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Using Rule-Based System for Monitoring Marine Navigation Data Processing
PublicationProcessing marine navigational data requires sophisticated software solutions. Typically, specialized tools called processors are analyzing raw data from different sensors. It becomes important to create the monitoring software that is able to validate and verify processing components integrated into the final system. Drools®business rule management platform provides a core business rules engine, web authoring and rules management...
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Modelling charge transfer processes in C2+ -tetrahydrofuran collision for ion-induced radiation damage in DNA building blocks
PublicationInvestigations of collision-induced processes involving carbon ions and molecules of biological interest in particular DNA building blocks, are crucial to model the effect of radiation on cells in order to improve medical treatments for cancer therapy. Using carbon ions appears to be one of the most efficient ways to increase biological effectiveness to damage cancerous cells by irradiating deep-seated tumors. Therefore, interest...
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Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublicationOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
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Molecular basis for the DNA damage induction and anticancer activity of asymmetrically substituted anthrapyridazone PDZ-7
Publicationnthrapyridazones, imino analogues of anthraquinone, constitute a family of compounds with remarkable anti-cancer activity. To date, over 20 derivatives were studied, of which most displayed nanomolar cytotoxicity towards broad spectrum of cancer cells, including breast, prostate and leukemic ones. BS-154, the most potent derivative, had IC50 values close to 1 nM, however, it was toxic in animal studies. Here, we characterize another...
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The Influence of Different Hydrothermal Processes Used in the Preparation of Brussels Sprouts on the Availability of Glucosinolates to Humans
PublicationCruciferous vegetables represent a valuable source of bioactive compounds. However, there is currently a deficiency of information regarding the extent to which these compounds remain bioaccessible to the body following thermal treatment and digestion processes within the digestive tract. Accordingly, the aim of this study was to evaluate the impact of heat treatment and in vitro digestion on the level of selected bioactive compounds...
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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublicationLow solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of the...
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Antitumor imidazoacridinone derivative C-1311 induces cell cycle arrest and cellular senescence-like phenotypic changes in human non-small lung A549 cancer cells
PublicationPrzeprowadzone badania miały na celu zbadanie rodzaju odpowiedzi komórkowej indukowanej przez pochodną C1311 w komórkach ludzkiego, niedrobnokomórkowego raka płuc A549, wyselekcjonowanych do badań ze względu na wysoką wrażliwość na działanie pochodnej C-1311. Wszystkie eksperymenty przeprowadzone zostały przy stężeniu hamującym proliferację komórek nowotworowych w 80%. Badania z wykorzystaniem techniki cytometrii przepływowej oraz...
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Three-dimensional modeling and automatic analysis of the human nasal cavity and paranasal sinuses using the computational fluid dynamics method
PublicationPurpose The goal of this study was to develop a complete workflow allowing for conducting computational fluid dynam- ics (CFD) simulation of airflow through the upper airways based on computed tomography (CT) and cone-beam computed tomography (CBCT) studies of individual adult patients. Methods This study is based on CT images of 16 patients. Image processing and model generation of the human nasal cavity and paranasal sinuses...
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The influence of 4-substituted and unsubstituted derivatives of 1-nitroacridine on the cell cycle and induction of apoptosis in human cancer HT29 and HeLa S3.
PublicationZbadano wpływ pochodnych 1-nitroakrydyny C-1748 i C-857, w stężeniach biologicznie istotnych, na cykl życiowy oraz indukcję apoptozy komórek raka jelita grubego HT29 oraz raka szyjki macicy HeLa S3. Metodą cytometrii przepływowej wykazano, że 4-metylo-1-nitroakrydyna C-1748 powoduje akumulację komórek HT29 w fazie S i komórek HeLa S3 w fazie G2 cyklu komórkowego zaś związek C-857 indukuje akumulację komórek HT29 i HeLa S3 w fazie...
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High temperature oxidation behavior of SUS430 SOFC interconnects with Mn-Co spinel coating in air
PublicationIn this study, SUS430 alloy is evaluated for its high temperature corrosion properties as a possible material for interconnects of solid oxide fuel cells (SOFCs). Samples are coated with Mn-Co by commercial physical vapor deposition (PVD) process and oxidized in air for 1250 h at 800 °C. A dense cubic Mn-Co-Fe spinel layer is formed on the surface, showing great effect on corrosion reduction compared with the samples without coating....
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Influence of the particle size of carbonate-siliceous rock on the efficiency of phosphorous removal from domestic wastewater
PublicationtThe aim of the study was to determine the influence of the particle size of carbonate–silica rock (opoka)used in rock filters on the efficiency of phosphorus removal from domestic wastewater. The investigationswere carried out in a laboratory using a model consisting of three vertical flow filters with carbonate–silicarock of different particle sizes (G1= 1–2 mm; G2= 2–5 mm; G3= 5–10 mm). The tested rock was subjectedto decarbonising...
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A low-voltage CMOS negative impedance converter for analogue filtering applications
PublicationLow-voltage high-frequency continuous-time filters are still required in many applications and are the subject of continuing research. There are many techniques to realize integrated filters, including OTA C, Opamp RC and MOSFET-C-Opamp. The latter two show high dynamic range at low supply voltage, but their frequency operating range is usually limited to several megahertz. Transconductance filters are dedicated to higher frequencies....
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Computer-aided reconstruction of the railway track axis geometrical shape
PublicationIn the paper a method of the railway track axis geometrical shape identification in a horizontal plane, directly from the continuous satellite measurements, is presented. In this method, an algorithm for the design of railway track sections located in the horizontal arc is used. The algorithm uses an analytical description of the layout by means of suitable mathematical formulas. The design procedure has a universal character and...
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublicationThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublicationRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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Wybrane problemy szlifowania powierzchni płaskich z kinematyką docierania
PublicationW pracy przedstawiono teoretyczne i doświadczalne podstawy szlifowania powierzchni płaskich z kinematyką docierania. Dokonano kompleksowej analizy zastosowanych układów kinematycznych szlifierek. Przeprowadzono eksperymenty szlifowania jednostronnego ściernicami o spoiwie galwanicznym z ziarnami diamentowymi (D107, D64 i D46) oraz z regularnego azotku boru (B107 i B64). Innowacyjność ściernic polegała na zróżnicowanym utwierdzeniu...
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Morphological and cellular alternations of HepG2 cells overexpressing CYP3A4 after treatment with antitumor imidazoacridinone derivative C-1311
PublicationW pracy badano odpowiedź biologiczną komórek nowotworu wątroby HepG2 z nadekspresją izoenzymu CYP3A4 pod wpływem pochodnej imidazoakrydonu C-1311. Wyniki porównywano z odpowiedzią komórek HepG2 z tzw. wektorem zerowym.Izoeznym CYP3A4 jest jednym z izoenzymów cytochromu P450 odpowiedzialnych za przemiany metaboliczne pochodnej C-1311. Wykazano, że pochodna C-1311 indukuje w obu liniach komórkowych blok w fazie G2/M cyklu komórkowego,...
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Antitumour imidazoacridone C-1311 induces cell death by mitotic catastrophe in human colon carcinoma cells
PublicationW przedstawionych badaniach określano mechanizm śmierci komórkowej indukowanej przez imidazoakrydon C-1311 (Symadex) w komórkach HT-29 ludzkiego raka jelita grubego, które wykazywały szczególną wrażliwość na ten związek w eksperymentalnych modelach in vitro i in vivo. Przy stężeniu odpowiadającemu dawce IC99, związek powodował zahamowanie progresji cyklu komórkowej w fazie S po czym następował blok w fazie G2. Po czasach 48-96...
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublicationHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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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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Regulacja topologii DNA przez topoizomerazę typu II, czyli jak struktura DNA wpływa na funkcjonowanie genów
PublicationW wielu ważnych procesach jakie zachodzą w komórce zmienia się topologia DNA i struktura chromatyny. Enzym, topoizomeraza typu II, jest jednym z ważnych czynników, który reguluje zmiany topologiczne i strukturalne w jądrze, przez co ma bezpośredni lub pośredni wpływ na takie procesy jak uporządkowanie struktury chromatyny poprzez wiązanie pętli chromatyny do szkieletu jądrowego, transkrypcję i replikację DNA, reperację uszkodzeń...
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Improved cytotoxicity and preserved level of cell death induced in colon cancer cells by doxorubicin after its conjugation with iron-oxide magnetic nanoparticles
PublicationA promising strategy for overcoming the problem of limited efficacy in antitumor drug delivery and in drug release is the use of a nanoparticle-conjugated drug. Doxorubicin (Dox) anticancer chemotherapeutics has been widely studied in this respect, because of severe cardiotoxic side effects. Here, we investigated the cytotoxic effects, the uptake process, the changes in cell cycle progression and the cell death processes in the...
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The increased level of cytochrome P450 isoenzyme CYP3A4 affects the cellular response in CHO cells upon antitumor imidazoacridinone C-1311 treatment
PublicationPochodna C-1311 to potencjalny związek przeciwnowotworowy, który dotarł do II fazy badań klinicznych. Związek ten ulega metabolicznej transformacji pod wpływem szczurzych i ludzkich białek mikrosomalnych. Wykazano, że białka cytochromu P450 odpowiadają za przemiany metaboliczne C-1311 jedynie w niewielkim stopniu. Z drugiej strony wykazano, że pochodna C-1311 jest inhibitorem białek cytochromu P450, zwłaszcza izoenzymu CYP1A2...
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DNA-damaging imidazoacridinone C-1311 induces autophagy followed by irreversible growth arrest and senescence in human lung cancer cells
PublicationImidazoacridinone 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) is an antitumor inhibitor of topoisomerase II and FMS-like tyrosine kinase 3 receptor. In this study, we describe the unique sequence of cellular responses to C-1311 in human non-small cell lung cancer (NSCLC) cell lines, A549 and H460. In A549 cells, C-1311 (IC80 = 0.08 µM) induced G1 and G2/M arrests, whereas H460 cells (IC80 = 0.051 µM) accumulated...
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Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.
PublicationThe acridinone derivates C-1305 and C-1311 are promising antitumor agents with high activity against several experimental cellular and tumor models and which are under evaluation in pre-clinical and early phase clinical trials. Recent evidence from our laboratories has indicated that both compounds were conjugated by several UGT isoforms with the most active being extrahepatic UGT1A10. The present studies were designed to test...
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Mitotic catastrophe followed by necrosis versus pro-survival autophagy - two opposite cellular effects triggered upon C-1311 treatment in MCF-7 cells
PublicationPrzeprowadzone badania miały na celu określenie zdolności imidazoakrydonu C-1311 do indukcji katastrofy mitotycznej, nekrozy i autofagii w komórkach ludzkiego raka piersi MCF-7. Wszystkie eksperymenty przeprowadzone zostały przy stężeniu hamującym proliferację komórek nowotworowych w 80%. Wykazano, że pochodna C-1311 powoduje przejściową akumulację komórek MCF-7 w fazie G2 cyklu życiowego (59% po 48 godz. inkubacji) z równoczesnym...
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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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Exploring the Antitumor Efficacy of N-Heterocyclic Nitrilotriacetate Oxidovanadium(IV) Salts on Prostate and Breast Cancer Cells
PublicationThe crystal structures of two newly synthesized nitrilotriacetate oxidovanadium(IV) salts, namely [QH][VO(nta)(H2O)](H2O)2 (I) and [(acr)H][VO(nta)(H2O)](H2O)2 (II), were determined. Additionally, the cytotoxic effects of four N-heterocyclic nitrilotriacetate oxidovanadium(IV) salts— 1,10-phenanthrolinium, [(phen)H][VO(nta)(H2O)](H2O)0.5 (III), 2,2′-bipyridinium [(bpy)H][VO(nta)(H2O)](H2O) (IV), and two newly synthesized compounds...
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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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CYP3A4 overexpressin enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
PublicationW pracy badano wpływ nadekspresji izoenzymu CYP3A4 na cytotoksyczność i odpowiedź komórkową indukowaną przez przeciwnowotworową pochodną triazoloakrydonu w modelowym układzie komórek CHO: dzikego typu, z nadekspresją reduktazy cytochromu P450 (CHO-HR) oraz z koekspresją reduktazy i izoenzymu CYP3A4 (CHO-HR-3A4). Wykazano, że komórki CHO wykazywały różną wrażliwość na badany związek, a linia CHO-HR okazała się najbardziej wrażliwa,...
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A mechanistically approached review upon assorted cell lines stimulated by athermal electromagnetic irradiation
PublicationThe probable influence of electromagnetic irradiation on cancer treatment has been deduced from the interaction of artificial electromagnetic emissions with biological organisms. Nonetheless, the suspected health effects induced by electromagnetic-based technology imply that such a treatment may contaminate the adjacent healthy cells. Thus, gaining mechanistic insights into the problem is required to avoid athermal health hazards....
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Diamond Nanofilm Normalizes Proliferation and Metabolism in Liver Cancer Cells
PublicationPurpose: Surgical resection of hepatocellular carcinoma can be associated with recurrence resulting from the degeneration of residual volume of the liver. The objective was to assess the possibility of using a biocompatible nanofilm, made of a colloid of diamond nanoparticles (nfND), to fill the side after tumour resection and optimize its contact with proliferating liver cells, minimizing their cancerous transformation. Methods:...
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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the antitumor imidazoacridinone C-1311 in human hepatoma cells
PublicationThere is increasing evidence that the expression level of drug metabolic enzymes affects the final cellular response following drug treatment. Moreover, anti-tumour agents may modulate enzymatic activity and/or cellular expression of metabolic enzymes in tumour cells. We investigated the influence of CYP3A4 overexpression on the cellular response induced by the anti-tumour agent C-1311 in hepatoma cells. C-1311-mediated CYP3A4...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublicationDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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Sequence variants of p21 gene of the MRL/MpJ mouse: a possible association with the deficit of p21 protein and regenerative phenotype.
PublicationThe MRL/MpJ mouse is known for its enhanced regeneration abilities that manifested themselves by scarless ear-hole wound closure. The deficit of p21 found in the MRL is associated with the regenerative capacity as the p21 gene knockout in a mouse strain unrelated to the MRL mouse results in an ear-hole closure effect, similar to that observed in the MRL mouse. Cdkn1a gene encodes p21 protein, a cyclin-dependent kinase inhibitor,...
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Antitumor 1-nitroacridine derivative C-1748 induces significant apoptosis in pancreatic cancer cells.
PublicationPancreatic cancer is the fifth leading cause of cancer death and has the lowest survival rate of any solid cancer in the industrial countries. The poor prognosis of pancreatic cancer results from its tendency for late presentation, aggressive invasion, early metastasis, and resistance to chemotherapy. Gemcitabine still remains the best chemotherapeutic agent available for the treatment of advanced pancreatic cancer. However, gemcitabine...