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Wyniki wyszukiwania dla: tyrosinase inhibitors
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Solubilization of keratins and functional properties of their isolates and hydrolysates
PublikacjaThe 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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Roman Kotlowski dr hab. inż.
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Understanding the origin of high corrosion inhibition efficiency of bee products towards aluminium alloys in alkaline environments
PublikacjaVarious 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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Optimised five-hour multiplex PCR test for the detection of Tinea ungium: performance in a routine PCR laboratory
PublikacjaWe 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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Glucosamine-6-phosphate synthase,a novel target for antifungalagents.Molecular modelling studies in drug design
PublikacjaPraca 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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Maria Jolanta Milewska prof. dr hab. inż.
OsobyMaria 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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Dynamic impedance data for various carboxylic acids corrosion inhibition of aluminium in alkaline media (pH=11)
Dane BadawczeThis 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
PublikacjaIn 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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Influence of G2 arrest on the cytotoxicity of DNA topoisomerase inhibitorstoward human carcinoma cells with different p53 status
PublikacjaRola 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)
PublikacjaTransplantology 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
PublikacjaThe 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
Dane BadawczeResearch data includes an attempt to determine the effective concentration of ketoprofen that inhibits germination of Sorghum bicolor (sorghum) seeds.
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Pretreatment of Lignocellulosic Materials as Substrates for Fermentation Processes
PublikacjaLignocellulosic 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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Chemical and biological characterization of Ocimum basilicum L. phenolic extract and essential oil derived through ultrasound and microwave-assisted extraction techniques
PublikacjaPlant-derived bioactive molecules are increasingly utilized in food processing as natural additives, driven by a growing interest in healthier lifestyles. This trend has spurred industries to reformulate products to meet the demands of health-conscious consumers. This study investigates the phenolic extract and essential oil of O. basilicum L. obtained via ultrasound-assisted extraction and microwave-assisted extraction, respectively. Characterization...
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X-ray Photoelectron Spectroscopy studies of various carboxylic acids adsorption on aluminium alloys in alkaline media
Dane BadawczeThis 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.
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Chitosan and polyvinyl alcohol nanocomposites with cellulose nanofibers from ginger rhizomes and its antimicrobial activities
PublikacjaThe inhibitory effect of 5% GNF bionanocomposites against Bacillus cereus, Escherichia coli, Staphylococcus aureus and Salmonella typhimurium indicated good antibacterial activity of the nanocomposites due to the addition of GNF in the biopolymer matrices. The use of GNF will help to increase the economic values of agricultural waste and the characteristic properties of GNF derived bionanocomposites could be possibly used in medical...
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Structural motifs in the Cu(II), Mn(II) and Zn(II) complexes based on N,N,N-donor dipodal or N,N,N,N-donor tripodal ligands obtained in situ: Synthesis, crystal structures and xanthine oxidase inhibition properties
PublikacjaA series of four novel transition metal complexes, [Cu(NCS)2L1] (1), [Mn(NCS)2L1] (2) where L1 = bis(1-(3,5-dimethylpyrazolyl)methyl)amine, [Mn(NCS)2L2] (3) and [Zn(NCS)L2]2[Zn(NCS)4] (4) where L2 = tris(1-(3,5-dimethylpyrazolyl)methyl)amine, has been obtained in situ by a one-step, one-pot synthetic path starting from 1-hydroxymethyl-3,5-dimethylpyrazole (L). The isolated complexes were fully characterised by elemental analysis,...
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The influence of selenium addition during germination of Brassica seeds on health-promoting potential of sprouts
PublikacjaThe correlation among selenium uptake, the content of bioactive compounds in sprouts, and biological activities triggered in cultured human cells by sprout extracts was investigated. Seeds of Brassica crops and rye were treated with SeO2 water solution. The selenium levels in sprouts increased from 1.0-4.1 to 53.3-382 μg/g dw with no influence on plant physiology according to the indices used. Neither the composition of glucosinolates...
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Analiza weryfikująca poprawność istniejącego układu ochrony przed korozją i osadami instalacji DRW4 w kontekście obecnych warunków pracy instalacji
PublikacjaCelem pracy były pomiary korozyjności kondensatów pochodzących z kolumny destylacyjnej z dodatkiem neutralizatora oraz inhibitora korozji, ponadto przeprowadzono badania SEM i EDX produktów korozji pochodzących z rurek chłodnicy powietrznej. Wykazano, że znacznie większą agresywnością charakteryzują się kondensaty które pochodzą z przerobu ropy naftowej zawierającą slopy.
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Modified DNA polymerases for PCR troubleshooting
PublikacjaPCR has become an essential tool in biological science. However, researchers often encounter problems with difficult targets, inhibitors accompanying the samples, or PCR trouble related to DNA polymerase. Therefore, PCR optimization is necessary to obtain better results. One solution is using modified DNA polymerases with desirable properties for the experiments. In this article, PCR troubleshooting, depending on the DNA polymerase...
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
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Fuzyjne polimerazy DNA – otrzymywanie, charakterystyka i zastosowanie
PublikacjaObecnie reakcje PCR (ang. Polymerase Chain Reaction) wykazują bardzo szerokie zastosowanie w diagnostyce medycznej, biologii molekularnej czy inżynierii genetycznej. Efektywność tych reakcji rozumiana jako wydajność i wierność przeprowadzonej amplifikacji jest nieodłącznie związana ze stosowaną polimerazą DNA i warunkami prowadzenia reakcji PCR. Aby sprostać wymaganiom stawianym przez nowoczesne metody diagnostyczne oraz współczesną...
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The antitumor derivatives, C1305 and C1748, were different in effects on CYP3A4 expression and catalytic activity in HepG2 cells
PublikacjaCytochromy P450 (CYP) należą do grupy enzymów biorących udział w 70-80% metabolizmu fazy I większości stosowanych klinicznie leków. Z tego powodu oddziaływanie leków z enzymami cytochromu P450 stało się istotnym elementem w projektowaniu chemoterapeutyków, szczególnie tych, które są stosowane w terapii wielolekowej. Znajomość substratów, induktorów i inhibitorów poszczególnych izoenzymów P450, nie tylko może obniżać częstość występowania...
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Combretastatin A-4 and its analogues as antineoplastic agenst.
PublikacjaCombretastatyna A-4 jest naturalnym związkiem wyizolowanym z wierzby afrykańskiej Combretum caffrum. W pracy opisano syntezę i aktywność biologiczną combretastatyny A-4 i jej analogów jako potencjalnych inhibitorów angiogenezy.
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Bioavailability of Tannins and Other Oligomeric Polyphenols: a Still to Be Studied Phenomenon
PublikacjaPurpose 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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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublikacjaMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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Synergistic Effects of Propolis Combined with 2-Phenoxyethanol and Antipyretics on the Growth of Staphylococcus aureus
PublikacjaThe present investigation aimed to assess the combinational effect of commonly usedantipyretics and antiseptics with ethanolic extracts of propolis (EEPs) on the growth inhibition ofStaphylococcus aureus. The broth microdilution checkerboard assay revealed synergistic interactionsbetween all investigated antipyretics, namely acetylsalicylic acid, ibuprofen, and acetaminophen,with EEPs samples. The values of the fractional inhibitory...
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Correlation between partial inhibition of hydrogen evolution using thiourea and catalytic activity of AB5-type hydrogen storage alloy towards borohydride electrooxidation
PublikacjaDirect borohydride fuel cells (DBFCs) are devices which directly convert the chemical energy stored in the borohydride ion and oxidant into electrical energy as a result of redox reactions. Unfortunately, a significant amount of fuel is lost as a result of the undesirable hydrolysis reaction. The selection of an efficient borohydride hydrolysis inhibitor requires detailed knowledge regarding the interaction mechanism between the...
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Glucosinolates from lepidium peruvianum as potential antiamnestic drugs
PublikacjaLepidium peruvianum (maca) (Brassicaceae) is a naturally occurring plant mainly in the high Andes of Peru. In recent years, it has been intensively researched in terms of its influence on various diseases and towards health improvement. Alzheimer’s disease is an incurable disease that most often affects adults over the age of 60. As since 2003 the US Food and Drug Administration (FDA) did not approve any new drug for Alzheimer’s...
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Nowe inhibitory jednostki katalitycznej telomerazy.
ProjektyProjekt realizowany w Katedra Technologii Leków i Biochemii zgodnie z porozumieniem UMO-2014/13/B/NZ7/02207 z dnia 2015-01-28
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Young Shoots of White and Red Headed Cabbages Like Novel Sources of Glucosinolates as Well as Antioxidative Substances
PublikacjaMost literature data indicate that the diet rich in plant products reduces the risk of developing chronic non-communicable diseases and cancer. Brassica vegetables are almost exclusively synthesizing glucosinolates. Glucosinolates are higher in sprouts than in mature plants, being related to the activity of the specific myrosinase involved in the degradation of glucosinolates during developmental stages. This study compares the...
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Paweł Sachadyn prof. dr hab. inż.
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures 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...
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1,3,4-Thiadiazole-based diamides: Synthesis and complexation properties
PublikacjaAromatic diamides, derivative of 2,6-pyridinedicarboxylic acid and isophthalic acid, bearing 1,3,4-thiadiazole residue were prepared with satisfactory yields in conventional procedures and microwave stimulated reactions. X-ray structure of N,N-bis (1,3,4-thiadiazol-2-yl)-2,6-pyridinedicarboxamide (2) DMSO solvate (2DMSO) was described. Selective zinc(II), lanthanum(III), terbium(III) and L-tyrosine recognition was found for N,N-bis(1,3,4-thiadiazol-2-yl)-2,6-pyridinedicarboxamide...
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The impact of equity pledge on inefficient investment: a perspective from family entrepreneurship
PublikacjaAs an efficient and convenient financing method, equity pledges may have a heterogeneous impact on the inefficient investment of family firms. In order to verify this point, this paper takes A-share listed family enterprises from 2010 to 2021 as a research sample. It conducts an empirical test on the impact of equity pledges on inefficient investment in family firms by constructing a panel regression model. The results show...
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Kinetic characterization of hydrogen sulfide inhibition of suspended anammox biomass from a membrane bioreactor
PublikacjaThe inhibition effects of hydrogen sulfide (H2S) on anammox-enriched biomass from a laboratory membrane reactor were analyzed in a series of batch respirometric experiments. The determined half maximal inhibitory concentration (IC50) was 4.67 mg H2S-S L−1 at the constant pH = 7.0 and the total sulfide concentration varying between 1 and 15 mg TS-S L−1. In another test, the IC50 was found to be 4.25 mg H2S-S L−1 under a constant...
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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublikacjaAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
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Novel method of expression and purification of hirudin based on pBAD TOPO, pTYB12 vectors and gene synthesis
PublikacjaW pracy przedstawiono nową, szybką i tanią metodę otrzymywania, ekspresji i oczyszczania białka hirudyny naturalnie izolowanego z ślinianek pijawki lekarskiej. Hirudyna pełni funkcje bezpośredniego inhibitora trombiny, głównego białka biorącego udział w tworzeniu skrzepów krwi. Właściwości te wykorzystywane są od wielu lat w klinice. Opracowana metoda pozwoliła uzyskać 17 mg/l hodowli E. coli białka o wysokiej czystości i aktywności...
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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublikacjaConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublikacjaIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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Molecular docking studies towards development of novel Gly-Phe analogs for potential inhibition of Cathepsin C (dipeptidyl peptidase I).
PublikacjaCathepsin C is a cysteine protease required for activation of various pro-inflammatory serine proteases and, essentially, is of interest as a therapeutic target. Cathepsin C coordinate system was employed as a model to study the interaction of some already available inhibitors of Cathepsin C. Compounds containing Gly-Phe fragment with functional groups at its ends were designed by knowledge based approach. Using AutoDock and...
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RESIDUE ANALYSIS OF ETU AND PTU BY LC/MS
PublikacjaDithiocarbamates (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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Microstructure and corrosion behaviour of carbon steel and ferritic and austenitic stainless steels in NaCl solutions and the effect of p-nitrophenyl phosphate disodium salt
PublikacjaThe microstructure and corrosion behavior of carbon steel (CSA516) and ferritic (SS410) and austenitic (SS304L) stainless steels were studied and compared. Corrosion tests were carried out in 0.5 M NaCl solutions. Rates of corrosion were monitored based on weight loss, Tafel extrapolation and linear polarization resistance (LPR) methods. Rates of corrosion were ranked following the order: CSA516 >> SS410 > SS304L. The impact of...
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Long range molecular dynamics study of interactions of the eukaryotic glucosamine-6-phosphate synthase with fructose-6-phosphate and UDP-GlcNAc
PublikacjaGlucosamine-6-phosphate synthase (EC 2.6.1.16) is responsible for catalysis of the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5 diphospho Nacetyl- d-glucosamine (UDP-GlcNAc), is an essential substrate for assembly of bacterial and fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which...
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Regenerative Drug Discovery Using Ear Pinna Punch Wound Model in Mice
PublikacjaThe ear pinna is a complex tissue consisting of the dermis, cartilage, muscles, vessels, and nerves. Ear pinna healing is a model of regeneration in mammals. In some mammals, including rabbits, punch wounds in the ear pinna close spontaneously; in common-use laboratory mice, they remain for life. Agents inducing ear pinna healing are potential regenerative drugs. We tested the effects of selected bioactive agents on 2 mm ear pinna...
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Interaction of the conserved region 4.2 of sigma(E) with the RseA anti-sigma factor
PublikacjaEo-E RNA polymerase transcribes a regulon of folding factors for the bacterial envelope and is induced by physical and chemical stresses. The RseA anti-sigma factor inhibits the activity of Esigma(E) RNA, polymerase. It is shown here that the N-terminal portion of sigma(E), residues 1-153, binds core RNA polymerase. RseA interacts with residues 154-191 of sigma(E), a site that is homologous to region 4, the sigma factor binding...
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Oxygen sensitivity of hydrogenesis’ and methanogenesis’
PublikacjaIn the chapter, results of dark fermentation of sour cabbage in presence of oxygen with concentrations 2-9% are presented. The presence of oxygen in such concentration inhibits methanogesis (and methane production more than 2 times) and increases hydrogen production 6 times. It also shortens the fermentation process above 40%.
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Synthesis of 2-amino-2,6-dideoxy-D-glucitol-6-sulfonic acid as a potential antifungal agent.
PublikacjaGlucosamine-6P (GlcN-6P) synthase catalyzes the first committed step in the biosynthetic pathway leading to the formation of UDP-GlcNAc, a sugar nucleotide precursor providing D-glucosamine for the formation of chitin and manoproteins. 2-Amino-2,6-dideoxy-D-glucitol-6-sulfonic acid is an analog of 2-amino-2-deoxy-D-glucitol 6-phosphate (GlcN-ol-6-P), a known inhibitor of GlcN-6-P synthase, in which the phosphate group of the latter...
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The comparison of cytotoxic and genotoxic activities of glucosinolates, isothiocyanates, and indoles
PublikacjaChemopreventive properties of Brassica vegetables are attributed mainly to their characteristic compounds—glucosinolates (GLs) and their main hydrolysis products—isothiocyanates (ITCs) and indoles. In this study, we compared antiproliferative activity (MTT test in HT29 cells) and genotoxic effects (comet assay in HT29 cells and restriction analysis in a cell-free system) of three GLs (sinigrin (SIN), glucotropaeolin (GTL), and...
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Synthetic strategies in construction of organic low molecular-weight carrier-drug conjugates
PublikacjaInefficient transportation of polar metabolic inhibitors through cell membranes of eukaryotic and prokaryotic cells precludes their direct use as drug candidates in chemotherapy. One of the possible solutions to this problem is application of the ‘Trojan horse’ strategy, i.e. conjugation of an active substance with a molecular carrier of organic or inorganic nature, facilitating membrane penetration. In this work, the synthetic...