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Search results for: CELLULAR ANTIOXIDANT ACTIVITY
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Design, Synthesis, and Enzymatic Evaluation of Novel ZnO Quantum Dot-Based Assay for Detection of Proteinase 3 Activity
PublicationHerein, the synthesis and application of functionalized quantum dot-based protease probes is described. Such probes are composed of nontoxic ZnO nanocrystals decorated by amino groups followed by linker and labeled peptide attachment. Spherical NH2-terminated ZnO quantum dots (QDs) with the average size ranging from 4 to 8 nm and strong emission centered at 530 nm were prepared using the sol−gel method. The fluorescence of ZnO...
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Chiral Pyrazolo[4,3-e][1,2,4]triazine Sulfonamides—Their Biological Activity, Lipophilicity, Protein Affinity, and Metabolic Transformations
PublicationReferring to our previous laboratory results related to the tyrosinase and urease inhibition by pyrazolo[4,3-e][1,2,4]triazine sulfonamides, we examined here in silico the mechanism of action at the molecular level of the investigated pyrazolotriazine sulfonamides by the molecular docking method. The studied compounds being evaluated for their cytotoxic effect against cancer cell lines (MCF-7, K-562) and for recombinant Abl and...
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Blue-berried honeysuckle a promising cancer preventing fruit; Polish genotypes as a source of bioactive phytochemicals
PublicationFrom the ancient times, plants containing health-oriented compounds in their matrices are used in the treatment of different complaints and diseases. One of these groups are plant secondary metabolites (PSM), especially phenolic compounds, terpenes and terpenoids. A large number of PSM exhibit cytotoxicity against a variety of tumor cells, as well as cancer preventive and anticancer efficacy in preclinical animal models. For this...
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Selectivity Tuning by Natural Deep Eutectic Solvents (NADESs) for Extraction of Bioactive Compounds from Cytinus hypocistis—Studies of Antioxidative, Enzyme-Inhibitive Properties and LC-MS Profiles
PublicationIn the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. The extracts were found to possess total phenolic and total flavonoid contents in the ranges of 26.47–186.13...
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Profile and Content of Phenolic Compounds in Leaves, Flowers, Roots, and Stalks of Sanguisorba officinalis L. Determined with the LC-DAD-ESI-QTOF-MS/MS Analysis and Their In Vitro Antioxidant, Antidiabetic, Antiproliferative Potency
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From tryptophan to novel mitochondria-disruptive agent, synthesis and biological evaluation of 1,2,3,6-tetrasubstituted carbazoles
PublicationMitochondrial targeting plays an important role in anticancer therapy. The Mn(III)-promoted cyclization of 5- (1H-indol-3-yl)-3-oxopentanoic acid allow to obtain novel substituted carbazole derivatives that can act as mitochondria-disruptive agents. The starting materials used for the synthesis of these new aminocarbazoles are oxopentanoate derivatives of tryptophan. The scope and limitation of this method of synthesis are determined...
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublicationIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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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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CYP3A4 overexpression enhances apoptosis induced by anticancer agent imidazoacridinone C-1311, but does not change the metabolism of C-1311 in CHO cells
PublicationWe examine whether CYP3A4 overexpression influences the rate and pattern of antitumor imidazoacridinone C-1311 metabolism, in relation to the impact of this overexpression on cell cycle progression and final cellular response of CHO cells following C-1311 treatment. Methods: Three CHO cell lines: CHO-WT, wild type, CHO-HR, overexpressing cytochrome P450 reductase (CPR) and CHO-HR-3A4, coexpressing CPR and CYP3A4 were applied....
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Activity of antimicrobial peptides and conventional antibiotics against superantigen positive Staphylococcus aureus isolated from patients with atopic dermatitis
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Partial inhibition of borohydride hydrolysis using porous activated carbon as an effective method to improve the electrocatalytic activity of the DBFC anode
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Diazepinoporphyrazines Containing Peripheral Styryl Substituents and Their Promising Nanomolar Photodynamic Activity against Oral Cancer Cells in Liposomal Formulations
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Surface Site Modulations by Conjugated Organic Molecules To Enhance Visible Light Activity of ZnO Nanostructures in Photocatalytic Water Splitting
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Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C
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Xanthine Oxidoreductase Activity in Platelet-Poor and Rich Plasma As a Oxidative Stress Indicator in Patients Required Renal Replacement Therapy
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Inhibitory activity of double‐sequence analogues of trypsin inhibitor SFTI‐1 from sunflower seeds: an example of peptide splicing
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Xanthine oxidoreductase activity in platelet-poor and rich plasma as a oxidative stress indicator in patients required renal replacement therapy
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Synthesis of Novel Phosphonic‐Type Activity‐Based Probes for Neutrophil Serine Proteases and Their Application in Spleen Lysates of Different Organisms
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The Effect of Subinhibitory Concentrations of trans-Anethole on Antibacterial and Antibiofilm Activity of Mupirocin Against Mupirocin-Resistant Staphylococcus aureus Strains
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Effects of acute and long-term slow breathing exercise on muscle sympathetic nerve activity in untreated male patients with hypertension
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Synthesis, activity on NK-3 tachykinin receptor and conformational solution studies of scyliorhinin II analogs modified at position 16
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Influence of Dimerization of Lipopeptide Laur-Orn-Orn-Cys–NH2 and an N-terminal Peptide of Human Lactoferricin on Biological Activity
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Lipidated Analogs of the LL-37-Derived Peptide Fragment KR12—Structural Analysis, Surface-Active Properties and Antimicrobial Activity
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Red phosphorus as self-template to hierarchical nanoporous nickel phosphides toward enhanced electrocatalytic activity for oxygen evolution reaction
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The activity of different extracts from Panax quinquefolium L. cultures against pathogenic Staphylococcus aureus with respect to ginsenoside content
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Quantification of Biodiversity Related to the Active Protection of Grassland Habitats in the Eastern Lublin Region of Poland Based on the Activity of Soil Enzymes
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Acute effects of unilateral and bilateral conditioning activity on countermovement jump, linear speed, and muscle stiffness: A randomized crossover study
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Inulin-type fructans trigger changes in iron concentration and activity of bone metabolism biomarkers in blood plasma of growing pigs
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Truncation of Huia versabilis Bowman-Birk inhibitor increases its selectivity, matriptase-1 inhibitory activity and proteolytic stability
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Cholinesterase inhibitory activity, antioxidative potential and microbial stability of innovative liver pâté fortified with rosemary extract (Rosmarinus officinalis)
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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the anti-tumour imidazoacridinone C-1311 in human hepatoma cells
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On Raman optical activity sign-switching between the ground and excited states leading to an unusual resonance ROA induced chirality
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Transmembrane Transport and Anticancer Activity of Strontium Ranelate Delivered with Nanosecond Pulsed Electric Fields (nsPEFs) into Human Cells in Vitro
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Antiproliferative Activity of Double Point Modified Analogs of 1,25-Dihydroxyvitamin D2 Against Human Malignant Melanoma Cell Lines
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EFFECTS OF DOWNHILL AND UPHILL EXERCISES OF EQUIVALENT SUBMAXIMAL INTENSITIES ON SELECTED BLOOD CYTOKINE LEVELS AND BLOOD CREATINE KINASE ACTIVITY
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Inhibiting Activity of HIV-1: Protease, Reverse Transcriptase and Integrase All Together by Novel Compounds Using Computational Approaches
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Transcriptomic Pattern of Genes Regulating Protein Response and Status of Mitochondrial Activity Are Related to Oocyte Maturational Competence—A Transcriptomic Study
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Enhanced Activity and Sustained Release of Protocatechuic Acid, a Natural Antibacterial Agent, from Hybrid Nanoformulations with Zinc Oxide Nanoparticles
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Pre-clinical evaluation of 1-nitroacridine derived chemotherapeutic agent that has preferential cytotoxic activity towards prostate cancer
PublicationPraca zawiera wyniki badań przedklinicznych pochodnej 1-nitroakrydyny C-1748 wobec komórek ludzkiego raka prostaty CaP in vitro, jak i przeszczepialnego na zwierzęta. W oparciu o fosforylację histonu H2AX jako markera podwójnych cięć DNA wykazano, że C-1748 jest bardziej aktywny w komórkach CaP niż HL60. Zidentyfikowano poza tym receptor androgenny (AR) jako cel molekularny badanego związku. W doświadczeniach na zwierzętach stwierdzono...
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Photocatalytic activity of boron-modified TiO2 under visible light: The effect of boron content, calcination temperature and TiO2 matrix
PublicationPrzedstawiono wpływ temperatury kalcynacji (200, 300, 350, 400, 450 oraz 600oC) na fotoaktywność w świetle widzialnym (l> 400 nm) oraz właściwości powierzchniowe TiO2 modyfikowanego borem. B-TiO2 został przygotowany metodą impregnacji powierzchniowej. Jako prekursor bory wykorzystano ester trietylowy kwasu borowego (BATE). Charakterystyka otrzymywanych fotokatalizatorów obejmowała wyznaczenie powierzchni właściwej, właściwości...
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Structure modification of acridine antitumor agents results in changes of enzymatic activity and gene expression of CYP3A4 isoenzyme in HepG2 cells.
PublicationEkspresja izoenzymu CYP3A4, który zaangażowany jest w metabolizm ok. 60% leków stosowanych klinicznie, może być modulowana przez takie czynniki jak: polimorfizm, czynniki transkrypcyjne oraz obecność ksenobiotyków. Przykładem induktorów genów kodujących izoenzym CYP3A4 jest fenobarbital i rifampicyna, których obecność w organizmie przyspiesza metabolizm innych leków stosowanych jednocześnie, które są substratami dla CYP3A4. Dlatego...
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Preliminary Investigation of the Antibacterial Activity of Antitumor Drug 3-Amino-1,2,4-Benzotriazine-1,4-Dioxide (Tirapazamine) and its Derivatives
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Phytotoxic Activity of Metabolites Isolated from Rutstroemia sp.n., the Causal Agent of Bleach Blonde Syndrome on Cheatgrass (Bromus tectorum)
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Potential of mucoadhesive chitosan glutamate microparticles as microbicide carriers – antiherpes activity and penetration behavior across the human vaginal epithelium
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Towards plant-mediated chemistry – Au nanoparticles obtained using aqueous extract of Rosa damascena and their biological activity in vitro
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Influence of pH of sol-gel solution on phase composition and photocatalytic activity of TiO 2 under UV and visible light
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Indicators of recent geodynamic activity in the Książ Castle area (Świebodzice Unit, Sudetes) in the light of structural analysis and geodetic measurements
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Evaluation of Chemotherapeutic Activity of the Selected Bases’ Analogues of Nucleic Acids Supported by ab initio Various Quantum Chemical Calculations
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Heterogeneous distribution of surface electrochemical activity in polycrystalline highly boron-doped diamond electrodes under deep anodic polarization
PublicationThe surface homogeneity of boron-doped diamond electrodes is variable and depends on anodic polarization conditions. The differentiation factor is the gradual and localized change in surface termination. A series of measurements under different polarization conditions was performed in order to investigate the scale of this effect. Nanoscale impedance microscopy (NIM) revealed large variation of surface resistance in individual...
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Design and Microwave-Assisted Synthesis of TiO2-Lanthanides Systems and Evaluation of Photocatalytic Activity under UV-LED Light Irradiation
PublicationThe TiO2-Eu and TiO2-La systems were successfully synthesized using the microwave method. Based on the results of X-ray diffraction analysis, it was found that regardless of the analyzed systems, two crystal structures were noted for the obtained samples: anatase and rutile. The analysis, such as XPS and EDS, proved that the doped lanthanum and europium nano-particles are present only on the TiO2 surface without disturbing the...