JPH10262606A - Food composition having inhibitory action on lipase and medicine composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition having high safety, capable of controlling accumulation of lipid in vivo, consequently contributing to suppression and prevention of obesity by including a plant of the family Labiatae having inhibitory effects on lipase and/or an extracted oil of plant of the family Labiatae and a raw material of product. SOLUTION: This composition contains a plant of the family Labiatae [e.g. rosemary and ENNMEISOU (grass of Plectranthus rugosus)] and an extracted oil of plant of the family Labiatae alone or in a mixture as an active ingredient. The extracted oil of plant of the family Labiatae is preferably an extracted oil extracted with water and/or a polar organic solvent. The plant of the family Labiatae is preferably a plant belonging to the genus Rosmarius or Isodon. The plant of the family Labiatae is preferably rosemary, Isodon japonica, Isodon trichocarpus or Isodon sikokianus var. intermodius.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a highly safe food composition and a pharmaceutical composition having a lipase inhibitory effect. More particularly, the present invention relates to a food composition and a pharmaceutical composition containing a Labiatae plant (particularly, rosemary (mannan wax) or life-extending grass) or a Labiatae plant extract, thereby having a lipase inhibitory effect. Because pancreatic lipase is involved in the digestion and absorption of lipids in vivo, inhibition of pancreatic lipase using the food composition or pharmaceutical composition of the present invention suppresses lipid accumulation in the body and suppresses obesity And can be prevented.

[0002]

2. Description of the Related Art In recent years, Japanese meals have become remarkably westernized,
High calorie is progressing. In particular, excessive intake of lipids causes obesity, which is also called modern civilization disease.
Obesity is one of the social problems because it is closely related to various diseases such as hyperlipidemia, arteriosclerosis, and diabetes, and it is desired to provide a method for improving obesity.

[0003] As a method of improving obesity, diet and exercise therapy can be mentioned. However, diet and exercise regimens often result in transient weight loss. It is known that a temporary weight loss causes a rebound of body weight and may trigger various adult diseases, which is not preferable. Next, there is a method using a central appetite suppressant. However, it is known that a central appetite suppressant has side effects, and there is a problem in safety. Therefore, it is still desirable to provide a method for improving obesity more safely.

It is known that various plants contain various physiologically active ingredients. For example,
-44230 describes that herbal spices (especially rosemary and sage) have an antioxidant effect. Japanese Patent Application Laid-Open No. 2-304409 describes that extraction of a Labiatae plant (for example, rosemary and life-extinging grass) with an aqueous alcohol solution extracts many components including antibacterial substances. Japanese Patent Laid-Open No. 4
No. 13630 describes that extracts of rosemary and sage have an inhibitory effect on plaque formation of Streptococcus mutans, an oral microorganism involved in caries and plaque formation. However, these prior arts do not describe that Labiatae plants (especially rosemary) and their extracts have a lipase inhibitory effect.

[0005] In addition, prolonged life grass has been used in folk medicine since ancient times as a bitter stomach medicine. JP-A-1-172333
The publication describes that the life-prolonging grass (herbal medicine which is a dried product of Hioki-koi or Kurobana-hioki-koi) or an extract thereof has a specific bacteriostatic and bactericidal action against streptococcus streptococcus in vitro or in vivo. JP-A-59-5176 describes that some diterpenoid compounds contained in a dried above-ground extract of San Inoki sorghum have antitumor activity. JP-A-48-5911 describes a method for extracting a medically active ingredient from lentils of a Labiatae plant. The medical effect of the effective substance obtained by this method is described as a gastric secretion inhibitory effect. Japanese Patent Laid-Open No. 5-
Japanese Patent No. 310537 describes that an extract of Hioki koshi has an effect of preventing hair loss, hair growth and hair growth.
However, these prior arts do not describe that Lamiaceae plants (especially life-extending grasses) and their extracts have a lipase inhibitory effect.

As described above, it has not been known that a Labiatae plant or an extract thereof has a lipase inhibitory effect.

[0007]

DISCLOSURE OF THE INVENTION The present invention has been made to solve the above-mentioned problems, and in particular, relates to a pancreatic lipase which is a key to obesity in order to regulate the digestion and absorption of lipids in a living body. An object of the present invention is to provide a highly safe food composition and a pharmaceutical composition which exhibit an extremely high inhibitory effect and suppress the accumulation of lipids in the body by the pancreatic lipase inhibitory effect, thereby contributing to the suppression and prevention of obesity. Aim.

[0008]

Means for Solving the Problems In order to solve the above-mentioned problems, the present inventors inhibit pancreatic lipase, which is the first enzyme of digestion and absorption of lipids, in humans to suppress the accumulation of lipids in the body. As a result, they sought to find components that suppress and prevent obesity. As a result, it was found that Labiatae plants (especially rosemary and life-extending grasses) and their extracts have excellent lipase inhibitory effects.

That is, the present invention provides a Labiatae plant (eg, rosemary and life-extending grass) and a Labiatae extract.
Provided is a highly safe food composition and a pharmaceutical composition which can be contained alone or in combination as an active ingredient to suppress and prevent obesity.

The food composition of the present invention contains a Labiatae plant and / or a Labiatae plant extract, and the Labiatae plant and / or the Labiatae plant extract has a lipase inhibitory effect.

The pharmaceutical composition of the present invention contains a Labiatae plant and / or Labiatae plant extract, and the Labiatae plant and / or the Labiatae plant extract has a lipase inhibitory effect.

In a preferred embodiment, the Labiatae extract is an extract extracted with water and / or a polar organic solvent.

[0013] In a preferred embodiment, the Lamiaceae plant belongs to the genus Rosmarius or the genus Isodon.

In a preferred embodiment, the Lamiaceae plant is selected from the group consisting of rosemary, sprouts, sagebrush
Or Takakuma Hikikoshi.

[0015]

BEST MODE FOR CARRYING OUT THE INVENTION In the present specification, a "Labiatae plant" refers to a plant belonging to the Labiatae family. Lamiaceae plants are of the genus Mannerou (Rosmarius) and the genus Yamatta (Iso
gen). Rosemary (Rosmarius officinalis) is an example of a plant belonging to the genus Mannenuro. Further, in the present specification, “extended life grass” means a group of plants that are generally called endowed grass among the genus Yamaha. An example of a prolonged life grass is Hikiokoshi (Isodon
japonica), black clover (Isodon trichocarp)
us), Takakuma Hikikoshi (Isodon sikokianus var.
intermodius) and the like.

As a Labiatae plant, any part of a plant body may be used. When the Labiatae plant is rosemary, the above-ground part is preferred, and the foliage is even more preferred. When the Labiatae plant is a life-extending grass, the whole plant is preferred, and the foliage is more preferred. The Labiatae plant may be used as it is after being collected, or may be used after being subjected to drying treatment such as sun drying and shade drying. When the Lamiaceae plant is a life-extending grass, a commercially available crude drug “Enmei-so”, which is a dried product of the life-extending grass, can also be used.

The Labiatae extract is obtained by extracting the Labiatae plant with a solvent. The Labiatae plant to be extracted may be in any form, but is preferably cut or crushed strip or powder in terms of extraction efficiency. The method and means of solvent extraction are not limited. The Labiatae extract may be the extract itself obtained by solvent extraction, or a concentrated solution or a diluted solution obtained by concentrating or diluting the extract or evaporating the solvent in the extract. It may be a liquid, a dried product or a granule.

The solvent used for extracting the Labiatae extract is
It is water, an organic solvent, or a mixture of water and an organic solvent.
Examples of the organic solvent used for extraction include methanol, ethanol, n-propanol, acetone, ethyl acetate, ether, methylene chloride, chloroform, benzene, carbon tetrachloride, petroleum ether, and the like. preferable.

The extraction temperature is not particularly limited, and may be room temperature, but is preferably heated to reflux. The extraction time varies depending on the extraction temperature, but is usually 2 to 48 hours. After extraction,
After obtaining a crude extract by filtration or centrifugation, if necessary, post-treatment such as concentration, dilution or drying is performed to obtain an extract.

(Food composition) The food composition of the present invention contains at least one of a Labiatae plant and a Labiatae plant extract, and preferably contains a plant belonging to the genus Mannerou or the genus Yamatta, or an extract thereof. And more preferably, rosemary or life-prolonging grass or an extract thereof. The Labiatae plant or Labiatae plant extract may include a single species or a plurality of species.

In the food composition of the present invention, the dry weight is used for Labiatae plants and the solid content is used for Labiatae extracts, typically about 0.001% to about 99% by weight. Preferably from about 0.01% to about 50% by weight, more preferably from about 0.05% to about 20% by weight.

[0022] The food composition of the present invention further includes food ingredients commonly used in the art. Examples of food raw materials include lactose, dextrose, sucrose, sorbitol, mannitol, apple fiber, soy fiber, meat extract, black vinegar extract, gelatin, corn starch, honey, animal and vegetable fats and oils, and polysaccharides. The food composition of the present invention may contain one or more of these food ingredients.

The food composition of the present invention further comprises one or more components such as a lubricant, an emulsifier, a suspending agent, an antioxidant, a preservative, a sweetener and a flavoring agent in addition to the above-mentioned food ingredients. May be included. Further, it may further contain other active ingredients including water-soluble vitamins and oil-soluble vitamins. Those skilled in the art can easily select appropriate components that do not interfere with the lipase inhibitory effect of the Labiatae plant or Labiatae plant extract.

[0024] The food composition of the present invention is produced by a method well known in the art. The form of the food composition of the present invention is not particularly limited. Examples of the form of the food composition of the present invention include granules, tablet confectionery, jelly, candy, and beverages.

The food composition of the present invention is ingested as needed.

(Pharmaceutical composition) The pharmaceutical composition of the present invention contains at least one of a Labiatae plant and a Labiatae plant extract, and is preferably a plant belonging to the genus Mannerou or the genus Yamatta, or an extract thereof. And more preferably, rosemary or life-prolonging grass or an extract thereof. The Labiatae plant or Labiatae plant extract may include a single species or a plurality of species.

In the pharmaceutical composition of the present invention, the dry weight is used for Labiatae plants, and the solid content is used for Labiatae extracts, typically about 0.001% by weight to about 99% by weight. , Preferably from about 0.01% to about 50% by weight, more preferably from about 0.01% to about 20% by weight.

[0028] The pharmaceutical composition of the present invention further comprises a pharmaceutically acceptable carrier. Examples of carriers include lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia gum, calcium phosphate, alginate, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose derivatives, tragacanth, gelatin, syrup, methyl hydroxybenzoate. , Talc, magnesium stearate, water, mineral oil and the like. The pharmaceutical composition of the present invention may contain one or more of these carriers.

The pharmaceutical composition of the present invention comprises, as in the case of the above-mentioned food composition, a lubricant, an emulsifier, a suspending agent, an antioxidant, a preservative, a sweetener and a flavoring agent, and a water-soluble vitamin. And one or more other active ingredients, including oil-soluble vitamins and the like.

[0030] The pharmaceutical composition of the present invention is produced by a method well known in the art.

The form of the pharmaceutical composition of the present invention is not particularly limited. Examples of the form of the pharmaceutical composition of the present invention include external preparations such as ointments and patches; internal preparations such as tablets, pills, powders, syrups, emulsions, solutions, suspensions,
Examples include forms such as gelatin capsules; and forms such as injections and sprays. Pharmaceutical compositions in the form of injections, sprays and the like can be administered by transdermal, injection, intranasal routes and the like.

The Labiatae plant or Labiatae extract used in the pharmaceutical composition of the present invention is effective over a wide dosage range. Therefore, the daily dose of a Labiatae plant or Labiatae plant extract is typically about 0.01 to 1 kg body weight in terms of the solid content of the Labiatae plant extract.
mg to about 1000 mg, preferably about 0.1 mg to about 5 mg
00 mg, more preferably in the range of about 1 mg to about 200 mg. This dose is administered once or in several divided doses. The actual dose will be determined taking into account the age, weight and severity of the condition to be treated and the route of administration chosen.

[0033]

EXAMPLES Hereinafter, the present invention will be described in more detail by way of examples, but the present invention is not limited to the following examples.

Example 1 Preparation of rosemary extract [0034] To 320 kg of dried and chopped rosemary foliage, 1
0 times the volume of ordinary water (tap water) was added and digested at 95 ° C. or higher for 1 hour. After allowing to cool to 65 ° C., the mixture was centrifuged to obtain an extract. To the residue was added 8 volumes of ordinary water again, followed by digestion and centrifugation to obtain an extract. This extract was combined with the previous extract, concentrated under reduced pressure at 40 ° C., and concentrated extract 130
Liters were obtained. This extract was spray-dried to obtain 35 kg of rosemary extract.

Example 2 Production of a life-extending herbal extract To 320 kg of a life-prolonging grass (whole plant, crudely cut; manufactured by Takasago Pharmaceutical Co., Ltd.) sold as a crude drug, 10 times the amount of ordinary water was added, and 95 ° C.
This was digested for 1 hour. After allowing to cool to 65 ° C., the mixture was centrifuged to obtain an extract. To the residue was added 8 times the amount of ordinary water again,
Similarly, digestion and centrifugation were performed to obtain an extract. This extract was combined with the previous extract and concentrated under reduced pressure at 40 ° C. to obtain 130 liters of concentrated extract. This extract was spray-dried to obtain 38 kg of life-extended grass extract.

Example 3 Measurement of Lipase Inhibition Ratio of Rosemary Extract and Lifelong Grass Extract The lipase inhibition ratio of the rosemary extract and lifelong grass extract obtained in Examples 1 and 2 was measured. The lipase inhibition rate was determined using a lipase (manufactured by Sigma, derived from porcine pancreas,
50 μg / ml) and “Lipase Kit S” manufactured by Dainippon Pharmaceutical. The measuring method followed the manufacturer's instructions.

The measurement method is briefly described as follows. 300 μl of a sample aqueous solution containing 0.025% by weight or 0.01% by weight of the rosemary extract or the life-extended grass extract (control: 300 μl of water), 0.0%
80 μl of 5 mg / ml lipase, coloring solution (0.1 mg
1 ml of a buffer containing 5,5-'dithiobis (2-nitrobenzoic acid) / ml, and then add 20 μl of an esterase inhibitor (3.48 mg / ml of phenylmethylsulfonyl fluoride). These reaction solutions are kept at 30 ° C.
After heating for 5 minutes at 100 ° C., 100 μl of a substrate solution (6.69 mg / ml methyl capnol tributyrate + 5.73 mg / ml sodium dodecyl sulfate) was added, and the mixture was heated at 30 ° C. for 30 minutes.
React under dark conditions. Thereafter, 2 ml of a reaction stop solution is added to stop the enzyme reaction. A blind sample was prepared by adding a sample aqueous solution, a lipase, a coloring solution, and an esterase inhibitor, for 5 minutes at 30 ° C, and 30 minutes at 30 ° C.
After heating for 10 minutes and adding a reaction stopping solution,
Is added. 412n of each sample in the absorbance meter
Measure absorbance at m. The lipase activity value is calculated from the absorbance difference between the absorbance of the test sample and the corresponding absorbance of the blind sample (absorbance difference 0.001 = 0.147 IU / liter).

Using the obtained lipase activity value, the lipase inhibition rate was calculated by the following equation.

[0039]

(Equation 1)

FIG. 1 shows the lipase inhibition rates of the rosemary extract and the life-extending grass extract. The stippled bars indicate the rosemary extract, and the white bars indicate the life-extending grass extract. The horizontal axis represents the concentration (% by weight = (W / V)%), and the vertical axis represents the lipase inhibition rate (%). The rosemary extract showed 72% and 86% lipase inhibition at 0.025% and 0.1% by weight, respectively. On the other hand, the life-extending grass extract showed 54% and 79% lipase inhibition at 0.025% by weight and 0.1% by weight, respectively.

From the above results, it was confirmed that the rosemary extract and the life-extending grass extract have high lipase inhibitory effects.

Accordingly, in the present invention, "a plant or a plant extract having a lipase inhibitory effect" means at least about 30%, preferably about 50%, more preferably about 50% under the above conditions (0.025% by weight). A plant extract showing an inhibition rate of 70% or more, and a plant giving such an extract.

Example 4 Preparation of Food A Food A having the composition shown in Table 1 below was prepared using the rosemary extract and the life-extending grass extract as active ingredients.

[0044]

[Table 1]

After mixing the components in a fluidized-granulation apparatus, the mixture is sprayed with water to perform granulation, and dried at an air inlet temperature of 80 ° C.
I got

Example 5 Preparation of Food B Food B having the composition shown in Table 2 below was prepared using the life-extending grass extract as an active ingredient.

[0047]

[Table 2]

After sufficiently mixing the above components with 10 kg of water, the mixture was heated to 60 ° C. to form a paste. This is poured into 50 kg of soybean oil preheated to 70 ° C.,
The mixture was sufficiently mixed with a stirrer equipped with iris-type stirring blades (two pieces). After confirming that the paste was dispersed in the soybean oil, the mixture was cooled to 5 ° C., and then filtered to separate generated particles. After the obtained particles were washed with n-hexane and dried, microcapsules (food B) containing the above components were obtained according to a conventional method.

Example 6 Preparation of Tablet A tablet was prepared using the rosemary extract as an active ingredient and the components shown in Table 3 below.

[0050]

[Table 3]

Example 7 Preparation of Intravenous Formulation An intravenous formulation was prepared using the life-extending grass extract as an active ingredient and the components shown in Table 4 below.

[0052]

[Table 4]

Example 8 Administration of Food Compositions and Pharmaceutical Compositions and Results The foods or pharmaceutical compositions obtained in Examples 3 to 7 above were given to experimental animals such as rats and mice. Good results were also obtained with the pharmaceutical composition.

[0054]

Industrial Applicability According to the present invention, there are provided a highly safe food composition and a pharmaceutical composition capable of suppressing or preventing obesity, comprising a rosemary extract or a life-prolonging grass extract as an active ingredient. You. Furthermore, the Labiatae plant or its extract can also be used to prevent food deterioration and odor caused by lipase.

[Brief description of the drawings]

FIG. 1 is a graph showing the lipase inhibition rates of a rosemary extract and a life-extending grass extract.

Claims (5)

[Claims] A food composition comprising a Labiatae plant and / or a Labiatae plant extract and a food material, wherein the Labiatae plant and / or the Labiatae plant extract has a lipase inhibitory effect. Food composition. 2. The food composition according to claim 1, wherein the Labiatae extract is extracted with water and / or a polar organic solvent. 3. The Lamiaceae plant is of the genus Mannerou (Ro)
The food composition according to claim 1, which belongs to the genus Smarius or the genus Yamadona (the genus Isodon). 4. The food composition according to claim 1, wherein the Labiatae plant is any one of rosemary, hinoki, kurobana hirokoshi, and takakumakioki. 5. A pharmaceutical composition comprising a Labiatae plant and / or a Labiatae plant extract and a pharmaceutically acceptable carrier, wherein the Labiatae plant and / or the Labiatae plant extract is a lipase. A pharmaceutical composition having an inhibitory effect.