JP3559482B2 - Lipase inhibitor - Google Patents

Lipase inhibitor Download PDF

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Publication number
JP3559482B2
JP3559482B2 JP29932999A JP29932999A JP3559482B2 JP 3559482 B2 JP3559482 B2 JP 3559482B2 JP 29932999 A JP29932999 A JP 29932999A JP 29932999 A JP29932999 A JP 29932999A JP 3559482 B2 JP3559482 B2 JP 3559482B2
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Prior art keywords
lipase
lipase inhibitor
extract
clove
present
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Expired - Fee Related
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JP2001120237A (en
Inventor
尚人 岩田
健一 石渡
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Fancl Corp
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Fancl Corp
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  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Food Preservation Except Freezing, Refrigeration, And Drying (AREA)
  • Seeds, Soups, And Other Foods (AREA)
  • Medicines Containing Plant Substances (AREA)

Description

【0001】
【発明の属する技術分野】
本発明は、リパーゼ阻害剤に関し、更に詳しくは、生体内での脂質の消化吸収に関与する膵リパーゼを有効に阻害して肥満・高脂血の予防および抑制することができるとともに、リパーゼに起因する食品等の劣化や悪臭の防止、さらには、リパーゼに起因する皮膚炎などの疾患の防止・予防に利用できるリパーゼ阻害剤に関する。
【0002】
【従来の技術】
近年、日本人の食事は高カロリー化が進み、高脂血症、動脈硬化、糖尿病などの生活習慣病の要因となる肥満を引き起こしている。その治療および予防法としては、食事療法や運動療法などが提案され実施されている。食事療法においては、脂肪が食品成分中もっとも高カロリーであり、その減量が肥満の予防に効果的と考えられている。しかしながら、食事制限は過度のストレスがかかり日常生活で継続することは困難であり、消化吸収抑制作用を有する食品が開発されている。
【0003】
食事中の脂肪は、膵リパーゼによって一旦分解されて小腸から吸収される。このため、膵リパーゼを阻害して余剰の脂肪を排泄させる薬剤としてテトラヒドロリプスタチン(Biochem.J.,256,357,1988)が開発されている。このリパーゼ阻害剤は副作用の報告例が多く、より安全性の高いリパーゼ阻害剤が求められ、植物等に含まれるリパーゼ阻害作用の応用も報告されている。例えば、果実やその種子の抽出物(明治大学農学部研究報告,69,16,1985)、大豆タンパク質(Agric.Biol.Chem.,37,1225,1973)、穀類タンパク質(Nutrition Reports Int.,32,1107,1985)、大根種子タンパク質(日本食品工業学会誌,35,430,1988)、ハーブ(Biosci.Biotech.Biochem.,56,1478,1992)、小麦(New Food Industry,40,65,1997)、海藻類(Lipids,34,441,1999)、ウーロン茶の成分(特開平1−102022)、ピーマン、かぼちゃ、しめじ、まいたけ、ひじき、緑茶、紅茶、ウーロン茶の水抽出物(特開平3−219872)、ブドウ種子、カキ葉、プーアル茶など12種の植物抽出物(特開平9−227398)、シソ科植物(特開平10−262606)、タンニン類では、縮合型タンニンとして(Br.J.Nutr.,60,275,1988)(特開平9−291039)、カワラケツメイに含まれる特定タンニン(特開平8−259557)、エピガロカテキンガレート(特開平3−228664)のリパーゼ阻害作用が報告されている。
【0004】
さらに、生薬類に関しては、微生物由来リパーゼに対するものとして、シャクヤク、オオレン、オオバク、ボタンピ、ゲンノショウコ、茶などの14種の抽出物(特開昭64−90131)、ドッカツ、リョウキョウ、ビンロウシなど6種の抽出物(特開平5−255100)が開示されている。また、ヘミセルロースや小麦ふすまなど(J.Food Sci.,49,956,1984)(Am.J.Clin.Nutr.,42,629,1985)、大豆種子のフォスファチジルコリン(明治大学農学部研究報告,73,9,1986)、ミオイノシトール(J.Food Sci.,53,250,1988)、フラボノイドに関しては、ルテオリン、アピゲニン、ケンフェロール、ケルセチン、ミリセチン(特開平7−61927)、柑橘類に多く含まれるヘスペリジン(Biosci.Biotech.Biochem.,61,102,1997)のリパーゼ阻害活性が報告されている。しかし、これらの先行技術はクローブ抽出物のリパーゼ阻害作用については記載がない。
【0005】
【発明が解決しようとする課題】
本発明は、生体内で脂肪の消化吸収に関与する膵リパーゼに対して強い阻害作用を示し、肥満や高脂血の予防や抑制に寄与するとともに、食品等の劣化や悪臭発生の防止に利用できる安全性の高いリパーゼ阻害剤およびこれを添加した食品組成物を提供するものである。
【0006】
【課題を解決する手段】
天然の香辛料は種々の薬効が知られており、長年食品として利用されてきたことから安全性は極めて高い。これらの香辛料の抽出物より膵リパーゼを阻害するものを鋭意探索した。その結果、クローブに代表される香辛料およびその抽出物が優れた膵リパーゼ阻害作用を有することを見出した。即ち、本発明は、クローブのエタノール抽出物を有効成分とするリパーゼ阻害剤、及びクローブのエタノール抽出物を含有してなる食品組成物である。
【0007】
【発明の実施の形態】
クローブ、例えばSyzygium aromaticumの開花前の蕾は強い香りを持ち、殺虫剤、鎮痛剤、胃腸薬等に用いられる。
レモングラス、例えばCymbopogon citratusの葉は腹痛、下痢、頭痛、発熱等の治療に使われる。
シナモン、例えばCinnamomum verumの葉は吐き気や高血圧の治療に用いる。
オールスパイス、例えばPimenta dioicaの未成熟の漿果は悪寒を抑える。
【0008】
本発明の植物は乾燥物、乾燥粉末あるいは植物そのものを使用できる。
本発明の抽出物は、例えば、植物またはその乾燥物を粉砕、破砕、裁断し、これに極性あるいは非極性の溶媒を加えることによって得られる。本発明の抽出物は、そのままでも使用できるが、単独あるいは適当な担体とともに噴霧乾燥、凍結乾燥、減圧乾燥、流動乾燥等の方法により粉末状あるいはペースト状にして使用することができる。
これらの植物および抽出物は、高いリパーゼ阻害活性を有し、脂肪の消化吸収の阻害に基づく肥満の抑制および予防に利用可能で、また、リパーゼによる食品等の劣化や悪臭の発生防止に利用できる。
【0009】
【実施例】
以下に実施例を挙げて本発明を詳細に説明するが、本発明はこれらに限定されるものではない。
【0010】
実施例1
乾燥した表1に示す植物を粉砕し、粉砕物に対して10倍量の蒸留水を加え100℃にて1時間加熱した。これを遠心分離の後ろ過し抽出物とした。
クローブ粉末についてはエタノール抽出も行った。クローブ粉末に10倍量のエタノールを加え、一晩放置した。これをろ過し、減圧乾固の後蒸留水に再溶解し試験に用いた。
【0011】
リパーゼ阻害活性の測定は次のようにして行った。
基質に三酪酸ジメルカプロール(BALB)を使用し、生成するジメチルカプロールと5,5‘−ジチオビス(2−ニトロ安息香酸)(DTNB)との反応によって生じる5−チオ−2−ニトロ安息香酸の定量を412nmの吸光度を測定することによって行った。
抽出物50μl、ブタ膵リパーゼ(30μg/ml、Sigma社)50μl、10mg/mlDTNB,3.48m/mlフェニルメチルフルフォニルフルオライド(PMSF)を含む0.1Mトリス緩衝液(pH8.5)350μlを30℃で5分間インキュベートした後、6.69mg/mlBALB,5.73mg/mlラウリル硫酸ナトリウムを含むエタノール溶液50μlを加え30℃で30分間インキュベートした。アセトン1mlを加え反応を停止させ、412nmの吸光度を測定した。結果を表−1に示す。
【0012】
【表1】

Figure 0003559482
【0013】
【発明の効果】
このように、本発明によるリパーゼ阻害剤は、リパーゼ阻害活性がきわめて高い。またこの効果は、クローブのエタノール抽出物に顕著であった。 [0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a lipase inhibitor, and more specifically, it is possible to effectively inhibit pancreatic lipase involved in digestion and absorption of lipids in a living body to prevent and suppress obesity and hyperlipidemia, The present invention relates to a lipase inhibitor that can be used for preventing deterioration of foods and the like and odor, and for preventing and preventing diseases such as dermatitis caused by lipase.
[0002]
[Prior art]
In recent years, the diet of Japanese people has been increasing in calories, causing obesity which is a cause of lifestyle-related diseases such as hyperlipidemia, arteriosclerosis, and diabetes. Diet therapy, exercise therapy and the like have been proposed and implemented as treatment and prevention methods. In diet, fat is the highest calorie in food components, and its weight loss is considered to be effective in preventing obesity. However, dietary restrictions are excessively stressful and difficult to continue in daily life, and foods having a digestive absorption inhibitory effect have been developed.
[0003]
Fat in the diet is once broken down by pancreatic lipase and absorbed from the small intestine. For this reason, tetrahydrolipstatin (Biochem. J., 256, 357, 1988) has been developed as a drug that inhibits pancreatic lipase and excretes excess fat. There are many reports of side effects of this lipase inhibitor, and a lipase inhibitor with higher safety has been demanded, and application of the lipase inhibitory action contained in plants and the like has also been reported. For example, extracts of fruits and their seeds (Research Report, Faculty of Agriculture, Meiji University, 69, 16, 1985), soybean protein (Agric. Biol. Chem., 37, 1225, 1973), cereal protein (Nutrition Reports Int., 32, 1107, 1985), radish seed protein (Japanese Journal of Food Industry, 35, 430, 1988), herb (Biosci. Biotech. Biochem., 56, 1478, 1992), wheat (New Food Industry, 40, 65, 1997). , Seaweeds (Lipids, 34,441, 1999), components of oolong tea (JP-A-1-102022), peppers, pumpkin, shimeji, maitake, hijiki, green tea, black tea, water extract of oolong tea (JP-A-3-219872) , Grape seed , Oyster leaf, Puer tea, etc., 12 kinds of plant extracts (Japanese Patent Application Laid-Open No. 9-227398), Labiatae plants (Japanese Patent Application Laid-Open No. 10-262606), and tannins as condensed tannins (Br. J. Nutr., 60, 275, 1988) (Japanese Unexamined Patent Publication No. 9-291039), and the lipase inhibitory effects of specific tannin (Japanese Unexamined Patent Application Publication No. 8-259557) and epigallocatechin gallate (Japanese Unexamined Patent Application Publication No. 3-228664) contained in Kawataketsumei are reported.
[0004]
Further, as for crude drugs, 14 kinds of extracts such as peonies, oren, psyllium, peanuts, genoshoko, tea and the like (Japanese Patent Application Laid-Open No. 64-90131), 6 kinds such as Dokkatsu, Ryokyo, Amberjack, etc., against microbial lipases (JP-A-5-255100) is disclosed. In addition, hemicellulose and wheat bran (J. Food Sci., 49, 956, 1984) (Am. J. Clin. Nutr., 42, 629, 1985), phosphatidylcholine in soybean seeds (Meiji University Agricultural Science Research Report, 73, 9 , 1986), myo-inositol (J. Food Sci., 53, 250, 1988) and flavonoids include luteolin, apigenin, kaempferol, quercetin, myricetin (Japanese Patent Laid-Open No. 7-61927), and hesperidin (Biosci. Biochem., 61, 102, 1997). However, these prior arts do not describe the lipase inhibitory effect of the clove extract.
[0005]
[Problems to be solved by the invention]
INDUSTRIAL APPLICABILITY The present invention has a strong inhibitory effect on pancreatic lipase involved in digestion and absorption of fat in a living body, contributes to prevention and suppression of obesity and hyperlipidemia, and is used for prevention of deterioration of foods and the generation of bad smell It is intended to provide a highly safe lipase inhibitor and a food composition containing the same.
[0006]
[Means to solve the problem]
Natural spices are known for their various medicinal effects and have been used as foods for many years, so their safety is extremely high. From the extracts of these spices, those that inhibit pancreatic lipase were intensively searched. As a result, they have found that spices represented by cloves and extracts thereof have an excellent pancreatic lipase inhibitory action. That is, the present invention is a food composition comprising a lipase inhibitor containing an ethanol extract of clove as an active ingredient, and an ethanol extract of clove.
[0007]
BEST MODE FOR CARRYING OUT THE INVENTION
Cloves, for example, buds before flowering of Syzygium aromaticum have a strong aroma and are used as insecticides, analgesics, gastrointestinal drugs and the like.
Lemongrass, such as Cymbopogon citratus leaves, is used to treat abdominal pain, diarrhea, headache, fever and the like.
Cinnamon, eg, leaves of Cinnamomum verum, are used to treat nausea and hypertension.
Immature berries of allspice, such as Pimenta dioica, control chills.
[0008]
The plant of the present invention can use a dried product, a dried powder or the plant itself.
The extract of the present invention can be obtained, for example, by pulverizing, crushing, or cutting a plant or a dried product thereof and adding a polar or nonpolar solvent thereto. The extract of the present invention can be used as it is, but can be used alone or together with a suitable carrier in the form of a powder or paste by a method such as spray drying, freeze drying, reduced pressure drying, and fluid drying.
These plants and extracts have a high lipase inhibitory activity and can be used for suppressing and preventing obesity based on inhibition of digestion and absorption of fat, and can also be used for preventing degradation of foods and the like and odor generation due to lipase. .
[0009]
【Example】
Hereinafter, the present invention will be described in detail with reference to Examples, but the present invention is not limited thereto.
[0010]
Example 1
The dried plants shown in Table 1 were pulverized, and a 10-fold amount of distilled water was added to the pulverized material, followed by heating at 100 ° C. for 1 hour. This was filtered after centrifugation to obtain an extract.
The clove powder was also subjected to ethanol extraction. A 10-fold amount of ethanol was added to the clove powder and left overnight. This was filtered, dried under reduced pressure, then redissolved in distilled water and used for the test.
[0011]
The lipase inhibitory activity was measured as follows.
Using dimercaprol tributyrate (BALB) as a substrate, 5-thio-2-nitrobenzoic acid produced by the reaction of the resulting dimethylcaprol with 5,5′-dithiobis (2-nitrobenzoic acid) (DTNB) Was determined by measuring the absorbance at 412 nm.
50 μl of extract, 50 μl of porcine pancreatic lipase (30 μg / ml, Sigma), 350 μl of 0.1 M Tris buffer (pH 8.5) containing 10 mg / ml DTNB, 3.48 m / ml phenylmethyl fluphonyl fluoride (PMSF) Was incubated at 30 ° C. for 5 minutes, 50 μl of an ethanol solution containing 6.69 mg / ml BALB and 5.73 mg / ml sodium lauryl sulfate was added, and the mixture was incubated at 30 ° C. for 30 minutes. 1 ml of acetone was added to stop the reaction, and the absorbance at 412 nm was measured. The results are shown in Table 1.
[0012]
[Table 1]
Figure 0003559482
[0013]
【The invention's effect】
Thus, the lipase inhibitor according to the present invention has extremely high lipase inhibitory activity. This effect was remarkable in the ethanol extract of clove.

Claims (2)

クローブのエタノール抽出物を有効成分とするリパーゼ阻害剤。A lipase inhibitor comprising an ethanol extract of clove as an active ingredient. クローブのエタノール抽出物を含有することを特徴とする食品組成物。 A food composition comprising an ethanol extract of clove .
JP29932999A 1999-10-21 1999-10-21 Lipase inhibitor Expired - Fee Related JP3559482B2 (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI329516B (en) * 2000-12-12 2010-09-01 Kaneka Corp Composition for preventing or ameliorating multiple risk factor syndromes and visceral fat-type obesity
CN1406131A (en) * 2000-12-25 2003-03-26 株式会社资生堂 Sympathetic-activating perfume composition
JP5110673B2 (en) * 2001-07-10 2012-12-26 丸善製薬株式会社 Lipase inhibitor
JP2004238310A (en) * 2003-02-05 2004-08-26 Ichimaru Pharcos Co Ltd Cosmetic composition, drink or food
US20060013903A1 (en) * 2004-07-16 2006-01-19 Timothy Romero Dietary supplements containing extracts of cinnamon and methods of using same to promote weight loss
WO2007111242A1 (en) 2006-03-24 2007-10-04 Rohto Pharmaceutical Co., Ltd. Ameliorating agent for metabolic syndrome
JP2011051901A (en) * 2009-08-31 2011-03-17 Riyo Miura alpha-GLUCOSIDASE INHIBITOR
JP5596654B2 (en) * 2011-10-14 2014-09-24 丸善製薬株式会社 Lipase inhibitor
JP6324458B2 (en) * 2016-09-21 2018-05-16 一丸ファルコス株式会社 Kinesin inhibitor

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