About Herbs

Bottom Line: The active compound in goldenseal is berberine, which was found helpful in certain conditions. But there is no proof that goldenseal can be used to treat cancer in humans.

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. In human research, berberine treated acute diarrhea, probably because of its antibacterial properties, and improved chronic gall bladder inflammation and liver cirrhosis. 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 uterus smooth muscles.

To control muscle spasms
Laboratory studies in animal tissues support this use, but no clinical trials have been performed to confirm that this effect occurs in humans.

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 cirrhosis of the liver
Two clinical trials show that berberine, a compound in goldenseal, improves the condition of patients with cirrhosis.

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. No clinical trials have been conducted in humans to confirm this effect.

To treat conjunctivitis
Laboratory data shows that berberine, a compound in goldenseal, has antibacterial properties, but no clinical trials have been conducted to study this effect humans.

To treat diabetes
Two small clinical studies showed that berberine, a compound found in goldenseal, lowers blood glucose levels in type 2 diabetics.

To manage painful and heavy menstruation
Laboratory evidence regarding goldenseal's ability to relax uterus muscle is mixed. No clinical trials have been performed in humans.

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 lower fevers
Laboratory studies support this use, but no clinical trials have been performed.

To reduce swelling and edema
Laboratory studies show that berberine, a compound in goldenseal, blocks some of the molecules involved in inflammation. No clinical trials have been performed to confirm that this effect occurs in humans.

No clinical trials have been conducted with goldenseal.

Eye root, yellow Indian plant, turmeric root, yellow paint root, orange root, goldenroot

Derived from the root of the plant, goldenseal is though to have anti-inflammatory and antimicrobial activities. It 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. Studies done on berberine indicate that it has antimicrobial property and also induces apoptosis in certain cancer cells ^{(11) (13)}. No clinical studies evaluating its efficacy have been published.

Minimal adverse events have been reported at recommended doses, but nausea, vomiting, hallucinations, or seizures may be signs of toxicity ⁽¹⁾. Potential drug interactions include reduced effect of anticoagulants, altered response to antihypertensives, and inhibition of cytochrome P (CYP) 450 3A4/5 ^{(2) (3) (4)} and CYP2D6 ⁽⁵⁾. Goldenseal supplementation did not affect P-Glycoprotein activity in vivo ⁽⁶⁾. One case of hypernatremia, which may have been induced by goldenseal supplementation, was reported in a patient with diabetic ketoacidosis ⁽⁷⁾. Patients with hypertension, cardiovascular disease, or are pregnant should not take this herb.

Goldenseal is claimed to have anti-inflammatory, astringent, antimicrobial, and laxative properties ⁽⁸⁾. The pharmacological action of goldenseal is attributed to both 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 ^{(9) (10) (11)}. In an animal study, berberine has been shown to prolong QTc interval and to help prevent ventricular fibrillation after myocardial infarction ⁽¹²⁾. The hydrastine component induces constriction of peripheral blood vessels ⁽¹³⁾. While two small clinical trials reported that goldenseal affects CYP2D6 ⁽¹⁴⁾ and CYP3A ⁽⁴⁾, another could not confirm such effects ⁽¹⁵⁾.

Berberine-containing botanicals may cause QTc prolongation in patients with severe underlying heart disease.

Patients who have hypertension or cardiovascular disease or women that are pregnant or nursing should not consume goldenseal.

Common: GI complaints
Rare: Nervousness
Toxicity: Stomach ulcerations, constipation, convulsions, hallucinations, nausea, vomiting, depression, nervousness, bradycardia, respiratory depression, seizures  ⁽¹⁾

Antihypertensives: Goldenseal may interfere with blood pressure control.
Anticoagulants / Antiplatelets: Berberine may inhibit anticoagulant effects.
Barbiturates: Goldenseal may potentiate effects.
Cytochrome P-450: Goldenseal may inhibit the CYP3A4 and CYP2D6 isoenzymes, resulting in increased levels of certain medications such as cyclosporine A ⁽¹⁶⁾.
Vitamin B Complex: Goldenseal may decrease gastric absorption resulting in possible deficiency.

Berberine may increase bilirubin levels due to displacement of bilirubin from albumin ⁽¹⁷⁾.
Goldenseal may cause a darkening in urine color in illicit drug testing ⁽¹⁸⁾.
Goldenseal may alter PT / PTT / INR anticoagulation test results ⁽²⁾.
May prolong QTc interval in electrocardiogram ⁽¹²⁾.
One case of hypernatremia was reported in a patient with diabetic ketoacidosis ⁽⁷⁾.

There are no clinical studies reported in Medline using goldenseal. The following studies concern berberine, an active component of Goldenseal.

Werbach MR, et al. Botanical Influences on Illness: A Sourcebook of Clinical Research. Tarzana, California: Third Line Press; 1994.
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. The berberine alkaloids have shown potent macrophage-activating activity for inducing cytostatic activity against tumor cells.

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
In vitro studies were performed on a series of human malignant brain tumor cells and rat brain tumor cells. Berberine used alone at a dose of 150 mcg/ml had an average cancer cell kill rate of 91%. BCNU 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 on killing cancer cells.