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WO2024080290A1 - Inhibiteur de synthèse de pigment de mélanine - Google Patents

Inhibiteur de synthèse de pigment de mélanine Download PDF

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Publication number
WO2024080290A1
WO2024080290A1 PCT/JP2023/036830 JP2023036830W WO2024080290A1 WO 2024080290 A1 WO2024080290 A1 WO 2024080290A1 JP 2023036830 W JP2023036830 W JP 2023036830W WO 2024080290 A1 WO2024080290 A1 WO 2024080290A1
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Prior art keywords
composition
weight
skin
extract
agent
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PCT/JP2023/036830
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English (en)
Japanese (ja)
Inventor
幸子 藤田
弘之 小島
紀幸 中村
イダマルゴダ アルナシリ
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Ichimaru Pharcos Co Ltd
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Ichimaru Pharcos Co Ltd
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Priority to CN202380062719.5A priority Critical patent/CN119730833A/zh
Priority to JP2024551708A priority patent/JPWO2024080290A1/ja
Publication of WO2024080290A1 publication Critical patent/WO2024080290A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin

Definitions

  • the present invention relates to a melanin pigment production inhibitor containing tranexamic acid, etc., for use on the skin of humans, etc.
  • the epidermis is the skin tissue that exists in the outermost layer of the skin.
  • the epidermis is mainly composed of the stratum corneum, stratum granulosum, stratum spinosum, and stratum basale. Basal cells in the stratum basale divide and migrate to the outer layer. During this migration, the cells undergo enucleation, flattening, and differentiation into the stratum corneum, which eventually peels off. This turnover period is said to be about 45 days. However, in aged skin, the turnover rate slows down and the entire epidermis becomes thinner. As a result, it is known that skin functions such as a decrease in barrier function and a decrease in moisture content occur (Patent Document 1, Patent Document 2).
  • the problem that the present invention aims to solve is to provide a novel composition for use on human skin, etc., to prevent a decline in skin function (for example, by suppressing melanin pigment production).
  • the inventors of the present invention therefore conducted extensive research and developed the present invention.
  • the present invention includes the following items.
  • [Item 1] A melanin pigment production inhibitor comprising the following components (A) to (E): (A) tranexamic acid (B) nicotinamide (C) glutathione (D) a vitamin C derivative (E) sodium pyrosulfite
  • [Item 2] The agent according to [Item 1], further comprising citric acid.
  • [Item 3] The agent according to [Item 1] or [Item 2], further comprising arbutin.
  • [Item 4] A composition for external application to the skin, comprising any one of the agents according to [Item 1] to [Item 3].
  • the present invention provides a novel composition for use on human skin to prevent a decline in skin function.
  • composition of the present invention will be used as an example, but the explanation of the composition of the present invention can be used to explain the agent of the present invention.
  • Tranexamic acid is an abbreviation for trans-4-aminomethylcyclohexane-1-carboxylic acid.
  • Tranexamic acids include, for example, tranexamic acid, tranexamic acid salts, tranexamic acid esters, tranexamic acid amides, and tranexamic acid multimers.
  • salts of tranexamic acid salts include metal salts such as sodium salts, potassium salts, and magnesium salts; and inorganic acid salts such as hydrochlorides, phosphates, and sulfates.
  • esters of tranexamic acid esters include vitamin esters such as vitamin A ester, vitamin E ester, and vitamin C ester; and alkyl esters.
  • amides of tranexamic acid amides include methyl amides.
  • the tranexamic acid may include, for example, a derivative of tranexamic acid.
  • the derivative of tranexamic acid include a dimer of tranexamic acid (trans-4-(trans-4-aminomethylcyclohexanecarbonyl)aminomethylcyclohexanecarboxylic acid hydrochloride), an ester of tranexamic acid and hydroquinone (trans-4-aminomethylcyclohexanecarboxylic acid 4'-hydroxyphenyl ester), an ester of tranexamic acid and gentisic acid (2-(trans-4-aminomethylcyclohexylcarbonyloxy)-5-hydroxybenzoic acid and its salts), and an amide of tranexamic acid (trans-4-aminomethylcyclohexanecarboxylic acid methylamide and its salts, trans-4-acetylaminomethylcyclohexanecarboxylic acid and its salts, trans-4-(
  • the content of tranexamic acid (including derivatives of said tranexamic acid) contained in the composition of the present invention is not particularly limited, but in order to exert the desired effect, the content of said tranexamic acid relative to the total amount of the composition is, for example, preferably 0.001% by weight or more, more preferably 0.01% by weight or more, and even more preferably 0.1% by weight or more. Also, taking into consideration the desired effect, etc.
  • the content of said tranexamic acid relative to the total amount of the composition is, for example, preferably 20% by weight or less, more preferably 10% by weight or less, and even more preferably 7% by weight or less.
  • Nicotinic acid is an amide compound of nicotinic acid (vitamin B3, niacin), and is also called nicotinamide or niacinamide, and is a derivative of nicotinic acid.
  • the nicotinamide is a water-soluble vitamin and a substance that is one of the vitamin B group, and can be extracted from natural products (such as rice bran) or synthesized by known methods. Specifically, those listed in the 15th revised Japanese Pharmacopoeia (revised in 2008) can be used.
  • the content of nicotinamide contained in the composition of the present invention is not particularly limited, but in order to exert the desired effect, the content of nicotinamide is generally, for example, preferably 0.001% by weight or more, more preferably 0.01% by weight or more, and even more preferably 0.1% by weight or more, based on the total amount of the composition. Also, taking into consideration the desired effect, etc.
  • the content of nicotinamide is generally, for example, preferably 20% by weight or less, more preferably 10% by weight or less, and even more preferably 8% by weight or less, based on the total amount of the composition.
  • Glutathione Glutathione is an antioxidant and the most abundant SH compound (thiol compound) in the body. It reacts enzymatically and non-enzymatically with disulfides in proteins and other compounds to maintain their SH status, and is converted into oxidized glutathione through this reaction.
  • the amount of glutathione contained in the composition of the present invention is not particularly limited, but in order to achieve the desired effect, the amount of glutathione contained in the composition is generally, for example, preferably 0.0001% by weight or more, more preferably 0.0005% by weight or more, relative to the total amount of the composition.
  • the amount of glutathione contained in the composition is generally, for example, preferably 20% by weight or less, more preferably 10% by weight or less, relative to the total amount of the composition.
  • vitamin C derivative The concept of vitamin C derivatives encompasses derivatives of L-ascorbic acid and their salts, and is produced by modifying the molecular structure of vitamin C by binding it with other molecules in order to increase its stability.
  • the vitamin C derivatives include water-soluble, fat-soluble, and amphipathic.
  • water-soluble vitamin C derivatives include ascorbic acid 2-glucoside, ascorbic acid 6-glucoside, 3-O-ethyl ascorbic acid, and sodium ascorbyl phosphate.
  • examples of the fat-soluble vitamin C derivatives include ascorbyl tetrahexyldecanoate, ascorbyl palmitate, and ascorbyl stearate.
  • Examples of the amphipathic vitamin C derivatives include trisodium ascorbyl palmitate phosphate, and glyceryl octyl ascorbic acid.
  • the content of the vitamin C derivative contained in the composition of the present invention is not particularly limited, but in order to exert the desired effect, the content of the vitamin C derivative relative to the total amount of the composition is generally, for example, preferably 0.01% by weight or more, more preferably 0.1% by weight or more. Also, taking into consideration the desired effect, etc. (for example, even if more than a certain amount is added, the effect is not substantially increased, and it tends to be difficult to add the derivative to compositions for external use on the skin, etc.), the content of the vitamin C derivative relative to the total amount of the composition is generally, for example, preferably 10% by weight or less, more preferably 5% by weight or less.
  • Sodium pyrosulfite sodium metabisulfite
  • the sodium pyrosulfite can be produced by the dehydration reaction of sodium hydrogensulfite or by adding sulfur dioxide to sodium sulfite.
  • the content of sodium pyrosulfite contained in the composition of the present invention is not particularly limited, but in order to exert the desired effect, the content of sodium pyrosulfite relative to the total amount of the composition is generally, for example, preferably 0.0001% by weight or more, more preferably 0.001% by weight or more, and even more preferably 0.01% by weight or more. Also, taking into consideration the desired effect, etc.
  • the content of sodium pyrosulfite relative to the total amount of the composition is generally, for example, preferably 2% by weight or less, more preferably 1% by weight or less, and even more preferably 0.5% by weight or less.
  • Citric acid is a buffer (pH adjuster).
  • the citric acid may include, for example, sodium citrate, trisodium citrate, etc.
  • the amount of citric acid contained in the composition of the present invention is not particularly limited, but in order to achieve the desired effects, the amount of citric acid contained in the composition is generally, for example, preferably 0.5% by weight or less relative to the total amount of the composition.
  • Arbutin Arbutin is an ingredient approved by the Ministry of Health, Labor and Welfare as a quasi-drug whitening active ingredient in 1989.
  • the arbutin is present in the leaves of, for example, Ericaceae plants such as Arctostaphylos uva-ursi, Vaccinium vitis-idaea, and Vaccinium oxycoccos, and Rosaceae plants such as Pyrus communis.
  • the arbutin may include, for example, ⁇ -arbutin (a hydroquinone derivative in which hydroquinone and glucose are ⁇ -bonded), ⁇ -arbutin, etc.
  • the content of arbutin contained in the composition of the present invention is not particularly limited, but in order to exert the desired effect, the content of arbutin relative to the total amount of the composition is generally, for example, preferably 0.0001% by weight or more, more preferably 0.001% by weight or more, and even more preferably 0.01% by weight or more. Also, taking into consideration the desired effect, etc. (for example, even if more than a certain amount is added, the effect cannot be substantially increased, and it tends to be difficult to add in compositions for external use on the skin), the content of arbutin relative to the total amount of the composition is generally, for example, preferably 2% by weight or less, more preferably 1% by weight or less, and even more preferably 0.5% by weight or less.
  • Skin whitening refers to the prevention and/or improvement of pigmentation, and more specifically, refers to the prevention and/or improvement of pigmentation symptoms caused by increased production, excessive accumulation, and abnormal deposition of melanin pigment, such as age spots, dullness, freckles, sunburn, and darkening due to inflammation or irritation of the skin, as well as pigmentation symptoms caused by diseases that result in pigmentation, such as skin melanosis due to drugs such as steroids.
  • Inhibition of melanin pigmentation refers to the inhibition of the formation of skin melanocytes and the prevention and/or improvement of skin pigmentation phenomena such as spots, freckles, age spots, etc. Such prevention and/or improvement can, for example, improve the overall skin tone, brighten the skin, and improve dark spots.
  • the agent and composition of the present invention may contain, for example, a specific plant extract in order to exert a desired effect.
  • the extraction method used to prepare the plant extract may be, for example, a method of extraction using an appropriate solvent.
  • the plant may be used as is, or may be crushed or dried before use. It is preferable to crush the plant, and more preferable to use a dried plant.
  • the plant while immersed in the extraction solvent, the plant may be stirred or left to stand.
  • the plant extract of the present invention may be made into a high-concentration plant extract by repeating the extraction procedure.
  • the solvent used for the extraction is not particularly limited, and examples thereof include water, lower monohydric alcohols such as methanol, ethanol, propanol, and butanol, polyhydric alcohols such as propylene glycol, dipropylene glycol, butylene glycol, and glycerin, esters such as methyl acetate and ethyl acetate, ketones such as acetone and methyl ethyl ketone, polar solvents such as ethers such as diethyl ether and tetrahydrofuran, halogenated hydrocarbons such as chloroform and carbon tetrachloride, and hydrocarbons such as hexane, heptane, and cyclohexane.
  • lower monohydric alcohols such as methanol, ethanol, propanol, and butanol
  • polyhydric alcohols such as propylene glycol, dipropylene glycol, butylene glycol, and glycerin
  • the solvent used for the extraction may be, for example, a single solvent or a mixed solvent consisting of two or more solvents, and it is particularly preferable to use a polar solvent.
  • the extraction procedure is not particularly limited, and examples thereof include a procedure in which the plant used for the extraction is immersed in the solvent at 20 to 40°C for 1 hour to 7 days and then filtered.
  • the obtained extract may be used as it is as a plant extract, or may be used after dilution, concentration, freeze-drying, purification, etc.
  • the total content of the plant extract in the composition of the present invention is not particularly limited, but in order to achieve the desired effect, it is preferably 0.000001 to 10% by mass, more preferably 0.00001 to 5% by mass, and even more preferably 0.0001 to 3% by mass, in terms of the mass of the dry matter, based on the total mass of the composition.
  • Specific plant extracts include, for example, Peony root extract, Scutellaria root extract, Caraway extract, Thymus vulgaris extract, and Celastrus arbutus extract.
  • the above-mentioned Paeonia suffruticosa extract is obtained, for example, by subjecting the root bark of the peony (Paeonia suffruticosa Andrews) of the family Paeoniaceae to an extraction treatment using an extraction solvent.
  • the above-mentioned Paeonia suffruticosa extract was prepared by adding 1,3-butylene glycol and water to the residue obtained by removing the solvent from the extract of the root bark of the peony in ethanol, and dissolving it there; Paeonia suffruticosa Liquid B, Ichimaru Pharcos Co., Ltd.
  • the Scutellaria root extract is obtained, for example, by subjecting the root, rhizome and/or root bark of Scutellaria baicalensis Georgia, a plant of the Scutellaria genus in the Lamiaceae family, to an extraction treatment using an extraction solvent.
  • Scutellaria root extract an ethanol extract of the roots of Scutellaria baicalensis Georgia (Labiatae), with the periderm removed, dissolved in 1,3-butylene glycol solution, Scutellaria root liquid B, Ichimaru Pharcos Co., Ltd.
  • the above-mentioned Geranium robertianum extract is obtained, for example, by subjecting Geranium robertianum L. (Geraniaceae) of the Geraniaceae family to an extraction process.
  • Geranium robertianum extract obtained by extracting the whole plant of Geranium robertianum L. (Geraniaceae) with a 1,3-butylene glycol solution, Princess Care, Ichimaru Pharcos Co., Ltd. was used as the above-mentioned Geranium robertianum extract.
  • thymus extract is obtained by subjecting, for example, Thymus serpyllum, which is native to Europe and is known as wild thyme or creeping thyme, to an extraction process.
  • Thymus extract was obtained by concentrating an extract obtained by extracting the above-ground parts of Thymus serpyllum L. (Labiatae) with an ethanol solution and dissolving it by adding a 1,3-butylene glycol solution, Cinderella Care, Ichimaru Pharcos Co., Ltd.
  • Zingiberaceae extract is obtained, for example, by subjecting the seeds of Alpinia katsumadai, a traditional Chinese plant, to an extraction process.
  • Zingiberaceae extract an extract obtained by extracting the seeds of Alpinia katsumadai Hayata (Zingiberaceae) with an ethanol solution, concentrating the extract, and dissolving it by adding a 1,3-butylene glycol solution, Alpinia White, Ichimaru Pharcos Co., Ltd. was used as the above-mentioned Zingiberaceae extract.
  • composition of the present invention may be in the form of ampoules, capsules, powders, granules, liquids, gels, foams, emulsions, sheets, mists, sprays, etc., and may be in the form of 1) medicines, 2) quasi-drugs, 3) topical or whole body external skin preparations (for example, basic cosmetics such as lotions, milky lotions, creams, ointments, lotions, oils, and packs, face washes and skin cleansers such as solid soaps, liquid soaps, and hand washes, massage preparations, cleansing preparations, hair removal preparations, depilatories, shaving treatments, aftershave lotions, preshave lotions, shaving creams, foundations, lipsticks, blushers, eye shadows, and eyeshadows).
  • basic cosmetics such as lotions, milky lotions, creams, ointments, lotions, oils, and packs
  • face washes and skin cleansers such as solid soaps, liquid soaps, and hand washes
  • makeup cosmetics such as eyeliner and mascara, perfumes, nail beautifying agents, nail beautifying enamel, nail beautifying enamel remover, poultices, plasters, tapes, sheets, patches, aerosols, etc.); 4) medicinal and/or cosmetic preparations to be applied to the scalp and hair (for example, shampoos, rinses, hair treatments, pre-hair treatments, permanent solutions, hair dyes, hair styling products, hair tonics, hair growth and care products, poultices, plasters, tapes, sheets, aerosols, etc.); 5) bath products to be added to the bath; 6) other products such as underarm odor prevention agents, deodorants, antiperspirants, sanitary products, sanitary cotton, wet tissues, etc.
  • medicinal and/or cosmetic preparations to be applied to the scalp and hair for example, shampoos, rinses, hair treatments, pre-hair treatments, permanent solutions, hair dyes, hair styling products, hair tonics, hair growth and care products, poultices, plasters, tapes, sheets, aerosol
  • compositions may contain, as necessary, appropriate amounts of ingredients typically used in cosmetics, such as oily ingredients, lower alcohols, polyhydric alcohols, aqueous ingredients such as moisturizers, UV absorbers, antioxidants, cosmetic ingredients, preservatives, oil-soluble resins, dyes, cooling agents, pigments, fragrances, etc., within the scope of the effects of the present invention.
  • ingredients typically used in cosmetics such as oily ingredients, lower alcohols, polyhydric alcohols, aqueous ingredients such as moisturizers, UV absorbers, antioxidants, cosmetic ingredients, preservatives, oil-soluble resins, dyes, cooling agents, pigments, fragrances, etc.
  • the melanin pigment production inhibitor contained in the composition of the present invention is, for example, in order to exert a desired effect (such as a whitening effect), preferably 0.25 (v/v)% or more, more preferably 0.5 (v/v)% or more, more preferably 0.75 (v/v)% or more, more preferably 1 (v/v)% or more, and even more preferably 2 (v/v)% or more.
  • the melanin pigment production inhibitor contained in the composition of the present invention is, for example, in consideration of the desired toxicity, etc., preferably 50 (v/v)% or less, more preferably 25 (v/v)% or less, and even more preferably 10 (v/v)% or less.
  • the present invention will be described in more detail below with reference to examples, but the present invention is in no way limited to these examples.
  • the unit % of the numerical values showing the amount of each component added means % by mass.
  • B16 mouse melanoma cells (melanoma cells): B16 melanoma 4A5, RIKEN CELL BANK Preculture medium for the cells: MEM medium containing 5% fetal bovine serum; MEM medium: E-MEM (051-07615), Fujifilm Wako Pure Chemical Industries; Fetal bovine serum: Thermofisher Scientific Main culture medium: MEM medium containing 0.036% defolin
  • Nicotinamide Product code 000-54225, CAS RNTM98-92-0, Kishida Chemical Co., Ltd.
  • Tranexamic acid Japanese Pharmacopoeia tranexamic acid
  • Glutathione L-glutathione, Kohjin Life Sciences Co., Ltd.
  • Vitamin C derivative Pacificos VAP, Ichimaru Pharcos Co., Ltd.
  • Sodium pyrosulfite Junsei Chemical Co., Ltd.
  • Abrutin ⁇ -arbutin
  • Product ID A6804, LKT Laboratories INC.
  • ⁇ Moutan pea extract Moutan pea Liquid B, Ichimaru Pharcos Co., Ltd.
  • ⁇ Scutellaria root extract Scutellaria root Liquid B, Ichimaru Pharcos Co., Ltd.
  • ⁇ Geranium extract Princess Care, Ichimaru Pharcos Co., Ltd.
  • Thymus vulgaris extract Cinderella Care, Ichimaru Pharcos Co., Ltd.
  • ⁇ Soumony tree extract Alpinia White, Ichimaru Pharcos Co., Ltd.
  • Example 1 Melanin production inhibition test
  • a sample By adding a sample to a specific cell (the above-mentioned melanoma cell), it was confirmed whether there was a change in melanin production in the specific cell.
  • B16 mouse melanoma cell was used as the cell to which the sample was added.
  • Pre-culture step of melanoma cells The above-mentioned melanoma cells were cultured in the above-mentioned pre-culture medium (MEM medium containing 5% fetal bovine serum) under conditions of 5% CO2 and 37°C for 24 hours.
  • MEM medium containing 5% fetal bovine serum
  • melanoma cells were seeded in each well (wells containing the main culture medium, 24-well plate) at 8.5 ⁇ 10 4 cells/well. After the seeding, the cells were cultured for 24 hours under conditions of 5% CO 2 and 37° C.
  • each group was divided into a cultured sample for use in the following measurement 1 and a cultured sample for use in the following measurement 2.
  • Measurement 1 Melanin amount measurement
  • the cultured sample for use in this measurement 1 was treated with trypsin to recover cells.
  • the recovered cells were dissolved in a solution (containing 1N NaOH and 10% DMSO).
  • the absorbance of the dissolved solution (control, positive control, Comparative Examples 1 to 5, and Examples 1 to 3) was measured at 420 nm.
  • the measured value was taken as the amount of melanin.
  • the example Compared to the comparative example, the example had the effect of inhibiting melanin pigment production and was also non-toxic.
  • a melanin pigment production inhibitor or composition comprising the following components (A) to (E): (A) Tranexamic acid (B) Nicotinamide (C) Glutathione (D) Vitamin C derivatives (E) Sodium pyrosulfite (Appendix 2)
  • Appendix 15 The agent or composition described in Appendix 13 or 14, wherein the plant extract is a plant extract selected from the group consisting of Peony root extract, Scutellaria root extract, Geranium globulus extract, Thymus vulgaris extract, and Celastrus arvensis extract.
  • Appendix 16 A method for inhibiting melanin pigment production, comprising using an agent or composition according to any one of claims 1 to 15.
  • Appendix 17 17.
  • the method of claim 16 wherein the agent or composition is contacted with the skin of a subject.
  • Appendix 18 18.
  • the method of claim 17, wherein the subject is a human or a non-human animal.
  • Appendix 19 Use of an agent or composition according to any one of claims 1 to 15 for inhibiting the production of melanin pigment.
  • the composition can be used as a composition for preventing the deterioration of skin function for use on the skin of humans, etc.

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Abstract

La présente invention concerne une nouvelle composition ou similaire destinée à être utilisée sur la peau d'un être humain ou similaire et pour empêcher une détérioration des fonctions de la peau.　Cet inhibiteur de synthèse de pigment de mélanine comprend (a) de l'acide tranexamique, (b) un amide d'acide nicotinique, (c) du glutathion, (d) un dérivé de vitamine c, et (e) du pyrosulfite de sodium.
PCT/JP2023/036830 2022-10-12 2023-10-11 Inhibiteur de synthèse de pigment de mélanine Ceased WO2024080290A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN202380062719.5A CN119730833A (zh) 2022-10-12 2023-10-11 黑色素生成抑制剂
JP2024551708A JPWO2024080290A1 (fr) 2022-10-12 2023-10-11

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