Search results for "Hip"

showing 10 items of 9327 documents

An in vitro investigation on the cytotoxic and nuclear receptor transcriptional activity of the mycotoxins fumonisin B1 and beauvericin.

2016

Fumonisin B1 (FB1) and beauvericin (BEA) are secondary metabolites of filamentous fungi, which under appropriate temperature and humidity conditions may develop on various foods and feeds. To date few studies have been performed to evaluate the toxicological and endocrine disrupting effects of FB1 and BEA. The present study makes use of various in vitro bioassays including; oestrogen, androgen, progestagen and glucocorticoid reporter gene assays (RGAs) for the study of nuclear receptor transcriptional activity, the thiazolyl blue tetrazolium bromide (MTT) assay to monitor cytotoxicity and high content analysis (HCA) for the detection of pre-lethal toxicity in the RGA and Caco-2 human colon …

0301 basic medicineTranscription GeneticCell SurvivalBiologyAdenocarcinomaEndocrine DisruptorsToxicologyFumonisins03 medical and health scienceschemistry.chemical_compound0404 agricultural biotechnologyGlucocorticoid receptorReceptors GlucocorticoidGenes ReporterDepsipeptidesmedicineHumansCytotoxicityReceptorCell NucleusFumonisin B1Dose-Response Relationship Drug04 agricultural and veterinary sciencesGeneral Medicine040401 food scienceBeauvericin030104 developmental biologychemistryNuclear receptorBiochemistryReceptors AndrogenToxicityColonic NeoplasmsCaco-2 CellsReceptors ProgesteroneGlucocorticoidmedicine.drugToxicology letters
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2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.

2018

Macrocyclic inhibitors of rhodesain (RD), a parasitic cysteine protease and drug target for the treatment of human African trypanosomiasis, have shown low metabolic stability at the macrocyclic ether bridge. A series of acyclic dipeptidyl nitriles was developed using structure-based design (PDB ID: 6EX8). The selectivity against the closely related cysteine protease human cathepsin L (hCatL) was substantially improved, up to 507-fold. In the S2 pocket, 3,4-dichlorophenylalanine residues provided high trypanocidal activities. In the S3 pocket, aromatic residues provided enhanced selectivity against hCatL. RD inhibition (Ki values) and in vitro cell-growth of Trypanosoma brucei rhodesiense (I…

0301 basic medicineTrypanosoma brucei rhodesienseStereochemistrySwineTrypanosoma cruziPlasmodium falciparumTriazoleProtozoan ProteinsCysteine Proteinase InhibitorsLigands01 natural sciencesCysteine Proteinase InhibitorsCell LineCathepsin L03 medical and health scienceschemistry.chemical_compoundMiceStructure-Activity RelationshipIn vivoDrug DiscoveryNitrilesStructure–activity relationshipAnimalsHumansATP Binding Cassette Transporter Subfamily B Member 1Trypanocidal agentBinding SitesbiologyMolecular Structure010405 organic chemistryChemistryTrypanosoma brucei rhodesienseDipeptidesTriazolesCysteine proteaseTrypanocidal Agents0104 chemical sciencesRatsCysteine Endopeptidases030104 developmental biologyDrug Designbiology.proteinMicrosomes LiverMolecular MedicineFemaleLeishmania donovaniJournal of medicinal chemistry
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Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents

2016

Novel 1,4-benzodiazepines, endowed with a Michael acceptor moiety, were designed taking advantage of a computational prediction of their pharmacokinetic parameters. Among all the synthesized derivatives, we identified a new lead compound (i.e., 4a), bearing a vinyl ketone warhead and endowed with a promising antitrypanosomal activity against Trypanosoma brucei brucei (IC50 = 5.29 µM), coupled with a lack of cytotoxicity towards mammalian cells (TC50>100 µM).

0301 basic medicineTrypanosomaKetonePeptidomimeticPeptidomimeticStereochemistryTrypanosoma brucei bruceiClinical BiochemistryPharmaceutical ScienceTrypanosoma brucei01 natural sciencesBiochemistryCell LineBenzodiazepinesMiceStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundparasitic diseasesDrug DiscoveryAnimalsStructure–activity relationshipMoietyCytotoxicityMolecular BiologyMicrowave irradiationchemistry.chemical_classificationDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryMacrophagesOrganic Chemistrybiology.organism_classificationMichael acceptors Microwave irradiation Peptidomimetics Pharmacokinetic parameters TrypanosomaTrypanocidal Agents0104 chemical sciencesPharmacokinetic parameter030104 developmental biologychemistryMichael reactionMolecular MedicineMichael acceptorLead compoundBioorganic & Medicinal Chemistry Letters
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Vitamin K antagonism impairs the bone marrow microenvironment and hematopoiesis

2018

Abstract Vitamin K antagonists (VKAs) have been used in 1% of the world’s population for prophylaxis or treatment of thromboembolic events for 64 years. Impairment of osteoblast function and osteoporosis has been described in patients receiving VKAs. Given the involvement of cells of the bone marrow microenvironment (BMM), such as mesenchymal stem cells (MSCs) and macrophages, as well as other factors such as the extracellular matrix for the maintenance of normal hematopoietic stem cells (HSCs), we investigated a possible effect of VKAs on hematopoiesis via the BMM. Using various transplantation and in vitro assays, we show here that VKAs alter parameters of bone physiology and reduce funct…

0301 basic medicineVitamin KImmunologyPopulationBone Marrow CellsPeriostinBiochemistryMice03 medical and health sciences0302 clinical medicineLeukocytesAnimalsMedicineeducationeducation.field_of_studyDose-Response Relationship Drugbusiness.industryMacrophagesMonocyteMesenchymal stem cellAnticoagulantsCell BiologyHematologyHematopoietic Stem CellsHematopoiesisTransplantationHaematopoiesis030104 developmental biologymedicine.anatomical_structureCellular MicroenvironmentMyelodysplastic Syndromes030220 oncology & carcinogenesisCancer researchWarfarinBone marrowStem cellbusinessCell Adhesion MoleculesBiomarkersBlood
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Vitamin D and Cardiovascular Health

2021

The principal source of vitamin D in humans is its biosynthesis in the skin through a chemical reaction dependent on sun exposure. In lesser amounts, the vitamin can be obtained from the diet, mostly from fatty fish, fish liver oil and mushrooms. Individuals with vitamin D deficiency, defined as a serum level of 25 hydroxyvitamin D < 20 ng/dl, should be supplemented. Vitamin D deficiency is a prevalent global problem caused mainly by low exposure to sunlight. The main role of 1,25 dihydroxyvitamin D is the maintenance of calcium and phosphorus homeostasis. However, vitamin D receptors are found in most human cells and tissues, indicating many extra-skeletal effects of the vitamin, particula…

0301 basic medicineVitaminmedicine.medical_specialtyVitamina DEnfermedad cardiovascularchemistry.chemical_element030209 endocrinology & metabolismCalciumCritical Care and Intensive Care Medicinemedicine.disease_causevitamin D deficiencyNitric oxide03 medical and health scienceschemistry.chemical_compound0302 clinical medicineImmune systemInternal medicineHipertensiónmedicineVitamin D and neurologyHumansSupplementsVitamin D030109 nutrition & dieteticsNutrition and DieteticsEnfermedad coronariabusiness.industryEndothelial functionVitamin D Deficiencymedicine.diseaseCardiovascular diseaseCoronary heart diseaseEndocrinologyDietéticachemistryCardiovascular DiseasesNutriciónHypertensionNarrative ReviewbusinessHomeostasisOxidative stress
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Primjena ekstrakta proteina sirutke u proizvodnji smrznutog mliječnog deserta

2018

The aim of this work was to substantiate the use of whey protein extract (WPE), a by-product of dairy industry, combined with different berry purees in the formulation of a whipped frozen dairy dessert (WFDD). After freezing, the swelling ability of WPE decreased significantly while at higher temperatures of the dispersion medium, the degree of swelling increased. A mixture containing 55±2 % WPE and 45±2 % milk presented a homogeneous consistency while the further processing did not improve the structure of the mixture. Final formulations of WFDD containing different berry purees (i.e. 10 % black¬currant puree, 25 % cherry puree, or 30 % strawberry puree) were proposed for which the nutriti…

0301 basic medicineWhey protein030109 nutrition & dieteticsbusiness.industryChemistryorganoleptic propertiesswelling degreeOrganolepticekstrakt proteina sirutke; smrznuti mliječni desert; pire bobičastog voća; organoleptička svojstva; stupanj bubrenjaFood composition datalcsh:SF221-250whey protein extract; whipped frozen dairy dessert; berry puree; organoleptic properties; swelling degreewhey protein extract ; whipped frozen dairy dessert ; berry puree ; organoleptic properties ; swelling degreeberry puree03 medical and health scienceslcsh:DairyingMilk productsFood processingFood scienceFood qualitybusinesswhipped frozen dairy dessertwhey protein extractMljekarstvo
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Systematic gene overexpression in Candida albicans identifies a regulator of early adaptation to the mammalian gut.

2018

International audience; Candida albicans is part of the human gastrointestinal (GI) microbiota. To better understand how C. albicans efficiently establishes GI colonisation, we competitively challenged growth of 572 signature-tagged strains (~10% genome coverage), each conditionally overexpressing a single gene, in the murine gut. We identified CRZ2, a transcription factor whose overexpression and deletion respectively increased and decreased early GI colonisation. Using clues from genome-wide expression and gene-set enrichment analyses, we found that the optimal activity of Crz2p occurs under hypoxia at 37°C, as evidenced by both phenotypic and transcriptomic analyses following CRZ2 geneti…

0301 basic medicine[SDV.MHEP.AHA] Life Sciences [q-bio]/Human health and pathology/Tissues and Organs [q-bio.TO]030106 microbiologyImmunologyMicrobiologyMannosyltransferasesBiological pathwayTranscriptomeFungal ProteinsMannans03 medical and health scienceschemistry.chemical_compoundtranscriptomicsregulatory networksCell WallVirologyGene Expression Regulation FungalCandida albicanssignature‐tagged overexpression[SDV.MHEP.AHA]Life Sciences [q-bio]/Human health and pathology/Tissues and Organs [q-bio.TO]AnimalsGene Regulatory NetworksCandida albicansPromoter Regions GeneticGeneTranscription factorResearch ArticlesFungal proteinMice Inbred BALB CCRZ2chromatin immunoprecipitation‐on‐chipbiologyCRZ2;Candida albicans;chromatin immunoprecipitation-on-chip;gastrointestinal colonisation;regulatory networks;signature-tagged overexpression;transcriptomicsTunicamycinTunicamycinHydrogen-Ion Concentrationbiology.organism_classificationPhenotypeCell biologyGastrointestinal MicrobiomeGastrointestinal Tractchemistrychromatin immunoprecipitation-on-chipFemalesignature-tagged overexpressionMicroorganisms Genetically-Modifiedgastrointestinal colonisationResearch Article
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Genomic characterization of Algerian Guelmoise cattle and their genetic relationship with other North African populations inferred from SNP genotypin…

2018

International audience; Understanding between and within-breeds genetic variability is essential in the choice of conservation management decisions for threatened populations. In this study we assessed the genetic diversity of the Algerian Guelmoise cattle (GUE) by analyzing data on 24 GUE individuals genotyped for the Illumina BovineSNP50 BeadChipv2. We also provided a detailed description of the population structure of GUE using comparisons with 23 worldwide cattle populations, selected as being representative of African, South European and indicine populations, in addition to four North African populations. We show that GUE is an admixed population which has strong genetic similarity to …

0301 basic medicine[SDV]Life Sciences [q-bio]PopulationSNPGenetic relationshipBiologyRuns of homozygosityGene flow03 medical and health sciencesAlgerian cattlePhylogeneticSettore AGR/17 - Zootecnica Generale E Miglioramento GeneticoGenetic variabilityeducationsnps2. Zero hunger[SDV.GEN]Life Sciences [q-bio]/Geneticseducation.field_of_studyGenetic diversityGeneral VeterinaryPhylogenetic tree0402 animal and dairy science04 agricultural and veterinary sciences040201 dairy & animal scienceSNP genotypingphylogenetics[SDV.GEN.GA]Life Sciences [q-bio]/Genetics/Animal genetics030104 developmental biologyEvolutionary biologyVeterinary (all)Animal Science and ZoologyGenetic structureInbreeding
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Hypocellularity in the murine model for Down Syndrome Ts65Dn is not affected by adult neurogenesis

2016

Down syndrome (DS) is caused by the presence of an extra copy of the chromosome 21 and it is the most common aneuploidy producing intellectual disability. Neural mechanisms underlying this alteration may include defects in the formation of neuronal networks, information processing and brain plasticity. The murine model for DS, Ts65Dn, presents reduced adult neurogenesis. This reduction has been suggested to underlie the hypocellularity of the hippocampus as well as the deficit in olfactory learning in the Ts65Dn mice. Similar alterations have also been observed in individuals with DS. To determine whether the impairment in adult neurogenesis is, in fact, responsible for the hypocellularity …

0301 basic medicineanimal diseasesHippocampusSubventricular zoneBiotecnologiaHippocampusSubgranular zonelcsh:RC321-57103 medical and health sciences0302 clinical medicinedoublecortinNeuroplasticitymental disordersmedicineBrdUlcsh:Neurosciences. Biological psychiatry. NeuropsychiatryOriginal ResearchbiologyGeneral NeuroscienceNeurogenesisOlfactory BulbOlfactory bulbDoublecortinCell biologyadult neurogenesisTs65Dn mice030104 developmental biologymedicine.anatomical_structureHypocellularityPsicobiologianervous systembiology.proteinDown SyndromeKi67Neuroscience030217 neurology & neurosurgeryNeuroscienceFrontiers in Neuroscience
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A retrospective study of the characterization of Rickettsia species in ticks collected from humans

2017

Rickettsiae (family Rickettsiaceae, order Rickettsiales) are obligate intracellular bacteria transmitted by arthropod vectors. Several Rickettsia species causing vector-borne rickettsioses belong to the spotted fever group (SFG). Traditionally, Rickettsia conorii has been considered as the main etiologic agent of Mediterranean spotted fever. However, the molecular characterization of rickettsiae allowed identifying other species involved in spotted fever in the Mediterranean region. In this study, 42 ticks collected from humans were subjected to morphological identification and molecular characterization of Rickettsia species potentially involved in human rickettsiosis in Sicily. Fourteen t…

0301 basic medicineanimal structuresRhipicephalus sanguineusHyalomma marginatum030231 tropical medicine030106 microbiologyBacterial ProteinTickTicks rickettsia spotted fever group humans zoonosis molecular analysisMicrobiologyMicrobiology03 medical and health sciencesZoonosis0302 clinical medicineTicksBacterial ProteinsZoonosiRetrospective Studieparasitic diseasesmedicineAnimalsHumansRickettsiaSicilyRetrospective StudiesRickettsia massiliaebiologyMolecular analysiAnimalMolecular analysisRickettsia InfectionRickettsia Infectionsbiology.organism_classificationmedicine.diseasebacterial infections and mycosesSpotted feverRickettsiaRickettsiosisInfectious DiseasesInsect ScienceSpotted fever groupbacteriaParasitologyRickettsia conoriiHumanTick
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