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Wyniki wyszukiwania dla: cholinesterase inhibitory activity
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The antitumor derivatives, C1305 and C1748, were different in effects on CYP3A4 expression and catalytic activity in HepG2 cells
PublikacjaCytochromy P450 (CYP) należą do grupy enzymów biorących udział w 70-80% metabolizmu fazy I większości stosowanych klinicznie leków. Z tego powodu oddziaływanie leków z enzymami cytochromu P450 stało się istotnym elementem w projektowaniu chemoterapeutyków, szczególnie tych, które są stosowane w terapii wielolekowej. Znajomość substratów, induktorów i inhibitorów poszczególnych izoenzymów P450, nie tylko może obniżać częstość występowania...
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Stannates, titanates and tantalates modified with carbon and graphene quantum dots for enhancement of visible-light photocatalytic activity
PublikacjaMost efforts in heterogeneous photocatalysis are focused on development of new and stable photoactive materials efficient in degradation of various pollutants under visible-light irradiation. In this regard, the wide-bandgap perovskite semiconductors, i.e., SrTiO3 (titanate), SrSnO3 (stannate) and AgTaO3 (tantalate), were prepared by a solvothermal method, and then modified with carbon quantum dots (CQDs) or graphene quantum dots...
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Ewa Augustin dr hab.
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Polyacrylamide substrate viscosity impact on temozolomide activity in glioblastoma cells by flow cytometry and rheological measurements
Dane BadawczeDataset includes raw data on cell lines LN-229 and LN-18 treated with temozolomide measured by flow cytometry, rheometry and cell projections. It also includes calculations necessary for creation of figures and conclusions based on those figures in the publication titiled: "Substrate viscosity impairs temozolomide-mediated inhibition of glioblastoma...
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublikacjaFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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The antitumor derivative, C-1748, affects CYP3A4: crosstalk between drug metabolism, CYP3A4 expression and enzymatic activity
PublikacjaJedną z głównych przeszkód w przewidywaniu wyników terapii u pacjentów z nowotworem jest indywidualny przebieg metabolizmu stosowanych leków wynikający z polimorfizmu genów enzymów metabolizujących, jak również duża zmienność farmakokinetyki leków obserwowana u różnych pacjentów podczas trwania chemioterapii. Z powodu tzw. ''wąskiego okna terapeutycznego'' występującego w przypadku terapii lekami przeciwnowotworowymi, małe zmiany...
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Surface properties and visible light activity of W-TiO2 photocatalysts prepared by surface impregnation and sol-gel method
PublikacjaTiO2 modyfikowany wolframem otrzymano dwiema metodami: metodą zol-żel oraz metodą impregnacji powierzchniowej. Fotokatalizatory kalcynowano w temperaturze 400C. Jako matrycę TiO2 zastosowano ST-01 (Ishihara Sangyo, Japonia, 300m2/g). jako prekursory wolframu zastosowano tlenek wolframu oraz heksakarbonylek wolframu. Badania obejmowały wpływ ilości domieszki na aktywność fotokatalityczną. Charakterystyka otrzymanych fotokatalizatorów...
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Synthesis of isomeric, oxathiolone fuded chalcones and comparison of their activity toward various microorganisms and human cancer cell lines
PublikacjaIzomeryczne oksationolowe sprzężone chalkony otrzymano w wyniku kondensacji odpowiedniego acetylobenzo[1,3]oksatiolo-2-onu z aldehydem benzoesowym w środowisku kwaśnym. Określono aktywność cytotoksyczną otrzymanych związków wobec komórek linii HeLa, przeciwbakteryjną wobec Micrococcus luteus, Staphylococcus aureus, Salmonella typhimurium, Escherichia coli i Proteus vulgaris, przeciwgrzybową wobec Candida albicans i tuberkulostatyczną...
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Acid-catalysed synthesis of oxathiolone fused chalkones. Comparison of their activity toward various microrganisms and human cancer lines
PublikacjaOtrzymano podstawione pochodne oksationolowych sprzężonych chalkonów w wyniku kondensacji 4-acetylo-5-metoksy-2-0ksobenz[1,3]oksatiolu z aldehydem benzoesowym w środowisku kwaśnym. Badano właściwości biologiczne otrzymanych związków. Trzy z otrzymanych pochodnych wykazały umiarkowaną aktywność wobec komórek HeLa, dwa były aktywne wobec Micrococcus luteus i Staphylococcus aureus, a jeden wobec Mycobacterium tuberculosis.
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Chemical Composition and Antimicrobial Activity of Selected Essential Oils against Staphylococcus spp. Isolated from Human Semen
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Chemical Composition, Antioxidant, In Vitro and In Situ Antimicrobial, Antibiofilm, and Anti-Insect Activity of Cedar atlantica Essential Oil
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Effect of psoriasis activity and topical treatment on plasma epidermal growth factor (EGF) and its soluble receptor (sEGFR)
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Effect of psoriasis activity on epidermal growth factor (EGF) and the concentration of soluble EGF receptor in serum and plaque scales
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Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity
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FBG Strain Monitoring of a Road Structure Reinforced with a Geosynthetic Mattress in Cases of Subsoil Deformation in Mining Activity Areas
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Quantitative Structure–Activity Relationships in Two-Electron Reduction of Nitroaromatic Compounds by Enterobacter cloacae NAD(P)H:Nitroreductase
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Naphtho[1′,2′:4,5]imidazo[1,2-a]pyridine-5,6-diones: Synthesis, enzymatic reduction and cytotoxic activity
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Two-electron reduction of quinones by rat liver NAD(P)H:quinone oxidoreductase: quantitative structure–activity relationships
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Activation mechanism and activity of globupain, a thermostable C11 protease from the Arctic Mid-Ocean Ridge hydrothermal system
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Transcriptomics‐Based and AOP‐Informed Structure–Activity Relationships to Predict Pulmonary Pathology Induced by Multiwalled Carbon Nanotubes
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Advantages and limitations of classic and 3D QSAR approaches in nano-QSAR studies based on biological activity of fullerene derivatives
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Effect of Differentiated Nitrogen Fertilization on the Enzymatic Activity of the Soil for Sweet Potato (Ipomoea batatas L. [Lam.]) Cultivation
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Profile of phenolic compounds and antioxidant activity of organically and conventionally grown black-grain barley genotypes treated with biostimulant
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Polyphenolic Characterization, Antioxidant, Antihyaluronidase and Antimicrobial Activity of Young Leaves and Stem Extracts from Rubus caesius L.
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Antimicrobial Activity of Al2O3, CuO, Fe3O4, and ZnO Nanoparticles in Scope of Their Further Application in Cement-Based Building Materials
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Inhibition of ALDH1A1 activity decreases expression of drug transporters and reduces chemotherapy resistance in ovarian cancer cell lines
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The motif EXEXXXL in the cytosolic tail of the secretory human proprotein convertase PC7 regulates its trafficking and cleavage activity
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Use of NMR and Fluorescence Spectroscopy as well as Theoretical Conformational Analysis in Conformation-activity Studies of Cyclic Enkephalin Analogues
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Chemical composition and antifungal activity of Chelidonium majus extracts – antagonistic action of chelerythrine and sanguinarine against Botrytis cinerea
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Ultrashort Cationic Lipopeptides–Effect of N-Terminal Amino Acid and Fatty Acid Type on Antimicrobial Activity and Hemolysis
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Modification of Bacterial Cellulose with Quaternary Ammonium Compounds Based on Fatty Acids and Amino Acids and the Effect on Antimicrobial Activity
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Stability of Antiradical Activity of Protein Extracts and Hydrolysates from Dry-Cured Pork Loins with Probiotic Strains of LAB
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Acute Effects of High-Load vs. Plyometric Conditioning Activity on Jumping Performance and the Muscle-Tendon Mechanical Properties
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Studying the governing factors on the photo(electro)catalytic activity of surface-modified photocatalysts under visible light illumination
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Physical activity and childbirth classes during a pregnancy and the level of perceived stress and depressive symptoms in women after childbirth
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Properties of the HtrA Protease From Bacterium Helicobacter pylori Whose Activity Is Indispensable for Growth Under Stress Conditions
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Correction to “Emerging Anticancer Activity of Candidal Glucosamine-6-Phosphate Synthase Inhibitors upon Nanoparticle-Mediated Delivery”
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High- and low-Molecular Weight oat Beta-Glucan Reveals Antitumor Activity in Human Epithelial Lung Cancer
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Changes in Muscle Activity Imbalance of the Lower Limbs Following 3 Weeks of Supplementary Body-Weight Unilateral Training
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TiO2 Modified with Organic Acids for the Decomposition of Chlorfenvinphos under the Influence of Visible Light: Activity, Performance, Adsorption, and Kinetics
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Mechanism of selective anticancer activity of isothiocyanates relies on differences in DNA damage repair between cancer and healthy cells
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Glycerol and Natural Deep Eutectic Solvents Extraction for Preparation of Luteolin-Rich Jasione montana Extracts with Cosmeceutical Activity
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Dual-Activity Fluoroquinolone-Transportan 10 Conjugates offer alternative Leukemia therapy during Hematopoietic Cell Transplantation
PublikacjaHematopoietic cell transplantation (HCT) is often considered a last resort leukemia treatment, fraught with limited success due to microbial infections, a leading cause of mortality in leukemia patients. To address this critical issue, we explored a novel approach by synthesizing antileukemic agents containing antibacterial substances. This innovative strategy involves conjugating fluoroquinolone antibiotics, such as ciprofloxacin...
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Occupational Burnout as a Consequence of Workaholism – An Outline of the Problem Based on Studies of Polish Women Running Their Own Business Activity
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Long range molecular dynamics study of regulation of eukaryotic glucosamine-6-phosphate synthase activity by UDP-GlcNAc
PublikacjaGlucosamine-6-phosphate (GlcN-6-P) synthase catalyses the first and practically irreversible step in hexosamine metabolism. The final product of this pathway, uridine 5' diphospho N-acetyl-D-glucosamine (UDPGlcNAc), is an essential substrate for assembly of bacterialand fungal cell walls. Moreover, the enzyme is involved in phenomenon of hexosamine induced insulin resistance in type II diabetes, which makes it a potential target...
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Design, Synthesis, and Enzymatic Evaluation of Novel ZnO Quantum Dot-Based Assay for Detection of Proteinase 3 Activity
PublikacjaHerein, 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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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublikacjaConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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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.
PublikacjaEkspresja 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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Gentiana asclepiadea exerts antioxidant activity and enhances DNA repair of hydrogen peroxide- and silver nanoparticles-induced DNA damage
PublikacjaExposure to high levels of different environmental pollutants is known to be associated with induction of DNA damage in humans. Thus DNA repair is of great importance in preventing mutations and contributes crucially to the prevention of cancer. In our study we have focused on quantitative analysis of Gentiana asclepiadea aqueous or methanolic extracts obtained from flower and haulm, their antioxidant potency in ABTS post-column...
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Pre-clinical evaluation of 1-nitroacridine derived chemotherapeutic agent that has preferential cytotoxic activity towards prostate cancer
PublikacjaPraca 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...