KR20020060862A - Cosmetic for skin whitening containing a herb extract with inhibitory activity of melanin formation - Google Patents

Abstract

PURPOSE: A skin whitening cosmetic composition containing one or more effective components selected from Datura metel L. extract(or Datura innoxia Mill. extract), Hyoscyamus niger L. extract and a mixture thereof is provided which inhibits pigmentation and can be safely used without any side effect on the skin. CONSTITUTION: This skin whitening cosmetic composition contains 0.0001 to 10.0% by weight of Datura metel L. extract, Hyoscyamus niger L. extract or a mixture thereof, based on dried weight, wherein the extracts have melanogenesis-inhibiting activity. The composition is obtained by extracting in one or more solvents selected from the group consisting of water, C1-4 lower alcohol, ethylacetate and acetone.

Description

Cosmetic for skin whitening containing a plant extract having a melanogenesis inhibitory activity {Cosmetic for skin whitening containing a herb extract with inhibitory activity of melanin formation}

The present invention relates to a skin whitening cosmetic containing a plant extract having a melanin production inhibitory activity, in more detail can be safely used without side effects on the skin and has a melanin production inhibitory effect excellent yanghwa extract, cheonsunja extract, or these It relates to a cosmetic for skin whitening containing a mixture of.

It is everyone's constant desire to have white, fair skin. Human skin color is genetically determined by the concentration and distribution of melanin in the skin, but is also influenced by environmental or physiological conditions such as sun ultraviolet rays, fatigue and stress. Melanin is a type of amino acid tyrosine (tyrosinase) acts as an enzyme called tyrosinase (tyrosinase) is converted to dopa (DOPA), dopaquinone (dopaquinone) is produced through a non-enzymatic oxidation reaction. However, although the pathway by which melanin is made is known, it is still not clear what mechanisms induce melanin synthesis, the previous stages of tyrosinase action.

Such melanin can cause dark and uneven skin tone and acne when excessively synthesized in the skin. Therefore, by inhibiting the synthesis of melanin pigment in the skin, not only can the skin tone be brightened and the skin whitening can be realized, but also the hyperpigmentation of the skin such as UV rays, hormones, blemishes caused by heredity, ultraviolet rays, and freckles caused by heredity You can.

Therefore, conventionally, a substance having an inhibitory activity against tyrosinase such as hydroquinone, ascorbic acid, kojic acid, glutathione, and the like is blended into the ointment or cosmetics to produce skin whitening or cosmetics. It has been used for the purpose of improving blemishes and freckles. However, hydroquinone exhibits a predetermined whitening effect, but has a problem of limiting the amount of the compound to a very small amount due to severe skin irritation, and ascorbic acid is easily oxidized, causing cosmetic problems such as discoloration and discoloration. Unstable in solution complicates the manufacturing process of cosmetics. In addition, thiol-based compounds such as glutathione and cysteine not only have a characteristic unpleasant odor, but also have problems with transdermal absorption, and glycosides and derivatives thereof have a high polarity and thus have problems in being used as a component of cosmetics. On the other hand, placenta extracts, which are frequently used these days, are not irritating to the skin but have insufficient whitening effects.

Accordingly, the technical problem to be achieved by the present invention is to provide a cosmetic for skin whitening excellent in the pigmentation inhibitory effect by not only can be used safely without side effects to the skin by solving the above problems and inhibits melanin production.

In order to achieve the above object, the skin whitening cosmetics according to the present invention is characterized in that it comprises any one or more selected from the hydrangea extract, cheonsunja extract and mixtures thereof as an active ingredient.

It is preferable that the content of the hydrangea extract, cheonnja extract or a mixture thereof is 0.0001 to 10.0% by weight in dry weight.

In addition, the calendula extract or cheonnja extract is preferably extracted with one or more solvents selected from the group consisting of water, lower alcohol having 1 to 4 carbon atoms, ethyl acetate and acetone.

Hereinafter, the cosmetic for skin whitening according to the present invention will be described in detail.

The cosmetic for skin whitening according to the present invention comprises a hydrangea extract, a natural extract, or a mixture thereof, which is a natural substance having melanin production inhibitory activity, as an active ingredient.

The hydrangea is a dry flower of the branching plant Datura metel L. or Datura innoxia Mill. It is used to treat asthma and bronchitis. In Chinese herbal medicine dictionary, it is recorded that hydrangea contains substances such as scopolamine, hyoscyamine, norhyosciamine, atropine and the like. In addition, as a seed of Hyoscyamus niger L. belonging to the branch family, it was used for the treatment of chronic asthma, malignant swelling and rabies. In Chinese medicine metabolism, it is recorded that the astrologer contains substances such as atropamine, tetramethyl diaminobutane, and cuscohygrine.

As such, the hydrangea and cheonseonja are known as a herbal medicine that can treat asthma, etc., the present inventors can use the extract of the mouse melanoma cells that can screen (screening) to a substance that inhibits the melanin synthesis induction itself ( Experiments with B16 mouse melanoma cells revealed that they could have very potent melanin suppression and whitening effects. Therefore, the addition of natural extracts of hydrangea and / or cheonnyang to external skin ointments or cosmetics can exhibit a strong skin whitening effect without any side effects.

Calendula or catenary are readily available on the market, and their extracts are, for example, primary extracts of calendula or catenary with water or organic solvents such as anhydrous or hydrous lower alcohols having 1 to 4 carbon atoms or ethyl acetate or acetone. After concentration under reduced pressure, it can be obtained by lyophilization or spray drying. It is preferable to finely pulverize the hydrangea or cheonngi, etc., and to extract water or an organic solvent by heating at 50 to 100 ° C. for 1 to 5 hours to make 5 to 20 volumes with respect to the dry weight of the pulverized product. To obtain a high purity extract, the extract may be extracted one or more times in the same manner.

The calendula or cheonnja extract obtained as described above may be used in each or at the same time contained in various cosmetics such as skin ointment or lotion. The content of the hydrangea extract, cheonsunja extract or a mixture thereof contained in the cosmetic preparation according to the present invention is preferably in the range of 0.0001 to 10.0% by weight, more preferably 0.0005 to 10.0% by weight of dry weight. have. At concentrations of 0.0001% by weight or less, it is difficult to expect a clear melanin production inhibitory effect and a whitening effect, and at a concentration of 10% by weight or more, a distinct effect is not expected.

Hereinafter, the present invention will be described in detail with reference to Examples. However, embodiments according to the present invention can be modified in many different forms, the scope of the present invention should not be construed as limited to the embodiments described below. Embodiments of the present invention are provided to more completely explain the present invention to those skilled in the art.

Example of hydrangea extraction

Extraction Example 1

Purified 100 g of commercially available calendula was put into 3 l of 80% methanol, boiled for 3 hours in a reflux extractor equipped with a cooling capacitor, filtered through 100 mesh filter cloth, and the residue was extracted once more in the same manner. . Each extract was combined and filtered using Whatman No. 2 filter paper at room temperature to remove insoluble matters, concentrated under reduced pressure at 60 ° C. in a distillation apparatus equipped with a cooling condenser, and lyophilized to obtain 4.5 g of dry extract.

Extraction Example 2

Except for using purified water instead of 80% methanol extracted in the same manner as extraction Example 1 to obtain 4.1g of a dry extract.

Extraction Example 3

Except for using 85% ethanol instead of 80% methanol was extracted in the same manner as the extraction example 1 to obtain a dry extract of 4.6g.

Extraction Example 4

Except that 70% acetone instead of 80% methanol was extracted in the same manner as the extraction example 1 to obtain 3.2g of a dry extract.

Extraction Example 5

Except that ethyl acetate was used instead of 80% methanol, extraction was carried out in the same manner as in Extraction Example 1 to obtain 3.7 g of a dry extract.

Extraction Example 6

Except for using saturated normal butanol instead of 80% methanol was extracted in the same manner as the extraction example 1 to obtain 4.3g of the dry extract.

Extraction Example 7

Purchasing a commercially available millimeter 100g of the pulverized pulverized product was put in 3L of 80% methanol, boiled for 3 hours in a reflux extractor with a cooling capacitor, filtered with 100 mesh filter cloth and the residue was extracted once more in the same manner. Each extract was combined and filtered with Whatman No. 2 filter paper at room temperature to remove insoluble matters, concentrated under reduced pressure at 60 ° C. in a distillation apparatus equipped with a cooling condenser, and lyophilized to obtain 8.3 g of dry extract.

Extraction Example 8

Except for using purified water instead of 80% methanol extracted in the same manner as the extraction example 7 to obtain a dry extract of 7.4g.

Extraction Example 9

Except for using 85% ethanol instead of 80% methanol was extracted in the same manner as in Example 7 to obtain 8.6g of a dry extract.

Extraction Example 10

Except for using 70% acetone instead of 80% methanol was extracted in the same manner as the extraction example 7 to obtain a 6.8g dry extract.

Extraction Example 11

Except for using ethyl acetate instead of 80% methanol extracted in the same manner as in Example 7 to obtain 5.4g of a dry extract.

Extraction Example 12

Except for using saturated normal butanol instead of 80% methanol was extracted in the same manner as in Example 7 to obtain 7.0 g of a dry extract.

Examples 1-12

Each of the extracts obtained in accordance with the extraction examples 1 to 12 and hydroquinone aqueous solution was added to the culture solution of mouse melanoma cells (B-16 mouse melanoma cells) (Examples 1 to 12) to test the whitening effect at the cellular level. (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980). Each of the extracts obtained in accordance with the extraction examples 1 to 12 to a final concentration of 0.005%, the hydroquinone aqueous solution was added to the culture medium of B-16 melanoma cells with a concentration of 0.0001% of each of the cells were cultured for 3 days Trypsin treatment was removed from the culture vessel and centrifuged to extract melanin.

Here the amount of melanin produced was measured using a spectrophotometer from the absorbance, 400nm dissolved melanin boiled 10 minutes was added a solution of sodium (1N concentration) 1㎖ hydroxide in a manner represented by the absorbance of the unit cell allowance (10 ⁶ cell) The melanin production relative to the control group was calculated as the inhibition rate (%) and the results are summarized in Table 1.

sample Melanin production % Inhibition Control group (no addition) 0.048 ± 0.003 - Example 1 (final concentration 0.005%) 0.030 ± 0.003 37% Example 2 (final concentration 0.005%) 0.035 ± 0.002 28% Example 3 (final concentration 0.005%) 0.027 ± 0.002 43% Example 4 (final concentration 0.005%) 0.027 ± 0.002 44% Example 5 (final concentration 0.005%) 0.028 ± 0.003 41% Example 6 (final concentration 0.005%) 0.032 ± 0.003 33% Example 7 (final concentration 0.005%) 0.033 ± 0.004 32% Example 8 (final concentration 0.005%) 0.034 ± 0.002 29% Example 9 (final concentration 0.005%) 0.030 ± 0.002 38% Example 10 (final concentration 0.005%) 0.030 ± 0.002 38% Example 11 (final concentration 0.005%) 0.027 ± 0.003 43% Example 12 (final concentration 0.005%) 0.034 ± 0.003 30% Hydroquinone (final concentration 0.0001%) 0.025 ± 0.002 48%

* Repeat count = 3

As can be seen from the results of Table 1, each sample obtained according to the extraction examples 1 to 12 can be seen that there is a very strong melanin production inhibitory ability against the melanoma cells of the cultured mice compared to the control group (Example 1 ~ 12), considering that the extract is not purified at all, it can be seen that the effect does not fall even when compared with hydroquinone, a previously known whitening substance.

Examples 13-20

The melanoma production inhibitory ability of the rat melanoma cells cultured in the same manner as in Example 1 according to the concentration change of the extracts of the extraction examples 1 and 7 was investigated, and the results are shown in Table 2 below.

* Repeat count = 3

As shown in the results of Table 2, it can be seen that the higher the concentration of hydrangea and cheonnja extract has a significant improvement in melanin production inhibitory ability against the melanoma cells of the cultured rats.

On the other hand, hydroquinone has a strong melanin production inhibitory ability but exhibits severe cytotoxicity even at low concentration of 0.0001%, the extract of the present invention does not show cytotoxicity even at 0.05% or more concentration to have a higher melanin production inhibitory effect than hydroquinone can do.

In the following, it is prepared by adding a hydrangea or cheonnyangja extract to the skin external ointment, cream, supple cosmetics, nutrient cosmetics, packs, essences, and examines the pigmentation inhibitory effect by prescribing them to the test subjects.

Preparation Examples 1 and 2

The cinnamon extract obtained from the extraction example 5 and the cheonseonja extract obtained from the extraction example 11 as an active ingredient, respectively, to prepare an external topical ointment with the ingredients and contents as shown in Table 3.

Comparative Example 1

Without the addition of plant extracts, the skin external ointment was prepared with the ingredients and contents as shown in Table 3 below.

Composition (% by weight) Production Example Comparative example One 2 One Plant extracts Hydrangea extract 10 - - Paragon Extract - 10 - Diethyl sebacate 8 8 8 Prepayment 5 5 5 Polyoxyethylene oleyl ether phosphate 6 6 6 Sodium benzoate Quantity Quantity Quantity vaseline to 100 to 100 to 100

Preparation Examples 3 and 4

The cinnamon extract obtained from the extraction example 5 and the cheonseonja extract obtained from the extraction example 11 as an active ingredient, respectively, to prepare a cream in cosmetics with the ingredients and contents as shown in Table 4.

Comparative Example 2

Without adding a plant extract, a cream in cosmetics was prepared with the ingredients and contents as shown in Table 4 below.

Composition (% by weight) Production Example Comparative example 3 4 2 Plant extracts Hydrangea extract 1.0 - - Paragon Extract - 1.0 - Stearic acid 15.0 15.0 15.0 Cetanol 1.0 1.0 1.0 Potassium hydroxide 0.7 0.7 0.7 glycerin 5.0 5.0 5.0 Propylene glycol 3.0 3.0 3.0 antiseptic Quantity Quantity Quantity incense Quantity Quantity Quantity Purified water to 100 to 100 to 100

Preparation Examples 5 and 6

The hydrangea extract obtained from the extraction example 5 and the cheonseonja extract obtained from the extraction example 11, respectively, as an active ingredient, the flexible cosmetics in the cosmetic was prepared with the ingredients and contents as shown in Table 5.

Comparative Example 3

Without adding a plant extract, the flexible cosmetics in the cosmetic was prepared in the ingredients and contents as shown in Table 5.

Composition (% by weight) Production Example Comparative example 5 6 3 Plant extracts Hydrangea extract 0.2 - - Paragon Extract - 0.2 - ethanol 10.0 10.0 10.0 Polylauric acid polyoxyethylene sorbitan 1.0 1.0 1.0 Methyl paraoxybenzoate 0.2 0.2 0.2 glycerin 5.0 5.0 5.0 1,3-butylene glycol 6.0 6.0 6.0 incense Quantity Quantity Quantity Pigment Quantity Quantity Quantity Purified water to 100 to 100 to 100

Preparation Examples 7 and 8

The hydrangea extract obtained from the extraction example 5 and the cheonseonja extract obtained from the extraction example 11, respectively, as an active ingredient, the nutrient cosmetic water was prepared by the ingredients and contents as shown in Table 6 below.

Comparative Example 4

A nutritional lotion was prepared with the ingredients and contents as shown in Table 6 without adding plant extracts.

Composition (% by weight) Production Example Comparative example 7 8 4 Plant extracts Hydrangea extract 0.1 - - Paragon Extract - 0.1 - Waselin 2.0 2.0 2.0 Sesquioleate sorbitan 0.8 0.8 0.8 Polyoxyethylene oleylethyl 1.2 1.2 1.2 Methyl paraoxybenzoate Quantity Quantity Quantity Propylene glycol 5.0 5.0 5.0 ethanol 3.2 3.2 3.2 Carboxy Vinyl Polymer 18.0 18.0 18.0 Potassium hydroxide 0.1 0.1 0.1 Pigment Quantity Quantity Quantity incense Quantity Quantity Quantity Purified water to 100 to 100 to 100

Preparation Examples 9 and 10

The hydrangea extract obtained from the extraction example 5 and the cheonseonja extract obtained from the extraction example 11 as an active ingredient, and the pack in the cosmetic was prepared with the ingredients and contents as shown in Table 7 below.

Comparative Example 5

A nutritional lotion was prepared with the ingredients and contents as shown in Table 7 without adding plant extracts.

Composition (% by weight) Production Example Comparative example 9 10 5 Plant extracts Hydrangea extract 0.5 - - Paragon Extract - 0.5 - glycerin 5.0 5.0 5.0 Propylene glycol 4.0 4.0 4.0 Polyvinyl alcohol 15.0 15.0 15.0 ethanol 8.0 8.0 8.0 Polyoxyethylene oleylethyl 1.0 1.0 1.0 Methyl paraoxybenzoate 0.2 0.2 0.2 incense Quantity Quantity Quantity Pigment Quantity Quantity Quantity Purified water to 100 to 100 to 100

Preparation Examples 11 and 12

The hydrangea extract obtained from the extraction example 5 and the cheonseonja extract obtained from the extraction example 11 as an active ingredient, and the essence in the cosmetic was prepared with the ingredients and contents as shown in Table 8.

Comparative Example 6

No nutritional lotion was prepared with the ingredients and contents as shown in Table 8, without the addition of plant extracts.

Composition (% by weight) Extraction Example Comparative example 11 12 6 Plant extracts Hydrangea extract 5 - - Paragon Extract - 5 - Propylene glycol 10.0 10.0 10.0 glycerin 10.0 10.0 10.0 Sodium hyaluronate aqueous solution (1%) 5.0 5.0 5.0 ethanol 5.0 5.0 5.0 Polyoxyethylene Cured Castor Oil 1.0 1.0 1.0 Methyl paraoxybenzoate 0.1 0.1 0.1 incense Quantity Quantity Quantity Purified water to 100 to 100 to 100

The method used to verify the pigmentation inhibitory effect by the skin external ointment, cream, softening lotion, nutrient lotion, pack, essence prepared as follows.

First, select 20 healthy men and women and attach aluminum foil with two rows of 6 holes with a diameter of 7 mm in the lower part of both arms. Was investigated. The irradiation site was washed well with 70% ethanol aqueous solution before irradiation. Twice a day from 3 days before irradiation to 3 weeks after irradiation, containing cosmetics containing hydrangea or catenary extract prepared according to Preparation Examples 1 to 12, and the base containing no plant extract according to Comparative Examples 1 to 6. It was applied in the same row in pairs. Here, the pack agents of Preparation Examples 9, 10 and Comparative Example 5 were removed 15 minutes after the application.

Determination of the pigmentation degree after the prescription of the cosmetics according to the respective preparation examples and comparative examples visually determined, comparing the degree of inhibition of pigmentation of the cosmetics according to each embodiment and the cosmetics according to the comparative example, there is a distinct effect, effect, difference Evaluate in three stages of none, and also investigate the occurrence of side effects, the results are shown in Table 9 below.

Experimental substance Distinct Effects (persons) Effective (persons) No difference (persons) Side effects (persons) Preparation Example 1 4 8 8 0 Preparation Example 2 5 8 7 0 Preparation Example 3 3 6 11 0 Preparation Example 4 2 7 11 0 Preparation Example 5 2 6 12 0 Preparation Example 6 One 8 11 0 Preparation Example 7 2 7 11 0 Preparation Example 8 2 6 12 0 Preparation Example 9 2 6 12 0 Preparation Example 10 3 6 11 0 Preparation Example 11 3 8 9 0 Preparation Example 12 3 7 10 0

As shown in Table 10, the cosmetics containing the hydrangea or cheonseonja extract prepared according to Preparation Examples 1 to 12 showed a significant whitening effect on at least 8 or more of 20 subjects, in particular a large amount of hydrangea , Cosmetic preparations of Preparation Examples 1 and 2 containing a natural extract of the extract showed 60% and 65% of the pigmentation inhibitory effect than the cosmetic composition of Comparative Example 1 containing no plant extract, respectively, did not show any side effects in the skin And it was found.

As described above, the cosmetic for skin whitening containing the hydrangea or cheonngi extract of the present invention inhibits melanin production and inhibits pigmentation, thereby improving skin whitening or freckles and freckles. In addition, since the hydrangea or cheonnyang is a natural substance, it can be safely used as a cosmetic without side effects on the skin.

Claims (3)

Skin whitening cosmetics, characterized in that it contains any one selected from the hydrangea extract, cheonseonja extract and mixtures thereof. The skin whitening cosmetic according to claim 1, wherein the content of the hydrangea extract, the catenary extract or the mixture thereof is 0.0001 to 10.0 wt% based on the dry weight. The skin whitening cosmetic according to claim 1, wherein the hydrangea extract or the catenary extract is extracted with one or more solvents selected from the group consisting of water, a lower alcohol having 1 to 4 carbon atoms, ethyl acetate, and acetone.