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Berberine - Nature’s Natural Blood Sugar Regulator And More

By Max Cerquetti November 01, 2020

Berberine (say “BUR-bur-reen”) is a natural plant compound with multiple medicinal effects, such as the regulation of blood sugar, that are so powerful, some physicians prefer it over manufactured pharmaceuticals. The compound itself is found in a variety of plants that are found worldwide, including Oregon grape, European Barberry, Tree Turmeric, Phellodendron (also known as Cork Tree and not to be confused with the houseplant Philodendron), as well as Goldenseal and Goldthread.

 

Berberine has been used successfully for literally thousands of years in traditional Chinese medicine and was first mentioned in an ancient Chinese medical text, the Shennong Bencaojing or The Classic of Herbal Medicine, written between 200 and 250 CE. This plant compound is a gorgeous golden yellow and has also long been used as a valuable natural dye, specifically for coloring wool.

Besides berberine’s effectiveness as a regulator of blood sugar, it also has powerful antimicrobial and anti-inflammatory effects, it lowers blood pressure and cholesterol levels, enhances beneficial gut bacteria, and even has anti-aging properties among many other benefits. One might legitimately ask how just one compound could have such wide-ranging effects on so many varying bodily systems?


AMPK - The Master Energy Sensor 

 

To understand the far reaching effects of berberine you have to look closely at an enzyme found in your body called AMPK which stands for adenosine monophosphate-activated protein kinase. An enzyme is a protein that works to help speed up certain vital chemical reactions in your body that without the enzyme, simply would not be able to occur.

 

AMPK activation and autophagy in macrophages, ECs and VSMCs

 

AMPK activation and autophagy in macrophages, endothelial cells (ECs) and vascular smooth muscle cells (VSMCs).

AMPK activators such as Berberine induce macrophage autophagy via the PI3K/Akt/mTOR signaling pathway. The expression of pro-inflammatory cytokines (IL-1β, IL-6 and TNF-α) is down-regulated and expression of the anti-inflammatory cytokine (IL-10) expression is up-regulated. Therefore, inflammation, macrophage aggregation and oxidative stress are inhibited, and cell survival and plaque stability increased. AMPK activation and autophagy in ECs induce NO production, promote cell survival, and decrease
oxidative stress and the inflammatory response. AMPK activation and autophagy also promote cell survival and vasodilatation, inhibit cell migration and proliferation, and decrease neointima formation and vascular calcification in VSMCs.

 


AMPK is found in every cell in your body and can be thought of as an energy “switch” or even the master energy sensor. Find a way to activate AMPK and you’ve found a way to reduce dangerous abdominal fat as well as lower harmful inflammation. The activity of AMPK not only influences your body fat composition, but even has an influence on how long you will live! AMPK regulates multiple metabolic pathways that keep blood glucose, blood lipid levels and cellular energy pathways normalized.

 

Berberine effects on DNA Synthesis and Replication, Cell Cycle, Autophagy, Senescence and Apoptosis.

 

Pleiotropic effects of berberine on signalling pathways involved in cell growth.

Berberine can induce many pathways which may result in suppression of cell growth, induction of apoptosis, autophagy, senescence, DNA double strand breaks or inhibition of cell cycle progression and DNA replication. These events are indicated by red arrows. In addition, Berberine treatment can result in the suppression of many important proteins leading to decreased growth, decreased DNA synthesis, mitochondrial membrane potential, cell cycle arrest and inflammation indicated in black closed arrows.

 

 

But there is a problem. As you age, the levels of AMPK in your body naturally decline, and along with it, you are apt to put on pounds around your abdomen. Unlike the fat that accumulates in other areas, abdominal fat or “visceral” fat as it is sometimes called, produces dangerous hormones that accelerate the aging process and can even increase your risk of heart disease. 

 

When these critical AMPK influenced pathways are switched off due to decreasing AMPK levels, a disorder known as metabolic syndrome can be triggered. Metabolic syndrome is a highly dangerous condition that includes diabetes, blood lipid elevations, high blood sugar and high blood pressure. 

 

Treating patients who have metabolic syndrome is quite complicated and usually requires three to five different medications, all with various side effects, to manage all the different aspects of this syndrome. In fact, scientists have proposed research to develop a single drug that would target the activation of AMPK to replace all of these drugs with just one. 

 

One of the other ways that activation of AMPK can help to slow and even reverse biological aging is its role in the process of autophagy (say “aw-TOPH-ah-gee”), a normal process that your cells use to clear out metabolic waste products, mitochondria that are no longer functioning properly, damaged proteins and viruses. As you age, autophagy declines and premature aging accelerates. But research has shown that boosting AMPK can help to increase autophagy.

 

Berberine, AMPK and Autophagy

But back to berberine. While some drugs, such as the diabetes drug metformin, as well as exercise, and calorie restriction activate AMPK, so does berberine. It is this AMPK activation that explains many of berberine’s far reaching positive effects across so many different metabolic conditions. 

 

In addition to the treatment of Type 2 diabetes, berberine has powerful anti-inflammatory effects. Inflammation is thought to be a major underlying factor in a wide range of modern maladies, including heart disease, Type 2 diabetes, some auto-immune disorders and yes, even cancer, Alzheimer’s and other neurodegenerative diseases. 

 

There has been a resurgence of interest in the berberine’s potential to treat and even protect against neurodegenerative diseases, as berberine has been found to cross the blood-brain barrier and has neuroprotective effects in both cell and animal models of Alzheimer’s, Parkinson’s and Huntington’s disease, all devastating illnesses, both for patients as well as their families. Again, the efficacy of berberine in these illnesses is likely due to AMPK activation as well as the enhancement of autophagy, as autophagy is known to clear out the mis-folded proteins that are thought to play a role in the plaques that form in the brains of patients with Alzheimer’s disease.

 

Chronic inflammation has been shown to play a major role in the development of some cancers. Not only could the treatment of inflammation prevent the development of cancer, in those patients who have already been diagnosed, the simultaneous treatment of both the cancer and the underlying chronic inflammation shows significant therapeutic potential. Berberine has both anti-tumor and anti-inflammatory effects and shows great promise in this area.

 

Using Berberine To Increase AMPK Levels, Decrease Inflammation and Increase Autophagy

In light of the clinical evidence for the effectiveness of berberine in both the treatment and prevention of a wide range of human disease, it makes sense to consider supplementation with a high quality berberine product. Because berberine is not well absorbed, there is concern about its bioavailability, so you want to look for a product that has added piperine (a black pepper extract) which has been proven to increase berberine’s absorption. The addition of grape seed extract is a plus as well, as this compound works to lower blood sugar and is also a good source of antioxidants, which can help to lower inflammation.

 

You can find more information about our berberine supplements here, including information on our other supplements such as NAD+, NMN, resveratrol and others. Taken daily, our potent bioavailable berberine supplement is powerful protection against the effects of the aging process as well as the dangerous effects of chronic inflammation.

 

 

References:

 

Wang J, Wang L, Lou GH, et al. Coptidis Rhizoma: a comprehensive review of its traditional uses, botany, phytochemistry, pharmacology and toxicology. Pharm Biol. 2019;57(1):193-225. doi:10.1080/13880209.2019.1577466
Hardie DG. AMPK: a key regulator of energy balance in the single cell and the whole organism. Int J Obes (Lond). 2008;32 Suppl 4:S7-12.

Salminen A, Kaarniranta K. AMP-activated protein kinase (AMPK) controls the aging process via an integrated signaling network. Ageing Res Rev. 2012;11(2):230-41.

Rubinsztein David C, Mariño G, Kroemer G. Autophagy and Aging. Cell. 2011;146(5):682-95.

Madeo F, Zimmermann A, Maiuri MC, et al. Essential role for autophagy in life span extension. Journal of Clinical Investigation. 2015;125(1):85-93.

Yin J, Xing H, Ye J. Efficacy of berberine in patients with type 2 diabetes mellitus. Metabolism. 2008;57(5):712-717. doi:10.1016/j.metabol.2008.01.013

Zhang J., Yang J.Q., He B.C., Zhou Q.X., Yu H.R., Tang Y., Liu B.Z. Berberine and total base from rhizoma coptis chinensis attenuate brain injury in an aluminum-induced rat model of neurodegenerative disease. Saudi Med. J. 2009;30(6):760–766.

Habtemariam S. The therapeutic potential of Berberis darwinii stem-bark: Quantification of berberine and in vitro evidence for Alzheimer’s disease therapy. Nat. Prod. Commun. 2011;6(8):1089–1090.

Fan D, Liu L, Wu Z, Cao M. Combating Neurodegenerative Diseases with the Plant Alkaloid Berberine: Molecular Mechanisms and Therapeutic Potential. Curr Neuropharmacol. 2019;17(6):563-579. doi:10.2174/1570159X16666180419141613

Crusz SM, Balkwill FR. Inflammation and cancer: advance and new agents. Nat Rev Clin Oncol2015; 12: 584–96.


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