Fitoterapia · 2008
Selective modulation of P-glycoprotein activity by steroidal saponines from Paris polyphylla.
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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
Аннотация
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.
Предметные рубрики MeSH
ATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2ATP-Binding Cassette TransportersCyclosporineDaunorubicinDiosgeninDrug Resistance, MultipleDrug Resistance, NeoplasmEcdysteroidsEcdysteroneHumansImmunosuppressive AgentsK562 CellsLeukemiaMagnoliopsidaMembrane Transport ModulatorsATP-Binding Cassette, Sub-Family C ProteinsNeoplasm ProteinsPlant ExtractsRhizomeSaponinsSpirostansSteroids