JPH10158180A - Antiobestic agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antiobestic agent having both α-amylase antagonism and lipase antagonism activities, without affecting other nutrient components and causing small side effects by including an extract of a fruit of Diospyros kaki as an active ingredient. SOLUTION: This an antiobestic agent includes an extract of a fruit of Diospyros kaki obtained, for example, by using the fruit of the Diospyros kaki, especially astringent persimmon and its unripe fruit, fermenting the fruit of the Diospyros kaki by using a yeast such as the yeast belonging to genus saccharomyces, optionally adding dextrin to the fermented material and further performing an operation such as filtering, centrifugation and concentration. The extract is used as it is, or by diluting by a suitable solvent, concentrating, or forming into a powder form by drying with a suitable carrier or by other methods.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to an antiobesity agent, an α-amylase inhibitor, a lipase inhibitor and a food. More specifically, the present invention relates to an anti-obesity agent, an α-amylase inhibitor, a lipase inhibitor and a food for treating or preventing obesity by suppressing or inhibiting digestion and absorption of carbohydrates and lipids serving as energy sources in the body.

[0002]

2. Description of the Related Art

[0007] Obesity is not only a cosmetic risk, but also causes many diseases such as adult diseases. Diet therapy, exercise therapy, pharmacotherapy and the like have been proposed or implemented as the treatment and prevention methods. However, both therapies may impose physical and mental distress on the patient, such as malnutrition disorder, motor dysfunction, side effects, hunger or stress, and it is not only difficult to maintain the effect, but rather impair health. In many cases,
The choice of treatment and prevention is an important issue.

[0003] As a method of treating and preventing obesity, surplus energy is removed in a daily manner while taking a normal dietary form without imposing physical and mental distress, and nutrient components other than energy sources are removed. A method that eliminates as few defects as possible is desired. Energy sources in food include sugars such as starch, fats, fatty acids, glycerides, glycerol,
Most lipids such as cholesterol are expected to be used to treat or prevent obesity if their digestion and absorption are suppressed or inhibited. As an example, a method using a food having a function of inhibiting digestion and absorption of lipids (Japanese Patent Laid-Open No.
No. 28664), a method of inhibiting the activity of α-amylase by tea polyphenol (Japanese Patent Application Laid-Open (JP-A) No. 3-133928).
Japanese Patent Application Laid-Open No. 5-255100), and a method for inhibiting the activity of lipase by extracts such as Dokkatsu, Ryokyo, Acacia biloba, Spruce, Sampens, and Betula edulis.

[0004] α-amylase is a carbohydrate digestive enzyme,
In humans, it is secreted from salivary glands, parotid glands, and pancreas.
α-Amylase inhibitors are thought to be effective in treating and preventing obesity as well as in treating and preventing diabetes.

[0005] Lipase is a digestive enzyme for lipids, which is secreted from the pancreas in humans, and Candida cylindracc.
It is produced by microorganisms resident on the skin surface represented by ae. Lipase inhibitors are used to treat and prevent obesity,
It is also thought to be effective in treating and preventing hyperlipidemia, arteriosclerosis, acne, and dermatitis.

Therefore, a prophylactic / therapeutic agent which has both an α-amylase inhibitory action and a lipase inhibitory action, does not affect other nutritional components, and has few side effects is desired.

[0007]

Means for Solving the Problems The present inventors have conducted studies in view of the above circumstances. As a result, the extract of persimmon fruit inhibits digestion and absorption of carbohydrates and lipids, and inhibits α-amylase and lipase. Thus, the present invention has been completed.

That is, the present invention relates to an anti-obesity agent containing an extract of persimmon fruit as an active ingredient.

[0009] The present invention also relates to an α-amylase inhibitor comprising an extract of persimmon fruit as an active ingredient.

[0010] The present invention further relates to a lipase inhibitor comprising an extract of persimmon fruit as an active ingredient.

Further, the present invention relates to a food product to which an extract of persimmon fruit is added.

The persimmon fruit used in the present invention is a persimmon oyster fruit. One of its components, persimmon tannin, is used as a food additive to remove cloudiness in sake, and as a folk medicine for hypertension, burns, and soybeans. It is used for
However, it is not known that an extract of persimmon fruit has an anti-obesity effect.

As the persimmon fruit used in the present invention, any of sweet persimmon, astringent persimmon, and immature fruits thereof can be used. Among them, astringent persimmon and its immature fruits are preferably used.

The extract of persimmon fruit of the present invention is obtained by fermentation with yeast, or an extract obtained by extraction with a polar or non-polar solvent, a diluent, a concentrate, an extract or a dried product thereof. means. As the yeast, wild yeast and Saccharomyces yeast are used, and among them, Saccharomyces yeast having tannin resistance is preferable. As the extraction solvent, for example, methanol, ethanol, 1-
Propanol, 2-propanol, 1-butanol, 2
-Alcohols such as butanol, ethers, ethers such as tetrahydrofuran, esters such as ethyl acetate,
Ketones such as acetone, nitriles such as acetonitrile, aromatic hydrocarbons such as benzene and toluene, halogenated aliphatic hydrocarbons such as methylene chloride and chloroform, and water can be appropriately selected and used. From the viewpoint of safety in use after extraction, operation and handling, alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol and 2-butanol, and water are preferred. In the present invention, a commercially available extract can also be used. For example, a persimmon fruit extract (trade name:
Astrin, manufactured by Miyoshi Kashichi Shoten Co., Ltd.) and the like.

[0015]

BEST MODE FOR CARRYING OUT THE INVENTION The extract of the present invention is obtained by, for example, squeezing a persimmon fruit, adding yeast, and fermenting the resulting fermented product. If necessary, adding dextrin, filtration, centrifugation, concentration, etc. Operation can be performed. In the case of extraction with a solvent, the persimmon fruit is squeezed, and a 2- to 200-fold amount of a polar or non-polar solvent is added thereto.
Extraction is performed by stirring, standing and / or homogenizing for a time. After the extraction, operations such as filtration and centrifugation are performed to remove insolubles, and if necessary, dilution, filtration, and concentration operations are performed to obtain a target extract. if needed,
The removed insolubles can be extracted by the same operation as described above, and the extracted liquid can be used.

The extract of the present invention can be used as it is, but can also be diluted or concentrated with a suitable solvent, and can be used alone or together with a suitable carrier in spray drying, freeze drying, reduced pressure drying, fluid drying, etc. It can be used in the form of a powder by a known method or in the form of a liquid, tablet or granule by using a conventional additive. The extract of the present invention thus formulated can be used as a drug such as an anti-obesity agent, an α-amylase inhibitor, a lipase inhibitor or the like, or can be used by adding it to various foods.

[0017]

The antiobesity agent of the present invention has a strong carbohydrate and lipid absorption inhibitory effect and is useful for treating and preventing obesity. In addition, the antiobesity agent of the present invention has a stronger inhibitory effect on carbohydrate and lipid absorption than green tea, but has a weaker protein absorption inhibitory effect than green tea. It is possible to treat and prevent obesity safely without inhibition. Furthermore, the antiobesity agent of the present invention has high resistance to the first solution (artificial gastric juice) in the Japanese Pharmacopoeia General Test Disintegration Test Method, and has a strong inhibitory effect on carbohydrate and lipid absorption without causing a decrease in efficacy due to gastric juice. Show.

The α-amylase inhibitor of the present invention is useful for treating and preventing obesity and for treating and preventing diabetes caused by α-amylase.

Further, the lipase inhibitor of the present invention is useful for treating and preventing obesity and for treating and preventing hyperlipidemia, arteriosclerosis, acne and dermatitis caused by lipase.

[0020]

EXAMPLES The present invention will be described in more detail with reference to the following Examples, but it should not be construed that the present invention is limited thereto. The starch digestion test, fat digestion test, and protein digestion test listed below measure the degree of digestion and absorption of carbohydrates, lipids, and proteins, respectively, and in particular, pancreatin, an enzyme that digests carbohydrates, It measures the degree of inhibition of the enzyme activities of enzymes that digest lipids and enzymes that digest proteins. Also,
The α-amylase inhibition test and the lipase inhibition test measure the degree of inhibition of the enzyme activities of α-amylase and lipase, respectively.

<Preparation of Sample Solution> A persimmon fruit extract (Astrin: manufactured by Mimasa Kachichi Shoten Co., Ltd.) was used as a persimmon fruit extract, and a wheat extract extract (wheat extract-α: Tama Biochemical) was used as a comparative sample. Co., Ltd.) and green tea extract (Polyphenon-60S: manufactured by Mitsui Norin Co., Ltd.).

1. Preparation of sample solution without artificial gastric juice treatment Purified water was added to each extract at an arbitrary ratio to obtain a sample solution.

2. Preparation of Sample Solution Treated with Artificial Gastric Fluid 0.1 g of the extract was mixed with 50 ml of the first solution described in the General Test Method Disintegration Test Method of the 13th Revised Japanese Pharmacopoeia (Hirokawa Shoten)
After stirring at 37 ° C. for 1 hour, the pH was adjusted to 7.0 by adding a 1N aqueous sodium hydroxide solution, and water was added to adjust the total amount to 10%.
0 ml was used as a sample solution.

Using these sample solutions, Examples 1 to 7
The tests shown in Table 1 were performed.

Example 1 <Starch Digestion Test> 9 ml of a sample solution and an enzyme solution (4.
5-fold pancreatin 0.1 mg / ml: manufactured by Amano Pharmaceutical Co., Ltd.)
1 ml was added to the test tube, mixed well, left at 37 ° C. for 10 minutes, and then 1% potato starch solution (pH 7.0)
10 ml was added and shaken immediately. This solution is added at 37 ° C for 10
After standing for 1 minute, 1 ml of this solution was poured into 10 ml of 0.1N hydrochloric acid to stop the reaction. 1 ml of this solution is colored (0.000
4N iodine test solution) 10 ml, shake and mix.
The absorbance AT at 60 nm was measured. Separately, water was used instead of the sample solution as a control, and water was used as a blank instead of the sample solution and the enzyme solution, and the absorbances AS and AB were measured in the same manner.

Example 2 <Fat Digestion Test> 1 ml of sample solution, buffer solution (125 mM T
2 ml of ris-HCl, pH 7.4 and enzyme solution (4.
5-fold pancreatin 0.5 mg / ml: manufactured by Amano Pharmaceutical Co., Ltd.)
1 ml was added to the test tube, mixed well, and allowed to stand at 37 ° C. for 10 minutes. Then, 1 ml of 2% soybean oil (emulsified in an aqueous solution of 0.5% gum arabic) was added, and the mixture was immediately shaken. After leaving this solution at 37 ° C. for 10 minutes, 10 ml of chloroform was added and stirred for 5 minutes to stop the reaction. The chloroform layer was separated, and the same amount of a colored liquid (3.2 g of copper (II) nitrate trihydrate, 6.7 g of triethanolamine, and 0.3 g of acetic acid dissolved in purified water to make a total volume of 100 ml). ) Was added and stirred for 5 minutes. The chloroform layer was separated, and the same amount of the color developing solution (0.
After adding 1% sodium diethyldithiocarbamate in 1-butanol) and stirring, the absorbance AT at a wavelength of 440 nm was measured. Separately, water was used instead of the sample solution as a control, and water was used as a blank, instead of the sample solution and the enzyme solution.
And AB were measured.

Example 3 <Protein digestion test> 4 ml of a sample solution and 1 ml of an enzyme solution (4.5 times pancreatin 0.5 mg / ml: manufactured by Amano Pharmaceutical Co., Ltd.) were added to a test tube and mixed well. At 10 ° C. for 10 minutes, and then a 0.6% milk casein solution (p
H8.0) was added and shaken immediately. 37
After leaving at 10 ° C for 10 minutes, 0.11M trichloroacetic acid solution
The reaction was terminated by adding 10 ml and stirring at 37 ° C. for 10 minutes, followed by filtration. To 2 ml of the filtrate, 5 ml of a 0.55 M sodium carbonate test solution and 1 ml of a coloring solution (3-fold diluted folin solution) were added.
Immediately after shaking and standing at 37 ° C. for 30 minutes, the absorbance AT at a wavelength of 660 nm was measured. Separately, water was used instead of the sample solution as a control and the absorbance AS was measured in the same manner, and water was used instead of the sample solution and the enzyme solution as a blank, and the enzyme solution was added when the reaction was stopped. AB was measured.

Example 4 <α-amylase inhibition test 1> In Example 1, 4 units / ml of α-amylase derived from human saliva (manufactured by Sigma: 1 unit is 1 mg / 3 min from starch at 20 ° C and pH 6.9) as an enzyme solution. The amount of the enzyme that releases maltose) was measured in the same manner as in Example 1 except that the absorbance AT,
AS and AB were measured.

Example 5 <α-Amylase Inhibition Test 2> In Example 1, 4 units / ml of porcine pancreatic juice-derived α-amylase (Sigma: 1 unit: 1 mg / min from starch at 20 ° C., pH 6.9) was used as the enzyme solution. The amount of the enzyme that releases maltose) was measured in the same manner as in Example 1 except that the absorbance AT,
AS and AB were measured.

Example 6 <Lipase inhibition test 1> In Example 2, 200 units / ml of lipase derived from porcine pancreatic juice (manufactured by Sigma:
Absorbances AT, AS and AB were measured in the same manner as in Example 2 except that 1 unit used an enzyme amount which releases 1 μmole / hr of fatty acid from emulsified olive oil at 37 ° C. and pH 7.8.

Example 7 <Lipase inhibition test 2> In Example 2, 0.07 units of Candida cylindraccae-derived lipase was used as the enzyme solution.
ml (manufactured by Walsington Biochemical: 1 unit is 25
1 μmole / m from emulsified olive oil at ℃, pH 8.0
The absorbances AT, AS and AB were measured in the same manner as in Example 2 except that the amount of the enzyme that liberated the fatty acid in was used.

The inhibition rate was calculated from the measurement results of each example using the following formula, and a logarithmic plot was plotted against the concentration of the sample to obtain I.
C50 (weight of the extract required to inhibit the enzyme activity by 50%) was determined.

[0033]

(Equation 1)

The test results are shown in Tables 1 and 2.

[0035]

[Table 1]

[0036]

[Table 2]

[0037]

As is clear from Tables 1 and 2, the extract of the present invention strongly inhibits the digestion and absorption of carbohydrates and lipids in artificial gastric juice without losing its efficacy. Since it does not inhibit digestion and absorption, it hardly affects nutritional components other than energy sources, and is useful as an agent for treating and preventing obesity. In addition, it has an α-amylase inhibitory action and a lipase inhibitory action, and is therefore useful for treating and preventing not only obesity but also diabetes, hyperlipidemia, arteriosclerosis, acne, dermatitis and the like.

Claims (6)

[Claims] 1. An anti-obesity agent comprising an extract of persimmon fruit as an active ingredient. 2. The anti-obesity agent according to claim 1, wherein the anti-obesity effect is based on an α-amylase inhibitory effect. 3. The anti-obesity agent according to claim 1, wherein the anti-obesity effect is based on a lipase inhibitory effect. 4. An α-amylase inhibitor comprising an extract of persimmon fruit as an active ingredient. 5. A lipase inhibitor comprising an extract of persimmon fruit as an active ingredient. 6. A food product comprising an extract of persimmon fruit.