Composition for inhibiting tyrosinase activity
By combining glutathione, gamma-glutamylcysteine, and cysteylglycine, the problem of the insignificant effect of existing tyrosinase activity inhibitors is solved, achieving superior whitening and skin-beautifying effects while maintaining high safety.
Patent Information
- Application Number
- CN202480009662.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-01-31
- Filing Date
- 2024-01-30
- Publication Date
- 2025-08-26
AI Technical Summary
Existing tyrosinase activity inhibitors are not effective enough for whitening and skin beautification purposes, and better compositions are needed.
A combination of glutathione (GSH), γ-glutamylcysteine (γ-GC), and cysteylglycine (CG) in a ratio of 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, is used to prepare a tyrosinase activity inhibitory composition.
It achieves excellent inhibition of tyrosinase activity, exhibits synergistic effects, enhances whitening and skin-beautifying effects, and has high ingredient safety.
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Abstract
Description
Technical Field
[0001] The present invention relates to a tyrosinase activity inhibitory composition suitable for whitening and skin beautification. Background Art
[0002] The mechanism of skin pigmentation, spots, and freckles is unclear, but one possible cause is excessive melanin production and deposition in the skin due to hormonal abnormalities, excessive or chronic ultraviolet light stimulation. Tyrosinase is an enzyme that catalyzes the oxidation of tyrosine and dopa, which are sources of melanin. Activation of tyrosinase leads to increased melanin production.
[0003] Therefore, tyrosinase activity inhibitors are used in foods, beverages, and cosmetics for whitening and skin beautification, and known examples include ascorbic acid, kojic acid, arbutin, and L-cysteine. However, these inhibitors alone may not be sufficiently effective, and in order to more effectively inhibit tyrosinase activity, multiple compounds are often used in combination.
[0004] Glutathione is also known to inhibit tyrosinase activity and has been reported to be used for whitening and skin beautification. α - Combined use of lipoic acid (Patent Document 1), guava (Patent Document 2), L-cystine (Patent Document 3), etc. However, a composition having a more excellent tyrosinase activity inhibitory effect is desired.
[0005] Prior art literature Patent Literature Patent Document 1: Japanese Patent Application Laid-Open No. 2009-51768 Patent Document 2: Japanese Patent Application Laid-Open No. 2008-303180 Patent Document 3: Japanese Patent Application Laid-Open No. 2016-88875 Summary of the Invention Technical problem to be solved by the invention An object of the present invention is to provide a skin-whitening and skin-beautifying composition having an excellent tyrosinase activity inhibitory effect.
[0006] Technical solutions to technical problems The present inventors have conducted intensive research to solve the above problems and have found that by using glutathione (GSH) as a cysteine-containing peptide and c -Gly-Cys ( c -GC), Cys-Gly (CG), can achieve excellent tyrosinase activity inhibition effect.
[0007] That is, the present invention relates to the following contents: (1) A tyrosinase activity inhibitory composition comprising GSH, c -GC and CG; (2) The tyrosinase activity inhibitory composition according to (1) above, wherein GSH, c - The composition ratio (weight ratio) of GC and CG is 1:0.01 to 1:0.005 ~ 0.50, preferably 1:0.05 ~ 0.50:0.01 ~ 0.30, more preferably 1:0.10 ~ 0.21:0.03 ~ 0.13; (3) A skin-improving food or drink comprising the composition of (1) or (2) above; (4) A skin-improving cosmetic comprising the composition of (1) or (2) above; (5) A skin-improving pharmaceutical comprising the composition of (1) or (2) above.
[0008] Effects of the Invention In the present invention, glutathione (GSH), a cysteine-containing peptide, c -Glutamylcysteine ( c -Gly-Cys: c -GC), cysteinylglycine (Cys-Gly: CG), showing excellent synergistic effect, rather than the additive effect of adding the tyrosinase activity inhibitory effects of each, thus achieving excellent whitening and skin beautification effects. c -GC and CG are components that originally exist in food and living organisms, so they are highly safe for living organisms. DETAILED DESCRIPTION
[0009] Hereinafter, the present invention will be described in detail.
[0010] The composition of the present invention can utilize GSH, c - A mixture of purified products or crude purified products of GC and CG, or a mixture containing GSH, c -GC, CG all yeast extracts and other food raw materials. In the present invention, as long as it contains GSH, c -GC, CG are not particularly limited. Whether it contains GSH, c - Combination of GC and CG.
[0011] The composition of the present invention is used in combination with GSH, c -GC, CG, the composition ratio (weight ratio) of each is arbitrary, GSH, c -The composition ratio (weight ratio) of GC and CG is 1:0.01 ~1:0.005 ~ 0.50, preferably 1:0.05 ~ 0.50:0.01 ~ 0.30, more preferably 1:0.10 ~ 0.21:0.3 ~ These composition ratios were measured by the method described in Examples of this specification.
[0012] GSH in the composition of the present invention, c The content of -GC and CG is optional, but from the viewpoint of adding the composition of the present invention to food and the like, it is preferable that the composition contains 5% by weight or more of GSH, and more preferably 15% by weight or more. c -GC and CG may be contained in the above-mentioned weight ratio.
[0013] The composition of the present invention may contain other tyrosinase activity inhibitors such as ascorbic acid, kojic acid, arbutin, and L-cysteine, within a range that does not inhibit the effects of the present invention.
[0014] In addition to the aforementioned substances, the compositions of the present invention may also contain various food raw materials, food additives, cosmetics, and additives and excipients used in pharmaceuticals. For example, various amino acids, peptides, proteins, nucleic acids, sugars, and oils may be incorporated without limitation, as long as they do not hinder 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 labeled foods, nutritional supplements, dietary supplements, cosmetics, lotions, emulsions, creams, sunscreen cosmetics, hand creams, facial masks, body creams, and pharmaceuticals including oral medications, quasi-drugs such as external skin preparations, etc. The composition of the present invention can be used as a whitening composition or a skin beautifying composition, so foods and beverages, cosmetics, external skin preparations, and pharmaceuticals to which the composition of the present invention is added can be suitably used as skin beautifying or whitening foods and beverages. The content of the composition of the present invention is not particularly limited, but preferably contains 0.0001 in foods and beverages. ~ About 10% by mass.
[0016] When the composition of the present invention is added to foods, beverages, cosmetics, pharmaceuticals, etc., there is no particular limitation on their form. For various forms of other substrates, carriers, additives, etc. other than the composition of the present invention, commonly used substrates can be used without limitation.
[0017] Functional ingredients other than the composition of the present invention can also be added. For example, if it is a food or beverage, various vitamins, minerals, and amino acids can be added. If it is a cosmetic, various moisturizing ingredients, antibacterial ingredients, ultraviolet protection ingredients, whitening ingredients, etc. can be added. In addition, these active ingredients can be a single one or a combination of multiple ones.
[0018] <Measurement Method for Cysteine-Containing Peptides> The cysteine-containing peptides contained in the composition of the present invention were determined using the HPLC method. GSH, c -GC and CG are prepared by mixing a standard aqueous solution and a sample aqueous solution with known concentrations, and the content of the cysteine-containing peptide in the composition is determined based on the ratio of the peak heights.
[0019] Mobile phase: 40 mM ammonium phosphate buffer (pH 3.2) Column: ODS column (150×4.6mm, pore size 5 m m) Temperature: 35℃ Flow rate: 1.0 mL / min Detection wavelength: 210nm Example Hereinafter, the present invention will be described in detail with reference to Examples.
[0020] <Tyrosinase Activity Assay> First, the three solutions shown below were prepared.
[0021] Sample solution: the following reference example 1 ~ 3. The samples described in Examples 1, 2, and Comparative Example 1 were dissolved in 0.1 M phosphate buffer (pH 6.7).
[0022] 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.
[0023] 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.
[0024] The determination was first performed in a sample solution 10 m Add tyrosinase solution 50 m L, pre-incubated at 37 ° C for 15 minutes. Then, add 40 mL, and after incubation at 37°C for 30 minutes, the absorbance at 490 nm was measured. The tyrosinase activity inhibition rate was calculated according to the following formula 1, with the measured value excluding the sample being designated as C, the measured value excluding the sample and L-DOPA being designated as Cb, the measured value of each sample being designated as S, and the measured value excluding L-DOPA in each sample solution being designated as Sb.
[0025] <Formula 1> Tyrosinase activity inhibition rate (%) = {(C-Cb)-(S-Sb)} / (C-Cb)×100 <Comparative Example 1> A commercially available purified GSH was used.
[0026] Comparative Example 2 use c -GC purified product.
[0027] Comparative Example 3 Use a purified product of CG.
[0028] <Example 1> The purified products of the cysteine-containing peptides were mixed with GSH in the following composition ratio: c -GC:CG=1:0.15:0.077 were mixed and used.
[0029] <Results> Table 1 is a table showing the comparison of ~ 3 and the measured values of the tyrosinase activity inhibition rate of Example 1, and Reference Example 1 ~ The concentration of each cysteine-containing peptide contained in Example 1 was the same as that in Reference Example 1. ~ 3, the measured values of the tyrosinase activity inhibition rates of Examples 1 and 2 were higher than the calculated values. Comparative Example 1, which did not contain a cysteine-containing peptide, did not show any tyrosinase activity inhibitory effect.
[0030] Industrial Applicability The tyrosinase activity inhibitory composition of the present invention is prepared by combining GSH, c -GC, CG, show excellent synergistic effect, rather than simply adding the additive effect of their respective tyrosinase activity inhibitory effects, so excellent whitening and skin beautification effects can be obtained. c -GC and CG are components that originally exist in food and living organisms, so they are highly safe for living organisms.
Claims
1. A tyrosinase activity inhibitory composition, characterized in that: Contains GSH, γ -GC and Cys-Gly.
2. A tyrosinase activity inhibitory composition, characterized in that: Contains GSH, γ -GC and Cys-Gly, among which GSH, γ The composition ratio of -GC and Cys-Gly is 1:0.01 by weight. ~ 0.1:0.005 ~ 0.
50.
3. A skin-improving food or beverage, characterized in that: A composition comprising the composition of claim 1 or 2.
4. A skin-improving cosmetic, characterized in that: A composition comprising the composition of claim 1 or 2.
5. A skin-improving pharmaceutical product, characterized in that: A composition comprising the composition of claim 1 or 2.
Citation Information
Patent Citations
Skin-lightening agent, skincare preparation for external use, and functional oral composition
JP2008303180A
Thyrosinase activity inhibitory composition
JP2009051768A
Whitening and antioxidation composition
JP2016088875A