CN-122003431-A - Peptides having skin whitening activity and uses thereof

Abstract

The peptides of the invention exhibit skin whitening activity by inhibiting melanosome uptake in keratinocytes. The peptide of the present invention is useful as an active ingredient in a medicament for treating or preventing a hyperpigmentation disease caused by melanosome hyperpigmentation, or as an active ingredient in a cosmetic for skin whitening.

Inventors

• Zheng Rongchi
• JIN YINMEI
• LI YINGZHI
• Jin Minxiong
• Zheng minqing
• Zheng Duoyuan

Assignees

• 凯尔格恩有限公司

Dates

Publication Date

20260508

Application Date

20241014

Priority Date

20231016

Claims (15)

1. 1. A peptide comprising the amino acid sequence of SEQ ID No. 1.
2. 2. A composition for skin whitening comprising the peptide of claim 1 as an active ingredient.
3. 3. A pharmaceutical composition for preventing or treating hyperpigmentation diseases, comprising the peptide of claim 1 as an active ingredient.
4. 4. A pharmaceutical composition for preventing or treating a hyperpigmentation disease as defined in claim 3, wherein said peptide inhibits the absorption of melanosomes in keratinocytes.
5. 5. The pharmaceutical composition for preventing or treating a hyperpigmentation disease according to claim 4, wherein said peptide inhibits the expression of (i) PAR2 (protease-activated receptor 2) gene or (ii) KGFR (keratinocyte growth factor receptor) gene in keratinocytes.
6. 6. A pharmaceutical composition for preventing or treating a hyperpigmentation disease as defined in claim 3, wherein said hyperpigmentation disease is a disease that occurs when the amount of melanin in the skin is excessively increased.
7. 7. The pharmaceutical composition for preventing or treating a hyperpigmentation disease as defined in claim 3, wherein said hyperpigmentation disease is chloasma, freckle, age-related pigmentation, solar lentigo or post-inflammatory hyperpigmentation.
8. 8. A pharmaceutical composition for preventing or treating hyperpigmentation disease as defined in claim 3 wherein said pharmaceutical composition is a topical skin preparation.
9. 9. A cosmetic composition for skin whitening comprising the peptide of claim 1 as an active ingredient.
10. 10. The cosmetic composition for skin whitening according to claim 9, wherein the peptide inhibits the absorption of melanosomes in keratinocytes.
11. 11. The cosmetic composition for skin whitening according to claim 10, wherein the peptide inhibits the expression of (i) PAR2 (protease activated receptor 2) gene or (ii) KGFR (keratinocyte growth factor receptor) gene in keratinocytes.
12. 12. The cosmetic composition for skin whitening according to claim 9, wherein the cosmetic composition is a topical skin preparation.
13. 13. The cosmetic composition for skin whitening according to claim 12, wherein the cosmetic composition is at least one dosage form selected from the group consisting of a solution, a suspension, an emulsion, a paste, a gel, a cream, a lotion, a powder, a soap, a surfactant-containing cleanser, an oil, a powder foundation, an emulsion-type foundation, a waxy foundation, and a spray.
14. 14. A method for preventing or treating a hyperpigmentation disease comprising administering the peptide of claim 1 or a composition comprising said peptide to a subject in need of prevention or treatment of a hyperpigmentation disease.
15. 15. The method for preventing or treating a hyperpigmentation disease according to claim 14, wherein said hyperpigmentation disease is chloasma, freckle, age-related pigmentation, solar lentigo or post-inflammatory hyperpigmentation.

Description

Peptides having skin whitening activity and uses thereof Cross Reference to Related Applications The present application claims priority based on korean patent application No. 10-2023-01383103 filed on 10 months 16 of 2023, the entire contents of which are incorporated herein as part of the present specification. Technical Field The present invention relates to peptides having skin whitening activity and uses thereof. Background Skin melanin (cutaneous melanin) present in the skin, hair follicles, and eyes plays a vital role in protecting the skin from ultraviolet rays. However, excessive melanin production can lead to hyperpigmentation diseases such as chloasma, freckles and age spots, leading to reduced psychological stress and quality of life. Melanin is synthesized mainly in melanocytes (melanocytes) located between or below the basal layers of the epidermis (basal layers) and in hair follicles (hair follicle). Melanin is synthesized in the organelle melanosomes (melanosomes) within melanocytes. These melanosomes migrate through dendrites (dendrotes) to nearby keratinocytes (keratinocyte) and when the keratinocytes rise to the outer layer, they present a skin tone. The mechanism by which melanosomes migrate from melanocytes to keratinocytes is not known, but it is known that melanosomes migrate to dendrites of melanocytes and then are released from dendrites into the extracellular space, followed by membrane fusion and phagocytosis between melanosomes and keratinocytes (phagocytosis). Receptors such as PAR-2 (protease activated receptor 2, protease-ACTIVATED RECEPTOR), KGFR (keratinocyte growth factor receptor ) and TLR (Toll-like receptors) are known to be involved in the regulation of the phagocytosis of melanosomes by keratinocytes. Melanin is finally synthesized starting from L-tyrosine via DOPA (DOPA), dopaquinone (DOPAquinone), dopachrome (DOPAchrome) and DHI (5, 6-dihydroxyindole). Traditionally, inhibition of melanin synthesis has focused on factors that inhibit tyrosinase activity, an enzyme that catalyzes the rate control step of the melanin synthesis pathway. PCT International publication No. WO2020/153819 discloses polypeptides having an effect of inhibiting tyrosinase (a key enzyme in the melanin synthesis pathway) activity and their use for skin whitening. In addition, korean patent No. 10-1869783 describes peptides having an effect of inhibiting melanin production and tyrosinase activity and their use for whitening. Previous skin whitening agent developments have focused on inhibiting tyrosinase (a key enzyme in melanin synthesis) activity. However, in order to achieve a synergistic skin whitening effect through different sites of action, it is necessary to develop skin whitening agents having different mechanisms and sites of action. [ Prior Art literature ] [ Patent literature ] WO2020/153819 Korean patent No. 10-1869783 Disclosure of Invention Technical problem The present inventors have conducted research work to develop peptides with more improved skin whitening activity. As a result, the present inventors have experimentally confirmed that the novel peptides they developed have very excellent inhibitory activity on the uptake of melanosomes into keratinocytes (uptake), and that the peptides of the present invention can be used as active ingredients of skin whiteners, thereby completing the present invention. Accordingly, it is an object of the present invention to provide novel peptides having skin whitening activity. It is another object of the present invention to provide a composition for skin whitening comprising the peptide having the above-mentioned activity as an active ingredient. It is still another object of the present invention to provide a pharmaceutical composition for preventing or treating hyperpigmentation diseases, which comprises a peptide having the above-mentioned activity as an active ingredient. It is still another object of the present invention to provide a cosmetic composition for skin whitening comprising the peptide having the above-mentioned activity as an active ingredient. Technical proposal In order to achieve the above object, One aspect of the invention provides a peptide comprising the amino acid sequence of SEQ ID NO. 1. In another aspect of the present invention, there is provided a composition for skin whitening comprising the peptide as an active ingredient. In yet another aspect of the present invention, there is provided a pharmaceutical composition for preventing or treating hyperpigmentation diseases, comprising said peptide as an active ingredient. In yet another aspect of the present invention, there is provided a cosmetic composition for skin whitening comprising the peptide as an active ingredient. Hereinafter, the present invention will be described in detail. 1. Peptides and their activity According to one aspect of the present invention there is provided a peptide comprising the amino acid sequence disclosed in SEQ ID NO. 1. [ Amino