Application of polycarpus polycarpus extract

By using sensual grass extract as an ingredient that inhibits tyrosinase activity, the side effects of raw materials for inhibiting tyrosinase activity in existing whitening products were solved, and whitening cosmetics with effective whitening effect and high safety were achieved.

CN119499148APending Publication Date: 2025-02-25CAPITALBIO CORP +1
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Patent Information

Application Number
CN202411751625.1
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-02
Publication Date
2025-02-25

AI Technical Summary

Technical Problem

The commonly used raw materials for inhibiting tyrosinase activity in existing whitening products, such as kojic acid and hydroquinol, may lead to side effects such as skin sensitivity and cancer, and lack natural substitutes with fewer side effects and good efficacy.

Method used

Synopsis extract is used as a component to inhibit tyrosinase activity, and the synopsis extract is prepared by Soxhlet extraction and vacuum freeze-drying and other methods, which is used for the development of whitening cosmetics.

Benefits of technology

Sensei grass extract has good inhibition of tyrosinase activity, can effectively reduce the production of melanin and reduce the skin side effects caused by the use of whitening products. Compared with expensive medicinal materials such as Rhodiola, Sensei grass has more application value.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention provides an application of a polycarpus polycarpus extract in preparation of a product for inhibiting tyrosinase activity. The polycarpus polycarpus extract provided by the invention has good activity of inhibiting tyrosinase, and can be used for developing whitening cosmetics.
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Description

Technical Field

[0001] The invention belongs to the technical field of traditional Chinese medicine extraction, and particularly relates to a herb extract. Background Art

[0002] Tyrosinase (TYR) is an oxidase and a rate-limiting enzyme that regulates melanin production. The enzyme participates in two reactions in the melanin production process: one is to hydroxylate monophenols into diphenols, and the other is to oxidize o-diphenols into o-diquinones. o-Diquinones then undergo several steps of reaction to form melanin. Currently, the purpose of inhibiting melanin formation is mainly achieved through the following two strategies: Strategy 1 is to prevent the formation of melanin, that is, to inhibit the activity of tyrosinase; Strategy 2 is to promote the excretion of melanin that has been generated. Strategy 1 is currently the key research direction for the development of whitening products. For example, some raw materials that inhibit the activity of tyrosinase, such as kojic acid and hydroquinone, are often added to whitening cosmetics as functional ingredients. However, the long-term use of the aforementioned whitening cosmetic additives will cause side effects such as skin sensitivity and cancer.

[0003] Adding the traditional Chinese medicine Soxhlet alcohol extract to cosmetic products as a functional raw material is a combination of traditional Chinese medicine and modern cosmetics. In recent years, the number of cosmetics using Chinese herbal plant ingredients and the number of patent documents on Chinese herbal cosmetics have continued to increase, indicating that the public's recognition of Chinese herbal cosmetics is also increasing. Therefore, exploring natural Chinese herbal medicine Soxhlet alcohol extracts with fewer side effects and good efficacy is of great significance for the development of whitening cosmetics. Summary of the invention

[0004] In view of this, the technical problem to be solved by the present invention is to provide a herbaceous safflower extract. The herbaceous safflower extract provided by the present invention has good tyrosinase inhibitory activity and can be used for the development of whitening cosmetics.

[0005] The invention provides an application of a herbaceous safflower extract in preparing a product for inhibiting tyrosinase activity.

[0006] The invention also provides an application of the extract of the herbaceous safflower in preparing a product with whitening effect.

[0007] Preferably, the extract of Sedum sibiricum is an alcohol extract of Sedum sibiricum.

[0008] Preferably, the method for preparing the alcohol extract of the herb comprises the following steps:

[0009] The crushed herbal medicine is mixed with an ethanol aqueous solution and subjected to Soxhlet extraction to obtain an extract;

[0010] The extract is dried to obtain the alcohol extract of Senna strychnifolia.

[0011] Preferably, the volume percentage of the ethanol aqueous solution is 60% to 100%.

[0012] Preferably, the mass volume ratio of the crushed herbal medicine to the ethanol aqueous solution is 1g:5-20ml.

[0013] Preferably, the Soxhlet extraction time is 0.5 to 4 hours.

[0014] Preferably, the drying comprises vacuum freeze drying.

[0015] Preferably, the product is a whitening cosmetic, and the whitening cosmetic includes lotion, essence, emulsion, cream or facial mask.

[0016] Preferably, the amount of the Herba Lysimachiae extract added to the product is 0.0625-1 mg / mL.

[0017] Compared with the prior art, the present invention provides an application of a herbaceous sage extract in the preparation of a product that inhibits tyrosinase activity. The herbaceous sage extract provided by the present invention has good tyrosinase inhibition activity and can be used in the development of whitening cosmetics. DETAILED DESCRIPTION

[0018] The invention provides an application of a herbaceous safflower extract in preparing a product for inhibiting tyrosinase activity.

[0019] The present invention uses the herb of Polycarpaeacorymbosa (L.) Lam. as a raw material, wherein the herb is the whole herb of the Caryophyllaceae plant Polycarpaeacorymbosa (L.) Lam., which is distributed in South China, Jiangxi, Fujian, Yunnan and other places. It has the effects of clearing away heat and detoxifying, promoting dampness and removing accumulation. It is used for summer-heat diarrhea, dysentery, painful urination, ascites, infantile malnutrition, carbuncle and swelling. "Quanzhou Materia Medica" records, "60g of fresh Polycarpaeacorymbosa whole herb. Mash and squeeze the juice for oral administration, and apply the residue to the affected area."

[0020] The extract of the herb of senna provided by the present invention has the function of inhibiting tyrosinase activity. In the present invention, the extract of the herb of senna is an alcohol extract of the herb of senna.

[0021] The present invention has no particular limitation on the preparation method of the alcohol extraction of the herb, and any extraction method known to those skilled in the art may be used.

[0022] Preferably, in the present invention, the method for preparing the alcohol extract of the herb comprises the following steps:

[0023] The crushed herbal medicine is mixed with an ethanol aqueous solution and subjected to Soxhlet extraction to obtain an extract;

[0024] The extract is dried to obtain the alcohol extract of Senna strychnifolia.

[0025] The invention firstly grinds the dried herbal medicine to obtain the grinded herbal medicine, then wraps the grinded herbal medicine and places it in a Soxhlet extraction device, and then adds ethanol water solution for heating extraction.

[0026] Wherein, the volume percentage of the ethanol aqueous solution is 60% to 100%, and can be 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 100%, or any value between 60% and 100%.

[0027] The mass volume ratio of the crushed herbal medicine to the ethanol aqueous solution is 1g:5-20ml, which can be 1g:5ml, 1g:10ml, 1g:15ml, 1g:20ml, or any value between 1g:5-20ml.

[0028] In the present invention, the Soxhlet extraction is performed for 0.5 to 4 hours, and can be 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, or any value between 0.5 and 4 hours.

[0029] After the Soxhlet extraction is completed, an extract is obtained. The extract is dried. In the present invention, there is no particular limitation on the drying method, and any drying method of traditional Chinese medicine extracts known to those skilled in the art can be used.

[0030] Preferably, the present invention first removes the solvent in the extract, and then performs vacuum freeze drying. The present invention has no particular restrictions on the method of removing the solvent, and then performs vacuum freeze drying on the extract after the solvent is removed. Finally, the extract of the herb is obtained.

[0031] The present invention applies the extract of the herb to the preparation of a product that inhibits tyrosinase activity, thereby inhibiting tyrosinase activity. The content of the extract of the herb in the product is 0.0625 to 1 mg / mL, and can be 0.0625, 0.125, 0.25, 0.5, 1, or any value between 0.0625 and 1 mg / mL.

[0032] The present invention also provides an application of a herb extract in preparing a product with whitening effect. The type and specific preparation method of the herb extract are as described above and will not be described in detail here.

[0033] In the present invention, the product with whitening effect is a whitening cosmetic. The present invention has no special limitation on the type of the whitening cosmetic. Preferably, the whitening cosmetic includes lotion, essence, emulsion, cream or mask.

[0034] Among them, in the whitening cosmetics, the content of the Sedum vulgare extract in the product is an added amount of 0.0625-1 mg / mL, which can be 0.0625, 0.125, 0.25, 0.5, 1, or any value between 0.0625 and 1 mg / mL.

[0035] The extract of the herbaceous safflower provided by the invention has a good effect of inhibiting tyrosinase activity and is helpful to reduce the generation of melanin. The extract is added to cosmetics as a cosmetic additive and is used for the development of whitening cosmetics.

[0036] Furthermore, when the Herba Lysimachiae extract provided by the present invention is used in whitening products, in order to achieve a better whitening effect, it can be used in combination with other ingredients with whitening efficacy, for example, one or more of niacinamide and resveratrol.

[0037] In order to further understand the present invention, the application of the Herba Lysimachiae extract provided by the present invention is described below in conjunction with examples, and the protection scope of the present invention is not limited by the following examples.

[0038] In the following examples and comparative examples, the model of the Soxhlet extraction apparatus is BUChi B-811 Soxhlet extraction apparatus.

[0039] The ethanol extract of radix sennae was prepared by the following method:

[0040] The herb is crushed to form a powder of the herb, 10 g of the powder is weighed and placed on filter paper to form a medicine bag, the medicine bag is placed at the bottom of a cylindrical glass sample tube of a Soxhlet extractor, 15 times the volume (150 ml) of an ethanol aqueous solution with a volume fraction of 90% is poured into a solvent cup and fixed at the lower end interface of the Soxhlet extractor, the heating level of the extraction stage is set to 16, the extraction time is 3 hours; the heating level of the drying stage is set to 10, the drying time is 20 minutes, and Soxhlet extraction is performed. After the extraction is completed, the extract is subjected to vacuum low-temperature freeze drying to finally obtain the Soxhlet alcohol extract of the herb.

[0041] The Rhodiola rosea ethanol extract was prepared by the following method:

[0042] The rhodiola rosea medicinal material is crushed to form rhodiola rosea powder, 10g of the rhodiola rosea powder is weighed and placed on filter paper to wrap into a medicine bag, the medicine bag is placed at the bottom of a cylindrical glass sample tube of a Soxhlet extractor, and then 15 times the volume (150ml) of an ethanol aqueous solution with a volume fraction of 90% is poured into a solvent cup and fixed at the lower end interface of the Soxhlet extractor, and the heating level of the extraction stage is set to 16, and the extraction time is 3h; the heating level of the drying stage is set to 10, and the drying time is 20min, and Soxhlet extraction is performed. After the extraction is completed, the extract is subjected to vacuum low-temperature freeze drying to finally obtain a rhodiola rosea Soxhlet alcohol extract.

[0043] Embodiment 1:

[0044] Ten portions of the alcohol extract of Soxhletia serrata were taken and diluted with DMSO to form a 50 mg / mL sample, and then diluted with a phosphate buffer solution at pH=6.8 to form a 1 mg / mL sample.

[0045] Embodiment 2:

[0046] Ten portions of the alcohol extract of Soxhletia serrata were taken and diluted with DMSO to form a 50 mg / mL sample, and then diluted with a phosphate buffer solution at pH=6.8 to form a 0.5 mg / mL sample.

[0047] Embodiment 3:

[0048] Ten portions of the ethanol extract of Soxhletia serrata were taken and diluted with DMSO to form a 50 mg / mL sample, and then diluted with a phosphate buffer solution at pH=6.8 to form a 0.25 mg / mL sample.

[0049] Embodiment 4:

[0050] Ten portions of the ethanol extract of Soxhletia serrata were taken and diluted with DMSO to form a 50 mg / mL sample, and then diluted with a phosphate buffer solution at pH=6.8 to form a 0.125 mg / mL sample.

[0051] Embodiment 5:

[0052] Ten portions of the ethanol extract of Soxhletia serrata were taken and diluted with DMSO to form a 50 mg / mL sample, and then diluted with a phosphate buffer solution at pH=6.8 to form a 0.0625 mg / mL sample.

[0053] Comparative Example 1:

[0054] Take 10 portions of the Rhodiola rosea ethanol extract, dilute with DMSO to form a 50 mg / mL sample, and then dilute with a phosphate buffer solution with pH=6.8 to form a 1 mg / mL sample.

[0055] Comparative Example 2:

[0056] Ten portions of the Rhodiola rosea ethanol extract were diluted with DMSO to form a 50 mg / mL sample, and then diluted with a phosphate buffer solution with pH=6.8 to form a 0.5 mg / mL sample.

[0057] Comparative Example 3:

[0058] Take 10 portions of the Rhodiola rosea Soxhlet ethanol extract, dilute with DMSO to form a 50 mg / mL sample, and then dilute with a phosphate buffer solution with pH=6.8 to form a 0.25 mg / mL sample.

[0059] Comparative Example 4:

[0060] Take 10 portions of the Rhodiola rosea ethanol extract, dilute with DMSO to form a 50 mg / mL sample, and then dilute with a phosphate buffer solution with pH=6.8 to form a 0.125 mg / mL sample.

[0061] Comparative Example 5:

[0062] Take 10 portions of the Rhodiola rosea Soxhlet ethanol extract, dilute with DMSO to form a 50 mg / mL sample, and then dilute with a phosphate buffer solution with pH=6.8 to form a 0.0625 mg / mL sample.

[0063] Test Case

[0064] The specific process of detecting the inhibition rate of mushroom tyrosinase by Examples 1 to 5 and Comparative Examples 1 to 5 using tyrosine as a substrate is as follows:

[0065] 1. Accurately weigh 2.7 mg of L-tyrosine, dilute to 5 mL with pH 6.8 phosphate buffer solution to make a 2.98 mM L-tyrosine solution, keep it away from light and keep it ready for use.

[0066] 2. Use pH 6.8 phosphate buffer solution to dilute mushroom tyrosinase with an enzyme activity of 2.5 kU / mL into a tyrosinase solution with an enzyme activity of 200 U / mL and set aside.

[0067] 3. The reaction solutions shown in Table 1 were added to a 96-well plate in sequence, for a total of 22 experimental groups, namely Group A, Group B, Group C (including ten experimental groups, Examples 1 to 5, Comparative Examples 1 to 5) and Group D (including ten experimental groups, Examples 1 to 5, Comparative Examples 1 to 5) in Table 1, for a total of 22 experimental groups, each experimental group was repeated 3 times, the reaction system was 160 μL, and after incubation at 37° C. for 10 min, 40 μL of 2.98 mM L-tyrosine was added to each well, incubated at 37° C. in the dark for 10 min, and then quickly placed in a multifunctional microplate detector, and the OD value was measured at 475 nm. The above operation was repeated for 3 times in parallel, and the effect of the embodiment or comparative example group on tyrosinase activity was calculated according to Formula I.

[0068] Inhibition rate (%) = [(AB) - (CD)] / (AB) * 100%, Formula I

[0069] In Formula I, A, B, C, and D are absorbance values ​​corresponding to each group. SPSS software was used to calculate the mass concentration IC50 value corresponding to the inhibition rate of each embodiment and comparative example when it was 50%. The smaller the IC50 value, the stronger the inhibitory effect of the combination on tyrosinase.

[0070] Table 1 Composition of each reaction solution

[0071]

[0072] Effect of various examples and comparative examples on tyrosinase activity

[0073] 1. Using the formula shown in Formula I, the inhibition rates of Examples 1 to 5 on tyrosinase at different concentrations were calculated, and the results are shown in Table 2. As can be seen from Table 2, Examples 1 to 5 of the herb have the effect of inhibiting tyrosinase at different concentrations (the inhibition rates are all greater than 0), and as the concentration decreases, the inhibition rate also decreases. The IC 50 The value is 0.17mg / mL.

[0074] Table 2 Inhibition rate and IC of tyrosinase in each example 50 value

[0075]

[0076] 2. Using the formula shown in Formula I, the inhibition rates of Comparative Examples 1 to 5 on tyrosinase at different concentrations were calculated, and the results are shown in Table 3. As can be seen from Table 3, Comparative Examples 1 to 5 of Rhodiola rosea all have the effect of inhibiting tyrosinase at different concentrations (the inhibition rates are all greater than 0), and as the concentration decreases, the inhibition rate also decreases. IC 50 The value is 0.12mg / mL.

[0077] Table 3 Inhibition rate and IC of each comparative example on tyrosinase 50 value

[0078]

[0079]

[0080] From Table 2 and Table 3, Rhodiola rosea is often used as an active ingredient in whitening cosmetics. Taking Rhodiola rosea as a comparative example, it is found that the inhibitory effect of Herba Sinensis on tyrosinase is not much different from that of Rhodiola rosea, indicating that Herba Sinensis also has the potential to be developed into whitening cosmetics. However, since Rhodiola rosea is relatively expensive and is a rhizome medicinal material, it needs to be planted repeatedly, while Herba Sinensis is relatively cheap, which is one-third of the price of Rhodiola rosea. In addition, Herba Sinensis is a whole herb medicinal material, which can be harvested every year without repeatedly planting medicinal materials. Therefore, compared with Rhodiola rosea, the Herba Sinensis extract of the present invention has more application value.

[0081] The above is only a preferred embodiment of the present invention. It should be pointed out that for ordinary technicians in this technical field, several improvements and modifications can be made without departing from the principle of the present invention. These improvements and modifications should also be regarded as the scope of protection of the present invention.

Claims

1. Use of a herbaceous safflower extract in the preparation of a product that inhibits tyrosinase activity.

2. Application of a herbaceous safflower extract in the preparation of products with whitening effects.

3. The use according to claim 1 or 2, characterized in that: The extract of shengse grass is an alcohol extract of shengse grass.

4. The use according to claim 3, characterized in that: The preparation method of the alcohol extract of the herb comprises the following steps: The crushed herbal medicine is mixed with an ethanol aqueous solution and subjected to Soxhlet extraction to obtain an extract; The extract is dried to obtain the alcohol extract of Senna strychnifolia.

5. The use according to claim 4, characterized in that: The volume percentage of the ethanol aqueous solution is 60% to 100%.

6. The use according to claim 4, characterized in that: The mass volume ratio of the crushed herbal medicine to the ethanol aqueous solution is 1g:5-20ml.

7. The use according to claim 4, characterized in that: The Soxhlet extraction time is 0.5 to 4 hours.

8. The use according to claim 4, characterized in that: The drying includes vacuum freeze drying.

9. The use according to claim 2, characterized in that: The product is a whitening cosmetic, which includes lotion, essence, emulsion, cream or facial mask.

10. The use according to claim 1 or 2, characterized in that: The amount of the Herba Lysimachiae extract added to the product is 0.0625-1 mg / mL.