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.
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 wide?spread harvesting. of Hydrastis in the 19th century, coupled with loss of habitat, resulted in depletion of wild populations. In 1997, Hydrastis was listed under Appen?dix II of the Convention on International Trade in Endan?gered 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, gold?enseal, like other expensive herbs, has often been adul?terated. Common adulterants include species of Coptis and Xanthorrhiza, 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 String?town 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.
The isoquinoline alkaloids hydrastine (4%), berberine (up to 6%), and canadine are present in goldenseal root and are viewed as the principle bioactive components? Other minor alkaloids such as cana~ and canadinic acid9 have been isolated. Quinic esters were elucidated. Quantitation of the a~ has been accomplished in a variety of ways ind spectrophotometry, 11 thin-layer chromatography,! pair dye colorimetry,13 high-performance liquid en tography (HPLC),14 capillary electrophoresis,15 an mass spectrometry.
While berberine is widely uted in plants, hydrastine is characteristic of gale root and is considered to be the most important bi alkaloid. There is extensive pharmacologic Iiteral hydrastine and berberine. The alkaloids are poosorbed when taken orally, so studies of parea dministered goldenseal alkaloids must be inte with care. Goldenseal alkaloids have modest antir bial activity, which may be relevant when appliedl Berberine, canadine, and canadaline had disinll. activity against strains of bacteria, while hydrastine inactive.
Berberine sulfate was bactericidal Vibrio cholerae but bacteriostatic to Staphylococ reus.18 Berberine sulfate has been shown to blacka, ence of Streptococcus pyogenes to epithelial cells,! may be a reasonable mode of action for topical a crobial use.19 Berberine has been identified as the al component of Hydrastis in an antitubercular a while hydrastine and other isolated compounds activity. Berberine has been reported to inhibit up!, glucose by cancer cells,2O and to inhibit tumor pron by phorbol esters in a mouse skin carcinogel model.21 Berberine showed weak activity in an an dant model. Palmery investigated the inhibitoryac of Hydrastis alkaloids on isolated rabbit aorta stim by epinephrine, finding a weak synergistic effect berberine, canadine, and canadaline, but no actr hydrastine.23 In isolated guinea pig ileum preparal the same group found that berberine, canadine, canadaline evoked contractions, while hydrastine al was inactive.24 A third study found a relaxant eff! berberine on rabbit prostate strips stimulated by narephrine or phenylephrine;25 however, an adrenel mechanism was considered unlikely. While hydrasti closely related to the convulsant isoquinoline all bicuculline, hydrastine had no activity in a GABA.ree binding assay at high concentrations.