JP2001226263A - Prophylactic of obesity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare a prophylactic of obesity, effective for the improvement of the constitution of the obesity by promoting the decrease of the whole-body or topical adipose tissue, or the suppression or prevention of the obesity by inhibiting the increase of the same tissue. SOLUTION: This prophylactic of the obesity comprises a compound of general formula (1) (wherein, R is a hydrogen atom, a residue of monosaccharides or oligosaccharides).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an agent for preventing obesity, which is effective for improving obesity by promoting the reduction of systemic or local adipose tissue or preventing obesity by preventing the increase of the tissue.

[0002]

2. Description of the Related Art Fat in the body is
An excess of ingested energy is generated by accumulating white fat cells as neutral fat. It is often said that the accumulation of fat in the subcutaneous and liver is not only cosmetically unfavorable, but also complicated with adult diseases such as arteriosclerosis, cerebrovascular disease, heart disease, diabetes, hypertension, and kidney disease, and is likely to be complicated. ing. Recently, obesity due to overeating, lack of exercise, stress, etc. has been increasing, and at the same time, women in particular have a tendency to crave a slim and lean body from the outside, and there is a decrease or accumulation of subcutaneous fat and liver fat. Prevention is an important issue.

On the other hand, capsaicins contained in capsicum and the like as substances having an obesity preventing action bind to albumin in the blood and secrete hormones that promote adrenal metabolism,
It is known to act on the liver and fat cells to activate energy metabolism (Kazuo Iwai and Nobuji Nakatani, Food Function of Spice Components, p. 97, 1989). However, since capsaicins have a strong stimulus, there has been a problem that their uses and amounts used are limited. For this reason,
There have been various approaches using oral drugs such as an appetite suppressant, dietary restriction, exercise, etc., but no obesity preventive agent having a satisfactory effect of suppressing or reducing accumulation of subcutaneous fat, liver fat, etc. has been found. Was.

[0004]

Therefore, the present invention is effective for improving obesity by promoting the reduction of systemic or local adipose tissue, or for suppressing or preventing obesity by preventing the increase of the tissue. It is intended to provide a novel agent for preventing obesity.

[0005]

Means for Solving the Problems In order to achieve the above object, the present inventors have thought that it is important to suppress the increase and accumulation of fat, and made intensive studies. Fat in the body stores excess energy as oil droplets in fat cells when the intake energy obtained from food exceeds the energy consumed for maintaining life and exercising. Oil droplets are broken down by enzymes (phospholipase C) in the same way as proteins. However, the oil droplets are covered by a membrane of phospholipid that repels water, and enzymes in a mass of water, a parcel around the oil droplets, cannot be accessed. On the other hand, the lipolytic hormone is secreted by activating the sympathetic nerve by exercising, and the decomposition of fat is promoted. Like this hormone, a substance that has the function of increasing the affinity between oil droplets and enzymes promotes the breakdown of fat in the body, suppresses the increase and accumulation of fat,
We thought that obesity could be prevented.

The inventors of the present invention have studied the substances that suppress obesity in obese mice bred on a high calorie diet, and found that the following general formula (1)

[0007]

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(Where R is a hydrogen atom, a monosaccharide or oligosaccharide residue) has the above-mentioned action, and promotes the decomposition of fat or suppresses the increase / accumulation of fat, resulting in obesity. The present inventors have found that the present invention is effective for prevention or improvement of obesity, and completed the present invention.

That is, the present invention provides the following general formula (1)

[0010]

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(Wherein R is a hydrogen atom, a monosaccharide or oligosaccharide residue).

[0012]

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS Hereinafter, embodiments of the present invention will be described in detail.

Among the compounds represented by the general formula (1) used in the present invention, those in which R is a monosaccharide or a minor residue are so-called glycosides, and many are commercially available. Yes and easily available. Further, it can be easily synthesized by a known method described in the above-mentioned publications. For example, a saccharide and 4- (p-hydroxyphenyl)-
It can be easily synthesized by reacting 2-butanol with an acid. In addition, conventionally known Koenigs-
It is also possible to synthesize only the β-form by using the Knorr reaction or the like [Chem.ber., 34, 957 (1901)].
Furthermore, these glycosides can be purified using a means such as column chromatography. Here, the residue means the remaining portion of the saccharide except for the hydrogen of the hemiacetal hydroxyl group.

Here, oligosaccharides refer to disaccharides to hexasaccharides, and specifically include disaccharides such as lactose, maltose, cellobiose, isomaltose and epilactose, gentianose, meletitose, maltotriose, cellotriose, and the like. And trisaccharides such as manninotriose. Examples of the monosaccharide include glucose, galactose, mannose, rhamnose, xylose, ribose, arabinose, glucosamine, galactosamine and the like.

In addition to the synthesis, it is also possible to extract from a plant containing the compound represented by the above general formula (1) with a suitable solvent and, if necessary, concentrate and dry it by a known method. As plants, Megurinoki, rhubarb and the like are well known.

The compound represented by the general formula (1) can be used alone or in combination of two or more as an agent for preventing obesity. In addition, when used in an anti-obesity food, the amount can not be specified unconditionally. For example, in foods and drinks and animal feeds, it is preferable to add 0.001 to 20% by mass. If the amount is less than 0.001% by mass, the effect of the present invention may not be exhibited. Even if the amount exceeds 20% by mass, the effect corresponding to the amount may not be obtained. Also, as pharmaceutical preparations, known binders, excipients, etc. can be added and taken orally in the form of powders, granules, tablets or capsules by a conventional method, or usual stabilizers and auxiliaries It can also be administered parenterally without injection as well. The compounding amount in this case is 0.001 to 50% by mass.

[0017]

EXAMPLES The present invention will be described in detail below with reference to examples and comparative examples, but the present invention is not limited to these examples.
In addition, the following anti-obesity action evaluation test was performed as an evaluation of the obesity prevention action.

[Evaluation test of anti-obesity effect using mice fed high-calorie diet] ICR mice (female, 5 weeks old at the start of test)
5 animals in one group, high fat diet or rhododendrol,
10 with high fat diet containing rhododendrol glucoside
They were bred for weeks (Table 1). A breeding group using a normal diet (solid feed MF, manufactured by Oriental Yeast Co., Ltd.) was used as a control. Food and drinking water were allowed to be freely ingested, and the amount of ingested food was measured. Measure the weight gain from the weight of the day before the start of the test and the last day,
The rate of weight gain per food intake (%) was calculated. On the last day of the test, the weight of the genital girth and the liver were measured, and the weight of the genital girth per food intake (mg / g)
And liver weight (mg / g) were calculated. Table 1 shows the results of the antiobesity agent evaluated by the above antiobesity evaluation test together with the diet composition.

[0019]

[Table 1]

From the above results, rhododendrol and rhododendrol glucoside showed a much lower rate of weight gain per food intake than that of the high fat diet group, and showed an increase in weight gain due to excessive energy intake by high calorie diet. It has been shown to be suppressed and to prevent obesity. In addition, the amount of peri-genital fat and liver weight, which are indicators of excess fat accumulation, were much lower than those in the high-fat diet group.

[0021]

EFFECT OF THE INVENTION It is apparent that the present invention can provide an obesity preventive agent which reduces systemic or local adipose tissue, suppresses or prevents obesity, and improves obesity.

Continued on the front page F term (reference) 4C086 AA01 AA02 EA08 MA01 MA04 NA14 ZA70 4C206 AA01 AA02 CA20 MA01 MA04 NA14 ZA70

Claims (1)

[Claims] [Claim 1] The following general formula (1) (Where R is a hydrogen atom, a monosaccharide or oligosaccharide residue).