Syracuse

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

Archive ouverte

Nguyen, van Thi Bao | Darbour, Nicole | Bayet, Christine | Doreau, A. | Raad, Imad | Phung, B.H. | Dumontet, C. | Di Pietro, A. | Dijoux-Franca, Marie-Genevieve | Guilet, David

Edité par CCSD ; Elsevier -

International audience. 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(12)[Ara(14)]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.

• Description
• Sujet/Public
• Outil
• Outil d'anticipation
• Mémoire et thèse
• Gestion