JP3068551B2 - Slimming agent - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a slimming agent containing a safe and safe scallop extract as an active ingredient, preferably a slimming agent prepared in the form of a cosmetic.

[0002]

2. Description of the Related Art In recent years, Japanese meals have become remarkably westernized,
High calorie is progressing. In particular, excessive lipid intake causes obesity, which is also called modern civilization disease. Obesity is one of social problems because it is closely related to various diseases such as hyperlipidemia, arteriosclerosis, and diabetes. In addition, the desire to reduce the aesthetics of Japanese people in recent years has become extremely strong.

However, to date, none of the cosmetics marketed for slimming has been found to be extremely effective. On the other hand, in the literature, for example, epinephrine, an example using an adrenergic β-stimulant such as isoproterenol or theophylline (US Pat. No. 4,525,359) is described, but these have problems in safety. .

[0004]

SUMMARY OF THE INVENTION An object of the present invention is to provide a highly safe slimming agent which exerts a slimming effect by promoting the decomposition of fat in fat cells.

[0005]

Means for Solving the Problems In order to solve the above problems, the present inventors screened various plant extracts. This screen was performed for mouse 3T3-L1 that induced differentiation of preadipocytes into adipocytes.
The measurement was performed using the effect of promoting the decomposition of fat in fat cells as an index.
Furthermore, screening was performed using the effect of promoting the degradation of fat in free adipocytes obtained by using a collagenase solution from epididymal adipose tissue and subcutaneous adipose tissue of rats as an index.
As a result, it has been found that the Japanese sagebrush extract has the desired effect, and the present invention has been completed.

[0006] That is, the present invention provides a slimming agent containing a Japanese sagebrush extract as an active ingredient. In a preferred embodiment of the present invention, the slimming agent is prepared in the form of a cosmetic.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION Artemisia capilla
ris Thumb.) is a perennial plant of the Asteraceae family mainly produced in China, and the extract of its seedlings is known to have a bile effect, an antihypertensive effect, or a diuretic effect. It is also known to have an inhibitory action on the metabolism of arachidonic acid, which is thought to play an important role in allergic and / or inflammatory diseases (JP-A-8-1760).
03). However, it has not been known until now that mugwort or its extract has a slimming effect.

The sagebrush used in the present invention may be whole grass, or any of its leaves, root bark, stem, root, branch, fruit, seed or flower, or a mixture of two or more of these plant parts. . These plant raw materials may be raw or dried. Preferably, these plant raw materials are pulverized and then used for extraction. The termite extract used in the present invention means an extract obtained by solvent extraction of the above-mentioned plant material at room temperature or under heating, a diluent or a concentrate thereof, or a dried product thereof. It is preferable to use an extract obtained by extracting a dried product of the spikelets of Artemisia serrata.

As the solvent used for the extraction, water or one or more kinds of organic solvents such as lower alcohols (such as methyl alcohol, ethyl alcohol or butanol), acetone and ethyl acetate are appropriately mixed and used. it can. Preferred extraction solvents are water or lower alcohols alone or a mixture of water and lower alcohols. Particularly preferred extraction solvents are lower alcohols alone.

[0010] The extraction may be performed in a usual manner. The extraction temperature is usually in the range of 5 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 1 to 96 hours for extraction at 40 ° C. or higher.

The extract thus obtained can be used as it is for the slimming agent of the present invention. Alternatively, the extract may be concentrated or diluted with an appropriate solvent (eg, water or lower alcohol) before use. it can. Further, the extract can be evaporated to dryness and used as the slimming agent of the present invention.
Preferably, the extract is concentrated, water is added to the concentrate to remove precipitated insolubles, and the obtained filtrate is concentrated or diluted with a suitable solvent and used for the slimming agent of the present invention.

The slimming agent of the present invention is prepared in a form for external use, that is, in the form of a cosmetic, a quasi-drug, or a pharmaceutical. The slimming agent of the present invention is particularly preferably prepared and used in the form of a cosmetic. Examples of the form of the cosmetic include a gel cream, a face wash cream, a lotion, an emulsion and the like.

The mixing ratio of the Japanese sagebrush extract in the slimming agent of the present invention varies depending on the concentration of the sagebrush extract and the form of the slimming agent.
The range is from 0001 to 99% by weight, preferably from 0.001 to 10% by weight, more preferably from 0.001 to 5% by weight, and still more preferably from 0.01 to 2% by weight.

[0014] The slimming agent of the present invention contains, in addition to the active ingredient, the mugwort extract, various components generally used in preparing various slimming agents according to their forms. Other components commonly used in preparing cosmetics are, for example, oils, surfactants, humectants, thickeners, preservatives, fragrances, coloring agents, drugs and the like.

[0015]

EXAMPLES The present invention will be described in more detail below with reference to Examples relating to the production of an extract of pearl mugwort used for the slimming agent of the present invention, the measurement of the lipolytic effect, and the production of various cosmetics. It is not limited to the embodiment.

Example 1 Preparation of a Japanese Artemisia extract (1) To 50 g of Japanese Artemisia (flower spike), 400 mL of ethanol was added, and the mixture was heated and refluxed at 95 ° C. or more for 2 hours. This mixture is
After allowing to cool to 0 ° C., the mixture was filtered to obtain 340 mL of an extract. The extract was concentrated under reduced pressure while heating at 60 ° C. and dried to dryness. 250 mL of water was added, and the mixture was allowed to stand at 4 ° C. for 48 hours. The generated insoluble precipitate was removed by filtration to obtain 248 mL of a sagebrush extract. The solid content contained in the extract thus obtained was 0.5 (w / v)%.

Example 2 Preparation of Japanese Artemisia extract (2) To 100 g of Japanese Artemisia (flower spike) was added 800 mL of ethanol, extracted at 40 ° C. for 2 days, filtered, and filtered to obtain 700 ml of filtrate.
mL was obtained. This filtrate was concentrated under reduced pressure at 60 ° C. or lower to 80 mL. Next, 80 mL of distilled water was added to the concentrated solution, and the solution was allowed to stand at 10 ° C. or lower for 2 days, and the precipitated insoluble material was removed by filtration. Furthermore, 50 (v / v)% was added to 150 mL of the obtained filtrate.
Ethanol was added to make the total volume 500 mL, and this was used as a mugwort extract.

Example 3 Measurement of lipolytic activity on mouse 3T3-L1 adipocytes (1) Induction of differentiation from preadipocytes to adipocytes Using 3T3-L1 cells, which are often used as a model of adipocytes, lipolysis Activity was measured. Since these cells correspond to preadipocytes, a treatment for inducing differentiation into adipocytes was first performed according to a conventional method. That is, 10 wells in a 6 well plate
2x cells in D-MEM medium containing 5% fetal calf serum (FCS)
10 ⁴ cells were inoculated, and 5 days later, the medium was diluted with 10% FCS containing 0.25 μM dexamethasone, 0.5 mM isobutylmethylxanthine and 10 μg / ml insulin.
-Change to MEM medium. After culturing for another 2 days, the medium is returned to the usual D-MEM medium containing 10% FCS. If the culture is further continued for one week, the preadipocytes differentiate into adipocytes. These cells were used for measuring the lipolytic effect.

(2) Measurement of lipolytic activity When fat in fat cells is decomposed, glycerol and free fatty acids are released. Lipolytic activity was measured by quantifying the amount of glycerol released in the medium. Glycerol was quantified by the enzymatic method. To the adipocytes prepared in the above (1), the sprouts extract prepared in Example 1 were added at final concentrations of 1%, 3% and 5%, respectively, and the medium was recovered after 24 hours. The lipolytic activity was compared with that of the control plant to which no extract was added. These results are shown graphically in FIG. As is clear from this graph, the release of glycerol from adipocytes was higher when 1, 3 and 5% of the pearl mugwort extract was added, respectively, than in the case where no extract was added.
It was found that 11.0%, 11.2% and 59.0% were promoted. That is, it was revealed that the Japanese sagebrush extract promoted lipolysis and had a slimming effect.

Example 4 Measurement of lipolytic activity on rat epididymal fat cells The lipolytic activity was measured by quantifying the amount of free fatty acids released into the medium by the decomposition of fat in fat cells. Quantification of free fatty acids was performed by an enzymatic method. Rod bell [R
odbell, M, J. Biol. Chem. 239, 375 (1964)], free fat cells were prepared from epididymal adipose tissue of four male Wistar 8 week-old rats using a collagenase solution. Krebs Ringer (Krebs R) containing bovine serum albumin prepared so that the concentration of the sprouts extract prepared in Example 2 becomes 0.5 (v / v)% and 1.0 (v / v)%.
inger) In a bicarbonate buffer, the above adipocytes were incubated at 37 ° C. for 90 minutes, and the released fatty acids were measured using a commercially available kit (Wako Pure Chemical Industries, NEFA C-Test Wako). The lipolytic activity was compared with that of the control plant to which no extract was added. These results are shown in FIG. As is clear from FIG. 2, when the concentration of the Japanese sagebrush extract was 0.5 (v / v)% and 1.0 (v / v)%, the release of fatty acids from adipocytes was less than in the case of no addition. 61.2% and 157.8%, respectively.

Example 5 Measurement of Lipolytic Activity on Rat Subcutaneous Adipocytes Free adipocytes were prepared from a subcutaneous adipose tissue of four Wistar 10-week-old male rats using a collagenase solution. Krebs-Ringer bicarbonate buffer containing bovine serum albumin prepared so that the concentration of the sprouts extract prepared in Example 2 becomes 0.5 (v / v)% and 1.0 (v / v)%. In the above, the above adipocytes were incubated at 37 ° C. for 90 minutes, and the released fatty acids were replaced with a commercially available kit (NEFA).
C-Test Wako). The lipolytic activity was compared with that of the control plant to which no extract was added. These results are shown in FIG. As is clear from FIG. 3, when the concentration of the Japanese sagebrush extract was 0.5 (v / v)% and 1.0 (v / v)%, the release of fatty acids from adipocytes was less than in the case of no addition. , 33.5% and 38.7, respectively
% Promoted.

[0022] As described above, it was revealed that the Japanese mugwort extract promotes the release of glycerol or fatty acids from adipocytes. In other words, it was revealed that the Japanese sagebrush extract increased lipolytic activity.

Example 6 Gel Cream A mugwort extract (prepared in Example 2) is used as an active ingredient in the following gel cream formulation (total 100% by weight).

TABLE 1 Ingredients % by weight Mulberry extract 1.0 carboxyvinyl polymer 0.55 1,3-butylene glycol 4.0 concentrated glycerin 4.0 squalane 2.0 olive oil 1.0 adsorbed purified lanolin 2.0 self-emulsification Type monostearic acid polyoxyethylene sorbitan 0.1 Monostearic acid polyoxyethylene sorbitan 0.2 Natural vitamin E 0.15 Alanin 0.1 Paraoxybenzoate 0.2 Potassium hydroxide Appropriate amount of purified water All remaining components at room temperature Stir and mix to a uniform solution,
The pH was adjusted to 6.5 to obtain a gel cream.

COMPARATIVE EXAMPLE 1 Conventional Gel Cream The same procedure as in Example 6 except that the extract from the mugwort was replaced with purified water was prepared as a conventional gel cream.

Example 7 Facial cleansing cream The extract of Kawataya mugwort (prepared in Example 1) is used as an active ingredient in the following facial cleansing cream formulation (100% by weight in total).

TABLE 2 Ingredient A wt% myristine 14.0 stearic acid 12.0 lauric acid 3.5 oleyl alcohol 1.5 coconut oil fatty acid amidopropyl betaine 10.5 component B wt% concentrated glycerin 18.0 potassium hydroxide 7. 0 preservative (p-hydroxybenzoic acid esters) qs purified water balance component C wt% Artemisia capillaris extract 0.5 perfume 0.2 component a was heated and dissolved, kept at 80 ° C.. Separately, the component B heated and dissolved at 80 ° C. is added to the component A and mixed well. The mixture was cooled while stirring, and the component C was added at 50 ° C. to obtain a face wash cream.

Example 8 Lotion A skin mugwort extract (prepared in Example 1) is used as an active ingredient in the following lotion formulation (total 100% by weight).

TABLE 3 Ingredients % by weight concentrated glycerin 4.0 Sorbit solution (70% by weight aqueous solution) 4.0 Sodium citrate 0.3 Polyoxyethylene hydrogenated castor oil 0.5 Ethanol 15.0 Kawagomugi extract 1.0 Fragrance 0.05 Citric acid (pH adjuster) Appropriate amount of purified water All remaining components are stirred and mixed at room temperature to form a uniform solution.
The pH was adjusted to 5.5 to obtain a lotion.

Example 9 Emulsion A mugwort extract (prepared in Example 1) is used as an active ingredient in the following emulsion formulation (total 100% by weight).

Component A weight% sucrose fatty acid ester (Daiichi Kogyo Seiyaku S-160) 1.0 concentrated glycerin 6.0 carboxyvinyl polymer 0.06 potassium hydroxide 0.028 preservative (paraoxybenzoate) Purified water Remaining component B wt% olive oil 4.0 Jojoba oil 4.0 Lactic acid 2.0 Self-emulsifying glyceryl monostearate 1.5 Lipophilic glyceryl monostearate 1.5 Component C wt% Flavor 0.2 Component A is dissolved by heating and kept at 80 ° C. Separately, the component B heated and dissolved at 80 ° C. is added to the component A and mixed well. The mixture was cooled while stirring, and the component C was added at 50 ° C. to obtain an emulsion.

Example 10 Use of the gel cream of Example 6 and the gel cream of Comparative Example 1 for 20 women 20 to 50 years old for 4 months (external application, 1 Day 1
After bathing twice). After use, fixed points were measured around the hips and waist and compared with those before the start of the test. The results are shown in Tables 5 and 6 below.

[Table 5] Gel cream of the present invention (Example 6) 2-4 cm reduced 4-6 cm reduced 6 cm or more No change Increased hip 9 people 5 people 5 people 0 waist 5 people 8 people 2 people 5 people 0 Name

[Table 6] Gel cream of Comparative Example 1 2-4 cm reduced 4-6 cm reduced 6 cm or more no change increased hip 0 0 0 15 15 5 waist 1 0 0 17 2 These tables As is clear from the above, the gel-like cream containing the Japanese sagebrush extract showed an excellent slimming effect.

Example 11 As a result of applying the cosmetics such as the face-washing cream, lotion and milky lotion of the above-mentioned Examples 7 to 9 prepared by blending the scallop extract as an active substance having a slimming effect to humans, The tightness to the skin was extremely good.

From the above results, it was revealed that the Japanese sagebrush extract exhibited excellent lipolytic activity, and that the slimming agent containing the Japanese sagebrush extract exhibited an excellent slimming effect.

[Brief description of the drawings]

FIG. 1 is a graph showing the lipolytic effect of a mugwort extract on mouse 3T3-L1 adipocytes.

FIG. 2 is a graph showing the lipolytic effect of a mugwort extract on rat epididymal fat cells.

FIG. 3 is a graph showing the lipolytic effect of a mugwort extract on rat subcutaneous fat cells.

 ──────────────────────────────────────────────────続 き Continuation of the front page (72) Inventor Toshiji Miyazaki 2-2-2 Muroya, Nishi-ku, Kobe City, Hyogo Prefecture Inside the Research and Development Center of Nagase & Co., Ltd. (56) References JP-A-61-40763 (JP, A JP-A-8-301780 (JP, A) JP-A-8-245410 (JP, A) JP-A-8-81382 (JP, A) JP-A-4-253917 (JP, A) Chem. Phem, Bull. , (1985), 33 (5), p2028-2034

Claims (2)

(57) [Claims] 1. A topical slimming agent comprising an extract of A. mugwort as an active ingredient. 2. The slimming agent according to claim 1, which is prepared in the form of a cosmetic.