目的从三列凹顶藻Laurenciatristicha中寻找具有多样性结构的倍半萜化学成分, 供药理活性筛选。方法采用凝胶柱色谱、硅胶柱色谱、重结晶和高效液相色谱等方法进行分离;借助包括一维和二维NMR等波谱方法和X-单晶衍射鉴定化合物的结构;用MTT法对得到的化合物进行细胞毒活性评价。结果分离得到5个倍半萜类化合物, 分别鉴定为海兔阿普里素(aplysin, )、海兔阿普里醇(aplysinol, )、去溴海兔阿普里醇(debro-moaplysinol, )、凹顶藻联苯(laurebiphenyl, )、约翰斯顿醇(johnstonol, );在人肿瘤细胞株HCT-8、Bel-7402、BGc-823、A549和HeLa模型上, 化合物对所有细胞株均显示毒性, 化合物对HeLa细胞显示中等强度的细胞毒活性, 其他化合物对所有细胞株均无明显毒性, IC₅₀均大于10.0μg/mL。结论化合物~均为首次从三列凹顶藻中得到, 化合物对HeLa细胞具有中等强度的选择性细胞毒活性, 化合物对所有细胞株均显示毒性。

To search for sesquiterpene components with structural diversity from Laurencina tristicha to supply for pharmacological activity screen.Methods Compounds were isolated by means of column chromatography over normal phase silica gel and Sephadex LH-20,recrystallization,and HPLC.Structures were identified by spectroscopic methods including 1D and 2D NMR,IR,X ray,and MS.Cy totoxieities of the purified compounds were evaluated by MTT method.Results Five sesqujterpenes,aplysin(I),aplysinol(Ⅱ),debromoaplysinol(Ⅲ),laurebiphenyl(IV),and johnstonoI(V)have been isolated and identified.In the cytotoxic assay compound IV was active against human cancer cell lines.HCT-8,Bel-7402,BGc-823,A549,and HeLa with IC₅₀values of 1.77,1.91,1.22,1.68,and 1.61ug/mL,respectively.CompoundⅢshowed cytotoxicity against HeLa with 1C₅₀ value of 3.6 ug/mL while other compounds were inactive(IC₅₀>10ug/mL).Conclusion Compounds I-V are isolated from L.tristicha for the first time.CompoundⅢshows moderate selective cytotoxicity against Hel.a cell line and tompound IV is cytotoxicity against several human cancer eell lines.

国家863计划(2004AA625030;2001AA620503);国家自然科学基金资助项目(20432030);中国科学院方向性创新(KZCX3-SW-215);青岛市科技发展计划项目(04-2-NN-26)