目的 初步阐明头花蓼Polygonum capitatum醇提物和水提物与其体外抗炎活性之间的谱效关系。方法 采用脂多糖（LPS）诱导小鼠RAW264.7细胞制备细胞炎症模型，利用NO、肿瘤坏死因子-α（TNF-α）试剂盒检测细胞炎症因子释放量，利用偏最小二乘法关联UPLC-MS方法建立的指纹图谱数据和头花蓼不同提取物的药效活性指标，建立头花蓼化学成分的谱效关系。结果 头花蓼不同提取物在质量浓度小于250 mg/L时无细胞毒性，且均具有炎症抑制作用，存在一定的量效关系。应用偏最小二乘法对药效指标TNF-α和色谱峰进行关联度比较发现，峰24、17、22、23、20与抗炎药效呈正相关，峰11、1、7、15、5、3与抗炎药效呈负相关。对峰24、17、22、23、20分析发现，除17号峰为鞣花酸外，其余4个峰均为黄酮类化合物。结论 头花蓼不同提取物均可以抑制RAW264.7细胞的炎症反应，谱效关系分析得出槲皮苷、鞣花酸、金丝桃苷对头花蓼的抗炎药效（调节TNF-α水平）有较大贡献。

Objective To study the spectrum effect relationship between the water and ethanol extracts of Polygonum capitatum and its anti-inflammatory activity. Methods The inflammatory model of mice RAW264.7 cells induced by lipopolysaccharide (LPS) was established, and the release of inflammatory factors was detected by NO and TNF-α kit. The relationship of chemical constituents of P. capitatum was established by using the partial least square method to associate the fingerprint data established by UPLC-MS method and the pharmacodynamics index of different extracts of P. capitatum. Results Different extracts of P. capitatum had no cytotoxicity in the range of concentration less than 250 mg/L, and all of them had anti-inflammatory effect, which had a dose-effect relationship. By using partial least square method, the correlation degree between TNF-α and chromatographic peak was compared. The results showed that the correlation among the peaks 24, 17, 22, 23, 20 and the anti-inflammatory effect was positive, and the anti-inflammatory effect was negatively correlated with the peaks 11, 1, 7, 15, 5, 3. From the analysis of the five peaks, the results showed that all the four peaks were flavonoids except for the tannic acid at peak 17. Conclusion Different extracts of P. capitatum inhibited the inflammatory response of RAW264.7 cells. The flavonoids in P. capitatum had significant anti-inflammatory activity. The results showed that quercetin, tannic acid, and hyperoside had great contribution to the anti-inflammatory effect of P. capitatum.

国家自然科学基金资助项目（81260640）；国家“重大新药创制”科技重大专项（2014GX09301307-017）