Cosmetic composition for inhibiting sebum secretion

Abstract

The purpose of the present disclosure is to provide a cosmetic composition for inhibiting sebum secretion, the cosmetic composition being capable of suppressing excessive sebum secretion and reducing diseases of the sebaceous glands or skin problems caused thereby.

Description

Cosmetic composition for inhibiting sebum secretion

[0001] The present invention relates to a cosmetic composition for inhibiting sebum secretion, and more specifically, to a cosmetic composition for inhibiting sebum secretion that has an excellent acne prevention effect by inhibiting excessive sebum secretion.

[0002] This invention was made possible through the support of the Health and Medical Technology Research and Development Project of the Korea Health Industry Development Institute, funded by the Ministry of Health and Welfare (Project No.: RS-RS-2023-KH141511).

[0003] While sebum plays an important role in maintaining skin moisture and preventing the invasion of external microorganisms, excessive secretion can lead to various problems, such as oily skin, enlarged pores, and acne. The primary cause of excessive sebum secretion is known to be the activation of sebaceous gland cells by hormones, particularly male hormones. In the past, female hormones such as estrogen were used to treat excessive sebum secretion and acne, but they are rarely used today due to side effects. Although excessive sebum secretion is recognized as a significant issue in the cosmetics industry, research has not yet been sufficiently conducted. Currently, powders that temporarily absorb sebum or extracts known to have sebum-inhibiting effects are used, but their effectiveness is minimal.

[0004] Meanwhile, peroxisome proliferator-activated receptors (PPARs) are nuclear hormone receptors with four subtypes—α, β, δ, and γ—that play a crucial role in regulating fatty acid metabolism. In particular, PPAR-α is involved in fatty acid metabolism through the regulation of fatty acid oxidase genes and can contribute to the regulation of sebum secretion by reacting with lipid-activating agents such as linoleic acid. Additionally, while PPAR-γ has been reported to influence the maturation of sebaceous gland cells, there are few instances where this has been applied to address skin problems.

[0005] Accordingly, there is a need to develop cosmetic compositions effective in inhibiting sebum secretion by inhibiting the expression of PPAR-γ.

[0006] The present invention aims to provide a cosmetic composition for inhibiting sebum secretion that can suppress excessive sebum secretion and alleviate sebaceous gland diseases or skin troubles caused by it.

[0007] The present disclosure provides a cosmetic composition for inhibiting sebum secretion comprising a compound represented by the following chemical formula 1.

[0008] [Chemical Formula 1]

[0009]

[0010] (In the above chemical formula 1,

[0011] R1 is a straight-chain (C6-C20) alkyl, and

[0012] R2 is a straight-chain or branched-chain (C1-C10) alkyl, and

[0013] L1 is a (C1-C5)alkylene.

[0014] In one embodiment, R1 may be a straight-chain (C6-C10)alkyl, R2 may be a straight-chain (C1-C5)alkyl, and L1 may be a (C1-C5)alkylene.

[0015] The present disclosure provides a cosmetic composition for inhibiting sebum secretion comprising a compound represented by the above chemical formula 2.

[0016] [Chemical Formula 2]

[0017]

[0018] In one embodiment, the cosmetic composition for inhibiting sebum secretion of the present disclosure may contain 0.001 to 1 weight percent of a compound represented by Formula 1 with respect to the total composition.

[0019] The above cosmetic composition may be formulated as a softening lotion, astringent lotion, nourishing lotion, eye cream, nourishing cream, massage cream, cleansing cream, cleansing foam, cleansing water, powder, essence, or pack.

[0020] The present disclosure provides a pharmaceutical composition for the prevention or treatment of dermatitis comprising a compound represented by the following chemical formula 1.

[0021] [Chemical Formula 1]

[0022]

[0023] (In the above chemical formula 1,

[0024] R1 is a straight-chain (C6-C20) alkyl, and

[0025] R2 is a straight-chain or branched-chain (C1-C10) alkyl, and

[0026] L1 is a (C1-C5)alkylene.

[0027] In one embodiment, R1 may be a straight-chain (C6-C10)alkyl, R2 may be a straight-chain (C1-C5)alkyl, and L1 may be a (C1-C5)alkylene.

[0028] The present disclosure provides a pharmaceutical composition for the prevention or treatment of dermatitis comprising a compound represented by the following chemical formula 2.

[0029] [Chemical Formula 2]

[0030]

[0031] According to one embodiment, the dermatitis may be acne or seborrheic dermatitis.

[0032] A cosmetic composition for inhibiting sebum secretion according to one embodiment of the present invention can effectively inhibit excessive sebum secretion by inhibiting the expression of peroxisome proliferator-activated receptor (PPAR), thereby alleviating acne or seborrheic dermatitis.

[0033] Figure 1 shows the degree of PPAR-γ mRNA expression analyzed by qPCR when the compositions of the examples and comparative examples of the present disclosure were treated to sebaceous gland cell lines.

[0034] Figure 2 shows the results of treating an artificial skin model (EpiDermFT™) with the compositions of the examples and comparative examples of the present disclosure and staining it with Nile red.

[0035] FIG. 3 shows the ratio of stained areas according to the expression of PPAR-γ by treating an artificial skin model (EpiDermFT™) with the compositions of the examples and comparative examples of the present disclosure.

[0036] The present invention will be described in detail below. Unless otherwise defined, terms used in this specification should be interpreted as generally understood by those skilled in the art. The drawings and embodiments of this specification are intended to enable those skilled in the art to easily understand and practice the present invention; therefore, details that may obscure the essence of the invention may be omitted from the drawings and embodiments, and the present invention is not limited to the drawings and embodiments.

[0037] The singular form used in this specification may be intended to include the plural form unless specifically indicated otherwise in the context.

[0038] Furthermore, the numerical range used in this invention includes lower and upper limits and all values ​​within the range, increments logically derived from the form and width of the defined range, all of the specified values, and all possible combinations of upper and lower limits of the numerical range defined in different forms. Unless otherwise specifically defined in the specification of this invention, values ​​outside the numerical range that may occur due to experimental error or rounding are also included in the defined numerical range.

[0039] In this specification, terms such as "include," "have," and "have" mean that the features or components described in the specification are present, and unless specifically limited, this does not preclude the possibility that one or more other features or components may be added.

[0040] In this specification, "for inhibiting sebum secretion" means alleviating skin greasiness caused by excessive sebum secretion, sebaceous gland disorders, or skin troubles, and includes the improvement of acne derived from oversecretion of sebum.

[0041] The term "improvement" as used in this invention refers to any act in which excessive sebum secretion is suppressed or beneficially altered by the cosmetic composition according to this invention.

[0042] As a result of further research on the degree of inhibition of Peroxisome Proliferator-Activated Receptor (PPAR) activity for inhibiting sebum secretion, the applicant confirmed that a compound represented by the following chemical formula 1 has an excellent effect in inhibiting sebum secretion.

[0043] That is, the present disclosure can achieve an excellent sebum secretion inhibitory effect by inhibiting the maturation of sebaceous gland cells.

[0044] The present disclosure provides a cosmetic composition for inhibiting sebum secretion comprising a compound represented by the following chemical formula 1.

[0045] [Chemical Formula 1]

[0046]

[0047] (In the above chemical formula 1,

[0048] R1 is a straight-chain (C6-C20) alkyl, and

[0049] R2 is a straight-chain or branched-chain (C1-C10) alkyl, and

[0050] L1 is a (C1-C5)alkylene.

[0051] The substituents comprising the “alkyl,” “alkoxy,” and other “alkyl” portions described in the present invention may be in a straight-chain or branched-chain form, and the straight-chain form is preferred. Furthermore, the alkyl, alkoxy, and hydroxyalkyl according to the present invention have 1 to 7 carbon atoms in a straight-chain form or have a straight-chain form with said number of carbon atoms, but it is also known that having 8 to 30 carbon atoms is one embodiment of the present invention.

[0052] In addition, a composition according to one embodiment of the present disclosure contains a compound represented by the above chemical formula 1 as an active ingredient, thereby suppressing sebum secretion and enabling the improvement of skin shine and the prevention of acne.

[0053] That is, the cosmetic composition according to one embodiment of the present disclosure is primarily intended for inhibiting sebum secretion, but can prevent acne by improving the condition of pores accordingly, and furthermore, can be usefully utilized to maintain hair health by improving the oily condition of the scalp.

[0054] The compound represented according to the above chemical formula 1 is a very stable substance that is easy to formulate and, in particular, exhibits excellent effects in inhibiting sebum secretion. Specifically, R1 may be a straight-chain (C6-C10) alkyl, R2 may be a straight-chain (C1-C5) alkyl, and L1 may be a (C1-C5) alkylene.

[0055] According to one embodiment, the cosmetic composition for inhibiting sebum secretion of the present disclosure may include a compound represented by the following chemical formula 2.

[0056] [Chemical Formula 2]

[0057]

[0058] The cosmetic composition for inhibiting sebum secretion of the present disclosure may contain 0.001 to 1 weight% of a compound represented by Formula 1 with respect to the total composition, specifically, the lower limit may be 0.001, 0.003, 0.005, 0.007, 0.009, 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, or 0.1 weight% to the upper limit may be 1, 0.95, 0.9, 0.85, 0.8, 0.75, 0.7, 0.65, 0.6, 0.55, 0.5, 0.45, 0.4, 0.35, or 0.3 weight%.

[0059] The cosmetic composition according to the present disclosure may be prepared by including suitable additives commonly used. In this case, examples of said additives may include one or more aqueous additives selected from purified water, stabilizers, emulsifiers, thickeners, moisturizers, liquid crystal film strengtheners, pH adjusters, antimicrobial agents, water-soluble polymers, coating agents, metal ion chelating agents, amino acids, organic amines, polymer emulsions, pH adjusters, skin nutrients, antioxidants, antioxidant aids, preservatives, fragrances, etc.; and one or more oily additives selected from oils, waxes, hydrocarbon oils, higher fatty acid oils, higher alcohols, synthetic ester oils, and silicone oils, etc.

[0060] The above aqueous additives are not limited to raw materials commonly used in the industry, and specific examples include glycerin, dipropylene glycol, butylene glycol, pentylene glycol, methylpropanediol, sorbitol, diglycerin, erythritol, pentaerythritol, polybutylene glycol-10, polyglycerin-3, polyglycerin-4, polyglycerin-6, polyglycerin-10, polyglycerin-20, polyglycerin-40, sorbes-5, sorbes-6, sorbes-20, sorbes-30, sorbes-40, inositol, maltitol, maltose, mannan, mannitol, mannose, lactitol, lactose, dihydroxypropyl PG-glucoside, dithioctanediol, fructose, glucamine, methylglucarmine, glucose. 1,2,6-Hexanethiol, Methylgluceth-10, Methylgluceth-20, Ozonized Glycerin, Phytantriol, Thioglycerin, Threitol, Trimethylolpropane, Xylitol, EDTA, Guar Gum, Quince Seed, Carrageenan, Galactan, Gum Arabic, Pectin, Mannan, Starch, Xanthan Gum, Cuddlan, Methylcellulose, Hydroxyethylcellulose, Carboxymethyl Cellulose, Methylhydroxypropyl Cellulose, Chondroitin Sulfate, Dermatan Sulfate, Glycogen, Heparan Sulfate, Hyaluronic Acid, Sodium Hyaluronate, Tragant Gum, Keratan Sulfate, Chondroitin, Mucoitin Sulfate, Hydroxyethyl Guar Gum, Carboxymethyl Guar Gum, Dextran, Kerat Sulfate, Locust Bean Gum, It may be one or more selected from succinoglucan, caronic acid, chitin, chitosan, carboxymethylchitin, agar, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, sodium polyacrylate, polyethylene glycol, bentonite, methylparaben, propylparaben, phenoxyethanol, 1,2-hexanediol, ethylhexylglycerin, etc.In addition, the above-mentioned oily additives are not limited to raw materials commonly used in the industry, and examples include liquid oils such as olive oil, camellia oil, jojoba oil, triglycerides, trioctoglycerin, and triisopalmitic acid glycerin; solid oils such as palm oil, hydrogenated palm oil, palm oil, hydrogenated oil, and hydrogenated castor oil; and beeswax, candelilla wax, carnauba wax, lanolin, and jojoba wax. Examples of hydrocarbon oils include liquid paraffin, squalene, petroleum jelly, and microcrystalline wax. Examples of higher fatty acids include waxes such as lauric acid, myristic acid, palmitic acid, stearic acid, and behenic acid; cetyl alcohol, stearyl alcohol, behenyl alcohol, myristyl alcohol, and cetostearyl alcohol; and synthetic ester oils include higher alcohols such as isopropyl myristate, cetyl octanoate, octyldodecyl myristate, isopropyl palmitate, hexyl laurate, myristyl myristate, cetyl lactate, isocetyl isostearate, neopentyl glycol dicaprate, ethylhexylglycerin, cetyl ethylhexanoate, ethylhexyl palmitate, and cetostearyl alcohol; chain-type silicone oils such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane; and cyclic silicone oils such as dodecamethylcyclohexasiloxane, octamethylcyclotetrasiloxane, and decamethylcyclopentasiloxane. It may be selected from the back, but is not limited to this.

[0061] It is obvious that a cosmetic composition according to one embodiment of the present disclosure can be prepared in the form of a general emulsion formulation and a solubilized formulation, etc., by using a commonly known manufacturing method in addition to the manufacturing method specifically disclosed in the present invention.

[0062] According to one embodiment, the cosmetic composition may be formulated as a softening lotion, an astringent lotion, a nourishing lotion, an eye cream, a nourishing cream, a massage cream, a cleansing cream, a cleansing foam, a cleansing water, a powder, an essence, or a pack.

[0063] The present disclosure provides a pharmaceutical composition for the prevention or treatment of dermatitis comprising a compound represented by the following chemical formula 1.

[0064] [Chemical Formula 1]

[0065]

[0066] (In the above chemical formula 1,

[0067] R1 is a straight-chain (C6-C20) alkyl, and

[0068] R2 is a straight-chain or branched-chain (C1-C10) alkyl, and

[0069] L1 is a (C1-C5)alkylene.

[0070] A pharmaceutical composition according to one embodiment of the present disclosure may include a pharmaceutically acceptable carrier according to a method that can be easily practiced by a person skilled in the art to which the invention pertains. The pharmaceutically acceptable carrier included in the pharmaceutical composition is one that is commonly used in formulations, such as lactose,

[0071] It may be dextrose, sucrose, sorbitol, mannitol, starch, acacia gum, calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, or mineral oil, but is not limited thereto.

[0072] The pharmaceutical composition for the prevention or treatment of dermatitis of the present disclosure may additionally include, in addition to the above components, a lubricant, a humectant, a sweetener, a flavoring agent, an emulsifier, a suspending agent, or a preservative.

[0073] The pharmaceutical composition for the prevention or treatment of dermatitis disclosed in this invention may be manufactured using commonly known manufacturing methods in addition to the manufacturing method specifically disclosed in this invention, and may be formulated into an appropriate form as intended. Specific examples thereof include, but are not limited to, forms such as lotions, ointments, gels, creams, patches, and sprays.

[0074] The pharmaceutical composition of the present disclosure for the prevention or treatment of dermatitis has an effect of improving inflammatory skin diseases caused by sebum secretion. In particular, the dermatitis may be seborrheic dermatitis or acne.

[0075] According to one embodiment, in a pharmaceutical composition for preventing or treating dermatitis of the present disclosure, R1 may be a straight-chain (C6-C10) alkyl, R2 may be a straight-chain (C1-C5) alkyl, and L1 may be a (C1-C5) alkylene.

[0076] According to one embodiment, a pharmaceutical composition for preventing or treating dermatitis of the present disclosure may comprise a compound represented by the following chemical formula 2.

[0077] [Chemical Formula 2]

[0078]

[0079] The above pharmaceutical composition may inhibit the expression of peroxisome proliferator-activated receptor (PPAR), and specifically, may inhibit the expression of PPAR-γ.

[0080] Hereinafter, the cosmetic composition for inhibiting sebum secretion according to the present invention will be described in more detail through specific examples. However, the following examples are merely for reference to explain the present invention in detail, and the present invention is not limited thereto and may be implemented in various forms. Furthermore, the terms used in the description of the present invention are intended merely to effectively describe specific examples and are not intended to limit the present invention.

[0081] [Example 1]

[0082] A composition (into H2O) containing 1.0 wt% of the N-(1-oxodecyl)serine methyl ester of the following chemical formula 2, prepared from registered patent publication KR10-2264354B1, was prepared.

[0083] [Chemical Formula 2]

[0084]

[0085] [Comparative Example 1]

[0086] A composition (into H2O) containing 1.0 wt% of the methyl(2-hexyl octanoyl) serinate of the following chemical formula 3, prepared from registered patent publication KR10-2323662B1, was prepared.

[0087] [Chemical Formula 3]

[0088]

[0089] [Evaluation Example 1] Evaluation of sebum secretion inhibitory efficacy

[0090] mRNA expression measurement

[0091] To measure the efficacy of inhibiting sebum secretion, sebum secretion was promoted in sebaceous gland cell lines (SZ-95) using Insulin-like Growth Factor-1 (IGF-1), and the mRNA expression levels of PPAR-γ were measured when treated with the above Example 1 and Comparative Example 1. Specifically, media containing IGF-1 was used to promote sebum secretion, and the compounds of Example 1 were treated at concentrations of 12.5 μM, 25 μM, and 50 μM, respectively, and the compounds of Comparative Example 1 were treated at a concentration of 50 μM for 24 hours.

[0092] Subsequently, the expression level of PPAR-γ was evaluated via qPCR, and the results are shown in Figure 1 below.

[0093] Nile red dye

[0094] Sebum secretion was promoted in sebaceous gland cell lines (SZ-95) using Insulin-like Growth Factor-1 (IGF-1), and the compounds of Example 1 were treated at concentrations of 12.5 μM, 25 μM, and 50 μM, respectively, and the compound of Comparative Example 1 was treated at a concentration of 50 μM for 24 hours. Subsequently, lipid expression was observed by Nile red staining, and the results are shown in Figure 2.

[0095] According to FIGS. 1 and 3, it can be seen that the expression of PPAR-γ in Example 1 was significantly reduced in a concentration-dependent manner compared to Comparative Example 1. Accordingly, it is believed that the compound included in Example 1 has excellent effects in inhibiting sebum secretion and dermatitis.

[0096] As described above, the present invention has been explained by specific details, limited embodiments, and comparative examples; however, these are provided merely to aid in a more comprehensive understanding of the invention, and the invention is not limited to the above embodiments. Those skilled in the art can make various modifications and variations from this description.

[0097] Accordingly, the scope of the present invention is not limited to the described embodiments, and all things equivalent to or having equivalent variations to the claims set forth below, as well as the claims set forth below, shall be considered to fall within the scope of the concept of the present invention.

Claims

1. A cosmetic composition for inhibiting sebum secretion comprising a compound represented by the following chemical formula 1. [Chemical Formula 1] (In the above chemical formula 1, R1 is a straight-chain (C6-C20) alkyl, and R2 is a straight-chain or branched-chain (C1-C10) alkyl, and L1 is a (C1-C5)alkylene.

2. In Paragraph 1, The above R1 is a straight-chain (C6-C10) alkyl, and The above R2 is a straight-chain (C1-C5) alkyl, and L1 is a (C1-C5)alkylene, a cosmetic composition for inhibiting sebum secretion.

3. In Paragraph 1, A cosmetic composition for inhibiting sebum secretion comprising a compound represented by the above chemical formula 2. [Chemical Formula 2] 4. In Paragraph 1, A cosmetic composition for inhibiting sebum secretion, comprising 0.001 to 1 weight% of a compound represented by Chemical Formula 1 with respect to the total composition.

5. In Paragraph 1, The above cosmetic composition is a cosmetic composition for inhibiting sebum secretion, which is formulated as a softening lotion, astringent lotion, nourishing lotion, eye cream, nourishing cream, massage cream, cleansing cream, cleansing foam, cleansing water, powder, essence, or pack.

6. A pharmaceutical composition for the prevention or treatment of dermatitis comprising a compound represented by the following chemical formula 1. [Chemical Formula 1] (In the above chemical formula 1, R1 is a straight-chain (C6-C20) alkyl, and R2 is a straight-chain or branched-chain (C1-C10) alkyl, and L1 is a (C1-C5)alkylene.

7. In Paragraph 6, The above R1 is a straight-chain (C6-C10) alkyl, and The above R2 is a straight-chain (C1-C5) alkyl, and L1 is a (C1-C5)alkylene, a pharmaceutical composition for the prevention or treatment of dermatitis.

8. In Paragraph 6, A pharmaceutical composition for the prevention or treatment of dermatitis comprising a compound represented by the following chemical formula 2. [Chemical Formula 2] 9. In Paragraph 6, A pharmaceutical composition for the prevention or treatment of dermatitis, wherein the dermatitis is acne or seborrheic dermatitis.

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