WO2021215882A1 - Composition pour prévenir la chute des cheveux ou favoriser la pousse des cheveux comprenant un extrait de péricarpe de camélia en tant que principe actif - Google Patents

Composition pour prévenir la chute des cheveux ou favoriser la pousse des cheveux comprenant un extrait de péricarpe de camélia en tant que principe actif Download PDF

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WO2021215882A1
WO2021215882A1 PCT/KR2021/005186 KR2021005186W WO2021215882A1 WO 2021215882 A1 WO2021215882 A1 WO 2021215882A1 KR 2021005186 W KR2021005186 W KR 2021005186W WO 2021215882 A1 WO2021215882 A1 WO 2021215882A1
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hair
camellia
composition
hair loss
active ingredient
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PCT/KR2021/005186
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English (en)
Korean (ko)
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유지영
정은선
박덕훈
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바이오스펙트럼 주식회사
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Publication of WO2021215882A1 publication Critical patent/WO2021215882A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/82—Theaceae (Tea family), e.g. camellia
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat

Definitions

  • the present invention relates to a composition for preventing hair loss or promoting hair growth comprising a camellia peel extract as an active ingredient. More specifically, a camellia peel extract, which promotes hair growth by inducing proliferation of dermal papilla cells, and inhibits the activity of 5-alpha reductase to inhibit dihydrotestosterone production, thereby preventing hair loss and promoting hair growth. It relates to a cosmetic composition, a pharmaceutical composition, and a food composition including as an active ingredient.
  • Hair loss which was previously thought to be a part of aging, has become one of the causes that have the greatest influence on appearance since it appears at a high rate in young people in modern society.
  • the age of hair loss onset was about 50% in their 20s and 30s, 29.8 years old for men and 33.6 years old for women, and only 224,688 people were treated for hair loss in 2018.
  • the domestic hair loss treatment market is approaching 4 trillion won, including treatments, medical devices, shampoos, and herbal medicines.
  • causes of hair loss include an unbalanced diet and anemia due to iron deficiency, side effects of medications, use of strong chemical products such as dyes or perms, hormonal changes, decreased thyroid function, stress, hair handling habits, depression, extreme temperature changes Various factors such as changing seasons are known.
  • Types of hair loss are divided into scarring alopecia, in which the hair is not regenerated due to the destruction of the hair follicles due to scarring, and non-scarring alopecia, in which the hair is regenerated after the symptom site disappears because the hair follicle is maintained without scar formation.
  • the application of hair loss treatment or prevention agents focuses on scarring alopecia.
  • a product that prevents hair loss along with hair growth is called an anti-hair loss agent, and a hair growth agent that supplies nutrients to the hair root to make hair grow, a hair restorer that promotes blood circulation in the scalp to help prevent hair loss, and turns thin soft hair into healthy terminal hair. It is defined as a hair-forming agent (JY Lim et al ., Kor. J. Aesthet. Cosmetol ., 12(6):767-772, 2014).
  • Androgenetic alopecia in which male hormones act as an important etiology among scar alopecia, accounts for about 80% of all hair loss symptoms.
  • DHT 5-alpha dihydrotestosterone
  • DHT 5-alpha dihydrotestosterone
  • DHT 5-alpha dihydrotestosterone
  • Well-known anti-hair loss agents include minoxidil for external skin application approved by FDA, finasteride for oral use, and dutasteride approved by Korea's MFDS. Although there is strong speculation that minoxidil will follow the mechanism of supplying nutrients to hair follicles by dilating blood vessels through hyperpolarization of cell membranes, research results also announced that it can activate beta-catenin signaling, a representative proliferation mechanism, by acting directly on human hair follicle cells. (Kwack MH et al., J Dermatol Sci. , 62(3):154-159, 2011).
  • Finasteride and dutasteride have a known mechanism of inhibiting the production of DHT that causes hair loss by inhibiting 5-alpha reductase (5 ⁇ -Reductase) that changes testosterone to DHT (Yamana K et al., Horm Mol Biol Clin Investig. , 1,2(3):293-299, 2010; Clark RV et al., J Clin Endocrinol Metab. , 89(5):2179-2184, 2004).
  • 5-alpha reductase 5 ⁇ -Reductase
  • the main mechanisms of hair loss prevention agents include a method of activating the proliferation of human dermal papilla cells and related signaling mechanisms, and a method of lowering the production rate of DHT through the inhibition of the aforementioned 5-alpha reductase.
  • the dermal papilla cells are not only important for the development and growth of hair follicles, but are also cells with multipotency. Hair growth is largely divided into anagen, degenerative, telogen, and developmental phases, and overall hair growth occurs while dermal papilla cells proliferate during the anagen phase (Driskell RR et al., J Cell Sci. , 15;124(Pt8):1179). -1182, 2011).
  • FGF-7 which increases the growth phase
  • ERK activity which induces cell growth
  • beta-catenin mechanism which leads to the development of hair follicles
  • Akt activity which inhibits apoptosis
  • Camellia japonica ( Camillia japonica ) is an evergreen arboreal tree belonging to the family Cactaceae, and numerous horticultural varieties have been made and most have been used as ornamental trees or as camellia oil extracted from seeds.
  • the camellia flower contains leucoanthocyanin and anthocyanin, which have excellent physiological activity, and the fruit contains fatty oil, camelin, and thachysaponin.
  • Camellia oil which has been widely used as a hair oil since ancient times, contains about 80% of omega-9 oleic acid, and also contains polyphenols, vitamins A, C, D, E and other antioxidants. is known to do These secondary metabolites are known to have the effects of strengthening the heart, yanghyeol, hemostasis, live fish, and small bells.
  • Korean Patent No. 10-1672431 discloses the cardiovascular disease prevention effect of camellia extract
  • Korean Patent No. 10-1408019 discloses the antioxidant and whitening effect of camellia fruit extract
  • Korean Patent Registration Nos. 10-1547920 and 10-1452320 disclose the hair loss improvement effect of camellia oil, but there is no information on the hair loss prevention effect of Camellia japonica pericarp extract yet.
  • the present inventors conducted a study to find a natural anti-aging agent through activation of beta-catenin mechanism involved in the proliferation of dermal papilla cells and development of hair follicles, and inhibition of 5-alpha reductase. It was found that the present invention was completed accordingly.
  • Another object of the present invention is to provide a pharmaceutical composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • Another object of the present invention is to provide a food composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • the present invention provides a cosmetic composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • the present invention provides a pharmaceutical composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • the present invention provides a food composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • the composition for preventing hair loss or promoting hair growth containing the extract of the camellia peel of the present invention as an active ingredient, has excellent human safety due to no skin irritation and cytotoxicity, and promotes proliferation of dermal papilla cells by activating the Wnt signal transduction process, and dihydrotestosterone Since it is very effective in inhibiting the production of hair loss, it can be usefully used as an active ingredient in a cosmetic composition, pharmaceutical composition or food composition for preventing hair loss and promoting hair growth.
  • FIG. 1 is a graph showing the analysis of the dermal papilla cell proliferation effect by the extract of the camellia peel of the present invention.
  • Figure 2 is a graph showing the inhibitory effect of 5-alpha reductase activity by the extract of camellia bark of the present invention.
  • FIG. 3 is a graph showing the degree of Wnt signaling activation by camellia peel extract of the present invention.
  • the present invention relates to a composition for preventing hair loss or promoting hair growth comprising a camellia peel extract as an active ingredient. More specifically, it relates to a cosmetic composition, a pharmaceutical composition, and a food composition comprising an ethanol extract of camellia peel as an active ingredient, wherein the composition has excellent human safety due to no skin irritation and cytotoxicity, while activating the Wnt signaling process.
  • the present invention provides a cosmetic composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • camellia japonica is an evergreen tree belonging to the family Chamophyllaceae, and numerous horticultural varieties have been made and most have been used as ornamental trees or as camellia oil extracted from seeds.
  • pericarp ( ⁇ , pericarp) refers to the rest of the camellia fruit except for seeds.
  • extract in the present invention refers to a liquid component obtained by immersing a target substance in various solvents, and then extracting and fractionating it for a certain time at room temperature or a warm state, and removing the solvent from the liquid component. It means the result of one solid content, etc. In addition, in addition to the result, it can be comprehensively interpreted as including all of the diluent of the result, the concentrate thereof, the prepared product thereof, the purified product, and the like.
  • the camellia peel extract can be obtained by extraction with water or various organic solvents.
  • the organic solvent used is not particularly limited thereto, as long as an extract having an effect of preventing hair loss or promoting hair growth can be obtained, but preferably water, a polar solvent or a non-polar solvent, and more preferably water, A lower alcohol having 1 to 4 carbon atoms (ethanol, methanol, propanol or butanol, etc.), a mixed solvent thereof, etc. may be used, and ethanol may be used most preferably.
  • the method for obtaining the extract is also not particularly limited thereto, as long as it can obtain an extract having an effect of preventing hair loss or promoting hair growth.
  • the extraction method includes cold-chill extraction, ultrasonic extraction, or reflux cooling extraction method, and it is preferable to perform the ultrasonic extraction method.
  • the ultrasonic extraction is a method of extracting useful components from various natural materials at room temperature by physical force rather than chemical force using a vibration element with a frequency of 20,000 times per second, solvent extraction, vegetable oil extraction, or steam distillation extraction Unlike this, it has the advantage of being able to extract at a high concentration without destroying the active ingredients contained in natural materials at room temperature.
  • the ultrasonic extraction may be carried out for 24 hours to 72 hours at room temperature using a 60% to 80% ethanol solution of dried camellia peel powder. Preferably, it is carried out for 36 hours to 60 hours at room temperature using a 65% to 75% ethanol solution, and more preferably, it is carried out for 48 hours at room temperature using a 70% ethanol solution. If it exceeds the lower limit of the above numerical value, the active ingredient of the present invention contained in the camellia peel is not sufficiently extracted. will do
  • the obtained camellia peel extract is not limited thereto, but may be concentrated under reduced pressure using a vacuum concentrator or a vacuum rotary evaporator.
  • concentration under reduced pressure but not limited thereto, it may be dried through freeze drying, reduced pressure drying, vacuum drying, boiling drying, or spray drying.
  • hair loss refers to a state in which there is no hair in a region where hair should normally exist, and specifically refers to the loss of hair (thick and dark hair) of the scalp.
  • the cause of hair loss is not limited, but there are, for example, hereditary androgenic alopecia (baldness), alopecia areata, ringworm of the head due to fungal infection, telogen hair loss, hair growth wall, hair growth disorder disease, etc. may mean hair loss due to lupus, folliculitis solitary, lichen planus pilaris, hair loss due to burns and trauma.
  • prevention of the present invention means preventing any thing or phenomenon from occurring, and in the present invention, preventing hair loss means preventing hair loss from occurring.
  • hair growth means that hair grows in the hair follicle.
  • the hair includes hair roots and hair follicles of the head, hair and eyelashes, eyebrows, beards, armpits, pubic hair, and all parts of the body where there are hair roots and hair follicles.
  • the hair loss prevention or hair growth promoting effect may be achieved by promoting the proliferation of dermal papilla cells, inhibiting the activity of 5-alpha reductase, and activating the signal transduction pathway of Wnt-beta catenin by the extract. .
  • the proliferation effect of dermal papilla cells in order to confirm the hair loss prevention or hair growth promoting effect of the camellia peel extract, the proliferation effect of dermal papilla cells, the inhibitory effect of 5-alpha reductase activity, and the degree of activation of Wnt-beta catenin signaling were analyzed.
  • the camellia peel extract promoted the proliferation of dermal papilla cells, excellently inhibited the activity of 5-alpha reductase in a concentration-dependent manner, and effectively activated the Wnt-beta-catenin signaling pathway (FIGS. 3).
  • the camellia peel extract provided in the present invention activates the signal transduction pathway of Wnt-beta-catenin to induce proliferation of dermal papilla cells, thereby promoting hair growth, and dihydrotestosterone, which is one of the causes of hair loss. It is possible to prevent hair loss by inhibiting the activity of 5 alpha reductase, which converts it from testosterone. Accordingly, the camellia peel extract of the present invention can be usefully used as an active ingredient in a cosmetic composition, a pharmaceutical composition or a food composition for preventing hair loss and promoting hair growth.
  • the "cosmetic composition” includes hair tonic, hair cream, hair lotion, hair shampoo, hair conditioner, hair conditioner, hair spray, hair aerosol, pomade, powder, gel, sol gel, emulsion, oil, wax and aerosol. It can be selected from cosmetics for hair consisting of.
  • the cosmetic composition may include a conventional auxiliary or cosmetically acceptable carrier such as a stabilizer, a solubilizer, a vitamin, a pigment, and a fragrance commonly used in the field of cosmetic compositions.
  • a conventional auxiliary or cosmetically acceptable carrier such as a stabilizer, a solubilizer, a vitamin, a pigment, and a fragrance commonly used in the field of cosmetic compositions.
  • the cosmetic composition may include a moisturizing agent, an anti-inflammatory agent, an antibacterial agent, an antifungal agent, a vitamin, a sunscreen agent, an antibiotic, a perfume, and a dye, if necessary.
  • the cosmetic composition may be prepared in any conventionally prepared formulation, for example, a solution, emulsion, suspension, paste, cream, lotion, gel, powder, spray, surfactant-containing cleansing, oil, It may be formulated as soap, liquid detergent, bath agent, foundation, makeup base, essence, lotion, foam, pack, softening water, sunscreen cream or sun oil, but is not limited thereto.
  • a solvent, solubilizer or emulsifier is used as a carrier component, for example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 ,3-butylglycol oil, glycerol fatty esters, fatty acid esters of polyethylene glycol or sorbitan.
  • the formulation of the present invention is a suspension
  • a liquid diluent such as water, ethanol or propylene glycol
  • a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol esters and polyoxyethylene sorbitan esters, microcrystals Sex cellulose, aluminum metahydroxide, bentonite, or tracanth may be used.
  • the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as a carrier component.
  • lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and in particular, in the case of a spray, additional chlorofluorohydrocarbon, propane /may contain propellants such as butane or dimethyl ether.
  • the formulation of the present invention is a surfactant-containing cleansing agent
  • Ether sulfate, alkylamidobetaine, aliphatic alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative or ethoxylated glycerol fatty acid ester may be used.
  • the carrier may be a non-naturally occurring carrier.
  • the present invention provides a pharmaceutical composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • camellia fruit skin extract The effect of preventing hair loss and promoting hair growth of the camellia fruit skin extract is as described above.
  • the term "pharmaceutical composition” refers to one prepared for the purpose of preventing or treating a disease, and each can be formulated in various forms according to a conventional method and used. For example, it can be formulated in oral dosage forms such as powders, granules, tablets, capsules, suspensions, emulsions, syrups, and aerosols, and diluents or excipients such as lubricants, wetting agents, flavoring agents, emulsifying agents, suspending agents, preservatives, surfactants, etc.
  • the composition of the present invention can be used by a method such as applying or dispersing directly to the hair or scalp.
  • the hair to which the composition of the present invention is applied includes hair roots and follicles of the head, hair and eyelashes and eyebrows, beard, armpits, pubic hair, hair roots throughout the body, and all areas with hair follicles.
  • each formulation it may be prepared by further including a carrier known in the art, such as a pharmaceutically acceptable carrier, such as a buffer, an analgesic agent, a solubilizer, an isotonic agent, a stabilizer, a base, and the like.
  • a pharmaceutically acceptable carrier such as a buffer, an analgesic agent, a solubilizer, an isotonic agent, a stabilizer, a base, and the like.
  • pharmaceutically acceptable carrier may refer to a carrier or diluent that does not inhibit the biological activity and properties of the injected active ingredient without stimulating the organism.
  • the type of carrier usable in the present invention is not particularly limited, and any carrier commonly used in the art and pharmaceutically acceptable may be used.
  • Non-limiting examples of the carrier include saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, dextrose solution, maltodextrin solution, glycerol, ethanol, and the like. These may be used alone or in mixture of two or more.
  • the carrier may be a non-naturally occurring carrier.
  • the composition of the present invention can be administered in a pharmaceutically effective amount.
  • the pharmaceutically effective amount means an amount sufficient to treat a disease with a reasonable benefit/risk ratio applicable to medical treatment and not to cause side effects, and the effective dose level is determined by the patient's health condition, disease type, severity, The activity of the drug, sensitivity to the drug, administration method, administration time, administration route and excretion rate, treatment period, factors including drugs used in combination or concurrently, and other factors well known in the medical field may be determined according to factors. Specifically, it is generally 0.01 mg to 5000 mg per day per 1 kg of body weight of the administered subject, and may be administered in divided doses once or several times a day at regular time intervals according to the judgment of a doctor or pharmacist, but is not limited thereto.
  • the content of the camellia peel extract included in the composition is not particularly limited thereto, but is 0.00001 to 100% by weight, preferably 0.0001 to 15% by weight, more preferably 0.001 to 15% by weight, even more preferably based on the total weight of the composition. It may be included in an amount of 0.001 to 10% by weight.
  • composition of the present invention may be used alone or in combination with other pharmaceutically active compounds exhibiting the effect of preventing or improving hair loss-related diseases or in an appropriate group.
  • the pharmaceutical composition of the present invention may be administered as an individual therapeutic agent or may be administered in combination with other therapeutic agents, and may be administered sequentially or simultaneously with conventional therapeutic agents. and may be administered single or multiple. Taking all of the above factors into consideration, it is important to administer an amount that can obtain the maximum effect with a minimum amount without causing side effects, and can be easily determined by those skilled in the art.
  • the term "administration” means introducing the pharmaceutical composition of the present invention to an individual by any suitable method, and the administration route of the composition of the present invention is oral or parenteral as long as it can reach the target tissue. It can be administered through
  • the method of administration of the pharmaceutical composition according to the present invention is not particularly limited, and may follow a method commonly used in the art.
  • the composition may be administered by oral administration or parenteral administration.
  • the composition of the present invention can be used by a method such as applying or dispersing directly to the hair or scalp.
  • the pharmaceutical composition according to the present invention may be prepared in various dosage forms according to the desired administration method.
  • the frequency of administration of the composition of the present invention is not particularly limited thereto, but may be administered once a day or administered several times by dividing the dose.
  • the present invention provides a method for preventing, improving or treating hair loss-related diseases, comprising administering a pharmaceutical composition comprising a camellia peel extract.
  • the term "individual” may mean any animal, including humans, that has or is likely to develop a hair loss-related disease.
  • the animal may be a mammal, such as a cow, a horse, a sheep, a pig, a goat, a camel, an antelope, a dog, a cat, and the like, in need of treatment for symptoms similar to those of a human, but is not limited thereto.
  • the prevention or treatment method of the present invention may include administering the composition in a pharmaceutically effective amount to an individual who has or is at risk of developing a hair loss-related disease.
  • the method of administration is the same as described above.
  • the prevention may refer to any action of inhibiting or delaying the onset of hair loss-related diseases by administering the composition for preventing hair loss or promoting hair growth according to the present invention to an individual.
  • the treatment may refer to any act of administering the composition of the present invention to a subject suspected of having a hair loss-related disease so that the symptoms of the hair loss-related disease are improved or beneficial.
  • the pharmaceutical composition comprising the camellia peel extract is the same as described above.
  • the composition of the present invention may include a pharmaceutically acceptable carrier, excipient or diluent in addition to the active ingredients described above.
  • the carrier, excipient and diluent include lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia gum, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil.
  • a suitable dosage of the composition of the present invention varies depending on the condition and weight of the patient, the severity of the disease, the drug form, and time, but may be appropriately selected by those skilled in the art. Specifically, the dosage of the camellia peel extract may be 50 to 500 mg/Kg.
  • the hair loss-related diseases are alopecia areata (Alopecia Areata), hereditary androgenetic alopecia (Androgenetic Alopecia), telogen Effluvium, trauma, hair growth wall (Trichoti lomania), pressure (Pressure Alopecia), such as genital alopecia, nasal stiffness, It may include, but is not limited to, syphilis (Alopecia syphlltiac), seborrheic alopecia (Alopecia seborrhecia), symptomatic, scarring, congenital alopecia, etc., but is not limited thereto, and may refer to any disease resulting from hair loss from hair follicles.
  • the present invention provides a food composition for preventing hair loss or promoting hair growth, comprising a camellia peel extract as an active ingredient.
  • camellia fruit skin extract The effect of preventing hair loss and promoting hair growth of the camellia fruit skin extract is as described above.
  • the camellia peel extract may be added as it is or may be used together with other foods or food ingredients, and may be appropriately used according to a conventional method.
  • the mixing amount of the active ingredient may be suitably determined according to the purpose of use (prophylactic, health or therapeutic treatment), and may further include a food pharmaceutically acceptable food supplement additive. Since the composition of the present invention uses an extract derived from a natural product as an active ingredient, there is no problem in terms of stability, so there is no great limitation on the amount of mixing.
  • the food composition of the present invention may include all foods in a conventional sense, and may be used interchangeably with terms known in the art, such as functional food and health functional food.
  • the term "functional food” refers to food manufactured and processed using raw materials or ingredients useful for the human body. It means to ingest for the purpose of obtaining useful effects for health purposes such as
  • health functional food refers to a food manufactured and processed using a specific ingredient as a raw material for the purpose of health supplementation or by extracting, concentrating, refining, or mixing a specific ingredient contained in the food raw material, It refers to food designed and processed to sufficiently exert biological control functions such as biological defense, regulation of biological rhythm, prevention and recovery of disease, etc., by the above ingredients, and the composition for health food is used for prevention of diseases and prevention of diseases. It can perform functions related to recovery, etc.
  • compositions of the present invention for preventing hair loss or promoting hair growth can be used.
  • the composition comprising the camellia peel extract of the present invention as an active ingredient can be prepared by mixing other suitable auxiliary ingredients that may be contained in food and known additives according to the selection of those skilled in the art.
  • suitable auxiliary ingredients include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, tea, drinks, alcoholic beverages and
  • vitamins complexes and the like and it can be prepared by adding the extract according to the present invention as a main component to juice, tea, jelly, juice, and the like.
  • foods that can be applied to the present invention include, for example, special nutritional foods (eg, formula milk, infant food, etc.), processed meat products, fish meat products, tofu, jelly, noodles (eg, ramen, noodles, etc.), health supplements , Seasoned foods (eg soy sauce, soybean paste, red pepper paste, mixed soy sauce, etc.), sauces, sweets (eg snacks), dairy products (eg fermented milk, cheese, etc.), other processed foods, kimchi, pickled foods (various kimchi, pickles, etc.) ), beverages (eg, fruit, vegetable beverages, soy milk, fermented beverages, etc.), and natural seasonings (eg, ramen soup, etc.).
  • special nutritional foods eg, formula milk, infant food, etc.
  • processed meat products eg, fish meat products, tofu, jelly, noodles (eg, ramen, noodles, etc.)
  • health supplements e.
  • Seasoned foods eg soy sauce, soybean paste, red pepper paste
  • the health functional food composition of the present invention When used in the form of a beverage, it may contain various sweetening agents, flavoring agents, or natural carbohydrates as additional ingredients, as in a conventional beverage.
  • the health functional food composition of the present invention includes various nutrients, vitamins, electrolytes, flavoring agents, coloring agents, pectic acid and its salts, alginic acid and its salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin , alcohol, a carbonation agent used in carbonated beverages, and the like.
  • it may contain the pulp for the production of natural fruit juice, fruit juice beverage and vegetable beverage.
  • camellia peel extract more specifically, the camellia peel ethanol extract of the present invention, is made from natural medicinal plants, so even when used as a cosmetic composition, pharmaceutical composition or food composition, side effects may be less than that of general synthetic compounds, so it is safely included. It can be useful.
  • the remaining pericarp was thoroughly washed to remove foreign substances and impurities, dried in the shade at 20° C. to 35° C., and then pulverized so that the particle size was 1 mm or less. Then, 1 kg of the pulverized camellia peel powder was immersed in a 70% ethanol solvent, followed by ultrasonic extraction for 48 hours, and the resulting extract was filtered using filter paper (Advantec, No. 2). The filtrate was concentrated under reduced pressure to prepare a camellia peel extract.
  • Example 2 In vitro ( in vitro ) from camellia peel extract ( Camellia japonica Measurement of dermal papilla cell proliferation effect of pericarp coat extract)
  • the dermal papilla cell proliferation ability was measured. Specifically, human dermal papilla cells, HFDPC (Hair follicle dermal papilla cell, PromoCell), were cultured in a dermal papilla cell growth medium containing supplementMix and then inoculated into a 24-well plate (1.5 ⁇ 10 4 cells/well), 5% concentration. of CO 2 in an incubator at 37° C., and incubated for 24 hours. After dissolving the camellia peel extract in DMEM medium containing 1% FBS, it was treated in each cultured well and cultured again for 72 hours.
  • HFDPC Haair follicle dermal papilla cell, PromoCell
  • the cell culture supernatant was removed, washed once with PBS, diluted 10-fold with MTT reagent dissolved in 1 mg/ml, mixed with the medium, and then treated and cultured for 1 hour. After removing the MTT reagent after 1 hour, 200 ⁇ l of DMSO was added per well, formazan was dissolved, and the absorbance value was measured at 540 nm is shown in FIG. 1 .
  • the camellia peel extract exhibited about 60% of dermal papilla cell proliferation ability compared to the dermal papilla cell growth medium group, which is a positive control.
  • Example 3 In Vitro ( in vitro ) in the 5 alpha reductase activity inhibition effect of camellia peel extract
  • Camellia peel extract was added to the testosterone reaction solution by concentration to measure the activity of 5 alpha reductase. Specifically, 1 mmol/L DTT (dithiothreitol), pH 6.5, 40 mmol/L potassium phosphate, and 100 ⁇ mol/L NADPH were mixed, and then 3.5 ⁇ mol/L testosterone was added and finally 0.5 ml of A testosterone reaction solution was prepared. After leaving at room temperature for 20 minutes, finasteride was treated as a positive control, and camellia peel extract was treated in the other reaction solution, and rat liver granule was added to the whole reaction solution, followed by reaction at 37° C. for 30 minutes. After 30 minutes of lyophilization, the amount of testosterone remaining was analyzed by HPLC.
  • Testosterone was analyzed using a Waters 2695 Separation Module, Waters 2996 Photodiode Array Detector through a Phenomenex Luna C18 4.6 ⁇ 150 mm, 2.6 ⁇ m (reversed phase) column.
  • a sample dissolved in 0.5 ml of methanol was used as a sample solution, and 2.0 mg of a 98% pure Testosterone standard was precisely weighed and 40 ml of a solution dissolved in methanol was used as a testosterone standard stock solution (50 ppm). Precisely weigh 1 ml of this solution, add methanol to dissolve it, and make 10 ml as a standard solution (5 ppm).
  • the test solution and standard solution were analyzed according to the indicator component analysis method to determine the testosterone content in each sample as shown below [Equation 1] was calculated.
  • the result value obtained from this was converted based on 100% of the control group, and the result is shown in FIG. 2 .
  • the camellia peel extract showed excellent 5-alpha reductase inhibitory ability in a concentration-dependent manner compared to the positive control finasteride.
  • Example 4 In Vitro ( in vitro ) Measurement of Wnt-beta-catenin signaling activation effect of camellia peel extract in
  • Wnt-betacatenin signaling is a pathway majorly involved in hair follicle formation and regeneration, and TCF (T-cell factor) signaling is activated as a transcription factor. Activation of the Wnt-beta-catenin signaling pathway was measured using the TCF reporter luciferase system.
  • TCF luciferase plasmid was transfected using Lipofectamine 3000 reagent (Thermo Fisher scientific, USA). The transfected cells were treated with the camellia peel extract and reacted for 24 hours, and the reacted culture medium was reacted with a Gaussia luciferase substrate to measure the expression level of TCF luciferase.
  • As a positive control lithium chloride, a Wnt receptor agonist, was used. The results are shown in FIG. 3 .
  • the camellia peel extract induced TCF luciferase expression compared to the untreated group, and showed similar results compared to the positive control, lithium chloride (LiCl). Through this, it was confirmed that the camellia peel extract effectively activated the Wnt-beta-catenin signaling pathway.
  • a skin safety verification experiment was performed to confirm that the camellia peel extract according to the present invention is safe for human skin. To this end, a cumulative skin irritation test was conducted.
  • a nourishing cream containing 0.1%, 0.5% and 1% of the camellia peel extract of Example 1, respectively, was prepared. Specifically, the aqueous phase purified water, triethanolamine, and propylene glycol were heated to 70° C. and dissolved, and then beeswax, liquid paraffin, oily components, emulsifiers and preservatives were heated to 70° C. and dissolved, and emulsified. After the emulsification was completed, the solution was cooled to 45° C., and 0.1%, 0.5% and 1% of camellia peel extract were added and dispersed, respectively, and then cooled to 30°C. As the content of the camellia peel extract was increased to 0.1%, 0.5%, and 1%, the content of liquid paraffin was reduced to 9.91%, 9.51%, and 9.01%, respectively, to prepare a nourishing cream.
  • the patching method used a pin chamber (Finn chamber, Epitest Ltd, Finland). After 15 ⁇ l of each of the above external preparations for skin was dripped into the chamber, patching was performed. The degree of the reaction shown on the skin each time was scored using the following [Equation 2], and the results are shown in Table 1 below.
  • Average reactivity [[(response index ⁇ reactivity)/(total number of subjects ⁇ highest score (4 points))] ⁇ 100] ⁇ number of tests (9 times)
  • ⁇ is given a score of 1 point
  • + is given a score of 2
  • ++ is given a score of 4
  • the average reactivity is less than 3, it is judged as a safe composition.
  • the camellia peel extract according to the present invention was determined to be a safe material for human skin that does not show a distinct cumulative stimulation pattern.
  • composition of the present invention may be prepared as a formulation example as follows, but is not limited thereto.
  • a softened lotion containing a camellia peel extract extract as an active ingredient was prepared according to a conventional method.
  • Camellia peel extract 0.01 glycerin 3.0 butylene glycol 2.0 propylene glycol 2.0 carboxyvinyl polymer 0.1 ethanol 10.0 triethanolamine 0.1 Preservatives, trace colors, trace fragrances and trace purified water 82.79 sum 100.0
  • Nutrient lotion containing camellia peel extract as an active ingredient as shown in Table 3 below was prepared according to a conventional method.
  • Camellia peel extract 0.01 beeswax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.5 liquid paraffin 5.0 squalane 5.0 Caprylic/Capric Triglycerides 5.0 glycerin 3.0 butylene glycol 3.0 propylene glycol 3.0 carboxyvinyl polymer 0.1 triethanolamine 0.2 Preservatives, micro pigments, micro fragrances and micro-purified water 69.69 sum 100.0
  • a nourishing cream containing camellia peel extract as an active ingredient was prepared according to a conventional method.
  • Camellia peel extract 0.01 beeswax 10.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.5 liquid paraffin 10.0 squalane 5.0 Caprylic/Capric Triglycerides 5.0 glycerin 5.0 butylene glycol 3.0 propylene glycol 3.0 triethanolamine 0.2 Preservatives, micro pigments, micro fragrances and micro-purified water 56.79 sum 100.0
  • a nourishing cream containing camellia peel extract as an active ingredient was prepared according to a conventional method.
  • Camellia peel extract 0.01 beeswax 10.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.8 liquid paraffin 40.0 squalane 5.0 Caprylic/Capric Triglycerides 4.0 glycerin 5.0 butylene glycol 3.0 propylene glycol 3.0 triethanolamine 0.2 Preservatives, micro pigments, micro fragrances and micro-purified water 27.49 sum 100.0
  • Camellia peel extract 0.01 polyvinyl alcohol 13.0 Sodium Carboxymethylcellulose 0.2 allantoin 0.1 ethanol 5.0 nonylphenyl ether 0.3 Preservatives, micro pigments, micro fragrances and micro-purified water 81.39 sum 100.0
  • the above ingredients were mixed and filled in an airtight cloth to prepare a powder.
  • Camellia peel extract 100 corn starch 100 lactose 100 Magnesium Stearate 2
  • tablets were prepared by tableting according to a conventional method for manufacturing tablets.
  • Camellia peel extract 100 corn starch 100 lactose 100 Magnesium Stearate 2
  • the capsules were prepared by filling in gelatin capsules according to a conventional manufacturing method of capsules.
  • a gel containing camellia peel extract as an active ingredient was prepared according to a conventional method.
  • Camellia peel extract 1.0 diethanolamine 1.5 polyvinylptolidone 5.0 propylene glycol 30.0 Purified water 62.5 sum 100.0

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Abstract

La présente invention concerne une composition pour prévenir la chute des cheveux ou favoriser la pousse des cheveux comprenant un extrait de péricarpe de camélia en tant que principe actif. Plus spécifiquement, la présente invention concerne une composition cosmétique, une composition pharmaceutique et une composition alimentaire, comprenant en tant que principe actif un extrait de péricarpe de camélia qui peut favoriser la pousse des cheveux par induction de la prolifération des cellules de papille pilaire et inhiber la production de dihydrotestostérone par inhibition de l'activité de la 5-alpha réductase, ce qui permet de prévenir la chute des cheveux et de favoriser la pousse des cheveux. La composition selon la présente invention présente une excellente sécurité pour le corps humain sans irritation de la peau ni cytotoxicité et favorise également la prolifération des cellules de papille pilaire par activation du processus de signalisation Wnt, et est très efficace dans l'inhibition de la production de dihydrotestostérone, et peut ainsi être utilisé de façon utile en tant que principe actif dans une composition cosmétique, une composition pharmaceutique ou une composition alimentaire pour prévenir la chute des cheveux et favoriser la pousse des cheveux.
PCT/KR2021/005186 2020-04-24 2021-04-23 Composition pour prévenir la chute des cheveux ou favoriser la pousse des cheveux comprenant un extrait de péricarpe de camélia en tant que principe actif WO2021215882A1 (fr)

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KR101672431B1 (ko) 2015-01-06 2016-11-04 목포대학교산학협력단 동백나무 추출물을 유효성분으로 포함하는 심혈관계 질환의 예방 또는 치료용 조성물

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JP2010265252A (ja) * 2009-05-15 2010-11-25 Bhn Kk 育毛剤
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KR20160008055A (ko) * 2014-07-11 2016-01-21 주식회사 엘지생활건강 동백잎 추출물을 유효성분으로 포함하는 체모 또는 피부 상태 개선용 조성물
KR20160116834A (ko) * 2015-03-31 2016-10-10 (주)아모레퍼시픽 발모 또는 육모 촉진용 및 항염용 조성물

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