Search results for "activity"

showing 10 items of 7178 documents

Hepatoprotective effects of extracts, fractions and compounds from the stem bark of Pentaclethra macrophylla Benth: Evidence from in vitro and in viv…

2021

Abstract Aim To identify the bioactive hepatoprotective components of the ethanol extract of Pentaclethra macrophylla stem bark using in vitro and in vivo approaches. Methods The bioguided-fractionation of the ethanol extract was based on the substances’ capacity to prevent in vitro, the lipid peroxidation of hepatocytes’ membranes induced by hydrogen peroxide. For the in vivo hepatoprotective test, mice were treated orally with the ethyl acetate (EtOAc) fraction of the ethanol extract at doses of 50 and 75 mg/kg/day for one week and subjected to d -galactosamine/lipopolysaccharide (GaIN/LPS)-induced hepatotoxicity. Blood samples were collected for alanine aminotransferase (ALAT), aspartate…

0301 basic medicineAntioxidantPentaclethra macrophyllaIsolated compoundsmedicine.medical_treatmentInterleukin-1betaLipid peroxidationStructure-activity relationshipsRM1-950AntioxidantsLipid peroxidationSuperoxide dismutase03 medical and health scienceschemistry.chemical_compoundMice0302 clinical medicineIn vivomedicineAnimalsAspartate AminotransferasesRats WistarPharmacologybiologyTraditional medicinePlant StemsChemistryPlant ExtractsTumor Necrosis Factor-alphaBergeninAlanine TransaminaseFabaceaeGeneral MedicineGlutathioneDisease Models Animal030104 developmental biologyHepatoprotectionLiverCatalase030220 oncology & carcinogenesisbiology.proteinHepatocytesPlant BarkTherapeutics. PharmacologyChemical and Drug Induced Liver InjuryGaIN/LPSHepatoprotectionBiomedicine & Pharmacotherapy
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Impact of Fermentation on the Recovery of Antioxidant Bioactive Compounds from Sea Bass Byproducts

2020

The aim of the present research was to obtain antioxidant compounds through the fermentation of fish byproducts by bacteria isolated from sea bass viscera. To that purpose, bacteria from sea bass stomach, intestine, and colon were isolated. With the selected bacteria, growing research was undertaken, fermenting different broths prepared with sea bass meat or byproducts. After the fermentation, the antioxidant activity, phenolic acids, and some proteins were evaluated. The main phenolic acids obtained were DL-3-phenyl-lactic acid and benzoic acid at a maximum concentration of 466 and 314 ppb, respectively. The best antioxidant activity was found in the extracts obtained after the fermentatio…

0301 basic medicineAntioxidantPhysiologymedicine.medical_treatmentClinical Biochemistryantioxidant activityPositive correlationBiochemistryArticle03 medical and health scienceschemistry.chemical_compound0404 agricultural biotechnologymedicinefishing industry byproducts14. Life underwaterFood scienceSea bassMolecular BiologyfermentationBenzoic acidbiologylcsh:RM1-950Ambientalefood and beverages04 agricultural and veterinary sciencesCell Biologybiology.organism_classification040401 food scienceLactic acidAntioxidant capacity030104 developmental biologylcsh:Therapeutics. PharmacologychemistryAntioxidant activity; Bioactive peptides; Fermentation; Fishing industry byproducts; Phenolic acidsFermentationsense organsphenolic acidsbioactive peptidesBacteriaAntioxidants
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Anticancer, antioxidant, and antibacterial activities of low molecular weight bioactive subfractions isolated from cultures of wood degrading fungus …

2017

The aim of this study is to investigate in vitro the anticancer, antioxidant, and antibacterial activities of three low molecular weight subfractions I, II and III isolated from secondary metabolites produced by the wood degrading fungus Cerrena unicolor. The present study demonstrated that the low molecular weight subfractions III exhibited the strongest inhibitory activity towards breast carcinoma cells MDA-MB-231, prostatic carcinoma cells PC3, and breast cancer cells MCF7 with the half-maximal inhibitory concentration (IC50) value of 52,25 μg/mL, 60,66 μg/mL, and 54,92 μg/mL, respectively. The highest percentage of inhibition was noted at a concentration of 300 μg/mL in all the examined…

0301 basic medicineAntioxidantStaphylococcusmedicine.medical_treatmentlcsh:MedicineBacillusLaccasesBacillus subtilisPathology and Laboratory Medicinemedicine.disease_causeBiochemistryAntioxidantsNeoplasmsMedicine and Health SciencesCerrena unicolorStaphylococcus AureusFood sciencelcsh:ScienceMultidisciplinarybiologyAntimicrobialsChemistryDrugsEukaryota04 agricultural and veterinary sciencesWood040401 food scienceAnti-Bacterial AgentsBacterial PathogensEnzymesChemistryBacillus SubtilisExperimental Organism SystemsMedical MicrobiologyStaphylococcus aureusPhysical SciencesMCF-7 CellsProkaryotic ModelsPathogensAntibacterial activityResearch ArticleAntineoplastic AgentsResearch and Analysis MethodsMicrobiology03 medical and health sciencesMinimum inhibitory concentration0404 agricultural biotechnologyPhenolsMicrobial ControlmedicineHumansMicrobial PathogensIC50PharmacologyBacterialcsh:RChemical CompoundsOrganismsFungiBiology and Life SciencesProteinsbiology.organism_classificationIn vitro030104 developmental biologyEnzymologyAntibacterialslcsh:QPolyporalesPLOS ONE
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Chemical–physical characteristics, polyphenolic content and total antioxidant activity of three Italian-grown pomegranate cultivars

2019

Background: In Mediterranean countries, there is an increasing demand for pomegranate fruits due to their antioxidant properties and nutritional values. The large diffusion of new genotypes and cultivars requires the knowledge of all fruit characteristics in connection with the cultivation area, to satisfy the market demand. This study seeks to determine the fruit quality attributes and nutraceutical values of three pomegranate cultivars (Wonderful, Acco and Kamel) grown in the Mediterranean climate. Methods: The fruits were evaluated for their main physico-chemical traits (weight, volume, height, width, thickness, total arils number, total arils weight, juiciness, fruit index, peel index a…

0301 basic medicineAntioxidantmedicine.medical_treatmentPunica granatum Fruit quality Antioxidant activity Phytochemical Physico-chemical characteristic Bioactive compound contentTitratable acidlcsh:TX341-641Biology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineNutraceuticalArilSettore BIO/10 - BiochimicamedicineCultivar030109 nutrition & dieteticsNutrition and Dieteticslcsh:TP368-456food and beveragesSettore AGR/03 - Arboricoltura Generale E Coltivazioni ArboreeAntioxidant capacityHorticulturelcsh:Food processing and manufacturechemistryPolyphenolAnthocyanin030221 ophthalmology & optometrylcsh:Nutrition. Foods and food supplyFood Science
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Novel iodoacetamido benzoheterocyclic derivatives with potent antileukemic activity are inhibitors of STAT5 phosphorylation

2016

Signal Transducer and Activator of Transcription 5 (STAT5) protein, a component of the STAT family of signaling proteins, is considered to be an attractive therapeutic target because of its involvement in the progression of acute myeloid leukemia. In an effort to discover potent molecules able to inhibit the phosphorylation-activation of STAT5, twenty-two compounds were synthesized and evaluated on the basis of our knowledge of the activity of 2-(3’,4’,5’-trimethoxybenzoyl)-3-iodoacetamido-6-methoxy benzo[b]furan derivative 1 as a potent STAT5 inhibitor. Most of these molecules, structurally related to compound 1, were characterized by the presence of a common 3’,4’,5’-trimethoxybenzoyl moi…

0301 basic medicineApoptosisAntineoplastic Agentchemistry.chemical_compoundBenzophenone0302 clinical medicinehemic and lymphatic diseasesFuranDrug DiscoverySTAT5 Transcription FactorTumor Cells CulturedThiopheneMoietyPhosphorylationSTAT5Molecular StructurebiologyChemistryBiological activityGeneral MedicineApoptosis; BCR/ABL expressing leukemia; In vitro antiproliferative activity; STAT5 inhibitors; Structure-activity relationship; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyLeukemia Myeloid Acute030220 oncology & carcinogenesisBCR/ABL expressing leukemiaApoptosis; BCR/ABL expressing leukemia; In vitro antiproliferative activity; STAT5 inhibitors; Structure-activity relationship; Antineoplastic Agents; Apoptosis; Benzofurans; Benzophenones; Cell Proliferation; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; Humans; K562 Cells; Leukemia Myeloid Acute; Molecular Structure; Phosphorylation; STAT5 Transcription Factor; Structure-Activity Relationship; Tumor Cells Cultured; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyHumanStereochemistryAntineoplastic AgentsArticleNOBenzophenones03 medical and health sciencesK562 CellHumansStructure–activity relationshipBenzofuransCell ProliferationPharmacologyIndole testDose-Response Relationship DrugIn vitro antiproliferative activitySTAT5 inhibitorsDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryApoptosiSTAT5 inhibitorStructure-activity relationshipIn vitro030104 developmental biologybiology.proteinBenzofuranDrug Screening Assays AntitumorK562 Cells
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Effect of chronic exercise on myocardial electrophysiological heterogeneity and stability. Role of intrinsic cholinergic neurons: A study in the isol…

2018

[EN] A study has been made of the effect of chronic exercise on myocardial electrophysiological heterogeneity and stability, as well as of the role of cholinergic neurons in these changes. Determinations in hearts from untrained and trained rabbits on a treadmill were performed. The hearts were isolated and perfused. A pacing electrode and a recording multielectrode were located in the left ventricle. The parameters determined during induced VF, before and after atropine (1 mu M), were: fibrillatory cycle length (VV), ventricular functional refractory period (FRPVF), normalized energy (NE) of the fibrillatory signal and its coefficient of variation (CV), and electrical ventricular activatio…

0301 basic medicineAtropineMaleRefractory Period ElectrophysiologicalRefractory periodPhysiology030204 cardiovascular system & hematologyBiochemistryRunningTissue Culture Techniques0302 clinical medicineAnimal CellsMuscarinic acetylcholine receptorMedicine and Health SciencesMedicinePublic and Occupational HealthTreadmillMammalsNeuronsMultidisciplinaryQREukaryotaHeartNeurochemistryNeurotransmittersAnimal ModelsSports ScienceCardiovascular physiologyElectrophysiologyAtropineChemistrymedicine.anatomical_structureExperimental Organism SystemsVentricular FibrillationPhysical SciencesVertebratesCardiologyLeporidsMedicineRabbitsCellular TypesAnatomyArrhythmiamedicine.drugResearch Articlemedicine.medical_specialtyScienceCholinergicsCardiologyMuscarinic AntagonistsResearch and Analysis MethodsTECNOLOGIA ELECTRONICA03 medical and health sciencesAlkaloidsInternal medicineAnimalsCholinergic neuronSports and Exercise MedicineExercisebusiness.industryChemical CompoundsOrganismsParasympatholyticsBiology and Life SciencesCell BiologyPhysical ActivityElectrophysiology030104 developmental biologyVentriclePhysical FitnessCellular NeuroscienceAmniotesAnimal StudiesCardiovascular AnatomybusinessNeuroscience
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Dietary polyphenols for managing cancers: What have we ignored?

2020

Abstract Although the chemoprevention and anti-cancer activities of dietary polyphenols have been evidenced through both in vitro and in vivo studies, most of the human clinical trials were unsuccessful or even harmful. Debates on the beneficial roles of dietary polyphenols in cancer therapy are increasing. Many dietary polyphenols studies are conducted by in vitro experiments, but the nature of these studies does not consider the complexity of metabolic processes that are present in vivo. These can often cause instability in the dietary polyphenols, thereby leading to unsuccessful extrapolation into animal or human studies. Dietary polyphenols often have low bioavailability, which is mainl…

0301 basic medicineBioavailabilityCancer therapyMetabolitePharmacology03 medical and health sciences0302 clinical medicineAnti-cancer activityIn vivoMedicineTherapeutic windowCellular metabolismHuman studiesbusiness.industryMicrobiotafood and beveragesDietary polyphenolBioavailability030104 developmental biologyPolyphenol030220 oncology & carcinogenesisCancer cellbusinessStabilityFood ScienceBiotechnology
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NaCl-saturated brines are thermodynamically moderate, rather than extreme, microbial habitats

2018

NaCl-saturated brines such as saltern crystalliser ponds, inland salt lakes, deep-sea brines and liquids-of-deliquescence on halite are commonly regarded as a paradigm for the limit of life on Earth. There are, however, other habitats that are thermodynamically more extreme. Typically, NaCl-saturated environments contain all domains of life and perform complete biogeochemical cycling. Despite their reduced water activity, ∼0.755 at 5 M NaCl, some halophiles belonging to the Archaea and Bacteria exhibit optimum growth/metabolism in these brines. Furthermore, the recognised water-activity limit for microbial function, ∼0.585 for some strains of fungi, lies far below 0.755. Other biophysical c…

0301 basic medicineBiogeochemical cycleWater activity030106 microbiologySodium Chlorideengineering.materialBacterial Physiological PhenomenaMicrobiology03 medical and health sciencesEcosystemEcosystemBacteriabiologyBiospherebiology.organism_classificationArchaeaHalophile030104 developmental biologyInfectious DiseasesEnvironmental chemistryengineeringDunaliella salinaThermodynamicsHaliteSaltsWater MicrobiologyArchaeaFEMS Microbiology Reviews
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GABA and Gap Junctions in the Development of Synchronized Activity in Human Pluripotent Stem Cell-Derived Neural Networks.

2017

The electrical activity of the brain arises from single neurons communicating with each other. However, how single neurons interact during early development to give rise to neural network activity remains poorly understood. We studied the emergence of synchronous neural activity in human pluripotent stem cell (hPSC)-derived neural networks simultaneously on a single-neuron level and network level. The contribution of gamma-aminobutyric acid (GABA) and gap junctions to the development of synchronous activity in hPSC-derived neural networks was studied with GABA agonist and antagonist and by blocking gap junctional communication, respectively. We characterized the dynamics of the network-wide…

0301 basic medicineBiolääketieteet - Biomedicineneural networkstem cell derived neuronslcsh:RC321-57103 medical and health sciencesCellular and Molecular Neuroscience0302 clinical medicineCalcium imagingPremovement neuronal activityhuman pluripotent stem cellsInduced pluripotent stem celllcsh:Neurosciences. Biological psychiatry. Neuropsychiatrygap junctionsOriginal ResearchArtificial neural networkGABAA receptorChemistrymicroelectrode arrayGap junctionsynchronyDepolarizationMultielectrode arraycalcium imaging030104 developmental biologynervous systemexcitatory GABANeuroscienceNeurotieteet - Neurosciences030217 neurology & neurosurgeryNeuroscienceFrontiers in cellular neuroscience
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Dry selection and wet evaluation for the rational discovery of new anthelmintics

2017

Helminths infections remain a major problem in medical and public health. In this report, atom-based 2D bilinear indices, a TOMOCOMD-CARDD (QuBiLs-MAS module) molecular descriptor family and linear discriminant analysis (LDA) were used to find models that differentiate among anthelmintic and non-anthelmintic compounds. Two classification models obtained by using non-stochastic and stochastic 2D bilinear indices, classified correctly 86.64% and 84.66%, respectively, in the training set. Equation 1(2) correctly classified 141(135) out of 165 [85.45%(81.82%)] compounds in external validation set. Another LDA models were performed in order to get the most likely mechanism of action of anthelmin…

0301 basic medicineBiophysicsNon-stochastic and stochastic atom-based bilinear indicesBilinear interpolationLDA-based QSAR modelQuBiLs-MAS module01 natural sciencesSet (abstract data type)03 medical and health sciencesMolecular descriptorStatisticsPhysical and Theoretical ChemistryMolecular BiologySelection (genetic algorithm)MathematicsFree and open source softwareTraining setTOMOCOMD-CARDD softwareExternal validationAnthelmintic activityAtom (order theory)Computational creeningCondensed Matter PhysicsLinear discriminant analysis0104 chemical sciencesIndazole010404 medicinal & biomolecular chemistry030104 developmental biologyLead generationMolecular Physics
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