Composition with antioxidant effect and its uses

Abstract

The present application provides a composition having an antioxidant effect, comprising baicalin and astaxanthin, wherein the mass ratio of the baicalin to the astaxanthin is 1:(0.005-3). The present application combines astaxanthin with baicalin to enhance the antioxidant effect of baicalin, i.e., astaxanthin and baicalin synergize to achieve excellent antioxidant effect.

Description

Technical Field

[0001] The present application relates to a composition, in particular to a composition with synergistic antioxidant effect and its use. Background Art

[0002] Skin is a highly metabolically active tissue. Frequent exposure to the environment, including ultraviolet (UV) radiation and air pollution, can induce the production of harmful reactive oxygen species (ROS). These substances can cause oxidative damage to various biomolecules, including cell membranes, lipids, proteins, RNA, and DNA, damaging vital cells and increasing DNA damage and mutations. Oxidative stress occurs when large amounts of oxidants exceed the capacity of the antioxidant defense system. ROS are continuously produced as secondary metabolites in many metabolic pathways and during specific cellular physiological and pathological processes. Oxidative stress is caused by an imbalance between oxidants and antioxidants. Excessive ROS production, insufficient antioxidants, or decreased antioxidant cellular defense capacity can impair vital processes within cells, such as replication, transcription, and translation. This can lead to cell death, genetic mutations, various pathological processes, and increased aging. Oxidative stress is considered a contributing factor to the aging process and the pathogenesis of various skin diseases. Antioxidants terminate the oxidative chain by binding to free radicals and donating their electrons, preventing them from attacking intracellular biomolecules.

[0003] While there are some examples of antioxidants that can provide protective benefits, there remains a need for compositions that provide enhanced options for protective formulations, particularly in the cosmetic field, to more efficiently exert antioxidant efficacy. Summary of the Invention

[0004] In response to the problems existing in the prior art, the present application provides a composition and its use that can significantly improve the antioxidant effect.

[0005] The specific plan is as follows:

[0006] 1. A composition with antioxidant effect, comprising baicalin and astaxanthin, wherein the mass ratio of the baicalin to the astaxanthin is 1:(0.005-3).

[0007] 2. The composition according to item 1, wherein

[0008] The mass ratio of the baicalin to the astaxanthin is 1:(0.01-1), preferably 1:(0.02-0.3).

[0009] 3. The composition according to item 1 or 2, wherein

[0010] Calculated as a percentage by mass of the total mass of the composition, the baicalin is 0.3 wt% to 10 wt%, preferably 0.5 wt% to 10 wt%.

[0011] 4. Use of the composition according to any one of items 1 to 3 in cosmetics.

[0012] 5. An anti-oxidation method, comprising administering the composition according to any one of items 1 to 3 to a site in need of treatment in a subject.

[0013] 6. Use of the composition according to any one of items 1 to 3 in the preparation of an antioxidant product.

[0014] 7. Use of baicalin and astaxanthin in the preparation of antioxidant products.

[0015] 8. Use of the composition according to any one of items 1 to 3 as a cosmetic preparation or a personal care preparation for antioxidant purposes.

[0016] 9. Use of a combination of baicalin and astaxanthin as a cosmetic preparation or a personal care preparation for antioxidant effect.

[0017] 10. The use according to item 7 or 9, wherein

[0018] The mass ratio of the baicalin to the astaxanthin is 1:(0.005-3), preferably 1:(0.01-1), and more preferably 1:(0.02-0.3).

[0019] Technical Effects

[0020] The baicalin has a strong antioxidant effect. The present application combines astaxanthin with baicalin to enhance the antioxidant effect of baicalin, that is, astaxanthin and baicalin synergistically enhance the effect and have excellent antioxidant effect. DETAILED DESCRIPTION

[0021] The present application is further described below with reference to examples. It should be understood that the examples are only used to further illustrate and explain the present application and are not intended to limit the present application.

[0022] Unless otherwise defined, technical and scientific terms used in this specification have the same meanings as those commonly understood by those skilled in the art. Although methods and materials similar or identical to those described herein may be used in experiments or actual applications, the materials and methods are described herein below. In the event of a conflict, the present specification, including definitions, will prevail. Furthermore, the materials, methods, and examples are provided for illustrative purposes only and are not intended to be limiting. The following description further illustrates the present application with reference to specific examples, which are not intended to limit the scope of this application.

[0023] The present application provides a composition with antioxidant effect, which comprises baicalin and astaxanthin, wherein the mass ratio of the baicalin to the astaxanthin is 1:(0.005-3).

[0024] In the present application, a composition having an antioxidant effect refers to a substance that can effectively inhibit the oxidation reaction of free radicals at a low concentration. The composition described in the present application has excellent antioxidant efficacy by combining baicalin and astaxanthin.

[0025] In some embodiments, the mass ratio of the baicalin to the astaxanthin is 1:(0.01-1), preferably 1:(0.02-0.3);

[0026] For example, the mass ratio of the baicalin to the astaxanthin can be 1:0.005, 1:0.01, 1:0.02, 1:0.03, 1:0.04, 1:0.05, 1:0.06, 1:0.07, 1:0.08, 1:0.09, 1:0.1, 1:0.15, 1:0.2, 1:0.25, 1:0.3, 1:0.35, 1:0.4, 1:0.45, 1:0.5, 1:0.55, 1:0.6, 1:0.65 , 1:0.7, 1:0.75, 1:0.8, 1:0.85, 1:0.9, 1:0.95, 1:1, 1:1.1, 1:1.2, 1:1.3, 1:1.4, 1:1.5, 1:1.6, 1:1.7, 1:1.8, 1:1.9, 1:2, 1:2.1, 1:2.2, 1:2.3, 1:2.4, 1:2.5, 1:2.6, 1:2.7, 1:2.8, 1:2.9, 1:3 or any range therebetween.

[0027] Baicalin refers to a flavonoid compound extracted and isolated from the dried root of the dicotyledonous plant Scutellaria baicalensis Georgi. It is a pale yellow powder at room temperature with a bitter taste. It has significant biological activity, including antibacterial, diuretic, anti-inflammatory, anti-allergic, and antispasmodic effects, and has strong anti-cancer effects and other physiological effects. It has played an important role in clinical medicine. Baicalin can also absorb ultraviolet rays, scavenge oxygen free radicals, and inhibit the production of melanin. Therefore, it can be used in both medicine and cosmetics, and is an excellent raw material for functional beauty cosmetics.

[0028] In some embodiments, the baicalin is present in an amount of 0.3 wt% to 10 wt%, preferably 0.5 wt% to 10 wt%, based on the mass percentage of the total mass of the composition.

[0029] For example, the baicalin can be 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 2wt%, 3wt%, 4wt%, 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt% or any range therebetween, measured as a percentage by mass of the total mass of the composition.

[0030] In some embodiments, the composition further comprises cosmetically acceptable excipients and / or active ingredients.

[0031] In the present application, the excipients are commonly used by those skilled in the art, such as solvents, pH regulators, preservatives, spices, etc. The solvents include monohydric alcohols, polyols, etc., and the pH regulators include triethanolamine, arginine or citric acid, etc.

[0032] In the present application, the active ingredient is an active ingredient commonly used by those skilled in the art, for example, it can be a water-soluble active ingredient, for example, it can be hyaluronic acid, ectoine, ergothioneine, carnosine, etc.

[0033] In the present application, there is no limitation on the content of excipients and active ingredients in the composition, which can be conventionally selected as needed.

[0034] In the present application, there is no limitation on the preparation method of the composition, which can be prepared by conventional methods in the art. For example, baicalin and astaxanthin can be dissolved in water to obtain the composition.

[0035] The composition described in the present application has synergistic effects between baicalin and astaxanthin and has excellent antioxidant efficacy. The ORAC value of the composition is significantly greater than the sum of the ORAC values of baicalin and astaxanthin alone.

[0036] The composition described in the present application has a stronger protective effect against the damaging effects of free radicals and reactive oxygen species, and baicalin and astaxanthin in the composition show synergistic antioxidant activity.

[0037] In this application, there is no limitation on the method for determining antioxidant activity, and the method can be determined by conventional methods in the art, such as chemical reaction spectrophotometry, fluorescence method, and chemical titration method. Currently, the oxygen radical absorbance capacity (ORAC) is an internationally recognized and commonly used fluorescence decay method for determining the oxygen radical absorbance capacity of a sample.

[0038] ORAC stands for Oxygen Radical Absorbance Capacity. The ORAC method is one of the most commonly used methods for assessing the ability of antioxidants to combat ROS. Its principle is that a free radical initiator, such as the azo initiator compound 2,2-azobis(2,2-methylpropylimidazole) dihydrochloride, is mixed with a fluorescent probe (fluorescein sodium) to destroy the fluorescent probe, causing a change in fluorescence intensity. The fluorescence decay is quantified using a fluorimeter. The free radical initiator generates peroxyl radicals, which, in the absence of an inhibitor, rapidly destroy the fluorescence of the fluorescein dye. By tracking the time course of fluorescence decay and comparing the addition and absence of a test substance, the free radical-scavenging capacity of the test substance can be estimated. Using Trolox, a water-soluble vitamin E analog, as a quantitative standard, the ORAC method is analyzed using a fluorescence analyzer to determine the degree of protection provided by the compound compared to the standard control antioxidant Trolox. Results are expressed as μMol equivalents of Trolox. Devices that can automate measurement and calculation capabilities are 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] The experiment was tested using the ORAC Assay kit (ab233473) purchased from Abcam. Sample solutions of baicalin and astaxanthin at different concentrations were prepared, and 25 μL of sample or 25 μL of diluted standard (Trolox) control group were added to a 96-well plate. 150 μL of fluorescein solution was then added to each well, mixed well, and incubated in a 37°C incubator for 30 minutes. 25 μL of free radical initiator solution was added, mixed well, and immediately placed in a microplate fluorescence and chemiluminescence analyzer for reading at an excitation wavelength of 485 nm and an emission wavelength of 538 nm. The measurement temperature was 37°C, the measurement time was 60 minutes, and the data was read every 1 minute.

[0041] Calculation method of antioxidant activity:

[0042] Synergistic effects are determined by comparing the ORAC values actually measured for the combination with the expected or cumulative values for the individual compounds. Predicted ORAC is the combined (cumulative) antioxidant capacity of the various antioxidant compounds in the combination, where each antioxidant compound is measured individually and assuming they each act independently. The expected ORAC value for a combination can be calculated using the following equation: ORAC (total) = ORAC1 + ORAC2 + ... ORACn (n is the number of actives). Synergistic antioxidant activity is present when the ORAC value actually measured is significantly greater than the expected value. Significantly greater than the expected value means that the measured ORAC value is at least 25% higher than expected.

[0043] In the present application, most of the compositions shown in the examples showed a synergistic antioxidant activity greater than 50%, and some showed a synergistic antioxidant activity greater than 100%, which is very significant.

[0044] The composition provides stronger protection against the damaging effects of free radicals and reactive oxygen species, and the combination in the composition of this example 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] The present application provides use of the above composition in cosmetics.

[0046] In some embodiments, the cosmetic is a serum, a gel, a lotion, a foundation, or a cream.

[0047] The present application provides a cosmetic comprising the above composition.

[0048] The present application provides an antioxidant method, which comprises applying the above composition to a desired site of a subject, for example, topically applying the composition to the skin.

[0049] In the present application, there is no limitation on the dosage of the composition, which can be conventionally selected according to needs.

[0050] The present application provides use of the above composition in preparing antioxidant products.

[0051] The present application provides the use of the above composition as a cosmetic preparation or a personal care preparation for anti-oxidation.

[0052] The present application provides the use of baicalin and astaxanthin in the preparation of antioxidant products.

[0053] The present application provides a combination of baicalin and astaxanthin for use as a cosmetic preparation or a personal care preparation for antioxidant purposes.

[0054] In some embodiments, the mass ratio of the baicalin to the astaxanthin is 1:(0.005-3), preferably 1:(0.01-1), and more preferably 1:(0.02-0.3); for example, the mass ratio of the baicalin to the astaxanthin can be 1:0.005, 1:0.01, 1:0.02, 1:0.03, 1:0.04, 1:0.05, 1:0.06, 1:0.07, 1:0.08, 1:0.09, 1:0.1, 1:0.15, 1:0.2, 1:0.25, 1:0.3, 1:0.35, 1:0 .4, 1:0.45, 1:0.5, 1:0.55, 1:0.6, 1:0.65, 1:0.7, 1:0.75, 1:0.8, 1:0.85, 1:0.9, 1:0.95, 1:1, 1:1.1, 1:1.2, 1:1.3, 1:1.4, 1:1.5, 1:1.6, 1:1.7, 1:1.8, 1:1.9, 1:2, 1:2.1, 1:2.2, 1:2.3, 1:2.4, 1:2.5, 1:2.6, 1:2.7, 1:2.8, 1:2.9, 1:3 or any range therebetween.

[0055] The baicalin has a strong antioxidant effect. The present application combines astaxanthin with baicalin to enhance the antioxidant effect of baicalin, that is, astaxanthin and baicalin synergistically enhance the effect and have excellent antioxidant effect.

[0056] Example

[0057] The test was performed using the ORAC Assay kit (ab233473) purchased from Abcam. Sample solutions of baicalin and astaxanthin at varying concentrations were prepared, and 25 μL of sample or 25 μL of diluted standard (Trolox) control were added to a 96-well plate. 150 μL of fluorescein solution was then added to each well, mixed thoroughly, and incubated in a 37°C incubator for 30 minutes. 25 μL of free radical initiator solution was added, mixed thoroughly, and then immediately placed in a microplate fluorescence and chemiluminescence analyzer for reading at an excitation wavelength of 485 nm and an emission wavelength of 538 nm. The measurement temperature was 37°C, the measurement time was 60 minutes, and the data was read every 1 minute.

[0058] The antioxidant activity of each component alone and in combination was evaluated and the results are shown in the Examples below. Assuming that the antioxidant effect is additive, predictions were made for each composition and compared to the actual activity measurements of the present combination in the table.

[0059] When combined with astaxanthin, baicalin can produce significant synergistic effects, as shown by the oxygen radical absorbance capacity (ORAC) assay, thereby enhancing the antioxidant activity against reactive species, particularly superoxide radical species. These synergistic antioxidant effects, combined with other known benefits of the compounds alone, can be advantageously used in cosmetic compositions.

[0060] Concentration unit: mass %; ORAC unit: (μmol Trolox / g)

[0061] Examples 1 to 23

[0062] Baicalin (purchased from Shanghai Tongtian Biotechnology Co., Ltd., content >98%) and astaxanthin (purchased from Huaxi Biotechnology Co., Ltd., content 100%) were dissolved in water to obtain a composition. The content of baicalin and astaxanthin in the composition, as well as the mass and antioxidant measurement values of baicalin and astaxanthin are shown in Table 2.

[0063] Comparative Examples 1 to 27

[0064] Baicalin or astaxanthin is dissolved in water to obtain a composition. The content of baicalin or astaxanthin in the composition and the antioxidant measurement value are shown in Table 1.

[0065] Comparative Examples 28 to 33

[0066] Baicalin and astaxanthin were dissolved in water to obtain a composition. The contents of baicalin and astaxanthin in the composition and the antioxidant test values are shown in Table 2.

[0067] Table 1 Antioxidant activity of each component

[0068]

[0069]

[0070] Table 2

[0071]

[0072]

[0073] Experimental Example Determination of Antioxidant

[0074] The compositions obtained in the Examples and Comparative Examples were subjected to antioxidant assays, and the results are shown in Tables 1 and 2. The antioxidant assays were performed using the ORAC (Oxygen Radical Absorbance Capacity) method. Using Trolox, a water-soluble analog of vitamin E, as a quantitative standard, the assays were performed using a fluorescence analyzer to determine the protective effect of the compounds compared to the standard control antioxidant, Trolox. The results were expressed as μMol equivalents of Trolox. The assays were performed using an ORAC Assay kit purchased from Abcam. The specific procedure is as follows:

[0075] The compositions of the Examples and Comparative Examples were added to phosphate buffer, and then 25 μL of the compositions of the Examples and Comparative Examples or 25 μL of the diluted standard (Trolox) control group were added to a 96-well plate. Subsequently, 150 μL of fluorescein solution was added to each well, mixed well, and incubated in a 37°C incubator for 30 minutes. 25 μL of free radical initiator solution was added, mixed well, and immediately placed in a microplate fluorescence and chemiluminescence analyzer for reading at an excitation wavelength of 485 nm and an emission wavelength of 538 nm. The measurement temperature was 37°C, the measurement time was 60 minutes, and the data was read every 1 minute. The actual measured ORAC value of the composition was then compared with the expected or cumulative ORAC value of the individual compounds to determine synergy. The predicted ORAC is the combined (cumulative) antioxidant capacity of the various antioxidant compounds in the combination. Each antioxidant compound is measured separately and assumed to act independently. The expected ORAC value of a combination can be calculated using the following equation: ORAC (total) = ORAC1 + ORAC2 + ... ORACn (n is the number of active substances). Synergistic antioxidant activity is present when the actual measured ORAC value is significantly greater than the expected value, meaning that the measured ORAC value is at least 25% higher than expected.

[0076] As can be seen from Table 2 above, the combination of baicalin and astaxanthin shows synergistic antioxidant effect. When the mass ratio of baicalin to astaxanthin is between 1:(0.005-3), a synergistic antioxidant effect is shown. In particular, when the mass ratio is between 1:(0.02-0.3), the synergistic antioxidant activity exceeds 50% or even 100%, showing a very significant synergistic antioxidant effect.

[0077] Although the present invention has been disclosed above with reference to the embodiments, they are not intended to limit the present invention. Anyone with ordinary knowledge in the art may make slight changes and modifications without departing from the spirit and scope of the present invention. Therefore, the scope of protection of the present invention shall be determined by the scope of the patent application attached hereto.

Claims

1. A composition for topical application on the skin having an antioxidant effect, comprising baicalin and astaxanthin, wherein the mass ratio of the baicalin to the astaxanthin is 1:(0.04-0.1); Calculated as a percentage by mass of the total mass of the composition, the baicalin is 0.3 wt % to 10 wt %.

2. The composition according to claim 1, wherein In terms of mass percentage based on the total mass of the composition, the baicalin is 0.5 wt % to 10 wt %.

3. Use of the composition according to claim 1 or 2 in preparing cosmetics.

4. Use of the composition according to claim 1 or 2 in the preparation of antioxidant cosmetics.

Images