中国南海海绵Iotrochota sp.的化学成分研究  

Chemical investigation on the South China Sea sponge Iotrocota sp.

作　　者：袁莉 汤华[1] 孙鹏[1] 庄春林[1] 王静[1] 李铁军[1] 张文[1] 

机构地区：[1]第二军医大学药学院海洋药物研究中心,上海200433

出　　处：《中国海洋药物》2016年第4期11-15,共5页Chinese Journal of Marine Drugs

基　　金：国家自然基金项目(41576157);上海市卫生系统优秀学科带头人计划项目(XBR2013111);上海市优秀学科带头人计划项目(15XD1504600)资助

摘　　要：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 investigate the chemical constituents of Iotrochotasp.collected from the South China Sea.Methods The CH2Cl2 extract of Iotrochotasp.was purified by repeated column chromatography on silica gel,Sephadex LH-20,ODS and semi-preparative RP-HPLC.The structures of isolates were determined by spectroscopic analysis and comparison with reported data.The compounds were tested in vitro for their tumor cell growth inhibitory activity towards highly human metastatic hepatocellular carcinoma LM3 and human liver cancer HepG2 cell lines.Results Six compounds were isolated and identified,including four mono-indole alkaloids,namely 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）,and two simple phenolic compounds,namely 4-hydroxy-benzeneethanol（5）,3-hydroxybenzeneethanol（6）.All the compounds were reported for the first time from the sponges of genus Iotrochota.Compounds 2 and 4 were C-5brominated indole alkaloids.Their NMR data were reported for the first time.Compound 3 showed growth inhibitory activity towards LM3 and HepG2cells in vitro,with IC50 values of 29.3and 46.3mol/L.Other compounds showed no growth inhibitory activity in vitro bioassay（IC50 〉50μmol/L）.

关 键 词：Iotrochota sp. 化学成分 吲哚生物碱类 酚类 

分 类 号：R931.6[医药卫生—生药学]