JP2007015932A - Antidiabetic and/or antigout active composition, food and beverage containing the composition and method for producing the composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a composition that has slight adverse effect and other problems even in long-term use, remarkably reduces blood sugar level and uric acid level in blood and has antidiabetic and/or antigout activity and a food and a beverage that each contain the composition and have antidiabetic and/or antigout function and to provide a method for producing the composition. <P>SOLUTION: The antidiabetic and/or antigout active composition comprises an extract as an active ingredient obtained by extraction from stems and/or rhizomes of a plant of the family Actinidiaceae by using an aqueous solvent. The food and the beverage having antidiabetic and/or antigout function are obtained by mixing a food and a beverage with the antidiabetic and/or antigout active composition. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to an anti-diabetic and / or anti-gout active composition, a food and beverage containing the composition, and a method for producing the composition.

  Conventionally, various drugs for treating or preventing diabetes or diabetes-related diseases have been proposed. For example, aminoguanidine, a carbonyl reagent, has attracted attention. Therefore, there are problems such as side effects.

On the other hand, as a drug derived from a natural material with few side effects and other difficulties for long-term use, for example, a water-soluble extract from Toberaceae plants (see Patent Document 1), a cacao extract containing dietary fiber (Patent Document 2) Reference), banaba leaf extract (see Patent Document 3), and extract of wild rice, black rice, red rice, etc. (see Patent Document 4), etc., which can be put into practical use as a specific medicine for diabetes, etc. Is not obtained.
Japanese Patent Publication No. 6-99318 Japanese Patent No. 3533181 Japanese Patent No. 3507115 Japanese Patent No. 3333416

  Accordingly, the present invention is a composition having anti-diabetic and / or anti-gout activity such that it has few side effects and other problems even when used for a long period of time and significantly reduces blood glucose level and uric acid level in the blood, It is an object of the present invention to provide a food and beverage having anti-diabetic and / or anti-gout function, and a method for producing the composition.

The inventors of the present invention have found that an extract of the scorpionaceae plant that has been used as an edible food, beverage or medicinal herb for a long time has anti-diabetic and / or anti-gout activity, and completed the present invention. .
That is, the present invention employs the following configurations 1 to 9.
1. An anti-diabetic and / or anti-gout active composition characterized by containing a matabidae plant extract as an active ingredient.
2. 2. The anti-diabetic and / or anti-gout active composition according to 1, wherein the extract of the scorpionaceae plant is Actinidia kolomikta maxim.
3. 3. The anti-diabetic and / or anti-gout active composition according to 1 or 2, wherein the extract of the scorpionaceae plant is an extract of a stem and / or rhizome of the scallop plant.
4). 4. The anti-diabetic and / or anti-gout active composition according to any one of 1 to 3, characterized in that the extract of the scorpion family plant is an aqueous solvent extract.
5. A food having anti-diabetic and / or anti-gout function, comprising the anti-diabetic and / or anti-gout active composition described in any one of 5.1 to 4.
A beverage having an anti-diabetic and / or anti-gout function, comprising the anti-diabetic and / or anti-gout active composition described in any one of 6.1 to 4.
7). A method for producing an anti-diabetic and / or anti-gout active composition, which comprises extracting stems and / or rhizomes of a matabidae plant with an aqueous solvent.
8). 8. The method for producing a composition according to 7, wherein the scorpionaceae plant is Actinis colomicta maxim.
9. 9. The method for producing a composition according to 7 or 8, wherein the stem and / or rhizome of the scorpionaceae plant is steamed together with an aqueous solvent in a closed container.

The composition of the present invention has a remarkable effect as a therapeutic or prophylactic agent for diabetes or gout, such as lowering blood glucose level, uric acid level, glycated hemoglobin (HbA1c), etc. in the blood of the recipient. Further, even when used for a long time, it is less likely to cause side effects such as liver dysfunction.
The composition of the present invention can be easily taken orally as a pharmaceutical product by formulating with a carrier, or as a food or beverage having anti-diabetic and / or anti-gout function by blending in a food and beverage. it can.

In the present invention, an anti-diabetic and / or anti-gout active composition is constituted using an extract extracted from the scorpionaceae plant as an active ingredient.
A preferred example of the scorpionaceae plant is Actinis colomicuma maxim. Actinisia Colomicta Maxim is a plant distributed in the mountainous areas of Thailand, Laos and Vietnam, and has been used for food, drinks or medicinal herbs for a long time, but has anti-diabetic or anti-gout activity. Has never been known before.
The pharmacological activity of Actinis colomicta maxima varies depending on the region where it is distributed, and particularly preferred are Sam Nua Town, Hoa Pan Province, Dong Heng Town, Savannakhet Province, Phong Horn Town, Vientiane Province; Nakhon Panam Town, Thailand. The one that grows naturally in mountainous areas such as Dong Ha in Vietnam.

In the present invention, the target composition having antidiabetic and antigout activity is produced by extracting leaves, stems, rhizomes and the like of the scorpionaceae plant such as Actinidia colomicuma maxim with an aqueous solvent.
As an aqueous solvent, water, preferably pure water or deionized water, or water and alcohols such as methyl alcohol, ethyl alcohol, propyl alcohol, butyl alcohol, ethylene glycol, propanediol, butanediol, acetone, methyl ethyl ketone, acetonitrile A mixture with a water-soluble solvent such as ethyl acetate can be used. These water-soluble solvents may be used in combination of two or more. When a mixture of water and a water-soluble solvent is used, it is preferable to use a mixture containing about 10 to 90% by volume, particularly about 30 to 70% by volume of water in the mixture.

Hereinafter, an example of the process for producing the composition of the present invention using Actinis colomicum maxim as a raw material will be described.
(1) Roughly pulverize the stems and rhizomes of the raw material plant so that the center diameter is about 5 to 50 mm. The size of the coarsely pulverized raw material is preferably adjusted so that the average value of the center diameter is about 30 mm.
(2) About 10 to 20 times as much aqueous solvent as the weight ratio is used for the coarsely pulverized raw material, the raw material is directly immersed in the aqueous solvent in a sealed container, and the temperature is about 90 to 100 ° C. Cook for about 60 minutes. In that case, it is preferable to provide a gas phase part of about 1 to 2 times the liquid phase part by volume ratio on the upper part of the liquid phase part of the sealed container. Moreover, it is preferable that the canopy part of the gas phase part is maintained at a temperature lower by about 20 to 30 ° C. than the humidity of the liquid phase part, and the vapor is cooled and condensed to be refluxed to the liquid phase part.
(3) If necessary, an aqueous solvent is distilled off from the extract and concentrated to obtain a liquid or solid concentrate.

When the extract is used as a concentrate in the present invention, it may be used as it is after the concentration is adjusted. Further, the extract may be used after being subjected to treatment such as activated carbon treatment, resin treatment such as HP20, low-temperature standing, filtration, etc. for decolorization and removal of unnecessary substances.
Further, the extract can be used by fractionating a highly active fraction by an appropriate separation means such as gel filtration or silica gel column chromatography, or reversed-phase or normal-phase high-performance liquid chromatography. Preferable fractions include fractions having a molecular weight of 2 million to 4 million or less using a microfilter or an ultrafiltration membrane. In the present invention, such a fraction is also included in the scorpion family plant extract. The obtained extract can be used as it is or as a concentrate or a solid (for example, powder). Moreover, you may mix another component according to the intended purpose.

  In this extract, normally, about 1 to 10 mg each of anthraquinone, flavoid, and beta-d-glucan, about 0.01 to 0.5 mg of saponin, and 0.02 to 1 of zinc per 100 g of dry raw material plant. About 0 mg is included, but other heavy metals are not included.

(Pharmaceutical composition)
In the present invention, in the case where the extract of the scorpionaceae plant is a pharmaceutical composition (preventive or therapeutic agent) having anti-diabetic and / or anti-gout activity, there is no limitation on the form thereof, It may be in the form of a solution such as an aqueous solution diluted with water or the like, or a powder, a tablet or the like. In the case of molding into tablets or the like, conventionally known pharmaceutically acceptable carriers, triturating agents, disintegrating agents, lubricants and the like can be used. Any pharmaceutical form can be appropriately prepared by those skilled in the art based on the art in the pharmaceutical field. The matabidae plant extract may be added to the composition as an extract, a liquid obtained by diluting or dissolving the extract with water or the like, or a solid such as a powder.
Various routes of administration of the composition are possible, but oral administration is preferable because administration is simple. It is preferable that about 0.2-3.0 weight% is contained as content of the dry matter solid content of the extract of a scorpion family plant in a composition. However, when a highly active fraction is used, an amount corresponding to the activity can be used. Moreover, it can determine suitably by the relationship between the dosage per day and the frequency | count of administration shown below.

When the composition of the present invention is used as a therapeutic composition, about 0.01 to 0.5 g / kg (body weight) should be administered per day for an adult in terms of a matabidae plant extract (dry solid content). Is preferred.
When used as a prophylactic composition, it is preferable to administer about 0.005 to 0.3 g / kg (body weight) per day for adults in terms of a matabidae plant extract (dry solid content).

(Functional food or functional beverage)
In the present invention, an extract of the scorpion family plant can be used as an active ingredient of a functional food or functional beverage having anti-diabetic and / or anti-gout activity.
As a form of functional foods or beverages, so-called supplement foods and beverages (ie processed foods and beverages such as solutions, suspensions, powders, granules, tablets, oils, etc.) or miso, jams, dressings, etc. It may be a normal food or any other form. It does not specifically limit about the kind of functional food / beverage products, It uses as various food / beverage products. Specific examples include extract tablets, koji, confectionery, health tea, and the like, and drinks such as tea and miso soup are particularly preferred foods and drinks that are drunk in a warm state.

Moreover, in the present invention, the scorpion family plant extract can also be used as an additive for functional foods or beverages. The additive for functional food and drink may be in the form of a solution, powder, tablet, or oil. It does not specifically limit about the kind of food / beverage products added, The food / beverage products mentioned about the said functional food / beverage products are mentioned.
It is preferable that the amount of use of the scorpionaceae plant is about 0.001 to 0.05 g / kg (body weight) per day for an adult in terms of a scorpionaceae plant extract (dry solid content). It can be determined appropriately depending on the type of product.

EXAMPLES Next, the present invention will be further described with reference to examples, but the following specific examples are not intended to limit the present invention.
Example 1
The stems and rhizomes of Laotian actinidia colomicta maxim were cut so that the average central diameter was about 30 mm. 500 g (dry weight) of the cut material was placed in a sealable cylindrical container, immersed in 20 times the amount of pure water by weight, and then steamed at 95 to 97 ° C. for about 1 hour at normal pressure. At this time, the container was sealed, the temperature of the top of the container (lid part) was maintained at 70 to 80 ° C., and the water vapor generated in the container was cooled and condensed to be refluxed to the liquid phase part in the container.
Water was distilled off from the obtained extract, and it was concentrated twice to obtain 5,000 g of a solution-like concentrate.

(Example 2)
500 g (dry weight) of the cut material treated in the same manner as in Example 1 was immersed in 10 L of an aqueous mixed solvent of 1: 1 pure water: ethyl alcohol in a volume ratio, and then in a container similar to Example 1, at normal pressure. And the temperature at the top of the container was kept at 40-60 ° C. and steamed for about 1 hour.
From the obtained extract, ethyl alcohol was recovered at 50 to 60 ° C. under a reduced pressure of 10 to 20 Torr to obtain a concentrate having an alcohol content of 5% by volume or less. The concentrate was treated with a 0.2 μm microfilter to obtain 4,000 g of a liquid fraction having a molecular weight of 4 million or less.

(Example 3)
The stems and rhizomes of Laotian actinidia colomicta maxim were cut so that the average central diameter was about 30 mm. 50 g (dry weight) of the cut material is housed in a sealable cylindrical pressure vessel, immersed in deionized water 20 times the weight of the cut material by weight, and then a pressure of 1.2 to 2.0 kg / cm ² G (105 And steamed for 1 hour. The temperature at the top of the container was maintained at 80 to 95 ° C., and water vapor generated in the container was cooled and condensed to be refluxed to the liquid phase part in the container. Water was distilled off from the obtained extract to obtain about 50 g of a paste-like concentrate.

Example 4
In Example 3, instead of deionized water, an aqueous mixed solvent of 1: 1 deionized water: ethyl alcohol was used in a volume ratio, the cooking temperature was 80-90 ° C., and the temperature at the top of the vessel was 60-75 ° C. An extract was obtained in the same manner as in Example 1 except that the extract was retained.
From the obtained extract, ethyl alcohol was recovered at 50 to 60 ° C. under a reduced pressure of 10 to 20 Torr to obtain a concentrate having an alcohol content of 5% by volume or less. This concentrate was treated with an ultrafiltration membrane to obtain a liquid fraction having a molecular weight of 2 million or less.

(Example 5)
Using the solution-like concentrate obtained in Example 1 using 7 type 2 diabetic patients and 2 borderline patients as subjects, the antidiabetic activity of the composition of the present invention was tested as follows.
30 g of the concentrate obtained in Example 1 is made into tea every day, diluted to about 1 L per day, or drunk as it is for 3 months, and blood is collected on an empty stomach at the lapse of 1 month, 2 months, and 3 months, and blood sugar in the blood Values and HbA1c values were measured. The measurement results are shown in Table 1 together with the age and sex of the subject.

Type 2 diabetes is a typical lifestyle-related disease caused by overeating, lack of exercise, obesity, constitution, etc. In Japan, 95% of diabetics are said to be type 2. It is determined that the fasting blood glucose level (mg / dL) is 109 or less is normal and 126 or more is diabetic. On the other hand, the boundary type patient is a person whose blood glucose level does not enter either a normal person or a diabetic patient, and is a so-called diabetic reserve army. Among the subjects in Table 1, B and F are borderline patients. All others were type 2 diabetic patients who had received some treatment such as administration of a hypoglycemic agent, and treatment was continued during the above study.
[Glycated hemoglobin (HbA1c)]
Hemoglobin binds in the blood (glycation), and the more glucose in the blood, the more hemoglobin is glycated. Once saccharified, it remains saccharified until the end of the life of the red blood cells (about 120 days). By examining this glycated hemoglobin (in%), it is possible to know the long-term state of blood glucose control. Glycated hemoglobin indicates a weighted average value of increase or decrease in blood glucose level over the past 3 to 4 months. About half of them represent those formed within the past month, and the other half show glycated hemoglobin of the past 2-3 months.
Glycated hemoglobin is considered to have a normal value of 4.3 to 5.8 (%), is used to determine whether blood glucose control is successful, and is usually measured every month.

According to Table 1, it was found that the blood sugar level and HbA1c significantly decreased as a whole by ingestion of the composition of the present invention, and the composition of the present invention has excellent antidiabetic activity.
In all of the subjects 1 to 2 weeks after the start of drinking the composition, the stool tended to be slightly loosened, but recovered after 2 weeks. In addition, in type 2 diabetic patients, there was an example in which hands and feet were lightened in 1 week after drinking, and hands and feet were not swollen.

(About acute toxicity of the composition)
The Actinisia Colomicta Maxim used above is one that has been boiled with water for hundreds of years by residents living in the mountainous areas of Thailand, Vietnam, and Laos, and drinks like tea. It seems that there is no problem.
Among the above subjects, three subjects A, B, and C have a composition intake of 15 g / day of dry raw material in order to investigate the effect of the intake of the composition of the present invention on liver function. Table 2 shows the results of measuring the ALP, γ-GTP, and GOT, which are representative indicators of liver function, and blood was collected one month after the start of drinking. The reference range of each index is 100 to 340 IU / L for ALP, 4 to 70 IU / L for γ-GTP, and 11 to 35 IU / L for GOT, and all three persons are within the reference range. There seems to be no adverse effect on

(Example 6)
Using 3 type 2 diabetic patients (K, M, N in Table 3) and 1 borderline patient (L in Table 3) as subjects, 30 g of the fraction obtained in Example 2 was diluted with warm water. I was allowed to drink it as tea for 2 months. Table 1 shows the results of measuring blood sugar levels, HbA1c values, and uric acid levels in the blood by sampling on an empty stomach after 1 month and 2 months.

According to Table 3, the significant fall about all the blood glucose levels, HbA1c values, and uric acid levels was recognized about all the subjects.
As for the uric acid level, all members fall within the reference range (2.1 to 7.0 mg / L) after 2 months, and the composition of the present invention has an anti-diabetic activity and an excellent anti-gout activity. found.

(Example 7)
1000 mL of the solution-like concentrate obtained in Example 1 was lyophilized to obtain 5 g of powder.
4 g of this powder was mixed with 4.5 g of lactose, 6.0 g of corn starch, 0.5 g of magnesium stearate and a little sweetener, and tableted to prepare tablets each having 0.5 g.

(Example 8)
A beverage having anti-diabetic and anti-gout functions was produced by dissolving one tablet obtained in Example 7 in 1000 mL of water.

Claims (9)

  An anti-diabetic and / or anti-gout active composition characterized by containing a matabidae plant extract as an active ingredient.   The anti-diabetic and / or anti-gout active composition according to claim 1, characterized in that the scorpionaceae plant extract is Actinis colomicum maxim.   The anti-diabetic and / or anti-gout active composition according to claim 1 or 2, wherein the extract of the scorpionaceae plant is an extract of a stem and / or rhizome of the scorpion plant.   The anti-diabetic and / or anti-gout active composition according to any one of claims 1 to 3, wherein the matabidae plant extract is an aqueous solvent extract.   A food having anti-diabetic and / or anti-gout function, comprising the anti-diabetic and / or anti-gout active composition according to any one of claims 1 to 4.   A beverage having anti-diabetic and / or anti-gout function, comprising the anti-diabetic and / or anti-gout active composition according to any one of claims 1 to 4.   A method for producing an anti-diabetic and / or anti-gout active composition, comprising extracting a stem and / or rhizome of a matabidae plant with an aqueous solvent.   The method for producing a composition according to claim 7, wherein the scorpionid plant is Actinis colomicum maxim.   The method for producing a composition according to claim 7 or 8, wherein the stem and / or rhizome of the scorpion plant is steamed together with an aqueous solvent in a closed container.