Skin anti-wrinkle composition as well as preparation method and application thereof

Abstract

The invention relates to the technical field of biological composition preparation, and discloses a skin anti-wrinkle composition and a preparation method and application thereof.The skin anti-wrinkle composition is prepared from, by weight, 1.5 wt%-12 wt% of hexose and phosphate thereof, 0.2 wt%-2.0 wt% of organic copper complexes calculated according to Cu < 2 + >, 0.2 wt%-6 wt% of amino acid and the balance water. According to the composition, different physiological functions of all the components in the collagen synthesis process are utilized, and the proportion of all the components is reasonably set, so that the synthesis rate of collagen in skin cells can be greatly increased, and the anti-wrinkle and tightening effects are excellent.

Description

Technical Field

[0001] The present invention relates to the technical field of biological composition preparation, and in particular to a skin anti-wrinkle composition and a preparation method and application thereof. Background Art

[0002] Collagen is a family of proteins that are widely present in organisms. Type I collagen is the fibroblastic collagen in skin and tendon tissues and is the material basis for the skin to maintain elasticity. Collagen deficiency is one of the main causes of wrinkles on the skin.

[0003] The type I collagen molecule is a triple helix structure composed of peptide chains mainly composed of three amino acids: glycine, lysine / hydroxylysine, and proline / hydroxyproline. In cells, the anabolic process of type I collagen includes: on the rough endoplasmic reticulum of cells, through the corresponding mRNA, a procollagen α-peptide chain including 6 peptide regions such as a signal peptide is formed and transferred into the endoplasmic reticulum cavity; the procollagen α-peptide chain is partially hydroxylated by proline 4-hydroxylase, proline 3-hydroxylase, lysine hydroxylase, etc., and then glycosylated at hydroxylysine and asparagine as sites; the modified procollagen α-peptide chain forms a triple helix structure through disulfide bonds, enters the Golgi complex, and then enters the secretory cell body and removes the propeptide to form procollagen; the procollagen is acted on by endonucleases to form procollagen and automatically polymerizes into protofibrils; the protofibrils are specifically covalently cross-linked by lysyl oxidase to finally obtain collagen fibers. The research on the above-mentioned collagen synthesis and metabolism process is increasingly reflected in the application of anti-wrinkle skin care cosmetics.

[0004] Although there are many kinds of anti-wrinkle products on the market, there are not many products that can effectively increase the content of proprotein to achieve long-lasting anti-wrinkle and firming effects. Summary of the invention

[0005] (I) Purpose of the invention

[0006] The purpose of the present invention is to provide a skin anti-wrinkle composition and a preparation method and application thereof, wherein the composition makes full use of the different physiological functions of each component in the collagen synthesis process and greatly improves the collagen synthesis rate in skin cells by setting a reasonable ratio between different components.

[0007] (II) Technical solution

[0008] In order to solve the above problems, the first aspect of the present invention provides a skin anti-wrinkle composition, which comprises the following components by weight percentage: hexose and its phosphate ester are 1.5wt% to 12wt%, and the content of organic copper complex is Cu 2+ The calculated content is 0.2 wt% to 2.0 wt%, the amino acid is 0.2 wt% to 6 wt%, and the rest is water.

[0009] Furthermore, the hexose and its phosphate ester include mannose and mannose-6-phosphate, the content of mannose is 0.5wt% to 4wt% of the skin anti-wrinkle composition, and the content of mannose-6-phosphate is 1wt% to 8wt% of the skin anti-wrinkle composition.

[0010] Further, the organic copper complex includes one or more of glycyl-L-histidine-L-lysine copper, copper ethylenediaminetetraacetate, copper citrate, copper glycinate, copper glutamate, copper aspartate, copper lysine, copper polyaspartate, copper polyglutamate and copper polylysine.

[0011] Furthermore, the amino acids include lysine and proline, the lysine content is 0.1wt% to 3wt% of the skin anti-wrinkle composition, and the proline content is 0.1wt% to 3wt% of the skin anti-wrinkle composition.

[0012] Furthermore, the mass ratio of the lysine to the proline is 1:0.3-3.

[0013] Furthermore, the following components are included by weight percentage: hexose and its phosphate ester are 5wt% to 8wt%, and the content of the organic copper complex is Cu 2+ The amount of cellulose is 1wt% to 1.5wt%, the amount of amino acid is 2wt% to 4wt%, and the rest is water.

[0014] Furthermore, in terms of weight percentage, the mannose content is 2wt% to 3wt% of the skin anti-wrinkle composition, and the mannose-6-phosphate content is 3wt% to 5wt% of the skin anti-wrinkle composition.

[0015] Another aspect of the present invention provides a method for preparing the anti-wrinkle composition described in any one of the above descriptions, comprising the following steps:

[0016] The organic copper complex of the formula ratio is dissolved in water, and stirred at room temperature with a stirring speed of ≤100rpm; then hexose and its phosphate ester and amino acid of the formula ratio are added, and stirring is continued for 1 hour to make them completely dispersed, so as to obtain a skin anti-wrinkle composition.

[0017] The third aspect of the present invention provides a cosmetic active agent with skin anti-wrinkle function, comprising the skin anti-wrinkle composition as described in any one of the above descriptions, and also comprising a polyol.

[0018] Furthermore, in terms of weight percentage, the content of the polyol is 5wt% to 50wt% of the cosmetic active agent with skin anti-wrinkle function.

[0019] (III) Beneficial effects

[0020] The present invention provides a skin anti-wrinkle composition and a preparation method and application thereof. The skin anti-wrinkle composition is prepared by screening various substances that can effectively promote collagen synthesis metabolism, including hexose and its phosphate, organic copper complex and amino acid, etc. These substances have different effects of promoting collagen synthesis, and then they are combined into a composition by using different component ratios, wherein the hexose and its phosphate are 1.5wt% to 12wt%, the content of the organic copper complex is Cu 2+ The composition prepared by the present invention is calculated to be 0.2wt% to 2.0wt%, amino acids are 0.2wt% to 6wt%, and the rest is water. In the in vitro firming and anti-wrinkle efficacy evaluation, the relative content of type I collagen can reach up to 67.7%, which is more than twice that of the positive control. BRIEF DESCRIPTION OF THE DRAWINGS

[0021] Figure 1 It is a result diagram of increasing the collagen I content in the specific embodiments of the present invention and the comparative example. DETAILED DESCRIPTION

[0022] In order to make the purpose, technical scheme and advantages of the present invention clearer, the present invention is further described in detail below in conjunction with specific embodiments and with reference to the accompanying drawings. It should be understood that these descriptions are only exemplary and are not intended to limit the scope of the present invention. In addition, in the following description, the description of well-known structures and technologies is omitted to avoid unnecessary confusion of the concept of the present invention.

[0023] 1. Skin anti-wrinkle composition

[0024] The present invention provides a skin anti-wrinkle composition on one hand, comprising the following components: hexose and its phosphate ester, organic copper complex, amino acid, and the rest is water.

[0025] Among them, hexose and its phosphate include mannose and mannose-6-phosphate. Since mannose-6-phosphate is an important energy storage substance and an important synthetic precursor of hydroxylase cofactor vitamin C, oligosaccharide chains in glycosylation modification and glycosyl donor UDP-galactose (UDP-galactose is diphosphate uridine galactose), it can provide energy for the synthesis of collagen and promote the hydroxylation and glycosylation modification of procollagen α-peptide chain in the synthesis of collagen I. It can effectively promote the synthesis of collagen. In this composition, hexose and its phosphate is a mixture of hexose and hexose phosphate.

[0026] At the same time, signal peptide functional analogs such as glycyl histidyl lysine tripeptide, collagen-forming amino acids such as lysine / hydroxylysine and proline / hydroxyproline, and Fe of hydroxylase 2+ and vitamin C, Cu of lysyl oxidase 2+Coenzymes or cofactors of various biological enzymes such as lysyl oxidase and lysine have been confirmed to promote the synthesis of skin collagen by cell metabolism mechanism and efficacy evaluation. Therefore, in the present invention, organic copper complexes and amino acid components are also added. The organic copper complexes include one or more of glycyl-L-histidine-L-lysine copper, copper ethylenediaminetetraacetic acid, copper citrate, copper glycinate, copper glutamate, copper aspartate, copper lysine, copper polyaspartate, copper polyglutamate and copper polylysine. Since lysyl oxidase is the only biological enzyme involved in the covalent cross-linking of procollagen to obtain collagen fibers, Cu 2+ As the active center (cofactor) of lysyl oxidase, it can effectively increase the level of collagen synthesis; and, due to the free Cu 2+ It is easily affected by phosphate and hydroxide in cosmetic formulas and precipitates, so the use of organic copper complexes is more stable than inorganic copper salts. In addition, if glycyl-L-histidine-L-lysine copper is used as the component of the organic copper complex, the glycyl-L-histidine-L-lysine can be used as an amino-terminal signal peptide analog, which can induce the formation of procollagen α-peptide chains and thereby increase the synthesis of collagen I in cells.

[0027] The amino acids include lysine and proline. The main chain of collagen I molecule is composed of peptide chains mainly composed of three kinds of amino acids: glycine, lysine / hydroxylysine, and proline / hydroxyproline. Hydroxylysine and hydroxyproline are obtained by hydroxylase hydroxylation of lysine and proline in the procollagen α-peptide chain, respectively. Therefore, appropriate supplementation of lysine and proline can effectively increase the content of collagen I in cells.

[0028] Therefore, mannose-6-phosphate, glycyl histidyl lysine tripeptide (glycyl histidyl lysine tripeptide corresponds to the organic acid in the organic copper complex), Cu 2+ , lysine, proline, etc., substances that play different physiological roles in the collagen synthesis process are compounded to form a composition, which can promote each other and effectively enhance the beneficial effects of each component on collagen production.

[0029] Furthermore, in the composition, the components are calculated by weight percentage: hexose and its phosphate ester are 1.5wt% to 12wt%, preferably 5wt% to 8wt%, and the content of the organic copper complex is Cu 2+ Calculated as 0.2wt% to 2.0wt% (referring to the Cu in the organic copper complex 2+ The weight percentage of the anti-wrinkle composition is 0.2wt% to 2.0wt%, preferably 1wt% to 1.5wt%, the amino acid is 0.2wt% to 6wt%, preferably 2wt% to 4wt%, and the rest is water.

[0030] Furthermore, in terms of weight percentage, the mannose content is 0.5wt% to 4wt% of the anti-wrinkle composition, preferably 2wt% to 3wt%, and the mannose-6-phosphate content is 1wt% to 8wt% of the anti-wrinkle composition, preferably 3wt% to 5wt%.

[0031] Furthermore, in terms of weight percentage, the lysine content is 0.1wt% to 3wt% of the skin anti-wrinkle composition, preferably 1wt% to 2wt%, the proline content is 0.1wt% to 3wt% of the skin anti-wrinkle composition, preferably 1wt% to 2wt%. The mass ratio of the lysine to the proline is 1:0.3 to 3, preferably 1:1.

[0032] 2. Preparation method of skin anti-wrinkle composition

[0033] 1. Another aspect of the present invention provides a method for preparing the anti-wrinkle composition as described in any one of the above descriptions, comprising the following steps:

[0034] The organic copper complex of the formula ratio is dissolved in water, and stirred at room temperature with a stirring speed of ≤100rpm; then hexose and its phosphate ester and amino acid of the formula ratio are added, and stirring is continued for 1 hour to make them completely dispersed, so as to obtain a skin anti-wrinkle composition. 2. Specific embodiments

[0036] According to the scheme described in the present invention, a series of compositions with different components and proportions are prepared as examples, using mannose (Man) as a hexose, mannose-6-phosphate (M6P) as a hexose phosphate, glycyl-L-histidine-L-lysine copper (GHK-Cu), ethylenediaminetetraacetic acid copper (EDTACu), aspartate copper (Asp-Cu) or polyaspartate copper (PASPCu) as an organic copper complex, and lysine (Lys) and proline (Pro) as amino acids, and an inorganic water-soluble copper salt copper sulfate (CuSO 4 ) and copper chloride (CuCl 2 ) to replace the organic copper complex as Comparative Examples 1 and 2, and mannose and mannose-6-phosphate solutions without organic copper complex and amino acid as Comparative Example 3, and the specific components thereof are shown in Table 1.

[0037] Table 1 Compositions of different components and ratios

[0038]

[0039] The preparation method is as follows: a quantitative amount of an organic copper complex or copper salt is dissolved in a corresponding amount of deionized water under low-speed stirring at room temperature (stirring speed ≤ 100 rpm) until the solution is completely clarified; in a cold water bath (≤ 10° C.) and under low-speed stirring, hexose and its phosphate ester and amino acid in a formula ratio are added respectively, and the mixture is stirred for 1 hour to allow them to be completely dispersed, thereby obtaining the composition of the present invention.

[0040] 3. Evaluation of the firming and anti-wrinkle efficacy of the composition in vitro (collagen I content)

[0041] The compositions obtained according to the formulas of Examples 1, 2, 3 and Comparative Example 3 were used to investigate their effects on the content of collagen I in human skin fibroblasts to evaluate their firming and anti-wrinkle efficacy in vitro. The materials and equipment required for the test include: human skin fibroblasts (NHDFs), PBS (phosphate buffered saline), FM medium (fibroblast medium), type I collagen ELISA kit, vitamin C, 0.25% trypsin, CO 2 Incubator, biosafety cabinet, inverted microscope, microplate reader, water bath, mixer. The test sample was diluted to 0.32 (%, W / V) with culture medium, and 100 μg / mL vitamin C was used as a positive control, untreated cells as a negative control, and reaction system reagents and solvents as blank controls.

[0042] The test methods include:

[0043] (a) Collect cells in the logarithmic growth phase and set the cell density at 6×10 4 Each well was inoculated into a 12-well plate, with each well containing 100 μL of culture medium.

[0044] (b) In an incubator (37°C, 5% CO 2 ) for 24 h, the test samples and negative controls at different concentrations were added thereto, and 4 replicate wells were set up in each group.

[0045] (c) Incubate in an incubator (37°C, 5% CO 2 ) for 48 h, the culture fluid was collected, and the content of type I collagen in the culture fluid was detected using a Col I ELISA kit. The relative content of type I collagen relative to the blank control was calculated according to the following formula:

[0046] Relative content of type I collagen = collagen content in the dosing well ÷ collagen content in the blank control;

[0047] The above test results can be found in Figure 1 It can be seen that compared with the positive and negative control groups, the test samples have a good promoting effect on increasing the type I collagen content of human skin fibroblasts; at the same time, compared with the results of comparative example 3, the three groups of examples have Cu 2+The effect of promoting the content of collagen I is more obvious; and the three groups of examples have different effects on the increase of collagen I content due to the different ratios of hexose and organic copper complexes. The relative content of type I collagen in Example 1 can reach 63.9%, Example 2 can reach 67.7%, Example 3 can reach 49.1%, and Comparative Example 3 is 43.3%, among which the composition of Example 2 is the best. Comparative Examples 1 and 2 use inorganic copper salts in their formulas, and their test results of the relative content of type I collagen are similar to those of Comparative Example 3, because Cu 2+ This is caused by the formation of insoluble precipitation with anions in the cell culture medium, which makes it unable to play its role.

[0048] 3. Cosmetic active agents with anti-wrinkle function

[0049] 1. The third aspect of the present invention also provides a cosmetic active agent with skin anti-wrinkle function, which includes, in addition to the skin anti-wrinkle composition described in any one of the above descriptions, a polyol, and the polyol content is 5-50% of the cosmetic active agent with skin anti-wrinkle function by weight percentage. The polyol includes at least one of ethylene glycol, propylene glycol, butylene glycol, hexylene glycol and glycerol. The purpose is that the composition composed of hexose and its phosphate ester, organic copper complex and amino acid, each of which is an active ingredient with physiological function and is easily used by microorganisms. Therefore, it is necessary to add a lower alcohol accepted by cosmetics as a preservative ingredient to inhibit the reproduction of microorganisms therein under long-term storage. 2. Specific embodiments

[0051] The composition obtained according to the formula of Example 2 and Comparative Example 3 was sterilized for 20 minutes under steam heating at 80° C. Glycerin was added as an antibacterial component at a mass ratio of 1:1 to obtain an active agent with skin anti-wrinkle function, which was stored at low temperature and away from light.

[0052] 2.1 Preparation of anti-wrinkle cream

[0053] The cosmetic active agent obtained according to the formula of Example 2 and Comparative Example 3 was mixed with a solvent, an excipient and other auxiliary agents, and stirred evenly to obtain a whitening / anti-wrinkle cosmetic composition, the formula of which is shown in Table 2.

[0054] Table 2 Anti-wrinkle cream formula

[0055]

[0056]

[0057] 2.2 Human skin anti-wrinkle experiment

[0058] The anti-wrinkle cream prepared by the composition obtained according to the formula of Example 2 and Comparative Example 3 was used as the experimental group, and 24 volunteers (female, aged 35 to 47 years old, with an average age of 40.6 years old) were recruited and evenly divided into 2 groups corresponding to the above test groups.

[0059] The test method is: the test temperature is 20-22℃, the humidity is 40-60%, the volunteers must have wrinkles on their faces, the test parts are the forehead and cheeks, apply twice a day (once in the morning and once in the evening), and the test time is 0d, 15d and 30d. The ViewSkin (analyzer model) intelligent skin detection analyzer is used to collect facial images and count the changes in wrinkles.

[0060] The test results are shown in Table 3. It can be seen that the anti-wrinkle creams obtained according to the formulas of Example 2 and Comparative Example 3 can effectively smooth and remove facial wrinkles, but the effect of Example 2 is significantly better than that of Comparative Example 3.

[0061] Table 3 Human skin anti-wrinkle test results

[0062]

[0063]

[0064] T-Test value: *3.49×10 5 , **6.92×10 6 , ***3.96×10 4 , ****3.25×10 5 All values ​​are shown as significantly different (asterisks correspond to the asterisks in the table one by one, and the statistical data were obtained using the T-Test method).

[0065] It should be noted that the embodiments described above are only used to explain the present invention and do not constitute any limitation to the present invention. The present invention has been described with reference to typical embodiments, but it should be understood that the words used therein are descriptive and explanatory words, rather than restrictive words. The present invention may be modified as specified within the scope of the claims of the present invention, and the present invention may be revised without departing from the scope and spirit of the present invention. Although the present invention described therein relates to specific methods, materials and embodiments, it does not mean that the present invention is limited to the specific examples disclosed therein, on the contrary, the present invention can be extended to all other methods and applications with the same functions.

Claims

1. A skin anti-wrinkle composition, characterized in that: The components are as follows: hexose and its phosphate ester are 1.5wt% to 12wt%, and the content of organic copper complex is Cu 2+ The calculated content is 0.2 wt% to 2.0 wt%, the amino acid is 0.2 wt% to 6 wt%, and the rest is water.

2. The anti-wrinkle composition according to claim 1, characterized in that: The hexose and its phosphate ester include mannose and mannose-6-phosphate, the content of mannose is 0.5wt% to 4wt% of the skin anti-wrinkle composition, and the content of mannose-6-phosphate is 1wt% to 8wt% of the skin anti-wrinkle composition.

3. The anti-wrinkle composition according to claim 1, characterized in that: The organic copper complex includes one or more of glycyl-L-histidine-L-lysine copper, copper ethylenediaminetetraacetate, copper citrate, copper glycinate, copper glutamate, copper aspartate, copper lysine, copper polyaspartate, copper polyglutamate and copper polylysine.

4. The anti-wrinkle composition according to claim 1, characterized in that: The amino acids include lysine and proline, the lysine content is 0.1wt% to 3wt% of the skin anti-wrinkle composition, and the proline content is 0.1wt% to 3wt% of the skin anti-wrinkle composition.

5. The skin anti-wrinkle composition according to claim 4, characterized in that: The mass ratio of the lysine to the proline is 1:0.3-3.

6. The skin anti-wrinkle composition according to claim 2, characterized in that: The components are as follows: hexose and its phosphate ester are 5wt% to 8wt%, and the content of organic copper complex is Cu 2+ The amount of cellulose is 1wt% to 1.5wt%, the amount of amino acid is 2wt% to 4wt%, and the rest is water.

7. The anti-wrinkle composition according to claim 6, characterized in that: In terms of weight percentage, the content of mannose is 2wt% to 3wt% of the skin anti-wrinkle composition, and the content of mannose-6-phosphate is 3wt% to 5wt% of the skin anti-wrinkle composition.

8. The method for preparing the anti-wrinkle composition according to claims 1 to 7, characterized in that: The following steps are involved: The organic copper complex of the formula ratio is dissolved in water, and stirred at room temperature at a stirring speed of ≤100rpm until the solution is clear; then hexose and its phosphate ester and amino acid of the formula ratio are added, and stirring is continued for 1 hour to make them completely dispersed, to obtain a skin anti-wrinkle composition.

9. A cosmetic active agent with skin anti-wrinkle function, characterized in that: The anti-wrinkle composition of claims 1 to 7 further comprises a polyol.

10. The cosmetic active agent with skin anti-wrinkle function according to claim 9, characterized in that: In terms of weight percentage, the polyol content is 5wt% to 50wt% of the cosmetic active agent with skin anti-wrinkle function.

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