Peptidic Compounds Stimulating Extracellular Matrix Synthesis
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Solution Overview
Problem
Current cosmetic and dermopharmaceutical products lack effective compounds that can stimulate the synthesis of key skin extracellular matrix proteins such as collagen, elastin, fibronectin, and laminin, which decline with aging, leading to skin laxity and imperfections.
Innovation Solution
Development of peptidic compounds comprising lysine or its analogs with a grafted carboxylic acid containing a cycle or heterocycle, which are used to enhance the synthesis of these proteins, thereby improving skin firmness, elasticity, and density.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional cosmetic products use standard peptide mixtures, then general skin conditioning is achieved, but stimulation of specific ECM protein synthesis (collagen, elastin, fibronectin, laminin) is insufficient
Solution Approach 1:
The patent modifies the chemical structure of peptides by introducing specific amino acid sequences and modifications (such as N-terminal acetylation, C-terminal amidation, and specific residue substitutions) to enhance their ability to stimulate ECM protein synthesis. These parameter changes in peptide structure directly improve their biological activity and reliability in promoting collagen, elastin, fibronectin, and laminin production.
Solution Approach 2:
The invention uses composite peptide formulations combining multiple different peptides with specific sequences and modifications. These composite peptidic compounds work synergistically to stimulate various ECM proteins simultaneously, achieving comprehensive skin firmness and elasticity improvement that single peptides cannot accomplish alone.
2Quantity of substance
If peptide concentration is increased to improve ECM protein synthesis, then skin firmness and elasticity improve, but product complexity and manufacturing difficulty increase
Solution Approach 1:
The patent achieves enhanced biological activity at lower peptide concentrations through structural modifications including N-terminal acetylation, C-terminal amidation, and specific amino acid substitutions. These parameter changes increase the potency and stability of peptides, allowing effective ECM protein synthesis stimulation without requiring high concentrations that would complicate product formulation and manufacturing.
Data Source
Figure 1
AI summary
The peptidic compound comprises at least an aminoacid which is lysine, ornithine, diaminopropionic acid or diaminobutyric acid or a derivative of these aminoacids, on which a carboxylic acid is grafted via a peptidic bound on the nitrogen of the lateral chain, said carboxylic acid comprising a(poly)cycle or(poly)heterocycle. Preferably, the grafted carboxylic acid is an aminoacid or a derivative, in particular selected from, a proline, a hydroxyproline or pyroglutamic acid. The peptidic compound can stimulate the synthesis of the main molecules constituting the extracellular matrix of the skin, especially collagen 1 and 4 and elastin. It can be used for topical cosmetic treatment such as a global anti-aging treatment, or for specific activities, including anti- wrinkles, moisturizing, to improve the mechanical properties of the skin, firmness/tone/elasticity/flexibility, to increase density and volume of the skin, improve skin radiance, for a restructuring effect and/or to fight stretch marks.