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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers

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

Volume 12, Issue 3, 2015

Page: [166 - 171] Pages: 6

DOI: 10.2174/1570180811666140915221432

Price: $65


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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