鬼针草乙醇提取物化学成分及其生物活性研究

Studies on the compounds of ethanol extracts from Bidens bipinnata L. and their biological activities

目的对鬼针草乙醇提取物化学成分进行分离纯化鉴定,并初步筛选出具有较好生物活性的单体。方法用HPD 100型大孔吸附树脂、小孔树脂凝胶MCI、Sephadex LH-20凝胶、硅胶等柱层析方法分离纯化,经核磁解析并与文献比对鉴定结构。体外培养HSC-T6肝星状细胞和RAW264.7腹腔巨噬细胞,不同浓度(6.25、12.5、25、50、100μmol/L)单体化合物刺激后,MTT法观察单体化合物对细胞增殖的影响,ELISA法测定单体化合物对RAW264.7细胞分泌肿瘤坏死因子(TNF)-α的影响。结果本研究中共得到12个单体化合物,分别为:咖啡酸乙酯(1)、异奥卡宁(2)、苏式-二羟基脱氢二松柏醇(3)、正二十八烷(4)、橙皮苷(5)、柚皮素(6)、芹菜素(7)、山奈酚-3-O-α-l-鼠李糖苷(8)、木犀草素(9)、麦芽糖(10)、没食子酸(11)、金丝桃苷(12),其中化合物1、3为首次从该植物中分离得到。化合物9、11(6.25~100μmol/L)可抑制HSC-T6细胞增殖反应,并显著减少RAW264.7细胞培养上清液中的TNF-α浓度。结论本研究从鬼针草乙醇提取物中分离12个单体化合物,其中2个为首次分离得到。化合物9和11具有一定的体外抑制HSC-T6细胞增殖和RAW264.7细胞分泌TNF-α的作用。

Objective To isolate,purify and identify the chemical constituents from the ethanol extracts of Bidens bipinnata L. and screen for the bio activity. Methods The constituents of the total flavonoids of Bidens bipinnata L. were isolated by macroporous resin HPD100,following by middle chromatogram isolated gel（ MCI）,Sephadex LH-20 and silica gel column chromatography. The structures were identified by NMR. The HSC-T6 cells and RAW264. 7 cells were cultured and stimulated with the compounds with the concentrations ranging from 6. 25 to 100μmol/L. The cell proliferation ability was detected using MTT method,and the concentration of tumor necrosis factor α in the supernatant of RAW264. 7 cells was measured via ELISA. Results Twelve compounds were isolated and identified as ethyl caffeate（ 1）,isookanin（ 2）,Threo-dihydroxydehydrodiconiferyl alcohol（ 3）,octacosane（4）,hesperidin（5）,naringenin（6）,apigenin（7）,keampferol-3-O-α-l-rhamnoside（8）,luteolin（9）,maltose（10）,gallic acid（11）,hyperin（12）. Compounds 1 and 3 were isolated from this genus for the first time. Components 9 and 11 could inhibit the proliferation of HSC-T6 cells and decrease the tumor necrosis factor α concentration in the supernatant of RAW264. 7 cells. Conclusion Twelve compounds are isolated from ethanol extracts of Bidens bipinnata L.,among which compound 1 and 3 are first isolated. Compound 9 and 11 could inhibit the proliferation of HSC-T6 cells and decrease the TNF-α concentration in the supernatant of RAW264. 7 cells in vitro.