JP2002053484A - Lipase inhibitor, and food and drink containing the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a medicine for inhibiting the activity of a lipase contributing the digestion and absorption of a lipid, and further to provide a food and drink containing the medicine. SOLUTION: This lipase inhibitor is characterized in that the lipase inhibitor contains a flower of peony or the essence of the flower as an active ingredient. The food and drink contains the lipase inhibitor.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a lipase inhibitor obtained from peony flower or peony flower extract, and to a food or drink containing the same.

[0002]

2. Description of the Related Art In recent years, obesity caused by westernization of dietary habits and chronic lack of exercise in Japan has become a serious problem as a risk factor for lifestyle-related diseases such as hypertension, heart disease and diabetes. These lifestyle-related diseases currently account for about 60% of the causes of death in Japanese people, and it is considered that preventing obesity is effective in treating and preventing them. Therapeutic agents for obesity caused by excessive nutritional intake include inhibitors of digestive enzymes such as lipase. Lipase is an enzyme that decomposes lipids. By inhibiting this, it is considered that the absorption of lipids in food is suppressed, and obesity can be prevented and treated.

[0003] As for substances having a lipase inhibitory action, tannins contained in feed plants [(British
J. Nutrition, 60, 275 (198
8)], tannins, flavonoids and glycosides thereof contained in leguminous crabs
No. 9557, JP-A-7-61927), triterpene compounds and derivatives thereof (JP-A-9-40689).
No.), lipase inhibitor consisting of water extract such as green pepper, pumpkin, shimeji, maitake, hijiki, green tea, black tea, oolong tea (Japanese Patent Application Laid-Open No. 3-219873), and epigallocatechin gallate which is a main component in green tea. Combined lipid absorption-suppressed food (JP-A-3-228664), an anti-obesity agent containing procyanidin as an active ingredient (JP-A-9-29)
No. 1039), but none of them are sufficient in terms of effect and safety.

On the other hand, shakuyaku is a kind of crude drug and has an analgesic and antispasmodic action. Its analgesic action (JP-A-6-199676)
No.), cancer metastasis inhibitory action (JP-A-7-258104)
No.), apoptosis inhibitory effect (JP-A-9-87187)
And whitening effect (JP-A-8-92056).

[0005]

SUMMARY OF THE INVENTION It is an object of the present invention to provide a drug which suppresses the action of lipase which contributes to the digestion and absorption of lipids, and a food and drink containing the same.

[0006]

Means for Solving the Problems As a result of diligent studies on the above-mentioned problems, the present inventors have found that an extract extracted from a peony flower has a lipase inhibitory action, and have completed the present invention.

The first aspect of the present invention relates to a lipase inhibitor comprising a peony flower or a peony flower extract as an active ingredient.

[0008] A second aspect of the present invention relates to a food or drink comprising the lipase inhibitor according to claim 1 or 2.

In Japanese Patent Application Laid-Open No. 64-90131,
It has been confirmed that the solvent extract of the herbal medicine and the plant extracts of the peony has the effect of inhibiting lipase derived from microorganisms. The effect has been confirmed,
In addition, the inhibitory effect of pancreatic lipase, not of microbial origin, has been confirmed.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION
It is a flower of a peony of the family of the button family or a related plant.
The mode of use of the flower can be used in any form, such as fresh, dried, dried powder or a solvent extract, and the use form is not limited.

For extracting the extract from the flower of the peony, water or an organic solvent such as methanol, ethanol, isopropyl alcohol, butanol, ethyl acetate, acetone, ether, chloroform or a mixed solution thereof may be used as a solvent. These are appropriately concentrated, purified, sterilized,
It can be used after drying.

The flower extract of peony can be formulated with commonly used carriers, auxiliaries, additives and the like, and used as a medicament as an oral product according to a conventional method. Pharmaceuticals include tablets, capsules, granules and syrups as oral preparations. When these products are administered to the human body as pharmaceuticals, 125 mg to 2.0 mg
00 mg / kg body weight, preferably 250 mg to 1,
If the dose of 000 mg / kg body weight is administered once or several times a day, the effect can be sufficiently exerted.

The medicament of the present invention can take the required unit dosage form together with physiologically acceptable vehicles, carriers, excipients, integrating agents, stabilizers, flavoring agents and the like. The adjuvants mixed with tablets and capsules are as follows. Binders such as tragacanth, gum arabic, corn starch, gelatin, excipients such as microcrystalline cellulose, corn starch, whole gelatinized starch, leavening agents such as alginic acid, lubricants such as magnesium stearate, Sweeteners such as sugar, lactose, saccharin, flavoring agents such as peppermint, reddish oil, and cherry. In the case of a capsule, the above-mentioned materials may further contain a liquid carrier such as oil and fat, and other materials may be used as a coating agent or to change the physical form of the preparation by another method. it can. For example, tablets may be coated with shellac, sugar. A syrup or elixir may contain sucrose as a sweetening agent, methyl or propylparabens as preservatives, a dye and flavoring such as cherry or orange flavor.

[0014]

Hereinafter, the present invention will be described with reference to examples.
The present invention is not limited thereby.

Example 1 (1) Preparation of Shakuyaku flower extract 200 g of dried peony flower powder was subjected to ultrasonic extraction with 70% methanol, concentrated under reduced pressure, lyophilized and then methanol extract 110
g was obtained. Further, the mixture was partitioned and extracted with water-saturated butanol, and the butanol layer was separated, concentrated under reduced pressure, and freeze-dried to obtain 26 g of a butanol fraction. Using these extracts, the following test (2) was performed. In general, when extracting an active ingredient from a natural product such as a crude drug, first, extract with water-containing methanol (usually using 70% methanol), and then extract with butanol to further concentrate the active ingredient from the obtained extract. Or use a more hydrophobic organic solvent. Therefore, when searching for an active ingredient, ethanol is not used from the beginning. In this embodiment, since it is freeze-dried, methanol and butanol are completely removed.

(2) Lipase Inhibitory Effect The lipase activity was measured by using 4-methylumbelliferone oleate (4-MUO) as a substrate and porcine pancreatic lipase as an enzyme. 4-MU) was measured. Mcl suspended 0.1 mM amount of 4-MUO
lvine buffer (adjusted to pH 7.4 with 0.1 M disodium hydrogen phosphate, 0.1 M citric acid) 100 μl
1, Mcll in which 4.5 μg of porcine pancreatic lipase was dissolved
100 μl of the Vine buffer and 5 μl of the test substance solution were mixed and reacted at 37 ° C. for 20 minutes. 0.1m hydrochloric acid 1m
The reaction was stopped by adding 1 l and the pH was adjusted to around 4.3 by adding 2 ml of 0.1 M sodium citrate. The fluorescence intensity of 4-MU produced by the reaction
nm and a fluorescence wavelength of 450 nm were measured with a fluorometer.

As a test substance for activity measurement, in addition to the substance obtained in Example 1, epicatechin gallate, which is one of polyphenols contained in teas and whose lipase inhibitory activity is known, is used as a comparative product. As a control, a test was performed in the same manner without the addition of a test substance. The inhibitory activity of each sample, the sample amount to half the activity of the control sample without addition (IC _{5 0}
Value).

As shown in Table 1, the substance obtained in Example 1 showed a stronger inhibitory activity than epicatechin gallate.

Table 1 Enzyme inhibitory activity (IC ₅₀ value) Inhibitory activity (μg / mL) Epicatechin gallate 118 Substance obtained in Example 1. 1.46

Example 2 (Tablets, Capsules) Extract obtained in (1) of Example 1 10.0 g Lactose 75.0 g Magnesium stearate 15.0 g Total 100.0 g Each of the above parts by weight is uniform To make tablets and capsules according to a conventional method.

Example 3 (Powder, Granule) Extract obtained in (1) of Example 1 20.0 g Starch 30.0 g Lactose 50.0 g Total 100.0 g The above parts by weight are uniformly mixed. Then, powders and granules were prepared according to a conventional method.

Example 4 (Injection) The extract obtained in (1) of Example 1 1.0 g Surfactant 9.0 g Physiological saline 90.0 g Total 100.0 g Heating the above parts by weight It was mixed and sterilized to give an injection.

Example 5 (candy) Sucrose 19.9 g starch syrup (75% solid content) 70.0 g water 9.5 g coloring agent 0.45 g flavoring agent 0.05 g Extraction obtained in (1) of Example 1 0.1 g in total 100.0 g In total, each component in the above parts by weight was used to make a candy according to a conventional method.

Example 6 (Juice) Concentrated tangerine juice 15.0 g Fructose 5.0 g Citric acid 0.2 g Flavor 0.1 g Colorant 0.15 g Sodium ascorbate 0.05 g Obtained in Example 1, (1) 0.1 g of the obtained extract 79.4 g of water 100.0 g in total 100.0 g A juice was prepared from the above components by weight in accordance with a conventional method.

Example 7 (Cookie) Soft flour 32.0 g Whole egg 16.0 g Butter 16.0 g Sugar 25.0 g Water 10.7 g Baking powder 0.2 g Extract obtained in (1) of Example 1 0 0.1 g in total 100.0 g A cookie was prepared according to a conventional method using each of the above components by weight.

[0025]

Industrial Applicability The present invention is a lipase inhibitor derived from a natural product, which is excellent in processing characteristics and highly safe for a living body.
Since this lipase inhibitor has an effect of suppressing lipid absorption, the lipase inhibitor of the present invention or food and drink containing the same is effective for prevention and treatment of obesity.

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Claims (3)

[Claims] 1. A lipase inhibitor comprising a peony flower or a peony flower extract as an active ingredient. 2. The lipase inhibitor according to claim 1, wherein the lipase is pancreatic lipase. 3. A food or drink comprising the lipase inhibitor according to claim 1 or 2.