JP2002053475A - Glucosidase inhibitor and food or beverage including the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an α-glucosidase inhibitor of high safety originating from a naturally occurring substance and provide foods and beverages including the same. SOLUTION: The objective glucosidase inhibitor characteristically includes flowers of herbaceous peony or the essence of the flower as an effective component.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a carbohydrate digestive enzyme inhibitor effective for preventing diabetes and obesity, and to a food or drink containing the same.

[0002]

2. Description of the Related Art Inhibition of carbohydrate-degrading enzymes such as α-glucosidase slows the decomposition of disaccharides into monosaccharides, and slows the absorption of monosaccharides from the intestinal tract, thereby suppressing blood sugar rise. Having. Therefore, it is useful for various diseases such as hyperglycemic symptoms and obesity, adiposity, hyperlipidemia, and diabetes caused by hyperglycemia. Research on α-glucosidase inhibitors has been conducted for a long time. Many pseudo-monosaccharide or pseudo-oligosaccharide substances isolated from actinomycetes have been reported. Examples are acarbose and voglibose (Progress
in Clinical Biochemistry
and Medicine, 77-99, 1988,
Journal of the Japanese Society of Agricultural Chemistry, 63, 217, 1989).

Recently, Japanese Patent Application Laid-Open No. 9-29663 discloses a substance obtained from an extract obtained from eel, and Japanese Patent Application Laid-Open No. 9-48736 discloses an extract of Milkia cephaerocarpe. JP-A-65836 discloses a hydrolyzate such as a vegetable protein.
No. 9472 discloses that all extracts of Salacia purinoides inhibit α-glucosidase.

On the other hand, Shakuyaku is a kind of crude drug, its analgesic effect is disclosed in JP-A-6-199676, its cancer metastasis inhibitory effect is disclosed in JP-A-7-258104, and its apoptosis inhibitory effect is disclosed in JP-A-9-87187. The gazette and the whitening effect are disclosed in JP-A-8-92056, respectively. However, a crude drug consisting of a peony is collected from the root bark of a peony, and it is not known at all that the peony flower or its extract has an inhibitory effect on carbohydrate digestive enzymes.

[0005]

SUMMARY OF THE INVENTION An object of the present invention is to provide an α-glucosidase inhibitor derived from natural products with high safety and a food or drink containing the same.

[0006]

In view of such circumstances,
The present inventors have conducted intensive studies to find new inhibitors that effectively inhibit carbohydrate digestive enzymes such as α-glucosidase and have no harmful effects on the human body. As a result, it has been found that an extract containing a peony flower or an extract thereof as an active ingredient is highly safe for living organisms, excellent in efficacy, and useful for preventing and improving obesity and diabetes, and completed the present invention. did.

That is, the first aspect of the present invention relates to a carbohydrate-degrading enzyme inhibitor comprising a peony flower or a peony flower extract as an active ingredient.

[0008] A second aspect of the present invention relates to a food or drink comprising the carbohydrate-degrading enzyme inhibitor according to claim 1 or 2.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION As a peony flower that can be used in the present invention, a peony of the family Peonaceae or a closely related plant thereof is used. It can be used as it is, dried, dried powder or solvent extract, and its use form is not limited. Solvents for extracting extracts from peony flowers include water or alcohols such as methanol, ethanol, isopropyl alcohol and butanol; esters such as ethyl acetate; ketones such as acetone; ethers such as diethyl ether; organic solvents such as chloroform. Alternatively, a mixed solvent thereof may be used. The extract can be used after appropriately concentrating, purifying, sterilizing, drying and the like.

The flower extract of the peony can be formulated with commonly used carriers, auxiliaries, additives and the like, and can be used as an oral product as a pharmaceutical according to a conventional method. Pharmaceuticals include tablets, capsules, granules and syrups as oral preparations. When these products are administered to the human body as pharmaceuticals, 125 mg to 2.0 mg
00 mg / kg body weight, preferably 250 mg to 1,
The dose of 000 mg / kg body weight is administered once or several times a day, and the effect can be sufficiently exerted.

The medicament of the present invention can take the required unit dosage form together with physiologically acceptable vehicles, carriers, excipients, integrating agents, stabilizers, flavoring agents and the like. The adjuvants mixed with tablets and capsules are as follows. Binders such as tragacanth, gum arabic, corn starch, gelatin, excipients such as microcrystalline cellulose, corn starch, whole gelatinized starch, leavening agents such as alginic acid, lubricants such as magnesium stearate, Sweeteners such as sugar, lactose, saccharin, flavoring agents such as peppermint, reddish oil, and cherry. In the case of a capsule, the above-mentioned materials may further contain a liquid carrier such as oil and fat, and other materials may be used as a coating agent or to change the physical form of the preparation by another method. it can. For example, tablets may be coated with shellac, sugar. A syrup or elixir may contain sucrose as a sweetening agent, methyl or propylparabens as preservatives, a dye and flavoring such as cherry or orange flavor.

The food and drink of the present invention may be in the form of the above-mentioned preparations, but may also be processed and manufactured by adding a required amount to each food material in the form of candy, rice crackers, cookies, drinks, etc., and then by a general manufacturing method. it can. As intake as health food and functional food is used for disease prevention and health maintenance,
Oral intake is divided into several times a day, and the total daily amount is 6.2.
It is ingested as a processed product containing 5 to 100 g, preferably 12.5 g to 50 g.

The method of adding the drug of the present invention to these foods and drinks will be described. The extract or powder of the present invention may be added as it is.
A 2% aqueous solution or an aqueous alcohol solution or an alcohol solution having a final concentration of 0.001 for food and drink.
It is desirable to add so as to be 15 to 15% by weight, preferably 0.01 to 10% by weight.

[0014]

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

Example 1 (1) Preparation of Methanol Extract of Shakuyaku Flower 100 g of dried powder of Shakuyaku flower was ultrasonically extracted with 70% methanol, concentrated under reduced pressure, and freeze-dried to obtain 55 g of methanol extract. Further, the mixture was partitioned and extracted with water-saturated butanol, the butanol layer was separated, concentrated under reduced pressure, and lyophilized to obtain 13 g of a butanol extract. The butanol extract was subjected to ODS silica gel chromatography with acetonitrile and water to obtain 2.12 g of a 30% acetonitrile fraction. Hereinafter, examination was performed using these extracts.

(2) Measurement of α-Glucosidase Inhibitory Activity This test was performed according to the method of Asano et al. [Toshihiko Asano et al .: Journal of Japan Society of Nutrition and Food Science, 49 (3), 157-162 (1996)]. 0.45 mL of a 50 mM sucrose solution or a 50 mM maltose solution as a substrate and a sample solution (3 mg of an extract dissolved in 1 mL of water) 0.0
5 mL and 0.50 mL of rat small intestine crude enzyme solution were added,
The reaction was performed at 37 ° C. for 60 minutes. Thereafter, the reaction was stopped, and the amount of glucose produced by the enzyme reaction was quantified using a commercially available glucose measurement kit [F kit, Roche Diagnostics Co., Ltd.]. The inhibitory activity was determined by the amount of sample added (IC
₅₀ ).

[0017]

[Table 1]

(3) Investigation of Suppressive Effect on Blood Glucose Increase A 6-week-old male SD rat fasted for 20 hours was treated with sucrose (2.5 g / Kg) together with the methanol extract or acetonitrile fraction of Example 1 (1). 500mg /
Kg) was administered once, before administration, administration 30, 60 and 1
Twenty minutes later, blood was collected from the tail vein, and the blood glucose level was measured by the glucose oxidase method. In the control group, water was administered together with sucrose, and the blood glucose level was measured in the same manner as in the administration group.

[0019]

[Table 2] The SD is a standard deviation, and P <0.01
Indicates that there is a significant difference at a risk rate of 1% or less.

Example 2 (Tablets, Capsules) The extract obtained in (1) of Example 1 10.0 g Lactose 75.0 g Magnesium stearate 15.0 g Total 100.0 g The above parts by weight are uniform. To make tablets and capsules according to a conventional method.

Example 3 (Powder, Granule) Extract obtained in (1) of Example 1 20.0 g Starch 30.0 g Lactose 50.0 g Total 100.0 g The above parts by weight are uniformly mixed. Then, powders and granules were prepared according to a conventional method.

Example 4 (Injection) The extract obtained in (1) of Example 1 1.0 g Surfactant 9.0 g Physiological saline 90.0 g Total 100.0 g Heating the above parts by weight It was mixed and sterilized to give an injection.

Example 5 (candy) Sucrose 19.9 g starch syrup (75% solid content) 70.0 g water 9.5 g coloring agent 0.45 g flavoring agent 0.05 g Extraction obtained in (1) of Example 1 0.1 g in total 100.0 g In total, each component in the above parts by weight was used to make a candy according to a conventional method.

Example 6 (Juice) Concentrated orange juice 15.0 g Fructose 5.0 g Citric acid 0.2 g Flavor 0.1 g Colorant 0.15 g Sodium ascorbate 0.05 g Obtained in Example 1 (1) 0.1 g of the obtained extract 79.4 g of water 100.0 g in total 100.0 g A juice was prepared from the above components by weight in accordance with a conventional method.

Example 7 (Cookie) Soft flour 32.0 g Whole egg 16.0 g Butter 16.0 g Sugar 25.0 g Water 10.7 g Baking powder 0.2 g Extract obtained in (1) of Example 1 0 0.1 g in total 100.0 g A cookie was prepared according to a conventional method using each of the above components by weight.

[0026]

(1) The present invention is a saccharide-degrading enzyme inhibitor such as α-glucosidase derived from a natural substance which is a substance contained in a plant, has excellent processing characteristics, and is highly safe for a living body. , By inhibiting the activity of carbohydrate degrading enzymes, which are digestive enzymes, has an effect of suppressing blood glucose elevation, such as hyperglycemia and obesity, hyperlipidemia, hyperlipidemia, diabetes, etc. derived from hyperglycemia It is effective for various diseases. (2) According to the present invention, a food or drink containing the saccharolytic enzyme inhibitor having the above-mentioned properties can be provided.

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Claims (3)

[Claims] 1. A carbohydrate-degrading enzyme inhibitor comprising a peony flower or an extract of a peony flower as an active ingredient. 2. The saccharolytic enzyme inhibitor according to claim 1, wherein the saccharolytic enzyme is α-glucosidase. 3. A food or drink comprising the saccharide-degrading enzyme inhibitor according to claim 1 or 2.