WO2018186643A1 - Composition pour réduire les rides de la peau, hydrater la peau, améliorer l'élasticité de la peau, exfolier la peau, inhiber l'érythème ou réduire le photo-vieillissement de la peau, contenant de la cinchonine ou un sel de celle-ci en tant que principe actif - Google Patents

Composition pour réduire les rides de la peau, hydrater la peau, améliorer l'élasticité de la peau, exfolier la peau, inhiber l'érythème ou réduire le photo-vieillissement de la peau, contenant de la cinchonine ou un sel de celle-ci en tant que principe actif Download PDF

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WO2018186643A1
WO2018186643A1 PCT/KR2018/003866 KR2018003866W WO2018186643A1 WO 2018186643 A1 WO2018186643 A1 WO 2018186643A1 KR 2018003866 W KR2018003866 W KR 2018003866W WO 2018186643 A1 WO2018186643 A1 WO 2018186643A1
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skin
composition
cinchonine
improving
expression
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PCT/KR2018/003866
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Korean (ko)
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박태선
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연세대학교 산학협력단
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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
    • A61K8/30—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
    • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • 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
    • A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides 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
    • A61K8/64—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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • 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
    • 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
    • A61K8/9706—Algae
    • 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
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat

Definitions

  • the present invention relates to a cosmetic composition for improving skin wrinkles or enhancing elasticity comprising cinchonine or a cosmetically acceptable salt thereof as an active ingredient.
  • the skin is composed of three layers: epidermis, dermis and hypodermis.
  • the epidermis especially the stratum corneum, which is the outermost layer of the epidermis, acts as a skin barrier, inhibiting the loss of water and electrolytes from the skin.
  • the dermal layer plays a role in maintaining the elasticity of the skin and supporting the structure through collagen and elastin synthesis.
  • collagen and elastin are major proteins produced in fibroblasts and are involved in skin mechanical firmness, tissue cohesion and elasticity (Moskowit, RW et al, Role of collagen hydroiysate in bone and joint disease, Semin Arthritis Rheu, 30: 87, 2000).
  • Collagen forms various isoforms according to the form and structural features, and there are 28 kinds of collagen isotypes in human tissues. Among them, collagen is present in types 1, 3. 4. 6. 7. 13, 14, 17 and the like are known. Collagen types 1 and 3 make up the interstitial components of the dermal layer, and collagen type 7 is the major component of the dermal and epidermal junctions (Pei, M. et al., Expression of collagen type) I, II and III in loose body of osteoarthitis, J. Orthop. Sci., 5: 288, 2000).
  • Type I collagen is the largest amount of extracellular matrix protein in skin connective tissue, and other proteins such as elastin, fibronectin, integrin, fibrillin, and proteoglycan are present. do.
  • the newly synthesized procollagen is secreted into the extracellular space of skin cells through an enzymatic reaction to form a microfibril of triple helix configuration, and the microfibrils combine with leucine-rich small proteoglycans to form fibrils. As a result, these fibrils gather to form collagen fibers that provide skin binding and elasticity (Bateman, J.F. et al., Collagen superfamily.Extracellular matrix, Harwood, New York, 2, 22-26, 1996).
  • Skin aging is known to decrease collagen content, a protein that accounts for most of the collagen of skin dermis. Collagen decreases the skin's tension and strength. have.
  • Skin aging is largely divided into endogenous aging due to physiological aging and photoaging caused by continuous ultraviolet radiation (UV) exposure. Repeated ultraviolet exposure results in increased collagen degrading enzymes and causing denaturation and destruction of collagen fibers, reducing the elasticity of the skin and promoting the production of wrinkles.
  • ROS reactive oxygen species
  • increases continuously in skin tissues exposed to ultraviolet rays and the latter is a signaling system mediated by epidermal growth factor receptor (EGF-R), tumor necrosis factor (TNF) -receptor, etc. Schsenmaier, C.
  • MNK mitogen-activated protein kinase
  • MMPs ix metalloproteinases
  • skin elasticity is reduced and wrinkles are promoted (Kang, S. et al., Inflammation and extracellular matrix degradation mediated by activated transcription factors nuclear factor - ⁇ B and activator protein-l in Inflammatory acne lesions in vivo.Am J. Pathol., 166: 1691-1699, 2005).
  • AP-1 regulates the expression of numerous genes involved in cell growth and differentiation and strongly regulates the expression of some MMPs.
  • MMPs whose expression is regulated by AP-1, MMP-1 is known as collagenase 1, and is based on type 1 and 3 collagen.
  • the present invention is to provide a cosmetic composition for improving skin wrinkles or enhancing elasticity, including Cinchonine (Cinchonine) or a cosmetically acceptable salt thereof as an active ingredient.
  • the present invention provides a cosmetic composition for improving skin wrinkles or enhancing elasticity comprising cinchonine or a cosmetically acceptable salt thereof as an active ingredient.
  • the synonin is i) increased procollagen secretion, ii) decreased expression of matrix metalloproteinase (MMP) gene, iii) increased expression of collagen type alpha 1, ColI ⁇ 2 or Col3 ⁇ 1 or iv) elastin ( elastin) may increase the expression of the gene.
  • MMP matrix metalloproteinase
  • composition may further include at least one skin wrinkle improving component selected from the group consisting of vitamin C, retinoic acid, transforming growth factor (TGF), protein from animal placenta, betulinic acid and chlorella extract.
  • skin wrinkle improving component selected from the group consisting of vitamin C, retinoic acid, transforming growth factor (TGF), protein from animal placenta, betulinic acid and chlorella extract.
  • the present invention also provides a cosmetic composition for improving skin moisturizing, exfoliating, inhibiting erythema or improving skin photoaging, including cinchonine or a cosmetically acceptable salt thereof as an active ingredient.
  • the composition can inhibit thickening of the skin epidermal layer.
  • the composition can inhibit damage to the collagen fiber network of the skin epidermal-dermal bonds.
  • the present invention provides a health functional food composition for improving skin wrinkles or enhancing elasticity comprising Cinchonine or a food acceptable salt thereof as an active ingredient.
  • the present invention also provides a health functional food composition for improving skin moisturizing, exfoliating, inhibiting erythema or improving skin photoaging, including cinchonine or a food acceptable salt thereof as an active ingredient.
  • the present invention comprises the step of administering or taking a composition comprising Cinchonine (Cinchonine) or a salt thereof as an active ingredient to the subject to improve skin wrinkles, enhance elasticity, enhance skin moisturization, exfoliation, inhibit erythema or skin photoaging Provide ways to improve.
  • the present invention also provides a skin wrinkle improvement, elasticity enhancement, skin moisturization enhancement, exfoliation, erythema suppression or skin photoaging improvement of a composition comprising Cinchonine (Cinchonine) or a salt thereof as an active ingredient.
  • the present invention relates to a composition for improving skin wrinkles, enhancing elasticity, enhancing skin moisturizing, removing dead skin cells, inhibiting erythema or improving skin photoaging, including cinchonine or a salt thereof as an active ingredient, wherein the cinchonine is a fibroblast cell Promoting the secretion of procollagen in, it can increase the amount of activated collagen, increase the amount of collagen fibers in the dermal layer and inhibit the expression of MMPs genes that catalyze the breakdown of collagen, It can be used to improve skin wrinkles or to improve elasticity.
  • the cinconin increases the water content of the skin tissue and decreases the water evaporation amount, the skin moisturizing improvement effect, can suppress the erythema, can reduce the thickness of the thickened skin epidermal layer, exfoliation Or skin photoaging by ultraviolet rays etc. can be prevented.
  • Figure 1 shows the result of measuring the amount of procollagen secretion in human skin fibroblasts.
  • Figure 2 shows the results of measuring the weight gain and dietary intake of the mice ingested the experimental diet prepared according to Example 2, Comparative Examples 3 and 4.
  • Figure 3 shows the results of measuring the moisture content, elasticity and erythema index of the mouse skin tissue ingested experimental diet prepared according to Example 2, Comparative Examples 3 and 4.
  • Figure 4 is a photograph showing the back skin tissue of the mouse taking the experimental diet prepared in Example 2, Comparative Examples 3 and 4.
  • Figure 5 shows the results of measuring the degree of wrinkles of the skin tissue, such as the mouse taking the experimental diet prepared according to Example 2, Comparative Examples 3 and 4.
  • Figure 6 shows the results of measuring the skin thickness of the mouse taking the experimental diet prepared in Example 2, Comparative Examples 3 and 4.
  • Figure 7 shows the collagen fiber (collagen fiber) amount and morphological changes of mice fed the experimental diet prepared according to Example 2, Comparative Examples 3 and 4.
  • Figure 8 shows the expression changes of collagen and MMPs genes in the back tissue of hairless mice treated with Cinchonine according to the present invention.
  • Figure 9 shows the expression change of the elastin (Elastin) gene in the back tissue of the hairless mouse treated with Cinchonine according to the present invention.
  • the present inventors have found that by synonin promotes secretion of procollagen in dermal fibroblasts, increases the amount of collagen fibers in the dermal dermal layer, inhibits the expression of MMPs genes, promotes water content in skin tissues and inhibits water evaporation,
  • the present invention has been found to be effective in improving skin wrinkles, enhancing elasticity and enhancing skin moisturization, and reducing the erythema index and reducing the thickness of the thickened skin epidermal layer, thereby making it effective in inhibiting erythema and removing dead skin cells and improving skin photoaging.
  • skin improvement refers to maintaining or enhancing the capacity associated with wrinkles and elasticity of the skin.
  • Collagen (collagen) and elastic fiber elastin (collagen) in the dermal layer of the skin is the main protein that plays a role in the skin elasticity, collagen biosynthesis is affected by the internal and external skin.
  • the skin cells are reduced in cell activity due to natural aging, the collagen fibers are reduced, or the active oxygen generated by excessive irradiation of ultraviolet rays or stress as an external factor is the thiol group of the protein (thiol: -SH)
  • the enzyme activity or by increasing the expression of degradation enzymes, such as collagen, elastin, increase the wrinkles of the skin and decrease the elasticity, the skin aging progresses.
  • skin light aging refers to a physiological phenomenon in which the skin ages due to sun exposure (ultraviolet rays), and when exposed to the sun (ultraviolet rays) for a long period of time, deep wrinkles on the face and neck, and drying and The surface of the skin becomes rough or causes pigmentation such as spots and freckles.
  • the present invention provides a cosmetic composition for improving skin wrinkles or enhancing elasticity comprising cinchonine or a cosmetically acceptable salt thereof as an active ingredient.
  • the cinnacon is an alkaloid contained in a plant such as Cinchona, Cinona officinalis, Cinchona pubescens, Olive (Olea europaea), and Smilax china.
  • the structural formula is C 19 H 22 N 20
  • the molecular weight is 294.4 g / mol, it may be represented by the formula (1).
  • shinconin may include a sinconin hydrate, a sinconin derivative, and the like, and may also include a solvent compound or stereoisomer thereof.
  • the synonin is i) increased procollagen secretion, ii) decreased expression of matrix metalloproteinase (MMP) gene, iii) increased expression of collagen type alpha 1, ColI ⁇ 2 or Col3 ⁇ 1 or iv) elastin ( elastin) may increase the expression of the gene.
  • MMP matrix metalloproteinase
  • collagen a major protein constituting the skin
  • collagen is synthesized in the form of procollagen in fibroblasts present in the dermis and then secreted into the extracellular matrix.
  • the procollagen secreted into the extracellular matrix is present on the cell surface.
  • the C-terminus is decomposed by peptidase and converted into active collagen, the activated collagen content can be determined by measuring the C-peptide content.
  • the synonin may promote synthesis of procollagen in dermal fibroblasts, thereby increasing the amount of activated collagen.
  • MMPs matrix metalloproteinases
  • Nos. 1, 3 and 9 MMP types known to increase by UV rays
  • MMP types 1 and 3 MMP types known to increase by UV rays
  • MMP-1 the middle of the collagen fibers are cut and MMP-3 and MMP-9 serve to cut and cut the cut collagen fibers.
  • the cinconin according to the present invention can significantly inhibit the expression of the MMPs gene, thereby inhibiting the degradation of collagen fibers, and by increasing the synthesis of collagen protein in skin tissue, can inhibit wrinkle formation. .
  • the dermis of the skin is composed of collagen (collagen fiber) and elastin (elastic fiber).
  • the collagen fibers allow structural integration with skin tension formation, and elastin fibers can enhance skin elasticity by engaging in skin elasticity.
  • the syntholin according to the present invention promotes elastin expression, thereby exhibiting skin elasticity enhancing effect.
  • composition according to the present invention may further include at least one skin wrinkle improving component selected from the group consisting of vitamin C, retinoic acid, transforming growth factor (TGF), protein from animal placenta, betulinic acid and chlorella extract. It may be, but is preferably vitamin C, but is not limited thereto.
  • TGF transforming growth factor
  • the secretion of procollagen 20p% to when compared to the case of the single treatment with the neoconsin or vitamin C alone It can be seen that the 23p% increase, a significant synergistic effect was proved by Colby's formula.
  • Cinconin can effectively increase the amount of activated collagen as the secretion of procollagen increases in dermal fibroblasts compared to the case of using it alone.
  • the dose of cinconin is preferably included at a concentration of 0.1 ⁇ M to 1000 ⁇ M, but is not limited thereto.
  • the cinnaconin is less than the concentration range, the inhibition of MMPs gene expression catalyzing procollagen synthesis and collagen degradation is reduced, there is a problem that it is difficult to exert the effect of skin wrinkle improvement or elasticity enhancement, exceeding the concentration range If so, there may be toxicity concerns, including cytotoxicity.
  • the Cinconin according to the present invention promotes procollagen secretion, thereby increasing the amount of activated collagen, decreasing the expression of MMPs genes that catalyze collagen degradation, and increasing the expression of elastin genes. This can prevent or alleviate skin wrinkles and enhance skin elasticity.
  • the cosmetic composition of the present invention contains Cynconin as an active ingredient and with a dermatologically acceptable excipient, a basic cosmetic composition (washing agents such as cosmetics, creams, essences, cleansing foams and cleansing water, packs, body oils), color cosmetic compositions (Foundation, lipstick, mascara, makeup base), hair product composition (shampoo, rinse, hair conditioner, hair gel) and soap and the like.
  • a dermatologically acceptable excipient a basic cosmetic composition (washing agents such as cosmetics, creams, essences, cleansing foams and cleansing water, packs, body oils), color cosmetic compositions (Foundation, lipstick, mascara, makeup base), hair product composition (shampoo, rinse, hair conditioner, hair gel) and soap and the like.
  • the excipients include, but are not limited to, emollients, skin penetration enhancers, colorants, fragrances, emulsifiers, thickeners and solvents.
  • fragrances, pigments, fungicides, antioxidants, preservatives and moisturizing agents may be further included, and may include thickeners, inorganic salts, synthetic polymer materials and the like for the purpose of improving the properties.
  • it can be easily prepared by adding the above-mentioned sinconin to the normal face wash and the soap base.
  • the cream it may be prepared by adding cinnaconin or a salt thereof to a cream base of a general oil-in-water type (O / W).
  • synthetic or natural materials such as proteins, minerals, vitamins, etc.
  • for the purpose of improving physical properties such as flavors, chelating agents, pigments, antioxidants, and preservatives, may be added.
  • the content of cinconine contained in the cosmetic composition of the present invention is not limited thereto, but is preferably 0.001 to 10% by weight, more preferably 0.01 to 5% by weight based on the total weight of the composition. If the content is less than 0.001% by weight, the desired anti-aging or anti-wrinkle effect may not be expected, and if it is more than 10% by weight, there may be difficulties in safety or formulation preparation.
  • Health functional food composition for improving skin wrinkles or enhancing elasticity
  • the present invention provides a health functional food composition for improving skin wrinkles or enhancing elasticity, including cinchonine or a food acceptable salt thereof as an active ingredient. Specific details of the synonin are as described above.
  • the synonin when using the synonin as an additive of the health functional food, it may be added as it is or used with other foods or food ingredients, according to a conventional method It can be used properly.
  • the mixed amount of the active ingredient can be appropriately determined depending on the purpose of use, such as prevention, health or treatment.
  • Formulations of dietary supplements may be in the form of powders, granules, pills, tablets, capsules, as well as in the form of general foods or beverages.
  • the foodstuff which can add the said substance is a dairy product including meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum, ice cream, etc.
  • Various soups, beverages, teas, drinks, alcoholic beverages and vitamin complexes, etc. may include all foods in a conventional sense.
  • the ciconin in general, in the preparation of food or beverages, may be added in an amount of 15 parts by weight or less, preferably 10 parts by weight or less based on 100 parts by weight of the raw material.
  • the amount in the case of long-term intake for health and hygiene or for health control, the amount may be below the above range, and the present invention has no problem in terms of safety in terms of using fractions from natural products. The above amount can also be used.
  • the beverage in the health functional food according to the present invention may contain various flavors or natural carbohydrates, etc. as an additional ingredient, as in general drinks.
  • the above-mentioned natural carbohydrates may be monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose and polysaccharides such as dextrin and cyclodextrin, sugar alcohols such as xylitol, sorbitol and erythritol.
  • sweetening agent natural sweetening agents such as tautin and stevia extract, synthetic sweetening agents such as saccharin and aspartame, and the like can be used.
  • the ratio of the natural carbohydrate may be about 0.01 to 0.04 g, preferably about 0.02 to 0.03 g per 100 mL of the beverage according to the present invention.
  • the functional food for skin wrinkle improvement or elasticity enhancement is various nutrients, vitamins, electrolytes, flavors, coloring agents, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloid thickeners, pH adjusting agents. And stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated drinks.
  • the composition for improving sleep of the present invention may contain fruit flesh for the production of natural fruit juice, fruit juice beverage and vegetable beverage. These components can be used independently or in combination. The ratio of such additives is not limited, but is generally selected from the range of 0.01 to 0.1 parts by weight relative to 100 parts by weight of the health functional food of the present invention.
  • the present invention provides a cosmetic composition for improving skin moisturizing, exfoliating, inhibiting erythema or improving skin photoaging, including cinchonine or a cosmetically acceptable salt thereof as an active ingredient. Specific details of the synonin are as described above.
  • the composition may increase the water content of the skin tissue, reduce the amount of water evaporation, promote skin moisturization, and suppress the erythema by reducing the erythema index.
  • the composition may improve skin photoaging by inhibiting the thickening of the skin epidermal layer and inhibiting the damage of the collagen fiber network of the skin epidermal-dermal junction.
  • the thickening of the skin epidermal layer by ultraviolet irradiation means that the skin damage due to photoaging is large.
  • the skin thickness was significantly increased by ultraviolet irradiation, and by ingesting an experimental diet containing cinnamon to the ultraviolet irradiated mouse, It was confirmed that the thickness was significantly reduced. That is, the cinconin according to the present invention can improve skin photoaging by reducing the thickness of the epidermal layer thickened by ultraviolet irradiation.
  • the dose of cinconin is preferably included at a concentration of 0.1 ⁇ M to 1000 ⁇ M, but is not limited thereto.
  • the cinnamon is less than the above concentration range, it is possible to suppress the increase in water content of the skin tissue and increase the amount of water evaporation, it is not possible to effectively suppress the thickening of the skin epidermal layer, the skin moisturizing, exfoliation, suppressing erythema or improving skin photoaging There is a problem that is difficult to achieve the effect of, and if the concentration range is exceeded, there may be concerns of toxicity including cytotoxicity.
  • the Cinconin according to the present invention effectively maintains moisture in skin tissue, reduces the erythema index, prevents thickening of the skin epidermal layer, promotes skin moisturization and exfoliation, and promotes erythema. It can suppress and improve skin photoaging.
  • the present invention provides a health functional food composition for improving skin moisturizing, removing dead skin cells, inhibiting erythema or improving skin photoaging, including cinchonine or a food acceptable salt thereof as an active ingredient. Specific details of the synonin are as described above.
  • Normal human dermal fibroblasts (neonatal foreskin) were purchased from ATCC (Manassas, VA, USA), and the cells were purchased using fibroblast growth medium (Promo Cell, Heidelberg) at 37 ° C., 5% CO 2. Cultures in incubators were used for the experiment.
  • mice Five-week-old male albino hairless mice (Skh-1) were purchased from Orient Bio (Gyeonggi-do, Korea) and subjected to a one week period of solid feed. Experimental animals were divided into 4 groups and 5 animals were assigned to each group and used for the experiment. Feed and water were freely ingested during the breeding period, and the temperature was maintained at 22 ⁇ 1 °C and humidity at 60 ⁇ 5%, and the photoperiod and dark cycle were adjusted to 12 hours daily.
  • Human skin fibroblasts of Preparation Example 1 were dispensed at 1.0 ⁇ 10 6 cells / well into 12 well-plates and added at a concentration of 100 ⁇ M of cinnamonine (CN) and incubated in a CO 2 incubator for 24 hours. After removing the medium of each well, washed once with PBS and again put 1 ml of PBS was irradiated with ultraviolet B (UVB) at 20 mJ / cm 2 conditions. PBS of each well was replaced with medium again and cultured for 24 hours, and then the amount of procollagen secreted into the medium was measured using a procollagen type IC-peptide EIA kit (Takara Bio, Japan). The standard solution included in the collagen measurement kit was diluted by concentration, and the absorbance was measured at 450 nm to prepare a standard concentration curve and calculate the amount of collagen produced.
  • UVB ultraviolet B
  • Example 2 The same procedure as in Example 1 was conducted except that 100 ⁇ M of vitamin C was treated.
  • Example 2 The same procedure as in Example 1 was conducted except that 100 ⁇ M of cinconine and 100 ⁇ M of vitamin C were treated.
  • the control cells irradiated with ultraviolet rays (+ UVB), procollagen secretion was significantly reduced compared to the normal cells (-UVB), in the case of Example 1, the control cells irradiated only with ultraviolet rays ( + UVB) significantly increased the amount of collagen by 24%.
  • the amount of collagen was increased by 47% compared to the UV irradiation control cells (+ UVB), which is higher than the amount of collagen observed in Comparative Example 1 or Example 1.
  • the cinconine according to the present invention has a similar effect to vitamin C known to act to stabilize and promote collagen.
  • the cinconin may increase the amount of activated collagen by promoting the secretion of procollagen.
  • UVB ultraviolet B
  • Example 3-1) The same procedure as in Example 2 was carried out except that a tablet diet was prepared according to the composition of AIN-93 rodent diet.
  • UVB ultraviolet B
  • Example 2 The same procedure as in Example 2 was conducted except that the diet prepared by adding 0.2% vitamin C (Sigma-Aldrich) to the AIN-93 tablet diet was supplied.
  • 0.2% vitamin C Sigma-Aldrich
  • Skins of Examples 2, Comparative Examples 3-1, and 4 mice subjected to UV irradiation for 10 weeks were made of silicone rubber to measure the extent of wrinkle formation. Attach a disk with a circular hole having a diameter of 1 cm to the back of the mouse, mix the reagent for making a replica plate, thinly spread it on the back of the hairless mouse, dry it completely, and carefully remove the disk to copy the disk. was produced. Fabrication temperature of the replica plate was carried out at a constant temperature and humidity condition of 20 ⁇ 23 °C, humidity 45 ⁇ 50%, and a silicon rubber impression material (Epigem, Seoul, Korea) for producing a replica plate. Analysis of the simulated platen was performed using a computer image analyzer (Visioline VL650, CK electronic GmbH, Germany) for total wrinkle area, maximum wrinkle depth, mean depth and mean wrinkles. Four wrinkle indicator items such as mean length were analyzed.
  • Example 2 Comparative Examples 3 and 4
  • the skin thickness of the mouse hip was measured using a digital micro caliper (Marathon Watch Company Ltd, Ontario, Canada).
  • the caliper used for the measurement was able to measure up to 0.01 mm and the adjustment function to apply a constant force to the thickness was able to measure the thickness of the skin under the same force.
  • Example 2 The dorsal skin tissue of Example 2, Comparative Examples 3 and 4 mice was extracted and fixed in 10% formalin. Subsequently, Hematoxylin and eosin (H & E) staining was performed by a Korean CFC (Gyeonggi-do, Korea) and observed using an optical microscope (IX71, Olympus, JPN) and photographed using a digital camera (DP71, Olympus, JPN). Photographed.
  • Korean CFC Korean CFC (Gyeonggi-do, Korea) and observed using an optical microscope (IX71, Olympus, JPN) and photographed using a digital camera (DP71, Olympus, JPN). Photographed.
  • the tissues were pulverized by adding 1 ml of Trizol solution per 0.1 g of dorsal skin tissue of Examples 2, Comparative Examples 3 and 4, and then centrifuged at 4 ° C. and 12,000 ⁇ g for 10 minutes. The supernatant was transferred to a new tube and 200 ⁇ l of chloroform was added and vortexed. After repeating this process twice, the supernatant was transferred to a new tube and isoprophanol and supernatant were added at a 1: 1 ratio. After shaking vigorously 10 times, the mixture was left at room temperature for 15 minutes, centrifuged at 12,000 ⁇ g and 4 ° C.
  • RNA samples were dissolved using nuclease free water.
  • a UV / VIS spectrophotometer (Beckman coulter, DU730) was measured the concentration of RNA samples extracted at 260 nm and 280 nm wavelength, and the integrity of the RNA samples were confirmed by agarose gel electrophoresis.
  • CDNA was synthesized by reverse transcription using oligo dT primer and superscript reverse transcriptase (GIBCO BRL, Gaithersburg, MD, USA) on RNA samples extracted from the back skin tissue. PCR was performed using 5D and 3 'flanking sequences of the gene cDNA to be amplified and templated cDNA obtained by reverse transcription, the primer sequence used is shown in Table 2 below. 1 ⁇ l of the amplified PCR product was electrophoresed on 1% agarose gel to confirm DNA band.
  • Comparative Example 3-1) elastin expression was significantly decreased in comparison with Comparative Example 3-2) which was not irradiated with ultraviolet rays, and in Example 2, Comparative Example 3-1 Elastin expression was not only significantly increased, compared to Comparative Example 4, it was confirmed that shows an excellent effect. That is, the synonin may exhibit an effect of promoting skin elasticity through promoting elastin expression.
  • the above ingredients were mixed and filled in an airtight cloth to prepare a powder.
  • tablets were prepared by tableting according to a conventional method for producing tablets.
  • the above components are dissolved in purified water according to a conventional preparation method, dissolved in purified water, and then lemon juice is added in an appropriate amount. After adjusting to 100 mL in total, sterilized and filled in a brown bottle to prepare a liquid formulation.
  • Formulation example 6 Preparation of dietary supplements
  • Vitamin B6 0.5 mg
  • composition ratio of the above-mentioned vitamin and mineral mixtures is mixed with a component suitable for a health food in a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional health food manufacturing method.
  • the granules may be prepared and used for preparing a health food composition according to a conventional method.
  • Formulation example 7 Manufacture of health drinks
  • composition ratio is mixed with a component suitable for a favorite beverage in a preferred embodiment, the composition ratio may be arbitrarily modified according to regional and ethnic preferences such as demand hierarchy, demand country, and usage.
  • the compounding ratio is mixed with a component suitable for nutritional longevity in a preferred embodiment, the compounding ratio may be arbitrarily modified, and can be prepared according to a conventional manufacturing method in the cosmetic field.
  • the above blending ratio is mixed composition of a component suitable for a flexible softener in a preferred embodiment, but the blending ratio may be arbitrarily modified, it can be prepared according to the manufacturing method in the general cosmetic field.
  • the compounding ratio is mixed with a component suitable for nourishing cream in a preferred embodiment, the compounding ratio may be arbitrarily modified, and can be prepared according to a conventional manufacturing method in the cosmetic field.
  • the compounding ratio is mixed with a component suitable for a massage cream in a preferred embodiment, the compounding ratio may be arbitrarily modified, and can be prepared according to a manufacturing method in the general cosmetic field.
  • the compounding ratio is mixed with a component suitable for a pack in a preferred embodiment, the compounding ratio may be arbitrarily modified, and can be prepared according to a manufacturing method in the general cosmetic field.
  • the compounding ratio is mixed with a component suitable for a gel in a preferred embodiment, the compounding ratio may be arbitrarily modified, and can be prepared according to a conventional manufacturing method in the cosmetic field.
  • the blending ratio is a relatively suitable composition for the cosmetic composition in a preferred embodiment, but can be applied to cosmetics of various uses, including other color cosmetics, according to the efficacy that can be applied to a thin coating on the human body, that is, Ointment may be used for manufacturing, and the mixing ratio may be arbitrarily modified according to regional and ethnic preferences such as demand hierarchy, demand country, and usage.

Abstract

La présente invention concerne une composition cosmétique et une composition alimentaire fonctionnelle pour la santé pour réduire les rides de la peau, améliorer l'élasticité de la peau, favoriser l'hydratation de la peau, exfolier la peau, l'inhibition de l'érythème ou la réduction du photovieillissement de la peau, la composition cosmétique et la composition alimentaire fonctionnelle de santé contenant de la cinchonine ou un sel de celle-ci en tant que principe actif. Plus spécifiquement, la cinchonine, selon la présente invention, présente un effet d'augmentation de la quantité de sécrétion de procollagène, de promotion de la biosynthèse du collagène, de diminution de l'expression génique des MMP, d'augmentation de l'expression du gène de l'élastine, l'inhibition de l'érythème ou l'inhibition de l'hyperplasie épidermique, et est donc efficace dans la réduction des rides de la peau, l'amélioration de l'élasticité de la peau, la promotion de l'hydratation de la peau, l'exfoliation de la peau, l'inhibition de l'érythème ou la réduction du photo-vieillissement de la peau.
PCT/KR2018/003866 2017-04-03 2018-04-02 Composition pour réduire les rides de la peau, hydrater la peau, améliorer l'élasticité de la peau, exfolier la peau, inhiber l'érythème ou réduire le photo-vieillissement de la peau, contenant de la cinchonine ou un sel de celle-ci en tant que principe actif WO2018186643A1 (fr)

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KR1020170043172A KR101787319B1 (ko) 2017-04-03 2017-04-03 신코닌(Cinchonine) 또는 이의 염을 유효성분으로 함유하는 피부주름 개선, 보습, 탄력증진, 각질제거, 홍반억제 또는 피부광노화 개선용 조성물

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KR102557358B1 (ko) * 2021-09-03 2023-07-19 스노우화이트팩토리(주) 아네모시스 켈리포니카 추출물을 유효성분으로 포함하는 피부 탄력 및 주름개선용 조성물

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