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Peptides in Acne Therapy

for more than a century, amino acid sequences are of interest to scientists. Peptide regulation is spoken in a wide variety of variations. Peptides are used in biochemistry and cosmeceuticals, in regenerative medicine and in aesthetic gynecology.
Peptides have gained particular popularity over the past few decades in cosmetology and dermatology. Skin as a neuroendocrine organ is an ideal target for peptide exposure.

Since 2015, they have been talking about peptides in combination acne therapy protocols.

To date, the market has more than 60 peptide drugs that have received FDA approval. About 130 more are at the stage of clinical trials and 600 at the stage of preclinical development.

Peptides, Acne
Peptide classification
Peptide is a term denoting a molecule consisting of two or more amino acids that are interconnected by a peptide bond. Peptides with less than ten amino acid residues in their molecules formally belong to oligopeptides, peptides built from a larger number of amino acid residues (up to 100) belong to polypeptides. Proteins are sequences that contain more than 50 amino acid residues.

By the number of amino acids contained in the peptide, di-, tri-, tetra-, penta-, octa, decapeptides, etc. are distinguished. Bodanski proposed to avoid the problems with Greek numbering, designate the number of amino acid residues of the peptide in Arabic numerals and put before the word “ peptide”. So the names familiar to doctors and patients appeared, for example, 7-peptide instead of heptapeptide (Yakubke 1985).

Peptides are widely distributed in nature in all cellular organisms (the so-called peptide pool). Peptide hormones that are formed in different organs are most studied by their action.

When developing external products, peptides from animal and plant poisons, as well as peptide antibiotics, which will be discussed later, are of great importance.

Peptides in the treatment of acne: why?
One of the links in the pathogenesis of acne is the excessive activity of Propionibacterium acnes.

The modern view of inflammation as the main link in the pathogenesis of acne makes doctors and scientists look for different ways to suppress inflammation and reduce the activity of Propionibacterium acnes.

Here antimicrobial peptides come to the forefront, let’s see what is hidden behind this phrase that is important for science.

Antimicrobial peptides
They are relatively short molecules (on average about 30–40 amino acids) that can cause the death of microorganisms. Antimicrobial peptides are involved in the innate immunity system.

To date, more than 800 such peptides have been characterized. They include molecules from tissues and cells of invertebrates, vertebrates, plants and fungi; some chemokines, cytokines, neuropeptides, neurohormones and protein fragments. A number of peptides are also produced by the microorganisms themselves.

Four main classes of antimicrobial peptides are distinguished:

Molecules with a beta-folding structure that is stabilized by two or three disulfide bonds
Alpha-helical molecules
Linear peptides
Loop-like peptides (a loop is formed due to the formation of a single disulfide bond).
Currently, clinical trials of several antimicrobial peptides are active, including those against P. acnes.

CEN1HC-Br is isolated from a green sea urchin. In experiments in mice, it showed stronger antimicrobial activity against P. acnes than clindamycin, significantly reducing the expression of interleukins IL-12p40, IL-6, IL-1β, TNF-α, and TLR2 in monocytes not affected by clindamycin.

The in vitro peptides ASP-1 and ASP-2 have been shown to be effective against particular species and polymicrobial biofilms. When introduced into gels or dressings, both peptides destroyed mono- and polymicrobial biofilms of pathogens.

Peptide Esc (1-21) obtained from frog skin also destroyed the bacterial biofilm (up to 85% for some strains) and caused a more than four-fold decrease in the number of bacterial cells within 20 minutes and bacterial adhesion (77–97%) within 24 hours.

Another peptide RGN 137 is a natural peptide consisting of 43 amino acids and is present in almost all human cells. It stimulated the differentiation of endothelial cells and cell migration, suppressed a number of inflammatory cytokines and chemokines, and the induction of collagen deposition.

For the treatment of papulopustular rosacea, intraepithelial neoplasia of the vulva, genital warts, acne vulgaris and atopic dermatitis, CLS001 (omiganan pentahydrochloride) is being developed.

High activity against resistant strains of Pseudomonas aeruginosa and Staphylococcus aureus, Trichomonas vaginalis, Candida albicans, Aspergillus niger, Mucor sp. and Trichophyton mentagrophytes exhibit the peptides Demegel, Wap-8294A2, LTX-109 and D2A21, and PXL01 obtained from human lactoferrin showed antimicrobial activity in the local therapy of postoperative adhesions and scars.

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