Health Care Professional Information
Common Name
Eye root, yellow Indian plant, turmeric root, yellow paint root, orange root, goldenroot
Clinical Summary
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.
Purported Uses
- Anorexia
- Cancer treatment
- Cirrhosis
- Colitis
- Common cold
- Conjunctivitis
- Diabetes
- Edema
- Fever
- Infections
- Menorrhagia
Constituents
- Alkaloids: Hydrastine (1.5-4%), berberine (0.5- 6%), canadine, beta-hydrastine, canadaline
(23) (24)
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).
Warnings
Berberine-containing botanicals may cause QTc prolongation in patients with severe underlying heart disease.
Adverse Reactions
- 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).
Herb-Drug Interactions
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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References
- 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.
Consumer Information
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.
Purported Uses
- 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.
Patient Warnings
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).
Side Effects
- 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
animal study (A-nih-mul STUH-dee)
A laboratory experiment using animals to study the development and progression of diseases. Animal studies also test how safe and effective new treatments are before they are tested in people.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
antibacterial (AN-tee-bak-TEER-ee-ul)
A substance that kills bacteria or stops them from growing and causing disease.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
antifungal (AN-tee-FUN-gul)
A drug that treats infections caused by fungi.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
antimicrobial (AN-tee-my-KROH-bee-ul)
A substance that kills microorganisms such as bacteria or mold, or stops them from growing and causing disease.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
apoptosis (A-pop-TOH-sis)
A type of cell death in which a series of molecular steps in a cell leads to its death. This is the body’s normal way of getting rid of unneeded or abnormal cells. The process of apoptosis may be blocked in cancer cells. Also called programmed cell death.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
ARMS
A soft tissue tumor that is most common in older children and teenagers. It begins in embryonic muscle cells (cells that develop into muscles in the body). It can occur at many places in the body, but usually occurs in the trunk, arms, or legs. Also called alveolar rhabdomyosarcoma.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
bacteria (bak-TEER-ee-uh)
A large group of single-cell microorganisms. Some cause infections and disease in animals and humans. The singular of bacteria is bacterium.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
blood (blud)
A tissue with red blood cells, white blood cells, platelets, and other substances suspended in fluid called plasma. Blood takes oxygen and nutrients to the tissues, and carries away wastes.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
blood pressure (blud PREH-sher)
The force of circulating blood on the walls of the arteries. Blood pressure is taken using two measurements: systolic (measured when the heart beats, when blood pressure is at its highest) and diastolic (measured between heart beats, when blood pressure is at its lowest). Blood pressure is written with the systolic blood pressure first, followed by the diastolic blood pressure (for example 120/80).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
brain tumor (brayn TOO-mer)
The growth of abnormal cells in the tissues of the brain. Brain tumors can be benign (not cancer) or malignant (cancer).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
breast (brest)
Glandular organ located on the chest. The breast is made up of connective tissue, fat, and breast tissue that contains the glands that can make milk. Also called mammary gland.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
cancer (KAN-ser)
A term for diseases in which abnormal cells divide without control and can invade nearby tissues. Cancer cells can also spread to other parts of the body through the blood and lymph systems. There are several main types of cancer. Carcinoma is a cancer that begins in the skin or in tissues that line or cover internal organs. Sarcoma is a cancer that begins in bone, cartilage, fat, muscle, blood vessels, or other connective or supportive tissue. Leukemia is a cancer that starts in blood-forming tissue such as the bone marrow, and causes large numbers of abnormal blood cells to be produced and enter the blood. Lymphoma and multiple myeloma are cancers that begin in the cells of the immune system. Central nervous system cancers are cancers that begin in the tissues of the brain and spinal cord. Also called malignancy.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
cell (sel)
The individual unit that makes up the tissues of the body. All living things are made up of one or more cells.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
clinical (KLIH-nih-kul)
Having to do with the examination and treatment of patients.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
compound (KOM-pownd)
In science, a substance that is made up of more than one ingredient.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
dietary supplement (DY-uh-TAYR-ee SUH-pleh-ment)
A product that is added to the diet. A dietary supplement is taken by mouth, and usually contains one or more dietary ingredient (such as vitamin, mineral, herb, amino acid, and enzyme). Also called nutritional supplement.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
dose (dose)
The amount of medicine taken, or radiation given, at one time.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
doxorubicin (DOK-soh-ROO-bih-sin)
A drug that is used to treat many types of cancer and is being studied in the treatment of other types of cancer. Doxorubicin comes from the bacterium . It damages DNA and may kill cancer cells. It is a type of anthracycline antitumor antibiotic. Also called Adriamycin PFS, Adriamycin RDF, doxorubicin hydrochloride, hydroxydaunorubicin, and Rubex.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
drug (drug)
Any substance, other than food, that is used to prevent, diagnose, treat or relieve symptoms of a disease or abnormal condition. Also refers to a substance that alters mood or body function, or that can be habit-forming or addictive, especially a narcotic.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
electrocardiogram (ee-LEK-troh-KAR-dee-oh-gram)
A line graph that shows changes in the electrical activity of the heart over time. It is made by an instrument called an electrocardiograph. The graph can show that there are abnormal conditions, such as blocked arteries, changes in electrolytes (particles with electrical charges), and changes in the way electrical currents pass through the heart tissue. Also called ECG and EKG.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
extract (EK-strakt)
In medicine, a preparation of a substance obtained from plants, animals, or bacteria and used as a drug or in drugs.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
gastrointestinal (GAS-troh-in-TES-tih-nul)
Refers to the stomach and intestines. Also called GI.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
ginseng (JIN-seng)
An herb with a root that has been used in some cultures to treat certain medical problems. It may have anticancer effects.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
in vitro (in VEE-troh)
In the laboratory (outside the body). The opposite of in vivo (in the body).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
in vivo (in VEE-voh)
In the body. The opposite of in vitro (outside the body or in the laboratory).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
inflammation (IN-fluh-MAY-shun)
Redness, swelling, pain, and/or a feeling of heat in an area of the body. This is a protective reaction to injury, disease, or irritation of the tissues.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
L
A measure of volume for a liquid, using the metric system. One L is equal to 1,000 cubic centimeters (cc), 1,000 milliliters (mm), or 1.0567 quarts (qt). Also called liter.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
liver (LIH-ver)
A large organ located in the upper abdomen. The liver cleanses the blood and aids in digestion by secreting bile.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
malignant (muh-LIG-nunt)
Cancerous. Malignant cells can invade and destroy nearby tissue and spread to other parts of the body.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
tumor (TOO-mer)
An abnormal mass of tissue that results when cells divide more than they should or do not die when they should. Tumors may be benign (not cancer), or malignant (cancer). Also called neoplasm.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
urine (YOOR-in)
Fluid containing water and waste products. Urine is made by the kidneys, stored in the bladder, and leaves the body through the urethra.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
uterus (YOO-teh-rus)
The small, hollow, pear-shaped organ in a woman's pelvis. This is the organ in which a fetus develops. Also called womb.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)