What is Berberine and what does it do in the body?
Berberine is an isoquinoline alkaloid found in plants that has been studied for its pharmacological effects. It is found in plants including barberry, Oregon grape, goldenseal, and coptis. The use of Berberine containing plants goes back to Native Americans who used them for disorders of the eye and skin as well as inflammatory conditions. Berberine was isolated from goldenseal root by Constantine Rafinesque in 1828 and was subsequently used in the Eclectic medical practice of the mid-1800s for gastrointestinal complaints, jaundice, infections, as a bitter tonic for bile production, and as a uterine tonic.
Berberine has been shown to have antibiotic, anticonvulsant, antidiarrheal, anti-inflammatory, choleretic, carminative, hepatoprotective, hypolipidemic, hypotension, immunostimulatory, sedative, and uterine tonic effects on the body. It is most well known for its antibiotic activity against bacteria, Protozoa, and fungi including the specific strains of E. Coli, Streptococcus aureus, Candida albicans, and Mycobacterium tuberculosis just to name a few. It has also been shown that pathogens generally fail to develop resistance to its antimicrobial activities that work through multiple mechanisms of action, unlike antibiotics that tend to work through one mechanism of action and thus are easier for the pathogens to develop a resistance to. Berberine also may promote healthy intestinal microflora, unlike conventional antibiotics that work against both good and bad microflora.
There are numerous studies that show how Berberine may modulate the immune response and may suppress the growth of a wide spectrum of tumors. It was shown to increase blood supply to the spleen, which supports the release of compounds that potentiate the immune response, and has shown to activate macrophages. Berberine’s anti-cancer activity may be due to directly killing tumor cells and indirectly stimulating white blood cells.
Berberine has demonstrated a wide range of antidiabetic effects such as increasing insulin-receptor expression, improving the utilization of glucose, reducing insulin resistance through increasing protein kinase C-dependent insulin receptor expression, stimulating insulin secretion, and blocking glucose absorption.
As for its cardiovascular effects, Berberine may help increase Nitric Oxide production to lower blood pressure, may regulate glucose and increase insulin sensitivity, and may reduce plasma cholesterol and triglycerides.
Berberine seems to act via adenosine monophosphate–activated protein kinase (AMPK). This may account for its protective effects against reactive oxygen species and inflammation which are characteristic of vascular injury, as well as its ability to regulate glucose and protect the body against altered insulin signaling. AMPK is also responsible for Berberine's vasodilating effects because Berberine induces vasodilation through the mediation of eNOS, which leads to nitric oxide production through the AMPK cascade.
What is Berberine used for?
Berberine is used for infections due to its antimicrobial and immune stimulating effects. It is also used for infectious diarrhea and bowel health, trachoma, liver health, cancer prevention, heart disease, type 2 diabetes, metabolic syndrome, and weight loss.
Berberine has been shown to be effective in the treatment of acute diarrhea due to traveler’s diarrhea, shigellosis, food poisoning, infectious diarrhea, giardiasis, cholera, and IBS. To read more about the use of Berberine in IBS see our blog post: Irritable Bowel Syndrome (IBS).
Berberine can also be useful for gastrointestinal issues such as overgrowth of H.Pylori and Candida albicans. To read more about Berberine in gastrointestinal pathology, see our blog post: Digestion 101-Physio and Pathophysiology-Part III.
Berberine can support the body with cholecystitis and cirrhosis of the liver. It is among the category of herbal bitters and thus has a cholagogue effect on the body, which means that it stimulates the secretion of bile, which is helpful for detoxifying the liver and other toxins in the body. Berberine has been shown effective for cirrhosis due to its ability to decrease tyramine, an amino acid that is elevated with liver damage. Berberine may also protect the liver from chemical-induced liver damage, including acetaminophen (Tylenol) induced hepatotoxicity. One of the ways it protects the liver is by increasing antioxidants such as glutathione, which is protective for the liver.
Berberine is also effective for heart disease including congestive heart failure (CHF) and hyperlipidemia. Multiple studies have shown that Berberine may help decrease vascular arterial resistance, decrease blood pressure, and increase overall cardiac performance in patients with CHF. A number of studies have shown that Berberine can reduce low-density lipoprotein-cholesterol (LDL-C) inpatients with hyperlipidemia, including those with high cholesterol levels resistant to statin drug treatment.
Berberine has also shown to be effective in type 2 diabetes and metabolic syndrome. Berberine may help lower fasting blood glucose, hemoglobin A1C, triglycerides, and insulin levels in patients with type II diabetes.
Berberine may help with weight loss due to its effects on insulin resistance and blood sugar regulation. It also activates AMPK, an enzyme that plays a role in metabolism regulation, appetite regulation, and body fat composition, which may make it effective for weight loss.
What are the available forms of Berberine?
Berberine HCl is the hydrochloride salt form of Berberine; it is created by combining Berberine with hydrochloric acid, which increases its solubility and absorption in the body. Berberine HCl is more bio available than just Berberine, which is why you see this form many times when you are looking at Berberine supplements. Some options for Berberine HCl we offer are Berberine 500 Allergy Research Group and Berberine Integrative Therapeutics.
Berberine phytosome is a form of Berberine that is coated in a phospholipid layer, which increases the absorption rate and bioavailability in the body. Some options for this form of Berberine are Berberine Thorne and Berberine Ultrasorb Pure.
Dihydroberberine (DHB) is a highly bio-available metabolite of Berberine, the natural bio active form of Berberine, that has shown benefits for blood glucose metabolism. This form has shown to perform as well as Berberine at 5 times smaller of a dose. That is why the dosage in Berberine ES-5 Xymogen that contains DHB is lower than the standard 500mg dose you will find in most Berberine supplements.
For complexes with Berberine from different herbal sources try Berberine Complex Integrative Therapeutics and Candibactin-BR Metagenics.
What are the sources of Berberine?
The main herbs that contain Berberine used in North America include goldenseal (Hydrastis canadensis), barberry (Berberis vulgaris), Oregon Grape (Berberis aquifolium), and coptis (Coptis chinensis).
Goldenseal is an herb native to eastern North America that is grown in Oregon and Washington. It is a perennial herb with a yellow rhizome; the primary parts used are the dried rhizome and roots, but the leaf is used in the Southern United States.
Barberry is a deciduous spiny shrub that is native to Europe and has been naturalized in eastern North America. The primary parts used are the rhizomes and the roots, sometimes the bark of the stem and root are used.
Oregon Grape is an evergreen, spineless shrub native to the Rocky Mountains from British Columbia to California. The primary parts used are the rhizomes and roots, sometimes the bark of the stem and root are used.
Coptis, also known as goldthread, is a perennial herb native to China. The parts used are the rhizomes and the root.
What are contraindications of Berberine?
Berberine should not be taken during pregnancy. It may interact with prescription medications, so if you are taking any prescription medications, talk to your healthcare provider before taking Berberine. It is especially important to be cautious if you are taking drugs that interact with the liver. Berberine may interact with blood pressure lowering drugs and supplements, blood sugar lowering drugs and supplements, blood clotting drugs and supplements, and sedative drugs and supplements. Berberine can also make some medicines less effective or augment their effects .
What are the side effects of taking Berberine?
Some possible side effects from Berberine include GI upset, especially if taken on an empty stomach, abdominal discomfort or distension, constipation, diarrhea, and nausea. To lessen some of the side effects, it is recommended to take Berberine with food and start slowly when taking it.
References
Bagade, A., Tumbigeremutt, V., & Pallavi, G. Berberine for Cardiovascular Benefits. Restorative Medicine. https://restorativemedicine.org/journal/cardiovascular-effects-berberine/
Cleveland Clinic. (2023, June 19). What to know about Berberine: Benefits, Uses, and Side Effects. Cleveland Clinic. https://health.clevelandclinic.org/berberine-for-insulin-resistance-weight-loss
Nykin, Linda. Berberine vs Berberine HCl: Understanding the Differences and Benefits. Pacha Integrative Med. https://www.pachaintegrativemed.com/blog/berberine-vs-berberine-hcl
Pizzorno, J., & Murray, M. (2021). Textbook of Natural Medicine: Fifth Edition: Volume 1. Elsevier.
