JP2011182703A - Food and drink including 1, 2-di-o-galloyl-4,6-hhdp-b-d-glucopyranose at high concentration - Google Patents

Food and drink including 1, 2-di-o-galloyl-4,6-hhdp-b-d-glucopyranose at high concentration Download PDF

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JP2011182703A
JP2011182703A JP2010050891A JP2010050891A JP2011182703A JP 2011182703 A JP2011182703 A JP 2011182703A JP 2010050891 A JP2010050891 A JP 2010050891A JP 2010050891 A JP2010050891 A JP 2010050891A JP 2011182703 A JP2011182703 A JP 2011182703A
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hhdp
galloyl
glucopyranose
food
tea
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Hiroshi Sugiyama
洋 杉山
Daiki Honma
大樹 本間
Yoshihisa Tanaka
善久 田中
Mari Yamamoto
万里 山本
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National Agriculture and Food Research Organization
Asahi Group Holdings Ltd
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Asahi Group Holdings Ltd
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<P>PROBLEM TO BE SOLVED: To provide food and drink, a hyperglycemic suppressant, an α-amylase inhibitor, and a diabetes preventing or treating agent each for preventing diabetes. <P>SOLUTION: There are provided the food and drink including 1, 2-di-O-galloyl-4,6-HHDP-b-d-glucopyranose at high concentration, the hyperglycemic suppressant, the α-amylase inhibitor, and the diabetes preventing or treating agent each including 1, 2-di-O-galloyl-4,6-HHDP-b-d-glucopyranose as the active ingredient. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

本発明は、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを高濃度で含有する飲食品に関する。   The present invention relates to a food and drink containing a high concentration of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose.

日本では近年食生活の欧米化が進んでいる。この現象に伴い、糖尿病の罹患率は上昇傾向にある。また、こうした公衆衛生上の問題は国内に限らず世界でも発生している。糖尿病を根治できる療法はいまだ開発されておらず、糖尿病対策は治療よりも予防に重点が置かれている。糖尿病の発症に大きく寄与する因子として食後血糖が挙げられる。食後血糖は、食事として摂取した糖質が消化吸収を受けてグルコースとして血中に出現した濃度として定義される。食後血糖が高値で維持されることが糖尿病発症の大きなリスクであることが近年示されている。食後高血糖の上昇を穏やかにすることで糖尿病の発症が抑制できることが明らかになったことから、α−アミラーゼ阻害作用を有する飲食品には糖尿病の予防作用が期待されている。こうした背景から、血糖上昇を穏やかにすることで糖尿病予防効果を期待できる食品が望まれている。   In recent years, westernization of eating habits has progressed in Japan. With this phenomenon, the prevalence of diabetes is on the rise. These public health problems are occurring not only in Japan but also in the world. Therapies that can cure diabetes have not yet been developed, and antidiabetic measures focus on prevention rather than treatment. Postprandial blood glucose is a factor that greatly contributes to the onset of diabetes. Postprandial blood glucose is defined as the concentration at which carbohydrates taken as a meal are digested and absorbed and appear in the blood as glucose. It has recently been shown that maintaining high postprandial blood glucose is a significant risk of developing diabetes. Since it became clear that the onset of diabetes can be suppressed by moderately increasing the postprandial hyperglycemia, foods and drinks having an α-amylase inhibitory action are expected to have a preventive action against diabetes. Against this background, a food that can be expected to have an effect of preventing diabetes by mildly increasing blood sugar is desired.

植物に含有されるポリフェノールには、コレステロールの低下作用や体脂肪の低減作用があることが報告されており、その生理的な有用性が示唆されている。ポリフェノールのこれらの作用発揮を期待して、ポリフェノールを高濃度で含有させた飲食品が存在する。
茶類は古来より用いられている飲料である。茶にはポリフェノールをはじめさまざまな成分が含有されている。茶に含まれる成分の有する機能性については多くの報告がある。しかしながら、茶に存在する各成分は微量であるがゆえに茶自身を飲料として摂取した場合に明確な機能を発揮できる場合はほとんどない。
Yoshidaらは、サザンカ類の葉より1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースをはじめて発見した(非特許文献1)。また、Fukudaらは、クルミ中に1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースが存在することを発見し、10kg中のクルミから7.7mgを単離した(非特許文献2)。また、Gaoらは、カメリア・タリエンシスに属する茶の茶葉に2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースが0.02質量%含有されていることを発見した(非特許文献3)。
しかしながら、これらの文献には、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースが糖尿病を予防するために使用できることは、記載されていない。
Polyphenols contained in plants have been reported to have a cholesterol-lowering action and a body fat-reducing action, suggesting their physiological usefulness. There are foods and drinks containing polyphenols at high concentrations in anticipation of the action of polyphenols.
Tea is a beverage that has been used since ancient times. Tea contains various components including polyphenols. There are many reports on the functionality of the ingredients contained in tea. However, since there are only a small amount of each component present in tea, there are almost no cases where a clear function can be exhibited when tea is ingested as a beverage.
Yoshida et al. First discovered 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose from the leaves of Sasanqua (Non-patent Document 1). Fukuda et al. Also discovered the presence of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose in walnuts and isolated 7.7 mg from walnuts in 10 kg. (Non-Patent Document 2). Gao et al. Also discovered that 0.02% by mass of 2-di-O-galloyl-4,6-HHDP-bd-glucopyranose was contained in tea leaves belonging to Camellia taliensis ( Non-patent document 3).
However, these documents do not describe that 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose can be used to prevent diabetes.

Phytochemistry,37:241−244(1994)Phytochemistry, 37: 241-244 (1994) Phytochemistry,63:795−801(2003)Phytochemistry, 63: 795-801 (2003) J.Agric.Food Chem.56:7517−7521(2008)J. et al. Agric. Food Chem. 56: 7517-7521 (2008)

本発明は、αアミラーゼを阻害することによる食後の高血糖防止を通じて糖尿病を予防するための飲食品を提供することを目的とする。   An object of this invention is to provide the food-drinks for preventing diabetes through prevention of the hyperglycemia after a meal by inhibiting alpha amylase.

われわれは、ある種の茶に含有される成分1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースに優れた機能性を見出した。そして、この1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースは他の茶成分と比較して極めて微量で機能性を発揮することが明らかとなった。すなわち、特許請求の範囲において規定される量の1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを含有する飲食品は、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの有する機能を発揮することができる。
すなわち、本発明は、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを高濃度で含有する飲食品を提供する。
また、本発明は、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを有効成分として含有する血糖上昇抑制剤を提供する。
また、本発明は、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを有効成分として含有するα−アミラーゼ阻害剤を提供する。
また、本発明は、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを有効成分として含有する糖尿病の予防又は治療剤を提供する。
We have found excellent functionality in the component 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose contained in certain teas. And it became clear that this 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose exhibits functionality in a very small amount as compared with other tea components. That is, a food or drink containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose in an amount specified in the claims is 1,2-di-O-galloyl. The function of -4,6-HHDP-bd-glucopyranose can be exhibited.
That is, this invention provides the food-drinks which contain 1, 2- di-O-galloyl-4, 6-HHDP-bd-glucopyranose in high concentration.
The present invention also provides a blood sugar elevation inhibitor containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose as an active ingredient.
The present invention also provides an α-amylase inhibitor containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose as an active ingredient.
In addition, the present invention provides a preventive or therapeutic agent for diabetes containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose as an active ingredient.

飲食品に1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを含有させることでα−アミラーゼ阻害作用を通して、食後の血糖上昇を抑制することができる。この作用により糖尿病の予防効果が期待できる。さらに、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースはごく微量でその効果(例えば、血糖上昇抑制効果)を発揮することができ、風味をはじめとする製品の品質を損なうことなく用いることができる。   Inclusion of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose in a food or drink can suppress postprandial blood glucose elevation through an α-amylase inhibitory action. This action can be expected to prevent diabetes. Furthermore, 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose can exert its effect (for example, blood glucose elevation inhibitory effect) in a very small amount, including flavor. It can be used without damaging the quality of the product.

1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノース(CT−1)によるα−アミラーゼ阻害活性を示すグラフである。It is a graph which shows the alpha-amylase inhibitory activity by 1, 2- di-O-galloyl-4, 6-HHDP-bd-glucopyranose (CT-1). 経口糖負荷試験の結果を示すグラフである。It is a graph which shows the result of an oral glucose tolerance test. 経口糖負荷試験の結果を示すグラフである。It is a graph which shows the result of an oral glucose tolerance test.

本発明において使用される1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースは、例えばサザンカ類、カメリア・タリエンシス種、カメリア・イラワジエンシス種、カメリア・シネンシス種やそれらの雑種に属する茶、クルミなどに含まれており、本発明の飲食品、血糖上昇抑制剤、α−アミラーゼ阻害剤、並びに糖尿病の予防及び治療剤を調製する場合には、これらの植物体をそのまま使用してもよく、又はこれらの植物体から抽出して得られる抽出液を有効成分として使用してもよい。例えば、カメリア・タリエンシス種の植物体をそのまま使用する場合には、葉、果実、種子、幹又は根を生の状態、あるいは乾燥の後、適切な大きさに細砕又は粉末化する。また、抽出した抽出液を有効成分として使用する場合には、水、アルコール、又はその他の有機溶媒等を抽出溶媒として用いる。これらの溶媒の混合物を使用してもよい。好ましい抽出溶媒は水、又は水とアルコール等との混合溶媒である。抽出は、室温抽出、加熱抽出さらには加圧抽出等によって行ってもよい。一般的には、抽出は室温〜125℃で行われる。植物体からの抽出液の抽出後、遠心分離等により固形分と液体を分離し、さらに必要に応じて濾過等の処理を行った後、減圧濃縮等で濃縮してエキス化してもよい。さらに、真空乾燥、凍結乾燥等により粉末化することもできる。粉末化に際して、適当な賦形剤を加えてもよい。あるいは、抽出液をさらに精製して1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを単離して、本発明の飲食品、血糖上昇抑制剤、α−アミラーゼ阻害剤、並びに糖尿病の予防及び治療剤を調製するために添加してもよい。   The 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose used in the present invention includes, for example, sasanqua, Camellia taliensis, Camellia irawadiensis, Camellia sinensis, In the case of preparing the food and drink, the blood sugar elevation inhibitor, the α-amylase inhibitor, and the preventive and therapeutic agent for diabetes included in teas, walnuts and the like belonging to those hybrids, these plants May be used as they are, or an extract obtained by extraction from these plants may be used as an active ingredient. For example, when a plant body of Camellia taliensis is used as it is, leaves, fruits, seeds, trunks or roots are crushed or pulverized to an appropriate size in a raw state or after drying. Moreover, when using the extracted extract as an active ingredient, water, alcohol, other organic solvents, etc. are used as an extraction solvent. Mixtures of these solvents may be used. A preferred extraction solvent is water or a mixed solvent of water and alcohol. The extraction may be performed by room temperature extraction, heating extraction, or pressure extraction. In general, the extraction is performed at room temperature to 125 ° C. After extraction of the extract from the plant body, the solid and liquid may be separated by centrifugation or the like, and further subjected to a treatment such as filtration as necessary, and then concentrated by extraction under reduced pressure or the like for extraction. Furthermore, it can also be pulverized by vacuum drying, freeze drying or the like. An appropriate excipient may be added during the pulverization. Alternatively, the extract is further purified to isolate 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose, and the food / beverage product, blood sugar elevation inhibitor, α-amylase of the present invention It may be added to prepare an inhibitor and a preventive and therapeutic agent for diabetes.

本発明の血糖上昇抑制剤、α−アミラーゼ阻害剤、並びに糖尿病の予防及び治療剤を調製する際には、製剤化の常法を適宜使用することができ、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを含む植物体若しくはその抽出液や抽出エキス、又は1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの単体を単独で使用して、又はこれらに賦形剤、結合剤、滑沢剤、崩壊剤、風味改善剤、溶解補助剤、懸濁剤、コーティング剤などの常用される補助剤を加えて、錠剤、散剤、顆粒剤、カプセル剤、ドリンク剤などの形態で製剤化してもよい。
また、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを含む植物体若しくはその抽出液や抽出エキス、又は1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの単体を、必要に応じて上記補助剤若しくは食品素材とともに、固体状(粉末、顆粒状など)、ペースト状、液状ないし懸濁状の飲食品としてもよく、例えば茶飲料、ジュース、スポーツドリンク、アルコール飲料、発酵乳、チーズやバターなどの乳製品、ドリンクヨーグルトや乳酸菌飲料、バターケーキなどの菓子・パン類などの飲料又は食品の形態としてもよく、さらにサプリメントなどの医薬部外品としてもよい。また、飲料形態の場合は、飲料自体の風味や1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの保存安定性の観点から容器詰め飲料であることが好ましい。食品素材としては、固形物(粉状、薄片状、塊状など)、半固形物(ゼリー状、水飴状など)、又は液状物等のいずれであってもよい。製剤、飲料、食品又は医薬部外品1gあたりの1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの含有量は、0.1〜10.0mg(乾燥重量)であることが望ましい。
When preparing the blood sugar elevation inhibitor, α-amylase inhibitor, and diabetes preventive and therapeutic agent of the present invention, conventional methods for formulation can be used as appropriate, and 1,2-di-O-galloyl can be used. A plant containing -4,6-HHDP-bd-glucopyranose or an extract or extract thereof, or a simple substance of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose In combination with excipients, binders, lubricants, disintegrants, flavor improvers, solubilizers, suspension agents, coating agents, etc. , Powders, granules, capsules, drinks and the like.
Further, a plant containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose or an extract or extract thereof, or 1,2-di-O-galloyl-4,6 -HHDP-b-d-glucopyranose may be a solid (powder, granule, etc.), paste, liquid or suspension food or drink, if necessary, together with the above adjuvant or food material, For example, tea beverages, juices, sports drinks, alcoholic beverages, fermented milk, dairy products such as cheese and butter, drink yogurt and lactic acid bacteria beverages, beverages and foods such as confectionery and breads such as butter cake, and supplements It may be a quasi-drug such as. Moreover, in the case of a drink form, it is preferable that it is a container-packed drink from the viewpoint of the flavor of the drink itself and the storage stability of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose. . The food material may be any of solids (powder, flakes, lumps, etc.), semi-solids (jelly, syrup, etc.), or liquids. The content of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose per 1 g of the preparation, beverage, food or quasi drug is 0.1 to 10.0 mg (dry weight ) Is desirable.

本発明で用いる1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースは、安全性には問題ないため、これを経口投与する場合の投与量に制限はない。一般的には、1回につき0.1g(乾燥重量)/kg体重以上の量、好ましくは0.1〜2g(乾燥重量)/kg体重の量を1日に1〜数回経口投与する。また、1日当たりの総投与量としては、0.1mg以上、好ましくは0.1〜5.0mgである。   Since 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose used in the present invention has no safety problem, there is no limitation on the dose when it is orally administered. In general, an amount of 0.1 g (dry weight) / kg body weight or more, preferably 0.1 to 2 g (dry weight) / kg body weight, is orally administered once to several times a day. The total dose per day is 0.1 mg or more, preferably 0.1 to 5.0 mg.

本発明の飲食品として、容器詰め飲料の形態をとる場合、容量を500mLとすれば、1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの含有量は、一般的には0.02質量%以上、好ましくは0.02〜0.2質量%である。   When taking the form of a container-packed beverage as the food and drink of the present invention, if the capacity is 500 mL, the content of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose is Generally it is 0.02 mass% or more, Preferably it is 0.02-0.2 mass%.

(1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノース含有添加物の調製)
カメリア・タリエンシス種雑種の茶中間母本農6号の茶葉2gを100℃の熱水100mLに7分間接触させ熱水抽出物を得た。熱水抽出物を凍結乾燥し、茶葉熱水抽出物凍結乾燥物(以下、乾燥物という)を得た。乾燥物中の1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノース(実施例中において略称として「CT−1」と表示する場合がある。)含量を高速液体クロマトグラフィーにて定量した。分析条件は、カラム;Inertsil ODS−3 2.1×150mm,溶離液A;水:アセトニトリル=91:9(0.1%トリフルオロ酢酸含有),溶離液B;水:アセトリニトリル=40:60(0.1%トリフルオロ酢酸含有),溶出条件;溶離液B濃度8から40%への35分間のリニアグラジエントとした。乾燥物中のCT−1含量は7.7%であった。
(Preparation of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose-containing additive)
2 g of tea leaves from the tea middle mother Honno No. 6 of the Camellia taliensis hybrid were brought into contact with 100 mL of hot water at 100 ° C. for 7 minutes to obtain a hot water extract. The hot water extract was freeze-dried to obtain a freeze-dried tea leaf hot water extract (hereinafter referred to as a dried product). The content of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose (sometimes abbreviated as “CT-1” in the examples) in the dried product is the high-speed liquid. Quantified by chromatography. The analysis conditions were as follows: column; Inertsil ODS-3 2.1 × 150 mm, eluent A; water: acetonitrile = 91: 9 (containing 0.1% trifluoroacetic acid), eluent B; water: acetonitrile = 40: 60 (containing 0.1% trifluoroacetic acid), elution conditions; 35 minutes linear gradient from eluent B concentration 8 to 40%. The CT-1 content in the dried product was 7.7%.

(CT−1含有飲料の調製)
市販の緑茶(やぶきた茶)を用意し、茶葉2gを100℃の熱水100mLに7分間接触させ、やぶきた茶を得た。CT−1濃度が50、12.5、3.125ppmになるよう乾燥物をやぶきた茶に添加し溶解させ、CT−1を高濃度で含有する茶飲料を得た。
(Preparation of beverage containing CT-1)
Commercially available green tea (Yabukita tea) was prepared, and 2 g of tea leaves were brought into contact with 100 mL of hot water at 100 ° C. for 7 minutes to obtain Yabukita tea. The dried product was added and dissolved in Yabuki tea so that the CT-1 concentration was 50, 12.5, and 3.125 ppm to obtain a tea beverage containing CT-1 at a high concentration.

(大理茶抽出液の調製)
市販の大理茶を用意し、茶葉2gを100℃の熱水100mLに7分間接触させ、大理茶抽出液(CT−1濃度は46ppm)を得た。
(Preparation of Dairi tea extract)
Commercially available Dairi tea was prepared, and 2 g of tea leaves were brought into contact with 100 mL of hot water at 100 ° C. for 7 minutes to obtain a Dairi tea extract (CT-1 concentration was 46 ppm).

(CT−1含有飲料の効果)
CT−1を高濃度で含有する茶飲料、やぶきた茶及び大理茶抽出液の有するα−アミラーゼ阻害活性を測定した。測定は以下のように行った。酵素液には、ラット小腸アセトン抽出物(シグマ社)300mgを5mLマレイン酸バッファ(50mM、pH6.0)に分散させ、遠心分離により得た上清を使用直前にマレイン酸バッファにより100倍希釈して用いた。反応基質検体20μLと360μLの0.1%でんぷん(メルク社)溶液および20μLの酵素液を混合し、37℃で20分反応させた。反応液にヨウ素液を添加し、630nmの吸収波長で残存でんぷん量を定量した。阻害率は次のように算出した。
(阻害率%)=(1−(茶添加時の酵素活性)/(茶無添加時の酵素活性))×100
なお、「酵素活性」は酵素無添加時のでんぷん量と反応終了時の残存でんぷん量の差である。各種茶は段階希釈を行い、各希釈率に対する阻害率を求め、50%阻害を与える希釈率を線形トレンドの予測から算出し、IC50値とした。結果を図1に示す。
図1から、各種茶のIC50における希釈率は、大理茶では0.73、50ppmCT−1含有やぶきた茶では0.45、および12.5ppmCT−1含有やぶきた茶では0.86であり、その他は活性が無かった。少なくとも50ppm以上のCT−1を含有させたやぶきた茶では、大理茶抽出液以上のα−アミラーゼ阻害活性を有することが確認された。
(Effect of CT-1 containing beverage)
The α-amylase inhibitory activity of tea beverages containing high concentrations of CT-1, Yabukita tea and Dairi tea extract was measured. The measurement was performed as follows. In the enzyme solution, 300 mg of rat small intestine acetone extract (Sigma) was dispersed in 5 mL maleate buffer (50 mM, pH 6.0), and the supernatant obtained by centrifugation was diluted 100-fold with maleate buffer immediately before use. Used. 20 μL of a reaction substrate sample and 360 μL of a 0.1% starch (Merck) solution and 20 μL of an enzyme solution were mixed and reacted at 37 ° C. for 20 minutes. An iodine solution was added to the reaction solution, and the amount of residual starch was quantified at an absorption wavelength of 630 nm. The inhibition rate was calculated as follows.
(Inhibition rate%) = (1− (Enzyme activity when tea is added) / (Enzyme activity when tea is not added)) × 100
“Enzyme activity” is the difference between the amount of starch when no enzyme is added and the amount of starch remaining at the end of the reaction. Each tea was serially diluted to determine the inhibition rate for each dilution rate, and the dilution rate giving 50% inhibition was calculated from the prediction of the linear trend, and the IC50 value was obtained. The results are shown in FIG.
From FIG. 1, the dilution ratios of various teas in IC50 are 0.73 for Dairi tea, 0.45 for Yabukita tea containing 50 ppm CT-1, and 0.86 for Yabukita tea containing 12.5 ppm CT-1. Was not active. Yabukita tea containing at least 50 ppm or more of CT-1 was confirmed to have α-amylase inhibitory activity higher than Dairi tea extract.

(CT−1含有飲料の血糖上昇抑制効果)
マウス(9週齢雄性ddYマウス)を用いた評価系(経口糖負荷試験)により、CT−1含有飲料の有するα−アミラーゼ阻害作用を評価した。被検溶液は、コントロールとして、2g/10mLでんぷん水溶液を用いた。また、CT−1含有水として、2gでんぷんをそれぞれ含むCT-1水溶液を25mg/10mLおよび100mg/10mLの濃度で調製した。大理茶として、上述のとおりに調製した大理茶抽出液に2g/10mLでんぷん水溶液を添加して用いた。一晩絶食したマウスに被検溶液をマウス体重1kgあたり10mL経口投与し、経時的に血糖値を測定した。25mg/10mLおよび100mg/10mLのCT−1含有水は、デンプン摂取時のマウスの血糖上昇を有意に抑制した(図2)。一方、大理茶を投与した場合は、血糖値の上昇抑制作用は観察されなかった(図3)。
(Effect of CT-1-containing beverage on increase in blood sugar)
The α-amylase inhibitory action of the CT-1-containing beverage was evaluated by an evaluation system (oral glucose tolerance test) using mice (9-week-old male ddY mice). As a test solution, a 2 g / 10 mL starch aqueous solution was used as a control. Moreover, CT-1 aqueous solution each containing 2 g starch as CT-1 containing water was prepared with the density | concentration of 25 mg / 10mL and 100 mg / 10mL. As Dairi tea, 2 g / 10 mL aqueous starch solution was added to the Dairi tea extract prepared as described above. The test solution was orally administered to mice fasted overnight, and 10 mg / kg of mouse body weight was orally administered, and blood glucose levels were measured over time. 25 mg / 10 mL and 100 mg / 10 mL of CT-1 containing water significantly suppressed the increase in blood glucose level of mice upon ingestion of starch (FIG. 2). On the other hand, when Dairi tea was administered, the blood glucose level increase inhibitory effect was not observed (FIG. 3).

(試験結果からのヒト用量推定)
推定1:体表面積換算
マウス有効量を25mg、マウス体重を40g、ヒト体重を50kgとした場合、(ヒト有効量)=25(mg)×0.04(kg)×50(kg)2/3/0.04(kg)2/3=116.03(mg)となる。容器詰め飲料の容量を500mLとすれば、本有効量を含有させるには、0.116(g)/ 500 (g)× 100 = 0.02(質量%)となる。
(Dose estimation from test results)
Estimated 1: Body surface area conversion When the mouse effective amount is 25 mg, the mouse body weight is 40 g, and the human body weight is 50 kg, (human effective amount) = 25 (mg) × 0.04 (kg) × 50 (kg) 2/3 /0.04 (kg) 2/3 = 116.03 (mg). If the capacity of the container-packed beverage is 500 mL, 0.116 (g) / 500 (g) × 100 = 0.02 (mass%) in order to contain this effective amount.

推定2:体重換算
マウス有効量を25mg、マウス体重を40g、ヒト体重を50kgとした場合、(ヒト有効量)=25(mg/kg)×50(kg)=1250(mg)となる。容器詰め飲料の容量を500mLとすれば、本有効量を含有させるには、1.25(g)/500(g)×100=0.25(質量%)となる。
Estimated 2: Body weight conversion When the mouse effective amount is 25 mg, the mouse body weight is 40 g, and the human body weight is 50 kg, (human effective amount) = 25 (mg / kg) × 50 (kg) = 1250 (mg). If the capacity of the container-packed beverage is 500 mL, to contain this effective amount, 1.25 (g) / 500 (g) × 100 = 0.25 (mass%).

Claims (6)

1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを高濃度で含有する飲食品。   A food or drink containing a high concentration of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose. 1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの含有量が100mg以上である、請求項1記載の飲食品。   The food or drink according to claim 1, wherein the content of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose is 100 mg or more. 1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースの含有量が0.02質量%以上、請求項1記載の飲食品。   The food or drink according to claim 1, wherein the content of 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose is 0.02% by mass or more. 1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを有効成分として含有する血糖上昇抑制剤。   A blood sugar elevation inhibitor containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose as an active ingredient. 1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを有効成分として含有するα−アミラーゼ阻害剤。   An α-amylase inhibitor containing 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose as an active ingredient. 1,2−ジ−O−ガロイル−4,6−HHDP−b−d−グルコピラノースを有効成分として含有する糖尿病の予防又は治療剤。   A prophylactic or therapeutic agent for diabetes comprising 1,2-di-O-galloyl-4,6-HHDP-bd-glucopyranose as an active ingredient.
JP2010050891A 2010-03-08 2010-03-08 Food and drink including 1, 2-di-o-galloyl-4,6-hhdp-b-d-glucopyranose at high concentration Pending JP2011182703A (en)

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WO2018138929A1 (en) * 2017-01-30 2018-08-02 オリザ油化株式会社 Circadian rhythm regulator

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