JP2016165282A - 肥満や糖尿病を治療するため及び筋肉量を増加して運動能力を向上させるための組成物であって、有効成分としてヒハツモドキ果実(piperretrofractumvahl.fruits)の抽出成分を含む組成物 - Google Patents
肥満や糖尿病を治療するため及び筋肉量を増加して運動能力を向上させるための組成物であって、有効成分としてヒハツモドキ果実(piperretrofractumvahl.fruits)の抽出成分を含む組成物 Download PDFInfo
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Abstract
【解決手段】ヒハツモドキの抽出成分を含む組成物の新規使用、及び、低減された体重及び体脂肪によって抗肥満効果を発揮し、血中グルコース及び血中インスリンの低減による改善されたインスリン抵抗性によって抗糖尿病効果を発揮し、筋肉に供給されるエネルギー源を増大することによって筋肉量を増加し、増大した耐久性を含む運動能力を向上させる食品組成物や医薬組成物。有機溶媒又は超臨界抽出に寄り得られたヒハツモドキ果実の抽出物成分を有効成分として含み、前記有効成分がUCP活性化誘導熱発生メカニズムをもたらす、抗肥満医薬組成物や食品組成物。
【選択図】なし
Description
病は、相対的に減じられたインスリン分泌と組み合わせ可能なインスリン抵抗性によって特徴付けられる。インスリンに対する身体組織の欠陥のある応答性は、インスリン受容体の減少、IRS−1(インスリン受容体基質−1)の細胞内減少、不良チロシンキナーゼ活性を含む様々な要因と関わる。この疾患は慢性であり、糖尿病性網膜症、腎不全、糖尿病性足のような様々な合併症の続発を伴う様々な代謝性の異常をもたらす。糖尿病の高発生率は先進国で報告されている。
PK)によるリン酸化によって不活性化される。運動はAMPKの活性を増加させて、ACCのリン酸化及び不活性化をもたらし、マロニルCoAの現象を結果として招く。マロニル−CoAの減じられたレベルは、CPT−1の活性化を招き、その結果、アシル化された脂肪酸のミトコンドリアへの流入を増加させる。
<例>抽出成分
ヒハツモドキ果実の乾燥粉末が、4〜10の量(ボリューム)の抽出溶媒と共に抽出装置に置かれ、12時間以上にわたってそのまま放置され或いは超臨界抽出され、その後、抽出成分を与えるために濃縮器における濃縮および乾燥が続く。
ル、エリスリトール及びマルチトール等のサッカリド類と、トウモロコシデンプン、小麦デンプン、米デンプンおよびジャガイモデンプン等のデンプン類と、セルロース、メチルセルロース、ナトリウムカルボキシメチルセルロース及びヒドロキシプロピルメチルセルロース等のセルロース類と、ゼラチンおよびポリビニルピロリドン等の充填剤とを含む。架橋ポリビニルピロリドン、寒天、アルギン酸或いはアルギン酸ナトリウム等の崩壊剤が、必要に応じて、さらに加えられてもよい。また、医薬組成物は、さらに抗凝固剤、潤滑剤、保湿剤、香料、乳化剤、および防腐剤を含みうる。
発明のモード
例示のために記載されるが本発明を限定するものとして解釈されるべきではない以下の実施例を通じて、本発明のより良い理解を得ることができる。
[実験例1]動物モデルにおける体重と脂肪の変化
<1−1>実験動物および食品
抗肥満および抗糖尿病の実験では、マウス(EXT100)の1キログラム当たり100mgの量でヒハツモドキ抽出成分が与えられる一方で、40%脂肪カロリーを有する高脂肪食が用いられた。5週齢の雄性C57BL/6Jマウスは、高脂肪食対照群(HFD群)及びその抽出成分が異なる用量で投与されることになっていた複数の試験群(EXT群)にランダムに分けられ、その後、新しい研究室の環境に1週間慣らされた。それらは7週間にわたって高脂肪食が与えられ、その後にビヒクル(vehicle)またはビヒクル中の抽出物の分散体を8週間にわたって強制的に投与された。
<1−2>体重及び体脂肪の測定
ビヒクル又はビヒクルに分散された抽出成分が8週間にわたって強制的に投与されたマウスは屠殺する直前に秤量した。その後、副睾丸脂肪がマウスから摘出され、秤量された[図1及び図2]。
<2−1>血中グルコース及び血中インスリンの測定
マウスは、本発明のヒハツモドキ抽出成分を8週間摂取した後、6時間絶食させられ、血清がその尾から採取されてグルコースおよびインスリンレベルに関して調べられた。図4および図5に示すように、対照群(HFD)に比べ、血中グルコースおよび血中インスリンのレベルは、テスト材のヒハツモドキ抽出成分が与えられたEXT100群において著しく減少した。
<2−2>HOMA−IRの測定
HOMA−IRは、以下の式に従って、<2−1>で測定された血中グルコースおよびインスリンのレベルから計算された。
図6から分かるように、著しく低下したHOMA−IR値は、対照群(HFD)と比較して、ヒハツモドキ抽出成分が与えられたEXT100グループから検出され、その抽出成分がインスリン抵抗性を向上可能であることを示す。
<3−1>筋肉量の測定
マウスは、ヒハツモドキ抽出成分を8週間摂取した後、マイクロPET/CT(陽電子(ポジトロン)放射断層撮影/コンピュータ断層撮影、INVEON、シーメンス、米国)によって筋肉量が分析された。図8及び図9から分かるように、ヒハツモドキ抽出成分が与えられたPRE100及びPRE300の両者は、対照群(HFD)と比較して、筋肉量が200%大きくなった。
<3−2>筋肉脂肪の測定
筋肉は、ヒハツモドキ抽出成分の8週間の摂取後に屠殺されたマウスから行使され、脂質を可視化するためにヘマトキシリンおよびエオシン(H&E)で染色された。図10から分かるように、筋肉の脂肪含有量の著しい減少は、対照群(HFD)と比較して、抽出成分が与えられたPRE100及びPRE300の両者において見られ、このことは筋肉に蓄えられたIMTG(筋肉内トリグリセリド)がエネルギーの産生により減少したことを示す。
<3−3>運動パフォーマンスのテスト
マウスは、ヒハツモドキ抽出成分の8週間の摂取後に、11m/minの速度のトレッドミルにおいて運動パフォーマンスが評価された。図4から分かるように、運動パフォーマンスは、対照群(HFD)と比べ、抽出成分が与えられたグループであるPRE100及びPRE300の両者において著しく増大した[図11]。
[実験例4]動物モデルにおける抗肥満、抗糖尿病および運動パフォーマンスの向上に関与する遺伝子の上方調節
<4−1>抗肥満関連遺伝子の発現に及ぼす熱発生の影響
3T3−L1脂肪細胞は、10日間、脂肪を形成するためにインスリン、デキサメタゾンおよびIBMXによって、その後ヒハツモドキ抽出成分によって、培養された。ウェスタンブロッティングは、サンプルの一定の負荷を示すα−チューブリンスポット(α−tublin spots)と共に、UCP蛋白質の発現を示した[図3]。
<4−2>抗糖尿病関連遺伝子の発現に及ぼす影響
肝臓は、ヒハツモドキ果実抽出成分が8週間にわたって与えられたマウスから切り取られ、ウエスタンブロット法を行った。そのブロットは、サンプルの一定の負荷を示すα−チューブリンブロット(斑点)と共に、抽出成分がIRS−1の発現を上方調節することを示す[図7]。
<4−3>運動パフォーマンスに関連する遺伝子の発現に及ぼす影響
大腿部の筋肉は、ヒハツモドキ果実抽出成分が8週間にわたって与えられたマウスから切り取られ、ウエスタンブロット法を行った。ウエスタンブロットは、サンプルの一定の負荷を示すα−チューブリンブロットと共に、pAMPK、pACC及びCPT−1の発現を示した[図12]。その抽出成分は、pAMPK、pACC及びCPT−1の発現を上方調節することが観察された。
Claims (18)
- ヒハツモドキ果実抽出成分を有効成分として含み、当該有効成分が体重及び脂肪の低減の要因となるメカニズムをもたらす抗肥満機能性食品組成物。
- 前記ヒハツモドキ果実抽出成分は、有機溶媒によって又は超臨界抽出によって得られる請求項1に記載の抗肥満機能性食品組成物。
- ヒハツモドキ果実抽出成分を有効成分として含み、当該有効成分がUCP活性化誘導熱発生メカニズムをもたらす抗肥満医薬組成物。
- 前記組成物は体重及び脂肪の低減のためのメカニズムを示す請求項3に記載の抗肥満医薬部外品製品。
- 前記ヒハツモドキ果実抽出成分は、前記組成物の総重量に基づいて、0.001wt%から80wt%の量で含まれる請求項3に記載の抗肥満医薬組成物。
- 請求項1に記載の前記組成物を含む抗肥満機能性食品組成物であって、請求項1に記載の当該組成物は、散剤、錠剤、カプセル、シロップ又は飲料の形態であってUCPの活性化によって誘発される熱発生を喚起して体重及び脂肪の低減をもたらす抗肥満機能性食品組成物。
- インスリン抵抗性を改善する抗糖尿病機能性食品組成物であって、ヒハツモドキ果実抽出成分を有効成分として含み、当該有効成分が血中グルコースレベル及び血中インスリンレベルを同時的に低減させる抗糖尿病機能性食品組成物。
- 前記ヒハツモドキ果実抽出成分は、有機溶媒によって又は超臨界抽出によって、果実粉末から得られる請求項7に記載の抗糖尿病機能性食品組成物。
- インスリン抵抗性を改善するための抗糖尿病医薬組成物であって、ヒハツモドキ果実抽出成分を有効成分として含み、当該有効成分がIRS−1活性化メカニズムを誘因する抗糖尿病医薬組成物。
- 前記組成物は、血中グルコースレベルおよび血中インスリンレベルを低減するメカニズムを示す、請求項9に記載のインスリン抵抗性を改善するための抗肥満医薬部外品。
- ヒハツモドキ果実抽出成分は、前記組成物の総重量に対して0.001〜80wt%の量で含まれており、血中グルコースレベルおよび血中インスリンレベルを低減するメカニズムを誘因する請求項3に記載の抗肥満医薬組成物。
- 散剤、顆粒剤、カプセル剤、シロップ、または飲料の形態である請求項7に記載の抗糖尿病機能性食品組成物。
- ヒハツモドキ果実抽出成分を有効成分として含む健康機能性食品組成物であって、当該有効成分は筋肉量を増加させて運動パフォーマンスを高めて疲労を克服するメカニズムを刺激する健康機能性食品組成物。
- 前記ヒハツモドキ果実抽出成分は、有機溶媒又は超臨界抽出によりフルーツパウダーから得られる請求項13に記載の健康機能性食品組成物。
- ヒハツモドキ果実抽出成分を有効成分として含む医薬組成物であって、当該有効成分はAMPK活性化メカニズムを刺激する医薬組成物。
- 前記組成物は、筋肉量を増加して運動パフォーマンスを向上させて疲労を克服する働きを有する請求項15に記載の医薬組成物。
- 前記ヒハツモドキ果実抽出成分は、前記組成物の総重量に対して0.001〜80wt%の量で含まれ、筋肉量を増加させて運動パフォーマンスを高めて疲労を克服する働きを有する請求項15に記載の医薬組成物。
- 前記組成物は、散剤、顆粒、錠剤、カプセル、シロップまたは飲料の形態を有し、筋肉量を増加させて運動パフォーマンスを高めて疲労を克服する働きを有する請求項13に記載の健康機能性食品組成物。
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