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来自Euphorbia peplus的迪特尔类植物具有细胞毒性和抗炎活性

Ying Li¹, Zhi-Pu Yu², Yu-Peng Li¹

¹Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong 264117, People's Republic of China.

Bioorganic chemistry

|February 17, 2024

概括

这项研究确定了32种来自Euphorbia peplus的二类植物,揭示了新的结构和抗炎性质. 化合物13通过抑制关键信号通路表现出显著的抗炎作用.

科学领域:

植物化学植物化学
自然产品化学化学
药理学药理学是指药理学的学科.

背景情况:

欧比亚种 (Euphorbia peplus) 是生物活性化合物的植物来源.
迪特尔类是一种多样化的自然产品类别,具有各种生物活动.
了解药用植物的化学成分和生物活性对于药物发现至关重要.

研究的目的:

对Euphorbia peplus.的乙醇提取物进行植物化学研究.
为了识别和表征新型的二类动物.
评估分离化合物的细胞毒性和抗炎活性.

主要方法:

对Euphorbia peplus乙醇提取物中等极分的植物化学分析.
使用光谱方法隔离和结构阐明diterpenoids.
对抗癌细胞系的细胞毒性活动的评估.
通过测量脂多糖 (LPS) 刺激的RAW264.7巨细胞中氧化 (NO) 产生的抗炎活性来评估抗炎活性.
分析包括NF-κB和MAPK在内的信号通路.

主要成果:

确定了32个属于五种结构类型的四面体.
报告了五种新化合物 (1-5) 和五种新衍生物 (7-11),对化合物6的立体化学进行了修订.
化合物1-5在泰格利亚类型的双类家族中表现出一种罕见的结构变异.
化合物21显示了中度的细胞毒性活性.
化合物4,8,12,13,16和19显示出对NO产生的显著抑制活性 (IC50值为2-5μM).
恩根类型的二类药物表现出最强的抗炎活性,以3-OH或5-OH的化为关键.
化合物13抑制了NF-κB和MAPK信号通路,证实了它的抗炎作用.

结论:

对Euphorbia peplus的植物化学研究产生了一系列多样化的二类植物,包括新的结构.
几种孤立的迪特尔类物质具有显著的抗炎性质,其中英类化合物特别有效.
化合物13,主要代谢物,通过调节NF-κB和MAPK信号通路,产生抗炎作用,突出其治疗潜力.

关键词:

它具有抗炎活性,具有抗炎活性.细胞毒性活动的细胞毒性.迪特尔佩诺类动物 (Diterpenoids) 是一种形类动物.尤福里亚人群的增加.这就是MAPKK的意思.在 NF-κBB 中.

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