Escin, esculin and your skin
microcirculation, vein support, water retention/oedema, cellulite
The horse chestnut tree (aesculus hippocastanum) extracts escin (aescin / beta escin / beta aescin) and esculin (esculoside / esculetin) have been extensively studied for several decades and has been found to protect and tone veins, fight inflammation in blood vessels and boost microcirculation. As a result, escin and esculoside boost circulation and fight water retention (they have been found to be as effective as medical compression stockings for the treatment of chronic venous insufficiency (CVI) and clinical water retention (oedema).
For all these reasons, escin and esculin are also of great importance as active ingredients in under-eye, leg wellness and cellulite creams. Horse chestnut creams containing concentrated extracts of escin / esculin are popular for puffy, heavy legs with poor circulation [the Celluence® creams are the only cellulite creams in the world with high concentrations of 95%+ pure escin and 95%+ pure esculin, plus 38x other natural anti-cellulite actives].
Below you can find a comprehensive review of all the research papers on escin / esculin / horse chestnut extract and their effect on microcirculation, oedema/water retention and vein protection.
Escin and esculin: the science
escin prevents leaky capillaries and consequent water retention...
...by reducing the effects of the pro-inflammatory protein TNF-alpha on endothelial blood vessel cells
[Source: Molecular Mechanism for Cellular Response to β-Escin and Its Therapeutic Implications].
escin is as effective as compression garments for water retention and heavy legs
Compression garments are routinely used to treat the symptoms of water retention / oedema arising from chronic venous insufficiency. However, compression garments are uncomfortable, especially in the summer when actually water retention is at it's worst; they lead to reduced arterial flow and skin laxity; and they do not help nourish the blood vessels. This study has shown that 100mg/day of escin is as good as compression bandages for water retention, after 12 weeks of use. Escin, however, does not burden the patient with the discomfort of compression tights, offering a superior quality of life, and in addition it strengthens and nourishes the capillaries.
[Source: Comparison of leg compression stocking and oral horse-chestnut seed extract therapy in patients with chronic venous insufficiency]
Escin, rutin and Daflon equally effective for oedema / water retention
Escin, rutin/hydroxyethylrutoside and Daflon(hesperidin + diosmin) have been shown to be safe and effective for the treatment of chronic venous insufficiency (CVI). According to a review of three of the most popular venotonic natural actives, they all work by reducing the drop of ATP in vein endothelial cells during hypoxia (low oxygen levels). This prevents inflammation, damage to the veins and capillary permeability (leaky capillaries). All three phlebotonics boost venous tone, while escin additionally inhibits the breakdown of hyaluronic acid by the enzyme hyaluronidase.
[Source: Three treatments for chronic venous insufficiency: escin, hydroxyethylrutoside, and Daflon]
Aescin improves venous tone by boosting the formation of prostaglandin PGF2-alpha in vein cells
According to this paper the therapeutic effect of escin in acute and chronic water retention could be partly explained by it's ability to enhance PGF2α generation in the veins.
[Source: The mode of action of aescin on isolated veins: Relationship with PGF2α]
Escin reduces lower leg swelling, heaviness, fatigue, pain and itching caused by water retention
A review of all placebo-controlled studies on the the clinical effectiveness of beta-escin from horse chestnut has shown that it is "superior to placebo and as effective as reference medications in alleviating the objective signs and subjective symptoms of chronic venous insufficiency".
[Source: Horse-Chestnut Seed Extract for Chronic Venous Insufficiency: A Criteria-Based Systematic Review]
Escin improves chronic venous insufficiency (CVI), haemorrhoids and post-operative oedema...
...by raising venous tension, releasing the prostaglandin PGF2 from veins, antagonising serotonin and histamine in veins and reducing catabolism of hyaluronic acid. According to the authors of the study, escin displays "clear-cut anti-oedematous, anti-inflammatory and venotonic properties".
[Source: Aescin: pharmacology, pharmacokinetics and therapeutic profile]
ENDOTHELIUM PROTECTANT AND CONTRACTILE EFFECTS OF THE ANTIVARICOSE PRINCIPLE ESCIN IN RAT AORTA
- Journal: Vascular Pharmacology
- The triterpene saponin escin is the active component of the extract of seeds of Aesculus hippocastanum used in the treatment of chronic venous insufficiency. Escin is also used experimentally to increase membrane permeability in isolated cells. Since endothelial dysfunction is postulated to be involved in venous insufficiency, the possible endothelium-protectant effect of escin was explored in rat aortic rings, a model widely used to study such effects with cardiovascular agents. Escin enhanced endothelium-dependent relaxation induced by acetylcholine when such relaxation had been reduced by exposure to the superoxide ion generator pyrogallol. This effect was attributed to enhanced nitric oxide production by endothelial nitric oxide synthase, a calcium-dependent enzyme, activated by the increased endothelial cell permeability to calcium induced by escin. Another effect of escin thought to contribute to its therapeutic activity is its ability to produce venous contraction. The compound was found to induce concentration-related contraction also in rat aortic rings. This response was partially inhibited by removal of the endothelium or by preincubation with indomethacin, and was completely abolished by incubation in a calcium-free perfusion fluid. Contraction was considered to be due mainly to the aforementioned effect on calcium permeability, with some mediation by release of endothelial vasoconstrictor prostanoids. It was concluded that, in rat aorta, escin possesses an endothelium-protectant action and a direct contractile effect. The former could contribute to its beneficial effect in the treatment of venous insufficiency, while the latter could constitute a limiting side effect.
THE MODE OF ACTION OF AESCIN AND THE RELEASE OF PROSTAGLANDINS
- Journal: prostaglandins
- Abstract: The horse-chestnut saponin Aescin, an anti-exudative compound, induces contraction of isolated portal vein of rat and rabbit. This effect appears to be mediated by Prostaglandins of Fα type. The ability of Aescin to stimulate generation and release of Prostaglandins has been demonstrated in isolated lung of the rat. Mass-fragmentographic analysis of the lung effluent indicate that when Aescin is perfused through this organ the release of PGF2α is increased. The capability of Aescin to generate Prostaglandins is discussed in connection with its anti-exudative activity.
- Link: http://www.sciencedirect.com/science/article/pii/0090698077901691
EFFECT OF BETA-AESCIN EXTRACT FROM CHINESE BUCKEYE SEED ON CHRONIC VENOUS INSUFFICIENCY.
- Journal: Die Pharmazie
- Abstract: The aim of this study was to explore the mechanism of domestic beta-aescin treating chronic venous insufficiency through observing its actions on the isolated canine saphenous venous tension, venous pressure, venous return and lymphatic return. The isolated canine spiral saphenous venous tension test was performed to detect the activity of the beta-aescin. Furthermore, in the condition of constant canine femoral artery perfusion kept in the extracorporeal circulation, we measured the changes of the canine femoral artery pressure, femoral artery flow and the lymphatic return flow after intravenous injection of the agent. The results showed that when beta-aescin was administrated at the dose between 5.0 x 10(-5)-5.25 x 10(-4) mol/L, it increased obviously the contractile tension of the venous to norepinephrine in a dose-dependent manner. With canine femoral artery perfusion kept constant, beta-aescin, whose doses were 50 mg and 100 mg, reinforced intently the canine femoral venous tension accelerated the rise of the venous pressure. These finding suggested that domestic beta-aescin extracted from Chinese Buckeye Seed had an effect on chronic venous insufficiency by strengthening the venous tension, increasing the venous pressure and promoting venous return and lymphatic return.
- Link: http://www.ncbi.nlm.nih.gov/pubmed/23875249
PHARMACOLOGY OF ESCIN, A SAPONIN FROM AESCULUS HYPPOCASTANUM L. II. PHARMACODYNAMICS OF ESCIN. CHAPTERS I & II
- Journal: Bollettino Chimico Farmaceutico
- Abstract: N/A
- Links: http://www.ncbi.nlm.nih.gov/pubmed/1445691, http://www.ncbi.nlm.nih.gov/pubmed/1476699