

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. An in vitro study found that of all the herbs studied, an extract from Hydrastis canadensis was one of the most active in inhibiting the growth of H. pylori (1). Studies done on berberine indicate that it has antimicrobial property and also inhibit growth and induces apoptosis in certain cancer cells (2) (3) (4) (5) (6). 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 (7). Potential drug interactions include reduced effect of anticoagulants, altered response to antihypertensives, and inhibition of cytochrome P (CYP) 450 3A4 (8) (9) (10) and CYP2D6 (11). Goldenseal supplementation did not affect P-Glycoprotein activity in vivo (12). One case of hypernatremia, which may have been induced by goldenseal supplementation, was reported in a patient with diabetic ketoacidosis (13). 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 (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 doxorubicine (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).
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 (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).
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.
No clinical trials have been conducted with goldenseal.