JP2020132576A - サルコペニア肥満予防・改善剤 - Google Patents
サルコペニア肥満予防・改善剤 Download PDFInfo
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- JP2020132576A JP2020132576A JP2019028773A JP2019028773A JP2020132576A JP 2020132576 A JP2020132576 A JP 2020132576A JP 2019028773 A JP2019028773 A JP 2019028773A JP 2019028773 A JP2019028773 A JP 2019028773A JP 2020132576 A JP2020132576 A JP 2020132576A
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- Prior art keywords
- extract
- fucoxanthin
- acid
- fucoxanthinol
- active ingredient
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Abstract
Description
先行研究において、実験動物に対しフコキサンチンを摂取させた結果、白色脂肪組織の重量増加が抑制される(Maeda et al., 2007; Maeda et al., 2009)ことや、フコキサンチンの代謝産物であるフコキサンチノールが脂肪細胞の成長・成熟を抑制する(Maeda et al., 2006)という報告はされている。しかし,肥大化した脂肪細胞を分解して縮小化することも抗肥満においては肝要であるものの、 この観点でのフコキサンチンの有効性を検証した例は乏しい。
一方、筋萎縮に対するフコキサンチンの効果は明らかとなってはいないが、β-カロテンをマウスに投与することによって、活性酸素による筋萎縮を抑制したことが確認されている(Ogawa et al., 2013)。
しかしながら、フコキサンチン及びフコキサンチノールにおいて肥満予防効果(内臓脂肪減少)及び筋萎縮抑制効果の双方の作用を有することは知られていない。
即ち、本発明は、肥満予防効果及び筋萎縮抑制効果の双方を有する新規な成分を有効成分とするサルコペニア肥満予防改善剤を提供することを目的とする。
1.フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とするサルコペニア肥満予防改善剤。
2.フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とする成熟脂肪細胞における脂肪分解活性亢進剤。
3.フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とする内臓脂肪減少剤。
4.フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とする骨格筋細胞における筋萎縮抑制剤。
5.フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とするサルコペニア肥満予防改善剤であって、前記サルコペニア肥満予防改善剤は、成熟脂肪細胞における脂肪分解活性を亢進し、且つ骨格筋細胞において筋萎縮を抑制することによりサルコペニア肥満を予防改善することを特徴とするサルコペニア肥満予防改善剤。
6.フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とするサルコペニア肥満予防改善剤であって、前記サルコペニア肥満予防改善剤は、内臓脂肪を減少させ、且つ骨格筋細胞において筋萎縮を抑制することによりサルコペニア肥満を予防改善することを特徴とするサルコペニア肥満予防改善剤。
本発明は、フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とすることを特徴とする。
また、天然物からフコキサンチンを得る場合、その原料は特に限定されないが、例えば、海藻類、褐藻類、微細藻類等が挙げられる。尚、これらは、何れか一方のみを用いても良いし、これらを併用しても良い。これらのうち、特に微細藻類から抽出することが好ましい。
上記「褐藻類」としては、例えば、コンブ科(Laminariaceae)、ツルモ科(Chordaceae)等のコンブ目(Laminariales)、ヒバマタ科(Fucaceae)、ホンダワラ科(Sargassaceae)等のヒバマタ目(Fucales)、ナガマツモ科(Chordaceae)、モズク科(Spermatochnaceae)等のナガマツモ目(Chordariales)に属する褐藻類等がより好ましいがこれらに限定されない。尚、これらは1種のみ用いても良いし、2種以上併用しても良い。
上記「微細藻類」は特に限定されないが、例えば、Phaeodactylum tricornutumを用いることが好ましい。より高濃度なフコキサンチンを得ることができるからである。
なお、精製方法としては、例えば、活性炭処理、樹脂吸着処理、イオン交換樹脂、液−液向流分配等の方法が挙げられる。
また、フコキサンチン及び/又はフコキサンチノールを、例えば、油脂、エタノール、グリセリンあるいはこれらの混合物に溶解して液状にし、飲料に添加するか、固形食品に添加することが可能である。必要に応じてアラビアガム、デキストリン等のバインダーと混合して粉末状あるいは顆粒状にし、飲料に添加するか固形食品に添加することも可能である。
サルコペニア肥満予防改善剤の配合比は、剤型によって適宜変更することが可能であるが、通常、経口または粘膜吸収により投与される場合は約0.3〜15.0wt%、非経口投与による場合は、0.01〜10wt%程度にするとよい。なお、投与量は種々の条件で異なるので、前記投与量より少ない量で十分な場合もあるし、また、範囲を超えて投与する必要のある場合もある。
また、本発明のサルコペニア肥満予防改善剤を配合しうる医薬品または医薬部外品の形態としては、軟膏剤、クリーム剤、外用液剤等が挙げられる。
例を以下に羅列するが、本発明はこれらの例に限定されるものではない。
(1)油分の例
エステル系の油相成分:トリ2−エチルヘキサン酸グリセリル、2−エチルヘキサン酸セチル、ミリスチン酸イソプロピル、ミリスチン酸ブチル、パルミチン酸イソプロピル、ステアリン酸エチル、パルミチン酸オクチル、イソステアリン酸イソセチル、ステアリン酸ブチル、ミリスチン酸ブチル、リノール酸エチル、リノール酸イソプロピル、オレイン酸エチル、ミリスチン酸イソセチル、ミリスチン酸イソステアリル、パルミチン酸イソステアリル、ミリスチン酸オクチルドデシル、イソステアリン酸イソセチル、セバシン酸ジエチル、アジピン酸ジイソプロピル、ネオペンタン酸イソアラキル、トリ(カプリル・カプリン酸)グリセリル、トリ2−エチルヘキサン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、テトラ2−エチルヘキサン酸ペンタエリスリトール、カプリル酸セチル、ラウリン酸デシル、ラウリン酸ヘキシル、ミリスチン酸デシル、ミリスチン酸ミリスチル、ミリスチン酸セチル、ステアリン酸ステアリル、オレイン酸デシル、リシノレイン酸セチル、ラウリン酸イソステアリル、ミリスチン酸イソトリデシル、ミリスチン酸イソセチル、ミリスチン酸イソステアリル、パルミチン酸イソセチル、パルミチン酸イソステアリル、ステアリン酸オクチル、ステアリン酸イソセチル、オレイン酸イソデシル、オレイン酸オクチルドデシル、リノール酸オクチルドデシル、イソステアリン酸イソプロピル、2−エチルヘキサン酸セトステアリル、2−エチルヘキサン酸ステアリル、イソステアリン酸ヘキシル、ジオクタン酸エチレングリコール、ジオレイン酸エチレングリコール、ジカプリン酸プロピレングリコール、ジ(カプリル・カプリン酸)プロピレングリコール、ジカプリル酸プロピレングリコール、ジカプリン酸ネオペンチルグリコール、ジオクタン酸ネオペンチルグリコール、トリカプリル酸グリセリル、トリウンデシル酸グリセリル、トリイソパルミチン酸グリセリル、トリイソステアリン酸グリセリル、ネオペンタン酸オクチルドデシル、オクタン酸イソステアリル、イソノナン酸オクチル、ネオデカン酸ヘキシルデシル、ネオデカン酸オクチルドデシル、イソステアリン酸イソセチル、イソステアリン酸イソステアリル、イソステアリン酸オクチルデシル、ポリグリセリンオレイン酸エステル、ポリグリセリンイソステアリン酸エステル、炭酸ジプロピル、炭酸ジアルキル(C12−18)、クエン酸トリイソセチル、クエン酸トリイソアラキル、クエン酸トリイソオクチル、乳酸ラウリル、乳酸ミリスチル、乳酸セチル、乳酸オクチルデシル、クエン酸トリエチル、クエン酸アセチルトリエチル、クエン酸アセチルトリブチル、クエン酸トリオクチル、リンゴ酸ジイソステアリル、ヒドロキシステアリン酸2−エチルヘキシル、コハク酸ジ2−エチルヘキシル、アジピン酸ジイソブチル、セバシン酸ジイソプロピル、セバシン酸ジオクチル、ステアリン酸コレステリル、イソステアリン酸コレステリル、ヒドロキシステアリン酸コレステリル、オレイン酸コレステリル、オレイン酸ジヒドロコレステリル、イソステアリン酸フィトステリル、オレイン酸フィトステリル、12−ステアロイルヒドロキシステアリン酸イソセチル、12−ステアロイルヒドロキシステアリン酸ステアリル、12−ステアロイルヒドロキシステアリン酸イソステアリル等が挙げられる。
炭化水素系の油相成分:スクワラン、流動パラフィン、α−オレフィンオリゴマー、イソパラフィン、セレシン、パラフィン、流動イソパラフィン、ポリブテン、マイクロクリスタリンワックス、ワセリン等が挙げられる。
動植物油とその硬化油、および天然由来のロウ:牛脂、硬化牛脂、豚脂、硬化豚脂、馬油、硬化馬油、ミンク油、オレンジラフィー油、魚油、硬化魚油、卵黄油等の動物油およびその硬化油、アボカド油、アルモンド油、オリーブ油、カカオ脂、杏仁油、ククイナッツ油、ゴマ油、小麦胚芽油、コメ胚芽油、コメヌカ油、サフラワー油、シアバター、大豆油、月見草油、シソ油、茶実油、ツバキ油、トウモロコシ油、ナタネ油、硬化ナタネ油、パーム核油、硬化パーム核油、パーム油、硬化パーム油、ピーナッツ油、硬化ピーナッツ油、ヒマシ油、硬化ヒマシ油、ヒマワリ油、ブドウ種子油、ホホバ油、硬化ホホバ油、マカデミアナッツ油、メドホーム油、綿実油、硬化綿実油、ヤシ油、硬化ヤシ油等の植物油およびその硬化油、ミツロウ、高酸価ミツロウ、ラノリン、還元ラノリン、硬化ラノリン、液状ラノリン、カルナバロウ、モンタンロウ等のロウ等が挙げられる。
シリコーン系の油相成分:ジメチルポリシロキサン、メチルフェニルポリシロキサン、メチルシクロポリシロキサン、オクタメチルポリシロキサン、デカメチルポリシロキサン、ドデカメチルシクロシロキサン、メチルハイドロジェンポリシロキサン、ポリエーテル変性オルガノポリシロキサン、ジメチルシロキサン・メチルセチルオキシシロキサン共重合体、ジメチルシロキサン・メチルステアロキシシロキサン共重合体、アルキル変性オルガノポリシロキサン、末端変性オルガノポリシロキサン、アミノ変性シリコーン油、アミノ変性オルガノポリシロキサン、ジメチコノール、シリコーンゲル、アクリルシリコーン、トリメチルシロキシケイ酸、シリコーンRTVゴム等が挙げられる。
フッ素系の油相成分:パーフルオロポリエーテル、フッ素変性オルガノポリシロキサン、フッ化ピッチ、フルオロカーボン、フルオロアルコール、フルオロアルキル・ポリオキシアルキレン共変性オルガノポリシロキサン等が挙げられる。
(2)高級アルコールの例
ラウリルアルコール、ミリスチルアルコール、セチルアルコール、ステアリルアルコール、イソステアリルアルコール、オレイルアルコール、ベヘニルアルコール、2−エチルヘキサノール、ヘキサデシルアルコール、オクチルドデカノール等が挙げられる。
(3)脂肪酸の例
カプリル酸、カプリン酸、ウンデシレン酸、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、イソステアリン酸、オレイン酸、リノール酸、リノレン酸、アラキン酸、アラキドン酸、ベヘン酸、エルカ酸、2−エチルヘキサン酸等が挙げられる。
(4)紫外線吸収剤の例
パラアミノ安息香酸、パラアミノ安息香酸アミル、パラアミノ安息香酸エチルジヒドロキシプロピル、パラアミノ安息香酸グリセリル、パラアミノ安息香酸エチル、パラアミノ安息香酸オクチル、パラアミノ安息香酸オクチルジメチル、サリチル酸エチレングリコール、サリチル酸オクチル、サリチル酸トリエタノールアミン、サリチル酸フェニル、サリチル酸ブチルフェニル、サリチル酸ベンジル、サリチル酸ホモメンチル、ケイ皮酸ベンジル、パラメトキシケイ皮酸オクチル、パラメトキシケイ皮酸2−エチルヘキシル、ジパラメトキシケイ皮酸モノ2−エチルヘキサン酸グリセリル、パラメトキシケイ皮酸イソプロピル、パラメトキシヒドロケイ皮酸ジエタノールアミン塩、ジイソプロピル・ジイソプロピルケイ皮酸エステル混合物、ウロカニン酸、ウロカニン酸エチル、ヒドロキシメトキシベンソフェノン、ヒドロキシメトキシベンゾフェノンスルホン酸及びその塩、ジヒドロキシメトキシベンゾフェノン、ジヒドロキシメトキシベンゾフェノンジスルホン酸ナトリウム、ジヒドロキシベンゾフェノン、ジヒドロキシジメトキシベンゾフェノン、ヒドロキシオクトキシベンゾフェノン、テトラヒドロキシベンゾフェノン、ブチルメトキシジベンゾイルメタン、2、4、6−トリアニリノ−p−(カルボ−2−エチルヘキシル−1−オキシ)−1、3、5−トリアジン、2−(2−ヒドロキシ−5−メチルフェニル)ベンゾトリアゾール、メチル−O−アミノベンゾエート、2−エチルヘキシル−2−シアノ−3、3−ジフェニルアクリレート、フェニルベンゾイミダゾール硫酸、3−(4−メチルベンジリデン)カンフル、イソプロピルジベンゾイルメタン、4−(3、4−ジメトキシフェニルメチレン)−2、5−ジオキソ−1−イミダゾリジンプロピオン酸2−エチルヘキシル等、およびこれらの高分子誘導体やシラン誘導体等が挙げられる。
(5)粉体・顔料の例
赤色104号、赤色201号、黄色4号、青色1号、黒色401号等の色素、黄色4号ALレーキ、黄色203号BAレーキ等のレーキ色素、ナイロンパウダー、シルクパウダー、ウレタンパウダー、テフロン(登録商標)パウダー、シリコーンパウダー、ポリメタクリル酸メチルパウダー、セルロースパウダー、デンプン、シリコーンエラストマー球状粉体、ポリエチレン末等の高分子、黄酸化鉄、赤色酸化鉄、黒酸化鉄、酸化クロム、カーボンブラック、群青、紺青等の有色顔料、酸化亜鉛、酸化チタン、酸化セリウム等の白色顔料、タルク、マイカ、セリサイト、カオリン、板状硫酸バリウム等の体質顔料、雲母チタン等のパール顔料、硫酸バリウム、炭酸カルシウム、炭酸マグネシウム、珪酸アルミニウム、珪酸マグネシウム等の金属塩、シリカ、アルミナ等の無機粉体、ステアリン酸アルミニウム、ステアリン酸マグネシウム、パルミチン酸亜鉛、ミリスチン酸亜鉛、ミリスチン酸マグネシウム、ラウリン酸亜鉛、ウンデシレン酸亜鉛等の金属セッケン、ベントナイト、スメクタイト、窒化ホウ素等が挙げられる。これらの粉体の形状(球状、棒状、針状、板状、不定形状、燐片状、紡錘状等)および粒子径に特に制限はない。なおこれらの粉体は、従来公知の表面処理、例えばフッ素化合物処理、シリコーン処理、シリコーン樹脂処理、ペンダント処理、シランカップリング剤処理、チタンカップリング剤処理、油剤処理、N−アシル化リジン処理、ポリアクリル酸処理、金属セッケン処理、アミノ酸処理、レシチン処理、無機化合物処理、プラズマ処理、メカノケミカル処理等によって事前に表面処理されていてもいなくても構わない。
(6)界面活性剤の例
アニオン性界向活性剤:脂肪酸セッケン、α−アシルスルホン酸塩、アルキルスルホン酸塩、アルキルアリルスルホン酸塩、アルキルナフタレンスルホン酸塩、アルキル硫酸塩、POEアルキルエーテル硫酸塩、アルキルアミド硫酸塩、アルキルリン酸塩、POEアルキルリン酸塩、アルキルアミドリン酸塩、アルキロイルアルキルタウリン塩、N−アシルアミノ酸塩、POEアルキルエーテルカルボン酸塩、アルキルスルホコハク酸塩、アルキルスルホ酢酸ナトリウム、アシル化加水分解コラーゲンペプチド塩、パーフルオロアルキルリン酸エステル等が挙げられる。
カチオン性界面活性剤:塩化アルキルトリメチルアンモニウム、塩化ステアリルトリメチルアンモニウム、臭化ステアリルトリメチルアンモニウム、塩化セトステアリルトリメチルアンモニウム、塩化ジステアリルジメチルアンモニウム、塩化ステアリルジメチルベンジルアンモニウム、臭化ベヘニルトリメチルアンモニウム、塩化ベンザルコニウム、塩化ベヘニン酸アミドプロピルジメチルヒドロキシプロピルアンモニウム、ステアリン酸ジエチルアミノエチルアミド、ステアリン酸ジメチルアミノプロピルアミド、ラノリン誘導体第四級アンモニウム塩等が挙げられる。
両性界面活性剤:カルボキシベタイン型、アミドベタイン型、スルホベタイン型、ヒドロキシスルホベタイン型、アミドスルホベタイン型、ホスホベタイン型、アミノカルボン酸塩型、イミタゾリン誘導体型、アミドアミン型等が挙げられる。
ノニオン性界面活性剤:プロピレングリコール脂肪酸エステル、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、ソルビタン脂肪酸エステル、POEソルビタン脂肪酸エステル、POEソルビット脂肪酸エステル、POEグリセリン脂肪酸エステル、POEアルキルエーテル、POE脂肪酸エステル、POE硬化ヒマシ油、POEヒマシ油、POE・POP共重合体、POE・POPアルキルエーテル、ポリエーテル変性シリコーンラウリン酸アルカノールアミド、アルキルアミンオキシド、水素添加大豆リン脂質等が挙げられる。
天然系界面活性剤:レシチン、サポニン、糖系界面活性剤等が挙げられる。
(7)多価アルコール、糖の例
エチレングリコール、ジエチレングリコール、ポリエチレングリコール、プロピレングリコール、ジプロピレングリコール、ポリプロピレングリコール、グリセリン、ジグリセリン、ポリグリセリン、3−メチル−1、3−ブタンジオール、1、3−ブチレングリコール、ソルビトール、マンニトール、ラフィノース、エリスリトール、グルコース、ショ糖、果糖、キシリトール、ラクトース、マルトース、マルチトール、トレハロース、アルキル化トレハロース、混合異性化糖、硫酸化トレハロース、プルラン等が挙げられる。またこれらの化学修飾体等も使用可能である。
(8)高分子の例
アクリル酸エステル/メタクリル酸エステル共重合体(プラスサイズ、互応化学社製)、酢酸ビニル/クロトン酸共重合体(レジン28−1310、NSC社製)、酢酸ビニル/クロトン酸/ビニルネオデカネート共重合体(28−2930、NSC社製)、メチルビニルエーテルマレイン酸ハーフエステル(ガントレッツES、ISP社製)、T−ブチルアクリレート/アクリル酸エチル/メタクリル酸共重合体(ルビマー、BASF社製)、ビニルピロリドン/ビニルアセテート/ビニルプロピオネート共重合体(ルビスコールVAP、BASF社製)、ビニルアセテート/クロトン酸共重合体(ルビセットCA、BASF社製)、ビニルアセテート/クロトン酸/ビニルピロリドン共重合体(ルビセットCAP、BASF社製)、ビニルピロリドン/アクリレート共重合体(ルビフレックス、BASF社製)、アクリレート/アクリルアミド共重合体(ウルトラホールド、BASF社製)、ビニルアセテート/ブチルマレエート/イソボルニルアクリラート共重合体(アドバンテージ、ISP社製)、カルボキシビニルポリマー(カーボポール、BFGoodrich社製)、アクリル酸・メタクリル酸アルキル共重合体(ペミュレン、BFGoodrich社製)等のアニオン性高分子化合物や、ジアルキルアミノエチルメタクリレート重合体の酢酸両性化物(ユカフォーマー、三菱化学社製)、アクリル酸オクチルアクリルアミド/アクリル酸ヒドロキシプロピル/メタクリル酸ブチルアミノエチル共重合体(AMPHOMER、NSC社製)等の両性高分子化合物、ビニルピロリドン/ジメチルアミノエチルメタクリレートの4級化物(GAFQUAT、ISP社製)、メチルビニルイミダゾリウムクロリド/ビニルピロリドン共重合体(ルビコート、BASF社製)等のカチオン性高分子化合物、ポリビニルピロリドン(ルビスコールK、BASF社製)、ビニルピロリドン/酢酸ビニル共重合体(ルビスコールVA、BASF社製)、ビニルピロリドン/ジメチルアミノエチルメタクリレート共重合体(コポリマー937、ISP社製)、ビニルカプロラクタム/ビニルピロリドン/ジメチルアミノエチルメタクリレート共重合体(コポリマーVC713、ISP社製)等のノニオン性高分子化合物等がある。また、セルロースまたはその誘導体、ケラチン及びコラーゲンまたはその誘導体、アルギン酸カルシウム、プルラン、寒天、ゼラチン、タマリンド種子多糖類、キサンタンガム、カラギーナン、ハイメトキシルペクチン、ローメトキシルペクチン、グアーガム、アラビアゴム、結晶セルロース、アラビノガラクタン、カラヤガム、トラガカントガム、アルギン酸、アルブミン、カゼイン、カードラン、ジェランガム、デキストラン等の天然由来高分子化合物も好適に用いることができる。
(9)生理活性成分の例
生理活性成分としては、皮膚に塗布した場合に皮膚に何らかの生理活性を与える物質が挙げられる。例えば、美白成分、抗炎症剤、老化防止剤、紫外線防御剤、スリミング剤、ひきしめ剤、抗酸化剤、発毛剤、育毛剤、保湿剤、血行促進剤、抗菌剤、殺菌剤、乾燥剤、冷感剤、温感剤、ビタミン類、アミノ酸、創傷治癒促進剤、刺激緩和剤、鎮痛剤、細胞賦活剤、酵素成分等が挙げられる。これらの好適な配合成分の例としては、例えばアシタバエキス、アボカドエキス、アマチャエキス、アルテアエキス、アルニカエキス、アロエエキス、アンズエキス、アンズ核エキス、イチョウエキス、ウイキョウエキス、ウコンエキス、ウーロン茶エキス、エイジツエキス、エチナシ葉エキス、オウゴンエキス、オウバクエキス、オウレンエキス、オオムギエキス、オトギリソウエキス、オドリコソウエキス、オランダカラシエキス、オレンジエキス、海水乾燥物、海藻エキス、加水分解エラスチン、加水分解コムギ末、加水分解シルク、カモミラエキス、カロットエキス、カワラヨモギエキス、甘草エキス、カルカデエキス、カキョクエキス、キウイエキス、キナエキス、キューカンバ−エキス、グアノシン、クチナシエキス、クマザサエキス、クララエキス、クルミエキス、グレープフルーツエキス、クレマティスエキス、クロレラエキス、クワエキス、ゲンチアナエキス、紅茶エキス、酵母エキス、ゴボウエキス、コメヌカ発酵エキス、コメ胚芽油、コンフリーエキス、コラーゲン、コケモモエキス、サイシンエキス、サイコエキス、サイタイ抽出液、サルビアエキス、サボンソウエキス、ササエキス、サンザシエキス、サンショウエキス、シイタケエキス、ジオウエキス、シコンエキス、シソエキス、シナノキエキス、シモツケソウエキス、シャクヤクエキス、ショウブ根エキス、シラカバエキス、スギナエキス、セイヨウキズタエキス、セイヨウサンザシエキス、セイヨウニワトコエキス、セイヨウノコギリソウエキス、セイヨウハッカエキス、セ−ジエキス、ゼニアオイエキス、センキュウエキス、センブリエキス、ダイズエキス、タイソウエキス、タイムエキス、茶エキス、チョウジエキス、チガヤエキス、チンピエキス、トウキエキス、トウキンセンカエキス、トウニンエキス、トウヒエキス、ドクダミエキス、トマトエキス、納豆エキス、ニンジンエキス、ニンニクエキス、ノバラエキス、ハイビスカスエキス、バクモンドウエキス、パセリエキス、蜂蜜、ハマメリスエキス、パリエタリアエキス、ヒキオコシエキス、ビサボロール、ビワエキス、フキタンポポエキス、フキノトウエキス、ブクリョウエキス、ブッチャーブルームエキス、ブドウエキス、プロポリス、ヘチマエキス、ベニバナエキス、ペパーミントエキス、ボダイジュエキス、ボタンエキス、ホップエキス、マツエキス、マロニエエキス、ミズバショウエキス、ムクロジエキス、メリッサエキス、モモエキス、ヤグルマギクエキス、ユーカリエキス、ユキノシタエキス、ヨクイニンエキス、ヨモギエキス、ラベンダーエキス、リンゴエキス、レタスエキス、レモンエキス、レンゲソウエキス、ローズエキス、ローズマリーエキス、ローマカミツレエキス、ローヤルゼリーエキス、イチゴエキス、ヒハツエキス、ハスの葉エキス、パフィアエキス、スターフルーツエキス等を挙げることができる。
また、デオキシリボ核酸、ムコ多糖類、ヒアルロン酸ナトリウム、コンドロイチン硫酸ナトリウム、コラーゲン、エラスチン、キチン、キトサン、加水分解卵殻膜などの生体高分子、アミノ酸、加水分解ペプチド、乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウム、ベタイン、ホエイ、トリメチルグリシンなどの保湿成分、スフィンゴ脂質、セラミド、フィトスフィンゴシン、コレステロール、コレステロール誘導体、リン脂質などの油性成分、ε−アミノカプロン酸、グリチルリチン酸、β−グリチルレチン酸、塩化リゾチーム、グアイアズレン、ヒドロコールチゾン等の抗炎症剤、ビタミンA、ビタミンB2、ビタミンB6、ビタミンC、ビタミンD、ビタミンE、パントテン酸カルシウム、ビオチン、ニコチン酸アミド、ビタミンCエステル等のビタミン類、アラントイン、ジイソプロピルアミンジクロロアセテート、4−アミノメチルシクロヘキサンカルボン酸等の活性成分、トコフェロール、カロチノイド、フラボノイド、タンニン、リグナン、サポニン等の抗酸化剤、α−ヒドロキシ酸、β−ヒドロキシ酸などの細胞賦活剤、γ−オリザノール、ビタミンE誘導体などの血行促進剤、レチノール、レチノール誘導体等の創傷治癒剤、アルブチン、コウジ酸、プラセンタエキス、イオウ、エラグ酸、リノール酸、トラネキサム酸、グルタチオン等の美白剤、セファランチン、カンゾウ抽出物、トウガラシチンキ、ヒノキチオール、ヨウ化ニンニクエキス、塩酸ピリドキシン、DL−α−トコフェロール、酢酸DL−α−トコフェロール、ニコチン酸、ニコチン酸誘導体、パントテン酸カルシウム、D−パントテニルアルコール、アセチルパントテニルエチルエーテル、ビオチン、アラントイン、イソプロピルメチルフェノール、エストラジオール、エチニルエストラジオール、塩化カプロニウム、塩化ベンザルコニウム、塩酸ジフェンヒドラミン、タカナール、カンフル、サリチル酸、ノニル酸バニリルアミド、ノナン酸バニリルアミド、ピロクトンオラミン、ペンタテカン酸グリセリル、L−メントール、モノニトログアヤコール、レゾルシン、γ−アミノ酪酸、塩化ベンゼトニウム、塩酸メキシレチン、オーキシン、女性ホルモン、カンタリスチンキ、シクロスポリン、ジンクピリチオン、ヒドロコールチゾン、ミノキシジル、モノステアリン酸ポリオキシエチレンソルビタン、ハッカ油、ササニシキエキス等の育毛剤などが挙げられる。
(10)酸化防止剤の例
亜硫酸水素ナトリウム、亜硫酸ナトリウム、エリソルビン酸、エリソルビン酸ナトリウム、チオジプロピオン酸ジラウリル、トコフェロール、トリルビグアナイド、ノルジヒドログアヤレチン酸、パラヒドロキシアニソール、ブチルヒドロキシアニソール、ジブチルヒドロキシトルエン、ステアリン酸アスコルビル、パルミチン酸アスコルビル、没食子酸オクチル、没食子酸プロピル、カロチノイド、フラボノイド、タンニン、リグナン、サポニン、リンゴエキスやチョウジエキスなとの酸化防止効果の認められる植物エキス等が挙げられる。
(11)溶媒の例
精製水、エタノール、低級アルコール、エーテル類、LPG、フルオロカーボン、N−メチルピロリドン、フルオロアルコール、揮発性直鎮状シリコーン、次世代フロン等が挙げられる。
フコキサンチノールとして和光純薬工業株式会社製フコキサンチノールを使用した。
(1)試験方法
分化誘導後7日目の成熟脂肪細胞を、何も添加しないcontrol群と5μMの濃度のフコキサンチノール添加群に分け、フコキサンチノールの添加を72時間行った。その後、細胞内トリアシルグリセロール(TG) 量、培地中のグリセロール放出量および脂肪酸放出量の測定を、生化学的解析により行った。
成熟脂肪細胞に,フコキサンチノールを添加した結果、脂肪分解指標のグリセロール及び脂肪酸の放出量が有意に増加した(図1. A, B参照)。さらに細胞内中性脂肪量に関して、フコキサンチノール添加群は濃度依存的に有意に低値を示した(図1. C参照)。
これらの結果より、フコキサンチノールを成熟脂肪細胞に添加することで、脂肪の分解が促進され、中性脂肪の蓄積量が顕著に抑制されることが確認された。
(1)試験方法
成熟した筋管細胞を、何も添加しないControl 群、とフコキサンチノール添加群(5μM)に分け、24時間培養を行った。さらに過酸化水素(1mM)を24時間添加することで、酸化ストレス由来の筋萎縮を誘導させた。その際の筋管面積を、免疫染色法を用いて解析を行った。
筋タンパク分解誘導(1mMの過酸化水素を添加)を行った筋細胞に、5μMのフコキサンチノールを添加した結果,筋管を保護していることが確認された(図2(A)参照)。
また、フコキサンチノールを添加するとで、過酸化水素添加群よりも、有意に筋管面積の減少を抑制していた(図2(B)参照)。
これらの結果より、フコキサンチノールは酸化ストレス由来の筋萎縮の程度を緩和することが確認された。
(1)試験方法
対象:ICRマウス(5週齢)を、(1)コントロール群(Control群:n=7)(2)筋萎縮誘導群(DEX群n=7)(3)筋萎縮誘導+フコキサンチン投与群(FX-DEX群n=8)の3条件にわけて飼育した。
実験飼料:Hosokawaら(2010)の実験飼料投与方法を一部改変して実施した。フコキサンチン油(オリザ油化株式会社製「フコレックス−5」)及びコントロール油は混餌し、自由摂取させた。筋萎縮誘導に関しては、蒸留水で懸濁したデキサメタゾン(10mg/L)を自由引水させた(図3を参照)。
実験期間:予備飼育期間を12週間、FX投与を4週間,筋萎縮誘導期間を13日間とした。
測定内容:体重および前脛骨筋湿重量・内臓脂肪量を測定することにより、筋萎縮の抑制に及ぼす影響を評価した。その結果を図4に示す。
図4に示すように、体重に関して、 DEX群、FX-DEX群ではControl群と比較して有意な減少が認められた。一方,前脛骨筋湿重量は,Control群と比較してDEX群では有意に減少していたが(p<0.01)、FX-DEX群では有意な差は認められなかった。これにより、フコキサンチンは脛骨筋量の減少を抑制することが確認された。また、内臓脂肪の重量に関して,FX-DEX群はControl群と比較して,有意に低い値を示した(p<0.01)。これにより、フコキサンチンは内臓脂肪を減少させることが確認された。これらの結果から,FXの投与は内臓脂肪を減少させることができ、前脛骨筋湿重量の減少を抑制することができるため、DEX由来の筋萎縮の程度を和らげることが確認された。
以上により、上記試験例1及び2によれば、成熟脂肪細胞において脂肪の分解が促進され、酸化ストレス由来の筋萎縮の程度を緩和されるので、フコキサンチノールはサルコペニア肥満予防改善剤として有用であることが確認された。
また、試験例3により、フコキサンチンは内臓脂肪を減少させ、前脛骨筋湿重量の減少を抑制することができるため、フコキサンチンはサルコペニア肥満予防改善剤として有用であることが確認された。
配合例1:チューインガム
砂糖 53.0wt%
ガムベース 20.0
グルコース 10.0
水飴 16.0
香料 0.5
サルコペニア肥満予防改善剤 0.5
100.0wt%
還元水飴 40.0wt%
グラニュー糖 20.0
ブトウ糖 20.0
ゼラチン 4.7
水 9.68
ユズ果汁 4.0
ユズフレーバー 0.6
色素 0.02
サルコペニア肥満予防改善剤 1.0
100.0wt%
砂糖 50.0wt%
水飴 33.0
水 14.4
有機酸 2.0
香料 0.2
サルコペニア肥満予防改善剤 0.4
100.0wt%
牛乳 41.5wt%
脱脂粉乳 5.8
砂糖 8.0
寒天 0.15
ゼラチン 0.1
乳酸菌 0.005
サルコペニア肥満予防改善剤 0.4
香料 微量
水 残余
100.0wt%
果糖ブドウ糖液糖 30.0wt%
乳化剤 0.5
サルコペニア肥満予防改善剤 0.3
香料 適量
精製水 残余
100.0wt%
砂糖 76.4wt%
グルコース 19.0
ショ糖脂肪酸エステル 0.2
サルコペニア肥満予防改善剤 0.5
精製水 3.9
100.0wt%
玄米胚芽油 47.0wt%
ユズ種子油 40.0
乳化剤 12.0
サルコペニア肥満予防改善剤 1.0
100.0wt%
乳糖 54.0wt%
結晶セルロース 30.0
澱粉分解物 10.0
グリセリン脂肪酸エステル 5.0
サルコペニア肥満予防改善剤 1.0
100.0wt%
スクワラン 20.0wt%
ミツロウ 5.0
精製ホホバ油 5.0
グリセリン 5.0
グリセリンモノステアレート 2.0
ポリオキシエチレン(20)ソルビタン-
モノステアレート 2.0
サルコペニア肥満予防改善剤 1.0
防腐剤 適量
香料 適量
精製水 残余
100.0wt%
エタノール 5.0wt%
グリセリン 2.0
1,3−ブチレングリコール 2.0
ポリエチレンオレイルエーテル 0.5
クエン酸ナトリウム 0.1
クエン酸 0.1
PEG−60硬化ヒマシ油 0.5
ラウロイルグルタミン酸ジ(フィトステリル/オクチルドデシル)
1.5
サルコペニア肥満予防改善剤 0.1
精製水 残余
100.0wt%
マカデミアナッツ油 2.0wt%
ミリスチン酸オクチルドデシル 10.0
メチルフェニルポリシロキサン 5.0
ベヘニルアルコール 3.0
ステアリン酸 3.0
バチルアルコール 1.0
モノステアリン酸グリセリル 1.0
テトラオレイン酸ポリオキシエチレンソルビット
2.0
水素添加大豆リン脂質 1.0
セラミド 0.1
パルミチン酸レチノール 0.1
防腐剤 適量
ツボクサ抽出物 1.0
サルコペニア肥満予防改善剤 1.0
1、3−ブチレングリコール 5.0
精製水 残余
100.0wt%
スクワラン 4.0wt%
ワセリン 2.5
セタノール 2.0
グリセリン 2.0
親油型モノステアリン酸グリセリン 1.0
ステアリン酸 1.0
L−アルギニン 1.0
サルコペニア肥満予防改善剤 0.5
水酸化カリウム 0.1
香料 微量
精製水 残余
100.0wt%
プロピレングリコール 50.0wt%
エタノール 20.0
硫酸ナトリウム 5.0
サルコペニア肥満予防改善剤 0.5
ラノリン 0.5
アボガド油 0.5
色素 1.5
香料 22.0
100.0wt%
Claims (6)
- フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とするサルコペニア肥満予防改善剤。
- フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とする成熟脂肪細胞における脂肪分解活性亢進剤。
- フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とする内臓脂肪減少剤。
- フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とする骨格筋細胞における筋萎縮抑制剤。
- フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とするサルコペニア肥満予防改善剤であって、前記サルコペニア肥満予防改善剤は、成熟脂肪細胞における脂肪分解活性を亢進し、且つ骨格筋細胞において筋萎縮を抑制することによりサルコペニア肥満を予防改善することを特徴とするサルコペニア肥満予防改善剤。
- フコキサンチン及びフコキサンチノールのうちの少なくとも一方を有効成分とするサルコペニア肥満予防改善剤であって、前記サルコペニア肥満予防改善剤は、内臓脂肪を減少させ、且つ骨格筋細胞において筋萎縮を抑制することによりサルコペニア肥満を予防改善することを特徴とするサルコペニア肥満予防改善剤。
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