泽伊甲类A-D,具有抗炎活性的高氧化滴类,来自Leucas zeylanica (L.) R. Br
Ting Zhao1,2, Xuan Zhang1,2, Xu-Hua Nong1,2
1Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education Hainan Normal University, Haikou 571158, China.
Molecules (Basel, Switzerland)
|June 10, 2023
概括
从Leucas zeylanica中分离出四种新的二甲,并对其抗炎作用进行了测试. 化合物4表现出显著的氧化抑制和减少无毒的促炎性细胞因子.
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:
- 柳 (Leucas zeylanica) 是一种具有潜在药用功能的植物.
- 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:
- 从Leucas zeylanica.中分离和描述新的高氧化二氧化物.
- 为了评估隔离化合物的抗炎潜力.
主要方法:
- 使用NMR,ECD和X射线晶体学对化合物的隔离和结构阐明.
- 在体外抗炎测定包括氧化抑制,细胞因子释放和细胞毒性.
- 西方涂抹以确定分子点和分子对接以确定作用机制.
主要成果:
- 发现了四种新型的双类动物,即甲甲类动物AD-D.
- 泽伊卢卡化物D通过抑制氧化 (NO) 生产 (IC50 = 38.45μM) 显示出显著的抗炎活性.
- 化合物4剂量依赖地抑制了TNF-α和IL-6的释放,减少了iNOS和COX-2的表达,并且在斑马鱼胚胎中没有显示出毒性.
结论:
- 泽伊勒乌卡类A-D是来自Leucas zeylanica的新型双类.
- 泽伊基酸D具有强大的抗炎性质,可能通过抑制iNOS和COX-2来实现.
- 作用机制涉及和疏水性键与分子的相互作用.
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