JP2001181194A - Alpha-glucosidase inhibitor - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a highly safe α-glucosidase inhibitor which can be used for medicines, foods and so on, and is originated from natural products. SOLUTION: This α-glucosidase inhibitor containing the extract of Pimenta dioica or Syzygium aromaticum as an active ingredient.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an α-glucosidase inhibitor containing an extract of allspice and clove as an active ingredient which can be used for pharmaceuticals, foods and the like.

[0002]

2. Description of the Related Art An .alpha.-glucosidase inhibitor suppresses the metabolism of carbohydrates in animals including humans, and thus has an effect of suppressing an increase in blood glucose as an example. As a result, it is effective for prevention and treatment of hyperglycemic symptoms and obesity, adiposity, hyperlipidemia, diabetes and the like caused by hyperglycemia. Also, α-
The food produced containing the glucosidase inhibitor is suitable for the dietary treatment of patients and can also be applied as a disease prevention diet for healthy people.

[0003] Some natural plant products have long been used in traditional or folk remedies as being effective for diabetes, but the medicinal effects and the mechanism of action are rarely clearly demonstrated. Is the current situation.

[0004] Up to now, varienamine (JP-A-57-59813), epivariol (JP-A-58-124748) and acarbose have been used as α-glucosidase inhibitors.
(Japanese Patent Publication No. 54-39474), voglibose (Japanese Unexamined Patent Publication No.
No. 9-67271) as an active ingredient.

[0005]

As described above, many α-glucosidase inhibitors have been developed to date. However, those derived from plants have not yet been sufficiently applied to pharmaceuticals and foods. Therefore, the present invention
It is intended to prevent and improve obesity and diabetes by eating daily, and to provide an effective and safe plant-derived natural α-glucosidase agent.

[0006]

Means for Solving the Problems The present inventors have developed a novel α-glucosidase inhibitor which improves hyperglycemic symptoms by using a spice,
Screening was conducted on herbs, herbal medicines, and vegetables. As a result, allspice (Pimenta dioica),
The present inventors have found an α-glucosidase inhibitor which is excellent in safety and efficacy among extracts extracted from clove (Syzygium aromaticum) and is useful for prevention and improvement of obesity and diabetes, and completed the present invention.

The present invention is constituted by the following items. (Claim 1) α containing an extract of allspice as an active ingredient
-Glucosidase inhibitors. (Item 2) An α-glucosidase inhibitor comprising an extract of clove as an active ingredient.

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION Allspice is an evergreen tree of the family Myrtaceae, and its origin is the West Indies, tropical America and the like. Dried immature fruits are used for flatulence and indigestion, and as food flavors. Its main essential oil components are eugenol, cineol, ferrandrene and the like.

Clove (clove: clove) is an evergreen tree of the family Myrtaceae, and its origin is the Moroccan Islands of Indonesia. The dried buds are used as aromatic gastric medicines, dental disinfection, and as a food flavor for pain relief. Its main components are phenylpropanoids, sesquiterpenoids, chromone glycosides, flavonoids, tannins and the like.

[0010] Each of the collected materials, all spices and cloves may be extracted in an undried state, but is usually extracted after drying. Dried allspice and cloves, which are generally marketed as Chinese herbs and spices, can also be used. Their properties may be chip-like or powder-like. These α-glucosidase inhibiting active ingredients can be obtained by immersion in water or a hydrophilic organic solvent. As an extraction method, heat extraction and continuous extraction may be performed. The obtained extract is freeze-dried,
It can be dried by spray drying or the like.

[0011] The α-glucosidase inhibitor of the present invention contains all the extracts from allspice and clove as active ingredients. When used as a drug,
Dilution with non-toxic carriers such as water, ethanol, liquid carriers such as polyethylene glycol and ethylene glycol, and solid carriers such as starch, cellulose and lactose to make granules, tablets, pills, soft capsules, syrups, etc. You can also.

Since the α-glucosidase inhibitor of the present invention has an action of suppressing an increase in blood glucose, it can be used, for example, for liquid foods such as soups, miso soups, soft drinks, and nutritional supplement drinks, as well as crackers, snacks, breads and candies. And can be used as a dietary diet for patients or a disease prevention diet for healthy people. The addition amount at this time is particularly preferably 0.05 to 2% by weight. Furthermore, when the preparation containing the α-glucosidase inhibitor of the present invention is taken before, during, or after a meal, a rapid increase in blood glucose level after eating can be suppressed.

The dosage used is 1-2 times per day for the extract.
00 mg / kg body weight, preferably 20-100 mg / k
g, usually 1-5 times daily. However,
The exact dose may be selected from the above range in consideration of age, weight, symptoms, and the like.

[0014]

EXAMPLES The α-glucosidase inhibitory activity in the examples was determined by the following method. 1. α-Glucosidase As α-glucosidase, Bacillus stearothermo
α-glucosidase from philus (SIGMA) was used.

2. Measurement principle α-glucosidase activity is determined by p-nitrophenyl-α-D-gl
This is a measurement of the amount of p-nitrophenol produced by the hydrolysis of ucopyranoside.

3. Enzyme reaction (1) Sample solution (50 μl) The test extract (all spice, extract from clove) was dissolved in 70% ethanol. (2) Buffer (250 μl) A 0.25 M phosphate buffer (pH 6.5) was used. (3) Substrate solution (100 μl) 1.4 mM p-nitrophenyl-α-D-glucopyranoside
Solution (dissolved in 0.25 M phosphate buffer (pH 6.5))
Was used. (4) Enzyme solution (100 μl) An α-glucosidase enzyme solution (0.3 units, dissolved in a 0.25 M phosphate buffer (pH 6.5)) was used. (5) Reaction stopping solution (1000 μl) A 0.1 M sodium carbonate solution was used. Sample solution 50μ
After adding 250 μl of a buffer solution and 100 μl of a substrate solution to 1 liter, 100 μl of an enzyme solution was added and reacted at 37 ° C. for 20 minutes. After terminating the reaction by adding 1000 μl of a reaction stopping solution, the amount of the generated p-nitrophenol was reduced to 400 nm.
Was calculated from the absorbance. As a control, 70% ethanol was used instead of the sample solution. In addition, what added the enzyme solution after adding the reaction stopping solution was used as each blank.

4. Method for calculating α-glucosidase inhibitory activity Inhibitory activity rate (%) = [((A−B) − (C−D)) / (A−
B)] × 100 A: Absorbance of control solution B: Absorbance of blank of control solution C: Absorbance of sample solution D: Absorbance of blank of sample solution

Example 1 Ethanol Extraction 1000 g of dried allspice was pulverized, and 3 g
000 ml of 70% ethanol was added, the mixture was stirred occasionally, allowed to stand at room temperature, and extracted for 24 hours. The obtained extract was filtered, concentrated under reduced pressure, and further freeze-dried to obtain 52.5 g of an extract of the objective α-glucosidase inhibitor. In addition, the dried clove is also extracted 6 by the same extraction method.
2.4 g were obtained. The α-glucosidase inhibitory activity of each ethanol extract was measured and is shown in Table 1.

[0019]

[Table 1]

(Example 2) Water extraction 200 g of dried allspice was ground, and 40 g of
00 ml of purified water was added, and the mixture was heated to 95 to 100 ° C and extracted for 10 minutes. The obtained extract was filtered, concentrated under reduced pressure, and further dried by freeze-drying to obtain 5.4 g of the target α-glucosidase inhibitor extract. In addition, 9.6 g of an extract was obtained for the dried clove by the same extraction method.

Example 3 Tableting The all-spice extract obtained in Example 1 was prepared with the following composition. All-spice extract 10% by weight Lactose 68% by weight Crystalline cellulose 14% by weight Carboxymethylcellulose calcium 5% by weight Magnesium stearate 3% by weight The above materials are uniformly mixed, kneaded with water, dried and single shot. Tablets were produced with a tablet machine.

(Example 4) 50% inhibitory activity concentration The α-glucosidase inhibitory activity rate of the allspice and clove extract obtained in Examples 1 and 2 was examined.
% Inhibitory activity concentration (IC ₅₀ ) was determined. Table 2 shows the results.

[0023]

[Table 2]

As shown in Table 2, the α-glucosidase inhibitor containing a water-containing ethanol extract of each plant-derived material (allspice, clove) of the present invention as an active ingredient is:
It can be seen that the inhibitory activity is about 8 to 10 times higher than that of the water extract. The α-glucosidase inhibitor of the present invention,
It has been clarified that the compound has a sufficiently strong effect even in comparison with the reported inhibitors of natural products.

[0025]

According to the present invention, there is provided an α-glucosidase inhibitor containing a solvent extract from allspice and clove as a main component. Α- obtained by the present invention
The glucosidase inhibitor has a higher α-glucosidase inhibition than conventional α-glucosidase inhibitors and is effective at a low concentration, and is derived from a natural plant product and has excellent safety. When the α-glucosidase inhibitor of the present invention is contained in food, it can be used for the prevention and treatment of hyperglycemia or various diseases caused by hyperglycemia.

──────────────────────────────────────────────────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

Claims (2)

[Claims] An α-glucosidase inhibitor comprising an extract of allspice as an active ingredient. 2. An α-protein comprising a clove extract as an active ingredient.
Glucosidase inhibitors.