Allethrin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAllethrinCat.No.:HY-B1559CASNo.:584-79-2分⼦式:C₁₉H₂₆O₃分⼦量:302.41作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Allethrin⼀种拟除⾍菊酯杀⾍剂，⼀种主的驱蚊剂。Allethrin在⼤⿏丸癌细胞(LC540)中诱导氧化应激、细胞凋亡(apoptosis)和钙释放。Allethrin还诱导BCL-2、caspase-3激活和细胞内钙的释放[1]。体外研究Allethrin(0.001-250μM)inducescytotoxicityandoxidativestress.AllethriniscytotoxictoisolatedLeydigcellsandtesticularcancercells.Cytotoxicityisduetofreeradicalgenerationandalteredantioxidantstatus[1].MorphologicalanalysesofLC540cellstreatedwithAllethrin(125μM)revealsthepresenceofapoptoticbodies[1].Allethrin(125μM)inducesBCL-2,caspase-3activationandreleaseofintracellularcalcium[1].Allethrin(IC50≈85μM)istoxictohumancornealepithelial(HCE)cellscausingdeaththroughmitochondrialpathway[2].CellCytotoxicityAssay[1]CellLine:LC540cells(derivedfromratLeydigcelltumor)Concentration:0.001-250μMIncubationTime:24hoursResult:Atlowconcentrationsdidnotdisplayappreciablecellkillingactivityupto50μMwhenincubatedfor24h.Atconcentrationsabove100μM,cellkillingwasobserved.Basedontheresultsobtained,theIC50was125μM.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEApoptosisAnalysis[1]CellLine:LC540cellsConcentration:125μMIncubationTime:24hoursResult:Revealedthepresenceofapoptoticbodies.Thepercentageofcellsdisplayingearlyapoptoticfeaturesincreasedsignificantly.WesternBlotAnalysis[1]CellLine:LC540cellsConcentration:125μMIncubationTime:0,3,6,9,12,24hoursResult:BCL-2,pro-Caspase-3andPARP-1proteinexpressiondecreasedsignificantlywithanincreaseincleavedPARP-1levels.体内研究AdultmaleratsaretreatedorallywithAllethrin(25,50,100,and150mg/kg;everydayfor60days).Lipidperoxidationisincreasedinthecaput,cauda,andtestes.Nitricoxideproductionisincreasedinthecaput,butunalteredinthecaudaandtestes.Theactivitiesofcatalase,glutathioneperoxidase(GPx),glutathione-S-transferase(GST),andsuperoxidedismutase(SOD)aredecreasedinthecaputandcauda[3].AnimalModel:MaleWistarratsaged90days[3]Dosage:25,50,100,and150mg/kgAdministration:Orallyadministeredeverydayfor60daysResult:IncreasedlevelsofLPOproductswereobservedinthecaput,cauda,andtestesofallethrintreatedrats.Inthecaput,increasedlevelsofNOwasobservedatallthedosestested,whencomparedwiththevehicletreatedcontrol.Significantincreaseincatalaseactivitywasobservedinthecaudaobtainedfrom50,100,and150mg/kg.GPxactivitywassignificantlyincreasedinthecaputobtainedfrom150mg/kgtreatedrats.Inthecauda,itwasfoundtobeincreasedsignificantlyinthe50and100mg/kgtreatedgroups.Incontrast,theactivityofGPxactivitywassignificantlydecreasedinthetestesofratstreatedwith150mg/kg.GSTactivitywasfoundtobeincreasedsignificantlyinadosedependentmannerinthecaputandcaudaofallethrintreatedrats.Inthecaput,significantincreaseintheactivityofSODwasobservedinthe150mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEbodytreatedrats.Inthecaudaandtestes,treatmentresultedinincreaseofSODactivityatallthedosestested.REFERENCES[1].GollaMadhubabu,etal.Allethrininducesoxidativestress,apoptosisandcalciumreleaseinrattesticularcarcinomacells(LC540).ToxicolInVitro.2014Dec;28(8):1386-95.[2].GeetikaGupta,etal.Allethrintoxicityonhumancornealepithelialcellsinvolvesmitochondrialpathwaymediatedapoptosis.ToxicolInVitro.2013Dec;27(8):2242-8.[3].GollaMadhubabu,etal.Allethrininducedtoxicityinthemalereproductivetractofratscontributestodisruptioninthetranscriptionofgenesinvolvedingermcellproduction.EnvironToxicol.2014Nov;29(11):1330-45.McePdfHei