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Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers

Abstract : Saponins enhance the cytotoxicity of the type I ribosome-inactivating protein (RIP-I) saporin. In the present study, the synergistic cytotoxicity of nine newly isolated gypsogenin-containing saponins from Gypsophila trichotoma in combination with RIP-I was evaluated in vitro and used to derive a quantitative structure – activity relationship (QSAR). The QSAR model distinguished two important structural features of the studied saponins necessary for their cytotoxicity enhancing activity: the branched trisaccharide moiety attached to C-3 should contain one xylose residue instead of an arabinose and the branched tetrasaccharide at C-28 should contain one acetyl group attached to the glucose residue.
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Reneta Gevrenova, Alexander Weng, Laurence Voutguenne-Nazabadioko, Mayank Thakur, Irini Doytchinova. Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers. Letters in Drug Design & Discovery, 2014, 12 (3), pp.166-171. ⟨10.2174/1570180811666140915221432⟩. ⟨hal-01996585⟩



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