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目的研究中国南海海绵Iotrochotasp.的化学成分。方法应用正、反相硅胶柱色谱、Sephadex LH-20凝胶柱色谱、半制备反相高效液相色谱(RP-HPLC)等多种色谱手段,对海绵Iotrochotasp.的二氯甲烷提取物进行分离纯化,从中得到6个单体化合物,运用现代波谱技术结合文献报道对其进行结构鉴定,采用MTT法对分离得到的6个化合物进行人高转移肝癌细胞(LM3)和人肝癌细胞(HepG2)的体外抗肿瘤活性测试。结果分离得到6个化合物,包括4个吲哚生物碱类化合物(1-4)及2个酚类化合物(5、6),分别鉴定为:1 H-indole-3-carbaldehyde(1)、5-bromo-1 H-indole-3-carbaldehyde(2)、1 H-indole-3-hydroxyacetyl(3)、5-bromo-3-(hydroxylacetyl)-indole(4)、4-hydroxy-benzeneethanol(5)、3-hydroxy-benzeneethanol(6)。这些化合物均为首次从海绵Iotrochotasp.中分离得到,化合物2和4为C-5溴代吲哚生物碱,并对其NMR数据进行了报道。体外抗肿瘤活性测试显示,化合物3对LM3及HepG2细胞株显示不同程度的抑制活性,IC50值分别为29.3及46.3μmol/L;其他化合物不显示抑制作用(IC50>50μmol/L)。
Objective To study the chemical composition of sponge Iotrochotasp. Methods The dichloromethane extract of sponge Iotrochotasp was isolated by using various chromatographic methods, such as forward and reverse phase silica gel column chromatography, Sephadex LH-20 gel column chromatography and semi-preparative reverse phase high performance liquid chromatography (RP-HPLC) . Six compounds were isolated and purified, and their structures were identified by modern spectroscopic techniques and reported in the literature. Six compounds were isolated from human hepatocellular carcinoma cells (LM3) and human hepatocellular carcinoma cells (HepG2) by MTT assay In vitro anti-tumor activity test. Results Six compounds were isolated, including four indole alkaloids (1-4) and two phenolic compounds (5,6), which were identified as 1 H-indole-3-carbaldehyde 3-hydroxyacetyl (3), 5-bromo-3- (hydroxylacetyl) -indole (4), 4-hydroxy- benzeneethanol (5) , 3-hydroxy-benzeneethanol (6). These compounds were first isolated from the sponge Iotrochotasp. Compounds 2 and 4 were C-5 bromoindole alkaloids, and their NMR data were reported. In vitro antitumor activity test showed that compound 3 showed different degrees of inhibitory activity on LM3 and HepG2 cell lines with IC50 values of 29.3 and 46.3 μmol / L, respectively; other compounds showed no inhibitory effect (IC50> 50 μmol / L).