Antimicrobial-agent-34-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAntimicrobialagent-34Cat.No.:HY-161988分⼦式:C₃₂H₅₂N₂O₃分⼦量:512.77作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Antimicrobialagent-34(compound4h)⼀种抗剂(MIC=1–4μg/mL)，clogP值为9.14。Antimicrobialagent-34⾎浆稳定性好(HC50为131.1μg/mL)，具有良好的膜选择性(HC50/MIC为65.6)，具备快速杀能⼒。Antimicrobialagent-34通过破坏细细胞膜完整性，诱导细胞内活性氧增加及蛋⽩质和DNA泄漏，最终导致细死亡。Antimicrobialagent-34在⾦⾊葡萄球ATCC43300感染的⼩⿏败⾎症模型中，展现了显著的体内抗效⼒[1]。体外研究Antimicrobialagent-34canbestablypresentinhumanserum,plasmaandblood,withMBCsof16,16and32μg/mL,respectively,withoutlosingitsantimicrobialeffect[1].Antimicrobialagent-34hasthestrongestantibacterialactivityagainst6Gram-positivebacteria,withawideantibacterialspectrumandaMICrangeof1-4μg/mL.ItalsohasgoodantibacterialactivityagainstKlebsiellapneumoniaeATCC10031,UnstableBacteriaATCC19606,andEscherichiacoliATCC25922,withMICsof4,2,and4μg/mL,respectively[1].Antimicrobialagent-34(1×-16×MIC)showsrapidantibacterialactivityagainstStaphylococcusaureus,anditisdose-dependent[1].Antimicrobialagent-34(2-16mg/mL;0-24h)isdifficulttoinduceresistance.TheresistancetestofStaphylococcusaureusATCC43300undersub-MIC(1/2MIC)showsaMICchangeofonly2-4times[1].Antimicrobialagent-34(2-64mg/mL,0-20days)hasastrongabilitytoinhibitbiofilmformationanddestroypre-formedbiofilm,anditisdose-dependent[1].Antimicrobialagent-34(2-32mg/mL,0-20min)disruptesthetransmembranepotentialofS.aureus,therebyincreasingpermeabilityandeffectivelyincreasingthelevelsofROS,DNA,andproteininS.aureus[1].CellViabilityAssay[1]CellLine:StaphylococcusaureusATCC433001/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:2,4,8,16mg/mLIncubationTime:0,2,4,6,8,10,12,20,24hResult:Achieveda8.35logreduction(killing≥99.9%ofS.aureus)in4hcomparedwiththecontrol,andthekillingratewas100%after8h,whilereferencedrugvancomycinexhibiteda8.55logreductionofS.aureuswithin8hatthesameconcentration.CellViabilityAssay[1]CellLine:StaphylococcusaureusATCC43300Concentration:2,4,8,16,32,64mg/mLIncubationTime:20daysResult:InhibitedtheformationofbiofilmofStaphylococcusaureus,andtheformationofbiofilmwassignificantlyreducedwiththeincreaseofconcentration.8μg/mLeliminated26.69%oftheestablishedbiofilmofStaphylococcusaureus,andtheeradicationrateofbiofilmat64μg/mLexceeded40%.体内研究Antimicrobialagent-34(5and10mg/kg,i.p.,continuouslyat12-hintervalsfor2days)hasastronginhibitoryeffectonGram-positivebacteriainvivo,significantlyreducingthebacterialloadintheblood,liver,kidney,spleenandotherorgansofmiceinthesepsismodelofmiceinfectedwithStaphylococcusaureusATCC43300.TNF-αandIL-6inthebloodofmicearereducedaftertreatment[1].AnimalModel:MousesepsismodelinfectedbyS.aureusATCC43300[1].Dosage:5and10mg/kg;continuouslyat12-hintervalsfor2daysAdministration:Intraperitonealinjection(i.p.)Result:Achieved1.10,1.98,2.00and2.09log(91.8%,98.9%,99.0%and99.2%)reductionsinthenumberofsurvivingbacterialcoloniesinblood,liver,spleenandkidneyby5mg/mL.Achieved,respectively,1.46,2.69,2.24and2.84log(95.9%,99.8%,99.4%and99.9%)by10mg/mL.DecreasedinthelevelofproinflammatorycytokinesincludingTNF-αandIL-6.REFERENCES[1].FangquanLiu,etal.Design,synthesisandbiologicalevaluationofamphiphilicbenzopyranderivativesaspotentantibacterialagentsagainstmultidrug-resistantbacteria.EurJMedChem.2024Nov5:277:116784.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECa