Saponins can perturb biologic membranes and reduce the surface tension of aqueous solutions: A correlation?

Böttger, Stefan; Hofmann, Katja; Melzig, Matthias F.

doi:10.1016/j.bmc.2012.03.032

Cited by 98 publications

(87 citation statements)

References 29 publications

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“…A general feature of saponins is their amphiphilic character and their ability to integrate into the membranes [21]. In addition to this property we hypothesize the possibility of certain saponins (SA1641, SA1657 and SO1861) to associate with saporin in a pHdependent manner, which finally leads to the delivery of saporin into the cytosol.…”

Section: Binding Studiesmentioning

confidence: 89%

Saponins modulate the intracellular trafficking of protein toxins

Weng

Thakur

Mallinckrodt

et al. 2012

Journal of Controlled Release

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Section: Binding Studiesmentioning

confidence: 89%

Saponins modulate the intracellular trafficking of protein toxins

Weng

Thakur

Mallinckrodt

et al. 2012

Journal of Controlled Release

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“…Together, they create the mechanical barrier that limits the contact between irritants or micro-organisms and the upper respiratory tract mucosa, therefore reducing both the stimulation of nerve endings and the inflammation. Saponins are known for their ability to lower the surface tension [30]; thanks to this property, they reduce the viscosity of the mucus allowing an easier elimination. The polysaccharides attract water and moisturize the mucosa making the mucus less viscous and easier to be expelled [29].…”

Section: Discussionmentioning

confidence: 99%

Efficacy of Grintuss® pediatric syrup in treating cough in children: a randomized, multicenter, double blind, placebo-controlled clinical trial

Canciani

Murgia²,

Caimmi

et al. 2014

Ital J Pediatr

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BackgroundCough is an extremely common problem in pediatrics, mostly triggered and perpetuated by inflammatory processes or mechanical irritation leading to viscous mucous production and increased sensitivity of the cough receptors. Protecting the mucosa might be very useful in limiting the contact with micro-organisms and irritants thus decreasing the inflammation and mucus production. Natural molecular complexes can act as a mechanical barrier limiting cough stimuli with a non pharmacological approach but with an indirect anti-inflammatory action.ObjectiveAim of the study was to assess the efficacy of a medical device containing natural functional components in the treatment of cough persisting more than 7 days.MethodsIn this randomized, parallel groups, double-blind vs. placebo study, children with cough persisting more than 7 days were enrolled. The clinical efficacy of the study product was assessed evaluating changes in day- and night-time cough scores after 4 and 8 days (t4 and t8) of product administration.ResultsIn the inter-group analysis, in the study product group compared with the placebo group, a significant difference (t4 study treatment vs. t4 placebo, p = 0.03) was observed at t4 in night-time cough score.Considering the intra-group analysis, only the study product group registered a significant improvement from t0 to t4 in both day-time (t0 vs. t4, p = 0.04) and night-time (t0 vs. t4, p = 0.003) cough scores.A significant difference, considering the study product, was also found in the following intra-group analyses: day-time scores at t4 vs. t8 (p =0.01) and at t0 vs. t8 (p = 0.001); night-time scores at t4 vs. t8 (p = 0.05), and at t0 vs. t8 (p = 0.005). Considering a subgroup of patients with higher cough (≥3) scores, 92.9% of them in the study product group improved at t0 vs. t4 day-time.ConclusionsGrintuss® pediatric syrup showed to possess an interesting profile of efficacy and safety in the treatment of cough persisting more than 7 days.

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“…Nevertheless, all triterpenoid saponins can be described as amphiphilic due to the nonpolar triterpene backbone and the polar sugar chains. The ability of saponins to interact with both hydrophilic and lipophilic compounds enables them to interfere with or even disrupt cell membranes, phases and other amphiphilic structures [26]. These characteristics explain mostly all effects that are linked to saponins to date.…”

Section: Glycosylated Triterpenoidsmentioning

confidence: 99%

“…Most saponins show hemolytic [28] and membrane permeabilizing [26] properties at specific concentrations, used by plants to defend themselves from predators. Below these toxic concentrations, triterpenoid saponins are widely used in several fields of phytotherapy.…”

Section: Glycosylated Triterpenoidsmentioning

confidence: 99%

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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Saponins can perturb biologic membranes and reduce the surface tension of aqueous solutions: A correlation?

Cited by 98 publications

References 29 publications

Saponins modulate the intracellular trafficking of protein toxins

Saponins modulate the intracellular trafficking of protein toxins

Efficacy of Grintuss® pediatric syrup in treating cough in children: a randomized, multicenter, double blind, placebo-controlled clinical trial

Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies

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