基于多样性导向合成的海松烷类衍生物作为潜在的抗炎药物。
Diversity-oriented synthesis of cembranoid derivatives as potential anti-inflammatory agents.
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China; Nano Science and Technology Institute, University of Science and Technology of China, 166 Ren Ai Road, Suzhou 215123, China.
Laboratory of Anti-inflammation and Immunopharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
出版信息
Bioorg Chem. 2021 Jun;111:104887. doi: 10.1016/j.bioorg.2021.104887. Epub 2021 Apr 6.
Eleven novel cembranoid derivatives were designed, synthesized, and evaluated for their inflammation related activities on the basis of our isolated and previously reported anti-inflammatory marine cembranoids. In bioassay, compound 11 displayed the most promising inhibitory effects with IC value of 1.1 μM for the TNF-α inhibitory activity. The further mechanism study of 11 on the inflammatory signaling transduction of RAW264.7 cells was also performed. This research may give an insight for the discovery of marine cembranoid derived anti-inflammatory drug leads.
基于我们分离得到的具有抗炎活性的海洋枞烷类化合物，我们设计、合成并评价了 11 种新型枞烷类衍生物，研究其与炎症相关的活性。在生物测定中，化合物 11 表现出最有前景的抑制作用，其对 TNF-α 的抑制活性的 IC50 值为 1.1 μM。我们还对 11 抑制 RAW264.7 细胞炎症信号转导的作用机制进行了进一步研究。这项研究可能为发现海洋枞烷类衍生的抗炎药物先导化合物提供新的思路。
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