CN-122029178-A - Peptides having skin whitening activity and uses thereof

Abstract

The peptides of the present invention exhibit skin whitening activity by inhibiting melanin synthesis in melanocytes and inhibiting melanosome migration. Thus, the peptide of the present invention can be used 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
• Zheng minqing
• Zheng Duoyuan

Assignees

• 凯尔格恩有限公司

Dates

Publication Date

20260512

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 (i) melanin synthesis or (ii) melanosome migration in melanocytes.
5. 5. The pharmaceutical composition for preventing or treating hyperpigmentation disease as defined in claim 4, wherein said peptide has the following activity: (i) Inhibiting an increase in the phosphorylation level of CREB (cAMP response element binding protein); (ii) Inhibiting the increase of the expression level of MITF (microphthalmia-associated transcription factor), TYR (tyrosinase) or TYRP1 (tyrosinase-associated protein 1), or (Iii) Inhibiting the increase in the expression level of Rab27a, MYO5A or MLPH (melanin avidin) in melanocytes induced in melanin synthesis.
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 skin pigmentation.
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 (i) melanin synthesis or (ii) melanosome migration in melanocytes.
11. 11. Cosmetic composition for skin lightening according to claim 10, wherein said peptide has the following activity: (i) Inhibiting an increase in the phosphorylation level of CREB (cAMP response element binding protein); (ii) Inhibiting the increase of the expression level of MITF (microphthalmia-associated transcription factor), TYR (tyrosinase) or TYRP1 (tyrosinase-associated protein 1), or (Iii) Inhibiting the increase in the expression level of Rab27a, MYO5A or MLPH (melanin avidin) in melanocytes induced in melanin synthesis.
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 skin pigmentation.

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. 10-2023-01383102 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. Melanin synthesis starts with L-tyrosine, and DOPA (DOPA), dopaquinone (DOPAquinone), dopachrome (DOPAchrome) and DHI (5, 6-dihydroxyindole) are synthesized sequentially from L-tyrosine, and finally melanin is synthesized. The reactions of DOPA from L-tyrosine and DOPA to dopaquinone are catalyzed by tyrosinase (tyrosinase), which is the most important enzyme in melanin formation. In addition, enzymes TRP1 (tyrosinase related protein 1) and TRP2 (tyrosinase related protein 2) are also involved in the synthesis of the above melanin. The mechanism by which melanosomes containing melanin move from melanocytes to keratinocytes is not known, but it is known that melanosomes move to dendrites of melanocytes and then are released from dendrites into extracellular space, followed by membrane fusion and phagocytosis between melanosomes and keratinocytes. Melanin avidin (melanophilin), rab27a and myosin (myosin) 5a proteins are known to be involved in the migration of melanosomes into dendrites of melanocytes. Rab27a recognizes and binds to melanosomes, whereas melanin avidin connects Rab27a to myosin 5a (an intracellular cytoskeletal protein). Thus, melanosomes form complexes with Rab27a, melanin avidin and myosin 5a proteins and are transported to the terminal part of the dendrites, eventually reaching keratinocytes （J. Biochem. 2012;151(4):343-351, Lysosome-Related Organelles M Fukuda, Tohoku University, Sendai, Miyagi, Japan 2016 Elsevier Inc）. 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 not only inhibit melanin synthesis in melanocytes but also have an activity of inhibiting melanosome migration, and thus can be developed as skin whiteners and for treating hyperpigmentation diseases, 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