JP2014195425A - Method for production of artichoke extract - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide means which can efficiently extract a water-soluble active ingredient from an artichoke and also efficiently extract a linoleic acid derivative, being a lipophilicity component.SOLUTION: When artichoke extract is produced from artichoke, an artichoke is treated with a plant tissue collapse enzyme and then water with pH 7 to 12 is used as an extracting solvent to extract at 40-121°C.

Description

  The present invention relates to a method for producing an artichoke-derived extract.

  Artichoke (scientific name: Cynara scolymus L.) is a vegetable cultivated mainly in Europe and the United States, and its water extract has anti-allergic effects It is known to show many pharmacological actions (see, for example, Patent Document 1).

  In addition, so far, the water-soluble substance synaroside contained in artichoke has been reported as a compound having an effect of inhibiting cholesterol biosynthesis (see, for example, Non-Patent Document 1). In addition, it has been clarified that artichokes include many useful water-soluble substances, such as flavonoid glycosides such as scolimoside, luteolin-7-O-lutinoside, and inulin, a polysaccharide (for example, Patent Document 2). And non-patent document 2).

JP 2003-286184 A Special table 2008-535983 gazette

Rolf Gebhardt, J Pharmacol Exp Ther, Vol. 286, No. 3 (1998) pp. 1122-1128 Negro D et al., J Food Sci, Vol. 77, No. 2 (2012) pp. 244-252

  By the way, in recent years, the present inventors have found that linoleic acid derivatives, which are fat-soluble components derived from artichokes, have a cell activation action, an antioxidant stress action, a cell growth inhibitory action, etc., and have filed patent applications. Application 2012-064301, Japanese Patent Application No. 2012-064298, and Japanese Patent Application No. 2013-60763).

  Here, the linoleic acid derivative is a fat-soluble component. Originally, as a method for efficiently extracting a linoleic acid derivative that is a fat-soluble component, a method using an organic solvent such as hexane or ethyl acetate as an extraction solvent is desirable. However, considering the use of the extract for food, an organic solvent cannot be used as the extraction solvent. An extraction method using ethanol as an extraction solvent is also conceivable, but it is extremely preferable to use water as the extraction solvent from the viewpoint of equipment and cost. Furthermore, when extraction is performed using ethanol or an aqueous ethanol solution, the extraction efficiency of dietary fiber contained in artichoke and the above-mentioned water-soluble active ingredient is reduced, so that it contains various active ingredients originally contained in artichoke. In order to produce an extract for food, it can be said that water is preferably used as an extraction solvent.

  However, there is no known method that can efficiently extract a water-soluble active ingredient from artichoke using water as an extraction solvent and can also efficiently extract a linoleic acid derivative that is a fat-soluble ingredient. .

  Accordingly, an object of the present invention is to provide means for efficiently extracting a linoleic acid derivative, which is a fat-soluble component, while efficiently extracting a water-soluble active ingredient from artichoke.

  In view of the current state of the prior art as described above, the present inventors have intensively studied. In the process, surprisingly, after treating artichoke with a plant tissue disrupting enzyme, the above problem can be solved by performing extraction under a predetermined temperature condition using water having a predetermined pH as an extraction solvent. The headline and the present invention have been completed.

  That is, according to one aspect of the present invention, a method for producing an artichoke-derived extract from artichoke (a method for producing an artichoke-derived extract) is provided. And the said manufacturing method is characterized by including the process of extracting at 40-121 degreeC using the water of pH 7-12 as an extraction solvent, after processing artichoke with a plant tissue disintegration enzyme.

  According to the other form of this invention, the artichoke origin extract which can be obtained with said manufacturing method is provided.

  Moreover, according to the further another form of this invention, the foodstuff and medicine containing said artichoke origin extract are provided.

  ADVANTAGE OF THE INVENTION According to this invention, the means which can extract efficiently the linoleic acid derivative which is a fat-soluble component is provided, extracting a water-soluble active ingredient efficiently from artichoke.

  According to one aspect of the present invention, there is provided a method for producing an artichoke-derived extract from artichoke, wherein the artichoke is treated with a plant tissue-disintegrating enzyme and then adjusted to 40-121 ° C. using water having a pH of 7-12 as an extraction solvent. There is provided a method for producing an artichoke-derived extract comprising a step of performing extraction.

  Artichoke (Cynara scolymus) is a kind of medicinal herb, also known as datura, and belongs to the genus Asteraceae (Cynara) in terms of biological classification. Artichokes are widely produced commercially throughout Asia, Europe, North Africa and North and South America, and among these, those from Vietnam are particularly preferred. There are no particular restrictions on the varieties, and examples include green glove species, violet species, imperial star species, and Carldon species, all of which can be preferably used. Moreover, the site | part which can use artichoke is not specifically limited, The 1 type (s) or 2 or more types selected from the group which consists of site | parts, such as a stem, a leaf, and a flower part, are mentioned. That is, a partial position may be used alone, or a plurality of sites may be mixed and used. Furthermore, the artichoke may be natural or artificially cultivated, and any of fresh, dried, frozen, and freeze-dried can be used, but a dried one is preferably used.

  The present inventors include abundant linoleic acid derivatives, which are fat-soluble components without using an organic solvent, by performing extraction at 40 to 121 ° C. using water having a pH of 7 to 12 as an extraction solvent. It has been found that artichoke-derived extracts can be produced. In addition, as clarified in a series of patent applications by the applicant of the present invention described above, the linoleic acid derivative contained in the obtained artichoke-derived extract in the present invention includes the following chemical formulas 1 to 4:

The compound represented by these is illustrated. Hereinafter, the method for producing an artichoke-derived extract according to the present invention will be described in detail step by step.

[Preprocessing]
The artichoke used as a raw material can be used as it is, but is preferably washed with water. By washing with water, impurities adhering to the artichoke can be removed, and the purity of the extract can be improved. In such a case, the artichoke may be dried after the artichoke is washed with water.

  In this step, for example, water of 0.5 to 50 times the mass of artichoke is added to the artichoke and crushed to obtain a crushed artichoke. The amount of water added is not particularly limited as long as it is within the above range, but it is preferable to adjust appropriately depending on the state of artichoke. For example, when the artichoke is used in a fresh or frozen state, the artichoke contains water to some extent. For this reason, in such a case, it is sufficient to add a relatively small amount of water. Specifically, the water is 0.5 to 10 times the mass of the artichoke, more preferably It is preferable to add 1 to 5 times the mass. Further, when the artichoke is used in the form of a dried product or a freeze-dried product, the artichoke contains little or little water. For this reason, in such a case, it is necessary to add water in a relatively large amount as compared with the case of using it in a raw or frozen state. Specifically, water is added to the mass of artichoke, It is preferable to add 5 to 50 times the mass, more preferably 10 to 30 times the mass. Within such a range, the artichoke can be efficiently crushed. In this specification, “relative to the mass of artichoke” means that the mass of the artichoke as a raw material is used as a reference.

  The water used in the present specification is not particularly limited, and any of tap water, distilled water, pure water, ion-exchanged water, and the like may be used.

  Moreover, the crushing of this process is not specifically limited, It is performed by a well-known method. For example, a crusher such as a blender, a stone mill type crusher, a roller mill, a cutter mill, a ball mill, a jet mill, a hammer mill or the like can be used. Alternatively, the artichoke is mechanically processed in advance using a pulverizer as described above to obtain a coarse piece of artichoke, and then the coarse piece is further crushed by ultrasonic waves to obtain a crushed artichoke. Good. In the latter case, the artichoke that is mechanically processed is preferably crushed so as to have a size of about 10 μm or less. The ultrasonic crushing conditions are not particularly limited as long as the artichoke becomes an appropriate size, but the treatment is preferably performed for 5 to 20 minutes. The size of the artichoke crushed material obtained in this step is not particularly limited. Preferably, the size of the crushed artichoke is about 0.001 to 2 mm, more preferably about 0.005 to 1 mm. If it is such a magnitude | size, the enzyme process using the plant-tissue disintegration enzyme mentioned later is performed efficiently, and the improvement of extraction efficiency of fat-soluble components, such as a linoleic acid derivative, by the subsequent hot water extraction operation can be anticipated.

  In the above operation, if necessary, water may be added after crushing for the purpose of improving the efficiency of heat treatment or enzyme treatment. At this time, the amount of water added is not particularly limited, and is appropriately selected depending on the desired effect. Preferably, in this step, the total amount of water added to the artichoke is such an amount that is in the above range with respect to the mass of the artichoke.

  Next, it is preferable to heat (sterilize) the obtained crushed artichoke. Since many microbes are attached to the artichoke, sterilization treatment at this stage suppresses the growth of these microorganisms in the next process, and the microorganism itself or secretion from the microorganisms undergo enzyme treatment in the next process. Inhibition can be prevented. In addition, in the following and subsequent steps, the propagated microorganisms may assimilate the extracted components, or secrete toxins that are not desirable as foods. The propagation of the attached bacteria can be prevented in the subsequent manufacturing process. In addition, since the tissue (for example, cell wall) of the artichoke crushed material can be further partially pyrolyzed, the resulting artichoke crushed heated product is easily subjected to enzyme treatment in the next step, resulting in a hot water extraction step. The extraction efficiency can be increased.

  The heating conditions for the crushed artichoke are not particularly limited as long as the above-described effects can be achieved. For example, the crushed artichoke is preferably heated at 80 to 121 ° C. for 5 to 60 minutes, and more preferably heated at 80 to 121 ° C. for 10 to 30 minutes.

[Treatment with plant tissue disrupting enzymes]
In the method for producing an artichoke-derived extract of the present invention, the artichoke is treated with a plant tissue disrupting enzyme before the extraction step using an extraction solvent. There is no restriction | limiting in particular about the specific structure of a plant tissue disintegration enzyme, What is necessary is just an enzyme which can disintegrate the artichoke structure | tissue. Examples of plant tissue disrupting enzymes include cellulase, hemicellulase and pectinase.

  Here, cellulase and hemicellulase may be derived from any source having cellulase activity or hemicellulase activity, and are not particularly limited. For example, aspergillus niger, Trichoderma reesei, Trichoderma viride, Trichoderma longibrachiatum, Streptomyces lividans, Bacillus subtilis, Pyrococcus horikoshii, Clostridium thermocellum, Humicola, Pyrococcus horikoshii, etc .; Abalone, Ezobora Derived from shellfish such as bivalves; Derived from nematodes such as pine wood nematodes; Etc. Cellulase and hemicellulase may be produced from the above-mentioned appropriate sources by known methods, but commercially available products may be used. Examples of commercially available cellulases include cellulase A “Amano” 3, cellulase T “Amano” 4 (both manufactured by Amano Enzyme Co., Ltd.); Spezyme CP, GC220, Multifect CL, Prima First, Inage, Inage Neutra, Accelerase, Optimash, Multifect CX10L, Optimase CX40L, Puradax HA (all manufactured by Genencor Kyowa Co., Ltd.); GODO-TCF, GODO-TCL, GODO TCD-H3 (all manufactured by Godo Sake Co., Ltd.) ; Sofitergen C-1 (manufactured by Taisho Technos Co., Ltd.); super thermostable cellulase (manufactured by Thermostable Enzyme Laboratory Co., Ltd.); cell riser, cellulase XL-522, cell team C, cell riser HT Conch, cellulase SS , Cellulase XL-531 (all manufactured by Nagase ChemteX Corporation); bakezyme XE (manufactured by Nippon Shibel Hegner Co., Ltd.); Cellsoft, Denimax, Carezyme, Cellzyme, Cell Crust (all manufactured by Novozymes Japan Co., Ltd.) Cellulosin AC40, cellulosin AL, cellulosin T3, cellulosin TF (A feed) (all manufactured by HIBI Co., Ltd.); cellulase "Onozuka" 3S, cellulase Y-NC, pancerase br (all manufactured by Yakult Pharmaceutical Co., Ltd.) CellSEB Ts (manufactured by Higuchi Shokai Co., Ltd.); Sumiteam AC, Sumiteam C (both manufactured by Shin Nippon Chemical Industry Co., Ltd.); Sucrase C (manufactured by Mitsubishi Chemical Foods); Entilon CM, Entilon MCH, Biohit , Biostar, Fedrase Co., Ltd.)), and the like. Commercially available hemicellulases include, for example, hemicellulase “Amano” 90 (manufactured by Amano Enzyme Co., Ltd.); Bakezyme HS2000, Bakezyme 1 Conc (both manufactured by Nihon Shibel Hegner Co., Ltd.); Industrial Co., Ltd.); Sucrase X (Mitsubishi Chemical Foods Co., Ltd.) and the like.

  Examples of the pectinase include sucrase N and sucrase A (both manufactured by Mitsubishi Chemical Foods).

  The cellulase, hemicellulase and pectinase are not limited to the above. In addition, these plant tissue-disrupting enzymes may be used alone or in combination of two or more, or may be used in combination of cellulase, hemicellulase and pectinase as appropriate.

  The amount of the enzyme added when the artichoke is treated with the plant tissue-disintegrating enzyme is not particularly limited as long as the artichoke subjected to the extraction can be sufficiently treated with the enzyme, and can be appropriately selected depending on the type of the enzyme used. For example, the addition amount of the enzyme is preferably 0.01 to 10% by mass and more preferably 0.02 to 5% by mass with respect to 100% by mass of the artichoke that is the raw material. Within such a range, the artichoke can be sufficiently treated with an enzyme. During the enzyme treatment, it is preferable to mix with an agitator or the like so that the artichoke and the enzyme can be mixed uniformly and sufficiently.

  The enzyme treatment conditions are not particularly limited as long as the artichoke can be sufficiently treated with the enzyme. For example, the enzyme treatment temperature is preferably 20 to 60 ° C., more preferably 25 to 55 ° C., and the enzyme treatment time is preferably 0.1 to 16 hours, more preferably 0.5 to 8 hours. In addition, when using 2 or more types of enzymes together, you may add simultaneously and perform an enzyme treatment, or you may repeat an enzyme treatment using each enzyme independently. Of these, when the optimum conditions for each enzyme are different, the latter treatment is preferably performed. In addition, when performing an enzyme process repeatedly, it is preferable to perform an enzyme deactivation process between each enzyme process.

[Extraction process]
In the production method according to the present invention, an extraction step using an extraction solvent is performed after the treatment with the above-described plant tissue-disrupting enzyme. The extraction solvent is not particularly limited as long as it is a neutral to alkaline aqueous solvent substantially free of an organic solvent. For example, an inorganic base (for example, an alkali metal hydroxide such as sodium hydroxide or potassium hydroxide; Alkali earth metal hydroxides such as magnesium hydroxide and barium hydroxide; Alkali metal carbonates such as sodium carbonate and potassium carbonate; Alkaline earth metal carbonates such as magnesium carbonate and barium carbonate; Alkaline aqueous solution containing an alkali metal hydrogen carbonate such as potassium hydrogen carbonate; ammonium carbonate or ammonia; an organic base (for example, an organic acid salt of an alkali metal such as sodium acetate or potassium propionate; magnesium formate, magnesium acetate, etc. Organic acid salts of alkaline earth metals; trimethylamine, ethyl acetate An aqueous alkaline solution containing amines such as nitrogen, diethylamine, triethylamine, propylamine, butylamine, and piperidine; a nitrogen-containing heterocyclic compound such as pyridine), and an alkaline suspension containing an anion exchange resin. Of these, an aqueous sodium carbonate solution, an aqueous sodium hydroxide solution, or an anion exchange resin suspension can be suitably used.

  The content of the inorganic base, organic base or anion exchange resin in the extraction solvent is not particularly limited, and can be adjusted so that the pH of the extraction solvent becomes a value within a predetermined range.

  Here, the pH of the extraction solvent is neutral to alkaline, and is not particularly limited as long as it is specifically 7 to 12, but is preferably 7 to 11, and more preferably 7.5 to 10.

  The treatment temperature with the extraction solvent needs to be treated at an extraction temperature of 40 to 121 ° C. from the viewpoint that a sufficient amount of the linoleic acid derivative can be extracted. The extraction temperature is preferably 40 to 100 ° C. in that more linoleic acid derivatives can be extracted in a short time.

  Although the processing time with the extraction solvent varies depending on the processing temperature, for example, in the case of a processing temperature of 40 to 100 ° C., 1 to 16 hours is preferable, and 1 to 8 hours is more preferable.

  By further removing the extraction residue from the extract obtained by the production method described above, the artichoke-derived extract according to the present invention can be obtained. Examples of the step of removing the extraction residue include centrifugation, filtration, and ultrafiltration, but a filtration method suitable for large-scale production can be used more suitably. In the filtration, a filter aid can be used, and an example of the filter aid is Celite # 545.

  In the present specification, the “extract” refers to a substance obtained by a process of performing an extraction operation using an extraction solvent. Further, the extract obtained by subjecting the substance to further treatment such as filtration, centrifugation, concentration, ultrafiltration, molecular sieving, neutralization and the like is also included in the extract of the present invention. In addition, a fraction obtained by fractionating the above substances by a known method and a fraction obtained by repeating the fractionation operation a plurality of times are also included in the extract of the present invention. Examples of the fractionation means include extraction, fractional precipitation, column chromatography, thin layer chromatography and the like.

  In the present invention, the shape of the extract of the present invention is not particularly limited, but may be any of powder, solid, and liquid. When powdered, there is no particular limitation, but the extract extracted from the raw material with an alkaline aqueous solvent is concentrated, further added with excipients such as dextrin, sucrose fatty acid ester and lactose, dried and pulverized Thus, the extract of the present invention can be obtained. Moreover, the granular solid substance obtained by granulating the said extract by a well-known method can also be used as an extract of this invention. There are no particular limitations on the granulation method, but rolling granulation, stirring granulation, fluidized bed granulation, air flow granulation, extrusion granulation, compression molding granulation, pulverization granulation, spray granulation, spray granulation, or spray granulation. Examples are grains. Further, as the liquid extract, in addition to the liquid itself obtained by the method for producing the extract, its concentrate or dilution, the above-mentioned powdery extract is dissolved in a liquid such as water or alcohol. The liquid form is exemplified.

  The artichoke-derived extract according to the present invention is characterized by containing a large amount of linoleic acid derivatives such as the compounds represented by the above chemical formulas 1 to 4 which are physiologically active components derived from artichoke, for example, 10 μg or more per 1 g of dried solid product More specifically, it is an extract containing 100 to 500 μg of linoleic acid derivative per 1 g of the dried product. The weight per 1 g of the dried product refers to the weight of the target component in 1 g of the dried product obtained when the liquid is dried with an evaporator or the like.

  The food according to the present invention contains the artichoke-derived extract. Since the food according to the present invention contains many linoleic acid derivatives derived from artichokes of the compounds represented by the above chemical formulas 1 to 4, it can be expected to have a cell activation action, an antioxidant stress action, a cell growth inhibitory action, and the like. As the food, for example, a health food (a food for specified health use) with a label indicating that it is used for expression of a desired effect by a cell activation action, an antioxidant stress action, or a cell growth inhibitory action. You can also.

  There is no limitation in particular in the manufacturing method of the foodstuff which concerns on this invention. For example, blending, cooking, processing, and the like may be in accordance with those of general foods, and can be produced by their production method, and the obtained food may contain the extract according to the present invention. Further, the artichoke-derived extract itself of the present invention may be used as food.

  In the food according to the present invention, “containing” means containing, adding and / or diluting. Here, “containing” means that the extract used in the present invention is contained in the food, and “addition” means that the extract used in the present invention is added to the raw material of the food. "Dilution" refers to an embodiment in which a food material is added to the extract used in the present invention.

  The food according to the present invention is not particularly limited, but for example, processed cereal products (eg, processed flour products, processed starch products, processed premix products, noodles, macaroni, breads, bean paste, buckwheat) , Rice cakes, rice noodles, harsame, packaging rice cakes, etc.), processed oils and fats (eg, plastic oil, tempura oil, salad oil, mayonnaise, dressing, etc.), processed soybeans (eg, tofu, miso, natto, etc.), processed meat Products (eg, ham, bacon, press ham, sausage, etc.), marine products (eg, frozen groundnut, kamaboko, chikuwa, hanpen, fried fish, fish, ham, sausage, dried bonito, processed fish egg, canned fish ), Dairy products (eg, raw milk, cream, yogurt, butter, cheese, condensed milk, powdered milk, ice cream, etc.), processed vegetables and fruits (eg, pastes, jams, Foods, fruit drinks, vegetable drinks, mixed drinks, etc.), confectionery (eg, chocolate, biscuits, confectionery breads, cakes, candy sweets, rice confectionery, etc.), alcohols (eg, sake, Chinese sake, wine, whiskey) , Shochu, vodka, brandy, gin, rum, beer, soft alcoholic beverage, fruit liquor, liqueur, etc.), favorite beverages (eg, green tea, tea, oolong tea, coffee, health beverage, soft drink, lactic acid beverage, etc.), seasoning (Eg, soy sauce, sauce, vinegar, mirin, etc.), canned / bottled / packed food, semi-dried or concentrated food (eg, liver paste, other spreads, buckwheat / noodle soup, concentrated soup), dried Food (eg, instant noodles, instant curry, instant coffee, powdered juice, powdered soup, instant miso soup, cooked food, cooked beverage, cooked soup, etc.), frozen food Etc. The.

  The food according to the present invention is not particularly limited as long as it contains the extract, and includes orally ingestible shapes such as tablets, granules, and capsules. Moreover, glycerin etc. can be added to the said extract, and it can also be set as the health food with which the said extract was concentrated.

  The content of the extract in the food according to the present invention is not particularly limited, and can be set as appropriate from the viewpoint of its sensory and activity expression. For example, the dry weight of the extract in the food is 0.1 to 100 wt. %, Preferably 0.5 to 95% by weight, more preferably 1 to 90% by weight.

  The medicament according to the present invention contains the artichoke-derived extract described above. Examples of the medicament according to the present invention include those prepared by combining the above extract according to the present invention with a known pharmaceutical carrier.

  The medicament according to the present invention is usually produced by blending the extract with a pharmaceutically acceptable liquid or solid carrier, and optionally, a solvent, a dispersant, an emulsifier, a buffer, a stabilizer, an excipient. In addition, a binder, a disintegrant, a lubricant, and the like can be added to form a solid agent such as a tablet, a granule, a powder, a powder, and a capsule, and a liquid agent such as a normal solution, a suspension, and an emulsion. Moreover, it can also be used as a dried product which can be made liquid by adding an appropriate carrier before use, and other external preparations.

  The pharmaceutical carrier can be selected according to the administration form and dosage form of the medicament of the present invention. In the case of an oral preparation comprising a solid composition, it can be a tablet, pill, capsule, powder, fine granule, granule, etc., for example, starch, lactose, sucrose, mannitol, carboxymethylcellulose, corn starch Inorganic salts are used as carriers. In preparation of the oral preparation, a binder, a disintegrant, a surfactant, a lubricant, a fluidity promoter, a corrigent, a colorant, a fragrance and the like can be further added. For example, in the case of a tablet or pill, if desired, it may be coated with a sugar coating such as sucrose, gelatin or hydroxypropylcellulose, or a film of a gastric or enteric substance. In the case of an oral preparation comprising a liquid composition, it can be a pharmacologically acceptable emulsion, solution, suspension, syrup, etc. For example, purified water, ethanol, etc. are used as a carrier. Is done. Further, if desired, auxiliary agents such as wetting agents and suspending agents, sweetening agents, flavoring agents, preservatives and the like may be added. In addition, since the extract of the present invention exhibits a sufficient effect even by oral administration, it is a suitable form for use as a pharmaceutical for oral administration from the viewpoint of ease of administration.

  On the other hand, in the case of a parenteral preparation, distilled water for injection, physiological saline, aqueous glucose solution, vegetable oil for injection, sesame oil, peanut oil, soybean oil, corn oil as a diluent for the extract of the present invention as a diluent according to a conventional method It can be prepared by dissolving or suspending in propylene glycol, polyethylene glycol or the like, and adding a bactericidal agent, stabilizer, isotonic agent, soothing agent, etc., if necessary. In addition, a solid composition can be produced and dissolved in sterile water or a sterile solvent for injection before use.

  External preparations include solid, semi-solid or liquid preparations for transdermal administration or transmucosal (oral or intranasal) administration. Also included are suppositories and the like. For example, emulsions such as emulsions and lotions, tinctures for external use, liquid preparations such as liquids for transmucosal administration, ointments such as oily ointments and hydrophilic ointments, transdermal administration such as films, tapes, and poultices Or a patch for transmucosal administration.

  Each of the above-mentioned various preparations can be appropriately produced by a conventional method using a known pharmaceutical carrier. In addition, the content of the extract in such a preparation is not particularly limited as long as the extract can be administered within the dosage range described below, preferably in consideration of its administration form, administration method, and the like. . As content of the said extract in the pharmaceutical of this invention, it is about 0.1 to 100 weight% by dry weight.

  The dosage of the medicament of the present invention is appropriately set depending on the preparation form, administration method, purpose of use and age, weight, and symptom of the patient to whom the medicament is administered, and is not constant. In general, the amount of the extract contained in the preparation is expressed as a dry weight, for example, 1 μg to 100 mg / kg body weight per day for an adult, preferably 5 μg to 50 mg / kg body weight, more preferably 10 μg. -10 mg / kg body weight. Of course, since the dosage varies depending on various conditions, an amount smaller than the above dosage may be sufficient or may be necessary beyond the range. Administration may be carried out in a single dose or divided into several doses within a desired dose range. The administration period is also arbitrary. Moreover, the medicament of the present invention can be orally administered as it is, or can be added to any food or drink and taken on a daily basis.

  The linoleic acid derivative can be purified by subjecting the artichoke-derived extract obtained by the method for producing an artichoke-derived extract according to the present invention to a purification treatment. As a specific method of purification, a known method can be used, and examples thereof include extraction, fractional precipitation, column chromatography, thin layer chromatography, and a combination of these methods. Examples of column chromatography include high performance liquid chromatography.

  Hereinafter, preferred embodiments of the present invention will be described in more detail by way of examples. However, the technical scope of the present invention should not be construed as being limited to the following examples.

<Example>
The dried artichoke was crushed with a blender, and 30 mL of water was added to 3 g of the obtained crushed artichoke. Thereafter, 3 mg of cellulase XP-425 (manufactured by Nagase ChemteX Corporation) and sucrase N (manufactured by Mitsubishi Chemical Foods Corporation) were added and stirred at 40 ° C. for 1 hour (pH unadjusted). The pH immediately after stirring was 5. Subsequently, 1N sodium hydroxide was added to adjust the pH to 9, and the mixture was further stirred at 80 ° C. for 2 hours. After the stirring, the artichoke residue was removed by centrifugation to obtain an artichoke-derived extract in the form of an aqueous solution. In order to quantify the components in the obtained extract, the supernatant liquid containing the linoleic acid derivative was transferred to a separatory funnel, and then the liquid was separated by adding chloroform: methanol = 2: 1 solution. Each layer was collected. Each extraction layer was dried under reduced pressure with an evaporator to obtain a concentrate.

≪Comparative example 1≫
The dried artichoke was crushed with a blender, 30 mL of water was added to 3 g of the obtained crushed artichoke, and the mixture was stirred at 80 ° C. for 3 hours (pH unadjusted). The pH immediately after stirring was 5. After the stirring, the artichoke residue was removed by centrifugation to obtain an artichoke-derived extract in the form of an aqueous solution. In order to quantify the components in the obtained extract, the supernatant liquid containing the linoleic acid derivative was transferred to a separatory funnel, and then the liquid was separated by adding chloroform: methanol = 2: 1 solution. Each layer was collected. Each extraction layer was dried under reduced pressure with an evaporator to obtain a concentrate.

≪Comparative example 2≫
The dried artichoke was crushed with a blender, 30 mL of ethanol was added to 3 g of the obtained crushed artichoke, and the mixture was stirred at 80 ° C. under reflux conditions for 3 hours. After the stirring, the artichoke residue was removed by centrifugation to obtain an artichoke-derived extract in the form of a solution. In order to quantify the components in the obtained extract, the supernatant of the obtained extract was dried under reduced pressure using an evaporator to obtain a concentrate.

≪Evaluation≫
The contents of the water-soluble active ingredient and the linoleic acid derivative in the obtained extract were measured for each of the above-described Examples and Comparative Examples by the following method. The results are shown in Table 1 below.

[Method for measuring content of water-soluble active ingredient]
The weight of the concentrate derived from the aqueous layer was measured with a precision balance to determine the content of the water-soluble active ingredient.

[Method for measuring content of linoleic acid derivative]
To the concentrate derived from the organic solvent layer or the ethanol extract, 0.5 mL of acetonitrile: methanol = 5: 1 solution was added and stirred thoroughly, and then passed through a 0.45 μL (ADVANTEC Desmic25-cs) filter. The analysis was performed by HPLC under the following conditions.

  The analytical conditions were TSK-GEL ODS-80TS (4.6 mm × 150 mm) manufactured by Tosoh Corporation as the column, the eluent was 0.1% formic acid aqueous solution for liquid A, and acetonitrile for liquid B. Was 1.0 mL / min and isocratic elution was performed at A: B = 30: 70. The column temperature was 40 ° C., and the linoleic acid derivative was detected by measuring the absorbance at 278 nm to obtain the content of the linoleic acid derivative.

  From the results shown in Table 1, in the examples employing the extraction method according to the present invention, even without using an organic solvent as an extraction solvent in the extraction step, while sufficiently ensuring the yield of water-soluble components obtained from artichokes, It turns out that the linoleic acid derivative which is a fat-soluble component can also be extracted efficiently.

Claims (6)

A method for producing an artichoke-derived extract from artichoke,
A method for producing an artichoke-derived extract, comprising a step of treating artichoke with a plant tissue-disintegrating enzyme and then extracting at 40 to 121 ° C using water having a pH of 7 to 12 as an extraction solvent.   The production method according to claim 1, wherein the plant tissue-disrupting enzyme is one or more selected from the group consisting of cellulase, hemicellulase, and pectinase.   An artichoke-derived extract obtainable by the production method according to claim 1 or 2.   The artichoke-derived extract according to claim 3, comprising 10 μg or more of linoleic acid derivative per gram of the dried product.   A food containing the artichoke-derived extract according to claim 3 or 4.   A medicament comprising the artichoke-derived extract according to claim 3 or 4.