JP2000256176A - Skin cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject cosmetic excellent in prevention of skin aging for preventing or improving wrinkles, the deterioration of elasticity and dullness of skin without problems about safety or feeling of use by including an elastase inhibitor extracted from a fruit of Vaccinium vitis-idaca L. SOLUTION: This cosmetic contains an elastase inhibitor extracted from a fruit of Vaccinium vitis-idaca L. The above ingredient is obtained by using a flesh part freed from seeds of the fruit of the Vaccinium vitis-idaca L. and extracting the flesh part with water, methanol, ethanol, propanol, 1,3-butylene glycol or a mixture thereof as an extracting solvent at room temperature or under heating to 70 deg.C using an optional apparatus. The amount of the formulated extract in the skin cosmetic is 0.01-10 wt.% expressed in terms of a dried substance.

Description

Detailed Description of the Invention The present invention relates to a skin cosmetic which prevents or improves skin aging such as "wrinkles" based on elastase inhibitory activity and / or promotion of collagen production.

2. Description of the Related Art The skin is divided into three layers: epidermis, dermis, and subcutaneous tissue. The dermis is extremely important for the structure and maintenance of the skin, and is made firmly and flexibly by fibers such as elastin and collagen. Is formed. These proteins, such as elastin and collagen, which constitute the fibers of the connective tissue are synthesized by fibroblasts. Fibroblasts control the state of connective tissue by interacting with fibers such as collagen. However, it is believed that the dermis connective tissue of the skin loses contractile force, and further loses strength and elasticity, resulting in sagging and wrinkling of the skin. In recent years, many cosmetics that prevent this skin aging are known, and retinoic acid, α-hydroxy acid, retinol, and the like have been reported as active ingredients. However, these active ingredients have problems in skin irritation and stability, and it has been difficult to say that their effects are sufficient. Also, in plant extracts, raw materials having both elastase inhibitory activity and collagenase inhibitory activity are not well known, and even if they are known, each does not show a remarkable effect. Cowberry (scientific name: Va
ccinium vitis-idaca L .; ) Is a plant of the family Myrtaceae, the fruit of which has been used for food since ancient times. In addition, the extract of the leaves is used for hair and hair cosmetics (Registration No. 2212141, JP-A-7-196456).
The effect was confirmed as.

Accordingly, an object of the present invention is to have an elastase inhibitory action and a collagenase inhibitory action, which are excellent in preventing skin aging for preventing or improving wrinkles, decreased skin elasticity and dull skin, Another object of the present invention is to provide cosmetics having no problem in safety and usability.

Means for Solving the Problems A skin cosmetic which has successfully attained the above-mentioned object is contained in the fruit of a lingonberry which has been confirmed for the first time to contain an elastase inhibitor and a collagenase inhibitor, It has an action and a collagenase inhibitory action.

BEST MODE FOR CARRYING OUT THE INVENTION The berry of lingonberry, which is a raw material of the skin cosmetic of the present invention, uses a pulp portion obtained by removing seeds from the lingonberry. Although it has not yet been confirmed what kind of body promotes these actions, it can be easily extracted by an extraction treatment using water, methanol, ethanol, propanol, 1,3-butylene glycol or a mixture thereof as an extraction solvent. Will be. In extracting the elastase inhibitor and the collagenase inhibitor, it is not necessary to employ a special extraction method, and the extraction can be performed using an arbitrary apparatus while heating at room temperature to 70 ° C. Briefly, an extraction raw material is put into a treatment tank filled with an extraction solvent, and stirred occasionally to elute a soluble component. Thereafter, the residue is filtered to remove the extraction residue to obtain an extract. The obtained extract can be used as it is as a raw material of the skin cosmetic of the present invention, but it can also be concentrated and dried into a dosage form. Since the extract or extract obtained as described above has a fragrance peculiar to lingonberry, it can be used as a skin cosmetic. In addition, since the lingonberry fruit is also used for raw food, the production amount is large and there is no concern about the supply of raw materials. The official blending ratio of the extract of the present invention with respect to skin cosmetics is 0.01 to 10% by weight in terms of dry matter in the case of an unrefined standard extract.

The present invention will be described in more detail with reference to the following examples. Production Example 1 Water or 80% by weight ethanol or 80% by weight methanol or 50% by weight propanol (hereinafter 50% PG) or 50% by weight 1,3-butylene glycol (hereinafter 50) % BG) and add 3 ml while keeping the temperature at 70 ° C.
After gentle stirring for a time, the mixture was filtered using a filter paper to obtain an extract. The extract was concentrated under reduced pressure at 35 ° C., and dried in a vacuum drier to obtain a dry extract (hereinafter referred to as extract). <Table 1> Extract Yield Extraction Solvent Extract Yield (%) Water 12.3 80% Ethanol 10.9 80% Methanol 14.8 50% PG 8.5 50% BG 7.3 Test Example 1 Elastase Activity inhibitory activity Preparation of sample solution: Each extract described in Production Example 1 was dissolved in ethanol, and divided into three concentrations to determine the inhibitory concentration (IC50) and subjected to the following tests. Using a 96-well microplate, add 50 μl of sample solution and 50 μl of enzyme to each well. (Enzyme at this time is elastase type III (Sigma) 5m
g was dissolved in 1 ml of 0.2 M Tris-HCl buffer (pH 8.0) to obtain a stock solution, and stored at -20 ° C. As a control, a 0.2 M Tris-HCl buffer was added instead of the enzyme. Further, the substrate [N-SUCCIN
YL-ALA-ALA-ALA-p-NITROANI
LIDE (manufactured by Sigma) was dissolved in DMSO and 45.1 was dissolved.
Use it as a stock solution at 4 mg / ml. When used, dilute 100-fold with Tris-HCl buffer and use as 1 mM solution.]
100 μl is added and mixed, reacted at 25 ° C. for 50 minutes, and the absorbance at a wavelength of 415 nm is measured. Inhibition rate (%) = {1- (CD) / (AB)} × 10
0 A: Absorbance when no sample is added and enzyme is added B: Absorbance when no sample is added and enzyme is not added C: Absorbance when sample is added and enzyme is added D: Absorbance when sample is added and enzyme is not added The inhibition rate is measured with various changes, and the concentration of the sample solution that inhibits elastase activity by 50% is determined by interpolation. <Table 2> Test results Extraction solvent 50% inhibitory concentration (ppm) Water 58.6 80% Ethanol 45.5 80% Methanol 60.3 50% PG 85.3 50% BG 75.9 Test Example 2 Collagenase inhibitory activity Substrate: Pz-peptide (Pz-Pro-Leu-Gly
-Pro-D-Arg-OH; BACHEM Feni
ChemMalien AG (0.39 mg) and 0.1 M Tris-HCl buffer (pH 7.1, containing 20)
1 mM (equivalent to 0.5 M). The cleavage site is between Leu and Pro. Enzyme: 5 mg of collagenase type IV (manufactured by Sigma) is dissolved in 1 ml of water, and 100 μl each is dispensed at −20 ° C.
Keep in. At the time of use, 4.9 ml of water is added to 100 μl and diluted 50-fold for use in the reaction. Test method: Add 50 μl of sample solution, 50 μl of enzyme solution and 400 μl of substrate solution, and incubate at 37 ° C. for 30 minutes. Thereafter, the reaction is stopped with 1 ml of a 25 mM citric acid solution and extracted with 5 ml of ethyl acetate. After centrifugation (3,000 rpm, 10 minutes), the absorbance (A) of the ethyl acetate fraction at a wavelength of 320 nm was measured using ethyl acetate as a control. Separately, distilled water was used in place of the enzyme solution, and the same operation was carried out to make a blank test (B). Further, distilled water was used in place of the sample solution, and the same operation was made as (C). The blank test of (C) was taken as (D). Inhibition rate (%) = {1- (AB) / (CD)} × 10
0 A: Absorbance when sample is added and enzyme added B: Absorbance when sample is added and enzyme is not added C: Absorbance when sample is not added and enzyme is added D: Absorbance when sample is not added and enzyme is not added The inhibition rate is measured with various changes, and the concentration of the sample solution that inhibits collagenase activity by 50% is determined by interpolation. <Table 3> Test results Extraction solvent 50% Inhibitory concentration (ppm) Water 98.0 80% Ethanol 120.5 80% Methanol 112.5 50% PG 118.0 50% BG 122.5 Formulation Example 1 Production Example An emulsion was prepared using the dried extract prepared in 1. Stearic acid 2 parts Squalane 2 parts Olive oil 2 parts Cetanol 7 parts Jojoba oil 2 parts Polyoxyethylene (40EO) hydrogenated castor oil 1 part Glycerin 10 parts Water extract of Production Example 1 3 parts Purified water Preparation Example 2 A lotion was prepared using the dry extract prepared in Preparation Example 1. Glycerin 10 parts 1,3-butylene glycol 3 parts Polyoxyethylene sorbitan oleate (20EO) 3 parts Methyl parahydroxybenzoate 0.5 parts Citric acid 0.1 parts Sodium citrate 1 part Fragrance 0.05 parts Production 3 parts of 80% ethanol extract of Example 1 Purified water Remainder (total amount is 100 parts) Formulation Example 3 Preparation A cream was prepared using the dry extract prepared in Example 1. Liquid paraffin 5 parts Salami beeswax 4 parts Cetanol 3 parts Squalane 10 parts Lanolin 2 parts Stearic acid 1 part Polyoxyethylene sorbitan oleate (20EO) 3 parts Glyceryl monostearate 3 parts 1,3-butylene glycol 3 parts Paraoxyl 50% PG extract 1 part 50% BG extract 1 part purified water balance of example 1 benzoate 0.5 parts perfume, 0.05 parts preparation example 1 (100 parts total) formulation using practice EXAMPLE Group 10 using the cosmetics of Production Example 2 for 10 women between the ages of 29 and 48 (Group A), Production Example 2
Was divided into groups (group B) using the same composition except for the extract of lingonberry and used twice a day in the morning and evening for 3 months. <Table 4> Group A formulation use results <Table 5> Group B formulation use results

Industrial Applicability The skin cosmetic of the present invention has an excellent effect on providing smooth skin and preventing or improving skin aging such as wrinkles.

Claims (7)

[Claims] 1. An elastase inhibitor comprising an elastase inhibitor extracted from lingonberry fruits as an active ingredient. 2. An extract obtained by extracting a lingonberry fruit with water, methanol, ethanol, propanol, 1,3-butylene glycol or a mixture thereof, as an active ingredient. Elastase inhibitors. 3. A collagenase inhibitor comprising, as an active ingredient, a collagenase inhibitor extracted from lingonberry fruits. 4. An extract obtained by extracting a lingonberry fruit with water, methanol, ethanol, propanol, 1,3-butylene glycol or a mixture thereof, as an active ingredient. Collagenase inhibitors. (5) A skin cosmetic comprising (1) and (2). (6) A skin cosmetic comprising (3) and (4). 7. A skin cosmetic comprising the composition of claim 1, 2, 3, or 4.