What is Berberine?
Berberine is an isoquinoline alkaloid, a natural compound found in plants such as Chinese goldthread (Coptis chinensis) [1], barberry (Berberis vulgaris) [2], Oregon grape (Mahonia aquifolium) [3], and goldenseal (Hydrastis canadensis) [4]. It exhibits strong biological and pharmacological activity and has a rich history of use in traditional medicine, spanning over 400 years in China, India, and the Middle East [3].
Berberine has shown promise in addressing diverse health conditions, including those of metabolic, gastrointestinal, and neurological origin, among others [5]. Well-tolerated by the human body and clinically safe, few adverse reactions to the plant extract have been reported [1].
This article specifically delves into berberine’s role in addressing metabolic syndrome, a group of conditions marked by obesity, elevated cholesterol, increased blood sugar levels, and heightened blood pressure [1, 6]. A widespread public health issue, these conditions greatly increase the risk of heart disease, type 2 diabetes (T2DM), and stroke [1].
Berberine and Cardiovascular Health
Statins are the most commonly prescribed cholesterol-lowering drugs worldwide. With elevated blood sugar as a potential side effect of these drugs, their use in individuals suffering from both high cholesterol and diabetes is questionable. Further, combining statin drugs with anti-diabetic medications may increase the risk for cognitive impairment [1]. In some cases, statins prove simply ineffective for certain patients [7]. Thus, alternative treatment options are desirable and urgently warranted.
Research has highlighted a diverse range of benefits of berberine for the cardiovascular system. Berberine contributes to lowering blood pressure by reducing cholesterol through several mechanisms. These include enhancing the liver’s capture of cholesterol in the blood, promoting the disposal of LDL (“bad”) cholesterol from the blood, reducing cholesterol absorption in the gastrointestinal tract, and improving cholesterol excretion from the body [7].
One study noted a reduction in total cholesterol, triglycerides, and LDL cholesterol, along with an increase in HDL (“good”) cholesterol, after 3 months of berberine supplementation at a dosage of 300 mg 3 times daily [5, 8]. Clinical trials have demonstrated that combination therapy with berberine and statins yields positive outcomes on lipid profiles [7], although some studies have shown that berberine alone yields similar results [1].
Berberine is also suggested to offer benefits in protecting endothelial cells, the cells lining our blood vessels, and regulating their function to prevent cardiovascular disease. It accomplishes this by boosting the production of nitric oxide (NO), a molecule responsible for the following:
- Relaxing the blood vessels, thereby increasing blood flow and oxygen availability,
- Regulating blood pressure, and
- Preventing blood clots by inhibiting the aggregation of platelets.
Furthermore, berberine exhibits anti-inflammatory properties and acts as an antioxidant in the body, functions that contribute significantly to the treatment and prevention of cardiovascular disease [7].
Berberine and Blood Sugar
Extensive literature supports the role of berberine in reducing blood sugar levels, alleviating insulin resistance [1], and decreasing liver enzymes in individuals with T2DM[6]. This is achieved through various mechanisms:
- Stimulating glycolysis: Berberine enhances the breakdown of glucose, or blood sugar, by increasing the activity of certain enzymes in the liver known as glucokinases.
- Blocking sugar production: Berberine inhibits the liver’s production of glucose, aiding in the management of blood sugar levels.
- Influencing fat cells: Berberine prevents the formation of fat cells and promotes the breakdown of fat.
- Increasing insulin release: Berberine boosts insulin release from the pancreas when blood glucose levels are high. This is achieved by increasing the level of glucagon-like peptide-1 (GLP-1), a hormone that is released from intestinal cells in response to food intake. Insulin acts as a key, unlocking the door to our cells to allow sugar inside for energy use, effectively lowering the level of sugar in the blood.
- Activating AMPK (5-adenosine monophosphate kinase): Berberine activates AMPK, a protein crucial for energy balance. This activation improves insulin sensitivity, making cells more responsive to insulin and promoting glucose uptake into the cells.
- Reducing glucose absorption: By inhibiting an enzyme called glycosidase, berberine may decrease the absorption of glucose in the intestines. Glycosidase is responsible for breaking down sugars into simpler forms for easier absorption[6].
Berberine has also been proposed as an anti-obesity treatment, given its positive effects on the gut microbiome and downregulation of fat production[5]. In a 2023 study involving 49 overweight individuals with impaired fasting glucose levels, significant reductions in fasting blood sugar, total cholesterol, triglycerides, insulin, and fat mass were o (550 mg of Berberine PhytosomeTM, equivalent to 188 mg berberine, twice daily) compared to the placebo group after a 2-month treatment period. No side effects were reported [9], demonstrating berberine’s favorable safety profile.
Moreover, considering the prevalence of insulin resistance in women with polycystic ovarian syndrome (PCOS), the use of berberine has extended to this condition. By reducing insulin resistance, berberine is suggested to improve cholesterol profiles and enhance ovulation in this population[5].
The Bottom Line
The clinical applications of berberine are expansive, ranging from the regulation of blood sugar and cholesterol to a spectrum beyond the scope of this discussion. However, it’s crucial to emphasize that the use of berberine as a supplement needs to be carefully evaluated on an individual basis. While showcasing promising outcomes in addressing diverse conditions, it is imperative to underscore the ongoing need for research. Delving deeper into its potential is vital for a comprehensive understanding of berberine’s role in both the prevention and management of chronic diseases.
References
- Ye Y, Liu X, Wu N, et al. Efficacy and Safety of Berberine Alone for Several Metabolic Disorders: A Systematic Review and Meta-Analysis of Randomized Clinical Trials. Front Pharmacol. 2021;12:653887. Published 2021 Apr 26. doi:10.3389/fphar.2021.653887
- Tilgner S. Herbal Medicine: From the Heart of the Earth. 3rd ed. Wise Acres; 2020. ISBN 1881517055, 9781881517054.
- Utami AR, Maksum IP, Deawati Y. Berberine and Its Study as an Antidiabetic Compound. Biology (Basel). 2023;12(7):973. Published 2023 Jul 8. doi:10.3390/biology12070973
- Zhao JV, Yeung WF, Chan YH, et al. Effect of Berberine on Cardiovascular Disease Risk Factors: A Mechanistic Randomized Controlled Trial. Nutrients. 2021;13(8):2550. Published 2021 Jul 26. doi:10.3390/nu13082550
- Och A, Podgórski R, Nowak R. Biological Activity of Berberine-A Summary Update. Toxins (Basel). 2020;12(11):713. Published 2020 Nov 12. doi:10.3390/toxins12110713
- Och A, Och M, Nowak R, Podgórska D, Podgórski R. Berberine, a Herbal Metabolite in the Metabolic Syndrome: The Risk Factors, Course, and Consequences of the Disease. Molecules. 2022;27(4):1351. Published 2022 Feb 17. doi:10.3390/molecules27041351
- Rui R, Yang H, Liu Y, et al. Effects of Berberine on Atherosclerosis. Front Pharmacol. 2021;12:764175. Published 2021 Nov 26. doi:10.3389/fphar.2021.764175
- Wang L, Peng LY, Wei GH, Ge H. Zhongguo Zhong Xi Yi Jie He Za Zhi. 2016;36(6):681-684.
- Rondanelli M, Gasparri C, Petrangolini G, et al. Berberine phospholipid exerts a positive effect on the glycemic profile of overweight subjects with impaired fasting blood glucose (IFG): a randomized double-blind placebo-controlled clinical trial. Eur Rev Med Pharmacol Sci. 2023;27(14):6718-6727. doi:10.26355/eurrev_202307_33142
