Health Care Professional Information
Common Name
Goldthread, Coptis chinese, Coptis deltoidea, Coptis teetoides
Clinical Summary
Derived from the root of the plant, huanglian is used in traditional Chinese medicine for gastrointestinal complaints, diarrhea, hypertension, bacterial and viral infections. Berberine and berberine-like alkaloids are thought responsible for its activity (1). Studies show that berberine has hepatoprotective (9), anti-inflammatory (14) effects, and improves glucose metabolism in diabetic rats (10).
Jatrorrhizine, a protoberberine, was shown to offset postoperative ileus-induced delayed gastric emptying, and intestinal transit in rats (15).
Berberine also inhibits the growth of hepatoma cancer cells (3); an aqueous extract of huanglian demonstrated potent antiangiogenesis activity in vitro (6). Preliminary data support the hypothesis that huanglian suppresses cyclin B1 protein and causes cell cycle arrest at G2 (5).
Purported Uses
- Diarrhea
- Ear infections
- Hypertension
- Microbial infection
- Respiratory infections
Constituents
- Berberine (7-9%), coptisine, urbenine, worenine, palmaline, jatrorrhizine, columbamine, epiberberine and groenlandicine
(2) (10) (12) (15)
Mechanism of Action
Berberine and berberine-like compounds in huanglian are thought responsible for its activity. Berberine inhibits human hep-62 hepatoma cell growth due to morphological changes and internucleosomal DNA fragmentation (3). Berberine interferes with the gastric peristalsis resulting in antidiarrheal activity, interferes with bacterial metabolism of carbohydrates, protein synthesis, and complex with nucleic acids resulting in growth inhibition. Hypotensive effects are thought to be mediated by muscarinic stimulation and inhibition of cholinesterase. In dogs berberine shows positive inotropic effects and lowers peripheral vascular resistance. Berberine also inhibits platelet aggregation and can antagonize thromboxane B2. Berberine can cause potassium channel blockade resulting in prolongation of the action potential in cat ventricular monocytes (1).
Huanglian inhibits topoisomerase I and is thought to suppress cyclin B1 protein and cause cancer cell arrest at G2 phase (2). It also has potent antiangiogenic activity (6), induces apoptosis and arrests cell growth by upregulating Interferon beta and tumor necrosis factor-alpha genes in breast cancer cells (7).
Contraindications
Huanglian displaces bilirubin and should not be administered to jaundiced neonates.
Berberine-containing botanicals may prolong QTc in patients with underlying heart disease.
(4)
Herb-Drug Interactions
- Cytochrome P450 substrates: Huanglian inhibits CYP2D6 (11)and can affect the intracellular concentration of drugs metabolized by this enzyme.
Prolonged use of berberine can also inhibit CYP2D6, 2C9, and CYP3A4 in humans (13). However, another study showed that huanglian can induce CYP3A4 by activating pregnane X receptor (12) .
Dosage (Inside MSKCC Only)
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References
- Huang KC. The Pharmacology of Chinese Herbs, 2nd ed. New York: CRC Press; 1999.
- Kobayashi Y, et al. Inhibitors of DNA topoisomerase I and II isolated from the Coptis rhizomes. Planta Med 1995;61:414-8.
- Lin HL, et al. Up-regulation of multidrug resistance transporter expression by berberine in human and murine hepatoma cells. Cancer 1999;85:1937-42.
- Brinker F. Herb Contraindications and Drug Interactions, 3rd ed. Sandy (OR): Eclectic Medical Publications; 2001.
- Li XK, et al. Huanglian, A Chinese herbal extract, inhibits cell growth by suppressing the expression of cyclin B1 and inhibiting CDC2 kinase activity in human cancer cells. Mol Pharmacol 2000;58:1287-93.
- Wang S, et al. Angiogenesis and anti-angiogenesis activity of Chinese medicinal herbal extracts. Life Sci. 2004 Apr 2;74(20):2467-78.
- Kang JX, Liu J, Wang J, et al. The extract of huanglian, a medicinal herb, induces cell growth arrest and apoptosis by upregulation of interferon-beta and TNF-alpha in human breast cancer cells. Carcinogenesis 2005;26(11):1934-9.
- Auyeung KK, Ko JK. Coptis chinensis inhibits hepatocellular carcinoma cell growth through nonsteroidal anti-inflammatory drug-activated gene activation. Int J Mol Med. 2009 Oct;24(4):571-7.
- Feng Y, Siu KY, Ye X, et al. Hepatoprotective effects of berberine on carbon tetrachloride-induced acute hepatotoxicity in rats. Chin Med. 2010 Sep 18;5:33.
- Xia X, Yan J, Shen Y, et al. Berberine improves glucose metabolism in diabetic rats by inhibition of hepatic gluconeogenesis. PLoS One. 2011 Feb 3;6(2):e16556.
- Han YL, Yu HL, Li D, et al. In Vitro Inhibition of Huanglian [Rhizoma coptidis (L.)] and its Six Active Alkaloids on Six Cytochrome P450 Isoforms in Human Liver Microsomes. Phytother Res. 2011 Mar 21. [Epub ahead of print]
- Yu C, Chai X, Yu L, Chen S, Zeng S. Identification of novel pregnane X receptor activators from traditional Chinese medicines. J Ethnopharmacol. 2011 Jun 14;136(1):137-43.
- Guo Y, Chen Y, Tan ZR, et al. Repeated administration of berberine inhibits cytochromes P450 in humans. Eur J Clin Pharmacol. 2012 Feb;68(2):213-7.
- Zhang Q, Piao XL, Piao XS, Lu T, Wang D, Kim SW. Preventive effect of Coptis chinensis and berberine on intestinal injury in rats challenged with lipopolysaccharides. Food Chem Toxicol. 2011 Jan;49(1):61-9.
- Zhang B, Cao A, Zhou J, Hu Z, Wu D.Effect of jatrorrhizine on delayed gastrointestinal transit in rat postoperative ileus. J Pharm Pharmacol. 2012 Mar;64(3):413-9.
Consumer Information
How It Works
Bottom Line: There are not enough data which show that huanglian can treat cancer, high blood pressure, infections, or any other medical condition.
Huanglian is a root extract that is used in traditional Chinese medicine. Laboratory experiments have been performed with huanglian to study its possible anticancer activity. A substance called berberine in huanglian has been found to slow the replication of liver cancer cells in the laboratory by interfering with the mechanisms of cell division. Berberine also halts the growth of bacteria by interfering with their metabolism. Scientists think that berberine may have antidiarrheal activity due to its ability to slow down intestinal peristalsis (motion), but they are unsure exactly how this effect happens. The ability of berberine to lower blood pressure is attributed to its effects in the body that resemble parasympathetic nervous system stimulation (e.g., impulses to “rest and digest” rather than “fight or flight”). Human studies are needed.
Purported Uses
- To treat bacterial and viral infections
Laboratory studies show that berberine, a compound in huanglian, stops the growth of bacteria. Human data are lacking.
- To treat diarrhea and other gastrointestinal symptoms
Laboratory studies support this use, but it has not been studied in clinical trials.
- To lower high blood pressure
Laboratory and animal studies support this use, but human data are needed.
Do Not Take If
- You are taking antihypertensive medications (for high blood pressure) (In theory, huanglian may lower your blood pressure even further. Use with caution).
- You have severe underlying heart disease (Botanicals that contain berberine, such as huanglian, may cause QTc prolongation).
- Huanglian displaces bilirubin and should not be administered to jaundiced neonates.
- You are taking drugs that are substrates of Cytochrome P450 (Huanglian may increase the risk of side effects of these drugs). However, another study showed that huanglian can induce CYP3A4 by activating pregnane X receptor. This may decrease the concentration of drugs metabolized by CYP3A4.
Side Effects
- Nausea
- Vomiting
- Shortness of breath
- Toxicity from high doses of huanglian can cause seizures, liver toxicity, and cardiac toxicity.
Last updated: October 29, 2012
anti-inflammatory (AN-tee-in-FLA-muh-TOR-ee)
Having to do with reducing inflammation.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)antiangiogenesis (AN-tee-AN-jee-oh-JEH-neh-sis)
Prevention of the growth of new blood vessels.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)antiangiogenic (AN-tee-AN-jee-oh-JEH-nik)
Having to do with reducing the growth of new blood vessels.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)antidiarrheal (AN-tee-dy-uh-REE-ul)
A substance used to treat diarrhea (frequent and watery bowel movements).
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)aqueous (A-kwee-us)
Having to do with water.
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)bilirubin (BIH-lih-ROO-bin)
Substance formed when red blood cells are broken down. Bilirubin is part of the bile, which is made in the liver and is stored in the gallbladder. The abnormal buildup of bilirubin causes jaundice.
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)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)cardiac (KAR-dee-ak)
Having to do with the heart.
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)concentration (KON-sen-TRAY-shun)
In science, the amount of a substance, such as a salt, that is in a certain amount of tissue or liquid, such as blood. A substance becomes more concentrated when less water is present. For example, the salt in urine may become more concentrated when a person doesn’t drink enough water.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)DNA
The molecules inside cells that carry genetic information and pass it from one generation to the next. Also called deoxyribonucleic acid.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)enzyme (EN-zime)
A protein that speeds up chemical reactions in the body.
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)gastric (GAS-trik)
Having to do with the stomach.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)glucose (GLOO-kose)
A type of sugar; the chief source of energy for living organisms.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)hepatoma (HEH-puh-TOH-muh)
A liver tumor.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)hypothesis (hy-PAH-theh-sis)
A tentative proposal made to explain certain observations or facts that requires further investigation to be verified.
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)interferon (in-ter-FEER-on)
A biological response modifier (a substance that can improve the body's natural response to infections and other diseases). Interferons interfere with the division of cancer cells and can slow tumor growth. There are several types of interferons, including interferon-alpha, -beta, and -gamma. The body normally produces these substances. They are also made in the laboratory to treat cancer and other diseases.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)intestinal (in-TES-tih-nul)
Having to do with the intestines.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)intracellular (IN-truh-SEL-yoo-ler)
Inside a cell.
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)medicine (MEH-dih-sin)
Refers to the practices and procedures used for the prevention, treatment, or relief of symptoms of a diseases or abnormal conditions. This term may also refer to a legal drug used for the same purpose.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)metabolism (meh-TA-buh-lih-zum)
The chemical changes that take place in a cell or an organism. These changes make energy and the materials cells and organisms need to grow, reproduce, and stay healthy. Metabolism also helps get rid of toxic substances.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)necrosis (neh-KROH-sis)
Refers to the death of living tissues.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)nervous system (NER-vus SIS-tem)
The organized network of nerve tissue in the body. It includes the central nervous system (the brain and spinal cord), the peripheral nervous system (nerves that extend from the spinal cord to the rest of the body), and other nerve tissue.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)peristalsis (payr-ih-STAL-sis)
The rippling motion of muscles in the intestine or other tubular organs characterized by the alternate contraction and relaxation of the muscles that propel the contents onward.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)pharmacology (FAR-muh-KAH-loh-jee)
The study of the origin, chemistry, and uses of drugs and their effects on the body.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)platelet (PLAYT-let)
A tiny piece of a cell found in the blood that breaks off from a large cell found in the bone marrow. Platelets help wounds heal and prevent bleeding by forming blood clots. Also called thrombocyte.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)postoperative (post-AH-pruh-tiv)
After surgery.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)potassium (puh-TA-see-um)
A metallic element that is important in body functions such as regulation of blood pressure and of water content in cells, transmission of nerve impulses, digestion, muscle contraction, and heartbeat.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)protein (PROH-teen)
A molecule made up of amino acids that are needed for the body to function properly. Proteins are the basis of body structures such as skin and hair and of substances such as enzymes, cytokines, and antibodies.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)receptor (reh-SEP-ter)
A molecule inside or on the surface of a cell that binds to a specific substance and causes a specific physiologic effect in the cell.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)resistance
Failure of a cancer to shrink after treatment.
(http://www.cancer.gov/dictionary)toxicity (tok-SIH-sih-tee)
The extent to which something is poisonous or harmful.
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)
