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WO2016159567A2 - Composition for promoting hair growth or hair restoration and for anti-inflammation - Google Patents

Composition for promoting hair growth or hair restoration and for anti-inflammation Download PDF

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Publication number
WO2016159567A2
WO2016159567A2 PCT/KR2016/002976 KR2016002976W WO2016159567A2 WO 2016159567 A2 WO2016159567 A2 WO 2016159567A2 KR 2016002976 W KR2016002976 W KR 2016002976W WO 2016159567 A2 WO2016159567 A2 WO 2016159567A2
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WO
WIPO (PCT)
Prior art keywords
theasaponin
composition
assamsaponin
hair
asamsaponin
Prior art date
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PCT/KR2016/002976
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French (fr)
Korean (ko)
Other versions
WO2016159567A3 (en
Inventor
홍용덕
고재영
박준성
Original Assignee
(주)아모레퍼시픽
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by (주)아모레퍼시픽 filed Critical (주)아모레퍼시픽
Priority to SG11201707761WA priority Critical patent/SG11201707761WA/en
Priority to JP2017550108A priority patent/JP6697479B2/en
Priority to MYPI2017703528A priority patent/MY182581A/en
Priority to PH1/2017/501722A priority patent/PH12017501722B1/en
Priority to HK18103044.0A priority patent/HK1243356A1/en
Priority to CN201680025764.3A priority patent/CN107530258B/en
Publication of WO2016159567A2 publication Critical patent/WO2016159567A2/en
Publication of WO2016159567A3 publication Critical patent/WO2016159567A3/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/82Theaceae (Tea family), e.g. camellia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth

Definitions

  • compositions for promoting hair growth or hair growth Disclosed herein are compositions for anti-inflammatory.
  • hair loss The causes of hair loss are discussed, such as hyperthermia of male hormone action, excessive sebum secretion, poor blood circulation, hypoxia caused by peroxide, bacteria, genetic factors, aging, stress.
  • hair loss population is gradually increasing due to social stress and westernized eating habits such as environmental pollution and instant food, frequent perm and dyeing.
  • Hair cycles include anagen, which grows hair, catagen, which ends growth and hairball shrinks, talogen, which is the time when the nipple stops working and the hair stays in the scalp. It can be divided into a generator, which is a time to start or to dehair old hair by generating new hair.
  • the anagen stage (2-7 years) is the period of hair growth, which is divided into the stages of hair production, from which hair exits the hair follicles and the formation of hard keratin in the hair follicles. Hair continues to grow self-development.
  • Cataract Stage (two to three weeks) is the period when the growth phase ends and metabolism slows down while maintaining the shape of the hair. This stage does not produce keratin.
  • the degenerative stage accounts for 1% of all hair. At this time, the hair follicle contracts and is divided into the dermal papilla, surrounded by the hair follicle, and upwards, and cell division is stationary.
  • the Talogen Stage (3 months) is followed by atrophy of the nipples, the hair follicles clumping gradually, and the roots being pushed upwards. The period of hair loss is 3-4 months until the next growth stage begins.
  • Androgenetic alopecia is caused by a male hormone called Testosterone, which is converted to the more powerful hormone Dihydrotestosterone (DHT) by an enzyme called 5alpha-reductase. Hormones act on the hair follicles, leading the hair follicles from the growth phase to the degenerative phase, leading to hair loss. Therefore, a method of inhibiting the production of DHT by 5-alpha-reductase is mainly used to treat androgenetic alopecia.
  • DHT Dihydrotestosterone
  • Gynecologic alopecia is mainly caused by a decrease in the amount of estrogen after menopause.
  • Minoxidil and estrogen are mainly used as treatments for gynecomastia.
  • Alopecia areata is caused by autoimmune diseases, mental stress, or genetic predisposition. This alopecia areata is fundamentally different from androgenetic alopecia, and the treatment is also different, using a method of treating corticosteroids, or applying minoxidil to the affected area or artificially causing irritation in the affected area.
  • the mediators responsible for inflammation include Vaso-active amines, Vaso-active polypeptides, and other mediators.
  • Vascularly active amines include histamine and three secreted from mast cells. Letonin and the like mainly serves to promote vasodilation and permeability.
  • vascular active polypeptides include kinin, plasmin, and complement, which act as a vasoconstrictor, and other lymphokines such as interleukin-6 (IL-6).
  • IL-6 interleukin-6
  • Arachidonic acid produced by phospholipase activated by physical and chemical stimuli, again passes through two pathways, cyclooxygenase (COX) or lipooxygenase, to prostaglandin, an inflammatory mediator. Metabolized to leukotriene to mediate various inflammatory responses (Thomas. R., Rev. Physiol. Biochem. Pharmacol., 100, 1984, Pub. 10-2008-0020853).
  • the prior art is Korean Patent No. 10-1274029.
  • the present disclosure is asamsaponin B (Assamsaponin B), Theasaponin E1 (Theasaponin E1), Theasaponin E2 (Theasaponin E2), Asamsaponin H (Assamsaponin H), Asamsaponin D (Assamsaponin D) and (Theasaponin C1) It is an object to provide a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of.
  • the present disclosure is directed to Asamsaponin B, Theasaponin E1, Theasaponin E2, Asamsaponin H, Asamsaponin D, and Assamsaponin D1.
  • Theasaponin C1 It is an object to provide an anti-inflammatory composition comprising at least one selected from the group consisting of as an active ingredient.
  • the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the asasaponin E2, and the asamsaponin H, which are represented by the above formula. It provides a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
  • the techniques disclosed herein include Asamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, and Asamsaponin D represented by the above formula. It provides an anti-inflammatory composition comprising at least one selected from the group consisting of (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
  • the active ingredient may be isolated from Camellia Seed extract.
  • the composition may be to propagate hair follicular papilla cells.
  • the composition may be to inhibit PGE2, IL-6 or IL-8 production.
  • the active ingredient may be included in 0.001 to 20% by weight based on the total weight of the composition.
  • the composition may be a pharmaceutical composition.
  • the composition may be a cosmetic composition.
  • the composition may be a food composition.
  • the techniques disclosed herein include Asamsaponin B, Theasaponin E1, Thesaponin E2, Asamsaponin H, Asamsaponin D, and Asamsaponin D.
  • There is an effect of providing a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of thiasaponin C1 (Theasaponin C1) as an active ingredient.
  • the techniques disclosed herein include: Assamsaponin B, Thesaponin E1, Theasaponin E2, Asamsaponin H, Asamsaponin D, and Asamsaponin D. It is effective to provide an anti-inflammatory composition comprising at least one selected from the group consisting of thiasaponin C1 (Theasaponin C1) as an active ingredient.
  • the technology disclosed herein has the effect of providing a pharmaceutical composition, cosmetic composition, food composition for promoting hair growth or hair growth, anti-inflammatory, which has no side effects and excellent stability by including a natural plant as an active ingredient.
  • the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the asasaponin E2, and the asamsaponin H, which are represented by the above formula. It provides a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
  • the techniques disclosed herein are asamsaponin B, thesaponin E1, theasaponin E2, and asasaponin represented by the above formulas for use in promoting hair growth or hair growth.
  • the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the assamsaponin H, and assamsaponin Hair growth, comprising administering to the subject in need of hair growth or hair growth a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of D (Assamsaponin D) and thiasaponin C1, or as an active ingredient Or provide a method for promoting hair growth.
  • the administration can be carried out according to the administration method and administration dose described herein.
  • the techniques disclosed herein are asamsaponin B, thiasaponin E1, and thiasaponin E2 represented by the above formula for preparing a composition for promoting hair growth or hair growth. And at least one use selected from the group consisting of Asamsaponin H, Asamsaponin D, and Theasaponin C1.
  • the technology disclosed herein is assamsaponin B (Assamsaponin B), Theasaponin E1 (Theasaponin E1), Theasaponin E2 (Theasaponin E2), Assamsaponin H (Assamsaponin H), Assam represented by the above formula It provides an anti-inflammatory composition comprising at least one selected from the group consisting of Saponin D (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
  • the techniques disclosed herein are asamsaponin B, theasaponin E1, theasaponin E2, and assamsaponin H represented by the above formula for use in anti-inflammatory. H), Asamsaponin D and Assasaponin C1 (Theasaponin C1).
  • the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the assamsaponin H, and assamsaponin Provides an anti-inflammatory method comprising administering at least one selected from the group consisting of D (Assamsaponin D) and thiasaponin C1 (Theasaponin C1), or an anti-inflammatory composition comprising them as an active ingredient to a subject in need of inflammation relief do.
  • the administration can be carried out according to the administration method and administration dose described herein.
  • the technology disclosed herein for preparing an anti-inflammatory composition, Asamsaponin B, Thesaponin E1, Theasaponin E2, The Asaponin E2, Assam It provides at least one use selected from the group consisting of Saponin H, Assamsaponin D and Theasaponin C1.
  • the active ingredient may be isolated from Camellia Seed extract.
  • Saponin Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D or Theasaponin C1 isolated from the camellia seed extract are obtained from the camellia seed by using water or an organic solvent to obtain an extract containing saponin; And isolating Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 from the extract.
  • an extract containing saponin from the camellia seeds may be appropriately applied, modified or applied by a person of ordinary skill in the art selecting appropriately from a method for preparing an extract used in the art.
  • the organic solvent may be at least one organic solvent selected from the group consisting of ethanol, methanol, butanol, ether, ethyl acetate and chloroform or a mixture of water and 50% ethanol in one aspect.
  • 1 to 4 1), Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 can be obtained.
  • the composition may be to propagate hair follicular papilla cells.
  • the composition has the effect of activating keratinocytes by proliferating follicular dermal papilla cells and promoting the production of hair by enhancing the expression of hair growth factor VEGF.
  • the composition has an effect of promoting the growth of hair and preventing or improving hair loss by shortening the period of transition from the resting phase to the growth phase of the hair growth cycle.
  • the composition may be to inhibit PGE2, IL-6 or IL-8 production.
  • the active ingredient may be included in 0.001 to 20% by weight based on the total weight of the composition. According to another embodiment, the active ingredient may be included as 0.01 to 15% by weight, 0.01 to 10% by weight, or 0.1 to 5% by weight based on the total weight of the composition.
  • the active ingredient included in the composition disclosed herein may be included as 0.001% by weight, 0.01% by weight, 0.1% by weight, or 1.0% by weight or more based on the total weight of the composition, and in another aspect 20 wt% or less, 15 wt% or less, 10 wt% or less, or 5 wt% or less.
  • the content of 0.001% by weight or more is excellent in hair regrowth, hair growth, anti-inflammatory effect of the composition, it is contained in 20% by weight or less, easy to manufacture safety or formulation, and exhibits excellent efficacy without side effects. Can be.
  • the composition may be a pharmaceutical composition.
  • the pharmaceutical composition may further contain, in addition to the active ingredients disclosed herein, pharmaceutical supplements such as preservatives, stabilizers, hydrating or emulsifying accelerators, salts and / or buffers for controlling osmotic pressure, and other therapeutically useful substances, It may be formulated in various oral or parenteral dosage forms according to conventional methods.
  • pharmaceutical supplements such as preservatives, stabilizers, hydrating or emulsifying accelerators, salts and / or buffers for controlling osmotic pressure, and other therapeutically useful substances, It may be formulated in various oral or parenteral dosage forms according to conventional methods.
  • the oral dosage forms include, for example, tablets, pills, hard and soft capsules, solutions, suspensions, emulsifiers, syrups, powders, powders, fine granules, granules, pellets, and the like, and these formulations include surfactants in addition to active ingredients. , Diluents (eg lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and glycine), glidants (eg silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycols). .
  • Diluents eg lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and glycine
  • glidants eg silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycols.
  • Tablets may also contain binders such as magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidine, optionally starch, agar, alginic acid or its sodium salt Pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, and sweeteners.
  • binders such as magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidine, optionally starch, agar, alginic acid or its sodium salt
  • Pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, and sweeteners.
  • the tablets can be prepared by conventional mixing, granulating or coating methods.
  • parenteral dosage form may be a transdermal dosage form, for example, an injection, drop, ointment, lotion, gel, cream, spray, suspension, emulsion, suppository, patch, or the like. It may be, but is not limited thereto.
  • compositions according to one embodiment of the invention may be administered topically to the scalp, for example.
  • the daily dosage of the drug depends on a variety of factors, such as the progress of the subject to be administered, the onset, age, health status, complications, etc. On the basis of one side may be administered by dividing the composition 1 ⁇ g / kg to 200 mg / kg, in another aspect 50 ⁇ g / kg to 50 mg / kg 1 to 3 times a day, the dosage is any The method does not limit the scope of the present invention.
  • the pharmaceutical composition may be an external preparation for skin, and the external preparation for skin may be included herein as a generic term that may include anything applied outside the skin.
  • the composition may be a cosmetic composition.
  • the cosmetic composition may further include functional additives and components included in the general cosmetic composition in addition to the active ingredient disclosed herein.
  • the functional additive may include a component selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, sphingolipids and seaweed extract.
  • oils and fats moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavorings, blood circulation And accelerators, cooling agents, limiting agents, purified water, and the like.
  • the cosmetic composition is not particularly limited in formulation, and may be appropriately selected as desired.
  • skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nutrition lotion, massage cream, nutrition cream, moisturizing cream, hand cream, foundation, essence, nutrition essence, pack, soap, cleansing It may be prepared in any one or more formulations selected from the group consisting of foam, cleansing lotion, cleansing cream, body lotion and body cleanser, but is not limited thereto.
  • the formulation of the present invention is a paste, cream or gel
  • animal carriers vegetable fibers, waxes, paraffins, starches, tracantes, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide, etc.
  • carrier components can be used as carrier components.
  • lactose When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, and especially in the case of spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.
  • a solvent, solvating or emulsifying agent is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.
  • liquid carrier diluents such as water, ethanol or propylene glycol
  • suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline Cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.
  • the carrier component is an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, an isethionate, an imidazolinium derivative, a methyltaurate, a sarcosinate, a fatty acid amide.
  • Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.
  • the composition may be a food composition.
  • the food composition may be in a liquid or solid dosage form, for example, various foods, beverages, gums, teas, vitamin complexes, dietary supplements, and the like, and may be used in the form of powders, granules, tablets, capsules, or beverages. Can be.
  • the food composition of each formulation may be appropriately selected and blended by those skilled in the art according to the formulation or purpose of use, according to the formulation or purpose of use. Can happen.
  • liquid component that can be contained in addition to the active ingredient disclosed herein, and may include various flavors or natural carbohydrates as additional ingredients, such as ordinary drinks.
  • natural carbohydrates include conventional sugars such as disaccharides such as monosaccharides, glucose and fructose, polysaccharides such as maltose and sucrose, dextrins and cyclodextrins, and sugar alcohols such as xylitol, sorbitol and erythritol. Etc.
  • natural flavoring agents such as, tauumatin, stevia extract (for example, rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (for example, saccharin, aspartame, etc.) can be advantageously used.
  • the proportion of natural carbohydrates may generally be about 1-20 g, in one aspect about 5-12 g, per 100 ml of the composition disclosed herein.
  • the food composition may contain various nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, flavoring agents such as coloring and neutralizing agents (such as cheese, chocolate), pectic acid and salts thereof, alginic acid and salts thereof.
  • it may include a pulp for the production of natural fruit juices and vegetable drinks.
  • the components can be used independently or in combination.
  • the ratio of the additive may vary, but is generally selected from 0.001 to about 20 parts by weight per 100 parts by weight of the composition disclosed herein.
  • Assamsaponin B Assamsaponin B
  • Thiasaponin E1 Theasaponin E1
  • thiasaponin E2 Theasaponin E2
  • Assamsaponin H Assamsaponin H
  • Assamsaponin Preparation of Assamsaponin D Theasaponin C1
  • camellia seed extract 3L of hexane was added to 1 kg of camellia seed (Camellia Seed), and extracted by stirring and extraction at room temperature. Then, 4 L of 50% ethanol was added to 0.5 kg of degreased camellia seed, and refluxed three times, followed by immersion at 15 ° C. for 1 day. Thereafter, the residue and the filtrate were separated through filter cloth filtration and centrifugation, and the separated filtrate was concentrated under reduced pressure to prepare a camellia seed extract.
  • B41p1 (1.6 mg), B41p2 (Assamsaponin B, 3.9 mg), B42p1 (Theasaponin E1, 12.8 mg), B42p2 (Theasaponin E2, 5.6 mg), B43p2 (Assamsaponin H, 2.2 mg), B43p3 (Camelliasaponin B1, 1.6 mg), B44p1 (Assamsaponin D, 3 mg), B44p2 (Theasaponin C1, 1.6 mg) in total 8 kinds of substances were obtained (Scheme) Reference).
  • Test Example 1 Increased expression of hair growth factor VEGF in dermal papilla cells
  • Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 are growth factors necessary for blood vessel formation and express Vascular endothelial growth factor (VEGF), which is a growth factor required to move to the hair growth phase
  • VEGF Vascular endothelial growth factor
  • the in vitro system was applied to evaluate the efficacy of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 derived from Camellia saponin.
  • DPC male dermal papilla cells
  • P.11 4 ⁇ 10 5 cells were seeded in 12-well plates, containing 10% FBS (fetal bovine serum). Incubated overnight in Dulbecco's modified Eagle's medium (DMEM) medium. After incubation, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 derived from camellia saponin were treated with 20 ppm, respectively. Theasaponin was used as a comparative example, and DMSO was used as a negative control.
  • DPC male dermal papilla cells
  • VEGF ELISA Vascular endothelial growth factor Enzyme-Linked Immunosorbent Assay
  • Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 can be seen that there is a significant difference in effect compared to the comparative example and the control, specifically, in the hair papilla cells The expression of growth factor VEGF was increased by about three times or more. Therefore, it can be seen that Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 have excellent hair growth promoting ability.
  • the keratin proteins that make up hair are produced in hair root keratinocytes, which are differentiated from dermal papilla cells. Therefore, if Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 promote the activity of dermal papilla cells, they can promote the activity of keratinocytes that are differentiated therefrom and further promote hair production.
  • Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 was evaluated as follows.
  • a human dermal papilla cell obtained from Professor Kwon Oh-sang, Seoul National University
  • the cell line was incubated for 24 hours in an incubator maintained at 5% CO 2 and 37 ° C with Dulbecco's modified Eagle's medium (DMEM; Gibco BRL, Gaithersburg, MD, USA) containing 10% bovine serum serum (FBS), Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, and Theasaponin C1 derived from camellia saponin were treated with 20 ppm, respectively.
  • Theasaponin was used as a comparative example, and DMSO was used as a negative control.
  • Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 showed a 1.5 times higher growth rate of dermal papilla cells than the comparative and control groups. This means that Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 can promote the growth of dermal papilla cells, and more effectively promote the activity and hair production of keratinocytes.
  • Hair follicles were isolated from the back of the scalp scalp tissue of a 55 year old male with William's E medium (L-glutamine (2 mM), insulin (10 ⁇ g / ml), hydrocortisone (40 ng / ml), antibiotics (1%), and antifungal agents (1). %) Containing).
  • the hair follicles grown on the third day after culture were screened and cut into 3 mm, and the selected hair follicle tissues were treated with no drug.
  • Assamsaponin D 5 ppm of Theasaponin C1
  • Theasaponin was treated as a comparative example. After 8 days of treatment, length measurement and photographing were performed. The results are shown in Table 3.
  • Test Example 4 PGE2 , Inhibits IL-6 and IL-8 production
  • Human fibroblasts were seeded in 6-well culture plates at a concentration of 1 ⁇ 10 5 cells and incubated in 37 ° C. and 5% CO 2 incubator for 24 hours. After treatment with 500 ⁇ M of H 2 O 2 in the wells for 24 hours, they were treated with Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, and Theasaponin as comparative examples, respectively. The reaction was carried out for 48 hours. After completion of the reaction, the culture was collected and subjected to ELISA analysis. In this case, alpha-bisabolol ( ⁇ -bisabolol), which is a material frequently used as an anti-inflammatory and irritant, was used as a control.
  • ⁇ -bisabolol alpha-bisabolol
  • PGE2 used Asay Design's kit, IL-6 and IL-8 used Endogen's kit, and the experiment was conducted according to the method specified in each company's manual.
  • the inhibitory effect was calculated according to Equation 1 below, and the measurement results are shown in Table 4 below.
  • Inhibitory effect ⁇ 1- (test sample-control) / (H 2 O 2 -control) ⁇ ⁇ 100
  • the ointment was prepared in a conventional manner according to the composition described in Table 7.
  • Hair tonic was prepared by a conventional method according to the composition shown in Table 8.
  • the lotion was prepared in a conventional manner according to the composition described in Table 11 below.
  • the mixture was mixed, and 400 mg per capsule was filled according to a conventional method to prepare a soft capsule.
  • 50 mg of one or more compounds selected from the group consisting of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, 250 mg of anhydrous glucose, and 550 mg of starch are mixed and molded into granules using a fluid bed granulator and It was filled in to prepare a granule.

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Abstract

The present specification discloses a composition for promoting hair growth or hair restoration and a composition for anti-inflammation. The composition comprises a pharmaceutical composition, a cosmetic composition or a food composition, and contains at least one selected from the group consisting of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D and Theasaponin C1.

Description

발모 또는 육모 촉진용 및 항염용 조성물Hair growth or hair growth promoting and anti-inflammatory composition
본 명세서에는 발모 또는 육모 촉진용 조성물 및 항염용 조성물이 개시된다.Disclosed herein are compositions for promoting hair growth or hair growth and compositions for anti-inflammatory.
탈모의 원인으로는 남성호르몬 작용 과잉설, 피지분비 과잉설, 혈액순환 불량설, 과산화물, 세균 등에 의한 두피기능 저하설, 유전적 요인, 노화, 스트레스 등이 논의되고 있다. 아울러, 사회적 스트레스 증가와 더불어 환경오염 및 인스턴트 식품 등 서구화된 식습관, 잦은 파마와 염색 등으로 인하여 탈모 인구가 점차 증가하고 있다. 모발의 주기는 모발을 성장시키는 성장기(anagen), 성장을 종료하고 모구부가 축소하는 시기인 퇴화기(catagen), 모유두가 활동을 멈추고 모발을 두피에 머무르게 하는 시기인 휴지기(talogen), 모유두가 활동을 시작하거나 또는 새로운 모발을 발생시켜 오래된 모발을 탈모시키는 시기인 발생기로 나눌 수 있다.The causes of hair loss are discussed, such as hyperthermia of male hormone action, excessive sebum secretion, poor blood circulation, hypoxia caused by peroxide, bacteria, genetic factors, aging, stress. In addition, hair loss population is gradually increasing due to social stress and westernized eating habits such as environmental pollution and instant food, frequent perm and dyeing. Hair cycles include anagen, which grows hair, catagen, which ends growth and hairball shrinks, talogen, which is the time when the nipple stops working and the hair stays in the scalp. It can be divided into a generator, which is a time to start or to dehair old hair by generating new hair.
성장기(Anagen Stage; 2~7년)는 모발이 성장하는 기간으로, 다시 모발이 모구로부터 모포로 나가려는 모발 생성 단계와 딱딱한 케라틴이 모낭 안에서 만들어지는 단계로 나누어진다. 모발은 퇴행기까지 자가성장을 계속한다. 퇴행기(Catagen Stage; 2~3주)는 성장기가 끝나고, 모발의 형태를 유지하면서 대사과정이 느려지는 시기로, 이 단계에서는 케라틴을 만들어내지 않는다. 퇴화기는 전체 모발의 1%를 차지한다. 이때 모구부가 수축하여 모유두로 나눠지며 모낭에 둘러싸여 위쪽으로 올라가고 세포분열은 정지상태이다. 휴지기(Talogen Stage; 3개월)는 모유두가 위축되고 모낭이 차츰 쪼그라들며, 모근이 위쪽으로 밀려 올라가 빠진다. 모발이 없어지는 시기로서 다음 성장기 단계가 시작될 때까지의 수명은 3~4개월이다.The anagen stage (2-7 years) is the period of hair growth, which is divided into the stages of hair production, from which hair exits the hair follicles and the formation of hard keratin in the hair follicles. Hair continues to grow self-development. Cataract Stage (two to three weeks) is the period when the growth phase ends and metabolism slows down while maintaining the shape of the hair. This stage does not produce keratin. The degenerative stage accounts for 1% of all hair. At this time, the hair follicle contracts and is divided into the dermal papilla, surrounded by the hair follicle, and upwards, and cell division is stationary. The Talogen Stage (3 months) is followed by atrophy of the nipples, the hair follicles clumping gradually, and the roots being pushed upwards. The period of hair loss is 3-4 months until the next growth stage begins.
정상인 사람은 성장기 상태의 모발이 많은데 비해 탈모증(Alopecia)인 사람은 휴지기 상태의 모발이 많아 눈으로 보이는 탈모현상이 나타나게 된다. 탈모가 진행될수록 성장기의 기간이 짧아지고 이로 인해 모발은 점점 소형화된다. 따라서, 탈모의 치료를 위해서는 휴지기 상태의 모낭을 성장기로 빨리 갈 수 있도록 하고, 짧아진 성장기를 늘려주는 것이 중요하다.Normal people have a lot of hair growth phase, whereas alopecia (alopecia) people have a lot of hair at rest phase is a visible hair loss phenomenon. As hair loss progresses, the growth phase is shorter, which leads to smaller and smaller hairs. Therefore, for the treatment of hair loss, it is important to allow the hair follicles in the resting state to go to the growth phase quickly and to increase the shortened growth phase.
남성형 탈모증은 테스토스테론(Testosterone)이라는 남성호르몬에 의해 나타나는 현상으로 이 테스토스테론이 5알파-리덕타아제(5α-reductase)라는 효소에 의해 더 강력한 호르몬인 디히드로테스토스테론(Dihydrotestosterone, DHT)으로 바뀌게 되면, 이 호르몬이 모낭에 작용하여 모낭을 성장기 단계에서 퇴화기 단계로 유도하여 탈모가 일어나게 한다. 따라서, 남성형 탈모증을 치료하기 위하여 5알파-리덕타아제에 의한 DHT의 생성을 억제하는 방법이 주로 사용된다.Androgenetic alopecia is caused by a male hormone called Testosterone, which is converted to the more powerful hormone Dihydrotestosterone (DHT) by an enzyme called 5alpha-reductase. Hormones act on the hair follicles, leading the hair follicles from the growth phase to the degenerative phase, leading to hair loss. Therefore, a method of inhibiting the production of DHT by 5-alpha-reductase is mainly used to treat androgenetic alopecia.
여성형 탈모증은 주로 폐경기 이후 에스트로겐 양의 감소에 의해 발생한다. 여성형 탈모증을 위한 치료제로는 주로 미녹시딜이나 에스트로겐이 사용되고 있다.Gynecologic alopecia is mainly caused by a decrease in the amount of estrogen after menopause. Minoxidil and estrogen are mainly used as treatments for gynecomastia.
원형 탈모증은 자가면역질환이나 정신적 스트레스, 유전적 소인에 의해 발생한다. 이러한 원형 탈모증은 안드로겐성 탈모증과는 근본적으로 원인이 다르며, 치료법 또한 달라서 부신피질 호르몬제를 처리하는 방법을 사용하거나, 미녹시딜을 환부에 바르거나 인위적으로 환부에 자극을 유발하는 방법을 사용한다.Alopecia areata is caused by autoimmune diseases, mental stress, or genetic predisposition. This alopecia areata is fundamentally different from androgenetic alopecia, and the treatment is also different, using a method of treating corticosteroids, or applying minoxidil to the affected area or artificially causing irritation in the affected area.
그러나, 지금까지 탈모를 방지하여 주고 발모 촉진 및 모발의 생장에 효과를 가지고 있다고 알려져 있는 미녹시딜(minoxidil)이나 트리코사카라이드 (trichosaccharide) 등의 제제들의 경우, 뚜렷한 효능의 부재 및 인체 안정성, 피부자극 유발 등의 부작용 문제가 대두되고 있어 안전성 및 효능이 확보된 조성물의 개발이 시급한 실정이다.However, in the case of preparations such as minoxidil and trichosaccharide, which are known to prevent hair loss and have an effect on promoting hair growth and hair growth, the absence of obvious efficacy, human stability, and skin irritation are induced. As a side effect of the problem is emerging, the development of a composition having a safety and efficacy is urgently urgent.
한편, 염증을 담당하는 매개체로는 혈관 활성 아민(Vaso-active amines), 혈관 활성 폴리펩타이드(Baso-active polypeptide) 및 기타 매개물질 등이 있으며, 혈관 활성 아민으로는 비만세포에서 분비되는 히스타민과 세레토닌 등이 있고 주로 혈관 확장과 투과성을 증진시키는 작용을 한다. 또한, 혈관 활성 폴리펩타이드로는 키닌(kinin), 프라스민(plasmin), 컴프리먼트(complement) 등이 있고 이는 혈관 수축 작용을 하며, 그 외 인터루킨-6(IL-6) 등과 같은 림포카인과 아라키돈산(arachidonic acid) 등이 염증 반응을 담당한다. Meanwhile, the mediators responsible for inflammation include Vaso-active amines, Vaso-active polypeptides, and other mediators. Vascularly active amines include histamine and three secreted from mast cells. Letonin and the like mainly serves to promote vasodilation and permeability. In addition, vascular active polypeptides include kinin, plasmin, and complement, which act as a vasoconstrictor, and other lymphokines such as interleukin-6 (IL-6). Arachidonic acid is responsible for the inflammatory response.
물리적, 화학적 자극에 의해 활성화된 포스포리파제에 의해 생성된 아라키돈산은 다시 싸이클로옥시게나제(cyclooxygenase, COX) 혹은 리포옥시게나제(lipooxygenase)의 2가지 경로를 거쳐 염증 반응 매개체인 프로스타그란딘(prostaglandin), 류코트리엔(leukotriene)으로 대사되어 다양한 염증 반응을 매개한다(Thomas. R., Rev.Physiol. Biochem. Pharmacol., 100, 1984, 공개특허 10-2008-0020853).Arachidonic acid, produced by phospholipase activated by physical and chemical stimuli, again passes through two pathways, cyclooxygenase (COX) or lipooxygenase, to prostaglandin, an inflammatory mediator. Metabolized to leukotriene to mediate various inflammatory responses (Thomas. R., Rev. Physiol. Biochem. Pharmacol., 100, 1984, Pub. 10-2008-0020853).
종래기술로는 한국 등록특허 제10-1274029호가 있다.The prior art is Korean Patent No. 10-1274029.
일 측면에서, 본 명세서는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 발모 또는 육모 촉진용 조성물을 제공하는 것을 목적으로 한다.In one aspect, the present disclosure is asamsaponin B (Assamsaponin B), Theasaponin E1 (Theasaponin E1), Theasaponin E2 (Theasaponin E2), Asamsaponin H (Assamsaponin H), Asamsaponin D (Assamsaponin D) and (Theasaponin C1) It is an object to provide a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of.
다른 측면에서, 본 명세서는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 항염용 조성물을 제공하는 것을 목적으로 한다.In another aspect, the present disclosure is directed to Asamsaponin B, Theasaponin E1, Theasaponin E2, Asamsaponin H, Asamsaponin D, and Assamsaponin D1. (Theasaponin C1) It is an object to provide an anti-inflammatory composition comprising at least one selected from the group consisting of as an active ingredient.
[화학식][Formula]
Figure PCTKR2016002976-appb-I000001
Figure PCTKR2016002976-appb-I000001
Figure PCTKR2016002976-appb-I000002
Figure PCTKR2016002976-appb-I000002
Figure PCTKR2016002976-appb-I000003
Figure PCTKR2016002976-appb-I000003
Figure PCTKR2016002976-appb-I000004
Figure PCTKR2016002976-appb-I000004
Figure PCTKR2016002976-appb-I000005
Figure PCTKR2016002976-appb-I000005
Figure PCTKR2016002976-appb-I000006
Figure PCTKR2016002976-appb-I000006
일 측면에서, 본 명세서에 개시된 기술은 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 발모 또는 육모 촉진용 조성물을 제공한다.In one aspect, the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the asasaponin E2, and the asamsaponin H, which are represented by the above formula. It provides a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
다른 측면에서, 본 명세서에 개시된 기술은 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 항염용 조성물을 제공한다.In another aspect, the techniques disclosed herein include Asamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, and Asamsaponin D represented by the above formula. It provides an anti-inflammatory composition comprising at least one selected from the group consisting of (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
예시적인 일 구현예에 따르면, 상기 유효성분은 동백씨(Camellia Seed) 추출물에서 분리된 것일 수 있다.According to one exemplary embodiment, the active ingredient may be isolated from Camellia Seed extract.
예시적인 일 구현예에 따르면, 상기 조성물은 모낭 모유두 세포를 증식시키는 것일 수 있다.According to one exemplary embodiment, the composition may be to propagate hair follicular papilla cells.
예시적인 일 구현예에 따르면, 상기 조성물은 PGE2, IL-6 또는 IL-8 생성을 억제하는 것일 수 있다.According to an exemplary embodiment, the composition may be to inhibit PGE2, IL-6 or IL-8 production.
예시적인 일 구현예에 따르면, 상기 유효성분은 조성물 총 중량을 기준으로 0.001 내지 20 중량%로 포함될 수 있다.According to one exemplary embodiment, the active ingredient may be included in 0.001 to 20% by weight based on the total weight of the composition.
예시적인 일 구현예에 따르면, 상기 조성물은 약학 조성물일 수 있다.According to one exemplary embodiment, the composition may be a pharmaceutical composition.
예시적인 일 구현예에 따르면, 상기 조성물은 화장료 조성물일 수 있다.According to an exemplary embodiment, the composition may be a cosmetic composition.
예시적인 일 구현예에 따르면, 상기 조성물은 식품 조성물일 수 있다.According to one exemplary embodiment, the composition may be a food composition.
일 측면에서, 본 명세서에 개시된 기술은 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 발모 또는 육모 촉진용 조성물을 제공하는 효과가 있다.In one aspect, the techniques disclosed herein include Asamsaponin B, Theasaponin E1, Thesaponin E2, Asamsaponin H, Asamsaponin D, and Asamsaponin D. There is an effect of providing a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of thiasaponin C1 (Theasaponin C1) as an active ingredient.
다른 측면에서, 본 명세서에 개시된 기술은 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 항염용 조성물을 제공하는 효과가 있다.In another aspect, the techniques disclosed herein include: Assamsaponin B, Thesaponin E1, Theasaponin E2, Asamsaponin H, Asamsaponin D, and Asamsaponin D. It is effective to provide an anti-inflammatory composition comprising at least one selected from the group consisting of thiasaponin C1 (Theasaponin C1) as an active ingredient.
또 다른 측면에서, 본 명세서에 개시된 기술은 식물성 천연물질을 유효성분으로 포함함으로써 부작용이 없고 안정성이 우수한 발모 또는 육모 촉진용, 항염용 약학 조성물, 화장료 조성물, 식품 조성물을 제공하는 효과가 있다.In another aspect, the technology disclosed herein has the effect of providing a pharmaceutical composition, cosmetic composition, food composition for promoting hair growth or hair growth, anti-inflammatory, which has no side effects and excellent stability by including a natural plant as an active ingredient.
이하, 본 발명을 상세히 설명한다.Hereinafter, the present invention will be described in detail.
[화학식][Formula]
Figure PCTKR2016002976-appb-I000007
Figure PCTKR2016002976-appb-I000007
Figure PCTKR2016002976-appb-I000008
Figure PCTKR2016002976-appb-I000008
Figure PCTKR2016002976-appb-I000009
Figure PCTKR2016002976-appb-I000009
Figure PCTKR2016002976-appb-I000010
Figure PCTKR2016002976-appb-I000010
Figure PCTKR2016002976-appb-I000011
Figure PCTKR2016002976-appb-I000011
Figure PCTKR2016002976-appb-I000012
Figure PCTKR2016002976-appb-I000012
일 측면에서, 본 명세서에 개시된 기술은 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 발모 또는 육모 촉진용 조성물을 제공한다.In one aspect, the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the asasaponin E2, and the asamsaponin H, which are represented by the above formula. It provides a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
다른 측면에서, 본 명세서에 개시된 기술은 발모 또는 육모 촉진에 사용하기 위한, 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 어느 하나 이상을 제공한다.In another aspect, the techniques disclosed herein are asamsaponin B, thesaponin E1, theasaponin E2, and asasaponin represented by the above formulas for use in promoting hair growth or hair growth. Provides at least one selected from the group consisting of Assamsaponin H, Assamsaponin D, and Thiasaponin C1.
또 다른 측면에서, 본 명세서에 개시된 기술은 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상, 또는 이들을 유효성분으로 포함하는 발모 또는 육모 촉진용 조성물을, 발모 또는 육모가 필요한 개체에 투여하는 것을 포함하는 발모 또는 육모 촉진 방법을 제공한다. 본 발명의 일 측면에 있어서 상기 투여는 본 명세서에 기재된 투여 방법 및 투여 용량에 따라 수행될 수 있다.In another aspect, the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the assamsaponin H, and assamsaponin Hair growth, comprising administering to the subject in need of hair growth or hair growth a composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of D (Assamsaponin D) and thiasaponin C1, or as an active ingredient Or provide a method for promoting hair growth. In one aspect of the invention the administration can be carried out according to the administration method and administration dose described herein.
또 다른 측면에서, 본 명세서에 개시된 기술은 발모 또는 육모 촉진용 조성물을 제조하기 위한, 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상의 용도를 제공한다.In another aspect, the techniques disclosed herein are asamsaponin B, thiasaponin E1, and thiasaponin E2 represented by the above formula for preparing a composition for promoting hair growth or hair growth. And at least one use selected from the group consisting of Asamsaponin H, Asamsaponin D, and Theasaponin C1.
또한, 일 측면에서, 본 명세서에 개시된 기술은 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 항염용 조성물을 제공한다.In addition, in one aspect, the technology disclosed herein is assamsaponin B (Assamsaponin B), Theasaponin E1 (Theasaponin E1), Theasaponin E2 (Theasaponin E2), Assamsaponin H (Assamsaponin H), Assam represented by the above formula It provides an anti-inflammatory composition comprising at least one selected from the group consisting of Saponin D (Assamsaponin D) and thiasaponin C1 (Theasaponin C1) as an active ingredient.
다른 측면에서, 본 명세서에 개시된 기술은 항염에 사용하기 위한, 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 어느 하나 이상을 제공한다.In another aspect, the techniques disclosed herein are asamsaponin B, theasaponin E1, theasaponin E2, and assamsaponin H represented by the above formula for use in anti-inflammatory. H), Asamsaponin D and Assasaponin C1 (Theasaponin C1).
또 다른 측면에서, 본 명세서에 개시된 기술은 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상, 또는 이들을 유효성분으로 포함하는 항염용 조성물을, 염증 완화가 필요한 개체에 투여하는 것을 포함하는 염증 완화 방법을 제공한다. 본 발명의 일 측면에 있어서 상기 투여는 본 명세서에 기재된 투여 방법 및 투여 용량에 따라 수행될 수 있다.In another aspect, the techniques disclosed herein are asamsaponin B, thesaponin E1, thesaponin E2, the assamsaponin H, and assamsaponin Provides an anti-inflammatory method comprising administering at least one selected from the group consisting of D (Assamsaponin D) and thiasaponin C1 (Theasaponin C1), or an anti-inflammatory composition comprising them as an active ingredient to a subject in need of inflammation relief do. In one aspect of the invention the administration can be carried out according to the administration method and administration dose described herein.
또 다른 측면에서, 본 명세서에 개시된 기술은, 항염용 조성물을 제조하기 위한, 상기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상의 용도를 제공한다.In another aspect, the technology disclosed herein, for preparing an anti-inflammatory composition, Asamsaponin B, Thesaponin E1, Theasaponin E2, The Asaponin E2, Assam It provides at least one use selected from the group consisting of Saponin H, Assamsaponin D and Theasaponin C1.
예시적인 일 구현예에 따르면, 상기 유효성분은 동백씨(Camellia Seed) 추출물에서 분리된 것일 수 있다. 동백씨 추출물에서 분리된 사포닌 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D 또는 Theasaponin C1은 동백 종자로부터 물 또는 유기용매를 이용하여 사포닌을 함유하는 추출물을 수득하는 단계; 및 상기 추출물로부터 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1을 분리하는 단계;를 포함하는 제조방법에 의해 제조될 수 있다. According to one exemplary embodiment, the active ingredient may be isolated from Camellia Seed extract. Saponin Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D or Theasaponin C1 isolated from the camellia seed extract are obtained from the camellia seed by using water or an organic solvent to obtain an extract containing saponin; And isolating Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 from the extract.
상기 동백 종자로부터 사포닌을 함유하는 추출물을 수득하는 단계는 통상의 기술자가 당해 기술분야에서 이용되고 있는 추출물의 제조방법으로부터 적의 선택하여 적절하게 적용, 변형 또는 응용할 수 있다. Obtaining an extract containing saponin from the camellia seeds may be appropriately applied, modified or applied by a person of ordinary skill in the art selecting appropriately from a method for preparing an extract used in the art.
예시적인 일 구현예에 따르면, 상기 유기용매는 에탄올, 메탄올, 부탄올, 에테르, 에틸아세테이트 및 클로로포름으로 이루어진 군으로부터 선택된 하나 이상의 유기용매 또는 이들과 물의 혼합물, 일 측면에서 50% 에탄올을 사용할 수 있다.According to an exemplary embodiment, the organic solvent may be at least one organic solvent selected from the group consisting of ethanol, methanol, butanol, ether, ethyl acetate and chloroform or a mixture of water and 50% ethanol in one aspect.
또한, 예시적인 일 구현예에 따르면, 용매를 사용하여 분획한 후, 감압농축하여 용매를 제거하고 조 생성물을 수득한 다음, 수득된 조 생성물을 C18 컬럼 크로마토그래피(아세토나이트릴:물= 8:1~4:1)로 분리하여, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1를 수득할 수 있다. Further, according to one exemplary embodiment, fractionation using a solvent was followed by concentration under reduced pressure to remove the solvent to obtain a crude product, and then the obtained crude product was subjected to C18 column chromatography (acetonitrile: water = 8). 1 to 4: 1), Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 can be obtained.
예시적인 일 구현예에 따르면, 상기 조성물은 모낭 모유두 세포를 증식시키는 것일 수 있다. 상기 조성물은 모낭 모유두 세포를 증식시켜 케라틴 형성세포를 활성화하고, 모발 성장인자 VEGF의 발현을 증진시켜 모발 생성을 촉진하는 효과가 있다. 또한, 상기 조성물은 모발의 성장주기 중 휴지기에서 성장기로 이행되는 주기를 단축시켜 모발의 성장을 촉진시키고 탈모를 예방 또는 개선하는 효과가 있다.According to one exemplary embodiment, the composition may be to propagate hair follicular papilla cells. The composition has the effect of activating keratinocytes by proliferating follicular dermal papilla cells and promoting the production of hair by enhancing the expression of hair growth factor VEGF. In addition, the composition has an effect of promoting the growth of hair and preventing or improving hair loss by shortening the period of transition from the resting phase to the growth phase of the hair growth cycle.
예시적인 일 구현예에 따르면, 상기 조성물은 PGE2, IL-6 또는 IL-8 생성을 억제하는 것일 수 있다.According to an exemplary embodiment, the composition may be to inhibit PGE2, IL-6 or IL-8 production.
예시적인 일 구현예에 따르면, 상기 유효성분은 조성물 총 중량을 기준으로 0.001 내지 20 중량%로 포함될 수 있다. 다른 일 구현예에 따르면, 상기 유효성분은 조성물 총 중량을 기준으로 0.01 내지 15 중량%, 0.01 내지 10 중량%, 또는 0.1 내지 5 중량%로 포함될 수 있다. According to one exemplary embodiment, the active ingredient may be included in 0.001 to 20% by weight based on the total weight of the composition. According to another embodiment, the active ingredient may be included as 0.01 to 15% by weight, 0.01 to 10% by weight, or 0.1 to 5% by weight based on the total weight of the composition.
일 측면에서 본 명세서에 개시되는 조성물에 포함되는 유효성분은 조성물 총 중량을 기준으로 0.001 중량% 이상, 0.01 중량% 이상, 0.1 중량% 이상, 또는 1.0 중량% 이상으로 포함될 수 있으며, 다른 일 측면에서 20 중량% 이하, 15 중량% 이하, 10중량% 이하, 또는 5 중량% 이하로 포함될 수 있다. 상기 함유량에 특별히 한정되는 것은 아니나, 함유량이 0.001 중량% 이상 포함됨으로써 조성물의 발모 또는 육모, 항염 효과가 우수하고, 20 중량% 이하로 포함됨으로써 안전성 또는 제형상 제조가 용이하고 부작용 없이 우수한 효능을 나타낼 수 있다.In one aspect, the active ingredient included in the composition disclosed herein may be included as 0.001% by weight, 0.01% by weight, 0.1% by weight, or 1.0% by weight or more based on the total weight of the composition, and in another aspect 20 wt% or less, 15 wt% or less, 10 wt% or less, or 5 wt% or less. Although not particularly limited to the above content, the content of 0.001% by weight or more is excellent in hair regrowth, hair growth, anti-inflammatory effect of the composition, it is contained in 20% by weight or less, easy to manufacture safety or formulation, and exhibits excellent efficacy without side effects. Can be.
예시적인 일 구현예에 따르면, 상기 조성물은 약학 조성물일 수 있다.According to one exemplary embodiment, the composition may be a pharmaceutical composition.
상기 약학 조성물은 본 명세서에 개시된 유효성분 이외에 방부제, 안정화제, 수화제 또는 유화 촉진제, 삼투압 조절을 위한 염 및/또는 완충제 등의 약제학적 보조제 및 기타 치료적으로 유용한 물질을 추가로 함유할 수 있으며, 통상적인 방법에 따라 다양한 경구 투여제 또는 비경구 투여제 형태로 제형화할 수 있다.The pharmaceutical composition may further contain, in addition to the active ingredients disclosed herein, pharmaceutical supplements such as preservatives, stabilizers, hydrating or emulsifying accelerators, salts and / or buffers for controlling osmotic pressure, and other therapeutically useful substances, It may be formulated in various oral or parenteral dosage forms according to conventional methods.
상기 경구 투여제는 예를 들면, 정제, 환제, 경질 및 연질 캅셀제, 액제, 현탁제, 유화제, 시럽제, 분제, 산제, 세립제, 과립제, 펠렛제 등이 있으며, 이들 제형은 유효성분 이외에 계면 활성제, 희석제(예: 락토즈, 덱스트로즈, 수크로즈, 만니톨, 솔비톨, 셀룰로오스 및 글리신), 활택제(예: 실리카, 탈크, 스테아르산 및 그의 마그네슘 또는 칼슘염 및 폴리에틸렌 글리콜)를 함유할 수 있다. 정제는 또한 마그네슘 알루미늄 실리케이트, 전분페이스트, 젤라틴, 트라가칸스, 메틸셀룰로오스, 나트륨 카복시메틸셀룰로오스 및 폴리비닐피롤리딘과 같은 결합제를 함유할 수 있으며, 경우에 따라 전분, 한천, 알긴산 또는 그의 나트륨 염과 같은 붕해제, 흡수제, 착색제, 향미제, 및 감미제 등의 약제학적 첨가제를 함유할 수 있다. 상기 정제는 통상적인 혼합, 과립화 또는 코팅 방법에 의해 제조될 수 있다.The oral dosage forms include, for example, tablets, pills, hard and soft capsules, solutions, suspensions, emulsifiers, syrups, powders, powders, fine granules, granules, pellets, and the like, and these formulations include surfactants in addition to active ingredients. , Diluents (eg lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and glycine), glidants (eg silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycols). . Tablets may also contain binders such as magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidine, optionally starch, agar, alginic acid or its sodium salt Pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, and sweeteners. The tablets can be prepared by conventional mixing, granulating or coating methods.
또한, 상기 비경구 투여 형태로는 경피 투여형 제형일 수 있으며, 예를 들어 주사제, 점적제, 연고, 로션, 겔, 크림, 스프레이, 현탁제, 유제, 좌제(坐劑), 패취 등의 제형일 수 있으나, 이에 제한되는 것은 아니다.In addition, the parenteral dosage form may be a transdermal dosage form, for example, an injection, drop, ointment, lotion, gel, cream, spray, suspension, emulsion, suppository, patch, or the like. It may be, but is not limited thereto.
상기 약학 조성물은 비경구, 직장, 국소, 경피, 피하 등으로 투여될 수 있다. 본 발명의 일 실시예에 따른 약학 조성물은 예를 들어 두피에 국소 투여될 수 있다.The pharmaceutical composition may be administered parenterally, rectally, topically, transdermally, subcutaneously, and the like. Pharmaceutical compositions according to one embodiment of the invention may be administered topically to the scalp, for example.
상기 유효성분의 투여량 결정은 통상의 기술자의 수준 내에 있으며, 약물의 1일 투여 용량은 투여하고자 하는 대상의 진행 정도, 발병 시기, 연령, 건강상태, 합병증 등의 다양한 요인에 따라 달라지지만, 성인을 기준으로 할 때 일 측면에서 상기 조성물 1㎍/kg 내지 200mg/kg, 다른 일 측면에서 50㎍/kg 내지 50mg/kg을 1일 1 내지 3회 분할하여 투여할 수 있으며, 상기 투여량은 어떠한 방법으로도 본 발명의 범위를 한정하는 것이 아니다.Determination of the dosage of the active ingredient is within the level of ordinary skill in the art, the daily dosage of the drug depends on a variety of factors, such as the progress of the subject to be administered, the onset, age, health status, complications, etc. On the basis of one side may be administered by dividing the composition 1 ㎍ / kg to 200 mg / kg, in another aspect 50 ㎍ / kg to 50 mg / kg 1 to 3 times a day, the dosage is any The method does not limit the scope of the present invention.
상기 약학 조성물은 피부 외용제일 수 있으며, 상기 피부 외용제는 피부 외부에서 도포되는 어떠한 것이라도 포함될 수 있는 총칭으로서 다양한 제형의 의약품이 여기에 포함될 수 있다.The pharmaceutical composition may be an external preparation for skin, and the external preparation for skin may be included herein as a generic term that may include anything applied outside the skin.
예시적인 일 구현예에 따르면, 상기 조성물은 화장료 조성물일 수 있다.According to an exemplary embodiment, the composition may be a cosmetic composition.
상기 화장료 조성물에는 본 명세서에 개시된 유효성분 이외에 기능성 첨가물 및 일반적인 화장료 조성물에 포함되는 성분이 추가로 포함될 수 있다. 상기 기능성 첨가물로는 수용성 비타민, 유용성 비타민, 고분자 펩티드, 고분자 다당, 스핑고 지질 및 해초 엑기스로 이루어진 군에서 선택된 성분을 포함할 수 있다. 이외에 포함되는 배합 성분으로서는 유지 성분, 보습제, 에몰리엔트제, 계면 활성제, 유기 및 무기 안료, 유기 분체, 자외선 흡수제, 방부제, 살균제, 산화 방지제, 식물 추출물, pH 조정제, 알콜, 색소, 향료, 혈행 촉진제, 냉감제, 제한(制汗)제, 정제수 등을 들 수 있다.The cosmetic composition may further include functional additives and components included in the general cosmetic composition in addition to the active ingredient disclosed herein. The functional additive may include a component selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, sphingolipids and seaweed extract. In addition to the other components included, oils and fats, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavorings, blood circulation And accelerators, cooling agents, limiting agents, purified water, and the like.
상기 화장료 조성물은 제형이 특별히 한정되지 않으며, 목적하는 바에 따라 적절히 선택할 수 있다. 예를 들어, 스킨로션, 스킨소프너, 스킨토너, 아스트린젠트, 로션, 밀크로션, 모이스쳐 로션, 영양로션, 맛사지크림, 영양크림, 모이스처크림, 핸드크림, 파운데이션, 에센스, 영양에센스, 팩, 비누, 클렌징폼, 클렌징로션, 클렌징크림, 바디로션 및 바디클린저로 이루어진 군으로부터 선택된 어느 하나 이상의 제형으로 제조될 수 있으나, 이에 제한되는 것은 아니다.The cosmetic composition is not particularly limited in formulation, and may be appropriately selected as desired. For example, skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nutrition lotion, massage cream, nutrition cream, moisturizing cream, hand cream, foundation, essence, nutrition essence, pack, soap, cleansing It may be prepared in any one or more formulations selected from the group consisting of foam, cleansing lotion, cleansing cream, body lotion and body cleanser, but is not limited thereto.
본 발명의 제형이 페이스트, 크림 또는 겔인 경우에는 담체 성분으로서 동물섬유, 식물섬유, 왁스, 파라핀, 전분, 트라칸트, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크 또는 산화아연 등이 이용될 수 있다.When the formulation of the present invention is a paste, cream or gel, animal carriers, vegetable fibers, waxes, paraffins, starches, tracantes, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide, etc. may be used as carrier components. Can be.
본 발명의 제형이 파우더 또는 스프레이인 경우에는 담체 성분으로서 락토스, 탈크, 실리카, 알루미늄히드록시드, 칼슘 실리케이트 또는 폴리아미드 파우더가 이용될 수 있고, 특히 스프레이인 경우에는 추가적으로 클로로플루오로히드로카본, 프로판/부탄 또는 디메틸 에테르와 같은 추진체를 포함할 수 있다.When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, and especially in the case of spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.
본 발명의 제형이 용액 또는 유탁액의 경우에는 담체 성분으로서 용매, 용매화제 또는 유탁화제가 이용되고, 예컨대 물, 에탄올, 이소프로판올, 에틸 카보네이트, 에틸 아세테이트, 벤질 알코올, 벤질 벤조에이트, 프로필렌 글리콜, 1,3-부틸글리콜 오일, 글리세롤 지방족 에스테르, 폴리에틸렌 글리콜 또는 소르비탄의 지방산 에스테르가 있다.When the formulation of the present invention is a solution or emulsion, a solvent, solvating or emulsifying agent is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.
본 발명의 제형이 현탁액인 경우에는 담체 성분으로서 물, 에탄올 또는 프로필렌 글리콜과 같은 액상 희석제, 에톡실화 이소스테아릴 알코올, 폴리옥시에틸렌 소르비톨 에스테르 및 폴리옥시에틸렌 소르비탄 에스테르와 같은 현탁제, 미소결정성 셀룰로오스, 알루미늄 메타히드록시드, 벤토나이트, 아가 또는 트라칸트 등이 이용될 수 있다.When the dosage form of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline Cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.
본 발명의 제형이 계면-활성제 함유 클린징인 경우에는 담체 성분으로서 지방족 알코올 설페이트, 지방족 알코올 에테르 설페이트, 설포숙신산 모노에스테르, 이세티오네이트, 이미다졸리늄 유도체, 메틸타우레이트, 사르코시네이트, 지방산 아미드 에테르 설페이트, 알킬아미도베타인, 지방족 알코올, 지방산 글리세리드, 지방산 디에탄올아미드, 식물성 유, 리놀린 유도체 또는 에톡실화 글리세롤 지방산 에스테르 등이 이용될 수 있다.When the formulation of the present invention is a surfactant-containing cleansing, the carrier component is an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, an isethionate, an imidazolinium derivative, a methyltaurate, a sarcosinate, a fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.
예시적인 일 구현예에 따르면, 상기 조성물은 식품 조성물일 수 있다.According to one exemplary embodiment, the composition may be a food composition.
상기 식품 조성물은 액상 또는 고체 상태의 제형일 수 있고, 예를 들어, 각종 식품류, 음료, 껌, 차, 비타민 복합제, 건강보조 식품류 등이 있고, 분말, 과립, 정제, 캡슐 또는 음료인 형태로 사용될 수 있다. 각 제형의 식품 조성물은 본 명세서에 개시된 유효성분 이외에 해당 분야에서 통상적으로 사용되는 성분들을 제형 또는 사용 목적에 따라 당업자가 어려움 없이 적의 선정하여 배합할 수 있으며, 다른 원료와 동시에 적용할 경우 상승 효과가 일어날 수 있다.The food composition may be in a liquid or solid dosage form, for example, various foods, beverages, gums, teas, vitamin complexes, dietary supplements, and the like, and may be used in the form of powders, granules, tablets, capsules, or beverages. Can be. In addition to the active ingredients disclosed in the present specification, the food composition of each formulation may be appropriately selected and blended by those skilled in the art according to the formulation or purpose of use, according to the formulation or purpose of use. Can happen.
본 명세서에 개시된 유효성분 외에 함유할 수 있는 액체 성분에는 특별한 제한점이 없으며, 통상의 음료와 같이 여러가지 향미제 또는 천연 탄수화물 등을 추가성분으로 포함할 수 있다. 상기 천연 탄수화물의 예로는 모노사카라이드, 포도당, 과당 등의 디사카라이드, 말토스, 슈크로스 등의 폴리사카라이드, 덱스트린, 시클로덱스트린 등의 통상적인 당 및 자일리톨, 소르비톨, 에리트리톨 등의 당 알코올 등이 있다. 상기의 향미제로는 천연 향미제(타우마틴, 스테비아 추출물(예를 들어 레바우디오시드 A, 글리시르히진 등) 및 합성 향미제(예를 들어 사카린, 아스파르탐 등)를 유리하게 사용할 수 있다. 상기 천연 탄수화물의 비율은 본 명세서에 개시된 조성물 100ml 당 일반적으로 약 1 내지 20g, 일측면에서 약 5 내지 12g일 수 있다.There is no particular limitation on the liquid component that can be contained in addition to the active ingredient disclosed herein, and may include various flavors or natural carbohydrates as additional ingredients, such as ordinary drinks. Examples of the natural carbohydrates include conventional sugars such as disaccharides such as monosaccharides, glucose and fructose, polysaccharides such as maltose and sucrose, dextrins and cyclodextrins, and sugar alcohols such as xylitol, sorbitol and erythritol. Etc. As the flavoring agent, natural flavoring agents (tauumatin, stevia extract (for example, rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (for example, saccharin, aspartame, etc.) can be advantageously used. The proportion of natural carbohydrates may generally be about 1-20 g, in one aspect about 5-12 g, per 100 ml of the composition disclosed herein.
상기 식품 조성물은 일 측면에서 여러가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 중진제(치즈, 초콜릿 등), 펙트산 및 그 염, 알긴산 및 그 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 포함할 수 있다. 다른 측면에서 천연 과일 주스 및 야채 음료의 제조를 위한 과육을 포함할 수 있다. 상기 성분들은 독립적으로 또는 조합하여 사용될 수 있다. 상기 첨가제의 비율은 다양할 수 있으나, 본 명세서에 개시된 조성물 100 중량부 당 0.001 내지 약 20 중량부의 범위에서 선택되는 것이 일반적이다.In one aspect, the food composition may contain various nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, flavoring agents such as coloring and neutralizing agents (such as cheese, chocolate), pectic acid and salts thereof, alginic acid and salts thereof. , Organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated drinks and the like. In another aspect it may include a pulp for the production of natural fruit juices and vegetable drinks. The components can be used independently or in combination. The ratio of the additive may vary, but is generally selected from 0.001 to about 20 parts by weight per 100 parts by weight of the composition disclosed herein.
이하, 실시예를 통하여 본 발명을 더욱 상세히 설명하고자 한다. 이들 실시예는 오로지 본 발명을 예시하기 위한 것으로서, 본 발명의 범위가 이들 실시예에 의해 제한되는 것으로 해석되지 않는 것은 당업계에서 통상의 지식을 가진 자에게 있어서 자명할 것이다.Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention, it will be apparent to those skilled in the art that the scope of the present invention is not to be construed as limited by these examples.
제조예Production Example 1.  One. 아삼사포닌Assamsaponin B( B ( AssamsaponinAssamsaponin B),  B), 티아사포닌Thiasaponin E1( E1 ( TheasaponinTheasaponin E1), 티아사포닌 E2( E1), thiasaponin E2 ( TheasaponinTheasaponin E2),  E2), 아삼사포닌Assamsaponin H( H ( AssamsaponinAssamsaponin H),  H), 아삼사포닌Assamsaponin D(Assamsaponin D), 티아사포닌 C1(Theasaponin C1)의 제조 Preparation of Assamsaponin D, Theasaponin C1
동백씨(Camellia Seed) 1kg에 헥산 3L를 넣고, 상온에서 교반 추출하여 탈지시킨 다음, 탈지된 동백씨 0.5kg에 50% 에탄올 4L를 넣고, 3회 환류 추출한 후, 15℃에서 1일간 침적시켰다. 그 후, 여과포 여과와 원심분리를 통하여 잔사와 여액을 분리하고, 분리된 여액을 감압농축하여 동백씨 추출물을 제조하였다.3L of hexane was added to 1 kg of camellia seed (Camellia Seed), and extracted by stirring and extraction at room temperature. Then, 4 L of 50% ethanol was added to 0.5 kg of degreased camellia seed, and refluxed three times, followed by immersion at 15 ° C. for 1 day. Thereafter, the residue and the filtrate were separated through filter cloth filtration and centrifugation, and the separated filtrate was concentrated under reduced pressure to prepare a camellia seed extract.
또한, 상기 제조된 동백씨 추출물 7.37g을 물에 현탁하여 n-BuOH로 분획을 실시하였고, 확보한 BuOH 가용분획 2.54g에서 1.40g을 용출용매 35% MeOH로 RP MPLC를 실시하였다. 그 중 B4 소분획을 용출용매 CMIW=9:6:1:4 (+0.2% acetic acid) 조건으로 HPCCC를 실시하였다. 이렇게 얻은 소분획 B41, B42, B43 그리고 B44를 각각의 HPLC 조건으로 정제한 결과, B41p1 (1.6 mg), B41p2 (Assamsaponin B,3.9 mg), B42p1 (Theasaponin E1, 12.8 mg), B42p2 (Theasaponin E2, 5.6 mg), B43p2 (Assamsaponin H, 2.2 mg), B43p3 (Camelliasaponin B1, 1.6 mg), B44p1 (Assamsaponin D, 3 mg), B44p2 (Theasaponin C1, 1.6 mg) 총 8종의 물질을 수득하였다(하기 도식 참조).In addition, 7.37 g of the Camellia seed extract prepared above was suspended in water and fractionated with n-BuOH, and 1.40 g of the obtained BuOH soluble fraction was subjected to RP MPLC with 35% MeOH. Among them, a small fraction of B4 was subjected to HPCCC under the elution solvent CMIW = 9: 6: 1: 4 (+ 0.2% acetic acid). The small fractions B41, B42, B43 and B44 thus obtained were purified under respective HPLC conditions. As a result, B41p1 (1.6 mg), B41p2 (Assamsaponin B, 3.9 mg), B42p1 (Theasaponin E1, 12.8 mg), B42p2 (Theasaponin E2, 5.6 mg), B43p2 (Assamsaponin H, 2.2 mg), B43p3 (Camelliasaponin B1, 1.6 mg), B44p1 (Assamsaponin D, 3 mg), B44p2 (Theasaponin C1, 1.6 mg) in total 8 kinds of substances were obtained (Scheme) Reference).
Figure PCTKR2016002976-appb-I000013
Figure PCTKR2016002976-appb-I000013
시험예 1. 모유두 세포에서 모발 성장인자 VEGF의 발현 증가Test Example 1. Increased expression of hair growth factor VEGF in dermal papilla cells
Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1이 혈관 형성에 필요한 성장인자로 모발의 성장기로 이동하는데 필요한 성장인자인 혈관 내피 성장 인자(Vascular endothelial growth factor; VEGF)를 발현시키는 정도를 평가하기 위해, 생체 외(in vitro) 시스템을 적용하여 동백씨 사포닌으로부터 유래된 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1의 효능을 평가하였다.Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 are growth factors necessary for blood vessel formation and express Vascular endothelial growth factor (VEGF), which is a growth factor required to move to the hair growth phase In order to evaluate the degree, the in vitro system was applied to evaluate the efficacy of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 derived from Camellia saponin.
상기 실험을 위해 47세 남성의 모유두 진피세포(Dermal Papilla Cell; DPC) (P.11) 4 × 105 cell을 12웰 플레이트에 씨딩(seeding)하고, 10% FBS (fetal bovine serum)를 함유하는 DMEM(Dulbecco's modified Eagle's medium) 배지에서 하룻밤 동안 배양하였다. 배양 후, 동백씨 사포닌으로부터 유래된 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1을 각각 20ppm으로 처리하였다. 비교예로서 Theasaponin을 사용하였고, 음성 대조군으로는 DMSO를 사용하였다. For the experiment, 47-year-old male dermal papilla cells (DPC) (P.11) 4 × 10 5 cells were seeded in 12-well plates, containing 10% FBS (fetal bovine serum). Incubated overnight in Dulbecco's modified Eagle's medium (DMEM) medium. After incubation, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 derived from camellia saponin were treated with 20 ppm, respectively. Theasaponin was used as a comparative example, and DMSO was used as a negative control.
24시간 후 동백씨 사포닌으로부터 유래된 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1가 처리된 혼합액을 수집(soup collect)하고 VEGF ELISA (Vascular endothelial growth factor Enzyme-Linked Immunosorbent Assay; R&D biosystems)를 사용하여 VEGF 발현 정도를 확인하였다. 그 결과를 하기 표 1에 나타내었다.After 24 hours, the mixed solution treated with Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 derived from camellia seed saponin was collected and VEGF ELISA (Vascular endothelial growth factor Enzyme-Linked Immunosorbent Assay; R & D biosystems) were used to determine the degree of VEGF expression. The results are shown in Table 1 below.
[표 1]TABLE 1
Figure PCTKR2016002976-appb-I000014
Figure PCTKR2016002976-appb-I000014
표 1에서 볼 수 있듯이, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1은 비교예 및 대조군과 비교하여 현저한 효과의 차이가 있음을 알 수 있으며, 구체적으로, 모유두 세포에서 모발 성장인자 VEGF의 발현을 약 3배 이상 증가시켰다. 따라서, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1은 우수한 모발 생성 촉진능을 가짐을 알 수 있다.As can be seen in Table 1, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 can be seen that there is a significant difference in effect compared to the comparative example and the control, specifically, in the hair papilla cells The expression of growth factor VEGF was increased by about three times or more. Therefore, it can be seen that Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 have excellent hair growth promoting ability.
시험예 2. 모낭 모유두 세포 증식Test Example 2 Hair follicle papilla cells proliferation
모발을 구성하는 케라틴 단백질은 모근부 케라틴 형성세포(keratinocyte)에서 생성되며, 이 케라틴 형성세포는 모유두 세포로부터 분화된다. 따라서, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1가 모유두 세포의 활성을 촉진한다면 그로부터 분화되는 케라틴 형성세포의 활성을 촉진시킬 수 있고, 나아가 모발 생성을 촉진시킬 수 있다. 이에, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1의 모유두 세포 활성 촉진 효과를 하기와 같이 평가하였다. The keratin proteins that make up hair are produced in hair root keratinocytes, which are differentiated from dermal papilla cells. Therefore, if Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 promote the activity of dermal papilla cells, they can promote the activity of keratinocytes that are differentiated therefrom and further promote hair production. Thus, assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 was evaluated as follows.
먼저, 본 시험예에서는 사람 모유두 세포(Human dermal papilla cell;hDPc, 서울대 권오상교수로부터 입수) 세포주를 사용하여 실험하였다. 상기 세포주는 10% 소혈청세럼(FBS)이 함유된 Dulbecco's modified Eagle's medium (DMEM; Gibco BRL, Gaithersburg, MD, USA)으로 5% CO2 및 37℃가 유지되는 인큐베이터에서 24시간 동안 배양한 후, 동백씨 사포닌으로부터 유래된 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1을 20ppm으로 각각 처리하였다. 비교예로서 Theasaponin을 사용하였고, 음성 대조군으로는 DMSO를 사용하였다. First, in this test example, a human dermal papilla cell (hDPc, obtained from Professor Kwon Oh-sang, Seoul National University) was tested. The cell line was incubated for 24 hours in an incubator maintained at 5% CO 2 and 37 ° C with Dulbecco's modified Eagle's medium (DMEM; Gibco BRL, Gaithersburg, MD, USA) containing 10% bovine serum serum (FBS), Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, and Theasaponin C1 derived from camellia saponin were treated with 20 ppm, respectively. Theasaponin was used as a comparative example, and DMSO was used as a negative control.
시험 물질을 처리한 후 24시간 경과 후에 WST-1 키트(Roche)를 사용하여 세포 증식능(%)을 측정하였으며, 그 결과를 표 2에 나타내었다.24 hours after the test material was treated, cell proliferation (%) was measured using the WST-1 kit (Roche), and the results are shown in Table 2.
[표 2]TABLE 2
Figure PCTKR2016002976-appb-I000015
Figure PCTKR2016002976-appb-I000015
표 2에서 볼 수 있듯이, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1은 비교예 및 대조군 대비 약 1.5배 이상 높은 모유두 세포 증식 증가율을 나타내었다. 이는 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1이 모유두 세포의 증식을 촉진시킬 수 있으며, 케라틴 형성세포의 활성 및 모발 생성도 보다 효과적으로 촉진할 수 있음을 의미한다.As can be seen in Table 2, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 showed a 1.5 times higher growth rate of dermal papilla cells than the comparative and control groups. This means that Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 can promote the growth of dermal papilla cells, and more effectively promote the activity and hair production of keratinocytes.
시험예 3. 인체 모낭기관에서의 모발 성장 촉진Test Example 3 Hair Growth in Human Hair Follicle Organs
본 시험예에서는 실제 인체 모낭기관에서의 모발 성장 촉진능을 확인하였다.In this test example, the hair growth promoting ability in the human hair follicle organ was confirmed.
55세 남성의 후두부 두피 조직으로부터 모낭기관을 하나씩 분리하여 William's E 배지(L-글루타민(2mM), 인슐린(10㎍/ml), 히드로코르티손(40ng/ml), 항생제(1%), 항진균제(1%) 함유)에서 배양하였다. 배양 후 3일째에 성장이 일어난 모낭을 선별하여 3mm로 자르고, 선별한 모낭조직에 대해 약물을 처리하지 않은 경우를 대조군으로 하고, 동백씨 사포닌으로부터 유래된 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 5ppm, 비교예로서 Theasaponin을 각각 처리하였다. 그리고, 처리한지 8일 후 각각 길이 측정 및 사진촬영을 진행하였다. 그 결과를 표 3에 나타내었다.Hair follicles were isolated from the back of the scalp scalp tissue of a 55 year old male with William's E medium (L-glutamine (2 mM), insulin (10 μg / ml), hydrocortisone (40 ng / ml), antibiotics (1%), and antifungal agents (1). %) Containing). The hair follicles grown on the third day after culture were screened and cut into 3 mm, and the selected hair follicle tissues were treated with no drug. Assamsaponin B, Theasaponin E1, Theasaponin E2, and Assamsaponin H derived from camellia seed saponin. , Assamsaponin D, 5 ppm of Theasaponin C1, Theasaponin was treated as a comparative example. After 8 days of treatment, length measurement and photographing were performed. The results are shown in Table 3.
[표 3]TABLE 3
Figure PCTKR2016002976-appb-I000016
Figure PCTKR2016002976-appb-I000016
그 결과, 표 3에서 볼 수 있듯이, 모낭기관에서 모발의 길이 증가에 있어서 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1을 처리한 경우 비교예 및 대조군보다 우수한 모발 성장 촉진 효과가 나타났다. 따라서, Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1은 모낭에서 모발의 길이 성장을 촉진하는 효과가 우수함을 알 수 있다.As a result, as shown in Table 3, the hair growth promoting effect of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 in hair follicle organs increased compared to the comparative example and the control group Appeared. Therefore, it can be seen that Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 have an excellent effect of promoting hair length growth in hair follicles.
시험예Test Example 4.  4. PGE2PGE2 , IL-6 및 IL-8 생성 억제, Inhibits IL-6 and IL-8 production
사람의 섬유아세포를 6-웰 배양판에 1×105 세포의 농도로 접종하고, 24 시간 동안 37℃ 및 5% CO2 인큐베이터에서 배양하였다. H2O2 500μM을 웰에 처리하여 24시간 동안 자극을 준 후, 동백씨 사포닌으로부터 유래된 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, 비교예로서 Theasaponin을 각각 처리하여 48시간 동안 반응시켰다. 반응 완료 후 배양액을 수거하여 ELISA 분석을 수행하였다. 이때, 항염 및 자극 완화제로 많이 사용되는 물질인 알파-비사보롤(α-bisabolol)을 대조군으로 사용하였다. Human fibroblasts were seeded in 6-well culture plates at a concentration of 1 × 10 5 cells and incubated in 37 ° C. and 5% CO 2 incubator for 24 hours. After treatment with 500 μM of H 2 O 2 in the wells for 24 hours, they were treated with Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, and Theasaponin as comparative examples, respectively. The reaction was carried out for 48 hours. After completion of the reaction, the culture was collected and subjected to ELISA analysis. In this case, alpha-bisabolol (α-bisabolol), which is a material frequently used as an anti-inflammatory and irritant, was used as a control.
PGE2는 어세이 디자인(Assay Design)사의 키트, IL-6, IL-8은 엔도젠(Endogen)사의 키트를 사용하였으며, 각 회사의 매뉴얼에 명기된 방법에 따라 실험을 진행하였다. 억제 효과는 하기 수학식 1에 따라 계산하였으며, 측정 결과는 하기 표 4에 나타내었다.PGE2 used Asay Design's kit, IL-6 and IL-8 used Endogen's kit, and the experiment was conducted according to the method specified in each company's manual. The inhibitory effect was calculated according to Equation 1 below, and the measurement results are shown in Table 4 below.
[수학식 1][Equation 1]
억제 효과 = {1-(시험 시료-대조군)/(H2O2-대조군)} × 100Inhibitory effect = {1- (test sample-control) / (H 2 O 2 -control)} × 100
[표 4]TABLE 4
Figure PCTKR2016002976-appb-I000017
Figure PCTKR2016002976-appb-I000017
상기 표 4에 나타낸 바와 같이, 염증 매개 물질인 PGE2, IL-6, IL-8의 생성량이 Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 첨가에 의해 비교예 및 대조군과 비교하여 현저하게 줄어들어 우수한 항염 효과가 있음을 확인할 수 있었다. As shown in Table 4, the production of inflammatory mediators PGE2, IL-6, IL-8 compared with the comparative example and control by the addition of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 Remarkably reduced it was confirmed that the excellent anti-inflammatory effect.
본 발명의 일측면에 따른 조성물의 제형예를 아래에서 설명하나, 다른 여러 가지 제형으로도 응용 가능하며, 이는 본 발명을 한정하고자 함이 아닌 단지 구체적으로 설명하고자 함이다.Examples of the formulation of the composition according to one aspect of the present invention will be described below, but can be applied to other various formulations, which are intended to explain in detail only and not intended to limit the present invention.
[제형예 1] 샴푸Formulation Example 1 Shampoo
하기 표 5에 기재된 조성에 따라 통상적인 방법으로 샴푸를 제조하였다.To prepare a shampoo in a conventional manner according to the composition shown in Table 5.
[표 5]TABLE 5
Figure PCTKR2016002976-appb-I000018
Figure PCTKR2016002976-appb-I000018
[제형예 2] 린스Formulation Example 2 Rinse
하기 표 6에 기재된 조성에 따라 통상적인 방법으로 린스를 제조하였다.To prepare a rinse in a conventional manner according to the composition shown in Table 6.
[표 6]TABLE 6
Figure PCTKR2016002976-appb-I000019
Figure PCTKR2016002976-appb-I000019
[제형예 3] 연고Formulation Example 3 Ointment
하기 표 7에 기재된 조성에 따라 통상적인 방법으로 연고를 제조하였다.The ointment was prepared in a conventional manner according to the composition described in Table 7.
[표 7]TABLE 7
Figure PCTKR2016002976-appb-I000020
Figure PCTKR2016002976-appb-I000020
[제형예 4] 헤어토닉[Formulation Example 4] Hair Tonic
하기 표 8에 기재된 조성에 따라 통상적인 방법으로 헤어토닉을 제조하였다.Hair tonic was prepared by a conventional method according to the composition shown in Table 8.
[표 8]TABLE 8
Figure PCTKR2016002976-appb-I000021
Figure PCTKR2016002976-appb-I000021
[제형예 5] 헤어로션[Formulation Example 5] Hair Lotion
하기 표 9에 기재된 조성에 따라 통상적인 방법으로 헤어로션을 제조하였다.To prepare a hair lotion in a conventional manner according to the composition shown in Table 9.
[표 9]TABLE 9
Figure PCTKR2016002976-appb-I000022
Figure PCTKR2016002976-appb-I000022
[제형예 6] 비누Formulation Example 6 Soap
하기 표 10에 기재된 조성에 따라 통상적인 방법으로 비누를 제조하였다.To prepare a soap in a conventional manner according to the composition shown in Table 10.
[표 10]TABLE 10
Figure PCTKR2016002976-appb-I000023
Figure PCTKR2016002976-appb-I000023
[제형예 7] 로션[Formulation Example 7] Lotion
하기 표 11에 기재된 조성에 따라 통상적인 방법으로 로션을 제조하였다.The lotion was prepared in a conventional manner according to the composition described in Table 11 below.
[표 11]TABLE 11
Figure PCTKR2016002976-appb-I000024
Figure PCTKR2016002976-appb-I000024
[제형예 8] 크림Formulation Example 8 Cream
하기 표 12에 기재된 조성에 따라 통상적인 방법으로 크림을 제조하였다.To prepare a cream in a conventional manner according to the composition shown in Table 12.
[표 12]TABLE 12
Figure PCTKR2016002976-appb-I000025
Figure PCTKR2016002976-appb-I000025
[제형예 9] 팩[Formulation Example 9] Pack
하기 표 13에 기재된 조성에 따라 통상적인 방법으로 팩을 제조하였다.To prepare a pack in a conventional manner according to the composition described in Table 13.
[표 13]TABLE 13
Figure PCTKR2016002976-appb-I000026
Figure PCTKR2016002976-appb-I000026
[제형예 10] 미용액형 제제Formulation Example 10 Cosmetic Liquid Formulation
하기 표 14에 기재된 조성에 따라 통상적인 방법으로 미용액형 제제를 제조하였다.To prepare a cosmetic liquid formulation in a conventional manner according to the composition shown in Table 14.
[표 14]TABLE 14
Figure PCTKR2016002976-appb-I000027
Figure PCTKR2016002976-appb-I000027
[제형예 11] 연질캅셀제Formulation Example 11 Soft Capsule
Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1로 구성된 군에서 선택되는 하나 이상의 화합물 50mg, L-카르니틴 80~140mg, 대두유 180mg, 팜유 2mg, 식물성 경화유 8mg, 황납 4mg 및 레시틴 6mg을 혼합하고, 통상의 방법에 따라 1캡슐당 400mg씩 충진하여 연질캅셀제를 제조하였다.One or more compounds selected from the group consisting of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1 50 mg, L-carnitine 80-140 mg, Soybean oil 180 mg, Palm oil 2 mg, Vegetable hardened oil 8 mg, Saccharin 4 mg and Lecithin 6 mg The mixture was mixed, and 400 mg per capsule was filled according to a conventional method to prepare a soft capsule.
[제형예 12] 정제Formulation Example 12 Tablets
Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1로 구성된 군에서 선택되는 하나 이상의 화합물 50mg, 갈락토올리고당 200mg, 유당 60mg 및 맥아당 140mg을 혼합하고 유동층 건조기를 이용하여 과립한 후 당 에스테르(sugar ester)를 6mg을 첨가하여 타정기로 타정하여 정제를 제조하였다.50 mg of one or more compounds selected from the group consisting of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, 200 mg galactooligosaccharide, 60 mg lactose and 140 mg malt sugar, and then granulated using a fluidized bed dryer Tablets were prepared by adding 6 mg of ester (sugar ester) to a tablet press.
[제형예 13] 과립제Formulation Example 13 Granules
Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1로 구성된 군에서 선택되는 하나 이상의 화합물 50mg, 무수결정 포도당 250mg 및 전분 550mg을 혼합하고, 유동층 과립기를 사용하여 과립으로 성형한 후 포에 충진하여 과립제를 제조하였다.50 mg of one or more compounds selected from the group consisting of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, 250 mg of anhydrous glucose, and 550 mg of starch are mixed and molded into granules using a fluid bed granulator and It was filled in to prepare a granule.
[제형예 14] 드링크제Formulation Example 14 Drinks
Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1로 구성된 군에서 선택되는 하나 이상의 화합물 50mg, 포도당 10g, 구연산 0.6g, 및 액상 올리고당 25g을 혼합한 후 정제수 300ml를 가하여 각 병에 200ml씩 충진한다. 병에 충진한 후 130℃ 에서 4~5 초간 살균하여 드링크제 음료를 제조하였다.50 mg of one or more compounds selected from the group consisting of Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin C1, 10 g of glucose, 0.6 g of citric acid, and 25 g of liquid oligosaccharides were added to each bottle with 300 ml of purified water. Fill 200 ml each. After filling the bottle sterilized for 4-5 seconds at 130 ℃ to prepare a beverage drink.
이상, 본 발명내용의 특정한 부분을 상세히 기술하였는바, 당업계의 통상의 지식을 가진 자에게 있어서, 이러한 구체적인 기술은 단지 바람직한 실시태양일 뿐이며, 이에 의해 본 발명의 범위가 제한되는 것이 아닌 점은 명백할 것이다. 따라서 본 발명의 실질적인 범위는 첨부된 청구항들과 그것들의 등가물에 의해 정의된다고 할 것이다.As described above, specific portions of the present disclosure have been described in detail, and for those skilled in the art, these specific techniques are merely preferred embodiments, and the scope of the present disclosure is not limited thereto. Will be obvious. Thus, the substantial scope of the present invention will be defined by the appended claims and their equivalents.

Claims (9)

  1. 하기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 발모 또는 육모 촉진용 조성물.Asamsaponin B, Thesaponin E1, Theasaponin E2, Asamsaponin H, Asamsaponin D, and Theasaponin C1 A composition for promoting hair growth or hair growth comprising at least one selected from the group consisting of C1) as an active ingredient.
    [화학식][Formula]
    Figure PCTKR2016002976-appb-I000028
    Figure PCTKR2016002976-appb-I000028
    Figure PCTKR2016002976-appb-I000029
    Figure PCTKR2016002976-appb-I000029
    Figure PCTKR2016002976-appb-I000030
    Figure PCTKR2016002976-appb-I000030
    Figure PCTKR2016002976-appb-I000031
    Figure PCTKR2016002976-appb-I000031
    Figure PCTKR2016002976-appb-I000032
    Figure PCTKR2016002976-appb-I000032
    Figure PCTKR2016002976-appb-I000033
    Figure PCTKR2016002976-appb-I000033
  2. 하기 화학식으로 표시되는 아삼사포닌 B(Assamsaponin B), 티아사포닌 E1(Theasaponin E1), 티아사포닌 E2(Theasaponin E2), 아삼사포닌 H(Assamsaponin H), 아삼사포닌 D(Assamsaponin D) 및 티아사포닌 C1(Theasaponin C1)으로 이루어진 군에서 선택되는 하나 이상을 유효성분으로 포함하는 항염용 조성물.Asamsaponin B, Thesaponin E1, Theasaponin E2, Asamsaponin H, Asamsaponin D, and Theasaponin C1 Anti-inflammatory composition comprising at least one selected from the group consisting of C1) as an active ingredient.
    [화학식][Formula]
    Figure PCTKR2016002976-appb-I000034
    Figure PCTKR2016002976-appb-I000034
    Figure PCTKR2016002976-appb-I000035
    Figure PCTKR2016002976-appb-I000035
    Figure PCTKR2016002976-appb-I000036
    Figure PCTKR2016002976-appb-I000036
    Figure PCTKR2016002976-appb-I000037
    Figure PCTKR2016002976-appb-I000037
    Figure PCTKR2016002976-appb-I000038
    Figure PCTKR2016002976-appb-I000038
    Figure PCTKR2016002976-appb-I000039
    Figure PCTKR2016002976-appb-I000039
  3. 제 1항 또는 제 2항에 있어서,The method according to claim 1 or 2,
    상기 유효성분은 동백씨(Camellia Seed) 추출물에서 분리된 것인, 조성물.The active ingredient is isolated from Camellia Seed extract, composition.
  4. 제 1항에 있어서,The method of claim 1,
    상기 조성물은 모낭 모유두 세포를 증식시키는 것인, 조성물.Wherein said composition is for propagating follicular dermal papilla cells.
  5. 제 2항에 있어서,The method of claim 2,
    상기 조성물은 PGE2, IL-6 또는 IL-8 생성을 억제하는 것인, 조성물.Wherein said composition inhibits PGE2, IL-6 or IL-8 production.
  6. 제 1항 또는 제 2항에 있어서,The method according to claim 1 or 2,
    상기 유효성분은 조성물 총 중량을 기준으로 0.001 내지 20 중량%로 포함되는, 조성물.The active ingredient is 0.001 to 20% by weight based on the total weight of the composition, the composition.
  7. 제 1항 또는 제 2항에 있어서,The method according to claim 1 or 2,
    상기 조성물은 약학 조성물인, 조성물.The composition is a pharmaceutical composition.
  8. 제 1항 또는 제 2항에 있어서,The method according to claim 1 or 2,
    상기 조성물은 화장료 조성물인, 조성물.The composition is a cosmetic composition.
  9. 제 1항 또는 제 2항에 있어서,The method according to claim 1 or 2,
    상기 조성물은 식품 조성물인, 조성물.Wherein said composition is a food composition.
PCT/KR2016/002976 2015-03-31 2016-03-24 Composition for promoting hair growth or hair restoration and for anti-inflammation WO2016159567A2 (en)

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