JP2006104094A - alpha-GLUCOSIDASE INHIBITOR - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain an effective, safe and plant-based α-glucosidase inhibitor which can prevent and improve obesity and diabetes by being eaten every day, wherein, as α-glucosidase inhibitors inhibit carbohydrate metabolism of animals including human, for instance, have preventive action on elevation of glycemia, and as a result, are effective for preventing and treating hyperglycemia, hyperglycemia-caused obesity, adiposis, hyperlipemia, diabetes and the like, so many α-glucosidase inhibitors are developed, nevertheless plant-based ones are not put to practical use as foods and drinks, medicines and quasi drugs. <P>SOLUTION: This α-glucosidase inhibitor contains an extract of Phyllanthus emblica or Embica offinale as an active ingredient. The α-glucosidase inhibitor using fruits of Phyllanthus emblica or Embica offinale is provided. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to an α-glucosidase inhibitor.

  Since the α-glucosidase inhibitor suppresses metabolism of carbohydrates of animals including human beings, it has an action to suppress an increase in blood sugar. As a result, it is effective for the prevention and treatment of hyperglycemia symptoms and obesity, adiposity, hyperlipidemia, diabetes caused by hyperglycemia. Moreover, the foodstuff manufactured containing the alpha-glucosidase inhibitor is suitable for a patient's diet, and also suitable as a disease prevention food of a healthy person. Some plant natural products have long been used in traditional or folk remedies as being effective for diabetes, but there are currently only a few that have clearly demonstrated their efficacy and mechanism of action. is there. To date, inhibitors such as varienamine (patent document 1), epivariol (patent document 2), acarbose and voglibose (patent document 3) have been reported as α-glucosidase inhibitors.

JP-A-57-59813 (page 1-3) JP 58-124748 A (page 1-9) JP-A-9-67271 (page 1-18)

  As described above, many α-glucosidase inhibitors have been developed so far, but there has been a problem of side effects. In addition, plant-derived products have not been sufficiently put into practical use in foods and drinks, pharmaceuticals, and quasi drugs. Therefore, an object of the present invention is to provide a plant-derived α-glucosidase inhibitor that can prevent and ameliorate obesity and diabetes when taken daily, and is effective and safe.

  As a result of examining α-glucosidase inhibitory activity of extracts from natural plant materials, the present inventors found that Amla extract is a natural food material that is safe for the human body and also inhibits α-glucosidase. It was discovered that it has activity and the present invention was completed.

  Amla used in the present invention is a scientific name: Emblica officinale or Philanthus embrica, which is a sub-tree of deciduous trees belonging to the genus Euphorbiaceae, from the Indian region to southern Malaysia It is distributed over the country, and India is considered the origin. In addition, each region or language has its own unique name, such as citrus, oil sweets, Satsuma mushrooms, Emblic Mirobaran, Armala Key, Melaka tree, Malacca tree, Indian Gooseberry, Aronra, Amira, Amiraki, Amira Cattra, Nerikai, It is also called Neruri, Tasha, Kayuraka, Kemuraka, Nakhon Pong and others.

  The country of origin of Amla used in the present invention is from India to the Malaysian region and southern China, and any of those cultivated in these regions can be used. It is cultivated in China, most preferably cultivated in India.

  In the present invention, the site of Amla is not particularly limited, but fruits, roots, stems, leaves and flowers can be used. Preferably, a fruit can be used from the viewpoint of productivity. The form is not particularly limited, and any of immature fruits, fully-ripe fruits, dried fruits and the like may be used.

  It does not specifically limit as a solvent used for this invention, It can extract using water, an organic solvent, or these mixtures. Examples of the organic solvent include lower alcohols such as methanol, ethanol, and propanol, and ethers such as acetone, ethyl acetate, and diethyl ether. Ethyl acetate is preferable from the viewpoint of obtaining a high effect.

  The extraction time when producing the α-glucosidase inhibitor of the present invention is not particularly limited, but when the Amla site is a fruit, it differs between an undried fruit and a dried fruit. For example, (1) When Amla fruit is undried, the treatment time is 0.5 to 12 hours, preferably 2 to 8 hours, and most preferably 3 to 5 hours from the viewpoint of productivity. . When the treatment time is less than 0.5 hours, the treatment of Amla fruit tissue becomes insufficient, and the production yield of the α-glucosidase inhibitor of the present invention is small. Even if the treatment time exceeds 12 hours, the treatment of Amla fruit part does not proceed any further, and the production yield of the α-glucosidase inhibitor of the present invention does not increase so much. (2) When Amla fruit is dried, from the viewpoint of productivity, the treatment time is 0.5 to 48 hours, preferably 2 to 24 hours, and most preferably 5 to 20 hours. When the treatment time is less than 0.5 hours, the treatment of Amla fruit tissue becomes insufficient, and the production yield of the α-glucosidase inhibitor of the present invention is small. Even if the treatment time exceeds 48 hours, the treatment of the Amla fruit part does not proceed any further, and the production yield of the α-glucosidase inhibitor of the present invention does not increase so much.

  The α-glucosidase inhibitor of the present invention can be applied to foods and drinks, feeds, pharmaceuticals or quasi drugs, and preferably foods and drinks that can be easily consumed by humans.

  The food and drink in the present invention is not particularly limited as long as it is a form that can be taken orally, such as a solution, suspension, powder, or solid molded product. More specifically, instant noodles, retort food, canned food, microwave food, instant soups such as instant soup and miso soup, freeze-dried food, soft drink, fruit juice drink, vegetable drink, soy milk drink, coffee drink, tea drink Beverages such as powdered beverages, concentrated beverages, nutritional beverages, alcoholic beverages, bread, pasta, noodles, cake mixes, flour products such as fried flour and bread crumbs, rice cakes, caramel, chewing gum, chocolate, cookies, biscuits, cakes, Sweets such as pies, snacks, crackers, Japanese sweets, desserts, sauces, processed tomato seasonings, flavor seasonings, cooking mixes, sauces, dressings, soups, curry and stew seasonings, processing Fats and oils such as butter, margarine and mayonnaise, milk beverages, yogurts, lactic acid bacteria beverages, ice creams, chestnuts Agricultural processing of dairy products such as mussels, frozen foods, processed fishery products such as fish ham and sausages, marine products, processed livestock products such as livestock ham and sausages, canned agricultural products, jams and marmalades, pickles, boiled beans and cereals Goods etc. are illustrated. Examples of feed include dairy farming, pig farming, chicken farming, and fish farming. Examples of pharmaceuticals or quasi drugs include internal liquids, tablets, dragees, sublingual tablets, granules, capsules (hard capsules, soft capsules, microcapsules), liquids, emulsions, suspensions, powders, and the like. Illustrated.

In the present invention, the α-glucosidase inhibitor can enhance various nutritional components when processed into foods and drinks, feeds, pharmaceuticals or quasi drugs. Nutritional ingredients that can be strengthened include vitamins such as vitamin A, vitamin B ₁ , vitamin B ₂ , vitamin B ₆ , vitamin B ₁₂ , vitamin C, vitamin D, vitamin E, niacin (nicotinic acid), pantothenic acid, folic acid, Essential amino acids such as lysine, threonine and tryptophan, minerals such as calcium, magnesium, iron, zinc and copper, and for example, α-linolenic acid, EPA, DHA, evening primrose oil, octacosanol, casein phosphopeptide (CPP), Casein calcium peptide (CCP), water-soluble dietary fiber, insoluble dietary fiber, substances that contribute to human health, such as oligosaccharides, and one or more useful substances approved as other foods and food additives Can be used.

  EXAMPLES Hereinafter, although an Example demonstrates this invention in detail, the following Example does not limit the scope of the present invention.

(Example 1) Preparation 1 of an α-glucosidase inhibitor
1 liter of distilled water was added to 100 grams of dried Amla fruits and extracted at 55 ° C. for 2 hours. Then, it filtered and the filtrate was dried by freeze-drying and the alpha-glucosidase inhibitor 38g of this invention was obtained.

Example 2 Preparation 2 of α-Glucosidase Inhibitor
1 liter of distilled water was added to 100 grams of dried Amla fruits and extracted at 55 ° C. for 2 hours. 100 ml of the extract and 100 ml of ethyl acetate were mixed in a separatory funnel and extracted at room temperature for 24 hours. Thereafter, the ethyl acetate fraction and the water fraction were separated, and the solvent was completely removed, followed by drying by freeze drying. Thus, 0.5 g of the α-glucosidase inhibitor of the present invention was obtained from the ethyl acetate fraction.

(Test Example) α-Glucosidase Inhibitory Activity The α-glucosidase inhibitory activity in the examples was determined by the following method.
1. α-Glucosidase As α-glucosidase, α-glucosidase derived from Bacillus stearothermophilus (manufactured by SIGMA) was used.
2. Principle of measurement α-glucosidase inhibitory activity is determined by measuring the amount of p-nitrophenol produced by hydrolysis of p-nitrophenyl-α-D-glucopyranoside.
3. Enzymatic reaction (1) Sample solution (50 μl)
The test extract was dissolved in 0.25M phosphate buffer (pH 6.5).
(2) Buffer solution (250 μl)
A 0.25M phosphate buffer (pH 6.5) was used.
(3) Substrate solution (100 μl)
A 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 0.25M phosphate buffer (pH 6.5)) was used.
(5) Reaction stop solution (1000 μl)
A 0.1 M sodium carbonate solution was used.
4). Reaction After adding 250 μl of buffer solution and 100 μl of substrate solution to 50 μl of sample solution, 100 μl of enzyme solution was added and reacted at 37 ° C. for 20 minutes. After terminating the reaction by adding 1000 μl of the reaction stop solution, the amount of p-nitrophenol produced was calculated from the absorbance at 400 nm. As a control, 0.25M phosphate buffer (pH 6.5) was used instead of the sample solution. In addition, as each blank, what added the enzyme solution after adding reaction stop liquid was used.
5. Calculation method 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

  Table 1 shows the α-glucosidase inhibitory activity rates (%) at various concentrations of the Amla extract obtained in Examples 1 and 2.

The α-glucosidase inhibitory activity rate of the Amla extract obtained in Examples 1 and 2 was examined, and the 50% inhibitory activity concentration (IC ₅₀ ) was determined. The respective results are shown in Table 2.

  As shown in Example 2, it was revealed that the extract of Amla of the present invention exhibits inhibitory activity against α-glucosidase. Moreover, it became clear that the ethyl acetate fraction has α-glucosidase activity which is about 5 times higher than that of water extraction.

(Example 3) Tablet 150 g of Amla extract obtained in Example 1 was mixed with 150 g of lactose and 5 g of magnesium stearate, and tableted with a tableting machine to obtain a tablet.

(Example 4) Chocolate Using the Amla extract obtained in Example 1, chocolate was produced with the following composition.
(Blending ingredients) (Blending amount)
Cacaomas 15.4g
Sugar (sucrose) 40.0g
Whole milk powder 25.0g
Cocoa butter 20.0g
Amla extract 1.0g
Lecithin 0.5g
Fragrance 0.05g

(Example 5) Cookie Using the Amla extract obtained in Example 1, a cookie having the following composition was produced.
(Blending ingredients) (Blending amount)
Flour 100.0g
Shortening 20.0g
10.0 g butter
Sugar (sucrose) 30.0g
4.0g egg
0.3g of salt
Amla extract 0.5g
Expansion agent 0.5g
Fragrance 0.2g

(Example 6) Candy Using the Amla extract obtained in Example 1, a candy having the following composition was produced.
(Blending ingredients) (Blending amount)
Sugar (sucrose) 50.0g
Minamata 50.0g
Amla extract 0.5g
Citric acid 0.3g
Fragrance 0.2g
Appropriate amount of dye

(Example 7) Health drink A health drink having the following composition was produced using the Amla extract obtained in Example 1.
(Blending ingredients) (Blending amount)
15.0g of honey
Citric acid 0.1g
dl-malic acid 0.1g
Amla extract 2.0g
D-sorbitol solution (70%) 10.0 g
Sodium benzoate 0.05g
Perfume Appropriate amount of purified water 100

(Example 8) Fruit juice beverage Using the Amla extract obtained in Example 1, a fruit juice beverage having the following composition was produced.
(Blending ingredients) (Blending amount)
Glucose liquid sugar 33.0g
Grapefruit juice 40.0g
Amla extract 5.0g
Fragrance Appropriate amount Acidity agent Appropriate amount

  According to the present invention, Amla extract has an excellent α-glucosidase inhibitory activity, and therefore the α-glucosidase inhibitor of the present invention containing the extract as an active ingredient is hyperglycemic symptoms and obesity caused by hyperglycemia. It is effective for the prevention and treatment of infectious diseases, adiposity, hyperlipidemia, and diabetes.

  The amla extract used in the present invention is a naturally derived substance, which is highly safe and optimal for consumption in daily life. Food, food additives, animal feed, animal feed additives, pharmaceuticals The contribution to industry is expected to be significant.

Claims (7)

Α-Glucosidase inhibitor containing Amla extract as active ingredient The α-glucosidase inhibitor according to claim 1, wherein the site of Amla is a fruit. 2. The α-glucosidase inhibitor according to claim 1, wherein the extraction solvent for Amla is water, an organic solvent, or a mixture thereof. A food or drink comprising the α-glucosidase inhibitor according to any one of claims 1 to 3. A feed comprising the α-glucosidase inhibitor according to any one of claims 1 to 3. A pharmaceutical comprising the α-glucosidase inhibitor according to any one of claims 1 to 3. A quasi-drug containing the α-glucosidase inhibitor according to any one of claims 1 to 3.