摘要/Abstract
苯并呋喃是研发多种疾病药物的主要来源之一, 在合成药物化学领域受到越来越多的关注. Dorsmerunin A是一种从桑科植物中分离出来的具有弱细胞毒活性的苯并呋喃类天然产物. 以4-甲氧基水杨醛和2-溴-4'-甲氧基苯乙酮为起始原料, 经分子内缩合、还原和脱保护等4步反应, 以49%总收率首次完成了Dorsmerunin A的全合成. 另外, 采用小鼠巨噬细胞RAW264.7模型初步测试了Dorsmerunin A的体外抗炎活性及其作用机制, 结果表明该化合物在浓度为25 μmol/L时, 能有效抑制NO的生成, 且对炎症因子IL-6、IL-1β和TNF-α有显著抑制作用.
关键词: Dorsmerunin A, 全合成, 抗炎活性, 作用机制
Benzofurans have been found to be one of the major sources of drug development for a variety of diseases, and have received increasing attention in the field of synthetic medicinal chemistry. Dorsmerunin A, a natural cytotoxic product of 2-benzylbenzofurans, was isolated from the roots of Dorstenia kameruniana. In this work, Dorsmerunin A was firstly synthesized in 49% total yield from 4-methoxysalicylaldehyde and 2-bromo-4'-methoxyacetophenone through intramolecular condensation, reduction and deprotection. The in vitro anti-inflammatory activity of Dorsomerinein A was initially tested using the murine macrophage RAW264.7 model, and the results showed that it showed good inhibitory effect on NO production at a concentration of 25 μmol/L, as well as proinflammatory factors (IL-6, IL-1β and TNF-α).
Key words: Dorsmerunin A, total synthesis, anti-inflammatory activity, mechanism
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