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- W2127623656 abstract "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 Due to reported cases of liver toxicity, kava-kava extracts were withdrawn from the market in several countries in 2002.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." @default.
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- W2127623656 date "2005-07-28" @default.
- W2127623656 modified "2023-10-15" @default.
- W2127623656 title "EXTRACTS AND KAVALACTONES OF <i>PIPER METHYSTICUM</i> G. FORST (KAVA-KAVA) INHIBIT P-GLYCOPROTEIN IN VITRO" @default.
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- W2127623656 doi "https://doi.org/10.1124/dmd.105.005892" @default.
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