KR102249430B1 - Composition for whitening, anti-wrinkle or moisturizing comprising Cocos nucifera extract - Google Patents

Abstract

Skin whitening containing coconut extract, anti-wrinkle, or coconut house thorium (Coconut haustorium) extract or germination around the coconut (Cocos nucifera) germ extract in accordance with that, an aspect relates to a moisturizing composition for tyrosinase and / or Elastigirl In addition to exhibiting the inhibitory activity of the enzyme, it has a skin moisturizing effect, so that it can be usefully used in a composition for skin whitening, anti-wrinkle, and/or skin moisturizing.

Description

Composition for whitening, anti-wrinkle, or moisturizing skin containing coconut extract {Composition for whitening, anti-wrinkle or moisturizing comprising Cocos nucifera extract}

It relates to a composition for skin whitening, anti-wrinkle, or moisturizing containing coconut extract.

Melanin plays a role in protecting the skin from UV rays, but when excessively produced, pigmentation is deposited on the skin to form spots and freckles, and in severe cases, it can cause skin cancer. Therefore, in order to prevent pigmentation of the skin, it is necessary to reduce melanin production by inhibiting a part of the melanin production process. Melanin is a high molecular weight natural pigment of phenols that is widely present in animals, plants and microorganisms, and is synthesized from melanosomes in melanocytes present in the base layer of the epidermis. Melanin is synthesized by a continuous oxidation reaction of L-tyrosine. L-tyrosine is converted to L-DOPA (3,4-dihydrozyphenylalanine) by tyrosinase, and L-DOPA is phenyl. It is oxidized to anani-3,4-quinone, and finally becomes melanin through an intermediate metabolite. Therefore, in order to develop a material for functional cosmetics related to skin whitening, it is important whether the material inhibits the activity of tyrosinase.

In addition, because the skin has many opportunities to come into contact with various external stimuli, wrinkles are more likely to occur than other organs. Among them, facial skin is directly exposed to sunlight, dry air, and pollutants, so aging phenomena such as wrinkles occur earlier than skin that does not. The most characteristic change according to aging of the skin tissue is the change of the skin matrix, and the human skin fibroblast in the dermal layer is aged, reducing the ability to produce fibers and matrix. As the amount of the substrate decreases overall, the thickness of the skin becomes thinner, and the elasticity of the skin decreases, forming wrinkles. In other words, as the aging progresses, the skin becomes more severely deteriorated in elasticity, impaired blood circulation, and weakened skin barrier.

Therefore, in recent years, researches for the development of cosmetic materials using natural products are being actively conducted, and there is an increasing demand for the development of materials that are safe for skin and have whitening effect and wrinkle activity.

One aspect is to provide a cosmetic composition for skin whitening, anti-wrinkle, or skin moisturizing containing a coconut haustorium extract or a coconut before germination ( Cocos nucifera) germ extract.

Another aspect is to provide an external preparation for skin for skin whitening, anti-wrinkle or skin moisturizing, containing a coconut haustorium extract or a pre-emergence coconut ( Cocos nucifera) embryo extract.

Another aspect is to provide a pharmaceutical composition for skin whitening, anti-wrinkle, or skin moisturizing containing a coconut haustorium extract or a pre-germination coconut ( Cocos nucifera) germ extract.

One aspect provides a composition for skin whitening, anti-wrinkle, or skin moisturizing containing a coconut haustorium extract or a coconut before germination ( Cocos nucifera) germ extract.

As used herein, "Coconut haustorium" is used interchangeably with "an embryo of a coconut or a portion thereof after germination", and refers to a sponge absorbent tissue formed from the distal end of the embryo during the germination of the coconut. It can mean.

As used herein, the term "active ingredient" or "effective amount" refers to any amount of a composition used in the practice of the invention provided herein sufficient to alleviate, inhibit or prevent progression of a disease, disorder or condition, or one or more symptoms thereof. Can mean

As used herein, the terms "administering," "applying", and "introducing" are used interchangeably and into a subject by a method or route that results in at least partial localization of a composition according to one embodiment to a desired site. It may mean the arrangement of the composition according to one embodiment of.

The extract may be extracted using water, alcohol, for example, C1-C6 alcohol, for example, C1-C4 alcohol, or a mixture thereof as a solvent. The C1-C6 alcohol may be methanol, ethanol, propanol, isopropanol, 1,3-propanediol, butanol, pentanol, hexanol, and the like. The solvent may be, for example, a mixture of water and alcohol, that is, an aqueous alcohol solution. The alcohol concentration of the aqueous alcohol solution is 1 to 99.5 (v/v)%, for example, 10 to 99.5 (v/v)%, 1 to 70 (v/v)%, 1 to 40 (v/v)%, 5 to 25 (v/v)%, 7 to 20 (v/v)%, 5 to 25 (v/v)%, or 10 to 20 (v/v)%. The aqueous alcohol solution may be an aqueous ethanol solution.

The extraction is performed by 3 to 10 (vol/w) times, for example, 3 to 7 (vol/w), of the extraction solvent with respect to the whole, a part of the coconut, or a material derived therefrom, or a coconut embryo before germination. It may include adding weight) times, 3 to 5 (volume/weight) times, 5 to 10 (volume/weight) times, or 4 to 10 times. For example, it may include adding 3 to 10 L of the extraction solvent to 1 kg of the outpost of the phosphorus or rhubarb, a portion thereof, or a material derived therefrom.

The extraction is performed by warmed liquid extraction, pressurized liquid extraction (PLE), microwave assisted extraction (MAE), subcritical extraction (SE), or a combination thereof. Can be. The subcritical extraction may be subcritical water extraction (SWE). Subcritical water extraction is also referred to as superheated water extraction or pressurized hot water extraction (PHWE). The heated liquid extraction may be reflux extraction.

The extraction is 4 ℃ to 70 ℃, for example, 4 ℃ to 50 ℃, 4 ℃ to 40 ℃, 4 ℃ to 30 ℃, 10 ℃ to 70, 15 ℃ to 70, 20 ℃ to 70 ℃, 4 ℃ to It may be performed at 50°C, 10°C to 50°C, 4°C to 40°C, 4°C to 30°C, 10°C to 40°C, 10°C to 35°C, or 10°C to 30°C. The extraction time may vary depending on the selected temperature, for example, 1 hour to 2 months, for example, 1 hour to 1 month, 1 hour to 15 days, 1 hour to 10 days, 1 hour to 5 days, 1 hour to 3 days. , 1 hour to 2 days, 1 hour to 1 day, 5 hours to 1 month, 5 hours to 15 days, 5 hours to 10 days, 5 hours to 5 days, 5 hours to 3 days, 5 hours to 2 days, 5 It may be time to 1 day, 10 hours to 1 month, 10 hours to 15 days, 10 hours to 10 days, 10 hours to 5 days, 10 hours to 3 days, or 10 hours to 2 days. The extraction may include mixing the whole of the coconut Huis Thorium, a portion thereof, or a material derived therefrom, or a coconut embryo before germination in the solvent, and leaving it for a predetermined time. The standing may include suitable agitation. The extraction may be repeated one or more times, for example, 1 to 5 times.

The extraction may be performed by separating plant residues and extracts by known methods such as filtration. The extraction may also include removing the solvent from the obtained extract by known methods such as concentration under reduced pressure. The extraction may also include preparing a dried extract by drying the obtained extract, such as lyophilization.

The composition is from 0.001% to 80% by weight based on the total weight of the composition, for example, from 0.01% to 60% by weight, from 0.01% to 40% by weight, from 0.01% to 30% by weight, from 0.01% to 20% by weight %, 0.01% to 10%, 0.01% to 5%, 0.05% to 60%, 0.05% to 40%, 0.05% to 30%, 0.05% to 20%, 0.05% to 10% by weight, 0.05% to 5% by weight, 0.1% to 60% by weight, 0.1% to 40% by weight, 0.1% to 30% by weight, 0.1% to 20% by weight, 0.1% by weight % To 10% by weight, or 0.1% to 5% by weight of the extract may be contained.

In another embodiment, the extract may be a fermented extract.

In one embodiment, the fermentation may be performed for 1 to 7 days at pH 6 to 7 at 30 to 60° C. in a medium containing a carbon source. In one embodiment, the fermentation is Bacillus genus, Streptococcus genus, Lactococcus genus, Enterococcus genus, Lactobacillus genus, Pediococcus genus , Leukonostoc (Leuconostoc), Weissella (Weissella), Bifidobacterium (Bifidobacterium), Saccharomyces (Saccharomyce) and Galactomyces (Galactomyces) genus selected from the group consisting of one or more strains selected from the group consisting of It may be fermented. More specifically, the strain is Lactobacillus plantarum , Lactobacillus casei , Lactobacillus acidophilus , Lactobacillus fermentum , Lactobacillus fermentum Bacillus curvatus , Lactobacillus confusus , Lactobacillus gasseri , Bifidobacterium breve , Bifidobacterium breve, Bifidobacterium thermophilum (Bifidobacterium thermophilum) Streptococcus thermophilus , Leuconostoc mesenteroides , S. cerevisiae , S. bayanus , Saccharomyces para. reading can be one's (S. paradoxus), Saccharomyces access to US Mai category (S. mikatae), access to Sakae-ku My'll Havre lots (S. kudriavzevii), or galactose Mai Seth Kandy Doom (Galactomyces candidum).

Without being limited by a particular theory, the coconut haus thorium, or an extract (or fermented extract) of a coconut embryo before germination may inhibit the activity of tyrosinase and/or elastase. In addition, the coconut haus thorium, or an extract (or fermented extract) of a coconut embryo before germination may have a skin moisturizing activity. Accordingly, the composition has an effect that can be usefully used for skin whitening, anti-wrinkle, and/or moisturizing.

In one embodiment, the composition may be a cosmetic composition. The cosmetic composition may be, for example, a softening lotion, a nutritional lotion, a massage cream, a nutritional cream, an essence, a pack, a gel, an ampoule, or a cosmetic formulation of a skin adhesion type. Ingredients included in the cosmetic composition may include ingredients commonly used in cosmetic compositions in addition to the composition as an active ingredient. For example, conventional adjuvants and carriers such as stabilizers, solubilizers, vitamins, pigments and fragrances It may include.

In another embodiment, the composition may be a composition for external application for skin.

The external preparation for skin may be a cream, a gel, an ointment, a skin emulsifier, a skin suspension, a transdermal delivery patch, a drug-containing bandage, a lotion, or a combination thereof. The above skin external preparations are ingredients commonly used in external preparations for skin such as cosmetics and pharmaceuticals, such as aqueous ingredients, oily ingredients, powder ingredients, alcohols, moisturizers, thickeners, ultraviolet absorbers, whitening agents, preservatives, antioxidants, surfactants, fragrances. , Colorants, various skin nutrients, or a combination thereof and may be appropriately formulated according to need. The external preparations for the skin include metal sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, and gluconic acid, caffeine, tannin, bellapamil, licorice extract, glavidine, and caline. Hot-water extract of fruit, various herbal medicines, drugs such as tocopherol acetate, glytilithic acid, tranexamic acid and derivatives or salts thereof, vitamin C, ascorbic acid magnesium phosphate, ascorbic acid glucoside, arbutin, kojic acid, glucose, fructose, Sugars such as trehalose can also be appropriately blended.

In another embodiment, the composition may be a pharmaceutical composition.

The pharmaceutical composition may additionally include a pharmaceutically acceptable diluent or carrier. The diluent may be lactose, corn starch, soybean oil, microcrystalline cellulose, or mannitol, and as a lubricant, magnesium stearate, talc, or a combination thereof. The carrier may be an excipient, a disintegrant, a binder, a lubricant, or a combination thereof. The excipient may be microcrystalline cellulose, lactose, low-substituted hydroxycellulose, or a combination thereof. The disintegrant may be calcium carboxymethylcellulose, sodium starch glycolate, anhydrous calcium monohydrogen phosphate, or a combination thereof. The binder may be polyvinylpyrrolidone, low-substituted hydroxypropylcellulose, hydroxypropylcellulose, or a combination thereof. The lubricant may be magnesium stearate, silicon dioxide, talc, or a combination thereof.

The pharmaceutical composition may be formulated as an oral or parenteral dosage form. The oral dosage form may be a granule, a powder, a liquid, a tablet, a capsule, a dry syrup, or a combination thereof. The parenteral dosage form may be an injection.

Coconut Haustorium extract or Cocos nucifera embryo extract before germination according to one aspect not only exhibits inhibitory activity of tyrosinase and/or elastase, but also has a skin moisturizing effect, skin whitening, anti-wrinkle And/or there is an effect that can be usefully used in a composition for moisturizing the skin.

Hereinafter, the present invention will be described in more detail through examples. However, these examples are for illustrative purposes only, and the scope of the present invention is not limited to these examples.

Example 1. Preparation of Coconut Germ (Coconut Haus Thorium) Extract after Germination

After germination, a coconut germ (coconut haus thorium) extract was prepared as follows.

First, embryos (Coconut House Thorium) were isolated from germinated coconuts (directly imported from Vanuat). After separating about 100 g of coconut haus thorium, they were pulverized, 200 ml of water was added, and the mixture was stirred at room temperature for 48 hours, followed by extraction. After extraction, it was filtered with filter paper (Whatman NO. 2, Maidstone, UK), concentrated with a reduced pressure reflux cooling device (N-1110S, EYELA, Tokyo, Japan) in a water bath of 40° C. or lower, and then freeze-dried. All samples were stored frozen at 80 °C until the experiment, dissolved in dimethyl sulfoxide (DMSO) and used in the experiment. The recovery rate was 17.89%.

Example 2. Preparation of coconut germ extract before germination

First, embryos were isolated from coconuts (directly imported from Vanuat) before germination. After separating about 100 g of coconut embryos, they were pulverized, and then 200 ml of water were each added, stirred at room temperature for 48 hours, and then extracted. After extraction, it was filtered with filter paper (Whatman NO. 2, Maidstone, UK), concentrated with a reduced pressure reflux cooling device (N-1110S, EYELA, Tokyo, Japan) in a water bath of 40° C. or lower, and then freeze-dried. All samples were stored frozen at 80 °C until the experiment, dissolved in dimethyl sulfoxide (DMSO) and used in the experiment. The recovery rate was 19.21%.

Example 3. Preparation of fermented extract of coconut germ (coconut hausthorium) after germination

First, embryos (Coconut House Thorium) were isolated from germinated coconuts (directly imported from Vanuat). After culturing Lactobacillus casei in a culture medium at 37° C. for 1 day, the formed colonies were selected. Thereafter, the formed colonies were inoculated into a sterilized culture medium and then cultured again with shaking in a 37°C temperature incubator for 24 hours. Thereafter, the crushed coconut Haus Thorium was added to the strain culture solution to a concentration of 10 g/L, and then cultured at 37° C. for 1 to 3 days. Thereafter, in order to terminate the fermentation, heat was applied at 100° C. for 40 minutes to induce a loss of function of the bacteria. The precipitate was removed using a centrifuge and the supernatant was collected, or the filtered supernatant was used. The prepared fermentation broth was mixed in the same amount with MEM, an animal cell culture medium, and then filtered through a 0.22 μm filter to remove bacteria.

Experimental Example 1. Analysis of whitening activity of coconut germ extract

In order to analyze the whitening activity of the coconut humus thorium extract prepared in Examples 1 and 2 and the coconut germ extract before germination, the inhibitory effect of tyrosinase activity was measured.

Specifically, 50 µl of 1.5mM L-tyrosine was added to 150 µl of 0.1M phosphate buffer solution (Phosphate buffer pH 6.8). Thereafter, the coconut humus thorium extract and the pre-emergence coconut germ extract prepared in Examples 1 to 3 were added at concentrations of 50 ug/ml, 100 ug/ml and 200 ug/ml, respectively. As a positive control, coconut oil and coconut fruit extract were used. Coconut fruit extract was prepared in the same manner as in Example 1 after separating the kernel portion of the coconut. Next, 30 µl of tyrosinase (100 U/ml) was added, followed by reaction at 37°C for 15 minutes. DMSO was used as a control, and 0.1M phosphate buffer was added instead of tyrosinase enzyme as a blank sample, and the reaction was carried out in the same manner as above. Thereafter, absorbance was measured at 490 nm, and the tyrosinase inhibitory activity of the coconut embryo extract was analyzed according to Equation 1 below, and the results are shown in Table 1.

[Equation 1]

Tyrosinase inhibitory activity (%) = (1-(absorbance of test group-absorbance of sample)/(absorbance of control group-absorbance of blank sample solution)) * 100

sample Tyrosinase inhibitory activity (%) 50 ug/ml 100 ug/ml 200 ug/ml CH extract 12.33 20.54 35.67 CB extract 6.18 11.59 21.75 CH fermented extract 14.19 22.45 36.78 CO 4.52 7.54 15.33 CN extract 5.01 8.12 14.49

CH extract: Coconut Huisthorium extract; CB extract: pre-emergence coconut germ extract; CO: coconut oil; CN Extract: Coconut Fruit Extract

As shown in Table 1, it was found that the coconut haus thorium extract and the pre-emergence coconut germ extract according to one embodiment had tyrosinase inhibitory activity in a concentration-dependent manner. In addition, compared to the positive control coconut oil or coconut fruit extract, it was found that the coconut haus thorium extract inhibited tyrosinase by about two times more. The above results indicate that the coconut huis thorium extract and the coconut germ extract before germination exhibit high enzyme inhibitory activity and can be usefully used in a composition for skin whitening.

Experimental Example 2. Analysis of anti-wrinkle activity of coconut germ extract

In order to analyze the anti-wrinkle activity of the coconut humus thorium extract prepared in Examples 1 and 2 and the coconut germ extract before germination, the inhibitory effect of elastase activity was measured.

Specifically, the increase in the release amount of 4-nitroaniline produced per unit time through the hydrolysis of N-succinyl-(Ala)3-p-nitroaniline, a substrate of elastase peptide (Sigma-Aldrich, USA) It was measured by the activity value of the star enzyme. First, 30 µl of 8.8 mM N-succinyl-(Ala)3-p-nitroaniline was added to 160 µl of 0.276 M Trizma-HCl (pH 8.0) (Sigma-Aldrich, USA). Thereafter, thereafter, the coconut haus thorium extract prepared in Examples 1 to 3 and the coconut germ extract before germination were added at concentrations of 50 ug/ml, 100 ug/ml and 200 ug/ml, respectively. Next, 30 µl of elastase (3.5 U/ml) was added and reacted at 37° C. for 20 minutes. DMSO was added instead of the sample solution to the control, and DMSO and BSA solution were added instead of the enzyme to the sample solution. After the reaction, absorbance was measured at 410 nm, and the result was calculated according to Equation 2 below to determine the degree of enzyme inhibitory activity of the sample. The results are shown in Table 2.

[Equation 2]

Elastase inhibitory activity (%) = (1-(absorbance of test group-absorbance of sample)/(absorbance of control group-absorbance of blank sample solution)) * 100

sample Elastase inhibitory activity (%) 50 ug/ml 100 ug/ml 200 ug/ml CH extract 9.14 18.29 37.12 CB extract 6.15 12.15 24.55 CH fermented extract 11.21 20.08 35.28 CO 3.61 5.15 11.25 CN extract 4.05 7.12 14.33

CH extract: Coconut Huisthorium extract; CB extract: pre-emergence coconut germ extract; CO: coconut oil; CN Extract: Coconut Fruit Extract

As shown in Table 2, it was found that the coconut haus thorium extract and the pre-emergence coconut germ extract according to one embodiment had an elastase inhibitory activity in a concentration-dependent manner. In addition, compared to the positive control coconut oil or coconut fruit extract, it was found that the coconut haus thorium extract inhibited tyrosinase by about 2-3 times more. The above results mean that the coconut Huis Thorium extract and the coconut germ extract before germination exhibit high enzyme inhibitory activity, and can be usefully used in anti-wrinkle compositions.

Experimental Example 3. Analysis of moisturizing activity of coconut germ extract

In order to confirm the moisturizing effect of the coconut haus thorium extract prepared in Examples 1 and 2 and the coconut germ extract before germination, changes in skin moisture level over time after application of the sample were measured.

Specifically, 200 ug/ml of sample (coconut haus thorium extract, coconut germ extract before germination, and coconut oil) for 5 adult women in their 20s to 40s was applied before, immediately after application, and skin moisture level over time. Was measured using a Corneometer. First, 30 minutes before the test, the test site was washed with lukewarm water, and after waiting for 10 minutes in a constant temperature and humidity room (20 ± 2°C, 40 to 60% humidity), the skin moisture level when the test site was not applied was measured. In addition, after applying the test product to the test site, the skin moisture level was measured immediately after application of the product and after 2 hours. The unit is the unit constant A.U., and the measured value represents an average of three times, and the results are shown in Table 3 below.

sample Before application Immediately after application 2 hours after application No treatment 22.21 ± 4.35 22.52 ± 3.18 21.63 ± 4.42 CH extract 21.35 ± 3.64 58.45 ± 2.24 37.99 ± 3.54 CB extract 21.66 ± 3.38 45.89 ± 2.21 26.16 ± 3.32 CH fermented extract 20.59 ± 5.21 52.56 ± 3.18 35.22 ± 3.47 CO 58.45 ± 2.24 28.78 ± 4.21 23.59 ± 5.08 CN extract 58.45 ± 2.24 30.59 ± 5.18 24.13 ± 5.22

CH extract: Coconut Huisthorium extract; CB extract: pre-emergence coconut germ extract; CO: coconut oil; CN Extract: Coconut Fruit Extract

As shown in Table 3 above, the coconut haus thorium extract and the coconut germ extract before germination according to one embodiment showed a moisturizing effect both immediately after application and 2 hours after application, but in the case of coconut oil and coconut fruit extract, immediately after application It was found that the moisturizing effect appeared, but the skin moisture level was not maintained high. As a result of the above, it can be seen that the coconut haus thorium extract and the coconut germ extract before germination according to an embodiment have excellent moisturizing effects and can play a large role in maintaining skin moisture.

Claims (12)

A cosmetic composition for skin whitening containing coconut haustorium extract. The cosmetic composition of claim 1, wherein the extract is extracted using water, C1-C4 alcohol, or a combination thereof as a solvent. The cosmetic composition of claim 1, wherein the composition inhibits the activity of tyrosinase. The cosmetic composition for skin whitening according to claim 1, wherein the extract is a fermented extract. Cosmetic composition for anti-wrinkle containing coconut haustorium (Coconut haustorium) extract. The cosmetic composition for anti-wrinkle according to claim 5, wherein the extract is extracted using water, C1-C4 alcohol, or a combination thereof as a solvent. The cosmetic composition for anti-wrinkle according to claim 5, wherein the composition inhibits the activity of elastase. The anti-wrinkle cosmetic composition of claim 5, wherein the extract is a fermented extract. A cosmetic composition for moisturizing the skin containing coconut haustorium extract. The cosmetic composition for moisturizing skin according to claim 9, wherein the extract is extracted using water, C1-C4 alcohol, or a combination thereof as a solvent. An external preparation for skin whitening containing coconut haustorium extract as an active ingredient. Anti-wrinkle skin external preparation containing coconut haustorium extract as an active ingredient.