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LKT/GUGGULSTERONE/G8225/5 mg

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Description

Guggulsteroneisaplantsteroidobtainedfrommyrrhthatexhibitsawidevarietyofbeneficialproperties,includinganti-metastatic,anticancer,anti-angiogenic,anti-fibrotic,antioxidative,anti-inflammatory,andanti-hyperlipidemicactivities.Invitro,guggulsteroneincreasesactivationofcaspase3,decreasesexpressionofmatrixmetalloproteinase9(MMP9),cyclinD1,Bcl-2,xlAP,andmucinMUC4,inhibitsFAK,Src,andJAK/STATsignaling,anddisruptscytoskeletalorganization;together,thisresultsinapoptosisandinhibitionofgrowthandcolonyformationofpancreaticcancercells.Incoloncancercells,thiscompoundinhibitsexpressionofVEGF,ARNT,andSTAT3anddecreasesactivityofmatrixmetalloproteinases2and9(MMP2/9),inducingapoptosis.GuggulsteronealsoincreasesapoptosisinhepaticstellatecellsthroughinhibitionofNF-κBactivation,suggestingpotentialbenefitasatreatmentforchronicliverdisease.Guggulsteronealsoexhibitscardioprotectivebenefits,inhibitingdoxorubicin-inducedtoxicityincardiomyocytes;guggulsteronedecreasesactivityofROS,malondialdehyde,andcaspase3,andalsoreversesdoxorubicin-inducedchangesinpoly(ADP)-ribosepolymerase(PARP)cleavage,caspaseexpression,Bcl-2/Baxratio,andcytochromecrelease.Additionally,guggulsteroneincreaseshemeoxygenase1(HO-1)expressionandNrf2activity,potentiallythroughmodulationofphosphateandtensinhomolog(PTEN),invitro.Inothercellularmodels,guggulsteroneinhibitslipopolysaccharide-inducedincreasesinCOX-2andTNF-αaswellasdecreasesinIκBkinase-α.Incellularandanimalmodels,guggulsteroneinhibitspreADIpocytedifferentiationandincreaseslipolysisofmatureadipocytes.GuggulsteronealsoinhibitsthefarnesoidXreceptor(FXR).

ProductInfo

CasNo.

95975-55-6

Purity

≥98%

Formula

C21H28O2

FormulaWt.

312.45

ChemicalName

(17E)-Pregna-4,17(20)-diene-3,16-dione

IUPACName

(8R,9S,10R,13S,14S,17E)-17-ethylidene-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15-decahydrocyclopenta[a]phenanthrene-3,16-dione

Synonym

Pregna-4,17-diene-3,16-dione

MeltingPoint

194-195°C

Appearance

Offwhitetoyellowpowder

ShippingandStorage

StoreTemp

Ambient

ShipTemp

Ambient

Downloads

InfoSheet

G8225InfoSheetPDF

References

MachaMA,RachaganiS,GuptaS,etal.GuggulsteronedecreasesproliferationandmetastaticbehaviorofpancreaticcancercellsbymodulatingJAK/STATandSrc/FAKsignaling.CancerLett.2013Dec1;341(2):166-77.PMID:23920124.

KimBH,YoonJH,YangJI,etal.GuggulsteroneattenuatesactivationandsurvivalofhepaticstellatecellbyinhibitingnuclearfactorkappaBactivationandinducingapoptosis.JGastroenterolHepatol.2013Dec;28(12):1859-68.PMID:23808824.

WangWC,UenYH,ChangML,etal.Protectiveeffectofguggulsteroneagainstcardiomyocyteinjuryinducedbydoxorubicininvitro..BMCComplementAlternMed.2012Aug27;12:138.PMID:22920231.

SongJJ,KwonSK,ChoCG,etalGuggulsteronesuppressesLPSinducedinflammationofhumanmiddleearepithelialcells(HMEEC).IntJPediatrOtorhinolaryngol.2010Dec;74(12):1384-7.PMID:20971513.

KimES,HongSY,LeeHK,etal.GuggulsteroneinhibitsangiogenesisbyblockingSTAT3andVEGFexpressionincoloncancercells.OncolRep.2008Dec;20(6):1321-7.PMID:19020709.

AhnKS,SethiG,SungB,etal.Guggulsterone,afarnesoidXreceptorantagoNIST,inhibitsconstitutiveandinducIBLeSTAT3activationthroughinductionofaproteintyrosinephosphataseSHP-1.CancerRes.2008Jun1;68(11):4406-15.PMID:18519703.

YangJY,Della-FeraMA,BaileCA.Guggulsteroneinhibitsadipocytedifferentiationandinducesapoptosisin3T3-L1cells.Obesity(SilverSpring).2008Jan;16(1):16-22.PMID:18223606.

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