Erucin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEErucinCat.No.:HY-121323CASNo.:4430-36-8分?式:C?H??NS?分?量:161.29作?靶點(diǎn):Apoptosis作?通路:Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Erucin(ERU)?種異硫氰酸鹽(isothiocyanate)，在芝?菜(arugula)中尤其豐富。Erucin具有抗癌、神經(jīng)保護(hù)和抗炎活性[1][2][3][4]。體外研究Erucin(ERU)(0-100μM)releasesH2SandinhibitscellviabilityinAsPC‐1cellsinaconcentration-dependentmanner[1].ErucininhibitscellmigrationandalteredtheAsPC‐1cellcycle,reducingG0/G1phaseandincreasingG2/MandSphases[1].Erucin(30μM,72h)inducesAsPC‐1cellapoptosisandinhibitscellmigration[1].ErucinreduceslevelsofphosphorylatedERK1/2inAsPC‐1cells[1].Erucin(0-200μM,24h)showsantiproliferativeactivitywithanIC50of97.7μMinA549cells[2].Erucin(0-50μM,24h)inducesthecleavageofPARP-1at50μM,andincreasesp53andp21proteinexpressioninA549cells[2].ErucindecreasesLPS-inducedproductionofNO,prostaglandinE2(PGE2),TNF-α,IL-6andIL-1βinRAW264.7cells[3].ErucindecreasesLPS-inducedexpressionofinduciblenitricoxidesynthase(iNOS)andcyclooxygenase(COX)-2inRAW264.7cells[3].ErucininhibitsLPS-inducedactivationofNFκBSignalinginRAW264.7cells[3].CellViabilityAssay[1]CellLine:AsPC‐1Concentration:10,30,and100μM1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:72hResult:Showedasignificantandconcentration‐dependentreductionofcellviability.CellCycleAnalysis[1]CellLine:AsPC‐1Concentration:30μMIncubationTime:72hResult:ShowedaparticularincreaseofcellsnumberintheG2/Mphase(36.6%±3.5vs.vehicle‐treatedcellsintheG2/Mphase:24.0%±1.3)andintheS‐phase(18.1%±1.5vs.vehicle‐treated

cellsintheSphase:11.0%±0.7)andaconsequentsignificantreductionofcellsintheG0/G1

phase(35.1%±5.0vs.vehicle‐treatedcellsintheG0/G1phase:59.5%±1.8.ApoptosisAnalysis[1]CellLine:AsPC‐1Concentration:30μMIncubationTime:72hResult:Significantlyincreasedthenumberoftotalapoptoticcells(apoptoticdeadcellsandapoptoticlivecells;vehicle:17.7%±2.5vs.Erucin:28.7%±4.2).CellProliferationAssay[2]CellLine:A549Concentration:0-200μMIncubationTime:24hResult:ShowedantiproliferativeeffectwithanIC50of97.7μM.WesternBlotAnalysis[2]CellLine:A549Concentration:0-50μMIncubationTime:24hResult:InducedthecleavageofPARP-1at50μM.Increasedp53andp21proteinexpression.WesternBlotAnalysis[3]2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:RAW264.7Concentration:0,2.5,and5μMIncubationTime:30minResult:DecreasedtheexpressionofiNOSandCOX-2inducedbyLPS.SuppressedtheLPS-inducedreductioninIκB-α.SuppressedNFκBDNAbindingandtranscriptionalactivity.RT-PCR[3]CellLine:RAW264.7Concentration:0,2.5,and5μMIncubationTime:24hResult:DecreasedLPS-inducedTNF-α,IL-6andIL-1βproduction.體內(nèi)研究Erucin(ERU)(0-300nM)significantlyinhibitsTPA-inducededemaformation[3].Erucin(30μmol/kg;i.p.;twiceaweekfor4week)showsneuroprotectiveeffects[4].AnimalModel:FemaleICRmice(4weeksofage),TPA(12-O-tetradecanoylphorbol-13-acetate)-inducedmouseearedemamodel[3]Dosage:0,100,and300nMAdministration:Topicallyappliedtothemouseear30minpriortothetopicalapplicationofTPAResult:SignificantlyinhibitedTPA-inducededemaformation.AnimalModel:MaleC57Bl/6mice(9weeksold,25–30gbodyweight)[4]Dosage:30μmol/kgAdministration:Intraperitonealadministration,twiceaweek,4weeks(Inducebrainlesionbyintrastriatalinjectionof6-OHDA)Result:Inducedapartialrecoveryintherotationalbehaviortest.UpregulatedtheexpressionofTH.CounteractneuronaldeathandDNAfragmentationin6-OHDAlesionedmice.increasetotalGSHandNrf2levelsin6-OHDAlesionedmice.REFERENCES[1].ValentinaCiti,etal.Anticancerpropertiesoferucin,anH2S-releasingisothiocyanate,onhumanpancreaticadenocarcinomacells(AsPC-1).PhytotherRes.2019Mar;33(3):845-855.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].A.Melchini,etal.Erucin,anewpromisingcancerchemopreventiveagentfromrocketsalads,showsanti-proliferativeactivityonhumanlungcarcinomaA549cells.FoodChemToxicol.2009Jul;47(7):1430-6.[3].HanJinCho,etal.Erucinexertsanti-inflammatorypropertiesinmurinemacrophagesandmouseskin:possiblemediationthroughtheinhibitionofNFκBsignaling.IntJMolSci.2013Oct15;14(10):20564-77.[4].FabianaMorroni,etal.ComparisonofAdaptiveNeuroprotectiveMechanismsofSulforaphaneanditsInterconversionProductErucinininVitroandinVivoModelsofParkinson'sDisease.JAgricFoo