Goldenseal (Hydrastis canadensis)

 
Goldenseal a herb you should know, also known as berberine, is a member of the buttercup or Ranunculaceae family. It is a low growing perennial plant with red fruit. Its root has a bright, deep yellow appearance. Goldenseal is native to and grows in the midwestern and eastern parts of the USA in woodlands, including the Ohio River Valley, West Virginia, the mountains of North and South Carolina, Kentucky, Tennessee, and north to New England and Upstate New York and parts of Quebec, Canada.

Goldenseal can be difficult to cultivate for production level quantities, and wildcrafting this botanical agent can be challenging and that is why it is somewhat expensive compared to other herbs.

Harvesting the root by hand can leave a yellow stain on one’s fingers and it has a distinctive, sharp, pungent smell when working with the freshly dug root. It was harvested almost to extinction in the mid to late 1800’s in the Ohio River Valley where it was sold heavily in Cincinnati in amounts upwards of 200,000 pounds.

Eclectic physicians learned about the plant from Native Americans who
revered the plant for its medicinal, cultural, and practical uses. The deforestation of the North Eastern United states, along with demand and over harvesting, led to this plant’s status as endangered in its natural range. The Eclectics used purified forms of the crude
herb known in the commercial market as Hydrastine, Neutral Hydrastine, or Muriate of Hydrastin – preparations which were actually hydrochlorates of the alkaloid berberine. These preparations did not yield the same results as the concentrated whole plant extract and were soon abandoned.

ACTIVE CONSTITUENTS
A number of active constituents of Goldenseal have been identified. The root and rhizomes are highly concentrated in isoquinoline alkaloids or protoberberines, namely hydrastine, berberine, and canadine. Goldenseal has been reported to contain these alkaloids in the ranges of 1.5-4% hydrastine, 0.5-6% berberine, and 2-3% berberastine.1

Research evidence reports Goldenseal showed antimicrobial activity for both in vitro and animal research. This antimicrobial activity is thought to have action through inhibition of RNA and protein synthesis2, and inhibiting the adherence of pathological bacteria to epithelial cells.5

Antimicrobial activity: Berberine sulfate demonstrated antimicrobial activity against Gram-positive and Gram-negative organisms in vitro through inhibition of RNA and protein synthesis.2 In particular, berberine was also shown to be bactericidal against Vibrio cholera and against Staphylococcus aureus. 2
Other microorganisms that were inhibited by goldenseal include Clostridium tetani 3, Candida krusei 4, and Streptococcus pyogenes. Berberine inhibited the adherence of S. pyogenes to epithelial cells possibly by immobilizing fibronectin and hexadecane, and this disrupted a primary pathological process.5

Antifungal activity: Berberine exhibited antifungal activity against Alternaria, Aspergillus flavus, A. fumigates, Candida albicans, Curvularia, Drechslera, Fusarium, Mucor, and Rhizopus oryzae. 6 Berberine sulfate possessed antifungal activity in vitro through inhibition of RNA and protein synthesis.2

Antiparasitic effects: Berberine sulfate demonstrated antimicrobial activity against protozoal organisms in vitro through inhibition of RNA and protein synthesis.2
In vitro, a methanol extract of berberine demonstrated parasiticidal activity against T. vaginalis, G. lamblia, and E. histolytica.7 Subsequent research has shown berberine chloride to decrease parasitic load in animals.8

Cardiovascular effects: Berberine may possess partial agonist activity at platelet alpha-2 receptors.9 This may have particular effect in adrenaline-induced cardiac pathology and
cardiomyopathy affected by undue stress and related physiological changes in response to stress (distress).

A 12 patient study showed significant improvement in systemic and pulmonary vascular resistance, right atrial and left ventricular end-diastolic pressures, cardiac index, and left ventricular ejection fraction. 10

Digestive and Gastrointestinal effects: In 20 healthy subjects, the oral administration of 1.2g of berberine significantly delayed small intestinal transit time of a meglucamine
diatrizoate and sorbitol test mixture.11 Oral berberine sulfate (40-80mg/kg) significantly decreased the occurrence of diarrhea induced by ingestion of castor oil and Cassia angustifolia in mice.12

Clinical Indications
• Antibacterial
• Antifungal
• Antiparasitic
• Cardiovascular
• Digestive and gastrointestinal

Dosage range
General antimicrobial and related symptoms relief: The dosage range used in studies and clinical practice is varied. For liquid alcohol-based tincture or encapsulated tinctures, 200 – 250 mg (2x – 3x/day) is a typical dosage.

Cardiovascular: Dosing strategy is typically 300 mg a day, evenly divided doses, either with or without food. For heart failure, higher dosing may be warranted, based on patient symptom severity; up to 2g daily for 8 weeks has been researched, in divided
doses.13

Contraindications

Patients with known allergy/hypersensitivity to Hydrastis canadensis or any of its constituents, or to members of the buttercup or Ranunculaceae family, should avoid using this botanical agent.

Toxicity

Toxic doses of berberine may cause convulsions and irritation of the uppergastrointestinal tract when taken orally; however, the dose range for this toxicity is unclear.1

Conclusions

The overall botanical medicine benefit profile for Goldenseal makes it a viable botanical agent for its antimicrobial activity, including antibacterial, antifungal and antiparasitic activity. There is also research to support its use for the cardiovascular system, including cardiomyopathy, heart failure and other cardiovascular pathologies. It appears to be a safe herb for medicinal use when used within the established dosage guidelines and with regard for pertinent contraindications.

REFERENCES
1 Hamon, NW. Goldenseal. CPJ-RPC 1990;508-510.

2 Amin, A. H., Subbaiah, T. V., and Abbasi, K. M. Berberine sulfate: antimicrobial activity, bioassay, and mode of action. Can. J. Microbiol. 1969;15(9):1067-1076.

3 Palasuntheram C, Iyer KS, de Silva LB, and et al. Antibacterial activity of Coscinium fenestratum Colebr against Clostridium tetani. Ind J Med Res 1982;76(Suppl):71-76.

4 Park, K. S., Kang, K. C., Kim, J. H., Adams, D. J., Johng, T. N., and Paik, Y. K. Differential inhibitory effects of protoberberines on sterol and chitin biosyntheses in Candida albicans. J Antimicrob.Chemother 1999;43(5):667-674.

5 Sun D, Courtney HS, and Beachey EH. Berberine sulfate blocks adherence of Streptococcus pyogenes to epithelial cells, fibronectin, and hexadecane. Antimicrobial Agents and Chemotherapy 1988;32(9):1370-1374.

6 Mahajan VM, Sharma A, and Rattan A. Antimycotic activity of berberine sulphate: an alkaloid from an Indian medicinal herb. Sabouraudia 1982;20:79-81.

7 Kaneda Y, Tanaka T, and Saw T. Effects of berberine, a plant alkaloid, on the growth of anaerobic protozoa in axenic culture. Tokai J Exp Clin Med 1990;15(6):417-423.

8 Ghosh AK, Bhattacharyya FK, and Ghosh DK. Leishmania donovani: amastigote inhibition and mode of action of berberine. Experimental Parasitology 1985;60:404-413.

9 Hui, K. K., Yu, J. L., Chan, W. F., and Tse, E. Interaction of berberine with human platelet alpha 2 adrenoceptors. Life Sci. 1991;49(4):315-324.

10 Marin-Neto, J. A., Maciel, B. C., Secches, A. L., and Gallo, Junior L. Cardiovascular effects of berberine in patients with severe congestive heart failure. Clin.Cardiol. 1988;11(4):253-260.

11 Yuan, J., Shen, X. Z., and Zhu, X. S. [Effect of berberine on transit time of human small intestine].

Zhongguo Zhong.Xi.Yi.Jie.He.Za Zhi. 1994;14(12):718-720.
12 Freile, M. L., Giannini, F., Pucci, G., Sturniolo, A., Rodero, L., Pucci, O., Balzareti, V., and Enriz, R. D. Antimicrobial activity of aqueous extracts and of berberine isolated from Berberis heterophylla. Fitoterapia 2003;74(7-8):702-705.

13 Zeng, X. H., Zeng, X. J., and Li, Y. Y. Efficacy and safety of berberine for congestive heart failure secondary to ischemic or idiopathic dilated cardiomyopathy. Am J Cardiol. 7-15-2003;92(2):173-176. 5

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