Use of a utin and compositions thereof

By using vitexin and its specific ratio of resveratrol in cosmetics and skincare products, skin diseases caused by sebaceous gland dysfunction are addressed, achieving oil control and providing a gentle yet effective solution.

CN122123903APending Publication Date: 2026-06-02PROYA COSMETICS CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
PROYA COSMETICS CO LTD
Filing Date
2026-04-16
Publication Date
2026-06-02

AI Technical Summary

Technical Problem

In the existing technology, there is a lack of mild and effective natural active substances for the treatment of skin diseases caused by sebaceous gland dysfunction, such as sebaceous gland hyperplasia, sebaceous gland tumor, sebaceous gland carcinoma, sebaceous gland nevus and pilosebaceous cystic hamartoma, as well as skin diseases such as acne vulgaris, seborrheic dermatitis and androgenetic alopecia, thus limiting the application of isotretinoin.

Method used

Vitexin and its compositions, especially in specific ratios with resveratrol, are used in the preparation of cosmetics and skin care products. By adding 1-10 μg/mL, especially 2 μg/mL, 5 μg/mL or 10 μg/mL of the vitexin and resveratrol composition, the oil-controlling effect is achieved through synergistic effects.

Benefits of technology

Vitexin and its compositions exhibit significant oil-controlling effects, have a mild natural source, low toxicity and side effects, and when combined with resveratrol, the oil-controlling effect is better than when used alone, showing broad market application prospects.

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Abstract

This invention discloses the application of vitexin and its composition in products, wherein the vitexin and its composition can be used in the preparation of products with oil-controlling effects; the amount of vitexin added to the product is 1-10 μg / mL; the vitexin composition comprises vitexin and resveratrol, with a mass ratio of vitexin to resveratrol of 1:9-9:1; the amount of vitexin composition added to the product is 10 μg / mL. This invention has the advantage of being applicable to the preparation of products with oil-controlling effects.
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Description

Technical Field

[0001] This invention relates to the field of natural product chemistry, and in particular to the application of vitexin and its compositions. Background Technology

[0002] Sebaceous glands, as the core component of the pilosebaceous unit, are multilobe, holosecretive accessory organs derived from the epidermis. They are primarily responsible for the synthesis and secretion of neutral lipids, playing a crucial role in the regulation of skin physiological functions. Their embryonic development is synchronized with the development of hair follicles and epidermal tissue, beginning in the 13th-16th week of fetal development. No new sebaceous glands are formed after birth, but their size gradually increases with age. Sebaceous gland cells undergo terminal differentiation and lysis, secreting lipids to the skin surface through the hair follicle pores. In addition to their core sebum production and release functions, they also perform physiological functions such as lubricating the skin and hair, regulating body temperature, and providing antibacterial activity. They are an indispensable part of the epidermal barrier and the skin's immune system.

[0003] The function of sebaceous glands is regulated by various hormones, with androgens playing the most crucial role. This characteristic is closely related to the expression of multiple hormone receptors by sebaceous gland cells. When sebaceous gland function becomes abnormal, it can trigger a series of diseases.

[0004] On the one hand, it manifests as primary functional disorders such as sebaceous gland hyperplasia, sebaceous gland tumor, sebaceous gland carcinoma, sebaceous gland nevus, and pilosebaceous cystic hamartoma;

[0005] On the other hand, it also participates in the development of common skin diseases such as acne vulgaris, seborrheic dermatitis, and androgenetic alopecia.

[0006] Currently, clinical treatment for diseases related to abnormal sebum secretion often employs a combination of topical medication and phototherapy. Topical medications include isotretinoin, benzoyl peroxide, etc.

[0007] Although isotretinoin is currently recognized as a potent sebum secretion inhibitor, its clinical application is strictly limited due to its teratogenic risks.

[0008] Against this backdrop, naturally derived lipid secretion inhibitory active substances have become a research hotspot in recent years due to their advantages such as being mild and having no obvious side effects. Studies have confirmed that polyphenols, flavonoids and various plant extracts all have certain lipid secretion inhibitory effects.

[0009] Vitexin, a natural active substance widely found in various plants, has been shown in existing studies to have multiple biological effects such as anti-oxidation, anti-inflammation, cardiovascular protection, and neuroprotection. However, to date, no studies have reported its role in inhibiting sebum secretion or improving sebaceous gland dysfunction. Summary of the Invention

[0010] The purpose of this invention is to provide an application of vitexin and its compositions. This invention has the advantage of being applicable to the preparation of products with oil-controlling effects.

[0011] The technical solution of the present invention:

[0012] An application of vitexin, wherein the vitexin can be used in the preparation of products with oil-controlling effects.

[0013] In the aforementioned application of vitexin, the amount of vitexin added to the product is 1-10 μg / mL.

[0014] In the aforementioned application of vitexin, the amount of vitexin added to the product is 2 μg / mL.

[0015] In the aforementioned application of vitexin, the amount of vitexin added to the product is 5 μg / mL.

[0016] In the aforementioned application of vitexin, the amount of vitexin added to the product is 10 μg / mL.

[0017] In the aforementioned applications of vitexin, the products include cosmetics and skincare products.

[0018] Application of a vitexin composition, wherein the vitexin composition can be used in the preparation of products with oil-controlling effects; the vitexin composition comprises vitexin and resveratrol.

[0019] In the aforementioned application of the vitexin composition, the mass ratio of vitexin to resveratrol in the vitexin composition is 1:9-9:1.

[0020] In the aforementioned application of the vitexin composition, the mass ratio of vitexin to resveratrol in the vitexin composition is 2:8-3:7.

[0021] In the aforementioned application of the vitexin composition, the mass ratio of vitexin to resveratrol in the vitexin composition is 2:8.

[0022] In the aforementioned application of the vitexin composition, the amount of vitexin composition added to the product is 10 μg / mL.

[0023] In the aforementioned applications of the vitexin composition, the products include cosmetics and skincare products.

[0024] Compared with the prior art, the beneficial effects of this application are as follows:

[0025] 1. The application of vitexin provided by this invention in the preparation of products with oil-controlling effects. Through model experiments, it was found that vitexin has significant effects in oil control. Vitexin is a mild, naturally derived active substance with little toxic side effects on the human body.

[0026] 2. The binary combination of vitexin and resveratrol, when used in a specific ratio range, can achieve a synergistic effect compared to the single use of vitexin, resulting in better oil control and broad market application prospects. Attached Figure Description

[0027] Figure 1 This is a bar chart showing the effects of different concentrations of linoleic acid on sebaceous gland cell viability in Experiment 1.

[0028] Figure 2 This is a graph showing the results of detecting the viability of sebaceous gland cells at different concentrations of vitexin alone in Experiment 1.

[0029] Figure 3 These are comparison images of the staining effects obtained by using vitexin alone in Experiment 1;

[0030] Figure 4 This is a comparison of fluorescence intensity of different groups of vitexin in Experiment 1;

[0031] Figure 5 This is a comparison chart of the staining effects of different proportions of the vitexin composition in Experiment 2;

[0032] Figure 6 This is a comparison of fluorescence intensity of different proportions of vitexin composition in Experiment 2. Detailed Implementation

[0033] The present invention will be further described below with reference to the accompanying drawings and embodiments, but this should not be construed as limiting the present invention.

[0034] Example 1. An application of vitexin, wherein the amount of vitexin added to the product is 2 μg / mL.

[0035] Example 2. Application of vitexin, wherein the amount of vitexin added to the product is 5 μg / mL.

[0036] Example 3. An application of vitexin, wherein the amount of vitexin added to the product is 10 μg / mL.

[0037] Example 4. Application of a vitexin composition, wherein the mass ratio of vitexin to resveratrol in the vitexin composition is 2:8; and the amount of the vitexin composition added to the product is 10 μg / mL.

[0038] Verification Experiment

[0039] Experiment 1: Verification of the Single Efficacy of Vitexin

[0040] Experimental Procedure

[0041] 1.1): After resuscitating sebaceous gland cells (SZ95), cell growth was observed. Cells were counted when the cell coverage reached over 80%, and the cells were seeded into multiple 96-well and multiple 24-well plates. The 96-well plates were used to detect cell viability, and the 24-well plates were used to detect Nile Red staining of sebaceous gland cells. The plates were incubated overnight in a CO2 incubator (37°C, 5% CO2).

[0042] 1.2): Solution preparation: Prepare various sample working solutions, including linoleic acid (LA) working solution and vitexin working solution.

[0043] 1.3): When the cell deposition rate reaches about 60%, administer the drug to groups; each group has 3 replicates.

[0044] 1.3.1): Take linoleic acid (LA) working solution, group it according to Table 1 below, explore the experimental concentration of linoleic acid (LA), and select LA concentration in the range of 5-1000μM for cell viability experiments.

[0045] Table 1 Experimental Grouping Table

[0046]

[0047] 1.3.2): Take the vitexin working solution, group it according to Table 2 below, and explore the concentration of vitexin in SZ95 cells. Select a concentration of 0.5-100 μg / mL for cell viability experiments.

[0048] Table 2 Experimental Grouping Table

[0049]

[0050] 1.3.3): Based on the results of 1.3.1), the optimal concentration of LA for modeling was determined to be 100 μM. According to the grouping in Table 3, samples containing vitexin within the safe concentration range of 0.5-100 μg / mL were selected for Nile Red staining and photography to detect lipid droplet secretion in SZ95 cells.

[0051] Table 3 Experimental Grouping Table

[0052]

[0053] 1.3.4): The specific steps for Nile Red staining are as follows:

[0054] Rinse: Discard the culture medium and wash 3 times with PBS;

[0055] Fixation: Add 4% paraformaldehyde (300 µL) for 30 min;

[0056] Staining: Prepare Nile Red staining solution (working concentration is 10 μg / mL), discard the fixative, rinse the cells 3 times with PBS, add Nile Red staining solution (300 µL / well) and stain for 15 min;

[0057] Photography: Observe the staining of each group of cells under an inverted fluorescence microscope and take photos;

[0058] Results analysis: Fluorescence intensity was quantitatively analyzed using software.

[0059] II. Data Processing

[0060] 2.1) Cell viability test: For each group in Tables 1 and 2, the specific method was as follows: Discard the supernatant from the 96-well plate, add 100 µL of CCK-8 working solution (prepared by CCK8 stock solution: culture medium = 1:9) to each well, and incubate in an incubator (37℃, 5% CO2) for 2 hours. Then, use a microplate reader to measure the absorbance at 450 nm.

[0061] 2.2) Cell viability: For each group in Tables 1 and 2, the inhibition rate was calculated as follows:

[0062] Cell viability (%) = [(As-Ab) / (Ac-Ab)] x 100%

[0063] As: Absorbance of experimental wells (including cells, culture medium, CCK-8 solution and drug solution);

[0064] Ac: Absorbance of control wells (containing cells, culture medium, and CCK-8 solution, but excluding drugs);

[0065] Ab: Absorbance of blank wells (containing culture medium and CCK-8 solution, but excluding cells and drugs).

[0066] 2.3) Nile Red Staining: Rinse, fix cells, stain with Nile Red, and then take pictures using a fluorescence microscope.

[0067] 2.4) Statistical Analysis of Results: Fluorescence intensity was quantitatively analyzed and plotted using software, and the results are presented as Mean+SEM. The t-test was used for comparisons between groups. P<0.05 was considered statistically significant, and P<0.01 was considered highly significant.

[0068] III. Experimental Results

[0069] 3.1) Regulation of vitexin (single) lipid droplet secretion:

[0070] For each group in Table 1, such as Figure 1As shown in Table 4, SZ95 cells exhibited a viability of over 70% and low toxicity when LA concentrations ranged from 5 to 100 μM, indicating that further experiments could be conducted.

[0071] Table 4 Cell viability results

[0072]

[0073] For each group in Table 2, such as Figure 2 As shown in Table 5, when vitexin was used alone at concentrations ranging from 0.5 to 100 μg / mL, the viability of SZ95 cells was higher than 90%, and there was no cytotoxicity.

[0074] Table 5 Cell viability results

[0075]

[0076] 3.2.1) Based on the staining results of each group in Table 3, the data were processed to obtain... Figure 3 and Figure 4 ,from Figure 3 and Figure 4 It is evident that the LA group significantly increased lipid droplet secretion compared to the blank control group, while finasteride and isosorbide Vate significantly reduced lipid droplet secretion compared to the linoleic acid group.

[0077] Vitexin at concentrations of 2 μg / mL, 5 μg / mL, and 10 μg / mL significantly reduced lipid droplet secretion compared to the linoleic acid group, demonstrating an oil-controlling effect.

[0078] Therefore, vitexin alone has an oil-controlling effect and can be used alone in the preparation of products with oil-controlling effects (such as cosmetics). The concentration range is 1-10 μg / mL, preferably 2 μg / mL, 5 μg / mL or 10 μg / mL.

[0079] Experiment 2: Efficacy Verification of Resveratrol + Vitexin (Binary Combination)

[0080] Following step 1.1) of Experiment 1, seed the plates and administer the drugs according to the groupings in Table 6 below. After drug administration, place the 24-well plates in an incubator (37℃, 5% CO2) for 24 hours, and perform the Nile Red staining experiment as per step 1.3.4). Figure 5 and Figure 6 .

[0081] Table 6 Experimental Grouping Table

[0082]

[0083] from Figure 5 and Figure 6The results showed that the LA group significantly increased lipid droplet secretion compared to the blank control group; finasteride and isosorbide Vate significantly decreased lipid droplet secretion compared to the linoleic acid group.

[0084] Resveratrol + vitexin (total concentration 10 μg / mL) significantly reduced lipid droplet secretion compared to linoleic acid in the range of 1:9-9:1, and had an oil-controlling effect. In the range of 1:9 and 6:4-9:1, it was superior to the single effect and significantly superior to vitexin alone.

[0085] At ratios of 7:3 and 8:2, it was significantly superior to resveratrol and vitexin alone;

[0086] The 8:2 ratio is the most effective.

Claims

1. An application of vitexin, characterized in that: The vitexin can be used in the preparation of products with oil-controlling effects.

2. The application of vitexin according to claim 1, characterized in that: The amount of vitexin added to the product is 1-10 μg / mL.

3. The application of vitexin according to claim 2, characterized in that: The amount of vitexin added to the product is 2 μg / mL.

4. The application of vitexin according to claim 2, characterized in that: The amount of vitexin added to the product is 5 μg / mL.

5. The application of vitexin according to claim 2, characterized in that: The amount of vitexin added to the product is 10 μg / mL.

6. The application of a vitexin composition, characterized in that: The vitexin composition can be used in the preparation of products with oil-controlling effects; the vitexin composition includes vitexin and resveratrol.

7. The application of the vitexin composition according to claim 6, characterized in that: In the vitexin composition, the mass ratio of vitexin to resveratrol is 1:9-9:

1.

8. The application of the vitexin composition according to claim 7, characterized in that: In the vitexin composition, the mass ratio of vitexin to resveratrol is 2:8-3:

7.

9. The application of the vitexin composition according to claim 8, characterized in that: In the vitexin composition, the mass ratio of vitexin to resveratrol is 2:

8.

10. The application of the vitexin composition according to claim 7, characterized in that: The amount of the vitexin composition added to the product is 10 μg / mL.