海洋来源真菌Eutypella sp. F0219细胞松弛素类代谢产物及其抗肿瘤活性

Cytochalasins Isolated from the Marine-derived Fungus Eutypella sp.F0219 and Their Anti-tumor Activities

综合运用正、反相硅胶柱层析、薄层层析以及半制备HPLC等多种色谱方法对海洋真菌Eutypella sp.F0219的乙酸乙酯提取物进行系统分离纯化,获得8个细胞松弛素类化合物(1~8)。经一维核磁共振波谱数据、质谱以及X-射线单晶衍射方法等确定这些化合物分别为phenochalasin A (1),scoparasin D (2),phenochalasin B (3),cytochalasin Z26(4),cytochalasin Z24(5),[12]-cytochalasin (6),cytochalasin Z25(7)和cytochalasin Z27(8)。通过CCK-8实验评价上述化合物在非小细胞肺癌NCI-H1299细胞的增殖影响,筛选结果表明化合物2表现出中等的抗肿瘤活性,IC50值为(5.1±0.25)μmol/L。本研究首次报道了化合物phenochalasin A (1)的X-射线单晶结构。

Eight cytochalasins were isolated from the ethyl acetate extract of the marine-derived fungus Eutypella sp.F0219 by applying silica gel and C18 revised-phase column chromatography,TLC,and semi-preparative HPLC methods.On the basis of 1D-NMR,ESI-MS,and single-crystal X-ray diffraction crystallography,the structures of these compounds were elucidated as phenochalasin A(1),scoparasin D(2),phenochalasin B(3),cytochalasin Z26(4),cytochalasin Z24(5),[12]-cytochalasin(6),cytochalasin Z25(7),cytochalasin Z27(8),respectively.These compounds were evaluated for cytotoxic activities against NCI-H1299 cell line by the assay of CCK-8.Compound 2 exhibited moderate cytotoxicity with IC50 value of(5.1±0.25)μmol/L.In addition,this is the first report of the X-ray structure of phenochalasin A(1).