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综合运用正相和反相硅胶柱层析、Sephadex LH-20凝胶柱层析以及制备HPLC等分离方法,从1种中国南海海绵Xestospongia testudinaria中追踪分离抗肿瘤活性次级代谢产物。从95%乙醇提取物中分离获得8个单体化合物,通过NMR,MS等波谱技术鉴定其结构分别为:E-18,18-二溴-9,17-二烯-5,7-二炔硬脂酸甲酯(1),E-18,18-二溴-9,17-二烯-5,7-二炔硬脂酸乙酯(2),麦角甾-5,7,22-三烯-3-醇(3),麦角甾-4,6,8(14),22-四烯-3-酮(4),胆甾-4-烯-3-酮(5),3-吲哚醛(6),3-吲哚酸(7)和5-吲哚醛(8)。其中,化合物2-5和8为首次从该属海绵中分离得到。化合物1对肿瘤细胞株HCT116和A549显示较强的抑制活性。
The antitumor secondary metabolites were traced and isolated from one species of the South China Sea sponge Xestospongia testudinaria using normal-phase and reversed-phase silica gel column chromatography, Sephadex LH-20 gel column chromatography and preparative HPLC. Eight monomer compounds were isolated from the 95% ethanol extract. Their structures were identified by NMR, MS and other spectroscopic methods respectively as follows: E-18,18-Dibromo-9,17-diene-5,7-diyne Methyl stearate (1), ethyl E-18,18-dibromo-9,17-diene-5,7-diyne stearate (2), ergistetra-5,7,22-tris (4), Cholest-4-en-3-one (5), 3-indole Indole aldehyde (6), 3-indole acid (7) and 5-indolyl aldehyde (8). Among them, compounds 2-5 and 8 were isolated from this sponge for the first time. Compound 1 showed strong inhibitory activity on tumor cell lines HCT116 and A549.