KR20230089824A - Composition for anti-obesity - Google Patents
Composition for anti-obesity Download PDFInfo
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- KR20230089824A KR20230089824A KR1020210178531A KR20210178531A KR20230089824A KR 20230089824 A KR20230089824 A KR 20230089824A KR 1020210178531 A KR1020210178531 A KR 1020210178531A KR 20210178531 A KR20210178531 A KR 20210178531A KR 20230089824 A KR20230089824 A KR 20230089824A
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- obesity
- acid
- composition
- health food
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Abstract
본 발명은 항비만용 조성물에 관한 것으로, 보다 상세하게는 카프타르산(Caftaric acid) 또는 이의 약학적 또는 식품학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 건강식품 조성물 및 약학 조성물을 제공한다.
상기 조성물은 지방전구세포의 지방세포로의 분화를 억제하여 지방구(lipid droplet) 생성을 억제하거나 이의 분해를 촉진함으로써 우수한 항비만 활성을 보이는 바, 이를 활용하여 보다 안전하고 효과적으로 비만 또는 비만 관련 질환을 예방, 개선 또는 치료할 수 있다.The present invention relates to a composition for anti-obesity, and more particularly, to provide a health food composition and pharmaceutical composition for anti-obesity containing caftaric acid or a pharmaceutically or food-acceptable salt thereof as an active ingredient. do.
The composition exhibits excellent anti-obesity activity by suppressing the differentiation of preadipocytes into adipocytes, thereby suppressing the production of lipid droplets or promoting their decomposition, and by using this composition, obesity or obesity-related diseases are more safely and effectively treated. It can be prevented, ameliorated or cured.
Description
본 발명은 항비만용 조성물에 관한 것으로, 보다 상세하게는 카프타르산(Caftaric acid) 또는 이의 약학적 또는 식품학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 건강식품 조성물 및 약학 조성물에 관한 것이다.The present invention relates to a composition for anti-obesity, and more particularly, to a health food composition and pharmaceutical composition for anti-obesity containing caftaric acid or a pharmaceutically or food-acceptable salt thereof as an active ingredient. will be.
최근 제약업계가 비만치료제 개발에 적극적으로 달려들고 있다. 국내는 물론, 세계적으로 비만 인구가 계속해서 증가하고 있는 데다 과거와 달리 비만을 질환으로 인식해 의약품을 복용하는 환자가 늘어나면서 관련 시장에 대한 기대감이 높아지고 있어서다. 세계보건기구는 글로벌 비만 치료제 시장이 2016년 11억 달러(1조260억 원)에서 연평균 32.8%씩 성장해 2027년 241억 달러(한화 27조 원)으로 확대될 것으로 전망하고 있다.Recently, the pharmaceutical industry is actively working on the development of obesity treatment drugs. As the number of obese people continues to increase both domestically and globally, and as the number of patients who recognize obesity as a disease and take medicines is increasing, expectations for the related market are rising. The World Health Organization predicts that the global obesity treatment market will expand from 1.1 billion dollars (1.26 trillion won) in 2016 to 24.1 billion dollars (27 trillion won) in 2027, growing at an average annual rate of 32.8%.
비만(obesity)은 체내에 지방 조직이 과다한 상태로, 에너지 소비량에 비해 영양소를 과다 섭취할 경우 에너지 불균형에 의해 비만이 유발된다. 유전적으로 특정 유전자의 돌연변이에 의해 식욕 조절 중추 기능에 문제가 있거나, 쿠싱증후군과 같은 내분비 질환, 식욕을 증가시키는 다양한 약제에 의해 발생하는 경우도 있으나, 일반적으로는 에너지 섭취량이 에너지 소비량보다 커서 발생한다. 일반적인 비만의 경우 유전적 영향 및 환경적 영향이 복합적으로 작용하여 발생한다. 특히 칼로리가 높은 식품이 풍부하고 신체 활동을 덜 해도 사는데 불편이 없는 현대의 생활환경이 비만의 폭발적 증가를 초래하고 있다. Obesity is a state in which adipose tissue is excessive in the body, and obesity is induced by energy imbalance when nutrients are excessively consumed compared to energy consumption. In some cases, it may be caused by a genetic mutation in a specific gene, a problem with the appetite control center function, an endocrine disease such as Cushing's syndrome, or various drugs that increase appetite, but in general, energy intake is greater than energy consumption. . General obesity is caused by a combination of genetic and environmental influences. In particular, the modern living environment in which high-calorie foods are abundant and there is no inconvenience in living even with less physical activity is causing an explosive increase in obesity.
또한, 비만은 당뇨병, 순환기계 질환, 암 등 각종 질환의 발생 가능성을 증가시키는 위험 요소다. 국민 건강을 위협할 뿐만 아니라, 이로 인한 막대한 사회적 비용 지출을 초래해 국가 경쟁력에 타격을 주는 심각한 문제로 인식되고 있다.In addition, obesity is a risk factor that increases the possibility of various diseases such as diabetes, circulatory system disease, and cancer. It is recognized as a serious problem that not only threatens public health, but also causes enormous social costs and damages national competitiveness.
현재 이러한 비만치료제로는 식욕억제제, 체열발생제, 이뇨제 등이 사용되고 있다. 이 중 가장 많이 사용되는 식욕억제제는 뇌의 시상하부에 작용하여 식욕 억제로 인한 체중 감량 효과를 나타내는 작용 기전을 가지고 있으며, 이들 대부분은 중추 신경 흥분을 유발시켜 이의 작용을 유발하는 것으로 알려져 있다. 그러나 이들 대부분의 식욕억제제의 경우, 식욕억제 능력이 지속되지 못하고 일시적인 작용으로 두통, 불면증, 혈압상승, 초조, 긴장감, 환각 증세, 현기증, 시력 저하 등의 부작용을 유발시키는 문제점이 있다. 또한 일부 식욕억제제는 정신적, 신체적 의존성이 있는 것으로 알려져 있다. 따라서, 보다 안전하게 항비만 효과를 달성할 수 있는 기술 개발이 필요한 실정이다. Appetite suppressants, thermogenics, diuretics and the like are currently being used as such anti-obesity drugs. Among them, the most commonly used appetite suppressants act on the hypothalamus of the brain to have a mechanism of action that exhibits a weight loss effect due to appetite suppression, and most of them are known to induce central nervous stimulation to induce their action. However, in the case of most of these appetite suppressants, the ability to suppress appetite is not sustained and there is a problem of causing side effects such as headache, insomnia, blood pressure increase, nervousness, nervousness, hallucination symptoms, dizziness, and blurred vision due to temporary action. It is also known that some appetite suppressants have psychological and physical dependence. Therefore, it is necessary to develop a technology that can more safely achieve the anti-obesity effect.
본 발명의 목적은 안전하고 항비만 효과가 우수한 조성물을 제공하는 데에 있다.An object of the present invention is to provide a composition that is safe and has excellent anti-obesity effects.
상기의 목적을 달성하기 위하여, 본 발명은 하기 화학식 1로 표시되는 화합물 또는 이의 식품학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 건강식품 조성물을 제공한다.In order to achieve the above object, the present invention provides a health food composition for anti-obesity containing a compound represented by Formula 1 below or a pharmaceutically acceptable salt thereof as an active ingredient.
상기 화합물 또는 이의 식품학적으로 허용가능한 염은 지방전구세포의 지방세포로의 분화를 억제하여 지방구(lipid droplet) 생성을 억제하거나 이의 분해를 촉진할 수 있다.The compound or a food-acceptable salt thereof may inhibit the differentiation of pre-adipocytes into adipocytes, thereby suppressing the production of lipid droplets or promoting their decomposition.
상기 화합물 또는 이의 식품학적으로 허용가능한 염은 건강식품 조성물 전체 100 중량부에 대하여, 0.01 내지 1 중량부 함유될 수 있다.The compound or a food chemically acceptable salt thereof may be contained in an amount of 0.01 to 1 part by weight based on 100 parts by weight of the total health food composition.
상기 건강식품 조성물은 분말, 과립, 정제, 캡슐, 젤리, 시럽 또는 음료 형태일 수 있다.The health food composition may be in the form of a powder, granule, tablet, capsule, jelly, syrup or beverage.
또한, 본 발명은 하기 화학식 1로 표시되는 화합물 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 약학 조성물을 제공한다.In addition, the present invention provides a pharmaceutical composition for anti-obesity containing a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.
<화학식 1><
본 발명에 따른 조성물은 지방전구세포의 지방세포로의 분화를 억제하여 지방구(lipid droplet) 생성을 억제하거나 이의 분해를 촉진함으로써 우수한 항비만 활성을 가지는 바, 이를 건강식품 또는 약학 조성물로 활용하여 보다 안전하고 효과적으로 비만 또는 비만 관련 질환을 예방, 개선 또는 치료할 수 있다. The composition according to the present invention suppresses the differentiation of pre-adipocytes into adipocytes to suppress the production of lipid droplets or promote their decomposition, thereby having excellent anti-obesity activity. Obesity or obesity-related diseases can be safely and effectively prevented, ameliorated or treated.
도 1은 본 발명의 일 실시예에 따라 고성능액체크로마토그래피로 분석한 크로마토그램을 나타낸 것이다.
도 2는 농도에 따른 카프타르산의 표준 곡선을 나타낸 것이다.
도 3은 본 발명의 일 실험예에 따른 지방전구세포(3T3-L1)의 세포 독성을 분석한 그래프이다.
도 4는 본 발명의 일 실험예에 따른 오일 레드 O 염색 결과를 나타낸 것이다.
도 5는 도 4의 오일 레드 O 시약을 용출시켜 흡광도를 측정한 그래프이다.1 shows a chromatogram analyzed by high-performance liquid chromatography according to an embodiment of the present invention.
Figure 2 shows a standard curve of caftaric acid as a function of concentration.
3 is a graph analyzing the cytotoxicity of preadipocytes (3T3-L1) according to an experimental example of the present invention.
Figure 4 shows the results of Oil Red O staining according to an experimental example of the present invention.
5 is a graph obtained by measuring absorbance by eluting the Oil Red O reagent of FIG. 4 .
이하, 본 발명을 상세하게 설명하기로 한다.Hereinafter, the present invention will be described in detail.
본 발명에서 사용되는 용어는 본 발명에서의 기능을 고려하면서 가능한 현재 널리 사용되는 일반적인 용어들을 선택하였으나, 이는 당 분야에 종사하는 기술자의 의도 또는 판례, 새로운 기술의 출현 등에 따라 달라질 수 있다. 따라서 본 발명에서 사용되는 용어는 단순한 용어의 명칭이 아닌, 그 용어가 가지는 의미와 본 발명의 전반에 걸친 내용을 토대로 정의되어야 한다.The terms used in the present invention have been selected from general terms that are currently widely used as much as possible while considering the functions in the present invention, but these may vary depending on the intention of a person skilled in the art or precedent, the emergence of new technologies, and the like. Therefore, the term used in the present invention should be defined based on the meaning of the term and the overall content of the present invention, not simply the name of the term.
명세서 전체에서 어떤 부분이 어떤 구성요소를 "포함"한다고 할 때, 이는 특별히 반대되는 기재가 없는 한 다른 구성요소를 제외하는 것이 아니라 다른 구성요소를 더 포함할 수 있음을 의미한다.When it is said that a certain part "includes" a certain component throughout the specification, it means that it may further include other components without excluding other components unless otherwise stated.
본 발명은 하기 화학식 1로 표시되는 화합물 또는 이의 약학적 또는 식품학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 조성물을 제공한다.The present invention provides an anti-obesity composition containing a compound represented by the following formula (1) or a pharmaceutically or food-acceptable salt thereof as an active ingredient.
<화학식 1><
상기 화합물은 비-플라보노이드 페놀 화합물로, (2R,3R)-2-{[(2E)-3-(3,4-디하이드록시페닐)프로프-2-에노일]옥시}-3-하이드록시부탄디오익산{(2R,3R)-2-{[(2E)-3-(3,4-Dihydroxyphenyl)prop-2-enoyl]oxy}-3-hydroxybutanedioic acid}으로 명명될 수 있고, 또는 카프타르산(Caftaric acid)이라 명명될 수 있다.The compound is a non-flavonoid phenolic compound, (2R,3R)-2-{[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy}-3-hydroxy It can be named as hydroxybutanedioic acid {(2R,3R)-2-{[(2E)-3-(3,4-Dihydroxyphenyl)prop-2-enoyl]oxy}-3-hydroxybutanedioic acid}, or It can be named as caftaric acid.
상기 화합물은 이와 동일한 효능을 갖는 범위 내에서 약학적 또는 식품학적으로 허용가능한 염의 형태로 사용될 수 있다.The compound may be used in the form of a pharmaceutically or food-acceptable salt within the scope of having the same efficacy.
본 명세서에서, "약학적 또는 식품학적으로 허용가능한"이란, 상기 조성물에 노출되는 세포나 인간에게 독성이 없는 것을 의미한다.In the present specification, "pharmaceutically or food-gradely acceptable" means that the composition is not toxic to cells or humans exposed to the composition.
상기 염은 약학적 또는 식품학적으로 허용가능한 염기성 염 또는 산성염 중 어느 하나의 형태로 사용할 수 있다. 염기성염은 유기 염기염, 무기 염기염 중 어느 하나의 형태로 사용할 수 있으며, 나트륨염, 칼륨염, 칼슘염, 리튬염, 마그네슘염, 세슘염, 아미늄염, 암모늄염, 트리에칠아미늄염 및 피리디늄염으로 이루어진 군에서 선택될 수 있다.The salt may be used in the form of any one of a pharmaceutically or food-acceptable basic salt or an acidic salt. The basic salt can be used in the form of any one of an organic basic salt and an inorganic basic salt, and includes sodium salt, potassium salt, calcium salt, lithium salt, magnesium salt, cesium salt, aminium salt, ammonium salt, triethylaminium salt, and pyrol. It may be selected from the group consisting of dinium salts.
산성염은 유리산(free acid)에 의해 형성된 산부가염이 유용하다. 유리산으로는 무기산과 유기산을 사용할 수 있으며, 무기산으로는 염산, 브롬산, 황산, 아황산, 인산, 이중 인산, 질산 등을 사용할 수 있고, 유기산으로는 구연산, 초산, 말레산, 말산, 퓨마르산, 글루코산, 메탄설폰산, 벤젠설폰산, 캠퍼설폰산, 옥살산, 말론산, 글루타릭산, 아세트산, 글리콘산, 석신산, 타타르산, 4-톨루엔설폰산, 갈락투론산, 엠본산, 글루탐산, 시트르산, 아스파르탄산, 스테아르산 등을 사용할 수 있으나, 이에 제한되지 않고 당업계에서 통상적으로 사용되는 다양한 무기산 및 유기산을 이용하여 형성되는 염이 모두 포함될 수 있다.As the acid salt, an acid addition salt formed by a free acid is useful. Inorganic acids and organic acids can be used as free acids, and hydrochloric acid, hydrobromic acid, sulfuric acid, sulfurous acid, phosphoric acid, double phosphoric acid, and nitric acid can be used as inorganic acids, and citric acid, acetic acid, maleic acid, malic acid, and fumaric acid can be used as organic acids. , glucoic acid, methanesulfonic acid, benzenesulfonic acid, camphorsulfonic acid, oxalic acid, malonic acid, glutaric acid, acetic acid, glycolic acid, succinic acid, tartaric acid, 4-toluenesulfonic acid, galacturonic acid, embonic acid, Glutamic acid, citric acid, aspartic acid, stearic acid, etc. may be used, but are not limited thereto, and salts formed using various inorganic acids and organic acids commonly used in the art may all be included.
또한, 상기 화합물은 약학적 또는 식품학적으로 허용되는 염뿐만 아니라, 통상의 방법에 의해 제조될 수 있는 모든 염, 수화물, 용매화물, 유도체 등을 모두 포함할 수 있다. 부가염은 통상의 방법으로 제조할 수 있고, 수혼화성 유기용매, 예를 들면 아세톤, 메탄올, 에탄올, 또는 아세토니트릴 등에 녹여 과량의 유기염기를 가하거나 무기염기의 염기 수용액을 가한 후 침전시키거나 결정화시켜서 제조할 수 있다. 또는 이 혼합물에서 용매나 과량의 염기를 증발시킨 후 건조시켜서 부가염을 얻거나 또는 석출된 염을 흡인 여과시켜 제조할 수 있다.In addition, the compound may include all salts, hydrates, solvates, derivatives, and the like that can be prepared by conventional methods, as well as pharmaceutically or food-acceptable salts. The addition salt can be prepared by a conventional method, and is dissolved in a water-miscible organic solvent such as acetone, methanol, ethanol, or acetonitrile, and an excess organic base is added or an aqueous solution of an inorganic base is added, followed by precipitation or crystallization. can be manufactured by Alternatively, the solvent or excess base may be evaporated from the mixture and then dried to obtain an addition salt, or the precipitated salt may be suction filtered.
상기 화합물 또는 이의 염은 상기 항비만용 조성물 전체 100 중량부에 대하여, 0.1 내지 90 중량부 함유될 수 있으나, 이에 제한되는 것은 아니다.The compound or salt thereof may be contained in an amount of 0.1 to 90 parts by weight based on 100 parts by weight of the total anti-obesity composition, but is not limited thereto.
상기 화합물 또는 이의 염은 항비만 활성을 가질 수 있다.The compound or salt thereof may have anti-obesity activity.
본 명세서에서, "항비만(anti-obesity)"은 비만 치료, 예방, 개선 또는 억제 등을 포괄하는 의미이다.In the present specification, "anti-obesity" is meant to cover obesity treatment, prevention, improvement or suppression, and the like.
보다 상세하게는, 상기 화합물 또는 이의 염은 지방전구세포(preadipocyte)의 지방세포(adipocyte)로의 분화를 억제하여 지방구(lipid droplet) 생성을 억제하거나 이의 분해를 촉진하는 바, 이를 함유하는 항비만용 조성물을 이용하여 비만 또는 비만 관련 질환의 예방, 개선 또는 치료를 위한 약학 조성물 또는 건강식품 조성물로 활용할 수 있다.More specifically, the compound or its salt suppresses the differentiation of preadipocytes into adipocytes to inhibit the production of lipid droplets or promote their decomposition. It can be used as a pharmaceutical composition or health food composition for the prevention, improvement or treatment of obesity or obesity-related diseases using the composition for use.
본 명세서에서, "비만(obesity)"은 체내에 지방이 비정상적으로 많이 축적되는 질병을 의미한다.In the present specification, “obesity” refers to a disease in which an abnormally large amount of fat is accumulated in the body.
상기 항비만용 조성물을 이용하여 비만을 예방, 개선 또는 치료할 수 있고, 더불어 비만으로 인한 대사 합병증과 같은 비만 관련 질환을 예방, 개선 또는 치료할 수 있다.Obesity can be prevented, improved, or treated using the anti-obesity composition, and obesity-related diseases such as metabolic complications caused by obesity can be prevented, improved, or treated.
상기 대사 합병증은 중성지질, 콜레스테롤, 저밀도 지질의 혈중농도 상승에 기인한 질병을 포함할 수 있다.The metabolic complications may include diseases caused by elevated blood levels of triglycerides, cholesterol, and low-density lipids.
보다 상세하게는, 상기 대사 합병증은 대사증후군(내장 지방 증후군, 대사 이상 증후군 등), 고트리글리세라이드 혈증, 저HDL혈증, 협심증, 심근경색, 성기능부전증, 수면무호흡증, 월경전 증후군, 스트레스성 요실금을 포함하는 요실금, 과행동장애, 만성 피로 증후군, 골관절염, 체중 증가와 관련된 암, 기립성 저혈압, 폐고혈압, 월경장애, 당뇨병, 고혈압, 손상된 내당력, 관상동맥혈전증, 졸증, 우울증, 불안증, 정신병, 지연성 운동장애, 약물중독, 약물 남용, 인지장애, 알츠하이머병, 뇌허혈, 강박성 행동, 공황발작, 사회공포증, 대식증, 아테롬성동맥경화증, 담석증과 같은 담낭 질병, 식욕부진, 다낭성 난소 질환과 같은 생식장애, 감염, 정맥류성 정맥, 표피증식 및 습진과 같은 피부병, 인슐린 저항성, 만성 동맥폐색증, 정형외과적 상해, 혈전색전증, 심장질환, 비뇨기질환, 지질증후군, 과혈당증 또는 스트레스에서 선택될 수 있으나, 이에 제한되는 것은 아니다.More specifically, the metabolic complications include metabolic syndrome (visceral fat syndrome, metabolic syndrome, etc.), hypertriglyceridemia, hypoHDLemia, angina pectoris, myocardial infarction, sexual dysfunction, sleep apnea, premenstrual syndrome, and stress urinary incontinence. Including urinary incontinence, hyperactivity disorder, chronic fatigue syndrome, osteoarthritis, cancer associated with weight gain, orthostatic hypotension, pulmonary hypertension, menstrual disorders, diabetes mellitus, hypertension, impaired glucose tolerance, coronary thrombosis, apoplexy, depression, anxiety, psychosis, Reproductive disorders such as tardive dyskinesia, drug addiction, substance abuse, cognitive impairment, Alzheimer's disease, cerebral ischemia, obsessive-compulsive behavior, panic attacks, social phobia, bulimia, atherosclerosis, gallbladder diseases such as cholelithiasis, anorexia, polycystic ovary disease , infection, varicose veins, skin diseases such as epidermal hyperplasia and eczema, insulin resistance, chronic arterial occlusion, orthopedic injury, thromboembolism, heart disease, urinary disease, lipid syndrome, hyperglycemia, or stress, but is limited thereto it is not going to be
바람직하게는, 본 발명은 하기 화학식 1로 표시되는 화합물 또는 이의 식품학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 건강식품 조성물을 제공한다.Preferably, the present invention provides a health food composition for anti-obesity containing a compound represented by Formula 1 below or a pharmaceutically acceptable salt thereof as an active ingredient.
<화학식 1><
이에 상응하는 특징들은 상술된 부분에서 대신할 수 있다.Corresponding features may be substituted in the foregoing.
본 발명에 따른 건강식품 조성물에 있어서, 상기 건강식품은 비만 관련 질환의 예방 또는 개선 목적으로, 분말, 과립, 정제, 캡슐, 젤리, 시럽 또는 음료 등의 형태로 제조될 수 있다. 상기 건강식품이 취할 수 있는 형태에는 제한이 없으며, 일반적인 약학 조성물과 동일한 방식으로 제제화되어 기능성 식품으로 이용하거나, 각종 식품에 첨가될 수 있다.In the health food composition according to the present invention, the health food may be prepared in the form of powder, granule, tablet, capsule, jelly, syrup or beverage for the purpose of preventing or improving obesity-related diseases. There is no limit to the form that the health food can take, and it can be formulated in the same way as a general pharmaceutical composition and used as a functional food or added to various foods.
상기 건강식품 조성물에 함유된 상기 화합물 또는 이의 염의 유효 용량은 비만 또는 비만 관련 질환 예방 또는 개선 등 그 사용 목적에 따라 적절하게 조절될 수 있다.An effective dose of the compound or salt thereof contained in the health food composition may be appropriately adjusted according to the purpose of use, such as prevention or improvement of obesity or obesity-related diseases.
상기 화합물 또는 이의 식품학적으로 허용가능한 염은 건강식품 조성물 전체 100 중량부에 대하여, 0.01 내지 1 중량부, 보다 바람직하게는 0.01 내지 0.5 중량부 함유될 수 있으나, 이에 제한되는 것은 아니다.The compound or a food chemically acceptable salt thereof may be contained in an amount of 0.01 to 1 part by weight, more preferably 0.01 to 0.5 part by weight, based on 100 parts by weight of the total health food composition, but is not limited thereto.
본 발명의 일 제조예에 따르면, 상기 건강식품 조성물이 음료 형태인 경우, 건강식품 조성물 전체 100 중량부에 대하여, 0.01 내지 1 중량부, 보다 바람직하게는 0.01 내지 0.03 중량부 함유될 수 있으나, 이에 제한되는 것은 아니다.According to one preparation example of the present invention, when the health food composition is in the form of a beverage, it may be contained in an amount of 0.01 to 1 part by weight, more preferably 0.01 to 0.03 part by weight, based on 100 parts by weight of the total health food composition. It is not limited.
상기 건강식품 조성물이 분말 또는 정제형인 경우, 건강식품 조성물 전체 100 중량부에 대하여, 0.01 내지 1 중량부, 보다 바람직하게는 0.1 내지 0.5 중량부 함유될 수 있으나, 이에 제한되는 것은 아니다.When the health food composition is in powder or tablet form, it may be contained in an amount of 0.01 to 1 part by weight, more preferably 0.1 to 0.5 part by weight, based on 100 parts by weight of the total health food composition, but is not limited thereto.
상기 건강식품 조성물이 젤리형인 경우, 건강식품 조성물 전체 100 중량부에 대하여, 0.01 내지 1 중량부, 보다 바람직하게는 0.1 내지 0.3 중량부 함유될 수 있으나, 이에 제한되는 것은 아니다.When the health food composition is a jelly type, it may be contained in an amount of 0.01 to 1 part by weight, more preferably 0.1 to 0.3 part by weight, based on 100 parts by weight of the total health food composition, but is not limited thereto.
상기 건강식품은 통상적인 의미의 식품을 모두 포함할 수 있다. 예를 들어, 음료 및 각종 드링크, 과실 및 그의 가공식품(과일통조림, 잼 등), 어류, 육류 및 그 가공식품(햄, 베이컨 등), 빵류 및 면류, 쿠키 및 스낵류, 유제품(버터, 치즈 등) 등이 가능하며, 통상적인 의미에서의 기능성 식품을 모두 포함할 수 있다. 또한 동물을 위한 사료로 이용되는 식품도 포함할 수 있다.The health food may include all foods in a conventional sense. For example, beverages and various drinks, fruits and their processed foods (canned fruit, jam, etc.), fish, meat and their processed foods (ham, bacon, etc.), breads and noodles, cookies and snacks, dairy products (butter, cheese, etc.) ), etc., and may include all functional foods in a conventional sense. It may also include food used as feed for animals.
상기 건강식품 조성물은 당업계에서 통상적으로 사용되는 식품학적으로 허용 가능한 식품 첨가제(식품 첨가물) 및 적절한 기타 보조 성분을 더 포함하여 제조될 수 있다. 식품 첨가물로서의 적합 여부는 다른 규정이 없는 한, 식품의약품안전처에 승인된 식품 첨가물 공전의 총칙 및 일반시험법 등에 따라 해당 품목에 관한 규격 및 기준에 의하여 판정할 수 있다. 상기 '식품 첨가물 공전'에 수재된 품목으로는 예를 들어, 케톤류, 글리신, 구연산칼슘, 니코틴산, 계피산 등의 화학적 합성물; 감색소, 감초추출물, 결정셀룰로오스, 고량색소, 구아검 등의 천연첨가물; L-글루타민산나트륨 제제, 면류첨가알칼리제, 보존료 제제, 타르색소제제 등의 혼합 제제류 등을 들 수 있다.The health food composition may be prepared by further including food chemically acceptable food additives (food additives) commonly used in the art and other suitable auxiliary ingredients. Unless otherwise specified, suitability as a food additive can be determined according to the standards and standards for the item in accordance with the General Rules of the Code of Food Additives approved by the Ministry of Food and Drug Safety and general test methods. Examples of the items listed in the 'Food Additive Code' include, for example, chemical compounds such as ketones, glycine, calcium citrate, nicotinic acid, and cinnamic acid; natural additives such as persimmon pigment, licorice extract, crystalline cellulose, kaoliang pigment, and guar gum; mixed preparations such as sodium L-glutamate preparations, noodle-added alkali preparations, preservative preparations, and tar color preparations; and the like.
상기 기타 보조 성분은 예를 들어, 향미제, 천연 탄수화물, 감미제, 비타민, 전해질, 착색제, 펙트산, 알긴산, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알콜, 탄산화제 등을 추가로 함유할 수 있다. 특히, 상기 천연 탄수화물로는 포도당, 과당과 같은 모노사카라이드, 말토스, 수크로오스와 같은 디사카라이드, 및 덱스트린, 사이클로덱스트린과 같은 폴리사카라이드, 자일리톨, 소르비톨, 에리트리톨 등의 당알콜을 사용할 수 있으며, 감미제로서는 타우마틴, 스테비아 추출물과 같은 천연 감미제나 사카린, 아스파르탐과 같은 합성 감미제 등을 사용할 수 있다.The other auxiliary ingredients include, for example, flavoring agents, natural carbohydrates, sweeteners, vitamins, electrolytes, colorants, pectic acid, alginic acid, organic acids, protective colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents, etc. may additionally contain. In particular, as the natural carbohydrate, monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol may be used. As the sweetener, natural sweeteners such as thaumatin and stevia extract or synthetic sweeteners such as saccharin and aspartame may be used.
상기 건강식품 조성물은 식품을 원료로 하여 일반 약품의 장기 복용 시 발생할 수 있는 부작용 등이 없는 장점이 있고, 휴대성이 뛰어나, 비만 또는 비만 관련 질환 예방 또는 개선을 위한 보조제로 섭취될 수 있다.The health food composition uses food as a raw material and has the advantage of not having side effects that can occur when taking general medicines for a long time, and has excellent portability, so it can be taken as an adjuvant for preventing or improving obesity or obesity-related diseases.
바람직하게는, 본 발명은 하기 화학식 1로 표시되는 화합물 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 항비만용 약학 조성물을 제공한다.Preferably, the present invention provides a pharmaceutical composition for anti-obesity containing a compound represented by
<화학식 1><
이에 상응하는 특징들은 상술된 부분에서 대신할 수 있다.Corresponding features may be substituted in the foregoing.
본 발명에 따른 약학 조성물은 약학적 분야의 통상적인 방법에 따라 제조될 수 있다. 상기 약학 조성물은 제형에 따라 약학적으로 허용가능한 적절한 담체와 배합될 수 있고, 필요에 따라, 부형제, 희석제, 분산제, 유화제, 완충제, 안정제, 결합제, 붕해제, 용제 등을 더 포함하여 제조될 수 있다. 상기 적절한 담체 등은 본 발명에 따른 화합물 또는 이의 약학적으로 허용가능한 염의 활성 및 특성을 저해하지 않는 것으로, 투여 형태 및 제형에 따라 달리 선택될 수 있다.The pharmaceutical composition according to the present invention can be prepared according to conventional methods in the pharmaceutical field. The pharmaceutical composition may be formulated with an appropriate pharmaceutically acceptable carrier according to the formulation and, if necessary, may further contain excipients, diluents, dispersants, emulsifiers, buffers, stabilizers, binders, disintegrants, solvents, and the like. there is. The appropriate carrier and the like do not inhibit the activity and characteristics of the compound according to the present invention or a pharmaceutically acceptable salt thereof, and may be selected differently depending on the dosage form and dosage form.
상기 약학 조성물은 어떠한 제형으로도 적용될 수 있고, 보다 상세하게는 통상의 방법에 따라 경구형 제형, 외용제, 좌제 및 멸균 주사용액의 비경구형 제형으로 제형화하여 사용될 수 있다.The pharmaceutical composition may be applied in any dosage form, and more specifically, it may be formulated and used in parenteral dosage forms such as oral dosage forms, external preparations, suppositories and sterile injection solutions according to conventional methods.
상기 경구형 제형 중 고형 제형은 정제, 환제, 산제, 과립제, 캡슐제 등의 형태로, 적어도 하나 이상의 부형제, 예를 들면, 전분, 칼슘카보네이트, 수크로스, 락토오스, 솔비톨, 만니톨, 셀룰로오스, 젤라틴 등을 섞어 조제할 수 있고, 단순한 부형제 이외에 마그네슘 스테아레이트, 탈크 같은 윤활제들도 포함될 수 있다. 또한, 캡술제형의 경우 상기 언급한 물질 외에도 지방유와 같은 액체 담체를 더 포함할 수 있다.Among the oral dosage forms, the solid dosage form is in the form of tablets, pills, powders, granules, capsules, etc., and includes at least one excipient such as starch, calcium carbonate, sucrose, lactose, sorbitol, mannitol, cellulose, gelatin, etc. may be prepared by mixing, and lubricants such as magnesium stearate and talc may be included in addition to simple excipients. In addition, in the case of a capsule formulation, a liquid carrier such as fatty oil may be further included in addition to the above-mentioned materials.
상기 경구형 제형 중 액상 제형은 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순 희석제인 물, 리퀴드 파라핀 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다.Among the oral formulations, liquid formulations include suspensions, solutions for internal use, emulsions, syrups, etc. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, aromatics, and preservatives may be included. there is.
상기 비경구 제형은 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조 제제, 좌제가 포함될 수 있다. 비수성 용제, 현탁제로는 프로필렌글리콜, 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다. 좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈 61, 카카오지, 라우린지, 글리세로제라틴 등이 사용될 수 있다. 이에 제한되지 않고, 당해 기술 분야에 알려진 적합한 제제를 모두 사용 가능하다.The parenteral formulation may include a sterilized aqueous solution, a non-aqueous solvent, a suspension, an emulsion, a lyophilized formulation, and a suppository. Propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate may be used as non-aqueous solvents and suspending agents. As a base for the suppository, witepsol, macrogol, Tween 61, cacao butter, laurin fat, glycerogeratin, and the like may be used. It is not limited thereto, and all suitable agents known in the art may be used.
또한, 상기 약학 조성물은 치료 효능의 증진을 위해 칼슘이나 비타민 등을 더 첨가할 수 있다.In addition, calcium or vitamins may be further added to the pharmaceutical composition to enhance therapeutic efficacy.
본 발명에 따른 약학 조성물은 약학적으로 유효한 양으로 투여될 수 있다.The pharmaceutical composition according to the present invention can be administered in a pharmaceutically effective amount.
본 명세서에서, "약학적으로 유효한 양"이란, 의학적 치료에 적용 가능한 합리적인 수혜/위험 비율로 질환을 치료하기에 충분하며 부작용을 일으키지 않을 정도의 양을 의미한다.In the present specification, "pharmaceutically effective amount" means an amount that is sufficient to treat a disease with a reasonable benefit/risk ratio applicable to medical treatment and does not cause side effects.
상기 약학 조성물의 유효 용량 수준은 사용 목적, 환자의 연령, 성별, 체중 및 건강 상태, 질환의 종류, 중증도, 약물의 활성, 약물에 대한 민감도, 투여방법, 투여 시간, 투여 경로 및 배출 비율, 치료기간, 배합 또는 동시 사용되는 약물을 포함한 요소 및 기타 의학 분야에 잘 알려진 요소에 따라 달리 결정될 수 있다. 예를 들어, 일정하지는 않지만 일반적으로 0.001 내지 100mg/kg으로, 바람직하게는 0.01 내지 10mg/kg을 일일 1회 내지 수회 투여될 수 있다. 상기 투여량은 어떠한 면으로든 본 발명의 범위를 한정하는 것은 아니다.The effective dose level of the pharmaceutical composition is determined by the purpose of use, the patient's age, sex, weight and health condition, disease type, severity, drug activity, drug sensitivity, administration method, administration time, administration route and excretion rate, treatment Duration, combination, or factors including drugs used concurrently and other factors well known in the medical arts may be determined differently. For example, although not constant, generally 0.001 to 100 mg/kg, preferably 0.01 to 10 mg/kg, may be administered once or several times a day. The dosage is not intended to limit the scope of the present invention in any way.
상기 약학 조성물은 비만 또는 비만으로 인한 대사 합병증 등 비만 관련 질환이 발생할 수 있는 임의의 동물에 투여할 수 있고, 상기 동물은 예를 들어, 인간 및 영장류뿐만 아니라 소, 돼지, 말, 개 등의 가축 등을 포함할 수 있다.The pharmaceutical composition may be administered to any animal that may develop obesity-related diseases such as obesity or metabolic complications due to obesity, and the animal may include, for example, humans and primates as well as livestock such as cattle, pigs, horses, and dogs. etc. may be included.
상기 약학 조성물은 제제 형태에 따른 적당한 투여 경로로 투여될 수 있고, 목적 조직에 도달할 수 있는 한 경구 또는 비경구의 다양한 경로를 통하여 투여될 수 있다. 투여 방법은 특히 한정할 필요 없이, 예를 들면, 경구, 직장 또는 정맥, 근육, 피부 도포, 호흡기내 흡입, 자궁내 경막 또는 뇌혈관내(intracerebroventricular) 주사 등의 통상적인 방법으로 투여될 수 있다.The pharmaceutical composition may be administered by an appropriate administration route according to the formulation form, and may be administered through various oral or parenteral routes as long as it can reach the target tissue. The method of administration is not particularly limited, and may be administered by conventional methods such as oral, rectal or intravenous, intramuscular, dermal application, intraventricular inhalation, intrauterine epidural or intracerebroventricular injection.
본 발명에 따른 약학 조성물은 비만 또는 비만 관련 질환의 예방 또는 치료를 위하여 단독으로 사용될 수 있고, 수술 또는 다른 약물 치료 등과 병용하여 사용될 수 있다.The pharmaceutical composition according to the present invention may be used alone for the prevention or treatment of obesity or obesity-related diseases, and may be used in combination with surgery or other drug treatment.
또한, 본 발명은 하기 화학식 1로 표시되는 화합물 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 지방세포 분화 억제용 시약 조성물을 제공한다.In addition, the present invention provides a reagent composition for inhibiting adipocyte differentiation comprising a compound represented by
<화학식 1><
이에 상응하는 특징들은 상술된 부분에서 대신할 수 있다.Corresponding features may be substituted in the foregoing.
이하, 본 발명의 이해를 돕기 위하여 실시예를 들어 상세하게 설명하기로 한다. 다만 하기의 실시예는 본 발명의 내용을 예시하는 것일 뿐 본 발명의 범위가 하기 실시예에 한정되는 것은 아니다. 본 발명의 실시예는 당업계에서 평균적인 지식을 가진 자에게 본 발명을 보다 완전하게 설명하기 위해 제공되는 것이다.Hereinafter, examples will be described in detail to aid understanding of the present invention. However, the following examples are merely illustrative of the contents of the present invention, but the scope of the present invention is not limited to the following examples. The embodiments of the present invention are provided to more completely explain the present invention to those skilled in the art.
<실시예 1> 카프타르산의 분석<Example 1> Analysis of caftaric acid
1. 대상 물질1. Target substance
카프타르산(caftaric acid) 표준물질을 켐페이스(ChemFaces)로부터 구매하여 사용하였다. A caftaric acid standard was purchased from ChemFaces and used.
하기 표 1은 구매한 카프타르산의 정보이다.Table 1 below is information on purchased captaric acid.
2. 물질 분석 (HPLC)2. Material Analysis (HPLC)
대상 물질을 정밀히 칭량하고, 메탄올(HPLC grade)을 첨가하여 완전히 녹여 표준원액으로 하였다. 상기 표준원액을 메탄올로 적절히 희석하여 표준용액으로 하였다.The target substance was accurately weighed, and methanol (HPLC grade) was added to completely dissolve the mixture to form a standard stock solution. The standard stock solution was appropriately diluted with methanol to obtain a standard solution.
하기 표 2는 고성능액체크로마토그래피(HPLC) 분석 조건을 나타낸 것이다.Table 2 below shows high-performance liquid chromatography (HPLC) analysis conditions.
그 결과, 도 1 및 도 2에 나타난 바와 같이, 상기 대상 물질이 카프타르산 임을 확인할 수 있다.As a result, as shown in FIGS. 1 and 2, it can be confirmed that the target material is captaric acid.
<실험예 1> 카프타르산의 항비만 활성 확인<Experimental Example 1> Confirmation of anti-obesity activity of caftaric acid
1. 실험방법1. Experiment method
1) 실험 모델1) Experimental model
ATCC(American Type Culture Collection)로부터 분양 받은 마우스 지방전구세포인 3T3-L1 세포주를 사용하였다.The 3T3-L1 cell line, which is a mouse progenitor cell line distributed from ATCC (American Type Culture Collection), was used.
2) 지방전구세포(preadipocyte) 배양2) Culture of preadipocytes
1% 페니실린(penicillin)-스트렙토마이신(streptomycin) 및 10% 신생 송아지 혈청(newborn calf serum, NBCS)이 포함된 DMEM (high-glucose Dulbeco’s modified Eagle’s medium) 배지에서 37℃, 5% CO2 조건에서 배양하였다. 매 2일마다 배양액을 교환하였다.Cultured in DMEM (high-glucose Dulbeco's modified Eagle's medium) medium containing 1% penicillin-streptomycin and 10% newborn calf serum (NBCS) at 37°C and 5% CO 2 conditions. did The culture medium was exchanged every 2 days.
3) 세포 독성(생존율) 확인 (WST assay)3) Confirmation of cytotoxicity (survival rate) (WST assay)
세포 생존율 시험(Water soluble tetrazolium salt; WST assay)은 EZ-CYTOX(Daeillab service co., Ltd, seoul, Korea)를 사용하여 수행하였다.Cell viability test (Water soluble tetrazolium salt; WST assay) was performed using EZ-CYTOX (Daeillab service co., Ltd, Seoul, Korea).
3T3-L1 세포를 96웰 플레이트에 1×104 cells/well로 분주하여 24시간 동안 배양한 다음, 각 웰에 시료를 농도 별로 처리하였다. 24시간 후, 각 웰당 EZ-Cytox 10μL/100μL을 첨가하여 2시간 동안 인큐베이터에서 반응시켰다. 흡광도를 측정하기 전 1분 정도 부드럽게 진탕(shaking)하였고, ELISA reader(Bio-Rad Laboratories, Hercules, CA, USA)로 450 nm에서 흡광도를 측정하였다.3T3-L1 cells were dispensed in a 96-well plate at 1×10 4 cells/well and cultured for 24 hours, and samples were then treated in each well for each concentration. After 24 hours, 10 μL/100 μL of EZ-Cytox was added to each well and reacted in an incubator for 2 hours. Before measuring the absorbance, it was gently shaken for about 1 minute, and the absorbance was measured at 450 nm with an ELISA reader (Bio-Rad Laboratories, Hercules, CA, USA).
4) 지방세포(adipocyte)로의 분화 유도4) Induction of differentiation into adipocytes
6웰 플레이트에 2×105 cells/well을 균등하게 분주한 후, 100% confluet 상태로부터 48시간 배양하였다. 분화 유도 전까지 매 2일 배양액을 교환하였다.After equally dispensing 2×10 5 cells/well in a 6-well plate, they were cultured for 48 hours in a 100% confluent state. Culture medium was exchanged every 2 days until differentiation induction.
분화 유도 배양액 조성은 하기 표 3과 같다.The composition of the differentiation induction culture medium is shown in Table 3 below.
10% 소태아혈청(fetal bovine serum, FBS), 1% 페니실린-스트렙토마이신
3-이소부틸-1-메틸잔틴(3-isobutyl-1-methylxanthine, IBMX, 0.5 mM)
인슐린(human, 10μg/ml), 덱사메타손(dexamethasone, 1μM)DMEM (high-glucose Dulbeco's modified Eagle's medium)
10% fetal bovine serum (FBS), 1% penicillin-streptomycin
3-isobutyl-1-methylxanthine (IBMX, 0.5 mM)
Insulin (human, 10μg/ml), dexamethasone (1μM)
10% 소태아혈청, 1% 페니실린-스트렙토마이신, 인슐린(human, 10μg/ml)DMEM (high-glucose Dulbeco's modified Eagle's medium)
10% fetal bovine serum, 1% penicillin-streptomycin, insulin (human, 10μg/ml)
10% 소태아혈청, 1% 페니실린-스트렙토마이신DMEM (high-glucose Dulbeco's modified Eagle's medium)
10% fetal bovine serum, 1% penicillin-streptomycin
또한, 분화 유도일로부터 하기 표 4와 같이 배양액과 시료를 매일 교환하였다.In addition, as shown in Table 4 below, from the day of induction of differentiation, culture medium and samples were exchanged every day.
5) 오일 레드 O 염색 (Oil red O staining)5) Oil red O staining
지방전구세포(preadipocyte)에서 지방세포(adipocyte)로 분화하는 과정에서, 지방세포분화에 미치는 영향을 측정하기 위해 Oil red O staining을 수행하였다.In the process of differentiating from preadipocytes to adipocytes, Oil red O staining was performed to measure the effect on adipocyte differentiation.
세포배양 및 분화 유도 프로토콜에 따라 아디포제닉 칵테일(adipogenic cocktail)을 포함한 10% FBS를 함유하는 DMEM 배양액과 시료를 매일 교환하고, 분화 후기(9일째)에 각각 Oil red O staining을 실시하였다. According to the cell culture and differentiation induction protocol, samples were exchanged with DMEM culture medium containing 10% FBS including an adipogenic cocktail every day, and Oil red O staining was performed at the late stage of differentiation (9th day).
배양액을 석션(suction)하고 PBS 용액으로 2회 세척한 뒤, 다시 PBS 용액을 완전히 석션하였다. 10% 포르말린(formalin)을 넣고 5분간 실온에서 고정시킨 다음, 10% 포르말린을 석션한 뒤 다시 새로운 10% 포르말린을 넣어 2시간 이상 실온에서 고정시킨 후 포르말린을 석션하고 60% 이소프로판올(isopropanol)을 넣어 바로 석션한 다음 플라스크를 완전히 건조시켰다.The culture medium was suctioned and washed twice with the PBS solution, and then the PBS solution was completely suctioned again. After adding 10% formalin and fixing at room temperature for 5 minutes, suctioning 10% formalin and then adding new 10% formalin and fixing at room temperature for more than 2 hours, suctioning formalin and adding 60% isopropanol Immediately after suction, the flask was dried completely.
여기에 Oil red O solution 용액을 첨가하여 60분 동안 지방구를 염색하였다. 염색 후 증류수로 4번 세척하여 지방구의 세포내 축적을 현미경과 카메라로 관찰하였고, 지방구 축적 함량을 정량하기 위해 잘 건조된 상태에서 100% 이소프로판올을 첨가하여 Oil red O dye를 용출시켰다. 이후, ELISA reader(Molecular Devices, USA)를 사용하여 520 nm 파장에서 광학 밀도(optical density)를 측정하였다.Oil red O solution was added thereto to stain fat globules for 60 minutes. After staining, the intracellular accumulation of fat globules was observed with a microscope and a camera by washing with distilled
2. 실험결과2. Experimental results
1) 세포 독성 및 생존율 확인1) Confirmation of cytotoxicity and viability
하기 표 5는 카프타르산 농도에 따른 세포 생존율을 측정한 것이다.Table 5 below measures the cell viability according to the concentration of caftaric acid.
상기 표 5 및 도 3을 참조하면, 카프타르산은 40.0μg/mL까지 독성이 나타나지 않았고, 시료를 녹이는 용매로 디메틸설폭사이드(dimethyl sulfoxide, DMSO)를 1% 농도로 처리시에도 독성 및 특이적인 결과가 나타나지 않았다.Referring to Table 5 and FIG. 3, captaric acid did not show toxicity up to 40.0 μg/mL, and even when dimethyl sulfoxide (DMSO) was treated at a concentration of 1% as a solvent for dissolving the sample, toxicity and specific results did not appear
2) 오일 레드 O 염색 결과 확인2) Check the results of Oil Red O staining
도 4를 참조하면, 카프타르산(caftaric acid) 투여 시, 지방구(lipid droplet)가 대조구(contorl) 대비 적은 것을 직접 확인할 수 있고, 지방구 염색 시 투여 농도에 의존적으로 뚜렷한 차이를 나타냄을 확인할 수 있다.Referring to FIG. 4, when caftaric acid is administered, it can be directly confirmed that the number of lipid droplets is smaller than that of the control, and it can be confirmed that fat droplets show a distinct difference depending on the administration concentration during staining. can
하기 표 6은 오일 레드 O 시약을 용출시켜 흡광도를 측정한 결과이다.Table 6 below shows the results of measuring absorbance by eluting the Oil Red O reagent.
상기 표 6 및 도 5를 참조하면, 카프타르산 처리에 따라 그 흡광도 측정 결과도 유의적으로 차이가 남을 확인할 수 있다.Referring to Table 6 and FIG. 5, it can be confirmed that the absorbance measurement result also significantly differs depending on the caftar acid treatment.
즉, 이를 통해 카프타르산이 지방구 생성을 억제하거나 분해를 촉진함으로써 항비만 활성을 가짐을 확인할 수 있다.That is, through this, it can be confirmed that captaric acid has anti-obesity activity by inhibiting fat formation or promoting decomposition.
이하, 본 발명에 따른 카프타르산을 포함하는 조성물의 제제예를 설명하나, 본 발명은 이를 한정하고자 함이 아닌 단지 구체적으로 설명하고자 함이다.Hereinafter, formulation examples of the composition containing caftaric acid according to the present invention will be described, but the present invention is not intended to be limited, but only specifically described.
<제조예 1> 음료 제조<Production Example 1> Beverage production
하기 표 7은 본 발명에 따른 카프타르산을 포함하는 음료 제조를 위한 제제 및 이들의 배합비를 나타낸 것이다.Table 7 below shows formulations for preparing beverages containing caftaric acid according to the present invention and their mixing ratios.
<제조예 2> 건강식품 제조<Preparation Example 2> Manufacture of health food
2-1. 분말(powder) 및 정제(tablet)2-1. powder and tablet
하기 표 8은 본 발명에 따른 카프타르산을 포함하는 분말 또는 정제형의 건강식품 제조를 위한 제제 및 이들의 배합비를 나타낸 것이다.Table 8 below shows preparations for preparing health food in powder or tablet form containing captaric acid according to the present invention and their mixing ratios.
2-2. 젤리(jelly)2-2. jelly
하기 표 9는 본 발명에 따른 카프타르산을 포함하는 젤리형의 건강식품 제조를 위한 제제 및 이들의 배합비를 나타낸 것이다.Table 9 below shows formulations and their mixing ratios for preparing a jelly-type health food containing caftaric acid according to the present invention.
이상으로 본 발명의 특정한 부분을 상세히 기술한 바, 당업계의 통상의 지식을 가진 자에게 있어서 이러한 구체적인 기술은 단지 바람직한 구현 예일 뿐이며,이에 본 발명의 범위가 제한되는 것이 아닌 점은 명백하다. 따라서, 본 발명의 실질적인 범위는 첨부된 청구항과 그의 등가물에 의하여 정의된다고 할 것이다. 본 발명의 범위는 후술하는 청구범위에 의하여 나타내어지며, 청구범위의 의미 및 범위 그리고 그 균등 개념으로부터 도출되는 모든 변경 또는 변형된 형태가 본 발명의 범위에 포함되는 것으로 해석되어야 한다.Having described specific parts of the present invention in detail above, it is clear that these specific techniques are merely preferred embodiments for those skilled in the art, and the scope of the present invention is not limited thereto. Accordingly, the substantial scope of the present invention will be defined by the appended claims and equivalents thereof. The scope of the present invention is indicated by the following claims, and all changes or modifications derived from the meaning and scope of the claims and equivalent concepts should be interpreted as being included in the scope of the present invention.
Claims (5)
<화학식 1>
A health food composition for anti-obesity containing a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.
<Formula 1>
상기 화합물 또는 이의 식품학적으로 허용가능한 염은,
지방전구세포의 지방세포로의 분화를 억제하여 지방구(lipid droplet) 생성을 억제하거나 이의 분해를 촉진하는 것을 특징으로 하는, 항비만용 건강식품 조성물.
According to claim 1,
The compound or a food acceptable salt thereof,
A health food composition for anti-obesity, characterized in that by suppressing the differentiation of pre-adipocytes into adipocytes to inhibit the production of fat droplets or to promote their decomposition.
상기 화합물 또는 이의 식품학적으로 허용가능한 염은,
건강식품 조성물 전체 100 중량부에 대하여, 0.01 내지 1 중량부 함유되는 것을 특징으로 하는, 항비만용 건강식품 조성물.
According to claim 1,
The compound or a food acceptable salt thereof,
A health food composition for anti-obesity, characterized in that it is contained in an amount of 0.01 to 1 part by weight, based on 100 parts by weight of the total health food composition.
상기 건강식품 조성물은,
분말, 과립, 정제, 캡슐, 젤리, 시럽 또는 음료 형태인 것을 특징으로 하는, 항비만용 건강식품 조성물.
According to claim 1,
The health food composition,
A health food composition for anti-obesity, characterized in that in the form of powder, granule, tablet, capsule, jelly, syrup or beverage.
<화학식 1>
An anti-obesity pharmaceutical composition comprising a compound represented by Formula 1 below or a pharmaceutically acceptable salt thereof as an active ingredient.
<Formula 1>
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