Description
TroglitazoneisathiazolidinedionePPARγagoNISTthatexhibitsanti-diabetic,anticancer,anti-fibrotic,andanti-inflammatoryactivities.TroglitazonecontainsavitaminE-likeringstructurethatformshepatotoxicmetabolitesinvivo.TroglitazoneinducesapoptosisincervicalcancercellsanddecreasesexpressionandactivityoftelomeraseinER-breastcancercells.Invitro,troglitazoneactivatesAMPK,decreasesmembranepotential,inhibitshighglucose-closedATP-sensitiveK+channels,anddecreasesinsulinhypersecretion.Inalveolarepithelialcells,troglitazoneinhibitsTGF-β1-inducedactivationofAkt,GSK-3βandSmad2/3,decreasesβ-cateninsignaling,andsuppressesepithelial-to-mesenchymaltransition(EMT).Additionally,thiscompoundinhibitsPAM-inducedincreasesinTGF-β1andincreasesMUC1expressioninairwayepithelialcells.
References
ChenHM,ZhangDG,WuJX,etal.Ubiquitinationofp53isinvolvedintroglitazoneinducedapoptosisincervicalcancercells.AsianPacJCancerPrev.2014;15(5):2313-8.PMID:24716976.
DengR,NieA,JianF,etal.Acuteexposureofbeta-cellstotroglitazonedecreasesinsulinhypersecretionviaactivatingAMPK.BiochimBiophysActa.2014Jan;1840(1):577-85.PMID:24144566.
ZhouB,BuckleyST,PatelV,etal.TroglitazoneattenuatesTGF-β1-inducedEMTinalveolarepithelialcellsviaaPPARγ-independentmechanism.PLoSOne.2012;7(6):e38827.PMID:22745681.
ParkYS,LillehojEP,KatoK,etal.PPARγinhibitsairwayepithelialcellinflammatoryresponsethroughaMUC1-dependentmechanism.AmJPhysiolLungCellMolPhysiol.2012Apr1;302(7):L679-87.PMID:22268120.
Rashid-KolvearF,TaboskiMA,NguyenJ,etal.TroglitazonesuppressestelomeraseactivityindependentlyofPPARgammainestrogen-receptornegativebreastcancercells.BMCCancer.2010Jul22;10:390.PMID:20650001.
OzakiS,MinamisonoT,YamashitaT,etal.Supersaturation-nucleationbehaviorofpoorlysolubledrugsanditsimpactontheoralabsorptionofdrugsinThermodynamicallyhigh-energyforms.JPharmSci.2012Jan;101(1):214-222.PMID:21918988.
