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Antitumor 1-nitroacridine derivative C-1748 induces significant apoptosis in pancreatic cancer cells.
PublicationPancreatic cancer is the fifth leading cause of cancer death and has the lowest survival rate of any solid cancer in the industrial countries. The poor prognosis of pancreatic cancer results from its tendency for late presentation, aggressive invasion, early metastasis, and resistance to chemotherapy. Gemcitabine still remains the best chemotherapeutic agent available for the treatment of advanced pancreatic cancer. However, gemcitabine...
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Application of Multivariate Adaptive Regression Splines (MARSplines) for Predicting Hansen Solubility Parameters Based on 1D and 2D Molecular Descriptors Computed from SMILES String
PublicationA new method of Hansen solubility parameters (HSPs) prediction was developed by combining the multivariate adaptive regression splines (MARSplines) methodology with a simple multivariable regression involving 1D and 2D PaDEL molecular descriptors. In order to adopt the MARSplines approach to QSPR/QSAR problems, several optimization procedures were proposed and tested. The effectiveness of the obtained models was checked via standard...
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Novel fused pyran derivatives induce apoptosis and target cell cycle progression in anticancer efficacy against multiple cell lines.
PublicationNitrogen-based heterocycles such as pyrazole, imidazole, 1,2,4-triazole, benzimidazole, and benzotriazole substituted fused pyran derivatives (6a–e, 8a–e, 10a–e, 12a–e,&14a–e) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer cell lines. Among the compounds, 6e, 14b, and 8c were identified as the most potent against MCF7, A549, and HCT116, with IC50 values of 12.46 2.72...
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Selected symmetrically substituted carbazoles: Investigation of anticancer activity and mechanisms of action at the cellular and molecular levels
PublicationDNA topoisomerases play a critical role as essential enzymes in controlling alterations in the topology of DNA. They achieve this by orchestrating the coordinated process of breaking and rejoining DNA strands, which is crucial for maintaining the proper structure of DNA during regular cellular development. The search for and development of new potential anticancer drugs is a challenging yet immensely important area of research...
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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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Body surface area formulae: an alarming ambiguity
PublicationBody surface area (BSA) plays a key role in several medical fields, including cancer chemotherapy, transplantology, burn treatment and toxicology. BSA is often a major factor in the determination of the course of treatment and drug dosage. A series of formulae to simplify the process have been developed. Because easy-to-identify, yet general, body coefficient results of those formulae vary considerably, the question arises as to...
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Alternative treatment approaches of urinary tract infections caused by uropathogenic Escherichia coli strains
PublicationUrinary tract infections (UTIs) are the most widespread and annoying infections affecting millions of people every year annually. The biggest problem of urinary diseases are recurrences, the increasing resistance of uropathogens to commonly used antibiotics, as well as the high health care costs of afflicted persons. Uropathogenic Escherichia coli strains (UPECs) are the most dominant etiologic agent of community-acquired infections...
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Escherichia coli Strains with Virulent Factors Typical for Uropathogens were Isolated from Sinuses from Patients with Chronic Rhinosinusitis—Case Report
PublicationEscherichia coli were isolated from three patients with chronic rhinosinusitis (CRS) by intraoperative sinus tissue biopsy. Taking into account the unusual replicative niche and previous treatment failures, it was decided to focus on the virulence and drug resistance of these bacteria. The strains turned out to be multi-sensitive, but the rich virulence factors profile of bacteria typical for phylogenetic group B2 deserved attention....
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Towards Rational Biosurfactant Design—Predicting Solubilization in Rhamnolipid Solutions
PublicationThe efficiency of micellar solubilization is dictated inter alia by the properties of the solubilizate, the type of surfactant, and environmental conditions of the process. We, therefore, hypothesized that using the descriptors of the aforementioned features we can predict the solubilization efficiency, expressed as molar solubilization ratio (MSR). In other words, we aimed at creating a model to find the optimal surfactant and...
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Green Polymer Nanocomposites for Skin Tissue Engineering
PublicationFabrication of an appropriate skin scaffold needs to meet several standards related to the mechanical and biological properties. Fully natural/green scaffolds with acceptable biodegradability, biocompatibility, and physiological properties quite often suffer from poor mechanical properties. Therefore, for appropriate skin tissue engineering and to mimic the real functions, we need to use synthetic polymers and/or additives as complements...
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Pre-analytical aspects in metabolomics of human biofluids – sample collection, handling, transport, and storage
PublicationMetabolomics is the field of omics research that offers valuable insights into the complex composition of biological samples. It has found wide application in clinical diagnostics, disease investigation, therapy prediction, monitoring of treatment efficiency, drug discovery, or in-depth analysis of sample composition. A suitable study design constitutes the fundamental requirements to ensure robust and reliable results from the...
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Aggregation properties of some zirconium phosphate loaded with dirhenium(III) complexes
PublicationOne of the important areas of modern science is the selection of the right forms of drug delivery. Layered inorganic nanoparticles, such as zirconium phosphate, have proven themselves well in this area. The study of the properties of these systems and methods of their preparation makes it possible to determine a rational technology of their manufacture, storage conditions as well as suggest a possible mechanism of therapeutic action....
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Evaluating the antibacterial activity of muramyl dipeptide derivatives, retro-tuftsin derivatives, and anthraquinone oligopeptides against a range of pathogenic bacteria
PublicationSearch for new and efficient antibiotic is crucial because of microbial drug resistance and problems with side effects of the administered medication. In this study, we evaluate the in vitro microbiological activity of muramyl dipeptide derivatives, retro-tuftsin derivatives (i.e., tuftsin with reversed amino acid sequences), and combinations of retro-tuftsin derivatives with substituted anthraquinones. The potency of the investigated...
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In Vitro and In Vivo Imaging-Based Evaluation of Doxorubicin Anticancer Treatment in Combination with the Herbal Medicine Black Cohosh
PublicationAs a substitution for hormone replacement therapy, many breast cancer patients use black cohosh (BC) extracts in combination with doxorubicin (DOX)-based chemotherapy. In this study, we evaluated the viability and survival of BC- and DOX-treated MCF-7 cells. A preclinical model of MCF-7 xenografts was used to determine the influence of BC and DOX administration on tumor growth and metabolism. The number of apoptotic cells after...
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Predicting Value of Binding Constants of Organic Ligands to Beta-Cyclodextrin: Application of MARSplines and Descriptors Encoded in SMILES String
PublicationThe quantitative structure–activity relationship (QSPR) model was formulated to quantify values of the binding constant (lnK) of a series of ligands to beta–cyclodextrin (β-CD). For this purpose, the multivariate adaptive regression splines (MARSplines) methodology was adopted with molecular descriptors derived from the simplified molecular input line entry specification (SMILES) strings. This approach allows discovery of regression...
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Xanthone synthetic derivatives with high anticandidal activity and positive mycostatic selectivity index values
PublicationWith 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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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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Tailor-Made Polysaccharides for Biomedical Applications
PublicationPolysaccharides (PSAs) are carbohydrate-based macromolecules widely used in the biomedical field, either in their pure form or in blends/nanocomposites with other materials. The relationship between structure, properties, and functions has inspired scientists to design multifunctional PSAs for various biomedical applications by incorporating unique molecular structures and targeted bulk properties. Multiple strategies, such as...
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Methods for biomaterials printing: A short review and perspective
PublicationPrinting technologies have opened larger windows of innovation and creativity to biomaterials engineers by providing them with the ability to fabricate complex shapes in a reasonable time, cost, and weight. However, there has always been a trouble with function adjusting in printing technologies in view of the multiplicity of materials and apparatus parameters. 3D printing, also known as additive manufacturing, revolutionized biomaterials...
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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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Mitigating metal-organic framework (MOF) toxicity for biomedical applications
PublicationMetal-organic frameworks (MOFs) are a novel class of crystalline porous materials, consisting of metal ions and organic linkers. These hybrid materials are highly porous and have a large specific surface area, making them of great interest for applications in gas separation, energy storage, biomedical imaging, and drug delivery. As MOFs are being explored for biomedical applications, it is essential to comprehensively assess their...
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Antibacterial polyurethanes, modifed with cinnamaldehyde, as potential materials for fabrication of wound dressings
PublicationThe epidermis is a skin layer, which protects an organism from the different factors of external environment. Therefore, the fast and effective regeneration of epidermis is important. Potential materials used for epidermis regeneration may be polyurethane scaffolds in form of the thin permeable layers. One and main disadvantage of such polyurethane scaffolds are their lack of antibacterial and antifungal properties. The great proposition...
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Application of GC-MS/MS technique for the determination of benzodiazepines in blood samples
PublicationAbstract Benzodiazepines (BZD) are widely used as pharmaceuticals in medicine. However, due to psychostimulatory effect of BZD, in the last decade, they are more and more often used as drugs of abuse. These compounds produce similar effects to classical illicit drugs and are sold as “legal” alternatives to them as new psychoactive substances (NPS). Currently new BZD, named designer benzodiazepines (DBZD), are synthesized each year...
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Dynamics of Antimicrobial Peptide Encapsulation in Carbon Nanotubes: The Role of Hydroxylation
PublicationIntroduction: Carbon nanotubes (CNTs) have been widely employed as biomolecule carriers, but there is a need for further functionalization to broaden their therapeutic application in aqueous environments. A few reports have unraveled biomolecule–CNT interactions as a measure of response of the nanocarrier to drug-encapsulation dynamics. Methods: Herein, the dynamics of encapsulation of the antimicrobial peptide HA-FD-13 (accession...
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Morphology Regulation Mechanism and Enhancement of Photocatalytic Performance of BiOX (X = Cl, Br, I) via Mannitol-Assisted Synthesis
PublicationBiOX (X = Cl, Br, I) photocatalysts with dominant (110) facets were synthesized via a mannitol-assisted solvothermal method. This is the first report on the exposed (110) facets-, size-, and defects-controlled synthesis of BiOX achieved by solvothermal synthesis with mannitol. This polyol alcohol acted simultaneously as a solvent, capping agent, and/or soft template. The mannitol concentration on the new photocatalysts morphology...
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Presence of antibiotics in the aquatic environment in Europe and their analytical monitoring: Recent trends and perspectives
PublicationThe presence of antibiotics and their metabolites in the aquatic environment exerts a negative impact on all organisms. Moreover, the easy migration of these substances to drinking water may also have serious consequences for public health, such as drug resistance. Although antibiotics and their metabolites are detected in surface waters and wastewater, there are still no systemic solutions preventing environmental pollution with...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Consequences of New Approach of Chemical Stability Tests of Active Pharmaceutical Ingredients (APIs)
PublicationThere is a great need of broaden look on stability tests of active pharmaceuticalingredients (APIs) in comparison with current requirements contained in pharmacopeia.By usage of many modern analytical methods the conception of monitoring the changesof APIs during initial stage of their exposure to harmful factors has been developed. Newknowledge must be acquired in terms of identification of each degradation...
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Vascular stents - materials and manufacturing technologies
PublicationThe objective of this article is to present materials and technology for the manufacture of vascular stents with appropriate design requirements. The use of the right material is very important in implantology. A biomaterial introduced into the circulatory system must be biocompatible and hemocompatible. At the same time, it should not initiate toxic, mutagenic, or immunological reactions. Currently, 316L stainless steel (316L...
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Determination of the active ingredient in pharmaceutical gel formulation by NIR spectroscopy
PublicationPharmaceuticals of their intended must be thoroughly controlled. The traditional analytical methods are very costly and time consuming. NIR spectroscopy allows to analyze pharmaceutical materials very quickly and with very low costs. First pharmaceutical applications of the NIR spectroscopy appeared with some incuriosity in the late 1960s. Application of NIR in the contemporary pharmaceutical industry is very large. The most common...
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Biomarkers of alcohol consumption in body fluids - possibilities and limitations of application in toxicological analysis
PublicationEthyl alcohol is the most popular legal drug, but its excessive consumption causes social problems. Despite many public campaigns against alcohol use, car accidents, instances of aggressive behaviour, sexual assaults and deterioration in labor productivity caused by inebriated people is still commonplace. Fast and easy diagnosis of alcohol consumption is required in order to introduce proper and effective therapy, and is crucial...
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The Influence of Antitumor Unsymmetrical Bisacridines on 3D Cancer Spheroids Growth and Viability
PublicationThe culture of 3D spheroids is a promising tool in drug development and testing. Recently, we synthesized a new group of compounds, unsymmetrical bisacridines (UAs), which exhibit high cytotoxicity against various human cell lines and antitumor potency against several xenografts. Here, we describe the ability of four UAs—C-2028, C-2041, C-2045, and C-2053—to influence the growth of HCT116 and H460 spheres and the viability of HCT116...
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Permeability of the small intestinal mucus for physiologically relevant studies: Impact of mucus location and ex vivo treatment
PublicationThe small intestinal mucus is a complex colloidal system that coats the intestinal mucosa. It allows passage on nutrients/pharmaceuticals from the gut lumen towards the epithelium, whilst preventing it from direct contact with luminal microorganisms. Mucus collected from intestinal tissue is often used in studies looking at inter-mucosal transport of food particulates, drug carriers, etc. However, detaching the highly hydrated...
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Exploring the Solubility Limits of Edaravone in Neat Solvents and Binary Mixtures: Experimental and Machine Learning Study
PublicationThis study explores the edaravone solubility space encompassing both neat and binary dissolution media. Efforts were made to reveal the inherent concentration limits of common pure and mixed solvents. For this purpose, the published solubility data of the title drug were scrupulously inspected and cured, which made the dataset consistent and coherent. However, the lack of some important types of solvents in the collection called...
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Identification of novel psychoactive substances 25B-NBOMe and 4-CMC in biological material using HPLC-Q-TOF-MS and their quantification in blood using UPLC–MS/MS in case of severe intoxications
PublicationThis paper describes cases of poisoning caused by new psychoactive substances such as: 25BNBOMe (2-(4-bromo-2,5-dimethoxyphenyl)-N-[(2-methoxyphenyl)methyl]ethanamine) and 4-CMC (1-(4-chlorophenyl)-2-(methylamino)-1-propanone). The analytical procedure includes rapid and selective method for the extraction and determination of 4-CMC and 25B-NBOMe in blood samples using UPLC–MS/MS technique. To the best of our knowledge,this is...
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublicationThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublicationTelomerase plays a pivotal role in cell proliferation, homeostasis, and neoplastic transformation, making it a promising molecular target for cancer chemotherapy. Of note, although hTERT has been explored thoroughly as a target, none of the promising molecules has been approved as a drug until now. The subject of research conducted as part of my doctoral dissertation is explaining the cellular and molecular mechanism of action...
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Enzyme Conjugation - A Promising Tool for Bio-catalytic and Biotransformation Applications – A Review
PublicationEnzymes have revolutionized conventional industrial catalysts as more efficient, eco-friendly, and sustainable substitutes that can be used in different biotechnological processes, food, and pharmaceutical industries. Yet, the enzymes from nature are engineered to make them adapt and enhance their durability in the industrial environment. One promising approach involves the combined use of multiple enzymes that catalyze highly...
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Optimizing Ni–Cr patterned boron-doped diamond band electrodes: Doping effects on electrochemical efficiency and posaconazole sensing performance
PublicationThere is growing interest in developing diamond electrodes with defined geometries such as, for example, micrometer-sized electrode arrays to acquire signals for electroanalysis. For electroanalytical sensing applications, it is essential to achieve precise conductive patterns on the insulating surface. This work provides a novel approach to boron-doped diamond patterning using nichrome masking for selective seeding on an oxidized...
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In vitro biological evaluation of a novel folic acid-targeted receptor quantum dot−β−cyclodextrin carrier for C-2028 unsymmetrical bisacridine in the treatment of human lung and prostate cancers
PublicationTraditional small-molecule chemotherapeutics usually do not distinguish tumors from healthy tissues. However, nanotechnology creates nanocarriers that selectively deliver drugs to their site of action. This work is the next step in the development of the quantum dot−β−cyclodextrin−folic acid (QD−β−CD−FA) platform for targeted and selected delivery of C−2028 unsymmetrical bisacridine in cancer therapy.Herein, we report an initial...
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Nanodiamonds Doped with Manganese for Applications in Magnetic Resonance Imaging
PublicationNanodiamonds (NDs) are emerging with great potential in biomedical applications like biomarking through fluorescence and magnetic resonance imaging (MRI), targeted drug delivery, and cancer therapy. The magnetic and optical properties of NDs could be tuned by selective doping. Therefore, we report multifunctional manganese-incorporated NDs (Mn-NDs) fabricated by Mn ion implantation. The fluorescent properties of Mn-NDs were tuned...
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Virulence analysis and antibiotic resistance of Klebsiella pneumoniae isolates from hospitalised patients in Poland
PublicationKlebsiella pneumoniae (KP) is a nosocomial pathogen causing difficult-to-treat infections. The presence of virulence genes and antibiotic resistance of 109 KP isolates from hospitalized patients were investigated. Among them, 68.8% were multi-drug resistant (MDR) and 59.6% produced extended-spectrum beta-lactamases (ESBLs). Metallo-β-lactamases (MBLs) were produced by 22% of isolates (mainly from anus), including 16.5% of isolates...
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A novel in vitro assay for assessing efficacy and toxicity of antifungals using human leukaemic cells infected with Candida albicans
PublicationAims: This study describes a novel in vitro assay that simultaneously determines antifungal efficiency and host cell toxicity using suspensions of human leukaemic cells (HL-60) infected with Candida albicans. Methods and Results: The effect of Candida infection on host cell viability was evaluated by the microscopy of trypan blue-stained cells and lactate dehydrogenase (LDH) activity. The in vitro ‘drug potency assay’ utilized...
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Capillary gas chromatography using a -cyclodextrin forenantiomeric separation of methylamphetamine, its precursors andchloro intermediates after optimization of the derivatization reaction
PublicationtThe enantiomeric ratio of methylamphetamine (MAMP) is closely related to the optical activity of precur-sors and reagents used for the synthesis and this knowledge can provide useful information concerningthe origins and synthetic methods used for illicit manufacture. The information can be utilized for reg-ulation of the precursors and investigation of the manufacturing sources but this requires analyticalprocedures to determine...
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The influence of small intestinal mucus structure on particle transport ex vivo
PublicationMucus provides a barrier to bacteria and toxins while allowing nutrient absorption and waste transport. Unlike colonic mucus, small intestinal mucus structure is poorly understood. This study aimed to provide evidence for a continuous, structured mucus layer and assess the diffusion of different sized particles through it. Mucus structure was assessed by histology and immunohistochemistry. Ultra-structure was assessed by scanning...
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Application of gas chromatography–tandem mass spectrometry for the determination of amphetamine-type stimulants in blood and urine
PublicationAmphetamine, methamphetamine, phentermine, 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxymethamphetamine (MDMA), and 3,4-methylenedioxy-N-ethylamphetamine (MDEA) are the most popular amphetamine-type stimulants. The use of these substances is a serious societal problem worldwide. In this study, a method based on gas chromatography-tandem mass spectrometry (GC-MS/MS) with simple and rapid liquid-liquid extraction (LLE)...
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Antifungal Activity and Synergism with Azoles of Polish Propolis
PublicationThe aim of our work was to check if one of the products of natural origin, namely honey 19 bee propolis may be an alternative or supplement to currently used antifungal agents. The activity 20 of 50 ethanolic extracts of propolis (EEPs), harvested in Polish apiaries, was tested on a group of 69 21 clinical isolates of C. albicans. Most of the EEPs showed satisfactory activity, with minimum 22 fungicidal concentrations (MFC) mainly...
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LC-MS/MS dtermination of isoprostanes in plasma samples collected from mice exposed to doxorubicin or tert-butyl hydroperoxide
PublicationIsoprostanes are stable products of arachidonic acid peroxidation and are regarded as the most reliable markers of oxidative stress in vivo. Here we describe the LC-MS/MS procedure enabling simultaneous determination of four regioisomers (8-iso prostaglandin F2α, 8-iso-15(R)-prostaglandin F2α, 11β-prostaglandin F2α, 15(R)-prostaglandin F2α) in plasma samples collected from mice. The four plasma isoprostanes are determined by LC–ESI-MS/MS...
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Convolutional Neural Networks for C. Elegans Muscle Age Classification Using Only Self-Learned Features
PublicationNematodes Caenorhabditis elegans (C. elegans) have been used as model organisms in a wide variety of biological studies, especially those intended to obtain a better understanding of aging and age-associated diseases. This paper focuses on automating the analysis of C. elegans imagery to classify the muscle age of nematodes based on the known and well established IICBU dataset. Unlike many modern classification methods, the proposed...
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Advanced Oxidation Processes for Degradation of Water Pollutants—Ambivalent Impact of Carbonate Species: A Review
PublicationAdvanced oxidation processes (AOPs) hold great promise in the removal of organic contaminants. Reactive oxygen species (ROS) produced in AOPs react with target pollutants to initially form several intermediate compounds that finally undergo complete mineralization. Such observations are reported, especially for laboratory-scale experiments performed in pure water. On the other hand, while considering real contaminated wastewater...