KR20170078259A - Composition for improving skin conditions comprising Isosteviol - Google Patents
Composition for improving skin conditions comprising Isosteviol Download PDFInfo
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- KR20170078259A KR20170078259A KR1020150188605A KR20150188605A KR20170078259A KR 20170078259 A KR20170078259 A KR 20170078259A KR 1020150188605 A KR1020150188605 A KR 1020150188605A KR 20150188605 A KR20150188605 A KR 20150188605A KR 20170078259 A KR20170078259 A KR 20170078259A
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- skin
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/368—Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat
Abstract
본 발명은 피부에서 항당화, 흑화, 주름 개선, 탄력 개선 또는 피부 보습에 우수한 효과를 가지는 화장료 조성물, 약학적 조성물 및 건강식품에 관한 것이다. 본 발명의 조성물은 피부 또는 모발 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습에 우수한 효과를 나타낸다. 본 발명 조성물의 유효성분인 화학식 1의 화합물은 피부에 안전하면서도 피부 상태 개선 효과가 우수한 화장품 원료, 약학 성분 또는 건강식품 원료로 이용될 수 있다.The present invention relates to a cosmetic composition, a pharmaceutical composition and a health food, which have excellent effects on skin antigialization, blackening, wrinkle improvement, elasticity improvement or skin moisturization. The composition of the present invention exhibits excellent effects on skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturization. The compound of Chemical Formula (1), which is an active ingredient of the composition of the present invention, can be used as a cosmetic raw material, a pharmaceutical ingredient or a health food raw material which is safe for skin and has excellent skin condition improving effect.
Description
본 발명은 피부 상태의 개선에 우수한 효과를 가지는 조성물에 관한 것으로서, 보다 구체적으로 피부의 흑화, 주름 개선, 탄력 개선 또는 보습에 우수한 효과를 가지는 화장료 조성물, 약학적 조성물 및 건강식품에 관한 것이다.More particularly, the present invention relates to a cosmetic composition, a pharmaceutical composition, and a health food which have excellent effects on blackening, wrinkling, improvement in elasticity, or moisturization of the skin.
경제성장에 따른 문화수준의 향상으로 건강뿐 아니라 외모에 대한 관심이 높아지고 있으며, 피부를 가꾸고 건강하게 유지하고자 하는 욕구 또한 증가하고 있다. 최근에는 건강한 피부 유지뿐만 아니라, 피부를 건강하게 보이기 위한 셀프 태닝(Self tanning) 제품들의 사용도 증가하고 있다. 셀프 태닝은 자외선 과다노출에 의한 광노화를 피할 수 있고, 햇빛이 비치지 않는 계절에도 태닝 효과를 낼 수 있어 관심이 증대되고 있다. 최근 사용되는 셀프 태닝 제품들은 에리트룰로스(Erythrulose)나 디하이드록시아세톤(Dihydroxyacetone)과 같이 피부 각질층의 케라틴과 결합해 피부에 일시적으로 색소를 입혀 염색시키는 방법이 사용되고 있다. 하지만, 디하이드록시아세톤의 경우 사용방법에 따라 피부톤이 균일하지 못하는 경우가 많고, 각질이 벗겨지면서 피부가 얼룩져 보이는 문제점이 있으며, 에리트룰로스는 보다 균일한 피부톤으로 발색되나 발색력이 너무 약한 문제점이 있다. 또한, 피부에 바른 후 24시간내에 자외선에 노출될 경우 피부의 활성산소 생성을 촉진시킨다고 보고되었다. Due to the economic growth, the interest in the appearance as well as the health is increasing, and the desire to keep skin and keep healthy is also increasing. In recent years, not only healthy skin maintenance but also self-tanning products have been increasingly used to make skin look healthier. Self-tanning can avoid photo-aging due to overexposure to ultraviolet light, and it is possible to produce a tanning effect even in a season when sunlight does not shine. Recently used self-tanning products have been combined with keratin in the stratum corneum, such as Erythrulose and Dihydroxyacetone, to temporarily dye the skin and dye it. However, in the case of dihydroxyacetone, the skin tone is often not uniform according to the usage method, and there is a problem that the skin is smudged due to peeling of the keratin, and the erythrulose is colored with a more uniform skin tone, . In addition, it has been reported that exposure to ultraviolet light within 24 hours after application to the skin promotes active oxygen production of the skin.
또한, 백발은 일반적으로 연령이 높아지면 발생하는 것으로 노령이라는 느낌을 주며, 특히 젊은 나이에 있어서의 백발은 스트레스의 원인이 된다. 백모는 모발색이 밝은 백인에 비해 흑색 모발을 가진 동양인에게 더욱 뚜렷이 나타나며 보건미용, 심리적인 면에서 연구대상이 되고 있다. 멜라닌은 적황색인 페오멜라닌(Pheomelanin)과 흑갈색인 유멜라닌(Eumelanin)으로 나뉘며, 모발에 있어서의 멜라닌은 모발의 색상을 결정하는 중요한 인자로서, 모발상부에 존재하는 멜라노사이트 내에서 생성된 멜라닌은 모발피질세포 케라티노사이트에 전달된 후, 모발의 성장과 함께 위쪽으로 이동한다. 생리적 노화의 한 현상으로서 인식되는 백발은 모발 멜라노사이트의 수적 감소 및 멜라노사이트의 기능저하에 의한 멜라닌 생성의 감소에 의해 유발된다. 현재 백모의 해결방안으로 염색시술이 사용되고 있으나, 염색은 일시적인 방법으로 백발의 성장에 의해 다시 염색하지 않으면 안되고, 모발 염색약의 염료 속에 포함되어 있는 성분이 자극성분이 되어 접촉성 피부염 또는 피부 알러지를 일으켜 문제시 되고 있다.In addition, gray hair generally occurs when the age is higher, giving the feeling of old age, and gray hair, especially at a young age, causes stress. White moths are more prominent in Oriental populations with black hair than white ones with bright hair color, and are being studied in health and beauty and psychology. Melanin is divided into red-yellow Pheomelanin and black-brown Eumelanin. Melanin in hair is an important factor that determines the color of hair. Melanin produced in the melanocyte present in the hair, After being transferred to the cortical cell keratinocytes, the hair moves upward with the growth of the hair. The gray hair, recognized as a phenomenon of physiological aging, is caused by a decrease in the number of hair melanocytes and a decrease in the production of melanin due to a decrease in function of melanocytes. Dyeing is currently used as a solution to white moth, but dyeing must be re-pigmented by growth of gray hair in a temporary manner, and the ingredients contained in the dye of the hair dyes become irritants and cause contact dermatitis or skin allergy It is becoming a problem.
콜라겐은 피부의 섬유아세포(Fibroblast)에서 생성되는 주요 기질 단백질로서 세포외 간질에 존재하고, 중요한 기능으로는 피부의 기계적 견고성, 결합조직의 저항력과 조직의 결합력, 세포접착의 지탱, 세포분할과 분화(유기체의 성장 혹은 상처 치유시)의 유도 등이 알려져 있다. 이러한 콜라겐은 연령 및 자외선 조사에 의한 광 노화에 의해 감소하며, 콜라겐을 분해하는 콜라게나제 효소 활성으로 콜라겐 감소가 촉진된다. 이는 피부의 주름 형성과 밀접한 연관이 있다고 알려져 있다. Collagen is a major substrate protein produced in the fibroblasts of the skin and exists in extracellular epilepsy. Its important functions are mechanical durability of the skin, resistance of connective tissues and binding force of tissues, support of cell adhesion, cell division and differentiation (Induction of growth of an organism or wound healing) are known. Such collagen is reduced by photoaging by age and ultraviolet irradiation, and collagenase activity, which degrades collagen, promotes collagen reduction. This is known to be closely related to the formation of wrinkles in the skin.
또한, 엘라스틴(Elastin) 섬유는 콜라겐과 가교 결합을 형성하며 피부 탄력에 관여하고 있는 주름 생성에 중요한 피부 구성성분이다. 엘라스틴 섬유의 결핍과 응집, 엘라스틴 분해 효소인 엘라스테이즈(Elastase)의 활성도의 현격한 증가는 피부 주름생성 요인 중의 하나로 밝혀지고 있다. 엘라스테이즈는 엘라스틴을 분해할 수 있는 유일한 효소로서 이에 대한 저해는 피부 주름 개선을 근본적으로 줄여 줄 수 있다고 알려져 있다.In addition, Elastin fiber forms crosslinks with collagen and is a skin constituent important for wrinkle formation involved in skin elasticity. The deficiency and aggregation of elastin fibers and the marked increase in the activity of the elastin degrading enzyme Elastase have been found to be one of the causes of skin wrinkles. It is known that Elastase is the only enzyme capable of degrading elastin, and its inhibition can fundamentally reduce the wrinkles of the skin.
한편, 콜라겐 및 엘라스틴 섬유는 진피층 내의 수분 보유에 중요한 역할을 하는 기질 단백질로 이러한 기질 단백질이 수분을 흡착하며, 이들이 이루는 구조 내부에 수분 보유력을 높여 피부가 적정 수분을 함유한 상태를 유지할 수 있도록 해주며, 이를 통해 피부의 탄력을 유지하는데 관여한다고 알려져 있다.On the other hand, collagen and elastin fibers are substrate proteins that play an important role in water retention in the dermal layer. These protein proteins adsorb moisture and increase the water holding capacity inside the structure, thereby allowing the skin to maintain proper moisture content. And it is known to be involved in maintaining the elasticity of the skin.
또한, 피부의 섬유아세포(Fibroblast)에서 생성되는 탄력섬유(Elastic fiber)는 콜라겐과 가교 결합을 형성하며 피부 탄력에 관여하고 있는 주름 생성에 중요한 피부 구성성분이다. 탄력섬유의 결핍 및 분해는 피부 주름생성과 탄력 저하의 주요 요인 중의 하나로 밝혀졌다. In addition, the elastic fiber produced in the fibroblast of the skin forms a cross-link with collagen, and is a skin constituent important for wrinkle formation which is involved in skin elasticity. Deficiency and decomposition of elastic fibers were found to be one of the main factors of skin wrinkle formation and elasticity reduction.
탄력섬유를 구성하고 있는 피브릴린-1 단백질은 세포의 외부에 존재하는 미세섬유(microfibril)의 일종으로 탄력섬유가 형성될 때 뼈대를 형성하는 기능을 담당한다고 알려졌다. 피브릴린은 접착제와 같은 역할을 하여 우리 몸의 각 부분이 결합 및 유지될 수 있도록 도와 주는데, 피브릴린-1 유전자의 돌연변이는 폐, 피부 또는 골격 등에 이상을 일으키는 말판증후군(Marfan syndrome)의 원인이라고 알려졌다. 최근에는 피브릴린-1이 TGF-beta의 저장소 역할을 수행한다는 것이 밝혀졌다.The fibrillin-1 protein, which is a constituent of elastic fibers, is a type of microfibril that exists outside the cell and is known to function as a skeleton when elastic fibers are formed. Fibrillin acts as an adhesive to help each part of our body bind and maintain. Mutations in the fibrilin-1 gene are caused by the presence of Marfan syndrome, which causes abnormalities in the lungs, skin or skeletal system. It was known to be the cause. Recently, it has been found that fibrilin-1 acts as a reservoir of TGF-beta.
현재, 주름개선 화장료로는 레티노이드, 아데노신, 동물태반유래 단백질, 클로렐라 추출물 등이 알려져 있다. 가장 잘 알려져 있는 레티놀은 콜라겐 합성을 촉진하며 엘라스테이즈 효소를 저해하는 물질이지만 불안정하며, 피부 적용시 자극, 발적 등의 안전성 문제로 사용량의 제한이 있으며, 클로렐라 추출물 등은 효과가 미미하여 실질적으로 피부주름 개선효과를 기대하기가 어렵다고 알려져 있다.Presently, retinoids, adenosine, animal placenta-derived proteins, chlorella extract, and the like are known to improve wrinkles. The best known retinol promotes collagen synthesis and inhibits elastase enzymes, but it is unstable. When applied to the skin, it has a limited use due to safety problems such as irritation and redness, and chlorella extract has little effect, It is known that it is difficult to expect a wrinkle-improving effect.
당화(Glycation)는 일반적으로 효소의 관여 없이 일어나는 단백질 또는 지방에 포도당 또는 과당과 같은 단순당이 공유결합을 형성하는 반응을 의미한다. 당화는 일련의 아마도리 전위(Amadori rearrangement), 마이야르 반응(Maillard Reaction)으로 알려진 복잡한 화학적 반응을 거쳐 일어나게 되며 그 결과 최종당화산물(AGEs: Advanced glycation endproducts)이 생성된다.Glycation generally refers to a reaction in which a simple sugar such as glucose or fructose forms a covalent bond to a protein or fat that occurs without involvement of the enzyme. Saccharification takes place through a series of complex chemical reactions known as Amadori rearrangement, Maillard reaction, which results in the formation of advanced glycation endproducts (AGEs).
한편 단백질의 당화 과정은 효소 작용이 관여하지 않아 천천히 일어나게 되고 그 결과 콜라겐과 같이 반감기가 긴 단백질에서 더욱 많은 영향을 끼치게 된다. 최종당화산물을 분석한 결과 나이가 많을수록 당화된 콜라겐이 축적되는 양상을 보였으며, 최종당화산물의 축적은 단백질을 단단하고 더욱 부서지기 쉬운 상태로 변화시키며, 당화된 콜라겐은 진피층의 세포 외 기질에서 콜라겐이 적절한 구조를 형성하지 못하도록 함으로써 피부의 탄력을 잃게 하고 주름 생성을 촉진한다(Dyer, D. G. et al., The Journal of Clinical Investigation, 9, p. 2463, 1993).On the other hand, the glycation process of the protein does not involve the enzymatic action, so it occurs slowly, and as a result, the protein having a longer half-life such as collagen has more influence. Analysis of the final glycation products revealed that the more aged the glycated collagen was accumulated, the accumulation of the final glycated product changed the protein to a harder and more brittle state, and the glycated collagen was found in the extracellular matrix of the dermal layer (Dyer, DG et al. , The Journal of Clinical Investigation, 9, p. 2463, 1993), by inhibiting collagen from forming a proper structure and thereby reducing skin elasticity and promoting wrinkle formation.
당화를 억제하는 물질로 아미노구아니딘(Aminoguanidine), 피리독사민(Pyridoxamine), 아스피린(Aspirin) 등이 알려져 있으나, 이들 물질은 피부에 대한 안전성의 문제로 사용량의 제한이 있거나, 효과가 미미하여 실질적으로 효과를 기대할 수 없는 문제점이 있다.Aminoguanidine, pyridoxamine, and aspirin are known to inhibit glycosylation. However, these substances are limited in their use due to the safety of the skin, There is a problem that can not be expected.
따라서, 생체에 안전하고, 유효성분이 피부에 안전하고 안정성이 높으며, 무엇보다도 피부에서 항당화, 흑화, 주름 개선, 탄력 개선 효과가 있다고 기존에 알려진 물질보다 효과가 우수한 항당화, 흑화, 주름 개선, 탄력 개선용 성분의 개발이 절실히 요망되고 있다.Therefore, it has been found that it is safe for the living body, the effective ingredient is safe to the skin and the stability is high, and the anticalcification, the blackening, the wrinkle improvement, Development of a component for improving elasticity is urgently required.
따라서 본 발명이 해결하고자 하는 과제는 위와 같은 문제점을 해결하고, 부작용이 적고 인체에 안전하면서도 피부의 항당화, 흑화, 주름 개선, 탄력 개선 또는 항염 효과가 우수한 새로운 활성 성분, 즉, 활성 성분의 이러한 유용한 용도를 제공하는 것이다.Accordingly, a problem to be solved by the present invention is to solve the above-mentioned problems, and to provide a new active ingredient which is safe for human body and has little side effects and is excellent in antihalation, blackening, wrinkle improvement, elasticity improvement or anti- To provide useful applications.
다시 말해, 본 발명이 해결하고자 하는 과제는 상기 효능이 우수한 활성 성분을 유효성분으로 포함하는 조성물을 제공하는 것이다.In other words, a problem to be solved by the present invention is to provide a composition comprising an active ingredient having excellent efficacy as an active ingredient.
상기 과제를 해결하기 위하여, 본 발명은 아이소스테비올(Isosteviol) 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 유효성분으로 포함하는 피부 또는 모발의 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 조성물, 바람직하게는 화장료 조성물, 약학적 조성물 또는 건강식품을 제공한다. In order to solve the above-mentioned problems, the present invention provides a cosmetic composition for blackening, skin elasticity, skin wrinkle improvement, skin wrinkle improvement, and the like for skin or hair containing isosteviol or a pharmaceutically or cosmetically acceptable salt thereof as an active ingredient, Or skin moisturizing composition, preferably a cosmetic composition, a pharmaceutical composition or a health food.
즉, 본 발명은 아이소스테비올 또는 이의 약학적 또는 화장학적으로 허용 가능한 염의 화장료 조성물 또는 약학적 조성물로서의 용도와 피부 또는 모발의 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 이라는 새로운 용도를 제공한다.That is, the present invention relates to the use of isostearviol or a pharmacologically or cosmetically acceptable salt thereof as a cosmetic composition or a pharmaceutical composition, for use in blackening of skin or hair, for improving skin elasticity, for improving skin wrinkles, It provides a new use.
본 발명의 발명자들은 아이소스테비올이 피부의 콜라겐 생성을 촉진하고, 엘라스테이즈의 활성을 저해함으로써 피부의 주름 및 탄력 개선 효과가 있다는 사실을 발견하고 본 발명을 완성하게 되었다. 또한, 상기 아이소스테비올은 멜라닌의 총량을 증가시켜 피부 또는 모발의 흑화 효과를 나타내는 것을 확인하였다. 또한, 상기 아이소스테비올은 항당화 효과를 나타내어, 피부 주름 및 피부 탄력 개선에 보조적인 역할로 작용하여 상승효과를 나타낼 수 있다.The inventors of the present invention found that isostearvol promotes skin collagen production and inhibits the activity of the elastase, thereby improving wrinkles and elasticity of the skin, thus completing the present invention. In addition, it was confirmed that the isostearvol increased the total amount of melanin and showed blackening effect of skin or hair. In addition, the isostearvol exhibits an antihyperglycosylation effect, and acts as an auxiliary for improving skin wrinkles and skin elasticity, and can exhibit a synergistic effect.
본 발명에 있어서, '흑화 효과'라 함은 피부 또는 모발의 유색 색소가 증가되는 것을 의미하며, 특히 멜라닌 색소의 양이 증가되어 피부 또는 모발이 짙은 색을 나타내게 되는 현상을 의미할 수 있으나, 본 발명은 이러한 기전에 의해 한정되는 것은 아니다.In the present invention, the term 'blackening effect' means that the coloring matter of the skin or hair is increased, and in particular, the amount of the melanin pigment is increased, which means that the skin or hair shows a dark color. The invention is not limited by this mechanism.
본 발명에 있어서, '탄력 또는 피부 탄력 개선'이라 함은 피부가 쳐지거나 늘어지는 정도를 완화시켜주는 것을 의미한다. 또한, 상기 탄력은 엘라스틴과 콜라겐이 충분이 존재하는 상태에서 피부의 탄력성을 유지시켜 주는 것을 의미한다.In the present invention, the term 'improving elasticity or skin elasticity' means reducing the degree to which the skin is stuck or stretched. In addition, the elasticity means that elasticity of the skin is maintained in a state where elastin and collagen are sufficiently present.
본 발명에 있어서, '주름 개선'이라 함은 피부에 주름이 생성되는 것을 예방, 억제 또는 저해하거나, 이미 생성된 주름을 완화시키는 것을 말한다. In the present invention, "improving wrinkles" refers to preventing, suppressing or inhibiting the generation of wrinkles on the skin, or alleviating wrinkles that have already been formed.
본 발명에 있어서, '보습 또는 피부 보습'이라 함은 피부에 수분감을 증가시켜주고, 촉촉한 상태를 유지시키는 것을 의미한다. 피부 보습 효과는 피부의 주름개선 및 탄력 증가에 도움을 줄 수 있다. In the present invention, the term 'moisturizing or skin moisturizing' means increasing the skin moisture and maintaining a moist state. Skin moisturizing effect can help to improve wrinkles and elasticity of skin.
본 발명에 있어서, '항당화' 효과라 함은 진피층의 세포 외 기질에서 콜라겐이 당화되는 것을 막아 피부의 탄력을 증진하고 주름 생성을 방지하는 것을 말한다. 또한, 항당화 효과는 피부 노화에 따라 진피층 상부에 쌓이는 최종당화산물의 생성을 억제한다. 따라서, 본 발명에 있어서 항당화 효과는 피부 탄력 증진 및 주름 개선에 시너지 효과를 발생시킬 수 있다.In the present invention, the 'antagonism' effect means preventing the collagen from being saccharified in the extracellular matrix of the dermal layer, thereby enhancing elasticity of the skin and preventing wrinkle formation. In addition, the anti-glycation effect inhibits the production of a final glycation product accumulated on the dermal layer according to skin aging. Therefore, in the present invention, the anticarcinogenic effect can cause a synergistic effect on skin elasticity enhancement and wrinkle improvement.
본 발명은 상기와 같은 문제점들을 해결하고, 본 발명의 목적을 달성하기 위하여 하기 화학식 1로 대표되는 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 포함하는 조성물을 제공한다. In order to solve the above-mentioned problems and to achieve the object of the present invention, the present invention provides a composition comprising a compound represented by the following Chemical Formula 1, or a pharmaceutically or cosmetically acceptable salt thereof.
[화학식 1][Chemical Formula 1]
상기 화학식 1로 대표되는 화합물은 분자식 C20H30O3, 분자량 318.45을 가지며, 아이소스테비올(Isosteviol); CAS. No. : 27975-19-5; (4α,8β,13β)-13-Methyl-16-oxo-17-norkauran-18-oic acid 으로 명명된다. The compound represented by Formula 1 has a molecular formula C 20 H 30 O 3 , a molecular weight of 318.45, isosteviol; CAS. No. : 27975-19-5; (4α, 8β, 13β) -13-Methyl-16-oxo-17-norauran-18-oic acid.
본 발명은 상기 아이소스테비올의 획득 방법에 특별히 한정되지 않으며, 본 발명이 속한 분야에서 공지된 방법으로 화학적으로 합성하거나, 시판되는 물질을 사용할 수 있다.The present invention is not particularly limited to the method for obtaining isostearic acid, but may be chemically synthesized by a known method in the field of the present invention, or a commercially available substance may be used.
본 발명에 따른 화장료 조성물, 약학적 조성물 및 건강식품에 있어, 상기 아이소스테비올 또는 이의 약학적 또는 화장학적으로 허용 가능한 염의 함량은 화장료 조성물, 약학적 조성물 및 건강식품 전체 중량 대비 0.00001 내지 10 중량%인 것이 바람직하다.In the cosmetic composition, the pharmaceutical composition and the health food according to the present invention, the content of the isostearviol or the pharmaceutically or cosmetically acceptable salt thereof is 0.00001 to 10% by weight based on the total weight of the cosmetic composition, .
본 발명에 있어서, 유효성분으로 사용되는 상기 아이소스테비올은 "약학적 또는 화장학적으로 허용 가능한 염"의 형태로 사용될 수 있다. 상기 아이소스테비올의 "약학적 또는 화장학적으로 허용 가능한 염"은 아이소스테비올에 염기를 부가하여 제조된 염들을 포함할 수 있다. 상기 약학적 또는 화장학적으로 허용 가능한 염을 제조하기 위해 사용 가능한 부가 염은 나트륨, 칼륨, 칼슘, 암모늄, 마그네슘 및 유기 아미노 등으로 이루어진 군에서 선택된 어느 하나 이상의 염을 포함하나, 이에 한정되는 것은 아니다.In the present invention, the isosteviol used as an active ingredient can be used in the form of a "pharmaceutically or cosmetically acceptable salt ". The "pharmaceutically or cosmetically acceptable salt " of the isosteric has may include salts prepared by adding a base to isostearviol. Additional salts that can be used to prepare the pharmaceutically or cosmetically acceptable salts include, but are not limited to, any one or more salts selected from the group consisting of sodium, potassium, calcium, ammonium, magnesium, and organic amino .
본 발명의 아이소스테비올은 수화물, 에탄올화물 등의 형태를 포함하는 용매화된 형태뿐만 아니라 비-용매화된(unsolvated) 형태로 존재할 수도 있다. 본 발명의 아이소스테비올은 결정형 또는 무정형 형태로 존재할 수 있으며, 이러한 모든 물리적 형태는 본 발명의 범위에 포함된다.The isostearviol of the present invention may exist in solvated as well as unsolvated forms, including forms such as hydrates, ethanolates, and the like. The isostearvol of the present invention may exist in crystalline or amorphous form, and all such physical forms are included within the scope of the present invention.
본 발명에 따른 피부 또는 모발 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 조성물은 용액, 외용연고, 크림, 폼, 영양화장수, 유연화장수, 팩, 유연수, 유액, 메이크업베이스, 에센스, 비누, 액체 세정료, 입욕제, 선 스크린크림, 선오일, 현탁액, 유탁액, 페이스트, 겔, 로션, 파우더, 비누, 계면활성제-함유 클린싱, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션, 패취 및 스프레이로 구성된 군으로부터 선택되는 제형으로 제조할 수 있으나, 이에 제한되는 것은 아니다.The composition for skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing treatment according to the present invention may be used as a solution, an external ointment, a cream, a foam, a nutrition lotion, a softening water, a pack, A lotion, a powder, a soap, a surfactant-containing cleansing oil, a powder foundation, an emulsion foundation, a wax foundation, a wax foundation, But is not limited to, a formulation selected from the group consisting of patches and sprays.
또한, 본 발명의 화장료 조성물은 일반 피부 화장료에 배합되는 화장학적으로 허용 가능한 담체를 1종 이상 추가로 포함할 수 있으며, 통상의 성분으로 예를 들면 유분, 물, 계면활성제, 보습제, 저급 알코올, 증점제, 킬레이트제, 색소, 방부제, 향료 등을 적절히 배합할 수 있으나, 이에 제한되는 것은 아니다.In addition, the cosmetic composition of the present invention may further comprise at least one cosmetically acceptable carrier compounded in a cosmetic composition for general skin, and examples thereof include oil, water, a surfactant, a moisturizer, a lower alcohol, A thickening agent, a chelating agent, a coloring matter, an antiseptic, a perfume, and the like may be appropriately compounded, but the present invention is not limited thereto.
본 발명의 화장료 조성물에 포함되는 화장학적으로 허용 가능한 담체는 제형에 따라 다양하다. 본 발명의 제형이 연고, 페이스트, 크림 또는 겔인 경우에는, 담체성분으로서 동물성 유, 식물성 유, 왁스, 파라핀, 전분, 트라칸트, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크, 산화아연 또는 이들의 혼합물이 이용될 수 있다.The cosmetically acceptable carrier contained in the cosmetic composition of the present invention varies depending on the formulations. When the formulation of the present invention is an ointment, a paste, a cream or a gel, the carrier component may be an animal oil, a vegetable oil, a wax, a paraffin, a starch, a tracer, a cellulose derivative, polyethylene glycol, silicon, bentonite, silica, talc, zinc oxide Mixtures of these may be used.
본 발명의 제형이 파우더 또는 스프레이인 경우에는, 담체 성분으로서 락토오스, 탈크, 실리카, 알루미늄 히드록사이드, 칼슘 실케이트, 폴리아미드 파우더 또는 이들의 혼합물이 이용될 수 있고, 특히 스프레이인 경우에는 추가적으로 클로로플루오로히드로카본, 프로판/부탄 또는 디메틸 에테르와 같은 추진제를 포함할 수 있다.When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder or a mixture thereof may be used as the carrier component, Propellants such as fluorohydrocarbons, propane / butane or dimethyl ether.
본 발명의 제형이 용액 또는 유탁액인 경우에는, 담체 성분으로서 용매, 용해화제, 또는 유탁화제가 이용되고 예컨대 물, 에탄올, 이소프로판올, 에틸 카보네이트, 에틸 아세테이트, 벤질 벤조에이트, 프로필렌 글리콜, 1,3-부틸글리콜 오일이 있으며, 특히, 목화씨 오일, 땅콩 오일, 옥수수 배종 오일, 올리브 오일, 피마자 오일 및 참깨 오일, 글리세롤 지방족 에스테르, 폴리에틸렌 글리콜 또는 소르비탄의 지방산 에스테르가 있다.When the formulation of the present invention is a solution or an emulsion, a solvent, a solubilizing agent or an emulsifying agent is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl benzoate, -Butyl glycol oil, and in particular fatty acid esters of cottonseed oil, peanut oil, corn oil, olive oil, castor oil and sesame oil, glycerol aliphatic esters, polyethylene glycols or sorbitan.
본 발명의 제형이 현탁액인 경우에는, 담체 성분으로서 물, 에탄올 또는 프로필렌 글리콜과 같은 액상의 희석제, 에톡실화 이소스테아릴 알코올, 폴리옥시에틸렌 소르비톨 에스테르 및 폴리 옥시에틸렌 소르비탄 에스테르와 같은 현탁제, 미소결정성 셀룰로오스, 알루미늄 메타히드록시드, 벤토나이트, 아가 또는 트라칸트 등이 이용될 수 있다.When the formulation of the present invention 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, Crystalline cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.
본 발명의 제형이 비누인 경우에는 담체 성분으로서 지방산의 알칼리 금속 염, 지방산 헤미에스테르 염, 지방산 단백질 히드롤리제이트, 이세티오네이트, 라놀린 유도체, 지방족 알코올, 식물성 유, 글리세롤, 당 등이 이용될 수 있다.When the formulation of the present invention is a soap, alkali metal salts of fatty acids, fatty acid hemiesters, fatty acid protein hydrolizates, isethionates, lanolin derivatives, aliphatic alcohols, vegetable oils, glycerol, sugars and the like are used as carrier components .
본 발명은 또한 상기 화학식 1로 대표되는 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 개체의 피부에 도포하는 단계를 포함하는, 피부 또는 모발 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습 방법을 제공한다. 상기 개체는 쥐, 가축, 인간 등을 포함하는 포유동물을 제한 없이 포함한다. The present invention also relates to the use of a compound represented by the formula (I) or a pharmaceutically or cosmetically acceptable salt thereof for the treatment of skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, ≪ / RTI > The subject includes, without limitation, mammals including rats, livestock, humans, and the like.
본 발명의 또 다른 실시예에 따르면, 본 발명은 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 유효성분으로 함유하는 피부 또는 모발 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 약학적 조성물을 제공한다. According to another embodiment of the present invention, there is provided a composition for skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or the like, which contains the compound of Chemical Formula 1 or a pharmaceutically or cosmetically acceptable salt thereof as an active ingredient , Or a pharmaceutical composition for moisturizing the skin.
본 발명의 화합물을 포함하는 조성물은 경구 또는 비경구의 여러 가지 제형일 수 있으나, 바람직하게는 비경구 제제일 수 있다. 제제화할 경우에는 보통 사용하는 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제된다. 경구투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 하나 이상의 화합물에 적어도 하나 이상의 부형제 예를 들면, 전분, 탄산칼슘, 수크로오스(sucrose) 또는 락토오스(lactose), 젤라틴 등을 섞어 조제된다. 또한 단순한 부형제 이외에 스테아린산 마그네슘, 탈크 등과 같은 윤활제들도 사용된다. 경구투여를 위한 액상제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순 희석제인 물, 리퀴드 파라핀 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다. 비경구투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제가 포함된다. 비수성용제, 현탁용제로는 프로필렌글리콜(propylene glycol), 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다.The composition comprising the compound of the present invention may be various oral or parenteral formulations, but may preferably be a parenteral agent. In the case of formulation, a diluent or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, or a surfactant is usually used. Solid formulations for oral administration include tablets, pills, powders, granules, capsules, and the like, which may contain one or more excipients such as starch, calcium carbonate, sucrose or lactose lactose, gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate, talc, and the like are also used. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. Various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included in addition to water and liquid paraffin, which are simple diluents commonly used. have. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solutions, suspensions, and emulsions. Propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like can be used as the non-aqueous solvent and suspension agent.
본 발명은 또한 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 유효성분으로 포함하는 피부 또는 모발 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 피부 외용제의 제형으로 제공할 수 있다.The present invention also relates to a composition for external application for skin or hair for blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing comprising the compound of formula (1) or a pharmaceutically or cosmetically acceptable salt thereof as an active ingredient As shown in FIG.
상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 피부외용제로 사용하는 경우, 추가로 지방 물질, 유기 용매, 용해제, 농축제 및 겔화제, 연화제, 항산화제, 현탁화제, 안정화제, 발포제(foaming agent), 방향제, 계면활성제, 물, 이온형 또는 비이온형 유화제, 충전제, 금속이온봉쇄제 및 킬레이트화제, 보존제, 비타민, 차단제, 습윤화제, 필수 오일, 염료, 안료, 친수성 또는 친유성 활성제, 지질 소낭 또는 피부용 외용제에 통상적으로 사용되는 임의의 다른 성분과 같은 피부 과학 분야에서 통상적으로 사용되는 보조제를 함유할 수 있다. 또한 상기 성분들은 피부 과학 분야에서 일반적으로 사용되는 양으로 도입될 수 있다. When the compound of Chemical Formula 1 or a pharmaceutically or cosmetically acceptable salt thereof is used as an external preparation for skin, it may further contain a fatty substance, an organic solvent, a solubilizing agent, a thickening agent and a gelling agent, a softening agent, an antioxidant, a suspending agent, A foaming agent, a fragrance, a surfactant, water, an ionic or nonionic emulsifier, a filler, a sequestering and chelating agent, a preservative, a vitamin, a barrier, a wetting agent, A lipophilic active agent, a lipid vesicle or any other ingredient conventionally used in external preparations for skin. The components can also be introduced in amounts commonly used in the field of dermatology.
상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염이 피부 외용제 제형으로 제공될 경우, 이에 제한되는 것은 아니나, 연고, 패취, 겔, 크림 또는 분무제와 같은 제형을 가질 수 있다.When the compound of Formula 1, or a pharmaceutically or cosmetically acceptable salt thereof, is provided as an external dermal preparation, it may have a formulation such as, but not limited to, ointments, patches, gels, creams or sprays.
본 발명의 약학적 조성물은 특히 바람직하게 비경구용 제제로 이용될 수 있으며, 예를 들어, 피부외용제는 바세린, 스테아릴알코올 등의 약제학적으로 허용되는 적당한 기제; 폴리소르베이트, 소르비탄 세스퀴올레이트 등의 약제학적으로 허용되는 적당한 계면활성제; 글리세린 등의 약제학적으로 허용되는 적당한 보습제; 약제학적으로 허용되는 적당한 용제; 및 착향제, 착색제, 안정화제, 점성화제 등을 균질하게 혼합하는 통상의 피부외용제 제조방법에 의해서 제조될 수 있다.The pharmaceutical composition of the present invention is particularly preferably used as a parenteral preparation. For example, the external preparation for skin may be a pharmaceutically acceptable base such as vaseline or stearyl alcohol; Suitable pharmaceutically acceptable surfactants such as polysorbate, sorbitan sesquioleate, and the like; A suitable pharmaceutically acceptable humectant such as glycerin; A suitable pharmaceutically acceptable solvent; And a conventional external preparation for skin preparation in which a flavoring agent, a coloring agent, a stabilizer, a tackifier and the like are homogeneously mixed.
또한, 본 발명의 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 의약품으로 사용하는 경우, 추가로 동일 또는 유사한 기능을 나타내는 유효성분을 1종 이상 함유할 수 있다. 예컨대, 공지의 피부 또는 모발 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 성분을 포함할 수 있을 것이다. 추가적인 피부 또는 모발 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 성분을 포함하게 되면 본 발명의 조성물의 피부 또는 모발 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습 효과는 더욱 증진될 수 있을 것이다. 상기 성분 추가 시에는 복합 사용에 따른 피부 안전성, 제형화의 용이성, 유효성분들의 안정성을 고려할 수 있다. When the compound of Formula 1 of the present invention or its pharmaceutically or cosmetically acceptable salt is used as a medicament, it may further contain one or more active ingredients showing the same or similar functions. For example, it may contain known ingredients for skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing ingredients. The skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing effect of the composition of the present invention is further improved when the composition for skin or hair blacking, skin elasticity enhancement, skin wrinkle improvement, . When the above ingredients are added, skin safety, easiness of formulation, and stability of effective ingredients can be considered according to the combined use.
본 발명의 한 구체예에서, 상기 조성물은 당업계에 공지된 피부 탄력 또는 주름 개선 성분으로, 레티노산, TGF, 동물 태반 유래의 단백질, 베툴린산 및 클로렐라 추출물; 당업계에 공지된 보습 성분으로, 페트로라툼 (바세린), 미네랄오일, 실리콘, 중성지방, 필수지방산(예를 들어 감마리놀렌산(달맞이꽃 종자유)), GGF, 아미노산, 프로비타민 B5, 히알루론산, Poly-γ-글루탐산, 리피듀어(Lipidure) PMB, 세라마이드, 콜레스테롤, 지방산; 및 이들의 유도체와 각종 식물 추출물로 구성되는 군으로부터 선택되는 1종 또는 2종 이상의 성분을 추가로 포함할 수 있다. 추가의 성분은 전체 조성물 중량에 대하여 0.0001 중량% 내지 10 중량%로 포함될 수 있으며, 상기 함량 범위는 피부 안전성, 상기 화학식 1의 화합물의 제형화 시의 용이성 등의 요건에 따라 조절될 수 있다.In one embodiment of the invention, the composition is a skin elasticity or wrinkle improving ingredient known in the art and includes retinoic acid, TGF, animal placenta-derived proteins, betulinic acid and chlorella extract; Examples of moisturizing ingredients known in the art include petrolatum, mineral oil, silicone, triglycerides, essential fatty acids such as gamma linolenic acid (evening primrose oil), GGF, amino acids, provitamin B5, hyaluronic acid, γ-glutamic acid, Lipidure PMB, ceramide, cholesterol, fatty acids; And derivatives thereof, and various plant extracts. ≪ Desc / Clms Page number 2 > The additional ingredients may be included in an amount of 0.0001 to 10% by weight based on the total weight of the composition, and the content may be adjusted according to requirements such as skin safety, ease of formulation of the compound of Formula 1, and the like.
본 발명의 약학적 조성물은 유효량의 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 포함할 때 바람직한 피부 또는 모발 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습 효과를 제공할 수 있다. 본 발명에 있어서, '유효량'이라 함은 피부 또는 모발 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습 효과를 충분히 나타낼 수 있는 화합물의 양을 의미한다.The pharmaceutical composition of the present invention provides a desired skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing effect when it contains an effective amount of the compound of Formula 1 or a pharmaceutically or cosmetically acceptable salt thereof . In the present invention, the term "effective amount" means an amount of a compound capable of sufficiently exhibiting skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing effect.
본 발명의 조성물에 포함되는 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염의 유효량은 조성물이 제품화되는 형태, 상기 화합물이 피부에 적용되는 방법 및 피부에 머무르는 시간 등에 따라 달라질 것이다. 예컨대, 상기 조성물이 의약품으로 제품화되는 경우에는 일상적으로 피부에 적용하게 되는 화장품으로 제품화되는 경우에 비해 높은 농도로 상기 화학식 1의 화합물을 포함할 수 있을 것이다. 따라서, 일일 투여량은 상기 화학식 1의 화합물의 양을 기준으로 0.1 내지 100 ㎎/㎏이고, 바람직하게는 30 내지 80 ㎎/㎏이고, 더욱 바람직하게는 50 내지 60 mg/kg이며, 하루 1~6 회 투여될 수 있다. The effective amount of the compound of formula (I) or a pharmaceutically or cosmetically acceptable salt thereof contained in the composition of the present invention will vary depending on the form in which the composition is produced, the manner in which the compound is applied to the skin, and the time on the skin. For example, when the composition is commercialized as a pharmaceutical product, the compound of Formula 1 may be contained at a higher concentration than that of a cosmetic product that is routinely applied to skin. Accordingly, the daily dosage is 0.1 to 100 mg / kg, preferably 30 to 80 mg / kg, more preferably 50 to 60 mg / kg, based on the amount of the compound of formula (1) 6 times a day.
본 발명의 또 다른 실시예에 따르면 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 포함하는 피부 또는 모발 흑화용, 피부 탄력 증진용, 피부 주름 개선용, 또는 피부 보습용 건강식품을 제공한다.According to another embodiment of the present invention, there is provided a composition for treating skin or hair blackening, skin elasticity enhancement, skin wrinkle improving or skin moisturizing health food comprising the compound of formula 1 or a pharmaceutically or cosmetically acceptable salt thereof .
본 명세서에서 '건강식품'이란, 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 음료, 차류, 향신료, 껌, 과자류 등의 식품소재에 첨가하거나, 캡슐화, 분말화, 현탁액 등으로 제조한 식품으로, 이를 섭취할 경우 건강상 특정한 효과를 가져오는 것을 의미하나, 일반 약품과는 달리 식품을 원료로 하여 약품의 장기 복용 시 발생할 수 있는 부작용 등이 없는 장점이 있다. 이와 같이 하여 얻어지는 본 발명의 건강식품은, 일상적으로 섭취하는 것이 가능하기 때문에 피부 또는 모발의 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습에 우수한 효과를 기대할 수 있어 매우 유용하다.In the present specification, the term 'health food' is intended to include a compound of the above formula (1) or a pharmaceutically or cosmetically acceptable salt thereof to a food material such as a beverage, a tea, a spice, a gum or a confectionery, or to encapsulate, , Which means that it has a certain health effect when ingested. However, unlike general medicines, there is an advantage that there is no side effect that may occur when a drug is taken for a long time by using a food as a raw material. Since the health food of the present invention thus obtained can be taken on a daily basis, it can be expected to have excellent effects on blackening of the skin or hair, skin elasticity enhancement, skin wrinkle improvement, or skin moisturization.
상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 식품첨가물로 사용하는 경우, 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 그대로 첨가하거나 다른 식품 또는 식품 성분과 함께 사용될 수 있고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 유효성분의 혼합양은 그의 사용 목적(예방, 건강 또는 치료적 처치)에 따라 적합하게 결정될 수 있다. 일반적으로, 식품 또는 음료의 제조시에 본 발명의 조성물은 원료에 대하여 15 중량부 이하, 바람직하게는 10 중량부 이하의 양으로 첨가된다. 그러나, 건강 및 위생을 목적으로 하거나 또는 건강 조절을 목적으로 하는 장기간의 섭취의 경우에는 상기 양은 상기 범위 이하일 수 있으며, 안전성 면에서 아무런 문제가 없기 때문에 유효성분은 상기 범위 이상의 양으로도 사용될 수 있다. 상기 식품의 종류에는 특별한 제한은 없다. 상기 물질을 첨가할 수 있는 식품의 예로는 육류, 소세지, 빵, 초콜릿, 캔디류, 스넥류, 과자류, 피자, 라면, 기타 면류, 껌류, 아이스크림류를 포함한 낙농제품, 각종 스프, 음료수, 차, 드링크제, 알코올 음료 및 비타민 복합제 등이 있으며, 통상적인 의미에서의 건강식품을 모두 포함한다. 본 발명의 건강음료 조성물은 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상술한 천연 탄수화물은 포도당, 과당과 같은 모노사카라이드, 말토스, 수크로오스와 같은 디사카라이드, 및 덱스트린, 사이클로덱스트린과 같은 폴리사카라이드, 자일리톨, 소르비톨, 에리트리톨 등의 당알코올이다. 감미제로서는 타우마틴, 스테비아 추출물과 같은 천연 감미제나, 사카린, 아스파르탐과 같은 합성 감미제 등을 사용할 수 있다. 상기 천연 탄수화물의 비율은 본 발명의 조성물 100 mL 당 일반적으로 약 0.01 ∼ 0.04 g, 바람직하게는 약 0.02 ∼ 0.03 g 이다. 상기 외에 본 발명의 건강식품은 여러 가지 영양제, 비타민, 전해질, 풍미제, 착색제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산 음료에 사용되는 탄산화제 등을 함유할 수 있다. 그 밖에 본 발명의 건강식품은 천연 과일주스, 과일주스 음료 및 야채 음료의 제조를 위한 과육을 함유할 수 있다. 이러한 성분은 독립적으로 또는 혼합하여 사용할 수 있다. 이러한 첨가제의 비율은 크게 중요하진 않지만 본 발명의 조성물 100 중량부당 0.01 ~ 0.1 중량부의 범위에서 선택되는 것이 일반적이다.When the compound of Chemical Formula 1, or a pharmaceutically or cosmetically acceptable salt thereof, is used as a food additive, the compound of Chemical Formula 1 or a pharmaceutically or cosmetically acceptable salt thereof may be directly added, Can be used together, and can be suitably used according to a conventional method. The amount of the active ingredient to be mixed can be suitably determined according to its intended use (prevention, health or therapeutic treatment). Generally, the composition of the present invention is added in an amount of not more than 15 parts by weight, preferably not more than 10 parts by weight, based on the raw material, when the food or beverage is produced. However, in the case of long-term consumption intended for health and hygiene purposes or for health control purposes, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount exceeding the above range . There is no particular limitation on the kind of the food. Examples of the food to which the above substance can be added include dairy products including meat, sausage, bread, chocolate, candy, snack, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, Alcoholic beverages, and vitamin complexes, all of which include health foods in a conventional sense. The health beverage composition of the present invention may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages. The above-mentioned natural carbohydrates are sugar alcohols such as monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and xylitol, sorbitol and erythritol. Examples of sweeteners include natural sweeteners such as tau martin and stevia extract, synthetic sweeteners such as saccharin and aspartame, and the like. The ratio of the natural carbohydrate is generally about 0.01 to 0.04 g, preferably about 0.02 to 0.03 g per 100 mL of the composition of the present invention. In addition to the above, the health food of the present invention may contain various nutrients, vitamins, electrolytes, flavors, colorants, pectic acids and salts thereof, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, , A carbonating agent used in carbonated drinks, and the like. In addition, the health food of the present invention may contain flesh for the production of natural fruit juice, fruit juice drink and vegetable drink. These components may be used independently or in combination. The proportion of such additives is not critical, but is generally selected in the range of 0.01 to 0.1 parts by weight per 100 parts by weight of the composition of the present invention.
이에 제한되는 것은 아니나, 본 발명의 한 구체예에서, 상기 조성물은 상기 화학식 1의 화합물 또는 이의 약학적 또는 화장학적으로 허용 가능한 염을 전체 조성물 중량에 대하여 0.00001 중량% 내지 10 중량%로 포함할 수 있다.In one embodiment of the present invention, but not limited thereto, the composition may comprise 0.00001% to 10% by weight of the compound of Formula 1 or a pharmaceutically or cosmetically acceptable salt thereof, based on the total composition weight have.
본 발명의 아이소스테비올을 함유하는 조성물은 피부 또는 모발 흑화, 피부 탄력 증진, 피부 주름 개선, 또는 피부 보습에 우수한 효과를 나타낸다. The composition containing isostearvol of the present invention shows excellent effects on skin or hair blackening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturization.
본 발명의 아이소스테비올을 함유하는 조성물은 피부에 안전하면서도 피부 상태 개선 효과가 우수한 화장품 원료, 약학 성분 또는 건강식품 원료로 이용될 수 있다.The composition containing isostearic acid of the present invention can be used as a raw material for cosmetics, a pharmaceutical ingredient, or a health food, which is safe for skin and has excellent skin condition improving effect.
이하, 본 발명을 보다 구체적으로 설명하기 위하여 하기 실시예 등을 들어 설명한다. 그러나, 본 발명에 따른 실시예들은 여러 가지 다른 형태로 변형될 수 있으며 본 발명의 범위가 아래에서 상술하는 실시예들에 한정되는 것으로 해석되어서는 안 된다. 본 발명의 실시예들은 본 발명의 구체적 이해를 돕기 위해 예시적으로 제공되는 것이다.Hereinafter, the present invention will be described in more detail with reference to the following examples. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the embodiments described below. The embodiments of the present invention are provided by way of example to facilitate a specific understanding of the present invention.
참조예Reference Example 1: One: 아이소스테비올Isosteviol (( IsosteviolIsosteviol ) 물질 정보) Material information
[화학식 1][Chemical Formula 1]
물질명 : Isosteviol; NSC 231875; (4α,8β,13β)-13--Methyl-16-oxo-17-norkauran-18-oic acidMaterial name: Isosteviol; NSC 231875; (4α, 8β, 13β) -13-Methyl-16-oxo-17-norchauran-18-oic acid
CAS No. : 27975-19-5CAS No. : 27975-19-5
분자식 : C20H30O3 Molecular formula: C 20 H 30 O 3
분자량 : 318.45 Molecular weight: 318.45
구입처 : ShangHai YuanYe Biotechnology Co., Ltd.Where to buy: ShangHai YuanYe Biotechnology Co., Ltd.
실험예Experimental Example 1: 인체 유래의 섬유아세포에서 제1형 콜라겐(type I collagen) 합성 촉진 효과 1: promoting the synthesis of type I collagen in human fibroblasts
화학식 1의 화합물을 인간 유래 섬유아세포의 배양액에 첨가하여 세포수준에서 제1형 콜라겐 합성 촉진 효과를 확인하였다. 합성된 콜라겐의 측정은 PICP EIA kit(Procollagen Type I C-Peptide Enzyme Immuno Assay KIT)를 이용하여 정량하였다. 콜라겐 합성량을 측정하기 위해 화학식 1의 화합물을 섬유아세포의 배양배지(DMEM 배지)에 첨가하여 48 시간 배양한 후 배양액을 취하여 PICP EIA 키트로 각 농도에서 제1형 콜라겐 합성 정도를 분광광도계를 이용하여 450 nm에서 측정하였다.The compound of Chemical Formula 1 was added to the culture medium of human-derived fibroblasts to confirm the promoting effect of type I collagen synthesis at the cellular level. The synthesized collagen was quantitated using a PICP EIA kit (Procollagen Type I C-Peptide Enzyme Immuno Assay Kit). To measure the amount of collagen synthesis, the compound of formula (1) was added to a culture medium of fibroblasts (DMEM medium) and cultured for 48 hours. The culture broth was taken and the degree of type 1 collagen synthesis was measured by a PICP EIA kit using a spectrophotometer And measured at 450 nm.
효과의 비교를 위하여 시료를 처리하지 않은 섬유아세포의 배양배지(음성대조군)와 비타민 C(양성대조군)를 최종농도 52.85 ㎍/ml가 되도록 첨가한 시료에 대하여 동일한 방법으로 콜라겐 합성 정도를 측정하였다. 콜라겐 생성 증가율은 대조군에 대한 상대적인 콜라겐 생성량의 비율로 계산하고 결과를 하기 표 1에 나타내었다.For the comparison of the effects, the degree of collagen synthesis was measured in the same manner for the samples in which the culture medium of the untreated fibroblasts (negative control) and vitamin C (positive control) were added to a final concentration of 52.85 / / ml. The increase rate of collagen production was calculated as a ratio of relative collagen production to the control group, and the results are shown in Table 1 below.
화학식 1의 화합물의 콜라겐 합성 촉진 효과 (반복수 =4)Promoting collagen synthesis of the compound of formula (1) (number of repeats = 4)
상기 표 1의 결과에서 볼 수 있듯이, 화학식 1의 화합물을 처리한 경우, 농도 의존적으로 콜라겐 합성량이 증가되었고, 일반적으로 콜라겐 합성을 유도하는 것으로 잘 알려진 비타민C를 적용한 경우보다 더 낮은 농도에서 유사한 콜라겐 합성 효과를 나타내었다.As can be seen from the results of Table 1, when the compound of Chemical Formula 1 was treated, the amount of collagen synthesis was increased in a concentration-dependent manner. In the case of vitamin C, which is generally known to induce collagen synthesis, Synthesis effect.
실험예 2: 엘라스테이즈 활성 저해 효과Experimental Example 2: Elastase activity inhibitory effect
엘라스틴(Elastin)을 분해하는 효소인 엘라스테이즈(Elastase)의 활성 저해 효과를 다음과 같이 확인하였다.The activity inhibitory effect of Elastase, an enzyme that degrades elastin, was confirmed as follows.
엘라스테이즈(Elastase)는 사람의 백혈구 세포로부터 유래한 엘라스테이즈를 사용하였고, 엘라스테이즈의 기질로 합성 기질인 MeOSuc-Ala-Ala-Pro-Val-pNA를 사용하였다. 완충용액은 100mM의 Tris(pH 7.5) 용액을 사용하였다. 엘라스테이즈는 완충용액을 이용하여 최종적으로 0.2 mU을 사용하였다. 또한 엘라스테이즈의 합성 기질은 DMSO를 이용하여 100mM 용액을 만든 후 최종 농도가 0.5mM이 되도록 완충용액을 이용하여 희석하였다. 이 때, 양성 대조군은 엘라스테이즈 저해 물질로 알려진 퀘르세틴(Quercetin)을 10ppm 농도로 넣은 것으로 설정하였다. 엘라스테이즈 저해 후보는 최종농도가 10, 20ppm이 되도록 첨가하였다. 반응은 96-웰 플레이트에서 진행하였으며, 상온에서 20분간 반응시켰다. 분광 광도계를 이용하여 1분 간격으로 405 nm에서 흡광도를 측정하여, 시간 대비 흡광도의 기울기를 구하여 효소의 활성도로 정하였다. 엘라스테이즈 저해율은 다음과 같이 계산하였다.Elastase used Elastase from human leukocyte cells and MeOSuc-Ala-Ala-Pro-Val-pNA as synthetic substrate for Elastase. The buffer solution used was 100 mM Tris (pH 7.5) solution. Finally, 0.2 mU was used for the ELASTASES using a buffer solution. In addition, the synthetic substrate of Elastase was diluted with buffer solution to make a final concentration of 0.5 mM by making a 100 mM solution using DMSO. At this time, the positive control group was set to contain 10 ppm of quercetin, which is known as an ELASTIC inhibitor. Ella stase inhibition candidates were added to give a final concentration of 10, 20 ppm. The reaction was carried out in a 96-well plate and allowed to react at room temperature for 20 minutes. Absorbance was measured at 405 nm using a spectrophotometer at intervals of 1 minute, and the slope of the absorbance versus time was determined as the activity of the enzyme. Ella stasis inhibition rates were calculated as follows.
화학식 1의 화합물의 엘라스테이즈 활성 저해 효과 (반복수 =3)Elastase activity inhibitory effect (number of repeats = 3) of the compound of formula (1)
상기 표 2의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 10 ppm의 농도에서 엘라스테이즈 활성 저해 효과가 양성대조군인 퀘르세틴에 상응하는 정도로 높게 나타났으며, 20 ppm의 농도에서 퀘르세틴보다 우수한 엘라스테이즈 활성 저해 효과가 나타나, 화학식 1의 화합물은 엘라스테이즈 활성 저해효과가 우수한 것을 확인하였다. 따라서, 화학식 1의 화합물은 피부 탄력 및 주름 개선을 위한 용도로 효과적으로 사용될 수 있음을 알 수 있었다.As can be seen from the results in Table 2, the compound of Chemical Formula 1 showed a high level of inhibition of the enzyme activity at a concentration of 10 ppm, corresponding to that of the positive control, quercetin, and at a concentration of 20 ppm, And the compound of formula (1) was found to be excellent in the effect of inhibiting the enzyme activity. Thus, it has been found that the compound of formula (I) can be effectively used for skin elasticity and wrinkle improvement.
실험예 3: 당화 저해(anti-glycation) 효과Experimental Example 3: Anti-glycation effect
당화 저해(anti-glycation) 효능을 확인하기 위하여, L-arginine과 포도당을 이용하여 당화 저해 활성을 측정하였다. In order to confirm the anti-glycation effect, the saccharification inhibitory activity was measured using L-arginine and glucose.
먼저, 1M 인산 완충용액(pH 7.4)을 이용하여 1M L-아르기닌(arginine), 1M 포도당을 녹여 준비하고 1M 인산 완충용액을 이용하여 시료를 50, 100ppm이 되도록 희석해서 준비하였다. 1M L-아르기닌과 1M 인산 완충용액을 1대 4의 비율로 섞은 다음 96-웰 플레이트에 80 μl씩 분주하였다. 여기에 각각 50, 100ppm으로 희석한 시료와 양성대조군으로 사용될 0.01M 아미노구아니딘(aminoguanidin)을 100 μl씩 첨가하였다. 이 시료들을 잘 섞어준 다음, 마지막으로 포도당의 최종 농도가 0.1M이 되도록 1M 인산 완충용액으로 희석한 포도당을 넣은 후, 70℃에서 4시간 동안 반응 시켰다. 96-웰 플레이트를 분광 광도계를 이용하여 420 nm에서 흡광도를 측정하여 당화 정도를 측정하였다. First, 1 M L-arginine and 1 M glucose were prepared by dissolving 1 M phosphoric acid buffer (pH 7.4) and diluted to 50 ppm and 100 ppm using 1M phosphate buffer solution. 1M L-arginine and 1M phosphate buffer solution were mixed at a ratio of 1: 4, and then 80 [mu] l each was added to a 96-well plate. To each sample, 100 μl of 0.01 M aminoguanidine to be used as a positive control and a sample diluted to 50 ppm and 100 ppm, respectively, were added. These samples were mixed well and finally glucose diluted with 1M phosphate buffer solution was added to the final concentration of glucose to 0.1 M and reacted at 70 ° C for 4 hours. The degree of saccharification was measured by measuring the absorbance of the 96-well plate at 420 nm using a spectrophotometer.
하기 식의 Glycation 실험군은 1M L-아르기닌과 1M 포도당을 넣어 당화를 유발시킨 실험군이며, 시료 자체의 흡광도를 측정하기 위해서 포도당을 넣지 않고 1M L-아르기닌과 시료만을 넣어 420 nm에서 흡광도를 측정하였다. 당화 저해 활성은 다음과 같은 식으로 구할 수 있다.Glycation group of the following formula was an experimental group in which 1M L-arginine and 1M glucose were added to induce glycation. Absorbance was measured at 420 nm by adding 1M L-arginine and sample alone without glucose to measure the absorbance of the sample itself. The saccharide inhibitory activity can be obtained by the following formula.
화학식 1의 화합물의 항당화 효과The antagonism effect of the compound of formula (1)
상기 표 3의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 항당화 물질로 알려진 아미노구아니딘과 비교할 때, 항당화 효과가 더욱 뛰어남을 알 수 있었다. 즉, 화학식 1의 화합물은 우수한 항당화 효과를 나타내어, 피부 주름 및 탄력 개선에 있어서, 항당화 효과가 보조적인 역할로 작용하여 상승효과를 기대할 수 있다.As can be seen from the results shown in Table 3, the compound of Chemical Formula 1 was found to be more excellent in antagonism effect as compared with aminoguanidine known as an antagonist. That is, the compound of the formula (1) exhibits an excellent antihyperglycosylating effect, and antiherating effect plays an auxiliary role in improving the wrinkles and elasticity of the skin, and a synergistic effect can be expected.
실험예 4: 흑화 효과-멜라닌 총량 증가 효과Experimental Example 4: Blackening effect - Increasing effect of total amount of melanin
화학식 1의 화합물을 쥐의 멜라노마 세포(B-16 mouse melanoma cell)의 배양액에 첨가하여 세포 수준에서의 멜라닌 총량을 측정함으로써 흑화 효과를 확인하였다(Lotan R., Lotan D. Cancer Res. 40:3345-3350, 1980). 실험 전 쥐의 멜라노마 세포에 대하여 독성을 평가하여 독성이 없는 농도를 선정하여 흑화 평가를 수행하였다. The compound of the formula (1) was added to the culture solution of mouse B-16 mouse melanoma cells to determine the blackening effect by measuring the total amount of melanin at the cellular level (Lotan R., Lotan D. Cancer Res . 40: 3345-3350, 1980). To evaluate the toxicity of melanoma cells in rats before the experiment and to determine the concentration without toxicity, blackening evaluation was performed.
화학식 1의 화합물을 배양액에 최종 농도가 1 ppm, 10 ppm이 되도록 하였으며, 대조군인 포스콜린(Forskolin)은 10 ppm이 되도록 배지에 첨가하여 각각 B-16 멜라노마 세포에 처리하여 3일간 배양하였다. The compound of formula (1) was added to the culture medium to a final concentration of 1 ppm and 10 ppm, and the control group, Forskolin, was added to the medium so as to be treated with B-16 melanoma cells and cultured for 3 days.
이후, 세포들을 트립신(trypsin) 처리하여 배양용기로부터 떼어내 원심분리한 후, 멜라닌을 추출하였다. 떼어낸 세포는 수산화나트륨 용액(1N 농도) 1 ml를 가하여 10분간 끓여 멜라닌을 녹이고 분광 광도계를 이용하여, 400 nm에서 흡광도를 측정하여 생성된 멜라닌의 양을 측정하였다. Cells were then trypsinized, detached from the culture, centrifuged, and then melanin was extracted. The removed cells were incubated with 1 ml of sodium hydroxide solution (1N concentration), boiled for 10 minutes to dissolve melanin, and the absorbance was measured at 400 nm using a spectrophotometer to measure the amount of melanin produced.
상기 멜라닌 양은 단위 세포수당(1×106 cell)의 흡광도로 나타내는 방법으로 측정하였으며, 대조군에 대한 상대적인 멜라닌 총량을 증가율(%)로 계산하고 결과를 하기 표 4에 정리하였다.The amount of melanin was measured by the absorbance of 1 × 10 6 cells per unit cell, and the total amount of melanin relative to the control group was calculated as an increase rate (%). The results are summarized in Table 4 below.
농도에 따른 세포수준에서의 멜라닌 총량의 증가 효과 Increased effect of total melanin level at cell level according to concentration
(abs)Melanin production
(abs)
상기 표 4의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 양성대조군인 포스콜린과 비교했을 때, 10 ppm에서도 상당히 우수한 멜라닌 총량 증가 효과를 나타내어, 피부 또는 모발의 흑화 용도로 사용할 수 있음을 알 수 있었다.As can be seen from the results in Table 4, the compound of Chemical Formula 1 shows a remarkably superior total amount of melanin even at 10 ppm as compared with the positive control phosholin, and can be used for blackening of skin or hair there was.
Claims (7)
[화학식 1]
[Chemical Formula 1]
[화학식 1]
[Chemical Formula 1]
[화학식 1]
[Chemical Formula 1]
[화학식 1]
[Chemical Formula 1]
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| KR20210074770A (en) * | 2019-12-12 | 2021-06-22 | (주)아모레퍼시픽 | Composition for inducing alteration of surrounding environment of a aged cell |
| CN113476321A (en) * | 2021-07-07 | 2021-10-08 | 珠海沅芷健康科技有限公司 | Application of isosteviol in preparing cosmetic preparation for whitening skin and resisting melanin generation |
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| KR20210074770A (en) * | 2019-12-12 | 2021-06-22 | (주)아모레퍼시픽 | Composition for inducing alteration of surrounding environment of a aged cell |
| CN113476321A (en) * | 2021-07-07 | 2021-10-08 | 珠海沅芷健康科技有限公司 | Application of isosteviol in preparing cosmetic preparation for whitening skin and resisting melanin generation |
| CN113476321B (en) * | 2021-07-07 | 2023-09-22 | 珠海沅芷健康科技有限公司 | Application of isosteviol in preparing cosmetic preparation for whitening skin and resisting melanin generation |
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