Comparative Pharmacokinetics of Arctigenin in Normal and Type 2 Diabetic Rats After Oral and...

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Comparative Pharmacokinetics of Arctigenin in Normal and Type 2 Diabetic Rats After Oral and Intravenous Administration

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  • 9/4/2015 Comparativepharmacokineticsofarctigenininnormalandtype2diabeticratsafteroralandintravenousadministration.PubMedNCBI

    http://www.ncbi.nlm.nih.gov/pubmed/26102179 1/2

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

    Comparativepharmacokineticsofarctigenininnormalandtype2diabeticratsafteroralandintravenousadministration.ZengXY ,DongS ,HeNN ,JiangCJ ,DaiY ,XiaYF .

    DepartmentofChineseMateriaMedicaAnalysis,ChinaPharmaceuticalUniversity,24TongJiaXiang,Nanjing210009,China.DepartmentofPharmacologyofChineseMateriaMedica,ChinaPharmaceuticalUniversity,24TongJiaXiang,Nanjing210009,China.DepartmentofChineseMateriaMedicaAnalysis,ChinaPharmaceuticalUniversity,24TongJiaXiang,Nanjing210009,China.Electronicaddress:[email protected].

    AbstractArctigeninisthemainactiveingredientofFructusArctiiforthetreatmentoftype2diabetes.Inthisstudy,thepharmacokineticsofarctigenininnormalandtype2diabeticratsfollowingoralandintravenousadministrationwasinvestigated.Ascomparedtonormalrats,CmaxandAUC010hvaluesoforalarctigeninindiabeticratsincreasedby356.8%and223.4%,respectively.Incontrast,afterintravenousinjection,theCmaxandAUC010hvaluesofarctigeninshowednosignificantdifferencebetweendiabeticandnormalrats.Inordertoexplorehowthebioavailabilityoforalarctigeninincreasedunderdiabeticcondition,theabsorptionbehaviorofarctigeninwasevaluatedbyinsitusinglepassintestinalperfusion(SPIP).TheresultsindicatedthatarctigeninwasasubstrateofPglycoprotein(Pgp).TheabsorptiondifferenceofarctigenininthenormalanddiabeticratscouldbeeliminatedbythepretreatmentofclassicPgpinhibitorverapamil,suggestingthatPgpmightbethekeyfactorcausingtheabsorptionenhancementofarctigeninindiabeticrats.Furtherstudiesrevealedthattheuptakeofrhodamine123(Rho123)indiabeticratswassignificantlyhigher,indicatingthatdiabetesmellitusmightimpairPgpfunction.Consistently,alowermRNAlevelofPgpintheintestineofdiabeticratswasfound.Inconclusion,theabsorptionofarctigeninafteroraladministrationwaspromotedindiabeticrats,whichmightbepartiallyattributetothedecreasedexpressionandimpairedfunctionofPgpinintestines.

    Copyright2015ElsevierB.V.Allrightsreserved.

    AbsorptionArctigeninArctigenin(PubChemCID:64981)DiabetesmellitusInsitusinglepassintestinalperfusionIsobergapten(PubChemCID:68082)Ko143hydrate(PubChemCID:71311836)PglycoproteinPharmacokineticsProbenecid(PubChemCID:4911)Rhodamine123(PubChemCID:9929799)Streptozotocin(PubChemCID:29327)Verapamilhydrochloride(PubChemCID:62969)

    PMID:26102179[PubMedinprocess]

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  • 9/4/2015 Comparativepharmacokineticsofarctigenininnormalandtype2diabeticratsafteroralandintravenousadministration.PubMedNCBI

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