Peptide Sequence Stimulating Extracellular Matrix Synthesis

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Solution Overview

Problem

Current cosmetic and pharmaceutical solutions lack effective, broad-spectrum active ingredients that can stimulate skin regeneration and restructuring of the dermis while being dermatologically compatible, especially for addressing skin aging and external aggressions like UV exposure.

Innovation Solution

A peptide of the general formula R1-(AA)n-Ile-X1-Leu-X2-Phe-Leu-X3-(AA)p-R2, which stimulates the synthesis of extracellular matrix molecules such as fibronectin, type I and type III collagen, and keratins, is used in cosmetic, nutraceutical, or pharmaceutical compositions for topical or oral application.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cosmetic and pharmaceutical active ingredients are used, then skin aging manifestations can be addressed to some extent, but they lack broad-spectrum effectiveness and strong dermatological compatibility

Engineering Contradiction:
Improvedermatological compatibilityVSAvoidbroad spectrum of action
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by designing a peptide sequence that performs multiple functions simultaneously: it stimulates collagen synthesis, promotes elastin production, enhances skin regeneration, and provides protection against various aggressors (UV radiation, pollution). This multi-functional peptide replaces the need for multiple separate active ingredients, achieving broad-spectrum effectiveness while maintaining dermatological compatibility through its natural amino acid composition.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent utilizes parameter changes by optimizing the peptide's amino acid sequence parameters (specifically incorporating Ile-X1-Leu-X2-Phe-Leu-X3 motifs) to achieve optimal biological activity. By adjusting the chemical parameters of the peptide structure (hydrophobicity, charge, conformation), the invention maximizes its effectiveness across multiple skin functions while maintaining compatibility with dermatological tissues.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If active ingredients with strong effectiveness are sought, then dermatological compatibility may be compromised, potentially causing irritant reactions

Engineering Contradiction:
ImproveeffectivenessVSAvoidirritant reactions
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies this principle by using naturally occurring amino acids that are inherently biocompatible and non-irritating, yet when arranged in the specific peptide sequence, they produce potent biological effects. The naturally benign building blocks (amino acids) are converted into a highly effective active ingredient through strategic sequencing, achieving strong effectiveness without the harmful side effects typically associated with potent cosmetic ingredients.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The peptide acts as an intermediary molecule that mediates between the application and skin tissues. Rather than using direct-acting chemicals that may cause irritation, the peptide serves as a natural mediator that communicates with skin cells (fibroblasts, keratinocytes) through physiological pathways, stimulating their natural functions without causing harmful reactions. This intermediary approach ensures both effectiveness and compatibility.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If existing peptide solutions are used, then some extracellular matrix stimulation is achieved, but no peptide with the specific sequence pattern R1-(AA)n-Ile-X1-Leu-X2-Phe-Leu-X3-(AA)p-R2 has been described

Engineering Contradiction:
Improveextracellular matrix stimulationVSAvoidpeptide sequence complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the peptide into functional domains: N-terminal region (R1-(AA)n), central active motif (Ile-X1-Leu-X2-Phe-Leu-X3), and C-terminal region (-(AA)p-R2). Each segment contributes differently to the overall function, with the central motif being particularly critical for extracellular matrix stimulation. This segmentation allows for systematic optimization of each region's contribution while managing the overall sequence complexity.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2250187B1Peptide and cosmetic and/or pharmaceutical composition containing the same
Publication Date: 2012.12.12 SOCIETE D DEXTRACTION DES PRINCIPES ACTIFS (VINCIENCE SA)
  • EP2250187B1 patent drawing
  • EP2250187B1 patent drawing
  • EP2250187B1 patent drawing

AI summary

The present invention relates to a peptide of formula (I): R1-(AA)n-Ile-X1-Leu-X2-Phe-Leu-X3-(AA)p-R2, for stimulating the synthesis of the principal proteins of the extracellular matrix of the skin. The present invention also relates to a cosmetic, nutraceutical or pharmaceutical composition comprising a peptide of formula (I) as active agent. The invention also relates to the use of this novel active agent in a cosmetic or nutraceutical composition for preventing and/or combating the manifestations of skin ageing and for stimulating skin regeneration. The invention also relates to the use of this novel active agent for the preparation of a pharmaceutical, and in particular dermatological, composition for improving healing.