Topical skin preparations
A topical skin preparation with niacinamide and jujube extract enhances HIF-1α transcription to improve skin barrier function and prevent dryness and thinning, addressing the inadequacies of existing anti-aging solutions.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-04-14
- Publication Date
- 2026-03-27
AI Technical Summary
Existing cosmetic and pharmaceutical solutions for addressing skin aging and dryness, such as those containing α-hydroxycarboxylic acid, collagen, elastin, hyaluronic acid, and antioxidants, are insufficient in preventing and improving skin impairment and aging.
A topical skin preparation combining niacinamide and an extract from the jujube tree (Ziziphus jujuba) to enhance HIF-1α transcription activity, which addresses skin dryness and thinning.
The combination promotes HIF-1α transcription activity, improving skin barrier function, preventing dryness, and reducing skin thinning.
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Figure 0007836548000001
Abstract
Description
Technical Field
[0001] The present invention relates to a combination of active ingredients to be formulated in an external preparation for the skin.
Background Art
[0002] Conventionally, with aging, due to reasons such as inactivation of cell proliferation and differentiation, decrease in hormone secretion, quantitative decrease of extracellular matrix components (such as collagen and laminin) that constitute the skin, and further decrease in muscle strength due to decrease in muscle fibers, it is known that aging phenomena of the skin (such as wrinkles and sagging) or skin disorders (such as dryness and roughness) occur.
[0003] For the purpose of preventing and improving cell impairment and aging, various active ingredients have been conventionally proposed, and cosmetics, foods and drinks, and pharmaceuticals containing these active ingredients have been marketed. For example, cell-activating ingredients such as α-hydroxycarboxylic acid; extracellular matrix components such as collagen, elastin, hyaluronic acid or its salts; moisturizing agents such as urea; can be mentioned. Furthermore, antioxidants and moisturizing agents derived from plants have also been proposed, but they have been insufficient in terms of the effect of preventing and improving cell impairment and aging.
Patent Document 1
Patent Document 2
Patent Document 3
Patent Document 4
Disclosure of the Invention
Problems to be Solved by the Invention
[0004] In order to solve the problems of the above-mentioned conventional technology, the present applicant has focused on hypoxia-inducing factor (HIF-1α) involved in skin dryness and thinning of the skin (tenuity) caused by external factors such as ultraviolet rays and aging, and aims to find a combination of active ingredients for preventing and improving dry skin and thinning of the skin. [Means for solving the problem]
[0005] The present invention is an HIF-1α transcription activity enhancer comprising niacinamide and an extract of the fruit of the jujube tree (Ziziphus jujuba), a member of the Rhamnaceae family, as active ingredients. The present invention relates to a topical skin preparation containing a HIF-1α transcription activity enhancer, which comprises niacinamide and an extract of the fruit of the jujube tree (Ziziphus jujuba), a member of the Rhamnaceae family, as active ingredients. [Effects of the Invention]
[0006] According to the present invention, it is possible to provide a topical skin preparation that, through the active ingredients of the present invention, exhibits the effects of preventing and improving skin dryness, preventing and improving skin thinning, and improving skin barrier function. [Brief explanation of the drawing]
[0007] [Figure 1] This figure shows the HIF-1α transcription activity promoting effect of the composition according to the present invention. [Modes for carrying out the invention]
[0008] Preferred embodiments of the present invention will be described in detail below. The active ingredient of this invention, niacinamide (also known as nicotinamide), is a type of water-soluble vitamin and is an amide compound of niacin (nicotinic acid).
[0009] Furthermore, the active ingredient of this invention, jujube, is Ziziphus jujuba, a species of jujube belonging to the Rhamnaceae family, and its dried fruit (jujube) is known as a crude drug. In this invention, it is preferable to use the fruit of the jujube tree.
[0010] The preparation of jujube extract, one of the active ingredients of the present invention, can be carried out by washing the jujube, which is the object to be extracted, with water if necessary to remove foreign matter, then either leaving it as is or drying it, and if necessary, finely chopping or grinding it, and then contacting it with an extraction solvent according to conventional methods such as immersion, countercurrent extraction, or steam distillation. In addition, supercritical extraction may be used in the present invention.
[0011] Examples of extraction solvents used in the extraction process 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.
[0012] While there are no particular restrictions on the pH of the extract when preparing the extract, it is generally preferable to have a pH in the range of 3 to 9. pH adjustment can be performed by adding alkaline adjusting agents such as sodium hydroxide, sodium carbonate, or potassium hydroxide, or acid adjusting agents such as citric acid, hydrochloric acid, phosphoric acid, or sulfuric acid to the extraction solvent.
[0013] Extraction conditions such as extraction temperature and time vary depending on the type of solvent used, pH, and size of the plant material. For example, in the case of immersion extraction using a mixed solvent of water and a lower alcohol or polyhydric alcohol, the extraction temperature is in the range of 0 to 80°C. The extraction time is typically in the range of 1 hour to 7 days for cold extraction at 4°C, 1 hour to 3 days for medium-temperature extraction around 40°C, and 1 hour to 24 hours for high-temperature extraction at 70 to 80°C. In the immersion method, the bath ratio is generally 1 to 200 times the amount of solvent to the material (jujube), preferably 1 to 100 times.
[0014] To enhance the stability and effectiveness of the jujube extract prepared as described above, it is preferable to further prepare the extract by combining one or more of the following treatments: 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, or air, or by chemical methods such as heating after treating the raw materials with chemicals such as zinc chloride to make them 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. As for synthetic adsorbents, examples include chelate resins, strongly acidic cation adsorbent resins, styrene / divinylbenzene copolymers, and methacrylic acid ester polymers, which are nonionic resins.
[0015] In the present invention, the term "topical skin preparation" includes cosmetics, quasi-drugs, and topical pharmaceuticals, and includes, for example, emulsions, creams, lotions, essences, packs, lipsticks, foundations, liquid foundations, makeup pressed powders, blushes, face powders, facial cleansers, body shampoos, slimming agents, hair shampoos, soaps, and the like, as well as bath additives, but is not limited to these.
[0016] In addition to the combination of niacinamide and jujube extract, other ingredients used in topical skin preparations, such as oily components, surfactants (synthetic and natural), moisturizers, thickeners, preservatives / bactericides, powder components, UV absorbers, antioxidants, dyes, and fragrances, may be appropriately blended as needed. Furthermore, there is no problem in combining other physiologically active ingredients as long as the effectiveness and characteristics of the extract, hydrolysate, or fermented product according to the present invention are not impaired.
[0017] When using the combination of niacinamide and jujube extract according to the present invention in a topical skin preparation, various ingredients that can be incorporated into them, such as oily components, surfactants (synthetic and natural), emulsifiers, moisturizers, thickeners, preservatives / bactericides, defoaming agents, powder components, antioxidants, chelating agents, pH adjusters, pigments, fragrances, etc., can be appropriately added as needed. Furthermore, as long as the effectiveness and characteristics of the fermented product according to the present invention are not impaired, it is perfectly acceptable to combine it with other physiologically active ingredients.
[0018] Here, oily components include, for example, lotus oil, olive oil, jojoba oil, castor oil, soybean oil, rice oil, rice bran oil, rice germ oil, coconut oil, chamomile oil, palm oil, cocoa oil, meadowfoam oil, bergamot oil, rosehip oil, coffee arabic seed oil, lavender oil, shea butter, tea tree oil, avocado oil, macadamia nut oil, vanilla oil, plant-derived oils such as squalane; animal-derived oils such as mink oil and turtle oil; waxes such as beeswax, carnauba wax, rice wax, and lanolin; and liquid paraffin. Examples include hydrocarbons such as petrolatum, paraffin wax, and squalane; fatty acids such as myristic acid, palmitic acid, stearic acid, oleic acid, isostearic acid, and eicosenoic acid; higher alcohols such as lauryl alcohol, cetanol, and stearyl alcohol; synthetic esters and synthetic triglycerides such as isopropyl myristate, isopropyl palmitate, butyl oleate, cetyl isooctanoate, 2-ethylhexylglyceride, and higher fatty acid octyldodecyl (octyldodecyl stearate, etc.).
[0019] In addition, examples of surfactants include nonionic surfactants such as polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyethylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitol fatty acid ester; anionic surfactants such as fatty acid salts, alkyl sulfates, alkylbenzene sulfonates, polyoxyethylene alkyl ether sulfates, polyoxyethylene fatty amine sulfates, polyoxyethylene alkyl phenyl ether sulfates, polyoxyethylene alkyl ether phosphates, α-sulfonated fatty acid alkyl ester salts, polyoxyethylene alkyl phenyl ether phosphates; cationic surfactants such as quaternary ammonium salts, primary to tertiary fatty amine salts, trialkylbenzyl ammonium salts, alkylpyridinium salts, 2-alkyl-1-alkyl-1-hydroxyethyl imidazolinium salts, N,N-dialkyl morpholinium salts, polyethylene polyamine fatty acid amide salts; amphoteric surfactants such as N,N-dimethyl-N-alkyl-N-carboxymethyl ammonium betaine, N,N,N-trialkyl-N-alkylene ammonium carboxy betaine, N-acylamidopropyl-N′,N′-dimethyl-N′-β-hydroxypropyl ammonium sulfobetaine, etc. can be used.
[0020] In addition, as an emulsifier or emulsification aid, stevia derivatives such as enzymatically treated stevia, saponin or its derivatives, casein or its salts (such as sodium), complexes of sugars and proteins, sucrose or its esters, lactose, water-soluble polysaccharides derived from soybeans, complexes of soy-derived proteins and polysaccharides, lanolin or its derivatives, cholesterol, stevia derivatives (such as stevia enzyme fermentation products), silicates (such as aluminum, magnesium), carbonates (such as calcium, sodium), saponin and its 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 (such as wheat, beans, miscellaneous grains), etc. can also be blended.
[0021] In addition, examples of the humectant include glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol, sorbitol, xylitol, sodium pyrrolidone carboxylate, 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer liquid, and the like. Further, saccharides such as trehalose, mucopolysaccharides (e.g., hyaluronic acid and its derivatives, chondroitin and its derivatives, heparin and its derivatives, etc.), tuberose polysaccharide, elastin and its derivatives, collagen and its derivatives, NMF-related substances, hydrolyzed conchiolin, hydrolyzed silk, Sphingomonas culture, sphingoglycolipid, ceramide, lactic acid, urea, octyldodecyl higher fatty acid, seaweed extract, extract of Rhizoma Bletillae (Bletilla striata), various amino acids and their derivatives can be mentioned.
[0022] In addition, examples of the thickener include components derived from brown algae, green algae or red algae such as alginic acid, agar, carrageenan, fucoidan; extract of Rhizoma Bletillae (Bletilla striata); polysaccharides such as pectin, locust bean gum, aloe polysaccharide, polysaccharide produced by Alcaligenes; gums such as xanthan gum, tragacanth gum, locust bean gum, guar gum; cellulose derivatives such as carboxymethyl cellulose, hydroxyethyl cellulose; synthetic polymers such as polyvinyl alcohol, polyvinyl pyrrolidone, carboxyvinyl polymer, mastic resin, acrylic acid / methacrylic acid copolymer; hyaluronic acid and its derivatives; polyglutamic acid and its derivatives, and the like.
[0023] In addition, examples of the preservative and bactericide include urea; paraoxybenzoic acid esters such as methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate; phenoxyethanol, dichlorophen, hexachlorophene, chlorhexidine hydrochloride, benzalkonium chloride, salicylic acid, ethanol, undecylenic acid, phenols, Jamal (imidazolidinyl urea), polyphosphoric acid, propanediol, 1,2-pentanediol, various essential oils, dry distillate of bark, fermented radish liquid, ethanol or 1,3-butylene glycol derived from plants such as sugarcane, and the like.
[0024] In addition, powder components include, for example, 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.).
[0025] 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.
[0026] Examples of defoaming agents include ethanol, isopropanol, disiloxane, dimethylpolycyclosane, dimethicone silica, trisiloxane, silylated silica, dimethicone, trimethylsiloxysilicate, and DPG isobornyl ether.
[0027] Examples of antioxidants include butylhydroxyanisole, butylhydroxytoluene, propyl gallate, extract of Callicarpa japonica, extract of Bletilla striata root, extract of Paeonia lactiflora, vitamin E and its derivatives (e.g., vitamin E nicotinate, vitamin E linoleate, etc.).
[0028] Examples of chelating agents include trisodium ethylenediamine hydroxyethyl triacetate, EDTA or its salts, gluconic acid, phytic acid, sodium polyphosphate, sodium metaphosphate, and tetrasodium hydroxyethanediphosphonate.
[0029] Examples of pH adjusting agents include citric acid or its salts, lactic acid or its salts, glycolic acid, succinic acid, hydrochloric acid, monoethanolamine, diethanolamine, triethanolamine, sodium hydroxide, potassium hydroxide, and the like.
[0030] Furthermore, examples of whitening agents include t-cycloamino acid derivatives, 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, and AMP (adenosine monophosphate, adenosine monophosphate). These may be used individually or in combination.
[0031] Furthermore, the above-mentioned kojic acid derivatives include, for example, 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. Ascorbic acid derivatives include, for example, 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 ester salts, L-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 tetraisopalmitate, L-ascorbic acid tetralaurate, etc. Examples of hydroquinone derivatives include tetra-rubic acid fatty acid esters, 3-O-ethyl ascorbic acid, sodium L-ascorbic acid-2-phosphate-6-O-palmitate, glyceryl ascorbic acid or its acylated derivatives, ascorbic acid glycerin derivatives such as bisglyceryl ascorbic acid, aminopropyl L-ascorbic acid phosphate, hyaluronic acid derivatives of L-ascorbic acid, 3-OD lactose-L-ascorbic acid, isostearyl ascorbyl phosphate, etc., and as hydroquinone derivatives, arbutin (hydroquinone-β-D-glucopyrano Examples of tranexamic acid derivatives include α-arbutin (hydroquinone-α-D-glucopyranoside), 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, for example, 4-n-butylresorcinol, 4-isoamylresorcinol, and 2,5-dihydroxybenzoic acid derivatives include, for example, 2,Examples of nicotinic acid derivatives include 5-diacetoxybenzoic acid, 2-acetoxy-5-hydroxybenzoic acid, and 2-hydroxy-5-propionyloxybenzoic acid. Examples of nicotinic acid derivatives include nicotinamide and benzyl nicotinate. Examples of α-hydroxy acids include lactic acid, malic acid, succinic acid, citric acid, and α-hydroxyoctanoic acid.
[0032] Furthermore, the physiologically active ingredients include, for example, placenta extract, mulberry bark extract, saxifrage extract, perilla extract, rice bran extract or its hydrolysate, white mustard extract or its hydrolysate, white mustard ferment, peony extract or its hydrolysate, Japanese beautyberry extract, lotus seed extract or its hydrolysate, lotus seed ferment, Job's tears hydrolysate, Job's tears seed ferment, royal jelly ferment, sake lees extract or ceramide contained therein, chamomile extract, coral grass extract, rice leaf extract or its hydrolysate, eggplant (water eggplant, long eggplant, Kamo eggplant, rice) Eggplant extract or hydrolysate thereof, apricot fruit extract, seaweed extract such as kelp, sea lettuce or seaweed extract, marine flowering plant extract such as seagrass, soy milk ferment, jellyfish water, rice extract or hydrolysate thereof, rice fermentation extract, germinated rice extract or hydrolysate thereof, germinated rice ferment, black bean extract or hydrolysate thereof, brown sugar extract or ferment, damask rose flower extract, ylang-ylang flower extract, bamboo shoot peel extract, linoleic acid and its derivatives or processed products (e.g., liposomal linoleic acid), collagen and its derivatives derived from animals or fish Conductors, elastin and its derivatives, glycyrrhizic acid and its derivatives (such as dipotassium salt), t-cycloamino acid derivatives, vitamin A and its derivatives, allantoin, diisopropylamine dichloroacetate, γ-amino-β-hydroxybutyric acid, gentian extract, licorice extract, carrot extract, ginseng extract or fermented product thereof, camellia extract, red ginseng extract, loofah extract, peach extract, plum extract, peach kernel extract, kiwi extract, sunflower extract, Pau d'arco bark extract, daylily extract or fermented product, hibiscus flower extract These include extracts or fermented products, *Lysimachia japonica* extract, *Cherimoya* extract, *Mango* extract, *Mangosteen* extract, *Seaweed* extract, *Oolong tea* extract, *Benifuki* extract, *Bletilla striata* extract, *Sweet potato* extract, extract or hydrolysate of *Prunus serrulata* fruit peel or seed coat, *Safflower* extract, *Casablanca* extract, *Sweet potato* extract or its fermented product, *Guava* leaf extract, *Olive* leaf extract, *Horse chestnut* extract, *Ginger* extract, *Vanilla* extract, *Houttuynia cordata* extract, *Pomelo* extract, *Aloe* extract, *Aloe vera* extract, *Fig* flower extract, *Apple* extract, *White asparagus* extract, etc.
[0033] 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.
[0034] Manufacturing Example 1. Preparation of Jujube Extract (1) Dried jujube fruits were added to 2 kg of dried fruit and immersed at 40°C in 2 kg of purified water. This was filtered to obtain 18 kg of a brown, transparent jujube fruit extract (solid content 5.0%). To further enhance stability, the jujube fruit extract was concentrated using a styrene-divinylbenzene synthetic adsorbent. The resulting concentrate was then mixed with purified water and 1,3-butylene glycol, and insoluble matter was filtered to obtain a light brown, transparent jujube fruit extract. For the evaluation test described later, 5.0 kg of the light brown, transparent jujube fruit extract (solid content 1.1%) was used.
[0035] Manufacturing Example 2. Preparation of Jujube Extract (2) Instead of the preparation method in Production Example 1, the jujube fruit extract may be prepared by the following method. The fruit of the jujube tree (Ziziphus jujuba), a member of the Rhamnaceae family, was dried. 2 kg of the dried fruit was mixed with 20 kg of a 30% 1,3-butylene glycol aqueous solution and immersed at 40°C. After filtering, the mixture was diluted with purified water to obtain 5.0 kg of a pale brown, transparent jujube fruit extract (solid content concentration 1.1%).
[0036] In the present invention, the styrene-divinylbenzene-based synthetic adsorbent used in the concentration step of Production Example 1 may be replaced with other synthetic adsorbents, ion exchange resins, or activated carbon. Furthermore, in Production Example 1, the concentrated jujube fruit extract was mixed with purified water and 1,3-butylene glycol to obtain a light brown, transparent jujube fruit extract. However, instead of purified water and 1,3-butylene glycol, separately prepared jujube fruit extract and 1,3-butylene glycol may be used.
[0037] In this embodiment, we focused on HIF-1α (Biochemistry, Vol. 85, No. 3, pp. 187-195, 2013), which is involved in homeostatic mechanisms such as stem cell maintenance and inflammation control, and evaluated the effect of the active ingredient according to the present invention on promoting the transcriptional activity of HIF-1α.
[0038] Test Example 1. Evaluation of HIF-1α transcriptional activity (1) Sample preparation First, niacinamide was dissolved in purified water to prepare a final concentration of 2 mM, which was used in the following evaluation tests. A composition consisting of this niacinamide and the extract from Production Example 1 was used as Sample 1 of the present invention in the following evaluation tests. On the other hand, for comparison, Comparative Sample 1, consisting only of the extract from Production Example 1, and Comparative Sample 2, consisting only of niacinamide (final concentration 2 mM), were also prepared. (2) Evaluation Test Method Normal human epidermal cells were grown in Humedia-KG2 [Kurabo Corporation] containing a growth additive, resulting in 1 × 10⁶ cells. 5The solution was prepared at a concentration of cells / mL, and 100 μL was seeded into a 96-well microplate and cultured at 37°C under 5% CO2 and saturated steam. After 24 hours of culture, a firefly luciferase reporter vector incorporating the HIF-1α binding nucleotide sequence (HRE) and a vector incorporating sea urchin luciferase as an internal standard (Cignal HIF Pathway Reporter Assay Kit) [QIAGEN] were introduced into the cells using ViaFect transfection reagent (Promega). 24 hours later, the present invention sample 1, comparative sample 1, or comparative sample 2 were added to separate culture media to establish test group 1 and comparative test groups 1 and 2, respectively. The concentration of the extract from Production Example 1 in the present invention sample 1 and comparative sample 1 was adjusted to a final concentration of 2.0% of the total culture medium, and the concentration of niacinamide in the present invention sample 1 and comparative sample 2 was adjusted to a final concentration of 2 mM. Twenty-four hours after adding each sample, cell contents were extracted, and the luciferase activity of the cell extract was measured using a luciferase assay system (Promega) and a luminometer (Promega GloMax-Multi+ Detection System). The HIF-1α transcriptional activity per cell was calculated by dividing the measured value of firefly luciferase (HRE transcription amount) by the measured value of sea urchin luciferase (cell volume). Furthermore, the HIF-1α transcriptional activity of a control group (where only culture medium was added instead of the sample solution) was similarly tested and calculated. The HIF-1α transcriptional activity of sample 1 of the present invention and comparative samples 1 and 2 was calculated as a relative value with the control group's value set to 100.
[0039] This is shown in Figure 1 of Test Example 1. As shown in Figure 1, while comparative sample 1 (extract from production example 1 only) did not show any HIF-1α transcription activity promoting effect, the present invention sample 1 (combination of niacinamide and extract from production example 1) showed a significant HIF-1α transcription activity promoting effect compared to comparative sample 2 (niacinamide only). Therefore, it was confirmed that combining niacinamide and the extract from production example 1 produces a synergistic effect in promoting HIF-1α transcription activity.
[0040] HIF-1α is a factor involved in homeostatic mechanisms such as stem cell maintenance and inflammation control. It is suggested that activating the transcription of HIF-1α can improve dry skin, prevent and improve skin thinning, and enhance the skin's barrier function.
[0041] Prescription example 1. Lotion [Ingredients] Part Eucalyptus oil 0.2 Polyoxyethylene (5.5) cetyl alcohol 5.0 Tocopherol acetate 0.02 Dipotassium glycyrrhizinate 0.5 Monoammonium glycyrrhizinate 0.5 Stearyl glycyrrhetinate 0.05 Isopropylmethylphenol 0.1 Align In 0.1 D-Panthenyl alcohol 0.1 Salicylic acid 0.5 Urea 5.0 l-Menthol 0.9 dl-menthol 0.2 1,3-Butylene glycol 5.0 Sodium citrate 0.2 Methylparaben 0.1 Hinokitiol 0.003 Photosensor No. 201 0.002 Niacinamide 5.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0042] Prescription example 2. Lotion [Ingredients] Part Glyceryl caprylate 3.0 Polyglyceryl-10 laurate 3.0 Cetanol 2.0 Behenyl alcohol 2.0 Methylparaben 0.1 D-Panthenyl alcohol 0.1 Yeast hydrolyzate 2.0 Ascorbic acid 3.0 Glycyrrhizic acid 0.5 β-Glycyrrhetinic acid 0.05 Tocopherol nicotinate 0.1 Resorcinol 0.1 Zinc oxide 2.0 dl-camphor 0.5 Glycerin 2.0 1,3-Butylene glycol 5.0 Potassium hydroxide 0.5 Niacinamide 3.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0043] Prescription example 3. Emulsion [Ingredients] Part Liquid paraffin 6.0 Hexaran 4.0 Jojoba oil 1.0 Polyoxyethylene (20) sorbitan monostearate 1.0 Lipophilic glyceryl stearate 1.0 Soy lecithin 1.5 L-ascorbic acid-2-glucoside 2.0 Potassium hydroxide 0.5 Glycerin 3.0 1,3-Butylene glycol 2.0 Carboxymethylcellulose 0.3 Sodium hyaluronate 0.01 Niacinamide 5.0 Extract from Production Example 1 2.0 Fragrance (appropriate amount) Purified water, in an amount that makes the total volume 100 parts.
[0044] Prescription example 4. Emulsion An emulsion was prepared in the same manner as in Formula Example 3, except that 3.0 parts of arbutin were used instead of 2.0 parts of L-ascorbic acid-2-glucoside and 0.5 parts of potassium hydroxide in the components of Formula Example 3.
[0045] Prescription example 5. Emulsion An emulsion was obtained in the same manner as in Formula Example 3, except that 2.0 parts of tranexamic acid were used instead of 2.0 parts of L-ascorbic acid-2-glucoside and 0.5 parts of potassium hydroxide in the components of Formula Example 3.
[0046] Prescription example 6. Emulsion An emulsion was obtained in the same manner as in Formulation Example 3, except that the extract from Production Example 2 was used instead of 2.0 parts of the extract from Production Example 1 in Formulation Example 3.
[0047] Prescription example 7. Lotion [Ingredients] Part Ethanol 10.0 Glycerin 3.0 1,3-Butylene glycol 2.0 Methylparaben 0.2 Citric acid 0.1 Sodium citrate 0.3 Carboxyvinyl polymer 0.1 Xanthan gum 0.1 Niacinamide 1.0 Extract from Production Example 1 2.0 Eggplant extract 1.0 Fragrance (appropriate amount) Potassium hydroxide (appropriate amount) Purified water, in an amount that makes the total volume 100 parts.
[0048] Prescription Example 8: Essence [Ingredients] Part Ethanol 2.0 Glycerin 5.0 1,3-Butylene glycol 5.0 Methylparaben 0.1 Ceramide 1.0 Hyaluronic acid 0.1 Citric acid 0.3 Sodium citrate 0.6 Niacinamide 2.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0049] Prescription example 9. Cream [Ingredients] Part 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 0.3 Stearyl glycyrrhetinate 0.3 Ammonium glycyrrhizinate 0.3 Lactic acid fermented rice 2.0 Hydrogenated lecithin 0.5 Hydrogenated lysolecithin 0.5 Water-soluble collagen 1.0 Hydrolyzed collagen 1.0 Xanthan gum 1.0 Zinc oxide 0.5 dl-camphor 0.3 l-menthol 0.5 Niacinamide 5.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0050] Prescription Example 10: Serum [Ingredients] Part Ethanol 2.0 Glycerin 5.0 1,3-Butylene glycol 5.0 Methylparaben 0.1 Hyaluronic acid hydrolysate 1.0 Sodium hyaluronate salt 1.0 Kelp extract 1.0 Sea lettuce extract 1.0 Katamenkirinsai extract 1.0 Citric acid 0.3 Sodium citrate 0.6 Niacinamide 5.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0051] Prescription example 11. Pack Dipropylene glycol 5.0 Polyoxyethylene (60) hydrogenated castor oil 5.0 Cetanol 3.0 Behenyl alcohol 3.0 Allantoin 0.1 Dipotassium glycyrrhizinate 0.3 Ammonium glycyrrhizinate 0.3 β-Glycyrrhetinic acid 0.3 Stearyl glycyrrhetinate 0.3 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 Yeast hydrolyzate 3.0 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 Niacinamide 3.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0052] Prescription Example 12: Sheet Mask A sheet mask is obtained by impregnating a nonwoven fabric with the following ingredients. [Ingredients] Part Glycerin 3.0 1,3-Butylene glycol 2.0 L-ascorbic acid 2-glucoside 2.0 Methylparaben 0.2 Citric acid 0.1 Sodium citrate 0.3 Xanthan gum 1.0 Water-soluble collagen 1.0 Sodium hyaluronate 1.0 Niacinamide 3.0 Extract from Production Example 1 2.0 Potassium hydroxide (appropriate amount) Purified water, in an amount that makes the total volume 100 parts.
[0053] Prescription Example 13: Cleansing Cosmetics [Ingredients] Part 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 Job's tears seed fermented product 2.0 Isopropylmethyl alcohol 0.1 Allantoin 0.1 Sulfur 0.5 Glycyrrhizic acid 0.3 Dipotassium glycyrrhizinate 0.3 Monoammonium glycyrrhizinate 0.3 β-Glycyrrhetinic acid 0.1 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 Niacinamide 5.0 Extract of product 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0054] Prescription Example 14: Body Shampoo [Ingredients] Part N-Lauroyl Methylalanine Sodium 25.0 Potassium coconut oil fatty acid solution (40%) 26.0 Coconut oil fatty acid diethanolamide 3.0 Methylparaben 0.1 1,3-Butylene glycol 2.0 Niacinamide 2.0 Extract from Production Example 1: 5.0 Purified water, in an amount that makes the total volume 100 parts.
[0055] Prescription Example 15: Hair Shampoo [Ingredients] Part N-Coconut oil fatty acid methyl taurate sodium 10.0 Sodium polyoxyethylene(3) alkyl ether sulfate 20.0 Lauryldimethylaminoacetic acid betaine 10.0 Coconut oil fatty acid diethanolamide 4.0 Methylparaben 0.1 Citric acid 0.1 Niacinamide 4.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0056] Example 16. Hair Conditioner [Ingredients] Part Polyoxyethylene (10) hydrogenated castor oil 1.0 Distearyldimethylammonium chloride 1.5 Stearyltrimethylammonium chloride 2.0 Glyceryl 2-ethylhexanoate 1.0 Cetanol 3.2 Stearyl alcohol 1.0 Methylparaben 0.1 1,3-Butylene glycol 5.0 Niacinamide 3.0 Extract from Production Example 1 2.0 Purified water, in an amount that makes the total volume 100 parts.
[0057] Example 17. Liquid Foundation [Ingredients] Part Stearic acid 2.4 Propylene glycol monostearate 2.0 Cetostearyl alcohol 0.2 Liquid lanolin 2.0 Liquid paraffin 3.0 Isopropyl myristate 8.5 Propylparaben 0.05 Sodium carboxymethylcellulose 0.2 Bentonite 0.5 Propylene glycol 4.0 Triethanolamine 1.1 Methylparaben 0.1 Titanium dioxide 8.0 Talc 4.0 Niacinamide 1.0 Extract from Production Example 1 2.0 Appropriate amount of coloring pigment Purified water, in an amount that makes the total volume 100 parts.
Claims
1. An HIF-1α transcription activity enhancer comprising niacinamide and an extract of purified water from the fruit of the jujube tree (Ziziphus jujuba), a member of the Rhamnaceae family, or a mixed solvent of purified water and a polyhydric alcohol, as active ingredients.
2. A topical skin preparation for preventing or improving epidermal thinning, comprising the HIF-1α transcription activity promoter described in claim 1.
Citation Information
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