JP2022130618A - Foxo1活性阻害用組成物 - Google Patents
Foxo1活性阻害用組成物 Download PDFInfo
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- JP2022130618A JP2022130618A JP2022105383A JP2022105383A JP2022130618A JP 2022130618 A JP2022130618 A JP 2022130618A JP 2022105383 A JP2022105383 A JP 2022105383A JP 2022105383 A JP2022105383 A JP 2022105383A JP 2022130618 A JP2022130618 A JP 2022130618A
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Abstract
Description
(1)カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物を含有する、FOXO1活性阻害用組成物。
(2)カルコン類が、4-ヒドロキシカルコン、trans-カルコン、及び2,3-ジメトキシ-2'-ヒドロキシカルコンからなる群より選択される少なくとも一つの化合物である、(1)に記載の組成物。
(3)トリテルペン類が、コロソリン酸である、(1)又は(2)に記載の組成物。
(4)フラボン類が、6,7-ジヒドロキシフラボン、6-メチルフラボン、5-メトキシフラボン、7,8-ジヒドロキシフラボン、クリシン、及びサポナリンからなる群より選択される少なくとも一つの化合物である、(1)~(3)のいずれかに記載の組成物。
(5)モノテルペノイド類が、(±)イソメントンである、(1)~(4)のいずれかに記載の組成物。
(6)リグナン類が、エンテロジオール及び/又はトラケロゲニンである、(1)~(5)のいずれかに記載の組成物。
(7)クマリン類が、3,4-ジヒドロクマリンである、(1)~(6)のいずれかに記載の組成物。
(8)フィトケミカル類が、アマロゲンチンである、(1)~(7)のいずれかに記載の組成物。
(9)筋委縮抑制用、筋肉合成促進用、又は骨密度低下抑制用である、(1)~(8)のいずれかに記載の組成物。
(10)FOXO1活性の阻害により発揮される機能の表示を付した、(1)~(9)のいずれかに記載の組成物。
(11)機能の表示が、「筋肉を維持する」、「筋委縮を抑制する」、「筋肉の減少を防ぐ」、「筋肉の減少を抑える」、「筋肉の衰えを防ぐ」、「筋肉の衰えを抑える」、「筋肉をつける」、「筋肉を増やす」、「筋肉をつくる」、「筋肉をサポートする」、「骨密度を維持する」、「骨密度の低下を防ぐ」、「骨密度の低下を抑える」、「骨をサポートする」、「丈夫な骨を維持する」、「骨の健康を維持する」、及び「骨の健康に役立つ」からなる群より選択されるものである、(10)に記載の組成物。
(12)FOXO1活性を阻害するための、カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物の使用。
(13)カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物を使用する、FOXO1活性を阻害する方法。
本発明の一態様は、所定の化合物を含有する組成物である。本発明の組成物は、当該所定の化合物を有効成分とするものである。
本発明の組成物は、上記の化合物を有効成分として用いることによってFOXO1活性を阻害することができる。そのため、本発明の組成物は、FOXO1活性阻害用組成物として用いることができる。本明細書において、「FOXO1」とは、フォークヘッド型転写因子(Forkhead box protein O1)をいう。筋萎縮を引き起こす様々な条件として、例えば、絶食、徐神経、グルココルチコイド投与、小胞体ストレスなどの刺激により、FOXO1の発現が上昇し、細胞核内に脱リン酸化状態で存在するFOXO1により、筋萎縮関連の遺伝子発現(例えばユビキチン-プロテアソーム系によるタンパク分解、オートファジーの亢進、さらにタンパク合成の抑制等)が増加する。
本発明の組成物における上記の化合物の含有量は、その投与形態及び投与方法等を考慮し、本発明の所望の効果が得られるような量であればよく、特に限定されるものではない。例えば、上記の化合物の含有量は、本発明の組成物の全重量に対して0.1重量%以上、好ましくは0.2、0.3、0.4、0.5、0.6、0.7、0.8、0.9、1、1.5、2、5、又は10重量%以上であり、90重量%以下、好ましくは80、70、60、50、40、30、20、又は15重量%以下である。上述した通り、本発明の組成物において、上記の化合物は一種のみが含まれていてもよく、或いは二種以上が含まれていてもよい。二種以上の化合物が含まれる場合、前記の含有量は、各種化合物の含有量の合計値で規定される。なお、本明細書において用いる「重量%」は、特に断りがない限り重量/重量(w/w)を意味する。
本発明の一態様は、FOXO1活性を阻害するための、カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物の使用である。
本発明の一態様は、カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物を使用する、FOXO1活性を阻害する方法である。また、当該方法に関する別の態様は、FOXO1活性の阻害を必要とする対象に、上記の化合物を有効成分として治療有効量を投与することを含む、FOXO1活性を阻害する方法である。
Claims (13)
- カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物を含有する、FOXO1活性阻害用組成物。
- カルコン類が、4-ヒドロキシカルコン、trans-カルコン、及び2,3-ジメトキシ-2'-ヒドロキシカルコンからなる群より選択される少なくとも一つの化合物である、請求項1に記載の組成物。
- トリテルペン類が、コロソリン酸である、請求項1又は2に記載の組成物。
- フラボン類が、6,7-ジヒドロキシフラボン、6-メチルフラボン、5-メトキシフラボン、7,8-ジヒドロキシフラボン、クリシン、及びサポナリンからなる群より選択される少なくとも一つの化合物である、請求項1~3のいずれか1項に記載の組成物。
- モノテルペノイド類が、(±)イソメントンである、請求項1~4のいずれか1項に記載の組成物。
- リグナン類が、エンテロジオール及び/又はトラケロゲニンである、請求項1~5のいずれか1項に記載の組成物。
- クマリン類が、3,4-ジヒドロクマリンである、請求項1~6のいずれか1項に記載の組成物。
- フィトケミカル類が、アマロゲンチンである、請求項1~7のいずれか1項に記載の組成物。
- 筋委縮抑制用、筋肉合成促進用、又は骨密度低下抑制用である、請求項1~8のいずれか1項に記載の組成物。
- FOXO1活性の阻害により発揮される機能の表示を付した、請求項1~9のいずれか1項に記載の組成物。
- 機能の表示が、「筋肉を維持する」、「筋委縮を抑制する」、「筋肉の減少を防ぐ」、「筋肉の減少を抑える」、「筋肉の衰えを防ぐ」、「筋肉の衰えを抑える」、「筋肉をつける」、「筋肉を増やす」、「筋肉をつくる」、「筋肉をサポートする」、「骨密度を維持する」、「骨密度の低下を防ぐ」、「骨密度の低下を抑える」、「骨をサポートする」、「丈夫な骨を維持する」、「骨の健康を維持する」、及び「骨の健康に役立つ」からなる群より選択されるものである、請求項10に記載の組成物。
- FOXO1活性を阻害するための、カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物の使用。
- カルコン類、トリテルペン類、フラボン類、モノテルペノイド類、リグナン類、クマリン類、及びフィトケミカル類からなる群より選択される少なくとも一つの化合物を使用する、FOXO1活性を阻害する方法。
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