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Inhibition of Cytochrome P450 3A4 by Extracts and Kavalactones of<i>Piper methysticum</i>(Kava-Kava)
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2002
Year
Molecular PharmacologyMedicinal ChemistryCytochrome P450 3A4Positive FractionsBiochemistryBioassay-guided FractionationMedicineNatural SciencesBioassay-guided IsolationHerb-drug InteractionSecondary MetabolitePhytopharmacologyPhytochemicalPhytochemistryPharmacologyPharmaceutical ChemistryDrug Discovery
Inhibitors of cytochrome P450 3A4 (CYP3A4) were identified in crude extracts from the rhizomes of Piper methysticum G. Forst. (Kava-Kava) using bioassay-guided fractionation. After preliminary purification of an ethyl acetate extract with solid phase extraction, the eluate was further fractionated by means of HPLC and fractions were tested for inhibitory potency using cDNA expressed CYP3A4. Positive fractions were analysed with LC/MS using electrospray ionisation and kavapyrones could be identified as the main CYP3A4 inhibitory components of Piper methysticum.