WO2005099734A1

WO2005099734A1 - Lipase inhibitor containing water extract from leaf of hardy rubber tree

Info

Publication number: WO2005099734A1
Application number: PCT/JP2004/013945
Authority: WO
Inventors: Kazuyo Tanabe; Tetsuya Hirata
Original assignee: Kobayashi Pharmaceutical Co., Ltd.
Priority date: 2004-03-31
Filing date: 2004-09-24
Publication date: 2005-10-27
Also published as: JP4979184B2; JP2005289950A

Abstract

[PROBLEMS] To provide an effective means for the prevention of or treatments for diseases attributable to lipase activity and to provide a lipase inhibitor, fat absorption inhibitor, fat accumulation inhibitor, medicinal composition, food and beverage, and cosmetic preparation which each can be the means for treatments. [MEANS FOR SOLVING PROBLEMS] The lipase inhibitor comprises a powder of leaves of hardy rubber trees or an extract therefrom obtained with water. The medicinal composition, food, beverage, cosmetic preparation, etc. have a lipase inhibitory effect.

Description

Specification

Lipase inhibitor containing Tochu leaf extract

Technical field

[0001] The present application relates to a lipase inhibitor, a fat accumulation inhibitor, and a fat absorption inhibitor containing a Tonaka leaf component, particularly a Tonaka leaf water extract. Furthermore, the present invention relates to a composition for oral ingestion, a food and drink, a pharmaceutical composition, a food composition, a cosmetic and the like containing the lipase inhibitor, fat accumulation inhibitor or fat absorption inhibitor.

Background art

[0002] Obesity is a condition in which adipose tissue is excessively accumulated, and a condition that requires medical treatment especially for obesity is called "obesity". Obesity is a risk factor for diseases such as diabetes, hypertension, and hyperlipidemia, and in recent years, the increase in patients with the above diseases accompanied by obesity has become a problem. As one of the effective means for treating obesity, attention has been paid to the suppression of fat absorption by inhibiting ribose in vivo.

[0003] Spleen lipase, one of the major digestive enzymes of long-chain triglycerides (triacylglycerols) in ingested food, adds ester bonds at the 1st and 3rd positions of triacylglycerol. Catalyzes water splitting. The fatty acids and monoacylglycerol thus formed are absorbed into the digestive tract and then converted back to triacylglycerol. Triacylglycerol, which is transported to each tissue through the blood, consumes more fat than fat, which is consumed as energy. Focusing on the role of spleen lipase in such a mechanism of fat absorption and accumulation in vivo, attempts have been made to inhibit fat absorption by administering an inhibitor of spleen lipase. However, there is no case in which a lipase inhibitor for treating obesity has been used clinically to date.

[0004] Microbial lipases are known to be involved in specific skin diseases. That is, when sebum accumulates due to hyperplasia of sebaceous glands and hyperkeratosis of hair follicles, acne bacilli and staphylococci, which are resident bacteria in the hair follicle of the hair follicle, grow, These lipases constitute sebum and degrade triacylglycerol to produce free fatty acids. This free fatty acid acts on the epithelium to produce various enzymes, It is said to be a factor such as flame and dandruff (see Non-Patent Document 1). Therefore, if the microbial lipase could be inhibited, it would be possible to provide a therapeutic / preventive means for a specific skin disease caused by the lipase.

[0005] Naturally derived foods and herbal medicines generally have advantages such as fewer side effects, and therefore, their usefulness against various intractable diseases whose incidence has increased in recent years has attracted attention. Regarding the above-mentioned lipase-related diseases, a search is made for substances having a lipase activity inhibitory effect in food components derived from natural products (see Patent Documents 1 and 2).

[0006] Eucommia ulmoides oliver is a deciduous woody tree classified as a genus Eucommia genus Eucommia genus from central China, and is a high tree with a height of 20 m. Compared to the Camellia plant, which is generally called tea, Tonaka also has a different power content that does not contain any caffeine. For example, the leaves and bark of Tonaka contain a component that draws white thread when pulled. This is hardly observed in trees distributed in the temperate zone! Trans-polymer isoprenoid A substance called "Guptapel force". Tonakayo has been widely used as a beverage since the 1980s. Tochu's skin is treated as a medicine, and in China it is used as an effective herbal medicine for hypertension, low back pain, arthralgia, kidney disease, liver disease, stress, decreased energy, diuresis, and forgetfulness.

[0007] Several reports have been made on the investigation of the lipase inhibitory activity of the components of Tochu-yoha. V, Ru, but reports of Tochu-yoha components having sufficient inhibitory activity have not yet been made. References 3 and 4).

[0008] In addition, in the production of normal Tonaka tea leaves, processes such as sun drying and roasting are included, so that components originally contained in raw Tonaka leaves may be lost in this process. Little was known about the bioactivity of the components. Furthermore, even if it is a component that is stable in roasting and other processes, it is hardly contained in the water extract when it is extracted with water from Tonaka leaf, which is usually used as tea leaves, and some components remain in Tonaka leaf. Very little was known about the physiological activity of such components.

Patent Document 1: JP-A-2002-97147

Patent Document 2: Japanese Patent Application Laid-Open No. 2001-321166 Patent Document 3: JP 2002-179586 A

Patent document 4: JP 2002-275077 A

Non-Patent Document 1: "Shin-Dai Cosmetics", Takeo Mitsui, pp. 29-30, Nanzando, Tokyo, 1993. Disclosure of the invention

Means for solving the problem

[0009] The present inventors have conducted intensive studies to solve the above-mentioned problems. As a result, crushed Tonaka leaf prepared by a specific method, and an aqueous extract obtained therefrom were used as lipase inhibitors. The present inventors have discovered that they have a fat accumulation inhibitor and a fat absorption inhibitor, and have completed the present invention.

[0010] It is an object of the present invention to provide a crushed Tonaka leaf and an aqueous extract having lipase inhibitory activity, fat accumulation inhibitory activity, and fat absorption inhibitory activity, and a lipase inhibitor containing the milled or water extract. To provide. Further, an object of the present invention is to provide a composition for oral ingestion, a composition for transdermal absorption, a pharmaceutical composition, a food composition, a food and a drink, comprising the lipase inhibitor, fat accumulation inhibitor, or fat absorption inhibitor. As well as providing cosmetics.

[0011] That is, according to one aspect of the present invention, a step of steaming the Tonaka leaves; a step of kneading the Tonaka leaves; a step of drying the Tonaka leaves; a step of roasting the Tonaka leaves; And a water extract of Tonaka leaf obtained by a production method comprising a step of concentrating the extract. The extract may be a powder.

[0012] According to another aspect of the present invention, there is provided a lipase inhibitor comprising the above extract of Tochu leaf water extract.

[0013] According to another aspect of the present invention, there are provided foods, drinks, pharmaceutical compositions, and cosmetics containing the lipase inhibitor.

[0014] Further, according to another aspect of the present invention, there is provided a fat absorption inhibitor comprising the above extract of Tochu leaf water extract.

[0015] According to another aspect of the present invention, there is provided a food, drink, cosmetic, or pharmaceutical composition containing the above-mentioned fat absorption inhibitor.

[0016] Further, according to another aspect of the present invention, fat accumulation suppression containing the above extract of Tochu leaf water extract An agent is provided.

[0017] According to another aspect of the present invention, there is provided a food, drink, cosmetic, or pharmaceutical composition containing the fat accumulation inhibitor.

[0018] According to still another aspect of the present invention, the step of steaming the Tochu leaf; the step of kneading the Tochu leaf; the step of drying the Tochu leaf; the step of roasting the Tochu leaf; and the step of extracting the Tochu leaf with water And a method for producing an extract of Tochu foliage extract, comprising a step of concentrating the extract.

[0019] Further, according to another aspect of the present invention, the method for producing the above-mentioned Tochu leaf water extract, wherein the Tochu tea water extract is a concentrated extract having a volume ratio of 5 to 8% with respect to the original extract. Is also provided.

[0020] Further, according to another aspect of the present invention, the extraction temperature in the step of extracting Tochu leaves with water is 80-100 ° C; the extract is allowed to stand at 0-10 ° C before being concentrated. And removing the resulting precipitate; and further comprising a step of centrifuging the extract at a g value of 680 to 840 g for 20 to 30 minutes after the step of concentrating the extract to remove the precipitate. Is done.

Hereinafter, the present invention will be described more specifically.

The eucommia leaf in the present invention means eucommia leaf after harvest and before drying, and may be produced by cultivation or collected from nature. For example, fresh leaves before the fall of the current year may be used, and fresh leaves may be collected from April to October, preferably from May to August, and more preferably from July to August.

[0022] In the present invention, the step of steaming the Tonaka green leaves can be carried out using a commercially available steaming machine or an autoclave according to a method generally performed in the art. For example, it is possible to steam-treat the eucalypt leaf by spreading the eucalypt leaf on a net conveyor and passing it through a processing chamber filled with no-pressure steam supplied from the boiler. Although the steaming temperature is not particularly limited, it is appropriately selected, for example, in the range of 90 to 120 ° C, preferably 95 to 110 ° C, and more preferably 100 to 110 ° C, depending on the size of Tochu leaf. sell. Also, the steaming time can be appropriately selected in the range of 10 to 240 seconds, preferably 20 to 180 seconds, more preferably 20 to 120 seconds. The amount of steam to be used is, for example, 200-70 LZ Or 170-lOOLZ minutes. The treatment amount of the steamed leaves is not particularly limited according to the moisture content of the fresh leaves, but may be appropriately selected, for example, within a range of 3 to 10 kgZ, preferably 418 kgZ, more preferably 5 to 7 kgZ. In this steaming step, the components of the Tonaka leaves are easily retained by inactivating the enzyme that turns the Tonaka leaves to brown; and the softening of the Tonaka leaves makes the subsequent kneading process easier. And so on.

[0023] The kneading step in the present invention can be performed using, for example, a commercially available kneading machine, coarse kneading machine or medium kneading machine. For example, as a commercially available kneading machine, a kneading machine 60 kg type manufactured by Terada Seisakusho Co., Ltd. can be used. By this step, the water in the Tonaka leaves is evenly adjusted while removing excess water, and the components unique to Tonaka can be easily extracted. This step is performed without heating, if necessary. Although the time required for this step is not particularly limited, it can be appropriately selected, for example, within the range of 10 to 80 minutes, preferably 20 to 60 minutes, and more preferably 25 to 30 minutes. The amount of kneaded leaves to be treated is not particularly limited, but may be appropriately selected in the range of, for example, 25 to 40 kg, preferably 30 to 35 kg, more preferably 32 to 33 kg, depending on the moisture content. The water content of Tochu leaves obtained through this step is, for example, 25 to 40%, preferably 25 to 35%, more preferably 25 to 30% on a dry basis.

[0024] The step of drying the Tonaka leaf of the present invention can be performed, for example, by exposing to sunlight. Here, the time of exposure to the sun is not particularly limited, but can be appropriately selected, for example, in the range of 96 to 120 hours, preferably 96 to 114 hours, more preferably 96 to 102 hours. Further, the drying step can be performed using a commercially available dryer. The method of drying with a dryer is not particularly limited, but it can be performed by, for example, a dryer ND120 manufactured by Terada Seisakusho Co., Ltd. Here, the temperature of the hot air is not particularly limited, but a force in a range of, for example, 70 to 100 ° C, preferably 85 to 95 ° C may be appropriately selected. Although the time required for this step is not particularly limited, it can be appropriately selected in the range of 5 to 80 minutes, preferably 10 to 80 minutes, more preferably 20 to 80 minutes. Although the water content of Tonaka leaf obtained through this step is not particularly limited, for example, the water content is 5% or less, preferably 3% or less, more preferably 2% or less. [0025] The step of roasting Tonaka leaf of the present invention is not particularly limited, but can be performed using, for example, a commercially available roasting machine. The roasting method in this step is not particularly limited. For example, the roasting method can be performed by a hot-air rotary drying burner manufactured by Yokoyama Seisakusho Co., Ltd. The time required for this step is not particularly limited, but may be appropriately selected in the range of 30 to 50 minutes, preferably 30 to 45 minutes, more preferably 35 to 40 minutes. The roasting temperature in this step is not particularly limited, but may be appropriately selected within a range of, for example, 100 to 140 ° C, preferably 120 to 140 ° C, and more preferably 130 to 140 ° C. The water content of Tonaka leaf obtained through this step is, for example, 8% or less, preferably 4% or less, more preferably 2% or less on a dry basis.

[0026] In the step of obtaining the water extract of Tochu tea leaves of the present invention, for example, 5 to 50 kg, preferably 10 to 30 kg, more preferably 15 to 20 kg of water is added to 1 kg of Tochu tea leaves in an amount appropriately selected. Can be used. The extraction temperature can be appropriately selected, for example, from the range of 85 to 98 ° C, preferably 90 to 95 ° C. Although the extraction time is not particularly limited, for example, a force of 10 to 120 minutes, preferably 20 to 90 minutes, more preferably 30 to 60 minutes can be appropriately selected.

[0027] The extraction liquid can be filtered using, for example, a 30-200 mesh filter.

The filtrate may be allowed to stand for a certain period of time before concentration. Unnecessary substances can be removed by removing the precipitate generated by standing still. The standing time is not particularly limited, but may be appropriately selected from, for example, one to twenty-four hours, preferably six to twenty hours, and more preferably eight to eighteen hours. Although the temperature at the time of standing is not particularly limited, for example, a force of 0 to 35 ° C, preferably 0 to 16 ° C, and more preferably 2 to 8 ° C may be appropriately selected.

[0028] Concentration of the extract obtained as a filtrate can be carried out by using a force usually used in the art, such as a rotary evaporator. The concentration step is carried out under reduced pressure conditions, for example, which can be appropriately selected from the range of 20 to 140 mmHg, preferably 30 to 120 mmHg, more preferably 40 to 100 mmHg, for example, 30 to 80 ° C, preferably 35 to 70 ° C, Preferably, the reaction can be performed at a temperature that can be appropriately selected from the range of 40 to 60 ° C. In the concentration step, the concentration is reduced to, for example, 5 to 8%, preferably 5.6 to 7.5%, more preferably 6 to 6.6% by volume ratio with respect to the initial extract.

[0029] The obtained concentrate can be used as it is as the Tochu leaf water extract solution of the present invention. However, treatments such as centrifugation and heat sterilization can also be performed. The centrifugation can be performed using a commercially-available centrifuge by a method commonly used in the art. For example, a batch type centrifugal separator, a flow chamber type centrifugal separator, a decanter type centrifugal separator, a tubular centrifuge, or the like can be used. The conditions for centrifugation are not particularly limited. For example, in the case of a batch type centrifugal machine, the number of rotations is 1000 to 3100 rpm, preferably <1500 to 2500 rpm, more preferably <1800 to 2000 rpm; for example, 210 to 2010 g, preferably Is a g value of 470 to 1310 g, more preferably 680 to 840 g; and, for example, a treatment time appropriately selected from a treatment time of 10 to 60 minutes, preferably 15 to 40 minutes, more preferably 20 to 30 minutes. . When a continuous-pass centrifuge is used, it can be carried out under conditions appropriately selected from 100 to 400 mesh, preferably 150 to 350 mesh, and more preferably 200 to 300 mesh. The supernatant after centrifugation is collected by a water feeder, filtration with diatomaceous earth as a filter aid, or the like.

[0030] Heat sterilization is performed, for example, by heating to 75-100 ° C, preferably 80-95 ° C, more preferably 85-90 ° C. The processing time for heat sterilization can be appropriately selected, for example, in the range of 60 to 240 minutes, preferably 90 to 220 minutes, more preferably 120 to 180 minutes.

[0031] The concentration ratio of the obtained Tochu leaf extract extract is, for example, 5 to 7.5%, preferably 5.5 to 7%, more preferably 6 to 6 by volume ratio to the original extract. 5%, e.g. 6.5% Ge-poside acid content of the obtained Tochu leaf water extract solution is 6-40 mg / g, preferably 15 mg / g-40 mg / g, more preferably 28-37 mg. / g, for example 30 mg / g.

[0032] The concentrated extract liquid is dried by a method commonly used in this technical field such as spray drying or freeze drying to obtain a powdery extract of Tochu leaf water extract. After the roasting step, the extract powder is obtained, for example, in an amount of 200 to 600 g, preferably 200 to 400 g, from 1 kg of Tonaka leaf before water extraction. The Ge-posidic acid content of the obtained powdered extract of Tochu leaf water extract is 40-100 mg / g, preferably 50-90 mg / g, more preferably 60-80 mg / g, for example 77 mg / g. The content of the eucommia leaf glycoside in the obtained eucommia leaf extract powder is 30-60 mg / 100 g, girls or 35-55 mg / 100 g, J-girls is 40-50 mg / 100 g, for example, 47 mg / 1. OOg. [0033] As used herein, the term "lipase inhibitor" refers to, but is not limited to, a compound that inhibits an enzymatic reaction that produces triacylglycerol-free fatty acids. As used herein, “lipase” includes all enzymes having lipase activity. Examples of the lipases inhibited by the lipase inhibitor of the present invention include lipases related to fat absorption in the digestive tract of spleen lipase, and microorganisms propio-bacterium acnes, Pitilosporum ova, which are resident in skin epidermis. Lipases produced by bacteria indigenous to the skin, such as Nori (Pityrosporum ovale) and Micrococcus sp. A lipase of particular interest is spleen lipase.

[0034] As used herein, the term "fat absorption inhibitor" is not particularly limited. For example, it refers to a compound that suppresses the absorption of neutral fats such as intestinal tract, and includes, for example, digestion of lipase and the like. A lipase inhibitor that inhibits fat absorption by inhibiting an enzyme is included.

[0035] As used herein, the term "fat accumulation inhibitor" is not particularly limited, and for example, suppresses fat accumulation in a living body by suppressing absorption of neutral fat in intestinal tract power. A compound, a compound that suppresses the differentiation or proliferation of fat cells, and a compound that suppresses the uptake of neutral fat into fat cells due to maturation or enlargement of fat cells. Fat accumulation inhibitors include, for example, lipase inhibitors, fat absorption inhibitors and the like.

[0036] The lipase inhibitor, fat absorption inhibitor and fat accumulation inhibitor of the present invention are not particularly limited, but may be other fat absorption inhibitors, other therapeutic or prophylactic agents for obesity, and antilipidemic agents. It can be used together with prophylactic and therapeutic agents, and therapeutic or prophylactic agents such as obesity that may be a risk factor, for example, diabetes, hypertension. Diseases that can be cured by lipase inhibitors include arteriosclerosis, myocardial infarction, and fatty liver.

[0037] The lipase inhibitor, fat absorption inhibitor and fat accumulation inhibitor of the present invention can be used as an active ingredient of a pharmaceutical composition. The pharmaceutical composition may be in various dosage forms, for example, for oral administration, tablets, capsules, powders, granules, pills, solutions, emulsions, suspensions, solutions, spirits, syrups, Extracts, elixirs and the like can be used, for example, creams, jellies, gels, pastes, ointments and the like for topical administration, but are not limited to these. The pharmaceutical composition contains various commonly used components. May include, for example, one or more pharmaceutically acceptable excipients, disintegrants, diluents, lubricants, flavoring agents, coloring agents, sweetening agents, flavoring agents, suspending agents It may contain agents, wetting agents, emulsifiers, dispersants, adjuvants, preservatives, buffers, binders, stabilizers, coatings and the like. The pharmaceutical composition of the present invention may be in a sustained or sustained release dosage form.

[0038] The dosage of the lipase inhibitor, fat absorption inhibitor and fat accumulation inhibitor of the present invention can be appropriately selected depending on the patient's body type, age, physical condition, degree of disease, elapsed time after onset, and the like. The pharmaceutical compositions of the present invention can include a therapeutically effective amount and a Z or prophylactically effective amount of a lipase inhibitor, a fat absorption inhibitor, and a fat accumulation inhibitor. For example, it is generally used as the pulverized woody leaf of the present invention or an aqueous extract thereof at a dose of 10 to 50,000 mg / day / adult, preferably 100 to 5000 mg / day Z adult. The pharmaceutical composition may be administered in a single dose or in multiple doses, for example, by being used in combination with other agents such as other lipase inhibitors, fat absorption inhibitors and fat accumulation inhibitors. Monkey

[0039] The food and drink of the present invention include liquid beverages such as functional beverages, and functional foods. The food composition can be used as a quasi-drug, other ingredients such as food and drink, a food additive, and the like. In addition, the composition for oral ingestion in the present specification can be used as a functional food as it is, and can also be used as a pharmaceutical, a quasi-drug, a component of food and drink, a food additive, and the like. The use enables daily and continuous ingestion of the food composition or the composition for oral ingestion having the lipase inhibitory effect, the fat absorption inhibitory effect, and the fat accumulation inhibitory effect of the present invention, and effective fat absorption. The suppression effect enables treatment and prevention of obesity.

[0040] Furthermore, the presence of the lipase inhibitor in the food suppresses the hydrolysis of fat contained in the food by the lipase derived from microorganisms, and prevents the deterioration of the food caused by free fatty acids, Food quality can be maintained for a long time. Therefore, according to still another aspect of the present invention, there is also provided a food preservative comprising the water-extracted extract produced by the above method.

Examples of foods or beverages containing the lipase inhibitor, fat absorption inhibitor and fat accumulation inhibitor of the present invention include functional foods having a lipase inhibitory effect or an obesity inhibitory effect. Foods, health foods, general foods (juices, confectionery, processed foods, etc.), dietary supplements (nutrition drinks, etc.). Foods or beverages in the present specification include, but are not limited to, other than pulverized tobacco leaves or an aqueous extract of the pulverized substances, inorganic components such as iron and calcium, various vitamins, oligosaccharides and chitosan. It can include dietary fiber, proteins such as soy extract, lipids such as lecithin, and sugars such as sucrose and lactose.

[0042] Cosmetics containing the lipase inhibitor, fat absorption inhibitor and fat accumulation inhibitor of the present invention are not particularly limited, and include, for example, emulsions, cosmetics, face creams, hand creams, lotions, shampoos, rinses and the like. including.

The invention's effect

As shown in the following examples, the present invention has a lipase inhibitory action, a blood neutral fat lowering action, and a fat accumulation inhibitory action. Thus, the present invention provides an effective means for treating and / or preventing or preventing diseases caused by lipase activity, blood triglyceride and fat accumulation.

Brief Description of Drawings

FIG. 1 shows an example of the results of a spleen lipase activity inhibition test on a pre-distribution Tochu leaf extract solution.

[Fig. 2] Fig. 2 shows an example of test results on the effect of suppressing the serum triglyceride content of Tochu tea leaves and Tochu leaf extract solution for early delivery.

[Fig. 3] Fig. 3 shows an example of a test result on the effect of suppressing the serum triglyceride amount of the Tochu leaf extract solution for early delivery.

[4] This shows an example of test results on the effect of suppressing the weight of adipose tissue and the effect of suppressing the body fat percentage for Tochu tea leaves and Tochu leaf extract liquid for early delivery.

FIG. 5 shows an example of test results of an adipose tissue weight-inhibiting effect and a body fat percentage-inhibiting effect with respect to the early release Tochu leaf extract solution.

[Fig. 6] Fig. 6 shows an example of test results of the effect of suppressing weight gain with respect to Tochu tea leaves and Tochu leaf extract for early delivery.

BEST MODE FOR CARRYING OUT THE INVENTION

Hereinafter, the present invention will be described in further detail with reference to the preferred embodiments of the present invention. However, the present invention is not limited to the embodiment.

Example 1 Preparation of Tochu Tea Leaves Extract for Early Delivery

[0047] (1) Manufacture of Tochu tea leaves for early delivery

Manufacture of wood tea leaves for early delivery was carried out based on the description in Example 2 of JP-A-8-173110. 5 kg of fresh leaves of Tonaka were steamed at 110 ° C for 90 seconds by a feeding steamer for Japanese tea production. Fresh leaves were put into the machine through the inlet of the steamer, and steam was applied from the upper and lower steam supply devices while moving on the conveyor, and steamed at 110 ° C for 90 seconds. By spreading eucommia leaves on a net com- parator and passing them through a treatment room filled with unpressurized steam supplied by boiler power, eucommia leaves can be steam-heat treated. For example, a leaf feeding machine manufactured by Takamura Iron Works Co., Ltd., a ground-type 1500, a net conveyor, and a belt-feeding type 1000 can be used.

Next, the steamed Tonaka leaves were kneaded with a kneader for 30 minutes, and the kneaded material was dried with a dryer at 80 ° C for 5 hours to a water content of 5%. The color tone of Tochu leaves changed from brown to green after steaming to blackish brown with greenish color as it dried. Then, it was roasted at 110 ° C for 30 minutes using a stir-fryer (IR-10SP type: Terada Seisakusho) to obtain 2 kg of early-brewed Tochu tea leaf sample.

(2) Preparation of Tochu Tea Leaves Extract for Early Delivery

A sample of lkg of Tochu tea leaves for early delivery was poured into 15kg of hot water at 90 ° C, and 14kg was extracted at 90 ° C for 30 minutes. Thereafter, the mixture was filtered using a 150-mesh filter, and the filtrate was cooled to 5 ° C and left overnight. The supernatant was taken out and the filtrate was concentrated under reduced pressure at 50 ° C to obtain 1 kg.

The concentrated solution is treated with a centrifuge KS8000 manufactured by Kubota Corporation, the precipitate is removed by centrifugation at a rotation speed of 1800 rpm, and the obtained supernatant is sterilized by heating (85 ° C, 2 hours). An extract of Tochu leaf water extract for early delivery was obtained. The concentrated extract was dried by a spray-drying method to obtain a powder (300 g) of the extract of Tochu leaf water extract for early delivery as a brown powder.

[Comparative Example 1] Preparation of Tochu tea leaf extract for cooking

[0050] Tochu tea leaves for boiling out were produced by a conventionally performed method. Tonaka leaves are dried in the sun until the moisture content is reduced to 11% or less, and crushed by a pulverizer (Horai UGC-280). Grinding was carried out until the size became below the sieve. After that, it was roasted at 140 ° C-170 ° C for 20 minutes using a roasting machine (Yokoyama Seisakusho automatic exhaust air drying and burning machine 80 kg) to obtain Tonaka tea leaves for cooking. An aqueous extract was prepared from the tea leaves in the same manner as in Example 1, (2) Preparation of early-leaving Tochu tea leaves extract.

[Example 2] In vitro lipase inhibitory activity test

[0052] In preparing the test substance, the ready-to-use extract or the extract for boiling was prepared using 0.1M TES buffer (pH 7.0) containing 0.1M NaCl to reach final concentrations of 1, 5, 10, and 20mgZmL. It adjusted so that it was a sample liquid. The substrate solution was prepared by using 80 mg of triolein, 10 mg of phosphatidylcholine and 5 mg of sodium taurocholate which had been subjected to ultrasonic treatment in 9 mL of a 0.1 M buffer, and used as a substrate solution. As the enzyme solution, a lipase derived from pig spleen adjusted to a final concentration of 4 gZmL with a 0.1 M TES buffer was used. Lipase activity is measured by adding 50 L of enzyme solution and 50 / zL of sample solution to 100 L of substrate solution, reacting at 37 ° C for 30 minutes, and measuring the amount of released fatty acids using a commercially available kit (Wako Pure Chemical, NEFA Quantification was performed using C-test (1).

The results are shown in Figure 1. The concentration-dependent inhibitory effect of spleen lipase was confirmed by the addition of the extract for rapid release. In addition, the inhibitory effect was much higher than when the extract for boiling was added.

[Example 3] Evaluation test for serum triglyceride lowering action and fat accumulation inhibitory action

[0054] ICR female mice were fed a high fat diet containing beef tallow and Tonaka leaf, and the effects on the amount of neutral fat in blood, adipose tissue weight, and body weight were examined. The roasted Tochu tea leaves (Tochu tea leaves) manufactured in Example 1 after roasting were 10% (w / w), and the Toasting Tochu leaves were 2.5, 5, 7.5 and 10%. % (wZw) was added to the feed and ingested.

Specifically, randomly selected ICR female mice (4 weeks old, weighing 20-25 g) were divided into three groups (six in each group). The first group was administered with Tonaka tea leaves, and the second group was administered with feed containing early-release Tochu leaf extract and 40% beef tallow for 4 weeks (Tonaka tea leaves group, early-release Tochu leaves extract group). The mice in the third group were administered a diet containing only 40% tallow for 4 weeks as a negative control (control group). During the test, rats were allowed food and water ad libitum. Four weeks after the administration of the above feed, the body weight was measured and the mice were killed by ether anesthesia, blood was collected from the abdominal vena cava, and the neutral fat in the serum was measured. Neutral fat in serum was measured using Triglyceride E-Test II. After laparotomy, the weight of adipose tissue around the genitals was measured by weighing.

FIGS. 2 and 3 show the results of the evaluation test for the serum triglyceride lowering effect. It was confirmed that the intake of Tochu tea leaves and Tochu leaves extract significantly reduced the serum triglyceride level.

FIGS. 4 and 5 show the results of the evaluation test of the inhibitory effect on fat accumulation. Significant suppression of fat accumulation was confirmed in the groups receiving the Tochu tea leaves and the Hayashi Tochu leaves extract.

FIG. 6 shows the measurement results of weight change. In particular, a significant suppression of weight gain was confirmed in the group in which the Takenaka leaf extract was used.

Claims

The scope of the claims

[I] A Tonaka leaf water extract obtained by a production method comprising the steps of steaming Tonaka leaves; extracting Tonaka leaves with water; and concentrating the extract.

[2] The extract of Tochu leaf water extract according to claim 1, which is a powder.

[3] A lipase inhibitor comprising the extract of Tochu leaf water extract according to claim 1 or 2.

[4] A food and drink comprising the lipase inhibitor according to claim 3.

[5] A pharmaceutical composition comprising the lipase inhibitor according to claim 3.

[6] A cosmetic comprising the lipase inhibitor according to claim 3.

[7] A fat absorption inhibitor comprising the extract of Tochu leaf water extract according to claim 1 or 2.

[8] A food or drink comprising the fat absorption inhibitor according to claim 7.

[9] A pharmaceutical composition comprising the fat absorption inhibitor according to claim 7.

[10] A cosmetic comprising the fat absorption inhibitor according to claim 7.

[II] A fat accumulation inhibitor comprising the extract of Tochu leaf water extract according to claim 1 or 2.

[12] A food or drink comprising the fat accumulation inhibitor according to claim 11.

[13] A pharmaceutical composition comprising the fat accumulation inhibitor according to claim 11.

[14] A cosmetic comprising the fat accumulation inhibitor according to claim 11.

[15] A method for producing an extract of Tochu leaf water, comprising the steps of steaming Tochu leaf; extracting the Tochu leaf with water; and concentrating the extract.

[16] The method for producing a Tochu foliage extract according to claim 15, wherein the extract of Tochu foliage is a concentrated extract having a volume ratio of 5 to 8% with respect to the initial extract.

[17] The extraction temperature in the step of extracting the Tochu leaves with water is 80-100 ° C; including the step of leaving the extract at 0-10 ° C before concentrating to remove the precipitate formed; 17. The production method according to claim 15, further comprising a step of performing centrifugation at a g value of 680 to 840 g for 20 to 30 minutes after the concentration step of the extract to remove a precipitate.