Application of pterocarpus santalinus extract or pterostilbene in dual effects of removing acnes and controlling oil

By using rosewood extract and/or rosewood as raw materials for acne removal and oil control, the problem of difficult to achieve the dual effects of acne removal and oil control in the existing technology is solved, and multiple effects with high efficiency and low cost are achieved, including acne removal and oil control. Oil control, anti-inflammatory, whitening, etc., and has high safety raw materials for skin care products.

CN119074602APending Publication Date: 2024-12-06SHANGHAI INOHERB COSMETIC
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Patent Information

Application Number
CN202411074791.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-08-06
Publication Date
2024-12-06

AI Technical Summary

Technical Problem

The existing market has single raw materials for acne removal and oil control, which is difficult to achieve dual effects at the same time. The common methods are costly and highly irritating, which are prone to side effects and are difficult to cure repetitive and persistent skin inflammation.

Method used

Using rosewood extract and/or rosewood as the dual-function raw materials for acne removal and oil control, it was found that it has an inhibitory effect on Propionibacter acnes and human sebaceous cells through in vitro and cellular testing, combined with its anti-inflammatory, antioxidant and other effects. Used to prepare cosmetics or skin care products.

Benefits of technology

It has achieved efficient and low-cost acne removal and oil control effects, and has multiple effects such as acne marks, antibacterial, whitening, and anti-inflammatory, which significantly alleviates inflammation and melanin deposition caused by acne or acne, and is highly safe.

✦ Generated by Eureka AI based on patent content.

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Abstract

The pterocarpus santalinus extract or pterostilbene is applied to the dual effects of removing acnes and controlling oil. The invention provides a composition for removing acnes and / or controlling oil, wherein the composition comprises a pterocarpus santalinus extract and / or pterostilbene as an active ingredient for removing acnes and / or an active ingredient for controlling oil. The invention also provides application of the pterocarpus santalinus extract and / or pterostilbene in preparation of drugs, cosmetics or skin care products for removing acnes and / or controlling oil. The inventor finds that the pterocarpus santalinus extract and / or pterostilbene serving as a single active component can achieve multiple effects, and the pterocarpus santalinus extract and / or pterostilbene show potential application prospects in the field of modern skin care products with simplified skin care and natural multiple effects.
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Description

Technical Field

[0001] The present invention belongs to the technical field of cosmetics, and relates to the use of rosewood extract and / or pterostilbene for preparing medicines, cosmetics or skin care products with acne removal and oil control effects, and compositions containing rosewood extract and / or pterostilbene as acne removal active ingredients and / or oil control active ingredients. The present invention also relates to medicines, cosmetics or skin care products containing rosewood extract and / or pterostilbene. Background Art

[0002] With the continuous development of the skin care and cosmetics industry, various functional raw materials are constantly being discovered, raw material reserves are constantly expanding, and people's requirements for facial skin care are getting higher and higher.

[0003] However, the pace of life of modern people is getting faster and faster, and unreasonable eating habits and irregular lifestyles lead to many skin problems, such as excessive secretion of skin oil, blockage of the ducts of the sebaceous glands of the hair follicles, causing acne or acne, and further leading to a series of problems such as skin inflammation and dull skin. At the same time, endocrine disorders and hormone changes in adolescence can also cause acne or acne, promote the development of sebaceous glands and produce a large amount of sebum, causing sebum discharge disorders, forming keratin plugs, i.e., microacne and other skin problems. There are a variety of microbial flora in the hair follicles, among which the lipase produced by Propionibacterium acnes decomposes sebum to produce free fatty acids, promotes inflammatory cells and mediators, and causes skin problems such as inflammatory reactions. Therefore, it is very important to develop new, efficient, and low-cost acne-removing and oil-controlling functional raw materials.

[0004] At present, the effective raw materials for acne removal and oil control in the market are single, and it is difficult to achieve the dual effects of acne removal and oil control at the same time. At the same time, after the hair follicles, sebaceous glands and skin follicles are out of balance, the Propionibacterium acnes in the follicles induces a series of inflammations, and this series of inflammations are usually recurrent and persistent, which is difficult to cure, and requires the use of external medications and internal conditioning methods. However, this type of method is costly, has strong irritation, and is prone to side effects.

[0005] Therefore, there is an urgent need to develop a skin care product raw material that is highly efficient, low-cost, and has the synergistic dual effects of acne removal and oil control. Summary of the invention

[0006] In view of the deficiencies in the prior art, the object of the present invention is to provide a rosewood extract and / or pterostilbene as a medicine, cosmetic or skin care product raw material for acne removal and oil control. The inventor unexpectedly found that rosewood extract and / or pterostilbene have the dual effects of acne removal and oil control. Specifically, the inventor found through various in vitro and cell test results that rosewood extract and / or pterostilbene as active ingredients have a good inhibitory effect on bacteria such as Propionibacterium acnes, and have a good inhibitory effect on the secretion of sebum by human sebaceous gland cells. Therefore, the present invention provides rosewood extract and / or pterostilbene for the preparation of medicines, cosmetics or skin care products with acne removal and oil control effects, and a composition comprising rosewood extract and / or pterostilbene, wherein rosewood extract and / or pterostilbene as a single active ingredient achieve multiple effects, while having good acne removal and oil control effects, it also has additional effects such as acne removal, antibacterial, whitening, anti-inflammatory, and antioxidant.

[0007] In the present invention, pterostilbene has a chemical structure as shown in the following formula (I):

[0008]

[0009] The objective of the present invention is achieved through the following technical solutions:

[0010] A first aspect of the present invention relates to an acne-removing and / or oil-controlling composition, wherein the composition comprises rosewood extract and / or pterostilbene as an acne-removing active ingredient and / or an oil-controlling active ingredient.

[0011] In some embodiments, the composition is a pharmaceutical composition.

[0012] In some embodiments, the composition is a cosmetic composition.

[0013] In some embodiments, the composition is a skin care composition.

[0014] In some embodiments, the composition comprises rosewood extract and / or pterostilbene as the sole anti-acne active ingredient.

[0015] In some embodiments, the composition comprises rosewood extract and / or pterostilbene as the sole oil-controlling active ingredient.

[0016] In some embodiments, the composition comprises rosewood extract and / or pterostilbene as the sole anti-acne active ingredient and the oil-control active ingredient.

[0017] In some embodiments, the composition comprises rosewood extract and / or pterostilbene as the sole active ingredients.

[0018] In some embodiments, the rosewood extract and / or pterostilbene also serve as an active ingredient for removing acne scars.

[0019] In some embodiments, the composition comprises rosewood extract and / or pterostilbene as an anti-acne active ingredient, an oil-control active ingredient, and an anti-acne scar active ingredient.

[0020] In some embodiments, the composition comprises rosewood extract and / or pterostilbene as the sole anti-acne active ingredient, the oil control active ingredient, and the acne scar removing active ingredient.

[0021] In some embodiments, the weight of the rosewood extract and / or pterostilbene accounts for 0.01%-20% of the total weight of the composition.

[0022] In some embodiments, the rosewood extract comprises 5% to 50% pterostilbene by weight.

[0023] In some embodiments, the rosewood extract comprises 5% to 30% pterostilbene by weight.

[0024] In some embodiments, the rosewood extract further comprises one or more components selected from the group consisting of lipids, carbohydrates, polyphenols, flavonoids, terpenes, vitamins, fibers, pigments, acids, and volatile oils.

[0025] In some embodiments, the rosewood extract is extracted using conventional extraction methods in the art, such as organic solvent extraction, chromatography extraction, or supercritical fluid extraction.

[0026] In some embodiments, after the extraction, the extract is concentrated and dried to obtain the rosewood extract.

[0027] In some embodiments, the composition is a pharmaceutical composition, a cosmetic composition, or a skin care composition.

[0028] In some embodiments, the composition further comprises a pharmaceutically or cosmetically acceptable excipient.

[0029] In some embodiments, the pharmaceutical composition is selected from one or more of a cream, a gel, a patch, a spray, an ointment, a plaster, a lotion, a liniment, a paste, or a poultice.

[0030] In some embodiments, the cosmetic composition or skin care composition is selected from one or more of lotion, skin softener, toner, astringent, emulsion, massage cream, nourishing cream, moisturizing cream, hand cream, foundation, essence, facial mask, soap, facial cleanser, facial cleanser, facial cream, moisturizing milk or shower gel.

[0031] The second aspect of the present invention relates to the use of rosewood extract and / or pterostilbene in the preparation of medicines, cosmetics or skin care products for acne removal and / or oil control.

[0032] In some embodiments, the rosewood extract and / or pterostilbene is used as the only anti-acne active ingredient in a drug, cosmetic or skin care product.

[0033] In some embodiments, the rosewood extract and / or pterostilbene is used as the only oil-controlling active ingredient in a drug, cosmetic, or skin care product.

[0034] In some embodiments, the rosewood extract and / or pterostilbene is used as the only anti-acne active ingredient and oil-control active ingredient in medicines, cosmetics or skin care products.

[0035] In some embodiments, the rosewood extract and / or pterostilbene is added in an amount of 0.01%-20% by weight in medicines, cosmetics or skin care products.

[0036] In some embodiments, the rosewood extract comprises 5% to 50% pterostilbene by weight.

[0037] In some embodiments, the rosewood extract comprises 5% to 30% pterostilbene by weight.

[0038] In some embodiments, the medicament is selected from one or more of a cream, a gel, a patch, a spray, an ointment, a plaster, a lotion, a liniment, a paste, or a poultice.

[0039] In some embodiments, the cosmetics or skin care products are selected from one or more of lotion, skin softener, toner, astringent, emulsion, massage cream, nourishing cream, moisturizing cream, hand cream, foundation, essence, facial mask, soap, facial cleanser, facial cleanser, facial cream, moisturizing milk or shower gel.

[0040] In some embodiments, the use further comprises preventing skin inflammation.

[0041] In some embodiments, the use further comprises preventing skin melanin deposition.

[0042] In some embodiments, the use further comprises preventing skin inflammation and skin melanin deposition.

[0043] In some embodiments, the skin inflammation and / or skin melanin deposition is skin inflammation and / or skin melanin deposition associated with acne.

[0044] In some embodiments, the use further comprises removing acne scars.

[0045] The third aspect of the present invention relates to the use of rosewood extract and / or pterostilbene in the preparation of medicines, cosmetics or skin care products for removing acne and / or controlling oil and / or preventing skin inflammation and / or skin melanin deposition.

[0046] The fourth aspect of the present invention relates to the use of rosewood extract and / or pterostilbene in the preparation of medicines, cosmetics or skin care products for removing acne and / or controlling oil and / or removing acne marks.

[0047] In some embodiments, the rosewood extract and / or pterostilbene are used as an anti-acne active ingredient, an oil-control active ingredient, and an acne scar removing active ingredient in medicines, cosmetics, or skin care products.

[0048] In some embodiments, the rosewood extract and / or pterostilbene is used as the sole acne-removing active ingredient, oil-controlling active ingredient, and acne-scar removing active ingredient in medicines, cosmetics, or skin care products.

[0049] The composition of the present invention can be prepared by any suitable method known in the art using corresponding auxiliary materials according to the specific dosage form.

[0050] The beneficial effects of the present invention are as follows:

[0051] The inventors have discovered that rosewood extract and / or pterostilbene as a single active ingredient can achieve multiple functions. Obviously, when rosewood extract and / or pterostilbene are used as active ingredients, their multi-target and multi-functional properties help to meet the modern skin care concept of streamlined skin care, and show important scientific research value and potential application prospects in the field of streamlined skin care, natural and multi-functional modern skin care products.

[0052] The inventors have found that the rosewood extract and / or pterostilbene have at least the following effects:

[0053] 1) It has a good inhibitory effect on bacteria such as Propionibacterium acnes. The minimum bactericidal concentration test (MBC) results show that the MBC value of pterostilbene for Propionibacterium acnes is less than 0.156%. In addition, pterostilbene has a selective inhibitory effect on Propionibacterium acnes, selectively inhibiting Propionibacterium acnes without destroying other bacterial flora on the skin.

[0054] 2) It has a good oil control effect on human sebaceous gland cells (SZ95 line), and the oil control efficiency of 1μg / ml can reach 33.57%, which is better than the positive control epigallocatechin gallate (EGCG) (10μg / ml inhibition rate 31%).

[0055] 3) It can effectively alleviate the inflammation problems induced by acne or pimples. Through the test of TNF-α inflammatory factor induced by Propionibacterium acnes (PA) in THP-1 cell line, the inhibition rate of TNF-α of 1 μg / ml pterostilbene was as high as 70.16%.

[0056] 4) It can effectively alleviate the problem of melanin deposition caused by acne or pimples, and achieve the effect of removing acne marks. Pterostilbene has a good whitening effect. Through the mouse B16F10 cell melanin inhibition model test, 1μg / ml pterostilbene B16F10 cell melanin inhibition rate is as high as 45.42%.

[0057] 5) In addition, pterostilbene has a series of additional advantages, such as being mild to the skin, having little irritation, having good skin permeability, having good stability, etc.

[0058] In summary, the efficacy composition containing red sandalwood extract and / or pterostilbene of the present invention has excellent acne removal, oil control, anti-inflammatory, whitening and other effects. Red sandalwood extract and / or pterostilbene can effectively inhibit Propionibacterium acnes, thereby avoiding acne or acne; it has a good oil control effect, and can effectively avoid acne or various inflammatory reactions caused by clogged pores. In addition, it can also effectively alleviate the inflammation and melanin deposition caused by acne or acne, and achieve the effect of removing acne marks at the same time. It is a comprehensive acne removal, oil control and acne mark removal efficacy raw material. BRIEF DESCRIPTION OF THE DRAWINGS

[0059] Figure 1 The results of the oil control test of human sebaceous gland cells (SZ95 system) according to Example 2 of the present invention are shown; wherein the positive control is epigallocatechin gallate EGCG.

[0060] Figure 2 The results of the TNF-α inflammatory factor test on the THP-1 cell line induced by Propionibacterium acnes (PA) according to Example 3 of the present invention are shown.

[0061] Figure 3 The results of the IL-6 inflammatory factor test of RAW cells according to Example 4 of the present invention are shown;

[0062] Figure 4 The results of the NO inflammatory factor test of RAW cells according to Example 4 of the present invention are shown;

[0063] Figure 5 B according to Embodiment 5 of the present invention is shown 16 F 10 Results of the cytomelanocortin inhibition test;

[0064] Figure 6 The results of the stability test of pterostilbene according to Example 6 of the present invention at 60° C. for 14 days are shown. DETAILED DESCRIPTION

[0065] definition

[0066] The terms "weight %" and "weight percentage" are used interchangeably herein. If not otherwise specified, percentage refers to weight percentage.

[0067] Unless otherwise indicated, all component or composition levels are in terms of the active portion of that component or composition and are exclusive of impurities, for example, residual solvents or by-products, which may be present in commercially available sources of such component or composition.

[0068] Unless otherwise indicated, all temperatures herein are in degrees Celsius (° C.) Unless otherwise indicated, all measurements herein are made at 20° C., atmospheric pressure, and 50% relative humidity.

[0069] It should be understood that each maximum numerical limit given throughout this specification includes each lower numerical limit, as if such lower numerical limits were expressly written herein. Each minimum numerical limit given throughout this specification will include each higher numerical limit, as if such higher numerical limits were expressly written herein. Each numerical range given throughout this specification will include each narrower numerical range falling within such wider numerical range, as if such narrower numerical ranges were all expressly written herein.

[0070] As used herein, the term "acne" and "pimples" are used interchangeably, and is referred to as "pimples" in the cosmetic field and as "acne" in medicine.

[0071] As used herein, the term "skin care product" means any substance and any component thereof that is intended to be rubbed, poured, sprinkled, sprayed, introduced or otherwise applied to a mammalian body or any part thereof to provide a cosmetic benefit. Skin care products may include generally recognized as safe (GRAS) substances, food additives, and materials used in non-cosmetic consumer products (including over-the-counter drugs). Skin care products may include, but are not limited to: (i) chemicals, compounds, small or large molecules, extracts, preparations, or combinations thereof that are known to induce or cause at least one effect (positive or negative) on skin tissue; (ii) chemicals, compounds, small molecules, extracts, preparations, or combinations thereof that are unclear whether they have an effect on skin tissue and are found to induce or cause an effect on skin tissue using the provided methods and systems; and (iii) compounds or combinations of compounds that provide acute and / or chronic beneficial effects to the skin or cell types normally present therein when applied to the skin. Skin care products may regulate and / or improve the skin or its associated cells (e.g., improve skin elasticity; improve skin hydration; improve skin condition; and improve cell metabolism).

[0072] As used herein, the term "active ingredient" refers to a compound that provides a benefit or improvement to the skin when applied to the skin. It should be understood that active ingredients are not only for application to the skin, but also for application to hair, nails and other mammalian keratinous tissues.

[0073] As used herein, the term "cosmetically acceptable excipients" refers to excipients that are not necessary active ingredients in cosmetics and are suitable for use in humans and / or animals without excessive adverse side effects (such as toxicity, irritation, and allergic reactions), and have a reasonable benefit / risk ratio. Typically, cosmetically acceptable excipients may include moisturizers, emulsifiers, thickeners, chelating agents, emollients, and the like.

[0074] As used herein, the term "pharmaceutically acceptable excipient" refers to an excipient that is not a necessary active ingredient in a drug itself and is suitable for administration to humans and / or animals without excessive adverse side effects (such as toxicity, irritation, and allergic reactions), and has a reasonable benefit / risk ratio. Typically, pharmaceutically acceptable excipients may include fillers, stabilizers, diluents, adhesives, surfactants, solvents, etc.

[0075] Active ingredients and other ingredients useful herein may be classified or described herein according to their cosmetic and / or therapeutic benefits or their postulated modes of action. However, it should be understood that in some cases, active ingredients and other ingredients useful herein may provide more than one cosmetic and / or therapeutic benefit, or operate via more than one mode of action. Therefore, the classification herein is for convenience only and is not intended to limit the ingredients to the specifically indicated application or applications listed.

[0076] Example

[0077] The present invention can be implemented through the following embodiments, but the present invention is not limited thereto.

[0078] The percentages involved in the embodiments of the present invention are all weight percentages unless otherwise indicated.

[0079] The instruments and equipment used in the embodiments of the present invention are all conventional instruments and equipment in the field and can be replaced by instruments and equipment that meet the corresponding standards.

[0080] Unless otherwise specified, the Chinese herbal medicine raw materials and reagents used in the embodiments of the present invention are all commercially available analytically pure reagents.

[0081] Rosewood extract, obtained from Shaanxi Kepler Biotechnology Co., Ltd.;

[0082] Pterostilbene was obtained from Shanghai BiDe Pharmaceutical Technology Co., Ltd.;

[0083] White willow bark extract, obtained from Shanghai Xiangyi Bencao Cosmetics Co., Ltd.;

[0084] The human sebaceous gland cell SZ95 cell line was obtained from Qingqi (Shanghai) Biotechnology Development Co., Ltd.;

[0085] Mouse B 16 F 10 The melanin inhibition model was obtained from the Cell Bank of the Chinese Academy of Sciences;

[0086] RAW cells were obtained from Fuheng Biotechnology Co., Ltd.;

[0087] THP-1 cell line was obtained from the Cell Bank of the Chinese Academy of Sciences.

[0088] The raw materials and instruments and equipment mentioned in the present invention are all commonly used raw materials and instruments and equipment in the field, which are only examples and are not intended to limit the scope of protection of the present invention. Those skilled in the art can select equivalent raw materials and related instruments and equipment based on the disclosure of the present invention.

[0089] Example 1 Minimum bactericidal concentration (MBC) test

[0090] Pterostilbene was dispersed in sterilized reinforced Clostridium (RCM) agar medium to prepare pterostilbene solutions of different concentrations, with concentrations of 1.25%, 0.625%, 0.31%, and 0.156% by mass. Different concentrations of positive control white willow bark extract were prepared, with concentrations of 1.0%, 0.5%, 0.25%, and 0.125% by mass. The blank control group was only added with sterilized reinforced Clostridium (RCM) agar medium.

[0091] Antibacterial tests were performed on Propionibacterium acnes, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Candida albicans, etc. Samples were added and cultured at 37°C for 3-5 days, and then the live bacteria were counted. The results are shown in Table 1A and Table 1B, where + indicates a positive result, with no inhibition; - indicates a negative result, with an inhibitory effect.

[0092] Table 1A MBC test of pterostilbene against Propionibacterium acnes

[0093]

[0094] T means viable count > 200.

[0095] Table 1B MBC test of pterostilbene against other bacteria

[0096]

[0097] T means viable count > 200.

[0098] The results of Table 1A show that pterostilbene has the best inhibitory effect on Propionibacterium acnes, with an MBC value of 0.01%. Compared with the positive control white willow bark extract (MBC value of 0.5%), pterostilbene has a better effect. The results of Table 1B show that pterostilbene has no inhibitory effect on other types of bacteria, indicating that pterostilbene has a selective inhibitory effect on Propionibacterium acnes, and selectively inhibits Propionibacterium acnes without destroying other bacterial flora on the skin.

[0099] Example 2 Human sebaceous gland cells (SZ95 system) oil control test

[0100] The human sebaceous gland cell line SZ95 was used for testing, and the cells were plated in 96-well plates with DMEM++ (Thermo Fisher Scientific) at a density of 1×10 4 cells / well, 100 μL per well, and cultured overnight in a 37°C constant temperature incubator (5% CO2 concentration).

[0101] After 24 hours, the original culture medium was aspirated, washed 1-2 times with PBS buffer solution, and the stimulant linoleic acid (LA) solution prepared with the culture medium was added, with a final mass / volume concentration of 0.006% (g / ml), 100 μL per well. The sample was prepared with the culture medium, the sample included a culture medium without the sample as a blank control, a 10 μg / ml epigallocatechin gallate (EGCG) solution as a positive control, and pterostilbene solutions with concentrations of 0.5 μg / ml, 1 μg / ml, and 5 μg / ml, respectively, and the above samples were added to a 96-well plate, 100 μL per well, a total of 200 μL / well.

[0102] After incubation at 37°C for 24 h (5% CO2 concentration), all the solution in the well plate was aspirated, and the well plate was washed 1-2 times with PBS buffer. Nile red staining solution prepared in PBS (final concentration 1 μg / ml) was added, 100 μL per well, and incubated at 37°C for 20 min (5% CO2 concentration). The fluorescence was detected by a microplate reader at an excitation wavelength of 485 nm and an emission wavelength of 565 nm.

[0103] The results are as follows Figure 1 As shown in Table 2, it shows that pterostilbene active substance has a good oil control effect. At a concentration of 5 μg / ml, the oil control inhibition rate can reach 33.57%, which is better than the positive control 10 μg / ml EGCG (inhibition rate 31%).

[0104] Table 2 SZ95 cell oil control inhibition rate

[0105] substance SZ95 cell oil control inhibition rate 10 μg / ml EGCG 31% 5μg / ml Pterostilbene 33.57%

[0106] Example 3 Propionibacterium acnes (PA)-induced TNF-α inflammatory factor test in THP-1 cell line

[0107] The human monocytic leukemia THP-1 cell line was used for testing, 96-well plates were plated, medium 1640++, density 5×10 4 cells / well, and phorbol ester (PMA) was added at the same time, with a final concentration of 50ng / ml, 100μL per well, and cultured overnight at 37°C incubator (5% CO2 concentration). After 24h, the original culture medium was aspirated, washed 1-2 times with PBS buffer solution, 90μL 1640++ culture medium was added to each well, and the inactivated PA solution (0.05μg / ml) prepared with the culture medium was added, 5μL per well, and the sample was prepared with the culture medium, the sample included 0.1μg / ml dexamethasone solution as a positive control, culture medium 1640++ as a blank control, and the concentrations of pterostilbene solution were 0.5μg / ml, 1μg / ml, 2.5μg / ml, and 5μg / ml, respectively. The sample was added to a 96-well plate, 5μL per well, a total of 100μL / well. Cultured in a 37°C incubator for 24h (5% CO2 concentration). After 24h, the supernatant was collected and stored, and the lower layer of cells was used to measure the activity of cck8 cells. The collected supernatant was tested for TNF-α inflammatory factor using human TNF-α ELISA kit (Aibixin (Shanghai) Biotechnology Co., Ltd.). The results are shown in Table 3 and Figure 2 As shown, the inhibition rate of TNF-α inflammatory factor of 1 μg / ml pterostilbene was as high as 70.16%, which had a better effect than the control dexamethasone.

[0108] Table 3 Inhibition rate of pterostilbene on TNF-α inflammatory factor

[0109] substance THP-1 cell TNF-α inhibition rate 100ng / ml dexamethasone 58.9% 1ug / ml Pterostilbene 70.16%

[0110] Example 4 RAW cell IL-6 and NO inflammatory factor test

[0111] Mouse macrophage RAW cells were used for testing, and the cells were plated in 96-well plates with DMEM++ as the culture medium at a density of 4×10 4 cells / well, 100 μL per well, and cultured overnight in a 37°C constant temperature incubator (5% CO2 concentration).

[0112] After 24 hours, the original culture medium was aspirated, washed 1-2 times with PBS buffer solution, 100 μL DMEM++ culture medium was added to each well, and lipopolysaccharide (LPS) stimulator prepared with the culture medium was added, 50 μL per well, and the final concentration was 1 μg / ml. The sample was then prepared with the culture medium, and the sample included 0.025 μg / ml and 0.05 μg / ml dexamethasone solutions as positive controls, culture medium as blank control, and pterostilbene solutions with concentrations of 0.5 μg / ml, 1 μg / ml, 2.5 μg / ml, and 5 μg / ml, respectively, and added to a 96-well plate, 50 μL per well, a total of 200 μL / well. Cultured in a 37°C constant temperature incubator for 24 hours (5% CO2 concentration).

[0113] After 24 hours, 50 μL of supernatant was taken from each well and added to a new 96-well plate, and NO detection was performed using a NO detection kit (Biyuntian Biotechnology Co., Ltd.). The remaining 150 μL of supernatant was collected and stored, and the lower layer of cells was used to measure the activity of cck8 cells. For the collected supernatant, the IL-6 inflammatory factor was detected using a mouse IL-6 uncoated ELISA kit (Thermo Fisher Scientific).

[0114] The results are shown in Table 4 and Figure 3-4 As shown, pterostilbene inhibited the IC 50 The value is 0.88μg / ml, and the NO inhibition IC 50 The value is 0.135μg / ml.

[0115] Compared with the positive control dexamethasone (0.88 μg / ml, inhibition rate 56.17%), it has similar efficacy performance.

[0116] Table 4 Pterostilbene IL-6 inflammatory factor inhibition IC50

[0117]

[0118]

[0119] Example 5B 16 F 10 Melanin inhibition test

[0120] Mouse melanocyte B 16 F 10 Cell lines were tested, plated in 96-well plates, culture medium 1640++, density 1×10 4Cells / well, 100 μL per well, cultured overnight in a 37°C constant temperature incubator (5% CO2 concentration). After 24 hours, the original culture medium was aspirated, washed 1-2 times with PBS buffer solution, and a melanin stimulator α-MSH (Shanghai Myrel Biochemical Technology Co., Ltd.) solution prepared with phenol red-free DMEM medium was added to a final concentration of 1 μM, 100 μL per well, and then a sample was prepared with phenol red-free DMEM medium, the sample included kojic acid (KA) with a concentration of 100 μg / ml as a positive control, culture medium as a blank control, and pterostilbene solutions with concentrations of 1.25 μg / ml, 2.5 μg / ml, 5 μg / ml, 10 μg / ml and 20 μg / ml, respectively, added to a 96-well plate, 100 μL per well, a total of 200 μL / well. The plates were cultured in a 37°C constant temperature incubator for 72 h (5% CO2 concentration), 100 μL / well of the supernatant was taken out and placed in a new 96-well plate, and the absorbance was detected at a wavelength of 405 nm using an enzyme-labeled instrument.

[0121] Results Figure 5 .from Figure 5 It can be seen that 1.25 μg / ml pterostilbene has an effect on B 16 F 10 The cell melanin inhibition rate was as high as 45.42%, which was much better than the positive control 100 μg / ml kojic acid (KA) group (53.18%). Table 5 shows the results of the DPPH-free radical scavenging test and hTYR-human tyrosinase inhibition test. It can be seen from Table 5 that pterostilbene has a good inhibitory effect on both DPPH and hTYR-human tyrosinase.

[0122] Table 5 Pterostilbene B 16 F 10 Melanin inhibition rate

[0123] substance <![CDATA[DPPH IC 50 ]]> <![CDATA[hTYR IC 50 ]]> Pterostilbene 74.1μg / ml 212.9μg / ml

[0124] Example 6 Pterostilbene stability test

[0125] 8 bottles of 0.01 wt% pterostilbene solution were prepared with 50 wt% butanediol solution, one bottle was placed in a 4°C refrigerator, and the rest was placed in a 60°C oven. Starting from the second day, one bottle was taken out every day for the first 4 days to measure the pH value, and one bottle was taken out every 2-3 days to measure the pH value. After 14 days, all pterostilbene samples were collected and tested for their efficacy. The results showed that at room temperature (25°C), after 158.4 days (according to the calculation formula T25°C = T60°C * 2^3.5), that is, after 5.3 months, the test efficacy remained almost unchanged, indicating that it has good stability, see Table 6 and Figure 6 .

[0126] Table 6 Stability analysis of pterostilbene

[0127]

[0128] It should be understood that this specification is not limited to the technical solutions shown above, and various modifications and changes can be made to various technical solutions without departing from its scope. This specification is intended to cover any modification, use or adaptive change of the present invention, which follows the general principles of this specification and includes common knowledge or common technical means in the technical field. This specification and embodiments are only regarded as exemplary, and the scope of protection of the present invention is defined by the appended claims.

Claims

1. A composition for removing acne and / or controlling oil, wherein the composition comprises rosewood extract and / or pterostilbene as an acne removing active ingredient and / or an oil controlling active ingredient.

2. The composition according to claim 1, wherein the composition comprises rosewood extract and / or pterostilbene as the sole anti-acne active ingredient and / or oil-control active ingredient; preferably, the composition comprises rosewood extract and / or pterostilbene as the sole active ingredient; preferably, the weight of the rosewood extract and / or pterostilbene accounts for 0.01%-20% of the total weight of the composition.

3. The composition according to claim 1 or 2, wherein the rosewood extract and / or pterostilbene also serve as an active ingredient for removing acne scars.

4. A composition according to any one of claims 1 to 3, wherein the rosewood extract comprises 5 to 50%, preferably 5 to 30% by weight of pterostilbene.

5. The composition according to any one of claims 1 to 4, wherein the composition is a pharmaceutical composition, a cosmetic composition or a skin care composition, and the composition optionally comprises a pharmaceutically or cosmetically acceptable excipient.

6. The composition according to claim 5, wherein the pharmaceutical composition is selected from one or more of creams, gels, patches, sprays, ointments, plasters, lotions, liniments, pastes or mud compresses; the cosmetic composition or skin care composition is selected from one or more of lotions, skin softeners, toners, astringents, lotions, massage creams, nourishing creams, moisturizing creams, hand creams, foundations, essences, facial masks, soaps, facial cleansers, cleansing milks, cleansing creams, body lotions or shower gels.

7. Use of rosewood extract and / or pterostilbene in the preparation of medicines, cosmetics or skin care products for removing acne and / or controlling oil.

8. The use according to claim 7, wherein the rosewood extract and / or pterostilbene is used as the sole anti-acne active ingredient and / or oil-control active ingredient in a medicine, cosmetic or skin care product; preferably, the rosewood extract and / or pterostilbene is used as the sole active ingredient in a medicine, cosmetic or skin care product; preferably, the amount of the rosewood extract and / or pterostilbene added to the medicine, cosmetic or skin care product is 0.01%-20% by weight.

9. Use according to claim 7 or 8, wherein the rosewood extract comprises 5 to 50%, preferably 5 to 30%, by weight of pterostilbene.

10. The use according to any one of claims 7 to 9, wherein the medicine, cosmetic or skin care product further comprises a pharmaceutically or cosmetically acceptable excipient; preferably, the medicine is selected from one or more of creams, gels, patches, sprays, ointments, plasters, lotions, liniments, pastes or mud compresses; the cosmetic or skin care product is selected from one or more of lotions, skin softeners, toners, astringents, lotions, massage creams, nourishing creams, moisturizing creams, hand creams, foundations, essences, facial masks, soaps, facial cleansers, cleansing milks, cleansing creams, body lotions or shower gels.

11. The use according to any one of claims 7 to 10, wherein the use further comprises preventing skin inflammation and / or skin melanin deposition; preferably, the skin inflammation and / or skin melanin deposition is skin inflammation and / or skin melanin deposition associated with acne; preferably, the use further comprises removing acne marks.

Citation Information

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