KR20030090126A - A composition for whitening containing fruit of Chinese quince extract - Google Patents

Abstract

PURPOSE: Provided is a whitening composition containing the fruit extract of Chaenomeles sinensis Koehne which inhibits the activation of tyrosinase committed to the growth inhibition of melanin cells and the generation of melanin, and reduces the amount of melanin to exert the whitening effect. CONSTITUTION: A whitening composition comprises 0.01-10 wt.% of an extract of the fruit of Chaenomeles sinensis Koehne, and the extract is selected from the group consisting of a crude extract, a water soluble extract and an ethanol soluble extract. The crude extract is prepared by grating the fruit in a mixer or homogenizer, putting it in a deep freezer overnight, and drying it with a freeze dryer for 2-3 days. The water soluble extract is prepared by adding distilled water to the completely dried fruit, and extracting and filtering it, followed by the same processing steps as with the crude extract. The ethanol soluble extract is prepared by adding ethanol to the completely dried fruit, and extracting and filtering it at 45-55 deg.C for 4-6 hours, followed by the same processing steps as with the crude extract.

Description

A composition for whitening containing fruit of Chinese quince extract}

The present invention relates to a whitening composition containing the Chinese quince extract, and more particularly to a whitening composition containing a lyophilized powder hot water extract or ethanol extract of the Chinese quince which is a natural whitening material.

Chinese quince ( Chenomeles sinensis Koehne) is a cultivated plant native to China, and it is called the tree family because it looks like a melon, but because it runs on a tree, its main components are saponin, organic acid, and flavonoids. ), Tannins and the like.

The skin color of the human body becomes black when it is exposed to sunlight. This is because melanin (melanin), a kind of black pigment, is formed in the human body, and melanin is a polymer of phenols widely found in animals, plants, and microorganisms. It consists of black pigment and protein.

Melanin is tyrosine in melanocytes (tyrosine) as a substrate to act as a tyrosinase (tyrosinase) to produce a dopaquinone (dopaquinone) is synthesized through the oxidation and enzyme reaction.

Therefore, in order to inhibit the synthesis of melanin in the human skin, a substance having an effect of inhibiting the activity of tyrosinase or inhibiting some reactions during the production of melanin is required. As a tyrosinase inhibitor, Ascorbic acid, corticosteroids, retinoids azalacic acid, hydroquinone, hydroxyanisole, kojic acid, arbutin, etc. However, these chemical synthetic materials have problems such as safety, stability and discoloration and deodorization during long-term storage.

In order to overcome the above problems, research has been continuously conducted to utilize the extracts of plants, which are natural substances, as a whitening ingredient. As a well-known technique, whitening cosmetics using the ingredients of baekbaekpi (Korean Patent Publication No. 92-2109) , Japanese Patent Application No. 55-44375, Japanese Patent Application No. 64-26507, Japanese Patent Application No. 64-83009, Japanese Patent Application Publication No. 1-256587), Whitening cosmetics using ingredients of licorice ( Korean Patent Application Publication No. 92-2109, Japanese Patent Application Publication No. 60-214721, Japanese Patent Application Publication No. 63-23809, Japanese Patent Application Publication No. Hei 1-49706), and the like.

In addition, whitening cosmetics using ingredients of peony (Japanese Patent Laid-Open No. 61-246109), whitening cosmetics using ingredients of cinnamon (Japanese Laid-Open Patent No. 63-30403), whitening composition using gardenia berry extract (Korean publication) Patent No. 2002-4896), anti-aging cosmetic composition containing the extract of Yu-geun-pi (Korean Patent Publication No. 2002-4896), whitening composition containing the Cheonnyeonja extract (Korean Patent No. 2001-93861), pagoji extract A whitening composition (Korean Patent Publication No. 2001-93859) and a whitening composition (Korean Patent Publication No. 2001-93860) containing a sewage extract are disclosed.

It has been found that many of the above plant extracts act on tyrosinase to inhibit melanin synthesis, but such natural ingredients are insufficient to completely solve problems such as safety, stability, and discoloration potential while maintaining strong inhibitory activity. It is true.

The present inventors conducted a study to solve the above problems by maintaining the stability using a quince extract, a natural material while suppressing the activity of tyrosinase involved in the inhibition of melanocyte proliferation and the production of melanin melanin The present invention was completed by finding out that a whitening composition capable of reducing the amount of produced was prepared.

Accordingly, an object of the present invention is to provide a new whitening composition containing the Chinese quince extract as an active ingredient.

1 is a melanocyte proliferation inhibitory effect of Chinese quince extract according to the present invention,

2 is the effect of inhibiting dopa oxidase activity of Chinese quince extract according to the present invention,

3 is a melanogenesis inhibitory effect of the Chinese quince extract according to the present invention,

Figure 4 shows the morphology of B16 melanoma cells after 3 days treatment 1000 g / ㎖ of ethanol extract of the Chinese quince extract.

Chinese quincean is known to contain quercetin derivatives and caffeoylquinic acid derivatives (Silva BM et al) in addition to arbutin, which is widely used as a whitening substance. ., Analysis of phenolic compounds in evaluation of commercial Quince jam authenticity, J Agric food Chem 2000, 48, 2853-2857).

Herbal life is said to be used when the quince harmonizes the stomach and earth, harmonizing the stomach and earth, softens and strengthens the muscles. The ingredient is known to be effective in diarrheal diseases because it has a function of reducing the skin.

In the whitening composition according to the present invention, one or two quince extracts selected from the group consisting of lyophilized extracts of Chinese quince, hot water extracts or ethanol extracts of quince are used.

Crude extracts used in the present invention are put in a mixer or homogenizer (overnight) in the freezer (deep freezer) over night chopped Chinese quince, and then freeze dryer (freeze dryer) 2-3 Prepare by drying completely for days.

The water soluble extracts of Chinese quince used in the present invention are added to distilled water to a completely dried Chinese quince and extracted by hot water bath for 4-6 hours, the filtered extract overnight in a freezer, 2-3 in a freeze dryer. Prepared by drying for days.

In addition, the ethanol soluble extracts of Chinese quince (ethanol soluble extracts) used in the present invention is added to the ethanol to completely dried quince and extracted for 4-6 hours at 45-55 ℃ over night the filtered extract in the freezer and then in a freeze dryer Prepare by drying completely for 2-3 days.

In the present invention, the effect of the quince extract prepared above on melanocytes was verified through a cell proliferation experiment, a tyrosinase activity test, a melanin amount measurement test, and the quince extract used in the present invention was used for the proliferation of melanocytes. By inhibiting and inhibiting the activity of tyrosinase involved in the production of melanin as well as reducing the amount of melanin, it was confirmed that there is a whitening effect.

The whitening composition according to the present invention contains 0.01-10% by weight of the Chinese quince extract, preferably 0.01-5% by weight. This is because there may be a problem in the safety or formulation formulation.

The whitening composition according to the present invention may be used in cosmetics such as cosmetic creams, lotions, cosmetic emulsions, beauty waters, liquid or solid soaps or syrups, ointments, creams, premises, tinctures, extracts, herbal preparations, acupuncture agents, premises It may be formulated as an oral or external preparation, and may contain a skin absorption promoting substance to enhance the whitening effect.

Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples. However, the technical scope of the present invention is not limited to these examples and test examples.

Example 1 Preparation of Chinese Quince Lyophilized Extract

The quince 547g (1 quince weight) prepared by washing in water was finely chopped and dried in a freeze dryer at -50 ° C under reduced pressure for 3 days to prepare 91.552 g of quince dry extract.

<Example 2> (Preparation of Chinese quince hot water extract)

100 ml of distilled water was added to 5 g of the dried dried Chinese quince extract and extracted with hot water bath at 80 ° C. for 5 hours.

The extract obtained above was filtered through Whatman No. 2 filter paper overnight in a -70 ° C freezer, and then completely dried in a freeze dryer at -50 ° C under reduced pressure for 3 days. 2.18 g (39.917 g / quince) extract was prepared.

Example 3 Preparation of Chinese Quince Ethanol Extract

100 g of 70% ethanol was added to 5 g of the dried quince lyophilized extract prepared in Example 1, and extracted at 50 ° C. for 5 hours.

The extract obtained from the above-mentioned filtrate was overnight in a freezer at -70 ° C. overnight, and then completely dried in a freeze dryer under reduced pressure for 3 days, followed by 1.83 g of Chinese ethanol extract (33.508 g per Chinese quince). Was prepared.

Example 4 (Preparation of Nutrients Containing Quince Extract)

5 parts by weight of the quince hot water extract prepared in Example 2, 5 parts by weight of beeswax, 1 part by weight of polysorbate 60, 0.5 parts by weight of sorbitas sequiolade, 3 parts by weight of liquid paraffin, 3 parts by weight of squalane, capric triglyceride 3 parts by weight, glycerin 2.5 parts by weight, butylene glycol 2.5 parts by weight, propylene glycol 2.5 parts by weight, 0.1 parts by weight of carboxyvinyl polymer, 0.1 parts by weight of triethanol amine and a suitable amount of preservatives, pigments, flavors and purified water The nutritional cosmetics were prepared.

Example 5 Preparation of Cream Containing Chinese Quince Extract

10 parts by weight of the Chinese ethanol extract prepared in Example 3, 8 parts by weight of stearyl alcohol, 2 parts by weight of stearic acid, 2 parts by weight of stearic acid cholesterol, 4 parts by weight of squalane, 6 parts by weight of 2-octyldodecyl alcohol, polyoxyethylene alcohol Cream was prepared by the conventional method using 3 weight part of esters, 2 weight part of glyceryl monostearic acid esters, 5 weight part of propylene glycol, and purified water.

<Test Example 1> (B16 melanoma cell culture)

B16 melanoma cells used for cell proliferation, tyrosinase activity and melanin levels of the Chinese quince extract used in the whitening composition according to the present invention, 10% fetal bovine serum (fetal bovine serum) in RPMI1640 basic medium 1% penicillin-streptomycin was added to the culture medium at 37 ° C. and 5% CO _2. The culture medium was changed every three days.

Test Example 2 (Measurement of Cell Proliferation Inhibition Effect)

In order to investigate the melanocyte proliferation inhibitory effect of the Chinese quince extract used in the whitening composition according to the present invention, Chinese quince lyophilized extract (CE) Chinese quince hot water extract (WE) and Chinese ethanol extract (EE) prepared in Examples 1 to 3 The proliferation rate of B16 melanoma cells treated with) is shown in Table 1 and FIG. 1.

Cell proliferation was measured by the following method. First, B16 melanoma cells incubated at a concentration of 2 × 10 ⁴ / dish in a 60 mm culture dish to confirm cell adhesion at a concentration of 10 μg / ml, 100 μg / ml and 1000 μg / ml, respectively. Cells were harvested by treatment with 0.25% Trypsin-EDTA solution on the third day.

500 μl of the harvested cell shaker was mixed and uniformly mixed with 10 ml of isotone solution and counted with a Coulter counter (ZM, Coulter Co., England). The calculation was as follows.

Total cell count = number of cells counted by the Coulter counter x 42 X (cell shake amount / ml)

TABLE 1 Cell Proliferation Rate

division Concentration 10 μg / ml 100 μg / ml 1000 μg / ml WE 101% 87% 36% EE 90% 82% 27% CE 89% 72% 25%

As shown in Table 1 and FIG. 1, the melanocyte proliferation inhibition rate was low in the Chinese quince extract 10 ㎍ / ㎖ and 100 ㎍ / ㎖ treated group, the quince lyophilized extract (CE), quince hot water extract ( WE) and Chinese ethanol extract (EE) were found to have high melanocyte proliferation inhibition rate.

<Test Example 3> (Measurement of Dopa Oxidase Activity Inhibition Effect)

In order to examine the whitening effect of the Chinese quince extract used in the whitening composition according to the present invention in the Chinese quince hot water extract (WE) and Chinese quince lyophilized extract (CE), ethanol extract (EE) treatment prepared in Examples 1 to 3 Table 2 and FIG. 2 show the results of measuring the activity inhibition rate of dopa-oxidase involved in the conversion of dopaquinone to dopaquinone during melanin production.

The activity inhibition rate of dopa oxidase was measured by the following method. First, CE, WE, and EE were cultured in a 60 mm culture dish at a concentration of 2 × 10 ⁴ / dish at a concentration of 10 μg / ml, 100 μg / ml, and 1000 μg / ml, respectively. Cells were harvested by treatment with 0.25% Trypsin-EDTA solution on the third day and counted with a Coulter counter.

Then, divide 2X10 ⁵ cells per treatment group into 1.7 ml tubes, add 100 μl of 1 mM L-dopa (Sigma Chemical Co., St, Louis, Missouri), and then dissolve the cell grinding solution at 37 ° C. for 1 hour. After the reaction, the absorbance was measured at 490 nm with a spectrophotometer.

TABLE 2 Dopa Oxidase Activity

division Concentration 10 μg / ml 100 μg / ml 1000 μg / ml WE 87% 79% 47% EE 83% 80% 51% CE 80% 73% 41%

As shown in Table 2 and Figure 2, the inhibitory activity of dopa oxidase is low in the Chinese quince extract 10 ㎍ / ㎖ and 100 ㎍ / ㎖ treatment, but the quince lyophilized extract (CE), quince hot water extract in 1000 ㎍ / ㎖ treatment Both (WE) and Chinese ethanol extract (EE) have high dopa oxidase activity inhibition rates.

<Test Example 4> (Melanin production amount measurement)

In order to examine the whitening effect of Chinese quince extract used in the whitening composition according to the present invention, Chinese quince lyophilized extract (CE), Chinese quince hot water extract (WE) and Chinese ethanol extract (EE) were prepared in Examples 1 to 3. The results of measuring the amount of melanin produced by the are shown in Table 3 and FIG.

Melanin production was measured by the following method. First, B16 melanoma cells which were cultured at a concentration of 2 × 10 ⁴ / dish in a 60 mm culture dish were treated with WE and EE at concentrations of 10 μg / ml, 100 μg / ml and 1000 μg / ml, respectively. On the third day, 0.25% trypsin-EDTA solution (Trypsin-EDTA solution) was treated to harvest the cells and counted the cells with a Coulter counter.

Then, 100 μl of 1N NaOH solution per 2 × 10 ⁵ cell number was added to each treatment group, and the cells were lysed at 37 ° C. for 12 hours, and then synthetic melanin (Sigma. Chemical Co., St, Louis, Misso) 10mg dissolved in 10ml of 1N NaOH to prepare 1mg / ml of stock solution, 700g / ml, 300g / ml, 100g / ml, 70g / ml, 30g / ml, 10g / A standard solution was prepared by diluting to ml, 7g / ml, 3g / ml, 1g / ml, 0.1g / ml and 0g / ml.

The sample and the standard solution were placed in a 96 well assy plate, and the absorbance was measured with a spectrophotometer at 490 nm, and then the measured absorbance value was applied to a standard straight line made of synthetic melanin, and converted into melanin amount.

Table 3 Melanin Production

division Concentration 10 μg / ml 100 μg / ml 1000 μg / ml WE 92% 83% 32% EE 87% 78% 20% CE 84% 71% 25%

As shown in Table 3 and Figure 3, the quinine extracts 10 ㎍ / ㎖ and 100 ㎍ / ㎖ treated with a low melanin production inhibitory treatment, 1000 ㎍ / ㎖ treated quince lyophilized extract (CE), hot water extract (WE) And Chinese ethanol extract (EE) can be seen that the melanin production inhibition rate is high.

<Test Example 5> (stability test)

In order to test the stability of the whitening composition containing the Chinese quince extract according to the present invention, the nutrient lotion prepared in Example 4 and the cream prepared in Example 5 were used at 4 ° C, room temperature (25 ° C), 40 ° C and 50 ° C. After being left for months, the results of observing the stability of each composition are shown in Table 4.

TABLE 4 Stability Test Results

division Storage temperature (℃) 4 25 40 50 Example 4 stability stability stability stability Example 5 stability stability stability stability

As shown in Table 4, it can be seen that the whitening composition according to the present invention maintains stability even after a long time.

The whitening composition according to the present invention contains a quince extract, which is a natural material, and inhibits the activity of tyrosinase involved in the proliferation of melanocytes and the production of melanin, thereby reducing the amount of melanin, and at the same time for a long time Stability can be maintained even during storage.

Claims (3)

Whitening composition containing Chinese quince extract as an active ingredient The method of claim 1, The composition is a whitening composition, characterized in that it contains 0.01-10% by weight of the quince extract The method according to claim 1 or 2, The Chinese quince extract is a whitening composition, characterized in that one or two selected from the group consisting of lyophilized extract, hot water extract or ethanol extract of Chinese quince