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Search results for: ACHE AND BUCHE INHIBITION
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Divulging the anti-acetylcholinesterase activity of Colletotrichum lentis strain KU1 extract as sustainable AChE active site inhibitors
PublicationAlzheimer’s disease (AD), also called senile dementia is a neurodegenerative disease seen commonly in the elderly and is characterised by the formation of β-amyloid plaques and neurofbrillary tangles (NFT). Though a complete understanding of the disease is lacking, recent studies showed the role of the enzyme acetylcholinesterase (AChE) in pathogenesis. Finding new lead compounds from natural sources has always been a quest for...
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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer'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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Glucosinolates from lepidium peruvianum as potential antiamnestic drugs
PublicationLepidium 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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The Distribution of Glucosinolates in Different Phenotypes of Lepidium peruvianum and Their Role as Acetyl- and Butyrylcholinesterase Inhibitors—In Silico and In Vitro Studies
PublicationThe aim of the study was to present the fingerprint of different Lepidium peruvianum tu- ber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform)....
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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Current Enzyme Inhibition
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Aqueous Molybdate Provides Effective Corrosion Inhibition of WE43 Magnesium Alloy in Sodium Chloride Solutions
PublicationCorrosion and corrosion inhibition of WE43 magnesium alloy were investigated in NaCl solutions containing different amounts of sodium molybdate. Electrochemical, microscopic, and spectroscopic experiments were utilized to examine the mechanism of corrosion inhibition by molybdates. Electrochemical data showed that Na2MoO4 inhibitor provides reliable inhibition at concentrations at and above 100 mM. Raman and XPS spectroscopy demonstrated...
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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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Kinetic characterization of hydrogen sulfide inhibition of suspended anammox biomass from a membrane bioreactor
PublicationThe 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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Inhibition of the granular anammox process by the high concentration of free ammonia.
PublicationHigh concentrations of ammonia and nitrite, typical for reject water treatment in the anammox process with the use of high temperatures and pH, may cause free ammonia (FA) inhibition. In this study, the inhibitory effect of FA on anammox process rate was investigated in a bench-scale sequencing batch reactor (SBR) with granular anammox biomass. Results of the study present that the anammox process could be successfully operated...
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Desensitization of glucosamine-6-phosphate synthase to inhibition by UDP-GlcNAc
PublicationGlucosamine-6-phosphate (GlcN-6-P) synthase, known also as L-Glutamine: D-fructose-6-phosphate amidotransferase, catalyzes the first committed step in the pathway leading to the ultimate formation of UDP-GlcNAc. The final product of this pathway is an activated precursor of numerous macromolecules containing amino sugars, including chitin and mannproteins in fungi, peptidoglycan and lipopolysaccharides in bacteria, and glycoproteins...
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublicationTelomerase plays a pivotal role in cell proliferation, homeostasis, and neoplastic transformation, making it a promising molecular target for cancer chemotherapy. Of note, although hTERT has been explored thoroughly as a target, none of the promising molecules has been approved as a drug until now. The subject of research conducted as part of my doctoral dissertation is explaining the cellular and molecular mechanism of action...
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Educating planners in Europe: A review of 21st century study programmes
PublicationEducation for urban, regional and spatial planning has become a regular subject throughout most European nations; this can be attributed in part to European policies promoting planning and spatially balanced development, but also to the recognition that planning can support sustainability. Nevertheless, there is lingering and justifiable concern about the status, profile and recognition of planning as a profession in its own right...
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Exploring Mechanism of Corrosion Inhibition of WE43 and AZ31 Alloys by Aqueous Molybdate in Hank’s Solution by Multisine Impedimetric Monitoring
PublicationThe concept of utilizing multisine dynamic electrochemical impedance spectroscopy to monitor effectiveness of a model molybdate inhibitor for AZ31 and WE43 Mg alloys is proposed. The corrosion kinetics and instantaneous values of inhibition efficiency (IE) of molybdate at concentrations up to 150 mM were examined. The inhibitor provides inhibition in Hank’s solution at concentrations starting from ca. 25 mM, with the IE of about...
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Development of dynamic method for evaluation of inhibition efficiency on the example of 8-hydroxyquinolin
PublicationSelection of a proper inhibitor should be based on the evaluation of its mechanism and effective concentrations. Mechanism of inhibition usually has dynamic character due to changing physicochemical conditions of the environment and corroding metal surface. Most of actually used methods are stationary or contain assumptions which highly influences obtained values. Development of new dynamic method, based on modified EIS, allows...
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Inhibition of T-type calcium channel disrupts Akt signaling and promotes apoptosis in glioblastoma cells.
PublicationGlioblastoma multiforme (GBM) are brain tumors that are exceptionally resitant to both radio- and chemotherapy regimens and novel approaches to treatment are needed. T-type calcium channels are one type of low voltage-gated channel (LVCC) involved in embryonic cell proliferation and differentiation; however they are often over-expressed in tumors, including GBM. In this study, we found that inhibition of T-type Ca channels in GBM...
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The Application of Dynamic Electrochemical Impedance Spectroscopy (DEIS) Technique in Corrosion and Corrosion Inhibition Studies
Publicationorrosion studies have attracted considerable interest in the areas of materials chemistry and industrial chemistry, as it affects the direct and indirect costs of industry, leading to huge economic setbacks due to the need for repair, maintenance, and even shutdowns due corrosion damage. This new volume is a comprehensive resource that presents new and up-to-date, theoretical, and experimental corrosion inhibition studies.
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Growth inhibition of cultured cancer cells by Ribes nigrum leaf extract
PublicationThe present article includes data on the possible selective cytotoxic effect of extract of Ribes nigrum L. growing at high Armenian landscape. For this purpose, different non-cancer (microglial BV-2 wild type (Wt), acyl-CoA oxidase 1 (ACOX1) deficient (Acox1-/-) and cancer (human colon adenocarcinoma HT29 and human breast cancer MCF7) cell lines were applied. R. nigrum leaf ethanol extract showed a growth inhibition effect towards...
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Understanding the origin of high corrosion inhibition efficiency of bee products towards aluminium alloys in alkaline environments
PublicationVarious bee products were found to be efficient corrosion inhibitors of aluminium in different environments. In particular, bee pollen was found to be highly effective in alkaline electrolytes, yet its highly complex composition and possible synergistic interactions hinder determination of the compounds acting as active corrosion inhibitors. The main purpose of the following work is to investigate the effect of solvents used for...
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Mangiferin Affects Melanin Synthesis by an Influence on Tyrosinase: Inhibition, Mechanism of Action and Molecular Docking Studies
PublicationMangiferin is a strong antioxidant that presents a wide range of biological activities. The aim of this study was to evaluate, for the first time, the influence of mangiferin on tyrosinase, an enzyme responsible for melanin synthesis and the unwanted browning process of food. The research included both the kinetics and molecular interactions between tyrosinase and mangiferin. The research proved that mangiferin inhibits tyrosinase...
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RAAS inhibition – a practice of medical progress
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublicationHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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The inhibition effect of mad Honey on corrosion of 2007-type aluminium alloy in 3.5% NaCl solution
PublicationThe inhibition effect of mad honey on corrosion of 2007-type aluminium alloy in 3.5% NaCl solution was investigated by Tafel extrapolarisation (TP), electrochemical impedance spectroscopy (EIS) and dynamic electrochemical impedance spectroscopy (DEIS). All the studied parameters exhibited good anti-corrosive properties against corrosion of 2007-type aluminium alloy in the test solution; the corrosion rates decreased with the increase...
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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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Inhibition of cancer antioxidant defense by natural compounds
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Inhibition of Polymer Photodegradation by Incorporation of Coffee Silverskin
PublicationOver the last years, the trend associated with the incorporation of materials from renewable resources into polymer technology is getting significantly more vital. Researchers are trying to transfer the properties of natural raw materials into the polymer world. Therefore, different natural materials are more often investigated as potential additives for polymers. Such an effect is noted for the coffee industry by-products, such...
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Corrosion Inhibition of Aluminium Alloy AA6063-T5 by Vanadates: Local Surface Chemical Events Elucidated by Confocal Raman Micro-Spectroscopy
PublicationChemical interactions between aqueous vanadium species and aluminium alloy AA6063-T5 were investigated in vanadate-containing NaCl solutions. Confocal Raman and X-ray photoelectron spectroscopy experiments were utilised to gain insight into the mechanism of corrosion inhibition by vanadates. A greenish-grey coloured surface layer, consisting of V+4 and V+5 polymerized species, was seen to form on the alloy surface, especially on...
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Electrochemical, theoretical and surface physicochemical studies of the alkaline copper corrosion inhibition by newly synthesized molecular complexes of benzenediamine and tetraamine with π acceptor
PublicationTwo charge transfer complexes, namely [(BDAH)+(PA−)] CT1 [(BTAH)2+(PA−)2] and CT2 (BDAH = 1,2-benzenediamine, BTAH = 1,2,4,5-benzenetetramine, and PA− = 2,4,6-trinitrophenolate), were synthesized and fully characterized using various spectroscopic techniques. CT1 and CT2 were tested as inhibitors to effectively control the uniform and anodic corrosion processes of copper in an alkaline electrolyte (1.0 M KOH) using various electrochemical...
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Inhibition of amyloid fibril formation of hen egg white lysozyme by trimethylamine N-oxide at low pH
PublicationIn vitro inhibition of the formation of fibrous aggregates of proteins (amyloids) has gained increasing attention due to the number of diseases associated with protein misfolding and fibrillation. An interesting group of compounds for which pronounced activity against this phenomenon can be expected consists of low molecular weight substances (osmolytes) which have the ability to change protein stability. Here we investigate the...
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Dynamic impedance data for various carboxylic acids corrosion inhibition of aluminium in alkaline media (pH=11)
Open Research DataThis dataset contains the results of Dynamic Electrochemical Impedance Spectroscopy (DEIS) carried out in galvanostatic mode under iDC=0, carried out in order to define the corrosion inhibition effect of various studied carboxylic acids: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, carballylic acid, and serine. The experiment...
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PI3Kδ Inhibition by Idelalisib in Patients with Relapsed Indolent Lymphoma
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Overcoming carboxylic acid inhibition by granular consortia in high-load liquefied food waste fermentation for efficient lactate accumulation
PublicationGranular sludge, a self-aggregating spherical biofilm, possesses better stability compared to flocculent sludge under extreme conditions. This study compared the ability of anaerobic granular sludge (AnGS) and flocculent waste activated sludge (WAS) to convert food waste (FW) into highly-valuable optically active lactic acid (LA), a central and versatile intermediate platform molecule. Different loadings (30–60 g volatile suspended...
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Inhibition effect of free ammonia on deammonification process under different intermittent aeration strategies in sequencing batch reactor
PublicationThe deammonification process involves two steps. The first step is the partial nitrification of ammonia (NH4-N) by ammonia oxidizing bacteria (AOB) to produce nitrite (NO2-N) and the second step is the anammox process to “anaerobically” oxidize ammonia to nitrogen gas with nitrite as an electron acceptor (Lackner et al., 2014). Free ammonia (FA) plays a significant role in the stable, long-term deammonification system operation....
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The effect of mangiferin on skin: Penetration, permeation and inhibition of ECM enzymes
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C-1305 inactivation of recombinant human cytochrome P450, CYP1A2 and CYP3A4, is due to mechanism-based inhibition
PublicationPodjęto próbę określenia mechanizmu obserwowanej inhibicji izoenzymów CYP1A2 i CYP3A4 przez pochodną triazoloakrydonu C-1305.W pierwszym kroku stwierdzono, że hamowanie aktywnosci obu enzymów jest procesem nieodwracalnym. W kolejnych etapach badań wykazano między innymi, że obecność NADPH zwiększa istotnie stopień obserwowanej inhibicji, co wskazało, że mamy do czynienia z inhibicją samobójczą opartą na mechanizmie działania (ang....
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Corrosion Inhibition Mechanism and Efficiency Differentiation of Dihydroxybenzene Isomers Towards Aluminum Alloy 5754 in Alkaline Media
PublicationThe selection of efficient corrosion inhibitors requires detailed knowledge regarding the interaction mechanism, which depends on the type and amount of functional groups within the inhibitor molecule. The position of functional groups between different isomers is often overlooked, but is no less important, since factors like steric hinderance may significantly affect the adsorption mechanism. In this study, we have presented how...
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Modification of quaternary structure of Candida albicans GlcN-6-P synthase and its desensitization to inhibition by UDP-GlcNAc by site-directed mutagenesis
PublicationSite-directed mutagenesis of the CaGFA1 gene encoding glucosamine-6-phosphate synthase from Candida albicans was performed. Desensitization of the enzyme to inhibition by UDPGlcNAc was achieved upon T487I and H492F substitutions at the UDP-GlcNAc binding site, exchange of D524, S525 and S527 for Ala at the dimer:dimer interface and construction of the tail-lock array (L434R and L460A) at the C-tail region. The first two sets if...
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Therapeutic intervention by the simultaneous inhibition of DNA repair and type I or type II DNA topoisomerases: one strategy, many outcomes
PublicationMany anticancer drugs reduce the integrity of DNA, forming strand breaks. This can cause mutations and cancer or cell death if the lesions are not repaired. Interestingly, DNA repair-deficient cancer cells (e.g., those with BRCA1/2 mutations) have been shown to exhibit increased sensitivity to chemotherapy. Based on this observation, a new therapeutic approach termed 'synthetic lethality' has been developed, in which radiation...
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Human proteinase 3 resistance to inhibition extends to alpha‐2 macroglobulin
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Inhibition of protein glycosylation reverses the MDR phenotype of cancer cell lines
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Evaluation of citric acid corrosion inhibition efficiency and passivation kinetics for aluminium alloys in alkaline media by means of dynamic impedance monitoring
PublicationA novel approach is proposed for constructing the adsorption isotherm in corrosion studies, based on a well-known interaction between citric acid and aluminium in alkaline electrolytes. Our approach utilizes the instantaneous impedance measurements via Dynamic Electrochemical Impedance Spectroscopy in galvanostatic mode (g-DEIS). Unlike other common tools, g-DEIS delivers exact information about the concentration required for full...
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L-Homoserine O-acetyltransferase (CaMet2p) activity and inhibition
Open Research DataThe dataset contains the description of methodology and data files with the results obtained spectrophotometrically at 412 nm to determine the rate of fungal enzyme activity. The goal of the study was to obtain conditions optimal for L-homoserine O-acetyltransferase (Met2p) activity as well as evaluation of inhibitory potential of commercially available...
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Prolonged pharmacological inhibition of cathepsin C results in elimination of neutrophil serine proteases
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Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?
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Inhibition of Human and Yeast 20S Proteasome by Analogues of Trypsin Inhibitor SFTI-1
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Will we ever use angiotensin receptor neprilysin inhibition (ARNi) for the treatment of hypertension?
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Polyphosphates used for membrane scaling inhibition during water desalination by membrane distillation
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Cytotoxic effect on human melanoma cell lines and tyrosinase inhibition of Hottonia palustris
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Fatty acyl benzamido antibacterials based on inhibition of DnaK-catalyzed protein folding
PublicationWe have reported that the hsp70 chaperone DnaK from Escherichia coli might assist protein folding by catalyzing the cis/trans isomerization of secondary amide peptide bonds in unfolded or partially folded proteins. In this study a series of fatty acylated benzamido inhibitors of the cis/trans isomerase activity of DnaK was developed and tested for antibacterial effects in E. coli MC4100 cells. Nα-[Tetradecanoyl-(4-aminomethylbenzoyl)]-l-asparagine...