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基于对天然产品的查发现了一种新的强效FXR激活剂

Zongwen Yao¹, Lin Chen¹, Min Hu¹

¹College of Pharmaceutical Sciences, Southwest University, Chongqing, China.

Bioorganic chemistry

|November 23, 2023

概括

研究人员从Xylopia vielana中发现了具有FXR激活活性的新基. 化合物27显示出强大的FXR激活,改善小鼠胆固醇的状况,为新的药物开拓提供了潜力.

科学领域:

自然产品化学自然产品化学
药理学药理学是指药理学的学科.
药用化学医学化学

背景情况:

华氏体X受体 (FXR) 是胆酸平衡和代谢疾病的关键调节者.
自然产品是新型治疗剂的丰富来源,包括FXR调节器.

研究的目的:

从天然产品Xylopia vielana中发现和描述新的FXR激应剂.
在胆固醇病模型中研究已识别的FXR激活剂的治疗潜力.

主要方法:

使用HRESIMS,NMR,ECD和X射线晶体学对38个石的隔离和结构阐明.
高含量查FXR激进活性,分子对接和初步SAR分析.
试验室测试 (双化酶,西式涂抹) 和体内研究 (在小鼠中的ANIT诱导胆固醇酶模型) 用于目标验证和疗效评估.

主要成果:

鉴定了34种新型的类;13种表现出FXR激活活性.
化合物27显示出强大的FXR激活,对BSEP和SHP进行上调,对CYP7A1和NTCP进行下调.
化合物27有效地改善了小鼠的ANIT诱导胆固醇,减少了肝损伤和关键的生物化学标志物.

结论:

本研究提出了从天然产品中识别FXR激应剂的实用策略.
来自Xylopia vielana的Sesquiterpenoids,特别是化合物27,显示出作为治疗胆固醇性肝脏疾病的化合物的希望.

关键词:

外汇汇率对抗性活动的FXR.自然产品选对自然产品进行选.这种形形体是Sesquiterpenoids.结构阐明结构阐明目标验证的目标验证.X. 维拉纳维拉纳

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