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Search results for: Pharmaceutical%20cocrystals
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QSRR Evaluation of the New Anticancer Sulfonamides in View of the cis-trans Isomerism
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Biological Activity of Compounds Exhibiting Local Anesthetics's Properties Evaluated by QSAR Approach
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Function and Frustration of Multi-Drug ABC Exporter Protein and Design of Model Proteins for Drug Delivery Using Protein Hydration Thermodynamics
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Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
PublicationEstrogen is one of the most important signaling molecules which targets a number of genes. Estrogen levels regulate cell proliferation and a plethora of metabolic processes, which may interfere with a range of medical conditions and drug metabolism. The MCF7 breast cancer cell line, expressing the estrogen receptor α, is a well-studied model of cellular answer to estrogen. The aim of this study was to characterize transcriptomic...
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Effect of Glycemic Disorders and Habits on the Concentration of Selected Neurotrophic Factors in Patients with Lumbosacral Intervertebral Disc Degeneration
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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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Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublicationUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
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Electrochemical and in silico approaches for liver metabolic oxidation of antitumor-active triazoloacridinone C -1305
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) is a promising antitumor compound developed in our laboratory. A better understanding of its metabolic transformations is still needed to explain the multidirectional mechanism of pharmacological action of triazoloacridinone derivatives at all. Thus, the aim of the current work was to predict oxidative pathways of C-1305 that would reflect its phase I metabolism. The...
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Prophylaxis of Non-communicable Diseases: Why Fruits and Vegetables may be Better Chemopreventive Agents than Dietary Supplements Based on Isolated Phytochemicals?
PublicationThe World Health Organization (WHO) report from 2014 documented that non-communicable socalled civilization diseases such as cardiovascular disease, chronic respiratory diseases, cancer or type 2 diabetes are responsible for over 50% of all premature deaths in the world. Research carried out over the past 20 years has provided data suggesting that diet is an essential factor influencing the risk of development of these diseases....
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Chemical Aspects of Biological Activity of Isothiocyanates and Indoles, the Products of Glucosinolate Decomposition
PublicationThere is growing evidence that cancer chemoprevention employing natural, bioactive compounds may halt or at least slow down the different stages of carcinogenesis. A particularly advantageous effect is attributed to derivatives of sulfur-organic phytochemicals, such as glucosinolates (GLs) synthesized mainly in Brassicaceae plant family. GLs are hydrolysed enzymatically to bioactive isothiocyanates (ITC) and indoles, which exhibit strong...
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The Role of FLT3 Kinase as an AML Therapy Target
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pH-Induced modification to stratum corneum lipids investigated using thermal, spectroscopic, and chromatographic techniques
PublicationZbadano jakim zmianom jakościowym i ilościowym ulegają indywidualne klasy lipidów w Stratum Corneum (tkanka rogowa skóry) pod wpływem środowiska o zmiennym pH.
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Methods for Elucidation of DNA-Anticancer Drug Interactions and Their Applications in the Development of New Drugs
PublicationDNA damaging agents including anthracyclines, camptothecins and platinum drugs are among most frequently used drugs in the chemotherapeutic routine. Due to their relatively low selectivity for cancer cells, administration is associated with adverse side effects, whereas the inherent genotoxicity of these drugs is associated with risk of developing secondary cancers. Development of new drugs, which could be spared of these drawbacks...
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Experimental and theoretical studies on the Sulfamethazine-Urea and Sulfamethizole-Urea solid-liquid equilibria
PublicationThe miscibility of active pharmaceutical ingredients with excipients is an important aspect in pharmaceutical technology protocols. In this study, the differential scanning calorimetry (DSC) was used for Sulfamethazine-Urea (SI–U) and Sulfamethizole-Urea (SO–U) solid-liquid phase diagrams determination. Both sulfonamides form simple binary eutectics with Urea. The lack of new co-crystal phase formation was confirmed by inspection...
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Efficient three-dimensional fluorescence measurements for characterization of binding properties in some plants
PublicationThe main aim of this research was to characterize some plants and to determine their similarities and differences, using spectroscopic methods. The interactions of soluble polyphenols of different plants with human serum albumin (HSA) were investigated by 3D-fluorescence. The obtained fluorescence results allow to classify the investigated plants according to their binding properties. The HSA-binding capacities of these plants...
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Thermally activated persulfate-based Advanced Oxidation Processes — recent progress and challenges in mineralization of persistent organic chemicals: a review
PublicationThermally activated persulfate (TAP) finds application in Advanced Oxidation Processes for the removal of pollutants from contaminated water and soil. This paper reviewed the various cases of TAP in the environmental remediation. The pollutants such as individual pharmaceuticals, biocides, cyclic organic compounds, and dyes are considered in this review. It is interesting to note that most of the organic compounds undergo complete...
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Structural Characterization and in Vivo Evaluation of β-Hairpin Peptidomimetics as Specific CXCR4 Imaging Agents
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Reversed-Phase TLC and HPLC Retention Data in Correlation Studies with in Silico Molecular Descriptors and Druglikeness Properties of Newly Synthesized Anticonvulsant Succinimide Derivatives
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Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)
PublicationThe aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA−PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro...
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Microemulsion Delivery Systems with Low Surfactant Concentrations: Optimization of Structure and Properties by Glycol Cosurfactants
PublicationExtensive use of microemulsions as delivery systems raises interest in the safe ingredients that can form such systems. Here, we assessed the use of two glycols, i.e., propylene glycol and pentylene glycol, and their mixtures to manipulate the properties and structure of microemulsions. Obtained systems with glycols were extensively characterized in terms of capacity to incorporate water phase, droplet size, polydispersity, structure...
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99mTc-Galacto-RGD2: A Novel 99mTc-Labeled Cyclic RGD Peptide Dimer Useful for Tumor Imaging
PublicationThis study sought to evaluate [99mTc(HYNIC-Galacto-RGD2)-(tricine)(TPPTS)] (99mTc-Galacto-RGD2: HYNIC = 6-hydrazinonicotinyl; Galacto-RGD2 = Glu[cyclo[Arg-Gly-Asp-D-Phe-Lys(SAA-PEG2-(1,2,3-triazole)-1-yl-4-ethylamide)]]2 (SAA = 7-amino-L-glycero-L-galacto-2,6-anhydro-7-eoxyheptanamide, and PEG2 = 3,6-dioxaoctanoic acid); and TPPTS = trisodium triphenylphosphine-3,3',3''-trisulfonate) as a new radiotracer for tumor imaging. Galacto-RGD2...
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Mechanism of Binding of Antifungal Antibiotic Amphotericin B to Lipid Membranes: An Insight from Combined Single-Membrane Imaging, Microspectroscopy, and Molecular Dynamics
PublicationAmphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design safer derivatives. As the drug primarily targets the biomembranes of both fungi and humans, new insights into the...
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Stability and phase transition investigation of olanzapine polymorphs
PublicationWe use electrical embedded-fragment QM method with both DFT/ωB97XD/6-31G* and MP2/6-31G* to investigate the phase transformations of olanzapine. Gibbs free energy calculations predict that form I is always the most stable structure and form II is the least stable one, while form IV is more stable than form III below about 200 K but less stable above this temperature, implying a polymorphic phase transformation. This may account...
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NADZOROWANIE WYPOSAŻENIA DO MONITOROWANIA I POMIARÓW WEDŁUG WYMAGAŃ WYBRANYCH NORM ORAZ PRZEPISÓW PRAWNYCH
Publication: Przyrządy pomiarowe stanowią zasadniczy element złożonego systemu oceny jakości wyrobów na wszystkich etapach produkcji. Odpowiednio zaprojektowane procedury opisujące procesy kontrolne i pomiarowe, sprawnie zorganizowane i przeprowadzane operacje monitorowania i pomiarów parametrów procesów i produktów oraz skutecznie funkcjonujący nadzór nad wyposażeniem do monitorowania i pomiarów w organizacji są podstawą do wykazania, że...
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Characterization of metabolites in different kiwifruit varieties by NMR and fluorescence spectroscopy
PublicationIt is known from our previous studies that kiwifruits, which are used in common human diet, have preventive properties of coronary artery disease. This study describes a combination of 1H NMR spectroscopy, multivariate data analyses and fluorescence measurements in differentiating of some kiwifruit varieties, their quenching and antioxidant properties. A total of 41 metabolites were identified by comparing with literature data...
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Latest Insights on Novel Deep Eutectic Solvents (DES) for Sustainable Extraction of Phenolic Compounds from Natural Sources
PublicationPhenolic compounds have long been of great importance in the pharmaceutical, food, and cosmetic industries. Unfortunately, conventional extraction procedures have a high cost and are time consuming, and the solvents used can represent a safety risk for operators, consumers, and the environment. Deep eutectic solvents (DESs) are green alternatives for extraction processes, given their low or non-toxicity, biodegradability, and reusability....
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Modern trends in solid phase extraction: New sorbent media
PublicationBased on the recently published literature, this review provides an update of the most important features and application of formats and devices employed in solid phase extraction (SPE). Special attention was paid on new trapping media proposed in SPE prior the chromatography analysis, based on the use of nanostructured materials, including carbon nanomaterials, electrospun nanofibers, dendrimes and magnetic nanoparticles, molecular...
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Monosubstituted hydrazone β-cyclodextrin derivatives for pH-sensitive complex formation with aromatic drugs
PublicationA new and convenient synthetic pathway was developed to produce monosubstituted cyclodextrins with high yields. Each of the β-cyclodextrin derivatives described in this work has an aromatic substituent connected with cyclodextrin core by a pH-sensitive hydrazone linker and a carbon chain. Carbon chains differ in lengths having one or three carbon atoms. The correlation between water solubility and linker length was determined using...
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Modern solutions in the field of microextraction using liquid as a medium of extraction
PublicationThe monitoring of compounds present in samples at trace/ultra-trace level usually requires a preliminary step of isolation and/or enrichment of analytes. Against, sample preparation is considered as crucial part of whole analytical procedures, in particular in samples characterized by complex matrices composition. Several new miniaturized extraction techniques is introduced and extensively applied to different type of samples....
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COMPOSITION OF BIOACTIVE SECONDARY METABOLITES AND MUTAGENICITY OF SAMBUCUS NIGRA L. FRUIT AT DIFFERENT STAGES OF RIPENESS
PublicationThe relationship between the content of bioactive compounds and mutagenic activity of elderberry fruit at different stages of ripeness was investigated. Signifi cant differences in the antioxidant profi les (TLC, HPLC with post-column derivatization) and antioxidant activity (ABTS, DPPH, and FC tests) were observed for studied elderberry extracts. The more ripen the fruit at the time of harvest were, the higher the content of...
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Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions
PublicationBackground. Dapsone (DAP) is an anti-inflammatory and antimicrobial active pharmaceutical ingredient used to treat, e.g., AIDS-related diseases. However, low solubility is a feature hampering its efficient use. Objectives. First, deep eutectic solvents...
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Long-Term Stability of Benzodiazepines and Z-Hypnotic Drugs in Blood Samples Stored at Varying Temperatures
PublicationBenzodiazepines (BZDs) and Z-drugs are among the most commonly prescribed pharmaceuticals in the world and are considered standard care for various mental illnesses and for treatment of sleeping and anxiety disorders, alcohol withdrawal, muscle spasms and epilepsy. Some BZDs are not allowed as pharmaceuticals in many countries, and they are used as "designer benzodiazepines" (DBZDs). All these compounds are typically screened in...
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The effect of morphology and crystalline structure of Mo/MoO3 layers on photocatalytic degradation of water organic pollutants
PublicationMolybdenum oxide layers were formed by anodization of the Mo metallic foil in a water/ethylene glycol-based electrolyte containing fluoride ions. The as-prepared, amorphous samples were annealed in air at different temperatures in a range from 100 �C to 700 �C. The crystal phase and morphology of anodized and annealed MoO3 layers were investigated using X-ray diffraction, Raman spectroscopy, and scanning electron microscopy. The...
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Nanoparticles: Synthesis, characteristics, and applications in analytical and other sciences
PublicationNanoparticles (NPs) are widely employed in different research areas, ranging from analytical chemistry and environmental science to medicine, the agriculture and pharmaceutical industry. This is mainly due to the unique characteristics of NPs and the novelty they introduce in such applications. In analytical chemistry, the role of NPs can differ depending on the nature of the steps involved in analytical process. NPs are probably...
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Environmentally Oriented Models and Methods for the Evaluation of Drug x Drug Interaction Effects
PublicationThis detailed review compares known and widely used methods for drug interaction estimation, some of which now have historical significance. Pharmaceutical application has been noted as far back as several thousand years ago. Relatively late in the 20th century, however, researchers became aware that their fate and metabolism, which still remain a great challenge for environmental analysts and risk assessors. For the patient’s...
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The determination of elements in herbal teas and medicinal plant formulations and their tisanes
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Understanding element composition of medicinal plants used in herbalism—A case study by analytical atomic spectrometry
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Structure–bioavailability relationship study of genistein derivatives with antiproliferative activity on human cancer cell
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Silylation of acetaminophen by trifluoroacetamide-based silylation agents
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A new pH/organic modifier gradient RP HPLC method for convenient determination of lipophilicity and acidity of drugs as applied to established imidazoline agents
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Quantitative structure-(chromatographic) retention relationship models for dissociating compounds
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Combined pH/organic solvent gradient HPLC in analysis of forensic material
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Ocular irritation and cyclosporine A distribution in the eye tissues after administration of Solid Lipid Microparticles in the rabbit model
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New sorbent materials for selective extraction of cocaine and benzoylecgonine from human urine samples
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In honor of the 70th birthday of Professor Roman Kaliszan
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Combined computational-experimental approach to predict blood–brain barrier (BBB) permeation based on “green” salting-out thin layer chromatography supported by simple molecular descriptors
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The metabolic profiles of pterin compounds as potential biomarkers of bladder cancer—Integration of analytical-based approach with biostatistical methodology
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Determination of pterins in urine by HPLC with UV and fluorescent detection using different types of chromatographic stationary phases (HILIC, RP C8, RP C18)
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Simultaneous determination of creatinine and acetate by capillary electrophoresis with contactless conductivity detector as a feasible approach for urinary tract infection diagnosis
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