KR20120058413A - Antibacterial Composition Containing Zanthoxylum schinifolium Extract - Google Patents
Antibacterial Composition Containing Zanthoxylum schinifolium Extract Download PDFInfo
- Publication number
- KR20120058413A KR20120058413A KR1020110122852A KR20110122852A KR20120058413A KR 20120058413 A KR20120058413 A KR 20120058413A KR 1020110122852 A KR1020110122852 A KR 1020110122852A KR 20110122852 A KR20110122852 A KR 20110122852A KR 20120058413 A KR20120058413 A KR 20120058413A
- Authority
- KR
- South Korea
- Prior art keywords
- helicobacter
- extract
- active ingredient
- bergapten
- lupeol
- Prior art date
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Abstract
Description
본 발명은 산초 (Zanthoxylum schinifolium) 추출물 및 이로부터 분리한 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 헬리코박터균에 대한 항균 조성물에 관한 것이다.
The present invention relates to an antimicrobial composition against Helicobacter spp. Comprising Zanthoxylum schinifolium extract and bergapten or lupeol isolated therefrom as an active ingredient.
1982년 호주의 마샬 (Marshall)과 워렌 (Warren) 그리고 굳윈 (Goodwin)에 의해 B형 위염 환자의 위점막에서 순수 분리된 헬리코박터 파이로리균은 B형 만성위염, 위궤양과 십이지장궤양을 유발시키며 위암발생의 일차적 결정 요인으로 알려져 있다. 헬리코박터 파이로리균의 감염에 의한 위 및 십이지장질환의 발병기전 중 특히 위의 염증 유도에 있어 요소 분해효소인 우레아제 (urease)를 주요 인자로 들 수 있다. 헬리코박터 파이로리균은 전체 단백질의 6%에 해당하는 우레아제를 생성하는데, 생성된 우레아제는 요소를 암모니아와 이산화탄소로 분해하여 세균 주위환경을 중화하여 위 내강의 염산에 의한 공격을 방어할 뿐만 아니라, 위 점막에 축적된 암모니아 자체가 직접 위 점막 상피세포에 세포독성을 나타내어 위 점막 손상이 유발된다 (Sidebotham R.L., et al., J. Clin.Pathol.,44, pp 52-57, 1991). 이러한 우레아제의 작용으로 인해, 위 내강의 위산이 점막층 아래로 역류하게 되어 위산이 위 점막 상피세포를 광범위하게 손상시켜 위염과 위궤양이 발생한다. 또한, 암모니아 자체가 위 점액층 세포의 산소 소비와 미토콘드리아의 ATP 생성을 저해하고 (Tsujii M., et al., Gastroenterology, 102, pp 1881-1888, 1992), 궁극적으로 모노클로로아민 (monochloroamine)을 형성하여 반응성 산소종 (reactive oxygen pecies)을 생성하기 때문에 세포 손상을 유발하여 만성염증을 일으키고, 나아가 DNA 손상을 일으켜 암 발생 과정을 촉진시킨다는 보고가 있다 (Hahm K.B., et al., Am. J.Gastroenterol., 92, pp 1853-1857, 1997).Helicobacter pylori isolated from Marshall's, Warren and Goodwin's gastric mucosa in Australia in 1982 caused hepatitis B, gastric ulcer and duodenal ulcer. It is known as the primary determinant. Among the pathogenesis of gastrointestinal and duodenal diseases caused by Helicobacter pylori infection, urease, a urease, is particularly important in inducing inflammation of the stomach. Helicobacter pylori produces urease, which is 6% of the total protein. The urease breaks down urea into ammonia and carbon dioxide, neutralizes the bacterial environment, and protects against gastric mucosa attack. Ammonia itself accumulates directly in the gastric mucosal epithelial cells, causing gastric mucosal damage (Sidebotham RL, et al., J. Clin. Pathol., 44, pp 52-57, 1991). Due to the action of this urease, gastric acid in the gastric lumens flows back down the mucosal layer, which causes gastric inflammation and gastric ulceration. In addition, ammonia itself inhibits oxygen consumption of gastric mucosa cells and ATP production in mitochondria (Tsujii M., et al., Gastroenterology, 102, pp 1881-1888, 1992), ultimately forming monochloroamine It has been reported to produce reactive oxygen pecies, causing cell damage, causing chronic inflammation, and further DNA damage, thereby promoting the cancer development process (Hahm KB, et al., Am. J. Gastroenterol). , 92, pp 1853-1857, 1997).
헬리코박터의 전염은 동물 또는 인간을 통하거나, 의료행위시 부주의 또는 식품 등의 다양한 경로를 통하여 이루어지고 (Dunn, B. E., Cohen, H., and Blaser, M. J. (1997). Clinical Microbiology Reviews, 10 (4), 720-7; Kodaira, M.S., Escobar, A. M. U., & Grisi, S. (2002) Revista de Sade Pade Pblica.36: 356-369), 일단 감염되고 나면 쉽게 박멸되지 않는다.The transmission of Helicobacter is through animals or humans, or through various channels such as carelessness or food in medical practice (Dunn, BE, Cohen, H., and Blaser, MJ (1997). Clinical Microbiology Reviews, 10 (4) ), 720-7; Kodaira, MS, Escobar, AMU, & Grisi, S. (2002) Revista de Sade Pade Pblica. 36: 356-369), once infected, are not easily eradicated.
또한, 현재까지 사람과 동물에서 분리되는 헬리코박터 파이로리와 유사한 세균으로 헬리코박터 파이로리(Helicobacter pylori), 헬리코박터 카니스 (Helicobacter canis), 헬리코박터 시내디 (Helicobacter cinaedi), 헬리코박터 헤일마니 (Helicobacter heilmannii), 헬리코박터 펠리스 (Helicobacter felis), 헬리코박터 무스틸레 (Helicobacter mustelae), 헬리코박터 페넬리에 (Helicobacter fenelliae), 헬리코박터 라피니(Helicobacter rappini), 헬리코박터 헤파티쿠스 (Helicobacter hepaticus), 헬리코박터 빌리스 (Helicobacter bilis), 헬리코박터 풀로룸 (Helicobacter pullorum) 등이 알려져 있다.Helicobacter pylori-like bacteria that have been isolated from humans and animals to date are also known as Helicobacter pylori, Helicobacter canis, Helicobacter cinaedi, Helicobacter heilmann II, Helicobacter felis, Helicobacter mustelie, Helicobacter fenelliae, Helicobacter raffelli, Helicobacter hepaticus, Helicobacter bilis bacilli (Helicobacter bacilli) (Helicobacter pullorum) and the like are known.
헬리코박터 파이로리는 인간에게 특이적이며 위장 내의 특정 장소에서 주로 발견되는데, 소화성 궤양 (예를 들면, 위궤양 또는 십이지장 궤양 등), 염증 (예를 들면, 위염 등), 위암 등의 소화관 상부의 질환, MALT (점막-관련 임파조직 (mucosaassociated lymphoid tissue)) 임파종의 병인 또는 만성 심장 질환의 배경 병원성 인자라고 한다. 현재, 헬리코박터 파이로리 감염증 치료에 관한 연구는 활발히 이루어지고 있으며, 그의 치료법으로서는 제거를 목적으로 한 것, 재발 방지를 목적으로 한 것 등이 다수 보고되어 있다.Helicobacter pylori is specific to humans and is primarily found in certain places in the stomach, such as peptic ulcers (e.g. gastric or duodenal ulcers), inflammation (e.g. gastritis, etc.), diseases of the upper digestive tract such as gastric cancer, MALT (Mucosaassociated lymphoid tissue) Background of pathogenesis of lymphoma or chronic heart disease. At present, studies on the treatment of Helicobacter pylori infection have been actively conducted, and as a treatment method thereof, many reports for the purpose of removal and prevention of recurrence have been reported.
상술한 바와 같이, 헬리코박터 파이로리가 위장 질환에서 매우 위험한 미생물이지만, 천연소재를 이용한 적절한 항균물질 등 개발이 부족한 실정이다. 현재 헬리코박터 파이로리 치료법으로는 비스무스 (bismuth)제제, 메트로니다졸 (metronidazole)과 함께 테트라사이클린 (tetracycline) 또는 아목실린 (amoxicillin)을 방용 처리하는 일반적인 3중 요법과 비스무스 제제, 오메파라졸 (omeparazole), 테트라사이클린 및 메트로니다졸을 혼합한 4중 요법 등이 보고되어 있다. 그러나, 항생제 투여에 의한 내성 균주 출현 및 위 내에서의 약물의 침투성과, 치료 후에 성장이 억제되어 있던 균이 재 증식하는 문제가 지적되고 있다. 이런 이유로 헬리코박터 파이로리에 특이적인 항균물질을 탐색하려는 수많은 노력이 이루어졌으며, 최근에는 식물류에 들어있는 생리활성 성분에 대한 관심이 높아지고 있으며, 이들의 생체 조절 기능 및 질병의 회복이나 예방 등에 관한 가능성이 제시되어 왔다. 최근 백리향, 중국차, Cashew apple, 소목과 황련 등 여러 천연물의 헬리코박터 파이로리에 대한 항균활성이 보고되었으나, 아직은 연구가 미진한 실정이다.As described above, Helicobacter pylori is a very dangerous microorganism in gastrointestinal diseases, but there is a lack of development of appropriate antibacterial materials using natural materials. Current Helicobacter pylori treatments include general triple therapy, bismuth preparations, bismuth preparations, omeparazole and tetracycline in combination with bismuth preparations, metronidazole, and tetracycline or amoxicillin. And quadruple therapy with metronidazole. However, it has been pointed out that the emergence of resistant strains by antibiotic administration, the penetration of drugs in the stomach, and the regrowth of bacteria whose growth has been inhibited after treatment. For this reason, numerous efforts have been made to search for antimicrobial substances specific to Helicobacter pylori, and recently, interest in bioactive components in plants has increased, suggesting the possibility of their bioregulatory function and recovery or prevention of diseases. Has been. Recently, the antimicrobial activity of Helicobacter pylori of various natural products, such as thyme, Chinese tea, Cashew apple, joiner and rhubarb, has been reported, but the research is still insufficient.
따라서 자원이 많고 쉽게 구할 수 있는 식용민속자원으로부터 헬리코박터 파이로리에 대한 항균소재 발굴은 테트라사이클린 등 항생제를 대체할 중요한 소재이다. 특히, 가장 이상적인 헬리코박터 파이로리균에 대한 항균제는 항균 역할뿐 아니라 위상피세포에 자극을 주지 않는 것이다. Therefore, the discovery of antimicrobial material for Helicobacter pylori from abundant and easily available edible folk resources is an important material to replace antibiotics such as tetracycline. In particular, the antimicrobial agent against the most ideal Helicobacter pylori bacteria is not only an antibacterial role but also does not stimulate the epithelial cells.
이에 본 발명자는 상기한 바와 같은 문제점을 해결하기 위하여, 위장에 위해하지 않으면서 헬리코박터에 항균효과가 우수한 천연항균 소재를 찾기 위한 연구를 계속하던 중, 산초 추출물 및 이로부터 분리한 베르갑텐 (bergapten) 또는 루페올 (lupeol)이 위장에 상재하는 헬리코박터 파이로리균에 대한 항균효과를 갖는 것을 발견함으로써 본 발명을 완성하였다.
In order to solve the problems described above, the inventors continue to search for natural antibacterial material having excellent antibacterial effect on Helicobacter without harming the stomach, while extracting and extracting bergapten from it Alternatively, the present invention has been completed by finding that lupeol has an antimicrobial effect against Helicobacter pylori bacteria present in the stomach.
본 발명의 목적은 헬리코박터균에 대한 항균 조성물 및 헬리코박터 파이로리균에 의한 위 및 십이지장질환의 예방 및 치료용 조성물을 제공하는 것이다.
An object of the present invention is to provide an antimicrobial composition against Helicobacter bacteria and a composition for the prevention and treatment of gastrointestinal and duodenal diseases caused by Helicobacter pylori.
상기 목적을 달성하기 위하여 본 발명은 산초 추출물을 유효성분으로 포함하는 헬리코박터균에 대한 항균 조성물을 제공한다. In order to achieve the above object, the present invention provides an antimicrobial composition against Helicobacter bacterium comprising an acid extract as an active ingredient.
또한 본 발명은 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 헬리코박터균에 대한 항균 조성물을 제공한다. The present invention also provides an antimicrobial composition against Helicobacter bacteria comprising bergapten or lupeol as an active ingredient.
또한 본 발명은 산초 추출물을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 치료용 약학적 조성물을 제공한다.The present invention also provides a pharmaceutical composition for the prevention and treatment of gastrointestinal and duodenal diseases, including the extract of Sancho as an active ingredient.
또한 본 발명은 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 치료용 약학적 조성물을 제공한다.The present invention also provides a pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, including bergapten or lupeol as an active ingredient.
또한 본 발명은 산초 추출물을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 개선용 건강기능식품을 제공한다.In another aspect, the present invention provides a health functional food for the prevention and improvement of gastric and duodenal disease comprising an extract of the extract as an active ingredient.
또한 본 발명은 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 개선용 건강기능식품을 제공한다.
In another aspect, the present invention provides a dietary supplement for preventing and improving gastrointestinal and duodenal diseases, including bergapten or lupeol as an active ingredient.
본 발명의 항균성 산초 추출물 및 이로부터 분리한 베르갑텐 (bergapten) 또는 루페올 (lupeol)은 헬리코박터 파이로리균에 항균 활성을 보이면서도 위장에 자극을 주지 않아, 헬리코박터 파이로리균에 의한 각종 위장 질환을 예방 및 치료하는데 유용하다.
The antimicrobial sancho extract of the present invention and bergapten or lupeol isolated therefrom exhibit antimicrobial activity to Helicobacter pylori, but do not irritate the stomach, preventing and preventing various gastrointestinal diseases caused by Helicobacter pylori. It is useful for treatment.
도 1은 산초 추출물의 분획 모식도이다.
도 2는 산초 메탄올 추출물의 항균활성 결과이다.
도 3은 산초 분획물의 항균활성 결과이다.
도 4는 산초 추출물에서 분리한 베르갑텐 (bergapten) 또는 루페올 (lupeol)의 항균활성 결과이다. Figure 1 is a schematic diagram of the fraction of the extract.
Figure 2 is the antimicrobial activity of the methanol extract of Sancho.
Figure 3 shows the antimicrobial activity of the acid fraction.
Figure 4 shows the antimicrobial activity of bergapten or lupeol isolated from the extracts.
이하 본 발명에 대하여 보다 상세히 설명한다. Hereinafter, the present invention will be described in more detail.
하나의 양태로서, 본 발명은 산초 추출물을 유효성분으로 포함하는 헬리코박터균에 대한 항균 조성물을 제공한다. In one embodiment, the present invention provides an antimicrobial composition against Helicobacter bacterium comprising an acid extract as an active ingredient.
산초나무는 학명 잔톡실럼 스키니폴리움 (Zanthoxylum schinifolium)인 운향과에 속하는 식물로, 분지나무 또는 상초나무라고도 불린다. 산초나무는 우리나라, 일본, 중국 등 동북아시아에 널리 자생하고 있으며, 산초나무의 껍질, 잎 및 과실은 향신료, 약용 및 제유용으로 사용되고 있다(이종원 (1998) 한국식품영양학회, 11(5), p493-498).Japanese vine is the scientific name of Zanthoxylum schinifolium ) is a plant belonging to the Unhyangdae family, also called branched or lettuce. It is widely grown in Northeast Asia such as Korea, Japan, and China, and the bark, leaves, and fruits of Japanese pepper are used for spice, medicinal and oil-making (Lee Jong-won (1998), The Korean Society of Food and Nutrition, 11 (5), p493-498).
본 명세서에서 사용된 용어 "추출물 (extract)"이란 천연물로부터 분리된 활성성분 즉, 목적하는 활성을 보이는 물질을 의미한다. 상기 추출물은 물, 유기용매 또는 이들의 혼합용매를 이용하는 추출과정으로 획득할 수 있으며, 추출물 이의 건조 분말 또는 이를 이용하여 제형화된 모든 형태를 포함한다. 또한, 상기 추출물에는 상기 추출과정을 거친 추출액을 분획한 것도 포함된다.As used herein, the term "extract" refers to an active ingredient isolated from natural products, that is, a material that exhibits the desired activity. The extract may be obtained by an extraction process using water, an organic solvent or a mixed solvent thereof, and includes the dry powder thereof or any form formulated using the extract. In addition, the extract also includes a fraction obtained by the extraction through the extraction process.
본 발명에 따른 산초 추출물은 다음과 같은 과정을 거쳐 얻어질 수 있다.Sancho extract according to the present invention can be obtained through the following process.
산초의 추출부위는 이에 제한되는 것은 아니나, 산초의 가지 또는 잎이 바람직하다. 산초를 알코올, 에틸아세테이트, 클로로포름, 메틸에틸케톤, 아세톤 및 에테르로 이루어진 그룹으로부터 선택된 1종 이상의 용매로 추출하여 감압 농축시킨다. 상기 알코올은 저급 또는 고급 알코올일 수 있으며, 바람직하게는 메탄올, 에탄올, 이소프로판올 및 부탄올로 이루어진 그룹으로부터 선택된 저급 알코올이고, 보다 바람직하게는 메탄올이다. 상기 알코올은 물과의 혼합물일 수 있다. 상기 농축물에 추가적으로 헥산, 메틸린 클로라이드, 에틸아세테이트, 부탄올 또는 물로 각각 분획하여 다시 감압농축을 할 수 있다. 상기 분획 농축물을 담체로는 실리카 또는 종이를, 전개용매로는 클로로포름:아세톤:개미산의 혼합용액을 이용하여 크로마토그래피 (종이, TLC, 컬럼 등)를 실시하여 정제하는 단계를 추가로 실시할 수 있다. 여기서, 담체에 함유된 물과 전개용매간의 추출물 내 물질들의 분배가 일어나고, 분배율의 차이에 따라 물질이 분리된다. 상기 전개용매에서 클로로포름:아세톤:개미산은 50~100:10~20:5~10, 가장 바람직하게는 75:16.5:8.5의 비율로 혼합할 수 있다. 상기 크로마토그래피는 담체로서 실리카를 이용한 박층 크로마토그래피 (TLC) 또는 컬럼 크로마토그래피일 수 있다. 상기 TLC는 유리판 또는 플라스틱과 같은 지지체에 실리카겔을 얇게 입히고, 그 위에 추출물을 점적한 후 전개용매로 전개하여 정제하는 방식이다. 상기 컬럼 크로마토그래피는 컬럼 내에 실리카를 충진하고, 그 위에 추출물을 로딩한 후 전개용매로 전개하여 정제하는 방식이다. 추출물의 대량 제조 시에는 컬럼 크로마토그래피를 이용하는 것이 바람직하다.The extracting portion of the herb is not limited thereto, but branch or leaf of the herb is preferable. The acetic acid is extracted with one or more solvents selected from the group consisting of alcohol, ethyl acetate, chloroform, methyl ethyl ketone, acetone and ether and concentrated under reduced pressure. The alcohol may be a lower or higher alcohol, preferably a lower alcohol selected from the group consisting of methanol, ethanol, isopropanol and butanol, more preferably methanol. The alcohol may be a mixture with water. In addition to the concentrate, hexane, methyl chloride, ethyl acetate, butanol or water may be fractionated and concentrated under reduced pressure again. The fractional concentrate may be further purified by chromatography (paper, TLC, column, etc.) using silica or paper as a carrier, and a mixed solution of chloroform: acetone: formic acid as a developing solvent. have. Here, the distribution of the substances in the extract between the water contained in the carrier and the developing solvent occurs, and the substances are separated according to the difference in distribution ratio. Chloroform: acetone: formic acid in the developing solvent may be mixed in a ratio of 50-100: 10-20: 5-10, most preferably 75: 16.5: 8.5. The chromatography may be thin layer chromatography (TLC) or column chromatography using silica as a carrier. The TLC is a method of applying a thin coating of silica gel to a support such as a glass plate or plastic, dropping the extract thereon and then developing with a developing solvent to purify. In the column chromatography, silica is packed into a column, an extract is loaded thereon, and then purified by developing with a developing solvent. It is preferable to use column chromatography for mass production of the extract.
본 발명의 상기 헬리코박터 세균은 특별히 한정되는 것은 아니고 헬리코박터 종 (species)에 포함되는 모든 세균을 포함할 수 있으나, 바람직하게는 헬리코박터 파이로리 (Helicobacter pylori), 헬리코박터 카니스 (Helicobacter canis), 헬리코박터 시내디 (Helicobacter cinaedi), 헬리코박터 헤일마니 (Helicobacter heilmannii), 헬리코박터 펠리스 (Helicobacter felis), 헬리코박터 무스틸레 (Helicobacter mustelae), 헬리코박터 페넬리에 (Helicobacter fenelliae), 헬리코박터 라피니 (Helicobacter rappini), 헬리코박터 헤파티쿠스 (Helicobacter hepaticus), 헬리코박터 빌리스 (Helicobacter bilis), 헬리코박터 풀로룸 (Helicobacter pullorum)으로 구성된 세균으로부터 선택된 것일 수 있다.The Helicobacter bacteria of the present invention is not particularly limited and may include all bacteria included in Helicobacter spp. Helicobacter cinaedi, Helicobacter heilmannii, Helicobacter felis, Helicobacter mustelae, Helicobacter helielli, Helicobacter helicobacterii Helicobacter hepaticus, Helicobacter bilis (Helicobacter bilis), Helicobacter pullorum (Helicobacter pullorum) may be selected from bacteria.
또한 본 발명은 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 헬리코박터균에 대한 항균 조성물을 제공한다. 상기 베르갑텐 (bergapten) 은 화학식 1의 구조를, 루페올 (lupeol)은 화학식 2의 구조를 가진다. 상기 베르갑텐 (bergapten) 또는 루페올 (lupeol)은 산초 추출물로부터 수득할 수 있으며, 합성 또는 제조사로부터 구입하여 사용할 수 있다. The present invention also provides an antimicrobial composition against Helicobacter bacteria comprising bergapten or lupeol as an active ingredient. Bergapten has the structure of Formula 1, and lupeol has the structure of Formula 2. The bergapten or lupeol can be obtained from the extract of the herb and can be used synthetically or purchased from the manufacturer.
또 다른 양태로서, 본 발명은 산초 추출물을 유효성분으로 포함하는 위 및 십이지장질환의 예방 및 치료용 약학적 조성물을 제공한다. In another aspect, the present invention provides a pharmaceutical composition for the prevention and treatment of gastrointestinal and duodenal diseases, including an extract of Sancho as an active ingredient.
또한 본 발명은 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 치료용 약학적 조성물을 제공한다.The present invention also provides a pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, including bergapten or lupeol as an active ingredient.
상기 위 및 십이지장 질환이란 헬리코박터 파이로리에 의해 유발되고, 위 또는 십이지장 부위에 발생하는 질환을 의미하며, 소화성 궤양과 위암을 포함하는 것일 수 있고, 바람직하게는 위염, 십이지장염, 위궤양, 십이지장궤양, 위선암, 위림프종 및 위암으로 이루어진 군에서 선택된 1종 이상일 수 있으며, 상기 위염은 바람직하게는 만성 위축성 위염일 수 있다. 헬리코박터 파이로리가 발견된 이후로, 상기 위, 십이지장 질환의 주 원인균은 헬리코박터 파이로리로 보고되고 있으며, 헬리코박터 파이로리는 위점막, 구체적으로는 상피세포 및 점막층에 주로 결합하여 서식하는 것으로 알려져 있다. 따라서, 상기 위, 십이지장 질환을 치료하기 위해서는 원인균인 헬리코박터 파이로리에 대한 항균활성이 뛰어난 우수한 물질을 처방할 수 있다.The gastric and duodenal diseases are caused by Helicobacter pylori, mean a disease occurring in the stomach or duodenal region, and may include peptic ulcer and gastric cancer, preferably gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric adenocarcinoma It may be at least one selected from the group consisting of gastric lymphoma and gastric cancer, the gastritis may preferably be chronic atrophic gastritis. Since the discovery of Helicobacter pylori, the main causative agent of gastric and duodenal diseases has been reported as Helicobacter pylori, Helicobacter pylori is known to inhabit mainly by binding to the gastric mucosa, specifically epithelial cells and mucosal layers. Therefore, in order to treat the stomach and duodenal disease, it is possible to prescribe an excellent antimicrobial activity against the causative bacterium Helicobacter pylori.
본 발명의 약학적 조성물은 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁액, 에멀전, 시럽, 에어로졸 등 경구 투여용 제형, 멸균 주사용액, 좌제 및 경피 투여용 제제로 제형화하여 사용될 수 있다. 조성물에 포함될 수 있는 담체, 부형제 및 희석제로는 락토오스, 덱스트로오스, 수크로오스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로오스, 메틸 셀룰로오스, 미정질 셀룰로오스, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 프로필히드록시벤조에이트, 탈크, 마그네슘 스테아레이트 및 광물유를 들 수 있다. 필요에 따라 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 제형화한다.The pharmaceutical compositions of the present invention can be used in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, oral dosage forms, sterile injectable solutions, suppositories, and transdermal formulations according to conventional methods. have. Carriers, excipients and diluents that may be included in the composition include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, Microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. If necessary, it is formulated with diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, surfactants and the like.
한 양태로서, 본 발명의 약학적 조성물은 경구 투여용 고상 제제로 제형화할 수 있다. 경구 투여를 위한 고상 제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되는데, 이러한 고상 제제는 상기 추출물에 적어도 하나 이상의 부형제 예를 들면, 전분, 칼슘 카르보네이트, 수크로오스 또는 락토오스, 젤라틴 등을 혼합하여 제형화된다. 또한, 단순한 부형제 이외에 마그네슘 스테아레이트, 탈크 같은 윤활제들도 사용될 수 있다.In one embodiment, the pharmaceutical compositions of the present invention may be formulated as a solid preparation for oral administration. Solid form preparations for oral administration include tablets, pills, powders, granules, capsules and the like, which include at least one excipient such as starch, calcium carbonate, sucrose or lactose, gelatin and the like. It is formulated by mixing. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used.
다른 양태로서, 본 발명의 약학적 조성물을 경구 투여용 액상 제제로 제형화할 수도 있다. 경구 투여를 위한 액상 제제는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데, 이러한 액상 제제에는 통상적으로 사용되는 불활성 희석제 (예를 들면, 정제수, 에탄올, 리퀴드 파라핀) 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다.In another embodiment, the pharmaceutical compositions of the present invention may be formulated into liquid preparations for oral administration. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups, and the like. In addition to conventional inert diluents (e.g., purified water, ethanol, liquid paraffin), various excipients may be used. Wetting agents, sweetening agents, fragrances, preservatives and the like can be included.
또 다른 양태로서, 본 발명의 약학적 조성물은 비경구, 바람직하게는 복강 내 투여를 위한 제제로 제형화될 수도 있다. 비경구 투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조 제제, 좌제가 포함된다. 멸균된 수용액으로는 한스 용액 (Hank's solution), 링거 용액 (Ringer's solution) 또는 물리적으로 완충된 염수와 같은 적절한 완충용액을 이용할 수 있으며, 비수성용제로, 현탁제로는 프로필렌글리콜, 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 이용될 수 있다. 필요에 따라 방부제, 안정화제, 습윤제 또는 유화제, 삼투압 조절을 위한 염 및/또는 완충제를 이용할 수도 있다. 한편, 좌제의 경우에는 이의 통상적인 기제인 위텝솔 (witepsol), 마크로골, 트윈 (tween) 61, 카카오지, 라우린지, 글리세로제라틴 등이 사용될 수 있다.In another embodiment, the pharmaceutical compositions of the present invention may be formulated into preparations for parenteral, preferably intraperitoneal administration. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As a sterile aqueous solution, suitable buffer solutions such as Hanks' solution, Ringer's solution, or physically buffered saline can be used.For non-aqueous solvents, suspensions include propylene glycol, polyethylene glycol, olive oil, Same vegetable oils, injectable esters such as ethyloleate, and the like can be used. If necessary, preservatives, stabilizers, wetting or emulsifying agents, salts for controlling osmotic pressure and / or buffers may also be used. On the other hand, suppositories, such as witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin, and the like may be used.
상기와 같은 방법으로 제형화된 조성물은 유효량으로 비경구 또는 경구 (경피, 피하, 정맥, 근육, 복강등)를 포함한 여러 경로를 통해 투여될 수 있다. 상기에서 "유효량"이란 환자에게 투여하였을 때, 예방 또는 치료 효과를 나타내는 양을 말한다. 본 발명에 따른 조성물의 투여량은 투여 경로, 투여 대상, 연령, 성별, 체중, 개인차 및 질병 상태에 따라 적절히 선택될 수 있다. 바람직하게는, 본 발명의 조성물은 질환의 정도에 따라 유효성분의 함량을 달리할 수 있으나, 바람직하게는 0.1~10000 mg/체중kg/day, 보다 바람직하게는 10~1000 mg/체중kg/day의 유효량으로 투여될 수 있다.Compositions formulated in such a manner can be administered in various amounts, including parenteral or oral (dermal, subcutaneous, intravenous, intramuscular, intraperitoneal) in an effective amount. As used herein, an "effective amount" refers to an amount exhibiting a prophylactic or therapeutic effect when administered to a patient. The dosage of the composition according to the present invention may be appropriately selected depending on the route of administration, subject of administration, age, sex, weight, individual difference and disease state. Preferably, the composition of the present invention may vary the content of the active ingredient depending on the degree of disease, preferably 0.1 to 10000 mg / kg / day, more preferably 10 ~ 1000 mg / kg / day It may be administered in an effective amount of.
또 다른 양태로서, 본 발명은 산초 추출물을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 개선용 건강기능식품을 제공한다. As another aspect, the present invention provides a dietary supplement for preventing and improving gastrointestinal and duodenal diseases, including an extract of Sancho as an active ingredient.
또한 본 발명은 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 유효성분으로 포함하는 위 및 십이지장질환 예방 및 개선용 건강기능식품을 제공한다.In another aspect, the present invention provides a dietary supplement for preventing and improving gastrointestinal and duodenal diseases, including bergapten or lupeol as an active ingredient.
본 발명의 조성물을 식품 또는 음료 첨가물로 사용할 경우, 상기 산초 추출물 또는 베르갑텐 (bergapten) 또는 루페올 (lupeol)을 그대로 첨가하거나, 다른 식품 또는 식품 성분과 함께 사용되고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 상기 산초 추출물 또는 베르갑텐 (bergapten) 또는 루페올 (lupeol)의 혼합양은 그의 사용목적 (예방, 건강 또는 치료적 처치)에 따라 적합하게 결정될 수 있다. When the composition of the present invention is used as a food or beverage additive, the above extract or Bergapten or lupeol may be added as it is, or used together with other food or food ingredients, and used appropriately according to conventional methods. Can be. The mixed amount of the acid extract or bergapten or lupeol may be appropriately determined depending on the purpose of use (prevention, health or therapeutic treatment).
건강을 목적으로 하거나 또는 건강 조절을 목적으로 하는 장기간의 섭취의 경우, 상기 산초 추출물은 안전성 면에서 아무런 문제가 없기 때문에, 장기간 복용이 가능하다.In the case of prolonged ingestion for health or health control, long-term administration is possible because the sancho extract has no problem in terms of safety.
상기 식품의 종류에는 특별한 제한은 없다. 상기 물질을 첨가할 수 있는 식품의 예로는 육류, 소세지, 빵, 초콜릿류, 캔디류, 스낵류, 과자류, 피자, 라면, 기타 면류, 껌류, 아이스크림류를 포함한 낙농제품, 각종 수프, 음료수, 차, 드링크제, 알코올 음료 및 비타민 복합제 등이 있다.There is no particular limitation on the kind of the food. Examples of the food to which the substance may be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, teas, and drinks. Alcoholic beverages and vitamin complexes.
음료수로 제형화할 경우에 항균성 산초 추출물 이외에 첨가되는 액체 성분으로는 이제 한정되지는 않으나, 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상술한 천연 탄수화물의 예는 모노사카라이드 (예, 포도당, 과당 등), 디사카라이드 (예, 말토오스, 수크로오스 등) 및 폴리사카라이드 (예, 덱스트린, 시클로덱스트린 등과 같은 통상적인 당), 및 자일리톨, 소르비톨, 에리스리톨 등의 당알코올이다. 상기 천연 탄수화물의 비율은 본 발명의 조성물 100㎖당 일반적으로 약 1 내지 20g, 바람직하게는 약 5 내지 12g이다. 상술한 것 이외의 향미제로서 천연 향미제 (타우마린, 스테비아 추출물 (예, 레바우디오시드A, 글리시르히진 등)) 및 합성 향미제 (예, 사카린, 아스파르탐 등)를 사용할 수 있다.The liquid component added in addition to the antimicrobial sancho extract when formulated into a beverage is not limited to the above, but may contain various flavors or natural carbohydrates, etc. as additional ingredients, as in conventional beverages. Examples of the above-mentioned natural carbohydrates include monosaccharides (e.g. glucose, fructose and the like), disaccharides (e.g. maltose, sucrose and the like) and polysaccharides (e.g. conventional sugars such as dextrin, cyclodextrin and the like), and xylitol Sugar alcohols such as sorbitol and erythritol. The proportion of said natural carbohydrates is generally about 1 to 20 g, preferably about 5 to 12 g per 100 ml of the composition of the present invention. As flavoring agents other than those mentioned above, natural flavoring agents (for example, taumarin, stevia extracts (e.g., rebaudioside A, glycyrrhizin, etc.)) and synthetic flavoring agents (e.g., saccharin, aspartame, etc.) can be used. .
다른 양태로서, 본 발명의 식품 조성물은 여러 가지 영양제, 비타민, 광물 (전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 증진제 (치즈, 초콜릿 등), 펙트산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산 음료에 사용되는 탄산화제 등을 함유할 수 있다. 또한, 본 발명의 식품 조성물은 과일 및 야채 음료의 제조를 위한 과육을 함유할 수 있다. 이러한 성분은 단독으로 또는 조합으로 사용될 수 있으며, 이러한 첨가제의 비율은 조성물 전체 중량당 10 내지 20 중량%의 범위에서 선택할 수 있다.
In another embodiment, the food composition of the present invention comprises various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic and natural flavoring agents, colorants and enhancers (cheese, chocolate, etc.), pectic acid and salts thereof, organic acids , Protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated beverages, and the like. The food composition of the present invention may also contain pulp for the production of fruit and vegetable drinks. These ingredients may be used alone or in combination, and the proportion of such additives may be selected in the range of 10 to 20% by weight, based on the total weight of the composition.
이하 본 발명의 이해를 돕기 위하여 바람직한 실시예 및 제조예를 제시한다. 그러나 하기의 실시예 및 제조예는 본 발명을 보다 쉽게 이해하기 위하여 제공되는 것일 뿐, 실시예 및 제조예에 의해 본 발명의 내용이 한정되는 것은 아니다.
Hereinafter, preferred examples and preparation examples are provided to aid in understanding the present invention. However, the following examples and preparations are merely provided to more easily understand the present invention, and the contents of the present invention are not limited by the examples and preparations.
실시예Example 1. 산초 메탄올 및 1. Methanol and 분획물의Fraction 수득 purchase
산초를 음건한 후 메탄올 (methanol)을 이용해 계통적 추출을 실시하며 3회 이상 추출한 다음 40 ℃에서 감압농축기 (CCA-1100, EYELA)로 감압, 농축시켜, 산초 메탄올 추출물을 수득하였다. After drying the acid was extracted systematically using methanol (methanol) and extracted three times or more, and then concentrated under reduced pressure (CCA-1100, EYELA) at 40 ℃ under reduced pressure, to give a methanol extract of acid.
상기 메탄올 추출물을 헥산, 메틸린 클로라이드, 에틸아세테이트, 부탄올 또는 물로 각각 분획하여, 산초 분획물을 수득하였다. 분획 모식도는 도 1에 나타내었다.
The methanol extract was partitioned into hexane, methylene chloride, ethyl acetate, butanol or water, respectively, to obtain an acidic fraction. Fractional schematics are shown in FIG. 1.
실시예Example 2. 헬리코박터 2. Helicobacter 파이로리균에Pylori 대한 항균 효과 실험 Antimicrobial effect test
위, 십이지장 궤양등의 원인균인 헬리코박터 파이로리는 헬리코박터 파이로리 strain 26695로서 헬리코박터 파이로리 분리 균주은행에서 분양받아 사용하여 균의 배양에 최적배지 (Brucella Broth 0.56g <Pancreatic digest of casein 0.2g, dextrose 0.2g, Yeast extract 0.04g, sodium chloride 0.1g, sodium bisulfate 0.002g>, agar 0.24 g, Horse serum 2mL) 를 사용하였다. 미호기성 조건을 유지시켜 주기 위해서 10% CO2 incubator에서 95% 이상으로 유지하며 배양하였다. agar plate상에서 배양은 37℃로 48~72시간 동안 실시하였다.Helicobacter pylori, a causative agent of stomach and duodenal ulcers, is a Helicobacter pylori strain 26695, which is available from Helicobacter pylori isolated strain banks for optimal culture of bacteria (Brucella Broth 0.56g <Pancreatic digest of casein 0.2g, dextrose 0.2g, Yeast) extract 0.04 g, sodium chloride 0.1 g, sodium bisulfate 0.002 g>, agar 0.24 g, Horse serum 2 mL). In order to maintain aerobic conditions, the culture was maintained at 95% or more in a 10% CO 2 incubator. Incubation on an agar plate was carried out at 37 ° C. for 48-72 hours.
헬리코박터 파이로리 최적 배지 plate에 균분산액 100μL를 분주하여 멸균 유리봉으로 도말한 다음, 멸균된 disc paper (지름 8mm)를 올리고 0.45㎛ membrane filter로 제균한 각 추출물을 vacuum evaporator로 농축한 후 멸균수로 희석하여 다양한 농도의 각 추출물 30μL를 disc paper에 흡수시키고, 대조구로는 멸균수를 흡수시킨 후 37℃의 미호기성 조건에서 24시간 동안 incubation한 다음 disc주위의 clear zone 생성 유무를 확인하였다. Dispense 100 μL of the homogenous solution into a Helicobacter Pylori optimal medium plate, spread it with a sterile glass rod, place sterilized disc paper (8 mm in diameter), concentrate each extract sterilized with a 0.45 μm membrane filter, and dilute with sterile water. 30μL of each extract of various concentrations was absorbed into disc paper, and the control was absorbed in sterile water and then incubated for 24 hours at 37 ° C. in aerobic conditions, and then the presence of clear zones around the disc was confirmed.
2.1. 산초 메탄올 추출물의 항균활성 측정2.1. Antimicrobial Activity of Methanol Extract
산초 메탄올 추출물의 헬리코박터 파이로리균에 대한 항균효과를 살펴본 결과, 도 2에 나타낸 바와 같이, 멸균수에서는 Clear zone 이 8 mm로 나타나 헬리코박터 파이로리균의 항균효과가 없는 것으로 나타났으나, 10 μg/30μL농도의 산초나무 30μL 즉 10 μg의 산초나무에서는 Clear zone 이 17 mm으로 나타나 헬리코박터 파이로리균에 대한 항균효과를 확인하였다. As a result of examining the antimicrobial effect of Helicobacter pylori bacteria of methanol extract of Sancho, as shown in Fig. 2, the clear zone was 8 mm in sterile water, which showed no antimicrobial effect of Helicobacter pylori, but the concentration of 10 μg / 30μL 30 μL of vinegar, or 10 μg of vinegar, had a clear zone of 17 mm, confirming the antimicrobial effect against Helicobacter pylori.
2.2. 산초 메탄올 추출물의 2.2. Of Sancho methanol extract 분획물Fraction 및 활성 성분의 항균활성 측정 And antimicrobial activity of active ingredients
헬리코박터 파이로리균에 대한 항균활성을 나타내는 유효성분을 확인하기 위하여, 산초 메탄올 추출물을 유기용매로 분획한 후 (도 1), 분획층에서의 항균활성을 확인하였다. 실험 결과, 도 3에 나타낸 바와 같이, 산초 분획물 Hx, MC, EtOAc, BuOH은 E. coli 및 S. aureus의 일반세균에 대한 항균활성은 보이지 않았으나, H. pylori에 대해서는 Hx와 MC 분획물이 각각 11 mm, 10 mm의 억제환을 보였다.In order to confirm the active ingredient exhibiting the antimicrobial activity against Helicobacter pylori bacteria, after extracting the methanol extract of the vinegar with an organic solvent (Fig. 1), the antimicrobial activity in the fractionation layer was confirmed. Experimental results, as shown in Figure 3, the acid fractions Hx, MC, EtOAc, BuOH is E. coli The antimicrobial activity of S. aureus against S. aureus was not shown, but H. pylori Hx and MC fractions showed inhibitory effects of 11 mm and 10 mm, respectively.
상기 실험결과를 바탕으로, 활성 분획인 MC분획으로부터 항균활성을 나타내는 베르갑텐 (bergapten) 및 루페올 (lupeol)을 TLC를 통하여 확인하였다. 그 구조는 NMR을 통하여 동정하였으며, 하기 화학식 1 및 2에 나타내었다. Based on the experimental results, bergapten and lupeol showing antimicrobial activity from the active fraction MC fractions were identified through TLC. The structure was identified through NMR, and shown in the following formula (1) and (2).
Bergapten ; 1H-NMR (500 MHz, CDCl3):δ 4.26 (3H, s, OMe), 6.26 (1H, d, J = 9.5 Hz, H-3), 7.02 (1H, s, H-3’), 7.12 (1H, s, H-8), 7.59 (1H, s, H-2’), 8.14 (1H, d, J = 9.5 Hz, H-4)Bergapten; 1 H-NMR (500 MHz, CDCl 3 ): δ 4.26 (3H, s, OMe), 6.26 (1H, d, J = 9.5 Hz, H-3), 7.02 (1H, s, H-3 '), 7.12 (1 H, s, H-8), 7.59 (1H, s, H-2 '), 8.14 (1H, d, J = 9.5 Hz, H-4)
[화학식 1] [Formula 1]
Lupeol ; 1H-NMR (500 MHz, CDCl3):δ 0.76 (3H, s, H-28 ), 0.79 (3H, s, H-23), 0.83 (3H, s, H-25), 0.94 (3H, s, H-24), 0.97 (3H, s, H-27), 1.03 (3H, s, H-26), 1.68 (3H, s, H-30), 2.38 (1H, dd, J = 5.2, 11.0 Hz, H-19), 3.19 (1H, br d, J = 11.0 Hz, H-3), 4.56 (1H, br s, H-29b), 4.68 (1H, br s, H-29a)Lupeol; 1 H-NMR (500 MHz, CDCl 3 ): δ 0.76 (3H, s, H-28), 0.79 (3H, s, H-23), 0.83 (3H, s, H-25), 0.94 (3H, s, H-24), 0.97 (3H, s, H-27), 1.03 (3H, s, H-26), 1.68 (3H, s, H-30), 2.38 (1H, dd, J = 5.2, 11.0 Hz, H-19), 3.19 (1H, br d, J = 11.0 Hz, H-3), 4.56 (1H, br s, H-29b), 4.68 (1H, br s, H-29a)
[화학식 2] [Formula 2]
상기 과정을 통하여 MC분획층에서 얻은 활성물질인 베르갑텐 (bergapten) 및 루페올 (lupeol)의 항균활성을 확인한 결과, 헬리코박터 파이로리 균에 대해 베르갑텐 (bergapten)은 11mm 생육 억제환, 루페올 (lupeol)은 12mm의 큰 생육 억제환을 나타내었다 (도 4).As a result of confirming the antimicrobial activity of bergapten and lupeol, which are active substances obtained from the MC fraction layer, bergapten is 11 mm growth inhibitory ring, lupeol against Helicobacter pylori ) Shows a large growth inhibition ring of 12 mm (FIG. 4).
따라서, 본 실험을 통하여 국내 자생식물인 산초의 추출물 및 이로부터 분리한 활성 성분인 베르갑텐 (bergapten) 및 루페올 (lupeol)이 헬리코박터 파이로리균에 대한 뛰어난 항균활성을 보임을 확인하였으며, 이러한 항균활성을 바탕으로 헬리코박터 파이로리균에 의해 발생하는 위장 질환의 예방 및 치료제로 이용될 수 있음을 확인하였다.
Therefore, it was confirmed through the present experiment that the extracts of native Korean native plants and the active ingredients isolated from the bergapten (bergapten) and lupeol (lupeol) showed excellent antimicrobial activity against Helicobacter pylori, such antimicrobial activity On the basis of this, it was confirmed that it can be used as a preventive and therapeutic agent for gastrointestinal diseases caused by Helicobacter pylori.
이하 본 발명의 상기 조성물을 포함하는 약학적 조성물 및 건강기능식품의 제제예를 설명하나, 본 발명은 이를 한정하고자 함이 아닌 단지 구체적으로 설명하고자 함이다.
Hereinafter will be described a pharmaceutical composition comprising the composition of the present invention and a preparation example of a health functional food, the present invention is not intended to limit this but only to be described in detail.
제제예Formulation example 1. One. 산제의Powder 제조 Produce
산초 추출물 또는 베르갑텐 또는 루페올 2g2 ounces of extract or vergatten or lupeol
유당 100 mg
탈크 10 mg
상기의 성분들을 혼합하고 기밀포에 충진하여 산제를 제조한다.
The above components are mixed and filled in airtight bags to prepare powders.
제제예Formulation example 2. 정제의 제조 2. Preparation of tablets
산초 추출물 또는 베르갑텐 또는 루페올 100 mgSancho extract or Vergatten or
옥수수전분 100 mg
유당 100 mg
스테아린산 마그네슘 2 mgMagnesium stearate 2 mg
상기의 성분들을 혼합한 후 통상의 정제의 제조방법에 따라서 타정하여 정제를 제조한다.
After mixing the above components, tablets are prepared by tableting according to a conventional method for preparing tablets.
제제예Formulation example 3. 캅셀제의 제조 3. Preparation of capsules
산초 추출물 또는 베르갑텐 또는 루페올 100 mgSancho extract or Vergatten or
결정성 셀룰로오스 3 mgCrystalline cellulose 3 mg
락토오스 14.8 mgLactose 14.8 mg
마그네슘 스테아레이트 0.2 mgMagnesium stearate 0.2 mg
통상의 캡슐제 제조방법에 따라 상기의 성분을 혼합하고 젤라틴 캡슐에 충전하여 캡슐제를 제조한다.
The above components are mixed according to a conventional capsule preparation method and filled in gelatin capsules to prepare capsules.
제제예Formulation example 4. 주사제의 제조 4. Preparation of injections
산초 추출물 또는 베르갑텐 또는 루페올 100 mgSancho extract or Vergatten or
만니톨 180 mg180 mg mannitol
주사용 멸균 증류수 2974 mgSterile sterilized water for injection 2974 mg
Na2HPO4 ?2H2O 26 mgNa 2 HPO 4 ? 2H 2 O 26 mg
통상의 주사제의 제조방법에 따라 1 앰플당 (2 ml) 상기의 성분 함량으로 제조한다.
According to the conventional method for preparing an injection, the amount of the above ingredient is prepared per ampoule (2 ml).
제제예Formulation example 5. 5. 액제의Liquid 제조 Produce
산초 추출물 또는 베르갑텐 또는 루페올 100 mgSancho extract or Vergatten or
이성화당 10 g10 g per isomer
만니톨 5 g5 g mannitol
정제수 적량Purified water quantity
통상의 액제의 제조방법에 따라 정제수에 각각의 성분을 가하여 용해시키고 레몬향을 적량 가한 다음 상기의 성분을 혼합한 다음 정제수를 가하여 전체를 정제수를 가하여 전체 100 ml로 조절한 후 갈색병에 충진하여 멸균시켜 액제를 제조한다.
After dissolving each component in purified water according to the usual method of preparing a liquid solution, adding a proper amount of lemon aroma, and then mixing the above components, adding purified water and adjusting the whole to 100 ml by adding purified water and filling into a brown bottle. The solution is prepared by sterilization.
제제예Formulation example 6. 건강식품의 제조 6. Manufacture of health food
산초 추출물 또는 베르갑텐 또는 루페올 1 g1 g of pepper extract or bergapten or lufeol
비타민 혼합물 적량Vitamin mixture quantity
비타민 A 아세테이트 70 μg Vitamin A acetate 70 μg
비타민 E 1.0 mgVitamin E 1.0 mg
비타민 B1 0.13 mgVitamin B1 0.13 mg
비타민 B2 0.15 mgVitamin B2 0.15 mg
비타민 B6 0.5 mgVitamin B6 0.5 mg
비타민 B12 0.2 μg Vitamin B12 0.2 μg
비타민 C 10 mg
비오틴 10 μg Biotin 10 μg
니코틴산아미드 1.7 mgNicotinamide 1.7 mg
엽산 50 μg
판토텐산 칼슘 0.5 mgCalcium pantothenate 0.5 mg
무기질 혼합물 적량Mineral mixture
황산제1철 1.75 mgFerrous Sulfate 1.75 mg
산화아연 0.82 mgZinc Oxide 0.82 mg
탄산마그네슘 25.3 mgMagnesium carbonate 25.3 mg
제1인산칼륨 15 mg15 mg potassium monophosphate
제2인산칼슘 55 mgDicalcium Phosphate 55 mg
구연산칼륨 90 mgPotassium Citrate 90 mg
탄산칼슘 100 mg
염화마그네슘 24.8 mgMagnesium chloride 24.8 mg
상기의 비타민 및 미네랄 혼합물의 조성비는 비교적 건강식품에 적합한 성분을 바람직한 실시예로 혼합 조성하였지만, 그 배합비를 임의로 변형 실시하여도 무방하며, 통상의 건강식품 제조방법에 따라 상기의 성분을 혼합한 다음, 과립을 제조하고, 통상의 방법에 따라 건강식품 조성물 제조에 사용할 수 있다.
Although the composition ratio of the above-mentioned vitamin and mineral mixtures is mixed with a component suitable for a health food in a preferred embodiment, the compounding ratio may be arbitrarily modified. The granules may be prepared and used for preparing a health food composition according to a conventional method.
제제예Formulation example 7. 7. 건강음료의Health drink 제조 Produce
산초 추출물 또는 베르갑텐 또는 루페올 1 g1 g of pepper extract or bergapten or lufeol
비타민 C 15 g15 g of vitamin C
비타민 E(분말) 100 gVitamin E (powder) 100 g
젖산철 19.75 g19.75 g of ferrous lactate
산화아연 3.5 g3.5 g of zinc oxide
니코틴산아미드 3.5 gNicotinic acid amide 3.5 g
비타민 A 0.2 gVitamin A 0.2 g
비타민 B1 0.25 gVitamin B1 0.25 g
비타민 B2 0.3gVitamin B2 0.3g
물 정량Water quantification
통상의 건강음료 제조방법에 따라 상기의 성분을 혼합한 다음, 약 1시간 동안 85 ℃에서 교반 가열한 후, 만들어진 용액을 여과하여 멸균된 2 l 용기에 취득하여 밀봉 멸균한 뒤 냉장 보관한 다음 본 발명의 건강음료 조성물 제조에 사용한다.After mixing the above components according to the conventional healthy beverage production method, and stirred and heated at 85 ℃ for about 1 hour, the resulting solution is filtered and obtained in a sterilized 2 l container, sealed sterilization and refrigerated and then Used to prepare the healthy beverage composition of the invention.
상기 조성비는 비교적 기호음료에 적합한 성분을 바람직한 실시예로 혼합 조성하였지만 수요계층이나, 수요국가, 사용용도 등 지역적, 민족적 기호도에 따라서 그 배합비를 임의로 변형 실시하여도 무방하다.Although the compositional ratio is relatively mixed with a component suitable for a favorite drink, it is also possible to arbitrarily modify the compounding ratio according to the regional or national preference such as the demand class, the demanding country, and the use purpose.
Claims (10)
Antimicrobial composition against Helicobacter bacterium comprising an extract of Zanthoxylum schinifolium as an active ingredient.
The composition of claim 1, wherein the extract is extracted with an alcohol having 1 to 4 carbon atoms or a mixed solvent thereof.
According to claim 1, wherein the Helicobacter bacteria Helicobacter pylori (Helicobacter pylori), Helicobacter canis (Helicobacter canis), Helicobacter cinaedi, Helicobacter Heilmanii (Helicobacter heilmannii), Helicobacter bacilli Felis Helicobacter mustelae, Helicobacter fenelliae, Helicobacter raffini, Helicobacter hepaticus, Helicobacter billis (Helicobacter bilis) and Helicobacter pools Composition characterized in that the strain selected from the group.
Antimicrobial composition against Helicobacter bacterium comprising bergapten or lupeol as an active ingredient.
5. A composition according to claim 4, wherein the bergapten or lupeol is obtained from the herb.
A pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, which comprises an extract of the extract as an active ingredient.
The composition of claim 6, wherein the gastric and duodenal diseases are diseases selected from the group consisting of gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric adenocarcinoma, gastric lymphoma and gastric cancer caused by Helicobacter pylori.
A pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, including bergapten or lupeol as an active ingredient.
Health functional food for preventing and improving gastrointestinal and duodenal diseases, including bergapten or lupeol as an active ingredient.
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2017086572A1 (en) * | 2015-11-18 | 2017-05-26 | 차의과대학교 산학협력단 | Kimchi exhibiting preventive and therapeutic activity against helicobacter pylori caused disease |
JP2020029422A (en) * | 2018-08-23 | 2020-02-27 | 山本 芳栄 | Method for stabilizing sanshools |
-
2011
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2017086572A1 (en) * | 2015-11-18 | 2017-05-26 | 차의과대학교 산학협력단 | Kimchi exhibiting preventive and therapeutic activity against helicobacter pylori caused disease |
JP2020029422A (en) * | 2018-08-23 | 2020-02-27 | 山本 芳栄 | Method for stabilizing sanshools |
WO2020040315A1 (en) * | 2018-08-23 | 2020-02-27 | 山本 芳栄 | Method for stabilizing sanshool compound |
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