Goldenseal

Plant Part Used

Root/Rhizome.

Active Constituents

Alkaloids, including hydrastine, berberine, canadine, berberastine and palmatine. (1),(26)[span class=alert]

This section is a list of chemical entities identified in this dietary supplement to possess pharmacological activity. This list does not imply that other, yet unidentified, constituents do not influence the pharmacological activity of this dietary supplement nor does it imply that any one constituent possesses greater influence on the overall pharmacological effect of this dietary supplement.[/span]

Introduction

Goldenseal has a long history of use in the United States as a medicinal herb. It was initially used by Native Americans and gained popularity with the eclectic medical movement from the 1850's to the 1940's. It has been used for GI disturbances, as an anti-infective, to stimulate bile flow, and as an eye wash.

Goldenseal is one of the most popular herbs on the market in the United States. Its widespread use has resulted in over-harvesting in the wild and endangering the long-term survival of the species. There are alternative plants that contain similar active constituents as goldenseal (berberine and hydrastine), including Chinese goldthread (Coptis chinensis) and Oregon grape (Berberis aquifolium), barberry (Berberis vulgaris), and tree tumeric (Berberis aristata) that may be therapeutic substitutions for goldenseal. (2) Goldenseal is commonly found in combination with Echinacea purpurea (L.) Moench. (27)

Interactions and Depletions

Interactions

Dosage Info

Dosage Range

125-250mg (standardized extract), 2-4 times a day.

Most Common Dosage

125mg (standardized extract), 3-4 times a day.

Standardization

[span class=doc]Standardization represents the complete body of information and controls that serve to enhance the batch to batch consistency of a botanical product, including but not limited to the presence of a marker compound at a defined level or within a defined range.[/span]

The most current available medical and scientific literature indicates that this dietary supplement should be standardized to 10% alkaloids or 2.5% berberine and 1.5-5% hydrastine per dose.

Uses

Frequently Reported Uses

  • Bronchitis
  • Inflammation Of The GI Tract And Mucous Membranes
  • Urethritis
  • Antiviral.
  • Colds
Other Reported Uses
  • Antibacterial
  • Antifungal
  • Antiparasitic
  • Cystitis
  • Eye Inflammation
  • Hepatobiliary Disorders
  • Muscular Stimulant
  • Postpartum Hemorrhage

Toxicities & Precautions

General

The isoquinoline alkaloid, berberine, is contained in goldenseal and is responsible for some of the pharmacological activity. Due to varying and unknown amounts of berberine in goldenseal, excessive use of this supplement should be avoided. (3) Significantly, goldenseal plays a role in the inhibition of enzymes responsible for the metabolism of xenobiotics in the liver. Due to that, patients are contraindicated in taking goldenseal if they are consuming medication that affects the CYP2D6, including beta blockers, SSRI antidepressants, opioid analgesics and antipsychotic drugs. (30)

Health Conditions

The berberine contained in goldenseal possesses inotropic, chronotropic, antiarrhythmic, and vasodilator properties. (4) Patients with various cardiovascular conditions including congestive heart failure, arrhythmias, and hypertension should not use berberine containing products unless closely monitored by a health care professional.

Berberine also has the ability to displace bilirubin, (5) , (6) therefore use berberine with caution in jaundice individuals, especially neonates.

Side Effects

Dosages of 2-3gm may lower heart rate and, at higher doses, may cause central nervous system paralysis. (7)

A published review of berberine literature notes the following side effects: decrease in blood pressure, dyspnea, flu-like symptoms, gastrointestinal upset and possible cardiac damage. (8)

Pregnancy/ Breast Feeding

Based on animal data, avoid use in pregnancy. (9) Also, due to berberine's ability to displace bilirubin, (10) , (11) as well as the traditional use of berberine as a uterine stimulant, (12) berberine and berberine containing products should not be used while pregnant or breast-feeding.

Age Limitations

Due to berberine's ability to displace bilirubin, (13) , (14) berberine and berberine containing products should not be used in newborns, especially jaundiced newborns.

Pharmacology

The alkaloids in goldenseal have an astringent activity, which contributes to their anti-inflammatory activity on mucous membranes. (15) Hydrastine has been reported to have antitussive, antiperistaltic, and some blood pressure lowering effects. (16) Berberine has been used in upper respiratory infections and inflammation of the mucous membranes. Berberine stimulates the production of bile, (17) as well as having an associated antibiotic effect on a broad array of pathogens. (18) Berberine is claimed to increase blood flow to the spleen, which could have positive benefits for immune function. Berberine has been reported to possess anti-pyretic effects in rats. (19) , (20) Goldenseal has been studied in infectious diarrhea and other GI infections, (21) as well as against such organisms as Shigella dysenteriae, Salmonella paratyphi, Giardia lamblia, and Entamoeba histolytica. (22) It is believed that goldenseal may actually reduce the adhesive ability of streptococci to host tissues. (23)

Recent literature has reported that berberine may decrease the responsiveness of certain cancer cell lines to the chemotherapeutic drug paclitaxel. (24) Pretreatment of cells with berberine prior to paclitaxel blocked the paclitaxel-induced cell cycle responses and morphological changes. These results together suggest that berberine may modulate the expression and function of pgp-170 that leads to reduced response to paclitaxel in digestive track cancer cells.

There has been controversy regarding the absorption of goldenseal in vivo. However, the active constituent berberine was reported to be highly detectable in plasma and urine following in vitro testing by HPLC analysis. (25) Also, there has been centuries of traditional use of goldenseal as an effective antibacterial agent, which suggests that although absorption may vary in individuals, therapeutic efficacy still exists.

References

  1. Kowalewski Z, et al. Toxicity of Berberine Sulfate. Acta Pol Pharm. 1975;32(1):113-20.
  2. View Abstract: Berberine. Altern Med Rev. Apr2000;5(2):175-7.
  3. Newall CA, Anderson LA, Phillipson JD. Herbal Medicines; A Guide for Health-Care Professionals. London:The Pharmaceutical Press;1996.
  4. View Abstract: Lau CW, Yao XQ, Chen ZY, Ko WH, Huang Y. Cardiovascular actions of berberine. Cardiovasc Drug Rev. Sep2001;19(3):234-44.
  5. View Abstract: Chan E. Displacement of bilirubin from albumin by berberine. Biol Neonate. 1993;63(4):201-8.
  6. View Abstract: Chan MY. The effect of berberine on bilirubin excretion in the rat. Comp Med East West. Jun1977;5(2):161-8.
  7. Hardin JW, et al. Human Poisoning from Native and Cultivated Plants. 2nd ed. Durham, NC: Duke University Press; 1974:56-57.
  8. Birdsall TC, Kelly GS. Berberine: Therapeutic potential of an alkaloid in several medicinal plants. Altern Med Review. 1997;2(2):94-103.
  9. DeSmet P, et al. Adverse Effects of Herbal Drugs I. Berlin: Springer-Verlag; 1992:97-104.
  10. View Abstract: Chan E. Displacement of bilirubin from albumin by berberine. Biol Neonate. 1993;63(4):201-8.
  11. View Abstract: Chan MY. The effect of berberine on bilirubin excretion in the rat. Comp Med East West. Jun1977;5(2):161-8.
  12. Birdsall TC, Kelly GS. Berberine: Therapeutic potential of an alkaloid in several medicinal plants. Altern Med Review. 1997;2(2):94-103.
  13. View Abstract: Chan E. Displacement of bilirubin from albumin by berberine. Biol Neonate. 1993;63(4):201-8.
  14. View Abstract: Chan MY. The effect of berberine on bilirubin excretion in the rat. Comp Med East West. Jun1977;5(2):161-8.
  15. View Abstract: Zhang MF, et al. Antidiarrheal and Anti-inflammatory Effects of Berberine. Chung Kuo Yao Li Hsueh Pao. 1989;10(2):174-76.
  16. Sabir M, et al. Study of Some Pharmacological Actions of Berberine. Indian J Physiol Pharmacol. 1971;15(3):111-32.
  17. Newall CA, et al. Herbal Medicines: A Guide for Health Care Professionals. London: The Pharmaceutical Press; 1996:151-52.
  18. Amin AH, et al. Berberine Sulfate: Antimicrobial Activity, Bioassay, and Mode of Action. Can J Micro. 1969;15:1067-76.
  19. Sabir M, Akhter MH, Bhide NK. Further studies on pharmacology of berberine. Indian J Physiol Pharmacol 1978;22:9-23.
  20. Sabir M, et al. Study of Some Pharmacological Actions of Berberine. Indian J Physiol Pharmacol. 1971;15(3):111-32.
  21. View Abstract: Rabbani GH, et al. Randomized Controlled Trial of Berberine Sulfate Therapy for Diarrhea Due to Enterotoxigenic Escherichia coli and Vibrio cholerae. The Journal of Infectious Diseases. 1987;155(5):979-84.
  22. Amin AH, et al. Berberine Sulfate: Antimicrobial Activity, Bioassay, and Mode of Action. Can J Micro. 1969;15:1067-76.
  23. View Abstract: Berberine. Altern Med Rev. Apr2000;5(2):175-7.
  24. View Abstract: Lin HL, et al. Berberine Modulates Expression of Mdr1 Gene Product and The Responses of Digestive Track Cancer Cells to Paclitaxel. Br J Cancer. Oct1999;81(3):416-22.
  25. View Abstract: Chen CM, et al. Determination of Berberine in Plasma, Urine and Bile by High-Performance Liquid Chromatography. J Chromatogr B Biomed Appl. Mar1995;665(1):117-23.
  26. Chignell CF, et al. Photochemistry and Photocytotoxicity of Alkaloids from Goldenseal (Hydrastis canadensis L.) 3. Effect on Human Lens Retinal Pigment Epithelial Cells. Photochem Photobiol. 2007 ; 83(4): 938–943.
  27. Brown PN. and Roman MC. Determination of Hydrastine and Berberine in Goldenseal Raw Materials, Extracts, and Dietary Supplements by High-Performance Liquid Chromatography with UV: Collaborative StudyJ AOAC Int. 2008 ; 91(4): 694–701.
  28. Brown PN. and Roman MC. Determination of Hydrastine and Berberine in Goldenseal Raw Materials, Extracts, and Dietary Supplements by High-Performance Liquid Chromatography with UV: Collaborative StudyJ AOAC Int. 2008 ; 91(4): 694–701.
  29. He S, et al. Plant regeneration of an endangered medicinal plant Hydrastis canadensis L. Scientia Horticulturae 2007 (113): 82–86
  30. Gurley BJ, et al. Clinical assessment of CYP2D6-mediated herb-drug interactions in humans: Effects of milk thistle, black cohosh, goldenseal, kava kava, St. John's wort, and Echinacea. Mol Nutr Food Res. 2008 July; 52(7): 755–763.