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Search results for: DRUGS METABOLIZING ENZYMES
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublicationThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Small regulatory bacterial RNAs regulating the envelope stress response
PublicationMost bacteria encode a large repertoire of RNA-based regulatory mechanisms. Recent discoveries have revealed that the expression of many genes is controlled by a plethora of base-pairing noncoding small regulatory RNAs (sRNAs), regulatory RNA-binding proteins and RNA-degrading enzymes. Some of these RNA-based regulated processes respond to stress conditions and are involved in the maintenance of cellular homeostasis. They achieve...
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Effect of dendrimer-based interlayers for enzyme immobilization on a model electrochemical sensing system for glutamate
PublicationIn this paper, we discuss dendrimer usage in enzyme-based electrochemical biosensors, particularly with respect to biomolecule loading on the sensing surface. A novel approach to design bioactive layers with immobilized enzymes for electrochemical biosensors using the surface plasmon resonance (SPR) method in combination with electrochemical impedance spectroscopy was presented. The gold surface was modified with linear linkers...
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Which casein in sodium caseinate is most resistant to in vitro digestion? Effect of emulsification and enzymatic structuring
PublicationWe investigated the resistance of individual constituent casein epitopes (αS1-, αS2-, β- and κ-CN) in food-grademilk protein sodium caseinate (NaCN) to simulated human gastro-duodenal digestion. The influence of NaCNadsorption to the surface of oil-in-water emulsion droplets and the effect of crosslinking of the protein withenzyme transglutaminase (TG) on the proteolysis were studied by indirect ELISA. TG crosslinking renderedfragments...
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Chromatographic analyses of Lavandula angustifolia and Rosmarinus officinalis extracts and their biological effects in mammalian cells and cell-free systems
PublicationKnowledge of biological properties of natural compounds allows to understand their therapeutic value, efficacy and security. We investigated: composition of Lavandula angustifolia (LA) and Rosmarinus officinalis (RO) extracts, their antioxidant capacity, cytotoxicity and genotoxicity, their DNA-protective potential against DNA damage induced in hamster V79 cells by several genotoxins or in plasmid DNA by Fe2+ ions and activity...
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Progress in targeting tumor cells by using drug-magnetic nanoparticles conjugate.
PublicationTo limit the cytotoxicity of anticancer drugs against healthy cells, an appropriate carrier should be synthesized to deliver the drug to the tumor tissue only. A good solution is to anchor a magnetic nanoparticle to the molecule of the drug and to use a properly directed external magnetic field. We have shown that the improved by us synthesis of the conjugate of doxorubicin with iron-oxide magnetic nanoparticles allows a substantial...
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Preparation and evaluation of 1,3-alternate 25,27-bis-(pentafluorobenzyloxy)-26,28-bis-(3-propyloxy)-calix[4]arene-bonded silics gel high performance liquid chromatography stationary phase
PublicationA 1,3-alternate 25,27-bis-(pentafluorobenzyloxy)-26,28-bis-(3-propyloxy)-calix[4]arene-bonded silica gel stationary phase (CalixBzF10) was synthesized, structurally characterized, and used as a selector in liquid chromatography. The selectivity study of this phase was done by using fluorine-containing compounds (fluorobenzenes, fluoro-pyrimidine bases), as well as non-fluorinated analytes (non-steroidal anti-inflammatory drugs,...
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Analytical studies on ascosin, candicidin and levorin multicomponent antifungal antibiotic complexes. The stereostructure of ascosin A2
PublicationIn the class of polyene macrolides, there is a subgroup of aromatic heptaenes, which exhibit the highest antifungal activity within this type of antibiotics. Yet, due to their complex nature, aromatic heptaenes were not extensively studied and their potential as drugs is currently underexploited. Moreover, there are many inconsistencies in the literature regarding the composition and the structures of the individual components...
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublicationThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...
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Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity
PublicationEight new peptide conjugates composed of modified bovine lactoferricin truncated analogues (LFcinB) and oneof the three antimicrobials — ciprofloxacin (CIP), levofloxacin (LVX), and fluconazole (FLC) — were synthesized. Four different linkers were applied to connect a peptide and an antimicrobial agent. The FLC-containing peptidic conjugates were synthesized using the “click chemistry” method. This novel approach is reported here...
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First report on echinocandin resistant Polish Candida isolates
PublicationPurpose: Candida spp. are ranked as one of the four major causative agents of fungal infections. The number of infections caused by Candida species resistant to fluconazole, which is applied as the first line drug in candidiasis treatment, increases every year. In such cases the application of echinocandin is necessary. Echinocandin susceptibility testing has become a routine laboratory practice in many countries due to the increasing...
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An MTA-phosphorylase gene discovered in the metagenomic library derived from Antarctic top soil during screening for lipolytic active clones confers strong pink fluorescence in the presence of rhodamine B.
PublicationIn this work, we present the construction of a metagenomic library in Escherichiacoli using the pUC19 vector and environmental DNA directly isolated fromAntarctic topsoil and screened for lipolytic enzymes. Unexpectedly, the screeningon agar supplemented with olive oil and rhodamine B revealed one unusual pinkfluorescent clone (PINKuv) out of 85 000 clones. This clone harbored a plasmid,pPINKuv, which has an insert of 8317 bp that...
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Identification and molecular modeling of a novel lipase from an Antarctic soil metagenomic library.
PublicationIn this work, we present the construction of a metagenomic library in Escherichia coli using pUC19 vector and environmental DNA directly isolated from Antarctic topsoil and screened for lipolytic enzymes. The screening on agar supplemented with olive oil and rhodamine B revealed one clone with lipolytic activity (Lip1) out of 11,000 E. coli clones. This clone harbored a plasmid, pLip1, which has an insert of 4722 bp that has been...
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Cabbage Juices and Indoles Modulate the Expression Profile of AhR, ERα, and Nrf2 in Human Breast Cell Lines
PublicationOur previous studies showed the diversified effect of cabbage juices and indoles on the estrogen metabolism key enzymes (CYP1A1, CYP1A2, CYP1B1) in breast epithelial cells differing in ER status, i.e., in tumorigenic—MCF7, MDA-MB-231 and non-tumorigenic—MCF10A cells. The aim of the present study was to further investigate the mechanism of chemopreventive action of cabbage juice and its active components by evaluating their effect...
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Characterization of immobilized Escherichia coli cells transformed by β-galactosidase gene from Pyrococcus woesei
PublicationThermostable β-galactosidase from Escherichia coli transformant containing theenzyme gene from Pyrococcus woesei was immobilized on alginate gel.The benefits of using whole bacterial cells not only exclude expensive, laborious proteinisolation and purification but also stabilize enzymes by cytosol components. Increase inproductivity of enzyme can be achieved by cells permeabilization. To increase permeability ofcytoplasmic membrane...
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Investigation of the antimicrobial potential and microbiota of bee pollen and bee bread derived from Polish apiaries
PublicationThe phenomenon of resistance of microorganisms to antibiotics is becoming one of the greatest challenges of modern medicine. At the same time, the number of new antibiotics introduced into clinical practice is decreasing. This creates the need to search for new, effective, non-antibiotic methods of combating and preventing infectious diseases. Over the last two decades, there has been renewed interest in the antimicrobial potential...
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Study of pH and temperature effect on lipophilicity of catechol-containing antioxidants by reversed phase liquid chromatography
PublicationLipophilicity of selected antioxidant phytochemicals, including flavonoids, phenolic acids and xanthonoids, was determined by reversed phase high performance liquid chromatography with UV detection (RP-HPLC-UV). The analyses run at different temperature and pH conditions in isocratic mode suggested that lipophilicity as distribution coefficient (logD) between aqueous and organic phase decreases with increasing temperature. For...
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Hydrogen Production from Energy Poplar Preceded by MEA Pre-Treatment and Enzymatic Hydrolysis
PublicationThe need to pre-treat lignocellulosic biomass prior to dark fermentation results primarily from the composition of lignocellulose because lignin hinders the processing of hard wood towards useful products. Hence, in this work a two-step approach for the pre-treatment of energy poplar, including alkaline pre-treatment and enzymatic saccharification followed by fermentation has been studied. Monoethanolamine (MEA) was used as the...
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Prediction of Bioactive Peptides From Chicken Feather and Pig Hair Keratins Using In Silico Analysis Based on Fragmentomic Approach
PublicationBackground: Keratin is among the most abundant structural proteins of animal origin, however it remains broadly underutilized. Objective: Bioinformatic investigation was performed to evaluate selected keratins originating from mass-produced waste products, i.e., chicken feathers and pig hair, as potential sources of bioactive peptides. Methods: Pepsin, trypsin, chymotrypsin, papain, and subtilisin were used for in silico keratinolysis...
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Effect of Ethanol Extracts of Propolis (EEPs) against Staphylococcal Biofilm—Microscopic Studies
PublicationStaphylococci growing in the form of biofilm exhibit high resistance to a plethora of antibiotics. The aim of the study was to assess the influence of ethanolic extract of propolis (EEPs) on S. epidermidis ATCC 35984 biofilm using fluorescent microscopy. Propidium iodide (PI) and SYTO 9 were used for differentiation of live and dead cells, and calcofluor white was used to stain the extracellular matrix, the self-produced extracellular...
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Treatment innovation using solar/UV In book: The Treatment of Pharmaceutical Wastewater: Innovative Technologies and the Adaptation of Treatment Systems
PublicationSince 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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Common methods for the chiral determination of amphetamine and related compounds II: Capillary electrophoresis and nuclear magnetic resonance
PublicationAmphetamine group and related ring-substituted substances are generally synthetic compounds, belonging to one of the most heavily abused drug groups in recent years. Some compounds in this class also originate from plants. Analysis of the enantiomers of AM-type compounds and metabolites is extremely important for a number of scientific disciplines. From studies of biological activity or mechanisms through determination of precursor...
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Evaluation of Body Surface Area Formulae Based on 3D Body Scans
PublicationHuman body surface area (BSA) is an established parameter for the calculation of chemotherapy drugs dosage, treatment of chronic hepatitis B, treatment of burns or for establishing a dosing regimen for antimicrobials. Although being a critical parameter, usage of modern 3D scanners, which would measure the exact BSA value, is often impossible in time-sensitive operations or for patients unable to withstand the scanning process....
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‘Acridines’ as New Horizons in Antifungal Treatment
PublicationFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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Implementing fermentation technology for comprehensive valorisation of seafood processing by-products: A critical review on recovering valuable nutrients and enhancing utilisation
PublicationFermentation technology is a biorefining tool that has been used in various industrial processes to recover valuable nutrients from different side streams. One promising application of this technique is in the reclamation of nutritional components from seafood side streams. Seafood processing generates significant amounts of waste, including heads, shells, and other side streams. These side streams contain high quantities of valued...
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Optimization of Saccharification Conditions of Lignocellulosic Biomass under Alkaline Pre-Treatment and Enzymatic Hydrolysis
PublicationPre-treatment is a significant step in the production of second-generation biofuels from waste lignocellulosic materials. Obtaining biofuels as a result of fermentation processes requires appropriate pre-treatment conditions ensuring the highest possible degree of saccharification of the feed material. An influence of the following process parameters were investigated for alkaline pre-treatment of Salix viminalis L.: catalyst concentration...
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The bile salt content of human bile impacts on simulated intestinal proteolysis of β-lactoglobulin
PublicationThe gastrointestinal hydrolysis of food proteins has been portrayed in scientific literature to predominantly depend on the activity and specificity of proteolytic enzymes. Human bile has not been considered to facilitate proteolysis in the small intestine, but rather to assist in intestinal lipolysis. However, human bile can potentially influence proteins that are largely resistant to gastric digestion, and which are mainly hydrolysed...
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Distinguishing of cocrystals from simple eutectic mixtures: phenolic acids as potential pharmaceutical coformers
PublicationThe multiparameter model comprising 1D and 2D QSPR/QSAR descriptors was proposed and validated for phenolic acid binary systems. This approach is based on the optimization of regression coefficients for maximization of the percentage of true positives in the pool of systems comprising either simple binary eutectics or cocrystals. The training set consisted of 58 eutectics and 168 cocrystals. The solid dispersions collection used...
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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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Self-assembly, stability and conductance of amphotericin B channels: bridging the gap between structure and function
PublicationAmphotericin B (AmB), one of the most powerful but also toxic drugs used to treat systemic mycoses, is believed to selectively permeabilize fungal cell membranes to ions in a sterol-dependent manner. Unfortunately, the structure of the biologically active AmB channels has long eluded researchers, obstructing the design of safer alternatives. Here, we investigate the structural and thermodynamic aspects of channel formation, stability,...
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Właściwości katalityczne i biomedyczne związków zawierających jony rutenu(II) oraz rutenu(III)
PublicationRuthenium complexes appear in scientific publications mainly as catalysts in the olefins metathesis process. In this review, we want to indicate the research niche regarding the use of ruthenium(II) and ruthenium(III) complexes in other catalytic processes, i.e. polymerization or epoxidation of olefins and depolymerization. We would like to combine the catalytic properties of ruthenium(II,III) complex compounds with their biomedical...
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Stable nanoconjugates of transferrin with alloyed quaternary nanocrystals Ag–In–Zn–S as a biological entity for tumor recognition
PublicationOne way to limit the negative effects of anti-tumor drugs on healthy cells is targeted therapy employing functionalized drug carriers. Here we present a biocompatible and stable nanoconjugate of transferrin anchored to Ag-In-Zn-S quantum dots modified with 11-mercaptoundecanoic acid (Tf-QD) as a drug carrier versus typical anticancer drug, doxorubicin. Detailed investigations of Tf-QD nanoconjugates without and with doxorubicin...
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A five-year retrospective study shows increasing rates of antimicrobial drug resistance in Cabo Verde for both Staphylococcus aureus and Escherichia coli
PublicationObjectives Data on baseline drug resistance is important in informing future antimicrobial stewardship programs. So far, no data on the antimicrobial drug resistance of clinical isolates was available for the African archipelago of Cabo Verde. Methods We have performed a retrospective analysis over five-years (2013-17) of the antimicrombial drug susceptibility profiles of clinical isolates in the two main hospitals of Cabo Verde....
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Increased concentration of Taq DNA polymerase as a solution for GC-rich templates from clinical and environmental samples
PublicationDNA polymerase is an enzyme which plays crucial role in replication and DNA repair. It found application in PCR (polymerase chain reaction) where catalyses process of in vitro DNA synthesis. To meet the demands posed by mod- ern diagnostic, molecular biology or genetic engineering it is necessary to improve DNA polymerases to obtain new or better features useful in these fields. So far implemented modifications in majority are...
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Molecular Strategy for Survival at a Critical High Temperature in Eschierichia coli
PublicationThe molecular mechanism supporting survival at a critical high temperature (CHT) in Escherichia coli was investigated. Genome-wide screening with a single-gene knockout library provided a list of genes indispensable for growth at 47°C, called thermotolerant genes. Genes for which expression was affected by exposure to CHT were identified by DNA chip analysis. Unexpectedly, the former contents did not overlap with the latter except...
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The influence of selenium addition during seeds' germination on the biological properties of obtained sprouts
PublicationSelenium plays a vital role in human body, because in the form of aminoacids (Se-methionine, Se-cysteine) it is found in the active centres of over 25 enzymes, including those regarded as 'cytoprotective'. Unfortunatelly, its daily intake in Poland and other European countries is lower than predicted by dietary recommendations. The consequences of selenium deficiency in diet might be severe, including higher susceptibility to cardio-vascular...
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An overview of fermentation in the food industry - looking back from a new perspective
PublicationFermentation is thought to be born in the Fertile Crescent, and since then, almost every culture has integrated fermented foods into their dietary habits. Originally used to preserve foods, fermentation is now applied to improve their physicochemical, sensory, nutritional, and safety attributes. Fermented dairy, alcoholic beverages like wine and beer, fermented vegetables, fruits, and meats are all highly valuable due to their...
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Bovine Serum Albumin – Hydroxyapatite Nanoflowers as Potential Local Drug Delivery System of Ciprofloxacin
PublicationIntroduction: Hybrid nanoflowers are structures consisting of organic (enzymes, proteins, nucleic acids) and inorganic components (mostly metal phosphates) with a flower-like hierarchical structure. Novel hybrid nanoflowers based on bovine serum albumin (BSA) and hydroxyapatite (HA) were obtained and characterized. Study on BSA-HA nanoflowers as potential drug delivery system is reported for the first time. Methods: Embedding ciprofloxacin...
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Postbiotics in oncology: science or science fiction?
PublicationThe gut microbiome has been increasingly understood to play a critical role in carcinogenesis and cancer disease progression. The most recent research advancements have shown that different tools of microbiota manipulation contribute to gut microbiome–immune–oncology axis modulation, offering exciting opportunities for targeted interventions aimed at improving the efficacy of established anti-cancer therapy. Postbiotics are a new...
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Synthesis of green benzamide-decorated UiO-66-NH2 for biomedical applications
PublicationMetal-organic frameworks (MOFs) biocompatible systems can host enzymes/bacteria/viruses. Herein we synthesized a series of fatty acid amide hydrolase (FAAH)-decorated UiO-66-NH2 based on Citrus tangerine leaf extract for drug delivery and biosensor applications. Five chemically manipulated FAAH-like benzamides were localized on the UiO-66-NH2 surface with physical interactions. Comprehensive cellular and molecular analyses were...
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Catalytic Mechanism of Non-Target DNA Cleavage in CRISPR-Cas9 Revealed by Ab Initio Molecular Dynamics
PublicationCRISPR-Cas9 is a cutting-edge genome editing technology, which uses the endonuclease Cas9 to introduce mutations at desired sites of the genome. This revolutionary tool is promising to treat a myriad of human genetic diseases. Nevertheless, the molecular basis of DNA cleavage, which is a fundamental step for genome editing, has not been established. Here, quantum–classical molecular dynamics (MD) and free energy methods are used...
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INFOGEST static in vitro simulation of gastrointestinal food digestion
PublicationDeveloping a mechanistic understanding of the impact of food structure and composition on human health has increasingly involved simulating digestion in the upper gastrointestinal tract. These simulations have used a wide range of different conditions that often have very little physiological relevance, and this impedes the meaningful comparison of results. The standardized protocol presented here is based on an international consensus...
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A new factor LapD is required for the regulation of LpxC amounts and lipopolysaccharide trafficking
PublicationLipopolysaccharide (LPS) constitutes the major component of the outer membrane and is essential for bacteria, such as Escherichia coli. Recent work has revealed the essential roles of LapB and LapC proteins in regulating LPS amounts; although, if any additional partners are involved is unknown. Examination of proteins co-purifying with LapB identified LapD as a new partner. The purification of LapD reveals that it forms a complex...
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IFI16 Impacts Metabolic Reprogramming during Human Cytomegalovirus Infection
PublicationCellular lipid metabolism plays a pivotal role in human cytomegalovirus (HCMV) infection, as increased lipogenesis in HCMV-infected cells favors the envelopment of newly synthesized viral particles. As all cells are equipped with restriction factors (RFs) able to exert a protective effect against invading pathogens, we asked whether a similar defense mechanism would also be in place to preserve the metabolic compartment from HCMV...
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublicationNew unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of tumor cell lines but also against human tumor xenografts in nude mice. Representative UA compounds, named C-2028, C-2045 and C-2053, were characterized in respect to their physicochemical properties and the following studies aimed to elucidate the role of metabolic transformations in UAs action. We demonstrated with phase I and phase II enzymes...
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Mechanism-based inactivation of human cytochrome P450 1A2 and 3A4 isoenzymes by antitumor triazoloacridinone C-1305.
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, is a promising antitumor therapeutic agent with high activity against several experimental tumors. It was determined to be a potent and selective inhibitor of liver microsomal and human recombinant cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1305 might modulate the effectiveness of other drugs used in multidrug therapy. The objective of this study was...
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Chiral analysis of chloro intermediates of methylamphetamine by one-dimensional and multidementional NMR and GC/MS
PublicationImpurity profiling and classification of abused drugs using chiral analytical techniques is of particular interest and importance because of the additional information obtained fromthis approach. When these methods are applied to the synthesis of illicitly used substances, they can supply valuable information about the conditions/chemicals used in the synthesis. We have applied GC and NMR methods to the study of intermediates found...
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Cellular Effects of Selected Unsymmetrical Bisacridines on the Multicellular Tumor Spheroids of HCT116 Colon and A549 Lung Cancer Cells in Comparison to Monolayer Cultures
PublicationMulticellular tumor spheroids are a good tool for testing new anticancer drugs, including those that may target cancer stem cells (CSCs), which are responsible for cancer progression, metastasis, and recurrence. Therefore, we applied this model in our studies of highly active antitumor unsymmetrical bisacridines (UAs). We investigated the cellular response induced by UAs in 2D and 3D cultures of HCT116 colon and A549 lung cancer...
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Phytochemical screening and biological evaluation of Greek sage (Salvia fruticosa Mill.) extracts
PublicationThis study explores the influence of extraction solvents on the composition and bioactivity of Salvia fruticosa extracts. Ultrasound-assisted extraction with water, ethanol and their mixtures in variable proportions was used to produce four different extracts. An untargeted UPLC/MS‑based metabolomics was performed to discover metabolites profile variation between the extracts. In the analyzed samples, 2704 features had been detected,...
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Green and sustainable hydrogels based on quaternized chitosan to enhance wound healing
PublicationHydrogel-based biomaterials applied as wound dressings provide the wound with a moist environment, which facilitates tissue regeneration through granulation and re-epithelialization. The inherent flexibility and adjustable architecture of hydrogels enables incorporation of cells, antimicrobial drugs, growth factors, and bioactive compounds, which leads to expediting wound contraction and enhancing the regeneration process. The...