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Search results for: anti-tumor activity
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Identification of lipid fraction constituents from grasshopper (Chorthippus spp.) abdominal secretion with potential activity in wound healing with the use of GC–MS/MS technique
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Molecular Characterization of a Novel Lytic Enzyme LysC from Clostridium intestinale URNW and Its Antibacterial Activity Mediated by Positively Charged N-Terminal Extension
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Preparation, characterization and antimicrobial activity of polyvinyl alcohol/gum arabic/chitosan composite films incorporated with black pepper essential oil and ginger essential oil
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A comparison of muscle activity of the dominant and non-dominant side of the body during low versus high loaded bench press exercise performed to muscular failure
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Policy Evaluation Network (PEN): Protocol for systematic literature reviews examining the evidence for impact of policies on physical activity across seven different policy domains
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Anthrapyridones, a novel group of antitumour non-cross resistant anthraqui-none analogues. Synthesis and molecular basis of the cytotoxic activity towards K562/DOX cells
PublicationOpracowano syntezę nowej grupy związków z grupy antrapirydonów z odpowiednimi hydrofobowymi lub hydrofilowymi podstawnikami. Badano działanie tych związków na komórkach K562/S i K562/DOX (nadekspresja P-glikoproteiny). Stwierdzono, że zwiększenie lipofilowości zwiększa szybkość P-gp zależnego efluksu z komórki.
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Preparation, characterization and antimicrobial activity of polyvinyl alcohol/gum arabic/chitosan composite films incorporated with black pepper essential oil and ginger essential oil
PublicationIn this study, biocomposite films based on polyvinyl alcohol (PVA), gum arabic (GA) and chitosan (CS) incorporated with BPEO and GEO were fabricated by solvent casting method. FTIR, XRD, SEM and DSC were performed with mechanical and antimicrobial properties of PVA/GA/CS films with and without BPEO and GEO. The BPEO and GEO incorporated PVA/GA/CS films were significantly inhibited the growth of Bacillus cereus, Staphylococcus aureus,...
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Diagnostic Accuracy of Liquid Biopsy in Endometrial Cancer
PublicationBackground: Liquid biopsy is a minimally invasive collection of a patient body fluid sample. In oncology, they offer several advantages compared to traditional tissue biopsies. However, the potential of this method in endometrial cancer (EC) remains poorly explored. We studied the utility of tumor educated platelets (TEPs) and circulating tumor DNA (ctDNA) for preoperative EC diagnosis, including histology determination. Methods:...
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New 2-[(4-Amino-6-N-substituted-1,3,5-triazin-2-yl)methylthio]-N-(imidazolidin-2-ylidene)-4-chloro-5-methylbenzenesulfonamide Derivatives, Design, Synthesis and Anticancer Evaluation
PublicationIn the search for new compounds with antitumor activity, new potential anticancer agents were designed as molecular hybrids containing the structures of a triazine ring and a sulfonamide fragment. Applying the synthesis in solution, a base of new sulfonamide derivatives 20–162 was obtained by the reaction of the corresponding esters 11–19 with appropriate biguanide hydrochlorides. The structures of the compounds were confirmed...
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Reduced expression of ELAVL4 in male meningioma patients
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Pilicides effectively hinder chaperone-usher interactions in all Gram-negative bacteria
PublicationThe chaperone-usher pathway of adhesive structures biogenesis is highly conserved in all Gram-negative bacteria. Pili are polymers of thousands protein subunits that possess conserved immunoglobuline-like structure denoted by lack of the seventh G strand. The effect of this structural defect is a hydrophobic acceptor cleft. The folding of protein subunits is strictly dependent on the action of specific periplasmic chaperone protein...
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Harman and norharman, metabolites of the entomopathogenic fungus Conidiobolus coronatus (Entomophthorales), affect the serotonin levels and phagocytic activity of hemocytes, insect immunocompetent cells, in Galleria mellonella (Lepidoptera)
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Phytochemical screening and effect of Viscum album L. on monoamine oxidase A and B activity and serotonin, dopamine and serotonin receptor 5-HTR1A levels in Galleria mellonealla (Lepidoptera)
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Modification of Rapana thomasiana hemocyanin with choline amino acid salts significantly enhances its antiproliferative activity against MCF-7 human breast cancer cells
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Comparison of mouse plasma and brain tissue homogenate sample pretreatment methods prior to high-performance liquid chromatography for a new 1,2,4-triazole derivative with anticonvulsant activity
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A novel source of the cardiac glycoside digoxin from the endophytic fungus Epicoccum nigrum : isolation, characterization, production enhancement by gamma irradiation mutagenesis and anticancer activity evaluation
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Photoprotection and Antiaging Activity of Extracts from Honeybush (Cyclopia sp.)—In Vitro Wound Healing and Inhibition of the Skin Extracellular Matrix Enzymes: Tyrosinase, Collagenase, Elastase and Hyaluronidase
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Regioselective synthesis of novel 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via a non-Biginelli-type approach and evaluation of their in vitro anticancer activity
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Motility activity, slime production, biofilm formation and genetic typing by ERIC-PCR for Pseudomonas aeruginosa strains isolated from bovine and other sources (human and environment)
PublicationThe molecular-typing strategy, ERIC-PCR was used in an attempt to determine the genomic relationship of 28 P. aeruginosa strains isolated from faeces of healthy bovine, bovine mastitis and from faeces of hospital patients as well as from environment. ERIC-PCR fingerprinting revealed large molecular differentiation within this group of isolates. Twenty two out of 28 strains tested generated unique patterns of DNA bands and only...
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The effect of anthropogenic activity on BTEX, NO2, SO2, and CO concentrations in urban air of the spa city of Sopot and medium-industrialized city of Tczew located in North Poland
PublicationThe major goal of the present study is to compare the air quality of two urban locations situated in Northern Poland – the spa City of Sopot and the medium-industrialized city of Tczew using chemometric methods. As a criterion for the assessment of atmospheric air quality, measurements of benzene, toluene, ethylbenzene and total xylenes were used (collected from atmospheric air using diffusion-type passive samplers) as well as...
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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublicationOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublicationHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Caffeine Inhibits Differentiation Of Lung Cancer Stem Cells By Modulating Their Respiratory Metabolism
PublicationIt is ell established that many tumor types contain a fraction of cells, with stem cell-like properties, called cancer stem cells (CSCs), that are resistant to apoptosis induced by therapeutic agents. The presence of CSCs may explain why a standard anticancer treatment, that eliminates only differentiated cancer cells, does not lead to cancer cure.We previously showed the existence of caffeine-sensitive mechanism that controls...
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Effect of in vitro gastro‐pancreatic digestion on antioxidant activity of low‐molecular‐weight (<3.5 kDa) peptides from dry‐cured pork loins with probiotic strains of LAB
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Adipokine and cytokine levels in non-functioning adrenal incidentalomas (NFAI)
PublicationDue to the fact that overweight or obesity is accompanied by hormonally active adrenal tumors: Cushing Syndrome-(CS) and Subclinical Cushing Syndrome (SCS), it is of high interest the correlation between different adipokines and cytokines secreted by adipose tissue, with metabolic disorders and hormonal activity in this group. Even in non-functioning adrenal incidentalomas (NFAI) elevated risk for cardiovascular disease and metabolic...
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Medical Image Dataset Annotation Service (MIDAS)
PublicationMIDAS (Medical Image Dataset Annotation Service) is a custom-tailored tool for creating and managing datasets either for deep learning, as well as machine learning or any form of statistical research. The aim of the project is to provide one-fit-all platform for creating medical image datasets that could easily blend in hospital's workflow. In our work, we focus on the importance of medical data anonimization, discussing the...
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Novel 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives as potent anticancer agents – Synthesis, molecular structure, QSAR studies and metabolic stability
PublicationA series of new 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The obtained results indicated that these compounds display prominent cytotoxic effect. The best anticancer properties have been observed for derivatives...
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Screening of predicted synergistic multi-target therapies in glioblastoma identifies new treatment strategies
PublicationAbstract Background IDH-wildtype glioblastoma (GBM) is a highly malignant primary brain tumor with a median survival of 15 months after standard of care, which highlights the need for improved therapy. Personalized combination therapy has shown to be successful in many other tumor types and could be beneficial for GBM patients. Methods We performed the largest drug combination screen to date in GBM, using a high-throughput effort...
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Ageing-Time Dependent Changes of Angiotensin I-Converting Enzyme-Inhibiting Activity of Protein Hydrolysates Obtained from Dry-Cured Pork Loins Inoculated with Probiotic Lactic Acid Bacteria
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Panax quinquefolium L. Ginsenosides from Hairy Root Cultures and Their Clones Exert Cytotoxic, Genotoxic and Pro-Apoptotic Activity towards Human Colon Adenocarcinoma Cell Line Caco-2
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Structure-activity relationship study of a small cyclic peptide H-c[Lys-Pro-Glu]-Arg-OH: a potent inhibitor of Vascular Endothelial Growth Factor interaction with Neuropilin-1
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Synthesis and molecular structure of novel 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-1H-1,2,4-triazol-3-yl)-5-methylbenzenesulfonamideswith potential anticancer activity
PublicationOtrzymano 15 nowych związków: 2-(alkilotio)-4-chloro-N-(4,5-dihydro-5-oxo-1H-1,2,4-triazol-3-yl)-5-metylobenzenosulfonamidów, dla których opracowano nową metodę syntezy. Dla jednej pochodnej wyznaczono strukturę rentgenowską. Związek nr 36 wykazuje wysoką aktywność przeciwnowotworową w stosunku do 13 linii komórek nowotworowych o poziomie GI_50 w zakresie stężeń 1,9-3,0 μM.
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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublicationMultidrug resistance (MDR) remains a primary hindrance to curative cancer therapy. Thus, introduction of novel strategies to overcome MDR is of paramount therapeutic significance. Sequestration of chemotherapeutics in lysosomes is an established mechanism of drug resistance. Here, we show that MDR cells display a marked increase in lysosome number. We further demonstrate that imidazoacridinones (IAs), which are cytotoxic fluorochromes,...
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublicationNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...
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Bioreactor shoot cultures of Rhododendron tomentosum (Ledum palustre) for a large-scale production of bioactive volatile compounds
PublicationRhododendron tomentosum Harmaja (Ledum palustre), a peat bog plant from Ericaceae family, has been used in traditional medicine as the anti-arthritis agent. Although modern researches confirm its anti-inflammatory properties, it remains threatened by habitat degradation and possibilities to collect this endangered species from its natural environment for further biological activity studies are limited. Therefore, R. tomentosum...
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Anticancer Imidazoacridinone C-1311 is Effective in Androgen-Dependent and Androgen-Independent Prostate Cancer Cells
PublicationAndrogen receptor (AR) plays a crutial role in prostate cancer (PCa) development and metastasis. Here, we reported potent anti-PCa activity of a small molecule imidazoacridinone C-1311. In AR-positive PCa cells, C-1311 was found to inhibit the transcriptional activity of AR uncovering a novel mechanism that may be relevant for its anticancer effect. Mechanistically, C-1311 decreased AR binding to prostate-specific antigen (PSA)...
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Novel Resveratrol-Based Substrates for Human Hepatic, Renal, and Intestinal UDP-Glucuronosyltransferases
PublicationTrans-Resveratrol (tRes) has been shown to have powerful antioxidant, anti-inflammatory, anti-carcinogenic, and anti-aging properties; however, its use as a therapeutic agent is limited by its rapid metabolism into its conjugated forms by UDP-Glucuronosyltransferases (UGTs). The aim of the current study was to test the hypothesis that the limited bioavailability of tRes can be improved by modifying its structure to create analogs...
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ANALYSIS OF THE p53 PROTEIN GENE EXPRESSION MODEL
PublicationWe study the asymptotic behaviour of the solutions of the p53-Mdm2 model proposed by Monk (2003). The p53 gene is crucial for cellular inhibition of the angiogenesis process, while Mdm2 is a negative regulator of the p53 tumor-suppressor. We investigate the stability of the positive steady state and perform some numerical experiments.
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Doświadczanie bólu a aktywność fizyczna u osób z chorobą dyskową odcinka krzyżowo – lędźwiowego kręgosłupa/ Experience of pain and physical activity in people suffering from the disc disease of the lumbosacral spine
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Distance between the Basic Group of the Amino Acid Residue's Side Chain in Position P1of Trypsin Inhibitor CMTI-III and Asp189in the Substrate Pocket of Trypsin Has an Essential Influence on the Inhibitory Activity
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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A Model-Based Improved Control of Dissolved Oxygen Concentration in Sequencing Wastewater Batch Reactor
PublicationBiochemical processes at wastewater treatment plant are complex, nonlinear, time varying and multivariable. Moreover, relationships between processes are very strong. One of the most important issues is exerting proper control over dissolved oxygen levels during nitrification phase. This parameter has a very large impact on activity of microorganisms in activated sludge and on quality of pollution removal processes. Oxygen is supplied...
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A strong preference for the TA/TA dinucleotide step discovered for an acridine-based, potent antitumor dsDNA intercalator, C-1305: NMR-driven structural and sequence-specificity studies
PublicationTriazoloacridinone C-1305, a potent antitumor agent recommended for Phase I clinical trials, exhibits high activity towards a wide range of experimental colon carcinomas, in many cases associated with complete tumor regression. C-1305 is a well-established dsDNA intercalator, yet no information on its mode of binding into DNA is available to date. Herein, we present the NMR-driven and MD-refined reconstruction of the 3D structures...
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Strongly anisotropic surface elasticity and antiplane surface waves
PublicationWithin the new model of surface elasticity, the propagation of anti-plane surface waves is discussed. For the proposed model, the surface strain energy depends on surface stretching and on changing of curvature along a preferred direction. From the continuum mechanics point of view, the model describes finite deformations of an elastic solid with an elastic membrane attached on its boundary reinforced by a family of aligned elastic...
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublicationTelomerase plays a pivotal role in cell proliferation, homeostasis, and neoplastic transformation, making it a promising molecular target for cancer chemotherapy. Of note, although hTERT has been explored thoroughly as a target, none of the promising molecules has been approved as a drug until now. The subject of research conducted as part of my doctoral dissertation is explaining the cellular and molecular mechanism of action...
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QUANTITATIVE EASING POLICY AND ITS IMPACT ON THE GLOBAL ECONOMY
PublicationBased on the analysis of the impact of quantitative easing policies on the global economy, there was concluded that the world’s largest central banks and widespread debt stimulation have created the model of economic growth. This model was based on the productivity growth. The lack of productivity growth in the developed world, the active integration of developing countries (first of all China and India) in the global economy have...
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Badanie odporności na poślizg posadzkowych powłok żywicznych
PublicationW artykule przedstawiono badania wskaźnika szorstkości (odporności na poślizg) posadzki wykonanej z powłok żywicznych za pomocą wahadła angielskiego. Omówiono wybrane metody określania właściwości antypoślizgowych posadzek wraz z przeglądem literatury.
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Preliminary Study on the Antibacterial Activity of Essential Oils Alone and in Combination with Gentamicin Against Extended-Spectrum β-Lactamase-Producing and New Delhi Metallo-β-Lactamase-1-Producing Klebsiella pneumoniae Isolates
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NO-BROADCASTING OF NON-SIGNALLING BOXES VIA OPERATIONS WHICH TRANSFORM LOCAL BOXES INTO LOCAL ONES
PublicationWe deal with families of probability distributions satisfying non-signalling condition, called non-signalling boxes and consider a class of operations that transform local boxes into local ones (the one that admit LHV model). We prove that any operation from this class cannot broadcast a bipartite non-local box with 2 binary inputs and outputs. We consider a function called anti-Robustness which can not decrease under these operations....
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Selected adipocytokines in patients with an incidentally discovered pheochromocytoma
PublicationBACKGROUND: Adipose tissue secretes many adipokines and cytokines, which may be an additional risk factor of cardiovascular and metabolic diseases in patients with an incidentally discovered pheochromocytoma (PHEO). The aim of the study was to investigate levels of selected adipocytokines in these patients. METHODS: This prospective study included 12 patients with an incidentally discovered PHEO and 18 healthy participants. In...