An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry) of halistatin 1, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Phakellia carteri. Halistatin 1 (8.8 x 10-7% yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulin.
Halistatin 1 has the following structural formula :
通过对海洋
生物作为新型抗癌药物来源的长期深入研究,我们从西印度洋海绵 Phakellia carteri 中分离并阐明了 halistatin 1 的结构(主要通过高场核磁共振和质谱分析),这是一种新的卤代
吡喃类聚醚大环内酯。Halistatin 1(产率为 8.8 x 10-7%)可导致有丝分裂停止的细胞聚集,抑制微管蛋白聚合,并抑制放射性标记的
长春新碱和 GTP 与微管蛋白的结合。
Halistatin 1 的结构式如下::