KR20170114736A - Composition for improving skin conditions - Google Patents
Composition for improving skin conditions Download PDFInfo
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- KR20170114736A KR20170114736A KR1020160042212A KR20160042212A KR20170114736A KR 20170114736 A KR20170114736 A KR 20170114736A KR 1020160042212 A KR1020160042212 A KR 1020160042212A KR 20160042212 A KR20160042212 A KR 20160042212A KR 20170114736 A KR20170114736 A KR 20170114736A
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- skin
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Abstract
본 발명은 피부 상태 개선용 조성물에 관한 것이다. 본 발명에 따른 로가닌이 각질형성세포에서 항균 펩타이드의 발현을 증가시켜 피부면역 개선 및 항균 효과를 통해 피부방어력을 증진하고, 피부의 멜라노사이트에서 멜라닌 총량과 티로시나제 활성을 감소시켜 피부 미백 효과를 나타내며, 피부 수분량을 증가시키고, 섬유아세포에서 히알루론산의 생성을 촉진하고, 히알루론산 합성효소의 발현을 증가시키며, 피부 탄력을 개선함으로써 피부 보습 개선 및 피부 탄력 증진 효과를 나타내며, 섬유아세포에서 콜라겐 합성을 촉진하고, 콜라겐 분해효소인 MMP-1의 활성을 억제하여 피부 재생 및 주름 개선을 촉진함과 동시에 세포독성이 없어 인체에 부작용이 없으므로, 약학, 화장료, 식품 또는 피부 외용제 제형 제조에 사용할 수 있다.The present invention relates to a composition for improving skin condition. In accordance with the present invention, roganin increases the expression of antimicrobial peptides in keratinocytes to improve skin defense through skin immunity and antimicrobial effect, reduce total amount of melanin and tyrosinase activity in melanocytes of skin, It increases skin moisture content, promotes the production of hyaluronic acid in fibroblasts, increases expression of hyaluronic acid synthetase, improves skin elasticity and improves skin moisturization and skin elasticity. In fibroblasts, collagen synthesis And inhibits the activity of MMP-1, a collagenase, to promote skin regeneration and wrinkle improvement. In addition, since there is no cytotoxicity and no adverse effect on the human body, it can be used in the manufacture of pharmaceuticals, cosmetics, food or skin external preparation .
Description
본 발명은 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 효과를 나타내는 피부 상태 개선용 조성물에 관한 것이다. TECHNICAL FIELD The present invention relates to a composition for improving skin condition, which exhibits a skin protecting effect, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity improvement effect.
최근 산업발달 및 생활패턴의 변화로 인한 외인성 피부질환이 크게 증가하고 있다. 특히 최근 도시인들은 생활환경이 변화함에 따라 집안의 카펫에 서식하는 진드기, 습도와 온도에 따라 번식하는 세균 및 진균, 공공장소에서의 바이러스 등 외인성 병원균에 노출될 기회가 점차 커지고 있다. 이런 외인성 병원균에 대항하기 위해 인체의 최외각 기관인 피부에서의 면역이 중요시 되고 있는 실정이다. 피부의 방어기작 중 물리적인 방어를 제외한 생체 내 방어 기술을 담당하는 물질로서 항균 펩타이드가 있다. 항균 펩타이드는 크게 두 종류가 있는데 카델리시딘과 디펜신이 그것이다. 카델리시딘(cathelicidin)은 광범위한 항균작용을 나타내며 다양한 면역조절작용 기능을 한다. 이중 LL-37은 인간에서 발현되는 유일하게 알려진 카델리시딘으로 박테리아 존재, 숙주의 사이토카인(cytokines) 분비, 체내 이용 가능한 산소량, 비타민D 등의 요인에 의해서 생산이 정해진다. LL-37은 외부 조직 상처나 감염에 대하여 생체면역반응을 일으키는 역할을 하는데, 박테리아와 진균, 바이러스 등에 대한 직접적인 항균 활성과 함께 호중구(eosinophil), 단핵세포, T 세포에 대한 주화성을 나타내며 내피세포의 증식을 유도한다. 특히 피부에 존재하는 LL-37은 외래 항원의 침투 시 즉각적인 방어 역할을 함으로써 항원 억제 기능을 담당한다.Recently, extrinsic skin diseases due to changes in industrial development and life patterns have been greatly increased. Recently, urban people are increasingly exposed to extrinsic pathogens such as bacteria, fungi, and viruses in public places that reproduce with mites, humidity and temperature in carpets of households as the living environment changes. In order to combat these exogenous pathogens, immunity from the skin, which is the outermost organ of the human body, has become important. Among the defense mechanism of skin, there is an antimicrobial peptide as a substance which is in charge of in vivo defense technology except physical defense. There are two major types of antimicrobial peptides, cadelicidin and dipenthin. Cathelicidin exhibits a wide range of antimicrobial activities and has a variety of immunoregulatory functions. LL-37 is the only known cadelicidin expressed in humans, and its production is determined by factors such as the presence of bacteria, the secretion of cytokines from the host, the amount of oxygen available in the body, and vitamin D. LL-37 plays a role in inducing a bio-immune response against external tissue injury or infection. It has direct antimicrobial activity against bacteria, fungi, viruses, etc. and exhibits chemotaxis against eosinophils, mononuclear cells and T cells, Lt; / RTI > In particular, LL-37, which is present in the skin, plays an antigen-suppressing function by acting as an immediate defense when infiltrating the foreign antigen.
디펜신(defensin)은 항균 펩타이드 중 가장 연구가 많이 된 것들 중 하나이며, 그 구조적 특성에 따라 크게 α-디펜신과 β-디펜신이 있다. 그 중 β-디펜신은 피부, 폐, 기관, 신장, 생식기 등의 점막 상피에서 발현되는 펩타이드 물질로서, 현재까지 인간 유래 β-디펜신으로는 6종류, 즉 인간 β-디펜신-1(hBD1), 인간 β-디펜신-2(hBD2), 인간 β-디펜신-3(hBD3), 인간 β-디펜신-4(hBD4), 인간 β-디펜신-5(hBD5) 및 인간 β-디펜신-6(hBD6)이 분리, 동정되어 있다. 특히 hBD1이 표피세포에서 항상적으로 발현이 되는데 비하여, hBD2는 감염 부위나 물리적인 손상이 나타나는 부위에서 발현이 증가되며, 전신 면역 반응과 염증 반응의 조절에 중요한 역할을 하는 것으로 알려져 있다. 또한, hBD3가 건선 질환 환자의 피부 병변 부위에서 매우 높게 발현되는 것으로 보고된바 있고 사이토카인 및 세균 산물에 의해 유도적으로 발현된다. hBD4는 hBD1, hBD2, 또는 hBD3에 비해 더욱 제한된 분포를 나타내고, 이의 발현은 세균의 감염에 의해 상향조절될 수 있으나, hBD2 및 hBD3를 상향조절하는 염증성 인자에 의해서는 상향조절되지 않는다. hBD5 및 hBD6는 가장 최근에 확인된 것으로서 상피에 주로 위치해 있는 패밀리 일원이다. 이와 함께 최근 β-디펜신은 국소 감염 방어뿐만 아니라, 수상 세포(dendritic cells), T 림프구(lymphocytes), 단핵 세포(monocytes) 등의 세포를 주화성 이동(chemotactic migration) 시킴으로써 후천성 면역에도 관여하고 있는 것으로 알려져 있다.Defensin is one of the most studied antimicrobial peptides, and there are largely α-diphenhydrins and β-diphensins, depending on their structural properties. Among them,? -Dipensin is a peptide substance expressed in mucosal epithelium such as skin, lung, organ, kidney, and genitalia. Up to now, six kinds of human-derived? -Diphenes, namely human? -Diphenes-1 (hBD1) (HBD2), human beta -dipensin-3 (hBD3), human beta -dipensin-4 (hBD4) -6 (hBD6) has been isolated and identified. In particular, hBD1 is expressed in epidermal cells, whereas hBD2 is known to play an important role in the regulation of systemic immune response and inflammatory response. In addition, hBD3 has been reported to be highly expressed in skin lesions of patients with psoriasis and is induced by cytokines and bacterial products. hBD4 exhibits a more restricted distribution relative to hBD1, hBD2, or hBD3, and its expression can be upregulated by bacterial infection, but not upregulated by inflammatory factors that upregulate hBD2 and hBD3. hBD5 and hBD6 are the most recently identified family members that are primarily located in the epithelium. Recently, β-diphenzene has also been implicated in acquired immunity by chemotactic migration of cells such as dendritic cells, T lymphocytes and monocytes as well as local infection protection It is known.
또, 민감한 피부는 유해환경에 노출되면 아토피, 건선 등의 피부면역질환이 나타나기 쉽다. 종래 아토피, 건선 등 피부면역질환 개선은 주로 세라마이드를 이용하여 보습을 유지해주는 방법으로 해결되고 있지만 보습은 시간이 지나면 보습력이 떨어져 피부상태가 원래 상태로 돌아온다는 문제점이 있다. 외부에서 항균 펩타이드를 제작, 피부에 주입하는 방법도 생각해 볼 수 있겠으나 피부 속으로 직접적인 침투가 어렵고 자가면역반응 등의 위험이 있는 관계로 피부세포 자체적으로 항균 펩타이드의 생성을 촉진하게 하는 방법이 피부의 외부로부터의 면역력을 높이고 항균력을 갖추는 방법이 될 수 있겠다.In addition, sensitive skin is susceptible to skin immunological diseases such as atopy and psoriasis when exposed to a harmful environment. Conventionally, improvement of skin immune diseases such as atopy and psoriasis is mainly solved by a method of maintaining moisturization by using ceramide. However, there is a problem that moisturizing is less moisturizing over time and skin condition returns to its original state. Although it is possible to consider how to make an antimicrobial peptide from the outside and inject it into the skin, since it is difficult to directly penetrate into the skin and there is a risk of autoimmune reaction, a method of promoting the production of the antibacterial peptide itself It can be a method to increase the immunity from the outside and to obtain the antibacterial power.
희고 고운 피부를 갖고자 하는 것은 일반적인 소망이다. 피부색과 관련하여, 사람의 피부색은 피부 내 멜라닌(melanin) 농도와 분포에 의해 결정되며, 이러한 멜라닌의 농도와 분포는 유전적으로 결정될 뿐만 아니라 피로, 스트레스, 및 자외선과 같은 환경적 혹은 생리적 조건에 의해서도 영향을 받게 된다고 알려져 있다. 멜라닌은 아미노산의 일종인 티로신(tyrosine)에 티로시나제(tyrosinase)라는 효소가 촉매로 작용하여 도파(DOA) 및 도파퀴논(dopaquinone)으로 순차적으로 바뀐 후, 비효소적인 산화반응을 거쳐 만들어진다. It is a common desire to have white skin. With regard to skin color, the skin color of a person is determined by the concentration and distribution of melanin in the skin, and the concentration and distribution of melanin is not only genetically determined, but also by environmental or physiological conditions such as fatigue, stress and ultraviolet It is known to be affected. Melanin is produced by a nonenzymatic oxidation reaction in which tyrosine, an amino acid, is catalyzed by an enzyme called tyrosinase, which is subsequently converted to dopa (DOA) and dopaquinone.
한편, 기존에 알려진 미백 성분으로는 티로시나제 효소활성을 억제하는 알부틴(arbutin), 코지산(kojic acid) 등과 같은 물질이 있으며, 또한 하이드로퀴논(hydroquinone), 비타민-C(L-ascorbic acid) 및 이들의 유도체, 그리고 각종 식물 추출물이 미백 효능이 있다고 알려져 있다. 이들 물질은 체외 실험 시 멜라닌 색소의 합성을 저해하여, 피부 미백 실현뿐만 아니라 기미나 주근깨 등의 피부 과색소 침착증의 개선 가능성을 보였다. 그러나 이들을 피부에 적용하였을 때, 자극, 발적 등의 피부 안전성의 문제로 사용량의 제한이 있거나, 효과가 미미하여 실질적인 효과를 기대할 수 없는 문제점이 있다.On the other hand, existing whitening ingredients include substances such as arbutin, kojic acid and the like which inhibit tyrosinase enzyme activity, and hydroquinone, L-ascorbic acid and the like Derivatives, and various plant extracts are known to have whitening effect. These substances inhibited the synthesis of melanin pigment in vitro, and showed skin whitening as well as improvement of skin hypercholesterolemia such as spots and freckles. However, when they are applied to the skin, there is a problem that the use amount is limited due to the problem of skin safety such as irritation and redness, or the effect is insignificant so that a substantial effect can not be expected.
또한, 피부의 최외각에 위치하고 있는 표피(epidermis)는 외부의 다양한 물리적, 화학적 및 기계적 자극에 대한 방어와 피부를 통한 체내 수분의 과도한 발산을 막는 보호 기능을 수행하고 있다. 이러한 보호 기능은 각질형성세포로 구성된 각질층이 정상적으로 형성되고 유지됨으로써 가능하다. 각질형성세포는 표피최하층(stratum basale)에서 지속적으로 증식하던 기저세포(basal cell)가 각질층(stratum corneum)으로 이동하면서, 단계적으로 형태 및 기능상의 변화를 거치며 형성된 세포이다. 일정 기간이 지나면 오래된 각질형성세포는 피부에서 탈락되고, 표피 최하층으로부터 올라온 새로운 각질형성세포가 그 기능을 대신하는 표피 분화(epidermis differentiation) 또는 각화(keratinization)의 과정을 반복하게 된다. 이러한 각화과정에서 각질형성세포는 천연보습인자(Natural Moisturizing Factor; NMF)와 세라마이드, 콜레스테롤 및 지방산과 같은 세포 간 지질을 생성하여, 각질층이 외부와의 차단층 역할을 하게 됨으로써 피부장벽(skin barrier)로서의 기능을 보유하게 된다.In addition, the epidermis located at the outermost part of the skin protects against various external physical, chemical and mechanical stimuli and protects against excessive divergence of body water through the skin. This protective function is possible by normally forming and maintaining the stratum corneum composed of keratinocytes. The keratinocyte is a cell formed by a stepwise change in morphology and function, while the basal cell that continuously proliferates from the stratum basale moves to the stratum corneum. After a certain period of time, old keratinocytes are removed from the skin, and new keratinocytes from the epidermis bottom layer are repeatedly replaced by epidermis differentiation or keratinization. In this keratinization process, keratinocytes produce intercellular lipids such as natural moisturizing factors (NMF) and ceramides, cholesterol, and fatty acids, which act as barrier layers to the outside, As shown in Fig.
이와 관련하여, 현대 사회의 주요 질환의 하나로 여겨지는 피부 건조증은 피부 장벽 기능 이상에 의해 야기되는 증상의 하나이다. 최근 환경 오염, 아파트, 고층 건물과 같은 건조한 환경의 증가, 사회적 스트레스의 증가, 우리 나라 특유의 과도한 목욕 문화, 피부 노화 등과 같은 여러 가지 요인에 의해 점점 더 증가하고 있으며, 증세가 심하여 치료를 필요로 하는 경우 또한 지속적으로 증가하고 있다.In this regard, dry skin, which is considered to be one of the major diseases of modern society, is one of the symptoms caused by abnormal skin barrier function. Recently, it has been increasing due to various factors such as environmental pollution, an increase in dry environment such as apartments and high rise buildings, an increase in social stress, an excessive bath culture unique to our country, skin aging, etc., If you are also increasing steadily.
그러나, 앞서 언급한 보습제의 사용은 그 대부분이 근본적인 치료이기보다는 일시적인 증상의 완화에 불과하여, 아토피성 피부염을 포함하는 피부 건조증 및 피부 장벽 기능 이상의 치료에 대한 충분한 효과를 나타내지 못하고 있다. 이에, 손상된 피부 장벽을 근원적으로 재생시켜주는 물질의 개발이 시급한 실정이다.However, the use of the above-mentioned moisturizing agents is not only a fundamental treatment but a temporary symptom relief, and thus does not show sufficient effect for treatment of dry skin and skin barrier function including atopic dermatitis. Therefore, it is urgent to develop a substance that can restore the damaged skin barrier fundamentally.
히알루론산(hyaluronic acid)은 글리코사미노글리칸(glycosaminoglycans)의 일종으로 글루쿠론산과 N-아세틸글루코사민 잔기가 반복적으로 연결되어 있는 사슬모양의 고분자 다당류 물질이다. 다량의 물과 결합하여 겔을 만드는 성질이 있어 높은 점성과 탄성을 가진다. 히알루론산은 세포외 기질의 주요 성분으로, 수분 보유, 세포 간 간격 유지, 세포성장인자 및 영양성분의 저장과 확산에 관여할 뿐만 아니라, 세포의 분열과 분화, 이동 등에도 관여하는 것으로 보고된 바 있다.Hyaluronic acid is a kind of glycosaminoglycans, and is a chain-like polymer polysaccharide substance in which glucuronic acid and N-acetylglucosamine residues are repeatedly connected. It has high viscosity and elasticity because it has a property of making gel by combining with a large amount of water. Hyaluronic acid is a major component of the extracellular matrix and has been reported to be involved not only in the retention of water content, intercellular spacing, storage and spread of cell growth factors and nutrients, but also in cell division, differentiation and migration have.
포유류의 체내에 존재하는 히알루론산의 50% 이상이 피부, 특히 표피의 세포 간 간격과 진피의 결체 조직에 분포한다고 보고되었고, 이러한 히알루론산은 주로 각질형성세포와 섬유아세포에 의해 합성되는 것으로 알려져 있다. 인간 피부에서 히알루론산의 양은 노화와 함께 감소되는 것으로 보고되었고, 피부 내 히알루론산의 감소는 노화에 따른 피부 탄력 저하 및 수분 함유량 감소의 직접적인 원인 중 하나라고 여겨지고 있다(Biochem Biophys Acta 279, 265-275; Carbohydr Res 159, 127-136; Int J Dermatol 33, 119-122). 또한 히알루론산은 각질층의 구조유지와 피부장벽 기능을 유지하는 데에도 관여한다고 알려져 있다(J Cosmet Dermatol. 2007 Jun, 6(2), 75-82).It has been reported that more than 50% of the hyaluronic acid present in the mammalian body is distributed in the skin, in particular in the intercellular space of the epidermis and in the connective tissue of the dermis. Such hyaluronic acid is known to be synthesized mainly by keratinocytes and fibroblasts . The amount of hyaluronic acid in human skin has been reported to decrease with aging, and the reduction of hyaluronic acid in the skin is believed to be one of the direct causes of decreased skin elasticity and moisture content due to aging ( Biochem Biophys Acta 279, 265-275; Carbohydr Res 159, 127-136; Int J Dermatol 33, 119-122). It is also known that hyaluronic acid is involved in maintaining the structure of the stratum corneum and maintaining skin barrier function ( J Cosmet Dermatol . 2007 Jun, 6 (2), 75-82).
그러나, 상기와 같은 효과를 가진 히알루론산은 분자량이 커서 피부에 잘 흡수되지 않는다. 또한, 주사를 이용하여 히알루론산을 피부로 주입하는 방법이 현재 시술되고 있으나, 이러한 방법은 큰 자극을 유발할 뿐만 아니라 피부 세포 내의 히알루론산 합성을 증가시키는 방법이 더 효과적이다. 따라서 인체 내의 히알루론산의 생성을 증가시킬 수 있는 방법에 대한 연구가 활발히 진행되고 있으나, 괄목할 만한 연구 결과는 아직 알려진 바가 없는 실정이다.However, hyaluronic acid having the above effect is not absorbed to the skin because of its high molecular weight. In addition, a method of injecting hyaluronic acid into the skin using injection is currently being performed, but this method not only causes a large stimulus but also increases the synthesis of hyaluronic acid in skin cells. Therefore, studies on a method for increasing the production of hyaluronic acid in the human body are actively conducted, but the remarkable results of the study are not yet known.
한편, 세포 외 기질(matrix)의 주요 구성 성분인 콜라겐은 피부의 섬유아세포에서 생성되는 주요 기질 단백질로서 세포 외 간질에 존재한다. 또한, 생체 단백질 총 중량의 약 30%를 차지하는 중요한 단백질로서 견고한 3중 나선구조를 가지고 있다. 콜라겐은 피부, 건(tendon), 뼈 및 치아의 유기 물질의 대부분을 형성하는데, 특히 뼈와 피부(진피)에 그 비율이 높다. 대부분의 다른 체 구조물에서는 섬유상 봉입체로서 존재한다. On the other hand, collagen, which is a major component of the extracellular matrix, is a major substrate protein produced in the fibroblasts of the skin and exists in extracellular epilepsy. It is also an important protein that accounts for about 30% of the total weight of bioproteins, and has a solid triple helix structure. Collagen forms most of the organic matter in the skin, tendons, bones and teeth, especially in the bones and skin (dermis). In most other structures, it exists as a fibrous inclusion.
피부에 존재하는 콜라겐의 기능으로는 피부의 기계적 견고성, 결합조직의 저항력과 조직의 결합력, 세포접착의 지탱, 세포분할과 분화(유기체의 성장 혹은 상처 치유시)의 유도 등이 알려져 있다(van der Rest et al., Biochemie 72:473-484, 1990). 이러한 콜라겐은 피부의 재생, 피부탄력, 피부 노화 방지, 상처 치유, 보습 등에 관련이 있으며 특히 연령 및 자외선 조사에 의한 광노화에 의해 감소하며, 이는 피부의 주름 형성과 밀접한 연관이 있다고 알려져 있다(Arthur K. Balin et al., "Aging and the skin", 1989). 또한 최근에 들어 피부 노화에 대한 광범위한 연구가 발전되면서 피부에서의 콜라겐의 중요한 기능들이 밝혀지고 있다. The functions of collagen present in the skin are known as mechanical rigidity of the skin, resistance of connective tissues and binding force of tissues, support of cell adhesion, induction of cell division and differentiation (when organism grows or healing) (van der Rest et al. , Biochemie 72: 473-484, 1990). Such collagen is related to regeneration of skin, elasticity of skin, prevention of aging of skin, wound healing, moisturization, and particularly, it is reduced by aging and photoaging by ultraviolet irradiation, and it is known to be closely related to wrinkling of skin (Arthur K Balin et al. , "Aging and the skin ", 1989). In recent years, as a result of extensive research on skin aging, important functions of collagen in skin have been revealed.
기존에 콜라겐의 피부 주름 개선과 보습효과로부터 화장품에 콜라겐을 배합하는 제품들이 출시되어 있으나, 이러한 제품은 콜라겐을 피부 표면에 도포하는 것이나, 고분자인 콜라겐은 경피 흡수되기 어렵고, 따라서 뛰어난 효능을 기대할 수 없었다.In the past, products that combine collagen with cosmetic products have been introduced from the viewpoint of improving skin wrinkles and moisturizing effects of collagen. However, these products do not apply collagen to the skin surface and collagen, which is a polymer, is difficult to be percutaneously absorbed, There was no.
이러한 단점을 극복하기 위하여, 콜라겐의 합성을 촉진하여 주름 개선 효과를 나타내는 것으로 알려진 유효 성분들이 있다. 예를 들어, 콜라겐합성 촉진물질로 레티노익산(retinoic acid), 동물 태반 유래의 단백질, 베툴리닉산(betulinic acid), 클로렐라 추출물(섬유아세포 증식 촉진작용) 등이 알려져 있으나, 피부 적용 시 자극과 발적 등의 안전성의 문제로 사용량의 제한이 있거나, 그 효과가 미미하여 실질적으로 피부의 콜라겐 합성을 촉진하여 피부 기능 개선 효과를 기대할 수 없었다. 따라서, 생체에 안전하고 기존의 콜라겐 발현 촉진 물질보다 효과가 높은 새로운 콜라겐 발현 촉진제의 개발이 절실히 요망되고 있다.In order to overcome these disadvantages, there are active ingredients known to promote the synthesis of collagen and to exhibit wrinkle-reducing effects. For example, retinoic acid, an animal placenta-derived protein, betulinic acid, and chlorella extract (promoting fibroblast proliferation) are known to promote collagen synthesis. However, stimulation and redness Or the effect is insignificant, the collagen synthesis of the skin is substantially promoted and the effect of improving the skin function can not be expected. Therefore, it is urgently required to develop a new collagen expression promoter which is safe for living body and is more effective than the existing collagen expression promoting substance.
따라서, 인체에 적용 시에 안전하고, 유효성분이 안정하며, 무엇보다도 기존 물질보다 아토피, 건선 등 피부 면역개선 및 항균력 증진을 통한 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 또는 피부 탄력 증진 능력이 우수한 성분의 개발이 절실히 요구되고 있는 실정이다.Therefore, it is safe and effective in human body, and its effective ingredient is more stable than the existing ones. In particular, it is possible to improve skin defense, skin whitening, skin moisturization, skin regeneration or wrinkle improvement through improvement of skin immunity and anti- Development of an ingredient having excellent skin elasticity is strongly desired.
본 발명의 목적은 인체 적용 시 피부 자극 등의 부작용이 적고, 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 피부 탄력 증진 등 피부 상태를 개선할 수 있는 하기 화학식 1로 표현되는 화합물의 용도를 제공하는 것이다:The object of the present invention is to provide a skin care cosmetic composition which has few side effects such as skin irritation when applied to a human body and is capable of improving skin condition such as skin protection, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, skin elasticity improvement, To provide the use of the compounds:
[화학식 1][Chemical Formula 1]
상기 과제를 해결하기 위한 수단으로서, 본 발명은 약학, 화장료, 식품 또는 피부 외용제 제형 제조를 위한, 하기 화학식 1로 표현되는 화합물을 유효성분으로 포함하는 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진용 조성물을 제공한다:As a means for solving the above problems, the present invention relates to a composition for improving the skin defense, skin whitening, skin moisturizing, skin Regenerating or wrinkling, and skin elasticity:
[화학식 1][Chemical Formula 1]
본 발명은 또한 상기 화학식 1의 화합물 또는 이의 화장학적으로 허용 가능한 염을 개체의 피부에 도포하는 단계를 포함하는, 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진 방법을 제공한다.The present invention also relates to a method for improving skin defense, skin whitening, skin moisturization, skin regeneration or wrinkle improvement, and skin elasticity enhancement comprising the step of applying the compound of formula 1 or a cosmetically acceptable salt thereof to the individual's skin ≪ / RTI >
본 발명에 따른 로가닌이 각질형성세포에서 항균 펩타이드의 발현을 증가시켜 피부면역 개선 및 항균 효과를 통해 피부방어력을 증진하고, 피부의 멜라노사이트에서 멜라닌 총량과 티로시나제 활성을 감소시켜 피부 미백 효과를 나타내며, 피부 수분량을 증가시키고, 섬유아세포에서 히알루론산의 생성을 촉진하고, 히알루론산 합성효소의 발현을 증가시키며, 피부 탄력을 개선함으로써 피부 보습 개선 및 피부 탄력 증진 효과를 나타내며, 섬유아세포에서 콜라겐 합성을 촉진하고, 콜라겐 분해효소인 MMP-1의 활성을 억제하여 피부 재생 또는 주름 개선을 촉진함과 동시에 세포독성이 없어 인체에 부작용이 없으므로, 약학, 화장료, 식품 또는 피부 외용제 제형 제조에 사용할 수 있다.In accordance with the present invention, roganin increases the expression of antimicrobial peptides in keratinocytes to improve skin defense through skin immunity and antimicrobial effect, reduce total amount of melanin and tyrosinase activity in melanocytes of skin, It increases skin moisture content, promotes the production of hyaluronic acid in fibroblasts, increases expression of hyaluronic acid synthetase, improves skin elasticity and improves skin moisturization and skin elasticity. In fibroblasts, collagen synthesis And inhibits the activity of MMP-1, a collagenase, to promote skin regeneration or wrinkle improvement. In addition, since there is no cytotoxicity and no adverse effect on the human body, it can be used in the manufacture of pharmaceuticals, cosmetics, food or skin external preparation .
이하, 본 발명의 구성을 구체적으로 설명한다.Hereinafter, the configuration of the present invention will be described in detail.
피부면역 개선 및 항균력 증진을 통한 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 성분이 실제 피부에 적용 시 우수한 효과를 발휘하기 위해서는 저농도에서 고활성의 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 활성을 나타내고, 피부를 투과하여 흡수되는 능력이 우수하고, 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 효과를 나타내기에 충분한 시간 동안 머무를 수 있도록 휘발성이 낮고, 조성물이나 피부 상에서 활성 성분이 안정하게 유지되고, 약학, 화장료, 식품, 피부 외용제 등으로의 제형화가 용이하며, 또한 피부에 안전한 것이 바람직하다. 그러나, 공지의 성분 중 상기 특성을 모두 만족시키는 성분은 흔치 않다. 예를 들어, 몇몇 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 성분들은 시험관 내 실험 시 저농도에서도 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 활성은 우수하나, 피부를 투과하여 흡수되는 능력이 떨어져 실제 피부에 적용하기엔 어렵다. 또 다른 활성 성분들은 친수성이 낮아 의약이나 화장품, 식품으로 제형화가 어렵다. 또한, 몇몇 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 성분들은 열, 광, 또는 산소에 노출되었을 때 상기 활성 성분이 분해되거나 다른 화합물로 변형되어 피부에 적용하기 전에 이미 효과가 사라지는 경우도 있다. In order to enhance the skin defense, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement and skin elasticity enhancement by improving skin immunity and enhancing antibacterial power, it is necessary to increase the skin defense power at low concentration, The composition of the present invention exhibits skin whitening, improvement of skin moisturizing, improvement of skin regeneration or wrinkle and improvement of skin elasticity, and is excellent in ability to be absorbed through the skin and to enhance skin defense, skin whitening, skin moisturization, skin regeneration or wrinkle improvement, It is preferable to be low in volatility so as to be able to stay for a sufficient time to exhibit the enhancing effect and to keep the active ingredient stable on the composition or on the skin and to be easily formulated into pharmaceuticals, cosmetics, foods, skin external agents and the like, . However, the components satisfying all of the above-mentioned characteristics among the known components are not common. For example, some skin barrier enhancement, skin whitening, skin moisturization improvement, skin regeneration or wrinkle improvement, and skin elasticity enhancement components can be used to improve skin defense, skin whitening, skin moisturization, skin regeneration or wrinkle improvement, The skin elasticity enhancing activity is excellent, but it is difficult to apply to the actual skin because of its ability to be absorbed through the skin. Other active ingredients have low hydrophilicity, making them difficult to formulate into medicines, cosmetics, and foods. In addition, some skin barrier enhancement, skin whitening, skin moisturizing, skin regeneration or wrinkle enhancement, and skin elasticity enhancement ingredients can be applied to skin when the active ingredient is decomposed or transformed into another compound when exposed to heat, light or oxygen In some cases, the effect is already gone.
하기 실시예에서 확인할 수 있는 바와 같이, 로가닌은 세포 독성이 없어 인체에 부작용이 없으며, 조성물 내에서 안정성을 유지하면서, 각질형성세포에서 항균 펩타이드의 발현을 증가시켜 피부면역 개선 및 항균 효과를 통해 피부방어력을 증진하고, 피부의 멜라노사이트에서 멜라닌 총량과 티로시나제 활성을 감소시켜 피부 미백 효과를 나타내며, 피부 수분량을 증가시키고, 섬유아세포에서 히알루론산의 생성을 촉진하고, 히알루론산 합성효소의 발현을 증가시키며, 피부 탄력을 개선함으로써 피부 보습 개선 및 피부 탄력 증진 효과를 나타내며, 섬유아세포에서 콜라겐 합성을 촉진하고, 콜라겐 분해효소인 MMP-1의 활성을 억제하여 피부 재생 및 주름 개선을 촉진하므로, 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진을 위한 약학, 화장료, 식품, 피부 외용제 등의 유효성분으로 사용할 수 있다.As can be seen in the following examples, rogaine has no cytotoxicity and thus has no adverse effects on the human body. In addition, while maintaining stability in the composition, it increases the expression of the antimicrobial peptide in keratinocytes, To increase the skin defense, to reduce the total amount of melanin and tyrosinase activity in the melanocytes of the skin, to exhibit a skin whitening effect, to increase skin moisture content, to promote the production of hyaluronic acid in fibroblasts and to inhibit the expression of hyaluronic acid synthase , And exhibits skin moisturizing effect and skin elasticity improvement effect by improving skin elasticity, promotes collagen synthesis in fibroblasts, inhibits activity of collagenase MMP-1, promotes skin regeneration and wrinkle improvement, Improving armor, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and Unit may be used as an active ingredient of a pharmaceutical, cosmetic, food, etc. The external preparation for skin for improving elasticity.
따라서, 본 발명은 하기 화학식 1로 표현되는 화합물을 유효성분으로 포함하는 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진용 조성물을 제공한다.Accordingly, the present invention provides a composition for improving skin defense, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity enhancement comprising a compound represented by Chemical Formula 1 as an active ingredient.
[화학식 1][Chemical Formula 1]
상기 화학식 1의 화합물의 화합물명은 일명 로가닌(loganin)이라 한다. The compound name of the compound of the formula (1) is aka loganin.
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 발명의 조성물은 약학 제형 제조를 위해 사용할 수 있다.The compositions of the present invention may be used for the manufacture of pharmaceutical formulations.
따라서, 본 발명의 조성물은 상기 화학식 1의 화합물의 약제학적으로 허용 가능한 염을 포함할 수 있다.Accordingly, the composition of the present invention may comprise a pharmaceutically acceptable salt of the compound of 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.
상기 조성물은 추가로 동일 또는 유사한 기능을 나타내는 유효성분을 1종 이상 함유할 수 있다. 예컨대, 공지의 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진 성분을 포함할 수 있을 것이다. 추가적인 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진 성분을 포함하게 되면 본 발명의 조성물의 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진 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 재생 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 유도체, 또는 각종 식물 추출물 등을 단독 또는 2종 이상 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.The composition may further contain one or more active ingredients exhibiting the same or similar functions. For example, it may include known skin defense enhancement, skin whitening, skin moisturizing, skin regeneration or wrinkle enhancement, and skin elasticity enhancing ingredients. It is believed that the inclusion of additional skin protection, skin whitening, skin moisturizing, skin regeneration or wrinkle enhancement, and skin elasticity enhancing ingredients will enhance the skin barrier properties, skin whitening, skin moisturization, The skin elasticity enhancement effect can 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 is a skin regeneration component known in the art, including retinoic acid, TGF, animal placenta-derived protein, betulinic acid and chlorella extract, (Hydroquinone), vitamin C (L-ascorbic acid), derivatives thereof, or various plant extracts, such as kojic acid, arbutin and the like, As shown in FIG. 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 .
또한, 본 발명의 조성물은 약학적으로 허용 가능한 담체를 더 포함할 수 있다.In addition, the composition of the present invention may further comprise a pharmaceutically acceptable carrier.
약학적으로 허용 가능한 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, and the like.
본 발명의 조성물은 경구 또는 비경구로 투여할 수 있으며, 일반 약학 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 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, a filler, , A binder, a wetting agent, a disintegrant, a surfactant, and the like.
경구 투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 본 발명의 약학적 조성물에 적어도 하나 이상의 부형제 예를 들면, 전분, 칼슘 카보네이트(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 commonly used simple diluents.
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. Examples of the suppository base include witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin and the like.
본 명세서에서, '피부방어력'은 외부의 자극, 독소로부터 피부를 보호하는 능력으로, 상기 자극은 세균, 바이러스, 자외선, 건조함, 상처 등 피부에 유해한 자극을 모두 포함하는 광범위한 개념이다. 보다 구체적으로, 피부면역 개선과 항균력 증진을 통해 피부방어력을 증진하는 것을 포함한다.In the present specification, 'skin defense force' is an ability to protect the skin from external stimuli and toxins, and the stimulus is a broad concept including all kinds of stimuli harmful to the skin such as bacteria, viruses, ultraviolet rays, More specifically, it includes improving skin defense through improving skin immunity and enhancing antibacterial activity.
본 명세서에서, '피부면역'이라 함은 외부 병인균에 대해 항균 펩타이드는 외부 조직 상처나 감염에 대하여 생체면역반응을 일으키는 역할을 하는데, 박테리아와 진균, 바이러스 등에 대한 직접적인 항균 활성과 함께 호중구(eosinophil), 단핵세포, T 세포에 대한 주화성을 나타내며 내피세포의 증식을 유도하고, 특히 피부에 존재하는 항균 펩타이드는 외래 항원의 침투 시 즉각적인 방어 역할을 함으로써 항원 억제 기능을 담당하는 기능을 의미한다.In the present specification, the term 'skin immunity' refers to an external pathogen. The antimicrobial peptide plays a role in causing a bio-immune response against external tissue injury or infection. It has a direct antimicrobial activity against bacteria, fungi, ), Mononuclear cells, and T cells, and induces the proliferation of endothelial cells. Antimicrobial peptides present in the skin, in particular, function as an antigen-suppressing function by acting as an immediate defense in the penetration of foreign antigens.
본 명세서에서, '항균'이라 함은 세균, 진균, 바이러스를 포함하는 다양한 미생물에 대하여 항균 펩타이드가 특정 호중구 과립에 비 활성화된 형태로 존재하다가 펩타이드가 잘려지면서 세포밖으로 활성화된 형태로 분비되는데 이때, 항균 펩타이드의 양이온 부위가 미생물세포막이 가지고 있는 음이온성 인지질에 결합하여 미생물의 세포막을 파괴하는 기능을 의미한다.In the present specification, the term 'antimicrobial' refers to an antimicrobial peptide that is inactive to specific neutrophil granules against various microorganisms including bacteria, fungi, and viruses. When the peptide is cleaved, the antimicrobial peptide is secreted into an active form outside the cell. This means that the cationic site of the antibacterial peptide binds to the anionic phospholipid possessed by the microbial cell membrane and destroys the cell membrane of the microorganism.
본 명세서에서, '미백 효과'라 함은 피부 톤을 밝게 할 뿐만 아니라, 자외선, 호르몬 또는 유전에 기인한 기미나 주근깨 등의 피부 과색소 침착을 개선하는 것을 말한다. 이러한 미백 효과는 예를 들어, 멜라닌 색소 총량을 감소시킴으로써 달성될 수 있으나, 본 발명은 이러한 기전에 의해 한정되는 것은 아니다.In the present specification, the term 'whitening effect' refers to not only brightening the skin tone but also improving skin hypercholesterolemia such as stain or freckles due to ultraviolet rays, hormones or heredity. This whitening effect can be achieved, for example, by reducing the total amount of melanin pigment, but the present invention is not limited by this mechanism.
본 명세서에서, '보습 효과'라 함은 피부의 수분이 감소되는 것을 저해 또는 억제하거나 피부의 수분 함유량을 증가시켜 피부 표면을 매끄럽게 하며, 윤기를 부여하는 것을 말한다. 또는 수분 손실(수분 증발) 등을 적절히 조절하여 생체의 항상성을 유지하는 것을 의미한다. In the present specification, the term 'moisturizing effect' refers to inhibiting or reducing the reduction of moisture in the skin, or increasing the moisture content of the skin to smooth and smooth the surface of the skin. Or water loss (water evaporation), etc., to maintain the homeostasis of the living body.
본 명세서에서, '피부 재생 효과'는 피부 외부 및 내부 원인에 의한 손상에 대하여 피부 조직이 회복되는 것을 말한다. 상기 외부 원인에 의한 손상은 자외선, 외부 오염 물질, 창상, 외상 등을 들 수 있으며, 상기 내부 원인에 의한 손상은 스트레스 등을 들 수 있다.In this specification, the term " skin regeneration effect " refers to recovery of skin tissue against damage caused by external or internal causes of the skin. Damage due to external causes may include ultraviolet rays, external contaminants, wound, trauma, etc. The damage caused by the internal causes may be stress.
본 명세서에서, '피부 주름'은 피부가 쇠하여 생긴 잔줄을 의미하는데, 유전자에 의한 원인, 피부 진피에 존재하는 콜라겐의 감소, 외부 환경 등에 의해 유발될 수 있다. 또한, 엘라스틴과 콜라겐을 이어주는 히알루론산이 감소되면 피부 주름이 생성될 수 있다.In the present specification, 'skin wrinkles' refers to the scarring caused by skin degeneration, which can be caused by a cause of genes, a reduction of collagen existing in the skin dermis, and an external environment. In addition, skin wrinkles can be produced when the amount of hyaluronic acid between elastin and collagen is reduced.
본 명세서에서, '주름 개선'은 피부에 주름이 생성되는 것을 예방, 억제 또는 저해하거나, 이미 생성된 주름을 완화시키는 것을 말한다.In the present specification, "wrinkle improvement" refers to preventing, suppressing or inhibiting the generation of wrinkles on the skin, or alleviating wrinkles already generated.
본 명세서에서, '피부 탄력'은 진피층에 존재하는 엘라스틴(elastin)으로 구성된 탄력섬유에 의해 나타나는데, 이러한 탄력섬유는 고무와 같이 매우 낮은 탄성계수를 가지고 있어서 작은 힘에 의해서도 쉽게 변형되고, 또 그 힘이 제거되었을 때는 쉽게 원형으로 되돌아 온다. 상기 엘라스틴과 콜라겐을 이어주는 히알루론산이 감소되면 피부 탄력이 저하된다. 따라서, '탄력 증진 효과'라 함은 피부에 대한 탄력성이 증가되는 것으로, 피부 탄력의 손실을 억제 또는 저해하거나, 이미 감소된 탄력을 완화시키는 것을 말한다. In the present specification, 'skin elasticity' is represented by elastic fibers composed of elastin existing in the dermal layer. Such elastic fibers have a very low elastic modulus such as rubber, so that they are easily deformed by a small force, When removed, it easily returns to the original shape. When the amount of hyaluronic acid between the elastin and the collagen is decreased, the skin elasticity is lowered. Thus, the 'elasticity-enhancing effect' refers to an increase in elasticity to the skin, which suppresses or inhibits the loss of elasticity of the skin, or alleviates already-reduced elasticity.
본 명세서에서, '개선'은 유효성분을 포함하는 조성물의 투여로 인해 앞서 언급한 여러 가지 피부 상태가 호전 또는 이롭게 변경되는 모든 행위를 의미한다.As used herein, 'improvement' refers to any action that improves or alters the aforementioned various skin conditions due to administration of a composition comprising an active ingredient.
본 명세서에서, '피부'는 동물의 체표를 덮는 조직을 의미하는 것으로, 얼굴 또는 바디 등의 체표를 덮는 조직뿐만 아니라 두피와 모발을 포함하는 최광의의 개념이다.In the present specification, 'skin' refers to a tissue covering the body surface of an animal, and is a concept of the broadest notion including a scalp and a hair as well as a tissue covering a body surface such as a face or a body.
본 발명에 있어서, '유효량'이라 함은 각질형성세포에서 항균 펩타이드의 발현을 증가시켜 피부면역 개선 및 항균 효과를 통해 피부방어력을 증진하거나, 피부의 멜라노사이트에서 멜라닌 총량과 티로시나제 활성을 감소시켜 피부 미백 효과를 나타내며, 피부 수분량을 증가시키고, 섬유아세포에서 히알루론산의 생성을 촉진하고, 히알루론산 합성효소의 발현을 증가시키며, 피부 탄력을 개선함으로써 피부 보습 개선 및 피부 탄력 증진 효과를 나타내며, 섬유아세포에서 콜라겐 합성을 촉진하고, 콜라겐 분해효소인 MMP-1의 활성을 억제하여 피부 재생 및 주름 개선을 촉진 효과를 나타내어 피부 상태를 개선할 수 있는 화합물의 양을 의미한다. 본 발명의 조성물이 유효량의 상기 화학식 1의 화합물을 포함할 때 바람직한 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진 효과를 제공할 수 있다. 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 약학 제형으로 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.In the present invention, the term 'effective amount' refers to an increase in the expression of an antimicrobial peptide in keratinocytes, thereby improving skin defense by improving skin immunity and antimicrobial effect, decreasing total amount of melanin and tyrosinase activity in skin melanocytes, Exhibits a whitening effect, increases skin moisture content, promotes the production of hyaluronic acid in fibroblasts, increases the expression of hyaluronic acid synthetase, improves skin elasticity and thereby improves skin moisturization and skin elasticity. Refers to the amount of a compound capable of promoting collagen synthesis and inhibiting the activity of collagenase MMP-1 to promote skin regeneration and wrinkle improvement, thereby improving the skin condition. When the composition of the present invention contains an effective amount of the compound of Formula 1, it can provide desirable skin defense, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity enhancement. 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 produced into a pharmaceutical formulation, it may contain the compound of Formula 1 at a higher concentration than when it is commercialized as cosmetics that are routinely applied to the 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 조성물은 단독으로, 또는 수술, 방사선 치료, 호르몬 치료, 화학 치료 및 생물학적 반응조절제를 사용하는 방법들과 병용하여 사용할 수 있다.The composition of the present invention may be used alone or in combination with methods using surgery, radiation therapy, hormone therapy, chemotherapy, and biological response modifiers.
또한, 본 발명의 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진용 조성물은 피부 외용제 제형 제조를 위해 사용될 수 있다.In addition, the composition for enhancing skin defense, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity enhancement of the present invention can be used for the preparation of external preparation for skin.
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.
또한, 본 발명의 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진용 조성물은 화장료 제형 제조를 위해 사용될 수 있다.In addition, the composition for promoting skin defense, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity enhancement of the present invention can be used for the production of cosmetic formulations.
상기 화장료 제형은 일반적인 유화 제형 및 가용화 제형의 형태일 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. The cosmetic formulation may be in the form of a conventional emulsion 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 화장품은 상기 화학식 1의 화합물에 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 화장품에 통상적으로 사용되는 임의의 다른 성분과 같은 화장품학 분야에서 통상적으로 사용되는 보조제를 함유할 수 있다.The cosmetic composition may further contain, in addition to the compound of Formula 1, a lipid, an organic solvent, a solubilizing agent, a thickening agent and a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, , Ionic or nonionic emulsifiers, fillers, sequestering and chelating agents, preservatives, vitamins, barrier agents, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or cosmetics And may contain adjuvants commonly used in the cosmetics field, such as any of the other ingredients.
상기 화장료 제형은 유효성분이 단기간 내에 피부에 머무르게 되는 메이크업 제거제, 세정제 등과 같은 워쉬-오프(wash-off) 타입의 화장품의 경우에는 비교적 높은 농도의 상기 화학식 1의 화합물을 포함할 수 있을 것이다. 반면, 유효성분이 장기간 동안 피부에 머무르게 되는 화장수, 유액, 크림, 에센스 등의 리브-온(leave-on) 타입의 화장품의 경우에는 워쉬-오프 타입의 화장품에 비해 낮은 농도의 상기 화학식 1의 화합물을 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%(바람직하게는 0.0001 중량% 내지 1 중량%)로 포함할 수 있다. 본 발명의 조성물이 상기 화학식 1의 화합물을 0.0001 중량% 미만으로 포함할 경우에는 충분한 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 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.The cosmetic formulation may contain a relatively high concentration of the compound of formula (1) in the case of a wash-off type cosmetic such as a makeup remover, a detergent, etc. in which the active ingredient remains on the skin in a short period of time. On the other hand, in the case of leave-on type cosmetics, such as lotion, cream, essence, etc., in which the active ingredient remains on the skin for a long period of time, It may be included. In one embodiment of the present invention, although not limited thereto, the composition may contain 0.0001 wt% to 10 wt% (preferably 0.0001 wt% to 1 wt%) of the compound of Formula 1 based on the total weight of the composition . When the composition of the present invention contains less than 0.0001% by weight of the compound of the formula (1), it can not be expected to have sufficient skin protection, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, , It is intended to prevent such an unpleasant reaction such as allergy or a problem of skin safety.
또한, 본 발명의 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진용 조성물은 식품 제형 제조를 위해 사용될 수 있다.In addition, the composition for promoting skin defense, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity enhancement of the present invention can be used for manufacturing food formulations.
상기 식품 제형은 상기 화학식 1의 화합물을 음료, 차류, 향신료, 껌, 과자류 등의 식품 소재에 첨가하거나, 캡슐화, 분말화, 현탁액 등으로 제조한 식품을 의미한다. The food formulation refers to food prepared by adding the compound of Formula 1 to food materials such as beverage, tea, spice, gum, confectionery, etc., or by encapsulation, powdering, suspension or the like.
상기 식품 제형은 일상적으로 섭취하는 것이 가능하기 때문에 높은 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선 및 피부 탄력 증진 효과를 기대할 수 있어 매우 유용하다.Since the food preparation can be taken on a daily basis, it is very useful because it can expect high skin protection, skin whitening, skin moisturizing, skin regeneration or wrinkle improvement, and skin elasticity enhancement.
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.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 .
상기 식품의 종류에는 특별한 제한은 없다. 상기 물질을 첨가할 수 있는 식품의 예로는 육류, 소세지, 빵, 초콜릿, 캔디류, 스넥류, 과자류, 피자, 라면, 기타 면류, 껌류, 아이스크림류를 포함한 낙농제품, 각종 스프, 음료수, 차, 드링크제, 알코올 음료 및 비타민 복합제 등이 있으며, 통상적인 의미에서의 건강식품을 모두 포함한다.There is no particular limitation on the kind of the food. Examples of the food to which the above substance can be added include dairy products including meat, sausage, bread, chocolate, candy, snack, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, Alcoholic beverages, and vitamin complexes, all of which include health foods in a conventional sense.
식품 제형이 음료인 경우, 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 당알코올이다. 감미제로서는 타우마틴, 스테비아 추출물과 같은 천연 감미제나, 사카린, 아스파르탐과 같은 합성 감미제 등을 사용할 수 있다. 상기 천연 탄수화물의 비율은 본 발명의 조성물 100 mL 당 일반적으로 약 0.01 ∼ 0.04 g, 바람직하게는 약 0.02 ∼ 0.03 g 이다.When the food is a beverage, various flavors or natural carbohydrates may be added as an additional ingredient such as a normal drink. The above-mentioned natural carbohydrates are sugar alcohols such as monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and xylitol, sorbitol and erythritol. Examples of sweeteners include natural sweeteners such as tau martin and stevia extract, synthetic sweeteners such as saccharin and aspartame, and the like. The ratio of the natural carbohydrate is generally about 0.01 to 0.04 g, preferably about 0.02 to 0.03 g per 100 mL of the composition of the present invention.
상기 외에 식품 제형은 여러 가지 영양제, 비타민, 전해질, 풍미제, 착색제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산 음료에 사용되는 탄산화제 등을 함유할 수 있다. 그 밖에 식품 제형은 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.In addition to the above, the food formulations may contain various nutrients, vitamins, electrolytes, flavors, colorants, pectic acid and salts thereof, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, And the like. Other food formulations may contain flesh for the production of natural fruit juices, fruit juice drinks and vegetable drinks. 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.
본 발명은 또한 상기 화학식 1의 화합물 또는 이의 화장학적으로 허용 가능한 염을 개체의 피부에 도포하는 단계를 포함하는, 피부방어력 증진, 피부 미백, 피부 보습 개선, 피부 재생 또는 주름 개선, 및 피부 탄력 증진 방법에 관한 것이다.The present invention also relates to a method for improving skin defense, skin whitening, skin moisturization, skin regeneration or wrinkle improvement, and skin elasticity enhancement comprising the step of applying the compound of formula 1 or a cosmetically acceptable salt thereof to the individual's skin ≪ / RTI >
상기 개체는 쥐, 돼지, 인간 등의 포유동물을 포함하나, 이에 제한하지는 않는다.Such entities include, but are not limited to, mammals such as rats, pigs, humans, and the like.
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.
<참조예 1> 로가닌(loganin) 정보Reference Example 1 Loganin information
[화학식 1][Chemical Formula 1]
CAS No.: 18524-94-2CAS No .: 18524-94-2
구입처: Sigma AldrichWhere to buy: Sigma Aldrich
<실시예 1> 세포독성 평가<Example 1> Cytotoxicity evaluation
화학식 1의 화합물을 인간의 정상 각질형성세포(keratinocyte)의 배양액에 첨가하여 세포 수준에서의 세포독성을 평가하였다.The compound of formula 1 was added to the culture medium of human normal keratinocyte to assess cytotoxicity at the cellular level.
이를 위해, 화학식 1의 화합물을 농도별로 처리한 후 분광광도계를 이용하여 세포 생존능을 확인하였다. 인간 유래 각질형성세포를 24-웰 시험 플레이트에 1×105 cell씩 넣고 부착시킨 후 24시간 배양하여 90% 이상 차게 되었을 때 화학식 1의 화합물을 2 ㎍/mL, 5 ㎍/mL 농도로 각각 처리하였다. 그리고 24시간 배양 후에 배지를 제거하고 각 웰당 200 ㎕ 배지와 CCK8 용액 20 ㎕를 넣고 20분 동안 37℃, 5% CO2 배양기에서 배양한 후 450 nm에서 흡광도를 측정하였다. 무처리한 웰의 흡광도를 기준으로 하여 화학식 1의 화합물이 세포 생존에 미치는 영향을 평가하였고, 실험은 3회 반복하였다.For this, the compound of formula (1) was treated by concentration and cell viability was confirmed by using a spectrophotometer. Human-derived keratinocytes were added to a 24-well test plate in an amount of 1 × 10 5 cells. The cells were incubated for 24 hours and then treated with 2 μg / mL and 5 μg / mL, respectively, Respectively. After incubation for 24 hours, the culture medium was removed, and 200 μl of the culture medium and 20 μl of the CCK8 solution were added to each well. The culture was incubated in a 5% CO 2 incubator at 37 ° C. for 20 minutes, and the absorbance was measured at 450 nm. The effect of the compound of formula (1) on cell survival was evaluated based on the absorbance of the untreated well, and the experiment was repeated three times.
(2 ㎍/mL)The compound of formula (1)
(2 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
표 1에 나타난 바와 같이, 화학식 1의 화합물은 실험 농도에서 세포독성을 일으키지 않는 것을 확인하였다. 이는, 화학식 1의 화합물이 피부 자극 유발 가능성이 낮고 안전한 물질임을 의미한다. 또한, 화학식 1의 화합물은 5 ㎍/mL의 농도에서도 각질형성세포에 무해함을 알 수 있었다.As shown in Table 1, the compound of Chemical Formula 1 did not cause cytotoxicity at the experimental concentrations. This means that the compound of formula (I) is a safe and low-irritating substance. In addition, the compound of formula (1) was found to be harmless to keratinocytes even at a concentration of 5 / / mL.
<실시예 2> 항균능 평가<Example 2> Evaluation of antibacterial activity
화학식 1의 화합물의 항균 특성을 평가하기 위해 인간 유래의 정상 각질형성세포의 배양액에 첨가하여 세포 수준에서 항균 펩타이드, LL37 및 hBD2 mRNA의 발현에 미치는 영향을 측정하였다.To evaluate the antimicrobial properties of the compound of formula (I), the effect on the expression of the antimicrobial peptide, LL37 and hBD2 mRNA was measured at the cell level by adding to the culture medium of human keratinocyte.
이를 위해, 인간 유래의 각질형성세포를 24-웰 시험 플레이트에 5×104 cell씩 넣고 부착시킨 후 1일간 배양하여 80% 이상 차게 되었을 때 화학식 1의 화합물을 2 ㎍/mL 또는 5 ㎍/mL 처리하였다. 처리 후 24시간 후 세포를 회수하여 전체 RNA를 추출하고, 항균 펩타이드인 LL37 및 hBD2 mRNA 발현량을 측정하였고, 실험은 3회 반복하였다.To this end, human-derived keratinocytes were added to a 24-well test plate in an amount of 5 × 10 4 cells. After incubation for 1 day, the cells were treated with 2 μg / mL or 5 μg / mL Respectively. Twenty-four hours after the treatment, the cells were recovered and the total RNA was extracted. The amount of expression of the antimicrobial peptides LL37 and hBD2 mRNA was measured, and the experiment was repeated three times.
(2 ㎍/mL)The compound of formula (1)
(2 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
표 2에 나타난 바와 같이, 화학식 1의 화합물은 미처리군에 대비하여 피부 각질형성세포에서 항균 펩타이드 LL37, hBD2의 발현을 농도 의존적으로 높여주는 것을 볼 수 있었다. As shown in Table 2, the compound of Chemical Formula 1 showed an increase in the concentration of the antimicrobial peptides LL37 and hBD2 in the skin keratinocytes in a concentration-dependent manner in comparison with the untreated group.
<실시예 3> 멜라닌 총량 평가≪ Example 3 > Evaluation of the total amount of melanin
화학식 1의 화합물을 인간의 정상 멜라노사이트(normal human melanocyte: NHM)의 배양액에 첨가하여 세포 수준에서의 미백 효과를 실험하였다. 실험 전 인간의 정상 멜라노사이트에 대하여 독성을 평가하여 독성이 없는 농도를 선정하여 미백평가를 수행하였다.The compound of formula (1) was added to the culture medium of normal human melanocytes (NHM) to test the whitening effect at the cellular level. To evaluate the toxicity of normal melanocytes in humans before the experiment, whiteness evaluation was conducted by selecting the concentration without toxicity.
화학식 1의 화합물을 배양액에 최종농도가 1 ㎍/mL, 5 ㎍/mL, 또는 10 ㎍/mL가 되도록 하여 실험하였으며, 대조군인 알부틴은 500 ㎍/mL 가 되도록 배지에 첨가하여 각각 NHM 세포에 처리하여 3일간 배양하였다. The compound of Chemical Formula 1 was added to the culture medium to a final concentration of 1 μg / mL, 5 μg / mL, or 10 μg / mL, and the control group, arbutin, was added to the medium to a concentration of 500 μg / And cultured for 3 days.
이후, 세포들을 트립신(trypsin) 처리하여 배양용기로부터 떼어내 원심분리 한 후 멜라닌을 추출하였다. 떼어낸 세포는 10% DMSO를 포함한 1N 수산화 나트륨 용액 100 ㎕를 가하여 20분간 끓여 멜라닌을 녹이고, 분광 광도계를 이용, 400 nm에서의 흡광도로 생성된 멜라닌의 양을 측정하였다. Cells were then trypsinized, detached from the culture, centrifuged, and extracted with melanin. To the removed cells, 100 μl of 1 N sodium hydroxide solution containing 10% DMSO was added and the mixture was boiled for 20 minutes to dissolve melanin. The amount of melanin produced by absorbance at 400 nm was measured using a spectrophotometer.
상기 멜라닌 양은 단위 세포수당 (1×106 cell)의 흡광도로 나타내는 방법으로 측정하였으며, 대조군에 대한 상대적인 멜라닌 총량을 백분율(%)로 계산하였고, 실험은 3회 반복하였다.The amount of melanin was measured by an absorbance of 1 × 10 6 cells per unit cell, and the total amount of melanin relative to the control group was calculated as a percentage (%), and the experiment was repeated three times.
(500 ㎍/mL)Arbutin
(500 [mu] g / mL)
(1 ㎍/mL)The compound of formula (1)
(1 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
(10 ㎍/mL)The compound of formula (1)
(10 [mu] g / mL)
표 3에 나타난 바와 같이, 화학식 1의 화합물은 기존에 알려진 미백 물질인 알부틴(arbutin)보다 보다 훨씬 적은 농도이지만, 배양된 NHM 세포에 대하여 뛰어난 멜라닌 총량 감소 기능이 있음을 알 수 있었다.As shown in Table 3, the compound of the formula (1) has a much lower concentration of melanin than that of the known whitening substance arbutin but has excellent melanin total reducing ability for the cultured NHM cells.
<실시예 4> 티로시나제 효소 활성 평가<Example 4> Evaluation of tyrosinase enzyme activity
화학식 1의 화합물을 인간의 정상 멜라노사이트의 배양액에 첨가하여 세포 수준에서의 미백 효과를 실험하였다. 실험 전 인간의 정상 멜라노사이트에 대하여 독성을 평가하여 독성이 없는 농도를 선정하여 미백평가를 수행하였다.The compound of formula (I) was added to the culture medium of human normal melanocytes to examine the whitening effect at the cellular level. To evaluate the toxicity of normal melanocytes in humans before the experiment, whiteness evaluation was conducted by selecting the concentration without toxicity.
화학식 1의 화합물을 배양액에 최종농도가 1 ㎍/mL, 5 ㎍/mL, 또는 10 ㎍/mL가 되도록 하여 실험하였으며, 대조군인 알부틴은 500 ㎍/mL 가 되도록 배지에 첨가하여 각각 NHM 세포에 처리하여 3일간 배양하였다. The compound of Chemical Formula 1 was added to the culture medium to a final concentration of 1 μg / mL, 5 μg / mL, or 10 μg / mL, and the control group, arbutin, was added to the medium to a concentration of 500 μg / And cultured for 3 days.
이후, 세포들을 트립신 처리하여 배양용기로부터 떼어내 원심분리 한 후 1% Triton X-100, 0.1mM PMSF를 포함한 0.1M phosphate buffer로 세포에서 단백질을 추출하였다. 추출한 단백질 50 ㎕를 0.1M phosphate buffer에 희석한 1mM DOPA 50 ㎕와 함께 37℃에서 1시간 배양한 뒤 분광 광도계를 이용, 475nm에서의 흡광도로 티로시나제 효소 활성을 측정하였다. 상기 티로시나제 효소 활성은 단위 세포수당 (1×106 cell)의 흡광도로 나타내는 방법으로 측정하였으며, 대조군에 대한 상대적인 효소 활성을 백분율 (%)로 계산하였고, 실험은 3회 반복하였다.Then, the cells were trypsinized, detached from the culture vessel, centrifuged, and extracted with 0.1 M phosphate buffer containing 1% Triton X-100 and 0.1 mM PMSF. 50 μl of the extracted protein was incubated with 50 μl of 1 mM DOPA diluted in 0.1 M phosphate buffer for 1 hour at 37 ° C., and the activity of tyrosinase enzyme was measured by absorbance at 475 nm using a spectrophotometer. The tyrosinase enzyme activity was measured by an absorbance of 1 × 10 6 cells per unit cell. The relative enzyme activity relative to the control group was calculated as a percentage (%), and the experiment was repeated three times.
(500 ㎍/mL)Arbutin
(500 [mu] g / mL)
(1 ㎍/mL)The compound of formula (1)
(1 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
(10 ㎍/mL)The compound of formula (1)
(10 [mu] g / mL)
표 4에 나타난 바와 같이, 화학식 1의 화합물은 기존에 알려진 미백 물질인 알부틴(arbutin)보다 훨씬 적은 농도이지만 배양된 NHM 세포에 대하여 뛰어난 티로시나제 효소활성 억제 기능이 있음을 알 수 있었다.As shown in Table 4, the compound of Chemical Formula 1 has much lower concentration than arbutin, which is a known whitening substance, but has excellent tyrosinase enzyme activity inhibitory ability against cultured NHM cells.
<실시예 5> 피부 수분 보유능 평가≪ Example 5 > Evaluation of ability to retain skin moisture
화학식 1의 화합물의 보습 효과를 평가하기 위해, 22℃ 및 상대습도 50%의 항온 항습실에서 건강한 성인 30명의 하박 안쪽에 하기 제제예 2의 영양크림을 일정량(2 mg/㎠) 도포하고 도포 전, 도포 1시간 후 및 도포 2시간 후의 피부의 수분함량을 측정하였다. 대조군의 경우 화학식 1의 화합물 대신 동량의 에탄올을 함유한 영양크림을 같은 방법으로 제조하여 도포하였으며, 아무런 처리를 하지 않은 정상 피부를 무처리군으로 사용하였다. 수분 보유능 측정은 Corneometer(Courage + Khazaka, GmbH, Germany)를 사용하여 피부 표면의 전기 전도도를 측정하였다.In order to evaluate the moisturizing effect of the compound of Chemical Formula 1, a predetermined amount (2 mg / cm 2) of the nutritional cream of the following formulation 2 was applied to the inside of 30 healthy adults at a constant temperature and humidity chamber of 22 ° C and a relative humidity of 50% The moisture content of the skin after 1 hour of application and 2 hours after application was measured. In the control group, a nutrient cream containing the same amount of ethanol instead of the compound of formula (1) was prepared and applied in the same manner, and normal skin without any treatment was used as a non-treated group. The water conductivity was measured by using a Corneometer (Courage + Khazaka, GmbH, Germany).
(corneometer units)(n=30)unit
(n = 30)
영양크림Control group
Nourishing cream
표 5에 나타나는 바와 같이, 화학식 1의 화합물을 함유하는 영양크림은 사람 피부의 수분량을 증가시키며, 도포 2 시간 후에도 우수한 수분 보유능을 나타내었다. As shown in Table 5, the nutritional cream containing the compound of formula (1) increased the water content of human skin and showed excellent water holding ability even after 2 hours of application.
<실시예 6> 히알루론산 농도 평가Example 6 Evaluation of Hyaluronic Acid Concentration
인간 유래 섬유아세포(Human Dermal Fibroblast)를 10% 우혈청(fetal bovine serum)을 포함한 DMEM 배지에서 1×105 cells/mL로 배양해서 24-웰 플레이트에 500 ㎕씩 분주하여 18시간 배양한 후, 우혈청이 포함되어 있지 않은 DMEM 배지로 2회 세척하고 화학식 1의 화합물을 하기 농도별로 첨가하였다. 음성 대조군으로 동량의 에탄올을 처리하였고, 양성 대조군으로 히알루론산 생성을 촉진한다고 알려진 글루코사민 하이드로클로라이드(Glucosamine hydrochloride, Sigma-aldrich)를 100 ㎍/mL 처리하였다. 24시간 배양 후, 세포 배양액을 회수하여 Hyaluronan ELISA 키트(R&D Systems)를 이용하여 히알루론산 농도를 측정하였다. Human Dermal Fibroblast was cultured in DMEM medium containing 10% fetal bovine serum at 1 × 10 5 cells / mL, and 500 μl of each was added to a 24-well plate. After culturing for 18 hours, Washed twice with DMEM medium containing no serum, and the compound of formula (1) was added at the following concentrations. Negative controls were treated with the same amount of ethanol and treated with 100 μg / mL of glucosamine hydrochloride (Sigma-aldrich), a positive control known to promote hyaluronic acid production. After culturing for 24 hours, the cell culture medium was recovered and the hyaluronic acid concentration was measured using a Hyaluronan ELISA kit (R & D Systems).
또한, 무첨가 대조군의 히알루론산 농도를 기준(100%)으로 화학식 1의 화합물을 처리한 실험군의 히알루론산 농도를 수치화하여 표 6에 나타내었다.The hyaluronic acid concentration of the test group treated with the compound of formula (1) at the reference (100%) of the hyaluronic acid concentration of the no-added control group was quantified and is shown in Table 6.
표 6에 나타난 바와 같이, 화학식 1의 화합물은 인간 유래의 섬유아세포에서 히알루론산 생성을 증가시켰다.As shown in Table 6, the compound of Chemical Formula 1 increased hyaluronic acid production in human-derived fibroblasts.
<실시예 7> 히알루론산 합성효소의 발현량 평가Example 7 Evaluation of expression amount of hyaluronic acid synthase
인간 유래 섬유아세포(Human Dermal Fibroblast)를 10% 우혈청(fetal bovine serum)을 포함한 DMEM 배지에서 1×106 cells/ml로 배양해서 6-웰 플레이트에 3000 ㎕씩 분주하여 18시간 배양한 후, 우혈청이 포함되어 있지 않은 DMEM 배지로 2회 세척하고. 화학식 1의 화합물을 하기 농도별로 24시간 동안 처리하였다. 세포를 회수하여 RNeasy mini kit(Qiagen)로 전체 RNA를 추출한 뒤, 정량하여 1㎍의 RNA를 GeneAmp® RNA PCR kit(Applied Biosystems)를 이용하여 역전사(reverse transcription)시켰다. 역전사 반응은 Mycycler® PCR 기기(Biorad)를 이용하여 수행하였다. Human Dermal Fibroblast was cultured in DMEM medium containing 10% fetal bovine serum at a density of 1 × 10 6 cells / ml, and 3000 μl of each was dispensed into a 6-well plate. After culturing for 18 hours, And washed twice with DMEM medium containing no serum. The compound of formula (1) was treated at the following concentrations for 24 hours. Cells were collected and total RNA was extracted with RNeasy mini kit (Qiagen), and 1 μg of RNA was quantified and reverse transcribed using GeneAmp ® RNA PCR kit (Applied Biosystems). The reverse transcription reaction was performed using a Mycycler ® PCR instrument (Biorad).
이후 역전사 반응용액 2 ㎕와 HAS-2, HAS-3, GAPDH(Glyceraldehyde-3-phosphate dehydrogenase)의 Taqman® probe (Invitrogen, 미국, HS02511055_S1, HS03929097_g1)를 이용하여 정량적 실시간 PCR을 수행하였다. 실시간 PCR은 CFX96 TouchTM Real-Time PCR Detection System 기기(Biorad)를 이용하여 수행하였다. 실시간 PCR을 통해 얻은 실험 결과는 하우스키핑(housekeeping) 유전자인 GAPDH를 기준으로 Livak K.J. 외(Methods, 2001, 25, 402-408)에 기재된 방법으로 계산하여 나타내었다.After using the reverse transcription reaction solution 2 ㎕ and HAS-2, HAS-3, GAPDH Taqman ® probe (Invitrogen, USA, HS02511055_S1, HS03929097_g1) of (Glyceraldehyde-3-phosphate dehydrogenase) was carried out a quantitative real-time PCR. Real-time PCR was performed using a CFX96 Touch TM Real-Time PCR Detection System instrument (Biorad). Experimental results obtained by real-time PCR were calculated by the method described in Livak KJ et al. ( Methods , 2001, 25, 402-408) on the basis of the housekeeping gene GAPDH.
또한, 음성 대조군의 mRNA 발현량을 기준(100%)으로 하여 화학식 1의 화합물을 처리한 실험군의 mRNA 발현량을 수치화하여 표 7에 나타내었다. The mRNA expression level of the test group treated with the compound of the formula (1) was quantified as the standard (100%) of the mRNA expression level of the negative control group, and is shown in Table 7.
(100 ㎍/mL)Glucosamine
(100 [mu] g / mL)
(1 ㎍/mL)The compound of formula (1)
(1 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
(10 ㎍/mL)The compound of formula (1)
(10 [mu] g / mL)
표 7에 나타난 바와 같이, 화학식 1의 화합물은 히알루론산 합성효소의 mRNA 발현량을 증가시켜 히알루론산의 생성을 증가시킴을 알 수 있었다.As shown in Table 7, it was found that the compound of Chemical Formula (1) increases the amount of mRNA expression of hyaluronic acid synthase to increase the production of hyaluronic acid.
<실시예 8> 콜라겐 발현량 평가Example 8 Evaluation of Collagen Expression Level
화학식 1의 화합물을 인간 유래의 섬유아세포의 배양액에 첨가하여 세포 수준에서 콜라겐 발현량을 검정하였다. 발현된 콜라겐의 측정은 PICP EIA kit(Procollagen Type I C-Peptide Enzyme Immuno assay, TAKARA Korea)를 이용하여 정량하였다. The compound of formula (1) was added to the culture medium of human-derived fibroblasts to determine the amount of collagen expression at the cellular level. The expression of collagen was quantitated using a PICP EIA kit (Procollagen Type I C-Peptide Enzyme Immuno Assay, TAKARA Korea).
화학식 1의 화합물을 1 ㎍/mL, 5 ㎍/mL 또는 10 ㎍/mL 가 되도록 24시간 처리 후, 배양액을 취하여 PICP EIA Kit로 각 농도에서 콜라겐 발현 정도를 분광광도계를 이용하여 450 nm에서 측정하였다. 음성대조군은 무처리군이며, 양성대조군은 비타민 D를 50nM 처리한 군을 이용하였다. 콜라겐 발현양은 음성대조군에 대한 상대적인 발현량으로 증가율을 계산하였다.After the compound of formula (1) was treated for 1 hour at a concentration of 1 / / mL, 5 / / mL or 10 / / mL, the culture was taken and the degree of collagen expression was measured at 450 nm using a spectrophotometer at each concentration with PICP EIA Kit . Negative control group was untreated group and positive control group was treated with 50 nM vitamin D group. The amount of collagen expression was calculated by the relative amount of expression relative to the negative control.
(50 nM)Vitamin D
(50 nM)
(1 ㎍/mL)The compound of formula (1)
(1 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
(10 ㎍/mL)The compound of formula (1)
(10 [mu] g / mL)
표 8에 나타난 바와 같이, 화학식 1의 화합물은 세포 내 콜라겐의 발현을 증가시켰다.As shown in Table 8, the compound of Chemical Formula 1 increased the expression of intracellular collagen.
<실시예 9> 콜라겐 분해효소 MMP-1 총량 평가Example 9 Evaluation of total amount of collagenase MMP-1
화학식 1의 화합물의 콜라겐 분해효소 MMP-1 함량에 대한 억제 효과를 확인하였다. 실험 전 인간 유래 섬유아세포를 대상으로 실험물질의 농도 1 ㎍/mL, 5 ㎍/mL, 또는 10 ㎍/mL 에서 세포독성을 평가(섬유아세포를 배양하여 MTT 시험을 하는 방법으로 평가하였으며, 문헌 Mossman T. (1983). Rapid Colorimetric Assay for Cellular Growth & Survival: application to proliferation & cytotoxicity assays. Journal of Immunological Methods 65, 55-63을 참고하여 수행함)하였으며, 세포독성이 없는 농도를 선정하여 콜라게나제 평가법으로 평가하였다.The inhibitory effect of the compound of formula (1) on the content of collagenase MMP-1 was confirmed. To evaluate the cytotoxicity of human fibroblasts before the experiment at concentrations of 1, 5, and 10 μg / mL of the test substance (fibroblasts were cultured and evaluated by MTT test, Mossman T. (1983), Rapid Colorimetric Assay for Cellular Growth & Survival: Application to proliferation & cytotoxicity assays, Journal of Immunological Methods 65, 55-63) Respectively.
인간 정상 피부 세포인 섬유아세포를 24-웰 마이크로 플레이트에 각 웰당 2.5×104 세포가 되도록 접종하고, 10% 혈청 DMEM 배지 및 37℃의 조건에서 24시간 동안 배양한 후 10% 혈청 DMEM 배지를 제거하고 인산완충용액으로 1회 세척한 후 화학식 1의 화합물을 첨가한 무혈청 DMEM 배지 및 대조군으로 화학식 1의 화합물이 포함되지 않은 무혈청 DMEM 배지에서 30분 동안 추가로 배양하였다.Human normal skin cells, fibroblasts, were inoculated into 24-well microplates at 2.5 × 10 4 cells per well, cultured in 10% serum DMEM medium and 37 ° C. for 24 hours, and 10% serum DMEM medium was removed The cells were washed once with phosphate buffer solution and incubated for 30 minutes in serum-free DMEM medium supplemented with the compound of formula (I) and in serum-free DMEM medium containing no compound of formula (I).
시료 처리 30분 후 MMP-1를 생성시키는 것으로 알려진 물질인 TNF-알파(tumor necrosis factor-alpha) 50 ng/mL로 자극 후 24시간 배양하였다. 이때 TNF-알파 무처리군과 처리군은 화학식 1의 화합물이 포함되지 않은 대조군 중 TNF-알파를 처리하지 않은 무처리군과 TNF-알파를 처리한 처리군으로 하였다.After 30 minutes of sample treatment, the cells were cultured for 24 hours after stimulation with 50 ng / mL TNF-alpha (tumor necrosis factor-alpha), a substance known to produce MMP-1. At this time, the TNF-alpha-treated group and the treated group were treated with the TNF-alpha-untreated control group and the TNF-alpha treated control group, respectively.
각 웰의 상층액을 모아 MMP-1 분석 키트(Amersham, 미국)를 이용하여 새로 합성된 MMP-1의 양(ng/mL)을 측정하고 하기 수학식 1에 따라 MMP-1 생성 억제율(%)을 계산하였다.The supernatant of each well was collected and the amount (ng / mL) of the newly synthesized MMP-1 was measured using an MMP-1 assay kit (Amersham, USA) Respectively.
하기 수학식 1에서 대조군의 MMP-1의 양은 TNF-알파 처리군의 MMP-1양을 의미하며 실험군의 MMP-1의 양은 각각 농도로 물질이 첨가된 군을 말한다.In the following equation (1), the amount of MMP-1 in the control group means the amount of MMP-1 in the TNF-alpha treatment group, and the amount of MMP-1 in the test group means the group to which the substance is added at each concentration.
[수학식 1][Equation 1]
(50 ㎍/mL)TNF-a
(50 [mu] g / mL)
(1 ㎍/mL)The compound of formula (1)
(1 [mu] g / mL)
(5 ㎍/mL)The compound of formula (1)
(5 [mu] g / mL)
(10 ㎍/mL)The compound of formula (1)
(10 [mu] g / mL)
표 9에 나타난 바와 같이, 화학식 1의 화합물은 콜라겐 분해효소인 MMP-1을 효율적으로 억제하였다.As shown in Table 9, the compound of Chemical Formula 1 efficiently inhibited the collagenase, MMP-1.
<실시예 10> 피부 탄력 증진 평가Example 10 Evaluation of Skin Elasticity Enhancement
화학식 1의 화합물의 피부 탄력 증진 효과를 평가하기 위해, 22 및 상대습도 50%의 항온 항습실에서 건강한 성인 30명의 목가에 하기 제제예 2의 영양크림을 4주간 도포하였다. 도포한 후 도표 전 및 후의 탄력을 측정하여 피부 탄력 개선 효과를 비교 평가하였다.In order to evaluate the skin elasticity enhancement effect of the compound of Chemical Formula 1, the nutritional cream of the following formulation 2 was applied to 30 healthy adults at a constant temperature and humidity of 22 and a relative humidity of 50% for 4 weeks. After the application, the elasticity of the skin before and after the chart was measured and the skin elasticity improvement effect was compared and evaluated.
피검자의 목가 왼쪽 부위에는 화학식 1의 화합물을 함유한 영양크림을, 오른쪽 부위에는 화학식 1의 화합물 대신 동량의 에탄올을 함유한 영양크림을 1일 2회씩 아침ㆍ저녁으로 세안 후 4주간 사용하도록 하였다. 그 후, 피부탄력측정기(Cutometer, C+K, Germany)를 이용하여 각 부위에서의 탄력의 개선 정도를 측정하였다. 개선 정도는 Ur/Uf를 parameter로 사용하였다.The nutritional cream containing the compound of formula (1) was used on the left side of the subject's neck and the nutritional cream containing the same amount of ethanol instead of the compound of formula (1) on the right side was used twice daily for 4 weeks after cleansing in the morning and evening. After that, the degree of improvement of elasticity at each site was measured using a skin elasticity meter (Cutometer, C + K, Germany). The degree of improvement was used as a parameter of Ur / Uf.
표 10에 나타난 바와 같이, 화학식 1의 화합물은 사람 피부의 탄력을 개선하였고, 어떠한 부작용도 나타내지 않았다.As shown in Table 10, the compound of Chemical Formula 1 improved the elasticity of human skin and showed no side effects.
이하에서는 유효성분으로 화학식 1의 화합물을 포함하는 여러 제제의 예들을 기재한다. 다만, 본 발명은 이러한 제제예들에 한정되어 해석되는 것은 아니며, 후술하는 제제예들 이외에 본 발명이 속한 분야에서 통상의 지식을 가진 자에게 잘 알려진 여러 다른 제제들로 제형화 될 수 있다. Hereinafter, examples of various formulations containing the compound of formula (I) as an active ingredient are described. It should be understood, however, that the invention is not construed as being limited to these formulation examples, and may be formulated into various other preparations well known to those skilled in the art to which the present invention belongs.
<제제예 1> 약학적 제제의 제조≪ Formulation Example 1 > Preparation of pharmaceutical preparation
1. 산제의 제조1. Manufacturing of powder
성분: 화학식 1의 화합물 0.001g, 유당 1g Ingredients: 0.001 g of the compound of formula (1), 1 g of lactose
상기의 성분을 혼합하고 기밀포에 충전하여 산제를 제조하였다.The above components were mixed and filled in airtight bags to prepare powders.
2. 정제의 제조2. Preparation of tablets
성분: 화학식 1의 화합물 0.2㎎, 옥수수전분 100㎎, 유당 100㎎, 스테아린산 마그네슘 2㎎ Ingredients: 0.2 mg of the compound of formula (I), 100 mg of corn starch, 100 mg of lactose, 2 mg of magnesium stearate
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
성분: 화학식 1의 화합물 0.2㎎, 옥수수전분 100㎎, 유당 100㎎, 스테아린산 마그네슘 2㎎ Ingredients: 0.2 mg of the compound of formula (I), 100 mg of corn starch, 100 mg of lactose, 2 mg of magnesium stearate
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. 환제의 제조4. Manufacture of pills
성분: 화학식 1의 화합물 0.003 g, 유당 1.5 g, 글리세린 1 g, 자일리톨 0.5 gIngredients: 0.003 g of the compound of formula (I), 1.5 g of lactose, 1 g of glycerin, 0.5 g of xylitol
상기의 성분을 혼합한 후, 통상의 방법에 따라 1환당 4 g이 되도록 환제를 제조하였다.After mixing the above components, a pellet was prepared so as to be 4 g per one ring according to a conventional method.
5. 과립의 제조5. Manufacture of granules
성분: 화학식 1의 화합물 2 ㎎, 대두 추출물 50 ㎎, 포도당 200 ㎎, 전분 600 ㎎ Ingredients: 2 mg of the compound of formula (I), 50 mg of soybean extract, 200 mg of glucose, 600 mg of starch
상기의 성분을 혼합한 후, 30% 에탄올 100 ㎎을 첨가하여 과립을 제조한 후 이를 60℃에서 건조하고 건조된 과립을 과립포장용 봉지에 충진하였다.After mixing the above components, 100 mg of 30% ethanol was added to prepare granules. The granules were dried at 60 ° C, and the dried granules were filled in a granular packing bag.
<제제예 2> 화장품의 제조≪ Formulation Example 2 > Preparation of cosmetics
1. 유연화장수(스킨로션)의 제조1. Manufacture of softening longevity (skin lotion)
화학식 1의 화합물을 유효성분으로 포함하는 유연화장수를 하기 조성과 같이 통상의 방법에 따라 제조하였다.The softening water containing the compound of formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
유연화장수의 조성:Composition of softening longevity:
화학식 1의 화합물 0.1 중량%, 베타-1,3-글루칸 1.0 중량%, 부틸렌글리콜 2.0 중량%, 프로필렌글리콜 2.0 중량%, 카르복시비닐폴리머 0.1 중량%, 피이지-12 노닐페닐에테르 0.2 중량%, 폴리솔베이트80 0.4 중량%, 에탄올 10.0 중량%, 트리에탄올아민 0.1 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.1 weight% of the compound of the formula (1), 1.0 weight% of beta-1,3-glucan, 2.0 weight% of butylene glycol, 2.0 weight% of propylene glycol, 0.1 weight% of carboxyvinyl polymer, 0.2 weight% 0.05% by weight of coloring matter, 0.05% by weight of fragrance, 100% by weight of purified water, and 0.05% by weight of a preservative, 0.4% by weight of polysorbate 80, 10.0% by weight of ethanol,
2. 영양화장수(밀크로션)의 제조2. Manufacture of nutrition lotion (milk lotion)
화학식 1의 화합물을 유효성분으로 포함하는 영양화장수를 하기 조성과 같이 통상의 방법에 따라 제조하였다.A nutritional lotion comprising the compound of the formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
영양화장수의 조성:Composition of nutrition lotion:
화학식 1의 화합물 0.1 중량%, 베타-1,3-글루칸 1.0 중량%, 밀납 4.0 중량%, 폴리솔베이트60 1.5 중량%, 솔비탄세스퀴올레이트 1.5 중량%, 유동파라핀 0.5 중량%, 카프릴릭/카프릭트리글리세라이드 5.0 중량%, 글리세린 3.0 중량%, 부틸렌글리콜 3.0 중량%, 프로필렌글리콜 3.0 중량%, 카르복시비닐폴리머 0.1 중량%, 트리에탄올아민 0.2 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.1 weight% of the compound of Formula 1, 1.0 weight% of beta-1,3-glucan, 4.0 weight% of beeswax, 1.5 weight% of polysorbate 60, 1.5 weight% of sorbitan sesquioleate, 0.5 weight% of liquid paraffin, / Carboxy triglyceride 5.0 wt%, glycerin 3.0 wt%, butylene glycol 3.0 wt%, propylene glycol 3.0 wt%, carboxyvinyl polymer 0.1 wt%, triethanolamine 0.2 wt%, preservative 0.05 wt%, coloring matter 0.05 wt% 0.05% by weight of fragrance, 100% by weight of purified water,
3. 영양크림의 제조3. Manufacture of nutritional cream
화학식 1의 화합물을 유효성분으로 포함하는 영양크림을 하기 조성과 같이 통상의 방법에 따라 제조하였다.A nutritional cream containing the compound of formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
영양크림의 조성:Composition of nutrition cream:
화학식 1의 화합물 0.2 중량%, 베타-1,3-글루칸 5.0 중량%, 밀납 10.0 중량%, 폴리솔베이트60 1.5 중량%, 피이지 60 경화피마자유 2.0 중량%, 솔비탄세스퀴올레이트 0.5 중량%, 유동파라핀 10.0 중량%, 스쿠알란 5.0 중량%, 카프릴릭/카프릭트리글리세라이드 5.0 중량%, 글리세린 5.0 중량%, 부틸렌글리콜 3.0 중량%, 프로필렌글리콜 3.0 중량%, 트리에탄올아민 0.2 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.2 weight% of the compound of the formula (1), 5.0 weight% of beta-1,3-glucan, 10.0 weight% of wax, 1.5 weight% of polysorbate 60, 2.0 weight% of hardened castor oil, 0.5 weight% of sorbitan sesquioleate, , Paraffin 10.0% by weight, squalane 5.0% by weight, caprylic / capric triglyceride 5.0% by weight, glycerin 5.0% by weight, butylene glycol 3.0% by weight, propylene glycol 3.0% by weight, triethanolamine 0.2% by weight, preservative 0.05 0.05% by weight of pigment, 0.05% by weight of fragrance, 100% by weight of purified water,
4. 마사지크림의 제조4. Manufacture of massage cream
화학식 1의 화합물을 유효성분으로 포함하는 마사지크림을 하기 조성과 같이 통상의 방법에 따라 제조하였다.A massage cream containing the compound of formula (I) as an active ingredient was prepared by a conventional method such as the following composition.
마사지 크림의 조성: Composition of massage cream:
화학식 1의 화합물 0.1 중량%, 베타-1,3-글루칸 3.0 중량%, 밀납 10.0 중량%, 폴리솔베이트60 1.5 중량%, 피이지 60 경화피마자유 2.0 중량%. 솔비탄세스퀴올레이트 0.8 중량%, 유동파라핀 40.0 중량%, 스쿠알란 5.0 중량%, 카프릴릭/카프릭트리글리세라이드 4.0 중량%, 글리세린 5.0 중량%, 부틸렌글리콜 3.0 중량%, 프로필렌글리콜 3.0 중량%, 트리에탄올아민 0.2 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.1% by weight of the compound of formula (1), 3.0% by weight of beta-1,3-glucan, 10.0% by weight of wax, 1.5% by weight of polysorbate 60, 2.0% by weight of hardened castor oil. By weight of glycerin, 3.0% by weight of butylene glycol, 3.0% by weight of propylene glycol, 4.0% by weight of carrageenan / capric triglyceride, 0.8% by weight of sorbitan sesquioleate, 40.0% by weight of liquid paraffin, 0.2% by weight of triethanolamine, 0.05% by weight of preservative, 0.05% by weight of pigment, 0.05% by weight of fragrance, 100%
5. 팩의 제조5. Manufacture of pack
화학식 1의 화합물을 유효성분으로 포함하는 팩을 하기 조성과 같이 통상의 방법에 따라 제조하였다.A pack containing the compound of formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
팩의 조성:Composition of pack:
화학식 1의 화합물 0.2 중량%, 베타-1,3-글루칸 1.0 중량%, 폴리비닐알콜 13.0 중량%, 소듐카르복시메틸셀룰로오스 0.2 중량%, 글리세린 5.0 중량%, 알란토인 0.1 중량%, 에탄올 6.0 중량%, 피이지-12 노닐페닐에테르 0.3 중량%, 폴리솔베이트 60 0.3 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.2% by weight of the compound of formula (1), 1.0% by weight of beta-1,3-glucan, 13.0% by weight of polyvinyl alcohol, 0.2% by weight of sodium carboxymethyl cellulose, 5.0% by weight of glycerin, 0.1% by weight of allantoin, 0.3% by weight of iso-12 nonylphenyl ether, 0.3% by weight of polysorbate 60, 0.05% by weight of preservative, 0.05% by weight of pigment, 0.05% by weight of fragrance,
<제제예 3> 피부 외용제의 제조≪ Formulation Example 3 > Preparation of external preparation for skin
1. 젤의 제조1. Manufacture of gel
화학식 1의 화합물을 유효성분으로 포함하는 젤을 하기 조성과 같이 통상의 방법에 따라 제조하였다.A gel containing the compound of formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
젤의 조성:Composition of gel:
화학식 1의 화합물 0.1 중량%, 베타-1,3-글루칸 0.1 중량%, 에틸렌디아민초산나트륨 0.05 중량%, 글리세린 5.0 중량%, 카르복시비닐폴리머 0.3 중량%, 에탄올 5.0 중량%, 피이지-60 경화피마자유 0.5 중량%, 트리에탄올아민 0.3 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.1% by weight of the compound of formula (1), 0.1% by weight of beta-1,3-glucan, 0.05% by weight of sodium ethylenediaminetetraacetate, 5.0% by weight of glycerin, 0.3% by weight of carboxyvinyl polymer, 5.0% by weight of ethanol, 0.05 weight% of free, 0.3 weight% of triethanolamine, 0.05 weight% of preservative, 0.05 weight% of pigment, 0.05 weight% of perfume, 100 weight% of purified water,
2. 연고의 제조2. Manufacture of ointment
화학식 1의 화합물을 유효성분으로 포함하는 연고를 하기 조성과 같이 통상의 방법에 따라 제조하였다.Ointment containing the compound of formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
연고의 조성:Composition of ointment:
화학식 1의 화합물 0.5 중량%, 베타-1,3-글루칸 10.0 중량%, 밀납 10.0 중량%, 폴리솔베이트60 5.0 중량%, 피이지 60 경화피마자유 2.0 중량%, 솔비탄세스퀴올레이트 0.5 중량%, 바셀린 5.0 중량%, 유동파라핀 10.0 중량%, 스쿠알란 5.0 중량%, 쉐어버터 3.0 중량%, 카프릴릭/카프릭트리글리세라이드 5.0 중량%, 글리세린 10.0 중량%, 프로필렌글리콜 10.2 중량%, 트리에탄올아민 0.2 중량%, 방부제 0.05 중량%, 색소 0.05 중량%, 향료 0.05 중량%, 정제수 to 100 중량%0.5 wt% of the compound of formula (1), 10.0 wt% of beta-1,3-glucan, 10.0 wt% of wax, 5.0 wt% of polysorbate 60, 2.0 wt% of hydrogenated castor oil, 0.5 wt% of sorbitan sesquioleate, , 5.0% by weight of vaseline, 10.0% by weight of liquid paraffin, 5.0% by weight of squalane, 3.0% by weight of shea butter, 5.0% by weight of caprylic / capric triglyceride, 10.0% by weight of glycerin, 10.2% by weight of propylene glycol, 0.05% by weight of preservative, 0.05% by weight of pigment, 0.05% by weight of fragrance, 100% by weight of purified water,
3. 국소투여용 약제(겔 연고제) 의 제조3. Preparation of topical medicament (gel ointment)
화학식 1의 화합물을 유효성분으로 포함하는 겔 연고제를 하기 조성과 같이 통상의 방법에 따라 제조하였다.A gel ointment agent containing the compound of formula (1) as an active ingredient was prepared according to a conventional method as the following composition.
겔 연고제의 조성:Composition of gel ointment agent:
화학식 1의 화합물 0.5 중량%, 베타-1,3-글루칸 10.0 중량%, 폴리아크릴산(Carbopol 940) 1.5 중량%, 이소프로판올 5.0 중량%, 헥실렌글리콜 25.0 중량%, 트리에탄올아민 1.7 중량%, 탈이온수 to 100 중량%A mixture of 0.5% by weight of the compound of Formula 1, 10.0% by weight of beta-1,3-glucan, 1.5% by weight of polyacrylic acid (Carbopol 940), 5.0% by weight of isopropanol, 25.0% by weight of hexylene glycol, 1.7% by weight of triethanolamine, 100 wt%
4. 국소 투여용 약제(패취제)의 제조4. Preparation of topical medicines (patches)
화학식 1의 화합물을 유효성분으로 포함하는 패취제를 하기 조성과 같이 통상의 방법에 따라 제조하였다.A patch containing a compound of the formula (1) as an active ingredient was prepared according to a conventional method such as the following composition.
패취제의 조성:Composition of the patch:
화학식 1의 화합물 0.5 중량%, 베타-1,3-글루칸 3.0 중량%, 헥실렌글리콜 20.0 중량%, 디에틸아민 0.7 중량%, 폴리아크릴산(Carbopol 934P) 1.0 중량%, 아황산나트륨 0.1 중량%, 폴리옥시에틸렌라우릴에테르(E.O=9) 1.0 중량%, 폴리히드록시에틸렌세틸스테아릴에테르(Cetomacrogol 1000) 1.0 중량%, 점성의 파라핀 오일 2.5 중량%, 카프릴산에스테르/카프르산에스테르(Cetiol LC) 2.5 중량%, 폴리에틸렌글리콜400 3.0 중량%, 탈이온수 to 100 중량%0.5% by weight of the compound of the formula (1), 3.0% by weight of beta-1,3-glucan, 20.0% by weight of hexylene glycol, 0.7% by weight of diethylamine, 1.0% by weight of polyacrylic acid (Carbopol 934P) 1.0% by weight of oxyethylene lauryl ether (EO = 9), 1.0% by weight of polyhydroxyethylene cetyl stearyl ether (Cetomacrogol 1000), 2.5% by weight of viscous paraffin oil, caprylic acid ester / ) 2.5% by weight, polyethylene glycol 400 3.0% by weight, deionized water to 100%
Claims (10)
[화학식 1]
A composition for enhancing skin-protecting power comprising a compound represented by the following formula (1) as an active ingredient:
[Chemical Formula 1]
조성물은 피부방어력 증진용 약학, 화장료, 식품 또는 피부 외용제 제형 제조를 위한 것인, 피부방어력 증진용 조성물.
The method according to claim 1,
Wherein the composition is for the manufacture of a pharmaceutical, cosmetic, food or skin topical formulation for enhancing skin defense.
[화학식 1]
A skin whitening composition comprising a compound represented by the following formula (1) as an active ingredient:
[Chemical Formula 1]
조성물은 피부 미백용 약학, 화장료, 식품 또는 피부 외용제 제형 제조를 위한 것인, 피부 미백용 조성물.
The method of claim 3,
Wherein the composition is for the preparation of a skin whitening pharmacy, cosmetic, food, or external preparation for skin.
[화학식 1]
A composition for improving skin moisturization comprising a compound represented by the following formula (1) as an active ingredient:
[Chemical Formula 1]
조성물은 피부 보습 개선용 약학, 화장료, 식품 또는 피부 외용제 제형 제조를 위한 것인, 피부 보습 개선용 조성물.
6. The method of claim 5,
Wherein the composition is for the manufacture of a pharmaceutical, cosmetic, food or skin topical formulation for skin moisturisation improvement.
[화학식 1]
A composition for improving skin regeneration or wrinkling comprising a compound represented by the following formula (1) as an active ingredient:
[Chemical Formula 1]
조성물은 피부 재생 또는 주름 개선용 약학, 화장료, 식품 또는 피부 외용제 제형 제조를 위한 것인, 피부 재생 또는 주름 개선용 조성물.
8. The method of claim 7,
A composition for skin regeneration or wrinkle improvement, wherein the composition is for the manufacture of a pharmaceutical, cosmetic, food or external preparation for skin regeneration or wrinkle improvement.
[화학식 1]
A composition for promoting skin elasticity comprising a compound represented by the following formula (1) as an active ingredient:
[Chemical Formula 1]
조성물은 피부 탄력 증진용 약학, 화장료, 식품 또는 피부 외용제 제형 제조를 위한 것인, 피부 탄력 증진용 조성물.
10. The method of claim 9,
Wherein the composition is for the preparation of a pharmaceutical composition for promoting skin elasticity, a cosmetic composition, a food or an external preparation for skin.
Priority Applications (1)
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KR1020160042212A KR20170114736A (en) | 2016-04-06 | 2016-04-06 | Composition for improving skin conditions |
Applications Claiming Priority (1)
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KR1020160042212A KR20170114736A (en) | 2016-04-06 | 2016-04-06 | Composition for improving skin conditions |
Publications (1)
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KR20170114736A true KR20170114736A (en) | 2017-10-16 |
Family
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KR1020160042212A KR20170114736A (en) | 2016-04-06 | 2016-04-06 | Composition for improving skin conditions |
Country Status (1)
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KR (1) | KR20170114736A (en) |
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2016
- 2016-04-06 KR KR1020160042212A patent/KR20170114736A/en not_active Application Discontinuation
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