Search results for "METABOLITES"

showing 10 items of 182 documents

Total phenolic content in brown algae from the Sicilian coast

2019

Phlorotannins are polyphenolic secondary metabolites found in almost all brown algae that function as defense against grazers, pathogens and epiphytes but are also involved in photoprotection mechanisms. These com- pounds, produced in the Golgi apparatus, are accumulated in cytoplasm, within vesicules called physodes, or bound to the cell wall. The concentration of phlorotannins differs within and between species, shows geograph- ical variations but may be also affected by abiotic or biotic factors. We present here an overview of the studies carried out on total phenolic content in brown algae collected along the north-western coast of Sicily. The aims of these studies were in particular a)…

Settore BIO/02 - Botanica Sistematicasecondary metabolites phenols brown algae Mediterranean SeaSettore BIO/03 - Botanica Ambientale E Applicata
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Charged Tags for the Identification of Oxidative Drug Metabolites Based on Electrochemistry and Mass Spectrometry

2020

Abstract Most of the active pharmaceutical ingredients like Metoprolol are oxidatively metabolized by liver enzymes, such as Cytochrome P450 monooxygenases into oxygenates and therefore hydrophilic products. It is of utmost importance to identify the metabolites and to gain knowledge on their toxic impacts. By using electrochemistry, it is possible to mimic enzymatic transformations and to identify metabolic hot spots. By introducing charged‐tags into the intermediate, it is possible to detect and isolate metabolic products. The identification and synthesis of initially oxidized metabolites are important to understand possible toxic activities. The gained knowledge about the metabolism will…

Spectrometry Mass Electrospray IonizationAlkylationPyridinesElectrospray ionizationPyridinium CompoundsMass spectrometryHydroxylationlcsh:Chemistrydrug metabolitesCytochrome P-450 Enzyme Systemcharged tagsChromatography High Pressure Liquidmass spectrometrychemistry.chemical_classificationActive ingredientChromatographybiologyCommunicationanodic oxidationCytochrome P450General ChemistryMetabolismElectrochemical TechniquesMonooxygenaseCommunicationsEnzymelcsh:QD1-999chemistryelectrochemistrybiology.proteinOxidation-ReductionDrug metabolismMetoprololSignal TransductionChemistryOpen
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Genotoxic and endocrine activities of bis(hydroxyphenyl)methane (bisphenol F) and its derivatives in the HepG2 cell line

2008

International audience; Human can be exposed to bis(hydroxyphenyl)methane (bisphenol F or BPF) and its derivatives as environment and food's contaminants. This study was investigated to identify and to compare toxic potency of BPF, BFDGE, and two of BPF metabolites using in vitro methods. BPF did not induce any genic mutation in bacteria when the Ames test was performed according to the OECD guideline. In contrast, using Human cell lines and Comet assay, we demonstrated that BPF and Bisphenol F Diglycidyl Ether (BFDGE) were effective on HepG2 cell DNA fragmentation at non-cytotoxic concentrations. DHB was also positive but at higher concentrations, near its limit of solubility. Neither BPF,…

StereochemistryCell SurvivalEndocrine activitiesOxidative BPF metabolitesBisphenol F Diglycidyl Ether (BFDGE)[SDV.TOX.TCA]Life Sciences [q-bio]/Toxicology/Toxicology and food chain010501 environmental sciencesEndocrine DisruptorsToxicologymedicine.disease_causeTransfection01 natural sciencesAmes testCell Line03 medical and health scienceschemistry.chemical_compoundHuman cell linesmedicineHumansEstrogens Non-SteroidalBenzhydryl CompoundsBisphenol F (BPF)Bisphenol A diglycidyl ether030304 developmental biology0105 earth and related environmental sciences0303 health sciencesMicronucleus TestsMutagenicity TestsAndrogen AntagonistsMolecular biologyIn vitro3. Good healthComet assaychemistryCell cultureMicronucleus testDNA fragmentationComet AssayGenotoxicityGenotoxicityMutagens
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Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.

2015

Five new compounds, 4-O-geranylisoliquiritigenin (1), 12-dihydrousararotenoid B (2), 12-dihydrousararotenoid C (3), 4'-O-geranyl-7-hydroxyflavanone (4), and 4'-O-geranyl-7-hydroxydihydroflavanol (5), along with 12 known natural products (6-17) were isolated from the CH2Cl2/MeOH (1:1) extract of the root bark of Millettia usaramensis ssp. usaramensis by chromatographic separation. The purified metabolites were identified by NMR spectroscopic and mass spectrometric analyses, whereas their absolute configurations were established on the basis of chiroptical data and in some cases also by X-ray crystallography. The crude extract was moderately active (IC50 = 11.63 μg/mL) against the ER-negative…

StereochemistryPlasmodium falciparumMolecular ConformationPharmaceutical Scienceroot barkCrystallography X-Ray01 natural sciencesMillettiaAnalytical ChemistryMillettia usaramensischemistry.chemical_compoundAntimalarialsChalconesDrug DiscoveryPlant BarkHumansta116IC50Nuclear Magnetic Resonance Biomolecularta317metabolitesPharmacologyFlavonoidsChromatographyNatural productbiologyMolecular Structure010405 organic chemistryChemistryPlant ExtractsOrganic ChemistryPlasmodium falciparumChloroquinebiology.organism_classification0104 chemical sciencesMillettia010404 medicinal & biomolecular chemistryChromatographic separationHEK293 CellsComplementary and alternative medicinevisual_artFlavanonesvisual_art.visual_art_mediumPlant BarkMolecular MedicineBarkrotenoidsJournal of natural products
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Evaluation of anti-androgenic activity of di-(2-ethylhexyl)phthalate

2005

International audience; DEHP is a widely used platiciser in the manufacture of PVC-based materials. It is known to disrupt the reproductive tract development in male rats. We have performed the Hershberger assay with DEHP on an immature castrated rat model to check if DEHP antagonise the testosterone propionate androgenic effect on the accessory sex organs development. DEHP significantly decreased the BC/LA muscles, the prostate, and the seminal vesicles relative weights from 100, 200, and 400 mg/kg bw/day, respectively. DEHP increased the liver relative weight from 100 mg/kg bw/day. A study was also performed on MDA-MB453 cell line stably transfected with pMMTVneo-Luc with DEHP and its maj…

Testosterone propionateMalemedicine.medical_specialtyendocrine systemMDA-MB453 TRANSFECTED CELL LINEmedicine.drug_classMetabolitePhthalic AcidsMONO-(2-ETHYLHEXYL1)PHTHALATE010501 environmental sciencesGenitalia MaleToxicologyAntiandrogen01 natural sciences03 medical and health scienceschemistry.chemical_compoundProstatePlasticizersInternal medicineCell Line TumorDiethylhexyl PhthalatemedicineAnimalsRats WistarLuciferases030304 developmental biology0105 earth and related environmental sciences0303 health sciencesDose-Response Relationship DrugPhthalateMONO-(2-ETHYL-5-HYDROXYLHEXYL)PHTHALATEBiological activityAndrogen AntagonistsDihydrotestosteroneDrug SynergismOrgan SizeMETABOLITES MONO-(2-ETHYL-5-OXOHEXYL1)PHTHALATEIn vitroRatsTestosterone PropionateEndocrinologymedicine.anatomical_structurechemistryLiverCell culture[SDV.TOX]Life Sciences [q-bio]/ToxicologyHERSHBERGER ASSAYDI-(2-ETHYLHEXYL1)PHTHALATEOrchiectomy
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Pharmacological genome demethylation increases radiosensitivity of head and neck squamous carcinoma cells

2011

Aberrant inactivation of tumor suppressor genes by promoter hypermethylation has been recognized as a crucial step of tumor development and is related to aggressiveness and therapy resistance. To identify potential novel treatment strategies, we evaluated pharmacological genome demethylation for the increase of irradiation treatment effectiveness in head and neck squamous cell carcinoma (HNSCC) in this in vitro study. HNSCC cells were cultured with 2 different concentrations of 5-azacytidine (5-Aza) for 72 h, followed by a single fraction irradiation with 4 or 50 Gy, respectively. To show successful genome demethylation, the methylation status of the tumor suppressor gene hic1 (hypermethyla…

Transcriptional ActivationAntimetabolites AntineoplasticTumor suppressor geneBisulfite sequencingBiologyRadiation ToleranceCell Line TumorGeneticsmedicineHumansRadiosensitivityPromoter Regions GeneticDemethylationOncogeneSquamous Cell Carcinoma of Head and NeckGeneral MedicineDNA MethylationCell cyclemedicine.diseaseHead and neck squamous-cell carcinomaSquamous carcinomaGene Expression Regulation NeoplasticHead and Neck NeoplasmsAzacitidineCarcinoma Squamous CellCancer researchInternational Journal of Molecular Medicine
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The presence of conifer resin decreases the use of the immune system in wood ants.

2008

5 pages; International audience; 1. Wood ants ( Formica paralugubris ) incorporate large amounts of solidified conifer resin into their nest, which reduces the density of many bacteria and fungi and protects the ants against some detrimental micro-organisms. By inducing an environment unfavourable to pathogens, the presence of resin may allow workers to reduce the use of their immune system. 2. The present study tested the hypothesis that the presence of resin decreases the immune activity of wood ants. Specifically, three components of the humoral immune defences of workers kept in resin-rich and resin-free experimental nests (antibacterial, lytic, and prophenoloxidase activities) were com…

[ SDV.BA.ZI ] Life Sciences [q-bio]/Animal biology/Invertebrate ZoologyFormica paralugubrisBiologyFormica paralugubrisMicrobiologyImmune systemNestImmunityBotany[ SDV.IMM ] Life Sciences [q-bio]/Immunologyantibacterial activity; Formica paralugubris; immunity; lytic activity; medication; plant secondary metabolites; prophenoloxidaseEcologyprophenoloxidasetechnology industry and agriculturelytic activityProphenoloxidasebiochemical phenomena metabolism and nutritionbiology.organism_classificationimmunityplant secondary metabolitesLytic cycleInsect SciencemedicationAntibacterial activityAntibacterial activityBacteria
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Les herbicides β-tricétones : devenir et impact écotoxicologique dans les sols agricoles et caractérisation de souches bactériennes dégradantes

2016

P-triketone herbicides : fate and ecotoxicological impact in arable soils and characterization of degrading bacterial strains abstract :This work aims to describe the ecodynamics of synthetic (sulcotrione and mesotrione) and natural (leptospermone) -triketone herbicides and to estimate their ecotoxicological impact on the bacterial community in arable soils. The processes involved in the dissipation of these herbicides (adsorption and biodegradation) have been studied in soil microcosms. Two bacterial strains, Bradyrhizobium sp. SRl able to degrade sulcotrione and mesotrione, and Methylophilus sp. LS1 degrading leptospermone, have been isolated. A bank of 12 ooo mutants of Bradyrhizobium sp…

[SDE] Environmental Scienceseffets des herbicidesbiodégradationsolsbiodegradationécotoxicologie microbiennemicrobial ecotoxicologytriketone herbicides[SDV] Life Sciences [q-bio]herbicidesmétabolites[SDV.BV] Life Sciences [q-bio]/Vegetal Biologymicrobiologieherbicides-tricétonesécotoxicologiemetabolites
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Does the lingual film intervene in the perception of taste?

2017

International audience; The biological film at the surface of the tongue, composed of saliva and microorganims, is an important interface between exogenous taste molecules and receptors involved in taste perception. However, the relationships between the composition of the lingual film and the perception of taste are not fully described. Thus, the aim of the present work was to study the differences in the biochemical (protein concentration, metabolite profiles) and microbiological compositions of the tongue films from 20 adult subjects, and to explore the possible relationships between composition and taste sensitivity assessed by means of a rapid at-home test. Preliminary results showed t…

[SDV.AEN] Life Sciences [q-bio]/Food and Nutritionsalivamicrobiology[SDV.AEN]Life Sciences [q-bio]/Food and Nutritionlingual filmmetabolites
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Field-Grown and In Vitro Propagated Round-Leaved Sundew (Drosera rotundifolia L.) Show Differences in Metabolic Profiles and Biological Activities

2021

Drosera rotundifolia L. is a carnivorous plant used in traditional medicine for its therapeutic properties. Because of its small size, its collection in nature is laborious and different cultivation methods have been studied to ensure availability. However, only a few studies exist where the lab-grown sundew tissue and field-grown sundew would have been compared in their functionality or metabolic profiles. In this study, the antioxidant and antiviral activities of lab-grown and field-grown sundew extracts and their metabolic profiles are examined. The effect of drying methods on the chromatographic profile of the extracts is also shown. Antioxidant activity was significantly higher (5–6 ti…

antioksidantitantimikrobiset yhdisteetPlant Extractssecondary metabolitesOrganic chemistrylihansyöjäkasvitphenolic compoundsfenoliset yhdisteetIn Vitro TechniquesluonnonaineetAntiviral AgentsDroseraArticleCell LinePlant Leavesantiviral propertiesQD241-441antioxidantsA549 CellsMetabolomeHumansDrosera rotundifolia<i>Drosera rotundifolia</i>Cell ProliferationMolecules
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