Editor’s Note
Peptides are often hailed as the building blocks of youthful skin, but how exactly do they work? In this deep dive, we present a scientific analysis by Dr. Tan Kian Meng on the role of enzyme-inhibiting peptides. From neutralizing collagen-destroying enzymes to harnessing the power of Chia seeds, this paper uncovers the biochemical pathways to skin rejuvenation.
Key Takeaways
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The Enemy: Enzymes like Elastase and Matrix Metallopeptidases (MMPs) break down our skin’s structure.
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The Trigger: UV light and pollution cause Reactive Oxygen Species (ROS), accelerating these destructive enzymes.
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The Solution: Bioactive peptides from sources like Soy, Rice, Silk, and Chia seeds act as “inhibitors,” stopping the breakdown of collagen and elastin.
Enzyme inhibitory peptides can directly or indirectly inhibit enzymes that break down collagen or other proteins besides interfering with that process. They operate primarily by inhibiting the activity of skin ageing related enzymes, specifically matrix metallopeptidase (MMPs) as well as elastase, tyrosinase, hyaluronidase and collagenase.
The Mechanism of Skin Ageing
Daily exposure to light can lead to the accumulation of reactive oxygen species (ROS), triggering an upsurge in the production of MMPs. This, in turn, results in excessive degradation of collagen in extracellular matrix (ECM) proteins leading to the loss of skin elasticity and firmness.
ROS, reactive oxygen species; AhR, arylhydrocarbon receptor; NF-kB, nuclear factor kappa-B; IL, interleukin; TNF-α, tumor necrosis factor; CCN1, cysteine-rich protein 61; MAPK, mitogen-activated protein kinase; AP-1, activator protein 1; MMPs, matrix metalloproteinases; ROS, reactive oxygen species; UV, ultraviolet; VEGF, vascular endothelial growth factor
Figure 1: Mechanism of skin-ageing and rejuvenation by skin-ageing related enzyme activity.
There are numerous enzyme inhibitor peptides sources such as soy oligopeptides, rice-derived peptides and silk fibroin peptides have been used as inactive ingredients for skincare products.
Targeting Elastase: A New Frontier
While a couple of peptides have been developed as active cosmeceutical ingredients specifically targeting MMPs, there is a paucity of clinical data reporting elastase as the focal point for anti-ageing strategy. MMPs and elastase both are reported to cause the degradation of extracellular matrices (e.g. collagen and elastin) in human skin.
Elastase is a member of the chymotrypsin family of proteases which is primarily responsible for the breakdown of elastin (an important protein in ECM). It can cleave not only elastin but collagen, fibronectin and other ECM proteins as well.
Summary of Skincare Ingredients
The following table summarizes potential enzyme inhibiting peptides to be used as skincare ingredients:
| Name of Peptide | Commercial Name | Mechanism of Action | Cosmetic Functionality |
| Soybean amino acids | N/A | Inhibits MMPs (proteinase formation), increases the length and number of hair roots. | Increase collagen, elastin and fibronectin synthesis. |
| Rice peptides | N/A | Inhibits matrix metalloproteinase, MMPs activity. Induces expression of hyaluronan synthase gene in keratinocyte. | Inhibition of tyrosinase, increase melanogenesis inhibition, improve skin elasticity, reduce TEWL, minimise skin irritation. |
| Silk proteins (derived from silkworm Bombyx mori) | N/A | Antioxidant activity with high affinity to chelate with copper. It also inhibits lipid peroxidation and tyrosinase activity and keratinocyte apoptosis. | Reduce melanin synthesis. |
| Chia seed peptides | N/A | Peptide fraction F-II presented the highest potential for elastase inhibition. | N/A |
| Serpin A1-III (α-1 antitrypsin) | KP1 | Physiological inhibitor of neutrophil elastase, which prevent the degradation of ECM components. | Wound healing, modulation of collagen turnover, anti-wrinkles, dark eye circles. |
References
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Aguilar-Toalá JE, Liceaga AM. Identification of chia seed (Salvia hispanica L.) peptides with enzyme inhibition activity towards skin-aging enzymes. Amino Acids. 2020;52(8):1149-1159.
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Aguilar-Toalá, J.E., et al. Potential role of natural bioactive peptides for development of cosmeceutical skin products. Peptides 2019, 122, 170170.
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Ahsan, H. The biomolecules of beauty: Biochemical pharmacology and immunotoxicology of cosmeceuticals. J. Immunoass. Immunochem. 2018, 40, 1–18.
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Ferreira, M.S., et al. Trending anti-aging peptides. Cosmetics 2020, 7, 91.
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Fries, K.S.; Heldreth, B. Safety Assessment of Soy Proteins and Peptides as Used in Cosmetics. Int. J. Toxicol. 2023, 42.
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Manosroi, A., et al. Anti-aging efficacy of topical formulations containing niosomes entrapped with rice bran bioactive compounds. Pharm. Biol. 2012, 50, 208–224.
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Pickart, L.; Schagen, S. New data of the Cosmeceutical and tripeptide GHK. SOFW J. 2015, 9, 141.
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Schagen, S.K. Topical Peptide Treatments with Effective Anti-Aging Results. Cosmetics 2017, 4, 16.
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Schurink, M., et al. Novel peptides with tyrosinase inhibitory activity. Peptides 2007, 28, 485–495.
