Horse Chestnut
Scientific Name(s): Aesculus hippocastanum L. (horse chestnut), A. californica Nutt. (California buckeye) and A. glabra Willd. (Ohio buckeye). Family: Hippocastanaceae.
Common Name(s): Chestnut , horse chestnut , California buckeye , Ohio buckeye , buckeye .
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Uses of Horse Chestnut
Sweet chestnuts, used as food, are of a different genus (Castanez) than the horse chestnuts or buckeyes of traditional medicine, which are potentially useful against edema, inflammation, and venous insufficiency.
Horse Chestnut Dosing
Horse chestnut extracts typically are standardized on content of triterpene glycosides, calculated as the major component, escin. Doses corresponding to 20 to 120 mg of escin have been used for venous insufficiency. 1 , 2
Contraindications
No longer considered safe for use.
Pregnancy/Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking.
Horse Chestnut Interactions
None well documented.
Horse Chestnut Adverse Reactions
No data.
Toxicology
All parts of plants in the Aesculus family are potentially toxic, especially the seeds. Horse chestnut has been classified by the FDA as an unsafe herb. Buckeye sawdust and horse chestnut components in skin cleansers are potentially carcinogenic. Even buckeye honey may be toxic.
Botany
Members of the genus Aesculus grow as trees and shrubs, often attaining heights of 75 feet. The fruit is designated a capsule with a thick, leathery husk that contains from 1 to 6 dark seeds (the nuts). As the husk dries, the nuts are released. The pink and white flowers of the plant grow in clusters. The tree is native to the Balkan woods and western Asia, but is now cultivated worldwide. 3
History
Because of their prevalence, chestnuts have been used in traditional medicine and for a variety of other commercial applications for centuries. Extracts of the bark have been used as a yellow dye, and the wood has been used for furniture and packing cases. In the western US, the crushed unripe seeds of the California buckeye were scattered into streams to stupefy fish, and leaves were steeped as a tea to remedy congestion. The horse chestnut has been used as a traditional remedy for arthritis and rheumatism. Extracts are available commercially for oral, topical, and parenteral administration for the management of varicose veins and hemorrhoids. 4
Even though the seeds are toxic, several traditional methods were employed to rid them of their toxicity. Seeds were buried in swampy, cold ground during the winter to free them of toxic bitter components, then eaten in the spring after boiling. 5 Indians roasted the poisonous nuts, peeled, and mashed them, then leached the meal in lime water for several days, creating a meal used to make breads. 6
Chemistry
The seeds of Aesculus contain a variety of complex constituents. The seed oil contains 65% to 70% oleic acid. 7 The seeds contain protein, ash, and 74% carbohydrate. 6 In addition, 5 triterpene oligoglycosides from horse chestnut seeds have been isolated. 8 The main anti-inflammatory constituent aescin (escin) is present in the plant. 3 This mixture of triterpene glycosides has been radioimmunoassayed, 9 and investigated by HPLC where it was obtained from both cotyledon and stem parts. 10 Sapogenols hippocaesculin and barringtogenol-C 21–angelate have been obtained from fruit parts. 11 Flavonol glycosides quercitrin and its aglycone are also found. Coumarin glycosides found in horse chestnut include fraxin, scopolin, and their aglycones. 12 From the seeds, a lectin has been isolated and its amino acid composition determined. 13 Other constituents include allantoin, sterols, leucocyanidin, leucodelphinidin, tannins, adenine, adenosine, carotin, choline, citric, and uric acids. 6 , 12 Members of the genus produce the toxic glycoside esculin (aesculin in some texts). This poorly characterized toxin is found in the twigs, sprouts, leaves, and nuts. 7
Horse Chestnut Uses and Pharmacology
Commercial extracts of horse chestnut have been evaluated in the treatment of a number of disease states, primarily by European investigators.
CirculationEnzyme studies demonstrate that elastase (enzymes involved in turnover of perivascular substances) inhibition may be a mechanism involved. 14 Aesculin reduces capillary wall permeability by decreasing fluid retention, by increasing the permeability of capillaries, and allowing reabsorption of excess fluid back into the circulatory system. The bark yields aesculin, which improves vascular resistance and aids in toning vein walls. This is desirable for such ailments as hemorrhoids, varicose or problematic veins, leg ulcers, or frostbite. 3
Animal dataAn extract of the plant (containing 50 mg of triterpene glycosides) decreases venous capillary permeability and appears to have a “tonic” effect on the circulatory system. 15 Constituent aescin inhibits the increase of (induced) vascular permeability in mice and rats. 16 A commercial horse chestnut extract, which contains 70% aescin, has been found to possess a number of pharmacologic properties in vitro and in vivo, including the ability to contract the canine saphenous isolated vein and to potentiate the contractile response to norepinephrine. 17 Triterpene and steroid saponins from horse chestnut are effective in treating or preventing venous insufficiency in another report. 18
Clinical dataIn patients with chronic venous insufficiency, extracts have been found to be effective in reducing patient complaints, along with objective measures of edema. 19 In a placebo controlled study, horse-chestnut seed extract improved edema signs and symptoms in patients suffering from venous edema of chronic deep vein incompetence. 20
Diuretic effectsAnimal data
Aescin displayed moderate diuretic activity in rats, markedly increasing renal loss of sodium, chloride, and potassium. 18
Clinical dataResearch reveals no clinical data regarding the use of horse chestnut for diuretic effects.
Anti-inflammatory effectsAnti-inflammatory effects of horse chestnut preparations also have been reported. 3 , 21 The bark possesses anti-inflammatory activity, primarily due to the presence of the steroids stigmasterol, alpha-spinasterol, and beta-sitosterol. 22
Animal dataAescin extract reduces cutaneous capillary hyperpermeability induced by histamine or serotonin, and it decreases the formation of chemically induced rat paw edema. 17
Clinical dataOne reference reported a dosage of 20 mg/day (max) IV administration of preparation aescin to be effective in preventing or treating post-op edema. 23
Other usesOther varied pharmacological effects of horse chestnut preparations include: Treatment of whooping cough from a decoction of the leaves, 3 hypoglycemic activity in rats, 24 fever reduction, 3 , 6 ability to absorb the skin-damaging UV-B radiation in suntan products, 12 trophic effect on rat muscle by constituent proanthocyanioin-A2, 25 and antimicrobial actions from recently isolated antifungal proteins. 26
The pharmacology, pharmacokinetics, and toxicology of horse chestnut saponin (escin) has been reviewed. 27 , 28
Dosage
Horse chestnut extracts typically are standardized on content of triterpene glycosides, calculated as the major component, escin. Doses corresponding to 20 to 120 mg of escin have been used for venous insufficiency. 1 , 2
Pregnancy/Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking.
Interactions
None well documented.
Adverse Reactions
Research reveals little or no information regarding adverse reactions with the use of this product.
Toxicology
Aesculus (horse chestnut) is classified by the FDA as an unsafe herb; 6 all members of this genus should be considered potentially toxic. 29 A number of components have been attributed toxic properties, including glycosides and saponins. Potential toxins identified in the genus include nicotine, quercitin, quercitrin, rutin, saponin, and shikimic acid. 6
The most significant toxic principle is esculin. Poisoning is characterized by muscle twitching, weakness, lack of coordination, dilated pupils, vomiting, diarrhea, depression, paralysis, and stupor. 30 The nut is the most toxic part of the plant. 31 Children have been poisoned by drinking tea made from the leaves and twigs, and by eating the seeds; deaths have been reported following such ingestion. Amounts as little as 1% of a child's weight may be poisonous. Gastric lavage and symptomatic treatment have also been suggested. 30
The LD 50 of a single dose of the water-soluble portion of alcoholic extracts of horse chestnut seeds was calculated to be 10.6 mg/g body weight in chicks and 10.7 mg/g in hamsters. Extracts of the seeds of the Ohio buckeye were nontoxic to chicks and hamsters fed 80 mg/g in this study. 32
Honey made mainly from the California buckeye has been reported to be toxic. A potential association between nasal cancer and long-term exposure to wood dusts, including dust from chestnut trees, has been reported. 33 Aflatoxins have been identified in some commercial skin cleansing products containing horse chestnut. Since aflatoxins are potent carcinogens that can be absorbed through the skin, it is imperative that strict quality control be applied to topical products containing potentially contaminated horse chestnut material. 34
Horse chestnut pollen is allergenic and often associated with the development of allergic sensitization, particularly in urban children. 35
A case report describes drug-induced hepatic injury to a 37-year-old male, induced by venoplant (horse chestnut extract preparation) given for treatment of bone fracture inflammation. 36
An analysis of serious plant poisonings in Switzerland from 1966 to 1994 reveals horse chestnut to be responsible for 3 allergies and 2 anaphylactic shock episodes. 37
Bibliography
1. Pauschinger K. Clinico-experimental investigations of the effect of horse-chestnut extract on the transcapillary filtration and the intravasal volume in patients with chronic venous insufficiency. Phlebology Proctology . 1987;2:57-61.2. Diehm C, Trampisch HJ, Lange S, Schmidt C. Comparison of leg compression stocking and oral horse-chestnut seed extract therapy in patients with chronic venous insufficiency. Lancet . 1996;347:292-294.
3. Chevallier A. Encyclopedia of Medicinal Plants. New York, NY: DK Publishing, 1996;159.
4. Tyler V, et al. Pharmacognosy. Philadelphia, PA: Lea & Febiger, 1988.
5. Sweet M. Common Edible & Useful Plants of the West. Healdsburg, CA: Naturegraph Publishers, 1976.
6. Duke J. Handbook of Medicinal Herbs. Boca Raton, FL: CRC Press, 1985.
7. Evans W. Trease and Evans' Pharmacognosy, ed. 13. London, England: Bailliere Tindall, 1989.
8. Yoshikawa M, et al. Chem Pharm Bull 1994;42(6):1357-59.
9. Lehtola T, et al. J Immunoassay 1990;11(1):17-30.
10. Profumo P, et al. J Pharm Pharmacol 1994;46(11):924-25.
11. Konoshima T, et al. J Nat Prod 1986;49(4):650-56.
12. Bisset N. Herbal Drugs and Phytopharmaceuticals. Stuttgart, Germany: CRC Press, 1994;268-72.
13. Antoniuk V. UKR Biokhim Zh 1992;64(5):47-52.
14. Facino R, et al. Arch Pharm 1995;328(10):720-24.
15. Bisler H, et al. Dtsch Med Wochenschr 1986;111(35):1321.
16. Matsuda H, et al. Biol Pharm Bull 1997;20(10):1092-95.
17. Guillaume M, et al. Arzneimittleforschung 1994;44:25.
18. Martin M, et al. Ann Pharm Fr 1990;48(6):306-11.
19. Hitzenberger G. Wien Med Wochenschr 1989;139(17):385.
20. Diehm C, et al. Vasa 1992;21:188.
21. Tsutsumi S, et al. Shikwa Gakuho 1967;67(11):1324-28.
22. Senatore F, et al. Boll Soc Ital Biol Sper 1989;65(2):137.
23. Reynolds J, ed. Martindale: The Extra Pharmacopoeia, ed. 31. Royal Pharmaceutical Society, London, England, 1996:1670.
24. Yoshikawa M, et al. Chem Pharm Bull 1996;44(8):1454-64.
25. Ambrogini P, et al. Boll Soc Ital Biol Sper 1995;71(7-8):227-34.
26. Osborn R, et al. Febs Lett 1995;368(2):257-62.
27. Panigati, D. Boll Chim Farm 1992;131(7):284-93.
28. Panigati, D. Boll Chim Farm 1992;131(8):320-21.
29. Nagy M. JAMA (letter) 1973;226(2):213.
30. Hardin J, et al. Human Poisoning From Native and Cultivated Plants, ed. 2. Durham, NC: Duke University Press, 1974.
31. Anon. Vet Hum Toxicol 1983;25:80.
32. Williams M, et al. Am J Vet Res 1984;45(3):539.
33. Battista G, et al. Scand J Work Environ Health 1983;9(1):25.
34. el-Dessouki S. Food Chem Toxicol 1992;30:993.
35. Popp W, et al. Allergy 1992;47:380.
36. Takegoshi K, et al Gastroenterol Jpn 1986;21(1):62-65.
37. Jaspersen-Schib R, et al. Schweiz Med Wochenschr 1996;126(25):1085-98.
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horse chestnut Drug Interactions
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Varicose Veins, Hemorrhoids, Nocturnal Leg Cramps, Inflammatory Conditions
