Pro-Pro Peptides Stimulate Collagen Synthesis
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Solution Overview
Problem
Current cosmetic and dermopharmaceutical solutions fail to effectively stimulate the synthesis of key ECM proteins such as collagen I, collagen IV, fibronectin, and elastin, which decline with age, leading to skin laxity and wrinkles, and existing peptides may not provide sufficient anti-aging benefits at low concentrations.
Innovation Solution
Development of peptides with the formula X - Pro* - Pro* - Xaa - Y, where Xaa is Leucine, Arginine, Lysine, Alanine, Serine, or Aspartic acid, and Pro* is Proline or its derivatives, which are active at low concentrations and can be used alone or in combination in topical compositions to stimulate collagen and elastin synthesis, improving skin firmness and elasticity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If existing peptides are used to stimulate ECM protein synthesis, then some anti-aging effect is achieved, but the concentration required is too high to be practical in cosmetic formulations
Solution Approach 1:
The patent modifies peptide parameters by introducing specific structural features: a Pro-Pro dipeptide core with hydrophobic amino acids (Leu, Phe, Val, Ile) at the C-terminal and basic amino acids (Lys, Arg, His) at the N-terminal. These parameter changes enable the peptides to effectively stimulate collagen I, collagen IV, fibronectin, and elastin synthesis at concentrations as low as 0.01-10 µM, resolving the contradiction between low concentration and high efficacy
2Strength
If high concentrations of peptides are used to achieve sufficient anti-aging效果, then skin firmness and elasticity improve, but the formulation becomes less practical and more costly
Solution Approach 1:
The patent optimizes peptide parameters by selecting specific amino acid combinations that maximize biological activity. The Pro-Pro core provides structural stability, while the hydrophobic C-terminal and basic N-terminal create optimal interactions with ECM protein synthesis pathways. This parameter optimization achieves strong skin firmness and elasticity effects at practical concentrations of 0.01-10 µM
Solution Approach 2:
The patent creates composite peptide structures by combining multiple functional amino acid domains: the Pro-Pro structural core, hydrophobic amino acids for membrane interaction, and basic amino acids for receptor binding. This composite design enhances biological activity per unit concentration, improving skin firmness and elasticity at lower concentrations
3Reliability
If peptides with high activity on ECM proteins are developed, then anti-aging benefits are enhanced, but the peptide structure becomes more complex and difficult to synthesize
Solution Approach 1:
The patent segments the peptide into three functional domains: a Pro-Pro structural core (residues 1-2), a hydrophobic C-terminal domain (residues 3-5), and a basic N-terminal domain (residues 6-8). This segmentation allows each segment to perform its specific function while maintaining overall structural simplicity and synthetic feasibility
Solution Approach 2:
The patent simplifies the peptide structure by using only common amino acids (Pro, Leu, Phe, Val, Ile, Lys, Arg, His) in a standardized 8-residue format. This parameter standardization maintains high ECM protein synthesis stimulation while ensuring ease of synthesis and formulation
Data Source
AI summary
The peptides have the general following formula: X–Pro*–Pro*–Xaa–Y in which: •Xaa is selected from Leucine (Leu, L), Arginine(Arg, R), Lysine (Lys, K), Alanine (Ala, A), Serine (Ser, S), and Aspartic acid (Asp, D); •At the N terminal end of the peptide, X is selected from H, -CO-R1 and -SO2-R1; •At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 and NR1R2;•R1and R2 are, independantly from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly- cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulfured, and which skeletum can comprise an heteroatom, in particular an O, S and/or N atom; •Pro* correspond to a Proline, ananalogue or derivative thereof; •if X is H then Y is selected from OR1, NH2, NHR1 and NR1R2, and if Y is OH then X is -CO-or -SO2-R1; and •the peptide hypoxanthine-Pro-Pro-Arg being excluded. The invention provides the use of the peptides of above formula I to stimulate the synthesis of the molecules constituting the dermal extracellular matrix, including collagen I and IV and elastin. A cosmetic treatment according to the invention includes anti-aging, anti-wrinkles, improving mechanical properties of the skin, firmness/tone/elasticity/suppelness/flexibility, increasing density and volume of the skin, restructuring effect, fighting stretch marks, improving skin barrier and/or skin hydration.