PEPTIDES

It has become trendy, particularly among the internetistas, to advocate for the availability of “peptides”, as important new health items that are being unfairly withheld from the public by government bureaucracy.  I thought it might be useful to take a look at what these things are, what they claim to do, and how we should approach their use.

There are multiple Peptides being promoted on the internet.  Here are a few of them:

For Weight Loss, the well-known GLP’s, the less well-known Retatrutide and AOD-9604.

For Healing and Fitness, BPC-157, TB-500, CJC-1295, and Ipamorelin

For Skincare and Aesthetics, GHK-Cu, Matrixyl, and Tripeptides.

All of these things need to be put into your body through nasal sprays, topical applications or injections; on the whole they cannot be taken orally because they will not survive the digestive system and therefore will not be available to your cells through your blood.

It is certainly ironic that those people who are so suspicious of the “jab” of vaccines, so ardently want access to these other injectable things.

So, what is a “peptide”?   A peptide is a simple protein.  Like proteins, peptides are strings of amino acids; think of a string of multi-colored beads where each bead is an amino acid.  Any protein is made up of strings of amino acids; a peptide is just a relatively short protein, generally a string of around 30 beads or less. And, just like the food we eat has proteins that the digestive system breaks down into individual “beads” that can then be delivered to our cells to make new proteins, peptides are broken down into their own beads in the digestive tract.

Our bodies produce a number of short peptides during normal processes. These self-produced peptides include chemicals like Glucagon and its siblings GLP-1 and GLP-2 which induces release of sugar into the blood; Insulin which induces the body to store sugars out of the blood; Oxytocin, which is important in childbirth, breast feeding, sperm motility, sexual pleasure and bonding; Endothelin, which helps the circulatory system provide blood through the smallest blood vessels; and Calcitonin, which acts as an antimicrobial in the body.  There are many others, each of which has a function in our bodies.  And all of these proteins interact with many other proteins in the body, creating a very complicated network of responses in all of the organs and tissues.

PEPTIDE VACCINES

Here is something that you might find interesting: there are multiple VACCINES under review that are PEPTIDES! 

Peptide vaccines are small segments of the proteins on pathogens that produce immune response protection from those pathogens.  These peptides are generally around 20-30 amino acids in length that mimic antigenic determinants (the specific sites on a viral protein for which immune protection is stimulated).  You can imagine a doorknob with a jewel in the center which locks and unlocks the knob.  The immune response that inactivates that knob is directed at the jewel.  So, if you want to create a specific immune response to that doorknob, you can challenge the immune system with the whole knob, knowing that some of the response will be to the jewel.  Or you can isolate just the jewel and use it by itself to challenge the system.  This is the thought behind using a peptide for vaccines.  Rather than vaccinating with the whole virus, the peptide imitates the specific structure on the virus for which an immune response is protective.

Some examples of peptide vaccines are  those that protect against Influenza, or that have shown success in treating patients with advanced urothelial bladder cancer, or peptide vaccines targeting melanoma or new vaccines for COVID-19 mimicking sites on the S protein.

Again, there is great irony in that antivaxxers embrace injected peptides for purposes other than generating immunity.

Let’s take a look at some of the peptides receiving internet attention.

The most well-known of these peptides are the trio of peptides created when proglucagon (first identified in the early 1980’s) is broken apart by normal enzymes in the body.  Those three peptides are all just about identical in size, around 30 amino acids.  They are: Glucagon, GLP-1, and GLP-2.   We have known about Glucagon since 1922.  It is produced in the Pancreas in what are called the “alpha cells” and has generally been recognized as the antagonist (opposite to) insulin (discovered in 1921).  While insulin, also produced in the Pancreas in the “beta cells”, encourages sugar to be removed from the blood and stored, glucagon encourages the body to release sugar back into the blood.  Both of these hormones have effects on a huge number of reactions in our bodies.   Now we know that glucagon is only one of the three peptides created when the parent protein is broken up, and we are only beginning to understand the wide effects of all three of these peptides. 

The two most prevalent peptides derived from the breakdown of proglucagon used for treating diabetes and for weight loss are Wegovy/Ozempic and Zepbound/Mounjaro.  These are synthetic peptides designed to mimic the effects of GLP-1 and GLP-2, but to last longer in the body.  The two pairs are similar, although Zepbound/Mounjaro mimics an additional hormone called GIP to Wegovy/Ozempic.  You may have heard the term “GLP-1 agonist”.  An “agonist” is something that stimulates the same response as the chemical it mimics.  In this case the GLP agonists mimic the actions of the GLPs, but last longer.  It is easy to confuse the term “agonist” with the more common word “antagonist”.  They are the opposite of each other.  An “antagonist” works to negate the properties of the chemical to which they are related.

Eli Lilly has synthesized another peptide that may target more receptors than Ozempic or Mounjaro.  It is called Retatrutide.  It is also a synthetic peptide, and it shows great promise, but it is in clinical trials to determine what side effects may be associated with its use.   Injecting synthetic chemicals into our bodies needs to be rigorously studied because the positive effects may often be accompanied by negative effects, and the ratio of those effects needs to be considered before sanctioning their use.   Consider what might happen if a peptide injected into your blood triggered a response from your immune system, and that response reverberated through your body causing damage to your own organs.

I would strongly suggest that everyone be extremely careful in “jumping the gun” and injecting these proteins into your body, particularly on a routine basis, before the appropriate safety and efficacy trials have been completed. 

ALWAYS inform your primary care physician of ANYTHING that you are taking including vitamins, nutritional supplements or dietary supplements.  All of these may have interactions with each other or with prescription or OTC medications that you are also taking.  It is extremely important that a knowledgeable individual have a full picture of your diet.  That is why all medical screening includes questioning you about things like alcohol, foods, tobacco products, and any other herbal or nutritional items that you use on a routine basis.

Another peptide that is being promoted is AOD-9604.  It is a synthetically modified peptide that mimics a segment of Human Growth Hormone.  This peptide is 16 amino acids long and is supposed to stimulate weight loss by targeting fat loss.  In a very small study, it was shown to have few side effects, but in larger clinical trials in 2007, it was abandoned by the company that developed it because the weight-loss results were not significantly greater than with placebos.   There have been no long-term safety trials.

BPC-157 has become a favorite “healing peptide” in the fitness community.  It is a 15 amino acid peptide derived from gastric secretions.  There have been virtually no clinical trials of this peptide, no safety studies in humans, and no effectivity studies.  All of the quoted “results” are anecdotal.  It is banned by athletic organizations. 

GHK-Cu is a popular topical treatment for reducing fine lines and stimulating the production of collagen.  It is only 3 amino acids long, and that short string of amino acids carries a Copper ion through the blood.  When used topically as a skincare cream, it is safe and effective for accelerating skin and tissue repair and hydration.

However, when used in an injectable form or as an oral dietary supplement, with the goal of repairing tissues inside the body, there is very little clinical trial data.  And that is where internet influencers touting the injection of this peptide are potentially causing problems.  Just because something has worth when used topically, it is not a correct assumption that it would also work through an injection or taken orally.

Copper is an important element in our bodies.  It is essential for the production of ATP, the chemical in every cell that provides energy for all cellular processes.  It is essential for the absorption of iron into our blood; and iron is a component of every single red blood cell for allowing the transport of oxygen to all cells.  It is also essential for the ability to create collagen and elastin in healthy bones and joints. And it is an essential component of the enzyme Superoxide Dismutase, which is one of our body’s most important defenses against damage from free radicals.  Because GHK-Cu is only 3 beads long, fractions of orally administered GHK-Cu will pass through the digestive system and enter your blood.

The attraction to some influencers on the internet is that by increasing the amount of GHK-Cu we might accelerate the positive effects.  But we do not know what problems might be stimulated by increased amounts of copper in our body.  What we do know from studies, is that too much copper in the body can lead to liver and brain damage.  

TOO MUCH OF A GOOD THING CAN BE A BAD THING

This underscores the need to do clinical studies on ANY item that we choose to inject into ourselves.  Just because something is “naturally produced”, does not mean that it is safe at any level.  Let me give you an example.  Suppose you are a type II diabetic.  Your body does not produce adequat insulin to remove sufficient sugar from your blood, and high sugar causes multiple problems.   So, it is really beneficial to inject some insulin into your body prior to meals so that the sugar produced during digestion is removed from your blood and stored.   But, if some insulin is great, would more be even better?   No, no, no.  If you take too much insulin, your blood sugar may drop to low levels that cause seizures, coma, or even death.  So, even though insulin is natural, it still needs to be controlled to prevent serious health issues.

 EVEN WATER CAN BE TOXIC

There have been several cases of deaths from what is generally called “water toxicity”, most recently in 2023.  The deaths resulted from people drinking too much water in too short a time.  In 2023 the woman who died drank the equivalent of four 16-ounce bottles of water in 20 minutes.  In 2007 a woman who was participating in a radio contest “Hold your wee for a Wii” drank an undetermined amount of water died a few hours later.  In 2003 a 64-year-old woman who had mental problems drank 30-40 glasses of water one evening because she was convinced that she needed it.  She died the following morning. In 2005 a college student died from a hazing event at a fraternity in which he was forced to drink water from a jug.  There are dozens of confirmed cases like these. Death was caused because the disproportionate intake of water resulted in too much fluid in the blood, diluting the electrolytes in the body and causing death.

Even the most innocuous item, like water, can be toxic when taken in excess.

Without good clinical studies, long-term safety data, and cataloguing of adverse events, we simply do not know what is safe and what is not, and what is effective and what is not.

Anecdotal stories do not constitute scientific evidence.  Be careful what you read.