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Wyniki wyszukiwania dla: ANTI-TUMOUR IMIDAZOACRIDINONE
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Stratification of nano-pigments in anti-corrosive coatings by means of magnetic field
PublikacjaThe concept of self-stratification of coatings, although attractive, causes difficulties in its practical use, especially when pigments are added to the resins. An alternative way of obtaining a multilayer structure in a single step was presented. Using the inhomogeneous magnetic field and magnetically active components of the coating, the possibility of vertically graded differentiation of the one layer properties has been verified....
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Intercalation complex of imidazoacridinone C-1311, a potential anticancer drug, with DNA helix d(CGATCG)2: stereostructural studies by 2D NMR spectroscopy.
PublikacjaImidazoacridinone C-1311 (Symadex®) is a powerful antitumor agent, which successfully made its way through the Phase I clinical trials and has been recommended for Phase II few a years ago. It has been shown experimentally that during the initial stage of its action C-1311 forms a relatively stable intercalation complex with DNA, yet it has shown no base-sequence specificity while binding to DNA. In this paper, the d(CGATCG)2:C-1311...
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Interaction of the conserved region 4.2 of sigma(E) with the RseA anti-sigma factor
PublikacjaEo-E RNA polymerase transcribes a regulon of folding factors for the bacterial envelope and is induced by physical and chemical stresses. The RseA anti-sigma factor inhibits the activity of Esigma(E) RNA, polymerase. It is shown here that the N-terminal portion of sigma(E), residues 1-153, binds core RNA polymerase. RseA interacts with residues 154-191 of sigma(E), a site that is homologous to region 4, the sigma factor binding...
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The significance of VEGF-C/VEGFR-2 interaction in the neovascularization and prognosis of nephroblastoma (Wilms' tumour)
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A Robust Method for Sample Preparation of Gastrointestinal Stromal Tumour for LC/MS Untargeted Metabolomics
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Biomass-Derived Nitrogen Functionalized Carbon Nanodots and Their Anti-Biofouling Properties
PublikacjaThe prevalence of the antibiotic resistant bacteria remains a global issue. Cheap, sustainable and multifunctional antibacterial membranes are at the forefront of filtrating materials capable of treating multiple flow streams, such as water cleansing treatments. Carbon nanomaterials are particularly interesting objects shown to enhance antibacterial properties of composite materials. In this article, amino-functionalized, photoluminescent...
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M-integral for finite anti-plane shear of a nonlinear elastic matrix with rigid inclusions
PublikacjaThe path-independent M-integral plays an important role in analysis of solids with inhomogeneities. However, the available applications are almost limited to linear-elastic or physically non-linear power law type materials under the assumption of infinitesimal strains. In this paper we formulate the M-integral for a class of hyperelastic solids undergoing finite anti-plane shear deformation. As an application we consider the problem...
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Tiliroside Combined with Anti-MUC1 Monoclonal Antibody as Promising Anti-Cancer Strategy in AGS Cancer Cells
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Apoptosis of human leukemia cells induced by imidazoacridinone derivative C-1311 (Symadex)
PublikacjaPraca dotyczy różnej wrażliwości komórek białaczek ludzkich do ulegania apoptozie pod wpływem pochodnej imidazoakrydonu C-1311, co jest zgodne z aktywnością cytotoksyczną tego związku (EC90) wobec badanych komórek.
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The Imidazoacridinone Antitumor Drug, C-1311, Is Metabolized by Flavin Monooxygenases but Not by Cytochrome P450s.
PublikacjaPrezentowane w publikacji wyniki badań mają na celu wyjaśnienie roli enzymów wątrobowych w metabolizmie przeciwnowotworowych pochodnych C-1311 oraz C-1330. Oba związki inkubowane były z frakcją mikrosomalną oraz enzymami rekombinantowymi należącymi do grypy cytochromu P450, FMO oraz UGT. Badania wykazały, że oba związki są metabolizowane przez enzymy frakcji mikrosomalnej, ale nie przez enzymy cytochromu P450. Aktywność enzymatyczna...
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Molecular mechanism of the enzymatic oxidation investigated for imidazoacridinone antitumor drug C-1311.
PublikacjaPraca miala na celu określenie molekularnego mechanizmu enzymatycznej utleniającej aktywacji wymienionego związku przeciwnowotworowego w takim układzie modelowym, w którym wcześniej wykazano jego kowalencyjne wiązanie się do DNA. Badania struktur chemicznych produktów enzymatycznej aktywacji wykazały, że dwa z nich powstają w wyniku dealkilacji łańcucha bocznego cząsteczki, natomiast dwa inne w wyniku aktywacji pierścienia imidazoakrydonu....
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Volatile organic compounds in gastrointestinal stromal tumour tissue originating from patient-derived xenografts
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Anti-plane shear waves in an elastic strip rigidly attached to an elastic half-space
PublikacjaWe consider the anti-plane shear waves in a domain consisting of an infinite layer with a thin coating lying on an elastic half-space. The elastic properties of the coating, layer, and half-space are assumed to be different. On the free upper surface we assume the compatibility condition within the Gurtin–Murdoch surface elasticity, whereas at the plane interface we consider perfect contact. For this problem there exist two possible...
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Preparation, characterization and anti-colitis activity of curcumin-asafoetida complex encapsulated in turmeric nanofiber
PublikacjaUlcerative colitis (UC) is a main form of inflammatory bowel disease (IBD). Asafoetida (ASF) and turmeric have traditionally been used for the treatment of various inflammatory diseases, including UC, because ASF is rich in sulfur compounds and turmeric contains curcumin (CUR). Turmeric nanofiber (TNF), the modified cell wall component of turmeric is considered to play important role in the human diet, health and can be used as...
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Optimization of Cyclodextrin-Assisted Extraction of Phenolics from Helichrysum italicum for Preparation of Extracts with Anti-Elastase and Anti-Collagenase Properties
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Metabolic transformations of antitumor imidazoacridinone, C-1311, with microsomal fractions of rat and human liver
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Metabolic transformations of antitumor imidazoacridinone, C-1311, with microsomal fractions of rat and human liver
PublikacjaWykazano, że enzymatyczna aktywacja jest konieczna dla aktywności biologicznej pochodnej C-1311 (Symadex R), która znajduje się w II fazie badań klinicznych. Zbadano przemiany enzymatyczne tego związku w obecności frakcji enzymatycznych mikrosomalnych komórek wątroby szczura i ludzkiej. Badania te wykazały, że związek C-1311 jest bardziej podatny na przemiany w obecności frakcji mikrosomalnej niż S9 i cytozolowej. Inkubacja związku...
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The products of electro- and photochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinone derivatives
PublikacjaBadano reakcje elektrochemicznego utleniania 2-hydroksyakrydonu, związku modelowego aktywnych przeciwnowotworowo pochodnych imidazoakrydonu. Do badań zastosowano metody woltamperometrii cyklicznej, metodę spektroelektrochemiczną oraz elektrolizę przy kontrolowanym potencjale. Badano też reakcje fotochemicznego utleniania. Badania prowadzono w ramach szerszego problemu poznania przemian aktywacji metabolicznej pochodnych hydroksyakrydonu...
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On the influence of a surface roughness on propagation of anti-plane short-length localized waves in a medium with surface coating
PublikacjaWe discuss the propagation of localized surface waves in the framework of the linear Gurtin–Murdoch surface elasticity and taking into account a roughness of a free boundary. We derive a boundary-value problem for anti-plane motions with curvilinear boundary and surface stresses. Using the asymptotic technique developed earlier, we obtain the form of a localized wave and analyze its amplitude evolution. As the main result we present...
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Preliminary design of the last stage of supercritical steam turbine and proposition of anti-erosion coating for blades surface
PublikacjaIn this article a preliminary design of the last stage of supercritical steam turbine has been presented. A computational model of supercritical thermal cycle has been created in order to determine steam parameters at the stage inlet and outlet. The model was based on the structure of German coal-fired power plant Datteln 4. Further steam-flow parame-ters and dimensions of stator and rotor blades have been calculated analytically....
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Coumarins modulate the anti-glioma properties of temozolomide
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The potential anti-tumor activity of neoteric solvents
PublikacjaCiecze jonowe stały się obiektem zainteresowania naukowców. Znajdują one coraz to szersze zastosowanie. Dlatego też ważne jest określenie ich właściwości Eko-toksycznych. Aktywność anty-nowotworowa i cytotoksyczna cieczy jonowych stała się zatem ważnym aspektem badań. Artykuł podsumowuje najnowsze wyniki badań nad cytotoksycznością tych rozpuszczalników
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C-1311 (Symadex), a potential anti-cancer drug, intercalates into DNA between A and G moieties. NMR-derived and MD-refined stereostructure of the d(GAGGCCTC) 2 :C-1311 complex
PublikacjaImidazoacridinone C-1311 (Symadex®) is an antitumor agent which has been recommended for Phase II clinical trials a few years ago. Previously, it was shown experimentally that during the initial stage of its action C-1311 forms stable intercalation complexes with DNA duplexes. Herein, a NMR-derived stereostructure of d(GAGGCCTC)2:C-1311 complex was reported. The ligand was found locating itself between A and G moieties, forming...
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Spectrum of Epithelial-Mesenchymal Transition Phenotypes in Circulating Tumour Cells from Early Breast Cancer Patients
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Immunization with an anti-idiotypic antibody against the broadly lipopolysaccharide-reactive antibody WN1 222-5 induces Escherichia coli R3-core-type specific antibodies in rabbits
PublikacjaThe mouse monoclonal antibody (mAb) WN1 222-5 recognizes a carbohydrate epitope in the inner core region of LPS that is shared by all strains of Escherichia coli and Salmonella enterica and is able to neutralize their endotoxic activity in vitro and in vivo. Immunization of mice with mAb WN1 222-5 yielded several anti-idiotypic mAbs one of which (mAb S81-19) competitively inhibited binding of mAb WN1 222-5 to E. coli and Salmonella...
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Theoretical Encapsulation of Fluorouracil (5-FU) Anti-Cancer Chemotherapy Drug into Carbon Nanotubes (CNT) and Boron Nitride Nanotubes (BNNT)
PublikacjaIntroduction: Chemotherapy with anti-cancer drugs is considered the most common approach for killing cancer cells in the human body. However, some barriers such as toxicity and side effects would limit its usage. In this regard, nano-based drug delivery systems have emerged as cost-effective and efficient for sustained and targeted drug delivery. Nanotubes such as carbon nanotubes (CNT) and boron nitride nanotubes (BNNT) are promising...
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Imidazoacridinone C-1311 induces both autophagy and senescence in human lung cancer A549 cells
PublikacjaNiedrobnokomórkowy rak płuc (ang. NSCLC, non-small cell lung cancer), stanowiący blisko 80-87% wszystkich przypadków, jest najczęściej występującą formą raka płuc. Skuteczność dotychczas stosowanych chemoterapeutyków w stosunku do tej formy raka jest bardzo ograniczona dlatego poszukuje się nowych związków o lepszych właściwościach leczniczych. Imidazoakrydon C-1311 wykazuje wysoką aktywność cytotoksyczną wobec komórek niedrobnokomórkowego...
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The studies of imidazoacridinone antitumor agent, C-1311, in the field of metabolic transformations with cytochrome P450 isoenzymes
PublikacjaPraca zawiera wyniki badań metabolicznej transformacji przeciwnowotworowej pochodnej imidazoakrydonu C-1311 wobec rekombinantowych ludzkich izoenzymów P450. Związek nie ulegał transformacji w badanych warunkach, natomiast wykazano, że ma zdolność hamowania aktywności izoezymów CYP1A2 i CYP3A4.
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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublikacjaMultidrug 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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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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Analysis of passenger car crash with a cable barrier installed with anti-glare screens on a horizontal convex road curve with 400 m radius
PublikacjaHigh-tension cable barriers have been used on roads for a relatively short period compared with other types of road barriers. Hence, there remains a need for further research on various crash scenarios. An important issue is the performance of a cable barrier on a road curve, particularly when a vehicle impacts the convex side of the barrier. To address this issue, the analysis in this study considers a system of anti-glare screens...
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Effective anti-plane properties of piezoelectric fibrous composites
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A Method of Fast and Simultaneous Calibration of Many Mobile FMCW Radars Operating in a Network Anti-Drone System
PublikacjaA market for small drones is developing very fast. They are used for leisure activities and exploited in commercial applications. However, there is a growing concern for accidental or even criminal misuses of these platforms. Dangerous incidents with drones are appearing more often, and have caused many institutions to start thinking about anti-drone solutions. There are many cases when building stationary systems seems to be aimless...
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From the pills to environment – Prediction and tracking of non-steroidal anti-inflammatory drug concentrations in wastewater
PublikacjaThe extend of environment pollution by pharmaceuticals is in a stage that required more automatic and integrated solutions. The non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most popular pharmaceutical in the world and emerging pollutants of natural waters. The aim of the paper was to check the correlation of the sales data of selected NSAIDs (ibuprofen, naproxen, diclofenac) and their concentration in the WWTP...
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Sequential induction of mitotic catastrophe followed by apoptosis in human leukemia MOLT4 cells by imidazoacridinone C-1311
PublikacjaWykazano, że pochodna imidazoakrydonu C-1311 indukuje zahamowanie progresji komórek MOLT4 w fazie G2M cyklu życiowego. Podwyższona ekspresja fosfoepitopu MPM-2 przy jednoczesnym zaniku ufosforylowanej formy Tyr15-cdc2 wskazywała, iż komórki początkowo zablokowane w fazie G2 przechodziły do mitozy. Jednocześnie na skutek nieprawidłowego przebiegu mitozy komórki ulegały katastrofie mitotycznej. Analiza biochenicznych markerów apoptozy...
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Electrochemical simulation of metabolism for antitumor-active imidazoacridinone C-1311 and in silico prediction of drug metabolic reactions
PublikacjaThe metabolism of antitumor-active 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) has been investigated widely over the last decade but some aspects of molecular mechanisms of its metabolic transformation are still not explained. In the current work, we have reported a direct and rapid analytical tool for better prediction of C-1311 metabolism which is based on electrochemistry (EC) coupled on-line with electrospray...
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Keratin 7 expression in lymph node metastases but not in the primary tumour correlates with distant metastases and poor prognosis in colon carcinoma
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Analysis of Mitochondrial Genome from Labrador (Canis lupus familiaris) with Mammary Gland Tumour Reveals Novel Mutations and Polymorphisms
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Flowers and Leaves Extracts of Stachys palustris L. Exhibit Stronger Anti-Proliferative, Antioxidant, Anti-Diabetic, and Anti-Obesity Potencies than Stems and Roots Due to More Phenolic Compounds as Revealed by UPLC-PDA-ESI-TQD-MS/MS
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Yeast as a Model to Characterize Anti-Aging Potential of Flavonoids (poster)
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Yeast as a Model to Characterize Anti-Aging Potential of Flavonoids (poster)
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Yeast as a Model to Characterize Anti-Aging Potential of Flavonoids (poster)
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Vitamin D and its analogs as anticancer and anti-inflammatory agents
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Inkjet Printing of Lanthanide–Organic Frameworks for Anti-Counterfeiting Applications
PublikacjaPhotoluminescent lanthanide−organic frameworks (Ln-MOFs) were printed onto plastic and paper foils with a conventional inkjet printer. Ln-MOF inks were used to reproduce color images that can only be observed under UV light irradiation. This approach opens a new window for exploring Ln-MOF materials in technological applications, such as optical devices (e.g., lab-on-a-chip), as proof of authenticity for official documents.
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Anti-inflammatory Activity and Phytochemical Profile of Galinsoga Parviflora Cav.
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Imidazoacridinone antitumor agent, c-1311, as a selective mechanism-based inactivator of human recombinant cytochrome P450 1A2
PublikacjaPrzedmiotem badań była przeciwnowotworowa pochodna imidazoakrydonu, C-1311, która pod nazwą Symadex R, znajduje się aktualnie w II fazie badań klinicznych. Wcześniejsze wyniki pozwoliły stwierdzić, że związek ten jest selektywnym inhibitorem niektórych enzymów cytochromowych. Podjęto zatem próbę wyjaśnienia mechanizmu inhibicji izoenzymów cytochromu P450 przez C-1311. Wykazano, że utrata aktywności katalitycznej obu izoenzymów...
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Morphological and cellular alternations of HepG2 cells overexpressing CYP3A4 after treatment with antitumor imidazoacridinone derivative C-1311
PublikacjaW 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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The imidazoacridinone C-1311 induces p53-dependent senescence or p53-independent apoptosis and sensitizes cancer cells to radiation
PublikacjaC-1311 is a small molecule, which has shown promise in a number of preclinical and clinical studies. However, the biological response to C-1311 exposure is complicated and has been reported to involve a number of cell fates. Here, we investigated the molecular signaling which determines the response to C-1311 in both cancer and non-cancer cell lines. For the first time we demonstrate that the tumor suppressor, p53 plays a key role...
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Influence of narrowband ultraviolet B phototherapy on serum tumour necrosis factor-like weak inducer of apoptosis (TWEAK) in patients with psoriasis
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Capecitabine and temozolomide combination for treatment of high-grade, well-differentiated neuroendocrine tumour and poorly-differentiated neuroendocrine carcinoma — retrospective analysis
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