WO2020015726A1 - Utilisation d'extraits de nitraria tangutorum bobr. et des préparations externes pour la peau comprenant ceux-ci - Google Patents

Utilisation d'extraits de nitraria tangutorum bobr. et des préparations externes pour la peau comprenant ceux-ci Download PDF

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Publication number
WO2020015726A1
WO2020015726A1 PCT/CN2019/096712 CN2019096712W WO2020015726A1 WO 2020015726 A1 WO2020015726 A1 WO 2020015726A1 CN 2019096712 W CN2019096712 W CN 2019096712W WO 2020015726 A1 WO2020015726 A1 WO 2020015726A1
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WIPO (PCT)
Prior art keywords
extract
nitraria tangutorum
tangutorum bobr
external preparation
skin external
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PCT/CN2019/096712
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English (en)
Inventor
Hui Li
Morgan DOSSANTOS
Zhang Zhang
Dandan JIANG
You QIN
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Jala Group Inc.
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Publication of WO2020015726A1 publication Critical patent/WO2020015726A1/fr

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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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • 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
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782—Enzyme inhibitors; Enzyme antagonists
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/54—Improvements relating to the production of bulk chemicals using solvents, e.g. supercritical solvents or ionic liquids

Definitions

  • the present invention relates to a use of Nitraria tangutorum Bobr. extract and an skin external preparation comprising the same.
  • Skin is the largest organ of the human body, covering the whole body. It is mainly responsible for protecting the body, perspiration, feeling hot, cold, and pressure, and other functions, so that various tissues and organs in the body are protected from physical invasion, mechanical invasion, chemical invasion and pathogenic microorganisms invasion.
  • Endogenous aging is a natural aging process, which is caused by irresistible physiological factors with the increase of age. It belongs to the aging at the genetic level, which is characterized by the appearance of wrinkles and sagging of the skin. Exogenous aging is mainly caused by environmental factors such as ultraviolet radiation, high temperature, cold, environmental pollution, nutrient deficiencies, diseases and bad living habits.
  • UV radiation is the most important factor, so-called photoaging, which is characterized by the appearance of rough dry skin at the exposed parts, deepened wrinkles, irregular pigmentation, vasodilation, epidermal dyskeratosis, dermal elastic fiber degeneration and accumulation of degradation products, etc., which can theoretically be prevented and relieved.
  • Free radical aging theory states that excessive free radicals are an important cause of skin photoaging. Since the skin is exposed to the ultraviolet rays and other external environments, reactive oxygen species produced by ultraviolet rays and other external environment will produce various free radicals in the skin, causing damage to oxidative stress and eventually leading to the aging of the skin.
  • dermis aging is characterized by thinning of the thickness, reduced production of collagen and elastin, increased decomposition, and increased activity of catabolic enzymes.
  • the thickness of the dermis is reduced by 20-80%during aging, accompanied by a gradual degradation of tissues and functions.
  • Collagen is one of the most abundant proteins in the human body. Collagen provides the skin with toughness, elasticity and waterproof function, which is an important raw material for maintaining the shape and structure of the skin, tissues and organs, and also for repairing the damaged tissues.
  • the collagen is also the main component of the extracellular matrix.
  • the reduction in collagen production is an important feature of skin aging.
  • type I collagen COL I
  • type V collagen COL V
  • COL V is one of the most important collagens, a collagen that forms regulatory fibrils, localized with the papillary dermis and the matrix surrounding the basement membrane, and copolymerized with COL I.
  • BMP-1 (Bone Morphogenetic Protein-1) is a main protease in the assembly process of extracellular matrix molecules, and participates in this process.
  • the main function of BMP-1 is to cleave the peptide chain of some proteins in extracellular matrix (ECM) , and process and modify precursors of many biomolecules into biologically functional structural proteins and active enzymes, including many matrix molecules such as type I, type III, type V, type VII procollagen, lipoxygenase (LOX) , small leucine-rich proteoglycan (SLRP) and so on.
  • ECM extracellular matrix
  • LOX lipoxygenase
  • SLRP small leucine-rich proteoglycan
  • Collagen is a key indicator against skin aging, but the efficacy and mechanism claimed by most cosmetic products in the market are only about how to increase the collagen content (such as promoting production, replenishment, and protection) . Recent studies have shown that the three-dimensional conformation and structure of collagen also have a significant impact on skin gloss. For skin, collagen is the channel of light transmission, and light scattering mediated by collagen fibers plays an important role in the light transmission and penetration in the dermis.
  • the collagen content of the skin is high, the structure is normal and orderly arranged, the light will be directly projected into the skin, and the skin will be transparent and glossy; if the collagen content is low and the structure is abnormal and disorderly arranged, a diffuse reflection (the scattering effect of the collagen bundle) of the light path will be formed, which makes the skin look gray, yellow and dull surface.
  • Photoaging caused by UV exposure results in an increase in the activity of skin elastase.
  • Elastase is distributed in various tissues and cells.
  • Increase elastase activity can result in the hydrolysis of skin elastic fibers, thereby accelerating the decomposition of collagen and elastin in the dermis, causing the skin to lose its elasticity, and resulting in skin aging such as wrinkles.
  • the degree of pigmentation is also increased by the stimulation of UV exposure, which is caused by the synthesis of pigment from the melanocytes on the skin and transferred to surrounding keratinocytes.
  • the process of pigmentation is complex, which is mainly caused by biochemical reactions in melanocytes, tyrosine produces dopaquinone under the action of tyrosinase, which acts as a catalyst, and melanin is then formed through the reaction catalyzed by enzymes or non-enzymatic oxidation.
  • the key is the synthesis of melanin, which is controlled by tyrosinase.
  • Natural plant-derived extracts are increasingly used in the skin care field due to their long history of application and superior multi-functionality.
  • Nitraria tangutorum Bobr is a species in Nitraria genus belonging to Zygophyllaceae family, also known as ground jujube, sour fat, desert cherry, Tanggut Nitraria.
  • Nitraria tangutorum Bobr. is mainly distributed in northeast Shanxi, western Inner Mongolia, Ningxia, Gansu Hexi, Qinghai, Xinjiang and Cambodia, and grows in desert and semi-desert basins, river terraces, sand deposits in the pasmont plains, and clay fields with sand accumulation. Due to the long-term adaptation to the harsh habitat, Nitraria tangutorum Bobr.
  • Nitraria tangutorum Bobr has the biological characteristics of drought tolerance, high temperature resistance, salt and alkali resistance, barren tolerance, sand burial resistance and cold tolerance, and the strong resistance thereof is rare in nature. It has been traditionally stated that Nitraria tangutorum Bobr. has the functions of strengthening the spleen and stomach, helping digestion, soothing the nerves, relieving exterior syndromes, detoxifying, promoting lactation, and fattening the animals. Modern studies have shown that Nitraria tangutorum Bobr. seed oil has the functions of anti-oxidation, anti-fatigue, anti-radiation and protecting against liver damage, and total flavonoids of Nitraria tangutorum Bobr. has protective function against the vascular endothelial cell injury. Nitraria tangutorum Bobr.
  • seeds comprise 10%to 12%crude fat, wherein, the content of unsaturated fatty acids is as high as 95%, and the content of linoleic acid is the highest, generally at 65%to 70%relative content, which is one of the most notable characteristics of Nitraria tangutorum Bobr. seeds different from other seed oil.
  • the Nitraria tangutorum Bobr. seeds also comprise the substances such as VE, flavonoids, plant sterols, allantoin, etc.
  • the technical problem to be solved by the present invention is for overcoming the problem of the prior art in lacking an active ingredient which can be used to improve the anti-oxidative and anti-aging ability of the skin.
  • the present invention provides use of Nitraria tangutorum Bobr. extracts and skin external preparations comprising the same.
  • the present invention found that the Nitraria tangutorum Bobr. extracts have a clear mechanism of action, and is safe and reliable, and have anti-oxidative, whitening and anti-aging effects.
  • Nitraria tangutorum Bobr. extracts have an effect of scavenging free radical; 2) Nitraria tangutorum Bobr. extracts have an effect of inhibiting tyrosinase activity; 3) Nitraria tangutorum Bobr. extracts have effects of inhibiting elastase activity and increasing the expression of anti-aging protein in human fibroblasts, which can regulate the production of collagen in the dermis and is suitable for use in cosmetics having anti-aging effect.
  • the present invention solves the above technical problems through the following technical solutions:
  • the present invention provides a use of Nitraria tangutorum Bobr. extract for manufacturing of an agent selected from the group consisting of (one or more) an antioxidant, a melanin synthesis inhibitor, an elastic fiber hydrolysis inhibitor, and an anti-skin aging protein expression up-regulation agent.
  • the antioxidant can be a class of substances conventional known in the art, which can help capture and neutralize free radicals, such as a free radical scavenger.
  • the melanin synthesis inhibitor can be a conventional substance in the art that can inhibit the synthesis of melanin, such as a tyrosinase inhibitor.
  • the elastic fiber hydrolysis inhibitor can be a conventional substance in the art that can inhibit the hydrolysis of elastic fiber, such as an elastase inhibitor.
  • the hydrolysis of elastic fibers in the skin will accelerate the decomposition of collagen and elastin in the dermis, causing the skin to lose its elasticity, and resulting in skin aging such as wrinkles.
  • the anti-skin aging protein can be a conventional protein in the art which is related to skin aging, such as collagen and elastin.
  • the anti-skin aging protein expression up-regulation agent can be a conventional substance in the art, which can affect the expression of the protein related to skin aging and selected from the group consisting of BMP-1 (Bone Morphogenetic Protein-1) expression up-regulation agent, collagen I expression up-regulation agent, and collagen V expression up-regulation agent and so on.
  • the BMP-1 can process and modify type I, type III, type V and type VII procollagen to functionalize the collagen.
  • the concentration of the Nitraria tangutorum Bobr. extract in the antioxidant is preferably 0.025-0.075 mg/mL, more preferably 0.05 mg/mL.
  • the concentration of the Nitraria tangutorum Bobr. extract in the melanin synthesis inhibitor is preferably 0.25-0.75 mg/mL, more preferably 0.5 mg/mL.
  • the concentration of the Nitraria tangutorum Bobr. extract in the elastic fiber hydrolysis inhibitor is preferably 0.5-1.5 mg/mL, more preferably 1 mg/mL.
  • the concentration of the Nitraria tangutorum Bobr. extract in the anti-skin aging protein expression up-regulation agent is preferably 0.05-1 mg/mL, for example, 0.05 mg/mL or 1 mg/mL.
  • the concentration of the Nitraria tangutorum Bobr. extract in the anti-skin aging protein expression up-regulation agent is preferably 0.05 mg/mL.
  • the concentration of the Nitraria tangutorum Bobr. extract in the anti-skin aging protein expression up-regulation agent is preferably 1 mg/mL.
  • the antioxidant, the melanin synthesis inhibitor, the elastic fiber hydrolysis inhibitor, and the anti-skin aging protein expression up-regulation agent are suitable for use in cosmetics or skin care products.
  • the Nitraria tangutorum Bobr. extract can be prepared by a conventional method in the art, for example, by mixing the Nitraria tangutorum Bobr. with supercritical CO 2 , followed by extraction to obtain an extract solution.
  • the extraction part of the Nitraria tangutorum Bobr. can be any part of the Nitraria tangutorum Bobr. which can be used for medicine, preferably the Nitraria tangutorum Bobr. seeds.
  • the Nitraria tangutorum Bobr. seeds is the mature seeds of Nitraria tangutorum Bobr.
  • the Nitraria tangutorum Bobr. When the extraction part of the Nitraria tangutorum Bobr. is the Nitraria tangutorum Bobr. seeds, then the Nitraria tangutorum Bobr. extract is the Nitraria tangutorum Bobr. seeds extract.
  • the Nitraria tangutorum Bobr. is subjected to pretreatment, for example, pulverization; more preferably, after the pulverization, it is subjected to sieving, and the sieve mesh number can be 40 mesh.
  • the pressure of the extraction can be a conventional pressure in the art, for example, 30-40 MPa; preferably 35 MPa.
  • the temperature of the extraction can be a conventional temperature in the art, for example, 40-50 °C; preferably 45 °C.
  • the flow rate of the supercritical CO 2 can be a conventional flow rate in the art, for example, 20-30 kg/h; preferably 25 kg/h.
  • the duration of the extraction can be a duration in the art, for example, 2-3 hours; preferably 2.5 hours.
  • the extract solution can be subjected to purification treatment according to a conventional operation in the art, for example, the extract solution can be subjected to macroporous adsorption resin chromatography.
  • the type of the macroporous adsorption resin can be AB-8.
  • the eluent of the chromatography can be an aqueous ethanol solution, and the concentration of the aqueous ethanol solution is preferably 65 to 75%, more preferably 70%, and the percentage refers to volume percentage.
  • the volume of the eluent of the chromatography can be four-fold to six-fold of the column volume, for example, five-fold.
  • Decontamination treatment can also be carried out before the chromatography, such as elution with water, the elution volume of the water can be one-fold of the column volume; preferably, eluting with five-fold column volume of 25-35%aqueous ethanol solution after the elution with water, for example, eluting with a 30%aqueous ethanol solution, and the percentage refers to volume percentage.
  • the preparation method of the Nitraria tangutorum Bobr. extract comprises the following steps: mixing Nitraria tangutorum Bobr. with supercritical CO 2 , followed by extraction, and the pressure of the extraction is 30-40 MPa; the temperature of the extraction is 40-50 °C; the flow rate of the supercritical CO 2 is 20-30 kg/h; the duration of the extraction is 2-3 hours to obtain an extract solution; more preferably, the preparation method of the Nitraria tangutorum Bobr. extract comprises the following steps: mixing Nitraria tangutorum Bobr. with supercritical CO 2 , followed by extraction, and the pressure of the extraction is 35 MPa; the temperature of the extraction is 45 °C; the flow rate of the supercritical CO 2 is 25 kg/h; the duration of the extraction is 2.5 hours to obtain an extract solution.
  • the present invention also provides a use of the Nitraria tangutorum Bobr. extract as an antioxidant active ingredient, a whitening active ingredient and/or an anti-aging active ingredient in cosmetics or skin care products.
  • Nitraria tangutorum Bobr. extract is as defined above.
  • the present invention also provides a skin external preparation comprising 0.001-10%of the Nitraria tangutorum Bobr. extract, and the percentage refers to the weight percentage (g/100 mL) in the skin external preparation.
  • Nitraria tangutorum Bobr. extract is as defined above.
  • the content of the Nitraria tangutorum Bobr. extract is preferably 0.0025-0.15%, for example, 0.005%, 0.05%or 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
  • the content of the Nitraria tangutorum Bobr. extract is preferably 0.0025-0.0075%, more preferably 0.005%, and the percentage refers to the weight percentage in the skin external preparation.
  • the Nitraria tangutorum Bobr. extract is used as a melanin synthesis inhibitor in the skin external preparation, then the content of the Nitraria tangutorum Bobr. extract is preferably 0.025-0.075%, more preferably 0.05%, and the percentage refers to the weight percentage in the skin external preparation.
  • the Nitraria tangutorum Bobr. extract is used as a skin elastic fiber hydrolysis inhibitor in the skin external preparation, then the content of the Nitraria tangutorum Bobr. extract is preferably 0.05-0.15%, more preferably 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
  • the Nitraria tangutorum Bobr. extract is used as an anti-skin aging protein expression up-regulation agent in the skin external preparation, then the content of the Nitraria tangutorum Bobr. extract is preferably 0.005-0.1%, for example, 0.005%or 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
  • the anti-skin aging protein is BMP-1
  • the content of the Nitraria tangutorum Bobr. extract is preferably 0.005%, and the percentage refers to the weight percentage in the skin external preparation.
  • the anti-skin aging protein is collagen I or collagen V
  • the content of the Nitraria tangutorum Bobr. extract is preferably 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
  • the skin external preparation can further comprise other active ingredients, and the other active ingredients are preferably selected from the group consisting of moisturizing active ingredients, antioxidant active ingredients, oil control active ingredients, whitening active ingredients and anti-aging active ingredients.
  • the content of the other active ingredients is a conventional content in the art.
  • the skin external preparation can further comprise a medium or a matrix excipient which is conventionally used in the art, as long as the excipient is acceptable in the cosmetic or pharmaceutical field.
  • the content of the excipients is a conventional content in the art.
  • the excipient can be in form of an aqueous phase, an oil phase, a gel, a water-in-wax emulsion, an oil-in-water emulsion or a water-in-oil emulsion.
  • the skin external preparation of the present invention can further comprise any other components conventionally used in the cosmetic field selected from the group consisting of a preservative, spice, a hydrophilic active agent and a lipophilic active agent and so on.
  • the content of the other components as described above can be a conventional content in the art.
  • the skin external preparation can further comprise a particulate phase, and the particulate phase can be selected from the group consisting of a pigment, a pearling agent and a filler.
  • the form of the skin external preparation can be any suitable product form.
  • the product form includes, but is not limited to, an aerosol spray, a cream, an emulsion, a solid, a liquid, a dispersion, a foam, a gel, a lotion, a mousse, an ointment, a powder, a patch, a pomade, a hand-pumped spray, a stick, a mask, and a wet wipe, and also can be an essence and/or a cream.
  • the skin external preparation of the present invention can be a cosmetic, a dermatological or pharmaceutical topical application product, and the preparation method thereof can be a conventional preparation method in the art.
  • the skin external preparation is a toner, and the skin external preparation comprises the following components by weight: 4-6%of glycerin, 3-6%of polyol A, 0.5-1.5%of betaine, 0.25-1.0%of panthenol, 0.05-0.1%of dipotassium glycyrrhizinate, 0-2.0%of allantoin, 0.25-1.0%of polyethylene glycol-32, 0.15-0.2%of surfactant A, 0.4-0.45%of preservative A, 0-0.15%of xanthan gum, 0-0.03%of spice and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 3-6%of polyol A, 1%of betaine, 0.5%of panthenol, 0.05-0.1%of dipotassium glycyrrhizinate, 0.5%of polyethylene glycol-32, 0.15-0.2%of surfactant A, 0.4-0.45%of preservative A, 0-0.15%of xanthan gum, 0.03%of spices and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 3-6%of polyol A, 1%of betaine, 0.5%of panthenol, 0.05-0.1%of dipotassium glycyrrhizinate, 0.1-2.0%of allantoin, 0.5%of polyethylene glycol-32, 0.15-0.2 %of surfactant A, 0.4-0.45%of preservative A, 0-0.15%of xanthan gum, 0.03%of spice and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the polyol A is selected from the group consisting of butanediol, 1, 2-pentanediol and dipropylene glycol;
  • the surfactant A is polysorbate-20 and/or PEG-40 hydrogenated castor oil, and can also be hydroxyethyl cellulose; preferably the surfactant A is selected from the group consisting of hydroxyethyl cellulose, polysorbate-20 and PEG-40 hydrogenated castor oil;
  • the preservative A is methylparaben and/or phenoxyethanol, and can also be IS-45; preferably, the preservative A is selected from the group consisting of IS-45, methylparaben and phenoxyethanol.
  • the Nitraria tangutorum Bobr. extract is preferably the Nitraria tangutorum Bobr. seeds extract.
  • the content of the Nitraria tangutorum Bobr. seeds extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, for example, 0.005%, and the percentage refers to the weight percentage in the skin external preparation.
  • the preservative IS-45 is a preservative manufactured by Germall Co., US, which contains propylene glycol, diimidazolidinyl urea, methylparaben and iodopropynyl butylcarbamate.
  • the skin external preparation is an essence, and the skin external preparation comprises the following components by weight: 4-6%of glycerin, 3-6%of polyol B, 0.5-1.5%of panthenol, 0.05-0.1%of dipotassium glycyrrhizinate, 0.05-0.1%of allantoin, 0-4%of nicotinamide, 0.05-3.6%of surfactant B, 0.25-0.45%of preservative B, 0.2-0.4%of xanthan gum, 0.1-0.3%of acrylic resin Pemulen TR-2, 0-0.05%of spice and 0.001%-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 3-6%of polyol B, 1%of panthenol, 0.1%of dipotassium glycyrrhizinate, 0.1%of allantoin, 0.05-3.6%of surfactant B, 0.25-0.45%of preservative B, 0.2-0.4%of xanthan gum, 0.3%of acrylic resin Pemulen TR-2, 0.05%of spices and 0.001%-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 3-6%of polyol B, 1%of panthenol, 0.1%of dipotassium glycyrrhizinate, 0.1%of allantoin, 4%of nicotinamide, 0.05-3.6%of surfactant B, 0.25-0.45%of preservative B, 0.2-0.4%of xanthan gum, 0.3%of acrylic resin Pemulen TR-2, 0.05%of spice and 0.001%-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the polyol B is butanediol and/or 1, 3-propanediol;
  • the surfactant B is polyglyceryl-2 oleate and/or polyglyceryl-10 oleate, and can also be hydroxyethyl cellulose; preferably, the surfactant B is selected from the group consisting of hydroxyethyl cellulose, polyglyceryl-2 oleate and polyglyceryl-10 oleate;
  • the preservative B is selected from the group consisting of propyl paraben, methylparaben and phenoxyethanol.
  • the acrylic resin Pemulen TR-2 is an acrylic acid (acrylate) /C 10-30 alkanol acrylate cross-linked polymer manufactured by NOVOEAN Chemicals Co., US.
  • the xanthan gum is an extracellular microbial polysaccharide produced by the fermentation of sugars by Xanthomonas Campestris.
  • the Nitraria tangutorum Bobr. extract is preferably the Nitraria tangutorum Bobr. seeds extract.
  • the content of the Nitraria tangutorum Bobr. seeds extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, for example, 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
  • the skin external preparation is a lotion
  • the skin external preparation comprises the following components by weight: 4-6%of glycerin, 4-6%of 1, 3-propanediol, 0.5-1.5%of panthenol, 0.1-0.5%of tocopherol acetate, 0-0.1%of dipotassium glycyrrhizinate, 1-3%of polydimethylsiloxane, 1-2%of emulsifier A165, 2-3%of oil C, 2-4%of isopropyl isostearate, 0.1-0.5%of cetearyl alcohol, 0.1-0.3%of preservative C, 0.2-0.5%of xanthan gum and 0-0.1%of EDTA disodium;
  • the skin external preparation further comprises triethanolamine, and the triethanolamine is at such a content to adjust the pH of the skin external preparation to 5.5-7; and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 5%of 1, 3-propanediol, 1%of panthenol, 0.5%of tocopherol acetate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 2-3%of oil C, 3%of isopropyl isostearate, 0.5%of cetearyl alcohol, 0.3%of preservative C, 0.5%of xanthan gum and 0.1%of EDTA disodium; the skin external preparation further comprises triethanolamine, and the triethanolamine is at such a content to adjust the pH of the skin external preparation to 5.5-7; and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 5%of 1, 3-propanediol, 1%of panthenol, 0.5%of tocopherol acetate, 0.1%of dipotassium glycyrrhizinate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 2-3%of oil C, 3%of isopropyl isostearate, 0.5%of cetearyl alcohol, 0.3%of preservative C, 0.5%of xanthan gum and 0.1%of EDTA disodium; the skin external preparation further comprises triethanolamine, and the triethanolamine is at such a content to adjust the pH of the skin external preparation to 5.5-7; and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • oil C is mineral oil and/or isohexadecane; the preservative C is methylparaben and/or propyl paraben.
  • the emulsifier A165 is a commercial product comprising glyceryl stearate and PEG-100 stearate.
  • the Nitraria tangutorum Bobr. extract is preferably the Nitraria tangutorum Bobr. seeds extract.
  • the content of the Nitraria tangutorum Bobr. seeds extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, for example, 0.005%, and the percentage refers to the weight percentage in the skin external preparation.
  • the skin external preparation is a cream
  • the skin external preparation comprises the following components by weight: 4-6%of glycerin, 4-6%of 1, 3-propanediol, and 0.5-1.5%of panthenol, 0.1-0.5%of tocopherol acetate, 0-0.1%of dipotassium glycyrrhizinate, 1-3%of polydimethylsiloxane, 1-2%of emulsifier A165, 2-8%of oil D, 2-4%of isopropyl isostearate, 2-3%of cetearyl alcohol, 0.1-0.3%of preservative D, 1-2%of hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer and 0-0.1%of EDTA disodium;
  • the skin external preparation further comprises triethanolamine, and the triethanolamine is at such a content to adjust the pH of the skin external preparation to 5.5-7; and 0.001-10%of the Nitraria tang
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 5%of 1, 3-propanediol, and 1%of panthenol., 0.5%of tocopherol acetate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 2-8%of oil D, 3%of isopropyl isostearate, 2-3%of cetearyl alcohol, 0.3%of preservative D, 2%of hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer and 0.1%of EDTA disodium; the skin external preparation further comprises triethanolamine, and the triethanolamine is at such a content to adjust the pH of the skin external preparation to 5.5-7; and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • the skin external preparation comprises the following components by weight: 5%of glycerin, 5%of 1, 3-propanediol, and 1%of panthenol, 0.5%of tocopherol acetate, 0.1%of dipotassium glycyrrhizinate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 2-8%of oil D, 3%of isopropyl isostearate, 2-3%of cetearyl alcohol, 0.3%of preservative D, 2%of hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer and 0.1%of EDTA disodium; the skin external preparation further comprises triethanolamine, and the triethanolamine is at such a content to adjust the pH of the skin external preparation to 5.5-7; and 0.001-10%of the Nitraria tangutorum Bobr. extract; the rest of 100%is deionized water;
  • oil D is mineral oil and/or isohexadecane; the preservative D is methylparaben and/or propylparaben.
  • the Nitraria tangutorum Bobr. extract is preferably the Nitraria tangutorum Bobr. seeds extract.
  • the content of the Nitraria tangutorum Bobr. seeds extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, for example, 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
  • the emulsifier A165 is a commercial product comprising glyceryl stearate and PEG-100 stearate.
  • the hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer is a thickener of Sepinov TM EMT 10 manufactured by SEPPIC Co.
  • the reagents and raw materials used in the present invention are commercially available.
  • the present invention found that the Nitraria tangutorum Bobr. extract, especially the Nitraria tangutorum Bobr. seeds extract, has the effects of scavenging free radical activity, inhibiting tyrosinase activity, inhibiting elastase activity and up-regulating the anti-aging protein expression in human fibroblasts, regulating the production of collagen in the dermis, anti-aging, and especially the effect of free radical scavenging and inhibiting elastase activity.
  • the production rate of collagen I, collagen V and BMP1 in fibroblasts was 136%, 115%and 151%, respectively, which is of great significance for the development of anti-aging related skin care products or cosmetics.
  • the present invention firstly found that the Nitraria tangutorum Bobr. extract, especially the Nitraria tangutorum Bobr. seeds extract, can promote the production of bone morphogenetic protein-1 (BMP-1) , which is of great significance for the study of the mechanism of action of the Nitraria tangutorum Bobr. seeds extract and active ingredient acting on the BMP-1 target.
  • BMP-1 bone morphogenetic protein-1
  • Embodiment 1 Preparation of the Nitraria tangutorum Bobr. seeds extract
  • Dried Nitraria tangutorum Bobr. seeds was pulverized, passed through a 40-mesh sieve and loaded into a supercritical extraction machine, followed by extraction with supercritical CO 2 for 2.5 hours under the conditions, wherein, the amount of single feed was 300 g, the extraction pressure was 35 MPa, the extraction temperature was 45 °C, the CO 2 flow rate was 25 kg/h.
  • the Nitraria tangutorum Bobr. oil was collected from the separation kettle. The material was fed 5 times, and 1.5 kg of the raw materials were extracted to obtain 150 g of Nitraria tangutorum Bobr. oil. 10 g of Nitraria tangutorum Bobr.
  • a toner was prepared according to the following components and amounts, the percentage refers to the weight percentage of each component in the toner:
  • the skin external preparation of the present embodiment was prepared by a conventional toner preparation method in the art.
  • a toner was prepared according to the following components and amounts, the percentage refers to the weight percentage of each component in the toner:
  • the skin external preparation of the present embodiment was prepared by a conventional lotion preparation method in the art.
  • the skin external preparation of the present embodiment was prepared by a conventional essence preparation method in the art.
  • the skin external preparation of the present embodiment was prepared by a conventional essence preparation method conventional in the art.
  • a lotion was prepared according to the following components and amounts, wherein, the percentage refers to the weight percentage of each component in the lotion:
  • the skin external preparation of the present embodiment was prepared by a conventional lotion preparation method in the art.
  • a lotion was prepared according to the following components and amounts, wherein, the percentage refers to the weight percentage of each component in the lotion:
  • the skin external preparation of the present embodiment was prepared by a conventional lotion preparation method in the art.
  • a cream was prepared according to the following components and amounts, wherein, the percentage refers to the weight percentage of each component in the cream:
  • the skin external preparation of the present embodiment was prepared by a conventional cream preparation method in the art.
  • a cream was prepared according to the following components and amounts, wherein, the percentage refers to the weight percentage of each component in the cream:
  • the skin external preparation of the present embodiment was prepared by a conventional cream preparation method in the art.
  • 1, 1-Diphenyl-2-picrylhydrazyl is a stable nitrogen-centered organic free radical. Its ethanol solution is in dark-purple color and has a strong absorption at about 517 nm. When a free radical scavenger is present, the absorption of DPPH is weakened and gradually vanishes due to its single electron pairing. The fading degree of DPPH ethanol solution is quantitatively related to the number of electrons it receives. Therefore, spectrophotometer can be used for rapid quantitative analysis to detect the free radical scavenging effect, and to evaluate the free radical scavenging activity, antioxidant capacity and anti-aging ability of antioxidants.
  • DPPH ethanol solution 6 mg of DPPH was accurately weighed, dissolved with 95%ethanol and diluted to a 50 mL volumetric flask. The dissolution was assisted by ultrasound. When the solution was used, it was further diluted four-fold with 95%ethanol to obtain a DPPH ethanol solution having a concentration of 3 mg/100 mL (76 ⁇ M) , and stored in the dark (0 to 4 °C) .
  • Nitraria tangutorum Bobr. seeds extract prepared in Embodiment 1 and the ascorbic acid standard sample were dissolved in deionized water and diluted with deionized water to a suitable concentration for use.
  • T 0 Absorbance of the tested sample liquid plus an equal volume of 95%ethanol (sample solvent control group) ;
  • T Absorbance of the tested sample liquid plus an equal volume of DPPH solution (sample group) ;
  • the Nitraria tangutorum Bobr. seeds extract has DPPH free radicals scavenging activity. Compared with the blank control group, the free radical scavenging rate of the Nitraria tangutorum Bobr. seeds extract group was 88%.
  • the Nitraria tangutorum Bobr. seeds extract has an effect of inhibiting tyrosinase activity. Compared with the blank control group, the inhibition rate of tyrosinase of the Nitraria tangutorum Bobr. seeds extract group was 21%.
  • Embodiment 1 seeds extract prepared in Embodiment 1, and Elastatinal solution (both were diluted to a suitable concentration with deionized water) , wherein Elastatinal solution (elastic (protein) enzyme inhibitor, purchased from Sigma Co., Art. No. E0881) was used as a positive control group.
  • Elastatinal solution elastic (protein) enzyme inhibitor, purchased from Sigma Co., Art. No. E0881
  • the aqueous sample solution was replaced with deionized water as a reference solution, and the absorbance was also measured.
  • inhibition rate (%) (A 0 - (A 410 -B) ) /A 0 ⁇ 100%, where A 0 is the absorbance of the reference solution; A 410 is the absorbance of the sample solution; B is the absorbance of the blank sample solution.
  • the Nitraria tangutorum Bobr. seeds extract has an effect of inhibiting elastase activity. Compared with the blank control group, the inhibition rate of elastase of the Nitraria tangutorum Bobr. seeds extract group was 22%.
  • the human fibroblasts were seeded into a 96-well plate (5000 cells/well) , and the medium was removed after 72 hours of incubation, followed by addition of the solution prepared by the Nitraria tangutorum Bobr. seeds extract prepared in Embodiment 1 and the ascorbic acid standard solution (both were diluted to a suitable concentration with deionized water) , respectively. After incubation for further 48 hours, the supernatant was removed, and the content of COL I (collagen I) in the cells was determined by cell immunofluorescence, and the DNA content of the cell layer was determined (picogreen kit, purchased from thermo fisher) to normalized the COL I content data. The results would be compared to the untested control group, the production rate of type I accumulated collagen in the blank control group was 100%. A production rate greater than 100%exhibited a promoting effect.
  • the Nitraria tangutorum Bobr. seeds extract has an effect of promoting the secretion of collagen I.
  • the COL I production rate in human fibroblasts of the Nitraria tangutorum Bobr. seeds extract treatment group was 136%.
  • the human fibroblasts were seeded into a 96-well plate (5000 cells/well) , and the medium was removed after 72 hours of incubation, followed by addition of the solution prepared by the Nitraria tangutorum Bobr. seeds extract prepared in Embodiment 1 and the ascorbic acid standard solution (both were diluted to a suitable concentration with deionized water) , respectively. After incubation for further 48 hours, the supernatant was removed, and the content of COL V (collagen V) in the cells was determined by cell immunofluorescence, and the DNA content of the cell layer was determined (picogreen kit, purchased from thermo fisher) to normalize COL V content. The results would be compared to the untested control group, the production rate of type V accumulated collagen in the blank control group was 100%. A production rate greater than 100%exhibited a promoting effect.
  • the Nitraria tangutorum Bobr. seeds extract has an effect of promoting the secretion of collagen V.
  • the COL V production rate in human fibroblasts of the Nitraria tangutorum Bobr. seeds extract treatment group was up to 115%.
  • the human fibroblasts were seeded into a 96-well plate (5000 cells/well) , and the medium was removed after 72 hours of incubation, followed by addition of the solution prepared by the Nitraria tangutorum Bobr. seeds extract prepared in Embodiment 1 (diluted to a suitable concentration with deionized water) . After incubation for further 24 hours, the supernatant of the medium was collected, and the content of BMP-1 in the cells was determined by the BMP-1 ELISA kit, and the DNA content of the cell layer was determined (picogreen kit, purchased from thermo fisher) to normalize the BMP-1 content data. The results would be compared to the untested control group, the production rate of BMP1 in the blank control group was 100%. A production rate greater than 100%exhibited a promoting effect.
  • the Nitraria tangutorum Bobr. seeds extract has an effect of promoting the production of BMP-1.
  • the BMP-1 production rate in human fibroblasts of the Nitraria tangutorum Bobr. seeds extract treatment group was up to 151%.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Dermatology (AREA)
  • Microbiology (AREA)
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Abstract

L'invention concerne l'utilisation d'extraits de Nitraria tangutorum Bobr. et des préparations externes pour la peau comprenant ceux-ci Plus spécifiquement, l'invention concerne l'utilisation d'un extrait de Nitraria tangutorum Bobr. pour la préparation d'un agent choisi dans le groupe constitué d'un antioxydant, d'un inhibiteur de la synthèse de la mélanine, d'un inhibiteur d'hydrolyse de la fibre élastique, et d'un agent de régulation à la hausse de l'expression des protéines anti-vieillissement de la peau. L'extrait de Nitraria tangutorum Bobr., en particulier l'extrait de graines de Nitraria tangutorum Bobr., a pour effet de piéger l'activité des radicaux libres, d'inhiber l'activité de la tyrosinase, d'inhiber l'activité de l'élastase et de réguler à la hausse de l'expression des protéines anti-vieillissement dans les fibroblastes humains, qui peut réguler la production de collagène dans le derme et présente un effet anti-vieillissement.
PCT/CN2019/096712 2018-07-20 2019-07-19 Utilisation d'extraits de nitraria tangutorum bobr. et des préparations externes pour la peau comprenant ceux-ci WO2020015726A1 (fr)

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