What is Berberine?
Berberine is a natural isoquinoline alkaloid extracted from the roots, rhizomes, and stem bark of several medicinal plants, including goldenseal (Hydrastis canadensis), Coptis (Coptis chinensis), Oregon grape (Berberis aquifolium), barberry (Berberis vulgaris), and tree turmeric (Berberis aristata), with a 3000-year history of use in traditional Chinese and Ayurvedic medicine. 1, 2
Chemical Classification and Source
- Berberine is classified as an isoquinoline quaternary botanical alkaloid that can be isolated from the barks and roots of numerous plant species 3, 4
- The compound is present in multiple Berberis species and Coptis species, making it widely available from natural sources 4, 1
Pharmacological Properties and Mechanisms
Berberine demonstrates broad-spectrum antimicrobial activity against bacteria, viruses, fungi, protozoans, helminths, chlamydia, plasmodia, and trypanosomes. 1, 3
- The compound exhibits anti-inflammatory effects by reducing pro-inflammatory cytokines including IL-6, IL-1β, TLR4, and TNF-α 2
- Berberine functions as a natural PCSK9 inhibitor, contributing to its cholesterol-lowering effects by increasing low-density lipoprotein receptor expression, reducing intestinal cholesterol absorption, and promoting cholesterol excretion from liver to bile 2
- It enhances insulin sensitivity and secretion by pancreatic β-cells in Type 2 Diabetes Mellitus 2
Clinical Applications
The predominant clinical uses include treatment of bacterial diarrhea, intestinal parasite infections, and ocular trachoma infections. 1
- Research supports potential therapeutic applications in diabetes, cardiovascular disease, Alzheimer's disease, cancer, hyperlipidemia, cerebral ischemia, mental disease, and osteoporosis 4, 2
- The compound demonstrates neuroprotective properties in various neurodegenerative and neuropsychological conditions 3
- Berberine shows anti-obesity and antidiabetic effects through modulation of glucose and fat metabolism 3
Bioavailability and Limitations
The major limitation of berberine is its poor oral bioavailability, which has hindered widespread clinical use despite its therapeutic potential. 2, 5
- Oral delivery is challenged by poor absorption, requiring enhancement strategies before broader clinical application 5
- Despite low bioavailability, berberine may exert beneficial effects through modulation of the gut microbiome 3
- Novel synthetic berberine derivatives are being developed to optimize bioavailability and other pharmacokinetic properties 2
Safety Profile
- Berberine is generally well-tolerated with few side effects when used appropriately 2
- The compound has been safely used in traditional medicine for 3000 years, supporting its favorable safety profile 2
Available Formulations
- Berberine is available in homeopathic preparations, with Hydrastis canadensis 1M containing less than 10-12 mg of hydrastine and berberine alkaloids per pellet (0.443 mg of active ingredient per pellet) 6