一种降低胆固醇的天然产品,作为FXR的对手连接体
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.
Science (New York, N.Y.)
|May 4, 2002
概括
来自guggul树的guggulsterone通过阻止farnesoid X受体 (FXR) 来降低LDL胆固醇. 这一发现揭示了通过天然化合物降低胆固醇的机制.
科学领域:
- 生物化学 生物化学
- 药理学 药理学是指药理学的学科.
- 自然产品 自然产品
背景情况:
- 众所周知,古古尔树 (Commiphora mukul) 树脂提取物可以降低人类的LDL胆固醇.
- 古古斯特被认为是负责这种降胆固醇效应的活性植物.
- 华氏体X受体 (FXR) 是由胆酸激活的核受体,在代谢调节中起作用.
研究的目的:
- 为了阐明guggulsterone发挥降胆固醇作用的分子机制.
- 为了研究Farnesoid X受体 (FXR) 在调解guggulsterone活动中的作用.
主要方法:
- 在体外测试以确定guggulsterone与Farnesoid X受体 (FXR) 的相互作用.
- 在体内研究中,使用野生型和FXR-null小鼠食高胆固醇饮食.
- 在guggulsterone治疗后测量肝脏胆固醇水平.
主要成果:
- 古古尔斯特作为Farnesoid X受体 (FXR) 的强有力的对手.
- 在高胆固醇饮食中的野生类型小鼠中,古古斯特治疗显著降低了肝脏胆固醇.
- 在FXR-null小鼠中,guggulsterone的降胆固醇作用被废除了.
结论:
- 古古尔斯特的降胆固醇活性是通过抑制法尔内索伊德X受体 (FXR) 激活的介导.
- 这项研究提出FXR抑制是guggulsterone降脂效应的主要机制.
- 自然产品可能调节核激素受体的活性,如FXR,提供治疗潜力.
相关概念视频
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