JP2010209051A - Fat absorption inhibitor - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a fat absorption inhibitor having high safety and high effect of dieting. <P>SOLUTION: The fat absorption inhibitor and a lipase inhibitor each contains, as an active ingredient, at least one plant selected from the group consisting of black ginger, red ginger, cinnamon, young barley leaves, black garlic, gambir, hydrangea, myrobalan, pomegranate, flax plant (Linum usitatissimum), sweet osmanthus (Osmanthus fragrans var. aurantiacus), Sarcandra glabra tea, Saxifraga stolonifera, jasmine tea, oregano, olive leaves, everlasting flowers, sea buckthorn, chamomile, and curry leaves or an extract thereof. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention includes black ginger, red ginger, Nikkei (bark, root, leaf, or branch), barley young leaf, black garlic, Asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under snow, jasmine tea The invention relates to a fat absorption inhibitor and a lipase inhibitor comprising as an active ingredient at least one plant selected from the group consisting of oregano, olive leaf, shaba spine, and curry leaf.

  Obesity is thought to be caused by lifestyle disturbances such as lack of exercise and overeating, genetic predisposition, and a decrease in basal metabolism.In recent years, the appetite control function of leptin secreted from fat cells is closely related to obesity. It is also clear that they are involved. Excessive obesity can cause lifestyle-related diseases such as diabetes and cardiovascular disease (arteriosclerosis, stroke), and therefore needs to be treated promptly and promptly.

  Obesity elimination or treatment includes (1) suppressing appetite, (2) suppressing absorption of nutrients (especially fat), (3) increasing heat production, (4) lipid and protein Improvements in metabolism and (5) regulation of central weight control mechanisms have been extensively studied. Of these, only anti-obesity drugs classified as (1) and (2) have been clinically applied, but there are few side effects and safety has not yet been established. . In Japan, only appetite suppressant mazindol, which is classified as (1), is currently approved.

  On the other hand, the thing which expresses the function of said (2) other than a therapeutic agent is developed. For example, food containing ingredients having the function (2) has been attracting attention with the recent increase in obesity and increased diet orientation. This has the advantage that it does not require a prescription like a therapeutic agent, so it can be easily obtained and taken in daily life. However, it is required to have as few side effects as possible.

  Examples of the component having the function (2) include chitin and chitosan derived from crab shells and chondroitin sulfate derived from fish cartilage, which are frequently used in health foods and the like. Since these all have pancreatic lipase inhibitory activity, the ingested fat is not enzymatically hydrolyzed, and as a result, fat absorption from the intestinal tract is suppressed. However, since these ingredients have weak ability to suppress fat absorption, they have to be taken in large amounts in daily eating habits.

  Moreover, as a substance having pancreatic lipase inhibitory activity, oolong tea polymerized polyphenol in which catechins are polymerized in the process of semi-fermenting tea leaves is known (Patent Document 1 and Non-Patent Document 1), and oolong tea containing a large amount of this polyphenol is It is known to suppress fat absorption.

  Furthermore, as a food material having lipase inhibitory activity and thereby suppressing fat absorption, Tochu Nakaba (Patent Document 2); Bald Sow, Mitsumoka, Spruce, Haksidin and Togashi (Patent Document 3); and onion, onion hull, Chestnut skin, chestnut astringent, grape, dried grape, grape skin, cacao pot hull, coffee, buckwheat husk, black rice, black bean, goji, cassis, blueberry, ginkgo biloba, gymnema sylvestre, yam leaf, citrus peel, hydroclaved bone Examples include Dan, Taranoki, Japanese hollyhock, Hachitoen, Manzan Beni, Daiba Kinkaboshi, Winter Aoba, Nori Edaha, Ganoderma licorice, Yingshan Beni, Hakuhana Beni, and Hakuhanaei Sanku (Patent Document 4).

International Publication No. 2005/077384 JP 2005-289951 A JP 2006-169181 A JP 2008-74735 A

M. Nakai et al., J. Agric. Food Chem., 2005, 53, p.4593-4598

  An object of the present invention is to provide a plant-derived safe fat absorption inhibitor that can suppress the action of pancreatic lipase with a relatively small amount of ingestion and can exhibit a fat absorption inhibitory action.

  As a result of repeated research on a plant-derived safe fat absorption inhibitor that suppresses the action of pancreatic lipase with a small amount of ingestion and can express a fat absorption inhibitory effect, black ginger, red ginger, Nikkei, Extracts extracted from barley young leaves, black garlic, asen, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under the snow, jasmine tea, oregano, olive leaf, shaba spine, and curry leaf are excellent in in vitro tests It was found that pancreatic lipase inhibitory activity was exhibited. Based on this finding, an in vivo test in mice administered with olive oil was conducted to examine the fat absorption inhibitory action of these extracts. As a result, it was found that the fat absorption inhibitory action was expressed, and the present invention was completed.

  The present invention includes black ginger, red ginger, Nikkei, young barley leaves, black garlic, Asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under the snow, jasmine tea, oregano, olive leaf, saps, and curry A fat absorption inhibitor comprising at least one plant selected from the group consisting of leaves or an extract thereof as an active ingredient is provided.

  The present invention also includes black ginger, red ginger, Nikkei, barley young leaves, black garlic, Asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under the snow, jasmine tea, oregano, olive leaf, saps, and Provided is a lipase inhibitor containing as an active ingredient at least one plant selected from the group consisting of curry leaf or an extract thereof.

  ADVANTAGE OF THE INVENTION According to this invention, the plant-derived safe fat absorption inhibitor and lipase inhibitor which can suppress the action | operation of pancreatic lipase and can express a fat absorption inhibitory effect by ingesting a comparatively small amount are provided. Since the fat absorption inhibitor and lipase inhibitor of the present invention do not need to be ingested in large amounts, they can be added to foods, for example, within a range that does not impair the original taste of foods.

(Raw plant and extract)
The fat absorption inhibitor and the lipase inhibitor of the present invention are black ginger, red ginger, nikkei, barley young leaves, black garlic, asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura tea, Kuju tea, under snow, jasmine tea, It contains at least one plant selected from the group consisting of oregano, olive leaves, scallops, and curry leaves, or an extract thereof.

  Examples of the fat absorption inhibitor and lipase inhibitor of the present invention include the above-mentioned plants, processed products thereof (dried products, ruptured products, shredded products, dry powders obtained by pulverizing these, pulverized dried products, etc.) Or these extracts may be used. In the present specification, a plant simply includes a processed product of a plant (a dried product, a ruptured product, a shredded product, or a dry powder obtained by pulverizing these, a product obtained by pulverizing a dried product, etc.). In the present specification, the extract means an extract obtained by extracting the plant or a processed product thereof with a solvent, a diluted solution or a concentrated solution thereof, or a dried product thereof. In consideration of the point of use as food or medicine, it is preferable to use an extract.

  The plant extract is obtained by extracting a plant or a processed product thereof with a solvent. Examples of the solvent used for extraction include lower alcohols such as ethanol and methanol, lower esters such as ethyl acetate and methyl acetate, acetone, and a mixture of these with water. Among these, it is preferable to use ethanol alone or a mixture with water (so-called hydrous ethanol) because it is ingested by humans. In particular, it is more preferable to use an ethanol / water mixture containing ethanol at a concentration of 30% (v / v) or higher.

  Extraction is, for example, in the examples described below, using an acetone / water mixture (70:30, v / v) in extraction from red ginger, black ginger or nikkei (bark, root, leaf or branch). However, it is naturally possible to use an ethanol / water mixture of 30% (v / v) or more instead. In fact, acetone / water mixtures (70:30, v / v) extracts in in vitro and in vivo tests using extracts with ethanol / water mixtures containing ethanol at a concentration of 30% (v / v) or higher It has been confirmed that it exhibits the same excellent fat absorption inhibitory effect and pancreatic lipase inhibitory activity as the above. Specifically, a solvent having a mass of 5 to 20 times its mass is added to a red ginger or black ginger rhizome or Nikkei (bark, root, leaf, or branch), and is allowed to stand at room temperature or under heating for 1 to 3 hours. It is preferable to extract. The same is true for barley young leaves, black garlic, Asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under the snow, jasmine tea, oregano, olive leaf, sapin, and curry leaf.

  Although there is no particular limitation on the extraction method, it is preferable that the extraction is performed under conditions as gentle as possible from the viewpoint of safety and convenience in use. For example, a raw material plant part or a dried product thereof is pulverized, crushed or shredded, a 5 to 20-fold mass solvent is added thereto, and the temperature ranges from 0 ° C. to the reflux temperature of the solvent for 30 minutes to several weeks, for example under heating. Extraction is performed for 30 minutes to 48 hours under any condition such as standing, shaking, stirring or refluxing. After extraction, separation operations such as filtration and centrifugation are performed to remove insoluble matters, and dilution and concentration operations are performed as necessary to obtain an extract. Further, if necessary, the same operation may be repeated for the insoluble matter to further extract, and the extract may be used together.

  This extract is used as it is or after being concentrated to form a liquid, a concentrate, a paste, or a dried product obtained by drying these. Drying is performed by a method commonly used by those skilled in the art, such as spray drying, freeze drying, reduced pressure drying, and fluidized drying. The extract may be further purified by a purification method commonly used by those skilled in the art.

  The red ginger used in the present invention is a fresh or dried rhizome of the ginger family Zingiber officinale var. Rubra. Red ginger is a variety cultivated in Indonesia and India and contains pigment-based polyphenols such as anthocyanins in addition to essential oil components unique to ginger. In Indonesia, it is circulated as a vegetable and is used as a material for spices and syrups. It is also used as a folk remedy for rheumatism, osteoporosis and asthma. The extract from red ginger is obtained by extraction with water, a suitable organic solvent, or a combination thereof, followed by concentration.

  The black ginger used in the present invention is a raw or dried rhizome of the ginger family plant Kaempferia parviflora. Extracts obtained from black ginger can also be used.

  Nikkei used in the present invention is the bark, root, leaf, or branch of the camphoraceae Cinnamomum okinawense (or Cinnamomum sieboldii). Nikkei is also called Japanese cinnamon and, like Cinnamomum cassia, contains cinnamon oil, a kind of essential oil, as well as confectionery or cooking spices. It is used. Extracts obtained from Nikkei can also be used.

  The barley young leaves used in the present invention are young leaves of the gramineous barley Hordeum vulgare. Extracts obtained from young barley leaves can also be used.

  The black garlic used in the present invention is obtained by fermenting and maturing bulbs (bulbs) of the allium sativum plant (garicaceae in the classification method based on the Clonquist system) and turning the bulbs (bulbs) black. Black garlic is known to contain new components such as S-allyl cysteine and S-allyl mercaptocysteine, which were not originally present in raw garlic. Extracts obtained from black garlic can also be used.

  Asen drugs used in the present invention are leaves and shoots of the Rubiaceae plant Uncaria gambir. Extracts obtained from Asen may also be used.

  Hydrangea used in the present invention is a leaf of Hydrangea macrophylla. Extracts obtained from hydrangea can also be used.

  The coconut (oak) used in the present invention is a mature fruit of the ciraceae plant Milobaran Terminalia chebura. Extracts obtained from eggplant can also be used.

  The pomegranate used in the present invention is the fruit, stem bark, branch bark or root bark of the pomegranate plant Punica granatum. Extracts obtained from pomegranate can also be used.

  Flaxseed used in the present invention is a seed of the flaxseed plant flax Linum usitatissimum. Flaxseed oil is a yellowish dry oil obtained from mature flax seeds, which is obtained by pressing flaxseed seeds (flax seeds) or crushing them and extracting them with a solvent. In the present invention, an extract obtained from flaxseed can also be used.

  The katsura flower used in the present invention is a flower of the oleaceae plant Osmanthus fragrans. Extracts obtained from katsura can also be used.

  Kuju-cha tea used in the present invention is a stem and leaf of the Sardoraceae plant Sarcandra glabra. Extracts obtained from Kuju tea can also be used.

  Under the snow used in the present invention is the leaves of the Saxifraga stolonifera plant. Extracts obtained from under the snow can also be used.

  The jasmine tea used in the present invention is a tea produced from the flowers of the oleaceae plant Jasminum sambac. Extracts obtained from jasmine tea can also be used.

  The oregano used in the present invention is the leaf of the Labiatae Origanum vulgare. Extracts obtained from oregano can also be used.

  The olive leaf used in the present invention is a leaf of the Oleaceae plant Olea europea. Extracts obtained from olive leaves can also be used.

  The saps used in the present invention is the fruit of the gummy family plant Hippophaer rhamnoides. Extracts obtained from Sashimi can also be used.

  The curry leaf used in the present invention is the leaf of the mandarinae plant, Murraya koenigii. Extracts obtained from curry leaf can also be used.

  Red ginger, black ginger, Nikkei, barley young leaves, black garlic, Asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under snow, jasmine tea, oregano, olive leaf, sapin, Alternatively, the extract from curry leaf may be a water or solvent extract and a supercritical carbon dioxide extract obtained by the above procedure, and the obtained extract may be vacuum-dried or spray-dried (spray-dried) known in the art. The solid content obtained by removing the solvent by a method such as) and the fraction obtained by further purifying these are also included.

  For preferred purification procedures and conditions in the present invention, for example, silica gel column chromatography, reverse phase ODS column chromatography and preparative HPLC are combined, and eluent (for example, water or hexane, ethyl acetate) under suitable conditions. , Various organic solvents such as chloroform, methanol and n-butanol, or a mixture thereof), but is not particularly limited thereto.

  From the above red ginger, black ginger, Nikkei, barley young leaves, black garlic, Asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under snow, jasmine tea, oregano, olive leaf, sapin, or curry leaf The fraction obtained by further purifying the extract preferably contains polyphenols.

(Fat absorption inhibitor and lipase inhibitor)
The fat absorption inhibitor and the lipase inhibitor of the present invention are red ginger, black ginger, nikkei, barley young leaves, black garlic, asen medicine, hydrangea, eggplant, pomegranate, flaxseed, katsura tea, Kuju tea, under snow, jasmine tea, The composition contains at least one plant selected from the group consisting of oregano, olive leaf, spruce, or curry leaf or an extract thereof as an active ingredient, and particularly preferably contains an extract containing polyphenols. The fat absorption inhibitor and lipase inhibitor of the present invention, when taken before or during a meal, make the ingested fat less susceptible to enzymatic hydrolysis by pancreatic lipase, resulting in a decrease in the amount of absorbed fat from the intestinal tract. Can be. Therefore, even if a diet high in fat is ingested, absorption of fat in the body can be suppressed.

  The fat absorption inhibitor or lipase inhibitor of the present invention is used as food, pharmaceuticals and the like. The shape of food, medicine, etc. is appropriately set according to the purpose. For example, an additive usually used by those skilled in the art (for example, excipients such as dextrin, starch, saccharides, calcium phosphate, fragrance, perfume oil, etc.) may be used to form tablets, granules, or the like, or It may be dissolved in water, beverages or the like to form a liquid. Preferably, it is in the form of a capsule, granule, tablet or beverage.

  As a method for producing capsules, a conventionally known method for producing soft capsules may be used except that the above plant or extract is used as the contents. Examples of such a production method include a method of encapsulating contents with a rotary filling machine using a capsule film sheet and molding a capsule preparation, or a method of producing seamless capsules by a dropping method.

  As for the granules, various known wet and dry granulation methods can be applied, and the granules are molded together with appropriate binders and excipients. Tablets are prepared by known tableting methods by adding appropriate binders, excipients, disintegrants and, if necessary, lubricants to the granules containing the plant or the extract or the extract itself. be able to. Furthermore, about a drink, an appropriate saccharide | sugar, an acid, a fragrance | flavor, etc. can be added, a flavor can be adjusted, and it can prepare by a well-known manufacturing method.

  The intake of the fat absorption inhibitor or lipase inhibitor of the present invention is preferably performed before or during a meal. The fat absorption inhibitor or lipase inhibitor of the present invention is, for example, red ginger, black ginger, nikkei, barley young leaves, black garlic, asen, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under snow, jasmine When using water and / or solvent extracts from tea, oregano, olive leaves, shaba spine, or curry leaf, it is usually preferable to take 100-500 mg per adult three times a day during a meal. Moreover, when using the purified fraction from the said water and / or solvent extract as an extract, it is preferable to normally ingest 20-100 mg per adult at the time of a meal 3 times a day. The intake can be appropriately increased or decreased depending on the age, the intake of fat, and the like.

  When the fat absorption inhibitor or lipase inhibitor of the present invention is provided as a food, the amount of the plant or extract in such food is within a range that does not impair the original taste of the food, depending on the type of the target food. What is necessary is just to add. Usually, it may be added within a range of 0.1 to 10% by mass with respect to the target food.

  EXAMPLES Next, although an Example is given and this invention is further demonstrated, this invention is not limited to these Examples.

Example 1: Preparation of extracts from various plants
Dried red ginger, black ginger, Nikkei (bark, root, leaves, and branches), barley young leaves, black garlic, Asen, hydrangea, aubergine, pomegranate, flaxseed, katsura, Kuju tea, under snow, jasmine tea, Oregano, olive leaf, shaba spine, and curry leaf were each pulverized with a pulverizer to obtain powder. Extraction was performed by adding 1000 mL of 70% (v / v) acetone aqueous solution to 100 g of each powder and allowing to stand at room temperature for 1 week. After filtration through filter paper, the filtrate was collected, concentrated under reduced pressure, and dried to obtain a 70% (v / v) acetone extract. The yield of the obtained extract was 9.3%, 9.6%, and 15.2% for red ginger, black ginger, and nikkei (bark), respectively.

(Example 2: Pancreatic lipase inhibition test of various plant extracts)
The lipase inhibition test was performed using a porcine pancreatic lipase (Sigma) and a lipase kit S (Dainippon Pharmaceutical). First, red ginger, black ginger, Nikkei (bark, root, leaf, or branch), barley young leaf, black garlic, asen, hydrangea, eggplant, pomegranate, flaxseed, Keika, Kuju tea obtained in Example 1 above. Under snow, jasmine tea, oregano, olive leaves, shaba spine, and curry leaf extracts were each prepared in a dilution series of 20 times the final concentration in dimethyl sulfoxide. For each extract, add a coloring solution (390 μL), a dilution series (25 μL each), a lipase solution (25 μL) prepared to 40 μg / mL with a buffer provided with the kit, and an esterase inhibitor (10 μL). Each was reacted at 30 ° C. for 30 minutes. After adding a reaction stop solution (1 mL), the absorbance at 405 nm was measured, and the enzyme inhibition rate was calculated from the following formula.

In the above formula, ODsample is the absorbance of the extract of various concentrations after enzyme treatment, ODsample blank is the absorbance of the extract of various concentrations when no enzyme is added, and ODcontrol is the absorbance of the extract without addition of the enzyme and enzyme treatment. Furthermore, ODcotrol blank represents the absorbance when neither extract nor enzyme was added. Table 1 shows the 50% pancreatic lipase activity inhibitory concentration (IC ₅₀ ) of various extracts. Further, as a positive control, a concentrate obtained by concentrating a commercially available Oolong tea beverage about 300 times was evaluated in the same manner.

  As can be seen from Table 1, red ginger, black ginger, Nikkei (bark, root, leaf, or branch), barley young leaves, black garlic, asen, hydrangea, eggplant, pomegranate, flaxseed, katsura flower, Kuju tea, under the snow , Jasmine tea, oregano, olive leaf, shaba spine, and curry leaf extract were found to have pancreatic lipase inhibitory action.

(Example 3: Confirmation of fat absorption inhibitory action of red ginger, black ginger and Nikkei (bark) extract)
For the red ginger, black ginger and Nikkei (bark) extract obtained in Example 1 above, the fat absorption inhibitory effect was evaluated by measuring the change in serum triglyceride concentration by oral administration to olive oil-loaded mice. Red ginger, black ginger and Nikkei extracts were suspended in a 5% (w / v) aqueous gum arabic solution to prepare an aqueous suspension of each extract. To ddY male mice fasted for 20 to 24 hours, an aqueous suspension was orally administered at a rate of 10 mL / kg body weight, and olive oil was immediately orally administered at a rate of 5 mL / kg body weight, 2, 4 and 6 hours. Later, blood was collected from the orbital vein and the serum triglyceride concentration was measured. The results of oral administration for red ginger, black ginger and Nikkei extract (dose: 250 or 500 mg / kg) are shown together in Table 2. Further, as a positive control, a concentrate obtained by concentrating a commercially available Oolong tea beverage about 300 times was evaluated in the same manner.

  As can be seen from Table 2, red ginger, black ginger, and Nikkei (bark) extracts strongly suppress the increase in blood triglycerides compared to the concentrate of commercially available oolong tea drinks that are said to have fat absorption inhibitory action. It was. From these results, it was found that these extracts suppress the action of pancreatic lipase and express the fat absorption inhibitory action.

  According to the present invention, plants having a strong pancreatic lipase inhibitory activity (red ginger, black ginger, nikkei (bark, root, leaf, or branch), barley young leaves, black garlic, asen, hydrangea, eggplant, pomegranate, flaxseed , Katsura, Kubushi tea, under snow, jasmine tea, oregano, olive leaf, shaba spine, and curry leaf) or an extract thereof is provided.

  The fat absorption inhibitor and lipase inhibitor of the present invention, when taken before or during a meal, make the ingested fat less susceptible to enzymatic hydrolysis by pancreatic lipase, resulting in a decrease in the amount of absorbed fat from the intestinal tract. Can be. Therefore, even if you eat a diet high in fat, absorption of fat into the body can be suppressed, so it is useful for prevention and treatment of lifestyle-related diseases such as obesity, arteriosclerosis, hypertension, myocardial infarction, cerebral infarction, diabetes It is.

Claims (2)

  Group consisting of black ginger, red ginger, Nikkei, barley young leaves, black garlic, Asen medicine, hydrangea, aubergine, pomegranate, flaxseed, katsura tea, Kuju tea, under the snow, jasmine tea, oregano, olive leaf, shaba spine, and curry leaf A fat absorption inhibitor comprising at least one plant selected from the above or an extract thereof as an active ingredient.   Group consisting of black ginger, red ginger, Nikkei, barley young leaves, black garlic, Asen medicine, hydrangea, aubergine, pomegranate, flaxseed, katsura tea, Kuju tea, under the snow, jasmine tea, oregano, olive leaf, shaba spine, and curry leaf A lipase inhibitor comprising as an active ingredient at least one plant selected from the above or an extract thereof.