KR101847013B1 - Composition for enhancing elasticity and whitening - Google Patents
Composition for enhancing elasticity and whitening Download PDFInfo
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- KR101847013B1 KR101847013B1 KR1020120048928A KR20120048928A KR101847013B1 KR 101847013 B1 KR101847013 B1 KR 101847013B1 KR 1020120048928 A KR1020120048928 A KR 1020120048928A KR 20120048928 A KR20120048928 A KR 20120048928A KR 101847013 B1 KR101847013 B1 KR 101847013B1
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- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
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Classifications
-
- 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
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/03—Organic compounds
- A23L29/035—Organic compounds containing oxygen as heteroatom
-
- 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
- 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
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat
Abstract
본 발명은 피부 탄력 증진 및 미백용 조성물에 관한 것이다. 본 발명에 따른 시스타노사이드 A(cistanoside A)는 피부의 섬유아세포의 콜라겐 합성을 촉진하여, 콜라게네이즈 활성 억제함으로써, 피부의 탄력을 향상시키며, 멜라닌 생성을 저해함으로써, 미백 효과를 나타내며, 세포독성 또한 없으므로, 의약품 또는 화장료 조성물 또는 건강식품으로서 사용 가능하다.The present invention relates to a composition for enhancing skin elasticity and whitening. The cystanide A according to the present invention promotes collagen synthesis of fibroblasts of the skin to suppress collagenase activity, thereby enhancing skin elasticity, inhibiting melanin production, exhibiting a whitening effect, Since there is no toxicity, it can be used as a pharmaceutical or cosmetic composition or a health food.
Description
본 발명은 피부 탄력 증진 및 미백용 조성물에 관한 것이다.
The present invention relates to a composition for enhancing skin elasticity and whitening.
콜라겐은 피부의 섬유아세포에서 생성되는 주요 기질 단백질로서 세포 외 간질에 존재하고, 중요한 기능으로는 피부의 기계적 견고성, 결합조직의 저항력과 조직의 결합력, 세포접착의 지탱, 세포분할과 분화(유기체의 성장 혹은 상처 치유 시)의 유도 등이 알려져 있다. 이러한 콜라겐은 연령 및 자외선 조사에 의한 광 노화에 의해 감소하며, 이는 피부의 탄력과 밀접한 연관이 있다고 알려져 있다. 또한, 근래에 들어 피부 노화에 대한 광범위한 연구가 발전 되면서 피부에서의 콜라겐의 중요한 기능이 밝혀지고 있다. Collagen is a major substrate protein produced in fibroblasts of the skin and exists in extracellular epilepsy. Its important functions are mechanical rigidity of skin, resistance of connective tissues and binding force of tissues, support of cell adhesion, division of cells and differentiation Growth or wound healing) are known. Such collagen is reduced by aging and photo aging caused by ultraviolet irradiation, and it is known that it is closely related to elasticity of skin. Also, in recent years, extensive research on skin aging has developed, and important functions of collagen in skin have been revealed.
종래에는 콜라겐의 피부 보습 효과로부터 화장품에 콜라겐을 배합하는 제품들이 출시되어 있으나, 이들 화장품은 콜라겐을 피부 표면에 도포하는 것으로, 고분자인 콜라겐의 경피 흡수에 의한 보습작용을 기대할 수 없으므로 본질적인 피부 기능 개선이라고 말할 수 없다. In the prior art, there have been products that incorporate collagen into cosmetics from the skin moisturizing effect of collagen, but these cosmetics apply collagen to the skin surface, and since the collagen, which is a polymer, can not be expected to be moisturized by transdermal absorption, Can not be said.
한편, 콜라겐 합성 촉진하여 탄력 증진 효과를 나타내는 유효성분들이 알려져 있다. 예를 들어, 레티노산(retinoic acid), TGF(transforming growth factor)[비특허문헌 1], 동물 태반 유래의 단백질[특허문헌 1], 베튤린산(betulinic acid)[특허문헌 2], 클로렐라 추출물[특허문헌 3, 4] 등이 콜라겐 합성 촉진 물질로서 알려져 있다. 그러나, 상기 유효성분들은 피부 적용 시 자극과 발적 등의 안전성의 문제로 사용량의 제한이 있거나, 효과가 미미하여 실질적으로 피부의 콜라겐 합성을 촉진하여 피부 기능을 개선하는 효과를 기대할 수 없는 문제점이 있다. 따라서, 생체에 안전하고, 유효성분이 안정하며, 무엇보다도 기존의 콜라겐 합성 촉진 물질보다 효과가 우수한 탄력 개선 활성을 지닌 성분의 개발이 절실히 요망되고 있다.On the other hand, there have been known effective ingredients exhibiting an effect of promoting collagen synthesis and promoting elasticity. For example, retinoic acid, transforming growth factor (TGF) [non-patent document 1], animal placenta-derived protein [Patent document 1], betulinic acid [Patent document 2], chlorella extract [ Patent Documents 3 and 4] are known as collagen synthesis promoting substances. However, the above-mentioned effective ingredients are limited in the use amount due to safety problems such as irritation and redness when applied to the skin, or have insufficient effect, so that the effect of improving the skin function by promoting the collagen synthesis of the skin can not be expected. Therefore, there is a desperate need to develop a composition that is safe in living body, stable in its effective component, and most effective in improving elasticity, which is more effective than conventional collagen synthesis promoting substances.
또한, 희고 고운 피부를 갖고자 하는 것은 모든 사람의 한결같은 소망이다. 사람의 피부 내 멜라닌(melanin)의 농도와 분포에 따라 유전적으로 결정되나, 태양 자외선이나 피로, 스트레스 등의 환경적 또는 생리적 조건에 의해서도 영향을 받는다. 멜라닌은 아미노산의 일종인 티로신(tyrosine)에 티로시나제(tyrosinase)라는 효소가 작용하여 도파(DOPA), 도파퀴논(dopaquinone)으로 바뀐 후, 비효소적인 산화반응을 거쳐 만들어진다. 이와 같이 멜라닌이 만들어지는 경로는 알려져 있으나, 티로시나제가 작용하는 이전 단계인 멜라닌 합성을 유도하는 메커니즘이 무엇인지에 대해서는 아직도 자세히 밝혀지지 않고 있다. Also, it is the constant desire of everyone to want to have a white, fine skin. It is genetically determined by the concentration and distribution of melanin in human skin, but is also influenced by environmental or physiological conditions such as sunlight, fatigue, and stress. Melanin is produced by a nonenzymatic oxidation reaction after tyrosine tyrosine, which is an amino acid, is converted to DOPA or dopaquinone by an enzyme called tyrosinase. Thus, the pathway through which melanin is made is known, but the mechanism by which melanin synthesis, the previous step in which tyrosinase acts, is not yet elucidated.
한편, 일반적인 알려진 미백 성분으로서, 코지산(Kojic acid), 알부틴(Arbutin) 등과 같은 티로시나제 효소활성을 억제하는 물질, 하이드로퀴논(Hydroquinone), 비타민-C(L-Ascorbic acid) 및 이들의 유도체와 각종 식물 추출물이 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 상기 콜라겐 합성 촉진 물질들과 마찬가지로 피부 적용 시, 자극과 발적 등의 안전성의 문제로 사용량의 제한이 있거나, 효과가 미미하여 실질적인 효과를 기대할 수 없는 문제점이 있다. 따라서, 생체에 안전하고, 유효성분이 안정하며, 무엇보다도 기존의 멜라닌 합성 저해 능력이 우수한 미백 성분의 개발이 절실히 요망되고 있다.
On the other hand, commonly known whitening ingredients include substances inhibiting the activity of tyrosinase enzymes such as kojic acid and arbutin, hydroquinone, vitamin C (L-Ascorbic acid) There are plant extracts. By inhibiting the synthesis of melanin pigment, they can brighten the skin tone to realize skin whitening, and it is possible to improve skin hypercholesterolemia such as stain or freckles due to ultraviolet rays, hormones or heredity. However, as with the collagen synthesis promoting materials, there is a problem in that when the skin is applied, the use amount is limited due to safety problems such as irritation and redness, or the effect is insignificant, so that a substantial effect can not be expected. Therefore, it is urgently required to develop a whitening ingredient which is safe in the living body, stable in its effective ingredient and, above all, excellent in the ability to inhibit melanin synthesis.
[선행문헌] [Prior Art]
[특허문헌][Patent Literature]
일본 특개 평8-231370호 Japan Patent No. 8-231370
일본 특개 평8-208424호Japan Patent No. 8-208424
일본 특개 평9-40523호Japan Patent No. 9-40523
일본 특개 평10-36283호Japan Patent No. 10-36283
[비특허문헌][Non-Patent Document]
Cardinale G. et al, Adv. Enzymol., 41, p. 425, 1974
Cardinale G. et al, Adv. Enzymol., 41, p. 425, 1974
이에, 본 발명자들은 시스타노사이드 A(cistanoside A)가 피부의 섬유아세포의 콜라겐 합성을 촉진하여, 콜라게네이즈 활성을 억제함으로써, 피부의 탄력을 향상시키며, 멜라닌 생성을 저해함으로써, 미백 효과를 나타내는 것을 확인하고 본 발명을 완성하게 되었다.Thus, the present inventors have found that cystanide A promotes collagen synthesis of fibroblasts in skin and inhibits collagenase activity, thereby improving skin elasticity and inhibiting melanin production, thereby exhibiting a whitening effect And finally completed the present invention.
따라서, 본 발명의 목적은 시스타노사이드 A (cistanoside A)를 유효성분으로 함유하는 피부 탄력 증진 및 미백용 조성물을 제공하는데 있다.
Accordingly, an object of the present invention is to provide a skin elasticity-enhancing and whitening composition containing cystanide A as an active ingredient.
상기 과제를 해결하기 위한 수단으로서, 본 발명은As means for solving the above problems,
하기 화학식 1로 표현되는 화합물을 포함하는 피부 탄력 증진 및 미백용 약학적 조성물을 제공한다.There is provided a pharmaceutical composition for skin elasticity enhancement and whitening comprising a compound represented by the following formula (1).
[화학식 1][Chemical Formula 1]
상기 과제를 해결하기 위한 다른 수단으로서, 본 발명은 As another means for solving the above problems,
상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 피부 외용제를 제공한다.
The present invention provides a skin external preparation for enhancing skin elasticity and whitening comprising the compound of formula (1).
상기 과제를 해결하기 위한 또 다른 수단으로서, 본 발명은 상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 화장료 조성물을 제공한다.
As another means for solving the above problems, the present invention provides a cosmetic composition for skin elasticity enhancement and whitening comprising the compound of formula (1).
상기 과제를 해결하기 위한 또 다른 수단으로서, 본 발명은 상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 건강식품을 제공한다.
As another means for solving the above-mentioned problems, the present invention provides a skin health enhancing and whitening health food containing the compound of formula (1).
본 발명에 따른 시스타노사이드 A(cistanoside A)는 피부의 섬유아세포의 콜라겐 합성을 촉진하여, 콜라게네이즈의 활성을 억제함으로써, 피부의 탄력을 향상시키며, 멜라닌 생성을 저해함으로써, 미백 효과를 나타내며, 또한 세포독성이 없어 부작용없이 의약품 또는 화장료 또는 건강식품에 사용할 수 있다.
The cystanide A according to the present invention promotes collagen synthesis of the fibroblasts of the skin to inhibit collagenase activity, thereby improving skin elasticity and inhibiting melanin production, thereby exhibiting a whitening effect , And is also cytotoxic and can be used in medicines, cosmetics or health food without side effects.
이하, 본 발명의 구성을 구체적으로 설명한다.Hereinafter, the configuration of the present invention will be described in detail.
피부 탄력 증진 및 미백 성분이 실제 피부에 적용 시 우수한 효과를 발휘하기 위해서는 저농도에서 고활성의 탄력 증진 및 미백 활성을 나타내고, 피부를 투과하여 흡수되는 능력이 우수하고, 피부 탄력 증진 및 미백 효과를 나타내기에 충분한 시간 동안 머무를 수 있도록 휘발성이 낮고, 조성물이나 피부 상에서 활성 성분이 안정하게 유지되고, 의약이나 화장품으로의 제형화가 용이하며, 또한 피부에 안전한 것이 바람직하다. 그러나 공지의 피부 탄력 증진 및 미백 효과 개선 성분 중 상기 특성을 모두 만족시키는 성분은 흔치 않다. 예를 들어, 몇몇 피부 탄력 증진 및 미백 성분들은 시험관 내 실험 시 저농도에서도 피부 탄력 증진 및 미백 활성은 우수하나, 피부를 투과하여 흡수되는 능력이 떨어져 실제 피부에 적용하기엔 어렵다. 또 다른 피부 탄력 증진 및 미백 성분들은 친수성이 낮아 의약이나 화장품으로 제형화가 어렵다. 또한, 몇몇 피부 탄력 증진 및 미백 효과 성분들은 열, 빛, 또는 산소에 노출되었을 때 성분이 분해되거나 다른 화합물로 변형되어 피부에 적용하기 전에 이미 피부 탄력 증진 및 미백 효과가 사라지는 경우도 있다.In order to exert an excellent effect when the skin elasticity enhancement and whitening ingredient is applied to the actual skin, it exhibits a high activity of elasticity enhancement and whitening activity at a low concentration, has excellent ability to permeate and absorb the skin, exhibits skin elasticity enhancement and whitening effect It is preferable that the composition is low in volatility so that it can stay for a sufficient period of time, the active ingredient remains stable on the composition or on the skin, is easily formulated into medicines or cosmetics, and is safe for the skin. However, among the components for improving the skin elasticity and improving the whitening effect, there are not many components satisfying all of the above characteristics. For example, some skin elasticity enhancement and whitening ingredients are excellent in improving skin elasticity and whitening activity even at a low concentration in an in vitro test, but they are difficult to be applied to real skin because of their ability to be absorbed through the skin. Other skin elasticity enhancement and whitening ingredients have low hydrophilicity and are difficult to formulate into medicines or cosmetics. In addition, some skin elasticity enhancing and whitening effect ingredients may be decomposed or transformed into other compounds when exposed to heat, light, or oxygen, and the skin elasticity enhancement and whitening effect may already be lost before application to the skin.
하기 실시예에서 확인할 수 있는 바와 같이, 시스타노사이드 A(cistanoside A)는 저농도에서 우수한 효과를 나타내므로, 피부 탄력 증진 및 미백을 위한 의약품 또는 화장료 또는 건강식품 등의 유효성분으로 이용될 수 있다. As can be seen in the following examples, cistanoside A exhibits excellent effects at a low concentration, and thus can be used as an effective ingredient for medicines, cosmetics or health food for skin elasticity enhancement and whitening.
따라서, 본 발명은 하기 화학식 1로 표현되는 화합물을 포함하는 피부 탄력 증진 및 미백을 위한 약학적 조성물 또는 피부 외용제 또는 화장료 조성물 또는 건강식품을 제공한다 :Accordingly, the present invention provides a pharmaceutical composition, skin external preparation, cosmetic composition or health food for skin elasticity enhancement and whitening comprising a compound represented by the following formula 1:
[화학식 1][Chemical Formula 1]
상기 화학식 1의 화합물은 합성하여 이용하거나, 시판되고 있는 화합물을 이용할 수 있다.
The compound of formula (1) may be synthesized or a commercially available compound may be used.
본 발명에 따른 구체적인 예로, 본 발명은 상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 약학적 조성물을 제공한다. As a specific example according to the present invention, the present invention provides a pharmaceutical composition for skin elasticity enhancement and whitening comprising the compound of formula (1).
본 발명의 피부 탄력 증진 및 미백용 약학적 조성물은 상기 화학식 1의 화합물의 약제학적으로 허용 가능한 염을 포함할 수 있다.The pharmaceutical composition for skin elasticity enhancement and whitening of the present invention may include a pharmaceutically acceptable salt of the compound of the formula (1).
상기 화학식 1의 화합물의 약제학적으로 허용 가능한 염은 유기산 또는 무기산을 이용하여 형성된 산 부가염일 수 있으며, 상기 유기산은, 예를 들면 포름산, 아세트산, 프로피온산, 락트산, 부티르산, 이소부티르산, 트리플루오로아세트산, 말산, 말레산, 말론산, 푸마르산, 숙신산, 숙신산 모노아미드, 글루탐산, 타르타르산, 옥살산, 시트르산, 글리콜산, 글루쿠론산, 아스코르브산, 벤조산, 프탈산, 살리실산, 안트라닐산, 디클로로아세트산, 아미노옥시 아세트산, 벤젠술폰산, p-톨루엔술폰산 및 메탄술폰산계 염을 포함하며 무기산은 예를 들면 염산, 브롬산, 황산, 인산, 질산, 탄산 및 붕산계 염을 포함한다. 바람직하게는 염산염 또는 아세트산염 형태일 수 있으며, 보다 바람직하게는 염산염 형태일 수 있다.The pharmaceutically acceptable salt of the compound of Formula 1 may be an acid addition salt formed using an organic acid or an inorganic acid, and the organic acid may be, for example, formic acid, acetic acid, propionic acid, lactic acid, butyric acid, isobutyric acid, trifluoroacetic acid The organic acid may be selected from the group consisting of hydrochloric acid, hydrobromic acid, hydrochloric acid, hydrobromic acid, hydrobromic acid, hydrobromic acid, hydrobromic acid, hydrobromic acid, malic acid, maleic acid, malonic acid, fumaric acid, succinic acid, monoamide, glutamic acid, tartaric acid, oxalic acid, citric acid, glycolic acid, glucuronic acid, , Benzenesulfonic acid, p-toluenesulfonic acid and methanesulfonic acid-based salts, and the inorganic acid includes, for example, hydrochloric acid, bromic acid, sulfuric acid, phosphoric acid, nitric acid, carbonic acid and boric acid-based salts. Preferably in the hydrochloride or acetate form, more preferably in the hydrochloride form.
상기 언급된 산 부가염은 a) 상기 화학식 1의 화합물 및 산을 직접 혼합하거나, b) 이들 중 한 가지를 용매 또는 함수 용매 중에 용해시키고 혼합시키거나, 또는 c) 화학식 1의 화합물을 용매 또는 수하 용매 중의 산에 위치시키고 이들을 혼합하는 일반적인 염 제조방법으로 제조된다.The above-mentioned acid addition salts may be obtained by a) directly mixing the compound of formula 1 and an acid, or b) dissolving and mixing one of them in a solvent or a water solvent, or c) Lt; RTI ID = 0.0 > acid < / RTI > in a solvent and mixing them.
위와는 별도로 추가적으로 염이 가능한 형태는 가바염, 가바펜틴염, 프레가발린염, 니코틴산염, 아디페이트염, 헤미말론산염, 시스테인염, 아세틸시스테인염, 메티오닌염, 아르기닌염, 라이신염, 오르니틴염, 아스파르트산염 등이 있다. In addition to the above, additionally saltable forms include, but are not limited to, the salts of gabapentin, pregabalin, nicotinate, adipate, hemimarate, cysteine, acetylcysteine, methionine, arginine, Aspartate and the like.
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 탄력 증진 및 미백 성분을 포함할 수 있을 것이다. 추가적인 피부 주름 개선 성분, 탄력 증진 성분, 미백 성분을 포함하게 되면 본 발명의 조성물의 주름 개선, 탄력 증진, 미백 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 주름 및 탄력 개선 성분으로서, 레티노산, TGF, 동물 태반 유래의 단백질, 베튤린산 및 클로렐라 추출물, 당업계에 공지된 미백 성분으로서, 코지산(Kojic acid), 알부틴(Arbutin) 등과 같은 티로시나제 효소활성을 억제하는 물질, 하이드로퀴논(Hydroquinone), 비타민-C(L-Ascorbic acid) 및 이들의 유도체와 각종 식물 추출물로 구성되는 군으로부터 선택되는 1종 또는 2종 이상의 성분을 추가로 포함할 수 있다. 추가된 피부 탄력 증진 및 미백 성분은 전체 조성물 중량에 대하여 0.0001 중량% 내지 10 중량%로 포함될 수 있을 것이며, 상기 함량 범위는 콜라겐 합성 촉진 활성, 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 enhancement and whitening ingredients. When the skin wrinkle improving component, the elasticity improving component, and the whitening component are included, the wrinkle improvement, the elasticity enhancement, and the whitening effect of the composition of the present invention may be further enhanced. 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 comprises retinoic acid, TGF, proteins from animal placenta, betulinic acid and chlorella extract, whitening ingredients known in the art, as wrinkle and elasticity improving ingredients known in the art, (Hydroquinone), vitamin C (L-ascorbic acid), derivatives thereof, and various plant extracts, which are effective to inhibit tyrosinase enzyme activity such as kojic acid and arbutin One or more components may be further included. The added skin elasticity enhancement and whitening component may be included in an amount of 0.0001% by weight to 10% by weight with respect to the weight of the whole composition, and the content ranges include collagen synthesis promoting activity, skin safety, ease of formulation of the compound of Formula 1 And the like.
또한, 본 발명의 피부 탄력 증진 및 미백용 약학적 조성물은 약학적으로 허용 가능한 담체를 더 포함할 수 있다. In addition, the pharmaceutical composition for skin elasticity enhancement and whitening of the present invention may further comprise a pharmaceutically acceptable carrier.
약학적으로 허용되는 담체는 완충액, 주사용 멸균수, 일반 식염수 또는 인산염 완충 식염수, 슈크로스, 히스티딘, 염 및 폴리솔베이트 등과 같은 여러 성분을 함유할 수 있다.Pharmaceutically acceptable carriers may contain a variety of ingredients such as buffer, injectable sterile water, normal saline or phosphate buffered saline, sucrose, histidine, salts and polysorbates.
본 발명의 약학적 조성물은 경구 또는 비경구로 투여할 수 있으며, 일반 의약품 제제의 형태, 예를 들어, 임상 투여 시 경구 및 비경구의 여러 가지 제형으로 투여될 수 있는데, 제제화할 경우에는 보통 사용하는 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제될 수 있다. The pharmaceutical composition of the present invention can be administered orally or parenterally, and can be administered in the form of a general pharmaceutical preparation, for example, various forms of oral and parenteral administration at the time of clinical administration. In the case of formulation, , An extender, a binder, a wetting agent, a disintegrant, a surfactant, and the like.
경구투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 본 발명의 약학적 조성물에 적어도 하나 이상의 부형제 예를 들면, 전분, 칼슘카보네이트(Calcium carbonate), 수크로스(Sucrose) 또는 락토오스(Lactose), 젤라틴 등을 섞어 조제될 수 있다. Solid formulations for oral administration include tablets, pills, powders, granules, capsules and the like, which may be prepared by mixing the pharmaceutical composition of the present invention with at least one excipient such as starch, calcium carbonate, Sucrose, lactose, gelatin, and the like.
단순한 부형제 이외에 마그네슘 스티레이트 탈크 같은 윤활제들도 사용된다. 경구를 위한 액상 제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순희석제인 물, 리퀴드 파라핀 이외에 여러가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다. In addition to simple excipients, lubricants such as magnesium stearate talc are also used. Examples of liquid formulations 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.
비경구 투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조제제, 좌제가 포함된다. 비수성용제, 현탁용제로는 프로필렌 글리콜(Propylene glycol), 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다. 좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈(tween) 61, 카카오지, 라우린지, 글리세로제라틴 등이 사용될 수 있다.Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like can be used as the non-aqueous solvent and suspension agent. As a base for suppositories, witepsol, macrogol, tween 61, cacao paper, laurin, glycerogelatin and the like can be used.
본 발명에 있어서, '탄력 증진'이라 함은 늘어진 피부조직을 수축시키는 효과와 더불어 새로운 콜라겐을 생성시켜 저하된 피부 탄력을 되찾는 것을 말한다.In the present invention, the term 'elasticity enhancement' refers to the effect of shrinking the elongated skin tissue, as well as the generation of new collagen to restore the reduced elasticity of the skin.
본 발명에 있어서, '미백 효과'라 함은 멜라닌 색소의 합성을 저해함으로써 피부 톤을 밝게 할 뿐만 아니라, 자외선, 호르몬 또는 유전에 기인한 기미나 주근깨 등의 피부 과색소 침착을 개선하는 것을 말한다. In the present invention, the 'whitening effect' refers to not only brightening the skin tone by inhibiting the synthesis of the melanin pigment but also improving skin hypercholesterolemia due to ultraviolet rays, hormones or heredity, such as spots or freckles.
본 발명의 약학적 조성물은 유효량의 상기 화학식 1의 화합물을 포함할 때 바람직한 탄력 증진 및 미백 효과를 제공할 수 있다. 본 발명에 있어서, '유효량'이라 함은 새로운 콜라겐을 생성시켜, 피부 탄력 증진 및 미백 효능을 나타낼 수 있는 화합물의 양을 의미한다. 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 주름 생성, 탄력 감소, 기미, 주근깨 등에 따른 피부과적 치료를 위한 의약품으로 제품화되는 경우에는 일상적으로 피부에 적용하게 되는 화장품으로 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 pharmaceutical composition of the present invention can provide the desired elasticity enhancement and whitening effect when an effective amount of the compound of Formula 1 is included. In the present invention, the term "effective amount" means the amount of a compound capable of producing new collagen and showing skin elasticity and whitening effect. 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 medicament for dermatological treatment based on wrinkle formation, reduction in elasticity, spots, freckles, and the like, when it is commercialized as a cosmetic product that is routinely applied to skin, The compound of the formula (1) may be contained at a higher concentration than that of the compound of the formula (1). 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) Can be administered 6 times
본 발명의 약학적 조성물은 단독으로, 또는 수술, 방사선 치료, 호르몬 치료, 화학 치료 및 생물학적 반응 조절제를 사용하는 방법들과 병용하여 사용할 수 있다.
The pharmaceutical composition of the present invention can be used alone or in combination with methods using surgery, radiation therapy, hormone therapy, chemotherapy, and biological response modifiers.
본 발명에 따른 구체적인 예로, 본 발명은 상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 피부 외용제를 제공한다. As a specific example according to the present invention, the present invention provides an external skin preparation for enhancing skin elasticity and whitening comprising the compound of formula (1).
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.
이에 제한되는 것은 아니나, 본 발명의 한 구체예에서, 상기 조성물은 상기 화학식 1의 화합물을 전체 조성물 중량에 대하여 0.0001 중량% 내지 10 중량%, 보다 구체적으로 0.001 중량% 내지 1 중량%로 포함할 수 있다. 본 발명의 조성물이 상기 화학식 1의 화합물을 0.0001 중량% 미만으로 포함할 경우에는 충분한 피부탄력 증진 및 미백 효과를 기대할 수 없고, 10 중량%를 초과하여 포함할 경우에는 알러지 등 원치 않는 반응이 발생하거나 피부 안전성에 문제가 있을 수 있으므로 이를 방지하기 위한 것이다. In one embodiment of the present invention, but not limited thereto, the composition may comprise from 0.0001% to 10%, more specifically from 0.001% to 1% by weight of the compound of Formula 1, have. When the composition of the present invention contains less than 0.0001% by weight of the compound of formula (I), sufficient skin elasticity and whitening effect can not be expected. When the composition contains more than 10% by weight, This is to prevent skin safety problems.
또한 상기 화학식 1의 화합물을 피부 외용제로 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, 금속이온 봉쇄제 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 contain at least one selected from the group consisting of fatty substances, organic solvents, solubilizers, thickening and gelling agents, softening agents, antioxidants, suspending agents, stabilizers, foaming agents, A preservative, a vitamin, a blocking agent, a wetting agent, a essential oil, a dye, a pigment, a hydrophilic or lipophilic active agent, a lipid vesicle or a skin external preparation for oral administration in the form of an active agent, water, ionic or nonionic emulsifier, filler, sequestering agent and chelating agent And may contain adjuvants conventionally used in the field of dermatology, such as any other ingredient commonly used. The components can also be introduced in amounts commonly used in the field of dermatology.
본 발명에 따른 구체적인 예로, 본 발명은 상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 화장료 조성물을 제공한다. As a specific example according to the present invention, the present invention provides a cosmetic composition for skin elasticity enhancement and whitening comprising the compound of formula (1).
상기 화학식 1의 화합물을 화장품으로 사용하는 경우, 상기 화학식 1의 화합물을 유효성분으로 함유하여 제조되는 화장품은 일반적인 유화 제형 및 가용화 제형의 형태로 제조할 수 있다. 예컨대, 유연 화장수 또는 영양 화장수 등과 같은 화장수, 훼이셜 로션, 바디로션 등과 같은 유액, 영양 크림, 수분 크림, 아이 크림 등과 같은 크림, 에센스, 화장연고, 스프레이, 젤, 팩, 선 스크린, 메이크업 베이스, 액체 타입, 고체 타입 또는 스프레이 타입 등의 파운데이션, 파우더, 클렌징 크림, 클렌징 로션, 클렌징 오일과 같은 메이크업 제거제, 클렌징 폼, 비누, 바디 워쉬 등과 같은 세정제 등의 제형을 가질 수 있다. When the compound of Chemical Formula 1 is used as a cosmetic, the cosmetic product containing the compound of Chemical Formula 1 as an active ingredient may be prepared in the form of a general emulsified formulation and a solubilized formulation. For example, creams, essences, cosmetic creams, sprays, gels, packs, sunscreens, make-up bases, liquids such as lotions such as lotion, facial lotion, body lotion, A powder, a cleansing lotion, a makeup removing agent such as a cleansing oil, a cleaning agent such as a cleansing foam, a soap, a body wash and the like.
또한, 상기 화장료는 상기 화학식 1의 화합물에 추가로 화장료 조성물에 통상적으로 사용되는 안정화제, 용해화제, 비타민, 안료 또는 향료 등의 보조제 및 담체를 추가로 포함할 수 있다. 예컨대, 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 화장품에 통상적으로 사용되는 임의의 다른 성분과 같은 화장품학 분야에서 통상적으로 사용되는 보조제를 함유할 수 있다.In addition to the compound of Formula 1, the cosmetic composition may further comprise an auxiliary agent such as a stabilizer, a solubilizing agent, a vitamin, a pigment or a flavoring agent and a carrier which are commonly used in cosmetic compositions. For example, it is also possible to use other additives such as fatty substances, organic solvents, solubilizers, thickeners and gelling agents, softeners, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water, ionic or nonionic emulsifiers, In the cosmetology field, such as metal ion sequestrants and chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or any other ingredient commonly used in cosmetics And may contain auxiliary agents used.
상기 화학식 1의 화합물은 화장품으로 제품화되는 경우에 유효성분이 단기간 내에 피부에 머무르게 되는 메이크업 제거제, 세정제 등과 같은 워시-오프(wash-off) 타입의 화장품의 경우에는 비교적 높은 농도의 상기 화학식 1을 포함할 수 있을 것이다. 반면, 유효성분이 장기간 동안 피부에 머무르게 되는 화장수, 유액, 크림, 에센스 등의 리브-온(leave-on) 타입의 화장품의 경우에는 워시-오프 타입의 화장품에 비해 낮은 농도의 시스타노사이드 A(cistanoside A)를 포함해도 무방할 것이다. 이에 제한되는 것은 아니나, 본 발명의 한 구체예에서, 상기 조성물은 상기 화학식 1의 화합물을 전체 조성물 중량에 대하여 0.0001 중량% 내지 10 중량%, 보다 구체적으로 0.001 중량% 내지 1 중량%)로 포함할 수 있다. 본 발명의 조성물이 상기 화학식 1의 화합물을 0.0001 중량% 미만으로 포함할 경우에는 충분한 미백 효과를 기대할 수 없고, 10 중량%를 초과하여 포함할 경우에는 알러지 등 원치 않는 반응이 발생하거나 피부 안전성에 문제가 있을 수 있으므로 이를 방지하기 위한 것이다.
In the case of a wash-off type cosmetic such as a make-up remover, a detergent, etc., in which the active ingredient remains on the skin in a short period of time when the cosmetic product is commercialized, the compound of formula (1) It will be possible. On the other hand, in the case of leave-on type cosmetics such as lotion, cream, essence and the like in which the active ingredient remains on the skin for a long period of time, a lower concentration of cistanoside A than that of the wash- A) may be included. In one embodiment of the present invention, but not limited thereto, the composition comprises the compound of Formula 1 in an amount of 0.0001 wt% to 10 wt%, more specifically 0.001 wt% to 1 wt% based on the total weight of the composition . When the composition of the present invention contains less than 0.0001 wt% of the compound of the present invention, a sufficient whitening effect can not be expected. When the composition of the present invention is contained in an amount exceeding 10 wt%, undesired reactions such as allergy occur, To prevent this.
본 발명은 또한 상기 화학식 1의 화합물을 포함하는 피부 탄력 증진 및 미백용 건강식품에 관한 것이다.The present invention also relates to a skin elasticity enhancing and whitening health food 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.Herein, the term "health food" 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.
이와 같이 하여 얻어지는 본 발명의 건강식품은, 일상적으로 섭취하는 것이 가능하기 때문에 높은 피부 주름 개선 및 탄력 증진 효과를 기대할 수 있어 매우 유용하다.Since the health food of the present invention thus obtained can be ingested on a daily basis, it can be expected to have a high skin wrinkle improvement and an elasticity increasing effect, which is very useful.
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. 이에 제한되는 것은 아니나, 본 발명의 한 구체예에서, 상기 건강식품은 상기 화학식 1의 화합물을 전체 조성물 중량에 대하여 0.0001 중량% 내지 10 중량%, 보다 구체적으로 0.001 중량% 내지 1 중량%로 포함할 수 있다. 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. 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). In one embodiment of the present invention, the health food contains 0.0001 wt% to 10 wt%, more specifically 0.001 wt% to 1 wt% of the compound of Formula 1 based on the total composition weight . 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 .
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.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.
본 발명의 건강음료는 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상술한 천연 탄수화물은 포도당, 과당과 같은 모노사카라이드; 말토오스, 슈크로오스와 같은 이당류; 덱스트린, 사이클로덱스트린과 같은 다당류; 또는 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 건강음료 100 mL 당 일반적으로 약 0.01 ∼ 0.04 g, 바람직하게는 약 0.02 ∼ 0.03 g 이다.The health drink of the present invention may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages. The above-mentioned natural carbohydrates include monosaccharides such as glucose and fructose; Disaccharides such as maltose and sucrose; Polysaccharides such as dextrin, cyclodextrin; Or 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 health drink of the present invention.
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. 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.
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 건강식품 100 중량부당 0.01 ~ 0.1 중량부의 범위에서 선택되는 것이 일반적이다.
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 health food of the present invention.
이하, 본 발명을 실시예에 의해 상세히 설명한다. 단, 하기 실시예는 본 발명을 예시하는 것일 뿐, 본 발명의 내용이 하기 실시예에 한정되는 것은 아니다.
Hereinafter, the present invention will be described in detail with reference to examples. However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples.
<< 참조예Reference Example 1> 1> 화학식1의(1) 화합물의 정보 Compound information
b-D-Glucopyranoside,2-(4-hydroxy-3-methoxyphenyl)ethyl O-6-deoxy-a-L-mannopyranosyl-(1®3)-O-[b-D-glucopyranosyl-(1®6]-, 4-[(2E)-3-(3,4-dihydroxyphenyl)-2-propenoatebD-Glucopyranoside, 2- (4-hydroxy-3-methoxyphenyl) ethyl O-6-deoxy-aL-mannopyranosyl- (1R3) 2E) -3- (3,4-dihydroxyphenyl) -2-propenoate
CAS No.: 93236-42-1CAS No .: 93236-42-1
구입처: alibaba Where to buy: alibaba
기원식물: Cistanche deserticola
Origin Plants: Cistanche deserticola
실시예Example 1: 콜라겐 합성 효과 1: Collagen synthesis effect
하기 표 1의 물질을 인간 유래 섬유아세포의 배양액에 첨가하여 세포수준에서 콜라겐 합성 촉진 효과를 실험하였다. The substances of Table 1 below were added to the culture medium of human-derived fibroblasts to examine the promoting effect of collagen synthesis at the cellular level.
합성된 콜라겐의 측정은 PICP EIA kit(Procollagen Type I C-Peptide Enzyme ImmunoAssay KIT)를 이용하여 정량하였다. The synthesized collagen was quantitated using a PICP EIA kit (Procollagen Type I C-Peptide Enzyme Immunoassay Kit).
실험 전 인간 유래 섬유아세포를 대상으로 실험물질의 농도 10ppm, 1ppm, 0.1ppm, 0.01ppm, 0.001ppm에서 세포독성을 평가(섬유아세포를 배양하여 MTT시험을 하는 방법[참고문헌: Mossman T. (1983). Rapid Colorimetric Assay for Cellular Growth & Survival: application to proliferation & cytotoxicity assays. Journal of Immunological Methods 65, 55-63])하였으며, 전 농도에서 세포 독성은 나타나지 않았다.The cytotoxicity of human fibroblasts before the experiment was evaluated at concentrations of 10 ppm, 1 ppm, 0.1 ppm, 0.01 ppm, and 0.001 ppm of the test substance (method for MTT test by culturing fibroblasts [Reference: Mossman T. ) Rapid Colorimetric Assay for Cellular Growth & Survival: Application to proliferation & cytotoxicity assays. Journal of Immunological Methods 65, 55-63).
실험에서 시스타노사이드 A의 최종 농도는 1 ppm 및 10 ppm 으로 하였으며, 각각의 시료는 인간 섬유아 세포의 배양배지에 첨가하여 1일간 배양한 후, 배양액을 취하여 PICP EIA 키트로 각 농도에서의 콜라겐 합성 정도를 분광광도계를 이용하여 450 nm에서 측정하였다. 효과의 비교를 위하여 아무것도 첨가하지 않은 섬유아세포의 배양 배지(대조군)와 비타민 C를 최종 농도 52.8 ㎍/ml가 되도록 첨가한 시료에 대하여 동일한 방법으로 콜라겐 합성 정도를 측정하였다. 콜라겐 생성량은 UV 흡광도로서 측정하였으며, 콜라겐 생성 증가율은 대조군에 대한 상대적인 콜라겐 생성량 비율로 계산하고, 그 결과를 하기 표 1에 정리하였다.In the experiment, the final concentrations of Sistanoside A were 1 ppm and 10 ppm. Each sample was added to the culture medium of human fibroblasts and cultured for 1 day. Then, the culture broth was taken and the collagen The degree of synthesis was measured at 450 nm using a spectrophotometer. For the comparison of the effects, the degree of collagen synthesis was measured by the same method for the culture medium of fibroblasts (control group) to which nothing had been added and the sample added with vitamin C to a final concentration of 52.8 / / ml. The amount of collagen production was measured as the UV absorbance, and the increase rate of collagen production was calculated as a relative ratio of collagen production to the control. The results are summarized in Table 1 below.
시료
sample
흡광도
Absorbance
10 ppmSystanoside A
10 ppm
436.9
436.9
252.5
252.5
1 ppmSystanoside A
1 ppm
333.3
333.3
192.7
192.7
(52.8 ㎍/ml)Vitamin C
(52.8 [mu] g / ml)
221.4
221.4
128.0
128.0
상기 표 1의 결과에서 볼 수 있듯이, 시스타노사이드 A(cistanoside A)는 일반적으로 콜라겐 합성 능력이 있는 것으로 알려진 비타민 C를 적용한 경우보다 적은 농도로 더 우수한 콜라겐 합성 효과를 발휘하였다.
As can be seen from the results of Table 1, cysteinoside A exhibited better collagen synthesis effect at a lower concentration than that of vitamin C, which is generally known to have ability to synthesize collagen.
실시예Example 2: 미백 효과 실험 2: Whitening effect experiment
멜라닌 생성 저해 효과 확인Confirmation of inhibition of melanin formation
화학식1의 화합물을 쥐의 멜라노마 세포(B-16 mouse melanoma cell)의 배양액에 첨가하여 세포 수준에서의 미백 효과를 실험하였다. (Lotan R., Lotan D. Cancer Res. 40:3345-3350, 1980).The compound of Chemical Formula 1 was added to the culture solution of mouse melanoma cell of B-16 mouse to test the whitening effect at the cellular level. (Lotan R., Lotan D. Cancer Res. 40: 3345-3350, 1980).
실험 전 쥐의 멜라노마 세포에 대하여 독성을 평가하여 독성이 없는 농도를 선정하여 미백평가를 수행하였다.To evaluate the toxicity of melanoma cells in rats before the experiment, whitening evaluation was performed by selecting a concentration that is not toxic.
화학식1의 화합물을 배양액에 최종농도가 0.01ug/ml, 0.1ug/ml, 1ug/ml, 10ug/ml이 되도록 하여 실험하였으며, 대조군인 알부틴은 200ug/ml가 되도록 배지에 첨가하여 각각 B-16 멜라노마 세포에 처리하여 3일간 배양하였다. The compound of Chemical Formula 1 was added to the culture medium to a final concentration of 0.01 μg / ml, 0.1 μg / ml, 1 μg / ml and 10 μg / ml, and the control group, arbutin, Melanoma cells and cultured for 3 days.
이후, 세포들을 트립신(trypsin) 처리하여 배양용기로부터 떼어내 원심분리 한 후 멜라닌을 추출하였다. 떼어 낸 세포는 수산화 나트륨 용액(1N농도) 1ml를 가하여 10분간 끓여 멜라닌을 녹이고 분광 광도계를 이용하여, 400나노미터(nm)에서 흡광도를 측정하여 생성된 멜라닌의 양을 측정하였다. Cells were then trypsinized, detached from the culture, centrifuged, and extracted with melanin. The removed cells were melted with 1 ml of sodium hydroxide solution (1N concentration), boiled for 10 minutes, melanin was dissolved, and the amount of melanin produced by measuring the absorbance at 400 nanometers (nm) was measured using a spectrophotometer.
상기 멜라닌 양은 단위 세포수당(106 cell)의 흡광도로 나타내는 방법으로 측정하였으며, 대조군에 대한 상대적인 멜라닌 생성량을 저해율(%)로 계산하고 결과를 표 2에 정리하였다. 또한, 실험은 3번 반복된 것이다.
The amount of melanin was measured by the absorbance of 10 6 cells per unit cell, and the amount of melanin produced relative to the control group was calculated as the inhibition rate (%). The results are summarized in Table 2. The experiment was repeated three times.
표 2의 결과에서 볼 수 있듯이, 화학식1의 화합물은 기존에 알려진 미백 물질인 알부틴(Arbutin)과 비교할 때 배양된 쥐의 멜라노마 세포에 대하여 월등히 우수한 멜라닌 생성 억제능이 있음을 알 수 있다.
As can be seen from the results in Table 2, the compound of formula (I) has remarkably superior inhibitory effect on melanin formation in rat melanoma cells cultured in comparison with the known whitening substance arbutin (Arbutin).
제제예Formulation example 1: 약학적 제제의 제조 1: Preparation of pharmaceutical preparations
1. 산제의 제조1. Manufacturing of powder
화학식 1의 화합물 0.001g0.001 g of the compound of formula (1)
유당 1g Lactose 1g
상기의 성분을 혼합하고 기밀포에 충진하여 산제를 제조하였다.
The above components were mixed and packed in airtight bags to prepare powders.
2. 정제의 제조2. Preparation of tablets
화학식 1의 화합물 0.2㎎0.2 mg of the compound of formula (1)
옥수수전분 100㎎100 mg of corn starch
유 당 100㎎100 mg of milk
스테아린산Stearic acid 마그네슘 2㎎ Magnesium 2 mg
상기의 성분을 혼합한 후, 통상의 정제의 제조방법에 따라서 타정하여 정제를 제조하였다.
After mixing the above components, tablets were prepared by tableting according to a conventional method for producing tablets.
3. 캡슐제의 제조3. Preparation of capsules
화학식 1의 화합물 0.2㎎0.2 mg of the compound of formula (1)
옥수수전분 100㎎100 mg of corn starch
유 당 100㎎100 mg of milk
스테아린산Stearic acid 마그네슘 2㎎ Magnesium 2 mg
상기의 성분을 혼합한 후, 통상의 캡슐제의 제조방법에 따라서 젤라틴 캡슐에 충전하여 캡슐제를 제조하였다.
After mixing the above components, the capsules were filled in gelatin capsules according to the conventional preparation method of capsules.
4. 환의 제조4. Manufacture of rings
화학식 1의 화합물 0.003 g0.003 g of the compound of formula (1)
유당 1.5 gLactose 1.5 g
글리세린 1 gGlycerin 1 g
자일리톨Xylitol 0.5 g 0.5 g
상기의 성분을 혼합한 후, 통상의 방법에 따라 1 환 당 4 g이 되도록 제조하였다.
After mixing the above components, they were prepared so as to be 4 g per one ring according to a conventional method.
5. 과립의 제조5. Manufacture of granules
화학식 1의 화합물 2 ㎎2 mg of the compound of formula (1)
대두 추출물 50 ㎎Soybean extract 50 mg
포도당 200 ㎎200 mg of glucose
전분 600 ㎎ 600 mg of starch
상기의 성분을 혼합한 후, 30% 에탄올 100 ㎎을 첨가하여 60℃에서 건조하여 과립을 형성한 후 포에 충진하였다.
After mixing the above components, 100 mg of 30% ethanol was added and dried at 60 캜 to form granules, which were then filled in a capsule.
제제예Formulation example 2: 화장품의 제조 2: Manufacture of cosmetics
1. 유연화장수(스킨로션)의 제조1. Manufacture of softening longevity (skin lotion)
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 유연화장수를 통상의 방법에 따라 제조하였다.As the following composition, the number of softening times containing the compound of formula (1) as an active ingredient was prepared according to a conventional method.
화학식 1의 화합물 0.1 중량％0.1% by weight of the compound of formula (1)
베타-1,3-글루칸 1.0 중량％Beta-1,3-glucan 1.0 wt%
부틸렌글리콜 2.0 중량％Butylene glycol 2.0 wt%
프로필렌글리콜 2.0 중량％Propylene glycol 2.0 wt%
카르복시비닐폴리머 0.1 중량％Carboxyvinyl polymer 0.1 wt%
피이지-12 노닐페닐에테르 0.2 중량％0.2% by weight of phage-12 nonylphenyl ether
폴리솔베이트80 0.4 중량％Polysorbate 80 0.4 wt%
에탄올 10.0 중량％Ethanol 10.0 wt%
트리에탄올아민 0.1 중량％0.1% by weight triethanolamine
방부제 0.05 중량％Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량％
Purified water to 100%
2. 영양화장수(밀크로션)의 제조2. Manufacture of nutrition lotion (milk lotion)
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 영양화장수를 통상의 방법에 따라 제조하였다.As in the following composition, a nutritional lotion containing the compound of the formula (1) as an active ingredient was prepared by a conventional method.
화학식 1의 화합물 0.1 중량％0.1% by weight of the compound of formula (1)
베타-1,3-글루칸 1.0 중량％Beta-1,3-glucan 1.0 wt%
밀납 4.0 중량％4.0 wt%
폴리솔베이트60 1.5 중량％Polysorbate 60 1.5 wt%
솔비탄세스퀴올레이트 1.5 중량％1.5% by weight of sorbitan sesquioleate
유동파라핀 0.5 중량％0.5% by weight liquid paraffin
카프릴릭/카프릭트리글리세라이드 5.0 중량％Caprylic / capric triglyceride 5.0 wt%
글리세린 3.0 중량％Glycerin 3.0 wt%
부틸렌글리콜 3.0 중량％3.0% by weight of butylene glycol
프로필렌글리콜 3.0 중량％3.0% by weight of propylene glycol
카르복시비닐폴리머 0.1 중량％Carboxyvinyl polymer 0.1 wt%
트리에탄올아민 0.2 중량％0.2% by weight triethanolamine
방부제 0.05 중량％Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량％
Purified water to 100%
3. 영양크림의 제조3. Manufacture of nutritional cream
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 영양크림을 통상의 방법에 따라 제조하였다.A nutritional cream containing the compound of formula (1) as an active ingredient was prepared according to a conventional method, as shown below.
화학식 1의 화합물 0.2 중량％0.2% by weight of the compound of formula (1)
베타-1,3-글루칸 5.0 중량％Beta-1,3-glucan 5.0 wt%
밀납 10.0 중량％Wax 10.0 wt%
폴리솔베이트60 1.5 중량％Polysorbate 60 1.5 wt%
피이지 60 경화피마자유 2.0 중량％≪ tb > < tb > < tb >
솔비탄세스퀴올레이트 0.5 중량％0.5% by weight of sorbitan sesquioleate
유동파라핀 10.0 중량％Liquid paraffin 10.0 wt%
스쿠알란 5.0 중량％Squalane 5.0 wt%
카프릴릭/카프릭트리글리세라이드 5.0 중량％Caprylic / capric triglyceride 5.0 wt%
글리세린 5.0 중량％Glycerin 5.0 wt%
부틸렌글리콜 3.0 중량％3.0% by weight of butylene glycol
프로필렌글리콜 3.0 중량％3.0% by weight of propylene glycol
트리에탄올아민 0.2 중량％0.2% by weight triethanolamine
방부제 0.05 중량％Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량％
Purified water to 100%
4. 마사지크림의 제조4. Manufacture of massage cream
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 마사지크림을 통상의 방법에 따라 제조하였다.A massage cream containing the compound of formula (I) as an active ingredient was prepared according to a conventional method, as shown below.
화학식 1의 화합물 0.1 중량％0.1% by weight of the compound of formula (1)
베타-1,3-글루칸 3.0 중량％Beta-1,3-glucan 3.0 wt%
밀납 10.0 중량％Wax 10.0 wt%
폴리솔베이트60 1.5 중량％Polysorbate 60 1.5 wt%
피이지 60 경화피마자유 2.0 중량％≪ tb > < tb > < tb >
솔비탄세스퀴올레이트 0.8 중량％0.8% by weight of sorbitan sesquioleate
유동파라핀 40.0 중량％Liquid paraffin 40.0 wt%
스쿠알란 5.0 중량％Squalane 5.0 wt%
카프릴릭/카프릭트리글리세라이드 4.0 중량％Caprylic / capric triglyceride 4.0 wt%
글리세린 5.0 중량％Glycerin 5.0 wt%
부틸렌글리콜 3.0 중량％3.0% by weight of butylene glycol
프로필렌글리콜 3.0 중량％3.0% by weight of propylene glycol
트리에탄올아민 0.2 중량％0.2% by weight triethanolamine
방부제 0.05 중량％Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량％
Purified water to 100%
5. 팩의 제조5. Manufacture of pack
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 팩을 통상의 방법에 따라 제조하였다.A pack containing the compound of formula (1) as an active ingredient was prepared according to a conventional method, as shown below.
화학식 1의 화합물 0.2 중량％0.2% by weight of the compound of formula (1)
베타-1,3-글루칸 1.0 중량％Beta-1,3-glucan 1.0 wt%
폴리비닐알콜 13.0 중량％Polyvinyl alcohol 13.0 wt%
소듐카르복시메틸셀룰로오스 0.2 중량％0.2% by weight of sodium carboxymethylcellulose,
글리세린 5.0 중량％Glycerin 5.0 wt%
알란토인 0.1 중량％Allantoin 0.1 wt%
에탄올 6.0 중량％6.0% by weight of ethanol
피이지 -12 노닐페닐에테르 0.3 중량％0.3% by weight of phage-12 nonylphenyl ether
폴리솔베이트 60 0.3 중량％Polysorbate 60 0.3 wt%
방부제 0.05 중량％Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량％
Purified water to 100%
제제예Formulation example 3: 3: 피부외용제의Topical 제조 Produce
1. 젤의 제조1. Manufacture of gel
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 젤을 통상의 방법에 따라 제조하였다.As in the following composition, a gel containing the compound of formula (1) as an active ingredient was prepared according to a conventional method.
화학식 1의 화합물 0.1 중량％0.1% by weight of the compound of formula (1)
베타-1,3-글루칸 0.1 중량％0.1% by weight of beta-1,3-glucan
에틸렌디아민초산나트륨 0.05 중량％0.05% by weight of sodium ethylenediaminetetraacetate
글리세린 5.0 중량％Glycerin 5.0 wt%
카르복시비닐폴리머 0.3 중량％Carboxyvinyl polymer 0.3 wt%
에탄올 5.0 중량％5.0% by weight of ethanol
피이지-60 경화피마자유 0.5 중량％≪ tb > < tb > < tb >
트리에탄올아민 0.3 중량％Triethanolamine 0.3 wt%
방부제 0.05 중량％ Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량％
Purified water to 100%
2. 연고의 제조2. Manufacture of ointment
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 연고를 통상의 방법에 따라 제조하였다.An ointment containing the compound of formula (I) as an active ingredient was prepared according to a conventional method, as shown below.
화학식 1의 화합물 0.5 중량％0.5% by weight of the compound of formula (1)
베타-1,3-글루칸 10.0 중량%Beta-1,3-glucan 10.0 wt%
밀납 10.0 중량%Wax 10.0 wt%
폴리솔베이트60 5.0 중량%Polysorbate 60 5.0 wt%
피이지 60 경화피마자유 2.0 중량%≪ tb > < tb > < tb >
솔비탄세스퀴올레이트 0.5 중량%0.5% by weight of sorbitan sesquioleate
바셀린 5.0 중량%Vaseline 5.0 wt%
유동파라핀 10.0 중량%Liquid paraffin 10.0 wt%
스쿠알란 5.0 중량%Squalane 5.0 wt%
쉐어버터 3.0 중량%SHARE BUTTER 3.0 wt%
카프릴릭/카프릭트리글리세라이드 5.0 중량%Caprylic / capric triglyceride 5.0 wt%
글리세린 10.0 중량%Glycerin 10.0 wt%
프로필렌글리콜 10.2 중량%Propylene glycol 10.2 wt%
트리에탄올아민 0.2 중량%0.2% by weight triethanolamine
방부제 0.05 중량％Preservative 0.05 wt%
색소 0.05 중량％0.05% by weight of pigment
향료 0.05 중량％0.05% by weight fragrance
정제수 to 100 중량%
Purified water to 100%
3. 국소투여용 약제(겔 연고제) 의 제조3. Preparation of topical medicament (gel ointment)
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 겔 연고제를 통상의 방법에 따라 제조하였다.A gel ointment agent containing the compound of the formula (1) as an active ingredient was prepared according to a conventional method.
화학식 1의 화합물 0.5 중량％0.5% by weight of the compound of formula (1)
베타-1,3-글루칸 10.0 중량%Beta-1,3-glucan 10.0 wt%
폴리아크릴산(Carbopol 940) 1.5 중량%1.5% by weight of polyacrylic acid (Carbopol 940)
이소프로판올 5.0 중량%5.0% by weight of isopropanol
헥실렌글리콜 25.0 중량%Hexylene glycol 25.0 wt%
트리에탄올아민 1.7 중량%Triethanolamine 1.7 wt%
탈이온수 to 100 중량%
Deionized water to 100%
4. 국소 투여용 약제(패취제)의 제조4. Preparation of topical medicines (patches)
하기 조성과 같이, 화학식 1의 화합물을 유효성분으로 포함하는 패취제를 통상의 방법에 따라 제조하였다.As the following composition, a patch containing a compound of the formula (1) as an active ingredient was prepared by a conventional method.
화학식 1의 화합물 0.5 중량%0.5% by weight of the compound of formula (1)
베타-1,3-글루칸 3.0 중량%Beta-1,3-glucan 3.0 wt%
헥실렌글리콜 20.0 중량% Hexylene glycol 20.0 wt%
디에틸아민 0.7 중량%Diethylamine 0.7 wt%
폴리아크릴산(Carbopol 934P) 1.0 중량%1.0% by weight of polyacrylic acid (Carbopol 934P)
아황산나트륨 0.1 중량%0.1% by weight of sodium sulfite
폴리옥시에틸렌라우릴에테르(E.O=9) 1.0 중량%1.0% by weight of polyoxyethylene lauryl ether (E.O. = 9)
폴리히드록시에틸렌세틸스테아릴에테르(Cetomacrogol 1000) 1.0 중량%1.0% by weight of polyhydroxyethylene cetyl stearyl ether (Cetomacrogol 1000)
점성의 파라핀 오일 2.5 중량%Viscous paraffin oil 2.5 wt%
카프릴산에스테르/카프르산에스테르(Cetiol LC) 2.5 중량%2.5% by weight of caprylic acid ester / capric acid ester (Cetiol LC)
폴리에틸렌글리콜400 3.0 중량%Polyethylene glycol 400 3.0 wt%
탈이온수 to 100 중량%
Deionized water to 100%
제제예Formulation example 4: 식품의 제조 4: Manufacturing of food
본 발명의 화학식 1의 화합물을 포함하는 식품들을 다음과 같이 제조하였다.Foods containing the compound of formula (I) of the present invention were prepared as follows.
1. 밀가루 식품의 제조1. Manufacture of Flour Food
상기 화학식 1의 화합물 0.05 ∼ 1.0 중량부를 밀가루에 첨가하고, 이 혼합물을 이용하여 빵, 케이크, 쿠키, 크래커 및 면류를 제조하여 건강식품을 제조하였다.
0.05 to 1.0 part by weight of the compound of Formula 1 was added to wheat flour, and a bread, a cake, a cookie, a cracker and a noodle were prepared using the mixture to prepare a health food.
2. 유제품(dairy products)의 제조2. Manufacture of dairy products
상기 화학식 1의 화합물 0.2 중량부를 우유에 첨가하고, 상기 우유를 이용하여 버터 및 아이스크림과 같은 다양한 유제품을 제조하였다.
0.2 part by weight of the compound of Formula 1 was added to milk, and various dairy products such as butter and ice cream were prepared using the milk.
3. 선식의 제조3. Manufacturing of wire
현미, 보리, 찹쌀, 율무를 공지의 방법으로 알파화 시켜 건조 시킨 것을 배전한 후 분쇄기로 입도 60 메쉬의 분말로 제조하였다. 검정콩, 검정깨, 들깨도 공지의 방법으로 쪄서 건조 시킨 것을 배전한 후 분쇄기로 입도 60 메쉬의 분말로 제조하였다. 상기 화학식 1의 화합물을 진공 농축기에서 감압농축하고, 분무, 열풍 건조기로 건조하여 얻은 건조물을 분쇄기로 입도 60 메쉬로 분쇄하여 건조분말을 얻었다.Brown rice, barley, glutinous rice, and yulmu were dried by a known method and dried, and the mixture was granulated to a powder having a particle size of 60 mesh. Black soybeans, black sesame seeds, and perilla seeds were steamed and dried by a conventional method, and then they were prepared into powder having a particle size of 60 mesh by a pulverizer. The compound of Formula 1 was concentrated under reduced pressure in a vacuum concentrator, sprayed, and dried with a hot-air drier, and the resulting dried product was pulverized to a size of 60 mesh with a pulverizer to obtain a dried powder.
상기에서 제조한 곡물류, 종실류 및 화학식 1의 화합물의 건조분말을 혼합 분말 100 중량부에 대하여 다음의 비율로 배합하여 제조하였다.
The grains, seeds, and dry powder of the compound of formula (1) prepared above were blended in the following proportions relative to 100 parts by weight of the mixed powder.
곡물류(현미 30 중량부, 율무 15 중량부, 보리 20 중량부),(30 parts by weight of brown rice, 15 parts by weight of yulmu, 20 parts by weight of barley)
종실류(들깨 7 중량부, 검정콩 8 중량부, 검정깨 7 중량부),Seeds (7 parts by weight of perilla, 8 parts by weight of black beans, 7 parts by weight of black sesame seeds)
화학식 1의 화합물(0.1 중량부),(1) (0.1 part by weight),
영지(0.5 중량부),(0.5 part by weight),
지황(0.5 Rhubarb (0.5
중량부Weight portion
) )
제제예Formulation example 5: 음료의 제조 5: Manufacture of beverages
1. 건강음료의 제조1. Manufacture of health drinks
화학식 1의 화합물 0.1 ㎎0.1 mg of the compound of formula (1)
구연산 1000 ㎎Citric acid 1000 mg
올리고당 100 g100 g of oligosaccharide
매실농축액 2 gPlum concentrate 2 g
타우린 1 gTaurine 1 g
정제수를Purified water 가하여 전체 900 All 900 mLmL
통상의 건강음료 제조방법에 따라 상기의 성분을 혼합한 다음, 약 1 시간 동안 85℃에서 교반 가열한 후, 만들어진 용액을 여과하여 멸균된 2L-용기에 취득하여 밀봉 멸균한 뒤 냉장 보관한 다음 본 발명의 건강음료 조성물 제조에 사용하였다.The above components were mixed according to a conventional health drink manufacturing method, and the mixture was heated at 85 DEG C for about 1 hour with stirring. Then, the solution thus prepared was filtered and sterilized in a sterilized 2L-container, Lt; RTI ID = 0.0 > health < / RTI >
상기 조성비는 비교적 기호 음료에 적합한 성분을 바람직한 실시예로 혼합 조성하였지만, 수요계층, 수요국가, 사용 용도 등 지역적, 민족적 기호도에 따라서 그 배합비를 임의로 변형 실시하여도 무방하다.
Although the composition ratio is a mixture of the components suitable for the preferred beverage as a preferred embodiment, the blending ratio may be arbitrarily varied according to the regional and national preferences such as the demand level, the demanding country, and the intended use.
2. 야채주스의 제조2. Manufacture of vegetable juice
본 발명의 화학식 1의 화합물 1g을 토마토 또는 당근 주스 1,000mL에 가하여 건강 증진용 야채주스를 제조하였다.
1 g of the compound of formula (I) of the present invention was added to 1,000 mL of tomato or carrot juice to prepare vegetable juice for health promotion.
3. 과일주스의 제조3. Manufacture of fruit juice
화학식 1의 화합물 1 g을 사과 또는 포도 주스 1,000 mL에 가하여 건강 증진용 과일주스를 제조하였다.
1 g of the compound of formula (1) was added to 1,000 mL of apple or grape juice to prepare fruit juice for health promotion.
Claims (20)
[화학식 1]
A pharmaceutical composition for enhancing skin elasticity comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
상기 화학식 1로 표현되는 화합물은 전체 조성물 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 피부 탄력 증진용 약학적 조성물.
The method according to claim 1,
Wherein the compound represented by Formula 1 is contained in an amount of 0.0001 to 10% by weight based on the total weight of the composition.
[화학식 1]
An external preparation for skin elasticity enhancement comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
상기 외용제는 연고, 패취, 겔, 크림 또는 분무제의 제형인 피부 탄력 증진용 피부 외용제.
The method according to claim 3,
Wherein the external preparation is a formulation of ointment, patch, gel, cream or spray.
상기 화학식 1로 표현되는 화합물은 전체 피부 외용제 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 피부 탄력 증진용 피부 외용제.
The method according to claim 3,
Wherein the compound represented by Formula 1 is contained in an amount of 0.0001 to 10% by weight based on the total amount of the external preparation for skin.
[화학식 1]
A cosmetic composition for skin elasticity enhancement comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
상기 화장료 조성물은 화장수, 에센스, 로션, 크림, 팩, 젤, 파우더, 파운데이션 또는 세정제의 제형인 피부 탄력 증진용 화장료 조성물.
The method of claim 6,
Wherein the cosmetic composition is a formulation of a lotion, essence, lotion, cream, pack, gel, powder, foundation or detergent.
하기 화학식 1로 표현되는 화합물은 전체 조성물 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 피부 탄력 증진용 화장료 조성물.
The method of claim 6,
A cosmetic composition for skin elasticity enhancement, which comprises 0.0001 to 10% by weight of a compound represented by the following general formula (1).
[화학식 1]
A health functional food for skin elasticity enhancement comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
하기 화학식 1로 표현되는 화합물은 전체 건강기능식품 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 피부 탄력 증진용 건강기능식품.
The method of claim 9,
The health functional food for skin elasticity enhancement according to claim 1, wherein the compound represented by the following general formula (1) is contained in an amount of 0.0001 to 10% by weight relative to the entire health functional food.
[화학식 1]
A pharmaceutical composition for whitening comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
상기 화학식 1로 표현되는 화합물은 전체 조성물 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 미백용 약학적 조성물.
12. The method of claim 11,
Wherein the compound represented by Formula 1 is contained in an amount of 0.0001 to 10% by weight based on the total weight of the composition.
[화학식 1]
An external preparation for whitening skin comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
상기 외용제는 연고, 패취, 겔, 크림 또는 분무제의 제형인 미백용 피부 외용제.
The method of claim 13,
Wherein the external preparation is a formulation of ointment, patch, gel, cream or spray.
상기 화학식 1로 표현되는 화합물은 전체 피부 외용제 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 미백용 피부 외용제.
The method of claim 13,
Wherein the compound represented by Formula 1 is contained in an amount of 0.0001 to 10% by weight based on the total amount of the external preparation for skin.
[화학식 1]
A cosmetic composition for whitening comprising a compound represented by the following formula (1) (cistanoside A) as an active ingredient.
[Chemical Formula 1]
상기 화장료 조성물은 화장수, 에센스, 로션, 크림, 팩, 젤, 파우더, 파운데이션 또는 세정제의 제형인 미백용 화장료 조성물.
The method of claim 16,
Wherein the cosmetic composition is a formulation of a lotion, essence, lotion, cream, pack, gel, powder, foundation or detergent.
하기 화학식 1로 표현되는 화합물은 전체 조성물 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 미백용 화장료 조성물.
The method of claim 16,
Wherein the compound represented by the following formula (1) is contained in an amount of 0.0001 to 10% by weight relative to the total composition.
[화학식 1]
A health functional food for whitening comprising a compound represented by the following formula (1) (cystanide A) as an active ingredient.
[Chemical Formula 1]
하기 화학식 1로 표현되는 화합물은 전체 건강기능식품 대비 0.0001 내지 10 중량%로 포함하는 것을 특징으로 하는 미백용 건강기능식품.
The method of claim 19,
Wherein the compound represented by the following general formula (1) is contained in an amount of 0.0001 to 10% by weight relative to the total health functional food.
Applications Claiming Priority (2)
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