JP2018168144A - Lipase inhibitors and uses thereof - Google Patents

Abstract

To provide plant-derived lipase inhibitors usable as food and drinks, drugs, quasi-drugs, cosmetics or an ingredient thereof, as well as adiposity inhibitors or anti-obesity agents.SOLUTION: The lipase inhibitor of the present invention comprises as an effective ingredient one or more processed plant parts selected from the group consisting of leaves, stalks and fruits of Triadica sebifera, leaves of Morella rubra, leaves and branches of Quercus salicina, leaves and stalks of Mallotus japonicas, leaves of Vernicia cordata, leaves of Aleurites fordii Hemsl., leaves of Lindera umbellate, leaves of Perilla frutescens var. frutescens, leaves of Synurus palmatopinnatifidus, leaves of Magnolia salicifolia, leaves of Acanthopanax spinosus, leaves of Clerodendrum trichotomum, leaves and stalks of Ricinus communis, leaves of Thujopsis dolabrata, leaves of Cryptomeria japonica, leaves of Metaplexis japonica and leaves of Asimina triloba. The adiposity inhibitor or anti-obesity agents of the present invention comprises as an effective ingredient one or more processed plant parts selected from the group consisting of leaves, stalks and fruits of Triadica sebifera, leaves of Morella rubra, leaves and branches of Quercus salicina, leaves of Vernicia cordata, leaves of Aleurites fordii Hemsl., leaves of Lindera umbellate, leaves of Synurus palmatopinnatifidus, leaves of Magnolia salicifolia, leaves of Acanthopanax spinosus, leaves of Clerodendrum trichotomum, and leaves and stalks of Ricinus communis.SELECTED DRAWING: None

Description

  The present invention relates to a lipase inhibitor containing processed products of various plant parts as active ingredients. The present invention also relates to a fat accumulation inhibitor or an anti-obesity agent containing various processed plant parts as active ingredients. These lipase inhibitors and fat accumulation inhibitors or anti-obesity agents include food and beverage compositions, pharmaceutical compositions, quasi-drug compositions, cosmetic compositions, and additives for these compositions. included.

  Obesity refers to a condition in which calorie intake exceeds calorie consumption due to physical constitution, diet or lack of exercise, and as a result, abnormal fat accumulation is recognized in the living body. Obesity is one of the risk factors that cause so-called metabolic syndrome such as diabetes, hypertension, hyperlipidemia and arteriosclerosis, and an increase in the number of patients with the above-mentioned diseases that develop from obesity is a social problem. As one of effective methods for eliminating or preventing obesity, a method that inhibits lipase action in vivo and suppresses fat absorption has attracted attention.

  Pancreatic lipase, one of the main digestive enzymes of long-chain triglycerides (triacylglycerol) in ingested foods, catalyzes the hydrolysis of the 1st to 3rd ester bonds of triacylglycerol. The fatty acid and monoacylglycerol thus produced are absorbed from the gastrointestinal tract and then converted back to triacylglycerol. Triacylglycerol, which is transported to each tissue through the blood, is consumed as energy, but fat exceeding the consumption is accumulated in the adipose tissue. Paying attention to the role of pancreatic lipase in the mechanism of fat absorption and accumulation in vivo, attempts have been made to inhibit fat absorption by administering a pancreatic lipase inhibitor. However, to date, lipase inhibitors have been used clinically to treat or ameliorate obesity (Non-patent Document 1).

  In addition, microbial lipases are known to be involved in specific skin diseases. Specifically, when sebum accumulates due to an enlarged growth of sebaceous glands or increased keratinization of the follicular pore, acne gonococci and skin staphylococci that are resident in the hair follicle hair funnel proliferate. These lipases break down triacylglycerol, which constitutes sebum, to produce free fatty acids. This free fatty acid is said to act on the epithelium and produce various enzymes, causing acne, dermatitis, dandruff and the like (see Non-Patent Document 2). Therefore, if the microbial lipase can be inhibited, it is considered that a therapeutic or ameliorating means or a preventive means for a specific skin disease caused by the lipase can be provided.

  Naturally derived foods and herbal medicines generally have advantages such as fewer side effects. For this reason, if a component effective for treatment or improvement of various diseases can be obtained from natural products, it can be effectively used as a product with few side effects. Regarding the lipase-related diseases described above, based on the above idea, a search for substances having a lipase activity inhibitory action in food components derived from natural products has been conducted (see Patent Documents 1 to 3, etc.).

JP 2005-289950 A JP 2006-290807 A JP-A-9-227398

"Clinical Nutr.", Sternby, B., et al, 21, 395, 2002 "New Cosmetics", Takeo Mitsui, pp. 29-30, Nanzan-do, Tokyo, 1993

  The present invention relates to a novel lipase inhibitor, particularly a novel lipase inhibitor which is derived from a natural plant and can be used as a food / beverage composition, a pharmaceutical composition, a quasi-drug composition, a cosmetic composition or a compounding component thereof. It is an issue to provide. Further, the present invention has a fat accumulation inhibitory action or an anti-obesity action based on lipase inhibitory activity, and is used as a food / beverage composition, a pharmaceutical composition, a quasi-drug composition, a cosmetic composition or a compounding component thereof. It is an object of the present invention to provide a novel fat accumulation inhibitor or anti-obesity agent that can be used.

  The inventors of the present invention have been diligently researching to solve such problems, and found that a specific plant part contains a component having a lipase inhibitory activity, and these are used as a lipase inhibitor as a food and beverage composition. The present invention was confirmed to be applicable to products, pharmaceutical compositions, quasi-drug compositions, or cosmetic compositions. Further, it has been found that these fractions having lipase inhibitory activity have a fat accumulation-inhibiting action or an anti-obesity action, and can be widely used as a fat accumulation-inhibiting agent or anti-obesity agent in the food, pharmaceutical and cosmetic fields. It was.

  The present invention has been completed based on such findings, and has the following embodiments.

I. Lipase inhibitor (I-1) Nankin goby leaves, petioles and berries; bayberry leaves; A lipase inhibitor comprising, as an active ingredient, a processed product of at least one plant part selected from the group consisting of peony leaves; castor leaves and petiole; asnalo leaves; cedar leaves; potato leaves;
(I-2) The lipase inhibitor according to (I-1), wherein the processed product is a solvent extract.
(I-3) The lipase inhibitor according to (I-2), wherein the solvent is water.
(I-4) The plant part is peanut leaves, petiole and berries; bayberry leaves; vulgari leaves and branches; The lipase inhibitor according to (I-3), which is at least one selected from the group consisting of castor leaf and petiole; cedar leaf; potato leaf; and popo leaf.
(I-5) The lipase inhibitor according to (I-2), wherein the solvent is hydrous ethanol.
(I-6) Plant part is peanut leaves, petiole and berries; bayberry leaves; And the lipase inhibitor described in (I-5), which is at least one selected from the group consisting of potato leaves.
(I-7) A food / beverage composition, a pharmaceutical composition, a quasi-drug composition, a cosmetic composition, or any one of (I-1) to (I-6), which is an additive for these compositions The lipase inhibitor described.

II. Fat accumulation inhibitor or anti-obesity agent (II-1) peanut leaves, petiole and fruit; bayberry leaves; radish leaves and branches; And a fat accumulation inhibitor or anti-obesity agent comprising, as an active ingredient, a processed product of at least one plant part selected from the group consisting of castor leaf and petiole.
(II-2) The fat accumulation inhibitor or anti-obesity agent according to (II-1), wherein the processed product is a solvent extract. (II-3) The fat accumulation inhibitor or anti-obesity agent according to (II-2), wherein the solvent is water.
(II-4) A group consisting of peanut leaves, petioles and berries; bayberry leaves; radish leaves and branches; abragi leaves; sinabragi leaves; The fat accumulation inhibitor or anti-obesity agent described in (II-3), which is at least one selected from the group consisting of: .
(II-5) The fat accumulation inhibitor or anti-obesity agent according to (II-2), wherein the solvent is hydrous ethanol.
(II-6) The plant part is at least one selected from the group consisting of peanut leaves, petioles and berries; bayberry leaves; vulgari leaves and branches; The fat accumulation inhibitor or anti-obesity agent described in (II-5).
(II-7) Fat accumulation according to any of (II-1) to (II-6), which is a food / beverage product composition, a pharmaceutical composition, a quasi-drug composition, or an additive for these compositions Inhibitor or anti-obesity agent.

  According to the present invention, a novel lipase inhibitor derived from a natural plant can be provided. According to the lipase inhibitor of the present invention, fat absorption can be suppressed by inhibiting lipase activity in vivo, and therefore fat accumulation or obesity caused by intake calories exceeding calorie consumption can be prevented or improved. . It is also possible to prevent or ameliorate arteriosclerosis, myocardial infarction, and fatty liver which can be caused by fat accumulation; and metabolic syndrome (eg, diabetes, hypertension, hyperlipidemia, etc.) in which obesity can be a risk factor. Therefore, according to the present invention, a novel fat accumulation inhibitor or anti-obesity agent can be provided.

  Moreover, according to the lipase inhibitor of the present invention, skin troubles such as acne, dermatitis, and dandruff can be prevented or improved by inhibiting the activity of lipase produced by resident skin bacteria.

  Furthermore, according to the lipase inhibitor of the present invention, fats and oils (triacylglycerol) that cause malodor and deterioration included in food and beverage compositions, pharmaceutical compositions, quasi-drug compositions, and cosmetic compositions. Since lipase decomposition can be prevented, it is possible to stably maintain quality including flavor (odor, taste, etc.) and feeling of use.

I. Lipase Inhibitors The lipase inhibitors of the present invention include peanut leaves, petiole and berries; bayberry leaves; An active ingredient is a processed product of at least one plant part (plant part) selected from the group consisting of Yamakogi leaves; wedge leaves; castor leaves and petiole; asunaro leaves; cedar leaves;

  Nankin goby is a deciduous tree that belongs to the genus Nankin goby, called scientific name "Triadica sebifera". For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, leaves, petioles and berries of peanut are preferably used. These plant parts may be used individually by 1 type, and can also be used in combination of 2 or more types arbitrarily. Preferably it is a leaf and a petiole, More preferably, it is a petiole.

  The bayberry is an evergreen tree of the genus Dioscorea that is called the scientific name “Morella rubra”. For preparing a processed product which is an active ingredient of the lipase inhibitor of the present invention, bayberry leaves are preferably used.

  Vulgaris are the evergreen broad-leaved tree belonging to the genus Quercus salicina, which is called the scientific name “Quercus salicina”. For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, leaves and branches of radish are preferably used. These plant parts may be used individually by 1 type, and can also be used in combination of 2 or more types arbitrarily.

  Akamegashiwa (red buds, red buds) is a deciduous tree of the genus Akamegasiwa, which is called scientific name "Mallotus japonicus". For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, leaves and petioles of red-backed wrinkles are preferably used. These plant parts may be used individually by 1 type, and can also be used in combination of 2 or more types arbitrarily.

  Abragiri (oil paulownia) is a deciduous tree that belongs to the genus Brassicaceae, which is called scientific name "Vernicia cordata". In the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, abragi leaves are preferably used.

  Sina Abragiri is a deciduous tree of the genus Adragiri, which is called scientific name "Aleurites fordii Hemsl." For the preparation of a processed product that is an active ingredient of the lipase inhibitor of the present invention, a leaf of Sinabragiri is suitably used.

  Kuromoji (black letters) is a deciduous shrub belonging to the genus Kuromoji, which is called the scientific name “Lindera umbellata”. For the preparation of a processed product that is an active ingredient of the lipase inhibitor of the present invention, black leaves are preferably used.

  Sesame is an annual plant of the family Lamiaceae called the scientific name "Perilla frutescens var. Frutescens". Perilla (blue shiso) is a variant of the same kind. Sesame leaves are preferably used for the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention.

  Kikubayamabokuchi (Kikubayama Crater) is a perennial plant belonging to the genus Asteraceae, which is called the scientific name "Synurus palmatopinnatifidus". For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, Kikubayamabokuchi leaves are preferably used.

  Tamshiba (Toshiba) is a small deciduous tree of the magnolia family Magnolia, which is called scientific name “Magnolia salicifolia”. For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, a leaf of a bamboo shoot is preferably used.

  Yamakogi (Yamagoka) is a deciduous shrub belonging to the genus Uguigiaceae, which has the scientific name "Acanthopanax spinosus." Yamakogi leaves are preferably used for the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention.

  Wedge (smelling tree) is a deciduous small Takagi tree of the family Lamiaceae, which is called scientific name “Clerodendrum trichotomum”. For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, the leaves of magpie are preferably used.

  Castor sesame is a perennial plant belonging to the genus Spiraceae, which is called scientific name “Ricinus communis”. For the preparation of a processed product that is an active ingredient of the lipase inhibitor of the present invention, castor bean leaves and petiole are preferably used.

  Asunaro (next day) is an evergreen conifer of the cypress Asunaro genus called scientific name "Thujopsis dolabrata". Asunaro leaves are preferably used for the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention.

  Sugi (cedar) is an evergreen conifer belonging to the genus Cedaraceae and Subfamily Sugi under the scientific name “Cryptomeria japonica”. For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, cedar leaves are preferably used.

  Gagaimo is a perennial vine belonging to the genus Gagaimo, which is called the scientific name “Metaplexis japonica”. For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, potato leaves are preferably used.

  Pawpaw is a deciduous tree belonging to the genus Popow, which is called the scientific name “Asimina triloba”. For the preparation of a processed product which is an active ingredient of the lipase inhibitor of the present invention, poppo leaves are preferably used.

  The lipase inhibitor of the present invention only needs to contain at least one processed product of each part (plant part) of the plant as an active ingredient. The processed product may be obtained from one kind of plant part, or may contain any combination obtained from two or more kinds. Preferred plant parts include peanut leaves, petiole and berries; bayberry leaves; vulgari leaves and branches; And at least one selected from the group consisting of popo leaves, more preferably peanut leaves, petioles and berries; bay leaves; And at least one selected from the group consisting of cedar leaves; A small group selected from the group consisting of leaf A Kutomo one, particularly preferably at least one selected Chinese tallow leaves, Chinese tallow petioles, bayberry leaves, and from the group consisting of Magnolia salicifolia leaves.

  In the present invention, the processed product includes a dried pulverized product (including coarse powder and fine powder), juice, solvent extract (including diluted solution, concentrated solution, paste-like product, and dry powder). Is included.

  When the processed product is a dry pulverized product, the pulverized product is prepared by drying the collected plant part and then pulverizing it. Drying and pulverization can be performed according to a conventional method. For example, examples of the drying method include a heat drying method, sun drying, dehumidification drying, and freeze drying. The pulverization method is not particularly limited, and may be dry or wet. The order of the drying and pulverization steps is not particularly limited, and both steps can be performed simultaneously.

  When the processed product is a solvent extract, the part of each plant used for solvent extraction may be intact (raw) or may be a dried product thereof. Moreover, the raw material or its dried product may be cut or pulverized. Solvents used for extraction can include polar or nonpolar solvents that are typically used for plant extraction. A polar solvent is preferred. Nonpolar solvents include aromatic hydrocarbons such as benzene and toluene; halogenated aliphatic hydrocarbons such as methylene chloride and chloroform; ethers such as ether and tetrahydrofuran; esters such as ethyl acetate; However, these nonpolar solvents can be used for degreasing treatment before extraction with a polar solvent, if necessary. By performing an extraction process (degreasing process) using a nonpolar solvent, it may be possible to efficiently perform an extraction process using a polar solvent to be performed later.

  Specific examples of the polar solvent include water; alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol and 2-butanol; ketones such as acetone; nitriles such as acetonitrile and the like. Can do. These may be used alone or in any combination of two or more. Preferably, from the viewpoint of safety in use after extraction, water; and alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol and 2-butanol, more preferably water, ethanol and these (Water-containing ethanol), particularly preferably water and water-containing ethanol. Here, the concentration of ethanol contained in the hydrous ethanol is not limited, but can be appropriately selected in the range of usually 5 to 90% by volume. The range is preferably 10 to 80% by volume, more preferably 30 to 70% by volume, and still more preferably 40 to 70% by volume.

  Specifically, water and water-containing ethanol are used as a solvent for extracting an active ingredient of a lipase inhibitor from peanut leaves, petioles and berries; radish leaves and branches; It can be used suitably. In addition, water and water-containing ethanol, more preferably water-containing ethanol, can be suitably used as a solvent for extracting an active ingredient of a lipase inhibitor from bayberry leaves; abragiri leaves; black moji leaves; In addition, water is used as a solvent for extracting an active ingredient of a lipase inhibitor from sesame leaves; Yamakogi leaves; wedge leaves; castor leaves and petioles; As the solvent for extraction, hydrous ethanol can be suitably used.

  An extraction method using such an extraction solvent can follow a conventional method, and is not particularly limited, and examples thereof include a method in which a target plant part is immersed in a solvent and allowed to stand or stir. The temperature of the extraction solvent to be used (that is, the extraction temperature) can be appropriately set in the range of 0 to 100 ° C. When water is used as the extraction solvent, it is possible to increase extraction efficiency by using warm water or hot water of 25 ° C. or higher, preferably 40 ° C. or higher, more preferably 60 ° C. or higher, particularly preferably 80 ° C. or higher. preferable. On the other hand, when ethanol or hydrous ethanol is used as the extraction solvent, it is preferably performed at a temperature of 50 ° C. or lower in consideration of extraction efficiency and handling safety, for example, 5 ° C. or higher, preferably 15 ° C. or higher, more preferably. Can be appropriately set to a temperature of 25 ° C. or higher.

  The extraction time is not particularly limited as long as the target component having lipase inhibitory activity can be extracted from each plant part, and can be appropriately selected and set from the range of usually 10 minutes to 24 hours. Preferably about 10 minutes to 12 hours, more preferably about 10 minutes to 2 hours.

  After the extraction, the obtained extract is then subjected to filtration, centrifugation, or the like, so that it is subjected to solid-liquid separation to remove solid insoluble matter. The collected filtrate or supernatant can then be subjected to a purification step such as dilution, filtration, concentration, decolorization or deodorization as necessary. If necessary, the removed solid insoluble matter is extracted again using the above-mentioned solvent in the same manner as described above, and the extracted liquid after solid-liquid separation is used in the above filtrate or supernatant. You can also. In addition, filtration, centrifugation, concentration, decolorization, deodorization, etc. can use the conventional method of this industry, and are not restrict | limited in particular. Examples of purification treatment such as decolorization and deodorization include, but are not limited to, conventional methods such as activated carbon treatment, resin adsorption treatment, ion exchange resin treatment, and liquid-liquid countercurrent distribution.

  The extract thus prepared can be used as it is, but may be further concentrated or dried, or diluted with an appropriate solvent. Alternatively, it can be prepared as a powder by directly or after being diluted with an appropriate solvent and then drying by a known method such as spray drying, freeze drying, reduced pressure drying, or fluidized drying. The shape of these extracts can be appropriately selected and set according to the form and purpose of the lipase inhibitor of the present invention containing the extract. When drying, an excipient may be added as necessary.

  The “lipase” targeted by the present invention is a triacylglycerol lipase having an action of decomposing triacylglycerol and releasing a fatty acid (fatty acid releasing action). Specifically, pancreatic lipase associated with fat absorption in the gastrointestinal tract, as well as Candida cylindracea, Propionibacterium acnes, Pilyrosporum ovale, or micro A microbial lipase produced by a skin resident bacterium such as Micrococcus sp. Can be exemplified without limitation. Similarly to pancreatic lipase, examples of the microbial lipase exhibiting sn-1,3 specificity include Rhizomucor miehei and Rhizopus arrhizus.

  The “lipase inhibitor” of the present invention is not limited as long as it has an activity of inhibiting the above-mentioned fatty acid releasing action of lipase, but preferably has at least an activity of inhibiting the fatty acid releasing action of pancreatic lipase. More preferably, it has an activity to inhibit the fatty acid releasing action of not only pancreatic lipase but also microbial lipase. Moreover, the lipase inhibitor of this invention is not limited to what inhibits the fatty-acid releasing action (lipase activity) of lipase 100%, You may inhibit the one part. The lipase activity can be conveniently measured using, for example, a commercially available lipase measuring reagent and is not limited, but specifically, “Lipase Kit S” (manufactured by DS Pharma Biomedical Co., Ltd.) and the like are exemplified. be able to.

  The lipase inhibitor of the present invention is a component that exhibits lipase inhibitory activity (lipase inhibitory active ingredient or active ingredient) when preparing a pharmaceutical composition, quasi-drug composition, food / beverage product composition or cosmetic composition. Besides being added and blended, the lipase inhibitor itself can be prepared in the form of a pharmaceutical composition, a quasi-drug composition, a food / beverage composition or a cosmetic composition. Since the former lipase inhibitor is used as an additive in a pharmaceutical composition, quasi-drug composition, food / beverage composition or cosmetic composition, it is used as an “additive” for convenience in the present invention. Called. When the lipase inhibitor of the present invention is used as the additive, the lipase inhibitor of the present invention may consist of 100% by mass of the aforementioned processed plant product, and does not interfere with the lipase inhibitory activity. In addition to the above-mentioned processed plant products, those containing diluents, flavoring agents, coloring agents, sweetening agents, corrigents, suspending agents, emulsifying agents, dispersing agents, preservatives, buffering agents, stabilizers, etc. It may be. When the lipase inhibitor of the present invention is used as the latter pharmaceutical composition, quasi-drug composition, food / beverage composition, or cosmetic composition itself, the lipase inhibitor that is the final composition includes various types described below. The processed plant described above is contained in a proportion that exhibits lipase inhibitory activity according to the form. Although not limited, examples of the proportion include a range of 5 to 95 mass%. Preferably it is 50-95 mass%.

  Specifically, pharmaceutical compositions and quasi-drug compositions are, for example, for oral administration, tablets, capsules, powders, granules, pills, solutions, emulsions, suspensions, solutions, Alcohol, syrup, extract, elixir and the like can be used, for example, cream, jelly, gel, paste, ointment and the like for topical administration, but are not limited thereto. The pharmaceutical composition or quasi-drug composition may contain various commonly used components, such as one or more pharmaceutically acceptable excipients, disintegrants, diluents, lubricants. Agents, flavoring agents, coloring agents, sweetening agents, flavoring agents, suspending agents, wetting agents, emulsifying agents, dispersing agents, adjuvants, preservatives, buffering agents, binders, stabilizers, coating agents and the like can be included. The pharmaceutical composition or quasi drug composition of the present invention may have a sustained or sustained release dosage form.

  The food / beverage composition targeted by the present invention includes foods for specified health use, functional labeling foods, and health functional foods (including beverages) including nutritional functional foods; and nutritional supplements, health supplements, and nutritionally adjusted foods Any of the general foods (including beverages) containing These food / beverage products compositions should just have the shape of the usual food / beverage, for example, the form of the formulation generally provided as a supplement other than the form of a general food and a drink (apparent food) can be mentioned. . Examples of the preparation form include tablets, capsules, powders, granules, pills, and extracts as described above. The preparation can contain commonly used formulation ingredients depending on the shape, for example, one or more pharmaceutically acceptable excipients, disintegrants, diluents, lubricants, dressings, and the like. Flavoring agents, coloring agents, sweetening agents, flavoring agents, suspending agents, wetting agents, emulsifying agents, dispersing agents, auxiliary agents, preservatives, buffering agents, binders, stabilizers, coating agents and the like can be included. The formulation may also be a sustained or sustained release dosage form.

  The cosmetic composition targeted by the present invention is not particularly limited, and includes, for example, milky lotion, cosmetic liquid, face cream, hand cream, lotion, shampoo, and rinse. In addition, the plant processed material which has the activity which inhibits the fatty-acid releasing action which microbial lipase has as a lipase inhibitor used as a cosmetic composition is used as an active ingredient.

  According to the pharmaceutical composition and the quasi-drug composition and the food / beverage product composition having the oral dosage form described above, it is possible to ingest daily or continuously the lipase inhibitory active ingredient derived from the processed plant product. In addition, obesity can be prevented or ameliorated by an effective fat accumulation suppressing effect. Moreover, according to the pharmaceutical composition and quasi-drug composition having the above-mentioned topical dosage form, and the cosmetic composition, the lipase inhibitory active ingredient derived from the processed plant product is applied continuously or discontinuously to the skin. Thus, it is possible to prevent or improve skin troubles (acne, dermatitis, etc.) caused by fatty acids produced by lipase. Furthermore, the presence of a lipase inhibitory active ingredient derived from a processed plant product in a pharmaceutical composition, a quasi-drug composition, a food / beverage composition, and a cosmetic composition allows the fat in the target composition to be microbial lipase. Hydrolysis is suppressed, deterioration of the composition due to free fatty acids is prevented, and the quality of the composition can be maintained over a long period of time.

II. Fat accumulation inhibitor or anti-obesity agent The fat accumulation inhibitor or anti-obesity agent of the present invention includes peanut leaves, petiole and berries; bayberry leaves; An active ingredient is a processed product of at least one plant part (plant part) selected from the group consisting of leaves; Yamakogi leaves; wedge leaves; and castor leaves and petiole.

  In the present invention, “inhibition of fat accumulation” means to suppress the accumulation of fat in the living body by suppressing the absorption of neutral fat from the intestinal tract. Here, “inhibition of fat accumulation” includes suppression of fat uptake into fat cells. The above-described suppression of neutral fat absorption is due to the lipase inhibitory action, particularly pancreatic lipase inhibitory action, of the processed plant product targeted by the present invention. Further, in the present invention, “anti-obesity” is based on the above-described action of inhibiting the absorption of neutral fat from the intestinal tract and the action of inhibiting fat accumulation in the living body, and suppresses obesity (obesity prevention) or improves obesity (obesity elimination). Means.

  The processed plant product used in the fat accumulation inhibitor or the anti-obesity agent of the present invention and the preparation method thereof, the plant used therefor and its part, and the type of the extraction solvent used for the preparation of the solvent extract are as described in I above. It is as having demonstrated in the column and can be used here.

  As described above, the “fat accumulation inhibitor or anti-obesity agent” of the present invention is based on the pancreatic lipase inhibitory action of a plant processed product contained as an active ingredient, and when administered orally to mammals including humans. Exerts an action to suppress fat accumulation or an anti-obesity action. For this reason, the fat accumulation inhibitor or anti-obesity agent of the present invention is characterized by having at least pancreatic lipase inhibitory action. It should be noted that the fat accumulation inhibitor or anti-obesity agent of the present invention is not limited to one that inhibits 100% of the fatty acid releasing action (pancreatic lipase activity) of pancreatic lipase, but inhibits a part thereof. May be. Pancreatic lipase activity can be conveniently measured using, for example, a commercially available reagent for lipase measurement. Specific examples include “Lipase Kit S” (manufactured by DS Pharma Biomedical Co., Ltd.) and the like. can do.

  The fat accumulation inhibitor or anti-obesity agent of the present invention is a component having a fat accumulation-inhibiting action or an anti-obesity action, which is added to a pharmaceutical composition, a quasi-drug composition, or a food / beverage product composition. In addition to being used as an active ingredient or an additive as an active ingredient, a fat accumulation inhibitor or anti-obesity agent itself is prepared in the form of a pharmaceutical composition, a quasi-drug composition, or a food and beverage composition. be able to. When used as the former additive, the fat accumulation-inhibiting agent or anti-obesity agent of the present invention may comprise 100% by mass of the above-mentioned processed plant product, and may also be a fat accumulation-inhibiting action or anti-obesity action. In addition to the above-mentioned processed plant products, diluents, flavoring agents, coloring agents, sweeteners, corrigents, suspending agents, emulsifiers, dispersants, preservatives, buffering agents, stabilizers, etc. May be included. When the fat accumulation inhibitor or anti-obesity agent of the present invention is used as the latter pharmaceutical composition, quasi-drug composition, or food or beverage composition, the fat accumulation inhibitor or anti-obesity agent as the final composition is According to various forms, the aforementioned processed plant product is contained at a ratio that exhibits a fat accumulation suppressing action or an anti-obesity action (lipase inhibiting action). Although not limited, examples of the proportion include a range of 5 to 95 mass%. Preferably it is 50-95 mass%.

  When the fat accumulation inhibitor or anti-obesity agent of the present invention is a pharmaceutical composition or a quasi-drug composition, for example, tablet, capsule, powder, granule, pill, liquid, emulsion, suspension, solution Oral administration forms such as pills, spirits, syrups, extracts, and elixirs. These may have sustained or sustained release dosage forms. Such a dosage form can be mixed with any pharmaceutically acceptable pharmaceutical additive or quasi-drug additive according to a conventional method.

  When the fat accumulation inhibitor or anti-obesity agent of the present invention is a food / beverage product composition, the food / beverage product composition includes a food for specified health use, a functional food, a health functional food (a beverage) As well as general foods (including beverages) including nutritional supplements, health supplements, and nutritionally adjusted foods. These food / beverage products compositions should just have the shape of the usual food / beverage, for example, the form of the formulation generally provided as a supplement other than the form of a general food and a drink (apparent food) can be mentioned. . Preferably, it is a food for specified health use or a functional indication food that can have a fat accumulation inhibiting effect and / or an anti-obesity effect as a function of food and drink.

  According to the fat accumulation inhibitor or anti-obesity agent of the present invention, it is possible to orally ingest the pancreatic lipase inhibitory active ingredient derived from the above-mentioned plant processed product on a daily or continuous basis, and effective fat accumulation inhibiting effect Can prevent or improve obesity. The subjects who are orally ingested are mammals including humans and are not limited, but are preferably "persons who are concerned about neutral fat", "persons who are concerned about body fat", "persons who are obese or obese" .

  The oral intake time is not limited and may be taken with meals, or before or after meals. Considering the action of suppressing the absorption of fat contained in a meal, it is preferable to take it with or immediately after a meal.

  Hereinafter, the present invention will be described based on experimental examples and examples. However, these experimental examples are examples of the present invention, and the present invention is not limited by these experimental examples.

Experimental Example 1 Preparation of Processed Plant (1) Preparation of Plant Dry Powder Parts of various plants (Nankinase leaves, petiole and berries; bayberry leaves; radish leaves and branches; Sesame leaves; Kikubayamabokuchi leaves; Tamshiba leaves; Yamakogi leaves; Wedge leaves; Castor leaves and petioles; Asuna leaves; Sugi leaves; And dehydrated at −30 ° C. This frozen product was freeze-dried at 25 ° C. for 72 hours (using ULVAC vacuum freeze dryer (DF-03H)), and the dried sample was pulverized (VIBRATING SAMPLE MILL TI- 100) to prepare a plant dry powder.

(2) Preparation of plant extract After adding 10 ml of boiling Milli-Q water to 1 g of the above-prepared finely pulverized sample (plant dry powder) and extracting it by heating (approximately 100 ° C.) for 30 minutes in a boiling water bath, The extract was quenched and filtered using filter paper (No. 2), and the filtrate was recovered as a hot water extract of plant parts. Similarly, 10 ml of a 60 vol% ethanol aqueous solution is added to 1 g of the finely pulverized sample (plant dried powder), and the mixture is stirred and extracted overnight at room temperature (25 ± 5 ° C.). The filtrate was recovered as a 60% ethanol extract of plant parts. Each collected filtrate (hot water extract, 60% ethanol extract) was concentrated under reduced pressure using a rotary evaporator, and then the concentrate was freeze-dried to obtain a plant extract (dry extract). Among these plant extracts (dry extracts), dry extracts prepared from hot water extract were dissolved by adding milli-Q water at a rate of 1 ml per 10 mg of dry extract, and prepared from 60% ethanol extract. The dried extract was dissolved by adding 60 vol% ethanol aqueous solution at a rate of 1 ml per 10 mg of the dried extract to prepare a plant extract (concentrated reductate: 10 mg / ml). In addition, as a positive control (control example), 1 g of crushed dried tea leaves (sencha leaves) (trade name: Yakumo Homare) was treated in the same manner (hot water extraction, 60% ethanol extraction) to obtain a plant extract (concentrated reductant). : 10 mg / ml). The following lipase inhibitory activity test was conducted using each of these plant extracts.

Experimental Example 2 In Vitro Lipase Inhibitory Activity Test The lipase inhibitory activity of each plant extract prepared in Experimental Example 1 was measured using lipase (SIGMA porcine pancreatic lipase: Lipase from porcine pamcreas, Type II) and lipase kit S (DS Pharma). Biomedical Co., Ltd.). The measurement method followed the manufacturer's instructions.

The measurement method is briefly described as follows.
In a test tube, each plant extract prepared in Experimental Example 1 (Examples 1 to 22, control example), and a plant extract dilution prepared by diluting them twice to 32-fold dilution (hereinafter referred to as “test sample”) ) Put 25 μl each, add 40 μl of lipase aqueous solution prepared to 0.05 mg / ml, 500 μl of color developing solution (5,5′-dithiobis [2-nitrobenzoic acid]) and 10 μl of esterase inhibitor (phenylmethylsulfonyl fluoride) And reacted at 30 ° C. for 5 minutes. Thereafter, 50 μl of a substrate solution (dimercaprol tributyrate, sodium dodecyl sulfate) was added and mixed with each, followed by reaction at 30 ° C. for 30 minutes, and then 1 ml of a reaction stop solution was added. 250 μl of this reaction solution (test sample reaction solution) was collected in a 96-well plate, and the absorbance at 410 nm was measured with a spectrophotometer (PerspirElmer Enspire / 2300). As a control, an extraction solvent (Milli Q water or 60% ethanol aqueous solution) was used instead of the test sample, and the reaction was performed in the same manner as described above, and the absorbance at 410 nm (the absorbance of the control) was measured.

  From the obtained absorbance, the lipase inhibition rate was determined from the following equation.

[Equation 1]
Lipase inhibition rate (%) = {1- (S-SB) / (C-CB)} × 100
S: Absorbance of test sample reaction solution SB: Absorbance of test sample blank (test sample itself) C: Absorbance of control CB: Absorbance of control blank (extraction solvent itself)

Here, when the lipase activity was inhibited by 50% (lipase inhibition rate 50%), the test sample concentration in the test sample reaction solution was defined as the IC ₅₀ (mg / ml) value, that is, the lipase inhibitory activity.
The results are shown in Table 1.

  As shown in Table 1, the plant extracts of peanut leaves and petioles; bayberry leaves; radish leaves and branches; Showed activity. Moreover, the 60% ethanol extract of Akagasiwa and Abragiri leaves showed higher lipase inhibitory activity than the green tea extract (hot water and 60% ethanol extract). Furthermore, the 60% ethanol extract of Sina brachigiri leaf, black moji leaf, and cedar leaf showed higher lipase inhibitory activity than the 60% ethanol extract of green tea. In addition, the lipase inhibitory activity was recognized only in the hot-water extraction fraction about the sesame leaf, the Yamakogi leaf, the wedge leaf, the castor leaf, the petiole, and the popau leaf. On the other hand, as for Kikubayamabokuchi leaves and Asunaro leaves, lipase inhibitory activity was observed only in the 60% ethanol extract fraction.

  As shown above, it was found that the plant parts used in Examples 1 to 22 contained a component having lipase inhibitory activity. For this reason, these plant parts processed products (for example, dried pulverized products, solvent extracts, etc.) are effective in compositions utilizing their lipase inhibitory activity, such as lipase inhibitors, fat accumulation inhibitors or anti-obesity agents. As a component, it can be effectively used for pharmaceuticals, quasi drugs, cosmetics or foods.

  Although the inhibition of activity against pancreatic lipase was evaluated here, the lipase derived from the microorganisms described above also has the action of decomposing triacylglycerol to release fatty acids (fatty acid releasing action), similar to pancreatic lipase. ) Triacylglycerol lipase. For this reason, each said processed plant product is considered to have not only an inhibitory action on pancreatic lipase but also an inhibitory action on microbial lipase. In particular, each plant processed product is not limited, but is considered to have an inhibitory action on lipase having the property of acting on the sn-1 position and / or sn-3 position of triacylglycerol.

Claims (8)

  Bay leaf, petioles and berries; bayberry leaves; vulgari leaves and branches; A lipase inhibitor comprising, as an active ingredient, a processed product of at least one plant part selected from the group consisting of Asunaro leaves; cedar leaves; potato leaves; and popo leaves.   The lipase inhibitor according to claim 1, wherein the processed product is a solvent extract.   The lipase inhibitor according to claim 2, wherein the solvent is water or hydrous ethanol.   The lipase inhibitor according to any one of claims 1 to 3, which is a food / beverage composition, a pharmaceutical composition, a quasi-drug composition, a cosmetic composition, or an additive for these compositions.   At least one selected from the group consisting of bayberry leaves, petiole and berries; bayberry leaves; radish leaves and branches; A fat accumulation inhibitor or anti-obesity agent comprising a processed plant part of a seed as an active ingredient.   The fat accumulation inhibitor or anti-obesity agent according to claim 5, wherein the processed product is a solvent extract.   The fat accumulation inhibitor or anti-obesity agent according to claim 6, wherein the solvent is water or hydrous ethanol.   The fat accumulation inhibitor or anti-obesity agent according to any one of claims 5 to 7, which is a food / beverage composition, a pharmaceutical composition, a quasi-drug composition, or an additive for these compositions.