Berberine – The Game Changer for Diabetes?

17 Dec 2019 10:16 AM | Aliya Umm Omar (Administrator)

If you’re looking at natural ways to control your diabetes then consider this herbal compound. Berberine is fast becoming the go-to supplement to take for type-2 diabetes with very few side effects when compared with modern medicine. Here’s the scoop on this little-known, yet powerful supplement.

Berberine is a bioactive compound that can be extracted from several different plants, including a group of shrubs called Berberis. It is also present in other plants, including goldenseal, barberry, Oregon grape, and tree turmeric. It is found in the roots, rhizomes, stems, and bark of these plants. 

The oldest evidence of using barberry fruit as a blood purifying agent was written on the clay tablets in the library of Assyrian emperor Asurbanipal during 650 BC. It is a popular component in many traditions, such in Ayurvedic and Chinese Medicine with more than 3000 years of history. In Ayurveda, Berberis species have been traditionally used for the treatment of a wide range of infections of the ear, eye, and mouth, for quick healing of wounds, curing haemorrhoids, indigestion and dysentery. It has also been used to reduce obesity, and as an antidote for the treatment of scorpion sting or snakebite. Berberine extracts and decoctions are traditionally used for their activities against a variety of microorganisms including bacteria, viruses, fungi, protozoa, in Ayurvedic, Chinese, and Middle-Eastern folk medicines.

Technically, Berberine belongs to a class of compounds called alkaloids. It has a yellow colour, and has often been used as a dye. Its strong yellow colour and yellow fluorescence made it a widely used dye in early days of the industry. It’s still used today in India as a wool dye, and its fluorescence makes it useful as a histology stain.


Berberine Benefits

Berberine is known as a very important natural alkaloid for the synthesis of several bioactive derivatives. After you ingest berberine, it gets taken in by the body and transported into the bloodstream where it travels into the body’s cells. Inside the cells, it binds to several different “molecular targets” and changes their function. This is similar to how pharmaceutical drugs work.

Regulates Metabolic Pathways

One of the main actions of berberine is to activate an enzyme inside cells called adenosine monophosphate-activated protein kinase (AMPK). This enzyme is sometimes referred to as a “metabolic master switch”. It is found in the cells of various organs, including the brain, muscle, kidney, heart and liver. This enzyme plays a major role in regulating metabolism:

1.      The AMPK system senses and responds to changes in energy metabolism both on the cellular and the whole-body level. It acts as the central energy control switch regulating how energy is produced and used in the body. It induces a cascade of events within cells that are all involved in maintaining energy balance. 

2.      AMPK regulates an array of biological activities that normalise lipid, glucose, and energy imbalances (metabolic syndrome occurs when these AMPK-regulated pathways are turned off, triggering a syndrome that includes hyperglycemia, diabetes, lipid abnormalities, and energy imbalances).

3.      AMPK helps shift energy towards cellular repair, maintenance, or balance.

Only a few chemicals are known to activate AMPK. Berberine is one of them. Reports that berberine activates AMPK were first published in 2006. Resveratrol, salicylate, and metformin also activate this chemical pathway.

Lowers Blood Glucose Levels

Many studies show that berberine can significantly reduce blood sugar levels in individuals with type 2 diabetes. In fact, its effectiveness is comparable to the popular diabetes drug metformin (Glucophage). Berberine triggers AMPK activation which works by:

·        Decreasing insulin resistance, making the blood sugar lowering hormone insulin more effective.

·        Increasing glycolysis, helping the body break down glucose inside cells.

·        Decreasing glucose production in the liver.

·        Slowing the breakdown of carbohydrates in the gut.

In one study of 116 diabetic patients, 1 gram of berberine per day lowered fasting blood sugar by 20%, from 7.0 to 5.6 mmol/L (126 to 101 mg/dL), or from diabetic to normal levels. It also lowered haemoglobin A1c by 12% (a marker for long-term blood sugar levels).

Berberine VS Metformin

Metformin activates AMPK to a similar degree as berberine, and as a result, they affect metabolism similarly. So it should be no surprise that, like metformin, berberine appears useful for treating type-2 diabetes.

The hypoglycemic effect of berberine was similar to that of metformin when patients newly diagnosed with type-2 diabetes who were randomly treated to take either berberine or metformin (500 mg 3 times a day) in a 3-month trial. 

A meta-analysis combined data from 14 randomised trials involving 1,068 participants. Treatment with both berberine and metformin showed similar hypoglycemic and antidyslipidemic benefits.

Berberine has been studied and shown to be effective in treating other conditions that respond to metformin, such as when used to treat women with polycystic ovary syndrome (PCOS) or when used to reduce insulin resistance in ovarian theca cells and decrease their excessive testosterone production.

Promotes Weight Loss

While berberine is far from a “miracle” weight loss drug, research shows that it can help lead to weight reduction in those with obesity. In a 12-week study in obese individuals, 500 mg berberine taken three times per day caused about 2 kg of weight loss, on average. The participants also lost 3.6% of their body fat. 

Berberine helps improve insulin sensitivity and normalises blood glucose levels, while also helping to regulate the hormones that control appetite and satiety. It also works to speed up metabolism from inside each individual cell.

In one study berberine helped people drop from obese to overweight in just three months by reducing belly fat and improving overall health markers. This study relied on 300 mg berberine, three times daily, for three months. The researchers believe that the weight loss was caused by improved function of fat-regulating hormones, such as insulin, adiponectin and leptin.

Berberine also appears to inhibit the growth of fat cells at a molecular level. However, more research is needed on the weight loss effects of berberine.

Lowers Cholesterol

Berberine can help to lower blood lipids like LDL cholesterol and triglycerides, which, when elevated, can lead to heart disease, stroke, and many other inflammatory conditions. According to some studies, berberine works by inhibiting an enzyme called PCSK9. This leads to more LDL being removed from the bloodstream.

While cholesterol in and of itself isn’t a bad thing – it is used to transport nutrients in the body. However, when LDL cholesterol becomes oxidised, it is associated with plaque build-up in the arteries and heart disease.

Berberine has also been shown to lower apolipoprotein B which is a very important risk factor of cardiovascular disease.

Improves Heart Health

Berberine works to reduce the risk of cardiovascular disease, while also promoting normal blood pressure and defending against plaque build-up in the arteries, irregular heartbeat and even heart failure. (12, 13) When compared to medications aimed at lowering both systolic and diastolic levels, berberine wins.

Improves Gut Bacteria

Berberine is antimicrobial, making it great for the digestive system and microbiome. In particular, berberine can help to destroy the ulcer-forming bacteria H. pylori when taken twice daily for six weeks. It can also be used to fight other types of bacteria and fungi, such as staph and candida.

Supplementing with berberine can also modulate “bad” gut bacteria, which can have destructive effects on the body like insulin resistance, diabetes, and obesity. It is also helpful in cases of SIBO, or small intestinal bacterial overgrowth, and can work as an antibiotic treatment without the gut-disrupting side effects.

Berberine has shown promise in numerous other health benefits:

Depression: Studies show that it may help fight depression by increasing the neurotransmitters that produce a stable, regulated mood: serotonin and dopamine.

Cancer: Test tube and animal studies have shown that it can reduce the growth and spread of various different types of cancer.

Antioxidant and anti-inflammatory: It has been shown to have potent antioxidant and anti-inflammatory effects in some studies.

Fatty liver: It can reduce fat build-up in the liver, which should help protect against non-alcoholic fatty liver disease.

Many of these benefits need more research before firm recommendations can be made, but the current evidence is very promising.

Berberine Absorption and Bioavailability in the Body:

Berberine supplements were initially thought to be poorly absorbed across the gut wall. Pharmacokinetic researchers have found low plasma concentrations which could not exert the remarkable pharmaceutical effects mentioned. However, it now appears that the situation is more complex; berberine actually appears to be well absorbed. The confusion lies in the fact that it is quickly metabolised. Blood clearance is so fast and biotransformation in the liver so rapid that berberine disappears from the blood faster than it can be measured. 


Precautions

Berberine is not known to have serious side effects. The main side effects are related to digestion, and there are some reports of cramping, diarrhoea, flatulence, constipation and stomach pain. Having said this, berberine isn’t safe for long-term use. It’s also not safe for women who are pregnant or breastfeeding, children, or for people who are taking blood thinners, antibiotics, antidepressants, or any medication aimed at lowering glucose or insulin levels. Always take berberine with a meal to avoid an upset stomach and to improve its effectiveness.

The AMPK activation effects of berberine are incredible at improving blood glucose control and reducing blood lipids, but at the same time it could inhibit muscle growth. 

If you have a medical condition or are on any medications, then it is highly recommended that you speak to your doctor before taking it.

Dosages for Health

Berberine can be found in a few different forms, but the highest quality is known as “berberine HCL”. It can be found in health food stores or online retailers that sell supplements. 

To be effective, berberine needs to be taken two or three times daily, spread out, because it has a short half-life and will not remain in the bloodstream if you only take it once a day. 

Many of the studies cited uses dosages in the range of 900 to 1500 mg per day. Therefore, taking 300 - 500 mg, 3 times per day, with meals.

To Sum Up…

Berberine is one of the very few supplements that are as effective as a pharmaceutical drug. It has powerful effects on various aspects of health, especially blood glucose control and works as well as the ever-popular glucose-lowering drug ‘Metformin’. It does this by triggering the activation of the enzyme AMPK into increasing the breakdown of glucose in cells which leads to decreased insulin resistance. In fact, what makes berberine so special is that it is one of the very few compounds that actually has an effect on such a powerful enzyme. AMPK is involved in an array of biological functions in the body and switching it on means it shifts energy towards normalising lipid, glucose and other imbalances which helps to repair cellular damage and maintain cellular function for long term survival. In other words, activating AMPK could, theoretically, produce the same benefits as exercise, dieting, and weight loss.

Research is being undertaken to determine the effectiveness of using the AMPK-enzyme activator berberine to combat metabolic syndrome which causes all the major symptoms of diabetes (hyperglycaemia), high blood pressure (hypertension), high cholesterol (hyperlipidaemia), and inflammation, in one supplement!

Berberine can help improve heart health and gut bacteria and is showing promise in other conditions such as cancer, depression, and other neuropsychiatric diseases. However, it does interact with certain medications and is not suited for vulnerable individuals. If you are considering on supplementing with berberine please do your own research and consult your health professional first.

Sources

https://www.acs.org/content/acs/en/molecule-of-the-week/archive/b/berberine.html

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6111450/

https://selfhacked.com/blog/berberine-19-health-benefits-of-berberine-with-references/

https://www.medicalnewstoday.com/articles/325798.php

https://www.healthline.com/nutrition/berberine-powerful-supplement

https://www.ncbi.nlm.nih.gov/pubmed/10767672

https://www.naturalmedicinejournal.com/journal/2012-12/clinical-applications-berberine

https://www.precisionnutrition.com/surprising-supplements

https://blog.paleohacks.com/berberine/#

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