JPH04139132A - Anti-active oxygen action composition, anti-active oxygen agent, food, cosmetic and medicine containing the same as active ingredient - Google Patents

Abstract

PURPOSE:To obtain the subject readily usable and concentrated composition having extremely strong activity by roasting and fermenting plant seeds, preparing a composition therefrom, washing the resultant composition with a nonpolar solvent and then extracting the washed composition with a polar solvent. CONSTITUTION:Plant seeds and/or embryo buds are roasted and a microorganism is then added thereto and fermented while being sufficiently stirred to liberate and produce a large amount of a low-molecular anti-active oxygen substance. After completing the fermentation, the plant seeds are added to afford an anti-active oxygen action composition. The resultant composition is then washed with a nonpolar solvent such as benzene, n-hexane or ether to remove coloring matters, fat-soluble substances, etc., without any anti-active oxygen action in the aforementioned composition. Ingredients insoluble in the nonpolar solvent are subsequently extracted with a polar solvent (preferably acetone or a lower alcohol) and the extract solution is then concentrated to dryness according to a conventional method to provide an anti-active oxygen action composition in an amount of <=(1/10) based on the raw material composition. Since the weight is reduced while maintaining the activity, the composition can readily be administered as a medicine and added to cosmetics and foods.

Description

[Detailed Description of the Invention] [Field of Industrial Application] The present invention is useful for treating various diseases that impede health maintenance such as adult diseases, malignant rheumatoid arthritis, and intractable diseases such as Bartchet's disease, injuries such as burns, acne, and age spots. A composition having a novel anti-reactive oxygen effect that is effective in the prevention and treatment of cosmetic disorders, and
The present invention relates to anti-active oxygen agents, processed foods, health foods, functional foods, cosmetics, and pharmaceuticals containing this composition as an active ingredient.

[Conventional technology]

In recent years, arteriosclerosis, stroke, hypertension, myocardial infarction,
Adult diseases such as cancer and diabetes, incurable diseases such as malignant rheumatoid arthritis, Bartchett's disease, Coulomb's disease, ulcerative colitis, hepatitis, and nephritis, as well as diseases caused by chemicals (e.g., pesticides, etc.) are important for maintaining health. It has become an obstacle. In addition, external injuries such as burns, acne, cilantro, dermatitis, age spots, freckles, and the like pose cosmetic problems.

These various disorders do not necessarily develop from the same cause, but they are caused by excessive active oxygen and lipid peroxides (hereinafter referred to as active oxygen, etc.) in the human body due to external stimulation. ) is produced and is known to be involved in cell damage.

Conventionally, as a substance for suppressing these active oxygens, a composition is prepared by roasting plant seeds or germs, then adding microorganisms and fermenting them, and adding vegetable oil and plant seeds to this, as disclosed in JP-A-63-79834. It is disclosed in the publication number etc.

[Problem to be solved by the invention]

The active oxygen suppressing composition made from the above-mentioned plant seeds or germs and roasted and fermented has some degree of effectiveness, but since the daily oral dose is extremely large at 9 to 15 g, it cannot be administered parenterally. Of course, it is difficult to actually apply it as a form for oral pressure. In addition, even in the case of administration forms other than oral preparations, such as external preparations, cosmetics, injections, etc., the active ingredient composition contains many components other than the active oxygen component, making it difficult to formulate and utilize them. Furthermore, in order to make it easier to ingest, it was not appropriate to use it as an ingredient in small processed foods such as rice crackers, kutuki, and candy.

The present invention relates to an anti-slip oxygen effect composition obtained by extracting the anti-slip oxygen component from the above-mentioned active oxygen suppressing composition with higher purity, and foods, cosmetics, pharmaceuticals, quasi-drugs, etc. containing the composition. The purpose is to provide the following.

[Means for Solving the Problems 1] As a result of intensive research to solve the above problems, the present inventors found that an active oxygen suppressing composition (raw material) prepared by roasting and fermenting plant seeds and/or embryos. It was discovered that anti-reactive oxygen substances dissolve well in polar solvents and are insoluble in non-polar solvents.Furthermore, it was found that pigments and fat-soluble substances, which are inert substances that inhibit active oxygen in raw materials, are dissolved in non-polar solvents. It was also found that it was removed. By combining these solvents, it was possible to obtain a composition having an anti-active oxygen effect that has an activity greater than the total activity of the raw materials and is concentrated to a weight of 1710 or less, thereby completing the present invention.

In the present invention, after roasting plant seeds and/or embryos, the plant seeds are added to the enzymatically treated composition, the resulting composition is washed with a non-polar solvent, and then the insoluble matter is extracted with a polar solvent. These include compositions with a large active oxygen effect, and anti-active oxygen agents, foods, cosmetics, pharmaceuticals, and quasi-drugs containing the same compositions.

The active oxygen suppressing composition used in the present invention is prepared by roasting and fermenting plant seeds and germs, such as rice, wheat, barley,
Plant seeds such as soybeans, corn, pearl barley, adzuki beans, and peas and/or germs of the above plant seeds such as rice bran and wheat germ are fermented with koji mold, yeast, etc. to produce large amounts of low-molecular anti-active oxygen substances. It is produced freely and has enhanced anti-reactive oxygen activity. Matcha and sesame are added to this composition, as well as plant seeds such as sesame, soybean, cottonseed, corn, safflower, evening primrose, rice bran, rapeseed, and olive.

The above composition of the present invention can be obtained, for example, by the following method.

The main ingredients consisting of pearl barley, soybean, wheat germ and rice bran and/or brown rice germ in a total amount of 60 to 80% by weight based on the total weight are steamed at 50 to 150 ° C or 50 to 150 ° C.
Roast at ℃ or roast with far infrared rays, then steam, then add microorganisms and ferment while stirring well. After fermentation, 30~20% by weight of fine sesame powder and 10~O
% by weight of green leaf matcha (matcha) is added to produce an active oxygen suppressing composition.

It is preferable that each of the pearl barley, soybean, wheat germ, rice bran and/or brown rice germ be 7.5 to 27.5% by weight.

Although the chemical structure of the anti-active oxygen substance contained in the active oxygen suppressing composition is unknown, it is thought to be a substance with a relatively small molecular weight. Therefore, we thought that extraction with a solvent was possible, and when we extracted with various solvents and measured their anti-active oxygen activity, we found that ethanol>acetone>methyl isobutyl ketone>ethyl acetate>ether>n-hexane>benzene. As described above, anti-active oxygen substances are substances that are relatively well soluble in polar solvents.

Therefore, in the present invention, by washing with a non-polar solvent, pigments, fat-soluble substances, etc. that do not have anti-active oxygen effects in the raw material composition are removed without losing the anti-active oxygen substances. Next, when the non-polar solvent-insoluble components of the raw material composition thus obtained are extracted with a polar solvent, the anti-active oxygen substance is extracted and the weight becomes less than 1/1O of the raw material composition.

In the above-mentioned washing step, benzene, n-hexane, ether, etc. are suitable as non-polar solvents to be used, and this washing operation can be carried out repeatedly at room temperature or by Soxhlet extraction method.

As the polar solvent used in the above extraction step, water, water-soluble solvents such as lower alcohols, acetone, alkyl ketones, acetic esters, and especially acetone and lower alcohols are preferable. Two or more of these polar solvents may be used in combination. Although the extraction operation can be carried out at room temperature, it is preferable to carry out the extraction operation at a temperature of about 60 to 120°C.

The extract containing the anti-active oxygen substance obtained as described above is concentrated to dryness under reduced pressure in a conventional manner.

If necessary, the anti-reactive oxygen composition of the present invention can be obtained by freeze-drying. Note that since the active ingredient is somewhat unstable on an alkaline side, the extraction and purification steps are preferably carried out on a neutral or acidic side.

The composition of the present invention obtained as described above varies depending on its degree of purification, but it is a yellow to brown candy-like or solid substance, and is somewhat unstable on the alkaline side. It also suppresses active oxygen (superoxide, hydroxyl radical, hydrogen peroxide, etc.), DPPH (1,1-
It has a radical scavenging effect using the diphenyl-2-picrylhydratyl method, an inhibitory effect on lipid peroxide production, an antiventricular arrhythmia preventive effect in rats, and an anti-inflammatory effect.

All of these effects indicate that the drug has the ability to suppress damage caused by active oxygen and lipid peroxides generated in vivo.

Therefore, the composition of the present invention is an effective substance for the prevention and treatment of the aforementioned health disorders and cosmetic disorders.

The anti-reactive oxygen composition containing the above-mentioned anti-reactive oxygen agent of the present invention is a general carrier, auxiliary agent, additive, etc. used in the fields of oral and parenteral pharmaceuticals, quasi-drugs, cosmetics, etc. Then, it is formulated into pharmaceuticals, cosmetics, and various other products according to conventional methods.

Oral preparations include tablets, capsules, granules, fine granules,
Parenteral preparations such as syrups include external preparations such as ointments, creams, and solutions, and injections such as sterile solutions and suspensions.

20m when administering these products as medicines for diseases.
g~500mg once or several times a day, i.e. 20mg~lo
It can be administered at a total daily dose of oomg to achieve its full effect.

When the anti-active oxygen composition of the present invention is added to food, it may be in the form of the above-mentioned preparation, but it can be added to the respective food raw materials in the form of candy, rice crackers, kutuki, etc. in the required amount, and then added to the food using the general manufacturing method. Processed and manufactured by. Since ingestion as a health food or functional food is used for disease prevention and health maintenance, it is orally ingested several times a day as a processed product containing a total daily dose of 50 mg to 500 mg.

Further, the composition of the present invention can be used in combination with some compounds having antioxidant properties, such as vitamin C, vitamin E, and coenzyme Qn. These substances also act as stabilizers for the present composition, and are useful in combination. These antioxidants are used in less than conventional doses.

The anti-reactive oxygen compositions of the present invention are incorporated into the required unit dosage form with pharmaceutically acceptable physiologically acceptable vehicles, carriers, excipients, binders, preservatives, stabilizers, flavoring agents, and the like. Generally, 20 to 500 mg of anti-active oxygen composition
Contain.

Adjuvants mixed into tablets, capsules, etc. are as follows. tragacanth, gum arabic, cornstarch,
Binders such as gelatin, excipients such as microcellulose, cornstarch, pre-gelatinized starch, leavening agents such as alginic acid, lubricants such as magnesium stearate, sucrose, lactose, saccharin. Sweetening agents, flavoring agents such as peppermint, red radish oil, and cherry, and in the case of capsules, the above materials can also contain a liquid carrier such as a fatty oil. Other materials can also be present as coatings or to otherwise modify the physical form of the formulation. For example, tablets may be coated with shellac or sugar. A syrup or elixir may contain, in addition to the active composition of the invention, sucrose as a sweetening agent.
Methyl or propyl parabens as preservatives, dyes and flavoring agents such as cherry or orange flavor may be included.

Sterile compositions for injection include the active composition of the invention in a vehicle such as water for injection, sesame oil, coconut oil, peanut oil,
They can be formulated by conventional methods of dissolving or suspending naturally occurring vegetable oils such as cottonseed oil or the like or synthetic fatty vehicles such as ethyl oleate and the like. In addition, buffering agents,
Preservatives, antioxidants, etc. can be added as necessary.

For external preparations, petrolatum, paraffin, oils and fats, lanolin, macrogol, etc. are used as bases, and ointments, creams, etc. are prepared by conventional methods.

Next, Examples of the composition of the present invention and test examples showing the effects of the composition of the present invention will be given. This example shows a particularly preferred embodiment for the purpose of explaining the present invention in detail, and the present invention is not limited thereto.

〔Example〕

Reference example: Manufacture of raw materials of the present invention Soybean, pearl barley, wheat germ, rice bran, and brown rice germ are each roasted at 95 to 98°C for about 60 minutes, mixed with 1.0 part by weight of each, and then softened with steam. Steam until Add an appropriate amount of commercially available koji to this, stir well from time to time, and ferment for about 2 to 3 days. This is air-dried and then ground into a fine powder. To this, 1.5 parts of roasted black sesame seeds and 0.5 parts of matcha are added and mixed to obtain raw rice of the present invention.

Example 1 20g of raw rice obtained in the reference example was mixed with n-hexane 100-
After stirring at room temperature for 1 hour and allowing it to stand, the supernatant was removed as much as possible by decantation, and the solids were washed twice in the same manner, filtered, and air-dried to reduce the solid content to 15. Obtain 5 g. 15.5 g of the solid thus obtained is suspended in 50 nd of ethanol and boiled in a water bath (88-90°C) for 30 minutes with stirring. After cooling, filter and add about 30ml of ethanol to the filtered solid.
1, and the obtained solid is further added with 50 ml of ethanol, heated and extracted in the same manner as above, allowed to cool, and then filtered. The ethanol portions were combined and evaporated to dryness under reduced pressure to obtain 1.4 g of a brown semi-solid anti-active oxygen composition.

Example 2 When 15-ethanol was added to 1.3 g of the anti-active oxygen substance obtained in Example 1 and stirred thoroughly, a grayish brown solid was precipitated.
After separating this by filtration, adding 150 mg of activated carbon to the ethanol solution and stirring well, the activated carbon was separated by filtration, and the ethanol solution was concentrated under reduced pressure to obtain 0.9 g of a yellow-brown semi-solid candy-like anti-active oxygen composition. obtain.

Example 3 5 g of the anti-active oxygen composition obtained in Example 1 was added to 5 g of water (
ld to form an emulsion, which is washed five times with benzene 8072 each. The aqueous layer was extracted three times with 70 parts of ethyl acetate, the aqueous layer was saturated with common salt, and further extracted twice with 7 parts of ethyl acetate. The ethyl acetate extracts are combined, dried over anhydrous sodium sulfate, and concentrated to dryness to obtain 1.35 g of an anti-active oxygen composition as a yellowish brown powder.

Example 4 In the same manner as in Example 1, using a mixture of water and acetone (1:4) instead of ethanol, 3.1 g of an anti-active oxygen composition in the form of a brown semi-solid is obtained.

Example 5 5 g of raw rice obtained in Reference Example was washed with n-hexane using a Soxhlet extractor, 100 g of water was added to 3.8 g of solid, and the mixture was heated and extracted at 100° C. for 30 minutes. Same operation 2
The aqueous portion was collected and concentrated under reduced pressure, and then freeze-dried to obtain 0.4 g of the anti-slip oxygenated composition of the present invention in the form of a yellowish brown semi-solid.
get.

Example 6 5 g of the raw rice obtained in Reference Example was suspended in 25 g of n-hexane, stirred at room temperature for 1 hour, then left to stand, the supernatant was removed as much as possible by decanting, and the suspension was further dissolved in the same manner. It was washed twice and the solid matter was collected by filtration. This solid material is washed three times with 25 parts of benzene and in the same manner as that performed with n-hexane, and the solid material is filtered and dried. This solid substance is suspended in ethyl acetate and extracted by boiling in a water bath (88-90°C) for 30 minutes while stirring. After cooling, it is filtered and washed with 15 d of ethyl acetate. Furthermore, the obtained solid was subjected to thermal extraction twice with ethyl acetate in the same manner as above. The ethyl acetate extracts obtained in the above procedure were combined, washed with water, dried over anhydrous sodium sulfate, and evaporated to dryness under reduced pressure to obtain 0.13 g of an anti-slip composition in the form of a yellowish brown powder.

Example 7 The same procedure as in Example 6 was repeated using methyl isobutyl ketone in place of ethyl acetate to obtain 0.14 mm of an anti-slip oxygen-active composition in the form of a yellowish brown powder.

Example 8 Capsule, tablet anti-slip oxygen composition 15 milk
70 parts by weight of sugar and 15 parts by weight of magnesium stearate are mixed uniformly to form capsules or tablets.

Example 9 Powder, granule anti-slip oxygen composition 30 lees
Mix 30 parts by weight of powder and 40 parts by weight of lactose to make a powder or granules.

Example IO Injectable anti-slip oxygen composition 2 Surfactant 8 Physiological saline 90 Parts by weight are heated and mixed and sterilized to prepare an injection.

Example 11 Containing 2% weight of Kutsky anti-active oxygen composition/JX wheat flour seasoned with salt, sucrose, butter, etc., stirred well with an appropriate amount of water and baked at 190-200°C for 30 minutes to make Kutsky. do.

Example 12 13g of jelly agar was heated and dissolved in water at 1°C, and 500g of sucrose was added.
g, 150 g of starch syrup and a little salt were added, heated and dissolved with stirring, and then 2% by weight of anti-slip oxygen composition, fruit juice,
Add colorants, flavors, etc. and cool to make jelly.

Example 13 Add 10 parts by weight of water to 20 parts by weight of sucrose and 10 parts by weight of starch syrup (75% solids), mix, heat to 150°C and stir,
Add 2% by weight of the anti-slip oxygen composition, coloring agent, flavoring agent, etc., and cool to make a candy.

Example 14 15 parts by weight of hand lotion Carbowax 1500, 8 parts by weight of alcohol, and 90 parts by weight of propylene glycol were thoroughly mixed and dissolved, and 52.5 parts by weight of water, 2 parts by weight of anti-slip oxygen composition, fragrance, and preservative were added. Add an appropriate amount of the agent to make a hand lotion.

Example 15 External preparation (Formulation example 1) Ethyl paraoxybenzoate 0.1 Butyl paraoxybenzoate 0.1 Lauromacrogol 0.5 Cetanol
I8 White petrolatum 40 Water 36.3 Anti-active oxygen composition 6 The anti-slip oxygen composition is dissolved in water using 6 parts by weight of each component and made into an ointment according to a conventional method.

Example 16 External preparation (Formulation example 2) Polyethylene glycol 40 Stearate 3.1 Glyceryl stearate 7.7 Behenyl alcohol 8.5 Squalene 12.3 Glycerin trioctanoate 12.3 Propyl paraben 0.1 Methyl paraben 0.1 perilla EDT
A O,3 dipropylene glycol 7.7 Citric acid 0.2 Sodium citrate 1.4 Antiactive oxygen composition 6.0 Water
The anti-active oxygen composition is dissolved in water using 40.3 parts by weight of each component and made into an ointment according to a conventional method.

Next, a test example of the radical scavenging effect of the composition of the present invention will be shown.

Test example Radical scavenger action 1) Test method M, S, Blois: Nature 4617,1
+99 (1958) (antioxidant effect) and Hisano et al.: Takeda Research Institute Bulletin 44.30 (1985).

2) Test substance a) Composition of the present invention obtained in Example 1) α-tocopherol (control) 3) Results As is clear from the above results, the composition of the present invention has a radical scavenging action. The strength of its activity was close to that of α-tocopherol.

[Effects of the Invention] The present invention is a novel composition that has an extremely strong anti-active oxygen effect. In recent years, anti-active oxygen agents and pharmaceuticals containing this composition have been used to treat adult diseases such as arteriosclerosis, stroke, hypertension, myocardial infarction, cancer, and glycosylosis, as well as malignant rheumatoid arthritis, Bartchet's disease, Coulomb's disease, ulcerative colitis,
Prevention and treatment of intractable diseases such as hepatitis and nephritis, health maintenance disorders such as diseases caused by chemical substances (e.g. pesticides, etc.), injuries such as burns, and cosmetic disorders such as acne, cilantro, dermatitis, age spots, and freckles. Furthermore, the food containing the present composition is an extremely useful invention that is effective in preventing and treating the various diseases mentioned above.

Claims (1)

[Claims] 1. After roasting plant seeds and/or embryos, the plant seeds are added to the enzyme-treated mixture, the resulting composition is washed with a non-polar solvent, and then the insoluble matter is removed with a polar solvent. An anti-reactive oxygen composition characterized in that it is obtained by extraction. 2. An anti-active oxygen agent containing the composition according to claim 1. 3. A food product containing the composition according to claim 1. 4. A cosmetic comprising the composition according to claim 1. 5. A pharmaceutical product comprising the composition according to claim 1.