JP2015044747A - Pde3阻害剤 - Google Patents
Pde3阻害剤 Download PDFInfo
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- JP2015044747A JP2015044747A JP2013175259A JP2013175259A JP2015044747A JP 2015044747 A JP2015044747 A JP 2015044747A JP 2013175259 A JP2013175259 A JP 2013175259A JP 2013175259 A JP2013175259 A JP 2013175259A JP 2015044747 A JP2015044747 A JP 2015044747A
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- carotene
- marjoram
- parsley
- licorice
- mass
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Abstract
【解決手段】(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする。
【選択図】なし
Description
(1)(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とするPDE3阻害剤。
(2)(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする循環機能改善剤。
(3)(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする気管支機能改善剤。
(4)(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する非治療的PDE3阻害方法。
(5)(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する非治療的循環機能改善方法。
(6)(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する非治療的気管支機能改善方法。
また、当該PDE3には、3A、3Bの2種のタイプがあることが知られているが、本願発明においてはいずれも包含される。
本発明において、マジョラムは、シソ科ハナハッカ属のOriganum majoranaをいう。
パセリは、セリ科オランダゼリ属のCarum Petroselinum、Petroselium crispumをいう。
カンゾウは、マメ科カンゾウ属のウラルカンゾウ(Glycyrrhiza uralensis FISCHER)、チョウカカンゾウ(Glycyrrhiza inflata BATALIN)又はヨウカンゾウ(Glycyrrhiza glabra LINNE)をいう。
本発明において、β−カロテンは、種々の植物から抽出、精製したものが用いることができ、例えばオオヒゲマワリ科デュナリエラ(Dunaliella bardawil, Dunaliella salina)等から得られたものが挙げられる。
上記抽出物の酸化を防止するため、煮沸脱気や窒素ガス等の不活性ガスを通気して溶存酸素を除去しつつ、いわゆる非酸化的雰囲気下で抽出する手段を併用してもよい。
マジョラム、パセリの場合には、10〜30℃で3〜10日間抽出するのが好ましい。カンゾウの場合は、10〜30℃で1〜24時間抽出するのが好ましい。
具体的には、β−カロテンは、上記植物1質量部に対して、ヘキサン5〜15質量部の溶剤を用い、4〜85℃の温度(好ましくは、15〜85℃)で、1時間〜30日間(好ましくは3時間〜25日間)抽出することで得ることができる。
ここで、「非治療的」とは、医療行為を含まない、すなわち医師又は医師の指示を受けた者によりヒトを手術、治療又は診断する方法を含まない概念である。
錠剤や加工食品等の固形食品の形態では、上記(A)マジョラム、パセリ、カンゾウ又はそれらの抽出物(乾燥物換算)、(B)β-カロテンの含有量は、好ましくは0.005質量%以上、より好ましくは0.05質量%以上、更に好ましくは0.1質量%以上、好ましくは50質量%以下、より好ましくは5質量%以下、更に好ましくは1質量%以下である。また、好ましくは0.005〜50質量%、より好ましくは0.05〜5質量%、更に好ましくは0.1〜1質量%である。
循環機能低下に起因する冷え症、むくみ、肩こり、又はせきやたんなどに悩み、これらを改善したいと欲する対象者等に適用することができる。
<1>(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とするPDE3阻害剤。
<2>(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする循環機能改善剤。
<3>(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする気管支機能改善剤。
<4>PDE3阻害剤を製造するための、(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上の使用。
<5>循環機能改善剤を製造するための、(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上の使用。
<6>気管支機能改善剤を製造するための、(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上の使用。
<7>PDE3阻害に使用するための、(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上。
<8>循環機能改善に使用するための、(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上。
<9>気管支機能改善に使用するための、(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上。
<10>非治療的に使用するための、<7>〜<9>に記載の(A)植物又はそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上。
<11>(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取するPDE3阻害方法。
<12>(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する循環機能改善方法。
<13>(A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する気管支機能改善方法。
<14>非治療的方法である、<11>〜<13>に記載の方法。
<15><2>、<5>、<8>、<10>、<12>、<14>に記載の循環機能改善は、好ましくは心不全改善、慢性動脈閉塞症改善及び血栓症改善から選ばれる1種以上である。
<16><3>、<6>、<9>、<10>、<13>、<14>に記載の気管支機能改善は、好ましくは気管支喘息改善である。
<17><1>〜<16>のいずれかにおいて、上記抽出物は、好ましくはエタノール水溶液抽出物である。
丸善製薬より入手した油溶性カンゾウエキスPT(40)0.1gに、99.5容量%エタノール−水混合溶液10mLを加えて、抽出乾固物1%のカンゾウ抽出液を得た。
乾燥したマジョラムの全草(栃本天海堂)10gに、10倍量の50容量%エタノール−水混合溶液0.1Lを加え、約20℃、7日間、不溶物をろ別し、得られたろ液をマグネチックスターラーで撹拌しながらフラスコで抽出して、固形分濃度2.2%のマジョラム抽出液を得た。
乾燥したパセリの葉(新和物産)100gに、10倍量の50容量%エタノール−水混合溶液1Lを加え、約20℃、7日間、マグネチックスターラーで撹拌しながらフラスコで抽出し、得られた抽出液の不溶物をろ別後、固形分濃度は3.0%のパセリ抽出液を得た。
協和発酵より入手したバイオカロテン30MCT0.1gを、99.5%エタノール10mLに溶解して、固形濃度1%のβ−カロテン液を得た。
PDE-Glo Phosphodiesterase Assay (Promega社)を用いて、ヒトリコンビナントホスホジエステラーゼ3Bが0.8μg/mLになるようPDE−Glo反応溶液で調製した溶液10μL、及び上記実施例の溶液2.5μLを混合した後、2μM濃度になるように調製したcAMP溶液を添加することで酵素反応させた。得られた反応液を、37℃で10分間反応させ、その後PDE−Glo Termination Buffer 12.5μLを添加して反応を停止させた。そこへPDE−Glo検出溶液12.5μLを添加し、10分後にKinase-Glo溶液50μLを添加し、化学発光量を測定した。測定した発光量から、下記式でPDE3活性を求め、その結果を表1に示す。
PDE3活性(%)=(実施例1〜4、比較例2のいずれかの発光量/比較例1の発光量)×100
なお、比較例1はPDE−Glo反応溶液の調製液に上記実施例の溶液を未添加のもの、比較例2は前記調製液に上記実施例の溶液の代わりにカフェインを添加したものとした。
なお、カフェインは、既知のPDE3阻害作用を有する素材である。
Claims (8)
- (A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とするPDE3阻害剤。
- (A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする循環機能改善剤。
- 心不全改善剤、慢性動脈閉塞症改善剤及び血栓症改善剤から選ばれる1種以上である請求項2に記載の循環機能改善剤。
- (A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を有効成分とする気管支機能改善剤。
- 気管支喘息改善剤である請求項4に記載の気管支機能改善剤。
- (A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する非治療的PDE3阻害方法。
- (A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する非治療的循環機能改善方法。
- (A)マジョラム、パセリ、カンゾウ及びそれらの抽出物、(B)β-カロテンからなる群から選ばれる1種以上を、ヒト若しくは動物に投与又は摂取する非治療的気管支機能改善方法。
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