Spilanthol-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESpilantholCat.No.:HY-126383CASNo.:25394-57-4分子式:C??H??NO分子量:221.34儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 Spilanthol是一種具有口服活性的鎮(zhèn)痛、神經(jīng)保護、抗氧化、抗誘變、抗癌、抗炎、抗菌和殺蟲化合物。Spilanthol可誘導cAMP來抑制尿濃縮負調(diào)節(jié)機制。Spilanthol能夠用于利尿劑研究[1][4][5]。IC50&TargetCyclicAdenosinemonophosphate(cAMP)[5]體外研究Spilanthol(50~150μM,24h)hasnoeffectoncellviabilityinA549humanlungepithelialcell[3].Spilanthol(50~150μM,24h)hasanti-inflammatoryeffectsinA549humanlungepithelialcellline[3].Spilanthol(50~150μM,24h)canreducICAM-1geneexpressioninA549humanlungepithelialcellline[3].CellViabilityAssay[3]CellLine:A549humanlungepithelialcelllineConcentration:50μM,75μM,100μM,150μMIncubationTime:24hResult:Therewasnosignificantchangeincellviability.CellCytotoxicityAssay[3]CellLine:A549humanlungepithelialcelllineConcentration:50μM,75μM,100μM,150μMIncubationTime:24h1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:SignificantlyinhibitedthereleaseoftheinflammatorycytokineTNF-αandthechemokineMCP-1.WesternBlotAnalysis[3]CellLine:A549humanlungepithelialcelllineConcentration:50μM,75μM,100μM,150μMIncubationTime:24hResult:InhibitedCOX-2expressionandincreasedtheexpressionofHO-1.CellViabilityAssay[3]CellLine:A549humanlungepithelialcelllineConcentration:50μM,75μM,100μM,150μMIncubationTime:24hResult:SignificantlyreducedTHP-1cellsadhered.體內(nèi)研究Spilanthol(1-1.875mg/kg,Ip,Once)showsantinociceptiveactivityinaceticacid-inducedabdominalwrithesMaleICRmicemodelandcapsaicin-inducedlickingpawMaleICRmicemodel[2].Spilanthol(30mg/kg,Po,Onceadayforfourdays)aprotectiveeffectagainsttheintestinaldamageassociatedinswissmicemodelofintestinalmucositisinducedby5-fluorouracil(HY-90006)[4].Spilanthol(800mg/kg,Po,Once)hasadiureticeffectinadultC57BL/6Jmalemice[5].AnimalModel:Aceticacid-inducedabdominalwrithesMaleICRmicemodel[2]Dosage:1-1.875mg/kgAdministration:Intraperitonealadministration(i.p.),OnceResult:Asthedoseincreased,thenumberofabdominalcontractionsandlickingbehaviordecreased,andamaximumantinociceptiveeffectof46.67%AnimalModel:Swissmicemodelofintestinalmucositisinducedby5-fluorouracil[4].Dosage:30mg/kgAdministration:Oraladminstraion(p.o.),OnceadayforfourdaysResult:Showedtheintestinalwallrecovery,villiarehigherandlessirregularityandhighnumberandgreaterlengthofintestinalcrypts.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEAnimalModel:AdultC57BL/6Jmalemice[5].Dosage:800mg/KgAdministration:Oraladminstraion(p.o.),OnceResult:Increasedinurineoutput,sodium,andincreasedexcretionofsodium,potassiumandchloride.REFERENCESAlanF,etal.Spilanthol:occurrence,extraction,chemistryandbiologicalactivities.Elsevier.2016:128-133Déciga-CamposM,etal.AntinociceptiveeffectofHeliopsislongipesextractandaffinininmice.PlantaMed.2010May;76(7):665-70.HuangWC,etal.SpilantholInhibitsCOX-2andICAM-1ExpressionviaSuppressionofNF-κBandMAPKSignalinginInterleukin-1β-StimulatedHumanLungEpithelialCells.Inflammation.2018Oct;41(5):1934-1944.deFreitas-BlancoVS,etal.Spilanthol,thePrincipalAlkylamidefromAcmellaoleracea,Attenuates5-Fluorouracil-InducedIntestinalMucositisinMice.PlantaMed.2019Feb;85(3):203-209.[5]GerbinoA,etal..SpilantholfromAcmellaOleraceaLowerstheIntracellularLevelsofcAMPImpairingNKCC2PhosphorylationandWaterChannelAQP2MembraneExpressioninMouseKidney.PLoSOne.2016May23;11(5):e0156021.McePdfHeightCaution: