Search results for: CYTOTOXICITY OF NATURAL COMPOUNDS AGAINST CANCER CELLS
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Diminshed toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
PublicationThe narrow "therapeutic window" of anti-tumour therapy may be the result of drug metabolism leading to the activation or detoxification of antitumour agents. The aim of this work is to examine (i) whether the diminished toxicity of a potent antitumour drug, C-1748, 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine, compared with its 4-demethyl analogue, C-857, results from the differences between the metabolic pathways for the...
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New clicked full agonists of the estrogen receptor β
PublicationA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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Killing kinetics analysis of C-1311 derivative with octaarginine (Compound 1-R8) against Candida albicans
Open Research DataThe datasets contain the results of killing kinetics analysis of imidazoacridinone derivative and fluconazole against C. albicans ATCC 10231. The suspensions of Candida albicans ATCC 10231 cells (500 µL) in RPMI 1640 at cell density of 104 cells /mL were added to 500 µL of RPMI 1640 medium with various concentrations of the compounds, corresponding...
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A mechanistically approached review upon assorted cell lines stimulated by athermal electromagnetic irradiation
PublicationThe probable influence of electromagnetic irradiation on cancer treatment has been deduced from the interaction of artificial electromagnetic emissions with biological organisms. Nonetheless, the suspected health effects induced by electromagnetic-based technology imply that such a treatment may contaminate the adjacent healthy cells. Thus, gaining mechanistic insights into the problem is required to avoid athermal health hazards....
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublicationHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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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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Effect of package type on selected parameters of nutritional quality of chill-stored white sauerkraut
PublicationBrassica vegetables, including white cabbage, both fresh and sour (Brassica oleracea L. var. capitata L.), contain a lot of valuable metabolites which are effective in chemoprevention of cancer as documented by numerous studies. This work investigates the effect of different packaging types; low density polyethylene (PE-LD) and metalized polyethylene terephthalate (PET met/PE) with polyethylene bags on selected quality parameters in...
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Aminy w środowisku - niebezpieczeństwo czy jego naturalny element?
PublicationA lot of amines and their compounds are used in the industry. First of all they are used for the preparation of medicines, plant protection agents, fertilizers and plastics. Amines are also released into the environment as a result of natural biological processes such as the release of certain species of flowers to lure insects, and also biochemical breakdown of amino acids in the protein during decomposition of organic matter. Unfortunately,...
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Asfalteny jako fazy stacjonarne w chromatografii cieczowej w normalnych układach faz
PublicationRozprawa doktorska dotyczy zbadania możliwości wykorzystania asfaltenów wydzielonych z: próżniowej pozostałości ropy naftowej, produktów jej utleniania i naturalnego asfaltu jako fazy stacjonarnej na powierzchni sorpcyjnej żelu krzemionkowego do rozdzielania nisko polarnych organicznych związków chemicznych w warunkach chromatografii cieczowej w normalnych układach faz, w odniesieniu do żelu krzemionkowego jako nośnika. Opracowano...
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Higher platelet counts correlate to tumour progression and can be induced by intratumoural stroma in non-metastatic breast carcinomas
PublicationBackground Platelets support tumour progression. However, their prognostic significance and relation to circulating tumour cells (CTCs) in operable breast cancer (BrCa) are still scarcely known and, thus, merit further investigation. Methods Preoperative platelet counts (PCs) were compared with clinical data, CTCs, 65 serum cytokines and 770 immune-related transcripts obtained using the NanoString technology. Results High normal...
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublicationNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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Rhodotorulic Acid and its Derivatives: Synthesis, Properties, and Applications
PublicationSiderophores are low molecular weight compounds produced by microorganisms to scavenge iron in iron-deficient environments. Rhodotorulic acid, a natural hydroxamate siderophore, plays a vital role in iron acquisition for fungi and bacteria. As the simplest natural hydroxamate siderophore, it exhibits a high affinity for ferric ions, enabling it to form stable complexes that facilitate iron uptake and transport within microorganisms....
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Triazoloacridone C-1305 impairs XBP1 splicing by acting as a potential IRE1α endoribonuclease inhibitor
PublicationInositol requiring enzyme 1 alpha (IRE1α) is one of three signaling sensors in the unfolding protein response (UPR) that alleviates endoplasmic reticulum (ER) stress in cells and functions to promote cell survival. During conditions of irrevocable stress, proapoptotic gene expression is induced to promote cell death. One of the three signaling stressors, IRE1α is an serine/threonine-protein kinase/endoribonuclease (RNase) that...
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
PublicationPyrazine and its derivatives are a large group of compounds that exhibit broad biological activity, the changes of which can be easily detected by a substituent effect or a change in the functional group. The present studies combined theoretical research with the density functional theory (DFT) approach (B3LYP/6-311+G**) and experimental (potentiometric and spectrophotometric) analysis for a thorough understanding of the structure...
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The Concept of Construction of Hybrid Constructed Wetland for Wastewater Treatment in Roztocze National Park
PublicationRoztocze National Park (RNP) is one of 23 national parks in Poland. It was created in 1974 both to protect the natural and cultural heritage as well as to share the park area for science, education and tourism. In caring for the environment, the park removed asbestos coverage, performs thermo-modernization using renewable energy sources by the installation of solar panels and photovoltaic cells on the roofs of buildings, and pellet...
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Phytoecdysteroid containing plants – a source of bioactive compounds with potential anticarcinogenic effects
PublicationEcdysteroids are a group of steroids synthesized in inver- tebrates as molting hormones and also in some plants as secondary metabolites acting as a defense against parasites. These compounds do not naturally occur in mammals and are not structurally related to mammalian steroid hor- mones, consequently do not activate mammalian hormone receptors. Ecdysteroids exhibit very low toxicity to mam- mals and to date no serious side effects...
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The influence of selenium addition during germination of Brassica seeds on health-promoting potential of sprouts
PublicationThe correlation among selenium uptake, the content of bioactive compounds in sprouts, and biological activities triggered in cultured human cells by sprout extracts was investigated. Seeds of Brassica crops and rye were treated with SeO2 water solution. The selenium levels in sprouts increased from 1.0-4.1 to 53.3-382 μg/g dw with no influence on plant physiology according to the indices used. Neither the composition of glucosinolates...
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Chemical Quality of Bottled Waters: A Review
PublicationBottled water has become very popular for quenching thirst and as a dietary (mineral) supplement. Theplethora of natural mineral waters precludes any unequivocal system of classification, which makes it difficult for theconsumer to choose a water with properties that suits him/her exactly. The ever-increasing popularity of bottled watersmeans that it is of the utmost importance to determine not only their mineral content, but above...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal PNT1A cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal PNT1A cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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Synthesis, Molecular Structure, Metabolic Stability and QSAR Studies of a Novel Series of Anticancer N-Acylbenzenesulfonamides
PublicationA series of novel N-acyl-4-chloro-5-methyl-2-(R1-methylthio)benzenesulfonamides 18–47 have been synthesized by the reaction of N-[4-chloro-5-methyl-2-(R1-methylthio) benzenesulfonyl]cyanamide potassium salts with appropriate carboxylic acids. Some of them showed anticancer activity toward the human cancer cell lines MCF-7, HCT-116 and HeLa, with the growth percentages (GPs) in the range from 7% to 46%. Quantitative structure-activity relationship...
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Metals and metal-binding ligands in wine: Analytical challenges in identification.
PublicationBackground Due to important role of metals in the vinification process as well as their impact on the human health, their content in this alcoholic beverage has been extensively studied by many researchers. It is already known that speciation of metals determines their toxicity and bioavailability as well as influences their activity. Understanding the chemistry and knowing the structures of metal complexes could have relevant...
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Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation.
PublicationThe effectiveness of many anticancer drugs depends on the creation of specific metabolites that may alter their therapeutic or toxic properties. One significant route of biotransformation is a conjugation of electrophilic compounds with reduced glutathione, which can be non-enzymatic and/or catalyzed by glutathione-dependent enzymes. Glutathione usually combines with anticancer drugs and/or their metabolites to form more polar...
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Small Polymeric Toys Placed in Child-Dedicated Chocolate Food Products—Do They Contain Harmful Chemicals? Examination of Quality by Example of Selected VOCs and SVOCs
PublicationThis study was focused on child-dedicated chocolate food products that contain a plastic package with a small toy inside (also known as chocolate eggs). Three types of these products that are commercially available on the Polish market, with different prices, chocolate composition, and main types of polymers used in the toy manufacturing process, were investigated. The polymers were identified using Fourier-transform infrared (FT-IR)...
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Poloxamer: A versatile tri-block copolymer for biomedical applications
PublicationPoloxamers, also called Pluronic, belong to a unique class of synthetic tri-block copolymers containing central hydrophobic chains of poly(propylene oxide) sandwiched between two hydrophilic chains of poly(ethylene oxide). Some chemical characteristics of poloxamers such as temperature-dependent self-assembly and thermo-reversible behavior along with biocompatibility and physiochemical properties make poloxamer-based biomaterials...
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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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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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SrCe0.9In0.1O3-δ-based reversible symmetrical Protonic Ceramic Cell
PublicationIn-doped SrCe0.9In0.1O3-δ (SCI) perovskite-type oxide is utilized as the solid electrolyte, as well as a component, together with SrFe0.75Mo0.25O3-δ (SFM) compound, in the composite-type electrodes to construct symmetrical Protonic Ceramic Fuel Cells (PCFC). With good mutual stability of SCI and SFM at high temperatures in water vapor-containing reducing and oxidizing conditions, as well as sufficient ionic conductivity with high...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal MRC-5 cells
Open Research DataThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal MRC-5 cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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Selected anionic and cationic surface active agents determined in river sediments – the Klodnica catchment
PublicationSurface active agents (SAAs) are specific compounds that contain hydrophilic/ hydrophobic group in their molecules named as amphiphilic structures. According to charge on the hydrophilic part of surfactants they can be classified into three main groups: anionic, cationic and non-ionic compounds. Due to the amphiphilic structure of SAAs they have specific properties (e.g. ability to adsorption at different surfaces, reduction of...
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Invasive breast carcinoma of no special type - Female, 68 - Tissue image [7100730013391331]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 68 - Tissue image [7100730013397491]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 68 - Tissue image [7100730013391341]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 68 - Tissue image [7100730013393011]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 68 - Tissue image [710073001339961]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Invasive breast carcinoma of no special type - Female, 68 - Tissue image [7100730013393191]
Open Research DataThis is the histopathological image of BREAST tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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The potential of LC–MS technique in direct analysis of perfume content
PublicationPerfumes are products that consist of a wide range of natural and synthetic compounds. Due to complex composition, the determination of their ingredients is a difficult task. Most of the perfume components are either volatile or semi-volatile; however, most of the attention has been paid to volatile ones, and thus, gas chromatography or electronic noses are generally used. Nevertheless, in this study, liquid chromatography coupled...
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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Application of deep eutectic solvents (DES) in analytical chemistry
PublicationRecent years have been associated with efforts to reduce the impact on the natural environment. A greener approach has been introduced in various areas of science, including analytical chemistry. One of the basic procedures for preparing a sample for analysis is its extraction. Traditional methods involve the use of large amounts of organic compounds, often toxic, with an unfavorable impact on the environment. A representative...
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Cyanides in the environment—analysis—problems and challenges
PublicationCyanide toxicity and their environmental impact are well known. Nevertheless, they are still used in the mining, galvanic and chemical industries. As a result of industrial activities, cyanides are released in various forms to all elements of the environment. In a natural environment, cyanide exists as cyanogenic glycosides in plants seeds. Too much consumption can cause unpleasant side effects. However, environmental tobacco smoke...
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Data regarding a new, vector-enzymatic DNA fragment amplification-expression technology for the construction of artificial, concatemeric DNA, RNA and proteins, as well as biological effects of selected polypeptides obtained using this method
PublicationApplications of bioactive peptides and polypeptides are emerging in areas such as drug development and drug delivery systems. These compounds are bioactive, biocompatible and represent a wide range of chemical properties, enabling further adjustments of obtained biomaterials. However, delivering large quantities of peptide derivatives is still challenging. Several methods have been developed for the production of concatemers –...
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Phytoplankton communities of polar regions–Diversity depending on environmental conditions and chemical anthropopressure
PublicationThe polar regions (Arctic and Antarctic) constitute up to 14% of the biosphere and offer some of the coldest and most arid Earth's environments. Nevertheless several oxygenic phototrophs including some higher plants, mosses, lichens, various algal groups and cyanobacteria, survive that harsh climate and create the base of the trophic relationships in fragile ecosystems of polar environments. Ecosystems in polar regions are characterized...
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Similarities and differences in d6 low-spin ruthenium, rhodium and iridium half-sandwich complexes: synthesis, structure, cytotoxicity and interaction with biological targets
PublicationIn this paper, we discussed the similarities and diferences in d6 low-spin half-sandwich ruthenium, rhodium and iridium complexes containing 2,2′-biimidazole (H2biim). Three new complexes, {[RuCl(H2biim)(η6 -p-cymene)]PF6}2·H2O (1), [(η5 - Cp)RhCl(H2biim)]PF6 (2), and [(η5 -Cp)IrCl(H2biim)]PF6 (3), were fully characterized by CHN, X-ray difraction analysis, UV–Vis, FTIR, and 1 H, 13C and 15N NMR spectroscopies. The complexes exhibit...
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The Influence of Iron Doping on Performance of SrTi1-XFexO3-δ Perovskite Oxygen Electrode for SOFC
PublicationSolid Oxide Fuel Cells (SOFC) are based on electrolytes and mixed ionic and electronic conductivity (MIEC) materials. The need to reduce costs causes an increase in interest of new compounds suitable for operating temperatures between 600 °C and 800 °C. The SrTi1-xFexO3 (STF) perovskite material is a perspective material that could be used for the oxygen electrodes. In this work STF materials with different content of iron (x =...
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Inhibition of Polymer Photodegradation by Incorporation of Coffee Silverskin
PublicationOver the last years, the trend associated with the incorporation of materials from renewable resources into polymer technology is getting significantly more vital. Researchers are trying to transfer the properties of natural raw materials into the polymer world. Therefore, different natural materials are more often investigated as potential additives for polymers. Such an effect is noted for the coffee industry by-products, such...
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Membrane technologies assisting plant-based and agro-food by-products processing: A comprehensive review
PublicationBackground Nowadays, membrane-based technologies (e.g. microfiltration, ultrafiltration, nanofiltration, membrane distillation, and pervaporation) have demonstrated to meet the requirements to be involved in different food and bioproduct processes. Scope and approach Several applications have been developed, including either separation, recovery or concentration of bioactive molecules from agro-food products and by-products,...
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Use of Brassica plants in the phytoremediation and biofumigation processes
PublicationIn recent decades, serious contamination of soils by heavy metals has been reported. It is therefore a matter of urgency to develop a new and efficient technology for removing contaminants from soil. Another aspect to this problem is that environmental pollution decreases the biological quality of soil, which is why pesticides and fertilizers are being used in ever-larger quantities. The environmentally friendly solutions to these...
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Saccharides
PublicationSaccharides are widely distributed in nature as the major component of fruits and vegetables (primarily monosaccharides), milk and malt (mainly disaccharides), and grains (mostly polysaccharides). They are an important source of energy, structural material, as well as flavor and taste factors. Molecules of this class of compounds contain mainly carbon, hydrogen, and oxygen atoms; however, most natural saccha- rides do not have...
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IZOLACJA I IDENTYFIKACJA NATURALNYCH SUBSTANCJI BARWIĄCYCH OBECNYCH W PRÓBKACH FARB ARTYSTYCZNYCH I TKANINACH POCHODZENIA HISTORYCZNEGO
PublicationNatural organic dyes are group of substances that belong to various types of chemical compounds. The most commonly used in paintings and dyeing textiles were naturally occurring dyestuffs from group of anthraquinones, flavones and indigoid dyes. Identification of coloring substances present in historical artistic paints provides relevant information for a wide range of specialists dealing with works of art and in the field of conservation science....
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Relationship between the betalain composition in Opuntia ficus indica and Beta vulgaris varieties and biological activity of their extracts
PublicationBetalains are a class of pigments that are much less com- monly found in nature than anthocyanins or carotenoids. They occur only in a few edible plants such as red beetroot (Beta vulgaris), prickly pears (Opuntia ficus indica), amaranth (Amaranthus sp.) and some mushrooms. This group of pig- ments can be divided into two major groups: yellow vulgax- anthins and red betanins. Despite their structural similarity to compounds from...