, UGT, dla których substratami są bilirubina, hormony steroidowe, tyroidowe i kwasy żółciowe, oraz związki egzogenne, w tym leki, związki kancerogenne, chemiczne zanieczyszczenia środowiska i składniki żywności. Z terapeutycznego punktu widzenia szczególnie...
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Multivariate Statistical Approach for Nephrines in Womenwith Obesity
PublikacjaCatecholamines are physiological regulators of carbohydrate and lipid metabolism during stress, but their chronic influence on metabolic changes in obese patients is still not clarified. The present study aimed to establish the associations between the catecholamine metabolites and metabolic syndrome (MS) components in obese women as well as to reveal the possible hidden subgroups of patients through hierarchical cluster analysis...
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublikacjaThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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L'Italie. Gagner à tout prix. L'industrie de l'armenent italien pendant la Grande Guerre
PublikacjaThe chapter outlines the economic and technological transformations of the Italian armament industry during the First World War
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Integrable zero-range potentials in a plane
PublikacjaWe examine general statements in the Wronskian representation of Darboux transformations for plane zero-range potentials. Such expressions naturally contain scattering problem solution. We also apply Abel theorem to Wronskians for differential equations and link it to chain equations for Darboux transforms to fix conditions for further development of the underlying distribution concept. Moutard transformations give a convenient...
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Mentor & Student Reserch Lab
PublikacjaRelacja z realizacji projektów badawczych przygotowanych w ramach Mentor&Student Research Lab - Urban Transformations 2014
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Diminshed toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
PublikacjaThe narrow "therapeutic window" of anti-tumour therapy may be the result of drug metabolism leading to the activation or detoxification of antitumour agents. The aim of this work is to examine (i) whether the diminished toxicity of a potent antitumour drug, C-1748, 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine, compared with its 4-demethyl analogue, C-857, results from the differences between the metabolic pathways for the...
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Adipokine and cytokine levels in non-functioning adrenal incidentalomas (NFAI)
PublikacjaDue to the fact that overweight or obesity is accompanied by hormonally active adrenal tumors: Cushing Syndrome-(CS) and Subclinical Cushing Syndrome (SCS), it is of high interest the correlation between different adipokines and cytokines secreted by adipose tissue, with metabolic disorders and hormonal activity in this group. Even in non-functioning adrenal incidentalomas (NFAI) elevated risk for cardiovascular disease and metabolic...
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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublikacjaHere, we report the metabolic profile and the results of associated metabolic studies of 2-hydroxyacridinone (2-OH-AC), the reference compound for antitumor-active imidazo- and triazoloacridinones. Electrochemistry coupled with mass spectrometry was applied to simulate the general oxidative metabolism of 2-OH-AC for the first time. The reactivity of 2-OH-AC products to biomolecules was also examined. The usefulness of the electrochemistry...
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Sweet grass protection against oxidative stress formation in the rat brain
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Erratum to: Activities of genes controlling sphingolipid metabolism in human fibroblasts treated with flavonoids
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Activities of genes controlling sphingolipid metabolism in human fibroblasts treated with flavonoids
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Evidence for interactions between homocysteine and genistein: insights into stroke risk and potential treatment
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The model homologue of the partially defective human 5,10-methylenetetrahydrofolate reductase, considered as a risk factor for stroke due to increased homocysteine level, can be protected and reactivated by heat shock proteins
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Factors and processes modulating phenotypes in neuronopathic lysosomal storage diseases
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Mitochondrial DNA levels in Huntington disease leukocytes and dermal fibroblasts
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Thyroid Peroxidase as an Autoantigen in Hashimoto’s Disease: Structure, Function, and Antigenicity
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Thyroid Peroxidase Revisited – Whatʼs New?
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In vivo imaging of the human eye using a two-photon excited fluorescence scanning laser ophthalmoscope
PublikacjaBACKGROUND. Noninvasive assessment of metabolic processes that sustain regeneration of human retinal visual pigments (visual cycle) is essential to improve ophthalmic diagnostics and to accelerate development of new treatments to counter retinal diseases. Fluorescent vitamin A derivatives, which are the chemical intermediates of these processes, are highly sensitive to UV light; thus, safe analyses of these processes in humans...
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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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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...
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Effect of microstructure on mechanical properties and corrosion resistance of 2205 duplex stainless steel
PublikacjaThis paper presents results of the research on impact of microstructure of austenitic-ferritic steel of duplex type on its mechanical properties and susceptibility to stress corrosion cracking. As showed, improper processing technologies more and more often used in shipbuilding industry for plates and other half-finished products made of duplex steel may cause significant lowering their properties, which frequently makes their...
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Revealing dynamic changes of the volatile profile of food samples using PTR–MS
PublikacjaVolatile compounds carry valuable information regarding the properties of foodstuffs. Volatiles emitted from food can be used as, for example, indicators of quality, shelf-life, or authenticity. A better understanding of the multitude of transformations which occur during food processing could facilitate the optimisation of production, increase the desirability of food products, and also their wholesomeness. However, as some of...
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Influence of geotechnical conditions on damage states of Gdansk Bay Coast cliff formations
PublikacjaA geotechnical aspect of destruction processes of seashores was identified based on the case of erosion of Gdansk Bay Coast cliff formations. Causative factors of landslide were described in the context of natural phenomena, land development and its anthropogenic transformations. Possible directions of theoretical analysis of changes in groundwater relations were indicated.
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Urine headspace analysis in medical diagnostics
PublikacjaThe analysis of the volatile organic compounds in the bodily fluids such as urine may provide useful information on the patients’ general health. The potential application of urine headspace analysis could facilitate the diagnostics of various diseases such as metabolic disorders, urinary tract diseases and gastrointestinal conditions. Described in this paper are the currently available techniques of urine sample analysis as well...
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Applications of Alkanethiols in Organic Synthesis
PublikacjaThis manuscript is an update to the earlier Science of Synthesis contribution describing methods for the synthesis of alkanethiols. Thiols can be converted into sulfonic, sulfinic, sulfenic acid and their derivatives, sulfides, disulfides, polysulfides, sulfonium salts, and thiiranes, etc. These transformations are accomplished by nucleophilic displacement or addition, oxidation, condensation, or coupling reactions involving thiol...
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System of breath collection and analysis for diseases detection
PublikacjaCollection and study of composition of the exhaled air is now intensively investigated to develop non-invasive medical diagnostics based on presence of metabolic compounds in the exhaled air. The process of collecting and processing of the exhaled air must fulfill relevant conditions to achieve satisfactory results. The paper presents the system of collecting samples of exhaled breath and the proposed methods of its analysis, using...
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The role and scope of architectural and conservation research procedures in the process of restoring the splendour of an architectural monument created after 1945 on the example of the Suburban Railway Station in Gdynia
PublikacjaModern Movement buildings, despite their relatively recent construction, are sometimes affected by radical transformations of layout and form. The railway stations being one of the most important public buildings in the city are a special group of them. Due to long-term and intensive use they may bear the signs of exploitation of parts of its substance and have secondary transformations disharmony with the building. The subject...
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Acyl Meldrum's acid derivatives: application in organic synthesis
PublikacjaThis review is focused on one of the most important classes of Meldrum's acid derivatives commonly known as acyl Meldrum's acids. The preparation methods of these compounds are considered including the recently proposed and rather rarely used ones. The chemical properties of acyl Meldrum's acids are described in detail, including thermal stability and reactions with various nucleiophiles. The possible mechanisms of these transformations...
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Application, design and operation of constructed wetland systems: case studies of systems in the Gdańsk region, Poland
PublikacjaDifferences in operation result from physical, chemical and biological conditions, which directly influence transformations in the whole aquatic-matrix-plants environment. Depending on the quantity of inflowing organic matter load and the rate of biochemical processes, the contaminations could be removed or/and retuned in the system. From this point of view the facility should be designed and operated in such way that the highest...
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Instrumental techniques used in the analysis of exhaled air
PublikacjaExhaled 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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Transforming the Gdansk Bay Area
PublikacjaThe political transformation of Poland in the early nineties from a centrally steered economy to a free market economy entailed changes of the spatial planning system. The impact of these changes on the spatial transformations and current shape of urban structures in the Gdansk Bay Metropolitan Area is apparent and significant. The paper concentrates on the present spatial phenomena of Gdansk Agglomeration resulting from the main...
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Effect of long term service at elevated temperatures on mechanical properties of Manaurite XM reformer tubes
PublikacjaMicrostructure transformations occur in the Manaurite XM cast steel tubes during long-term operation in the reformer furnace were revealed and described. The rela tionship between mechanical properties, an increase of internal diameter of the tube and microstructure degradation is discussed. Static tensile test was performed on two types of samples with different shapes. It has been shown differences in the results of tests...
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Cardinal regenerative features of the MRL mouse
PublikacjaIn 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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A method of self-testing of an analog circuit terminated by an ADC in electronic embedded systems controlled by microcontrollers
PublikacjaA new self-testing method of analog parts terminated by an ADC in electronic embedded systems controlled by microcontrollers is presented. It is based on a new fault diagnosis method based on on-line (i.e. during measurement), transformations of voltage samples of the time response of a tested part to a square pulse - onto localization curves placed in the measurement space. The method can be used for fault detection and single...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublikacjaZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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The Imidazoacridinone Antitumor Drug, C-1311, Is Metabolized by Flavin Monooxygenases but Not by Cytochrome P450s.
PublikacjaPrezentowane w publikacji wyniki badań mają na celu wyjaśnienie roli enzymów wątrobowych w metabolizmie przeciwnowotworowych pochodnych C-1311 oraz C-1330. Oba związki inkubowane były z frakcją mikrosomalną oraz enzymami rekombinantowymi należącymi do grypy cytochromu P450, FMO oraz UGT. Badania wykazały, że oba związki są metabolizowane przez enzymy frakcji mikrosomalnej, ale nie przez enzymy cytochromu P450. Aktywność enzymatyczna...
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The Effect of Long Term Service at Elevated Temperatures on Microstructure Degradation of Austenitic Reformer Tubes
PublikacjaThe paper analyses the relationship between an increase of the inner diameter of tubes made of Manaurite XM cast steel and transformations occurring in their microstructure due to long-lasting operation in methane reformer. Examinations included metallographic analysis with light microscope (LM), scanning electron microscope (SEM) and microanalysis of the chemical composition of precipitates (EDX). It was indicated that there is...