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Search results for: Cell-Penetrating Peptide
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Synthesis of analogues of anthraquinones linked to tuftsin or retro-tuftsin residues as potential topoisomerase inhibitors
PublicationZsyntetyzowano 10 nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny jako potencjalne inhibitory topoizomerazy. Substratem wyjściowym były zsyntetyzowane 1,4-, 1,5- i 1,8-bis(tosyloksy)-9,10-antrachinony oraz odpowiednio chronione pochodne tuftsyny i retro-tuftsyny, które otrzymano metodą mieszanych bezwodników z zastosowaniem chloromrówczanu izobutylu i NMM. Reakcje prowadzone były w acetonitrylu pod azotem w...
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The immunological properties, cytotoxic effect and antimicrobial activities of novel analogues of edeine antibiotics
PublicationOpisano syntezę kilku nowych analogów edein a i d z zastosowaniem klasycznych metod syntezy peptydów w roztworze oraz przedstawiono wyniki badań cytotoksycznych na kilku liniach komórek ludzkich oraz wyniki badań mikrobiologicznych w stosunku do bakterii gramododatnich i gramoujemnych. Opisano również wyniki badań immunologicznych na modelu myszy.
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Synthesis of anthraquinone-tuftsin analogues as potential topoisomerase inhibitors
PublicationZaprezentowano syntezę nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny oraz wstępne badania biologiczne (aktywność cytotoksyczną na wybranych liniach nowotworowych oraz zdolność hamowania topoizomerazy I).
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Synthesis of conjugates of Combretastatin A-4 with tuftsin derivatives as potential anticancer agents
PublicationZaprezentowano syntezę nowych koniugatów Combretastatyny A-4 z pochodnymi tuftsyny i retro-tuftsyny, jako potencjalnych związków przeciwnowotworowych.
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Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G
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Pegylated Fluorescent Peptides as Substrates of Proteolytic Enzymes
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Design of serine proteinase inhibitors by combinatorial chemistry using trypsin inhibitor SFTI‐1 as a starting structure
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Designing of Substrates and Inhibitors of Bovine α-Chymotrypsin with Synthetic Phenylalanine Analogues in Position P1
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Theoretical conformational analysis of six arginine vasopressin analogs with the l -naphthylalanine in position 3
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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Molecular dynamics simulation of human neurohypophyseal hormone receptors complexed with oxytocin—modeling of an activated state
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Analysis of interactions responsible for vasopressin binding to human neurohypophyseal hormone receptors—molecular dynamics study of the activated receptor–vasopressin–Gα systems
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Chemical modification of natural immunomodulators tuftsin and muramyl dipeptide significantly influence their biological activity
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Conjugates of tuftsin and muramyl dipeptide as stimulators of monocyte-derived dendritic cells
PublicationOstatnio coraz częściej bada się związki oddziałujące na komórki dendrytyczne. Muramylodipeptyd i jego analogi przyspieszają dojrzewanie i aktywację komórek dendrytycznych. Do naszych badań otrzymaliśmy komórki dendrytyczne na drodze ekspansji z monocytów krwi obwodowej. Właściwa suplementacja hodowli monocytów czynnikami wzrostowymi - GM-CSF i IL-4, pozwoliła na uzyskanie niedojrzałych komórek dendrytycznych, które stymulowano...
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Conformational latitude – activity relationship of KPPR tetrapeptide analogues toward their ability to inhibit binding of vascular endothelial growth factor 165 to neuropilin‐1
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Oligopeptide antifungals are exceptionally active against multidrug-resistant yeast
PublicationPermeazy peptydowe w komórkach drożdżowych są zdolne do transportu do wnętrza komórek oligopeptydów, zawierających w swojej strukturze niebiałkowe aminokwasy o właściwościach przeciwgrzybowych. Wśród szerokiego wachlarza tego rodzaju związków przebadanych pod względem aktywności biologicznej na wielolekoopornych komórkach drożdżowych, zaobserwowano liczna grupę, wykazującą zwiększoną aktywność względem komórek eksprymujących transportery...
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Structure-activity relationship studies on the antimicrobial activity of novel edeine a and d analogues
PublicationOpisano syntezę 4 nowych analogów peptydowego antybiotyku, edeiny a i d z wykorzystaniem klasycznej syntezy w roztworze. Stosowano metodę estrów aktywnych oraz metodę azydową do tworzenia wiązań peptydowych. Zbadano także aktywność przeciwgrzybową i przeciwbakteryjną opisanych połączeń.
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublicationThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Transport deficiency is the molecular basis of Candida albicans resistance to antifungal oligopeptides
Publication(FMDP), an inhibitor of glucosamine-6-phosphate synthase, exhibited growth inhibitory activity against Candida albicans, with minimal inhibitory concentration values in the 0.05–50 mg/L range. Uptake by the peptide permeases was found to be the main factor limiting an anticandidal activity of these compounds. Di- and tripeptide containing FMDP (F2 and F3) were transported by Ptr2p/Ptr22p peptide transporters (PTR) and FMDP-containing...
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The influence of synthesis method on the microstructure and catalytic performance of Y 0.07 Sr 0.93 Ti 0.8 Fe 0.2 O 3-δ in synthetic biogas operated solid oxide fuel cells
PublicationThe Y0.07Sr0.93Ti0.8Fe0.2O3-δ (YSTF) material was fabricated using three different synthesis methods: modified polymer precursor method (MPP), Pechini method and a solid state reaction method. It was applied as an anode catalytic material for biogas reforming in solid oxide fuel cells. Clear differences in the microstructure of fabricated catalytic layers were found, mainly with respect to a grain size and distribution of grains....
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Performance and Stability in H2S of SrFe0.75Mo0.25O3-δ as Electrode in Proton Ceramic Fuel Cells
PublicationThe H2S-tolerance of SrFe0.75Mo0.25O3-δ (SFM) electrodes has been investigated in symmetric proton ceramic fuel cells (PCFC) with BaZr0.8Ce0.1Y0.1O3-δ (BZCY81) electrolyte. The ionic conductivity of the electrolyte under wet reducing conditions was found to be insignificantly affected in the presence of up to 5000 ppm H2S. The fuel cell exhibited an OCV of about 0.9 V at 700 °C, which dropped to about 0.6 V and 0.4 V upon exposure...
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The imidazoacridinone C-1311 induces p53-dependent senescence or p53-independent apoptosis and sensitizes cancer cells to radiation
PublicationC-1311 is a small molecule, which has shown promise in a number of preclinical and clinical studies. However, the biological response to C-1311 exposure is complicated and has been reported to involve a number of cell fates. Here, we investigated the molecular signaling which determines the response to C-1311 in both cancer and non-cancer cell lines. For the first time we demonstrate that the tumor suppressor, p53 plays a key role...
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H2AX phosphorylation, its role in DNA damage response and cancer therapy
PublicationDouble-strand breaks (DSBs) are the most deleterious DNA lesions, which, if left unrepaired, may have severe consequences for cell survival, as they lead to chromosome aberrations, genomic instability, or cell death. Various physical, chemical, and biological factors are involved in DSB induction. Cells respond to DNA damage by activating the so-called DNA damage response (DDR), a complex molecular mechanism developed to detect...
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High-performance anode-supported solid oxide fuel cells with co-fired Sm0.2Ce0.8O2-δ/La0.8Sr0.2Ga0.8Mg0.2O3−δ/Sm0.2Ce0.8O2-δ sandwiched electrolyte
PublicationIn this study, intermediate-temperature solid oxide fuel cells (IT-SOFCs) with a nine-layer structure are constructed via a simple method based on the cost-effective tape casting-screen printing-co-firing process with the structure composed of a NiO-based four-layer anode, a Sm0.2Ce0·8O2-δ(SDC)/La0·8Sr0.2Ga0.8Mg0·2O3−δ (LSGM)/SDC tri-layer electrolyte, and an La0·6Sr0·4Co0·2Fe0·8O3-δ (LSCF)-based bi-layer cathode. The resultant...
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Optimization of the Relative Humidity of Reactant Gases in Hydrogen Fuel Cells Using Dynamic Impedance Measurements
PublicationWater management is a key factor affecting the efficiency of proton exchange membrane fuel cells (PEMFCs). The currently used monitoring methods of PEMFCs provide limited information about which processes or components that humidity has a significant impact upon. Herein, we propose the use of a novel approach of impedance measurements using a multi-sinusoidal perturbation signal, which enables impedance measurements under dynamic...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Novel 5-Substituted 2-(Aylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl)benzenesulfonamides: Synthesis, Molecular Structure, Anticancer Activity, Apoptosis-Inducing Activity and Metabolic Stability
PublicationA series of novel 5-substituted 2-(arylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl) benzenesulfonamide derivatives 27–60 have been synthesized by the reaction of aminoguanidines with an appropriate phenylglyoxal hydrate in glacial acetic acid. A majority of the compounds showed cytotoxic activity toward the human cancer cell lines HCT-116, HeLa and MCF-7, with IC50 values below 100 M. It was found that for the analogues 36–38...
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Wodór jako paliwo cz. 1
PublicationW artykule przedstawiono wodór jako nowoczesny nośnik energii oraz jego zastosowanie techniczne w ujęciu konwersji energii. Przybliżono jego odkrycie, właściwości oraz jego wykorzystanie od odkrycia do współczesności. Dokonano opisu budowy i zasady działania ogniw paliwowych. Omówiono ich podział przedstawiając zalety i wady każdego rozwiązania oraz ich zastosowanie techniczne w zależności od typu ogniwa.
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Induction of G2/M phase arrest and apoptosis of human pancreatic cancer BxPC-3 cells by potenet antitumor 1-nitroacridine derivative C-1748
PublicationPancreatic ductal adenocarcinoma (PDA) is among the most lethal human cancers, in part because it is insensitive to many chemotherapeutic drugs. Gemcitabine still remains the best chemotherapeutic agent available for the treatment of advanced pancreatic cancer. However, gemcitabine treatment results in only a marginal survival advantage. Thus, there is a strong need for the continuous development of novel therapeutic agents...
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Characteristics of La 0.8 Sr 0.2 Ga 0.8 Mg 0.2 O 3-δ -supported micro-tubular solid oxide fuel cells with LaCo 0.4 Ni 0.6-x Cu x O 3-δ cathodes
PublicationIn this study, micro-tubular solid oxide fuel cells (T-SOFCs) with extruded La0.8Sr0.2Ga0.8Mg0.2O3-δ (LSGM) electrolyte as the mechanical support and LaCo0.4Ni0.6O3-δ (LCNO) or LaCo0.4Ni0.4Cu0.2O3-δ (LCNCO) as cathodes were prepared and characterized. Partial substitution of Cu for the Ni-ion positions in the LCNO lattices was found to significantly enhance the densification and accelerate the grain growth. The porosity-corrected...
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Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives
PublicationA series of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)benzenesulfonamides were synthesized from 4-amino-N-(aryl/heteroaryl)benzenesulfonamides and 2,5-dimethoxytetrahydrofuran. All the synthesized compounds were evaluated for their anticancer activity on HeLa, HCT-116, and MCF-7 human tumor cell lines. Compound 28, bearing 8-quinolinyl moiety, exhibited the most potent anticancer activity against the HCT-116, MCF-7, and HeLa cell lines,...
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Ceramic composites for single-layer fuel cells
PublicationComposite materials consisting of acceptor doped lanthanum orthoniobate electrolyte phase (La0.98Ca0.02NbO4) and Li2O:NiO:ZnO semiconducting phase were synthesized. The precursor powder of La0.98Ca0.02NbO4 was prepared in nanocrystalline (mechanosynthesis) and microcrystalline (solid-state synthesis) form. The composite can be applied in a single-layer fuel cell, because of the presence of two phases acting as an anode and a cathode...
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Single-phase power electronics transformer with active functions for smart grid
PublicationThis paper presents the control of one cell of a modular single-phase power electronics transformer with active functions for meeting the smart grid concept. In this way, the converter could be used not only as a conventional transformer but also for grid such as reactive power, harmonic elimination and energy storage. The topology of the cell is composed by a bidirectional converter with three stages: a half bridge in the input...
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Solid Oxide Fuel Cells with Ni infiltrated perovskite anode
PublicationNiobium-doped strontium titanate was used as the anode for a solid oxide fuel cell. Electrolyte-supported cells were prepared with pure perovskite and composite perovskite–yttria–stabilized-zirconia (YSZ) anodes. Fuel cell tests demonstrated significant improvement in power density after infiltration with a small amount of Ni. The obtained values of power densities are comparable with conventional Ni/YSZ cermet anode. In addition,...
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Cardinal regenerative features of the MRL mouse
PublicationIn this review, we discuss recent studies relating to major features of adult MRL mouse biology that contribute to the regenerative responses seen. These include an increased inflammatory cell profile, a unique glycolytic metabolic state typically found during embryogenesis, and a cell cycle phenotype of DNA damage and G2/M arrest. These traits have been found in other mammalian and non-mammalian regenerative systems. How these...
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Fluoroaromatic substituents attached to carbon nanotubes help to increase oxygen concentration on biocathode in biosensors and biofuel cells
PublicationBased on the known ability of perfluorodecalin/perfluorohydrocarbons to enhance oxygen solubility we modified oxygen sensitive biocathode by adding perfluorinated components to the catholite. This procedure improved the efficiency of the oxygen sensitive cathodes. Glassy carbon electrodes covered with single-wall carbon nanotubes (SWCNTs) with covalently bonded perfluoroaromatic groups were shown to be more sensitive to oxygen,...
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Microbial and chemical quality assessment of the small rivers entering the South Baltic. Part II: Case study on the watercourses in the Puck Bay catchment area
PublicationDue to its location, Puck Bay is an area particularly vulnerable to pollution of anthropogenic origin. The aim of the study was to assess the water quality of small watercourses entering the inner part of Puck Bay. The paper presents the results of chemical and microbiological analyses of 10 rivers and canals at their estuaries located on the western shore of the internal Puck Bay. The following environmental parameters were analyzed:...
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Radar technique in application of interlayer identification connections
PublicationOne of important issues in pavement construction is to ensure that layers applied directly one on top of the other make up a continuous whole and form an integral construction complex. An appropriate interlayer connection plays here significant role ensuring proper transmission of distortions generated by wheels of vehicles to lower layers and preventing water penetration between the layers. In case of damaged pavements where lack...
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An integrated geoarchaeological approach to late Iron Age settlement at Kaštelina hillfort (Lopar, Island of Rab, Croatia) using Amplitude Data Comparison (ADC) method and trial excavation
PublicationGeophysical prospection and small-scale archaeological excavation were undertaken on the site of Kaštelina, a Late Iron Age hillfort settlement located on the Stolac promontory in the northern part of Rab island (Kvarner Gulf, Croatia). Within the frame of the “Archaeological topography of the island of Rab” program, a Polish–Croatian team applied a series of multidisciplinary methods to study the occupational history of the...
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MARSTRUCT benchmark study on nonlinear FE simulation of an experiment of an indenter impact with a ship side-shell structure
PublicationThis paper presents a benchmark study on collision simulations that was initiated by the MARSTRUCT Virtual Institute. The objective was to compare assumptions, finite element models, modelling techniques and experiences between established researchers within the field. Fifteen research groups world-wide participated in the study. An experiment involving a rigid indenter penetrating a ship-like side structure was used as the case...
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Local atomic order in low Pt-content nanocatalysts investigated in situ by XAS
PublicationThe unique features of X-ray absorption spectroscopy allow investigations of nanosized catalysts for fuel cells under working conditions. We present the results of an experiment carried out on a low Pt content electrocatalyst supported by a mesoporous heteropolyacid salt and used at the cathode of a proton exchange membrane fuel cell (PEMFC). The analysis of the EXAFS signal at the Pt L3-edge indicates that upon operating the fuel...
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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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Isolation of Human Progenitor Epidermal Cells on Collagen Type IV and Analysis of Their Markers with Flow Cytometry and PCR Methods
PublicationEpidermal stem cells, located in the skin, together with keratinocytes are transplanted in regenerative therapies, e.g., for the treatment of burns or other wounds. Here, we describe the protocol of their enzymatic isolation from human skin. It includes separation of the epidermis form the dermis by incubation with dispase followed by cell isolation for epidermis by digestion with trypsin. Cell isolated with this method can be...
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The use of a genetic algorithm in the process of optimizing the shape of a three-dimensional periodic beam
PublicationMechanical periodic structures exhibit unusual dynamic behavior thanks to the periodicity of their structures, which can be attributed to their cellular arrangement. The source of this periodicity may result from periodic variations of material properties within their cells and/or variations in the cell geometry. The authors present the results of their studies on the optimization of physical parameters of a three-dimensional axisymetrical...
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CHEMOTHERAPY-MEDIATED COMPLICATIONS OF WOUND HEALING. AN UNDERSTUDIED SIDE EFFECT
PublicationSignificance: Chemotherapy is a primary method to treat cancer, but while cytotoxic drugs are designed to target rapidly dividing cancer cells, they can also affect other cell types, including dermal cells and macrophages involved in wound healing, which often leads to the development of chronic wounds. The situation becomes even more severe when chemotherapy is combined with surgical tumor excision. Recent advances: Despite its...
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Anticancer Study on IrIII and RhIII Half-Sandwich Complexes with the Bipyridylsulfonamide Ligand
PublicationTwo non-platinum compounds, organometallic half-sandwich complexes [(η 5 -Cp)IrCl(L)]PF 6 (1) and [(η 5 -Cp)RhCl(L)]PF 6 (2) were prepared by treating pentamethylcyclopentadienyl chloride dimers of iridium(III) or rhodium(III) with the obtained 4-amino-N-(2,2'-bipyridin-5- yl)benzenesulfonamide ligand (L) and ammonium hexafluorophosphate. The crystal structures of ligand (L) and complexes 1 and 2 were obtained and then analyzed. Coordination...
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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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REGULATION OF CELLULAR REDOX HOMEOSTASIS BY (-)-EPICATECHIN AND COCOA EXTRACTS – PILOT STUDY
PublicationCocoa polyphenols play an important role in protection against diseases in which oxidative stress is implicated as a causal or contributing factor. The main aim of this study was to elucidate the influence of different cocoa extracts and main cocoa bioactive compound (–)-epicatechin on cell growth and support of antioxidant cellular barrier in colon adenocarcinoma cell line model (HT29). Results show that the tested cocoa bioactivity...
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Regulation of Cellular Redox Homeostasis by (–)-Epicatechin and Cocoa Extracts—A Pilot Study
PublicationCocoa polyphenols play an important role in protection against diseases in which oxidative stress is implicated as a causal or contributing factor. The main aim of this study was to elucidate the influence of different cocoa extracts and main cocoa bioactive compound (–)-epicatechin on cell growth and support of antioxidant cellular barrier in colon adenocarcinoma cell line model (HT29). Results show that the tested cocoa bioactivity...