1. Org Biomol Chem. 2014 Oct 21;12(44):8803-22. doi: 10.1039/c4ob01652a.

The amphiphilic nature of saponins and their effects on artificial and biological
membranes and potential consequences for red blood and cancer cells.

Lorent JH(1), Quetin-Leclercq J, Mingeot-Leclercq MP.

Author information: 
(1)Université catholique de Louvain, Louvain Drug Research Institute, Cellular and
Molecular Pharmacology (FACM), Avenue Mounier 73, B1.73.05, B-1200 Brussels,
Belgium. marie-paule.mingeot@uclouvain.be jolorent@gmail.com.

Saponins, amphiphiles of natural origin with numerous biological activities, are 
widely used in the cosmetic and pharmaceutical industry. Some saponins exhibit
relatively selective cytotoxic effects on cancer cells but the tendency of
saponins to induce hemolysis limits their anticancer potential. This review
focused on the effects of saponin activity on membranes and consequent
implications for red blood and cancer cells. This activity seems to be strongly
related to the amphiphilic character of saponins that gives them the ability to
self-aggregate and interact with membrane components such as cholesterol and
phospholipids. Membrane interactions of saponins with artificial membrane models,
red blood and cancer cells are reviewed with respect to their molecular
structures. The review considered the mechanisms of these membrane interactions
and their consequences including the modulation of membrane dynamics, interaction
with membrane rafts, and membrane lysis. We summarized current knowledge
concerning the mechanisms involved in the interactions of saponins with membrane 
lipids and examined the structure activity relationship of saponins regarding
hemolysis and cancer cell death. A critical analysis of these findings speculates
on their potential to further develop new anticancer compounds.

PMID: 25295776  [PubMed - in process]