KR101399895B1 - A pharmaceutical comprising the extract of Acorus gramineus Soland for treating or preventing erectile dysfunction - Google Patents
A pharmaceutical comprising the extract of Acorus gramineus Soland for treating or preventing erectile dysfunction Download PDFInfo
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- KR101399895B1 KR101399895B1 KR1020110137926A KR20110137926A KR101399895B1 KR 101399895 B1 KR101399895 B1 KR 101399895B1 KR 1020110137926 A KR1020110137926 A KR 1020110137926A KR 20110137926 A KR20110137926 A KR 20110137926A KR 101399895 B1 KR101399895 B1 KR 101399895B1
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- KR
- South Korea
- Prior art keywords
- extract
- smooth muscle
- erectile dysfunction
- seokchangpo
- cgmp
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- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
Abstract
본 발명은 발기부전 질환의 예방과 치료를 위한 약학 조성물에 관한 것으로서, NO-cGMP경로를 통한 음경해면체 평활근 이완 효과 및 K+ 통로 개방에 따른 과분극을 통한 음경해면체 평활근 이완 효과를 보유하고 있는 약학 조성물에 관한 것이다.
본 발명은 발기부전 질환의 예방과 치료를 위한 약학 조성물에 관한 것으로, 석창포 추출물을 유효성분으로 함유하는 조성물에 관한 것이다.The present invention relates to a pharmaceutical composition for prevention and treatment of erectile dysfunction, which comprises a relaxation effect of the penile cavernosal smooth muscle via the NO-cGMP pathway and a pharmaceutical composition having relaxation effect of the penile cavernosal smooth muscle through hyperpolarization according to the opening of the K + channel .
The present invention relates to a pharmaceutical composition for prevention and treatment of erectile dysfunction, and relates to a composition containing an extract of Seokchangpo as an active ingredient.
Description
본 발명은 발기부전 질환의 예방과 치료를 위한 약학 조성물에 관한 것으로서, NO-cGMP경로를 통한 음경해면체 평활근 이완 효과 및 K+ 통로 개방에 따른 과분극을 통한 음경해면체 평활근 이완 효과를 보유하고 있는 약학 조성물에 관한 것이다.The present invention relates to a pharmaceutical composition for prevention and treatment of erectile dysfunction, which comprises a relaxation effect of the penile cavernosal smooth muscle via the NO-cGMP pathway and a pharmaceutical composition having relaxation effect of the penile cavernosal smooth muscle through hyperpolarization according to the opening of the K + channel .
본 발명은 발기부전 질환의 예방과 치료를 위한 약학 조성물에 관한 것으로, 석창포 추출물을 유효성분으로 함유하는 조성물에 관한 것이다.
The present invention relates to a pharmaceutical composition for prevention and treatment of erectile dysfunction, and relates to a composition containing an extract of Seokchangpo as an active ingredient.
일반적으로 발기부전(Eerectile Dysfunction, ED)은 성행위를 성공적으로 수행할 수 있도록 충분히 발기가 되지 못하거나 또는 충분한 시간 동안 발기 상태를 유지하지 못하는 증상을 의미한다. In general, Eerectile Dysfunction (ED) refers to a condition in which an erection is not sufficient to successfully perform sexual activity, or an erectile dysfunction can not be sustained for a sufficient period of time.
여기에서, 발기에 결정적인 역할을 하는 것은 음경해면체의 평활근으로서, 평활근이 이완되어야만 혈류량이 증가되거나 유지되어 발기력이 작용될 수 있기 때문이다. Here, it is the smooth muscle of the cavernous surface which plays a decisive role in the erection, since the blood flow is increased or maintained only when the smooth muscle is relaxed, so that the erectile force can be applied.
구체적으로 보면, 발기의 정도는 음경동맥과 음경해면체의 평활근에 작용하는 이완성 물질들과 수축성 물질들의 조합에 의해 발생되는 평활근의 긴장도에 따라 결정되는데, 혈관 이완인자(endotherium-derived relaxing factor; EDRF)로는 nitric oxide (NO), acetylcholine, prostaglandin E1, bradykinin 등이 있다.Specifically, the degree of erection is determined by the degree of relaxation of the smooth muscle caused by the combination of the relaxant materials acting on the smooth muscle of the penile artery and the cavernosal body and the shrinkable material. The endotherium-derived relaxing factor (EDRF) Nitric oxide (NO), acetylcholine, prostaglandin E1, and bradykinin.
또한 혈관 수축인자 (endotherium-derived constricting factor; EDCF)로는 norepinephrine, EDCF, endothelin, angiotensin Ⅱ 등이 있다.
The endotherium-derived constricting factor (EDCF) includes norepinephrine, EDCF, endothelin, and angiotensin II.
최근의 연구에 의하면 일산화질소(Nitric Oxide, NO)가 강력한 혈관 이완인자(EDRF)로 밝혀짐에 따라, 음경 해면체 평활근 이완에 대한 일산화질소의 역할에 대한 연구가 더욱 활발히 진행되고 있다.Recent studies have shown that Nitric Oxide (NO) is a powerful vasodilator (EDRF), and the role of nitric oxide in the relaxation of the corpus cavernosal smooth muscle is becoming more active.
구체적으로 보면, 성적 충동이 신경계를 통해 전달되면 혈관 내피세포(Endothelial cell)에서는 일산화질소 합성효소(NO Synthase, NOS)가 L-아르기닌(L-arginine)을 기질로 해서 일산화질소를 생성하게 된다.Specifically, when the sexual impulse is transmitted through the nervous system, NO synthase (NO synthase, NOS) produces NO in the endothelial cell using L-arginine as a substrate.
이 내피세포 유래 일산화질소는 가용성 구아닐산 고리화효소(soluble guanylate cyclase)를 활성화시킴으로써 평활근 세포내에서 GTP(guanosine 5'-triphosphate)를 cGMP(3’,5’- cyclic guanosine monophosphate)로 전환시켜 cGMP의 농도를 증가시키게 된다.This endothelium-derived nitric oxide converts soluble guanylate cyclase into smooth muscle cells to convert GTP (guanosine 5'-triphosphate) into cGMP (3 ', 5'-cyclic guanosine monophosphate) Thereby increasing the concentration.
이때 생성된 cGMP는 cGMP-특이 단백질 효소인 protein kinase G(PKG)를 자극하여 평활근 세포내 Ca2 + 유입을 억제하고, 따라서 Ca2 +의 수축적인 요소에 대한 감수성이 감소되어 평활근이 이완되는 것이다.(NO-cGMP Mechanism of Penile Erectiion) The generated cGMP is that it stimulates the protein kinase G (PKG) of cGMP- specific protein enzyme inhibiting smooth muscle intracellular Ca + 2 influx and thus the relaxation of smooth muscle sensitivity to shrinkage factor of Ca 2 + is reduced (NO-cGMP Mechanism of Penile Erection)
한편 NO-cGMP경로 외에도 음경해면체 평활근의 수축과 이완에 K+ 통로도 중요한 역할을 한다.In addition to the NO-cGMP pathway, K + channels play an important role in the contraction and relaxation of the smooth muscle of the corpus cavernosum.
즉 혈관 이완인자의 작용으로 K+통로가 활성화되어 개방되면, 세포내에 높은 농도로 존재해 있던 K+이 세포 밖으로 빠져나감으로써 세포 안팎의 분극이 심해져 세포의 과분극이 일어나는데, 이런 반응은 세포질 내로 Ca2 +이 유입되는 것을 억제함으로써, 평활근이 이완되는 것이다.That is, if K + channel is active opening by the action of vascular relaxing factor, as the exit is K + were in existence in high concentration in the cell out of the cell ileonaneunde of the polarization of the cell and out of simhaejyeo cell hyperpolarization, this reaction is Ca into the cytoplasm 2 + is prevented from flowing, the smooth muscle is relaxed.
여기에서, 음경해면체 평활근의 세포들에는 최소한 4종류의 K+ 통로 아형들이 존재한다: ① calcium-sensitive K+channel, ② metabolically regulated K+ channel, ③ fast transient A current ④ delayed rectifier. Here, there are at least four K + channel subtypes in the cells of the corpus cavernosal smooth muscle: ① calcium-sensitive K + channel, ② metabolically regulated K + channel, ③ fast transient A current, ④ delayed rectifier.
이들 K+ 통로들 중에서 칼슘 민감성 통로 및 KATP 통로가 가장 중요한데, 이들 통로들이 개방되면 세포로부터 K+의 유출이 일어나서 세포 내의 양전하가 소실되며, 이 효과로 과분극이 일어난다.
Among these K + channels, the calcium-sensitive channel and the K ATP channel are most important. When these channels are opened, K + outflows from the cell, and positive charge in the cell is lost, resulting in hyperpolarization.
한편 상기 서술한 바와 같이 음경 발기의 생리현상이 밝혀지고 해면체 평활근에 대한 다양한 약재들의 약리작용과 기전이 연구됨에 따라 평활근에 이완작용이 있는 약재들을 발기부전 치료에 이용해 보고자 하는 노력이 활발히 진행되고 있다.As described above, since the physiological phenomenon of penile erection is revealed and the pharmacological action and mechanism of the various pharmacological agents against the cavernosal smooth muscle are studied, efforts have been actively made to use the pharmacological agents having relaxation action in the smooth muscle for the erectile dysfunction treatment .
현재 전 세계적으로 시판되고 있는 발기부전 치료제로서, 구연산염제제인 화이자사의 ‘비아그라’, 화학적으로 합성된 단일물질 바데나필(Vardenafil), 타다라필(Tadalafil)등은 cGMP와 경쟁적 반응 물질로 작용하는 합성 유도체로서, PDE-5(phosphodiesterase-5)가 cGMP와 반응하는 단일경로만을 차단하여 음경해면체 내의 cGMP 농도를 증가시킴으로서 혈관 평활근의 이완 작용을 개선시킨다.Viagra, a chemically synthesized substance, Vardenafil, and Tadalafil, a citrate drug product, is a synthetic derivative that acts as a competitive reaction material with cGMP, as a commercially available drug for erectile dysfunction, PDE-5 (phosphodiesterase-5) blocks cGMP-mediated single pathway and improves vascular smooth muscle relaxation by increasing cGMP concentration in the corpus cavernosum.
그러나 이러한 치료제들은 효능이 한시적이고, 두통, 안면홍조, 소화불량, 심부전 등의 부작용이 보고되고 있다.However, these drugs have a temporary effect, and side effects such as headache, facial flushing, indigestion and heart failure have been reported.
따라서 일회성 및 강제성 발기보다 자연적인 발기 능력을 유지시켜주고, 부작용이 없는 약제의 필요성이 절실하다 하겠다.
Therefore, there is a need for a drug that maintains natural erectile ability rather than one - time and compulsive erection, and has no side effects.
한편 오랜 기간 동안 발기부전과 심장 건강 사이의 연관성에 대해 연구되어 왔는데, 현재까지는 분명한 증거가 없는 상황이다.On the other hand, the relationship between impotence and cardiac health has been studied over a long period of time, and there is no clear evidence to date.
이는 음경에 혈액을 공급하는 동맥이 심장에 혈액을 공급하는 보다 큰 동맥보다 일찍 막힐 수 있어 발기부전이 관상동맥질환의 조기 증후일 수 있다는 것에 근거한다.
This is based on the fact that the arteries supplying blood to the penis can be blocked earlier than the larger arteries supplying blood to the heart, so that erectile dysfunction can be an early symptom of coronary artery disease.
한편 우리나라에서는 예로부터 발기부전 치료에 대한 민간요법으로 인삼, 홍삼, 녹용, 구기자, 산수유, 복분자, 토사자 및 오미자 등 다양한 약제가 이용되어 왔으나 그 밖에 다른 약용식물에 대한 발기부전 연구는 부족한 실정이다.In Korea, a variety of medicines such as ginseng, red ginseng, antler, gugija, corn oil, bokbunja, tortoise, and omija have been used as folk remedies for erectile dysfunction in Korea. However, studies on erectile dysfunction have been lacking in other medicinal plants.
본 발명은 발기부전을 예방 및 치료하는 조성물로서, 석창포 추출물을 유효성분으로 하고 있는바, 이하 석창포에 관련하여 살펴본다.The present invention relates to a composition for preventing and treating erectile dysfunction, which comprises an extract of Seokchangpo as an active ingredient.
석창포(石菖蒲, Acorus gramineus Soland)는 천남성과 다년생 초본 식물인 석창포의 뿌리줄기(근경, 根莖)이다. Seok Changpo (Acorns, Acorns gramineus Soland) is the rootstock (rootstock, rootstock) of Seonchungpo and perennial herbaceous plant.
한의학적으로는, 성질은 온(溫)하고 맛은 매우며(辛), 심경(心經)과 위경(胃經)에 귀경한다고 하며, 풍한습사(風寒濕邪)의 비증(痺證)을 주치하고, 건위거풍(健胃祛風) 및 활혈지통(活血止痛) 즉 기의 순환을 조절하고 혈을 운행시키며 풍을 풀어주고 습을 제거하는 효능이 있다고 알려져 있다.In oriental medicine, it is said that the nature is warm, the taste is very high, and it is said to be in the heart and the stomach (胃 经), and it takes care of the nihilism of 风 寒濕 邪It is known that it has the effect of controlling the circulation of the blood circulation, circulating the blood, releasing the wind, and removing the wetness.
약리학적으로는, β-asarone, caryophyllene, α-humulene, sekishone 등 성분을 함유하고 있으며, 진정작용이 있으며 소화액의 분비를 촉진하고 위장의 이상 발효를 억제하며 동시에 장관 평활근의 경련을 완화하는 작용이 있다고 알려져 있다.
Pharmacologically, it contains ingredients such as β-asarone, caryophyllene, α-humulene, and sekishone. It has sedative action, promotes secretion of digestive juices, inhibits abnormal fermentation of the stomach and at the same time relaxes the seizures of the intestinal smooth muscle .
한편 석창포와 관련한 종래기술에 대해 살펴보면, 먼저, 한국등록특허 제0522176호에는 47여개의 천연물을 포함하는 성기능 조성물이 개시되어 있는데, 석창포가 조성물 성분에 포함되어서 기재되어 있다. Meanwhile, Korean Patent No. 0522176 discloses a sexual function composition containing about 47 natural products, which is disclosed in a composition component of Seok Changpo.
또한 한국등록특허 제0672950호에는 허혈성 심질환 예방 또는 치료를 위한 석창포 추출물에 대하여 기재되어 있다.Korean Patent No. 0672950 discloses an extract of Seokchangpo for the prevention or treatment of ischemic heart disease.
정리하여 보면, 발기부전과 관련해서는 47여종의 천연물 중 하나로서 석창포를 사용하고 있으며, 또한 심질환 예방 및 치료에 초점을 두어 석창포를 사용했음을 알 수 있다.
As a summary, we can see that Seok Changpo is used as one of 47 kinds of natural products in relation to erectile dysfunction, and the use of Seok Changpo is focused on prevention and treatment of heart disease.
본 발명의 목적은, 일회성 처치의 개념이 아닐 뿐더러 부작용을 가져오지 않으면서 지속적으로 복용함으로써, 발기부전의 근본원인으로서의 혈관 상태를 개선하여 발기부전 질환을 예방, 개선 및 치료하기 위한 조성물을 제공함에 있다.It is an object of the present invention to provide a composition for preventing, ameliorating and treating erectile dysfunction by improving vascular condition as a root cause of erectile dysfunction by not taking the concept of a one-time treatment but taking it continuously without causing side effects have.
본 발명의 목적은, NO-cGMP경로 및 K+ 통로 개방에 따른 음경해면체 평활근 이완 효과에 주목하여, 화이트 래빗의 음경 해면체 이완효과를 측정함으로써, 발기부전 질환을 예방, 개선 및 치료하는 효과가 현저한 조성물을 제공함에 있다. An object of the present invention, NO-cGMP route and K + to pay attention to the corpus cavernosum smooth muscle relaxation effects of the passage opening, by measuring the corpus cavernosum relaxation effect of the White Rabbit, erectile dysfunction prevention, an effect of improving and treating significant Composition.
또한 백서의 음경 해면체 발기 효과를 측정함으로써, 발기부전 질환을 예방, 개선 및 치료하는 효과가 현저한 조성물을 제공함에 있다.
The present invention also provides a composition which is remarkably effective in preventing, ameliorating, and treating erectile dysfunction by measuring erectile efficacy of penile corpus cavernosum.
본 발명은, 석창포 추출물을 유효성분으로 함유하는 발기부전 예방 및 치료를 약학 조성물을 제공함으로써, 기술적 과제를 해결하고자 한다.The present invention aims to solve the technical problem by providing a pharmaceutical composition for preventing and treating erectile dysfunction, which comprises extract of Seokchangpo as an active ingredient.
또한 본 발명은, 석창포의 추출용 용매로서, 바람직하게 에탄올(전체 시료 중량의 5배 내지 10배의 부피)를 사용하는 것을 특징으로 하는 발기부전 예방 및 치료를 약학 조성물을 제공함으로써, 기술적 과제를 해결하고자 한다.
Further, the present invention provides a pharmaceutical composition for preventing and treating erectile dysfunction, characterized in that ethanol (
본 발명은, 석창포 추출물을 유효성분을 포함하고 약제학적으로 허용되는 담체, 부형제 또는 희석제 등을 추가하여 약제학적 단위 투여형으로 제형화 된 발기부전 질환의 예방 및 치료제를 제공함으로써, 기술적 과제를 해결하고자 한다.The present invention solves the technical problem by providing an agent for preventing and treating erectile dysfunction which is formulated into a pharmaceutical unit dosage form by adding an extract of Seokchangpo as an effective ingredient and adding a pharmaceutically acceptable carrier, excipient or diluent I want to.
여기에서, 담체, 부형제, 희석제로는 토즈, 덱스트로즈, 수크로스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로즈, 메틸 셀룰로즈, 미정질 셀룰로스, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 프로필히드록시벤조에이트, 탈크, 마그네슘 스테아레이트 및 광물유를 들 수 있다.Examples of the carrier, excipient and diluent include tosse, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, Vaginal cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil.
또한 상기 약제학적 투여 형태는 약학적 허용 가능한 염의 형태로도 사용될 수 있고, 또한 단독으로 또는 타 약학적 활성 화합물과 결합뿐만 아니라 적당한 집합으로 사용될 수 있다.
The pharmaceutical dosage forms may also be used in the form of pharmaceutically acceptable salts, and may be used alone or in combination with other pharmaceutically active compounds as well as in a suitable set.
또한 상기 석창포 추출물을 제제화 할 경우에는 통상적으로 사용하는 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면 활성제 등의 희석제 또는 부형제를 사용하여 조제될 수 있다.
In addition, when the extract of Seokchangpo is prepared, it may be prepared using diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, surfactants and the like which are usually used.
또한 상기 약제학적 투여 형태는 각각 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁액, 에멀젼, 시럽, 에어로졸 등의 경구형 제형, 외용제, 좌제, 및 멸균 주사용액의 형태로 제형화하여 사용될 수 있다.In addition, each of the above pharmaceutical dosage forms may be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols or the like, oral preparations, suppositories, .
상기 경구 투여를 위한 고형 제제에는 상기 추출물에 적어도 하나 이상의 부형제 예를 들면, 전분은 칼슘 카보네이트(calcium carbonate), 수크로스(sucrose) 또는 락토오스(lactose), 젤라틴 등을 섞어 조제될 수 있다. 또한 단순한 부형제 이외에 마그네슘 스테아레이트, 탈크 같은 윤활제들도 사용될 수 있다.In the solid preparation for oral administration, at least one excipient such as starch may be prepared by mixing calcium carbonate, sucrose, lactose, gelatin or the like in the extract. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used.
상기 비경구 투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조 제제, 좌제가 포함될 수 있다. The preparation for parenteral administration may include a sterilized aqueous solution, a non-aqueous solvent, a suspension, an emulsion, a freeze-dried preparation, and a suppository.
상기 비 수성용제, 현탁제로는 프로필렌글리콜(propylene glycol), 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸 올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다.Examples of the non-aqueous solvent and the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like.
좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈(tween) 61, 카카오지, 라우린지, 글리세로제라틴 등이 사용될 수 있다.
Examples of the suppository base include witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin and the like.
본 발명의 추출물의 바람직한 투여량은 환자의 상태 및 체중, 질병의 정도, 연령, 성별, 약물형태, 투여경로 및 기간에 따라 다르지만, 당업자에 의해 적절하게 선택될 수 있다.The preferred dosage of the extract of the present invention varies depending on the condition and the weight of the patient, the degree of disease, age, sex, drug form, route of administration and period of time, but can be appropriately selected by those skilled in the art.
그러나 바람직한 효과를 위해서, 본 발명의 추출물은 0.001 내지 300 mg/kg으로 투여하는 것이 좋고, 투여는 하루에 한번 투여할 수도 있고, 수회 나누어 투여할 수도 있다.However, for the desired effect, the extract of the present invention is preferably administered at 0.001 to 300 mg / kg, and the administration may be carried out once a day or divided into several times.
상기 투여량은 어떠한 면으로든 본 발명의 범위를 한정하는 것은 아니다.
The dose is not intended to limit the scope of the invention in any way.
본 발명의 추출물은 쥐, 생쥐, 가축, 인간 등의 포유동물에 다양한 경로로 투여될 수 있다. 투여의 모든 방식은 예상될 수 있는데, 예를 들면, 경구, 직장 또는 정맥, 근육, 피하주사에 의해 투여될 수 있다.
The extract of the present invention can be administered to mammals such as rats, mice, livestock, humans and the like in various routes. All modes of administration may be expected, for example, by oral, rectal or intravenous, muscular, subcutaneous injection.
본 발명은 석창포 추출물에 식품 보조 첨가제를 추가하여 발기부전 질환 예방 및 치료용 건강기능식품 조성물을 제공함으로써 기술적 과제를 해결하고자 한다.The present invention aims to solve the technical problem by providing a health functional food composition for preventing and treating erectile dysfunction by adding a food auxiliary additive to the extract of Seokchangpo.
상기 추출물을 첨가할 수 있는 식품으로는, 예를 들어, 각종 식품류, 음료, 껌, 차, 비타민 복합제, 건강 기능성 식품류 등이 있다.Examples of foods to which the extract can be added include various foods, beverages, gums, tea, vitamin complexes, and health functional foods.
이때, 식품 또는 음료 중의 상기 추출물의 양은 전체 식품 중량의 0.01 내지 20 중량% 가할 수 있으며, 건강 음료 조성물은 100 ml를 기준으로 0.02 내지 5 g, 바람직하게는 0.3 내지 1 g의 비율로 가할 수 있다.
At this time, the amount of the extract in the food or drink may be 0.01 to 20% by weight of the total food, and the health beverage composition may be added in a proportion of 0.02 to 5 g, preferably 0.3 to 1 g based on 100 ml .
본 발명의 건강 기능성 음료 조성물은 상기 추출물을 함유하는 외의 다른 성분에는 특별한 제한이 없으며 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다.The health functional beverage composition of the present invention is not particularly limited to the components other than those containing the above extract, and may contain various flavors or natural carbohydrates as additional components such as ordinary beverages.
상술한 천연 탄수화물의 예는 모노사카라이드, 예를 들어, 포도당, 과당; 디사카라이드, 예를 들어 말토스, 슈크로스 등 및 폴리사카라이드, 예를 들어 덱스트린, 시클로덱스트린 등과 같은 통상적인 당, 및 자일리톨, 소르비톨, 에리트리톨 등의 당알코올이다. 상술한 것 이외에 향미제로써 천연 향미제(타우마틴, 스테비아 추출물(예를 들어 레바우디오시드 A, 글리시르히진 등) 및 합성 향미제(사카린, 아스파르탐 등)를 유리하게 사용할 수 있다.Examples of the above-mentioned natural carbohydrates are monosaccharides such as glucose, fructose; Disaccharides such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and sugar alcohols such as xylitol, sorbitol and erythritol. In addition to the above, natural flavoring agents (tau martin, stevia extracts (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavorings.
상기 천연 탄수화물의 비율은 본 발명의 조성물 100 ml당 일반적으로 약 1 내지 20 g, 바람직하게는 약 5 내지 12 g이다.
The ratio 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.
상기 외에 본 발명의 추출물은 여러 가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 중진제(치즈, 초콜릿 등), 펙트산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 함유할 수 있다.In addition to the above, the extract of the present invention can be used as a nutritional supplement, a vitamin, a mineral (electrolyte), a flavor such as a synthetic flavor and a natural flavor, a coloring agent and an aggravating agent (cheese, chocolate etc.), a pectic acid and its salt, Colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like.
그 밖에 본 발명의 추출물들은 천연 과일 주스 및 과일 주스 음료 및 야채 음료의 제조를 위한 과육을 함유할 수 있다.In addition, the extracts of the present invention may contain flesh for the production of natural fruit juices and fruit juice beverages and vegetable beverages.
이러한 성분은 독립적으로 또는 조합하여 사용할 수 있다. 이러한 첨가제의 비율은 그렇게 중요하진 않지만 본 발명의 추출물 100 중량부 당 0 내지 약 20 중량부의 범위에서 선택되는 것이 일반적이다.
These components may be used independently or in combination. The proportion of such additives is not so critical, but is generally selected in the range of 0 to about 20 parts by weight per 100 parts by weight of the extract of the present invention.
본 발명인 석창포 추출물을 유효성분으로 함유하는 발기부전 질환의 예방과 치료를 위한 약학 조성물은, 부작용을 가져오지 않으면서 지속적으로 복용함으로써, 발기부전의 근본원인으로서의 혈관 상태를 개선하여 발기부전 질환을 예방, 개선 및 치료하는 현저한 효과가 있다.The pharmaceutical composition for prevention and treatment of erectile dysfunction diseases containing the extract of Seokchangpo as an active ingredient of the present invention can be used continuously without taking side effects to improve the vascular condition as a root cause of erectile dysfunction and prevent erectile dysfunction , ≪ / RTI > improvement and treatment.
본 발명인 석창포 추출물을 유효성분으로 함유하는 발기부전 질환의 예방과 치료를 위한 약학 조성물은, 음경 해면체 평활근의 이완 작용을 수행함으로써 발기부전 질환을 예방, 개선 및 치료하는 현저한 효과가 있다.The pharmaceutical composition for prevention and treatment of erectile dysfunction disease containing the extract of Seokchonpo extract of the present invention as an active ingredient has a remarkable effect of preventing, ameliorating and treating erectile dysfunction by performing relaxation action of the smooth muscle of the corpus cavernosum.
본 발명인 석창포 추출물을 유효성분으로 함유하는 발기부전 질환의 예방과 치료를 위한 약학 조성물은, NO-cGMP경로를 통한 음경해면체 평활근 이완 효과 및 K+ 통로 개방에 따른 과분극을 통한 음경해면체 평활근 이완 효과를 보유하고 있다.The pharmaceutical composition for prevention and treatment of erectile dysfunction disease containing the extract of Seokchangpo extract as an active ingredient of the present invention is useful for relaxation of the smooth muscle of the corpus cavernosum through the NO-cGMP pathway and relaxation of the smooth muscle of the penile corpus cavernosum through hyperpolarization according to the opening of the K + .
본 발명인 석창포 추출물을 유효성분으로 함유하는 발기부전 질환의 예방과 치료를 위한 약학 조성물은, 음경 해면체 내압을 증가함으로써 발기기능을 증진하는, 발기부전 질환을 예방, 개선 및 치료하는 현저한 효과가 있다.
The pharmaceutical composition for prevention and treatment of erectile dysfunction diseases containing the extract of Seokchangpo extract of the present invention as an active ingredient has a remarkable effect of preventing erectile dysfunction which improves erectile function by increasing internal pressure of the corpus cavernosum and treating and treating it.
도 1은 실험예 1에 따른 음경해면체 평활근의 이완효과에 대한 실험결과를 나타내는 도면이다.
도 2는 실험예 2에 따른 NO-cGMP 활성 효과에 대한 실험결과를 나타내는 도면이다.
도 3은 실험예 3에 따른 cGMP 생성 효과에 대한 실험결과를 나타내는 도면이다.
도 4는 실험예 4에 따른 K+ 통로 활성 효과에 대한 실험결과를 나타내는 도면이다.
도 5 내지 도 7은 실험예 5에 따른 음경해면체 내부압력에 대한 ICP, ICP/MAP 및 AUC 측정 결과를 나타내는 각각 나타내는 도면이다.BRIEF DESCRIPTION OF THE DRAWINGS Fig. 1 is a graph showing experimental results on relaxation effect of smooth muscle of cauliflower according to Experimental Example 1. Fig.
2 is a graph showing the results of experiments on NO-cGMP activity according to Experimental Example 2. FIG.
3 is a graph showing experimental results on cGMP generation effect according to Experimental Example 3. FIG.
4 is a graph showing experimental results on the K + channel activity effect according to Experimental Example 4. FIG.
5 to 7 are graphs showing ICP, ICP / MAP, and AUC measurement results for the internal pressure of the cavernosal corpuscle according to Experimental Example 5, respectively.
본 명세서 및 청구범위에 사용된 용어나 단어는 통상적이거나 사전적인 의미로 한정해서 해석되어서는 안 되며, 발명자는 그 자신의 발명을 가장 최선의 방법으로 설명하기 위해 용어의 개념을 적절하게 정의할 수 있다는 원칙에 입각하여 본 발명의 기술적 사상에 부합하는 의미와 개념으로 해석되어야만 한다.The terms and words used in the present specification and claims should not be construed as limited to ordinary or dictionary terms and the inventor may properly define the concept of the term in order to best describe its invention It should be construed as meaning and concept consistent with the technical idea of the present invention.
따라서 본 명세서에 기재된 실시예와 도면에 도시된 구성은 본 발명의 가장 바람직한 일 실시예에 불과할 뿐이고 본 발명의 기술적 사상을 모두 대변하는 것은 아니므로, 본 출원시점에 있어서 이들을 대체할 수 있는 다양한 균등물과 변형예들이 있을 수 있음을 이해하여야 한다.Therefore, the embodiments described in the present specification and the configurations shown in the drawings are merely the most preferred embodiments of the present invention and are not intended to represent all of the technical ideas of the present invention. Therefore, various equivalents It should be understood that water and variations may be present.
이하 첨부된 도면을 참조하여 본 발명의 바람직한 실시예를 상세히 설명하기로 한다.
Hereinafter, preferred embodiments of the present invention will be described in detail with reference to the accompanying drawings.
실시예Example
1. One.
석창포Seokchangpo
추출물의 제조 Preparation of extract
석창포 400g을 전체 시료 중량의 5배 내지 10배, 바람직하게는 에탄올 2 L에 시료가 충분히 추출될 수 있도록 초음파분해기 (100 W, 40 kHz)를 이용하여 상온에서 일주일 동안 담가두었다.400 g of Seokchangpo were immersed for one week at room temperature using an ultrasonic digester (100 W, 40 kHz) so that the sample could be extracted sufficiently to 5 to 10 times the weight of the total sample, preferably to 2 L of ethanol.
일주일 동안 추출된 석창포 추출물을 1차적으로 무명베를 이용하여 잡질과 찌꺼기를 걸러주고, 2차적으로 분리된 맑은 전탕액만을 취하여 Watman NO.3 여과기를 사용하여 진공압을 걸어 여과하였다. The extracts of Seokchonpo extracted for one week were first filtered through mung bean mud to remove moss and debris, and then filtered using a Watman NO.3 filter by vacuum filtration.
최종적으로 여과된 석창포 에탄올 추출물을 감압 농축기를 이용하여 농축시킨 후 동결건조하여 만들어진 조성물 (41.09 g)을 분말상태로 만든 후 이를 실험에 사용하였다.
Finally, the filtered ethanol extract of Seokchangpo was concentrated by using a vacuum concentrator and then lyophilized to obtain a powdery composition (41.09 g).
참고예Reference example
1. 실험 준비 1. Experimental preparation
1-1. 실험동물1-1. Experimental animal
샘타코(Samtako, Korea)로부터 약 2 kg 내외의 웅성 뉴질랜드 흰 토끼(New Zealand white rabbit)을 분양받아 2주 동안 실험실 환경에 적응시켰다. New Zealand white rabbits (about 2 kg) were distributed from Samtako, Korea to the laboratory environment for 2 weeks.
실험동물은 항온항습 장치가 부착된 사육실 (온도 22±1℃, 습도 55±10%, 12시간 dark/light)에서 고형사료와 물을 충분히 공급받았다. The experimental animals were fed with solid feed and water at a temperature of 22 ± 1 ℃, humidity 55 ± 10%, dark / light for 12 hours.
모든 동물 실험은 미국 NIH의 동물실험원칙 (NIH guide for the care and use of laboratory animals, USA)과 원광대학교 실험동물 윤리위원회 승인(WKU09-102)을 받고 시행되었다.
All animal studies were conducted with the National Institutes of Health (NIH) guide for the care and use of laboratory animals (USA) and the Wonkwang University Laboratory Animal Ethics Committee (WKU09-102).
1-2. 시약 준비1-2. Reagent preparation
이 연구에 사용된 acetylcholine (ACh), phenylephrine HCl (PE), NG-nitroarginine methyl ester (L-NAME), 1 H-[1,2,4]-oxadiazolo-[4,3-α]-quinoxalin-1-one (ODQ), indomethacin, glibenclamide, tetraethylammonium (TEA), atropine, (±)-propranolol HCl, 3-isobutyl-1-methylxanthine (IBMX), trichloroacetic acid (TCA) 등은 Sigma Chemical Co.(St. Louis, MO)으로부터 구입하여 사용하였다.
The acetylcholine (ACh), phenylephrine HCl (PE), N G -nitroarginine methyl ester (L-NAME), 1 H- [1,2,4] -oxadiazolo- [4,3-a] -quinoxalin 1-one (ODQ), indomethacin, glibenclamide, tetraethylammonium (TEA), atropine, (±) -propranolol HCl, 3-isobutyl-1-methylxanthine (IBMX), trichloroacetic acid Louis, MO).
1-3. 음경해면체 평활근의 분리1-3. Isolation of smooth muscle of cavernous cavernosum
건강한 토끼의 이각 정맥을 통해 케타민(50 mg/kg i.v.)으로 마취하고 심장출혈로 희생시킨 후 음경조직을 치골 아래로 분지하여 들어가는 부위까지 박리, 적출하였다. The animals were anesthetized with ketamine (50 mg / kg i.v.) through a diaphragmatic vein of a healthy rabbit and sacrificed by cardiac hemorrhage. Then, the penis tissue was peeled and removed until it was branched into the lower part of the pubic bone.
음경조직을 4°C Krebs 완충액 (NaCl 136.9 mM, KCl 5.4 mM, MgCl26H2O 1.0 mM, CaCl2 2.0 mM, NaHCO3 23.8 mM, Glucose 5.5 mM)에 넣고 음경해면체 평활근 내피세포가 손상 받지 않도록 조심히 음경해면체 백막을 제거한 후, 2×2×6 mm 크기의 음경해면체 평활근 조직절편 (corpus cavernosal tissue strip)을 만들었다.
Penile tissues were washed with 4 ° C Krebs buffer (NaCl 136.9 mM, KCl 5.4 mM, MgCl 2 6H 2 O 1.0 mM, CaCl 2 2.0 mM, NaHCO 3 23.8 mM, and glucose 5.5 mM), and the corneal cavernosal tissue strips (2 × 2 × 6 mm) were prepared by carefully removing the cavernosal surface of the penis to prevent damage to the endothelial cells of the corpus cavernosal smooth muscle.
1-4. 이완 효과 측정1-4. Measurement of relaxation effect
음경해면체 평활근 조직절편을 95% O2- 5% CO2 기체로 포화시킨 37°C, pH 7.4의 Krebs 완충용액에서 고정시킨 후, isometric tension을 force-displacement transducer (Grass FT 03, Grass Instrument, MA)가 장착된 생리기록계 (Grass Model 7E, Grass Instrument, MA)를 이용하여 측정하였다. The isoflurane tissue sections were fixed in Krebs buffer at 37 ° C, saturated with 95% O 2 - 5% CO 2 gas. The isometric tension was measured using a force-displacement transducer (Grass FT 03, Grass Instrument, MA ) (Grass Model 7E, Grass Instrument, MA).
먼저 1 μM의 phenylephrine (PE)으로 수축시키고 5분 후, 1 μM의 acetylcholine (ACh)으로 이완반응을 시켜 음경해면체 평활근 내피세포의 안정성을 측정한 후 Krebs 완충용액으로 3회 세척하고 실험을 수행하였다. After 5 min of contraction with 1 μM of phenylephrine (PE), the stability of the endothelial cells of the penile cavernosal smooth muscle was measured by relaxation with 1 μM of acetylcholine (ACh), followed by washing three times with Krebs buffer .
각종 차단제들의 전 처리로 인한 석창포 에탄올 추출물이 음경해면체 평활근에 대한 이완효과의 변화측정은 먼저 약물을 20분간 전 처리하고 PE으로 수축시켰고 이어서 석창포 에탄올 추출물에 의한 이완반응을 관찰하였다.
In order to measure the relaxation effect of the ethanol extract of Seokchangpo on pretreatment of various blocking agents, the drug was pretreated for 20 minutes before shrinking with PE, followed by relaxation reaction with ethanol extract of Seokchangpo.
1-5. 1-5. cGMPcGMP 및 And cAMPcAMP 생성량 측정 Production amount measurement
음경해면체를 절개하여 해면체를 적출하고 절편으로 만들어 kreps용액과 95% O2와 5% CO2가 존재하는 bath에서 배양하고 5분간 PE과 IBMX을 전처리하고 5분간 약물을 처리한 후에 6%의 trichloroacetic acid (TCA)존재 하에서 균질화시킨 후 13,000 rpm에서 15분간 원심분리하여 얻은 상층액을 물이 포화된 diethylether를 이용하여 3회 추출하였다. 추출액을 Speed-vac 농축기로 농축하여 방사면역분석법으로 cGMP와 cAMP을 측정하였다.
The corpus cavernosum was excised and the corpuscle was excised and cultured in a kreps solution containing 95% O 2 and 5% CO 2 , pretreated with PE and IBMX for 5 minutes, treated with 5 minutes of drug and then treated with 6% trichloroacetic acid (TCA) and centrifuged at 13,000 rpm for 15 min. The supernatant was extracted three times with water saturated diethylether. The extract was concentrated with a Speed-vac concentrator and cGMP and cAMP were measured by radioimmunoassay.
1-6. 통계처리1-6. Statistical processing
실험 결과의 유의성 검증은 Sigma Plot 2010 프로그램을 이용하여 처리하였으며, 실험결과를 Students t-test 나 one-way ANOVA test를 통하여 p값이 0.05 이하인 경우 유의한 차이가 있는 것으로 판정하였다.
The significance of the test results was analyzed using the Sigma Plot 2010 program. The Student t-test or the one-way ANOVA test was used to determine the significance of the test results when the p-value was less than 0.05.
실험예Experimental Example
1. One.
석창포Seokchangpo
추출물의 음경 해면체 평활근 이완 효과 Relaxation effect of extracts on smooth muscle of corpus cavernosum
도 1은 실험예 1에 따른 음경해면체 평활근의 이완 효과에 대한 실험결과를 나타내는 도면이다.(Each value shows mean ± S.D.(n=4))1 is a graph showing experimental results on the relaxation effect of the smooth muscle of the penile cavernosa according to Experimental Example 1. (Each value shows mean SD (n = 4))
음경해면체 평활근을 1 μM PE으로 5분간 수축시킨 후 실시예 1에 따른 석창포 추출물(0.1 ug/ml∼0.3 mg/ml, EAG(Ethanol extract of Acorus gramineus Solan)로 표기함)을 농도 의존적으로 투여하여 음경해면체 평활근의 이완효과를 측정한 결과, 음경해면체 평활근은 농도 의존적으로 이완하였으며 0.3 mg/ml의 농도에서 96.48 ± 2.24% 이완효과를 관찰할 수 있었다.
The smooth muscle of the penile corpus cavernosum was shrunk with 1 μM PE for 5 minutes, and then the extract of Seokchangpo (0.1 ug / ml to 0.3 mg / ml, EAG (Ethanol extract of Acorus gramineus Solan) according to Example 1) As a result of measuring the relaxation effect of the smooth muscle of the corpus cavernosum, the smooth muscle of the corpus cavernosum relaxed in a concentration dependent manner, and a relaxation effect of 96.48 ± 2.24% was observed at a concentration of 0.3 mg / ml.
실험예2Experimental Example 2
. .
석창포Seokchangpo
추출물의 Extract
NONO
--
cGMPcGMP
활성 효과 Active effect
도 2는 실험예 2에 따른 NO-cGMP 활성 효과에 대한 실험결과를 나타내는 도면이다.(Each value shows mean ± S.D. (n=4). #p<0.05, *p<0.01, **P<0.001, vs. vehicle group.)
2 shows experimental results on the NO-cGMP activity effect according to Experimental Example 2. (Each value shows mean SD (n = 4). # P <0.05, * p <0.01, ** P <0.001 , etc. vehicle group.)
비특이적인 NO(산화질소) 억제제인 L-NAME 0.1 mM와 세포질 구아닐산 고리화효소(guanylate cyclase) 억제제인 ODQ 10 μM을 각각 20분동안 전 처리하고 1 μM PE으로 수축시킨 후 실시예 1에 따른 석창포 추출물을 농도 의존적으로 투여하여 음경해면체 이완 효과를 측정하였다.L-NAME 0.1 mM, a non-specific NO (nitric oxide) inhibitor, and 10 μM ODQ, a guanylate cyclase inhibitor, were each pretreated for 20 minutes and shrunk to 1 μM PE. The extracts were administered in a concentration-dependent manner to measure the relaxation effect of the corpus cavernosum.
도 2를 참조해보면, 석창포 추출물은 농도의존적으로 유의성 있게 NO-cGMP 경로를 활성화시키고 있으며 또한, NO 억제제 및 구아닐산 고리화 효소 억제제를 전처리한 경우에는 유의성 있게 NO-cGMP 경로가 억제되고 있음을 알 수 있다.
FIG. 2 shows that the extract of Seokchang extract significantly activates the NO-cGMP pathway in a concentration-dependent manner, and the NO-cGMP pathway is significantly inhibited when the NO inhibitor and the guanylate cyclase inhibitor are pretreated have.
실험예3Experimental Example 3
. .
석창포Seokchangpo
추출물의 Extract
cGMPcGMP
생성 효과 Generation effect
도 3은 실험예 3에 따른 cGMP 생성 효과에 대한 실험결과를 나타내는 도면이다.(Each value shows mean ± S.D. (n=5). *p<0.001, **P<0.001, vs. vehicle group; †p<0.01, vs. EAG (3 μg/ml) group.)
. Figure 3 is a diagram showing experimental results for cGMP generated effect according to the Experimental Example 3 (Each value shows mean ± SD (n = 5) * p <0.001, ** P <0.001, vs. vehicle group; † p <0.01, etc. EAG (3 μg / ml) group.)
실시예 1에 따른 석창포 추출물을 음경해면체 조직절편에 직접 투여한 후 cGMP와 cAMP의 생성량을 측정한 결과, 석창포 추출물을 투여하지 않은 군과 비교하여 석창포 추출물을 투여한 군이 농도 의존적으로 cGMP의 생성량을 증가시켰다.As a result of measuring the amount of cGMP and cAMP produced after direct administration of the extract of Seokchangpo extract according to Example 1 to the corpus cavernosum tissue section, the concentration of cGMP Respectively.
반면에 cAMP의 생성량은 석창포 에탄올 추출물을 투여에 의한 변화를 보이지 않았다.On the other hand, the amount of cAMP produced was not changed by the ethanol extract of Seokchangpo.
따라서 석창포 추출물은 음경해면체조직에서 농도의존적으로 유의성 있게 NO-cGMP 경로를 활성화시키고 있음을 알 수 있다.
Therefore, it can be shown that Seokchangpo extract activates the NO-cGMP pathway in a concentration-dependent manner in the corpus cavernosum tissue.
실험예4Experimental Example 4
. .
석창포Seokchangpo
추출물의 K The K of the extract
++
통로 활성 효과 Channel effect
도 4는 실험예 4에 따른 K+ 통로 활성 효과에 대한 실험결과를 나타내는 도면이다.(Each value shows mean ± S.D. (n=4). *p<0.01, **P<0.001, vs. vehicle group.)FIG. 4 is a graph showing experimental results on the K + channel activity effect according to Experimental Example 4. Each value shows mean SD (n = 4). * P <0.01, ** P <0.001, .)
비선택적 K+ 통로 억제제인 10 μM tetraethylammonium (TEA)과 ATP-감수성 K+ 통로 억제제인 10 μM glibenclamide를 각각 20분동안 전 처리하고 1 μM PE으로 5분동안 수축시킨 후 실시예 1에 따른 석창포 추출물에 의한 음경해면체 평활근의 이완효과를 측정하였다.10 μM tetraethylammonium (TEA), a non-selective K + channel inhibitor, and 10 μM glibenclamide, an ATP-sensitive K + channel inhibitor, were each pretreated for 20 min and shrunk with 1 μM PE for 5 min. The relaxation effect of the smooth muscle of cavernous cavernosum was measured.
도 4를 참조해보면, TEA 전 처리로 의하여 석창포 추출물에 의한 음경해면체 평활근의 이완 효과가 유의성 있게 억제되었으며, glibenclamide의 전 처리에 의하여서는 이완 효과가 유의성 있게 억제되지 않았음을 알 수 있다.
FIG. 4 shows that the relaxation effect of the smooth muscle of the penile corpus cavernosum was significantly inhibited by the TEA pretreatment, and the relaxation effect was not significantly inhibited by glibenclamide pretreatment.
실험예 1 내지 실험예 4를 총괄적으로 정리하여 보면, 석창포 추출물은 음경해면체 평활근을 농도의존적으로 이완시키는 효과를 보유하고 있다.(실험예 1)Experimental Examples 1 to 4 are summarized as follows. Experimental Example 1: The extract of Seokchonpo has the effect of relaxing the smooth muscle of the penile cavernosum in a concentration-dependent manner.
또한 산화질소 합성 억제제인 L-NAME 및 가용성 구아닐산 고리화효소 억제제인 ODQ를 전 처리한 후 측정한 결과, 석창포 추출물의 음경해면체 평활근에 대한 이완효과가 유의성 있게 억제되었다.(실험예 2) In addition, L-NAME, which is an inhibitor of nitric oxide synthesis, and ODQ, a soluble guanylate cyclase inhibitor, were measured after the pretreatment, and the relaxation effect on smooth muscle of corpus cavernosum was significantly inhibited by the extract of Seokchangpo. (Experimental Example 2)
또한 석창포 에탄올 추출물은 cGMP의 생성량을 농도 의존적으로 증가시키는 효과를 보유하고 있다.(실험예 3)In addition, the ethanol extract of Seokchangpo has an effect of increasing the production amount of cGMP in a concentration-dependent manner. (Experimental Example 3)
또한 K+ 통로에 대한 억제제로 비특이성 K+ 통로 차단제인 TEA와 KATP 통로 선택적인 차단제인 sulfonylurea계 약물 glibenclamide를 전 처리한 후 측정한 결과, TEA에 의하여 석창포 추출물의 이완 효과가 유의성 있게 억제되었다.(실험예 4)
In addition, the TEA and the K ATP non-specific K + channel blockers as inhibitors of the K + channel Pathway-selective blockers sulfonylurea drug glibenclamide was pretreated and the relaxation effect of Seokchonpo extract was significantly inhibited by TEA. (Experimental Example 4)
따라서 실시예 1에 따른 석창포 추출물에 의한 음경해면체 평활근의 이완효과는 NO-cGMP계를 경유하여 일어나는 것임을 알 수 있다.Therefore, it can be understood that the relaxation effect of the smooth muscle of the penile corpus cavernosum by the extract of Seokchang extract according to Example 1 occurs via the NO-cGMP system.
즉 석창포 추출물은 내피세포에서 산화질소의 합성을 증가시키고 가용성 구아닐산 고리화효소를 활성화시켜 cGMP의 생성을 증가시킴으로서 음경해면체 평활근을 이완시키는 것으로 판단할 수 있다. In other words, the extract of Seokchangpo can increase the synthesis of nitric oxide in the endothelial cells and activate the soluble guanylate cyclase to increase the production of cGMP, which can be considered to relax the smooth muscle of the cavernous cavernosal.
또한 석창포 추출물에 의한 음경해면체 평활근의 이완효과는 K+ 통로의 개방을 활성하여 일어나는 것임을 알 수 있다.
In addition, the relaxation effect of smooth muscle of corpus cavernosum by the extract of Seokchangpo extract is caused by activation of K + channel.
참고예Reference example
2. 실험 준비 2. Experimental preparation
2-1. 실험동물2-1. Experimental animal
샘타코(Samtako, Korea)으로부터 체중 380 g의 Sprague-Dawley (SD)계 웅성 백서를 분양받아 2주 동안 실험실 환경에 적응시켰다. Sprague-Dawley (SD) male white rats weighing 380 g were distributed from Samtako, Korea and were adapted to the laboratory environment for 2 weeks.
실험동물의 사육 및 동물 실험은 참고예 1-1의 기재사항과 동일하게 수행하였다.
The breeding of the experimental animals and the animal experiments were carried out in the same manner as described in Reference Example 1-1.
2-2. 시약 준비2-2. Reagent preparation
시약 준비는 참고예 1-2의 기재사항과 동일하게 준비되었다.
The reagent preparation was prepared in the same manner as described in Reference Example 1-2.
2-3. 음경해면체 내부압력 측정(2-3. Measuring pressure inside the corpus cavernosum intracavernosalintracavernosal pressurepressure : : ICPICP ))
몸무게가 약 400-450 g의 건강한 SD계 백서를 Sodium pentobabital (50 mg/kg. i.v.)로 마취하고 경동맥과 경정맥으로부터 각각 캐뉼라하여 경동맥으로 동맥압을 측정하고 경정맥으로 약물을 주입하였다. A healthy white rats weighing approximately 400-450 g were anesthetized with sodium pentobabital (50 mg / kg, i.v.) and cannulated with carotid artery and jugular vein, respectively, and carotid artery pressure was measured and injected into the jugular vein.
다음, 음경부위를 절개하여 음경을 완전히 노출한 후에 오른쪽 음경내부에 23 G의 needle을 삽입하고 방광신경총을 전기자극기에 연결하여 10 v, 0.1 ms, 3 Hz 및 5 Hz 강도로 5분 간격으로 전기적인 자극을 주어 음경내부압력을 측정하였다.
Then, the penis was incised and the penis was completely exposed. A 23 G needle was inserted into the right penis, and the bladder plexus was connected to an electrical stimulator, and electrical stimulation was performed at 5 min intervals at 10 V, 0.1 ms, 3 Hz and 5 Hz intensity And the pressure inside the penis was measured.
2-4. 통계처리2-4. Statistical processing
통계처리는 참고예 1-6의 기재사항과 동일하게 처리하였다.
The statistical treatment was carried out in the same manner as described in Reference Example 1-6.
실험예5Experimental Example 5
. .
석창포Seokchangpo
추출물의 음경해면체 내부압력 증가 효과 The effect of the extract on the internal pressure of the corpus cavernosum
도 5는 실험예 5에 따른 음경해면체 내부압력에 대한 ICP 측정 결과(Saline:vehicle, sildenafil:positive control, Each value shows mean ± S.D. (n=6). *p<0.05, **p<0.01, ***p<0.001 vs. saline group.)를, 도 6은 ICP/MAP 측정 결과(Each value shows mean ± S.D. (n=6). *p<0.05, **p<0.01, ***p<0.001 vs. saline group.)를, 도 7은 AUC 측정 결과(Each value shows mean ± S.D. (n=6). *p<0.05, **p<0.01, ***p<0.001 vs. saline group.)를 각각 나타내는 도면이다.
FIG. 5 is a graph showing the results of ICP measurement (saline: vehicle, sildenafil: positive control, each value shows mean ± SD (n = 6). * P <0.05, ** p <0.01, *** p <0.001 vs. saline group. FIG. 6 shows ICP / MAP measurement results (Each value shows mean SD (n = 6). * p <0.05, ** p < (P <0.05, ** p <0.01, *** p <0.001 vs. saline group, p <0.001 vs. saline group) Respectively.
석창포 추출물(EAG) 30 mg/kg, saline 0.9% NaCl, sildenafil 1mg/kg의 농도로 경정맥으로부터 약 0.1 ml/min의 속도로 주입하여 ICP, ICP/MAP와 AUC의 변화를 측정하였다. ICP, ICP / MAP, and AUC were measured by injecting 30 mg / kg of salicylic acid (EAG), saline 0.9% NaCl, and
이때 ICP(intracavernosal pressure)는 전기적인 자극을 준 시점으로부터 음경해면체 내부의 압력이 최고치에 달하였을 때의 수치이며, ICP/MAP는 음경해면체 내부의 압력이 최고치에 달하였을 때의 수치를 그에 상응하는 혈압으로 나눈 비율, 그리고 AUC (area under curve of cavernosometry)는 전기적인 자극을 준 1분 동안에 증가된 압력의 면적값을 계산한 수치이다.
ICP (intracavernosal pressure) is the value when the pressure inside the corpus cavernosum reaches the maximum from the time of the electric stimulation. ICP / MAP is the value when the pressure inside the corpus cavernosum reaches its peak, The ratio of blood pressure divided by area under curve of cavernosometry (AUC) is calculated by calculating the area of increased pressure over one minute of electrical stimulation.
도 5 내지 도 7을 참조하여 보면, 음경 해면체 내부압력(Intra-cavernosal pressure, ICP)의 최고치, 음경해면체 최대 내압/혈압(ICP/MAP) 및 AUC(Area under the curve) 수치가 각각 나타나 있으며, 석창포 추출물이 농도의존적으로 내부압력을 증가시켰음을 알 수 있다.5 to 7, the values of the intracavalular pressure (ICP), the ICP / MAP, and the area under the curve (AUC) are shown, respectively. It can be seen that the extract of Seokchangpo increased the internal pressure in a concentration dependent manner.
또한 saline 만 주입한 군과 비교하여 음경 해면체 내부압력을 유의성 있게 증가시켰음을 알 수 있다.
It was also found that the pressure in the corpus cavernosum was significantly increased compared with the saline alone group.
실험예 5를 정리하여 보면, 석창포 추출물은 음경 해면체 내에서의 국부적인 발기개선 효과가 보유하고 있음을 알 수 있다.Experimental Example 5 is summarized as follows. It can be seen that Seokchangpo extract has a local erectile improving effect in the corpus cavernosum.
또한 AUC 수치가 투여용량(dose)/청소율(clearance)이라는 점을 보면, 석창포 추출물의 발기기능 지속효과가 현저하다는 점을 나타낸다고 할 수 있다.
In addition, the AUC value is a dose / clearance, indicating that the effect of the extract of Seokchangpo on the erectile function is remarkable.
실험예 1 내지 5를 총괄하여 보면, 실시예 1에 따른 석창포 추출물은 NO-cGMP경로를 통한 음경해면체 평활근 이완 효과를 가지고 있으며, 또한, K+ 통로를 개방하여 과분극을 일으킴으로서 음경해면체 평활근을 이완시킨다고 할 수 있다.In Experimental Examples 1 to 5 as a whole, the extract of Seokchonpo according to Example 1 has relaxation effect of the penile cavernosal smooth muscle through the NO-cGMP pathway, and relaxes the smooth muscle of the cavernous cavernous smooth muscle by causing the hyperpolarization by opening the K + It can be said that.
또한 석창포 추출물은 국부적인 발기 효과 및 발기기능 지속 효과를 보유하고 있다고 할 수 있다.
In addition, Seokchangpo extract has a local erectile effect and a sustained effect of erectile function.
Claims (5)
Seok Changpo (Acorns, Acorns The present invention relates to a pharmaceutical composition for preventing and treating erectile dysfunction, which comprises an extract of Gramineus Soland as an active ingredient.
상기 추출물은 에탄올로 추출하여 얻어지는 것을 특징으로 하는 발기부전 질환의 예방과 치료를 위한 약학 조성물.
The method according to claim 1,
Wherein the extract is obtained by extracting with ethanol.
상기 추출물은 NO-cGMP경로를 통하여 음경해면체 평활근을 이완하는 것을 특징으로 하는 발기부전 질환의 예방과 치료를 위한 약학 조성물.
The method according to claim 1,
Wherein the extract relaxes the smooth muscle of the penile cavernosum through the NO-cGMP pathway.
상기 추출물은 K+ 통로 개방을 통하여 과분극을 일으켜 음경해면체 평활근을 이완하는 것을 특징으로 하는 발기부전 질환의 예방과 치료를 위한 약학 조성물.
The method according to claim 1,
Wherein the extract has hyperpolarization through the opening of the K + channel to relax the smooth muscle of the penile cavernosum.
A health functional food composition for preventing or improving erectile dysfunction, wherein a food additive is added to an extract of Seokchangba ( Acorus gramineus Soland).
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Non-Patent Citations (3)
Title |
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B. Singh et al. International Journal of Pharmaceutical Sciences Review and Research. Volume 5, Pages 104-113 (2010) * |
B. Singh et al. International Journal of Pharmaceutical Sciences Review and Research. Volume 5, Pages 104-113 (2010)* |
P. Temkitthawon et al. Journal of Ethnopharmacology. Volume 119, No. 2, Pages 214-217 (2008) * |
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