Search results for " 50"

showing 10 items of 2715 documents

Synthesis and antioxidant evaluation of novel silybin analogues

2006

In this work, we evaluated the antioxidant properties of the eight novel silybin analogues for their capacity to scavenge free radicals including superoxide anion radicals and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals in vitro. Compound 7d demonstrated an excellent antioxidant effect in scavenging superoxide anion free radical with an IC50 value of 26.5 microM, while the IC50 of quercetin (the reference compound) was 38.1 microM. Compounds 7b, 7e, 7h showed certain scavenging activities for both types of free radicals.

AnionsAntioxidantDPPHRadicalmedicine.medical_treatmentDrug Evaluation PreclinicalMedicinal chemistryAntioxidantsInhibitory Concentration 50chemistry.chemical_compoundPicratesSuperoxidesDrug DiscoverymedicineOrganic chemistryIC50PharmacologyDose-Response Relationship DrugSuperoxideBiphenyl CompoundsAnion radicalsFree Radical ScavengersGeneral MedicineIn vitroHydrazinesModels ChemicalchemistrySpectrophotometrySilybinQuercetinQuercetinSilymarinJournal of Enzyme Inhibition and Medicinal Chemistry
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Pyrano[2,3-e]isoindol-2-ones, new angelicin heteroanalogues

2009

A convenient synthesis of the pyrano[2,3-e]isoindol-2-one ring system, an heteroanalogue of angelicin, is reported. Our synthetic approach consists of the annelation of the pyran ring on the isoindole moiety using 5-dialkylamino- or 5-hydroxymethylene intermediates as building blocks. The photoantiproliferative activity of the new derivatives was studied. Some of them bearing the benzyl group at the 8 position were active with IC(50) in the micromolar range. Cell cytotoxicity involves apoptosis, alteration of cell cycle profile and membrane photodamage.

AnnulationPyrano-isoindolesStereochemistryChemistry PharmaceuticalClinical BiochemistryPharmaceutical ScienceApoptosisIsoindolesRing (chemistry)BiochemistryChemical synthesisInhibitory Concentration 50Jurkat CellsStructure-Activity Relationshipchemistry.chemical_compoundAngelicinCell Line TumorFurocoumarinsDrug DiscoveryHumansMoietyMolecular BiologyPyransMolecular StructurePyrano-isoindoleChemistryPhotochemotherapeutic activityOrganic ChemistryPyrano-isoindoles; Angelicin heteroanalogues; Photochemotherapeutic activity; ApoptosisSettore CHIM/08 - Chimica FarmaceuticaAngelicin heteroanaloguesOxygenModels ChemicalPyranDrug DesignBenzyl groupMolecular MedicineK562 CellsIsoindoleAngelicin heteroanalogueBioorganic & Medicinal Chemistry Letters
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Towards a multilevel ant colony optimization

2014

Masteroppgave i Informasjons- og kommunikasjonsteknologi IKT590 Universitetet i Agder 2014 Ant colony optimization is a metaheuristic approach for solving combinatorial optimization problems which belongs to swarm intelligence techniques. Ant colony optimization algorithms are one of the most successful strands of swarm intelligence which has already shown very good performance in many combinatorial problems and for some real applications. This thesis introduces a new multilevel approach for ant colony optimization to solve the NP-hard problems shortest path and traveling salesman. We have reviewed different elements of multilevel algorithm which helped us in construction of our proposed mu…

Ant colony optimizationIKT590MathematicsofComputing_NUMERICALANALYSISVDP::Technology: 500::Information and communication technology: 550ComputingMethodologies_ARTIFICIALINTELLIGENCE
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Modulation of COX, LOX and NFκB activities by Xanthium spinosum L. root extract and ziniolide.

2012

Xanthium spinosum L. (Asteraceae) is a medicinal weed distributed worldwide. Many of its diverse ethnopharmacological uses - namely diarrhoea, inflammation, liver disorders, snake bite and fever - are linked - at least in part - to an uncontrolled release of arachidonic acid metabolites. The crude extract of X. spinosum roots from Jordanian origin dose-dependently inhibited the 5-LOX (IC50 is approximately equal to 10 μg/mL), COX-1(IC50 is approximately equal to 50 μg/mL), and 12-LOX (IC50 is approximately equal to 170 μg/mL) enzymatic pathways in intact pro-inflammatory cells. A direct activity at the level of PLA2 is not probable, but the extract induced the synthesis of the anti-inflamma…

Anti-Inflammatory AgentsPharmacologySesquiterpene lactoneXanthiumPlant Rootslaw.inventionchemistry.chemical_compoundInhibitory Concentration 50Sesquiterpenes GuaianelawDrug DiscoveryHydroxyeicosatetraenoic AcidsHumansCyclooxygenase InhibitorsLipoxygenase InhibitorsPharmacologychemistry.chemical_classificationInflammationbiologyDose-Response Relationship DrugPlant ExtractsNF-kappa BGeneral MedicineLipoxygenasesbiology.organism_classificationXanthiumPhorbolsEnzymeEicosanoidchemistryBiochemistryXanthium spinosumArachidonate 5-lipoxygenasebiology.proteinCyclooxygenase 1Arachidonic acidPhytotherapyHeLa CellsPhytotherapyFitoterapia
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Synthesis and biological evaluation of (+)-labdadienedial, derivatives and precursors from (+)-sclareolide

2010

Labdadienedial and a series of C15,C16-functionalized derivatives were synthesized from commercial (+)-sclareolide and evaluated for their cytotoxic, antimycotic, and antiviral activities. Their precursors were similarly evaluated.

Antifungal AgentsStereochemistryAntineoplastic AgentsHerpesvirus 1 HumanAntiviral AgentsChemical synthesisInhibitory Concentration 50chemistry.chemical_compoundChlorocebus aethiopsDrug Discoveryotorhinolaryngologic diseasesAnimalsHumansCytotoxicityVero CellsPharmacologyOrganic ChemistryFungifood and beveragesSclareolideBiological activityGeneral MedicineCombinatorial chemistryTerpenoidIn vitrostomatognathic diseaseschemistrylipids (amino acids peptides and proteins)DiterpenesDiterpeneEnantiomerHeLa CellsEuropean Journal of Medicinal Chemistry
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Tiliroside and gnaphaliin inhibit human low density lipoprotein oxidation.

2004

Two flavonoids, gnaphaliin and tiliroside, isolated from Helichrysum italicum, were studied in vitro for their capacity to inhibit Cu(2+)-induced human low density lipoprotein (LDL) and diluted plasma oxidation. LDL oxidation was monitored by conjugated diene, thiobarbituric acid-reactive substances (TBARS) formation and electrophoretic mobility on agarose gel. Gnaphaliin and tiliroside increased the lag-phase for diene conjugate production in a dose-dependent manner. The reduction of TBARS production confirmed the antioxidant activity of gnaphaliin and tiliroside with 50% inhibitory concentration (IC(50)) values of 8.0+/-3.9 microM and 7.0+/-2.6 microM respectively. Furthermore, the flavon…

AntioxidantCopper Sulfatemedicine.medical_treatmentProbucolPharmacognosyThiobarbituric Acid Reactive SubstancesLipid peroxidationchemistry.chemical_compoundInhibitory Concentration 50Drug DiscoverymedicineTBARSHumansBenzopyransIC50PharmacologyFlavonoidsHelichrysumChromatographyPlant ExtractsGeneral MedicineCholesterol LDLPlant Components AerialFlavonesLipoproteins LDLBiochemistrychemistryLow-density lipoproteinAgaroseLipid Peroxidationmedicine.drugPhytotherapyFitoterapia
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Forecasting Aquaponic Systems Behaviour With Recurrent Neural Networks Models

2022

Aquaponic systems provide a reliable solution to grow vegetables while cultivating fish (or other aquatic organisms) in a controlled environment. The main advantage of these systems compared with traditional soil-based agriculture and aquaculture installations is the ability to produce fish and vegetables with low water consumption. Aquaponics requires a robust control system capable of optimizing fish and plant growth while ensuring a safe operation. To support the control system, this work explores the design process of Deep Learning models based on Recurrent Neural Networks to forecast one hour of pH values in small-scale industrial Aquaponics. This implementation guides us through the m…

AquaponicsRecurrent Neural NetworkGated Recurrent UnitData-driven ModellingGeneral MedicineVDP::Teknologi: 500::Informasjons- og kommunikasjonsteknologi: 550VDP::Landbruks- og Fiskerifag: 900::Fiskerifag: 920Long Short-term MemoryProceedings of the Northern Lights Deep Learning Workshop
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Oxygenated Cembrene Diterpenes from Sarcophyton convolutum: Cytotoxic Sarcoconvolutum A–E

2021

The soft coral genus Sarcophyton contains the enzymatic machinery to synthesize a multitude of cembrene-type diterpenes. Herein, highly oxygenated cembrenoids, sarcoconvolutum A–E (1–5) were purified and characterized from an ethyl acetate extract of the red sea soft coral, Sarcophyton convolutum. Compounds were assemblies according to spectroscopic methods including FTIR, 1D- and 2D-NMR as well as HRMS. Metabolite cytotoxicity was tested against lung adenocarcinoma, cervical cancer, and oral-cavity carcinoma (A549, HeLa and HSC-2, respectively). The most cytotoxic compound, (4) was observed to be active against cell lines A549 and HSC-2 with IC50 values of 49.70 and 53.17 μM, respectively.

Aquatic Organismssarcoconvolutum A–EMagnetic Resonance Spectroscopy<i>Sarcophyton convolutum</i>StereochemistryQH301-705.5MetaboliteEthyl acetatePharmaceutical ScienceAntineoplastic AgentsArticleHeLaInhibitory Concentration 50Structure-Activity Relationshipchemistry.chemical_compoundCell Line TumorDrug DiscoveryIc50 valuesAnimalsCytotoxic T cellBiology (General)CytotoxicityIndian OceanPharmacology Toxicology and Pharmaceutics (miscellaneous)cembrenoidschemistry.chemical_classificationbiologyChemistrySarcophyton<i>Sarcophyton convolutum</i>; sarcoconvolutum A–E; cembrenoids; cytotoxicitySarcophyton convolutumAnthozoabiology.organism_classificationEnzymecytotoxicityDiterpenesDrug Screening Assays AntitumorMarine Drugs
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Arginine-rich peptides are blockers of VR-1 channels with analgesic activity

2000

Vanilloid receptors (VRs) play a fundamental role in the transduction of peripheral tissue injury and/or inflammation responses. Molecules that antagonize VR channel activity may act as selective and potent analgesics. We report that synthetic arginine-rich hexapeptides block heterologously expressed VR-1 channels with submicromolar efficacy in a weak voltage-dependent manner, consistent with a binding site located near/at the entryway of the aqueous pore. Dynorphins, natural arginine-rich peptides, also blocked VR-1 activity with micromolar affinity. Notably, synthetic and natural arginine-rich peptides attenuated the ocular irritation produced by topical capsaicin application onto the eye…

ArginineReceptors DrugBiophysicsTRPV Cation ChannelsPainDynorphinPharmacologyArginineEyeDynorphinsBiochemistryInhibitory Concentration 50MiceXenopus laevisDynorphinchemistry.chemical_compoundStructural BiologyNon-competitive antagonistGeneticsAnimalsChannel blockerAmino Acid SequenceBinding siteReceptorMolecular BiologyNon-competitive antagonistAnalgesicsChemistryElectric ConductivityNociceptorCell BiologyCapsaicinIonic poreOocytesNociceptorCapsaicinPeptidesFEBS Letters
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Commento agli artt. 506 e 507 c.p.p., in Codice di procedura penale, a cura di G. Tranchina, Milano, 2008

2008

Commento dottrinario e giurisprudenziale degli artt. 506 e 507 c.p.p.

Art. 506 c.p.p. Art. 507 c.p.p.Settore IUS/16 - Diritto Processuale Penale
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