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Wyniki wyszukiwania dla: metabolity
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Human CYP2 family of cytochrome P-450 takes part in metabolism of two acridine antitumor agents, C-1311 and C-1748, selected for I phase of clinical trials
PublikacjaPraca zawiera wyniki badań metabolicznej transformacji przeciwnowotworowych pochodnych akrydyny wobec zestawu 16 prób enzymów mikrosomalnych, pochodzących z wątroby 16 różnych pacjentów. Wykazano, że za metabolizm tych związków u człowieka odpowiedzialne są głównie izoenzymy z rodziny CYP2.
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Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response
PublikacjaActivity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase...
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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
PublikacjaBackground 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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Budesonide treatment of professional athletes and anti-doping testing- case studies
PublikacjaAccording to the World Anti-Doping Agency (WADA) Prohibited List, glucocorticosteroids are prohibited in competition and only when administered by oral, intravenous, intramuscular or rectal routes. Up to now, in order to differentiate whether glucocorticosteroids were administered by one of the prohibited routes or not, a specific reporting limit for urinary concentrations of parent compounds and their metabolites was established...
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Phytochemical screening and biological evaluation of Greek sage (Salvia fruticosa Mill.) extracts
PublikacjaThis study explores the influence of extraction solvents on the composition and bioactivity of Salvia fruticosa extracts. Ultrasound-assisted extraction with water, ethanol and their mixtures in variable proportions was used to produce four different extracts. An untargeted UPLC/MS‑based metabolomics was performed to discover metabolites profile variation between the extracts. In the analyzed samples, 2704 features had been detected,...
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Justyna Płotka-Wasylka dr hab. inż.
OsobyUrodziła się w Słupsku (24.03.1986).W 2005 roku ukończyła I Liceum Ogólnokształcące im. Jana II Sobieskiego w Wejherowie i rozpoczęła studia na Wydziale Chemicznym Politechniki Gdańskiej. Po ich ukończeniu w 2010 rozpoczęła pracę naukową na tej uczelni, uzyskując w 2014 roku stopień doktora nauk chemicznych. Tematem jej rozprawy doktorskiej, wykonywanej pod kierunkiem prof. Marka Biziuka oraz dr Caluma Morrisona (Uniwersytet w...
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ANNALS OF NUTRITION AND METABOLISM
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TRENDS IN ENDOCRINOLOGY AND METABOLISM
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Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation.
PublikacjaThe effectiveness of many anticancer drugs depends on the creation of specific metabolites that may alter their therapeutic or toxic properties. One significant route of biotransformation is a conjugation of electrophilic compounds with reduced glutathione, which can be non-enzymatic and/or catalyzed by glutathione-dependent enzymes. Glutathione usually combines with anticancer drugs and/or their metabolites to form more polar...
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Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes
PublikacjaThe present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase...
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Nuclear Magnetic Resonance Metabolomics Reveals Qualitative and Quantitative Differences in the Composition of Human Breast Milk and Milk Formulas
PublikacjaCommercial formula milk (FM) constitutes the best alternative to fulfill the nutritional requirements of infants when breastfeeding is precluded. Here, we present the comparative study of polar metabolite composition of human breast milk (HBM) and seven different brands of FM by nuclear magnetic resonance spectroscopy. The results of the multivariate data analysis exposed qualitative and quantitative differences between HBM and...
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In Silico Safety Assessment of Bacillus Isolated from Polish Bee Pollen and Bee Bread as Novel Probiotic Candidates
PublikacjaBacillus species isolated from Polish bee pollen (BP) and bee bread (BB) were characterized for in silico probiotic and safety attributes. A probiogenomics approach was used, and in-depth genomic analysis was performed using a wide array of bioinformatics tools to investigate the presence of virulence and antibiotic resistance properties, mobile genetic elements, and secondary metabolites. Functional annotation and Carbohydrate-Active...
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Strategia analizy niecelowanej w metabolomice i lipidomice. Cz. 1. Aspekty praktyczne
PublikacjaStrategia analizy niecelowanej jest powszechnie wykorzystywana do analizy różnego rodzaju próbek biologicznych, takich jak tkanki czy płyny ustrojowe, w celu otrzymania „odcisku palca” oraz określenia różnic w składzie jakościowym oraz ilościowym pomiędzy badanymi próbkami. Wskazanie różnic w zawartości różnych biocząsteczek (peptydy, metabolity, lipidy) pozwala na uzyskanie informacji na temat powiązania składu biochemicznego...
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Novel 5-Substituted 2-(Aylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl)benzenesulfonamides: Synthesis, Molecular Structure, Anticancer Activity, Apoptosis-Inducing Activity and Metabolic Stability
PublikacjaA series of novel 5-substituted 2-(arylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl) benzenesulfonamide derivatives 27–60 have been synthesized by the reaction of aminoguanidines with an appropriate phenylglyoxal hydrate in glacial acetic acid. A majority of the compounds showed cytotoxic activity toward the human cancer cell lines HCT-116, HeLa and MCF-7, with IC50 values below 100 M. It was found that for the analogues 36–38...
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Applied Physiology Nutrition and Metabolism-Physiologie appliquee nutrition et metabolisme
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Agata Kot-Wasik prof. dr hab. inż.
OsobyAgata Kot-Wasik, urodzona w 1964 r. w Siedlcach (woj. mazowieckie), ukończyła studia magisterskie w 1988 r. na Wydziale Chemicznym Politechniki Gdańskiej, w specjalności Analityka Techniczna i Przemysłowa. W latach 1988–1992 była zatrudniona w Katedrze Chemii Organicznej na macierzystym wydziale na stanowisku naukowo-technicznym. W 1990 r. ukończyła na PG studia podyplomowe „Techniki Instrumentalne w Analizie Śladów i Ochronie...
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Phytotoxic Metabolites from Three Neofusicoccum Species Causal Agents of Botryosphaeria Dieback in Australia, Luteopyroxin, Neoanthraquinone, and Luteoxepinone, a Disubstituted Furo-α-pyrone, a Hexasubstituted Anthraquinone, and a Trisubstituted Oxepi-2-one from Neofusicoccum luteum
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A new dilution-enrichment sample preparation strategy for expanded metabolome monitoring of human breast milk that overcomes the simultaneous presence of low- and high-abundance lipid species
PublikacjaThe complex nature of human breast milk (HBM) makes samples difficult to analyze, requiring several extraction techniques and analytical platforms to obtain high metabolome coverage. In this work, we combined liquid-liquid extraction (LLE) and solid-phase extraction (SPE) techniques to prepare HBM samples to overcome the challenge of low- and high-abundance lipid species, enabling the semiquantitative analysis of total HBM lipids...
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Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents
PublikacjaA series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The studied compounds display selective activity mainly against HCT-116 and HeLa cells. Thus, five compounds show selective cytotoxic...
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The role of glucuronidation in drug resistance
PublikacjaThe final therapeutic effect of a drug candidate, which is directed to a specific molecular target strongly depends on its absorption, distribution, metabolism and excretion (ADME). The disruption of at least one element of ADME may result in serious drug resistance. In this work we described the role of one element of this resistance: phase II metabolism with UDP-glucuronosyltransferases (UGTs). UGT function is the transformation...
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NUTRITION METABOLISM AND CARDIOVASCULAR DISEASES
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T cell Activation Is Driven by an ADP-Dependent Glukosinase Linking Enhanced Glycolysis with Mitochondrial Reactive Oxygen Species Generation
PublikacjaMitochondria-originating reactive oxygen species control T cell receptor (TCR)-induced gene expression. Here, we show that TCR-triggered activation of ADP-dependent glucokinase (ADPGK), an alternative, glycolytic enzyme typical for Archaea, mediates generation of the oxidative signal. We also show that ADPGK is localized in the endoplasmic reticulum and suggest that its active site protrudes toward the cytosol. The ADPGK-driven...
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Andrzej Okuniewski dr inż.
OsobyWykształcenie 2010-2014: Katedra Chemii Nieorganicznej, Wydział Chemiczny, Politechnika Gdańskadoktor nauk chemicznych (nauki chemiczne – chemia, chemia nieorganiczna) 2009-2010: Wydział Chemiczny, Politechnika Gdańskamagister chemii (chemia stosowana) 2005-2009: Wydział Chemiczny, Politechnika Gdańskainżynier chemik (chemia stosowana) 2002-2005: II Liceum Ogólnokształcące im. Władysława Pniewskiego w Gdańskuprofil biologiczno-chemiczno-fizyczny...
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Gilmara De Assis Gg Ph.D
OsobyPost-Graduated in Exercise Physiology, my research interest in on brain-derived neurotrophic factor, metabolism, neuroplasticity, and cognition.
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Agnieszka Potęga dr inż.
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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.
PublikacjaEkspresja 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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In Vitro and In Vivo Imaging-Based Evaluation of Doxorubicin Anticancer Treatment in Combination with the Herbal Medicine Black Cohosh
PublikacjaAs a substitution for hormone replacement therapy, many breast cancer patients use black cohosh (BC) extracts in combination with doxorubicin (DOX)-based chemotherapy. In this study, we evaluated the viability and survival of BC- and DOX-treated MCF-7 cells. A preclinical model of MCF-7 xenografts was used to determine the influence of BC and DOX administration on tumor growth and metabolism. The number of apoptotic cells after...
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Determination of phenol biodegradation pathways in three psychrotolerant yeasts, Candida subhashii A011, Candida oregonensis B021 and Schizoblastosporion starkeyi-henricii L012, isolated from Rucianka peatland
PublikacjaIn this study, three psychrotolerant phenol-degrading yeast strains Candida subhashii (strain A011), Candida oregonenis (strain B021) and Schizoblastosporion starkeyi-henricii (strain L012) isolated from Rucianka peatland were examined to determine which alternative metabolic pathway for phenol biodegradation is used by these microorganisms. All yeast strains were cultivated in minimal salt medium supplemented with phenol at 500,...
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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
PublikacjaInduction 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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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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Glycerol and Natural Deep Eutectic Solvents Extraction for Preparation of Luteolin-Rich Jasione montana Extracts with Cosmeceutical Activity
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Systemic Effects of Radiotherapy and Concurrent Chemo-Radiotherapy in Head and Neck Cancer Patients—Comparison of Serum Metabolome Profiles
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The Application of Metabolomics in Forensic Science with Focus on Forensic Toxicology and Time-of-Death Estimation
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A Robust Method for Sample Preparation of Gastrointestinal Stromal Tumour for LC/MS Untargeted Metabolomics
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Serum Cholesteryl Ester Transfer Protein (CETP) and Sortilin (SORT) in Patients with Psoriasis with Relation to Systemic Treatment
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Potential Predictive Value of Serum Pentraxin 3 and Paraoxonase 1 for Cardiometabolic Disorders Development in Patients with Psoriasis—Preliminary Data
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HBM4EU Chromates Study: Urinary Metabolomics Study of Workers Exposed to Hexavalent Chromium
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Changes in the Secretion of Melatonin and Selected Adipokines during the Progression of Parkinson’s Disease—Preliminary Studies
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The Influence of Winter Swimming on Oxidative Stress Indicators in the Blood of Healthy Males
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How Does In Vitro Digestion Change the Amount of Phenolics in Morus alba L. Leaf? Analysis of Preparations and Infusions
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Potential Use of Thalidomide in Glioblastoma Treatment: An Updated Brief Overview
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JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
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Mass spectrometric identification of 13C-Labeled metaboloites during anaerobic propanoic acid oxidation
PublikacjaBiowaste digestion is a possibility to gain biogas as a renewable fuel source. However, the anaerobic food chain may be disrupted by, e.g., substrate overload or by inhibitors, leading to the accumulation of volatile fatty acids (VFAs), predominantly of propanoic acid (PA). VFA Accumulation may cause a rapid pH decrease, less biogas production, or even a total inhibition. To maintain high biogas productivity or to prevent a collapse...
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Badania nad doborem najkorzystniejszego składu eluentu do rozdzielenia metabolitów wtórnych z grupy naftochinonów i flawonoidów z zastosowaniem chromatografii planarnej w normalnym i odwróconym układzie faz = A research on the composition of the eluent for separation of plant metabolities by reversed phase planar chromatography
PublikacjaIn the paper the results of separation of plant extracts by RP-TLC with different composition of the eluents are presented. Analysis of retention data allowed to select components of the eluent with favorable retention parameters, which can be used in the future for separation of this type of plant extracts by column liquid chromatography techniques.
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Bioavailability of Tannins and Other Oligomeric Polyphenols: a Still to Be Studied Phenomenon
PublikacjaPurpose of Review Polyphenols are a group of plant secondary metabolites characterized with the presence ofmultiples of phenol structural units. Tannins are plant originated phenolic substances, which play an important role in plant defense system as well as have found applications in medicine, industry, and other fields of human activity. Despite these, the mechanisms of bioavailability of these substances are poorly studied and...
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Beata Krawczyk dr hab.
Osobydr hab. Beata Krawczyk, prof. uczelni Stopnie naukowe, wykształcenie, kwalifikacje Beata Krawczyk uzyskała tytuł magistra biologii na Wydziale Biologii (wówczas: Wydział Biologii i Nauk o Ziemi), Uniwersytetu Gdańskiego w 1986 roku, a doktorat z biologii molekularnej na Wydziale Biologii (wówczas: Wydział Biologii, Geografii i Oceanologii) Uniwersytetu Gdańskiego w 1996 roku. Stopień doktora habilitowanego w zakresie nauk biologicznych...
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C-1305 inactivation of recombinant human cytochrome P450, CYP1A2 and CYP3A4, is due to mechanism-based inhibition
PublikacjaPodjęto próbę określenia mechanizmu obserwowanej inhibicji izoenzymów CYP1A2 i CYP3A4 przez pochodną triazoloakrydonu C-1305.W pierwszym kroku stwierdzono, że hamowanie aktywnosci obu enzymów jest procesem nieodwracalnym. W kolejnych etapach badań wykazano między innymi, że obecność NADPH zwiększa istotnie stopień obserwowanej inhibicji, co wskazało, że mamy do czynienia z inhibicją samobójczą opartą na mechanizmie działania (ang....
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Novel Resveratrol-Based Substrates for Human Hepatic, Renal, and Intestinal UDP-Glucuronosyltransferases
PublikacjaTrans-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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Meconium analysis as a promising diagnostic tool for monitoring fetal exposure to toxic substances: Recent trends and perspectives
PublikacjaPrenatal exposure to toxic substances is an important public health problem. Many biological specimens obtained from the fetus or mother are used for biomonitoring. Each material reflects exposure in a specific time period and has different advantages and disadvantages in terms of accuracy, time window of detection and cost/benefit ratio. Recently, meconium has become the matrix of choice in toxicology screening for detecting exposure...
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Stimulation of antibacterial napthoquinones and flavonoids accumulation in carnivorous plants grown in vitro by addition of elicitors
PublikacjaRośliny owadożerne (D. muscipula, D. capensis) zawierają dwie grupy farmakologicznie czynnych substancji - naftochinony: plumbagina, ramentaceon, oraz flawonoidy: kwercetyna i mirycetyna. Na wzrost akumulacji tychże substancji w tkankach roślin owadożernych ma wpływ dodatek elicytora. Zbadano wpływ następujących elicytorów na zawartość metabolitów o znaczeniu farmaceutycznym: kwas jaśminowy oraz lizat Agrobacterium rhizogenes....