WO2020015725A1 - Use of mirabilis jalapa l. extracts and skin external preparations comprising the same - Google Patents
Use of mirabilis jalapa l. extracts and skin external preparations comprising the same Download PDFInfo
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- WO2020015725A1 WO2020015725A1 PCT/CN2019/096711 CN2019096711W WO2020015725A1 WO 2020015725 A1 WO2020015725 A1 WO 2020015725A1 CN 2019096711 W CN2019096711 W CN 2019096711W WO 2020015725 A1 WO2020015725 A1 WO 2020015725A1
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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]
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- 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
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- 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
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- 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
Definitions
- the extraction part of the Mirabilis jalapa L. can be any part of the Mirabilis jalapa L. which can be used for medicine, which can be selected from the group consisting of the Mirabilis jalapa L. root, the Mirabilis jalapa L. leaf, the Mirabilis jalapa L. flower and the Mirabilis jalapa L. seed and so on, preferably the Mirabilis jalapa L. flower.
- the Mirabilis jalapa L. flower is generally harvested from Mirabilis jalapa L. during the flower-bud stage.
- the content of the Mirabilis jalapa L. 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 xanthan gum is an extracellular microbial polysaccharide produced by the fermentation of sugars by Xanthomonas Campestris.
- the skin external preparation of the present embodiment was prepared by a conventional cream preparation method in the art.
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- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Dermatology (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Mycology (AREA)
- Botany (AREA)
- Biotechnology (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Engineering & Computer Science (AREA)
- Cosmetics (AREA)
Abstract
Use of Mirabilis jalapa L. extracts and skin external preparations comprising the same. Specifically the use of Mirabilis jalapa L. extract for manufacturing an agent selected from the group consisting of an antioxidant, a melanin synthesis inhibitor, an elastic fiber hydrolysis inhibitor, and an anti-skin aging protein expression up-regulation agent. The Mirabilis jalapa L. extract, especially the Mirabilis jalapa L. flower 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, which can regulate the production of collagen in the dermis and has anti-aging effect.
Description
The present invention claims the priority of the CN201810804107. X, filed on July 20
th, 2018, the contents of which are incorporated herein by its entirety.
Field of invention
The present invention relates to a use of Mirabilis jalapa L. extract and a skin external preparation comprising the same.
Prior arts
With the continuous development and maturity of the skin care products market, more and more brands have emerged. Consumers expect the efficacy of skin care products. Therefore, the research level of the efficacy mechanism of the active ingredients in skin care products needs to be improved. With the deepening explanation of the efficacy mechanism, it is necessary to integrate the cutting-edge biotechnology. With the continuous development of cell biology technology, the discovery of skin biology is gradually deepened and more targets and regulatory mechanisms related to the functional structure of the skin have been found.
Skin is the largest organ of the human body, covering the whole body. It 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.
Skin aging can be divided into endogenous aging and exogenous aging. 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. Among them, ultraviolet 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 aging of the skin.
In general, 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. The most important collagen in the dermis is type I collagen (COL I) , of which type V collagen (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.
In the dermis, many proteins are first expressed in progenitor form and then converted to mature proteins by proteolysis processing to perform normal functions. 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 modifyprecursors 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. Collagen is functionalized by BMP-1, ensuring that collagen is processed and modified in a desirable manner during biosynthesis to form the correct protein conformation.
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. If 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.
Photoaging caused by UV exposure results in an increase in the activity of skin elastase. Elastase is distributed in various tissues and cells. Increased 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.
In addition, the degree of pigmentation is also increased by the stimulation of UV exposure, which is caused by the synthesis of pigment from melanocytes on the skin and transfer 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 catalysis of enzymes or non-enzymatic oxidation. The key is the synthesis of melanin, which is controlled by tyrosinase.
Therefore, the researches on how to improve the anti-aging ability of the skin is of great significance for delaying skin aging.
Natural plant-derived extracts are increasingly used in the skin care field due to their long history of application and superior multi-functionality.
Mirabilis jalapa L. is a species in Mirabilis L. genus belonging to Nyctaginaceae family, also known as marvel-of-peru, pink bean flower, beauty of the night, champion flower, wild clove. Mirabilis jalapa L. is native to the tropical America, and is cultivated in the northern parts to the southern parts of China, which is an ornamental species and sometimes wild. Its medicinal use is first found in the "Compendium of Materia Medica" . It is cold in nature and sweet in taste, and its roots, leaves, flowers and seeds can be used as medicine for heat stranguria, gonorrhea, edema, leukorrhea with reddish discharge, painful swelling of joint, carbuncle, etc., and the white powdered of the seeds can be used for facial naevus acne. It is reported by the research that the water extracts of the Mirabilis jalapa L. flower comprise substances such as amino acids, sugars, glycosides, organic acids, phenols, volatile oils, etc.; the alcohol extracts comprise the substances such as phenols, cardiac glycosides, lactones, coumarin, flavonoids, etc.; the petroleum ether extracts mainly comprise the substances such as saponins, etc.
Content of the present invention
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 Mirabilis jalapa L. extracts and skin external preparations comprising the same. The present invention found that the Mirabilis jalapa L. extracts have a clear mechanism of action, and is safe and reliable, and have anti-oxidative, whitening and anti-aging effects.
The inventors have found through extensive research that: 1) Mirabilis jalapa L. extracts have an effect of scavenging free radical; 2) Mirabilis jalapa L. extracts have an effect of inhibiting tyrosinase activity; 3) Mirabilis jalapa L. 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 Mirabilis jalapa L. 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.
In the present invention, 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.
In the present invention, the melanin synthesis inhibitor can be a conventional substance in the art that can inhibit the synthesis of melanin, such as a tyrosinase inhibitor.
In the present invention, 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. In general, the hydrolysis of elastic fibers in the skin will accelerates the decomposition of collagen and elastin in the dermis, causing the skin to lose its elasticity, and resulting in skin aging such as wrinkles.
In the present invention, the anti-skin aging protein can be a conventional protein in the art which is related to skin aging, such as collagen and elastin.
In the present invention, 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.
In the present invention, the BMP-1 can process and modify type I, type III, type V and type VII procollagen to functionalize the collagen.
In the present invention, the concentration of the Mirabilis jalapa L. extract in the antioxidant is preferably 0.025-0.075 mg/mL, more preferably 0.05 mg/mL.
In the present invention, the concentration of the Mirabilis jalapa L. extract in the melanin synthesis inhibitor is preferably 0.25-0.75 mg/mL, more preferably 0.5 mg/mL.
In the present invention, the concentration of the Mirabilis jalapa L. extract in the elastic fiber hydrolysis inhibitor is preferably 0.5-1.5 mg/mL, more preferably 1 mg/mL.
In the present invention, the concentration of the Mirabilis jalapa L. extract in the anti-skinaging protein expression up-regulation agent is preferably 0.05-1 mg/mL, for example, 0.05 mg/mL or 1 mg/mL.
When the anti-skin aging protein is BMP-1, then the concentration of the Mirabilis jalapa L. extract in the anti-skin aging protein expression up-regulation agent is preferably 0.05 mg/mL.
When the anti-skin aging protein is collagen I or collagen V, then the concentration of the Mirabilis jalapa L. extract in the anti-skin aging protein expression up-regulation agent is preferably 1 mg/mL.
In the present invention, 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.
In the present invention, the Mirabilis jalapa extract can be prepared by a conventional method in the art, for example, by mixing the Mirabilis jalapa L. with a solvent, followed by extraction to obtain an extract solution.
The extraction part of the Mirabilis jalapa L. can be any part of the Mirabilis jalapa L. which can be used for medicine, which can be selected from the group consisting of the Mirabilis jalapa L. root, the Mirabilis jalapa L. leaf, the Mirabilis jalapa L. flower and the Mirabilis jalapa L. seed and so on, preferably the Mirabilis jalapa L. flower. The Mirabilis jalapa L. flower is generally harvested from Mirabilis jalapa L. during the flower-bud stage.
When the extraction part of the Mirabilis jalapa L. is the Mirabilis jalapa L. flower, then the Mirabilis jalapa L. extract is the Mirabilis jalapa L. flower extract.
The solvent is a conventional extraction solvent in the art, preferably ethanol. The concentration of the ethanol can be a conventional concentration in the art, preferably an aqueous solution of 60 to 80%ethanol, for example 70%, and the percentage refers to volume percentage.
The ratio of the mass of Mirabilis jalapa L. to the volume of the solvent can be a conventional ratio in the art, for example, 1: (8-12) g/mL, preferably 1: 10 g/mL.
The extraction method can be a conventional extraction method in the art, for example, cold-soaking extraction and heat extraction in sequence.
The duration of the cold-soaking extraction can be a conventional duration in the art, for example, 12 hours.
The temperature of the heat extraction can be a conventional temperature in the art, for example, 50-70 ℃, preferably 60 ℃.
The duration of the heat extraction may be a conventional duration in the art, for example, 1-3 hours, preferably 2 hours.
The frequency of the heat extraction can be a conventional frequency in the art, for example, three times. Those skilled in the art know that when the frequency of the heat extraction is greater than one, the extracts should be combined.
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.
Preferably, the extract solution is dried and re-dissolved with water, and then 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 25 to 35%, more preferably 30%, and the percentage refers to volume percentage.
The volume of the eluent of the chromatography can be five-fold of the column volume.
Decontamination treatment can also be carried out before the chromatography, such as elution with water, the elution volume of the water is preferably one-fold of the column volume.
Preferably, the preparation method of the Mirabilis jalapa L. extract comprises the following steps: mixing Mirabilis jalapa L. with an aqueous ethanol solution, followed by cold-soaking extraction and heat extraction in sequence to give the extract solution, wherein the concentration of the aqueous ethanol solution is 60-80%; the percentage refers to volume percentage; the duration of the cold-soaking extraction is 12 hours; the temperature of the heat extraction is 50-70 ℃; the duration of the heat extraction is 1-3 hours.
The present invention also provides a use of the Mirabilis jalapa L. extract as an antioxidant active ingredient, a whitening active ingredient and/or an anti-aging active ingredient in cosmetics or skin care products.
The definition of the Mirabilis jalapa L. extract is as defined above.
The present invention also provides a skin external preparation comprising 0.001-10%of the Mirabilis jalapa L. extract, and the percentage refers to the weight percentage (g/100 mL) in the skin external preparation.
The definition of Mirabilis jalapa L. extract is as defined above.
The content of the Mirabilis jalapa L. 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.
When the Mirabilis jalapa L. extract is used as an antioxidant in the skin external preparation, then the content of the Mirabilis jalapa L. extract is preferably 0.0025-0.0075%, more preferably 0.005%, and the percentage refers to the weight percentage in the skin external preparation.
When the Mirabilis jalapa L. extract is used as a melanin synthesis inhibitor in the skin external preparation, then the content of the Mirabilis jalapa L. extract is preferably 0.025-0.075%, more preferably 0.05%, and the percentage refers to the weight percentage in the skin external preparation.
When the Mirabilis jalapa L. extract is used as a skin elastic fiber hydrolysis inhibitor in the skin external preparation, then the content of the Mirabilis jalapa L. extract is preferably 0.05-0.15%, more preferably 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
When the Mirabilis jalapa L. extract is used as an anti-skin aging protein expression up-regulation agent in the skin external preparation, then the content of the Mirabilis jalapa L. 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.
When the anti-skin aging protein is BMP-1, then the content of the Mirabilis jalapa L. extract is preferably 0.005%, and the percentage refers to the weight percentage in the skin external preparation.
When the anti-skin aging protein is collagen I or collagen V, then the content of the Mirabilis jalapa L. extract is preferably 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
In the present invention, the skin external preparation refers to a collective concept of all ingredients generally applied on the exterior skin, and can be, for example, a cosmetic or a medicine. The cosmetic can be a basic cosmetic, a facial makeup cosmetic, a body cosmetic, a head care product, etc., and the dosage form thereof is not particularly limited, and it can be properly selected depending on different purposes.
In the present invention, 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.
In terms of the common knowledge in the art, depending on the different dosage forms and purposes, 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 excipient 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 component 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 component as described above can be a conventional content in the art.
In the present invention, 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.
In the present invention, the form of the skin external preparation can be any suitable product form. The product form include, 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 can also be an essence and/or a cream. As is known to all, 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.
In a first preferred embodiment of the present invention, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 spice and 0.001-10%of the Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
wherein 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 Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract. The content of the Mirabilis jalapa L. flower 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.
In terms of the common knowledge in the art, the preservative IS-45 is a preservative manufactured by Germall Co., US, which contains propylene glycol, diimidazolidinyl urea, methylparaben and iodopropynyl butylcarbamate.
In a second preferred embodiment of the present invention, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 spice and 0.001%-10%of the Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
wherein 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 propylparaben, methylparaben and phenoxyethanol.
In terms of the common knowledge in the art, 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.
In terms of the common knowledge in the art, the xanthan gum is an extracellular microbial polysaccharide produced by the fermentation of sugars by Xanthomonas Campestris.
The Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract. The content of the Mirabilis jalapa L. flower 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.
In a third preferred embodiment of the present invention, the skin external preparation is an lotion, and 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
wherein the oil C is mineral oil and/or isohexadecane; the preservative C is methylparaben and/or propylparaben.
Wherein, the Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract. The content of the Mirabilis jalapa L. flower 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.
In a fourth preferred embodiment of the present invention, the skin external preparation is a cream, and 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
or, 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, 1-2%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 Mirabilis jalapa L. extract; the rest of 100%is deionized water;
wherein the oil D is mineral oil and/or isohexadecane; the preservative D is methylparaben and/or propylparaben.
The Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract. The content of the Mirabilis jalapa L. flower 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.
In terms of the common knowledge in the art, 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.
Without violating the common sense in the art, the above preferred conditions can be arbitrarily combined, then preferred embodiments of the present invention are obtained.
The reagents and raw materials used in the present invention are commercially available.
The positive and progressive effects of the present invention are that
(1) The present invention that the Mirabilis jalapa L. extract, especially the Mirabilis jalapa L. flower 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 up-regulating the anti-aging protein expression in human fibroblasts. Compared with the blank control group, the production rate of collagen I, collagen V and BMP-1 in fibroblasts was 133%, 125%and 150%, respectively, which is of great significance for the development of anti-aging related skin care products or cosmetics.
(2) The present invention firstly found that the Mirabilis jalapa L. extract, especially the Mirabilis jalapa L. flower 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 Mirabilis jalapa L. flower extract and active ingredients acting on the BMP-1 target.
Detailed description of the preferred embodiment
The following embodiments further illustrate the present invention, but the present invention is not limited thereto. The experimental methods in the following embodiments, of which conditions are not specified, are referred to the conventional methods and conditions, or the product specifications.
Embodiment 1: Preparation of the Mirabilis jalapa L. flower extract
100 g of dried Mirabilis jalapa L. flower was weighed and pulverized, followed by addition of 100 mL or 10-fold volume (1000 mL) of 70%ethanol, and cold-soaked for 12 hours until the material was fully moistened by the solvent. Afterwards, the mixture was heated at 60 ℃, and extracted for 2 hours, followed by filtration to collect the extract solution. The extraction was repeated 3 times. The three extract solution was combined and dried under reduced pressure in vacuum to obtain 15 g of crude extract. 1 g of the crude extract was weighed, dissolved in water, and then passed through a macroporous adsorption resin AB-8, eluted with one-fold column volume of water, and the water washing solution was discarded. Afterwards, it was eluted with five-fold column volume of 30%ethanol, and the eluent was concentrated to dryness to obtain 0.5 g of the Mirabilis jalapa L. flower extract as a dry powder.
Embodiment 2
A toner was prepared according to the following components and amounts, the percentage refers to the weight percentage of each component in the toner:
5%of glycerin, 3%of butanediol, 1%of betaine, 0.5%of panthenol, 0.1%of dipotassium glycyrrhizinate, 0.5%of polyethylene glycol-32, 0.15-0.2 %of hydroxyethyl cellulose, 0.4%of methylparaben, 0.15%of xanthan gum, 0.03%of spice and 0.005%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional toner preparation method in the art.
Embodiment 3
A toner was prepared according to the following components and amounts, the percentage refers to the weight percentage of each component in the toner:
5%of glycerin, 3%of butanediol, 1%of betaine, 0.5%of panthenol, 0.1%of dipotassium glycyrrhizinate, 2.0%of allantoin, 0.5%of polyethylene glycol-32, 0.15-0.2 %of hydroxyethyl cellulose, 0.4%of IS-45, 0.15%of xanthan gum, 0.03%of spice and 0.005%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional toner preparation method in the art.
Embodiment 4
An essence was prepared according to the following components and amounts, the percentage refers to the weight percentage of each component in the essence:
5%of glycerin, 3%of butanediol, 1%of panthenol, 0.1%of dipotassium glycyrrhizinate, 0.1%of allantoin, 0.05%of polyglyceryl-2 oleate, 0.15%of methylparaben, 0.3%of phenoxyethanol, 0.2%of xanthan gum, 0.3%of acrylic resin Pemulen TR-2, 0.05%of spice and 0.1%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional essence preparation method in the art.
Embodiment 5
An essence was prepared according to the following components and amounts, the percentage refers to the weight percentage of each component in the essence:
5%of glycerin, 3%of butanediol, 1%of panthenol, 0.1%of dipotassium glycyrrhizinate, 0.1%of allantoin, 4%of nicotinamide, 0.05%of hydroxyethyl cellulose, 0.15%of methylparaben, 0.3%of phenoxyethanol, 0.2%of xanthan gum, 0.3%of acrylic resin Pemulen TR-2, 0.05%of spice and 0.1%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional essence preparation method in the art.
Embodiment 6
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:
5%of glycerin, 5%of 1, 3-propanediol, 1%of panthenol, 0.5%of tocopheryl acetate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 3%of mineral oil, 3%of isopropyl isostearate, 0.5%of cetostearyl alcohol, 0.2%of methylparaben, 0.1%propylparaben, 0.5%of xanthan gum, 0.1%of EDTA disodium, the pH value of the lotion was adjusted to 5.5-7 with triethanolamine; 0.005%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional lotion preparation method in the art.
Embodiment 7
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:
5%of glycerin, 5%of 1, 3-propanediol, 1%of panthenol, 0.5%of tocopheryl acetate, 0.1%of dipotassium glycyrrhizinate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 3%of isopropyl isostearate, 3%of mineral oil, 0.5%of cetostearyl alcohol, 0.2%of methylparaben, 0.1%propylparaben, 0.5%of xanthan gum, 0.1%of EDTA disodium, the pH value of the lotion was adjusted to 5.5-7 with triethanolamine; 0.005%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional lotion preparation method in the art.
Embodiment 8
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:
5%of glycerin, 5%of 1, 3-propanediol, 1 %of panthenol, 0.5%of tocopheryl acetate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 3%of isopropyl isostearate, 2%of mineral oil, 2%of cetostearyl alcohol, 0.2%of methylparaben, 0.1%propylparaben, 2%of hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer, 0.1%of EDTA disodium, the pH value of the cream was adjusted to 5.5-7 with triethanolamine; 0.1%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional cream preparation method in the art.
Embodiment 9
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:
5%of glycerin, 5%of 1, 3-propanediol, 1 %of panthenol, 0.5%of tocopheryl acetate, 0.1%of dipotassium glycyrrhizinate, 2%of polydimethylsiloxane, 2%of emulsifier A165, 3%of isopropyl isostearate, 2%of mineral oil, 2%of cetostearyl alcohol, 0.2%of methylparaben, 0.1%propylparaben, 2%of hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer, 0.1%of EDTA disodium, the pH value of the cream was adjusted to 5.5-7 with triethanolamine; 0.1%of the Mirabilis jalapa L. flower extract in Embodiment 1; the rest of 100%is deionized water.
The skin external preparation of the present embodiment was prepared by a conventional cream preparation method in the art.
Effect Embodiment 1: Efficacy determination of the Mirabilis jalapa L. flower extract
(1) Determination of free radical scavenging activity by DPPH method
1, 1-Diphenyl-2-picrylhydrazyl (DPPH) 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.
Preparation of 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 μM) , and stored in the dark (0 to 4 ℃) .
Pretreatment of the tested sample: The Mirabilis jalapa L. flower 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.
Experimental procedure: 2 mL of the tested sample solution was added into the test tube, followed by addition of 2 mL of DPPH ethanol solution, and evenly mixed. The reaction was carried out in the dark at room temperature for 30 minutes, and the absorbance Abs was measured at 525 nm. In addition to the sample group, a sample solvent control group, a blank control group and a solvent control group (the solvent of DPPH) and the ascorbic acid group as the positive control group were set, respectively.
Scavenging rate I (%) = [1- (T-T
0) / (C-C
0) ] ×100%
wherein,
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) ;
C
0: Absorbance of the distilled water plus an equal volume of 95%ethanol (solvent control group) ;
C: Absorbance of the distilled water plus an equal volume of DPPH solution (blank control group) .
Table 1: Results of the free radical scavenging activity
As shown in Table 1, the Mirabilis jalapa L. flower extract has DPPH free radicals scavenging activity. Compared with the blank control group, the free radical scavenging rate of the Mirabilis jalapa L. flower extract group was 76%.
(2) Determination of the inhibition rate of tyrosinase activity
Experimental procedure: 70 μL of phosphate buffer solution (pH 6.8, 30 mM) , 80 μL of 1.66 mM tyrosine solution, and 80 μL of sample solution were added to a 96-well plate, evenly mixed, and incubated in an incubator at 37 ℃ for 5 minutes or more, followed by addition of 10 μL of tyrosinase solution (125 U/mL) (purchased from Sigma, Art. No. T3824) . After incubating at 37 ℃ for 10 minutes, the absorbance A
475 at 475 nm wavelength was measured with a microplate reader. The sample solutions included the solution prepared by the Mirabilis jalapa L. flower extract prepared in Embodiment 1, and the arbutin standard solution (both were diluted to a suitable concentration with deionized water) , wherein the arbutin standard solution was used as a positive control group. The aqueous sample solution was replaced with deionized water as a reference solution, and the absorbance was also measured. The inhibition rate of tyrosinase activity was calculated by: inhibition rate (%) = (A
0- (A
475-B) ) /A
0 × 100%, where A0 is the absorbance of the reference solution; A
475 is the absorbance of the sample solution; B is the absorbance of the blank sample solution.
Table 2: Results of the inhibition rate of tyrosinase activity
As shown in Table 2, the Mirabilis jalapa L. flower extract has an effect of inhibiting tyrosinase activity. Compared with the blank control group, the inhibition rate of tyrosinase of the Mirabilis jalapa L. flower extract group was 44%.
(3) Determination of the inhibition rate of elastase activity
Experimental procedure: 10 μL of sample solution and 130 μL of 0.1 M Tris-HCl buffer solution (pH 8.0) containing 1.015 mM of the reaction substrate Succ-Ala-Ala-Ala-p-nitroanilide were added to a 96-well plate, and incubated at 25 ℃ for 5 minutes, followed by addition of 15 μL of elastase solution (0.5 U/mL) . After incubating at 25 ℃ for further 30 minutes, the absorbance A
410 at 410 nm wavelength was measured with a microplate reader. The sample solutions included the solution prepared by the Mirabilis jalapa L. flower 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. The aqueous sample solution was replaced with deionized water as a reference solution, and the absorbance was also measured.
The inhibition rate of elastase activity was calculated by: 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.
Table 3: Results of the inhibition rate of elastase activity
As shown in Table 3, the Mirabilis jalapa L. flower extract has an effect of inhibiting elastase activity. Compared with the blank control group, the inhibition rate of elastase of the Mirabilis jalapa L. flower extract group was 26%.
(4) Determination of collagen I production rate in fibroblasts
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 Mirabilis jalapa L. flower 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 normalize 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.
Table 4: Results of COL I content
As shown in Table 4, the Mirabilis jalapa L. flower extract has an effect of promoting the secretion of collagen I. Compared with the blank control group, the COL I production rate in human fibroblasts of the Mirabilis jalapa L. flower extract treatment group was 133%.
(5) Determination of collagen V production rate in fibroblasts
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 Mirabilis jalapa L. flower 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 the 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.
Table 5: Results of COL V content
As shown in Table 5, the Mirabilis jalapa L. flower extract has an effect of promoting the secretion of collagen V. Compared with the blank control group, the COL V production rate in human fibroblasts of the Mirabilis jalapa L. flower extract treatment group was up to 125%.
(6) Determination of BMP-1 production rate in fibroblasts
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 Mirabilis jalapa L. flower 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 BMP-1 in the blank control group was 100%. A production rate greater than 100%exhibited a promoting effect.
Table 6: Results of BMP-1 content
As shown in Table 6, the Mirabilis jalapa L. flower extract has an effect of promoting the production of BMP-1. Compared with the blank control group, the BMP-1 production rate in human fibroblasts of the Mirabilis jalapa L. flower extract treatment group was up to 150%.
Claims (10)
- A use of Mirabilis jalapa L. extract for manufacturing of an agent selected from the group consisting of an antioxidant, a melanin synthesis inhibitor, an elastic fiber hydrolysis inhibitor, and an anti-skin aging protein expression up-regulation agent.
- The use of claim 1, wherein, the antioxidant is a free radical scavenger;and/or, the melanin synthesis inhibitor is a tyrosinase inhibitor;and/or, the elastic fiber hydrolysis inhibitor is an elastase inhibitor;and/or, the anti-skin aging protein expression up-regulation agent is selected from the group consisting of BMP-1 expression up-regulation agent, collagen I expression up-regulation agent, and collagen V expression up-regulation agent.
- The use of claim 1 or 2, wherein,when the Mirabilis jalapa L. extract is used for manufacturing the antioxidant, then the concentration of the Mirabilis jalapa L. extract in the antioxidant is 0.025-0.075 mg/mL, preferably 0.05 mg/mL;when the Mirabilis jalapa L. extract is used for manufacturing the melanin synthesis inhibitor, then the concentration of the Mirabilis jalapa L. extract in the melanin synthesis inhibitor is 0.25-0.75 mg/mL, preferably 0.5 mg/mL;when the Mirabilis jalapa L. extract is used for p manufacturing the elastic fiber hydrolysis inhibitor, then the concentration of the Mirabilis jalapa L. extract in the elastic fiber hydrolysis inhibitor is 0.5-1.5 mg/mL, preferably 1 mg/mL;when the Mirabilis jalapa L. extract is used for manufacturing the anti-skin aging protein expression up-regulation agent, then the concentration of the Mirabilis jalapa L. extract in the anti-skin aging protein expression up-regulation agent is 0.05-1 mg/mL; preferably, when the anti-skin aging protein is BMP-1, then the concentration of the Mirabilis jalapa L. extract in the anti-skin aging protein expression up-regulation agent is 0.05 mg/mL; when the anti-skin aging protein is collagen I or collagen V, then the concentration of the Mirabilis jalapa L. extract in the anti-skin aging protein expression up-regulation agent is 1 mg/mL.
- The use of at least one of claims 1-3, wherein, the preparation method of the Mirabilis jalapa L. extract comprises the following steps: mixing the Mirabilis jalapa L. with a solvent, followed by extraction to obtain an extract solution.
- The use of claim 4, wherein, the extraction part of the Mirabilis jalapa L. is the Mirabilis jalapa L. flower;and/or, the solvent is an aqueous solution of 60 to 80%ethanol, and the percentage refers to volume percentage;and/or, the ratio of the mass of Mirabilis jalapa L. to the volume of the solvent is 1: (8-12) g/mL; preferably 1: 10 g/mL;and/or, the extraction method is cold-soaking extraction and heat extraction in sequence; the duration of the cold-soaking extraction is preferably 12 hours; the temperature of the heat extraction is preferably 50-70 ℃, more preferably 60 ℃; the duration of the heat extraction is preferably 1-3 hours, more preferably 2 hours; the frequency of the heat extraction is preferably three times;and/or, the extract solution is subjected to purification treatment; preferably, the extract solution is subjected to macroporous adsorption resin chromatography; more preferably, the extract solution is dried and re-dissolved with water, and then subjected to macroporous adsorption resin chromatography; the type of the macroporous adsorption resin is preferably AB-8; the eluent of the chromatography is preferably an aqueous ethanol solution, and the concentration of the aqueous ethanol solution is preferably 25 to 35%, more preferably 30%, and the percentage refers to volume percentage; the volume of the eluent of the chromatography is preferably five-fold of the column volume; decontamination treatment is preferably carried out before the chromatography, more preferably, elution with water, and the elution volume of the water is preferably one-fold of the column volume.
- A skin external preparation comprising 0.001-10%of the Mirabilis jalapa L. extract, and the percentage refers to the weight percentage in the skin external preparation;preferably, the preparation method of the Mirabilis jalapa L. extract comprises the following steps: mixing the Mirabilis jalapa L. with a solvent, followed by extraction to obtain an extract solution.
- The skin external preparation of claim 6, wherein, the extraction part of the Mirabilis jalapa L. is the Mirabilis jalapa L. flower;and/or, the solvent is an aqueous solution of 60 to 80%ethanol, and the percentage refers to volume percentage;and/or, the ratio of the mass of Mirabilis jalapa L. to the volume of the solvent is 1: (8-12) g/mL; preferably 1: 10 g/mL;and/or, the extraction method is cold-soaking extraction and heat extraction in sequence; the duration of the cold-soaking extraction is preferably 12 hours; the temperature of the heat extraction is preferably 50-70 ℃, more preferably 60 ℃; the duration of the heat extraction is preferably 1-3 hours, more preferably 2 hours; the frequency of the heat extraction is preferably three times;and/or, the extract solution is subjected to purification treatment; preferably, the extract solution is subjected to macroporous adsorption resin chromatography; more preferably, the extract solution is dried and re-dissolved with water, and then subjected to macroporous adsorption resin chromatography; the type of the macroporous adsorption resin is preferably AB-8; the eluent of the chromatography is preferably an aqueous ethanol solution, and the concentration of the aqueous ethanol solution is preferably 25 to 35%, more preferably 30%, and the percentage refers to volume percentage; the volume of the eluent of the chromatography is preferably five-fold of the column volume; decontamination treatment is preferably carried out before the chromatography, more preferably, elution with water, and the elution volume of the water is preferably one-fold of the column volume.
- The skin external preparation of claim 6 or 7, wherein,the content of the Mirabilis jalapa L. extract is 0.0025-0.15%, preferably, 0.005%, 0.05%or 0.1%, and the percentage refers to the weight percentage in the skin external preparation;when the Mirabilis jalapa L. extract is used as an antioxidant, then the content of the Mirabilis jalapa L. extract is preferably 0.0025-0.0075%, more preferably 0.005%, and the percentage refers to the weight percentage in the skin external preparation;when the Mirabilis jalapa L. extract is used as a melanin synthesis inhibitor, then the content of the Mirabilis jalapa L. extract is preferably 0.025-0.075%, more preferably 0.05%, and the percentage refers to the weight percentage in the skin external preparation;when the Mirabilis jalapa L. extract is used as an elastic fiber hydrolysis inhibitor, then the content of the Mirabilis jalapa L. extract is preferably 0.05-0.15%, more preferably 0.1%, and the percentage refers to the weight percentage in the skin external preparation;when the Mirabilis jalapa L. extract is used as an anti-skin aging protein expression up-regulation agent, then the content of the Mirabilis jalapa L. extract is preferably 0.005-0.1%; more preferably, 0.005%or 0.01%, and the percentage refers to the weight percentage in the skin external preparation; more preferably, when the anti-skin aging protein is BMP-1, then the content of the Mirabilis jalapa L. extract is 0.005%, and the percentage refers to the weight percentage in the skin external preparation; when the anti-skin-aging protein is collagen I or collagen V, then the content of the Mirabilis jalapa L. extract is 0.1%, and the percentage refers to the weight percentage in the skin external preparation.
- The skin external preparation of at least one of claims 6-8, wherein, the skin external preparation further comprises 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.and/or, the skin external preparation further comprises a medium or a matrix excipient, the excipient is preferably 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;and/or, the skin external preparation further comprises other components selected from the group consisting of a preservative, spice, a hydrophilic active agent and a lipophilic active agent.and/or, the skin external preparation further comprises a particulate phase, and the particulate phase is preferably selected from the group consisting of a pigment, a pearling agent and a filler.
- The skin external preparation of at least one of claims 6-9, wherein,the form of the skin external preparation is selected from the group consisting of an aerosol spray, a cream, an emulsion, a solid, a liquid, a dispersion, a foam, a gel, a lotion, an essence, a mousse, an ointment, a powder, a patch, a pomade, a hand-pumped spray, a stick, a mask, and a wet wipe;when the skin external preparation is a toner, and the skin external preparation preferably comprises the following components by weight: (1) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; or (2) 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 spice and 0.001-10%of the Mirabilis jalapa L. extract; the rest of 100%is deionized water; or, (3) 5%of glycerin, 3-6%of polyol A, 1%of betaine, 0.5%of panthenol, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; wherein the polyol A is selected from the group consisting of butanediol, 1, 2-pentanediol and dipropylene glycol; the surfactant A is selected from the group consisting of hydroxyethyl cellulose, polysorbate-20 and PEG-40 hydrogenated castor oil; the preservative A is selected from the group consisting of IS-45, methylparaben and phenoxyethanol, the Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract; the content of the Mirabilis jalapa L. flower extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, and the percentage refers to the weight percentage in the skin external preparation;when the skin external preparation is an essence, and the skin external preparation preferably comprises the following components by weight: (1) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; or (2) 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 spice and 0.001%-10%of the Mirabilis jalapa L. extract; the rest of 100%is deionized water; or (3) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; wherein the polyol B is butanediol and/or 1, 3-propanediol; 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 propylparaben, methylparaben and phenoxyethanol; the Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract; the content of the Mirabilis jalapa L. flower extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, and the percentage refers to the weight percentage in the skin external preparation;when the skin external preparation is a lotion, and the skin external preparation preferably comprises the following components by weight: (1) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; or, (2) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; or, (3) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; wherein the oil C is mineral oil and/or isohexadecane; the preservative C is methylparaben and/or propylparaben; the Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract; the content of the Mirabilis jalapa L. flower extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, and the percentage refers to the weight percentage in the skin external preparation;when the skin external preparation is a cream, and the skin external preparation preferably comprises the following components by weight: (1) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; or, (2) 5%of glycerin, 5%of 1, 3-propanediol, 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; or, (3) 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 Mirabilis jalapa L. extract; the rest of 100%is deionized water; wherein the oil D is mineral oil and/or isohexadecane; the preservative D is methylparaben and/or propylparaben; the Mirabilis jalapa L. extract is preferably the Mirabilis jalapa L. flower extract, the content of the Mirabilis jalapa L. flower extract is preferably 0.0025-0.15%, more preferably 0.005-0.1%, and the percentage refers to the weight percentage in the skin external preparation.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810804107.XA CN110731919B (en) | 2018-07-20 | 2018-07-20 | Application of mirabilis jalapa extract and skin external preparation containing mirabilis jalapa extract |
| CN201810804107.X | 2018-07-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2020015725A1 true WO2020015725A1 (en) | 2020-01-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/CN2019/096711 Ceased WO2020015725A1 (en) | 2018-07-20 | 2019-07-19 | Use of mirabilis jalapa l. extracts and skin external preparations comprising the same |
Country Status (2)
| Country | Link |
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| CN (1) | CN110731919B (en) |
| WO (1) | WO2020015725A1 (en) |
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| CN113940905A (en) * | 2021-06-25 | 2022-01-18 | 太和康美(北京)中医研究院有限公司 | Face-beautifying cream and preparation method thereof |
| CN113995084A (en) * | 2021-11-18 | 2022-02-01 | 桂林理工大学 | Extraction method and application of jasmine flower extract |
| CN115444802A (en) * | 2022-09-05 | 2022-12-09 | 福州萍晴日用化妆品有限公司 | Jasmine moisturizing essence emulsion composition and preparation method thereof |
| CN115844746A (en) * | 2022-09-28 | 2023-03-28 | 山东宽源生物科技有限公司 | Anti-inflammatory and repairing bodhi cream and preparation method thereof |
| CN115998665A (en) * | 2023-02-10 | 2023-04-25 | 泉后(广州)生物科技研究院有限公司 | Cosmetic composition with soothing and repairing effect and application thereof |
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| CN111973509A (en) * | 2020-08-19 | 2020-11-24 | 澳宝化妆品(惠州)有限公司 | Skin care composition containing plant extract for soothing allergy |
| CN114392215A (en) * | 2021-12-29 | 2022-04-26 | 珠海金肽生物科技有限公司 | Composition containing plant callus extract and application thereof |
| CN115177566A (en) * | 2022-07-28 | 2022-10-14 | 杭州舒彩网络科技有限公司 | Synergistic hydroxy pinacolone retinoic acid ester anti-aging essence and preparation method thereof |
| CN115400058A (en) * | 2022-09-20 | 2022-11-29 | 杭州舒彩网络科技有限公司 | Composition for improving skin cell activity and application of composition in skin external product |
| CN118593376B (en) * | 2024-06-27 | 2025-01-28 | 广州瑞嘉精细化工有限公司 | A wrinkle-resistant and skin-firming composition and its application in cosmetics |
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| CN113940905A (en) * | 2021-06-25 | 2022-01-18 | 太和康美(北京)中医研究院有限公司 | Face-beautifying cream and preparation method thereof |
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| CN113995084A (en) * | 2021-11-18 | 2022-02-01 | 桂林理工大学 | Extraction method and application of jasmine flower extract |
| CN113995084B (en) * | 2021-11-18 | 2023-08-11 | 桂林理工大学 | A kind of extraction method and application of jasmine flower extract |
| CN115444802A (en) * | 2022-09-05 | 2022-12-09 | 福州萍晴日用化妆品有限公司 | Jasmine moisturizing essence emulsion composition and preparation method thereof |
| CN115844746A (en) * | 2022-09-28 | 2023-03-28 | 山东宽源生物科技有限公司 | Anti-inflammatory and repairing bodhi cream and preparation method thereof |
| CN115998665A (en) * | 2023-02-10 | 2023-04-25 | 泉后(广州)生物科技研究院有限公司 | Cosmetic composition with soothing and repairing effect and application thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN110731919B (en) | 2022-07-12 |
| CN110731919A (en) | 2020-01-31 |
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