Classifications

• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/66—Phosphorus compounds
  • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• compositions for preventing or treating Alzheimer's disease relate to compositions for preventing or treating Alzheimer's disease.
• Amyloid ⁇ peptide is widely known to be the most important factor in the development of Alzheimer's disease (AD).
• a ⁇ is known to be generated by cleavage from the amyloid precursor protein (APP) by ⁇ -secretase (BACE1) and ⁇ -secretase.
• APP amyloid precursor protein
• BACE1 ⁇ -secretase
• ⁇ -secretase BACE1
• BACE1 ⁇ -secretase
• glycerophospholipids with a specific structure can efficiently inhibit BACE1, and have made further improvements.
• R 1 represents an alkyl or alkenyl group having 14 to 20 carbon atoms, which may be substituted with an OH group
• R2 represents a group in which R2 -COOH represents a fatty acid having 18 carbon atoms
• R3 represents -CH2CH2N + ( CH3 ) 3 .
• R 1 represents an alkyl group or alkenyl group having 14 to 20 carbon atoms which may be substituted with an OH group
• R 2 represents a group in which R 2 -COOH represents a fatty acid having 18 carbon atoms
• R3 represents -CH2CH2N + ( CH3 ) 3
• R 1 represents a linear alkyl group or linear alkenyl group having 16 or 18 carbon atoms, which may be substituted with one OH group
• Item 3 The composition according to item 1 or 2.
• Item 4. Item 4.
• a new means for efficiently inhibiting BACE1 is provided. This is expected to lead to the efficient prevention and treatment of Alzheimer's disease.
• the left side shows the ratio of expression levels of C83 and C99 produced from APP (C83/C99) when SH-SY5Y cells were treated with PC-PLS-18 or PC-DPL-18.
• the right side shows the results of Western blotting to examine the expression levels of ⁇ -secretase (ADAM9, ADAM10, TACE) when the same treatment was performed.
• ADAM9, ADAM10, TACE ⁇ -secretase
• the mechanism by which A ⁇ is produced from APP is outlined below. 1 shows the results of examining the expression level of BACE1 when SH-SY5Y cells were treated with PC-PLS-18 or PC-DPL-18.
• 1 shows the results of examining the expression level of BACE1 when SH-SY5Y cells were treated with PE-PLS-18 or PE-DPL-18.
• 1 shows the results of examining the expression levels of CLU and Tau proteins when SH-SY5Y cells were treated with PC-PLS-18.
• the present disclosure preferably includes compositions for inhibiting BACE1 that contain glycerophospholipids having a specific structure, and further includes compositions for preventing or treating Alzheimer's disease, but is not limited thereto, and the present disclosure includes everything disclosed in the present specification that can be recognized by a person skilled in the art.
• a composition containing a glycerophospholipid having a specific structure included in the present disclosure may be referred to as a composition of the present disclosure.
• the composition of the present disclosure is useful as a composition for inhibiting BACE1, and thus as a composition for preventing or treating Alzheimer's disease.
• a glycerophospholipid having a specific structure contained in a composition of the present disclosure may be referred to as a glycerophospholipid of the present disclosure.
• the glycerophospholipid of the present disclosure has the formula (1):
• R 1 represents an alkyl group or alkenyl group having 14 to 20 carbon atoms (14, 15, 16, 17, 18, 19, or 20), which may be substituted with an OH group.
• the alkyl group or alkenyl group may be linear or branched, and is preferably linear.
• the carbon-carbon double bond is preferably present between the 6th and 7th carbons, or between the 8th and 9th carbons, counting from the carbon atom to which R 1 is bonded (excluding the carbon atom to which R 1 is bonded).
• the formulation form is also not particularly limited, and the active ingredient and other ingredients can be mixed in a conventional manner to prepare formulations such as tablets, coated tablets, powders, granules, fine granules, capsules, pills, liquids, suspensions, emulsions, jellies, chewable tablets, and soft tablets.
• the glycerophospholipid of the present disclosure may be appropriately blended with a base, carrier, additive, or other ingredient or material that can be used as a food or beverage that is acceptable from the viewpoint of food hygiene.
• food compositions that contain the glycerophospholipid of the present disclosure include processed foods, beverages, health foods (nutritional functional foods, foods for specified health uses, etc.), supplements, foods for the sick (hospital foods, foods for sick people, or nursing care foods, etc.).
• processed meat foods such as burgers, meatballs, wieners, minced chicken, and chicken skin chips, and health foods (nutritional functional foods, foods for specified health uses, etc.), supplements, foods for the sick, etc. that contain processed meat foods are preferred.
• the plasmalogen may be, for example, powdered and contained in various foods and beverages such as beverages (juices, etc.), confectioneries (e.g. gum, chocolate, candy, biscuits, cookies, rice crackers, rice crackers, puddings, almond tofu, etc.), breads, soups (including powdered soups, etc.), and processed foods.
• beverages Juices, etc.
• confectioneries e.g. gum, chocolate, candy, biscuits, cookies, rice crackers, rice crackers, puddings, almond tofu, etc.
• breads e.g. gum, chocolate, candy, biscuits, cookies, rice crackers, rice crackers, puddings, almond tofu, etc.
• soups including powdered soups, etc.
• the food and drink of the present invention As a health food (nutritional functional food, food for specified health uses, etc.) or supplement, it is preferable to prepare it in the form of, for example, granules, capsules, tablets (including chewable tablets, etc.), beverages (drinkables), etc., so that it can be easily taken continuously.
• granules, capsules, tablets (including chewable tablets, etc.), beverages (drinkables), etc. so that it can be easily taken continuously.
• capsule, tablet, and tablet forms are preferable from the standpoint of ease of intake, but are not limited to these.
• DMEM/Ham's F-12 Dulbecco's modified Eagle's medium/Ham's F-12 containing 10% fetal bovine serum (FBS), 100 ⁇ g/mL streptomycin, and 100 IU/mL penicillin under conditions of 95% air, 5% CO2 , and 37°C.
• PC-PLS-18 and PE-PLS-18 are represented by the formula (1):
• R 1 to R 3 each represent a group as described below.
• PC-DPL-18 and PE-DPL-18 are represented by the formula (2):
• R 1 to R 3 each represent a group as described below.
• the cells were treated with choline-type plasmalogen with oleic acid (18:1) bound to the sn-2 position (PC-PLS-18) and phosphatidylcholine-type diacylphospholipid with oleic acid (18:1) bound to the sn-2 position (PC-DPL-18), ethanolamine-type plasmalogen with oleic acid (18:1) bound to the sn-2 position (PE-PLS-18) and ethanolamine-type diacylphospholipid with oleic acid (18:1) bound to the sn-2 position (PE-DPL-18) at 1 ⁇ g/mL each, and incubated.

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• 2025
  • 2025-01-13 TW TW114101315A patent/TW202539627A/zh unknown
  • 2025-01-14 JP JP2025544453A patent/JP7765027B1/ja active Active
  • 2025-01-14 WO PCT/JP2025/000770 patent/WO2025154692A1/ja active Pending

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