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Wyniki wyszukiwania dla: ENDOGENOUS REDOX-ACTIVE COMPOUNDS
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Procognitive activity of nitric oxide inhibitors and donors in animal models
PublikacjaNitric oxide is a small gaseous molecule that plays important roles in the majority of biological functions. Impairments of NO-related pathways contribute to the majority of neurological disorders, such as Alzheimer’s disease (AD), and mental disorders, such as schizophrenia. Cognitive decline is one of the most serious impairments accompanying both AD and schizophrenia. In the present study, the activities of NO donors, slow (spermine...
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Selected anionic and cationic surface active agents determined in river sediments – the Klodnica catchment
PublikacjaSurface active agents (SAAs) are specific compounds that contain hydrophilic/ hydrophobic group in their molecules named as amphiphilic structures. According to charge on the hydrophilic part of surfactants they can be classified into three main groups: anionic, cationic and non-ionic compounds. Due to the amphiphilic structure of SAAs they have specific properties (e.g. ability to adsorption at different surfaces, reduction of...
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The impact of mGlu2 or mGlu5 receptor activators on the production of l-arginine derivatives and the expression of PRMT5 or DDAH1 enzymes in animal models of cognitive decline
PublikacjaL-arginine derivatives (ADMA, SDMA, NMMA) are endogenous inhibitors of nitric oxide (NO֗) production, which is essential in critical brain processes including blood-brain barrier (BBB) integrity and long-term potentiation (LTP). ADMA and NMMA are degraded by dimethylarginine dimethylaminohydrolase 1 (DDAH1) and protein arginine methyltransferase 5 (PRMT5) is an emerging epigenetic enzyme that mainly represses transcription of target...
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Cathodes for Sodium‑Ion Batteries
PublikacjaAdvances in lithium-ion battery (LIBs) technology have improved living conditions around the globe. However, there are increasing concerns regarding the sustainability and criticality of materials (lithium and cobalt) for LIBs. Considering sodium’s superiority in cost and abundance, the development of electrode materials for sodium-ion batteries (NIBs) has been intensively revisited. Limited types of structures are suitable for...
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Magnetically recyclable TiO2/MXene/MnFe2O4 photocatalyst for enhanced peroxymonosulphate-assisted photocatalytic degradation of carbamazepine and ibuprofen under simulated solar light
PublikacjaIn this study, a novel TiO2/Ti3C2/MnFe2O4 magnetic photocatalyst with dual properties, enabling (i) improved photocatalytic degradation with PMS activation under simulated solar light and (ii) magnetic separation after the degradation process in an external magnetic field was developed and applied for the efficient photodegradation pharmaceutically active compounds (PhACs) frequently present in wastewater and surface waters worldwide. MXene...
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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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Pathways of nitrogen compounds depletion in hybrid constructed wetlands
PublikacjaHybrid Constructed Wetlands are composed of two or more filters with mixed flow direction of sewage. Apparently in the HCWS the benefits of both types of bed are merged, resulting in better effluent quality (organic and nitrogen componds removal). Such heterogeneous environment creates possibilities for different ways of nitrogen "disappearing". The objective of the present study was to compare the removal of nitrogen with accompanying...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Analytics of Surfactants in the Environment: Problems and Challenges
PublikacjaSurfactants (surface active agents = SAAs) are a group of compoundswith specific physicochemical properties (amphiphilicity,solubility in polar and nonpolar liquids, ability to form micelles,adsorption at phase boundaries).1,2 Because of their properties,surface-active compounds are widely applied in industry and thehousehold (e.g., in detergents, personal-care products, paints,pesticides, petroleum products). As their applications...
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Technologie wytwarzania żywności funkcjonalnej. Metodyki badania jej składu. Kierunki rozwojowe- cz. I
PublikacjaObserwuje się rozwój technologii produkcji żywności w kierunku wzmocnienia funkcji jej składników, które wspomagają system odpornościowy, przyczyniają się do zapobiegania rozwoju chorób sercowo-naczyniowych czy dolegliwości żołądkowych. Można stwierdzić, że nastąpił coraz bardziej zauważalny postęp w dziedzinie nanotechnologii, której metody są przydatne w procesach produkcji żywności bezpiecznej, o dłuższym terminie przydatności...
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Effect of Agitation and Temporary Immersion on Growth and Synthesis of Antibacterial Phenolic Compounds in Genus Drosera
PublikacjaSundews (Drosera sp.) are the source of biologically active secondary metabolites: phenolic acids, flavonoids, and 1,4-naphtoquinones. Because obtaining them from the natural environment is impossible (rare and endangered species), in this study modifications of traditional tissue cultures grown in solid medium (SM), such as agitated cultures (ACs) (cultures in liquid medium with rotary shaking) and temporary immersion bioreactors...
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LC-MS and LC-NMR as Complementary Techniques for the Determination of Pharmaceuticals in Dosage Formulations
PublikacjaPharmaceuticals contain not only pharmacologically active compounds but also a range of excipients. The danger exists that impurities may also be present in such drugs, which may adversely affect their efficacy and even endanger patient health and life. Monitoring the composition of pharmaceutical products is therefore essential. The trace amounts of such impurities in pharmaceuticals are often identified and determined with liquid...
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Recent breakthroughs in the stability testing of pharmaceutical compounds
PublikacjaPharmaceutical development is mostly focused on the research leading to approval of a new and viable active substance. However, there is a number of old generation compounds that are still being used in contemporary medicinal practice. So that new analytical developments should cover not only the safety of newly developed drug substances, which is obvious, but should also be directed into the search of individual stability issues...
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublikacjaGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
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Approaches Towards Better Immunosuppressive Agents
PublikacjaSeveral classes of compounds are applied in clinics due to their immunosuppressive properties in transplantology and the treatment of autoimmune diseases. Derivatives of mycophe-nolic acid, corticosteroids and chemotherapeutics bearing heterocyclic moieties like methotrexate, azathioprine, mizoribine, and ruxolitinib are active substances with investigated mechanisms of action. However, improved synthetic approaches of known drugs...
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Non-Nutritive Bioactive Compounds in Food of Plant Origin
PublikacjaThe increasing knowledge on the health benefits of certain food ingredients, in particular, those of plant origin, opened the discussion of the possibility of using edible plants or their active components in the prevention of non-communicable diseases. The health-promoting properties of plant foods are related to the presence of non-nutritive compounds, mainly plant secondary metabolites, which can affect many biological mechanisms...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublikacjaHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublikacjaA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Pathways of Nitrogen Removal in Hybrid Treatment Wetlands
PublikacjaHybrid Treatment Wetlands (HTWs) are composed of two or more filters with different modes of flow, allowing the benefits of both types of bed to be combined, resulting in better effluent quality (nitrogen and organic compounds removal). Such a heterogeneous environment creates possibilities for different mechanisms of nitrogen removal. The objective of the present study was to investigate the removal of nitrogen versus a range...
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Nutritional and Pharmaceutical Properties of Bioactive Compounds in Organic and Conventional Growing Kiwifruit
PublikacjaThe bioactivity of two kiwifruit’s cultivars growing under organic and conventional conditions were studied and compared. The bioactive compounds were extracted with water and ethanol using similar conditions which are applied in pharmaceutical applications and for daily fruit consumption such as tea drink. Antioxidant radical scavenging assays [ferric-reducing/antioxidant power (FRAP); cupric reducing antioxidant capacity (CUPRAC);...
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Deciphering the Molecular Mechanism of Substrate-Induced Assembly of Gold Nanocube Arrays toward an Accelerated Electrocatalytic Effect Employing Heterogeneous Diffusion Field Confinement
PublikacjaThe complex electrocatalytic performance of gold nanocubes (AuNCs) is the focus of this work. The faceted shapes of AuNCs and the individual assembly processes at the electrode surfaces define the heterogeneous conditions for the purpose of electrocatalytic processes. Topographic and electron imaging demonstrated slightly rounded AuNC (average of 38 nm) assemblies with sizes of ≤1 μm, where the dominating patterns are (111) and...
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Treatment innovation using solar/UV In book: The Treatment of Pharmaceutical Wastewater: Innovative Technologies and the Adaptation of Treatment Systems
PublikacjaSince ancient times, sunlight irradiation has been widely used for water purification. Apart from solar water disinfection techniques, UV irradiation is of particular interest when considering the photodegradation of various classes of emerging pollutants. Pharmaceutically active compounds are one of the largest classes of micropollutants. The main sources of these contaminants in wastewater and aqueous environments are households,...
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Recent advances on magnetic carbon-related materials in advanced oxidation processes of emerging pollutants degradation
PublikacjaRecently, carbon-related materials have been proposed to improve the charge separation of the photogenerated carriers in the semiconductor matrices’ and surface properties. Carbon-related materials may act as co-catalysts, enhancing the pollutants adsorption on the surface, improving the charge carriers separation and photocatalyst stability and providing more active centres for photocatalytic reactions. This review summarizes...
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Importance of the combined effects of dissolved oxygen and pH on optimization of nitrogen removal in anammox-enriched granular sludge
PublikacjaThe combined effects of dissolved oxygen (DO) and pH on nitrogen removal were investigated in a laboratory-scale sequencing batch reactor (SBR) with anammox-enriched granular sludge obtained from a nitritation/anammox system. The highest specific nitrogen removal rate (SNRR) (1.1 gN gVSS−1 d−1) was observed under non-aerated conditions, resulting in the nitrogen removal efficiency of 81.6%. Although nitrogen removal was readily...
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Analityka surfaktantów w próbkach środowiskowych
PublikacjaSurfaktanty stanowią grupę związków charakteryzujących się specyficznymi właściwościami fizykochemicznymi (m.in. amfifilowa budowa, zdolność rozpuszczania się w cieczach o różnej polarności, zdolność do tworzenia micelli) i z tego względu są one wykorzystywane w wielu sferach działalności człowieka. Związki powierzchniowo-czynne ulegają różnorodnym przemianom fizykochemicznym, co umożliwia ich migrację między różnymi elementami...
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Analysis and bioanalysis: an effective tool for data collection of environmental conditions and processes
PublikacjaReliable information that allows us to estimate the state of the environment and to forecast changes in the ecosystem are constantly required. Increasing environmental consciousness and dynamic development of analytical techniques are the main reasons for determining the wide range of pollutants occurring at very low concentrations in complex matrix samples. The presence and concentration of many of those pollutants in the environment...
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Comparative Analysis of Metabolic Variations, Antioxidant Profiles and Antimicrobial Activity of Salvia hispanica (Chia) Seed, Sprout, Leaf, Flower, Root and Herb Extracts
PublikacjaThe purpose of this study was to evaluate the phytochemical profiles of the seeds, sprouts, leaves, flowers, roots and herb of Salvia hispanica and to demonstrate their significant contribution to antioxidant and antimicrobial activities. Applied methods were: HPLC-DAD coupled with post-column derivatization with ABTS reagent, untargeted metabolomics performed by LC-Q-Orbitrap HRMS, and two-fold micro-dilution broth method, which...
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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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Relationship between Chemical Structure and Biological Activity Evaluated In Vitro for Six Anthocyanidins Most Commonly Occurring in Edible Plants
PublikacjaNumerous studies have provided evidence that diets rich in anthocyanins show a broad spectrum of health benefits. Anthocyanins in nature are usually found in the form of glycosides. Their aglycone forms are called anthocyanidins. The chemical structure of anthocyanins is based on the flavylium cation, but they differ in the position and number of substituents. However, the bioactives and foods that contain them are frequently treated...
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Novel 2-alkythio-4-chloro-N-[imino(heteroaryl)methyl]benzenesulfonamide Derivatives: Synthesis, Molecular Structure, Anticancer Activity and Metabolic Stability
PublikacjaA series of novel 2-alkythio-4-chloro-N-[imino-(heteroaryl)methyl]benzenesulfonamide derivatives, 8–24, were synthesized in the reaction of the N-(benzenesulfonyl)cyanamide potassium salts 1–7 with the appropriate mercaptoheterocycles. All the synthesized compounds were evaluated for their anticancer activity in HeLa, HCT-116 and MCF-7 cell lines. The most promising compounds, 11–13, molecular hybrids containing benzenesulfonamide...
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New methodology for determination cationic surfactants in liquid environmental samples
PublikacjaBecause of their specific physical and chemical properties (e.g. amphiphilicity, solubility in polar and nonpolar liquids, ability to form micelles, adsorption at phase boundaries, low toxicity) surfactants (surface-active compounds) are widely applied in industry and in the household. As their applications are on a very large scale, it has become necessary to acquire a more detailed understanding of their environmental fate. Mainly,...
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Forced Degradation Studies of Ivabradine and In Silico Toxicology Predictions for Its New Designated Impurities
PublikacjaAll activities should aim to eliminate genotoxic impurities and/or protect the API against degradation. There is a necessity to monitor impurities from all classification groups, hence ivabradine forced degradation studies were performed. Ivabradine was proved to be quite durable active substance, but still new and with insufficient stability data. Increased temperature, acid, base, oxidation reagents and light were found to cause...
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Chitosan-based electrospun nanofibers for encapsulating food bioactive ingredients: A review
PublikacjaToday, society has been more aware of healthy food products and related items containing bioactive compounds, which potentially contribute to human health. Unfortunately, the long-term stability and bioactivity of biologically active compounds against environmental factors compromise their target and effective action. In this way, lab-designed vehicles, such as nanoparticles and nanofibers, provide enough properties for their preservation...
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublikacjaDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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Are the short cationic lipopeptides bacterial membrane disruptors? Structure-Activity Relationship and molecular dynamic evaluation
PublikacjaShort cationic lipopeptides are amphiphilic molecules that exhibit antimicrobial activity mainly against Grampositives. These compounds bind to bacterial membranes and disrupt their integrity. Here we examine the structure-activity relation (SAR) of lysine-based lipopeptides, with a prospect to rationally design more active compounds. The presented study aims to explain how antimicrobial activity of lipopeptides is affected by...
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Standing Waves in a Rectangular Resonator Containing Acoustically Active Gases
PublikacjaThe distribution of perturbations of pressure and velocity in a rectangular resonator is considered. A resonator contains a gas where thermodynamic processes take place, such as exothermic chemical reaction or excitation of vibrational degrees of a molecule’s freedom. These processes make the gas acoustically active under some conditions. We conclude that the incident and reflected compounds of a sound beam do not interact in the...
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Synthesis and electrochemical characteristics of novel dithiocarbamate polymers
PublikacjaNovel dithiocarbamate compounds have been obtained by reacting a linear poly(ethylenimine)polymer, MW 50,000, with CS2. The resulting anionic polymers contain, depending on the reaction conditions, up to two sulfur atoms per one nitrogen atom (approx. 40% w/w). The polymers are soluble in dimethylsulfoxide and insoluble in acetonitrile solutions. In both solvents they are electrochemically active, in the latter case as a cast film...
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Biopolymers in designing modern antimicrobial medical materials. Part I. Biopolymer medical materials - collagen, chitosan
PublikacjaThe article is a review of the literature concerning the possible use of biopolymers for the preparation of dressings with antimicrobial activity. Authors show the potential of biopolymers: collagen and chitosan - which have the ability to immobilize and control the release of various active compounds - for providing the appropriate antibacterial, bacteriostatic and wound healing properties. Types of threats, for which the dressing...
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublikacjaNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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The impact of interactions between polyphenolic antioxidants on the redox-related chemical and biological properties of their mixtures – the extension of food synergy concept.
PublikacjaThe results of studies indicate that chemopreventive efficiency of isolated phytochemicals is lower than that of polyphenol-rich foods. This discrepancy has been ascribed to the food synergy concept that assumes additive or even synergistic influence of different food ingredients on human health. The results presented in the dissertation made it possible to propose an alternative and innovative explanation of these observations. The...
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NUTRITIONAL AND PHARMACEUTICAL APPLICATIONS OF BIOACTIVE COMPOUNDS IN TROPICAL FRUITS
PublikacjaDuring the past two decades our international scientific group investigated in vitro the physicochemical and nutritional characteristics of some cultivars of durian at various stages of ripening, mangosteen and new cultivars of snake fruit in comparison with widely used avocado, kiwifruit and mango, and in vivo their influence on laboratory animals. The main objective of the present study was to screen and compare the properties...
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Hybrid analogues of SFTI-1 modified in P1 position by β- and γ-amino acids and N-substituted β-alanines
PublikacjaA series of compounds containing either non-proteinogenic beta-/gamma-amino acids or N-substituted beta-alanine residues (beta-peptoid units) in P-1 specificity position were synthesized based on the structure of sunflower trypsin inhibitor 1 (SFTI-1). The compounds were synthesized on a solid support; the N-substituted beta-alanines (beta Nhlys and beta Nhphe) were introduced into a peptidomimetic chain via a two-step approach...
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Chapter 8 – Active Sampling of Air
PublikacjaThis chapter reviews the literature information on analytical techniques and laboratory equipment used for active sampling of air (atmospheric and indoor) in regular monitoring research. It describes popular analytical devices applied for sample collection using various types of polymeric bags, e.g. Tedlar bags, Teflon or Nafion bags, and/or stainless steel vacuum containers. It reviews literature data about the application of...
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Forced degradation studies of ivabradine and in silico toxicology predictions for its new designated impurities
PublikacjaAll activities should aim to eliminate genotoxic impurities and/or protect the API againstdegradation. There is a necessity to monitor impurities from all classification groups,hence ivabradine forced degradation studies were performed. Ivabradine was provedto be quite durable active substance, but still new and with insufficient stability data.Increased temperature, acid, base, oxidation reagents and...
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Investigations on the removal of hydrophobic odorous volatile organic compounds by biotrickling filtration monitored with electronic nose
PublikacjaThe presented paper presents the results of research on the removal of selected hydrophobic volatile organic compounds (VOCs) from their mixture with air by means of a trickled-bed biofiltration. The efficiency of the removal of toluene and α-pinene, as model VOCs, in a three-section biotrickling filter is evaluated using GCFID and additionally monitored with an electronic nose. The results show that the removal of the model mixture...
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Xanthone synthetic derivatives with high anticandidal activity and positive mycostatic selectivity index values
PublikacjaWith the current massive increases in drug-resistant microbial infection as well as the significant role of fungal infections in the death toll of COVID-19, discovering new antifungals is extremely important. Natural and synthetic xanthones are promising derivatives, although only few reports have demonstrated their antifungal mechanism of action in detail. Newly synthetized by us xanthone derivative 44 exhibited strong antifungal...
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Application of deep eutectic solvents for separation and determination of bioactive compounds in medicinal plants
PublikacjaThe medicinal plants industry, particularly in regard to products rich in biologically active substances for maintaining health, has grown by leaps and bounds in the last decade, with sales of over-the-counter drugs containing these substances growing by billions of dollars. Attention has thus also been paid to the safety and effectiveness of these medicines. We are currently witnessing a rapid increase in the number of publications...
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Novel 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives as potent anticancer agents – Synthesis, molecular structure, QSAR studies and metabolic stability
PublikacjaA series of new 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The obtained results indicated that these compounds display prominent cytotoxic effect. The best anticancer properties have been observed for derivatives...
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Molecular geometry and optical activity of helically chiral N-nitrosamines derived from 1,2,3,4-tetrahydro- and 1,2,3,4,7,8,9,10-octahydro-1,10-phenanthroline
PublikacjaX-ray crystallographic analysis of the title N-nitrosamines revealed that they assume helical conformations in the solid state. Nitrosamines 1b and 2b were resolved by inclusion crystallization with optically active diols (TADDOLs). The absolute configuration of the guest molecules in the complexes 1b·3b and 2b·3b was assigned as M. The optical activity of the resolved compounds is manifested by their solid state CD spectra, which...
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In vitro and in silico assessment of anti-inflammatory activity of cocoa powders
PublikacjaPlants are considered the major sources of biologically active compounds, which provide unlimited opportunities for their use either as medical treatments or as novel drug formulations. Cocoa powder is frequently used in nutrition and is known to have many benefits thanks to its wide range of biological activities. The presented study was focused on th evaluation of the anti-inflammatory potential of extracts obtained from cocoa...