Evodiamine-plus-Evodiamine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEvodiamineCat.No.:HY-N0114CASNo.:518-17-2Synonyms:(+)-Evodiamine;d-Evodiamine分⼦式:C₁₉H₁₇N₃O分⼦量:303.36作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:10mg/mL(32.96mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2964mL16.4821mL32.9641mL5mM0.6593mL3.2964mL6.5928mL10mM0.3296mL1.6482mL3.2964mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1mg/mL(3.30mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Evodiamine从吴茱萸的果实中分离的⽣物碱,具有多种⽣物活性，⽐如抗炎，抗肥胖和抗肿瘤。体外研究Evodiamineshowscytotoxicityagainstavarietyofhumancancercell-linesbyinducingapoptosis.Moreover,itisanaturallymulti-targetingantitumormolecule,whichexertstheantitumoractivitybyvariousmolecularmechanismsuchascaspase-dependentand-independentpathways,sphingomyelinpathway,calcium/JNKsignaling,31PI3K/Akt/caspaseandFas-L/NF-κBsignalingpathways32[1].体内研究Evodiamineinhibitsthemetabolismofdapoxetine.Comparedtothecontrolgroup,thepharmacokineticparameteroft1/2,AUC(0-∞)andTmaxofdapoxetineinevodiaminegroupissignificantlyincreasedby63.3%,44.8%and50.4%,respectively.Moreover,evodiaminehassignificantlydecreasedthepharmacokineticparameteroft1/2andAUC(0-∞)ofdesmethyldapoxetine[2].EvodiaminesuppressestumorgrowthinasubcutaneousH22xenograftmodel.EvodiamineattenuatesVEGF-inducedangiogenesisinvivo[3].PROTOCOLCellAssay[1]EvodiamineisdissolvedinDMSOanddilutedwithappropriatemediumbeforeuse.Theevodiamine-inspirednewscaffoldsareassayedforgrowthinhibitoryactivitiestowardhumancancercell-linesA549(lungcancer),MDA-MB-435(breastcancer)andHCT116(coloncancer)usingtheMTTassay.Evodiamineandcamptithecinareusedasreferencedrugs[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:TwelvehealthymaleSprague-Dawleyratsarerandomlydividedinto2groups:thecontrolgroupAdministration[2][3](receivedoral10mg/kgdapoxetinealone)andthecombinationgroup(10mg/kgdapoxetineorallyco-administeredwith100mg/kgevodiamine).Theplasmaconcentrationofdapoxetineanddesmethyldapoxetineareestimatedbyultra-performanceliquidchromatography-tandemmassspectrometry(UPLC-MS/MS),anddifferentpharmacokineticparametersarecalculated[2].Mice:Anudemousexenograftmodelisestablishedbyusing4–6-week-oldmaleBALB/cnudemice.Micearedoseddailywith20mg/kg(10mL/kg)ofevodiamineintragastrically,sixmicearedosedintraperitoneallywith10mg/kgof5-flurouracil(5-FU)twiceaweek,andsixmicearenottreated.Thetumorvolumesaredeterminedbymeasuringtwodimensions,withtumorvolume=length×width×width/2.After2or3weeksoftreatment,micearesacrificedbycervicaldislocationunderanesthesiawithether,andthetumortissuesarecollected[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•PharmacolRes.2020May;155:104751.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Phytomedicine.10October2022,154493.•PhytotherRes.2021Mar3.•JEthnopharmacol.2022Aug2;115586.•OncolLett.2020Oct;20(4):121.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WangS,etal.ScaffoldDiversityInspiredbytheNaturalProductEvodiamine:DiscoveryofHighlyPotentandMultitargetingAntitumorAgents.JMedChem.2015Aug27;58(16):6678-96.[2].LiRF,etal.EffectsofEvodiamineonthePharmacokineticsofDapoxetineandItsMetaboliteDesmethylDapoxetineinRats.Pharmacology.2016;97(1-2):43-7.[3].ShiL,etal.Evodiamineexertsanti-tumoreffectsagainsthepatocellularcarcinomathroughinhibitingβ-catenin-mediatedangiogenesis.TumourBiol.2016Sep;37(9):12791