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Berberine molecular structure

Berberine Supplement Benefits

Are you considering a berberine nutritional supplement to support your health? Lately, berberine has gained significant attention owing to its significant nutritional support benefits. So, is it worth the hype to be included in your diet? Get all the answers to common queries about the benefits of berberine nutritional supplements, including how berberine supplements promote various health functions and the best way to include one in your diet. Use the links below to jump ahead to different topics on the page.

Table of Contents
What Is Berberine and Where Is It Found?Potential Applications of Berberine
How Does Berberine Support Glucose Metabolism?How Does Berberine Promote Immune Health?
Factors Affecting Berberine AbsorptionWhy Do You Need A Berberine Supplement?
Berberine Supplement FormulationsFAQs: Frequently Asked Questions

What Is Berberine and Where Is It Found?

Berberine is a phytochemical, an alkaloid that is extracted from the roots, rhizomes, and stem bark of barberry trees, including Berberis vulgaris (barberry), Berberis aristata (tree turmeric), Berberis aquifolium (Oregon grape), and others. Berberine is known for its antioxidant properties and the ability to help maintain a balanced inflammatory response in the body.* Extracts and decoctions of berberine have been traditionally used in Ayurveda and Chinese medicine. 

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Potential Applications of Berberine

Recent studies have associated the beneficial effects of berberine with positive changes in oxidative stress markers, antioxidant enzymes, and the proinflammatory cytokines that are involved in the up-regulation of inflammatory processes. The therapeutic potential of berberine lies in its antioxidant and immunomodulatory properties. 

  • Antioxidant property of berberine: Berberine mitigates oxidative stress — the imbalance in the internal environment when there are insufficient antioxidants to eliminate free radicals.* Berberine has been found1 to remediate oxidative stress through various biochemical pathways and increases the amounts of glutathione (GSH) and the antioxidant enzymes superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) that help scavenge excessive free radicals.*
  • Immunomodulatory property of berberine: Berberine plays a critical role in down-regulating the production of those proinflammatory cytokines that can cause unbalanced inflammatory responses.* Berberine also influences acute phase proteins — the plasma proteins whose concentrations fluctuate during inflammatory responses.*   

The following table summarizes the potential beneficial applications of berberine.  

System Beneficial Applications
Endocrine Health*
Immune Health*
  • Berberine vs. Turmeric: Which is Right for You?
Hepatic Health*
  • Berberine’s Liver Detox Benefits
Neuro-Hormonal System*

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How Does Berberine Support Glucose Metabolism? 

There has been extensive research investigating berberine’s glucose support properties. Although the mechanism of berberine’s action on glucose metabolism is not fully understood, studies have shown berberine’s role in promoting glucose and lipid metabolism.* 

Berberine and Glucose Homeostasis
Promoting Insulin Secretion and Addressing Insulin Resistance*   As an antioxidant, berberine protects the insulin-producing cells in the pancreas.* It promotes insulin secretion and reduces insulin resistance through various cellular signal transduction pathways, such as the cyclic adenosine monophosphate (cAMP) pathway.*  
Stimulating Glucose Breakdown*Berberine-induced activation of signaling pathways and stimulates2 the break down of glucose into pyruvic acid, thereby releasing energy.*
Inhibiting Glucose Synthesis from Non-carbohydrate Components* Berberine regulates mitochondria-related pathways to inhibit glucose synthesis from non-carbohydrate components in liver cells.*
Limiting Digestion of Carbohydrates in the Intestine*By limiting carbohydrate digestion in the intestine, berberine inhibits intestinal absorption of glucose.* 
Promoting Lipid Metabolism*Insulin is integral to lipid metabolism as it promotes cholesterol biosynthesis and uptake. Berberine is a known activator of adenosine monophosphate-activated protein kinase (AMPK) that contributes3 to fatty acid oxidation and limits lipid accumulation, particularly that of low-density lipoprotein cholesterol (LDL-C).* 

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How Does Berberine Promote Immune Health?

Berberine supports a healthy immune response in multiple tissues, including adipose tissues, the liver, the kidneys, and the pancreas.* It exerts immuno-modulatory effects through several cellular kinases and signaling pathways* that still need further investigation. Berberine particularly interacts with T-helper cells of the immune system to help maintain a healthy inflammatory response.*  

  • Directly modulating function and differentiation of Th cells: Berberine directly suppresses the functioning and differentiation of Th1 and Th17 cells — subsets of T helper cells that contribute to optimal immune function.*
  • Indirectly affecting Th-cell-mediated inflammation: Berberine can also indirectly benefit Th-cell-mediated immune responses by suppressing or modulating the actions of other immune cells, such as macrophages and dendritic cells.*    

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Factors Affecting Berberine Absorption in the Body

The wide application of berberine is greatly restricted due to its poor intestinal absorption. The following are several of the key factors4 affecting berberine’s absorption in the body.

  • Physicochemical Property: Berberine is a hydrophilic compound with a  temperature-dependent aqueous solubility that increases with a rise in temperature. It is mostly lipophobic with poor membrane permeability.
  • Intestinal First-Pass Elimination: Berberine undergoes intestinal first-pass elimination — the pre-systemic metabolism of berberine before it reaches systemic circulation.
  • Degradation in Liver: Berberine degrades and undergoes phase I transformation in the liver, producing four major metabolites. 
  • Efflux to Intestinal Lumen: Under the action of permeability glycoprotein (P-glycoprotein), berberine is effluxed back to the intestinal lumen to be excreted out of the body.  

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Unformulated Berberine versus Berberine Supplement Benefits

Unformulated berberine poses three key challenges that impact its efficacy:

  • Intolerable taste: Berberine has an intensely bitter taste. Its chloride salt, a common ingredient of commercially-available berberine supplements, has high aqueous solubility, making it difficult to mask its taste.  
  • Intake in high amounts: Ingesting a high amount of berberine to address its low bioavailability can result in gastrointestinal adverse events, such as upset stomach, cramping, diarrhea, etc.  
  • Poor absorption: Poor absorption means your body does not experience the desired beneficial effects of berberine. 

More recent berberine supplement formulations address these shortcomings of unformulated berberine to optimize its absorption and efficacy. 

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Berberine Supplement Formulations

Most commercially available berberine supplement formulations contain 400-500 mg of berberine per capsule, with berberine hydrochloride (BH) being the primary ingredient. Berberine supplements are usually in the form of tablets, capsules, and fluid extracts.  

Compared to unformulated berberine, supplement formulations use innovative approaches, such as nanotechnology, to enhance berberine’s palatability and bioavailability to make it a therapeutic reality. However, the safety and efficacy of berberine greatly vary depending on the type of formulation. 

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FAQs: Frequently Asked Questions About Berberine Nutritional Supplements 

Are there side effects to taking a berberine supplement?

Clinical studies have established that berberine is safe and well-tolerated. However, side effects such as flatulence, nausea, constipation, and diarrhea can occur. In rat studies, no adverse side effects of berberine on kidney or liver functions were reported.  

Can I take a berberine supplement with a prescription medicine?

It is always recommended to consult with your healthcare provider before including a berberine supplement in your diet or taking it with a prescription medicine.   

How do I determine the efficacy of a berberine supplement?

The efficacy of a berberine supplement lies in enhanced palatability, bioavailability, and absorption of the active nutrient molecules. Tesseract’s BerberActiv®, an innovative, hypoallergenic, berberine supplement formulation achieves optimal absorption of the active ingredient while enhancing its palatability to achieve patient compliance.    

The proprietary CyLoc® - DexKey® nutrient delivery nanotechnology ensures unprecedented absorption of berberine molecules in the intestinal tract — one molecule at a time to maximize berberine supplement benefits. The CyLoc® matrix encases each berberine molecule in its smart delivery system and masks the bitterness of berberine. The DexKey® reactors release each molecule at the desired point in the intestinal tract to achieve maximum absorption. Enhanced absorption enables micro-dosing — the ingestion of a lesser amount of berberine to achieve a powerful and rapid physiological response.  

With better delivery of berberine to the body tissues, BerberActiv® supports blood glucose metabolism and lipid metabolism, optimal gastrointestinal and cardiovascular health, healthy weight management, and healthy inflammatory and immune responses.*    

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The power of Tesseract supplements lies in enhancing palatability, maximizing bioavailability and absorption, and micro-dosing multiple nutrients in a single, highly effective capsule. Shop products on our website and learn more about how they can help support your immune health.* 

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1Li Z, et al. Antioxidant …activities of berberine... Evidence-based complementary and alternative medicine 2014:289264. doi:10.1155/2014/289264

2Yin J, et al. Berberine improves glucose metabolism…. American journal of physiology. Endocrinology and metabolism 2008;294(1):E148-E156. doi:10.1152/ajpendo.00211.2007

3Rong Q, et al. Berberine reduces lipid accumulation by promoting fatty acid oxidation …. Frontiers in pharmacology 2022;12:729384. doi:10.3389/fphar.2021.729384

4Habtemariam S. The quest to enhance the efficacy of berberine…. Biomedicines 2020;8(4):90. doi:10.3390/biomedicines8040090

Al Czap, Founder | Tesseract

Al Czap has more than four decades of professional experience in preventative medicine. He founded Thorne Research in 1984 (sold in 2010) and he published Alternative Medicine Review for 17 years beginning in 1996. AMR was a highly acclaimed, peer-reviewed, and indexed medical journal. Al was the first to recognize the need for hypoallergenic ingredients and to devise methods of manufacture for and delivery of hypoallergenic products to underserved patient populations. His work has greatly impacted those with impaired immune and digestive systems and compromised health due to environmental exposures.

The advanced formulations based on our revolutionary, patented, and patent-pending technology are only available through Tesseract. No other medical, pharmaceutical, or supplement company is licensed to utilize our proprietary technology.
*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.
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