KR20140090794A - Composition for treating or preventing disease related to sebaceous gland comprising eggplant extract - Google Patents

Abstract

The present disclosure discloses compositions for preventing, alleviating, ameliorating, and / or treating sebaceous gland-related diseases, including eggplant extracts. The composition according to the present invention can be effectively used for prevention, improvement and / or treatment of sebaceous gland-related diseases due to various causes through inhibition of sebum secretion, inhibition of sebum cell proliferation and inhibition of acne bacteria, It has excellent stability without influence. Accordingly, the composition according to the present invention can be variously developed into a food, a pharmaceutical composition or a cosmetic composition effective for prevention, alleviation, improvement, or treatment of sebaceous gland-related diseases.

Description

[0001] The present invention relates to a composition for preventing or treating sebaceous gland-related diseases,

The present invention relates to a field of compositions that can be effectively used for the improvement, treatment or prevention of sebaceous gland-related diseases using natural substances.

In addition to economic development, there is a great increase in the demand for treating acne-related diseases, such as acne, in a social atmosphere that emphasizes appearance. Acne, which is a representative sebaceous gland-related disease, is a chronic disease that occurs in fur branch lines, which are characterized by lesions such as blackhead, whitehead, papule, and pustule that occur in areas where sebaceous glands such as face, Inflammatory disease. If not treated, it will leave a deep scar on the skin.

In addition to environmental factors, sebaceous gland secretion, pore and keratinization, and proliferation of hair follicles such as Propionibacterium acnes are known to be the main causes of acne, and therapeutic agents are being developed in this respect.

Currently, active ingredients used as acne remedies include erythromycin, isotretinoin, benzoyl peroxide, vitamin A, triclosan, and azelaic acid. Acne rosacea, an inflammation of the chronic sebaceous glands in the nose, forehead or the ball, also uses anti-inflammatory agents such as METROGEL®, NORITATE®, or metronidazole as therapeutic agents.

However, these drugs are known to have many problems such as the incidence of oral antibiotic resistant bacteria or recurrence at the time of discontinuation of treatment, as well as adverse effects such as hypofluorescence, dryness of the mucous membranes, spots or thrombosis.

Recently, natural materials have been developed for the development of acne remedies that have been effective even without these side effects.

U.S. Patent No. 7314634 discloses a polyphenol-based anti-wrinkle agent or an anti-acne agent for use in the treatment of skin diseases.

Korean Patent Laid-Open Publication No. 10-2007-0094340 discloses a composition for inhibiting sebum secretion, which comprises a white powder extract as an active ingredient.

However, the natural products are very diverse and have unlimited potential, and development of acne remedies through the development of new active ingredients in natural products is required.

And to develop a substance which is effective for preventing, alleviating, improving or treating sebaceous gland-related diseases derived from novel natural substances.

In one embodiment, the present invention provides a pharmaceutical composition for preventing, ameliorating, or treating sebaceous gland-related disease, including a branched extract. The composition according to the present invention has an effect of suppressing sebum secretion, alleviating skin keratopathy or inhibiting acne bacteria, and preventing, ameliorating, alleviating and / or treating sebaceous gland-related diseases such as acne, injection or seborrheic dermatitis . ≪ / RTI >

In one embodiment according to the present application, the compositions of the present application and the inhibitory effect acne bacteria, acne bacteria such for example propynyl sludge tumefaciens arc Ness (Propionibacterium acnes), Staphylococcus Aureus (Staphylococcus aureus), or Staphylococcus epi-der US Death (Staphylococcus It not necessarily contained a epidermidis) one which limits, in particular propionyl sludge, but can be generated by the arc tumefaciens Ness, and the like.

In one embodiment according to the present disclosure, the eggplant extract is extracted using an organic solvent, such as, but not limited to, Hexane or chloroform.

In another embodiment according to the present application, the extract may comprise from about 0.001% to 30% by weight of the total composition weight.

In another embodiment according to the present disclosure, the composition according to the invention is provided as a cosmetic composition, for example a cosmetic, and if necessary, the cosmetic composition comprises an unsaturated fatty acid comprising conjugated linoleic acid, linoleic acid, gamma- linoleic acid, alpha-linoleic acid, ≪ RTI ID = 0.0 > water-soluble < / RTI >

In another embodiment according to the present application, the composition according to the present invention may be provided as a health supplement, a functional food, or a food additive.

In another aspect, the present disclosure provides a cosmetic product comprising a branched extract or composition according to the present disclosure. Cosmetics may be manufactured in a variety of formulations including, but not limited to, for example, cleansers, lotions, lotions, creams or packs.

The composition comprising the eggplant extract according to the present invention can prevent, ameliorate, alleviate and / or prevent sebaceous gland-related diseases caused by various causes through inhibition of sebum secretion, inhibition of sebaceous cell proliferation and inhibition of acne bacterium, Or can be effectively used for treatment, and has excellent stability without affecting keratinocytes. Accordingly, the composition according to the present invention can be variously developed as a food, a pharmaceutical composition or a cosmetic composition which is effective for alleviating, improving, preventing and / or treating sebaceous gland-related diseases.

Fig. 1 shows the effect of SEB-1 and HaCaT cell death on the fraction of eggplant extracts. The vertical axis is expressed as a percentage of the negative control group.
Fig. 2 shows the effect of sub-fractions 8-1 to 8-5 of eggplant extract fraction 8 on SEB-1 and HaCaT cell death. The vertical axis is expressed as a percentage of the negative control group.
Figure 3 shows the effect of sub-fractions 8-1 to 8-5 of eggplant extract fraction 8 on P. acnes inhibition and keratinocyte growth. The vertical axis is expressed as a percentage of the negative control group.
Figure 4 shows the effect of sub-fractions 8-1 to 8-5 of eggplant extract fraction 8 on inflammatory cytokine, the production of inflammatory signaling substances.
Figure 5 shows the results of clinical experiments using the extract according to the present invention.

In one embodiment, the present invention relates to a composition for preventing, ameliorating or treating acne, comprising an eggplant extract.

As used herein, the term " Solanum & melongena ) is an annual or perennial plant belonging to the genus Gilberto. It grows in Korea and other tropical and temperate regions. Various varieties and subspecies can be included here. As used herein, a plant or a part thereof such as flesh, leaf, stem, seed and / or root containing physiological activity may be used.

The term " sebaceous gland-related disease " as used herein includes, but is not limited to, excessive sebum secretion due to activation of sebaceous glands and inflammation resulting therefrom such as, for example, acne, injection and seborrheic dermatitis. In one embodiment according to the present application, it is used in the prevention or treatment of acne.

The term "acne " as used herein encompasses all skin diseases commonly referred to in the art as acne, or all skin diseases that are invented through a mechanism similar to acne, such as collective acne, general acne, congoblate acne ), Cosmetic use acne, acne detergicans, teen acne, acne fulminans, acne furunculoid, acne by halogen, acne acne, keloid acne, physical stimuli Acne, acne, acne, acne, pomade acne, pre-menstrual acne, injections acne, acne, acne, acne, acne, acne, necrotizing acne, acne vulgaris acne rosacea, migratory acne, tropical acne, addictive

But are not limited to, acne venenata, adult acne, or acne vulgaris.

As used herein, the term "injection " is a chronic disease with major symptoms such as papules, pustules, edema, and the like, which are accompanied by erythema on the middle part of the face such as the nose and cheeks (Meyer-Hoffert U et al., J Investig Dermatol Symp Proc Dec. 15 (1): 16-23).

As used herein, the term " seborrheic dermatitis "refers to an inflammatory disease that occurs in a skin having a high fat content and develops in the skin, nose, eyebrows and chest. The skin is reddish and covered with a yellowish, It is a dermatitis accompanied by erythema and thin scar.

The compositions according to the present application has the acne bacteria inhibiting effect, these acne bacteria, for example, propynyl sludge tumefaciens arc Ness (Propionibacterium acnes ), Staphylococcus Aureus (Staphylococcus aureus ), or Staphylococcus Epi der mide switch is included a (Staphylococcus epidermidis) one which limit is not particularly program ropi sludge, but can be generated by tumefaciens arc Ness, not limited to this, the effect on the composition of the present application due to these various causative diseases .

The branched extract of the present invention is effective for the improvement, prevention, or treatment of acne as described above. The term " treatment ", "alleviating " or " improvement ", as used herein, refers to any act that improves or alleviates the symptoms of sebaceous gland-related diseases by administration of the extract or composition comprising it. If you are a normal person, you can refer to the data provided by the Korean Medical Association, etc. to know the exact criteria of the disease, and to judge the degree of improvement, improvement and treatment.

The term "prophylactic, " as used herein, refers to any act that inhibits or delays the onset of acne or related disease by administration of the extract or composition comprising it. It will be apparent to those skilled in the art that the extract of the present invention can prevent the early symptoms of acne, or that these diseases can be prevented when administered prior to appearance.

The branched extracts of the present disclosure can be prepared using conventional methods known in the art, that is, using conventional solvents under ordinary temperature and pressure conditions. Examples of the extraction solvent that can be used in the production of the egg plant extract of the present invention include water, C1 to C3 lower alcohol, acetone, ethyl acetate, butyl acetate and 1,3-butylene glycol, chloroform, Solvents may be used alone or in combination. A suitable amount of the extraction solvent is about 1 to 15 times the weight of the branch, may be 5 to 12 times, and may be 10 times, but is not limited thereto. As the extraction method, it is possible to use heat extraction, cold extraction, reflux cooling extraction, ultrasonic extraction and the like, and they can be extracted once or repeatedly. The extraction temperature is not particularly limited so long as the effective activity of the useful component of the branch is not removed, but is preferably extracted by immersion at room temperature.

The eggplant extract of the present invention has antimicrobial activity against sebum secretion, diseases and acne causative bacteria, and is effective for treating acne due to various causes.

The term "extract " as used herein means an active ingredient isolated from a natural product, that is, a substance exhibiting the desired activity. The extract can be obtained by an extraction process using water, an organic solvent, or a mixed solvent thereof, and includes all the forms that are formulated with the dry powder of the extract. In addition, the above-mentioned extract also includes fractions obtained by fractionating the extract obtained through the above extraction process.

The extract can be prepared by a known method. For example, by hot water extraction or using an appropriate organic solvent such as methanol, ethanol or the like as an extraction solvent according to a known method (Nomura T. Phenolic compounds of the mulberry tree and related plants. Progress in the Chemistry of Organic Natural Products (Herz W, Grisebach H, Kirby GW, Tamm Ch, eds.), 53. Springe: Vienna, 1988, 87-201.)

The solvent may be water, an organic solvent or a mixture thereof. Specific examples of the solvent include water, a polar solvent such as lower alcohol having 1 to 5 carbon atoms, such as ethanol, butanol, propanol and isopropanol, such as ethyl acetate, and a nonpolar solvent such as hexane or dichloromethane Organic solvents or mixtures thereof.

The extract of the present invention can be produced by using a common general production method of a conventional plant extract, and is not particularly limited. For example, it may be an ultrasonic extraction method, a reflux cooling extraction method, a hot water extraction method, or a method in which the above solvent is used as an extraction solvent by a known method (see, for example, Nomura T, 1988, etc.). Further, the extracted extract can be further fractionated with a solvent selected from the group consisting of hexane, methylene chloride, acetone, ethyl acetate, chloroform, and mixtures thereof. Two or more kinds of solvents may be used in the fractionation step, or they may be used individually or in combination. Depending on the polarity of the solvent, an extract of each solvent may be sequentially used. The extract preparation temperature may be 4 to 120 ° C, but is not limited thereto. The extraction time is not particularly limited, but may be 10 minutes to 30 days, and conventional extraction equipment, ultrasonic pulverization extractor or fractionation unit may be used. The produced extract can then be subjected to vacuum filtration and / or lyophilization to remove the solvent.

For example, about 10 to 15 g of the concentrate obtained by concentrating the ethanol extract obtained by adding about 0.5 to 5 L of ethanol per 100 g of ash is suspended in about 100 to 1000 mL of water, 100 to 1000 mL of hexane is added, A hexane fraction extract is obtained. After removing the hexane fraction extract, 100-1000 ml of methylene chloride is added to the remaining water layer, followed by extraction to obtain a methylene chloride fraction extract. After the methylene chloride fraction extract is removed, 100 to 1000 ml of ethyl acetate is added to the remaining water layer, and extraction is performed to obtain an ethyl acetate fraction extract. After removal of the ethyl acetate fraction extract, 100 to 1000 ml of butanol is further added to the remaining water layer, and then extracted to obtain a butanol fraction extract. At this time, a water layer excluding the butanol fraction extract is obtained as a water extract have. When extracting with hexane, methylene chloride, ethyl acetate, or butanol, the extraction temperature may be 20 to 40 ° C, but is not limited thereto. The extraction time is not limited, but may be 30 minutes to 20 hours. An ultrasonic wave pulverizing extractor may be used. The produced extract is then subjected to vacuum filtration and freeze-drying to remove the solvent. In addition, it may further comprise a separation process by various chromatographies (chromatography based on size, charge, hydrophobicity or hydrophilicity). In the present invention, the drying process may be performed by a method including, but not limited to, freeze drying, vacuum drying, hot air drying, spray drying, vacuum drying, foam drying, high frequency drying or infrared drying.

The composition comprising the eggplant extract according to the present invention can be used as a cosmetic composition for improving sebaceous gland-related diseases such as acne, injection and seborrheic dermatitis, and as a cosmetic composition, especially a cosmetic composition for treating, improving, alleviating or preventing acne. At this time, the composition can be applied to the area where the sebaceous glands are developed, but it is not particularly limited, and it is preferable to apply various administration routes such as face, scalp or back region having a great sebum secretion, for example, , Orally, transdermally, or by injection, in particular by the transdermal route.

In one embodiment, the present invention discloses a cosmetic composition for prevention, improvement or treatment of acne, which comprises eggplant extract. The content of the extract may vary depending on the specific use or formulation of the desired product, About 50% by weight, about 1% by weight to 30% by weight, and 5% by weight to 30% by weight, or 5% by weight to 25% by weight.

The cosmetic composition comprising the extract of the present invention may contain, in addition to the above extracts, conventional auxiliaries and carriers such as antioxidants, stabilizers, solubilizers, vitamins, pigments and / or flavors.

The cosmetic composition of the present invention may comprise a water-soluble base material comprising an unsaturated fatty acid or propylene glycol including conjugated linoleic acid, linoleic acid, gamma-linoleic acid, alpha-linoleic acid.

In addition, the cosmetic composition of the present invention may be prepared in any form conventionally produced in the art, and examples thereof include a solution, a suspension, an emulsion, a paste, a gel, a cream, a lotion, a powder, a soap, But are not limited to, cleansing, oil, powder foundation, emulsion foundation, wax foundation, and spray. More specifically, it can be prepared in the form of a flexible lotion, a nutritional lotion, a nutritional cream, a massage cream, an essence, an eye cream, a hair tonic, a shampoo, a rinse, a cleansing cream, a cleansing foam, a cleansing water, a pack, a spray or a powder .

When the composition of the present invention is a paste, cream or gel, an animal oil, a vegetable oil, a wax, a paraffin, a starch, a tracer, a cellulose derivative, polyethylene glycol, silicon, bentonite, silica, talc or zinc oxide may be used as a carrier component .

When the composition of the present composition is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. In particular, in the case of a spray, a mixture of chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

When the formulation of the composition is a solution or an emulsion, a solvent, a solubilizing agent or an emulsifying agent is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, , 3-butyl glycol, glycerol aliphatic ester, polyethylene glycol or fatty acid esters of sorbitan can be used.

When the formulation of the present composition is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspension such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.

When the formulation of the composition of the present invention is an interface-active agent-containing cleansing, the carrier component is selected from the group consisting of aliphatic alcohol sulfates, aliphatic alcohol ether sulfates, sulfosuccinic acid monoesters, isethionates, imidazolium derivatives, methyltaurates, sarcosinates, fatty acid amide ethers A fatty acid glyceride, a fatty acid diethanolamide, a vegetable oil, a lanolin derivative, or an ethoxylated glycerol fatty acid ester, etc. According to a preferred administration type, the composition of the present invention contains at least one Of a pharmaceutically acceptable excipient, especially a dermatologically acceptable excipient.

Further, in the composition for dermatological preparation of each of the formulations, components other than the above-mentioned essential components may be selected and mixed without difficulty by those skilled in the art depending on other compositions for dermal use or the purpose of use.

The composition according to the invention may also comprise at least one adjuvant selected from the group of pharmaceutical adjuvants known to the person skilled in the art, thickeners, preservatives, flavors, coloring agents, chemical or mineral salts filters, moisturizers, hot spring water and the like. Preservatives commonly used in cosmetics or functional foods are, for example, molecules having antimicrobial activity, such as capryl derivatives (capryloylglycine and glyceryl caprylate), such as hexanediol and sodium levorinate, zinc And copper derivatives (gluconate and PCA), phytosphingosine and derivatives thereof, benzoyl peroxide, pyrrothonol amine, zinc pyrocite and selenium sulfide, econazole, ketoconazole or topical antibiotics such as erythromycin and Clindamycin can be called.

The composition of the present invention may also contain, if necessary, other ingredients such as an anti-inflammatory agent, an antimicrobial agent, an antifungal agent, a keratolytic agent, an exfoliation regulator, an astringent, an anti-inflammatory / anti- irritant, an antioxidant / free radical capturing agent, / RTI > and / or at least one anti-acne compound selected from moisturizers.

Fatty regulators that can be used in the compositions herein include, for example, 5-alpha-reductase inhibitors, zinc and its gluconate, salicylate and pyroglutamic acid, spironolactone, anti-androgens and aldosterone antagonists. Antibacterial or antifungal agents herein are substances that limit the growth of pathogenic microorganisms such as acne bacteria such as P. acnes . The exfoliating regulators and keratolytic agents are used herein as agents for removing the dead horny layer, for example, alpha-hydroxy acids (AHA) (citric acid, glycolic acid, maleic acid, lactic acid, etc.), AHA esters, AHA and other molecules For example, a combination of malate and almond proteins (Keratolite), a combination of glycolic acid or arginine of lactic acid or a combination of hydroxy acid and lipid molecules such as LHA (lipo-hydroxy acid), amphoteric hydroxy acid (AHCare), salicylic acid and derivatives thereof such as a combination of capryloylsalicylic acid or other molecules such as salicylic acid and a polysaccharide (beta-hydroxy acid, or BHA), tazarotene, adapalene, retinoids Family molecules, such as tretinoin, retinaldehyde, isotretinoin, and retinol. As the astringent agent of the present application, polyphenol and zinc derivatives are generally used as a substance that helps pores contraction.

Anti-inflammatory / anti-irritant agents of the present application are intended to mean those agents which limit the inflammatory response and have sedative and anti-irritant properties such as glycyrrhetinic acid (licorice derivatives) and its salts and esters, alpha-bisabolol, Ginkgo biloba extract, marigold extract, lipoic acid, beta-carotene, vitamin B3 (niacinamide, nicotinamide), vitamin E, vitamin C, vitamin B12, flavonoid (green tea, quercetin, etc.), lycopene or lutein, avocado sugar, Such as, for example, carnosine, N-acetyl-cysteine, isoflavones or other anti-inflammatory agents such as distillate, arabinogalactan, lupine peptides, lupine total extract, quinoa peptide extract, Cycloceramide (oxazoline derivatives) It contains drugs.

Antioxidants are substances which reduce or prevent the oxidation of other chemicals, for example thiol and phenol, licorice derivatives such as glycyrrhetinic acid and its salts and esters, alpha-bisabolol, ginkgo extract, marigold extract , Vitamin C 3 (niacinamide, nicotinamide), vitamin C, vitamin E, coenzyme Q10, and the like can be given as examples of the antioxidants, antioxidants, antioxidants, antioxidants, have.

The moisturizing / emollient agents herein include, but are not limited to, commonly used glycerin or derivatives thereof, urea, pyrrolidone carboxylic acid and derivatives thereof, hyaluronic acid having any molecular weight, glycosaminoglycans and other various water and terrestrial plant sources Polysaccharides such as xanthan gum, fucogel, fatty acids such as lauric acid, myristic acid, monounsaturated and polyunsaturated omega-3, -6, -7 and -9 fatty acids (linoleic acid and palmitoleic acid) Oleodistillate, avocado peptide, and cupuacu butter.

Furthermore, the composition of the present invention can be used in a variety of health supplement foods, functional foods, food additives and the like for prevention and improvement of sebaceous gland-related diseases, for example, acne. Examples of foods to which the composition of the present invention can be added include various foods, beverages, gums, tea, vitamin complexes, health supplements and the like, and they can be used in the form of powders, granules, tablets, have.

Since the composition of the present invention has little toxicity and side effects, it can be safely used even for long-term administration for preventive purposes.

In one embodiment, the composition of the present invention may be added to a food or beverage for the purpose of preventing and improving sebaceous gland-related diseases, such as acne. At this time, the amount of the composition in the food or beverage is generally 0.01 to 15% by weight of the total food weight of the health food composition of the present invention, and the health beverage composition is 0.02 to 30 g based on 100 ml, May be added at a ratio of 0.3 to 10 g, but is not limited thereto.

In addition to the above-mentioned composition, the composition of the present invention can be used as a flavoring agent such as various nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, coloring agents and intermediates (cheese, chocolate etc.), pectic acid and its salts, Salts, organic acids, protective colloid thickening agents, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated beverages and the like. In addition, the compositions of the present invention may contain flesh for the production of natural fruit juices and fruit juice drinks and vegetable drinks. These components may be used independently or in combination. The ratio of such additives is generally selected from the range of 0 to about 20 parts by weight per 100 parts by weight of the composition of the present invention, but is not limited thereto.

Hereinafter, embodiments are provided to facilitate understanding of the present invention. However, the following examples are provided only for the purpose of easier understanding of the present invention, and the present invention is not limited to the following examples.

Example  Production of one extract

The outbreds were purchased from the Korea Plant Extract Bank and extracted with chloroform and hexane and separated by chromatography. Specifically, 3 g (1 g x 3) of the outpouring powder was dissolved by shaking in 750 ml of hexane (250 ml × 3), transferred to a separating funnel, 750 ml (250 ml × 3) of water was added thereto and mixed , And allowed to separate into a water layer (light green) and an organic layer (dark green). Then 750 ml of 1N HCl (250 ml × 3) was slowly added to the separated organic layer and then separated into a water layer (light green) and an organic layer (dark blue green) using a separating funnel. The hexane organic layer thus separated was dried under reduced pressure using a rotary evaporator at a temperature of less than 25 ° C, filtered through a suction flask, and filtered to obtain a total of 379 mg of egg planted extract.

Then 379 mg of the extract was dissolved in 10 ml of hexane and subjected to semi-preparative HPLC (Dionex, USA). The conditions are as follows: Particle size 10 μm, flow rate 21 ml / min, temperature 25 ° C. Solvent Gradient Solvent A = acetonitrile, solvent B = water (third distilled water) A: 235 nm, collecting channel B: 293 nm). Eight kinds of branched organic acid hexane acid fractions were obtained in this manner. After confirming that 8 of these effectively reduced sebum cells, they were again fractionated as follows. That is, 30 mg of sample No. 8 in hexane acid was dissolved in 10 ml of hexane and then separated under the following conditions. Solvent A = acetonitrile, solvent B = water (third distilled water), detection method: UV detector (collecting channel A: 235 nm, collecting) Channel B: 293 nm). After separating the peaks appearing in the detailed chromatogram of the collecting channel 1, they were dried under reduced pressure using a rotary evaporator at a temperature of less than 25 ° C., and the remaining water was removed by using a pump and nitrogen. 5 was obtained.

Hexane-acidic-8-1: 7 mg (light yellow, not visible during drying).

Hexane-acidic-8-2: 7 mg (light green)

Hexane-acidic-8-3: 2 mg (green)

Hexane-acidic-8-4: 3 mg (green, not visible during drying)

Hexane-acidic-8-5: 7 mg (dark green green)

Example  Effect of two extracts on acne

Example  2-1 Sebaceous glands  Cell proliferation inhibition and safety experiment

The effect of the extract of Example 1 on acne was determined as follows.

First, for cell experiments, SEB-1 (human sebocyte (SEB-1)) (Thiboutot D, et al., J Invest Dermatology 2003; 120: 905-914) and keratinocyte cell line HaCaT SEP-1 cells were treated with 2.5% fetal bovine serum, 1.8 x 10 ^-4 M adenine, 0.4 μg / ml hydrocortisone, 10 ng / ml insulin and epidermal growth factor (EGF, epidermal The cells were cultured in DMEM (5.5 mM glucose) / F-12 3: 1 medium containing 3 ng / ml growth factor and 1.2 × 10 ^-10 M cholera toxin at 37 ° C and 5% CO ₂ . HaCaT was cultured in DMEM medium containing 10% FBS.

Cell viability tests using SEB-1 and HaCaT were performed to identify fractions and concentrations that effectively reduce SEB-1 without affecting HaCaT survival.

For cell viability testing, SEB-1 and HaCaT cells were added to each well of a 96-well plate at a concentration of ¹ x 10 ⁴ cells and 5 x 10 ³ cells, respectively. After 24 hours, the fractions 1 to 8 and 8-1 to 5 of Example 1 and the remnants after preparation were treated in the amounts of 1, 5, 50 and 100 μg, respectively, and the control group was not treated. After culturing for 24 hours, 48 hours, or 72 hours, 10 μl of MTT (3- (4,5-Dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide, Sigma) After incubation for 1 h, live cells were measured using a plate reader at 570 nm. Live cells degrade MTT by succinate dehydrogenase in mitochondria to form MTT formazan.

The results are described in Figures 1a, 1b, and 2a, b. No effect on SEB-1 cells and HaCaT cells was observed in the fractions 1 to 6, and the cell survival rate of substance 7 was not significantly different according to the concentration. In the fraction No. 8, the cell survival rate was found to differ by the concentration. Based on this, five fractions (hexane-acidic-8-1, hexane-acidic-8-2, hexane-acidic-8-3, hexane-acidic- 8-4, hexane-acidic-8-5), the growth of SEB-1 was suppressed at a relatively low concentration in the four fractions except hexane-acidic-8-1, HaCaT survival was not affected. This indicates that the branched extract fractions 8-2 to 8-5 have a therapeutic effect on acne without adverse effects on keratinocytes.

Example  2-2 P. acnes   Suppression and effects on keratinocytes

Acne Gain Propionibacterium The minimum amount of candidate substance concentration (MIC) required to inhibit or kill the growth of acnes was determined. The MIC assay was performed with some modification of the broth dilution using a 96 well plate. In summary, P. acnes (KCTC3314) was cultivated in anaerobic condition on reinforced clostridial broth (Merck, Germany) for 3 days and the absorbance was adjusted to a value of McFarland 0.5 (1.5 × 10 ⁸ cells / ml) at 620 nm . Subsequently, the bacteria were serially diluted in duplicate (two fold serial dilution), and 100 μl was added to each well of a 96-well plate and 10 μl of the strain was inoculated. As a control, DMSO in which the extract was dissolved was used. After incubation at 37 ° C for 72 hours in the anaerobic chamber, the minimum concentration of inhibiting P. acnes was determined by observing the bacterial growth (turbidity of culture medium) at 620 nm absorbance. Erythromycin antibiotics were used as a positive control and no treatment with P. acnes as a negative control.

The results are shown in Figures 3a and 3b. As shown, eggplant extracts No. 2 to 4 and fraction 8 were respectively as follows: prep 8-2: 250 μg, prep 8-3: 500 μg, prep 8-4: 500 μg, Something: 500 μg. These results indicate that P. acnes (KCTC3314), or exhibit bactericidal effects.

Example  2-3 anti inflammatory effect

To determine whether the extract could reduce the secretion of inflammatory cytokines, that is, inflammatory signaling substances. RT-PCR is a laboratory technique for studying the changes in RNA before protein expression. Treatment of acne usually results in inflammation, which produces many substances that respond to inflammation in the sebaceous glands, which are measured at the RNA level.

SEB-1 cells were cultured for 48 h in SEB-1 medium containing 2.5% fetal bovine serum in a 60 mm cell culture dish at a density of 1.5 × 10 ⁴ cells. After that, P. acnes (KCTC3314) Fractions 1 to 5 and residuals were treated with bacteria, and after 3 h and 6 h, the medium was removed, and 1 ml of Trizol was added and RNA was extracted from the SEB-1 cells to perform reverse transcription PCR. The primers for RT-PCR are as follows: GAPDH primer Forward 5'-CAAGGTCATCCATGACAACTTTG-3 '; Reverse 5'-GTCCACCACCCTGTTGCTGTAG-3 '; IL-8 primer Foward 5'-GCCAACACAGAAATTATTGTAAAGCTT-3 '; Reverse 5-AATTCTCAGCCCTCTTCAAAACTT-3'; IL-6 primer Forward 5'-ATGGCTGAAAAAGATGGATGCT-3 '; Reverse 5'-GCTCTGGCTTGTTCCTCACTACTC-3 '; TNF-α primer Forward 5'-GAAGACCTCACCTAGAAATT-3 '; Reverse 5'-AGGGCGATTACAGACACAAC -3 '.

The reaction conditions of IL-6 and IL-8 were 5 min at 95 ° C, 30 sec at 94 ° C, 30 min at 58 ° C, For 30 seconds at 72 ° C, and reacted at 72 ° C for 5 minutes. Then, 29 cycles of 95 ° C for 5 minutes, 94 ° C for 30 seconds, 61.5 ° C for 30 seconds, and 72 ° C for 30 seconds were amplified and reacted at 72 ° C for 5 minutes. Then, using 1.5% agarose gel Chain reaction products were observed at 143 bp for IL-6, 131 bp for IL-8 and 430 bp for TNF-α

The results are shown in Figures 4a and b. As described, prep1 and 5 of eggplant extract fraction 8 decreased mRNA expression compared to SEB-1 + P. acnes (control) in TN8- and TNF-α in IL8 and prep5 , (IL-8, IL-6, TNF-α), which is an anti-inflammatory effect of the extract of the present invention.

Example  2-4 Clinical Trials

Clinical trials were conducted to confirm that the extracts of this invention are applicable to human beings and that they are effective against acne. Twenty-three patients with acne were randomly selected. The composition (experimental drug) containing the plant extracts of Example 1 was applied twice a day to half of randomly selected faces using the split-face method and the other half was treated with propylene glycol - Control drug) was applied and the follow - up was performed. The double eyelid method was applied using a random number table so that neither the patient nor the evaluator would be able to know which one was applying the test drug. The efficacy was evaluated before application and at 2, 4, 6, and 8 weeks after application for 8 weeks. The efficacy was assessed by a subjective assessment of the patient (VAS) and an objective assessment of two dermatologists. Objective assessments were performed to assess changes in the number of acne lesions and the overall Revised Leeds acne severity grading (SC O'Brien, JB Lewis, WJ Cunliffe, The Leeds revised acne grading system, J Dermatol Treat (1998) In the case of acne lesions, the numbers of various types of acne lesions, such as comedone, papule, pustule, nodule, were measured periodically before and after application. In the later statistical analysis, non - inflammatory lesions, papules and pustules, and nodules were classified into inflammatory lesions. In addition, sebum secretion was quantitatively measured using a sebumeter (Skin-O-Mat, Choyang medics, Seongnam, Korea). Statistical analysis was performed with SPSS 17.0 ver. Were used.

The mean Leeds grade of the experimental group was 2.52, 2.04, 1.79, and 1.43 at 0, 2, 4, and 8 weeks, respectively, and 2.52, 2.27, 2.06, and 1.95, respectively. The mean number of noninflammatory lesions was 38.58, 30.88, 24.83, 15 at the experimental drug sites, 37.21, 33.92, 27.71 and 21.71 at the control site at 0, 2, 4 and 8 weeks, 2.88, 1.38, 2, 1.17 at the experimental drug site and 2.71, 1.92, 2.25 and 2.13 at the control drug site at 8 weeks, respectively. In VAS, which quantified the subjective evaluation of patients, 10, 8, 6.96, and 5.48 were evaluated at 0, 2, 4, and 8 weeks, and 10, 8.83, 8.38, and 6.6 at the reference drug sites. The amount of sebum secretion was measured as 79.38, 85.25, 75.13, 81.57, and 91.13, 99.17, 89.33, and 102.17, respectively, on the experimental drug site at time 0, 2, 4 and 8 5e).

Statistical analysis was performed to determine whether the variables were significant at 0, 2, 4, and 8 weeks in the experimental drug application and the reference drug application. The results are shown in Figures 5A through 5E.

Inflammatory lesions did not show a significant improvement in the right side of the control compared to before treatment, whereas the lesion on the experimental drug showed significant improvement in lesion at 2, 4 and 8 weeks. Compared with the experimental drug and the reference drug, the inflammatory lesions did not show a significant difference at 2 and 4 weeks, but they showed significant differences at 8 weeks. (*; p &lt; 0.05, **; p < 0.005) (see Fig. Among the various variables measured, Leeds grade was significantly different at 2, 4, and 8 weeks when the experimental drug and the reference drug were compared. (*; p < 0.05) (see FIG. 5B). Non-inflammatory lesions were significantly different in both sides at 2, 4, and 8 weeks when the experimental drug and the reference drug were compared. (*; p <0.05, **; p <0.005) (see FIG. In addition to objective objective lesion assessment, the patient's subjective assessment of VAS showed significant differences between the experimental drug portion and the reference drug portion at 4 and 8 weeks (see FIG. 5d).

The results of the above analysis show that the efficacy of the experimental drug and the comparator was analyzed at each time point, and the experimental drug was more effective than the control drug in reducing the number of noninflammatory lesions at 2, 4, and 8 weeks In the week, it was also statistically significant in reducing inflammatory lesions. In addition to these effects, none of the 23 clinical investigators completed the 8-week follow-up, and none of the 26 patients who initiated the first clinical trial were able to demonstrate the tolerability of the test drug after completion of the clinical trial .

While the present invention has been described in connection with what is presently considered to be the preferred embodiments, it is to be understood that the invention is not limited to the disclosed embodiments, but, on the contrary, .

All technical terms used in the present invention are used in the sense that they are generally understood by those of ordinary skill in the relevant field of the present invention unless otherwise defined. The contents of all publications referred to herein are incorporated herein by reference.

Claims (11)

A pharmaceutical composition for preventing, ameliorating, or treating sebaceous gland-related diseases, comprising a plant extract.
The pharmaceutical composition according to claim 1, wherein the composition has an effect of inhibiting sebum secretion, alleviating skin keratoses, or inhibiting acne bacteria.
The pharmaceutical composition according to claim 1, wherein the sebaceous gland-related disease is acne, injection or seborrheic dermatitis.
The pharmaceutical composition according to claim 1, wherein the eggplant extract is an organic solvent extract.
5. The pharmaceutical composition according to claim 4, wherein the organic solvent is Hexane or chloroform.
The pharmaceutical composition of claim 1, wherein the composition is included in the range of 0.001% to 30% by weight.
The pharmaceutical composition according to claim 1, wherein the composition is provided for cosmetic use.
8. The pharmaceutical composition according to claim 7, wherein the cosmetic composition comprises a water-soluble base material comprising an unsaturated fatty acid or propylene glycol including conjugated linoleic acid, linoleic acid, gamma-linoleic acid, alpha-linoleic acid.
The pharmaceutical composition according to claim 1, wherein the composition is provided as a health supplement, a functional food, or a food additive for improving or alleviating the symptoms of sebaceous gland-related diseases.
A cosmetic comprising the composition according to claim 1.
11. The cosmetic composition according to claim 10, wherein the cosmetic is a cleanser, a lotion, a lotion, a cream or a pack, a cosmetic.

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