WO2023282528A1 - Composition de blanchiment de la peau comprenant un extrait de feuille blanche de saururus chinensis (lour.) baill - Google Patents

Composition de blanchiment de la peau comprenant un extrait de feuille blanche de saururus chinensis (lour.) baill Download PDF

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WO2023282528A1
WO2023282528A1 PCT/KR2022/009314 KR2022009314W WO2023282528A1 WO 2023282528 A1 WO2023282528 A1 WO 2023282528A1 KR 2022009314 W KR2022009314 W KR 2022009314W WO 2023282528 A1 WO2023282528 A1 WO 2023282528A1
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extract
sambaekcho
melanin
skin whitening
white
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PCT/KR2022/009314
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English (en)
Korean (ko)
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정수경
윤석균
이예린
강승현
박명삼
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코스맥스 주식회사
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Priority to CN202280045631.8A priority Critical patent/CN117561050A/zh
Publication of WO2023282528A1 publication Critical patent/WO2023282528A1/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
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/78—Saururaceae (Lizard's-tail family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat

Definitions

  • It relates to a cosmetic composition for skin whitening, and a pharmaceutical composition and health functional food composition for preventing, treating, or improving melanin hyperpigmentation disease.
  • Pigmentation occurring on the skin is caused by an increase in melanin in the epidermis, and an important factor determining skin color is also caused by melanin.
  • the melanin biosynthesis mechanism refers to the process by which melanin is formed by the action of tyrosinase and TRP-1/2 (tyrosinase related protein-1/2) in melanosomes, which are organelles of melanocytes.
  • the melanosome transport mechanism is a process in which melanosomes are connected to microorganelles and actin and move to the tips of dendrites.
  • the melanosome transfer mechanism refers to the process in which melanosomes moved to the tip of the dendrites of melanocytes are moved to the surrounding epidermis.
  • Skin color is determined by the content and distribution of melanin, and is related to the number and distribution of melanosomes generated in melanocytes within cells and then released to the outside of the cells.
  • Skin hyperpigmentation may be caused by various factors such as hormonal abnormalities in the body after an inflammatory reaction of the skin, genetic diseases, ultraviolet irradiation, etc., the main cause is due to abnormal synthesis and distribution of melanin pigments.
  • the main function of melanin is to protect the skin from damage by removing oxygen radicals, and the high amount of melanin means that it has an effective countermeasure system to protect the skin from physical and chemical toxic substances.
  • composition containing the white leaf extract of Sambaekcho as an active ingredient.
  • a method for preventing or treating hypermelanin hyperpigmentation disease comprising administering a composition containing an effective amount of an extract of the white leaf of Sambaekcho to a subject in need thereof.
  • a white leaf extract of Sambyeongcho for use in preparing a medicament for preventing or treating hypermelanin hyperpigmentation disease.
  • One aspect provides a composition comprising the white leaf extract of Sambaekcho as an active ingredient.
  • Sambaekcho "Asian lizard's tail ( Saururus chinensis )" is called Sambaekcho because its leaves, roots and flowers are white. The leaves of Sambaekcho are green before blooming, but when it comes to flowering, the leaves turn white to attract insects, and after flowering, they turn green again. It is known that the flowering period of 300 seconds is from June to August. In other words, Sambaekcho has a "white leaf” only at a specific time.
  • the "three hundred seconds white leaves” means the white leaves of three hundred seconds harvested at the flowering time of three hundred seconds.
  • the 300 seconds white leaves are different from the 300 seconds green leaves and color, harvest time, etc.
  • extract includes all substances obtained by extracting components of a natural product, regardless of extraction method, extraction solvent, extraction conditions, extracted component or extract form, and is processed or treated by other methods after extracting components of a natural product. It also includes materials that can be obtained by For example, the processing or treatment may include dilution, concentration, drying, purification, fractionation, filtration, fermentation, enzymatic treatment, and the like. Therefore, the extract may include an extract, a dilution or concentrate of the extract, a dried product obtained by drying the extract, or a crude or purified product thereof, or a fraction obtained by fractionating the same.
  • the extraction method known natural product extraction methods such as hot water extraction, ethanol extraction, heat extraction, cold extraction, reflux extraction, reflux cooling extraction, ultrasonic extraction, and subcritical extraction may be used, but are not limited thereto.
  • the extraction method may be hot water extraction or ethanol extraction.
  • the extraction solvent may be selected from water, organic solvents, or mixtures thereof.
  • the water may be distilled water or purified water.
  • the organic solvent may include one or more of C1 to C6 lower alcohol, acetone, ether, ethyl acetate, diethyl ether, ethyl methyl ketone, and chloroform, but is not limited thereto.
  • the extraction solvent of the extract may be water, C1 to C4 alcohol, or a mixture thereof. In another embodiment, the extraction solvent of the extract may be a mixture of water and C1 to C4 alcohol. In another embodiment, the extraction solvent of the extract may be ethanol. In another embodiment, the extraction solvent of the extract is 10% (v / v) to 90% (v / v), 20% (v / v) to 80% (v / v), 30% (v / v) to 70% (v/v), 40% (v/v) to 60% (v/v) or 50% (v/v) ethanol. Therefore, the 300 seconds white leaf extract may be a 300 seconds white leaf hot water extract or a 300 seconds white leaf ethanol extract.
  • the 300 seconds white leaf extract may be 300 seconds white leaf ethanol extract.
  • the extraction conditions refer to conditions for extracting components of natural substances, such as extraction time and extraction temperature.
  • the extraction time is 30 minutes to 120 hours, 30 minutes to 100 hours, 30 minutes to 80 hours, 30 minutes to 60 hours, 30 minutes to 40 hours, 30 minutes to 20 hours, 30 minutes to 10 hours, 2 hours to 120 hours time, 2 hours to 100 hours, 2 hours to 80 hours, 2 hours to 60 hours, 2 hours to 40 hours, 2 hours to 20 hours, or 2 hours to 10 hours, but other conditions such as extraction solvent and extraction temperature can be selected appropriately.
  • the extraction temperature is 10 to 150 °C, 10 to 120 °C, 10 to 100 °C, 10 to 80 °C, 20 to 150 °C, 20 to 120 °C, 20 to 100 °C, 20 to 80 °C, 20 to 60 °C, 20 to 40 ° C., or room temperature, but may be appropriately selected according to other conditions such as extraction solvent and extraction time.
  • the "included as an active ingredient” means that the white leaf extract of Sambaekcho is added to the extent that it can exhibit the effect mentioned in this specification, and various ingredients are added as subcomponents for drug delivery and stabilization, and formulated in various forms. ) is meant to include being.
  • composition containing the white leaf extract of Sambaekcho as an active ingredient is used for skin whitening, for inhibiting melanin production, for inhibiting melanin secretion, for reducing melanin, for inhibiting melanin hyperpigmentation, or for preventing, treating or improving melanin hyperpigmentation diseases.
  • skin whitening may mean not only brightening the skin tone by inhibiting the synthesis of melanin pigment, but also improving skin hyperpigmentation such as spots or freckles caused by ultraviolet rays, hormones, or heredity.
  • inhibitortion of melanin production may mean suppression of new melanin production in cells or the like.
  • inhibitortion of melanin secretion may mean suppression of secretion of melanin from cells or the like.
  • reducing melanin may mean reducing the content of melanin existing in cells or the like.
  • melanin hyperpigmentation is a broad concept that includes all melanin hyperplasia caused by various causes, and means that certain parts of the skin, nails, or toenails become darker than other parts due to excessive increase in melanin pigment. .
  • the melanin hyperpigmentation disease is freckles (freckle); melasma; chloasma; liver spots; nevus; solar lentigo; melanosis; pelviz-jegher's syndrome; gestational brown spots (chloasma gravidarum); hyperpigmentation after drug use; And it may be any one selected from postinflammatory hyperpigmentation (postinflammatory hyperpigmentation), but is not limited thereto.
  • prevention includes inhibiting the development of a disease.
  • treatment includes inhibition of the development of, alleviation of, or elimination of a disease.
  • improvement can mean any action that at least reduces a parameter associated with alleviation or treatment of a condition, eg, the severity of a symptom.
  • the white leaf extract of Sambaekcho has a high skin whitening effect, melanin production inhibition, melanin secretion inhibition, melanin reduction, or melanin hyperpigmentation inhibition compared to the green leaf extract of Sambaekcho.
  • the white leaf extract of Sambaekcho may contain at least one of quercitrin and afzelin. In one embodiment, it was confirmed that the content of quercitrin and afzelin in the white leaf extract of Sambaekcho was significantly higher than that of the green leaf extract of Sambaekcho.
  • the composition may inhibit melanin production or secretion.
  • the white leaf extract of 3 baekcho is excellent in melanin production inhibitory effect and melanin secretion inhibitory effect compared to the green leaf extract of 3 baekcho.
  • quercitrin contained in the white leaf extract of Sambaekcho had excellent melanin production inhibitory effects and melanin secretion inhibitory effects.
  • the ethanol extract of Sambaekcho leaves had superior melanin production inhibitory effect and melanin secretion inhibitory effect compared to the hot water extract of Sambaekcho leaves.
  • the composition may inhibit the expression of PAR-2 (protease-activated receptor-2) involved in melanosome transmission.
  • PAR-2 prote-activated receptor-2
  • the afgeline contained in the white leaf extract of Sambaekcho inhibits the expression of PAR-2 involved in melanosome transmission, it was confirmed that there is an effect of inhibiting skin pigmentation.
  • the triticale white leaf extract may be included at a concentration of 0.0001 ⁇ g/ml to 0.1 ⁇ g/ml, 0.0001 ⁇ g/ml to 0.05 ⁇ g/ml, or 0.0001 ⁇ g/ml to 0.001 ⁇ g/ml based on the total composition, but is limited thereto It doesn't work.
  • the concentration of the white leaf extract of Sambaekcho can be selected in an appropriate range that can exhibit whitening efficacy without exhibiting cytotoxicity.
  • the quercitrin contained in the triticale white leaf extract is 0.0001 ⁇ g/ml to 100 ⁇ g/ml, 0.0001 ⁇ g/ml to 10 ⁇ g/ml, 0.0001 ⁇ g/ml to 1 ⁇ g/ml, 0.001 ⁇ g/ml based on the total composition. to 100 ⁇ g/ml, 0.001 ⁇ g/ml to 10 ⁇ g/ml, 0.001 ⁇ g/ml to 1 ⁇ g/ml, 0.01 ⁇ g/ml to 100 ⁇ g/ml, 0.01 ⁇ g/ml to 10 ⁇ g/ml, or 0.01 ⁇ g/ml. It may be included at a concentration of ml to 1 ⁇ g/ml, but is not limited thereto. The concentration of the quercitrin may be selected within an appropriate range capable of exhibiting a whitening effect without exhibiting cytotoxicity.
  • the triticale white leaf extract is 0.0001% to 20.0% by weight, 0.0001% to 10.0% by weight, 0.0001% to 5.0% by weight, 0.0001% to 1.0% by weight, 0.001% to 20.0% by weight based on the total composition. , 0.001% to 10.0%, 0.001% to 5.0%, 0.001% to 1.0%, 0.01% to 20.0%, 0.01% to 10.0%, 0.01% to 5.0%, or It may be included in 0.01% by weight to 1.0% by weight, but is not limited thereto.
  • the content of the white leaf extract of Sambaekcho can be selected in an appropriate range that can exhibit whitening efficacy without exhibiting cytotoxicity.
  • the composition may be a cosmetic composition.
  • the cosmetic composition may be used for skin whitening, inhibition of melanin production, inhibition of melanin secretion, reduction of melanin, or inhibition of excessive melanin pigmentation.
  • the cosmetic composition may further include ingredients commonly used in cosmetic compositions, functional additives, etc., in addition to the active ingredients disclosed herein, such as antioxidants, stabilizers, solubilizers, surfactants, dispersants, thickeners, Conventional adjuvants such as preservatives, vitamins, pigments, fragrances, and the like, and cosmetically acceptable carriers may be included.
  • ingredients commonly used in cosmetic compositions, functional additives, etc. such as antioxidants, stabilizers, solubilizers, surfactants, dispersants, thickeners, Conventional adjuvants such as preservatives, vitamins, pigments, fragrances, and the like, and cosmetically acceptable carriers may be included.
  • the cosmetic composition may be prepared in any formulation that is conventionally prepared.
  • the cosmetic composition may be cosmetic water, cream, essence, cleansing foam, cleansing water, pack, ampoule, body lotion, body oil, body gel, shampoo, rinse, hair conditioner, hair gel, foundation, lipstick, mascara, or It may have a cosmetic formulation of a makeup base.
  • the composition may be an external composition for skin.
  • composition for external application for skin may be used for skin whitening, inhibition of melanin production, inhibition of melanin secretion, reduction of melanin, inhibition of melanin hyperpigmentation, or prevention, treatment, or improvement of melanin hyperpigmentation disease.
  • the external skin preparation may be a cream, gel, ointment, skin emulsifier, skin suspension, transdermal patch, drug-containing bandage, lotion, or a combination thereof.
  • the external skin preparation is a component usually used in external preparations for skin such as cosmetics or pharmaceuticals, for example, water-based components, oil-based components, powder components, alcohols, moisturizers, thickeners, ultraviolet absorbers, whitening agents, preservatives, antioxidants, surfactants, and fragrances. , colorants, various skin nutrients, or combinations thereof and may be suitably blended as needed.
  • the composition may be a pharmaceutical composition.
  • the pharmaceutical composition may be used for skin whitening, inhibition of melanin production, inhibition of melanin secretion, reduction of melanin, inhibition of melanin hyperpigmentation, or prevention or treatment of melanin hyperpigmentation diseases.
  • the pharmaceutical composition may additionally include a pharmaceutically acceptable diluent or carrier.
  • the diluent may be lactose, corn starch, soybean oil, microcrystalline cellulose, or mannitol, and magnesium stearate, talc, or a combination thereof as a lubricant.
  • the carrier may be an excipient, a disintegrant, a binder, a lubricant, or a combination thereof.
  • the excipient may be microcrystalline cellulose, lactose, low-substituted hydroxycellulose, or a combination thereof.
  • the disintegrant may be calcium carboxymethylcellulose, sodium starch glycolate, calcium monohydrogen phosphate, or a combination thereof.
  • the binder may be polyvinylpyrrolidone, low-substituted hydroxypropylcellulose, hydroxypropylcellulose, or a combination thereof.
  • the lubricant may be magnesium stearate, silicon dioxide, talc, or a combination thereof.
  • the pharmaceutical composition may be formulated for oral or parenteral administration.
  • Oral dosage forms may be granules, powders, solutions, tablets, capsules, dry syrups, or combinations thereof.
  • Parenteral dosage forms may be injections.
  • the composition may be a health functional food composition.
  • It may be used for skin whitening, inhibition of melanin production, inhibition of melanin secretion, reduction of melanin, inhibition of melanin hyperpigmentation, or prevention or improvement of melanin hyperpigmentation disease.
  • the health functional food composition may be used alone with the extract, or in combination with other foods or food ingredients, and may be appropriately used according to conventional methods.
  • the mixing amount of the active ingredient may be appropriately determined depending on the purpose of use (prevention, health or therapeutic treatment).
  • beverage compositions may contain various flavoring agents or natural carbohydrates as additional components, like conventional beverages.
  • the natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol.
  • the sweetener natural sweeteners such as thaumatin and stevia extract, or synthetic sweeteners such as saccharin and aspartame may be used.
  • the health functional food composition may also contain nutrients, vitamins, electrolytes, flavors, colorants, pectic acid and its salts, alginic acid and its salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohol, carbonated beverages It may contain a carbonation agent used for, or a combination thereof.
  • the health functional food composition may also contain natural fruit juice, fruit juice beverages, fruit flesh for preparing vegetable beverages, or a combination thereof.
  • Another aspect provides a method for preparing the white leaf extract of Sambaekcho.
  • the method includes obtaining an extract by incubating the white leaves of Sambaekcho with an extraction solvent.
  • the incubation may be performed under conventional extraction conditions. Details of the extraction conditions are as described above.
  • the method may further include filtering and/or drying the obtained extract.
  • filtering and/or drying known conventional methods may be used.
  • Another aspect provides a method for preventing or treating melanin hyperpigmentation disease comprising administering to a subject in need thereof a composition comprising an effective amount of a white leaf extract of triticale.
  • administering means the arrangement of the composition according to.
  • Administration may be administered by a method known in the art. Administration may be administered directly to a subject by any means, for example, by routes such as intravenous, intramuscular, oral, transdermal, mucosal, intranasal, intratracheal or subcutaneous administration. can The administration may be administered systemically or locally. The administration may be applied to the skin.
  • the subject may be a mammal, such as a human, cow, horse, pig, dog, sheep, goat, or cat.
  • the subject may be a subject in need of prevention or treatment of melanin hyperpigmentation disease.
  • the dosage may be prescribed in various ways depending on factors such as formulation method, administration method, patient's age, weight, sex, medical condition, food, administration time, administration route, excretion rate and reaction sensitivity, and those skilled in the art can determine these factors Dosage can be appropriately adjusted in consideration of these factors.
  • the number of administrations can be once a day or two or more times within the range of clinically acceptable side effects, and administration can be performed at one or two or more sites, daily or at intervals of 2 to 5 days.
  • the number of administration days may be administered from 1 day to 30 days per treatment. If necessary, the same treatment can be repeated after a titration period.
  • the same dosage per kg as for humans is used, or the above dosage is converted by the volume ratio (eg, average value) of the organ (heart, etc.) between the target animal and the human.
  • a single dose can be administered.
  • Another aspect provides the use of a white leaf extract of Sambyeongcho for use in preparing a medicament for the prevention or treatment of melanin hyperpigmentation disease.
  • Redundant content is omitted in consideration of the complexity of the present specification, and terms not defined otherwise in the present specification have meanings commonly used in the technical field to which the present invention belongs.
  • the composition according to one aspect may have skin whitening, suppression of melanin production and secretion, and suppression of melanin hyperpigmentation by including the white leaf extract of Sambaekcho. Since the white leaf extract of Sambaekcho has excellent melanin production and secretion inhibitory effects and skin pigmentation inhibitory effects compared to the green leaf extract of Sambaekcho, it can be used as a cosmetic composition or pharmaceutical composition for skin whitening.
  • Figure 1a shows the results of LC-QTOF-MS analysis of the white leaf extract of Sambaekcho of Example 1.
  • Figure 1b shows the results of LC-QTOF-MS analysis of the green leaf extract of Sambaekcho of Comparative Example 1.
  • 2a and 2b are MS fragmentation patterns of quercitrin contained in the white leaves of Sambaekcho.
  • 3a and 3b are MS fragmentation patterns of afgeline contained in the white leaves of Schiekcho.
  • Figure 4 shows the cytotoxicity test results of Example 1, Comparative Example 1, Example 2 and Comparative Example 2.
  • Figure 5 shows the results of the cytotoxicity test of quercitrin contained in the white leaf extract of Sambaekcho.
  • Figure 6 shows the results of the cytotoxicity test of afgeline contained in the white leaf extract of Sambaekcho.
  • Figure 7 shows the melanin biosynthesis results of Example 1, Comparative Example 1, Example 2 and Comparative Example 2.
  • Figure 8 shows the melanin biosynthesis results of quercitrin contained in the white leaf extract of Sambaekcho.
  • Figure 11 shows the PAR-2 expression inhibitory effect of afgeline contained in the white leaf extract of Sambaekcho.
  • distilled water corresponding to 10 times the weight of the original weight of 300 seconds white leaves was added and mixed, and then extracted at a temperature of 90 ° C. for 4 hours and 30 minutes.
  • the obtained extract was filtered using a filter paper, and then the filtrate was concentrated under reduced pressure using a rotary evaporator.
  • the filtrate subjected to concentration under reduced pressure was lyophilized to remove the remaining solvent to obtain a powdery hot-water extract of Sambaekcho white leaves.
  • distilled water corresponding to 10 times the weight of the raw material of the three hundred seconds green leaves was added and mixed, and then extracted at a temperature of 90 ° C. for 4 hours and 30 minutes.
  • the obtained extract was filtered using a filter paper, and then the filtrate was concentrated under reduced pressure using a rotary evaporator.
  • the filtrate subjected to concentration under reduced pressure was lyophilized to remove the remaining solvent to obtain a powdery hot-water extract of the green leaves of Sambaekcho.
  • the white leaf extract and the green leaf extract of Sambaekcho were dissolved in 50% methanol, respectively, to a concentration of 1 mg/mL. Then, after filtering with a 0.45 ⁇ m PVDF (Polyamide Fluoride) filter, it was analyzed by LC-QTOF-MS (liquid chromatography-quadrupole-time of flight mass spectrometry). LC-QTOF-MS analysis results are shown in Figures 1a and 1b.
  • FIGS. 2a to 2b MS fragmentation patterns for two peaks showing major differences among the four flavonoid glycosides are shown in FIGS. 2a to 2b and FIGS. 3a to 3b. Table 1 also shows the MS fragment dereplication results for the two peaks.
  • the cytotoxicity of the white leaf and green leaf extracts of Sambaekcho and the indicator component quercitrin on B16 melanoma cells was evaluated.
  • melanoma cells were inoculated in a 6-well plate and cultured for 24 hours, then replaced with new DMEM medium containing ⁇ -MSH and 10% bovine serum, and each sample was treated by concentration and cultured for 72 hours.
  • the cultured cells were reacted by replacing the medium with a 10-fold diluted MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) solution at 2.5 mg/ml. Thereafter, the supernatant was removed, and 2 ml of dimethyl sulfoxide (DMSO) was added to dissolve the MTT-formazan crystals, and the absorbance was measured at 570 nm using an ELISA reader. What was treated with ⁇ -MSH was used as a control. Cytotoxicity was expressed as a percentage of absorbance compared to the control group, and the results are shown in Tables 2 and 3 and FIGS. 4 and 5.
  • Example 1 As shown in Table 2, Table 3, Figures 4 and 5, in melanoma cells, Example 1's white leaf extract, Comparative Example 1's green leaf extract, Example 2's white leaf hot water extract, and comparison All of the hot-water extracts of Sambaekcho green leaves in Example 2 showed no toxicity up to a concentration of 0.1 ⁇ g/ml. In addition, quercitrin, a marker component, showed no toxicity up to a concentration of 100 ⁇ g/ml.
  • HaCaT keratinocytes
  • HaCaT keratinocytes
  • the medium of the cultured cells was replaced with a serum-free medium, and the samples were treated by concentration and cultured for 24 hours.
  • the cultured cells were reacted by replacing the 2.5 mg/ml MTT solution with a 10-fold diluted medium. Thereafter, the supernatant was removed and 1 ml of DMSO was added to dissolve the MTT-formazan crystals, and the absorbance was measured at 570 nm using an ELISA reader.
  • the untreated group was used as a control group. Cytotoxicity was expressed as a percentage of absorbance compared to the control group, and the results are shown in Table 4 and FIG. 6.
  • afgeline a marker component, showed no toxicity to keratinocytes up to a concentration of 100 ⁇ g/ml.
  • the whitening effect of the white leaf and green leaf extracts of Sambaekcho and the indicator component quercitrin to inhibit melanin biosynthesis per unit cell in melanoma cells was measured.
  • the medium was replaced with new DMEM medium containing ⁇ -MSH and 10% bovine serum, and the samples were treated by concentration and cultured for 72 hours.
  • the medium was transferred to a 96-well plate, and then the absorbance was measured at 450 nm to obtain the amount of melanin secreted per unit cell.
  • the cells from which the medium was completely removed were washed with 2 ml of phosphate-buffered saline (PBS), treated with 0.25 ml of 1N NaOH, and the cells were collected in a 1.5 ml tube to obtain intracellular melanin.
  • PBS phosphate-buffered saline
  • the harvested cell lysate was incubated at 60° C. for 30 minutes, vortexed, and then transferred to a 96-well plate and absorbance was measured at 450 nm to determine the amount of melanin produced per unit cell.
  • ⁇ -MSH treatment was used as a control group
  • arbutin manufactured: Hyundai Bioland
  • the melanin biosynthesis results per unit cell are shown in Tables 5 and 6 and FIGS. 7 and 8, and the melanin secretion rate results per unit cell are shown in Tables 7 and 8 and FIGS. 9 and 10.
  • the white leaf ethanol extract and green leaf ethanol extract of Sambaekcho decreased the melanin production rate and secretion rate per unit cell increased by ⁇ -MSH in a concentration-dependent manner.
  • the ethanol extract of the white leaf of Sambaekcho was superior to the ethanol extract of the green leaf in inhibition of melanin production and secretion per unit cell.
  • quercitrin a marker component, also exhibits a whitening effect by inhibiting melanin biosynthesis and secretion by inhibiting melanin production and secretion per unit cell.
  • Keratinocytes were inoculated into a 60 mm culture dish (corning), cultured for 24 hours, washed twice with HBSS (Hank's Buffered Salt Solution), and then UVB 30 mJ/cm 2 was irradiated with HBSS. Thereafter, the medium was replaced with a serum-free medium, and each sample was treated by concentration and cultured for 8 hours. Then, the cells were collected with QIAzol Lysis Reagent (Qiagen) and RNA was isolated according to the manufacturer's method. After quantifying the isolated RNA, real-time PCR was performed by synthesizing cDNA with 1 ⁇ g of RNA.
  • HBSS Horatinocytes
  • the PAR-2 and ⁇ -Actin primers used in PCR were synthesized and used by Cosmogenetec (Korea), and the primer sequences are shown in Table 9. UVB irradiation was used as a control group, and niacinamide (manufacturer: Sigma) was used as a positive control group. PAR-2 expression results are shown in Table 10 and FIG. 11.

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Abstract

La présente invention concerne une composition cosmétique de blanchiment de la peau, une composition pharmaceutique pour la prévention, le traitement, ou le soulagement d'une maladie d'hyperpigmentation, et une composition alimentaire fonctionnelle pour la santé, comprenant chacune un extrait de feuilles blanches de Saururus chinensis (Lour.) Baill en tant que principe actif. L'extrait de feuilles blanches de Saururus chinensis (Lour.) Baill est supérieur à celui de feuilles vertes de Saururus chinensis (Lour.) Baill en termes d'activité inhibitrice contre la mélanogenèse et la sécrétion de mélanine et contre la pigmentation de la peau, et peut ainsi être utilisé dans une composition cosmétique ou une composition pharmaceutique pour le blanchiment de la peau.
PCT/KR2022/009314 2021-07-09 2022-06-29 Composition de blanchiment de la peau comprenant un extrait de feuille blanche de saururus chinensis (lour.) baill WO2023282528A1 (fr)

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KR20150023601A (ko) * 2015-02-03 2015-03-05 (주)아모레퍼시픽 삼백초 추출물 함유 조성물
KR101993699B1 (ko) * 2017-04-19 2019-06-28 주식회사 진켐 피부 개선용 조성물
KR102202554B1 (ko) * 2019-07-23 2021-01-14 주식회사 현대바이오랜드 삼백초잎 추출물, 포도씨 추출물, 마치현 추출물 및 고두밥 발효물을 포함하는 피부 미백용 화장료 조성물

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KR100865071B1 (ko) 2007-04-27 2008-10-23 영남대학교 산학협력단 삼백초 추출물 또는 이로부터 분리된 화합물을유효성분으로 함유하는 미백용 조성물

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20070087552A (ko) * 2004-12-17 2007-08-28 가부시키가이샤 시세이도 미백용 피부 외용제, 미백제, 미백 방법 및 미백용 피부외용제의 제조 방법
KR20100086728A (ko) * 2009-01-23 2010-08-02 (주)아모레퍼시픽 피부 미백용 화장료 조성물
KR20150023601A (ko) * 2015-02-03 2015-03-05 (주)아모레퍼시픽 삼백초 추출물 함유 조성물
KR101993699B1 (ko) * 2017-04-19 2019-06-28 주식회사 진켐 피부 개선용 조성물
KR102202554B1 (ko) * 2019-07-23 2021-01-14 주식회사 현대바이오랜드 삼백초잎 추출물, 포도씨 추출물, 마치현 추출물 및 고두밥 발효물을 포함하는 피부 미백용 화장료 조성물

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