菲兰法林A-F,来自Phyllanthus franchetianus的抗炎性恩特-克利斯坦二特类药物
Siyu Qin1, Jianbing Tan1, Yuting Zheng1
1Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, 410013, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Central South University, Changsha, Hunan, 410013, PR China.
从Phyllanthus franchetianus中分离出了六种新的克利斯坦二类物质 - - 菲兰法林A-F. 两种化合物在基于细胞的测试中显示出显著的抗炎活性.
科学领域:
- 自然产品化学 自然产品化学
- 植物化学 植物化学
- 药用化学 医学化学
背景情况:
- 弗朗切蒂安纳斯 (Phyllanthus franchetianus) 是一种具有潜在药用功能的植物物种.
- 迪特尔类是一种具有多样化的生物活动的自然产品类.
研究的目的:
- 为了分离和描述Phyllanthus franchetianus的化学成分.
- 评估隔离化合物的抗炎潜力.
主要方法:
- 采用色谱技术进行提取和分离.
- 使用HRESIMS,NMR光谱和ECD计算进行结构阐明.
- 用X射线晶体学来确定绝对配置.
- 在体外使用LPS刺激的RAW264.7巨细胞进行抗炎试验.
主要成果:
- 确定了6种新的克利斯坦二类 (菲兰法林A-F) 和3种已知的化合物.
- 菲兰法林F是第一个报告的具有6/6/6/6四环系统的ent-cleistanthane diterpenoid.
- 化合物4和8表现出显著的氧化 (NO) 抑制活性,IC50值分别为19.03微米和18.14微米.
结论:
- 这项研究扩大了克利斯坦二甲的化学多样性.
- 化合物4和8显示出作为抗炎药物的潜力.
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