发现了来自Andrographis paniculata的ent-labdane衍生物及其抗炎活性
Yang Yu1, Yang Wang2, Lan Ding2
1School of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230012, China; Institute of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei, 230012, China; Key Laboratory for Functional Substances of Chinese Medicine and Natural Medicine State, Hefei, 230012, China.
研究人员发现了来自Andrographis paniculata的新的抗炎化合物. 与德克萨梅他和安德罗格拉福利德相比,安德罗帕尼利德D显示出更强的抗炎作用,表明其在治疗炎症方面的潜力.
科学领域:
- 植物化学 植物化学
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
背景情况:
- 安德罗格拉菲斯 (Andrographis paniculata) 是东南亚和中国传统医学 (TCM) 的重要药用植物.
- 它以其抗炎性质而闻名,andrographolide 是一个关键的活性化合物.
- 目前正在进行研究,以从这种植物中发现具有增强抗炎活性的新型化合物.
研究的目的:
- 从Andrographis paniculata中分离和表征不同的二甲烯乳.
- 评估这些分离化合物的抗炎活性.
- 确定具有优越抗炎潜力的新型化合物并阐明它们的机制.
主要方法:
- 隔离了21种ent-labdanes,其中包括6种新化合物 (andropanilides D-I).
- 使用全面的NMR,HRESIMS和量子化学计算来阐明结构.
- 通过Griess方法评估抗炎活性,并使用LPS诱导的RAW264.7巨细胞的Western blot和ELISA进行机制研究.
主要成果:
- 六种新的ent-labdanes,andropanilides D-I,与已知的十五种化合物一起被确定.
- 安德罗巴尼利德D表现出强大的抗炎活性 (IC50 = 2.31 μM),表现优于德克萨米他 (IC50 = 6.52 μM) 和安德罗格拉福利德 (IC50 = 5.89 μM).
- 安德罗巴尼利德D显著降低了TNF-α,IL-6和IL-1β的分泌,并降低了COX-2和iNOS蛋白质的表达.
结论:
- 安德罗巴尼利德D具有显著的抗炎功能,超过了现有的对照剂.
- 这一发现扩大了来自Andrographis paniculata的已知抗炎化合物.
- 安德罗巴尼利德D代表了开发新的抗炎疗法的有希望的候选人.
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