A novel series of hybrids designed on the basis of aurantiamide acetate and isopropylated genipin were synthesized and biologically evaluated as anti‐inflammatory agents. Among them, compound 7o exhibited the best inhibitory activity against TNF‐α secretion (IC₅₀ = 16.90 μM) and was selected for further in vitro and in vivo functional study. The results demonstrated that 7o was capable of suppressing the expression of LPS‐induced iNOS and COX‐2, as well as reducing the production of NO at the concentration of 5 μM, which may be resulted from its regulation of NF‐κB signaling and MAPK signaling. Moreover, compound 7o exhibited favorable in vivo anti‐inflammatory activity with an inhibition rate of 53.32% against xylene‐induced ear swelling in mice at the dose of 5 mg/kg.

中文翻译：

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醋酸橙皮酰胺和异丙基化京尼平的混合物作为潜在的抗炎剂：设计、合成和生物学评价

合成了一系列基于醋酸橙皮酰胺和异丙基化京尼平设计的新型杂化物，并在生物学上评估为抗炎药。其中，化合物7o对 TNF- α分泌的抑制活性最好（IC ₅₀  = 16.90 μM），被选为进一步的体外和体内功能研究。结果表明，70是能够抑制LPS诱导的iNOS和COX-2的表达，以及减少在5μM的浓度，这可从其NF-的调整来产生NO的产生的κ乙信令和MAPK 信号。此外，化合物7o 在 5 mg/kg 的剂量下，对二甲苯引起的小鼠耳肿胀的抑制率为 53.32%，显示出良好的体内抗炎活性。