来自Acanthopanacis皮质的迪特尔酸和它们的抗炎活性研究研究
Hao-Dong Yang1, Bao-Long Hou1, Yuan-Gui Yang1
1Co-construction Collaborative Innovation Center for Chinese Medicine Resources Industrialization by Shaanxi & Education Ministry, State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), Shaanxi University of Chinese Medicine, Xianyang 712083, PR China.
Fitoterapia
|May 18, 2024
概括
阿坎托帕纳西斯皮层产生了19种二甲,包括6种新的化合物. 化合物15表现出显著的选择性COX-2抑制,为新型抗炎药物设计提供了潜力.
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.
背景情况:
- 阿坎托帕纳西斯皮层 (Acanthopanacis Cortex,A.-C) 在治疗风湿症方面有着超过1000年的记录历史.
- 迪特尔类是具有多种生物活动的重要自然产品类别.
研究的目的:
- 从Acanthopanacis Cortex中分离和表征diterpenoids. 为了分离和表征Acanthopanacis Cortex中的diterpenoids.
- 评估分离化合物的抗炎潜力,特别是它们对中性粒细胞弹性酶,COX-1和COX-2的抑制作用.
主要方法:
- 从AC中分离了19种二甲,包括6种新型化合物.
- 使用NMR光谱和电子循环二元化 (ECD) 分析进行结构阐明.
- 单晶X射线衍射用于确定所选化合物的结构确认.
- 在体外抗炎试验测量中性粒细胞弹性酶,COX-1和COX-2的抑制.
主要成果:
- 在13种已知的化合物之外,发现了6种新的二甲 (1-6),以及13种已知的化合物.
- 第一次从AC报告了7,9-11,13和17的化合物.
- 化合物15表现出强烈而选择性的循环氧化酶-2 (COX-2) 抑制,IC50为0.73μM,同时显示出最小的COX-1抑制.
结论:
- 这项研究成功地从Acanthopanacis Cortex中分离和表征了新型的二类物质.
- 化合物15显示出作为选择性COX-2抑制剂的显著潜力,需要进一步研究抗炎治疗开发.
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