Goldenseal

Scientific Name(s): Hydrastis canadensis L. Family: Ranunculaceae (buttercups)

Common Name(s): Goldenseal , yellowroot , orangeroot , eyebalm , eyeroot , goldenroot , ground raspberry , Indian turmeric , yellow puccoon , jaundice root , sceau d'or

Clinical Overview

Uses of Goldenseal

Goldenseal may be of use in topical infections and is used as an eyewash. Goldenseal has been included in cold and flu preparations for its anticatarrhal effects but little evidence supports this use and its effects are debatable. Goldenseal may be of use in topical infections and is used as an eyewash.

Goldenseal Dosing

Extracts standardized to 5% hydrastine are available; however, the berberine content may be more important for goldenseal's medicinal uses. Doses of 100 mg hydrastine and 2 g crude root have been proposed.

Contraindications

Goldenseal is contraindicated in patients who have hypertension.

Pregnancy/Lactation

Documented uterine stimulant. Avoid use.

Goldenseal Interactions

Based on available data, goldenseal does not appear to interact with indinavir.

Goldenseal Adverse Reactions

Adverse effects to usual doses are rare. Very high doses of goldenseal may rarely induce nausea, anxiety, depression, seizures, or paralysis.

Toxicology

Research reveals little or no information regarding toxicology with the use of this product.

Botany

Goldenseal is a perennial herb found in the rich woods of the Ohio River valley and other locations in the northeastern US. The single, green-white flower, which has no petals, appears in the spring on a hairy stem above a basal leaf and 2 palmate, wrinkled leaves. The flower develops into a red seeded berry. The plant grows from horizontal, bright yellow rhizomes, which have a twisted, knotty appearance.

History

Goldenseal root was used medicinally by American Indians of the Cherokee, Catawba, Iroquois, and Kickapoo tribes as an insect repellent, a diuretic, a stimulant, and a wash for sore or inflamed eyes. 1 It was used to treat arrow wounds and ulcers, 2 as well as to produce a yellow dye. Early settlers learned of these uses from the Indians and the root found its way into most 19th century pharmacopeias. The Eclectic medical movement was particularly enthusiastic in its adoption of goldenseal for gonorrhea and urinary tract infections. The widespread harvesting of Hydrastis in the 19th century, coupled with loss of habitat, resulted in depletion of wild populations. In 1997, Hydrastis was listed under Appendix ΙΙ of the Convention on International Trade in Endangered Species of Wild Fauna and Flora (CITES), which controls exports of the root to other countries. The final listing included roots or live plants but excluded finished products. As an alternative to wild harvesting, goldenseal was cultivated in the Skagit Valley of Washington state and is being promoted as a cash crop in New York, North Carolina, 3 and Canada. Because of its high price, goldenseal, like other expensive herbs, has often been adulterated. Common adulterants include species of Coptis and Xanthorrhiza , 4 both of which also contain large amounts of the yellow alkaloid berberine. The popular notion that goldenseal can be used to affect the outcome of urinalysis for illicit drugs evolved from the novel Stringtown on the Pike by pharmacist John Uri Lloyd, in which goldenseal bitters are mistaken for strychnine in a simple alkaloid test by an expert witness in a murder trial. 5 Goldenseal can be variously ingested prior to testing or added to the urine sample after collection. It is one of several adulterants commonly detected in urinalysis samples. 6

Chemistry

The isoquinoline alkaloids hydrastine (4%), berberine (up to 6%), and canadine are present in goldenseal root and are viewed as the principle bioactive components. 7 Other minor alkaloids such as canadaline 8 and canadinic acid 9 have been isolated. Quinic acid esters were elucidated. 10 Quantitation of the alkaloids has been accomplished in a variety of ways including spectrophotometry, 11 thin-layer chromatography, 12 ion-pair dye colorimetry, 13 high-performance liquid chromatography (HPLC), 14 capillary electrophoresis, 15 and CE-mass spectrometry. 16

Goldenseal Uses and Pharmacology

While berberine is widely distributed in plants, hydrastine is characteristic of goldenseal root and is considered to be the most important bioactive alkaloid. There is extensive pharmacologic literature on hydrastine and berberine. The alkaloids are poorly absorbed when taken orally, so studies of parenterally administered goldenseal alkaloids must be interpreted with care.

Research reveals no animal data regarding the use of goldenseal for antimicrobial activity.

Goldenseal alkaloids have modest antimicrobial activity, which may be relevant when applied topically. Berberine, canadine, and canadaline had disinfectant activity against 6 strains of bacteria, while hydrastine was inactive. 17 Berberine sulfate was bactericidal against Vibrio cholerae but bacteriostatic to Staphylococcus aureus . 18 Berberine sulfate has been shown to block adherence of Streptococcus pyogenes to epithelial cells, which may be a reasonable mode of action for topical antimicrobial use. 19 Berberine has been identified as the active component of Hydrastis in an antitubercular assay, 10 while hydrastine and other isolated compounds had no activity.

Berberine has been reported to inhibit uptake of glucose by cancer cells, 20 and to inhibit tumor promotion by phorbol esters in a mouse skin carcinogenesis model. 21 Berberine showed weak activity in an antioxidant model. 22 Palmery investigated the inhibitory activity of Hydrastis alkaloids on isolated rabbit aorta stimulated by epinephrine, finding a weak synergistic effect for berberine, canadine, and canadaline, but no activity in hydrastine. 23 In isolated guinea pig ileum preparations, the same group found that berberine, canadine, and canadaline evoked contractions, while hydrastine again was inactive. 24 A third study found a relaxant effect of berberine on rabbit prostate strips stimulated by norepinephrine or phenylephrine; 25 however, an adrenergic mechanism was considered unlikely. While hydrastine is closely related to the convulsant isoquinoline alkaloid bicuculline, hydrastine had no activity in a GABA-receptor binding assay at high concentrations. 26

Dosage

Goldenseal has not been the subject of any formal clinical trials for external antiseptic or antiherpes properties. Extracts standardized to 5% hydrastine are available; however, the berberine content may be more important for goldenseal's medicinal uses. Doses of 100 mg hydrastine and 2 g crude root have been proposed. 27

Pregnancy/Lactation

Documented uterine stimulant. Avoid use. 28 , 29 , 30

Interactions

Based on available data, goldenseal does not appear to interact with indinavir. In 10 healthy subjects, pretreatment with 1140 mg of goldenseal root twice daily for 14 days did not alter the peak plasma concentration, oral clearance, half-life, or time to reach the peak concentration of indinavir when administered as a single oral dose of 800 mg. 31

Adverse Reactions

Very high doses of goldenseal may rarely induce nausea, anxiety, depression, seizures, or paralysis. Hydrastine was once used as a uterine hemostatic, 7 but was found inferior to ergot in the treatment of postpartum hemorrhage. Goldenseal is generally contraindicated for use in pregnancy. Because of hypertensive actions of the alkaloids, it is also contraindicated in cardiovascular patients.

Toxicology

Research reveals little or no information regarding toxicology with the use of this product.

Bibliography

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