KR102563878B1 - Composition for preventing, improving or treating prostate disease comprising extract of Cirsium japonicum De Candole as effective component - Google Patents
Composition for preventing, improving or treating prostate disease comprising extract of Cirsium japonicum De Candole as effective component Download PDFInfo
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- KR102563878B1 KR102563878B1 KR1020210118201A KR20210118201A KR102563878B1 KR 102563878 B1 KR102563878 B1 KR 102563878B1 KR 1020210118201 A KR1020210118201 A KR 1020210118201A KR 20210118201 A KR20210118201 A KR 20210118201A KR 102563878 B1 KR102563878 B1 KR 102563878B1
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- extract
- candole
- cirsium japonicum
- prostate
- prostatic hyperplasia
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Abstract
본 발명이 해결하고자 하는 과제는 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방, 개선 또는 치료용 조성물을 제공하는 것이다. 본 발명은 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선질환의 예방 또는 치료용 약학 조성물이다.An object to be solved by the present invention is to provide a composition for preventing, improving or treating prostate diseases, comprising Cirsium japonicum De Candole extract as an active ingredient. The present invention is a pharmaceutical composition for the prevention or treatment of prostate disease comprising an extract of Cirsium japonicum De Candole as an active ingredient.
Description
본 발명은 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방, 개선 또는 치료용 조성물에 관한 것이다.The present invention relates to a composition for the prevention, improvement or treatment of prostate disease comprising Cirsium japonicum De Candole extract as an active ingredient.
전립선은 요도가 건조해지지 않도록 여러 가지 분비물을 만들어 내는 장기로, 남성 호르몬인 안드로겐과 밀접한 관련이 있다. 분비가 증가함에 따라 점점 커지는데, 20~30대의 전립선이 50대까지 유지되다 그 이후부터 비대해진다. 이것을 양성 전립선 비대증이라고 하며, 호르몬 치료로 크기를 정상으로 돌려놓았다 하더라도 부작용의 위험이 크고, 호르몬 치료를 멈추면 곧 원상 복귀되기 때문에 완치하기 어렵다.The prostate is an organ that produces various secretions to prevent the urethra from drying out, and is closely related to androgens, male hormones. As the secretion increases, it gradually enlarges, and the prostate in the 20s and 30s is maintained until the 50s and then enlarges. This is called benign prostatic hyperplasia, and even if the size is returned to normal by hormone treatment, the risk of side effects is high, and it is difficult to cure because it returns to its original state soon after hormone treatment is stopped.
전립선에 발생하는 대표적인 질환은 전립선 비대증, 만성 전립선염 및 전립선암이 있다. 전립선염은 다양한 원인이 있지만 주로 세균 감염, 원인 모를 염증, 만성통증의 일환으로 생기는 질환이고, 전립선암은 전립선 중 비교적 바깥쪽부분에 악성 종양이 생긴 것인데, 미국의 한 조사 결과에 따르면, 전립선암이 전체 남성 암환자 중 약 35%를 차지하고 있으며, 매년 2~3%씩 증가하고 있다고 한다. 우리나라에서의 발생 빈도는 10만 명당 세 명으로 아직까지 걱정할 수위는 아니지만, 점차 서구적으로 변해가는 식생활이나 급격히 불어나는 노년층 인구로 그 비율이 점차 높아지고 있다.Representative diseases occurring in the prostate include benign prostatic hyperplasia, chronic prostatitis and prostate cancer. Prostatitis has various causes, but it is a disease that occurs mainly as a part of bacterial infection, inflammation of unknown cause, and chronic pain, and prostate cancer is a malignant tumor in the relatively outer part of the prostate. According to a survey in the United States, prostate cancer It accounts for about 35% of all male cancer patients, and is increasing by 2-3% every year. The frequency of occurrence in Korea is three per 100,000 people, which is not yet a level of concern, but the rate is gradually increasing due to the rapidly changing diet and rapidly increasing elderly population.
한편, 전립선 비대증(Benign prostatic hyperplasia, BPH)은 노화와 성호르몬의 불균형의 영향으로 요도 주위 전립선 '샘조직'이 커져 요도를 압박하여 배뇨증상이 나타나는 질환으로, 남성의 50세 이후 발병이 급격히 일어나는 남성질환이다. 최근 우리나라에서 전립선 비대증 질환자의 증가율이 매년 20%를 상회할 정도로 가파른 증가 추세이며, 전립선 이행대 부분의 평활근(smooth cell)과 상피세포(epithelial)의 과도한 증식으로 야기되고, 전립선 비대증은 하부요로증상을 동반하는데, 이는 비대해진 전립선에 의한 해부학적 폐색과 전립선 평활근을 수축시키는 α1-수용체에 의한 기능적 폐색에 기인하는 것으로 알려져 있다. 폐색에 의한 주요 증상으로는 소변 줄기가 가늘고 약해지는 세뇨 또는 약뇨, 소변을 시작할 때 한참 기다려야 하는 지연뇨, 소변 중 의지와 관계없이 중단되는 배뇨중단, 소변 후 물방울처럼 떨어지는 배뇨 말기 적하, 및 잔뇨감 등이 대표적이다. 전립선 비대의 다양한 기전 중에서 대표적인 기전은 남성호르몬인 테스토스테론(testosterone, T)과 디하이드로테스토스테론(dihydrotestosterone, DHT)이 관련되어 있다고 알려져 있다.On the other hand, Benign prostatic hyperplasia (BPH) is a disease in which the prostate 'glandular tissue' around the urethra enlarges under the influence of aging and imbalance of sex hormones and compresses the urethra, resulting in urination symptoms. It occurs rapidly after the age of 50 in men. It is a male disease. Recently, the rate of increase in patients with BPH in Korea is rapidly increasing, exceeding 20% every year, and it is caused by excessive proliferation of smooth cells and epithelial cells in the prostate transition zone. It is known to be caused by anatomical obstruction by an enlarged prostate and functional obstruction by α1-receptors that contract prostatic smooth muscle. The main symptoms due to obstruction are thin urine or weak urine stream, delayed urine that requires a long wait to start urinating, cessation of urination that stops regardless of the will while urinating, dripping at the end of urination that falls like water droplets after urinating, and a feeling of residual urine, etc. This is typical. Among various mechanisms of prostatic hyperplasia, it is known that a representative mechanism is related to male hormones, testosterone (T) and dihydrotestosterone (DHT).
한편, 대계(Cirsium japonicum De Candole)는 국화과의 엉겅퀴 또는 기타 같은 속에 포함된 근연식물의 전초를 의미한다. 대계는 혈열(血熱)을 식히고 지혈시키는 효능이 있으며 어혈을 없애고 옹종(癰腫)을 치료하기도 한다. 따라서 열로 인한 각혈, 코피, 자궁출혈, 소변출혈, 외상으로 인한 출혈 및 부스럼 등에 활용할 수 있으며, 약리작용으로 지혈작용, 혈압강하작용, 항균작용 등이 보고되어 있다.On the other hand, Daegye ( Cirsium japonicum De Candole ) refers to the outpost of thistle or other related plants included in the same genus of Asteraceae. Daegye has the effect of cooling blood fever and hemostasis, eliminating blood stasis and treating carbuncles. Therefore, it can be used for hemoptysis due to heat, nosebleeds, uterine bleeding, urine bleeding, bleeding and swelling due to trauma, and hemostasis, blood pressure lowering action, and antibacterial action have been reported as pharmacological actions.
한국등록특허 제1522273호 및 한국등록특허 제1793379호에는 전립선 비대증의 예방 및 효과로 안드로겐 수용체 감소 및 전립선 무게 감소 효과를 나타내는 울금 추출물 및 조각자 가시 추출물에 대하여 개시되어 있으나, 본 발명의 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방, 개선 또는 치료용 조성물에 대해서는 개시된 바 없다.Korean Patent No. 1522273 and Korean Patent No. 1793379 disclose a turmeric extract and a thorn extract showing an androgen receptor reduction and prostate weight reduction effect through the prevention and effect of prostatic hyperplasia, but the present invention ( Cirsium japonicum De Candole ) There is no disclosure of a composition for preventing, improving or treating prostate diseases comprising an extract as an active ingredient.
본 발명이 해결하고자 하는 과제는 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방, 개선 또는 치료용 조성물을 제공하는 것이다.An object to be solved by the present invention is to provide a composition for preventing, improving or treating prostate diseases, comprising Cirsium japonicum De Candole extract as an active ingredient.
본 발명은 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선질환의 예방 또는 치료용 약학 조성물을 제공한다.The present invention provides a pharmaceutical composition for the prevention or treatment of prostate disease comprising Cirsium japonicum De Candole extract as an active ingredient.
상기 대계(Cirsium japonicum De Candole) 추출물의 추출용매는 물, C1~C4의 저급 알코올 또는 이들의 혼합물일 수 있다.The extraction solvent of the Cirsium japonicum De Candole extract may be water, C1-C4 lower alcohol, or a mixture thereof.
상기 전립선 질환은 전립선염, 전립선 비대증 또는 전립선 비대에 의한 하부요로증일 수 있다.The prostate disease may be prostatitis, benign prostatic hyperplasia or lower urinary tract disease due to benign prostatic hyperplasia.
상기 대계(Cirsium japonicum De Candole) 추출물은 전립선 평활근을 이완시킬 수 있다.The mackerel ( Cirsium japonicum De Candole ) extract can relax the smooth muscle of the prostate.
상기 전립선 평활근 이완은 칼륨 채널(potassium channel)의 활성화에 의한 것일 수 있다. The prostate smooth muscle relaxation may be due to activation of a potassium channel.
또한 본 발명은 약학 조성물을 유효성분으로 포함하는 전립선 질환에 의한 배뇨장애 개선제를 제공한다.In addition, the present invention provides an agent for improving dysuria caused by prostate disease, comprising a pharmaceutical composition as an active ingredient.
또한 본 발명은 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방 또는 개선용 건강 기능식품 조성물을 제공한다.In addition, the present invention provides a health functional food composition for preventing or improving prostate disease, containing Cirsium japonicum De Candole extract as an active ingredient.
본 발명은 전립선 평활근을 이완시킴으로써 전립선 비대증과 같은 전립선 질환을 예방 및 치료하고, 전립선 비대증과 동반하는 하부요로증, 빈뇨, 야간뇨 등과 같은 배뇨장애 증상을 개선시킬 수 있다.The present invention can prevent and treat prostate diseases such as benign prostatic hyperplasia by relaxing the prostatic smooth muscle, and can improve symptoms of dysuria such as lower urinary tract disease, frequent urination, and nocturia accompanying benign prostatic hyperplasia.
도 1은 본 발명의 대계(Cirsium japonicum De Candole) 추출물에 의한 전립선 평활근의 이완 효과를 확인한 결과이다.
도 2는 본 발명의 대계(Cirsium japonicum De Candole) 추출물에 의한 전립선 평활근 이완이 NOS에 의해 조절되는지를 확인한 결과이다.
도 3은 본 발명의 대계(Cirsium japonicum De Candole) 추출물에 의한 전립선 평활근의 이완효과가 칼륨 채널(potassium channel)의 활성화를 통한 과분극 조절을 통해 이루어지는 것을 확인한 결과이다.1 is a result of confirming the relaxation effect of prostate smooth muscle by the extract of Cirsium japonicum De Candole of the present invention.
2 is a result confirming whether the prostate smooth muscle relaxation by the extract of Cirsium japonicum De Candole of the present invention is regulated by NOS.
3 is a result confirming that the relaxation effect of the prostate smooth muscle by the Cirsium japonicum De Candole extract of the present invention is achieved through the hyperpolarization control through the activation of the potassium channel.
본 발명은 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방 또는 치료용 약학 조성물에 관한 것이다.The present invention relates to a pharmaceutical composition for the prevention or treatment of prostate disease comprising an extract of Cirsium japonicum De Candole as an active ingredient.
상기 전립선 질환은 전립선 비대증, 전립선암 또는 전립선염인 것이 바람직하지만 이에 한정하지 않으며, 더 바람직하게는 전립선 비대증이고, 전립선 비대증에 의한 배뇨장애를 포함할 수 있으며, 상기 배뇨장애는 하부요로증, 빈뇨, 야간뇨 등을 포함할 수 있다.The prostate disease is preferably, but not limited to, benign prostatic hyperplasia, prostate cancer or prostatitis, more preferably benign prostatic hyperplasia, and may include dysuria caused by benign prostatic hyperplasia, wherein the dysuria is lower urinary tract disease, frequent urination. , nocturia, etc.
상기 대계(Cirsium japonicum De Candole) 추출물은 하기의 단계를 포함하는 방법에 의해 제조할 수 있으나, 이에 한정하지 않는다:The mackerel ( Cirsium japonicum De Candole ) extract may be prepared by a method comprising the following steps, but is not limited thereto:
(1) 대계(Cirsium japonicum De Candole)에 추출용매를 가하여 추출하는 단계;(1) extracting by adding an extraction solvent to Cirsium japonicum De Candole ;
(2) 단계 (1)의 추출물을 여과하는 단계; 및(2) filtering the extract of step (1); and
(3) 단계 (2)의 여과한 추출물을 감압 농축하고 건조하여 추출물을 제조하는 단계.(3) preparing an extract by concentrating the filtered extract of step (2) under reduced pressure and drying.
상기 단계 (1)에서 추출용매는 물, C1~C4의 저급 알코올 또는 이들의 혼합물 중에서 선택하는 것이 바람직하며, 더 바람직하게는 C1~C4의 저급 알코올이고, 더욱 더 바람직하게는 95%(v/v) 에틸알코올(Ethyl alcohol)이지만 이에 한정하지 않는다.In the step (1), the extraction solvent is preferably selected from water, C1-C4 lower alcohols, or mixtures thereof, more preferably C1-C4 lower alcohols, and still more preferably 95% (v/ v) Ethyl alcohol, but is not limited thereto.
상기 제조방법에 있어서, 추출방법은 여과법, 열수 추출, 침지 추출, 환류 냉각 추출 및 초음파 추출 등의 당업계에 공지된 모든 통상적인 방법을 이용할 수 있다. 상기 추출용매는 건조된 대계(Cirsium japonicum De Candole) 중량의 1~20배 첨가하여 추출하는 것이 바람직하며, 더 바람직하게는 5~15배 첨가하는 것이다. 추출온도는 4 내지 50℃인 것이 바람직하나 이에 한정하지 않는다. 또한, 추출시간은 0.5~10시간인 것이 바람직하며, 0.5~5시간이 더욱 바람직하나 이에 한정하지 않는다. 상기 방법에 있어서, 단계 (3)의 감압농축은 진공 감압 농축기 또는 진공회전증발기를 이용하는 것이 바람직하나 이에 한정하지 않는다. 또한, 건조는 감압건조, 진공건조, 비등건조, 분무 건조 또는 동결 건조하는 것이 바람직하나 이에 한정하지 않는다.In the above production method, as the extraction method, all conventional methods known in the art such as filtration, hot water extraction, immersion extraction, reflux cooling extraction, and ultrasonic extraction may be used. The extraction solvent is preferably extracted by adding 1 to 20 times the weight of dried Daegye ( Cirsium japonicum De Candole ), more preferably 5 to 15 times. The extraction temperature is preferably 4 to 50 ° C, but is not limited thereto. In addition, the extraction time is preferably 0.5 to 10 hours, more preferably 0.5 to 5 hours, but is not limited thereto. In the above method, the vacuum concentration in step (3) is preferably performed using a vacuum vacuum concentrator or a vacuum rotary evaporator, but is not limited thereto. In addition, drying is preferably performed under reduced pressure, vacuum drying, boiling drying, spray drying or freeze drying, but is not limited thereto.
상기 대계(Cirsium japonicum De Candole) 추출물은 전립선 평활근을 이완시킬 수 있으며, 상기 전립선 평활근 이완은 전립선 평활근 이완은 칼륨(K) 채널의 활성화에 의한 것일 수 있다.The mackerel ( Cirsium japonicum De Candole ) extract can relax the prostate smooth muscle, and the prostate smooth muscle relaxation may be due to the activation of potassium (K) channels.
상기 대계(Cirsium japonicum De Candole) 추출물은 요도 또는 전립선 평활근을 이완시킬 수 있으며, 상기 전립선 평활근의 이완은 NOS 조절에 의한 것일 수 있다.The mackerel ( Cirsium japonicum De Candole ) extract can relax urethral or prostate smooth muscle, and the relaxation of the prostate smooth muscle may be due to NOS regulation.
본 발명의 약학 조성물은 상기 대계(Cirsium japonicum De Candole) 추출물 이외에 추가로 담체, 부형제 또는 희석제를 더 포함할 수 있다.The pharmaceutical composition of the present invention may further include a carrier, excipient or diluent in addition to the Cirsium japonicum De Candole extract.
본 발명의 약학 조성물은 경구 또는 비경구로 투여될 수 있으며, 비경구 투여 시 피부 외용 또는 복강 내, 직장, 정맥, 근육, 피하, 자궁 내 경막 또는 뇌혈관 내 주사 방식을 선택하는 것이 바람직하다.The pharmaceutical composition of the present invention may be administered orally or parenterally, and in the case of parenteral administration, it is preferable to select an external skin or intraperitoneal, rectal, intravenous, intramuscular, subcutaneous, intrauterine intrathecal or intracerebrovascular injection method.
본 발명의 약학 조성물은 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제될 수 있다. 경구투여를 위한 고형 제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형 제제는 하나 이상의 화합물에 적어도 하나 이상의 부형제 예를 들면, 전분, 탄산칼슘, 수크로오스(sucrose) 또는 락토오스(lactose), 젤라틴 등을 섞어 조제된다. 또한, 단순한 부형제 이외에 스테아린산 마그네슘, 탈크 등과 같은 윤활제들도 사용된다. 경구 투여를 위한 액상 제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순 희석제인 물, 리퀴드 파라핀 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다. 비경구 투여를 위한 제제에는 멸균된 수용액, 비수성 용제, 현탁제, 유제, 동결건조제제, 좌제가 포함된다. 비수성 용제 및 현탁 용제로는 프로필렌글리콜(propylene glycol), 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다. 좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈tween) 61, 카카오지, 라우린지, 글리세로 젤라틴 등이 사용될 수 있다.The pharmaceutical composition of the present invention may be prepared using diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, and surfactants. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and these solid preparations include at least one excipient in one or more compounds, for example, starch, calcium carbonate, sucrose or lactose ( lactose) and gelatin. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid formulations for oral administration include suspensions, internal solutions, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, aromatics, and preservatives may be included. there is. Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solvents, suspensions, emulsions, freeze-dried formulations, and suppositories. Propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate may be used as non-aqueous solvents and suspending solvents. As the base of the suppository, witepsol, macrogol, tween) 61, cacao butter, laurin paper, glycerogelatin, etc. may be used.
본 발명에 따른 조성물은 약제학적으로 유효한 양으로 투여한다. 본 발명에 있어서, "약제학적으로 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 발명의 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 부작용없이 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, "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 based on the type, severity, and activity of the drug in the patient. , sensitivity to the drug, time of administration, route of administration and excretion rate, duration of treatment, factors including drugs used concurrently, and other factors well known in the medical field. The composition of the present invention may be administered as an individual therapeutic agent or in combination with other therapeutic agents, may be administered sequentially or simultaneously with conventional therapeutic agents, and may be administered single or multiple times. Considering all of the above factors, it is important to administer an amount that can obtain the maximum effect with the minimum amount without side effects, which can be easily determined by those skilled in the art.
본 발명의 조성물의 투여량은 환자의 체중, 연령, 성별, 건강상태, 식이, 투여시간, 투여방법, 배설률 및 질환의 중증도에 따라 그 범위가 다양하게 사용할 수 있다.The dosage of the composition of the present invention can be used in a variety of ranges depending on the patient's body weight, age, sex, health condition, diet, administration time, administration method, excretion rate, and severity of the disease.
또한, 본 발명은 상기 약학 조성물을 유효성분으로 포함하는 전립선 질환에 의한 배뇨장애 개선제에 관한 것이다.In addition, the present invention relates to an agent for improving dysuria due to prostate disease, comprising the pharmaceutical composition as an active ingredient.
또한, 본 발명은 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방 또는 개선용 건강기능식품 조성물에 관한 것이다.In addition, the present invention relates to a health functional food composition for preventing or improving prostate disease comprising Cirsium japonicum De Candole extract as an active ingredient.
상기 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방 또는 개선용 건강기능식품 조성물은 음료, 환, 정제(tablet), 캡슐제(capsule), 산제 중에서 선택된 어느 하나로 제조하거나, 식품의 성분으로 첨가하여 제조될 수 있으며, 통상적인 방법에 따라 적절하게 제조될 수 있다.The health functional food composition for preventing or improving prostate disease containing Cirsium japonicum De Candole extract as an active ingredient is prepared as any one selected from beverages, pills, tablets, capsules, and powders, It can be prepared by adding it as a component of food, and can be appropriately prepared according to conventional methods.
본 발명의 대계(Cirsium japonicum De Candole) 추출물을 첨가할 수 있는 식품의 일례로는 육류, 소시지, 빵, 초콜릿, 캔디류, 스넥류, 과자류, 피자, 라면, 기타 면류, 껌류, 아이스크림류를 포함한 낙농제품, 각종 스프, 음료수, 차, 드링크제, 알코올 음료 및 비타민 복합제 중에서 선택된 어느 하나의 형태일 수 있으며, 통상적인 의미에서의 건강기능식품을 모두 포함한다.Dairy products , including meat, sausages, bread, chocolate, candies, snacks, confectionery, pizza, ramen, other noodles, chewing gum, and ice cream, are examples of foods to which the extract of the present invention can be added. , It may be in any one form selected from various soups, beverages, tea, drinks, alcoholic beverages, and vitamin complexes, and includes all health functional foods in the conventional sense.
상기 건강기능식품은 여러 가지 영양제, 비타민, 광물(전해질), 합성 및 천연 풍미제, 착색제 및 증진제(치즈, 초콜릿 등), 펙트산 및 그의 염, 알킨산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 함유할 수 있다. 그 밖에 천연 과일 주스 및 야채 음료의 제조를 위한 과육을 함유할 수 있다. 이러한 성분은 독립적으로 또는 조합하여 사용할 수 있다.The health functional food includes various nutrients, vitamins, minerals (electrolytes), synthetic and natural flavors, coloring agents and enhancers (cheese, chocolate, etc.), pectic acids and their salts, alkynic acids and their salts, organic acids, protective colloidal thickeners , pH regulators, stabilizers, preservatives, glycerin, alcohol, carbonation agents used in carbonated beverages, and the like. In addition, it may contain fruit flesh for the production of natural fruit juice and vegetable beverages. These components may be used independently or in combination.
본 발명의 건강기능식품 조성물은 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상기 천연 탄수화물은 포도당, 과당과 같은 모노사카라이드, 말토스, 슈크로스와 같은 디사카라이드, 및 덱스트린, 사이클로덱스트린과 같은 폴리사카라이드, 자일리톨, 소르비톨, 에리트리톨 등의 당알콜이다. 감미제로서는 타우마틴, 스테비아 추출물과 같은 천연 감미제나, 사카린, 아스파르탐과 같은 합성 감미제 등을 사용할 수 있다.The health functional food composition of the present invention may contain various flavoring agents or natural carbohydrates as additional components. The natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As the sweetener, natural sweeteners such as thaumatin and stevia extract, or synthetic sweeteners such as saccharin and aspartame may be used.
이하, 실시예를 이용하여 본 발명을 더욱 상세하게 설명하고자 한다. 이들 실시예는 오로지 본 발명을 보다 구체적으로 설명하기 위한 것으로 본 발명의 범위가 이들에 의해 제한되지 않는다는 것은 당해 기술분야에서 통상의 지식을 가진 자에게 있어 자명한 것이다.Hereinafter, the present invention will be described in more detail using examples. These examples are only for explaining the present invention in more detail, and it is obvious to those skilled in the art that the scope of the present invention is not limited thereto.
실시예 1 : 대계(Example 1: Subsystem ( Cirsium japonicum De CandoleCirsium japonicum De Candole ) 추출물의 제조) preparation of the extract
광명당제약에서 대계(Cirsium japonicum De Candole)를 구매하여, 한국식물추출물은행(Korea Plant Extract Bank)에 의뢰하여 대계(Cirsium japonicum De Candole) 추출물을 제조하였으며, 이때, 추출용매로는 95%(v/v)의 에틸알코올(Ethyl alcohol)(GR grade)을 사용하였고, 6.89% 추출수율로 11.20g을 분양받았다. Cirsium japonicum De Candole was purchased from Kwang Myung Dang Pharmaceutical Co., Ltd., and the Korea Plant Extract Bank was commissioned to manufacture Cirsium japonicum De Candole extract. At this time, 95% (v /v) of ethyl alcohol (GR grade) was used, and 11.20 g was distributed with an extraction yield of 6.89%.
분양 받은 대계(Cirsium japonicum De Candole) 추출물을 DMSO(Dimethyl Sulfoxide)에 녹여 스톡(stock)를 제조하여 사용하였다.The pre-sale ( Cirsium japonicum De Candole ) extract was dissolved in DMSO (Dimethyl Sulfoxide) to prepare a stock (stock) and used.
실시예 2 : 대계(Example 2: Subsystem ( Cirsium japonicum De CandoleCirsium japonicum De Candole ) 추출물의 전립선 이완효과 확인) Confirmation of the prostate relaxing effect of the extract
실험동물은 13~14주령 수컷 SD(Sprague Dawley) 랫트를 CO2 가스가 들어있는 데시케이터에서 1~2분간 마취시키고, 경추탈구법(Cervical dislocation) 이후, 신속하게 방광과 근위부 요도 부위를 적출하여 전립선 주변부의 capsular muscle 층을 깨끗이 제거하였다. 실험에 사용된 생리학적 용액은 modified Kreb's 용액을 사용하였으며, 그 조성은 하기 표 1에 개시하였다. 이하 전립선의 주변 지방조직 및 결합조직을 제거한 후 실험하였다Experimental animals are 13-14 weeks old male SD (Sprague Dawley) rats anesthetized for 1-2 minutes in a desiccator containing CO 2 gas, and after cervical dislocation, the bladder and proximal urethra are quickly removed The capsular muscle layer around the prostate was clearly removed. The physiological solution used in the experiment was a modified Kreb's solution, and its composition is shown in Table 1 below. Hereafter, the test was performed after removing the adipose tissue and connective tissue around the prostate.
조직절편은 3~5mm 길이의 절편으로 자르고 실험에 이용하였다. 조직 절편을 텅스텐 와이어로 제작한 고리에 단일 실크섬유로 매듭을 지어 장착한다. 두 개의 텅스텐 고리 중 한쪽은 organ bath 하단에, 다른 한쪽은 Isometric transducer(havard bioscience 52-9503)에 연결한다. 전립선 조직은 실험기간 동안 95% O2와 5% CO2 혼합가스를 지속적으로 공급하여 생리학적 pH를 유지하도록 한다. 등척성 수축은 디지털/아날로그 변환기(Powerlab PL3504/P, ADIinstruments)를 통해 컴퓨터에 저장하였으며, 이후 LabChart Pro(ADIinsturments)를 이용하여 기록 및 분석하였다. 대계(Cirsium japonicum De Candole) 추출물의 전립선 이완 효과를 확인하기 위하여, 10 μM 페닐레프린(Phenylephrine)에 의한 수축 반응이 최고점에 도달하고 지속적인 상태가 되면 준비된 대계 추출물을 각각 0.1, 1, 10, 100, 300 및 500 ㎍/㎖의 농도로 organ bath에 축적되도록 첨가하여 각 시료에 대한 전립선 조직의 수축력의 변화를 관찰하고 dose-response curve를 기록하였다.통계학적 분석은 t-test로 수행하였으며, ** P<0.01, * P<0.05는 vehicle 대조군 (control)과 비교시 유의적으로 차이가 있을 경우를 고려하였고, ## P<0.01, # P<0.05는 inhibitor 들의 처리시와 비교하여 통계적인 유의성을 고려하였다.Tissue sections were cut into 3-5 mm long sections and used in the experiment. Tissue sections are attached to a loop made of tungsten wire by knotting a single silk fiber. One of the two tungsten rings is connected to the bottom of the organ bath and the other to the Isometric transducer (Havard Bioscience 52-9503). Prostate tissue was continuously supplied with a mixed gas of 95% O 2 and 5% CO 2 during the experiment period to maintain physiological pH. Isometric contractions were stored in a computer through a digital/analog converter (Powerlab PL3504/P, ADIinstruments), and then recorded and analyzed using LabChart Pro (ADIinstruments). In order to confirm the prostate relaxing effect of the Cirsium japonicum De Candole extract, when the contraction response by 10 μM phenylephrine reaches its peak and becomes a continuous state, the prepared soybean extract is 0.1, 1, 10, 100 , 300 and 500 μg/ml were added to accumulate in the organ bath, and changes in contractile force of prostate tissue for each sample were observed and a dose-response curve was recorded. Statistical analysis was performed by t-test, * * P<0.01, * P<0.05 were considered when there was a significant difference compared to the vehicle control group (control), ## P<0.01, # P<0.05 were statistically significant compared to the treatment of inhibitors was considered.
도 1을 참조하면, 적출된 흰쥐의 전립선 절편에 10 μM 페닐레프린(Phenylephrine)을 가하여 수축을 유발한 후 대계(Cirsium japonicum De Candole) 추출물을 0.1, 1, 10, 100, 300, 500㎍/㎖의 농도로 organ bath에 축적되게 첨가하여 평활근의 이완을 관찰한 결과, 0.1㎍/㎖의 농도에서부터 전립선 평활근의 유의적 이완을 관찰할 수 있었다. Referring to FIG. 1, 10 μM phenylephrine was applied to prostate sections of isolated rats to induce contraction, and Cirsium japonicum De Candole extract was added at 0.1, 1, 10, 100, 300, 500 μg/ As a result of observing smooth muscle relaxation by adding it to the organ bath at a concentration of ㎖, significant relaxation of prostate smooth muscle could be observed from a concentration of 0.1 μg/㎖.
실시예 3: 대계(Example 3: Subsystem ( Cirsium japonicum De CandoleCirsium japonicum De Candole ) 추출물의 전립선 이완효과에 대한 Nitric oxide (NO) pathway 작용 확인) Confirmation of Nitric oxide (NO) pathway action on the prostate relaxation effect of the extract
대계(Cirsium japonicum De Candole) 추출물에 의한 전립선 이완이 NO synthase (NOS)에 의해 억제되는지 알아보기 위하여, 상기 실시예 2에서 적출한 조직 절편에 100 μM L-NAME(N omega-Nitro-L-arginine methyl ester)를 전처리하고, 0.1, 1, 10, 100, 300, 500㎍/㎖의 대계(Cirsium japonicum De Candole) 추출물을 처리하여 전립선 평활근 이완 효과를 확인하고, 전처리 없이 대계(Cirsium japonicum De Candole) 추출물을 처리한 군과 비교하였다.In order to examine whether the prostate relaxation by the Cirsium japonicum De Candole extract is inhibited by NO synthase (NOS), 100 μM L-NAME (N omega-Nitro-L-arginine methyl ester), and 0.1, 1, 10, 100, 300, 500 μg/ml of Cirsium japonicum De Candole extract to confirm the prostate smooth muscle relaxation effect, and without pretreatment ( Cirsium japonicum De Candole ) The extract was compared with the treated group.
도 2를 참조하면, L-NAME를 전처리한 경우는 전처리 없이 대계(Cirsium japonicum De Candole) 추출물을 처리한 군과 비교하여 전립선 평활근 이완 효과가 감소한 것을 확인할 수 있었으며, 300㎍/㎖ 농도부터 유의적인 이완효과의 억제가 관찰되었다. 이러한 결과로부터 대계(Cirsium japonicum De Candole) 추출물에 의한 전립선 이완은 NOS(nitric oxide synthase)를 활성화 함으로써 평활근 이완효과를 나타내고, Nitric Oxide 경로를 통해 일어나는 것을 알 수 있다.Referring to Figure 2, in the case of L-NAME pre-treatment, it was confirmed that the prostate smooth muscle relaxation effect was reduced compared to the group treated with Cirsium japonicum De Candole extract without pre-treatment, and a significant Inhibition of the relaxing effect was observed. From these results, it can be seen that the prostate relaxation by Cirsium japonicum De Candole extract activates NOS (nitric oxide synthase), thereby exhibiting a smooth muscle relaxation effect and occurring through the Nitric Oxide pathway.
실시예 4 : 칼륨 채널(potassium channel)을 통한 대계(Example 4: Through the potassium channel (potassium channel) passage ( Cirsium japonicum De CandoleCirsium japonicum De Candole ) 추출물의 전립선 이완 효과 확인) Confirmation of the prostate relaxing effect of the extract
실시예 2에서 적출한 조직 절편에 10mM의 TEA(tetraethylammonium)를 전처리하고, 0.1, 1, 10, 100, 300, 500㎍/㎖의 대계 추출물을 organ bath에 축적되도록 첨가하여 전립선 평활근의 이완 효과를 확인하고, 전처리 없이 대계 추출물을 처리한 군과 비교하였다.Tissue sections excised in Example 2 were pretreated with 10 mM TEA (tetraethylammonium), and 0.1, 1, 10, 100, 300, and 500 μg/ml of soybean extract were added to accumulate in an organ bath to increase the relaxation effect of the smooth muscle of the prostate. It was confirmed and compared with the group treated with Daegye extract without pretreatment.
도 3을 참조하면, 전처리 없이 대계(Cirsium japonicum De Candole) 추출물을 처리한 군과 비교할 때, TEA 전처리 한 경우에는 전립선 조직에서의 이완효과가 부분적으로 억제되는 것을 관찰하였다. 이러한 결과로부터 본 발명의 대계(Cirsium japonicum De Candole) 추출물에 의한 전립선 이완은 칼륨 채널(potassium channel)의 활성화를 통한 과분극(hyperpolarization)이 관여함을 알 수 있다.Referring to Figure 3, compared to the group treated with Cirsium japonicum De Candole extract without pretreatment, it was observed that the relaxation effect in prostate tissue was partially suppressed in the case of TEA pretreatment. From these results, it can be seen that hyperpolarization through activation of potassium channels is involved in prostate relaxation by the Cirsium japonicum De Candole extract of the present invention.
이와 같이, 본 발명에 따른 대계(Cirsium japonicum De Candole) 추출물을 유효성분으로 포함하는 전립선 질환의 예방 또는 치료용 조성물은 전립선 평활근을 이완시킴으로써 전립선 비대증과 같은 전립선 질환을 예방 및 치료하고, 전립선 비대증과 동반하는 하부요로증, 빈뇨, 야간뇨 등과 같은 배뇨장애 증상을 개선시킬 수 있다.As such, the composition for preventing or treating prostate diseases comprising Cirsium japonicum De Candole extract as an active ingredient according to the present invention prevents and treats prostate diseases such as benign prostatic hyperplasia by relaxing prostatic smooth muscle, It can improve symptoms of dysuria such as accompanying lower urinary tract disease, frequent urination, and night urination.
이상으로 본 발명의 바람직한 실시예를 상세하게 설명하였다. 본 발명의 설명은 예시를 위한 것이며, 본 발명이 속하는 기술분야에서 통상의 지식을 가진 자는 본 발명의 기술적 사상이나 필수적인 특징을 변경하지 않고서 다른 구체적인 형태는 쉽게 변형이 가능하다는 것을 이해할 수 있을 것이다.Above, preferred embodiments of the present invention have been described in detail. The description of the present invention is for illustrative purposes, and those skilled in the art will understand that other specific forms can be easily modified without changing the technical spirit or essential features of the present invention.
따라서, 본 발명의 범위는 상기 상세한 설명보다는 후술하는 특허청구범위에 의하여 나타내어지며, 특허청구범위의 의미, 범위 및 그 균등 개념으로부터 도출되는 모든 변경 또는 변형된 형태가 본 발명의 범위에 포함되는 것으로 해석되어야 한다.Therefore, the scope of the present invention is indicated by the following claims rather than the above detailed description, and all changes or modifications derived from the meaning, scope and equivalent concept of the claims are included in the scope of the present invention. should be interpreted
Claims (7)
Daegyeol ( Cirsium japonicum De Candole ) A pharmaceutical composition for preventing or treating urination disorders caused by benign prostatic hyperplasia or prostatic hypertrophy, containing an extract as an active ingredient.
상기 대계(Cirsium japonicum De Candole) 추출물의 추출용매는 물, C1~C4의 저급 알코올 또는 이들의 혼합물인 것을 특징으로 하는 전립선 비대증 또는 전립선 비대에 의한 배뇨장애의 예방 또는 치료용 약학 조성물.
According to claim 1,
The extract ( Cirsium japonicum De Candole ) The extraction solvent of the extract is water, a lower alcohol of C1 ~ C4 or a pharmaceutical composition for the prevention or treatment of dysuria due to benign prostatic hyperplasia or prostatic hyperplasia, characterized in that a mixture thereof.
상기 대계(Cirsium japonicum De Candole) 추출물은 전립선 평활근을 이완시키는 것을 특징으로 하는 전립선 비대증 또는 전립선 비대에 의한 배뇨장애의 예방 또는 치료용 약학 조성물.
According to claim 1,
The mackerel ( Cirsium japonicum De Candole ) Extract is a pharmaceutical composition for the prevention or treatment of dysuria due to benign prostatic hyperplasia or prostatic hyperplasia, characterized in that to relax the prostatic smooth muscle.
상기 전립선 평활근 이완은 칼륨 채널(potassium channel)의 활성화에 의한 것을 특징으로 하는 전립선 비대증 또는 전립선 비대에 의한 배뇨장애의 예방 또는 치료용 약학 조성물.
According to claim 4,
The prostatic smooth muscle relaxation is a pharmaceutical composition for preventing or treating urination disorder caused by benign prostatic hyperplasia or prostatic hyperplasia, characterized in that by the activation of the potassium channel (potassium channel).
A dysuria improving agent comprising the pharmaceutical composition of any one of claims 1, 2, 4 and 5 as an active ingredient.
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