コレステロールを下げる天然製品で,FXRの対抗リガンドとしてコレステロールを下げる
Nancy L Urizar1, Amy B Liverman, D'Nette T Dodds
1Department of Molecular and Cellular Biology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX 77030, USA.
まとめ
グーグルツリー (guggul tree) のグーグルステロンは,ファルネソイドX受容体 (FXR) を阻害することによって,LDLコレステロールを低下させます. この発見は,天然の化合物によるコレステロール低下のメカニズムを明らかにしています.
科学分野:
- バイオケミストリー バイオケミストリー
- 薬理学 薬理学とは
- 自然製品 自然製品
背景:
- グーグルツリー (Commiphora mukul) の樹脂抽出物は,ヒトのLDLコレステロールを減らすことが知られている.
- ググルステロンは,コレステロールを低下させるこの効果に責任を負う活性植物ステロールとして識別されています.
- ファーネソイドX受容体 (FXR) は,胆酸によって活性化される核受容体であり,代謝調節に役割を果たします.
研究 の 目的:
- ググルステロンがコレステロールを下げる効果を発揮する分子機構を解明する.
- ググルステロンの活性を媒介するファルネソイドX受容体 (FXR) の役割を調査する.
主な方法:
- ガグルステロンがファルネソイドX受容体 (FXR) との相互作用を決定するためのインビトロアッセイ.
- 野生型およびFXR-nullのマウスを用いたインビボ研究では,高コレステロールの食事を与えられました.
- ググルステロン治療後の肝臓のコレステロール値の測定.
主要な成果:
- ググルステロンは,ファルネソイドX受容体 (FXR) の強力な抗体として作用する.
- グーグルステロンの治療は,コレステロールが高いダイエット中の野生型のマウスの肝臓のコレステロールを著しく低下させた.
- ググルステロンのコレステロール低下効果は,FXR-nullマウスでは廃止されました.
結論:
- ググルステロンのコレステロールを下げる活動は,ファルネソイドX受容体 (FXR) の活性化を阻害することによって媒介されます.
- この研究は,グルグルステロンの脂質低下効果の主なメカニズムとしてFXR抑制を提案しています.
- 天然製品は,FXRのような核ホルモン受容体の活動を調節し,治療的可能性を秘めています.
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