Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPapiliocinCat.No.:HY-P11093分子式: C???H???N??O??分子量: 4002.8Sequence: Arg-Trp-Lys-Ile-Phe-Lys-Lys-Ile-Glu-Lys-Val-Gly-Arg-Asn-Val-Arg-Asp-Gly-Ile-Ile-Lys-Ala-Gly-Pro-Ala-Val-Ala-Val-Val-Gly-Gln-Ala-Ala-Thr-Val-Val-Lys-NH2SequenceShortening:RWKIFKKIEKVGRNVRDGIIKAGPAVAVVGQAATVVK-NH2作用靶點(diǎn): Antibiotic;Bacterial;Fungal;Apoptosis;ReactiveOxygenSpecies(ROS);TNFReceptor;NOSynthase;InterleukinRelated;NF-κB;Toll-likeReceptor(TLR)作用通路: Anti-infection;Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB儲(chǔ)存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Papiliocin是一種兼具抗炎和抗菌活性的強(qiáng)效肽類抗生素。Papiliocin主要對(duì)革蘭氏陰性菌有活性。Papiliocin對(duì)細(xì)胞具有較高的抗炎活性，通過抑制NO的產(chǎn)生以及TNF-α和MIP-2的分泌來發(fā)揮其抗炎活性。Papiliocin通過抑制Toll樣受體(Toll-likeReceptor)通路和NF-κB參與先天防御反應(yīng)機(jī)制。Papiliocin誘導(dǎo)真菌(fungal)細(xì)胞凋亡(apoptosis),誘導(dǎo)細(xì)胞內(nèi)ROS總水平升高。Papiliocin在膿毒癥模型中充當(dāng)有效的防腐肽。Papiliocin可用于抗炎和抗菌研究。IC50&TargetIL-1βIL-6TLR4iNOS體外研究Papiliocin(37°Cfor16h)showsantibacterialactivityagainstGram-negativespecies(E.coli,S.typhimurium,andP.aeruginosa)andGram-positivespecies(B.subtilis,S.epidermidis,andS.aureus),withMICsof0.25,0.5,1,16,2,32μM[1].Papiliociniscalcium-andmagnesium-toleranttoGram-negativebacteria[1].Papiliocin(0-100μM,37°Cfor1h)lackshemolyticactivityandisnotcytotoxictoRAW264.7cells,withanIC50of58μm[1].Papiliocin(0-25μM,3-24h)inhibitstheexpressionofNO,TNF-α,MIP-2,iNOS,TLR4,NF-κB,andallinflammatorycytokinesIL-1β,IL-6,MIP-1,MIP-2,andTNF-αgenesinLPS(HY-D1056)-stimulatedRAW264.7cells[1].Papiliocin(0-10μM)induceslipidvesiclepermeabilization,showslowStern-Volmerquenchingconstants1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE(KSV)inmicellesorSUVs,resultsinthedissociationofLPSaggregatesthroughinteractionwithLPS[1].Papiliocin(30μM,28°Cfor2h)inducesROSproductionandincreasesintracellularhydroxylradicallevelsinCandidaalbicanscells[2].Papiliocin(30μM,28°Cfor2h)inducesapoptoticcelldeath,membranedepolarizationandmetacaspaseactivation,DNAdamageinCandidaalbicanscells[2].Papiliocin(0-50μM)displaces74.6%oftheBCprobesfromLPS,neutralizesLPS,withthebindingaffinityof0.063μM[3].Papiliocin(40μM,30min)inhibits52%ofFITC-LPSbindingtothesurfaceofRAW264.7cells,butalsocompetitivelydisplaces25%ofpre-boundLPSfromtheLPS-receptorcomplexonRAW264.7cells[3].Papiliocin(0-100μM)reducesTLR4-mediatedSEAPactivitywithanIC50of1.1μM[3].Papiliocin(0.1-10μM,1h)blockstheLPS-inducedinflammatorycascadebytargetingTLR4andtheMAPKpathwayandbyblockingthenucleartranslocationofp-NF-κBinRAW264.7cells[3].ELISAAssay[1]CellLine:LPS(20ng/mL)-stimulatedRAW264.7cellsConcentration:1,10μMIncubationTime:18?hResult:InhibitedtheproductionofTNF-αandMIP-2.RT-PCR[1]CellLine:LPS(20ng/mL)-stimulatedRAW264.7cellsConcentration:20μMIncubationTime:3?hResult:InhibitedtheexpressionofiNOSandallinflammatorycytokines,includingIL-1β,IL-6,MIP-1,MIP-2,andTNF-α.WesternBlotAnalysis[1]CellLine:LPS(20ng/mL)-stimulatedRAW264.7cellsConcentration:25μMIncubationTime:24?hResult:InhibitedTLR4andNF-κBexpressionandpreventedthetranslocationofNF-κBfromthecytoplasmtothenucleus.ApoptosisAnalysis[2]CellLine:Candidaalbicanscells2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:30μMIncubationTime:28°Cfor2hResult:Inducedapoptosiscelldeath,withtheearlyapoptoticcellsof61.14%,thelateapoptoticof0.52%.InducedthebreakdownofΔΨmandthelossofmitochondrialpermeability.Inducedthegenerationofstrongoxidanthydroxylradicals.IncreasedtheproportionofTUNEL-positivecellnuclei.WesternBlotAnalysis[3]CellLine:LPS(50ng/mL)-stimulatedRAW264.7cellsConcentration:0.1,0.5,1μMIncubationTime:1?hResult:ReducedMyD88overexpressionandphosphorylationlevelsofTAK1,p38,c-JunN-terminalkinase(JNK),andextracellularsignal-regulatedkinase(ERK).Immunofluorescence[3]CellLine:LPS(50ng/mL)-stimulatedRAW264.7cellsConcentration:10μMIncubationTime:1?hResult:ReducedexpressionofAlexa546inhibitedLp-NF-κBp65translocation.REFERENCESKimJK,etal.Structureandfunctionofpapiliocinwithantimicrobialandanti-inflammatoryactivitiesisolatedfromtheswallowtailbutterfly,Papilioxuthus.JBiolChem.2011Dec2;286(48):41296-41311.HwangB,etal.Inductionofyeastapoptosisbyanantimicrobialpeptide,Papiliocin.BiochemBiophysResCommun.2011Apr29;408(1):89-93.KrishnanM,etal.MolecularmechanismunderlyingtheTLR4antagonisticandantisepticactivitiesofpapiliocin,aninsectinnateimmuneresponsemolecule.ProcNatlAcadSci