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Search results for: ANTI-TUMOR AGENT
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Mechanism-based inactivation of human cytochrome P450 1A2 and 3A4 isoenzymes by antitumor triazoloacridinone C-1305.
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, is a promising antitumor therapeutic agent with high activity against several experimental tumors. It was determined to be a potent and selective inhibitor of liver microsomal and human recombinant cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1305 might modulate the effectiveness of other drugs used in multidrug therapy. The objective of this study was...
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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublicationInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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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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Electrochemical formation of the adduct between antitumor agent C_1311 and DNA nucleoside dG. 75.
PublicationPrzyjmuje się, że metaboliczna aktywacja przeciwnowotworowej pochodnej C_1311 jest procesem koniecznym dla jej aktywności przeciwnowotworowej. Wykazano wcześniej, że taka aktywacja prowadzi do kowalencyjnego wiązania się leku z DNA w komórce nowotworowej. Aby zbadać molekularny mechanizm powyższej reakcji metabolicznej przeprowadzono badania elektrochemicznego utleniania pochodnej C_1311. Wykazano w pracy, że dwa produkty elektrochemicznego...
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Softwood-lignin/natural rubber composites containing novel plasticizing agent: Preparation and characterization
PublicationComposite materials based on natural rubber were obtained by using glycerolysate (decomposition prod- uct of polyurethane) as a novel plasticizer. In order to determine the effect of various lignin content, four different filler amounts were used, namely, 5 phr (parts per 100 parts of natural rubber) of lignin (WLI5G), 10 phr (WLI10G), 20 phr (WLI20G), and 40 phr (WLI40G). The reference specimen without lignin (WLI0G) was also...
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Experimental Evaluation of the Agent-Based Population Learning Algorithm for the Cluster-Based Instance Selection
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Conversion of Biomass and Municipal Wastes into Syngas and Hydrogen using Highly Preheated Agent (HTAG)
PublicationGasification is considered to be one of the most promising energy recovery technologies for the widespread utilization of biomass and wastes. During this process raw feedstock is converted into a combustible gas, which can then be burnt to produce thermal energy, or to run engines for mechanical or electrical power. The studies of biomass gasification demonstrate it as a friendly alternative to fossil fuels as one of renewable...
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Milky Sap of Greater Celandine (Chelidonium majus L.) and Anti-Viral Properties
PublicationThe milky juice of the greater celandine herb has been used in folk medicine and in homeopathy for treatment of viral warts for years. However, classical medicine fails to use properties of celandine herbs in treatment of diseases induced by papilloma viruses. Nevertheless, dermatological outpatient clinics are regularly visited by patients reporting efficacy of milky sap isolated from celandine herb in treatment of their own...
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Silybum marianum glycerol extraction for the preparation of high-value anti-ageing extracts
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New Flavone C-Glycosides from Scleranthus perennis and Their Anti-Collagenase Activity
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Fabrication of anti-corrosion nitrogen doped graphene oxide coatings by electrophoretic deposition
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Parallel in vitro and in silico investigations into anti-inflammatory effects of non-prenylated stilbenoids
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Developing electrochemical measurements in order to assess anti-corrosive coatings more effectively
PublicationCelem pracy było sprawdzenie powtarzalności wyników uzyskanych metodą pomiaru szumu (Electrochemical Noise method - ENM) elektrochemicznego wykonanych na powłokach organicznych w konfiguracji bez połączenia z podłożem metalowym (NOCS - No Connection to the Substrate). NOCS polega na wykonaniu pomiarów na trzech teoretycznie takich samych obszarach badanego układu. W takim układzie nie jest wymagane połączenie elektryczne z metalowym...
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SYNTHESIS OF PHOSPHORUS TACRINE ANALOGUES AS A NEW POTENTIAL ANTI-ALZHEIMER’S DISEASE AGENTS
PublicationA series of novel phosphorus tacrine derivatives was obtained in three steps, including synthesis of 9-chlorotacrine, connection of 9-chlorotacrine with hexamethylenediamine, 1,8-diaminooctane and 1,12-diaminododecane linkers and reaction of obtained tacrine diamine analogues with corresponding acid ester to give nine tacrine organophosphorus compounds. All of the obtained final structures were characterized by 1H NMR, 13C NMR,...
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Effect of the Sorption Layer on the Protection Time Provided by Anti-Smog Half-Masks
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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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DNA structure and integrity checkpoints in the cell cycle and their role in drug targeting and resistance of tumor cells to anticancer treatment
PublicationW artykule dokonaliśmy przeglądu literatury dotyczącej różnych typów uszkodzeń DNA indukowanych przez różne czynniki terapeutyczne w komórkach nowotworowych. Omówiliśmy także w jaki sposób aktywują różne typy punktów kontrolnych w cyklu komórkowym i w jaki sposób punkty te są regulowane przez inne szlaki sygnalizacji wewnątrzkomórkowej takie jak szlaki naprawy uszkodzeń DNA, stresu komórkowego i śmierci-przeżycia. W szczególności...
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Synthesis of new antrapyridazone derivatives - a novel group of anticancer agents active on a multidrugresistant(MDR) tumor cell lines
PublicationNovel antrapyridazone derivatives were synthesized and biologically evaluated in order tobroaden the data on structure-activity relationship of this class of cytostatics. Recent literaturedata prove that acetamides react better with aryl chlorides. A new approach based onintroduction of other amides form into aromatic ring in Ullmann was tested. This new methodcould give better yields and make purification step more convenient.
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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublicationA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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The effect of roasting beetroot and chicory on the anti-oxidative activity of their extracts
Open Research DataThe eThe data set presents the results of the assessment of the impact of roasting raw materials in the form of beetroot and chicory on their antioxidant activity measured by the standard ABTS and DPPH radical tests. The numerical results were compared with the visual assessment of the roasted raw materials. The obtained results confirmed the increase...
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Phenylalanine-Based AMPA Receptor Antagonist as the Anticonvulsant Agent with Neuroprotective Activity—In Vitro and In Vivo Studies
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The studies of imidazoacridinone antitumor agent, C-1311, in the field of metabolic transformations with cytochrome P450 isoenzymes
PublicationPraca 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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Application of agent-based simulated annealing and tabu search procedures to solving the data reduction problem
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SELECTING A REPRESENTATIVE DATA SET OF THE REQUIRED SIZE USING THE AGENT-BASED POPULATION LEARNING ALGORITHM
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From tryptophan to novel mitochondria-disruptive agent, synthesis and biological evaluation of 1,2,3,6-tetrasubstituted carbazoles
PublicationMitochondrial targeting plays an important role in anticancer therapy. The Mn(III)-promoted cyclization of 5- (1H-indol-3-yl)-3-oxopentanoic acid allow to obtain novel substituted carbazole derivatives that can act as mitochondria-disruptive agents. The starting materials used for the synthesis of these new aminocarbazoles are oxopentanoate derivatives of tryptophan. The scope and limitation of this method of synthesis are determined...
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Rapana thomasiana hemocyanin modified with ionic liquids with enhanced anti breast cancer activity
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Evaluation of the anti-tyrosinase activity of extracts and rare flavonoids from Scleranthus perennis L.
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In vitro antioxidant, anti-inflammatory activities and acetylcholinesterase inhibition properties of selected plant extracts
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Determination of anti-tyrosinase activity of acetone extracts from selected Potentilla L. species.
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Fulminant hepatic failure in woman with iron and non-steroidal anti-inflammatory drug intoxication
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The Action Mechanisms, Anti-Cancer and Antibiotic-Modulation Potential of Vaccinium myrtillus L. Extract
PublicationHerbal medicinal products containing Vaccinium myrtillus L. (bilberry) fruits and fruit extracts are widely available in the market. Although bilberry leaves and stems are considered as bio-waste, they contain much higher levels of phenolic compounds than fruits. The study aimed to investigate the antimicrobial and anticancer potential of aerial part extracts from Vaccinium myrtillus L. (V. myrtillus, VM) plants harvested at high...
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Ornamental Flowers Grown in Human Surroundings as a Source of Anthocyanins with High Anti-Inflammatory Properties
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Polyoxygenated cyathane diterpenoids from the mushroom Cyathus africanus, and their neurotrophic and anti-neuroinflammatory activities
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Non-steroidal anti-inflammatory drugs are safe with respect to the transcriptome of human dermal fibroblasts
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The enhancement of anti-staphylococcal potential of plant derived naphthoquinones as a result of combination with silver nanoparticles
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Large nonsaturating magnetoresistance, weak anti-localization, and non-trivial topological states in SrAl2Si2
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Non-destructive inspection of anti-corrosion protective coatings using optical coherent tomography
PublicationW artykule przedstawiono zastosowanie optycznej tomografii koherentnej (OCT) do badania antykorozyjnych powłok ochronnych. Omówiono właściwości optycznej interferometrii niskokoherentnej jako zastosowanej metody pomiarowej, opisano budowę pomiarowego systemu OCT, zbudowanego w Katedrze Metrologii i Optoelektroniki WETI PG. Przy pomocy zrealizowanego systemu przebadano grupę powierzchni metalicznych pokrytych różnymi powłokami antykorozyjnymi....
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Identification of High-Risk Stage II Colorectal Tumors by Combined Analysis of the NDRG1 Gene Expression and the Depth of Tumor Invasion
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Expression of stem cell and mesenchymal markers in circulating tumor cells is associated with poor prognosis of early breast cancer patients
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Tumor infiltrating lymphocyte signature is associated with single nucleotide polymorphisms and predicts survival in esophageal squamous cell carcinoma patients
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Anti-cancer effect of Rumex obtusifolius in combination with arginase/nitric oxide synthase inhibitors via downregulation of oxidative stress, inflammation, and polyamine synthesis
PublicationCancer continues to be a leading cause of death worldwide, making the development of new treatment methods crucial in the fight against it. With cancer incidence rates increasing worldwide, ongoing research must focus on identifying new and effective ways to prevent and treat the disease. The combination of herbal extracts with chemotherapeutic agents has gained much interest as a novel strategy to combat cancer. Rumex obtusifolius...
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Whole genome sequencing of Fowl aviadenovirus A - a causative agent of gizzard erosion and ulceration, in adult laying hens
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Institution of the health care agent in Polish legislation: position of the Polish Working Group on End-of-Life Ethics
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Isoform-specific inhibition of DNA topoisomerase II as the mechanism of action of novel anticancer agent C-1305
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The overexpression of CPR and P450 3A4 in pancreatic cancer cells changes the metabolic profile and increases the cytotoxicity and pro-apoptotic activity of acridine antitumor agent, C-1748
PublicationDrug resistance is one of the major cause of pancreatic cancer treatment failure. Thus, it is still imperative to develop new active compounds and novel approach to improve drug efficacy. Here we present 9-amino-1-nitroacridine antitumor agent, C-1748, developed in our laboratory, as a candidate for pancreatic cancer treatment. We examined (i) the cellular response of pancreatic cancer cell lines: Panc-1, MiaPaCa-2, BxPC-3 and...
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A novel green one-step synthesis of gold nanoparticles using crocin and their anti-cancer activities
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Compression and Fatigue Testing of High-Strength Thin Metal Sheets by Using an Anti-Buckling Device
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Potentiation of the anti-tumour effects of Photofrin®-based photodynamic therapy by localized treatment with G-CSF
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In Vitro Screening for Anti-Acetylcholinesterase and Antioxidant Activities of Hottonia palustris L. Extracts and Their Unusual Flavonoids
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Tuning of the Anti-Breast Cancer Activity of Betulinic Acid via Its Conversion to Ionic Liquids
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