Plant Profiler

Horse chestnut (Aesculus hippocastanum)


Horse chestnut (Aesculus hippocastanum) Image
Synonyms / Common Names / Related Terms
Aescin, aescine, Aesculaforce®, aescule, aesculetin, buckeye, bongay, chestnut, conkers, Conquerors, coumarins, eschilo, escin, escina, escine, fatty acids, fish poison, flavonoids, graine de marronier d'Inde (French), fraxetin glucoside, fraxin, H. vulgare Gaertnhestekastanje, HCSE, Hippocastabi foliu, Hippocastanaceae (family), Hippocastani semen, horse chestnut seed extract, horsechestnut, linolenic acid, Marron Europeen, Marronier, NV-101, palmitic acid, quinines, Rokastaniensamen, rosskastanie, scopoletin glucoside, scopolin, Spanish chestnut, tannins, steric acid, sterols, Venastat, Venoplant, Venostasin.



Mechanism of Action

Pharmacology:

  • Constituents: Horse chestnut seed contains a triterpene saponin mixture called escin (3-6%), flavonoids, condensed tannins, quinines, sterols and fatty acids (including linolenic acid, palmitic acid and steric acid), and coumarins (including aesculetin, fraxin [fraxetin glucoside], and scopolin [scopoletin glucoside]). The main active ingredient is considered to be escin (or aescin), which acts on capillary membranes to normalize vascular permeability.8 Horse chestnut seeds contain approximately 95mg of lectin per 1kg of fresh seeds.9
  • Anti-inflammatory effects: Purified escin has been shown to decrease chemically-induced inflammation in rats.5,6,2
  • Antioxidant effects: HCSE extract has been reported to have antioxidant effects.2,7
  • Antithrombin effects: Horse chestnut contains the hydroxycoumarin component esculin, which may have antithrombin activity. Esculin is found in the bark, buds, and other parts of the fruits, but it should not be present in properly extracted HCSE.
  • Vascular effects: Horse chestnut seed extract (HCSE) inhibits enzymes that are implicated in the pathogenesis of chronic venous insufficiency.1 It has been found to dose-dependently contract canine2 and human3 isolated saphenous veins in vitro, possibly due to preferential formation of the vasoconstrictive eicosanoid, PGF 2-alpha4. HCSE has also been shown to: increase femoral venous pressure and flow, decrease the formation of edema induced in rat paw models, and to suppress plasma extravasation and leucocyte emigration into the pleural cavity in an experimental rat model of pleurisy.2 Purified escin has been shown to decrease histamine and serotonin-induced capillary hyperpermeability.5,6,2 In aggregate, these findings suggest that HCSE increases venous tone, improves venous return, and reduces vascular permeability, all which lead to the clinical benefit of dependent edema reduction.

Pharmacodynamics/Kinetics:

  • Oral escin is not well absorbed and undergoes substantial first-pass effect. The half-life of horse chestnut is approximately 10-20 hours. Peak plasma levels occur 2-3 hours after ingestion.10 The bioavailability of beta-aescin, the main active constituent of horse chestnut seed extract, was evaluated in two randomized crossover clinical trials involving 18 healthy volunteers each. The trials found that there was no difference between the absorption rates for the retarded versus nonretarded preparation and that daytime absorption was slightly better than nighttime.11

References

  1. Kreysel, H. W., Nissen, H. P., and Enghofer, E. A possible role of lysosomal enzymes in the pathogenesis of varicosis and the reduction in their serum activity by Venostasin. Vasa 1983;12(4):377-382. 6659692
  2. Guillaume, M. and Padioleau, F. Veinotonic effect, vascular protection, antiinflammatory and free radical scavenging properties of horse chestnut extract. Arzneimittelforschung 1994;44(1):25-35. 8135874
  3. Brunner, F., Hoffmann, C., and Schuller-Petrovic, S. Responsiveness of human varicose saphenous veins to vasoactive agents. Br J Clin Pharmacol 2001;51(3):219-224. 11298067
  4. Longiave, D., Omini, C., Nicosia, S., and Berti, F. The mode of action of aescin on isolated veins: relationship with PGF2 alpha. Pharmacol Res Commun 1978;10(2):145-152. 652841
  5. Matsuda, H., Li, Y., Murakami, T., Ninomiya, K., Yamahara, J., and Yoshikawa, M. Effects of escins Ia, Ib, IIa, and IIb from horse chestnut, the seeds of Aesculus hippocastanum L., on acute inflammation in animals. Biol Pharm Bull 1997;20(10):1092-1095. 9353571
  6. Matsuda H, Yuhao, L, Murakami T, and et al. Antiinflammatory effects of escins Ia, Ib, IIa, and IIb from horse chestnut, the seeds of Aesculus Hippocastanum L. Bioorganic Med Chem Lett 1997;7(13):1611-1616.
  7. Masaki, H., Sakaki, S., Atsumi, T., and Sakurai, H. Active-oxygen scavenging activity of plant extracts. Biol Pharm Bull 1995;18(1):162-166. 7735233
  8. Brunner, F., Hoffmann, C., and Schuller-Petrovic, S. Responsiveness of human varicose saphenous veins to vasoactive agents. Br J Clin Pharmacol 2001;51(3):219-224. 11298067
  9. Antoniuk, V. O. [Isolation of lectin from horse chestnut (Aesculus hippocastanum L.) seeds and study of its interaction with carbohydrates and glycoproteins]. Ukr Biokhim Zh 1992;64(5):47-52. 1462370
  10. Schrader, E., Schwankl, W., Sieder, C., and Christoffel, V. [Comparison of the bioavailability of beta-aescin after single oral administration of two different drug formulations containing an extract of horse-chestnut seeds]. Pharmazie 1995;50(9):623-627. 7480102
  11. Bassler, D., Okpanyi, S., Schrodter, A., Loew, D., Schurer, M., and Schulz, H. U. Bioavailability of beta-aescin from horse chestnut seed extract: comparative clinical studies of two Galenic formulations. Adv Ther 2003;20(5):295-304. 14964349




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