JP2009091261A - 血小板凝集抑制剤 - Google Patents
血小板凝集抑制剤 Download PDFInfo
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- JP2009091261A JP2009091261A JP2007260672A JP2007260672A JP2009091261A JP 2009091261 A JP2009091261 A JP 2009091261A JP 2007260672 A JP2007260672 A JP 2007260672A JP 2007260672 A JP2007260672 A JP 2007260672A JP 2009091261 A JP2009091261 A JP 2009091261A
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- Prior art keywords
- platelet aggregation
- aggregation inhibitor
- carbon atoms
- active ingredient
- present
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Abstract
【解決手段】下記式(1)乃至(6)
で示される含酸素環状構造を有する化合物群から選ばれた少なくとも1つの化合物を有効成分として含有する血小板凝集抑制剤、および該化合物を有効成分とする血流改善剤、抗血栓剤。該血小板凝集抑制剤としては、特に、(R)−2−デセノ−δ−ラクトンが好ましい。
【選択図】 なし
Description
人の血液に10%濃度になるように3.8%クエン酸ナトリウム液を加え、この血液を1000rpmで10分間遠心分離し、上層部を採取して、これを多血小板血漿(PRP)とした。さらに、下層部を3000rpmで15分間遠心分離し、上層部から乏血小板血漿(PPP)を採取して、これを血小板凝集能測定時におけるコントロールとした。
・PRP+アラキドン酸のみを加えたときの最大凝集率をAとする。
・被験物質+PRP+アラキドン酸を加えたときの最大凝集率をBとする。
・凝集阻害率(%)をCとすると
C=100−B/A×100
(試験結果)
前記の試験方法において、被験物質の濃度が1mMとなる量を添加した条件下で血小板凝集阻害活性を測定した。その試験結果を、表1にアラキドン酸惹起における血小板凝集阻害率(%)で示す。また、表1中に比較例として、従来血小板凝集阻害活性が知られている市販のトウガラシチンキと、血流改善効果が知られている松樹皮抽出物の試験結果を収載した。
人の血液に10%濃度になるように3.8%クエン酸ナトリウム液を加え、この血液を1000rpmで10分間遠心分離し、上層部を採取して、これを多血小板血漿(PRP)とした。さらに、下層部を3000rpmで15分間遠心分離し、上層部から乏血小板血漿(PPP)を採取して、これを血小板凝集能測定時におけるコントロールとした。
・PRP+A23187のみを加えたときの最大凝集率をAとする。
・被験物質+PRP+A23187を加えたときの最大凝集率をBとする。
・凝集阻害率(%)をCとすると
C=100−B/A×100
(試験結果)
前記試験方法において、被験物質の濃度が1mMから開始して、順次、阻害活性が消失するまで試料を1/2希釈してと添加し、血小板凝集阻害活性を測定した。カルシウムイオノフォア(A23187)惹起時の血小板凝集阻害率(%)を表2に示す。
・錠剤配合例(配合割合は質量比である。)
──────────────────────
本発明の血小板凝集抑制剤 5.0
6%HPC乳糖 80.0
ステアリン酸マグネシウム 4.0
バレイショデンプン 6.0
──────────────────────
・軟膏剤配合例(配合割合は質量比である。)
─────────────────────────
白色ワセリン 20.0
ステアリルアルコール 22.0
プロピレングリコール 12.0
ラウリル硫酸ナトリウム 1.5
パラベン 0.2
本発明の血小板凝集抑制剤 5.0
精製水 39.3
─────────────────────────
・入浴剤配合例(配合割合は質量比である。)
――――――――――――――――――――――─
炭酸水素ナトリウム 50.0
硫酸ナトリウム 45.0
本発明の血小板凝集抑制剤 1.3
香料 0.7
色素 3.0
───────────────────────
以下に、本発明の血小板凝集抑制剤の食品への配合例について一例を示す。
・アイスクリーム配合例(配合割合は質量比である。)
────────────────────────
全脂練乳 10.0
生クリーム 9.4
無塩バター 2.0
脱脂粉乳 3.4
砂糖 12.0
安定剤 0.3
乳化剤 0.2
pH調整剤 0.1
カラメル色素 0.1
本発明の血小板凝集抑制剤 0.01
香料 0.01
水 49.0
────────────────────────
・クッキー生地配合例(配合割合は質量比である。)
────────────────────────
薄力粉 62.5
全粒粉 37.5
ショートニング 30.0
全卵 30.0
砂糖 20.0
水飴 1.0
脱脂粉乳 5.0
食塩 1.2
食用油脂 30.0
重炭酸ソーダ 1.0
重炭酸アンモニウム 1.0
本発明の血小板凝集抑制剤 0.1
香料 0.3
水 11.0
────────────────────────
・チョコレート配合例(配合割合は質量比である。)
─────────────────────────
カカオ液 12.0
カカオバター 24.0
ショ糖 33.0
フルクリームミルクパウダー 19.0
スキムミルクパウダー 11.4
レシチン 0.5
本発明の血小板凝集抑制剤 0.01
香料 0.1
─────────────────────────
・ノンオイルドレッシング配合例(配合割合は質量比である。)
─────────────────────────
濃口醤油 10.0
醸造酢 6.0
リンゴ酢 5.0
レモン果汁 4.0
液糖 7.0
食塩 2.0
調味料 7.0
香料 0.2
本発明の血小板凝集抑制剤 0.01
水 50.0
─────────────────────────
・飲料配合例(配合割合は質量比である。)
――――――――――――――――――――――───
果糖ぶどう糖液糖 60.0
アップル透明果汁 4.3
クエン酸 2.3
クエン酸三ナトリウム 0.8
アスコルビン酸 0.2
スクラロース 0.03
アセスルファムカリウム 0.02
香料 0.99
本発明の血小板凝集抑制剤 0.1
水 31.0
――――――――――――――――――――――───
・チューインガム配合例(配合割合は質量比である。)
――――――――――――――――――――――─
ガムベース 20.0
砂糖 60.0
ブドウ糖 10.0
水飴 8.0
グリセリン 5.0
香料 0.9
本発明の血小板凝集抑制剤 0.1
───────────────────────
Claims (5)
- 下記式(1)乃至(6)
- 2−デセノ−δ−ラクトン、3−プロピリデンフタリド、3−ブチリデンフタリド、2,3−ジヒドロベンゾフラン、3,4−ジヒドロクマリン、5,7−ジメトキシクマリン、4−メチル−7−メトキシクマリン、4−メチル−7−エトキシクマリン、8−メトキシソラレンおよび3,4−ジメチル−5−ペンチリデン−5H−フラン−2−オンからなる群から選ばれた少なくとも1つの化合物を有効成分として含有する血小板凝集抑制剤。
- 2−デセノ−δ−ラクトンが(R)−2−デセノ−δ−ラクトンであることを特徴とする請求項2に記載の血小板凝集抑制剤。
- 請求項1乃至請求項3に記載の血小板凝集抑制剤を有効成分とする血流改善剤。
- 請求項1乃至請求項3に記載の血小板凝集抑制剤を有効成分とする抗血栓剤。
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WO2013146539A1 (ja) * | 2012-03-27 | 2013-10-03 | 辻本化学工業株式会社 | PPARsアゴニスト活性亢進薬 |
CN103965150A (zh) * | 2014-05-28 | 2014-08-06 | 广州康臣药物研究有限公司 | 东莨菪内酯衍生物及其制备方法和应用 |
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