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Inhibition of DNA-topoisomerase I by acylated triterpene saponins from pittosporum angustifolium Lodd

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Item Type:Article
Title:Inhibition of DNA-topoisomerase I by acylated triterpene saponins from pittosporum angustifolium Lodd
Creators Name:Baecker, C. and Drwal, M.N. and Preissner, R. and Lindequist, U.
Abstract:Previous phytochemical investigation of the leaves and seeds of Pittosporum angustifolium Lodd. led to the isolation and structural elucidation of polyphenols and triterpene saponins. Evaluation for cytotoxicity of isolated saponins revealed that the predominant structural feature for a cytotoxic activity are acyl substituents at the oleanane aglycon backbone. The present work reports the results of a screening of 10 selected acylated saponins for their potential to inhibit the human DNA-topoisomerase I, giving rise to IC50 values in a range of 2.8-46.5 microM. To clarify the mode of observed cytotoxic action and, moreover, to distinguish from a pure surfactant effect which is commonly accompanied with saponins, these results indicate an involvement of the topoisomerase I and its role as a possible target structure for a cytotoxic activity. In addition, computational predictions of the fitting of saponins to the topoisomerase I-DNA complex, indicate a similar binding mode to that of clinically used topoisomerase I inhibitors. Ten acylated triterpene saponins from Pittosporum angustifolium were investigated for their potential to inhibit the human DNA-topoisomerase I and computational predictions of the fitting of saponins to the topoisomerase I-DNA complex were carried out.
Keywords:Pittosporum angustifolium, Acylated Triterpene Saponins, Cytotoxicity, Topoisomerase I, Docking
Source:Natural Products and Bioprospecting
ISSN:2192-2209
Publisher:Springer
Volume:6
Number:2
Page Range:141-147
Date:April 2016
Official Publication:https://doi.org/10.1007/s13659-016-0087-5
PubMed:View item in PubMed

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