Anti-inflammatory and Anti-cancer Properties of β-Escin, a Triterpene Saponin

Abstract

Horse chestnut seed extract is well known for its antiedematous and anti-inflammatory medicinal properties. More recently, potential anti-carcinogenic properties have been described. β-Escin, a pentacyclic triterpene saponin with aglycone moieties, is the main active compound in horse chestnut seed extract. Here, we summarize the anti-cancer properties of β-escin in preclinical models, and its potential pharmacological use as an anti-inflammatory agent for the treatment of edema and chronic venous insufficiency. The major mechanisms for the anti-inflammatory activities are through modulation of eicosanoids and nuclear factor-kappa B (NF-kB). Anti-proliferation activities occur via induction of p21 and decreased expression of cyclin D1 and anti-apoptotic members of the Bcl-2 family of proteins. In addition, we discuss the clinical pharmacokinetics of β-escin and review the factors that determine its absorption, bioavailability, and distribution in animals. Despite the many beneficial effects of β-escin, it has been studied less extensively in models of cancer. Further studies are warranted to assess the usefulness of β-escin for cancer prevention and therapy.

The positive clinical therapeutically effects of Escin on advanced thyroid cancer

“…In traditional Chinese medicine, Escin has been widely used to promote appetite, prevent gas formation of gastrointestinal tract, and documented as an antiseptic, anti‐edematous, and anti‐inflammatory agent in various disease models . Studies have shown the major mechanisms for the anti‐inflammatory effects of Escin are through modulation of NF‐ κ B signaling pathway .…”

“…Unless otherwise noted, all data presented as n (%).The disease control rate was defined as the proportion of patients who had a best response rating of a complete response, partial response, or stable disease that was maintained for ≥4 weeks from the first manifestation of the rating. gastrointestinal tract, and documented as an antiseptic, anti-edematous, and anti-inflammatory agent in various disease models [29]. Studies have shown the major mechanisms for the anti-inflammatory effects of Escin are through modulation of NF-κB signaling pathway [29].…”

Endothelia-Targeting Protection by Escin in Decompression Sickness Rats

“…Escin, or aescin, a natural mixture of triterpene saponins, is the major active compound in extracts from the seeds of Aesculus hippocastanum (horse chestnut tree), a widely used medicinal plant since ancient times910. It exists in two forms, α and β and the latter is the active component of the mixture10.…”

“…It exists in two forms, α and β and the latter is the active component of the mixture10. Escin has been traditionally used as a carminative, stomachic, and endothelia-protective agent in treating peripheral vascular disorders, in particular varicosis11.…”

“…Accumulating evidence suggests that escin exerts anti-edematous and anti-inflammatory properties mainly due to its endothelia-protective ability11. Escin reduces endothelia activation and sensitization to ions resulting in decreased neutrophil adherence and permeability to water13, and exerts anti-inflammatory and synergistic anti-inflammatory effects without immunosuppression1014. In addition, escin has been found effective as an antioxidant agent with the ability to scavenge reactive oxygen species (ROS)15 and induce endothelial NO synthesis by sensitization to Ca 2+ ions16.…”