JP2020128355A - Ace阻害活性を有する組成物 - Google Patents
Ace阻害活性を有する組成物 Download PDFInfo
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- JP2020128355A JP2020128355A JP2019021538A JP2019021538A JP2020128355A JP 2020128355 A JP2020128355 A JP 2020128355A JP 2019021538 A JP2019021538 A JP 2019021538A JP 2019021538 A JP2019021538 A JP 2019021538A JP 2020128355 A JP2020128355 A JP 2020128355A
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Abstract
Description
すなわち、本発明は、以下の態様を含む。
[1]マメ科カンゾウ属に属する植物の抽出物を含有することを特徴とする、アンギオテンシン変換酵素(ACE)阻害活性作用を有する組成物。
[2]マメ科カンゾウ属に属する植物の抽出物が、水、有機溶媒、またはこれらの混合物で抽出された抽出物である、[1]に記載の組成物。
[3]有機溶媒が、メタノール、エタノール、1−プロパノール、2−プロパノール、アセトン、1−ブタノール、2−ブタノール、2−メチル−2−プロパノール、プロピレングリコール、グリセリン、酢酸メチル、酢酸エチル、ヘキサン、ジエチルエーテル、2−ブタノン、シクロヘキサン、ジクロロメタン、食用油脂、プロパン、ブタン、1,1,1,2−テトラフルオロエタンおよび1,1,2−トリクロロエテンからなる群から選択される少なくとも1つである、[1]または[2]に記載の組成物。
[4]マメ科カンゾウ属に属する植物の抽出物が、根および/またはストロンからの抽出物である、[1]〜[3]いずれか記載の組成物。
[5]マメ科カンゾウ属に属する植物の抽出物の濃度が、0.10mg/mL以上である、[1]〜[4]いずれか記載の組成物。
[6]マメ科カンゾウ属に属する植物が、ウラルカンゾウ種である、[1]〜[5]いずれか記載の組成物。
[7][1]〜[6]いずれか記載の組成物を有効成分とする、アンギオテンシン変換酵素(ACE)に関連する疾患の予防あるいは軽減のための食品または医薬品。
有機溶媒としては、例えば、メタノール、エタノール、1−プロパノール、2−プロパノール、アセトン、1−ブタノール、2−ブタノール、2−メチル−2−プロパノール、プロピレングリコール、グリセリン、酢酸メチル、酢酸エチル、ヘキサン、ジエチルエーテル、2−ブタノン、シクロヘキサン、ジクロロメタン、食用油脂、プロパン、ブタン、1,1,1,2−テトラフルオロエタンおよび1,1,2−トリクロロエテンが挙げられる。
好ましくは、水、エタノールまたはこれらの混合物が挙げられる。また、水とエタノールの混合物を使用する場合、該混合物中のエタノール濃度は、例えば0.1〜99.5v/v%、好ましくは5〜80v/v%、より好ましくは10〜70v/v%である。
抽出条件は、十分に抽出される条件であれば特に限定されないが、通常、抽出温度が低温であればより長時間の抽出を行い、抽出溶媒が高温であればより短時間の抽出を行う。抽出温度は、0〜100℃の範囲で適宜設定され、好ましくは室温(約25℃)から抽出溶媒の沸点以下の範囲である。抽出時間は、10分〜24時間の範囲で設定され、好ましくは30分〜5時間の範囲である。抽出溶媒として水を用いる場合、抽出条件は、例えば約20〜95℃で約30分〜3時間である。抽出溶媒としてエタノールまたは水とエタノールとの混合溶媒を用いる場合、抽出条件は、例えば約20〜80℃で約30分〜3時間である。
抽出回数は単回でもよく、収率を上げるために複数回であってもよい。
また、本発明の組成物が固体組成物である場合、固体組成物中の配合割合(抽出物の乾燥重量/組成物の乾燥重量)として、その下限は、例えば0.01重量%以上、好ましくは0.1重量%以上であり、その上限は、例えば99重量%以下、好ましくは50重量%以下である。
担体または添加剤としては、例えば賦形剤、崩壊剤、結合剤、滑沢剤、着色剤、pH調整剤、界面活性剤、安定化剤、酸味料、香料などが挙げられる。これら添加剤は、製剤技術分野において慣用の量が用いられる。
崩壊剤としては、例えば、カルメロース、カルメロースカルシウム、カルボキシメチルスターチナトリウム、カルボキシメチルセルロース、カルボキシメチルセルロースカルシウム、カルボキシメチルスターチナトリウム、クロスカルメロースナトリウム、クロスポビドン、低置換度ヒドロキシプロピルセルロース(L-HPC)、ヒドロキシプロピルスターチなどが用いられ、好ましくは、クロスカルメロースナトリウム、L-HPCである。
結合剤としては、例えば、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ポリビニルピロリドン、コポリビドン、アラビアゴム末、メチルセルロース、低置換度ヒドロキシプロピルセルロース、ヒプロメロース、カルメロースナトリウム、デキストリン、部分アルファー化デンプン、プルラン、アラビアゴム、カンテン、ゼラチン、トラガント、アルギン酸ナトリウムなどが用いられ、好ましくは、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースである。
流動化剤としては、例えば、軽質無水ケイ酸、含水二酸化ケイ素、ケイ酸カルシウム、ケイ酸マグネシウム、メタケイ酸アルミン酸マグネシウム、タルクなどが用いられ、好ましくは、軽質無水ケイ酸、メタケイ酸アルミン酸マグネシウムである。
滑沢剤としては、例えば、ステアリン酸、ステアリン酸マグネシウム、ステアリン酸カルシウム、タルク、ショ糖脂肪酸エステルなどが挙げられる。
着色剤としては、例えば、黄色三二酸化鉄、三二酸化鉄、食用青色1号、食用青色2号、食用黄色4号、食用黄色5号、食用緑色3号、食用赤色2号、食用赤色3号、食用赤色102号、食用赤色104号、食用赤色105号、食用赤色106号、食用レーキ色素、リボフラビン、リボフラビンリン酸エステルナトリウムなどが挙げられる。
pH調整剤としては、例えば、クエン酸、リン酸、炭酸、酒石酸、フマル酸、酢酸、アミノ酸およびそれらの塩類などが挙げられる。
界面活性剤として、ラウリル硫酸ナトリウム、ポリソルベート80、ポリオキシエチレン(160)ポリオキシプロピレン(30)グリコールなどが挙げられる。
安定化剤としては、例えばトコフェロール、エデト酸四ナトリウム、ニコチン酸アミド、シクロデキストリン類などが挙げられる。
酸味料としては、例えば、アスコルビン酸、クエン酸、酒石酸、リンゴ酸などが挙げられる。
香料としては、例えば、L-メントール、ハッカ油、レモン油、バニリンなどが挙げられる。
上記した担体または添加剤は、2種以上を適宜、混合して用いてもよい。
都甘草の根およびストロン3kgに水約30Lを加え、90℃で約2時間抽出した後、メッシュろ過し、23.2Lの抽出液を得た。さらにこの抽出液を約60℃で減圧濃縮し、2544gの濃縮液を得た。この濃縮液2511gを噴霧乾燥し、乾燥抽出物608gを得た。
上記乾燥抽出物約1.0gを50%エタノール溶液20mlで抽出後、0.1mol/l HEPES緩衝液(pH8.3)にて適宜希釈して、0.1mg/mL(実施例1)、0.125mg/mL(実施例2)、0.15mg/mL(実施例3)、0.2mg/mL(実施例4)および0.225mg/mL(実施例5)の試料濃度を有する都甘草の根およびストロンからの水製エキス含有組成物を得た。
都甘草の根およびストロン3kgに30%エタノール約30Lを加え、60℃で約2時間抽出した後、メッシュろ過し、25.2Lの抽出液を得た。さらにこの抽出液を約60℃で減圧濃縮し、2849gの濃縮液を得た。この濃縮液2802gを噴霧乾燥し、乾燥抽出物636gを得た。
上記乾燥抽出物約1.0gを50%エタノール溶液20mlで抽出後、0.1mol/l HEPES緩衝液(pH8.3)にて適宜希釈して、0.1mg/mL(実施例6)、0.125mg/mL(実施例7)、0.15mg/mL(実施例8)、0.175mg/mL(実施例9)および0.2mg/mL(実施例10)の試料濃度を有する都甘草の根およびストロンからのエタノールエキス含有組成物を得た。
1.試験概要
アンギオテンシン変換酵素(ACE)活性試験はNakno etal. Biosci Biotechnol. Biochem., 70, 1118−1126(2006)に記載の方法に基づき、基質(His−His−Leu)からACEにより分解されるジペプチドをオルトフタルアルデヒド(以下「OPA」と略す。)により蛍光化した後、反応物の蛍光強度を測定することで実施した。ACE活性阻害は試験溶液を加えない未処置区の活性を100%とした場合の相対ACE活性をもとに評価した。IC50値は試料濃度(mg/ml)と阻害率(%)のグラフから算出した。
下記検体1)および2)の試験溶液として、上記実施例で得られた組成物を使用した。また、ポジティブコントロール(検体3))として、サーデンペプチド(商品名:サーデンペプチドN100、製造者:仙味エキス株式会社)を使用した。
1)都甘草の根およびストロンからの水製エキス(実施例1〜5)
2)都甘草の根およびストロンからのエタノールエキス(実施例6〜10)
3)サーデンペプチド(ポジティブコントロール)
0.1mol/l HEPES緩衝液(pH8.3)(未処置区)または各試験溶液を96穴マイクロプレートに25μl加え、20mU/ml ACE溶液を25μl加えて37℃で5分間インキュベートした。8mmol/l His−His−Leu溶液を25μl加え、37℃で30分間反応した。その後、0.1mol/l 水酸化ナトリウム溶液を25μl加えて反応を停止し、1%OPA溶液を25μl加え、室温で20分間放置した。さらに、0.1mol/l 塩酸を25μl入れて室温で10分間放置し、マイクロプレートリーダーで蛍光強度を測定した。なお、ブランクは20mU/ml ACE溶液の代わりにPBSを用いて同様に試験した。
<マイクロプレートリーダー操作条件>
機種:SpectraMax M2e
測定条件:蛍光、endpointモード、ボトムリード
励起波長:355nm
蛍光波長:460nm
Claims (7)
- マメ科カンゾウ属に属する植物の抽出物を含有することを特徴とする、アンギオテンシン変換酵素(ACE)阻害活性作用を有する組成物。
- マメ科カンゾウ属に属する植物の抽出物が、水、有機溶媒、またはこれらの混合物で抽出された抽出物である、請求項1に記載の組成物。
- 有機溶媒が、メタノール、エタノール、1−プロパノール、2−プロパノール、アセトン、1−ブタノール、2−ブタノール、2−メチル−2−プロパノール、プロピレングリコール、グリセリン、酢酸メチル、酢酸エチル、ヘキサン、ジエチルエーテル、2−ブタノン、シクロヘキサン、ジクロロメタン、食用油脂、プロパン、ブタン、1,1,1,2−テトラフルオロエタンおよび1,1,2−トリクロロエテンからなる群から選択される少なくとも1つである、請求項1または2に記載の組成物。
- マメ科カンゾウ属に属する植物の抽出物が、根および/またはストロンからの抽出物である、請求項1〜3いずれか記載の組成物。
- マメ科カンゾウ属に属する植物の抽出物の濃度が、0.10mg/mL以上である、請求項1〜4いずれか記載の組成物。
- マメ科カンゾウ属に属する植物が、ウラルカンゾウ種である、請求項1〜5いずれか記載の組成物。
- 請求項1〜6いずれか記載の組成物を有効成分とする、アンギオテンシン変換酵素(ACE)に関連する疾患の予防あるいは軽減のための食品または医薬品。
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JP2002114695A (ja) * | 2000-09-21 | 2002-04-16 | Ready Made 37 (1999) Ltd | 薬物として使用するための甘草抽出物 |
WO2002047699A1 (fr) * | 2000-12-12 | 2002-06-20 | Kaneka Corporation | Compositions de prévention ou d'amélioration de syndromes multifactoriels |
KR20050090972A (ko) * | 2005-08-25 | 2005-09-14 | 순 택 정 | 생약재를 이용한 침출주 제조방법 |
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