Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers

Title:Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers

Volume: 12 Issue: 3

Author(s): Reneta Gevrenova, Alexander Weng, Laurence Voutguenne-Nazabadioko, Mayank Thakur and Irini Doytchinova

Affiliation:

Keywords: Cancer, cytotoxicity, saponins, saporin, targeted anticancer therapy, QSAR, PLS.

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.

Cite this article as:

Gevrenova Reneta, Weng Alexander, Voutguenne-Nazabadioko Laurence, Thakur Mayank and Doytchinova Irini, Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers, Letters in Drug Design & Discovery 2015; 12 (3) . https://dx.doi.org/10.2174/1570180811666140915221432