目的 探究玫瑰花的抗炎活性，并建立基于超高效液相色谱-四级杆/飞行时间质谱（UPLC-Q/TOF）结合荧光素酶报告基因检测系统筛选玫瑰花中核转录因子-κB（NF-κB）抑制剂的方法。方法 通过建立铜绿假单胞菌感染的小鼠急性肺感染模型来进行玫瑰花水提物的抗炎药效学评价，同时采用UPLC-Q/TOF结合NF-κB荧光素酶报告基因检测系统筛选玫瑰花提取物的抗炎药效物质基础。结果 动物实验结果表明，玫瑰花给药组能显著改善铜绿假单胞菌感染的小鼠肺部中性粒细胞浸润，降低肿瘤坏死因子-α（TNF-α）、白细胞介素-6（IL-6）、IL-8等细胞炎症因子水平。得到玫瑰花谱效关系图并筛选出7个NF-κB抑制剂。结论 玫瑰花能减轻铜绿假单胞菌感染的小鼠炎症反应。7个单体物质（包括没食子酸、4-O-没食子酰基奎宁酸、没食子酸甲酯、矢车菊黄素、小木麻黄素、木麻黄鞣质及并没食子酸）可能为玫瑰花中潜在的NF-κB抑制剂。

Objective To investigate the anti-inflammatory effect of Rosae Rugosae Flos (RRF) and screen its bioactive components on nuclear factor-κappa B (NF-κB) inhibition by ultra-performance liquid chromatography coupled with quadrupole/time of flight mass spectrometry (UPLC-Q/TOF MS). Methods The anti-inflammatory effect of RRF was assessed in Pseudomonas aeruginosa strain-induced acute lung infection mouse model. UPLC-Q/TOF MS coupled with NF-κB activity luciferase reporter assay system was applied to detect the potential anti-inflammatory components in RRF extract. Results The administration of RRF extract could ameliorate the neutrophil infiltration and diminish the levels of inflammatory cytokines such as tumor necrosis factor-α (TNF-α), interlukin-6 (IL-6), and IL-8 in P. aeruginosa induced mice. Seven components were screened to have potential NF-κB inhibitory effects based on the bioactivity-integrated UPLC-Q/TOF assay system. Conclusion RRF can contribute to the alleviation of inflammation in mice with acute lung infection induced by P. aeruginosa strain. Seven potentially active ingredients, such as gallic acid, 4-O-galloylquinic acid, methylgallate, centaureidin, strictinin, casuariin, and ellagic acid are found to have anti-inflammatory effects as NF-κB inhibitors.

国家自然科学基金资助项目（81102835）