Search results for "I.5"

showing 10 items of 399 documents

Interactions between T-2 toxin and its metabolites in HepG2 cells and in silico approach

2021

Abstract The T-2 toxin (T-2) is commonly metabolized to HT-2 toxin (HT-2), Neosolaniol (NEO), T2-triol and T2-tetraol and they can modify the toxicity of T-2. In this study, T-2 and its modified forms were evaluated by in vitro and in silico methods. The in vitro cytotoxicity individually was evaluated by MTT and Total Protein Content (PC) assays in human hepatocarcinoma (HepG2) cells. The order of IC50 was T-2 tetraol > T-2 triol > NEO > T-2 = HT-2. The T-2 and HT-2 evidenced the highest cytotoxic effect in HepG2 cells individually. No differences were observed in binary combinations tested and the two mycotoxins in the mixture tested individually. The T-2+HT-2 combination showed the highe…

Cell SurvivalIn silicoToxicologymedicine.disease_cause03 medical and health sciences0404 agricultural biotechnologymedicineHumansCytotoxic T cellComputer SimulationCytotoxicityIC50030304 developmental biologyADME0303 health sciencesDose-Response Relationship DrugToxinChemistryHep G2 Cells04 agricultural and veterinary sciencesGeneral Medicine040401 food scienceIn vitroT-2 ToxinBiochemistryToxicityFood ScienceFood and Chemical Toxicology
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Cyclic heptapeptides from the soil-derived fungus Clonostachys rosea

2019

Abstract Three new cyclic heptapeptides (1–3) together with three known compounds (4–6) were isolated from a solid rice culture of the soil-derived fungus Clonostachys rosea. Fermentation of the fungus on white beans instead of rice afforded a new γ-lactam (7) and a known γ-lactone (8) that were not detected in the former extracts. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR spectra as well as by HRESIMS data. Compounds 1 and 4 exhibited significant cytotoxicity against the L5178Y mouse lymphoma cell line with IC50 values of 4.1 and 0.1 µM, respectively. Compound 4 also displayed cytotoxicity against the A2780 human ovarian cancer cell line with an IC50…

Cell SurvivalStereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsFungusPeptides Cyclic01 natural sciencesBiochemistryMiceStructure-Activity RelationshipCell Line TumorDrug DiscoveryIc50 valuesAnimalsHumansCytotoxicityMolecular BiologyIC50Cell ProliferationDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryChemistryOrganic ChemistryGliocladiumbiology.organism_classification0104 chemical sciences010404 medicinal & biomolecular chemistryCell cultureFermentationClonostachys roseaMolecular MedicineFermentationDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopyBioorganic & Medicinal Chemistry
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Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin

2007

A series of 11 bis-indolylthiophenes of formula I were obtained by cyclization of bis-indole 1,4-diketones using Lawesson''s reagent. Derivs. I (R = OMe, R1 = SO2Ph), I (R = OMe, R1 = Me), I (R = Cl, R1 = Me), and I (R = OMe, R1 = H) were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the re…

Cell typeIndolescyclizationHL60StereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsThiophenesBiochemistryChemical synthesisInhibitory Concentration 50chemistry.chemical_compoundAlkaloids5-bis(3'-indolyl)thiophenesCell Line TumorDrug DiscoverymedicineAnimalsHumansantitumor activityMolecular BiologyCell Proliferationbis-indolylthiopheneCell growthNortopsentinMelanomaOrganic ChemistryImidazolesCancerBiological activityDNAmedicine.diseasediketonesTopoisomerase II5-bis(3'-indolyl)thiophenes; antitumor activity; Topoisomerase II; NortopsentinDNA Topoisomerases Type IIchemistryCell cultureMolecular Medicine
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Essential oil of Citrus lumia Risso: Phytochemical profile, antioxidant properties and activity on the central nervous system

2018

Citrus lumia Risso Essential oil Antioxidant properties Anti-cholinesterase activity Cytotoxicity Neuroactive effects 1. Introduction Plants that produce essential oils (EOs) represent a large part of natural flora and an important resource in various fields such as pharmaceutical, food and cosmetic industries, due to their flavor, fra- grance and biological activity (Swamy et al., 2016). EOs play a pivotal role in the growth and colonization of plants, giving color and scent to reproductive organs, attracting pollinators, favoring seed dispersion (Sharifi-Rad et al., 2017), and defending the plant against abiotic (light, temperature, etc.) and biotics (herbivores, harmful insects and pa- t…

Central Nervous System0106 biological sciences0301 basic medicineCitrusAntioxidantCytotoxicitymedicine.medical_treatmentToxicology01 natural sciencesAntioxidantsEssential oillaw.inventionTerpeneMicechemistry.chemical_compoundLinaloollawSettore BIO/15 - Biologia FarmaceuticaFood scienceCitrus lumia Risso Essential oil Antioxidant properties Anti-cholinesterase activity Cytotoxicity Neuroactive effectsbiologyGeneral MedicineNeuroprotective AgentsPhytochemicalNeuroactive effectsAnti-cholinesterase activityAcyclic MonoterpenesAntioxidant propertiesNeuroprotectionGas Chromatography-Mass SpectrometryCell Line03 medical and health sciencesCyclohexenesOils VolatilemedicineAnimalsRats WistarIC50Essential oilCholinesteraseCell-Free SystemTerpenesAnti-cholinesterase activity; Antioxidant properties; Citrus lumia Risso; Cytotoxicity; Essential oil; Neuroactive effects; Food Science; Toxicology030104 developmental biologychemistryMicroscopy Electron ScanningMonoterpenesbiology.proteinCitrus lumia RissoCholinesterase InhibitorsLimonene010606 plant biology & botanyFood ScienceFood and Chemical Toxicology
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Phenylsulphonyl urenyl chalcone derivatives as dual inhibitors of cyclo-oxygenase-2 and 5-lipoxygenase

2005

Two series of phenylsulphonyl urenyl chalcone derivatives (UCH) with various patterns of substitution were tested for their effects on nitric oxide (NO) and prostaglandin E2 (PGE2) overproduction in RAW 264.7 macrophages. None of the tested compounds reduced NO production more than 50% at 10 microM but most of them inhibited the generation of PGE2 with IC50 values under the micromolar range. Me-UCH 1, Me-UCH 5, Me-UCH 9, Cl-UCH 1, and Cl-UCH 9 were selected to evaluate their influence on human leukocyte functions and eicosanoids generation. These derivatives selectively inhibited cyclo-oxygenase-2 (COX-2) activity in human monocytes being Me-UCH 5 the most potent (IC50 0.06 microM). Selecte…

ChalconeNeutrophilsNitric OxideLeukotriene B4DinoprostoneGeneral Biochemistry Genetics and Molecular BiologyCell LineNitric oxideMiceStructure-Activity Relationshipchemistry.chemical_compoundChalconesmedicineAnimalsHumansCyclooxygenase InhibitorsLipoxygenase InhibitorsGeneral Pharmacology Toxicology and PharmaceuticsProstaglandin E2IC50Molecular StructurebiologySuperoxideMacrophagesElastaseGeneral MedicinechemistryBiochemistryCyclooxygenase 2MyeloperoxidaseArachidonate 5-lipoxygenasebiology.proteinmedicine.drugLife Sciences
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The climate change effect on the african monsoon region : evolution of the precipitation and atmospheric fields in the CMIP3 and CMIP5 simulations un…

2013

The fourth IPCC report in 2007 established the synthesis of previously published work onthe effects of climate change on global and regional scales. It shows in particular that no consensuscan be found with regard to the future of rainfall — and atmospheric dynamics- associatedwith region — African monsoon. This dissertation revisits this issue in the light of new dataand using an approach avoiding over-representation of the number of simulations available forone type of model and taking into account the diversity of models and their evolution in time :twenty general circulation models (GCMs) participating in the exercises CMIP3 (twelve GCMs)and CMIP5 (eight GCMs) under the A1B emissions sc…

Changement climatiqueA1B and rcp45 emission scenariosMousson africaineClimate ChangeSahel[SDU.STU] Sciences of the Universe [physics]/Earth SciencesAfrican MonsoonCMIP5[ SDU.STU ] Sciences of the Universe [physics]/Earth SciencesScénarios d’émission A1B et rcp45CMIP3General Circulation ModelsModèles de circulation générale
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Tropical Temperate Toughs over southern Africa : mechanisms and evolution in response to climate change (2010-2099)

2014

In the Southern Hemisphere, Southern Africa and the south-west Indian Ocean are one of the three preferred regions where interactions between the tropics and midlatitudes develop. This is the South Indian Convergence Zone (SICZ), where northwest-southeast oriented cloud bands form at the synoptic scale (between 3 and 5 days). These bands are mainly found during the austral summer and are commonly referred to as tropical temperate troughs (TTTs). This research aims at improving our knowledge related to TTTs, with a study on the dynamics associated with these systems, and an analysis of their possible evolution during the 21st century.The first part of this thesis aims at identifying favorabl…

Changement climatiqueMidlatitude perturbationsTalweg tropical-tempéréAfrique australeGeneral circulation modelsRCP 8.5Perturbation des moyennes latitudesInteractions d’échelleClassificationModèles « système-Terre »[SDU.STU.CL] Sciences of the Universe [physics]/Earth Sciences/ClimatologyTropical-temperate toughClimate changeCMIP5Southern AfricaRCP2.6Scale interactions
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Interaction effects of enniatin B, deoxinivalenol and alternariol in Caco-2 cells.

2015

Enniatin B (ENN B), deoxinivalenol (DON) and alternariol (AOH) are secondary metabolites of filamentous fungi. These mycotoxins are contaminants of vegetables and cereals. They are cytotoxic and their effects are enhanced by their mixtures. The objectives of this study were to compare the cytotoxicity of ENN B, DON and AOH alone or in combination in human adenocarcinoma (Caco-2) cells and to evaluate the type of interactions of mycotoxin mixtures by the isobologram analysis. Cells were treated with concentrations ranging from 1.85 to 90μM (AOH) and from 0.312 to 10μM (for ENN B and DON), individually and in combination of two and three mycotoxins (from 1.85 to 30μM for AOH and from 0.312 to…

ChemistryStereochemistryCell SurvivalAlternariolFood Contamination04 agricultural and veterinary sciencesGeneral MedicineMycotoxinsToxicology040401 food scienceCellular viabilitychemistry.chemical_compoundLactones0404 agricultural biotechnologyCaco-2DepsipeptidesIc50 valuesHumansDrug InteractionsFood scienceCaco-2 CellsMycotoxinTrichothecenesCell survivalEnniatin BToxicology letters
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Efficient Production of Isoflavonoids by Astragalus membranaceus Hairy Root Cultures and Evaluation of Antioxidant Activities of Extracts

2014

In this study, Astragalus membranaceus hairy root cultures (AMHRCs) were established as an attractive alternative source for the efficient production of isoflavonoids (IF). A. membranaceus hairy root line II was screened as the most efficient line and was confirmed by PCR amplification of rolB, rolC and aux1 genes. Culture parameters of AMHRCs were systematically optimized, and five main IF constituents were quali-quantitatively determined by LC-MS/MS. Under optimal conditions, the total IF accumulation of 34 day old AMHRCs was 234.77 μg/g dry weight (DW). This yield was significantly higher compared to that of 3 year old field grown roots (187.38 μg/g DW). Additionally, in vitro antioxidan…

ChromatographyAntioxidantbiologymedicine.medical_treatmentCell Culture TechniquesGeneral ChemistryAstragalus propinquusbiology.organism_classificationIsoflavonesPlant RootsAntioxidantsAstragalusNutraceuticalDry weightLc ms msmedicineIc50 valuesFood scienceGeneral Agricultural and Biological SciencesDrugs Chinese HerbalJournal of Agricultural and Food Chemistry
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Combined approaches to identify genomic regions involved in phenotypic differentiation between low divergent breeds: Application in Sardinian sheep p…

2019

Selective breeding has led to modifications in the genome of many livestock breeds. In this study, we identified the genomic regions that may explain some of the phenotypic differences between two closely related breeds from Sardinia. A total of 44 animals, 20 Sardinian Ancestral Black (SAB) and 24 Sardinian White (SW), were genotyped using the Illumina Ovine 50K array. A total of 68, 38 and 15 significant markers were identified using the case–control genome-wide association study (GWAS), the Bayesian population differentiation analysis (FST) and the Rsb metric, respectively. Comparisons among the approaches revealed a total of 22 overlapping markers between GWAS and FST and one marker bet…

CoatGenotypePopulationGenome-wide association studygenome-wide methodsBiologySelective breedingGenomePolymorphism Single NucleotideSettore AGR/17 - Zootecnica Generale E Miglioramento GeneticoFood Animalsgenome-wide methods; genomic regions; Ovine BeadChip50K; Sardinian sheep breedsSardinian sheep breedsAnimalsGenetic variabilitygenomic regionseducationGeneOvine BeadChip50Keducation.field_of_studySheepHomozygoteMolecular Sequence AnnotationGeneral MedicineGenomicsgenome-wide methodgenomic regionWhite (mutation)PhenotypeEvolutionary biologyAnimal Science and ZoologyJournal of animal breeding and genetics = Zeitschrift fur Tierzuchtung und ZuchtungsbiologieREFERENCES
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