昆明山海棠茎叶中的二萜类成分及生物活性研究

Diterpenoids of the Stem and Leaf of Tripterygium Hypoglaucum and Their Biological Activities

利用羟丙基葡聚糖凝胶、正相硅胶、反相硅胶等色谱层析材料及半制备高效液相色谱(semi-PHPLC)等色谱层析技术,从昆明山海棠茎叶的95%甲醇水提取液中分离鉴定了9个二萜类化合物(包括对映贝壳杉烷型1,松香烷型2~8和异海松烷型9),其中化合物3,5和8为首次从该植物分离得到.采用MTT法、Griess法和CellTiter-Glo化学发光法评价了肝癌细胞毒、NO生成抑制和抗流感病毒活性,化合物8对肝癌HepG2(IC50=0.2μM)和肝癌阿霉素耐药株HepG2/Adr(IC50=2.7μM)具有显著的细胞毒活性;2,3,7和8具有显著的抑制NO生成活性(IC50范围:0.0019~15.4μM);化合物4和7具有抗A/PR/8/34(H1N1)流感病毒(达菲耐药株)活性,EC50分别为38.6±10.7μM和22.9±6.4μM;化合物7还具有显著的抗A/Hong Kong/8/68(H3N2)流感病毒(敏感株)活性,EC50为21.6±0.6μM.

Nine diterpenoids,one kaurane-type(1),six abietane-type(2-8),and one isopimarane-type(9),were isolated from 95%MeOH/H2O extract of Tripterygium hypolaucum by column chromatography using Sephadex LH-20,normal phase silica gel and reversed phase silica gel,as well as semi-preparative high performance liquid chromatography(semi-PHPLC).Compounds 3,5,and 8 were isolated from T.hypoglaucum for the first time.The cytotoxicity,NO production inhibitory activity,and anti-influenza activity were evaluated by using the MTT,Griess,and Cell Titer-Glo chemiluminescence methods,respectively.Compound 8 showed significant cytotoxicity against HepG2(IC50=0.2μM)and HepG2/Adr cells(IC50=2.7μM).Compounds 2,3,7,and 8 exhibited significant activity in inhibiting NO production(IC50 from 0.0019 to 15.4μM).Compounds 4 and 7 have anti A/PR/8/34(H1 N1)influenza virus(oseltamivir-resistance)activity with EC50 values of 38.6±10.7μM,and 22.9±6.4μM,respectively.Compound 7 exhibited anti A/Hong Kong/8/68(H3 N2)influenza virus(sensitivity)activity with EC50 value of 21.6±0.6μM.