新型不饱和甘草次酸衍生物的设计、合成及抗炎活性研究。
Novel unsaturated glycyrrhetic acids derivatives: Design, synthesis and anti-inflammatory activity.
机构信息
School of Pharmacy, Anhui Province Key Laboratory of Major Autoimmune Diseases, Anhui Institute of Innovative Drugs, Anhui Medical University, Hefei 230032, China.
Elion Nature Biological Technology Co., Ltd, Nanjing 210038, China.
出版信息
Eur J Med Chem. 2017 Oct 20;139:337-348. doi: 10.1016/j.ejmech.2017.08.002. Epub 2017 Aug 3.
To develop novel anti-inflammatory agents, a series of unsaturated glycyrrhetic acids were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. The structure-activity relationship (SAR) of NO inhibitory activity was analyzed. α,β-Unsaturated glycyrrhetic acids showed better activity, among them, compounds 6k and 6l with piperazine unit exhibited the most potent nitric oxide (NO) and interleukin-6 (IL-6) inhibitory activity (IC = 13.3 and 15.5 μM respectively). Furthermore, compound 6k could also significantly suppress LPS-induced iNOS and COX-2 expression and IL-6 production through MAPKs and NF-kB signaling pathway.
为了开发新型抗炎药物，设计、合成了一系列不饱和甘草次酸，并通过 RAW264.7 细胞评估其抗炎活性。分析了 NO 抑制活性的构效关系（SAR）。α，β-不饱和甘草次酸表现出更好的活性，其中具有哌嗪单元的化合物 6k 和 6l 表现出最强的一氧化氮（NO）和白细胞介素-6（IL-6）抑制活性（IC 分别为 13.3 和 15.5μM）。此外，化合物 6k 还可以通过 MAPKs 和 NF-kB 信号通路显著抑制 LPS 诱导的 iNOS 和 COX-2 表达和 IL-6 产生。
Zotero 插件