Berberine
“Dr. Nally, my blood sugar is great, but my metformin gives me chronic stomach bubbles and explosive diarrhea . . .”
85% of people who see me in the office have some degree of insulin resistance, impaired fasting glucose or diabetes. That means, they over produce insulin in response to any form of carbohydrate, starch or sugar. They will produce between two to 30 times the normal amount of insulin if they eat a piece of bread, cereal, oatmeal, cottage cheese or a bowl of pasta, for example.
The primary step I recommend for all of these patient is a carbohydrate restricted diet. This works well. However, there are other steps that can be taken that have tremendous health benefits.
If you are not using metformin prescribed by me or your doctor, then I will often recommend using berberine.
Berberine is an alkaloid you can find in several plants, including barberry, goldenseal, and Oregon grape. It is also available as a supplement in tablets or capsule form, as a powder, and as a liquid.
Berberine is available in several forms, including:
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Berberine HCL (hydrochloride):
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Berberine HCL, the most common form of berberine, is the least expensive form available. It is typically extracted and purified from bitter melon. It is just as effective as the other forms and this is the form that I personally use in my Berberine Plus formulation through Ketoliving.com.
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Berberine sulfate:
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Berberine sulfate is a water-soluble salt of berberine and is often used for medicinal purposes. It can be extracted from the roots of certain plants, including goldenseal.
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Berberine glucoside:
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Berberine glucoside is extracted from berberis vulgaris. This form of berberine is rarely used.
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How does berberine work?
Berberine is effective due to its targeting of adensine monophosphate-activated protein kinase (AMPK). This enzyme is important regulator of cellular energy and is involved in inflammation control, improving insulin resistance and slowing cellular aging or death. AMPK also affects the production of fatty acids and glucose metabolism, improving obesity and diabetes blood sugar control.
Berberine use leads to enhanced insulin signaling, glucose uptake and stabilizing blood glucose. This is the most important mechanism of berberine, and it works similar to Glucophage (metformin) without the GI side-effects like stomach upset and diarrhea.
In liver, berberine inhibit cholesterol and triglyceride synthesis. In the brain, it reduces malonyl-CoA, which is the first step to creating more mitochondria, the cell’s powerhouse, decreasing risk of dementia and slowing the aging process.
Berberine also activates AMPK indirectly by changing how hormones interact with receptors. This is achieved by reducing the activity of proteins such as protein kinase C (PKC) and AMP-activated protein kinase (AMPK). That’s how berberine improves insulin signaling.
Additionally, berberine prevents the activation of AMPK through glucose, which can also inhibit glucose uptake without leading to hypoglycemia. There is also an interaction with the testosterone receptors, improving testosterone in most men with hyperinsulinemia induced hypogonadism, and lowering abnormally high testosterone in women with poly-cystic ovarian syndrome (PCOS).
Berberine has the following positive outcomes when studied with the following conditions:
Cancer
Berberine has been shown to inhibit the growth of cancer cells and prevent them from spreading to other tissues. For instance, it is a promising solution for prostate cancer and benign prostatic hyperplasia. The mechanism of androgen receptor modulation found in berberine use can help reduce prostate growth triggered by testosterone.
It may also reduce the rate of testosterone synthesis in cancer cells, improving the outcome of castrate-resistant prostate cancer.
Diabetes
Berberine has been shown to lower blood sugar and improve insulin sensitivity in near identical levels to metformin. It regulates energy metabolism at different levels and in different tissues. Thus, both type 2 diabetes and metabolic syndrome patients can benefit from berberine supplementation.
Heart Disease
Berberine has been shown to improve blood flow and reduce cardiovascular disease risk factors, including plaque build-up in the arteries. That’s because other than a carbohydrate restricted diet, berberine is considered one of the best cholesterol supplement options.
Berberine reduces cholesterol levels in the blood and improves cardiovascular risk. Heart and circulation problems are common in males, and they may benefit significantly from berberine supplements to lower their risk.
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References:
- Vuddanda PR, et al. Berberine: a ptential phytochemical with multispectrum theraputic activities. Expert opinion on investigational drugs. 2010. 19910:1297-1307. https://pubmed.ncbi.nlm.nih.gov/20836620/
- Wang YX, et al. Sythesis and structure-activity relationship of berberine analogues in LDLR up-regulation and AMPK activation. Bioorgain & Medicinal Chemistry. 2012. 20(22):6552-6558 https://pubmed.ncbi.nlm.nih.gov/23058107/
- Li J, et al. Berberine Suppresses Androgen Receptor Signaling in Prostate Cancer: Berberine Downregulates Androgen Receptor. Molecular Cancer Therapeutics. 2011. 10(8): 1346-1356. https://pubmed.ncbi.nlm.gov/21613449/
- Xie L, et al. The effect of berberine on reproduction and metabolism in women with polycystic overy syndrome: a systematic review and meta-analysis of randomized control trials. Evidence-Based Complimentary and Alternative Medicine. 2019.
- Wang Y, Zidichouskin JA, Update on the benefits and mechanism of action of the bioactive vegetal alkaloid berberine on lipid metabolism and homeostasis. Choelsterol. 2018. https://pubmed.ncbi.nlm.nih.gov/30057809/