Classifications

• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/81—Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
  • A61P9/12—Antihypertensives

Definitions

• the present invention relates to a composition having an effect of lowering blood pressure containing an eggplant-derived component and a method for producing the same.
• the present inventors have studied the blood pressure-lowering action and vasodilatory active ingredient contained in fermented Kyou-baku (lactic acid fermented product of buckwheat plant), and mainly composed of a plurality of choline esters containing at least acetylcholine and propionylcholine.
• An extract composition containing a quaternary alkylammonium compound was provided, and it was clarified that the purified acetylcholine, propionylcholine, and butyrylcholine exhibited a hypotensive effect when they were administered orally once to spontaneously hypertensive rats (SHR).
• Patent Documents 1 and 2 lactic acid fermented product of buckwheat plant
• freeze-dried powders of edible plants such as eggplant and bamboo
• extracts of edible plants with ethanol or hydrous ethanol include active ingredients having a hypotensive action such as acetylcholine, which are orally administered. It was clarified that it can be used for intake (Patent Document 3).
• Patent Document 4 a blood pressure increase suppressing composition containing a vegetable squeezed product such as tomato, carrot and spinach and a germinated buckwheat squeezed product as an active ingredient, and a composition containing a water-soluble, sugar-free tomato extract Has been reported to be used as an antihypertensive drug (Patent Document 5).
• Patent Document 5 a blood pressure increase suppressing composition containing a vegetable squeezed product such as tomato, carrot and spinach and a germinated buckwheat squeezed product as an active ingredient
• Patent Document 5 a composition containing a water-soluble, sugar-free tomato extract
• the inventors of the present invention can prepare a composition having a lower blood pressure effect more effectively by using less raw materials, and if a composition having a more effective hypotensive effect is obtained, it can be used as a health food such as a supplement or a pharmaceutical product at a low cost and in a large amount. Focusing on the possibility of production, we sought a new material with a blood pressure lowering effect. Therefore, an object of the present invention is to provide a new composition having an effective blood pressure lowering action by simple preparation.
• the inventors of the present invention have found that all water-soluble components derived from eggplant (Solanum melongena) have an excellent systolic blood pressure lowering action in the course of intensive research to solve the above problems, and further researched. As a result, the present invention has been completed.
• the invention therefore relates to: [1] A composition for lowering blood pressure, which comprises, as an active ingredient, all water-soluble components of the fruits of eggplant (Solanum melongena). [2] A composition for lowering blood pressure, which comprises all water-soluble components of the fruits of eggplant (Solanum melongena). [3] The composition for lowering blood pressure according to the above [1] or [2], which is to be taken orally at a dose such that the amount of acetylcholine in all the water-soluble components is 0.5 ⁇ g/kg body weight to 50 mg/kg body weight. [4] The composition for lowering blood pressure according to any one of the above [1] to [3], which is a dry powder. [5] The composition for lowering blood pressure according to any one of the above [1] to [4], which is a food composition.
• a method for producing a composition for lowering blood pressure which comprises a component derived from eggplant (Solanum melongena), The said manufacturing method including extracting all the water-soluble components from an eggplant fruit.
• the production method according to the above [6], wherein the extraction is water extraction.
• Water extraction Adding water to the eggplant fruit after making it a dry powder and The production method according to [7] above, which comprises obtaining a supernatant from a dry powder added with water by centrifugation or obtaining a filtrate by suction filtration.
• the present invention can provide a composition having an excellent blood pressure lowering action, which can be simply and inexpensively produced from the fruits of eggplant (Solanum melongena).
• Eggplant fruit as a raw material of the composition of the present invention is widely edible, it is also possible to compose the composition of the present invention only natural ingredients, high safety, continuous for a long period of time Can be ingested.
• the composition of the present invention includes a water extract of eggplant fruit, a concentrated extract obtained by concentrating the extract, a dry powder (freeze-dried powder, hot-air dried powder, spray-dried powder, etc.), a suspension of the dried powder, and the like. It can be used for foods and drinks and pharmaceuticals in various forms.
• the blood pressure lowering composition of the present invention contains all water-soluble components of eggplant fruit as an active ingredient.
• the composition for lowering blood pressure of the present invention may consist of all water-soluble components of eggplant fruit.
• the total water-soluble component of eggplant fruit means a water-soluble component obtained by pressing the eggplant fruit, but is included in the juice obtained by adding water to the eggplant fruit and squeezing the juice. It also means all water-soluble components. For example, even when the water-insoluble component is unavoidably contained in the juice, or even when a part of the water-soluble component is inevitably left as a residue during the juice, it is contained in the juice. The component corresponds to the total water-soluble component.
• the eggplant used in the present invention is not particularly limited. Eggplants that are commonly eaten are preferred, and for example, varieties such as Tosataka, Shintaro, Ryoma, Senshumizu eggplant, batten eggplant, Hiroryo salad eggplant (also known as Yoshio), Higuranasaki, Ocho eggplant, Chikuyo, and Senryo are used. be able to.
• the amount of acetylcholine in the total water-soluble components is 0.5 ⁇ g/kg body weight to 50 mg/kg body weight, preferably 2 ⁇ g/kg body weight to 20 mg/kg body weight.
• the composition for lowering blood pressure of the present invention may be a dry powder such as a freeze-dried powder or a hot-air dried powder.
• the composition of the present invention can be used as a food composition such as various functional health foods or a pharmaceutical composition.
• a food composition such as various functional health foods or a pharmaceutical composition.
• it may be used in combination with an appropriate food additive.
• an appropriate food additive not limited to such a composition for food, green tea, black tea, oolong tea, millet tea, health drink, as a drink blended into sports drinks, or as a food blended into biscuits, bread, candy, etc., everyday It is also possible to provide it in a form that can be ingested physically.
• it can be used as a so-called supplement in a suitable dosage form in accordance with the following pharmaceutical preparations.
• dosage forms When it is used as a drug, it can be used as various dosage forms in combination with an appropriate drug additive according to the usual preparation method.
• dosage forms include solid preparations such as powders, granules, capsules, pills and tablets, and oral administration preparations such as liquid preparations such as water preparations, suspension preparations and emulsions.
• composition of the present invention When used as a food, it can be used not only as a general food and drink, but also as a functional health food that exerts a specific function to promote health.
• capsules containing the composition of the present invention as an active ingredient tablets, powders, supplements consisting of granules, bread, cakes, bakery foods such as cookies, sauces, Seasonings such as soups, dressings, mayonnaise, dairy products such as milk, yogurt, creams, confectionery such as chocolate and candy, or green tea, black tea, oolong tea, barley tea, millet tea, fruit juice, vegetable drinks, dairy drinks , Various beverages such as soft drinks and carbonated drinks.
• the dose varies depending on the ratio of each ingredient, and also varies depending on various factors such as age, weight, sex, symptoms of patient, administration method and the like. .. Further, it may be increased or decreased as appropriate depending on the degree of symptom improvement.
• the frequency of administration can be divided into one to several times a day.
• the amount of intake when the composition of the present invention is used as a food can be selected according to the case of oral administration of the above-mentioned drug.
• the dose and frequency of administration are not particularly limited.Therefore, the purpose of maintaining good health, taste, and palatability should be considered as long as no serious symptoms occur. Then, the intake amount may be selected without limitation.
• the composition of the present invention can be used for, for example, a subject with hypertension or a subject who is healthy (not hypertensive) but has high blood pressure.
• various additives can be added to the composition of the present invention.
• various ones can be used and are not particularly limited, and examples thereof include lactose hydrate, sucrose, glucose, reduced maltose, mannitol, saccharides such as sorbitol, corn starch, potato starch, and partial sugar.
• starches such as alpha starch, dextrin and pullulan and their derivatives, celluloses such as crystalline cellulose and microcrystalline cellulose, derivatives such as carboxymethyl cellulose, macrogol and magnesium aluminometasilicate. Can be mentioned. Of these, dextrin is more preferable.
• additive one type may be used alone, or two or more types may be used in combination. These additives are preferably contained in an amount of 1 to 1000 parts by weight, more preferably 10 to 300 parts by weight, based on 100 parts by weight of the composition of the present invention.
• the present invention in one aspect, relates to a method for producing a blood pressure lowering composition containing an eggplant-derived component.
• the production method of the present invention includes extracting all water-soluble components from eggplant fruits.
• the extraction method is not particularly limited as long as all the water-soluble components are obtained, but for example, the water contained in the eggplant fruit is used to squeeze the eggplant fruit without adding water to obtain a juice. You may extract by. Alternatively, water extraction may be performed. Water extraction is carried out by adding water to the eggplant fruit, squeezing the water-added fruit, adding water after making the eggplant fruit a dry powder, and drying the water-added dry powder. It may be to extract.
• the water added to the eggplant fruit is not particularly limited, and water in the temperature range of 5°C to 40°C may be added. It is preferable to add water at room temperature.
• the amount of water added is preferably 50 to 200 parts by mass, more preferably 75 to 150 parts by mass, and particularly preferably 100 parts by mass, relative to 100 parts by mass of the eggplant fruit as a raw material. When the amount of water is small, the extraction of the water-soluble component that is the active ingredient may be insufficient, and when the amount of water is large, the processing volume may be large, and it may not be easy to process it into a dry powder, for example.
• Eggplant fruit may be crushed before squeezing or extracting. Particularly in the case of water extraction, it is preferable to crush the eggplant fruit before or after adding water, and it is particularly preferable to crush it before adding water from the viewpoint of ease of crushing.
• the crushing can be performed in various forms such as, for example, cutting into strips, dice-shaped blocks, and pastes, but it is preferable to crush into pastes for easier squeezing.
• a juicer mixer, mill, crusher or the like can be used for example.
• Water used in the production method of the present invention is water generally used for food processing such as mineral water, distilled water, deionized water, ion-exchanged water, electrolyzed water, tap water, well water, and industrial water used for food. it can.
• the pH is also not particularly limited, but in order to stably hold acetylcholine, pH 9.0 to pH 3.0 is preferable, pH 8.0 to pH 4.0 is more preferable, and pH 6.5 to pH 4.5 is more preferable.
• Water whose pH has been adjusted using a pH adjuster such as ascorbic acid can be used.
• ethanol may be added in order to reduce contamination of bacteria during the juice extraction work.
• the ethanol concentration should be 9.9 wt% or less, preferably 6 wt% or less, More preferably, it is 4 wt% or less.
• eggplant fruits may be heated.
• the acetylcholine degrading enzyme can be inactivated, and acetylcholine can be efficiently extracted.
• the eggplant fruit tissue is softened, the cell wall is destroyed, so that the water-soluble component of the eggplant fruit and the crushing of the eggplant fruit can be facilitated.
• the mode of heating is not particularly limited, and for example, heating can be performed in the temperature range of 30 to 100° C. for 2 minutes to 60 minutes.
• the heating temperature is preferably 80 to 100°C.
• Examples of the method of heating eggplant fruit include a method of heating with a microwave oven, a hot plate or a pot, a method of immersing in eggplant hot water, a method of applying steam, and the like.
• the method of dipping in hot water and the method of applying steam to the eggplant are preferable.
• the heating of the eggplant fruit may be performed at any time before addition of water, after addition, during heating with water, before crushing, after crushing, or during crushing. It is preferable to rapidly heat the acetylcholine degrading enzyme for inactivation.
• the method of squeezing the crushed eggplant fruit is not particularly limited as long as it can be divided into a squeezing liquid and a residue.
• it can be squeezed by using a dashi-koshi bag and squeezing with a squeezing machine such as wine, or by squeezing with a fruit juice squeezer.
• a centrifuge, pulper finisher or the like may be used.
• extracting eggplant fruits with water particularly when water is added to dry powder of eggplant fruits to obtain a water extract, a centrifugal separator or a suction filter may be used.
• the obtained squeezed juice or water extract (for example, supernatant of centrifugation, filtrate of a suction filter, etc.) can be dried into a lump or powdery dried product.
• the drying method is not particularly limited, but it is preferable that the water content in the dried product can be dried to 0 to 10 wt %.
• it can be dried by heat drying such as hot air drying, drum drying, freeze drying, spray drying and the like.
• the dried product can be pulverized into a dry powder.
• the pulverization method is not particularly limited, but it is preferable that the pulverization can be performed to about 5 to 100 mesh. For example, it can be ground using a mill.
• the composition produced by the production method of the present invention tends to be low in dietary fiber and high in sugar.
• the ratio of dietary fiber to sugar in the composition of the present invention is, for example, 1:2 to 1:100, preferably 1:5 to 1:40, particularly preferably 1:10 to 1 : 20.
• EN (2-aminoethyl)trimethylammonium pivaloylamide
• AcCh acetylcholine
• BuCh butyrylcholine
• Ch choline
• LaCh lactoylcholine
• PrCh propionylcholine
• EN, AcCh, BuCh, Ch, LaCh, and PrCh are collectively referred to as choline compounds.
• EtOH ethanol.
• Example 1 50 kg of fresh eggplant (Tosataka: 2018) from Kochi prefecture was crushed with a crusher, 50 kg of water and 50 kg of water were added to a pan, and the mixture was heated to 90°C and boiled for 20 minutes to obtain a slurry-like crushed product .. The obtained crushed product was pressed with a fruit juicer (fruit press) to obtain 69 kg of juice and 22 kg of residue. The obtained juice was lyophilized as it was and pulverized to obtain 1.34 kg (water content 5.1%) of lyophilized powder (Example 1).
• Example 1 10 kg of the crushed material of Example 1 was freeze-dried as it was without squeezing and crushed to obtain 600 g of freeze-dried powder (Comparative Example 1).
• Solid phase extraction As a solid phase extraction cartridge, a weakly acidic cation exchange cartridge Inert Sep CBA 100 mg/1 mL (GL Science Co., Ltd.) was used. A solid phase extraction cartridge activated with methanol (1 mL) and pure water (1 mL) was equilibrated with 10 mM phosphate buffer (8 mL), and then the extraction sample (about 600 ⁇ L) prepared in (3) above was added. It was stabilized with 10 mM phosphate buffer (600 ⁇ L), washed with pure water (2.5 mL), and then eluted with hydrochloric acid (500 ⁇ L).
• a choline compound mixed solution was prepared as shown in Table 2, and the addition concentration of each choline compound stock solution was determined according to the analysis result of the choline compound mixed solution-free sample (Table 1-A).
• the choline compound stock solution was diluted with the LC/MS/MS analysis solvent to prepare each concentration. If any choline compound was not detected, only an equal volume of LC/MS/MS analytical solvent without that compound was added.
• LC/MS/MS analysis (1) LC/MS/MS analysis conditions The column used was YMC-Triart PFP (4.6 mm ⁇ 250 mm, 5 ⁇ m, YMC Co., Ltd.). Water containing 0.01% formic acid-33% methanol was used as the analysis solvent, the flow rate was 0.5 mL/min (LC), 0.3 mL/min (MS), the injection volume was 50 ⁇ L, the separation temperature was 40° C., and the analysis time was Is 30 min, ionization mode is ESI+ ⁇ MRM, Capillary Voltage is 3500 V, Cone Voltage is 10 V, Collision Voltage is 10 V, N2 gas flow (desolvation) is 600 L/hr, N2 gas flow (cone) is 50 L/hr, N2 source temp.
• Example 1 The acetylcholine content of Example 1 was 1.73 (mg/g DW), and the acetylcholine content of Comparative Example 1 was 0.62 (mg/g DW).
• Example 1 The freeze-dried powder of Example 1 and the freeze-dried powder of Comparative Example 1 were given in an amount such that the amount of acetylcholine was 10 ⁇ 9 mol/kg body weight so that the amount of acetylcholine was the same.
• systolic blood pressure was measured by the tail cuff method using a non-invasive blood pressure measuring device Softron BP-98A (Softron Co., Ltd., Tokyo). The results are shown in Table 4.
• Group B was ingested 4 capsules of Comparative Example 1 twice a day (morning and evening) for a total of 8 capsules for 4 weeks.
• the freeze-dried powder of Comparative Example 1 contained approximately 8 times the dietary fiber of the freeze-dried powder of Example 1. Further, it was found that the freeze-dried powder of Example 1 contained more sugar.
• Example 2 One week after harvesting, 3 kg of Kochi eggplant Tosataka (produced in 2017), which had been frozen and stored, was thawed, put in a pot as it was, and covered with a lid-type heater for 30 minutes. 1 kg was freeze-dried as it was to obtain Comparative Example 2. After cooling the remaining 2 kg, the heated eggplant was crushed with a juicer mixer for 10 minutes. After adding 2 kg of water and stirring well, they were mixed with a juicer mixer for 10 minutes. The obtained slurry-like crushed product was divided and placed in six 1 L capacity dashi-koshi bags, and a squeezing liquid and a residue were obtained with a 12 L capacity squeezing machine (wine press).
• the amount of juice was 2700 g and Brix 1.9%.
• the residue was 530 g.
• 900 g of squeezed juice was freeze-dried and pulverized with a mill to obtain 28 g of eggplant squeezed powder, which was used as Example 2-1.
• Dextrin (17 g) was added to 900 g of squeezed liquid, dissolved, freeze-dried, and pulverized with a mill to obtain 74 g of eggplant squeezed powder containing 50% dextrin, which was used as Example 2-2.
• Example 3 50 kg of water (produced in 2018) of Tosataka, fresh eggplant produced in Kochi prefecture, was added with 50 kg of water, heated to 90° C. and boiled for 20 minutes. All of the obtained eggplants and broth were crushed with a crusher to obtain a slurry-like crushed product. 1 kg thereof was freeze-dried as it was to obtain Comparative Example 3. The remainder was squeezed with a fruit juicer (fruit press) to obtain 68.5 kg of juice and 23.8 kg of residue. The squeezed liquid was divided into two, and 34 kg of the squeezed liquid was spray-dried as it was with a spray dryer to obtain 675 g of the powder of Example 3-1. 700 g of lactose was added to 34 kg of squeezed juice, dissolved well, and spray-dried with a spray dryer to obtain 1.23 kg of powder, which was used as Example 3-2.
• Example 4 Comparative Example 4 and Example 4 were obtained in the same manner as in Example 1 except that the raw eggplant was changed to a fresh eggplant produced in Kumamoto Prefecture, Higuranasaki (produced in 2018).
• Example 5 The raw eggplant was Kumamoto prefecture fresh eggplant, Higuranasaki (produced in 2018), 20 kg was crushed with a crusher, heated to 90° C. and boiled for 1 hour. 1 kg of the obtained crushed product was freeze-dried as it was to obtain Comparative Example 5. Water was not added to the remaining 19 kg, and the mixture was pressed as it was to obtain 8 kg of juice. Freeze-drying and pulverization gave 250 g of the powder of Example 5.
• Example 6 To 100 g of Comparative Example 1, 10 times the amount of water was added and stirred for 1 hour. The obtained slurry-like solution was centrifuged (3,000 rotations, 30 minutes) to obtain a supernatant. The supernatant was freeze-dried and pulverized to obtain 42 g of the powder of Example 6.
• Example 7 10 kg of fresh eggplant (Tosataka: 2017) from Kochi Prefecture was heated at 95°C for 50 minutes, cooled to room temperature, crushed with a crusher, and 10 kg of water was added to obtain a slurry-like crushed material. .. The obtained crushed product was dried with a drum dryer to obtain 550 g of powder (referred to as Comparative Example 6). To 300 g of this powder was added 20 times the amount of water, the mixture was stirred for 1 hour, and 5000 ml of the filtrate obtained by suction filtration using filter paper was freeze-dried and pulverized to obtain 90 g of Example 7.

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• 2020
  • 2020-02-07 JP JP2020572213A patent/JPWO2020166494A1/ja active Pending
  • 2020-02-07 WO PCT/JP2020/004708 patent/WO2020166494A1/ja active Application Filing
  • 2020-02-07 TW TW109103836A patent/TW202034936A/zh unknown

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