A whitening composition with short peptide synergistically enhanced with arbutin and its application

Abstract

The present invention discloses a whitening composition with synergistic effect of short peptide and arbutin and its application. The whitening composition with synergistic effect of short peptide and arbutin comprises arbutin and a short peptide; the short peptide is selected from one or more of AHW, LRY, LWF, CFV and IWC. The whitening composition with synergistic effect of short peptide and arbutin of the present invention produces a synergistic effect by combining a specific short peptide with arbutin, synergistically increasing the inhibitory effect on tyrosinase, so that arbutin can achieve a better tyrosinase inhibition effect at a lower, safer and more stable concentration, and can greatly reduce the use concentration of arbutin, reduce cytotoxicity and improve stability. The whitening composition of the invention has the advantages of low concentration, high efficiency, low toxicity and good stability, and has good application prospects.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, in particular to a whitening composition in which a short peptide synergizes with arbutin and its application, and in particular to an arbutin whitening composition capable of taking into account both safety and tyrosinase inhibition effect and its application. Background Art

[0002] Human skin is repeatedly exposed to the environment and therefore requires numerous endogenous protective systems. Melanin, a naturally occurring pigment found throughout the body, primarily functions to reduce skin damage caused by ultraviolet (UV) radiation. However, overproduction and accumulation of melanin can lead to the development of physiological abnormalities such as pigmentation spots, melasma, freckles, and age spots.

[0003] As research into melanin biosynthesis continues to deepen, it has been discovered that tyrosinase is a key, rate-limiting enzyme in melanin production, and overexpression of tyrosinase is the primary cause of hyperpigmentation. Furthermore, tyrosinase is produced exclusively by melanocytes and can specifically inhibit melanin production in these cells, achieving a whitening effect. Therefore, tyrosinase has become the most prominent and successful target for melanin production inhibitors.

[0004] Although a large number of tyrosinase inhibitors have been discovered so far, such as kojic acid, arbutin, hydroquinone, VC and its derivatives, relatively few tyrosinase inhibitors have been used due to safety and stability issues and weak whitening effects. Among them, arbutin has a better whitening effect and relatively low cytotoxicity, so it is currently the most widely used whitening agent.

[0005] Research has found that the dosage of arbutin is closely related to its stability, safety, and activity. When used as a cosmetic additive, low doses of arbutin have a weak inhibitory effect on the catalytic activity of tyrosinase in the skin, resulting in a subtle whitening effect. High doses significantly inhibit tyrosinase activity, but this significantly reduces stability, leading to easy decomposition and cytotoxicity to body cells.

[0006] Therefore, it is of great practical significance to develop an arbutin composition that takes into account both safety and tyrosinase inhibitory effect. Summary of the Invention

[0007] Due to the above-mentioned defects in the prior art, the present invention provides an arbutin composition that takes into account both safety and tyrosinase inhibitory effect. Specifically, it provides a whitening composition that is synergistically enhanced by a novel short peptide and arbutin. The composition can achieve a better tyrosinase inhibitory effect using a lower concentration of arbutin. While maintaining the tyrosinase inhibitory activity, the concentration of arbutin can be greatly reduced, the cytotoxicity can be reduced, and the stability can be improved, thereby overcoming the current defects of poor tyrosinase inhibitory effect of low-concentration arbutin and poor safety and stability of high-concentration arbutin.

[0008] In order to achieve the above object, the present invention provides the following technical solutions:

[0009] A whitening composition with synergistic effect of short peptide and arbutin, comprising arbutin and short peptide;

[0010] The short peptide is selected from one or more of AHW, LRY, LWF, CFV and IWC.

[0011] Bioactive peptides are composed of 2 to 50 amino acids and are a special type of protein fragment that can have a positive impact on the function and state of the human body. Compared with traditional chemical drugs, polypeptide drugs have the characteristics of simple structure, small molecular weight, strong specificity, easy absorption, and high safety. The present invention selects specific short peptides (one or more of AHW, LRY, LWF, CFV and IWC) to synergize with arbutin, so that arbutin can achieve better tyrosinase inhibition effect (i.e., good whitening effect) at a lower, safer and more stable concentration. It can greatly reduce the use concentration of arbutin, while reducing cytotoxicity and improving stability, and has good application prospects.

[0012] As the preferred technical solution:

[0013] As described above, a whitening composition with a short peptide synergistically enhanced with arbutin, the peptide sequence of AHW is Ala-His-Trp; the peptide sequence of LRY is Leu-Arg-Tyr; the peptide sequence of LWF is Leu-Trp-Phe; the peptide sequence of CFV is Cys-Phe-Val; and the peptide sequence of IWC is Ile-Trp-Cys.

[0014] A whitening composition as described above in which the short peptide synergizes with arbutin for enhanced synergy, the whitening composition further comprising water;

[0015] The total concentration of solutes in the whitening composition is 0.021 to 0.055 wt %.

[0016] A whitening composition in which the short peptide synergizes with arbutin, wherein the concentration of arbutin in the whitening composition is 0.02-0.05 wt%;

[0017] The concentration of the short peptide in the whitening composition is 0.001 to 0.005 wt %.

[0018] In addition, the present invention also provides the use of the above-mentioned short peptide synergistically enhanced whitening composition with arbutin in the preparation of a tyrosinase inhibitor.

[0019] The above technical solution is only a feasible technical solution of the present invention. The protection scope of the present invention is not limited thereto. Those skilled in the art can reasonably adjust the specific design according to actual needs.

[0020] The above invention has the following advantages or beneficial effects:

[0021] (1) The whitening composition of the present invention, which is synergistically enhanced by short peptides and arbutin, is selected to synergize with arbutin by selecting specific short peptides (one or more of AHW, LRY, LWF, CFV and IWC) so that arbutin can achieve a better tyrosinase inhibition effect (i.e., a good whitening effect) at a lower, safer and more stable concentration. The concentration of arbutin can be greatly reduced, while reducing cytotoxicity and improving stability.

[0022] (2) The whitening composition of the present invention, which is enhanced by the synergistic effect of the short peptide and arbutin, can be used to prepare a tyrosinase inhibitor, which has low cytotoxicity, good stability, good tyrosinase inhibition effect and good application prospects. BRIEF DESCRIPTION OF THE DRAWINGS

[0023] The present invention and its features, configurations, and advantages will become more apparent upon reading the detailed description of non-limiting embodiments with reference to the following drawings. Like reference numerals indicate like parts throughout the drawings. The drawings are not necessarily drawn to scale, emphasis being placed on illustrating the subject matter of the present invention.

[0024] Figure 1 Schematic diagram of the effect of different concentrations of arbutin on tyrosinase activity in Comparative Example 1;

[0025] Figure 2 Schematic diagram of the effect of different concentrations of arbutin on cell activity in Comparative Example 1;

[0026] Figure 3 Schematic diagram of the effect of different concentrations of short peptides on tyrosinase activity in Comparative Example 2;

[0027] Figure 4 Schematic diagram of the effect of different concentrations of short peptides on cell activity in Comparative Example 2;

[0028] Figure 5 Schematic diagram of the effects of the products prepared in experimental group 1, experimental group 12, experimental group 17, and comparative examples 3 to 5 on tyrosinase activity;

[0029] Figure 6 Schematic diagram of the effects of the products prepared in experimental group 1, experimental group 12, experimental group 17, and comparative examples 3 to 5 on cell activity. DETAILED DESCRIPTION

[0030] The structure of the present invention is further described below with reference to the accompanying drawings and specific embodiments, but is not intended to limit the present invention.

[0031] In the following examples, the peptide sequence of AHW is Ala-His-Trp; the peptide sequence of LRY is Leu-Arg-Tyr; the peptide sequence of LWF is Leu-Trp-Phe; the peptide sequence of CFV is Cys-Phe-Val; and the peptide sequence of IWC is Ile-Trp-Cys.

[0032] Example 1

[0033] It specifically provides a whitening composition that enhances the effect of a short peptide and arbutin:

[0034] Experimental group 1: a whitening composition with a short peptide synergistically enhanced with arbutin, comprising 0.02 wt % arbutin, 0.005 wt % AHW short peptide and the balance water.

[0035] The formulas of experimental groups 2 to 5 are basically the same as those of experimental group 1, except that the AHW short peptide in experimental group 1 is replaced by LRY short peptide, LWF short peptide, CFV short peptide and IWC short peptide, respectively.

[0036] Example 2

[0037] It specifically provides a whitening composition that enhances the effect of a short peptide and arbutin:

[0038] Experimental group 6: A whitening composition with a short peptide synergistically enhanced with arbutin, comprising 0.05 wt % arbutin, 0.001 wt % AHW short peptide and the balance water.

[0039] The formulas of experimental groups 7 to 10 are basically the same as those of experimental group 1, except that the AHW short peptide in experimental group 1 is replaced by LRY short peptide, LWF short peptide, CFV short peptide and IWC short peptide, respectively.

[0040] Example 3

[0041] The invention specifically provides a whitening composition with synergistic effect of short peptides and arbutin, comprising 0.03wt% arbutin, 0.001wt% AHW short peptide, 0.001wt% LRY short peptide, 0.0005wt% LWF short peptide, 0.001wt% CFV short peptide, 0.0005wt% IWC short peptide and the balance water.

[0042] Comparative Example 1

[0043] Experimental groups 11 to 15 were arbutin solutions with concentrations of 0.01 wt%, 0.02 wt%, 0.05 wt%, 0.2 wt% and 0.5 wt%, respectively.

[0044] Comparative Example 2

[0045] Experimental groups 16 to 20 were 0.001 wt%, 0.005 wt%, 0.02 wt%, 0.05 wt%, and 0.2 wt% AHW short peptide solutions, respectively;

[0046] Experimental groups 21 to 25 were 0.001 wt%, 0.005 wt%, 0.02 wt%, 0.05 wt%, and 0.2 wt% LRY short peptide solutions, respectively;

[0047] Experimental groups 26 to 30 were 0.001 wt%, 0.005 wt%, 0.02 wt%, 0.05 wt%, and 0.2 wt% LWF short peptide solutions, respectively;

[0048] Experimental groups 31 to 35 were 0.001 wt%, 0.005 wt%, 0.02 wt%, 0.05 wt%, and 0.2 wt% CFV short peptide solutions, respectively;

[0049] Experimental groups 36 to 40 were 0.001 wt%, 0.005 wt%, 0.02 wt%, 0.05 wt%, and 0.2 wt% IWC short peptide solutions, respectively.

[0050] Comparative Example 3

[0051] A whitening composition, wherein the components and component contents thereof are substantially the same as those of experimental group 1 in Example 1, except that the AHW short peptide is replaced by APK.

[0052] Comparative Example 4

[0053] A whitening composition, wherein the components and component contents thereof are substantially the same as those of Experimental Group 1 in Example 1, except that the AHW short peptide is replaced by ILW.

[0054] Comparative Example 5

[0055] A whitening composition, wherein the components and component contents thereof are substantially the same as those of experimental group 1 in Example 1, except that the AHW short peptide is replaced by THN.

[0056] The products of Examples 1 to 3 and Comparative Examples 1 to 5 were tested for tyrosinase inhibitory activity, cytotoxicity and stability. The results are shown in Tables 1 to 2 and Figures 1 to 6 .

[0057] The detection method is as follows:

[0058] 1. Determination of Tyrosinase Inhibition Rate: Take B16F10 cells in good growth condition and plate them in a 96-well plate. After culturing for 24 hours, add 10% of the test sample to the 96-well plate and incubate for 24 hours. Discard the culture medium and wash with PBS. Add 90% of the test sample to each well. Incubate in a 37°C incubator for 60 minutes. After that, measure the OD at 475nm using a microplate reader and calculate the tyrosinase inhibition rate. PBS was used instead of sample in the blank control group. 0.2% arbutin solution was used as a positive control.

[0059] 2. Cytotoxicity Assay: B16F10 cells in good growth condition were plated in 96-well plates and cultured for 24 hours before adding the sample. OD450nm was measured using CCK-8 assay after 48 hours to determine the effect of the sample on B16F10 cell viability. A 0.2wt% arbutin solution was used as a control.

[0060] 3. Stability Test: The whitening compositions prepared in Examples 1-3 were added with an appropriate amount of preservative and stored at 50°C for 4 weeks. The arbutin content in each sample was determined by high-performance liquid chromatography (HPLC). The remaining arbutin content after 4 weeks was calculated to evaluate the thermal stability of the compositions. The whitening compositions prepared in Examples 1-3 were also added with an appropriate amount of preservative and stored under light for 4 weeks. The photostability of the samples was then tested and their properties were observed to evaluate the photostability of the whitening compositions. A 0.2 wt% arbutin solution was used as a control.

[0061] Table 1 Effects of the compositions prepared in Examples 1 to 3 and the control group on tyrosinase activity and cell activity

[0062]

[0063]

[0064] Table 2 Stability test of the compositions prepared in Examples 1 to 3 and the control group

[0065]

[0066] from Figures 5-6 It can be seen that under the same arbutin concentration, the tyrosinase inhibition rate of the composition of Example 1 is much higher than that of the compositions of Experimental Groups 12 and 17 and Comparative Examples 3, 4, and 5. It can be seen that only the combination of specific tripeptides (one or more of AHW, LRY, LWF, CFV, and IWC) and arbutin can achieve excellent tyrosinase inhibition effect. At the same time, the addition of specific tripeptides greatly reduces the arbutin concentration required to achieve the same tyrosinase inhibition effect, which greatly improves the safety of the composition, thereby achieving a good balance between the safety of the composition and the tyrosinase inhibition effect.

[0067] Those skilled in the art should understand that they can implement variations by combining the prior art with the above embodiments, which will not be described in detail here. Such variations do not affect the essence of the present invention and will not be described in detail here.

[0068] The above describes the preferred embodiments of the present invention. It should be understood that the present invention is not limited to the above-mentioned specific embodiments, and the devices and structures that are not described in detail should be understood to be implemented in a common manner in the art; any technician familiar with the art can use the above-mentioned disclosed methods and technical contents to make many possible changes and modifications to the technical solutions of the present invention without departing from the scope of the technical solutions of the present invention, or modify them into equivalent embodiments of equivalent changes, which does not affect the essential content of the present invention. Therefore, any simple modifications, equivalent changes and modifications made to the above embodiments based on the technical essence of the present invention that do not depart from the content of the technical solutions of the present invention are still within the scope of protection of the technical solutions of the present invention.

Claims

1. A whitening composition with a short peptide and arbutin as synergistic enhancer, characterized by: Including arbutin and short peptides; The short peptide is selected from one or more of AHW, LRY, LWF, CFV and IWC.

2. The whitening composition according to claim 1, wherein the short peptide and arbutin enhance the skin's appearance. The whitening composition also includes water; The total concentration of solutes in the whitening composition is 0.021-0.055 wt %.

3. The whitening composition according to claim 2, wherein the short peptide and arbutin enhance the skin's appearance, The concentration of arbutin in the whitening composition is 0.02-0.05 wt %; The concentration of the short peptide in the whitening composition is 0.001-0.005 wt %.

4. Use of a whitening composition comprising a short peptide and arbutin as claimed in any one of claims 1 to 3 in the preparation of whitening cosmetics.

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