Real-time analysis of membrane permeabilizing effects of oleanane saponins

Saponins are a group of plant and marine derived glycosides with numerous biological functions. Two important characteristics of certain plant saponins are their ability to enhance cytotoxicity of type I ribosome inactivating proteins and stimulation of the immune system. The main objective of the p...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2013-04, Vol.21 (8), p.2387-2395
Main Authors: Gilabert-Oriol, Roger, Mergel, Katharina, Thakur, Mayank, von Mallinckrodt, Benedicta, Melzig, Matthias F, Fuchs, Hendrik, Weng, Alexander
Format: Article
Language:English
Subjects:
Cell Line, Tumor
Cell Membrane - drug effects
Cell Membrane - metabolism
Cell Membrane Permeability - drug effects
Cell membranes
chemistry
cytotoxicity
digitonin
Electrophoresis
glycyrrhizin
Gypsophila
hemolysis
Humans
immune system
monitoring
Oleanolic Acid - analogs & derivatives
Oleanolic Acid - pharmacology
proteins
Quillaja saponaria
ribosomes
saponins
Saponins - pharmacology
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Summary:Saponins are a group of plant and marine derived glycosides with numerous biological functions. Two important characteristics of certain plant saponins are their ability to enhance cytotoxicity of type I ribosome inactivating proteins and stimulation of the immune system. The main objective of the present study was to investigate in real-time the permeabilizing effects of saponins on cell membrane. A set of oleanane saponins (glycyrrhizinic acid, Gypsophila, Saponaria and Quillaja saponins) and a steroid saponin (digitonin) were tested. The effects of these saponins on lysosomal membranes and hemolysis, along with their charge were also studied. Real-time monitoring of cell membrane permeabilization facilitated a highly sensitive analysis of the cellular kinetics. Saponins showed variable permeabilizing effects on cellular and lysosomal membranes at concentrations from 6μM and hemolysis from 3μM. Further, the results suggest that charge of the saponin may be relevant for permeabilizing effects of oleanane saponins.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2013.01.061