WO2023195718A1 - Composition permettant de supprimer la sucrosité et procédé de suppression de sucrosité d'aliments - Google Patents

Composition permettant de supprimer la sucrosité et procédé de suppression de sucrosité d'aliments Download PDF

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Publication number
WO2023195718A1
WO2023195718A1 PCT/KR2023/004469 KR2023004469W WO2023195718A1 WO 2023195718 A1 WO2023195718 A1 WO 2023195718A1 KR 2023004469 W KR2023004469 W KR 2023004469W WO 2023195718 A1 WO2023195718 A1 WO 2023195718A1
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Prior art keywords
acid
sweetness
composition
suppressing
food
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PCT/KR2023/004469
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English (en)
Korean (ko)
Inventor
박가연
최평강
황혜영
최명환
Original Assignee
서울대학교산학협력단
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Priority claimed from KR1020230043527A external-priority patent/KR20230143117A/ko
Publication of WO2023195718A1 publication Critical patent/WO2023195718A1/fr

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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, 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
    • A23L27/00Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
    • A23L27/30Artificial sweetening agents
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, 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
    • A23L29/00Foods or foodstuffs containing additives; Preparation or treatment thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Definitions

  • the present invention relates to a composition for suppressing sweetness and a method for suppressing sweetness of food.
  • Taste in a narrow sense, refers to the sensation felt when a substance is placed on the tongue. Thousands of small taste buds covering the surface of the tongue contain various types of taste receptors. Taste receptors include sweet, salty, sour, bitter, Detect the five basic tastes of umami. This connects to taste-related nerve cells and processes information about taste in the brain.
  • the sweet taste receptor has the form and function of GPCR (G-protein coupled receptor), a representative type of cell membrane receptor, and the GPCRs of TAS1R2 and TAS1R3 each form a heterodimer.
  • GPCR G-protein coupled receptor
  • TAS1R2 and TAS1R3 each form a heterodimer.
  • the receptor and ligand bind, the activity of the G-protein present inside the cell is induced, resulting in signal transduction.
  • PIP2 phosphatidylinositol 4,5-bisphosphate
  • DAG Diacylglycerol
  • IP3 inositol3-phosphate
  • IP3 stimulates calcium channels in the ER (Endoplasmic reticulum) and promotes calcium secretion within the ER. Since taste cells are activated according to this pathway, receptor activation can be confirmed by checking changes in the amount of calcium ions within the cells.
  • the purpose of the present invention is to provide a better sweetness suppressing composition by improving the sweet aftertaste characteristic of lactisol, a conventional sweetness suppressing agent.
  • the purpose of the present invention is to provide a food containing the composition for suppressing sweetness.
  • the purpose of the present invention is to provide an excellent method for suppressing sweetness.
  • composition for suppressing sweetness in 1 above wherein the salt is a sodium salt.
  • composition for suppressing sweetness according to 1 above further comprising a chelating agent selected from the group consisting of edetic acid, citric acid, metaphosphoric acid, pyrophosphoric acid, polyphosphoric acid, malic acid, tartaric acid, phytic acid, and salts thereof.
  • a chelating agent selected from the group consisting of edetic acid, citric acid, metaphosphoric acid, pyrophosphoric acid, polyphosphoric acid, malic acid, tartaric acid, phytic acid, and salts thereof.
  • composition for suppressing sweetness according to 1 above, wherein the concentration of diquafosol or its salt is 20mM to 60mM.
  • a method of suppressing the sweetness of food comprising the step of treating food with the composition of any one of items 1 to 4 above.
  • composition and food of the present invention have an excellent effect in suppressing the sweetness of food. This can improve the sensory characteristics of foods by enriching other flavors other than sweetness, and can be used to maintain sweetness at an appropriate level.
  • Figure 1 relates to the response of type I taste cells to diquafosol. Specifically, the picture on the left shows that the calcium signal of type I taste cells in the taste buds of living mice was increased by diquafosol. The graph on the right confirms the reactivity of taste cells according to the concentration of diquafosol, and confirms that the EC50 value is about 117 nM.
  • Figure 2 confirms that sweet taste nerve reactivity to 30 mM acesulfame K, an artificial sweetener, was decreased in the tongue previously exposed to diquafosol.
  • Figure 3 relates to a sensory test reporting the intensity of perceived sweetness for acesulfame K after exposure to 40 mM diquafosol. As a result, it was confirmed that the evaluation of sweetness was reduced by 10-20% due to diquafosol.
  • Figure 4 is a schematic diagram of the mechanism of action of diquafosol to suppress sweetness.
  • the present invention relates to a composition for suppressing sweetness containing diquafosol or a salt thereof.
  • Diquafosol may be a compound represented by the following formula (1).
  • the salt of diquafosol is not particularly limited as long as it is a salt acceptable as a food composition, and includes metal salts of lithium, sodium, potassium, calcium, magnesium, zinc, etc.; Salts with inorganic acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, sulfuric acid, and phosphoric acid; Acetic acid, fumaric acid, maleic acid, succinic acid, citric acid, tartaric acid, adipic acid, gluconic acid, glucoheptonic acid, glucuronic acid, terephthalic acid, methanesulfonic acid, lactic acid, hippuric acid, 1,2-ethanedisulfonic acid.
  • inorganic acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, sulfuric acid, and phosphoric acid
  • Acetic acid fumaric acid, maleic acid, succinic acid, citric acid, tartaric acid, adipic acid,
  • diquafosol or its salt also includes hydrates and organic solvates of diquafosol (free form) or its salt.
  • crystal polymorph group refers to the individual crystal forms at each stage and the entire process when the crystal form changes depending on the conditions and states of production, crystallization, preservation, etc. of these crystals.
  • Diquafosol or a salt thereof of the present invention is the sodium salt of Diquafosol, and the tetrasodium salt of Diquafosol represented by the following formula (2) is particularly preferred.
  • Diquafosol or its salt can be produced by the method disclosed in Japanese Patent Publication No. 2001-510484, etc.
  • composition of the present invention may contain active ingredients other than diquafosol or its salt, or may contain diquafosol or its salt as the only active ingredient.
  • the concentration of diquafosol or its salt in the present composition is not particularly limited, but for example, it is preferably 0.0001 to 10% (w/v), more preferably 0.001 to 5% (w/v), and 0.01 to 10% (w/v). It is more preferably 5% (w/v), more preferably 0.1 to 5% (w/v), even more preferably 1 to 5% (w/v), and 3% (w/v). v) is particularly preferable.
  • the concentration of diquafosol or its salt in the present composition is not particularly limited, but may be, for example, 20mM to 60mM, 22mM to 58mM, 24mM to 56mM, 26mM to 54mM, 28mM to 52mM. It may be 30mM to 50mM, 32mM to 48mM, 34mM to 46mM, 36mM to 44mM, 37mM to 43mM, 38mM to 42mM, 39mM to 41mM. Within the above range, safety to the human body can be ensured and a good sweetness suppression effect can be shown.
  • Sweetness refers to a sweet taste
  • sweetness suppression refers to a use that completely eliminates or reduces sweetness
  • the composition of the present invention may contain additional ingredients that are commonly used in food compositions to improve odor, taste, vision, etc.
  • additional ingredients may include vitamins A, C, D, E, B1, B2, B6, B12, niacin, biotin, folate, pantothenic acid, etc.
  • minerals such as zinc (Zn), iron (Fe), calcium (Ca), chromium (Cr), magnesium (Mg), manganese (Mn), copper (Cu), and chromium (Cr).
  • it may contain amino acids such as lysine, tryptophan, cysteine, and valine.
  • the composition contains chelating agents (edetic acid, citric acid, metaphosphoric acid, pyrophosphoric acid, polyphosphoric acid, malic acid, tartaric acid, phytic acid and their salts), preservatives (potassium sorbate, sodium benzoate, salicylic acid, sodium dehydroacetate, etc.), Disinfectants (bleaching powder, high bleaching powder, sodium hypochlorite, etc.), antioxidants (butylhydroxyanisole (BHA), butylhydroxytoluene (BHT), etc.), colorants (tar color, etc.), coloring agents (sodium nitrite, nitrous acid, etc.) sodium, etc.), bleach (sodium sulfite), seasoning (MSG, etc.), flavoring (vanillin, lactones, etc.), leavening agent (alum, D-potassium hydrogen tartrate, etc.), strengthening agent, emulsifier, thickener (grease), coating agent, gum base It may further include additive,
  • composition of the present invention can be formulated into powders, granules, tablets, pills, sugar-coated tablets, capsules, solutions, gels, syrups, slurries, suspensions, etc. using methods known in the art.
  • oral preparations can be prepared by combining the active ingredient with solid excipients, grinding them, adding suitable auxiliaries, and processing them into a granule mixture to obtain tablets or dragees.
  • excipients examples include sugars including lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol and maltitol, starches including corn starch, wheat starch, rice starch and potato starch, cellulose, Fillers such as celluloses including methyl cellulose, sodium carboxymethylcellulose, and hydroxypropylmethyl-cellulose, gelatin, polyvinylpyrrolidone, etc. may be included. Additionally, in some cases, cross-linked polyvinylpyrrolidone, agar, alginic acid, or sodium alginate may be added as a disintegrant.
  • composition of the present invention commercial products can be used without limitation, for example, Santen Pharmaceutical's Diquas ophthalmic solution 3% and Diquas-S ophthalmic solution 3% products can be used.
  • the present invention relates to a food containing a composition for suppressing sweetness containing diquafosol or a salt thereof.
  • diquafosol its salt, sweetness suppressing use and composition is as above.
  • Food refers to meat, sausages, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum, dairy products including ice cream, various soups, beverages, tea, drinks, alcoholic beverages, vitamin complexes, and health functional foods. and health foods, etc., and include all foods in the conventional sense, and are not limited thereto, as long as the diquafosol can be included.
  • the food composition may further include a physiologically acceptable carrier.
  • the type of carrier is not particularly limited and any carrier commonly used in the art can be used.
  • the present invention relates to a method for suppressing the sweetness of food, comprising the step of treating the food with the composition for suppressing sweetness.
  • Treating the composition to food may include including the composition in each step of the food manufacturing process, such as pre-processing of raw materials, molding, heating, and cooling, or applying it to finished food. It is not limited to this.
  • Methods of suppressing the sweetness of food include, but are not limited to, methods of reducing the sweetness of the food itself and methods of making the person who consumes the food feel less sweet, and where the sweetness felt when a person consumes the food is reduced. , This is called the sweetness suppression method.
  • a genetically engineered mouse (GAD2-GCaMP6) in which a calcium marker (GCaMP6) was introduced into type I cells was used.
  • GCaMP6 a calcium marker
  • the tongue of a genetically modified mouse was administered Diquas ophthalmic solution from Santen Pharmaceuticals, which contains 40mM Diquafosol dissolved in physiological saline, for 10 to 20 seconds, activation of calcium signals in taste cells was confirmed. .
  • the EC50 value was confirmed to be 117 nM.
  • PIRT-GCaMP genetically modified mice expressing a calcium marker (GCaMP6) in the gustatory nerve were used.
  • the tongues of living mice were divided into a group exposed to 1mM acesulfame K for 10 seconds and a group exposed to 1mM diquafosol for 10 seconds, and then each group was exposed to 30mM acesulfame K.
  • the sweet taste nerve response was suppressed by about 20% in the group exposed to diquafosol.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Polymers & Plastics (AREA)
  • Food Science & Technology (AREA)
  • Nutrition Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Veterinary Medicine (AREA)
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Abstract

La présente invention se rapporte à une composition permettant de supprimer la sucrosité et un procédé de suppression de la sucrosité d'aliments, la composition contenant du diquafosol et présentant ainsi une capacité considérable de suppression de la sucrosité.
PCT/KR2023/004469 2022-04-04 2023-04-03 Composition permettant de supprimer la sucrosité et procédé de suppression de sucrosité d'aliments WO2023195718A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR20220041602 2022-04-04
KR10-2022-0041602 2022-04-04
KR1020230043527A KR20230143117A (ko) 2022-04-04 2023-04-03 감미 억제용 조성물 및 식품의 감미 억제 방법
KR10-2023-0043527 2023-04-03

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WO2023195718A1 true WO2023195718A1 (fr) 2023-10-12

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR850006494A (ko) * 1984-03-29 1985-10-14 로버트 피ㆍ멀그류 식품의 감미를 억제시키는 방법
KR20140136980A (ko) * 2012-03-26 2014-12-01 산텐 세이야꾸 가부시키가이샤 디쿠아포솔 함유 점안액
KR20170020859A (ko) * 2014-06-12 2017-02-24 포 엘엘씨 단맛 수용체 안타고니스트 조성물
CN112691080A (zh) * 2021-03-01 2021-04-23 南京恒道医药科技有限公司 一种地夸磷索钠组合物、制剂及其制备方法
KR20210158354A (ko) * 2020-06-23 2021-12-30 주식회사태준제약 디쿠아포솔을 포함하는 점안 조성물

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR850006494A (ko) * 1984-03-29 1985-10-14 로버트 피ㆍ멀그류 식품의 감미를 억제시키는 방법
KR20140136980A (ko) * 2012-03-26 2014-12-01 산텐 세이야꾸 가부시키가이샤 디쿠아포솔 함유 점안액
KR20170020859A (ko) * 2014-06-12 2017-02-24 포 엘엘씨 단맛 수용체 안타고니스트 조성물
KR20210158354A (ko) * 2020-06-23 2021-12-30 주식회사태준제약 디쿠아포솔을 포함하는 점안 조성물
CN112691080A (zh) * 2021-03-01 2021-04-23 南京恒道医药科技有限公司 一种地夸磷索钠组合物、制剂及其制备方法

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