KR20160066171A - Composition containing icariside B2 for antibacterial - Google Patents

Abstract

The present invention relates to an antibacterial cosmetic composition and, more specifically, to a cosmetic composition providing an excellent antibacterial effect and having effects of alleviating acne and inhibiting dandruff by containing icariside B2 as an active ingredient. The antibacterial composition contains, as an active ingredient, icariside B2 represented by chemical formula 1.

Description

Composition containing icaricide B2 as an active ingredient {Composition containing icariside B2 for antibacterial}

The present invention relates to a cosmetic composition for antibacterial use, and more particularly, to a cosmetic composition having an antimicrobial effect by containing icaricide B2 as an active ingredient and having an effect of improving acne, inhibiting lipid formation and inhibiting dandruff.

Acne refers to inflammation of hair follicles, hair follicles and surrounding tissues due to the action of hormones, excess sebum secretion, bacterial infection, and the like.

The causes of acne can be divided into several types. The first cause is excessive sebum production. Sebum is secreted from the sebaceous glands, and in normal amounts, it prevents the harmful substances from outside the skin from penetrating between keratinocytes. However, in the environment of puberty, before and after menstruation, at the beginning of pregnancy, taking contraceptive pill, stress, etc., the human body shows a hormone balance different from the normal state. This altered hormone balance stimulates the sebaceous glands, which are induced by excessive secretion of sebum. In addition, there are many oils that are genetically high in sebum secretion and may be increased by changes in outside temperature or increased skin temperature due to erroneous eating habits.

The second cause is infection of pores. Excessively secreted sebum contains a lot of fatty acids, which increases the pH of the skin surface and dissolves the lipids of the skin, thereby reducing the skin's own defense. On the surface of the skin with increased pH, the causative bacteria of acne become easily proliferated, and the acne bacteria that are proliferated cause the pyogenic inflammation through weakened skin.

In general, acne can be divided into 4 stages according to symptoms. The first step is acne-causing acne that causes excess sebum to accumulate in the pores around the sebaceous glands and form a mucosa. Acne blemishes in the first step are acne lesions that are initially a mild stage, but they are not good for cosmetics and become skin troubles. At this stage, good management can inhibit the development of inflammation. In stage 2 acne vulgaris, acne bacterium grows and inflammation reaction occurs and red acne appears. It is called papule and scarring can occur if not properly managed. In stage 3 acne, red acne inflammation reaction becomes worse, and a pus is formed inside. It is called pustule. In this stage, special treatment is needed because scars may remain after treatment. The last four-stage nodular acne is a stage in which pus pockets burst from the skin and cause more inflammation around the acne lesion. This is called a nodule. It is a period when the inflammation has penetrated into the dermis. It requires professional treatment. Can be prolonged.

The treatment of acne is topical drug application and oral medication, and surgical treatment such as laser treatment, lapping, etc.

Topical application is the use of antibacterial agents such as azelaic acid and salicylic acid for the purpose of antibacterial action against propionibacterium acnes , which is known as a cause of acne, and benzoyl peroxide peroxide and the like are used as external ointment type. However, azelaic acid is difficult to formulate and salicylic acid is classified as a preservative in Korea and can not contain more than 0.5% in the formulation. Benzoyl peroxide is a raw material that can not be used as a raw material for cosmetics in Korea.

Oral drug therapy uses retinoids, corticosteroids, and other drugs to inhibit the function of sebaceous glands and inhibit hair follicle wall destruction. These preparations have side effects such as skin rash and skin dryness when taking too much dose, and allergies may occur depending on the individual, so caution is required for their use.

On the other hand, the causative bacteria of dandruff include Malassezia furfur or Malassezia globosa , which are the causative bacteria of the scalp and inflammation of the scalp.

Considering various aspects such as the onset of onset, progression of acne, dandruff and other skin diseases, the external application agent directly used for skin can be said to be more effective (refer to Korean Patent Publication No. 2004-0056081) .

At the stage of cosmetics, there are not many substances that can see this effect. However, it can be used over a long period of time. Therefore, many plant extracts and synthetic materials are being developed as a composition for improving acne skin, but there are not many products that are safe for skin and exhibit the effect desired by consumers because of high therapeutic effect and skin side effect such as skin keratinization after use.

On the other hand, icaride B2 (icariside B2) can be isolated from the terpenoid component extracted from a part of the perennial plant Asplenium scolopendrium belonging to the fern gossypii and can be chemically synthesized (Natural Product Sciences, 14 (4): 265-268 (2008)). As to the icaricide compound icaride II (icariside II), whitening activity has already been known (International Patent Publication No. WO 2008/035918, published on Mar. 27, 2008). On the other hand, remarkable research results on icaricide B2, which is an icaricide compound, have not been reported yet.

International Patent Publication No. WO 2008/035918, published on March 27, 2008

Thus, the present inventors completed the present invention by confirming that icaricide B2 provides excellent antibacterial activity against acne cause bacteria and dandruff causative bacteria, suppresses excessive sebum production, and effectively inhibits lipid production of skin.

In order to achieve the above object, the present invention provides an antimicrobial cosmetic composition comprising icaricide B2 as an active ingredient as an active ingredient.

The cosmetic composition containing the icaricide B2 of the present invention as an active ingredient exhibits its effect by rapidly suppressing the growth and growth of microorganisms primarily involved in skin acne and skin irritation. Secondly, It suppresses excess sebaceous secretion and improves acne skin by extinguishing acne blemishes.

Further, the cosmetic composition containing the icaricide B2 of the present invention as an active ingredient suppresses the occurrence of dandruff.

In addition, the cosmetic composition containing icaricide B2 of the present invention as an active ingredient suppresses the generation of lipid by inhibiting lipid production, suppressing the occurrence of acne, and suppressing seborrheic dandruff in the case of scalp.

The cosmetic composition of the present invention contains icaricide B2 as an active ingredient.

[Chemical Formula 1]

The cosmetic composition according to the present invention may contain 0.0001 to 50% by weight of the icaricide B2 based on the total weight of the composition. If the content of the icaricide B2 is less than 0.0001% by weight, the effect of improving the antimicrobial and anti-inflammatory properties of the extract may not be significantly improved. If the content of the icaricide B2 is more than 50% by weight, skin safety or shape problems may occur.

The cosmetic composition for improving acne according to the present invention is excellent in antibacterial effect, particularly antibacterial effect against acne causing bacteria.

Further, the cosmetic composition containing the icaricide B2 of the present invention as an active ingredient suppresses dandruff and suppresses the occurrence of dandruff.

In addition, the cosmetic composition containing icaricide B2 of the present invention as an active ingredient suppresses the generation of lipid by inhibiting lipid production, suppressing the occurrence of acne, and suppressing seborrheic dandruff in the case of scalp.

The cosmetic composition according to the present invention may be formulated containing a cosmetically or dermatologically acceptable medium or base. These are all formulations suitable for topical application, for example as a solution, a gel, a solid, a paste anhydrous product, an emulsion obtained by dispersing an oil phase in water, a suspension, a microemulsion, a microcapsule, a microgranule or an ionic form (liposome) In the form of ionic fibrin dispersions, or in the form of creams, skins, lotions, powders, ointments, sprays or conical sticks. It can also be used in the form of a foam or in the form of an aerosol composition further containing a compressed propellant. These compositions may be prepared according to conventional methods in the art.

In addition, the cosmetic composition of the present invention can be specifically used as a hair cleanser, a scalp cleanser, a softening agent, a convergent lotion, a nutritional lotion, a nutritional cream, a massage cream, an essence, an eye cream, an eye essence, a cleansing cream, a cleansing foam, a cleansing water, A body lotion, a body cream, a body oil, and a body essence.

The cosmetic composition according to the present invention may further comprise at least one selected from the group consisting of a fatty substance, an organic solvent, a solubilizer, a thickening agent, a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, The active ingredient may be combined with any other ingredients commonly used in cosmetics, such as ionic emulsifiers, fillers, sequestering agents, chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, And may contain adjuvants commonly used in the same cosmetic or dermatological fields. Such adjuvants are introduced in amounts commonly used in the cosmetics or dermatological fields.

Hereinafter, the constitution and effects of the present invention will be described in more detail with reference to test examples and examples. However, these test examples and examples are provided for illustrative purposes only in order to facilitate understanding of the present invention, and the scope and scope of the present invention are not limited by the following examples.

[Reference Example]

Icaricid B2 for testing the efficacy of the composition of the present invention was purchased from Simagchem Corporation.

[Formulation Example 1 and Comparative Formulation Examples 1 and 2]

Formulation Example 1 and Comparative Formulation Examples 1 and 2 were prepared according to the ingredients and the contents (% by weight) shown in Table 1 below. Specifically, Formulation Example 1 was prepared by blending icaricide B2 of the above Reference Example, Comparative Formulation Example 1 contained no effective ingredient for improving acne skin, Comparative Formulation Example 2 was used as a standard for antibacterial activity As a standard substance, it contains erythromycin, which is widely used as an acne remedy.

The production methods of Formulation Example 1 and Comparative Formulation Examples 1 and 2 are as follows. The components of the phase A in Table 1 were completely dissolved, the components of the phase B were completely dissolved in a separate melting tank, and the phase B was added to the phase A to be mixed and solubilized. Here, the components of the C phase were mixed according to the mixing ratios shown in Table 1 (the unit of the numerical value is% by weight), and the components were mixed and homogenized and filtered to prepare the compositions.

division Formulation Example 1 Comparative Formulation Example 1 Comparative Formulation Example 2 A Deionized Water To 100 To 100 To 100 EDTA-2Na 0.02 0.02 0.02 glycerin 5.0 5.0 5.0 B PEG-60 hydrogenated castor oil 0.4 0.4 0.4 Perfume 0.04 0.04 0.04 C Icari seed B2 5.0 - - Erythrombomycin - - 5.0

[Test Example 1] Test for antimicrobial activity against acne bacteria

Each of the cosmetic compositions prepared in the formulations of Formulation Example 1 and Comparative Formulation Examples 1 and 2 was tested for the antibacterial activity against Propionibacterium acnes (ATCC 6919: medium-BHI broth), which is a causative strain of acne .

The test method for the antimicrobial activity against acne bacteria was as follows.

(1) Preparation of test strain

Propionibacterium acnes were cultured in an anaerobic culture inoculated with BHI broth.

(2) Dilution solution preparation

0.15 ml of the above test solution was added to 15 ml of BHI broth (pH 6.8) or LB broth (pH 4.5), and the mixture was used as a diluting solution.

(3) Preparation of sample

The undiluted cosmetic composition prepared from Formulation Example 1 and Comparative Formulation Examples 1 and 2 was used as a sample.

(4) Antimicrobial activity test

1) In a 96-well 96-well plate, place the sample in line 1 and add 200 μl of diluted solution.

2) Thoroughly mix the mixture of line 1, and then take 100 μl of the mixture, place it in the second row, mix well, and then repeat the double dilution by adding 100 μl to the third row.

3) After culturing the cells at 32 ° C for 24 hours and 48 hours, determine whether the bacteria are proliferating to the extent of suspension, and determine the minimum concentration without bacterial growth as the MIC (Minimum Inhibitory Concentration) value. If the mixture is opaque and it is difficult to judge the growth of the microorganism, check with a microscope.

The results of the antimicrobial activity tests against acne bacteria are shown in Table 2 below. The MIC was expressed in terms of the concentration of the active ingredient contained in the formulation.

Item pH Propionibacterium acnes Formulation Example 1 5.7 ≪ 89 ppm Comparative Formulation Example 1 5.7 > Highest concentration (no antimicrobial activity) Comparative Formulation Example 2 5.7 ≪ 100 ppm

The lower the ppm concentration in the MIC, the more effective the antimicrobial activity against acne bacteria. In the case of Formulation 1, the ppm concentration is smaller than that of Comparative Formulation Example 2 using erythrombomycin, a known acne treatment agent, It can be confirmed that it has excellent antibacterial activity.

[Test Example 2] Lipogenesis inhibition test

3T3-L1 cells (CL-173; ATCC, USA) were cultured in a 6-well culture medium containing DMEM (Dulbecco's modified eagles medium, GIBCO BRL, Life Technologes) medium containing 10% fetal bovine serum Lt; ⁵ > cells / well in a culture plate. After 2 days, the cells were replaced with fresh DMEM (containing 10% FBS) medium and cultured for 2 days. Then, the cultured cells were again induced to differentiate into DMEM (containing 10% FBS) containing 1 μg / ml insulin, 0.5 mM IBMX and 0.25 μM dexamethasone, and after 2 days, The cells were cultured for 5 days in DMEM supplemented with insulin. After 5 days, the cells were replaced with normal medium (DMEM, containing 10% FBS) and cultured while observing until the cells morphologically changed into adipocytes.

To evaluate the inhibitory effect of icaricide B2 on adipocyte accumulation in adipocytes, the above-described 3T3-L1 adipocytes were stained with S-III (S4136, sigma-aldrich). The adipocytes were fixed with 4% paraformaldehyde (pH 7.2) in phosphate buffer at room temperature, washed with PBS (phsphate buffered saline), stained with SIII and then photographed and compared visually. As a control group, 50 μM caffeine and 50 μM icaricide B2 were used as test groups, respectively. The degree of inhibition of fat accumulation was evaluated as +++ , ++, +, -. The results are shown in Table 3.

sample % Inhibition Control group +++ Comparative group + Icari seed B2 +

As shown in Table 3, it can be seen that the icaricide B2 used in the present invention has lipid synthesis inhibitory effect. Therefore, it can be seen that the lipid synthesis is suppressed and sebum is reduced to suppress the occurrence of acne, and in the case of the scalp, seborrheic dandruff can be suppressed.

[Test Example 3] Test for improvement of acne and reduction of sebum secretion and stimulation

Twelve individuals with acne were allowed to use the cosmetic composition prepared from Formulation Example 1 and Comparative Formulation Examples 1 and 2 for one month. Acne improvement scale is from 1 point to 5 points, 1 point is 'No', 3 points are 'Normal' and 5 points are 'Very agree'. The results of the experiment are shown in Table 4 below with an average score of 12 persons.

The acne extermination period was based on the number of days of disappearance readings, and the results were based on the results after 1 month with or without recurrence of acne. The reduction of sebaceous secretion was from 1 point to 5 points, 1 point was 'No', 3 points were 'Normal' and 5 points were 'Very agree'. The experimental results are shown in Table 4 below with an average score of 12 persons. The presence or absence of skin irritation was evaluated as (number of stimuli) / (total number of test subjects).

Inflammatory acne improvement Acne-bloating period Recurrence of acne Decrease sebaceous glands Presence or absence of stimulation Formulation Example 1 3.4 5 days radish 4.3 0/12 Comparative Formulation Example 1 2.1 13th U 2.0 0/12 Comparative Formulation Example 2 4.2 2 days radish 4.1 9/12

As shown in Table 4, it can be seen that Formulation Example 1 has no recurrence of acne as compared with Comparative Formulation Example 1, and has excellent effects on improvement of acne as a whole. On the other hand, Comparative Formulation Example 2 containing the antimicrobial activity standard has similar efficacy to that of Formulation Example 1, but it has a strong irritation in use and may cause skin irritation for long-term use.

[Formulation Example 4 and Comparative Formulation Example 5]

A shampoo was prepared in the composition shown in Table 5 (unit of the numerical value is% by weight). Specifically, the surfactant and ethylene glycol distearate were added to purified water, heated to 80 deg. C to uniformly dissolve, and gradually cooled to 40 deg. C with stirring. To the mixture was added icariisside B2 , A preservative, a viscosity controlling agent, a perfume, and a hair conditioning agent were mixed and stirred, followed by cooling to room temperature.

ingredient Formulation Example 4 Comparative Formulation Example 5 Ammonium lauryl sulfate 10 10 Polyoxyethylene lauryl ammonium sulfate 5 5 Cocoamidopropyl betaine 2 2 Ethylene glycol distearate 1.5 1.5 Cocoyl monoethanolamide 0.8 0.8 Icari seed B2 5.0 - Polyquaternium-10 0.2 0.2 Blue No. 1 0.0002 0.0002 Yellow No. 4 0.0001 0.0001 Methyl paraben 0.1 0.1 Spices 0.8 0.8 Citric acid 0.1 0.1 Dimethicone 1.0 1.0 water to 100 to 100

[Test Example 5] Dandruff reduction effect test

In order to evaluate the antibacterial activity of the cosmetic composition according to the present invention, Formulation Example 4 and Comparative Formulation Example 5 were applied to P. ovale 12078 (Malassezia furfur) and Malassezia globosa (ATCC 96807) The antimicrobial activity was tested.

Prepare Malassezia globosa and Malassezia furfur test broth by shaking culture at 32 ° C for 2 days with a yeast culture medium suitable for culturing Malassezia , and dilute the test broth with culture medium. A sample dilution solution for the antimicrobial test was prepared by diluting the culture medium with 2.0% concentration.

Add 200 μl of the sample dilution to the 96 well plate. In the remaining wells, add 100 μl of medium for each strain. Mix well and mix well. Mix well and mix well. Add 100 μl and mix well. Perform double dilution by adding 100 μl to the third row. Add 10 μl of each test solution to 10 ⁵ to 10 ⁶ in all wells. After culturing under the same conditions as the culture conditions of the test organism, the minimum concentration without bacterial growth is determined as the MIC value by judging whether or not the bacteria are proliferated to the extent of suspension. If the mixture is opaque and it is difficult to judge the growth of the microorganism, check with a microscope. Table 6 shows the inhibition of growth of the test bacteria of Formulation Example 4 and Comparative Formulation Example 5 when the suspension was transparent to the same extent as the culture solution.

sample Scalp Minimum development inhibition concentration MIC (%) Formulation Example 4 Malassezia globosa 0.0833 Formulation Example 4 P. ovale 12078 ( Malassezia furfur ) 0.028 Comparative Formulation Example 5 Malassezia globosa > 2 Comparative Formulation Example 5 P. ovale 12078 ( Malassezia furfur ) > 2

From the results of Table 6, it was confirmed that Formulation Example 4 has antibacterial activity against Malassezia furfur and Malasseziaglobosa . MICs of less than 0.125% may have significant antimicrobial efficacy in the product.

[Test Example 6] Dandruff reduction effect test

Twenty-four men aged 19 to 35 years with a relatively large number of dandruff were selected and the dandruff reduction rate was measured after using the shampoo of each of Formulation Example 4 and Comparative Example 5 for 2 months in the following manner for 12 months in the following manner .

Before the start of the test, the dandruff was smeared with ordinary shampoo, and the dandruff accumulated for 2 days after shedding was collected. The dandruff weight was sampled once every two days with the shampoo of each of Formulation 4 and Comparative Example 5, The weight of accumulated dandruff was compared and evaluated. The accumulated dandruff was collected directly from the scalp using a vacuum suction device, and the dandruff reduction rate was calculated according to the following equation (1). The results are shown in Table 7 below.

[Equation 1]

Formulation Example 4 Comparative Formulation Example 5 Dandruff reduction rate (%, average value) 51.4 3.4

As can be seen from Table 7 above, Formulation Example 4 containing icaricide B2 as an active ingredient shows excellent dandruff-preventing effect.

While the present invention has been particularly shown and described with reference to specific embodiments thereof, those skilled in the art will readily appreciate that many modifications are possible in the exemplary embodiments without materially departing from the novel teachings and advantages of this invention. something to do. Accordingly, the actual scope of the present invention will be defined by the appended claims and their equivalents.

Claims (7)

1. An antimicrobial cosmetic composition comprising icaricide B2 represented by the following formula (1) as an active ingredient.
[Chemical Formula 1]

The cosmetic composition according to claim 1, wherein the composition is for improving acne. [Claim 3] The cosmetic composition according to claim 2, wherein the composition is for antibacterial use against Propionibacterium acnes which is a cause of acne. The cosmetic composition according to claim 1, wherein the composition inhibits lipid production. The cosmetic composition according to claim 1, wherein the composition is for dandruff repression. The cosmetic composition according to claim 1, wherein the composition is for antibacterial use against Malassezia furfur or Malassezia globosa which is a cause of dandruff. The cosmetic composition according to any one of claims 1 to 4, wherein the icaricide B2 is contained in an amount of 0.001 to 50% by weight based on the total weight of the composition.