KR20160019765A - Cosmetic or pharmaceutical composition for melanism, elasticity, anti-wrinkle, or skin moisturizing comprising dihydroartemisinin - Google Patents
Cosmetic or pharmaceutical composition for melanism, elasticity, anti-wrinkle, or skin moisturizing comprising dihydroartemisinin Download PDFInfo
- Publication number
- KR20160019765A KR20160019765A KR1020140104508A KR20140104508A KR20160019765A KR 20160019765 A KR20160019765 A KR 20160019765A KR 1020140104508 A KR1020140104508 A KR 1020140104508A KR 20140104508 A KR20140104508 A KR 20140104508A KR 20160019765 A KR20160019765 A KR 20160019765A
- Authority
- KR
- South Korea
- Prior art keywords
- skin
- present
- composition
- elasticity
- hair
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- 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
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
-
- 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
- A61Q19/007—Preparations for dry skin
-
- 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
- A61Q19/08—Anti-ageing preparations
-
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Mycology (AREA)
- Birds (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
본 발명은 흑화, 탄력, 주름개선, 또는 보습 등의 우수한 효과를 가지는, 특히 피부 또는 모발과 관련된 우수한 효과를 가지는 화장료 조성물, 약학 조성물 및 건강식품에 관한 것이다. 본 발명은 또한 적은 양으로도 위와 같은 효과를 발휘할 수 있는 화장료 조성물, 약학 조성물 및 건강식품에 관한 것이다.The present invention relates to a cosmetic composition, a pharmaceutical composition and a health food, which have excellent effects such as blackening, elasticity, wrinkle improvement, moisturizing and the like, particularly excellent effects related to skin or hair. The present invention also relates to a cosmetic composition, a pharmaceutical composition and a health food which can exert such effects even in a small amount.
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 dark brown Eumelanin. Melanin in hair is an important factor that determines the color of hair. Melanin produced in the melanocyte present in the hair is 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 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.
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 반응, 마이야르 반응으로 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. The glycation takes place through a series of chemical reactions known as amarylidation, maillard reaction, resulting 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), which inhibits skin elasticity and promotes wrinkle formation by preventing collagen from forming a proper structure
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 glycation. 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 안정하며, 무엇보다도 기존의 피부 탄력, 주름개선, 보습 및 피부 또는 모발의 흑화가 있는 물질보다 효과가 우수한 피부 탄력, 주름개선, 보습 또는 피부 또는 모발의 흑화 효과를 지닌 성분의 개발이 절실히 요망되고 있다.Accordingly, it is possible to provide a composition which is safe and biologically safe, has an excellent effect on skin elasticity, wrinkle, moisturizing effect, skin elasticity, wrinkle improvement, moisturizing effect or blackening effect of skin or hair, The development of a component having the above properties is urgently required.
따라서 본 발명은 위와 같은 문제점을 해결하고, 부작용이 적고 인체에 안전하면서도 피부 탄력, 주름개선, 보습, 또는 피부 또는 모발의 흑화가 우수한 새로운 활성 성분, 즉, 활성 성분의 이러한 유용한 용도를 제공하는 것이다.Accordingly, the present invention provides such a useful use of a new active ingredient, i.e., an active ingredient, which solves the above problems and is safe for the human body and has excellent skin elasticity, wrinkle, moisturizing, or blackening of skin or hair, .
다시 말해, 본 발명이 해결하고자 하는 과제는 상기 효능이 우수한 활성 성분을 유효성분으로 포함하는 조성물을 제공하고자 한다.In other words, a problem to be solved by the present invention is to provide a composition comprising the active ingredient having excellent efficacy as an active ingredient.
상기 과제를 해결하기 위하여, 본 발명은 다이하이드로아르테미시닌(Dihydroartemisinin)을 유효성분으로 포함하는 피부 탄력 증진용, 주름개선용, 보습용, 및 피부 또는 모발의 흑화용 조성물, 바람직하게는 화장료 조성물, 약학 조성물 또는 건강식품을 제공한다. In order to solve the above problems, the present invention relates to a composition for skin elasticity enhancement, wrinkle improvement, moisturizing, and blackening of skin or hair comprising dihydroartemisinin as an active ingredient, , A pharmaceutical composition or a health food.
즉, 본 발명은 다이하이드로아르테미시닌의 피부 탄력 증진용, 주름개선용, 보습용 및 피부 또는 모발의 흑화용 이라는 새로운 용도를 제공한다.That is, the present invention provides a novel use of dihydroartemisinin for skin elasticity enhancement, wrinkle improvement, moisturizing, and blackening of skin or hair.
본 발명의 발명자들은 다이하이드로아르테미시닌이 피부의 콜라게나제 및 엘라스타제 활성을 저해하고, 항당화 효과를 나타냄으로써 피부의 재생을 촉진하며, 보습, 피부 탄력 및 주름개선 효과가 있다는 사실을 확인하고 본 발명을 완성하게 되었다. 또한 상기 다이하이드로아르테미시닌은 멜라닌 합성을 촉진시켜 피부 또는 모발의 흑화 효과를 나타내는 것을 확인하고 본 발명을 완성하게 되었다.The inventors of the present invention have found that dihydroartemisinin inhibits collagenase and elastase activity of skin and exhibits antagonism effect, thereby promoting regeneration of skin, moisturizing, skin elasticity and wrinkle-reducing effect And completed the present invention. Further, it has been confirmed that the dihydroartemisinin promotes the synthesis of melanin to show the blackening effect of the skin or hair, and the present invention has been completed.
본 발명에 있어서, '흑화'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 있다.In the present invention, 'blackening' means that the coloring matter of the skin or hair is increased, and in particular, the amount of melanin pigment is increased, which means that the skin or hair becomes dark color.
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, '주름개선 효과'라 함은 피부에 주름이 생성되는 것을 억제 또는 저해하거나, 이미 생성된 주름을 완화시키는 것을 말한다. In the present invention, the term " wrinkle-reducing effect " refers to inhibiting or inhibiting the generation of wrinkles on the skin, or alleviating already-generated wrinkles.
본 발명에 있어서, '보습 또는 피부 보습'이라 함은 피부에 수분감을 증가시켜주고, 촉촉한 상태를 유지시키는 것을 의미한다. 피부 보습 효과는 피부의 주름개선, 탄력도 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 발명은 상기와 같은 문제점들을 해결하고, 본 발명의 목적을 달성하기 위하여 하기 화학식 1로 대표되는 화합물을 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 general formula (1).
[화학식 1][Chemical Formula 1]
상기 화학식 1로 대표되는 화합물은 분자식 C15H24O5, 분자량 284.35 을 가지며, 다이하이드로아르테미시닌(Dihydroartemisinin), dihydroqinghaosu, artenimol 또는 DHA 등으로 명명된다. The compound represented by the formula (1) has the molecular formula C 15 H 24 O 5 , the molecular weight is 284.35, and is named dihydroartemisinin, dihydroqinghaosu, artenimol or DHA.
본 발명은 상기 다이하이드로아르테미시닌의 획득 방법에 특별히 한정되지 않으며, 당 업계에 공지된 방법으로 화학적으로 합성하거나, 시판되는 물질을 사용할 수 있다. The present invention is not particularly limited to the method for obtaining dihydroartemisinin, and may be chemically synthesized by a method known in the art, or a commercially available material may be used.
본 발명에 따른 화장료 조성물, 약학 조성물 및 건강식품에 있어, 상기 다이하이드로아르테미시닌의 함량은 화장료 조성물, 약학 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 dihydroartemisinin is preferably 0.00001 to 10% by weight based on the total weight of the cosmetic composition, the pharmaceutical composition and the health food.
본 발명의 다이하이드로아르테미시닌은 수화물, 에탄올화물 등의 형태를 포함하는 용매화된 형태뿐만 아니라 비-용매화된(unsolvated) 형태로 존재할 수도 있다. 본 발명의 다이하이드로아르테미시닌은 결정형 또는 무정형 형태로 존재할 수 있으며, 이러한 모든 물리적 형태는 본 발명의 범위에 포함된다.The dihydroartemisinin of the present invention may exist in solvated as well as unsolvated forms, including forms such as hydrates, ethanolates, and the like. The dihydroartemisinin 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 탄력, 주름개선, 보습 효과 또는 피부 또는 모발의 흑화용 화장료 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 cosmetic composition for skin elasticity, wrinkle improvement, moisturizing effect, or blackening of skin or hair according to the present invention can be used as a cosmetic composition for skin, hair or the like in the form of a solution, an external ointment, a cream, a foam, a nutrition lotion, a softening water, The compositions of the present invention may be formulated as liquid cleansers, bath salts, sunscreen creams, sun oils, suspensions, emulsions, pastes, gels, lotions, powders, soaps, surfactant- containing cleansing oils, powder foundations, emulsion foundations, waxes, But are not limited thereto. ≪ Desc / Clms Page number 12 >
또한, 본 발명의 화장료 조성물은 일반 피부 화장료에 배합되는 화장품학적으로 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 incorporated 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 화장품학적으로 허용 가능한 담체는 제형에 따라 다양하다. 본 발명의 제형이 연고, 페이스트, 크림 또는 젤인 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 to be 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, silicone, bentonite, silica, talc, zinc oxide Mixtures of these may be used.
본 발명의 제형이 파우더 또는 스프레이인 경우에는, 담체 성분으로서 락토스, 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-브틸글리콜 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 ester, polyethylene glycol 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 화합물을 개체의 피부에 도포하는 단계를 포함하는, 피부 탄력, 주름개선, 보습 또는 피부 또는 모발의 흑화방법을 제공한다. 상기 개체는 쥐, 가축, 인간 등을 포함하는 포유동물을 제한 없이 포함한다. The present invention also provides a method for skin elasticity, wrinkle improvement, moisturizing, or blackening of skin or hair, comprising the step of applying the compound represented by formula (1) to the individual's skin. The subject includes, without limitation, mammals including rats, livestock, humans, and the like.
본 발명의 또 다른 실시예에 따르면, 본 발명은 상기 화학식 1의 화합물을 유효성분으로 함유하는 피부 탄력, 주름개선, 보습 또는 피부 또는 모발의 흑화용 약학적 조성물을 제공한다. According to another embodiment of the present invention, there is provided a pharmaceutical composition for skin elasticity, wrinkle improvement, moisturizing, or blackening of skin or hair containing the compound of Chemical 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 에스테로 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. Examples of the non-aqueous solvent and the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate.
본 발명은 또한 상기 화학식 1의 화합물을 유효성분으로 포함하는 피부 탄력, 주름개선, 보습 효과 또는 피부 또는 모발의 흑화효과를 위한 피부 외용제의 제형으로 제공할 수 있다.The present invention can also be provided as a form of external skin preparation for skin elasticity, wrinkle improvement, moisturizing effect or blackening effect of skin or hair 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 preparation for skin, it may further comprise at least one selected from the group consisting of fatty substances, organic solvents, solubilizers, thickeners and gelling agents, softeners, antioxidants, suspending agents, stabilizers, foaming agents, , Water, ionic or nonionic emulsifiers, fillers, sequestering agents and chelating agents, preservatives, vitamins, blocking agents, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or external preparations for skin And any other ingredients used in the skin sciences. The components can also be introduced in amounts commonly used in the field of dermatology.
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 an external preparation for skin, 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, 스테아릴알콜 등의 약제학적으로 허용되는 적당한 기제; 폴리소르베이트, 솔르비탄 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 화합물을 의약품으로 사용하는 경우, 추가로 동일 또는 유사한 기능을 나타내는 유효성분을 1종 이상 함유할 수 있다. 예컨대, 공지의 피부 피부 탄력, 주름개선, 보습 효과 또는 피부 또는 모발의 흑화 성분을 포함할 수 있을 것이다. 추가적인 피부 탄력, 주름개선, 보습 또는 피부 또는 모발의 흑화 성분을 포함하게 되면 본 발명의 조성물의 피부 탄력, 주름개선, 보습효과 또는 피부 또는 모발의 흑화 효과는 더욱 증진될 수 있을 것이다. 상기 성분 추가 시에는 복합 사용에 따른 피부 안전성, 제형화의 용이성, 유효성분들의 안정성을 고려할 수 있다. 본 발명의 한 구체예에서, 상기 조성물은 당업계에 공지된 피부 탄력 또는 주름 개선 성분으로서, 레티노산, TGF, 동물 태반 유래의 단백질, 베툴린산 및 클로렐라 추출물; 당업계에서 공지된 흑화용 성분으로 에리트룰로스 (Erythrulose), 디하이드록시아세톤 (Dihydroxyacetone); 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 있을 것이며, 상기 함량 범위는 피부 안전성, 상기 화학식 1의 화합물의 제형화 시의 용이성 등의 요건에 따라 조절될 수 있을 것이다.When the compound of Chemical Formula 1 of the present invention is used as a medicine, it may further contain one or more active ingredients showing the same or similar functions. For example, it may contain known skin elasticity, wrinkle improvement, moisturizing effect or blackening component of skin or hair. The skin elasticity, wrinkle improvement, moisturizing effect, or blackening effect of the skin or hair of the composition of the present invention can be further enhanced by the addition of the additional skin elasticity, wrinkle improvement, moisturizing or blackening component of skin or hair. When the above ingredients are added, skin safety, easiness of formulation, and stability of effective ingredients can be considered according to the combined use. In one embodiment of the invention, the composition is a skin elasticity or wrinkle improving ingredient known in the art as retinoic acid, TGF, animal placenta-derived proteins, betulinic acid and chlorella extract; As components for blackening known in the art, such as Erythrulose, Dihydroxyacetone; And derivatives thereof, and various plant extracts. ≪ Desc / Clms Page number 2 > 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, ease of formulation of the compound of Formula 1 .
본 발명의 약학적 조성물은 유효량의 상기 화학식 1의 화합물을 포함할 때 바람직한 피부 탄력, 주름개선, 보습 효과 또는 피부 또는 모발의 흑화 효과를 제공할 수 있다. 본 발명에 있어서, '유효량'이라 함은 피부 또는 모발의 흑화 효과를 나타내거나, 탄력 증진 및 주름 개선 효과를 나타내거나 보습 효과를 나타낼 수 있는 화합물의 양을 의미한다.The pharmaceutical composition of the present invention can provide a desired skin elasticity, wrinkle, moisturizing effect, or blackening effect of skin or hair when an effective amount of the compound of Formula 1 is included. In the present invention, the term "effective amount" means an amount of a compound which exhibits a blackening effect of skin or hair, exhibits an elasticity improving effect and a wrinkle-improving effect, or exhibits a 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. An effective amount of the compound of formula (1) contained 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 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 화합물을 포함하는 피부 탄력 효과, 주름개선 효과, 보습 효과 또는 피부 또는 모발의 흑화 효과를 위한 건강식품을 제공한다.According to another embodiment of the present invention, there is provided a skin elasticity improving effect, a wrinkle improving effect, a moisturizing effect, or a health food for skin or hair blackening effect containing the compound of formula (1).
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 높은 피부 또는 모발의 흑화 효과, 탄력 증진 효과, 주름개선 효과, 및 보습 효과를 기대할 수 있어 매우 유용하다.The term 'health food' as used herein means a food prepared by adding the compound of formula (1) to food materials such as beverage, tea, spice, gum and confectionery, or by encapsulation, powdering or suspension, But it has the advantage that there are no side effects that can occur when a drug is used for a long period of time using a food as a raw material. Since the health food of the present invention thus obtained can be routinely ingested, it is very useful because it can be expected to have a high skin or hair blackening effect, an elasticity increasing effect, a wrinkle reducing effect, and a moisturizing effect.
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, 알콜 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, 슈크로스와 같은 디사카라이드, 및 덱스트린, 사이클로덱스트린과 같은 폴리사카라이드, 자일리톨, 소르비톨, 에리트리톨 등의 당알콜이다. 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, 알콜, 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 is used as a food additive, the compound of Chemical Formula 1 may be added as it is or may be used together with other food or food ingredients, and may 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 healthy 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. Such natural carbohydrates are monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, and polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as 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 adjusting agents, stabilizers, preservatives, , 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 화합물을 전체 조성물 중량에 대하여 0.00001 중량% 내지 10 중량%로 포함할 수 있다.
In one embodiment of the present invention, the composition may include 0.00001 wt% to 10 wt% of the compound of Formula 1 based on the weight of the entire composition.
본 발명의 다이하이드로아르테미시닌을 함유하는 조성물은 피부 또는 모발의 흑화 효과를 나타낸다.The composition containing the dihydroartemisinin of the present invention exhibits the blackening effect of the skin or hair.
본 발명의 다이하이드로아르테미시닌을 함유하는 조성물은 피부 탄력 증진 또는 주름 개선 효과를 나타낸다. The composition containing dihydroartemisinin of the present invention exhibits skin elasticity enhancement or wrinkle improvement effect.
본 발명의 다이하이드로아르테미시닌을 함유하는 조성물은 피부 보습 효과를 나타낸다. The composition containing dihydroartemisinin of the present invention shows skin moisturizing effect.
본 발명의 다이하이드로아르테미시닌을 함유하는 조성물은 안전하면서도 우수한 화장품 원료, 약학 성분으로 이용될 수 있다.The composition containing the dihydroartemisinin of the present invention can be used as safe and excellent cosmetic ingredients and pharmaceutical ingredients.
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: 다이하이드로아르테미시닌Dihydroartemisinin (( DihydroartemisininDihydroartemicinin ) 물질 정보) Material information
[화학식 1][Chemical Formula 1]
물질명 : DihydroartemisininMaterial name: Dihydroartemisinin
CAS No. : 71939-50-9CAS No. : 71939-50-9
분자식 : C15H24O5 Molecular formula: C 15 H 24 O 5
분자량 : 284.35 Molecular weight: 284.35
구입처 : Tauto Biotech (중국)
Where to buy: Tauto Biotech (China)
실시예Example 1: One: 콜라게네이즈Collagenase 활성 억제 효과 Activity inhibitory effect
콜라겐(Collagen)을 분해하는 효소인 콜라게나제의 활성 저해 효과를 다음과 같이 확인하였다. The inhibitory effect of collagenase, an enzyme that degrades collagen, was confirmed as follows.
콜라게나제는 쥐의 이자에서 유래한 콜라게나제를 사용하였고, 콜라게나제의 기질로 합성 기질인 N-(3-[2-Furyl]acryloyl)-Leu-Gly-Pro-Ala을 사용하였다. 완충용액은 50mM Tricine, 10mM CaCl2·H2O, 400mM NaCl(pH 7.5)이 녹아 있는 용액을 사용하였다. 합성 기질은 완충용액을 이용하여 10mM의 농도로 녹인 후 최종적으로 75μM이 되도록 희석하였다. 콜라게나제는 4도의 차가운 3차 증류수를 이용하여 1unit/ml 농도로 녹인 후 최종적으로 0.05unit/ml이 되도록 완충용액을 이용하여 희석하였다. 콜라게나제 저해 후보는 최종농도 25, 50ppm에서 실험하였다. 이 때, 양성 대조군은 콜라게나제 저해 효과가 알려진 에피갈로카테킨 갈레이트(EGCG)를 최종농도 50ppm이 되도록 설정하였다. 반응은 96-웰플레이트에서 진행하였으며, 상온에서 10분간 반응시켰다. 분광 광도계를 이용하여 1분 간격으로 345 nm에서 흡광도를 측정하여 시간 대비 흡광도의 최대 기울기를 구하여 효소의 활성으로 정하였다. 콜라게나제 저해율은 다음과 같이 계산하였다.Collagenase used collagenase derived from rat's interest and N- (3- [2-Furyl] acryloyl) -Leu-Gly-Pro-Ala was used as a collagenase substrate. The buffer solution used was a solution of 50 mM Tricine, 10 mM CaCl 2 .H 2 O, 400 mM NaCl (pH 7.5) dissolved therein. The synthetic substrate was dissolved in a buffer solution at a concentration of 10 mM and finally diluted to 75 μM. The collagenase was dissolved at a concentration of 1 unit / ml using cold third distilled water at 4 ° C and then diluted with buffer solution to a final concentration of 0.05 unit / ml. Collagenase inhibition candidates were tested at final concentrations of 25 and 50 ppm. At this time, the positive control group was set to have a final concentration of 50 ppm of epigallocatechin gallate (EGCG) whose collagenase inhibitory effect was known. The reaction was carried out in a 96-well plate and allowed to react at room temperature for 10 minutes. Absorbance was measured at 345 nm using a spectrophotometer at intervals of 1 minute, and the maximum slope of absorbance versus time was determined to determine the activity of the enzyme. Collagenase inhibition rates were calculated as follows.
화학식 1의 화합물의 콜라게나제 활성 저해 효과 (반복수 =3)Inhibition of Collagenase Activity of Compound (1) (Number of Repeats = 3)
상기 표 1의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 양성대조군인 EGCG 보다 콜라게나제 활성 저해 효과가 뛰어남을 알 수 있다. 즉, 화학식 1의 화합물은 우수한 콜라게나제 활성 저해효과를 발휘하였다. 따라서, 화학식 1의 화합물은 피부재생, 주름개선을 위한 용도로 사용할 수 있음을 알 수 있었다.
As can be seen from the results shown in Table 1, the compound of Chemical Formula 1 is more excellent in inhibiting collagenase activity than EGCG, which is a positive control. That is, the compound of formula (1) exerts excellent collagenase activity inhibitory effect. Therefore, it was found that the compound of Chemical Formula 1 can be used for skin regeneration and wrinkle improvement.
실시예Example 2: 2: 엘라스타제Elastase 활성 저해 효과 Active 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-웰플레이트에서 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 absorbance versus time was determined as the activity of the enzyme. Ella stasis inhibition rates were calculated as follows.
화학식 1의 화합물의 엘라스타제 활성 저해 효과 (반복수 =3)Inhibitory effect of the compound of formula (1) on elastase activity (number of repeats = 3)
상기 표 2의 결과에서 볼 수 있듯이, 화학식 1의 화합물을 처리한 경우, 양성대조군 보다 효과는 적으나, 엘라스타제 활성 저해가 뛰어남을 알 수 있다. 즉, 화학식 1의 화합물은 우수한 엘라스타제 활성 저해효과를 발휘하였다. 따라서, 화학식 1의 화합물은 피부재생, 주름개선을 위한 용도로 사용할 수 있음을 알 수 있었다.
As can be seen from the results in Table 2, when the compound of Chemical Formula 1 was treated, it was found that the effect was less than that of the positive control, but the inhibition of the elastase activity was excellent. That is, the compound of formula (1) exerted a superior inhibitory effect on elastase activity. Therefore, it was found that the compound of Chemical Formula 1 can be used for skin regeneration and wrinkle improvement.
실시예Example 3: 3: 흑화Blackening 효과-멜라닌 총량 증가 효과 Effect - Increase in the total amount of melanin
화학식1의 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 흑화평가를 수행하였다. The compound of Chemical 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) 흡광도로 나타내는 방법으로 측정하였으며, 대조군에 대한 상대적인 멜라닌 총량을 증가율(%)로 계산하고 결과를 표 3에 정리하였다.
The amount of melanin was measured by an absorbance at 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 3.
농도에 따른 세포수준에서의 멜라닌 총량의 증가 효과Increased effect of total melanin level at cell level according to concentration
(abs)Melanin production
(abs)
상기 표 3의 결과에서 볼 수 있듯이, 화학식 1의 화합물은 대조군에 비해서 멜라닌 생성량이 증가하였으며, 농도 증가에 따라 멜라닌 생성율이 증가된다는 것을 확인할 수 있었다. As can be seen from the results of Table 3, it was confirmed that the compound of Chemical Formula 1 increased the amount of melanin production as compared with that of the control, and that the production of melanin increased with increasing concentration.
따라서, 화학식 1의 화합물을 이용하여 흑화 용도로 사용할 수 있음을 알 수 있었다.
Therefore, it was found that the compound of formula (1) can be used for blackening purposes.
실시예Example 4: 4: 항당화Antialcification 효과 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-아지닌(arginine), 1M 포도당을 녹여 준비하고 1M 인산 완충용액을 이용하여 시료를 50, 100ppm이 되도록 희석해서 준비한다. 1M L-아지닌과 1M 인산 완충용액을 1대 4의 비율로 섞은 다음 96-웰플레이트에 80 μl씩 분주한다. 여기에 각각 50, 100ppm으로 희석한 시료와 양성 대조군으로 사용될 0.01M aminoguanidin을 100 μl씩 첨가한다. 이 시료들을 잘 섞어준 다음, 마지막으로 포도당의 최종 농도가 0.1M이 되도록 1M 인산 완충용액으로 희석한 포도당을 넣어 준다. 70℃에서 4시간 동안 반응 시킨다. 96-웰플레이트를 분광 광도계를 이용하여 420 nm에서 흡광도를 측정하여 당화 정도를 측정하였다. First, dissolve 1 M L-arginine and 1 M glucose in 1 M phosphate buffer (pH 7.4) and dilute the sample to 50 and 100 ppm using 1M phosphate buffer solution. Mix 1 M L-arginine and 1 M phosphate buffer at a ratio of 1: 4, and dispense 80 μl each into 96-well plates. Add 100 μl of 0.01 M aminoguanidine to be used as a positive control and a sample diluted to 50 and 100 ppm, respectively. Mix these samples well and then add glucose diluted in 1 M phosphate buffer to a final concentration of 0.1 M glucose. 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-아지닌과 1M 포도당을 넣어 당화를 유발시킨 실험군이며, 시료 자체의 흡광도를 측정하기 위해서 포도당을 넣지 않고 1M L-아지닌과 시료만을 넣어 420 nm에서 흡광도를 측정하였다. 당화 저해 활성은 다음과 같은 식으로 구할 수 있다. Glycation in the following formula was an experimental group in which 1M L-arginine and 1M glucose were added to induce glycation. To measure the absorbance of the sample itself, absorbance was measured at 420 nm by adding 1M L-arginine and sample without glucose Respectively. 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 4의 결과에서 볼 수 있듯이, 화학식1의 화합물은 우수한 항당화 효과를 나타내어 피부 탄력, 주름 개선 효과를 가질 수 있을 것으로 생각된다.As can be seen from the results of Table 4, the compound of Chemical Formula (1) shows excellent antihyperglycosylation effect and can have skin elasticity and wrinkle improving effect.
Claims (5)
[화학식 1]
1. A composition for skin or hair blackening comprising a compound represented by the following formula (1) as an active ingredient.
[Chemical Formula 1]
[화학식 1]
A composition for improving skin elasticity or wrinkle comprising a compound represented by the following formula (1) as an active ingredient.
[Chemical Formula 1]
[화학식 1]
A composition for moisturizing the skin comprising, as an active ingredient, a compound represented by the following formula (1).
[Chemical Formula 1]
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