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金银花中酚酸类成分及其抗炎活性研究

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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.
Study on anti-inflammatory activities of phenolic acids from Lonicerae Japonicae Flos
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.

Lonicerae Japonicae Flosphenolic acidsanti-inflammatory activity3,5-di-O-caffeoylquinic acidchlorogenic acidcaffeic acidsecologanoside

宋亚玲、王红梅、倪付勇、王雪晶、赵祎武、黄文哲、王振中、萧伟

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江苏康缘药业股份有限公司,江苏连云港222000

中药制药过程新技术国家重点实验室,江苏连云港222000

金银花 酚酸类 抗炎活性 3,5-二咖啡酰奎宁酸 绿原酸 咖啡酸 裂环马钱苷

科技部重大新药创制项目:

2013ZX09402203

2015

10.7501/j.issn.0253-2670.2015.04.006

中草药
天津药物研究院,中国药学会

中草药

CSTPCDCSCD北大核心
影响因子：1.632
ISSN：0253-2670
年,卷(期)：2015.46(4)
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