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目的合成7-羟基-α,β-二苄基-γ-丁内酯类木脂素并观察其抗炎活性。方法设计合成了15个目标化合物(7a-7o),结构经MS、1H-NMR确认。通过巴豆油致小鼠耳肿胀试验观察合成产物的局部用药抗炎活性。结果大部分目标化合物具有抑制小鼠耳肿胀活性,其中化合物7e活性最强,抑制率达60.5%,略好于阳性药吲哚美辛。结论目标化合物具有明显的抗炎活性,苯环上甲氧基和羟基的位置和数量对抗炎活性有影响,值得进一步研究。
AIM: To synthesize 7-hydroxy-α, β-dibenzyl-γ-butyrolactones and observe its anti-inflammatory activity. Methods Fifteen target compounds (7a-7o) were designed and synthesized. Their structures were confirmed by MS and 1H-NMR. Topical anti-inflammatory activity of the synthesized product was observed by croton oil-induced mouse ear swelling test. Results Most of the target compounds had inhibitory activity on mice ear swelling. Among them, compound 7e had the strongest activity with the inhibition rate of 60.5%, slightly better than the positive drug indomethacin. Conclusion The target compound has obvious anti-inflammatory activity. The position and number of methoxy and hydroxyl on the benzene ring have an impact on the anti-inflammatory activity and deserve further study.