Health Care Professional Information
Goldthread, Coptis chinese, Coptis deltoidea, Coptis teetoides
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).
- Ear infections
- Microbial infection
- Respiratory infections
- 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).
Huanglian displaces bilirubin and should not be administered to jaundiced neonates.
Berberine-containing botanicals may prolong QTc in patients with underlying heart disease.
- 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) .
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- 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.
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.
- 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.
- Shortness of breath
- Toxicity from high doses of huanglian can cause seizures, liver toxicity, and cardiac toxicity.
Last updated: October 29, 2012