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Planta Med 2002; 68(12): 1055-1058
DOI: 10.1055/s-2002-36360
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© Georg Thieme Verlag Stuttgart · New York

Inhibition of Cytochrome P450 3A4 by Extracts and Kavalactones of Piper methysticum (Kava-Kava)

Matthias Unger1 , Ulrike Holzgrabe1 , Wolfgang Jacobsen2 , Carolyn Cummins3 , Leslie Z. Benet3
  • 1Institute of Pharmacy and Food Chemistry, Julius-Maximilians-University, Würzburg, Germany
  • 2Department of Anesthesiology, University of Colorado, Denver, USA
  • 3Department of Biopharmaceutical Sciences, University of California, San Francisco, USA
Further Information

Publication History

Received: July 28, 2002

Accepted: September 22, 2002

Publication Date:
20 December 2002 (online)

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Abstract

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.

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Dr. Matthias Unger

Institute of Pharmacy and Food Chemistry

Department of Pharmaceutical Chemistry

Am Hubland

97074 Würzburg

Germany

Phone: +49 931 888 5451

Fax: +49 931 888 5494

Email: m.unger@pharmazie.uni-wuerzburg.de

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