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

ISSN

1873-6971

Autores

Van 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

Resumo

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.

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