JP2003321362A - Food composition and medicament composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a food composition and a medicament composition capable of preventing or treating a diabetic complication. <P>SOLUTION: The food composition and the medicament composition comprise (A) proanthocyanidin and (B) Mori Cortex (mulberry bark) essence. The proanthocyanidin used preferably comprises 20 wt.% or more OPC. <P>COPYRIGHT: (C)2004,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a food composition and a pharmaceutical composition containing (A) a proanthocyanidin and (B) an extract of Sohakuhi.

[0002]

2. Description of the Related Art In Japan, the total number of diabetic patients and their reserves has reached 13.7 million, and the probability of developing diabetes is particularly high after the age of 40. ing. The most terrifying aspect of diabetes is its complications such as renal damage, neuropathy and retinal damage as it progresses. As a therapeutic drug for such complications, there is an aldose reductase inhibitor, but at present, the indication is limited to neuropathy, and a drug which is particularly effective for the prevention or treatment of diabetic complications. There is no such thing.

[0003]

Therefore, there is a need for food or pharmaceutical compositions that prevent or treat diabetic complications.

[0004]

The present invention provides a food composition or a pharmaceutical composition containing (A) proanthocyanidin and (B) an extract of Sophoraceae, which is a food composition or a pharmaceutical composition. May prevent the development of diabetic complications or treat the complications.

In a preferred embodiment, 20% by weight or more of the proanthocyanidin is OPC (oligomeric).
proanthocyanidin).

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The food composition and pharmaceutical composition of the present invention will be described below. It is obvious to those skilled in the art that the configurations described below do not limit the present invention and can be variously modified within the scope of the present invention.

The food composition or pharmaceutical composition of the present invention contains (A) proanthocyanidins and (B) sow extract. Hereinafter, each component will be described.

(A) Proanthocyanidins In the present invention, proanthocyanidins are a group of compounds consisting of a condensation polymer having flavan-3-ol and / or flavan-3,4-diol as a constituent unit and having a degree of polymerization of 2 or more. Say. Proanthocyanidins are known to have various activities such as antioxidant activity. Also,
It is known to have a vitamin P-like action, suppress the weakness of capillaries, and reduce retinal disorders.

In the present specification, among proanthocyanidins, flavan-3-ol and / or flavan-
A polycondensate having a degree of polymerization of 2 to 4 and containing 3,4-diol as a constitutional unit is referred to as OPC (oligomeric proanthocyanidin). OPC
Is a type of polyphenol, a powerful antioxidant produced by plants, which is concentrated in plant leaves, bark, fruit skins or seeds. Specifically, it is contained in grape seeds, pine bark, peanut thin skin, ginkgo, black locust fruit, cowberry and the like. It is also known that cola nuts in West Africa, roots of Latania in Peru, and green tea in Japan also contain OPC. OP
C is a substance that cannot be produced in the human body.

As the proanthocyanidin contained in the food composition or pharmaceutical composition of the present invention, crushed fruits or seeds such as grapes, blueberries, strawberries and avocados, or foods or pharmaceutical raw materials such as extracts thereof are used. Can be used. In particular, it is preferable to use an extract of pine bark. Since pine bark is rich in OPC among proanthocyanidins, it is preferably used as a raw material for proanthocyanidins in the present invention.

A method for preparing proanthocyanidins will be described below by taking an extract of pine bark rich in OPC as an example.

Pine bark extracts include French coastal pine (Pinus Martima), larch, black pine, red pine,
Himekomatsu, Japanese pine, Japanese pine, Japanese pine,
An extract of bark of a plant belonging to the order Pine such as Ryukyu pine, Utsukushimatsu, Rheuma pine, White pine, and Anneda of Quebec region of Canada is preferably used. Of these, bark extract of French coastal pine (Pinus Martima) is preferable.

The French coastal pine is a marine pine that grows on a part of the Atlantic coast of southern France. The bark of this French coastal pine tree contains proanthocyanidins, organic acids, and other physiologically active components, and the main component, the flavonoid proanthocyanidins, has a strong antioxidant effect that removes active oxygen. Are known.

The pine bark extract is obtained by extracting the above pine bark with water or an organic solvent. When water is used, hot water or hot water is used. As the organic solvent used for the extraction, an organic solvent acceptable for the production of foods or drugs is used, for example, methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, butane, acetone, hexane. , Cyclohexane, propylene glycol, hydrous ethanol, hydrous propylene glycol, ethyl methyl ketone, glycerin,
Mention may be made of methyl acetate, ethyl acetate, diethyl ether, dichloromethane, edible oils and fats, 1,1,1,2-tetrafluoroethane, and 1,1,2-trichloroethene. These water and organic solvent may be used alone or in combination. In particular, hot water, hydrous ethanol, and hydrous propylene glycol are preferably used.

The method for extracting proanthocyanidins from pine bark is not particularly limited, but for example, a heating extraction method,
A supercritical fluid extraction method or the like is used.

The supercritical fluid extraction method is a method of performing extraction using a supercritical fluid that is a fluid in a state of exceeding the gas-liquid critical point (critical temperature, critical pressure) of a substance. As the supercritical fluid, carbon dioxide, ethylene, propane, nitrous oxide (laughing gas), etc. are used, and carbon dioxide is preferably used.

The supercritical fluid extraction method comprises an extraction step of extracting a target component with a supercritical fluid and a separation step of separating the target component and the supercritical fluid. In the separation step, either extraction separation due to pressure change, extraction separation due to temperature change, or extraction separation using an adsorbent / absorbent may be performed.

Supercritical fluid extraction may be carried out by the entrainer addition method. This method applies to supercritical fluids
For example, ethanol, propanol, n-hexane, acetone, toluene, other aliphatic lower alcohols,
By adding about 2 to 20 W / V% of aliphatic hydrocarbons, aromatic hydrocarbons, or ketones and performing supercritical fluid extraction with the obtained extraction fluid, OPC, catechins (described later), etc. It is a method of dramatically increasing the solubility of a target substance to be extracted in an extraction fluid or enhancing the selectivity of separation, and is a method of efficiently obtaining a pine bark extract.

Since the supercritical fluid extraction method can be operated at a relatively low temperature, it has the advantage that it can be applied to substances that are altered or decomposed at high temperatures; the advantage that no extraction fluid remains; and the solvent can be recycled. In addition, there is an advantage that the desolvation process and the like can be omitted and the process is simplified.

Extraction from pine bark can be carried out by the liquid carbon dioxide batch method, liquid carbon dioxide reflux method,
It may be carried out by a supercritical carbon dioxide reflux method or the like.

For extraction from pine bark, a plurality of extraction methods may be combined. By combining a plurality of extraction methods, it becomes possible to obtain pine bark extracts having various compositions.

The pine bark extract used in the food composition or pharmaceutical composition of the present invention is specifically prepared by the following method, but this is an example and not limited to this method. .

1 kg of bark of French coastal pine is placed in 3 L of saturated sodium chloride solution and extracted at 100 ° C. for 30 minutes to obtain an extract (extraction step). Then, the extract is filtered and the resulting insoluble matter is saturated with 50 ml of sodium chloride.
Wash with 0 ml to obtain a washing solution (washing step). A crude pine bark extract is obtained by combining the extract with the wash.

Then, ethyl acetate 250 was added to the crude extract.
The process of adding ml and separating the layers and collecting the ethyl acetate layer is performed 5 times. The collected ethyl acetate solutions are combined and directly added to 200 g of anhydrous sodium sulfate for dehydration. Then, the ethyl acetate solution was filtered, and the filtrate was reduced to 1/5 of the original volume.
Concentrate under reduced pressure to volume. The concentrated ethyl acetate solution is poured into 2 L of chloroform, and the precipitate obtained by stirring is collected by filtration. Then, a washing step is carried out in which the precipitate is dissolved in 100 ml of ethyl acetate and then added again to 1 L of chloroform for precipitation to repeat twice. By this method, for example, 2 to 4 mer OPCs
About 5 g of pine bark extract containing 0% by weight or more and 5% by weight or more of catechins is obtained.

Extracts from the above-mentioned raw material plants, which are typically used as (A) proanthocyanidins in the food composition or pharmaceutical composition of the present invention, particularly pine bark extracts, include proanthocyanidins, namely flavan- 3-
It contains a polycondensate having a degree of polymerization of 2 or more and having oar and / or flavan-3,4-diol as a constituent unit. A polymer containing a large amount of a polycondensation polymer having a low degree of polymerization is preferably used. As the polycondensate having a low degree of polymerization, a polycondensate having a degree of polymerization of 2 to 30 (2 to 30 mer) is preferable, and a polycondensate having a degree of polymerization of 2 to 10 (2 to 10 mer) is more preferable. A polycondensate having a degree of polymerization of 2 to 4 (2 to 4 mer; that is, OPC) is more preferable.

Since OPC is an antioxidant as described above, it has the effect of lowering the risk rate of adult diseases such as cancer, heart disease and cerebral thrombosis, and the improvement of allergic constitution such as arthritis, atopic dermatitis and hay fever. It also has effects.

In addition to the antioxidant effect, OPC has the effect of suppressing bacterial growth in the oral cavity to reduce plaque (gum); the effect of restoring elasticity of blood vessels; lipoprotein in blood is active oxygen. To prevent the damage of fat from agglomeration on the inner wall of blood vessels and to prevent cholesterol from adhering to it; the effect of regenerating vitamin E degraded by active oxygen; as a vitamin E enhancer It is known to have the effect of.

In the present invention, proanthocyanidins containing 20% by weight or more of OPC are preferably used. More preferably, it is 30% by weight or more. Pine bark extract is preferably used as such a proanthocyanidin.

When a proanthocyanidin having a high OPC content is used, a proanthocyanidin (OP having a high degree of polymerization)
An excellent preventive or therapeutic effect for diabetic complications can be obtained, as compared with the case where the C content is small).

In addition, proanthocyanidins derived from raw material plants, especially plant extracts, contain catechin (ca
techin) is included. Catechins is a general term for polyhydroxyflavan-3-ols. As catechins, (+)-catechin, (-)-epicatechin,
(+)-Gallocatechin, (-)-epigallocatechin, epigallocatechin gallate, epicatechin gallate, etc. are known. In addition to (+)-catechin, which is called catechin in a narrow sense, gallocatechin, afzerekin, and 3-galloyl derivatives of (+)-catechin or gallocatechin have been isolated from natural products. For catechins, carcinogenesis suppression, arteriosclerosis prevention, fat metabolism abnormality suppression, blood pressure increase suppression, thrombosis prevention, anti-allergy, anti-virus,
It is known to have antibacterial, dental caries prevention, halitosis prevention, intestinal bacterial flora normalizing effect, scavenging effect of active oxygen and free radicals, and antioxidant effect. Further, catechins are known to have an antidiabetic effect of suppressing an increase in blood sugar. Further, catechins have the property of becoming more water-soluble and being activated at the same time in the presence of OPC.

Catechins are added to the above-mentioned raw material plant extract by 5
It is preferable that the content is at least wt%. More preferably, the raw material plant extract containing 20% by weight or more of OPC contains 5% by weight or more of catechins. For example, if the catechins content of the pine bark extract is less than 5% by weight, the catechins content may be added to be 5% by weight or more. It is most preferable to use a pine bark extract containing 5% by weight or more of catechins and 20% by weight or more of OPC.

(B) Sophoraceae Extract Sophorae japonica is the root bark of mulberry plants, is rich in flavonoids, and is used as an anti-inflammatory diuretic, laxative, or antitussive / expectorant drug as a herbal medicine. As the sowakuhi extract contained in the food composition or the pharmaceutical composition of the present invention, sowakuhi extract according to the Japanese Pharmacopoeia; or sowaku powder powder obtained by drying the root bark of mulberry and then pulverizing it is preferably used.

The food composition or pharmaceutical composition of the present invention contains the above-mentioned (A) proanthocyanidin and (B) sowaku extract in an arbitrary ratio, preferably 1: 0.
It is included in a weight ratio of 5 to 50, more preferably 1: 1 to 30.

The food composition or pharmaceutical composition of the present invention contains the above-mentioned (A) proanthocyanidin and (B) sow extract, and, if necessary, various additives usually used in foods or pharmaceuticals. . Examples of such additives include excipients, fillers, binders, thickeners, emulsifiers, colorants, flavors, food additives and the like. The food composition and the pharmaceutical composition of the present invention may be formed into a shape such as a tablet or a pill, for example, by adding an excipient or the like to a pine bark extract and a sophoraceae extract rich in proanthocyanidins. Alternatively, it may be in the form of powder or other form without being molded.

Capsules such as hard capsules and soft capsules, powders, granules, tea bags, candy, liquids, pastes and the like may be used.

Further, for example, nutritional components such as royal jelly, vitamins, proteins, calcium such as egg shell calcium, chitosan, lecithin, chlorella powder, ashitaba powder, and moloheiya powder can be added. The taste may be adjusted by adding stevia powder, matcha powder, lemon powder, honey, reduced maltose, lactose, sugar solution, seasoning and the like.

The method of ingesting the food composition or pharmaceutical composition of the present invention is not particularly limited. The food composition or pharmaceutical composition of the present invention, depending on its shape or preference, may be eaten or drink as it is, or may be dissolved in water, hot water, milk or the like, or one in which the ingredients are leached out. You can drink it.

The intake amount of the food composition and the pharmaceutical composition of the present invention is not particularly limited, but 20 to 1000 mg of (A) proanthocyanidin and 10 to 1000 mg of (B) sow extract can be ingested per day. Is preferred.

The food composition and the pharmaceutical composition of the present invention have an excellent preventive or preventive effect against diabetic complications by enhancing the vascular protective action of proanthocyanidins by a component contained in the extract of Sohakuhi. It seems to have a therapeutic effect.

[0040]

The present invention will be described below with reference to examples.
It goes without saying that the invention is not limited by this example.

(Example 1) 40 parts of proanthocyanidins were used.
Using an ethanol extract of pine bark containing 20% by weight (OPC 20% by weight) and 5% by weight of catechin (trade name: Flavangenol, Toyo Shinyaku Co., Ltd.) and Sohakuhi Extract (Nippon Powder Chemicals Co., Ltd.) The effect on diabetic cataract, which is one of the diabetic complications, was evaluated as follows.

Streptozotocin was intraperitoneally administered to 10-week-old Wistar rats consisting of 10 animals per group at a dose of 50 mg / kg / body weight to prepare diabetic rats. Then, the basic feed (MF powder) was fed with the feed mixed in the ratios shown in Table 1 below for 15 days, and the progress of diabetic cataract was visually evaluated. In addition, the visual evaluation was performed by evaluating the white turbidity of the crystalline lens in 5 grades as follows: No change ... -Shaped dots can be observed ..... The surface of the 1-point crystalline lens is cloudy ..... The surface of the 2-point crystalline lens is cloudy and the fundus cannot be seen through .. 3-point crystalline lens. Is completely cloudy ... 4 points.

The results are shown in Table 2. The results in Table 2 are
It is the average score of the evaluation of each group.

(Comparative Examples 1 and 2) As in Example 1, the cloudiness of the crystalline lens was measured in the same manner as in Example 1, except that either the ethanol extract of Pine bark or the soybean agar extract used in Example 1 was used. Was evaluated. The results are also shown in Table 2.

[0045]

[Table 1]

[0046]

[Table 2]

The results in Table 2 show that the combination of proanthocyanidins and the sow extract can suppress the progression of cataract, which is one of the complications of diabetes.

[0048]

INDUSTRIAL APPLICABILITY As described above, by ingesting a food composition or a pharmaceutical composition characterized by containing (A) proanthocyanidin and (B) sow extract, diabetic complications can be prevented. It has been found to prevent or treat. In particular, by using proanthocyanidins containing OPC in an amount of 20% by weight or more, more excellent effects can be obtained.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61P 25/28 A61P 25/28 27/12 27/12 F term (reference) 4B018 MD52 MD53 MD61 ME03 4C086 AA01 AA02 BA08 MA02 MA04 MA17 MA28 MA35 MA36 MA37 MA41 MA43 MA52 NA14 ZA36 ZA39 ZA44 ZA45 ZA54 ZA67 ZA89 ZA96 ZB13 ZB26 ZC33 ZC35 ZC41 4C088 AB03 AB34 AC08 AC11 BA07 BA09 MA10 CA22 CA07 MA17 CA11 CA07 CA09 CA10 CA10 CA10 CA10 CA10 CA10 CA10 CA10 CA10 CA09 MA41 MA43 MA52 NA14 ZA33 ZA36 ZA42 ZA44 ZA45 ZA54 ZA67 ZA89 ZA96 ZB13 ZB21 ZB26 ZB35 ZC33 ZC35 ZC41

Claims (4)

[Claims] 1. A food composition comprising (A) a proanthocyanidin and (B) an extract of Sophoraceae. 2. 20% by weight of said proanthocyanidins
The food composition according to claim 1, wherein the above is composed of OPC (oligomeric proanthocyanidin). 3. A pharmaceutical composition containing (A) a proanthocyanidin and (B) an extract of Sophoraceae. 4. 20% by weight of said proanthocyanidins
The pharmaceutical composition according to claim 3, wherein the above is composed of OPC (oligomeric proanthocyanidin).