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Berberine: a Multimodal Supplement

Berberine has long been in use as an antibacterial. However newer data and promoted the substance to higher ground. Berberine is typically found as a purified supplement from the botanicals: Coptis chinensis (Coptis) and Hydrastis canadensis (Goldenseal) and have now been shown to exhibit significant activity as: 

  • anti-cancer 
  • balancing/lowering blood sugar 
  • balancing/lowering “bad” cholesterol

Let’s discuss these in reverse order. “Bad” cholesterol is actually called low-density lipoprotein. Lipoproteins are little “packets” which contain cholesterol and cholesterol either goes from-the-liver-to-the-rest-of-the-body or from-the-rest-of-the-body back to the liver for processing and ultimately removal from the body. There are multipole ways that berberine can achieve this but most importantly are by

  1. inhibiting HMG-CoA reductase, the same enzyme that “statin” drugs inhibit; however berberine does this at a much lower and hence less-toxic rate. Berberine does not need to inhibit with such a heavy hand as do the drugs since berberine also inhibits other aspects of lipids.  
  2. Berberine actually can help inhibit one of the steps necessary for the synthesis/production of LDLs which means that it can stop bad cholesterol from even being produced in the body, not all of the LDL that is produced. but some.  Also, berberine has been shown to improve “fatty liver,” which is sometimes a stubborn clinical problem.

In terms of blood sugar: berberine can help by

  1. modulation of an enzyme called: AMP-activated protein kinase (AMPK), a highly relevant sensor blood sugar regulation, with particular relevance in the modulation of liver and muscle insulin sensitivity. What this means is that berberine can actually help the cells of the liver and muscles be more sensitive to insulin.  Insulin is the chaperone of glucose and without insulin we could not get glucose into our cells.  All cells of the body have insulin receptor and the job of such receptor is to allow insulin to “dock” on the cell surface and deliver the glucose into the cell so the cell can do its work.  If the insulin receptors on the cell are not attuned (insensitive) enough to be able to accept the insulin, then this is considered insulin resistance. If the cell is resistant to insulin then the glucose cannot be delivered; this is generally the starting point for the development of type-2 diabetes
  2. Berberine can also promote glucose uptake via other metabolic pathways in the cells which means that not only can it improve the insulin receptor activity but it can also help the glucose get in the cells more easily.  Further berberine can reduce the body’s own unnecessary production of glucose (gluconeogenesis) which causes the body to be more conservative and judicious with the glucose coming in via the diet a swell as already store in the body as glycogen.

and finally, regarding cancer, berberine can:

  1. regulate the cell cycle: in order for any cell to make a copy of itself, it must go through the cell cycle.  Normal cells “behave” in a way that causes them to be self-regulatory, i.e. only replicate when its deemed absolutely necessary.  On the contrary, cancer cells’ have a dysfunctional monitoring system which causes them to proliferate out of control. This is one of the hallmarks of cancer.
  2. regulate apoptosis: normal cells, as described above, go through a necessary cell cycle, the more often this occurs, the greater the chance for a mistake to be made.  In normal cells, when a mistake is made, “self-destruct” mechanisms in the nucleus become activated and the cell goes through what is called apoptosis or cell suicide.  In cancer cells, especially the highly-proliferative ones, apoptosis deranged and the cancer cells do not die, yet another hallmark of cancer.
  3. inhibit invasion and metastases: the more a cancer cell proliferates the more copies of itself it makes, which develops into a cancer mass, which is then termed a malignant tumor.  For that cancer tumor to spread it either has to invade or metastasize.  I often describe the differences between the two as such:  let’s say you are sitting in the doctor’s office, the door is closed, and you want to get into the next room: you have two options to get there.  One, you can walk out the door and walk down the hall into the next room or two, you can break through the wall into the next office; either way you get to your destination.  The former is akin to a cancer cell leaving the tumor and jumping on the “blood vessel highway,” a form of metastatic (evil) spread, while the latter is considered direction invasion.  Berberine plays a role in regulating both processes.
  4. regulate the tumor microenvironment: all living things live in an environment, both a micro and a macro environment.  A humans’ micro environment can be considered their home and interaction with those very, very close to them while their macro environment is considered all other places a human visits from day-to-day. A cancer cell is no different and its microenvironment is considered the place where it resides inside of a tumor. The microenvironment can regulate the success of a tumor by allowing it to be fed (nutrition), remove waste, as well as how it interacts with the other nearby (normal cells) as well as protecting it from immune surveillance and attack. Berberine has been show to favorable augment the tumor microenvironment in favor of the body and not in favor of the tumor cells. 

As you can clearly see, berberine can be a wonderful supplement to a therapeutic regimen for many reasons. Berberine is not expensive and generally well-tolerated. Some people do have gastrointestinal distress when they start berberine but many times their body either accommodates to the use of the doctor can work with them to achieve a tolerable regimen. 

References:

  1. PMID: 30484403 DOI: 10.2174/1389557519666181128120726
  2. PMID: 30117113 DOI: 10.1007/s12020-018-1689-y
  3. DOI https://doi.org/10.2147/CMAR.S242329, https://www.dovepress.com/the-anti-cancer-mechanisms-of-berberine-a-review-peer-reviewed-article-CMAR