KR102128624B1 - Pharmaceutical composition comprising the extract of apis mellifera as an effective component for prevention or treatment of diabetes and health functional food comprising the same - Google Patents
Pharmaceutical composition comprising the extract of apis mellifera as an effective component for prevention or treatment of diabetes and health functional food comprising the same Download PDFInfo
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- KR102128624B1 KR102128624B1 KR1020180083220A KR20180083220A KR102128624B1 KR 102128624 B1 KR102128624 B1 KR 102128624B1 KR 1020180083220 A KR1020180083220 A KR 1020180083220A KR 20180083220 A KR20180083220 A KR 20180083220A KR 102128624 B1 KR102128624 B1 KR 102128624B1
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- extract
- bee
- amylase
- adult
- present
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
- A61K35/56—Materials from animals other than mammals
- A61K35/63—Arthropods
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/328—Foods, ingredients or supplements having a functional effect on health having effect on glycaemic control and diabetes
Abstract
본 발명은 꿀벌(Apis mellifera) 추출물을 유효성분으로 함유하는 항당뇨 조성물에 관한 것으로서, 보다 상세하게는, 양봉에 사용되는 서양꿀벌의 추출물을 유효성분으로 함유하는 알파-아밀라아제(α-amylase) 저해, 베타-아밀라아제(β-amylasse) 저해 및 알파-글루코시다아제(α-glucosidase) 저해를 통한 당뇨병의 예방 또는 치료/개선용 약학적 조성물 및 건강 기능 식품에 관한 것이다. 본 발명의 항당뇨 조성물의 유효성분으로서의 꿀벌 추출물은, 본 명세서의 실시예를 통해 증명된 바와 같이, 당뇨병의 예방 또는 개선용 의약품 및 건강 기능 식품으로 사용할 수 있는 뛰어난 효과가 있다. 뿐만 아니라, 본 발명의 꿀벌 추출물은 열 안정성이 우수하고, pH 2의 산성조건 및 혈장 내에서도 전분분해효소 저해 활성의 손실이 나타나지 않아, 액상, 크림, 분말, 환, 정 등의 다양한 형태로 손쉽게 가공될 수 있어 제약 산업 및 식품 산업상 매우 유용하게 이용될 수 있다.The present invention relates to an anti-diabetic composition containing bee ( Apis mellifera ) extract as an active ingredient, more specifically, inhibition of alpha-amylase (α-amylase) containing an extract of Western honey bee used for beekeeping as an active ingredient , Beta-amylase (β-amylasse) inhibition and alpha-glucosidase (α-glucosidase) inhibition of diabetes through the prevention or treatment / improvement pharmaceutical composition and health functional food. Bee extract as an active ingredient of the anti-diabetic composition of the present invention, as demonstrated through the examples of the present specification, has an excellent effect that can be used as a drug or health functional food for preventing or improving diabetes. In addition, the honey bee extract of the present invention has excellent thermal stability, and does not exhibit a loss of starch enzyme inhibitory activity even in the acidic condition of pH 2 and plasma, and is easily processed into various forms such as liquid, cream, powder, pills, tablets, etc. It can be very useful in the pharmaceutical industry and food industry.
Description
본 발명은 꿀벌(Apis mellifera) 추출물을 유효성분으로 함유하는 항당뇨 조성물에 관한 것으로서, 보다 상세하게는, 양봉에 사용되는 서양꿀벌의 추출물을 유효성분으로 함유하는 알파-아밀라아제(α-amylase) 저해, 베타-아밀라아제(β-amylasse) 저해 및 알파-글루코시다아제(α-glucosidase) 저해를 통한 당뇨병의 예방 또는 치료/개선용 약학적 조성물 및 건강 기능 식품에 관한 것이다.The present invention relates to an anti-diabetic composition containing bee ( Apis mellifera ) extract as an active ingredient, more specifically, inhibition of alpha-amylase (α-amylase) containing an extract of Western honey bee used for beekeeping as an active ingredient , Beta-amylase (β-amylasse) inhibition and alpha-glucosidase (α-glucosidase) inhibition of diabetes through the prevention or treatment / improvement pharmaceutical composition and health functional food.
현대인에게 가장 흔한 질병중 하나인 당뇨병은 인슐린의 분비량이 부족하거나 정상적인 기능이 이루어지지 않는 등의 대사질환의 일종으로서 혈중 포도당 농도가 높은 것이 특징이며, 고혈당으로 인하여 여러 증상 및 징후를 일으킨다. 당뇨병은 제1형과 제2형으로 구분되는데, 제1형 당뇨병은 유전적 영향에 의해 인슐린을 전혀 생산하지 못하는 것이 원인이 되어 발생하며, 제2형 당뇨병은 인슐린 기능이 떨어져 인슐린 저항성(insulin resistance)이 원인으로 알려져 있다. 특히, 제2형 당뇨병은 식생활의 서구화에 따른 고열량, 고지방, 고단백의 식단, 운동부족, 스트레스 등 환경적인 요인이 크게 작용하는 것으로 알려져 있다. 당뇨병의 치료를 위해서는 제1형 당뇨병의 경우에는 인슐린 주사가 필수적이며, 제2형 당뇨병의 경우에는 생활습관 교정 및 약물치료가 필요하며, 대표적으로 인슐린 분비 촉진제(예, 레파글리나이드, 미티글이나이드) 및 소장에서의 탄수화물 흡수 지연제[글루코바이: 성분명-아카보즈(acarbose), 베이슨: 성분명-보글리보스(voglibose)] 등이 이용되고 있다.Diabetes, one of the most common diseases in modern people, is a type of metabolic disease such as lack of insulin secretion or normal function, and is characterized by high blood glucose concentration and causes various symptoms and signs due to high blood sugar. Diabetes is divided into type 1 and type 2, and type 1 diabetes is caused by the inability to produce insulin at all due to genetic effects, and type 2 diabetes is insulin resistance due to poor insulin function. ) Is known as the cause. In particular, type 2 diabetes is known to have a large environmental effect such as high calorie, high fat, high protein diet, lack of exercise, and stress due to westernization of diet. In order to treat diabetes, insulin injection is essential in case of type 1 diabetes, lifestyle correction and drug treatment are required in case of type 2 diabetes, and insulin secretagogues (eg, repaglinide, mitigle) are typical. Nied) and a carbohydrate absorption retarder in the small intestine (glucobia: component name-acarabose, basin: component name-voglibose), and the like are used.
한편, 꿀벌(Apis mellifera)은 벌목 꿀벌과의 집단 생활을 하는 곤충으로, 인류에게 사육된 가장 오래된 곤충이다. 전 세계적으로 식물의 화분매개에 결정적인 역할을 수행하며, 또한 양봉을 통해 벌꿀, 벌집, 로열젤리, 프로폴리스, 화분, 봉독 등을 생산하여 인간 생활에 큰 도움을 주는 유익 곤충이다. 꿀벌은 전 세계적으로 가장 많이 식용되고 있는 곤충 중의 하나이기도 하며, 약용으로 이용되기도 한다. On the other hand, bees ( Apis mellifera ) are insects that live collectively with felling bees and are the oldest insects bred to mankind. It is a beneficial insect that plays a decisive role in plant pollination of plants around the world, and also produces honey, honeycomb, royal jelly, propolis, pollen, and bee venom through beekeeping to help human life. Bees are one of the most edible insects in the world and are also used for medicinal purposes.
최근, 식용 곤충의 사회적 인식 변화 및 곤충 산업 활성화에 의해 곤충의 고부가가치화 연구가 진행되고 있으며, 봉독의 항균 활성(Somwongin S. et al., 2018. Toxicon. 145:32-39; 한상미 외, 2011. Journal of Fish Pathology 24: 113-120), 봉독의 항응고 활성(H. Zolfagharian 등, 2015. J. Pharmacopuncture, 18(4): 7-11), 꿀벌 유충 추출물의 fibrin 혈전의 용해 활성(김현애 등, 2013, Journal of Sericultural and Entomological Science v.51 no.2 ,pp. 147-152), 봉독으로부터 다양한 효소저해제(정태숙 외, 1997. Korean Journal of Apiculture 12: 85-92; 양결, 2017. 동아대학교 석사논문) 등이 알려지고 있다. Recently, research on high value-added of insects has been conducted by changing social perception of edible insects and activating the insect industry, and antibacterial activity of bee venom (Somwongin S. et al., 2018. Toxicon. 145:32-39; Han Sang-mi et al., 2011 Journal of Fish Pathology 24: 113-120), anticoagulant activity of bee venom (H. Zolfagharian et al., 2015. J. Pharmacopuncture, 18(4): 7-11), dissolving activity of fibrin thrombi of bee larva extract (Hyunae Kim) Et al., 2013, Journal of Sericultural and Entomological Science v.51 no.2, pp. 147-152), various enzyme inhibitors from bee venom (Jung Tae-suk et al., 1997. Korean Journal of Apiculture 12: 85-92; Yang, 2017) University master's thesis) etc. are known.
꿀벌과 관련된 특허는 [양봉용 관제시스템] (대한민국 등록특허 제10-1867985호), [차량용 벌통 다단 수납장치] (대한민국 등록특허 제10-1856641호)과 같은 꿀벌 양봉 관련 장치에 대한 것이 대부분이며, 최근에는 [꿀벌의 전염병 예방 및 치료용 조성물] (대한민국 등록특허 제10-1847532호), [부저병의 예방 및 치료용 조성물] (대한민국 등록특허 제10-1828563호), [꿀벌의 면역증강용 조성물] (대한민국 등록특허 제10-1424083호), [양봉장 수의학 조성물] (대한민국 등록특허 제10-1185328호)와 같은 꿀벌 양봉 관련 조성물 특허가 개시되어 있다. 특히, 꿀벌과 관련된 유용 기능성 특허는 대부분이 봉독에 집중되어 있으며, 대한민국 등록특허 제10-1316600호에는 [봉독을 함유하는 어류용 사료조성물], 대한민국 등록특허 제10-1834758호에는 [봉독을 유효성분으로 포함하는 치주염의 예방 또는 치료용 조성물]가 개시되어 있으며, 공개특허로 제10-2009-0114999호에 [봉독을 포함하는 간경변 치료용 약학 조성물], 제10-2012-0047593호에 [봉독을 유효성분으로 포함하는 유방암 전이 억제용 조성물]이 알려져 있다. Most of the bee-related patents are related to bee-beekeeping-related devices such as [beekeeping control system] (Republic of Korea Patent No. 10-1867985), [Vehicle Multistage Storage Device] (Republic of Korea Patent No. 10-1856641), Recently, [Composition for the prevention and treatment of infectious diseases of bees] (Republic of Korea Patent No. 10-1847532), [Composition for the prevention and treatment of buzzer disease] (Republic of Korea Patent No. 10-1828563), [For immunity enhancement of bees] Composition] Patents for bee-beekeeping related compositions such as (Republic of Korea Patent No. 10-1424083) and [Apiary Veterinary Medicine Composition] (Republic of Korea Patent No. 10-1185328) are disclosed. In particular, most of the useful functional patents related to bees are concentrated in bee venom, and [Korean bee venom No. 10-1316600 is [Feed composition for fish containing bee venom], and the Republic of Korea registered no. 10-1834758 is effective for bee venom A composition for the prevention or treatment of periodontitis comprising as a component] is disclosed, and in Patent Publication No. 10-2009-0114999 [Pharmaceutical composition for treating cirrhosis including bee venom], No. 10-2012-0047593 It is known a composition for inhibiting breast cancer metastasis comprising as an active ingredient.
본 발명은 상기와 같은 종래 기술의 문제점을 해결하기 위하여 안출된 것으로서, 본 발명에서 해결하고자 하는 과제는 꿀벌 추출물을 유효성분으로 함유하는 항당뇨 활성을 갖는 약학 조성물 및 건강 기능 식품을 제공하고자 하는 것이다.The present invention is to solve the problems of the prior art as described above, the problem to be solved in the present invention is to provide a pharmaceutical composition and a health functional food having anti-diabetic activity containing bee extract as an active ingredient .
상기와 같은 과제를 해결하기 위하여, 본 발명은 꿀벌(Apis mellifera) 추출물을 유효성분으로 함유하는 당뇨병의 예방 또는 치료용 약학적 조성물을 제공한다.In order to solve the above problems, the present invention provides a pharmaceutical composition for preventing or treating diabetes containing bee ( Apis mellifera ) extract as an active ingredient.
상기 꿀벌 추출물은 꿀벌 유충의 열수 추출물 또는 에탄올 추출물인 것이 바람직하다.The bee extract is preferably a hot water extract or ethanol extract of bee larvae.
상기 꿀벌 추출물은 꿀벌 번데기 또는 성충의 에탄올 추출물인 것이 바람직하다.It is preferable that the bee extract is an ethanol extract of a bee pupa or adult.
상기 꿀벌 추출물은 꿀벌 성충의 열수 추출물의 에틸아세테이트 분획물인 것이 바람직하다.The bee extract is preferably an ethyl acetate fraction of a hot water extract of a bee adult.
상기 꿀벌 추출물은 꿀벌 성충의 에탄올 추출물의 헥센 분획물, 에틸아세테이트 분획물 또는 부탄올 분획물인 것이 바람직하다.The bee extract is preferably a hexene fraction, an ethyl acetate fraction or a butanol fraction of the ethanol extract of bee adult.
또한, 본 발명은 꿀벌(Apis mellifera) 추출물을 유효성분으로 함유하는 당뇨병의 예방 또는 개선용 건강 기능 식품을 제공한다.In addition, the present invention provides a health functional food for preventing or improving diabetes containing bee ( Apis mellifera ) extract as an active ingredient.
상기 꿀벌 추출물은 꿀벌 유충의 열수 추출물 또는 에탄올 추출물인 것이 바람직하다.The bee extract is preferably a hot water extract or ethanol extract of bee larvae.
상기 꿀벌 추출물은 꿀벌 번데기 또는 성충의 에탄올 추출물인 것이 바람직하다.It is preferable that the bee extract is an ethanol extract of a bee pupa or adult.
상기 꿀벌 추출물은 꿀벌 성충의 열수 추출물의 에틸아세테이트 분획물인 것이 바람직하다.The bee extract is preferably an ethyl acetate fraction of a hot water extract of a bee adult.
상기 꿀벌 추출물은 꿀벌 성충의 에탄올 추출물의 헥센 분획물, 에틸아세테이트 분획물 또는 부탄올 분획물인 것이 바람직하다.The bee extract is preferably a hexene fraction, an ethyl acetate fraction or a butanol fraction of the ethanol extract of bee adult.
본 발명의 항당뇨 조성물의 유효성분으로서의 꿀벌 추출물은, 본 명세서의 실시예를 통해 증명된 바와 같이, 당뇨병의 예방 또는 개선용 의약품 및 건강 기능 식품으로 사용할 수 있는 뛰어난 효과가 있다. 뿐만 아니라, 본 발명의 꿀벌 추출물은 열 안정성이 우수하고, pH 2의 산성조건 및 혈장 내에서도 전분분해효소 저해 활성의 손실이 나타나지 않아, 액상, 크림, 분말, 환, 정 등의 다양한 형태로 손쉽게 가공될 수 있어 제약 산업 및 식품 산업상 매우 유용하게 이용될 수 있다.Bee extract as an active ingredient of the anti-diabetic composition of the present invention, as demonstrated through the examples of the present specification, has an excellent effect that can be used as a drug or health functional food for preventing or improving diabetes. In addition, the honey bee extract of the present invention has excellent thermal stability, and does not exhibit a loss of starch enzyme inhibitory activity even in the acidic condition of pH 2 and plasma, and is easily processed into various forms such as liquid, cream, powder, pills, tablets, etc. It can be very useful in the pharmaceutical and food industries.
도 1은 실시예에서 사용된 꿀벌 유충, 번데기, 성충 분말의 사진도이다. 1 is a photograph of bee larvae, pupae and adult powder used in Examples.
이하, 본 발명을 상세하게 설명한다.Hereinafter, the present invention will be described in detail.
본 발명의 발명자들은 우수한 영양성과 다양한 약리 활성이 알려진 꿀벌을 대상으로 항당뇨 효능을 검정하기 위하여, 먼저, 꿀벌의 유충, 번데기 및 성충을 각각 구입한 후, 이를 -20℃로 급속냉동하여 사멸시킨 다음, -50℃에서 동결건조하였으며, 이후 막자사발을 이용하여 꿀벌 유충, 번데기 및 성충 분말을 각각 제조하였다. 이후, 제조분말을 이용하여 열수 추출물과 에탄올 추출물을 조제하고, 상기 열수 추출물 및 에탄올 추출물로부터 헥센, 에틸아세테이트 및 부탄올의 순차적 유기용매 분획물 및 물 잔류물을 각각 회수하여, 항당뇨 활성 성분을 회수하였으며, 상기 활성 성분들은 열 안정성과 산 안정성이 우수한 특징을 가짐을 확인함으로써 상기 활성 성분들을 당뇨병의 예방 또는 치료/개선용 약학적 조성물 및 건강 기능 식품으로 활용하고자 하였다.The inventors of the present invention, in order to test the anti-diabetic effect on bees targeted for bees with excellent nutritional properties and various pharmacological activities, first purchased the bee larvae, pupae and adult, respectively, and then rapidly frozen them to -20°C to kill them. Next, lyophilization was performed at -50°C, and then bee larvae, pupae and adult powders were prepared using a pestle. Thereafter, a hot water extract and an ethanol extract were prepared using the manufactured powder, and sequential organic solvent fractions and water residues of hexene, ethyl acetate, and butanol were recovered from the hot water extract and ethanol extract, respectively, and the antidiabetic active component was recovered. , It was intended to utilize the active ingredients as a pharmaceutical composition for preventing or treating/improving diabetes and a health functional food by confirming that the active ingredients have excellent thermal stability and acid stability.
구체적으로, 본 발명자들은 항염증 및 항고혈압 효과가 있다고 알려진 꿀벌을 이용하여 항당뇨 조성물을 개발하기 위하여, 꿀벌 유충, 번데기 및 성충을 대상으로 열수 추출물과 에탄올 추출물을 조제하고, 이들 추출물을 대상으로 알파-아밀라아제(α-amylase), 베타-아밀라아제(β-amylase) 및 알파-글루코시다아제(α-glucosidase)에 대한 저해 활성을 평가한 결과, 유충의 열수 추출물과 에탄올 추출물, 번데기와 성충의 에탄올 추출물에서 우수한 항당뇨 활성을 확인하였으며, 특히, 꿀벌 성충의 열수 추출물로부터 분획된 에틸아세테이트 분획물, 에탄올 추출물로부터 분획된 헥센 분획물, 에틸아세테이트 분획물 및 부탄올 분획물에서 강력한 효소 저해 활성을 확인하였다.Specifically, the present inventors prepare a hot water extract and an ethanol extract for bee larvae, pupae, and adult insects to develop an antidiabetic composition using bees known to have anti-inflammatory and antihypertensive effects, and target these extracts As a result of evaluating inhibitory activity on alpha-amylase (α-amylase), beta-amylase (β-amylase), and alpha-glucosidase (α-glucosidase), larvae's hot water extract and ethanol extract, pupae and adult ethanol Excellent anti-diabetic activity was confirmed in the extract. In particular, strong enzyme inhibitory activity was confirmed in ethyl acetate fraction fractionated from hot water extract of bee adult, hexene fraction fractionated from ethanol extract, ethyl acetate fraction and butanol fraction.
따라서, 본 발명은 꿀벌(Apis mellifera) 추출물을 유효성분으로 함유하는 당뇨병의 예방 또는 치료용 약학적 조성물을 제공한다.Accordingly, the present invention provides a pharmaceutical composition for the prevention or treatment of diabetes containing bee ( Apis mellifera ) extract as an active ingredient.
상기 꿀벌 추출물은 꿀벌 유충의 열수 추출물 또는 에탄올 추출물인 것이 바람직하다.The bee extract is preferably a hot water extract or ethanol extract of bee larvae.
상기 꿀벌 추출물은 꿀벌 번데기 또는 성충의 에탄올 추출물인 것이 바람직하다.It is preferable that the bee extract is an ethanol extract of a bee pupa or adult.
상기 꿀벌 추출물은 꿀벌 성충의 열수 추출물의 에틸아세테이트 분획물인 것이 바람직하다.The bee extract is preferably an ethyl acetate fraction of a hot water extract of a bee adult.
상기 꿀벌 추출물은 꿀벌 성충의 에탄올 추출물의 헥센 분획물, 에틸아세테이트 분획물 또는 부탄올 분획물인 것이 바람직하다.The bee extract is preferably a hexene fraction, an ethyl acetate fraction or a butanol fraction of the ethanol extract of bee adult.
또한, 본 발명은 꿀벌(Apis mellifera) 추출물을 유효성분으로 함유하는 당뇨병의 예방 또는 개선용 건강 기능 식품을 제공한다.In addition, the present invention provides a health functional food for preventing or improving diabetes containing bee ( Apis mellifera ) extract as an active ingredient.
상기 꿀벌 추출물은 꿀벌 유충의 열수 추출물 또는 에탄올 추출물인 것이 바람직하다.The bee extract is preferably a hot water extract or ethanol extract of bee larvae.
상기 꿀벌 추출물은 꿀벌 번데기 또는 성충의 에탄올 추출물인 것이 바람직하다.It is preferable that the bee extract is an ethanol extract of a bee pupa or adult.
상기 꿀벌 추출물은 꿀벌 성충의 열수 추출물의 에틸아세테이트 분획물인 것이 바람직하다.The bee extract is preferably an ethyl acetate fraction of a hot water extract of a bee adult.
상기 꿀벌 추출물은 꿀벌 성충의 에탄올 추출물의 헥센 분획물, 에틸아세테이트 분획물 또는 부탄올 분획물인 것이 바람직하다.The bee extract is preferably a hexene fraction, an ethyl acetate fraction or a butanol fraction of the ethanol extract of bee adult.
이하에서는, 본 발명의 꿀벌 추출물 및 항당뇨 활성 성분의 제조 방법 및 효능 실험 등을 보다 구체적으로 설명한다.Hereinafter, a method and an efficacy test of the bee extract and anti-diabetic active ingredient of the present invention will be described in more detail.
본 발명의 발명자들은 본 발명의 목적을 달성하기 위하여, 꿀벌 사육 단계; 꿀벌 유충, 번데기, 성충의 회수/전처리 및 동결건조 단계; 꿀벌 유충, 번데기, 성충의 분말화 단계; 꿀벌 유충, 번데기, 성충의 추출물 조제 단계; 꿀벌 성충 추출물로부터 헥센, 에틸아세테이트, 부탄올의 순차적 유기용매 분획물 조제 및 이후 얻어지는 물 잔류물 조제 단계; 상기 추출물 및 분획물의 항당뇨 활성 평가 단계 및 활성 물질의 안정성 조사 단계의 실험들을 수행하였다.Inventors of the present invention to achieve the object of the present invention, bee breeding step; Recovery/pre-treatment and freeze-drying of bee larvae, pupae, and adults; Bee larvae, pupae and adult stages of powdering; Bee larva, pupa, adult extract preparation step; Sequential organic solvent fraction preparation of hexene, ethyl acetate and butanol from the bee adult extract and subsequent water residue preparation step; The extracts and fractions were tested for anti-diabetic activity evaluation and active substance stability investigation.
바람직한 구체예로서, 본 발명은 통상의 곤충 사육과 동일한 방법으로 꿀벌을 사육한 후, 양봉 현장에서 유충, 번데기, 성충을 각각 회수하고, 이후 -20℃로 급속냉동하여 사멸시킨 다음, -50℃에서 동결건조 후, 막자사발을 이용하여 분말로 제조하여 용매로 추출한 다음, 추출액을 0.06mm 이하의 여과망을 사용하여 여과하고, 이를 감압농축하여 추출물을 조제하며, 이를 유기용매로 순차 분획하여 유기용매 분획물과 물 잔류물을 수득할 수 있다.As a preferred embodiment, the present invention, after raising the bees in the same way as the normal insect breeding, after collecting the larvae, pupae, and adult in the beekeeping site, and then rapidly frozen to -20 ℃ to kill, then -50 ℃ After freeze-drying, the mixture was prepared as a powder using a mortar, extracted with a solvent, and then the extract was filtered using a filter network of 0.06 mm or less, concentrated under reduced pressure to prepare an extract, and sequentially fractionated with an organic solvent to produce an organic solvent. Fractions and water residues can be obtained.
본 발명에서 사용되는 용매는 물(냉수, 열수), 주정, 탄소수 1~4의 무수 또는 함수 저급 알코올(메탄올, 에탄올, 주정, 프로판올, 부탄올 등), 상기 저급 알코올과 물과의 혼합용매 등을 이용할 수 있으며, 열수, 또는 95% 에탄올 추출이 가장 바람직하다.The solvent used in the present invention includes water (cold water, hot water), alcohol, anhydrous or hydrous lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, alcohol, propanol, butanol, etc.), mixed solvents of the lower alcohol and water, and the like. Can be used, hot water, or 95% ethanol extraction is most preferred.
본 발명에서 사용되는 유기용매는 헥센, 에틸아세테이트 및 부탄올을 이용할 수 있으며, 이들 유기용매로 추출물을 순차 또는 각각 분획하여 헥센 분획물, 에틸아세테이트 분획물, 부탄올 분획물 및 물 잔류물을 수득할 수 있다. As the organic solvent used in the present invention, hexene, ethyl acetate and butanol may be used, and the extracts may be sequentially or separately fractionated with these organic solvents to obtain a hexene fraction, ethyl acetate fraction, butanol fraction, and water residue.
본 발명에서는, 꿀벌 유충, 번데기, 성충의 열수 추출물과 에탄올 추출물을 0.5mg/ml의 농도로 하여 알파-아밀라아제(α-amylase), 베타-아밀라아제(β-amylase) 및 알파-글루코시다아제(α-glucosidase) 저해 활성을 측정한 결과, 꿀벌 유충의 열수 추출물에서 알파-글루코시다아제(α-glucosidase) 저해 활성에 의한 항당뇨 활성이 우수함을 확인하고, 에탄올 추출물에서 알파-아밀라아제(α-amylase) 저해 활성에 의한 항당뇨 활성이 우수함을 확인하였다. 또한, 꿀벌 번데기와 성충의 에탄올 추출물에서도 알파-아밀라아제(α-amylase) 저해 활성에 의한 항당뇨 활성이 우수함을 확인하였다. 특히, 성충의 경우, 열수 추출물의 에틸아세테이트 분획물에서 우수한 알파-아밀라아제(α-amylase) 저해 활성을 확인하였고, 에탄올 추출물의 헥센 분획물에서는 알파-아밀라아제(α-amylase), 베타-아밀라아제(β-amylase) 및 알파-글루코시다아제(α-glucosidase) 저해 활성이 모두 우수하였으며, 에틸아세테이트 분획물과 부탄올 분획물에서는 알파-아밀라아제(α-amylase) 및 알파-글루코시다아제(α-glucosidase) 저해 활성이 우수함을 확인하여, 이들 활성 추출물 및 분획물들을 항당뇨 활성 성분의 소재로 사용할 수 있을 것으로 기대되었다.In the present invention, bee larvae, pupae, adult hot water extract and ethanol extract at a concentration of 0.5mg/ml, alpha-amylase (α-amylase), beta-amylase (β-amylase) and alpha-glucosidase (α As a result of measuring the inhibitory activity of -glucosidase), it was confirmed that the anti-diabetic activity by the alpha-glucosidase inhibitory activity in the hot water extract of bee larvae was excellent, and the alpha-amylase (α-amylase) from the ethanol extract. It was confirmed that the anti-diabetic activity by the inhibitory activity is excellent. In addition, it was confirmed that the anti-diabetic activity due to the alpha-amylase inhibitory activity was also excellent in the ethanol extracts of bee pupae and adult insects. In particular, in the case of adults, excellent alpha-amylase (α-amylase) inhibitory activity was confirmed in the ethyl acetate fraction of the hot water extract, and in the hexene fraction of the ethanol extract, alpha-amylase (α-amylase) and beta-amylase (β-amylase) ) And alpha-glucosidase (α-glucosidase) inhibitory activity was excellent, and in ethyl acetate fraction and butanol fraction, alpha-amylase (α-amylase) and alpha-glucosidase (α-glucosidase) inhibitory activity was excellent. By confirming, it was expected that these active extracts and fractions could be used as a material for an anti-diabetic active ingredient.
본 발명의 꿀벌 추출물을 포함하는 항당뇨 활성 성분은 감압건조 및 동결건조, 또는 분무건조 등과 같은 통상적인 분말화 과정을 거쳐 분말로 제조될 수 있다. 꿀벌 추출물을 포함하는 항당뇨 활성 성분은 혈장 내의 다양한 분해효소에 분해되지 않으며, 100℃의 열처리와 pH 2의 인체 위 내의 pH에서도 활성을 유지한다.The anti-diabetic active ingredient comprising the bee extract of the present invention may be prepared as a powder through a conventional powdering process such as vacuum drying and lyophilization, or spray drying. Anti-diabetic active ingredients, including bee extract, are not degraded to various degrading enzymes in plasma, and maintain activity even at pH in the human stomach at a heat treatment of 100° C. and pH 2.
본 발명의 꿀벌 추출물은 강력한 α-amylase, β-amylase 및 α-glucosidase에 대한 전분분해효소 저해 활성을 나타내어, 제1형 당뇨병, 제2형 당뇨병 또는 당뇨병성 망막증, 당뇨병성 신증 등과 같은 당뇨 합병증의 예방 및 치료/개선과 관련되는 약학적 조성물 및 건강 기능 식품의 소재로 사용될 수 있다.The honey bee extract of the present invention shows potent protease inhibitory activity against potent α-amylase, β-amylase and α-glucosidase, so that diabetes complications such as type 1 diabetes, type 2 diabetes or diabetic retinopathy, diabetic nephropathy, etc. It can be used as a material for pharmaceutical compositions and dietary supplements related to prevention and treatment/improvement.
바람직한 구체예로서, 본 발명의 항당뇨 조성물은 약학적 조성물의 용도로서 적용될 수 있다. In a preferred embodiment, the anti-diabetic composition of the present invention can be applied as a pharmaceutical composition.
상기 약학적 조성물은 각각의 사용 목적에 맞게 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁제, 에멀젼, 시럽, 에어로졸 등의 경구 제형, 멸균 주사용액의 주사제 등 다양한 형태로 제형화하여 사용할 수 있으며, 경구 투여하거나 정맥 내, 복강 내, 피하, 직장, 국소 투여 등을 포함한 다양한 경로를 통해 투여될 수 있다. 이러한 약학적 조성물에는 추가적으로 담체, 부형제 또는 희석제 등이 더 포함될 수 있으며, 포함될 수 있는 적합한 담체, 부형제 또는 희석제의 예로는 락토오스, 덱스트로오스, 수크로오스, 솔비톨, 만니톨, 자일리톨, 에리쓰리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로스, 메틸 셀룰로스, 비정질 셀룰로스, 폴리비닐 피롤리돈, 물, 메틸하이드록시벤조에이트, 프로필하이드록시벤조에이트, 탈크, 마그네슘 스테아레이트 및 광물유 등을 들 수 있다. 또한, 본 발명의 약학적 조성물은 충전제, 항응집제, 윤활제, 습윤제, 향료, 유화제, 방부제 등을 추가로 더 포함할 수도 있다. The pharmaceutical composition is formulated in various forms such as oral formulations such as powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, injections of sterile injectable solutions, etc. It can be used orally or by various routes including intravenous, intraperitoneal, subcutaneous, rectal and topical administration. The pharmaceutical composition may further include a carrier, excipient or diluent, and examples of suitable carriers, excipients or diluents that may be included include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, Starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, amorphous cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil And the like. In addition, the pharmaceutical composition of the present invention may further include a filler, an anti-coagulant, a lubricant, a wetting agent, a fragrance, an emulsifier, a preservative, and the like.
본 발명의 약학적 조성물은 약제학적으로 유효한 양으로 투여한다. 본 발명에서, "약제학적으로 유효한 양"은 의학적 치료에 적용 가능한 합리적인 수혜/위험 비율로 질환을 치료하기에 충분한 양을 의미하며, 유효 용량 수준은 환자의 질환의 종류, 중증도, 약물의 활성, 약물에 대한 민감도, 투여 시간, 투여 경로 및 배출 비율, 치료 기간, 동시 사용되는 약물을 포함한 요소 및 기타 의학 분야에 잘 알려진 요소에 따라 결정될 수 있다. 본 발명의 약학적 조성물은 개별 치료제로 투여하거나 다른 치료제와 병용하여 투여될 수 있고, 종래의 치료제와 순차적으로 또는 동시에 투여될 수 있으며, 단일 또는 다중 투여될 수 있다. 상기한 요소들을 모두 고려하여 부작용 없이 최소한의 양으로 최대 효과를 얻을 수 있는 양을 투여하는 것이 중요하며, 이는 당업자에 의해 용이하게 결정될 수 있다. The pharmaceutical composition of the present invention is administered in a pharmaceutically effective amount. In the present invention, "a pharmaceutically effective amount" means an amount sufficient to treat a disease at a reasonable benefit/risk ratio applicable to medical treatment, and the effective dose level is the type of patient's disease, severity, drug activity, Sensitivity to the drug, time of administration, route of administration and rate of excretion, duration of treatment, factors including co-drugs and other factors well known in the medical arts. The pharmaceutical composition of the present invention may be administered as an individual therapeutic agent or in combination with other therapeutic agents, may be administered sequentially or simultaneously with a conventional therapeutic agent, and may be administered single or multiple. Considering all of the above factors, it is important to administer an amount that can achieve the maximum effect in a minimal amount without side effects, which can be easily determined by those skilled in the art.
본 발명의 약학적 조성물에서 항당뇨 활성을 갖는 성분의 유효량은 환자의 나이, 성별, 체중에 따라 달라질 수 있으며, 일반적으로는 체중 당 1 내지 5,000mg, 바람직하게는 100 내지 3,000mg을 매일 또는 격일 투여하거나 1일 1 내지 3회로 나누어 투여할 수 있다. 그러나, 투여 경로, 질병의 중증도, 성별, 체중, 연령 등에 따라서 증감될 수 있으므로 상기 투여량이 어떠한 방법으로도 본 발명의 범위를 한정하는 것은 아니다. 본 발명의 약학적 조성물은 다양한 경로를 통하여 대상에 투여될 수 있다. 투여의 모든 방식은 예상될 수 있는데, 예를 들면, 경구, 직장 또는 정맥, 근육, 피하, 자궁내 경막 또는 뇌혈관 내(intra-cerebroventricular) 주사에 의해 투여될 수 있다. 본 발명에서 "투여"는 임의의 적절한 방법으로 환자에게 소정의 물질을 제공하는 것을 의미하며, 본 발명의 약학적 조성물의 투여 경로는 목적 조직에 도달할 수 있는 한 일반적인 모든 경로를 통하여 경구 또는 비경구 투여될 수 있다. 또한, 본 발명의 조성물은 유효성분을 표적 세포로 전달할 수 있는 임의의 장치를 이용해 투여될 수도 있다. 본 발명에서 "대상"은, 특별히 한정되는 것은 아니지만, 예를 들어, 인간, 원숭이, 소, 말, 양, 돼지, 닭, 칠면조, 메추라기, 고양이, 개, 마우스, 쥐, 토끼 또는 기니아 피그를 포함하고, 바람직하게는 포유류, 보다 바람직하게는 인간을 의미한다. The effective amount of the component having anti-diabetic activity in the pharmaceutical composition of the present invention may vary depending on the patient's age, sex and body weight, and generally 1 to 5,000 mg per body weight, preferably 100 to 3,000 mg daily or every other day It can be administered or divided into 1 to 3 times a day. However, since the dosage may be increased or decreased depending on the route of administration, the severity of the disease, sex, weight, and age, the dosage is not limited to the scope of the present invention in any way. The pharmaceutical composition of the present invention can be administered to a subject through various routes. All modes of administration can be expected, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intrauterine dura mater or intra-cerebroventricular injection. In the present invention, "administration" means providing a predetermined substance to a patient in any suitable method, and the route of administration of the pharmaceutical composition of the present invention is oral or parenteral through all general routes as long as it can reach the target tissue. It can be administered orally. In addition, the composition of the present invention may be administered using any device capable of delivering an active ingredient to target cells. “Subject” in the present invention includes, but is not particularly limited to, humans, monkeys, cows, horses, sheep, pigs, chickens, turkeys, quails, cats, dogs, mice, mice, rabbits, or guinea pigs, for example. And, preferably, a mammal, more preferably a human.
바람직한 구체예로서, 본 발명의 항당뇨 조성물은 건강 기능 식품의 용도로서 적용될 수 있다. In a preferred embodiment, the anti-diabetic composition of the present invention can be applied as the use of dietary supplements.
본 발명의 항당뇨 활성이 우수한 유효성분을 포함하는 식품으로는, 예를 들어, 각종 식품류, 음료, 껌, 차, 비타민 복합제, 건강보조 식품류 등이 있고, 분말, 과립, 정제, 캡슐 또는 음료인 형태로 사용할 수 있다. 본 발명의 활성 성분은 일반적으로 전체 식품 중량의 0.01 내지 15중량%로 가할 수 있으며, 건강음료 조성물은 100 ml를 기준으로 0.02 내지 10g, 바람직하게는 0.3 내지 1g의 비율로 가할 수 있다. 본 발명의 건강 기능 식품은 지시된 비율로 필수 성분으로서 상기 화합물을 함유하는 것 외에 식품학적으로 허용 가능한 식품보조 첨가제, 예컨대, 천연 탄수화물 및 다양한 향미제 등을 추가 성분으로서 함유할 수 있다. 상기 천연 탄수화물의 예로는 포도당, 과당 등의 단당류, 말토오스, 수크로오스 등의 이당류 및 덱스트린, 시클로덱스트린 등의 다당류와 같은 통상적인 당 및 자일리톨, 소르비톨, 에리쓰리톨 등의 당알코올이 있다. 상기 향미제로는 타우마틴, 레바우디오시드 A, 글리시르히진, 사카린, 아스파르탐 등을 사용할 수 있다. 상기 향미제의 비율은 본 발명의 건강 기능 식품 100ml당 일반적으로 약 1 내지 20g, 바람직하게는 약 5 내지 12g을 사용한다. 상기 외에 본 발명의 건강 기능 식품은 여러 가지 영양제, 비타민, 광물, 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 중진제, 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알코올, 탄산음료에 사용되는 탄산화제 등을 함유할 수 있다. 그 밖에 본 발명의 건강 기능 식품은 천연 과일 주스 및 과일 주스 음료 및 야채 음료 등의 제조를 위한 과육을 함유할 수도 있다. 이러한 성분은 독립적으로 또는 조합하여 사용할 수 있다. 이러한 첨가제의 비율은 본 발명의 상기 활성 분획물 100 중량부 당 0.01 내지 약 20중량부의 범위에서 선택되는 것이 일반적이다.Foods containing the active ingredient having excellent anti-diabetic activity of the present invention include, for example, various foods, beverages, gums, teas, vitamin complexes, health supplements, etc., which are powders, granules, tablets, capsules, or beverages. Can be used in form. The active ingredient of the present invention can generally be added at 0.01 to 15% by weight of the total food weight, and the health drink composition can be added at a rate of 0.02 to 10 g, preferably 0.3 to 1 g, based on 100 ml. The dietary supplement of the present invention may contain, as an essential ingredient in the indicated proportions, the above compound as an essential ingredient, and may contain, as an additional ingredient, a food additive that is food-acceptable, such as natural carbohydrates and various flavoring agents. Examples of the natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, and sugars such as xylitol, sorbitol, and erythritol, and common sugars such as dextrin and cyclodextrin. As the flavoring agent, taumatin, rebaudioside A, glycyrrhizine, saccharin, aspartame, or the like can be used. The flavoring agent is generally used in an amount of about 1 to 20 g, preferably about 5 to 12 g per 100 ml of health functional food of the present invention. In addition to the above, the health functional food of the present invention includes various nutrients, vitamins, minerals, synthetic flavors and flavors such as natural flavors, colorants and neutralizers, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, and protective colloids It may contain a thickening agent, pH adjusting agent, stabilizer, preservative, glycerin, alcohol, carbonic acid used in carbonated beverages, and the like. In addition, the health functional food of the present invention may contain natural fruit juice and pulp for the production of fruit juice beverages and vegetable beverages. These ingredients can be used independently or in combination. The proportion of these additives is generally selected from 0.01 to about 20 parts by weight per 100 parts by weight of the active fraction of the present invention.
이하에서는 실시예를 통하여 본 발명을 더욱 상세하게 설명한다. 하기 실시예는 본 발명의 바람직한 일 구체예일 뿐이며, 본 발명의 권리범위가 하기 실시예의 범위로 한정되는 것은 아니다. Hereinafter, the present invention will be described in more detail through examples. The following examples are only preferred embodiments of the present invention, and the scope of the present invention is not limited to the following examples.
[실시예][Example]
실시예 1: 꿀벌 사육, 유충, 번데기, 성충의 동결건조 분말 조제 Example 1: Preparation of lyophilized powder of bee breeding, larvae, pupae, and adult
꿀벌은 집단사회를 구성하며, 여왕벌, 일벌, 숫벌로 구성되어 있으며, 유충, 번데기, 성충 단계를 거치게 된다. 따라서, 본 실시예에서는 다양한 봉분으로부터 꿀벌의 유충, 번데기, 성충을 각각 회수하고, 이를 -20℃로 급속냉동하여 사멸시킨 다음, -50℃에서 동결건조하였으며, 동결건조물을 막자사발을 이용하여 분말로 제조하였다(도 1). 제조된 분말의 색차는 표 1에 나타내었으며, 성충 분말은 유충 및 번데기와는 달리 낮은 명도 및 황색도와 높은 적색도를 나타내어 다른 시료들과 확연히 구분되었다. Bees make up a collective society, and are composed of queen bees, worker bees, and male bees, and go through the larva, pupa, and adult stages. Therefore, in this embodiment, the larvae, pupae, and adult of bees are recovered from various rods, respectively, and rapidly frozen to -20°C to kill them, then lyophilized at -50°C, and the lyophilisate is powdered using a mortar. It was prepared as (Fig. 1). The color difference of the prepared powder is shown in Table 1, and the adult powder was clearly distinguished from other samples by showing low brightness and yellowness and high redness, unlike larvae and pupae.
[표 1] 꿀벌의 유충, 번데기, 성충 분말의 색차 분석[Table 1] Color difference analysis of bee larvae, pupae and adult powder
실시예 2: 꿀벌 유충, 번데기, 성충 분말의 추출물 조제Example 2: Preparation of extracts of bee larvae, pupae and adult powder
실시예 1에서 제조된 꿀벌 유충, 번데기, 성충 분말을 대상으로 에탄올 추출물과 열수 추출물을 제조하였다. 에탄올 추출물의 경우, 각각의 시료에 대해 10배의 에탄올을 가하고, 상온에서 1회 추출한 후 추출액을 모아 필터링한 후, 감압 농축하여 분말로 제조하였다. 또한, 열수 추출물의 경우, 각각의 시료에 대해 10배의 증류수를 가하고, 100℃에서 1시간 추출한 후 상기와 동일한 방법으로 필터, 감압 농축하여 분말로 조제하였다. Ethanol extract and hot water extract were prepared for bee larvae, pupae and adult powder prepared in Example 1. In the case of ethanol extract, 10 times ethanol was added to each sample, and the extract was collected and filtered once at room temperature, and then concentrated under reduced pressure to prepare a powder. In addition, in the case of a hot water extract, 10 times distilled water was added to each sample, extracted at 100° C. for 1 hour, and then filtered and concentrated under reduced pressure in the same manner as above to prepare a powder.
실시예 3: 꿀벌 유충, 번데기, 성충 분말 추출물의 항당뇨 활성 평가Example 3: Evaluation of anti-diabetic activity of bee larvae, pupae and adult powder extract
실시예 2에서 제조된 꿀벌 유충, 번데기 및 성충의 열수 및 에탄올 추출물을 대상으로 항당뇨 활성을 평가하였으며, in-vitro α-amylase 저해 활성, β-amylase 저해 활성 및 α-glucosidase 저해 활성을 평가하여 나타내었다. Anti-diabetic activity was evaluated on the hot water and ethanol extracts of bee larvae, pupae and adult prepared in Example 2, and in-vitro α-amylase inhibitory activity, β-amylase inhibitory activity, and α-glucosidase inhibitory activity were evaluated. Shown.
먼저, α-amylase 저해 활성은 Lim 등이 보고한 방법(Lim, CS 등, 2005. J. Kor. Soc. Appl. Biol. Chem. 48: 103-108)을 수정하여 사용하였다. 시료 2.5μl와 50mM phosphate buffer(pH 6.8)로 희석한 α-amylase(0.25U/ml) 25μl를 혼합하여 37℃에서 10분간 1차 반응한 후, 0.5% soluble starch(Samchun Chemicals Co., Korea) 25μl를 가하여 37℃에서 10분간 2차 반응하였다. 이후, 2N acetic acid를 25μl를 가하여 반응을 정지시켰으며, 반응액에 0.75% KI/I2 용액 10μl를 가하여 발색하였다. 발색액은 540nm에서 흡광도를 측정하였으며, 각각의 실험은 3반복한 후 평균값을 구하여 다음의 식으로 저해율을 계산하였다.First, α-amylase inhibitory activity was used by modifying the method reported by Lim et al. (Lim, CS et al., 2005. J. Kor. Soc. Appl. Biol. Chem. 48: 103-108). 2.5 μl of sample and 25 μl of α-amylase (0.25 U/ml) diluted with 50 mM phosphate buffer (pH 6.8) were mixed and reacted first at 37° C. for 10 minutes, followed by 0.5% soluble starch (Samchun Chemicals Co., Korea) 25 µl was added and reacted for 2 minutes at 37°C for 10 minutes. Thereafter, 25 μl of 2N acetic acid was added to stop the reaction, and 10 μl of a 0.75% KI/I 2 solution was added to the reaction solution to develop color. The absorbance of the color developing solution was measured at 540 nm, and each experiment was repeated three times to obtain an average value, and the inhibition rate was calculated by the following equation.
저해율 (%) = 시료 첨가구 효소활성/대조구 첨가구 효소활성 x 100Inhibition rate (%) = Enzyme activity of sample addition/enzyme activity of control addition x 100
또한, β-amylase(4-alpha-D-glucan maltohydrolase) 저해 활성은 시료 2.5μl와 50mM phosphate buffer(pH 6.8)로 희석한 α-amylase(0.25U/ml) 25μl를 혼합하여 37℃에서 10분간 1차 반응한 후, 0.5% soluble starch(Samchun Chemicals Co., Korea) 25μl를 가하여 37℃에서 10분간 2차 반응한 후 100℃에서 5분간 가열하여 반응을 정지시켰으며, 반응액에 150μl의 DNS(3,5-dinitrosalicylic acid, Sigma Co., st. Louis, USA) 용액을 가하여 100℃에서 5분간 가열하여 발색한 후 상온에서 방냉하였다. 발색액은 540nm에서 흡광도를 측정하여 저해율을 계산하였다. In addition, β-amylase (4-alpha-D-glucan maltohydrolase) inhibitory activity was mixed with 2.5 μl of sample and 25 μl of α-amylase (0.25 U/ml) diluted with 50 mM phosphate buffer (pH 6.8) for 10 minutes at 37°C. After the first reaction, 25 μl of 0.5% soluble starch (Samchun Chemicals Co., Korea) was added and the second reaction was performed at 37° C. for 10 minutes, followed by heating at 100° C. for 5 minutes to stop the reaction, and 150 μl of DNS in the reaction solution (3,5-dinitrosalicylic acid, Sigma Co., st. Louis, USA) was added and heated at 100° C. for 5 minutes to develop color and then cooled to room temperature. In the color developing solution, the absorbance was measured at 540 nm to calculate the inhibition rate.
저해율 (%) = [1-(시료 첨가구 효소활성/대조구 첨가구 효소활성)] x 100Inhibition rate (%) = [1-(Enzyme activity in sample added/enzyme activity in control added)] x 100
마지막으로, α-glucosidase 저해 활성은 pNPG(p-nitrophenol glucoside; Sigma Co., USA)를 이용하여 평가하였으며, 생강 추출물 시료 2.5μl와 50mM Sodium acetate buffer(pH 5.6)로 희석한 α-glucosidase(0.25U/ml) 25μl를 혼합하여 37℃에서 10분간 1차 반응하고, 1mM pNPG 용액 25μl를 가하여 60℃에서 10분간 2차 반응하였다. 이후, 1M NaOH 25μl를 가하여 반응을 정지시키고, 405nm에서 흡광도를 측정하여 저해율을 계산하였다. Finally, α-glucosidase inhibitory activity was evaluated using pNPG (p-nitrophenol glucoside; Sigma Co., USA), α-glucosidase (0.25) diluted with 2.5 μl of ginger extract sample and 50 mM Sodium acetate buffer (pH 5.6). U/ml) 25 μl was mixed and reacted first at 37° C. for 10 minutes, and 25 μl of a 1 mM pNPG solution was added to perform a second reaction at 60° C. for 10 minutes. Then, 25 μl of 1M NaOH was added to stop the reaction, and the absorbance was measured at 405 nm to calculate the inhibition rate.
저해율 (%) = [1-(시료 첨가구 효소활성/대조구 첨가구 효소활성)] x 100Inhibition rate (%) = [1-(Enzyme activity in sample added/enzyme activity in control added)] x 100
[표 2] 꿀벌 유충, 번데기 및 성충 추출물의 항당뇨 활성[Table 2] Anti-diabetic activity of bee larvae, pupae and adult extracts
그 결과, 표 2에 나타낸 바와 같이, 에탄올 추출물이 열수 추출물보다 항당뇨 활성이 전반적으로 우수하였으며, 특히, 유충의 열수 추출물과 에탄올 추출물에서 각각 우수한 α-glucosidase 저해 활성 및 α-amylase 저해 활성을 확인하였고, 번데기와 성충의 경우, 에탄올 추출물에서 우수한 α-amylase 저해 활성을 확인하였다. As a result, as shown in Table 2, the ethanol extract had better overall anti-diabetic activity than the hot water extract. In particular, it was confirmed that the α-glucosidase inhibitory activity and α-amylase inhibitory activity were excellent in the hot water extract and the ethanol extract, respectively. In the case of pupae and adults, excellent α-amylase inhibitory activity was observed in ethanol extract.
실시예 4: 꿀벌 성충 추출물의 유기용매 분획물 제조 및 분획물의 성분 분석 Example 4: Preparation of organic solvent fraction of bee adult extract and analysis of components of fraction
상기 실시예 3의 실험 결과를 통해, 꿀벌 성충 열수 추출물과 에탄올 추출물을 대상으로 헥센, 에틸아세테이트, 부탄올로 순차적 유기용매 분획하였으며, 최종적으로 물 잔류물을 회수하였다. 에탄올 추출물과 열수 추출물 및 이들 추출물로부터 수득되는 유기용매 분획물들의 성분 분석으로 총 폴리페놀, 총 플라보노이드, 총 당 및 환원당 함량을 측정하였다. 총 폴리페놀 함량은 추출 검액 400μl에 50μl의 Folin-ciocalteau, 100μl의 Na2CO3 포화용액을 넣고 실온에서 1시간 방치한 후 725nm에서 흡광도를 측정하였다. 표준시약으로는 tannic acid를 사용하였다. 총 플라보노이드 함량은 각각의 시료를 18시간 메탄올 교반 추출하고, 여과한 추출 검액 400μl에 90% diethylene glycol 4ml를 첨가하고 다시 1N NaOH 40μl를 넣고 37℃에서 1시간 반응 후 420nm에서 흡광도를 측정하였다. 표준시약으로는 rutin을 사용하였다. 환원당은 DNS법으로, 총 당은 phenol-sulfuric acid법을 이용하여 정량하였다. 열수 추출물과 에탄올 추출물 및 이들의 유기용매 분획물의 분획 효율 및 성분 분석 결과는 표 3 및 표 4에 나타내었다. Through the experimental results of Example 3, the bee adult hot water extract and ethanol extract were subjected to sequential organic solvent fractionation with hexene, ethyl acetate, and butanol, and finally the water residue was recovered. The content of total polyphenol, total flavonoid, total sugar and reducing sugar was measured by analyzing the components of the ethanol extract and the hot water extract and organic solvent fractions obtained from these extracts. The total polyphenol content was 50 μl of Folin-ciocalteau, 100 μl of Na 2 CO 3 saturated solution in 400 μl of the extracted sample solution, and allowed to stand at room temperature for 1 hour, and absorbance was measured at 725 nm. As a standard reagent, tannic acid was used. The total flavonoid content was extracted by stirring each sample with methanol for 18 hours, adding 4 ml of 90% diethylene glycol to 400 μl of the filtered extraction sample, adding 40 μl of 1N NaOH again, and reacting at 37° C. for 1 hour to measure absorbance at 420 nm. Rutin was used as a standard reagent. The reducing sugar was quantified using the DNS method and the total sugar was phenol-sulfuric acid method. Fractional efficiency and component analysis results of the hot water extract and the ethanol extract and their organic solvent fractions are shown in Tables 3 and 4.
[표 3] 꿀벌 성충 에탄올 추출물 및 이의 순차적 유기용매 분획물의 성분 분석[Table 3] Component analysis of ethanol extract of bee adult and its sequential organic solvent fraction
표 3에 나타낸 바와 같이, 꿀벌 성충 에탄올 추출물의 51.4%는 헥센 분획으로 이행되어, 성충 에탄올 추출물의 대부분이 지질 성분임을 알 수 있었으며, 추출물 중, 물 잔류물이 39.6%, 부탄올 분획물이 6.4%, 에틸아세테이트 분획물은 4.4%를 차지하였다. 분획물의 총 폴리페놀 및 총 플라보노이드 함량 측정 결과, 부탄올 분획에서 가장 높은 35.0mg/g 및 0.4mg/g을 나타내었으며, 총당 및 환원당 함량은 물 잔류물에서 가장 높은 157.0mg/g 및 183.2mg/g을 나타내었다. As shown in Table 3, 51.4% of the bee adult ethanol extract was transferred to the hexene fraction, and it was found that most of the adult ethanol extract is a lipid component. Among the extracts, water residue was 39.6%, butanol fraction was 6.4%, The ethyl acetate fraction accounted for 4.4%. As a result of measuring the total polyphenol and total flavonoid content of the fractions, the highest 35.0mg/g and 0.4mg/g were found in the butanol fraction, and the total sugar and reducing sugar contents were the highest in the water residue, 157.0mg/g and 183.2mg/g. It was shown.
[표 4] 꿀벌 성충 열수 추출물 및 이의 순차적 유기용매 분획물의 성분 분석[Table 4] Component analysis of honey bee adult hot water extract and its sequential organic solvent fraction
또한, 표 4에 나타낸 바와 같이, 꿀벌 성충 열수 추출물의 71.4%는 부탄올 분획, 24.0%는 물 잔류물로 이행되어, 열수 추출물의 대부분은 수용성 성분임을 예상할 수 있었다. 분획물의 총 폴리페놀 및 총 플라보노이드 함량 측정 결과, 에틸아세테이트 분획에서 가장 높은 54.7mg/g 및 6.3mg/g을 나타내었으며, 총당 및 환원당 함량은 부탄올 분획에서 가장 높은 202.4mg/g 및 205.5mg/g을 나타내었다.In addition, as shown in Table 4, 71.4% of the honey bee adult hydrothermal extract was converted to a butanol fraction and 24.0% to a water residue, and most of the hot water extract could be expected to be water-soluble components. As a result of measuring the total polyphenol and total flavonoid content of the fraction, the ethyl acetate fraction showed the highest 54.7 mg/g and 6.3 mg/g, and the total sugar and reducing sugar content was highest in the butanol fraction, 202.4 mg/g and 205.5 mg/g. It was shown.
실시예 5: 꿀벌 성충 추출물로부터 수득된 유기용매 분획물의 항당뇨 활성 평가 Example 5: Evaluation of anti-diabetic activity of organic solvent fraction obtained from bee adult extract
꿀벌 성충 에탄올 추출물 및 열수 추출물의 분획물들을 이용하여 실시예 3의 in-vitro α-amylase 저해 활성, β-amylase 저해 활성 및 α-glucosidase 저해 활성 평가와 동일한 방법으로 항당뇨 활성을 측정하고, 그 결과를 다음 표 5 및 표 6에 나타내었다. Anti-diabetic activity was measured in the same manner as in-vitro α-amylase inhibitory activity, β-amylase inhibitory activity, and α-glucosidase inhibitory activity evaluation of Example 3 using fractions of bee adult ethanol extract and hot water extract. It is shown in Table 5 and Table 6 below.
[표 5] 꿀벌 성충 에탄올 추출물로부터 수득된 유기용매 분획물의 항당뇨 활성[Table 5] Anti-diabetic activity of organic solvent fraction obtained from ethanol extract of bee adult
그 결과, 표 5에 나타낸 바와 같이, 에탄올 추출물의 헥센 분획물, 에틸아세테이트 분획물 및 부탄올 분획물에서 모두 강력한 α-amylase 및 α-glucosidase 저해 활성을 확인하였으며, 특히, 헥센 분획물에서는 β-amylase 저해 활성도 매우 우수함으로 확인하였다. 따라서, 꿀벌 성충 에탄올 추출물의 헥센 분획물, 에틸아세테이트 분획물 및 부탄올 분획물은 제2형 당뇨병의 예방 및 치료에 이용 가능함을 예상할 수 있다.As a result, as shown in Table 5, the strong α-amylase and α-glucosidase inhibitory activities were confirmed in the hexene fraction, the ethyl acetate fraction, and the butanol fraction of the ethanol extract. In particular, the β-amylase inhibitory activity was also very good in the hexene fraction. It was confirmed by. Therefore, it can be expected that the hexene fraction, ethyl acetate fraction, and butanol fraction of the ethanol extract of bee adult can be used for prevention and treatment of type 2 diabetes.
[표 6] 꿀벌 성충 열수 추출물로부터 수득된 유기용매 분획물의 항당뇨 활성[Table 6] Anti-diabetic activity of organic solvent fractions obtained from honey bee adult hot water extract
또한, 표 6에 나타낸 바와 같이, 열수 추출물의 에틸아세테이트 분획물에서 강력한 α-amylase 및 α-glucosidase 저해 활성을 확인하였으며, 꿀벌 성충 열수 추출물의 에틸아세테이트 분획물은 제2형 당뇨병의 예방 및 치료에 이용 가능함을 예상할 수 있다.In addition, as shown in Table 6, a strong α-amylase and α-glucosidase inhibitory activity was confirmed in the ethyl acetate fraction of the hot water extract, and the ethyl acetate fraction of the bee adult hot water extract can be used for the prevention and treatment of type 2 diabetes. Can be expected.
실시예 6: 꿀벌 추출물 및 분획물의 혈장, 산 및 열 안정성 평가 Example 6: Plasma, acid and thermal stability evaluation of bee extracts and fractions
상기 실시예 2 및 실시예 4에서 얻은 꿀벌 유충, 번데기 및 성충의 에탄올 추출물과 열수 추출물 및 성충의 에탄올 추출물과 열수 추출물로부터 분획되는 분획물들을 대상으로 항당뇨 활성에 대한 혈장 안정성, 열 안정성 및 산 안정성을 확인하였다. 상기 추출물 및 분획물들은 100℃에서 1시간 열 처리, pH 2(0.01M HCl)에서의 1시간 처리, 혈장에서 1시간 처리시에도 α-amylase, β-amylase 및 α-glucosidase 저해 활성의 심각한 소실 없이 우수한 활성을 유지하였다. Plasma stability, thermal stability, and acid stability against anti-diabetic activity for ethanol extracts of honey bee larvae, pupae, and adult obtained in Examples 2 and 4 and fractions fractionated from ethanol extracts and hot water extracts of adults. Was confirmed. The extracts and fractions were heat treated at 100° C. for 1 hour, treated for 1 hour at pH 2 (0.01M HCl), and treated with plasma for 1 hour without significant loss of α-amylase, β-amylase and α-glucosidase inhibitory activity. Excellent activity was maintained.
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