KR100710657B1 - Whitening cosmetic composition containing dihydroquercetin - Google Patents

Abstract

The present invention relates to a cosmetic composition for whitening, and to a whitening cosmetic composition containing Dihydroqercetin as an active ingredient, which shows an excellent effect of inhibiting tyrosinase activity and melanin synthesis.

Dihydroquercetin, whitening, cosmetic

Description

Whitening cosmetic composition containing Dihydroquercetin

The present invention relates to a cosmetic composition for whitening, and to a whitening cosmetic composition comprising Dihydroqercetin as an active ingredient, which shows excellent results of inhibiting tyrosinase activity and melanin synthesis.

Hyperpigmentation of the skin involves over-synthesis and distribution of melanin pigment due to abnormalities in the body, such as hormonal abnormalities, genetic diseases, irrespective of ultraviolet rays and excessive UV irradiation.

The proper amount of melanin pigment in the skin keeps the skin healthy and absorbs ultraviolet rays.However, the excess melanin pigment makes the skin black and shows an uneven skin color. Research is underway to inhibit pigment production.

As a whitening ingredient, extracts obtained through extraction and purification from natural plants, such as ascorbic acid, kojic acid, arbutin, hydroquinone, hydroquinone, etc. Has been used. Related patents include ascorbic acid (Japanese Patent Laid-Open No. 4-9320), ascorbic acid (Korean Patent 0417874), hydroquinone (Japanese Laid-Open Patent Publication No. 6-192062), kojic acid (Japanese Laid-Open Patent Application No. 56-7710), and arbutin (Japanese Laid-Open Patent Application). 4-9315) and there are many patents related to this. However, among the aforementioned ingredients, hydroquinone has severe skin side effects, which is limited to use in cosmetics. Although kojic acid has an excellent whitening effect, safety problems are raised in Japan, and ascorbic acid has excellent safety and efficacy. Nevertheless, there are many problems such as O _{2 in} the air, reaction with metal ions in the sanction, and stability when hydrated in water.

Therefore, in recent years, many efforts have been made to research whitening materials having excellent safety and effectiveness using whitening raw materials extracted from natural plants at home and abroad. Therefore, while investigating the whitening ingredients extracted from many natural materials, the researchers found that the dihydroqercetin purified from Larix Sibirica Wood extract had a high whitening effect, and among the many polyphenols contained in Larix Sibirica Wood, more than 90% of the dihydroqercetin was found. It was found that the concentrated crystal raw material is very effective in the whitening effect.

It is an object of the present invention to provide a whitening cosmetic containing high purity Dihydroqercetin purified from natural plant extracts that are excellent in whitening and safe for humans.

It is also an object of the present invention to provide a whitening composition having a function of inhibiting tyrosinase activity. It is also an object of the present invention to provide a whitening composition having a function of inhibiting melanin synthesis.

In order to achieve the above object, the present invention provides a cosmetic composition containing Dihydroqercetin represented by the following formula (1).

Dihydroqercetin is characterized by high-purity separation from Larix Sibirica wood, a conifer that occupies a vast Siberian region. Larix Sibirica wood contains a variety of flavonoids, which contain Dihydroquercetin, Aromadendrin, Quercetin, eriodictiol and Nariagenia, among which Dihydroquercetin is highly purified over 90%. Dihydroquercetin used in the present invention is a raw material purchased from "Bioflavon", characterized in that it contains more than 90% of Dihydroquercetin, it is characterized in that it contains Aromadendrin, Eriodictiol, Quercetin, Naringenin and the like as other impurities. However, although Dihydroquercetin was studied as a raw material of Bioflavon in this study, if Dihydroquercetin is contained in high concentration, it is not limited to Bioflavon.

In another aspect, the present invention can provide a whitening cosmetic composition containing one or two or more of the antioxidants such as Dihydroqercetin and EGCG, gamma -Glabridin, Co-enzime Q-10, BHT, BHA. Hereinafter, the present invention will be described in detail.

The inventors found that the whitening effect was very excellent while examining the possibility of whitening effect of Dihydroqercetin, and based on this, Epigallocatechin gallate (EGCG), Butylated hydroxytoluene (BHT), Butylated Hydroxyanisole (BHA) for the purpose of whitening synergy and stabilization of Dihydroqercetin In addition, many antioxidants such as gamma-Glabridin, Co-enzyme Q-10, Ferulic Acid, DL-α-Tocopherol, and Propyl gallate were examined simultaneously to complete the present invention.

In the present invention, a cosmetic composition having excellent whitening effect was prepared by blending 0.001 to 3.0% by weight of Dihydroqercetin with skin cosmetics, and most preferably, 0.001 to 1.0% by weight of Dihydroqercetin. Experimental results showed that when Dihydroqercetin was blended more than 1.0%, the appearance of the cosmetics was slightly yellowish, which reduced the value of the product.

In addition, the Dihydroqercetin is formulated in a preferred concentration, and in addition, one or two of the aforementioned EGCG, BHA, BHT, r-Glabridin, Co-enzime Q-10, Ferulic Acid, DL-α-Tocopherol, Propyl Gallate, etc. It has been found to be more effective when added in the range of 0.001 to 0.1% by weight of the total cosmetic composition.

In addition, the cosmetic composition of the present invention may further contain at least 0.001 to 3.0% by weight of one or more such as Arbutin, Kojic acid, Rucinol, Vitamin C and Vitamin C derivatives, Mulberry ext, licorice extract for the purpose of skin whitening effect, For the purpose of improving wrinkles, it may further contain 0.001 to 2.0% by weight of one or more of Retinol and its derivatives, Indol Acetic Acid and its derivatives, Adenosin, tocopherol and its derivatives, and kinitin.

Hereinafter, preferred examples are provided to help understanding of the present invention. However, the following examples are provided only to more easily understand the present invention, and the present invention is not limited to the following examples.

Example 1 Cosmetic Composition Containing Dihydroqercetin

* Flexible Lotion (Skin) Manufacturer

0.3 wt% Dihydroqercetin, 7.0 wt% Glycerin, 4.0 wt% 1,3-butylene glycol, 0.3 wt% Hyaluronic Acid, 0.1 wt% Allantoin, 0.1 wt% DL-Pantenol, 0.02 wt% EDTA-2Na, Ethanol 8.0 A flexible lotion containing Dihydroqercetin was prepared by mixing 20% by weight, 0.4% by weight of polysorbate, 0.6% by weight of octyldodeces-16, 0.3% by weight of paraoxybenzoic acid ester, and a small amount of dye, aroma and residual purified water.

* Manufacture of nutritional cream

Dihydroqercetin 0.5 wt%, Beeswax 0.7 wt%, Setostearyl alcohol 0.5 wt%, Glyceryl monostearate 1.1 wt%, Paraoxybenzoic acid ester 0.3 wt%, Polyoxyethylene sorbitan triisostearate (20, EO) 1.1 Weight%, Cyclomethicone 1.0 weight%, Dimethicone 0.3 weight%, Jojoba oil 1.0 weight%, Squalane 2.0 weight%, Octyldodecanol 2.0 weight%, Liquid paraffin 3.0 weight%, Glycerin 3.0 weight%, Glycerin 4.0 weight% , Nutritional cream containing Dihydroqercetin was prepared by mixing 3.0% by weight of 1,3-butylene glycol, 0.08% by weight of Carvermo 940 and a trace amount of pigment, aroma and residual purified water.

<Example 2: Cosmetic composition containing antioxidants of Dihydroqercetin, Epigallocatechin gallate (EGCG), Propyl gallate, Co-enzyme Q-10, gamma-glabridin

* Flexible Lotion (Skin) Manufacturer

The preparation of the flexible lotion of Example 1 was carried out in the same manner as the preparation of the flexible lotion of Example 1, except that 0.01 wt% of EGCG and 0.01 wt% of propyl gallate were added to the same composition.

* Manufacture of nutritional cream

In the preparation of the nutrition cream of Example 1 was always the same as the nutrition cream preparation of Example 1 except that 0.003% by weight of Co-enzyme Q-10, 0.003% by weight of gamma-glabridin to the same composition.

Experimental Example 1 Test for Measuring Mushroom Tyrosinase Activity of Dihydroqercetin

Tyrosinase activity was shown to measure DOPA oxidase activity. Prepare tyrosinase at a concentration of 1,500-2,000 u / ml. 850 µl of 0.1M Sodium pyosphate buffer (pH 7.0), 50 µl of test substance and 50 µl of tyrosinase are mixed in a micro tube and left at 37 ° C. for 6 minutes.

After adding 50 μl of 6 mM L-DOPA, the mixture was reacted at 37 ° C. for 1 minute. The absorbance was measured at 490 nm.

  Measurement of Mushroom tyrosinase Activity of Dihydroquercetin Test substance density activation (%) Control 100 Arbutin 0.1% (w / v) 79 Dihydroqercetin 0.01% (w / v) 91 Dihydroqercetin 0.05% (w / v) 85 Dihydroqercetin 0.1% (w / v) 78

The inhibition rate of enzyme activity is obtained by the following equation.

Active (%) = [(Control A 490 Sample A 490) / Control A 490] X 100 (%)

In this DATA, the no treatment group control was 100, and there was no inhibitory effect on the mushroom tyrosinase activity. The lower the result, the better the mushroom tyrosinase activity inhibition effect and the higher whitening effect is expected.

Experimental Example 2: Antioxidant Synergy of Dihydroqercetin (Mushroom tyrosinase Activity Test)

Tyrosinase activity was shown to measure DOPA oxidase activity. Prepare tyrosinase at a concentration of 1,500-2,000 u / ml. 850 µl of 0.1M Sodium pyosphate buffer (pH 7.0), 50 µl of test substance and 50 µl of tyrosinase are mixed in a micro tube and left at 37 ° C. for 6 minutes.

After adding 50 μl of 6 mM L-DOPA, the mixture was reacted at 37 ° C. for 1 minute. The absorbance was measured at 490 nm.

  Synergistic Effect of EGCG Inhibiting Mushroom Tyrosinase Activity Test substance density activation (%) Control 100 Arbutin 0.1% (w / v) 79 Dihydroqercetin 0.01% (w / v) 91 EGCG 0.01% (w / v) 93 Dihydroqercetin 0.05% (w / v) 85 Dihydroqercetin0.05%) + EGCG (0.01%) 0.05% (w / v) + 0.01% (w / v) 77 Dihydroqercetin 0.1% (w / v) 78

The inhibition rate of enzyme activity is obtained by the following equation.

Active (%) = [(Control A 490 Sample A 490) / Control A 490] X 100 (%)

In this data, the control group is 100, which has no inhibitory effect on mushroom tyrosinase activity. The lower the result, the better the mushroom tyrosinase activity inhibition effect and the higher whitening effect. In Table 2, the activity was 85 at Dihydroquercetin 0.05%, and the activity was synergistic at 77 when EGCG 0.01% was added at the same concentration as Dihydroquercetin.

Experimental Example 3 Test of B16 F10 tyrosinase Activity Tested and Treated with Dihydroqercetin

Melanin synthesis may affect not only the activity of intracellular tyrosinase but also the protein expression level of tyrosinase, and the intracellular tyrosinase activity was measured after culturing by adding concentrations of test substances to the culture medium of B16 F10 cells (purchased from Korea Cell Line Bank). .

In the test method, the cultured cells are collected and lysed using RIPA lysis buffer.

The lysed cells are transferred to a micro tube and centrifuged for 5 minutes at 12,000 rpm.

The supernatant is used to measure tyrosinase activity. Activity measurement is the same as the activity measurement method of mushroom tyrosinase, and 50 μl of the supernatant obtained previously is used instead of mushroom tyrosinase.

  Activity measurement results of B16 F10 tyrosinase treated and cultured with test substance containing dihydroqercetin Test substance density activation (%) Control 100 Arbutin 0.1% (w / v) 114 DHQ 0.05% (w / v) 21 DHQ 0.1% (w / v) 14.9 DHQ 0.15% (w / v) 7

The inhibition rate of enzyme activity is obtained by the following equation.

Active (%) = [(Control A 490 Sample A 490) / Control A 490] X 100 (%)

In this data, the control group is 100, which has no inhibitory effect on mushroom tyrosinase activity. The lower the result, the better the mushroom tyrosinase activity inhibition effect and the higher whitening effect. In Table 3, Dihydroquercetin has a superior whitening effect at an equivalent content compared to Arbutin, which is widely known as a whitening effect, and shows a very good whitening effect depending on the concentration of Dihydroquercetin.

Experimental Example 4 Measurement of Melanin Content Change According to Test Substance Including Dihydroqercetin

Inoculate the cells in 6 well plates at a concentration of 20,000 cells / ml and incubate 24 hours prior. After pre-culture, replace the medium added with theophiline 2mM, α-melanocyte stimulating hormone (α - MSH) 500nM and 0.1% Arbutin, 0.01%, Dihydroqercetin 0.01%, 0.05%, 0.1%, 0.15%. After changing the medium and incubating for about 72 hours, the cells are recovered by centrifugation. The recovered cells are transferred to a micro tube, washed with PBS (Phosphate Buffered Saline) and centrifuged twice. The supernatant is removed and 1N NaOH is added to cause liquefaction of melanin which is insoluble in water and then treated at 70 ° C. for 1 hour. Since the absorbance at 405nm was measured and expressed as a relative value.

  Results of Changes in Melanin Content of Test Substances Including Dihydroqercetin Test substance density activation (%) Control 100 Arbutin 0.1% (w / v) 109 DHQ (0.05%) 0.05% (w / v) 24 DHQ (0.1%) 0.1% (w / v) 17.7 DHQ (0.15%) 0.15% (w / v) 9.6

The melanin content change is calculated by the following equation.

Melanin content (%) = [(Control A 405 Sample A 405) / Control A 405] X 100 (%)

In this data, the untreated group control is 100. There is no significant change in melanin content, and it can be seen that the whitening effect is very excellent as it can be seen that the melanin content is drastically reduced depending on the increase of the dihydroquercetin concentration.

The present invention provides a whitening cosmetic composition which is very effective for the skin dull, blemishes, and freckles with excellent melanogenesis inhibitory action of Dihydroqercetin.

Claims (8)

A whitening cosmetic composition containing 0.001 to 3.0% by weight and 0.001 to 0.1% by weight, respectively, of dihydroqercetin and Epigallocatechin gallate (EGCG) separated and purified from Larix Sibirica wood, based on the total weight of the cosmetic composition. [Formula 1]

The whitening cosmetic composition of claim 1, wherein the dihydroqercetin is contained in an amount of 0.001 to 1.0% by weight based on the total weight of the cosmetic composition. delete delete delete  The whitening cosmetic composition according to claim 1 or 2, wherein the formulation of the cosmetic composition is a flexible lotion, astringent lotion, nourishing lotion, nourishing cream, massage cream, essence, pack, powder, ointment, spray or gel. An anti-aging cosmetic composition containing Dihydroqercetin and Epigallocatechin gallate (EGCG) purified from Larix Sibirica wood containing 0.001 to 3.0% by weight and 0.001 to 0.1% by weight, respectively, based on the total weight of the composition. delete