EXTRACTS AND KAVALACTONES OF PIPER METHYSTICUM G. FORST (KAVA-KAVA) INHIBIT P-GLYCOPROTEIN IN VITRO
| Autor: | Alexandra Sauer, A. Frank, Matthias Unger, Johanna Weiss |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Pharmaceutical Science
Pharmacology Transfection Dihydromethysticin Plant Roots Lactones Mice chemistry.chemical_compound Cell Line Tumor Animals ATP Binding Cassette Transporter Subfamily B Member 1 Yangonin Kavain Kava Desmethoxyyangonin Dose-Response Relationship Drug Leukemia P388 Plant Extracts Piper methysticum Dihydrokavain Fluoresceins Anti-Anxiety Agents chemistry Pyrones Methysticin |
| Zdroj: | Drug Metabolism and Disposition. 33:1580-1583 |
| ISSN: | 1521-009X 0090-9556 |
| DOI: | 10.1124/dmd.105.005892 |
| Popis: | Root extracts from kava-kava (Piper methysticum G. Forst) are clinically used for the treatment of anxiety and restlessness. Due to reported cases of liver toxicity, kava-kava extracts were withdrawn from the market in several countries in 2002. Because the efflux transporter P-glycoprotein (P-gp) is involved in the absorption, distribution, and excretion of many drugs and often participates in drug-drug interactions, we studied the effect of a crude kava extract and the main kavalactones kavain, dihydrokavain, methysticin, dihydromethysticin, yangonin, and desmethoxyyangonin on the P-gp-mediated efflux of calcein-acetoxymethylester in the P-gp-overexpressing cell line P388/dx and the corresponding cell line P388. The crude extract and the kavalactones showed a moderate to potent inhibitory activity with f2) (concentration needed to double baseline fluorescence) values of 170 microg/ml and 17 to 90 microM, respectively. The f2 value of yangonin could not be determined due to its higher lipophilicity. In conclusion, our results for the first time demonstrate P-gp-inhibitory activity of kava-kava and its components in vitro. |
| Databáze: | OpenAIRE |
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