What is berberine?
Berberine, is an important bioactive compound found in several popular medicinal plants, including barberry (cranberry) and coptis (Chinese golden thread). Berberine can be isolated from these plants and used as a dietary supplement, usually in the form of berberine (hydro)chloride or berberine sulfate.
In Asian countries, especially China, berberine has been widely used since the 1950s due to its efficacy against gastrointestinal infections and diarrheal diseases and its good safety record.
It is also used to treat type 2 diabetes, high blood pressure, heart failure, inflammation, and liver disease.
Scientific interest in berberine has increased significantly since the turn of the century. Although the number of published preclinical studies (in vitro and animal studies) is much higher than the number of clinical (human) studies, this situation is gradually changing.
Berberine has antibacterial, resistance-enhancing, anti-inflammatory, immunomodulatory, analgesic, anti-allergic, antioxidant, hypoglycemic, lipid-lowering, organ protection, neuroprotection, inhibition of atherosclerosis, and blood pressure lowering effects. Berberine has a positive effect on the gut microbiome and intestinal barrier function, and fights diarrheal diseases.
Where does berberine come from?
Berberine (hydro)chloride is a yellowish, bitter benzylisoquinoline alkaloid found in the roots (stems) and bark of medicinal plants, including B. vulgaris, B. aristata, B. croatica, B. aquifolium. B. sibirica), coptis (C. chinensis, C. japonica), bloodroot (S. canadensis), Hydrastis (H. canadensis), Xanthorhiza (X. simplicissima), Phellodendri (P. chinense, P. amurense), Celandine (C. majus), Argemone (A. mexicana) and Thalictrum (T. flavum).
What diseases and symptoms is berberine effective for?
- Prevention and (additional) treatment of (gastrointestinal) infections (bacteria, viruses, fungi, parasites)
- infectious diarrhea
- Leaky gut, intestinal flora imbalance
- PDS-D (Irritable Bowel Syndrome Predominantly Diarrhea)
- inflammatory bowel disease
- Gastritis, gastric ulcer
- Reflux esophagitis
- Prevention of adhesions after abdominal surgery
- Prevent radiation-induced intestinal inflammation (enteritis) and lung damage
- Supports the immune system in (chronic) inflammatory diseases, allergies and autoimmune diseases
- Lipid metabolism disorders (hypercholesterolemia, hypertriglyceridemia)
- overweight/obese
- Metabolic syndrome
- Diabetes (complications)
- Polycystic ovary syndrome (PCOS)
- Cardiovascular disease (atherosclerosis, hypertension, arrhythmia, ischemic heart disease, heart failure, abdominal aortic aneurysm)
- Liver disease (non-alcoholic fatty liver disease, fibrosis, cirrhosis)
- mondaften
- Thrombocytopenia
- Prevention (recurrence) of colorectal adenomas
- Familial adenomatous polyposis (FAP)
- Helps with cancer, neurodegenerative diseases, mood disorders (depression, anxiety), post-traumatic stress disorder (PTSD), schizophrenia and psychosis
Who should not use berberine?
- Pregnancy and breastfeeding
- hypotension
Usage and dosage of berberine (for reference only):
- General recommended dosage: 500-2000 mg/day
- Lipid metabolism disorders: 500-1500 mg/day
- Metabolic syndrome: 1000-1500 mg/day
- Diabetes (complications): 1000-2000 mg/day or 20 mg/kg/day
- PDS-D (diarrhoea-predominant irritable bowel syndrome): 500 mg/day
- Radiation enteritis prophylaxis: 1000 mg/day
- Radiation lung injury prevention: 20 mg/kg/day
- Liver disease: 500-1500 mg/day
- Arrhythmia: 1000-2000 mg/day
- Heart failure: 100-2000 mg/day
- Polycystic ovary syndrome daytime: 1500 mg/day
Tip: Berberine is best taken throughout the day with meals.
Interactions with drugs:
Berberine has hypoglycemic, lipid-lowering, antiplatelet and antihypertensive effects. People taking antidiabetic, cholesterol-lowering, anticoagulant, antiplatelet, or antihypertensive medications should consider this. Adjust medication appropriately.
In a preliminary human study, berberine (300 mg three times daily) significantly reduced the activity of the cytochrome P450 enzymes CYP2D6, CYP2C9, and CYP3A4. This effect may be dose-dependent. This means that the blood levels (and bioavailability) of drugs metabolized by CYP2D6, CYP2C9, and/or CYP3A4 may be (strongly) increased when taken concurrently with berberine. Since many drugs are broken down by CYP3A4, it is important to be aware of possible interactions. Supplementation with berberine requires caution or discussion as to whether the medication dose can be adjusted.
Plasma levels of cyclosporine (also determined by the activity of the efflux pumps P-glycoprotein and CYP3A4) were significantly increased during concurrent use of berberine (200 mg three times daily). This has been confirmed in multiple human studies. If the dose of cyclosporine is adjusted, berberine may be continued.
Berberine may increase blood concentrations of digoxin and metformin (animal studies)
It is best not to combine berberine with macrolides (such as erythromycin, clarithromycin, and azithromycin) because of the potential for enhanced cardiotoxicity.
Concomitant use of berberine with statins increases the risk of (severe) cardiotoxicity. It is understood that berberine is safe when combined with red yeast rice.
Berberine prevents the toxicity of cisplatin, cyclophosphamide, doxorubicin, paclitaxel, bleomycin, methotrexate, and paracetamol (animal testing).
Berberine may prevent iron accumulation and iron-induced liver and kidney damage, in part by chelating iron and reducing oxidative stress (animal studies).
Berberine may prevent lead-induced oxidative stress as well as liver and kidney toxicity (animal studies).
Preclinical studies have shown that berberine has antidepressant effects, in part by inhibiting monoamine oxidase. It is unclear whether normal doses of berberine can potentiate the effects of MAO inhibitors.
Berberine may prevent ethanol-induced ulcers (animal study).
Berberine Safety
Berberine is less toxic at recommended doses (200-2000 mg/day) and can be used long-term. But at higher doses, some people experienced (mild) gastrointestinal discomfort (eg, constipation, diarrhea, gas) similar to placebo.
These symptoms usually resolve within 4 weeks; dose reduction to a maximum of 500 mg/day is sometimes required.
Gastrointestinal problems are less likely to occur if you take berberine after a meal.
Berberine is safe for people with chronic liver disease.
In most cases, berberine works well with conventional medications; however, medication dosage adjustments may be needed (see Interactions with Drugs).