JPH0940572A - Inhibitor of amylase and composition for inhibiting amylase - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a safe inhibitor of an amylase, containing a substance prepared by carrying out treatments of deoiling and extracting of Cinnamomi Cortex with a hydrous ethanol solution as an active ingredient, having excellent inhibiting actions on the amylase and hardly causing any bitterness or irritant smell peculiar to the Cinnamomi Cortex. SOLUTION: This inhibitor of an amylase contains a treated Cinnamomi Cortex prepared by carrying out treatments of deoiling and extracting of Cinnamomi Cortex with a hydrous ethanol solution as an active ingredient. For example, KANNAN Cinnamomi Cortex prepared from Cinnamomum cassia Blume as an original plant can be used as the Cinnamomi Cortex. Either of the treatments of deoiling and extracting with the hydrous ethanol solution can previously be performed; however, the deoiling can be carried out by the treatment with steam or a solvent. The extracting treatment with the hydrous ethanol solution is preferably performed by using an aqueous solution of ethanol at 50-90vol.% concentration in a weight of 1-5 times based on the Cinnamomi Cortex under heating conditions up to 80 deg.C for 1-5hr. The operations are preferably repeated 2-5 times. When the objective inhibitor is used as a medicinal composition, the daily dose thereof for an adult is preferably 0.5-2,000mg, expressed in terms of the amount of active ingredient at a time and administered three times before a meal.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an amylase inhibitor obtained from cinnamon bark and the amylase inhibitor,
The present invention relates to a composition for amylase inhibition used as a medicine or food.

[0002]

2. Description of the Related Art In recent years,
Obesity resulting from dietary habits such as satiation, overeating, and gourmet has become an important issue not only for young women but also for a wide range of age groups due to its close relationship with adult diseases such as diabetes. As a means for eliminating this obesity, methods such as exercising to burn fat and restricting diet can be considered. However, exercise is difficult to continue,
It is difficult to eliminate obesity by these methods because not only is dietary restriction accompanied by mental distress, but the burden of calorie calculation is large. In addition, it is said that adult diseases such as diabetes and gallstones which are closely related to obesity are often triggered by an increase in blood sugar due to excessive intake of starch and the like.

From these things, recently, as a simple prevention and treatment method for obesity, a method of suppressing the digestion of carbohydrates such as starch, which accounts for 60% of the energy source of the Japanese, has been considered. In other words, when eating starch foods such as rice and udon, which are the center of Japanese dietary habits, a method of suppressing the digestion of starch by taking an amylase inhibitor that inhibits the activity of amylase, which is a digestive enzyme of starch, etc. Is being considered.

Against this background, amylase inhibitors have recently attracted attention as effective means for preventing and treating obesity, and various oligosaccharides obtained mainly from seeds of seeds such as legumes and microorganisms and microorganisms. Sugar (JP-A-63-483)
No. 02) and the like contain substances having an amylase inhibitory action, and it has been proposed to apply these substances to diet foods and the like.

However, these substances have problems in effectiveness and taste of amylase inhibitory action, and most of them have not reached the stage of practical use.

The present invention has been made in view of the above circumstances, and has no problem in terms of safety and effectiveness as a medicine or food, and also has no problem in taste when ingested or eaten or eaten. And an amylase-inhibiting composition.

[0007]

Means for Solving the Problems and Modes for Carrying Out the Invention As a result of intensive investigations by the present inventors to achieve the above object,
It was found that the substance obtained by subjecting cinnamon bark to deoiling treatment and extraction process with a water-containing ethanol solution has an excellent amylase inhibitory action, and has almost no bitterness or irritating odor peculiar to cinnamon bark, and forms the present invention I arrived.

[0008] That is, the present invention is an amylase inhibitor characterized by deoiling cinnamon bark and an extract treated with a water-containing ethanol solution as an active ingredient, and an amylase inhibitor composition used as a pharmaceutical or food. Thus, there is provided a composition for inhibiting amylase, which comprises the above-mentioned amylase inhibitor as an active ingredient.

The present invention will be described in more detail below. In the present invention, the cinnamon is Cinnamom.
Guangnan cinnamon that uses um cassia Blume as a progenitor plant can be used, but the species is not particularly limited. For example, C. zeylanicum Nees, which is a closely related species, and Vietnam cinnamon (C. obtussifolium Nees), Japanese cinnamon (C. sieboldii Meisn), Java cinnamon (C. burmanni Blume), Thai cinnamon (C. iners Reinw. ex Blume)
Etc. can be effectively used. Further, cinnamon powder can be used as the cinnamon of the present invention.

The amylase inhibitor applicable to the present invention is
It is obtained by subjecting the cinnamon bark to a deoiling treatment and a hydrous ethanol extraction treatment. In this case, the order of both processes is not particularly limited.

The deoiling treatment and hydrous ethanol extraction treatment performed on the cinnamon of the present invention will be described in more detail below.

The oil removal treatment applied to the cinnamon bark of the present invention may be carried out before or after extraction with a water-containing ethanol solution. This oil removal is carried out by steam treatment or hexane,
It can be performed by solvent treatment using an organic solvent such as acetone or ether.

More specifically, when the deoiling treatment is carried out by steaming and the steaming is carried out before the hydrous ethanol extraction, for example, cinnamon bark is 0.5 to 10 times its weight, more preferably 1 ~ 5 times the weight of water, then 0.5 to 24 hours, more preferably 1 to 10 hours,
Examples thereof include a method of introducing steam. on the other hand,
When the steam treatment is carried out after the hydrous ethanol extraction treatment, the dried and concentrated product of the cinnamon bark extract obtained by the hydrous ethanol extraction treatment described in detail below is 5 to 100 times its weight, more preferably 10 to 50 times. Immerse in double weight of water,
Then, a method of treating in the same manner as described above can be mentioned.

When the deoiling treatment is carried out by a solvent treatment such as hexane and the treatment is carried out before the water-containing ethanol extraction treatment, the cinnamon bark is 0.5 to 10 times its weight, more preferably 1 to 5 times its weight. Immerse in heavy solvent, then 0.5-2
A method of carrying out a stirring operation for 4 hours, particularly 1 to 10 hours can be mentioned. In this case, the stirring operation can be carried out at room temperature, but it is preferable to carry out heating at 30 ° C. or higher, especially to the boiling temperature of the solvent used. The solvent treatment may be performed once, but is preferably performed 2 to 5 times. On the other hand, if the solvent treatment is performed after the hydrous ethanol extraction treatment, the cinnamon bark extract is concentrated and the dried product is
A method of immersing in a solvent having a weight of 100 to 100 times, more preferably 10 to 50 times, and then treating in the same manner as described above can be mentioned.

Next, the water-containing ethanol extraction treatment applied to the cinnamon of the present invention will be described more specifically. The water-containing ethanol solution used here contains 10 to 95% by volume of ethanol based on the whole solution. Particularly, an aqueous solution of 50 to 90% by volume is suitable. As shown in Examples described later, the extraction treatment with water or ethanol has a high amylase inhibitory activity, and while it is not possible to obtain a good substance in terms of taste, the extraction treatment with the above-mentioned hydrous ethanol, In particular, it is effective to obtain the target extract of the present invention by combining with a deoiling treatment. The amount of water-containing ethanol used is 0.5 for cinnamon bark.
The weight is preferably 10 to 10 times, more preferably 1 to 5 times. In this case, the extraction time is preferably 0.5 to
It is 10 hours, more preferably 1 to 5 hours. The extraction temperature may be room temperature, but it is preferable to perform the extraction by heating to 80 ° C. This extraction operation may be performed once, but 2 to 5
It is preferable to carry out the procedure twice.

After the deoiling treatment and the hydrous ethanol extraction treatment as described above, the amylase inhibitor of the present invention can be obtained by the following treatments.

That is, when the deoiling treatment is carried out before the hydrous ethanol extraction treatment, after the deoiling treatment, water or an organic solvent is removed by a filtration treatment or the like, and then extraction with a hydrous ethanol solution is carried out, A method of concentrating and drying the obtained extract can be adopted. Here, the extraction liquid is concentrated and dried by vacuum concentration, concentration method such as flash distillation, reduced pressure drying (vacuum drying), freeze drying, spray drying, thin film drying,
Known concentration and drying methods such as hot air drying, infrared ray drying, and high frequency drying can be used. In addition, the amylase inhibitor becomes powdery as the water content of the extract increases, and it becomes easier to handle.

On the other hand, when the deoiling treatment is performed after the hydrous ethanol extraction treatment, the cinnamon bark extract is concentrated, dried and concentrated, and the dried product (solid matter) is deoiled and then filtered. The amylase inhibitor of the present invention can be obtained by a method of removing water or an organic solvent and further drying in the same manner as above.

The amylase inhibitor of the present invention is not limited to the one obtained by pulverizing the extract or the like, but may be used as a concentrated extract, a diluent or a paste. Further, if necessary, a purification step may be added for the purpose of, for example, further increasing the amylase inhibitory activity.

The amylase inhibitor of the present invention contains a drug, other drugs used in quasi-drugs and the like, and a pharmaceutically acceptable base or food.
It can be an amylase-inhibiting composition used as a health food or food.

When the amylase-inhibiting composition of the present invention is used as a medicine, for example, an excipient, a coloring agent, a lubricant,
Binders, disintegrants, coating agents, stabilizers, preservatives and the like can be added. In this case, the mixing ratio of each component and the amylase inhibitor is not particularly limited, and a ratio suitable for formulation thereof can be appropriately selected. In addition, the dosage form of the formulation of the composition (medicine) containing these is
Examples include tablets, capsules, powders, fine granules and granules. Since the amylase inhibitor of the present invention has no problem in terms of taste, it is not necessary to mask the taste when it is used as a drug, and various dosage forms can be freely selected, and particularly in the production thereof. No special processing is required.

Although the dose of the above-mentioned drug varies depending on the condition of the disease and is not constant, it is usually preferable to take 0.5 to 2000 mg of the active ingredient per adult 3 times a day before meals.

When the amylase-inhibiting composition of the present invention is used as a food, it may be of any kind. For example, in addition to starch-containing foods such as bread, noodles, biscuits, cakes, etc., along with rice. Ingestible furikake, side dishes such as sausage, ham and kamaboko, desserts such as jelly and pudding, dairy products such as yogurt, ice cream and milk, confectioneries such as gummy candies, candy, chocolate and gum, drinks such as juice and drinks. Is mentioned.

In this case, it is preferable that the amylase inhibitor is added in an amount of 0.001 to 100% by weight, particularly 0.01 to 30% by weight, based on the total amount of the food. As described above, the amylase inhibitor of the present invention has no problem in terms of taste, and therefore, when the composition for amylase inhibition of the present invention is used as a food, it is not necessary to mask the taste, It can be manufactured by a method of appropriately mixing it with the above-mentioned food during manufacturing.

[0025]

Industrial Applicability Since the amylase inhibitor of the present invention is obtained from cinnamon bark which has been widely used as a food, a herbal medicine, etc., there is no problem in safety for human body and its amylase inhibitory activity is high. Moreover, there is almost no bitterness or irritating odor peculiar to cinnamon bark. Therefore, the amylase-inhibiting composition containing the amylase inhibitor of the present invention as an active ingredient can be suitably used as a pharmaceutical product and a food without any special taste masking treatment.

[0026]

EXAMPLES The present invention will be specifically described below with reference to examples and comparative examples, but the present invention is not limited to the following examples.

[Example 1] 100 g of cinnamon powder (sold by: Uchida Wakan Yaku Co., Ltd.) was immersed in 500 ml of hexane,
After stirring at room temperature for 3 hours, hexane was removed by filtration. This operation was repeated twice to obtain a deoiled product.
This deoiled product is treated with a 50% by volume aqueous ethanol solution of 500 m.
It was immersed in 1 and extracted under boiling for 1 hour. This operation 2
Repeated times to collect the extract. The obtained extract was concentrated under reduced pressure at 60 ° C. by an evaporator and freeze-dried to obtain about 6 g of extract. The obtained extract was in powder form.

[Example 2] The extraction treatment was carried out in the same manner as in Example 1 except that 500 ml of 90% by volume ethanol aqueous solution was used in place of 500 ml of 50% by volume aqueous ethanol solution, and the obtained extract was frozen. After drying, about 4 g of extract was obtained. In addition, the obtained extract was lumpy.

[Example 3] 100 g of cinnamon powder (sold by: Uchida Wakan Yaku Co., Ltd.) in 50% by volume ethanol solution 500
Immerse in ml and extract under boiling for 1 hour. This operation was repeated twice to collect the extract. The obtained extract was concentrated under reduced pressure at 60 ° C with an evaporator and freeze-dried to obtain an extract. This extract was immersed in 100 ml of hexane, stirred at room temperature for 3 hours, and then hexane was removed by filtration. After repeating this operation twice, about 6 g of a dried and deoiled extract was obtained. The obtained extract was in powder form.

[Comparative Example 1] 100 g of cinnamon powder (sold by Uchida Wakan Yaku Co., Ltd.) in 50% by volume ethanol solution 500
Immerse in ml and extract under boiling for 1 hour. This operation was repeated twice to collect the extract. The obtained extract was concentrated under reduced pressure at 60 ° C. by an evaporator and freeze-dried to obtain about 7 g of extract.

[Comparative Example 2] Cinnamon powder (sold by: Uchida Wakhan Co., Ltd.) was used as it was.

[Comparative Example 3] An extract was obtained in the same manner as in Comparative Example 1 except that water was used instead of the 50% by volume aqueous ethanol solution in Comparative Example 1.

[Comparative Example 4] An extract was obtained in the same manner as in Comparative Example 1 except that ethanol was used in place of the 50% by volume aqueous ethanol solution in Comparative Example 1.

The extracts of Examples 1 to 3 and Comparative Examples 1 to 4 were dissolved in methanol to a concentration of 10 mg / ml and filtered to obtain α-amylase (derived from Bacillus subtilis, sold by:
Wako Pure Chemical Industries, Ltd.) The activity inhibition rate was measured by the following measuring method. Also, prepare a 0.1 wt% aqueous solution of each extract,
Sensory test of the taste of each aqueous solution with 5 panelists,
The evaluation was made (average value) according to the following taste evaluation criteria. Table 1 shows the results. Method for measuring α-amylase inhibitory activity 1) 0.5 wt% soluble starch, 20 mM CaCl ₂ , 1
50 mM acetate buffer (pH 6.
An appropriate amount of α-amylase enzyme solution (derived from Bacillus subtilis) and 20 μl of a sample are added to 5) to make the total amount 0.5 ml. (In ice bath) 2) Incubate at 37 ° C for 15 minutes to carry out reaction,
Immediately stop the reaction in an ice bath. 3) Iodine reagent (1 / 6000M iodine, 1 / 600M
Add 5 ml of potassium iodide and 1/600 M hydrochloric acid, and add 7
The absorbance at 00 nm is measured. As controls, those without enzyme (Control 1: OD ₇₀₀ = about 1.2) and those with further enzyme (Control 2: OD ₇₀₀ = about 0.2) are measured at the same time. 4) The suppression rate is calculated from the following formula. Inhibition rate (%) = (Sample-Control 2) / (Control 1-Control 2)
× 100 Evaluation criteria of taste ○: Almost no bitterness or irritating odor peculiar to cinnamon is felt Δ: Bitterness or irritating odor peculiar to cinnamon is weak ×: Strong bitterness or irritating odor peculiar to cinnamon is strongly felt

[0035]

[Table 1]

According to Table 1, the amylase inhibitor (extract) of the present invention has a high amylase inhibitory activity and does not have the bitterness or pungent odor characteristic of cinnamon bark, while the taste is improved. As such (Comparative Example 2), when only water or ethanol extraction treatment was carried out (Comparative Examples 3 and 4), the amylase inhibitory activity was low, and there was bitterness and irritating odor characteristic of cinnamon bark,
When the oil removal treatment is not performed (Comparative Example 1), the amylase inhibitory activity is high, but it is recognized that the cinnamon bark has a bitter taste and an irritating odor.

Next, animal (SD rat, male, 4 weeks old)
6 groups per group, 2% of the extract obtained in the above Example 1 was mixed in the feed, and the group fed for 2 weeks was used as the cinnamon group, and the group fed in the same manner with the feed containing no extract was used as the control group. . Then, the feed efficiency obtained from the weight gain and the feed intake of the animals in each group after being raised for 2 weeks was obtained by the following formula, and the fat percentage was obtained from the body weight of the animals in each group and the epididymal adipose tissue weight. . Table 2 shows the results. Feed efficiency (%) = weight gain (g) ÷ feed intake (g)
× 100

[0038]

[Table 2]

Further, the extract obtained in the above Example 1 was
3 female panelists (A, B, C) 3 times a day (315m
g / day) Taken before meals. This was carried out for 30 days, and the change in body weight during that period was measured. The results are shown in FIG.

[Example 4] Extract 3 obtained in Example 2
Disperse and dissolve 50 mg in 250 ml of boiling water, add 6.0 g of coffee powder and 5.0 g of erythritol, and finally add 5.0 g of gelatin, and store in refrigeration to obtain coffee jelly (composition for amylase inhibition). It was

[Example 5] Extract 3 obtained in Example 1
00 mg and flour 120 g, erythritol 10 g, shortening 15 g, whole egg powder 0.5 g, salt 1 g, sodium hydrogen carbonate 0.6 g, ammonium carbonate 0.75 g
Using 20 g of water and 20 g of water, a dough was prepared by a conventional method, molded and roasted to produce a biscuit (composition for amylase inhibition).

The amylase-inhibiting compositions of Examples 4 and 5 were subjected to a sensory test of the taste of each composition by 5 panelists, and evaluated according to the above-mentioned taste evaluation criteria. Table 3 shows the results
Shown in

[0043]

[Table 3]

According to Table 3, it is recognized that the composition for amylase inhibition of the present invention has no problem in the taste even if the taste of the amylase inhibitor itself has a great influence on eating and drinking. .

[Brief description of drawings]

FIG. 1 is a graph showing changes in body weight when the amylase inhibitor of the present invention obtained in Example 1 was taken.

 ─────────────────────────────────────────────────── ─── Continuation of front page (72) Inventor Sonoko Miyamoto 1-3-7, Sumida-ku, Tokyo Lion Corporation (72) Inventor Hideaki Ozeki 1-3-7, Sumida-ku, Tokyo Within Lion Corporation

Claims (2)

[Claims] 1. An amylase inhibitor, which comprises a deoiled cinnamon and an extract treated with an aqueous ethanol solution as active ingredients. 2. A composition for amylase inhibition, which is used as a medicine or food, and which contains the amylase inhibitor according to claim 1 as an active ingredient.