Search results for "Chromone"

showing 10 items of 11 documents

Chromone and phenanthrene alkaloids from Dennettia tripetala.

2002

Dennettine, a new 2,6-dimethoxychromone and three known phenanthrene alkaloids (uvariopsine, stephenanthrine and argentinine) in addition to the phenolic and known compound vanillin were isolated from the roots of Dennettia tripetala. Their structures were determined by physical and spectroscopical one dimensional (1D) and 2D-NMR analysis, including heteronuclear multiple bond correlation and nuclear Overhauser enhancement spectroscopy.

Magnetic Resonance SpectroscopyTertiary amineStereochemistryAnnonaceaePharmacognosyPlant RootsStephenanthrinechemistry.chemical_compoundAlkaloidsDrug DiscoveryOrganic chemistrySpectroscopyDennettia tripetalabiologyMolecular StructureVanillinUvariopsineGeneral ChemistryGeneral MedicineNuclear magnetic resonance spectroscopyPhenanthrenePhenanthrenesbiology.organism_classificationchemistryHeteronuclear moleculeAnnonaceaeChromonesChromoneChemicalpharmaceutical bulletin
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Effect of LIF-withdrawal on acetylcholine synthesis in the embryonic stem cell line CGR8 is not mediated by STAT3, PI3Ks or cAMP/PKA pathways.

2015

Acetylcholine (ACh) acts as a local cellular signaling molecule and is widely expressed in nature, including mammalian cells and embryonic stem cells. The murine embryonic stem cell line CGR8 synthesizes and releases substantial amounts of ACh. Particularly during early differentiation - a period associated with multiple alterations in geno-/phenotype functions - synthesis and release of ACh are increased by 10-fold. In murine stem cells second messengers of the STAT-3, PI3K and cAMP/PKA pathways are involved in maintaining self-renewal and pluripotency. The present experiments were designed to test whether blockers of these signaling pathways enhance ACh cell content in the presence of LIF…

STAT3 Transcription FactorCell signalingCurcuminMorpholinesImmunologyBiologyLeukemia Inhibitory FactorGene Expression Regulation Enzymologicchemistry.chemical_compoundMicePhosphatidylinositol 3-KinasesCyclic AMPImmunology and AllergyAnimalsLY294002PI3K/AKT/mTOR pathwayEmbryonic Stem CellsPharmacologySulfonamidesForskolinColforsinIsoquinolinesEmbryonic stem cellCyclic AMP-Dependent Protein KinasesAcetylcholineCell biologychemistryChromonesSecond messenger systemSignal transductionStem cellSignal TransductionInternational immunopharmacology
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Retinoids as a Perspective in Treatment of Alzheimer’s Disease

2010

<i>Background:</i> In the past, we demonstrated that the disintegrin metalloproteinase ADAM10 has α-secretase activity in vitro and in cultured cells. We also found out that moderate overexpression of this proteinase inhibits Aβ peptide production and prevents the formation of amyloid plaques in an Alzheimer’s disease (AD) mouse model. Moreover, it corrects early hippocampal defects like LTP impairment and increases cortical synaptogenesis. <i>Objective:</i> Upregulation of ADAM10 might be an alternative approach concerning AD therapy. Our current research therefore focuses on substances and/or pathways which regulate ADAM10 gene expression. <i>Methods:</i&g…

endocrine systemMorpholinesADAM10DiseaseBiologyADAM10 ProteinMiceNeuroblastomaRetinoidsPromoter activityCell Line TumorDisintegrinAnimalsHumansEnzyme InhibitorsMetalloproteinaseDose-Response Relationship DrugTerpenesPerspective (graphical)Membrane ProteinsVitaminshumanitiesIn vitroUp-Regulationcarbohydrates (lipids)ADAM ProteinsNeurologyChromonesImmunologyCancer researchbiology.proteinNeurology (clinical)Amyloid Precursor Protein SecretasesSignal TransductionNeurodegenerative Diseases
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Leptin and leptin receptor expression in asthma.

2009

Background The adipokine leptin is a potential new mediator for bronchial epithelial homeostasis. Asthma is a chronic inflammatory disease characterized by airway remodeling that might affect disease chronicity and severity. TGF-β is a tissue growth factor the dysregulation of which is associated with airway remodeling. Objective We sought to determine whether a bronchial epithelial dysfunction of the leptin/leptin receptor pathway contributes to asthma pathogenesis and severity. Methods We investigated in vitro the presence of leptin/leptin receptor on human bronchial epithelial cells. Then we studied the effect of TGF-β and fluticasone propionate on leptin receptor expression. Finally, th…

AdultLeptinMalemedicine.medical_specialtyPyridinesMorpholinesImmunologyAdipokineBronchiRespiratory MucosaSettore MED/10 - Malattie Dell'Apparato RespiratorioSettore BIO/09 - FisiologiaCell LinePathogenesisTransforming Growth Factor beta1Leptin leptin receptor severe asthma epithelium TGF-b remodelingInternal medicineImmunology and AllergyMedicineHumansEnzyme InhibitorsReceptorCell ProliferationLeptin receptorbusiness.industryTumor Necrosis Factor-alphaLeptindigestive oral and skin physiologyImidazolesMiddle AgedEpitheliumAsthmaRecombinant Proteinsrespiratory tract diseasesAndrostadienesmedicine.anatomical_structureEndocrinologyChromonesImmunologyFluticasoneReceptors LeptinFemalebusinesshormones hormone substitutes and hormone antagonistsEx vivoTransforming growth factorThe Journal of allergy and clinical immunology
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Rhodium catalyzed oxidative coupling of salicylaldehydes with diazabicyclic olefins: a one pot strategy involving aldehyde C–H cleavage and π-allyl c…

2013

An efficient one pot strategy for the synthesis of cyclopentene fused chromanone derivatives through the direct oxidative coupling of salicylaldehydes with bicyclic olefins in the presence of a rhodium-copper catalyst system is described. This is the first report on the ring opening-ring closing of bicyclic hydrazines via metal catalyzed oxidative coupling reaction.

chemistry.chemical_elementAlkenesRing (chemistry)Medicinal chemistryAldehydeCatalysisCatalysisRhodiumchemistry.chemical_compoundMaterials ChemistryOrganic chemistryMoleculeCyclopenteneRhodiumta116chemistry.chemical_classificationAldehydesAza CompoundsMolecular StructureOxidative CouplingBicyclic moleculeMetals and AlloysGeneral ChemistrySurfaces Coatings and FilmsElectronic Optical and Magnetic MaterialschemistryChromonesCyclizationCeramics and CompositesOxidative coupling of methaneChemical Communications
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TRAIL-R4 promotes tumor growth and resistance to apoptosis in cervical carcinoma HeLa cells through AKT.

2011

International audience; BACKGROUND: TRAIL/Apo2L is a pro-apoptotic ligand of the TNF family that engages the apoptotic machinery through two pro-apoptotic receptors, TRAIL-R1 and TRAIL-R2. This cell death program is tightly controlled by two antagonistic receptors, TRAIL-R3 and TRAIL-R4, both devoid of a functional death domain, an intracellular region of the receptor, required for the recruitment and the activation of initiator caspases. Upon TRAIL-binding, TRAIL-R4 forms a heteromeric complex with the agonistic receptor TRAIL-R2 leading to reduced caspase-8 activation and apoptosis. METHODOLOGY/PRINCIPAL FINDINGS: We provide evidence that TRAIL-R4 can also exhibit, in a ligand independent…

Proliferation indexlcsh:MedicineTNF-Related Apoptosis-Inducing LigandHeLaMicePhosphatidylinositol 3-Kinases0302 clinical medicineMolecular Cell BiologyBasic Cancer ResearchMembrane Receptor SignalingEnzyme Inhibitorslcsh:SciencePhosphoinositide-3 Kinase Inhibitors0303 health sciencesMultidisciplinaryCell Deathbiologyapoptosis3. Good healthCell biologyOncology030220 oncology & carcinogenesisMedicineFemaleSignal transductionResearch ArticleSignal TransductionProgrammed cell deathMorpholinesproliferationBlotting WesternMice Nude03 medical and health sciencesTRAIL-R4[SDV.BBM] Life Sciences [q-bio]/Biochemistry Molecular BiologyAnimalsHumans[SDV.BBM]Life Sciences [q-bio]/Biochemistry Molecular BiologyBiology[ SDV.BBM ] Life Sciences [q-bio]/Biochemistry Molecular BiologyProtein kinase BPI3K/AKT/mTOR pathwayCell Proliferation030304 developmental biologyCell growthAktCell Membranelcsh:RPTEN PhosphohydrolaseNeoplasms Experimentalbiology.organism_classificationTumor Necrosis Factor Decoy ReceptorsChromonesApoptosislcsh:QProto-Oncogene Proteins c-aktHeLa Cells
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Rad51 and BRCA2 - New Molecular Targets for Sensitizing Glioma Cells to Alkylating Anticancer Drugs

2011

First line chemotherapeutics for brain tumors (malignant gliomas) are alkylating agents such as temozolomide and nimustine. Despite growing knowledge of how these agents work, patients suffering from this malignancy still face a dismal prognosis. Alkylating agents target DNA, forming the killing lesion O(6)-alkylguanine, which is converted into DNA double-strand breaks (DSBs) that trigger apoptosis. Here we assessed whether inhibiting repair of DSBs by homologous recombination (HR) or non-homologous end joining (NHEJ) is a reasonable strategy for sensitizing glioma cells to alkylating agents. For down-regulation of HR in glioma cells, we used an interference RNA (iRNA) approach targeting Ra…

Cancer Treatmentlcsh:MedicineApoptosisToxicologyBiochemistrychemistry.chemical_compoundDrug DiscoveryRNA Small Interferinglcsh:ScienceHomologous RecombinationNeurological TumorsGene knockdownMultidisciplinaryBrain NeoplasmsGliomaFlow CytometryNon-homologous end joiningOncologyPARP inhibitorMedicinemedicine.drugResearch ArticleBiotechnologyDrugs and DevicesDrug Research and DevelopmentDNA damageMorpholinesToxic AgentsOlaparibGliomaCell Line TumormedicineHumansBiologyAntineoplastic Agents AlkylatingProtein Kinase InhibitorsBRCA2 ProteinTemozolomideBase SequenceNimustinelcsh:RCancers and NeoplasmsChemotherapy and Drug Treatmentmedicine.diseasechemistryMicroscopy FluorescenceChromonesCancer researchlcsh:QRad51 RecombinaseDNA DamagePLoS ONE
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Estrogen Receptor Signaling and the PI3K/Akt Pathway Are Involved in Betulinic Acid-Induced eNOS Activation

2016

Betulinic acid (BA) is a naturally occurring pentacyclic triterpenoid with anti-inflammatory, antiviral and anti-cancer properties. Beneficial cardiovascular effects such as increased nitric oxide (NO) production through enhancement of endothelial NO synthase (eNOS) activity and upregulation of eNOS expression have been demonstrated for this compound. In the present study, immortalized human EA.hy 926 endothelial cells were incubated for up to 1 h with 1–100 µM BA and with the phosphatidylinositol-3-kinase (PI3K) inhibitors LY294002 and wortmannin, or the estrogen receptor (ER) antagonist ICI 182,780. Phosphorylation status of eNOS and total eNOS protein were analyzed by Western blotting us…

0301 basic medicinePharmaceutical ScienceEstrogen receptorPI3KAnalytical ChemistryWortmanninchemistry.chemical_compound0302 clinical medicineEnosDrug DiscoveryLY294002PhosphorylationFulvestrantLungbiologyEstradiolendothelial cellsReceptors EstrogenChemistry (miscellaneous)030220 oncology & carcinogenesisMolecular MedicinePhosphorylationSignal transductionPentacyclic TriterpenesWortmanninSignal Transductionestrogen receptormedicine.medical_specialtyNitric Oxide Synthase Type IIIMorpholinesArticleCell Linelcsh:QD241-44103 medical and health sciencesbetulinic acidlcsh:Organic chemistryInternal medicinemedicineAnimalsHumansPhysical and Theoretical ChemistryProtein kinase BPI3K/AKT/mTOR pathwayendothelial nitric oxide synthaseAktOrganic ChemistryFibroblastsbiology.organism_classificationMolecular biologyTriterpenesbetulinic acid; endothelial nitric oxide synthase; endothelial cells; estrogen receptor; PI3K; AktRatsAndrostadienes030104 developmental biologyEndocrinologychemistryGene Expression RegulationChromonesPhosphatidylinositol 3-KinaseProto-Oncogene Proteins c-aktMolecules
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Targeting DNA double strand break repair with hyperthermia and DNA-PKcs inhibition to enhance the effect of radiation treatment

2016

// Bregje van Oorschot 1 , Giovanna Granata 1 , Simone Di Franco 2 , Rosemarie ten Cate 1 , Hans M. Rodermond 1 , Matilde Todaro 3 , Jan Paul Medema 1 , Nicolaas A.P. Franken 1 1 Laboratory for Experimental Oncology and Radiobiology (LEXOR), Center for Experimental Molecular Medicine, Department of Radiation Oncology, Academic Medical Center, Cancer Genomics Center, Amsterdam, The Netherlands 2 Department of Surgical, Oncological and Stomatological Sciences (DICHIRONS), Cellular and Molecular Pathophysiology Laboratory, University of Palermo, Palermo, Italy 3 Biomedical Department of Internal and Specialistic Medicine (DIBIMIS), University of Palermo, Palermo, Italy Correspondence to: Nicol…

double-strand break0301 basic medicineRadiation-Sensitizing AgentsPathologymedicine.medical_specialtyDNA End-Joining RepairRadiobiologyDNA repairDNA damageMorpholinesmedicine.medical_treatmentMice NudeUterine Cervical NeoplasmsDNA repairBreast NeoplasmsDNA-Activated Protein KinaseRadiation ToleranceMice03 medical and health sciences0302 clinical medicineCancer stem cellTumor Cells CulturedAnimalsHumansMedicineDNA Breaks Double-StrandedHomologous RecombinationDNA-PKcsdouble-strand breaksRadiotherapybusiness.industryCancerradiation oncologyHyperthermia Inducedhyperthermiamedicine.diseaseRadiation therapyradiation oncology.030104 developmental biologyOncologyChromones030220 oncology & carcinogenesisCancer cellNeoplastic Stem CellsCancer researchFemalebusinessResearch PaperDNA DamageOncotarget
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Control of ovarian steroidogenesis by insulin-like peptides in the blowfly (Phormia regina).

2004

0022–0795/04/0181–147; This study investigated the ability of insulin and of insect insulin-like peptides (ILPs) to stimulate ovarian steroidogenesis in the blowfly Phormia regina. Bovine insulin was active on ovaries isolated in vitro, which showed an age-dependent sensitivity; this peptide progressively stimulated steroidogenesis in ovaries isolated from the third day after adult molt, but not in younger ones, and had maximal activity after the fifth day. This stimulatory effect was observed equally from females reared in the presence or in the absence of males, excluding a regulatory effect of mating. The mode of action of insulin in blowflies did not involve cAMP, but triggered a specif…

medicine.medical_specialtyTime FactorsEndocrinology Diabetes and Metabolismmedicine.medical_treatmentMorpholinesEndogenyblowflychemistry.chemical_compoundPhosphatidylinositol 3-KinasesEndocrinologyOrgan Culture TechniquesInternal medicineControlmedicineAnimalsInsulinPhosphatidylinositolPI3K/AKT/mTOR pathwayPhosphoinositide-3 Kinase InhibitorsbiologyInsulinDipteraNeuropeptidesOvaryEstrogensPhormia reginabiology.organism_classificationinsulin-like peptidesIn vitroStimulation ChemicalInsulin receptorEndocrinologychemistryChromonesPhormia reginaInsect Hormonesbiology.proteinCattleFemaleovarian steroidogenesisSignal transductionThe Journal of endocrinology
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