The influence of saponins on cell membrane cholesterol

Böttger, Stefan; Melzig, Matthias F.

doi:10.1016/j.bmc.2013.09.008

Cited by 64 publications

(58 citation statements)

References 12 publications

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“…Böttger and Melzig postulated a membrane toxicity mechanism that is caused by the saponin-dependent loss of membrane cholesterol. Notably, no significant effect of the investigated membrane-active saponins on the cholesterol of endosomes and lysosomes was measurable [65]. These results corroborated the observations of Krawczyk et al who revealed the cell membrane-permeabilizing effect of digitonin, however, a saponin composite from Quillaja saponaria Molina in addition caused perturbation of intracellular membrane systems [66].…”

Section: Glycosylated Triterpenoidssupporting

confidence: 79%

“…Since many studies demonstrated that saponins have different abilities to cause membrane perturbation and permeabilization, these phenomena were analyzed by Böttger and Melzig using a cell culture model and radioactive 3 H-labeled cholesterol [65]. The authors revealed that cell membrane-active saponins (those with significant membrane toxicity) decreased the cholesterol content while no significant change in the cholesterol content was detectable after treatment with saponins that are not or only slightly cell membrane-active.…”

Section: Glycosylated Triterpenoidsmentioning

confidence: 99%

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Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies

et al. 2017

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Protein-based targeted toxins play an increasingly important role in targeted tumor therapies. In spite of their high intrinsic toxicity, their efficacy in animal models is low. A major reason for this is the limited entry of the toxin into the cytosol of the target cell, which is required to mediate the fatal effect. Target receptor bound and internalized toxins are mostly either recycled back to the cell surface or lysosomally degraded. This might explain why no antibody-targeted protein toxin has been approved for tumor therapeutic applications by the authorities to date although more than 500 targeted toxins have been developed within the last decades. To overcome the problem of insufficient endosomal escape, a number of strategies that make use of diverse chemicals, cell-penetrating or fusogenic peptides, and light-induced techniques were designed to weaken the membrane integrity of endosomes. This review focuses on glycosylated triterpenoids as endosomal escape enhancers and throws light on their structure, the mechanism of action, and on their efficacy in cell culture and animal models. Obstacles, challenges, opportunities, and future prospects are discussed.

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Section: Glycosylated Triterpenoidssupporting

confidence: 79%

Section: Glycosylated Triterpenoidsmentioning

confidence: 99%

Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies

et al. 2017

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“…Besides, the antiviral activity was discovered for other enveloped viruses in addition to HSV‐1, such as VSV and dengue, but neither β‐escin nor AH was able to inhibit a non‐enveloped virus replication, such as adenovirus (Figure ). Therefore, considering the well‐known ability of β‐escin to interfere with cell membranes, and that cholesterol homeostasis is critical for enveloped viruses replication, we speculate that the virucidal as well as the antiviral activity of β‐escin and AH could be at least partially attributed to their perturbation of membrane integrity. In fact, with respect to the antiviral activity, we observed that it was related to a late event during viral multiplication, distinct from HSV‐1 egress (Figure ).…”

Section: Discussionmentioning

confidence: 98%

Virucidal, antiviral and immunomodulatory activities of β-escin and Aesculus hippocastanum extract

Michelini

Alché

Bueno

2018

Journal of Pharmacy and Pharmacology

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“…Upon extensive saponin molecule incorporation into the membrane, these complexes aggregate inducing the formation of pores. The concomitant membrane permeabilization ultimately leads to cell death [5,[13][14][15]. In the last decade, the interaction between saponins and biological membranes was shown to strongly depend on the structure of the saponins [5,[13][14][15][16].…”

Section: Introductionmentioning

confidence: 99%

Enhancing the Membranolytic Activity of Chenopodium quinoa Saponins by Fast Microwave Hydrolysis

et al. 2020

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Saponins are plant secondary metabolites. There are associated with defensive roles due to their cytotoxicity and are active against microorganisms. Saponins are frequently targeted to develop efficient drugs. Plant biomass containing saponins deserves sustained interest to develop high-added value applications. A key issue when considering the use of saponins for human healthcare is their toxicity that must be modulated before envisaging any biomedical application. This can only go through understanding the saponin-membrane interactions. Quinoa is abundantly consumed worldwide, but the quinoa husk is discarded due to its astringent taste associated with its saponin content. Here, we focus on the saponins of the quinoa husk extract (QE). We qualitatively and quantitively characterized the QE saponins using mass spectrometry. They are bidesmosidic molecules, with two oligosaccharidic chains appended on the aglycone with two different linkages; a glycosidic bond and an ester function. The latter can be hydrolyzed to prepare monodesmosidic molecules. The microwave-assisted hydrolysis reaction was optimized to produce monodesmosidic saponins. The membranolytic activity of the saponins was assayed based on their hemolytic activity that was shown to be drastically increased upon hydrolysis. In silico investigations confirmed that the monodesmosidic saponins interact preferentially with a model phospholipid bilayer, explaining the measured increased hemolytic activity.

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The influence of saponins on cell membrane cholesterol

Cited by 64 publications

References 12 publications

Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies

Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies

Virucidal, antiviral and immunomodulatory activities of β-escin and Aesculus hippocastanum extract

Enhancing the Membranolytic Activity of Chenopodium quinoa Saponins by Fast Microwave Hydrolysis

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