Goldenseal (Hydrastis Canadensis L.), Berberine
  
Goldenseal (Hydrastis Canadensis L.), Berberine
Background
Goldenseal is one of the five top-selling herbal products in the United States. However, there is little scientific evidence about its safety or effectiveness. Goldenseal can be found in dietary supplements, eardrops, feminine cleansing products, cold/flu remedies, allergy remedies, laxatives, and digestive aids.
Goldenseal is often found in combination with echinacea in treatments for upper respiratory infections, and is suggested to enhance the effects of echinacea. However, the effects when these agents are combined are not scientifically proven.
Goldenseal has been used by some people due to the popular notion that detection of illegal drugs in urine may be hidden by use of the herb, although scientific information is limited in this area.
The popularity of goldenseal has led to a higher demand for the herb than growers can supply. This high demand has led to the substitution of other isoquinoline alkaloid-containing herbs, such as Chinese goldthread ( Coptis chinensis Fransch.) and Oregon grape ( Mahonia aquifolium [Pursh] Nutt.), that do not contain exactly the same isoquinoline alkaloids, and may not affect the body in the same way as goldenseal.
Studies of the effectiveness of goldenseal are limited to one of its main chemical ingredients, berberine salts (there are few published human studies of goldenseal itself). Due to the small amount of berberine actually present in most goldenseal preparations (0.5-6%), it is difficult to extend the research of berberine salts to the use of goldenseal. Therefore, there is not enough scientific evidence to support the use of goldenseal in humans for any medical condition.
Synonyms
Berberine bisulfate, curcuma, eye balm, eye root, golden root, goldensiegel, goldsiegel, ground raspberry, guldsegl, hydrastidis rhizoma, hydrophyllum, Indian dye, Indian paint, Indian plant, Indian turmeric, jaundice root, kanadische gelbwurzel, kurkuma, Ohio curcuma, orange root, tumeric root, warnera, wild curcuma, wild turmeric, yellow eye, yellow Indian plant, yellow paint, yellow paint root, yellow puccoon, yellow root, yellow seal, yellow wort.
Note : Goldenseal is sometimes referred to as "Indian turmeric" or "curcuma," but should not be confused with turmeric ( Curcuma longa Linn.).
Evidence
These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider.
Uses based on scientific evidenceGrade*Chloroquine-resistant malaria
A small amount of research reports that berberine, a chemical found in goldenseal, may be beneficial in the treatment of chloroquine-resistant malaria when used in combination with pyrimethamine. Due to the very small amount of berberine found in most goldenseal preparations, it is unclear whether goldenseal contains enough berberine to have these effects. In addition, the available studies have not been well designed. More research is needed before a recommendation can be made.
C
Immune system stimulation
Goldenseal is sometimes suggested to be an immune system stimulant. However, there is little human or laboratory evidence in this area. More research is needed before a firm conclusion can be drawn.
C
Infectious diarrhea
In several animal and small human studies, berberine has been used as a treatment for diarrhea caused by bacterial infections (including diarrhea from cholera). However, most of this research has not been well designed, and results have been unclear. Due to the very small amount of berberine in most goldenseal products, it is unclear whether goldenseal contains enough berberine to have the same effects. Therefore, there is currently not enough scientific evidence to make a recommendation in this area.
C
Narcotic concealment (urine analysis)
It has been suggested that taking goldenseal can hide the presence of illegal drugs from urine tests. However, there is limited research to support this idea. One study from the National Institute on Drug Abuse, National Institutes of Health, looked at marijuana and cocaine use, and suggested that goldenseal probably does not have this effect.
C
Trachoma (Chlamydia trachomatosis eye infection)
Animal and laboratory research suggests that the goldenseal component berberine has effects against bacteria and inflammation. Several poorly designed human studies report benefits of berberine used in the eye to treat trachoma. Better research is needed before a recommendation can be made.
C
Common cold / upper respiratory tract infection
Goldenseal has become a popular treatment for the common cold and upper respiratory tract infections, and is often added to echinacea in commercial herbal cold remedies. Animal and laboratory research suggests that the goldenseal component berberine has effects against bacteria and inflammation. However, due to the very small amount of berberine in most goldenseal preparations, it is unclear whether goldenseal contains enough berberine to have the same effects. Currently, there are no reliable human studies of goldenseal or berberine in the treatment of respiratory tract infections.
C
Heart failure
One study suggests that berberine in addition to a standard prescription drug regimen for chronic congestive heart failure (CHF) may improve quality of life, and decrease ventricular premature complexes (VPCs) and mortality. Further research is needed to confirm these results.
C
* Key to grades
A: Strong scientific evidence for this use;
B: Good scientific evidence for this use;
C: Unclear scientific evidence for this use;
D: Fair scientific evidence against this use (it may not work);
F: Strong scientific evidence against this use (it likely does not work).
Uses based on tradition or theory
The below uses are based on tradition or scientific theories. They often have not been thoroughly tested in humans, and safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider.
Abnormal heart rhythms, acne, AIDS, alcoholic liver disease, anal fissures, anesthetic, antibacterial, anticoagulant (blood "thinning"), antifungal, anti-heparin, antihistamine, anti-inflammatory, astrocytoma, atherosclerosis ("hardening" of the arteries), anxiety, appetite stimulant, arthritis, asthma, athlete's foot, bile flow stimulant, blood circulation stimulant, boils, bronchitis, cancer, candida yeast infections, canker sores, cervicitis, chicken pox, chronic fatigue syndrome, colitis (intestinal inflammation), conjunctivitis, constipation, Crohn's disease, croup, cystic fibrosis, cystitis, dandruff, deafness, diabetes mellitus, diarrhea, digestion problems, diphtheria, diuretic (increasing urine flow), eczema, enhancement of insulin effects, eyewash, fever, fistula problems, flatulence (gas), gallstones, gangrene, gastroenteritis, genital disorders, giardia infection, gingivitis, glioblastoma, headache, infection, , hemorrhage (bleeding), hemorrhoids, hepatitis, herpes, hiatal hernia, high blood pressure, high cholesterol, high tyramine levels, hypoglycemia (low blood sugar levels), impetigo, inducing (causing) abortion, indigestion, infections, influenza, itching, jaundice, keratitis (inflammation of the cornea of the eye), leishmaniasis, liver disorders, lupus, menstruation problems, morning sickness, mouthwash, muscle pain, muscle spasm, night sweats, obesity, osteoporosis, otorrhea (fluid from the ear), pain, pneumonia, premenstrual syndrome, prostatitis, psoriasis, sciatica, seborrhea, sedative, sinusitis, stomach ulcers, stimulant, strep throat, syphilis, tetanus, thrombocytopenia (low blood platelets), thrush, tinnitis (ringing in the ears), tonsillitis, tooth disease, trichomoniasis, tuberculosis, urinary tract disorders, uterus inflammation, uterus stimulant, vaginal irritation, varicose veins.
Dosing
The below doses are based on scientific research, publications, traditional use, or expert opinion. Many herbs and supplements have not been thoroughly tested, and safety and effectiveness may not be proven. Brands may be made differently, with variable ingredients, even within the same brand. The below doses may not apply to all products. You should read product labels, and discuss doses with a qualified healthcare provider before starting therapy.
Standardization
Standardization involves measuring the amount of certain chemicals in products to try to make different preparations similar to each other. It is not always known if the chemicals being measured are the "active" ingredients. An analysis of several goldenseal products found large differences in the amounts of chemicals thought to be active (berberine and hydrastine). Some sources note standardization of goldenseal to isoquinoline alkaloids (5% to 10% total alkaloids, including hydrastine, berberine, and canadine).
Adults (18 years and older)
Goldenseal dosing : For general use, various types of goldenseal dosing have been used, each taken by mouth three times daily, including 0.5 to 1 gram tablets or capsules, 0.3 to 1 milliliter of liquid/fluid extract (1:1 in 60% ethanol), 0.5 to 1 gram as a decoction, or 2 to 4 milliliters as a tincture (1:10 in 60% ethanol).
Berberine dosing : For infectious diarrhea, 100 to 200 milligrams of berberine hydrochloride taken by mouth four times daily, or a single dose of 400 milligrams taken by mouth has been studied. Berberine sulfate is often used as well, and the hydrochloride and sulfate forms are generally thought to be equivalent.
Children (younger than 18 years)
There is not enough scientific evidence to safely recommend the use of goldenseal in children. Doses of 25 to 50 milligrams of berberine four times daily have been studied in children for the management of diarrhea, although safety has not been established.
Safety
The U.S. Food and Drug Administration does not strictly regulate herbs and supplements. There is no guarantee of strength, purity or safety of products, and effects may vary. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy. Consult a healthcare provider immediately if you experience side effects.
Allergies
Goldenseal should be avoided by people with known allergy/hypersensitivity to goldenseal or any of its constituents, including berberine and hydrastine.
Side Effects and Warnings
Goldenseal is rarely reported to cause nausea, vomiting, breathing failure or a feeling of numbness in the arms or legs. Large doses of goldenseal may cause mucus membrane irritation and worsening or stomach ulcers. Goldenseal used on the skin may cause irritation or ulcers.
Possible effects of berberine, a chemical found in small amounts in goldenseal, include headache, slow heart rate, nausea, vomiting, abdominal bloating, and low white blood cell count. It is not clear if the amount of berberine in goldenseal products is enough to cause these reactions. Toxic doses of berberine may cause seizures or irritation of the esophagus and stomach when taken by mouth. Berberine used intravenously (through the veins) may cause abnormal heart rhythms. Based on laboratory and animal studies, berberine may increase blood concentrations of bilirubin. Berberine theoretically may cause low blood pressure, although a different chemical in goldenseal, hydrastine, may actually cause increased blood pressure. There is limited study of the blood pressure effects of these agents in humans.
Based on laboratory and animal studies, the use of goldenseal or berberine could increase the risk of bleeding. However, there are no reliable published reports of bleeding in humans. Caution is advised in patients with bleeding disorders or taking drugs that may increase the risk of bleeding. Dosing adjustments may be necessary.
Based on laboratory study, goldenseal and berberine may cause increased sun sensitivity.
Based on laboratory studies, berberine may lower blood sugar. Caution is advised in patients with diabetes or hypoglycemia, and in those taking drugs, herbs, or supplements that affect blood sugar. Serum glucose levels may need to be monitored by a healthcare provider, and medication adjustments may be necessary.
The popularity of goldenseal has led to the substitution of other alkaloid-containing herbs, including Chinese goldthread ( Coptis chinensis ) and Oregon grape, that do not contain the same active components and may increase the risk of serious toxicity or adverse events.
Pregnancy and Breastfeeding
Use of goldenseal or berberine is not recommended during pregnancy or breastfeeding. The chemical hydrastine (found in goldenseal) may induce labor when taken by mouth during pregnancy, and could have dangerous effects.
References
1. Budzinski JW, Foster BC, Vandenhoek S, Arnason JT. An in vitro evaluation of human cytochrome P450 3A4 inhibition by selected commercial herbal extracts and tinctures. Phytomedicine 2000;7(4):273-282.
2. Cone EJ, Lange R, Darwin WD. In vivo adulteration: excess fluid ingestion causes false-negative marijuana and cocaine urine test results. J Anal Toxicol 1998;22(6):460-473.
3. Foster BC, Vandenhoek S, Hana J, et al. In vitro inhibition of human cytochrome P450-mediated metabolism of marker substrates by natural products. Phytomedicine 2003;10(4):334-342.
4. Govindan M, Govindan G. A convenient method for the determination of the quality of goldenseal. Fitoterapia 2000;71(3):232-235.
5. Inbaraj JJ, Kukielczak BM, Bilski P, et al. Photochemistry and photocytotoxicity of alkaloids from Goldenseal (Hydrastis canadensis L.) 1. Berberine. Chem Res Toxicol 2001;14 (11) :1529-1534.
6. Khin MU, Myo K, Nyunt NW, et al. Clinical trial of berberine in acute watery diarrhoea. Br Med J (Clin Res Ed) 1985;291(6509):1601-1605.
7. Khin-Maung U, Myo-Khin, Nyunt-Nyunt-Wai, et al. Clinical trial of high-dose berberine and tetracycline in cholera. J Diarrhoeal Dis Res 1987;5(3):184-187.
8. Lahiri S, Dutta NK. Berberine and chloramphenicol in the treatment of cholera and severe diarrhoea. J Indian Med Assoc 1967;48(1):1-11.
9. Maeng HJ, Yoo HJ, Kim IW, et al. P-glycoprotein-mediated transport of berberine across Caco-2 cell monolayers. J Pharm Sci 2002;91(12):2614-2621.
10. Mahady GB, Pendland SL, Stoia A, et al. In vitro susceptibility of Helicobacter pylori to isoquinoline alkaloids from Sanguinaria canadensis and Hydrastis canadensis. Phytother Res 2003;17(3):217-221.
11. Pan GY, Huang ZJ, Wang GJ, et al. The antihyperglycaemic activity of berberine arises from a decrease of glucose absorption. Planta Med 2003;69(7):632-636.
12. Pan GY, Wang GJ, Liu XD, Fawcett JP, Xie YY. The involvement of P-glycoprotein in berberine absorption. Pharmacol Toxicol. 2002;91(4):193-197.
13. Pan JF, Yu C, Zhu DY, et al. Identification of three sulfate-conjugated metabolites of berberine chloride in healthy volunteers' urine after oral administration. Acta Pharmacol Sin 2002;23(1):77-82.
14. Rabbani GH, Butler T, Knight J, et al. Randomized controlled trial of berberine sulfate therapy for diarrhea due to enterotoxigenic Escherichia coli and Vibrio cholerae. J Infect Dis 1987;155(5):979-984.
15. Sheng WD, Jiddawi MS, Hong XQ, et al. Treatment of chloroquine-resistant malaria using pyrimethamine in combination with berberine, tetracycline or cotrimoxazole. East African Med J 1997;74(5):283-284.
16. Wang DY, Yeh CC, Lee JH, et al. Berberine inhibited arylamine N-acetyltransferase activity and gene expression and DNA adduct formation in human malignant astrocytoma (G9T/VGH) and brain glioblastoma multiforms (GBM 8401) cells. Neurochem Res 2002;27(9):883-889.
17. Yin, J, Hu R, Chen M, Tang J, et al. Effects of berberine on glucose metabolism in vitro. Metabolism 2002; 51(11):1439-1543.
18. Zeng XH, Zeng XJ, Li YY. Efficacy and safety of berberine for congestive heart failure secondary to ischemic or idiopathic dilated cardiomyopathy. Am J Cardiol 2003;92(2):173-176.
January 01, 2004 
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