KR19980034292A - Skin whitening composition containing galloylquinic acid - Google Patents

Abstract

The present invention relates to a skin whitening composition containing galloyl quinic acid as an anti-fog and freckles improving and skin whitening agent.

Description

[Name of invention]

Skin whitening composition containing galloylquinic acid

Detailed description of the invention

[Purpose of invention]

The present invention relates to a skin whitening composition containing galloyl quinic acid as an anti-finite freckles and skin whitening agent.

[Technical Field to which the Invention belongs and Prior Art in the Field]

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 solar ultraviolet light, fatigue and stress. Melanin is a type of amino acid tyrosine (tyrosine) enzyme called tyrosinase (tyrosinase) acts to convert to dopa (DOPA), dopaquinone (dopaquinone) is produced through a non-enzymatic oxidation reaction. Because tyrosinase plays such an important role in melanin synthesis process, by combining substances having inhibitory activity against tyrosinase, such as hydroquinone, ascolic acid, kojic acid, and glutathione, in ointments or cosmetics, Although it has been used for the purpose of skin whitening, blemishes, and freckles, the use is limited because it causes irritation to skin or poor product stability, and the effect is also weak.

[Technical problem to be achieved]

The present inventors have conducted numerous studies and experiments to solve these problems and to develop better whitening materials, and the galloylquine isolated from natural products while searching for a material having excellent whitening effect among natural products that have already been proved in safety. As well as showing an excellent inhibitory effect of tyrosinase on acid, the present invention was found to be effective in melanin production inhibition experiments and human experiments using cultured cells.

[Configuration and Function of Invention]

The present invention relates to a composition for skin whitening, characterized in that it contains 0.001 to 20% by weight of galloyl quinic acid with respect to dry weight.

In the composition for skin whitening of the present invention, the galloylquinic acid is 3-o-galloyl-quinic acid, 4-o-galloyl-quinic acid, 5-o-galloyl-quinic acid, 3,5-di-o- One or two or more selected from galloyl-quinic acid, 3,4-di-o-galloylquinic acid and 4,5-di-o-galloylquinic acid are used.

According to the present invention, galloylquinic acid is added in an amount of 0.001-20% by weight, preferably 0.01-10% by weight, to the skin external ointment or cosmetics. When galloylquinic acid is used at 0.001% by weight or less, it is difficult to expect sufficient whitening effect.When it is used at 20% by weight or more, it affects the formulation and product stability, and it is impossible to expect further increase in effect due to excessive use. Not economical

The skin whitening composition of the present invention is a common cosmetic ingredient in addition to the galloylquinic acid, as emulsifiers, solubilizers, oils, waxes, fatty acids, alcohols, polymers, humectants, skin protectants, thickeners, film forming agents, antioxidants, metals. Ion blockers, sunscreens, discoloration inhibitors, vitamins, astringents, preservatives, fragrances, pigments and the like can be used in a wide variety of applications and properties of the cosmetic.

Skin whitening composition according to the present invention was found to be very effective when used as an external skin ointment or cosmetic. Here, the cosmetics include softening cream, nutrient cream, nourishing cream, massage cream, essence, pack and the like.

Hereinafter, the present invention will be described in more detail based on Experimental Examples and Examples. However, it should not be understood that the technical scope of the present invention is limited thereto.

[Production example]

Isolation of Galloyl Quinic Acid

48.5 kg of fresh Echohorbia Helioscopia L. starch is finely chopped and soaked in 50 L of 80% acetone solution and extracted at room temperature for 10 days. The extract was concentrated with a vacuum concentrator, filtered through a filter paper (Whatman No. 1) to remove the precipitate, and dried under reduced pressure to obtain 840 g of the extract. 360 mg of 3-o-galloyl-quinic acid was isolated using sephadex LH-20 column chromatography (H ₂ O-MeOH → H ₂ O-acetone).

Experimental Example 1

The tyrosinase inhibitory effect on the galloyl quinic acid isolated in the preparation example was measured as follows.

Enzyme tyrosinase was extracted from the mushroom (mushroom), Sigma (Sigma) was used. First, a solution of tyrosine, a substrate, was dissolved in sodium phosphate buffer (0.05 mol, pH 6.8) in a concentration of 1.5 mM, and 0.1 ml of 0.3 ml spectrophotometer Cuvette was added, and a cofactor of waveguide was 0.6 mM. Make a concentration and add 0.01 ml each. To each is added galloylquinic acid at different concentrations, and sodium phosphate buffer is added so that the volume of galloylquinic acid added to each is 0.1 ml. Here, tyrosinase is prepared in sodium phosphate buffer at 60 U / ml, and 0.1 ml of each is added to proceed with the reaction. At this time, the control group (Blank) is added only 0.1ml of buffer instead of tyrosinase.

The reaction was carried out at 37 ° C. using a spectrophotometer (Beckman DU-7500), and the change in absorbance at 475 nanometers was measured for 5 minutes every minute. The inhibition rate of tyrosinase was determined by the difference of the reaction rate (rate of change in absorbance with time, dA / dmim) obtained as follows.

The concentration of galloyl simic acid when the inhibition rate is 50% was expressed as IC 50 (inhibition concentration 50), and the IC 50 values for each galloyl quinic acid are shown in Table 1 below.

TABLE 1

Tyrosinase Inhibitory Effect of Galoyl Quinic Acids (IC50)

From the results of Table 1, it can be seen that galloyl quinic acid has an excellent inhibitory effect on tyrosinase.

Experimental Example 2

The whitening effect at the cellular level was examined by adding galloyl quinic acid isolated in the above preparation to the culture of rat melanoma cells (B-16 mouse melanoma cells) (Lotan R., Lotan D. Cancer Res). 40: 3345-3350, 1980).

Galoyl quinic acid is added to the culture medium of B-16 melanoma cells and cultured for 3 days, and then cells are trypsinized, separated from the culture vessel, centrifuged, and melanin is extracted. To this, 1 ml of sodium hydroxide solution (1N concentration) was added, boiled for 10 minutes to dissolve the melanin, and the absorbance was measured at 400 nanometers using a spectrophotometer indicating the amount of melanin produced as the absorbance of a unit cell allowance (10 ⁶ cells). It was performed by the method. The results are shown in Table 2 below.

TABLE 2

Inhibitory Effect of Galoyl Quinic Acid on Melonogenesis in B-16 Melanoma Cells

* Repeat count = 3

From the results of Table 2, it can be seen that galloyl quinic acid has strong and excellent melanin production inhibitory ability. This demonstrates that the composition for skin whitening of the present invention can be very usefully used for improving skin or freckles or skin whitening.

Thus, the composition for skin whitening of Examples 1 to 5 was prepared according to the following composition ingredients and composition ratios with galloyl quinic acid having an excellent melanin production inhibitory effect.

Example 1

Example 2

Example 3

Example 4

Example 5

Experimental Example 3

20 healthy male subjects were covered with aluminum foil with two perforated lines of 2cm x 2cm in the upper arm of each arm, and 120mJ / ㎠ light at 50cm distance using a ORIEL Solar Simulator 1000W. Investigate. The irradiation site was washed well with 70% aqueous ethanol solution before irradiation. After UV irradiation, Examples 1, 3, and 5 were applied to one row of three irradiation sites, and each base was applied twice a day for four weeks to the other row. Four weeks later, the degree of pigmentation was visually determined by comparison with the control group (gigi coating), and the criterion was a three-step evaluation of remarkable inhibitory effect, slight inhibitory effect, and no inhibitory effect. The results are shown in Table 3 below.

TABLE 3

Pigmentation inhibitory effect (persons)

As can be seen from the results of Table 3, Examples 1, 3 and 5 according to the present invention are all at least 14 people at least a slight pigmentation inhibitory effect is more excellent pigmentation composition for skin whitening according to the present invention Demonstrates an inhibitory effect.

Claims (6)

A skin whitening composition comprising galloylquinic acid in an amount of 0.001-20% by weight based on dry weight. The method of claim 1, wherein the galloylquinic acid is 3-o-galloyl-quinic acid, 4-o-galloyl-quinic acid, 5-o-galloyl-quinic acid, 3,5-di-o-galloyl -Quinic acid, 3,4-di-o-galloyl-quinic acid and 4,5-di-o-galloyl-quinic acid is one or two or more selected from the composition for skin whitening. The skin whitening composition according to claim 1, which contains 0.01-10% by weight of galloylquinic acid. The composition for skin whitening according to claim 1, which is a cosmetic composition. The skin whitening composition according to claim 1, which is a composition for external application of the skin. 5. The composition for skin whitening according to claim 4, wherein the cosmetic is a softening cream, a nutrient cream, a nourishing cream, a massage cream, an essence or a pack.