A composition, product containing salicin and uses thereof

By regulating tyrosinase activity through salicin compositions, melanin production is promoted, solving the problem of the lack of effective melanin production promotion in existing technologies and achieving significant melanin production effects. This technology can be applied in the fields of cosmetics and pharmaceuticals.

CN116617103BActive Publication Date: 2026-04-10BLOOMAGE BIOTECHNOLOGY CORP LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-06-14
Publication Date
2026-04-10

AI Technical Summary

Technical Problem

There are no reports in the existing technology that salicylic acid-like substances increase melanin deposition, and there is a lack of ingredients that can effectively promote melanin production.

Method used

A composition containing salicin is provided to promote melanin synthesis by regulating tyrosinase activity. The concentration of salicin in the composition is 0.005%-10%, and it may include melanocyte protectants such as antioxidants and sunscreens. It is suitable for use in cosmetics and pharmaceuticals.

Benefits of technology

Salicylic acid can significantly promote melanin production, increase tyrosinase activity, and enhance the rate of melanin production. It is used in cosmetics and pharmaceuticals, especially for improving and treating gray hair and vitiligo.

✦ Generated by Eureka AI based on patent content.

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Abstract

The application provides a composition containing salicin, a product and application thereof, and relates to the technical field of cosmetics. Specifically, the application provides application of salicin in promoting intracellular melanin synthesis, and it is first proved that salicin can promote intracellular melanin synthesis by promoting tyrosinase activity, thereby providing a new functional ingredient for enhancing intracellular melanin synthesis, and preparing a product for improving and treating white hair and vitiligo.
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Description

TECHNICAL FIELD

[0001] The present application relates to the field of cosmetics, in particular to a composition containing salicin, a product and application thereof. BACKGROUND

[0002] In animals, the synthesis and metabolism of melanin is a complex process. Currently, 663 related genes have been found (http: / / www.espcr.org / micemut / ), which play a regulatory role in melanin metabolism at different stages and in different tissues. The biosynthesis of melanin occurs in the melanosome of melanocytes and involves a series of reactions. Tyrosine is converted into 3,4-dihydroxyphenylalanine (L-dopa) under the catalysis of tyrosinase, and L-dopa is further oxidized to dopaquinone. Dopaquinone generates two types of melanin with different colors, eumelanin and pheomelanin, through two different reaction pathways. The eumelanin synthesis reaction pathway: dopaquinone generates dopachrome through non-enzymatic polymerization and oxidation, and dopachrome forms eumelanin through multiple steps under the action of tyrosinase, tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2, also known as dopachrome isomerase). The pheomelanin synthesis reaction pathway: after dopaquinone is formed, cysteine and glutathione are added to generate glutathionyl dopaquinone, which is finally converted into pheomelanin through ring closure and decarboxylation.

[0003] How to effectively intervene, effectively increase the rate of melanin production, has important value in the field of drugs and cosmetics. There are many Chinese herbs known to increase melanin production, including radix polygoni multiflori, ligustrum lucidum, dried ginger, and salvia miltiorrhiza (reference: Liu X. Screening and pharmacodynamic study of Chinese herbal compound for hair growth and black hair [D]. China Pharmaceutical Industry Research Institute, 2020. DOI: 10.27886 / d.cnki.gyygy.2020.000016.). Melanogenesis-promoting components with a clear molecular structure include melanocyte-stimulating hormone (MSH) (LIM H W, GRIMES P E, AGBAI O, et al. Afamelanotide and narrowband UV-B phototherapy for the treatment of vitiligo [J]. JAMA Dermatol, 2015, 151(1): 42-49.), stilbene glycoside (

[44] Han M N, Lu J M, Zhang G Y, Yu J, Zhao R H. Mechanistic Studies on the Use of Polygonum multiflorum for the Treatment of Hair Graying. Biomed Res Int. 2015;2015:651048.), sulforaphane (Yuan Q P, Liu P T, Cheng L. Use of sulforaphane in the preparation of a pharmaceutical composition for improving and treating white hair and / or hair loss: CN113893237A [P]. 2022-01-07.), tyrosine, and others.

[0004] Salicylic acid substances were first discovered in willow bark. Thousands of years ago, humans discovered that willow trees could reduce fever and relieve pain. In the 18th century, scientists isolated salicin and salicylic acid, which have medicinal value, from willow bark. Later, its analog acetylsalicylic acid, aspirin, was artificially synthesized. Because salicylic acid substances can exert anti-inflammatory and anti-platelet aggregation effects, they have applications in wound care, inflammation, and oral hygiene. However, to date, there have been no reports of salicylic acid substances increasing melanin deposition. SUMMARY

[0005] The purpose of the present application is to provide a composition containing salicin, a product, and its application, which first proves that salicin can be used to promote melanin synthesis.

[0006] In one aspect, the present application provides the use of salicin in promoting melanin synthesis.

[0007] In another aspect, the present application also provides the use of salicin in improving tyrosinase activity.

[0008] Further, the concentration of the salicin is 0.005%-10% by mass; preferably 0.005%-1%.

[0009] Preferably, the concentration of the salicin can be 0.005%, 0.01%, 0.015%, 0.02%, 0.025%, 0.03%, 0.035%, 0.04%, 0.045%, 0.05%, 0.055%, 0.06%, 0.065%, 0.07%, 0.075%, 0.08%, 0.085%, 0.09%, 0.095%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%.

[0010] In another aspect, the present application also provides a composition for promoting melanin synthesis, which comprises salicin.

[0011] Further, the concentration of the salicin is 0.005%-10% by mass; preferably 0.005%-1%.

[0012] Further, the composition further comprises a melanocyte protective agent.

[0013] Further, the melanocyte protective agent comprises an antioxidant, a sunscreen, and / or a nutritional supplement.

[0014] It is conceivable to those skilled in the art that the composition can further comprise known stabilizers, preservatives, foaming agents, flavoring agents, and other functional ingredients, and further adjust the formula of the composition according to different application scenarios and use requirements.

[0015] Preferably, the composition can comprise one or more of sodium lauryl ether sulfate, cocamidopropyl betaine, sodium chloride, citric acid, fragrance oil, hydroxyacetophenone, 1,2-pentanediol, polyquaternium-55, lauryl glucoside, ethylene glycol distearate, laureth-10, cocamide MEA, sodium chloride, phenoxyethanol, parabens, and polyquaternium-10.

[0016] In a preferred embodiment, the ingredients of the composition can be: 10%-20% sodium lauryl ether sulfate, 1%-5% cocamidopropyl betaine, 1%-5% sodium chloride, 1%-5% citric acid, 0.1%-0.5% fragrance oil, 0.1%-0.5% hydroxyacetophenone, 1%-5% 1,2-pentanediol, 1%-5% polyquaternium-55, 1%-5% salicin, and the balance being water.

[0017] In a preferred embodiment, the composition can comprise: 12% sodium lauryl ether sulfate, 2.0% cocamidopropyl betaine, 1.4% sodium chloride, 1.3% citric acid, 0.3% fragrance oil, 0.5% hydroxyacetophenone, 1.0% 1,2-pentanediol, 1.0% polyquatemium-55, 3.0% salicylate, and the balance being water.

[0018] In a preferred embodiment, the composition can comprise: 10%-20% sodium lauryl ether sulfate, 5%-10% lauryl glucoside, 1%-5% ethylene glycol distearate, 1%-5% laureth-10, 1%-5% cocamide MEA, 1%-5% sodium chloride, 1%-5% citric acid, 0.1%-0.5% fragrance oil, 0.1%-0.5% phenoxyethanol, 0.1%-0.5% paraben, 1%-5% polyquatemium-10, 1%-5% salicylate, and the balance being water.

[0019] In a preferred embodiment, the composition can comprise: 12% sodium lauryl ether sulfate, 8.0% lauryl glucoside, 2.0% ethylene glycol distearate, 1.0% laureth-10, 3.0% cocamide MEA, 1.4% sodium chloride, 1.3% citric acid, 0.5% fragrance oil, 0.2% phenoxyethanol, 0.3% paraben, 1.0% polyquatemium-10, 1.0% salicylate, and the balance being water.

[0020] In another aspect, the present application also provides a product comprising the above-mentioned composition.

[0021] Preferably, the product can be in the form of a water agent, an oil agent, or an emulsion.

[0022] More preferably, the product can be a shampoo, a hair conditioner, a hair growth agent, and / or a product for treating vitiligo.

[0023] In another aspect, the present application also provides the use of the above-mentioned composition or the above-mentioned product in promoting melanin synthesis.

[0024] In another aspect, the present application also provides the use of the above-mentioned composition or the above-mentioned product in increasing the activity of tyrosinase.

[0025] In another aspect, the present application also provides the use of the above-mentioned composition or the above-mentioned product in the field of chemistry, the field of medicine, and / or the field of cosmetics.

[0026] Preferably, the use is specifically for promoting melanin synthesis by promoting the activity of tyrosinase.

[0027] The present application has the following advantages:

[0028] 1、The application first proves that salicin can promote tyrosinase activity, thereby enhancing the growth rate of colored substances and the growth rate of melanin, and the tyrosinase activity increases with the increase of salicin concentration, and the melanin growth rate of the 1% salicin treatment group can reach 35.5%, and the colored substance growth rate can reach 25.4%;

[0029] 2、In the application, salicin can promote the synthesis of melanin and colored substances by promoting tyrosinase activity, thereby providing a new functional ingredient for enhancing melanin synthesis in the body, preparing products for improving and treating white hair and vitiligo. DETAILED DESCRIPTION

[0030] In order to more clearly illustrate the overall concept of the application, the following will be described in the form of examples. In the following description, a large number of specific details are given in order to provide a more thorough understanding of the present application. However, it is obvious to those skilled in the art that the present application can be implemented without one or more of these details. In other examples, some technical features known in the art are not described in order to avoid obscuring the present application.

[0031] Unless specific conditions are specified in the examples, the routine conditions or the conditions recommended by the manufacturer are used.

[0032] Among them, salicin is purchased from Shanghai Yuan Ye Biotechnology Co., Ltd.; B16 mouse melanoma cells are purchased from the China Academy of Sciences Typical Culture Preservation Committee Cell Library; RPMI 1640 culture solution containing 10% fetal bovine serum is purchased from HyClone.

[0033] Unless otherwise specified, in the following embodiments, the reagents or instruments used are not specified by the manufacturer, and are all conventional products that can be purchased on the market.

[0034] Example 1 Effect of salicin on melanin synthesis in melanoma cells

[0035] In this example, salicin is used to treat melanoma cells to explore the effect of salicin on melanin synthesis in cells.

[0036] The specific experimental method is as follows: 5x10 4B16 mouse melanoma cells were dispersed in 6-well cell culture plates at a concentration of 1 cell / well. The cells were incubated in RPMI 1640 medium containing 10% fetal bovine serum at 37°C and 5% CO2 for 24 hours. The medium was replaced with fresh medium containing 40 μM forskolin and test compounds, i.e. 1% (35 mM) salicin, 0.3% (10 mM) salicin, 0.06% (2 mM) salicin, 0.3% (10 mM) salicin + 0.1% tyrosine (6.7 mM), and incubated for 96 hours. A group containing only forskolin was used as a blank control. After incubation, the medium was discarded, and 1 M NaOH solution was added to the culture medium, and the cell lysate was collected after 2 hours, centrifuged, and the supernatant was measured for absorbance at 400 nm (A). The melanin production increase rate (pigmentation increase ratio) of each group of cells in the presence of test compounds was calculated, and the test results are shown in Table 1.

[0037] The melanin production increase rate in the presence of test compounds was calculated using the following equation:

[0038] Melanin production increase rate (%) = (A 测试化合物 / A 空白对照 ) x 100% - 100%

[0039] wherein: A 测试化合物 : light absorbance value of the well using the test substance, forskolin, and cells; and A 空白对照 : light absorbance value of the well containing forskolin and cells without the test substance.

[0040] Table 1 Effect of salicin on melanin production

[0041]

[0042] As can be seen from the results in Table 1, the addition of salicin at a concentration of 0.06%, 0.3%, and 1% to melanoma cells can effectively increase the melanin production increase rate. In particular, the melanin production increase rate increases with increasing salicin concentration, and the melanin production increase rate of the 1% salicin treatment group is 35.5%, which is 135.1% higher than that of the 0.3% salicin treatment group.

[0043] The melanin biosynthetic pathway in mammals is generally believed to start from tyrosine, and through a series of complex chemical changes, eventually forms several different types of pigments, collectively known as melanin. Among them, tyrosinase is a key rate-limiting enzyme. The influence on the activity of tyrosinase is considered to be an important factor affecting melanin production. In this example, 0.1% tyrosine and 0.3% salicin were also used for co-treatment, and the results showed that the melanin production growth rate of the combination of the two was 28.4%, thus it is speculated that salicin can promote the production of melanin in melanoma cells by affecting the activity of tyrosinase in melanoma cells.

[0044] Example 2 Effect of salicin on the activity of tyrosinase in melanoma cells

[0045] Based on the results of Example 1, this example further explores the effect of salicin on the activity of tyrosinase in cells.

[0046] The specific experimental method is as follows: B16 mouse melanoma cells were dispersed in a 6-well cell culture plate at a concentration of 1 x 10 5 B16 mouse melanoma cells were dispersed in a 6-well cell culture plate at a concentration of 1 x 10 测试化合物 After the culture was completed, the culture medium was discarded, 0.5 mL of Tris-HCl solution with a pH of 6.8 and a concentration of 1 M was added to lyse the cells, then 1 mL of 0.1% L-dopa was added, and the mixture was incubated at 37°C for 60 min. After centrifugation, the supernatant was collected and the absorbance (A) at 400 nm was measured. The color substance production growth rate (pigmentation increase ratio) of each group of cells in the presence of the test compound was calculated as follows, and the test results are shown in Table 2.

[0047] The melanin production growth rate in the presence of the test compound was calculated using the following equation:

[0048] Color substance production growth rate (%) = (A 空白对照 / A 测试化合物 ) x 100% - 100%

[0049] Wherein: A 测试化合物 : the light absorption value of the well using the test substance, forskolin and cells; A 空白对照 : the light absorption value of the well without the test substance, containing forskolin and cells.

[0050] Table 2 Effect of salicin on the activity of tyrosinase

[0051]

[0052] L-DOPA is a substrate of tyrosinase, and it is known that tyrosinase can catalyze L-DOPA to generate colored substances. Therefore, in this embodiment, L-DOPA is used as a substrate for testing, and the light absorption of the product is detected to evaluate the activity of tyrosinase.

[0053] As can be seen from Table 2, the addition of salicin with a concentration of 0.06%, 0.3% and 1% in melanoma cells can effectively improve the activity of tyrosinase. Moreover, the activity of tyrosinase increases with the increase of the concentration of salicin. Specifically, the growth rate of tyrosinase colored substances in the 1% salicin treatment group is 25.4%, which is increased by 120.9% compared with the 0.3% salicin treatment group.

[0054] Example 3 Application of salicin in promoting the synthesis of melanin related products

[0055] A shampoo containing salicin:

[0056] In this embodiment, a shampoo product containing salicin is provided, and the specific components and amounts of the shampoo are shown in Table 3.

[0057] Table 3 Shampoo formula

[0058]

[0059] A shampoo containing salicin: A shampoo containing salicin:

[0060] In this embodiment, a shampoo product containing salicin is provided, and the specific components and amounts of the shampoo are shown in Table 3.

[0061] Table 4 Shampoo formula for shampoo and hair care two-in-one

[0062]

[0063] The above only describes the embodiments of the present application and is not intended to limit the present application. For those skilled in the art, the present application can have various modifications and changes. Any modification, equivalent replacement, improvement, etc. made within the spirit and principles of the present application shall be included in the scope of the claims of the present application.

Claims

1. Use of salicin in the preparation of a cosmetic product for promoting melanin synthesis.

2. Use of salicin in the preparation of a cosmetic product for increasing the activity of tyrosinase.

3. Use of salicin in the preparation of a product for improving and / or treating white hair and / or vitiligo.

4. Use according to any one of claims 1 to 3, characterized in that, The concentration of salicin is 0.005%-10% by mass.

5. Use according to claim 4, characterized in that, The concentration of salicin is 0.005%-1% by mass.

Citation Information

Patent Citations

  • Application of raphanin in preparation of pharmaceutical composition for improving and treating white hair and / or alopecia

    CN113893237A

  • Use of (2-hydroxyphenyl) alcohols, and cosmetic or therapeutic formulations containing said compounds

    CN1933801A