DPhe-Arg Peptide Melanogenesis Activation for Hair Pigmentation
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Solution Overview
Problem
Current treatments for preventing greying hair are ineffective in addressing the underlying causes of reduced melanin production and melanocyte activity in the hair bulb, leading to inadequate hair pigmentation.
Innovation Solution
Development of peptides and peptidic conjugates containing the sequence DPhe-Arg, which activate melanogenesis in melanocytes, promoting melanin synthesis and transfer within the hair bulb, thereby addressing the reduction in melanin production and melanocyte activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used for preventing greying hair, then hair pigmentation is maintained at current levels, but the underlying causes of reduced melanin production and melanocyte activity are not addressed
Solution Approach 1:
The invention segments the melanocyte stimulating hormone (MSH) into smaller peptide fragments containing the critical DPhe-Arg sequence. These fragmented peptides retain the ability to stimulate melanogenesis while being simpler in structure than full MSH, thereby addressing the technical contradiction between treatment effectiveness and structural complexity.
Solution Approach 2:
The invention extracts the essential DPhe-Arg sequence from the complete MSH structure. By isolating and utilizing only the critical amino acid sequence responsible for melanogenesis stimulation, the patent achieves effective hair pigmentation treatment without requiring the complexity of the full hormone structure.
2Quantity of substance
If melanin production is stimulated in melanocytes, then hair pigmentation is improved, but the number of melanocytes in the hair bulb is reduced
Solution Approach 1:
The peptide acts as an intermediary substance that stimulates melanin production in existing melanocytes without directly affecting melanocyte proliferation or survival. This mediator approach allows increased melanin synthesis while preserving the melanocyte population, resolving the contradiction between melanin quantity and melanocyte reliability.
3Quantity of substance
If melanin synthesis is activated through tyrosinase, then hair colour is enhanced, but the transfer of melanin from melanosomes to keratinocytes is defective
Solution Approach 1:
The peptide maintains continuous stimulation of melanogenesis throughout the melanocyte lifecycle, ensuring both sustained melanin synthesis and continuous transfer to keratinocytes. This continuous action prevents the defect where melanin is produced but not transferred, by keeping the entire melanin production and transfer pathway actively functioning.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The peptides and peptidic conjugates demonstrate a substantial activating effect on melanogenesis, leading to improved hair pigmentation and potential prevention of greying hair, as shown by pharmacological tests and cosmetic application examples.
Implementation Method 1
Melanin synthesis, or melanogenesis, involves tyrosine which is transformed into melanin under the effect of tyrosinase
Implementation Method 2
Tyrosinase is the principal enzyme involved in this cascade reaction
Data Source
AI summary
The invention relates to a peptide of formula W-DPhe-Arg-Z (I) and to a conjugate thereof of a formula A-W-DPhe-Arg-Z (II), wherein A is a radical corresponding to a monocarboxylic acid of general formula HOOC—R (III), wherein R is an linear or branched possibly substituted by a hydroxy group aliphatic C1-C24 radical which can comprise one or several unsaturations, preferably from 1 to 6 unsaturations, a lipoic acid or the reduced form thereof, a dihydrolipoic acid, N-lipoyl-lysine or a phenylbutyric acid, W is His, Ala-His, Ala-Ala-His, Nle-Ala-His, DTrp-Ala-His, Nle-Trp-His, Lys, Ala-Lys, Nle-Ala-Lys, Orn, Ala-Orn, Nle-Ala-Orn, Ala, Nle-Ala-Ala, Arg, Ala-Arg. Nle-Ala-Arg, Nle-Ala-DTrp or a bond in case of compounds of formula (II), Z is NH2, OH and OR, wherein R is a linear or branched aliphatic C1-C24 radical, TrpNH2, NapNH2, TpiNH2, TicNH2, AlaNH2i TrpOH, NapOH, TpiOH, TicOH, AlaOH, PheNH2, or PheOH, exempting a peptidic conjugate for which A is a radical corresponding to an acetic acid, W is Nle-Ala-His and Z is TrpNH2 in the form of enantiomers or diastereoisomer and the mixtures thereof including racemic mixtures. The use of the inventive compounds for cosmetically fighting against canities is also disclosed.