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来自Euphorbia wallichii的Ent-atisane二基和它们的抗流感A病毒活性

Jie Zhang¹, Xiao-Jia Guo², Xiao-Juan Chen³

¹Guangdong Provincial Key Laboratory of Translational Cancer Research of Chinese Medicines, Joint International Research Laboratory of Translational Cancer Research of Chinese Medicines, International Institute for Translational Chinese Medicine, School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, 510006, PR China; Beijing Institute of Radiation Medicine, Beijing, 100850, PR China; Guangdong-Hongkong-Macau Joint Lab on Chinese Medicine and Immune Disease Research, Guangzhou, 510006, PR China.

|February 4, 2024

概括

研究人员从Euphorbia wallichii根中分离了29种ent-atisane diterpenoids,其中包括14种新型化合物. 一些化合物显示出显著的抗流感A病毒活性,标志着第一个关于具有抗H1N1效应的ent-atisanes的报告.

科学领域:

自然产品化学自然产品化学
病毒学病毒学
有机化学有机化学

背景情况:

欧白 (Euphorbia wallichii) 是植物中各种化学化合物的来源.
A型流感病毒对全球健康构成重大威胁.
乙太二烯酸是一种具有潜在生物活性的自然产品.

研究的目的:

为了隔离和描述来自Euphorbia wallichii根的化合物.
评估隔离化合物的抗病毒活性对抗流感A病毒.
建立新的方法来确定工艺品中的立体化学.

主要方法:

使用色谱技术分离化合物.
通过综合光谱方法 (NMR,MS) 和计算的电子循环二元化来阐明结构.
使用X射线晶体分析确定绝对配置.
在体外抗病毒检测对抗流感A病毒 (A/波多黎各/8/1934).

主要成果:

他们分离了29种Ent-atisane二类化合物,包括14种名为euphorwanoids A-N.N.的新型化合物.
化合物18,20和24对流感A病毒具有显著的抗病毒活性,EC50值分别为8.56,1.22和4.97μM.
这项研究报告了第一个表现出抗H1N1活性的ent-atisane二烯的实例.
经验性NMR规则是为了区分C-13和C-16配置而开发的.

结论:

欧白 (Euphorbia wallichii) 是结构多样化的丰富来源.
某些Ent-atisane二特类物质在体外对A型流感病毒具有强烈的抗病毒活性.
这些发现为开发基于天然产品的抗病毒疗法开辟了新的途径,并为特特类的表征提供了新的分析工具.

关键词:

抗H1N1活动活动.经验性的NMR规则它们是Ent-atisane二次化物.尤福里亚或许会发生.欧豆科 (Euphorbiaceae) 是一个植物.

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