酯类双缩合化合物的合成及抗炎活性研究

目的:合成新型的丹皮酚衍生物,并研究其抗炎活性。方法:以丹皮酚、乙醇胺、非甾体抗炎药为原料,经修饰后与非甾体抗炎药缩合,合成6个目标化合物。以布洛芬为对照,二甲苯致炎法考察目标化合物的抗炎活性,并且探究目标化合物小鼠胃肠道的不良反应。结果:化合物的结构经¹H-NMR及MS得到确证,6个目标化合物均能显著减轻小鼠的耳肿胀,与阳性对照组相比,都具有良好的抗炎效果,同时能明显减少小鼠炎症组织中的前列腺素E₂(PGE₂)的含量。结论:合成6个丹皮酚衍生物,抗炎活性均明显强于布洛芬,且胃肠道不良反应明显降低。

Synthesis and anti-inflammatory activity of ester double condensation compounds

OBJECTIVE To synthesize novel paeonol derivatives and study their anti-inflammatory activities. METHODS Paeonol, cholamine and non-steroidal antiinflammatory drugs (NSAIDs) were used as materials, modified and condensed with NSAIDs to synthesize 6 target compounds. Ibuprofen was used as reference. Anti-inflammatory activities of compounds were evaluated in xylene-induced mouse ear swelling model. Gastrointestinal side effects of target compounds were investigated. RESULTS Structures of six compounds were confirmed by ¹H-NMR and MS. Six target compounds could significantly alleviate mouse ear swelling, and had good anti-inflammatory activities compared with reference drug. Meanwhile, all six compounds could obviously decrease the content of prostaglandin E₂ (PGE₂) in inflammation tissues of mice. CONCLUSION Six paeonol derivatives synthesized show stronger anti-inflammatory activities than ibuprofen, and less gastrointestinal side effects.