岩黄连乙酸乙酯部位化学成分及其抗炎活性研究

Chemical constituents of ethyl acetate extract from Corydalis saxicola and its anti-inflammatory activity

为研究岩黄连的化学成分及其抗炎活性,该研究采用硅胶、MCI、Sephadex LH-20、制备型高效液相色谱等方法对岩黄连95%乙醇提取物的乙酸乙酯萃取部位进行分离和纯化,通过核磁共振波谱(NMR)、高分辨质谱(HR-MS)等谱学手段鉴定其结构,同时采用脂多糖(LPS)诱导的小鼠巨噬细胞RAW264.7建立体外炎症筛选模型,并评价其抗炎活性。结果表明:从岩黄连乙醇提取物的乙酸乙酯部位中分离并鉴定了13个化合物,分别为黄连碱(1)、盐酸小檗碱(2)、文殊兰新碱(3)、甲基小檗碱(4)、脱氢卡维丁(5)、左旋四氢巴马汀(6)、药根碱(7)、紫堇定(8)、反式阿魏酸酰对羟基苯乙胺(9)、对苯二甲酸二丁酯(10)、山奈酚(11)、异地芰普内酯(12)、地芰普内酯(13)。其中,化合物3、4、8-13为首次从该植物中分离获得;化合物4、9、11对LPS诱导巨噬细胞RAW264.7产生炎症因子NO均具有良好的抑制作用,半抑制浓度(IC_(50))值分别为(18.8±0.2)、(29.1±0.3)、(18.0±0.1)μmol·L^(-1),优于阳性对照吲哚美辛,在抗炎药物的研究与开发中表现出良好的发展潜力。该研究结果明确了岩黄连的抗炎物质基础,为其进一步深度研究与开发利用提供了一定的科学依据。

Corydalis saxicola which belongs to the family of Papaveraceae,is always used to treat various diseases such as hepatitis B,cirrhosis,furuncle,acute icteric hepatitis,and advanced cancer as traditional Zhuang medicine in Guangxi province.To study the anti-inflammatory activity of the chemical constituents of C.saxicola,silica gel,MCI,Sephadex LH-20 column chromatography and preparative high performance liquid chromatography were used to separate the chemical constituents from the ethyl acetate fraction of 95%ethanol extract of C.saxicola.Their structures were identified by nuclear magnetic resonance(NMR)and high resolution mass spectrum(HR-MS).In addition,the anti-inflammatory activity was evaluated by the mouse macrophage RAW264.7 induced by lipopolysaccharide(LPS).The results showed that 13 chemical compounds were isolated and identified as coptisine(1),berberine hydrochloride(2),crinumaquine(3),worenine(4),dehydrocavidine(5),(-)-tetrahydropalmatine(6),jatrorrhizine(7),corydaldine(8),N-trans-feruloyl tyramine(9),dibutylterephthalate(10),kaempferol(11),isololiolide(12),loliolide(13)respectively.Compounds 3,4,8-13 were isolated from this plant for the first time.Compounds 4,9 and 11 showed good inhibitory effects on LPS induced NO production by macrophage RAW264.7 with IC_(50)values of(18.8±0.2),(29.1±0.3),(18.0±0.1)μmol·L^(-1)respectively,which was better than the positive control indomethacin,exhibited good potential in the research and development of anti-inflammatory drugs.These results can clarify the anti-inflammatory material basis of C.saxicola,and provide a scientific theoretical basis for its further utilization.