JP2001261569A - Antiobestic agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a antiobestic agent capable of substituting the antiobestic agent in a synthetic medicine system, derived from a natural product, excellent in antiobestic properties and further excellent in safety and economy. SOLUTION: This antiobestic agent is characterized in that the agent contains (a) an extract of Peucedanum terebinthaceum or Peucedanum deltoideum of the family Umbelliferae, and (b) an extract of at least one plant selected from Salacia oblonga, Salacia prinoides and Salacia prinoides, as an active ingredient.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an antiobesity agent derived from a natural plant which is effective for prevention and treatment of obesity, and which is excellent in safety and economical. More specifically, the present invention relates to an antiobesity agent comprising a combination of a natural plant-derived plant of the family Apiaceae, Hyugatouki (Hyuga Toki), and a Euonymiaceae plant of a specific genus Salacia.

[0002]

2. Description of the Related Art As a method for preventing or treating obesity,
2. Description of the Related Art Diet therapy, exercise therapy, surgery, drug therapy and the like have been conventionally known. However, these methods for preventing or treating obesity have advantages and disadvantages, and at present, satisfactory results have not been obtained.

For example, a method for preventing or treating obesity using a synthetic drug such as fenfuramine or azindol as an appetite suppressant has drawbacks such as dry mouth and habit.

[0004] In epidemiological investigations, obesity-induced hypertension, diabetes, circulatory diseases and the like have not changed so much before 1980. However,
For example, in an epidemiological survey in the Netherlands from 1996 to 1997, it was reported that 20% of artificials between the ages of 3 and 21 were obese, and today obesity is becoming a huge social problem.

[0005]

DISCLOSURE OF THE INVENTION The present invention aims to remarkably remedy the drawbacks of conventional prevention or treatment of obesity by using an antiobesity agent derived from a natural product.

The ease of action and safety, which are the general characteristics of natural products, are extremely important in view of the fact that prevention and treatment of this kind of obesity require a long time (long term). .

[0007] That is, obesity drugs derived from natural products include (1) drug therapy in which the side effects of synthetic drugs must be considered;
(2) It can be said to be superior to conventional obesity prevention and treatment methods such as diet and exercise therapy that require patience and effort to sustain.

[0008] The present invention relates to an obesity agent derived from a natural product, which (a) can prevent the deposition of excess visceral fat while living a normal life, and (b) is abnormal in serum lipids. It is an object of the present invention to provide an obesity agent derived from a natural product which has characteristics such as being able to control the value or weight and is excellent in safety and economy.

[0009]

SUMMARY OF THE INVENTION The present invention is summarized as follows: (a) Hyugatouki (Hyuga Toki), an Apiaceae plant;
And (b) Salicia oblonga, Salicia reticulata (Salasia prinoid)
es), Saracia Prinoides (Salasia p.
(Rinoides) as an active ingredient.

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

The antiobesity agent derived from a natural product of the present invention has been developed with an emphasis on the fact that obesity is often caused not only by the accumulation of fat in the body but also by the complications of water retention. There is a big feature in that.

That is, the present inventor has a viewpoint of (a) excreting excess water by a diuretic effect, and (b) a viewpoint of inhibiting excess saccharides to be converted into lipids from flowing into blood.
From the two aspects, we have been working diligently to develop new anti-obesity agents.

[0013] The present inventor has already discovered that the family of Euonymus (Cela)
staaeae plants, ie, Salacia oblonga (Salacia o)
blonga), ・ Salacia reticulata (Salasiar)
ethiculata), ・ Salacia purinoides (Salasia p.
A patent has been obtained for a therapeutic agent for diabetes (antidiabetes) containing an extract of the present invention as an active ingredient (Patent No. 3,030,008).

Then, the inventor of the present invention, in the patent,
The active ingredient of the plant belonging to the genus Salacia has the property of effectively inhibiting the activity of α-glucosidase, which is a decomposition oxygen such as disaccharides, and what is a true active substance for treating diabetes. Is revealed.

The present inventor has further proposed that the active ingredient of the Salacia plant prevents decomposition of various carbohydrates and oligosaccharides (disaccharides or trisaccharides) ingested into meals into monosaccharides and absorption into the body, He has the ability to prevent obesity due to overnutrition.

[0016] 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 Euonymus (Celastaceae) is a climbing plant (a woody climbing plan).
t), which are naturally abundant in terms of resources in India and Sri Lanka.

The antiobesity agent derived from a natural product of the present invention is, as described above, a crude drug having a diuretic effect and a crude drug having an effect of inhibiting excessive inflow of saccharides into the blood (in other words, α-glucosidase). (A crude drug having an activity inhibiting ability of the present invention).

In the antiobesity agent derived from the natural product of the present invention, the herbal medicine having a diuretic effect in combination with the herbal medicine of the plant belonging to the genus Salacia of the family Euonymus is Hyugatouki (Hyuga Toki), a Umbelliferae plant.

There are many crude drugs classified into diuretic crude drugs. These crude drugs having a diuretic effect are used for excreting excess water when renal function is reduced for some reason and water is stored in the body. As a crude drug having this kind of diuretic effect, picked-up hair, watermelon, catalpa, and the like are well known. Also,
As a synthetic drug having a diuretic effect, a thiazide-based preparation classified as a hypotensive diuretic is widely used.

In the present invention, among the crude drugs having a diuretic effect, the Hyugatouki (Hyuga Toki), a Umbelliferae plant, is a member of the family Euonymus (Celapus).
stagee) is characterized in that it exhibits an excellent effect (synergistic effect) in combination with a plant of the genus Salacia.

The aforementioned Apiaceae plant, Hyugatouki (Hyuga Toki) (Peucedanum terebinthac)
eum or Peucedanum deltoide
um) is used in Miyazaki, Oita and part of Ehime as a folklore medicine as a tonic, gynecological, gastrointestinal and anti-alcoholic agents. As the name suggests, Toki is similar in appearance to medicinal herbal crude drugs, but it has not been studied because it is slightly less aromatic. Hyugatouki (Hyuga Touki) was sometimes called Inukito.

The antiobesity agent derived from a natural product of the present invention includes (1).
An active ingredient comprising an extract of Hyugatouki (Hyuga Toki) of the Umbelliferae plant, for example, an extract of root matter, and (2) an extract of Salacia genus of the Euonymus plant, for example, an extract of the underground part What is necessary is just to comprise.

The antiobesity agent derived from a natural product of the present invention comprises an extract of the above-mentioned two specific herbal plants as an active ingredient, and its form may be any desired one. . For example, the form of the extract may be in the form of an extract (liquid) or powder (solid).

In order to prepare an extract or powder from the above-mentioned specific herbal plant, 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. Raw material is roughly cut or pulverized by 3
Grind to about 0 mesh. Then, crushed 1k
5 g (l) of water, alcohol or hydrous alcohol as a solvent is added to the g, and the mixture is allowed to stand at 80 ° C. to 90 ° C. for 3 hours. The solvent is distilled off 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.

In the present invention, when preparing an anti-obesity agent from the powder of the above-mentioned specific crude drug, the powder may be added to desired excipients such as potato starch, lactose and dextrin to form granules or tablets. It is. The antiobesity agent of the present invention may be in the form of a tea bag or in the form of a liquid (decoction).

[0026]

EXAMPLES Hereinafter, the antiobesity agent derived from a natural product 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.

(Experimental Method) (1) An extract of Salacia oblonga / an extract of Hyugatouki is orally administered to a genetically obese female Zucker obese female rat. consider. (2) Demonstrate strong diuretic effect in Hyugatouki.

(Method for Preparing Antiobesity Agent) (1) The roots of dried Salacia oblonga and the roots of Hyugatouki were individually minced to obtain experimental materials. (2) Next, 5 times the amount of water was added to these experimental materials (each crude drug), and the mixture was heated and extracted for 3 hours, filtered through filter paper, concentrated at 45 ° C or lower under reduced pressure, and dried with hot water extract. I got The yield was 5.0% in the case of Salacia oblonga and 15.9% in the case of Hyugatouki. (3) A dry extract of the alcohol extract was prepared by the same operation. The yield was 6.2% for Salacia oblonga and 18.2% for Hyugatouki.

(Test of Diuretic Effect) The presence or absence of a diuretic effect was examined for each of the components of Hyugatouki (Hyuga Toki) and Salacia plants, which are essential components of the antiobesity agent of the present invention.
The diuretic effect test was performed in Wistar male rats, group 8
The test was performed as follows. (1) After a 20-hour fast, 5 ml / 100 g of physiological saline was loaded and the urine volume for 5 hours was determined. (2) The test drug was orally administered 30 minutes before the physiological saline load. In the control group, only water was orally administered. The results are shown in Table 1 below.

[0030]

[Table 1]

As can be seen from Table 1, Hyugatouki (Hyuga Toki) has a strong diuretic effect. Salacia oblonga also tends to show a diuretic effect, albeit to a lesser extent than that of Hyugatouki (Hyuga Toki).

(Test of anti-obesity effect on hereditary obese rats)
13-week-old Zucker obse female rats, group 8
The test was performed as follows. (1). As test drugs: ・ Salacia oblonga hot water extract (abbreviated as SH extract); ・ Hyugatoki hot water extract (abbreviated as HH extract) ・ Salacia oblonga alcohol extract (abbreviated as SA extract) The test drug consisting of Higatouki alcohol extract (abbreviated as HA extract) was used alone or in combination. (2) Test drug suspended in 5% CMC at 5 pm daily
Oral administration at 6 o'clock. Food and water were allowed ad libitum. (3). Two weeks later, the rats are killed, and (a) visceral fat content,
(B) The amount of fat in serum water and (c) the change in body weight were examined.
The measurement of (a) the amount of visceral fat and (b) the amount of lipid in serum used a commercially available clinical test kit (Wako Pure Chemical Industries, Ltd.). The results are shown in Table 2 (visceral fat content), Table 3 (fat content in serum), and Table 4 (change in body weight).

[0033]

[Table 2]

As shown in Table 2 (visceral fat content), when a hot water extract of Salacia oblonga and Hyugatouki was used together (SH extract + HH extract),
Visceral fat deposition is suppressed by all the combination test drugs (concomitant drugs). In particular, in the case of the above-mentioned concomitant drug, effectiveness is recognized when a large amount of hyugatouki is mixed. On the other hand, when the hot water extract of the alcoholic extract of Salacia oblonga and Hyugatouki was used together (S
A extract + HA extract), although the effect was observed, it was not as potent as the former.

[0035]

[Table 3]

The commercially available clinical test kits used for measuring the amount of lipids in the various sera shown in Table 3 above are as follows. (A) Triglyceride ………… Triglyceride G-Test Wako (Wako Pure Chemical) (b) Cholesterol …………… Cholesterol CII Test Wako (Wako Pure Chemical) (c) Free fatty acids ……… NEFAC-Test Wako (Wako Pure Chemical)

As shown in Table 3 above (the amount of fat in serum), the following can be understood. (A) In the case of Salacia oblonga hot water extract alone (SH extract alone), the amount of triglyceride, which is not significant, is reduced by about 20%. (B) However, Salacia oblonga hot water extract (SH extract) and Hyugatoki hot water extract (H
H extract) significantly reduces not only neutral fat (triglyceride) but also cholesterol. (C) In the case of the combination of the alcoholic extract of Salacia oblonga and the alcoholic extract of Hyugatouki (SA extract + HA extract), the effect of inhibiting the deposition of neutral fat (triglyceride) and cholesterol was observed, but not as great as the former. (D) The amount of free fatty acids in the serum was equivalent to or higher than that of the test drug alone.

Today, many drugs are known as drugs that suppress the amount of lipids in serum, especially drugs that lower cholesterol levels. However, at present, a drug effective for hyperlipidemia having a high neutral fat (triglyceride) has not been developed. It is to be noted that the hyperlipidemia is an example in which a fatty liver caused by excessive drinking of alcohol is remarkable. From the above, the antiobesity agent of the present invention has a great significance.

[0039]

[Table 4]

As shown in Table 4 above (changes in body weight), in the case of the combination of the Salacia oblonga hot water extract (SH extract) and the Hyugatoki hot water extract (HH extract) (SH extract + HH extract) , A remarkable effect can be obtained. The weight of the rat at the start of the test was (508.2 ± 13.3 g).

For example, in the case of the mixed extract (SH extract: HH extract = 1: 4), the weight of the test rats on day 14 is 542.1 ± 10.5 g in the control group, whereas
518.5 ± 13.3 g, indicating that the weight was reduced by 23.6 g. Further, as shown in Table 4, it can be seen that, as compared with the case where each extract is used alone, the effect of suppressing body weight is greater when the two are used in combination, particularly when the extract with hot water is used in combination.

As shown in Tables 2 to 4, in the combined use system of the Salacia oblonga hot water extract (SH extract) and the Hyugatoki hot water extract (HH extract), the amount of visceral fat, the amount of lipid in serum, Weight loss (weight loss)
It shows a remarkable effect from the viewpoint of the effect, indicating that the antiobesity agent of the present invention is excellent.

Hyugatouki (Hyuga Toki), which is one of the essential components of the anti-obesity agent of the present invention, is already marketed as a health food or the like as alias Japanese ginseng. Hyugatouki (Hyuga Toki) does not have the effect of remarkably improving abnormal lipid values as described above, but has a marked effect when used in combination with Salacia oblonga.
This point is the same when other plants of the genus Salacia, ie, Salacia purinoides and Salacia reticulata, are used.

[0044]

Industrial Applicability According to the present invention, (a) Hyugatouki (Hyuga Toki), an Apiaceae plant excellent in diuretic effect, and (b) α
-An anti-obesity agent excellent in anti-obesity properties derived from natural products in combination with a specific Salacia plant of the Euonymus family, which is excellent in glycosidase utilization inhibiting ability and useful as a therapeutic agent for diabetes, and which is excellent in safety and economy Is provided. The antiobesity agent of the present invention, when used in combination (combination) with the above-mentioned specific plant extract, has a synergistic effect excellent in the effect of suppressing the amount of visceral fat and the amount of lipid in serum and the effect of suppressing body weight. There is a great feature in exhibiting.

Claims (2)

[Claims] (1) An extract of a plant of the family Apiaceae, Hyugatouki (Hyuga Toki), and (b) an extract of a plant of the family Euonymus, Salacia oblonga (Sala)
sia oblonga), Salacia reticulata (Salasia prinoides), Salacia prinoides (Salasia prinoides)
An anti-obesity agent comprising, as an active ingredient, at least one plant extract selected from s). 2. A Umbellifer (Hyuga Touki) of the Umbelliferae plant (Peucedanum terebinthac)
eum or Peucedanum deltoide
um), and a root extract of a plant belonging to the genus Salacia of the Euonymus family.
The anti-obesity agent according to the above.