Search results for "SHI"

showing 10 items of 9733 documents

Clinical effect of toothpaste and mouth rinse containing zinc lactate on oral malodor reduction

2019

Background This study aimed to investigate the effect of toothpaste and mouth rinse containing 0.14% zinc lactate on the reduction of three volatile oral malodor gases. Material and Methods Ten subjects with good health were recruited to take part in a crossover design study with a 7-day washout period. They were randomly assigned to use the test (toothpaste and rinse containing 0.14% zinc lactate) or placebo (negative control) treatment regimens within the two-week period. All subjects were asked to refrain from tooth brushing and eating in the morning prior to the gas collection periods. The assessment of malodor measured the quantity of three volatile sulphur compounds (VSCs) using an Or…

0301 basic medicineToothpastebusiness.product_categorybusiness.industryResearch030106 microbiologyDentistry030206 dentistry:CIENCIAS MÉDICAS [UNESCO]PlaceboCrossover studyOral hygieneCommunity and Preventive DentistryTooth brushing03 medical and health sciencesRegimen0302 clinical medicineUNESCO::CIENCIAS MÉDICASMouth rinseMedicinebusinessGeneral DentistryMorningJournal of Clinical and Experimental Dentistry
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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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Evaluation of scientific output in Dentistry in Spanish Universities

2016

Background: The aim of this study was to assess the scientific output of Spanish universities that offer a bachelor’s degree in dentistry through the use of various bibliometric indicators. Material and Methods: A total of 21 universities offered a bachelor’s degree in dentistry in academic year 2016- 2017. The search for papers published by authors associated with these institutions was carried out using the selection of journals listed in the Journal Citation Reports (JCR) and the Web of Knowledge database for the period 1986-2017. On the basis of these data, we determined the output, the h-, g- and hg-indexes, the most productive authors, international collaborations, and the most releva…

0301 basic medicineUniversitiesOral surgerymedia_common.quotation_subjectLibrary scienceDentistryUniversitatsBachelorOdontologia03 medical and health sciencesInvestigació0302 clinical medicineCitation rateMedicineImpact factorGeneral Dentistrymedia_commonRecercaPublishingUniversityAcademic yearImpact factorbusiness.industryResearch:CIENCIAS MÉDICAS [UNESCO]030104 developmental biologyOtorhinolaryngologyKnowledge baseSpain030220 oncology & carcinogenesisDentistryUNESCO::CIENCIAS MÉDICASSurgeryJournal Impact FactorOral SurgerybusinessCitationH-indexOral medicine
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Seasonal recovery ofEdwardsiella piscicidafrom wild European eels and natural waters: Isolation methods, virulence and reservoirs

2018

A total of 127 wild eels caught in the L'Albufera Lake (Spain) and 24 samples of lagoon freshwater were analysed for 1-year period. Edwardsiella strains were isolated from liver/kidney on TSA-1 plates in 31.9% of total diseased specimens, and the edwardsiellosis prevalence in the fishery was of 11.8%. The use of double-strength Salmonella-Shigella (DSSS) broth and SS agar yielded Edwardsiella isolation from intestine in 100% of those edwardsiellosis-diseased eels, but also in 40.4% of other sick fish with vibriosis or aeromonosis and in 28.8% of healthy eels, as well as from freshwater in 8.3% of samples. Pure cultures were isolated on SS agar from the former, but motile Aeromonas, Plesiomo…

0301 basic medicineVeterinary medicineanimal structuresfood.ingredientVeterinary (miscellaneous)030106 microbiologyVirulenceAquatic ScienceBiologyFish Diseases03 medical and health sciencesfoodPrevalenceAnimalsAgarVirulenceEdwardsiella piscicidaIncidenceEnterobacteriaceae InfectionsAnguillabiology.organism_classificationIsolation (microbiology)LakesEdwardsiellaAeromonasSpainPlesiomonas shigelloidesEdwardsiellaBacteriaJournal of Fish Diseases
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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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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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Effects of Pimozide Derivatives on pSTAT5 in K562 Cells

2017

STAT5 is a transcription factor, a member of the STAT family of signaling proteins. STAT5 is involved in many types of cancer, including chronic myelogenous leukemia (CML), in which this protein is found constitutively activated as a consequence of BCR-ABL expression. The neuroleptic drug pimozide was recently reported to act as an inhibitor of STAT5 phosphorylation and is capable of inducing apoptosis in CML cells in vitro. Our research group has synthesized simple derivatives of pimozide with cytotoxic activity and that are able to decrease the levels of phosphorylated STAT5. In this work we continued the search for novel STAT5 inhibitors, synthesizing compounds in which the benzoimidazol…

0301 basic medicineantiproliferationApoptosisPharmacologyBiochemistryAntineoplastic Agent0302 clinical medicinePimozidehemic and lymphatic diseasesDrug DiscoverySTAT5 Transcription FactorCytotoxic T cellPhosphorylationGeneral Pharmacology Toxicology and PharmaceuticsBCR-ABL-expressing leukemia; STAT5 inhibitors; antiproliferation; apoptosis; pimozideSTAT5Molecular StructurebiologyPimozidefood and beverages030220 oncology & carcinogenesisMolecular MedicinePhosphorylationHumanmedicine.drugAntineoplastic AgentsNOStructure-Activity Relationship03 medical and health sciencesK562 CellmedicineHumansTranscription factorCell ProliferationPharmacologyDose-Response Relationship DrugCell growthSTAT5 inhibitorsOrganic ChemistryApoptosiSTAT5 inhibitormedicine.disease030104 developmental biologyPharmacology Toxicology and Pharmaceutics (all)biology.proteinCancer researchBCR-ABL-expressing leukemiaDrug Screening Assays AntitumorK562 CellsK562 cellsChronic myelogenous leukemiaChemMedChem
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Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives

2018

A comprehensive set of 3-phenylcoumarin analogues with polar substituents was synthesised for blocking oestradiol synthesis by 17-b-hydroxysteroid dehydrogenase 1 (HSD1) in the latter part of the sulphatase pathway. Five analogues produced 62% HSD1 inhibition at 5 mM and, furthermore, three of them produced 68% inhibition at 1 mM. A docking-based structure-activity relationship analysis was done to determine the molecular basis of the inhibition and the cross-reactivity of the analogues was tested against oestrogen receptor, aromatase, cytochrome P450 1A2, and monoamine oxidases. Most of the analogues are only modestly active with 17-b-hydroxysteroid dehydrogenase 2 – a requirement for lowe…

0301 basic medicinearomatase17-Hydroxysteroid Dehydrogenasesmedicine.drug_classStereochemistry3-imidazolecoumarinaromataasiDehydrogenaseta3111LigandsStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundstructure-activity relationship (SAR)0302 clinical medicineCoumarinsIn vivo17-β-hydroxysteroid dehydrogenase 1 (HSD1)Drug DiscoverymedicineHumansMoietyEnzyme InhibitorsAromatasePharmacologyAromatase inhibitorDose-Response Relationship DrugEstradiolMolecular StructurebiologyChemistrylcsh:RM1-950CYP1A2ta1182General MedicineCoumarin3. Good healthMolecular Docking Simulationlcsh:Therapeutics. Pharmacology030104 developmental biologyDocking (molecular)030220 oncology & carcinogenesisbiology.proteinComputer-Aided Design3-Phenylcoumarinhormones hormone substitutes and hormone antagonistsResearch PaperJournal of Enzyme Inhibition and Medicinal Chemistry
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