Huanglian

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Common Names

Goldthread
Chinese coptis
Coptis deltoidea
Coptis teetoides

For Patients & Caregivers

Tell your healthcare providers about any dietary supplements you’re taking, such as herbs, vitamins, minerals, and natural or home remedies. This will help them manage your care and keep you safe.

How It Works

Available data are insufficient to determine whether huanglian is effective in preventing or treating cancer.

Huanglian and berberine showed anti-hyperglycemic activity in small studies, but well-designed trials are lacking. In addition, studies done in laboratory and in animal models indicate that huanglian and berberine have anticancer effects. Clinical trials 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 claim, but clinical data are lacking.
To lower high blood pressure
Laboratory and animal studies support this claim, but human data are needed.

Do Not Take If

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 also induce CYP3A4 by activating pregnane X receptor. This may decrease the concentration of drugs metabolized by CYP3A4. Clinical significance is not known.

Special Point

Huanglian displaces bilirubin and should not be administered to jaundiced neonates.
Berberine-containing botanicals may prolong QTc in patients with underlying heart disease

For Healthcare Professionals

Scientific Name

Coptis chinensis

Clinical Summary

Derived from the rhizome of the perennial herb Coptis chinensis, huanglian is used in traditional Chinese medicine for diarrhea, vomiting, abdominal fullness, jaundice, high fever coma, toothache, diabetes and eczema. It showed antimicrobial, antidiabetic, antioxidant and anti-inflammatory effects ⁽¹⁶⁾. Alkaloids that include berberine are considered to be the bioactive components ⁽¹⁾.

Berberine demonstrated hepatoprotective ⁽⁹⁾ and anti-inflammatory ⁽¹⁴⁾ effects, as well as improving glucose metabolism in a murine model of diabetes ⁽¹⁰⁾. Jatrorrhizine, a protoberberine, was shown to offset postoperative ileus-induced delayed gastric emptying, and intestinal transit in mice ⁽¹⁵⁾.

Huanglian and berberine have also been reported to exert anti-hyperglycemic activity in small studies, but well-designed trials are lacking ⁽¹⁷⁾ ⁽¹⁸⁾. In addition, preclinical findings indicate that huanglian ⁽⁵⁾ ⁽⁶⁾ and berberine ⁽³⁾ ⁽¹⁹⁾ ⁽²⁰⁾ have anticancer effects. Clinical trials have yet to be conducted.

Purported Uses

Microbial infections
Diarrhea
Hypertension

Mechanism of Action

Berberine and berberine-like alkaloids are thought responsible for the biological effects of huanglian. Berberine inhibits human hep-62 hepatoma cell growth due to morphological changes and internucleosomal DNA fragmentation ⁽³⁾. Berberine also inhibits platelet aggregation and can antagonize thromboxane B2. In an animal model, it caused potassium channel blockade resulting in prolongation of the action potential in ventricular monocytes ⁽¹⁾.

Huanglian inhibits topoisomerase I and is thought to suppress cyclin B1 protein, causing cancer cell arrest at G2 phase ⁽²⁾. In other studies, it demonstrated antiangiogenic activity ⁽⁶⁾, induced apoptosis and arrested cell growth by upregulating Interferon beta as well as 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) CYP2D6, CYP2C9, as well as CYP3A4 (13), and can therefore affect drugs metabolized by these enzymes.
Prolonged use of huanglian can induce CYP3A4 by activating pregnane X receptor (12). This may reduce the effectiveness of drugs metabolized by this enzyme. But clinical relevance is not known.

Dosage (OneMSK Only)

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.
Wang J, Wang L, Lou GH, et al. Coptidis Rhizoma: a comprehensive review of its traditional uses, botany, phytochemistry, pharmacology and toxicology. Pharm Biol. 2019 Dec;57(1):193-225.
Wang H, Mu W, Shang H, Lin J, Lei X. The antihyperglycemic effects of Rhizoma Coptidis and mechanism of actions: a review of systematic reviews and pharmacological research. Biomed Res Int. 2014;2014:798093.
Dong H, Wang N, Zhao L, Lu F. Berberine in the treatment of type 2 diabetes mellitus: a systemic review and meta-analysis. Evid Based Complement Alternat Med. 2012;2012:591654.
Wang N, Tan HY, Li L, Yuen MF, Feng Y. Berberine and Coptidis Rhizoma as potential anticancer agents: Recent updates and future perspectives. J Ethnopharmacol. 2015 Dec 24;176:35-48.
Liu Y, Hua W, Li Y, et al. Berberine suppresses colon cancer cell proliferation by inhibiting the SCAP/SREBP-1 signaling pathway-mediated lipogenesis. Biochem Pharmacol. 2019 Dec 23;174:113776.

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Last Updated

Wednesday, January 22, 2020