KR20150050984A - Cosmetic composition and external composition comprising alkaloid for anti-inflammatory - Google Patents
Cosmetic composition and external composition comprising alkaloid for anti-inflammatory Download PDFInfo
- Publication number
- KR20150050984A KR20150050984A KR1020130132310A KR20130132310A KR20150050984A KR 20150050984 A KR20150050984 A KR 20150050984A KR 1020130132310 A KR1020130132310 A KR 1020130132310A KR 20130132310 A KR20130132310 A KR 20130132310A KR 20150050984 A KR20150050984 A KR 20150050984A
- Authority
- KR
- South Korea
- Prior art keywords
- alkaloid
- acid
- inflammatory
- skin
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/35—Ketones, e.g. benzophenone
-
- 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
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
- A61K8/492—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid having condensed rings, e.g. indol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Dermatology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Cosmetics (AREA)
Abstract
Description
본 발명은 알칼로이드(alkaloid)를 유효성분으로 포함하는 항염 화장료 조성물 또는 항염 피부 외용제에 관한 것이다.
The present invention relates to an anti-inflammatory cosmetic composition comprising an alkaloid as an active ingredient or an anti-inflammatory external preparation for skin.
화장품은 피부를 보호하고 미화 청결을 위해 사용되는 제품이지만 화장품 조성물을 자세하게 살펴보면 피부 보호 목적과는 상이한 성분들이 제품 형성에 불가결한 존재로서 사용된다. 예를 들면 계면활성제, 방부제, 향료, 자외선 차단제, 색소 및 기타 효능, 효과를 부여하기 위해 쓰이는 여러 가지 성분들을 들 수 있다. 이러한 성분들은 일반적으로 피부에 염증, 뾰루지, 부종 등 여러 가지 부작용을 발생시키는 것으로 알려져 있다(Maibach, H. I., Contact Dermatitis, 6; (1980) 369-404). 또한 체내로부터 배출되는 피지 성분, 땀 성분 및 화장품 성분 중의 지방산, 고급 알콜, 단백질 등이 피부상에 존재하는 피부 상재균들에 의해 독성이 강한 물질로 분해되어 이들에 의해 피부 염증이 유발될 수도 있다. 특히 최근에는 기능성 화장품이 개발되면서 AHA(알파 하이드로시산), 레티놀, 알부틴 등의 성분을 포함한 제품들 즉, 피부에 다소의 부작용이 있더라도 각종 기능을 가진 다양한 기능성 화장품이 시판되고 있다.Cosmetics are products used to protect the skin and clean the hair, but when the cosmetic composition is examined in detail, ingredients different from the purpose of skin protection are used as an indispensable substance for product formation. Examples include surfactants, preservatives, fragrances, sunscreens, pigments, and other ingredients used to impart other benefits and effects. These ingredients are generally known to cause skin irritation, rashes, edema and many other side effects (Maibach, H. I., Contact Dermatitis, 6; (1980) 369-404). In addition, sebum components, sweat components, cosmetic ingredient fatty acids, higher alcohols, proteins, etc., emitted from the body are decomposed into highly toxic substances by the skin-damaging bacteria existing on the skin, thereby causing skin inflammation . In recent years, functional cosmetics have been developed, and various functional cosmetics having various functions have been put on the market even if there are some side effects such as AHA (alpha hydroxy acid), retinol, and arbutin.
현재까지 항염의 목적으로 이용되는 물질로는 비스테로이드계로 프루폐나믹산(flufenamic acid), 이부프로펜(ibuprofen), 벤지다민(benzydamine), 인도메타신(indomethacin) 등이 있고, 스테로이드계로 프레드니솔론(prednisolone) 및 덱사메타손(dexamethasone) 등이 있고, 그 외 알란토인, 아즈엔, 하이드로코티존, 감초산 및 그 유도체(β-글리칠레친산, 글리칠레친산 유도체) 등이 항염증에 효과가 있는 것으로 알려져 있다(광정무부, 신화장품학, 남산당, p162, 1993). 그러나 스테로이드계 물질은 피부에 대한 안전성 면에서 대부분 문제점을 안고 있어서 그 사용량이 제한되고 있으며(김창종, 병태심리학, 한림상사, p61-69, 1988), 인도메타신은 화장료에는 사용할 수 없고, 감초산 및 그 유도체는 안정화시키기 어렵거나 용해도가 좋지 않아 실제 제품 적용 시 농도의 제한으로 인하여 실질적인 효과를 거두기 어려운 점이 있다.
To date, substances used for antiinflammatory purposes include nonsteroidal antiinflammatory agents such as flufenamic acid, ibuprofen, benzydamine, and indomethacin, and steroids such as prednisolone and Dexamethasone, and other allantoin, azene, hydrocotizone, licorice acid, and derivatives thereof (? -Glycyrrhetinic acid, glycyrrhetinic acid derivative) New Cosmetics, Namsan, p. 162, 1993). However, the use of steroids has been limited in terms of safety to skin (Kim Chang-jong, Pathology Psychology, Hallym Company, p61-69, 1988). Indomethacin can not be used for cosmetics, The derivatives are difficult to stabilize or have poor solubility, and therefore, it is difficult to achieve a practical effect due to the limitation of the concentration when the product is actually applied.
이에, 본 발명은 항염 효과가 뛰어날 뿐만 아니라, 피부에도 안전하고, 화장료 조성물 또는 피부 외용제로 제형화도 용이한 물질을 발굴하고, 이를 포함한 항염 화장료 조성물 또는 항염 피부 외용제를 제공하고자 한다.
Accordingly, it is an object of the present invention to provide a novel anti-inflammatory cosmetic composition or an anti-inflammatory external preparation for skin which is not only excellent in anti-inflammatory effect but also safe for skin, easily formable as a cosmetic composition or external preparation for skin.
상기 과제를 해결하기 위한 수단으로서, 본 발명은 알칼로이드(alkaloid)를 유효성분으로 포함하는 항염 화장료 조성물 또는 항염 피부 외용제를 제공한다.As means for solving the above problems, the present invention provides an anti-inflammatory cosmetic composition comprising an alkaloid as an active ingredient or an anti-inflammatory external preparation for skin.
상기 알칼로이드(alkaloid)는 질소를 포함하고 있는 염기성 유기화합물로서, 단백질 아미노산의 이차대사산물의 일종으로서, 박테리아, 균, 식물 및 동물을 비롯한 다양한 생물군에서 얻을 수 있다. 피리딘, 퀴놀린, 이소퀴놀린, 피롤리딘, 피페리딘, 인돌, 프로판, 푸린 등의 고리구조를 갖는 것이 많으며, 대표적인 알칼로이드로는 카페인(caffeine), 모르핀 (morphine), 니코틴(nicotine), 스트리크닌(strychnine), 아트로핀 (atropine), 코카인(cocaine), 키닌(kinin)이 있으며, 이들은 주로 신경조직이나, 심장근육, 호흡기 조직의 흥분을 야기하고, 마약이나 의약품으로 주로 사용된다. 그 외 알칼로이드의 효과로 항염, 항균 및 항암 활성이 알려졌으며, 이에 대한 연구가 진행되고 있다. The alkaloid is a basic organic compound containing nitrogen and is a kind of secondary metabolites of protein amino acids and can be obtained from various biological groups including bacteria, fungi, plants and animals. Many of them have a cyclic structure such as pyridine, quinoline, isoquinoline, pyrrolidine, piperidine, indole, propane, purine, etc. Representative alkaloids include caffeine, morphine, nicotine, strychnine, atropine, cocaine, and kinin, which cause excitation of nerve tissue, heart muscle, respiratory tissue, and are mainly used as drugs and medicines. Anti-inflammation, antimicrobial and anticancer activities have been known by the effects of other alkaloids, and studies are underway.
한편, 본 발명자들은 항염 효과도 우수할 뿐만 아니라, 피부에도 안전하고, 화장료 조성물 또는 피부 외용제로 제형화도 용이한 물질을 발굴하는 과정에서 알칼로이드(alkaloid)가 항염 효과가 뛰어나면서 특이취가 적고, 피부에 안전한 성분임을 발견하여, 본 발명을 완성하였다. 하기 실시예를 통해, 본 발명자들은 본 발명에 따른 알칼로이드가 우수한 시클로옥시게나제 저해 효과 및 항염 효과가 있음을 확인하였다(실시예 1, 2). 또한 인체에 대한 피부 안전성이 매우 우수함을 확인하였다(실시예 3, 4).On the other hand, the inventors of the present invention have found that alkaloids are excellent in anti-inflammatory effect and have little specific odor in the process of finding substances which are safe for skin, easily formulated into cosmetic compositions or external preparations for skin, And thus the present invention has been completed. Through the following examples, the present inventors confirmed that the alkaloid according to the present invention had excellent cyclooxygenase inhibitory effect and anti-inflammatory effect (Examples 1 and 2). It was also confirmed that skin safety to human body was excellent (Examples 3 and 4).
본 발명에 따른 알칼로이드(alkaloid)는 시판품을 사용하거나, 식물로부터 분리, 반합성 또는 합성을 통해 제조된 것일 수 있다. 이에 제한되지 않으나, 상기 식물은 윈터체리(withania somnifera, ashwagandha) 및 그린볼야자(Castanospermum austral)일 수 있다. 또한 이에 제한되지 않으나, 예를 들어, 상기 알칼로이드는 이소펠레티에린(isopelletierine), 아나페린(anaferine) 또는 카스타노스퍼민(Castanospermine)일 수 있다. The alkaloid according to the present invention may be commercially available, or may be one prepared by separation, semi-synthesis or synthesis from a plant. The plant may be, but is not limited to, winter cherry (withania somnifera, ashwagandha) and green ball palm (Castanospermum austral). For example, but not limited to, the alkaloid may be isopelletierine, anaferine, or Castanospermine.
본 발명에 따른 알칼로이드(alkaloid)는 시판품을 사용하거나 공지된 방법에 근거하여 제조할 수 있다. 알칼로이드(alkaloid)의 제조는 당업자에게 자명한 범위 내에서 변경될 수 있고, 본 발명은 그 범위를 포함한다. The alkaloid according to the present invention can be manufactured using a commercial product or based on known methods. The preparation of alkaloids can be varied within a range that is obvious to a person skilled in the art, and the present invention includes the scope thereof.
예를 들어, 본 발명은 식물의 추출물로부터 분리 및 정제된 것일 수 있다.For example, the present invention may be those isolated and purified from plant extracts.
식물에서 알칼로이드(alkaloid)를 추출하기 위해 사용되는 추출용매는 이에 제한되는 것은 아니나, 물, 유기용매 또는 이들의 혼합물로부터 선택되는 용매일 수 있다. 상기 유기용매는 탄소수 1 내지 5의 알코올, 에틸아세테이트, 아세톤 등의 극성용매와 에테르, 클로로포름, 벤젠, 헥산 또는 디클로로메탄 등의 비극성용매 또는 이들의 혼합용매일 수 있다. 예를 들어, 상기 탄소수 1 내지 5의 알코올은 메탄올, 에탄올, 프로판올, 부탄올 또는 이소프로판올 등으로부터 선택될 수 있다. Extraction solvents used to extract alkaloids from plants include, but are not limited to, solvents selected from water, organic solvents or mixtures thereof. The organic solvent may be a polar solvent such as an alcohol having 1 to 5 carbon atoms, ethyl acetate or acetone, a non-polar solvent such as ether, chloroform, benzene, hexane or dichloromethane, or a mixture thereof. For example, the alcohol having 1 to 5 carbon atoms may be selected from methanol, ethanol, propanol, butanol or isopropanol.
또한 본 발명에 따른 알칼로이드(alkaloid)는 상기 추출용매를 이용하여 추출된 1차 추출물을 극성이 다른 추출용매를 이용하여 다시 분획한 분획물일 수 있다. 예를 들어, 극성이 다른 용매는 에테르, 벤젠 또는 헥산일 수 있다.In addition, the alkaloid according to the present invention may be a fraction obtained by further fractionating the primary extract extracted using the extraction solvent with an extraction solvent having a different polarity. For example, solvents with different polarity may be ether, benzene or hexane.
상기 분획 시 용매는 2종 이상 사용할 수 있으며, 용매의 극성에 따라 순차적으로 사용하거나 혼합하여 사용하여, 각 용매 추출물을 제조할 수 있으나, 이에 제한되지 않는다.Two or more kinds of solvents may be used for the fractionation, and the solvent extracts may be sequentially used or mixed according to the polarity of the solvent, but not limited thereto.
상기 제조된 추출물 또는 상기 분획과정을 수행하여 수득한 분획물은 이후, 통상의 분리정제법에 따라 유효성분을 분리 및 정제할 수 있다. 이에 제한되는 것은 아니나, 액체크로마토그래피(High Performance Liquid Chromatography, HPLC)를 이용할 수 있다.The thus-prepared extract or the fraction obtained by performing the fractionation process can then separate and purify the active ingredient according to a conventional separation and purification method. But is not limited to, high performance liquid chromatography (HPLC) can be used.
상기의 방법을 통해 제조된 알칼로이드(alkaloid)는 염의 형태일 수 있다. 상기 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, 타르타산, 옥살산, 시트르산, 글리콜산, 글루쿠론산, 아스코르브산, 벤조산, 프탈산, 살리실산, 안트라닐산, 디클로로아세트산, 아미노옥시 아세트산, 벤젠술폰산, p-톨루엔술폰산 및 메탄술폰산계 염으로 이루어진 군으로 선택되는 하나 이상일 수 있다. 상기 무기산은 예를 들면 염산, 브롬산, 황산, 인산, 질산, 탄산 및 붕산계 염으로 이루어진 군으로 부터 선택되는 하나 이상일 수 있다. 바람직하게는 염산염 또는 아세트산염 형태일 수 있으며, 보다 바람직하게는 염산염 형태일 수 있다.The alkaloid prepared by the above method may be in the form of a salt. The salt 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, malic acid, maleic acid, malonic acid, fumaric acid , Succinic acid, succinic monoamide, glutamic acid, tartaric acid, oxalic acid, citric acid, glycolic acid, gluconic acid, ascorbic acid, benzoic acid, phthalic acid, salicylic acid, anthranilic acid, dichloroacetic acid, aminooxyacetic acid, benzenesulfonic acid, Methanesulfonic acid-based salts, and methanesulfonic acid-based salts. The inorganic acid may be at least one selected from the group consisting of 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.
위와는 별도로 추가적으로 염이 가능한 형태는 가바염, 가바펜틴염, 프레가발린염, 니코틴산염, 아디페이트염, 헤미말론산염, 시스테인염, 아세틸시스테인염, 메티오닌염, 아르기닌염, 라이신염, 오르니틴염 또는 아스파르트산염 등이 있다.Separately, additionally saltable forms include, but are not limited to, the salts of gabapentin, gabapentin, pregabalin, nicotinate, adipate, hemimarate, cysteine, acetylcysteine, methionine, arginine, lysine, Aspartate and the like.
본 발명에 있어서, "염증"이란, 세포나 조직이 어떠한 원인에 의해 손상을 받으면 그 반응을 최소화하고 손상된 부위를 원상으로 회복시키려는 일련의 방어 목적으로 나타나는 현상을 의미하는 것으로, 신경, 혈관, 임파관, 체액 반응, 세포 반응을 일으켜 결과적으로 통증, 부종, 발적, 발열 등을 일으켜 기능장애를 유발하는 것을 통칭한다. 상기 염증으로 인한 질환은 각종 피부염, 알레르기, 전신성 홍반성 낭창, 망막염, 위염, 간염, 장염, 췌장염 및 신장염으로 이루어진 군 중에서 선택된 1종 이상일 수 있고, 상기 알레르기는 과민증(anaphylaxis), 알러지성 비염(allergic rhinitis), 천식(asthma), 알러지성 결막염, 알러지성 피부염, 아토피성 피부염(atopic dermatitis), 접촉성 피부염, 두드러기(urticaria), 곤충 알러지, 식품 알러지 및 약품 알러지를 포함한다. In the present invention, the term "inflammation" means a phenomenon appearing for a series of defensive purposes for minimizing the reaction of a cell or a tissue caused by any cause and restoring the damaged region to the original state. , Body fluid reaction, and cell reaction, resulting in pain, edema, redness, fever, etc., resulting in dysfunction. The disease caused by inflammation may be at least one selected from the group consisting of various dermatitis, allergies, systemic lupus erythematosus, retinitis, gastritis, hepatitis, enteritis, pancreatitis and nephritis. The allergies include anaphylaxis, allergic rhinitis allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, atopic dermatitis, contact dermatitis, urticaria, insect allergies, food allergies and drug allergies.
상기 염증은 생체 내에서 다양한 생화학적 현상에 의해 발생되며, 특히, 아라키돈산(arachidonic acid)으로부터 프로스타글란딘(prostaglandin)을 생합성하는데 관련된 효소인 시클로옥시게나제(Cyclooxygenase, COX)와 L-아르기닌(L-arginin)으로부터 니트릭옥사이드(nitric oxide, NO)를 생성시키는 효소인 니트릭옥사이드 신타제(nitric oxide synthase, NOS)는 염증 반응을 매개하는데 있어서 중요한 역할을 하고 있는 것으로 알려져 있다. The inflammation is caused by various biochemical phenomena in vivo. In particular, the inflammation is caused by an enzyme involved in biosynthesis of prostaglandin from arachidonic acid, such as cyclooxygenase (COX) and L-arginine (L- It is known that nitric oxide synthase (NOS), an enzyme that produces nitric oxide (NO) from arginine, plays an important role in mediating the inflammatory response.
본 발명에서의 용어, "프로스타글란딘(prostaglandin, PG)"은 몸속에서 합성되는 일종의 생리활성 호르몬으로서, 염증반응을 조절하는 기능이 있다. 상기 프로스타글란딘은 PG1, PG2, PG3로 3종류가 있으며, PG1과 PG3는 염증을 억제하고, PG2는 염증을 유발시킨다. 상기 프로스타글란딘은 아라키돈산을 전구체로 하여 시클로옥시게나제(Cyclooxygenase, COX)를 통해 생합성 된다.The term " prostaglandin (PG) "in the present invention is a kind of physiologically active hormone synthesized in the body and has a function of regulating the inflammatory reaction. The prostaglandins are classified into PG1, PG2 and PG3, PG1 and PG3 inhibit inflammation, and PG2 induce inflammation. The prostaglandin is biosynthesized through cyclooxygenase (COX) using arachidonic acid as a precursor.
본 발명에서의 용어, "시클로옥시게나제(Cyclooxygenase, COX)"는 프로스타글란딘의 합성의 제1단계를 촉매하는 효소로서, 아라키돈산에 2분자의 산소를 도입하여, PG2를 합성하며, 프로스타글란딘 엔도페록시드 신타아제라고도 불린다. 한편 시클로옥시게나제(Cyclooxygenase, COX)도 2종류의 이소형태가 존재하는데 시클로옥시게나제-1(Cyclooxygenase-1; COX-1)는 세포 내에 항상 존재하여 세포보호 작용에 필요한 프로스타글란딘(PGs)을 합성하는 작용을 하는 반면 COX-2는 염증 반응 시 세포내에서 급격히 증가하여 염증 반응에 중요한 역할을 수행하는 것으로 알려져 있다.The term "cyclooxygenase (COX)" in the present invention is an enzyme that catalyzes the first step of the synthesis of prostaglandin, wherein two molecules of oxygen are introduced into arachidonic acid to synthesize PG2, and prostaglandin endoperox It is also called seed synthase. Cyclooxygenase-1 (COX-1), which is always present in cells, contains prostaglandins (PGs) required for cytoprotective action, while cyclooxygenase COX-2 is known to play an important role in the inflammatory response by increasing rapidly in the cell during the inflammatory reaction.
본 발명에서의 용어, "니트릭옥사이드(nitric oxide, NO)"는 각종 싸이토카인이나 외부 자극에 의해 유도되는 iNOS(induced NOS)에 의해 발생되며, 세포독성이나 각종 염증 반응을 일으키는 것으로 알려져 있다. 또한, 만성염증은 iNOS 활성 증가와 관련이 있다고 알려져 있다(Appleton L.et al Adv. Phamacol., 35. 27-28.1996). The term "nitric oxide (NO)" in the present invention is caused by various cytokines or iNOS induced by external stimuli, and is known to cause cytotoxicity or various inflammatory responses. Chronic inflammation is also known to be associated with increased iNOS activity (Appleton L. et al. Pharmacol., 35. 27-28.1996).
본 발명에 따른 알칼로이드는 시클로옥시게나제(Cyclooxygenase, COX) 저해 활성을 가짐으로써, 특히, 프로스타글란딘(prostaglandin)류의 생합성을 매개로 한 염증에 효과적이다.The alkaloids according to the present invention have a cyclooxygenase (COX) inhibitory activity, and are thus particularly effective for inflammation mediated by biosynthesis of prostaglandins.
본 발명의 항염 조성물은 유효량의 알칼로이드를 포함할 때, 바람직한 항염 효과를 제공할 수 있다. 본 발명에 있어서, "유효량"이라 함은 충분한 시클로옥시게나제(Cyclooxygenase, COX) 저해 활성을 나타낼 수 있는 양을 의미한다. 예컨대, 본 발명의 항염 조성물에 포함되는 상기 알칼로이드의 유효량은 전체 조성물 100 중량부에 대하여, 0.001 내지 20 중량부로 포함할 수 있다. 예를 들어, 0.001 중량부 내지 10 중량부, 0.01 중량부 내지 20 중량부, 0.01 중량부 내지 10 중량부 및 0.1 중량부 내지 10 중량부일 수 있다. 이는 상기 알칼로이드를 0.001 중량부 미만으로 포함할 경우에는 충분한 항염 효과를 기대할 수 없고, 20 중량부를 초과하여 포함할 경우에는 알러지 등 원치 않는 반응이 발생하거나 피부 안전성에 문제가 있을 수 있으므로 이를 방지하기 위한 것이다. 상기와 같은 조성은 반드시 이에 한정되는 것은 아니고, 상기 조성물의 목적, 제품화되는 형태 및 적용 대상자의 상태에 따라 변할 수 있다. The anti-inflammatory composition of the present invention can provide a desirable anti-inflammatory effect when it contains an effective amount of alkaloid. In the present invention, "effective amount" means an amount capable of exhibiting sufficient cyclooxygenase (COX) inhibitory activity. For example, the effective amount of the alkaloid contained in the anti-inflammatory composition of the present invention may be 0.001 to 20 parts by weight based on 100 parts by weight of the total composition. For example, 0.001 to 10 parts by weight, 0.01 to 20 parts by weight, 0.01 to 10 parts by weight, and 0.1 to 10 parts by weight. If the alkaloid is contained in an amount of less than 0.001 part by weight, a sufficient anti-inflammatory effect can not be expected. If the alkaloid is contained in an amount exceeding 20 parts by weight, an unwanted reaction such as allergy may occur or there may be a problem in skin safety. will be. The composition is not necessarily limited to this, and may vary depending on the purpose of the composition, the form of the composition, and the condition of the applicant.
한편, 본 발명의 조성물은 공지된 항염 효과를 나타내는 성분이나, 항염 효과를 증강하는 성분을 1종 이상 추가로 함유할 수 있다. On the other hand, the composition of the present invention may contain one or more components which exhibit a known anti-inflammatory effect or a component that enhances the anti-inflammatory effect.
추가적인 항염 성분을 포함하게 되면, 본 발명의 항염 효과는 더욱 증진될 수 있을 것이다. 당업계에 공지된 항염 성분으로서, 비스테로이드계로 이부프로펜(ibuprofen), 플루페나믹산(flufenamic acid) 또는 인도메타신(indomethacin), 스테로이드계로 프레드니솔론(prednisolone) 또는 덱사메타손(dexamethasone), 그 외 알란토인, 아즈엔, 하이드로코티존, 감초산 및 그 유도체로 구성되는 군으로부터 선택되는 1종 또는 2종 이상의 성분을 추가로 포함할 수 있다. 상기 추가의 항염 성분은 상기 나열한 성분 외에도 이들과 동등한 효과를 나타내는 이들의 유사체 등을 모두 포함한다. 또한 화장료 조성물에서 사용할 수 있는 공지의 항염 성분으로서, 히알루론산(Hyaluronic acid), 다프네틴(Daphnetin), 글리시리진(Glycyrrhizin), 케르세틴(Quercetin), 로즈마린산(Rosmarinic acid), 마데카식산(Madecassic acid), 카마줄렌(Chamazulene), 바이칼레인(Bicalein), 에모딘(Emodin), 아스타잔틴(Astaxanthin), 노르베르게닌(norbergenin), 4-O-메틸호노키올(4-O-methylhonokiol), 폴리다틴(polydatin), 페룰산(ferulic acid), 2-메톡시신남알데하이드(2-methoxycinnamaldehyde), 2,4-다이하이드록시아세토페논(2,4-dihydroxyacetophenone), 터피넨-4-올(terpinen-4-ol) 및 그 유도체로 구성되는 군으로부터 선택되는 1종 또는 2종 이상의 성분을 추가로 포함할 수 있다. 상기 추가의 항염 성분은 상기 나열한 성분 외에도 이들과 동등한 효과를 나타내는 이들의 유사체 및 식물 추출물 등을 모두 포함할 수 있다. If the additional anti-inflammatory component is included, the anti-inflammatory effect of the present invention can be further enhanced. As anti-inflammatory ingredients known in the art, ibuprofen, flufenamic acid or indomethacin in a non-steroid system, prednisolone or dexamethasone in a steroid system, other allantoin, , Hydrocortisone, licorice acid, and derivatives thereof. The additional anti-inflammatory component includes all of the above-listed components and analogs thereof exhibiting an equivalent effect thereto. In addition, as a known anti-inflammatory component which can be used in cosmetic compositions, there may be mentioned hyaluronic acid, Daphnetin, Glycyrrhizin, Quercetin, Rosmarinic acid, Madecassic acid, Carmine julren (Chamazulene), Baikal lane (Bicalein), the emodine (Emodin), astaxanthin (astaxanthin), Nord bereuge Nin (norbergenin), 4-O- methyl hono kiol (4-O-methylhonokiol), poly datin ( polydatin, ferulic acid, 2-methoxycinnamaldehyde, 2,4-dihydroxyacetophenone, terpinen-4-ol, ol, and derivatives thereof. The present invention is further illustrated by the following examples. The additional anti-inflammatory component may include all of the analogues and plant extracts exhibiting the same effects as those listed above.
추가된 성분은 전체 조성물 100 중량부에 대하여 0.0001 내지 10중량부로 포함될 수 있을 것이며, 상기 함량 범위는 시클로옥시게나제(Cyclooxygenase, COX)의 활성, 피부 안전성, 제형화 시의 용이성 등의 요건에 따라 조절될 수 있을 것이다. The added components may be contained in an amount of 0.0001 to 10 parts by weight based on 100 parts by weight of the total composition. The content of the added components may vary according to requirements such as the activity of cyclooxygenase (COX), skin safety, It can be adjusted.
본 발명에 따른 화장료 조성물 또는 피부 외용제는 통상의 방법을 통해 제형화될 수 있다. 피부 외용제로의 제형화시에는 Remington's Pharmaceutical Science, Mack Publishing Company, Easton PA에 개시되어 있는 내용을 참조할 수 있으며, 화장품으로 제형화시에는 International cosmetic ingredient dictionary, 6th ed., The cosmetic, Toiletry and Fragrance Association, Inc., Washington, 1995에 개시되어 있는 내용을 참조할 수 있을 것이다. 상기 문헌들은 본 명세서의 일부로서 포함된다. The cosmetic composition or external preparation for skin according to the present invention can be formulated by a conventional method. For formulation into a skin external preparation, reference may be made to the contents disclosed in Remington's Pharmaceutical Science, Mack Publishing Company, Easton PA, and International Cosmetic ingredient dictionary, 6th ed., The cosmetic, Toiletry and Fragrance Association, Inc., Washington, 1995, which is incorporated herein by reference in its entirety. Which are incorporated herein by reference.
이에 제한되는 것은 아니나, 상기 화장료 조성물은 일반적인 유화 제형 및 가용화 제형의 형태로 제조할 수 있다. 예컨대, 유연 화장수 또는 영양 화장수 등의 화장수; 훼이셜 로션, 바디로션 등의 유액; 영양 크림, 수분 크림, 아이 크림 등의 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 오일 등의 메이크업 제거제; 또는 클렌징 폼, 비누, 바디워시 등의 세정제 등의 제형을 가질 수 있다. 또한 상기 피부 외용제는 이에 제한되는 것은 아니나, 연고, 패취, 겔, 크림 또는 분무제와 같은 제형을 가질 수 있다. The cosmetic composition may be prepared in the form of a general emulsified formulation and a solubilized formulation. For example, lotion such as soft lotion or nutrition lotion; Lotion such as facial lotion, body lotion; Nourishing cream, moisture cream, cream such as eye cream; essence; Makeup ointment; spray; Gel; pack; Sunscreen; Makeup base; A foundation such as a liquid type, a solid type or a spray type; powder; Make-up removers such as cleansing creams, cleansing lotions and cleansing oils; Or cleansing agents such as cleansing foams, soaps, bodywashes, and the like. The external preparation for skin may have a formulation such as, but not limited to, ointments, patches, gels, creams or sprays.
상기 제형에 따라 유효성분의 함량이 달라질 수 있다. 상기 화장료 조성물을 예로 들면, 유효성분이 단기간 내에 피부에 머무르게 되는 메이크업 제거제, 세정제 등과 같은 워시-오프(wash-off) 타입의 화장품의 경우에는 비교적 높은 농도의 상기 알칼로이드를 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 알칼로이드를 포함해도 무방할 것이다. The content of the active ingredient may be varied according to the formulation. For example, the cosmetic composition may contain a relatively high concentration of the alkaloid in the case of a wash-off type cosmetic such as a make-up removing agent, a detergent or the like in which the active ingredient remains on the skin in a short period of time. On the other hand, leave-on type cosmetics such as cosmetics, milky lotions, creams, and essences whose effective ingredients stay on the skin for a long period of time may contain lower alkaloids than wash-off type cosmetics will be.
또한 통상적으로 화장료 조성물 또는 피부 외용제에 사용되는 안정화제, 용해제, 비타민, 안료 또는 향료 등의 보조제 또는 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 및 화장품 또는 피부 외용제에 통상적으로 사용되는 임의의 다른 성분과 같은 화장품학 분야 또는 피부 과학 분야에서 통상적으로 사용되는 보조제를 함유할 수 있다. 또한 상기 성분들은 화장품학 분야 또는 피부 과학 분야에서 일반적으로 사용되는 양으로 도입될 수 있다.
In addition, it may further include adjuvants or carriers such as stabilizers, solubilizers, vitamins, pigments or fragrances which are conventionally used in cosmetic compositions or external skin preparations. A surfactant, a water, an ionic or nonionic emulsifier, a filler, a metal, or a combination thereof. The present invention also relates to the use of the above- A cosmetic field such as an ionic sequestering and chelating agent, a preservative, a vitamin, a barrier, a wetting agent, a essential oil, a dye, a pigment, a hydrophilic or lipophilic active agent, a lipid vesicle and any other ingredient commonly used in cosmetic or dermatological applications, May contain adjuvants conventionally used in the field of dermatology. The components can also be introduced in amounts commonly used in the cosmetics field or the skin science field.
본 발명에 따른 알칼로이드(alkaloid)는 우수한 시클로옥시게나제(Cyclooxygenase, COX) 저해 및 염증 억제 효과를 나타내고, 기존의 항염제에 비해서 세포독성 및 피부 안전성에서 매우 우수하였다.
The alkaloids according to the present invention exhibit excellent cyclooxygenase (COX) inhibition and inflammation inhibitory effects, and are superior in cytotoxicity and skin safety to the conventional anti-inflammatory agents.
본 발명의 이점 및 특징, 그리고 그것들을 달성하는 방법은 상세하게 후술되어 있는 실시예 및 제조예들을 참조하면 명확해질 것이다. 그러나 본 발명은 이하에서 개시되는 실시예 및 제조예에 한정되는 것이 아니라, 서로 다른 다양한 형태로 구현될 것이며, 단지 본 발명의 개시가 완전하도록 하고, 본 발명이 속하는 기술분야에서 통상의 지식을 가진 자에게 발명의 범주를 완전하게 알려주기 위해 제공되는 것이다.
Advantages and features of the present invention and methods of achieving them will become apparent with reference to the embodiments and preparations which will be described in detail below. However, it should be understood that the present invention is not limited to the embodiments and manufacturing examples described below, but may be embodied in many different forms and should not be construed as being limited to the exemplary embodiments set forth herein. It is provided to inform the person completely of the scope of the invention.
[실시예 1][Example 1]
시클로옥시게나제(Cyclooxygenase, COX) 저해효과Cyclooxygenase (COX) inhibitory effect
본 발명에서는 시클로옥시게나제(Cyclooxygenase, COX)를 Pel-Freeze사의 양 저정낭(sheep seminal vesicle)으로부터 추출하여 사용하였다. 본 발명에 따른 시클로옥시게나제(Cyclooxygenase, COX)는 상기 양 저정낭을 분쇄 후 3000rpm에서 10분 동안 원심 분리하여 상등액을 취한 후, 상등액을 10000rpm에서 1 시간 동안 원심 분리하여 침전물을 분리하고 트리스 완충액 (0.1M, pH 8.0)에 녹여 제조되었다. In the present invention, cyclooxygenase (COX) was extracted from sheep seminal vesicles of Pel-Freeze. The cyclooxygenase (COX) according to the present invention was prepared by crushing the two hypocotyls and then centrifuging at 3000 rpm for 10 minutes to take up the supernatant. The supernatant was centrifuged at 10000 rpm for 1 hour to separate precipitates, (0.1 M, pH 8.0).
25㎍ 헤모글로빈을 트리스 완충용액(0.1M, pH 8.0) 100mL에 넣고 1.1mM 아라키돈산이 되도록 기질을 만든 후, 상기 기질에10,000 unit의 시클로옥시게나제 10 ㎕를 넣는다. 여기에 이소펠레티에린, 아나페린 또는 카스타노스퍼민을 각각 0.5ppm, 10ppm, 50ppm씩 첨가한 후, 측정기(Yellow Spring Instrument company. Model 53 oxygen monitor)로 초기 산소 소모량을 측정하여 시클로옥시게나제 활성을 확인하였다. 그 결과를 하기 표 1에 나타내었다.
25 μg of hemoglobin is added to 100 mL of Tris buffer solution (0.1 M, pH 8.0) to make a substrate to be 1.1 mM arachidonic acid, and then 10 μl of 10,000 units of cyclooxygenase is added to the substrate. After adding 0.5 ppm, 10 ppm and 50 ppm of isopelletriene, anapelin or carnano-spermin, respectively, the initial oxygen consumption was measured with a measuring device (Yellow Spring Instrument company, Model 53 oxygen monitor) to measure the cyclooxygenase activity Respectively. The results are shown in Table 1 below.
n=3
n = 3
상기 표 1에서 볼 수 있듯이, 50ppm일 때, 시클로옥시게나제에 대해 음성대조군 대비 이소펠레티에린 44%, 아나페린 48%, 카스타노스퍼민은 51%의 저해효과를 나타냄을 확인할 수 있었다.
As shown in Table 1, it was confirmed that 44 ppm of isopelletriene, 48 percent of anapelin, and 51 percent of castanospermine had an inhibitory effect on cyclooxygenase at 50 ppm, compared with the negative control.
[실시예 2][Example 2]
항염 효과 시험Anti-inflammatory effect test
아라키돈산(arachidonic acid)을 이용한 평가법(A. Crummey, G. P. Harper, E. A. Boyle and F. R. Mangan. Inhibition of arachidonic acid-induced ear edema as a model for assessing topical anti-inflammatory compound. Agents and Actions 1987: 20: 69-76)을 이용하여, 항염 효과를 알아보았다.(A. Crummey, GP Harper, EA Boyle and FR Mangan. Inhibition of arachidonic acid-induced ear edema as a model for assessing topical anti-inflammatory compounds. Agents and Actions 1987: 20: 69 -76) was used to examine the anti-inflammatory effect.
마우스(hairless mouse) 56마리를 7마리씩 한 세트로 하여 총 8세트로 만들고, 마우스의 양쪽 귀를 에탄올로 깨끗이 세척한 후 마이크로미터를 이용하여 두께를 측정한다. 이소펠레티에린, 아나페린 또는 카스타노스퍼민을 각각 1ppm, 10ppm 함유한 시료를 도포한 시료군과 인도메타신(indomethacin) 1ppm을 함유한 시료를 도포한 비교군 그리고 에탄올을 도포한 대조군으로 나누었다. A total of 8 sets of 7 hairless mice (7 mice) were prepared, and both ears of the mice were thoroughly washed with ethanol, and the thickness was measured using a micrometer. A control group coated with a sample containing 1 ppm or 10 ppm of isopelletriene, anapelin or carnanoferrin, a control group containing 1 ppm of indomethacin, and a control group coated with ethanol.
마우스의 우측 귀에는 아라키돈산을 2㎎/ear 도포하여, 염증을 유발하였으며, 좌측 귀에는 시료 자체에 의한 염증 유발 정도를 알아보기 위해, 에탄올을 도포하였다. 상기 시료군은 이소펠레티에린, 아나페린 또는 카스타노스퍼민을 각각 1ppm, 10ppm씩 함유한 시료를, 상기 비교군은 인도메타신 1ppm 을 함유한 시료를, 상기 대조군은 에탄올을 1일 1회 20㎕씩 4일간 지속적으로 마우스의 양쪽 귀에 도포하였다. 양쪽 귀의 부종(edema) 정도는 마이크로미터를 이용하여 양쪽 귀에 대하여 각각 3회씩 반복 측정하였다. The right ear of the mouse was coated with 2 mg / ear of arachidonic acid to induce inflammation, and the left ear was coated with ethanol to examine the degree of inflammation caused by the sample itself. The sample group contained 1 ppm and 10 ppm of isopelletiene, anapelin or carnano-spermin, respectively. The control group contained 1 ppm of indomethacin, and the control group was 20 minutes of ethanol. ≪ / RTI > in each ear for 4 days. The degree of edema of both ears was measured repeatedly three times for each ear using a micrometer.
대조군(에탄올)에 대한 시료의 부종 억제율을 표 2에 나타내었으며, 비교군(인도메타신)에 대한 부종 억제율을 표 3에 나타내었다.
Table 2 shows the inhibition rates of swelling of the samples against the control (ethanol), and the inhibition rates of swelling against the comparative group (indomethacin) are shown in Table 3.
※ 억제율(%) = (A-B) / A × 100 ※ Inhibition rate (%) = (AB) / A × 100
A : 대조군 귀의 평균 두께 변화 A: Mean thickness change of the control ear
(아라키돈산 처리 귀의 두께 - 비처리 귀의 두께) (Thickness of ear treated with arachidonic acid - thickness of untreated ear)
B : 시료 도포군 귀의 평균 두께 변화 B: Mean thickness change of sample application group ear
(시료 처리 귀의 두께 - 비처리 귀의 두께) (Thickness of sample treated ear - thickness of untreated ear)
상기 표 2에 나타난 바와 같이, 10ppm에서 이소펠리티에린은 36.7%, 아나페린은 34.5%, 카스타노스퍼민은 38.9%의 높은 염증 억제율을 보였다. 또한, 상기 표 3에 나타난 바와 같이 10ppm에서 인도메타신 대비 이소펠레티에린은 67%, 아나페린은 63%, 카스타노스퍼민은 71%의 우수한 항염 효과를 나타내었다. As shown in Table 2, the degree of inflammation was as high as 36.7% for isopellitriane, 34.5% for anapelin and 38.9% for carthanospermine at 10 ppm. In addition, as shown in Table 3, the anti-inflammatory effect of isopeletiene 67%, anapelin 63%, and carnano-spermine was superior to indomethacin at 10 ppm.
한편, 부종 증가율로 유의차 검증 시, 이소펠레티에린, 아나페린 또는 카스타노스퍼민은 각각 아라키돈산과 99%의 유의차를 갖는 효과를 나타내었다.
On the other hand, when verifying the significant difference in the rate of edema growth, isopeletriene, anapelin or carnano-spermine showed 99% significant difference with arachidonic acid.
[실시예 3][Example 3]
인체에 대한 1차 자극성 시험(Human patch test)The first human stimulation test (Human patch test)
건강한 성인 남녀 50명을 대상으로 CTFA 가이드라인(The Cosmetic, Toiletry and Fragrance Association. Inc. Washington, D.C., 20036, 1991)에 따라 인체에 대한 1 차 자극시험을 실시하였다. 이소펠레티에린, 아나페린 또는 카스타노스퍼민을 각각 50ppm, 소디움라우릴셀페이트 1.0% 및 에탄올 10%를 함유한 시료, 소디움라우릴셀페이트 1.0%와 에탄올 10%를 함유한 시료 그리고 에탄올 10%를 시료로 하여 인체 자극성을 평가하였다. 핀 쳄버(Finn Chamber)에 상기 시료들을 각각 20㎕씩 적하시킨 후, 이것을 시험 부위인 인체의 등에 얹어 테이프로 고정시켰다. 이어서 24시간 동안 첩포한 후, 첩포를 제거하였다. 첩포를 제거한 후 4시간이 경과한 다음 시험 부위의 피부 반응을 다음 기준에 따라 판정하여 그 결과를 표 4에 나타내었다.The first human stimulation test was conducted on 50 healthy adult men and women according to the CTFA guidelines (The Cosmetic, Toiletry and Fragrance Association, Inc., Washington, DC, 20036, 1991). A sample containing 50 ppm each of isopelletin, anapelin or carnenoprecamine, 1.0% sodium lauryl sulfate and 10% ethanol, a sample containing 1.0% sodium lauryl sulfate and 10% ethanol, and 10% Was used as a sample to evaluate human irritation. Each of the samples was dropped in a Finn chamber (20 占 퐇 each), and the sample was placed on the back of the human body to be tested and fixed with a tape. After 24 hours of application, the patches were removed. After 4 hours from the removal of the patches, the skin reaction of the test site was judged according to the following criteria, and the results are shown in Table 4.
<판정 기준> <Criteria>
- : 홍반이나 특이한 현상 없음 -: No erythema or unusual phenomenon
± : 주위보다 약간 붉어짐 ±: slightly redder than around
+ : 주위보다 현저히 붉어짐 +: Significantly reddened than surrounding
++ : 주위보다 심하게 붉어지고 부풀어 오름 ++: More reddening and swelling than the surrounding area
자극도=[{(±)수 × 1} + {(+)수 × 2} + {(++) 수 × 3}] / 피시험자 수 The number of subjects to be tested is expressed by the following formula: Number of stimuli = [{(占) number 占 1} + {占 number 占 2} + {
소디움라우릴설페이트(1%),
에탄올(10%)Isopelletriene (50 ppm),
Sodium lauryl sulfate (1%),
Ethanol (10%)
소디움라우릴설페이트(1%),
에탄올(10%)Anapelin (50 ppm),
Sodium lauryl sulfate (1%),
Ethanol (10%)
소디움라우릴설페이트(1%),
에탄올(10%)Carnano-sipper (50 ppm),
Sodium lauryl sulfate (1%),
Ethanol (10%)
상기 표 4에서 알 수 있는 바와 같이, 이소펠레티에린, 아나페린 및 카스타노스퍼민은 소디움 라우릴설페이트와 에탄올의 자극을 크게 완화시켰다. 이러한 결과는 전술한 항염효과 실험에서 나타난 바와 같이 뛰어난 염증완화 효과에 기인된 것이라고 생각되며, 이를 통해, 본 발명에 따른 이소펠레티에린, 아나페린 또는 카스타노스퍼민이 피부에 안전한 성분임을 알 수 있다.
As can be seen in Table 4 above, isopeletierein, anapherin and carnano-spermine significantly alleviated the stimulation of sodium lauryl sulfate and ethanol. These results are believed to be attributable to the excellent anti-inflammatory effect as shown in the anti-inflammatory effect test described above. Thus, it can be seen that isopeletielin, anapelin, or castanospermine according to the present invention is a skin-safe ingredient .
[실시예 4][Example 4]
인체에 대한 항염 관능시험Anti-inflammatory sensory test for human body
10명의 피험자를 대상으로 뾰루지가 난 곳에 50ppm의 이소펠레티에린, 아나페린, 카스타노스퍼민을 하루 2회 7일간 첩포하여 변화를 관찰하였다. 대조군으로는 물을 사용하였다.Ten subjects were randomly assigned to receive 50 ppm of isopelletirin, anapelin, and carnano-spermine twice a day for 7 days. Water was used as a control.
상기 표 5에서 알 수 있는 바와 같이, 이소펠레티에린, 아나페린, 카스타노스퍼민은 뾰루지를 효과적으로 완화시켰다. 이러한 결과는 전술한 항염효과 실험에서 나타난 바와 같이 이들의 뛰어난 염증완화 효과에 기인된 것이라고 생각되며, 이를 통해, 본 발명에 따른 이소펠레티에린, 아나페린, 카스타노스퍼민이 피부에 안전한 성분임을 알 수 있다.
As can be seen in Table 5 above, isopeletriene, anapherin, and carnano-spermine effectively relieve rashes. These results are believed to be attributable to their excellent anti-inflammatory effect as shown in the anti-inflammatory effect test described above. Thus, it was confirmed that isopeletielin, anapherin, and carnano-spermine according to the present invention are safe ingredients for skin .
이하, 본 발명의 화장료 조성물의 제조예(제형예)를 제시하나 하기 제조예는 본 발명의 조성물을 예시하는 것일 뿐, 이에 한정되는 것은 아니다.
Hereinafter, the preparation examples (formulation examples) of the cosmetic composition of the present invention are presented, but the following production examples are illustrative of the composition of the present invention, but are not limited thereto.
[제조예][Manufacturing Example]
하기 조성에 따라 통상의 방법을 이용하여, 제조예 1 내지 6의 제형을 제조하였다.
The formulations of Preparation Examples 1 to 6 were prepared using conventional methods according to the following composition.
[제조예 1][Production Example 1]
화장수 toilet water
원료명 중량 %(w/w) Raw material wt% (w / w)
글리세린 5.0 Glycerin 5.0
디프로필렌글리콜 3.0 Dipropylene glycol 3.0
히아루론산 0.5 Hyaluronic acid 0.5
폴리옥시에틸렌 0.1 Polyoxyethylene 0.1
경화피마자유 0.1Hardened castor oil 0.1
폴리에틸렌 올레일에틸에탄올 5.0Polyethylene oleyl ethyl ethanol 5.0
방부제 0.15Preservative 0.15
향료 적량Fragrance quantity
색소 적량Pigment amount
화학식 1의 화합물 0.1The compound of formula 1 0.1
정제수 to 100
Purified water to 100
[제조예 2][Production Example 2]
에센스essence
원료명 중량 %(w/w) Raw material wt% (w / w)
세토스테아릴알코올 1.0Cetostearyl alcohol 1.0
자기유화형모노스테아린산 1.0Self-emulsifying monostearic acid 1.0
밀납 0.5Wax 0.5
스쿠알란 5.0Squalane 5.0
이소세틸옥타노에이트 3.0Isocetyl octanoate 3.0
디메틸실록산 0.3Dimethylsiloxane 0.3
모노스테아린산소르비탄 0.5Sorbitan monostearate 0.5
모노스테아린산폴리에틸렌글리콜 8.0Polyethylene glycol monostearate 8.0
글리세린 4.0Glycerin 4.0
프로필렌글리콜 0.2Propylene glycol 0.2
카르복시폴리머 0.22Carboxy polymer 0.22
트리에탄올아민 0.25Triethanolamine 0.25
방부제 적량Antiseptic
향료 적량Fragrance quantity
색소 적량Pigment amount
화학식 1의 화합물 7.0Compound of Formula 1 7.0
정제수 to 100
Purified water to 100
[제조예 3][Production Example 3]
로션Lotion
원료명 중량 %(w/w) Raw material wt% (w / w)
세토스테아릴알코올 0.8Cetostearyl alcohol 0.8
자기유화형모노스테아린산 10Self emulsifying monostearic acid 10
밀납 0.5 Wax 0.5
스테아린산 0.5Stearic acid 0.5
유동파라핀 7.0Liquid paraffin 7.0
스쿠알란 5.0Squalane 5.0
마카데미아오일 3.0Macadamia Oil 3.0
이소세틸옥타노에이트 2.0Isocetyl octanoate 2.0
디메틸실록산 0.3Dimethylsiloxane 0.3
모노스테아린산소르비탄 0.5Sorbitan monostearate 0.5
모노스테아린산폴리에틸렌글리콜 1.2Polyethylene glycol monostearate 1.2
글리세린 4.0Glycerin 4.0
프로필렌글리콜 4.0Propylene glycol 4.0
베타인 4.0Betain 4.0
카르복시폴리머 0.12Carboxy polymer 0.12
트리에탄올아민 0.15Triethanolamine 0.15
방부제 0.25Preservative 0.25
향료 적량Fragrance quantity
색소 적량Pigment amount
화학식 1의 화합물 5.0Compounds of Formula 1 5.0
정제수 to 100
Purified water to 100
[제조예 4][Production Example 4]
크림cream
원료명 중량 %(w/w) Raw material wt% (w / w)
세토스테아릴알코올 3.0Cetostearyl alcohol 3.0
자기유화형모노스테아린산 1.5Self emulsifying monostearic acid 1.5
친유형모노스테아린산 1.5Chin type monostearate 1.5
밀납 0.5Wax 0.5
유동파라핀 8.0Liquid paraffin 8.0
스쿠알란 7.0Squalane 7.0
이소세틸옥타노에이트 4.0Isocetyl octanoate 4.0
정제호호바유 4.0Tablet Jojoba 4.0
디메틸실록산 0.3Dimethylsiloxane 0.3
모노스테아린산소르비탄 1.0Monostearic acid sorbitan 1.0
모노스테아린산폴리에틸렌글리콜 1.2Polyethylene glycol monostearate 1.2
글리세린 6.0Glycerin 6.0
프로필렌글리콜 4.0Propylene glycol 4.0
베타인 4.0Betain 4.0
산탄검 0.06Xanthan gum 0.06
트리에탄올아민 0.10Triethanolamine 0.10
방부제 0.25Preservative 0.25
향료 적량Fragrance quantity
색소 적량Pigment amount
화학식 1의 화합물 7.0Compound of Formula 1 7.0
정제수 to 100
Purified water to 100
[제조예 5][Production Example 5]
젤Gel
원료명 중량 %(w/w) Raw material wt% (w / w)
글리세린 4.0Glycerin 4.0
프로필렌글리콜 4.0Propylene glycol 4.0
에탄올 10Ethanol 10
폴리옥시에틸렌경화피마자유 0.1Polyoxyethylene hydrogenated castor oil 0.1
카르복시폴리머 0.30Carboxy polymer 0.30
트리에탄올아민 0.30Triethanolamine 0.30
방부제 적량Antiseptic
향료 적량Fragrance quantity
색소 적량Pigment amount
화학식 1의 화합물 1.0Compound of Formula 1 1.0
정제수 to 100
Purified water to 100
[제조예 6][Production Example 6]
연고Ointment
원료명 중량 %(w/w) Raw material wt% (w / w)
세토스테아릴알코올 2.0Cetostearyl alcohol 2.0
자기유화형모노스테아린산 2.0Self emulsifying type monostearic acid 2.0
스테아린산 1.0Stearic acid 1.0
밀납 4.0Beeswax 4.0
스쿠알란 7.0Squalane 7.0
모노스테아린글리세린 3.0Monostearin glycerin 3.0
모노스테아린산소르비탄 1.0Monostearic acid sorbitan 1.0
폴리솔베이트 80 3.0Polysorbate 80 3.0
글리세린 5.0Glycerin 5.0
프로필렌글리콜 4.0Propylene glycol 4.0
향료 적량Fragrance quantity
색소 적량Pigment amount
화학식 1의 화합물 10.0Compound 10.0
바세린 to 100
Vaseline to 100
Claims (12)
An anti-inflammatory cosmetic composition comprising an alkaloid as an active ingredient.
상기 알칼로이드(alkaloid)는 식물에서 분리된 추출물이거나 합성 또는 반합성을 통해 얻어진 것인 항염 화장료 조성물.
The method according to claim 1,
Wherein the alkaloid is an extract isolated from a plant or obtained through synthesis or semisynthetic.
상기 식물은 윈터체리(Withania somnifera) 및 그린볼야자(Castanospermum austral)로 이루어진 군으로부터 선택되는 1종 이상인 항염 화장료 조성물.
3. The method of claim 2,
Wherein said plant is at least one selected from the group consisting of winter cherry (Withania somnifera) and green ball palm (Castanospermum austral).
상기 알칼로이드(alkaloid)는 이소펠레티에린(isopelletierine), 아나페린(anaferine) 및 카스타노스퍼민(Castanospermine)으로 이루어진 군으로부터 선택되는 1종 이상인 항염 화장료 조성물.
The method according to claim 1,
Wherein the alkaloid is at least one selected from the group consisting of isopelletierine, anaferine, and castanospermine.
상기 알칼로이드(alkaloid)는 전체 화장료 조성물 100 중량부에 대하여, 0.001 내지 20 중량부로 포함되는 항염 화장료 조성물.
The method according to claim 1,
Wherein the alkaloid is contained in an amount of 0.001 to 20 parts by weight based on 100 parts by weight of the total cosmetic composition.
상기 항염 화장료 조성물은 화장수, 유액, 크림, 에센스, 화장연고, 스프레이, 젤, 팩, 선크림, 메이크업 베이스, 파운데이션, 파우더 및 세정제로 이루어진 군으로부터 선택되는 제형을 갖는 항염 화장료 조성물.
The method according to claim 1,
Wherein the anti-inflammatory cosmetic composition has a formulation selected from the group consisting of lotion, milky lotion, cream, essence, cosmetic lotion, spray, gel, pack, sunscreen, makeup base, foundation, powder and detergent.
An anti-inflammatory dermatological agent containing an alkaloid as an active ingredient.
상기 알칼로이드(alkaloid)는 식물에서 분리된 추출물이거나 합성 또는 반합성을 통해 얻어진 것인 항염 피부 외용제.
8. The method of claim 7,
Wherein the alkaloid is an extract isolated from a plant or obtained through synthesis or semisynthetic.
상기 식물은 윈터체리(Withania somnifera) 및 그린볼야자(Castanospermum austral)로 이루어진 군으로부터 선택되는 1종 이상인 항염 피부 외용제.
9. The method of claim 8,
Wherein said plant is at least one selected from the group consisting of winter cherry (Withania somnifera) and green ball palm (Castanospermum austral).
상기 알칼로이드(alkaloid)는 이소펠레티에린(isopelletierine), 아나페린(anaferine) 및 카스타노스퍼민(Castanospermine)으로 이루어진 군으로부터 선택되는 1종 이상인 항염 피부 외용제.
8. The method of claim 7,
Wherein the alkaloid is at least one selected from the group consisting of isopelletierine, anaferine and castanospermine.
상기 알칼로이드(alkaloid)는 전체 조성물 100 중량부에 대하여, 0.001 내지 20 중량부로 포함되는 항염 피부 외용제.
8. The method of claim 7,
Wherein the alkaloid is contained in an amount of 0.001 to 20 parts by weight based on 100 parts by weight of the total composition.
상기 피부 외용제는 연고, 패취, 겔, 크림 또는 분무제로 이루어진 군으로부터 선택되는 제형을 갖는 항염 피부 외용제.
8. The method of claim 7,
Wherein the external preparation for skin has a formulation selected from the group consisting of ointments, patches, gels, creams or sprays.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN116747291A (en) * | 2023-07-03 | 2023-09-15 | 华中科技大学同济医学院附属协和医院 | Cystatin A, cystatin A cream, application of cystatin A cream and preparation method of cystatin A cream |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN116747291A (en) * | 2023-07-03 | 2023-09-15 | 华中科技大学同济医学院附属协和医院 | Cystatin A, cystatin A cream, application of cystatin A cream and preparation method of cystatin A cream |
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