Quantitative Structure – Activity Relationship Study on Saponins as Cytotoxicity Enhancers

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

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 3 , 2015

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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.

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

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Article Details

VOLUME: 12
ISSUE: 3
Year: 2015
Page: [166 - 171]
Pages: 6
DOI: 10.2174/1570180811666140915221432
Price: $58

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