JP2002255734A - Elastase activity inhibitor and anti-aging agent comprising the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an anti-aging agent capable of preventing the skin from aging by restoring/maintaining the firmness or resilience of the skin through inhibiting the activity of elastase acting to denature and degrade elastin as one of substances giving the skin firmness or resilience. SOLUTION: The anti-aging agent is obtained by formulating a solvent extract of Bursera lancifolia plant. Because the extract has excellent elastase activity inhibitory effect, this anti-aging agent can prevent the skin from aging by restoring/maintaining the firmness or resilience 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 that 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 the cause of skin aging that progresses in parallel, aging is generally the most important, but dryness, oxidation, sunlight and the like can also be mentioned as direct factors related to skin aging.

[0003] 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.

[0004]

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.

[0005]

Means for Solving the Problems In view of the above-mentioned problems, the present inventors evaluated the elastase inhibitory activity of a variety of plant extracts, and found that plants belonging to the genus Burseraceae belonging to the genus Burseraceae native to Mexico The Brucella
It has been found that a solvent extract of ransifolia (scientific name: Bursera lancifolia) has a strong elastase activity inhibitory effect.

[0006] That is, the present invention provides an elastase activity inhibitor characterized by containing an extract of Brusera lancifolia (scientific name: Bursera lancifolia) and an anti-aging agent such as cosmetics and quasi-drugs containing the same. Is what you do.

[0007]

Embodiments of the present invention will be described below in detail. Brucella ransifolia used in the invention (scientific name:
Bursera lancifolia) belongs to the family Orchidaceae, which is widely distributed in the tropics and usually grows from arid forests to moist forests up to an altitude of 1500 m, and is particularly widely distributed in Mexico. The Brucella ransifolia extract 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.

[0008] The extraction solvent used in the extraction is 2 to 20 times the extraction solvent per dry matter of the present plant or fresh plant.

As the extraction solvent, 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.

The extraction method is not particularly limited, but 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 blending amount of the Brucella ransifolia extract in the present invention in terms of dry matter is not particularly limited, but is 0.002 to 20.0% by weight, preferably 0.01 to 10.0% by weight based on the total amount. desirable.

[0013] The extract of Brucella ransifolia according to the present invention has an excellent elastase activity inhibitory effect on human skin. Therefore, an anti-aging agent containing this extract prevents skin aging and makes youthful. A healthy skin condition can be maintained. 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. These cosmetics include various components commonly used in cosmetics, that is, aqueous components, oily components, powder components, alcohols, esters, surfactants, humectants,
Components such as whitening agents, antioxidants, ultraviolet absorbers, thickeners, coloring agents, fragrances, antioxidants, pH adjusters, chelating agents, preservatives and the like can be added.

[0014]

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.

[0015] [Extraction Example 1] Brucella Ranshiforia (scientific name: Bursera lancifolia) portion 10 of the stems and leaves of
A 10-fold amount of 50% ethanol was added to 0 g, and the mixture was stirred and extracted at room temperature for 21 hours. After the treatment, the residue was filtered off, and the obtained extract was concentrated to dryness to obtain 12.2 g of Brucella lansifolia extract. This extract was dissolved in DMSO at 2%, and this solution was appropriately diluted to adjust the concentration, and the following test was conducted.

[Test method for elastase activity inhibition and its results] Brucella obtained in [Extraction Example 1] described above
The elastase activity inhibition measurement method used in the present invention for examining the elastase activity inhibition ability of the ransifolia extract is as follows. As a reaction buffer, 0.
This was performed using 1 M HEPES, 0.5 M NaCl (pH 7.4). MeOSuc-Ala-A as an elastase substrate
la-Pro-Val-pNA (L-1335 BACHEM) was dissolved in DMSO to 80 mM, dispensed in 20 μl aliquots, and stored frozen (−80 ° C.). At the time of measurement, use 8
It was used after diluting to mM. Elastase uses human-derived saliva (SE-563 Cosmo Bio Inc.)
And dissolved in a reaction buffer to give a concentration of 10 μg / ml.
The resulting solution was dispensed in aliquots and stored frozen (-80 ° C). At the time of measurement, the reaction buffer was diluted to 5 μg / ml before use. 96 hole plate (Corning No.2586
0), 25 μl each of 8 mM elastase substrate
Then, 50 μl of the inhibitor (sample diluted appropriately and adjusted in concentration) was added. Then, on ice, 5 μg / ml
Of elastase was added immediately at 37 ° C for 20 μl.
Incubated for minutes. Thereafter, the absorbance was measured at 415 nm. However, the inhibition rate was determined by the following formula.

[0017]

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

FIG. 1 shows the result. 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, the 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 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 ) Brucella ransifolia 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) Brucella ransifolia extract from Example 1, all creams were prepared in the same manner as in Example 1 and used for a use effect test.

Example 2 Emulsion Emulsion 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, then the component C was injected, mixed and stirred, and then cooled to 30 ° C. with stirring to obtain an emulsion.

Ingredients Ingredients (wt%) (A) 1,3-butylene glycol 5.0 ethyl alcohol 5.0 Brucella ransifolia extract (Extraction Example 1) 5.0 Appropriate amount of purified water (B) Squalane 5.0 Vaseline 2.0 Beeswax 0.5 Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether (20E.O.) 1.2 Preservative appropriate amount Perfume appropriate amount (C) Carboxyvinyl polymer (1% aqueous solution) 20.0 water Potassium oxide 0.1 Purified water Remaining

Comparative Example 2 Emulsion The emulsion was prepared in the same manner as in Example 2 except that the component (A) Brucella ransifolia extract was omitted, and used in the effect test.

[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 cosmetics containing the Brucella ransifolia extract prepared in Examples 1 and 2 were used, the results were higher than those of Comparative Examples 1 and 2 not containing the Brucella ransifolia extract. Good results were obtained in that wrinkles and wrinkles were improved, and the skin was improved in terms of firmness and skininess. From these results, it is recognized that blending the Brucella ransifolia extract as an active ingredient is a very useful formulation.

[0028]

As described above, by blending the brucella ransifolia extract of the present invention having excellent elastase activity inhibition as an active ingredient, denaturation and destruction of elastic fibers, elastin, are suppressed, and elasticity is improved. There is provided an anti-aging agent which has an effect of maintaining skin without wrinkles and lumps and preventing skin aging.

[Brief description of the drawings]

FIG. 1 shows the inhibition of elastase activity of Brucella ransifolia extract in comparison with fetal calf serum.

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Claims (3)

[Claims] [Claim 1] Brucella Rancifolia (scientific name: Burs
era lancifolia) An elastase activity inhibitor comprising 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.