秭禾酮（coixol），一种从裸麦（裸麦糙齿种），经过提取的2-苯并噁唑酮衍生物，表现出良好的抗炎活性和低细胞毒性。本研究通过与肉桂酸的杂交设计和合成了26个秭禾酮衍生物，以寻找新的抗炎剂。使用LPS诱导的RAW264.7巨噬细胞中过表达的一氧化氮（NO）的方法筛选了这些衍生物的抗炎活性。根据筛选结果，含有呋喃（9c）或硝基呋喃（9j）基团的化合物比秭禾酮和瑞芬布替显示了更好的活性。机制研究揭示，9c和9j抑制了诱导型一氧化氮合酶（iNOS）、肿瘤坏死因子（TNF）-α、白细胞介素（IL）-6和IL-1β的表达，这与核因子（NF）-κB信号通路的抑制有关。体内研究证实了9c和9j在二甲基苯氧基甲烷诱导的小鼠耳廓水肿模型中的抗炎活性。初步的体外和体内研究结果表明，9c和9j具有作为抗炎剂开发的潜力。

Coixol, a derivative of 2-benzoxazolinone extracted from coix (Coix lachryma-jobi L. var. ma-yuen Stapf), has demonstrated promising anti-inflammatory activity and low cytotoxicity. In this study, 26 coixol derivatives were designed and synthesized by hybridization with cinnamic acid to identify new anti-inflammatory agents. The anti-inflammatory activities of the derivatives were screened using LPS-induced overexpression of nitric oxide (NO) in RAW264.7 macrophages. On the basis of the screening results, compounds containing furan (9c) or nitrofuran (9j) moieties displayed more pronounced activity than coixol and celecoxib. Mechanistic investigations revealed that 9c and 9j suppressed the expression of induced nitric oxide synthase (iNOS), tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β, which was associated with the inhibition of the nuclear factor (NF)-κB signaling pathway. In vivo studies confirmed the anti-inflammatory activity of 9c and 9j in a xylene-induced mice auricles edema model. The preliminary in vitro and in vivo research findings suggest that 9c and 9j have the potential to be developed as anti-inflammatory agents.