代谢物作为鉴定 COX-2 活性部位的探针，以及在体外用和体内抗炎的试剂。
Metabolites as Probes to Identify a COX-2 Active Site and as in Vitro and in Vivo Anti-Inflammatory Agents.
机构信息
School of Pharmaceutical Sciences, School of Medicine, College of Life Sciences and Oceanography, Shenzhen University, Shenzhen 518060, P. R. China.
Center for Translation Medicine Research and Development, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, P. R. China.
出版信息
Org Lett. 2020 Apr 3;22(7):2574-2578. doi: 10.1021/acs.orglett.0c00452. Epub 2020 Mar 13.
(±)-Dispirocochlearoids A-C (-), meroterpenoids with a 6/6/5/6/6/6 ring system, were isolated from . - are selective COX-2 inhibitors with an IC value of (-)- at 386 nM. Site-directed mutagenesis identified His351 as a COX-2 active site. In vivo anti-inflammatory activities of (-)- were performed against acute lung injury in mice.
(±)-Dispirocochlearoids A-C (-)，具有 6/6/5/6/6/6 环系的 Meroterpenoids，从. - 中分离得到，是选择性 COX-2 抑制剂，IC 值为 (-)- 为 386 nM。定点突变鉴定 His351 为 COX-2 的活性位点。(-)-对小鼠急性肺损伤的体内抗炎活性进行了研究。
Zotero 插件