Health Care Professional Information
Eye root, yellow Indian plant, turmeric root, yellow paint root, orange root, goldenroot
Derived from the root of the plant, goldenseal is used by patients to treat a variety of ailments including common cold, fever, infections, heart conditions, constipation, and muscle spasms. Primary active components are hydrastine, berberine, and canadine. Among several herbs tested in vitro, goldenseal extract was the most active in inhibiting the growth of H. pylori (1). Studies done on berberine indicate that it has antimicrobial property (3); and inhibits the growth and induces apoptosis in certain cancer cells (2) (4) (6). Clinical studies are lacking.
- Cancer treatment
- Common cold
- Alkaloids: Hydrastine (1.5-4%), berberine (0.5- 6%), canadine, beta-hydrastine, canadaline
Mechanism of Action
The pharmacological action of goldenseal is attributed to the compounds hydrastine and berberine. The majority of clinical studies were not performed with goldenseal, but rather on berberine and hydrastine. Berberine has anti-microbial activity against certain pathogens such enterotoxigenic E. coli and V. cholera. It also induces cell cycle arrest and apoptosis in a variety of cancer cell lines (2) (15) (16). One in vitro study found that berberine inhibited the growth of adherent and anoikis resistant MCF-7 and MDA-MB-231 breast cancer cells to a greater extent than doxorubicin (4). In one study, berberine alkaloids produced an average of 91% tumor inhibition against 6 malignant brain tumor cell lines both in vivo in mice and in vitro against human brain tumors (5). Berberine alkaloids were also shown to have potent macrophage-activating and cytostatic activity against tumor cells. Another study performed in vitro tests on a series of human malignant brain tumor cells and rat brain tumor cells (6). Berberine used alone at a dose of 150 mcg/ml had an average cancer cell kill rate of 91%. BCNU (carmustine) had a cell kill rate of 43%. Rats treated with berberine at 10 mg/kg had an 81% kill rate. The combination of both berberine and BCNU had additive effects in killing cancer cells. In an animal study, berberine has been shown to prolong QTc interval and to help prevent ventricular fibrillation after myocardial infarction (17). The hydrastine component induces constriction of peripheral blood vessels (13). While two small clinical trials reported that goldenseal affects CYP2D6 (18) and CYP3A (10), another could not confirm such effects (19).
Berberine-containing botanicals may cause QTc prolongation in patients with severe underlying heart disease.
- Photosensitivity was reported in a patient following use of a dietary supplement containing ginseng, goldenseal, bee pollen, and other ingredients (25).
- Rats and mice that were fed goldenseal root powder had an increase in liver tumors (26).
Cytochrome P450 substrates: Goldenseal inhibits CYP3A4 and CYP2D6 isoenzymes, and can affect the intracellular concentration of drugs metabolized by these enzymes (11) (18).
Herb Lab Interactions
Berberine may increase bilirubin levels due to displacement of bilirubin from albumin (21).
Goldenseal may cause a darkening in urine color in illicit drug testing (22).
Goldenseal may alter PT / PTT / INR anticoagulation test results (8).
May prolong QTc interval in electrocardiogram (17).
One case of hypernatremia was reported in a patient with diabetic ketoacidosis (13).
Dosage (Inside MSKCC Only)
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- Cwikla C, Schmidt K, Matthias A, et al. Investigations into the antibacterial activities of phytotherapeutics against Heliobacter pylori and Campylobacter jejuni. Phytotherapy Research. 2010;24:649-656.
- Mantena SK, Sharma SD, Katiyar SK. Berberine, a natural product, induces G1-phase cell cycle arrest and caspase-3-dependent apoptosis in human prostate carcinoma cells. Mol Cancer Ther. Feb 2006;5(2):296-308.
- Rabbani G, et al. Randomized controlled trial of berberine sulfate therapy for diarrhea due to enterotoxigenic Escherichia coli and vibrio cholerae. J Infect Dis 1987;155:979-84.
- Kim JB, Yu JH, Ko E, et al. The alkaloid Berberine inhibits the growth of Anoikis-resistant MCF-7 and MDA-MB-231 breast cancer cell lines by inducing cell cycle arrest. Phytomedicine. 2010 May;17(6):436-40.
- Werbach MR, et al. Botanical Influences on Illness: A Sourcebook of Clinical Research. Tarzana, California: Third Line Press; 1994.
- Zhang RX, et al. Laboratory studies of berberine use alone and in combination with 1,3-bis(2-chloroethyl)-1-nitrosourea to treat malignant brain tumors. Chin Med J 1990;103:658-65 PMID: 2122945
- Barnes J, Anderson LA, Phillipson JD. Herbal Medicines: A Guide for Health-Care Professionals. London: Pharmaceutical Press; 1996.
- Budzinski JW, et al. An in vitro evaluation of human cytochrome P450 3A4 inhibition by selected commercial herbal extracts and tinctures. Phytomedicine 2000;7:273-82.
- Chatterjee P,.Franklin MR. Human cytochrome p450 inhibition and metabolic-intermediate complex formation by goldenseal extract and its methylenedioxyphenyl components. Drug Metab Dispos. 2003;31:1391-7.
- Gurley BJ, Swain A, Hubbard MA, et al. Supplementation with goldenseal (Hydrastis canadensis), but not kava kava (Piper methysticum), inhibits human CYP3A activity in vivo. Clin Pharmacol Ther. Jan 2008;83(1):61-69.
- Gurley BJ, Gardner SF, Hubbard MA, et al. In vivo effects of goldenseal, kava kava, black cohosh, and valerian on human cytochrome P450 1A2, 2E1, and 3A4/5 phenotypes. Clin Pharmacol Ther 2005;77(5):415-26.
- Gurley BJ, Swain A, Barone GW, et al. Effect of goldenseal (Hydrastis canadensis) and kava kava (Piper methysticum) supplementation on digoxin pharmacokinetics in humans. Drug Metab Dispos 2007;35(2):240-5.
- Bhowmick SK, Hundley OT, Rettig KR. Severe hypernatremia and hyperosmolality exacerbated by an herbal preparation in a patient with diabetic ketoacidosis. Clin Pediatr (Phila). Nov 2007;46(9):831-834.
- Gruenwald J, Brendler T, Jaenicke C. PDR for Herbal medicines. 2nd ed. Montvale (NJ): Medical Economics Company; 1998.
- Jantova S, Cipak L, Letasiova S. Berberine induces apoptosis through a mitochondrial/caspase pathway in human promonocytic U937 cells. Toxicol In Vitro. Feb 2007;21(1):25-31.
- Serafim TL, Oliveira PJ, Sardao VA, Perkins E, Parke D, Holy J. Different concentrations of berberine result in distinct cellular localization patterns and cell cycle effects in a melanoma cell line. Cancer Chemother Pharmacol. May 2008;61(6):1007-1018.
- Xu Z, Cao HY, Li Q. [Protective effects of berberine on spontaneous ventricular fibrillation in dogs after myocardial infarction]. Zhongguo Yao Li Xue Bao. Jul 1989;10(4):320-324.
- Gurley BJ, Swain A, Hubbard MA, 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. Jul 2008;52(7):755-763.
- Sandhu RS, Prescilla RP, Simonelli TM, Edwards DJ. Influence of goldenseal root on the pharmacokinetics of indinavir. J Clin Pharmacol. 2003;43:1283-8.
- Wu X, Li Q, Xin H, Yu A, Zhong M. Effects of berberine on the blood concentration of cyclosporin A in renal transplanted recipients: clinical and pharmacokinetic study. Eur J Clin Pharmacol. Sep 2005;61(8):567-572.
- Chan E. Displacement of bilirubin from albumin by berberine. Biol Neonate. 1993;63(4):201-208.
- Mikkelsen SL, Ash KO. Adulterants causing false negatives in illicit drug testing. Clin Chem 1988; 34:2333-6.
- Abidi P, Chen W, Kraemer FB, Li H, Liu J. The medicinal plant goldenseal is a natural LDL-lowering agent with multiple bioactive components and new action mechanisms. J Lipid Res. 2006 Oct;47(10):2134-47.
- Chignell CF, Sik RH, Watson MA, Wielgus AR. Photochemistry and photocytotoxicity of alkaloids from Goldenseal (Hydrastis canadensis L.) 3: effect on human lens and retinal pigment epithelial cells. Photochem Photobiol. 2007 Jul-Aug;83(4):938-43.
- Palanisamy A, Haller C, Olson KR. Photosensitivity reaction in a woman using an herbal supplement containing ginseng, goldenseal, and bee pollen. J Toxicol Clin Toxicol. 2003;41(6):865-7.
- Dunnick JK, Singh B, Nyska A, et al. Investigating the potential for toxicity from long-term use of the herbal products, goldenseal and milk thistle. Toxicol Pathol. 2011 Feb;39(2):398-409.
How It Works
Bottom Line: Goldenseal has not been shown to treat or prevent cancer.
The two compounds in goldenseal, berberine and hydrastine, have been studied widely. In animal studies, berberine was found to lower fevers, kill bacteria, fungi and protozoa, and slow the growth of tumors. It also stimulated contractions of the uterus, increased blood flow to the heart, and blocked some molecules involved in inflammation. Hydrastine was found to constrict blood vessels in the arms and legs. Although an extract of goldenseal caused muscle relaxation in animal tissues, berberine and hydrastine are also known to simulate contraction of the smooth muscles of uterus.
- To control muscle spasms
Laboratory studies support this use, but human data are lacking.
- To treat cancer
Laboratory studies show that berberine, a compound in goldenseal, inhibits the growth of a variety of tumors in rats, but no clinical trials have been performed.
- To stimulate the heart and increase blood pressure
Laboratory studies show that berberine, a compound in goldenseal, stimulates the heart and increases blood flow to it, but results concerning blood pressure are mixed. Clinical trials that confirm this effect have not been conducted.
- To treat gastrointestinal disorders
Laboratory studies show that a goldenseal extract causes relaxation of smooth muscle like that found in the gastrointestinal tract, but it is not known if goldenseal helps treat gastrointestinal disorders.
- To treat conjunctivitis
Laboratory data shows that berberine, a compound in goldenseal, has antibacterial properties, but human data are lacking.
- To manage painful and heavy menstruation
Laboratory evidence regarding goldenseal's ability to relax uterus muscle is mixed. Clinical trials have not yet been conducted.
- To treat infections topically
Laboratory studies show that berberine, a compound in goldenseal, has wide antibacterial and antifungal properties, but no clinical trials have been performed to confirm that this effect occurs in humans.
- To reduce swelling and edema
Laboratory studies show that berberine, a compound in goldenseal, blocks some of the molecules involved in inflammation.
Berberine-containing botanicals may cause QTc prolongation in patients with severe underlying heart disease.
Do Not Take If
- You are taking drugs that are substrates of cytochromeP450 3A4 and 2D6enzymes: (Goldenseal may increase the risk of side effects of these drugs).
- Photosensitivity was reported in a patient following use of a dietary supplement containing ginseng, goldenseal, bee pollen, and other ingredients.
- Rats and mice that were fed goldenseal root powder had an increase in liver tumors.
Last updated: October 12, 2012