JP2001288099A - Antihyperlipemic agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a natural product-based effective and safe antihyperlipemic agent in place of a conventional synthetic medicine-based antihyperlipemic agent having problems in adverse effects. SOLUTION: This antihyperlipemic agent comprises (a) an extract from a plant belonging to the genus Salacia of the family Celastaceae and (b) a chitinous material as active ingredients.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an antihyperlipidemic agent for improving hyperlipidemia caused by overeating, liquor drinking, diabetes associated therewith, and the like. More specifically, the present invention relates to an antihyperlipidemic agent excellent in safety and economy derived from a natural product comprising a plant belonging to the genus Salicaceae and a chitinous substance as active ingredients for improving hyperlipidemia.

[0002]

2. Description of the Related Art Hyperlipidemia is regarded as an important risk factor for cardiovascular diseases including vascular complications such as cerebral arteriosclerosis and ischemic heart disease. And, for the treatment of this hyperlipidemia, a cholesterol synthesis inhibitor, an absorption inhibitor, a neutral fat lowering agent and the like have been used depending on the purpose of the treatment.

[0003] However, since the onset of hyperlipidemia takes a long time and the treatment thereof also requires a long time,
The problem of side effects seen in conventional synthetic pharmaceutical antihyperlipidemic agents cannot be overlooked.

[0004] Natural products are known as antihyperlipidemic agents. For example, sterols contained in soybean and the like have long been known as antihyperlipidemic agents. Sex is not so clear.

[0005]

SUMMARY OF THE INVENTION In view of the above-mentioned circumstances, the present inventors have intensively studied to develop a natural product-based antihyperlipidemic agent which is highly safe and highly effective. The inventor of the present invention has proposed an antihyperlipidemic agent derived from natural products, which has been assured of safety, especially if any of those exhibiting an effect on abnormal cholesterol level or neutral fat level (triglyceride level) We believe that it can be replaced by synthetic drug-based antihyperlipidemic agent.

The present invention has been made in the direction of the research and development described above. According to the present invention, certain natural products,
That is, (a) an extract of a plant belonging to the genus Salacia of the Euonymus family and (b) an antihyperlipidemic agent excellent in safety and economic efficiency of a natural product containing a chitinous substance as an active ingredient. .

[0007]

SUMMARY OF THE INVENTION In summary, the present invention is directed to a natural product-based antihyperlipidemic agent, wherein the antihyperlipidemic agent comprises (a) Celistacea.
e) An extract of a plant of the genus Salasia, and (b) a chitinous substance as active ingredients.

Hereinafter, the technical configuration and embodiments of the present invention will be described in detail.

In order to develop a natural product-based antihyperlipidemic agent, the present inventors conducted screening tests on a large number of natural products, including folklore drugs, which are considered to be effective in improving hyperlipidemia. did. At that time, the test was conducted using diabetic mice in which hypercholesterolemia and hypertriglyceridemia were developed by streptodosin.

The present inventors have proposed natural anti-diabetic agents (an
In the development of Tidiabetes, a plant belonging to the genus Salacia of the family Euonymus (Celastanceae) has been found to be extremely effective, and has been previously proposed (for example, Japanese Patent No. 3,030,008, Japanese Patent Application Laid-Open No. 11-116).
496).

[0011] Therefore, the present inventor has suggested that since hyperlipidemia is deeply related to diabetes, the anti-diabetic agent (ant) should be used.
We thought that an extract of a plant belonging to the genus Salicaceae of the Lysaceae family, which is an active ingredient of diabetes, could be a remedy for hyperlipidemia in cooperation with other plants. As a result, the combination system of (a) the extract of the genus Salacia of the Euonymus family and (b) the chitinous substance has an excellent effect as an antihyperlipidemic agent, specifically, hypercholesterolemia or hypercholesterolemia. It was found that triglycerideemia was significantly improved.

The first component of the natural product-based anti-hyperlipidemic agent of the present invention, Cerusaceae
For example, the extract of the plant of the genus Salacia (Salasia) is, for example, (1) Salacia oblonga (Salasia o
blonga), (2) Salacia reticulata, (3) Salacia prinois
des), at least one extract of a plant belonging to the genus Salacia.

[0013] The euonymaceae (Celastacea)
e) The Salacia plant is a traditional medicine of India and Sri Lanka, that is, the AYURVED medicine (the AYURVED).
Sinhalese (Sinhale) traditionally used by ICtraditional medicine
se) and Kotara Himbriul
utuwel). The plant belonging to the genus Salacia of the family Cerastaceae is a vine plant (a woody climbing pl).
ant), which are naturally abundant in terms of resources in India and Sri Lanka.

In the present invention, the extract from the plant belonging to the genus Salacia of the Euonymus family may be in a desired form such as a liquid (extract) or a solid (powder, granule, etc.). In order to prepare an extract or powder from the Salacia genus plant of the Euonymus family, a desired embodiment may be adopted. For example, to prepare an extract from a plant belonging to the genus Salacia, the following procedure may be performed. The raw material is roughly cut or pulverized to about 30 mesh by a pulverizer. Next, 5 l (liter) of water, alcohol or hydrated alcohol as a solvent was added to 1 kg of the pulverized material, and the mixture was heated at 80 ° C to 90 ° C.
℃ 3 hours, in the case of cold immersion for 3 days at room temperature and filtered,
The solvent is completely distilled off from the filtrate at 45 ° C. under reduced pressure to prepare a dry extract solid. In order to prepare a powdery preparation, the solid extract may be powdered to about 100 to 150 mesh.

The chitin substance as the second component in the natural product-based antihyperlipidemic agent of the present invention should be released in a broad sense. The chitinous substances of the present invention include (1) chitin (cuticle), (2) chitin (chitin),
(3) It should be understood that chemically modified chitin and the like are included.

The above-mentioned chitin (cuticle) is a general name for a substance that forms an exoskeleton or firm skin such as an oyster, and contains chitin and a protein described later in terms of chemical composition. The chitin
Is a kind of polysaccharide composed of amino sugars, is a linear molecule in which amino-acetylated D-glucosamine is linked by β-1,4, and is a major structural polysaccharide in non-cephaloid animals and the like. is there. Examples of the chemically modified chitin include chitosan, which is a deacetylated product of chitin.

The above-mentioned chitin is contained in about 30% of shells of oysters such as crabs. In addition, chitin is contained in about 10% in not only oysters but also matsutake and shiitake. The chitin is known to be excellent in safety. In addition, it has properties such as activation of ecological defense function, activation of cellular immunity, cholesterol lowering action, antibacterial action, etc.It is widely used in agricultural water, forestry, etc., such as artificial skin, sutures, cosmetic materials, water purification, etc. It is also known as one of general-purpose materials.

In the natural hyperlipidemic agent of the present invention comprising a combination of (a) the extract of the genus Salacia of the Euonymus family and (b) a chitinous substance, the mixing ratio of both components is desired. Should be determined. As demonstrated in the examples described below, for example, (a) :( b) = 1: 2-
Hypercholesterolemia and hypertripriderideemia are significantly improved at a mixing ratio of 2: 1.

The natural antihyperlipidemic agent of the present invention comprising a combined use of (a) an extract of the genus Salacia of the Euonymus family and (b) a chitinous substance is, for example, a powder of both components. Granules or tablets may be prepared by adding desired excipients such as potato starch, lactose, dextrin and the like.

[0020]

EXAMPLES Hereinafter, the antihyperlipidemic agent of the present invention will be described in more detail with reference to examples. Needless to say, the present invention is not limited to the embodiments.

(Method for Preparing Pharmaceutical Ingredients) (1) Salacia Plant: An extract was prepared from a Salacia plant such as Salacia oblonga, Salacia reticulata, and Salacia purinoides as follows.
4 l of water per 1 kg of crude drug (Salacia genus plant)
(Liter), heated, filtered after 3 hours, 40 ° C
The mixture was concentrated under reduced pressure, and the solvent was completely distilled off to obtain about 65 g of an extract. (2) Chitin: Chitosan (manufactured by Kimitsu Chemical Co., Ltd.) was used as the chitin.

(Experimental Method) (1) A mouse model of hypercholesterolemia and hypertriglyceridemia was prepared as follows. That is, a group of 12 male ddY mice weighing 20 to 30 and streptodotomin (manufactured by Sigma) (hereinafter, STZ) which develops hyperlipidemia simultaneously with diabetes by destroying β-cells of the pancreas. Was given an intravenous injection of 100 mg / kg after 20 hours of fasting. (2). Immediately thereafter, a feed obtained by adding an extract of the Salacia genus plant and chitosan at a predetermined mixing ratio (addition rate: 3%) to a normal feed feed powder was fed, and after breeding for 4 weeks, blood was collected.
Blood glucose level, total cholesterol level, and triglyceride level were measured.

(Experimental Results) The following Table 1 shows the results when each of the components constituting the antihyperlipidemic agent of the present invention was administered alone to the mouse (model). Table 1
In (*), the mark (**) indicates that there is a significant difference at a risk rate of 0.01%, and the mark (*) indicates that there is a significant difference at a risk rate of 0.1%.

[0024]

[Table 1]

The following points are evident from Table 1. (1) In the treatment group bred by administering only STZ (streptodotocin), 12 mice died at the start of the experiment, 7 mice died, and the blood glucose level also increased to nearly 800 mg / dl. (2) On the other hand, those given only the extract of the genus Salacia after STZ administration showed significant effects in terms of deaths and suppression of blood glucose elevation. (3). The case where only chitosan was given after the administration of STZ was better than the treatment group, but did not show the same effect as the case where only the extract of the genus Salacia was given.

Next, as shown in Table 1, in view of the fact that all the plants of the genus Salacia show the same action and effect, Salasia oblonga (Salasia oblonga) was used.
a) Using an extract, an experiment was performed in a combined system of this and chitosan. The mixing ratio of both components is shown in Table 2 below. The amount of both components added to the feed was 3% of the feed as a mixture. The results are shown in Table 2 below. In Table 2, (**) indicates that there is a significant difference at a risk rate of 0.01%, and (*) indicates that there is a significant difference at a risk rate of 0.1%. .

[0027]

[Table 2]

The following points are evident from Table 2. (1). Salacia oblonga extract / chitosan 1: 2
In the combination system mixed at a ratio of ２2: 1, significant improvement in hypercholesterolemia and hypertriglyceridemia is observed. And it is recognized that these improvement effects are superior to the single system of each component. (2) In particular, a remarkable effect on improvement of hypercholesterolemia and hypertriglyceridemia is observed in a combination system in which Salacia obroga extract / chitosan is mixed at an equal ratio (1: 1).

As shown in Table 1, when Salacia oblonga extract is used alone, blood sugar level, cholesterol level, triglyceride level, STZ
Reduction of mortality from the origin is observed. However, as shown in Table 2, it is surprising that the combined use of Salacia oblonga extract and chitosan can improve the above-mentioned improvement points synergistically. In addition, chitosan itself has a cholesterol lowering action (this point is also apparent from Table 1), but this effect is also synergistically improved in the combination system.

(Acute toxicity) A group of 10 male ddY mice weighing about 20 g was orally administered orally at 2000 mg / kg to which a mixture of Salacia oblonga extract: chitosan = 1: 1 can be physically administered. Water was provided ad libitum and one week of life and death was observed. As a result, no deaths or abnormal behavior were observed, confirming that the antihyperlipidemic agent of the present invention is safe.

[0031]

Industrial Applicability According to the present invention, there is provided an antihyperlipidemic agent which is excellent in safety and economical efficiency of a natural product in place of a conventional synthetic pharmaceutical antihyperlipidemic agent.

[0032] Hyperlipidemia due to westernization of the diet of today, overeating, overdose of alcoholic beverages, diabetes mellitus associated therewith, and vascular complications such as cerebral arteriosclerosis and ischemic disease. The natural product-based antihyperlipidemic agent of the present invention, which is effective and safe against hyperlipidemia, which is regarded as an important risk factor for cardiovascular diseases, has great significance.

Claims (3)

[Claims] (1) (C) Celastacea
An antihyperlipidemic agent comprising, as active ingredients, an extract of a plant of the genus Salacia of (e) and (b) a chitinous substance. 2. The plant of the genus Salacia, wherein the plant is of the genus Salacia oblonga (Salasiaoblonga) or Salacia reticulata.
a), Salacia prinoides (Salasia pr
2. The antihyperlipidemic agent according to claim 1, which is at least one member selected from the group consisting of: 3. The method according to claim 1, wherein the chitin substance is cutin (cuti).
2. The antihyperlipidemic agent according to claim 1, which is at least one selected from cle), chitin, and a chemically modified chitin.