JPH1180014A - Hypoglycemic agent containing agaricus blazei extract as active ingredient - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare a hypoglycemic agent, useful as an antidiabetic agent, a health food or the like, capable of being orally, safely and effectively administered by including an extract of Agaricus blazei as an active ingredient. SOLUTION: This hypoglycemic agent contains an extract of Agaricus blazei, preferably in an amount of >=30 wt.% of the total amount as an active ingredient. The extract is preferably the one obtained by drying a basidiocarp and/or a mycelium of the Agaricus blazei, and extracting the dried basidiocarp and/or the mycelium with a mixed solvent of water and a primary alcohol such as ethanol, or the mixed solvent of the water and a ketone such as acetone. The daily dose is preferably 2-10 g, e.g. 9 g (3 g×3 times/day).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a hypoglycemic agent containing Agaricus blazei extract as an active ingredient. More specifically, the present invention relates to a hypoglycemic agent containing, as an active ingredient, Agaricus blazei extract, which is suitably used for oral diabetes drugs and health foods.

Heretofore, the treatment of diabetes has mainly been replacement therapy using an insulin preparation, and this method has drawbacks that the preparation is a protein and cannot be used other than for injection, and its duration is short. Furthermore, it has been pointed out that the efficacy is lowered due to the accumulation of antibodies, and the emergence of an insulin substitute by oral administration has been desired. From such a viewpoint, drugs and the like containing a biguanide compound or a sulfonylurea compound as a main component have been developed so far. However, these drugs have not surpassed insulin and have not been able to replace them. Therefore, at present, the emergence of a safe and effective diabetic drug suitable for oral administration is expected.

[0003]

DISCLOSURE OF THE INVENTION The present invention has been made in view of the above-mentioned problems, and is a hypoglycemic agent which can be safely and effectively taken orally and which is preferably used for a diabetic drug or a health food. The purpose is to provide.

[0004]

SUMMARY OF THE INVENTION The present invention has been made to achieve the above object, and has the following gist. [1] A hypoglycemic agent containing Agaricus blazei extract as an active ingredient. [2] The above-mentioned [1], wherein the Agaricus blazei extract is an extract of a fruiting body and / or mycelium of Agaricus blazei using a mixed solution of water and a primary alcohol or water and a ketone. Hypoglycemic agent.

[0005]

DESCRIPTION OF THE PREFERRED EMBODIMENTS Embodiments of the present invention will be specifically described below. The hypoglycemic agent of the present invention contains Agaricus blazei extract as an active ingredient. The Agaricus blazei extract is preferably an extract of the fruiting body and / or mycelium of Agaricus blazei, using a mixed solution of water and a primary alcohol or water and a ketone.

[0006] 1. Agaricus blazei extract Agaricus blazei used in the present invention is a kind of mushroom in Brazil, and its extract has recently attracted attention as a folk medicine for immunotherapy of cancer and the like. The extraction method of Agaricus blazei extract is not particularly limited, for example, after drying the fruiting body and / or mycelium of Agaricus blazei obtained by solid culture or liquid culture, water and primary alcohol, or It is preferable to perform extraction using a mixed solution of water and a lower ketone. Here, as the primary alcohol, for example, ethyl alcohol or methyl alcohol, and as the lower ketone,
For example, acetone can be mentioned. In particular,
After hot water extraction, it is more preferable to extract the residue with 40% ethanol, mix with the hot water extract, and concentrate under reduced pressure. The residue is dried as it is or by a freeze-drying method or the like to form a powder into a desired dosage form. However, it can be obtained by a method other than the above, and such an extract can also be effectively used for the hypoglycemic agent of the present invention.

[0007] 2. Content of Active Ingredient The content of the active ingredient in the hypoglycemic agent of the Agaricus blazei extract used in the present invention is preferably at least 25% by weight, more preferably at least 30% by weight of the total amount of the hypoglycemic agent.

[0008] 3. Other Components In addition to the Agaricus blazei extract, the hypoglycemic agent of the present invention can contain, for example, shiitake mushroom extract, reishi extract, and the like. Its content is, for example, Agaricus blazei extract 45%, Shiitake mushroom extract 35
%, Reishi Extract 20%. The hypoglycemic agent containing an Agaricus blazei (fruit body and mycelium) extract of the present invention as an active ingredient shows excellent antidiabetic activity upon oral administration and has no toxicity. It is preferably used.

[0009]

EXAMPLES The present invention will be described more specifically with reference to the following examples. [Example 1] Dried Agaricus blazei fruit body 50
g, heated for 1 hour, filtered through a 200-mesh sieve, and added 40% ethanol 250m to the residue.
The mixture was extracted with heating under reflux and filtered through a 200-mesh sieve. It was combined with the first hot water extract and concentrated under reduced pressure of 100 to 200 mmHg at 40 to 50 ° C to obtain 70 ml of a liquid extract. This was vacuum-dried until the water content became 5% by weight or less to obtain 22.5 g of a powder extract. The yield based on the dried mushroom fruit body was 45%.

Example 2 Extraction was carried out in the same manner as in Example 1 except that mycelium was used in place of the dried mushroom fruit body, thereby obtaining 10.0 g of an extract with a yield of 20%.

Example 3 22.0 g of a liquid extract was obtained in substantially the same manner as in Example 1 except that acetone was used instead of ethanol.

Example 4 8.5 g of a liquid extract was obtained in substantially the same manner as in Example 2 except that acetone was used in place of ethanol.

The pharmacological tests (antidiabetic action test and acute toxicity test) of the Agaricus blazei fruit body and mycelium extract obtained according to the above Examples were carried out. 1) Antidiabetic action test In this test, Agaricus
Brassica fruiting body extract and mycelium extract powder were used as test substances, respectively. Alloxan diabetic rats are divided into three groups, one group is provided with 200 mg / kg / day of fruiting body extract, and the other group is provided with 200 mg / kg / day of mycelium extract continuously for 1
Five doses were administered, and blood was collected every 5 days to measure the blood sugar level. On the other hand, untreated animals served as control groups for the three groups. As a result, 15
After day, the blood glucose level of the control group was 440 ± 25 mg / dl, while the blood glucose level of the administration group was 212 ± 25 in the fruiting body extract group.
mg / dl, 188 ± 15 mg / dl in mycelium extract group
And a decrease in blood glucose levels. Next, a sugar tolerance test was performed.
That is, alloxan diabetic rats and healthy rats were fasted overnight, and then 2 g / kg of glucose was orally administered to measure the blood glucose level. Then, the increase in blood sugar level in healthy rats was 20 to 30 mg / dl, whereas the increase in blood sugar level in alloxan diabetic rats reached 200 mg / dl. Next, 200 mg / kg of each of the fruiting body extract and the mycelium extract was administered in advance, and the above-mentioned load test was performed. dl. This suggests that the fruiting body extract and mycelium extract of Agaricus blazei used in the present invention have not only a blood glucose lowering effect but also a pancreatic function enhancing effect. Furthermore, the anti-diabetic effects of the fruiting body extract and mycelium extract of Agaricus blazei of the present invention were tested. One month after the alloxan injection, the fruiting body extract and mycelium extract powder were added to alloxan diabetic rats for 2 minutes each.
00 mg / kg / day was administered for 3 weeks, and the blood sugar level was measured every week. Blood glucose began to drop gradually from the second week and dropped sharply at the third week. (The blood glucose level of the administration group at the third week was 298 ± 25 mg / dl with fruiting body extract,
(275 ± 12 mg / dl with mycelium extract, blood sugar level of control group is 388 mg / dl) A glucose tolerance test was carried out in the same manner as described above. It was confirmed that both the Agaricus blazei fruit body and the mycelium extract obtained had a therapeutic effect on alloxan diabetes.

2) Acute toxicity test The acute toxicity of Agaricus blazei fruit body and mycelium extract used in the present invention was determined using 5-week-old ddY-N mice (22-26 g male, 20-24 g female). Tested. 20 g of each of the fruiting body and mycelium extract powders was suspended in distilled water to prepare a 20% by weight suspension, which was used as a test solution. Five groups of 10 males and females were prepared, and the animals in each group were given 4,800 mg / kg and 5,800 mg / k.
g, 6,900 mg / kg, 8,300 mg / kg, and 10,000 mg / kg were orally administered with the test substance via a gastric probe. The 50% lethal dose (liter D50) calculated based on the probit method was 7,662 mg / kg for males and 7,352 mg / kg for females in the fruiting body extract group (95% confidence limits were 7,110 to 8, respectively). , 21
4 and 6,754-8,011). In the mycelium extract group, 7,358 mg / kg for males and 7,248 mg / kg for females
kg (95% confidence limits were 6,798-
7,918 and 6,578-7,918). The results of the above pharmacological tests show that Agaricus blazei fruiting bodies and mycelium extracts used in the present invention are effective for oral administration of diabetes. Accordingly, the hypoglycemic agent containing the Agaricus blazei fruit body of the present invention and a mycelium extract as an active ingredient are generally used in the form of tablets or capsules together with a pharmaceutical carrier or excipient suitable for oral administration. Served for use. Granules, tablets or capsules for oral administration may be in unit dosage form and combined with, for example, syrups, acacia, gelatin,
Sorbitol tragacanth or polyvinylpyrrolidone, excipients such as lactose, dextrin, corn starch,
It may contain conventional excipients such as calcium phosphate, sorbite or glycine, talc, polyethylene glycol or silica, disintegrants such as starch, acceptable wetting agents such as sodium lauryl sulfate. Oral liquid preparations may be aqueous or oily suspensions, solutions, syrups, elixirs and the like. Such liquid preparations may contain commonly used additives, suspending agents such as sorbit syrup and methylcellulose, emulsifiers such as lecithin and sorbitan monooleate, and the like. Alternatively, it can be used as a dry preparation, which is redissolved in water or a suitable medium at the time of use.

[Formulation Example 1] Ingredient Content (g) Agaricus blazei fruiting body extract 30 Dextrin 50 DK ester 10 Crystalline cellulose 10 These ingredients are sufficiently mixed to form a uniform composition into kneaded granules according to a conventional method. Molded. Next, the granules were processed into a tablet using a tableting machine.

Formulation Example 2 Ingredient Content (g) Agaricus blazei mycelium extract 25 Dextrin 65 Lactose 10 The above ingredients were thoroughly mixed and homogenized. This mixed powder 2
g into a stick pack and sealed.
It was dissolved in 80 ml to prepare a dry preparation for oral administration. The dose of the hypoglycemic agent containing the Agaricus blazei fruit body and mycelium extract of the present invention as an active ingredient is 2 g to 1 g per day.
0 g, for example, 9 g (3 g × 3
Times / day) is preferred.

[0017]

As described above, according to the present invention,
It is possible to provide a hypoglycemic agent which can be taken orally safely and effectively, and which is suitably used for diabetes drugs and health foods.

Claims (2)

[Claims] 1. A hypoglycemic agent containing Agaricus blazei extract as an active ingredient. 2. The Agaricus blazei extract is an extract of Agaricus blazei fruit body and / or mycelium extracted from a mixed solution of water and primary alcohol or water and ketone. The hypoglycemic agent according to the above.