A composition with whitening effect and its application in preparing a product with whitening effect

By combining white chrysanthemum with plantain extract and using specific extraction and treatment methods, the problem of limited whitening effects in existing whitening products is solved, significantly improving the whitening effect, and providing for skin care products and cosmetics High-efficiency whitening composition.

CN115869227BActive Publication Date: 2024-12-31XIAN JIABOLI BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202211537121.0
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2022-12-02
Publication Date
2024-12-31
Estimated Expiration
2042-12-02

AI Technical Summary

Technical Problem

The whitening effect of using plantain extract alone in existing whitening products is limited, which is difficult to meet the pursuit of whitening in modern women.

Method used

Combining leucorin with plantain extract, and by specific extraction methods and solvent selection, a composition with significant whitening effect is prepared, such as a combination of plantain ethyl acetate extract and plantain leucorin, further through polymerization Amide column chromatography is used to improve whitening effect.

Benefits of technology

It significantly improves the whitening effect of plantain extract, significantly reduces melanin synthesis, provides better whitening effects, and has important application value in skin care products and cosmetics.

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Abstract

The present invention relates to the technical field of whitening active ingredients and whitening product preparation, and specifically discloses a composition with whitening effect and its application in the preparation of products with whitening effect; the composition with whitening effect comprises plantain extract and praeruptorin A; the weight ratio of the plantain extract to praeruptorin A is 5 to 10:1. Studies have shown that praeruptorin A has a good whitening effect, and adding praeruptorin A to plantain water extract can significantly improve the whitening effect of the plantain water extract. Since the composition of the present invention has a good whitening effect, it has important application value to use it as an active ingredient in the preparation of skin care products, cosmetics or medicines with whitening effect.
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Description

Technical Field

[0001] The invention relates to the technical field of whitening active ingredients and whitening product preparation, and in particular to a composition with whitening effect and application thereof in the preparation of a product with whitening effect. Background Art

[0002] Influenced by the traditional aesthetic concept of "whiteness hides three uglinesses", modern women have a persistent pursuit of whitening. Whitening means making the skin fair. Currently, the whitening products on the market mainly achieve this by reducing the production of melanin in the skin.

[0003] Plantain extract is one of the common raw materials in skin care products. Studies have shown that it has a certain whitening effect. However, the inventors found in actual applications that the whitening effect of plantain extract alone is limited and needs to be further improved. Therefore, it is of great application value to develop a composition with good whitening effect using plantain extract as the main ingredient. Summary of the invention

[0004] In order to overcome at least one of the technical problems existing in the prior art, the present invention provides a composition with whitening effect.

[0005] The above technical problems to be solved by the present invention are achieved through the following technical solutions:

[0006] A composition with whitening effect comprises plantain extract and praeruptorin A.

[0007] The inventors surprisingly found in the study that praeruptorin A has an excellent whitening effect, and adding praeruptorin A to the water extract of plantain can significantly improve the whitening effect of the water extract of plantain.

[0008] Preferably, the weight ratio of the plantain extract to praeruptorin A is 5 to 10:1.

[0009] Most preferably, the weight ratio of the plantain extract to praeruptolide A is 8:1.

[0010] Preferably, the plantain extract is prepared by the following method:

[0011] The dried plantain is extracted by heating and refluxing with water. After the extraction, the extract is concentrated and dried to obtain the plantain water extract, namely the plantain extract.

[0012] Preferably, the weight amount of water is 5 to 20 times the weight of the dry plantain.

[0013] Most preferably, the weight amount of water is 15 times the weight of the dry plantain.

[0014] Preferably, the heating reflux extraction time is 0.5 to 2 hours.

[0015] Preferably, the heating reflux extraction time is 1 hour.

[0016] Preferably, the plantain extract is prepared by the following method: soaking dried plantain in ethyl acetate at 20-30°C for 4-7 days, concentrating and drying the ethyl acetate extract after soaking to obtain the plantain ethyl acetate extract, i.e., the plantain extract.

[0017] The inventors surprisingly found in a large number of experiments that the whitening effects of the composition obtained by combining the plantain extract obtained by extraction with different solvents and praeruptorin A are very different. The inventors surprisingly found through a large number of experiments that the composition obtained by combining the plantain ethyl acetate extract prepared by the above method with praeruptorin A has a significantly higher whitening effect than the composition obtained by combining the plantain water extract with praeruptorin A; in addition, the inventors also surprisingly found that the whitening effect of the composition obtained by combining the plantain organic solvent extract obtained by extraction with other organic solvents with praeruptorin A cannot be significantly improved.

[0018] Preferably, the weight amount of ethyl acetate is 10 to 20 times the weight of the dried plantain.

[0019] Most preferably, the weight amount of ethyl acetate is 15 times the weight of the dried plantain.

[0020] Furthermore, the plantain ethyl acetate extract is further applied to a polyamide column, and first eluted with an ethanol aqueous solution with a volume fraction of 20-25% to remove impurities; then eluted with an ethanol aqueous solution with a volume fraction of 55-60%, and the eluate eluted with the ethanol aqueous solution with a volume fraction of 55-60% is collected, and the plantain extract is obtained after concentration and drying.

[0021] The inventors surprisingly found in further research that the whitening effect of the composition obtained by combining the plantain extract obtained by further passing the plantain ethyl acetate extract through the polyamide column chromatography with peucedanum praeruptoside A was further greatly improved compared with the composition obtained by combining the plantain ethyl acetate extract with peucedanum praeruptoside A; it has a very excellent whitening effect.

[0022] Here, the inventors need to explain that the selection conditions of the elution solvent of the polyamide column are very critical; studies have shown that only under the above-mentioned elution conditions of the present invention (i.e., first eluting with an ethanol aqueous solution with a volume fraction of 20-25% to remove impurities; then eluting with an ethanol aqueous solution with a volume fraction of 55-60%), the whitening effect of the composition obtained by combining the plantain extract and purpurinol A can be further significantly improved compared with the composition obtained by combining the plantain ethyl acetate extract and purpurinol A; while the whitening effect of the composition obtained by combining the plantain extract and purpurinol A prepared under other elution conditions cannot be significantly improved compared with the composition obtained by combining the plantain ethyl acetate extract and purpurinol A.

[0023] The present invention provides an application of the above composition with whitening effect in preparing a product with whitening effect.

[0024] Preferably, the product is a skin care product, a cosmetic or a medicine.

[0025] Beneficial effects: The present invention provides a new composition comprising a plantain extract and praeruptorin A; studies have shown that praeruptorin A has a good whitening effect, and adding praeruptorin A to a plantain water extract can significantly improve the whitening effect of the plantain water extract. Since the composition of the present invention has a good whitening effect, it has important application value to use it as an active ingredient in the preparation of skin care products, cosmetics or medicines with whitening effects. DETAILED DESCRIPTION

[0026] The present invention is further explained below with reference to the examples, but the examples do not limit the present invention in any form.

[0027] Example 1 Preparation of a composition having a whitening effect

[0028] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0029] The plantain extract is prepared by the following method: taking dried plantain and heating and refluxing it with 15 times the weight of water at 100° C. for 1 hour, and after the extraction, concentrating and drying the extract to obtain a plantain water extract, namely the plantain extract.

[0030] Example 2 Preparation of a composition having a whitening effect

[0031] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 5:1;

[0032] The plantain extract is prepared by the following method: taking dried plantain and heating and refluxing with 5 times the weight of water at 100° C. for extraction for 0.5 h. After the extraction, the extract is concentrated and dried to obtain a plantain water extract, namely the plantain extract.

[0033] Example 3 Preparation of a composition having a whitening effect

[0034] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 10:1;

[0035] The plantain extract is prepared by the following method: taking dried plantain and heating and refluxing it with 20 times the weight of water at 100° C. for 2 hours. After the extraction, the extract is concentrated and dried to obtain a plantain water extract, namely the plantain extract.

[0036] Example 4 Preparation of a composition having a whitening effect

[0037] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0038] The plantain extract is prepared by the following method: taking dried plantain and soaking it in 15 times the weight of ethyl acetate at 25°C for 5 days, and after the soaking, concentrating and drying the ethyl acetate extract to obtain the plantain ethyl acetate extract, namely the plantain extract.

[0039] The difference between Example 4 and Example 1 is that the preparation methods of the plantain extract are different; Example 4 uses ethyl acetate to extract plantain to obtain the plantain ethyl acetate extract; while Example 1 uses water to extract plantain to obtain the plantain water extract.

[0040] Example 5 Preparation of a composition having a whitening effect

[0041] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0042] The plantain extract is prepared by the following method:

[0043] (1) soaking dried plantain in 15 times the weight of ethyl acetate at 25° C. for 5 days, concentrating and drying the ethyl acetate extract to obtain a plantain ethyl acetate extract;

[0044] (2) The ethyl acetate extract of plantain is further applied to a polyamide column (the polyamide column is filled with a 60-90 mesh polyamide resin; the weight of the polyamide resin is 35 times the weight of the ethyl acetate extract of plantain), and impurities are first eluted with 5 times the column volume of an ethanol aqueous solution with a volume fraction of 23%; then, it is eluted with 5 times the column volume of an ethanol aqueous solution with a volume fraction of 58%, and the eluate eluted with the 58% ethanol aqueous solution is collected, and the plantain extract is obtained after concentration and drying.

[0045] The difference between Example 5 and Example 4 is that in Example 5, the ethyl acetate extract of Plantain is further enriched with effective components through a polyamide column.

[0046] Comparative Example 1 Preparation of a composition having a whitening effect

[0047] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0048] The plantain extract is prepared by the following method: taking dried plantain and soaking it in 15 times the weight of methanol at 25°C for 5 days, and after the soaking, concentrating and drying the methanol extract to obtain the plantain methanol extract, namely the plantain extract.

[0049] The difference between Comparative Example 1 and Example 4 is that, in Comparative Example 1, methanol is used to extract plantain to obtain plantain methanol extract; while in Example 4, ethyl acetate is used to extract plantain to obtain plantain ethyl acetate extract.

[0050] Comparative Example 2 Preparation of a composition having a whitening effect

[0051] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0052] The plantain extract is prepared by the following method: taking dried plantain and soaking it in 15 times the weight of acetone at 25°C for 5 days. After the soaking, the acetone extract is concentrated and dried to obtain the plantain acetone extract, that is, the plantain extract.

[0053] The difference between Comparative Example 2 and Example 4 is that, in Comparative Example 2, acetone is used to extract plantain to obtain plantain methanol extract; while in Example 4, ethyl acetate is used to extract plantain to obtain plantain ethyl acetate extract.

[0054] Comparative Example 3 Preparation of a composition having a whitening effect

[0055] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0056] The plantain extract is prepared by the following method:

[0057] (1) soaking dried plantain in 15 times the weight of ethyl acetate at 25° C. for 5 days, concentrating and drying the ethyl acetate extract to obtain a plantain ethyl acetate extract;

[0058] (2) The ethyl acetate extract of plantain is further applied to a polyamide column (the polyamide column is filled with a 60-90 mesh polyamide resin; the weight of the polyamide resin is 35 times the weight of the ethyl acetate extract of plantain), and impurities are first eluted with 10% ethanol aqueous solution with a volume fraction of 5 times the column volume; then, it is eluted with 30% ethanol aqueous solution with a volume fraction of 5 times the column volume, and the eluate eluted with the 30% ethanol aqueous solution is collected, and the plantain extract is obtained after concentration and drying.

[0059] The difference between Comparative Example 3 and Example 5 is that the elution conditions of the polyamide column in Comparative Example 3 are different; in Comparative Example 3, impurities are first eluted with an ethanol aqueous solution having a volume fraction of 10%; and then eluted with an ethanol aqueous solution having a volume fraction of 30%; while in Example 5, impurities are first eluted with an ethanol aqueous solution having a volume fraction of 23%; and then eluted with an ethanol aqueous solution having a volume fraction of 58%.

[0060] Comparative Example 4 Preparation of a composition having a whitening effect

[0061] The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1;

[0062] The plantain extract is prepared by the following method:

[0063] (1) soaking dried plantain in 15 times the weight of ethyl acetate at 25° C. for 5 days, concentrating and drying the ethyl acetate extract to obtain a plantain ethyl acetate extract;

[0064] (2) The ethyl acetate extract of plantain is further applied to a polyamide column (the polyamide column is filled with a 60-90 mesh polyamide resin; the weight of the polyamide resin is 35 times the weight of the ethyl acetate extract of plantain), and impurities are first eluted with 40% ethanol aqueous solution with a volume fraction of 5 times the column volume; then, it is eluted with 80% ethanol aqueous solution with a volume fraction of 5 times the column volume, and the eluate eluted with 80% ethanol aqueous solution is collected, and the plantain extract is obtained after concentration and drying.

[0065] The difference between Comparative Example 4 and Example 5 is that the elution conditions of the polyamide column in Comparative Example 3 are different; in Comparative Example 4, impurities are first eluted with a 40% by volume ethanol aqueous solution; and then eluted with an 80% by volume ethanol aqueous solution; while in Example 5, impurities are first eluted with a 23% by volume ethanol aqueous solution; and then eluted with a 58% by volume ethanol aqueous solution.

[0066] Experimental example

[0067] Human epidermal melanocytes (HEM-L cells) were taken and added to the melanocyte culture medium so that the concentration of human epidermal melanocytes was 1×10 5 / mL; then 100 μL of culture medium containing human epidermal melanocytes was added to the 96-well plate and cultured for 24 hours; then 100 μL of melanocyte culture medium containing different concentrations of the test sample was added to the experimental group; 100 μL of melanocyte culture medium was added to the blank control group and cultured for 48 hours; after the culture was completed, the supernatant was discarded and washed with PBS solution; 6 replicate wells were set for each group, of which 3 replicate wells were taken from each group for calculating the number of cells, and 100 μL of sodium hydroxide solution (2 mol / L) was added to the remaining 3 replicate wells for lysis at 90°C for 1 hour; after the lysis was completed, the OD value (absorbance value) of each well at 490nm was measured, the melanin synthesis inhibition rate was calculated, and the IC50 value was further calculated; the test results are shown in Table 1.

[0068] Melanin synthesis inhibition rate (%) = [1-(OD value of the sample group to be tested / number of cells in the sample group to be tested) / (OD value of the blank control group / number of cells in the blank control group)] × 100%.

[0069] The test samples are the compositions with whitening effect prepared in Examples 1 to 5 and Comparative Examples 1 to 4; and praeruptorin A and the plantago asiatica aqueous extract prepared according to the method of Example 1.

[0070] Table 1. Melanin synthesis inhibition test results of the composition with whitening effect of the present invention

[0071] IC50 Values Purpura chinensis 7.6 mg / mL Plantago asiatica aqueous extract 23.6mg / mL Embodiment 1 has the composition of whitening effect 15.3mg / mL Embodiment 2 has the composition of whitening effect 15.9 mg / mL Example 3 Composition with whitening effect 16.3mg / mL Embodiment 4 has the composition of whitening effect 8.1mg / mL Example 5 Composition with whitening effect 1.9 mg / mL Comparative Example 1 Composition with whitening effect 13.1mg / mL Comparative Example 2 Composition with whitening effect 13.9mg / mL Comparative Example 3 Composition with whitening effect 7.4 mg / mL Comparative Example 4 Composition with Whitening Effect 6.9 mg / mL

[0072] From the experimental data in Table 1, it can be seen that the IC50 value of peucedanum praeruptorin A in inhibiting melanin synthesis is much lower than that of the water extract of plantain; the compositions with whitening effect in Examples 1 to 3 obtained by adding peucedanum praeruptorin A to the water extract of plantain have significantly lower IC50 values ​​for inhibiting melanin synthesis than that of the water extract of plantain. This shows that peucedanum praeruptorin A has an excellent whitening effect, and adding peucedanum praeruptorin A to the water extract of plantain can significantly improve the whitening effect of the water extract of plantain.

[0073] From the experimental data in Table 1, it can be seen that the IC50 value of the whitening composition described in Example 4 for inhibiting melanin synthesis is much smaller than that of the whitening composition described in Example 1; this indicates that the whitening effect of the composition obtained by combining the ethyl acetate extract of Plantago asiatica obtained by ethyl acetate extraction with peucedanum praeruptoside A is much higher than that of the composition obtained by combining the water extract of Plantago asiatica with peucedanum praeruptoside A. In addition, the IC50 values ​​of the whitening compositions described in Comparative Examples 1 and 2 for inhibiting melanin synthesis are not significantly reduced compared with those in Example 1; their IC50 values ​​are also much higher than those of the whitening composition described in Example 4. This shows that the whitening effects of the compositions obtained by combining the plantain extracts obtained by extraction with different solvents with pekinensis apigenin A are very different; only the composition obtained by combining the plantain ethyl acetate extract obtained by extraction with ethyl acetate and pekinensis apigenin A has a significantly higher whitening effect than the composition obtained by combining the plantain water extract and pekinensis apigenin A; while the whitening effect of the composition obtained by combining the plantain organic solvent extract obtained by extraction with other organic solvents and pekinensis apigenin A cannot be significantly improved.

[0074] From the experimental data in Table 1, it can be seen that the IC50 value of the whitening composition described in Example 5 for inhibiting melanin synthesis is further significantly lower than that of the whitening composition described in Example 4, and much lower than that of the whitening composition described in Example 1 and praeruptorin A. This shows that the whitening effect of the composition obtained by combining the plantago extract obtained by further subjecting the ethyl acetate extract of grass to the polyamide column chromatography described in the present invention with praeruptorin A is further significantly improved compared with the composition obtained by combining the plantago asiatica ethyl acetate extract with praeruptorin A; and it has a very excellent whitening effect.

[0075] In addition, the IC50 values ​​of the whitening compositions described in Comparative Examples 3 and 4 for inhibiting melanin synthesis are not significantly reduced compared with Example 4; their IC50 values ​​are significantly higher than those of the whitening compositions described in Example 5. This shows that the selection of the elution solvent of the polyamide column is very critical; only the composition obtained by combining the plantago extract and praeruptorin A prepared under the elution conditions described in the present invention (i.e., first eluting with an ethanol aqueous solution with a volume fraction of 20 to 25% to remove impurities; and then eluting with an ethanol aqueous solution with a volume fraction of 55 to 60%) can further significantly improve the whitening effect of the composition compared with the composition obtained by combining the plantago asiatica ethyl acetate extract and praeruptorin A; while the composition obtained by combining the plantago extract and praeruptorin A prepared under other elution conditions cannot further significantly improve the whitening effect.

Claims

1. A composition having a whitening effect, characterized in that: The whitening composition is prepared by mixing plantain extract and praeruptorin A in a weight ratio of 8:1; The plantain extract is prepared by the following method: (1) soaking dried plantain in 15 times the weight of ethyl acetate at 25°C for 5 days, concentrating and drying the ethyl acetate extract to obtain the plantain ethyl acetate extract; (2) The ethyl acetate extract of plantain is further applied to a polyamide column, wherein the polyamide column is filled with a 60-90 mesh polyamide resin, wherein the weight of the polyamide resin is 35 times the weight of the ethyl acetate extract of plantain; first, elution is performed with 5 times the column volume of an ethanol aqueous solution with a volume fraction of 23% to remove impurities; then, elution is performed with 5 times the column volume of an ethanol aqueous solution with a volume fraction of 58%, and the eluate eluted with the 58% ethanol aqueous solution is collected, and the plantain extract is obtained after concentration and drying.

2. Use of the composition with whitening effect according to claim 1 in the preparation of products with whitening effect.

3. The use according to claim 2, characterized in that: The product is a skin care product or a cosmetic.