Cholesterol management continues to be a primary strategy for the prevention of cardiovascular disease
The American Heart Association and the American College of Cardiology recommend statin medications to lower cholesterol in select individuals.
However, some patients are intolerant of statin medications, and others choose not to take them. Dietary supplements may offer an alternative approach to cholesterol management for these patients. One such dietary supplement is berberine.
Berberine is an isoquinoline alkaloid isolated from Coptis chinensis, Hydrastis canadensis and other plants in the genus Berberis. Berberine has been used for thousands of years in Traditional Chinese Medicine for conditions ranging from type 2 diabetes to hypertension. Recent evidence suggests that berberine is effective at managing healthy cholesterol levels.
A review article, published in the Journal of Evidence Based Complementary and Alternative Medicine in 2018, summarised the clinical trials of berberine for the treatment of hyperlipidaemia. Twelve randomised controlled trials of berberine were included in the review. The data were not pooled for a meta-analysis because of high heterogeneity among studies.
Three of the 12 studies evaluated berberine as a standalone treatment (1000-1500 mg/day), compared with placebo. The other 9 studies evaluated berberine (500 mg/day) in combination with other natural ingredients and compared with either a placebo or conventional treatment.
The combination that was studied most frequently (five studies) included berberine (500 mg), red yeast rice extract (200 mg), policosanol (10 mg), folic acid (0.2 mg), coenzyme Q10 (2 mg) and astaxanthin (0.5 mg). Study durations ranged from 4 weeks to 1 year.
The majority of studies consistently suggested that berberine had a beneficial effect on LDL cholesterol (reducing it by 20-50 mg/dL) and triglycerides (reducing them by 25-55 mg/dL).
Berberine alone and in combination with other supplements provided an average LDL percent reduction of 20–30%. This can be compared with the proven LDL reduction capacity of 30–50% with moderate-intensity statin therapy.
Berberine’s mechanism of action has been shown to be similar to that of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, which are approved medications for hyperlipidaemia.
PCSK9 inhibitors decrease the degradation of LDL receptors thereby increasing the clearance of LDL cholesterol. This is a different mechanism than that of statins and red rice yeast extract, suggesting that berberine might work synergistically with these other cholesterol-lowering agents.
It should also be noted that berberine has been shown in human studies to inhibit cytochrome P450 (CYP) 2D6, 2C9, and 3A4 affecting the concentrations of drugs metabolised by these enzymes.
In sum, the authors of this review conclude that berberine (at a dosage of 500 mg/day, alone or in combination with other supplements) could serve as an alternative for patients who are intolerant of statin medications, resist taking statin medications, or do not have a risk profile that indicates statin therapy.