JP2015134752A - エンドセリン−1阻害剤及び美白用皮膚外用剤 - Google Patents
エンドセリン−1阻害剤及び美白用皮膚外用剤 Download PDFInfo
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- JP2015134752A JP2015134752A JP2014252836A JP2014252836A JP2015134752A JP 2015134752 A JP2015134752 A JP 2015134752A JP 2014252836 A JP2014252836 A JP 2014252836A JP 2014252836 A JP2014252836 A JP 2014252836A JP 2015134752 A JP2015134752 A JP 2015134752A
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Abstract
本発明の目的はエンドセリン−1の過剰産生を抑制し、皮膚を健全に保つ製剤を得ることであり、特に美白に有効な製剤を得ることにある。
さらには高血圧症、肺高血圧症、くも膜下出血後の脳血管攣縮、腎不全、心筋梗塞、喘息、動脈硬化、血管炎、敗血症等の疾患にも有効な製剤を得ることにある。
【解決手段】
ピロリドンカルボン酸またはその塩、L−アルギニン、L−アスパラギン酸、グリシン、L−アラニン、L−セリン、L−バリン、L−プロリン、L−スレオニン、L−イソロイシン、L−ヒスチジン、L−フェニルアラニンの混合物はエンドセリン−1の産生を促進することがわかび美白にも有効なことがわかった。
【選択図】図1
Description
またエンドセリンは、血管平滑筋収縮作用および血圧上昇作用であることが知られており、現在脚光を浴びている生理活性物質のひとつであり、高血圧症、肺高血圧症、くも膜下出血後の脳血管攣縮、腎不全、心筋梗塞、喘息、動脈硬化、血管炎、敗血症等の疾患に有効である。
さらには高血圧症、肺高血圧症、くも膜下出血後の脳血管攣縮、腎不全、心筋梗塞、喘息、動脈硬化、血管炎、敗血症等の疾患にも有効な製剤を得ることにある。
さらには以下の割合がエンドセリン−1の産生を阻害する効果が高いこともわかった。
ピロリドンカルボン酸またはその塩を20〜50重量部、L−アルギニンを10〜20重量部、L−アスパラギン酸を5〜15重量部、グリシンを2.0〜5.0重量部、L−アラニンを2.0〜5.0重量部、L−セリンを1.0〜3.0重量部、L−バリンを1.0〜2.0重量部、L−プロリンを0.4〜1.2重量部、L−スレオニンを0.4〜1.2重量部、L−イソロイシンを0.4〜1.2重量部、L−ヒスチジンを0.1〜0.5重量部、L−フェニルアラニンを0.1〜0.5重量。
さらに乳酸ナトリウムを配合することによって有効であることもわかった。
上記のアミノ酸の混合物を皮膚外用剤に0.01〜60重量%、好ましくは0.1〜50重量%配合する。
色素類;黄色4号、青色1号、黄色202号等の厚生省令に定められたタール色素別表I及びIIの色素、クロロフィル、リボフラビン、クロシン、紅花、アントラキノン等の食品添加物として認められている天然色素等。
ビタミン類;ビタミンA、ビタミンC、ビタミンD、ビタミンE等。
その他;殺菌剤、防腐剤、その他製剤上必要な成分等。
実施例
ピロリドンカルボン酸ナトリウム 37.5重量部
ピロリドンカルボン酸 10.9重量部
L−アルギニン 20.0重量部
L−アスパラギン酸 13.0重量部
グリシン 3.2重量部
L−アラニン 3.0重量部
L−セリン 2.0重量部
L−バリン 1.6重量部
L−プロリン 1.0重量部
L−スレオニン 1.0重量部
L−イソロイシン 1.0重量部
L−ヒスチジン 0.4重量部
L−フェニルアラニン 0.4重量部
乳酸ナトリウム 30.0重量部
精製水 125.0重量部
以上の原料を充分に撹拌して得られる水溶液。
2継代目のヒト***由来表皮細胞(クラボウ)を50−70%コンフルエントとなるようHuMedia−KG2培地(フェノールレッド不含)で培養後、前日にカルシウム濃度を1.8mMに変更したHuMedia−KG2培地に、実施例を添加し、37℃、5%CO2インキュベータ中で2日間培養した。
細胞からの Total RNAの抽出は、トリプシン/EDTAで剥離後、SV Total RNA Isolation System(プロメガ社)を用い、プロメガ社の添付マニュアル(日本語プロトコールNoTM048J2001年6月作成)に従い調製した。RNA濃度は、NanoDrop1000(Thermo SCIENTIFIC)を用い算出した。
2.5μgのTotal RNAを使い、MMLV Reverse Transcriptase RNaseH−(東洋紡社)を用い、東洋紡社推奨プロトコール(TOYOBO BIOCHEMICALS FOR LIFE SCIENCE 2008/2009のページ1−42)に従いRT反応を行なった。
リアルタイムPCRはAppliedBiosystems 7500 リアルタイムPCR Systemを用い、以下のように実施した。SYBR Green法を用い(THUNDERBIRD SYBR qPCR Mix,東洋紡社)、7500 リアルタイムPCR Systemの操作マニュアル(AppliedBiosystems)を用いて、Comparative CT(△△CT)法(n=3)により遺伝子発現比較を実施した。内部標準としてGAPDHを使用した。
エンドセリン−1:フォワードプライマーがTCCTCTGCTGGTTCCTGACT(配列番号1)の塩基配列と、リバースプライマーがCAGAAACTCCACCCCTGTGT(配列番号2)の塩基配列とのセット
GAPDH:フォワードプライマーがGAGTCAACGGATTTGGTCGT(配列番号3)の塩基配列と、リバースプライマーがTTGATTTTGGAGGGATCTCG(配列番号4)の塩基配列とのセット
結果を見ると、実施例は1.0%で作用させた場合、エンドセリン−1の遺伝子発現量を約60%抑制することがわかった。
Claims (5)
- ピロリドンカルボン酸またはその塩、L−アルギニン、L−アスパラギン酸、グリシン、L−アラニン、L−セリン、L−バリン、L−プロリン、L−スレオニン、L−イソロイシン、L−ヒスチジン、L−フェニルアラニンを有効成分とするエンドセリン−1阻害剤。
- ピロリドンカルボン酸またはその塩を20〜50重量部、L−アルギニンを10〜20重量部、L−アスパラギン酸を5〜15重量部、グリシンを2.0〜5.0重量部、L−アラニンを2.0〜5.0重量部、L−セリンを1.0〜3.0重量部、L−バリンを1.0〜2.0重量部、L−プロリンを0.4〜1.2重量部、L−スレオニンを0.4〜1.2重量部、L−イソロイシンを0.4〜1.2重量部、L−ヒスチジンを0.1〜0.5重量部、L−フェニルアラニンを0.1〜0.5重量部配合した請求項1のエンドセリン−1阻害剤。
- さらに乳酸ナトリウムを配合した請求項1乃至請求項2のエンドセリン−1阻害剤。
- ピロリドンカルボン酸またはその塩、L−アルギニン、L−アスパラギン酸、グリシン、L−アラニン、L−セリン、L−バリン、L−プロリン、L−スレオニン、L−イソロイシン、L−ヒスチジン、L−フェニルアラニンの合計量を10重量部としたときに、乳酸ナトリウムの配合量が1〜5である請求項3のエンドセリン−1阻害剤。
- 請求項1乃至請求項4のエンドセリン−1阻害剤を配合した美白用皮膚外用剤。
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Publication number | Priority date | Publication date | Assignee | Title |
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Non-Patent Citations (3)
Title |
---|
富田 靖: "遺伝子レベルからみた美白剤開発研究の展望", FRAGRANCE JOURNAL, JPN6017037695, January 2002 (2002-01-01), pages 21 - 25, ISSN: 0003653735 * |
新化粧品ハンドブック, JPN6017037693, 30 October 2006 (2006-10-30), pages 525 - 539, ISSN: 0003653734 * |
落合康宣: "抗酸化剤の美白メカニズム", FRAGRANCE JOURNAL, JPN6017037691, May 2005 (2005-05-01), pages 38 - 42, ISSN: 0003653733 * |
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