JP2003095941A - Sugar digestion enzyme inhibitor, hyperglycemia inhibitor, therapeutic or prophylactic agent for obesity, therapeutic or prophylactic agent for diabetes, and healthy food and drink - Google Patents

Sugar digestion enzyme inhibitor, hyperglycemia inhibitor, therapeutic or prophylactic agent for obesity, therapeutic or prophylactic agent for diabetes, and healthy food and drink

Info

Publication number
JP2003095941A
JP2003095941A JP2001294640A JP2001294640A JP2003095941A JP 2003095941 A JP2003095941 A JP 2003095941A JP 2001294640 A JP2001294640 A JP 2001294640A JP 2001294640 A JP2001294640 A JP 2001294640A JP 2003095941 A JP2003095941 A JP 2003095941A
Authority
JP
Japan
Prior art keywords
baroneaic
acid
inhibitor
sugar
therapeutic
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2001294640A
Other languages
Japanese (ja)
Inventor
Hiroko Suzuki
裕子 鈴木
Iwao Sakane
巌 坂根
Hirokazu Hosoyama
広和 細山
Akio Sugimoto
明夫 杉本
Kozo Nagata
幸三 永田
Takami Tsunoda
隆巳 角田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ito En Ltd
Original Assignee
Ito En Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ito En Ltd filed Critical Ito En Ltd
Priority to JP2001294640A priority Critical patent/JP2003095941A/en
Publication of JP2003095941A publication Critical patent/JP2003095941A/en
Pending legal-status Critical Current

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Non-Alcoholic Beverages (AREA)
  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

PROBLEM TO BE SOLVED: To provide new applications of a specific component derived from an extract of Lagerstroemia speciosa, more precisely, to provide new applications based on α-amylase inhibitory activity of the component. SOLUTION: A sugar digestion enzyme inhibitor containing valoneaic acid as an active ingredient is proposed based on such information that the valoneaic acid obtained by subjecting the extract of the Lagerstroemia speciosa to separation through liquid-liquid partition, column chromatography, or the like, has the excellent α-amylase inhibitory activity. Because the α-amylase is such an enzyme as especially effective for breaking α-1,4 bonds of starch and glycogen, the inhibitor prevents digestion and absorption of the starch and the glycogen. Therefore, rapid increase in a blood sugar level after a meal is prevented and secretion of insulin is controlled by the inhibitor, so that the inhibitor is effective for treating and preventing diabetes, and inhibiting obesity.

Description

【発明の詳細な説明】Detailed Description of the Invention

【0001】[0001]

【産業上の利用分野】本発明は、バナバに由来する或る
特定成分の新たな用途、詳しくは糖質消化酵素活性、血
糖値上昇、肥満、糖尿病等に関する新たな用途に関す
る。
BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a new use of a specific component derived from banaba, more specifically to a new use relating to carbohydrate digestive enzyme activity, elevated blood sugar level, obesity, diabetes and the like.

【0002】[0002]

【従来の技術及び発明が解決しようとする課題】バナバ
(Lagerstroemia speciosa(L.)Pers.)は、フトモモ
目ミソハギ科に属し、オオバナサルスベリともいわれる
熱帯アジアに分布するサルスベリの一種である。この葉
や花を煮た汁は、フィリピンなどでは古くから糖尿病の
治療薬として飲用され、最近では我が国でもその糖尿病
治療効果や血糖値抑制効果が着目され、健康茶などとし
て飲用する人が増えている。
BACKGROUND OF THE INVENTION Banaba (Lagerstroemia speciosa (L.) Pers.) Is a kind of crape myrtle that is distributed in tropical Asia and belongs to the family Myrtaceae, also known as L. persica. This boiled juice of leaves and flowers has long been taken as a therapeutic drug for diabetes in the Philippines and other countries, and recently in Japan, attention has been paid to its diabetes therapeutic effect and blood sugar level suppressing effect, and the number of people who drink it as health tea etc. is increasing. There is.

【0003】バナバの薬理効果については、1940年
代には既にバナバの乾燥葉の煎出汁を正常家兎に投与し
た結果、乾燥葉1〜2g/体重1kgの投与量で血糖値
を16〜49mg/dl下げることができたという報告
がなされている(F.Garcia:On the hypoglycemic effe
ct of decoction of Lagerstroemia speciosa(Banaba)
J.Philip.Med.Assoc. 20,395(1940))。
Regarding the pharmacological effect of banaba, in the 1940s, as a result of administration of the decoction of dried banaba leaves to normal rabbits, the blood glucose level was 16 to 49 mg / dose at a dose of 1 to 2 g of dried leaves / kg of body weight. It has been reported that dl could be lowered (F. Garcia: On the hypoglycemic effe
ct of decoction of Lagerstroemia speciosa (Banaba)
J.Philip.Med.Assoc. 20,395 (1940)).

【0004】また、特開平5−310587号は、II型
糖尿病マウスにバナバ抽出粉末エキスを3%混合した食
餌を1週間投与し、その後バナバ抽出粉末エキスを5%
混合した食餌で3週間飼育した結果、バナバ抽出粉末エ
キス摂取群の血糖値が有意に抑制されたことを開示し、
特開平9−227398号は、バナバ葉乾燥粉砕物に1
00倍量50%エタノールを加え、1時間加熱還流して
なる抽出液を減圧濃縮して得た試料、すなわちバナバ葉
抽出物がアミラーゼ及びリパーゼの阻害効果を発揮した
ことを開示すると共に、バナバ葉抽出物が肥満、糖尿
病、高脂血症、動脈硬化症、ニキビ、皮膚炎等の治療・
予防に有用である旨の知見を開示している。
Further, JP-A-5-310587 discloses that a type II diabetic mouse is administered with a diet in which 3% of Banaba extract powder extract is mixed for 1 week, and then 5% of Banaba extract powder extract is administered.
As a result of breeding the mixed diet for 3 weeks, it was disclosed that the blood sugar level of the group that ingested the banaba extract powder extract was significantly suppressed,
Japanese Unexamined Patent Publication No. 9-227398 describes a banaba leaf dry pulverized product
It is disclosed that a sample obtained by concentrating under reduced pressure an extract obtained by adding 00 times amount of 50% ethanol and heating and refluxing for 1 hour, that is, a banaba leaf extract exerted an inhibitory effect on amylase and lipase, and banaba leaf. Extracts for treatment of obesity, diabetes, hyperlipidemia, arteriosclerosis, acne, dermatitis, etc.
It discloses the knowledge that it is useful for prevention.

【0005】バナバの血糖低下作用の主な作用機序につ
いては、上記特開平9−227398号のほかにも、バ
ナバにデンプンの消化酵素であるα―アミラーゼの酵素
活性阻害作用があることが確認された(日本農芸化学会
誌、1997 Mar.71)結果、糖質消化酵素の阻
害作用によって摂取した飲食物中の糖類分解を阻害し、
腸管からの単糖吸収を遅延させて血糖値の上昇を抑制す
るという作用機序が確からしくなってきた。ちなみに、
医療の現場では消化酵素阻害剤は既に抗肥満症剤や抗糖
尿病剤などとして使われている。
Regarding the main mechanism of the blood sugar lowering action of banaba, it was confirmed that banaba has an enzyme activity inhibiting action of α-amylase which is a starch digestive enzyme, in addition to the above-mentioned JP-A-9-227398. As a result (Journal of the Japanese Society of Agricultural Chemistry, 1997 Mar. 71), it inhibits the saccharide decomposition in the ingested food and drink by the inhibitory action of the carbohydrate digestive enzyme,
The mechanism of action that delays the absorption of monosaccharides from the intestinal tract and suppresses the rise in blood glucose levels has become uncertain. By the way,
In the medical field, digestive enzyme inhibitors are already used as antiobesity agents and antidiabetic agents.

【0006】そこで本発明者は、代表的な消化酵素の一
つであるα-アミラーゼの阻害活性を指標にバナバ抽出
物について精査した結果、バナバ抽出物中の或る特定成
分に強い活性を見出し、かかる知見に基づいて本発明を
想到したものである。
[0006] Therefore, the present inventor investigated the banaba extract with an inhibitory activity of α-amylase, which is one of the typical digestive enzymes, as a result, and found that a certain specific component in the banaba extract had a strong activity. The present invention has been accomplished based on such knowledge.

【0007】[0007]

【課題を解決するための手段】バナバ抽出成分のαアミ
ラーゼ阻害活性について精査した結果、バナバ抽出物を
液液分配並びにカラムクロマトグラフィー等によって分
離して得られた画分に優れたαアミラーゼ阻害活性を見
出すと共に、当該画分がバロネア酸であることを同定
し、かかる知見に基づいて本発明を想到するに至ったも
のである。
[Means for Solving the Problems] As a result of detailed examination of α-amylase inhibitory activity of banaba extract component, α-amylase inhibitory activity excellent in fractions obtained by separating banaba extract by liquid-liquid partitioning and column chromatography The present invention has led to the discovery of the present invention, identification of the relevant fraction as baroneaic acid, and the present invention based on such findings.

【0008】すなわち、本発明は、バロネア酸を有効成
分として含有する糖質消化酵素阻害剤を提案するもので
ある。
That is, the present invention proposes a sugar digestive enzyme inhibitor containing baroneaic acid as an active ingredient.

【0009】バロネア酸は、次の式で表される。Baroneaic acid is represented by the following formula.

【0010】[0010]

【化2】 [Chemical 2]

【0011】また、バロネア酸配糖体すなわちバロネア
酸を基本骨格とする配糖体は、体内においてバロネア酸
に分解するため、バロネア酸配糖体を有効成分として含
有する糖質消化酵素阻害剤も同様の効果を発揮するもの
と考えることができる。
[0011] Further, baroneaic acid glycosides, that is, glycosides having a basic skeleton of baroneaic acid, are decomposed into baroneaic acid in the body, so that a sugar digestive enzyme inhibitor containing baroneaic acid glycosides as an active ingredient is also available. It can be considered that the same effect is exhibited.

【0012】そこで本発明は、バロネア酸配糖体を有効
成分として含有する糖質消化酵素阻害剤を提案する。こ
の際のバロネア酸配糖体は、次の式(式中、R1〜R4
の少なくともいずれか一つが糖であって、R1〜R4の
残りが水素原子、炭素数1以上を有する官能基、糖のい
ずれかである。)で表される。
Therefore, the present invention proposes a sugar digestive enzyme inhibitor containing baronea acid glycoside as an active ingredient. At this time, the baroneaic acid glycoside has the following formula (wherein R1 to R4
Is a sugar, and the rest of R1 to R4 is a hydrogen atom, a functional group having 1 or more carbon atoms, or a sugar. ).

【0013】[0013]

【化3】 [Chemical 3]

【0014】本発明の糖質消化酵素阻害剤は、糖質消化
酵素、特にα―アミラーゼの酵素活性を阻害する。α−
アミラーゼは、デンプン(アミロース、アミロペクチ
ン)、グリコーゲンのα−1,4結合を任意に切断する
酵素である。この消化酵素の活性を阻害してこれらの消
化吸収を阻害することにより、食後血糖値の急激な上昇
を抑制し、インスリンの分泌も抑えることができ、糖尿
病の治療予防、肥満防止に効果を発揮する。そこで本発
明は、バロネア酸、バロネア酸配糖体のいずれか、或い
はこれらの混合物を有効成分として含有する血糖値上昇
抑制剤、肥満治療予防剤、糖尿病治療予防剤をも提案す
る。
The carbohydrate digestive enzyme inhibitor of the present invention inhibits the enzymatic activity of a carbohydrate digestive enzyme, particularly α-amylase. α-
Amylase is an enzyme that arbitrarily cleaves α-1,4 bonds of starch (amylose, amylopectin) and glycogen. By inhibiting the activity of this digestive enzyme and inhibiting its digestion and absorption, it is possible to control the rapid rise in postprandial blood glucose level and also the secretion of insulin, which is effective in the treatment and prevention of diabetes and the prevention of obesity. To do. Therefore, the present invention also proposes a blood glucose elevation inhibitor, an obesity treatment preventive agent, a diabetes treatment preventive agent, which contains any one of baroneaic acid and baroneaic acid glycoside or a mixture thereof as an active ingredient.

【0015】本発明の糖質消化酵素阻害剤、血糖値上昇
抑制剤、肥満治療予防剤、糖尿病治療予防剤は、上記の
効果以外にも、栄養過多を原因とする心筋梗塞、動脈硬
化、高血圧等の心臓管系の疾病や、ニキビ、吹出物等の
皮膚系の疾病、その他の疾病の治療及び予防に効果を発
揮することが期待できる。また、安全性の面でも有用で
ある。バナバはフィリピンなどにおいて昔から常用され
ているから安心して摂取することができ、特に継続摂取
に適している。よって、上記疾病の根本治療のための長
期摂取や予防のための日常摂取のほか、ダイエット食品
や体質改善飲食品などとしても有用である。また、ヒト
以外の動物にも有効であるから、ペットや家畜その他の
動物のための血糖値上昇抑制剤、糖尿病治療・予防剤、
肥満予防剤、ダイエットペットフード、ダイエット飼料
などの素材、原料としても有用である。
In addition to the above-mentioned effects, the carbohydrate digestive enzyme inhibitor, blood sugar level elevation inhibitor, obesity treatment preventive agent, diabetes treatment preventive agent of the present invention have myocardial infarction, arteriosclerosis and hypertension caused by overnutrition. It can be expected to be effective in treating and preventing cardiovascular diseases such as the following, skin diseases such as acne and pimples, and other diseases. It is also useful in terms of safety. Banaba can be safely taken because it has been used regularly in the Philippines and elsewhere, and is particularly suitable for continuous intake. Therefore, in addition to long-term intake for the basic treatment of the above diseases and daily intake for prevention, it is also useful as a diet food, a physical condition-improving food and drink, and the like. In addition, since it is also effective for animals other than humans, blood sugar elevation suppressants for pets, livestock, and other animals, diabetes treatment / prevention agents,
It is also useful as a material and raw material for obesity preventive agents, diet pet food, diet feed and the like.

【0016】本発明の有効成分は上記の如くα―アミラ
ーゼの酵素活性を阻害するから、食事と共に、又は食事
の前後に摂取できる形態の食品(茶飲料などの飲料やス
ープ、味噌汁など)に添加したり、ご飯、パン、麺類な
どデンプンを多く含む食品に添加したりして健康飲食物
を製造し、血糖値上昇抑制飲食品、糖尿病治療予防飲食
品、肥満治療予防飲食品、ダイエット飲食品、ダイエッ
トペットフード、或いはダイエット飼料などとして様々
に提供することができる。
Since the active ingredient of the present invention inhibits the enzymatic activity of α-amylase as described above, it is added to foods (beverages such as tea drinks, soups, miso soups, etc.) that can be taken with or before and after meals. , Rice, bread, added to foods containing a lot of starch such as noodles to produce healthy foods and drinks, foods and drinks for suppressing blood sugar level increase, foods and drinks for preventing and treating diabetes, foods and drinks for preventing and treating obesity, diet foods and drinks, It can be variously provided as a diet pet food or diet feed.

【0017】[0017]

【発明の実施の形態】以下、本発明の実施の形態につい
て説明する。
BEST MODE FOR CARRYING OUT THE INVENTION Embodiments of the present invention will be described below.

【0018】本発明の糖質消化酵素阻害剤、血糖値上昇
抑制剤、肥満治療予防剤、糖尿病治療予防剤(以下、こ
れらを総括して「糖質消化酵素阻害剤等」という。)
は、バロネア酸、或いは、バロネア酸配糖体、或いはバ
ロネア酸とバロネア酸配糖体の混合物を配合することに
より製造することができる。
The sugar digestive enzyme inhibitor, the blood sugar level increase inhibitor, the obesity treatment preventive agent, the diabetes treatment preventive agent of the present invention (hereinafter, these are collectively referred to as "sugar digestive enzyme inhibitor and the like").
Can be produced by blending baroneaic acid, baroneaic acid glycoside, or a mixture of baroneaic acid and baroneaic acid glycoside.

【0019】バロネア酸及びバロネア酸配糖体は、バナ
バその他の植物から抽出・精製することにより得ること
ができる。
Baroneaic acid and baroneaic acid glycoside can be obtained by extraction and purification from banaba and other plants.

【0020】抽出に用いる溶媒としては、水、温水、熱
水、メタノール、エタノールなどのアルコール類、アセ
トンなどのケトン類等、その他の有機溶媒、或いはこれ
らのうち二種類以上の混合溶液などを用いることが可能
である。ヒト或いはその他の動物が体内に摂取すること
を考えると、水、エタノール、またはアセトンなどが望
ましい。抽出するの際の植物と抽出溶液との比率、抽出
温度、抽出時間等の抽出条件については、抽出する植物
及び抽出溶媒によって任意に調整すればよい。そして、
抽出によって得られた植物抽出物は、更に吸着剤処理
法、膜分離法、或いは溶媒分画法、その等の精製法によ
りバロネア酸或いはバロネア酸配糖体の含有濃度を高め
るように精製すればよい。
As the solvent used for extraction, water, warm water, hot water, alcohols such as methanol and ethanol, ketones such as acetone, and other organic solvents, or a mixed solution of two or more of these is used. It is possible. Considering human or other animal ingestion, water, ethanol, or acetone is preferable. The extraction conditions such as the ratio of the plant to the extraction solution at the time of extraction, the extraction temperature, the extraction time, etc. may be arbitrarily adjusted depending on the plant to be extracted and the extraction solvent. And
The plant extract obtained by the extraction may be further purified by an adsorbent treatment method, a membrane separation method, or a solvent fractionation method, or a purification method such as such that the content concentration of baroneaic acid or baroneaic acid glycoside is increased. Good.

【0021】ここで、「バナバ」を抽出・精製してバロ
ネア酸及びバロネア酸配糖体を得る方法について説明す
る。
Here, a method for extracting and purifying "banaba" to obtain baroneaic acid and a glycoside of baroneaic acid will be described.

【0022】バナバすなわちLagerstroemia speciosa
(L.)Pers.は、フトモモ目ミソハギ科に属する植物で
あり、これの葉や、花、或いは、これらと茎、木部、
根、実のいずれかの混合物などを抽出に用いることがで
きる。但し、バナバは、極めて多くの雑菌を含んでいる
ため、抽出処理を行う前に、オートクレーブ殺菌などの
加熱殺菌を充分に行う必要がある。特に、特許第281
8458号記載の特許発明の如く、乾燥させ破砕したバ
ナバ葉を加熱殺菌処理後、いったん細菌培養環境下で保
管し、その後加熱殺菌処理を行うのが好ましい。
Banaba or Lagerstroemia speciosa
(L.) Pers. Is a plant belonging to the family Myrtaceae of the order Pleurotus, and its leaves, flowers, or these and stems, xylem,
Mixtures of either roots or fruits can be used for extraction. However, since Banaba contains an extremely large amount of various bacteria, it is necessary to sufficiently perform heat sterilization such as autoclave sterilization before performing the extraction treatment. In particular, Patent No. 281
As in the patented invention described in No. 8458, it is preferable that the dried and crushed Banaba leaf is heat-sterilized, then temporarily stored in a bacterial culture environment, and then heat-sterilized.

【0023】加熱殺菌したバナバは、水(熱水含む)、
エタノールまたはアセトンなどで抽出し、次いで抽出に
よって得られた抽出液を液液分配並びにカラムクロマト
グラフィーなどによって分取し、バロネア酸及びバロネ
ア酸配糖体を精製すればよい。この際、抽出溶媒には下
記試験に示すようにアセトンを用いるのが好ましく、抽
出条件については限定しないが、抽出操作及び効率の点
で5〜100倍容の抽出溶媒にて、抽出温度50℃〜沸
点の下、抽出時間1分〜3日程度で抽出するのが望まし
い。飲料用に供する場合は、有効成分の抽出状況と抽出
液自体の食味を考慮に入れて抽出条件を適宜設定するの
が好ましい。液液分配及びカラムクロマトグラフィーに
よる分取については、例えば、抽出液を水に転溶し、酢
酸エチル、ブタノールで順次分配して「酢酸エチル相」
「ブタノール相」及び「水相」を得、その中の「酢酸エ
チル相」をカラムクロマトグラフィーで分離すればよ
い。
Banaba, which has been sterilized by heating, contains water (including hot water),
Extraction may be performed with ethanol or acetone, and then the extract obtained by the extraction may be separated by liquid-liquid partitioning, column chromatography and the like to purify baroneaic acid and baroneaic acid glycoside. At this time, it is preferable to use acetone as the extraction solvent as shown in the following test, and the extraction conditions are not limited, but the extraction solvent is 5 to 100 volumes in terms of extraction operation and efficiency, and the extraction temperature is 50 ° C. ~ It is desirable to perform extraction at a boiling point for about 1 minute to 3 days. When used for beverages, it is preferable to appropriately set the extraction conditions in consideration of the extraction status of the active ingredient and the taste of the extraction liquid itself. For liquid-liquid partitioning and preparative separation by column chromatography, for example, the extract is redissolved in water and sequentially partitioned with ethyl acetate and butanol to obtain an “ethyl acetate phase”.
The "butanol phase" and the "aqueous phase" are obtained, and the "ethyl acetate phase" therein may be separated by column chromatography.

【0024】本発明の有効成分すなわちバロネア酸、バ
ロネア酸配糖体或いはこれらの混合物は、それぞれ単独
で本発明の有効成分として用いることもできるが、これ
らを従来公知或いは将来公知の消化酵素活性阻害物質等
と組み合わせて有効成分とすることにより消化酵素活性
阻害作用を相乗的に高めることが可能である。従来公知
の消化酵素活性阻害物質としては、例えば、小麦より抽
出した蛋白性物質(M.D.O'Donnell et.al., Biochemi.
Biophys. Acta 422 (1976) 159-169)、大豆由来の多糖
(特開平3−290187公報)、サトイモ(Colocasi
a esculenta)より抽出した蛋白性物質NSAI−I、
NSAI−II(特願平2−95992)、月桂樹(Laur
us nobilis L.)より抽出した粗エキス(特願平2−1
30852)、そのほか小麦アルブミン、桑属のアルカ
ロイド、ニシキギ科植物の含硫加工物、ナンバンカラス
ウリなどの天然物由来の消化酵素活性阻害物質を好まし
い例として挙げることができる。なお、単独の有効成分
として配合する場合、例えば、バロネア酸、バロネア酸
配糖体或いはこれらの混合物をそれぞれ、精製水又は生
理食塩水などに溶解して薬剤(経口投与剤)などとして
提供することができる。
The active ingredients of the present invention, namely baroneaic acid, baroneaic acid glycosides and mixtures thereof, can be used alone as the active ingredients of the present invention. It is possible to synergistically enhance the digestive enzyme activity inhibitory action by combining it with a substance or the like to obtain an active ingredient. As a conventionally known digestive enzyme activity inhibitor, for example, a proteinaceous substance extracted from wheat (MDO'Donnell et.al., Biochemi.
Biophys. Acta 422 (1976) 159-169), polysaccharide derived from soybean (JP-A-3-290187), taro (Colocasi)
a esculenta), a proteinaceous substance NSAI-I extracted from
NSAI-II (Japanese Patent Application No. 2-95992), Laurel (Laur
crude extract extracted from us nobilis L. (Japanese Patent Application No. 2-1)
30852), as well as digestive enzyme activity-inhibiting substances derived from natural products such as wheat albumin, mulberry alkaloids, sulfur-containing processed products of Euphorbiaceae plants, and Nanbankarasuuri. When blended as a single active ingredient, for example, barone acid, barone acid glycoside or a mixture thereof may be dissolved in purified water or physiological saline to be provided as a drug (orally administered drug) or the like. You can

【0025】本発明の糖質消化酵素阻害剤等はいずれも
経口投与剤として使用することができ、この場合それぞ
れの投与に適した配合及び剤型とするのが好ましい。剤
型について言えば、経口投与剤用として液剤、錠剤、散
剤、顆粒、糖衣錠、カプセル、懸濁液、乳剤、丸剤など
の形態に調製することができる。配合(製剤)について
言えば、通常用いられている賦形剤、増量剤、結合剤、
湿潤化剤、崩壊剤、表面活性剤、潤滑剤、分散剤、緩衝
剤、保存剤、溶解補助剤、防腐剤、矯味矯臭剤、無痛化
剤、安定化剤などを用いて常法により製造することがで
きる。また、例えば乳糖、果糖、ブドウ糖、でん粉、ゼ
ラチン、炭酸マグネシウム、合成ケイ酸マグネシウム、
タルク、ステアリン酸マグネシウム、メチルセルロー
ス、カルボキシメチルセルロースまたはその塩、アラビ
アゴム、ポリエチレングリコール、シロップ、ワセリ
ン、グリセリン、エタノール、プロピレングリコール、
クエン酸、塩化ナトリウム、亜硫酸ソーダ、リン酸ナト
リウムなどの無毒性の添加剤を配合することも可能であ
る。
Any of the carbohydrate digestive enzyme inhibitors and the like of the present invention can be used as an orally-administered agent, and in this case, it is preferable that the formulation and dosage form are suitable for each administration. With respect to the dosage form, it can be prepared for oral administration in the form of liquid, tablet, powder, granule, dragee, capsule, suspension, emulsion, pill and the like. Speaking of formulation (formulation), commonly used excipients, fillers, binders,
Manufactured by a conventional method using a wetting agent, a disintegrating agent, a surface active agent, a lubricant, a dispersant, a buffer, a preservative, a solubilizing agent, a preservative, a flavoring agent, a soothing agent, a stabilizer and the like. be able to. Also, for example, lactose, fructose, glucose, starch, gelatin, magnesium carbonate, synthetic magnesium silicate,
Talc, magnesium stearate, methyl cellulose, carboxymethyl cellulose or its salt, gum arabic, polyethylene glycol, syrup, petrolatum, glycerin, ethanol, propylene glycol,
It is also possible to add non-toxic additives such as citric acid, sodium chloride, sodium sulfite and sodium phosphate.

【0026】また、本発明の糖質消化酵素阻害剤等は、
医薬品のほか、医薬部外品、薬理効果を備えた健康食品
・健康飲料・特定保健用食品・機能性食品、食品添加
剤、その他ヒト以外の動物に対する薬剤や飼料、飼料用
添加剤などとして提供することもできる。例えば、医薬
部外品として調製し、これを瓶ドリンク飲料等の飲用形
態、或いはタブレット、カプセル、顆粒等の形態とする
ことにより、より一層摂取し易くすることができる。薬
理効果を備えた健康食品・健康飲料・特定保健用食品・
機能性食品としては、例えば本発明の有効成分を、炭
酸、賦形剤(造粒剤含む)、希釈剤、或いは更に甘味
剤、フレーバー、小麦粉、デンプン、糖、油脂類等の各
種タンパク質、糖質原料やビタミン、ミネラルなどの飲
食品材料群から選ばれた一種或いは二種以上と混合した
り、或いは、現在公知の飲食品、例えばスポーツ飲料、
果実飲料、乳飲料、茶飲料、野菜ジュース、乳性飲料、
アルコール飲料、ゼリー、ゼリー飲料、炭酸飲料、チュ
ーインガム、チョコレート、キャンディ、ビスケット、
スナック、パン、乳製品、魚肉練り製品、畜肉製品、冷
菓、乾燥食品、サプリメント、ペットフード、飼料など
に添加して製造することができる。
Further, the carbohydrate digestive enzyme inhibitor and the like of the present invention are
In addition to drugs, quasi-drugs, health foods / health drinks / foods with specified health benefits / functional foods, food additives with pharmacological effects, and other non-human animal drugs, feeds, feed additives, etc. You can also do it. For example, it can be made easier to ingest by preparing it as a quasi-drug and making it into a drinkable form such as a bottled drink, or a tablet, capsule, granule or the like. Health foods, health drinks, foods for specified health use, with pharmacological effects
Functional foods include, for example, carbon dioxide, excipients (including granulating agents), diluents, or further sweeteners, flavors, flour, starch, sugars, various proteins such as fats and oils, sugars. Mixtures with one or more selected from food and drink ingredients such as quality raw materials, vitamins and minerals, or currently known food and drink, such as sports drinks,
Fruit drinks, milk drinks, tea drinks, vegetable juices, dairy drinks,
Alcoholic drinks, jellies, jelly drinks, carbonated drinks, chewing gum, chocolate, candy, biscuits,
It can be produced by adding it to snacks, breads, dairy products, fish meat products, livestock products, frozen desserts, dried foods, supplements, pet foods, feeds and the like.

【0027】上記本発明の糖質消化酵素阻害剤等は、肥
満や糖尿病などの栄養過多による悩みや疾病を予防する
ために食事の前に予め摂取するようにしても勿論よい
が、食事と同時に或いは食後に摂取するようにしても、
又、食事に混ぜて摂取するようにしてもよい。
The carbohydrate digestive enzyme inhibitor and the like of the present invention may be taken in advance before meals in order to prevent troubles and diseases caused by overnutrition such as obesity and diabetes, but they may be taken at the same time as meals. Or even if you take it after eating,
Also, it may be mixed with meals and ingested.

【0028】本発明の摂取量は、使用方法、投与方法、
病気の重軽、摂取するヒト或いは動物の年齢等によって
も異なるが、一般的に言って、医薬品であれば、バロネ
ア酸は、大人ならば有効成分として一日当たり20mg
〜1,000mg、子供ならば6mg〜300mgが好
ましく、バロネア酸及びその配糖体は、大人ならば有効
成分として一日当たり40mg〜2,000mg、子供
ならば12mg〜600mgが好ましい。医薬品として
の有効成分の濃度は、バロネア酸としては、乾燥重量換
算にして0.01〜10重量%、中でも0.1〜5重量
%が好ましく、バロネア酸及びその配糖体としては、乾
燥重量換算にして0.004〜40重量%、中でも0.
04〜20重量%とするのが好ましい。他方、医薬品以
外については、バロネア酸は、大人ならば有効成分とし
て一日当たり20mg〜500mg、子供ならば6mg
〜150mgの摂取量が好ましく、バロネア酸及びその
配糖体としては、大人ならば40mg〜1,000m
g、子供ならば12mg〜300mgの摂取量が好まし
い。有効濃度は、バロネア酸としては、乾燥重量換算に
して0.01〜5重量%、中でも0.1〜2重量%が好
ましく、バロネア酸及びその配糖体としては、乾燥重量
換算にして0.004〜20重量%、中でも0.04〜
8重量%配合するのが好ましい。
The intake amount of the present invention is determined by the method of use, administration method,
Although it depends on the severity of the illness, the age of the human or animal to be ingested, generally speaking, as a drug, baroneaic acid is 20 mg per day as an active ingredient for adults.
-1,000 mg, 6 mg-300 mg for children is preferred, and 40 mg-2,000 mg of baroneaic acid and its glycosides as active ingredients per day for adults and 12 mg-600 mg for children are preferred. The concentration of the active ingredient as a drug is 0.01 to 10% by weight, particularly 0.1 to 5% by weight, in terms of dry weight of baroneaic acid. Converted to 0.004 to 40% by weight, and especially 0.
It is preferably from 04 to 20% by weight. On the other hand, except for medicines, baroneaic acid is 20 mg to 500 mg per day as an active ingredient for adults and 6 mg for children.
An intake of ~ 150 mg is preferable, and as for baroneaic acid and its glycosides, 40 mg to 1,000 m for adults
g, for children, an intake amount of 12 mg to 300 mg is preferable. The effective concentration of baroneaic acid is 0.01 to 5% by weight in terms of dry weight, preferably 0.1 to 2% by weight, and baroneamic acid and its glycoside are preferably in the range of 0. 004 to 20% by weight, especially 0.04 to
It is preferable to add 8% by weight.

【0029】(健康飲食物)本発明の健康飲食物は、バ
ロネア酸、バロネア酸配糖体、或いはこれらの混合物
を、デンプン(アミロース、アミロペクチン)、その他
のα−グルコシド結合を有する糖質を含有、好ましくは
当該糖質を主材とする飲食物素材に添加することにより
製造することができる。
(Health Food and Beverage) The health food and beverage of the present invention contains baroneacetic acid, baroneaic acid glycoside, or a mixture thereof, starch (amylose, amylopectin) and other sugars having an α-glucoside bond. Preferably, it can be produced by adding the sugar to a food or drink material containing the sugar as a main ingredient.

【0030】この際のバロネア酸及びバロネア酸配糖体
は、上記と同様の方法により入手可能である。
Baroneaic acid and baroneaic acid glycoside in this case can be obtained by the same method as described above.

【0031】α−グルコシド結合を有する糖質とは、デ
ンプン(アミロース、アミロペクチン)以外の糖質でも
構わない。要するに、本発明の有効成分はα−グルコシ
ド結合に作用するα―アミラーゼの酵素活性を阻害する
から、α−グルコシド結合を有する糖質であれば当該糖
質の消化・吸収を妨げることができる。
The saccharide having an α-glucoside bond may be a saccharide other than starch (amylose, amylopectin). In short, since the active ingredient of the present invention inhibits the enzymatic activity of α-amylase acting on α-glucoside bond, a sugar having an α-glucoside bond can prevent digestion / absorption of the sugar.

【0032】α−グルコシド結合を有する糖質を含有或
いは主材とする飲食物素材としては、野菜・果物ジュー
ス、お茶、乳飲料、乳性飲料、アルコール飲料などの飲
料、加工水産物、乳製品、カレーやシチューなどの調理
品、ご飯、麺類、菓子、パン、アイスクリーム、ペット
フード、飼料などを挙げることができる。また、デンプ
ンを多く含む飲食物のみでなく、食事の際に摂取する
茶、飲料、スープ、味噌汁なども好ましい。
Examples of food and drink materials containing or containing a sugar having an α-glucoside bond are beverages such as vegetable / fruit juice, tea, dairy drinks, dairy drinks and alcoholic drinks, processed seafood, dairy products, Examples include cooked products such as curry and stew, rice, noodles, confectionery, bread, ice cream, pet food, and feed. Further, not only foods and drinks containing a large amount of starch, but also teas, beverages, soups, miso soup, etc., which are ingested during meals are preferable.

【0033】なお、健康飲食物の調製に当たっては、常
法に従って、増量剤、賦形剤、炭酸、賦形剤(造粒剤含
む)、希釈剤、甘味剤、フレーバー、油脂類等の各種タ
ンパク質、ビタミン、ミネラルなど飲食品製造上許容さ
れ得る基剤や食品等を配合することは任意である。ま
た、健康飲食物中の有効成分の濃度は0.1〜2重量%
とするのが好ましい。
In the preparation of healthy foods and drinks, various proteins such as bulking agents, excipients, carbonic acid, excipients (including granulating agents), diluents, sweeteners, flavors, oils and fats, etc. are prepared according to a conventional method. It is optional to add a base such as vitamins and minerals, which is acceptable in the production of foods and drinks, foods and the like. The concentration of active ingredients in healthy food and drink is 0.1-2% by weight.
Is preferred.

【0034】本発明の健康食品は、日常的に摂取してい
る飲食物の消化・吸収を阻害することができるから、日
常的に摂取している飲食物をダイエット食品や糖尿病患
者用の飲食物、その他の体質改善飲食物などに容易に改
良することができる。特にダイエット食品としては、摂
食しながらダイエットすることができる点で大きな効果
を期待することができる。
Since the health food of the present invention can inhibit the digestion and absorption of foods and drinks that are routinely ingested, the foods and drinks that are routinely taken are diet foods and foods and drinks for diabetics. , Other constitution improving foods and drinks can be easily improved. In particular, as a diet food, a great effect can be expected in that it is possible to diet while eating.

【0035】なお、上記医薬品、医薬部外品、薬理効果
を備えた健康食品・健康飲料・特定保健用食品・機能性
食品、食品添加剤、その他ヒト以外の動物に対する薬剤
や飼料、飼料用添加剤などにおいて、バロネア酸の定量
法は、バロネア酸そのものを高速液体クロマトグラフィ
ーを用いて定量分析する方法が好ましい。(分離条件:
グラジエント法、A液:アセトニトリル/水/酢酸=5/95
/0.1、B液:アセトニトリル/水/酢酸=50/50/0.1、カ
ラム:YMC J'sphere-H80、測定波長:254および350ナノ
メートル)。一方、バロネア酸配糖体の定量法について
は、ポリフェノール含量を測定する方法が有用である。
測定方法は科学的な根拠があれば特に限定されないが、
特に茶などのポリフェノール分析において公定分析法と
して採用されている酒石酸鉄比色法が簡便かつ信用でき
る点で好ましい。
The above-mentioned pharmaceuticals, quasi-drugs, health foods / health drinks / foods for specified health use / functional foods, food additives having other pharmacological effects, other drugs for humans other than humans, feeds, feed additives In agents and the like, the method for quantifying baroneaic acid is preferably a method for quantitatively analyzing baroneaic acid itself using high performance liquid chromatography. (Separation conditions:
Gradient method, solution A: acetonitrile / water / acetic acid = 5/95
/0.1, B solution: acetonitrile / water / acetic acid = 50/50 / 0.1, column: YMC J'sphere-H80, measurement wavelengths: 254 and 350 nanometers). On the other hand, a method of measuring the polyphenol content is useful for the quantification method of baroneaic acid glycoside.
The measuring method is not particularly limited as long as it has a scientific basis,
Particularly, the iron tartrate colorimetric method, which is adopted as an official analytical method in the analysis of polyphenols such as tea, is preferable because it is simple and reliable.

【0036】以下、試験に基づいて本発明の構成及び効
果について考察する。
The structure and effects of the present invention will be discussed below based on tests.

【0037】(試験材料の調製)フィリピン産バナバの
生葉を適宜量自然乃至強制的に乾燥、殺菌し、乾燥・殺
菌したバナバ葉を粉砕器で粉砕し、得られた粉砕バナバ
葉10gを熱水100mLで85℃・15分間抽出し、
得られた抽出物を濾過、冷却及び凍結乾燥して「熱水抽
出物」を得た。
(Preparation of test material) An appropriate amount of Philippine Banaba leaves were naturally or forcibly dried and sterilized, and the dried and sterilized Banaba leaves were crushed with a crusher, and 10 g of the obtained crushed Banaba leaves were heated. Extract with 100mL at 85 ℃ for 15 minutes,
The obtained extract was filtered, cooled and freeze-dried to obtain a "hot water extract".

【0038】他方、乾燥・殺菌したバナバ葉1kgを8
0%含水アセトン3Lで室温にて2回抽出し、得られた
抽出物を濃縮して「アセトン抽出物」を得た。この「ア
セトン抽出物」は更に水に転溶した後、酢酸エチル、ブ
タノールで順次分配し、「酢酸エチル相」「ブタノール
相」及び「水相」を得た。「酢酸エチル相」については
更に、カラム(MCI gel、20×300mm)に吸着させた後、
カラム体積4倍容の70%エタノール及び100%エタ
ノールを用いて溶出させた。70%エタノール画分をカ
ラムクロマトグラフィー(Sephadex LH20、20×300mm)
で分離後、展開溶媒にエタノール/メタノール系(10
0:0〜0:100)を用いて順次溶出させ、下記表1
の「酢酸エチル−1〜7」を得た。そして更に、「酢酸
エチル−4(エタノール/メタノール=40:60)」
については、高速液体クロマトグラフィー(C18、Capce
ll Pak、20×300mm、展開溶媒30%エタノール/0.
1%酢酸、流速8mL/min)で単離することにより
下記表2の「酢酸エチル−4-1(後にバロネア酸と同
定。)」を得る一方、バロネア酸以外の溶出液を濃縮、
凍結乾燥して「酢酸エチル−4-2」を得た。
On the other hand, 1 kg of dried and sterilized Banaba leaf is used as 8
It was extracted twice with 3 L of 0% hydrous acetone at room temperature, and the obtained extract was concentrated to obtain an "acetone extract". The "acetone extract" was further dissolved in water and then sequentially partitioned with ethyl acetate and butanol to obtain "ethyl acetate phase", "butanol phase" and "water phase". For the “ethyl acetate phase”, after adsorbing it on a column (MCI gel, 20 × 300 mm),
Elution was performed with 70% ethanol and 100% ethanol with a column volume of 4 times. Column chromatography of 70% ethanol fraction (Sephadex LH20, 20 x 300 mm)
After separation with, the developing solvent is ethanol / methanol (10
0: 0 to 0: 100) and sequentially eluted using Table 1 below.
“Ethyl acetate-1 to 7” was obtained. And further, "ethyl acetate-4 (ethanol / methanol = 40:60)"
For high performance liquid chromatography (C18, Capce
ll Pak, 20 × 300 mm, developing solvent 30% ethanol / 0.
Isolation with 1% acetic acid at a flow rate of 8 mL / min) yielded "ethyl acetate-4-1 (later identified as baroneaic acid.)" In Table 2 below, while concentrating eluates other than baroneaic acid.
It was freeze-dried to obtain "ethyl acetate-4-2".

【0039】(有効成分の活性評価)α-アミラーゼ阻
害試験は、Klein et al.1)の方法に従い測定した。すな
わち、酵素としてブタ膵液由来のα-アミラーゼ(Sigma
社製)を、基質にStarch azure(Sigma社製)を用いた。
25mL容の三角フラスコに200mgの基質及び4.
5mLの20mM塩化ナトリウムを含む40mMリン酸
緩衝液(pH7.0)を加え、40℃に保温した。50
μLの酵素溶液と50μLの試料とを200μg/ml
又は100μg/mlとなるように加え、振盪させ(8
0ストローク/min)15分間反応させた。この際、
下記表1の試料(酢酸エチル−1〜7等)については2
00μg/mlとなるように加え、下記表2の試料(酢
酸エチル−4−1〜2等)については100μg/ml
となるように加えた。上記の如く試料を加えた後、2.
4mLの100mMリン酸緩衝液(pH4.3)を加え
て反応を停止させ、フラスコの内容物をよく攪拌した
後、15mL遠沈管に移し、遠心分離後、上清の625
nmの吸光度を測定し、下記式(KleinB, Foreman JA,
Searcy RL(1969) The synthesis and utilization of c
ibachron blue-amylase: A new chromogenic substrate
for determination of amylaseactivity. Anal Bioche
m 31:412-25)にてα-アミラーゼ阻害率(%)を求め
た。
(Evaluation of activity of active ingredient) The α-amylase inhibition test was measured according to the method of Klein et al. That is, as an enzyme, α-amylase derived from pig pancreatic juice (Sigma
Was used as the substrate, and Starch azure (made by Sigma) was used as the substrate.
3. 200 mg substrate and 4. 25 mL Erlenmeyer flask.
A 40 mM phosphate buffer solution (pH 7.0) containing 5 mL of 20 mM sodium chloride was added, and the mixture was kept at 40 ° C. Fifty
200 μg / ml of μL enzyme solution and 50 μL sample
Or add to 100 μg / ml and shake (8
The reaction was performed for 15 minutes (0 stroke / min). On this occasion,
2 for the samples in Table 1 below (ethyl acetate-1 to 7 etc.)
100 μg / ml for the samples shown in Table 2 below (ethyl acetate-4-1 and 2 etc.).
Was added. After adding the sample as described above, 2.
The reaction was stopped by adding 4 mL of 100 mM phosphate buffer (pH 4.3), the contents of the flask were well stirred, transferred to a 15 mL centrifuge tube, centrifuged, and the supernatant 625
The absorbance at nm is measured and the following formula (KleinB, Foreman JA,
Searcy RL (1969) The synthesis and utilization of c
ibachron blue-amylase: A new chromogenic substrate
for determination of amylase activity. Anal Bioche
m 31: 412-25), the α-amylase inhibition rate (%) was determined.

【0040】[0040]

【数1】 [Equation 1]

【0041】上記式において、 A:試料溶液を加えない対照溶液の吸光度 B:対照溶液のブランク C:試料溶液の吸光度 D:試料溶液のブランク である。In the above equation, A: Absorbance of control solution without addition of sample solution B: blank of control solution C: Absorbance of sample solution D: Blank of sample solution Is.

【0042】[0042]

【表1】 [Table 1]

【0043】[0043]

【表2】 [Table 2]

【0044】上記画分の中で最もアミラーゼ阻害率
(%)の高かった「酢酸エチル−4−1」について機器
分析を行ったところ“バロネア酸”であることが判明し
た。なお、この際の機器分析は、分離条件:グラジエン
ト法、A液:アセトニトリル/水/酢酸=5/95/
0.1、B液:アセトニトリル/水/酢酸=50/50
/0.1、カラム:C18逆相カラム(YMC J'sphere-H
80,測定波長:254および350nm、流速1ml/
min)の条件で行った。
"Ethyl acetate-4-1" having the highest amylase inhibition rate (%) among the above fractions was subjected to instrumental analysis and found to be "baroneaic acid". In addition, the instrumental analysis at this time is as follows: Separation condition: gradient method, solution A: acetonitrile / water / acetic acid = 5/95 /
0.1, B solution: acetonitrile / water / acetic acid = 50/50
/0.1, column: C18 reverse phase column (YMC J'sphere-H
80, measurement wavelength: 254 and 350 nm, flow rate 1 ml /
min).

【0045】(実施例1)バロネア酸、ビタミンC、重
曹を配合した調合液を再度95℃に加熱し、缶に充填し
レトルト殺菌し、下記配合の糖質消化酵素阻害剤、血糖
値上昇抑制剤、肥満治療予防剤又は糖尿病治療予防剤を
作成した。
(Example 1) A mixed solution containing baroneaic acid, vitamin C and baking soda was heated to 95 ° C again, filled in a can and sterilized by retort, and a sugar digestive enzyme inhibitor having the following composition and suppression of blood sugar level increase were prepared. An agent, an obesity treatment preventive agent, or a diabetes treatment preventive agent was prepared.

【0046】 全量 200mL バロネア酸を含むバナバ抽出物 ・・300mg ビタミンC ・・ 40mg 重曹 ・・ 40mg 香料 ・・ 適量 水 ・・ 適量[0046] Total volume 200 mL Banaba extract containing baroneaic acid 300 mg Vitamin C ... 40 mg Baking soda ・ ・ 40mg Perfume ・ ・ Appropriate amount Water

【0047】(実施例2)バロネア酸及びバロネア酸配
糖体混合物、ビタミンC、重曹を配合した調合液を再度
95℃に加熱し、缶に充填しレトルト殺菌し、下記配合
の糖質消化酵素阻害剤、血糖値上昇抑制剤、肥満治療予
防剤又は糖尿病治療予防剤を作成した。
Example 2 A mixed solution of baroneaic acid and a mixture of baroneaic acid glycosides, vitamin C and baking soda was heated again to 95 ° C., filled in a can and sterilized by retort, and a sugar-digesting enzyme having the following composition. An inhibitor, a blood glucose elevation inhibitor, an obesity treatment preventive agent, or a diabetes treatment preventive agent was prepared.

【0048】 全量 200mL バロネア酸及びバロネア酸配糖体混合物 ・・100mg ビタミンC ・・ 40mg 重曹 ・・ 40mg 香料 ・・ 適量 水 ・・ 適量[0048] Total volume 200 mL Baroneaic Acid and Baroneaic Acid Glycoside Mixture ... 100mg Vitamin C ... 40 mg Baking soda ・ ・ 40mg Perfume ・ ・ Appropriate amount Water

【0049】(実施例3)下記配合で、健康飲食物(ジ
ュース)を作成した。
Example 3 A healthy food / beverage (juice) was prepared with the following composition.

【0050】 全量 200mL バロネア酸 ・・ 50mg みかん果汁 ・・ 20g ショ糖 ・・ 20g クエン酸 ・・ 2g ビタミンC ・・ 適量 香料 ・・ 適量 水 ・・ 適量[0050] Total volume 200 mL Baroneaic acid: 50 mg Mandarin orange juice 20g 20g sucrose Citric acid 2g Vitamin C ··· Perfume ・ ・ Appropriate amount Water

【0051】(実施例4)下記配合で、健康飲食物(パ
ン)を作成した。
Example 4 A healthy food / beverage (bread) was prepared with the following composition.

【0052】 バロネア酸及びバロネア酸配糖体 ・・600mg 強力粉 ・・300g 砂糖 ・・ 15g 塩 ・・ 6g スキムミルク ・・ 6g ドライイースト ・・ 6g 水 ・・195g ショートニング ・・ 15g[0052] Baroneaic Acid and Baroneaic Acid Glycosides-600mg Strong powder ... 300g 15g sugar 6g salt Skim milk ... 6g Dry yeast 6g Water: 195g Shortening: 15g

───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 FI テーマコート゛(参考) A61K 35/78 A61P 3/04 4C088 A61P 3/04 3/06 3/06 43/00 111 43/00 111 C07D 493/06 C07D 493/06 C12N 9/99 C12N 9/99 C07H 13/08 // C07H 13/08 17/04 17/04 A23L 2/00 F (72)発明者 細山 広和 静岡県榛原郡相良町女神21番地 株式会社 伊藤園内 (72)発明者 杉本 明夫 静岡県榛原郡相良町女神21番地 株式会社 伊藤園内 (72)発明者 永田 幸三 静岡県榛原郡相良町女神21番地 株式会社 伊藤園内 (72)発明者 角田 隆巳 静岡県榛原郡相良町女神21番地 株式会社 伊藤園内 Fターム(参考) 4B017 LC03 LC04 LK06 4B018 MD07 MD42 ME01 ME03 ME04 4C057 BB02 CC01 DD01 KK02 KK11 4C071 AA02 BB01 BB06 CC12 EE07 FF17 HH09 JJ01 LL01 4C086 AA01 AA02 CA01 EA11 MA01 MA04 NA14 ZA70 ZC20 ZC35 4C088 AB71 AC04 ZA70 ZC20 ZC35─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. 7 Identification code FI theme code (reference) A61K 35/78 A61P 3/04 4C088 A61P 3/04 3/06 3/06 43/00 111 43/00 111 C07D 493/06 C07D 493/06 C12N 9/99 C12N 9/99 C07H 13/08 // C07H 13/08 17/04 17/04 A23L 2/00 F (72) Inventor Hirokazu Hosoyama Sagara-cho, Haibara-gun, Shizuoka Prefecture 21 Goddess Itoenai Co., Ltd. (72) Inventor Akio Sugimoto 21 Goddess Sagara-cho, Haibara-gun, Shizuoka Prefecture Itoenai Co., Ltd. (72) Inventor Kozo Nagata 21 Goddess Sagara-cho, Haibara-gun Shizuoka Itoenai Co., Ltd. (72) Inventor Takami Tsunoda 21 Goddess, Sagara-cho, Hara-gun, Shizuoka Itoennai F-term Co., Ltd. (reference) 4B017 LC03 LC04 LK06 4B018 MD07 MD42 ME01 ME03 ME04 4C057 BB02 CC01 DD01 KK02 KK11 4C071 AA02 BB01 BB06 CC12 EE07 FF17 HH09 JJ01 LL01 4C086 AA01 AA02 CA01 EA11 MA01 MA04 NA14 ZA70 ZC20 ZC35 4C088 AB71 AC04 ZA70 ZC20 ZC35

Claims (7)

【特許請求の範囲】[Claims] 【請求項1】 バロネア酸を有効成分として含有する糖
質消化酵素阻害剤。
1. A sugar digestive enzyme inhibitor containing baroneacic acid as an active ingredient.
【請求項2】 バロネア酸配糖体を有効成分として含有
する糖質消化酵素阻害剤。
2. A sugar digestive enzyme inhibitor containing baroneaic acid glycoside as an active ingredient.
【請求項3】 バロネア酸配糖体は、次の式(式中、R
1〜R4の少なくともいずれか一つが糖であって、R1
〜R4の残りが水素原子、炭素数1以上を有する官能
基、糖のいずれかである。)で表されるものである請求
項2に記載の糖質消化酵素阻害剤。 【化1】
3. The baroneaic acid glycoside has the following formula (wherein R is
At least any one of 1 to R4 is a sugar, and R1
The remainder of R4 to R4 is any one of a hydrogen atom, a functional group having 1 or more carbon atoms, and a sugar. ] The sugar digestive enzyme inhibitor of Claim 2 represented by these. [Chemical 1]
【請求項4】 バロネア酸、バロネア酸配糖体のいずれ
か、或いはこれらの混合物を有効成分として含有する血
糖値上昇抑制剤。
4. A blood sugar level increase inhibitor containing, as an active ingredient, either baroneaic acid, baroneaic acid glycoside, or a mixture thereof.
【請求項5】 バロネア酸、バロネア酸配糖体のいずれ
か、或いはこれらの混合物を有効成分として含有する肥
満治療予防剤。
5. An agent for treating and preventing obesity, which comprises any one of baroneaic acid and baroneaic acid glycoside, or a mixture thereof as an active ingredient.
【請求項6】 バロネア酸、バロネア酸配糖体のいずれ
か、或いはこれらの混合物を有効成分として含有する糖
尿病治療予防剤。
6. A therapeutic / preventive agent for diabetes which comprises, as an active ingredient, any one of baroneaic acid, baroneaic acid glycoside, or a mixture thereof.
【請求項7】 バロネア酸、バロネア酸配糖体のいずれ
か或いはこれらの混合物を、α−グルコシド結合を有す
る糖質を含有する飲食物素材に添加してなる健康飲食
物。
7. A healthy food or drink obtained by adding any one of baroneaic acid and baroneaic acid glycoside or a mixture thereof to a food and drink material containing a sugar having an α-glucoside bond.
JP2001294640A 2001-09-26 2001-09-26 Sugar digestion enzyme inhibitor, hyperglycemia inhibitor, therapeutic or prophylactic agent for obesity, therapeutic or prophylactic agent for diabetes, and healthy food and drink Pending JP2003095941A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2001294640A JP2003095941A (en) 2001-09-26 2001-09-26 Sugar digestion enzyme inhibitor, hyperglycemia inhibitor, therapeutic or prophylactic agent for obesity, therapeutic or prophylactic agent for diabetes, and healthy food and drink

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2001294640A JP2003095941A (en) 2001-09-26 2001-09-26 Sugar digestion enzyme inhibitor, hyperglycemia inhibitor, therapeutic or prophylactic agent for obesity, therapeutic or prophylactic agent for diabetes, and healthy food and drink

Publications (1)

Publication Number Publication Date
JP2003095941A true JP2003095941A (en) 2003-04-03

Family

ID=19116208

Family Applications (1)

Application Number Title Priority Date Filing Date
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Country Status (1)

Country Link
JP (1) JP2003095941A (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007060911A1 (en) 2005-11-25 2007-05-31 Morinaga Milk Industry Co., Ltd. Aloe vera extract, process for production of aloe vera extract, and ameliorating agent for hyperglycemia
US7534770B2 (en) 2004-03-31 2009-05-19 Morinaga Milk Industry Co., Ltd. Glycoside having 4-methylergost-7-en-3-ol skeleton and hyperglycemia improving agent
US7674784B2 (en) 2004-09-29 2010-03-09 Morinaga Milk Industry Co., Ltd. Drug and food or drink for improving hyperglycemia
US7754704B2 (en) 2004-03-31 2010-07-13 Morinaga Milk Industry Co., Ltd. Method for treating hyperglycemia

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7534770B2 (en) 2004-03-31 2009-05-19 Morinaga Milk Industry Co., Ltd. Glycoside having 4-methylergost-7-en-3-ol skeleton and hyperglycemia improving agent
US7754704B2 (en) 2004-03-31 2010-07-13 Morinaga Milk Industry Co., Ltd. Method for treating hyperglycemia
US8338403B2 (en) 2004-03-31 2012-12-25 Morinaga Milk Industry Co., Ltd. Drug for improving hyperglycemia
US8486462B2 (en) 2004-03-31 2013-07-16 Morinaga Milk Industry Co., Ltd. Glycoside having 4-methylergost-7-en-3-ol skeleton and hyperglycemia improving agent
US7674784B2 (en) 2004-09-29 2010-03-09 Morinaga Milk Industry Co., Ltd. Drug and food or drink for improving hyperglycemia
WO2007060911A1 (en) 2005-11-25 2007-05-31 Morinaga Milk Industry Co., Ltd. Aloe vera extract, process for production of aloe vera extract, and ameliorating agent for hyperglycemia
EP2206509A1 (en) 2005-11-25 2010-07-14 Morinaga Milk Industry Co., Ltd. Aloe vera extract, method of producing aloe vera extract, and hyperglycemia improving agent

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