澳大利亚厚皮海绵化学成分分离鉴定及其抗肿瘤活性研究

为进一步探求澳大利亚厚皮海绵Craniella australiensis在海洋药物研制中的作用,采用硅胶柱层析及Sephadex LH-20凝胶过滤层析等技术,从澳大利亚厚皮海绵乙酸乙酯层浸膏中分离纯化出两种化合物,并通过波谱数据与文献对照的方法对化合物进行了结构鉴定,采用CCK-8法对2个化合物进行体外抗肿瘤细胞活性试验。结果表明:从澳大利亚厚皮海绵分离得到的2个化合物分别为Aldisin和2-Bromoaldisin;体外抗肿瘤细胞活性试验显示,化合物Aldisin和2-Bromoaldisin对人克隆结肠腺癌细胞(Caco-2)、人结肠癌细胞(HCT116)、人肝癌细胞(7721)、人胶质瘤细胞(U251)和人肾癌细胞(A498)均具有抑制活性的作用,其中化合物Aldisin处理7721细胞的IC50为(67.56±3.06)μg/m L,抑制作用显著。研究表明,两种化合物属于天然产物,可作为潜在的抗肿瘤药物进行进一步研究。

Isolation,identification and anti-tumor activity of constituents from sponge Craniella australiensis

Two compounds were isolated from sponge Craniella australiensis by column chromatography on silica gel and gel filtration chromatography, and identified by spectroscopic analysis and physical-chemistry property to eval-uate the application of the sponge in preparation of marine drugs. The inhibition on tumor cells of both extracts from the sponge was evaluated by CCK-8 assay. The results showed that the two compounds were identified as Aldisin and 2-Bromoaldisin which exhibited the potent inhibitory activities against Caco-2 , HCT116 , 7721 , U251 and A495 cells in human. The Aldisin showed the strongest cytotoxic activity against 7221 cell with IC50(67. 56±3. 06)μg/mL. The findings indicate that the extracts as natural products are considered as a potential anti-tumor candi-date for further study.