Mauritius Oceanography Institute, France Centre, Quatre-Bornes, Mauritius.
Institut de Chimie des Substances Naturelles, CNRS UPR 2301, Centre de Recherche de Gif, Gif sur Yvette, France.
Environ Toxicol Pharmacol. 2012 Sep;34(2):397-408. doi: 10.1016/j.etap.2012.05.013. Epub 2012 Jun 9.
The ocean is an exceptional source of natural products with many of them exhibiting novel structural features and bioactivity. As one of the most interesting phylum with respect to pharmacological active marine compounds, Poriferas have been investigated widely in the last few decades. A total of 60 organic extracts (hexane, ethyl acetate and butanol) from 20 species of marine sponges from Mauritius were screened at 50μg/ml in an in vitro screening assay against 9 human cancer cell lines. From these tested extracts, many exhibited pronounced cytotoxic effect at least in one of the cell lines and cell type cytotoxic specificity was observed. 27% of ethyl acetate, 11% of hexane and 2% of butanol extracts were found to possess a cytotoxicity ≥75% on 9 different cancer cell lines with the sponges Petrosia sp. 1, Petrosia sp. 2, Pericharax heteroraphis and Jaspis sp. being the most active. Overall, the HL-60cells were much more sensitive to most of the extracts than the other cell lines. We further evaluated the properties of the ethyl acetate (JDE) and hexane extract (JDH) of one sponge, Jaspis sp. on KB cells. JDE displayed a smaller IC(50) than JDH. Clonogenic assay confirmed the antiproliferative effect of both extracts while mitochondrial membrane potential change and microscopic analysis demonstrated extracts-induced apoptosis. Treatment with 100ng/ml of JDE led to a significant increase of cells (24h: 4.02%; 48h: 26.23%) in sub-G1 phase. The cytotoxic properties of the tested extracts from these sponges suggest the presence of compounds with pharmacological potential and are currently undergoing fractionation to isolate the active constituents.
海洋是天然产物的特殊来源，其中许多具有新颖的结构特征和生物活性。作为最有趣的具有药理活性海洋化合物的门之一，多孔动物在过去几十年中得到了广泛的研究。从毛里求斯的 20 种海洋海绵中提取的 60 种有机提取物（己烷、乙酸乙酯和正丁醇），在 50μg/ml 的体外筛选试验中针对 9 个人类癌细胞系进行了筛选。从这些测试的提取物中，许多在至少一种细胞系中表现出明显的细胞毒性作用，并且观察到细胞类型细胞毒性特异性。27%的乙酸乙酯、11%的己烷和 2%的正丁醇提取物对 9 种不同的癌细胞系具有≥75%的细胞毒性，其中海绵 Petrosia sp.1、Petrosia sp.2、Pericharax heteroraphis 和 Jaspis sp.最为活跃。总体而言，HL-60 细胞对大多数提取物的敏感性比其他细胞系高得多。我们进一步评估了一种海绵 Jaspis sp.的乙酸乙酯（JDE）和正己烷提取物（JDH）对 KB 细胞的特性。JDE 的 IC50 小于 JDH。集落形成试验证实了两种提取物的抗增殖作用，而线粒体膜电位变化和显微镜分析表明提取物诱导了细胞凋亡。用 100ng/ml 的 JDE 处理导致细胞（24h：4.02%；48h：26.23%）在 sub-G1 期显著增加。这些海绵的测试提取物具有细胞毒性，表明存在具有药理潜力的化合物，目前正在进行分离活性成分的分馏。
