Everything You Should Know About The Benefits and Uses of KPV Peptide
In this article, we will discuss one of the smallest but best peptides: KPV.
So, let’s get started on our deep-dive into the powerful benefits of KPV peptide.
What Is KPV Peptide?
KPV represents a tripeptide (consisting of 3 amino acids) situated at the C-terminal extremity of a larger naturally existing melanocortin peptide hormone within your body, recognised as alpha-melanocyte-stimulating hormone (α-MSH).
α-MSH is an incredibly important neuroregulatory peptide. Although α-MSH is widely acknowledged for its anti-inflammatory impacts within the human body, its significant drawback lies in its multifaceted functions extending beyond this role: “The anti-inflammatory effects of α-MSH can be elicited via melanocortin receptors (MC-Rs) broadly expressed in a number of tissues ranging from the central nervous system to cells of the immune system and on resident somatic cells of peripheral tissues.
α-MSH affects various pathways regulating inflammatory responses such as NF-κB activation, expression of adhesion molecules, inflammatory cytokines, chemokine receptors, T-cell proliferation and activity and inflammatory cell migration. “A broad range of effects of α-MSH exerted beyond the field of inflammation, its pigmentory capacity being only the most visible aspect, has been one of the major impediments limiting the use of α-MSH in human inflammatory disorders“. The encouraging development is that KPV was identified as the “minimum effective sequence” required for α-MSH to manifest its anti-inflammatory attributes.
As far back as 1984, a study involving rabbits revealed the capacity of KPV to effectively reduce fever: “The idea that the 11-13 amino acid sequence is important to the effect of the parent molecule was tested by giving lysine-proline-valine both centrally and peripherally to rabbits made febrile by IV administration of leukocytic pyrogen. The tripeptide reduced fever after both central (0.5-2.0 mg) and peripheral (2-200 mg) administration.
It appears that the 11-13 sequence is part of the message sequence of alpha-MSH with regard to antipyretic activity. However, the lower potency relative to that of the parent molecule suggests that other portions of the molecule are essential to full expression of the antipyretic effect.”
Many more studies later, KPV was concluded to “exert a similar or even more pronounced anti‐inflammatory activity as full‐length α‐MSH”
How Does KPV Work?
Despite KPV being the functional component of the α-MSH molecule accountable for its anti-inflammatory effect, both KPV and α-MSH address inflammation through related but distinct mechanisms: “In vitro, macrophage activation, determined as release of [the chemokine KC] and interleukin (IL)-1β was inhibited by α-MSH and MTII [Melanotan II] but not by KPV.
Furthermore, macrophage activation by MTII led to an increase in cAMP accumulation, which was attenuated by SHU9119, whereas KPV failed to increase cAMP. The anti-inflammatory properties of KPV were also evident in IL-1β-induced peritonitis inflammation and in mice with a nonfunctional MC1-R (recessive yellow e/e mice).
In conclusion, these data highlight that the C-terminal MSH peptide KPV exhibits an anti-inflammatory effect that is clearly different from that of the core MSH peptides. KPV is unlikely to mediate its effects through melanocortin receptors but is more likely to act through inhibition of IL-1β functions”.
What makes KPV particularly effective is that this process directly happens inside your cells:
“KPV exerts its anti-inflammatory function inside cells, where it inactivates inflammatory pathways.
KPV enters the cell and interacts directly with inflammatory signaling molecules inside the cell. It enters the nucleus of the cell and, once there, can inhibit the interaction of inflammatory substances and molecules”.
In order for KPV on its own to exert its inflammation-lowering effects, it relies on a transporter peptide known as PepT1:
“One of the normal transport functions of gut epithelial cells is the absorption of small peptides from the diet by peptide transport activity. This is mediated via the H+-coupled oligopeptide transporter (PepT1) which is located at the apical membrane of intestinal epithelial cells (IEC) and which cotransports peptides and H+”
“…Since expression of colonic hPepT1 is up-regulated in IBD [inflammatory bowel disease], its transport activity constitutes a potential new target for anti-inflammatory therapies.
Furthermore, the importance of hPepT1 expression by immune cells during intestinal inflammation should be evaluated as it may be therapeutically advantageous to develop PepT1-mediated anti-inflammatory drugs”
Which leads scientists to the conclusion that KPV has three parts to its mode of action:
“i) KPV reduces the two most important intracellular signaling pathways in the pathogenesis of inflammatory bowel diseases: the NF-κB and MAPK cascade pathways as well as the subsequent synthesis of pro-inflammatory cytokines, ii) the anti-inflammatory effect of KPV is mediated through the transporter PepT1, and iii) oral delivery of KPV reduces the severity of DSS- and TNBS-induced colitis in mice.
These results indicate that targeting KPV transport into both epithelial and immune cells may reduce the overall level of pro-inflammatory cytokine production by mucosal and immune cells and therefore raise the use of KPV as an attractive therapeutic strategy against [inflammatory bowel disease]”.
One specific paper has an excellent summary of what KPV is able to do best:
“… the broad anti‐inflammatory effect will not result in strong immunosuppression as seen with the corticosteroids or systemic calcineurin inhibitors.
Accordingly, activation of NF‐κB as well as subsequent expression of pro‐inflammatory molecules is never fully suppressed, but mostly only reduced.
In the absence of inflammation or pro‐inflammatory stimuli such as LPS or IL1, the anti‐inflammatory and immunosuppressive potential of α‐MSH and its peptides was usually weak or absent. “
The essential goal is to maintain a state of inflammation in your body that is optimally balanced, rather than excessive or insufficient.
What Are The Benefits of KPV Peptide?
KPV doesn’t boast an extensive range of published studies; PubMed lists only 70 results from 1973 to 2021.
Our understanding of this peptide predominantly stems from in vivo investigations, in vitro examinations, animal trials, a handful of minor human experiments, limited engagement with biohackers, and only a few peptide experts.
Furthermore, a significant portion of KPV’s health advantages is extrapolated from knowledge about its precursor, α-MSH.
However, this won’t hinder our enthusiasm for embracing what is poised to become another valuable addition to Nūūtro’s arsenal of fully optimised health resources.
Let’s delve into the potential of KPV to contribute to an extended and ailment-free life experience!
What Are The Benefits of KPV Peptide?
Is KPV Anti-Inflammatory?
From the elucidated mechanism of action described above, the correlation between KPV and its role in rectifying chronic inflammation, thereby reinstating bodily equilibrium, becomes apparent.
This knowledge is grounded in a 2008 systematic review that aggregates 37 animal studies conducted between 1981 and 2008, exhibiting the consistent anti-inflammatory attributes of α-MSH.
Remember: KPV constitutes the active segment of α-MSH, and it’s arguably responsible for a substantial portion of its inflammation-reducing capability.
What’s particularly intriguing is the extensive range of the anti-inflammatory effects.
These effects have been investigated across five distinct species: rabbits, mice, rats, guinea pigs, and squirrel monkeys.
The studies explored various disease conditions, including:
- Systemic inflammation
- Brain inflammation
- Ocular inflammation
- Contact dermatitis
- Allergic airway inflammation
- Acute pancreatitis
- Gastrointestinal inflammation
Furthermore, the effects extend to shielding against cytotoxicity, offering protection to multiple organs, and encompassing numerous other domains.
To underscore the significance of these outcomes, let’s examine two of the studies analyzed within the review.
One example is a 2007 research paper that delved into the efficacy of KPV in murine models of inflammatory bowel disease:
“…treatment with KPV led to earlier recovery and significantly stronger regain of body weight. Histologically, inflammatory infiltrates were significantly reduced in KPV-treated mice, which was confirmed by the significant reduction of MPO activity in colonic tissue after KPV treatment.
Supporting these findings, KPV treatment of transfer colitis led to recovery, regain of body weight, and reduced inflammatory changes histologically. In MC1Re/e mice, KPV treatment rescued all animals in the treatment group from death during DSS colitis.”
Another 2011 study examined the use of the derivative KDPT (Lysine-d-Proline-Threonine) in treating intestinal inflammation in mice:
“KdPT-treated animals showed markedly reduced severity of inflammation in both colitis models. In colonic epithelial cells, KdPT increased proliferation, accelerated closure of wounds, and improved transepithelial electrical resistance after stimulation with interferon-γ/tumor necrosis factor-α.
Moreover, treatment with KdPT also prevented the loss of tight junction protein expression and improved barrier function in vivo.
KdPT acted independently of IL-1 receptor type I in vivo and did not affect melanogenesis in vitro.
KdPT is capable of attenuating the course of experimental colitis in different models and maintains epithelial cell function.
Furthermore, KdPT does not induce pigmentation, emphasizing the potential of this small molecule for the future treatment of IBD”.
Diminishing inflammation was merely a singular outcome; additional observed effects encompass tangible results such as the regulation of body weight and the revival of cellular functionality.
Is KPV Anti-Microbial?
While further research is warranted for this particular application of KPV, substantial effects have already been observed in relation to two pathogens: the bacterium Staphylococcus aureus and the fungus Candida albicans.
This notable effect has been firmly established since the year 2000, when a groundbreaking paper highlighted this phenomenon:
“alpha-MSH peptides significantly inhibited S. aureus colony formation and reversed the enhancing effect of urokinase on colony formation.
Antimicrobial effects occurred over a broad range of concentrations including the physiological (picomolar) range. Small concentrations of alpha-MSH peptides likewise reduced viability and germ tube formation of the yeast C. albicans.”
“Reduced killing of pathogens is a detrimental consequence of therapy with anti-inflammatory drugs.
Because α-MSH has potent anti-inflammatory effects we determined influences of α-MSH on C. albicans and S. aureus killing by human neutrophils.
α-MSH peptides did not reduce killing but rather enhanced it, likely as a consequence of the direct antimicrobial activity.”
The pharmaceutical company Zengen identified that KPV was the optimal sequence of amino acids to yield the most formidable pathogen-eliminating impact:
“In this structure-activity study, the team developed several compounds that have greater candidacidal activity than a-MSH and, in fact, one particular peptide (number 19) killed nearly 100 percent (99.7 percent) of Candida cells over repeated experiments”.
“The power of this new a-MSH analogue against C. albicans appears to be significantly greater than any other known peptides, as it is super-potent, super-stable and super-durable…
We’ve not only improved upon Mother Nature by developing a ‘super’ peptide that kills C. albicans, but also may have unlocked the key to understanding how a-MSH really works – through a receptor in yeast which is yet to be identified.”
Given the swift development of resistance by fungal infections against current therapies, it’s conceivable that we might be on the verge of resolving a longstanding issue in the medical field spanning several decades.
Does KPV Improve Gut Health?
The term “second brain” is frequently used to describe the gut, and for good reason.
The gut actively contributes to the regulation of all other organs within your body.
Whether it’s the brain, heart, or even fat around your abdomen, the bacteria in your gut can significantly influence the emergence of age-related illnesses.
Going back to 1997, the importance of a-MSH in addressing inflammatory bowel disease (IBD), a prevalent gut disorder, was already evident.
“The peptide treatment had marked salutary effects: it reduced the appearance of fecal blood by over 80%, inhibited weight loss, and prevented disintegration of the general condition of the animals.
Mice given alpha-MSH showed markedly lower production of TNF alpha by tissues of the lower colon stimulated with concanavalin A; the inhibitory effect of alpha-MSH on production of inflammatory nitric oxide by lower bowel tissue was even greater.
The combined results indicate that alpha-MSH modulates experimental IBD, perhaps by inhibiting production within the gut of the local proinflammatory agents TNF alpha and nitric oxide, or by inhibiting inflammatory processes closely linked to these mediators.”
KPV was administered to mice via a special formulation of nanoparticles and the results were promising:
“These NPs successfully mediated the targeted delivery of KPV to key UC therapy-related cells (colonic epithelial cells and macrophages).
In addition, these KPV-loaded NPs appear to be nontoxic and biocompatible with intestinal cells.
Intriguingly, we found that HA-KPV-NPs exert combined effects against UC by both accelerating mucosal healing and alleviating inflammation.
Oral administration of HA-KPV NPs encapsulated in a hydrogel (chitosan/alginate) exhibited a much stronger capacity to prevent mucosa damage and downregulate TNF-a, thus they showed a much better therapeutic efficacy against UC in a mouse model, compared with a KPV-NP/hydrogel system.”
KPV and BPC-157 emerge as the forefront contenders in utilizing peptides to improve overall gut health, possibly by decreasing the synthesis of pro-inflammatory substances.
Can KPV Help With Skin Conditions?
Could components of KPV potentially expedite the recovery process of wounds and injuries, particularly those affecting the skin?
Fortunately, the anti-inflammatory properties of a-MSH are similarly noticeable in various skin-related medical conditions.
“α-MSH was shown to elicit a plethora of anti-inflammatory and/or immunomodulatory effects in a variety of animal models including experimentally induced cutaneous vasculitis, experimental psoriasis, experimental autoimmune encephalitis, allergic contact dermatitis, allergic bronchiolitis and colitis”
“..resolution of inflammation is further crucial to prevent the development of a chronic inflammatory process that finally may lead to hypertrophic scar and keloid formation (v. i.). Such chronic skin wounds are characterized by a proinflammatory phenotype, that is presence of macrophage infiltration, TNF immunoreactivity and neutrophil infiltration.
However, what truly captures the intrigue is the process of angiogenesis, which involves the creation of new blood vessels:
“The increased vascularisation and the angiogenesis that accompany chronic inflammation prolong and intensify the inflammatory response, which has intrigued researchers.
It is believed that angiogenesis sustains inflammation by delivering oxygen and nutrients to support the increased metabolic needs of cells at sites of inflammation.”
The most analogous research to a KPV study involves an experiment conducted using human skin models, revealing that KDPT effectively reduced skin inflammation caused by psoriasis:
“Psoriasis is a chronic inflammatory disease appearing as scaly erythematous cutaneous lesions, which are characterized by parakeratosis and acanthosis as well as the infiltration of immune cells, such as T helper-1 and T helper-17 cells”
“…systemic KdPT treatment significantly reduced hyperkeratosis and acanthosis in murine as well as human skin.
Moreover, KdPT upregulated Foxp3 in CD4+ T cells from mice and from peripheral blood of individuals with psoriasis and decreased the expression of type 1 inflammatory cytokines, indicating that the beneficial effect of KdPT was, at least in part, mediated by the induction of functional regulatory T cells that suppressed the activation of pathogenic CD4+IFN-γ+ and CD4+IL-17+ T cells.”
Other Benefits of KPV:
- Low levels of α-MSH are observed in conditions such as Lyme disease and mold illness, along with arthritis.
- α-MSH plays a pivotal role in regulating ocular immunity, which is why it’s being investigated in an ongoing clinical trial.
- In a mouse study, KPV lowered inflammation and tumorigenesis during colitis-associated cancer.
- α-MSH has implications in treating disorders like “asthma, sarcoidosis, and the acute respiratory distress syndrome”.
KPV Dosage and How To Take It:
After reading our science backed article onKPV, we know you will be looking forward to giving it a try, especially if you’re just discovering Peptide Therapy and want something that has a wide range of therapeutic benefits.
You can acquire any of our peptides by booking in a consultation with our Integrative and Functional Medicine practitioner, Jessica, who has years of experience working with Peptide Therapy.
These consultations are available for international clients, and are not subject to the UK only.
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Why Nūūro is Gold-Standard in Peptide Therapy
Like health and wellness trends, there is a lot of misinformation about Peptide Therapy being spread across the world wide web.
And on top of that, many manufacturers producing peptides, or pharmacies selling peptides, are taking shortcuts, using low-quality ingredients and sourcing their peptides from high-risk Chinese suppliers.
But that is not us.
Here at Nūūtro, you can trust our team, products, and programs to help change your health trajectory.
We’re so excited to be bringing Peptide Therapy to our community, and we have seen first-hand how peptides can invoke life-enhancing results.
- We only source our peptides from accredited USA-labs that use the purest ingredients.
- Jessica has personally met the owner and COO of our peptide supplier, we only do business with integrity.
- Our peptides are rigorously third-party tested.
- We work with you to discuss other issues such as gut inflammation and hormonal disbalance prior to ensuring the peptides work to their full efficacy.
To learn more about our Peptide Therapy programmes click here.
KPV is one of the smallest peptides on the market, but has miraculous results.
Based on the existing information, KPV showcases a highly favorable profile.
Firstly, in vivo and in vitro studies have been conducted, both in mice, revealing therapeutic effectiveness devoid of any undesirable repercussions. Interestingly, this holds true regardless of the method of KPV administration.
Additionally, it’s worth noting that even at significantly high doses, the more potent analogs of α-MSH have been demonstrated to be safe.
We’re so excited to help you kickstart your Peptide Therapy and for you to feel and look your best!
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Our staff is made up of skilled professionals who are dedicated to helping you achieve your goals while providing the highest quality care.