Peptides: Molecules that pep up your health

Peptides: Molecules that pep up your health
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Peptides, the building blocks of proteins, are a formidable force in the body—essential to everything from keeping your DNA in smooth order to keeping your brain sharp. Cate Montana investigates their use as therapeutics

Considering that proteins are the building blocks of the body, and peptides are the building blocks of proteins, as tiny as they are, peptides are a mighty force. So far, researchers have discovered that the human body makes over 7,000 different peptides for specific purposes.

They aid in everything from DNA replication to sexual arousal, from cell division to cognitive function. Mood, memory, muscle mass, mitochondrial function, metabolic activities, aging and longevity—name the bodily function, and you’ll find peptides are at work.

Short chains of amino acids (organic compounds) linked together by peptide bonds (a type of chemical bond), peptides play vital roles throughout the body such as cell signaling, enzyme and hormone activity, and immune system regulation. The simplest peptides are dipeptides containing only two amino acids, followed by tripeptides (three amino acids), et cetera.

If a peptide chain contains more than 50 amino acids, it’s called a protein. If it has fewer than 20, it’s called an oligopeptide. Polypeptides contain 10–100 amino acids.

How peptides work

Epigenetically, peptides act by turning gene expression on and off. They interact with hundreds of healing pathways in the body. And because they’re made up of short amino acid chains, they can easily bind to receptor sites on the surface of cells, so they’re critical to cellular communication.

Pleiotropic in nature, which means they produce more than one effect, peptides work best in combinations. According to one of the leading peptide specialists in the US, Regan Archibald, LAc, FMP (reganarchibald.com), they have a healing response up to three times faster than diet, lifestyle and supplements alone. Because they’re involved in cellular and molecular signaling and follow so many pathways throughout the body, they “talk” to the body in a holistic, self-amplifying way.

“Peptides regulate most known processes and systems in the body in a tissue- and cell-specific manner,” says Archibald. “They don’t tend to have toxic accumulation based on their short half-life. Contrast that with some supplements, such as fat-soluble vitamins, which can accumulate in the body and lead to toxicity and harmful side effects.”

Compared to medications and hormones, Archibald says, peptides tend to be more selective. And because they hit their cellular receptor site targets more effectively than drugs or supplements, they have very few adverse side effects.

“They don’t set off an immune alarm or histamine response,” he says. “And as a medication, they can be given in up to 100 times greater doses without any known side effects, which is unheard of. The amount of supplementation you’d have to take to match the power and effectiveness of peptides could be insurmountable in terms of cost and volume.”

A plurality of peptides

Endogenous peptides are created in the human body and maintain our natural biochemical balance. They can work as hormones released from the endocrine system, regulating reproductive processes and helping balance metabolism. Insulin is an endogenous peptide that helps regulate the amount of glucose within cells and the blood.

Cell-penetrating peptides carry protein and nucleic acid molecules across the cell plasma barrier. Short-chain signaling peptides carry information for protein secretion, reproduction and protein targeting throughout the body. Antimicrobial polypeptides fight pathogens in the body. And finally, neuropeptides like oxytocin play a role in brain activity and behavioral processes.

Natural peptides come from animals, plants and microorganisms. For example, dynorphins are a class of opioid peptides first isolated from the pituitary gland of pigs but also made in the human body. Like endorphins, they’re inhibitory neurotransmitters that reduce pain.

Snake venom peptides are non-enzymatic polypeptides that have distinct pharmacological functions and different bioactivities. They’re useful for treating conditions ranging from diabetes to heart disease to chronic pain. Plant-derived peptides, such as cyclotides from coffee plants, are antimicrobial.

Fungi produce cyclosporine A, an immunosuppressant. Bacteriocins produced by bacteria are useful for treating infections.

Synthetic peptides are also called peptide therapeutics. They’re created in laboratories and can be designed to mimic endogenous and natural peptides. They can also be designed to have novel amino acid sequences and structures for highly tailored purposes, such as targeting one kind of receptor site and delivering one specific effect.

For example, oxytocin is an endogenous neuropeptide and hormone made by the hypothalamus to support lactation and maternal bonding after childbirth. It’s also produced in a lab (one brand name is Pitocin) and altered to create a different effect, namely inducing labor and reducing bleeding after delivery.

“The line between synthetic and non-synthetic peptides has got more to do with the structure than the purpose of the peptide,” says Dr Chris Maclay, medical director at MedBridge Global in Charlotte, North Carolina. His private practice focuses on functional, anti-aging and regenerative medicine (maclaymedical.com.au).

“We can make anything for the purpose, but the structure is native. Therapeutic peptides look like the native hormone. They may not be identical. But they are structurally so similar to what is endogenous that the body doesn’t react to it.

“And for that reason, it doesn’t have side effects. But because it doesn’t look exactly like the native molecule, it’s patentable. It’s a new molecule, but it’s an ‘analog peptide’ that’s analogous to the endogenous version.”

Endogenous human peptides are totally safe even at high doses. But because of their analogous structure, therapeutic/synthetic peptides are also relatively safe, or so the practitioners claim.

“From the point of view of the clinical literature, on balance, the demonstrated safety is high,” says Maclay. “I’ve not had a single patient have a life-threatening reaction.

“And I could count on one hand the number of patients who were upset by a reaction. Like feeling a bit of a hot flash after an injection, which is actually part of the appropriate mechanism of action. Or perhaps a bit of fatigue, which is also actually part of the mechanism of action.”

It’s important to keep in mind that the medical industry has also claimed synthetic vitamins and hormones are just as good as the real thing, but the evidence reveals otherwise (for examples, see our stories on HRT, GMO foods and homemade bread).

Popular use

More than anything, peptides are support molecules that build and maintain health rather than treat disease. They work best when used in combination under the supervision of a health specialist familiar with peptide therapy.

They should also be used in tandem with a healthy eating regimen that includes regular exercise and lots of organic whole foods: meats (more protein!), vegetables and fruits. Moderate supplementation is helpful when necessary.

The most effective delivery system for peptides is subcutaneous injection, permitting direct absorption into the bloodstream for maximum impact and efficacy. Topical application is used to target specific areas of the skin requiring anti-aging and regenerative effects.

Peptides can also be administered through the nasal passages for rapid absorption. Least effective is oral administration because the digestive system can break down the peptides before they’re absorbed.

Because of their specificity, selective interactions, highly refined ability to attach to receptor sites on target proteins (called “docking”) and purportedly high levels of safety, synthetic peptides—which are available only by prescription and are injectable—have emerged as the darlings of modern medicinal and biochemical research.

They’re highly popular for their therapeutic and money-making potential, and their bonding capacity makes them useful for drug delivery. In addition, their enhanced stability and longer-lasting effects in the body allow them to work effectively at lower doses than natural peptides—making them more cost-effective.

Since the first therapeutic peptide, bovine insulin, was introduced in 1922, government regulators have approved more than 100 peptide drugs worldwide. More come online every year, and hundreds more are being tested. Studies show they may be effective for a wide range of uses:

This purpose-oriented approach generally aligns with the traditional allopathic medical model more closely than with functional and integrative medicine and more natural approaches.

“Synthetic peptides are very much a part of natural medicine. They’re just a part that requires biomedical science,” argues Maclay.

“That said, because peptides’ natural role in the body is to promote a metabolic pathway of homeostasis (steady-state, optimal functioning), while functional medical practitioners may use patentable peptides like semaglutide (brand name Ozempic or Wegovy), they may also look at peptides that support more functional concerns.

“For example, they might use peptides not so much to focus just on reducing sugar levels but on increasing the body’s ability to burn sugar or increasing muscle mass so that the basal metabolism is preserved.”

Regarding practitioners of naturopathy, homeopathy, acupuncture, Traditional Chinese Medicine and other more natural approaches, Maclay says most tend to be less inclined to use or recommend peptide medicines because most lack prescriptive license. As well, there is still a lack of knowledge and awareness of the peptides and their many uses.

“Naturopaths and natural medicine practitioners will use natural peptides and endogenous peptide bioregulators, which are shorter amino acid chains than most therapeutic peptides,” says Maclay. “Many of them are only two or three amino acids long, but they actually often have specific receptors deep inside the cell because they’re so small.

“When we see a healthy gland, there are a lot of peptide bioregulators. When we see an aged or sickly gland, we see few of them. So, when they’re replaced, the youthful, healthy functions tend to be replicated.”

EPIC triggers

According to Archibald, four triggers turn off peptide signaling properties in the body and thus turn off the maintenance of human health. He uses the acronym EPIC to list them.

Emotional triggers. “Try to get healthy when you’re angry all the time or when you’re stressed out all the time or you’ve got chronic grief,” says Archibald. “Diseases build up based on these emotional imprints that we have in our body. You can track the neuropeptides that change in the body based on these emotional triggers and emotional trauma.”

Physical pain. Any kind of physical trauma, old and new, as well as chronic pain, wreaks havoc on peptides and cellular signaling.

Infections. Infectious elements are everywhere, always affecting us. “There’s Lyme, there’s Epstein-Barr, there’s Covid,” says Archibald. “Mycotoxins are a big deal from the moldy environments that we live in. At least 60 percent of the toxicity we’re impacted by comes from our own homes.

“There are parasites, Candida infections, small-intestinal bacterial overgrowth (SIBO). All these little microbes that we collect along the way never really leave our bodies. They just wait until the environment’s right, and then they start proliferating.”

Chemicals. This is the trigger that drove Archibald into the health field and into studying peptides in the first place.

“I was raised on a farm,” he says. “By the time I was in my 20s, the glyphosate from Roundup and all the other chemicals we consider necessary had completely compromised my health. And the traditional medical model was ineffectual in getting it back. Which meant I had to find another way.”

Heavy metal toxicity, chemical preservatives in our food, industrial pollution, agricultural herbicides and pesticides—removing these triggers and mitigating the other three EPIC triggers allow people to experience significant reversals of a myriad of health issues, claims Archibald. However, he points out, without adjunct peptide therapy, these reversals can be agonizingly slow and can even eventually reverse.

“A lot of times people do these big cleanses to deal with EPIC triggers, and they detox and they end up really sick and tired. They never really get through the process because they didn’t build up the cellular energy that they needed to do it.

“And that’s where peptides like the mitochondrial peptides come in. When you remove the cell danger response signaling (stress response) and get rid of EPIC interferences, people have a reversal of significant issues in their health. And it’s permanent. And they don’t have to stay on the peptides long term.”

He’s found that people on peptide therapy who also maintain good sleep rhythms, hydration, nutrition, exercise, some type of mindfulness and some type of temperature variation to stimulate hormone activity usually start feeling better within the first two weeks of therapy.

They remark on how their energy is better and they’re sleeping better, losing weight and feeling calmer. These are all typical signs they’re getting back on the track to better health.

“It’s not an overnight, magic-bullet approach,” says Archibald. “But people experience a restoration of their former athletic self, which is when they can start diving into the age-reversal process. It’s truly remarkable. And peptides support this process every step of the way.”

Testimonials

Dr Chris Maclay tells stories about two patients he treated strictly with peptides. The first was a tradesman who’d injured his wrist 15 years previously. Over the course of 13 years, the patient had undergone surgery, and doctors had prescribed cortisone injections and physiotherapy, but nothing had helped.

“I injected a ‘bundle,’ a combination of therapeutic peptides, and two weeks later, he contacted me to tell me that he could use his wrist again for the first time in 13 years,” says Maclay.

Another patient took a holiday in Thailand and developed post-infectious irritable bowel syndrome. They had gone to medical doctors and “tried everything.” They had also used natural therapies, including broad-spectrum probiotics and prebiotics, peppermint oil and a variety of quercetin, and nothing had worked.

“The symptoms resolved within about a month after they started BPC-157 (gastric pentadecapeptide, a 15–amino acid oligopeptide) also known as the ‘body protection compound.’ When I spoke to them again about 12 months later, the symptoms hadn’t returned, which makes me believe it had restored the gut lining and the flora. It was a dramatic symptomatic improvement for this person.”

Peptides for longevity

There are currently over 250 known anti-aging peptides that work through multiple mechanisms, mostly fighting inflammation and promoting cellular repair. The rest have antioxidant properties or various specific roles, such as enhancing learning and memory.

Most anti-aging peptides are relatively small, containing between six and 25 amino acids. (The smaller size gives them greater penetrating power.) They’re rich in the amino acids proline, tryptophan and glutamine. Of all the anti-aging peptides studied so far, the large majority have been clinically studied for their effects on skin aging. These are some popular anti-aging peptides:

Peptides to boost your immune system

Immunosenescence is the gradual deterioration of the immune system as we age. It’s characterized by signs of aging such as a weakened immune system, chronic inflammation, cancer development, and cardiovascular and neurodegenerative diseases.

A strong causative factor in immunosenescence is the lack of thymus function and a decrease in its production of regulatory thymic peptides as the years go by. These are some peptides that help to establish a healthy immune system:

Anticancer peptides

These peptides work by inducing cell death (apoptosis) in tumors, disrupting cancer cell membranes, inhibiting the production of tumor cells and serving as a type of vaccine against self-tumor antigens:

Tissue-building peptides

Weight loss peptides

Skincare peptides

Supplementary peptides: Uncharted territory

While we provide a long list of available peptides and their believed effects here, many of them lack substantial research in humans to determine their actual effects and the outcomes of long-term use. They may also have side effects, so it’s wise to be cautious and consult with your practitioner before using them.

Synthetic peptides in particular should be approached with caution. For example, semaglutide has been available for only a short time, but its serious adverse effects are already coming to light.