KR20190051578A - Composition for alalgesic comprising high functional Capsicum frutescens IT 221919 extract - Google Patents
Composition for alalgesic comprising high functional Capsicum frutescens IT 221919 extract Download PDFInfo
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- KR20190051578A KR20190051578A KR1020170147405A KR20170147405A KR20190051578A KR 20190051578 A KR20190051578 A KR 20190051578A KR 1020170147405 A KR1020170147405 A KR 1020170147405A KR 20170147405 A KR20170147405 A KR 20170147405A KR 20190051578 A KR20190051578 A KR 20190051578A
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Classifications
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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Abstract
Description
본 발명은 고기능성 고추 추출물을 유효성분으로 함유하는 진통제 조성물 및 통증 개선용 식품 조성물에 관한 것이다.The present invention relates to a painkiller composition and a food composition for pain relief which contain a high-functional pepper extract as an active ingredient.
고추는 다양한 비타민을 많이 함유하며 붉은색소와 매운맛을 함유해서 대표적인 양념채소로 자리 잡고 있다. 말린 붉은 고추의 단백질 지질 탄수화물 무기질, 비타민류의 함량은 대략 11%, 11%, 0.37%, 0.15%를 포함하고 있다. 이외에도 고추에는 플라보노이드 계열(비특허문헌 1)의 기능성 성분과 알칼로이드 계열의 기능성 성분들도 다량 포함하고 있는 것으로 알려져 있다. 이러한 기능성 효능으로는 비만[비특허문헌 2, 3]을 예방 해소하고 운동 시에 심폐 기능(비특허문헌 4)을 강화하며 성 호르몬 대사 기능[비특허문헌 5, 6]을 높여 정력을 증강하고 치매를 예방하는 것으로 알려져 있다. 최근의 연구결과에 따르면 치매의 예방 효과는 고추의 캡사이시노이드, 카로티노이드, 플라보노이드 등 다양한 항산화 성분을 기반으로 유해물질인 활성산소의 폐해를 막음으로써 항치매의 기능적 활성을 나타내는 것으로 보고되었다[비특허문헌 7]. 고추는 한방요법으로도 활용되었는데 한약재명은 번초, 당초, 고초 등으로 명명되며 한방에서 고추는 열을 내는 식품으로 심장, 혈관의 활동을 활발하게 하는 것으로 국소자극제로써 신경통, 근육통 등 외용으로 사용되며, 가벼운 동상, 복통, 어깨 결림 등에도 활용되었던 것으로 전해진다. Red pepper is rich in various vitamins, and contains red pigment and spicy taste. The content of protein lipid carbohydrate minerals and vitamins of dried red pepper contains approximately 11%, 11%, 0.37%, and 0.15%. In addition, it is known that red pepper also contains a large amount of functional components of flavonoid series (Non-Patent Document 1) and alkaloid series functional components. Such functional efficacy may include prevention of obesity (Non-Patent Documents 2 and 3), enhancement of cardiopulmonary function during exercise (non-patent document 4), enhancement of sexual hormone metabolism function (non-patent documents 5 and 6) It is known to prevent dementia. Recent studies have shown that the preventive effect of dementia is based on various antioxidant components such as capsaicinoids, carotenoids, and flavonoids of pepper, thereby preventing functional damage of active oxygen, which is a harmful substance, Patent Document 7]. Pepper is also used as a herbal medicine. The name of herbal medicinal herb is named as Gancho, originally called Gancho, and the hot pepper is a heat-stimulating food. It is used as external stimulant such as neuralgia and muscular pain as a local stimulant. It is said to have been used for light statues, abdominal pain, stiff shoulders.
현재 농촌진흥청에서는 고추의 형질 개선 및 신품종 개발을 위하여 유전적 다양성을 99% 이상 포함할 수 있는 핵심집단을 수집하고 보존하고 있다. 이러한 고추의 다양한 자원을 기반으로 고추의 농업적 생산량을 증대시킬 수 있는 연구 뿐 아니라 일상적인 섭취를 통하여 인간의 건강을 향상시키거나 다양한 질병으로부터 예방할 수 있는 고추의 기능성에 대한 연구가 필요하게 되었다. Currently, RDA is collecting and preserving core groups that can contain more than 99% of genetic diversity in order to improve the quality and develop new varieties of pepper. In addition to the research that can increase the agricultural production of pepper based on various resources of the pepper, it is necessary to study the function of the pepper which can improve the human health through daily ingestion or prevent various diseases.
이에, 본 발명자들은 국내에 다양한 고추 자원들 중 통증 완화에 탁월한 기능성을 나타내는 자원을 탐색 연구한 결과, IT 221919 고추 품종에 대한 TRPA1 억제능이 탁월한 효과를 확인함으로써 본 발명을 완성하게 되었다.Accordingly, the inventors of the present invention have searched out resources showing excellent functionality for pain relief among various pepper resources in Korea, and found out the excellent effect of TRPA1 inhibition on the
본 발명의 목적은 통증 완화에 탁월한 기능성을 나타내는 고추 IT 221919 추출물을 유효성분으로 포함하는 진통제 조성물을 제공하기 위한 것이다.It is an object of the present invention to provide an analgesic composition comprising, as an active ingredient, an extract of
본 발명의 다른 목적은 상기 고추 추출물을 유효성분으로 포함하는 통증 개선용 식품 조성물을 제공하기 위한 것이다.Another object of the present invention is to provide a food composition for improving pain comprising the extract of pepper as an active ingredient.
본 발명의 또 다른 목적은 상기 고추 추출물을 유효성분으로 포함하는 통증 개선용 건강기능식품을 제공하기 위한 것이다.It is still another object of the present invention to provide a health functional food for improving pain comprising the extract of pepper as an active ingredient.
상기의 과제를 해결하기 위한 수단으로서, 본 발명은 국립농업과학원 농업유전자원센터 IT번호 IT 221919의 고추 추출물을 유효성분으로 포함하는 진통제 조성물을 제공한다.As a means for solving the above-mentioned problems, the present invention provides an analgesic composition comprising, as an active ingredient, a red pepper extract of ITN
상기의 과제를 해결하기 위한 다른 수단으로서, 본 발명은 상기 고추 추출물을 유효성분으로 포함하는 통증 개선용 식품 조성물을 제공한다.As another means for solving the above problems, the present invention provides a food composition for improving pain comprising the extract of pepper as an active ingredient.
상기의 과제를 해결하기 위한 또 다른 수단으로서, 본 발명은 상기 고추 추출물을 유효성분으로 포함하는 통증 개선용 건강기능식품을 제공한다.As another means for solving the above problems, the present invention provides a health functional food for improving pain comprising the extract of pepper as an active ingredient.
본 발명에 따른 고기능성 고추(IT 221919) 추출물은 다른 계통 고추 추출물에 비해 오메가-하이드록시캡사이신(omega-hydroxycapsaicin), 호모캡사이신(homocapsaicin), 캡사이신(capsaicin), 디하이드로캡사이신(dihydrocapsaicin) 및 호모디하이드로캡사이신(homodihydrocapsaicin) 등의 캡사이신 유사체가 다량으로 포함되어 있어 TRPA1(Transient Receptor Potential A1) 억제능이 매우 우수하여 진통 효과가 탁월하다. 따라서, 본 발명은 천연물에서 유래한 우수한 진통제 조성물이라는 측면에서 그 의의가 있으며 이를 의약품 또는 건강기능식품의 제조를 위하여 이용될수 있으며 나아가 국민 건강에 기여할 수 있다.The high-performance red pepper (IT 221919) extract according to the present invention is superior to other systematic red pepper extracts in omega-hydroxycapsaicin, homocapsaicin, capsaicin, dihydrocapsaicin, And capsaicin analogues such as homodihydrocapsaicin are contained in a large amount, and TRPA1 (Transient Receptor Potential A1) is highly inhibited and excellent analgesic effect is excellent. Accordingly, the present invention has significance in that it is a superior analgesic composition derived from a natural product and can be used for the production of medicines or health functional foods, and further contributes to the public health.
도 1은 본 발명에 일 실시예에 따른 고추 시료 추출 및 전처리 과정을 나타낸 것이다.
도 2는 75점의 고추를 TRPA1 억제 소재 발굴을 위하여 고속 대량 스크리닝한 결과이다.
도 3은 고추 추출물 내에 함유되어 있는 5종의 유용성분들을 LC-MS를 이용하여 분석한 결과로, omega-hydroxycapsaicin과 homocapsaicin의 상대적 함량을 비교한 것이다.
도 4는 고추 추출물 내에 함유되어 있는 5종의 유용성분들을 LC-MS를 이용하여 분석한 결과로, capsaicin, dihydrocapsaicin 및 homodihydrocapsaicin의 상대적 함량을 비교한 것이다.1 shows a process of extracting a pepper sample and a preprocessing process according to an embodiment of the present invention.
FIG. 2 shows the result of high-speed mass screening of 75 peppers to find TRPA1 inhibitory material.
FIG. 3 is a graph comparing the relative contents of omega-hydroxycapsaicin and homocapsaicin as a result of LC-MS analysis of the five kinds of oil components contained in the pepper extract.
Figure 4 compares the relative content of capsaicin, dihydrocapsaicin, and homodihydrocapsaicin as a result of LC-MS analysis of the five oil soluble components contained in the pepper extract.
본 발명은 고기능성 고추 추출물을 유효성분으로 함유하는 진통제 조성물 및 이를 포함하는 통증 개선용 식품 조성물에 관한 것이다.The present invention relates to an analgesic composition containing a high-functional pepper extract as an active ingredient and a composition for improving pain comprising the same.
이하, 이를 보다 상세히 설명한다.Hereinafter, this will be described in more detail.
본 발명자들은 75종 계통이 다른 고추의 진통 활성을 확인하였으며, 유용성분의 함량을 분석함으로써 진통 효과가 탁월한 고기능성 고추를 선별하였다.The present inventors confirmed the analgesic activity of the other peppers in the 75 species, and analyzed the contents of the useful components to select the highly functional peppers having excellent analgesic effect.
본 발명에 기재된 “고기능성 고추”는 국립농업과학원 농업유전자원센터 IT번호 IT 221919 계통의 Capsicum frutescens이며, 일반 고추에 포함된 유용성분이 다량 함유되어 있는 고추를 의미한다. 상기 유용성분은 오메가-하이드록시캡사이신(omega-hydroxycapsaicin), 호모캡사이신(homocapsaicin), 캡사이신(capsaicin), 디하이드로캡사이신(dihydrocapsaicin), 호모디하이드로캡사이신(homodihydrocapsaicin) 등을 포함한다. 특히, 상기 오메가-하이드록시캡사이신(omega-hydroxycapsaicin)은 다른 고추 계통에 비해 60~70 배 높은 함량으로 포함된다. 상기 호모캡사이신(homocapsaicin)은 다른 고추 계통에 비해 20~30배 높은 함량으로 포함된다. 상기 캡사이신(capsaicin)은 다른 고추 계통에 비해 5~7배 높은 함량으로 포함된다. 상기 디하이드로캡사이신(dihydrocapsaicin)은 다른 고추 계통에 비해 4~6배 높은 함량으로 포함된다. 상기 호모디하이드로캡사이신(homodihydrocapsaicin)은 다른 고추 계통에 비해 7~10배 높은 함량으로 포함된다.&Quot; High-functioning red pepper " described in the present invention means Capsicum frutescens of the ITN
상기 고추 추출물은 고추를 물, 및 탄소수 1 내지 4의 알코올로 이루어진 군에서 선택된 1종 이상의 용매로 추출하여 얻어진 것일 수 있다. 구체예에 있어서, 상기 고추 추출물은 고추를 10 내지 95 %(v/v)의 탄소수 1 내지 4의 알코올, 바람직하게는 30 내지 70 %(v/v)의 메탄올로 추출하여 얻어진 것일 수 있다.The pepper extract may be obtained by extracting red pepper with at least one solvent selected from the group consisting of water and an alcohol having 1 to 4 carbon atoms. In an embodiment, the pepper extract may be obtained by extracting red pepper with 10 to 95% (v / v) alcohol having 1 to 4 carbon atoms, preferably 30 to 70% (v / v) methanol.
고추 내의 유효성분이 충분히 추출될 수 있도록, 상기 추출용매의 사용량은 고추 중량 기준으로 약 5 내지 50배, 바람직하게는 약 10 내지 20배일 수 있으며, 초음파 처리하여 추출한다.The amount of the extraction solvent used may be about 5 to 50 times, preferably about 10 to 20 times, based on the weight of the red pepper, so that the active ingredient in the red pepper can be sufficiently extracted.
본 발명의 조성물은 유효성분인 고추 추출물 외에, 영양제, 비타민, 전해질, 풍미제, 착색제, 중진제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산 음료에 사용되는 탄산화제 등을 추가로 함유할 수 있다. 상기 성분들은 독립적으로 또는 조합하여 추가될 수 있다. 상기 추가성분의 함량은 바람직하게는 상기 고추 추출물 100 중량부에 대하여 0.01 내지 100 중량부 범위에서 추가할 수 있으나, 이에 제한되는 것은 아니다.The composition of the present invention may contain, in addition to the pepper extract as an active ingredient, a nutrient, a vitamin, an electrolyte, a flavoring agent, a coloring agent, a thickening agent, a pectic acid and its salt, an alginic acid and its salt, an organic acid, a protective colloid thickener, Preservatives, glycerin, alcohols, carbonating agents used in carbonated beverages, and the like. The components can be added independently or in combination. The content of the additional ingredient may be added in the range of 0.01 to 100 parts by weight based on 100 parts by weight of the extract, but is not limited thereto.
상기 조성물 내의 상기 고추 추출물의 함량은 질환의 증상, 증상의 정도, 환자의 상태 등에 따라서 적절히 조절 가능하며, 예컨대, 전체 조성물 중량을 기준으로 0.0001 내지 99.9중량%, 바람직하게는 0.001 내지 50 중량%인 것이 좋으나, 이에 한정되는 것은 아니다. 상기 함량비는 용매를 제거한 건조량을 기준으로 한 값이다.The content of the capsicum extract in the composition may be appropriately adjusted depending on the symptom of the disease, the degree of symptoms, the condition of the patient and the like, for example, 0.0001 to 99.9% by weight, preferably 0.001 to 50% But is not limited thereto. The content ratio is a value based on the dried amount from which the solvent is removed.
상기 조성물은 약학적 조성물의 제조에 통상적으로 사용하는 적절한 담체, 부형제 및 희석제를 더 포함할 수 있으며, 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁액, 에멀젼, 시럽, 에어로졸 등의 경구형 제형, 외용제, 좌제 또는 멸균 주사용액 등의 형태로 제형화하여 사용될 수 있다. The composition may further contain an appropriate carrier, excipient and diluent conventionally used in the production of a pharmaceutical composition. The composition may be administered orally or parenterally in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, An external preparation, a suppository or a sterilized injection solution, and the like.
상기 조성물을 제제화할 경우에는 보통 사용하는 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제된다. 경구 투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형 제제는 적어도 한 가지 이상의 부형제 및/또는 윤활제 등을 포함할 수 있다. 경구 투여를 위한 액상 제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순희석제인 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, 좌제 등이 포함된다. When the composition is formulated, it is prepared using a diluent such as a filler, an extender, a binder, a wetting agent, a disintegrant, a surfactant, or an excipient usually used. Solid formulations for oral administration include tablets, pills, powders, granules, capsules, and the like, and such solid preparations may include at least one excipient and / or lubricant. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. Various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included in addition to water and liquid paraffin, which are simple diluents commonly used. have. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, freeze-dried preparations, suppositories, and the like.
상기 조성물의 바람직한 투여량은 환자의 상태 및 체중, 질병의 정도, 약물형태, 투여경로 및 기간에 따라 다르지만, 당업자에 의해 적절하게 선택될 수 있다. 보다 바람직한 효과를 위해서, 본 발명의 조성물의 투여량은 유효성분을 기준으로 1일 1 mg/kg 내지 100 mg/kg으로 하는 것이 좋으나 이에 제한되는 것은 아니다. 투여는 하루에 한번 투여할 수도 있고, 수회 나누어 투여할 수 있다. 본 발명의 조성물은 동물, 바람직하게는 인간을 포함하는 포유동물에 다양한 경로로 투여될 수 있다. 투여의 모든 방식은 예상될 수 있는데, 예를 들면, 경구, 정맥, 근육, 피하주사 등에 의해 투여될 수 있다. 본 발명의 조성물의 약학적 투여 형태는 유효성분의 약학적 허용 가능한 염의 형태로도 사용될 수 있고, 또한 단독으로 또는 타 약학적 활성 화합물과 결합뿐만 아니라 적당한 집합으로 사용될 수 있다.The preferred dosage of the composition varies depending on the condition and the weight of the patient, the degree of the disease, the drug form, the administration route and the period, but can be appropriately selected by those skilled in the art. For a more preferable effect, the dose of the composition of the present invention is preferably 1 mg / kg to 100 mg / kg per day based on the active ingredient, but is not limited thereto. The administration may be carried out once a day or divided into several doses. The compositions of the present invention may be administered to a mammal, including a human, in various ways. All modes of administration may be expected, for example, by oral, intravenous, intramuscular, subcutaneous injection, and the like. The pharmaceutical dosage form of the composition of the present invention may be used in the form of a pharmaceutically acceptable salt of the active ingredient, and may be used alone or in combination with other pharmaceutically active compounds as well as in a suitable combination.
또한, 본 발명은 상기 고추 추출물을 포함하는 통증 개선용 식품 조성물을 포함한다.In addition, the present invention includes a food composition for improving pain comprising the pepper extract.
본 발명에서 식품은 영양소를 한 가지 또는 그 이상 함유하고 있는 천연물 또는 가공품을 의미하며, 바람직하게는 어느 정도의 가공 공정을 거쳐 직접 먹을 수 있는 상태가 된 것을 의미하며, 통상적인 의미로서, 각종 식품, 건강기능 식품, 음료, 식품 첨가제 및 음료 첨가제를 모두 포함하는 의미로 사용된다. 상기 식품의 예로서 각종 식품류, 음료, 껌, 차, 비타민 복합제, 기능성 식품 등이 있다. 추가로, 본 발명에서 식품에는 특수영양식품(예, 조제유류, 영,유아식 등), 식육가공품, 어육제품, 두부류, 묵류, 면류(예, 라면류, 국수류 등), 건강보조식품, 조미식품(예, 간장, 된장, 고추장, 혼합장 등), 소스류, 과자류(예, 스넥류), 유가공품(예, 발효유, 치즈 등), 기타 가공식품, 김치, 절임식품(각종 김치류, 장아찌 등), 음료(예, 과실,채소류 음료, 두유류, 발효음료류, 아이스크림류 등), 천연조미료(예, 라면 스프 등), 비타민 복합제, 알코올 음료, 주류 및 그 밖의 건강보조식품류를 포함하나 이에 한정되지 않는다. 상기 건강기능식품, 음료, 식품첨가제 또는 음료첨가제는 통상의 제조방법으로 제조될 수 있다.In the present invention, the term " food " means a natural product or a processed product containing one or more nutrients, preferably a state of being able to be directly eaten through a certain processing step, , Health functional foods, beverages, food additives and beverage additives. Examples of the food include various foods, beverages, gums, tea, vitamin complex, and functional foods. In addition, in the present invention, the food may contain special nutritional foods (e.g., crude oil, spirits, infant food, etc.), meat products, fish products, tofu, jelly, noodles (Such as soy sauce, soybean paste, hot pepper paste, mixed sauce), sauces, confectionery (eg snacks), dairy products (eg fermented milk, cheese), other processed foods, kimchi, pickled foods But are not limited to, natural flavors (eg, ramen soup, etc.), vitamin complexes, alcoholic beverages, alcoholic beverages and other health supplement foods. The health functional food, beverage, food additive or beverage additive can be produced by a usual production method.
상기 식품 조성물은 식품학적으로 허용 가능한 식품 보조 첨가제를 포함할 수 있으며, 기능성 식품의 제조에 통상적으로 사용되는 적절한 담체, 부형제 및 희석제 등을 더욱 포함할 수 있다.The food composition may comprise a pharmaceutically acceptable food-aid additive and may further comprise suitable carriers, excipients and diluents conventionally used in the manufacture of functional foods.
또한, 상기 식품에 있어서, 상기 고추 추출물의 양은 전체 식품 중량의 0.00001 중량% 내지 50 중량%로 포함될 수 있으며, 상기 식품이 음료인 경우에는 식품 전체의 부피 100 ml 를 기준으로 0.001 g 내지 50 g, 바람직하게는 0.01 g 내지 10 g의 비율로 포함될 수 있으나, 이에 한정되는 것은 아니다.In addition, the amount of the pepper extract in the food may be 0.00001% to 50% by weight of the whole food. When the food is a beverage, the amount of the pepper extract is 0.001 to 50 g, Preferably 0.01 to 10 g, but is not limited thereto.
또한, 본 발명은 상기 고추 추출물을 유효성분으로 포함하는 건강기능식품을 포함한다.In addition, the present invention includes a health functional food containing the above-described capsicum extract as an active ingredient.
본 발명의 건강기능식품은 통증 개선의 목적으로, 정제, 캅셀, 분말, 과립, 액상, 환 등을 포함하지만 이에 한정하지 않는 형태로 제조 및 가공할 수 있다. 본 발명에서 사용된 용어 "건강기능식품"은 건강기능식품에 관한 법률 제6727호에 따른 인체에 유용한 기능성을 가진 원료나 성분을 사용하여 제조 및 가공한 식품을 말하며, 인체의 구조 및 기능에 대하여 영양소를 조절하거나 생리학적 작용 등과 같은 보건 용도에 유용한 효과를 얻을 목적으로 섭취하는 것을 의미한다.The health functional food of the present invention may be manufactured and processed for the purpose of improving pain, including but not limited to tablets, capsules, powders, granules, liquids, rings and the like. The term " health functional food " used in the present invention refers to foods prepared and processed using raw materials or ingredients having useful functions in accordance with Law No. 6727 on Health Functional Foods. It is meant to be ingested for the purpose of obtaining a beneficial effect for health use such as controlling nutrients or physiological action.
본 발명의 건강기능식품은 통상의 식품 첨가물을 포함할 수 있으며, 상기 "식품 첨가물"로서의 적합 여부는 다른 규정이 없는 한, 식품의약품안정청에 승인된 식품 첨가물 공전의 총칙 및 일반시험법 등에 따라 해당 품목에 관한 규격 및 기준에 의하여 판정한다.The health functional foods of the present invention may contain conventional food additives and, unless otherwise specified, whether or not they are suitable as the "food additives" may be used in accordance with the General Rules and General Test Methods approved by the Food and Drug Administration, It shall be judged according to standards and standards for items.
상기 "식품 첨가물 공전"에 수재된 품목으로는 예를 들어, 케톤류, 글리신, 구연산칼륨, 니코틴산, 계피산 등의 화학적 합성물, 감색소, 감초추출물, 결정셀룰로오스, 고량색소, 구아검 등의 천연첨가물, L-글루타민산나트륨 제제, 면류첨가알칼리제, 보존료제제, 타르색소제제 등의 혼합제제류 등을 들 수 있다.Examples of the substances found in the above-mentioned "food additives" include natural compounds such as ketones, chemical compounds such as glycine, potassium citrate, nicotinic acid and cinnamic acid, coloring pigments, licorice extracts, crystalline cellulose, high- L-glutamic acid sodium preparations, noodle-added alkalis, preservative preparations, tar coloring preparations and the like.
예를 들어, 정제 형태의 건강기능식품은 고추 추출물을 부형제, 결합제, 붕해제, 및 다른 첨가제와의 혼합물을 통상의 방법으로 과립화한 다음, 활택제 등을 넣어 압축 성형하거나, 상기 혼합물을 직접 압축 성형할 수 있다. 또한, 상기 정제 형태의 건강기능식품은 필요에 따라 교미제 등을 함유할 수 있으며, 필요에 따라 적당한 제피제로 제피할 수도 있다.For example, the health functional food in the form of tablets can be prepared by granulating a mixture of the extract of pepper with excipients, binders, disintegrants, and other additives by a conventional method, and then extruding the mixture with a lubricant or the like, Compression molding can be performed. The health functional food of the tablet form may contain a mating agent and the like if necessary, and may be sieved to a suitable skin care agent if necessary.
캅셀 형태의 건강기능식품 중 경질캅셀제는 통상의 경질캅셀에 고추 추출물을 부형제 등의 첨가제와의 혼합물 또는 그의 입상물 또는 제피한 입상물을 충진하여 제조할 수 있으며, 연질캅셀제는 고추 추출물을 부형제 등의 첨가제와의 혼합물을 젤라틴 등 캅셀기제에 충진하여 제조할 수 있다. 상기 연질캅셀제는 필요에 따라 글리세린 또는 소르비톨 등의 가소제, 착색제, 보존제 등을 함유할 수 있다.The hard capsule of the capsule type health functional food can be prepared by filling a common hard capsule with a mixture of the capsicum extract with an additive such as an excipient or a granular material thereof or a granular material with a scalpel and the soft capsules can be prepared by mixing the capsicum extract with an excipient, Of the present invention may be filled in a capsule base such as gelatin. The soft capsule may contain a plasticizer such as glycerin or sorbitol, a coloring agent, a preservative and the like, if necessary.
환 형태의 건강기능식품은 고추 추출물과 부형제, 결합제, 붕해제 등과의 혼합물을 적당한 방법으로 성형하여 조제할 수 있으며, 필요에 따라 백당이나 다른 적당한 제피제로 제피를, 또는 전분, 탈크 또는 적당한 물질로 환의를 입힐 수도 있다.The ring-shaped health functional food can be prepared by molding a mixture of pepper extract, excipient, binder, disintegrant and the like in an appropriate manner. If necessary, the preparation may be mixed with white sugar or other suitable skin care agent, or starch, talc or a suitable substance It is possible to make a ring.
과립형태의 건강기능식품은 상기 고추 추출물과 부형제, 결합제, 붕해제 등과의 혼합물을 적당한 방법으로 입상으로 제조할 수 있으며, 필요에 따라 착향제, 교미제 등을 함유할 수 있다.The granular health functional food may be prepared by granulating the mixture of the above-mentioned capsicum extract, excipient, binder, disintegrant and the like in a suitable manner and, if necessary, a flavoring agent, a mating agent and the like.
본 발명의 상기 부형제, 결합제, 붕해제, 활택제, 교미제, 착향제 등에 대한 용어 정의는 당업계에 공지된 문헌에 기재된 것으로 그 기능 등이 동일 내지 유사한 것들을 포함한다 (대한약전 해설편, 문성사, 한국약학대학협의회, 제 5 개정판, p33-48, 1989).The definitions of the excipients, binders, disintegrants, lubricants, mating agents, flavoring agents and the like of the present invention are described in documents known in the art and include the same or similar functions (see, for example, Korean Association of Pharmacy, 5th ed., Pp. 33-48, 1989).
이하, 실시예를 통하여 본 발명의 구성 및 효과를 더욱 상세히 설명하고자 한다. 이들 실시예는 오로지 본 발명을 예시하기 위한 것일 뿐, 본 발명의 범위가 이들 실시예에 의해 한정되는 것은 아니다.Hereinafter, the constitution and effects of the present invention will be described in more detail through examples. These examples are only for illustrating the present invention, and the scope of the present invention is not limited by these examples.
실시예Example 1: 고추 추출물 제조 1: Preparation of pepper extract
1) 고추 재료 준비1) Preparation of red pepper material
본 발명세서 사용된 고추재료는 차세대바이오그린21사업 농생물게놈활용연구사업단에서 현재 진행 중인 고추 과제와 연계하여 2015년도에 수확된 연구재료를 제공받아 활용하였다. 고추재료의 세부정보는 국립농업유전자원센터에서 운영하는 농업생명자원서비스(http://genebank.rda.go.kr/)에서 확인할 수 있으며, 검색 뿐 아니라 분양 신청도 가능하다.The pepper material used in the present invention was obtained by utilizing the research material harvested in 2015 in connection with the ongoing pepper task in the next generation BioGreen 21 business genome utilization research institute. Details of the red pepper ingredients can be found in the Agriculture and Life Resources Service (http://genebank.rda.go.kr/) operated by the National Center for Agricultural Genetic Resources.
상기 표 1의 75계통 고추 재료를 준비하였다. The 75 series pepper material of Table 1 was prepared.
2) 고추 추출물 제조2) Preparation of pepper extract
동결건조된 75계통 각각의 고추 핵심집단 과실을 그라인더로 분쇄하여 미세하게 분말화하였고, 입자 크기의 표준화 과정을 거치지 않고 기능성 평가와 성분 분석을 위한 추출과정을 진행하였다. 고추 분말 시료를 0.5 g씩 vial에 넣고, 1 g/10 mL의 농도로 70% MeOH을 첨가한 후 30분 동안 2회 초음파 처리를 하여 대사물질들을 추출하였다. 이후 1,000 rpm에서 5분 동안 원심분리한 후 상등액을 0.45 um syringe filter를 이용하여 여과하여 무게를 측정한 새로운 vial에 옮긴 후 질소농축기로 농축하여 완전히 수분을 제거하였다. 농축된 시료는 40 mg/mL의 농도로 DMSO에 재용해하였고, 0.2 um syringe filter를 이용하여 여과 후 활성 분석과 성분 분석을 수행하였다(도 1). The main fruit of each group of 75 freeze - dried chilli was pulverized by a grinder and finely pulverized. The extraction process for functional evaluation and component analysis was carried out without the standardization process of particle size. Each 0.5 g of red pepper powder was put into a vial, and 70% MeOH was added at a concentration of 1 g / 10 mL. Then, the metabolites were extracted by ultrasonication twice for 30 minutes. After centrifugation at 1,000 rpm for 5 minutes, the supernatant was filtered through a 0.45 μm syringe filter and transferred to a new vial, which was weighed. The filtrate was concentrated with a nitrogen concentrator to completely remove water. Concentrated samples were redissolved in DMSO at a concentration of 40 mg / mL, and analyzed by a 0.2 μm syringe filter for activity and composition analysis (FIG. 1).
성분 분석용 시료는 100% MeOH을 이용하여 5 mg/mL 농도로 희석하여 사용하였다. Samples for component analysis were diluted to a concentration of 5 mg / mL using 100% MeOH.
실시예Example 2: 고속 대량 스크리닝을 이용한 2: Using high-speed bulk screening TRPA1TRPA1 억제 소재 탐색 Explore Suppress Material
신경세포, 피부, 호흡기관, 신장 등 다양한 조직에서 발현되는 양이온 채널인 TRP A1(Transient Receptor Potential A1)은 외부 자극 및 화학적 자극원에 의해 활성화되어 양이온을 세포 내로 유입시킴으로써 세포를 자극시키는 수용체이다. TRPA1을 발현하는 안정세포주와 Ca2 +에 결합하는 Fluo-4 DirectTM를 이용하여 자극원에 의한 TRPA1의 활성을 저해하는 소재를 발굴하기 위하여 고속 대량 스크리닝을 수행하였다. TRP A1 (Transient Receptor Potential A1), a cation channel expressed in various tissues such as neurons, skin, respiratory organs and kidneys, is activated by external stimuli and chemical stimulants to stimulate cells by introducing cations into cells. Was performed to high-speed mass-screening using the Fluo-4 TRPA1 Direct TM binding to stable cell lines expressing the Ca 2 + to identify materials which inhibit the activity of TRPA1 by irritants.
96 well black clear plate에 TRPA1 H10 세포(경기과학기술진흥원에서 자체 제작한 TRP A1 억제소제 대량 검색을 위한 안정세포주)를 4 X 104 cells/well, 100 ㎕를 깔고 상온에서 1,000 rpm으로 1분 동안 원심분리해준 뒤 37℃, 5% CO2 인큐베이터에서 48시간 동안 배양하였다[배지: DMEM, 10% FBS, 1% Penicillin-Streptomycin, 500 ㎍/㎖ G418]. TRPA1 H10 cells (stable cell line for large-scale screening of TRP A1 inhibitor) manufactured by Gyeonggi Science and Technology Agency were placed on a 96-well black clear plate at 100 rpm at 4 x 10 4 cells / well. After centrifugation, the cells were cultured in a 5% CO 2 incubator at 37 ° C for 48 hours (medium: DMEM, 10% FBS, 1% Penicillin-Streptomycin, 500 μg / ml G418).
Fluo-4 DirectTM Calcium assay kit(Thermo Fisher Scientific F10472)에 포함되어 있는 Probenecid (Component B) 77mg 1vial에 Fluo-4 DirectTM Calcium assay buffer(Component C) 1㎖ 넣고, Vortex해서 잘 섞어주었다(최종 농도 250 mM probenecid). 1 ml of Fluo-4 Direct ™ Calcium Assay Buffer (Component C) was added to 77 mg of 1 mg of Probenecid (Component B) contained in Fluo-4 Direct ™ Calcium Assay Kit (Thermo Fisher Scientific F10472), vortexed and mixed well 250 mM probenecid).
Fluo-4 DirectTM Calcium assay Reagent(Component A)에 10 ㎖의 Fluo-4 DirectTM Calcium assay buffer(Component C)와 200 ㎕의 250 mM Probenecid(Component B)를 넣어준 뒤, 잘 섞은 후(2 X Fluo-4 Direct TM calcium reagent), 세포에 2 X Fluo-4 Direct TM calcium reagent를 100 ㎕씩 넣고, 37℃ 인큐베이터에서 1시간 동안 반응시켰다. Add 10 μl of Fluo-4 Direct ™ Calcium Assay Buffer (Component C) and 200 μl of 250 mM Probenecid (Component B) to Fluo-4 Direct ™ Calcium Assay Reagent (Component A) Fluo-4 Direct TM calcium reagent), 100 μl of 2 × Fluo-4 Direct ™ calcium reagent was added to the cells, and reacted in a 37 ° C. incubator for 1 hour.
Agonist의 효과를 확인하기 위하여 Polygodial을 이용하여 Calcium assay를 수행하였고, flexstation의 Calcium assay protocol [fluorescence at EX. 495 nm /Em. 516, 140s read, 67번 read, 25s agonist 25㎕ injection (Flexstation)]을 이용하여 측정하였다. Calcium assay was performed using polygodial to confirm the effect of agonist. Calcium assay protocol [fluorescence at EX. 495 nm / Em. 516, 140s read, 67 read, 25s agonist 25l injection (Flexstation)].
상기에서 사용한 모든 시약 및 프로토콜은 Thermo Fisher Scientific사의 카달로그 번호 F10472인 Fluo-4 DirectTM Calcium assay kit 제품 내에 포함된 시약들과 실험방법에 따라 사용하였다. All of the reagents and protocols used above were used according to the reagents and experimental methods contained in the Fluo-4 Direct ™ Calcium Assay kit product, Thermo Fisher Scientific's catalog number F10472.
총 75계통의 고추 추출물을 이용하여 TRPA1 억제 정도를 측정한 결과, 0 ~ 54.4% 범위의 저해율을 나타냈고, 이중 IT 221919 고추 계통에서 가장 높은 저해 활성을 확인할 수 있었다. 분석한 고추 추출액 75점에 대한 TRPA1 저해율 평균과 표준편차는 11.3±10.9%로 나타났고, 가장 활성이 우수한 IT 221919 계통은 전체 평균치 보다 약 43% 이상의 강화된 진통 활성이 있음을 보여주었다. Total inhibition of TRPA1 inhibition was obtained in 75 systematic pepper extracts. The highest inhibitory activity was observed in
실시예 3: 고추 추출물 유용성분 5종의 LC-MS 분석Example 3: LC-MS analysis of five kinds of useful components of pepper extract
고추 추출물 내에 함유되어 있는 5종의 유용성분들(오메가-하이드록시캡사이신(omega-hydroxycapsaicin), 호모캡사이신(homocapsaicin), 캡사이신(capsaicin), 디하이드로캡사이신(dihydrocapsaicin) 및 호모디하이드로캡사이신(homodihydrocapsaicin))을 LC-MS를 이용하여 다음과 같이 분석하였다.The five oil soluble components (omega-hydroxycapsaicin, homocapsaicin, capsaicin, dihydrocapsaicin and homodihydrocapsaicin) contained in the capsicum extract were identified as LC-MS analysis was performed as follows.
- 분석 장비: Nexera X2 UHPLC (Shimadzu)- Analytical equipment: Nexera X2 UHPLC (Shimadzu)
Q-TOF-MS (TripleTOF 5600+system, AB SCIEX)Q-TOF-MS (TripleTOF 5600 + system, AB SCIEX)
- 분석 칼럼: Shim-pack GIS-ODS column (3μm, 3.0×100 mm) Analysis Column: Shim-pack GIS-ODS column (3 占 퐉, 3.0 占 100 mm)
- 검출기 : Diode-array detector (DAD) & MS detector - Detector: Diode-array detector (DAD) & MS detector
- 용매 조건: 이동상 A - 0.1% formic acid in water- Solvent conditions: mobile phase A - 0.1% formic acid in water
·이동상 B - 0.1% formic acid in 100% acetonitrile · Mobile phase B - 0.1% formic acid in 100% acetonitrile
- UHPLC 분석 조건: - UHPLC analysis conditions:
- Q-TOF/MS 분석 조건 : - Q-TOF / MS analysis conditions:
고추 추출물 내에 함유되어 있는 5종의 유용성분들을 LC-MS를 이용하여 분석한 결과를 도 3 및 도 4에 나타내었다. The results of analyzing the five kinds of useful components contained in the capsicum extract using LC-MS are shown in FIG. 3 and FIG.
계통들 내 함유되어 있는 capsaicin, dihydrocapsaicin 및 homodihydrocapsaicin의 함량 분포는 일정한 패턴을 보이는 것을 확인할 수 있었다. 하지만 IT 221919 계통의 경우 capsaicin과 dihydrocapsaicin 성분은 매운 맛이 강한 일부 고추들과 큰 함량 차이를 보여주지 않은 반면에 omega-hydroxycapsaicin과 homocapsaicin 함량은 다른 계통들과 비교하였을 때 월등히 높은 경향을 보여주었다. 고추 계통 IT 221919는 omega-hydroxycapsaicin의 함유량에서 나머지 74계통 분석 결과의 평균값과 비교하였을 경우 약 68.4배 정도로 높은 피크 면적 값을 나타냈고, homocapsaicin 성분에서도 27.4배 정도로 높은 수치를 보여주었다. 반면에 capsaicin, dihydrocapsaicin, homodihydrocapsaicin의 경우에는 IT 221919 제외 74계통의 평균치에 비해 각각 5.7배, 5.0배, 8.6배 높음을 확인할 수 있었다. The contents of capsaicin, dihydrocapsaicin, and homodihydrocapsaicin in the strains showed a uniform pattern. However, in the
따라서 본 발명에서 사용된 고추 IT 221919 계통의 추출물은 다른 계통에 비해 omega-hydroxycapsaicin, homocapsaicin, homodihydrocapsaicin, capsaicin 및 dihydrocapsaicin의 함량이 더 높은 것으로 나타났다. Therefore, the extracts of the
Claims (11)
An analgesic composition comprising pepper extract of IT No. IT 221919 as an active ingredient.
상기 추출물은 물 및 탄소수 1 내지 4의 알코올로 이루어진 군에서 선택된 1종 이상의 용매로 추출하여 얻어진 것인, 진통제 조성물.
The method according to claim 1,
Wherein the extract is obtained by extraction with at least one solvent selected from the group consisting of water and an alcohol having 1 to 4 carbon atoms.
상기 고추 추출물은 고추를 10 내지 95 %(v/v) 메탄올로 추출하여 얻어진 것인, 진통제 조성물.
The method according to claim 1,
Wherein the pepper extract is obtained by extracting pepper with 10 to 95% (v / v) methanol.
상기 고추 추출물은 오메가-하이드록시캡사이신(omega-hydroxycapsaicin), 호모캡사이신(homocapsaicin), 캡사이신(capsaicin), 디하이드로캡사이신(dihydrocapsaicin) 및 호모디하이드로캡사이신(homodihydrocapsaicin)로 이루어진 군에서 선택된 하나 이상이 다량 포함된 것인, 진통제 조성물.
The method according to claim 1,
The pepper extract contains a large amount of at least one selected from the group consisting of omega-hydroxycapsaicin, homocapsaicin, capsaicin, dihydrocapsaicin, and homodihydrocapsaicin. ≪ / RTI >
상기 오메가-하이드록시캡사이신(omega-hydroxycapsaicin)은 다른 고추 계통에 비해 60~70 배 높은 함량으로 포함된 것인, 진통제 조성물.
5. The method of claim 4,
Wherein the omega-hydroxycapsaicin is contained at a 60- to 70-fold higher content than other pepper systems.
상기 호모캡사이신(homocapsaicin)은 다른 고추 계통에 비해 20~30배 높은 함량으로 포함된 것인, 진통제 조성물.
5. The method of claim 4,
Wherein the homocapsaicin is included in an amount 20 to 30 times higher than the other pepper line.
상기 캡사이신(capsaicin)은 다른 고추 계통에 비해 5~7배 높은 함량으로 포함된 것인, 진통제 조성물.
5. The method of claim 4,
Wherein the capsaicin is included at a 5 to 7-fold higher content than the other pepper line.
상기 디하이드로캡사이신(dihydrocapsaicin)은 다른 고추 계통에 비해 4~6배 높은 함량으로 포함된 것인, 진통제 조성물.
5. The method of claim 4,
Wherein the dihydrocapsaicin is contained in a content 4- to 6-fold higher than other pepper systems.
상기 호모디하이드로캡사이신(homodihydrocapsaicin)은 다른 고추 계통에 비해 7~10배 높은 함량으로 포함된 것인, 진통제 조성물.
5. The method of claim 4,
Wherein the homodihydrocapsaicin is included in a content 7 to 10 times higher than other pepper systems.
A food composition for pain relief comprising pepper extract of IT No. IT 221919 as an active ingredient.
A health functional food for pain relief containing pepper extract of IT No. IT 221919 as an active ingredient.
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