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Search results for: MODULACJA METABOLIZMU ENZYMÓW UGT
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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Flavonoids as inhibitors of human neutrophil elastase
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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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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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublicationIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublicationOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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Chemical reactivity and antimicrobial activity of N-substituted maleimides
PublicationZsyntezowano kilkanaście N-podstawionych maleimidów, zawierających w swojej strukturze podstawniki o różnej wielkości i polarności.Maleimidy o charakterze obojętnym wykazywały silny efekt przeciwgrzybowy; ich aktywność przeciwbakteryjna była zróżnicowana. Niską aktywność przeciwbakteryjną, ale wysoką aktywność cytostatyczną stwierdzono dla maleimidów o charakterze zasadowym. Reaktywność chemiczna i lipofilowość miały wpływ na aktywność...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublicationThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublicationIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Bioaccumulation of metals in tissues of marine animals, Part II - metal concentrations in animal tissues
PublicationThe bioaccumulation of metals in an animal depends on a multitude of factors: biotic ones, like its body dimensions and mass, age, sex, diet, metabolism and position in the trophic web, as well as abiotic ones such as the distribution of metals in its environment, the salinity, temperature and pH of the water, habitat type, interactions with other metals. But it is diet that has the greatest influence on the accumulation of metals...
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Hydraty metanu jako źródło energii
PublicationHydraty metanu są strukturami krystalicznymi, składającymi się z cząsteczki gazu otoczonej cząsteczkami wody. Koncentrują one ogromne ilości metanu - szacuje się, że ok. 10 tys. Gt węgla organicznego jest uwięzionych w złożach hydratów. Dwukrotnie przewyższa to ilość węgla organicznego dostępnego w postaci konwencjonalnych paliw kopalnych
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Niching mechanisms in evolutionary computations
PublicationDozorowanie nisz stanowi mechanizm, którego celem jest utrzymanie gorzej przystosowanych osobników tak, aby populacja była różnorodna, zawierała odpowiednią liczbę istniejących gatunków, zarówno tych bardziej licznych, jak i tych mniej licznych, a przez to nie powodowała przedwczesnej zbieżności algorytmów ewolucyjnych. Efekt taki uzyskuje się poprzez odpowiednią modyfikację stopnia przystosowania lub rang osobników (zwiększa się...
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The influence of different acids and pepsin on the extractability of collagen from the skin of Baltic cod (Gadus morhua)
PublicationZastosowano 5,0 M roztwory kwasu cytrynowego, mlekowego, octowego oraz 0,115 M roztwór kwasu solnego. Kolagen z całych skór ekstrahowano w 4 st.C odpowiednimi kwasami (1 : 6, w/v) w czasie 24, 48 i 72 h. Stwierdzono, że kwas solny jest najmniej efektywnym rozpuszczalnikiem kolagenu spośród użytych kwasów. W zastosowanych warunkach doświadczeń maksymalnie można wyekstrahować kwasem cytrynowym 60 % kolagenu, kwasem octowym i mlekowym...
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The New LM-PCR/Shifter Method for the Genotyping of Microorganism
PublicationTechniques relies on the ligation of appropriates adapters (LM-PCR) as AFLP, PCR MP and ADSRRS are successfully used for epidemiological studies for prokaryotic and eukaryotic microorganisms. In this study we propose a new method, called the LM-PCR/Shifter, based on the use of a Class IIS restriction enzyme giving restriction fragments with different 4 base 5' overhangs (Shifter) and the ligation of appropriate oligonucleotide...
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A Novel Cryptic Clostridial Peptide That Kills Bacteria by a Cell Membrane Permeabilization Mechanism
PublicationThis work reports detailed characteristics of the antimicrobial peptide Intestinalin (P30), which is derived from the LysC enzyme of Clostridium intestinale strain URNW. The peptide shows a broader antibacterial spectrum than the parental enzyme, showing potent antimicrobial activity against clinical strains of Gram-positive staphylococci and Gram-negative pathogens and causing between 3.04 ± 0.12 log kill for Pseudomonas aeruginosa...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublicationThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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Quantification of unconjugated and total ibuprofen and its metabolites in equine urine samples by gas chromatography–tandem mass spectrometry: Application to the excretion study
PublicationIbuprofen (IBU) is a widely used nonsteroidal anti-inflammatory drug (NSAID) in human and also veterinary medicine. NSAIDs are usually highly metabolized compounds in horses; they are often present in equine urine, mostly in their conjugated forms (glucuronides). Thus, hydrolysis to cleave the glucuronide linkage prior to anti-doping analysis is often necessary for improving detection. In this study, unconjugated and total IBU...
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Polychlorinated Biphenyls (PCBs) and Polycyclic Aromatic Hydrocarbons (PAHs): Sediments and Water Analysis
PublicationUnfavorable side effects of different forms of anthropogenic activities can be found anywhere in the world. One of the basic characteristics of pollutants entering marine and ocean waters is their spread and movement in the global ocean. A portion of the substances entering the marine environment is rapidly degraded by chemical processes occurring in the air, sediments, and water, thereby losing their toxic properties. The biggest...
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Biomarkers of alcohol consumption in body fluids - possibilities and limitations of application in toxicological analysis
PublicationEthyl alcohol is the most popular legal drug, but its excessive consumption causes social problems. Despite many public campaigns against alcohol use, car accidents, instances of aggressive behaviour, sexual assaults and deterioration in labor productivity caused by inebriated people is still commonplace. Fast and easy diagnosis of alcohol consumption is required in order to introduce proper and effective therapy, and is crucial...
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Ocena przydatności bakterii Thermus ruber jako źródła termostabilnej alfa-glukozydazy użytecznej do wytwarzania syropów glukozowych
PublicationThermus ruber wytwarza alfa-glukozydazę o maksymalnej aktywności w temperaturze 65 C i przy pH 6,0. Wymieniony enzym zachowuje aktywność w zakresie pH 5,5-8,0 i prawie nie zmniejsza aktywności po 60 min inkubacji w 65 C. Szybkość hydrolizy maltozy, maltotetraozy, maltopentaozy oraz maltoheksaozy maleje wraz ze wzrostem masy cząsteckowej substratu.
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Rtęć w organizmach żywych – źródła i formy występowania, bioakumulacja, metody oznaczania
PublicationRtęć (Hg) jest metalem ciężkim o znanej i szeroko badanej toksyczności. Toksyczność rtęci zależy od formy chemicznej tego pierwiastka. Metylortęć (MeHg) jest uważana za najbardziej toksyczną formę rtęci, która po spożyciu jest bioakumulowana i biomagnifikowana w organizmach znajdujących się na kolejnych, następujących po sobie, ogniwach łańcucha pokarmowego. W ekosystemach wodnych, mikroorganizmy przekształcają nieorganiczne formy...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publication6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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RESIDUE ANALYSIS OF ETU AND PTU BY LC/MS
PublicationDithiocarbamates (DTCs) are important organosulfur compounds, which act as inhibitors of metal dependant and sulphydryl enzymes and have a serious consequence on biological systems. They possess variety of applications in agriculture as fungicides, as well as, in the rubber industry as vulcanization accelerators and antioxidants. In this way, DTCs are the main group of fungicides used to control approximately 400 pathogens of more...
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Polish Academic Libraries in the Face of the Covid-19 Pandemic: Crisis Management and Communication within the Organisation
PublicationThe developing SARS-CoV-2 coronavirus pandemic, which was announced in March 2020, has had a significant impact on the activities of universities and their academic libraries. The article aims to present the activities of academic libraries at the time of introducing restrictions on their activities and closing for several months to users and reformulating the services they provide, on the example of the Library of the Gdańsk University...
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Ocena przydatności bakterii Thermus ruber jako źródła syntazy trehalozy
PublicationWykazano, że termofilna bakteria Thermus ruber jest źródłem syntazy trehalozy,katalizującej wewnątrzcząsteczkową transglikozylację maltozy. Wymieniony enzym przejawia największą aktywność w temp. 65 st. C przy pH 6,5. Najlepszą wydajność syntazy trehalozy uzyskiwano podczas hodowli bakterii w 55 st. C na podłożu zawierającym 0,5% peptonu 0,1% wyciągu drożdżowego i 0,5% maltozy lub skrobi.
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Thermostable Pyrococcus woesei beta-D-galactosidase - high level expression, purification and biochemical properties
PublicationGen kodujący termostabilną beta-D-galaktozydazę Pyrococcus woesei zamplifikowano z zastosowaniem techniki PCR i klonowano w komórkach Escherichia coli. Skonstruowany system ekspresji genu pozwolił na uzyskanie znacznej ilości termostabilnego białka w komórkach mezofilnego gospodarza. Enzym oczyszczono z zastosowaniem chromatografii powinowactwa po wcześniejszej denaturacji termicznej białek Escherichia coli i scharakteryzowano...
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DDLMS PCR double digestion Ligation Mediated Suppression PCR - a new technique for bacterial specific differentiation
PublicationA new diagnostic kit for K. oxytoca specific differentiation based on ddLMS PCR (ang. double digest ligation Mediated PCR) technique is shown. As a species-specific DNA fragment pehX gene, encoding the enzyme polygalactouronase, was chosen. The genome sequence of K. oxytoca is digested with two endonucleases: AclI and BclI which cut DNA before and after pehX gene. The polymorphic DNA fragments are ligated with AclI-end-specific...
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Integrated Application of GPR and Ultrasonic Testing in the Diagnostics of a Historical Floor
PublicationThe paper presents the results of integrated ground penetrating radar (GPR) and ultrasonic testing (UT) measurements conducted on a historical floor in St. Nicholas’ Church, Gdańsk, Poland. The described inspection was the first stage of the technical state assessment of the building. The aim of the study was the detection of underfloor air gaps, which were observed in a few trial pits. The condition of the ground under the floor...
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Freehand drawing versus digital design tools in architectural teaching
PublicationThe oldest drawings resembling modern architectural designs date from the 22nd Century BC. Throughout history, the first drawings have evolved into the basic tool of the architect’s work. The exchange of information between the architect and the contractor began to take place through a drawing system, allowing to describe three-dimensional space using flat representations. With time, architectural drawings also began to resemble...
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Mitochondrial DNA copy number and trimethylamine levels in the blood: New insights on cardiovascular disease biomarkers
PublicationAmong cardiovascular disease (CVD) biomarkers, the mitochondrial DNA copy number (mtDNAcn) is a promising candidate. A growing attention has been also dedicated to trimethylamine-N-oxide (TMAO), an oxidative derivative of the gut metabolite trimethylamine (TMA). With the aim to identify biomarkers predictive of CVD, we investigated TMA, TMAO, and mtDNAcn in a population of 389 coronary artery disease...
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Sound engineering as our commitment to its creators in Poland
PublicationSound engineering is an interdisciplinary and rapidly expanding domain. It covers many aspects, such as sound perception, studio and sound mastering technology, music information retrieval including content-based search systems and automatic music transcription frameworks, sound synthesis, sound restoration, electroacoustics, and other ones constituting multimedia technology. Moreover, machine learning methods applied to the topics...
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City walk: a didactic innovative experiment in architectural education
PublicationWalking is an activity that involves studying physical space and requires careful observation to be immersed in the surrounding reality. City walks are popular ways of encountering an urban space, spatial relation, its history, and recognising the problems and needs of space users, as well as future development of the city. City walks also may be educationally p owerful: the exploration of certain...
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Developing a methodology for model tests of floating platforms in a towing tank of low depth
PublicationThe paper presents two ways to mooring model of semi-submersible platform for research in the small depth towing pool. The tested model was made in the likeness of 1:100 Thunder Horse platform moored in the Gulf of Mexico at a depth of 1,920 m. Its mooring system consisted of 16 semi-taut mooring lines (chain-wire-chain) spaced Star-shape and attached at the bottom to the suction piles. The tests were performed in the towing pool...
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The best practices transfer part I
PublicationThis expertise describes the possibilities of best practices implementation. These examples of best practices concern to improve the women’ entrepreneurship and were identified at the earlier stage of the project. One of the areas of activity within the QUICK IGA project was the selection of best practices related to strengthening the economic activity of women in the context of developing the competitiveness and innovation of...
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Recurrent potential pulse technique for improvement of glucose sensing ability of 3D polypyrrole
PublicationIn this work, a new approach for using a 3D polypyrrole (PPy) conducting polymer as a sensing material for glucose detection is proposed. Polypyrrole is electrochemically polymerized on a platinum screen-printed electrode in an aqueous solution of lithium perchlorate and pyrrole. PPy exhibits a high electroactive surface area and high electrochemical stability, which results in it having excellent electrocatalytic properties. The...
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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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Bioactivities of Phenolic Compounds from Kiwifruit and Persimmon
PublicationFruit used in the common human diet in general, and kiwifruit and persimmon particularly, displays health properties in the prevention of heart disease. This study describes a combination of bioactivity, multivariate data analyses and fluorescence measurements for the differentiating of kiwifruit and persimmon, their quenching and antioxidant properties. The metabolic differences are shown, as well in the results of bioactivities...
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Evaluation of Partial Nitritation/Anammox (PN/A) Process Performance and Microorganisms Community Composition under Different C/N Ratio
PublicationA one-stage partial nitritation/anammox (PN/A) process with intermittent aeration is possible under sidestream conditions, but implementation in a mainstream is a challenge due to increased Carbon/Nitrogen (C/N) ratios in domestic wastewater. This study investigated the effect of C/N ratios on process efficiency and the effect of narrowing non-aeration time on process improvement at high chemical oxygen demand (COD) load. An increase...
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Clinical studies of detecting COVID-19 from exhaled breath with electronic nose
PublicationThe COVID‑19 pandemic has attracted numerous research studies because of its impact on society and the economy. The pandemic has led to progress in the development of diagnostic methods, utilizing the polymerase chain reaction (PCR) as the gold standard for coronavirus SARS‑CoV‑2 detection. Numerous tests can be used at home within 15 min or so but of with lower accuracy than PCR. There is still a need for point‑of‑care tests available...
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Periodic and continuous niching in genetic optimization of detection observers.
PublicationNiszowanie stanowi mechanizm, którego celem jest utrzymanie gorzej przystosowanych osobników tak, aby populacja była różnorodna (zawierała także osobniki przeciętne i słabiej przystosowane). Niszowanie prowadzi do utrzymania odpowiedniej liczby istniejących gatunków, zarówno tych bardziej licznych (lepiej przystosowanych), jak i tych mniej licznych (słabiej przystosowanych), a przez to zapobiega przedwczesnej zbieżności algorytmów....
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Characteristics of hydration water around hen egg lysozyme as the protein model in aqueous solution. FTIR spectroscopy and molecular dynamics simulation
PublicationW niniejszej pracy przedstawiono wyniki badań dotyczące hydratacji białka modelowego - lizozymu z jaja kurzego w roztworze wodnym. Wiodącą techniką stosowaną w badaniach była spektroskopia oscylacyjna FTIR z zastosowaniem techniki rozcieńczenia izotopowego wody półciężkiej HDO w roztworze wody zwykłej. Analiza widma HDO przy pomocy "metody widm zaburzonych" pozwoliła na wyizolowanie widma wody zaburzonej przez lizozym, a tym samym...
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Feasibility Study of Biohydrogen Production from Acid Cheese Whey via Lactate-Driven Dark Fermentation
PublicationThe high loading of lactic acid bacteria (LAB) present in cheese whey still limits its use as hydrogen feedstock. This study aims to investigate the feasibility of producing hydrogen from acid cheese whey via lactate-driven dark fermentation (LD-DF). Mesophilic batch fermentations were performed with delipidated acid cheese whey at a fixed pH of 5.8 and driven by an acidogenic bacterial culture containing LAB and lactate-oxidizing...
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublicationStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...