KR20090105320A - Composition for prevention or treatment of Acne - Google Patents

Abstract

PURPOSE: A composition for preventing or treating acne is provided to ensure effective anti-bacterial and anti-inflammatory effects and relieve inflammation of skin tissue. CONSTITUTION: A composition for preventing or treating acne contains extract of Mollugo pentaphylla, Angelica anomala, Matteuccia orientalis, Orixa japonica and their mixture. The composition has anti-bacterial activity to Propionibacterium acnes and Staphylococcus epidermidis. The composition has the function of suppressing IL-8 and TNF-α secretion.

Description

Composition for prevention or treatment of Acne

The present invention is directed to a composition for preventing or treating acne containing an extract selected from the group consisting of pomegranate grass, pomegranate, open horse, normal acid and mixtures thereof, a method for preparing the same, and a cosmetic and preparation for preventing or treating acne containing the composition. It is about.

Acne generally refers to chronic inflammatory diseases of the hair follicle sebaceous glands characterized by the formation of comedones, papules, pustules, cysts or nodules that occur mainly in men and women of puberty. Acne appears in the most visible areas of the skin, especially the face, chest, back and upper arms, and if the skin damage caused by acne is severe, this may cause mental damage, such as depression or avoiding interpersonal relationships. The cause of acne is still unclear, but it is recognized by three factors that exclude genetic and environmental factors.

First, the sebum is abnormally oversecreted. Excess sebum secretion is closely related to the testosterone testosterone, which is converted to dihydrotestosterone (DHT) by 5 alpha-reductase in skin cells, It is known to promote sebum secretion by enhancing activity (Rosenfield RL et al., The American Journal of Medicine, 16, pp 80-88, 1995).

Second, the wall of the follicles is exaggerated and the pores are closed. The generated sebum should be smoothly discharged out of the skin, but when the pores are blocked due to the exaggeration of the hair follicles, the smooth discharge of the sebum is suppressed, so the sebum is stagnated in the hair follicles to form microsurfaces. This condition is the early stage of acne outbreaks.

Third, stagnant sebum in hair follicles exacerbates acne lesions by promoting the growth of propionibacterium acnes, an anaerobic bacterium that resides in hair follicles. As acne bacteria grow in the sebaceous glands, triglycerides that make up sebum are converted into free fatty acids to act as irritants or act as a comedonogenic substance to produce acne. This is accompanied by an inflammatory response (Sergio Nacht, Cosmetics Toiletries, 101, pp 47-55,1986).

In addition, various microorganisms exist in human skin. These microorganisms cause various skin diseases. Staphylococcus aureus, which causes purulent skin, also includes Staphylococcus epidermis, a bacterium that decomposes sebum and sweat secreted on the skin along with acne bacteria (Propionibacterium acnes). Odors, and decomposition products irritate and irritate the skin.

The inflammatory response is that arachidonic acid, a component of phospholipids in the skin's endothelium, is separated from cell membranes by phospholipase (PL) A2, which is a cyclooxygenase. , COX) acts as a prostaglandin (PG) E2, which plays an important role in the inflammatory response. In addition, PLA 2 is activated by free radicals (Lehinger, A. et al., Principles of Biochemistry.second ed.Worth Publisher.pp 229-235, 1993), and propionibacterium acnes produces leukocytes. Free radicals are produced (Webster, GF et al., Inflammation, 1980). COX includes COX-1 and COX-2, COX-1 is a constitutive enzyme, and COX-2 is an inducing enzyme that is induced during inflammation (Crofford, LJ, J. Rheumatol., Suppl 49, 24, pp 5-19, 1997). As described above, the inflammatory response through the arachidonic acid and the COX-2 reaction is the main reaction of acne and dermatitis.

Acne is thus regarded as a disease caused by multiple factors leading to overproduction of sebum, hyperkeratosis of pores and action of propionibacterium acnes, and induction of inflammation.

To date, methods for treating or alleviating acne include the use of female hormones, such as anti-androgens, which control the release of abnormal testosterone to suppress sebaceous hypersecretion, the use of antibacterial and antibiotics that inhibit the growth of acne bacteria, and anti-inflammatory A method of using a nonsteroidal anti-inflammatory agent that acts has been used. Recently, a method of inhibiting sebum hypersecretion using an alpha-reductase inhibitor has been proposed.

However, the use of female hormones is a side effect during the treatment of acne, and there is a high possibility of skin inflammation, and there have been many reports of side effects caused by long-term administration of female hormones. It is also reported that the anase inhibitor is also ineffective. In addition, typical antibacterial agents against acne bacteria include resorcinol, sulfur, benzoyl peroxide, tetracycline, erythromycin or methacycline. There are several problems in terms of this. For example, retinoic acid and benzoyl peroxide, which are antimicrobial agents, are highly susceptible to skin irritation and contact dermatitis, and antibiotics containing tetracycline have been reported to have side effects due to the appearance of resistant bacteria and photosensitive effects. In addition, salicylic acid and vitamin A derivatives, such as retinoic acid, are used to suppress the formation of keratin in the pores or to remove the pores to facilitate the release of acne, but salicylic acid has only a minimal therapeutic effect. Not only can cause skin redness, swelling or skin respiratory tract, retinoic acid and the like has an effect through inhibiting hyperkeratosis, but contact dermatitis, erythema, dry skin and peeling phenomenon may occur. On the other hand, the relatively recently introduced azelaic acid (azelaic acid) preparations have reduced side effects of the drug, but the therapeutic effect is lower than that of the existing therapeutic products.

In order to reduce side effects of hormones or compound preparations used in the past, researches on natural product preparations have recently been conducted.

Formulations composed of natural products are known to have fewer side effects, generally have a mild and continuous action, and in some cases, poorly soluble components become usable ingredients and are highly biodegradable and environmentally friendly. Examples of such natural product formulations include Korean Patent No. 467,031, Korean Patent No. 491,746, and Korean Laid-Open Patent No. 1999-0025848, and the compositions include boiled red barley, red peony, Kang Bok, Gardenia jasminoides, jangil root extract, benzoyl per Oxide, retinoic acid, β-glyciretinic acid, 2- [2- (3-heptyl-4-methyl-2-thiazoline-2-iridine) methane] -3-heptyl-4-methyl thiazolinium Although a cosmetic composition containing iodide (photosensitive dye), salicylic acid and the like as an active ingredient is disclosed, it does not provide a satisfactory effect on acne improvement and causes irritation to the skin.

Therefore, the inventors of the present invention, while searching for a substance having antibacterial and anti-inflammatory effects, which are essential items of acne treatments derived from natural substances, which are harmless to the human body, the pomegranate grass, pore stalk, open horse or normal acid extract of the present invention improves acne skin. Confirmed that the effect is to complete the present invention.

An object of the present invention relates to a composition for preventing or treating acne, and a method for producing the same, comprising an extract selected from the group consisting of pomegranate grass, pomegranate, open horse, normal acid and mixtures thereof.

Another object of the present invention relates to cosmetics and preparations for preventing or treating acne containing the composition.

In one embodiment the present invention is to provide a composition for the prevention or treatment of acne, containing an extract selected from the group consisting of pomegranate grass, poultice, open hemp, normal acid and mixtures thereof.

Pomegranate grass (Mollugo pentaphylla) used in the present invention is a perennial herb with pomegranate grass, the height is 10 ~ 30cm, leaves are turned from the bottom and face from the top. In July-October, yellowish brown flowers inflorescences bloom at the tip of stems and fruits are in the form of granules. They grow in roads and fields, and are known to be distributed in Korea, Japan, China and India.

Angelica anomala is a perennial herb of mountainous family, stem is about 2 meters high, and hollow inside. The leaves are double leaves, serrated, and white flowers bloom in double inflorescences in August. Fruits are elliptical, about 7mm long, with four stalks on the back, separated when ripe. Roots are known to be used primarily as a medicinal herb. Grows in the valley and is distributed in Gangwon, Gyeonggi, Gyeongsang, Pyeongbuk, Hamnam, and Hwanghae.

Materuccia orientalis is a perennial herbaceous plant of cotton, and is 60 ~ 90cm high and leaves are clustered and feathered. There is a black brown hole of the hole. It grows in the shade of mountains or forests and is known to be distributed in Korea, Japan, China and the Himalayas.

Sangsan (Orixa japonica) refers to the roots of the meadowsweet, which is tasteful, spicy and toxic, and is mainly used for the treatment of mucus and phlegm. It is a deciduous broad-leaved shrub with the Hyanghyang family, about 2 meters high, and the leaves are alternate and long oval. Yellow flowers bloom in April in inflorescences, and the fruit is brownish, ripening in November. The roots are medicinal and the wood is used for handwork. It grows at the foot of the mountain and is known to be distributed in Korea's Jeolla-do and Japan.

In a specific embodiment, the extracts selected from the group consisting of pomegranate grass, poultice, open horse, hemp, and mixtures thereof are propionibacterium acnes and staphylococcus epidermis which are the main causes of acne invention. It showed antimicrobial activity against staphylococcus epidermidis, as well as inhibitory effect on the secretion of basophilic cytokines IL-8 and TNF-α. In addition, no irritation was observed when applied to the human skin was confirmed that it can be usefully used as a cosmetic and formulation for the purpose of improving acne.

In another aspect, the present invention

(a) drying and pulverizing the pomegranate grass, poultices, cotton hemp or normal acid;

(b) extracting and filtering the dried plant in (a);

(c) repeating extraction and filtration once to five times; And

(d) Concentration under reduced pressure and freeze drying after filtration of the extract of (c)

It provides a method for producing a composition for preventing or treating acne comprising a.

In step (a), pomegranate grass, poultry, open hemp or normal acid can be taken and dried, preferably air-dried and pulverized to be used in powder form. The ventilation drying is preferably carried out for 2 weeks at room temperature in a specifically shielded state.

In step (a) the plant in powder form is extracted. The extraction solvent is to use ethanol, preferably 70% ethanol. After extraction, it is preferable to filter using two layers of cotton fabric.

Extracting and filtering the filter cake of step (b) may be repeated once to five times, preferably three times. This process is for increasing yield.

The combined extracts obtained above were filtered using a filter paper, and then the filtrate was concentrated under reduced pressure to remove the solvent. After that, it can be lyophilized to prepare a composition for preventing or treating acne of the present invention.

In another aspect, the present invention relates to cosmetics and preparations for the prevention or treatment of acne, containing the composition as an active ingredient.

Acne prophylactic or therapeutic cosmetics contain the composition as an active ingredient, such as skin, lotions, essences, nourishing creams, massage creams and cleansing creams, such as basic creams and powders such as cleansing foams, soaps, sunscreens and packs. , Cosmetics, foundations, and makeup cosmetics, including makeup bases. At this time, in order to facilitate the distribution of the cosmetic, it may also include a variety of excipients acceptable for the cosmetic, which acts as a diluent, dispersant or carrier for the active ingredient in the composition. Excipients other than water or excipients containing water include emollients, solvents, wetting agents, fats and oils, emulsifiers, surfactants, organic and inorganic pigments, ultraviolet absorbers, preservatives, fungicides, antioxidants, pH adjusting agents in liquid or solid form. , But may also include flavors, thickeners, or powders, but is not limited thereto.

In addition, preparations for preventing or treating acne may be formulated into parenteral dosage forms such as oral dosages, injections, patches, ointments, lotions and creams, such as tablets and capsules, containing the composition as an active ingredient. . In addition, a pharmaceutically acceptable carrier may be included in addition to the above-mentioned composition as an active ingredient. Such pharmaceutically acceptable carriers are commonly used in pharmaceutical preparations, such as lactose, dextrose, sucrose, sorbitol, mannitol, Starch, acacia rubber, calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, Magnesium stearate or mineral oil and the like, but is not limited thereto. The preparations for preventing or treating acne of the present invention may also further include lubricants, wetting agents, sweeteners, flavoring agents, emulsifiers, suspending agents or preservatives as additives.

In addition, antimicrobial agents such as benzoyl peroxide, tetracycline, erythromycin, triclosan, and hormones such as androgen and steroids, which have been used in conventional acne treatments, may be used in combination with vitamin A derivatives such as retinoids, but are not limited thereto. It doesn't happen.

The following examples illustrate the invention in more detail. These examples are only for illustrating the present invention, but the scope of the present invention is not limited to the following examples.

As described above, the pomegranate grass, poultice, chaff, or hepatic extract of the present invention have excellent antibacterial and anti-inflammatory effects, which can alleviate the inflammatory phenomenon of skin tissue and prevent acne by being safe without any other irritation or side effects on the skin. Or may be usefully used for treatment.

Preparation Example: Preparation of Plant Extract

Pomegranate grass, poultry, open hemp or normal acid was taken and air-dried at room temperature for 2 weeks in a shaded state and then ground and used in powder form. The dried powdered plants were extracted using 70% ethanol. After extraction, it was filtered using two layers of cotton fabric. In order to increase the yield, the filter cake was repeatedly extracted and filtered three times. The obtained extracts were combined and filtered using a filter paper. The filtrate was concentrated under reduced pressure to remove the solvent, and then freeze-dried to prepare a composition of the present invention.

Example 1: Antimicrobial Activity Experiment

Propionibacterium acnes (ATCC6919) and staphylococcus epidermidis (KCTC3958) were used for microbial testing. Before analysis, propionibacterium acnes (ATCC6919) was incubated in GAM broth for 48 hours at 37 ° C. in anaerobic conditions. Staphylococcus epidermidis (KCTC3958) was incubated with Corynebacterium medium (10.0 g of casein peptone per liter, 5.0 g of yeast extract, 5.0 g of glucose, 5.0 g of NaCl) at 37 ° C. for 24 hours. In vitro antimicrobial activity was measured by the broth microdilution method in a 96-well microtiter plate. 2-fold dilution of each extract was prepared in broth medium at a concentration of 500-15.6 μg / ml. Each well was injected with 5 μl of bacterial suspension at a density of 10 ⁷ CFU / mL. Microtiter plates were incubated at 37 ° C. for 24 hours. Microbial culture was determined by the degree of suspension with a spectrophotometer (Power Wave, Bio-tek Inc., VT, USA) at 600 nm. MIC defines microbial culture results that are not visible to the naked eye as the minimum broth concentration of 70% ethanol extract.

plant MIC (μg / ml) Propionibacterium Acnes Staphylococcus epidermis Pomegranate grass 250 125 Aperture 15.6 125 Cotton horse 250 31.2 Sangsan 250 125

As shown in Table 1, the four extracts were confirmed to have excellent antibacterial activity against Propionibacterium Acnes and Staphylococcus epidermidis.

Example 2: Evaluation of cytokine inhibitory effect

Treatment of 1 × 10 ⁶ THP-1 cells, a human monocyte cell line, with 100 μg / ml propionibacterium acnes inactivated by heat treatment in the absence of serum alone or with pomegranate, poultice, open hemp or normal acid After incubation for 48 hours. The amount of IL-8 and TNF-α secreted into the cell medium was measured using an ELISA kit (Genzyme, Minneapolis, MN, USA).

As shown in Figure 1a and Figure 1b, pomegranate grass, ponylet, open horse or acid extract extract was confirmed that the concentration-dependent inhibition of the production of inflammatory factors IL-8 and TNF-α.

Example 3: Cytotoxicity Assay

HaCaT and human normal fibroblasts were cultured in 37 ° C., 5% CO ₂ incubator using DMEM medium containing 10% FBS (Gibco), penicillin-streptomycin. Cells were cultured in 24-well plates and drug treatment started 24 hours after incubation. The general production of cultured cells was determined by MTT, ie MTT analysis, reduced to formazan. HaCaT and human normal fibroblasts were incubated at 37 ° C., 5% CO ₂ incubator with various concentrations of pomegranate grass, pony rot, open horse or normal acid extract, MTT (1 mg / ml PBS) in 1/10 volume of medium To each well, and DMSO was added to dissolve the formazan crystals. Absorbance was measured at 570 nm using an absorbance spectrometer (Power Wave, Bio-tek).

As shown in Figures 2a and 2b, MTT analysis showed that the extract of the present invention in HaCaT and human normal fibroblasts is safe for the skin through the results of more than 80% viability at high concentrations.

Figure 1a is a graph showing the IL-8 production inhibitory effect by the concentration of four extracts of the present invention.

Figure 1b is a graph showing the TNF-α production inhibitory effect by the concentration of the four kinds of extracts of the present invention.

Figure 2a is a graph showing the viability in human normal fibroblasts by the concentration of four extracts of the present invention by concentration.

 Figure 2b is a graph showing the viability in HaCaT by concentration of four extracts of the present invention by concentration.

Claims (7)

A composition for preventing or treating acne, comprising an extract selected from the group consisting of pomegranate grass, poultice, open horse, normal acid and mixtures thereof. The composition of claim 1 having antimicrobial activity against propionibacterium acnes and staphylococcus epidermidis. The composition of claim 1, wherein the composition has an inhibitory effect on IL-8 and TNF-α secretion. (a) drying and pulverizing the pomegranate grass, poultices, cotton hemp or normal acid; (b) extracting and filtering the dried plant in (a); (c) repeating extraction and filtration once to five times; And (d) Concentration under reduced pressure and freeze drying after filtration of the extract of (c) Method of producing a composition for preventing or treating acne comprising a. The method of claim 4, wherein the extraction solvent is ethanol. A cosmetic for preventing or treating acne containing the composition of claim 1 as an active ingredient. A preparation for preventing or treating acne, comprising the composition of claim 1 as an active ingredient.

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