In the realm of natural medicine, berberine stands out as a potent phytochemical with a rich history and an impressive array of therapeutic properties. Derived from a variety of plants like Oregon grape root, barberry root and berry, Isatis, coptis, and goldenseal root, berberine is a powerhouse for the immune system and metabolism.
Since it’s my pet peeve when people refer to berberine as an herb, allow me to explain what exactly it is and where it comes from, as well as traditional and science-backed indications for its use.
What is Berberine?
Berberine is in fact, not a plant, but a bioactive substance that possesses potent antioxidant and anti-inflammatory properties, providing numerous health benefits. It is an isoquinoline alkaloid (phytochemicals found in a number of plants) with a bright yellow color and bitter taste, with a bright yellow color and bitter taste, found in plants belonging to the Berberidaceae family (and some related families).
Famously sourced from goldenseal (though I would recommend staying away from wild harvested since it’s on the UPS endangered list currently), it was first isolated from Xanthoxylon cava (Southern Prickly Ash) in 1826.
It is commonly found in the root, rhizome, and stem bark of the Chinese herb Coptis chinensis and other Berberis plants [1]. For centuries, berberine has been used in Ayurvedic and traditional Chinese medicine (TCM) to treat various ailments. The plants that contain berberine are not only admired for their beauty but also their strong medicinal properties [2].
The benefits of berberine include its ability to fight inflammation, aid in diabetes, support weight loss, lower cholesterol, and regulate blood pressure. Berberine has been used in traditional medicine for its antimicrobial and antiprotozoal properties, and its use is encouraged for the treatment of chronic disorders due to its potential to offer a safer alternative to synthetic drugs [3]. Current clinical research supports berberine’s various pharmacological properties and multi-spectrum therapeutic potential.
Health Benefits of Berberine
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Metabolic Regulation:
Berberine plays a crucial role in regulating glucose and lipid metabolism through various mechanisms, including the inhibition of mitochondrial glucose oxidation and stimulation of glycolysis, which leads to increased glucose metabolization. This effect is particularly important for individuals managing conditions like type 2 diabetes mellitus. Studies have shown that berberine can improve glucose metabolism and have a good impact on HbA1c levels just as well as more conventional medications like metformin, currently first line in treatment (and having itself been derived from Gallega officinalis plant originally, but that’s for another post) [4].
Berberine’s ability to enhance glucose metabolism by stimulating glycolysis and increasing glucose uptake independently of insulin makes it a promising natural compound for managing metabolic disorders, especially diabetes.
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Liver and Kidney Protection:
Berberine is known for its hepatoprotective and nephroprotective properties, contributing to its appeal in holistic health circles. By maintaining liver function and protecting renal health, berberine supports the body’s natural detoxification processes and promotes overall well-being. Studies have shown that berberine can protect the liver and kidneys against toxicity induced by compounds like ferrous sulfate (aka the iron form found in supplements), which can cause functional disorders and histological damage [5]. This protection is mediated through berberine’s ability to reduce lipid peroxidation and chelate iron.
Furthermore, berberine has been found to have antifibrotic effects in the liver, kidney, and lung, suggesting its potential to protect these organs from damage and dysfunction. The nephroprotective effects of berberine have been particularly notable in the context of diabetic nephropathy, where it was found to attenuate renal fibrosis and improve kidney function in diabetic mice through the activation of the AMPK pathway [6].
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Immunomodulatory Effects:
Berberine exhibits immunomodulatory effects that contribute to its multifaceted benefits by enhancing the body’s ability to combat infections and maintain a balanced immune response. This is especially valuable in the context of the prevalent autoimmune and chronic diseases in today’s world.
Berberine has been shown to suppress inflammatory responses, inhibit the differentiation of pro-inflammatory Th1 and Th17 cells, modulate the balance between Treg and Th17 cells, and enhance cell-mediated immunity. These mechanisms collectively indicate berberine’s potential to ameliorate destructive autoreactive inflammation in autoimmune conditions while enhancing the body’s immune defenses [7].
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Antioxidant and Anti-inflammatory Properties:
Berberine’s antioxidant and anti-inflammatory activities contribute to its holistic impact on health, allowing it to combat oxidative stress and inflammation – key drivers of numerous chronic and autoimmune diseases.
Berberine has been shown to inhibit oxidative stress in a variety of tissues, including the liver, adipose tissue, kidney, and pancreas. It achieves this through mechanisms involving cellular kinases and signaling pathways like AMPK, MAPKs, and the Nrf2 pathway. By reducing oxidative stress, berberine can help combat the development and progression of numerous chronic diseases [8].
Berberine exhibits potent anti-inflammatory effects by inhibiting the activation of inflammatory factors like iNOS, COX-2, IL-1, IL-6, and NF-κB. Berberine’s ability to suppress inflammation makes it a valuable therapeutic for inflammatory diseases [9].
The Science Behind Berberine
Glycolysis Stimulation: By promoting the metabolization of glucose through enhanced glycolysis, berberine ensures that sugar levels in the blood are regulated efficiently.
Inhibition of DPP4: Berberine has been shown to inhibit Dipeptidyl Peptidase-4 (DPP4), an enzyme involved in glucose metabolism that breaks down natural incretin hormones such as Glucagon-like peptide 1. Research indicates that berberine inhibits human DPP4, as evidenced by its ability to fit within the binding pocket of DPP4 and inhibit the enzyme in vitro with an IC50 of 13.3 microM [10]. This inhibition of DPP4 can lead to increased effects of endogenous GLP-1 peptides, increased insulin levels and anti-hyperglycemic effects. There is a category of pharmaceutical drugs on the market that have this mechanism of action, such as Januvia (sitagliptin).
Lipid Lowering Effects: Research indicates that berberine can significantly reduce lipid levels, including triglycerides and plasma-free fatty acids, thus supporting cardiovascular health [11][12].
Incorporating Berberine into Your Health Regime
Integrating berberine into one’s diet involves understanding its potency and potential interactions with other medications. As with any potent herbal medicine, consultation with a healthcare provider, particularly those familiar with both allopathic and herbal medicine, is essential.
With its wide range of health advantages, berberine is a gem among natural supplements, offering a comprehensive approach to wellness that is in harmony with the body’s natural functions. Berberine is an option to improve health and wellbeing organically, regardless of your medical background—a medical practitioner seeking to broaden their knowledge of herbal remedies, or a health enthusiast keen to capitalize on the advantages of herbs.
Remember, it is an isolated phytochemical, which gives it a more concentrated and potent pharmacology and mechanism of action. If you’re looking for a more holistic approach, I’d recommend utilizing whole plant medicine from berberine-containing herbs, such as Oregon grape root or barberry (which is a ubiquitous weed here in the Northeast!).
If you’d like to know more about berberine and how it may fit into your daily health routine, leave a comment below.
**For specific vitamin/mineral complex recommendations, I’ve curated my top picks in my herbal dispensary here.**
References:
- Biological properties and clinical applications of berberine | Frontiers of Medicine
- Berberine: Botanical Occurrence, Traditional Uses, Extraction Methods, and Relevance in Cardiovascular, Metabolic, Hepatic, and Renal Disorders
- Berberine: a potential phytochemical with multispectrum therapeutic activities
- Berberine improves glucose metabolism through induction of glycolysis
- Berberine protects the liver and kidney against functional disorders and histological damages induced by ferrous sulfate
- Therapeutic Effects of Berberine on Liver Fibrosis are associated With Lipid Metabolism and Intestinal Flora – PMC
- Anti‐inflammatory and immune‐modulatory impacts of berberine on activation of autoreactive T cells in autoimmune inflammation – PMC
- Antioxidant and Anti-Inflammatory Activities of Berberine in the Treatment of Diabetes Mellitus – PMC
- Advances in the study of berberine and its derivatives: a focus on anti-inflammatory and anti-tumor effects in the digestive system | Acta Pharmacologica Sinica
- Inhibition of dipeptidyl peptidase IV (DPP IV) is one of the mechanisms explaining the hypoglycemic effect of berberine
- Efficacy of Berberine Alone and in Combination for the Treatment of Hyperlipidemia: A Systematic Review
- Therapeutic Potential and Mechanisms of Berberine in Cardiovascular Disease | Current Pharmacology Reports
