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Selective modulation of P-glycoprotein activity by steroidal saponines from Paris polyphylla

Bio-guided fractionation of the roots of Paris polyphylla (Trilliaceae), based on inhibition of P-glycoprotein-mediated daunorubicin efflux in K562/R7 cell line, led to isolation and identification of the three saponins 3- O-Rha(1 → 2)[Ara(1 → 4)]Glc-pennogenine, gracillin and polyphyllin D, and the...

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Bibliographic Details
Published in:Fitoterapia 2009, Vol.80 (1), p.39-42
Main Authors: Nguyen, Van Thi Bao, Darbour, Nicole, Bayet, Christine, Doreau, Agnès, Raad, Imad, Phung, Binh Hoa, Dumontet, Charles, Di Pietro, Attilio, Dijoux-Franca, Marie-Geneviève, Guilet, David
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Language:English
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Summary:Bio-guided fractionation of the roots of Paris polyphylla (Trilliaceae), based on inhibition of P-glycoprotein-mediated daunorubicin efflux in K562/R7 cell line, led to isolation and identification of the three saponins 3- O-Rha(1 → 2)[Ara(1 → 4)]Glc-pennogenine, gracillin and polyphyllin D, and the two ecdysteroids 20-hydroxyecdysone and pinnatasterone. These compounds were tested for multidrug reversion on P-glycoprotein (ABCB1) with both drug-selected and transfected cell lines, and also on Breast Cancer Resistance Protein (BCRP/ABCG2). By contrast to a weak efficiency on BCRP, the three saponins displayed significant effects as inhibitors of P-glycoprotein-mediated drug efflux.
ISSN:0367-326X
1873-6971
DOI:10.1016/j.fitote.2008.09.010