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目的设计合成一类青藤碱衍生物,并研究其体外抗炎活性。方法以青藤碱为原料,经脱N-甲基、亲核取代、经典的Click Reaction,共合成9个青藤碱衍生物,考察所得化合物体外对NF-κB转染的影响。结果合成的目标化合物均为首次报道,并经1 HNMR和LC-MS确证结构。所得化合物体外对NF-κB转染均具有一定的抑制作用,但活性较青藤碱有所下降。结论N原子上引入较大基团或者长链可能会降低青藤碱的抗炎活性。
Objective To design and synthesize a derivative of sinomenine and study its in vitro anti-inflammatory activity. Methods Sinomenine was used as starting material to synthesize 9 sinomenine derivatives via demethylation, nucleophilic substitution and classical Click Reaction. The effects of the obtained compounds on NF-κB transfection were investigated. Results The target compounds were all reported for the first time and their structures were confirmed by 1 H NMR and LC-MS. The obtained compounds had some inhibitory effects on NF-κB transfection in vitro, but the activity was decreased compared with sinomenine. Conclusion The introduction of larger groups or long chains on the N atom may reduce the anti-inflammatory activity of sinomenine.