Search results for: cancer treatment
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublicationBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Transcriptomic landscape of blood platelets in healthy donors
PublicationBACKGROUND Blood platelet RNA-sequencing is increasingly used among the scientific community. Aberrant platelet transcriptome is common in cancer or cardiovascular disease, but reference data on platelet RNA content in healthy individuals are scarce and merit complex investigation. METHODS We sought to explore the dynamics of platelet transcriptome. Datasets from 204 healthy donors were used for the analysis of splice variants,...
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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Interactions between bioactive components determine antioxidant, cytotoxic and nutrigenomic activity of cocoa powder extract
PublicationNumerous studies have shown, rather disappointingly, that isolated bioactive phytochemicals are not as biologically effective as natural plant products. Such a discrepancy may be explained by the concept of food synergy, which was verified in this research for cocoa extract versus its major components with regard to cancer chemoprevention. The evaluation embraced the relationship between redox properties evaluated in cell-free systems...
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Synthesis, physicochemical and theoretical studies on new rhodium and ruthenium dimers. Relationship between structure and cytotoxic activity
PublicationTwo dimeric compounds of the general formulae (Et3NH)2[Rh2(μ2-L)4Cl2] (1) (where L = thiophene-2-carboxylate) and [((η6-p-cymene)Ru)2(μ-Cl)3]PF6 (2) have been synthesized using a new method. The unique anionic complex 1 (space group P bca) has octahedral coordination in which the equatorial positions are occupied by the oxygen atoms of four thiophene-2-carboxylates in a paddle wheel fashion. In complex 2 (space group ), each Ru(II)...
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Transcriptomic landscape of blood platelets in healthy donors
PublicationBlood platelet RNA-sequencing is increasingly used among the scientific community. Aberrant platelet transcriptome is common in cancer or cardiovascular disease, but reference data on platelet RNA content in healthy individuals are scarce and merit complex investigation. We sought to explore the dynamics of platelet transcriptome. Datasets from 204 healthy donors were used for the analysis of splice variants, particularly with...
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Antitumor Activity of Triazine Mimic Antibiotics for DNA-binding Implications (Impressive Activity in Vitro Against a Variety of Tumor Types in the NCI-60 Screen): NSC 710607 To Fight HCT-116 Human Colon Carcinoma Cell Lines in Vivo Using the Hollow Fiber Assay and Xenograft Mouse Models
PublicationPurpose Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. Methods The NCI initial hollow...
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Synthesis, crystal structure and cytotoxic activity of ruthenium(II) piano-stool complex with N,N-chelating ligand
PublicationA mononuclear compound of the general formula [(η6-p-cymene)RuIICl(2,2′-PyBIm)]PF6 has been synthesized from a bidentate N,N-donor ligand, viz. 2,-(2′-pyridyl)benzimidazole (2,2′-PyBIm) and the corresponding chloro-complex [(η6-p-cymene)Ru(μ-Cl)Cl]2 (precursor). The isolated coordination compound was characterized by IR, UV–vis and 1H, 13C NMR spectroscopies. The single crystal X-ray analysis of the complex reveals that the asymmetric...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublicationA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Spatio-Temporal Validation of GNSS-Derived Global Ionosphere Maps Using 16 Years of Jason Satellites Observations
PublicationExisting ionospheric models perform very well in mapping the calm state of the ionosphere. However, the problem is accurately determining the total electron content (TEC) for disturbed days. Knowledge of the exact electron density is essential for single−frequency receivers, which cannot eliminate the ionospheric delay. This study aims to investigate temporal and spatial variability in the distribution of TEC based on differences...
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Longitudinal drug synergy assessment using convolutional neural network image-decoding of glioblastoma single-spheroid cultures
PublicationAbstract Background In recent years, drug combinations have become increasingly popular to improve therapeutic outcomes in various diseases, including difficult to cure cancers such as the brain cancer glioblastoma. Assessing the interaction between drugs over time is critical for predicting drug combination effectiveness and minimizing the risk of therapy resistance. However, as viability readouts of drug combination experiments...
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Synthesis, crystal structure and spectroscopic characterization of new anionic iridium(III) complexes and their interaction with biological targets
PublicationThe synthesis and characterisation of new anionic iridium(II) complexes (NH4)2[IrCl4(κ2N,N’-H2biim)]2 · 5H2O (1) and ((CH3)2NH2)[IrCl4(κ2N,N’-PyBIm)] · H2O (2) are presented in this article. Spectroscopic methods (1H, 13C and 15N NMR, FTIR, UV-Vis) were used to characterize these new complexes. Solid-state structural analysis (SC-XRD) of complexes 1 and 2 shows a slightly distorted octahedral geometry of Ir(III) ions, which is...
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Drinking water safety evaluation in the selected sub-Saharan African countries: A case study of Madagascar, Uganda and Rwanda
PublicationIn the sub-Saharan region of Africa, access to safe drinking water remains limited in many countries. This study provides an overview of the quality of surface water and groundwater in rural and peri-urban areas of Madagascar, Uganda, and Rwanda. Selected physico-chemical parameters, inorganic species (including inorganic ions), and organic pollution indicators, such as total organic carbon, non-ionic surfactants, cationic surfactants, anionic...
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Efficient Calibration of Cost-Efficient Particulate Matter Sensors Using Machine Learning and Time-Series Alignment
PublicationAtmospheric particulate matter (PM) poses a significant threat to human health, infiltrating the lungs and brain and leading to severe issues such as heart and lung diseases, cancer, and premature death. The main sources of PM pollution are vehicular and industrial emissions, construction and agricultural activities, and natural phenomena such as wildfires. Research underscores the absence of a safe threshold for particulate exposure,...
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Effects of CO2 and utilization of spent trickling liquid towards plant growth
Open Research DataDataset presents the results of biomass yield for Phaseolus vulgaris pot cultures watered with diluted trickling liquid from biotrickling filtration experiments with or without additional CO2 in air by means of introducting post-biofilter air to the plant culture.
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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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Trzej prorocy: Sołżenicyn, Friedman, Dugin. Część pierwsza: Sołżenicyn
PublicationArtykuł przedstawia na tle biograficznym dzieło i myśl profetyczną Aleksandra Sołżenicyna. Podstawą jej analizy jest mowa z okazji przyznania autorowi Oddziału chorych na raka literackiej Nagrody Nobla oraz jego wykład na temat stanu cywilizacji Zachodu wygłoszony na Uniwersytecie Harvarda – zatytułowany Zmierzch odwagi. Proroctwa Sołżenicyna dotyczące Zachodu pokazane są w kontekście jego pracy Jak odbudować Rosję? W artykule...
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Anticancer imidazoacridinone C-1311 inhibits hypoxia-inducible factor-1α (HIF-1α), vascular endothelial growth factor (VEGF) and angiogenesis
PublicationAntitumor imidazoacridinone C-1311 is a DNA-reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor. Here, we demonstrate the mechanism of C-1311 inhibitory action on novel targets: hypoxia-inducible factor-1α (HIF-1α), vascular-endothelial growth factor (VEGF), and angiogenesis. In a cell-free system, C-1311 prevented HIF-1α binding to an oligonucleotide encompassing a canonical hypoxia-responsive element (HRE),...
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Covalent DNA modification by products of myrosinase catalysed glucosinolate degradation in cell-free system
PublicationThe bioactive phytochemicals found in Brassica vegetables belonging to glucosinolates (GLS) and especially the products of their degradation isothiocyanates (ITC) and indoles are regarded as the most promising cancer chemopreventive compounds. These secondary metabolites constitute defence system repelling or preventing the development of agrophages attacking brassica plants. The antibiological properties of these compounds suggest...
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Nonlinear impedance of Bi2VO5.5 ceramic of thickness 2.52 mm (after second heat-treatment at 913 K) was measured at high temperature range with impedance spectroscopy method
Open Research DataThe nonlinear electrical properties of Bi2VO5.5 ceramic of thickness 2.52 mm (after second heat-treatment at 913 K) was measured by impedance spectroscopy method.
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublicationThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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Unveiling the electron-induced ionization cross sections and fragmentation mechanisms of 3,4-dihydro-2H-pyran
PublicationThe interactions of electrons with molecular systems under various conditions are essential to interdisciplinary research fields extending over the fundamental and applied sciences. In particular, investigating electron-induced ionization and dissociation of molecules may shed light on the radiation damage to living cells, the physicochemical processes in interstellar environments, and reaction mechanisms occurring in combustion...
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Development of biocompatible iron oxide-silicon oxide core-shell nanoparticles as subcellular delivery platform for glucosamine-6-phosphate synthase inhibitors
PublicationIn order to develop the preparation of iron oxide-silica coreshell nanoparticles (CSNPs), thesis deeply explores the cetyltrimethylammonium (CTA+) directed silica coating methods of the oleic-acid capped iron oxide nanoparticles (OA-IONPs) initialized under near-neutral pH conditions. It is demonstrated that the initial alkaline hydrolysis of ethyl acetate in the presence of CTA+ and OA-IONPs induces an unusual ligand exchange...
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Segmentation-Based BI-RADS ensemble classification of breast tumours in ultrasound images
PublicationBackground: The development of computer-aided diagnosis systems in breast cancer imaging is exponential. Since 2016, 81 papers have described the automated segmentation of breast lesions in ultrasound images using arti- ficial intelligence. However, only two papers have dealt with complex BI-RADS classifications. Purpose: This study addresses the automatic classification of breast lesions into binary classes (benign vs. ma- lignant)...
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Nonlinear impedance of 50Bi2VO5.5-50SrB4O7 fully crystallized glass at 813 K measured with impedance spectroscopy method at high temperature region
Open Research DataThe nonlinear electrcial properties of 50Bi2VO5.5-50SrB4O7 fully crystallized glass was measured by impedance spectroscopy method.
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Nonlinear impedance of 50Bi2VO5.5-50SrB4O7 partially crystallized glass at 613 K measured with impedance spectroscopy method at high temperature region
Open Research DataThe nonlinear electrcial properties of 50Bi2VO5.5-50SrB4O7 partially crystallized glass was measured by impedance spectroscopy method.
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublicationNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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Development of conductive porous media as packing materials for biotrickling filter – microbial fuel cell system (BTF-MFC system)
Open Research DataDataset presents values of electrical resistance measured for three developed conductive packimg materials for the application in a BTF-MFC system.
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A set of data constituting the basis for the publication entitled "Mitochondria dysfunction is one of the causes of diclofenac toxicity in the green alga Chlamydomonas reinhardtii"
Open Research DataNon-steroidal anti-inflammatory drugs (NSAIDs), such as diclofenac (DCF), form a significant group of environmental contaminants. When the toxic effects of DCF on plants are analyzed, authors often focus on photosynthesis, whilemitochondrial respiration is usually overlooked. Therefore, an in vivo investigation of plant mitochondria functioning under...