Search results for "Lactones"

showing 10 items of 98 documents

Involvement of protein kinase Cdelta in contact-dependent inhibition of growth in human and murine fibroblasts.

2001

There is evidence that protein kinase C delta (PKCdelta) is a tumor suppressor, although its physiological role has not been elucidated so far. Since important anti-proliferative signals are mediated by cell-cell contacts we studied whether PKCdelta is involved in contact-dependent inhibition of growth in human (FH109) and murine (NIH3T3) fibroblasts. Cell-cell contacts were imitated by the addition of glutardialdehyde-fixed cells to sparsely seeded fibroblasts. Downregulation of the PKC isoforms alpha, delta, epsilon, and mu after prolonged treatment with 12-O-tetradecanoylphorbol-13-acetate (TPA, 0.1 microM) resulted in a significant release from contact-inhibition in FH109 cells. Bryosta…

Cancer ResearchTime FactorsBryostatin 1ImmunoprecipitationActive Transport Cell NucleusDown-RegulationBiologychemistry.chemical_compoundFixativesLactonesMiceDownregulation and upregulationGeneticsmedicineAnimalsHumansProtein IsoformsBenzopyransEnzyme InhibitorsFibroblastProtein kinase AMolecular BiologyProtein kinase CProtein Kinase CChemotaxisCell CycleAcetophenones3T3 CellsFibroblastsBryostatinsMolecular biologyBlotIsoenzymesProtein Kinase C-deltamedicine.anatomical_structurechemistryGlutaralTetradecanoylphorbol AcetateMacrolidesMitogensRottlerinCell DivisionProtein BindingOncogene
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Cytotoxic effects and degradation products of three mycotoxins: Alternariol, 3-acetyl-deoxynivalenol and 15-acetyl-deoxynivalenol in liver hepatocell…

2015

This work is focused in studying the cytotoxic effects on HepG2 cells of the mycotoxins alternariol (AOH), 3-acetyl-deoxynivalenol (3-ADON) and 15-acetyl-deoxynivalenol (15-ADON) by the MTT assay, as well as in the identification of the degradation products and/or metabolites originated after treatment by liquid chromatography tandem mass spectrometry (LC-MS/MS) equipment and extracted from culture media. HepG2 cells were treated at different concentrations over 24, 48 and 72 h. The IC50 values were from 65 to 96 μM, from 3.6 to 6.2 μM and from 5.2 to 8.1 μM for AOH, 3-ADON and 15-ADON, respectively. Among all three mycotoxins assayed, deoxynivalenol (DON) derivated presented the highest to…

Carcinoma HepatocellularTime FactorsCell SurvivalAlternariolToxicologyMass spectrometryInhibitory Concentration 50Lactoneschemistry.chemical_compoundTandem Mass SpectrometryLiquid chromatography–mass spectrometryHumansMTT assayCysteineMycotoxinBiotransformationChromatography Reverse-PhaseChromatographyDose-Response Relationship DrugLiver NeoplasmsHep G2 CellsGeneral MedicineGlutathioneSulfuric AcidsGlutathionechemistryTrichothecenesConjugateCysteineToxicology Letters
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Cytotoxicity and antileishmanial activity of Annona muricata pericarp

2000

Abstract Hexane, ethyl acetate and methanol extracts of Annona muricata pericarp were tested in vitro against Leishmania braziliensis and L. panamensis promastigotes, and against cell line U-937. The ethyl acetate extract was more active than the other extracts and even of Glucantime® used as reference substance. Its fractionation led to the isolation of three acetogenins — annonacin, annonacin A and annomuricin A.

Chemical structureAntiprotozoal AgentsEthyl acetateAnnonacinFractionationCell LineLactoneschemistry.chemical_compound4-ButyrolactoneDrug DiscoveryAnimalsHumansFuransMedicinal plantsCytotoxicityAnnona muricataLeishmaniaPharmacologyPlants MedicinalbiologyTraditional medicinePlant ExtractsGeneral Medicinebiology.organism_classificationLeishmania braziliensischemistryBiochemistryFitoterapia
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Interaction effects of enniatin B, deoxinivalenol and alternariol in Caco-2 cells.

2015

Enniatin B (ENN B), deoxinivalenol (DON) and alternariol (AOH) are secondary metabolites of filamentous fungi. These mycotoxins are contaminants of vegetables and cereals. They are cytotoxic and their effects are enhanced by their mixtures. The objectives of this study were to compare the cytotoxicity of ENN B, DON and AOH alone or in combination in human adenocarcinoma (Caco-2) cells and to evaluate the type of interactions of mycotoxin mixtures by the isobologram analysis. Cells were treated with concentrations ranging from 1.85 to 90μM (AOH) and from 0.312 to 10μM (for ENN B and DON), individually and in combination of two and three mycotoxins (from 1.85 to 30μM for AOH and from 0.312 to…

ChemistryStereochemistryCell SurvivalAlternariolFood Contamination04 agricultural and veterinary sciencesGeneral MedicineMycotoxinsToxicology040401 food scienceCellular viabilitychemistry.chemical_compoundLactones0404 agricultural biotechnologyCaco-2DepsipeptidesIc50 valuesHumansDrug InteractionsFood scienceCaco-2 CellsMycotoxinTrichothecenesCell survivalEnniatin BToxicology letters
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Anti-inflammatory drimane sesquiterpene lactones from an Aspergillus species

2014

Abstract IFN-γ inducible protein 10 (IP-10, CXCL10) is a 10 kDa chemokine, which is secreted from various cell types after exposure to pro-inflammatory stimuli. This chemokine is a ligand for the CXCR3 receptor and regulates immune responses by activating and recruiting leukocytes such as T cells, eosinophils, monocytes, and NK cells to sites of inflammation. Altered expression of CXCL10 has been associated with chronic inflammatory and infectious diseases and therefore CXCL10 represents a promising target for the development of new anti-inflammatory drugs. In a search for inhibitors of CXCL10 promoter activity, three structurally related drimane sesquiterpene lactones (compounds 1–3) were …

ChemokineCell SurvivalClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsInflammationCXCR3BiochemistryLactonesStructure-Activity RelationshipImmune systemDrug DiscoveryTumor Cells CulturedmedicineHumansCXCL10RNA MessengerReceptorMolecular BiologyCell ProliferationPolycyclic SesquiterpenesDose-Response Relationship DrugbiologyChemistryAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryBiological activityTransfectionMolecular biologyChemokine CXCL10AspergillusBiochemistrybiology.proteinMolecular MedicineDrug Screening Assays Antitumormedicine.symptomSesquiterpenesBioorganic & Medicinal Chemistry
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Lactones from the Sponge-Derived Fungus Talaromyces rugulosus.

2017

The marine-derived fungus Talaromyces rugulosus isolated from the Mediterranean sponge Axinella cannabina and cultured on solid rice medium yielded seventeen lactone derivatives including five butenolides (1–5), seven (3S)-resorcylide derivatives (6–12), two butenolide-resorcylide dimers (13 and 14), and three dihydroisocoumarins (15–17). Among them, fourteen compounds (1–3, 6–16) are new natural products. The structures of the isolated compounds were elucidated by 1D and 2D NMR (Nuclear Magnetic Resonance) spectroscopy as well as by ESI-HRMS (ElectroSpray Ionization-High Resolution Mass Spectrometry). TDDFT-ECD (Time-Dependent Density Functional Theory-Electronic Circular Dichroism) calcul…

Circular dichroismElectrosprayTalaromyces rugulosusStereochemistryPharmaceutical ScienceFungus010402 general chemistry01 natural sciences<i>Talaromyces rugulosus</i>; lactones; ECD calculation; cytotoxicityECD calculationArticlelactonesMiceTermészettudományok4-ButyrolactoneCell Line TumorDrug DiscoveryAnimalsLeukemia L5178Kémiai tudományokCytotoxicitylcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)Nuclear Magnetic Resonance Biomolecularchemistry.chemical_classificationBiological Productsbiology010405 organic chemistryChemistryCircular DichroismTalaromyces rugulosusbiology.organism_classification0104 chemical sciencesPoriferaSpongelcsh:Biology (General)Talaromycesddc:540cytotoxicityTwo-dimensional nuclear magnetic resonance spectroscopyLactoneMarine drugs
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Biochemical and chemical characterization of Cynara cardunculus L. extract and its potential use as co-adjuvant therapy of chronic myeloid leukemia

2017

Abstract Ethnopharmacological relevance Ancient mediterranean diet was characterized by consuming the spontaneous forms of Cynara cardunculus L. (CCL), commonly called artichoke. Cultivated and/or spontaneous forms of CC studies have demonstrated that methanol extract of CCL flower and/or cynaropicrin showed remarkable anti-proliferative activity in vitro models of leukocyte cancer cell. Aim of the study Chronic myeloid leukemia (CML) is associated with a reciprocal translocation of the long arms of chromosomes 9 and 22 generating the BCR/ABL fusion gene, translated in the p210 BCR/ABL oncoprotein kinase. This chimeric protein is the target of a kinase inhibitor, imatinib, but the developme…

Cynara cardunculus L.Sesquiterpene0301 basic medicineSettore MED/06 - Oncologia MedicaFusion Proteins bcr-ablPharmacologyAntineoplastic AgentLactoneschemistry.chemical_compound0302 clinical medicinehemic and lymphatic diseasesDrug DiscoveryK562 cellABLChemistryChronic myeloid leukemiabreakpoint cluster regionMyeloid leukemiaLactoneCynaropicrinImatinib resistantChemotherapy Adjuvant030220 oncology & carcinogenesisImatinib MesylateChronic myeloid leukemia; Cynara cardunculus L.; Imatinib resistant; K562 cells; P210BCR/ABLoncoprotein; Antineoplastic Agents; Antineoplastic Agents Phytogenic; Cell Survival; Chemotherapy Adjuvant; Cynara; Drug Resistance Neoplasm; Fusion Proteins bcr-abl; Humans; Imatinib Mesylate; K562 Cells; Lactones; Leukemia Myelogenous Chronic BCR-ABL Positive; Plant Extracts; Sesquiterpenes; Pharmacology; Drug Discovery3003 Pharmaceutical ScienceSesquiterpenesHumanmedicine.drugCell SurvivalAntineoplastic AgentsCynaraPlant Extract03 medical and health sciencesLeukemia Myelogenous Chronic BCR-ABL PositivemedicineHumansViability assayneoplasmsPharmacologyPlant ExtractsCell growthDrug Discovery3003 Pharmaceutical ScienceImatinibAntineoplastic Agents PhytogenicP210BCR/ABLoncoprotein030104 developmental biologyDrug Resistance NeoplasmCancer researchK562 CellsK562 cellsJournal of Ethnopharmacology
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Inhibition of pro-inflammatory enzymes by inuviscolide, a sesquiterpene lactone from Inula viscosa

2006

Abstract This work concerns the pharmacological activity of inuviscolide, a sesquiterpenoid from Inula viscosa. It exerts inhibitory effects on elastase, cyclooxygenase 1 and secretory phospholipase A2. Furthermore, it reduces the skin leukocyte infiltration in a murine model of dermatitis induced by repeated application of 12-O-tetradecanoylphorbol 13-acetate.

DermatitisBiologyPharmacognosyPharmacologySesquiterpene lactoneSesquiterpeneLactonesMicechemistry.chemical_compoundDrug DiscoveryLeukocytesAnimalsHumansEnzyme InhibitorsPharmacologychemistry.chemical_classificationPancreatic Elastaseintegumentary systemPlant ExtractsAnti-Inflammatory Agents Non-SteroidalElastaseBiological activityGeneral MedicineEnzymechemistryBiochemistrybiology.proteinTetradecanoylphorbol AcetateInulaCyclooxygenaseSesquiterpenesLactonePhytotherapyFitoterapia
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Fungal genes related to calcium homeostasis and signalling are upregulated in symbiotic arbuscular mycorrhiza interactions

2012

Fluctuations in intracellular calcium levels generate signalling events and regulate different cellular processes. Whilst the implication of Ca2+ in plant responses during arbuscular mycorrhiza (AM) interactions is well documented, nothing is known about the regulation or role of this secondary messenger in the fungal symbiont. The spatio-temporal expression pattern of putatively Ca2+-related genes of Glomus intraradices BEG141 encoding five proteins involved in membrane transport and one nuclear protein kinase, was investigated during the AM symbiosis. Expression profiles related to successful colonization of host roots were observed in interactions of G. intraradices with roots of wild-ty…

EXPRESSION[SDV]Life Sciences [q-bio]STRIGOLACTONESBiologySymbiosis-related plant mutantsPlant RootsCalcium in biologyFungal ProteinsRNA ACCUMULATIONCA2+Gene Expression Regulation FungalMycorrhizaeGene expressionBotanyMedicago truncatulaMedicagoGeneticsHomeostasis[SDV.BV]Life Sciences [q-bio]/Vegetal BiologyPLANTSGLOMUS-INTRARADICESGIGASPORA-ROSEAGlomeromycotaSymbiosisGeneEcology Evolution Behavior and SystematicsRegulation of gene expressionGene Expression ProfilingLasersMAGNAPORTHE-ORYZAEfungiMembrane transportbiology.organism_classificationMEDICAGO-TRUNCATULAMedicago truncatulaUp-RegulationCell biologyArbuscular mycorrhizaInfectious DiseasesMUTANTS[SDE]Environmental SciencesCalciumGlomus intraradicesGene expressionSignal transductionLaser microdissectionMicrodissectionSignal Transduction
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New Vocabulary for Bacterial Communication

2019

Abstract Quorum sensing (QS) is widely accepted as a procedure that bacteria use to converse. However, prevailing thinking places acyl homoserine lactones (AHLs) at the forefront of this communication pathway in Gram‐negative bacteria. With the advent of high‐throughput genomics and the subsequent influx of bacterial genomes, bioinformatics analysis has determined that the genes encoding AHL biosynthesis, originally discovered to be indispensable for QS (LuxI‐like proteins and homologues), are often absent in QS‐capable bacteria. Instead, the sensing protein (LuxR‐like proteins) is present with an apparent inability to produce any outgoing AHL signal. Recently, several signals for these Lux…

GenomicsCell CommunicationBacterial genome sizeComputational biologyAcyl-Butyrolactones010402 general chemistry01 natural sciencesBiochemistryDNA sequencing570 Life sciencesGram-Negative Bacteriabacterial communicationMolecular BiologyGeneAcyl-Homoserine Lactonesgene sequencingbiology010405 organic chemistryOrganic Chemistryquorum sensingfood and beveragesMinireviewsbiochemical phenomena metabolism and nutritionbiology.organism_classification0104 chemical sciencesQuorum sensingQuorum Quenchingquorum quenchingMolecular MedicineMinireviewbiosynthesisBacteria570 BiowissenschaftenChemBioChem
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