Application of dipeptide as soothing raw material, composition with soothing effect and cosmetic
By using Ala-Tyr to reduce the levels of inflammatory factors IL-6 and TNF-ɑ, the side effects caused by long-term use of glucocorticoids in the prior art are solved, providing a safe and reliable anti-inflammatory soothing solution.
Patent Information
- Application Number
- CN202411951171.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-12-26
- Publication Date
- 2025-04-01
AI Technical Summary
In the prior art, long-term use of glucocorticoids to treat skin inflammation can easily lead to side effects such as exogenous Cushing syndrome, and there is a lack of safe and reliable alternatives to anti-inflammatory compounds.
Using Ala-Tyr as a soothing raw material, it was verified by cellular experiments that it can reduce the levels of inflammatory factors IL-6 and TNF-ɑ, providing a new anti-inflammatory dipeptide.
Ala-Tyr significantly reduces the level of inflammatory factors, has anti-inflammatory and soothing effects, can relieve symptoms such as redness and itching of the skin, and provides a safe and reliable anti-inflammatory solution.
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Abstract
Description
Technical Field
[0001] The present invention belongs to the technical field of cosmetics, and in particular relates to an application of a dipeptide as a soothing raw material, a composition with soothing efficacy, and cosmetics. Background Art
[0002] The skin is the first barrier of the human body and has many functions in maintaining human life activities, such as preventing water evaporation and electrolyte loss; maintaining body temperature; preventing pathogens and some toxic substances from entering the body. When affected by exogenous factors such as ultraviolet rays, dust particles, drugs, etc. or endogenous factors such as ischemia and hormone metabolism, the skin may be infected. In order to cope with the infection, the body will release a large number of inflammatory factors. Inflammation is a natural defense reaction of the body against external stimuli and infection by pathogenic microorganisms. However, excessive inflammatory reactions can cause the body's immune system to be out of balance, thereby causing damage to the body's tissue structure, which manifests on the skin as seborrheic dermatitis, contact dermatitis, allergic dermatitis, hormone-dependent dermatitis, atopic dermatitis, neurodermatitis, etc.
[0003] Currently, the typical drug for these skin inflammations is glucocorticoids. Although glucocorticoids can be used to treat inflammation, long-term use of glucocorticoids can lead to side effects such as exogenous Cushing's syndrome. Therefore, it is of great significance to find a new anti-inflammatory compound.
[0004] Peptides are composed of amino acids, have unique biological functions, are complex and varied, and are widely present in the human body. Compared with glucocorticoids, they are safer and more reliable, so finding anti-inflammatory active raw materials from peptides has become a new strategy. Summary of the invention
[0005] In view of this, the technical problem to be solved by the present invention is to provide an application of a dipeptide as a soothing raw material, a composition and cosmetics with soothing effects.
[0006] Ala-Tyr is a dipeptide that is used to study cell uptake mechanisms and dipeptide metabolism. It can also be used as a nutrient for cell culture. It has not yet been used as a soothing raw material in the cosmetics field. The specific information of the polypeptide is shown in Table 1. The present invention studies the effect of Ala-Tyr on RAW264.7 cells through cell experiments. The compound can reduce the levels of inflammatory factors IL6 and TNF-ɑ in RAW264.7 cells and has an anti-inflammatory effect. Therefore, the present invention provides an application of a dipeptide as a soothing raw material, wherein the dipeptide is Ala-Tyr.
[0007] More specifically, the present invention also provides the use of Ala-Tyr as a soothing raw material in the field of cosmetics.
[0008] Table 1 Basic information of Ala-Tyr
[0009]
[0010] More specifically, the Ala-Tyr is used as an anti-inflammatory and soothing raw material.
[0011] The dipeptide provided by the present invention is applicable to the field of cosmetics. Cell experiments have shown that Ala-Tyr can reduce the content of inflammatory factors IL-6 and TNF-ɑ, has a soothing effect, and can solve the problem of facial inflammation in sensitive people.
[0012] The present invention also provides a composition with soothing effect, comprising a dipeptide; the dipeptide is Ala-Tyr.
[0013] More specifically, the soothing composition also includes blue copper peptide.
[0014] More specifically, the mass ratio of the dipeptide to the blue copper peptide is 2:1 to 1:2; optionally, the mass ratio of the dipeptide to the blue copper peptide is 2:1, 1.5:1, 1:1, 1:1.5, 1:2 or a range between any two of the above ratios.
[0015] In a specific embodiment provided by the present invention, the mass ratio of the dipeptide to the blue copper peptide is 1:1.
[0016] More specifically, the composition with soothing effect is a composition with anti-inflammatory and soothing effect.
[0017] The composition provided by the present invention can relieve symptoms such as skin redness and itching, and has significant anti-inflammatory and soothing effects.
[0018] The present invention also provides a cosmetic comprising the above-mentioned composition with soothing effect.
[0019] More specifically, the mass of the composition with soothing effect is 0.1% to 6% of the mass of the cosmetic; optionally, the mass of the composition with soothing effect is 0.1%, 0.5%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6% of the mass of the cosmetic or a range between any two of the above values.
[0020] In a specific embodiment provided by the present invention, the mass of the composition with soothing effect is 3% of the mass of the cosmetic.
[0021] In a specific embodiment provided by the present invention, the cosmetic is an essence.
[0022] Further preferably, in terms of mass percentage, the essence comprises 85% to 95% of component A, 0.1% to 6% of component B, 2% to 6% of component C and 0.1% to 2% of component D; the component A is a matrix component; the component B is a composition with soothing effect; the component C comprises a first antioxidant and / or a first moisturizer; the component D comprises a second antioxidant and / or a second moisturizer; the thermal stability of the first antioxidant is higher than that of the second antioxidant; and the thermal stability of the first moisturizer is higher than that of the second moisturizer.
[0023] Optionally, the mass of component A is 85%, 86%, 87%, 88%, 89%, 90%, 91%, 92%, 93%, 94%, 95% of the mass of the essence or a range between any two of the above values.
[0024] In a specific embodiment provided by the present invention, the component A is a matrix component, including water, glycerin, a chelating agent and an emulsifier stabilizer; the mass of the water is 84% to 87% of the mass of the essence, more preferably 85% to 85%, and more preferably 85.65%; the mass of the glycerin is preferably 1% to 3% of the mass of the essence, more preferably 1.5% to 2.5%, and more preferably 2%; the mass of the chelating agent is preferably 0.01% to 0.1% of the mass of the essence, more preferably 0.02% to 0.08%, more preferably 0.04% to 0.06%, and most preferably 0.05%; the chelating agent is preferably EDTA-2Na; the mass of the emulsifier stabilizer is preferably 0.5% to 1.5% of the mass of the essence, more preferably 0.8% to 1.2%, and more preferably 1%; the emulsifier stabilizer is preferably sodium polyacryloyldimethyl taurate.
[0025] Optionally, the mass of component B is 0.1%, 0.5%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6% of the mass of the essence or a range between any two of the above values.
[0026] The B component is the above-mentioned composition with soothing effect.
[0027] Optionally, the mass of component C is 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6% of the mass of the essence or a range between any two of the above values.
[0028] Optionally, the mass of the D component is 0.1%, 0.5%, 0.6%, 1%, 1.2%, 1.5%, 1.8%, 2% of the mass of the essence or a range between any two of the above values.
[0029] In a specific embodiment provided by the present invention, the C component includes a first antioxidant and / or a first moisturizer; the D component includes a second antioxidant and / or a second moisturizer; the thermal stability of the first antioxidant is higher than that of the second antioxidant; the thermal stability of the first moisturizer is higher than that of the second moisturizer; the total mass of the first moisturizer and the second moisturizer is preferably 2% to 6% of the mass of the essence, more preferably 3% to 5%, and more preferably 4%; the mass ratio of the first moisturizer to the second moisturizer is preferably (5 to 10): 1, more preferably (6 to 8): 1, and more preferably is 7:1; the first moisturizing agent is preferably methylpropanediol and / or hexylene glycol; the second moisturizing agent is preferably D-panthenol; the total mass of the first antioxidant and the second antioxidant is preferably 0.1% to 2% of the mass of the essence, more preferably 0.4% to 1.5%, more preferably 0.4% to 1%, more preferably 0.4% to 0.8%, and most preferably 0.6%; the mass ratio of the first antioxidant to the second antioxidant is preferably (2 to 8):1, more preferably (4 to 6):1, and more preferably 5:1; the first antioxidant is preferably p-hydroxyacetophenone; the second antioxidant is preferably ergothioneine.
[0030] The present invention also provides a method for preparing the above-mentioned essence, which can be prepared according to methods well known to those skilled in the art without any special restrictions, specifically: heat and sterilize component A and then cool it for the first time, add component B and homogenize it for the first time, add component C and homogenize it for the second time, cool it for the second time, add component D, homogenize it for the third time, and cool it to room temperature to obtain the essence.
[0031] Further preferably, the temperature of the heating sterilization is preferably 115°C to 125°C, more preferably 120°C to 121°C; the time of the heating sterilization is preferably 10 to 20 min, more preferably 14 to 16 min, and even more preferably 15 min.
[0032] More preferably, the temperature of the first cooling is preferably 50°C to 60°C, more preferably 55°C; the temperature of the second cooling is preferably 40°C to 50°C, more preferably 45°C.
[0033] More preferably, the time for the first homogenization, the second homogenization and the third homogenization is each independently preferably 10 to 60 seconds, more preferably 20 to 40 seconds, and even more preferably 30 seconds. BRIEF DESCRIPTION OF THE DRAWINGS
[0034] Figure 1 This is a graph showing the effects of different substances on the inflammatory factor IL-6 in Example 1 of the present invention;
[0035] Figure 2This is a graph showing the effects of different substances on the inflammatory factor TNF-α in Example 1 of the present invention;
[0036] Figure 3 This is a graph showing the results of different ratios of Ala-Tyr and GHK-Cu soothing essence in Example 2 of the present invention improving histamine pain;
[0037] Figure 4 This is a graph showing the results of different ratios of Ala-Tyr and carnosine soothing essence in comparative example 1 of the present invention improving histamine pain. DETAILED DESCRIPTION
[0038] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative work are within the scope of protection of the present invention.
[0039] In order to further illustrate the present invention, the application of a dipeptide provided by the present invention as a soothing raw material, a composition with soothing effect and a cosmetic are described in detail below in conjunction with examples.
[0040] The reagents used in the following examples are all commercially available; among them, mouse macrophages (RAW264.7) are from Wuhan Pronocell Life Science Co., Ltd.; lipopolysaccharide (LPS) is from Beijing Solebold Technology Co., Ltd.; RAW264.7 special culture medium is from Wuhan Pronocell Life Science Co., Ltd.; mouse tumor necrosis factor α (TNF-α) enzyme-linked immunosorbent assay kit is from Wuhan Elaruite Biotechnology Co., Ltd.; mouse interleukin 6 (IL-6) enzyme-linked immunosorbent assay kit is from Wuhan Elaruite Biotechnology Co., Ltd.
[0041] Example 1
[0042] Ala-Tyr has anti-inflammatory effects and can reduce the levels of inflammatory factors IL-6 and TNF-ɑ.
[0043] Experimental process: 2 million RAW264.7 cells (P9) were plated in each well of a 6-well plate (RAW264.7 special culture medium). After 24 hours, dexamethasone (DEX, 100ppm) and Ala-Tyr (1000ppm) were added. After 1.5h, 2μL of 1000ppm LPS (LPS was dissolved in culture medium) was added to the control group. The culture was continued for 24 hours, the supernatant was collected, centrifuged, and the supernatant was taken. The TNF-α experiment was diluted 200 times and the IL-6 experiment was diluted 50 times, and then the ELISA kit was used for detection. Within 15 minutes after adding the stop solution, the absorbance at 450nm was detected.
[0044] Experimental results: The effects of different substances on the inflammatory factor IL-6 are as follows Figure 1 The results of the effects of different substances on the inflammatory factor TNF-α are shown in Figure 2 As shown. Lipopolysaccharide (LPS) can promote inflammation, produce a large number of inflammatory factors and promote the expression of related inflammatory proteins. LPS is often used to activate mouse leukemia macrophages (RAW264.7) as a cell inflammation model. Figure 1 and Figure 2 It can be seen that compared with the negative control group, the IL-6 concentration and TNF-ɑ concentration in the Ala-Tyr group decreased by 23% and 30%, respectively, and were statistically significant (P<0.05 was considered statistically significant, "**", P<0.01; "****", P<0.0001). This shows that Ala-Tyr can significantly reduce the levels of inflammatory factors (IL-6, TNF-ɑ) and has soothing and anti-inflammatory effects.
[0045] Example 2
[0046] Prepare soothing essence. Prepare component A according to the formula in Table 2, stir component A, disperse it evenly, heat and sterilize it (121°C×15min), then stir it evenly, wait for it to cool (temperature 55°C), add component B, homogenize for 30s, add component C, homogenize for 30s, stir evenly, cool to 45°C, add component D, homogenize for 30s, cool to room temperature, filter, and obtain the final soothing essence.
[0047] Table 2 Formulas of soothing essence with different ratios of Ala-Tyr and carnosine
[0048]
[0049] Histamine stimulation is a classic model for inducing inflammation. Skin inflammation caused by histamine mainly includes: itching, redness, pimples, blisters, etc. Using the performance of the histamine model, the anti-inflammatory and redness-removing ability test is fast and intuitive.
[0050] Number of testers: 5; Gender: Both men and women; Age: 18-55 years old; The itch / pain scoring standard is shown in Table 3; These 5 people showed obvious severe itch / pain in response to histamine stimulation, and could not help scratching / unbearable, that is, the itch / pain scoring standard for histamine stimulation was 5 points for the volunteers.
[0051] Each subject took 6 2×2 cm areas on the inner side of the arm and applied 0.02 g of the sample.
[0052] Test method (puncture method): Use a puncture needle to puncture the test area on the inside of the arm, with no bleeding as the standard; use 1% histamine phosphate solution, drip 0.02mL on the inside of the arm, absorb the histamine solution after 5 minutes, and wait for about 10 minutes. Apply 0.02g of sample to the sample area and the control area 2×2cm area, record the redness and itching of the arm at each time point, and score and record. Evaluate the test site after 15 minutes, and the results are shown in Table 4.
[0053] Histamine pain improvement rate (%) = (5-histamine pain score n minutes after histamine prick modeling) × 100% / 5.
[0054] Table 3 Itch / pain scoring criteria
[0055]
[0056] Table 4 Soothing effects of different ratios of Ala-Tyr and GHK-Cu soothing essence
[0057]
[0058] Experimental results: Different ratios of Ala-Tyr and GHK-Cu soothing essence improve histamine pain. Figure 3 As shown in Table 4 and Figure 3 It can be seen that soothing essences with different ratios of Ala-Tyr and GHK-Cu can relieve the stinging sensation caused by histamine to a certain extent, among which the combination of Ala-Tyr and GHK-Cu has a better effect. When the ratio of Ala-Tyr:GHK-Cu is 2.0:1.0, 1.5:1.5, and 1.0:2.0, the improvement rate of histamine stinging is higher than that of using Ala-Tyr or GHK-Cu alone, among which the ratio of 1.5:1.5 has the best effect, with significant difference (P<0.05 is considered statistically significant, "*", P<0.05), so Ala-Tyr and GHK-Cu have a synergistic effect.
[0059] Comparative Example 1
[0060] Prepare soothing essence. Prepare component A according to the formula in Table 5, stir component A to disperse it evenly, heat and sterilize it, then stir it evenly, add component B after cooling, homogenize for 30 seconds, add component C, homogenize for 30 seconds, stir evenly, cool to 45°C, add components D and E, homogenize for 30 seconds, cool to room temperature, filter, and obtain the final soothing essence.
[0061] Table 5 Formulas of soothing essence with different ratios of Ala-Tyr and carnosine
[0062]
[0063] Histamine stimulation is a classic model for inducing inflammation. Skin inflammation caused by histamine mainly includes: itching, redness, pimples, blisters, etc. Using the performance of the histamine model, the anti-inflammatory and redness-removing ability test is fast and intuitive.
[0064] Number of testers: 5; Gender: Both men and women; Age: 18-55 years old; These 5 people showed obvious severe itching / pain in response to histamine stimulation, and could not help scratching / could not bear it, that is, the itch / pain scoring standard for histamine stimulation was 5 points for the volunteers.
[0065] Each subject took 6 2×2 cm areas on the inner side of the arm and applied 0.02 g of the sample.
[0066] Test method (puncture method): Use a puncture needle to puncture the test area on the inside of the arm, with no bleeding as the standard; use 1% histamine phosphate solution, drip 0.02mL on the inside of the arm, absorb the histamine solution after 5 minutes, and wait for about 10 minutes. Apply 0.02g of sample to the sample area and the control area 2×2cm area, record the redness and itching of the arm at each time point, and score and record. Evaluate the test site after 15 minutes, and the results are shown in Table 6.
[0067] Histamine pain improvement rate (%) = (5-histamine pain score n minutes after histamine prick modeling) × 100% / 5.
[0068] Table 6 Soothing effect of different ratios of Ala-Tyr and carnosine soothing essence
[0069]
[0070]
[0071] Experimental results: Different ratios of Ala-Tyr and carnosine soothing essence improve histamine pain. Figure 4 As shown in Table 6 and Figure 4It can be seen that different proportions of Ala-Tyr and carnosine soothing essence can relieve the stinging sensation caused by histamine to a certain extent, but the combination of Ala-Tyr and carnosine does not have a better effect, indicating that Ala-Tyr and carnosine do not have a synergistic effect.
[0072] The above is only a preferred embodiment of the present invention. It should be pointed out that for ordinary technicians in this technical field, several improvements and modifications can be made without departing from the principle of the present invention. These improvements and modifications should also be regarded as the scope of protection of the present invention.
Claims
1. Use of a dipeptide as a soothing raw material, wherein the dipeptide is Ala-Tyr.
2. A composition with soothing effect, characterized in that: A dipeptide is included; the dipeptide is Ala-Tyr.
3. The composition according to claim 2, characterized in that Also included is blue copper peptide.
4. The composition according to claim 3, characterized in that The mass ratio of the dipeptide to the blue copper peptide is 2:1 to 1:
2.
5. The composition according to claim 3 or 4, characterized in that The mass ratio of the dipeptide to the blue copper peptide is 1:
1.
6. A cosmetic, characterized in that: A composition with soothing effect comprising any one of claims 2 to 5.
7. The cosmetic according to claim 6, characterized in that: The mass of the composition with soothing effect is 0.1% to 6% of the mass of the cosmetics.
8. The cosmetic according to claim 6, characterized in that: The mass of the composition with soothing effect is 3% of the mass of the cosmetics.
9. The cosmetic according to claim 6, characterized in that: The cosmetic is an essence; in terms of mass percentage, the essence comprises 85% to 95% of component A, 0.1% to 6% of component B, 2% to 6% of component C and 0.1% to 2% of component D; the component A is a matrix component; the component B is a composition with soothing effect; the component C comprises a first antioxidant and / or a first moisturizer; the component D comprises a second antioxidant and / or a second moisturizer; the thermal stability of the first antioxidant is higher than that of the second antioxidant; the thermal stability of the first moisturizer is higher than that of the second moisturizer.
10. The cosmetic according to claim 9, characterized in that: The component A includes water, glycerin, a chelating agent and an emulsifier stabilizer; the mass of the water is 84% to 90% of the mass of the essence; the mass of the glycerin is 1% to 3% of the mass of the essence; the mass of the chelating agent is 0.01% to 0.1% of the mass of the essence; the mass of the emulsifier stabilizer is 0.5% to 1.5% of the mass of the essence; The total mass of the first moisturizer and the second moisturizer is 2% to 6% of the mass of the essence; the mass ratio of the first moisturizer to the second moisturizer is (5 to 10):1; the total mass of the first antioxidant and the second antioxidant is 0.1% to 2% of the mass of the essence; the mass ratio of the first antioxidant to the second antioxidant is (2 to 8):1.