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Wyniki wyszukiwania dla: drugs metabolizing enzymes
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Impact of high-pressure processing on the bioactive compounds of milk - A comprehensive review
PublikacjaHigh-pressure processing (HPP) is a promising alternative to thermal pasteurization. Recent studies highlighted the effectivity of HPP (400–600 MPa and exposure times of 1–5 min) in reducing pathogenic microflora for up to 5 logs. Analysis of modern scientific sources has shown that pressure affects the main components of milk including fat globules, lactose, casein micelles. The behavior of whey proteins under HPP is very important...
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Bee Pollen and Bee Bread as a Source of Bacteria Producing Antimicrobials
PublikacjaThe principal objective of the study was the isolation and identification of bacteria that are present in mature bee bread (BB) and dried (ready for selling and consumption) bee pollen (BP). Obtained isolates were screened for their potential to inhibit select human pathogenic bacteria and their ability to produce enzymes of particular industrial importance. Four and five samples of BP and BB, respectively, were used for the study....
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Determination of antibiotic residues in honey
PublikacjaHoney produced by honeybees is a valuable food product. The presence of xenobiotics in honey may harm its quality and constitute a danger to human health. Antibiotics are commonly applied by beekeepers to eliminate disease among honeybees. Moreover, ubiquitous administration of antibiotics may cause bacteria to become resistant to many drugs and spread antibioticresistant strains of bacteria. Appropriate sample preparation and...
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Electrochemicalsynthesis of 3D nano-/micro-structured porous polypyrrole
PublikacjaIn this work, electrosynthesis of electroactive, 3D nano-/micro-structured porous polypyrrole film is presented. The PPy film was synthesized potentiostatically in a one-step process from aqueous solution of pyrrole and lithium perchlorate. The growth mechanism of such structure included: the formation of typical globular PPy film, followed by the formation of the PPy fibers, which then took part in the formation of 3D highly porous...
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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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Common methods for the chiral determination of amphetamine and related compounds I. Gas, liquid and thin-layer chromatography
PublikacjaThis article reviews the most common, useful methods for the chiral determination of amphetamine (AM) and AM-deriveddesigner drugs in different of matrix, including blood, hair, urine, medicaments or standard solutions, taking into considerationarticles published in the past 15 years. We consider chromatographic methods (e.g., gas, liquid, high-performance liquid, and thinlayer). We describe several types of chiral derivatization...
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Phospholipids as potential prevention factor in carcinogenesis
PublikacjaPhospholipids are a group of complex lipids, which can be used in cancer chemoprevention. Glicerophospholipids are composed of fatty acids esterified to a glycerol backbone, a phosphate group and a hydrophilic residue such as: cho- line, ethanoloamine, serine or inositol. In the sn-2 position of glicerophospholipid usually there are unsaturated fatty acids, i.e. linolenic acid, while in the sn-1 position more typi- cal are saturated...
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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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Investigation of interaction between xanthene dye rhodamine B and metagenomic-derivated methylthioadenosine phosphorylase RSFP
PublikacjaIn the previous study we found that the expression of the metagenomic - derived methylthioadenosine phosphorylase gene (rsfp) in E. coli cells and the presence of rhodamine B in the growth medium were crucial for the pink fluorescence of one E. coli colony from Antarctic soil metagenomic library (Cieśliński et al., 2009). In this study, rsfp gene expression was induced by an arabinose promoter in an LMG194 E. coli strain and the...
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Analytical procedures for determination of cocaine and its metabolites in biological samples
PublikacjaThe dangerous effects and increased usage of illicit drugs have inspired the development of analytical methodologies. We based our review of analytical procedures for determination of cocaine (COC) and its metabolites on literature from the past two decades. Our main aim was to compare the capabilities of different analytical techniques. The diversity of matrices from which COC is determined (e.g., blood, hair, saliva, plasma,...
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Crystal structures of (E)-3-(4-hydroxybenzylidene)chroman-4-one and (E)-3-(3-hydroxybenzylidene)-2-phenylchroman-4-one
PublikacjaThe synthesis and crystal structures of (E)-3-(4-hydroxybenzylidene)chroman-4-one, C16H12O3,I, and (E)-3-(3-hydroxybenzylidene)-2-phenylchroman-4-one,C22H16O3,II, are reported. These compounds are of interest with respect to biological activity. Both structures display intermolecular C—H---O and O—H---O hydrogen bonding, forming layers in the crystal lattice. The crystal structure of compound I is consolidated...
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Biochemistry - Laboratory exercises - Nowy
Kursy OnlineExerise 1. The ability to accumulate metal cations by edible mushrooms, comparison with edible plants Exercise 2. Measurement of activity of glutathione S-transferases - the detoxifying enzymes present in the cytosol of eukaryotic cells Exercise 3. Cell membranes permeability Exercise 4. Detection of mutagenic substances using Ames test Exercise 5. Gluten content in food products part 1. Exercise 6. Gluten content in food...
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Biochemistry - Laboratory exercises
Kursy OnlineExerise 1. The ability to accumulate metal cations by edible mushrooms, comparison with edible plants Exercise 2. Measurement of activity of glutathione S-transferases - the detoxifying enzymes present in the cytosol of eukaryotic cells Exercise 3. Cell membranes permeability Exercise 4. Detection of mutagenic substances using Ames test Exercise 5. Gluten content in food products part 1. Exercise 6. Gluten content in food...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublikacjaMany people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. Todate, many acridine/acridone analogues have been obtained,which, inter alia, exhibit...
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Rapid determination of multiple aminoglycoside antibiotics in veterinary formulations by ion-pair chromatography coupled with evaporative light scattering detection
PublikacjaA fast and simple method for simultaneous determination of eight aminoglycoside antibiotics using ion-pairing liquid chromatography (IPLC) coupled with evaporative light scattering detection (ELSD) has been developed and validated. Separation of amikacin, apramycin, gentamicin (as a sum of gentamicin C1, C2 and C1A), kanamycin A, neomycin B, paromomycin, streptomycin and tobramycin was achieved using C18 column with H2O and MeOH/acetone,...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publikacja6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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3D polypyrrole structures as a sensing material for glucose detection
PublikacjaIn this work, 3D polypyrrole (PPy) structures as material for glucose detection is proposed. Polypyrrole was electrochemically polymerized on platinum screen-printed electrode from an aqueous solution of lithium perchlorate and pyrrole. The growth mechanism of such PPy structures was studied by ex-situ scanning electron microscopy. Preliminary studies show that studied here PPy film is a good candidate as a sensing material for...
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RESIDUE ANALYSIS OF ETU AND PTU BY LC/MS
PublikacjaDithiocarbamates (DTCs) are important organosulfur compounds, which act as inhibitors of metal dependant and sulphydryl enzymes and have a serious consequence on biological systems. They possess variety of applications in agriculture as fungicides, as well as, in the rubber industry as vulcanization accelerators and antioxidants. In this way, DTCs are the main group of fungicides used to control approximately 400 pathogens of more...
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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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Polymer and graphitic carbon nitride based nanohybrids for the photocatalytic degradation of pharmaceuticals in wastewater treatment – A review
PublikacjaPharmaceuticals, including antibiotics and anti-inflammatory drugs, have been frequently detected in water reservoirs, in concentrations ranging from ng/L to μg/L, owing to their wide use in treatment of human and animal disease. Their uncontrolled use results in their increased release into the environment which is harmful for humans, animals, aquatic life and aquatic system. To remove these pollutants from water bodies, various...
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Recent developments in biological sample testing methods for the confirmation of gestational exposure to tobacco smoke anddrugs of abused
PublikacjaSubstance use is most prevalent in reproductive-aged people also by women during pregnancy. In national prevalence surveys among women aged 15 to 44 years, 10.8 % of women reported using alcohol during pregnancy, 17 % reported smoking during pregnancy, and 4.4 % reported abusing any illicit substances during pregnancy. Virtually all illegal drugs, such as heroin and cocaine, pose dangers to a pregnant woman. Legal substances, such...
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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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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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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the antitumor imidazoacridinone C-1311 in human hepatoma cells
PublikacjaThere is increasing evidence that the expression level of drug metabolic enzymes affects the final cellular response following drug treatment. Moreover, anti-tumour agents may modulate enzymatic activity and/or cellular expression of metabolic enzymes in tumour cells. We investigated the influence of CYP3A4 overexpression on the cellular response induced by the anti-tumour agent C-1311 in hepatoma cells. C-1311-mediated CYP3A4...
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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublikacjaChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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Characterization of two aminotransferases from Candida albicans
PublikacjaAminoadipate aminotransferase (AmAA) is an enzyme of α-aminoadipate pathway (AAP) for l-lysine biosynthesis. AmAA may also participated in biosynthesis or degradation of aromatic amino acids and in d-tryptophan based pigment production. The AAP is unique for fungal microorganisms. Enzymes involved in this pathway have specific structures and properties. These features can be used as potential molecular markers. Enzymes catalyzing...
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Proteomic and Metabolomic Changes in Psoriasis Preclinical and Clinical Aspects
PublikacjaSkin diseases such as psoriasis (Ps) and psoriatic arthritis (PsA) are immune-mediated inflammatory diseases. Overlap of autoinflammatory and autoimmune conditions hinders diagnoses and identifying personalized patient treatments due to different psoriasis subtypes and the lack of verified biomarkers. Recently, proteomics and metabolomics have been intensively investigated in a broad range of skin diseases with the main purpose...
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Results of the effect of mixtures of ketoprofen with three cations on the germination of Sorghum bicolor (sorghum) seeds
Dane BadawczeThe research data includes an attempt to verify whether the addition of cations (sodium, ammonium and potassium) at levels found in the environment would affect the toxicity of pharmaceuticals to Sorghum Bicolor grain. Ion concentrations were selected based on studies of water samples collected in water bodies receiving wastewater from wastewater treatment...
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Results of the effect of mixtures of ketoprofen with three anions on the germination of Sorghum bicolor (sorghum) seeds
Dane BadawczeThe research data includes an attempt to verify whether the addition of anions (bromide, chloride and fluoride) at levels found in the environment would affect the toxicity of pharmaceuticals to Sorghum Bicolor grain. Ion concentrations were selected based on studies of water samples collected in water bodies receiving wastewater from wastewater treatment...
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Recurrent potential pulse technique for improvement of glucose sensing ability of 3D polypyrrole
PublikacjaIn this work, a new approach for using a 3D polypyrrole (PPy) conducting polymer as a sensing material for glucose detection is proposed. Polypyrrole is electrochemically polymerized on a platinum screen-printed electrode in an aqueous solution of lithium perchlorate and pyrrole. PPy exhibits a high electroactive surface area and high electrochemical stability, which results in it having excellent electrocatalytic properties. The...
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Low frequency of itraconazole resistance found among avian Aspergillus fumigatus isolates
PublikacjaAspergillus fumigatus is the most frequent etiological factor of invasive aspergillosis in human as well as animals, including birds. Aspergillosis caused by drug-resistant strains poses a significant therapeutic issue, especially if resistance pattern includes insensitivity to triazoles, i.e. drugs recommended for the primary therapy purposes. Majority of resistant isolates hold the TR34/L98H...
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The impact of lipophilicity on environmental processes, drug delivery and bioavailability of food components
PublikacjaLipophilic properties of the compound allow to predict its fate in living organisms and to propose the models of chemicals transport and accumulation in the ecosystem. Lipophilicity is also useful as the characteristic of chemicals in respect to their optimal attributes for specific biological and non-biological tasks. The lipophilicity descriptors define the potency of endo- and xenobiotics to metabolic transformations and their...
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Novel Tools for Comprehensive Functional Analysis of LDLR (Low-Density Lipoprotein Receptor) Variants
PublikacjaFamilial hypercholesterolemia (FH) is an autosomal-dominant disorder caused mainly by substitutions in the low-density lipoprotein receptor (LDLR) gene, leading to an increased risk of premature cardiovascular diseases. Tremendous advances in sequencing techniques have resulted in the discovery of more than 3000 variants of the LDLR gene, but not all of them are clinically relevant. Therefore, functional studies of selected variants...
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Assestment of the anti-cancer activity of the copper complexes with imidazole and pivalato ligands
PublikacjaDespite the development of science and technology progress so far there have not been found effective drugs for cancer. Many coordination compounds were investigated due to their antitumor potential. The most known cis-diamminedichloroplatinum(II) is used as anti-cancer therapeutic agent. The copper complexes are the coordination compounds possessing anti-tumour properties. Their capability to kill cancer cells is mainly linked...
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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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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publikacja5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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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
PublikacjaTwo 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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Antimicrobial Activity of Chimera Peptides Composed of Human Neutrophil Peptide 1 (HNP-1) Truncated Analogues and Bovine Lactoferrampin
PublikacjaThree chimera peptides composed of bovine lactoferrampin and the analogue of truncated human neutrophil peptide 1 were synthesized by the solid-phase method. In two compounds peptide chains were connected via isopeptide bond, whereas in the third one disulfide bridge served as a linker. All three chimeras displayed significantly higher antimicrobial activity than the constituent peptides as well as their equimolar mixtures. The...
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Problematyka dotycząca zapewnienia fotostabilności substancji leczniczych w postaciach leku
PublikacjaUV and visible radiation may influence on the stability of some active pharmaceutical ingredients and in a consequence destabilizes such medicinal products, causes changesin its physicochemical properties also with negative pharmacological and sometimes even toxic effects. For this reason it is important to conduct the routine testing photostability. The knowledge of chemistry and technology as well as some methods of...
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Detection of some volatile degradation products released during photoexposition of ranitidine in a solid state
PublikacjaRanitidine (RAN) is on top of the list of prescribed drugs, due to its popularity as a selective H2-receptor antagonist, which efficiently decreases the amount of acid produced in the stomach. RAN is not stable both in a solid state and in a solution, which creates manufacturing problems, requires appropriate storage conditions, and results in a short drug shelf-life. The aim of this work was to study the emission of volatile...
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Determination of pharmaceuticals in fish: method optimization and occurrence in different species from Mediterranean rivers
PublikacjaThe multi-residue analytical method developed, based on accelerated solvent extraction, gel permeation chromatography purification and UPLC-MS/MS analysis allowed the simultaneous determination of 21 pharmaceuticals. Recoveries obtained for most of the target compounds were higher than 50%. The application of UPLC-MS/MS operating in the MRM mode, with two transitions monitored for each compound, provided good sensitivity and selectivity....
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New oryginal generic technologies: A Polish R&D strategic implementation programme
PublikacjaPolands's pharmaceutical industry is of great significance to the whole economy. According to Forbs (2 October 2012), the cost of launching a new drug varies from USD 1 to 11 bilion. There is little Chance of a Polish pharmaceutical company developing an original drug due to financial reason.Many research teams in Poland take up research projects aimed at new biologically active compounds. But such an objective has no broader perspective,...
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Review on Current Status of Echinocandins Use
PublikacjaFungal infections are rising all over the world every year. There are only five medical compound classes for treatment: triazoles, echinocandins, polyenes, flucytosine and allylamine. Currently, echinocandins are the most important compounds, because of their wide activity spectrum and much lower sides effects that may occur during therapy with other drugs. Echinocandins are secondary metabolites of fungi, which can inhibit the...
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Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery
PublikacjaAbstract: Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently...
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A new assay based on terminal restriction fragment length polymorphism of homocitrate synthase gene fragments for Candida species identification
PublikacjaCandida sp. have been responsible for an increasing number of infections, especially in patients with immunodeficiency. Species specific differentiation of the Candida sp. is difficult in routine diagnosis. This identification can have a highly significant association in therapy and prophylaxis. This work has shown a new application of terminal restriction fragment length polymorphism (t-RFLP) method in molecular identification...
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Green chemical and hybrid enzymatic pretreatments for lignocellulosic biorefineries: Mechanism and challenges
PublikacjaThe greener chemical and enzymatic pretreatments for lignocellulosic biomasses are portraying a crucial role owing to their recalcitrant nature. Traditional pretreatments lead to partial degradation of lignin and hemicellulose moieties from the pretreated biomass. But it still restricts the enzyme accessibility for the digestibility towards the celluloses and the interaction of lignin-enzymes, nonproductively. Moreover, incursion...
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Determination of isoprostanes in exhaled breath condensate samples by liquid chromatography coupled with tandem mass spectrometry
PublikacjaOxidative stress (OS) is a state of imbalance between continuously generating reactive oxygen species (ROS) during normal cell metabolism and mechanism of detoxifying oxygen radicals through a network of antioxidative enzymes. Isoprostanes are prostaglandin -like substances that are produced in vivo primarily by free radical-induced peroxidation of arachidonic acid. The measurement of isoprostanes in biological fluids and/or tissue...
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Virulence of Clinical Candida Isolates
PublikacjaThe factors enablingCandidaspp. infections are secretion of hydrolytic enzymes, adher-ence to surfaces, biofilm formation or morphological transition, and fitness attributes. The aim of thisstudy was to investigate the correlation between known extracellular virulence factors and survivalofGalleria mellonellalarvae infected with clinicalCandida. The 25 isolates were tested and the activityof proteinases among 24/24, phospholipases...
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Chiral Pyrazolo[4,3-e][1,2,4]triazine Sulfonamides—Their Biological Activity, Lipophilicity, Protein Affinity, and Metabolic Transformations
PublikacjaReferring to our previous laboratory results related to the tyrosinase and urease inhibition by pyrazolo[4,3-e][1,2,4]triazine sulfonamides, we examined here in silico the mechanism of action at the molecular level of the investigated pyrazolotriazine sulfonamides by the molecular docking method. The studied compounds being evaluated for their cytotoxic effect against cancer cell lines (MCF-7, K-562) and for recombinant Abl and...
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Vehicle Dynamics - L-15/C-15/L-15/P-15, Design and Production Engineering, WIMiO, undergraduate studies, engineering studies, full-time (stationary) studies, 2021/2022, se06, (M:320383W0), summer semester 2023/2024
Kursy OnlineModuł przedmiotów wybieralnych, MiBM, I stopień, specjalność w j. angielskim: Design and Production Engineering (DaPE), semestr 6?, (przedmiot dla Chińczyków), Lecture: Throttle by tyred wheel: slip rolling, rolling with tyre strain, vertical and lateral surface reactions, traction, energetic looses, forces in contact path. Drugs of movement: rolling, air, gradient, inertia, cornering and towing. Forces ant torques acting to vehicle...