Selective modulation of P-glycoprotein activity by steroidal saponines from Paris polyphylla
2008; Elsevier BV; Volume: 80; Issue: 1 Linguagem: Inglês
10.1016/j.fitote.2008.09.010
ISSN1873-6971
AutoresVan Thi Bao Nguyen, Nicole Darbour, Christine Bayet, Agnès Doreau, Imad Raad, Binh Hoa Phung, Charles Dumontet, Attilio Di Pietro, Marie‐Geneviève Dijoux‐Franca, David Guilet,
Tópico(s)Phytochemistry and Biological Activities
ResumoBio-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.
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