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一个新类强大的肝损伤保护性化合物:结构阐明,总合成和生物活性研究

Kailong Ji¹, Wei Liu¹, Weihang Yin¹

¹State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

Acta pharmaceutica Sinica. B

|September 1, 2023

概括

来自Phyllanthus franchetianus的新型花素AD显示出强大的肝损伤保护作用. 化合物4是一种有前途的治疗,在临床前研究中表现出显著的抗炎和肝保护作用.

科学领域:

自然产品化学自然产品化学
药用化学医学化学
药理学药理学是指药理学的学科.

背景情况:

一种中国药用植物Phyllanthus franchetianus产生了新的化合物.
一个独特的五环框架定义了基A-D (1-4).
化合物2 - 4被分离为racemic混合物,并分离成反体.

研究的目的:

从P.franchetianus中分离和描述新的化合物.
研究生物合成途径并合成这些化合物.
评估分离的化合物的抗炎和肝脏保护作用.

主要方法:

使用光谱学方法分离和阐明基A-D的结构.
状高性能液体染色学 (HPLC) 用于反体分离.
生物启发的化合物的总合成 2-4.
在体外测试抗炎活性 (IL-1β抑制).
在体内研究以评估小鼠肝损伤保护.

主要成果:

菲切丁A-D (1-4) 被分离和表征,具有新的五环结构.
提出了一种涉及分子内弗里德尔-克拉夫特反应的生物合成途径.
实现了 2-4 种化合物的有效总合成.
化合物通过抑制IL-1β.表现出体外抗炎活性.
化合物4在小鼠中表现出强大的肝损伤保护,剂量为3mg/kg.

结论:

菲切丁A-D代表了一类新的生物活性化合物.
合成策略提供了对这些复杂分子的访问.
化合物4是开发急性肝损伤疗法的有希望的头.

关键词:

这是一种抗炎症药物.肝损伤保护肝损伤保护肉类的质物质.弗兰切蒂安纳斯 (Phyllanthus franchetianus) 是一个葡萄树.结构阐明结构阐明总的合成总的合成.

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