Real-time analysis of membrane permeabilizing effects of oleanane saponins

Bioorg Med Chem. 2013 Apr 15;21(8):2387-2395. doi: 10.1016/j.bmc.2013.01.061. Epub 2013 Feb 8.

Abstract

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 6 μM and hemolysis from 3 μM. Further, the results suggest that charge of the saponin may be relevant for permeabilizing effects of oleanane saponins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Cell Membrane Permeability / drug effects
  • Electrophoresis
  • Humans
  • Oleanolic Acid / analogs & derivatives*
  • Oleanolic Acid / pharmacology
  • Saponins / pharmacology*

Substances

  • Saponins
  • oleanane
  • Oleanolic Acid