Composition with anti-oxidation effect as well as application and cosmetics thereof

Through the composition of silybin and ektoin, the synergistic effect of the combination of silybin and ektoin achieves efficient antioxidant at a lower application amount, solving the problem of the need for high doses of existing antioxidants, reducing the risk of adverse reactions, and enhancing skin moisturizing and barrier functions.

CN119587396APending Publication Date: 2025-03-11SHANGHAI HUARUI WANMEI BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202411789821.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-05
Publication Date
2025-03-11

AI Technical Summary

Technical Problem

Only at higher doses of administration can existing antioxidants effectively reduce the damage to the skin by oxidative stress and may cause adverse reactions, such as skin irritation and allergies.

Method used

A composition including silybin and ektoin is provided, with a mass ratio of 1:0.1 to 1:4000. Through synergistic effects, the antioxidant can achieve efficient antioxidant at a lower application amount.

Benefits of technology

The composition significantly improves the antioxidant capacity at a lower application amount, avoids adverse reactions caused by high dose use, and enhances the barrier function and moisturizing effect of the skin.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention provides a composition with an anti-oxidation effect, application of the composition and cosmetics, the composition comprises silibinin and Ectoine, and the mass ratio of the silibinin to the Ectoine is (1: 0.1)-(1: 4000). The invention further provides an application of the silybin in promoting the anti-oxidation effect of the ectoine and an application of the ectoine in promoting the anti-oxidation effect of the silybin. The invention further provides application of the composition in preparation of cosmetics. The invention further provides an antioxidant cosmetic containing the composition. According to the application, the composition of silibinin and Ectoine is utilized to generate a relatively good synergistic effect in the aspect of oxidation resistance, so that the Ectoine realizes an efficient oxidation resistance effect at a relatively low application amount.
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Description

Technical Field

[0001] The present application relates to the technical field of cosmetics, and mainly to a composition with antioxidant effect, its application, and cosmetics. Background Art

[0002] The skin is the largest organ in the human body and is also the part most vulnerable to external environmental factors such as ultraviolet radiation and air pollution. These factors can cause the skin to produce a large amount of reactive oxygen species (ROS), which can trigger oxidative stress, damage skin cells, accelerate the skin aging process, and even cause a variety of skin diseases. Therefore, finding effective antioxidants to reduce or prevent this oxidative damage is an important research direction in the field of cosmetics.

[0003] Although existing antioxidants can alleviate the damage of oxidative stress to the skin to a certain extent, they often require a higher application amount to achieve significant antioxidant effects. This not only increases product costs, but may also cause adverse reactions such as skin irritation and allergies due to excessive use.

[0004] Ecdoin has an antioxidant effect. However, how to make Ecdoin achieve efficient antioxidant effect at a lower application amount has become a key technical problem in the research and development of this field. Summary of the invention

[0005] In order to solve the problem of how to make ectoine achieve efficient antioxidant effect at a lower application amount, the present application provides a composition with antioxidant effect, which includes silybin and ectoine, and the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

[0006] Skin is a tissue with high metabolic activity. Frequent exposure of the skin to the external environment, including UV and air pollution, can induce the production of harmful reactive oxygen species (ROS), which can cause oxidative damage to various biomacromolecules, including cell membranes, lipids, proteins, RNA and DNA, destroy important cells and increase DNA damage and mutations. When a large amount of oxidants exceeds the capacity of the antioxidant defense system, a situation called oxidative stress occurs. Reactive oxygen species (ROS) are continuously produced as secondary metabolites of many metabolic pathways and specific cell physiological and pathological processes. Oxidative stress is caused by an imbalance between oxidants and antioxidants. If reactive oxygen species (ROS) are produced excessively or there are insufficient antioxidants in the body or the capacity of the antioxidant cell defense system is reduced, important processes such as intracellular replication, transcription and translation will be damaged, leading to cell death, gene mutation, various pathological processes and increased aging. Oxidative stress is considered to be a contributing factor to the aging process and the pathogenesis of various skin diseases. Antioxidants can terminate the oxidation chain transmission by binding to free radicals and donating their electrons to them, thereby preventing free radicals from attacking intracellular biomacromolecules.

[0007] Silybin is a flavonolignan compound extracted from milk thistle seeds, and ectoine is an amino acid derivative. The silybin and ectoine composition provided in the present application can produce a good synergistic effect in terms of anti-oxidation, improve the antioxidant performance, and enable the antioxidant to achieve a high-efficiency antioxidant effect at a lower application amount.

[0008] Optionally, the mass ratio of silybin to ectoine is 1:100 to 1:4000.

[0009] Optionally, the mass ratio of silybin to ectoine is 1:4000.

[0010] The present application also provides use of the above composition in preparing cosmetics.

[0011] Optionally, the cosmetics include anti-oxidant cosmetics. The cosmetics are suitable for topical application to the skin, and include essences, gels, lotions, foundations and creams.

[0012] The present application also provides the use of silybin in promoting the antioxidant effect of ectoine, wherein the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

[0013] The present application also provides the use of ectoine in promoting the antioxidant effect of silybin, wherein the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

[0014] The present application also provides a cosmetic, comprising any of the above-mentioned compositions.

[0015] Optionally, based on the total mass of the cosmetic being 100%, the content of silybin in the cosmetic is 0.001% to 1.000%.

[0016] Optionally, the content of silybin in the cosmetic is 0.001% to 0.010%.

[0017] The present application provides a composition with antioxidant effect, its use, and cosmetics, the composition includes silybin and ectoine, and the mass ratio of silybin to ectoine is 1:0.1 to 1:4000. The present application also provides the use of silybin in promoting the antioxidant effect of ectoine, and the use of ectoine in promoting the antioxidant effect of silybin. The present application also provides the use of the composition in the preparation of cosmetics. The present application also provides an antioxidant cosmetic containing the above composition. The present application utilizes the composition of silybin and ectoine to produce a good synergistic effect in antioxidant effect, so that ectoine can achieve efficient antioxidant effect at a lower application amount. BRIEF DESCRIPTION OF THE DRAWINGS

[0018] In order to more clearly illustrate the technical solution of the present application, the drawings required for use in the embodiments are briefly introduced below. Obviously, for ordinary technicians in this field, other drawings can be obtained based on these drawings without any creative work.

[0019] Figure 1 Schematic diagram of antioxidant measurement results. DETAILED DESCRIPTION

[0020] The following embodiments are described in detail, and examples thereof are shown in the accompanying drawings. When the following description refers to the drawings, unless otherwise indicated, the same numbers in different drawings represent the same or similar elements. The implementations described in the following embodiments do not represent all implementations consistent with the present application. They are only examples of systems and methods consistent with some aspects of the present application as detailed in the claims.

[0021] In order to solve the problem of how to make antioxidants achieve efficient antioxidant effects at lower application amounts, the present application provides a composition with antioxidant effects, the composition comprising silybin and ectoine, the mass ratio of silybin to ectoine being 1:0.1 to 1:4000.

[0022] Skin is a tissue with high metabolic activity. Frequent exposure of the skin to the external environment, including UV and air pollution, can induce the production of harmful reactive oxygen species (ROS), which can cause oxidative damage to various biomacromolecules, including cell membranes, lipids, proteins, RNA and DNA, destroy important cells and increase DNA damage and mutations. When a large amount of oxidants exceeds the capacity of the antioxidant defense system, a situation called oxidative stress occurs. Reactive oxygen species (ROS) are continuously produced as secondary metabolites of many metabolic pathways and specific cell physiological and pathological processes. Oxidative stress is caused by an imbalance between oxidants and antioxidants. If reactive oxygen species (ROS) are produced excessively or there are insufficient antioxidants in the body or the capacity of the antioxidant cell defense system is reduced, important processes such as intracellular replication, transcription and translation will be damaged, leading to cell death, gene mutation, various pathological processes and increased aging. Oxidative stress is considered to be a contributing factor to the aging process and the pathogenesis of various skin diseases. Antioxidants can terminate the oxidation chain transmission by binding to free radicals and donating their electrons to them, thereby preventing free radicals from attacking intracellular biomacromolecules.

[0023] Silybin, also known as silymarin, is the main active ingredient extracted from the seeds of Milk Thistle and belongs to the flavonolignan class of compounds. Due to its strong biological activity and natural sources, silybin has broad application prospects in the fields of health products, medicines and cosmetics.

[0024] Ectoine, also known as tetrahydropyrimidine, is a naturally occurring amino acid derivative with a unique osmotic pressure regulating function. It can protect biological macromolecules such as proteins and enzymes in cells from damage under extreme conditions, thereby maintaining the normal physiological functions of cells. In addition, it also has excellent moisturizing and soothing effects, can enhance the barrier function of the skin, and improve problems such as dry and sensitive skin. Due to the multi-biological activities of ectoine and its natural origin, it has been widely used in cosmetics and personal care products, especially showing unique advantages in moisturizing, anti-allergy and anti-aging.

[0025] The silybin and ectoine composition provided in the present application can produce good synergistic effects in terms of anti-oxidation, improve the antioxidant performance, and enable ectoine to achieve efficient antioxidant effects at a lower application rate. In addition, ectoine can also provide other additional effects for the products to which it is applied.

[0026] In some embodiments, the mass ratio of silybin to ectoine is 1:50 to 1:4000.

[0027] In some embodiments, the mass ratio of silybin to ectoine is 1:100 to 1:4000.

[0028] In some embodiments, the mass ratio of silybin to ectoine is 1:800 to 1:4000.

[0029] In some embodiments, the mass ratio of silybin to ectoine is 1:4000.

[0030] The present application also provides use of the above composition in preparing cosmetics.

[0031] In some embodiments, the cosmetic comprises an antioxidant cosmetic. The cosmetic is suitable for topical application to the skin, and the cosmetic comprises serum, gel, lotion, foundation and cream.

[0032] The present application also provides the use of silybin in promoting the antioxidant effect of ectoine, wherein the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

[0033] The present application also provides the use of ectoine in promoting the antioxidant effect of silybin, wherein the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

[0034] The present application also provides a cosmetic, comprising any of the above-mentioned compositions.

[0035] In some embodiments, based on the total mass of the cosmetic being 100%, the content of silybin in the cosmetic is 0.001% to 1.000%.

[0036] In some embodiments, the present application does not impose any limitation on the method for determining antioxidant activity, and the activity may be determined by conventional methods in the art, such as chemical reaction spectrophotometry, fluorescence, and chemical titration. Currently, oxygen radical absorbance capacity (ORAC) is an internationally recognized and commonly used fluorescence attenuation method for determining the oxygen radical absorbance capacity of a sample.

[0037] ORAC is the abbreviation of Oxygen Radical Absorbance Capacity. The ORAC method is one of the most commonly used methods to detect the ability of antioxidants to resist ROS. The principle is that a free radical initiator such as an azo initiator compound 2,2-azobis(2,-methylpropylimidazole) dihydrochloride is mixed with a fluorescent probe (sodium fluorescein) to destroy the fluorescent probe, causing a change in fluorescence intensity. The fluorescence decay is quantified by using a fluorometer. The free radical initiator produces peroxy radicals. In the absence of an inhibitor, these free radicals will quickly destroy the fluorescence of the fluorescein dye. By tracking the time course of fluorescence decay and comparing the addition and non-addition of the test substance, the free radical capture ability of the test substance can be estimated.

[0038] The water-soluble analog of vitamin E, Trolox, was used as a quantitative standard and analyzed using a fluorescence analyzer to determine the degree of protection of the compound compared to the standard control antioxidant Trolox, and the results were expressed as μMol equivalents of Trolox. Equipment that can automatically measure and calculate capabilities is commercially available, such as the Fluoroskan FL microplate fluorescence and chemiluminescence analyzer from Thermo Scientific.

[0039] References for ORAC determination include: Cao G, Alessio H, Cutler R (1993). "Oxygen-radical absorbance capacity assay for antioxidants". Free Radic Biol Med 14(3): 303-11; Ou B, Hampsch-Woodill M, Prior R (2001). "Comparing antioxidant values ​​with the ORAC method". Alternat. Complement. Ther. 2004, 10, 167-160; Cronin, JR

[0040] In the composition provided in the present application, ectoine and silybin synergize to have excellent antioxidant efficacy. The ORAC value of the composition is significantly greater than the sum of the ORAC values ​​of ectoine and silybin alone, compared with the sum of the ORAC values ​​of ectoine and silybin alone.

[0041] Specific data calculation method:

[0042] Synergy is determined by comparing the actual measured ORAC value of the combination to the expected or additive values ​​of the individual compounds.

[0043] The predicted ORAC is the combined (cumulative) antioxidant capacity of the various antioxidant compounds in the combination, where each antioxidant compound is measured separately and assumed to work independently, the expected ORAC value of a combination can be calculated using the following equation, ORAC predicted value (total) = ORAC1 + ORAC2 + ... ORACn (n is the number of actives). When the actual measured ORAC value is significantly greater than the expected value, there is a synergistic antioxidant activity.

[0044] The composition provides a stronger protection against the damaging effects of free radicals and reactive oxygen species, and the combination in the composition of this embodiment shows synergistic antioxidant activity, wherein the activity of the composition of the present application is greater than the sum (cumulative value) of the individual antioxidant activities of each component.

[0045] Example:

[0046] The test was performed using an ORAC Assay kit (ab233473) purchased from Abcam. Silybin and ectoine sample solutions of different concentrations were prepared using PBS according to the composition in Table 1 to prepare sample compositions No. 1 to No. 65 and No. 1 to No. 23 comparative compositions.

[0047] In a 96-well plate, add 25 μL of the above sample or 25 μL of diluted Trolox standard to each well as a control. Then add 150 μL of fluorescein solution to each well, mix well, and incubate in a 37°C incubator for 30 minutes. Add 25 μL of free radical initiator solution, mix well, and immediately place in a microplate fluorescence and chemiluminescence analyzer to read the fluorescence intensity at an excitation wavelength of 485 nm and an emission wavelength of 538 nm. The measurement temperature is 37°C, the measurement time is 60 min, and the data is read every 1 min. (Concentration unit: mass %; ORAC unit: (μmol Trolox / g))

[0048] The antioxidant activity of each component alone and in combination was evaluated, and the results are shown in Table 2. Assuming that the antioxidant effect is simply additive and there is no synergistic effect, predictions were made for each composition and compared with the actual activity measurements of the composition of the present invention in Table 2. The results are shown in Table 2. Figure 1 As shown. The higher the ORAC value, the stronger the antioxidant capacity of the substance. The basis for judging synergy is that the ORAC value of the combined sample is significantly higher than the simple sum of the ORAC values ​​of the individual components (i.e. the predicted ORAC value). Increase percentage = (measured value - predicted value) ÷ predicted value × %.

[0049] Table 1 Sample composition table

[0050]

[0051]

[0052]

[0053] Table 2 Antioxidant properties measurement results

[0054]

[0055]

[0056]

[0057] The results of the antioxidative properties of the samples in the examples are shown in Table 2. Figure 1 The experimental results show that the measured ORAC values ​​of all compositions containing silybin and ectoine are significantly higher than their predicted values, indicating that silybin and ectoine have significant synergistic effects in antioxidation.

[0058] In particular, when the mass ratio of silybin and ectoine is 1:50 to 1:4000, the measured value is more than 4 times the predicted value; when the mass ratio of silybin and ectoine is 1:100 to 1:4000, the measured value is more than 5 times the predicted value; when the mass ratio of silybin and ectoine is 1:800 to 1:4000, the measured value is more than 11 times the predicted value; in the composition with a mass ratio of silybin and ectoine of 1:4000 (such as the 9th composition), although the content of silybin is very low (0.001%), the antioxidant capacity of the composition is significantly enhanced, and the measured ORAC value reaches 63.72 μmol Trolox / g, which is nearly 20 times higher than the predicted value, verifying that silybin and ectoine in the composition provided in the present application have synergistic effects in antioxidant properties.

[0059] In particular, based on the total mass of the composition as 100%, when the content of silybin in the composition is 0.001% to 0.010%, the antioxidant capacity of the composition is outstanding, which verifies that the composition of the present application achieves a high-efficiency antioxidant effect at a lower application amount.

[0060] The present application provides a composition with antioxidant effect, its use, and cosmetics, the composition includes silybin and ectoine, and the mass ratio of silybin to ectoine is 1:0.1 to 1:4000. The present application also provides the use of silybin in promoting the antioxidant effect of ectoine, and the use of ectoine in promoting the antioxidant effect of silybin. The present application also provides the use of the composition in the preparation of cosmetics. The present application also provides an antioxidant cosmetic containing the above composition. The present application utilizes the composition of silybin and ectoine to produce a good synergistic effect in antioxidant effect, so that ectoine can achieve efficient antioxidant effect at a lower application amount.

[0061] Similar parts between the embodiments provided in this application can be referenced to each other. The specific implementation methods provided above are only a few examples under the general concept of this application and do not constitute a limitation on the protection scope of this application. For those skilled in the art, any other implementation methods expanded based on the scheme of this application without creative work belong to the protection scope of this application.

Claims

1. A composition having an antioxidant effect, characterized in that: The composition comprises silybin and ectoine, and the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

2. The composition according to claim 1, characterized in that The mass ratio of silybin to ectoine is 1:100 to 1:4000.

3. The composition according to claim 2, characterized in that The mass ratio of silybin to ectoine is 1:4000.

4. Use of the composition according to any one of claims 1 to 3 in the preparation of cosmetics.

5. The use according to claim 4, characterized in that The cosmetics include antioxidant cosmetics.

6. Use of silybin in promoting the antioxidant effect of ectoine, wherein the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

7. Use of ectoine in promoting the antioxidant effect of silybin, wherein the mass ratio of silybin to ectoine is 1:0.1 to 1:4000.

8. A cosmetic, characterized in that: The cosmetic comprises the composition according to any one of claims 1 to 3.

9. The cosmetic according to claim 8, characterized in that: Taking the total mass of the cosmetic as 100%, the content of silybin in the cosmetic is 0.001% to 1.000%.

10. The cosmetic according to claim 9, characterized in that: The content of silybin in the cosmetic is 0.001% to 0.010%.