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[摘要]
目的 对腰痹通胶囊内容物醇提抗炎活性部位的化学成分进行研究。方法 采用体外抗炎模型进行活性部位的筛选,运用硅胶柱色谱、Sephadex LH-20以及制备型HPLC等方法对活性部位进行分离纯化,根据理化性质及波谱数据对得到的单体化合物进行结构鉴定;采用脂多糖(LPS)诱导的大鼠胸主动脉平滑肌细胞(A7r5)炎症反应模型,考察化合物对炎症因子NO的影响,评价其抗炎活性。结果 从腰痹通胶囊内容物中共分离得到11个化合物,包括2个有机酸、1个生物碱、2个洋川芎内酯、1个倍半萜和5个香豆素类成分,分别鉴定为咖啡酸乙酯(1)、阿魏酸(2)、延胡索甲素(3)、洋川芎内酯H (4)、洋川芎内酯I (5)、藁本酚(6)、哥伦比亚苷元(7)、尤劳帕替醇(8)、meranzin hydrate (9)、angelitriol (10)、6-[1(R),2(R)-1,2,3-thihydroxy-3-methylbutyl]-7-methoxycoumarin (11)。化合物1~6对LPS刺激的A7r5细胞炎症因子NO具有不同程度的抑制作用。结论 化合物1、3、6、8~11为首次从该复方中分离得到,有机酸和洋川芎内酯类化合物可能是腰痹通胶囊抗炎的主要活性成分。
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[Abstract]
Objective To investigate the anti-inflammatory constituents from the ethanol extract of Yaobitong Capsule.Methods The chemical constituents were isolated by repeated silica gel column, Sephadex LH-20, and preparative HPLC. The structures were identified by various spectral data analysis and physicochemical properties. The anti-inflammatory effects were evaluated by in vitro model of LPS-stimulated rat thoracic aortic smooth muscle cells (A7r5).Results Eleven compounds were isolated from the contents of the capsule, including 2 organic acids, 1 alkaloid, 2 senkyunolides, 1 sesquiterpene, and 5 coumarins, which identified as ethyl caffeate (1), ferulic acid (2), corydaline (3), senkyunolide H (4), senkyunolide I (5), ligustiphenol (6), columbianetin (7), ulopterol (8), meranzin hydrate (9), angelitriol (10), and 6-[1(R),2(R)-1,2,3-thihydroxy-3-methylbutyl]-7-methoxycoumarin (11). Compounds 1—6 showed the anti-inflammatory activity in different degrees.Conclusion Compounds 1, 3, 6, and 8—11 are isolated from Yaobitong Capsule for the first time, and organic acids and senkyunolide compounds may be the anti-inflammatory pharmacodynamic material bases of Yaobitong Capsule.
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[基金项目]
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)