Peptides For Inflammation | A Comprehensive Comparison

Researchers looking to learn more about peptides for inflammation have come to the perfect place.

This detailed guide will delve into peptides that show promise for inflammation-focused research.

Our examination encompasses scientific findings on common inflammation-related processes and the peptides that could potentially mitigate them. These peptide may exert benefits like:

• Reducing inflammatory response
• Alleviating pain associated with inflammation
• Enhancing tissue repair and recovery

Continue reading to unveil the peptides that hold the greatest promise for inflammation research, including insights into their mechanisms, potential benefits, and safety profiles. We'll begin by highlighting our top three peptides for targeting inflammatory processes.

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Top 3 Peptides For Inflammation

Here are our top three peptides for reducing inflammation, chosen based on the available scientific data:

1) TB-500

TB-500 is a synthetic version of the endogenous thymosin beta-4 (TB4), a 43-amino acid peptide initially derived from bovine thymus glands. The peptide aids tissue recovery by upregulating cell motility and also exhibits significant anti-inflammatory action in various tissues. Research suggests that TB-500 can reduce the accumulation of inflammatory cells at injury sites and hinder the activation of NF-κB, curtailing the release of inflammatory cytokines [1, 2, 3, 4].

2) KPV

KPV, or lysine-proline-valine, is a potent segment of the alpha-Melanocyte-stimulating hormone (alpha-MSH) shown in cell studies and animal disease models to exert strong anti-inflammatory effects. KPV regulates crucial inflammatory processes, including NF-κB pathways, T-cell proliferation, and inflammatory mediator levels, such as TNF alpha [5, 6].

3) BPC-157

BPC-157 is a synthetic pentadecapeptide formulated in the 1990s and noted to foster healing in various tissues, partly by stimulating growth factors and other mediators. Its capability to modulate inflammation by altering nitric oxide production and the action of inflammatory mediators contributes to its beneficial effects [7, 8, 9, 10].

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What are Research Peptides?

Peptides are organic molecules produced in all living organisms, including humans. They are polymers composed of monomers called amino acids, which are bound together through peptide bonds. By convention, proteins encompassing up to 50 amino acids are called peptides, whereas larger proteins are simply called proteins [11].

While peptides share some similarities with proteins, the key differentiator is length and complexity; proteins comprise one or more polypeptide chains that include hundreds to thousands of amino acids [12].

Despite their compact size compared to proteins, peptides are indispensable for myriad physiological activities.

Given their significant roles and ability to precisely target specific receptors, peptides have become a focal point in medical and research arenas.

Their unique sequences enable them to modulate intricate biological pathways, which has led to the synthesis of research peptides that mimic physiological functions with enhanced stability, selectivity, and effectiveness.

As of writing, over 60 peptide-derived medications have been approved by regulatory bodies like the United States Food and Drug Administration (FDA) [13, 14].

Many more peptides are actively researched in settings including but not limited to:

• Reducing inflammation
• Immune system support
• Treating infections
• Speeding up tissue healing
• Longevity and aging processes

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Understanding Peptides and Inflammation

Before delving into how research peptides may help inflammation, it is essential to first understand its role and mechanisms.

Inflammation can be either acute and chronic, both which are vital for human survival. Either form can occur due to a variety of processes, including those related to injury or pathogens. The main purpose of inflammation is to clear infectious agents, dead cells, and cellular debris, facilitating healing and recovery [15].

A controlled inflammatory response is essential for human survival. Yet, both acute and chronic inflammation can become dysregulated:

• When excessive, acute inflammation can cause large amounts of collateral damage and potentially life-threatening complications.
• When dysregulated, chronic inflammation can cause a continuous release of inflammatory mediators and enzymes, which can damage surrounding tissues.

For example, persisting injury in a joint can lead to chronic inflammation and the development of debilitating arthritis, which manifests with joint pain, stiffness, tenderness, swelling, and weakness [16].

Further, excess adipose tissue, especially visceral fat around internal organs, can lead to chronic systemic inflammation and increased risk of atherosclerosis, heart diseases, type 2 diabetes, and even cancer [17].

Research peptides may help regulate both acute and chronic inflammation at various levels:

• Peptides like thymosin beta-4 (TB-500) may work on a cellular level to reduce excessive inflammation by supporting autophagy—a cellular process related to the effective disposal of dysfunctional components and cellular waste [18].
• Peptides like KPV may reduce inflammation by suppressing pro-inflammatory cytokines (signaling molecules) such as TNF alpha [19].
• Peptides like BPC-157 may help regulate inflammation by modulating nitric oxide (NO) synthesis, a key player in inflammation and vasodilation, and inhibiting inflammatory mediators like myeloperoxidase and thromboxane B2 [7].

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Are Peptides Beneficial for Inflammation?

The available evidence on the anti-inflammatory potential of research peptides stems primarily from preclinical research in vitro and in vivo.

Despite the lack of clinical data, available studies on peptides for inflammation showcase significant benefits in experimental models. Here are some of the most notable studies to date:

• In a murine model of autoimmune encephalomyelitis, the application of thymosin beta-4 (TB-500) markedly decreased the number of inflammatory cells in the brains of the treated animals [1].
• In models of liver injury, thymosin beta-4 prevented the activation of nuclear factor kappa B (NF-κB), thereby preventing the production of pro-inflammatory cytokines such as tumor necrosis factor-α (TNF alpha), IL-1β, and IL-6 [1].
• In vitro studies suggest that KPV may ameliorate inflammation in various human cell cultures, including human intestinal cells and human bronchial cells. Additionally, one study also reported significant improvement following KPV administration in a murine model of colitis [19, 20].

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Best Peptides For Inflammation

Below, our expert team will outline the most notable peptides with the potential for modulating inflammation and anti-inflammatory effects based on the available data.

TB-500

TB-500 is a synthetic version of the endogenously-produced thymosin beta-4 (TB4). It was initially developed for veterinary purposes in the early 2010s, and currently lacks approval for human use [21].

TB4 is a 43-amino acid peptide present in most human cells, originally isolated from bovine thymus gland extract in 1981 [2].

Studies suggest that TB4 may influence cell migration, especially in progenitor cells vital for tissue repair. It has also been linked to the formation of new blood vessels, stem cell maturation, various cell type survival, and inflammation reduction [3, 4].

Additionally, a fragment of thymosin beta-4, known as N-acetyl seryl-aspartyl-lysyl-proline (Ac-SDKP), is an orally active peptide that is thought to possess similar healing and anti-inflammatory properties [22, 23].

As mentioned, TB-500 (TB4) has shown potent anti-inflammatory effects in several preclinical experiments [1].

In addition, the peptide has been clinically tested for its healing properties, with data suggesting that its healing potential may be related to reducing inflammation:

• A study in 73 patients with venous ulcers reported that TB-500 sped up wound healing in the patients, with the authors adding that the peptide could achieve complete wound healing in three months in around 25% of the venous ulcer patients [24].
• A 28-day phase 2 clinical study including 9 patients with severe dry eye reported that the peptide may facilitate healing of the eye cornea by reducing inflammation. The study volunteers experienced 35.1% greater reduction in ocular discomfort compared to placebo after 56 days [25].

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KPV

KPV (alpha-MSH 11-13), aka lysine-proline-valine, is the C-terminal segment of endogenous alpha-melanocyte-stimulating hormone (alpha-MSH).

Found in the pituitary gland of various vertebrates, including humans, alpha-MSH acts as a melanocortin receptor agonist. It is integral to melanogenesis, appetite adjustments, and sexual attraction, and showcases anti-inflammatory capabilities. Notably, its C-terminal (KPV) is suggested to mediate these anti-inflammatory effects [5, 26].

KPV’s anti-inflammatory action includes managing responses like NF-κB initiation, T-cell expansion, adhesion molecule representation, inflammatory cytokine and chemokine receptor presentation, and the movement of inflammatory cells [6].

Research suggests that KPV may reduce inflammation and speed up healing in the following settings:

• KPV has been shown in rabbits to reduce inflammation and facilitate faster healing of corneal epithelial wounds compared to placebo [27].
• In murine models of inflammatory bowel disease, KPV exhibited anti-inflammatory properties by speeding up recovery and attenuating colonic cell inflammation, as evidenced by reduced mucosal damage and a significant decrease in TNF alpha levels post-experiment [19, 28].

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BPC-157

BPC-157 (Body Protection Compound-157, PL-10, PL 14736, or Bepecin) is a synthetic pentadecapeptide discovered in the 1990s. It is derived from a gastric protein and does not share any homology with known human peptide sequences [8].

The peptide is researched for its potential to stimulate healing in various tissues, due to the peptide’s ability to activate various growth factors and cells involved in connective tissue repair [9, 10].

BPC-157’s anti-inflammatory potential is also linked to its ability to modulate NO levels and the activity of inflammatory mediators like myeloperoxidase and thromboxane B2 [7].

In a study in rats with surgically transected Achilles tendons, treatment with stable peptide BPC-157 improved the formation of new blood vessels and led to significant improvements in early functional recovery.

The anti-inflammatory effect of BPC-157 was evident through the reduction of myeloperoxidase (an enzyme in inflammatory cells) activity and a decrease in the influx of inflammatory cells into the tissue, as observed in histological samples [29].

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Epithalon

Epithalon is a synthetic tetrapeptide (Ala-Glu-Asp-Gly) that originates from polypeptides present in the pineal gland.

Its longevity-promoting properties have been explored across different tissue types, with epithalon showing promise in decelerating aging. Epithalon’s potential stems from its ability to stimulate telomerase activity within cells, thus extending the length of telomeres, which are key to cellular longevity [30].

Several studies have suggested that epitahlon may ameliorate certain chronic conditions and even reduce mortality rates in older populations [31, 32]

Another contribution to these effects could be eptihalon’s potent antioxidative effects, as reported by numerous preclinical studies [33, 34, 35].

Epithalon's antioxidative action can help to neutralize free radicals, thus preventing cellular damage that can trigger inflammation.

Based on a review of epithalon’s effects on free radicals, conducted by Anisimov et al., the peptide potentially reduces inflammation by stabilizing free radical processes and strengthening antioxidative defense systems [36]. More specifically, the researchers shared that:

• Epithalon suppresses blood serum peroxide chemiluminescence by 2.8-fold and decreases diene conjugate contents by 4.1-fold.
• Epithalon increases general antioxidative activity by 36.6% and superoxide dismutase (SOD) activity by 19.7%.

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Thymalin

Thymalin is a synthetic version of thymulin—a peptide hormone produced by thymic epithelial cells. The peptide is well-regarded for its immune-modulatory and anti-inflammatory capabilities, and research indicates its potential therapeutic implications in various inflammatory conditions.

The molecule may act by inhibiting the phosphorylation of p38 MAPK, a key player in inflammatory response. This modulation reduces the production of pro-inflammatory cytokines like TNF alpha and IL-6.

In addition, thymulin has demonstrated an ability to counteract the accumulation of plasma pro-inflammatory cytokines like IL-1 beta, IL-2, and interferon-gamma [37].

Here are some of the most notable preclinical studies showcasing thymulin’s effects:

• In mice with inflammation induced by lipopolysaccharides (LPS), a prior injection of thymulin was shown to halt the buildup of multiple pro-inflammatory cytokines in plasma. The peptide was also shown to deter the LPS-induced surge in cytokine production by spleen lymphocytes and peritoneal macrophages [37].
• In a rat model of inflammation induced by Complete Freund's adjuvant (CFA), thymulin led to notable reductions in both thermal hyperalgesia and paw edema. These effects were further corroborated by molecular investigations indicating diminished activation of microglia cells and suppressed production of inflammatory mediators [38].
• In a type 1 diabetes mellitus model with streptozotocin-induced diabetes in mice, thymulin lowered concentrations of pro-inflammatory cytokines, including TNF alpha, interleukin-5, and 17, and interferon-γ. Additionally, thymulin inhibited the NF-kB and JNK pathways and decreased Hsp90α expression in immune cells [39].

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ARA-290

ARA-290, also known as Cibinetide and helix B surface peptide (HBSP), is an 11-amino acid peptide synthesized to mimic a portion of the structure of erythropoietin (EPO)—specifically the helix B surface, which interacts with the innate repair receptor (IRR). Unlike EPO, ARA-290 selectively binds to the IRR without promoting erythropoiesis [40].

Clinically, ARA-290 has been tested in phase 2 trials, demonstrating safety and potential efficacy in improving complications in type 2 diabetes and treating small nerve fiber loss in patients with sarcoidosis [41, 42].

Studies have suggested that ARA-290 can reduce inflammation by modulating the activity of the innate immune system, which is responsible for the initial response to infections and tissue damage:

• ARA-290 has been shown to inhibit the activation of macrophages and reduce the production of pro-inflammatory cytokines, such as TNF-alpha and IL-1beta, in models of colon inflammation [43].
• A study in aged rats reported that chronic ARA-290 treatment reduces inflammation and fibrosis in the heart, improves mitochondrial and myocardial cell health, and preserves left ventricular ejection fraction [44].

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GHK-Cu

Copper peptide GHK-Cu is a tripeptide comprising glycyl-L-histidyl-L-lysine that is present within bodily fluids. Known for its repair signaling potential, levels of GHK normally decrease with age [45].

GHK-Cu is under active investigation for its potential effects on collagen, elastin, and hyaluronic acid synthesis. Upregulating these processes can provide various benefits for the skin, ranging from reducing wrinkles to speeding up skin healing [45].

The peptide has also been suggested to reduce inflammation in the skin, primarily by acting as an antioxidant and inactivating damaging free radical byproducts of lipid peroxidation, such as 4-hydroxynoneal, acrolein, malondialdehyde, and glyoxal [46].

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Peptides Side Effects and Safety

Research peptides like BPC-157 and KPV have not undergone comprehensive safety studies in humans. Our information on the safety of these compounds primarily comes from laboratory animal research, with the full spectrum of possible side effects yet to be identified.

On the other hand, existing clinical data for TB4 (TB-500), GHK-Cu, and epithalon show that these compounds are well-tolerated, exhibiting no substantial side effects [31, 47].

For example, in a study examining TB4 (TB-500), 10 participants experienced minor adverse effects when given doses varying from 42 to 1260mg for two weeks. Symptoms reported included occasional headaches, feelings of light-headedness, and mild fever [48].

Overall, a significant challenge with evaluating the safety of anti-inflammatory peptides is the paucity of comprehensive clinical data. Thus, scientists must be vigilant to detect any unexpected side effects during their investigations.

Additionally, since these peptides are typically delivered through subcutaneous injections, attention must be given to the possibility of local reactions at the injection site, such as discomfort, bleeding, swelling, and redness.

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Can Peptides Help With Pain?

Certain research peptides may help to reduce pain by reducing inflammation. Here are some of the most notable peptides with pain-reducing potential:

• BPC-157: In a rat study, BPC-157 demonstrated transient pain-reducing potential following surgical incisions. Rats treated with BPC-157 exhibited significantly higher pain thresholds compared to controls, indicating reduced sensitivity to pain initially and effectiveness in the early phase after incision. This analgesic effect was notable at two hours and persisted somewhat until day four but was not sustained by day seven [7].
• Thymalin: Thymalin was found to alleviate thermal hyperalgesia and paw swelling in a rat model of inflammation. Administered after inducing inflammation, thymalin reduced spinal microglia activation and the production of inflammatory cytokines. This anti-inflammatory action may be linked to thymulin's inhibition of p38 MAPK phosphorylation, highlighting its potential in treating inflammatory pain [38].
• ARA-290: In a rat study, ARA-290 significantly alleviated neuropathic pain and cold allodynia in a dose-responsive manner, with effects lasting up to 20 weeks. It suppressed spinal cord microglia activation, a key factor in neuropathic pain, without affecting astrocyte response. This suggests ARA-290's potential as a targeted therapy for neuropathic pain through its suppression of central nervous system inflammation [49].

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Can Peptides Help With Healing?

Inflammation reduction is one of the main mechanisms via which peptides may help heal various tissues. Peptides like TB-500 and BPC-157 possess potent healing effects related to their anti-inflammatory potential.

In addition, peptides can also help tissue healing via other mechanisms, including but not limited to:

• Upregulation of growth factors: Peptides like BPC-157 may promote the generation of new cellular structures and vasculature by enhancing growth factors, including VEGF and EGR-1. Research indicates that BPC-157 may boost repair in epithelial tissue, muscles, and tendons by elevating EGR-1 and collagen synthesis [9, 10].
• Enhancing progenitor cell migration: TB4 (TB-500) can alter the cytoskeleton of various cells, impacting their movement and reshaping abilities. Such changes can enable progenitor cells from various tissues to converge at the injury site, promoting healing [50, 51].
• Acting as a repair signal: GHK-Cu mirrors a sequence generated when skin collagen is enzymatically degraded after injury, specifically alpha 2(I) collagen. GHK-Cu application may thus simulate a repair cue, triggering restoration mechanisms in tissues like skin [45, 46].

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Inflammation and Peptides | Overall

Research compounds like TB-500, KPV, BPC-157, epithalon, thymalin, ARA-290, and GHK-Cu are at the forefront of research into how peptides may help with inflammatory conditions.

The peptides on our list have shown great potential in targeting chronic inflammation and related diseases, aiding in tissue recovery, and interacting with aging processes by influencing various cellular mechanisms.

Researchers looking to explore the vast potential of peptides for inflammation are highly encouraged to obtain third party-verified compounds from a trusted vendor.

Visit our top recommended source of peptides for inflammation today.

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