KR101049541B1 - Pharmaceutical composition comprising cAMP regulator - Google Patents
Pharmaceutical composition comprising cAMP regulator Download PDFInfo
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- KR101049541B1 KR101049541B1 KR1020080042535A KR20080042535A KR101049541B1 KR 101049541 B1 KR101049541 B1 KR 101049541B1 KR 1020080042535 A KR1020080042535 A KR 1020080042535A KR 20080042535 A KR20080042535 A KR 20080042535A KR 101049541 B1 KR101049541 B1 KR 101049541B1
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- camp
- pharmaceutical composition
- anthrax
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Abstract
본 발명은 하기 화학식 1의 크리신 유도체를 포함하는 약학적 조성물을 제공한다:The present invention provides a pharmaceutical composition comprising a glycine derivative of the formula
[화학식 1][Formula 1]
이 때 R1 은 수소(H) 또는 프로필(propyl)이고, R2는 프로필, 부틸(butyl), 옥틸(octyl) 등의 알킬 또는 톨루익산(toluic acid)이고, R3은 수소, 또는 탄소수 1 내지 6의 알킬기이고, n은 0 내지 3의 정수이다. Wherein R 1 is hydrogen (H) or propyl, R 2 is alkyl or toluic acid such as propyl, butyl, octyl, R 3 is hydrogen, or 1 carbon It is an alkyl group of -6, and n is an integer of 0-3.
본 발명의 cAMP 조절제는 각종 만성 스트레스 질병을 유발하는 코티솔(cortisol) 등과 같은 호르몬 분비, 위산 분비, 탄저균 활성 등에 관여하는 cAMP의 양을 효과적으로 조절하여 cAMP의 과다 생성으로 유발되는 각종 질환, 예를 들어 스트레스성 질환, 위산과다분비, 탄저균 감염 등에 효과적으로 사용될 수 있다. The cAMP modulator of the present invention effectively regulates the amount of cAMP involved in hormone secretion, gastric acid secretion, anthrax activity such as cortisol, which causes various chronic stress diseases, and various diseases caused by overproduction of cAMP. It can be effectively used for stress diseases, gastric acid secretion, anthrax infections, and the like.
크리신, 세포사멸, 탄저균, cAMP, 아데닐릴 사이클라제 Chrysin, apoptosis, anthrax, cAMP, adenylyl cyclase
Description
본 발명은 cAMP 조절제를 포함하는 약학적 조성물에 관한 것으로서, 보다 상세하게는 아데닐릴 사이클라제의 활성을 감소시켜 cAMP 의 생성량을 감소시켜 만성 스트레스 호르몬과 위산과다 분비를 효과적으로 조절하고 탄저균 침입에 의해유발되는 세포사멸을 억제할 수 있는 cAMP 조절제를 포함하는 약학적 조성물에 관한 것이다. The present invention relates to a pharmaceutical composition comprising a cAMP modulator, and more particularly, by reducing the activity of adenyl cyclase to reduce the amount of cAMP produced, thereby effectively regulating the secretion of chronic stress hormone and gastric acid excess and by anthrax invasion. It relates to a pharmaceutical composition comprising a cAMP modulator that can inhibit the induced cell death.
외부 화학적 메신저(예, 호르몬, 림포카인, 성장인자, 신경전달물질 등)에 대한 많은 세포들의 응답은 이들 물질에 대한 수용체들을 통해서 유발된다. 이들 다양한 수용체들은 효소계, 즉, 아데닐릴 사이클라제(adenylyl cyclase)와 연관되어 있으며, 이것은 아데노신 트리포스페이트(ATP)의 사이클릭 아데노신 모노포스페이트 (사이클릭 AMP, 또는 간략히 cAMP라고도함) 및 피로포스페이트로의 전환을 촉매한다.The response of many cells to external chemical messengers (eg, hormones, lymphokines, growth factors, neurotransmitters, etc.) is elicited through receptors on these substances. These various receptors are associated with the enzyme system, namely adenylyl cyclase, which is a cyclic adenosine monophosphate of adenosine triphosphate (ATP) (also referred to as cyclic AMP, or simply cAMP) and pyrophosphate. Catalyzes the conversion.
cAMP는 세포 내부에서 방출되어 기타 효소의 활성화를 유발함으로써, 결과적으로 생물학적 응답을 초래하게 된다. 질병의 치료 또는 생리적 상태의 조절에 있 어서 중요한 접근 방식은 이들 메신저에 대한 세포의 반응을 변형시키는 능력에 의한 것이다. 이렇게 함으로써, 전반적인 기전에 의한 다수의 상태들을 변형시키는 것이 가능할 수 있다. cAMP is released inside the cell causing the activation of other enzymes, resulting in a biological response. An important approach in the treatment of disease or in the regulation of physiological conditions is by its ability to modify the cellular response to these messengers. By doing so, it may be possible to modify a number of states by the overall mechanism.
cAMP의 생성량은 여러가지 물질에 의하여 조절된다고 알려져 있다. 이중 탄저균에 의한 질병을 유발하는 독소중 하나인 에데마 팩터(edema factor; EF) 단백질은 세포 내에서 cAMP의 조절과정을 무력화시켜 과량의 cAMP를 생성시키도록 한다. The production amount of cAMP is known to be controlled by various substances. The edema factor (EF) protein, one of the toxins causing anthrax, causes the regulation of cAMP in the cell to produce excess cAMP.
cAMP는 아데닐릴 사이클라제에 의해 만들어지며 세포의 물의 양이나 에너지 균형을 비롯하여 수많은 과정을 조절하기 때문에 그 농도가 엄격하게 조절되어야만 한다. 따라서 이러한 cAMP의 생성량을 조절하기 위한 연구가 활발하게 이루어지고 있다.cAMP is produced by adenylyl cyclase and must be tightly regulated because it regulates a number of processes, including the amount of water and energy balance in cells. Therefore, studies for controlling the amount of cAMP production are being actively made.
본 발명의 목적은 아데닐릴 사이클라제 활성을 억제하여 cAMP의 생성량을 감소시켜 만성 스트레스 호르몬과 위산과다 분비를 효과적으로 조절하고 탄저균 침입에 의해 유발되는 세포사멸을 억제할 수 있는 cAMP 조절제를 포함하는 약학적 조성물을 제공하는 것이다.It is an object of the present invention to reduce the amount of cAMP produced by inhibiting adenylyl cyclase activity to effectively regulate the secretion of chronic stress hormones and gastric acid excess and to contain a cAMP modulator that can inhibit apoptosis caused by anthrax invasion To provide a composition.
본 발명의 일 구현예에 따르면, 하기 화학식 1의 크리신(chrysin) 유도체를 포함하는 cAMP 조절제를 제공한다:According to one embodiment of the present invention, it provides a cAMP modulator comprising a chrysin derivative of the general formula (I):
[화학식 1][Formula 1]
이 때 R1 은 수소(H) 또는 프로필(propyl)이고, R2는 프로필, 부틸(butyl), 옥틸(octyl) 등의 알킬 또는 톨루익산(toluic acid)이고, R3은 수소 또는 탄소수 1 내지 6의 알킬기이고, n은 0 내지 3의 정수이다. In this case, R 1 is hydrogen (H) or propyl, R 2 is alkyl or toluic acid, such as propyl, butyl, octyl, R 3 is hydrogen or C1 to C It is an alkyl group of 6, n is an integer of 0-3.
본 발명은 또한 상기 cAMP 조절제를 유효량으로 함유하는 약학적 조성물을 제공한다. The present invention also provides a pharmaceutical composition containing an effective amount of the cAMP modulator.
본 발명의 cAMP 조절제는 각종 만성 스트레스 질병을 유발하는 코티솔(cortisol) 등과 같은 호르몬 분비, 위산 분비, 탄저균 활성 등에 관여하는 cAMP의 양을 효과적으로 조절하여 cAMP의 과다 생성으로 유발되는 각종 질환, 예를 들어 스트레스성 질환, 위산과다분비, 탄저균 감염 등에 효과적으로 사용될 수 있다. The cAMP modulator of the present invention effectively regulates the amount of cAMP involved in hormone secretion, gastric acid secretion, anthrax activity such as cortisol, which causes various chronic stress diseases, and various diseases caused by overproduction of cAMP. It can be effectively used for stress diseases, gastric acid secretion, anthrax infections, and the like.
이하, 본 발명을 보다 상세하게 설명한다.Hereinafter, the present invention will be described in more detail.
본 발명의 일 구현예에 따르면, 하기 화학식 1의 크리신 유도체를 포함하는 cAMP 조절제를 제공한다:According to one embodiment of the present invention, there is provided a cAMP modulator comprising a chrysine derivative of Formula 1 below:
[화학식 1][Formula 1]
이 때 R1 은 수소(H) 또는 프로필(propyl)이고, R2는 프로필, 부틸(butyl), 옥틸(octyl) 등의 알킬 또는 톨루익산(toluic acid)이고, R3은 수소 또는 탄소수 1 내지 6의 알킬기이고, n은 0 내지 3의 정수이다. In this case, R 1 is hydrogen (H) or propyl, R 2 is alkyl or toluic acid, such as propyl, butyl, octyl, R 3 is hydrogen or C1 to C It is an alkyl group of 6, n is an integer of 0-3.
상기 크리신(5,7-dihydroxy-2-phenyl-4H-chromen-4-one)은 천연꿀(Honey)과 프로폴리스(Propois)의 함유 성분인 플라보노이드중 하나이며, 본 발명에서의 크리신 유도체는 천연성분에서 추출할 수도 있고 인공적으로 합성할 수도 있다. The glycine (5,7-dihydroxy-2-phenyl-4H-chromen-4-one) is one of the flavonoids containing the components of natural honey (Honey) and propolis (Propois), the glycine derivative in the present invention It can be extracted from natural ingredients or artificially synthesized.
상기 크리신 유도체는 아데닐릴 사이클라제 단백질과 탄저독소 단백질 에데마 팩터(Edema factor)의 활성의 억제하여 cAMP의 생성량을 감소시킬 수 있다.The crysin derivative may reduce the amount of cAMP produced by inhibiting the activity of adenyl cyclase protein and anthrax toxin protein Edema factor.
따라서 상기 크리신 유도체는 cAMP의 과다 생성으로 유발되는 각종 질환의 치료 및 예방에 사용되는 약학적 조성물에 포함될 수 있다. 상기 cAMP의 과다 생성과 관련된 질병으로는 스트레스성 불안, 우울증, 피로증후군, 신경변성 질환, 위염, 위궤양, 염증성 장질환, 과민성 대장 증후군, 탄저균 감염, 관절, 류머티즘, 췌장염, 건선, 편두통, 알쯔하이머병, 파킨슨 병, 천식, 이식거부반응, 뇌졸중, cAMP 축적에 의한 멜라닌(Melanin) 색소침착, 기미 주근깨 등이 있다. Therefore, the glycine derivative may be included in a pharmaceutical composition used for the treatment and prevention of various diseases caused by the excessive production of cAMP. Diseases associated with overproduction of cAMP include stress anxiety, depression, fatigue syndrome, neurodegenerative diseases, gastritis, gastric ulcer, inflammatory bowel disease, irritable bowel syndrome, anthrax infections, joints, rheumatism, pancreatitis, psoriasis, migraine, Alzheimer's disease , Parkinson's disease, asthma, transplant rejection, stroke, melanin pigmentation due to cAMP accumulation, blemish freckles and the like.
상기 약학적 조성물은 유효한 양으로 상기 화학식 1의 크리신 유도체를 포함할 수 있다. 상기 크리신 유도체의 유효한 양은 조성물 총량에 대하여 0.01 내지 99.99 중량%일 수 있으나 이에 한정되는 것은 아니다. The pharmaceutical composition may include a glycine derivative of Formula 1 in an effective amount. An effective amount of the glycine derivative may be 0.01 to 99.99% by weight based on the total amount of the composition, but is not limited thereto.
상기 약학적 조성물의 적합한 제형으로는 정제, 당의정, 경질 또는 연질의 캡슐제, 용액제, 현탁제 또는 유화액제, 주사제, 좌약제 등이 있으나 이에 한정되는 것은 아니다. 상기 크리신 유도체 및 이들의 약제학적으로 허용되는 염을 약학적으로 불활성인 유기 또는 무기 담체를 이용하여 적합한 제형으로 제조할 수 있다. 즉 제형이 정제, 코팅된 정제, 당의정 및 경질 캡슐제인 경우 락토스, 옥수수 전분 또는 그 유도체, 활석, 스테아르산 또는 그 염을 사용할 수 있다. 또한 제형이 연질 캡슐제의 경우에는 식물성 오일, 왁스, 지방, 반고체 및 액체의 폴리올이 사용가능하다. 용액 또는 시럽 형태의 경우에는 물, 폴리올, 글리세롤, 및 식물성 오일 등이 사용될 수 있다. 좌약용 담체로는 천연 오일 또는 경화된 오일, 왁스, 지방, 액체 폴리올 등이 사용가능하다.Suitable formulations of the pharmaceutical composition include, but are not limited to, tablets, dragees, hard or soft capsules, solutions, suspensions or emulsions, injections, suppositories, and the like. The crysin derivatives and their pharmaceutically acceptable salts can be prepared in suitable formulations using pharmaceutically inert organic or inorganic carriers. That is, when the formulation is a tablet, coated tablets, dragees and hard capsules, lactose, corn starch or derivatives thereof, talc, stearic acid or salts thereof can be used. Also in the case of soft capsule formulations, polyols of vegetable oils, waxes, fats, semisolids and liquids can be used. In the case of solution or syrup form, water, polyols, glycerol, vegetable oils and the like can be used. As suppository carriers, natural or hardened oils, waxes, fats, liquid polyols and the like can be used.
본 발명의 약학적 조성물은 보존제, 안정화제, 습윤제, 유화제, 용해제, 감미제, 착색제, 삼투압 조절제, 산화방지제 등을 더 포함할 수 있다.The pharmaceutical composition of the present invention may further include a preservative, stabilizer, wetting agent, emulsifier, solubilizer, sweetener, colorant, osmotic pressure control agent, antioxidant, and the like.
투여 방법은 제형에 따라 용이하게 선택될 수 있으며, 경구 또는 비경구 투여될 수 있다. 투여량은 환자의 체중, 병증의 정도, 성별, 연령에 따라 다를 수 있으나 통상 건강한 성인 남성의 경우 1일 1mg/kg 내지 10mg/kg의 양으로 투여되는 것이 바람직하다. 투여회수 또한 환자의 체중, 병증의 정도, 성별, 연령에 따라 용이하게 조절될 수 있다.The method of administration can be readily selected according to the dosage form and can be administered orally or parenterally. The dosage may vary depending on the weight, severity, sex, and age of the patient, but in the case of a healthy adult male, the dosage is preferably 1 mg / kg to 10 mg / kg per day. The number of doses can also be easily adjusted according to the weight, severity, sex, and age of the patient.
또한 상기 크리신 유도체는 각종 식품에 첨가되어 cAMP의 과다 생성과 관련된 질병을 예방, 치료하기 위한 기능성 식품에도 사용될 수 있다. 첨가될 식품은 시중에서 유통되고 있는 모든 식품이 될 수 있으며 특별히 한정되지 않는다. In addition, the glycine derivatives may be added to various foods and used in functional foods for preventing and treating diseases associated with excessive production of cAMP. The food to be added may be any food in the market and is not particularly limited.
상기 기능성 식품으로는 예를 들어, 캔디, 초콜릿, 음료, 껌, 차등의 각종 식품류 비타민복합체 등의 건강보조 식품류 등을 들 수 있으며, 분말, 과립, 정제, 캡슐 또는 음료의 형태로 사용할 수 있다.The functional foods include, for example, health supplements such as candy, chocolate, beverages, gums, teas, and various kinds of food vitamin complexes, and can be used in the form of powders, granules, tablets, capsules, or beverages.
이때, 식품 또는 음료 중의 상기 유효 성분은 식품 총량에 대하여 0.01 내지 15 중량%, 바람직하게는 0.1 내지 10 중량%로 가할 수 있으며, 건강 음료 조성물의 경우 100ml를 기준으로 0.02 내지 10g, 바람직하게는 0.3 내지 1g의 비율로 포함할 수 있다. At this time, the active ingredient in the food or beverage may be added to 0.01 to 15% by weight, preferably 0.1 to 10% by weight based on the total amount of food, 0.02 to 10g, preferably 0.3 based on 100ml for the health beverage composition It may be included in the ratio of 1g.
상기 건강기능식품은 유효 성분과 함께 식품학적으로 허용가능한 식품 보조 첨가제를 더 포함할 수 있다. The dietary supplement may further comprise a food supplement acceptable food additive with the active ingredient.
본 발명의 건강 음료 조성물은 지시된 비율로 필수성분으로서 상기 유효성분을 함유하는 외에는 액체 성분에 특별한 제한은 없으며, 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가성분으로서 함유할 수 있다. 상술한 천연 탄수화물의 예는 포도당, 과당 등의 모노사카라이드 말토오스, 수크로오스 등의 디사카라이드 덱스트린, 시클로덱스트린 등의 폴리사카라이드 등과 같은 통상적인 당 및 자일리톨, 소르비톨, 에리트리톨 등의 당알코올을 들 수 있다. 상술한 것 외의 향미제로서 천연 향미제(타우마틴, 스테비아 추출물(예를 들어 바우디오시드A, 글리시르히진(glycyrrhizin) 등) 및 합성 향미제(사카린, 아스프르탐 등)을 사용할 수도 있다. 상기 천연 탄수화물의 비율은 본 발명의 조성물 100ml당 일반적으로 약 1 내지 20g, 바람직하게는 약 5 내지 12g이다.The health beverage composition of the present invention is not particularly limited to the liquid component except for containing the active ingredient as an essential ingredient in the indicated ratio, and may contain various flavors or natural carbohydrates as additional ingredients, as in general beverages. . Examples of the natural carbohydrates described above include conventional sugars such as monosaccharide maltose such as glucose and fructose, polysaccharides such as disaccharide dextrin such as sucrose and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. Can be. As flavoring agents other than those mentioned above, natural flavoring agents (tauumatin, stevia extract (for example, baudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can also be used. The proportion of the natural carbohydrate is generally about 1 to 20 g, preferably about 5 to 12 g per 100 ml of the composition of the present invention.
또한 상기 외 여러 가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 충진제(치즈, 초콜릿 등), 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제, 풍미 증진을 위해 대추, 감초 등의 생약 추출물 등을 함유할 수 있다. 그 밖에 본 발명의 건강기능식품은 천연 과일 쥬스 및 과일 쥬스 음료 및 야채 음료의 제조를 위한 과육을 함유할 수 있다. 이러한 성분들은 독립적으로 또는 조합하여 사용할 수 있다. 이러한 첨가제의 비율은 그다지 중요하진 않지만 본 발명의 건강기능식품 100 중량부 당0.01 내지 약 20 중량부의 범위에서 선택하는 것이 일반적이다.In addition, various nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, such as colorants and fillers (cheese, chocolate, etc.), pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protection Sex colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated beverages, and may contain herbal extracts such as jujube, licorice to enhance flavor. In addition, the health functional food of the present invention may contain fruit flesh for the production of natural fruit juice and fruit juice beverage and vegetable beverage. These components can be used independently or in combination. The ratio of such additives is not critical but is generally selected from 0.01 to about 20 parts by weight per 100 parts by weight of the health functional food of the present invention.
이하 본 발명의 바람직한 실시예 및 비교예를 기재한다. 그러나 하기한 실시에는 본 발명의 바람직한 일 실시예일뿐 본 발명이 하기한 실시예에 한정되는 것은 아니다.Hereinafter, preferred examples and comparative examples of the present invention are described. However, the following embodiments are only preferred embodiments of the present invention, and the present invention is not limited to the following embodiments.
(실시예 1: 크리신의 아데닐릴 사이클라제 활성에 미치는 영향)Example 1 Effect of Chrysine on Adenylyl Cylase Activity
크리신을 1, 3, 10, 30 및 100uM의 농도로 각각 전처리한 후 포스콜린(Forskolin)에 의한 아데닐릴 사이클라제 활성에 따른 cAMP 생성량에 미치는 영향을 검사하였다. 신경교세포 C6 세포에 크리신을 전처리 한 뒤 10분 후 포스콜린을 처리하고 20분 후 세포를 융해시켜 세포질액을 취하였다. 세포 융해전의 모든 실험 용매에는 cAMP의 분해를 막는 Ro20-1724를 함유하였다. 그 후 세포질액을 섭씨 60도 오븐에서 건조시킨 뒤 이를 생리완충액(또는 TE 용액) 200microliter로 재용해시킨 뒤 이를 방사능 표지된 cAMP([3H]-cAMP)와 cAMP 결합단백질(cAMP binding protein)을 함께 넣고 2시간 섭씨 4도에 냉장보관하여 반응시켰다. 이후, 결합단백질에 결합되지 않은 cAMP를 활성탄 분말(Charcoal)을 넣어 흡착, 원심분리하고 상등액을 취하여 액상 폭광 계수기(liquid scintillation counter)로 방사능을 측정함으로써 결합단백질에 결합된 방사능 표지된 cAMP의 양을 측정하였다. 이러한 과정에서 농도를 알고 있는 cAMP를 대조군으로 하여 각각의 방사능을 구한 뒤 원하는 검체의 방사능을 이들과 비교함으로써 cAMP 생성량을 측정하였다. 그 결과를 도 1에 도시하였다. 도 1에서 보는 바와 같이 포스콜린을 처리하였을 때 유도되는 아데닐릴 사이클라제 활성이 크리신 처리 농도의 증가함에 따라 억제되는 것을 알 수 있다. After the pre-treatment of crysin at concentrations of 1, 3, 10, 30 and 100 uM, respectively, the effects on cAMP production according to adenylyl cyclase activity by Forskolin were examined. After 10 minutes after pretreatment with the glial C6 cells treated with phospholine, 20 minutes later, the cells were fused to obtain cytoplasm. All experimental solvents prior to cell fusion contained Ro20-1724 which prevented the degradation of cAMP. The cytosol was then dried in an oven at 60 degrees Celsius and redissolved with 200 microliters of physiological buffer (or TE solution), followed by radiolabeled cAMP ([ 3 H] -cAMP) and cAMP binding protein (cAMP binding protein). Put together and refrigerated at 4 degrees Celsius for 2 hours to react. Then, the amount of radiolabeled cAMP bound to the binding protein was determined by adding activated carbon powder (Charcoal) to adsorbed, centrifuged, supernatant, and measuring the radioactivity with a liquid scintillation counter. Measured. In this process, cAMP production was measured by comparing the radioactivity of a desired sample with each of the radioactivity of the known cAMP concentration as a control. The results are shown in FIG. As shown in FIG. 1, it can be seen that adenylyl cyclase activity induced by treatment with phoscholine is inhibited by increasing the concentration of chrysine treatment.
(실시예 2: 크리신의 ACTH 수용체 및 히스타민 수용체 활성에 미치는 영향)Example 2: Effect of Chrysine on ACTH Receptor and Histamine Receptor Activity
크리신을 100uM 전처리 한 후 ACTH와 히스타민에 의한 ACTH수용체 및 히스타민 수용체 활성에 따른 cAMP 생성량에 미치는 영향을 검사하였다. 부신 피질 세포(Adrenal Cortex cell)와 HL-60 혈구 세포에 크리신을 전처리한 뒤 10분 후 각각 ACTH와 히스타민을 처리하고 20분 후 세포를 융해시켜 세포질액을 취하였다. 세포 융해전의 모든 실험 용매에는 cAMP의 분해를 막는 Ro20-1724를 함유하였다. 그 후 세포질액을 섭씨 60도 오븐에서 건조시킨 뒤 이를 생리완충액 (또는 TE 용액) 200microliter로 재 용해 시킨 뒤 이를 방사능 표지된 cAMP ([3H]-cAMP)와 cAMP 결합단백질(cAMP binding protein)을 함께 넣고 2시간 섭씨 4도에 냉장보관하여 반응시켰다. 이후, 결합단백질에 결합되지 않은 cAMP를 활성탄 분말(Charcoal)을 넣어 흡착, 원심분리하고 상등액을 취하여 액상 폭광 계수기(liquid scintillation counter)로 방사능을 측정함으로써 결합단백질에 결합된 방사능 표지된 cAMP의 양을 측정하였다. 이러한 과정에서 농도를 알고 있는 cAMP를 대조군으로 하여 각각의 방사능을 구한 뒤 원하는 검체의 방사능을 이들과 비교함으로써 cAMP 생성량을 측정하였다. 그 결과를 도 2a와 도 2b에 도시하였다. 도 2a 및 도 2b에서 보는 바와 같이 ACTH와 히스타민을 처리하였을 때 유도되는 ACTH수용체와 히스타민 수용체 활성에 의한 cAMP생성이 크리신 전처리에 따라 억제되는 것을 알 수 있다. After 100 uM of chrysine, the effects of ACTH and histamine on ACTH receptor and histamine receptor activity were examined. After 10 minutes of pretreatment with chrysine to adrenal cortex cells and HL-60 blood cells, ACTH and histamine were treated, and after 20 minutes, cells were fused to obtain cytoplasm. All experimental solvents prior to cell fusion contained Ro20-1724 which prevented the degradation of cAMP. The cytosol was then dried in an oven at 60 degrees Celsius and re-dissolved with 200 microliters of physiological buffer (or TE solution), followed by radiolabeled cAMP ([ 3 H] -cAMP) and cAMP binding protein (cAMP binding protein). Put together and refrigerated at 4 degrees Celsius for 2 hours to react. Then, the amount of radiolabeled cAMP bound to the binding protein was determined by adding activated carbon powder (Charcoal) to adsorbed, centrifuged, supernatant, and measuring the radioactivity with a liquid scintillation counter. Measured. In this process, cAMP production was measured by comparing the radioactivity of a desired sample with each of the radioactivity of the known cAMP concentration as a control. The results are shown in Figures 2a and 2b. As shown in Figure 2a and Figure 2b it can be seen that the cAMP production by ACTH receptor and histamine receptor activity induced when ACTH and histamine is treated according to the crysin pretreatment.
(실시예 3: 크리신의 Edema factor 활성에Example 3: Edema factor activity of chrysin 미치는 영향)Impact)
크리신을 1, 3, 10, 및 30 uM 농도로 전처리한 후 Edema factor 활성에 따른 cAMP 생성량에 미치는 영향을 검사하였다. CHO 세포에 크리신을 전처리한 뒤 1시간 후 Protective antigen과 Edema factor를 처리하고 3시간 후 세포를 융해시켜 세포질액을 취하였다. 세포 융해전의 모든 실험 용매에는 cAMP의 분해를 막는Ro20-1724를 함유하였다. 그 후 세포질액을 섭씨 60도 오븐에서 건조시킨 뒤 이를 생리완충액 (또는 TE 용액) 200 microliter로 재 용해시킨 뒤 이를 방사능 표지된 cAMP ([3H]-cAMP)와 cAMP 결합단백질(cAMP binding protein)을 함께 넣고 2시간 섭씨 4도에 냉장보관하여 반응시켰다. 이후, 결합단백질에 결합되지 않은 cAMP를 활성탄 분말(Charcoal)을 넣어 흡착, 원심분리하고 상등액을 취하여 액상 폭광 계수기(liquid scintillation counter)로 방사능을 측정함으로써 결합단백질에 결합된 방사능 표지된 cAMP의 양을 측정하였다. 이러한 과정에서 농도를 알고 있는 cAMP를 대조군으로 하여 각각의 방사능을 구한 뒤 원하는 검체의 방사능을 이들과 비교함으로써 cAMP 생성량을 측정하였다. 그 결과를 도 3에 도시하였다. 도3에 도시된 바와 같이 Edema factor를 처리하였을 때 유도되는 cAMP 생성이 크리신 처리 농도의 증가함에 따라 억제되는 것을 알 수 있다. After pre-treatment with chrysine at concentrations of 1, 3, 10, and 30 uM, the effects on cAMP production according to Edema factor activity were examined. After pretreatment of Crysin to CHO cells, protective antigen and Edema factor were treated 1 hour later, and cells were lysed after 3 hours to obtain cytoplasm. All experimental solvents before cell fusion contained Ro20-1724, which prevents the degradation of cAMP. The cytosol was then dried in an oven at 60 degrees Celsius and re-dissolved with 200 microliters of physiological buffer (or TE solution) and then radiolabeled cAMP ([ 3 H] -cAMP) and cAMP binding protein (cAMP binding protein). Put together and refrigerated at 4 degrees Celsius for 2 hours to react. Then, the amount of radiolabeled cAMP bound to the binding protein was determined by adding activated carbon powder (Charcoal) to adsorbed, centrifuged, supernatant, and measuring the radioactivity with a liquid scintillation counter. Measured. In this process, cAMP production was measured by comparing the radioactivity of a desired sample with each of the radioactivity of the known cAMP concentration as a control. The results are shown in FIG. As shown in FIG. 3, it can be seen that cAMP production induced when the Edema factor is treated is inhibited with increasing the concentration of chrysine treatment.
본 발명의 단순한 변형 또는 변경은 모두 이 분야의 통상의 지식을 가진 자에 의하여 용이하게 실시될 수 있으며 이러한 변형이나 변경은 모두 본 발명의 영역에 포함되는 것으로 볼 수 있다.All simple modifications or changes of the present invention can be easily carried out by those skilled in the art, and all such modifications or changes can be seen to be included in the scope of the present invention.
도 1은 포스콜린을 처리하였을 때 유도되는 아데닐릴 사이클라제 활성이 크리신 처리 농도에 따라 억제되는 것을 나타내는 그래프이고,1 is a graph showing that adenylyl cyclase activity induced by treatment with forskolin is inhibited according to the concentration of chrysine treatment,
도 2a 및 도 2b는 ACTH와 히스타민으로 처리하였을 때 유도되는 cAMP 생성이 크리신 처리에 의해서 억제되는 것을 나타내는 그래프이고,2A and 2B are graphs showing that cAMP production induced when treated with ACTH and histamine is inhibited by chrysine treatment,
도 3은 탄저독소 edema factor를 처리하였을 때 유도되는 cAMP 생성이 크리 신 처리 농도에 따라 억제되는 것을 나타내는 그래프이다.FIG. 3 is a graph showing that cAMP production induced when anthrax toxin edema factor is treated is suppressed according to the concentration of chrysin treatment.
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| CN103405408B (en) * | 2013-06-27 | 2015-11-11 | 天津医科大学总医院 | The application of chrysin in treatment ischemic cerebral apoplexy Chinese medicine |
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