JPS61171427A - Substance for preventing thrombosis or the like - Google Patents

Abstract

PURPOSE:The titled substance comprising a specific polygonaceous plant and/or its extract as an essential component. CONSTITUTION:A substance for preventing thrombosis, etc., containing a specific polygonaceous plant such as Reynoutria japonica Houtt, Pleuropterus T, or Persicaria pilosa Kitag, Antenoron filiforme R., etc., and/or and extract obtained by extracting from the specific polygonaceous plant [compound shown by the formula (resveratrol when R1=R2=H; piceid when R1=D-glucose, R2=H; 2,3,5,4'- tetrahydroxystilbene-2-O-D-glycoside when R1=H, R2=O-D-glucose)] as an active ingredient. A dose is 20-1,000mg/day (dried powder of Reynoutria japon ica Houtt). The dosage form is powder, granule, tablet, solution for internal use, refreshing drinking water, etc. The dried powder is obtained by cutting undried Reynoutria japonica Houtt into thin pieces, extracting it with a lower fatty alcohol, condensing or concentrating the extracted solution to dryness.

Description

DETAILED DESCRIPTION OF THE INVENTION (Industrial Application Field) The present invention relates to a substance for preventing blood clots, etc., and more specifically, the object of this invention is
The purpose of the present invention is to provide a substance for preventing blood clots, etc., which contains a specific Polygonaceae plant such as Polygonaceae (Nica Houtt) and/or an extract extracted from this specific Polygonaceae plant as an essential component.

(Background of the Invention) Generally, a thrombus is a state in which blood has clotted within a blood vessel and is caused by damage to the vascular endothelium, inflammation, ulcer, etc., resulting in the formation of platelets, thrombocytes, white blood cells, fibrin, red blood cells, etc. This results in a stuck thrombus, resulting in lumen narrowing and occlusion.

This thrombus occurs due to causes such as increased red blood cells, water deficiency, anemia, bleeding, malignant ulcers, obesity, etc. If it occurs in a vein, it causes changes in blood flow and blood flow stagnation, and if it occurs in an artery, it causes It is said to lead to conditions such as peripheral blood circulation disorder and tissue necrosis.

From a biochemical perspective, when there is damage to the vascular endothelium, inflammation, ulcer, etc., aggregation of platelets, etc. starts at that location, and the metabolite of arachidonic acid, thealrxs2
．． nn7 Released (7) TXB2. It is believed that HHT also synergistically promotes blood aggregation.

TXB2, a metabolite of arachidonic acid. HHT is converted into leukotrienes that protect blood vessel walls through the metabolism of cyclooxygenase, while 5-HE is converted into leukotrienes by arachidonic acid poxygenase.
It is metabolized to TE, 12-HETE and prostaglasin, which is an antagonist of leukotrienes.
It is thought that substances that inhibit the production of arachidonic acid lipoxygenase metabolites, that is, specifically (selectively) inhibit the activity of lipoxygenase, which is an arachidonic acid metabolic enzyme, have an extremely high ability to prevent thrombosis.

(Prior art and its drawbacks) Conventionally, such thrombosis has been treated by giving heparin, an acidic mucopolysaccharide, but there is currently no effective treatment other than surgical methods. It is said that

(Progress of the Invention) Therefore, in order to eliminate all of the above-mentioned conventional drawbacks, the inventor endeavored to discover a specific (selective) inhibitor of boxygenase. Japanese knotweed (Reynoutria japo) is a plant belonging to the Polygonaceae family, which was eaten as a tea or as a tea.
nica Houtt), Tsurumi Dokudami (Pl.
europterus multiflorun+ T
) + Persicaria pilosa
Kitag, ) + Mizuhiki (Antenoron)
It has been discovered that when a specific Polygonaceae plant such as filiforse R.) and/or an extract extracted from this specific Polygonaceae plant is applied as a medicine or food, it is effective in preventing and resolving the thrombotic symptoms, etc., and the present invention reached.

(Solution Means) That is, the present invention is applied to Japanese knotweed (Reynoutria j.
aponica Houtt) + Pleuropterus 5uitiflora
T) + Persicaria pilo
sa Kitag, )l Mizuhiki (Antenor
on filiforme R,) and/or an extract extracted from this specific Polygonaceae plant, and in particular, the extract extracted from this specific Polygonaceae plant is represented by the following structural formula +1). The present invention relates to a substance for preventing thrombosis, etc., which is characterized by containing a stilbene compound. (Structure of the invention) Japanese knotweed (Reynoutria) used in this invention
jap.

n1ca Houtt) Pleuro
pterus suitiflorum T) + Persicaria pilosa Kita
g, ) + Antenoron fili
for+me R,)+ are all perennial plants of the Polygonaceae family.
In addition, other related species can also be suitably used, and all parts of these (above-ground or underground parts (tubers, basal, roots),
or seeds), especially roots can be suitably used as raw materials.

In this invention, to obtain dry powder of Japanese knotweed etc.
First, it is dried by any known natural drying, hot air drying, or freeze drying, and the dried product is then mechanically pulverized (
Powder by ball mill/screw). In this invention, this powder can also be effectively used as an essential ingredient.

The extract is then obtained from the dry powder as follows.

First, non-dried Japanese knotweed is cut into pieces, and the cut pieces or the dried powder are extracted with lower aliphatic alcohol.

If this extract is concentrated or dried before use, it can be used as an essential component of the thrombosis prevention substance according to the present invention.

Alternatively, if the shredded material or the dried powder is extracted with acetone-methanol, filtered, the filtrate is further extracted with ethyl ether, and this ethyl ether hardly soluble portion is purified by column chromatography and repurified with ethanol, the following stilbene can be obtained. The compound is obtained in the form of colorless crystals.

Of course, the ethyl ether hardly soluble portion does not necessarily have to be purified to a stilbene compound, but can be used as a component of the thrombosis prevention food according to the present invention by simply evaporating the portion to dryness.

In this invention, it can be used as an essential blending component even in the concentrated liquid stage, and can also be used as a blending component in the dry solid state.

Sveratrol, Piceide, 2.3,5.4''-tetrahydroxystilbene-2-0-D-glucoside.

Japanese knotweed (Reynoutria japo) like the one above
nica Houtt), Tsurumi Dokudami (Ple
uropterus multifloru-T), Persicaria pilosa Ki
tag,).

Antenoron filiforme
The substance for preventing blood clots, etc. according to the present invention contains a dry powder of a specific Polygonaceae plant such as R, ) or an extract (purified stilbene compound if necessary) from this specific Polygonaceae plant as an essential component Typically, an employee will have two jobs per day.
Any pharmaceutical or food form that can be applied with dry powder such as Japanese knotweed in an amount of about 0+wg to 1000mg may be used.

Specific examples of the form include powders, granules, tablets, oral solutions, soft drinks, and confectionery.

In the present invention, any pharmaceutical or food form may be prepared by adding excipients, fillers, sweeteners, and flavorings according to conventional methods.

(Effects of the Invention) As described above, the substance for preventing blood clots, etc. according to the present invention can be obtained from Reynoutria japonica (Reynoutria japonica Hout
T), Pleuropterus
s+ultifloru+m T)+Oketade (P
ersicaria pilosa Kitag, )+
Mizuhiki (Antenoron filifor+)
It is a thrombosis prevention substance that contains a specific Polygonaceae plant such as we R, ) and/or an extract extracted from this specific Polygonaceae plant (including a stilbene compound) as an essential component.
Arachidonic acid glue poxygenate such as 5-HETE, which is the cause of worsening symptoms of thrombosis. Therefore, it is a food with extremely high antithrombotic preventive ability.

Furthermore, when the substance for preventing blood clots, etc. according to the present invention is prepared in food form, it is not a pharmaceutical, so there is no need to seek diagnosis and instructions from a doctor for treatment, and the effect can be easily applied at home.

The effects of the present invention will be made clearer by describing Examples and Test Examples of the substance for preventing thrombosis, etc. according to the present invention.

(Example) Japanese knotweed (Reynoutria japonica)
Houtt) rhizomes and roots (15 kg) were defatted twice with 10 Il of n-hexane, and after defatting, Japanese knotweed roots 13.
2Kg was extracted with acetone-methanol (1:1) 2Of, this extract was concentrated to 0.51, this concentrate was extracted with ethyl ether 51, and the extraction residue was extracted with ethanol on a silicic acid column. , white crystals were obtained.

600 g of this crystal was obtained.

Qualitative analysis of this crystal using thin layer chromatography revealed that
Resveratrol, piceido, 2.3.5.4'-0-
It was D-glucoside.

(Test example) Wistar male rats were used, and the rat intraperitoneal polynuclear leukocytes were washed with HEPS-saline buffer (pH 7,4), suspended in the same buffer, and sonicated, and then arachidonic acid It was used as an enzyme solution for metabolism. This platelet homocinate, samples of each stilbene compound, Japanese knotweed powder, and blank at various concentrations were heated at 37°C.
, kept warm for 5 minutes, and then added [IC] arachidonic acid (0,
05 μCi) was added and ink-painted for 5 minutes.

The reaction was stopped with formic acid (pH 3), and arachidonic acid metabolites were extracted with ethyl acetate and subjected to silica gel thin layer chromatography.
The radioactive substances were detected by autoradiography and the spots It was excised and radioactivity was quantified using a liquid scintillation counter.

The test results are summarized in Tables 1 and 2 below.

As is clear from the above results, the Japanese knotweed powder and the stilbene compound used in the present invention have an excellent effect as inhibitors of the enzymatic activity of poxygenase, that is, the thrombosis prevention substance according to the present invention has an excellent thrombosis prevention effect. It turns out that it is effective.

Claims (2)

[Claims] (1) Japanese knotweed (Reynoutria japoni)
ca Houtt), Pleurop
terus multiflorum T), Persicaria pilosa Kitag
．． ), Antenoron filifor
me R. ) and/or an extract extracted from the specific Polygonaceae plant as an essential ingredient. (2) The substance for preventing thrombosis, etc. according to claim 1, wherein the extract extracted from a specific Polygonaceae plant contains a stilbene compound represented by the following structural formula (1). ▲There are mathematical formulas, chemical formulas, tables, etc.▼...(1) [When R_1=R_2=H, resveratrol, R=
D-glucose, when R_2=H, piceide, R_1
=H, R_2=OD-glucose is 2,3,5
, 4'-tetrahydroxystilbene-2-O-D-glucoside]