1,10-贝壳杉烷二萜类化合物来自和它们的抗炎作用。

1,10-Secoguaianolides from and Their Anti-Inflammatory Effects.

机构信息

Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China.

出版信息

Molecules. 2018 Jul 5;23(7):1639. doi: 10.3390/molecules23071639.

Seven 1,10-secoguaianolides ⁻, including a new one (compound ), were isolated from and identified by HRESIMS and other spectroscopic methods. Their anti-inflammatory effects were evaluated by the model of LPS-induced RAW264.7 cells in . Bioassay results showed that six of them (⁻, and ), with the exception of , produce some cytotoxicity on RAW264.7 cells at its high dosage, can significantly decrease the release of NO, TNF-, IL-1, IL-6 and PGE2 in a dose dependent manner, and down-regulate the expression of proteins iNOS and COX-2. The mechanism study indicated they regulated the NF-B dependent transcriptional activity through decreasing the phosphorylation of NF-B. Further, the relationship between their structures and cytokines to anti-inflammatory were studied by PCA and discussed.

从中分离得到了 7 个 1,10-贝壳杉烷二萜，包括一个新化合物（化合物），并通过高分辨质谱和其他光谱方法进行了鉴定。通过 LPS 诱导的 RAW264.7 细胞炎症模型评价了它们的抗炎活性。生物测定结果表明，其中 6 个化合物（−、− 和），除外，在高剂量时对 RAW264.7 细胞表现出一定的细胞毒性，能够显著剂量依赖性地降低 NO、TNF-α、IL-1、IL-6 和 PGE2 的释放，并下调 iNOS 和 COX-2 蛋白的表达。机制研究表明，它们通过降低 NF-κB 的磷酸化来调节 NF-κB 依赖的转录活性。此外，通过 PCA 进一步研究了它们的结构与细胞因子之间的抗炎关系，并进行了讨论。