Peptides with Immobilized Aromatic Cycles for Skin Whitening

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Solution Overview

Problem

Current cosmetic products for addressing skin hyperpigmentation and skin aging issues, such as those using tyrosinase inhibitors, have not yielded satisfactory results, and there is a need for more effective lightening agents that minimize secondary effects.

Innovation Solution

The use of peptides with immobilized aromatic cycles, specifically peptides following the structure A-(Xa)m-Xc-(Xb)n-B, where A and B are defined by certain amino acid residues and Xc is an aromatic amino acid, which inhibit melanogenesis and are used in dermopharmaceutical and cosmetic compositions to lighten or whiten the skin.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional tyrosinase inhibitors are used for lightening skin pigmentation, then some lightening effect is achieved, but the results are not satisfactory and secondary effects occur

Engineering Contradiction:

Improvelightening effectivenessVSAvoidsecondary effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention changes the chemical structure parameter of the peptide by introducing an immobilized aromatic cycle (cyclic structure) at positions Xa or Xb, which fundamentally alters the interaction mechanism with melanogenesis pathways, achieving superior lightening效果 without the harmful secondary effects of conventional inhibitors

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The peptide combines multiple functional components: aromatic cycles (for structural stability and target interaction), amino acid residues (for biological activity), and specific sequences (for melanogenesis inhibition), creating a composite molecular structure that achieves both effectiveness and safety

Inventive Principle:

Principle #40Composite materials

2Reliability

If existing lightening ingredients are used to address hyperpigmentation, then some pigmentation reduction is achieved, but the results are not satisfactory enough

Engineering Contradiction:

Improvepigmentation reduction effectivenessVSAvoidmolecular structure complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The peptide is segmented into distinct functional domains: the immobilized aromatic cycle segment (providing structural rigidity and target binding), the amino acid sequence segment (providing biological activity), and the terminal groups (A and B, providing solubility and stability), allowing optimization of each segment's function

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention introduces local quality by placing the immobilized aromatic cycle at specific positions (Xa or Xb) within the peptide chain, creating localized structural features that enhance target interaction while maintaining overall peptide flexibility and bioavailability

Inventive Principle:

Principle #3Local quality

Data Source

PatentEP2510982B1Cosmetic compositions comprising at least one peptide with at least one immobilized aromatic cycle

Publication Date: 2017.04.26 SEDERMA SA

AI summary

Topical cosmetic use as a whitening active ingredient of at least one peptide, comprising at least one immobilized aromatic cycle and having the general formula (I): A- (Xa)m-Xc-(Xb)n-B. The invention also discloses a cosmetic composition comprising at least said peptide and a method of decreasing skin pigmentation, whitening or lightening human skin, comprising a topical application of said composition.