WO2023282528A1 - Skin whitening composition comprising extract from white leaf of saururus chinensis (lour.) baill - Google Patents
Skin whitening composition comprising extract from white leaf of saururus chinensis (lour.) baill Download PDFInfo
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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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- Prior art keywords
- extract
- sambaekcho
- melanin
- skin whitening
- white
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Classifications
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- 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
- 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
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- 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)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
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- 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
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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
- 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
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- 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
The present invention relates to a skin whitening cosmetic composition, a pharmaceutical composition for prevention, treatment, or alleviation of hyperpigmentation disease, and a health functional food composition, each comprising an extract from white leaves of Saururus chinensis (Lour.) Baill as an active ingredient. The extract from white leaves of Saururus chinensis (Lour.) Baill is superior to that from green leaves of Saururus chinensis (Lour.) Baill in terms of inhibitory activity against melanogenesis and melanin secretion and against skin pigmentation and thus can be used in a cosmetic composition or pharmaceutical composition for skin whitening.
Description
본 출원은 2021년 7월 9일 출원된 대한민국 특허출원 제 10-2021-0090492호 를 우선권으로 주장하고, 상기 명세서 전체는 본 출원의 참고문헌이다.This application claims priority to Republic of Korea Patent Application No. 10-2021-0090492 filed on July 9, 2021, and the entire specification is a reference in this application.
피부 미백용 화장료 조성물, 및 멜라닌 색소 과다 침착 질환의 예방, 치료 또는 개선용 약학적 조성물 및 건강기능식품 조성물에 관한 것이다.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.
기미, 주근깨 등 피부에 생기는 색소 침착은 표피 내 멜라닌의 증가에 기인하며, 피부색을 결정하는 중요 요인도 멜라닌에 의한 것이다. Pigmentation occurring on the skin, such as spots and freckles, is caused by an increase in melanin in the epidermis, and an important factor determining skin color is also caused by melanin.
피부 색소 형성 기전은 크게 멜라닌 생합성(melanogenesis), 멜라노좀 수송(melanosome transport), 및 멜라노좀 전달(melanosome transfer) 세가지로 나누어 볼 수 있다. 멜라닌 생합성 기전은 멜라노사이트(melanocyte)의 소기관인 멜라노좀(melanosome)에서 티로시나제(tyrosinase), TRP-1/2 (tyrosinase related protein-1/2)의 작용으로 멜라닌이 형성되는 과정을 말한다. 멜라노좀 수송 기전은 멜라노좀이 미세소기관과 액틴에 연결되어 수상돌기 끝부분으로 이동하는 과정이다. 마지막으로 멜라노좀 전달 기전은 멜라노사이트의 수상돌기 끝부분으로 이동된 멜라노좀이 주변에 퍼져있는 표피로 이동되는 과정을 말한다. 위 세가지 기전들을 통해, 자외선으로부터 활성화된 멜라노사이트에서 티로시나제의 합성이 촉진되고 멜라닌의 생성이 항진되어 이를 표피 밖으로 운반, 배출하게 되는 것이다(Jody P. Ebanks, Mechanisms Regulating Skin Pigmentation: The Rise and Fall of Complexion Coloration, Int J Mol Sci. Sep; 10(9): 4066-4087, 2009).Skin pigment formation mechanisms can be largely divided into three types: melanogenesis, melanosome transport, and melanosome transfer. 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. Finally, 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. Through the above three mechanisms, the synthesis of tyrosinase is promoted in melanocytes activated by ultraviolet rays and the production of melanin is promoted, which is transported and discharged out of the epidermis (Jody P. Ebanks, Mechanisms Regulating Skin Pigmentation: The Rise and Fall of Complexion Coloration, Int J Mol Sci. Sep;10(9): 4066-4087, 2009).
피부색은 멜라닌의 함량, 분포 등에 따라 색이 결정되며, 세포내 멜라노사이트에서 생성된 후 세포 외부로 방출되는 멜라노좀의 수와 분포에 연관되어 있다. 피부의 과색소침착(hyperpigmentation)은 피부의 염증 반응 이후의 체내 호르몬 이상, 유전 질환, 자외선 조사 등 여러 요인에 의해 발생될 수 있는데, 주된 요인은 멜라닌 색소 합성 이상 및 분포 이상에 의한 것이다. 멜라닌의 주요한 기능은 산소 라디칼을 제거하여 이에 의한 손상으로부터 피부를 보호하는 것으로, 멜라닌이 많다는 것은 물리적, 화학적 독성 물질로부터 피부를 보호하기 위한 효과적인 대응체계를 가지고 있음을 의미한다.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 (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.
하지만 과도한 멜라닌의 침착은 피부 등의 병리적 문제의 원인이 되기도 하지만, 기미, 주근깨, 점, 검버섯과 같은 미용적인 측면의 문제로도 인식되고 있다. 따라서, 멜라닌 형성을 근본적으로 억제할 수 있는 미백제의 개발이 필요하다.However, excessive melanin deposition causes pathological problems such as the skin, but is also recognized as a cosmetic problem such as melasma, freckles, spots, and age spots. Therefore, it is necessary to develop a whitening agent capable of fundamentally inhibiting melanin formation.
최근에 발표된 사실에 의하면, 멜라닌 생합성 과정 뿐만 아니라 멜라노좀 수송 및 전달 과정과 연관된 주요 인자들을 저해할 수 있는 물질을 개발하는 것도 피부 색소침착을 방지할 수 있는 방법이 될 수 있다(Jong il Park at al., Inhibitory effect of 2-methyl-naphtho[1,2,3-de]quinolin-8-one on melanosome transport and skin pigmentation, Scientific Reports volume 6, Article number: 29189, 2016).According to a recently published fact, developing a substance capable of inhibiting not only the melanin biosynthesis process but also the major factors related to the melanosome transport and delivery process can be a way to prevent skin pigmentation (Jong il Park at al., Inhibitory effect of 2-methyl-naphtho[1,2,3-de]quinolin-8-one on melanosome transport and skin pigmentation, Scientific Reports volume 6, Article number: 29189, 2016).
따라서, 멜라닌 생합성을 저해하고, 멜라노좀 전달 과정과 연관된 인자를 저해할 수 있는 새로운 미백 원료의 개발이 필요하다.Therefore, it is necessary to develop a new whitening raw material capable of inhibiting melanin biosynthesis and inhibiting factors related to the melanosome transmission process.
삼백초 흰 잎 추출물을 유효성분으로 포함하는 조성물을 제공한다.Provided is a composition containing the white leaf extract of Sambaekcho as an active ingredient.
삼백초 흰 잎 추출물을 제조하는 방법을 제공한다.Provides a method for preparing the white leaf extract of Sambaekcho.
유효량의 삼백초 흰 잎 추출물을 포함하는 조성물을 이를 필요로 하는 개체에게 투여하는 단계를 포함하는 멜라닌 색소 과다 침착 질환을 예방 또는 치료하는 방법을 제공한다.Provided is 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.
멜라닌 색소 과다 침착 질환의 예방 또는 치료용 약제를 제조하는 데 사용하기 위한, 삼백초 흰 잎 추출물의 용도를 제공한다.Provided is the use of a white leaf extract of Sambyeongcho for use in preparing a medicament for preventing or treating hypermelanin hyperpigmentation disease.
일 양상은 삼백초 흰 잎 추출물을 유효성분으로 포함하는 조성물을 제공한다.One aspect provides a composition comprising the white leaf extract of Sambaekcho as an active ingredient.
"삼백초(Asian lizard's tail, Saururus chinensis)"는 잎, 뿌리 및 꽃이 흰색을 띠어 삼백초라고 불리게 되었다. 삼백초는 꽃이 피기 전에는 잎이 초록색이었다가 개화시기가 되면 곤충들을 유혹하기 위해 잎이 흰색으로 변하며, 개화 후에는 다시 초록색으로 변하는 특징이 있다. 삼백초의 개화시기는 6월 내지 8월로 알려져 있다. 즉, 삼백초는 특정 시기에만 "흰 잎(white leaf)"을 가지게 된다."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.
따라서, 상기 "삼백초 흰 잎"은 삼백초의 개화시기에 수확된 삼백초의 흰 잎을 의미한다. 상기 삼백초 흰 잎은 삼백초 초록 잎과 색상, 수확시기 등에 차이가 있다.Therefore, 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.
용어 "추출물"은 추출 방법, 추출 용매, 추출 조건, 추출된 성분 또는 추출물의 형태를 불문하고, 천연물의 성분을 추출함으로써 얻어진 물질을 모두 포함하며, 천연물의 성분을 추출한 후 다른 방법으로 가공 또는 처리하여 얻어질 수 있는 물질도 포함한다. 예를 들어, 상기 가공 또는 처리는 희석, 농축, 건조, 정제, 분획, 여과, 발효, 효소 처리 등을 포함할 수 있다. 따라서, 상기 추출물은 추출액, 추출액의 희석액 또는 농축액, 추출액을 건조하여 얻어지는 건조물, 또는 이들 조정제물 또는 정제물, 이를 분획한 분획물을 포함할 수 있다.The term "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.
상기 추출 방법은 열수 추출, 에탄올 추출, 가열 추출, 냉침 추출, 환류 추출, 환류냉각 추출, 초음파 추출, 아임계 추출 등 공지된 천연물 추출 방법을 사용할 수 있으나, 이에 제한되지 않는다. 일 구체예에서, 상기 추출 방법은 열수 추출 또는 에탄올 추출일 수 있다.As 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. In one embodiment, the extraction method may be hot water extraction or ethanol extraction.
상기 추출 용매는 물, 유기 용매, 또는 이들의 혼합물로부터 선택될 수 있다. 상기 물은 증류수 또는 정제수일 수 있다. 상기 유기 용매는 C1 내지 C6의 저급 알코올, 아세톤, 에테르, 에틸아세테이트, 디에틸에테르, 에틸메틸케톤 및 클로로포름 중 1종 이상을 포함할 수 있으나, 이에 제한되지 않는다.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.
일 구체예에서, 상기 추출물의 추출 용매는 물, C1 내지 C4의 알코올, 또는 이들의 혼합물일 수 있다. 다른 구체예에서, 상기 추출물의 추출 용매는 물 및 C1 내지 C4의 알코올의 혼합물일 수 있다. 다른 구체예에서, 상기 추출물의 추출 용매는 에탄올일 수 있다. 다른 구체예에서, 상기 추출물의 추출 용매는 10%(v/v) 내지 90%(v/v), 20%(v/v) 내지 80%(v/v), 30%(v/v) 내지 70%(v/v), 40%(v/v) 내지 60%(v/v) 또는 50%(v/v) 에탄올일 수 있다. 따라서, 상기 삼백초 흰 잎 추출물은 삼백초 흰 잎 열수추출물 또는 삼백초 흰 잎 에탄올 추출물일 수 있다. 일 실시예에서, 삼백초 흰 잎 에탄올 추출물은 삼백초 흰 잎 열수추출물에 비해 멜라닌 생성 저해 효과 및 멜라닌 분비 저해 효과가 우수함을 확인하였다. 따라서, 상기 삼백초 흰 잎 추출물은 삼백초 흰 잎 에탄올 추출물일 수 있다.In one embodiment, 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. In one embodiment, it was confirmed that the ethanol extract of Sambaekcho white leaves had superior melanin production inhibitory effect and melanin secretion inhibitory effect compared to the hot water extract of Sambaekcho white leaves. Therefore, the 300 seconds white leaf extract may be 300 seconds white leaf ethanol extract.
상기 추출 조건은 추출 시간, 추출 온도 등 천연물의 성분을 추출하기 위한 조건을 의미한다. 상기 추출 시간은 30분 내지 120시간, 30분 내지 100시간, 30분 내지 80시간, 30분 내지 60시간, 30분 내지 40시간, 30분 내지 20시간, 30분 내지 10시간, 2시간 내지 120시간, 2시간 내지 100시간, 2시간 내지 80시간, 2시간 내지 60시간, 2시간 내지 40시간, 2시간 내지 20시간, 또는 2시간 내지 10시간일 수 있으나, 추출 용매, 추출 온도 등 다른 조건에 따라 적절히 선택할 수 있다. 상기 추출 온도는 10 내지 150℃, 10 내지 120℃, 10 내지 100℃, 10 내지 80℃, 20 내지 150℃, 20 내지 120℃, 20 내지 100℃, 20 내지 80℃, 20 내지 60℃, 20 내지 40℃, 또는 상온일 수 있으나, 추출 용매, 추출 시간 등 다른 조건에 따라 적절히 선택할 수 있다.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 ℃, 10 to 120 ℃, 10 to 100 ℃, 10 to 80 ℃, 20 to 150 ℃, 20 to 120 ℃, 20 to 100 ℃, 20 to 80 ℃, 20 to 60 ℃, 20 to 40 ° C., or room temperature, but may be appropriately selected according to other conditions such as extraction solvent and extraction time.
상기 "유효성분으로 포함"은 본 명세서에서 언급한 효과를 나타낼 수 있는 정도로 삼백초 흰 잎 추출물이 첨가되는 것을 의미하고, 약물전달 및 안정화를 위하여 다양한 성분을 부성분으로 첨가하여 다양한 형태로 제형화(formulation)되는 것을 포함하는 의미이다.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.
상기 삼백초 흰 잎 추출물을 유효성분으로 포함하는 조성물은 피부 미백용, 멜라닌 생성 억제용, 멜라닌 분비 억제용, 멜라닌 감소용, 멜라닌 색소 과다 침착 억제용, 또는 멜라닌 색소 과다 침착 질환의 예방, 치료 또는 개선용 일 수 있다.The 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. can be dragon
용어 "피부 미백"은 멜라닌 색소의 합성을 저해함으로써 피부 톤을 밝게 할 뿐만 아니라, 자외선, 호르몬 또는 유전에 기인한 기미나 주근깨 등의 피부 과색소 침착을 개선하는 것을 의미할 수 있다.The term "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.
용어 "멜라닌 생성 억제"란 세포 등에서 멜라닌이 새롭게 생성되는 것을 억제하는 것을 의미할 수 있다.The term “inhibition of melanin production” may mean suppression of new melanin production in cells or the like.
용어 "멜라닌 분비 억제"란 세포 등에서 멜라닌이 분비되는 것을 억제하는 것을 의미할 수 있다. The term “inhibition of melanin secretion” may mean suppression of secretion of melanin from cells or the like.
용어 "멜라닌 감소"란 세포 등에 기존에 존재하는 멜라닌 함량을 감소시키는 것을 의미할 수 있다.The term "reducing melanin" may mean reducing the content of melanin existing in cells or the like.
용어 "멜라닌 색소 과다 침착"이란 다양한 원인에 의해서 발생한 멜라닌 색소 과다 침착을 모두 포함하는 광범위한 개념이며, 피부 또는 손톱, 발톱의 특정 부위에서 멜라닌 색소의 과도한 증가로 인해 다른 부위에 비해 어둡게 되는 것을 의미한다.The term "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. .
상기 멜라닌 색소 과다 침착 질환은 주근깨(freckle); 기미(melasma); 간반(chloasma); 검버섯(liver spot); 모반(nevus); 일광흑자(solar lentigo); 흑피증(melanosis); 포이츠-예거 증후군(peutz-jegher's syndrome); 임신성 갈색반(chloasma gravidarum); 약물 사용 후 과다색소침착; 및 염증 후 과다색소침착(postinflammatory hyperpigmentation) 중에서 선택된 어느 하나일 수 있으나, 이에 제한되지 않는다.The melanin hyperpigmentation disease is freckles (freckle); melasma; chloasma; liver spots; nevus; solar lentigo; melanosis; peutz-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.
용어 "예방"은 질병의 발생을 억제하는 것을 포함한다. 용어 "치료"는 질병의 발전의 억제, 경감, 또는 제거를 포함한다. 용어 "개선"은 상태의 완화 또는 치료와 관련된 파라미터, 예를 들면 증상의 정도를 적어도 감소시키는 모든 행위를 의미할 수 있다.The term "prevention" includes inhibiting the development of a disease. The term "treatment" includes inhibition of the development of, alleviation of, or elimination of a disease. The term "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.
상기 삼백초 흰 잎 추출물은 삼백초 초록 잎 추출물에 비해 높은 피부 미백 효능, 멜라닌 생성 억제능, 멜라닌 분비 억제능, 멜라닌 감소능, 또는 멜라닌 색소 과다 침착 억제능을 갖는다. 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.
상기 삼백초 흰 잎 추출물은 퀘르시트린(quercitrin) 및 아프젤린(afzelin) 중 어느 하나 이상을 포함할 수 있다. 일 실시예에서, 상기 삼백초 흰 잎 추출물은 삼백초 초록 잎 추출물에 비해 퀘르시트린 및 아프젤린 함량이 현저히 높음을 확인하였다.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.
상기 조성물은 멜라닌 생성 또는 분비를 저해하는 것일 수 있다. 일 실시예에서, 상기 삼백초 흰 잎 추출물은 삼백초 초록 잎 추출물에 비해 멜라닌 생성 저해 효과 및 멜라닌 분비 저해 효과가 우수함을 확인하였다. 또한, 삼백초 흰 잎 추출물에 함유된 퀘르시트린은 멜라닌 생성 저해 효과 및 멜라닌 분비 저해 효과가 우수함을 확인하였다. 또한, 삼백초 잎 에탄올 추출물은 삼백초 잎 열수추출물에 비해 멜라닌 생성 저해 효과 및 멜라닌 분비 저해 효과가 우수함을 확인하였다.The composition may inhibit melanin production or secretion. In one embodiment, it was confirmed that 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. In addition, it was confirmed that quercitrin contained in the white leaf extract of Sambaekcho had excellent melanin production inhibitory effects and melanin secretion inhibitory effects. In addition, it was confirmed that 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.
상기 조성물은 멜라노좀 전달에 관여하는 PAR-2(protease-activated receptor-2)의 발현을 저해하는 것일 수 있다. 일 실시예에서, 상기 삼백초 흰 잎 추출물에 함유된 아프젤린은 멜라노좀 전달에 관여하는 PAR-2의 발현을 저해함을 확인하였으므로, 피부 색소 침착 저해 효능이 있음을 확인하였다.The composition may inhibit the expression of PAR-2 (protease-activated receptor-2) involved in melanosome transmission. In one embodiment, since it was confirmed that 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.
상기 삼백초 흰 잎 추출물은 조성물 전체를 기준으로 0.0001 ㎍/ml 내지 0.1 ㎍/ml, 0.0001 ㎍/ml 내지 0.05 ㎍/ml, 또는 0.0001 ㎍/ml 내지 0.001 ㎍/ml의 농도로 포함될 수 있으나, 이에 제한되지 않는다. 상기 삼백초 흰 잎 추출물의 농도는 세포 독성을 나타내지 않으면서 미백 효능을 나타낼 수 있는 적절한 범위를 선택할 수 있다.The triticale white leaf extract may be included at a concentration of 0.0001 μg/ml to 0.1 μg/ml, 0.0001 μg/ml to 0.05 μg/ml, or 0.0001 μg/ml to 0.001 μg/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.
상기 삼백초 흰 잎 추출물에 함유된 퀘르시트린은 조성물 전체를 기준으로 0.0001 ㎍/ml 내지 100 ㎍/ml, 0.0001 ㎍/ml 내지 10 ㎍/ml, 0.0001 ㎍/ml 내지 1 ㎍/ml, 0.001 ㎍/ml 내지 100 ㎍/ml, 0.001 ㎍/ml 내지 10 ㎍/ml, 0.001 ㎍/ml 내지 1 ㎍/ml, 0.01 ㎍/ml 내지 100 ㎍/ml, 0.01 ㎍/ml 내지 10 ㎍/ml, 또는 0.01 ㎍/ml 내지 1 ㎍/ml의 농도로 포함될 수 있으나, 이에 제한되지 않는다. 상기 퀘르시트린의 농도는 세포 독성을 나타내지 않으면서 미백 효능을 나타낼 수 있는 적절한 범위를 선택할 수 있다. The quercitrin contained in the triticale white leaf extract is 0.0001 μg/ml to 100 μg/ml, 0.0001 μg/ml to 10 μg/ml, 0.0001 μg/ml to 1 μg/ml, 0.001 μg/ml based on the total composition. to 100 μg/ml, 0.001 μg/ml to 10 μg/ml, 0.001 μg/ml to 1 μg/ml, 0.01 μg/ml to 100 μg/ml, 0.01 μg/ml to 10 μg/ml, or 0.01 μg/ml. It may be included at a concentration of ml to 1 μg/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.
상기 삼백초 흰 잎 추출물은 조성물 전체를 기준으로 0.0001 중량% 내지 20.0 중량%, 0.0001 중량% 내지 10.0 중량%, 0.0001 중량% 내지 5.0 중량%, 0.0001 중량% 내지 1.0 중량%, 0.001 중량% 내지 20.0 중량%, 0.001 중량% 내지 10.0 중량%, 0.001 중량% 내지 5.0 중량%, 0.001 중량% 내지 1.0 중량%, 0.01 중량% 내지 20.0 중량%, 0.01 중량% 내지 10.0 중량%, 0.01 중량% 내지 5.0 중량%, 또는 0.01 중량% 내지 1.0 중량%로 포함될 수 있으나, 이에 제한되지 않는다. 상기 삼백초 흰 잎 추출물의 함량은 세포 독성을 나타내지 않으면서 미백 효능을 나타낼 수 있는 적절한 범위를 선택할 수 있다.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.
일 구체예에서, 상기 조성물은 화장료 조성물일 수 있다.In one embodiment, the composition may be a cosmetic composition.
상기 화장료 조성물은 피부 미백용, 멜라닌 생성 억제용, 멜라닌 분비 억제용, 멜라닌 감소용, 또는 멜라닌 색소 과다 침착 억제용 일 수 있다.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.
상기 화장료 조성물은 본 명세서에 개시된 유효성분 이외에 화장료 조성물에 통상적으로 이용되는 성분들, 기능성 첨가물 등을 추가로 포함할 수 있으며, 예컨대 항산화제, 안정화제, 용해화제, 계면활성제, 분산제, 점증제, 방부제, 비타민, 안료, 향료 등과 같은 통상적인 보조제, 그리고 화장품학적으로 허용가능한 담체를 포함할 수 있다.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.
상기 화장료 조성물은 통상적으로 제조되는 어떠한 제형으로도 제조될 수 있다. 예를 들면, 상기 화장료 조성물은 화장수, 크림, 에센스, 클렌징 폼, 클렌징 워터, 팩, 앰플, 바디 로션, 바디 오일, 바디 젤, 샴푸, 린스, 헤어 컨디셔너, 헤어 젤, 파운데이션, 립스틱, 마스카라, 또는 메이크업 베이스의 화장료 제형을 갖는 것일 수 있다. The cosmetic composition may be prepared in any formulation that is conventionally prepared. For example, 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.
일 구체예에서, 상기 조성물은 피부 외용제 조성물일 수 있다.In one embodiment, the composition may be an external composition for skin.
상기 피부 외용제 조성물은 피부 미백용, 멜라닌 생성 억제용, 멜라닌 분비 억제용, 멜라닌 감소용, 멜라닌 색소 과다 침착 억제용, 또는 멜라닌 색소 과다 침착 질환의 예방, 치료 또는 개선용 일 수 있다.The 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.
상기 피부 외용제는 크림, 겔, 연고, 피부 유화제, 피부 현탁액, 경피전달성 패치, 약물 함유 붕대, 로션, 또는 그 조합일 수 있다. 상기 피부외용제는 통상 화장품이나 의약품 등의 피부외용제에 사용되는 성분, 예를 들면 수성성분, 유성성분, 분말성분, 알코올류, 보습제, 증점제, 자외선흡수제, 미백제, 방부제, 산화방지제, 계면활성제, 향료, 색제, 각종 피부 영양제, 또는 이들의 조합과 필요에 따라서 적절하게 배합될 수 있다. 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.
일 구체예에서, 상기 조성물은 약학적 조성물일 수 있다.In one embodiment, the composition may be a pharmaceutical composition.
상기 약학적 조성물은 피부 미백용, 멜라닌 생성 억제용, 멜라닌 분비 억제용, 멜라닌 감소용, 멜라닌 색소 과다 침착 억제용, 또는 멜라닌 색소 과다 침착 질환의 예방 또는 치료용 일 수 있다.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.
상기 약학적 조성물은 약제학적으로 허용가능한 희석제 또는 담체를 추가적으로 포함할 수 있다. 상기 희석제는 유당, 옥수수 전분, 대두유, 미정질 셀룰로오스, 또는 만니톨, 활택제로는 스테아린산 마그네슘, 탈크, 또는 그 조합일 수 있다. 상기 담체는 부형제, 붕해제, 결합제, 활택제, 또는 그 조합일 수 있다. 상기 부형제는 미결정 셀룰로오즈, 유당, 저치환도 히드록시셀룰로오즈, 또는 그 조합일 수 있다. 상기 붕해제는 카르복시메틸셀룰로오스 칼슘, 전분글리콜산 나트륨, 무수인산일수소 칼슘, 또는 그 조합일 수 있다. 상기 결합제는 폴리비닐피롤리돈, 저치환도 히드록시프로필셀룰로오즈, 히드록시프로필셀룰로오즈, 또는 그 조합일 수 있다. 상기 활택제는 스테아린산 마그네슘, 이산화규소, 탈크, 또는 그 조합일 수 있다.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.
상기 약학적 조성물은 경구 또는 비경구 투여 제형으로 제형화될 수 있다. 경구 투여 제형은 과립제, 산제, 액제, 정제, 캅셀제, 건조시럽제, 또는 그 조합일 수 있다. 비경구 투여 제형은 주사제일 수 있다.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.
일 구체예에서, 상기 조성물은 건강기능식품 조성물일 수 있다.In one embodiment, the composition may be a health functional food composition.
피부 미백용, 멜라닌 생성 억제용, 멜라닌 분비 억제용, 멜라닌 감소용, 멜라닌 색소 과다 침착 억제용, 또는 멜라닌 색소 과다 침착 질환의 예방 또는 개선용 일 수 있다.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.
상기 건강기능식품 조성물은 상기 추출물 단독, 또는 다른 식품 또는 식품 성분과 함께 사용될 수 있고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 유효 성분의 혼합양은 사용 목적 (예방, 건강 또는 치료적 처치)에 따라 적합하게 결정될 수 있다. 상기 건강기능식품의 종류에는 특별한 제한은 없다. 건강기능식품의 종류 중 음료 조성물은 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상기 천연 탄수화물은 포도당, 과당과 같은 모노사카라이드, 말토스, 슈크로스와 같은 디사카라이드, 및 덱스트린, 사이클로덱스트린과 같은 폴리사카라이드, 자일리톨, 소르비톨, 에리트리톨 등의 당알콜이다. 감미제로서는 타우마틴, 스테비아 추출물과 같은 천연 감미제나, 사카린, 아스파르탐과 같은 합성 감미제 등을 사용할 수 있다. 상기 건강기능식품 조성물은 또한 영양제, 비타민, 전해질, 풍미제, 착색제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알콜, 탄산 음료에 사용되는 탄산화제, 또는 그 조합을 함유할 수 있다. 상기 건강기능식품 조성물은 또한, 천연 과일쥬스, 과일쥬스 음료, 야채 음료의 제조를 위한 과육, 또는 그 조합을 함유할 수 있다.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). There is no particular limitation on the type of health functional food. Among the types of health functional foods, 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. As 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.
다른 양상은 삼백초 흰 잎 추출물을 제조하는 방법을 제공한다.Another aspect provides a method for preparing the white leaf extract of Sambaekcho.
상기 방법은 삼백초 흰 잎을 추출 용매와 인큐베이션하여 추출물을 수득하는 단계를 포함한다.The method includes obtaining an extract by incubating the white leaves of Sambaekcho with an extraction solvent.
상기 삼백초 흰 잎, 추출 용매 및 추출물에 관한 상세는 상술한 바와 같다.Details of the three hundred second white leaves, the extraction solvent and the extract are as described above.
상기 인큐베이션은 통상적인 추출 조건에서 수행될 수 있다. 상기 추출 조건에 관한 상세는 상술한 바와 같다.The incubation may be performed under conventional extraction conditions. Details of the extraction conditions are as described above.
상기 방법은 상기 수득된 추출물을 여과 및/또는 건조하는 단계를 더 포함할 수 있다. 상기 여과 및 건조는 공지된 통상적인 방법을 사용할 수 있다.The method may further include filtering and/or drying the obtained extract. For the filtration and drying, known conventional methods may be used.
다른 양상은 유효량의 삼백초 흰 잎 추출물을 포함하는 조성물을 이를 필요로 하는 개체에게 투여하는 단계를 포함하는 멜라닌 색소 과다 침착 질환을 예방 또는 치료하는 방법을 제공한다.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.
용어 "유효량"이란 상기에서 언급한 효과를 나타낼 수 있을 정도로 유효한 양을 의미한다.The term "effective amount" means an amount effective enough to exhibit the above-mentioned effects.
용어 "투여하는", "도입하는", 및 "이식하는"은 상호교환적으로 사용되고 일 구체예에 따른 조성물의 원하는 부위로의 적어도 부분적 국소화를 초래하는 방법 또는 경로에 의한 개체 내로의 일 구체예에 따른 조성물의 배치를 의미할 수 있다.The terms "administering," "introducing," and "implanting" are used interchangeably and are used interchangeably in accordance with one embodiment into a subject by a method or route that results in at least partial localization of a composition to a desired site. It may mean the arrangement of the composition according to.
투여는 당업계에 알려진 방법에 의하여 투여될 수 있다. 투여는 예를 들면, 정맥내, 근육내, 경구, 경피(transdermal), 점막, 코안(intranasal), 기관내(intratracheal) 또는 피하 투여와 같은 경로로, 임의의 수단에 의하여 개체로 직접적으로 투여될 수 있다. 상기 투여는 전신적으로 또는 국부적으로 투여될 수 있다. 상기 투여는 피부에 도포하는 것일 수 있다.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.
상기 개체는 포유동물, 예를 들면, 인간, 소, 말, 돼지, 개, 양, 염소, 또는 고양이일 수 있다. 상기 개체는 멜라닌 색소 과다 침착 질환의 예방 또는 치료를 필요로 하는 개체일 수 있다.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.
투여량은 제제화 방법, 투여 방식, 환자의 연령, 체중, 성별, 병적 상태, 음식, 투여 시간, 투여 경로, 배설 속도 및 반응 감응성과 같은 요인들에 의해 다양하게 처방될 수 있고, 당업자라면 이러한 요인들을 고려하여 투여량을 적절히 조절할 수 있다. 투여 횟수는 1일 1회 또는 임상적으로 용인가능한 부작용의 범위 내에서 2회 이상이 가능하고, 투여 부위에 대해서도 1개소 또는 2개소 이상에 투여할 수 있으며, 매일 또는 2 내지 5일 간격으로 총 투여 일수는 한번 치료 시 1일에서 30일까지 투여될 수 있다. 필요한 경우, 적정 시기 이후에 동일한 치료를 반복할 수 있다. 인간 이외의 동물에 대해서도, kg당 인간과 동일한 투여량으로 하거나, 또는 예를 들면 목적의 동물과 인간과의 기관(심장 등)의 용적비(예를 들면, 평균값) 등으로 상기의 투여량을 환산한 양을 투여할 수 있다.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. For non-human animals, 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.
다른 양상은 멜라닌 색소 과다 침착 질환의 예방 또는 치료용 약제를 제조하는 데 사용하기 위한, 삼백초 흰 잎 추출물의 용도를 제공한다.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.
중복되는 내용은 본 명세서의 복잡성을 고려하여 생락하며, 본 명세서에서 달리 정의되지 않은 용어들은 본 발명이 속하는 기술분야에서 통상적으로 사용되는 의미를 갖는 것이다.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.
일 양상에 따른 조성물은 삼백초 흰 잎 추출물을 포함함으로써 피부 미백, 멜라닌 생성 및 분비 억제, 및 멜라닌 색소 과다 침착 억제 효능을 가질 수 있다. 상기 삼백초 흰 잎 추출물은 삼백초 초록 잎 추출물에 비해 멜라닌 생성 및 분비 억제 효능, 및 피부 색소 침착 억제 효능이 우수하므로, 피부 미백을 위한 화장료 조성물 또는 약학적 조성물 등으로 이용될 수 있다.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.
도 1a는 실시예 1의 삼백초 흰 잎 추출물의 LC-QTOF-MS 분석 결과를 나타낸 것이다.Figure 1a shows the results of LC-QTOF-MS analysis of the white leaf extract of Sambaekcho of Example 1.
도 1b는 비교예 1의 삼백초 초록 잎 추출물의 LC-QTOF-MS 분석 결과를 나타낸 것이다.Figure 1b shows the results of LC-QTOF-MS analysis of the green leaf extract of Sambaekcho of Comparative Example 1.
도 2a 및 도 2b는 삼백초 흰 잎에 함유된 퀘르시트린의 MS 조각화 패턴이다.2a and 2b are MS fragmentation patterns of quercitrin contained in the white leaves of Sambaekcho.
도 3a 및 도 3b는 삼백초 흰 잎에 함유된 아프젤린의 MS 조각화 패턴이다.3a and 3b are MS fragmentation patterns of afgeline contained in the white leaves of Schiekcho.
도 4는 실시예 1, 비교예 1, 실시예 2 및 비교예 2의 세포 독성 시험 결과를 나타낸 것이다.Figure 4 shows the cytotoxicity test results of Example 1, Comparative Example 1, Example 2 and Comparative Example 2.
도 5는 삼백초 흰 잎 추출물에 함유된 퀘르시트린의 세포 독성 시험 결과를 나타낸 것이다.Figure 5 shows the results of the cytotoxicity test of quercitrin contained in the white leaf extract of Sambaekcho.
도 6은 삼백초 흰 잎 추출물에 함유된 아프젤린의 세포 독성 시험 결과를 나타낸 것이다.Figure 6 shows the results of the cytotoxicity test of afgeline contained in the white leaf extract of Sambaekcho.
도 7은 실시예 1, 비교예 1, 실시예 2 및 비교예 2의 멜라닌 생합성 결과를 나타낸 것이다.Figure 7 shows the melanin biosynthesis results of Example 1, Comparative Example 1, Example 2 and Comparative Example 2.
도 8은 삼백초 흰 잎 추출물에 함유된 퀘르시트린의 멜라닌 생합성 결과를 나타낸 것이다.Figure 8 shows the melanin biosynthesis results of quercitrin contained in the white leaf extract of Sambaekcho.
도 9는 실시예 1 및 비교예 1의 멜라닌 분비율 결과를 나타낸 것이다.9 shows the melanin secretion rate results of Example 1 and Comparative Example 1.
도 10은 삼백초 흰 잎 추출물에 함유된 퀘르시트린의 멜라닌 분비율 결과를 나타낸 것이다.10 shows the results of the melanin secretion rate of quercitrin contained in the white leaf extract of Sambaekcho.
도 11은 삼백초 흰 잎 추출물에 함유된 아프젤린의 PAR-2 발현 저해 효과를 나타낸 것이다.Figure 11 shows the PAR-2 expression inhibitory effect of afgeline contained in the white leaf extract of Sambaekcho.
이하 본 발명을 실시예를 통하여 보다 상세하게 설명한다. 그러나, 이들 실시예는 본 발명을 예시적으로 설명하기 위한 것으로 본 발명의 범위가 이들 실시예에 한정되는 것은 아니다.Hereinafter, the present invention will be described in more detail through examples. However, these examples are intended to illustrate the present invention by way of example, and the scope of the present invention is not limited to these examples.
실시예 1. 삼백초 흰 잎 추출물의 제조Example 1. Preparation of Sambaekcho white leaf extract
삼백초에서 흰 잎만을 분리하여 50% 에탄올로 구성 성분이 깨지지 않도록 3일간 상온 침지 추출하였다. 여과 후 여액을 농축하고 진공 건조하였다.Only the white leaves were separated from Sambaekcho and immersed in 50% ethanol for 3 days at room temperature so that the components were not broken. After filtration, the filtrate was concentrated and vacuum dried.
비교예 1. 삼백초 초록 잎 추출물의 제조Comparative Example 1. Preparation of Sambaekcho green leaf extract
삼백초에서 초록 잎만을 분리하여 50% 에탄올로 구성 성분이 깨지지 않도록 3일간 상온 침지 추출하였다. 여과 후 여액을 농축하고 진공 건조하였다.Only the green leaves were separated from Sambaekcho and immersed in 50% ethanol for 3 days at room temperature so that the components were not broken. After filtration, the filtrate was concentrated and vacuum dried.
실시예 2. 삼백초 흰 잎 열수추출물의 제조Example 2. Preparation of hot water extract of Sambaekcho white leaves
삼백초에서 흰 잎만을 분리하여 삼백초 흰 잎 원물 중량에 10배 중량에 해당하는 증류수를 첨가하고 혼합한 후, 90℃의 온도로 4시간 30분 동안 추출하였다. 얻어진 추출액을 여과지를 이용하여 여과를 한 다음, 여과액을 회전식 증발 건조기로 감압 농축하였다. 감압 농축이 진행된 여액에 남아있는 용매를 제거하기 위해 동결건조하여, 분말상의 삼백초 흰 잎 열수추출물을 수득하였다.After separating only the white leaves from 300 seconds, 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.
비교예 2. 삼백초 초록 잎 열수추출물의 제조Comparative Example 2. Preparation of hot-water extract of 300 seconds green leaves
삼백초에서 초록 잎만을 분리하여 삼백초 초록 잎 원물 중량에 10배 중량에 해당하는 증류수를 첨가하고 혼합한 후, 90℃의 온도로 4시간 30분 동안 추출하였다. 얻어진 추출액을 여과지를 이용하여 여과를 한 다음, 여과액을 회전식 증발 건조기로 감압 농축하였다. 감압 농축이 진행된 여액에 남아있는 용매를 제거하기 위해 동결건조하여, 분말상의 삼백초 초록 잎 열수추출물을 수득하였다.After separating only the green leaves from the three hundred seconds, 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.
실험예 1. 흰 잎과 초록 잎 추출물의 2차 대사산물 확인 및 그의 함량 비교Experimental Example 1. Identification of secondary metabolites of white leaf and green leaf extracts and comparison of their contents
실시예 1의 삼백초 흰 잎 추출물과 비교예 1의 삼백초 초록 잎 추출물의 2차 대사산물을 확인하고, 그의 함량을 비교하기 위한 실험을 하였다.Secondary metabolites of the white leaf extract of Sambaekcho of Example 1 and the green leaf extract of Sambaekcho of Comparative Example 1 were identified, and experiments were conducted to compare their contents.
먼저, 삼백초 흰 잎 추출물과 삼백초 초록 잎 추출물을 각각 50% 메탄올에 녹여 1 mg/mL 농도가 되도록 하였다. 이후 0.45 ㎛ PVDF (Polyamide Fluoride) 필터로 여과한 후, LC-QTOF-MS (liquid chromatography-quadrupole-time of flight mass spectrometry)로 분석하였다. LC-QTOF-MS 분석 결과를 도 1a 및 도 1b에 나타내었다. First, 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 μm 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.
도 1a 및 도 1b에 나타낸 바와 같이, 삼백초 초록 잎보다 흰 잎에 더 많이 함유되어 있다고 보이는 4개의 피크(peak)를 확인하였다. 4개의 피크에 대해 MS 조각화 패턴(fragmentation pattern)을 해석한 결과, 모두 플라보노이드 글리코시드(flavonoid glycoside)로 예상할 수 있었다.As shown in Figures 1a and 1b, it was confirmed that four peaks (peaks) appear to be contained more in the white leaves than the green leaves of 300 seconds. As a result of analyzing MS fragmentation patterns for the four peaks, all of them could be expected to be flavonoid glycosides.
상기 4종의 플라보노이드 글리코시드 중 주요하게 차이를 보이는 2개의 피크에 대한 MS 조각화 패턴을 도 2a 내지 도 2b 및 도 3a 내지 도 3b에 나타내었다. 또한, 상기 2개의 피크에 대한 MS 조각 데레플리케이션(dereplication) 결과를 표 1에 나타내었다.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.
RT (분)RT (minute) |
선구 이온 (Precursor ion) m/zPrecursor ion m/z | 생성 이온 (Product ion) m/zProduct ion m/z | 분자식molecular formula | 동정Sympathy |
9.769.76 |
471.0886 [M + Na]+ 449.0886 [M + H]+ 471.0886 [M + Na] + 449.0886 [M+H] + |
303.0499 [M - Rha + H]+ 303.0499 [M - Rha + H] + |
C21H20O11 C 21 H 20 O 11 | 퀘르시트린 (quercitrin)quercitrin |
12.8412.84 |
455.0952 [M + Na]+ 433.1118 [M + H]+ 455.0952 [M + Na] + 433.1118 [M+H] + |
287.0553 [M - Rha + H]+ 287.0553 [M - Rha + H] + |
C21H20O10 C 21 H 20 O 10 | 아프젤린 (afzelin)afzelin |
도 2a, 도 2b, 도 3a, 도 3b 및 표 1에 나타낸 바와 같이, 삼백초 초록 잎보다 흰 잎에 더 많이 함유되어 있다고 보이는 2개의 주요 피크는 퀘르시트린 및 아프젤린인 것으로 예상되었다. 퀘르시트린과 아프젤린의 표준품과 함께 측정하여 해당 성분을 확인하였으며, 이들은 초록 잎보다 흰 잎에 다량 함유되어 있음을 확인하였다.As shown in Figure 2a, Figure 2b, Figure 3a, Figure 3b and Table 1, the two main peaks that appear to be contained more in white leaves than in the green leaves of 300 seconds were expected to be quercitrin and afzelin. The corresponding components were confirmed by measuring with the standards of quercitrin and afzeline, and it was confirmed that they were contained in a large amount in white leaves rather than green leaves.
실험예 2. B16 멜라노마세포에 대한 세포독성 평가Experimental Example 2. Cytotoxicity evaluation on B16 melanoma cells
삼백초 흰 잎 및 초록 잎 추출물과 지표 성분 퀘르시트린의 B16 멜라노마세포에 대한 세포독성을 평가하였다.The cytotoxicity of the white leaf and green leaf extracts of Sambaekcho and the indicator component quercitrin on B16 melanoma cells was evaluated.
구체적으로, 6웰 플레이트에 멜라노마세포를 접종하여 24시간 배양한 뒤, α-MSH와 10% 소혈청이 함유된 새로운 DMEM 배지로 교체하고, 각 시료를 농도 별로 처리하여 72시간 배양하였다. 배양이 끝난 세포에 2.5 mg/ml의 MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) 용액을 10배 희석시킨 배지로 교체하여 반응시켰다. 그 후, 상등액을 제거하고 DMSO (dimethyl sulfoxide) 2 ml을 첨가하여 생성된 MTT-formazan 결정체를 용해시켜 ELISA reader로 570 nm에서 흡광도를 측정하였다. α-MSH를 처리한 것을 대조군으로 하였다. 세포 독성은 대조군과 비교하여 흡광도의 백분율로 표시하였으며, 그 결과는 표 2 및 표 3과 도 4 및 도 5에 나타내었다.Specifically, melanoma cells were inoculated in a 6-well plate and cultured for 24 hours, then replaced with new DMEM medium containing α-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 α-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.
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
세포생존율 (%)cell viability (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 100.48100.48 | 2.072.07 | 0.8560.856 | |
α-MSH 처리군α-MSH treatment group | 100.00100.00 | 3.733.73 | 1.0001.000 | |
α-MSH + 알부틴α- |
100100 | 94.3194.31 | 2.972.97 | 0.1080.108 |
α-MSH + 삼백초 흰 잎 추출물 (실시예 1)α-MSH + Sambaekcho white leaf extract (Example 1) | 0.0250.025 | 94.2994.29 | 0.340.34 | 0.0580.058 |
0.050.05 | 95.7595.75 | 0.820.82 | 0.1270.127 | |
0.10.1 | 93.5193.51 | 1.981.98 | 0.0560.056 | |
0.250.25 | 0.700.70 | 0.050.05 | 0.0000.000 | |
α-MSH + 삼백초 초록 잎 추출물 (비교예 1)α-MSH + Sambaekcho Green Leaf Extract (Comparative Example 1) |
0.0250.025 | 93.9793.97 | 1.301.30 | 0.0570.057 |
0.050.05 | 92.2492.24 | 0.860.86 | 0.0250.025 | |
0.10.1 | 86.0286.02 | 0.300.30 | 0.0030.003 | |
0.250.25 | 0.720.72 | 0.030.03 | 0.0000.000 | |
α-MSH + 삼백초 흰 잎 열수추출물 (실시예 2)α-MSH + Sambaekcho white leaf hot water extract (Example 2) | 0.0250.025 | 93.1193.11 | 1.101.10 | 0.0560.056 |
0.050.05 | 94.3194.31 | 0.560.56 | 0.0210.021 | |
0.10.1 | 92.0092.00 | 0.200.20 | 0.0120.012 | |
0.250.25 | 0.10.1 | 0.010.01 | 0.0120.012 | |
α-MSH + 삼백초 초록 잎 열수추출물 (비교예 2)α-MSH + hot water extract of Sambaekcho green leaf (Comparative Example 2) | 0.0250.025 | 92.8892.88 | 1.101.10 | 0.0550.055 |
0.050.05 | 91.5691.56 | 0.760.76 | 0.0250.025 | |
0.10.1 | 85.0185.01 | 0.400.40 | 0.0110.011 | |
0.250.25 | 0.120.12 | 0.010.01 | 0.0100.010 |
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
세포생존율 (%)cell viability (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 107.65107.65 | 4.024.02 | 0.0360.036 | |
α-MSH 처리군α-MSH treatment group | 100.00100.00 | 1.371.37 | 1.0001.000 | |
α-MSH + 알부틴α- |
100100 | 91.8191.81 | 0.800.80 | 0.0010.001 |
α-MSH + 퀘르시트린α-MSH + Quercitrin | 1One | 104.10104.10 | 2.822.82 | 0.0860.086 |
1010 | 102.96102.96 | 2.012.01 | 0.1030.103 | |
2525 | 108.81108.81 | 4.424.42 | 0.0300.030 | |
5050 | 110.19110.19 | 1.261.26 | 0.0010.001 | |
100100 | 104.85104.85 | 4.674.67 | 0.1600.160 | |
250250 | 85.9985.99 | 0.670.67 | 0.0000.000 |
표 2, 표 3, 도 4 및 도 5에 나타낸 바와 같이, 멜라노마 세포에서 실시예 1의 삼백초 흰 잎 추출물, 비교예 1의 삼백초 초록 잎 추출물, 실시예 2의 삼백초 흰 잎 열수추출물, 및 비교예 2의 삼백초 초록 잎 열수추출물은 모두 0.1 ㎍/ml 농도까지 독성을 나타내지 않았다. 또한, 지표성분인 퀘르시트린은 100 ㎍/ml 농도까지 독성을 나타내지 않았다.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 μg/ml. In addition, quercitrin, a marker component, showed no toxicity up to a concentration of 100 μg/ml.
실험예 3. 각질형성세포(HaCaT)에 대한 세포독성 평가Experimental Example 3. Evaluation of cytotoxicity to keratinocytes (HaCaT)
지표 성분 아프젤린의 각질형성세포(HaCaT)에 대한 세포독성을 평가하였다.The cytotoxicity of the indicator component afgeline on keratinocytes (HaCaT) was evaluated.
구체적으로, 24웰 플레이트에 각질형성세포 (HaCaT)를 접종하여 24시간 배양한 뒤, 배양된 세포의 배지를 무혈청(serum-free) 배지로 교체하고 시료를 농도 별로 처리하여 24시간 배양하였다. 배양이 끝난 세포에 2.5 mg/ml의 MTT 용액을 10배 희석시킨 배지로 교체하여 반응시켰다. 그 후, 상등액을 제거하고 DMSO 1 ml을 첨가하여 생성된 MTT-formazan 결정체를 용해시켜 ELISA reader로 570 nm에서 흡광도를 측정하였다. 무처리군을 대조군으로 하였다. 세포 독성은 대조군과 비교하여 흡광도의 백분율로 표시하였으며, 그 결과는 표 4 및 도 6에 나타내었다.Specifically, after inoculating keratinocytes (HaCaT) in a 24-well plate and culturing for 24 hours, 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.
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
세포생존율 (%)cell viability (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 107.65107.65 | 4.024.02 | 0.0360.036 | |
아프젤린Afgeline | 1One | 104.10104.10 | 2.822.82 | 0.0860.086 |
1010 | 102.96102.96 | 2.012.01 | 0.1030.103 | |
2525 | 108.81108.81 | 4.424.42 | 0.0300.030 | |
5050 | 110.19110.19 | 1.261.26 | 0.0010.001 | |
100100 | 104.85104.85 | 4.674.67 | 0.1600.160 | |
250250 | 85.9985.99 | 0.670.67 | 0.0000.000 |
표 4 및 도 6에 나타낸 바와 같이, 지표성분인 아프젤린은 각질형성세포에 대해 100 ㎍/ml 농도까지 독성을 나타내지 않았다.As shown in Table 4 and FIG. 6, afgeline, a marker component, showed no toxicity to keratinocytes up to a concentration of 100 μg/ml.
실험예 4. 멜라노마세포에서 단위 세포당 멜라닌 생합성을 억제하는 미백 효능 측정Experimental Example 4. Measurement of whitening efficacy of inhibiting melanin biosynthesis per unit cell in melanoma cells
삼백초 흰 잎 및 초록 잎 추출물과 지표성분 퀘르시트린의 멜라노마세포에서 단위 세포당 멜라닌 생합성을 억제하는 미백 효능을 측정하였다.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.
구체적으로, 6웰 플레이트에 멜라노마세포를 접종하여 24시간 배양한 뒤, α-MSH와 10% 소혈청이 함유된 새로운 DMEM 배지로 교체하고, 시료를 농도 별로 처리하여 72시간 배양하였다. 72시간 배양 후 배지로 분비된 멜라닌 양을 측정하기 위해 배지를 96웰 플레이트에 옮긴 후 450 nm에서 흡광도를 측정하여 단위 세포당 멜라닌 분비량을 구하였다. 그 후, 배지를 모두 제거한 세포를 PBS (phosphate-buffered saline) 2 ml로 세척하고, 1N NaOH 0.25 ml을 처리하여 세포를 1.5 ml 튜브로 수거하여 세포 내 멜라닌을 얻었다. 수거한 세포 용해물(lysate)을 60℃에서 30분 인큐베이션 한 후, 볼텍싱(Vortexing) 한 다음, 96웰 플레이트에 옮긴 후 450 nm에서 흡광도를 측정하여 단위 세포당 멜라닌 생성량을 구하였다. α-MSH 처리한 것을 대조군으로 하였으며, 양성대조군으로는 알부틴(arbutin, 제조사: HyundaiBioland)을 사용하였다. 단위 세포당 멜라닌 생합성 결과는 표 5 및 표 6과 도 7 및 도 8에 나타내었으며, 단위 세포당 멜라닌 분비율 결과는 표 7 및 표 8과 도 9 및 도 10에 나타내었다.Specifically, after inoculating melanoma cells in a 6-well plate and culturing for 24 hours, the medium was replaced with new DMEM medium containing α-MSH and 10% bovine serum, and the samples were treated by concentration and cultured for 72 hours. In order to measure the amount of melanin secreted into the medium after 72 hours of culture, 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. Thereafter, 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. 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. α-MSH treatment was used as a control group, and arbutin (manufacturer: Hyundai Bioland) was used as a positive control group. 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.
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
단위 세포당 멜라닌생성율 (%)Melanin production rate per unit cell (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 58.4258.42 | 2.712.71 | 0.0000.000 | |
α-MSH 처리군α-MSH treatment group | 100.00100.00 | 0.530.53 | 1.0001.000 | |
α-MSH + 알부틴α- |
100100 | 64.8264.82 | 2.332.33 | 0.0000.000 |
α-MSH + 삼백초 흰 잎 추출물 (실시예 1)α-MSH + Sambaekcho white leaf extract (Example 1) | 0.0250.025 | 88.2488.24 | 1.531.53 | 0.0000.000 |
0.050.05 | 73.0373.03 | 1.261.26 | 0.0000.000 | |
0.10.1 | 67.5567.55 | 3.603.60 | 0.0000.000 | |
α-MSH + 삼백초 초록 잎 추출물 (비교예 1)α-MSH + Sambaekcho green leaf extract (Comparative Example 1) | 0.0250.025 | 96.7996.79 | 1.831.83 | 0.0430.043 |
0.050.05 | 76.3976.39 | 0.710.71 | 0.0000.000 | |
0.10.1 | 76.1976.19 | 2.592.59 | 0.0000.000 | |
α-MSH + 삼백초 흰 잎 열수추출물 (실시예 2)α-MSH + Sambaekcho white leaf hot water extract (Example 2) | 0.0250.025 | 98.1298.12 | 2.122.12 | 0.0000.000 |
0.050.05 | 85.1285.12 | 1.111.11 | 0.0000.000 | |
0.10.1 | 79.9979.99 | 3.123.12 | 0.0000.000 | |
α-MSH + 삼백초 초록 잎 열수추출물 (비교예 2)α-MSH + hot water extract of Sambaekcho green leaf (Comparative Example 2) | 0.0250.025 | 99.1999.19 | 1.431.43 | 0.0430.043 |
0.050.05 | 88.3988.39 | 1.511.51 | 0.0000.000 | |
0.10.1 | 81.1981.19 | 0.010.01 | 0.0000.000 |
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
단위 세포당 멜라닌생성율 (%)Melanin production rate per unit cell (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 45.0445.04 | 2.472.47 | 0.0000.000 | |
α-MSH 처리군α-MSH treatment group | 100.00100.00 | 0.660.66 | 1.0001.000 | |
α-MSH + 알부틴α- |
100100 | 64.0764.07 | 1.461.46 | 0.0000.000 |
α-MSH + 퀘르시트린α-MSH + Quercitrin | 1One | 89.5889.58 | 1.151.15 | 0.0000.000 |
1010 | 92.9292.92 | 1.721.72 | 0.0030.003 | |
2525 | 82.0682.06 | 2.372.37 | 0.0000.000 | |
5050 | 80.0080.00 | 3.353.35 | 0.0010.001 | |
100100 | 84.4884.48 | 2.022.02 | 0.0000.000 |
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
단위 세포당 멜라닌분비율 (%)Melanin secretion rate per unit cell (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 58.0358.03 | 2.532.53 | 0.0000.000 | |
α-MSH 처리군α-MSH treatment group | 100.00100.00 | 2.232.23 | 1.0001.000 | |
α-MSH + 알부틴α- |
100100 | 73.5673.56 | 0.760.76 | 0.0000.000 |
α-MSH + 삼백초 흰 잎 추출물 (실시예 1)α-MSH + Sambaekcho white leaf extract (Example 1) | 0.0250.025 | 91.9791.97 | 7.187.18 | 0.1380.138 |
0.050.05 | 79.3079.30 | 1.691.69 | 0.0000.000 | |
0.10.1 | 69.3669.36 | 1.091.09 | 0.0000.000 | |
α-MSH + 삼백초 초록 잎 추출물 (비교예 1)α-MSH + Sambaekcho green leaf extract (Comparative Example 1) | 0.0250.025 | 100.29100.29 | 2.402.40 | 0.8850.885 |
0.050.05 | 79.6579.65 | 3.073.07 | 0.0010.001 | |
0.10.1 | 76.5276.52 | 0.880.88 | 0.0000.000 |
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
단위 세포당 멜라닌분비율 (%)Melanin secretion rate per unit cell (%) |
표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
무처리군untreated group | 47.7447.74 | 1.841.84 | 0.0000.000 | |
α-MSH 처리군α-MSH treatment group | 100.00100.00 | 0.750.75 | 1.0001.000 | |
α-MSH + 알부틴α- |
100100 | 69.1669.16 | 1.881.88 | 0.0000.000 |
α-MSH + 퀘르시트린α-MSH + Quercitrin | 1One | 93.9693.96 | 4.504.50 | 0.0830.083 |
1010 | 96.6396.63 | 2.462.46 | 0.0860.086 | |
2525 | 86.4186.41 | 2.262.26 | 0.0010.001 | |
5050 | 74.1274.12 | 1.131.13 | 0.0000.000 | |
100100 | 82.3682.36 | 1.491.49 | 0.0000.000 |
표 5 내지 8 및 도 7 내지 10에 나타낸 바와 같이, 삼백초 흰 잎 에탄올 추출물 및 초록 잎 에탄올 추출물은 α-MSH 로 인해 증가된 단위 세포당 멜라닌 생성율과 분비율을 농도의존적으로 감소시켰다. 특히, 삼백초 흰 잎 에탄올 추출물이 초록 잎 에탄올 추출물보다 단위 세포당 멜라닌 생성 및 분비 저해 효능이 뛰어난 것으로 확인되었다. 또한, 지표성분인 퀘르시트린도 단위 세포당 멜라닌 생성율과 분비율을 억제함으로써 멜라닌 생합성 및 분비 저해에 의한 미백 효능을 나타내는 것으로 판단되었다.As shown in Tables 5 to 8 and FIGS. 7 to 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 α-MSH in a concentration-dependent manner. In particular, it was confirmed that 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. In addition, it was determined that quercitrin, a marker component, also exhibits a whitening effect by inhibiting melanin biosynthesis and secretion by inhibiting melanin production and secretion per unit cell.
또한, 삼백초 흰 잎과 초록 잎 모두에서 열수추출물 대비 에탄올 추출물이 단위 세포당 멜라닌 생성율을 농도의존적으로 감소시키는 효과가 더 우수한 것으로 확인되었다. In addition, it was confirmed that the ethanol extract was more effective in concentration-dependently reducing the melanin production rate per unit cell than the hot water extract in both the white and green leaves of Sambaekcho.
실험예 5. 표피로 전달되는 멜라노좀을 억제하여 피부 색소 침착을 저해하는 미백 효능 측정Experimental Example 5. Measurement of whitening efficacy to inhibit skin pigmentation by inhibiting melanosomes delivered to the epidermis
지표 성분 아프젤린의 멜라노좀 억제에 의한 피부 색소 침착 저해 효능을 측정하였다.The effect of inhibiting skin pigmentation by inhibiting melanosomes of the indicator component afzeline was measured.
멜라노사이트(Melanocyte)에서 표피로 멜라노좀이 전달되는 과정인 멜라노좀 전달(melanosome transfer)에는 다양한 메커니즘이 있는데, 이 중 핵심매개인자인 PAR-2 (protease-activated receptor-2)에 의한 식세포작용(phagocytosis)이 가장 많이 알려져 있다. 이러한 PAR-2의 발현을 저해시킴으로써 표피로 전달되는 멜라노좀을 억제하여 피부 색소 침착을 저해하는 미백 효능을 확인하였다(Eun-Jung CHOI at al, Macelignan Inhibits Melanosome Transfer Mediated by Protease-Activated Receptor-2 in Keratinocytes, Biol. Pharm. Bull. 34(5) 748-754, 2011).Melanosome transfer, the process by which melanosomes are transferred from melanocytes to the epidermis, has various mechanisms, among which phagocytosis by PAR-2 (protease-activated receptor-2), phagocytosis) is the most well known. By inhibiting the expression of PAR-2, the whitening effect of inhibiting skin pigmentation by suppressing melanosomes transferred to the epidermis was confirmed (Eun-Jung CHOI at al, Macelignan Inhibits Melanosome Transfer Mediated by Protease-Activated Receptor-2 in Keratinocytes, Biol. Pharm. Bull. 34(5) 748-754, 2011).
60 mm 배양 디쉬 (corning)에 각질형성세포(HaCaT)를 접종하여 24시간 배양한 뒤, HBSS (Hank's Buffered Salt Solution)로 세척을 2번 한 다음, HBSS를 넣고 UVB 30 mJ/㎠ 를 조사하였다. 그 후, 무혈청(serum-free) 배지로 교체하고, 각 시료를 농도 별로 처리하여 8시간 동안 배양 후, 세포를 QIAzol쪠 Lysis Reagent (Qiagen)로 모아 제조사의 방법에 따라 RNA를 분리하였다. 분리된 RNA를 정량한 뒤 1 μg의 RNA로 cDNA를 합성하여 Real-time PCR을 실시하였다. PCR에 사용된 PAR-2, β-Actin 프라이머는 코스모진텍사(Korea)에서 합성하여 사용하였으며, 그 프라이머 서열은 표 9에 나타내었다. UVB 조사한 것을 대조군으로 하였으며, 양성대조군으로는 나이아신아마이드(niacinamide, 제조사: Sigma)을 사용하였다. PAR-2 발현 결과는 표 10 및 도 11에 나타내었다.Keratinocytes (HaCaT) 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 μg of RNA. The PAR-2 and β-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.
프라이머primer | 서열order | 서열번호sequence number | |
PAR-2PAR-2 | 정방향forward | 5'- TGC TAG CAG CCT CTC TCT CC -3'5'-TGC TAG CAG CCT CTC TCT CC -3' | 1One |
역방향reverse | 5'- CCA GTG AGG ACA GAT GCA GA -3'5'- CCA GTG AGG ACA GAT GCA GA -3' | 22 | |
β-Actinβ-Actin | 정방향forward | 5'-GGC ACC CAG CAC AAT GAA G -3'5'-GGC ACC CAG CAC AAT GAA G -3' | 33 |
역방향reverse | 5'-CCG ATC CAC ACG GAG TAC TTG -3'5'-CCG ATC CAC ACG GAG TAC TTG -3' | 44 |
시험군test group |
실험농도 (μg/ml)Experimental Concentration (μg/ml) |
PAR-2 mRNA 발현율 (%)PAR-2 mRNA expression rate (%) | 표준편차 (Stdev.)standard deviation (Stdev.) | P-값P-value |
비조사군non-irradiation group | 56.1156.11 | 2.432.43 | 0.0000.000 | |
UVB 30 mJ/㎠ |
100.00100.00 | 0.000.00 | 1.0001.000 | |
UVB + 나이아신아마이드UVB + |
100100 | 67.9067.90 | 3.293.29 | 0.0000.000 |
UVB + 아프젤린UVB + |
5050 | 109.05109.05 | 4.804.80 | 0.0370.037 |
100100 | 81.2481.24 | 6.646.64 | 0.0130.013 | |
250250 | 77.9977.99 | 4.484.48 | 0.0010.001 |
표 10 및 도 11에 나타낸 바와 같이, 지표성분인 아프젤린을 각질형성세포에 처리하면 UVB로 인해 증가된 PAR-2 발현을 저해하는 것을 확인하였다. 이를 통해 지표성분 아프젤린은 표피로 전달되는 멜라노좀을 억제하여 피부 색소 침착을 저해하는 미백 효능을 나타내는 것으로 확인되었다.As shown in Table 10 and FIG. 11, it was confirmed that treatment of keratinocytes with afgeline, which is an indicator component, inhibited the increased PAR-2 expression due to UVB. Through this, it was confirmed that the indicator component afzeline inhibits melanosomes transmitted to the epidermis and exhibits a whitening effect that inhibits skin pigmentation.
Claims (12)
- 삼백초 흰 잎 추출물을 유효성분으로 포함하는 피부 미백용 화장료 조성물.A cosmetic composition for skin whitening comprising a white leaf extract of Sambaekcho as an active ingredient.
- 청구항 1에 있어서, 상기 추출물의 추출 용매는 물, C1 내지 C4의 알코올, 또는 이들의 혼합물인 것인 피부 미백용 화장료 조성물.The cosmetic composition for skin whitening according to claim 1, wherein the extraction solvent of the extract is water, C1 to C4 alcohol, or a mixture thereof.
- 청구항 1에 있어서, 상기 추출물의 추출 용매는 10%(v/v) 내지 90%(v/v) 에탄올인 것인 피부 미백용 화장료 조성물.The cosmetic composition for skin whitening according to claim 1, wherein the extraction solvent of the extract is 10% (v/v) to 90% (v/v) ethanol.
- 청구항 1에 있어서, 상기 삼백초 흰 잎 추출물은 삼백초 초록 잎 추출물에 비해 높은 피부 미백 효능을 갖는 것인 피부 미백용 화장료 조성물.The cosmetic composition for skin whitening according to claim 1, wherein the white leaf extract of Sambaekcho has a higher skin whitening effect than the green leaf extract of Sambaekcho.
- 청구항 1에 있어서, 상기 추출물은 퀘르시트린(quercitrin) 및 아프젤린(afzelin) 중 어느 하나 이상을 포함하는 것인 피부 미백용 화장료 조성물. The cosmetic composition for skin whitening according to claim 1, wherein the extract contains at least one of quercitrin and afzelin.
- 청구항 1에 있어서, 멜라닌 생성 또는 분비를 저해하는 것인 피부 미백용 화장료 조성물.The cosmetic composition for skin whitening according to claim 1, which inhibits melanin production or secretion.
- 청구항 1에 있어서, 멜라노좀 전달에 관여하는 PAR-2(protease-activated receptor-2)의 발현을 저해하는 것인 피부 미백용 화장료 조성물.The cosmetic composition for skin whitening according to claim 1, which inhibits the expression of PAR-2 (protease-activated receptor-2) involved in melanosome transmission.
- 삼백초 흰 잎 추출물을 유효성분으로 포함하는 멜라닌 색소 과다 침착 질환의 예방 또는 치료용 약학적 조성물.A pharmaceutical composition for the prevention or treatment of hypermelanin hyperpigmentation disease comprising an extract of the white leaf of Sambaekcho as an active ingredient.
- 청구항 8에 있어서, 상기 멜라닌 색소 과다 침착 질환은 주근깨(freckle); 기미(melasma); 간반(chloasma); 검버섯(liver spot); 모반(nevus); 일광흑자(solar lentigo); 흑피증(melanosis); 포이츠-예거 증후군(peutz-jegher's syndrome); 임신성 갈색반(chloasma gravidarum); 약물 사용 후 과다색소침착; 및 염증 후 과다색소침착(postinflammatory hyperpigmentation) 중에서 선택된 어느 하나인 것인, 멜라닌 색소 과다 침착 질환의 예방 또는 치료용 약학적 조성물.The method according to claim 8, wherein the melanin hyperpigmentation disease is freckles (freckle); melasma; chloasma; liver spots; nevus; solar lentigo; melanosis; peutz-jegher's syndrome; gestational brown spots (chloasma gravidarum); hyperpigmentation after drug use; And post-inflammatory hyperpigmentation (postinflammatory hyperpigmentation) of any one selected from, a pharmaceutical composition for the prevention or treatment of melanin hyperpigmentation disease.
- 삼백초 흰 잎 추출물을 유효성분으로 포함하는 멜라닌 색소 과다 침착 질환의 예방 또는 개선용 건강기능식품 조성물.A health functional food composition for preventing or improving melanin hyperpigmentation disease, comprising an extract of white leaves of Sambaekcho as an active ingredient.
- 유효량의 삼백초 흰 잎 추출물을 포함하는 조성물을 이를 필요로 하는 개체에게 투여하는 단계를 포함하는 멜라닌 색소 과다 침착 질환을 예방 또는 치료하는 방법.A method for preventing or treating hypermelanin hyperpigmentation disease comprising administering to a subject in need thereof a composition comprising an effective amount of a white leaf extract.
- 멜라닌 색소 과다 침착 질환의 예방 또는 치료용 약제를 제조하는 데 사용하기 위한, 삼백초 흰 잎 추출물의 용도.Use of an extract of the white leaf of Sambaekcho for use in preparing a medicament for the prevention or treatment of hypermelanin hyperpigmentation disease.
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KR20070087552A (en) * | 2004-12-17 | 2007-08-28 | 가부시키가이샤 시세이도 | Skin whitening preparation for external use, whitening preparation, whitening method and method of producing skin whitening preparation for external use |
KR20100086728A (en) * | 2009-01-23 | 2010-08-02 | (주)아모레퍼시픽 | Cosmetic composition for skin whitening |
KR20150023601A (en) * | 2015-02-03 | 2015-03-05 | (주)아모레퍼시픽 | Composition Containing Extracts of Saururus chinensis |
KR101993699B1 (en) * | 2017-04-19 | 2019-06-28 | 주식회사 진켐 | Composition for improving skin |
KR102202554B1 (en) * | 2019-07-23 | 2021-01-14 | 주식회사 현대바이오랜드 | Skin whitening cosmetic composition with the extract of Saururus chinensis leaf, the extract of Grape seed, the extract of Portulaca oleracea and rice fermented product |
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KR20070087552A (en) * | 2004-12-17 | 2007-08-28 | 가부시키가이샤 시세이도 | Skin whitening preparation for external use, whitening preparation, whitening method and method of producing skin whitening preparation for external use |
KR20100086728A (en) * | 2009-01-23 | 2010-08-02 | (주)아모레퍼시픽 | Cosmetic composition for skin whitening |
KR20150023601A (en) * | 2015-02-03 | 2015-03-05 | (주)아모레퍼시픽 | Composition Containing Extracts of Saururus chinensis |
KR101993699B1 (en) * | 2017-04-19 | 2019-06-28 | 주식회사 진켐 | Composition for improving skin |
KR102202554B1 (en) * | 2019-07-23 | 2021-01-14 | 주식회사 현대바이오랜드 | Skin whitening cosmetic composition with the extract of Saururus chinensis leaf, the extract of Grape seed, the extract of Portulaca oleracea and rice fermented product |
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