JP2019142801A - 脂肪分解促進剤並びに脂肪分解促進剤を含む皮膚外用組成物及び入浴剤組成物 - Google Patents
脂肪分解促進剤並びに脂肪分解促進剤を含む皮膚外用組成物及び入浴剤組成物 Download PDFInfo
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- lipolysis promoter
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Abstract
Description
従来、肥満の解消に用いられる組成物としては、カフェイン、クエン酸といった成分を経口投与することが行われてきたが、安全性の点から、その実用性が限定され満足できる効果が得られにくかった。そこで、植物の抽出成分の肥満解消作用が研究されている。
たとえば、特許文献1には、キョウニンエキス、カノコソウエキス、サンザシエキス、オドリコソウエキス等を経皮投与することにより、血管内皮増殖因子C(VEGFC)発現を誘導し、リンパ管機能の活性化を促進することによる肥満改善剤が記載されている。特許文献2には、ローズオキサイド、シトロネリルアセテート及びニアウリオイルを成分とした、特許文献1と同じ機構による経皮投与の肥満改善剤が記載されている。
肥満とは、脂肪組織に過剰な中性脂肪(トリグリセリド)が蓄積され、脂肪組織が増大する状態を指す。肥満の予防では、この蓄積が抑制されるが、一度蓄積された脂肪組織を縮小させるものではなく痩身は図れない。すなわち、過剰に蓄積された脂肪組織を縮小させるためには、白色脂肪細胞内に脂肪滴として蓄えられている中性脂肪が分解されて消費される必要があり、この過程が蓄積された脂肪組織を縮小させるための第1段階として重要となる。第1段階で中性脂肪が分解されると、その結果として脂肪滴が小さくなり、白色脂肪細胞のサイズの減少につながり、最終的には脂肪組織の体積の減少が生じ、痩身が図られる。
そこで、本発明は、身体に蓄積された脂肪を分解するための、脂肪分解促進剤を提供することを目的とする。
[1]オトギリソウ、ツルシキミ、アモムム・ツァオコ、ブロード−リーブドティーツリー(broad−leaved teatree)及びセイヨウサンザシからなる群から選択される少なくとも1種の植物の抽出物を有効成分として含む、脂肪分解促進剤。
[2]オトギリソウ、ツルシキミ及びアモムム・ツァオコからなる群から選択される少なくとも1種の植物の抽出物を有効成分として含む、[1]の脂肪分解促進剤。
[3][1]又は[2]の脂肪分解促進剤を含む皮膚外用組成物。
[4][1]又は[2]の脂肪分解促進剤を含む入浴剤組成物。
[5]身体の少なくとも一部に塗布して温浴して使用するための[3]の皮膚外用組成物。
脂肪分解促進剤の有効成分となる植物の抽出物に用いられる植物は、以下の植物からなる群から選ばれる少なくとも1種である。
オトギリソウ(学名:Hypericum erectum)、ツルシキミ(学名:Skimmia japonica (Thunb.) var. intermedia Komatsu f. repens)、アモムム・ツァオコ(学名:Amomum tsao−ko)、ブロード−リーブドティーツリー(broad−leaved teatree)(学名:Melaleuca quinquenervia)及びセイヨウサンザシ(学名:Crataegus oxyacantha)。
これらの中でも、オトギリソウ、ツルシキミ及びアモムム・ツァオコが好ましく、オトギリソウがより好ましい。
これらは、1種単独で用いても2種以上組み合わせて用いてもよい。
上記植物は、抽出物にして用いられる。
抽出に用いられる溶媒としては、水、有機溶媒等が挙げられ、組み合わせて用いてもよい。有機溶媒としては、例えば、メタノール、エタノール、プロパノール、ブタノール等の脂肪族アルコール、酢酸エチル、酢酸ブチル等のエステル類、アセトン、メチルエチルケトン等のケトン類が挙げられる。これらは1種単独で用いても、2種以上組み合わせて用いてもよい。
抽出後、必要に応じて、濾過、遠心分離等により抽出残渣を分離してもよい。
本発明にいう脂肪分解促進剤とは、脂肪滴の体積を減少させる効果のあるものをいう。
脂肪滴とは、トリグリセリドやコレステロールなどの脂質を貯蔵する細胞小器官をいい、リン脂質一重層の内部に中性脂肪(トリグリセリド)などの脂質が存在する。
オトギリソウは、0.001mg/ml〜1mg/mlが好ましく、0.01mg/ml〜0.2mg/mlがより好ましい。ツルシキミは、0.001mg/ml〜1mg/mlが好ましく、0.005mg/ml〜0.1mg/mlがより好ましい。アモムム・ツァオコは、0.001mg/ml〜1mg/mlが好ましく、0.01mg/ml〜0.2mg/mlがより好ましい。ブロード−リーブドティーツリーは、0.001mg/ml〜1mg/mlが好ましく、0.005mg/ml〜0.1mg/mlがより好ましい。セイヨウサンザシは、0.001mg/ml〜1mg/ml以上が好ましく、0.01mg/ml〜0.2mg/ml以上がより好ましい。
上記脂肪分解促進剤は、他の成分とともに組成物として用いることができる。この組成物は、痩身用、脂肪分解用、肥満改善用、抗肥満用、肥満予防用、肥満防止用、肥満抑制用等に用いることができ、好ましくは痩身用、脂肪分解用、又は抗肥満用に用いることができ、より好ましくは痩身用に用いることができる。
前記組成物には、任意成分として、他の抗肥満成分を加えることも好ましい。
これらは、1種単独で用いても、2種以上組み合わせて用いてもよい。
後述する実施例1の培地当たりのこれらの植物抽出物の濃度は、イリスは、0.001mg/ml〜1mg/mlが好ましく、0.01mg/ml〜0.2mg/mlがより好ましい。ショウガは、0.001mg/ml〜1mg/ml以上が好ましく、0.005mg/ml〜0.1mg/ml以上がより好ましい。タイムは、0.001mg/ml〜1mg/mlが好ましく、0.01mg/ml〜0.2mg/mlがより好ましい。
上記組成物は、皮膚外用組成物として使用すると、使用部位が引き締まる等の効果が得られる。
皮膚外用組成物には、上記抗肥満成分の他にも薬学上許容される添加剤や皮膚に塗布可能な添加剤を任意成分として含んでいてもよい。
例えば、保湿剤、油性成分、紫外線吸収剤、界面活性剤、増粘剤、アルコール類、粉末成分、スクラブ、色剤、水性成分、水、抗炎症剤、殺菌剤、酸化防止剤、防腐剤、皮膚栄養剤等が挙げられる。
この皮膚外用組成物の剤型は特に限定されるものではないが、化粧水(ローション)及び乳液等の液剤、クリーム剤、ジェル剤、軟膏剤、パック剤、スティック剤、シート剤、パップ剤、粉末剤、顆粒剤等が挙げられる。
上記組成物は、入浴剤組成物として用いることができる。入浴剤組成物には、上記抗肥満成分の他にも入浴剤組成物の成分として公知の成分を任意成分として含んでいてもよい。
このような任意成分としては、界面活性剤、炭酸塩、有機酸、無機顔料、保湿剤、防腐剤、香料、無機塩類、油性成分、滑沢剤、水溶性高分子、白濁剤、着色剤等が例示できる。
皮膚外用組成物及び入浴剤組成物は、本発明の脂肪分解促進剤に必要に応じ上記任意の抗肥満成分及びその他の成分を常法にしたがって混合することにより製造することができる。
なお、実施例における植物抽出物等の濃度は、培地の体積当たりの濃度である。
脂肪前駆細胞(3T3−L1、大日本製薬株式会社製)を、96−well black plate(株式会社グライナー・バイオワン製)に1×104 cells/wellで撒き、10%の牛胎児血清(FBS)(ハイクローン社製)を含有するDMEM培地(低グルコース)(和光純薬工業社製)で37℃−5% CO2インキュベーターにて培養し、増殖させた。24時間培養後、培地を、0.25μM デキサメタゾン、0.5mM 1−メチル−3−イソブチルキサンチン及び1μg/mlのインスリンを含む培地に交換した。48時間かけて脂肪細胞への分化を誘導した後、培地を10%の牛胎児血清(FBS)及び1μg/ml インスリンを含む培地に交換し、その後、1日おきに培地を10%の牛胎児血清(FBS)及び1μg/ml インスリンを含む培地に交換し、4日間培養し、脂肪滴の蓄積サンプルとした。
光学顕微鏡(DIAPHOT、株式会社ニコン製)下で、倍率 100倍で目視により細胞内に脂肪滴が蓄積されたことを確認した。
下記表1に、実施例において使用した植物、その使用部位を示す。抽出方法の詳細は、以下の通りである。抽出には、各植物の使用部位の乾燥粉砕物を使用した。
上記表1に示す部位の粉砕物20gをそれぞれ50容量%エタノール、200ml(10(W/V)倍量)に浸し、2時間加熱還流抽出を行い、濾過後抽出液を得た。抽出液全量を濃縮後、凍結乾燥し、それを蒸留水80mlに溶解又は懸濁させ、酢酸エチル40mlを加えて攪拌、分離した抽出物を得た。得られた抽出物を濃縮後、凍結乾燥し、試験に供した。
脂肪滴の蓄積サンプルの培地を、毎日、10μg/mlのインスリン及び0.025mg/mlのブロード−リーブドティーツリー抽出物を含む培地に交換し、3日間培養を行なった。
培養終了後、培地をリン酸緩衝食塩水(PBS)に置き換え、AdipoRed(登録商標) assay reagent(ロンザ社製)を添加して、脂肪滴を染色した。染色した脂肪滴を蛍光光度計(EnSpire、パーキンエルマー社製)により、572nmで蛍光強度を測定した。得られた測定値の初期値に対する値(%)を求め、その値を100(%)から引いた値を脂肪滴の体積減少率とした。
ブロード−リーブドティーツリー抽出物の代わりに、表2に記載の植物抽出物及び添加量とした以外は、実施例1と同様にして脂肪滴の体積減少率を求めた。
ブロード−リーブドティーツリー抽出物の代わりに、パルミチン酸ヒドロキシクエン酸(HCAP)0.05mg/mlとした以外は、実施例1と同様にして、脂肪滴の体積減少率を求めた。
ブロード−リーブドティーツリー抽出物の代わりに、カフェイン0.05mg/mlとした以外は、実施例1と同様にして、脂肪滴の体積減少率を求めた。
<皮膚外用剤>
成分 配合量(質量%)
ステアリン酸 2.0%
ステアリルアルコール 3.0%
脱臭ラノリン 2.0%
オリーブ油 15.0%
モノステアリン酸グリセリン 2.0%
トリ(カプリル・カプリン酸)グリセリル 5.0%
1,3−ブチレングリコール 3.0%
ソルビトール 1.0%
ジグリセリン 1.0%
キサンタンガム 0.25%
カルボキシビニルポリマー 0.1%
オトギリソウ抽出物 0.02%
ショウガ抽出物 0.02%
香料 微量
精製水 残量
成分 配合量(質量%)
硫酸ナトリウム 69.2%
炭酸水素ナトリウム 23.3%
無水ケイ酸 0.5%
炭酸カルシウム 1.0%
香料 0.8%
オトギリソウ抽出物 0.1%
ショウガ抽出物 0.1%
白濁剤* 5.0%
*白濁剤 酸化チタンのデキストリン被覆物
成分 配合量(質量%)
流動パラフィン 30.0%
コメヌカ油 10.0%
POEセチルエーテル 2.5%
モノパルミチン酸ソルビタン 2.5%
フェノキシエタノール 0.3%
香料 0.5%
オトギリソウ抽出物 0.1%
ショウガ抽出物 0.1%
パラオキシ安息香酸メチル 0.2%
精製水 残量
成分 配合量(質量%)
フマル酸 20.0%
リンゴ酸 18.0%
炭酸水素ナトリウム 21.0%
炭酸ナトリウム 20.0%
硫酸ナトリウム 18.58%
POE(カプリル・カプリン酸)グリセリル 0.2%
エチレンジアミンテトラPOE・POP 0.02%
大豆油 0.3%
ポリビニルピロリドン 0.2%
PEG6000 0.5%
オトギリソウ抽出物 0.1%
ショウガ抽出物 0.1%
香料 1.0%
Claims (5)
- オトギリソウ、ツルシキミ、アモムム・ツァオコ、ブロード−リーブドティーツリー(broad−leaved teatree)及びセイヨウサンザシからなる群から選択される少なくとも1種の植物の抽出物を有効成分として含む、脂肪分解促進剤。
- オトギリソウ、ツルシキミ及びアモムム・ツァオコからなる群から選択される少なくとも1種の植物の抽出物を有効成分として含む、請求項1記載の脂肪分解促進剤。
- 請求項1又は2記載の脂肪分解促進剤を含む皮膚外用組成物。
- 請求項1又は2記載の脂肪分解促進剤を含む入浴剤組成物。
- 身体の少なくとも一部に塗布して温浴して使用するための請求項3記載の皮膚外用組成物。
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JPH02240009A (ja) * | 1989-03-13 | 1990-09-25 | Beijin Riiyuen Riiyon Fuashiyue Guufuen Youshien Gonsuu | 皮膚外用剤 |
JPH03163026A (ja) * | 1989-08-31 | 1991-07-15 | Kao Corp | 血管拡張剤 |
JPH11269079A (ja) * | 1998-03-17 | 1999-10-05 | Shiseido Co Ltd | 脂質分解促進用皮膚外用剤 |
JP2003192605A (ja) * | 2001-12-27 | 2003-07-09 | Fancl Corp | リパーゼ阻害剤 |
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JP2000063259A (ja) * | 1998-08-20 | 2000-02-29 | Shiseido Co Ltd | 脂質分解促進剤及び痩身用皮膚外用剤 |
JP4143223B2 (ja) * | 1999-07-30 | 2008-09-03 | 一丸ファルコス株式会社 | 保湿性植物抽出物を含有する化粧料組成物 |
JP4244093B2 (ja) * | 2000-01-24 | 2009-03-25 | 三省製薬株式会社 | 美白化粧料 |
WO2008034699A1 (en) * | 2006-09-20 | 2008-03-27 | L'oreal | Process for preparing a cosmetic composition from plant or mineral extracts |
JP6527715B2 (ja) * | 2015-02-27 | 2019-06-05 | 株式会社東洋新薬 | 黒生姜含有組成物 |
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