JPS60181026A - Polysaccharide - Google Patents

Abstract

NEW MATERIAL:A polysaccharide [specific rotatory powder [alpha]<25>D=3, 4 deg. (C 0.5, water); decomposition temperature: about 360 deg.C; infrared absorption spectrum (KBr method) numax: 3325, 1610, 1050 (broad) and 550cm<-1>; no specific absorption is observed in ultraviolet light part; nuclear magnetic resonance spectrum: table 1; pH: pH of aqueous solution is 6.72]. USE:A drug composition for a blood sugar lowering agent, etc. PREPARATION:A fruit body of a bracket fungus of the genus Fomes is sufficiently dried, ground, its surface area is enlarged, and extracted with water or an aqueous organic solvent. When it is extracted with water, it is thermally extracted under boiling. The prepared extracted solution is filtered or decanted to remove components insoluble in hot water, it is concentrated under reduced pressure at room temperature -60 deg.C, to give an extract. The extract is dissolved in water, and a lower alcohol is dropped in it. The prepared precipitate is filtered off, and washed with the alcohol. The precipitate is evaporated to dryness under reduced pressure -60 deg.C, to give a powdery polysaccharide.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to medicinal components of Reishi, particularly polysaccharides having hypoglycemic effects, methods for producing the same, and pharmaceutical compositions thereof, particularly hypoglycemic agents.

Reishi (W Shiba), which is used as a raw material, is classified as Basidiomycota, Basidiomycota subclass, ***, It is a mushroom that belongs to the order Polygonaceae and the family Arunocycodae, such as stonecrop (Ganoderma lucidum, karst), stonecrop (Ganoderma neoyabonicum, imazeki), stonecrop (Ganoderma tsugae maril), and stonecrop (Ganoderma secile).

Examples include Marirun, Ganoderma curteisi, Berg. Currently, in Japan, the mantis mushroom is produced through artificial cultivation and is a type of mushroom that is relatively easily available.

In particular, it is widely known that Cinnamon mushroom is used as an effective drug for chronic bronchitis, coronary insufficiency, hyperlipidemia, hypertension, neurasthenia, hepatitis, and the like.
However, the active ingredients of reishi have not been disclosed.

The inventors of this invention conducted research on the isolation and medicinal effects of medicinal components of Reishi, and as a result, they discovered poly*i, which has a particularly hypoglycemic effect, and came up with this invention.

Thus, this invention has the following physical properties: Amount) has a hypoglycemic effect, j) Specific optical rotation 2 (&)"6'= + 3.4' (C
0.51 water), vagina) decomposition temperature: approximately 360°C, Iv) infrared absorption spectrum (KBr method) Vmax:
3325.1610.1050 (broad) and 55
Q am'-', ■> Vυ nuclear magnetic resonance spectrum (90 MHz DtO') with no specific absorption in the ultraviolet region
:s, 'ax(s), 4.50~5.09 axis), 4
．． 18(''), 3.28-3.89(s), 1.83
(S), 1.50s) and 1.15 (t, J =
7,13), vi) pH+The pH of the aqueous solution is to provide a polysaccharide characterized by having a pH of 6.72. This polysaccharide is isolated as follows.

It is preferable to use the fruiting body of the Ganoderma as a raw material, and it is preferable to use the dried product rather than the fresh one.Reishi is usually artificially cultivated from pure cultured mycelia from natural products. Although the type is not limited, the yield of the polysaccharide of the present invention may vary depending on the type.

The polylI compound of the present invention can be produced, for example, by the following procedure.

The collected Ganoderma fruiting body is sufficiently dried and crushed into small pieces using a crusher or the like to increase its surface area and increase extraction efficiency.

Next, the crushed fruit bodies are extracted with water or an aqueous organic solvent without being defatted or after defatting using a conventional fat-soluble organic solvent. Extraction can be carried out sufficiently with water, but an aqueous organic solvent may be used to prevent spoilage of the extract and to accelerate the extraction. Alternatively, extraction may be performed with both. Examples of organic solvents for the aqueous organic solvent include methanol, Lower alcohols such as ethanol and water-soluble organic solvents such as acetone are used, and the concentration ranges from as low as about 1% to about 30% depending on the type of raw material.
A concentration of Moreover, these extractions are accelerated by heating.

When extracting with water, it is usually heated under boiling.

The amount of water used is usually 5 to 30 times the weight of the fruiting body, and it is appropriate to perform extraction about 2 to 3 times. Extraction performed under boiling is performed for about 2 to 5 hours each time, and the extraction time and number of extractions are selected as appropriate. Moreover, this water extraction can be performed at room temperature.

The extract obtained as above is filtered or decanted to remove hot water insoluble matter, and then concentrated under reduced pressure at room temperature to 60°C or evaporated to dryness to obtain liquid or powder extract (A). It will be done.

Approximately 10-30% of the extract-A) obtained as above
It is dissolved in twice the amount of water, and about 4 to 6 times the amount of lower alcohol is added dropwise to the solution while stirring. Examples of lower alcohols include methanol and ethanol, but ethanol is preferred. Next, this liquid is allowed to stand, and the formed precipitate is collected by filtration and washed with the above-mentioned lower alcohol. The polysaccharide (B) of the present invention is obtained as a powder by evaporating this precipitate to dryness under reduced pressure at room temperature to 60°C, preferably 50 to 60°C.

Also, dissolve the above extract (A) in about 3 to 5 times the amount of water,
The aqueous solution is used as the inner solution and water is used as the outer solution. Dialysis is performed using, for example, Visklng Tube 36/32 (cellulose dialysis tube manufactured by Visklng, which passes through particles with a size of 24 angstroms or less), and the resulting inner solution is depressurized. The polysaccharide (B) of the present invention can also be obtained by evaporation to dryness at room temperature to 60°C.

The thus obtained polysaccharide of the present invention has the following properties.

I) Has a hypoglycemic effect, 1i) Specific optical rotation 2 [α)^=+3.4° (co, 5.
water), 11i) Decomposition temperature: approximately 360°C, lv) Infrared absorption spectrum (KBt method) 'Vmax
:3325.1610.1050 (broad) and 5
50 (to) -1, ■) No specific absorption in the ultraviolet region, vi) Nuclear magnetic resonance spectrum (90MHz DzO)
+5.3Hs), 4.50-5.09(m), 4
．． 18(s), 3.28-3.89(m), 1.83
(1) , 1.51 (s) and 1.15 (t, J
=7,13), vM) pi(=The pH of the aqueous solution is 6.
It is 72.

Thus, the present invention provides a hypoglycemic agent containing the polysaccharide of the present invention as an active ingredient, which is effective in treating symptoms such as diabetes.

The dosage of the medicinal ingredient of Reishi in this invention varies depending on the severity of the symptoms and the weight of the person to whom it is administered, but in the case of oral administration to adults, it is usually 50 to 50 per dose.
0 ■, preferably 100 to 250 ■, administered 2 to 3 times a day.

The drug according to the present invention is composed of the medicinal ingredient of Ganoderma alone or the medicinal ingredient of Reishi of the invention and a solid or liquid excipient.

The administration methods and dosage forms are usually powders, tablets, emulsions, capsules, drugs, granules, and liquids (alcoholic agents,
There are oral forms such as liquid extract, syrup, etc.). It may also be in a form injected into the body, such as an intravenous drip. As solid or liquid excipients used herein, those known in the art are used.

However, it is desirable to formulate the drug so that it contains the medicinal ingredients of the present invention necessary for one dose as described above.

To name a few specific examples, excipients in the powder for internal use (II) include lactose, starch, carboxymethyl cellulose or its alkali metal salts, dextrin, calcium phosphate, calcium carbonate, synthetic and natural aluminum silicate. , magnesium oxide, dried aluminum hydroxide, magnesium stearate, sodium bicarbonate, dried yeast, and the like.

Excipients in liquid preparations include water, simple syrup, ethanol, and the like.

Other disintegrants, flavoring agents, sweeteners used in the field,
A coloring agent or the like may be added as appropriate.

Although the water extract of Reishi is used as a health food, the hypoglycemic substance of the present invention can be used as a health food in an amount that does not exhibit a medicinal therapeutic effect and is sufficient to maintain health. As the projection, liquids, capsules, soft capsules, granules, drugs, etc. are suitable.

Next, the invention will be explained by examples and animal experiments.

Thoroughly dry the fruiting bodies of properly matured stone mushrooms, wash approximately 10 kg of them with cold water, drain thoroughly, dry, and then dry.
Approximately 10
Add 01 deionized water and extract under boiling for about 3 hours.

Repeat this extraction t3 times. Combine the obtained extracts and add 50 to 6
The brown powder extract (A) of 0.6 to 9 was obtained by evaporation drying under reduced pressure at a temperature of 0°C.
o Dissolve in deionized water, suction filter the solution to remove insoluble matter, and add 98% ethanol 101 to the filtrate with stirring.
After the mixture was left to stand overnight, the resulting precipitate was collected by filtration and evaporated to dryness under reduced pressure at 0° C. to obtain polysaccharide (2) 20f of the present invention as a pale brown powder.

Create a group of 5 Enkoko vein mice (8td, ddY strain, weight 25-30y), collect blood from the fundus vein of each mouse using a hematocrit tube, and immediately centrifuge at 12,000 rpm for 5 minutes to obtain plasma. . This plasma glucose 1it-/lucose analyzer (Yatron Rei-700
0. (manufactured by Yatron) 1 when not administered (Ohr)
blood sugar level. Immediately after Ohr's blood collection, the sample dissolved in physiological saline is administered intraperitoneally.

Blood was collected 7 hours and 24 hours after the administration of the sample, and the amount of glucose in the plasma was measured.The relative value when the 0 hour blood sugar level was set as 100 was calculated, and the relative blood sugar level was shown in Table 1.

The results were expressed as the mean value and the standard difference value, and significant differences were determined by one-dimensional analysis of variance.

Table 1

Claims (1)

[Claims] 1. The following physical properties: 1) Has a hypoglycemic effect; it) Specific rotation = [α] = +3.4 @ (C0,5
, water), ■) Decomposition temperature: approximately 360°C, iv) Infrared absorption spectrum (KBr method) Vtaax
! 3325.1610.1050 (broad) and 5
50 cm-', ■) No specific absorption in the ultraviolet region, ■) Nuclear magnetic resonance spectrum (90MHi C20):
5.31 (8,), 4.50-5.09 (m), 4
．． 18(su, 3.28~3.89(steel), 1.83(
8) , 1.51 (s) and 1.15 (t, J =
7,13), vi) pH: A polysaccharide characterized by an aqueous solution pH of 6.72. 2. The following physical properties: 1) Has a hypoglycemic effect, Amount ■) Specific rotation: [α) = +3.4° (CG, 5.
water), +1) Decomposition temperature: approximately 360°C, iv) Infrared absorption spectrum (KBw method) Vmax:
3325.1610.1050 (broad) and 55
0 cll-', V) No specific absorption in the ultraviolet region, M1) Nuclear magnetic resonance spectrum (90MHz C20)
:5.31(S), 4.50~5.09(s),
4.18 ('), 3.28-3.89 (durability, 183 (1
), 1.5Hs) and 1.15 (t, J = 7
．． 13), vi) A hypoglycemic agent containing a polysaccharide as an active ingredient characterized by the pH of the pH 1 aqueous solution being 6.72.