JPH0363561B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a novel adlay polysaccharide substance and a novel lipid metabolism improving agent containing this substance. Conventionally, so-called "dietary fibers" such as pectin and glucomannan have been said to have the effect of suppressing the rise in serum cholesterol, but the effects of pectin and the like have not yet been fully elucidated. It is also known that substances mainly composed of cellulose, hemicellulose, and ligrin obtained from rice bran have an effect of suppressing the rise in cholesterol (Japanese Patent Application Laid-Open No. 141415/1983). The present inventors searched for a powerful lipid metabolism improving agent that has a therapeutic effect on hyperlipidemia and arteriosclerosis, which are considered to be the causes of cardiovascular diseases such as the heart. The present inventors discovered that a coix seed polysaccharide substance has a high lipid metabolism improving effect, and confirmed that this coix seed polysaccharide substance is a new substance, leading to the present invention. That is, the present invention is a pearl barley polysaccharide substance having the following properties. a Weight average molecular weight: Approximately 500,000 b Sugar composition: xylose 36.4%, arabinose 34.4%, glucose 17.6%, uronic acid 7.4%, galactose, mannose (trace amount) c Specific optical rotation: [α] ²⁴ _D = -97.5゜d Infrared absorption spectrum: 900cm ^-1 and 1650cm ^-1
Solubility: Soluble in water, soluble in alkaline aqueous solution,
Insoluble in acetone, benzene, alcohol, hydrous alcohol, and chloroform, respectively Color reaction: Aniline/phthalic acid reaction (+),
Ammonia/silver nitrate reaction (+), ninhydrin reaction (+), ferric base reaction (±) g Basic, acidic, neutral: Neutral h Properties: White to light brown (lyophilized powder) Tasteless, odorless , i Physiological Activity: Lipid Metabolism Improving Effect The present invention is also a lipid metabolism improving agent containing a Coix barley polysaccharide substance or (and) a composition containing the substance as an active ingredient. The lipid metabolism improving agent of the present invention has an extremely high lowering effect on serum index components such as cholesterol,
Moreover, since it has no toxicity or side effects, it can be effectively used for the treatment of hyperlipidemia and arteriosclerosis. As mentioned above, it is known that rice bran hemicellulose and the like have an effect of suppressing the increase in cholesterol, but it has not been reported to date that a polysaccharide substance having an excellent lipid metabolism improving effect can be obtained from adlay bran. The adlay polysaccharide material of the present invention has the following properties. a The weight average molecular weight determined by high performance liquid chromatography is approximately 500,000. b Sugar composition is 36.4% by weight of xylose, 34.4% by weight of arabinose, 17.6% by weight of glucose, 7.4% by weight of uronic acid, 4.1% by weight of galactose, and mannose (trace amount). c Specific rotation [α] ²⁴ _D is -97.5° (concentration 88mg/100ml)
It is. d Infrared absorption spectrum shows β-D- at 900 cm ^-1
Absorption due to glucoside bonds and absorption due to peptide bonds at 1650 cm ^-1 are shown. e Regarding solubility, this substance is soluble in cold water and hot water, and an aqueous solution of this substance shows some viscosity. It is also soluble in alkaline aqueous solutions of various concentrations. Insoluble in acetone, benzene, alcohol, hydroalcohol, and chloroform. f Color reactions include aniline/phthalic acid reaction (+), ammonia/silver nitrate reaction (+), ninhydrin reaction (+), and ferric chloride reaction (±). g, h This substance is a neutral substance, and the color of the freeze-dried powder is white to light brown, and it is tasteless and odorless. i Shows a strong lipid metabolism improving effect as a physiological activity. The polysaccharide substance of the present invention is usually obtained from adlay bran and can be extracted by the following method. After degreasing pearl barley bran by treating it with an organic solvent,
After chemical treatment or oxygen treatment, the resulting treatment liquid is filtered to remove starch and the like as a liquid, and a residue is obtained. Dissolve this residue in a 0.5N alkaline aqueous solution,
The soluble content is separated as a hemicellulose fraction. This composition is mainly composed of adlay polysaccharide substances and also contains crude protein, lignin, cellulose, and ash. After neutralizing the alkaline aqueous solution containing this substance, the protein is precipitated and removed, the supernatant liquid is filtered, and ethanol is added to obtain the polysaccharide substance of the present invention as a precipitate. The present invention is a lipid metabolism improving agent containing a coix seed polysaccharide substance or/and a composition containing the substance as an active ingredient. As shown in the experimental examples below, this drug lowers the levels of various cholesterols, free fatty acids, neutral fats, phospholipids, β-lipoproteins, etc. in serum when administered orally, and has a remarkable effect on improving lipid metabolism. be. Additionally, this drug has no toxicity or side effects. The lipid metabolism improving agent of the present invention is usually orally administered,
Oral dosage is 50-100 mg/Kg body weight per day,
Long-term use is possible. Regarding the dosage form, the usual oral dosage form is applied;
For example, it is possible to select a preferred dosage form such as an aqueous solution, a tablet compressed with starch or lactose, a powder, or a granule. Next, an experimental example of the lipid metabolism improving effect will be shown. [Experimental Example A, Lipid Metabolism Improving Effect] Although rats were used as experimental animals, it is well known that the experimental results in rats are comparable to those in humans. Thirty-two SD male rats weighing approximately 60 g were preliminarily fed with the following high-cholesterol diet for 8 days, and then blood was collected from the tail vein of each rat to confirm that the serum cholesterol levels were averaged. 4, 8 fish per county
The animals were divided into groups, and one group was immediately decapitated, blood was collected, and the measurement items listed in Table 1 below were examined, and the average value of the measurements was taken as the value at "start of administration." The three groups were fed the following target food A, experimental feed, and the same for 8 days, and then decapitated, blood was collected, and measured in the same manner as the value at the end of administration. The above feed is commonly used in this type of experiment, and its composition is as follows. High-cholesterol feed: Contains sucrose and casein as main ingredients, 1% cholesterol and 0.25% sodium bile.Control feed A: Main ingredients contain sucrose and casein.Experimental feed: Contains sucrose and casein as the main ingredients. Experimental feed in which part of the sucrose in Control Feed A was replaced with 0.5% of the substance of the present invention: 1% of the substance of the present invention was substituted for part of the sucrose in Control Feed A. The experimental results were as shown in Table 1.

[Experimental example B, daily change in cholesterol increase suppressing effect]

SD male rat 16 weighing approximately 60g as experimental animal.
After raising them on the following cholesterol-free feed for 10 days,
Divide into 2 groups of 8 animals each, and administer the following cholesterol-added feed (control feed B) to one group.
On days 9, 9, and 18, blood was collected from the rat's tail vein and serum cholesterol levels were measured. In addition, the following cholesterol and the present invention substance-added feed (experimental feed) were administered to another group, and in the same manner, on the 5th day,
Serum cholesterol levels were measured on the 9th and 18th days. Cholesterol-free feed: 22% casein, 9% lard, corn oil (contains vitamins A, D, and E)
1%, salt mixture 4%, vitamin mixture (Harper formulation: contains all aqueous vitamins) 0.85
%, choline chloride 0.15%, sucrose 63% Control feed B: In the above cholesterol-free feed, sucrose was 61.75%, and cholesterol 1
% and 0.25% sodium bile acid.Experimental feed: In the control feed B, sucrose was added to
61.25% and 0.5% of the substance of the present invention was added.The experimental results were as shown in Table 2.

[Table] According to Table 2, the serum cholesterol levels on the 9th and 18th days were significantly lower values with a small risk rate of 5%, as a result of examining the significant difference using stochastic processing. Ta. From the above results, it is determined that this substance suppresses the increase in serum cholesterol. Furthermore, after the experiment was completed, blood was collected by decapitation, serum was separated, and total cholesterol and HDL-cholesterol levels were analyzed to calculate arteriosclerosis index. The results are as follows.

[Extraction of substances]

Add n-hexane 4 to 400g of pearl barley bran,
It was left overnight to degrease. Next, n-hexane was completely removed to obtain 200 g of defatted bran. To 100 g of this defatted bran, 0.1% by weight glycoamylase aqueous solution 5 and several drops of toluene were added, stirred thoroughly, and then subjected to an oxygen reaction at 40° C. for 24 hours in a thermostatic chamber. The resulting reaction solution was filtered through a glass filter, and the residue was washed with water and then added to 0.5N sodium hydroxide solution 1. This liquid was placed in a container filled with nitrogen gas, tightly sealed, and then shaken at room temperature for 18 hours to extract the alkali-soluble hemicellulose fraction. This is a composition containing adlay polysaccharide substances, with 67.9% by weight of adlay polysaccharide substances and 23.3% crude protein.
Weight% (total nitrogen amount x 5.83), lignin 11.1% by weight,
It contained 0.4% by weight of cellulose and 3.4% by weight of ash. After centrifuging the hemicellulose fraction extract to remove precipitates, the supernatant was neutralized with glacial acetic acid, and then trichloroacetic acid was added to a final concentration of 7% by weight to precipitate and remove proteins. After the obtained supernatant was dialyzed for 3 days, 4 times the amount of 99.5% by weight ethanol solution was added to obtain a precipitate. Dilute this precipitate with distilled water
After dissolving in 200 ml, the liquid was freeze-dried to obtain 5 g of a light brown powder substance. This substance had the above-mentioned properties of the adlay polysaccharide substance. Example 2 [Manufacture of drug] Compound powder for tableting (51% potato starch, 30% lactose)
%, Avicel 8%, Dextrin 8.5%, Magnesium stearate 0.5%, Calcium carbonate 2%
5 g of the polysaccharide substance obtained in Example 1 or 5 g of the substance-containing composition were uniformly mixed with 500 g of the mixed powder of 100 g of the polysaccharide obtained in Example 1, and the mixture was directly compressed using a tablet machine to obtain tablets. As shown in Table 4 below, the agent of the present invention containing the adlay polysaccharide substance as an active ingredient is clearly superior to rice bran hemicellulose in reducing serum total cholesterol, and has an excellent lipid metabolism improving effect.

[Table] shows the values on the 9th day of administration.

Claims (1)

[Scope of Claims] 1. Coix barley polysaccharide substance having the following properties. a Weight average molecular weight: Approximately 500,000 b Sugar composition: xylose 36.4% by weight, arabinose 34.4% by weight, glucose 17.6% by weight, uronic acid 7.4% by weight, galactose 4.1% by weight, mannose (trace amount) c Specific rotation: [α] ²⁴ _D = -97.5゜d Infrared absorption spectrum: 900cm ^-1 and 1650cm ^-1
Solubility: Soluble in water and alkaline aqueous solution, insoluble in acetone, benzene, alcohol, hydrous alcohol, and chloroform Color reaction: Aniline-phthalic acid reaction (+),
Ammonia/silver nitrate reaction (+), ninhydrin reaction (+), ferric chloride reaction (±) g Basic, acidic, neutral: Neutral h Properties: White to light brown (lyophilized powder) Tasteless, odorless , i Physiological activity: Lipid metabolism improving effect 2 A lipid metabolism improving agent comprising, as an active ingredient, a adlay polysaccharide substance having the following properties or (and) a composition containing the substance. a Weight average molecular weight: Approximately 500,000 b Sugar composition: xylose 36.4% by weight, arabinose 34.4% by weight, glucose 17.6% by weight, uronic acid 7.4% by weight, galactose 4.1% by weight, mannose (trace amount) c Specific rotation: [α] ²⁴ _D = -97.5゜d Infrared absorption spectrum: 900cm ^-1 and 1650cm ^-1
Solubility: Soluble in water, soluble in alkaline aqueous solution,
Insoluble in acetone, benzene, alcohol, hydrous alcohol, and chloroform, respectively Color reaction: Aniline/phthalic acid reaction (+),
Ammonia/silver nitrate reaction (+), ninhydrin reaction (+), ferric chloride reaction (±) g Basic, acidic, neutral: Neutral h Properties: White to light brown (lyophilized powder) Tasteless, odorless , i Physiological activity: lipid metabolism improvement effect