Search results for: inhibitors of angiogenesis
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Selected symmetrically substituted carbazoles: Investigation of anticancer activity and mechanisms of action at the cellular and molecular levels
PublicationDNA topoisomerases play a critical role as essential enzymes in controlling alterations in the topology of DNA. They achieve this by orchestrating the coordinated process of breaking and rejoining DNA strands, which is crucial for maintaining the proper structure of DNA during regular cellular development. The search for and development of new potential anticancer drugs is a challenging yet immensely important area of research...
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Regulacja aktywności syntazy glukozamino-6-fosforanu z Candida albicans – badania metodami obliczeniowymi
PublicationNiniejsza praca przedstawia wyniki badań, prowadzonych metodami obliczeniowymi, poświęconych enzymowi syntazie GlcN-6-P pochodzącemu z drożdży C. albicans. Enzym ten odpowiedzialny jest między innymi za biosyntezę kluczowych składników ściany komórkowej grzybów i bakterii, ma również wpływ na regulację metabolizmu glukozy. Przedstawione badania stanowią jeden z etapów poszukiwania molekularnego mechanizmu inhibicji, której eukariotyczna...
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Electrochemical, theoretical and surface physicochemical studies of the alkaline copper corrosion inhibition by newly synthesized molecular complexes of benzenediamine and tetraamine with π acceptor
PublicationTwo charge transfer complexes, namely [(BDAH)+(PA−)] CT1 [(BTAH)2+(PA−)2] and CT2 (BDAH = 1,2-benzenediamine, BTAH = 1,2,4,5-benzenetetramine, and PA− = 2,4,6-trinitrophenolate), were synthesized and fully characterized using various spectroscopic techniques. CT1 and CT2 were tested as inhibitors to effectively control the uniform and anodic corrosion processes of copper in an alkaline electrolyte (1.0 M KOH) using various electrochemical...
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Electrochemical investigations on corosivity of de-icing liquids for railway infrastructure
PublicationThe paper presents the results of electrochemical tests of the de-icing fluid for railway infrastructure. DC and AC electrochemical tests were performed to determine the corrosion rates of structural steel, cast iron and aluminium in the newly produced fluid. The results were compared with the corrosion rates of the same materials in the fluid without corrosion inhibitors. The obtained test results indicate a low corrosion risk...
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Amino Acid and Peptide‐Based Antiviral Agents
PublicationA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Korozja w środowisku ropy naftowej. Czynniki i monitorowanie
PublicationPrzedstawiono analizy właściwości ropy naftowej z punktu widzenia zawartych w niej czynników korozyjnych oraz ich wpływu na korozję stali w trakcie procesu destylacji ropy naftowej. Krytycznej analizie poddane zostały możliwości oferowane przez współczesne techniki pomiarowe. Wskazano na istotność prowadzenia kompleksowego programu oceny ropy, monitorowania korozji oraz stosowania ochrony inhibitorowej w celu ochrony instalacji...
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Synthesis, Chemical Characterization and Multiscale Biological Evaluation of a dimericcRGD Peptide for Targeted Imaging of αVβ3 Integrin Activity
PublicationCyclic peptides containing the Arg-Gly-Asp (RGD) sequence have been shown to specifically bind the angiogenesis biomarker α V β3 integrin. We report the synthesis, chemical characterization, and biological evaluation of two novel dimeric cyclic RGD-based molecular probes for the targeted imaging of α V β3 activity (a radiolabeled version, 64Cu-NOTA-PEG4-cRGD2, for PET imaging, and a fluorescent version, FITC-PEG4-cRGD2, for in...
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The protection and monitoring of a distribution piping network for potable water supply
PublicationPurpose – The purpose of this paper is to implement the corrosion protection method for steel pipes used in a municipal water-pipe network. Results of an inhibitor protection system installed on the system are presented. Inhibitor protection was required due to the high corrosivity of the water collected by a surface intake, which had resulted in a large number of failures and low water quality, due to the presence of corrosion...
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Actions of a nitric oxide donor on prostaglandin production and angiogenic activity in the equine endometrium
PublicationNitric oxide (NO) plays an important role in prostaglandin secretion and angiogenesis in the reproductive system. In the present study, the roles of the NO donor spermine NONOate and tumour necrosis factor-alpha (TNF; as a positive control) in prostaglandin production and angiogenic activity of equine endometria during the oestrous cycle were evaluated. In addition, the correlation between NO production...
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The microstructure of AA5754 alloy under corrosion in alkaline media (pH=11) with 20 mM of various carboxylic acids
Open Research DataThis dataset contains scanning electron microscopy (SEM) micrographs taken for polished aluminum AA5754 alloy samples, exposed for 100 min in bicarbonate buffer (pH=11) with the addition of 20 mM of carboxylic acids, namely: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, tricarballylic acid and serine. The goal of this study was...
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The microstructure of AA5754 alloy under corrosion in alkaline media (pH=11) with 4.5 mM of various carboxylic acids
Open Research DataThis dataset contains scanning electron microscopy (SEM) micrographs taken for polished aluminum AA5754 alloy samples, exposed for 100 min in bicarbonate buffer (pH=11) with the addition of 4.5 mM of carboxylic acids, namely: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, tricarballylic acid and serine. The goal of this study was...
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L-Homoserine O-acetyltransferase (CaMet2p) activity and inhibition
Open Research DataThe dataset contains the description of methodology and data files with the results obtained spectrophotometrically at 412 nm to determine the rate of fungal enzyme activity. The goal of the study was to obtain conditions optimal for L-homoserine O-acetyltransferase (Met2p) activity as well as evaluation of inhibitory potential of commercially available...
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Hypericum alpestre extract exhibits in vitro and in vivo anticancer properties by regulating the cellular antioxidant system and metabolic pathway of L‐arginine
PublicationConventional treatment methods are not effective enough to fight the rapid increase in cancer cases. The interest is increasing in the investigation of herbal sources for the development of new anticancer therapeutics. This study aims to investigate the antitumor capacity of Hypericum alpestre (H. alpestre) extract in vitro and in vivo, either alone or in combination with the inhibitors of the L‐arginine/polyamine/nitric oxide...
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Extractive detoxification of hydrolysates with simultaneous formation of deep eutectic solvents
PublicationThe hydrolysis of lignocellulosic biomass results in the production of so-called fermentation inhibitors, which reduce the efficiency of biohydrogen production. To increase the efficiency of hydrogen production, inhibitors should be removed from aqueous hydrolysate solutions before the fermentation process. This paper presents a new approach to the detoxification of hydrolysates with the simultaneous formation of in-situ deep eutectic...
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Selectivity Tuning by Natural Deep Eutectic Solvents (NADESs) for Extraction of Bioactive Compounds from Cytinus hypocistis—Studies of Antioxidative, Enzyme-Inhibitive Properties and LC-MS Profiles
PublicationIn the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. The extracts were found to possess total phenolic and total flavonoid contents in the ranges of 26.47–186.13...
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Synthesis of phosphono and phosphate derivatives of hydroxyimino-D-alditols as new potential antifungal agents
PublicationIn search for new effective we antyfungals we focus on two enzymes involved in biosynthesis of the fungal cell wall. The first enzyme is glucosamine-6-phosphate (GlmS), which catalyzes transformation of D-fructose-6-phosphate (Fru-6P) to D-glucosamine-6-phodphate (GlcN-6P) in the chitin biosynthesis pathway. The second enzyme is phosphomannose isomerase (PMI) repored to play a crucial role in biosynthesis of many mannosylated structures,...
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Enzymes of the lysine biosynthetic pathway as targets for antifungals ?
PublicationSystemic infections caused by human pathogenic fungi in immunocompromized patients continue to be one of the important clinical problems. Limited availability of safe and efficacious antifungal chemotherapeutics and emerging resistance to existing drugs stimulates search for novel molecular targets for antifungals. The α-aminoadipate pathway (AAP) of L-lysine biosynthesis is unique in fungi and thus has been so far considered...
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System monitorowania korozji w instalacjach wodnych platformy wydobywczej Baltic Beta
PublicationRealizacja doktoratu rozwiązała problemy korozyjne w jednym ze strategicznych obszarów procesu eksploatacji ropy. Polegała na uruchomieniu monitoringu korozji w instalacji zatłaczającej wodę morską do złoża ropy, na platformie wydobywczej firmy LOTOS Petrobaltic. Wdrożono automatyczny system monitorowania korozji metodą polaryzacji liniowej, oszacowano korozyjność uzdatnionej wody, zidentyfikowano rodzaje korozji występujące w...
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Evaluation of antimicrobial properties of thermomelt adhesives modified with zinc compounds
Open Research DataThe dataset contains the results of microbiological tests of thermomelt adhesives modified with zinc compounds, whose activity was assessed for their ability to reduce the number of Escherichia coli and Staphylococcus aureus strain, representing the Gram (-) and Gram (+) bacteria, respectively. The evaluation of antimicrobial properties of samples were...
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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublicationAcquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is one of the most challenging diseases in recent decades. Nevertheless the shortcomings of chemical drugs such as toxicity, lack of curative effects, the search for more potent anti-HIV agents have been focused in our study. In current study, novel scaffold was designed having a benzyl and imidazole in it which are very...
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Exploring Mechanism of Corrosion Inhibition of WE43 and AZ31 Alloys by Aqueous Molybdate in Hank’s Solution by Multisine Impedimetric Monitoring
PublicationThe concept of utilizing multisine dynamic electrochemical impedance spectroscopy to monitor effectiveness of a model molybdate inhibitor for AZ31 and WE43 Mg alloys is proposed. The corrosion kinetics and instantaneous values of inhibition efficiency (IE) of molybdate at concentrations up to 150 mM were examined. The inhibitor provides inhibition in Hank’s solution at concentrations starting from ca. 25 mM, with the IE of about...
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Inhibitive effect of sodium molybdate on corrosion of AZ31 magnesium alloy in chloride solutions
PublicationIn this work, corrosion inhibition of the AZ31 magnesium alloy was investigated in NaCl solutions containing different amounts of sodium molybdate inhibitor. Electrochemical, hydrogen evolution, microscopic, and spectroscopic experiments were utilized to examine the mechanism of corrosion inhibition by molybdates. The results showed that Na2MoO4 inhibitor provides reliable inhibition at high concentrations (150 mM). Surface examination...
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Mateusz Daśko dr inż.
PeopleDr inż. Mateusz Daśko urodził się w 1990 roku w Kołobrzegu. Od 2009 roku związany jest z Politechniką Gdańską gdzie uzyskał stopień inżyniera (2013) oraz magistra (2014) na kierunku biotechnologia. W 2014 rozpoczął Studia Doktoranckie na Wydziale Chemicznym Politechniki Gdańskiej, gdzie zajmował się projektowaniem oraz syntezą chemiczną nowych inhibitorów sulfatazy steroidowej jako potencjalnych leków przeciwnowotworowych w grupie...
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Ryszard Andruszkiewicz prof. dr hab. inż.
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Antifungal Effect of Penicillamine Due to the Selective Targeting of L-Homoserine O-Acetyltransferase
PublicationDue to the apparent similarity of fungal and mammalian metabolic pathways, the number of established antifungal targets is low, and the identification of novel ones is highly desirable. The results of our studies, presented in this work, indicate that the fungal biosynthetic pathway of L-methionine, an amino acid essential for humans, seems to be an attractive perspective. The MET2 gene from Candida albicans encoding L-homoserine...
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Therapeutic Potential of Multifunctional Tacrine Analogues
PublicationTacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as a model inhibitor of cholinesterases in the therapy of Alzheimer’s disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we...
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Instantaneous Impedance Analysis of Non-Stationary Corrosion Process: a Case Study of Carbon Steel in 1M HCl
PublicationThe paper concerns the problem of evaluation of stationarity of carbon steel corrosion in 1M HCl. Comparison of corrosion rate with addition of corrosion inhibitor to the reference measurement is the most often used way of evaluating inhibitor efficiency. Such an approach is valid only if corrosion rate is a stationary process. Two complementary techniques were used simultaneously: volumetric analysis of evolved hydrogen and instantaneous...
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Estimation of the effectiveness of nbpt for limiting ammonia emission from urea based on the field experiments
PublicationThe efectiveness of the ammonia emission reduction from NBPT-stabilized urea was investigating in 2011 during a field experiment on a grassland plot fertilized with a one-time dose of 60 kgN/ha. The obtained reduction coefficient of ammonia emission equaled 73% and 39-51% relative to erea without the inhibitor and ammonium nitrate, respectively.
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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Therapeutic intervention by the simultaneous inhibition of DNA repair and type I or type II DNA topoisomerases: one strategy, many outcomes
PublicationMany anticancer drugs reduce the integrity of DNA, forming strand breaks. This can cause mutations and cancer or cell death if the lesions are not repaired. Interestingly, DNA repair-deficient cancer cells (e.g., those with BRCA1/2 mutations) have been shown to exhibit increased sensitivity to chemotherapy. Based on this observation, a new therapeutic approach termed 'synthetic lethality' has been developed, in which radiation...
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Two small RNAs conserved in Enterobacteriaceae provide intrinsic resistance to antibiotics targeting the cell wall biosynthesis enzyme glucosamine-6-phosphate synthase
PublicationFormation of glucosamine-6-phosphate GlcN6P) by enzyme GlcN6P synthase (GlmS) represents the first step in bacterial cell envelope synthesis. In Escherichia coli, expression of glmS is controlled by small RNAs (sRNAs) GlmY and GlmZ. GlmZ activates the glmS mRNA by base-pairing. When not required, GlmZ is bound by adapter protein RapZ and recruited to cleavage by RNase E inactivating the sRNA. The homologous sRNA GlmY activates...
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AFM images of the platinum (111) single crystal surface as delivered, without the polishing treatment
Open Research DataPlatinum (111) single crystal surface images as delivered, without polishing treatment. Topographic measurements in contact mode. NTEGRA Prima (NT-MDT) device. CSG probe 10.
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Roman Kotlowski dr hab. inż.
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Solubilization of keratins and functional properties of their isolates and hydrolysates
PublicationThe keratinous wastes of the textile industry and poultry slaughterhouses may be used as sources of soluble keratins or hydrolysates. This review presents methods for processing raw keratin-based materials into bioproducts with functional and bioactive properties suitable for biomedical, cosmetic, food, and agricultural applications. Soluble keratin can be obtained by thermal treatment in some organic solvents, reduction, or oxidation...
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Thanos Of Titan
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Understanding the origin of high corrosion inhibition efficiency of bee products towards aluminium alloys in alkaline environments
PublicationVarious bee products were found to be efficient corrosion inhibitors of aluminium in different environments. In particular, bee pollen was found to be highly effective in alkaline electrolytes, yet its highly complex composition and possible synergistic interactions hinder determination of the compounds acting as active corrosion inhibitors. The main purpose of the following work is to investigate the effect of solvents used for...
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Glucosamine-6-phosphate synthase,a novel target for antifungalagents.Molecular modelling studies in drug design
PublicationPraca dotyczy modelowania zarówno samych inhibitorów syntazy glukozamino-6-fosforanu jak i ich oddziaływania z obydwiema domenami tego enzymu. Enzym syntaza glukozamino-6-fosforanu został zaproponowany jako nowy cel molekularny w chemoterapii infekcji grzybowych. Zaprojektowano i zsyntezowano szereg inhibitorów tego enzymu - potencjalnych nowych leków przeciwgrzybowych. Dzięki modelowaniu molekularnemu udało się wyjaśnić mechanizm...
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Optimised five-hour multiplex PCR test for the detection of Tinea ungium: performance in a routine PCR laboratory
PublicationWe recently published the development of a 5-hour multiplex PCR test for the detection of dermatophyte nail infection. We have optimized this test by inclusion of an inhibition control and evaluated the test in a routine laboratory when compared to the conventional microscopy and culture. A total of 109 clinical samples received at the mycology reference lab at Statens Serum Institute were included. The samples were divided equally...
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Materials Design for the Titanium Scaffold Based Implant
PublicationThe main objective of here presented research is a design the scaffold/porous titanium(Ti) alloy based composite material demonstrating better biocompatibility, longer lifetime andbioactivity behaviour for load-bearing implants. The development of such material is proposed bymaking a number of consecutive tasks. Modelling the mechanical, biomechanical and biologicalbehavior of porous titanium structure and an elaboration of results...
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Materials Design for the Titanium Scaffold Based Implant
PublicationThe main objective of here presented research is a design the scaffold/porous titanium(Ti) alloy based composite material demonstrating better biocompatibility, longer lifetime andbioactivity behaviour for load-bearing implants. The development of such material is proposed bymaking a number of consecutive tasks. Modelling the mechanical, biomechanical and biologicalbehavior of porous titanium structure and an elaboration of results...
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Dynamic impedance data for various carboxylic acids corrosion inhibition of aluminium in alkaline media (pH=11)
Open Research DataThis dataset contains the results of Dynamic Electrochemical Impedance Spectroscopy (DEIS) carried out in galvanostatic mode under iDC=0, carried out in order to define the corrosion inhibition effect of various studied carboxylic acids: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, carballylic acid, and serine. The experiment...
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Maria Jolanta Milewska prof. dr hab. inż.
PeopleMaria Jolanta Milewska, po ukończeniu Technikum Chemiczno-Mechanicznego w Wąbrzeźnie (specjalizacja: przetwórstwo tworzyw sztucznych) kontynuowała naukę na Wydziale Chemicznym Politechniki Gdańskiej. W 1979 r. zdobywa tytuł mgr inżyniera na kierunku Chemia, o specjalizacji Lekka Synteza Organiczna. Studium Doktoranckie PG ukończyła w 1984 r. W 1983 r została zatrudniona na macierzystym wydziale w Katedrze Chemii Organicznej, początkowo...
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Influence of G2 arrest on the cytotoxicity of DNA topoisomerase inhibitorstoward human carcinoma cells with different p53 status
PublicationRola bloku G2 w efekcie cytotoksycznym inhibitorów DNA topoizomeraz w stosunku do ludzkich komórek rakowych różniących się funkcjonalnością białka p53.
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Poszukiwanie nowych leków immunosupresyjnych (Quest for new immunosuppressive drugs)
PublicationTransplantology is getting more and more important in medicine. Development of surgical techniques and immunosuppressive treatment enabled to establish successful transplantations with various organs and tissues. However, allografts are recognized as foreign tissues and stimulate rejection, i.e. a strong immunological response which, if not stopped, results in complete destruction of the transplanted tissue. In order to prevent...
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Novel fast non-linear electrochemical impedance method for corrosion investigations
PublicationThe paper presents a novel approach to corrosion rate monitoring using non-linear electrochemical impedance spectroscopy. The authors propose a new variant of non-linear impedance measurement using amplitude-modulated multi-frequency ac perturbation signal. It allows shortening of measurement duration so it is possible to monitor corrosion rate of the systems experiencing rapid changes. In this way a limitation resulting from lack...
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Determination of the effective concentration of ketoprofen against the germination of Sorghum bicolor (sorghum) seeds
Open Research DataResearch data includes an attempt to determine the effective concentration of ketoprofen that inhibits germination of Sorghum bicolor (sorghum) seeds.
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In Vitro and In Vivo Imaging-Based Evaluation of Doxorubicin Anticancer Treatment in Combination with the Herbal Medicine Black Cohosh
PublicationAs a substitution for hormone replacement therapy, many breast cancer patients use black cohosh (BC) extracts in combination with doxorubicin (DOX)-based chemotherapy. In this study, we evaluated the viability and survival of BC- and DOX-treated MCF-7 cells. A preclinical model of MCF-7 xenografts was used to determine the influence of BC and DOX administration on tumor growth and metabolism. The number of apoptotic cells after...
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Pretreatment of Lignocellulosic Materials as Substrates for Fermentation Processes
PublicationLignocellulosic biomass is an abundant and renewable resource that potentially contains large amounts of energy. It is an interesting alternative for fossil fuels, allowing the production of biofuels and other organic compounds. In this paper, a review devoted to the processing of lignocellulosic materials as substrates for fermentation processes is presented. The review focuses on physical, chemical, physicochemical, enzymatic,...
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X-ray Photoelectron Spectroscopy studies of various carboxylic acids adsorption on aluminium alloys in alkaline media
Open Research DataThis dataset contains the results of high-resolution XPS studies obtained during evaluation of high corrosion inhibition efficiency of various carboxylic acids towards aluminium alloy 5754 in bicarbonate buffer pH=11.