Berberine: Uses, Benefits, and Properties Explained
Berberine is a quarternary ammonium salt (Figure 1) found in the roots, rhizomes, stems, and bark of plants such as Barberry (Berberis Vulgaris), Tree Turmeric (Berberis Aristata), Goldenseal (Hydrastis canadensis), and Oregon Grape (Mahonia Aquifolium). The use of berberine plant rich species such as the Berberis family has been used in Asia for over 3000 years1. Many clinical and experimental studies show that berberine has pharmacological properties such as immunomodulatory, antioxidative, cardioprotective, hepatoprotective, and renoprotective effects. In medicinal chemistry, the structure of Berberine has been modified to create bioactive derivatives in order to increase potency and selectivity2.
Figure 1: The Structure of Berberine
Berberine is Anti-Diabetic and Increases Insulin Sensitivity
Berberine has been used successfully in the treatment of type 2 diabetic patients, and had similar hypoglycemic effects as the prescription diabetic drug metformin. In a 3 month trial, patients taking 500mg Berberine 3x daily saw decreases in Hemoglobin A1c, blood glucose levels, triglycerides, as well as total and LDL Cholesterol 3. In the second part of the study, subjects also experienced plasma insulin reduction of up to 44% 3.
Another study with 116 patients with type 2 diabetes and dyslipidemia were given 1g of berberine per day for 3 months. These subjects experienced a significant decrease in plasma glucose levels, triglycerides, and LDL cholesterol compared to the placebo group. Patients given the berberine also experienced an increase in Glucose Disposal Rate (Greater Insulin Senstivity)4.
The results of these studies are extremely beneficial due to the limited availability of effective medications for blood glucose. Single berberine is a single, purified compound found in several plant sources, it has the potential to be effective for reducing blood glucose levels in populations worldwide.
Berberine is able to improve glucose metabolism and thus insulin sensitivity by activating AMPK – an enzyme responsible for glucose uptake – as well as induction of glycolysis13.
Berberine Reduces Cholesterol and Triglycerides
In addition to being used for effective hypoglycemic treatment and increasing insulin sensitivity, Berberine is effective at improving cholesterol levels, as the studies mentioned above also showed with decreased LDL Cholesterol levels. In a separate study, using Berberine for 3 months reduced serum cholesterol by 29%, LDL cholesterol by 25%, and triglycerides by 35%. Berberine lowers cholesterol by acting upon the Low Density Lipoprotein Receptor (LDLR): Elevating LDLR expression by stabilizing the mRNA. This means that Berberine is capable of lowering cholesterol through a different mechanism than statin drugs5.
Berberine’s Anti-Inflammatory and Anti-Tumor Effects
Berberine also possesses anti-inflammatory and anti-tumor effects. Berberine’s anti-inflammatory activity comes from inhibiting mitogen-activated protein kinase and cellular reactive oxygen species production6. Berberine also inhibits gene transcription by forming strong complexes with DNA or RNA to induce DNA damage and telomerase inhibition7. These effects of berberine may lead to cell death in carcinogenic tumors. Use of Berberine with radiation therapy enhances the cytotoxic effect on tumors and reduces side effects from the therapy8.
Making modifications to the chemical structure of Berberine is able to increase its bioactivity, bioavailability, and specific effects of the molecule (Figure 2).
Figure 2: Modifications at Numbered Positions Change the Properties of Berberine.
Adding functional groups at carbon 8 or 13 will increase the antimicrobial activity of berberine. Adding a substituent at carbon position 9 will enhance its anti-tumor activity9.
Berberine and Non-Alcoholic Fatty Liver Disease Treatment
Berberine also shows promise in the treatment of Non Alcoholic Fatty Liver Disease (NAFLD) Treatment. Patients who received 500mg of Berberine 2x per day for 16 weeks saw reduced bodyweight, an improvement in lipid profile, and a significant reduction of Hepatic Fat Content. Berberine shows promise in regulating hepatic lipid metabolism10.
Berberine and its Effect on the Digestive System
Because Berberine has relatively poor bioavailability, much of its activity occurs in the gastrointestinal system. For this reason, it is an effective treatment for Inflammatory Bowel Disease and possesses strong anti-inflammatory effects on the digestive system11.
Berberine and Antimicrobial Properties
Berberine has well established anti-microbial properties and can control infection by bacteria, viruses, fungi, protozoans, and helminthes. An example of this is Berberine has the ability to inhibit E.Coli12. Berberine is sold as an over the counter drug for gastrointestinal infections in China.
Berberine has many uses, ranging from use in reducing blood glucose levels and increasing insulin sensitivity, improving cholesterol levels and triglycerides, anti-inflammatory and gastrointestinal benefits. These benefits can be very useful for bodybuilders or other athletes, with 500mg given twice daily proving to be a beneficial dose in clinical studies. Our new upcoming product, Leviathan Nutrition Ire will feature 1000mg of Berberine per serving, providing all of the benefits mentioned in this article.
DISCLAIMER: These statements have not been evaluated by the Food and Drug Administration, these products are not intended to diagnose, treat, cure, or prevent any disease.