论文部分内容阅读
目的合成丹皮酚及其类似物与萘普生的酯化产物,并研究其抗炎活性。方法将萘普生分别与丹皮酚、2-羟基-5-甲氧基-苯乙酮、3-羟基苯乙酮、2-羟基苯乙酮和3-甲氧基苯酚通过酯化反应合成系列化合物。用HPLC考察目标化合物在不同pH缓冲液中的降解情况,用二甲苯致小鼠耳肿胀模型对其进行抗炎活性筛选。结果合成了5个目标化合物,经MS和1H-NMR确证其结构。HPLC证明其在体内稳定。小鼠实验表明,目标化合物具有较强的抗炎作用。结论目标化合物在胃肠道pH值中稳定,抗炎活性较强,值得进一步研究。
OBJECTIVE To synthesize esterification products of paeonol and its analogues with naproxen and study their anti-inflammatory activity. Methods Naproxen was respectively esterified with paeonol, 2-hydroxy-5-methoxy-acetophenone, 3-hydroxyacetophenone, 2-hydroxyacetophenone and 3-methoxyphenol Series of compounds. The degradation of the target compound in different pH buffers was investigated by HPLC. The anti-inflammatory activity of the target ear swelling model was screened by xylene. Results Five target compounds were synthesized and confirmed by MS and 1H-NMR. HPLC proved stable in the body. Mouse experiments show that the target compound has a strong anti-inflammatory effect. Conclusion The target compound is stable in the gastrointestinal pH value and has strong anti-inflammatory activity, which deserves further study.