Topical skin preparations
A topical skin preparation using Zantedeschia extract from the Araceae family addresses the lack of effective, naturally derived ingredients by enhancing skin barrier function and improving skin texture, offering biotic safety and stability.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- KYOEI KAGAKU KOGYO KK
- Filing Date
- 2022-01-11
- Publication Date
- 2026-04-20
AI Technical Summary
Conventional skin care products lack effective, naturally derived ingredients that can inhibit the deterioration of the skin barrier function and improve rough skin while ensuring biotic safety.
A topical skin preparation containing an extract from the genus Zantedeschia of the Araceae family, preferably using flowers, spathes, or stems, extracted with hydrophilic solvents like water or polyhydric alcohols, which is formulated into cosmetics or quasi-drugs to enhance skin barrier function and improve skin texture.
The Zantedeschia extract effectively suppresses the decline in skin barrier function and improves rough skin by enhancing moisture content and reducing water evaporation, while being safe and stable for topical application.
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Abstract
Description
Technical Field
[0001] The present invention relates to a compounding component of an external preparation for skin, which has an extract of a plant as an active ingredient and excellent skin physiological activity and biotic safety.
Background Art
[0002] Conventionally, as causes of deterioration of the skin barrier function and rough skin, external factors such as damage to cells and tissues by active oxygen induced by chemical substances (nitrogen compounds, sulfur compounds, etc.) contained in sunlight (ultraviolet rays), exhaust gas, or inflammation have been known.
[0003] Conventionally, various moisturizing agents (natural moisturizing factors [NHF], glycerin, polyhydric alcohols, sodium lactate, etc.), antioxidants (vitamin E, astaxanthin, polyphenols, etc.) for preventing and improving rough skin have been proposed, but components that are derived from natural products, have high safety, and exhibit sufficient effects for preventing and improving rough skin have not been known.
Disclosure of the Invention
Problems to be Solved by the Invention
[0004] In view of the problems of such conventional technologies, the present inventors have intensively studied to find a new active ingredient derived from a natural product from the viewpoint of skin safety. As a result, it has been found that an extract of a plant of the genus Zantedeschia of the family Araceae has excellent preventive and improving effects.
[0005] Conventionally, although it has been disclosed in, for example, Patent Documents 1 and 2 that an extract of a plant of the genus Zantedeschia of the family Araceae has skin physiological activity, it has not been known that an extract of a plant of the genus Zantedeschia has both an inhibitory effect on the deterioration of the skin barrier function and preventive and improving effects on rough skin.
Patent Document 1
Patent Document 2
[0006] The present invention is a topical skin preparation containing a plant extract from the genus Zantedeschia of the family Araceae. [Effects of the Invention]
[0007] This invention provides a topical skin preparation that uses a plant extract from the genus Zantedeschia of the Araceae family as an active ingredient, exhibiting effects that suppress the decline in the skin's barrier function and prevent and improve rough skin. [Brief explanation of the drawing]
[0008] [Figure 1] Figure 1 shows the effect of the extract according to the present invention on improving the moisture content of the stratum corneum. [Figure 2] Figure 2 shows the effect of the extract according to the present invention on inhibiting water evaporation from the skin. [Modes for carrying out the invention]
[0009] Examples of plants belonging to the genus Zantedeschia of the Araceae family used in this invention include Zantedeschia aethiopica (also known as calla lily), Zantedeschia albomaculata, Zantedeschia elliottiana, Zantedeschia macrocarpa, and Zantedeschia rehmannii.
[0010] In this invention, any of the following parts of the Zantedeschia plant can be used for extraction: flowers, spathes, leaves, seeds, stems, and roots. However, the use of flowers, spathes, and stems is preferred.
[0011] To prepare the extract, first, the usable parts of each plant are washed with water if necessary to remove foreign matter, then either left as is or dried, and finely chopped or pulverized as needed, before being brought into contact with the extraction solvent for extraction. Extraction can be carried out by conventional methods such as immersion, but supercritical fluid extraction can also be used in addition to immersion.
[0012] Examples of extraction solvents include water; lower alcohols such as methanol, ethanol, and propanol; polyhydric alcohols such as ethylene glycol, propylene glycol, 1,3-butylene glycol, and glycerin; esters such as ethyl acetate, butyl acetate, and methyl propionate; ketones such as acetone and methyl ethyl ketone; ethers such as ethyl ether and isopropyl ether; and hydrocarbon solvents such as n-hexane, toluene, and chloroform. These can be used individually or in combination of two or more.
[0013] Among these extraction solvents, hydrophilic solvents such as water, lower alcohols, or polyhydric alcohols are preferred in the present invention, from the viewpoint of the effectiveness of the resulting extract mixture, as well as its low skin irritancy, and its broad applicability to topical skin preparations (cosmetics, quasi-drugs, topical pharmaceuticals, etc.). Preferred examples of using these hydrophilic solvents include, for example, the use of water, lower alcohols (especially ethanol), or polyhydric alcohols (especially 1,3-butylene glycol) alone, or a mixed solvent of water and lower alcohols (especially ethanol), or a mixed solvent of water and polyhydric alcohols (especially 1,3-butylene glycol, glycerin), but water alone or a mixed solvent of water and ethanol are particularly preferred.
[0014] When using a mixed solvent, the preferred mixing ratio is, for example, 1:1 to 25:1 by volume (the same applies below) if water and ethanol are used.
[0015] Furthermore, the weight ratio of the part of each plant used to the extraction solvent is preferably 1:1 to 1:50, and more preferably 1:2 to 1:30.
[0016] While there are no particular limitations on the pH of the extract during preparation, it is generally preferable to have a pH in the range of 3 to 9. In this sense, if necessary, the extraction solvent may be mixed with an alkaline adjusting agent such as sodium hydroxide, sodium carbonate, or potassium hydroxide, or an acidic adjusting agent such as citric acid, hydrochloric acid, phosphoric acid, or sulfuric acid to adjust the pH to the desired level.
[0017] Extraction conditions such as extraction temperature and extraction time vary depending on the type of solvent and pH used. For example, when using water, ethanol, or a mixture of water and ethanol as the solvent, the extraction temperature is preferably in the range of 0°C to 80°C, more preferably in the range of 0°C to 20°C, and the extraction time is preferably in the range of 1 to 168 hours (1 hour to 1 week), more preferably in the range of 1 to 120 hours (1 hour to 5 days).
[0018] The extract according to the present invention may be extracted with water or a mixed solvent of water and a lower alcohol or polyhydric alcohol to remove impurities that contribute to the reduction of skin barrier function and skin roughness improvement effects, and to improve stability, and the filtered residue may be extracted again with water or a mixed solvent of water and a lower alcohol or polyhydric alcohol. Furthermore, for the purpose of removing skin irritants, it is preferable to remove impurities other than the active ingredient by combining one or more of the following: activated carbon treatment, ion exchange resin treatment, synthetic adsorbent, silica gel, and recrystallization treatment. As for activated carbon, any of the following may be used: plant materials such as pine wood, bamboo, coconut shells, and walnut shells, as well as coal and petroleum materials, and activated carbon obtained by physical methods such as high-temperature carbonization using gases such as steam, carbon dioxide, and air, or by chemical methods such as heating after treating with chemicals such as zinc chloride to make it porous. As for ion exchange resins, examples include weakly basic anion exchange resins, strongly acidic cation exchange resins, strongly basic inion exchange resins, and weakly acidic cation exchange resins. Furthermore, examples of synthetic adsorbents include chelate resins, strongly acidic cation adsorbent resins, styrene-divinylbenzene copolymers, and nonionic resins such as methacrylate ester polymers. It is suggested that any of these treatments can remove impurities that contribute to the reduction of skin barrier function and skin roughness improvement effects, as well as compounds that cause skin irritation.
[0019] The extract prepared as described above may be used as is in a formulation for topical skin preparations after adjusting the pH to 3-8, or it may be concentrated under reduced pressure to the desired concentration. The extract may also be dried using conventional methods such as spray drying.
[0020] Examples of skin preparations (cosmetics, quasi-drugs, topical pharmaceuticals) containing the extract of the present invention include, but are not limited to, emulsions, creams, lotions, essences, packs, lipsticks, foundations, sheet masks, liquid foundations, makeup press powders, blushes, face powders, facial cleansers, body shampoos, hair shampoos, soaps and other cleansing cosmetics, as well as bath additives.
[0021] When the extract of the present invention is formulated in a topical skin preparation for skin care, as the solid content of each extract, it is generally in the range of 0.00001 to 5.0% by weight, preferably 0.0001 to 1.0% by weight. When formulated in a topical skin preparation for hair, as the solid content of each extract, it is generally 0.00001 to 5.0% by weight (solid content weight %, the same hereinafter), preferably 0.0001 to 3.0% by weight.
[0022] When formulating the extract of the present invention in a topical skin preparation (cosmetics, quasi-drugs, topical pharmaceuticals, etc.), components used in topical skin preparations, such as oily components, surfactants (synthetic, natural), humectants, thickeners, emulsifiers or emulsification aids, preservatives and bactericides, powder components, ultraviolet absorbers, antioxidants, pigments, fragrances, anti-wrinkle agents, and other physiologically active components can be appropriately formulated as needed. Also, as long as the effectiveness and characteristics of the extract of the present invention are not impaired, it can be combined with other physiologically active components and formulated in a topical skin composition without any problem.
[0023] Here, examples of the oily component include plant-derived oils and fats such as olive oil, jojoba oil, castor oil, soybean oil, rice oil, rice bran oil, coconut oil, palm oil, cocoa butter, meadowfoam oil, shea butter, tea tree oil, avocado oil, macadamia nut oil, bergamot oil, lavender oil, rose oil, bergamot oil, chamomile oil, etc., such as plant-derived squalane; vitamin A oil; animal-derived oils and fats such as mink oil and turtle oil; waxes such as beeswax, carnauba wax, rice wax, and lanolin; hydrocarbons such as liquid paraffin, petrolatum, paraffin wax, and squalane; fatty acids such as myristic acid, palmitic acid, stearic acid, oleic acid, isostearic acid, and cis-11-eicosenoic acid; higher alcohols such as lauryl alcohol, cetyl alcohol, pantothenyl alcohol, and stearyl alcohol; synthetic esters and synthetic triglycerides such as isopropyl myristate, isopropyl palmitate, butyl oleate, 2-ethylhexyl glyceride, and octyldodecyl higher fatty acid (such as octyldodecyl stearate).
[0024] Examples of surfactants include nonionic surfactants such as polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters, polyoxyethylene sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene hydrogenated castor oil, and polyoxyethylene sorbitol fatty acid esters; fatty acid salts, alkyl sulfates, alkylbenzene sulfonates, polyoxyethylene alkyl ether sulfates, polyoxyethylene fatty amine sulfates, polyoxyethylene alkylphenyl ether sulfates, polyoxyethylene alkyl ether phosphates, α-sulfonated fatty acid alkyl ester salts, and polyoxyethylene Anionic surfactants such as ethylene alkylphenyl ether phosphates; cationic surfactants such as quaternary ammonium salts, primary to tertiary fatty amine salts, trialkylbenzylammonium salts, alkylpyridinium salts, 2-alkyl-1-alkyl-1-hydroxyethylimidazolinium salts, N,N-dialkylmorphonium salts, polyethylene polyamine fatty acid amide salts; and amphoteric surfactants such as N,N-dimethyl-N-alkyl-N-carboxymethylammonium betaine, N,N,N-trialkyl-N-alkyleneammonium carboxybetaine, and N-acylamidopropyl-N′,N′-dimethyl-N′-β-hydroxypropylammonium sulfobetaine can be used.
[0025] As emulsifiers and / or emulsifying aids, stevia derivatives such as enzyme-treated stevia, saponins or their derivatives, casein or its salts (sodium, etc.), sugar-protein complexes, sucrose or its esters, lactose, water-soluble polysaccharides derived from soybeans, complexes of soybean-derived proteins and polysaccharides, lanolin or its derivatives, cholesterol, stevia derivatives (such as enzyme-treated stevia), silicates (aluminum, magnesium, etc.), carbonates (calcium, sodium, etc.), saponins and their derivatives, lecithin and its derivatives (such as hydrogenated lecithin), lactic acid bacteria-fermented rice, lactic acid bacteria-fermented germinated rice, lactic acid bacteria-fermented grains (wheat, beans, grains, etc.), etc. may also be included.
[0026] Examples of humectants include glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol, sorbitol, xylitol, sodium pyrrolidone carboxylate, and sugars such as trehalose and raffinose, mucopolysaccharides (e.g., hyaluronic acid and its derivatives, hyaluronic acid ferment filtrate, chondroitin and its derivatives, heparin and its derivatives, etc.), elastin and its derivatives, collagen and its derivatives, collagen peptides, NMF-related substances, lactic acid, urea, higher fatty acid octyldodecyl, seaweed extracts, estradiol, various amino acids and their derivatives.
[0027] Examples of thickening agents include components derived from brown algae, green algae, or red algae such as alginic acid, agar, carrageenan, and fucoidan; polysaccharides such as pectin and aloe polysaccharide; gums such as tragacanth gum, locust bean gum, xanthan gum, and guar gum; cellulose derivatives such as carboxymethylcellulose, hydroxyethylcellulose, and hydroxypropylcellulose; synthetic polymers such as carboxyvinyl polymer, alkyl-modified carboxyvinyl polymer, polyvinyl alcohol, polyvinylpyrrolidone, and acrylic acid / methacrylic acid copolymer; hyaluronic acid and its derivatives; polyglutamic acid and its derivatives, polyacrylic acid, etc.
[0028] Anti-inflammatory agents include allantoin, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, β-glycyrrhetinic acid, stearyl glycyrrhetinate, ε-aminocaproic acid, d-camphor, dl-camphor, zinc oxide, panthenol, pyridoxine hydrochloride, and riboflavin or its derivatives.
[0029] Examples of preservatives and disinfectants include urea; benzoic acid or its salts, parahydroxybenzoic acid esters such as methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, and butyl parahydroxybenzoate; phenoxyethanol, dichlorophene, hexachlorophene, chlorhexidine hydrochloride, benzalkonium chloride, salicylic acid, sodium salicylate, zinc pyrithione, benzalkonium chloride, ethanol, undecylenic acid, phenols, and aluminum bromide. These include chloroisoquinolinium, resorcinol, jamal (imidazodinylurea), isopropylmethylphenol, triclosan, trichlorocarbanide, trichlorohydroxydiphenol ether, hinokitiol, 1,2-pentanediol, propanediol, concentrated benzalkonium chloride solution 50, essential oils such as peppermint oil and eucalyptus oil, tree bark distillates, radish ferment filtrate, plant-derived ethanol such as sugarcane and corn, or 1,3-butylene glycol.
[0030] Examples of cell activators include pantothenyl alcohol, menthol, dl-menthol, and γ-oryzanol.
[0031] Examples of anti-acne agents include sulfur, salicylic acid or its salts, photosensitizer 201, and pyridoxine dicaprylate.
[0032] Examples of powder components include sericite, titanium dioxide, talc, kaolin, bentonite, zinc oxide, magnesium carbonate, magnesium oxide, zirconium oxide, barium sulfate, anhydrous silicic acid, mica, nylon powder, polyethylene powder, silk powder, cellulose-based powders, grain powders (rice, wheat, corn, millet, etc.), and legume powders (soybeans, adzuki beans, etc.).
[0033] Examples of UV absorbers include ethyl para-aminobenzoate, ethylhexyl para-dimethylaminobenzoate, amyl salicylate and its derivatives, 2-ethylhexyl para-methoxycinnamate, octyl cinnamate, oxybenzone, 2,4-dihydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone-5-sulfonate, 4-tert-butyl-4-methoxybenzoylmethane, 2-(2-hydroxy-5-methylphenyl)benzotriazole, urocanic acid, ethyl urocanate, and aloe extract.
[0034] Examples of antioxidants include carotenoids such as butylhydroxyanisole, butylhydroxytoluene, propyl gallate, and astaxanthin, vitamin E and its derivatives (e.g., tocopherol acetate, tocopherol nicotinate), and vitamin A or its derivatives (e.g., retinol palmitate).
[0035] Furthermore, examples of whitening agents include one or more selected from ellagic acid and its derivatives, resorcinol derivatives, potassium 4-methoxysalicylate, magnolignan (5,5'-dipropyl-biphenyl-2,2'-diol), hydroxybenzoic acid and its derivatives, vitamin E and its derivatives, α-hydroxy acids, nicotinic acid derivatives, and AMP (adenosine monophosphate, adenosine monophosphate).
[0036] Examples of resorcinol derivatives include 4-n-butylresorcinol and 4-isoamylresorcinol; examples of 2,5-dihydroxybenzoic acid derivatives include 2,5-diacetoxybenzoic acid, 2-acetoxy-5-hydroxybenzoic acid, and 2-hydroxy-5-propionyloxybenzoic acid; and examples of α-hydroxy acids include lactic acid, malic acid, succinic acid, citric acid, and α-hydroxyoctanoic acid. One or more substances selected from kojic acid and its derivatives, ascorbic acid and its derivatives, hydroquinone or its derivatives, ellagic acid and its derivatives, nicotinic acid and its derivatives, resorcinol derivatives, tranexamic acid and its derivatives, potassium 4-methoxysalicylate, magnolignan (5,5'-dipropyl-biphenyl-2,2'-diol), hydroxybenzoic acid and its derivatives, vitamin E and its derivatives, α-hydroxy acids, AMP (adenosine monophosphate, adenosine monophosphate), t-cycloamino acid derivatives, mulberry bark extract, chamomile extract, hydrolyzed rice bran extract, saxifrage extract, and white poppy extract or their hydrolyzed products.
[0037] Examples of kojic acid derivatives include kojic acid esters such as kojic acid monobutyrate, kojic acid monocaprate, kojic acid monopalmitate, and kojic acid dibutyrate, kojic acid ethers, and kojic acid sugar derivatives such as kojic acid glucoside. Examples of ascorbic acid derivatives include ascorbic acid ester salts such as L-ascorbic acid-2-phosphate sodium, L-ascorbic acid-2-phosphate magnesium, L-ascorbic acid-2-sulfate sodium, and L-ascorbic acid-2-sulfate magnesium. Ascorbic acid sugar derivatives such as ascorbic acid-2-glucoside, L-ascorbic acid-5-glucoside, ascorbyl tocopheryl maleate, ascorbyl tocopheryl potassium phosphate, myristyl 3-glyceryl ascorbate, caprylyl 2-glyceryl ascorbate, 6-position acylated products of these ascorbic acid sugar derivatives (acyl groups include hexanoyl, octanoyl, and decanoyl groups), L-ascorbic acid tetra fatty acid esters such as L-ascorbic acid tetraisopalmitate and L-ascorbic acid tetralaurate, 3 As for hydroquinone derivatives, examples include -O-ethyl ascorbic acid, L-ascorbic acid-2-phosphate-6-O-palmitate sodium, glyceryl ascorbic acid or its acylated derivatives, ascorbic acid glycerin derivatives such as bisglyceryl ascorbic acid, L-ascorbic acid aminopropyl phosphate, hyaluronic acid derivatives of L-ascorbic acid, 3-OD lactose-L-ascorbic acid, isostearyl ascorbyl phosphate, etc. Hydroquinone derivatives include arbutin (hydroquinone-β-D-glucopyranoside), α-arbutin (hydroquinone-α-D-glucopyranoside), Examples of tranexamic acid derivatives include lucopyranoside, tranexamic acid esters (e.g., lauryl tranexamic acid ester, hexadecyl tranexamic acid ester, cetyl tranexamic acid ester or their salts), amide forms of tranexamic acid (e.g., methyl tranexamic acid amide), resorcinol derivatives include 4-n-butylresorcinol, 4-isoamylresorcinol, and 2,5-dihydroxybenzoic acid derivatives include 2,5-diacetoxybenzoic acid, 2-acetoxy-5-hydroxybenzoic acid,Examples of nicotinic acid derivatives include 2-hydroxy-5-propionyloxybenzoic acid, nicotinamide (niacinamide) and benzyl nicotinate, and alpha-hydroxy acids include lactic acid, malic acid, succinic acid, citric acid, and alpha-hydroxyoctanoic acid.
[0038] Furthermore, examples of anti-wrinkle agents include vitamin A or its derivatives, vitamin E or its derivatives (such as tocopherol acetate), vitamin C or its derivatives (such as ascorbic acid glucoside, 3-O-ethyl ascorbic acid, magnesium ascorbic acid phosphate salt, etc.), pantothenyl alcohol, tranexamic acid, nicotinamide, and allantoin.
[0039] Furthermore, the following natural ingredients derived from plants or microorganisms can also be used in combination: for example, collagen or its hydrolysates, yeast extract or hydrolysates, lactic acid bacteria cultures, grasses, cruciferous plants, camellias, roses, peonyes, citrus plants, amaranthaceae plants, eelgrasses, legumes, daisies, legumes, mallows, gentians, mints, lotus, cucurbits, Araliaceae plants, nightshades, bignoniaceae plants, Actinidiaceae plants, mulberries, irises, bellflowers, olives, Actinidiaceae plants, mulberries, rhamnoides, orchids, and sumac. Examples include extracts or hydrolyzed or fermented products thereof from one or more plants selected from the families of plants, Garcinia, Valenciaceae, Rutaceae, Myrtaceae, Liliaceae, Crassulaceae, Cupressaceae, Convolvulaceae, and Asparagaceae; extracts or hydrolyzed or fermented products thereof from one or more seaweeds selected from the families of Laminariaceae, Mylinaceae, and Ulvaceae; jellyfish (autolyzed products of moon jellyfish, Echizen jellyfish, etc.); hydrolyzed or fermented products of hyaluronic acid; and extracts or hydrolyzed or fermented products thereof from royal jelly.
[0040] As plant-derived components from the grass family, rice leaf hydrolysate, rice extract hydrolysate, rice bran extract hydrolysate, germinated brown rice hydrolysate, rice ferment filtrate, sake lees extract derived from sake, bamboo shoot peel extract of Madake or Moso bamboo, and adlay seed ferment. As plant-derived components from the Brassicaceae family, extracts or hydrolysates or fermentations thereof of the seeds of Hakugai, Ougai, or Kokugai are particularly preferred. As plant-derived components from the Camellia family, green tea (Yabukita, Samidori, Asahi, Gokou, Ujimidori, Kyomidori, Ujihikari, Samidori, Benifuki, etc.) and black tea (Darjeeling, Assam, Ceylon, Earl Grey, Honey Black Tea, etc.) are particularly preferred. As plant-derived components from the Rosaceae family, extracts of Damask rose flowers, peach flowers, leaves, or immature fruits, strawberry flower extract, and cherry blossom or leaf extract are preferred. Furthermore, as components derived from Paeoniaceae plants, extracts of peony root or flower, or peony flower are preferred. Furthermore, as components derived from Amaranthaceae plants, glasswort extract is particularly preferred. Furthermore, as components derived from Zosteraceae plants, extracts of Zostera margaritacea or Zostera japonica are particularly preferred. As components derived from Fabaceae plants, extracts of white soybeans or black soybeans or their hydrolysates or fermented soy milk liquid, adzuki bean extract, red clover extract, and kudzu root extract are particularly preferred. Furthermore, as components derived from Asteraceae plants, extracts of burdock root, sunflower sprout extract, starflower extract, arnica extract, or chamomile flower extract are particularly preferred. As components derived from Malvaceae plants, fermented products of hibiscus, rose of Sharon, or hibiscus are preferred. As components derived from Gentianaceae plants, gentian extract is preferred. Furthermore, as components derived from Lamiaceae plants, extracts of green perilla and Callicarpa japonica fruit are preferred. As for ingredients derived from Nelumbonaceae plants, lotus flower or lotus seed extract or lotus seed ferment is particularly preferred. As for ingredients derived from Cucurbitaceae plants, loofah extract is particularly preferred. As for ingredients derived from Araliaceae plants, ginseng extract or ferment is preferred. As for ingredients derived from Solanaceae plants, eggplant (long eggplant, water eggplant, American eggplant, Kamo eggplant, etc.) extract is an example. As for ingredients derived from Bignoniaceae plants, Pau d'arco bark extract is preferred. As for ingredients derived from Actinidiaceae plants, immature kiwi extract is preferred.Preferred ingredients from the Moraceae family include mulberry bark extract, mulberry fruit extract, and fig fruit or bark extract. Preferred ingredients from the Rhamnaceae family include jujube fruit extract. Preferred ingredients from the Iridaceae family include saffron. Preferred ingredients from the Campanulaceae family include root extract or hydrolysate of Codonopsis lanceolata. Preferred ingredients from the Anacardiaceae family include mango fruit extract. Preferred ingredients from the Garciniaaceae family include mangosteen fruit extract. Preferred ingredients from the Valenciaceae family include cherimoya fruit extract. Preferred ingredients from the Rutaceae family include Satsuma mandarin, bergamot fruit extract, grapefruit or pomelo fruit (including immature fruit), extracts containing flavonoids and their glycosides found in plants such as grapefruit or hassaku, or sansho seed extract. As ingredients derived from lily-family plants, extracts of Hemerocallis middendorffii, Hemerocallis fulva, Casablanca lily, Madonna lily, or Lilium japonicum are preferred. As ingredients derived from crasliaceae plants, extracts or fermented products of Rhodiola rosea are particularly preferred. As ingredients derived from olive-family plants, extracts of jasmine flowers are particularly preferred. As ingredients derived from cypress-family plants, extracts of Juniperus chinensis fruit are particularly preferred. As ingredients derived from myrtaceae plants, extracts of guava leaf are particularly preferred. As ingredients derived from orchids, extracts of Bletilla striata root are particularly preferred. As ingredients derived from morning glory-family plants, extracts or fermented products thereof of sweet potato, or extracts or fermented products thereof of sweet potato shochu lees are preferred. As ingredients derived from lamibariaceae seaweed, extracts of kelp are particularly preferred, as ingredients derived from miltiorrhiza, extracts of Sargassum fuciformis are preferred, and as ingredients derived from Ulvaceae seaweed, extracts of Ulva lactuca are particularly preferred. As for components derived from seaweed of the family *Sargassum*, *Sargassum* extract is particularly preferred.
[0041] Next, the present invention will be described in more detail with reference to manufacturing examples, formulation examples, and test examples, but the present invention is not limited thereto. In the following, all parts refer to parts by weight, and all percentages refer to weight percent.
[0042] Manufacturing Example 1. Preparation of Extract (1) The flowers, spathes, and stems of Calla Lily (Z. aethiopica) were dried, and 100g of the dried material was mixed with 4000g of purified water and immersed at a low temperature (4°C to 20°C) for 24 hours. Next, the resulting liquid was filtered and the residue was collected. Then, 4000g of a 50% ethanol aqueous solution was added to the residue and extracted at a temperature slightly higher than room temperature (30°C to 40°C) for 2 to 3 hours. This was filtered to obtain 3700g of a brown, transparent crude extract of Calla Lily flowers.
[0043] Manufacturing Example 2. Preparation of Extracts (2) The flowers, spathes, and stems of Calla Lily (Z. aethiopica) were dried, and 100g of the dried material was mixed with 4000g of purified water and immersed at a low temperature (4°C to 20°C) for 24 hours. Next, the resulting liquid was filtered and the residue was collected. 4000g of a 50% 1,3-butylene glycol aqueous solution was added and extracted at a temperature slightly above room temperature (30°C to 40°C) for 2 to 3 hours. This was filtered to obtain 3750g of a brown, transparent crude extract of Calla Lily flowers.
[0044] Manufacturing Example 3. Preparation of Extracts (3) The flowers, spathes, and stems of Calla Lily (Z. aethiopica) were dried, and 100g of the dried material was mixed with 4000g of purified water and immersed at a low temperature (4°C to 20°C) for 24 hours. The resulting liquid was filtered, and the residue was collected. Next, 4000g of a 50% propylene glycol aqueous solution was added to the residue, and the mixture was extracted at a temperature slightly above room temperature (30°C to 40°C) for 2 to 3 hours. This was filtered to obtain 3750g of a brown, transparent crude extract of Calla Lily flowers.
[0045] Alternatively, the above extract may be prepared by removing the organic solvent by vacuum concentration, etc., then applying the concentrated extract to an adsorbent (e.g., a methacrylate ester-based adsorbent), washing with an aqueous ethanol solution, and then eluting with 1,3-butylene glycol. The eluate is filtered, purified water is added, and a yellowish-brown transparent extract with a predetermined solid content concentration is prepared as appropriate (solid content concentration: 0.09% to 0.15%). By performing the concentration and adsorption treatment as described above, impurities are removed, and an extract solution with high efficacy and stability as shown below is obtained.
[0046] Test Example 1. Evaluation Test of SOD-like Activity A test solution was prepared by mixing 0.15 mL of 1 M Tris-HCl buffer, 0.30 mL of 1 mM ethylenediaminetetraacetic acid disodium salt solution, 0.30 mL of 1 mM xanthine solution, 0.20 mL of 0.75 mM nitrobule-tetrazolium solution, 0.10 mL of the extract solution from Preparation Example 1, and 1.90 mL of purified water. In addition, a mixed solution (control) with the same composition as the above test solution was prepared, except that 0.10 mL of 30% 1,3-butylene glycol was used instead of 0.10 mL of the extract solution from Preparation Example 1. For the test solution, the final concentrations (concentration as a solution) of each extract solution relative to the total volume were 0.5%, 1.0%, and 2.0%. Furthermore, a mixture (positive control) with the same composition as the above test solution was prepared, except that 0.10 mL of a 0.875 Unit / mL superoxide dismutase solution was used instead of 0.10 mL of the extract solution from Production Example 1 in the test solution. The above test solution, or the mixture without sample, was incubated at 37°C, and then 0.05 mL of a 1 Unit / mL xanthine oxidase solution was added. After a certain period of time (5 minutes), the absorbance of each test solution at 570 nm (an indicator of the amount of superoxide anion in the test solution) was measured. The results are shown as percentages of the absorbance of each test solution or the positive control (superoxide dismutase) mixture, with the absorbance of the control mixture set to 100%.
[0047] The results of Test Example 1 are shown in Table 1. [Table 1] JPEG0007847815000001.jpg37123
[0048] As shown in Table 1, the extract according to the present invention was confirmed to have remarkably superior SOD-like activity.
[0049] In the evaluation tests for Test Example 2 and Test Example 3, the effects of substances involved in immunity (inflammasomes) will be evaluated as follows. Here, an inflammasome is a protein complex consisting of NLRP3, ASC, and caspase-1, etc., that is formed in cells in response to bacteria and various other external stimuli. When this protein complex is formed, caspase-1 is activated, and caspase-1 further activates cytokines (IL-1β, IL-18, etc.), resulting in the release of cytokines outside the cell, which cause inflammation. In this invention, a substance that induces inflammasome formation (external ATP) will be used to evaluate the inhibitory effect of the extract according to the present invention on the decline of skin barrier function and the preventive and ameliorative effects on rough skin.
[0050] Test Example 2. Intracellular Caspase 1 Activity Evaluation Test The experiment was conducted using normal human epidermal cells (NHEK). 6 × 10⁶ cells were used per well in a 24-well plate. 4 The cells were seeded to a total of 1.5%. Extract solutions from Production Example 1 (prepared so that the final concentrations of the solutions in the culture medium were 0.25%, 0.5%, and 1.0%) were added to each culture medium (HuMedia-KB2) as sample solutions, and the cells were cultured in each culture medium for 2 days. After culturing, Lipopolysaccharide (Invitrogen) was added to a final concentration of 2.5 μg / mL, and the culture was continued for 4 hours. Then, the culture was replaced with HuMedia-KB2 containing 2 mM ATP as an inflammasome activity inducer, and cultured for another 1 hour. For the control, cells were cultured without replacing them with HuMedia-KB2 containing ATP, and this control (uninduced) was used as the control for the caspase-1 activity evaluation test. Next, the cultured cells were stained using Pyroptosis / Caspase-1 Assay (ImmunoChemistry Technologies), and flow cytometry (BD Accuri) was performed. TMThe fluorescence intensity (Ex. = 488 nm, Em. = 533 ± 15 nm) was measured using a C6 Plus Flow Cytometer (BD Biosciences). The activation rate of caspase-1 in cells was calculated using the fluorescence intensity of the control (uninducible) as a baseline of 100.
[0051] The results of Test Example 2 are shown in Table 2. [Table 2] JPEG0007847815000002.jpg53122
[0052] As shown in Table 2, in cells cultured with the control (50% 1,3-butylene glycol aqueous solution), caspase-1 was activated by foreign ATP [Control (Induced) in Table 2]. In contrast, it was confirmed that the extract according to the present invention suppresses the activity of caspase-1 activated by foreign ATP. Thus, the extract according to the present invention can suppress the activity of caspase-1, a substance that causes cytokine activation in cells due to various environmental factors (bacteria, viruses, etc.), and can suppress the decline in skin barrier function caused by cytokines and prevent and improve rough skin.
[0053] Test Example 3. Evaluation test for increased expression of filaggrin 2 (natural moisturizing factor) Experiments were conducted using normal human epidermal cells (NHEK). Extract solutions from Production Example 1 (prepared to achieve final concentrations of 0.25%, 0.5%, and 1.0% in the culture medium) and a 50% 1,3-butylene glycol aqueous solution (prepared to achieve a final concentration of 1.0% in the culture medium) were added to HuMedia-KB2 culture medium, and the cells were cultured for 2 days. Furthermore, ATP was added as an inflammasome activation inducer to a final concentration of 200 μM, and the cells were cultured for another 2 days. For the control, cells cultured without substituting ATP-containing HuMedia-KB2 were also prepared and used as the control (uninducible) for the evaluation of filaggrin 2 gene expression enhancement. After the completion of culture, filaggrin 2 expression levels were measured using real-time PCR with total RNA extracted from NHEK cells. PrimeScript was used for the reverse transcription reaction. TM RT reagent kit with gDNA Eraser (TaKaRaBio), TB Green® Premix Ex Taq for real-time PCR reactions. TM We used II (TaKaRaBio). GAPDH was used as the internal standard, and the expression level of filaggrin 2 was determined as the relative expression level to GAPDH according to the established method.
[0054] The results of Test Example 3 are shown in Table 3. [Table 3] JPEG0007847815000003.jpg45142
[0055] As shown in Table 3, in cells cultured with the control (50% 1,3-butylene glycol aqueous solution), the expression of the filaggrin 2 gene, a natural moisturizing factor, was suppressed by the inflammasome [Control (Induction) in Table 3]. In contrast, the extract according to the present invention was confirmed to enhance the expression of the filaggrin 2 gene, which is suppressed by the inflammasome. As a result, the extract according to the present invention can suppress the decrease of moisturizing factors produced in cells by various environmental factors (bacteria, viruses, etc.), thereby suppressing the decline in skin barrier function and preventing and improving rough skin.
[0056] Test Example 4. Evaluation Test of Stratum Corneum Moisture Content Two test areas (15mm x 15mm) were set on the medial side of the left forearm of three male subjects (ages 20-50). The stratum corneum moisture content of each test area was measured five times using a Skicon-200, and a Tewameter was also used. TM Transepidermal water loss (TEW) was measured using a specific method, and the average of these measurements was used as the initial value for each test area. After measuring each initial value, the application of the respective samples to the test and control areas was started. Three days later, 5% SDS was patched onto filter paper for one hour to reduce the barrier function. Starting one day later, stratum corneum water content and transepidermal water loss were measured over time. The initial values were set to 0, the stratum corneum water content after the SDS barrier reduction treatment to -100, and transepidermal water loss to 100, and measurements were taken for each test area on days 1, 2, and 3. The measurement results were calculated from the average values for each test area.
[0057] The results of Test Example 4 are shown in Figures 1 and 2. As shown in Figures 1 and 2, the extract according to the present invention has the effect of quickly restoring the stratum corneum moisture content that has decreased due to SDS treatment compared to the control, and also showed the effect of suppressing the transepidermal water loss that increased due to the decrease in skin barrier function caused by SDS treatment.
[0058] Prescription example 1. Lotion [Ingredients] Part Extract from manufacturing example 1: 0.5 Squalane 0.2 Polyoxyethylene (5.5) cetyl alcohol 5.0 Tocopherol acetate 0.02 Dipotassium glycyrrhizinate 0.5 Monoammonium glycyrrhizinate 0.5 Isopropylmethylphenol 0.1 1,3-Butylene glycol 5.0 Sodium citrate 0.2 Methylparaben 0.1 Purified water, in an amount that makes the total volume 100 parts
[0059] Prescription example 2. Lotion A lotion was obtained in the same manner as in Formulation Example 1, except that 0.5 parts of the extract from Manufacturing Example 2 were used instead of 0.5 parts of the extract from Manufacturing Example 1 in the ingredients of Formulation Example 1.
[0060] Prescription example 3. Lotion A lotion was obtained in the same manner as in Formulation Example 1, except that 0.5 parts of the extract from Manufacturing Example 3 were used instead of 0.5 parts of the extract from Manufacturing Example 1 in the ingredients of Formulation Example 1.
[0061] Prescription example 4. Lotion [Ingredients] Part Extract from Production Example 1: 1.0 Glyceryl caprylate 3.0 Polyglyceryl-10 laurate 3.0 Cetanol 2.0 Behenyl alcohol 2.0 Niacinamide 5.0 Dipotassium glycyrrhizinate 0.1 Peony flower extract 1.0 Saffron extract 1.0 Glycerin 1.0 1,3-Butylene glycol 1.0 Pentanediol 1.0 Potassium hydroxide 0.5 Purified water, in an amount that makes the total volume 100 parts.
[0062] Prescription example 5. Lotion [Ingredients] Part Extract from manufacturing example 1: 0.5 Jojoba oil 1.0 Polyoxyethylene (5.5) cetyl alcohol 5.0 Methylparaben 0.1 Ascorbic acid glucoside 2.0 Niacinamide 5.0 ε-aminocaproic acid 0.1 Sulfur 0.2 Estradiol 0.1 Pyridoxine hydrochloride 0.5 Glycerin 5.0 1,3-Butylene glycol 5.0 Sodium citrate 0.2 Sodium metabisulfite 0.2 d-camphor 0.1 Purified water, in an amount that makes the total volume 100 parts.
[0063] Prescription example 6. Emulsion [Ingredients] Part Extract from Production Example 1: 1.5 Squalane 5.0 Cyclopentasiloxane 1.0 Hexaran 3.0 Hexyldecyl isostearate 1.0 Caprylic / Capric Triglyceride 1.0 Polyglyceryl-10 laurate 5.0 Polyglyceryl-10 isostearate 5.0 Ascorbyl dipalmitate 15.0 Hydrogenated soy lecithin 1.5 Magnesium ascorbic acid phosphate salt 3.0 Arbutin 3.0 Potassium hydroxide 0.5 Glycerin 3.0 1,3-Butylene glycol 2.0 Carboxymethylcellulose 0.3 Xanthan gum 0.2 Tremella fuciformis polysaccharide 0.2 Sodium hyaluronate 0.01 Tocopherol acetate 0.3 Tocopherol nicotinate 0.1 Glycyrrhizic acid 0.1 Dipotassium glycyrrhizinate 0.1 Isopropylmethylphenol 0.1 Water-soluble collagen 1.0 Hydrolyzed collagen 1.0 Acetylated hyaluronic acid 0.1 Purified water, in an amount that makes the total volume 100 parts.
[0064] Prescription example 7. Emulsion An emulsion was obtained in the same manner as in Formula Example 6, except that 2.0 parts of L-ascorbic acid-2-glucoside were used instead of 2.0 parts of magnesium ascorbic acid phosphate in the ingredients of Formula Example 6.
[0065] Prescription example 8. Emulsion An emulsion was obtained in the same manner as in Formula Example 6, except that 2.0 parts of magnesium ascorbic acid phosphate and 1.0 part of tranexamic acid were used instead of potassium hydroxide in the components of Formula Example 6.
[0066] Prescription example 9. Emulsion An emulsion was obtained in the same manner as in Formulation Example 6, except that 3.0 parts of 3-O-ethyl ascorbic acid were used instead of 2.0 parts of magnesium ascorbic acid phosphate in Formulation Example 6.
[0067] Prescription example 10. Emulsion An emulsion was obtained in the same manner as in Formula Example 6, except that 2.0 parts of magnesium ascorbic acid phosphate and 1.0 part of niacinamide were used instead of potassium hydroxide in the components of Formula Example 6.
[0068] Prescription example 11. Cream [Ingredients] Part Olive oil 5.0 Squalane 5.0 Jojoba oil 5.0 Jojoba wax 1.0 Behenyl alcohol 1.0 Stearyl alcohol 1.0 Candelilla wax 1.0 Lactic acid fermented rice 2.0 Hydrogenated lecithin derived from soybeans 0.5 Extract from Production Example 1: 1.0 Peony flower extract 1.0 Saffron flower extract 1.0 Carboxyvinyl polymer 1.0 Sodium alginate 1.0 Glycerin 2.0 Pentanediol 1.0 pH adjuster (appropriate amount) Purified water, in an amount that makes the total volume 100 parts.
[0069] Prescription example 12. Cream [Ingredients] Part Extract from Production Example 1: 1.0 Olive oil 5.0 Jojoba oil 5.0 Squalane 5.0 Hexyldecyl isostearate 5.0 Lauroyl glutamate di(octyldodecyl / phytosteryl) (Behenir) 5.0 Glyceryl caprylate 1.0 Glyceryl stearate 1.0 Isostearyl glyceryl 3.0 γ-oryzanol 0.1 Behenyl alcohol 2.0 Palmitic acid 2.5 D-Panthenyl alcohol 3.0 Allantoin 0.1 Riboflavin 0.01 Resorcinol 0.1 Benzalkonium chloride 0.05 Urea 3.0 β-Glycyrrhetinic acid 0.1 Stearyl glycyrrhetinate 0.1 Ammonium glycyrrhizinate 0.1 Niacinamide 5.0 Lactic acid fermented rice 2.0 Hydrogenated lecithin 0.5 Hydrogenated lysolecithin 0.5 Hydrolyzed collagen 1.0 Xanthan gum 1.0 Zinc oxide 0.5 dl-camphor 0.3 l-menthol 0.5 Purified water, in an amount that makes the total volume 100 parts.
[0070] Example 13. Pack [Ingredients] Part Extract from Production Example 1: 1.0 Dipropylene glycol 5.0 Polyoxyethylene (60) hydrogenated castor oil 5.0 Cetanol 3.0 Behenyl alcohol 3.0 Allantoin 0.1 Dipotassium glycyrrhizinate 0.1 Ammonium glycyrrhizinate 0.1 β-Glycyrrhetinic acid 0.1 Stearyl glycyrrhetinate 0.1 Salicylic acid 0.1 Tocopherol acetate 0.5 Tocopherol nicotinate 0.1 D-Pantothenyl alcohol 0.3 Resorcinol 0.1 Sulfur 2.0 Estradiol 0.002 Water-soluble collagen 1.0 Xanthan gum 2.0 Polyglyceryl-6 myristate 1.0 Potassium cocoyl glutamate 1.0 Hydrogenated lecithin 3.0 Hydroxylated lecithin 3.0 Purified water, in an amount that makes the total volume 100 parts.
[0071] Prescription Example 14: Hair Shampoo [Ingredients] Part Extract from Production Example 1 2.0 Sodium laureth sulfate 10.0 Glyceryl monostearate 1.0 Coconut oil fatty acid diethanolamide 2.0 Polyoxyethylene (40) hydrogenated castor oil 0.5 Benzalkonium chloride 1.0 Stearyl alcohol 2.0 Behenyl alcohol 2.0 Dimethicone 3.0 Allantoin 0.1 Dipotassium glycyrrhizinate 0.1 Salicylic acid 0.1 Sodium salicylate 0.1 Tocopherol acetate 0.1 Pyrithione Zinc 0.3 Benzoic acid 0.2 Triclosan 0.2 Citric acid 0.1 Propylene glycol 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0072] Prescription Example 15: Hair Conditioner [Ingredients] Part Extract from Production Example 1: 1.0 Polyoxyethylene (10) hydrogenated castor oil 1.0 Distearyldimethylammonium chloride 1.5 Stearyltrimethylammonium chloride 2.0 Glyceryl 2-ethylhexanoate 1.0 Benzalkonium chloride 1.0 Cetanol 3.0 Stearyl alcohol 1.0 Allantoin 0.1 Isopropylmethylphenol 0.1 Dipotassium glycyrrhizinate 0.1 Salicylic acid 0.1 Sulfur 0.5 Alkylisoquinolinium bromide solution (75%) 0.06 Pyrithione Zinc 0.3 Methylparaben 0.1 Triclosan 0.2 Resorcinol 0.1 Purified water, in an amount that makes the total volume 100 parts.
[0073] Prescription Example 16. Cleansing Cosmetics [Ingredients] Part Extract from Production Example 1 2.0 Potassium cocoyl glycine 5.0 Glycerin 10.0 Glyceryl caprylate 1.0 Sodium lauroyl aspartate 10.0 Water-soluble collagen 5.0 Cetanol 3.0 Myristyl alcohol 3.0 Isopropylmethyl alcohol 0.1 Allantoin 0.1 Sulfur 0.5 Glycyrrhizic acid 0.1 Dipotassium glycyrrhizinate 0.1 Monoammonium glycyrrhizinate 0.1 β-Glycyrrhetinic acid 0.05 Stearyl glycyrrhetinate 0.1 Salicylic acid 0.2 Tocopherol acetate 0.2 Triclosan 0.1 Trichlorocarbanide 0.5 Trichlorohydroxydiphenyl ether 0.2 Concentrated benzalkonium chloride solution 50 0.2 Benzalkonium chloride 0.1 Purified water, in an amount that makes the total volume 100 parts.
[0074] Prescription Example 17: Sheet Mask A sheet mask is obtained by impregnating a nonwoven fabric with the following ingredients. [Ingredients] Part Extract from Production Example 1: 1.0 Niacinamide 1.0 Peony flower extract 1.0 Saffron flower extract 1.0 Citric acid 0.1 Sodium citrate 0.3 Xanthan gum 0.1 Water-soluble collagen 0.1 Sodium hyaluronate 0.01 Glycerin 1.0 1,3-Butylene glycol 2.0 Pentanediol 1.0 Potassium hydroxide (appropriate amount) Purified water, in an amount that makes the total volume 100 parts.
[0075] Prescription Example 18: Serum [Ingredients] Part Extract from Production Example 1 2.0 Sodium hyaluronate 1.0 Water-soluble collagen 1.0 Tranexamic acid 0.1 Ethanol 2.0 Glycerin 5.0 1,3-Butylene glycol 5.0 Methylparaben 0.1 Citric acid 0.3 Sodium citrate 0.6 Katamenkirinsai extract 5.0 Purified water, in an amount that makes the total volume 100 parts.
[0076] Prescription example 19. Cream [Ingredients] Part Olive oil 5.0 Squalane 5.0 Jojoba oil 5.0 Jojoba wax 1.0 Shea butter 2.0 Behenyl alcohol 1.0 Stearyl alcohol 1.5 Candelilla wax 0.5 Niacinamide 1.0 Extract from manufacturing example 1: 0.5 Peony flower extract 0.5 Saffron flower extract 0.5 Lactic acid fermented rice 3.0 Hydrogenated lecithin 2.0 Katamenkirinsai extract 2.0 Carboxyvinyl polymer 0.3 Sodium alginate 0.2 Glycerin 4.0 Potassium hydroxide (appropriate amount) Purified water, in an amount that makes the total volume 100 parts.
Claims
1. A caspase-1 activity inhibitor containing a plant extract from the genus Zantedeschia of the Araceae family as its active ingredient.
2. A filaggrin gene expression enhancer comprising a plant extract of the genus Zantedeschia of the family Araceae as an active ingredient.
Citation Information
Patent Citations
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