JP2000247830A - Elastase inhibitor - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an elastase inhibitor suppressing the activity of elastase, restoring and keeping the springiness and elasticity and preventing the aging of skin and keeping the state of fresh and youthful skin by including an extract of a plant such as guava. SOLUTION: The objective inhibitor preferably having the form of a cosmetic can be produced by including an extract of one or more plants selected from guava, guarana, rosemary, Saint-John's wort, Botanpi (root of Paeonia moutan), hop, peony, Sohakuhi (bark of Morus bombycis) and quince. Water and one or more kinds of organic solvents such as methyl alcohol or their mixture can be used as the extraction solvent. The extraction temperature is preferably 40-120 deg.C and the extraction time is 1-10 days in the case of extracting at room temperature or thereabout and 0.5-120 hr in the case of extracting at >=40 deg.C. The compounding ratio of the extract in the inhibitor is preferably 0.001-5 wt.%.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention has an elastase inhibitory activity, can prevent skin aging by maintaining elasticity and firmness of the skin, and can maintain a young and fresh skin condition. The present invention relates to an elastase inhibitor, particularly an elastase inhibitor prepared in the form of a cosmetic.

[0002]

2. Description of the Related Art A typical example of a change in appearance caused by aging of the skin is the occurrence of wrinkles or lumps or a decrease in firmness. In particular, aging of the skin caused by exposure to ultraviolet rays is called photoaging. Elastin is an elastic fiber that makes up 2-4% of the dermal extracellular matrix. It is thought that the overexpression of elastase, an elastin-degrading enzyme, due to exposure to ultraviolet light causes the elastin to be denatured and degraded, leading to a decrease in skin elasticity [Cosmetics & Toiletries magazine, Voss
l.113, 51-58, 1998]. Therefore, it is important to prevent the aging of the skin by suppressing the action of elastase and suppressing the denaturation and decomposition of elastin which gives the skin elasticity and firmness. However, at present, an elastase inhibitor with high safety and sufficient effect has not been obtained so far.

[0003]

SUMMARY OF THE INVENTION It is an object of the present invention to prevent aging of the skin by suppressing the activity of elastase to restore and maintain the elasticity and firmness of the skin, and to provide a young and fresh skin condition. An object of the present invention is to provide an elastase inhibitor having an effect of maintaining the elastase inhibitor.

[0004]

Means for Solving the Problems In order to solve the above problems, the present inventors examined elastase inhibitory activity of various plant extracts, and found that guava, guarana, rosemary, hypericum, buttonpi, hop, Peonies,
The present inventors have found that extracts of sow scab and mocca have the desired effects, and have completed the present invention.

[0005] That is, the present invention relates to a method selected from the group consisting of guava, guarana, rosemary, hypericum, buttonpi, hop, peony, soybean and mocca.
It is intended to provide an elastase inhibitor comprising an extract of a species or two or more plants as an active ingredient. In a preferred embodiment of the present invention, the elastase inhibitor is prepared in the form of a cosmetic.

[0006]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The present invention will be described below in detail. Guava, guarana, rosemary, hypericum, buttonpips, hops, peonies, soybeans, and mokka used for extraction are the whole grass, the above-ground parts, leaves, root bark, stems,
Any of roots, branches, fruits, seeds or flowers, or a mixture of two or more of these plant parts may be used. These plant raw materials may be raw or dried.

[0007] Preferably, guava is a leaf of Psidium guajava, a guarana is a seed of Paulinia cupana, a rosemary is a whole plant of a perilla plant, Rosmarinus officinalis, and a hypericum is St. John's wort. Family Hypericum perforatum (Hyp
ericum erectum), the buttonpi is the root bark of the button family plant (Paeonia suffruticosa), the hop is the flower of the mulberry plant hop (Humulus lupulus), the peonies are the roots of the button family plant peonies (Paeonia lactiflora), and The root bark and mokka of the family plant Yamaguwa (Morus bombycis) use the fruits of the rose family plant karin (Chaenomeles sinensis), and these plant materials are pulverized and used for extraction.

The extract of guava, guarana, rosemary, hypericum, buttonpi, hops, peonies, soybeans and mocca used in the present invention is an extract obtained by extracting the above-mentioned plant material with a solvent at room temperature or under heating. , Its diluent or concentrate, or its dried product. In the present invention, two or more of the above plants can be mixed for extraction, and the extracts of each plant can be mixed and used.

In the present invention, it is preferable to use extracts of guava, guarana, rosemary, hypericum, buttonpi, hop and mocca from the viewpoint of elastase inhibitory effect. More preferably, extracts of guava, rosemary and buttoned peas are used.

As the solvent used for the extraction, water, lower alcohols (such as methyl alcohol, ethyl alcohol or butanol), acetone, ethyl acetate, and 1,3-
One or more kinds of organic solvents such as butylene glycol or propylene glycol can be used by being appropriately mixed.

[0011] The extraction may be performed in a usual manner. The extraction temperature is usually in the range of 4 to 120C, preferably 40 to 120C. Although the extraction time varies depending on the extraction temperature, it is generally 1 to 10 days for extraction near room temperature, and 0.5 to 120 hours for extraction at 40 ° C. or higher.

The extract thus obtained can be used as it is for the elastase inhibitor of the present invention. However, this extract is concentrated or diluted with an appropriate solvent (eg, water or lower alcohol) before use. Can also. Further, the extract can be evaporated to dryness and used as the elastase inhibitor of the present invention.

The elastase inhibitor of the present invention is prepared in the form for external use, especially in the form of cosmetics and baths. As cosmetics, gel cream, face wash cream, lotion,
Emulsions and the like can be mentioned, and examples of bath preparations include solid and liquid ones.

The mixing ratio of the plant extract in the elastase inhibitor of the present invention varies depending on the concentration of the plant extract and the form of the elastase inhibitor, but is usually 0.0001 to 99% by weight based on the total amount of the elastase inhibitor. , Preferably 0.001 to 10% by weight, more preferably 0.001 to 10% by weight.
It is in the range of 5% by weight.

The elastase inhibitor of the present invention contains, in addition to the plant extract as an active ingredient, various components generally used in preparing various elastase inhibitors according to their forms. These components are, for example, oils, surfactants, humectants, thickeners, preservatives, fragrances, colorings, drugs and the like.

[0016]

EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.

Example 1 Preparation of Guava Extract 30 g of guava was immersed in 300 mL of a 50% aqueous ethanol solution and extracted at room temperature for one week. The insolubles were filtered off and the filtrate was evaporated, yielding about 6.0 g of solids.

Example 2 Preparation of Guarana Extract 30 g of guarana was immersed in 300 mL of a 50% aqueous ethanol solution and extracted at room temperature for one week. The insolubles were filtered off and the filtrate was evaporated, yielding about 6.2 g of solid.

Example 3 Preparation of rosemary extract 30 g of rosemary was added to 300 m of a 50% aqueous ethanol solution.
L and extracted for 1 week at room temperature. The insolubles were filtered off and the filtrate was evaporated, yielding about 3.7 g of solid.

Example 4 Preparation of Hypericum perforatum extract 30 g of Hypericum perforatum was added to 300 m of a 50% aqueous ethanol solution.
L and extracted for 1 week at room temperature. The insolubles were filtered off and the filtrate was evaporated, yielding about 4.6 g of solids.

Example 5 Preparation of a buttonpi extract 30 g of a buttonpi extract was immersed in 300 mL of a 50% aqueous ethanol solution and extracted at room temperature for one week. The insolubles were filtered off and the filtrate was evaporated, yielding about 7.4 g of solids.

Example 6 Preparation of Hop Extract 30 g of hops were immersed in 300 mL of a 50% aqueous ethanol solution and extracted at room temperature for one week. The insolubles were filtered off and the filtrate was evaporated, yielding about 10.5 g of solid.

Example 7 Preparation of a peony extract 30 g of a peony extract was added to 300 mL of a 50% aqueous ethanol solution.
And extracted at room temperature for one week. Filter the insoluble matter,
The filtrate was evaporated to give about 10.0 g of solid.

Example 8 Preparation of Sophora oleracea extract 30 g of Sophora oleracea in 300 mL of a 50% aqueous ethanol solution
And extracted at room temperature for one week. Filter the insoluble matter,
The filtrate was evaporated to give about 4.0 g of solid.

Example 9 Preparation of Mokka Extract 30 g of mokka was immersed in 300 mL of 50% aqueous ethanol solution and extracted at room temperature for one week. The insolubles were filtered off and the filtrate was evaporated, yielding about 10.0 g of solid.

Comparative Example 1 Preparation of Clara extract (comparative product) 30 g of Clara was immersed in 300 mL of a 50% aqueous ethanol solution and extracted at room temperature for one week. The insolubles were filtered off and the filtrate was evaporated, yielding about 6.3 g of solids.

Example 10 Measurement of Elastase Inhibitory Activity As a reaction buffer, 0.1 M HEPES and 0.5 M Na were used.
Elastase derived from human leukocytes (ELASTIN PRODUCT CO., INC.) Was used as elastase using Cl (pH 7.4). This elastase was dissolved in a reaction buffer so as to have a concentration of 5 μg / mL, and 25 μL of the solution was dispensed into a 96-well plate. Furthermore, 400 μg of each of the above plant extracts (prepared in Examples 1 to 9 and Comparative Example 1)
/ ML was dissolved in a reaction buffer to prepare a plant extract solution, and these solutions were added to the 96-well plate at 50 μL each. Warm at 37 ° C. for 15 minutes and then on ice 8 mM methoxy-succinyl-alanyl-alanyl-prolyl-valine-p-nitroanilide (ELASTIN PRODUCT CO., INC.) 2 as elastase substrate
5 μL was added, and the mixture was heated at 37 ° C. for 30 minutes. 30 minutes later,
The absorbance at 415 nm was measured immediately. As a comparative product, Clara extract (JP-A-10-17460), which is already known to have elastase inhibitory activity, was used.
Elastase inhibition was determined by the following equation:

## EQU1 ## Elastase inhibition rate (%) = [1- (A ₁ / A ₀ )]
x 100 where A ₁ is the absorbance in the presence of the inhibitor and A ₀ is the control
(No inhibitor added)].

The results are shown in Table 1 below.

[Table 1] The above results revealed that these plant extracts have elastase inhibitory activity. In particular, it was found that the extracts of guava, rosemary and buttonpi have high elastase inhibitory activity, then the extracts of guarana, hypericum, mocca and hops have high activity, and then the activities of soybean and peonies are higher. . It was also found that these elastase inhibitory activities were higher than Clara extract already known to have elastase inhibitory activity.

Hereinafter, various dosage forms of the elastase inhibitor of the present invention will be exemplified. Example 11 Emulsion An emulsion having the following formulation was prepared.

[Table 2] The component A is dissolved by heating and kept at 80 ° C. Separately, add Component B heated and dissolved at 80 ° C. to Component A, and mix well. The mixture was cooled while stirring, and the component C was added at 50 ° C. to obtain an emulsion.

Example 12 Lotion A lotion having the following formulation was prepared.

[Table 3] Stir and mix all components at room temperature to make a homogeneous solution,
The pH was adjusted to 5.5 to obtain a lotion.

Example 13 Cream A cream having the following formulation was prepared.

[Table 4] Add propylene glycol to purified water, heat to 70 ° C
(Aqueous phase). Mix other ingredients, heat and melt at 70 ° C
(Oil phase). The oil phase was added to the water phase, preliminarily emulsified, and then uniformly emulsified with a homomixer to obtain a cream.

Example 14 In the lotion of Example 12, invention extract 1 was obtained by using a guava extract as a plant extract, invention product 2 was obtained by using a guarana extract, and invention was obtained using a rosemary extract. Article 3,
Invention product 4 as a hypericum extract, invention product 5 as a hop extract, invention product 6 as a peony extract, invention product 7 as a peanut extract, and soybean extract From the age of 20 as a comparative product, a product prepared using purified water in place of the plant extract as a comparative product
A two-month use test (face application, once a day) was performed on 50 year-old women.

(A) Wrinkles and wrinkles after the test and
(B) The improvement effect of the elastase inhibitor of the present invention was evaluated by comparing the skin firmness and the skin condition with the condition before the start of the test. The evaluation was performed by visually observing the condition of the skin and based on the following evaluation criteria. (A) Evaluation criteria for wrinkles and fine wrinkles ++: Clearly disappeared; +: Slightly less noticeable; ±: No change;-: Increased. (B) Evaluation criteria for skin firmness and tarumi ++: greatly improved; +: improved; ±: no change;-: no firmness or more thickening. In this test, no subject had abnormal skin.

The results are shown in Tables 5 and 6 below.

[Table 5]

[Table 6] From the above results, elastase characterized by containing a guava extract, a guarana extract, a rosemary extract, a hypericum extract, a hop extract, a peony extract, a peanut extract, a soybean extract or a mocca extract The inhibitor was found to be effective in improving wrinkles and fine wrinkles, as well as skin firmness and tallness.

[0035]

As described above, guava extract, guarana extract, rosemary extract, hypericum extract, hop extract, peonies extract, peanut extract, soybean extract and mocca extract are excellent. Elastase inhibitory activities, and elastase inhibitors containing these plant extracts, showed improvement in wrinkles and fine wrinkles, as well as skin firmness and tallness.

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification FI FI Theme Court ゛ (Reference) A61K 35/78 A61K 35/78 Q (72) Inventor Kunio Kosaka 2- 2-3 Muroya, Nishi-ku, Kobe-shi, Hyogo Prefecture No. Nagase & Co., Ltd. R & D Center F-term (reference) 4C083 AA111 AA112 AA122 AB032 AB352 AC022 AC072 AC092 AC102 AC122 AC132 AC182 AC242 AC302 AC352 AC422 AC432 AC482 AD092 AD222 AD512 CC01 CC04 CC05 DD23 DD31 EE12 FF05 4C088 AB12 AB32 AB34 AB AB57 AB58 AC01 AC02 AC04 AC05 AC11 BA09 BA10 CA03 MA63 NA14 ZA89 ZC20

Claims (2)

[Claims] 1. An active ingredient comprising one or more plant extracts selected from the group consisting of guava, guarana, rosemary, hypericum, buttonpi, hops, peonies, soybeans and mocca. Elastase inhibitor. 2. The elastase inhibitor according to claim 1, which is prepared in the form of a cosmetic.