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Wyniki wyszukiwania dla: ACHE AND BUCHE INHIBITION
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Evaluation of corrosion inhibition of brass -118 in artificial seawater by benzotriazole using dynamic EIS
PublikacjaPrzedstawiono wyniki korozji mosiądzu 118 w sztucznej wodzie morskiej oraz efekt inhibicyjny benzotriazolu (BTA) przy użyciu nowoczesnej dynamicznej elektrochemicznej spektroskopii impedancyjnej (DEIS). metoda ta pozwala śledzić dynamikę procesu korozyjnego i efektu inhibicyjnego poprzez ocenę parametrów elektrycznych obwodu zastępczego. Chwilowe widma impedancyjne rejestrowane przez 10h wykazują iż ekspozycja przez okres kilku...
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Inhibition Ability of Natural Compounds on Receptor-Binding Domain of SARS-CoV2: An In Silico Approach
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Antiplasmodial activity of quinones: Roles of aziridinyl substituents and the inhibition of Plasmodium falciparum glutathione reductase
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In vitro antioxidant, anti-inflammatory activities and acetylcholinesterase inhibition properties of selected plant extracts
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublikacjaThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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Selective inhibition of cancer cells' proliferation by compounds included in extracts from Baltic Sea cyanobacteria
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In vitro characteristics ofLactobacillusspp. strains isolated from the chicken digestive tract and their role in the inhibition ofCampylobactercolonization
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A role for accessory genes rI.-1 and rI.1 in the regulation of lysis inhibition by bacteriophage T4
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Phytocomponents and evaluation of acetylcholinesterase inhibition by Ginkgo biloba L. leaves extract depending on vegetation period
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Inhibition of HIV‐1 or bacterial activation of macrophages by products of HIV‐1‐resistant human cells
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Antiplasmodial Activity of Nitroaromatic and Quinoidal Compounds: Redox Potential vs Inhibition of Erythrocyte Glutathione Reductase
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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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Genetic inactivation and chemical inhibition of PARP-1 lead to increased cytotoxicity to antitumor triazoloacridone C-1305
PublikacjaOkreśliliśmy aktywność cytotoksyczną związku C-1305 wobec komórek z obniżoną aktywnością PARP-1 w wyniku działania inhibitora tego enzymu związku NU1025. Dane wskazują, że w zależności od rodzaju inhibitora topoizomerazy II obniżenie aktywności PARP-1 przez związek NU1025 prowadzi do zwiększenia bądź obniżenia cytotoksyczności tych leków. Działanie NU1025 prowadzi również do re-aktywacji szlaku p53 w komórkach HeLa, czego jak dotąd...
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Isoform-specific inhibition of DNA topoisomerase II as the mechanism of action of novel anticancer agent C-1305
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Inhibition of phthalocyanine-sensitized photohemolysis of human erythrocytes by polyphenolic antioxidants: description of quantitative structure–activity relationships
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The Potential Mechanism of Tiliroside-Dependent Inhibition of t-Butylhydroperoxide-Induced Oxidative Stress in Endometrial Carcinoma Cells
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Improvement of CO2 absorption and inhibition of NH3 escape during CaCO3 precipitation in the presence of selected alcohols and polyols
PublikacjaThis research aims to investigate the effect of selected organic substances containing hydroxyl groups on the reduction of NH3 escape and the improvement of CO2 capture during the precipitation of calcium carbonate by carbonation method using post-distillation liquid from the Solvay process and gas stream containing CO2 in the amount corresponding to the exhausted gases produced by the combustion of fossil fuels. Glycerol, ethylene...
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Extracting functional groups of ALLINI to design derivatives of FDA‐approved drugs: Inhibition of HIV‐1 integrase
PublikacjaHIV‐1 integrase (IN) is crucial for integration of viral DNA into the host genome and a promising target in development of antiretroviral inhibitors. In this work, six new compounds were designed by linking the structures of two different class of HIV‐1 IN inhibitors (active site binders and allosteric IN inhibitors (ALLINIs)). Among newly designed compounds, INRAT10b was found most potent HIV‐1 IN inhibitor considering different...
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Inhibition of impurities formation in the synthesis of N-alkyltheobromines stimulated by microwave irradiation. Cationic and anionic response of membrane electrodes
PublikacjaN-Alkyltheobromine (1-9) derivatives were obtained by reacting theobromine with appropriate alkyl halide under microwave irradiation at 100-150 W and by conventional synthesis. Formation of by-products of oxygen atom alkylation and 1-N-alkyltheobromine ring opening were considered. The presented compounds 1-5 have been studied as ion carriers in ion-selective membrane electrodes. Selectivity of these membranes was studied towards...
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Evaluation of inhibition of cancer cell proliferation in vitro with different berries and correlation with their antioxidant level by advanced analytical methods
PublikacjaW pracy opisano wyniki badań:- właściwości przeciwutleniających ekstraktów rozpuszczalnikowych (DMSO) uzyskanych z różnych gatunków owoców jagodowych- zdolność do infibizacji proliferacji komórek rakowych.W badaniach wykorzystano testy (DPPH) oraz zaawansowane techniki analityczne (spektroskopia FTIR oraz fluoroscencja 3D)Wyniki badań wskazują, że spożywanie owoców jagodowych może zredukować zagrożenie procesu proliferacji komórek...
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Inhibition of ALDH1A1 activity decreases expression of drug transporters and reduces chemotherapy resistance in ovarian cancer cell lines
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Comparison of antioxidant and enzyme inhibition activities as well chemical composition of different extracts and fractions of Rubus caesius leaves
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c-Myc inhibition and p21 modulation contribute to unsymmetrical bisacridines-induced apoptosis and senescence in pancreatic cancer cells
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Partial inhibition of borohydride hydrolysis using porous activated carbon as an effective method to improve the electrocatalytic activity of the DBFC anode
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Dimethyl fumarate and 4-octyl itaconate are anticoagulants that suppress Tissue Factor in macrophages via inhibition of Type I Interferon
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Partial inhibition of borohydride hydrolysis using porous activated carbon as an effective method to improve the electrocatalytic activity of the DBFC anode
PublikacjaCarbon materials are commonly used catalyst supports in various types of fuel cells. Due to the possibility of designing their properties, they seem to be attractive and functional additives. In Direct Borohydride Fuel Cells (DBFCs), the electrooxidation reaction of borohydride competes with the undesirable hydrolysis reaction, therefore our work aimed to modify anodes based on a multi-component hydrogen storage alloy with a small...
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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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Dynamic electrochemical impedance spectroscopy and polarization studies to evaluate the inhibition effect of benzotriazole on copper-manganese-aluminium alloy in artificial seawater
PublikacjaPrzeprowadzono badania wpływu benzotriazolu (BTA) na korozję nowego typ mosiądzu (CMA) w środowisku syntetycznej wody morskiej przy użyciu dynamicznej elektrochemicznej spektroskopii impedancyjnej (DEIS), techniki polaryzacji rezystancyjnej i ekstrapolacji krzywych Tafela. Wyniki pomiarowe otrzymane przy użyciu tych metod wskazują spadek szybkości korozji wraz ze wzrostem stężenia BTA. Wskazuje to na inhibicyjne własności BTA w...
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Triple Combination of Ascorbate, Menadione and the Inhibition of Peroxiredoxin-1 Produces Synergistic Cytotoxic Effects in Triple-Negative Breast Cancer Cells
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Enhancement of Inhibition of the Pseudomonas sp. Biofilm Formation on Bacterial Cellulose-Based Wound Dressing by the Combined Action of Alginate Lyase and Gentamicin
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Efficacious Alkaline Copper Corrosion Inhibition by a Mixed Ligand Copper(II) Complex of 2,2′-Bipyridine and Glycine: Electrochemical and Theoretical Studies
PublikacjaA mixed ligand copper(II) complex, namely, [Cu(BPy)(Gly)Cl]⋅2H2O (CuC) (BPy=2,2′-bipyridine and Gly=glycine), was synthesized and characterized. The synthesized CuC complex was tested as inhibitor to effectively mitigate the corrosion of copper in alkaline solutions using the linear sweep voltammetry (LSV) and linear polarization resistance (LPR) techniques. For the sake of comparison, such two D.C. electrochemical techniques were...
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Dual inhibition of PI3K/Akt signaling and the DNA damage checkpoint in p53-deficient cells with strong survival signaling: implications for cancer therapy
PublikacjaOporność komórek nowotworowych na leki uszkadzjące DNA związana jest ściśle ze zdolnością do utrzymywania blok z fazie G2 cyklu komórkowego. Blok ten regulowany jest przez mechanizmy punktu kontrolnego G2/M oraz szlaki przeżycia komórkowego. W pracy badaliśmy rolę szlaku kinazy PI3K/Akt w funkcjonowaniu punktu kontrolnego cyklu komórkowego i wpływ na przeżycie komórek traktowanych lekiem przeciwnowotworowym - cisplatyną. Nasze...
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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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Inhibition of inflammatory response in human keratinocytes by magnetic nanoparticles functionalized with PBP10 peptide derived from the PIP2-binding site of human plasma gelsolin
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Promising effects of xanthine oxidase inhibition by allopurinol on autonomic heart regulation estimated by heart rate variability (HRV) analysis in rats exposed to hypoxia and hyperoxia
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Structure-based design and evaluation of novel N-phenyl-1H-indol-2-amine derivatives for fat mass and obesity-associated (FTO) protein inhibition
PublikacjaFat mass and obesity-associated (FTO) protein contributes to non-syndromic human obesity which refers to excessive fat accumulation in human body and results in health risk. FTO protein has become a promising target for anti-obesity medicines as there is an immense need for the rational design of potent inhibitors to treat obesity. In our study, a new scaffold N-phenyl-1H-indol-2-amine was selected as a base for FTO protein inhibitors...
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Photoprotection and Antiaging Activity of Extracts from Honeybush (Cyclopia sp.)—In Vitro Wound Healing and Inhibition of the Skin Extracellular Matrix Enzymes: Tyrosinase, Collagenase, Elastase and Hyaluronidase
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Evaluation of the Role of the Pharmacological Inhibition of Staphylococcus aureus Multidrug Resistance Pumps and the Variable Levels of the Uptake of the Sensitizer in the Strain-Dependent Response of Staphylococcus aureus to PPArg2-Based Photodynamic Ina
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Differential Response of MDA-MB-231 and MCF-7 Breast Cancer Cells to In Vitro Inhibition with CTLA-4 and PD-1 through Cancer-Immune Cells Modified Interactions
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublikacjaIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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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
PublikacjaThe 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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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublikacjaA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublikacjaA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Inhibitive effect of sodium molybdate on corrosion of AZ31 magnesium alloy in chloride solutions
PublikacjaIn 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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Surface and Corrosion Properties of AA6063-T5 Aluminium Alloy in Molybdate-containing Sodium Chloride Solutions
PublikacjaCorrosion properties of aluminium alloy AA6063-T5 were investigated in molybdate-containing NaCl solutions. Electrochemical, microscopic, and spectroscopic experiments were utilized to examine the mechanism of corrosion inhibition by molybdates. SEM-EDX, magnetic force, and intermodulation electrostatic force microscopy data suggested that the inhibition initiation preferentially occurred over Fe-rich cathodic IMPs. Spectroscopic...
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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
PublikacjaThe 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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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
PublikacjaElegant 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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Sodium nitrite as a corrosion inhibitor of copper in simulated cooling water
PublikacjaThe corrosion inhibition behavior of sodium nitrite (NaNO2) towards pure copper (99.95%) in simulated cooling water (SCW) was investigated by means of electrochemical impedance spectroscopy (EIS) and dynamic electrochemical impedance spectroscopy (DEIS). NaNO2 interferes with metal dissolution and reduce the corrosion rate through the formation or maintenance of inhibitive film on the metal surface. Surface morphologies illustrated...
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Carboxylic acids as efficient corrosion inhibitors of aluminium alloys in alkaline media
PublikacjaThe efficiency of AA5754 aluminium alloy corrosion inhibition achieved with maleic, malic, succinic, tartaric, citric, tricarballylic acids and serine in alkaline environment (pH 11) was examined. Selected corrosion inhibitors are characterized by different numbers and distribution of carbonyl and hydroxyl groups within their molecules. We have proposed and verified a novel approach for determining the adsorption isotherms based...
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Experimental and Quantum Chemical Evaluation of 8-Hydroxyquinoline as a Corrosion Inhibitor for Copper in 0.1 M HCl
PublikacjaThe corrosion inhibition properties of 8-hydroxyquinoline (8-HQ) in 0.1 M HCl for copper have been investigated by using experimental (electrochemical impedance spectroscopy (EIS), dynamic electrochemical impedance spectroscopy (DEIS), and potentiodynamic polarization) and theoretical methods complemented by surface morphological examination with the aid of scanning electron microscopy (SEM) and electron dispersive X-ray spectroscopy...