Membrane Disintegration Caused by the Steroid Saponin Digitonin Is Related to 
the Presence of Cholesterol

Sudji, Ikhwan Resmala; Subburaj, Yamunadevi; Frenkel, Nataliya; García-Sáez, Ana J.; Wink, Michael

doi:10.3390/molecules201119682

Item

ITEM ACTIONSEXPORT

Add to Basket

Local TagsRelease HistoryDetailsSummary

Released

Journal Article

Membrane Disintegration Caused by the Steroid Saponin Digitonin Is Related to the Presence of Cholesterol

MPS-Authors

There are no MPG-Authors in the publication available

External Resource

No external resources are shared

Fulltext (restricted access)

There are currently no full texts shared for your IP range.

Fulltext (public)

molecules-20-19682.pdf
(Any fulltext), 40MB

Supplementary Material (public)

There is no public supplementary material available

Citation

Sudji, I. R., Subburaj, Y., Frenkel, N., García-Sáez, A. J., & Wink, M. (2015). Membrane Disintegration Caused by the Steroid Saponin Digitonin Is Related to the Presence of Cholesterol. Molecules, 20(11), 20146-20160. doi:10.3390/molecules201119682.

Cite as: https://hdl.handle.net/21.11116/0000-000F-3E9C-D

Abstract

In the present investigation we studied the molecular mechanisms of the monodesmosidic saponin digitonin on natural and artificial membranes. We measured the hemolytic activity of digitonin on red blood cells (RBCs). Also different lipid membrane models (large unilamellar vesicles, LUVs, and giant unilamellar vesicles, GUVs) in the presence and absence of cholesterol were employed. The stability and permeability of the different vesicle systems were studied by using calcein release assay, GUVs membrane permeability assay using confocal microscopy (CM) and fluorescence correlation spectroscopy (FCS) and vesicle size measurement by dynamic light scattering (DLS). The results support the essential role of cholesterol in explaining how digitonin can disintegrate biological and artificial membranes. Digitonin induces membrane permeability or causes membrane rupturing only in the presence of cholesterol in an all-or-none mechanism. This effect depends on the concentrations of both digitonin and cholesterol. At low concentrations, digitonin induces membrane permeability while keeping the membrane intact. When digitonin is combined with other drugs, a synergistic potentiation can be observed because it facilitates their uptake.