Whitening cosmetic composition and application thereof

Abstract

The invention discloses a whitening cosmetic composition and application thereof, and relates to the technical field of cosmetics. The cosmetic composition for whitening is prepared from resveratrol and a small molecule dipeptide derivative, wherein the molecular weight of the small molecule dipeptide derivative is 400 to 850Da. According to the cosmetic composition for whitening, the benzylsulfonyl D-seryl high phenylalanine amidino benzylamine acetate and the resveratrol are compounded for use, so that the whitening effect of the resveratrol is improved, and the whitening effect is more remarkable and quicker.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, and in particular to a cosmetic composition for whitening and application thereof. Background Art

[0002] In the field of pharmaceutical chemistry, the research and development of whitening skin care products has always been a hot topic. The main purpose of whitening skin care products is to make the skin whiter and more even by inhibiting the production of melanin or promoting the metabolism of melanin. Resveratrol is a natural antioxidant with antioxidant and anti-inflammatory effects. It is also recognized as a whitening agent with good whitening effects and has been widely used in cosmetics. Benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate (BIO-HPT for short) is a small molecule dipeptide derivative and a cosmetic raw material with anti-wrinkle and firming effects. It can reduce the matrix metalloproteinase MMP9 caused by inflammatory factors, thereby reducing the degradation of type I collagen and type IV collagen.

[0003] Existing whitening technologies mainly inhibit the synthesis of melanin by using various plant extracts and chemical synthetics. For example, resveratrol is a small amount of polyphenols that exist in nature. It exists in grapes, knotweed, and mulberries. It is a strong antioxidant. This raw material has a high degree of recognition in the scientific community and consumers. Resveratrol is a common whitening agent that can regulate multiple targets that affect melanin production, thereby making the skin fair and even.

[0004] In addition, Chinese consumers currently have a high level of awareness of peptides, but peptide substances are generally used in cosmetics for anti-wrinkle, firming and other effects. The small molecule peptide derivatives mentioned in the present invention can reduce collagen degradation by inhibiting MMP9, thereby improving skin quality.

[0005] Although the existing technology shows that resveratrol has a good whitening effect, there are still some problems and limitations. First, the cost of resveratrol is high and it has the characteristics of being insoluble in water and oil, which is difficult to apply in the formula. The present invention uses benzylsulfonyl D-seryl homophenylalanine amidino benzylamine acetate and resveratrol to improve the whitening effect of resveratrol, making the whitening effect more significant and rapid, thereby reducing the use of resveratrol in the formula. The present invention discloses that the addition of a small molecule dipeptide derivative is benzylsulfonyl D-seryl homophenylalanine amidino benzylamine acetate, and its mechanism of action is mainly to reduce the matrix metalloproteinase MMP9 caused by inflammatory factors, thereby reducing the degradation of type I collagen and type IV collagen, and its mechanism of action is not related to the target and whitening. Summary of the invention

[0006] In order to solve the above technical problems, the present invention provides a whitening cosmetic composition and application thereof, which has the advantages of low cost, good whitening effect and good safety.

[0007] The specific technical solutions include the following:

[0008] In a first aspect, a whitening cosmetic composition is provided, comprising resveratrol and a small molecule dipeptide derivative, wherein the molecular weight of the small molecule dipeptide derivative is 400-850 Da.

[0009] Furthermore, the structural formula of the small molecule dipeptide derivative is as follows:

[0010] Wherein, R is a C1 to C6 linear or branched aliphatic hydrocarbon chain, and the aliphatic hydrocarbon chain is substituted by one or more aromatic groups selected from C6 to C10.

[0011] Furthermore, the small molecule dipeptide derivative is benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate.

[0012] Furthermore, the mass ratio of resveratrol to benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate is (50-509):1.

[0013] Furthermore, the whitening cosmetic composition is composed of resveratrol, benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate and deionized water.

[0014] Furthermore, the whitening cosmetic composition comprises the following components in percentage by mass: 0.0509% resveratrol and 0.0001% benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate.

[0015] Furthermore, the whitening cosmetic composition comprises the following components in percentage by mass: 0.05% resveratrol and 0.001% benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate.

[0016] In a second aspect, there is provided use of the whitening cosmetic composition as described in the first aspect in the preparation of cosmetics.

[0017] Furthermore, the mass percentage of the whitening cosmetic composition in the cosmetic is 0.01-2%.

[0018] Furthermore, the cosmetic is one of cream, lotion, facial mask, lotion, and foundation.

[0019] The beneficial effects of the present invention are:

[0020] The present invention uses benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate in combination with resveratrol, thereby improving the whitening effect of resveratrol and making the whitening effect more significant and rapid. DETAILED DESCRIPTION

[0021] The technical solutions in the embodiments of the present invention are described clearly and completely below. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0022] It should be understood that when used in this specification and the appended claims, the terms "include" and "comprises" indicate the presence of described features, integers, steps, operations, elements and / or components, but do not exclude the presence or addition of one or more other features, integers, steps, operations, elements, components and / or combinations thereof.

[0023] It should also be understood that the terms used in this specification of the present invention are only for the purpose of describing specific embodiments and are not intended to limit the present invention. As used in the specification of the present invention and the appended claims, unless the context clearly indicates otherwise, the singular forms "a", "an" and "the" are intended to include plural forms.

[0024] It should be further understood that the term "and / or" used in the present description and the appended claims refers to any and all possible combinations of one or more of the associated listed items, and includes these combinations.

[0025] In order to more fully understand the technical content of the present invention, the technical solution of the present invention is further introduced and illustrated in conjunction with specific embodiments below.

[0026] Example 1

[0027] A cosmetic composition for whitening is composed of the following components in percentage by mass: 0.0509% of resveratrol, 0.0001% of benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate, and the balance of deionized water.

[0028] Example 2

[0029] A cosmetic composition for whitening is composed of the following components in percentage by mass: 0.05% resveratrol, 0.001% benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate, and the balance being deionized water.

[0030] Comparative Example 1

[0031] A cosmetic composition for whitening is composed of the following components in percentage by mass: 0.051% resveratrol and the balance deionized water.

[0032] Comparative Example 2

[0033] A cosmetic composition for whitening is composed of the following components in percentage by mass: 0.001% of benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate and the balance of deionized water.

[0034] Performance Testing

[0035] 1. Experimental Principle

[0036] Melanocytes in the skin produce melanin, which leads to skin problems such as dull skin and spots. 3D melanin model As a testing tool, the sample to be tested is applied to the 3D melanin model by surface drug delivery. The whitening effect of the test substance was evaluated through four dimensional indicators: apparent brightness of the model after administration (L* value), ITA° value, melanin distribution and inflammatory mediators (PGE2).

[0037] The apparent brightness is detected by a colorimeter to measure the chromaticity of the model. The whitening effect of the sample to be tested is evaluated by comparing the surface brightness of the melanin model after the action of different experimental groups. The larger the L* value, the brighter the skin color.

[0038] ITA° (Individual Type Angle) is a parameter used to characterize the color depth of human skin. Its calculation formula is based on the L* and b* values ​​of the skin in the Lab color space. Among them, L* represents the brightness value of the skin in the Lab color space, indicating the lightness and darkness of the skin; b* represents the value of the skin in the yellow-blue direction, representing the color deviation of the skin between yellow and blue. The larger the ITA° value, the lighter the skin color; conversely, the smaller the ITA° value, the darker the skin color.

[0039] Melanin distribution is the result of showing the distribution location of melanin in the skin model. It is analyzed by silver staining. The migration process of melanin from the basal layer to the stratum corneum can be observed from the melanin distribution.

[0040] PGE2 is a typical prostaglandin inflammatory mediator. PGE2 is formed by the cleavage of arachidonic acid by cyclooxygenase. The synthesized PGE2 can bind to the corresponding receptor EP2 on the surface of melanocytes, further activating the transcription pathway of melanin synthesis-related proteins, and regulating the activity of melanocytes, causing changes in the dendritic structure of melanocytes, thereby enhancing the activity of melanocytes and producing more melanin. Therefore, after the test sample is acted on, the content of inflammatory mediator (PGE2) decreases, indicating that it has a certain degree of whitening effect.

[0041] 2. Experimental Purpose

[0042] To explore whether resveratrol and BIO-HPT have whitening effects, and whether their combination can play a synergistic role, and to determine their synergistic mechanism.

[0043] 3. Test Materials

[0044] The 3D melanin model used in this test Batch number: MS241001, provided by Guangdong Boxi Biotechnology Co., Ltd.

[0045] PBS (Soleb), DMSO (Sigma), kojic acid (Yuanye Biotechnology), silver staining kit (Soleb), PGE2 ELISA kit (ENZO).

[0046] IV. Experimental Procedure

[0047] 1. Experimental Preparation

[0048] Prepare a 6-well plate, add 3.7 mL of melanin model culture medium to each well, and transfer the model on the day of model reception (Day 0) to the marked 6-well plate; each experimental group requires 3 models, and transfer all 6-well plates with models to a CO2 incubator for culture (37°C, mass concentration of 5% CO2).

[0049] 2. Stimulation and drug administration

[0050] From the day the model was received (Day 0), the negative control, positive control and sample groups (Example 1-2, Comparative Example 1-2) were irradiated with UVB every day, while the blank control group was not irradiated with UVB, and only the culture medium was replaced every day. The positive control group and sample group were administered with topical administration (2 mg / cm 2 After the model was cultured for 7 consecutive days (Day 7), samples were collected for testing.

[0051] 3. Apparent brightness (L* value) and b* value test

[0052] The L* value and b* value of the model are tested.

[0053] The test operation is as follows: place the model on a flat, hard white surface with the cuticle facing upwards, and align the colorimeter detection hole vertically with the model surface for testing. Repeat the reading three times for each model, and take the average value as the L* and b* value reading of the single model. The L* value is the apparent brightness.

[0054] ITA° value calculation:

[0055]

[0056] The tested model was placed in a clean centrifuge tube for melanin distribution detection.

[0057] 4. Melanin distribution detection

[0058] After the L* and b* value tests were completed, the melanin distribution test was performed on the model. The model was fixed with 4% paraformaldehyde solution for 24 hours, embedded and sliced, and then stained according to the instructions of the silver staining kit and photographed under a microscope.

[0059] 5.ELISA test

[0060] Except for the sample nicotinamide group, the other groups were tested by ELISA. After the incubation, the 3D melanin model was collected The culture medium was placed in a centrifuge tube. After collection, the samples for ELISA detection were placed in a -80°C refrigerator for freezing and storage, and the detection and analysis were performed according to the operating instructions of the ELISA kit.

[0061] 6. Statistical Analysis of Results

[0062] GraphPad Prism was used for graphing, and the results were expressed as Mean ± SD. The t-test was used for statistical analysis between the groups. All statistical analyses were two-tailed. P < 0.05 was considered to be significantly different, and P < 0.01 was considered to be extremely significantly different.

[0063] V. Experimental Results

[0064] 1. L* value; 2. ITA° value; 3. MI value (melanin distribution); 4. PGE2.

[0065] The performance tests were conducted on the whitening cosmetic compositions of Examples 1-2 and Comparative Examples 1-2. The test results are shown in Tables 1-4 below:

[0066] Table 1 L* value test results of Examples 1-2 and Comparative Examples 1-2

[0067]

[0068]

[0069] Table 2 ITA value test results of Example 1-2 and Comparative Example 1-2

[0070]

[0071]

[0072] Table 3 MI value (melanin distribution) test results of Example 1-2 and Comparative Example 1-2

[0073]

[0074]

[0075] Table 4 PEG2 test results of Example 1-2 and Comparative Example 1-2

[0076]

[0077]

[0078] It can be seen from the test results of Tables 1 to 4 that, compared with the single ingredient group (Comparative Example 1 and Comparative Example 2), when the ratio of resveratrol to benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate is 509:1 to 50:1, the whitening cosmetic composition of the embodiment of the present invention has a better effect on the 3D melanin model. Under the test conditions, it has the effect of improving the apparent brightness (L* value) and ITA value, reducing melanin particles, inhibiting the secretion of inflammatory mediators (PGE2), and having a whitening effect. In addition, the whitening cosmetic composition provided by the embodiment of the present invention can reduce the concentration of resveratrol, playing a better, safer and more effective role.

[0079] The above is only a specific embodiment of the present invention, but the protection scope of the present invention is not limited thereto. Any technician familiar with the technical field can easily think of various equivalent modifications or replacements within the technical scope disclosed by the present invention, and these modifications or replacements should be included in the protection scope of the present invention. Therefore, the protection scope of the present invention shall be based on the protection scope of the claims.

Claims

1. A cosmetic composition for whitening, characterized in that: It comprises resveratrol and a small molecule dipeptide derivative, wherein the molecular weight of the small molecule dipeptide derivative is 400-850Da.

2. The skin-whitening cosmetic composition according to claim 1, characterized in that: The structural formula of the small molecule dipeptide derivative is as follows: Wherein, R is a C1 to C6 linear or branched aliphatic hydrocarbon chain, and the aliphatic hydrocarbon chain is substituted by one or more aromatic groups selected from C6 to C10.

3. The skin-whitening cosmetic composition according to claim 1, characterized in that: The small molecule dipeptide derivative is benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate.

4. The skin-whitening cosmetic composition according to claim 3, characterized in that: The mass ratio of the resveratrol to the benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate is (50-509):

1.

5. The skin-whitening cosmetic composition according to claim 4, characterized in that: The invention is composed of resveratrol, benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate and deionized water.

6. The skin-whitening cosmetic composition according to claim 3, characterized in that: The invention comprises the following components in percentage by weight: 0.0509% of resveratrol and 0.0001% of benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate.

7. The skin-whitening cosmetic composition according to claim 3, characterized in that: The invention comprises the following components in percentage by weight: 0.05% of resveratrol and 0.001% of benzylsulfonyl D-seryl homophenylalanine amidinobenzylamine acetate.

8. Use of the whitening cosmetic composition according to any one of claims 1 to 7 in the preparation of cosmetics.

9. Use of the whitening cosmetic composition according to claim 8 in the preparation of cosmetics, characterized in that: The mass percentage of the whitening cosmetic composition in the cosmetic is 0.01-2%.

10. Use of the whitening cosmetic composition according to claim 9 in preparing cosmetics, characterized in that: The cosmetic is one of cream, lotion, facial mask, water solution and foundation.

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