KR20170133074A - Skin brightening composition - Google Patents
Skin brightening composition Download PDFInfo
- Publication number
- KR20170133074A KR20170133074A KR1020160064049A KR20160064049A KR20170133074A KR 20170133074 A KR20170133074 A KR 20170133074A KR 1020160064049 A KR1020160064049 A KR 1020160064049A KR 20160064049 A KR20160064049 A KR 20160064049A KR 20170133074 A KR20170133074 A KR 20170133074A
- Authority
- KR
- South Korea
- Prior art keywords
- composition
- anthrapyrazolone
- skin
- present
- skin whitening
- Prior art date
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
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Abstract
Description
본 발명은 안트라피라졸론을 유효성분으로 포함하는 피부 미백용 조성물에 관한 것이다.The present invention relates to a skin whitening composition comprising anthrapyrazolone as an active ingredient.
사람의 피부색을 결정하는 주요 인자인 멜라닌은 표피층에서 자외선을 차단하여 진피 아래 피부 기관을 보호하고, 생체의 자유 라디칼을 흡수함으로써 피부를 보호하는 역할을 한다. 이러한 멜라닌은 과잉으로 존재하는 경우 기미, 주근깨, 점 등 피부 색소 침착의 원인이 된다.Melanin, a key factor in determining the color of a person's skin, protects the skin by blocking the ultraviolet rays from the epidermis layer, protecting the dermis organs, and absorbing free radicals in the body. When melanin is present in excess, it causes skin pigmentation such as spots, freckles, and dots.
멜라닌은 피부의 기저층에 존재하는 멜라닌 형성 세포(Melanocyte)에서 만들어지며, 멜라닌 형성과정에서 가장 중요한 역할을 하는 효소는 티로시나제(Tyrosinase)로 알려져 있다. 티로시나제는 티로신(Tyrosine)을 도파(DOPA), 도파퀴논(Dopaquinone)으로 전환시키며, 이들의 비효소적인 산화 반응을 통하여 멜라닌 색소가 생성된다.Melanin is produced in melanocytes, which are found in the basal layer of the skin. The most important enzyme in melanin formation is known as tyrosinase. Tyrosinase transforms tyrosine into DOPA and Dopaquinone, and melanin is produced through the nonenzymatic oxidation of these tyrosinases.
멜라닌 생성은 자외선이나 염증 등의 자극에 의해서 촉진된다고 알려져 있다. 따라서 외부 자극을 줄이고 신호 전달을 차단하거나, 멜라닌 생성 효소의 합성을 억제하고 활성을 저해함으로써 멜라닌의 생성량을 감소시킬 수 있다.Melanogenesis is known to be stimulated by stimuli such as ultraviolet light or inflammation. Thus, the amount of melanin produced can be reduced by reducing external stimuli, blocking signal transduction, inhibiting the synthesis of melanin-producing enzymes, and inhibiting activity.
현재 멜라닌 생성을 조절할 수 있는 것으로 알려진 물질로는 코지산, 하이드로퀴논, 알부틴, 아젤라익산, 4-부틸레소시놀, 레스베라트롤, 세라마이드, 스핑고신-1-인산, 스핑고실포스포릴콜린 등이 있다. 상기 물질들은 티로시나제의 활성을 억제하거나 당화를 조절함으로써 멜라닌 생성을 조절한다. 그러나 이들은 만족스럽지 않은 미백 효과, 낮은 안정성, 피부 자극 때문에 그 활용도가 높지 않다. 따라서 우수한 미백 효과를 가지면서도 부작용이 적은 물질의 개발이 필요한 실정이다.Materials currently known to be able to regulate melanin production include kojic acid, hydroquinone, arbutin, azelaic acid, 4-butyl resorcinol, resveratrol, ceramide, sphingosine-1-phosphate and sphingolipphosphorylcholine. These substances regulate melanogenesis by inhibiting the activity of tyrosinase or by controlling glycosylation. However, they are not used because of unsatisfactory whitening effect, low stability, and skin irritation. Therefore, it is necessary to develop a substance having a good whitening effect and a low side effect.
한편, 안트라피라졸론(Anthrapyrazolone)은 스트레스에 의하여 활성화되는 JNK(c-Jun N-terminal kinase)의 저해제(inhibitor)로서, 류마티스성 관절염, 통풍, 천식, 기관지염, 건선, 습진, 피부염 등 다양한 질환의 예방 및 치료에 효과가 있는 것으로 알려져 있다. 그러나 안트라피라졸론이 피부 미백 효과를 나타낸다는 점은 아직까지 알려진 바가 없다.Anthrapyrazolone is an inhibitor of c-Jun N-terminal kinase (JNK) that is activated by stress. It is an inhibitor of various diseases such as rheumatoid arthritis, gout, asthma, bronchitis, psoriasis, eczema, It is known to be effective for prevention and treatment. However, it is not yet known that anthrapyrazolone exhibits skin whitening effect.
본 발명자들은 JNK 저해제로 알려져 있는 안트라피라졸론이 티로시나제의 활성을 저해하여 멜라닌 생성을 억제함으로써 피부 미백 효과를 나타내는 점을 확인하여 본 발명을 완성하였다.The present inventors have confirmed that anthrapyrazolone, which is known as a JNK inhibitor, inhibits the activity of tyrosinase and inhibits melanin production, thereby exhibiting a skin whitening effect, thereby completing the present invention.
따라서, 본 발명의 목적은 안트라피라졸론을 유효성분으로 포함하는 피부 미백용 조성물을 제공하는 것이다.Accordingly, an object of the present invention is to provide a skin whitening composition comprising anthra pyrazolone as an active ingredient.
본 발명은 하기 화학식 1로 표시되는 안트라피라졸론을 유효성분으로 포함하는 피부 미백용 조성물을 제공한다:The present invention provides a skin whitening composition comprising anthrapyrazolone represented by the following formula (1) as an active ingredient:
[화학식 1][Chemical Formula 1]
본 발명에 따른 피부 미백용 조성물은 안트라피라졸론을 유효성분으로 포함하여 우수한 피부 미백 효과를 나타낸다.The composition for skin whitening according to the present invention contains anthrapyrazolone as an active ingredient and exhibits excellent skin whitening effect.
구체적으로, 본 발명에 따른 피부 미백용 조성물은 티로시나제의 활성을 저해함으로써 멜라닌 생성을 억제하여 피부 미백 효과를 나타내며, 세포 독성을 나타내지 않으므로 화장품 또는 식품의 원료로 이용될 수 있다.Specifically, the composition for skin whitening according to the present invention inhibits the activity of tyrosinase to inhibit melanin production to exhibit a skin whitening effect, and does not exhibit cytotoxicity, and thus can be used as a raw material for cosmetics or foods.
도 1은 안트라피라졸론을 처리한 세포 및 비처리한 세포를 용해 및 원심분리하여 얻은 펠렛의 사진이다.
도 2는 안트라피라졸론을 처리한 세포와 비처리한 세포의 멜라닌 색소 함량을 확인하기 위한 450 nm 파장의 흡광도 측정 결과이다.
도 3은 안트라피라졸론을 처리한 세포와 비처리한 세포의 티로시나제 활성을 비교하기 위한 450 nm 파장의 흡광도 측정 결과이다.
도 4는 안트라피라졸론의 세포 독성 실험 결과이다.1 is a photograph of pellets obtained by dissolving and centrifuging cells treated with anthra pyrazolone and untreated cells.
FIG. 2 shows the results of absorbance measurement at a wavelength of 450 nm for confirming the melanin pigment content of cells treated with anthrapyrazolone and untreated cells.
Fig. 3 shows the results of absorbance measurement at a wavelength of 450 nm for comparing tyrosinase activities of cells treated with anthrapyrazolone and untreated cells.
Fig. 4 shows the cytotoxicity test results of anthra pyrazolone.
이하, 본 발명이 속하는 기술 분야에서 통상의 지식을 가진 자가 용이하게 실시할 수 있도록 본 발명의 실시예에 대하여 첨부한 도면을 참고로 하여 상세히 설명한다. 그러나 본 발명은 여러 가지 상이한 형태로 구현될 수 있으며, 여기에서 설명하는 실시예에 한정되지 않는다.Hereinafter, embodiments of the present invention will be described in detail with reference to the accompanying drawings so that those skilled in the art can easily carry out the present invention. The present invention may, however, be embodied in many different forms and should not be construed as limited to the embodiments set forth herein.
본 발명은 하기 화학식 1로 표시되는 안트라피라졸론(Anthrapyrazolone)을 유효성분으로 포함하는 피부 미백용 조성물을 제공한다:The present invention provides a skin whitening composition comprising anthrapyrazolone represented by the following formula (1) as an active ingredient:
[화학식 1][Chemical Formula 1]
본 발명에서, 안트라피라졸론은 JNK(c-Jun N-terminal kinase) 저해제로 사용되는 물질로서, 1,9-피라졸로안트론(1,9-Pyrazoloanthrone), SP600125로도 알려져 있다.In the present invention, anthrapyrazolone is a substance used as a c-Jun N-terminal kinase (JNK) inhibitor, also known as 1,9-pyrazoloanthrone, SP600125.
c-JUN은 사람의 JUN 유전자에 의하여 발현되는 단백질이며, JNK는 상기 c-JUN의 53번 및 73번 세린에 결합하여 이들을 인산화시키는 효소이다. JNK는 스트레스 자극, 즉, 사이토카인, 삼투압 충격 등에 의하여 반응한다. JNK가 참여하는 신호 전달계는 포유류 및 곤충의 염증 반응에 관여하는 것으로 알려져 있다.c-JUN is a protein expressed by a human JUN gene, and JNK is an enzyme that binds to and phosphorylates serine 53 and 73 of c-JUN. JNK responds by stress stimulation, that is, cytokine, osmotic shock, and the like. Signaling systems involving JNK are known to be involved in the inflammatory response of mammals and insects.
본 발명자들은 JNK 저해제인 안트라피라졸론을 피부 미백용 조성물의 유효성분으로 적용하였으며, 그 결과 소량으로도 높은 미백 효과를 나타내는 점을 확인하였다. 이러한 안트라피라졸론은 세포 독성을 나타내지 않으므로, 화장료 조성물, 식품 조성물의 성분으로 포함될 수 있다.The present inventors have applied an anthrapyrazolone, which is a JNK inhibitor, as an effective ingredient of a composition for skin whitening, and found that it shows a high whitening effect even in a small amount. Since such anthrapyrazolone does not exhibit cytotoxicity, it can be included as a component of a cosmetic composition or a food composition.
이때 사용되는 안트라피라졸론의 입수 방법은 특별히 제한되지 않으며, 시판되는 것을 구입하거나 직접 제조하여 사용할 수 있다.The method of obtaining the anthra pyrazolone to be used at this time is not particularly limited, and a commercially available anthra pyrazolone can be obtained or used directly.
본 발명에 따른 피부 미백용 조성물에서, 안트라피라졸론은 조성물 총 중량의 0.001 내지 10 중량%로 포함되는 것이 바람직하다. 만일 그 함량이 상기 범위 미만이면 피부 미백 효과를 확보하기 어려우며, 상기 범위를 초과하면 자극을 초래할 수 있으므로, 상기 범위 내에서 적절히 조절한다.In the skin whitening composition according to the present invention, the anthrapyrazolone is preferably contained in an amount of 0.001 to 10% by weight based on the total weight of the composition. If the content is less than the above range, skin whitening effect is difficult to be ensured. If the content exceeds the above range, irritation may be caused.
본 발명의 안트라피라졸론을 유효성분으로 포함하는 피부 미백용 조성물은 화장료 조성물일 수 있다.The skin whitening composition comprising the anthrapyrazolone of the present invention as an active ingredient may be a cosmetic composition.
본 발명에 따른 화장료 조성물은 당업계에서 통상적으로 제조되는 어떠한 제형으로도 제조될 수 있으며, 예를 들어, 용액, 현탁액, 유탁액, 페이스트, 겔, 크림, 로션, 파우더, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션 또는 스프레이 등으로 제형화 될 수 있으나, 이에 한정되는 것은 아니다. 보다 상세하게는, 썬 크림, 유연 화장수, 수렴 화장수, 영양 화장수, 영양 크림, 마사지 크림, 에센스, 아이 크림, 팩, 스프레이 또는 파우더의 제형으로 제조될 수 있다.The cosmetic composition according to the present invention may be prepared in any form conventionally produced in the art and may be in the form of solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, oils, powder foundations, Liquid foundation, wax foundation or spray, but the present invention is not limited thereto. More specifically, it can be manufactured in the form of a sun cream, a flexible lotion, a convergent lotion, a nutritional lotion, a nutritional cream, a massage cream, an essence, an eye cream, a pack, a spray or a powder.
또한, 본 발명에 의한 화장료 조성물은 지방 물질, 유기용매, 용해제, 농축제, 겔화제, 연화제, 항산화제, 현탁화제, 안정화제, 발포제(foaming agent), 방향제, 계면활성제, 물, 이온형 또는 비이온형 유화제, 충전제, 금속이온봉쇄제, 킬레이트화제, 보존제, 비타민, 차단제, 습윤화제, 필수 오일, 염료, 안료, 친수성 또는 친유성 활성제, 지질 소낭 또는 화장품에 통상적으로 사용되는 임의의 다른 성분과 같은 화장품학 또는 피부과학 분야에서 통상적으로 사용되는 보조제를 함유할 수 있다. 상기 보조제는 화장품학 또는 피부과학 분야에서 일반적으로 사용되는 양으로 도입된다.In addition, the cosmetic composition according to the present invention can also be used as a cosmetic composition in the form of a cosmetic composition containing a lipid, an organic solvent, a solubilizing agent, a thickening agent, a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, Any other ingredient commonly used in cosmetics, lipid vesicles or cosmetics may be added to the composition, including, but not limited to, nonionic emulsifiers, fillers, sequestering agents, chelating agents, preservatives, vitamins, blocking agents, wetting agents, essential oils, dyes, pigments, Such as < RTI ID = 0.0 > cosmetics < / RTI > or dermatology. Such adjuvants are introduced in amounts commonly used in the cosmetics or dermatological fields.
상기 제형이 페이스트, 크림 또는 겔인 경우에는 담체 성분으로서 동물성유, 식물성유, 왁스, 파라핀, 전분, 트라칸트, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크 또는 산화아연 등이 이용될 수 있다.When the formulation is a paste, cream or gel, an animal oil, a vegetable oil, a wax, a paraffin, a starch, a tracer, a cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as a carrier component .
상기 제형이 파우더 또는 스프레이인 경우에는 담체 성분으로서 락토스, 탈크, 실리카, 알루미늄 히드록시드, 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 is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. In the case of a spray, in particular, chlorofluorohydrocarbons, propane / Or propellants such as dimethyl ether.
상기 제형이 용액 또는 유탁액인 경우에는 담체 성분으로서 용매, 용해 화제 또는 유탁화제가 이용된다. 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 is a solution or an emulsion, a solvent, a dissolving agent or an emulsifying agent is used as a carrier component. For example, fatty acid esters of water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.
상기 제형이 현탁액인 경우에는 담체 성분으로서 물, 에탄올 또는 프로필렌 글리콜과 같은 액상의 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 formulation is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspension such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, a microcrystalline cellulose , Aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.
또한, 본 발명에 따른 피부 미백용 조성물은 식품 조성물일 수 있다.In addition, the composition for whitening skin according to the present invention may be a food composition.
본 발명에 따른 식품 조성물의 제형은 특별히 한정되지 않으나, 예를 들면 정제, 캅셀, 분말, 액상, 과립, 환, 편상, 페이스트상, 시럽, 겔, 젤리, 바 또는 드링크제일 수 있다.The formulation of the food composition according to the present invention is not particularly limited and may be, for example, tablets, capsules, powders, liquids, granules, pills, flakes, pastes, syrups, gels, jellies, bars or drinks.
또한, 상기 식품 조성물은 통상적으로 사용되는 부형제, 결합제, 붕해제, 감미제, 방향제, 착색제, 보존제로 이루어지는 군으로부터 선택된 적어도 하나 이상을 더 포함할 수 있다. 이러한 부가 성분의 종류 및 함량은 본 발명에서 특별히 제한하지 않으며, 필요에 따라 적절히 조절될 수 있다.In addition, the food composition may further include at least one selected from the group consisting of excipients, binders, disintegrants, sweeteners, fragrances, colorants and preservatives conventionally used. The kind and content of these additional components are not particularly limited in the present invention and can be appropriately adjusted as needed.
상기 부형제는 제제를 섭취하기 쉽게 하거나 일정한 형태를 만들기 위하여 첨가되는 물질이면 본 발명에서 특별히 제한하지 않는다. 이러한 부형제의 예로는 전분, 칼슘 카보네이트, 수크로오스, 락토오스, 젤라틴, 미결정 셀룰로오스, 소듐 라우릴 설페이트, 소듐 알지네이트, 인산칼슘 등을 들 수 있으나, 이에 제한되는 것은 아니다.The excipient is not particularly limited in the present invention as long as it is a substance that is easily added to the formulation or added to make a certain form. Examples of such excipients include, but are not limited to, starch, calcium carbonate, sucrose, lactose, gelatin, microcrystalline cellulose, sodium lauryl sulfate, sodium alginate, calcium phosphate and the like.
상기 결합제는 제제의 형태가 유지될 수 있도록 하는 물질로서, 예를 들어 물, 메타크릴산 공중합체의 수성 현탁액, 에틸셀룰로오스 수성 현탁액, 및 폴리비닐아세테이트 수성 현탁액으로부터 선택되는 1종 이상일 수 있다.The binder may be at least one selected from water, aqueous suspension of methacrylic acid copolymer, aqueous ethylcellulose suspension, and aqueous polyvinyl acetate suspension to maintain the form of the formulation.
상기 붕해제는 체내 소화관 중에서 붕해를 촉진하기 위한 것으로서, 예를 들어 히드록시프로필메칠셀룰로오스, 벤토나이트, 히드록시프로필스타치, 카르복시메칠셀룰로오스나트륨, 알긴산나트륨, 라우릴황산나트륨, 무수규산, 1 -히드록시프로필셀룰로오스, 덱스트란, 이온교환수지, 초산폴리비닐, 포름알데히드처리 카제인 및 젤라틴, 알긴산, 아밀로오스, 구아르고무(Guar gum), 중조 폴리비닐피롤리돈, 아라비아고무, 아밀로펙틴, 펙틴, 폴리인산나트륨, 에칠셀룰로오스, 백당, 및 규산마그네슘알루미늄으로부터 선택되는 1종 이상일 수 있다.The disintegrant is for promoting disintegration in the gastrointestinal tract, and includes, for example, hydroxypropylmethylcellulose, bentonite, hydroxypropyl starch, carboxymethylcellulose sodium, sodium alginate, sodium lauryl sulfate, silicic anhydride, Propyl cellulose, dextran, ion exchange resins, polyvinyl acetate, formaldehyde treated casein and gelatin, alginic acid, amylose, guar gum, neutral polyvinylpyrrolidone, gum arabic, amylopectin, pectin, sodium polyphosphate , Ethylcellulose, white sugar, and magnesium aluminum silicate.
상기 감미제는 쓴 맛을 차폐하는 역할을 하는 것으로서, 예를 들어 백설탕, 포도당, 올리고당, D-소르비톨, 아스파탐, 감초추출물, 에리스리톨 등을 사용할 수 있다.The sweeteners serve to mask bitter taste, and for example, white sugar, glucose, oligosaccharide, D-sorbitol, aspartame, licorice extract, erythritol and the like can be used.
상기 방향제로는 예를 들어 오렌지유, 과즙엑스, 계피유, 스페아민트유, 박하수, 바닐라, 페퍼민트유, 장미유, 레몬유 등을 사용할 수 있다.Examples of the flavoring agent include orange oil, fruit juice extract, cinnamon oil, spearmint oil, peppermint, vanilla, peppermint oil, rose oil, and lemon oil.
상기 착색제로는 예를 들어 식용합성색소와 같은 인공착색제; 치차황색소, 코치닐추출색소, 카라멜색소, 홍국적색소, 사프란색소와 같은 천연착색제; 등을 사용할 수 있다.Examples of the coloring agent include an artificial coloring agent such as an edible synthetic pigment; Natural coloring agents such as tooth yellow cow, cochineal extract color, caramel color, red national color, safflower color; Etc. may be used.
상기 보존제로는 예를 들어 데히드로초산류, 소르빈산류, 안식향산류, 프로피온산류, 파라옥시안식향산에스테르류 등을 사용할 수 있다.Examples of the preservative include dehydroacetic acid, sorbic acid, benzoic acid, propionic acid, and paraoxybenzoic acid esters.
그 밖에도, 본 발명의 식품 조성물은 그레이프프루트, 사과, 오렌지, 레몬, 파인애플, 바나나, 배 등의 각종 과즙(농축 과즙, 분말 과즙 등이어도 좋다); 비타민류(팔미트산 레티놀, 리보플라빈, 피리독신, 시아노코발아민(cyanocobalamine), 아스코르빈산 나트륨, 니코틴산 아미드, 판토텐산 칼슘, 엽산, 비오틴, 콜레칼시페롤(cholecalciferol), 중주석산 콜린, 토코페롤, β-카로틴 등의 수용성 및 지용성 비타민류); 아미노산, 핵산 및 그들의 염류(글루탐산, 글루탐산나트륨, 글리신, 알라닌, 아스파라긴산, 아스파라긴산 나트륨, 이노신산 등); 식물 섬유(폴리덱스트로즈, 펙틴, 크산탄 고무, 글루코만난, 알긴산 등); 또는 미네랄류(염화 나트륨, 초산 나트륨, 황산 마그네슘, 염화 칼륨, 염화 마그네슘, 탄산 마그네슘, 염화 칼슘, 인산 2칼륨, 인산 1나트륨, 글리세로 인산 칼슘, 구연산 제1철 나트륨, 구연산철 암모늄, 구연산철, 황산망간, 황산구리, 요오드화나트륨, 솔빈산칼륨, 아연,망간, 구리, 요오드, 코발트 등) 등의 기타 첨가제를 더 포함할 수 있다.In addition, the food composition of the present invention may be various kinds of fruit juice such as grapefruit, apple, orange, lemon, pineapple, banana, and pear (may be concentrated juice, powdered juice, etc.); Vitamins (such as retinol palmitate, riboflavin, pyridoxine, cyanocobalamine, sodium ascorbate, nicotinamide, calcium pantothenate, folic acid, biotin, cholecalciferol, chondroitin cholinic acid, tocopherol, - water-soluble and fat-soluble vitamins such as carotene); Amino acids, nucleic acids and salts thereof (glutamic acid, sodium glutamate, glycine, alanine, aspartic acid, sodium aspartate, inosine, etc.); Vegetable fibers (polydextrose, pectin, xanthan gum, glucomannan, alginic acid, etc.); Or minerals such as sodium chloride, sodium acetate, magnesium sulfate, potassium chloride, magnesium chloride, magnesium carbonate, calcium chloride, dipotassium phosphate, monosodium phosphate, calcium glycerophosphate, sodium ferrous citrate, Manganese sulfate, copper sulfate, sodium iodide, potassium sorbate, zinc, manganese, copper, iodine, cobalt and the like).
실험예 1: 멜라닌 생성량 측정Experimental Example 1: Measurement of Melanin Production
멜라닌 생성이 과도한 MNT-1 세포(Human melanoma cell line, Lonza, SWISS)에 10 μM 안트라피라졸론(SP600125)을 이틀간 처리한 후, 세포 용해질을 원심분리(eppendorf, centrifuge 5415R, Germany)하고 그 펠렛을 분리해 색깔을 관찰하였다(도 1). 그런 다음, 수산화나트륨으로 상기 펠렛 속의 내용물을 용해시키고, 멜라닌 색소에 특이적인 450 nm 파장에 대한 흡광도를 측정하고 전체 단백질 양으로 보정하였다. 이때 대조군(control)으로서는 안트라피라졸론을 처리하지 않은 MNT-1세포를 이용하였다(도 2).After lysing 10 μM anthrapyrazolone (SP600125) for 2 days in MNT-1 cells (human melanoma cell line, Lonza, SWISS) with excessive melanogenesis, the cell lysate was centrifuged (eppendorf, centrifuge 5415R, Germany) And the color was observed (FIG. 1). The contents of the pellet were then dissolved in sodium hydroxide and the absorbance at 450 nm wavelength specific for the melanin pigment was determined and corrected for the total protein amount. At this time, MNT-1 cells not treated with anthra pyrazolone were used as a control (Fig. 2).
도 1을 보면, 안트라피라졸론을 처리한 세포에서 멜라닌 색소의 양이 감소한 것을 알 수 있으며, 이는 도 2의 흡광도 측정 결과에서도 확인된다. 이로부터 안트라피라졸론이 멜라닌 색소 생성을 저해하는 역할을 한다는 것을 알 수 있다.1, it can be seen that the amount of melanin pigment decreased in cells treated with anthra pyrazolone, which is also confirmed in the results of the absorbance measurement of FIG. From this, it can be seen that anthrapyrazolone plays a role in inhibiting melanin pigment formation.
실험예 2: 티로시나제 활성도 측정Experimental Example 2: Measurement of tyrosinase activity
멜라닌 합성에 관여하는 주요 효소인 티로시나제(tyrosinase)의 활성에 미치는 안트라피라졸론의 영향을 확인하기 위하여 다음과 같은 실험을 수행하였다. 멜라닌 생성이 과도한 MNT-1 세포에 10 μM 안트라피라졸론을 이틀간 처리한 후, 세포를 용해하였다. 세포 용해질에 DOPA(dihydroxyphenylalanine)를 첨가한 다음, 1시간 후 티로시나제의 작용으로 생성된 도파크롬(dopachrome)의 양을 확인하기 위해 450 nm의 흡광도를 측정하였다. 이때 대조군으로서 안트라피라졸론을 처리하지 않은 MNT-1세포에 대하여도 동일한 실험을 수행하였다.The following experiment was conducted to confirm the effect of anthrapyrazolone on the activity of tyrosinase, a major enzyme involved in melanin synthesis. MNT-1 cells with excessive melanin production were treated with 10 [mu] M anthrapyrazolone for two days, and then the cells were lysed. DOPA (dihydroxyphenylalanine) was added to the cell lysate. After 1 hour, the absorbance at 450 nm was measured to confirm the amount of dopachrome produced by the action of tyrosinase. At this time, the same experiment was performed on MNT-1 cells not treated with anthra pyrazolone as a control group.
그 결과, 도 3에서 나타난 바와 같이, 안트라피라졸론을 처리한 세포의 경우 티로시나제의 활성도가 비처리 대조군에 비하여 약 40 % 감소한 것을 확인하였다. 이로부터, 안트라피라졸론은 티로시나제의 활성을 감소시켜 멜라닌 합성을 억제한다는 점을 알 수 있다.As a result, as shown in FIG. 3, it was confirmed that the activity of tyrosinase was reduced by about 40% in cells treated with anthrapyrazolone, compared with the untreated control. From this, it can be seen that anthrapyrazolone reduces the activity of tyrosinase and inhibits melanin synthesis.
실험예 3: 세포 독성 실험Experimental Example 3: Cytotoxicity test
안트라피라졸론의 독성 유무를 확인하기 위하여 다음과 같은 실험을 수행하였다. 인간 배아 간세포 HEK293을 96 웰 플레이트(well plate)에 넣고 (3*103 cells) 24시간 동안 배양하였다. 그런 다음, 안트라피라졸론의 농도를 달리하여 상기 배아 간세포에 처리하고, 100 μL의 CCK-8 용액을 첨가하여 37 ℃에서 3시간 동안 배양한 후, 450 nm에서의 흡광도를 측정하여 세포 생존도를 측정하였다. 도 4는 상기 흡광도 측정 그래프이며, 안트라피라졸론을 처리하지 않은 세포군의 흡광도를 1로 하였을 때 나머지 실험군들의 상대적인 흡광도를 나타낸 것이다.In order to confirm the toxicity of anthra pyrazolone, the following experiment was conducted. Human embryonic stem cell HEK293 was added to a 96-well plate (3 * 10 3 cells) and cultured for 24 hours. Then, 100 μL of CCK-8 solution was added to the embryonic stem cells treated at different concentrations of anthra pyrazolone, and incubated at 37 ° C. for 3 hours. The absorbance at 450 nm was measured to determine cell viability Respectively. FIG. 4 is a graph showing the absorbance of the test sample. FIG. 4 is a graph showing the relative absorbance of the remaining test groups when the absorbance of an anthrapyrazolone-untreated cell group is 1. FIG.
실험 결과, 안트라피라졸론 처리군의 세포 생존도는 비처리군과 비교하여 크게 감소하지 않았다. 이와 같이 안트라피라졸론은 세포 독성을 나타내지 않으므로, 피부 미백 효과를 얻기 위하여 인체에 적용하기 적합하다. As a result, the cell viability of the anthrapyrazolone-treated group was not significantly reduced compared to the untreated group. Since anthrapyrazolone does not exhibit cytotoxicity, it is suitable for application to a human body in order to obtain a skin whitening effect.
이하 본 발명의 제형예를 설명한다. 그러나 본 발명에 따른 피부 미백용 조성물의 제형이 이들 예로만 한정되는 것은 아니다.Hereinafter, a formulation example of the present invention will be described. However, the formulation of the skin whitening composition according to the present invention is not limited to these examples.
제형예 1: 화장수Formulation Example 1: Lotion
아래 표에 기재된 조성으로 통상의 방법에 따라 화장수를 제조하였다.Lotion was prepared according to a conventional method with the composition shown in the following table.
제형예 2: 영양 크림Formulation Example 2: Nourishing cream
아래 표에 기재된 조성으로 통상의 방법에 따라 영양 크림을 제조하였다.Nutritive creams were prepared according to a conventional method with the compositions shown in the following table.
제형예 3: 마사지 크림Formulation Example 3: Massage cream
아래 표에 기재된 조성으로 통상의 방법에 따라 마사지 크림을 제조하였다.A massage cream was prepared according to a conventional method with the composition shown in the following table.
제형예 4: 팩Formulation Example 4: Pack
아래 표에 기재된 조성으로 통상의 방법에 따라 팩을 제조하였다.A pack was prepared according to a conventional method with the composition shown in the following table.
제형예 5: 드링크제Formulation Example 5: Drinking agent
안트라피라졸론 80mg, 비타민 E 9mg, 비타민 C 9mg, 포도당 10g, 구연산 0.6g, 및 액상 올리고당 25g을 혼합한 후, 정제수 300㎖를 가하여 각 병에 200㎖씩 되도록 충진하였다. 그런 다음, 130에서 4~5 초간 살균하여 드링크제를 제조하였다.Anthrapyrazolone (80 mg), vitamin E (9 mg), vitamin C (9 mg), glucose (10 g), citric acid (0.6 g) and liquid oligosaccharide (25 g) were mixed and purified water (300 ml) was added. Then, the drink was sterilized at 130 for 4 to 5 seconds to prepare a drink.
Claims (6)
[화학식 1]
A composition for skin whitening comprising an anthra pyrazolone represented by the following formula (1) as an active ingredient.
[Chemical Formula 1]
상기 안트라피라졸론은 피부 미백용 조성물 총 중량의 0.001 내지 10 중량%로 포함되는 것을 특징으로 하는 피부 미백용 조성물.The method according to claim 1,
Wherein the anthrapyrazolone is contained in an amount of 0.001 to 10% by weight based on the total weight of the composition for skin whitening.
상기 피부 미백용 조성물은 화장료 조성물인 것을 특징으로 하는 피부 미백용 조성물.The method according to claim 1,
Wherein the skin whitening composition is a cosmetic composition.
상기 화장료 조성물은 용액, 현탁액, 유탁액, 페이스트, 겔, 크림, 로션, 파우더, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션 또는 스프레이로 제형화 되는 것을 특징으로 하는 피부 미백용 조성물.The method of claim 3,
Wherein the cosmetic composition is formulated into a solution, suspension, emulsion, paste, gel, cream, lotion, powder, oil, powder foundation, emulsion foundation, wax foundation or spray.
상기 피부 미백용 조성물은 식품 조성물인 것을 특징으로 하는 피부 미백용 조성물.The method according to claim 1,
Wherein the composition for skin whitening is a food composition.
상기 식품 조성물은 정제, 캅셀, 분말, 액상, 과립, 환, 편상, 페이스트상, 시럽, 겔, 젤리, 바 또는 드링크제로 제형화 되는 것을 특징으로 하는 피부 미백용 조성물.6. The method of claim 5,
Wherein the food composition is formulated into tablets, capsules, powders, liquids, granules, rings, flakes, pastes, syrups, gels, jellies, bars or drinks.
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