Search results for "pero"

showing 10 items of 3365 documents

Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.

2013

Chagas disease is today one of the most important neglected diseases for its upcoming expansion to non-endemic areas and has become a threat to blood recipients in many countries. In this study, the trypanocidal activity of ten derivatives of a family of aza-scorpiand like macrocycles is evaluated against Trypanosoma cruzi in vitro and in vivo murine model in which the acute and chronic phases of Chagas disease were analyzed. The compounds 4, 3 and 1 were found to be more active against the parasite and less toxic against Vero cells than the reference drug benznidazole, 4 being the most active compound, particularly in the chronic phase. While all these compounds showed a remarkable degree …

Chagas diseaseMacrocyclic CompoundsTrypanosoma cruziAntiprotozoal AgentsLigandsMicrobiologyMiceIn vivoDrug DiscoveryChlorocebus aethiopsmedicineEscherichia coliAnimalsHumansTrypanosoma cruziVero CellsCells CulturedPharmacologychemistry.chemical_classificationAza CompoundsMice Inbred BALB CbiologyMolecular StructureSuperoxide DismutaseOrganic ChemistryGeneral Medicinebiology.organism_classificationmedicine.diseaseIn vitroDisease Models AnimalEnzymechemistryMechanism of actionBenznidazoleImmunologyChronic DiseaseVero cellFemalemedicine.symptommedicine.drugEuropean journal of medicinal chemistry
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Synthesis and pharmacological evaluation of 2'-hydroxychalcones and flavones as inhibitors of inflammatory mediators generation.

1995

2'-Hydroxy-3,4-dimethoxy-3',4'-dimethylchalcone (3a), 2'-hydroxy-3',4',3,4-tetramethoxychalcone (3b), and their corresponding flavones, 3',4'-dimethoxy-7,8-dimethylflavone (4a) and 3',4',7,8-tetramethoxyflavone (4b), were prepared from 3,4-dimethoxycinnamic acid and the respective phenol. The four compounds inhibited enzymic lipid peroxidation and showed weak peroxyl scavenging activity. They also reduced LTB 4 release from human neutrophils stimulated by A23187. The chalcone 3b was the only compound able to inhibit in a concentration-dependent way, synovial human recombinant phospholipase A 2 activity, human platelet TXB 2 generation, and human neutrophil degranulation. This chalcone exert…

ChalconeAntioxidantNeutrophilsmedicine.medical_treatmentFlavonoidChemical synthesisFlavonesCell DegranulationPhospholipases ALipid peroxidationchemistry.chemical_compoundMiceChalconeChalconesDrug DiscoverySynovial FluidmedicineAnimalsHumanschemistry.chemical_classificationFlavonoidsPhospholipase APancreatic ElastaseChemistryDegranulationFree Radical ScavengersPhospholipases A2BiochemistryMolecular MedicineEicosanoidsLipid PeroxidationInflammation MediatorsJournal of medicinal chemistry
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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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Synthesis and anti-inflammatory activity of chalcone derivatives

1998

Chalcones and their derivatives were synthesized and evaluated for their anti-inflammatory activity. In vitro, chalcones 2, 4, 8, 10 and 13 inhibited degranulation and 5-lipoxygenase in human neutrophils, whereas 11 behaved as scavenger of superoxide. Only four compounds (4-7) inhibited cyclo-oxygenase-2 activity. The majority of these samples showed anti-inflammatory effects in the mouse air pouch model.

ChalconeNeutrophilsmedicine.drug_classLeukotriene B4Clinical BiochemistryPharmaceutical ScienceLeukotriene B4BiochemistryChemical synthesisAnti-inflammatoryMiceStructure-Activity Relationshipchemistry.chemical_compoundChalconeIn vivoDrug DiscoverymedicineAnimalsHumansCyclooxygenase InhibitorsLipoxygenase InhibitorsMolecular BiologyPropiophenonesArachidonate 5-LipoxygenaseCyclooxygenase 2 InhibitorsMolecular StructureChemistrySuperoxideAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryDegranulationMembrane ProteinsIn vitroIsoenzymesBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesDrug DesignMolecular MedicineBioorganic & Medicinal Chemistry Letters
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Chaperones: General Characteristics and Classifications

2013

This chapter presents the classification of chaperones, their molecular properties among which that of forming functional complexes involving various molecules, and their distribution inside and outside the cell. The chaperone genes in the human genome are listed and briefly described, focusing on the small heat-shock proteins (sHsp), Hsp60, Hsp70, and Hsp90, and mentioning all others known. The chapter also introduces the concept of chaperoning system, i.e., the physiological system of an organism which is composed of all its chaperones, co-chaperones, and chaperone co-factors.

Chaperone (protein)biology.proteinHuman genomeComputational biologyBiologyOrganism
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CtsR is the master regulator of stress response gene expression in Oenococcus oeni.

2005

ABSTRACT Although many stress response genes have been characterized in Oenococcus oeni , little is known about the regulation of stress response in this malolactic bacterium. The expression of eubacterial stress genes is controlled both positively and negatively at the transcriptional level. Overall, negative regulation of heat shock genes appears to be more widespread among gram-positive bacteria. We recently identified an ortholog of the ctsR gene in O. oeni . In Bacillus subtilis , CtsR negatively regulates expression of the clp genes, which belong to the class III family of heat shock genes. The ctsR gene of O. oeni is cotranscribed with the downstream clpC gene. Sequence analysis of t…

ChaperoninsOperonMolecular Sequence DataBiologyMicrobiologyGenome03 medical and health sciencesBacterial ProteinsSigma factorHeat shock proteinOperon[SDV.BBM]Life Sciences [q-bio]/Biochemistry Molecular BiologyGene RegulationPromoter Regions GeneticMolecular BiologyGeneHeat-Shock Proteins030304 developmental biologyRegulator geneOenococcus oeniGeneticsRegulation of gene expressionAdenosine Triphosphatases0303 health sciencesBase Sequence030306 microbiologyCTSRGene Expression Regulation Bacterialbiology.organism_classificationDNA-Binding ProteinsGram-Positive CocciRepressor ProteinsMutagenesis Site-DirectedOenococcus oeniGenome BacterialHeat-Shock ResponseBacillus subtilisMolecular ChaperonesJournal of bacteriology
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Human chaperonin disease-causing mutations: study with a prokaryotic model.

2012

Chaperonopathies HspsSettore CHIM/08 - Chimica Farmaceutica
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Myelin pathology: Involvement of molecular chaperones and the promise of chaperonotherapy

2019

The process of axon myelination involves various proteins including molecular chaperones. Myelin alteration is a common feature in neurological diseases due to structural and functional abnormalities of one or more myelin proteins. Genetic proteinopathies may occur either in the presence of a normal chaperoning system, which is unable to assist the defective myelin protein in its folding and migration, or due to mutations in chaperone genes, leading to functional defects in assisting myelin maturation/migration. The latter are a subgroup of genetic chaperonopathies causing demyelination. In this brief review, we describe some paradigmatic examples pertaining to the chaperonins Hsp60 (HSPD1,…

ChaperonotherapyMyelinopathiechaperonopathiescctlcsh:RC321-571Chaperonin03 medical and health sciencesMyelin0302 clinical medicinemedicineAxonlcsh:Neurosciences. Biological psychiatry. NeuropsychiatryGene030304 developmental biologyMyelinopathies0303 health sciencesbiologyGeneral NeuroscienceHsp60medicine.anatomical_structureMyelinChaperone (protein)PerspectiveProteinopathiesbiology.proteinChaperonopathiemyelinopathiesHSP60Neuroscience030217 neurology & neurosurgeryMyelin pathology
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Working Principles of Perovskite Solar Cells

2018

Charge generationMaterials science02 engineering and technology010402 general chemistry021001 nanoscience & nanotechnology0210 nano-technology01 natural sciencesEngineering physics0104 chemical sciencesPerovskite (structure)
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Thermodynamic stability of stoichiometric LaFeO 3 and BiFeO 3 : a hybrid DFT study

2017

BiFeO3 perovskite attracts great attention due to its multiferroic properties and potential use as a parent material for Bi1−xSrxFeO3−δ and Bi1−xSrxFe1−yCoyO3−δ solid solutions in intermediate temperature cathodes of oxide fuel cells. Another iron-based LaFeO3 perovskite is the end member for well-known solid solutions (La1−xSrxFe1−yCoyO3−δ) used for oxide fuel cells and other electrochemical devices. In this study an ab initio hybrid functional approach was used for the study of the thermodynamic stability of both LaFeO3 and BiFeO3 with respect to decompositions to binary oxides and to elements, as a function of temperature and oxygen pressure. The localized (LCAO) basis sets describing th…

ChemistryAb initioOxideGeneral Physics and AstronomyThermodynamics02 engineering and technology010402 general chemistry021001 nanoscience & nanotechnology01 natural sciences7. Clean energy0104 chemical sciencesHybrid functionalchemistry.chemical_compoundLinear combination of atomic orbitalsAtomPhysical chemistryChemical stabilityPhysical and Theoretical Chemistry0210 nano-technologyPerovskite (structure)Phase diagramPhysical Chemistry Chemical Physics
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