Composition for inhibiting tyrosinase activity

A synergistic composition of GSH, γ-GC, and CG addresses the ineffectiveness of existing tyrosinase inhibitors, achieving enhanced skin whitening and beautification with natural, safe ingredients.

JP7829071B2Active Publication Date: 2026-03-12MITSUBISHI CORP LIFE SCI LTD
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2024-01-30
Publication Date
2026-03-12

AI Technical Summary

Technical Problem

Existing compositions for inhibiting tyrosinase activity are not effective enough for skin whitening and beautification, necessitating a composition with enhanced inhibitory effects.

Method used

A composition comprising glutathione (GSH), γ-Gly-Cys (γ-GC), and Cys-Gly (CG) in specific weight ratios, providing a synergistic inhibitory effect on tyrosinase activity.

Benefits of technology

The combined use of GSH, γ-GC, and CG exhibits a synergistic effect, resulting in superior skin whitening and beautifying outcomes, with all components being naturally occurring and safe for the body.

✦ Generated by Eureka AI based on patent content.

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Abstract

[Problem] To provide a whitening and skin care composition having excellent tyrosinase activity inhibitory effects. [Solution] The present invention was completed by discovering that excellent tyrosinase activity inhibitory effects can be obtained by using glutathione (GSH) as a cysteine-containing peptide together with γ-Gly-Cys (γ-GC) and Cys-Gly (CG). In particular, these components are preferably used in combination at the composition ratio (weight ratio) of the GSH, γ-GC, and CG being 1:0.01 to 1:0.005-0.50.
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Description

[Technical Field]

[0001] The present invention relates to a composition for inhibiting tyrosinase activity that is suitable for use in whitening and skin beautifying applications. [Background technology]

[0002] Although the mechanisms of skin pigmentation, age spots, and freckles are still unclear, one possible cause is thought to be excessive melanin production and deposition in the skin due to hormonal abnormalities or excessive or chronic exposure to ultraviolet light. Tyrosinase is an enzyme that catalyzes the oxidation of tyrosine or dopa, which are the source of melanin, and activation of tyrosinase promotes melanin production.

[0003] Therefore, tyrosinase activity inhibitors are used in foods, beverages, and cosmetics for whitening and skin beautifying purposes, and known inhibitors include ascorbic acid, kojic acid, arbutin, L-cysteine, etc. However, these inhibitors alone may not be effective enough, and in most cases, multiple compounds are used in combination to more effectively inhibit tyrosinase activity.

[0004] Glutathione is also known to inhibit tyrosinase activity, and its combined use with α-lipoic acid (Patent Document 1), plants of the genus Bungeishunju (Patent Document 2), L-cystine (Patent Document 3), etc. has been reported for whitening and skin beautifying purposes. However, there is a demand for compositions with even better tyrosinase activity inhibitory effects. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] Patent Publication No. 2009-51768 [Patent Document 2] Patent Publication No. 2008-303180 [Patent Document 3] Patent Publication No. 2016-88875 DISCLOSURE OF THE INVENTION [Problem to be solved by the invention]

[0006] An object of the present invention is to provide a composition for whitening and beautifying skin, which has an excellent tyrosinase activity inhibitory effect. [Means for solving the problem]

[0007] As a result of extensive research into solving the above problems, the inventors have discovered that the combined use of glutathione (GSH), a cysteine-containing peptide, with γ-Gly-Cys (γ-GC) and Cys-Gly (CG) provides an excellent inhibitory effect on tyrosinase activity.

[0008] That is, the present invention provides: (1) A composition for inhibiting tyrosinase activity comprising GSH, γ-GC, and CG; (2) The tyrosinase activity inhibitory composition according to (1) above, wherein the composition ratio (weight ratio) of GSH, γ-GC, and CG is 1:0.01 to 1:0.005 to 0.50, preferably 1:0.05 to 0.50:0.01 to 0.30, and more preferably 1:0.10 to 0.21:0.03 to 0.13. (3) A skin-improving food or drink containing the composition of (1) or (2). (4) A skin-improving cosmetic comprising the composition of (1) or (2). (5) A skin-improving drug containing the composition of (1) or (2) above. This relates to: [Effects of the Invention]

[0009] In the present invention, the combined use of the cysteine-containing peptides glutathione (GSH), γ-glutamylcysteine ​​(γ-Gly-Cys:γ-GC), and cystenylglycine (Cys-Gly:CG) exhibits an excellent synergistic effect rather than an additive effect resulting from the sum of the tyrosinase activity inhibitory effects of each compound, resulting in excellent whitening and skin-beautifying effects. Furthermore, because GSH, γ-GC, and CG are naturally present in foods and in living organisms, they are highly safe for the body. DETAILED DESCRIPTION OF THE INVENTION

[0010] The present invention will be specifically described below. The composition of the present invention can be a mixture of purified or crudely purified products of GSH, γ-GC, and CG, or a food material such as yeast extract containing all of them. In the present invention, there are no particular limitations as long as the composition contains GSH, γ-GC, and CG. Whether the composition contains GSH, γ-GC, and CG can be confirmed by reading the Examples section of this specification.

[0011] The composition of the present invention uses GSH, γ-GC, and CG in combination, and although the respective composition ratios (weight ratios) are arbitrary, the composition ratio (weight ratio) of GSH to γ-GC to CG is preferably 1:0.01 to 1:0.005 to 0.50, preferably 1:0.05 to 0.50:0.01 to 0.30, and more preferably 1:0.10 to 0.21:0.03 to 0.13. These composition ratios are measured by the methods described in the Examples section of this specification.

[0012] The contents of GSH, γ-GC, and CG in the composition of the present invention are arbitrary, but since the composition of the present invention is used by adding it to foods, etc., it is preferable that GSH is contained in an amount of 5% by weight or more. More preferably, it is a composition containing 15% by weight or more. The contents of γ-GC and CG may be contained in the weight ratios described above.

[0013] The composition of the present invention may contain other tyrosinase activity inhibitors, such as ascorbic acid, kojic acid, arbutin, and L-cysteine, as long as the effects of the present invention are not impaired.

[0014] In addition to the substances mentioned above, the composition of the present invention can contain additives and excipients used in various food ingredients, food additives, cosmetics, and pharmaceuticals. For example, various amino acids, peptides, proteins, nucleic acids, sugars, oils, and fats can be added without restriction as long as they do not inhibit the effects of the product. Oxidized glutathione may also be included.

[0015] The composition of the present invention can be added to various foods and beverages, functional foods, nutritional supplements, supplements, cosmetics, lotions, emulsions, creams, sunscreen cosmetics, hand creams, packs, body creams, and pharmaceuticals including quasi-drugs such as oral medications and topical skin preparations. Because the composition of the present invention can be used as a whitening composition or a skin-beautifying composition, foods and beverages, cosmetics, topical skin preparations, and pharmaceuticals containing the composition of the present invention can be suitably used as foods and beverages for improving skin, such as for skin beautification or whitening. The content of the composition of the present invention is not particularly limited, but it is preferably contained in a food or beverage product in an amount of about 0.0001 to 10% by mass. When the composition of the present invention is added to foods and beverages, cosmetics, pharmaceuticals, etc., there are no particular limitations on the form of these. Depending on the various forms of base materials, carriers, additives, etc. other than the composition of the present invention, base materials and the like that are commonly used can be used without limitation.

[0016] Functional ingredients other than the composition of the present invention can also be added. For example, in the case of foods and beverages, vitamins, minerals, and amino acids can be added, and in the case of cosmetics, various moisturizing ingredients, antibacterial ingredients, UV protection ingredients, whitening ingredients, etc. can be added. Furthermore, these active ingredients can be added alone or in combination.

[0017] <Method for measuring cysteine-containing peptides> The cysteine-containing peptides contained in the composition of the present invention were measured by HPLC. Standard aqueous solutions of known concentrations of GSH, γ-GC, and CG, as well as a sample aqueous solution, were analyzed under the following conditions, and the content of the cysteine-containing peptides in the composition was determined from the peak height ratio. Mobile phase: 40 mM ammonium phosphate buffer (pH 3.2) Column: ODS column (150 x 4.6 mm, pore size 5 μm) Temperature: 35℃ Flow rate: 1.0mL / min Detection wavelength: 210 nm [Example]

[0018] The present invention will be described in detail below with reference to examples. <Tyrosinase activity measurement> First, the following three types of solutions were prepared. Sample solution: The samples shown in the following Reference Examples 1 to 3, Examples 1 and 2, and Comparative Example 1 were dissolved in 0.1 M phosphate buffer (pH 6.7). Tyrosinase solution: Mushroom-derived tyrosinase (Sigma-Aldrich) was dissolved in 0.1 M phosphate buffer (pH 6.7) to a concentration of 200 U / mL. Dopa solution: L-DOPA (Sigma-Aldrich) was dissolved in 0.1 M phosphate buffer (pH 6.7) to a concentration of 0.8 mg / mL. First, 50 μL of tyrosinase solution was added to 10 μL of sample solution and pre-incubated at 37°C for 15 minutes. Next, 40 μL of DOPA solution was added, and after 30 minutes of incubation at 37°C, the absorbance at 490 nm was measured. The measured value without sample was designated C, the measured value without sample or L-DOPA was designated Cb, the measured value for each sample was designated S, and the measured value for each sample solution without L-DOPA was designated Sb. The tyrosinase activity inhibition rate was calculated using the following formula 1.

[0019] <Expression 1> Tyrosinase activity inhibition rate (%) = {(C-Cb)-(S-Sb)} / (C-Cb) × 100

[0020] <Comparative Example 1> A commercially available purified GSH product was used.

[0021] <Comparative Example 2> A purified γ-GC product was used.

[0022] <Comparative Example 3> CG refined products were used.

[0023] Example 1 The purified products of each cysteine-containing peptide were mixed at a composition ratio of GSH:γ-GC:CG=1:0.15:0.077 and used.

[0024] <Result> Table 1 shows the calculated values ​​obtained by adding together the measured values ​​of the tyrosinase activity inhibition rates in Comparative Examples 1 to 3 and Example 1 and the tyrosinase activity inhibition rates in Reference Examples 1 to 3. Although the concentrations of the cysteine-containing peptides contained in Example 1 were the same as those in Reference Examples 1 to 3, the measured values ​​of the tyrosinase activity inhibition rates in Examples 1 and 2 were higher than the calculated values. Comparative Example 1, which did not contain a cysteine-containing peptide, did not exhibit any tyrosinase activity inhibitory effect.

[0025] TIFF0007829071000001.tif40133 [Industrial Applicability]

[0026] The tyrosinase activity inhibitory composition of the present invention, when used in combination with the cysteine-containing peptides GSH, γ-GC, and CG, exhibits an excellent synergistic effect rather than simply an additive effect of the tyrosinase activity inhibitory effects of each peptide, thereby achieving excellent whitening and skin-beautifying effects. Furthermore, since GSH, γ-GC, and CG are naturally present in foods and in living organisms, they are also highly safe for living organisms.

Claims

1. A composition for inhibiting tyrosinase activity, comprising GSH, γ-GC, and Cys-Gly.

2. A tyrosinase activity inhibitory composition comprising GSH, γ-GC, and Cys-Gly, wherein the composition ratio (weight ratio) of GSH, γ-GC, and Cys-Gly is 1:0.01-0.1:0.005-0.

50.

3. A skin-improving food or drink containing the composition of claim 1 or 2.

4. A skin-improving cosmetic comprising the composition of claim 1 or 2.

5. A skin-improving drug comprising the composition of claim 1 or 2.

Citation Information

Patent Citations

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