JP5739180B2 - インスリン分泌促進用油脂組成物 - Google Patents
インスリン分泌促進用油脂組成物 Download PDFInfo
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- JP5739180B2 JP5739180B2 JP2011018534A JP2011018534A JP5739180B2 JP 5739180 B2 JP5739180 B2 JP 5739180B2 JP 2011018534 A JP2011018534 A JP 2011018534A JP 2011018534 A JP2011018534 A JP 2011018534A JP 5739180 B2 JP5739180 B2 JP 5739180B2
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Description
本発明のインスリン分泌促進用油脂組成物(以下、油脂組成物という。)の有効成分の1つであるトリアシルグリセロールは、分子内に中鎖脂肪酸残基を1つ又は2つ有し、且つ、構成脂肪酸として、炭素数6〜12の中鎖脂肪酸と炭素数16〜24の長鎖脂肪酸とを含有する。すなわち、トリアシルグリセロールの形態としては、1分子のトリアシルグリセロール中に構成脂肪酸として中鎖脂肪酸のみが存在する中鎖脂肪酸トリアシルグリセロール(以下、MCTという。)、長鎖脂肪酸のみが存在する長鎖脂肪酸トリアシルグリセロール(以下、LCTという。)、及び中鎖脂肪酸と長鎖脂肪酸とが混在する中・長鎖脂肪酸トリアシルグリセロール(以下、M・LCTという。)があるが、本発明の油脂組成物は、1分子のトリアシルグリセロール中に炭素数6〜12の中鎖脂肪酸と炭素数16〜24の長鎖脂肪酸とを構成脂肪酸として含有するM・LCTを有効成分の1つとして含有する。
本発明の油脂組成物の有効成分の1つである乳化剤は、リン脂質、ショ糖脂肪酸エステル、ポリグリセリン脂肪酸エステル、及びグリセリンモノ脂肪酸エステルからなる群より選ばれる少なくとも1種であり、ポリグリセリン脂肪酸エステル及び/又はグリセリンモノ脂肪酸エステルであることが好ましく、ポリグリセリン脂肪酸エステルであることがより好ましい。ポリグリセリン脂肪酸エステルは、上記トリアシルグリセロールとの併用によるインスリン分泌促進作用が上記乳化剤の中で最も優れるからである。
本発明の油脂組成物では、有効成分である乳化剤としてリン脂質を含有してもよい。本発明の油脂組成物において、リン脂質は、特に限定されるものではなく、例えば、動植物由来のリン脂質、酵素合成や化学合成により得られたリン脂質等が挙げられ、好ましくは動植物由来のリン脂質である。リン脂質の種類は、特に限定されるものではなく、例えば、ホスファチジルコリン(PC)、ホスファチジルエタノールアミン(PE)、ホスファチジルイノシトール(PI)、ホスファチジルセリン(PS)、ホスファチジン酸(PA)等のグリセロリン脂質、リゾホスファチジルコリン(LPC)等のグリセロリゾリン脂質、スフィンゴリン脂質等のリン脂質が挙げられ、これらの1種又は2種以上の混合物を用いてもよい。
本発明の油脂組成物では、有効成分である乳化剤としてショ糖脂肪酸エステルを含有してもよい。ショ糖脂肪酸エステルは、親水性部分としてのショ糖と、親油性部分としての1つ以上の脂肪酸とをエステル結合してなる。ショ糖には8個の水酸基があるため、ショ糖脂肪酸エステルにはモノエステルからオクタエステルまで種々のものが存在し得るが、本発明では、ショ糖脂肪酸エステルの平均置換度(ショ糖の水酸基に結合している脂肪酸の数の平均値)は、特に限定されるものではない。また、ショ糖脂肪酸エステルのHLB値についても、特に限定されるものではないが、インスリン分泌促進効果が顕著であるという点において、4〜16であることが好ましく、8〜14であることがより好ましく、10〜12であることが更により好ましい。なお、本発明の油脂組成物において、異なるHLBのショ糖脂肪酸エステルを2種以上含有する場合には、それらのHLBの平均値を意味する。ここで、HLB値は、界面活性剤における親水性と疎水性のバランスを表す数値であり、例えば、「食品用乳化剤−基礎と応用−」(戸田義郎ら、(株)光琳)p.13に記載の方法により求めることができる。
本発明の油脂組成物では、有効成分である乳化剤としてポリグリセリン脂肪酸エステルを含有してもよい。本発明の油脂組成物において、ポリグリセリン脂肪酸エステルは、特に限定されるものではないが、インスリン分泌促進効果が顕著であるという点において、好ましくはHLBが4〜15であり、より好ましくは4〜9である。なお、本発明の油脂組成物において、異なるHLBのポリグリセリン脂肪酸エステルを2種以上含有する場合には、それらの平均HLB値を意味する。
本発明の油脂組成物では、有効成分である乳化剤としてグリセリンモノ脂肪酸エステルを含有してもよい。グリセリン1分子と脂肪酸1分子とがエステル結合したものである。本発明の油脂組成物では、グリセリンモノ脂肪酸エステルを構成する脂肪酸は、特に限定されるものではなく、その炭素数が通常6〜24、好ましくは8〜12、より好ましくは8〜10の飽和又は不飽和脂肪酸である。具体的には、カプロン酸(n−ヘキサン酸)、カプリル酸(n−オクタン酸)、カプリン酸(n−デカン酸)、ラウリン酸、ミリスチン酸、パルミチン酸、パルミトレイン酸、ステアリン酸、オレイン酸、リノール酸、リノレン酸、アラキジン酸、アラキドン酸、ベヘン酸、エルカ酸、リグノセリン酸等が挙げられる。これらの中でも、炭素数8のn−オクタン酸が好ましい。
上記トリアシルグリセロールは、糖(グルコース)を摂取する際に、単独摂取することで、血漿のインスリン濃度を上昇させることができる。また、上記乳化剤は、糖を摂取する際に、LCTと併用することで、血漿のインスリン濃度を上昇させることができる。これに対して、上記トリアシルグリセロールと上記乳化剤とを有効成分として含有する本発明の油脂組成物によれば、上記トリアシルグリセロールと上記乳化剤との相乗効果により、血漿のインスリン濃度を顕著に上昇させることができる。このような本発明の油脂組成物は、インスリンの分泌量を高める必要がある糖尿病又はその予備軍に該当するヒトを含む動物に対して有効に作用する。特に、インスリン分泌量が低下するインスリン分泌不全を伴うII型糖尿病の予防又は治療に好適である。ここで、予防とは、例えば、発症の抑制、遅延等を意味し、治療とは、例えば、進行の遅延、症状の緩和、軽減、改善等を意味する。
糖負荷を与えたラットを用いて、LCTを対照に、本発明の油脂組成物(MLCT+乳化剤)の血漿インスリン分泌促進効果を検討した。
40%グルコース(D(+)−Glucose,和光純薬社製)溶液10mlに、LCT(商品名:日清キャノーラ油,日清オイリオグループ社製)2gと、牛血清アルブミン(SIGMA社製)200mgとを添加し、得られた溶液を氷上で冷却しながら超音波処理(5分間を2セット、合計10分間)し、試料1を得た。対照として用いたLCT(商品名:日清キャノーラ油,日清オイリオグループ社製)の脂肪酸組成を表1に示す。
MCT(商品名:O.D.O,構成脂肪酸:n−オクタン酸/n−デカン酸=3/1,日清オイリオグループ社製)と、LCT(商品名:日清キャノーラ油,日清オイリオグループ社製)と、を14:86(質量比)の割合で混合し、混合油を得た。得られた混合油に、リパーゼ粉末を上記混合油に対して0.1質量%添加した後、60℃で15時間撹拌し、エステル交換反応させた。次いで、反応生成物からリパーゼ粉末を濾別し、濾液を水洗、乾燥後、脱色、脱臭して、MCTとLCTとのエステル交換油(MLCT)を得た。そして、40%グルコース(D(+)−Glucose,和光純薬社製)溶液10mlに、上記MLCT2gと、乳化剤(トリオレイン酸ペンタグリセリン,商品名:サンソフトA−173E,HLB:7,太陽化学社製)20mgと、牛血清アルブミン(SIGMA社製)200mgとを添加し、得られた溶液を氷上で冷却しながら超音波処理(5分間を2セット、合計10分間)し、試料2を得た。
糖負荷を与えたラットを用いて、LCTを対照に、LCT+乳化剤の血漿インスリン分泌促進効果を検討した。
40%グルコース(D(+)−Glucose,和光純薬社製)溶液10mlに、LCT(商品名:日清キャノーラ油,日清オイリオグループ社製)2gと、乳化剤(トリオレイン酸ペンタグリセリン,商品名:サンソフトA−173E,HLB:7,太陽化学社製)20mgと、牛血清アルブミン(SIGMA社製)200mgとを添加し、得られた溶液を氷上で冷却しながら超音波処理(5分間を2セット、合計10分間)し、試料3を得た。
糖負荷を与えたラットを用いて、LCTを対照に、MLCTの血漿インスリン分泌促進効果を検討した。
40%グルコース(D(+)−Glucose,和光純薬社製)溶液10mlに、上記製造例2にて得たMLCT2gと、牛血清アルブミン(SIGMA社製)200mgとを添加し、得られた溶液を氷上で冷却しながら超音波処理(5分間を2セット、合計10分間)し、試料4を得た。
糖負荷を与えたラットを用いて、LCTを対照に、MCTとLCTとの混合油(MCT+LCT)の血漿インスリン分泌促進効果を検討した。
MCT(商品名:O.D.O,構成脂肪酸:n−オクタン酸/n−デカン酸=3/1,日清オイリオグループ社製)と、LCT(商品名:日清キャノーラ油,日清オイリオグループ社製)と、を14:86(質量比)の割合で混合し、MCTとLCTの混合油(MCT+LCT)を得た。そして、40%グルコース(D(+)−Glucose,和光純薬社製)溶液10mlに、上記MCT+LCT2gと、牛血清アルブミン(SIGMA社製)200mgとを添加し、得られた溶液を氷上で冷却しながら超音波処理(5分間を2セット、合計10分間)し、試料5を得た。
糖尿病モデル動物を用いて、LCTを対照に、本発明の油脂組成物(MLCT+乳化剤)の血漿インスリン分泌促進効果を検討した。
Claims (4)
- トリアシルグリセロールと乳化剤とを有効成分として含有し、
前記トリアシルグリセロールは、分子内に中鎖脂肪酸残基を1つ又は2つ有し、且つ、構成脂肪酸として、炭素数6〜12の中鎖脂肪酸と炭素数16〜24の長鎖脂肪酸とを含有し、
前記乳化剤は、リン脂質、ショ糖脂肪酸エステル、ポリグリセリン脂肪酸エステル、及びグリセリンモノ脂肪酸エステルからなる群より選ばれる少なくとも1種であることを特徴とする、糖尿病の治療又は予防のための医薬組成物。 - 前記トリアシルグリセロールの構成脂肪酸は、炭素数6〜12の中鎖脂肪酸と炭素数16〜24の長鎖脂肪酸とからなる請求項1に記載の医薬組成物。
- 前記中鎖脂肪酸が炭素数8及び/又は10の飽和脂肪酸である請求項1又は2に記載の医薬組成物。
- 前記乳化剤は、ポリグリセリン脂肪酸エステル及び/又はグリセリンモノ脂肪酸エステルである請求項1〜3のいずれか1項に記載の医薬組成物。
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