KR20230100908A - Composition of skin external application for improving atopic dermatitis comprising allicin - Google Patents

Abstract

The present invention relates to a composition for topical skin application for the treatment of atopic dermatitis, and more particularly, is characterized in that it contains allicin and citron extract as active ingredients. According to the composition for topical skin application for the treatment of atopic dermatitis containing allicin of the present invention, it has the advantage of ultimately improving atopic dermatitis by suppressing the expression of TSLP and sterilizing staphylococcus aureus.

Description

Composition for external application for skin for treating atopic dermatitis containing allicin

The present invention relates to a composition for external application for skin for the treatment of atopic dermatitis, and more particularly, to a composition for external application for skin for the treatment of atopic dermatitis using allicin as an active ingredient.

Atopic dermatitis is a skin disease that represents a chronic inflammatory skin condition with severe itching, usually appearing in infancy and continuing into adulthood, or continuing throughout life. The induction rate is 10-20% in children and 1-3% in adults, which has increased 2-3 times over the past 30 years. Such atopic dermatitis can cause insomnia, emotional disorders, learning difficulties, and difficulties in social activities. It is known that complex factors such as immunological, physiological, and biochemical triggers are involved along with genetic factors. The cause has not been clearly identified (Park Young-lip et al., Journal of the Korean Skin Research Society, 2007, 14(3), 67-72).

Extrinsic dermatitis, which accounts for 70 to 80% of atopic dermatitis, is caused by IgE-related immune mechanisms, and in this case, there are many reports that a delayed immune response by T cell abnormality is involved. The infiltration of immune-related cells, such as macrophages, Th lymphocytes, and mast cells, greatly increases in areas where atopic dermatitis occurs. In the case of atopic dermatitis patients, the concentration of IgE in the blood is high in the skin of atopic dermatitis. This is because the number of Th2 cells increases and Th2 cytokines such as IL-4 and 13 secreted by these cells stimulate B lymphocytes to promote IgE secretion. am. Especially in the case of early atopic dermatitis, IL-4 and IL-13 are important (Donald YM Leung et al, J Clin Invest 2004, 113, 651-657).

According to recent reports, thymic stromal lymphopoietin (TSLP) is known to play an important role in atopic dermatitis. This is known as a factor specific to atopic dermatitis because the concentration of TSLP increases in keratinocytes of patients with atopic dermatitis, whereas the concentration is similar to normal in other dermatitis patients. TSLP is increased by increased pro-inflammatory cytokine and Th2 cytokine in keratinocytes exposed to physical and chemical stimuli (Eric B Brandt etal J Clin Cell Immunol, 2011, 2(3)). The increased TSLP activates CD11c+ dendritic cells, and the activated dendritic cells promote the secretion of Th2 cytokines, including thymus and activation-regulated chemokine (TARC) and macrophage-derived chemokine (MDC) from T cells (Sarah R et al. al, Cell, 155, 285-295).

In addition, Staphylococcus aureus has also been reported as one of the causes of atopic dermatitis.

For the treatment of atopic dermatitis, moisturizers are applied consistently, and in severe cases, steroid ointments or antihistamines are prescribed. Although this has the effect of temporarily relieving symptoms, long-term use of steroid hormones may cause skin atrophy or dilation of capillaries, and may cause side effects such as weakening of the skin barrier function and inducing osteoporosis. Therefore, there is a demand for the development of a new mechanism of atopic treatment with fewer side effects while having excellent effects in atopy treatment.

Meanwhile, allicin is a representative component of garlic, and allin is converted into allicin by allinase. Allicin has strong bactericidal, antibacterial, whitening, and antioxidant activities, and has higher efficacy when combined with carbohydrates, lipids, and proteins. This allicin is included in a lot of lily plants such as garlic, onion, green onion, leek, and wild chives.

The allicin is widely used in various cosmetic compositions due to its strong bactericidal and antibacterial action, whitening action and antioxidant activity.

However, there was no example applied to improve atopic dermatitis anywhere in the prior literature.

KR 10-1458758 B1 KR 10-2316909 B1

Therefore, an object of the present invention is to suppress the expression of TSLP, a cytokine that acts as one of the causes of atopic dermatitis, and to inhibit the activity of Staphylococcus aureus, thereby treating atopic dermatitis containing allicin having an effect of improving atopic dermatitis It is to provide a composition for external application for skin.

A composition for external application for skin for treating atopic dermatitis containing allicin to achieve the above object is characterized by containing allicin and citron extract as active ingredients.

The active ingredient is characterized by inhibiting the expression of TSLP (thymic stromal lymphopoietin), which is one of the causes of atopic dermatitis.

The active ingredient is characterized by having antibacterial activity against Staphylococcus aureus, which is one of the causes of atopic dermatitis.

It is characterized in that it further comprises a pink celandine extract as an active ingredient.

Characterized in that it further comprises olive liquid, hyaluronic acid, nucleic acid, ethanol and distilled water.

It is characterized in that it comprises 10 to 30 parts by weight of citron extract with respect to 100 parts by weight of allicin.

According to the composition for topical skin application for the treatment of atopic dermatitis containing allicin of the present invention, it has the advantage of ultimately improving atopic dermatitis by suppressing the expression of TSLP and sterilizing staphylococcus aureus.

1 to 3 are graphs showing the results of Test Example 1 according to the present invention.

Hereinafter, the present invention will be described in more detail.

Most of the conventional external preparations for treating atopic dermatitis have a moisturizing effect, and there is a limit to improving atopic dermatitis only with such a moisturizing effect. The greatest feature of the present invention is that it can ultimately improve atopic dermatitis by inhibiting the expression of TSLP and sterilizing Staphylococcus aureus.

The composition for external application for skin for treating atopic dermatitis of the present invention is characterized by containing allicin and citron extract as active ingredients.

First, allicin is a representative component of garlic, and allin is converted into allicin by allinase. Allicin has strong bactericidal and antibacterial effects.

Allicin is included in many Liliaceae plants such as garlic, garlic, onion, green onion, chives, and wild chives. In the present invention, artificially prepared allicin may be used, but natural allicin extracted from the lily family plant may also be used, and in particular, the juice of the lily family plant, most preferably garlic juice, is preferably used as a source of allicin. can

The citron extract has excellent anti-inflammatory action and helps to obtain an atopic treatment effect by rich vitamin organic acids. Compared to other citrus fruits, citron is rich in vitamins B1, B2, C, various organic acids, carbohydrates, and proteins, as well as limonoid and anti-inflammatory substances known to have excellent anti-cancer effects. It is rich in hesperidin, which is known to have antibacterial and antibacterial properties. In particular, since allicin has a higher bactericidal and antibacterial effect by combining with carbohydrates and proteins, the effect is maximized when used in combination with citron extract.

In the present invention, the extraction method of the citron extract is not limited, and water, ethanol or a mixed solvent thereof is added to citron fruits in an amount of 2 to 10 times the volume, extracted at 20 to 100 ° C for 2 to 10 hours, filtered, concentrated and dried It can be manufactured by It goes without saying that various methods known in the art can be used for the filtration, concentration and drying methods.

The citron extract may be included in 10 to 30 parts by weight based on 100 parts by weight of allicin. If it is less than 10 parts by weight, the effect of improving atopic dermatitis is insignificant, and even if it exceeds 30 parts by weight, no further enhanced effect can be obtained. .

In the present invention, when the allicin and the citron extract are included together as active ingredients, the expression of TSLP, a cytokine that acts as one of the causes of atopic dermatitis, can be significantly suppressed compared to using the allicin alone, and other causes It can exert strong antibacterial activity against Staphylococcus aureus.

That is, the composition for external application for skin for treating atopic dermatitis, which contains allicin and citron extract as active ingredients according to the present invention, inhibits the expression of TSLP (thymic stromal lymphopoietin), one of the causes of atopic dermatitis, and other causes of atopic dermatitis. It has strong antibacterial activity against Staphylococcus aureus, which is one of them, and has the advantage of fundamentally improving atopic dermatitis.

In addition, the composition for external application for skin for treating atopic dermatitis according to the present invention preferably further includes an extract of celandine oleifera as an active ingredient.

When only the allicin and citron extracts are included as active ingredients, sufficient moisturizing effect is not provided, and when using external preparations, there may be irritation such as skin irritation at the beginning of application. , skin irritation can also be alleviated.

The pink Arabidopsis (Binghamia californica J Agardh) is a seaweed of the red algae plant pink algae family, and grows in the lower intertidal zone. The plant body is membranous, pink, and several flat stems come out from the string-shaped thin roots.

The extraction method of the pink Arabidopsis extract is not limited, and water, ethanol or a mixed solvent thereof is added to the pink Arabidopsis in an amount of 2 to 10 times by volume, extracted at 20 to 100 ° C. for 2 to 10 hours, filtered, concentrated, and dried. there is. The filtration, concentration and drying methods use various methods known in the art.

The pink Arabidopsis extract is preferably included in an amount of 10 to 20 parts by weight based on 100 parts by weight of allicin. because it can

In addition, the composition for external application for skin for treating atopic dermatitis of the present invention may further include olive liquid, hyaluronic acid, nucleic acid, ethanol, and distilled water.

The olive liquid is sodium PEG-7 olive oil carboxylate, which provides proper moisturizing without irritating the skin and functions as a natural emulsifier. Therefore, olive liquid also plays a role in ensuring allicin and other components are well mixed without being separated.

The nucleic acid is the main body of the gene present in the cells of all organisms, promotes metabolism, has excellent antioxidant action, prevents aging, enhances skin regeneration, and is also excellent in anti-inflammatory and wound healing effects. . Thus, it heals wounds caused by atopic dermatitis.

The hyaluronic acid (hyaluronic acid) is a natural polymer that is present in the skin of animals and the like, and is present in vivo in the epidermis, cartilage, vitreous humor of the eye, synovial fluid of the joint, etc., to maintain the structure of the skin and to function normally Plays an important role.

The ethanol (ethanol) disinfects the wound and functions to prevent deterioration of the composition according to the present invention. In addition, when the composition for the present invention is applied to the skin, it volatilizes and lowers the feeling of heat, thereby reducing pain, itching, and the like.

And distilled water controls the overall concentration and viscosity of the composition.

At this time, the content includes 200 to 300 parts by weight of olive liquid, 1 to 10 parts by weight of nucleic acid, 1 to 10 parts by weight of hyaluronic acid, 100 to 500 parts by weight of ethanol, and 50 to 150 parts by weight of distilled water, based on 100 parts by weight of allicin. However, this is not necessarily limited.

In the present invention, the composition for external use is skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisture lotion, nutrient lotion, massage cream, nutrient cream, moisture cream, hand cream, ointment, foundation, essence, nutrient essence , It may have one or more formulations selected from the group consisting of packs, soaps, cleansing foams, cleansing lotions, cleansing creams, body lotions and body cleansers, but is not limited thereto. In addition, it can be applied in various forms such as liquid, cream, paste, and solid.

In addition, various additives known in the art to which this technology belongs may be added for the formulation, but are not limited thereto. In addition, when formulating, the total active ingredient including allicin may be included in 5 to 100% by weight based on 100% by weight of the total composition, but it is also noted that this is not limited.

Hereinafter, the present invention will be described in detail through specific examples.

(Example 1)

100 g of allicin and 20 g of citron extract were mixed.

At this time, garlic juice was used as the allicin, and for the citron extract, citron fruit was crushed, 5 times the volume of 50% ethanol was added thereto, and reflux-cooled hot water extraction was performed three times for 3 hours at 80 ° C., An extract was prepared by concentrating with a vacuum concentrator at 40°C and drying.

(Example 2)

It was carried out in the same manner as in Example 1, but 20 g of the pink Arabidopsis extract was further mixed.

After adding 5 times the volume of 50% ethanol to the pink Arabidopsis extract, extracting with reflux cooling hot water three times for 3 hours at 80 ° C., concentrating with a vacuum concentrator at 40 ° C., and drying to prepare an extract did

(Test Example 1)

TSLP, MDC, TARC inhibition test

Thymic stromal lymphopoietin (TSLP) is classified as the top cytokine that initiates type 2 helper T cell-mediated immune bias identified as the cause of atopic dermatitis. MDC and TARC are inflammatory chemokines and are subfactors of TSLP.

In order to confirm the reducing effect of Examples 1 and 2 on the expression of cytokines and chemokines generated in human keratinocytes HaCaT, the expression level of each gene was evaluated.

HaCaT keratinocytes, a constitutive cell line of human skin, were cultured using DMEM medium containing 10% fetal bovine serum (FBS) and antibiotics. A 75T-flask and a 6 well plate were used for the culture vessel, and culture was performed in a 37°C incubator supplied with 5% CO ₂ . The culture medium was exchanged every 3 to 4 days, and subculture was performed when the cells proliferated excessively. Cells were dispensed into a 6-well plate, washed with phosphate buffered saline (PBS) after 24 hours of culture, and samples were placed in DMEM medium without FBS in each well along with Poly I:C and IL-4. It was diluted to a final concentration of 10 ppm and added to each well. The positive control group was treated with dexamethasone 1uM. After 4 hours, cDNA was synthesized and PCR was performed to evaluate the level of gene expression.

The synthesized cDNA was subjected to real-time polymerase chain reaction (PCR) using a target template (primer) and a cyanine dye, SYBR green master mix, to determine the final level of TSLP gene expression. evaluated. Expression of the genes was compared as a relative value through correction quantification of the internal control gene β-actin by the Ct (threshold cycle) method.

As a result, as shown in FIGS. 1 to 3, it was confirmed that TSLP, MDC, and TARC overexpressed by poly I:C and IL-4 were significantly suppressed by sample treatment.

Therefore, it was confirmed that Examples 1 and 2 of the present invention can treat and improve atopic dermatitis by inhibiting the expression of TSLP, which is directly or indirectly related to atopic dermatitis.

(Test Example 2)

Antibacterial activity against Staphylococcus aureus

In order to evaluate the antibacterial activity against Staphylococcus aureus KACC10768, a pathogenic strain that causes secondary infection of atopic dermatitis, a paper disc method was used with gentamicin as a control. .

For quantitative evaluation of antibacterial activity, soybean casein digest agar medium (Tryptic soy agar 0.7%, casein peptone 15.0 g, soy peptone 5.0 g, sodium chloride 5.0 g, purified water 975 g, pH 7.2±0.1) for Staphylococcus aureus culture 100 μl of Staphylococcus aureus strain was added, and 50 μl of each sample was treated on a filter paper disc (9 mm). Thereafter, by culturing at 37 ° C for 48 hours, the diameter of the antibacterial activity range in which the strain did not proliferate was converted into units (the diameter of the antibacterial activity range of 10 mg / ml of gentamicin was defined as 1 unit) to confirm the antibacterial activity. did And the results are shown in Table 1 below.

Test Example 2 Results division Diameter (mm) unit Gentamicin 12 1.00 Example 1 20 1.66 Example 2 21 1.75 Comparative Example 1 12 1.00

As can be seen in Table 1, the diameter of the antimicrobial activity range of the control group, gentamicin, was 12 mm, and as a result of comparing it by defining it as 1 unit, it can be confirmed that Examples 1 and 2 exhibit excellent antibacterial activity. could

Therefore, it was confirmed that Examples 1 and 2 of the present invention can be usefully used for the purpose of atopic dermatitis and its secondary infection or improvement.

(Example 3)

Allicin 100g, citron extract 20g, olive liquid 250g, nucleic acid 5g, hyaluronic acid 5g, ethanol 300g and distilled water 100g were mixed. At this time, allicin and citron extracts were prepared in the same manner as in Example 1.

(Example 4)

It was carried out in the same manner as in Example 3, but 20 g of celandine extract was further mixed. At this time, the pink Arabidopsis extract was prepared in the same manner as in Example 2.

(Test Example 3)

For 30 adult men and women with atopic dermatitis, Examples 1 and 2 and the control group were distributed, and 1 ml was applied to the affected area twice a day for 10 days (divide the affected area into 3 areas per subject and apply each sample) ) was tested by the method. After application for 10 days, the atopy improvement effect, the degree of skin irritation, and the moisturizing effect were evaluated, and the results are shown as average values in Table 2 below. As a control group, a commercially available moisturizing cream for atopy was provided.

Test Example 2 Results division atopy improvement degree of skin irritation Moisturizing overall satisfaction Example 1 4.2 4.6 3.0 4.5 Example 2 4.7 5.0 4.3 4.7 control group 2.8 5.0 4.0 3.1 5: Great improvement, or no irritation at all.
4: Slight improvement, or slight irritation.
3: No improvement, or moderate irritation.
2: Slight aggravation, or severe irritation.
1: Cannot be used due to severe aggravation or severe irritation.

As shown in Table 2, it was confirmed that Examples 1 and 2 of the present invention had excellent atopic dermatitis improvement effects compared to the control group.

From the above description, those skilled in the art to which this application pertains will be able to understand that this application can be implemented in other specific forms without changing its technical spirit or essential features. In this regard, it should be understood that the embodiments described above are illustrative in all respects and not limiting. The scope of the present application should be construed as including all changes or modifications derived from the meaning and scope of the claims to be described later and equivalent concepts rather than the detailed description above are included in the scope of the present application.

Claims (6)

A composition for topical skin application for the treatment of atopic dermatitis containing allicin, characterized in that it contains allicin and citron extract as active ingredients.
According to claim 1,
The active ingredient,
A composition for topical skin application for treating atopic dermatitis containing allicin, characterized in that it inhibits the expression of TSLP (thymic stromal lymphopoietin), which is one of the causes of atopic dermatitis.
According to claim 1,
The active ingredient,
A composition for topical skin application for the treatment of atopic dermatitis containing allicin, characterized by having antibacterial activity against Staphylococcus aureus, one of the causes of atopic dermatitis.
According to any one of claims 1 to 3,
A composition for topical skin application for the treatment of atopic dermatitis containing allicin, further comprising an extract of pink celandine as an active ingredient.
According to any one of claims 1 to 3,
A composition for topical skin application for treating atopic dermatitis containing allicin, further comprising olive liquid, hyaluronic acid, nucleic acid, ethanol and distilled water.
According to claim 1,
A skin external composition for treating atopic dermatitis containing allicin, characterized in that it comprises 10 to 30 parts by weight of citron extract based on 100 parts by weight of allicin.

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