Search results for "DISCOVERY"

showing 10 items of 4119 documents

Zum Einfluss von Xanthopterin auf Phosphatasen

1951

Die in einer fruheren Mitteilung zunachst als Xanthopterinwirkung gedeutete Erhohung der Phosphataseaktivitat in ungepufferten Ansatzen nachGreenstein beruht auf einer unspezifischen Salzwirkung.

Xanthopterinchemistry.chemical_compoundchemistryBiochemistryDrug DiscoveryPhosphataseMolecular MedicineGeneral MedicineMolecular medicineGenetics (clinical)Klinische Wochenschrift
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The effect of excipients on the stability and phase transition rate of xylazine hydrochloride and zopiclone

2015

The compatibility of thermodynamically unstable polymorph of two active pharmaceutical compounds (xylazine hydrochloride form X and zopiclone form C) with different excipients was investigated. The effects of the excipient and its amount in the sample on the thermal properties and possible chemical interactions were studied. The most commonly used excipients in the pharmaceutical industry - calcium carbonate, lactose hydrate, cellulose, magnesium stearate hydrate and calcium stearate hydrate were selected for this study. The dependence of the phase transition rate from an unstable to a more stable polymorph on the excipients and their amounts in the initial sample was analysed at 80°C, and …

XylazinePhase transitionDrug IndustryClinical BiochemistryPharmaceutical ScienceExcipientCalcium stearatePhase TransitionPiperazinesAnalytical ChemistryExcipientschemistry.chemical_compoundReaction rate constantDrug StabilityDrug DiscoverymedicineMagnesium stearateCelluloseSpectroscopyChromatographyTemperatureKineticsCalcium carbonatechemistryThermodynamicsHydrateAzabicyclo CompoundsNuclear chemistrymedicine.drugJournal of Pharmaceutical and Biomedical Analysis
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Cytotoxicity and modes of action of four Cameroonian dietary spices ethno-medically used to treat cancers: Echinops giganteus, Xylopia aethiopica, Im…

2013

Abstract Ethnopharmacological relevance. Echinops giganteus , Imperata cylindrica , Piper capense and Xylopia aethiopica are four medicinal spices used in Cameroon to treat cancers. Aim of the study The above plants previously displayed cytotoxicty against leukemia CCRF-CEM and CEM/ADR5000 cell lines as well as human pancreatic MiaPaCa-2 cells. The present study aims at emphasizing the study of the cytotoxicity and the modes of action of the above plants on a panel of ten cancer cell lines including various sensitive and drug-resistant phenotypes. The study has been extended to the isolation of the bioactive constituents from Echinops giganteus . Materials and methods The cytotoxicity of th…

Xylopia aethiopicaCell SurvivalCell Culture TechniquesApoptosisPoaceaeCell Line TumorDrug DiscoverymedicineCytotoxic T cellHumansCameroonSpicesCytotoxicityMedicine African TraditionalPharmacologyMembrane Potential MitochondrialEchinopsbiologyTraditional medicineMolecular StructurePlant ExtractsEchinops Plantmedicine.diseasebiology.organism_classificationAntineoplastic Agents PhytogenicXylopiaLeukemiaApoptosisCell cultureCancer cellImmunologyEthnopharmacologyPiperJournal of ethnopharmacology
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Cytotoxicity of compounds from Xylopia aethiopica towards multi-factorial drug-resistant cancer cells.

2015

Abstract Introduction Multidrug resistance (MDR) in cancer represent a major hurdle in chemotherapy. Previously, the methanol extract of the medicinal spice Xylopia aethiopica displayed considerable cytotoxicity against multidrug resistant (MDR) cancer cell lines. Methods The present study was designed to assess the cytotoxicity of compounds, 16 α -hydroxy- ent -kauran-19-oic acid ( 2 ), 3,4′,5-trihydroxy-6″,6″-dimethylpyrano[2,3-g]flavone ( 3 ), isotetrandrine ( 5 ) and trans -tiliroside ( 6 ) derived from the methanol crude extract of Xylopia aethiopica against 9 drug-sensitive and -resistant cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of these c…

Xylopia aethiopicaPharmaceutical ScienceAntineoplastic AgentsApoptosisPharmacologyAlkaloidsCell Line TumorDrug DiscoveryCytotoxic T cellHumansCytotoxicityPharmacologyFlavonoidsMembrane Potential MitochondrialbiologyMolecular StructurePlant ExtractsCell Cyclebiology.organism_classificationFlavonesAntineoplastic Agents PhytogenicXylopiaDrug Resistance MultipleMultiple drug resistanceComplementary and alternative medicineBiochemistryApoptosisCell cultureDoxorubicinDrug Resistance NeoplasmCaspasesCancer cellMolecular MedicineReactive Oxygen SpeciesXylopiaPhytomedicine : international journal of phytotherapy and phytopharmacology
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Evaluation of Fused Pyrrolothiazole Systems as Correctors of Mutant CFTR Protein.

2021

Cystic fibrosis (CF) is a genetic disease caused by mutations that impair the function of the CFTR chloride channel. The most frequent mutation, F508del, causes misfolding and premature degradation of CFTR protein. This defect can be overcome with pharmacological agents named “correctors”. So far, at least three different classes of correctors have been identified based on the additive/synergistic effects that are obtained when compounds of different classes are combined together. The development of class 2 correctors has lagged behind that of compounds belonging to the other classes. It was shown that the efficacy of the prototypical class 2 corrector, the bithiazole corr-4a, could be impr…

Yellow fluorescent proteinProtein FoldingCystic FibrosisMutantPharmaceutical ScienceCystic Fibrosis Transmembrane Conductance RegulatorCarboxamidemedicine.disease_cause01 natural sciencesAnalytical Chemistrychemistry.chemical_compoundMutant ProteinDrug DiscoveryMoietyCFTR potentiatorCFTRchemistry.chemical_classification0303 health sciencesMutationbiologyChemistryChemistry (miscellaneous)Chloride channelMolecular MedicineHumanStereochemistrymedicine.drug_classCFTR correctorArticleF508del-CFTRlcsh:QD241-44103 medical and health scienceslcsh:Organic chemistrymedicineHumansBenzodioxolesPhysical and Theoretical ChemistryThiazoleCystic Fibrosi030304 developmental biology010405 organic chemistryOrganic ChemistryAminoimidazole Carboxamide0104 chemical sciencesThiazolesMutationbiology.proteinMutant ProteinsBenzodioxoleTricyclicMolecules (Basel, Switzerland)
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Cytotoxicity of the crude extract and constituents of the bark of Fagara tessmannii towards multi-factorial drug resistant cancer cells.

2019

Abstract Ethnopharmacological relevance Fagara tessmannii Engl. is an African medicinal plant used in Cameroonian traditional medicine to treat various types of cancers. Aim of the study This work was designed to determine the cytotoxicity of the crude extract (FTB), fractions (FTBa-d) and compounds isolated from the bark of Fagara tessmannii, namely lupeol (1), fagaramide (2), zanthoxyline (3), hesperidin (4), nitidine chloride (5), fagaridine chloride (6), and β-sitosterol-3-O-β-D-glucopyranoside (7). The study was extended to the mode of induction of apoptosis by FTB, compounds 5 and 6. Materials and methods The resazurin reduction assay was used to evaluate the cytotoxicity of samples. …

ZanthoxylumApoptosisFlow cytometry03 medical and health scienceschemistry.chemical_compoundHesperidinInhibitory Concentration 500302 clinical medicineCell Line TumorNeoplasmsDrug DiscoverymedicineHumansCytotoxicity030304 developmental biologyLupeolPharmacologychemistry.chemical_classificationMembrane Potential Mitochondrial0303 health sciencesReactive oxygen speciesmedicine.diagnostic_testPlant ExtractsCell CycleCell cycleMolecular biologyAntineoplastic Agents PhytogenicchemistryApoptosisDoxorubicinDrug Resistance Neoplasm030220 oncology & carcinogenesisCancer cellPlant BarkReactive Oxygen SpeciesJournal of ethnopharmacology
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Antimicrobial Activity of Resveratrol Analogues

2014

Stilbenes, especially resveratrol and its derivatives, have become famous for their positive effects on a wide range of medical disorders, as indicated by a huge number of published studies. A less investigated area of research is their antimicrobial properties. A series of 13 trans-resveratrol analogues was synthesized via Wittig or Heck reactions, and their antimicrobial activity assessed on two different grapevine pathogens responsible for severe diseases in the vineyard. The entire series, together with resveratrol, was first evaluated on the zoospore mobility and sporulation level of Plasmopara viticola (the oomycete responsible for downy mildew). Stilbenes displayed a spectrum of acti…

Zoosporeresveratrol; stilbenes; grapevine; downy mildew; grey mold; <i>Plasmopara viticola</i>; <i>Botrytis cinerea</i>[SDV]Life Sciences [q-bio]resveratrol;stilbenes;grapevine;downy mildew;grey mold;Plasmopara viticola;Botrytis cinereaPharmaceutical ScienceFungusResveratrolArticleAnalytical ChemistryMicrobiologylcsh:QD241-441chemistry.chemical_compoundPlasmopara viticolaBotrytis cinerealcsh:Organic chemistryAnti-Infective AgentsDrug DiscoveryStilbenesmildiou de la vigne[SDV.BV]Life Sciences [q-bio]/Vegetal Biologygrey moldPhysical and Theoretical ChemistryBotrytis cinereaOomycetebiologydowny mildewOrganic Chemistrybiology.organism_classificationAntimicrobialgrapevinestilbenechemistryChemistry (miscellaneous)ResveratrolPlasmopara viticola[SDE]Environmental SciencesMolecular MedicineDowny mildewpourriture grise de la vigneBotrytisvigneMolecules
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Towards A Twitter Observatory: A Multi-Paradigm Framework For Collecting, Storing And Analysing Tweets

2016

International audience; In this article we show how a multi-paradigm framework can fulfil the requirements of tweets analysis and reduce the waiting time for researchers that use computational resources and storage systems to support large-scale data analysis. The originality of our approach is to combine concerns about data harvesting, data storage, data analysis and data visualisation into a framework that supports inductive reasoning in multidisciplinary scientific research. Our main contribution is a polyglot storage system with a generic data model to support logical data independence and a set of tools that can provide a suitable solution for mixing different types of algorithms in or…

[ INFO.INFO-IR ] Computer Science [cs]/Information Retrieval [cs.IR][ INFO ] Computer Science [cs]Computer scienceknowledge discovery02 engineering and technology[INFO] Computer Science [cs][INFO.INFO-SI]Computer Science [cs]/Social and Information Networks [cs.SI]Data modelingmassive datasetsopen source softwareData visualization[ INFO.INFO-IT ] Computer Science [cs]/Information Theory [cs.IT]polyglot storage020204 information systems0202 electrical engineering electronic engineering information engineering[INFO]Computer Science [cs]Twitter analysis . SystemsComputingMilieux_MISCELLANEOUS[INFO.INFO-DB]Computer Science [cs]/Databases [cs.DB]business.industryPolyglotInductive reasoningData science[SPI.TRON] Engineering Sciences [physics]/ElectronicsData independence[ SPI.TRON ] Engineering Sciences [physics]/Electronics[SPI.TRON]Engineering Sciences [physics]/ElectronicsData model[INFO.INFO-IT]Computer Science [cs]/Information Theory [cs.IT][INFO.INFO-IR]Computer Science [cs]/Information Retrieval [cs.IR]020201 artificial intelligence & image processing[INFO.INFO-IR] Computer Science [cs]/Information Retrieval [cs.IR][INFO.INFO-IT] Computer Science [cs]/Information Theory [cs.IT]Data architecturebusinessSoftware architecture
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Towards Iron(II) Complexes with Octahedral Geometry: Synthesis, Structure and Photophysical Properties

2020

The control of ligand-field splitting in iron (II) complexes is critical to slow down the metal-to-ligand charge transfer (MLCT)-excited states deactivation pathways. The gap between the metal-centered states is maximal when the coordination sphere of the complex approaches an ideal octahedral geometry. Two new iron(II) complexes (C1 and C2), prepared from pyridylNHC and pyridylquinoline type ligands, respectively, have a near-perfect octahedral coordination of the metal. The photophysics of the complexes have been further investigated by means of ultrafast spectroscopy and TD-DFT modeling. For C1, it is shown that&mdash

[CHIM.INOR] Chemical Sciences/Inorganic chemistryLigand field theoryCoordination sphereMaterials scienceIronPharmaceutical Scienceexcited states dynamics[CHIM.INOR]Chemical Sciences/Inorganic chemistryCrystallography X-RayLigands010402 general chemistry01 natural sciencesArticletime-resolved spectroscopyAnalytical Chemistrylcsh:QD241-441MetalX-Ray Diffractionlcsh:Organic chemistryDrug DiscoveryOctahedral molecular geometry[CHIM.CRIS]Chemical Sciences/Cristallographyiron (II) complexes[CHIM.COOR]Chemical Sciences/Coordination chemistryFerrous Compounds[CHIM.CRIS] Chemical Sciences/CristallographyPhysical and Theoretical Chemistryoctahedral geometrydensity functional theoryComputingMilieux_MISCELLANEOUSMolecular Structure010405 organic chemistryLigandOrganic Chemistry[CHIM.COOR] Chemical Sciences/Coordination chemistry0104 chemical sciences3. Good healthCrystallographyOctahedron[CHIM.OTHE] Chemical Sciences/OtherChemistry (miscellaneous)Excited statevisual_artvisual_art.visual_art_mediumThermodynamicsMolecular MedicineDensity functional theory[CHIM.OTHE]Chemical Sciences/Other
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Context-aware semantic Web service discovery protocol

2009

The Web of today represents a broad space where users research, discover and share information. In this context, the process of Web service discovery plays a significant role. Indeed, such process allows linking the information published by service providers and the requests of users, looking for information. Generally, such process involves text or keyword-based techniques. Still, this kind of discovery fails in retrieving only relevant information. Our approach is to design a more " intelligent " system that allows using a knowledge base during the service discovery process, as it is done in the Semantic Web vision. This thesis presents a framework for semantic Web service discovery using…

[INFO.INFO-WB] Computer Science [cs]/Webdécouverte de servicesservice discoveryRDFservices Web sémantiques[INFO.INFO-MC] Computer Science [cs]/Mobile ComputingAndroiddécouverte de services Web sémantiquessemantic Web serviceWeb sémantique[INFO.INFO-IR] Computer Science [cs]/Information Retrieval [cs.IR]semantic Web service discoverySemantic WebOWL
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