KR102503108B1 - Composition for improving skin conditions comprising Timosaponin A-Ⅲ - Google Patents
Composition for improving skin conditions comprising Timosaponin A-Ⅲ Download PDFInfo
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- KR102503108B1 KR102503108B1 KR1020150191263A KR20150191263A KR102503108B1 KR 102503108 B1 KR102503108 B1 KR 102503108B1 KR 1020150191263 A KR1020150191263 A KR 1020150191263A KR 20150191263 A KR20150191263 A KR 20150191263A KR 102503108 B1 KR102503108 B1 KR 102503108B1
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- 239000000203 mixture Substances 0.000 title claims abstract description 55
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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
- A61K8/60—Sugars; Derivatives thereof
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K8/00—Cosmetics or similar toiletry preparations
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- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
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- 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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Abstract
본 발명은 피부에서 항당화, 미백, 주름 개선, 탄력 개선 또는 피부 보습에 우수한 효과를 가지는 화장료 조성물, 약학적 조성물 및 건강식품에 관한 것이다. 본 발명의 조성물은 피부 미백, 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 having excellent effects on antiglycation, whitening, wrinkle improvement, elasticity improvement, or skin moisturizing in the skin. The composition of the present invention exhibits excellent effects on skin whitening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing. The compound of 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 that is safe for the skin and has excellent skin condition improvement effects.
Description
본 발명은 피부 상태의 개선에 우수한 효과를 가지는 조성물에 관한 것으로서, 보다 구체적으로 피부의 항당화, 미백, 주름 개선, 탄력 개선, 또는 피부 보습에 우수한 효과를 가지는 화장료 조성물, 약학적 조성물 및 건강식품에 관한 것이다.The present invention relates to a composition having an excellent effect on improving skin conditions, and more specifically, a cosmetic composition, a pharmaceutical composition, and a health food having excellent effects on skin antiglycation, whitening, wrinkle improvement, elasticity improvement, or skin moisturizing. It is about.
희고 고운 피부를 갖고자 하는 것은 일반적인 소망이다. 피부의 색깔 또는 밝기는 사람의 피부 내 멜라닌(Melanin)의 농도와 분포에 따라 유전적으로 결정되나, 태양 자외선, 피로 또는 스트레스 등의 환경적 또는 생리적 조건에 의해서도 영향을 받는다. 멜라닌은 아미노산의 일종인 티로신(Tyrosine)에 티로시나제(Tyrosinase)라는 효소가 촉매로 작용하여 도파(DOPA) 및 도파퀴논(Dopaquinone)으로 순차적으로 바뀐 후, 비효소적인 산화반응을 거쳐 만들어진다. 이와 같이 멜라닌이 만들어지는 경로는 알려져 있으나, 멜라닌 합성을 유도하는 메커니즘에서 티로시나제가 촉발되는 원인이 무엇인지에 대해서는 아직도 자세히 밝혀지지 않고 있다. It is a common desire to have white and fair skin. Skin color or brightness is genetically determined according to the concentration and distribution of melanin in human skin, but is also influenced by environmental or physiological conditions such as solar ultraviolet rays, fatigue or stress. Melanin is produced through a non-enzymatic oxidation reaction after sequentially converting tyrosine, a kind of amino acid, into DOPA and dopaquinone by an enzyme called tyrosinase acting as a catalyst. Although the pathway by which melanin is produced is known, the cause of triggering tyrosinase in the mechanism inducing melanin synthesis has not yet been clarified in detail.
한편, 일반적으로 알려진 미백 성분으로 코지산(Kojic acid) 또는 알부틴(Arbutin) 등과 같은 티로시나제 효소활성을 억제하는 물질이 있으며, 또 하이드로퀴논(Hydroquinone), 비타민 C(L-Ascorbic acid) 또는 이들의 유도체와 각종 식물 추출물이 미백 효능이 있다고 알려져 있다. 이들은 멜라닌 색소의 합성을 저해함으로써 피부 톤을 밝게 하여 피부 미백을 실현할 수 있을 뿐만 아니라, 자외선, 호르몬 또는 유전에 기인한 기미나 주근깨 등의 피부 과색소 침착증의 개선이 가능하다. 그러나 피부 적용 시, 자극과 발적 등의 안전성의 문제로 사용량의 제한이 있거나, 효과가 미미하여 실질적인 효과를 기대할 수 없는 문제점이 있다.On the other hand, commonly known whitening ingredients include substances that inhibit tyrosinase enzyme activity, such as Kojic acid or arbutin, and also hydroquinone, vitamin C (L-Ascorbic acid) or derivatives thereof. and various plant extracts are known to have whitening effects. By inhibiting the synthesis of melanin pigment, they can realize skin whitening by brightening the skin tone, and can improve skin hyperpigmentation such as spots and freckles caused by ultraviolet rays, hormones, or heredity. However, when applied to the skin, there is a problem in that the amount of use is limited due to safety problems such as irritation and redness, or a practical effect cannot be expected because the effect is insignificant.
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 matrix protein produced by fibroblasts of the skin and is present in the extracellular matrix. Its important functions include mechanical robustness of the skin, resistance and cohesiveness of connective tissue, support of cell adhesion, cell division and differentiation. (in the growth of organisms or wound healing), etc. are known. Such collagen is reduced by age and photoaging caused by ultraviolet irradiation, and collagen reduction is promoted by the activity of collagenase enzyme that decomposes collagen. It is known that it is 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 fibers form cross-linked bonds with collagen and are an important skin component for wrinkle formation involved in skin elasticity. Deficiency and aggregation of elastin fibers and marked increase in the activity of elastase, an elastin degrading enzyme, have been found to be one of the causes of skin wrinkles. Elastase is the only enzyme capable of decomposing elastin, and inhibition of it is known to fundamentally reduce skin wrinkle improvement.
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 matrix proteins that play an important role in retaining moisture in the dermal layer, and these matrix proteins adsorb moisture and increase the moisture retention within the structure they form so that the skin can maintain an appropriate moisture state. It is known to be involved in maintaining skin elasticity.
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, elastic fibers generated from fibroblasts of the skin form cross-linked bonds with collagen and are an important skin component for wrinkle formation involved in skin elasticity. Deficiency and decomposition of elastic fibers have been found to be one of the main causes of wrinkle formation and deterioration of skin elasticity.
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.Currently, retinoids, adenosine, animal placenta-derived proteins, chlorella extracts, and the like are known as wrinkle-improving cosmetics. Retinol, the most well-known, is a substance that promotes collagen synthesis and inhibits the elastase enzyme, but is unstable and has limitations in usage due to safety issues such as irritation and redness when applied to the skin. It is known that it is difficult to expect wrinkle improvement effects.
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 with a protein or fat that occurs without the involvement of enzymes. Glycation occurs through a series of complex chemical reactions known as Amadori-rearrangements and Maillard-reactions, resulting in 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 glycosylation process of protein occurs slowly because enzyme action is not involved, and as a result, it has more effect on proteins with a long half-life such as collagen. As a result of the analysis of advanced glycation end products, it was shown that as the age increases, glycated collagen accumulates. By preventing collagen from forming its proper structure, it loses skin elasticity and promotes wrinkle formation (Dyer, DG et al. , The Journal of Clinical Investigation, 9, p. 2463, 1993).
또한 당화로 인해 생성된 최종당화산물은 갈색 빛을 띠는 물질로써 피부 노화가 진행됨에 따라 진피층 상부에 쌓이는 것으로 알려져 있다. 피부 노화가 진행되면서 점차 얼굴빛이 노랗게 변하는 원인 물질로 생각되고 있으며, 특정 최종당화산물이 쌓일수록 피부에서 반사되는 반사 빛이 줄어든다고 알려져 있다. 피부 속 멜라닌 색소의 양은 피부 노화와 관계가 약한 반면, 피부 진피층에 쌓이는 최종당화산물은 피부 노화가 진행됨에 따라 점차 그 양이 늘어나게 되고 얼굴빛을 칙칙하게 만들 수 있다(Hiroshi, O. et al., Skin Research and Technology, 15, p. 496, 2009).In addition, the final glycation product produced by glycation is a brownish substance and is known to accumulate in the upper dermal layer as skin aging progresses. It is thought to be a causative substance that gradually turns yellow as skin aging progresses, and it is known that as specific final saccharification products accumulate, reflected light from the skin decreases. While the amount of melanin pigment in the skin has a weak relationship with skin aging, the amount of advanced glycation end products accumulated in the dermal layer of the skin gradually increases as skin aging progresses and can make the complexion dull (Hiroshi, O. et al ., Skin Research and Technology, 15, p. 496, 2009).
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 as substances that inhibit glycation, but these substances have limitations in usage due to safety issues on the skin, or are ineffective due to insignificant effects. There are problems that cannot be expected.
따라서, 생체에 안전하고, 유효성분이 피부에 안전하고 안정성이 높으며, 무엇보다도 피부에서 항당화, 미백, 주름 개선 또는 탄력 개선 효과가 있다고 기존에 알려진 물질보다 효과가 우수한 항당화, 미백, 주름 개선 또는 탄력 개선 성분의 개발이 절실히 요망되고 있다.Therefore, it is safe for the body, active ingredients are safe and stable for the skin, and above all, antiglycation, whitening, anti-wrinkle or Development of an elasticity improving component is desperately desired.
따라서 본 발명이 해결하고자 하는 과제는 위와 같은 문제점을 해결하고, 부작용이 적고 인체에 안전하면서도 피부의 항당화, 미백, 주름 개선 또는 탄력 개선 효과가 우수한 새로운 활성 성분, 즉, 활성 성분의 이러한 유용한 용도를 제공하는 것이다.Therefore, the problem to be solved by the present invention is to solve the above problems, and to solve the above problems, and while being safe to the human body, a new active ingredient that is excellent in antiglycation, whitening, wrinkle improvement or elasticity improvement effect of skin, that is, this useful use of the active ingredient is to provide
다시 말해, 본 발명이 해결하고자 하는 과제는 상기 효능이 우수한 활성 성분을 유효성분으로 포함하는 조성물을 제공하는 것이다.In other words, the 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 티모사포닌 에이-쓰리(Timosaponin A-Ⅲ)를 유효성분으로 포함하는 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용 조성물, 바람직하게는 화장료 조성물, 약학적 조성물 또는 건강식품을 제공한다. In order to solve the above problems, the present invention is a composition for skin whitening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing comprising Timosaponin A-III as an active ingredient, preferably a cosmetic. A composition, pharmaceutical composition or health food is provided.
즉, 본 발명은 티모사포닌 에이-쓰리의 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용이라는 새로운 용도를 제공한다.That is, the present invention provides new uses of thymosaponin A-3 for skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing.
본 발명의 발명자들은 티모사포닌 에이-쓰리가 피부의 콜라겐 생성을 촉진하고, 엘라스테이즈의 활성을 저해함으로써 피부의 주름 및 탄력 개선 효과가 있다는 사실을 발견하고 본 발명을 완성하게 되었다. 또한, 상기 티모사포닌 에이-쓰리는 멜라닌의 총량을 감소시켜 피부 미백 효과를 나타내는 것을 확인하였다. 또한, 상기 티모사포닌 에이-쓰리는 항당화 효과를 나타내어, 피부 미백, 피부 주름 및 피부 탄력 개선에 보조적인 역할로 작용하여 상승효과를 나타낼 수 있다.The inventors of the present invention found that thymosaponin A-3 promotes skin collagen production and inhibits the activity of elastase, thereby improving skin wrinkles and elasticity, and completed the present invention. In addition, it was confirmed that the thymosaponin A-3 exhibits a skin whitening effect by reducing the total amount of melanin. In addition, the thymosaponin A-3 exhibits an anti-glycation effect, so it can act as an auxiliary role in improving skin whitening, skin wrinkles, and skin elasticity, resulting in a synergistic effect.
본 발명에 있어서, '미백 효과'라 함은 피부 톤을 밝게 할 뿐만 아니라, 자외선, 호르몬 또는 유전에 기인한 기미나 주근깨 등의 피부 과색소 침착을 개선하는 것을 말한다. 이러한 미백 효과는 예를 들어, 멜라닌 색소 총량을 감소시킴으로써 달성될 수 있으나, 본 발명은 이러한 기전에 의해 한정되는 것은 아니다.In the present invention, the 'whitening effect' refers to not only brightening the skin tone, but also improving skin hyperpigmentation such as spots or freckles caused by ultraviolet rays, hormones, or heredity. This whitening effect can be achieved, for example, by reducing the total amount of melanin pigment, but the present 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, 'improvement of elasticity or skin elasticity' means alleviating the degree of sagging or sagging of the skin. In addition, the elasticity means maintaining the elasticity of the skin in a state in which 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, 'wrinkle improvement' refers to preventing, suppressing, or inhibiting the formation of wrinkles on the skin, or alleviating wrinkles that have already been created.
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, 'moisturizing or skin moisturizing' means to increase the feeling of moisture in the skin and to maintain a moist state. The skin moisturizing effect can help improve wrinkles and increase elasticity of the 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 억제함으로써 피부 미백에 도움을 줄 수 있다. 따라서, 본 발명에 있어서 항당화 효과는 피부 탄력 증진 및 주름 개선뿐만 아니라, 피부 미백에 시너지 효과를 발생시킬 수 있다.In the present invention, the 'anti-glycation' effect refers to preventing collagen from being glycated in the extracellular matrix of the dermal layer, enhancing skin elasticity and preventing wrinkles. In addition, the anti-glycation effect can help skin whitening by suppressing the production of advanced glycation end products accumulated in the upper dermal layer according to skin aging. Therefore, in the present invention, the antiglycation effect can generate a synergistic effect on skin whitening as well as skin elasticity enhancement and wrinkle improvement.
본 발명은 상기와 같은 문제점들을 해결하고, 본 발명의 목적을 달성하기 위하여 하기 화학식 1로 대표되는 화합물을 포함하는 조성물을 제공한다. The present invention provides a composition containing a compound represented by Formula 1 to solve the above problems and achieve the object of the present invention.
[화학식 1][Formula 1]
상기 화학식 1로 대표되는 화합물은 분자식 C39H64O13, 분자량 740.92를 가지며, 티모사포닌 에이-쓰리(Timosaponin A-Ⅲ)로 명명된다.The compound represented by Formula 1 has a molecular formula of C 39 H 64 O 13 , a molecular weight of 740.92, and is named Timosaponin A-III.
본 발명은 상기 티모사포닌 에이-쓰리의 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 thymosaponin A-3, and it may be chemically synthesized by a known method in the field to which the present invention belongs, or a commercially available material may be used.
본 발명에 따른 화장료 조성물, 약학적 조성물 및 건강식품에 있어, 상기 티모사포닌 에이-쓰리의 함량은 화장료 조성물, 약학적 조성물 및 건강식품 전체 중량 대비 0.00001 내지 10 중량%인 것이 바람직하다.In the cosmetic composition, pharmaceutical composition and health food according to the present invention, the content of thymosaponin A-3 is preferably 0.00001 to 10% by weight based on the total weight of the cosmetic composition, pharmaceutical composition and health food.
본 발명의 티모사포닌 에이-쓰리는 수화물, 에탄올화물 등의 형태를 포함하는 용매화된 형태뿐만 아니라 비-용매화된(unsolvated) 형태로 존재할 수도 있다. 본 발명의 티모사포닌 에이-쓰리는 결정형 또는 무정형 형태로 존재할 수 있으며, 이러한 모든 물리적 형태는 본 발명의 범위에 포함된다.The thymosaponin A-3 of the present invention may exist in unsolvated forms as well as solvated forms including hydrates, ethanolates and the like. The thymosaponin A-3 of the present invention may exist in crystalline or amorphous form, and all such physical forms are included in the scope of the present invention.
본 발명에 따른 피부 미백용, 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 whitening, enhancing skin elasticity, improving skin wrinkles, or moisturizing the skin according to the present invention is a solution, external ointment, cream, foam, nutrient lotion, softening lotion, pack, softening water, emulsion, makeup base, essence, soap , liquid cleansers, bath salts, sun screen creams, sun oils, suspensions, emulsions, pastes, gels, lotions, powders, soaps, surfactant-containing cleansers, oils, powder foundations, emulsion foundations, wax foundations, patches and sprays It can be prepared in a formulation selected from the group consisting of, but is not limited thereto.
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 include one or more cosmetically acceptable carriers formulated in general skin cosmetics, and as typical ingredients, for example, oil, water, surfactants, moisturizers, lower alcohols, A thickener, a chelating agent, a colorant, a preservative, a flavoring agent, and the like may be suitably blended, but are 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.Cosmetically acceptable carriers included in the cosmetic composition of the present invention vary depending on the formulation. When the formulation of the present invention is an ointment, paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide or 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 spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder, or a mixture thereof may be used as a carrier component, and especially in the case of a spray, chloro 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 emulsion, a solvent, solubilizing agent, or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl benzoate, propylene glycol, 1,3 -There is butyl glycol oil, in particular cottonseed oil, peanut oil, corn germ oil, olive oil, castor oil and sesame oil, glycerol aliphatic ester, polyethylene glycol or fatty acid ester of 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 dosage form of the present invention is a suspension, a liquid diluent such as water, ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, a micro Crystalline cellulose, aluminum metahydroxide, bentonite, agar or tracanth and the like 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 hemiester salts, fatty acid protein hydrolyzates, isethionates, lanolin derivatives, aliphatic alcohols, vegetable oils, glycerol, sugars, etc. may be used as carrier components. can
본 발명은 또한 상기 화학식 1로 대표되는 화합물을 개체의 피부에 도포하는 단계를 포함하는, 피부 미백, 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 provides a method for skin whitening, enhancing skin elasticity, improving skin wrinkles, or moisturizing the skin, comprising the step of applying a compound represented by Chemical Formula 1 to the skin of a subject. The subject includes, without limitation, mammals including mice, livestock, humans, and the like.
본 발명의 또 다른 실시예에 따르면, 본 발명은 상기 화학식 1의 화합물을 유효성분으로 함유하는 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용 약학적 조성물을 제공한다. According to another embodiment of the present invention, the present invention provides a pharmaceutical composition for skin whitening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing, containing the compound of Formula 1 as an active ingredient.
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.A composition containing the compound of the present invention may be in various oral or parenteral formulations, but may preferably be a parenteral formulation. When formulated, it is prepared using diluents or excipients such as commonly used fillers, extenders, binders, wetting agents, disintegrants, and surfactants. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and these solid preparations include at least one excipient in one or more compounds, for example, starch, calcium carbonate, sucrose or lactose ( lactose) and gelatin. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral administration include suspensions, solutions for oral administration, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, aromatics, and preservatives may be included. there is. Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, and emulsions. Propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate may be used as non-aqueous solvents and suspending agents.
본 발명은 또한 상기 화학식 1의 화합물을 유효성분으로 포함하는 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용 피부 외용제의 제형으로 제공할 수 있다.The present invention may also be provided in the form of an external skin preparation for skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing, containing the compound of Formula 1 as an active ingredient.
상기 화학식 1의 화합물을 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 Formula 1 is used as an external skin preparation, it may additionally include 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 stabilizer, a foaming agent, a fragrance, and a surfactant. , water, ionic or nonionic emulsifiers, fillers, sequestering agents and chelating agents, preservatives, vitamins, blocking agents, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic actives, lipid vesicles, or external preparations for skin It may contain adjuvants commonly used in the field of dermatology, such as any other ingredients used as In addition, the components may be introduced in an amount generally used in the field of skin science.
상기 화학식 1의 화합물이 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 is provided as a formulation for external application to the skin, it may have formulations 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 can be particularly preferably used as a parenteral preparation, and for example, the external skin preparation may include a suitable pharmaceutically acceptable base such as petrolatum and stearyl alcohol; suitable pharmaceutically acceptable surfactants such as polysorbate and sorbitan sesquioleate; suitable pharmaceutically acceptable moisturizers such as glycerin; suitable pharmaceutically acceptable solvents; and a flavoring agent, a colorant, a stabilizer, a viscosifying agent, and the like can be prepared by a conventional method for preparing an external preparation for skin.
또한, 본 발명의 상기 화학식 1의 화합물을 의약품으로 사용하는 경우, 추가로 동일 또는 유사한 기능을 나타내는 유효성분을 1종 이상 함유할 수 있다. 예컨대, 공지의 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용 성분을 포함할 수 있을 것이다. 추가적인 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용 성분을 포함하게 되면 본 발명의 조성물의 피부 미백, 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. In addition, when the compound represented by Formula 1 of the present invention is used as a pharmaceutical, it may additionally contain one or more active ingredients exhibiting the same or similar functions. For example, it may include known ingredients for skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing. When additional skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing components are included, the skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing effect of the composition of the present invention may be further enhanced. When adding the above components, skin safety according to combined use, ease of formulation, and stability of active ingredients may be considered.
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 미백 성분으로, 코즈산(Kojic acid), 알부틴(Arbutin) 등과 같은 티로시나제 효소활성을 억제하는 물질, 하이드로퀴논(Hydroquinone), 비타민-C(L-Ascorbic acid); 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 present invention, the composition is a skin elasticity or wrinkle improvement component known in the art, retinoic acid, TGF, protein derived from animal placenta, betulinic acid and chlorella extract; As a whitening ingredient known in the art, substances that inhibit tyrosinase enzyme activity such as Kojic acid and arbutin, hydroquinone, vitamin-C (L-Ascorbic acid); As moisturizing ingredients known in the art, petrolatum (vaseline), mineral oil, silicone, neutral fat, essential fatty acids (eg gamma linolenic acid (evening primrose oil)), GGF, amino acids, provitamin B5, hyaluronic acid, poly- γ-glutamic acid, Lipidure PMB, ceramides, cholesterol, fatty acids; And it may further include one or two or more components selected from the group consisting of derivatives thereof and various plant extracts. The additional component may be included in an amount of 0.0001% to 10% by weight based on the total weight of the composition, and the content range may be adjusted according to requirements such as skin safety and ease of formulation of the compound of Formula 1.
본 발명의 약학적 조성물은 유효량의 상기 화학식 1의 화합물을 포함할 때 바람직한 피부 미백, 피부 탄력 증진, 피부 주름 개선 또는 피부 보습 효과를 제공할 수 있다. 본 발명에 있어서, '유효량'이라 함은 피부 미백, 피부 탄력 증진, 피부 주름 개선 또는 피부 보습 효과를 충분히 나타낼 수 있는 화합물의 양을 의미한다.When the pharmaceutical composition of the present invention contains an effective amount of the compound of Formula 1, it can provide desirable skin whitening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing effects. In the present invention, 'effective amount' refers to an amount of a compound capable of sufficiently exhibiting skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing effect.
본 발명의 조성물에 포함되는 상기 화학식 1의 화합물의 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 1 included in the composition of the present invention will vary depending on the form in which the composition is commercialized, how the compound is applied to the skin, and how long the compound stays on the skin. For example, when the composition is commercialized as a pharmaceutical product, it may contain the compound of Formula 1 at a higher concentration than when the composition is commercialized as a cosmetic product that is routinely applied to the skin. Therefore, the daily dose 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, and 1 to 100 mg/kg per day. 6 doses may be administered.
본 발명의 또 다른 실시예에 따르면 상기 화학식 1의 화합물을 포함하는 피부 미백용, 피부 탄력 증진용, 피부 주름 개선용 또는 피부 보습용 건강식품을 제공한다.According to another embodiment of the present invention, a health food for skin whitening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing containing the compound of Formula 1 is provided.
본 명세서에서 '건강식품'이란, 상기 화학식 1의 화합물을 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 미백, 피부 탄력 증진, 피부 주름 개선 또는 피부 보습에 우수한 효과를 기대할 수 있어 매우 유용하다.In the present specification, 'health food' refers to a food prepared by adding the compound of Formula 1 to food materials such as beverages, teas, spices, chewing gum, confectionery, etc., or encapsulated, powdered, or suspended. It means that it brings about a specific effect, but unlike general drugs, it has the advantage of not having side effects that may occur when taking drugs for a long time using food as a raw material. Since the health food of the present invention obtained in this way can be consumed on a daily basis, it is very useful because it can be expected to have excellent effects on skin whitening, skin elasticity enhancement, skin wrinkle improvement, or skin moisturizing.
상기 화학식 1의 화합물을 식품첨가물로 사용하는 경우, 상기 화학식 1의 화합물을 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 Formula 1 is used as a food additive, the compound of Formula 1 may be added as it is or used together with other foods or food ingredients, and may be appropriately used according to conventional methods. The mixing amount of the active ingredient may be appropriately determined depending on the purpose of use (prevention, health or therapeutic treatment). In general, when preparing food or beverage, the composition of the present invention is added in an amount of 15 parts by weight or less, preferably 10 parts by weight or less, based on the raw material. However, in the case of long-term intake for the purpose of health and hygiene or health control, 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 above the above range. . There is no particular limitation on the type of food. Examples of foods to which the substance can be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum, dairy products including ice cream, various soups, beverages, tea, drinks, There are alcoholic beverages and vitamin complexes, and includes all health foods in a conventional sense. The health beverage composition of the present invention may contain various flavoring agents or natural carbohydrates as additional components, like conventional beverages. The aforementioned natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As the sweetener, natural sweeteners such as thaumatin and stevia extract, or synthetic sweeteners such as saccharin and aspartame may be used. The proportion 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 includes various nutrients, vitamins, electrolytes, flavors, colorants, pectic acid and its salts, alginic acid and its salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohol , carbonation agents used in carbonated beverages, and the like. In addition, the health food of the present invention may contain fruit flesh for the production of natural fruit juice, fruit juice beverages and vegetable beverages. These components may be used independently or in combination. The ratio of these additives is not very important, 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 화합물을 전체 조성물 중량에 대하여 0.00001 중량% 내지 10 중량%로 포함할 수 있다.Although not limited thereto, in one embodiment of the present invention, the composition may include the compound of Formula 1 in an amount of 0.00001% to 10% by weight based on the total weight of the composition.
본 발명의 티모사포닌 에이-쓰리를 함유하는 조성물은 피부 미백, 피부 탄력 증진, 피부 주름 개선 또는 피부 보습에 우수한 효과를 나타낸다. The composition containing thymosaponin A-3 of the present invention shows excellent effects on skin whitening, skin elasticity enhancement, skin wrinkle improvement or skin moisturizing.
본 발명의 티모사포닌 에이-쓰리를 함유하는 조성물은 피부에 안전하면서도 피부 상태 개선 효과가 우수한 화장품 원료, 약학 성분 또는 건강식품 원료로 이용될 수 있다.The composition containing thymosaponin A-3 of the present invention can be used as a cosmetic raw material, a pharmaceutical ingredient, or a health food raw material that is safe for the skin and has an excellent skin condition improvement 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 following examples and the like will be described in order to explain the present invention in more detail. However, embodiments according to the present invention can be modified in many different forms, and the scope of the present invention should not be construed as being limited to the embodiments described below. Embodiments of the present invention are provided by way of example to help a detailed understanding of the present invention.
참조예reference example 1: One: 티모사포닌thymosaponin 에이- no way- 쓰리three (( TimosaponinTimosaponin A-Ⅲ) 물질 정보A-Ⅲ) Substance information
[화학식 1][Formula 1]
물질명 : Timosaponin A-ⅢSubstance name: Timosaponin A-Ⅲ
CAS No. : 41059-79-4CAS No. : 41059-79-4
분자식 : C39H64O13 Molecular Formula: C 39 H 64 O 13
분자량 : 740.92Molecular Weight: 740.92
구입처 : Kang Zhongshan and the source of BiotechnologyWhere to buy: Kang Zhongshan and the source of Biotechnology
실험예Experimental example 1: 인체 유래의 섬유아세포에서 제1형 콜라겐(type I collagen) 합성 촉진 효과 1: Effect of promoting synthesis of type I collagen in human-derived 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 Formula 1 was added to the culture medium of human-derived fibroblasts to confirm the effect of promoting type 1 collagen synthesis at the cellular level. The measurement of synthesized collagen was quantified using a PICP EIA kit (Procollagen Type I C-Peptide Enzyme Immuno Assay KIT). In order to measure the amount of collagen synthesis, the compound of Formula 1 was added to the culture medium (DMEM medium) of fibroblasts, cultured for 48 hours, and then the culture medium was taken and the degree of type 1 collagen synthesis at each concentration was measured using 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 comparison of the effect, the degree of collagen synthesis was measured in the same manner for the samples to which the culture medium of untreated fibroblasts (negative control) and vitamin C (positive control) were added to a final concentration of 52.85 μg/ml. The rate of increase in collagen production was calculated as the ratio of the amount of collagen production relative to the control group, and the results are shown in Table 1 below.
화학식 1의 화합물의 콜라겐 합성 촉진 효과 (반복수 =4)Collagen synthesis promoting effect of the compound of Formula 1 (Number of repetitions = 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 Formula 1 was treated, the amount of collagen synthesis was increased in a concentration-dependent manner, and in general, similar collagen at a lower concentration than when vitamin C, which is well known to induce collagen synthesis, was applied. synthetic effect was shown.
실험예Experimental example 2: 2: 엘라스테이즈Elastase 활성 저해 효과 active inhibitory effect
엘라스틴(Elastin)을 분해하는 효소인 엘라스테이즈(Elastase)의 활성 저해 효과를 다음과 같이 확인하였다.The effect of inhibiting the activity 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 derived from human leukocytes was used, and a synthetic substrate MeOSuc-Ala-Ala-Pro-Val-pNA was used as a substrate for the elastase. A 100 mM Tris (pH 7.5) solution was used as the buffer solution. Elastase was finally used at 0.2 mU using a buffer solution. In addition, the synthetic substrate of Elastase was diluted with a buffer solution to a final concentration of 0.5 mM after making a 100 mM solution using DMSO. At this time, as a positive control group, quercetin known as an elastase inhibitor was set at a concentration of 10 ppm. The elastase inhibitory candidate was added to a final concentration of 10 or 20 ppm. The reaction was carried out in a 96-well plate and reacted at room temperature for 20 minutes. The absorbance was measured at 405 nm at 1-minute intervals using a spectrophotometer, and the slope of the absorbance versus time was determined to determine the activity of the enzyme. The elastase inhibition rate was calculated as follows.
화학식 1의 화합물의 엘라스테이즈 활성 저해 효과 (반복수 =3)Elastase activity inhibitory effect of the compound of Formula 1 (number of repetitions = 3)
상기 표 2의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 20 ppm의 농도에서 엘라스테이즈 활성 저해 효과가 양성대조군인 퀘르세틴에 상응하는 정도로 높게 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 of Table 2, the compound of Formula 1 exhibits an elastase activity inhibitory effect corresponding to that of the positive control, quercetin, at a concentration of 20 ppm, and the compound of Formula 1 has an excellent elastase activity inhibitory effect. confirmed that Accordingly, it was found that the compound of Formula 1 can be effectively used for improving skin elasticity and wrinkles.
실험예Experimental example 3: 3: 당화glycosylation 저해(anti- inhibition (anti- glycationglycation ) 효과) effect
당화 저해(anti-glycation) 효능을 확인하기 위하여, L-arginine과 포도당을 이용하여 당화 저해 활성을 측정하였다. In order to confirm anti-glycation efficacy, anti-glycation 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, 1M L-arginine and 1M glucose were dissolved in 1M phosphate buffer (pH 7.4), and samples were diluted to 50 and 100 ppm using 1M phosphate buffer. 1M L-arginine and 1M phosphate buffer were mixed at a ratio of 1:4, and then 80 μl was dispensed into a 96-well plate. Samples diluted to 50 and 100 ppm, respectively, and 100 μl of 0.01 M aminoguanidine to be used as a positive control were added thereto. After mixing these samples well, finally, after adding glucose diluted with 1M phosphate buffer so that the final concentration of glucose is 0.1M, the mixture was reacted at 70°C for 4 hours. The degree of glycosylation was measured by measuring the absorbance at 420 nm of the 96-well plate 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. The Glycation experimental group of the following formula is an experimental group in which 1M L-arginine and 1M glucose are added to induce glycation. Glycosylation inhibitory activity can be obtained by the following formula.
화학식 1의 화합물의 항당화 효과Anti-glycation 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 미백 또는 피부 주름 및 탄력 개선에 있어서, 항당화 효과가 보조적인 역할로 작용하여 상승효과를 기대할 수 있다.As can be seen from the results in Table 3, it was found that the compound of Formula 1 has a more excellent anti-glycation effect than aminoguanidine known as an anti-glycation substance. That is, the compound of Formula 1 exhibits an excellent antiglycation effect, and thus, in skin whitening or improvement of skin wrinkles and elasticity, the antiglycation effect acts as an auxiliary role, and a synergistic effect can be expected.
실험예Experimental example 4: 미백 효과-멜라닌 총량 감소 효과 4: Whitening effect - melanin total amount reduction effect
화학식 1의 화합물을 쥐의 멜라노마 세포(B-16 mouse melanoma cell)의 배양액에 첨가하여 세포 수준에서의 멜라닌 총량을 측정함으로써 미백 효과를 확인하였다(Lotan R., Lotan D. Cancer Res. 40:3345-3350, 1980). 실험 전 쥐의 멜라노마 세포에 대하여 독성을 평가하여 독성이 없는 농도를 선정하여 미백평가를 수행하였다. The compound of Formula 1 was added to the culture medium of mouse melanoma cells (B-16 mouse melanoma cells), and the whitening effect was confirmed by measuring the total amount of melanin at the cellular level (Lotan R., Lotan D. Cancer Res . 40: 3345-3350, 1980). Prior to the experiment, toxicity was evaluated for melanoma cells of mice, and whitening evaluation was performed by selecting a non-toxic concentration.
화학식 1의 화합물을 배양액에 최종 농도가 1 ppm 또는 10 ppm이 되도록 하였으며, 대조군인 알부틴은 100 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 or 10 ppm, and arbutin, a control, was added to the medium to be 100 ppm, and each B-16 melanoma cell was treated 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. Thereafter, the cells were treated with trypsin, detached from the culture vessel, centrifuged, and then melanin was extracted. The detached cells were boiled for 10 minutes in 1 ml of sodium hydroxide solution (1N concentration) 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 저해율(%)로 계산하고 결과를 하기 표 5에 정리하였다.The amount of melanin was measured by a method of expressing absorbance per unit cell number (1×10 6 cell), and the total amount of melanin relative to the control group was calculated as an inhibition rate (%), and the results are summarized in Table 5 below.
농도에 따른 세포수준에서의 멜라닌 총량의 감소 효과The effect of reducing the total amount of melanin at the cellular level according to the concentration
상기 표 4의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 양성대조군인 알부틴과 비교했을 때, 10 ppm에서도 상당히 우수한 멜라닌 총량 감소 효과를 나타내어, 미백 용도로 사용할 수 있음을 알 수 있었다.As can be seen from the results of Table 4, the compound of Formula 1 showed a significantly superior effect of reducing the total amount of melanin even at 10 ppm, compared to arbutin, a positive control group, and it was found that it could be used for whitening purposes.
Claims (7)
[화학식 1]
A composition for skin whitening comprising a compound represented by Formula 1 below as an active ingredient.
[Formula 1]
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