Resolvin E3 的合成，一种促解决的脂质介质，及其脱氧衍生物：鉴定 18-脱氧-Resolvin E3 为一种有效的抗炎剂。
Synthesis of Resolvin E3, a Proresolving Lipid Mediator, and Its Deoxy Derivatives: Identification of 18-Deoxy-resolvin E3 as a Potent Anti-Inflammatory Agent.
机构信息
Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
出版信息
J Org Chem. 2020 Nov 6;85(21):14190-14200. doi: 10.1021/acs.joc.0c01701. Epub 2020 Oct 13.
We synthesized RvE3 and its deoxy derivatives, 17-deoxy-RvE3 and 18-deoxy-RvE3, by a common route via Sonogashira coupling as a key step. The evaluation of their anti-inflammatory activities revealed that 18-deoxy-RvE3 was remarkably more potent than the parent RvE3 and significantly active at a 300 fg dose in mice; additionally, 17-deoxy-RvE3 was significantly less potent than the parent RvE3. For the first time, we found that the 17-hydroxy group of RvE3 is very important for anti-inflammatory activity.
我们通过 Sonogashira 偶联反应这一关键步骤，以通用路线合成了 RvE3 及其脱氧衍生物，17-脱氧-RvE3 和 18-脱氧-RvE3。评估它们的抗炎活性表明，18-脱氧-RvE3 比母体 RvE3 显著更有效，在小鼠中 300fg 剂量时就有显著活性；此外，17-脱氧-RvE3 的效力明显低于母体 RvE3。我们首次发现，RvE3 的 17-羟基对抗炎活性非常重要。
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