CN-121991168-A - Stapler peptide compound, preparation method and application thereof, and skin care product

Abstract

The invention relates to the technical field of polypeptide compounds, in particular to a staple peptide compound, a preparation method and application thereof, and a skin care product. The structural formula of the stapling peptide compound is shown as follows: . The collagen protein has high enzymolysis stability, can obviously improve the expression capacity of up-regulating fibroblasts, promotes the expression of collagen protein, and can be used in the fields of crease resistance, aging resistance, repair and the like.

Inventors

• SUN HUAIQING
• SUN YUNQI
• GUO CHAOWAN
• FENG CHAO
• NIE YANFENG
• PU YAN
• KUANG XIAOSHAN
• HUANG YI

Assignees

• 广东丸美生物技术股份有限公司

Dates

Publication Date

20260508

Application Date

20260206

Priority Date

20250825

Claims (10)

1. 1. A stapling peptide compound characterized by the following structural formula: 。
2. 2. A method of producing a stapling compound of claim 1, comprising stapling two side chain residues of a linear polypeptide to form said stapling compound, wherein the amino acid sequence of said linear polypeptide is AC-Lys-Glu-Pro-Pro-Pro-Lys-Arg-Pro-Ala-Asp-NH 2 .
3. 3. The method of claim 2, wherein binding comprises reacting the linear polypeptide with activated glutaric acid in the presence of a catalyst system.
4. 4. A process according to claim 3, wherein the means for activating glutaric acid comprises activation with any of bissuccinimide ester, pentafluorophenyl ester, dicyclohexylcarbodiimide carbonate, hydroxybenzotriazole and azide.
5. 5. The method according to claim 3, wherein the molar ratio of the linear polypeptide to the activated glutaric acid is 1 (1-1.5).
6. 6. The method of claim 3, wherein the catalyst comprises at least one of DIC, HOBt, and DIEA.
7. 7. The method of claim 3, wherein the molar ratio of the linear polypeptide to the catalyst is 1 (5-10).
8. 8. Use of a stapled peptide compound according to claim 1 for the preparation of an accelerator for the expression of collagen.
9. 9. Use of a stapling peptide compound according to claim 1 for the preparation of a skin care product for anti-wrinkle, anti-ageing and/or repair.
10. 10. A skin care product comprising the stapled peptide compound of claim 1.

Description

Stapler peptide compound, preparation method and application thereof, and skin care product The present invention claims priority to China patent application number 202511198912.9, entitled "staple peptide Compounds, methods for their preparation and their use and skin care products", the disclosure of which and the description of the claims are incorporated in their entirety into the description of the present invention and are incorporated as part of the original description of the present invention. Technical Field The invention relates to the technical field of polypeptide compounds, in particular to a staple peptide compound, a preparation method and application thereof, and a skin care product. Background The polypeptide compound is an organic compound formed by dehydrating and condensing a plurality of amino acids through peptide bonds (amido bonds), has high target affinity and specificity, is weaker than antibody substances in toxicity and side effects, has better tissue permeability than biological activity advantages such as macromolecules, and is widely applied to the fields of aging resistance, skin repair and the like. However, traditional polypeptide compounds are extremely susceptible to degradation under physiological conditions, which in turn affects the longevity of their efficacy. In view of this, the present invention has been made. Disclosure of Invention The invention aims to provide a stapling peptide compound, a preparation method and application thereof, and a skin care product. The embodiment of the invention provides a novel stapling peptide compound which has high enzymolysis resistance, can obviously improve the expression capacity of up-regulating fibroblasts, promotes the expression of collagen, and can be used in the fields of crease resistance, aging resistance, repair and the like. The invention is realized in the following way: in a first aspect, the present invention provides a stapling peptide compound having the structural formula: 。 In a second aspect, the invention provides a preparation method of the stapling peptide compound, which comprises stapling two side chain residues of a linear polypeptide to form the stapling peptide compound, wherein the amino acid sequence of the linear polypeptide is shown as AC-Lys-Glu-Pro-Pro-Pro-Lys-Arg-Pro-Ala-Asp-NH 2. In an alternative embodiment, the binding process comprises reacting the linear polypeptide with activated glutaric acid in the presence of a catalyst system. In an alternative embodiment, the means for activating the glutaric acid comprises activation with any of bis-succinimidyl ester, pentafluorophenyl ester, dicyclohexylcarbodiimide carbonate, hydroxybenzotriazole and azide. In an alternative embodiment, the molar ratio of the linear polypeptide to the activated glutaric acid is 1 (1-1.5). In an alternative embodiment, the catalyst comprises at least one of DIC, HOBt, and DIEA. In an alternative embodiment, the molar ratio of said linear polypeptide to said catalyst is 1 (5-10). In a third aspect, the present invention provides an application of the staple peptide compound according to the foregoing embodiment in preparing an accelerator for accelerating collagen expression. In a fourth aspect, the present invention provides a use of a staple peptide compound according to the previous embodiments for the preparation of a skin care product for anti-wrinkle, anti-aging and/or repair. In a fifth aspect, the present invention provides a skin care product comprising the stapled peptide compound of the previous embodiment. The invention has the beneficial effects that the embodiment of the invention provides the stapling peptide compound which has higher stability, particularly has high enzymolysis resistance stability, and can ensure the long-acting property of the stapling peptide compound. Meanwhile, the stapler peptide compound can obviously up-regulate the expression capacity of fibroblasts, and improve the expression capacity of various collagens, so that the stapler peptide compound can be used in the fields of crease resistance, aging resistance, repair and the like. Drawings In order to more clearly illustrate the technical solutions of the embodiments of the present invention, the drawings that are needed in the embodiments will be briefly described below, it being understood that the following drawings only illustrate some embodiments of the present invention and therefore should not be considered as limiting the scope, and other related drawings may be obtained according to these drawings without inventive effort for a person skilled in the art. FIG. 1 is a high-level spectrum of a stapled peptide compound provided in example 1 of the present invention; FIG. 2 is a mass spectrum of a stapled peptide compound provided in example 1 of the present invention; FIG. 3 is a graph showing the test results provided in test example 1 of the present invention; FIG. 4 is a graph of test results provided in test example