目的 研究金银花Lonicerae Japonicae Flos中酚酸类成分及其抗炎活性.方法 采用硅胶柱色谱、Sephadex LH-20柱色谱等方法分离纯化,根据理化性质和波谱数据进行结构鉴定;采用脂多糖(LPS)诱导的小鼠巨噬细胞RAW264.7炎症反应模型,考察金银花中酚酸类成分对巨噬细胞经LPS刺激后产生的炎症因子 [NO、肿瘤坏死因子-α(TNF-α)及白细胞介素-6(IL-6)] 的影响,评价其抗炎活性.结果 从金银花醋酸乙酯部位中分离得到12个化合物,包括8个酚酸、3个环烯醚萜苷和1个黄酮类成分,分别鉴定为新绿原酸(1)、隐绿原酸(2)、3,5-二咖啡酰奎宁酸(3)、3,4-二咖啡酰奎宁酸(4)、4,5-二咖啡酰奎宁酸(5)、绿原酸(6)、咖啡酸(7)、咖啡酸甲酯(8)、断氧化马钱子苷(9)、裂环马钱苷(10)、獐芽菜苷(11)和木犀草素(12).对其中的酚酸类化合物1～8进行了体外抗炎活性实验,结果表明,化合物1～8对LPS刺激的巨噬细胞炎症因子均具有不同程度的抑制作用.结论 酚酸类成分是金银花的主要抗炎活性成分之一,其中化合物7活性最强.

Objective To study the anti-inflammatory of phenolic acids from Lonicerae Japonicae Flos. Methods The compounds in the EtOAc fraction were isolated and purified by silica gel and Sephadex LH-20 column chromatographies, and preparative HPLC as well. The structures were identified by various spectroscopic data such as ESI-MS, ¹H-NMR, and ¹³C-NMR data. The anti-inflammatory effects were evaluated by a in vitro model of LPS-stimulated RAW264.7 macrophages. Results Eight phenolic acids, three iridoids, and one flavonoid were isolated from the extracts of Lonicerae Japonicae Flos and identified as 5-O-caffeoylquinic acid (1), 4-O-caffeoylquinic acid (2), 3,5-di-O-caffeoylquinic acid (3), 3,4-di-O-caffeoylquinic acid (4), 4,5-di-O-caffeoylquinic acid (5), chlorogenic acid (6), caffeic acid (7), methyl caffeate acid (8), secoxyloganin (9), secologanoside (10), sweroside (11), and luteolin (12). Compounds 1-8 showed the anti-inflammatory activity in different degrees. Conclusion Phenolic acids are the main anti-inflammatory constituents in Lonicerae Japonicae Flos. Caffeic acid shows the strongest activity in vitro.

科技部重大新药创制项目:现代中药创新集群与数字制药技术平台(2013ZX09402203)