Composition for promoting desmogranulocytin expression, skin care preparation and application

Abstract

The embodiment of the invention provides a composition for promoting desmogranulocytin expression, a skin care preparation and application. The composition and the skin care preparation can be used for promoting DSG1 expression. The composition for promoting the expression of desmogranulocytin comprises: silibinin; and a compound of formula (I); formula (I): # imgabs0 #

Description

Technical Field

[0001] The present invention relates to the technical field of desmoglein expression, and in particular to a composition, a skin care preparation and uses thereof for promoting desmoglein expression. Background Art

[0002] Desmosomes are important cell-cell junction structures that maintain the mechanical integrity of epidermal cells.

[0003] DSG1 (Desmoglein 1) is a member of the desmoglein family and a major component of desmosomes. DSG1 expression promotes tight cell assembly and barrier formation, helping to establish and strengthen the skin barrier. With aging, the number and density of desmosomes (including desmoglein) in the skin decrease, weakening their adhesive function. This is a key factor contributing to skin thinning, sagging, decreased elasticity, and the appearance of wrinkles.

[0004] The molecular formula of silybin is C 25 H 22 O 10 Silybin, with a molecular weight of 482.44, is an extract obtained from the fruit and seeds of milk thistle (Silybummarianum L. Gaertn). Silybin has been previously reported to be useful in the preparation of skincare products, but studies using silybin to promote DSG1 expression have not been conducted.

[0005] Therefore, how to use silybin to promote the expression of DSG1 is an issue to be solved. Summary of the Invention

[0006] One purpose of the embodiments of the present application is to solve at least one of the problems in the above background and provide corresponding beneficial effects.

[0007] Another object of the embodiments of the present application is to provide a composition, a skin care preparation and a use for promoting the expression of desmoglein, which can be used to solve the technical problem of how to promote the expression of DSG1.

[0008] In a first aspect, the present invention provides a composition comprising:

[0009] Silybin; and

[0010] A compound represented by formula (I);

[0011] Formula (I):

[0012] The composition described in the embodiment of the first aspect, combining the compound represented by formula (I) with silybin, can play a synergistic role in promoting the expression of DSG1.

[0013] In some technical solutions, in the composition, the mass ratio of the compound represented by formula (I) to silybin is 10:(1-30).

[0014] In some technical solutions, in the composition, the concentration of the compound represented by formula (I) is 15 μg / mL, and the concentration of silybin is 1.5-45 μg / mL.

[0015] In some embodiments, the concentration of silybin in the composition is 1.5 μg / mL.

[0016] In some embodiments, the concentration of silybin in the composition is 45 μg / mL.

[0017] In a second aspect, embodiments of the present application provide a skin care preparation comprising the composition described in the first aspect.

[0018] In a third aspect, an embodiment of the present application provides a use of the composition described in the first aspect in preparing a skin care preparation.

[0019] In a fourth aspect, the present invention provides an embodiment of a method for preparing a composition for promoting the expression of desmoglein by providing silybin and / or a compound represented by formula (I).

[0020] Formula (I):

[0021] It can be understood that silybin and the compound represented by formula (I) can play a synergistic role in promoting the expression of DSG1, thereby enabling the composition having the function of promoting the expression of DSG1 to have the effect of promoting the expression of DSG1.

[0022] In some technical solutions of the fourth aspect, the composition is a skin care preparation.

[0023] In some technical solutions of the fourth aspect, the skin preparation is an external skin care preparation.

[0024] In some technical solutions of the fourth aspect, the mass ratio of the compound represented by formula (I) to silybin is 15:

[0025] (1.5~45).

[0026] In some technical solutions of the fourth aspect, the concentration of the compound represented by formula (I) is 15 μg / mL, and the concentration of silybin is 1.5-45 μg / mL; optionally, the concentration of silybin is 1.5 μg / mL; optionally, the concentration of silybin is 45 μg / mL.

[0027] The beneficial effects of the embodiments of the present invention include:

[0028] 1. In some embodiments, the composition provided in the embodiments of the present application comprises silybin and a compound represented by formula (I). The combination of the compound represented by formula (I) and silybin in the composition can synergistically promote the expression of DSG1.

[0029] 2. In some embodiments, the composition provided in the embodiments of the present application promotes the expression of DSG1 through the synergistic effect of the compound represented by formula (I) and silybin, thereby achieving the effect of protecting the skin barrier.

[0030] 3. In some embodiments, the composition provided in the embodiments of the present application promotes the expression of DSG1 through the synergistic effect of the compound represented by formula (I) and silybin, thereby achieving anti-aging and firming effects.

[0031] 4. In some embodiments, the present application provides a use of the composition described in the first aspect in preparing a skin care preparation.

[0032] 5. In some embodiments, the present application provides a use of silybin and a compound represented by formula (I) in the preparation of a composition having the function of promoting DSG1 expression. BRIEF DESCRIPTION OF THE DRAWINGS

[0033] Figure 1 This is a schematic structural diagram of the compound represented by formula (I) in the examples of this application;

[0034] Figure 2 This is a schematic structural diagram of silybin in the examples of this application;

[0035] Figure 3 A mass spectrum of the compound represented by formula (I) in the examples of this application;

[0036] Figure 4 This is a schematic diagram of a hydrogen nuclear magnetic resonance spectrum of the compound represented by formula (I) in the examples of this application;

[0037] Figure 5 This is a schematic diagram of a carbon nuclear magnetic resonance spectrum of the compound represented by formula (I) in the examples of this application;

[0038] Figure 6 This is a schematic diagram of the relative mRNA expression levels corresponding to the Control sample, sample 2-1, sample 2-2, and sample 2-4 in Experimental Example 2 of this application;

[0039] Figure 7 This is a schematic diagram of the relative mRNA expression levels corresponding to the Control sample, sample 2-1, sample 2-3, and sample 2-5 in Experimental Example 2 of this application. DETAILED DESCRIPTION

[0040] The present invention will be described in further detail below in conjunction with the accompanying drawings so that those skilled in the art can implement the invention with reference to the description.

[0041] The terms "first," "second," etc., in the embodiments of this application are used for descriptive purposes only and should not be understood to indicate or imply relative importance or implicitly specify the number of technical features indicated. Therefore, a feature defined as "first," "second," etc. may explicitly or implicitly include at least one of such features.

[0042] Furthermore, the terms "comprise," "comprising," and any variations thereof, are intended to cover non-exclusive inclusions. For example, a process, method, system, product, or apparatus comprising a series of steps or elements is not limited to the listed steps or elements, but may optionally include steps or elements not listed, or may optionally include other steps or elements inherent to the process, method, product, or apparatus.

[0043] In addition to the above, it is still important to emphasize that references to "embodiments" herein mean that a particular feature, structure, or characteristic described in conjunction with the embodiments may be included in at least one embodiment of the present application. The appearance of such phrases in various locations in the specification does not necessarily refer to the same embodiment, nor does it necessarily refer to independent or alternative embodiments that are mutually exclusive of other embodiments. It is understood, both explicitly and implicitly, by those skilled in the art that the embodiments described herein may be combined with other embodiments.

[0044] <Composition>

[0045] The present application provides a composition that promotes the expression of DSG1.

[0046] The composition comprises:

[0047] Silybin; and

[0048] A compound represented by formula (I);

[0049] The structure of formula (I) can be found in Figure 1 , or as follows:

[0050] Formula (I):

[0051] The molecular formula of silybin is C 25 H 22 O 10 , molecular weight 482.44, is an extract of the fruit and seeds of silybummarianum L.Gaertn. The structure can be found in Figure 2 .

[0052] The composition described in the embodiment of the first aspect combines the compound represented by formula (I) (referred to as the compound of formula (I)) with silybin, which can play a synergistic role in promoting the expression of DSG1.

[0053] In addition, promoting the expression of DSG1 can have a protective effect on the skin, such as protecting the skin barrier. The specific reason is that DSG1 is a member of the desmosome glycoprotein subfamily, the main component of desmosomes, and one of the key proteins that constitute desmosomes. DSG1 forms tight intercellular connections between skin keratinocytes by interacting with DSG1 and other desmosome components of adjacent cells, enabling skin cells to resist external physical friction, chemical stimulation and microbial invasion, and maintain the integrity and barrier function of the skin. With age, the number and density of desmosomes (including desmosome proteins) in the skin will decrease, and their adhesion function will also weaken. This is also one of the important reasons for thinning, sagging, decreased elasticity and wrinkles of the skin.

[0054] In addition, DSG1 is involved in intracellular signal transduction. When DSG1 binds to corresponding proteins in adjacent cells, it triggers the activation or inhibition of a series of intracellular signaling pathways, thereby regulating biological behaviors such as cell proliferation, differentiation, migration, and apoptosis. For example, during skin wound repair, the DSG1-mediated signaling pathway can promote the migration and proliferation of keratinocytes, accelerating wound healing.

[0055] In some embodiments, the mass ratio of the compound represented by formula (I) to silybin is 15:(1.5-45), that is, 10:(1-30).

[0056] In some embodiments, the concentration of the compound of formula (I) is 15 μg / mL, and the concentration of silybin is 1.5-45 μg / mL; alternatively, the concentration of silybin is 1.5 μg / mL; alternatively, the concentration of silybin is 45 μg / mL.

[0057] In some embodiments, the composition includes a solvent for dissolving silybin and the compound represented by formula (I).

[0058] In some embodiments, the solvent is a cosmetically acceptable solvent, for example, it can be selected from one or more of water, dimethyl sulfoxide (DMSO), dibutyl adipate, isononyl isononanoate, pentaerythritol tetra(ethylhexanoate), caprylic / capric triglyceride, cetyl ethylhexanoate, diisostearyl malate, and octyldodecanol.

[0059] In some embodiments, the composition includes: a cosmetically acceptable adjuvant. Optionally, the adjuvant is selected from one or more of surfactants and / or emulsifiers, preservatives, buffers, chelating agents, denaturants, opacifiers, pH adjusters, reducing agents and stabilizers, thickeners, gelling agents, film-forming polymers, fillers, matting agents, glossing agents, pigments, dyes, fragrances, and mixtures thereof.

[0060] In certain embodiments, the composition can be manufactured in the form of a cream, liquid, gel, powder, block, paste-like solid, wax-based, freeze-dried, spray, aerosol, or matrix.

[0061] Optionally, the cream is in the form of milk, ointment, cream, honey, fat, milk, emulsion, milk or milk solution.

[0062] Optionally, the liquid form is further in the form of dew, liquid, water, oil or oil-water separation.

[0063] Optionally, the gel form can be further in the form of jelly or glue.

[0064] Optionally, the powder form can be further in the form of loose powder or granules.

[0065] Alternatively, the bulk form may be further in the form of bulk powder, bulk solid, and the like.

[0066] Optionally, the wax base uses wax as the main base material.

[0067] Optionally, the lyophilized form is further in the form of lyophilized powder, lyophilized tablets, etc.

[0068] Optionally, the spray contains no propellant.

[0069] Optionally, the aerosol contains a propellant.

[0070] Optionally, the substrate is in the form of a sticker, a film, etc.

[0071] In certain embodiments, the composition can be topically applied to the hair, body hair, trunk, head, face, eyes, lips, hands, feet, skin all over the body, fingernails, nails, etc.

[0072] In some embodiments, the composition can be used to prepare a skin care preparation, and can protect the skin by promoting the expression of DSG1.

[0073] In some embodiments, the skin preparation is a topical skin care preparation.

[0074] In some embodiments, the composition is a skin care preparation, and the sum of the mass fractions of silybin and the compound represented by formula (I) in the composition is 0.0001 to 10%.

[0075] It should be noted that the compound of formula (I) can be directly purchased or synthesized by the method shown in the following steps S11 to S17:

[0076] Step S11: 3-(Benzo[d][1,3]dioxolane-5-yl)acrylic acid, bakuchiol, 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride, 4-dimethylaminopyridine, triethylamine, and tetrahydrofuran are mixed and stirred at room temperature to obtain a mixture.

[0077] In practice, 4.5 g (22.6 mmol, 1.5 equiv) of 3-(benzo[d][1,3]dioxolane-5-yl)acrylic acid, 4.5 g (15 mmol, 1 equiv) of bakuchiol, 5.76 g (30 mmol, 2 equiv) of 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride, 180 mg (1.5 mmol, 0.1 equiv) of 4-dimethylaminopyridine, 4.8 mL (37.6 mmol, 2.5 equiv) of triethylamine and 80 mL of tetrahydrofuran can be added to a 200 mL reactor and stirred at room temperature for 12 hours to obtain a mixture.

[0078] Step S12: performing a first reduced-pressure concentration on the mixture to obtain a first concentrate.

[0079] The mixture is concentrated under reduced pressure at a temperature of 40±5° C. to obtain a first concentrate.

[0080] Step S13, extracting the first concentrate dissolved in water with ethyl acetate for a target number of times, and collecting the organic layer.

[0081] In practice, first, 200 mL of water was added to the first concentrate to dissolve the first concentrate in water. Then, the aqueous layer of the first concentrate after dissolution was extracted with ethyl acetate (200 mL x 3) a target number of times, where the target number of times is ≥ 1. Finally, the organic layers were combined.

[0082] Step S14: performing a second reduced-pressure concentration on the dried organic layer to obtain a second concentrate.

[0083] In practice, first, 10 g of anhydrous sodium sulfate was added to the organic layer to dry the organic layer and filter it to obtain the dried organic layer. Then, the dried organic layer was concentrated under reduced pressure at 40±5° C. to obtain a second concentrate (crude oily product).

[0084] Step S15: adding petroleum ether to the second concentrate and performing a third concentration under reduced pressure to obtain a first solid.

[0085] In practice, 60 mL of petroleum ether was added to the second concentrate, and the mixture was concentrated under reduced pressure at 40±5° C. to obtain a first solid (yellow solid).

[0086] Step S16: mixing the mixed liquid with the first solid, beating and filtering to obtain a filter cake.

[0087] The mixed liquid includes petroleum ether and ethyl acetate, and the volume ratio of petroleum ether to ethyl acetate is 50:1.

[0088] In practice, 200 mL of a mixture of petroleum ether and ethyl acetate was mixed with the first solid and slurried for 30 minutes, and filtered using a Buchner funnel to obtain a filter cake.

[0089] Step S17: vacuum-dry the filter cake to obtain the compound of formula (I).

[0090] In practice, the filter cake is vacuum dried at 40±5° C. to obtain the compound of formula (I).

[0091] Specifically, the mass spectrum of the compound of formula (I) is as follows Figure 3 As shown, the chemical formula is C 28 H 30 O4, molecular weight is 431.22.

[0092] The nuclear magnetic properties of the compound of formula (I) are as follows Figure 4-5 As shown, the data is as follows:

[0093] 1 H NMR (500MHz, CDCl3) δ7.77(d,J=15.9Hz,1H),7.39(d,J=8.6Hz,2H),7.10(d,J=2.0Hz,1H),7.09(q,J=2 .8,2.3Hz,2H),7.06(dd,J=8.1,1.7Hz,1H),6.84(d,J=8.0Hz,1H),6.44(d,J=15.9Hz,1H),6.32(d,J=16 .2Hz,1H),6.18(d,J=16.3Hz,1H),6.03(s,2H),5.89(dd,J=17.5,10.7Hz,1H),5.11(tt,J=7.1,1.4Hz,1 H),5.08–4.99(m,2H),1.96(q,J=7.5Hz,2H),1.68(s,3H),1.59(s,3H),1.54–1.48(m,2H),1.21(s,3H).

[0094] 13C NMR (101MHz, CDCl3) δ165.59,149.95,149.71,148.42,146.20,145.65,138.07,135.56,131.33,128.60,126.94,12 6.32,124.86,124.68,121.59,115.09,112.08,108.60,106.56,101.62,42.62,41.19,25.66,23.27,23.19,17.62.

[0095] The H NMR data were obtained using a nuclear magnetic resonance spectrometer (model: Bruker AV NEO 400, manufacturer: Bruker, USA), and the C NMR data were obtained using a nuclear magnetic resonance spectrometer (model: JNM-ECZ500R / S1, manufacturer: JEOL, Japan).

[0096] <Purpose>

[0097] The present application also provides an example of the use of silybin and a compound represented by formula (I) in preparing a composition for promoting DSG1 expression.

[0098] Formula (I):

[0099] It can be understood that silybin and the compound represented by formula (I) can act synergistically to promote the expression of DSG1, and thus the composition for promoting the expression of DSG1 can have the effect of promoting the expression of DSG1.

[0100] In some embodiments, the composition is a skin care formulation.

[0101] In some embodiments, the skin preparation is a topical skin care preparation.

[0102] In some embodiments, the mass ratio of the compound represented by formula (I) to silybin is 15:(1.5-45).

[0103] In some embodiments, the concentration of the compound of formula (I) is 15 μg / mL, and the concentration of silybin is 1.5-45 μg / mL; alternatively, the concentration of silybin is 1.5 μg / mL; alternatively, the concentration of silybin is 45 μg / mL.

[0104] <Experiment>

[0105] It should be noted that in the following Experimental Examples 1 and 2, when cell culture fluid is involved, it is prepared according to the following preparation method.

[0106] The cell culture medium is a DMEM medium solution containing 10% FBS and 1% penicillin / streptomycin. The preparation method is as follows: fetal bovine serum (FBS), penicillin / streptomycin and DMEM medium are mixed to obtain a DMEM medium solution containing 10% FBS and 1% penicillin / streptomycin, wherein the volume fraction of FBS is 10% and the volume fraction of penicillin / streptomycin is 1%.

[0107] DMEM (Dulbecco's Modified Eagle Medium) refers to Dulbecco's Modified Eagle Medium, a basal culture medium widely used in cell culture. It is rich in nutrients and maintains cell pH balance. It is suitable for the culture of various cell types and has a very wide range of applications.

[0108] <Experimental Example 1>

[0109] Samples 1-1 to 1-25 were prepared and used to treat human immortalized keratinocytes, respectively. The survival rate of the cells treated with each sample was then detected using the CCK8 method (Cell Counting Kit-8 method).

[0110] The CCK8 method can be performed according to the experimental methods described in "Molecular Biology Experimental Techniques" or "Molecular Experimental Technique Guide" or "Cell Biology Experimental Course" or "Biochemistry and Molecular Biology Experiments".

[0111] Specifically, in Experimental Example 1, the CCK8 method was performed according to the relevant method described in "Molecular Biology Experimental Techniques".

[0112] 1. Experimental samples

[0113] Sample 1-1:

[0114] Sample 1-1 is a cell culture medium, which does not contain the compound of formula (I) and silybin.

[0115] Sample 1-2:

[0116] Sample 1-2 is a culture solution containing the compound of formula (I), wherein the concentration of the compound of formula (I) is 10 μg / mL.

[0117] The preparation method of sample 1-2 is as follows:

[0118] The cell culture medium and the compound of formula (I) were mixed to obtain sample 1-2.

[0119] Sample 1-3 to Sample 1-5:

[0120] Samples 1-3 to 1-5 are basically the same as sample 1-2, except for the concentration of the compound of formula (I). Therefore, the preparation method can be implemented with reference to sample 1-1.

[0121] The concentration of the compound of formula (I) in sample 1-3 was 20 μg / mL;

[0122] The concentration of the compound of formula (I) in sample 1-4 was 40 μg / mL;

[0123] The concentration of the compound of formula (I) in Sample 1-5 was 60 μg / mL.

[0124] Samples 1-6:

[0125] Samples 1-6 are culture solutions containing silybin, wherein the concentration of silybin is 25 μg / mL.

[0126] The preparation method of samples 1-6 is as follows:

[0127] The cell culture medium and silybin were mixed to obtain samples 1-6.

[0128] Sample 1-7 to Sample 1-9:

[0129] Samples 1-7 to 1-9 are basically the same as sample 1-6, except for the concentration of silybin. Therefore, the preparation method can be implemented with reference to sample 1-6.

[0130] The concentration of silybin of formula (I) in sample 1-7 was 50 μg / mL;

[0131] The concentration of silybin of formula (I) in sample 1-8 was 100 μg / mL;

[0132] The concentration of silybin of formula (I) in Samples 1-9 was 150 μg / mL.

[0133] Samples 1-10:

[0134] Samples 1-10 are culture solutions containing the compound of formula (I) and silybin; wherein the concentration of the compound of formula (I) is 10 μg / mL, and the concentration of silybin is 25 μg / mL.

[0135] The preparation method of samples 1-10 is as follows:

[0136] The cell culture medium, the compound of formula (I) and silybin were mixed to obtain samples 1-10.

[0137] Samples 1-11 to 1-13:

[0138] Samples 1-11 to 1-13 are basically the same as sample 1-10, except for the concentration of the compound of formula (I). Therefore, the preparation method can be implemented with reference to sample 1-10; wherein,

[0139] The concentration of the compound of formula (I) in sample 1-11 was 20 μg / mL;

[0140] The concentration of the compound of formula (I) in sample 1-12 was 40 μg / mL;

[0141] The concentration of the compound of formula (I) in Sample 1-13 was 60 μg / mL.

[0142] Samples 1-14:

[0143] Sample 1-14 is a culture solution containing the compound of formula (I) and silybin, wherein the concentration of the compound of formula (I) is 10 μg / mL and the concentration of silybin is 50 μg / mL;

[0144] The difference between sample 1-14 and sample 1-10 lies in the concentration of silybin. The preparation method can refer to that of sample 1-10.

[0145] Samples 1-15 to 1-17:

[0146] Samples 1-15 to 1-17 are essentially the same as sample 1-14, except for the concentration of the compound of formula (I);

[0147] The concentration of the compound of formula (I) in sample 1-15 was 20 μg / mL;

[0148] The concentration of the compound of formula (I) in sample 1-16 was 40 μg / mL;

[0149] The concentration of the compound of formula (I) in Sample 1-17 was 60 μg / mL.

[0150] Samples 1-18:

[0151] Sample 1-18 is a culture solution containing the compound of formula (I) and silybin, wherein the concentration of the compound of formula (I) is 10 μg / mL and the concentration of silybin is 100 μg / mL;

[0152] The difference between sample 1-18 and sample 1-10 lies in the concentration of silybin. The preparation method can refer to that of sample 1-10.

[0153] Samples 1-19 to 1-21:

[0154] Samples 1-19 to 1-21 are essentially the same as sample 1-18, except for the concentration of the compound of formula (I);

[0155] The concentration of the compound of formula (I) in sample 1-19 was 20 μg / mL;

[0156] The concentration of the compound of formula (I) in sample 1-20 was 40 μg / mL;

[0157] The concentration of the compound of formula (I) in sample 1-21 was 60 μg / mL.

[0158] Sample 1-22:

[0159] Sample 1-22 is a culture solution containing the compound of formula (I) and silybin, wherein the concentration of the compound of formula (I) is 10 μg / mL and the concentration of silybin is 150 μg / mL;

[0160] The difference between sample 1-22 and sample 1-10 lies in the concentration of silybin. The preparation method can refer to that of sample 1-10.

[0161] Sample 1-23 to Sample 1-25:

[0162] Samples 1-23 to 1-25 are basically the same as sample 1-22, except for the concentration of the compound of formula (I). Therefore, the preparation method can be implemented with reference to sample 1-22.

[0163] The concentration of the compound of formula (I) in sample 1-23 was 20 μg / mL;

[0164] The concentration of the compound of formula (I) in sample 1-24 was 40 μg / mL;

[0165] The concentration of the compound of formula (I) in Sample 1-25 was 60 μg / mL.

[0166] 2. Experimental results:

[0167] The experimental results are shown in Table 1.

[0168] Table 1

[0169]

[0170]

[0171] According to the above results, when the concentration of the compound of formula (I) is 0-60 μg / mL and the concentration of silybin is 0-50 μg / mL, the combination of silybin and the compound of formula (I) has essentially no adverse effect or little effect on cells.

[0172] <Experimental Example 2>

[0173] A control group (Control) and experimental groups 2-1 to 2-5 were set up, and human immortalized keratinocytes were treated with samples from each group. The expression level of DSG1 in human immortalized keratinocytes from each group was then measured using QPCR (quantitative real-time polymerase chain reaction), i.e., the relative mRNA expression level of the DSG1 gene.

[0174] The QPCR method can be performed according to the experimental methods described in "Molecular Biology Experimental Techniques" or "Molecular Experimental Technique Guide" or "Cell Biology Experimental Course" or "Biochemistry and Molecular Biology Experiments".

[0175] Specifically, in Experimental Example 2, the QPCR method was performed according to the relevant method described in "Molecular Biology Experimental Techniques".

[0176] 1. Experimental samples

[0177] The samples of the control group (Control) and experimental groups 2-1 to 2-5 are Control sample, sample 2-1, sample 2-2, sample 2-3, sample 2-4, and sample 2-5, respectively, as follows:

[0178] Control sample:

[0179] Specifically, it is a cell culture medium (DMEM medium solution containing 10% FBS and 1% penicillin / streptomycin).

[0180] Sample 2-1:

[0181] Sample 2-1 is a culture solution containing the compound of formula (I), wherein the concentration of the compound of formula (I) is 15 μg / mL.

[0182] The preparation method of sample 2-1 is as follows: the cell culture medium and the compound of formula (I) are mixed to obtain sample 2-1.

[0183] Sample 2-2:

[0184] Sample 2-2 is a culture solution containing silybin, wherein the concentration of silybin is 1.5 μg / mL.

[0185] The preparation method of sample 2-2 is as follows: the cell culture medium and silybin are mixed to obtain sample 2-2.

[0186] Sample 2-3:

[0187] Sample 2-3 is a culture solution containing silybin, wherein the concentration of silybin is 45 μg / mL.

[0188] Sample 2-3 is basically the same as sample 2-2, except for the concentration of silybin. The preparation method can refer to sample 2-2.

[0189] Samples 2-4:

[0190] Sample 2-4 is a culture solution containing the compound of formula (I) and silybin, wherein the concentration of the compound of formula (I) is 15 μg / mL and the concentration of silybin is 1.5 μg / mL.

[0191] The preparation method of sample 2-4 is as follows: cell culture medium, the compound of formula (I) and phytol are mixed to obtain sample 2-4.

[0192] Samples 2-5:

[0193] Sample 2-5 is a culture solution containing the compound of formula (I) and silybin, wherein the concentration of the compound of formula (I) is 15 μg / mL and the concentration of silybin is 45 μg / mL.

[0194] Sample 2-5 is basically the same as sample 2-4, except for the concentration of silybin. The preparation method can refer to sample 2-4.

[0195] 2. Experimental Results

[0196] The experimental results are detailed in Figures 6-7 ;

[0197] Figure 6 This is a schematic diagram of the relative expression levels of mRNA corresponding to the Control sample, sample 2-1, sample 2-2, and sample 2-4 in Experimental Example 2;

[0198] Figure 7 This is a schematic diagram of the relative mRNA expression levels corresponding to the Control sample, sample 2-1, sample 2-3, and sample 2-5 in Experimental Example 2.

[0199] from Figures 6-7 It can be seen from the results that the combination of the compound of formula (I) and silybin, especially when used at a concentration of 15 μg / mL of the compound of formula (I) and a concentration of 1.5 to 45 μg / mL of silybin, can produce a synergistic effect, increase the relative expression level of the mRNA of the DSG1 gene, and promote the expression of DSG1.

[0200] Therefore, it can be understood that when the compound of formula (I) and silybin are combined into a composition, the composition can have the function of promoting the expression of DSG1.

[0201] <Application Example 1>

[0202] This application also provides an emulsion in Application Example 1.

[0203] The emulsion is a composition containing silymarin and the compound of formula (I).

[0204] The formula of the emulsion is shown in Table 2, and the preparation process is as follows:

[0205] Heat phase A to 85°C and swell evenly;

[0206] Heat phase B to 85°C and dissolve evenly;

[0207] Add the evenly swollen phase A to the evenly dissolved phase B and homogenize for 2-3 minutes to obtain the first homogenate;

[0208] Add phase C to the first homogenate and homogenize for 1-2 minutes to obtain a second homogenate;

[0209] The second homogenate was stirred and cooled to below 40°C, and phase D and dissolved phase E were added and stirred evenly to obtain an emulsion.

[0210] Table 2

[0211]

[0212] It can be understood that the emulsion contains silymarin and the compound of formula (I), and thus can promote the expression of DSG1 and produce the technical effect of skin care.

[0213] <Application Example 2>

[0214] This application also provides an emulsion in Application Example 2.

[0215] The emulsion is a composition containing silymarin and the compound of formula (I).

[0216] The formula of the emulsion is shown in Table 3, and the preparation process is as follows:

[0217] After heating and swelling phase A uniformly, cool to below 40°C with stirring, add phase B and stir uniformly to obtain the first mixture;

[0218] Add the dissolved phase C to the first mixture and stir evenly to obtain a second mixture;

[0219] Add phase D to the second mixture and mix well to obtain an emulsion.

[0220] Table 3

[0221]

[0222] It can be understood that the emulsion contains silymarin and the compound of formula (I), and thus can promote the expression of DSG1 and produce the technical effect of skin care.

[0223] The above specific embodiments provide a detailed description of the present invention, but these do not constitute limitations of the present invention. The scope of protection of the present invention is not limited to the above embodiments. Any equivalent modifications or variations made by a person skilled in the art based on the disclosure of the present invention should be included in the scope of protection described in the claims.

Claims

1. A composition for promoting desmoglein expression, characterized in that: include: Silybin; and A compound represented by formula (I); Formula (I):

2. The composition according to claim 1, characterized in that In the composition, the mass ratio of the compound represented by formula (I) to silybin is 10:(1-30).

3. The composition according to claim 1, characterized in that In the composition, the concentration of the compound of formula (I) is 15 μg / mL, and the concentration of silybin is 1.5-45 μg / mL.

4. The composition according to claim 1, characterized in that In the composition, the concentration of silybin was 1.5 μg / mL.

5. The composition according to claim 1, characterized in that In the composition, the concentration of silybin was 45 μg / mL.

6. A skin care preparation, characterized in that include: Silybin; and A compound represented by formula (I); Formula (I):

7. Use of the composition for promoting desmoglein expression according to claim 1 in preparing a skin care preparation.

8. Use of silybin and / or a compound represented by formula (I) in the preparation of a composition for promoting desmoglein expression, Formula (I):

9. The use according to claim 8, wherein The composition is a skin care preparation.

10. The use according to claim 8, wherein In the composition, the mass ratio of the compound represented by formula (I) to silybin is 15:(1.5-45).

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