JP2002255782A - Elastase activity inhibitor and antiaging agent containing the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antiaging agent preventing the skin from aging by inhibiting activity of elastase degenerating and decomposing an elastin which is one of a substance imparting firmness and slasticity to the skin and restoring and maintaining the firmness and elasticity of the skin. SOLUTION: A solvent extract of Talauma mexicana plant is formulated. The extract of Talauma mexicana has excellent elastase activity inhibiting actions and prevents the skin from aging by restoring and maintaining the firmness and elasticity of the skin.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an elastase activity inhibitor effective for preventing aging of human skin and a composition containing the same. Furthermore, the present invention relates to an anti-aging agent which can be used in the fields of cosmetics, quasi-drugs and the like containing the inhibitor.

[0002]

2. Description of the Related Art According to recent studies on skin aging, changes in the tissue level occurring in the skin where external aging is observed include reduction of collagen and elastin in the skin dermis, hyaluronic acid and the like. Reduced mucopolysaccharides and damage to epidermal cells.

As a cause of skin aging that progresses in parallel, aging is generally the most important factor. Dryness, oxidation, sunlight and the like are also cited as direct factors related to skin aging. .

[0004] Among the above-mentioned skin aging phenomena, the reduction of elastin, which gives a particularly remarkable result, is caused by ultraviolet rays or by aging. Elastin is a coil-shaped hard protein that is entangled with fibrous collagen, and has the property of returning to its original state after stretching like an elastic body, giving the skin firmness and elasticity in cooperation with collagen. Is what it is. Ultraviolet light activates the activity of elastase, a protease that specifically acts on this elastin, so that the skin exposed to a large amount of ultraviolet light promotes the decomposition of elastin, and as a result, the skin becomes firmer and more elastic. Leading to loss. (Fragrance Journal Vol. 25, No. 4) The effect of elastase is activated by aging, and the same result is brought about. Therefore, if the action of elastase can be inhibited, skin aging can be prevented.

[0005]

SUMMARY OF THE INVENTION An object of the present invention is to provide a plant extract having a high elastase activity inhibitory activity and suppressing elastin denaturation and destruction caused by elastase, and an anti-aging agent containing the same. It is in.

[0006]

Means for Solving the Problems In view of the above-mentioned problems, the present inventors evaluated elastase inhibitory activity of a variety of plant extracts, and as a result, the magnoliaceous plant Talauma mexicana (scientific name: Talauma mexicana) Was found to have a strong elastase activity inhibitory effect on the solvent extract.

That is, the present invention provides an elastase activity inhibitor containing an extract of Talauma mexicana (scientific name: Talauma mexicana) and an anti-aging agent such as cosmetics and quasi-drugs containing the same. To provide.

[0008]

Embodiments of the present invention will be described below in detail. Taraumaxicana used in the invention (scientific name: Tala
(uma mexicana) is a plant belonging to the magnoliaceae family distributed in southern East Asia, Southeast Asia and Central and South America. The extract of tarau mexicana used in the present invention is obtained by extracting from a part or the whole of a plant such as a leaf, stem, flower, rhizome or the like of the plant. Preferably, it may be obtained by extracting from one or both of the leaves and stems. Generally, after drying or after cutting a live plant as it is, it is used.

[0009] The extraction solvent used for the extraction is 2 to 20 times the extraction solvent per dry matter of the present plant or fresh plant.

As extraction solvents, water, lower monohydric alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.) and liquid polyhydric alcohols (1,3- Butylene glycol, propylene glycol, etc.), lower alkyl esters (ethyl acetate, etc.), hydrocarbons (benzene, hexane, pentane, etc.), ketones (acetone, methyl ethyl ketone, etc.), ethers (diethyl ether, tetrahydrofuran, dipropyl ether, acetonitrile, etc.) ). These solvents may be used alone or as a mixture of two or more. Preferably, one or more of water or a water-soluble solvent (eg, methanol, ethanol, propylene glycol, etc.) is used.

Although the extraction method is not particularly limited, the extraction is carried out at normal temperature or under heating. As the method, there are ordinary extraction, Soxhlet extraction and the like. The extraction time is not limited, but is preferably several hours to two weeks.

As described above, the extract according to the present invention is usually obtained as a liquid extract. The extract may be used as it is, or a processed product obtained by performing various treatments may be used. Such a processed product is also included in the extract according to the present invention. As such, for example, a concentrated liquid obtained by concentrating an extract under normal pressure or reduced pressure, a solid obtained by evaporating the solvent in the concentrated liquid to dryness, a solid obtained by crystallizing an active ingredient from the concentrated liquid, followed by filtration and drying. Objects and the like.

The amount of the tarau mexicanana extract in the present invention per dry matter is not particularly limited,
0.002 to 20.0% by weight, preferably 0.01 to 10.0% by weight, based on the total amount.

The extract of tarau mexicana according to the present invention has an excellent elastase activity inhibitory effect on human skin.
It can prevent skin aging and maintain a youthful and healthy skin condition. The anti-aging agent of the present invention can be widely used for cosmetics, quasi-drugs and the like, and particularly preferably can be widely used for cosmetics. The cosmetics to which the present invention is applied are not particularly limited, such as the dosage form. For example, lotions, emulsions, creams, foundations, packs, facial cleansers, shampoos, rinses, hair tonics and the like can be mentioned. In these cosmetics, various components usually used in cosmetics, that is, an aqueous component, an oily component, a powder component,
Alcohols, esters, surfactants, humectants, whitening agents, antioxidants, ultraviolet absorbers, thickeners, coloring agents, fragrances,
Components such as an antioxidant, a pH adjuster, a chelating agent and a preservative can be added.

[0015]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to Examples, but the present invention is not limited to these Examples. Prior to the examples, preparation examples of the plant extract of the present invention, test methods for elastase activity inhibition of the plant extract, and the results thereof will be described.

[Extraction Example 1] A 5-fold amount of 50% ethanol was added to 100 g of stem and leaves of Talauma mexicana (scientific name: Talauma mexicana ), and 146 was added at room temperature.
It was immersed and extracted for hours. After the treatment, the residue was filtered off, and the obtained extract was concentrated and freeze-dried to obtain 7.6 g of Tarauma mexicana extract. Dissolve this extract in DMSO 2%
This solution was appropriately diluted to adjust the concentration, and the following test was conducted.

[Test method for elastase activity inhibition and its results] The elastase activity inhibition measurement method used in the present invention was used in order to examine the elastase activity inhibition ability of the Tarauma mexicana extract obtained in [Extraction Example 1]. Is as follows. 0.1M as reaction buffer
This was performed using HEPES, 0.5 M NaCl (pH 7.4). MeOSuc-Ala-Ala-P as elastase substrate
ro-Val-pNA (L-1335 BACHEM) was dissolved in DMSO to a concentration of 80 mM, dispensed in 20 μl aliquots, and stored frozen (−80 ° C.). At the time of measurement, 8 mM with reaction buffer
It was used after dilution. Elastase was prepared using human-derived saliva (SE-563 Cosmo Bio Inc.).
Dissolve in the reaction buffer to a concentration of 10 μg / ml.
Each was dispensed and stored frozen (-80 ° C). At the time of measurement,
The solution was diluted to 5 μg / ml with a reaction buffer and used. 96-hole plate (Corning No.25860)
Then, 25 μl each of 8 mM elastase substrate was dispensed, and 50 μl of the inhibitor (sample appropriately diluted and adjusted in concentration) was added. Next, 25 μl of 5 μg / ml elastase was added on ice, and the mixture was immediately incubated at 37 ° C. for 20 minutes. Thereafter, the absorbance was measured at 415 nm. However, the inhibition rate was determined by the following formula.

[0018]

## EQU1 ## Inhibition rate (%) = 100− (presence of inhibitor / no inhibitor) × 100

The results are shown in FIG. Further, as a reference example, a test similar to that described above was performed for fetal calf serum (Moregate), which is an in vivo substance showing elastase activity inhibition, and compared. See FIG. In the following, examples of various formulations and formulations of the anti-aging agent according to the present invention are described.

[Example 1] Cream At the mixing amount described below, component A was heated and mixed at 70 ° C.
To keep. Next, the component B is heated and mixed and kept at 70 ° C. The component B was mixed with the component A so as to be uniform, and then the component C was injected and mixed, and then cooled to 30 ° C. with stirring to obtain a cream.

Ingredients Amount (wt%) (A) Squalane 10.0 Olive oil 10.0 Solid paraffin 5.0 Cetanol 4.0 Sorbitan monostearate 2.0 Polyoxyethylene sorbitan monostearate 2.0 (B ) Tarauma mexicana extract (Extraction Example 1) 0.05 (C) glycerin 5.0 methyl parapen 0.1 perfume qs purified water balance

[Comparative Example 1] Cream Except for removing the component (B) Tarauma mexicana extract in Example 1, the cream was prepared in the same manner as in Example 1 and used for an effect test.

Example 2 Emulsion Emulsion A component was heated and mixed at 70 ° C.
To keep. Next, the component B is heated and mixed and kept at 70 ° C. The component B was mixed with the component A so as to be uniform, then the component C was injected, mixed and stirred, and then cooled to 30 ° C. with stirring to obtain an emulsion. Ingredients Ingredients Amount (wt%) (A) 1,3-butylene glycol 5.0 Ethyl alcohol 5.0 Tarauma mexicana extract (Extraction Example 1) 5.0 Appropriate amount of purified water (B) Squalane 5.0 Vaseline 2 0.0 Beeswax 0.5 Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether (20E.O.) 1.2 Preservatives Appropriate perfume Appropriate amount (C) Carboxyvinyl polymer (1% aqueous solution) 20.0 Potassium hydroxide 0.1 Remaining purified water

[Comparative Example 2] Emulsion The emulsion was prepared in the same manner as in Example 2 except that the component (A) was not used.

[Test Example 1] Use effect test The following use tests were performed on the creams and emulsions prepared in Examples 1 and 2 and Comparative Examples 1 and 2, respectively. Table 1 shows the results. The use test was performed on 40 healthy adult women aged 28 to 55 years, which were randomly selected, as subjects, and applied each cosmetic to the skin after face washing for 4 weeks every day. The improvement effect on wrinkles and fine wrinkles after use and the effect on firmness and tarmi were examined. The condition of the skin was visually observed and evaluated based on the following evaluation criteria. (Evaluation criteria) A: Effective B: Somewhat effective C: No change D: Invalid

[0026]

[Table 1]

From the results shown in Table 1, when the cosmetic containing the extract of Tarauma mexicana prepared in Examples 1 and 2 was used, Comparative Examples 1, 2 and 2, in which the extract of Tarauma mexicana was not used. Wrinkles, wrinkles and skin tension
A good result was obtained, which was improved in terms of tarmi. From this result, it is recognized that blending the Tarauma mexicana extract as an active ingredient is a very useful formulation.

[0028]

As described above, by blending the Tarauma mexicana extract of the present invention having excellent elastase activity inhibition as an active ingredient, denaturation and destruction of elastic fiber elastin are suppressed, and elasticity is improved. There is provided an anti-aging agent having the effect of maintaining the skin without wrinkles and no wrinkles and preventing aging of the skin.

[Brief description of the drawings]

FIG. 1 is a diagram showing the inhibition of elastase activity of a Tarauma mexicana extract in comparison with fetal calf serum.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 43/00 111 A61P 43/00 111 F term (Reference) 4C083 AA082 AA111 AA112 AA122 AB032 AC012 AC022 AC072 AC102 AC122 AC442 AC482 AD092 CC05 DD31 EE12 4C088 AB65 AC05 BA08 NA14 ZA89 ZB21 ZC20 ZC21

Claims (3)

[Claims] [Claim 1] Talauma Mexicana (scientific name: Talauma
mexicana) An elastase activity inhibitor, which comprises a solvent extract of a plant. 2. A composition comprising the elastase activity inhibitor according to claim 1. 3. An anti-aging agent comprising the elastase activity inhibitor according to claim 1.