KR20210003670A - Anti-allergy composition comprising velutin - Google Patents
Anti-allergy composition comprising velutin Download PDFInfo
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- KR20210003670A KR20210003670A KR1020200074324A KR20200074324A KR20210003670A KR 20210003670 A KR20210003670 A KR 20210003670A KR 1020200074324 A KR1020200074324 A KR 1020200074324A KR 20200074324 A KR20200074324 A KR 20200074324A KR 20210003670 A KR20210003670 A KR 20210003670A
- Authority
- KR
- South Korea
- Prior art keywords
- allergic
- present
- composition
- velutin
- beloutine
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 42
- ROCUOVBWAWAQFD-UHFFFAOYSA-N velutin Chemical compound C=1C(OC)=CC(O)=C(C(C=2)=O)C=1OC=2C1=CC=C(O)C(OC)=C1 ROCUOVBWAWAQFD-UHFFFAOYSA-N 0.000 title claims abstract description 10
- WHDYZMQZOAULDI-UHFFFAOYSA-N velutin Natural products Cc1cc(O)c2C(=O)C=C(Oc2c1)c3ccc(O)c(C)c3 WHDYZMQZOAULDI-UHFFFAOYSA-N 0.000 title claims abstract description 10
- 230000003266 anti-allergic effect Effects 0.000 title abstract description 4
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims abstract description 34
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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Abstract
Description
본 발명은 벨루틴(Velutin)을 포함하는, 알레르기성 질환의 예방, 치료 또는 개선용 조성물에 관한 것이다.The present invention relates to a composition for preventing, treating or improving allergic diseases, including velutin.
플라보노이드는 천연에 존재하는 페놀 화합물의 일종으로 항산화, 항염증, 항균, 항암 등의 다양한 생리활성이 보고되었다. 플라보노이드의 다양한 생리활성으로 인해 건강기능식품, 기능성 화장품 및 의약 소재로 다양하게 활용되고 있다. 특히 플라보노이드의 히드록시기와 메톡시기의 위치에 따라 구조적 다양성이 가능할 뿐 아니라 다양한 생리활성을 나타낸다.Flavonoids are a kind of phenolic compounds that exist in nature, and various physiological activities such as antioxidant, anti-inflammatory, antibacterial, and anti-cancer have been reported. Due to the various physiological activities of flavonoids, they are widely used as health functional foods, functional cosmetics, and pharmaceutical materials. In particular, structural diversity is possible depending on the position of the hydroxy group and the methoxy group of the flavonoid, as well as various physiological activities.
벨루틴(Velutin)은 플라보노이드의 일종으로 겨우살이(Viscum album), 팽이버섯(Flammulina velutipes), 아사이베리(Euterpe oleracea Mart), 칠면초(Suaeda japonica) 등의 천연물에서 발견되고 있으며 항산화, 항암, HIV 역전사 효소 억제, 강력한 쓴맛 차폐 효능 등 다양한 생리활성을 나타내는 것으로 보고되었다.Velutin is a type of flavonoid and is found in natural products such as Viscum album, Enoki mushroom (Flammulina velutipes), Acai berry (Euterpe oleracea Mart), and Suaeda japonica. It is an antioxidant, anticancer, and HIV reverse transcriptase. It has been reported to exhibit various physiological activities such as inhibition and strong bitter taste masking effect.
한편, 알레르기는 무해한 환경에서 외래 항원(알레르기 항원, allergen)에 의해 야기되는 면역 시스템의 과민반응이다. 천식, 아토피성 피부염 및 알레르기성 비염의 주요 증상인 가려움증, 발열 및 통증과 같은 증상은 알레르기 반응을 통해 나타나며, 이러한 증상은 비만세포(mast cell)의 과도한 활성화에 의해 발생한다.On the other hand, allergy is a hypersensitivity reaction of the immune system caused by foreign antigens (allergens) in a harmless environment. Symptoms such as itching, fever, and pain, which are the main symptoms of asthma, atopic dermatitis, and allergic rhinitis, appear through allergic reactions, and these symptoms are caused by excessive activation of mast cells.
비만세포는 알레르기 반응의 시작에 결정적인 역할을 하며 비만세포의 활성화는 전형적인 활성화제로서 특이적 면역 글로불린 E(IgE) 항체와 밀접한 관련이 있다. IgE는 비만세포의 표면에 발현되는 Fcε 수용체 I(Fc epsilon receptor I, FcεRI)과 결합한다. 비만세포 상에서 FcεRI가 항원과 가교 결합하면 세포 내 신호전달 계통(signaling cascade)이 유발되어 Lyn, Syk, 단백질 키나아제 C(protein kinase C, PKC), 및 미토젠 활성화된 단백질 키나아제(mitogen activated protein kinase, MAPK)와 같은 하류(downstream) 매개체가 활성화되고, 세포 내 Ca2+(칼슘 이온) 농도를 증가시킨다. 또한, IgE-FcεRI의 응집(aggregation)은 히스타민, 케모카인(chemokine), 사이토카인(cytokine) 및 세린 프로테아제(serine protease)를 포함하는 전형성된(preformed) 과립의 엑소사이토시스를 유도하고, 류코트리엔 및 프로스타글란딘의 새로운 합성을 자극한다. 이러한 염증 매개체는 기도 평활근의 수축, 점액의 분비 및 다른 염증 세포의 모집을 포함한 알레르기 반응에서 다양한 병태 생리학적 증상을 일으킨다. 따라서, 염증 매개체 생산의 조절은 알레르기 반응 제어에 중요하다.Mast cells play a critical role in the initiation of allergic reactions, and activation of mast cells is closely related to specific immunoglobulin E (IgE) antibodies as typical activators. IgE binds to Fcε receptor I (Fc epsilon receptor I, FcεRI) expressed on the surface of mast cells. Cross-linking of FcεRI with antigens on mast cells triggers intracellular signaling cascades, resulting in Lyn, Syk, protein kinase C (PKC), and mitogen activated protein kinase. Downstream mediators such as MAPK) are activated, increasing the concentration of Ca2+ (calcium ions) in the cell. In addition, aggregation of IgE-FcεRI induces exocytosis of preformed granules including histamine, chemokine, cytokine and serine protease, and leukotriene and prostaglandin Stimulates the new synthesis of These inflammatory mediators cause a variety of pathophysiological symptoms in allergic reactions, including contraction of airway smooth muscle, secretion of mucus and recruitment of other inflammatory cells. Thus, the regulation of inflammatory mediator production is important for controlling allergic reactions.
랫트 호염기성 백혈병(rat basophilic leukemia, RBL)-2H3 세포는 염증 매개체를 분비하는 설치류 점막형 비만세포이다. RBL-2H3 세포주는 1차 비만세포와 호염기성 세포(basophil)를 완전히 대표하지는 않지만, RBL-2H3 세포주는 상기 두 가지 세포의 특징을 공유하며 단순한 계대배양이 가능하다. 비만세포의 주요 특징은 히스타민의 분비이다. 히스타민은 알레르기 및 염증 반응에 관여하며, 다른 세포들 사이의 상호작용을 매개하는데 중요한 역할을 한다. 또한, 히스타민은 RBL-2H3 세포에서 분비된다. 따라서, RBL-2H3 세포는 일반적으로 알레르기 반응에 대한 시험관내(in vitro) 연구에 사용되어 왔다. PKC의 활성화 인자인 포볼 미리스테이트 아세테이트(phorbol myristate acetate, PMA)와 칼슘 운반체(calcium ionophore)인 A23187은 RBL-2H3 세포에서 세포 내 칼슘 이온 농도를 증가시키고 신호전달 경로(signaling pathway)의 활성화를 유도한다.Rat basophilic leukemia (RBL)-2H3 cells are rodent mucosal mast cells that secrete inflammatory mediators. The RBL-2H3 cell line does not completely represent primary mast cells and basophils, but the RBL-2H3 cell line shares the characteristics of the two cells and can be simply subcultured. The main characteristic of mast cells is the secretion of histamine. Histamine is involved in allergic and inflammatory reactions, and plays an important role in mediating interactions between different cells. In addition, histamine is secreted by RBL-2H3 cells. Therefore, RBL-2H3 cells have generally been used for in vitro studies of allergic reactions. Phobol myristate acetate (PMA), an activating factor of PKC, and A23187, a calcium ionophore, increase the intracellular calcium ion concentration and induce activation of the signaling pathway in RBL-2H3 cells. do.
이러한 알레르기 관련 메커니즘의 다양한 보고 하에서, 보다 효과적인 항 알레르기성 물질을 개발하고자 많은 연구가 진행되고 있다.Under various reports of these allergy-related mechanisms, many studies are being conducted to develop more effective antiallergic substances.
본 발명의 발명자들은 복용 시에 졸음이 오거나 현기증, 구토, 설사, 소화불량, 흥분 등의 종래 항히스타민제의 부작용을 인식하고, 이러한 부작용이 완화된 물질에 대하여 연구하던 중, 벨루틴이 비만세포로부터 히스타민 및 β-헥소사미니다아제의 방출을 억제하여 탈과립이 저해되는 효과를 나타낸다는 것을 확인하였다.The inventors of the present invention recognize the side effects of conventional antihistamines such as drowsiness, dizziness, vomiting, diarrhea, indigestion, excitement, etc. when taking it, and while studying on substances that alleviate these side effects, beloutine from mast cells It was confirmed that the release of histamine and β-hexosaminidase was inhibited, thereby exhibiting an effect of inhibiting degranulation.
이에 본 발명의 목적은 벨루틴(Velutin)을 포함하는, 알레르기성 질환 예방 또는 치료용 약학적 조성물을 제공하는 것이다.Accordingly, it is an object of the present invention to provide a pharmaceutical composition for preventing or treating allergic diseases, including velutin.
본 발명의 다른 목적은 벨루틴을 포함하는, 알레르기성 질환 예방 또는 개선용 식품 조성물을 제공하는 것이다.Another object of the present invention is to provide a food composition for preventing or improving allergic diseases, including beloutine.
본 발명의 또 다른 목적은 벨루틴을 포함하는, 알레르기성 질환 예방 또는 개선용 화장료 조성물을 제공하는 것이다.Another object of the present invention is to provide a cosmetic composition for preventing or improving allergic diseases, including beloutine.
상기 본 발명의 목적을 달성하기 위해 본 발명은 벨루틴(Velutin)을 포함하는, 알레르기성 질환 예방 또는 치료용 약학적 조성물을 제공한다.In order to achieve the object of the present invention, the present invention provides a pharmaceutical composition for preventing or treating allergic diseases, including velutin.
또한, 본 발명은 벨루틴을 포함하는, 알레르기성 질환 예방 또는 개선용 식품 조성물을 제공한다.In addition, the present invention provides a food composition for preventing or improving allergic diseases, including beloutine.
또한, 본 발명은 벨루틴을 포함하는, 알레르기성 질환 예방 또는 개선용 화장료 조성물을 제공한다.In addition, the present invention provides a cosmetic composition for preventing or improving allergic diseases, including beloutine.
본 발명의 일 구현예로 상기 벨루틴이 치료 농도 1 ~ 200 μg/ml 일 수 있다.In one embodiment of the present invention, the beloutine may have a therapeutic concentration of 1 to 200 μg/ml.
본 발명의 일 구현예로, 상기 알레르기성 질환은 알레르기성 염증 질환일 수 있다.In one embodiment of the present invention, the allergic disease may be an allergic inflammatory disease.
본 발명의 일 구현예로, 상기 알레르기성 질환은 즉시형 알레르기 반응에 의한 천식, 고초열(알레르기성 비염) 및 아토피성 습진으로 이루어진 군으로부터 선택된 1종일 수 있다.In one embodiment of the present invention, the allergic disease may be one selected from the group consisting of asthma, hay fever (allergic rhinitis), and atopic eczema caused by an immediate allergic reaction.
본 발명의 일 구현예로, 상기 조성물은 비만세포의 탈과립화를 억제할 수 있다.In one embodiment of the present invention, the composition may inhibit degranulation of mast cells.
본 발명의 일 구현예로, 상기 조성물은 β-헥소사미니다아제 또는 히스타민 방출을 억제할 수 있다.In one embodiment of the present invention, the composition may inhibit the release of β-hexosaminidase or histamine.
본 발명에 의해, 벨루틴을 포함하는 조성물이 비만세포로부터 β-헥소사미니다아제 및 히스타민의 방출을 억제하여 탈과립이 저해되는 효과를 나타내어, 졸음, 현기증, 구토, 설사, 소화불량, 흥분 등의 항히스타민제의 부작용을 완화시킬 수 있다는 것이 밝혀졌다. 따라서, 본 발명의 벨루틴을 포함하는 조성물은 항알레르기 조성물이 필요한 화장료 또는 약학 분야에서 부작용이 개선된 항히스타민성 조성물로서 유용하게 사용될 수 있다.According to the present invention, the composition containing beloutin inhibits the release of β-hexosaminidase and histamine from mast cells to inhibit degranulation, such as drowsiness, dizziness, vomiting, diarrhea, indigestion, excitement, etc. It has been shown that the side effects of antihistamines can be alleviated. Therefore, the composition containing beloutine of the present invention can be usefully used as an antihistamine composition with improved side effects in the field of cosmetics or pharmaceuticals requiring an antiallergic composition.
도 1은 본 발명의 벨루틴 및 이와 유사한 화합물인 겐크와닌(Genkwanin)과 루테올린(luteolin)의 구조를 나타낸 것이다.
도 2는 본 발명의 벨루틴 처리시 우수한 β-헥소사미니다아제 및 히스타민 방출억제 효과를 나타낸 것이다.
도 3은 제조된 벨루틴의 1H-NMR 스펙트럼을 나타낸 것이다.
도 4 제조된 겐크와닌의 1H-NMR 스펙트럼을 나타낸 것이다.Figure 1 shows the structure of the beloutin of the present invention and the similar compounds genkwanin (Genkwanin) and luteolin (luteolin).
Figure 2 shows the excellent β-hexosaminidase and histamine release inhibitory effect upon beloutine treatment of the present invention.
3 shows the 1 H-NMR spectrum of the prepared beloutin.
Figure 4 shows the 1 H-NMR spectrum of the prepared genkwanin.
본 발명은 벨루틴(Velutin)을 포함하는, 알레르기성 질환 예방 또는 치료용 약학적 조성물을 제공한다.The present invention provides a pharmaceutical composition for preventing or treating allergic diseases, including velutin.
본 발명에서 상기 벨루틴은 치료 농도 1 ~ 200 μg/ml일 수 있으며 바람직하게는 50 ~ 150 μg/ml일 수 있으며 가장 바람직하게는 100μg/ml일 수 있으나 이에 제한되는 것은 아니다.In the present invention, the beloutine may have a therapeutic concentration of 1 to 200 μg/ml, preferably 50 to 150 μg/ml, and most preferably 100 μg/ml, but is not limited thereto.
본 발명의 일 구현예에서, 상기 알레르기성 질환은 알레르기성 염증성 질환일 수 있으며 바람직하게는 즉시형 알레르기 반응에 의한 것일 수 있으며 더욱 바람직하게는 즉시형 알레르기 반응에 의한 천식, 고초열(알레르기성 비염) 및 아토피성 습진으로 이루어진 군으로부터 선택된 1종일 수 있다.In one embodiment of the present invention, the allergic disease may be an allergic inflammatory disease, preferably due to an immediate allergic reaction, and more preferably, asthma and hay fever (allergic rhinitis) due to an immediate allergic reaction. ) And atopic eczema may be one selected from the group consisting of.
본 발명에서 사용하는 용어 알레르기성 질환이란 알레르기 때문에 생기는 질환을 의미한다. 알레르기(allergy)란, 개체에 어떤 종류의 물질(항원 또는 알레르겐)이 들어왔을 때 이것에 대하여 항체가 만들어지고, 그 후 다시 동일물질인 항원이 체내로 들어갔을 때 생기는 항원항체반응을 말한다. 주된 질환은 기관지천식, 알레르기성 비염, 두드러기, 약진, 약제 알레르기, 혈청병 등이고, 알레르겐의 종류나 알레르기 반응을 일으키는 조직에 따라 여러 가지 병의 유형을 나타낸다. 또한 본 발명에서 알레르기성 염증 질환이란 상기 알레르기 반응에 의해 유도된 염증성 질환을 의미한다.The term allergic disease as used in the present invention refers to a disease caused by allergies. Allergy refers to an antigen-antibody reaction that occurs when a certain kind of substance (antigen or allergen) enters an individual, an antibody is made against it, and then the same substance, the antigen, enters the body. The main diseases are bronchial asthma, allergic rhinitis, urticaria, abruption, drug allergy, serum diseases, etc., and various types of diseases are indicated depending on the type of allergen or tissue causing an allergic reaction. In addition, in the present invention, the allergic inflammatory disease refers to an inflammatory disease induced by the allergic reaction.
본 발명에서 사용하는 용어 즉시형 알레르기 반응이란 Ⅰ형, Ⅱ형, Ⅲ형, Ⅳ형 4개 유형의 알레르기 반응 중 Ⅰ형을 의미한다. Ⅰ형(type I reaction)은 비만세포나 호염기성 세포의 표면에 IgE가 결합하여 이 IgE 항체에 특이항원이 결합하면, 비만세포나 호염기성 세포에서 과립탈출(탈과립 현상)이 일어나, 히스타민, 세로토닌, 브라디키닌과 같은 화학물질이 방출되어 혈관투과성 항진, 점액분비 촉진 등이 초래되는 현상을 말한다. 이에 포함되는 증상으로서 아나필락시스, 기관지 천식, 알레르기성 비염, 두드러기 등이 있다.The term immediate-type allergic reaction used in the present invention refers to type Ⅰ of four types of allergic reactions of type Ⅰ, type Ⅱ, type Ⅲ, and type Ⅳ. In type I reaction, when IgE is bound to the surface of mast cells or basophilic cells and specific antigens are bound to this IgE antibody, granule prolapse (degranulation) occurs in mast cells or basophilic cells, histamine, serotonin. , It refers to a phenomenon in which chemical substances such as bradykinin are released, resulting in increased vascular permeability and promotion of mucus secretion. Symptoms included in this include anaphylaxis, bronchial asthma, allergic rhinitis, and hives.
본 발명의 조성물은 비만세포의 탈과립화를 억제할 수 있고, β-헥소사미니다아제 또는 히스타민 방출을 억제할 수 있다. 비만세포(Mast cell)는 활성화되면 과민 반응(알러지)을 일으키고, 이러한 과민 반응은 아토피, 천식과 같은 질병을 유발한다. 비만세포는 세포 내 수많은 과립(granule)을 보유하고 있으며, 그 과립은 히스타민, TNF-α와 같은 다수의 염증성 물질을 포함하고 있다. 비만세포가 활성화되면 이러한 과립들이 세포막과 융합되고, 과립 속 물질들이 세포 외부로 분비되어 과민성 염증 반응이 유발된다. 이러한 과정을 탈과립(degranulation)이라고 한다. β-헥소사미니다아제(β-hexosaminidase)는 비만세포의 탈과립이 일어날 때 히스타민과 동시에 분비되는 물질로, 비만세포의 탈과립 정도를 알아볼 수 있는 지표로 널리 활용되고 있다.The composition of the present invention can inhibit degranulation of mast cells and inhibit β-hexosaminidase or histamine release. When Mast cells are activated, they cause hypersensitivity reactions (allergies), and these hypersensitivity reactions cause diseases such as atopy and asthma. Mast cells have numerous granules in cells, and the granules contain a number of inflammatory substances such as histamine and TNF-α. When mast cells are activated, these granules fuse with the cell membrane, and substances in the granules are secreted to the outside of the cells, causing an irritable inflammatory reaction. This process is called degranulation. β-hexosaminidase is a substance that is secreted simultaneously with histamine when mast cell degranulation occurs, and is widely used as an index to determine the degree of mast cell degranulation.
본 발명에서 사용되는 용어, “예방”이란 본 발명에 따른 약학적 조성물의 투여에 의해 알레르기 질환을 억제시키거나 발병을 지연시키는 모든 행위를 의미한다.The term "prevention" used in the present invention means any action that suppresses or delays the onset of an allergic disease by administration of the pharmaceutical composition according to the present invention.
본 발명에서 사용되는 용어, “치료”란 본 발명에 따른 약학적 조성물의 투여에 의해 알레르기질환에 의한 증세가 호전되거나 이롭게 변경되는 모든 행위를 의미한다.The term "treatment" used in the present invention refers to any action in which symptoms caused by an allergic disease are improved or advantageously changed by administration of the pharmaceutical composition according to the present invention.
본 발명에 따른 약학적 조성물은 벨루틴을 유효성분으로 포함하며, 약학적으로 허용 가능한 담체를 포함할 수 있다. 상기 약학적으로 허용 가능한 담체는 제제시에 통상적으로 이용되는 것으로서, 식염수, 멸균수, 링거액, 완충 식염수, 사이클로덱스트린, 덱스트로즈 용액, 말토덱스트린 용액, 글리세롤, 에탄올, 리포좀 등을 포함하지만 이에 한정되지 않으며, 필요에 따라 항산화제, 완충액 등 다른 통상의 첨가제를 더 포함할 수 있다. 또한, 희석제, 분산제, 계면활성제, 결합제, 윤활제 등을 부가적으로 첨가하여 수용액, 현탁액, 유탁액 등과 같은 주사용 제형, 환약, 캡슐, 과립, 또는 정제로 제제화할 수 있다. 적합한 약학적으로 허용되는 담체 및 제제화에 관해서는 레밍턴의 문헌에 개시되어 있는 방법을 이용하여 각 성분에 따라 바람직하게 제제화할 수 있다. 본 발명의 약학적 조성물은 제형에 특별한 제한은 없으나 주사제 또는 경구 섭취제 등으로 제제화할 수 있다.The pharmaceutical composition according to the present invention includes beloutine as an active ingredient, and may include a pharmaceutically acceptable carrier. The pharmaceutically acceptable carrier is commonly used in formulation, and includes, but is limited to, saline, sterile water, Ringer's solution, buffered saline, cyclodextrin, dextrose solution, maltodextrin solution, glycerol, ethanol, liposome, and the like. It is not, and other conventional additives such as antioxidants and buffers may be further included if necessary. In addition, diluents, dispersants, surfactants, binders, lubricants, and the like may be additionally added to form an injectable formulation, pill, capsule, granule, or tablet such as an aqueous solution, suspension, or emulsion. Regarding suitable pharmaceutically acceptable carriers and formulations, it can be preferably formulated according to each component using a method disclosed in Remington's literature. The pharmaceutical composition of the present invention is not particularly limited in its formulation, but may be formulated as an injection or oral ingestion.
본 발명의 약학적 조성물은 목적하는 방법에 따라 경구 투여하거나 비경구투여(예를 들어, 정맥 내, 피하에 적용)할 수 있으며, 투여량은 환자의 상태 및 체중, 질병의 정도, 약물형태, 투여경로 및 시간에 따라 다르지만, 당업자에 의해 적절하게 선택될 수 있다.The pharmaceutical composition of the present invention can be administered orally or parenterally according to a desired method (for example, intravenously or subcutaneously), and the dosage is the patient's condition and weight, the degree of disease, the drug form, It depends on the route and time of administration, but may be appropriately selected by those skilled in the art.
본 발명에 따른 조성물은 약학적으로 유효한 양으로 투여한다. 본 발명에 있어서, “약학적으로 유효한 양”은 의학적 치료에 적용 가능한 합리적인 수혜/위험 비율로 질환을 치료하기에 충분한 양을 의미하며, 유효용량 수준은 환자의 질환의 종류, 중증도, 약물의 활성, 약물에 대한 민감도, 투여 시간, 투여 경로 및 배출 비율, 치료기간, 동시 사용되는 약물을 포함한 요소 및 기타 의학 분야에 잘 알려진 요소에 따라 결정될 수 있다. 본 발명에 따른 조성물은 개별 치료제로 투여하거나 다른 치료제와 병용하여 투여될 수 있고 종래의 치료제와는 순차적 또는 동시에 투여될 수 있으며, 단일 또는 다중 투여될 수 있다. 상기한 요소들을 모두 고려하여 부작용 없이 최소한의 양으로 최대 효과를 얻을 수 있는 양을 투여하는 것이 중요하며, 이는 당업자에 의해 용이하게 결정될 수 있다.The composition according to the present invention is administered in a pharmaceutically effective amount. In the present invention, “a pharmaceutically effective amount” means an amount sufficient to treat a disease at a reasonable benefit/risk ratio applicable to medical treatment, and the effective dose level is the type, severity, and activity of the drug of the patient. , Sensitivity to drugs, time of administration, route of administration and rate of excretion, duration of treatment, factors including drugs used concurrently, and other factors well known in the medical field. The composition according to the present invention may be administered as an individual therapeutic agent or administered in combination with other therapeutic agents, may be administered sequentially or simultaneously with a conventional therapeutic agent, and may be administered single or multiple. It is important to administer an amount capable of obtaining the maximum effect in a minimum amount without side effects in consideration of all the above factors, and this can be easily determined by a person skilled in the art.
구체적으로, 본 발명에 따른 조성물의 유효량은 환자의 나이, 성별, 체중에 따라 달라질 수 있으며 투여 경로, 질환의 중증도, 성별, 체중, 연령 등에 따라서 증감될 수 있다.Specifically, the effective amount of the composition according to the present invention may vary depending on the age, sex, and weight of the patient, and may increase or decrease according to the route of administration, the severity of the disease, sex, weight, age, and the like.
본 발명에서 사용되는 용어, "약제학적으로 허용 가능한 이의 염"은 당해 기술분야에서 통상적인 방법에 의해 제조될 수 있는 것으로, 예를 들면, 염산, 브롬화수소, 황산, 황산수소나트륨, 인산, 탄산 등의 무기산과의 염 또는 개미산, 초산, 옥살산, 벤조산, 시트르산, 타르타르산, 글루콘산, 게스티스산, 푸마르산, 락토비온산, 살리실릭산, 또는 아세틸살리실릭산(아스피린)과 같은 유기산과 함께 약제학적으로 허용 가능한 이들의 산의 염을 형성하거나, 또는 나트륨, 칼륨 등의 알칼리금속이온과 반응하여 이들의 금속염을 형성하거나, 또는 암모늄 이온과 반응하여 또 다른 형태의 약제학적으로 허용 가능한 그의 염을 형성하는 것을 의미한다.The term "pharmaceutically acceptable salts thereof" used in the present invention can be prepared by a method conventional in the art, for example, hydrochloric acid, hydrogen bromide, sulfuric acid, sodium hydrogen sulfate, phosphoric acid, carbonic acid Salts with inorganic acids such as formic acid, acetic acid, oxalic acid, benzoic acid, citric acid, tartaric acid, gluconic acid, gastisic acid, fumaric acid, lactobionic acid, salicylic acid, or organic acid such as acetylsalicylic acid (aspirin) Forms salts of these acids that are scientifically acceptable, or reacts with alkali metal ions such as sodium and potassium to form their metal salts, or reacts with ammonium ions to form another form of pharmaceutically acceptable salts thereof. Means to form.
다른 양태로서 본 발명은 벨루틴을 포함하는, 알레르기성 질환 예방 또는 개선용 식품 조성물을 제공한다.In another aspect, the present invention provides a food composition for preventing or improving allergic diseases, including beloutine.
상기 식품 조성물은 건강기능성 식품을 포함하는 개념이다.The food composition is a concept including a health functional food.
본 발명에서 사용되는 용어, “개선”이란, 치료되는 상태와 관련된 파라미터, 예를 들면 증상의 정도를 적어도 감소시키는 모든 행위를 의미한다.As used herein, the term "improvement" refers to any action that at least reduces the severity of a parameter related to the condition being treated, for example, symptoms.
본 발명의 식품 조성물에서 벨루틴을 식품에 그대로 첨가하거나 다른 식품 또는 식품 성분과 함께 사용될 수 있고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 벨루틴의 혼합량은 그의 사용 목적(예방 또는 개선용)에 따라 적합하게 결정될 수 있다. 일반적으로, 식품 또는 음료의 제조시에 본 발명의 조성물은 원료에 대하여 15 중량% 이하, 바람직하게는 10 중량% 이하의 양으로 첨가된다. 그러나 건강 및 위생을 목적으로 하거나 또는 건강 조절을 목적으로 하는 장기간의 섭취의 경우에는 상기 양은 상기 범위 이하일 수 있다.In the food composition of the present invention, beloutine may be added to food as it is or may be used together with other foods or food ingredients, and may be appropriately used according to a conventional method. The amount of beloutin mixed may be appropriately determined depending on the purpose of use (for prevention or improvement). In general, in the manufacture of food or beverage, the composition of the present invention is added in an amount of 15% by weight or less, preferably 10% by weight or less based on the raw material. However, in the case of long-term intake for the purpose of health and hygiene or for health control purposes, the amount may be less than the above range.
본 발명의 건강기능성식품 조성물은 지시된 비율로 필수 성분으로서 상기 성분을 함유하는 것 외에 다른 성분에는 특별한 제한이 없으며 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상술한 천연 탄수화물의 예는 모노사카라이드, 예를 들어, 포도당, 과당 등; 디사카라이드, 예를 들어 말토스, 슈크로스 등; 및 폴리사카라이드, 예를 들어 덱스트린, 시클로덱스트린 등과 같은 통상적인 당, 및 자일리톨, 소르비톨, 에리트리톨 등의 당알콜이다. 상술한 것 이외의 향미제로서 천연 향미제(타우마틴, 스테비아 추출물(예를 들어 레바우디오시드 A, 글리시르히진등) 및 합성 향미제(사카린, 아스파르탐 등)를 유리하게 사용할 수 있다. 상기 천연 탄수화물의 비율은 당업자의 선택에 의해 적절하게 결정될 수 있다.The health functional food composition of the present invention is not particularly limited in other ingredients other than containing the above ingredients as an essential ingredient in the indicated ratio, and may contain various flavoring agents or natural carbohydrates, etc. as additional ingredients as in ordinary beverages. . Examples of the above-described natural carbohydrates include monosaccharides such as glucose, fructose, and the like; Disaccharides such as maltose, sucrose, and the like; And polysaccharides, for example, common sugars such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As flavoring agents other than those described above, natural flavoring agents (taumatin, stevia extract (for example, rebaudioside A, glycyrrhizin, etc.)) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used. The proportion of the natural carbohydrate can be appropriately determined by the choice of a person skilled in the art.
상기 외에 본 발명의 건강기능성식품 조성물은 여러 가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 중진제(치즈, 초콜릿 등), 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 함유할 수 있다. 이러한 성분은 독립적으로 또는 조합하여 사용할 수 있다. 이러한 첨가제의 비율 또한 당업자에 의해 적절히 선택될 수 있다.In addition to the above, the health functional food composition of the present invention includes various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic flavoring agents and natural flavoring agents, coloring agents and heavy weight agents (cheese, chocolate, etc.), pectic acid and salts thereof, Alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonates used in carbonated beverages, and the like may be contained. These components may be used independently or in combination. The proportion of these additives can also be appropriately selected by a person skilled in the art.
다른 양태로서 본 발명은 벨루틴을 포함하는, 알레르기성 질환 예방 또는 개선용 화장료 조성물을 제공한다.In another aspect, the present invention provides a cosmetic composition for preventing or improving allergic diseases, including beloutine.
본 발명에서 상기 화장료 조성물은 용액, 현탁액, 유탁액, 페이스트, 겔, 크림, 파우더, 비누, 계면활성제-함유 클린싱, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션 및 스프레이로 구성된 군으로부터 선택되는 제형을 가질 수 있으나 이에 제한되는 것은 아니다.In the present invention, the cosmetic composition is a formulation selected from the group consisting of solutions, suspensions, emulsions, pastes, gels, creams, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, wax foundations, and sprays. May have, but is not limited thereto.
본 발명의 상기 화장료 조성물은 화장료 조성물에 통상적으로 이용되는 성분들을 포함할 수 있으며, 예컨대 항산화제, 안정화제, 용해화제, 비타민, 안료, 및 향료와 같은 통상적인 보조제, 그리고 담체를 포함할 수 있다. The cosmetic composition of the present invention may include components commonly used in cosmetic compositions, and may include conventional adjuvants such as antioxidants, stabilizers, solubilizers, vitamins, pigments, and fragrances, and carriers. .
또한, 본 발명의 조성물은 유기 자외선 차단제를 혼합하여 사용할 수도 있다. 상기 유기 자외선 차단제로는 글리세릴파바, 드로메트리졸트리실록산, 드로메트리졸, 디갈로일트리올리에이트, 디소듐페닐디벤즈이미다졸테트라설포네이트, 디에틸헥실부타미도트리아존, 디에틸아미노하이드록시벤조일헥실벤조에이트, 디이에이-메톡시신나메이트, 로우손과 디하이드록시아세톤의 혼합물, 메틸렌비스-벤조트리아졸릴테트라메칠부틸페놀, 4-메틸벤질리덴캠퍼, 멘틸안트라닐레이트, 벤조페논-3(옥시벤존),벤조페논-4, 벤조페논-8(디옥시페벤존), 부틸메톡시디벤조일메탄, 비스에틸헥실옥시페놀메톡시페닐트리아진, 시녹세이트, 에틸디하이드록시프로필파바, 옥토크릴렌, 에틸헥실디메틸파바, 에틸헥실메톡시신나메이트, 에틸헥실살리실레이트, 에틸헥실트리아존, 이소아밀-p-메톡시신나메이트, 폴리실리콘-15(디메치코디에틸벤잘말로네이트), 테레프탈릴리덴디캠퍼설포닉애씨드 및 그 염류, 티이에이-살리실레이트 및 아미노벤조산(파바)으로 이루어진 군으로부터 선택된 1종 이상을 사용할 수 있다.In addition, the composition of the present invention may be used by mixing an organic sunscreen. The organic sunscreens include glycerylpava, dromethrizoltrisiloxane, dromethrizol, digaloyltrioleate, disodiumphenyldibenzimidazoletetrasulfonate, diethylhexylbutamidotriazone, diethylamino Hydroxybenzoylhexylbenzoate, DieA-methoxycinnamate, mixture of Lawson and dihydroxyacetone, methylenebis-benzotriazolyltetramethylbutylphenol, 4-methylbenzylidene camphor, menthylanthranylate, benzophenone -3 (oxybenzone), benzophenone-4, benzophenone-8 (dioxyfebenzone), butylmethoxydibenzoylmethane, bisethylhexyloxyphenolmethoxyphenyltriazine, sinoxate, ethyldihydroxypropylpaba, Octocrylene, ethylhexyldimethylpaba, ethylhexylmethoxycinnamate, ethylhexylsalicylate, ethylhexyltriazone, isoamyl-p-methoxycinnamate, polysilicon-15 (dimethicodiethylbenzalmalonate) , Terephthallylidene dicamphor sulfonic acid and salts thereof, TEA-salicylate, and one or more selected from the group consisting of aminobenzoic acid (pava) may be used.
이하, 본 발명을 실시예를 통하여 더욱 상세히 설명한다. 그러나, 하기 실시예는 본 발명을 예시하기 위한 것으로, 본 발명의 범위가 이에 제한되는 것은 아니다.Hereinafter, the present invention will be described in more detail through examples. However, the following examples are for illustrating the present invention, and the scope of the present invention is not limited thereto.
<실시예 1: 벨루틴, 겐크와닌의 합성><Example 1: Synthesis of beloutine and genkwannin>
3가지 플라본 유도체중에서 벨루틴과 겐크와닌은 화학적으로 합성하였고, 루테올린은 주식회사 켐원 (ChemOne, Korea)에서 구매하였다. Among the three flavone derivatives, belutin and genkwannin were chemically synthesized, and luteolin was purchased from ChemOne, Korea.
벨루틴 및 겐크와닌 제조 : 2‘,4’,6‘-트리하이드록시아세토페논으로부터 4단계의 순차적인 메틸레이션, 알돌 컨덴세이션, 고리화, 디프로텍션 반응을 거쳐 제조하였다(도 3 및 4 참조).Belutin and Genkwanin Preparation: Prepared from 2',4',6'-trihydroxyacetophenone through four sequential methylation, aldol condensation, cyclization, and deprotection reactions (Fig. 3 and 4).
벨루틴의 제조 : 1H NMR (DMSO-d6, 400MHz), δ : 12.97 (s, 1H), 10.00 (s, 1H), 7.61-7.59 (m, 2H, J = 4.62 Hz), 6.96-6.93 (m, 2H, J = 9.96 Hz), 6.80 (d, 1H, J = 2.24 Hz), 6.38-6.37 (d, 1H, J = 2.20 Hz), 3.93 (s, 3H), 3.91 (s, 3H).Preparation of Belloutine: 1 H NMR (DMSO-d 6 , 400 MHz), δ : 12.97 (s, 1H), 10.00 (s, 1H), 7.61-7.59 (m, 2H, J = 4.62 Hz), 6.96-6.93 (m, 2H, J = 9.96 Hz), 6.80 (d, 1H, J = 2.24 Hz), 6.38-6.37 (d, 1H, J = 2.20 Hz), 3.93 (s, 3H), 3.91 (s, 3H) .
겐크와닌의 제조 : 1H NMR (DMSO-d6, 400MHz), δ : 12.96 (s, 1H), 7.96 (d, 2H, J = 8.84 Hz), 6.93 (d, 2H, J = 8.84 Hz), 6.84 (s, 1H), 6.77 (d, 1H, J = 2.25 Hz), 6.37 (d, 1H, J = 2.25 Hz), 3.87 (s, 1H)Preparation of Genkwanin: 1 H NMR (DMSO-d 6 , 400 MHz), δ : 12.96 (s, 1H), 7.96 (d, 2H, J = 8.84 Hz), 6.93 (d, 2H, J = 8.84 Hz) , 6.84 (s, 1H), 6.77 (d, 1H, J = 2.25 Hz), 6.37 (d, 1H, J = 2.25 Hz), 3.87 (s, 1H)
<실시예 2: 실험준비><Example 2: Preparation for experiment>
RBL-2H3 세포는 10% 열 불활성화 소태아혈청(FBS), 1% 페니실린 및 1% 스트렙토마이신(Hyclone) 보충된 DMEM 배지(Dulbecco 's modified Eagle 's medium, Hyclone Logan, UT, USA)에서 배양하였다.RBL-2H3 cells were in DMEM medium (Dulbecco's modified Eagle's medium, Hyclone Logan, UT, USA) supplemented with 10% heat inactivated fetal bovine serum (FBS), 1% penicillin and 1% streptomycin (Hyclone). Cultured.
<실시예 3: 벨루틴의 β-hexosaminidase 방출 감소 효과 확인><Example 3: Confirmation of the effect of beloutin on reducing the release of β-hexosaminidase>
24-well plate에 RBL-2H3 (비만세포) 세포를 10% FBS가 포함된 DMEM media를 이용해 seeding하고 24시간동안 배양하였다. 그 다음 배양액을 제거하고 벨루틴을 2-100 μg/ml의 농도가 되도록 siraganian buffer (NaCl 119mM, KCl 5mM, Glucose 5.6mM, PIPES 25mM, MgCl2, 0.4mM, CaCl2 1mM, BSA 0.1%, pH 7.2)에 희석하여 세포에 1시간 동안 처리하였고 또한 벨루틴의 효과와 비교하기 위해 대조군으로 겐크와닌과 루테올린을 100 μg/ml 농도로 처리하였다. 그 다음 세포로부터 용액을 제거하고, PIPES를 이용해 두 번 washing 하였으며, 50 nM PMA (phorbol myristate acetate)와 1 μM A23187 (calcium ionophore)를 30 분 동안 처리하여 면역반응을 유도하였다. 그 다음 20 μL 상층액을 취해 96-well plate로 옮기고, substrate인 4-p-nitrophenyl-N-acetyl-β-D-glucosaminide를 2 mM 농도가 되도록 0.05 M sodium citrate buffer (pH 4.5)에 희석하여 80 μL 와 섞고 30분간 37도에서 반응시켰다. 그 후 stop buffer (0.1 M·NaHCO3, pH 10) 200 μL 를 첨가하여 반응을 종결시키고, 405 nm에서 흡광도를 측정하였다.RBL-2H3 (mast cells) cells were seeded in a 24-well plate using DMEM media containing 10% FBS and cultured for 24 hours. Then, remove the culture medium and add beloutin to a concentration of 2-100 μg/ml in a siraganian buffer (NaCl 119mM, KCl 5mM, Glucose 5.6mM, PIPES 25mM, MgCl 2 , 0.4mM, CaCl 2 1mM, BSA 0.1%, pH 7.2) was diluted to the cells and treated for 1 hour. In order to compare the effect of beloutin, genkwanin and luteolin were treated at a concentration of 100 μg/ml as controls. Then, the solution was removed from the cells, washed twice using PIPES, and treated with 50 nM PMA (phorbol myristate acetate) and 1 μM A23187 (calcium ionophore) for 30 minutes to induce an immune response. Then, take 20 μL of the supernatant and transfer it to a 96-well plate, and dilute the substrate 4-p-nitrophenyl-N-acetyl-β-D-glucosaminide in 0.05 M sodium citrate buffer (pH 4.5) to a concentration of 2 mM. Mix with 80 μL and react at 37 degrees for 30 minutes. Thereafter, 200 μL of a stop buffer (0.1 M NaHCO 3 , pH 10) was added to terminate the reaction, and absorbance was measured at 405 nm.
그 결과, 도 2에 나타난 바와 같이 아무것도 처리하지 않은 정상비만세포(-)에 비해서 탈과립화가 활성화 되었을 때 β-hexosaminidase 방출이 현저히 증가하였고, 벨루틴 처리 농도가 증가함에 따라 β-hexosaminidase 방출이 감소됨을 확인하였다. 반면 겐크와닌과 루테올린의 경우 동일한 100μg/ml 농도로 처리하여도 벨루틴 보다 낮은 효과를 나타냄을 확인하였다.As a result, as shown in FIG. 2, the release of β-hexosaminidase was significantly increased when degranulation was activated compared to normal mast cells (-) that were not treated with anything, and the release of β-hexosaminidase was decreased as the concentration of beloutine treatment increased. Confirmed. On the other hand, it was confirmed that genkwanin and luteolin showed lower effects than beloutin even when treated at the same concentration of 100 μg/ml.
<실시예 4: 벨루틴의 히스타민 방출 감소 효과 확인><Example 4: Confirmation of the effect of beloutin on reducing histamine release>
24-well plate에 RBL-2H3 (비만세포) 세포를 10% FBS가 포함된 DMEM media를 이용해 seeding하고 24시간동안 배양하였다. 그 다음 배양액을 제거하고 벨루틴을 2-100 μg/ml의 농도가 되도록 siraganian buffer (NaCl 119mM, KCl 5mM, Glucose 5.6mM, PIPES 25mM, MgCl2, 0.4mM, CaCl2 1mM, BSA 0.1%, pH 7.2)에 희석하여 세포에 1시간 동안 처리하였고 또한 벨루틴의 효과와 비교하기 위해 대조군으로 겐크와닌과 루테올린을 100 μg/ml 농도로 처리하였다. 그 다음 세포로부터 용액을 제거하고, PIPES를 이용해 두 번 washing하고 50 nM PMA (phorbol myristate acetate)와 1 μM A23187 (calcium ionophore)를 30 분 동안 처리하여 면역반응을 유도하였다. 그 다음 1 mL 상층액을 취해, 2 mL 의 1 N·NaOH, 및 0.1 mL of 1% OPT (o-phtha-laldehyde)와 섞고 상온에서 5분동안 반응시켰다. 그 다음 0.1 mL 3 N·HCl를 첨가하여 반응을 종결시키고, 360 nm에서 excitation, 450 nm에서 emission 되는 형광강도를 측정하였다.RBL-2H3 (mast cells) cells were seeded in a 24-well plate using DMEM media containing 10% FBS and cultured for 24 hours. Then, remove the culture medium and add beloutin to a concentration of 2-100 μg/ml in a siraganian buffer (NaCl 119mM, KCl 5mM, Glucose 5.6mM, PIPES 25mM, MgCl 2 , 0.4mM, CaCl 2 1mM, BSA 0.1%, pH 7.2) was diluted to the cells and treated for 1 hour. In order to compare the effect of beloutin, genkwanin and luteolin were treated at a concentration of 100 μg/ml as controls. Then, the solution was removed from the cells, washed twice using PIPES, and treated with 50 nM PMA (phorbol myristate acetate) and 1 μM A23187 (calcium ionophore) for 30 minutes to induce an immune response. Then, a 1 mL supernatant was taken, mixed with 2 mL of 1 N·NaOH, and 0.1 mL of 1% OPT (o-phtha-laldehyde), and reacted at room temperature for 5 minutes. Then, 0.1 mL 3 N·HCl was added to terminate the reaction, and excitation at 360 nm and fluorescence intensity emitted at 450 nm were measured.
그 결과, 도 2에 나타난 바와 같이 아무것도 처리하지 않은 정상세포 (-)에 비해서 탈과립화를 활성화 되었을 때 히스타민방출이 현저히 증가하였고, 벨루틴 농도가 증가함에 따라 히스타민 방출이 감소됨을 확인하였다. 반면 겐크와닌과 루테올린의 경우 동일한 100μg/ml 농도로 처리하여도 벨루틴 보다 낮은 효과를 나타냄을 확인하였다.As a result, as shown in FIG. 2, it was confirmed that histamine release was significantly increased when degranulation was activated compared to normal cells (-) that were not treated with anything, and histamine release was decreased as the beloutine concentration increased. On the other hand, it was confirmed that genkwanin and luteolin showed lower effects than beloutin even when treated at the same concentration of 100 μg/ml.
Claims (8)
A pharmaceutical composition for preventing or treating allergic diseases, including velutin.
The pharmaceutical composition of claim 1, wherein the beloutine is at a therapeutic concentration of 1 to 200 μg/ml.
The pharmaceutical composition according to claim 1, wherein the allergic disease is an allergic inflammatory disease.
The pharmaceutical composition according to claim 1, wherein the allergic disease is one selected from the group consisting of asthma, hay fever (allergic rhinitis), and atopic eczema caused by immediate allergic reaction.
The pharmaceutical composition of claim 1, wherein the composition inhibits degranulation of mast cells.
The pharmaceutical composition of claim 1, wherein the composition inhibits the release of β-hexosaminidase or histamine.
Food composition for preventing or improving allergic diseases, including beloutine.
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| KR20180052226A (en) | 2016-11-10 | 2018-05-18 | 경희대학교 산학협력단 | Fusion flavonoid O-methyltransferase and use thereof |
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| KR20040087223A (en) | 2003-04-04 | 2004-10-13 | 학교법인 현동학원 | Isolation of velutin and betulinic acid isolated from the organic extract of Korean mistletoe and its anti-tumor activity |
| KR20180052226A (en) | 2016-11-10 | 2018-05-18 | 경희대학교 산학협력단 | Fusion flavonoid O-methyltransferase and use thereof |
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