Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers
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.
Keywords: Cancer, cytotoxicity, saponins, saporin, targeted anticancer therapy, QSAR, PLS.
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