9/4/2015

Comparativepharmacokineticsofarctigenininnormalandtype2diabeticratsafteroralandintravenousadministration.PubMedNCBI

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Abstract

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Fitoterapia.2015Sep105:11926.doi:10.1016/j.fitote.2015.06.014.Epub2015Jun20.

Comparativepharmacokineticsofarctigenininnormalandtype2
diabeticratsafteroralandintravenousadministration.
ZengXY1,DongS1,HeNN1,JiangCJ1,DaiY2,XiaYF3.

Authorinformation
1

DepartmentofChineseMateriaMedicaAnalysis,ChinaPharmaceuticalUniversity,24TongJia
Xiang,Nanjing210009,China.
2
DepartmentofPharmacologyofChineseMateriaMedica,ChinaPharmaceuticalUniversity,24
TongJiaXiang,Nanjing210009,China.
3
DepartmentofChineseMateriaMedicaAnalysis,ChinaPharmaceuticalUniversity,24TongJia
Xiang,Nanjing210009,China.Electronicaddress:yfxiacpu@126.com.

Abstract
ArctigeninisthemainactiveingredientofFructusArctiiforthetreatmentoftype2diabetes.Inthis
study,thepharmacokineticsofarctigenininnormalandtype2diabeticratsfollowingoraland
intravenousadministrationwasinvestigated.Ascomparedtonormalrats,CmaxandAUC010h
valuesoforalarctigeninindiabeticratsincreasedby356.8%and223.4%,respectively.In
contrast,afterintravenousinjection,theCmaxandAUC010hvaluesofarctigeninshowedno
significantdifferencebetweendiabeticandnormalrats.Inordertoexplorehowthebioavailability
oforalarctigeninincreasedunderdiabeticcondition,theabsorptionbehaviorofarctigeninwas
evaluatedbyinsitusinglepassintestinalperfusion(SPIP).Theresultsindicatedthatarctigenin
wasasubstrateofPglycoprotein(Pgp).Theabsorptiondifferenceofarctigenininthenormal
anddiabeticratscouldbeeliminatedbythepretreatmentofclassicPgpinhibitorverapamil,
suggestingthatPgpmightbethekeyfactorcausingtheabsorptionenhancementofarctigenin
indiabeticrats.Furtherstudiesrevealedthattheuptakeofrhodamine123(Rho123)indiabetic
ratswassignificantlyhigher,indicatingthatdiabetesmellitusmightimpairPgpfunction.
Consistently,alowermRNAlevelofPgpintheintestineofdiabeticratswasfound.Inconclusion,
theabsorptionofarctigeninafteroraladministrationwaspromotedindiabeticrats,whichmight
bepartiallyattributetothedecreasedexpressionandimpairedfunctionofPgpinintestines.
Copyright2015ElsevierB.V.Allrightsreserved.
KEYWORDS: AbsorptionArctigeninArctigenin(PubChemCID:64981)DiabetesmellitusInsitusingle
passintestinalperfusionIsobergapten(PubChemCID:68082)Ko143hydrate(PubChemCID:
71311836)PglycoproteinPharmacokineticsProbenecid(PubChemCID:4911)Rhodamine123
(PubChemCID:9929799)Streptozotocin(PubChemCID:29327)Verapamilhydrochloride(PubChem
CID:62969)
PMID:26102179[PubMedinprocess]

http://www.ncbi.nlm.nih.gov/pubmed/26102179

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Comparativepharmacokineticsofarctigenininnormalandtype2diabeticratsafteroralandintravenousadministration.PubMedNCBI

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