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Search results for: METABOLIZM LEKÓW
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Comparison of RP-HPLC columns used for determination of nucleoside metabolic patterns in urine of cancer patients
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublicationIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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Structure modification of acridine antitumor agents results in changes of enzymatic activity and gene expression of CYP3A4 isoenzyme in HepG2 cells.
PublicationEkspresja izoenzymu CYP3A4, który zaangażowany jest w metabolizm ok. 60% leków stosowanych klinicznie, może być modulowana przez takie czynniki jak: polimorfizm, czynniki transkrypcyjne oraz obecność ksenobiotyków. Przykładem induktorów genów kodujących izoenzym CYP3A4 jest fenobarbital i rifampicyna, których obecność w organizmie przyspiesza metabolizm innych leków stosowanych jednocześnie, które są substratami dla CYP3A4. Dlatego...
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The Effect of Long-Term Administration of Fatty Acid Amide Hydrolase Inhibitor URB597 on Oxidative Metabolism in the Heart of Rats with Primary and Secondary Hypertension
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Products of Vitamin D3 or 7-Dehydrocholesterol Metabolism by Cytochrome P450scc Show Anti-Leukemia Effects, Having Low or Absent Calcemic Activity
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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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Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism
PublicationIn spite of the current advances and achievements in cancer treatments, colorectal cancer (CRC) persists as one of the most prevalent and deadly tumor types in both men and women worldwide. Drug resistance, adverse side effects and high rate of angiogenesis, metastasis and tumor relapse remain one of the greatest challenges in long-term management of CRC and urges need for new leads of anticancer drugs. We demonstrate that CRC...
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CYP3A4-dependent cellular response does not relate to CYP3A4-catalysed metabolites of C-1748 and C-1305 acridine antitumor agents in HepG2 cells
PublicationHigh CYP3A4 expression sensitizes tumor cells to certain antitumor agents while for others it can lower their therapeutic ef fi cacy. We have elucidated the in fl uence of CYP3A4 overexpression on the cellular response induced by antitumor acridine derivatives, C-1305 and C-1748, in two hepatocellular carcinoma (HepG2) cell lines, Hep3A4 stably transfected with CYP3A4 isoenzyme, and HepC34 expressing empty vector. The compounds...
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The Rate of Improvement in Metabolic Control in Children with Diabetes Mellitus Type 1 on Insulin Glargine Depends on Age
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Emerging Role of Adenylate Kinase 4 as a Metabolic Player Regulating Cellular Hypoxic Responses in Pulmonary Cells
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Effects of Low Concentration of Selected Analgesics and Successive Bioaugmentation of the Activated Sludge on Its Activity and Metabolic Diversity
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Perturbations of the hepatic proteome behind the onset of metabolic disorders in mouse offspring developed following embryo manipulation
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
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Chicken feather keratin as a source of bioactive peptides useful in prevention of metabolic disorders – in silico and in vitro hydrolysis
PublicationProtein derived bioactive peptides not only serve as nutrients but can also exert drug-like activity, e.g. antidiabetic, antihypertensive, or antimicrobial, to name a few. Most biopeptides have beneficial effects on health that make them attractive for nutraceutical applications. The majority of bioactive peptides have been obtained from food proteins, but protein-rich by-products generated by agriculture...
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Primary mediastinal B-cell lymphoma – metabolic and anatomical features in 18FDG-PET/CT and response to therapy
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Cardiovascular, anthropometric, metabolic and hormonal profiling of normotensive women with polycystic ovary syndrome with and without biochemical hyperandrogenism
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29 Metabolic Syndrome and Selected Coronary Heart Disease Risk Factors in the Group of Krakow Adult Residents
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Exposure to non-continuous rotating magnetic field induces metabolic strain-specific response of Komagataeibacter xylinus
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The Co-Culture of Staphylococcal Biofilm and Fibroblast Cell Line: The Correlation of Biological Phenomena with Metabolic NMR1 Footprint
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The Impact of Intraspecies Variability on Growth Rate and Cellular Metabolic Activity of Bacteria Exposed to Rotating Magnetic Field
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Sustainable nitrogen removal in anammox-mediated systems: Microbial metabolic pathways, operational conditions and mathematical modelling
PublicationAnammox-mediated systems have attracted considerable attention as alternative cost-effective technologies for sustainable nitrogen (N) removal from wastewater. This review comprehensively highlights the importance of understanding microbial metabolism in anammox-mediated systems under crucial operation parameters, indicating the potentially wide applications for the sustainable treatment of N-containing wastewater. The partial...
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublicationNew unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of tumor cell lines but also against human tumor xenografts in nude mice. Representative UA compounds, named C-2028, C-2045 and C-2053, were characterized in respect to their physicochemical properties and the following studies aimed to elucidate the role of metabolic transformations in UAs action. We demonstrated with phase I and phase II enzymes...
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Non-Targeted Metabolite Profiling Reveals Host Metabolomic Reprogramming during the Interaction of Black Pepper with Phytophthora capsici
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Prediction of Overall In Vitro Microsomal Stability of Drug Candidates Based on Molecular Modeling and Support Vector Machines. Case Study of Novel Arylpiperazines Derivatives
PublicationOther than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline. The ideal drug candidate should be stable enough to reach its therapeutic site of action. Despite many recent excellent achievements in the field of computational methods supporting drug metabolism studies, a well-recognized procedure to model...
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Amino acids metabolism and degradation is regulated during porcine oviductal epithelial cells (OECs) primary culture in vitro – a signaling pathways activation approach
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Flavin monooxygenases, FMO1 and FMO3, not cytochrome p450 isoenzymes, contribute to metabolism of anti-tumour triazoloacridinone, C-1305, in liver microsomes and HepG2 cells.
PublicationCelem pracy było określenie roli wybranych enzymów frakcji mikrosomalnej komórek wątroby w metabolizmie pochodnej triazoloakrydonu, związku C-1305. Wykazano, że badana pochodna ulega transformacji wobec frakcji enzymów izolowanych z hepatocytów szczurzych i ludzkich oraz jest metabolizowana przez komórki linii HepG2. Badania wykazały ponadto, że enzymami odpowiedzialnymi za obserwowane przemiany były monooksygenazy flawinowe, FMO1...
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Replicating DNA by cell factories: roles of central carbon metabolism and transcription in the control of DNA replication in microbes, and implications for understanding this process in human cells
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Dietary chicory root and chicory inulin trigger changes in energetic metabolism, stress prevention and cytoskeletal proteins in the liver of growing pigs – a proteomic study
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The antitumor derivatives, C1305 and C1748, were different in effects on CYP3A4 expression and catalytic activity in HepG2 cells
PublicationCytochromy P450 (CYP) należą do grupy enzymów biorących udział w 70-80% metabolizmu fazy I większości stosowanych klinicznie leków. Z tego powodu oddziaływanie leków z enzymami cytochromu P450 stało się istotnym elementem w projektowaniu chemoterapeutyków, szczególnie tych, które są stosowane w terapii wielolekowej. Znajomość substratów, induktorów i inhibitorów poszczególnych izoenzymów P450, nie tylko może obniżać częstość występowania...
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Metabolic response of cornflower (Centaurea cyanus L.) exposed to tribenuron-methyl: one of the active substances of sulfonylurea herbicides
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30‐Day morbidity and mortality of bariatric metabolic surgery in adolescence during the COVID‐19 pandemic – The GENEVA study
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Role of adenylate kinase 4 as a new metabolic regulator of pulmonary artery smooth muscle cells under hypoxia
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The metabolic profiles of pterin compounds as potential biomarkers of bladder cancer—Integration of analytical-based approach with biostatistical methodology
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Chiral Pyrazolo[4,3-e][1,2,4]triazine Sulfonamides—Their Biological Activity, Lipophilicity, Protein Affinity, and Metabolic Transformations
PublicationReferring to our previous laboratory results related to the tyrosinase and urease inhibition by pyrazolo[4,3-e][1,2,4]triazine sulfonamides, we examined here in silico the mechanism of action at the molecular level of the investigated pyrazolotriazine sulfonamides by the molecular docking method. The studied compounds being evaluated for their cytotoxic effect against cancer cell lines (MCF-7, K-562) and for recombinant Abl and...
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Electrochemical simulation of metabolic reduction and conjugation reactions of unsymmetrical bisacridine antitumor agents, C-2028 and C-2053
PublicationElectrochemistry (EC) coupled with analysis techniques such as liquid chromatography (LC) and mass spectrometry (MS) has been developed as a powerful tool for drug metabolism simulation. The application of EC in metabolic studies is particularly favourable due to the low matrix contribution compared to in vitro or in vivo biological models. In this paper, the EC(/LC)/MS system was applied to simulate phase I metabolism of the representative...
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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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Biopaliwa z rzepaku. Przygotowanie surowca do otrzymywania biodiesla w warunkach gospodarstwa rolnego oraz pilotowe metanolizy
PublicationScharakteryzowano olej rzepakowy jako surowiec do produkcji biodiesla i opisano etapy procesu transestryfikacji. Oceniono metody wydobywania oleju rzepakowego poprzez tłoczenie w warunkach gospodarstwa rolnego i scharakteryzowano oleje pod względem przydatności do reakcji metanolizy (zawartość fosforu, LK, LOO, skład kwasów tłuszczowych). Przeprowadzono wstępne, laboratoryjne reakcje transestryfikacji i na ich podstawie wytypowano...
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Induction of secondary metabolite production in transformated callus of Ammi majus L. grown after electromagnetic treatment of culture medium
PublicationW pracy przedstawiono wyniki badań, których celem było zbadanie wpływu elicytacji przy użyciu ADR-4, na produkcję metabolitów wtórnych. Elicytacja ADR-4 zwiększyła 2-krotnie zawartość bergaptenu. Porównano również efektywność 3 technik ekstrakcyjnych stosowanych do izolacji feuranokumaryn, kumaryn i ich glikozydów z kalusa A.majus. Ekstrakcja przy użyciu techniki ASE okazała się najbardziej efektywna.
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Electrochemistry/mass spectrometry (EC/MS) for fast generation and identification of novel reactive metabolites of two unsymmetrical bisacridines with anticancer activity.
PublicationThe development of a new drug requires knowledge about its metabolic fate in a living organism, regarding the comprehensive assessment of both drug therapeutic activity and toxicity profiles. Electrochemistry (EC) coupled with mass spectrometry (MS) is an efficient tool for predicting the phase I metabolism of redox-sensitive drugs. In particular, EC/MS represents a clear advantage for the generation of reactive drug transformation...
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Genes encoding proteins regulating fatty acid metabolism and cellular response to lipids are differentially expressed in porcine luminal epithelium during long-term culture
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Protective effect of Aronia melanocarpa polyphenols against cadmium-induced disorders in bone metabolism: A study in a rat model of lifetime human exposure to this heavy metal
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PREVALENCE OF METABOLIC SYNDROME AMONG PATIENTS WITH SCHIZOPHRENIA FROM LONG CARE UNIT IN FORENSIC PSYCHIATRY PROGRAM: AN OBSERVATIONAL STUDY
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“Positive Regulation of RNA Metabolic Process” Ontology Group Highly Regulated in Porcine Oocytes Matured In Vitro: A Microarray Approach
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Cross-linking of sodium caseinate-structured emulsion with transglutaminase alters postprandial metabolic and appetite responses in healthy young individuals
PublicationThe physico-chemical and interfacial properties of fat emulsions influence lipid digestion and may affect postprandial responses. The aim of the present study was to determine the effects of the modification of the interfacial layer of a fat emulsion by cross-linking on postprandial metabolic and appetite responses. A total of fifteen healthy individuals (26·5 (sem 6·9) years and BMI 21·9 (sem 2·0) kg/m2) participated in a cross-over...
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Metabolic Evaluation of Urine from Patients Diagnosed with High Grade (HG) Bladder Cancer by SPME-LC-MS Method
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Toxic potencies of metabolite(s) of non-cylindrospermopsin producing Cylindrospermopsis raciborskii isolated from temperate zone in human white cells
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Dodecanol, metabolite of entomopathogenic fungus Conidiobolus coronatus, affects fatty acid composition and cellular immunity of Galleria mellonella and Calliphora vicina
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Contribution of UDP-glucuronosyltransferases (UGTs) in metabolism of acridinone antitumor agents, C-1311, C-1305, and their less active structural analogues, C-1330 and C-1299
PublicationCelem prowadzonych badań było określenie roli UDP-glukuronylotransferaz, uważanych za najważniejsze enzymy detoksykujące, w metabolizmie pochodnych imidazo- i triazoloakrydonu. Wykazano, że najbardziej aktywne przeciwnowotworowo związki z obu grup, tj. C-1311 i C-1305 są transformowane do O-glukuronidów, w przeciwieństwie do ich metoksylowych analogów, odpowiednio związku C-1330 i C-1299. Analiza składu mieszanin reakcyjnych zawierających...
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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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Metabolic Profiling of Jasminum grandiflorum L. Flowers and Protective Role against Cisplatin-Induced Nephrotoxicity: Network Pharmacology and In Vivo Validation
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