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Wyniki wyszukiwania dla: mechanism-based inhibition
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublikacjaWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
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Study of anticorrosion and microwave absprption properties of NiZn ferrite pigments
PublikacjaPurpose - The purpose of this paper is to report the electrochemical verification of anticorrosive properties of NiZn ferrites as pigments in protective coatings and evaluation of their microwave absorbing properties. Design/methodology/approach - Ferrites, represented by formula NixZn(1-x)Fe2O4, where x=0, 0.2, 0.4, 0.6, 0.8, 1.0, were synthesized using a ceramic method. The samples of ferrites were examined by X-ray diffraction...
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Valorization of paper-mill sludge laden with 2-chlorotoluene using hydroxyapatite@biochar nanocomposite to enrich methanogenic community: A techno-economic approach
PublikacjaWhile several studies have investigated the anaerobic digestion of paper-mill sludge (PMS), this technology suffers from nutrient insufficiency, inhibition by aromatic compounds, and low bio-CH4 yield. Hence, PMS was anaerobically co-digested with chicken manure (CM) and supplemented by hydroxyapatite@biochar (HAP@BC) nanocomposite for enhancing 2-chlorotoluene degradation and enriching the methanogenic archaea. Multiple continuous...
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Corrosion mechanisms in columns for atmospheric distillation of crude oil
PublikacjaThe paper presents the most common corrosion processes occurring in the columns for atmospheric distillation of crude oil. It describes the mechanisms leading to formation of the chemical compounds, which contribute to corrosion phenomena. The main technological factors influencing corrosion processes have been indicated. The paper also presents the interactions between particular corrosion mechanisms resulting in acceleration...
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Krótko- i długookresowe skorygowane krańcowe skłonności do konsumpcji. Gospodarka Polski w latach 1995-2018
PublikacjaWe wstępnej części artykułu - odwołując się do teorii Keynesa - omówiono i zdefiniowano podstawowe relacje makroekonomiczne pomiędzy konsumpcją globalną a produktem krajowym brutto. W następnej kolejności przeprowadzono analizę informacji statystycznych dotyczących prywatnych wydatków konsumpcyjnych gospodarstw domowych (C) oraz globalnych wydatków konsumpcyjnych społeczeństwa (CO) na tle produktu krajowego brutto (PKB) w Polsce...
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Polyurethane based hybrid ciprofloxacin-releasing wound dressings designed for skin engineering purpose
PublikacjaPurpose Even in the 21st century, chronic wounds still pose a major challenge due to potentially inappropriate treatment options, so the latest wound dressings are hybrid systems that enable clinical management, such as a hybrid of hydrogels, antibiotics and polymers. These wound dressings are mainly used for chronic and complex wounds, which can easily be infected by bacteria. Materials and methods Six Composite Porous Matrices...
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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Combination of air-dispersion cathode with sacrificial iron anode generating Fe2+Fe3+2O4 nanostructures to degrade paracetamol under ultrasonic irradiation
PublikacjaIn the present study, ultrasound (US) was coupled with an electrochemical process (ECP) consisting of a novel cathode of carbon cloth (CC)-carbon black (CB) as the nano-composite air-dispersion cathode (NADC) for the degradation of paracetamol (APAP) in an aquatic medium. The NADC favored in situ production of H2O2 by the cathodic reduction. The implementation of iron sacrificial anode instead of dimensionally stable anodes resulted...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublikacjaA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Wykorzystanie klasyfikacji funkcjonalnej usług do efektywnego zarządzania zasobami chmurowymi
PublikacjaWykazano jak istotnym problemem jest zarzadzanie chmurą obliczeniową, w tym alokacja zasobów do wykonania usług (workloadów) zgłoszonych przez użytkownika. Przeanalizowano problem podziału usług wdrażanych w środowiskach chmurowych na klasy określające ich funkcjonalność. Zaproponowano oryginalną metodę alokacji workloadów wykorzystującą wprowadzoną klasyfikację funkcjonalną oraz identyfikację tych klas na podstawie wielkości generowanego...
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Mechatronics and mechanism theory
Kursy Online -
A comprehensive evaluation of mimosa extract as a corrosion inhibitor on AA6060 alloy in acid rain solution: part I. Electrochemical AC methods
PublikacjaThe 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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Optimized 5-hour multiplex PCR test for the detection of tinea unguium: performance in a routine PCR laboratory
PublikacjaWe recently reported the development of a 5-hour multiplex PCR test for the detection of tinea unguium and the optimization of this test by the inclusion of an inhibition control. Here we report the performance of this procedure as used in a routine clinical laboratory as compared to conventional microscopy and culture-based techniques performed in a mycology reference laboratory. We found in processing 109 samples that 22 (20.2%)...
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New 2-[(4-Amino-6-N-substituted-1,3,5-triazin-2-yl)methylthio]-N-(imidazolidin-2-ylidene)-4-chloro-5-methylbenzenesulfonamide Derivatives, Design, Synthesis and Anticancer Evaluation
PublikacjaIn the search for new compounds with antitumor activity, new potential anticancer agents were designed as molecular hybrids containing the structures of a triazine ring and a sulfonamide fragment. Applying the synthesis in solution, a base of new sulfonamide derivatives 20–162 was obtained by the reaction of the corresponding esters 11–19 with appropriate biguanide hydrochlorides. The structures of the compounds were confirmed...
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Coffee silverskin as a potential bio-based antioxidant for polymer materials: Brief review
PublikacjaCoffee silverskin is one of the by-products generated by the coffee industry. Although it is not the most burdensome one, because it stands only for ~4.2 wt % of coffee, it seems like an auspicious raw material for industrial processes. Coffee silverskin is characterized by a relatively low moisture content of ~5–7%, so it often does not require quite energy-consuming drying processes. The chemical composition of coffee silverskin,...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublikacjaDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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Sonocatalytic degradation of tetracycline antibiotic using zinc oxide nanostructures loaded on nano-cellulose from waste straw as nanosonocatalyst
PublikacjaThe aim of the present investigation was the combination of ZnO nanostructures with nano-cellulose (NC) for the efficient degradation of tetracycline (TC) antibiotic under ultrasonic irradiation. The removal efficiency of 12.8% was obtained by the sole use of ultrasound (US), while the removal efficiency increased up to 70% by the US/ZnO treatment process. Due to the integration of ZnO nanostructures with NC, the removal efficiency...
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Bacterial consortium an axenic cultures isolated from activated sewage sludge for biodegradation of imidazolium-based ionic liquid
PublikacjaExtensive research and increasing number of potential industrial applications made ionic liquids (ILs) important materials in design of new, cleaner technologies. Together with the technological applicability, the environmental fate of these chemicals is considered and significant efforts are being made in designing strategies to mitigate their potential negative impacts. Many ILs are proven to be poorly biodegradable and relatively...
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Bioactive and biodegradable cotton fabrics produced via synergic effect of plant extracts and essential oils in chitosan coating system
PublikacjaFunctional antibacterial textile materials are in great demand in the medical sector. In this paper, we propose a facile, eco-friendly approach to the design of antibacterial biodegradable cotton fabrics. Cotton fiber fabrics were enhanced with a chitosan coating loaded with plant extracts and essential oils. We employed Fourier-transform infrared (FTIR) and X-ray photoelectron spectroscopy (XPS), UV–Vis spectrophotometry, optical...
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c-Myc Protein Level Affected by Unsymmetrical Bisacridines Influences Apoptosis and Senescence Induced in HCT116 Colorectal and H460 Lung Cancer Cells
PublikacjaUnsymmetrical bisacridines (UAs) are highly active antitumor compounds. They contain in their structure the drugs previously synthesized in our Department: C-1311 and C-1748. UAs exhibit different properties than their monomer components. They do not intercalate to dsDNA but stabilize the G-quadruplex structures, particularly those of the MYC and KRAS genes. Since MYC and KRAS are often mutated and constitutively expressed in cancer...
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KNOWLEDGE-BASED SYSTEMS
Czasopisma -
Comparative Analysis of Phytochemical Profiles and Selected Biological Activities of Various Morphological Parts of Ligustrum vulgare
PublikacjaLigustrum vulgare (LV), widely cultivated in Europe and often used in hedges, has been histori-cally recognized in folk medicine for its potential health benefits. This study focused on exploring the untargeted identification of secondary metabolites in ethanol extracts (70% v/v) from differ-ent morphological parts (young shoots, leaves, flowers and fruits) of LV at various stages of plant development, using ultra-high-performance...
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Evaluation of the yield, chemical composition and biological properties of essential oil from bioreactor-grown cultures of Salvia apiana microshoots
PublikacjaMicroshoot cultures of the North American endemic Salvia apiana were established for the first time and evaluated for essential oil production. Stationary cultures, grown on Schenk-Hildebrandt (SH) medium, supplemented with 0.22 mg/L thidiazuron (TDZ), 2.0 mg/L 6-benzylaminopurine and 3.0% (w/v) sucrose, accumulated 1.27% (v/m dry weight) essential oil, consisting mostly of 1,8-cineole, β-pinene, α-pinene, β-myrcene and camphor....
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Modulation of CYP19 expression by cabbage juices and their active components: indole-3-carbinol and 3,30-diindolylmethene in human breast epithelial cell lines
PublikacjaThe aim of this study was to evaluate the effect of white cabbage and sauerkraut juices of different origin and indole-3-carbinol (I3C) and diindolylmethane (DIM) on expression of CYP19 gene encoding aromatase, the key enzyme of estrogen synthesis.Remarkable differences in the effect on CYP19 transcript and protein level were found between the cab- bage juices (in 2.5-25 mL/L concentrations) and indoles (in 2.5-50 lM doses) in...
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Effect of aeration of antibiotic-loaded bone cement on its properties and bactericidal effectiveness
PublikacjaBACKGROUND: Antibiotic-loaded bone cements are now widely used in medicine. They are able to locally deliver antibiotic particles and they allow treat or protect against infection. It is assumed that the bactericidal effectiveness of bioactive bone cements depend on the parameters of its production. Hence, the aim of this study was to check the effect of aeration of bone cement before mixing the components on its properties as...
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Antibacterial Activity and Cytocompatibility of Bone Cement Enriched with Antibiotic, Nanosilver, and Nanocopper for Bone Regeneration
PublikacjaBacterial infections due to bone replacement surgeries require modifications of bone cement with antibacterial components. This study aimed to investigate whether the incorporation of gentamicin or nanometals into bone cement may reduce and to what extent bacterial growth without the loss of overall cytocompatibility and adverse effects in vitro. The bone cement Cemex was used as the base material, modified either with gentamicin...
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Model zaangażowania w relacji usługodawca-klient
PublikacjaW niniejszej monografii przedstawiono rozwiązania pozwalające lepiej zrozumieć złożoność relacji występujących pomiędzy usługodawcami a klientami oraz metody, które pozwalają tę wiedzę wykorzystać w doskonaleniu procesów organizacji usługowych. Monografia podejmuje problem kształtowania zaangażowania na styku usługodawca–klient jako wstępnego i koniecznego warunku rozwijania relacji w usługach. Opierając się na klasycznej drabinie...
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Sugar matters: sugar moieties as reactivity-tuning factors in quercetin O-glycosides
PublikacjaQuercetin, one of the most abundant flavonoids in plant-based foods, commonly occurs in nature in various glycosylated forms. There is still a less explored aspect regarding the cause of its glycosides diversity, depending on the sugars moiety attached. This work focuses on four widespread quercetin glycosides—hyperoside, isoquercitrin, quercitrin and rutin—by testing property-tuning capacity of different sugar moieties and thus...
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The Effect of Marginal Zn2+ Excess Released from Titanium Coating on Differentiation of Human Osteoblastic Cells
PublikacjaComposite coatings based on chitosan and zinc nanoparticles (ZnNPs) were successfully produced on Ti13Zr13Nb substrates by cathodic electrophoretic deposition (EPD). The unfavorable phenomenon of water electrolysis-induced nonuniformity was reduced by applying a low voltage (20 V) and a short deposition time (1 min). Surface analysis (roughness and hydrophilicity) reveals the potential of these coatings for enhancing cell attachment...
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Nitric Oxide-Dependent Pathways as Critical Factors in the Consequences and Recovery after Brain Ischemic Hypoxia
PublikacjaBrain ischemia is one of the leading causes of disability and mortality worldwide. Nitric oxide (NO), a molecule that is involved in the regulation of proper blood flow, vasodilation, neuronal and glial activity constitutes the crucial factor that contributes to the development of pathological changes after stroke. One of the early consequences of a sudden interruption in the cerebral blood flow is the massive production of reactive...
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Synthesis of Cyano-Benzylidene Xanthene Synthons Using a Diprotic Brønsted Acid Catalyst, and Their Application as Efficient Inhibitors of Aluminum Corrosion in Alkaline Solutions
PublikacjaNovel cyano-benzylidene xanthene derivatives were synthesized using one-pot and condensation reactions. A diprotic Brønsted acid (i.e., oxalic acid) was used as an effective catalyst for the promotion of the synthesis process of the new starting xanthene–aldehyde compound. Different xanthene concentrations (ca. 0.1–2.0 mM) were applied as corrosion inhibitors to control the alkaline uniform corrosion of aluminum. Measurements were...
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ADAPTATION OF THE ACTIVATED SLUDGE TO THE DIGESTATE LIQUORS DURING THE NITRIFICATION AND DENITRIFICATION PROCESSES
PublikacjaThe activated sludge process of the digestate liquors after chemical separation was conducted using a 10 L lab-scale sequencing batch reactor (SBR) and a 0.50 m3 pilotscale SBR independently (with pH control). Due to the relatively high concentration of free ammonia (FA), clear inhibitory effects of the digestate liquors on the nitrifying bacteria were observed. The adaptation of the activated sludge to the toxicity was evaluated...
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The Efficacious Benefit of 25-Hydroxy Vitamin D to Prevent COVID-19: An In-Silico Study Targeting SARS-CoV-2 Spike Protein
PublikacjaThe environment has rapidly looked at proven specialist task forces in the aftermath of the COVID-19 pandemic to build public health policies and measures to mitigate the effects of emerging coronaviruses. According to the researchers, taking 10 μg of 25-hydroxy vitamin D daily is recommended to keep us safe. There have been several studies recently indicating that there is a reduced risk of contracting Coronavirus by 25-hydroxy...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublikacjaCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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Current Enzyme Inhibition
Czasopisma -
Molecular basis and potential activity of HIV-1 reverse transcriptase toward trimethylamine-based compounds
PublikacjaReverse transcriptase (RT) inhibitors are currently used to treat human immunodeficiency virus (HIV)-1 infections. In this work, novel triethylamine derivatives were designed and studied by rigid and flexible docking and molecular dynamics (MD) approaches. An apo form of HIV-1 RT was also studied by MD simulation to analyze comparative response of protein in ligand-bound and ligand-unbound forms. Among newly designed HIV-1 RT inhibitors,...
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Ochrona Przeciwkorozyjna Instalacji Przemysłowych i Risk Based Inspection (RBI)
Kursy OnlineRisk Based Inspection
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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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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublikacjaBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublikacjaIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
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Divulging the anti-acetylcholinesterase activity of Colletotrichum lentis strain KU1 extract as sustainable AChE active site inhibitors
PublikacjaAlzheimer’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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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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Synthesis of 3-(2-Alkylthio-4-chloro-5-methylbenzenesulfonyl)-2-(1-phenyl-3-arylprop-2-enylideneamino)guanidine Derivatives with Pro-Apoptotic Activity against Cancer Cells
PublikacjaThe untypical course of reaction between chalcones and benzenesulfonylaminoguanidines led to the new 3-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-2-(1-phenyl-3-arylprop-2- enylideneamino)guanidine derivatives 8–33. The new compounds were tested in vitro for their impact on the growth of breast cancer cells MCF-7, cervical cancer cells HeLa and colon cancer cells HCT-116 by MTT assay. The results revealed that the activity of...
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Hybrid metal and non-metal activation of Oxone by magnetite nanostructures co-immobilized with nano-carbon black to degrade tetracycline: Fenton and electrochemical enhancement with bio-assay
PublikacjaElectrochemically synthesized magnetite nanostructures (ESMNPs) as a metal activator and nano-carbon black (NCB) as a non-metal activator were co-immobilized by alginate natural polymer to activate Oxone for the degradation of tetracycline (TC) antibiotic. The formation of sulfate radical was indirectly confirmed during the Oxone/ESMNPs/NCB/alginate process via the addition of scavenging compounds. This study revealed the high...
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REVIEW ON COMPETITION АОB AND NОВ AS AN IMPORTANT ELEMENT FOR COST EFFECTIVE METHODS OF REMOVING NITROGEN FROM WASTEWATER
PublikacjaThe aim of this paper is analysis of process principles and possible factors used to induce inhibition of nitrite oxidation by NOB (Nitrite Oxidizing Bacteria) which could be obtained during not very well understood processes: so called “shortcut” or “partial” nitrification as well deammonification, by qualitative/quantitative studies of AOB (Ammonium Oxidizing Bacteria) and NOB populations in activated...
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Application of Extreme Doses of Aluminium for Growth Control of Filmentous Bacteria Microthrix Parvicella in an Activated Sludge System - Laboratory Investigations
PublikacjaLaboratory investigations of aluminium (PAX-16) application for control of population of filamentous bacteria Microthrix Parvicella in a three-phase bioreactor in lab-scale were performed. Dosing of small aluminium doses (approximately 0.5 mgAl/gMLSS·d) in the period preceding seasonal growth of M.Parvicella failed to prevent mass growth of this microorganism leading to activated sludge bulking phenomenon (SVI-250 ml/gMLSS)...
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublikacjaThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublikacjaThirteen 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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Drug-Eluting Biopsy Needle as a Novel Strategy for Antimicrobial Prophylaxis in Transrectal Prostate Biopsy
PublikacjaOBJECTIVES: To preclinically evaluate drug-eluting biopsy needles (patent pending WO2016118026) as a new potential way of antimicrobial prophylaxis for transrectal prostate biopsy. METHODS: Twenty steel biopsy needles have been coated with polyvinyl alcohol, ciprofloxacin, and amikacin. Modified biopsy needles have been randomly divided into 3 groups (1:2:1 ratio). Needles from group I were immersed for 30 minutes in dedicated...
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