Can Berberine Aid Fat Loss, And Replace Diabetic Medication? The Facts

Berberis_vulgarisTraditional medicine is an interesting thing to research, not only due to the scientific side of things, but also due to geography. In the past, an herb discovered in Thailand would slowly make its way to China if it was incredible, but unlikely to make it to Europe (and forget about it making its way to the Americas). Conversely, medicinal plants from Europe rarely reach eastern Russia or China. Due to this, different locations have different cures for the same diseases and conditions.

Something to note is that a lot of medicinal plants, while being technically different plants, tend to share the same bioactives. For example, many edible berries belong to the genus vaccinium and they all tend to be high in polyphenols. The same principle applies to the multitude of mulberries and the hawthorn berries – while different, many of them share the same medicinal properties.

This article is about a compound that is found in a lot of different herbs. Traditionally, these herbs have been used for anti-diabetic properties and intestinal health. These herbs are found in a variety of traditional medicines (remember as we mentioned – not a lot of mixing happens in traditional medicines), and this compound is the common thread.

Today, we’re highlighting berberine, a supplement that is actually underrated (truly hard to find those). Found in a variety of traditional medicines, it appears to be as potent as some anti-diabetic pharmaceuticals.

Berberine: Its origins and structure

Berberine has been detected in the berberidaceae family of plants (from where it got its name), specifically the medicinal plant berberis aristata (indian barberry), from which it was first extracted.

It has since been isolated from goldenthread (coptis chinensis from the family ranunculaceae) and goldenseal (hydrastis canadensis from the same family). It is also found in tinospora cordifolia (guduchi) from the family menispermaceae and also in amur cork tree (phellodendron amurense) from the family rutaceae. The only things tying these plants together is their history of being used to fight diabetes, and how they all contain berberine (beyond that, they are quite different).

The molecule itself looks like a snake.

berberine_molecule

Berberine is a simple and easy to remember name derived from the structural name, 2,3-methylenedioxy-9,10-dimethoxy-protoberberine.

What is the best attribute of Berberine?

The anti-diabetic effects of berberine are the most remarkable, and when an oral dose of 900mg (300mg thrice a day) or 1500mg (500mg thrice a day) is taken by people with diabetes, berberine appears to be as effective at reducing blood glucose, serum insulin, and HbA1c as the pharmaceutical metformin at the same doses (limited evidence suggests also as potent as glibenclamide, another pharmaceutical).

The most remarkable part is that this isn’t information derived from a rat study, but is the conclusion from a meta-analysis conducted on diabetic people published in 2012 (1) The only downside really is that the data the information derived from was not of the best quality (good research, just not optimal).

The best conclusion we can make right now is that berberine appears to be roughly as effective as commonly used anti-diabetic pharmaceuticals. Think about that for a moment – we know that most supplement claims are pure marketing hyperbole. Here we have a supplement that seems to work just as well as pharmaceutical drugs, and not only that, it tackles a huge societal problem!

Additionally, the only two studies to measure weight noted that obese people (one with metabolic syndrome, the other being ‘otherwise healthy’) who consumed berberine had weight loss of roughly 6-13% over just 3 months. Diet was not recorded during this time, and no research has been done in lean people, but berberine appears to have a fairly strong anti-obese effect (2,3).

It also appears to reduce circulating cholesterol levels, which sets it apart from the pharmaceutical metformin (which cannot boast the same), this may be related to an enzyme it suppresses, known as PCSK9, and this inhibition has also been linked to reducing resistance to statin drug therapy(4,5). Due to this, some researchers think Berberine may play a role in augmenting statin therapy for reducing cholesterol.

In the end, berberine is one of the rare nutraceutical compounds that actually has therapeutic use combined with a low toxicity risk and may be useful as an adjuvant for other therapeutics. In a way, berberine is the nutraceutical equivalent of metformin in regards to diabetes (metformin being a remarkable pharmaceutical actually, being potent and healthy while also being quite safe).

What might it also do, pending more research?

The anti-obese actions are too remarkable, yet too variable (one study said 13% while the other said 6% weight loss; same doses and time period, with the only difference being that the 13% study had metabolic syndrome), and definitely requires more research. Future studies in lean people will determine if the compound is fat burning (reduce fat mass in general) or merely anti-obese (reduce fat in obese people only).

Other aspects of Berberine that are noteworthy are cardiac health (acting on the cardiac tissue in a beneficial manner), possible antidepressant effects that might be synergistic with other antidepressants, reducing both triglycerides as well as cholesterol, reducing the risk of heart disease via relaxing blood vessels and reducing plaque buildup (needs some more research in humans, animal models look good), and its effects on inflammatory intestinal disorders (traditionally used for intestinal health, and appears to be very rehabilitative for ulcerative colitis in rats).

It interacts with the telomerase enzyme, and might have a role in anti-cancer research as well as life extension (no trials yet).

It has the mechanisms to build muscle, but this requires abolishing or at least inhibiting a protein known as atrogin-1. Atrogin-1 effectively negates the inherent muscle building effects of berberine drawing nutrients into a muscle cell.

What are the side effects?

Like all compounds that are not 100% absorbed, excessive oral doses (around one gram at a time) of berberine can cause diarrhea. Berberine needs to go somewhere if it isn’t all being absorbed and your colon happens to be the only way out.

Secondary to the absorption issues, cramping and nausea have been reported very infrequently. Not enough to make people voluntarily stop berberine supplementation (so, it appears to be a low degree of nausea and cramping).

That’s about it.

If we want to start grasping at straws, we find that some in vitro studies (human cells in a petri dish) suggest that brain cells don’t like being deprived of oxygen and then exposed to berberine. It seems berberine may actually protect brain cells if introduced before the injury, but damage them if introduced after the injury. There really isn’t any evidence to suggest how relevant this information is (many studies that are notable in a petri dish become irrelevant in an actual human), but it is worth mentioning.

It might inhibit an enzyme known as CYP2C9, which would require a warning to anybody taking pharmaceuticals that are metabolized by this enzyme. Berberine isn’t remarkably potent at this inhibition, but the warning is just prudency.

Overall, Berberine appears to be remarkably safe as a supplement when the dose is adhered to. And remarkably powerful.

Practical supplement combination

Simply put, berberine would probably go great with some Metamucil.

Metamucil is the brand name for psyllium husk, which is a mostly soluble fiber commonly recommended to alleviate constipation due to it being a ‘bulk laxative’ (causes laxative effects, but solely due to the bulk of the stool formed; definitely a lot less forgiving than caffeine or the really potent senna alexandria). Psyllium absorbs water, and resists intestinal fermentation by your colonic microflora and thus it commonly causes stools to become larger, softer, and easier to pass.

Berberine, being a herbal imodium, is anti-motility and although it isn’t likely to outright cause constipation it could definitely delay transit time. Psyllium is pro-motility, and theoretically normalizes transit time (this normalization has been noted many times with psyllium).

Additionally, both agents are fairly healthy for the intestinal structure itself and while berberine is potent enough to be a reference drug for diabetes psyllium has basically been shown that:

  • It may benefit blood glucose, but this is short lived (only occurs throughout consumption of psyllium) and really isn’t that potent overall
  • It appears to be recommended as an adjuvant alongside pharmaceutical diabetes therapy for persons who have intestinal problems related to constipation or loose stools

The combination shows no signs of reducing either of their efficacies, while they may have additive effects on both glucose regulation and fecal regulation (there’s a lot of ways to dance around the term ‘shit’).

This post was written by Kurtis Frank and Sol Orwell, Co-founders of a site called Examine.com. Examine is a site where you can find the cold hard facts on any supplement you could possibly imagine (from studies to possible uses and stacks). If you’re even remotely interested in researching supplements, then Examine is the place to go. I personally use it for supplement research and cannot recommend it enough.

References

  1. http://www.ncbi.nlm.nih.gov/pubmed/23118793
  2. http://www.ncbi.nlm.nih.gov/pubmed/22739410
  3. http://www.ncbi.nlm.nih.gov/pubmed/22474499
  4. http://www.ncbi.nlm.nih.gov/pubmed/18355829
  5. http://www.ncbi.nlm.nih.gov/pubmed/19687008

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4 Comments

  • Dmitry April 29, 2015 at 1:42 am

    I am interested in weight loss and blood sugar control for myself. Sounds like Barberine is good for me. I’ve seen Barberine by itself and Barberine with Glycox. What is the difference? What does Glycox provides additionally to Berberine performance?

  • Brett Maas August 13, 2015 at 8:27 pm

    Fat burning pills only work as hard as you do. If you have a terrible diet and do not go to the gym, then the pills will do absolutely nothing for you. But if you actually are eating clean and hitting the gym at least 4 times a week then these pills could only be beneficial to reaching your weight loss goal and shredding that belly fat. Here is a link to the one I use to take and it worked great for me, now i’m in the best shape of my life. http://www.amazon.com/Cellucor-Thermogenic-Burners-Capsules-Chrome/dp/B007FGCAFU

  • Mike Maas January 18, 2016 at 4:16 am

    I’ve found some interesting information/research on goldenseal and its predominant and most active alkaloid berberine. It looks to me like there is a significant danger of carcinoma/adenoma in the commonly used dosage range of berberine for hyperglycemia.

    Let me summarize first. In the 2010/2011 timeframe a long term 2 year rat/mouse study was undertaken by the National Toxicology Program at NIH. They ran 2 week, 3 month and 2 year studies. Liver cell hypertrophy was found in both the 2 week and 3 month trials but the 2 year trials showed even more significant damage.

    In the two year study male rats fed 25,000 ppm of goldenseal powder ad libitum showed a 20+% incidence of liver hepatocellular adenoma or carcinoma. This was the most significant effect. The concentration of berberine in the goldenseal powder was 3.9% by weight. When all the calculations of converting the amounts taken daily by the rats to a human equivalent dose are done it turns out that the rats with the 20% rate of carcinoma/adenoma were consuming the equivalent of a 100 kg human consuming @880mg/day of berberine. 

    Interestingly there was no carcinoma in the female rats and only 2 with hepatocellular adenoma.

    Jumping from goldenseal powder to berberine as the culprit is a big jump but reading the paper you will see that the researchers, even though avoiding saying it was definitively berberine that was the cause, did talk a lot about berberine in the discussion.
That first paper is here:http://tpx.sagepub.com/content/39/2/398.long

    Subsequent to the paper and motivated by it a second in vitro study was done to try to ascertain how that cancer in the rats might have been caused. In that study the researchers examined 5 alkaloids from goldenseal and found two that were active. Both were topoisomerase I and II interruptors and the researchers felt that this may have been the cause of the cancer in the first experiment. One of those alkaloids palmatine was of much lower concentration and somewhat weaker than that of berberine.
That paper is here:http://www.sciencedirect.com/science/article/pii/S0378427413008412

    As I said the NTP of the NIH actually ran 3 different trials. A paper containing all the work is here:
http://ntp.niehs.nih.gov/ntp/htdocs/lt_rpts/tr562.pdf (190 pp)
    There is a summary of the long report immediately above here:
http://ntp.niehs.nih.gov/results/pubs/longterm/reports/longterm/tr500580/listedreports/tr562/index.html

    I know it is difficult to get supplements tested but it certainly does seem that another longer term in vivo study of berberine itself is in order. Berberine has become a very popular alternative to metformin and more and more diabetics are taking it. It seems particularly risky when considering the fact that the dosage range that appears to have caused cancer in the rats is the same human equivalent range as many people are taking for hyperglycemia on a daily basis.

    Since I think the first thing you will want to check is dosage here are my dosage calculations taken from a forum post:

    The weight to weight mg/kg ratio is designed to eliminate the need to take into account the individual weight of the differing subjects. When the number of 54.6 mg/kg (from the research) is cited it means that the animal is consuming his own weight * that amount in berberine as a constituent of the total Goldenseal added to the diet which is 3.9% of the total Goldenseal. If the rat weighed 1kg it would have consumed 54.6mg if it weighed 0.1 kg it would have consumed 0.1 * 54.6mg or 05.46mg.
    Now let’s move to humans. If we had a 1 kg human being they would consume exactly the same as a 1 kg rat or 54.6mg. If we had a 100kg human they would consume 100*54.6mg or 5460mg.

    However, because animals have different consumption rates depending on volume:weight ratios experimenters adjust dosages according to those ratios. For rat:human that ratio is 6.2:1 meaning a rat has to consume 6.2 times as much as a human per kg of weight to get the same effect from a drug. Therefore to get the human EQUIVALENT dose the rat dose is divided by 6.2. 5460mg/6.2 = 880mg or slightly less than 2 500mg caps for a 100kg human. 100kg=220pounds.

    Clearly this dose of 880mg is well within what is considered “therapeutic” by the manufacturers and consumers of berberine.

  • Annalise March 23, 2017 at 5:56 pm

    I started taking berberine on the advice of my doctor to help treat insulin resistance and to help with weight loss (I don’t tolerate metformin very well). I was taking 500mg in the morning, and in the evening – so a total of 1 gram per day split in two doses. I had also been depressed for about the past year, and had taken Wellbutrin for about six months but didn’t find it to be particularly helpful, and so I just kept suffering on with depression. The depression seemed to be getting worse, I would wake up crying and I would cry and cry even though nothing was wrong in my life. I was a very negative, unhappy person, and certainly not very easy to be married to! Anyway, after a couple of weeks on berberine something began to change. The depression and negativity began to life off and I began loving and appreciating life. It was gradual. My whole outlook shifted from completely negative, to very positive. My husband started noticing it, and my family and then so did I. The longer that I took it, the better this became, and it completely changed my life. It became evident to all of us that I had been going through a chemical depression, and whatever was wrong with me was clearly related to my brain chemistry. The berberine helped me like no antidepressant ever had. Something was wrong, and this completely set it right. I wasn’t even thinking of insulin resistance or weight loss, but I did lose weight without even trying! 1kg in a month to be exact. So it did seem to work for that, but the antidepressent effects that I experienced were so profound that it overshadows the other.

    HOWEVER, I also developed the most horrible constipation of my life! I would eat loads of fiber (large volumes of leafy greens, raw carrots, apples – even large quantities of prunes!), and drink copious amounts of water but nothing worked. It took laxatives, and they barely worked. I had to take more than the recommended dose. I considered going for colonic hydrotherapy, because I was so desperate. It was as if my intestines were completely paralyzed. Like I had taken a handful of immodium! I decided to go off of the berberine for a few days, and I can feel quite a difference in my brain chemistry. I am not nearly as depressed as I was, but I can tell that my brain chemistry isn’t what it was as when I had taken the berberine. That stuff was a godsend, and answer to my prayers – literally. I don’t ever want to go back to that depression again, I would also like to take control of my insulin resistance (I eat very clean, limited sugar – but everything still has a tendency to want to turn to fat) and I would like to do it without medication.

    Does anyone have any advice about this?? Because my intestines were basically frozen, I am worried about taking psylium fiber that Coach Sahil has recommend as this will just create greater bulk that I fear I won’t be able to evacuate. I don’t want to get a blockage! Has anyone tried this, and can it help reverse this nasty side effect? I had such positive results with berberine, and totally unexpected results that I want to find a way to manage the side effect. Any advice would be appreciated.

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