JP3261090B2 - Antidiabetic agent and food containing it - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an antidiabetic agent for reducing the amount of sugar absorbed from the digestive tract, especially a mixture of a substance extracted from Salacia reticulata belonging to the family Euonymaceae and an extract of a specific natural substance. The present invention relates to an antidiabetic agent contained as an essential active ingredient.

[0002]

2. Description of the Related Art In recent years, among drugs classified as antidiabetic agents, the action of disaccharide hydrolase (α-glucosidase) present on the digestive tract mucosa is inhibited, and the production of glucose from starch and oligosaccharides is inhibited. Several types of α-glucosidase inhibitors, which suppress the rise of blood sugar by suppressing them, have been released, and are frequently used as part of the treatment and dietary treatment of diabetic patients. Also, in the life of healthy people, the so-called “diabetes reserve”, in which the intake of high calorie foods, overeating, or lack of exercise due to a Western-style dietary lifestyle or lack of exercise is a factor, and the blood sugar level is higher than in healthy people, is also known. The increase in the number of people called the "military" has become a major problem at home and abroad.

On the other hand, in the treatment of diabetes, a sulfonylurea agent, a sulfonamide agent, which promotes insulin secretion, a biguanide agent, which increases insulin sensitivity, and an α-glucosidase inhibitor, which inhibits the decomposition and absorption of carbohydrate from the intestinal tract [ For example, acarbose (manufactured by Bayer AG, trade name Gulcobay (Glucobay)) and voglibose (manufactured by Takeda Pharmaceutical Co., Ltd., trade name Basin) are commonly used as oral hypoglycemic agents. However, the oral hypoglycemic drug is not readily available because it must be prescribed strictly under the control of a physician because the purpose of use and the effect of the drug vary from patient to patient and there are problems with side effects. It is.

[0004] Among the above antidiabetic agents, α-glucosidase inhibitors can be effective for eliminating obesity due to overeating or lack of exercise and for dieting, in addition to acting as therapeutic agents for diabetes. However, not only is the above drug not readily available, but when taken, it can suppress the absorption of polysaccharides into the body, but cannot suppress the absorption of monosaccharides such as glucose, so that a remarkable inhibitory effect on sugar absorption cannot be expected. . In addition, various side effects may occur after taking the drug.

[0005] In the prevention of obesity and diabetes caused by overeating and lack of exercise, etc., and the treatment of diabetes, the most basic is a dietary regimen. Carbohydrate-derived sugars, which make up 60-70% of the diet, are absorbed from the digestive tract and become blood sugar. By becoming hyperglycemic and sustaining that hyperglycemia,
Obesity, the "pre-diabetes group", and diabetes and vascular complications derived from diabetes may occur. The body component that treats hyperglycemic conditions is insulin. Hyperglycemic conditions require hypersecretion of insulin at all times, resulting in disorders due to hypersecretion of insulin. To break this vicious cycle,
It is important to make it difficult for some form of sugar to be absorbed from the digestive tract. For that purpose, there is a demand for the development of safe and inexpensive compositions of natural origin that can be ingested as food.

[0006] As a natural substance which satisfies the above-mentioned requirements and is effective in suppressing an increase in blood sugar, Salacia reticula (Salacia reticula) which has been conventionally used as an effective drug for diabetes in India and Sri Lanka and which has been used for a long time has been used.
ta) exists. Alternatively, as other natural substances, for example, various saponin-containing substances are known. The mechanism of action of saponin-containing natural substances is generally attributed to the suppression of glucose absorption from the gastrointestinal tract, and its effect is to nonspecifically inhibit not only oligosaccharides and starch but also glucose-induced increases in blood sugar levels. It is.

[0007]

Accordingly, an object of the present invention is to suppress the rise in blood glucose more efficiently by using the above-mentioned natural materials (Salacia reticulata and a saponin-containing substance) in combination than by using each alone. Having obtained the necessary knowledge, the technical problem was overcome.

[0008]

Means for Solving the Problems The present inventor has conducted intensive studies to achieve the above object, and as a result, (a) Salacia reticulata (hereinafter abbreviated as SR) and (b) Thonburi and Taranoki Root bark, arabian bark, arabian sprouts, sugar beet root, conker nuts, gymnema leaves, bitter melon fruit, bitter melon seeds, nambankarasuri fruit, nambankarasuri seed, senega root, spinach root, Combination with at least one member selected from the group consisting of the roots of chard, the roots of Inoschiko and the bark of the cashew nut tree, in particular (a)
An antidiabetic agent comprising a combination of SR and (b) Thonburi as an active ingredient. The present invention also provides a diet food containing as an active ingredient a combination of (a) Salacia reticulata and (b) Thonburi.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION (a) SR, which is an essential element of the antidiabetic agent of the present invention, is a plant of the family Euonymus that grows mainly in Sri Lanka and India, and has aerial parts (leaves, bark, xylem, etc.).
It can be used for both underground and root (root bark). Locally, root bark is particularly effective in treating diabetes, but its activity is found in whole plants. The SR can be used as the dry powder, or as an extract from the dry powder,
Usually, they can be stored in the form of a dry powder of extracts from them. At the time of use, the dry powder of the extract is used as it is or after being dissolved in an appropriate solvent. The solvent is a solvent used at the time of extraction and may be any solvent that does not adversely affect the human body when remaining in a drug or food after preparation, and is usually water or ethanol. For example, methanol, propanol, butanol, etc.). In the present invention, the SR extract may be in the form of the filtrate after extraction, in the form of a concentrated or diluted state or its dry powder, or in the form of a mixture thereof.

Hereinafter, the natural substance extract (b) combined with the above-mentioned SR in the present invention will be described in order. Firstly, Thonburi is a fruit of the annual grass family Kochia scoparia (Kochia scoparia), which is native to Europe, and is cultivated mainly in China and Japan in Akita Prefecture.
It is marketed as food with the touch of “land caviar”. Thonburi (pea seeds) contains saponin, a triterpene glycoside such as momodin Ic, and the dried product is used in China as a crude drug called diphtheria (Kochiae fructus).

[0011] Taraxacum (Arallia elta SEEM) is a plant of the araliaceae family, and its main bud portion is used for food in Japan. It contains saponins such as elatoside l,
Not only buds but also bark and root bark can be used.

[0012] Sugar beet is also called sugar beet,
Beta vulgaris LINN.var.saccharifera AL
It is a plant based on EFELD. It is cultivated as a raw material for sugar in Europe, China, and Hokkaido in Japan. It contains a saponin such as Betavulgaroside in addition to sugars and the like, and can use the root part.

The conker is a horse chestnut (Aesculus turbina)
ta BL.) seeds, which are exposed and exposed to water in Japan, are used for food. Contains saponins such as escin la.

Gymnema sylvestre R.BR is
Potato family plant native to India, gymnemic acid and gym
It contains triterpene saponins such as nemasaponinn. The leaves are known to have a strong sweet taste suppressing effect, and the present invention uses the leaves.

The bitter melon (Momordica charantia L.)
A plant belonging to Cucurbitaceae native to India, mainly in tropical Asia,
It is cultivated in Okinawa, China, and uses its fruits for food.
It also contains the same saponins as Butterfly. In the present invention, bitter melon fruits and seeds are used.

[0016] Namambakarasuuri (Momordica cochinch)
inensis SPRENG) is a plant belonging to Cucurbitaceae. The seeds are called mokubetsushi, and are used as anti-inflammatory and antidote as an external medicine in Chinese medicine. Contains saponins, such as momordic acid, and the fruits are edible. In the present invention,
Uses the fruits and seeds of Namban Callas Uri.

[0017] Senega is a plant belonging to the family Lameidae, and is generally Senega (Polygala senega Linne) or Hirohasenega (P.
olygala senega Linne var. latifoloa Torrery et Gla
y) means the root. It is cultivated in North America as a raw material for expectorants and in Hokkaido and Hyogo Prefecture in Japan, and is also distributed in Senega Syrup of the Japanese Pharmacopoeia. presen
sene, a triterpene saponin with igenin as genin
Contains gin- etc. In the present invention, a root portion is used.

Spinach (Spinacia oleraceae L)
Is a plant of the family Acalyptaceae, whose leaves are widely used for food in Japan, and whose roots contain saponins such as saponin A. In the present invention, a root portion is used.

The chard is Beta vulgaris Li
It is an edible vegetable based on nn.Varrapa, a plant similar to sugar beet, and contains the same oleanane-based saponin. In the present invention, a root portion is used.

Achiranthes japonica (Miq)
Nakai or Achyranthes bidentata Bl.var. Japonica
Miq.) Is a plant of the family Amaranthaceae and grows in lowlands in Japan. Dried roots are called beef knees in Chinese medicine and contain saponins (momordins), similar to buffaloes. As a medicinal effect, it is used for diuresis, tonicity and the like. In the present invention, a root portion is used.

[0021] Cashew nuts are anacardium occidenta belonging to the family Urushiaceae.
ls). Although the seeds are widely cultivated in the tropics for food, bark is used in the present invention. The active ingredients of the bark of the cashew nut tree are currently unknown.

The form of use of the above-mentioned natural substance in the present invention may be a pulverized product at a predetermined site. The above-mentioned form, after considering the efficiency of the preparation, after thoroughly drying each substance,
It may be a dry powder crushed to 200 to 300 mesh by a crusher or the like. Alternatively, in the present invention, a dry powder of the above substance can be used as an extract extracted with water or alcohols (however, the extraction solvent is completely evaporated before use).

When the above natural substance is extracted with water or alcohol, 1.5 kg to 5.0 L of a solvent (water or an alcohol such as methanol, ethanol, propanol, butanol, etc.) is added to 1 kg of the above-mentioned dry powder, and heated (80%). ~
After subjecting to 90 ° C. for 2 to 4 hours or cold soaking (15 to 25 ° C. for 3 to 5 days), the solvent is completely distilled off under reduced pressure at 45 ° C. or less to obtain the target extract. . When the solvent containing the natural substance is heated in the above procedure, the yield of the obtained extract is about 20 to 28% of a water extract, about 15 to 18% of a methanol extract, about 12 to 15% of an ethanol extract, and n-propyl. Alcohol about 7-11
%, N-butanol about 8-10%. Also, when the natural substance and the solvent are subjected to cold soaking in the above procedure, the yield of the obtained extract may be reduced by 20% as compared with the case of the above heating.

The first aspect of the present invention relates to a combination of (a) SR and (b) one or more extracts of the above natural substances (for example, SR / Thonburi, SR / Taranoki root bark, S
R / Taranoki bark, SR / Taranoki sprouts, SR / Sugar beet root, SR / Conker nut, SR / Gimunema leaf, SR / bitter fruit, SR / bitter seed, S
R / Nambankasouri fruit, SR / Nambankasouri seed, SR / Senega root, SR / Spinach root, SR / Fusanthus root, SR / Inokozuchi root or SR / Kashnut tree bark, or SR / Etc.) as an active ingredient. In the antidiabetic agent of the present invention, the most preferred combination is a combination containing at least SR and Thonburi.

The mixing ratio of (a) SR and (b) the extract in the above combination is 1: 4 to 1: by weight.
Mix to get 15. When the content of salicia is larger than the above mixing ratio, the effect of suppressing glucose absorption from the digestive tract, which is the object of the present invention, becomes weak. On the other hand, when the SR content is low, the flavor changes and it becomes difficult to take the SR, which is not preferable. Alternatively, when using SR dry powder,
It requires 3 to 5 times (weight ratio) the amount of when using SR extract.

The antidiabetic agent of the present invention can be formed into a form suitable for oral administration (eg, powder, solid preparation, liquid preparation, tea preparation). The dosage of the antidiabetic agent of the present invention can vary depending on age, symptoms, etc., for example, an effective amount in an adult is
Each time, the total amount of the extract of natural substances other than SR is 80 to 150 mg per 10 mg of SR water extract.
It is preferable to take it three times a day at about 0 minutes.

In the food containing the anti-diabetic agent according to the second aspect of the present invention, the anti-diabetic agent can be appropriately added during the production of the food. The antidiabetic agent has an effect of suppressing the absorption of carbohydrates contained in food and preventing a rapid rise in blood sugar. Therefore, foods mainly containing carbohydrates (eg, rice, noodles, breads, pasta, cookies, etc.) and foods high in sugar (eg, steamed buns,
Japanese sweets such as yokan, cakes, candy, gums,
By blending the anti-diabetic agent into soft drinks such as juice and cola), it is possible to provide a food having both functions as a diet food for obesity elimination or a diet for diabetic patients, etc. However, the present invention is not particularly limited to the above foods. Such foods, just like other normal foods, can express the above-mentioned mechanism of action only by eating, so that they are free from the inconvenience of dietary restrictions and can be easily used. . In the food,
The antidiabetic agent of the present invention can be contained in an effective amount required for a single ingestion.

[0028]

EXAMPLES The antidiabetic agent of the present invention and a food containing the same will be described below using examples, but the present invention is not limited to the following examples. Preparation Example 1 (1) Preparation of SR Extract First, 1.5-5.0 kg of water was added to 1 kg of a dried and rough cut SR trunk (xylem and bark), and the mixture was heated and extracted at 80-90 ° C. for 3 hours. After cooling, the mixture was filtered. The solvent was completely distilled off from the filtrate at a temperature of 45 ° C. or lower under reduced pressure to obtain an SR water extract. (1 ′) Preparation of SR dry powder First, after a dried rough cut piece of SR trunk (xylem and bark) is sufficiently dried, it is pulverized to 200 to 300 mesh using a pulverizer to obtain SR powder. A dry powder was prepared. (2) Preparation of extract of Thonburi A methanol extract of Thonburi was obtained in the same manner as above except that 1 kg of diphtheria was used and methanol was used as a solvent. (3) Preparation of Extract of Taraxacum Using 1 kg each of bark, root bark and buds of Taraxacum, a methanol extract was obtained in the same manner as in the extraction of Thonburi. (3 ') After the dried crude cut product of arachis bark powder (bark) is sufficiently dried,
By pulverizing to 200-300 mesh using a pulverizer, barley bark powder was obtained. (4) Preparation of sugar beet root extract An extract of methanol was obtained using 1 kg of sugar beet root in the same manner as in the extraction of thrush.

(5) Preparation of conker nut extract An extract of methanol was obtained using 1 kg of conker nut in the same manner as in the extraction of thrombus. (6) Preparation of Gymnema Extract Using 1 kg of Gymnema leaves, a methanol extract was obtained in the same manner as in the extraction of Thonburi. (7) Preparation of bitter melon extract Extract 1 kg each of bitter melon fruit and seed was used, and a methanol extract was obtained in the same manner as in the extraction of thrush. (8) Preparation of Extract of Namamba Callus Uri Using 1 kg of each fruit and seed of Namamba Callas Uri, a methanol extract was obtained in the same manner as in the extraction of Thonburi. (9) Preparation of Senega extract A methanol extract was obtained using 1 kg of Senega root in the same manner as the above methanol extract. (10) Preparation of spinach extract Extract 1 kg of spinach root was used to obtain a methanol extract in the same manner as in the extraction of thrush.

(11) Preparation of Swiss Chard Extract An extract of methanol was obtained using 1 kg of Chard's root in the same manner as in the extraction of Thonburi. (12) Preparation of Inokozuchi extract An extract of methanol was obtained in the same manner as in the extraction of Thonburi using 1 kg of roots of Inokozuchi. (13) Preparation of cashew nut extract An extract of methanol was obtained using 1 kg of the bark of a cashew nut tree in the same manner as in the extraction of Thonburi.

Example 1: Inhibition of sugar absorption as an antidiabetic agent
Evaluation of Ability (1) Using the SR dry powder or water extract obtained in Preparation Example 1 above, the dry powder and / or methanol extract of each substance, and a combination thereof, using the compositions shown in Tables 1 to 3 Test drugs were prepared. Next, male Wistar rats (weight 150-180 g) fasted for 24 hours
The test drug prepared above was dissolved in water and orally administered (5 ml / kg body weight). 30 minutes later, sucrose 0.5g / kg
Body weight (5 ml / kg body weight as 10% (w / v) aqueous solution) was administered orally. Thirty minutes after administration of sucrose, 200 μl of blood was collected from the orbit under ether anesthesia, serum was separated by a conventional method, and the blood glucose level (the glucose concentration in the serum measured by the glucose oxidase method; mg / dL) was measured. This result is also shown in Table 1.
3 are shown. In the table, "dose" indicates SR in terms of oral dose (mg / kg) to rats and the amount of each substance prepared above.

[0032]

[Table 1]

[0033]

[Table 2]

[0034]

[Table 3]

From the above results, it can be seen that the SR alone (both pulverized and dried products and the water-extracted extract) and the substances prepared above (both pulverized dried products and the water-extracted extract) were mixed rather than administered alone. , The increase in blood glucose level is significantly suppressed when administered
It can also be seen that a mixture of R and a Thaliana extract is the most effective.

Example 2 and Comparative Example 1 Breads containing an antidiabetic agent (Example 2) and, as a control, breads containing no antidiabetic agent (Comparative Example 1) were prepared according to the formulations shown in the following table. It was manufactured by a conventionally known procedure.

[Table 4]

The breads of Example 2 and Comparative Example 1 were subjected to a sensory evaluation of taste and aroma for 10 panelists. As a result, in both breads, virtually no difference was found in both taste and aroma.

Example 3 and Comparative Example 2 Mizuyokan containing an antidiabetic agent (Example 3) and mizuyokan not containing an antidiabetic agent (Comparative Example 2) having the formulations shown in the following table were known. Manufactured by the procedure.

[Table 5]

The mizuyokan of Example 3 and Comparative Example 2 was
Sensory evaluation of taste and aroma was conducted for the name panelists. As a result, in both mizuyokan, virtually no difference was found in taste and aroma.

Example 4 and Comparative Example 3 A cake containing an antidiabetic agent (Example 4) and a cake not containing an antidiabetic agent (Comparative Example 3) having the composition shown in the following table were prepared by a conventionally known procedure. Manufactured.

[Table 6]

The cakes of Example 4 and Comparative Example 3 were subjected to a sensory evaluation of taste and aroma for 10 panelists. As a result, both cakes, statistically,
No substantial difference in taste and aroma was observed.

Example 5 and Comparative Example 4 A candy containing an antidiabetic agent (Example 5) and a candy not containing an antidiabetic agent (Comparative Example 4) were prepared according to a conventionally known procedure with the formulations shown in the following table. Manufactured.

[Table 7]

The candy of Example 5 and Comparative Example 4 was replaced with 1
Sensory evaluation of taste and aroma was performed on 0 panelists. As a result, between the two candies, there was no statistically significant difference in taste and aroma.

[0044]

The antidiabetic agent of the present invention is extremely useful for suppressing a postprandial rise in blood sugar level. In addition, since the raw material is an extract derived from a natural substance, it is highly safe for the human body.
In the present invention, by using an extract from Salacia reticulata (SR) in combination with another substance or an extract (extract) from SR, which has a different mechanism of action in inhibiting sugar absorption from SR, Excellent effects can be obtained with a smaller intake than each effective amount when each is used alone. The food containing the anti-diabetic agent of the present invention is very convenient because it can suppress the increase in blood glucose level after eating simply by ingesting, not only for the purpose of treating diabetes, but also for obesity elimination and diet. It is also useful for the purpose of.

──────────────────────────────────────────────────続 き Continuation of the front page (56) References JP-A-9-301882 (JP, A) JP-A-9-315990 (JP, A) JP-A-9-194498 (JP, A) Japanese Pharmaceutical Society 110th year Meeting Abstracts, 2, 214, 1990 (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 35/78 A23L 1/30 BIOSIS (STN) CA (STN) MEDLINE (STN)

Claims (3)

(57) [Claims] (1) Thalassia reticulata, (b) Thonburi, taro tree bark, taro tree bark, taro tree bud, sugar beet root, conker, gymnema leaf, bitter melon fruit, bitter gourd One or more selected from the group consisting of seeds, fruit of nambankarasuri, seeds of nambankarasuri, seeds of senega, roots of spinach, roots of chard, roots of Inokozuchi and crushed or extracted bark of cashew nut tree An antidiabetic agent comprising a combination of as an active ingredient. 2. An antidiabetic agent comprising as an active ingredient a combination of (a) Salacia reticulata and (b) Thonburi. 3. A diet food containing as an active ingredient a combination of (a) Salacia reticulata and (b) Thonburi.