KR102436291B1 - Cosmetic Composition for Skin Whitening Containing Eleutheroside E As Active Ingredient - Google Patents

Abstract

The present invention provides a cosmetic composition containing eluteroside E as an active ingredient. The eluteroside E is a single component or isolated from a plant belonging to the genus oleracea, and it suppresses melanin production by inhibiting the activity of tyrosinase, a melanin synthetase, and the expression of tyrosinase, TRP-1, and TRP-2, resulting in excellent whitening. Having an effect, the present invention provides a cosmetic composition for skin whitening comprising the same.

Description

A cosmetic composition for skin whitening containing eluteroside E as an active ingredient {Cosmetic Composition for Skin Whitening Containing Eleutheroside E As Active Ingredient}

The present invention relates to a cosmetic composition for skin whitening containing eleutheroside E as an active ingredient.

Several factors are involved in determining a person's skin color. There are factors such as the activity of melanocytes that make melanin pigment, the distribution of blood vessels, the thickness of the skin, and the presence or absence of pigments inside and outside the human body such as carotenoids and bilirubin. Among them, a representative factor is due to the exposure of the skin to ultraviolet rays. That is, when the skin is exposed to ultraviolet rays, tyrosinase is activated, which acts on tyrosine, a kind of amino acid present in the skin tissue, to generate dopa, and then through the oxidation process to generate dopaquinone, skin pigment. A polymer called melanin is synthesized in melanosomes in the melanocytes, which are cells. This melanin is transferred to keratinocytes, which are keratinocytes of the skin, and reaches the skin surface by the keratinization process to protect the skin from UV rays.

Melanin is an essential UV protection agent for our human body and plays a role as an effective free radical scavenger to remove various radicals that modify biocomponents such as proteins, lipids, and nucleic acids. However, when melanin is locally synthesized excessively or the physiological function of the skin is deteriorated due to skin lesions and aging, melanin is deposited on the skin surface, causing melasma, freckles and various pigmentation.

As the cause and mechanism of skin blackening have been revealed, a method of reducing the production of melanin by mixing substances having an inhibitory effect on the activity of tyrosinase, which is involved in the skin blackening process, into cosmetics, or by inhibiting some reactions in the process of melanin production It is commonly used to prevent skin darkening. Representative substances used for this purpose include plant extracts such as arbutin, ascorbic acid, hydroquinone, sagebrush extract and licorice extract.

However, in the case of arbutin, while it has an excellent tyrosinase activity inhibitory action, it has problems in stability such as discoloration and a decrease in potency due to changes over time when formulated in cosmetics, and has a limitation in use due to large skin irritation. Ascorbic acid has a low tyrosinase activity inhibitory effect and is not suitable as a melanogenesis inhibitor due to low molecular stability. Hydroquinone has a high irritation to the skin, so there is a problem in that its usability is limited in the current cosmetic formulation due to safety issues. In addition, most plant extracts exhibit a relatively high tyrosinase activity inhibitory effect only at a high concentration, and have problems such as almost no inhibitory effect at a low concentration. In particular, the existing inhibitors of melanin production have the biggest problem that the whitening effect is weak during clinical trials on actual human skin.

Therefore, there is a demand for the development of a material that ensures stability and safety while exhibiting an excellent whitening effect in the human body, and thus, a whitening composition based on a natural product with few side effects is attracting attention.

Korean Patent No. 10-1536231 discloses a technology related to a composition for preventing or treating insulin resistance or insulin resistance-related diseases including eluteroside E. In addition, Korean Patent Registration No. 10-1768097 discloses a technology related to an extraction method capable of simultaneously extracting eluteroside E and beta-glucan, which are functional components of S.

An object of the present invention is to provide a cosmetic composition for skin whitening containing eluteroside E as an active ingredient. Specifically, a cosmetic composition that contains eluterosite E isolated from various natural products as an active ingredient, inhibits the expression of melanin synthetase acting in the melanin synthesis process, and inhibits melanin production to help skin whitening intended to provide

The above object is achieved by a cosmetic composition for skin whitening, characterized in that it contains eluteroside E as an active ingredient.

Preferably, the eluteroside E may be isolated from ginseng, red ginseng, or a plant of the genus Ogaryophyllum selected from the group consisting of S. oleifera, oleracea, and oleracea.

Also preferably, the eluteroside E may inhibit melanin production by inhibiting the activity and expression of melanin synthetase.

Also preferably, the eluteroside E may be included in an amount of 0.001 to 30.0% by weight based on the total weight of the cosmetic composition.

The cosmetic composition of the present invention exhibits an excellent effect on skin whitening.

1 is a result confirming the inhibitory effect of eluteroside E on tyrosinase activity.
2 is a result confirming the inhibitory effect of eluteroside E on melanin production.
3 is a result confirming the inhibitory effect of eluteroside E on the expression of tyrosinase, TRP-1, and TRP-2.

All technical terms used in the present invention, unless otherwise defined, have the following definitions and have the meanings as commonly understood by one of ordinary skill in the art of the present invention. In addition, although preferred methods and samples are described herein, similar or equivalent ones are also included in the scope of the present invention.

The term "about" means 30, 25, 20, 15, 10, 9, 8, 7, 6, 5, means an amount, level, value, number, frequency, percentage, dimension, size, amount, weight or length varying by 4, 3, 2 or 1%.

Throughout this specification, unless the context requires otherwise, the terms "comprises" and "comprising" include the steps or elements presented, or groups of steps or elements, but include any other step or element, or It is to be understood that a step or group of elements is meant to be implied not to be excluded.

The present invention provides a cosmetic composition for skin whitening comprising eluteroside E as an active ingredient.

Preferably, the cosmetic composition of the present invention contains eluteroside E as an active ingredient, thereby inhibiting the activity of tyrosinase, a melanin synthetase, and the expression of tyrosinase, TRP-1, and TRP-2 to suppress melanin production. By reducing it, an excellent effect on skin whitening can be exhibited.

The above, eluteroside E is known to be identified together with eluteroside B in ginseng, red ginseng, or plants belonging to the genus Arachnidae belonging to the family Araliaceae, such as S. In addition, eluteroside E is effective in anti-fatigue, anticancer, heart disease protection, antioxidant, liver function enhancement, etc., and inhibits nuclear factor NF-κB and acivator protein-1 (AP-1), important factors involved in inflammation. It is reported to have an anti-inflammatory action, and it is known that it is effective in strengthening immunity by activating immune cells. Eluteroside E used in the present invention may be isolated from or synthesized from ginseng, red ginseng, or a plant selected from the group consisting of oleracea, oleracea, and oleracea.

The eluteroside E has a structure represented by the following formula (1).

In the present invention, eluteroside E may be contained in an amount of 0.001 wt% to 30.0 wt%, more specifically 0.01 wt% to 10 wt%, based on the total weight of the cosmetic composition. When the content of Eluteroside E is less than 0.001% by weight, the skin whitening improvement effect does not appear, and when it exceeds 30.0% by weight, the degree of increase in the skin whitening improvement effect with increasing the content is insignificant, and safety and stability in formulation There is a problem with it, and it is not economical.

The cosmetic composition of the present invention may include components commonly used in the cosmetic composition, for example, it includes conventional adjuvants such as antioxidants, stabilizers, solubilizers, vitamins, pigments and fragrances, and carriers.

The cosmetic composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil , powder foundation, emulsion foundation, wax foundation, pack, massage cream, spray, etc., but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, a nourishing lotion, a nourishing cream, a massage cream, an essence, an eye cream, a cleansing cream, a cleansing foam, a cleansing water, a pack, a spray, or a powder.

In the cosmetic composition of the present invention, when the formulation is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tragacanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or Zinc oxide and the like may be used.

In the cosmetic composition of the present invention, when the formulation is a solution or emulsion, a solvent, solubilizer or emulsifier is used as a carrier component, for example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzo Acid, propylene glycol, 1,3-butylene glycol oil, glycerol aliphatic ester, polyethylene glycol or fatty acid ester of sorbitan may be used.

In the cosmetic composition of the present invention, when the formulation is a suspension, as a carrier component, a liquid diluent such as water, ethanol or propylene glycol, ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, and polyoxyethylene sorbitan ester, such as Suspending agents, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar or tragacanth and the like can be used.

In the cosmetic composition of the present invention, when the formulation is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. propellants such as hydrohydrocarbons, propane/butane or dimethyl ether.

In the cosmetic composition of the present invention, when the formulation is surfactant-containing cleansing, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, sarcosinate, fatty acid amide as carrier components Ether sulfate, alkylamidobetaine, fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative or ethoxylated glycerol fatty acid ester and the like can be used.

In the cosmetic composition of the present invention, in the case of a surfactant-containing cleansing formulation or a surfactant-free cleansing formulation or soap, it may be applied to the skin and then wiped off, removed, or washed off with water. For example, the soap is liquid soap, powder soap, solid soap, and oil soap, the surfactant-containing cleansing formulation is a cleansing foam, cleansing water, cleansing towel and cleansing pack, and the surfactant-free cleansing formulation is a cleansing cream, cleansing lotions, cleansing waters and cleansing gels, but not limited thereto.

The cosmetic composition of the present invention may be used overlapping with other cosmetic compositions other than the present invention. In addition, the cosmetic composition according to the present invention can be used according to a conventional method of use, and the number of times of use can be changed according to the skin condition or taste of the user.

Hereinafter, the content of the present invention will be described in more detail in the following examples, but the scope of the present invention is not limited to the following examples, and includes modifications of technical ideas equivalent thereto.

Experimental Example 1: Effect of Eluteroside E on Inhibiting Tyrosinase Activity

In this experiment, the inhibitory effect of eluteroside E on tyrosinase activity was investigated.

Tyrosinase is an enzyme that promotes the oxidation process of a substance called tyrosine in a living body to produce melanin. Tyrosinase was dissolved in 0.05 M sodium phosphate buffer (pH 6.8) to 1200 unit/ml, and L-tyrosine, a substrate, was dissolved in 0.05 M sodium phosphate buffer (pH 6.8) to make 1.5 mM. 50 ul of L-tyrosine, 10 μl of tyrosinase, 20 μl of eluteroside E, 220 μl of 0.05 M sodium phosphate buffer (pH 6.8) were added, and then reacted for 10 minutes in an incubator at 37°C. Absorbance was measured at 490 nm. As a positive control, kojic acid was used. At this time, the activity inhibition rate (%) for tyrosinase was calculated by Equation 1 below, and the results are shown in FIG. 1 and Table 1 below.

sample Tyrosinase activity inhibition rate (%) Eluteroside E 25 uM 0.73 50 uM 12.32 100 uM 20.59 200 uM 32.88 Kojic acid (200 uM) 69.07

1 and Table 1, eluteroside E inhibited the activity of tyrosinase in a concentration-dependent manner and inhibited the activity of tyrosinase by up to 32.88% at a concentration of 200 μM. In the case of kojic acid as a positive control, the activity of tyrosinase was inhibited by 69.07%.

Experimental Example 2: Effect of Eluteroside E on Melanin Generation Inhibition

In this experimental example, in order to confirm the inhibitory effect of eluteroside E on melanin biosynthesis, the degree of melanogenesis inhibition was investigated using B16F10 melanin-forming cells. At this time, arbutin, a well-known whitening agent, was used as a positive control.

B16F10 melanin-forming cells were aliquoted in a 96-well plate at a concentration of 2.5×10 ³ per well, and stabilized in a 37° C. incubator for one day. Eluteroside E was diluted by concentration and treated at concentrations of 25, 50, 100, and 200 μM, and α-MSH was treated at a concentration of 150 nM, followed by reaction in an incubator at 37° C. for 72 hours. After 72 hours, the amount of melanin was confirmed by measuring the absorbance at 405 nm, and 20 μl of MTT reagent at a concentration of 5 mg/ml was added to each well for cell viability analysis. After reacting in an incubator at 37° C. for 1 hour, all of the supernatant was removed, and 100 μl of DMSO was added to completely lyse the cells. Cell viability was confirmed by measuring the absorbance at 550 nm. Melanin production inhibition rate (%) was calculated by Equation 2 below, and the results are shown in FIG. 2 and Table 2.

A: Absorbance value of the well to which no sample was added

B: Absorbance value of wells treated with stimulant (α-MSH)

C: Absorbance value of the well to which the sample was added

sample Melanin production inhibition rate (%) Eluteroside E 25 uM 0.24 50 uM 15.86 100 uM 42.04 200 uM 69.31 Arbutin (50 ug/ml) 66.88

As a result of the experiment, as shown in FIG. 2 and Table 2, eluteroside E inhibited melanin production in a concentration-dependent manner, and when 200 μM was treated, it was 69.31%, indicating a higher melanin production inhibition rate than 66.88% of arbutin, a positive control. Confirmed.

Experimental Example 3: Effect of inhibiting the expression of melanin synthase of eluteroside E

B16F10 cells were seeded in a 6-well plate at 3 x 10 ⁵ cells/well, and the cells were stabilized for one day in a 37 ^o C, 5% CO ₂ incubator. After treatment by diluting eluteroside E by concentration, α-MSH, a stimulant, was treated at a concentration of 150 nM. After reacting in an incubator at 37 ^o C, 5% CO ₂ for 48 hours, the protein was isolated. The supernatant was removed, washed once with 1 x PBS, and scraped with a scraper to collect cells. Proteins were isolated using cell lysis buffer, proteins were quantified by BCA assay, and a certain amount of proteins was electrophoresed on a 10% SDS-PAGE gel. The separated protein on the gel was transferred to a PVDF membrane and blocked for 1 hour using 5% skim milk. After washing 3 times with 1 x TTBS solution and reacting the primary antibody at 4 ^o C overnight (over night), the HRP-conjugated secondary antibody was reacted at room temperature for 2 hours. Thereafter, the band was detected with a Chemi Doc instrument by washing 3 times with 1 x TTBS and reacting the ECL solution. Beta-actin (β-actin) expression was quantified based on the expression level of melanin synthetase (tyrosinase, TRP-1, TRP-2) was calculated and quantified using Image J 1.47 software (Table 3). As a positive control, arbutin was used.

melanin synthase sample density Expression inhibition rate (%) Tyrosinase Eluteroside E (μM) 50 18.37 100 47.76 200 60.19 Arbutin (μg/ml) 50 53.86 TRP-1 Eluteroside E (μM) 50 15.14 100 43.81 200 49.04 Arbutin (μg/ml) 50 50.87 TRP-2 Eluteroside E (μM) 50 42.78 100 52.50 200 61.97 Arbutin (μg/ml) 50 43.96

As a result of the experiment, as shown in FIG. 3 and Table 3, eluteroside E inhibited the expression of tyrosinase, TRP-1, and TRP-2 in a concentration-dependent manner. In particular, when 200 μM was treated, the expression of tyrosinase, TRP-1, and TRP-2 was confirmed as high as 60.19%, 49.04%, and 61.97%, respectively. Compared to the positive control arbutin, eluteroside E showed similar or more inhibitory effects.

Through this, it was confirmed that eluteroside E of the present invention exerts an excellent whitening effect by inhibiting melanin production by inhibiting the activity of tyrosinase, a melanin synthesizing enzyme, and the expression of melanin synthesizing enzyme.

Claims (4)

A cosmetic composition for skin whitening, comprising eleutheroside E as an active ingredient, wherein the eluteroside E is included in an amount of 0.001 to 30.0% by weight based on the total weight of the cosmetic composition. The cosmetic composition for skin whitening according to claim 1, wherein the eluteroside E is isolated from ginseng, red ginseng, or a plant selected from the group consisting of ginseng, oleracea, and oleracea. The cosmetic composition for skin whitening according to claim 1, wherein the eluteroside E inhibits melanin production by inhibiting the activity and expression of melanin synthetase. delete

Images