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Search results for: INHIBITORY KOROZJI
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New and potent production platform of the acetylcholinesterase inhibitor huperzine A by gamma-irradiated Alternaria brassicae under solid-state fermentation
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Removal of phenolic inhibitor compounds from hydrolysates and post-fermentation broths by using a Hydrophobic Magnetic Deep Eutectic Solvent
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Binding modes of a new epoxysuccinyl–peptide inhibitor of cysteine proteases. Where and how do cysteine proteases express their selectivity?
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Antitumor triazoloacridinone C-1305 as a potent FLT3 tyrosine kinase inhibitor in human acute myeloid leukemia (AML) cells.
PublicationJednym z defektów molekularnych u pacjentów z ostrą białaczką szpikową (AML) jest konstytutywna aktywacja receptoroweej kinazy tyrozynowj FLT3.Najczęstszą mutacją genu kodującego FLT3 jest wewnętrzna tandemowa duplikacja ITD we fragmencie okołobłonowym receptora. W pracy zbadano, czy przeciwnowotworowy triazoloakrydon C-1305 może być inhibitorem kinazy tyrozynowej FLT3. Badania przeprowadzono na dwóch liniach komórkowych białaczek...
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Antitumor DNA-Damaging C-1748 is a New Inhibitor of Autophagy that Triggers Apoptosis in Human Pancreatic Cancer Cell Lines
PublicationDespite the enormous progress that has been made over the past decades in diagnosis, treatment and prevention of many types of tumors, survival rates in pancreatic cancer still remain poor. Pancreatic cancer is one of the most malignant and chemoresistant tumors and the profound mechanism supporting these phenomena is the constitutively activated prosurvival autophagy. The antitumor 1-nitroacridine derivative C-1748 belongs to...
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Removal of phenolic inhibitor compounds from hydrolysates and post-fermentation broths by using a Hydrophobic Magnetic Deep Eutectic Solvent
PublicationHydroxymethylfurfural (HMF), furfural (FF), hydroquinone (HQ), and vanillin (VAN) are among the main inhibitors generated during most of biomass pre-treatments prior to fermentation processes. They are recognized as toxic to several fermentative microorganisms and therefore cause a decrease in biohydrogen or biofuel production (after hydrolysis). Moreover, if they are released into aqueous solutions (after fermentation), they can...
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Orzeczenie techniczne dotyczące stanu zachowania oraz możliwości dalszej eksploatacji uszkodzonych korozją słupów w przyziemiu budynku Akwarium Morskiego w Gdyni
PublicationOkreślenie możliwości nośnych oraz wskazanie sposobu naprawy uszkodzonych korozją słupów żelbetowych wykonanych w latach 30. ubigłego wieku.
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Determination of the minimum inhibitory concentration of C-1305 derivatives (IKE1-IKE8) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of acridone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 by the modified M27-A3 specified by the CLSI.
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Determination of the minimum inhibitory concentration of C-1330 derivatives (IKE9-IKE14) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of C-1330 derivatives (IKE9-IKE14) against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 by the modified M27-A3 specified by the CLSI.
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IKE1-IKE3 (C-1305 derivatives) inhibitory effect of the Yeast Topoisomerase II relaxation activity
Open Research DataInhibition of Yeast Topoisomerase II were analyzed according to relaxation assay kit from Inspiralis. Briefly, 250 ng of supercoiled pBR322 DNA, 1 mM ATP, 1-200 μM of analyzed compound were mixed with reaction buffer (1 mM Tris-HCl (pH 7.9), 10 mM KCl, 0.5 mM MgCl 2, 0.2 % (v/v) glycerol). The reaction was initiated by the addition of an enzyme, allowed...
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Determination of the minimum inhibitory concentration of new bisacridines IKE15-19 and IKE21, against yeast strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of new bisacridines against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019, S. cerevisiae ATCC 9763 and fluconazole resistant C. albicans strains by the modified M27-A3 specified by the CLSI.
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Influence of heat transformations on microstructure and properties of some wrought aluminium alloys.
PublicationOmówiono wpływ spawania na podatność do korozji naprężeniowej stopów Al-Mg i Al-Zn-Mg stwierdzając, że wzrost zawartości cynku wywołuje wzrost właściwości mechanicznych i spadek odporności na korozję naprężeniową. Wykazano, że obróbka cieplna złożona z retrogresji i powtórnego starzenia w przypadku stopów Al-Zn-Mg nie powoduje szczególnych zmian odporności na korozję naprężeniową, co pozostaje w związku z niewielką zmianą struktur...
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Glucosylceramide Mimics: Highly Potent GCase Inhibitors and Selective Pharmacological Chaperones for Mutations Associated with Types 1 and 2 Gaucher Disease
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Trypsin inhibitors from the garden four o’clock (Mirabilis jalapa) and spinach (Spinacia oleracea) seeds: Isolation, characterization and chemical synthesis
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Changes in Gene and Protein Expression of Metalloproteinase-2 and -9 and Their Inhibitors TIMP2 and TIMP3 in Different Parts of Fluoride-Exposed Rat Brain
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Screening of potential inhibitors for COVID-19 main protease from phytoconstituents of Tectona grandis Linn: application of molecular modeling studies
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Branched pentapeptides as potent inhibitors of the vascular endothelial growth factor 165 binding to Neuropilin-1: Design, synthesis and biological activity
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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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Manganese(III) Promoted Cyclization of N-alkenyl-N-(2-hydroxyethyl) amides to Iso-Oxacepham Potent β-Lactamase Inhibitors
PublicationBackground: β-Lactams are still a subject of interest of organic chemists. The main reason for this interest is due to their application as a chemotherapeutic. β-Lactam antibiotics are still the most commonly used drugs in bacterial infections. Method: Methods using 4-exo-trig radical cyclization leading to β-lactams are an alternative to classical Staudinger`s β-Lactams formation. We prepared N-alkenyl-N-(2-hydroxyethyl)amides...
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Alternative method for the synthesis of imidazo[5,1-f][1,2,4]triazin-4(3H)-one—a substrate for the preparation of phosphodiesterase (5) inhibitors
PublicationImidazo[5,1-f][1,2,4]triazin-4(3H)-ones, as isosteres of purine, are of interest for pharmaceutical research as potential substrates for the synthesis of cGMP-PDE5 inhibitors. We present a novel, alternative method for the synthesis of imidazotriazinones, that differs from the previously reported ones with respect to the method of construction of the triazinone ring in the molecule. The key step in our approach is condensation...
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Angiotensin receptor - neprilysin inhibiton (ARNI) – A novel therapeutic concept for management of hypertension and heart failure
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublicationThirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural...
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Mechanical properties and corrosion resistance of dissimilar stainless steel welds
PublicationW artykule przedstawiono właściwości mechaniczne oraz odporność korozyjną doczołowych złączy różnoimiennych stali odpornych na korozję, austenitycznej 316L oraz duplex 2205. Blachy o grubości 15 mm spawano automatycznie łukiem krytyn z różnymi energiami liniowymi. Wykazano, że właściwości mechaniczne złączy spełniają wymagania okrętowych towarzystw klasyfikacyjnych, natomiast najbardziej narażoną strefą złącza na działanie korozji...
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Substrate profiling of Finegoldia magna SufA protease, inhibitor screening and application to prevent human fibrinogen degradation and bacteria growth in vitro
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Trypsin inhibitor, antioxidant and antimicrobial activities as well as chemical composition of potato sprouts originating from yellow- and colored-fleshed varieties
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Design, synthesis and in vitro biological evaluation of a small cyclic peptide as inhibitor of vascular endothelial growth factor binding to neuropilin-1
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A comprehensive evaluation of mimosa extract as a corrosion inhibitor on AA6060 alloy in acid rain solution: part I. Electrochemical AC methods
PublicationThe inhibition effect of mimosa extract on the corrosion of AA6060 aluminum alloy in acid rain solution was investigated by electrochemical impedance spectroscopy and dynamic electrochemical impedance spectroscopy (DEIS). All the studied electrochemical parameters showed good corrosion inhibitive characteristics with respect to the aluminum alloy in the tested solution. Inhibitor efficiency increased with the concentration and...
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Induction of unique structural changes in guanine-rich DNA regions by the triazoloacridone C-1305, a topoisomerase II inhibitor with antitumor activities.
PublicationCelem pracy było scharakteryzowanie odziaływania związku C-1305 z DNA w porównaniu do innych inhibitorów topoizomerazy II. Badania pokazują, że C-1305 odziaływuje preferencyjnie z parami CG, interkaluje do DNA i zaburza sąsiednie otoczenie w bardzo charakterystyczny sposób, który nie został zaobserwowany u pozostałych 22 badanych związków.
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Ekspertyza numer 75/01/II/2016 - Określenie stanu powierzchni wewnętrznej, rury wykonanej ze stopu CuNi10Fe1,6Mn ze względu na możliwość wystąpienia produktów korozji. Określenie statusu warstwy pasywnej
PublicationElementy systemów rurociągów okrętowych mających kontakt z wodą zaburtową, takich jak np. instalacja chłodzenia silnika głównego, czy instalacja przeciw pożarowa, wykonywane są często ze stopów miedzi z nikem zwanych Cuniferami (Cu Ni Fe R-reszta pierwiastków stopowych). Cunifery charakteryzują się bardzo wysoką odpornością na korozję, pod warunkiem że procesy spawania i późniejszej pasywacji rurociągu przebiega zgodnie z właściwymi...
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DEIS evaluation of the relative effective surface area of AISI 304 stainless steel dissolution process in conditions of intergranulatar corrosion
PublicationWyniki przedstawione w tej pracy stanowią dalszą część badań dotyczących procesu roztwarzania wysokostopowej stali AISI 304 w warunkach zachodzenia korozji międzykrystalicznej z wykorzystaniem techniki dynamicznej elektrochemicznej spektroskopii impedancyjnej (DEIS). Po raz pierwszy zaprezentowano zmiany względnej powierzchni efektywnej procesu roztwarzania stali AISI 304 w warunkach zachodzenia korozji międzykrystalicznej w funkcji...
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Meat Proteins as Dipeptidyl Peptidase IV Inhibitors and Glucose Uptake Stimulating Peptides for the Management of a Type 2 Diabetes Mellitus In Silico Study
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Efficacy of high-dose corticosteroid-based treatment for chronic lymphocytic leukemia patients with p53 abnormalities in the era of B-cell receptor inhibitors
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Microbial acetylcholinesterase inhibitors for Alzheimer’s therapy: recent trends on extraction, detection, irradiation-assisted production improvement and nano-structured drug delivery
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Synthesis, anticandidal activity of N3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives – Novel inhibitors of glucosamine-6-phosphate synthase
PublicationNovel FMDP amiders 4-6 have been synthesized and tested against Candida strains. The anticandidal activity has been confined only to Candida albicans. Anticandidal activity of the tested amides has correlated with their inhibitory activity of glucosamine-6-phosphate synthase in cell free extract from Candida albicans.
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Development of biocompatible iron oxide-silicon oxide core-shell nanoparticles as subcellular delivery platform for glucosamine-6-phosphate synthase inhibitors
PublicationIn order to develop the preparation of iron oxide-silica coreshell nanoparticles (CSNPs), thesis deeply explores the cetyltrimethylammonium (CTA+) directed silica coating methods of the oleic-acid capped iron oxide nanoparticles (OA-IONPs) initialized under near-neutral pH conditions. It is demonstrated that the initial alkaline hydrolysis of ethyl acetate in the presence of CTA+ and OA-IONPs induces an unusual ligand exchange...
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Płyny do odladzania i zabezpieczania przed oblodzeniem samolotów, bazujące na trójskładnikowym ekologicznym układzie glikoli propylenowych i glicerolu.
PublicationPrzedstwiono wyniki badań korozji w zanurzeniu stopów metali i korozji9 powłoki kadmowej na stali w nowym płynie do odladzania samolotów (typI) i nowym płynie zapobiegającym ich ponownemu oblodzeniu (typII). Opracowane kompozycje oparto na ekologicznej, trójskładnikowej mieszaninie glikolu 1,2-propylenowego, 1,3-propylenowego oraz glicerolu.
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The mechanism of internalization study of QDgreen−CD−FA−C−2028 conjugate at IC80 value to cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells
Open Research DataThe influence of different endocytosis inhibitors on the internalization of QDgreen−CD−FA−C−2028 conjugate at IC80 value in cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells. First, the cells were preincubated with: drug-free medium (no inhibitor), at 4 °C, 5 µM Cytochalasin D, 30 µM Amiloride, 80 µM Dynasore, 25 µM Pitstop 2 and 1.5...
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Adsorption behavior and corrosion inhibitive characteristics of newly synthesized cyano-benzylidene xanthenes on copper/sodium hydroxide interface: Electrochemical, X-ray photoelectron spectroscopy and theoretical studies
PublicationElegant process for synthesis of 3-(7H-dibenzo[c,h]xanthen-7-yl)benzaldehyde (3), as new starting material to create a set of novel xanthene analogues, 2-(3-(7H-dibenzo[c,h]xanthen-7-yl)benzylidene)malononitrile (4), 3-(3-(7H-dibenzo[c,h]xanthen-7-yl)phenyl)-2-cyanoacrylic acid (5), and Ethyl-3-(3-(7H-dibenzo[c,h]xanthen-7-yl)phenyl)-2-cyanoacrylate (6), was achieved starting with available materials under mild conditions. Various...
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Susceptibility of Cr-Ni-Mn steel to the hydrogen degradation in boiler fuel = Podatnośc stali Cr-Mn-Ni na niszczenie wodorowe w paliwie kotłowym
PublicationStal 34HNM poddana różnym obróbkom cieplnym wykazała skłonność do korozji naprężeniowej w pomiarach ze stałą niską szybkością rozciągania i do zmęczenia korozyjnego niskocyklowego. Mechanizmem zniszczenia była degradacja wodorowa. Możliwe źródła pochłaniania wodoru to: korozja, degradacja węglowodorów z tworzeniem się kwasów organicznych i promotorów wnikania wodoru.
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The Effect of Long-Term Administration of Fatty Acid Amide Hydrolase Inhibitor URB597 on Oxidative Metabolism in the Heart of Rats with Primary and Secondary Hypertension
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PdCl2-catalyzed synthesis of a new class of isocoumarin derivatives containing aminosulfonyl / aminocarboxamide moiety: First identification of a isocoumarin based PDE4 inhibitor
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Simultaneous impedance and volumetric studies and additionally potentiodynamic polarization measurements of molasses as a carbon steel corrosion inhibitor in 1M hydrochloric acid solution
PublicationThe inhibition effect of molasses on the corrosion of low carbon steel in 1M hydrochloric acid solution was investigated by volumetric and electrochemical measurements. Potentiodynamic polarization and dynamic electrochemical impedance spectroscopy (DEIS) results were obtained and compared with to those, obtained with the hydrogen evolution technique. All results indicate that molasses functioned as a good inhibitor in 1M hydrochloric...
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PARP inhibition potentiates the cytotoxic activity of C-1305, a selective inhibitor of topoisomerase II, in human BRCA1-positive breast cancer cells
PublicationTwo cellular proteins encoded by the breast and ovarian cancer type 1 susceptibility (BRCA1 and BRCA2) tumor suppressor genes are essential for DNA integrity and the maintenance of genomic stability.Approximately 5-10% of breast and ovarian cancers result from inherited alterations or mutations in these genes.Remarkably, BRCA1/BRCA2-deficient cells are hypersensitive to selective inhibition of poly(ADPribose) polymerase 1 (PARP-1),...
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Different expression level of CYP3A4 isoenzyme modulate cellular response of CHO cells following treatment with the CYP3A4 inhibitor, C-1311 compound
PublicationEfektywność terapii przeciwnowotworowej może być zmieniana przez różne czynniki. Jednym z ograniczeń jest odmienny u każdego pacjenta poziom enzymów metabolizujących odpowiedzialnych za aktywację i detoksykację leków, co może zmieniać jego odpowiedź na zastosowaną terapię. Co więcej, enzymy metabolizujące często są celem molekularnym wielu ksenobiotyków, co dodatkowo może zmieniać skuteczność terapii. Zatem zrozumienie oddziaływań...
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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Phytochemical screening and biological evaluation of Greek sage (Salvia fruticosa Mill.) extracts
PublicationThis study explores the influence of extraction solvents on the composition and bioactivity of Salvia fruticosa extracts. Ultrasound-assisted extraction with water, ethanol and their mixtures in variable proportions was used to produce four different extracts. An untargeted UPLC/MS‑based metabolomics was performed to discover metabolites profile variation between the extracts. In the analyzed samples, 2704 features had been detected,...
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Nowe estrowe i amidowe pochodne inhibitorów syntazy glukozamino-6-fosforanu - synteza i aktywność biologiczna
PublicationPrzedmiotem rozprawy doktorskiej są modyfikacje chemiczne analogów glutaminy – kwasu N3-(4-metoksyfumaroilo)-S-2,3-diaminopropanowego (FMDP) oraz kwasu N3-[(E)-4-fenylo-4-okso-2-butenoilo]-S-2,3-diaminoaminopropanowego (BADP). Związki te są inhibitorami syntazy glukozamino-6-fosforanu i mimo ich silnych właściwości inhibicyjnych, nie wykazują zdolności do hamowania wzrostu drobnoustrojów. Brak aktywności przeciwdrobnoustrojowej...
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Pasywacja stali nierdzewnych
PublicationOdporność chemiczna stali odpornych na korozję oparta jest calkowicie na pasywnym charakterze warstw powierzchniowych istniejących na tych stalach. Pasywność to stan, w którym metal aktywny wykazuje podwyższoną odporność korozyjną dzięki tworzeniu na powierzchni warstewki, która jest stabilna w danym środowisku, pH i potencjale oraz stanowi produkt korozji.
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SEM micrographs of aluminium corrosion in alkaline media with various bee products as corrosion inhibitors
Open Research DataThis dataset contains various scanning electron microscopy (SEM) micrographs of AA5754 aluminum alloy samples exposed to the corrosive alkaline environment without and with the addition of various bee products to act as green corrosion inhibitors. The products are bee pollen, honey, and putty. They were investigated in bicarbonate buffer (pH =10 or...
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Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM)
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