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Modulation of P-glycoprotein activity by acridones and coumarins from Citrus sinensis
1Université Claude Bernard Lyon 1, Laboratoire de Pharmacognosie, Faculté de Pharmacie, 8 avenue Rockefeller, 69373 Lyon Cedex 8, France.
Abstract:
Bioguided fractionation of the roots of Citrus sinensis (Rutaceae) led to the isolation and identification of five coumarins, namely, clausarin, suberosin, poncitrin, xanthyletin and thamnosmonin, seven acridones, namely, acrimarine B, 2-methoxycitpressine I, citpressine I, buntanine, acrimarine E, honyumine and acrimarine C, and one terpenoid, namely, limonin. Among these compounds, clausarin, 2-methoxycitpressine I and acrimarine E inhibited P-glycoprotein-mediated drug efflux in K562/R7 human leukemic cells over-expressing P-glycoprotein.
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