Search results for "rase"

showing 10 items of 4343 documents

Synthesis and biological evaluation of a D-ring-contracted analogue of lamellarin D

2017

A D-ring contracted analogue of the strongly cytotoxic marine pyrrole alkaloid lamellarin D was synthesized and investigated for its antiproliferative action towards a wild type and a multidrug resistant (MDR) cancer cell line. The compound was found to inhibit tumor cell growth at submicromolar concentrations and showed a lower relative resistance in the MDR cell line than the antitumor drug camptothecin to which lamellarin D shows cross resistance and with which lamellarin D shares the same binding site.

Cell SurvivalStereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic Agents010402 general chemistryHeterocyclic Compounds 4 or More Rings01 natural sciencesBiochemistrychemistry.chemical_compoundCoumarinsCell Line TumorDrug DiscoverymedicineHumansCytotoxic T cellheterocyclic compoundsBinding siteMolecular BiologyBinding Sites010405 organic chemistryChemistryAlkaloidOrganic ChemistryWild typeIsoquinolinesProtein Structure Tertiary0104 chemical sciencesG2 Phase Cell Cycle CheckpointsMolecular Docking SimulationMultiple drug resistanceDNA Topoisomerases Type IDrug Resistance NeoplasmMutagenesisCell cultureLamellarin DM Phase Cell Cycle CheckpointsMolecular MedicineTopoisomerase I InhibitorsCamptothecinmedicine.drugBioorganic & Medicinal Chemistry
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Enzyme-Controlled Nanodevice for Acetylcholine-Triggered Cargo Delivery Based on Janus Au–Mesoporous Silica Nanoparticles

2017

[EN] This work reports a new gated nanodevice for acetylcholine-triggered cargo delivery. We prepared and characterized Janus Au-mesoporous silica nanoparticles functionalized with acetylcholinesterase on the Au face and with supramolecular b-cyclodextrin: benzimidazole inclusion complexes as caps on the mesoporous silica face. The nanodevice is able to selectively deliver the cargo in the presence of acetylcholine via enzyme-mediated acetylcholine hydrolysis, locally lowering the pH and opening the supramolecular gate. Given the key role played by ACh and its relation with Parkinson's disease and other nervous system diseases, we believe that these findings could help design new therapeuti…

Cell SurvivalSupramolecular chemistryNanoparticleNanotechnologymacromolecular substances02 engineering and technology010402 general chemistry01 natural sciencesCatalysisQUIMICA ORGANICACIENCIA DE LOS MATERIALES E INGENIERIA METALURGICAQUIMICA ANALITICAmedicineOrganometallic CompoundsControlled releaseNanotechnologyHumansJanusNanodevicechemistry.chemical_classificationDrug CarriersChemistryHydrolysisQUIMICA INORGANICAOrganic Chemistrybeta-CyclodextrinsGeneral ChemistryMesoporous silicaHydrogen-Ion Concentration021001 nanoscience & nanotechnologyEnzymes ImmobilizedSilicon DioxideControlled releaseMesoporous materialsAcetylcholine0104 chemical sciencesEnzymeDoxorubicinAcetylcholinesteraseNanoparticlesBenzimidazolesGold0210 nano-technologyPorosityAcetylcholinemedicine.drugHeLa Cells
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Comparison of viability assays for Cryptosporidium parvum oocysts after disinfection.

2003

Abstract In order to test various viability assays for Cryptosporidium parvum oocysts were used to infect HCT-8 cells in vitro or baby mice. Infected cells were either stained with fluorescent anti- Cryptosporidium -antibody or lysed and subjected to C. parvum- specific PCR after 48 h. Titrations with infective oocysts were performed and compared to oocysts disinfected with Neopredisan © for 2 h at varying concentrations. Caecal smears and histological sections from infected animals were examined in parallel. The number of foci of parasite development in vitro after immunofluorescent staining correlated well with the infection dose. PCR was less quantifiable and the results were not always …

Cell Survivalanimal diseasesFluorescent Antibody TechniqueImmunofluorescencePolymerase Chain ReactionMicrobiologyCell LineCresolsMiceparasitic diseasesmedicineParasite hostingAnimalsCell SizeInfectivityCryptosporidium parvumGeneral Veterinarymedicine.diagnostic_testbiologyDose-Response Relationship DrugOocystsCryptosporidiumGeneral MedicineDNA Protozoanbiology.organism_classificationVirologyIn vitroStainingFungicides IndustrialDisinfectionCryptosporidium parvumbiology.proteinParasitologyAntibodyVeterinary parasitology
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mRNA-induction and cytokine release during in vitro exposure of human nasal respiratory epithelia to methyl methacrylate

2007

Abstract Background Methyl methacrylate (MMA) has been reported to cause histopathological changes in rodent nasal epithelium after inhalation challenges. Data in humans are lacking. Methods In this in vitro design 22 primary cell cultures taken from inferior turbinate tissue of healthy individuals were exposed to MMA concentrations of 50 ppm (German MAK-value) and 200 ppm. mRNA expression and cytokine release of inflammatory mediators were quantified after 4 h and after 24 h. Controls were exposed to synthetic air. Q-PCR analysis was performed for TNF-α, IL-1β, IL-6, IL-8, MCP-1, GMCSF, Cox-1 and Cox-2. ELISA assays were performed from culture supernatants for TNF-α, IL-1β, IL-6, IL-8, MCP…

Cell Survivalmedicine.medical_treatmentCell Culture TechniquesEnzyme-Linked Immunosorbent AssayInflammationMethylmethacrylateBiologyToxicologyAndrologyDownregulation and upregulationmedicineHumansRNA MessengerRespiratory systemCells CulturedChemokine CCL2Dose-Response Relationship DrugReverse Transcriptase Polymerase Chain ReactionTumor Necrosis Factor-alphaInterleukinsGranulocyte-Macrophage Colony-Stimulating FactorAntimutagenic AgentsEpithelial CellsGeneral MedicineEpitheliumIn vitroNasal MucosaDose–response relationshipCytokinemedicine.anatomical_structureGene Expression RegulationCyclooxygenase 2Cell cultureImmunologyCyclooxygenase 1Cytokinesmedicine.symptomToxicology Letters
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Anti-inflammatory effects of chemically modified tetracyclines by the inhibition of nitric oxide and interleukin-12 synthesis in J774 cell line

2001

We investigated the effects of chemically modified tetracyclines (CMTs) on the production of nitric oxide (NO) and on the synthesis of some cytokines: tumour necrosis factor alpha (TNF-alpha), interleukin(IL)-10 and IL-12 in lipopolysaccharide (LPS)-treated J774 cell line. Furthermore, we studied the ability of these drugs to modify the viability in LPS-stimulated J774 macrophages. CMTs decreased, in a dose-dependent manner, inducible NO synthase (iNOS) activity and, consequently, nitrite formation in J774 cultures. The CMT-induced decrease in NO production is due to the inhibition of enzyme activity rather than to a direct effect on enzyme expression. The absence of the inhibition in mRNA …

Cell Survivalmedicine.medical_treatmentImmunologyNitric Oxide Synthase Type IIApoptosisEnzyme-Linked Immunosorbent AssayNitric OxideCell LineNitric oxideMicechemistry.chemical_compoundEthidiumIn Situ Nick-End LabelingmedicineAnimalsImmunology and AllergyRNA MessengerViability assayEnzyme InhibitorsFluorescent DyesPharmacologybiologyReverse Transcriptase Polymerase Chain ReactionAnti-Inflammatory Agents Non-SteroidalInterleukinBiological activityInterleukin-12Acridine OrangeCell biologyNitric oxide synthaseInterleukin 10CytokinechemistryBiochemistryTetracyclinesApoptosisbiology.proteinCytokinesElectrophoresis Polyacrylamide GelIndicators and ReagentsNitric Oxide SynthaseInternational Immunopharmacology
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Corrigendum to "poly (ADP-ribose) polymerase inhibition synergizes with the NF-κB inhibitor DHMEQ to kill hepatocellular carcinoma cells" [Biochim. B…

2018

Fig. 1. The effects of the DHMEQ–Olaparib combination on HCC cells. (A) Cells were treated for 72 hwith the indicated concentrations of DHMEQ–Olaparib and cell viability was assessed by MTS assays. The DHMEQ–Olaparib combination showed synergistic inhibition of cell viability in Hep3B cells and additive inhibition in Huh7 cells. Combination index (CI) values are indicated above the bar. Data are expressed as percent cell growth and are the mean ± SD of three separate experiments (each of which was performed in triplicate). *p b 0.05 and **p b 0.01 versus each agent alone. (B) Cells were treated for 24 h with DHMEQ (μg/ml) or Olaparib (μM) alone or in combination, allowed to grow for 14 days…

Cell growthPoly ADP ribose polymeraseCellCaspase 3Cell BiologyTransfectionBiologyMolecular biologyOlaparibchemistry.chemical_compoundmedicine.anatomical_structurechemistryApoptosismedicineViability assayMolecular BiologyBiochimica et biophysica acta. Molecular cell research
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An unconventional role for miRNA: let-7 activates Toll-like receptor 7 and causes neurodegeneration

2011

Activation of innate immune receptors by host-derived factors exacerbates CNS damage, but the identity of these factors remains elusive. We uncovered an unconventional role for the microRNA let-7, a highly abundant regulator of gene expression in the CNS, in which extracellular let-7 activates the RNA-sensing Toll-like receptor (TLR) 7 and induces neurodegeneration through neuronal TLR7. Cerebrospinal fluid (CSF) from individuals with Alzheimer’s disease contains increased amounts of let-7b, and extracellular introduction of let-7b into the CSF of wild-type mice by intrathecal injection resulted in neurodegeneration. Mice lacking TLR7 were resistant to this neurodegenerative effect, but thi…

Cell signalingApoptosisElectrophoretic Mobility Shift AssayBiologyReal-Time Polymerase Chain ReactionMiceAlzheimer DiseasemicroRNAExtracellularmedicineAnimalsHumansReceptorIn Situ HybridizationMice KnockoutNeuronsToll-like receptorMembrane GlycoproteinsMicroscopy ConfocalInnate immune systemGeneral NeuroscienceNeurodegenerationBrainvirus diseasesTLR7medicine.diseaseImmunohistochemistryMice Inbred C57BLMicroRNAsHEK293 CellsToll-Like Receptor 7Nerve DegenerationCancer researchSignal TransductionNature Neuroscience
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Resveratrol reduces oxidative stress and cell death and increases mitochondrial antioxidants and XIAP in PC6.3-cells.

2010

Resveratrol, a polyphenol derived e.g. from red grapes, has been shown to mediate several positive biological actions such as protection of cells against oxidative stress. It can also influence cell signaling, but the mechanisms behind its antioxidant properties are largely unknown. Here we show that RSV reduces oxidative stress and enhances cell survival in PC6.3 cells depending on the concentration. In these cells, RSV increased the levels of antioxidants, SOD2 and TRX2, and of X chromosome-linked inhibitor of apoptosis protein. RSV also activated NFκB signaling as shown using luciferase reporter constructs. These findings show that RSV regulates oxidative stress and mitochondrial antioxi…

Cell signalingProgrammed cell deathBlotting WesternSOD2Settore BIO/11 - Biologia MolecolareApoptosisX-Linked Inhibitor of Apoptosis ProteinMitochondrionBiologyResveratrolmedicine.disease_causeInhibitor of apoptosisSettore BIO/09 - FisiologiaPolymerase Chain ReactionAntioxidantsCell LineMitochondrial Proteins03 medical and health scienceschemistry.chemical_compoundXIAP0302 clinical medicineThioredoxinsStilbenesmedicineTRX2Humans030304 developmental biologyNeurons0303 health sciencesSuperoxide DismutaseGeneral Neurosciencefood and beveragesROSSOD23. Good healthXIAPCell biologyMitochondriaOxidative StressBiochemistrychemistryResveratrolSettore BIO/14 - FarmacologiaOxidative stre030217 neurology & neurosurgeryOxidative stressNFκBNeuroscience letters
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Lafora disease fibroblasts exemplify the molecular interdependence between thioredoxin 1 and the proteasome in mammalian cells

2013

13 páginas, 8 figuras (que no aparecen en este documento, se pueden consultar en: http://www.sciencedirect.com/science/article/pii/S0891584913003274#ec0005)

Cell signalingProteasome Endopeptidase ComplexBlotting WesternFree radicalsBiologyBiochemistryLafora diseaseThioredoxin 1MiceThioredoxinsPhysiology (medical)medicineAnimalsHumansImmunoprecipitationLafora diseaseEndoplasmic Reticulum Chaperone BiPCell proliferationMicroscopy ConfocalProteasomeReverse Transcriptase Polymerase Chain ReactionEndoplasmic reticulumCell cycleFibroblastsSubcellular localizationmedicine.diseaseFlow CytometryCell biologyRare diseasesCytosolOxidative StressBiochemistryProteasomeLafora DiseaseUnfolded protein responseNIH 3T3 CellsAntioxidant enzymesOxidation-Reduction
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Endothelial transcriptomic changes induced by oxidized low density lipoprotein disclose an up-regulation of Jak-Stat pathway.

2015

Oxidized low density lipoproteins (oxLDLs) act as an etiological factor in the development of atherosclerosis by modifying the biological properties of endothelial cells through mechanisms of vascular inflammation. To deepen the oxLDL changes at cellular level, a transcriptomic analysis of human umbilical artery endothelial cells (HUAECs) treated with oxLDL was performed to identify the modified signaling pathways. Total RNA was isolated from HUAECs treated with oxLDL (100 μg/ml). Gene expression analysis was carried out using Affymetrix oligonucleotide microarrays. Biological pathway analysis was performed using Ingenuity Pathway Analysis software. Microarray assay demonstrated that oxLDL …

Cell signalingTime FactorsPhysiologyBlotting WesternBiologyReal-Time Polymerase Chain ReactionTransfectionGene Expression Regulation EnzymologicBiological pathwayTranscriptomeRNA interferenceGene expressionHuman Umbilical Vein Endothelial CellsHumansGene Regulatory NetworksProtein Kinase InhibitorsCells CulturedOligonucleotide Array Sequence AnalysisPharmacologyGene Expression ProfilingJAK-STAT signaling pathwaySTAT2 Transcription FactorJanus Kinase 1Janus Kinase 2Cell biologyEndothelial stem cellLipoproteins LDLSTAT1 Transcription FactorMolecular Medicinelipids (amino acids peptides and proteins)RNA InterferenceSignal transductionTranscriptomeSignal TransductionVascular pharmacology
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