KR20180127279A - Anti-acne composition comprising extracts of rubus coreanus and willow - Google Patents

Abstract

The present invention relates to an anti-acne composition which contains at least one among extracts of Rubus coreanus, Salix pierotii, and propolis as an effective component. The anti-acne composition of the present invention exhibits high NO production inhibitory activity and antimicrobial activity at the same time, and thus can provide an excellent effect on acne treatment.

Description

(ANTI-ACNE COMPOSITION COMPRISING EXTRACTS OF RUBUS COREANUS AND WILLOW)

The present invention relates to an anti-acne composition comprising a bramble extract and a willow extract.

Acne (Acne vulgaris) is a chronic inflammatory disease of the hair follicles and sebaceous glands. The cause of acne is mainly caused by an increase in sebum secretion, hair follicular epithelium abnormalization and keratinization, and proliferation of anaerobic skin bacteria, Propionibacterium acnes. In addition, hormone imbalance, stress, The cause of acne is very complicated because it is affected by body or mental condition, such as bad body condition.

If you look at the progress of acne, the initial stage is that excess sebum is piled up in the pores, the inside of the blanket is expanded to the pressure of sebum to become a comedo, the clogged pores become white acne (closed skin) It looks a little open and black, it becomes black acne (open cotton). As the acne progresses, the bacteria become inflamed, resulting in a reddish-purple papule which has a red and milky skin. This becomes a pus containing pus.

About 90% of acne appears in teenagers, but it also appears in adults and men in their 20s and 30s. Teen acne and adult acne show some differences. Teenage acne is prone to occur in the forehead, face, and oily skin during spring and summer, when sebaceous gland is dominant, whereas adult acne tends to recur throughout the year without limitation. As a cause of adult acne, the hormones that are attracting attention are the balance of male hormones that stimulate sebaceous glands to secrete sebum and the female hormones that inhibit the action of sebaceous glands, resulting in excessive sebum secretion and acne.

Conventionally, for the treatment of acne, acne bacteria are suppressed by using antibiotics such as erythromycin and benzoyl peroxide, or acne bacteria are removed by using triclosan or salicylic acid. However, And it is impossible to control excess sebum secretion, which is one of the main causes of acne. Therefore, there is a limit to the fundamental acne treatment method.

In addition, estrogen, which is a female hormone, has been used to treat acne by controlling sebaceous secretion. However, hormones have disadvantages in that they cause disturbance to human homeostasis and have serious side effects and can not be used continuously.

In addition, although there is a method of removing skin exfoliation using a vitamin A derivative, such a treatment method has some effect, but most of the problems are skin irritation, skin irritation or side effects such as photosensitivity and frequent recurrence.

Furthermore, acne usually involves inflammation without exception, and in the case of pyuric inflammatory acne, since it leaves permanent marks on the skin from puberty to adults, it is also necessary to inhibit the inflammatory response for the desired treatment of acne , Mostly products that depend on antibacterial effect.

Accordingly, studies on the treatment and prevention of acne using natural extracts have been increasing in recent years. Conventional techniques for the treatment and prevention of acne using natural extracts can be exemplified by the following Patent Documents 1 to 4. Thus, the entire contents of the following Patent Documents 1 to 4 are incorporated as the background art of this specification.

Patent Document 1 discloses a composition for reducing sebum production in sebaceous glands including Psidium guajava fruit extract or Kunzea ericoides leaf extract or both.

Patent Document 2 discloses an antimicrobial agent containing an antimicrobial extract having an excellent antibacterial activity against Propionibacterium acnes which is a causative agent of acne, A composition effective for alleviating and preventing acne symptoms is disclosed.

Patent Document 3 discloses a method of inhibiting the growth of Propionibacterium acnes, which is a main pathogen that exacerbates acne symptoms, by using a natural plant, Cucumber tree. There is no side effect compared to conventional acne treatment methods, and continuous use Discloses a cosmetic composition for acne skin which is capable of being safe and has excellent safety.

Patent Document 4 relates to a cosmetic composition containing active fractions of Rubus coreanus MIQ roots, wherein an active fraction of Rubus coreanus MIQ roots contains 5α-reductase inhibiting the initial symptoms of acne ) Suppressing the production of excessive sebum due to inhibition, inhibiting the keratinization, and exhibiting an action of inhibiting the induction of nitric oxide activity against progressive acne, thereby preventing and improving acne. In addition, And relates to a cosmetic composition having a moisturizing effect.

However, it is not known that a composite composition containing a bokbunja extract and a combination of willow extract or propolis is used.

KR publication 10-2014-0008335 A (2014.01.21.) KR registration 10-1507889 B1 (2015.04.07.) KR public 10-2011-0130184 A (2011.12.05.) KR publication 10-2014-0025239 A (2014.03.04.)

Skin diseases, like most diseases, are accompanied by an inflammatory reaction, and acne, in particular, is accompanied by inflammation. Therefore, in the current market, it is necessary not only to protect the skin from inflammation by directly inhibiting the nitric oxide synthase (NOS) involved in inflammation, but also to suppress the bacteria (especially acne bacteria) Is required.

Thus, the inventors of the present invention have confirmed that a combination preparation obtained by mixing willow bark extract and / or propolis with brambone extract exhibits remarkable NO production inhibitory activity and antimicrobial activity, respectively, as compared with the respective preparations, and completed the present invention .

SUMMARY OF THE INVENTION The present invention has been made to solve the above-mentioned problems of the prior art,

Wherein the active ingredient is at least one selected from the group consisting of bamboo extracts, willow extracts, and propolis extracts.

In addition, the present invention provides an anti-acne composition, wherein the active ingredient is contained in a ratio of brambane extract: willow extract = 1: 1 to 4: 1.

The present invention also provides an anti-acne composition comprising the active ingredient in a ratio of brambler extract: propolis = 1: 0.5 ~ 2.

The present invention also provides an anti-acne composition, wherein the active ingredient is contained in a ratio of brambler extract: propolis extract: willow extract = 1: 1: 2.

In the present invention, there is also provided an anti-acne composition comprising the active ingredient in an amount of 0.001 to 20 wt% based on the total weight of the composition.

In the present invention, there is also provided an anti-acne composition, wherein the active ingredient has an antibacterial action and an anti-inflammatory action.

In addition, the composition of the present invention can be used as a cosmetic composition for cosmetics including toner, flexible lotion, convergent lotion, nutritional lotion, ampoule, lotion, essence, nutritional cream, eye cream, massage cream, cleansing cream, cleansing lotion, foaming wash, cleansing foam, , Cleansing gel, wash off pack, peel off pack, sheet mask pack, hydrogel mask pack, lipo gel mask pack, clay mask pack, soap, spray, line cream, sun lotion, Make-up base, foundation, and primer product.

INDUSTRIAL APPLICABILITY The present invention simultaneously exhibits a high NO production inhibiting activity and an antimicrobial activity, and thus has a high effect for the treatment of acne.

Hereinafter, the present invention will be described in detail.

The present invention relates to an anti-acne composition comprising as an active ingredient at least one selected from bramble extract, willow extract and propolis extract.

In order to enhance the anti-acne effect (prevention and treatment of acne), the above-mentioned active ingredient may be contained in a ratio of 1: 1 to 4: 1 by weight of brambone extract: willow extract, or 1: 0.5 to 2 by weight of brambone extract: propolis . Particularly, it is more preferable that the effective ingredient is contained in a ratio of brambane extract: propolis extract: willow extract = 1: 1: 2. In this range, the antimicrobial and anti-inflammatory effects are shown to be the greatest. A more detailed understanding of this may be made through the following examples and experimental examples.

The active ingredient is preferably contained in an amount of 0.001 to 20% by weight based on the total weight of the composition. If the amount of the extract is less than 0.001, the desired effect can not be exhibited. If the amount of the extract is more than 20% by weight, the degree of increase in the effect of the extract is insignificant. Even if the cytotoxicity is not a problem, May cause storage stability problems such as shortening the shelf life and problems in the formulation process.

The active ingredient not only has an antibacterial action and an anti-inflammatory action, but also exhibits an increased effect due to the combination of each ingredient. A more detailed understanding of this may be made through the following examples and experimental examples.

The anti-acne compositions of the present invention may be formulated into various cosmetic composition formulations and include, but are not limited to, toners, softening lotion, convergent lotion, nutritional lotion, ampoule, lotion, essence, Cleansing Cream, Cleansing Lotion, Foaming Wash, Cleansing Foam, Cleansing Water, Cleansing Gel, Wash Off Pack, Peel Off Pack, Sheet Mask Pack, Hydrogel Mask Pack, Ripo Gel Mask Pack, Clay Mask Pack, Soap, Spray , Sun cream, sun lotion, sun lotion, sun mist, bee cream, makeup base, foundation, and primer products.

Hereinafter, the present invention will be described in more detail with reference to examples. The following examples are for the purpose of illustrating the present invention and are not intended to limit the scope of the present invention.

Example

Preparation of bokbunja extract

Rubus root was washed with purified water, dried and sieved. Purified water and ethanol 3: 7 mixed solvent were extracted by adding about 10 times volume. A cooling condenser was installed to prevent the solvent from evaporating and was extracted by heating for 12 hours while maintaining a temperature of 60 to 80 캜. The extract was filtered with 400 mesh filter cloth, and the residue was extracted once more by the same method. The extract was cooled to room temperature and filtered through a filter paper of Wattman No. 2. The filtrate was filtered through a filter paper of Wattman No. 2 and filtered using a distillation apparatus (Buchi Rotavapor R-124, Water Bath B-480 Made in Switzerland, Eyela A-3S Tokyo rikakikai) The mixture was distilled while maintaining the temperature at 80 ° C. After the evaporated solvent was recovered, it was concentrated under reduced pressure and then lyophilized to obtain an extract powder of brambly root.

Production of willow extract

The freeze-dried powder was obtained through the same procedure as in Example 1 except that the willow skin was used.

Preparation of propolis extract

Propolis powder was washed thoroughly with water, and the propolis powder was prepared by passing propolis powder through the filter after extracting the propolis by stirring the cornstarch and the cut propolis raw material in a stirrer.

The extracted extracts were mixed at the mixing ratios shown in Tables 1 and 2 to prepare extract bases having various mixing ratios.

Mixing weight ratio Sample name Y1 Y2 Y3 Y4 Y5 Y6 Y7 Bokbunja
extract One - - One One One 2 Propolis extract - One - One One 2 One Willow extract - - One One 2 One One

Mixing weight ratio Sample name Y8 Y9 Y10 Y11 Y12 Y13 Bokbunja
extract One One 2 One One 2 Propolis extract One 2 One - - - Willow extract - - - One 2 One

The prepared extract base was mixed with prescribed excipients as shown in Tables 3 and 4 to finally prepare a cosmetic composition.

Example 1

Raw material name Content (wt%) water Balance glycerin 10 1,3-butylene glycol 10 EDTA-2Na 0.05 Oil 20 Y5 extract base 0.1

Example 2

Raw material name Content (wt%) water Balance glycerin 10 1,3-butylene glycol 10 EDTA-2Na 0.05 Oil 20 Y5 extract base 5

Experimental Example

To the prepared extract base (concentration 1wt%, 5wt%), the following NO production inhibitory effect measurement experiment, cytotoxicity evaluation test and antibacterial activity test were carried out.

Experiment to inhibit nitric oxide (NO) formation

The production amount of NO, which is one of active oxygen and plays an important role in inflammation induction, was confirmed by the following method using griess reagent.

- checking way:

(1) RAW264.7 cells were adjusted to 1.0 × 10 ⁵ cells / ml using DMEM medium, and then inoculated on a 48-well plate and cultured for 18 hours.

(2) A new medium containing the test substance and LPS (1 μg / ml) was treated at the same time and cultured for 24 hours.

③ 100 ㎕ of cell culture supernatant and 100 ㎕ of Griess reagent were mixed and reacted in 96-well plate for 10 minutes, and absorbance was measured at 540 nm using an ELISA reader. The amount of NO produced was measured using the reagent in the form of NO ^{2 -} present in the cell culture.

Positive control: 2-Amino-4-methylpyridine (10 uM)

Cytotoxicity assay (MTT assay)

Living cells convert MTT (3- [4,5-dimethylthiazol-2-yl] -2,5-dipheny-Ltertrazolium bromide) into a bule formazon product by the action of the dehydrogenase in mitochondria, The product was eluted with a solvent, and the relative growth of living cells was measured by measuring the absorbance at 540 nm using ELISA. The specific confirmation method was as follows.

- checking way:

1) RAW264.7 cells were adjusted to 1.0 × 10 ⁵ cells / ml using DMEM medium, and then inoculated into 48-well plates and cultured for 18 hours.

(2) A new medium containing the test substance and LPS (1 μg / ml) was treated at the same time and cultured for 24 hours.

③ 100 ㎕ of MTT solution (2 ㎎ / ㎖) was added and reacted at 37 ℃ for 2-4 hours.

④ Remove the medium and dissolve 300 ~ 500 μl of DMSO crystals.

⑤ Absorbance was measured at 540 nm.

As described above, the effects of the bacterium root extract, the propolis extract and the willow extract on macrophage-mediated NO production, an inflammatory factor induced by LPS, were examined. The results are shown in Table 5 below Respectively.

NO production (%) cell viability (%) LPS (-) -6.44 114.0 LPS (+) 100.00 100.0 2-Am 10 uM 0.51 100.6 Y1 1.0% 89.72 100.1 5.0% 58.98 96.1 Y2 1.0% 81.06 92.8 5.0% 51.81 84.1 Y3 1.0% 74.58 88.6 5.0% 25.46 81.2 Y4 1.0% 61.20 108.1 5.0% 30.42 105.5 Y5 1.0% 41.20 110.9 5.0% 2.13 108.1 10% 1.73 102.2 Y6 1.0% 63.15 108.5 5.0% 14.03 105.8 Y7 1.0% 69.26 108.1 5.0% 22.50 105.5 Y8 1.0% 74.62 102.5 5.0% 48.13 101.3 Y9 1.0% 85.53 102.1 5.0% 29.57 101.0 Y10 1.0% 65.01 102.6 5.0% 35.65 101.8 Y11 1.0% 66.48 101.8 5.0% 26.07 100.9 Y12 1.0% 48.23 101.1 5.0% 7.79 100.0 Y13 1.0% 77.84 101.8 5.0% 22.79 100.0

In addition, the extracts of willow extracts showed the highest NO inhibitory activity among the extracts of each of the extracts. In addition, the combination of propolis and willow extracts inhibited NO production It has been surprisingly found that not only the activity but also the toxicity to the cells are lowered, it is preferable to use the respective extracts in combination with each other rather than using them alone. Especially, it was confirmed that the extracts of Rubus coreanus: Propolis extract: Willow tree extract showed the highest activity and the lowest toxicity at 1: 1: 2 treatment ratio.

Furthermore, the toxicity was increased so that the concentration exceeded 1% of the extract overall, and the concentration of the extract considering the toxicity and NO inhibitory activity is preferably in the range of 0.001 wt% to 20 wt% 10 wt% is more preferable.

Antimicrobial effect test of acne bacteria

The antimicrobial activity test was performed by liquid culture dilution method and paper disc method. Experimental strains were purchased from Korea Gene Bank. Propionibacterium acnes (KCTC 3314), a causative organism of acne, was used for the experiment.

The minimum inhibitory concentration was determined using the Agar Serial Dilution Method to determine the antimicrobial activity of the extract containing the sample. The culture medium was a Reinforced clostridial medium (Merck, Germany). After the bacteria were inoculated in the culture medium, they were anaerobically cultured for 3 days in an incubator at 37 ° C under anaerobic conditions.

The strains cultured for 72 hours were diluted to 1.5 × 10 ⁸ cfu / ml and inoculated into each well. Each sample was prepared for each concentration. The minimum inhibitory concentration (MIC) was determined as the minimum inhibitory concentration (MIC) after incubation for 3 days in an anaerobic condition. The results are shown in Table 6. At this time, the minimum inhibitory concentration means that the smaller the value, the higher the antibacterial effect.

Name of sample Minimum inhibitory concentration (MIC,%) Y1 2.5 Y2 5 Y3 2.5 Y4 1.5 Y5 One Y6 1.5 Y7 One

As shown in Table 6 above, the single composition of bokbunja root extract, propolis extract and willow extract showed a stronger antimicrobial effect against acne strains in complex composition treatment. Also, in order to test the inhibitory effect of the extracts containing the sample on the acne strain, the following experiment was conducted by the paper disc method. One platinum amount of each strain cultured on RC plate medium was inoculated in 10 mL of RC liquid medium for 3 days and then inoculated to the RC plate medium at a concentration of about 10 ⁷ cfu / mL. . After sterilized paper discs (6 mm, Satorius, Germany) were placed on a solid plate medium, the samples dissolved in the solvent were absorbed to 5 mg / disc and incubated at 37 ° C for 3 days in an anaerobic tank. As a comparative group, Triclosan, a synthetic antiseptic known to have strong antibacterial activity, was used. The results are shown in Table 12 below. At this time, the transparent zone around the disc is an indicator of the degree of inhibition of proliferation of the strain, and the larger the diameter, the higher the antibacterial effect against the strain.

Name of sample Transparent zone diameter (mm) Y1 7.2 Y2 7.5 Y3 9.3 Y4 10.6 Y5 12.5 Y6 10.8 Y7 13.2 Triclosan 21

As shown in Table 7, the single composition of bokbunja root extract, propolis extract and willow extract showed stronger antimicrobial effect against acne bacterium when treated with complex composition. Clinical trial for prevention and improvement of acne

In order to examine the effect of improving the acne of the essence prepared in the above examples, clinical experiments were conducted by the following methods.

Subjects were 50 men and women between the late teens and early thirties who had acne on their face. The essence of Example 1 was applied to the left side of the face and the essence of Comparative Example 1 was applied to the right side of the face twice a day in the morning and evening to evaluate the effect of improving acne for 8 weeks. After 8 weeks, the degree of prevention and improvement of acne was judged by photographing and visual observation. The criteria for evaluation were as follows. 8.

Rating Skin condition criteria 0 Normal state One The number of cotton balls is very small, 2 The number or size of cottonseed is medium and the inflammation does not proceed 3 The presence of a small number of inflammatory papules 4 In the presence of a small and wide range of crystals and inflammatory cells 5 In the presence of small and small sized nodules 6 The presence of intermediate inflammatory nodules 7 The presence of a large number of inflammatory nodules 8 In the presence of severe nodular cotton 9 In the presence of severe cystic and inflammatory nodules

The results of the clinical test were judged to be 'excellent' if the grade of the subject's acne was reduced by at least grade 3 according to the criteria of Table 7, The test is judged to be 'no effect' if the decrease does not occur, and it is judged 'worse' when the test grade is higher than that before the test.

Prevention and improvement effect of essence on acne essence division Excellent effect Middle effect no effect Worse Side Effect Example 1 The test group (n = 50) 36 (72%) 12 (24%) 2 (4%) 0 0 Example 2 The test group (n = 50) 42 (84%) 7 (14%) 1 (2%) 0 0 Comparative Example Control group (n = 50) 0 5 (10%) 37 (74%) 8 (16%) 0 * Comparative Examples are those in which only the extract base is not added to the basic prescriptions of Examples 1 and 2

As shown in the above clinical results, Examples 1 and 2 according to the present invention were found to be superior to the Comparative Examples in improving acne.

Claims (3)

The present invention also relates to a method for producing an extract of willow bark, which comprises essentially extracting bokbunja and further containing willow extract as an active ingredient, and containing 0.001 to 20 wt.
Wherein the active ingredient is contained in a ratio of bergillus extract: willow extract = 1: 1 ~ 4 weight ratio. [Claim 2] The cosmetic composition for relieving inflammation of purulent acne according to claim 1, wherein the active ingredient has antibacterial action and anti-inflammatory action. A composition comprising the composition of claim 1,
Cleansing Lotion, Foaming Wash, Cleansing Foam, Cleansing Water, Cleansing Gel, Wash-off Pack, Peel-off, Lotion, Lotion, Essence, Nourishing Cream, Eye Cream, Massage Cream Such as a pack, a sheet-like mask pack, a hydrogel mask pack, a liposcel mask pack, a clay mask pack, a soap, a spray, a line cream, a sun lotion, a sunbath, a sun mist, a babe cream, a makeup base, A cosmetic composition for alleviating inflammation of purulent acne produced by a selected formulation.