Field Jessica J, Singh A Jonathan, Kanakkanthara Arun, Halafihi Tu'ikolongahau, Northcote Peter T, Miller John H
Centre for Biodiscovery, Victoria University of Wellington, P.O. Box 600, Wellington, New Zealand.
J Med Chem. 2009 Nov 26;52(22):7328-32. doi: 10.1021/jm901249g.
Zampanolide (1), a 20-membered macrolide from a Tongan marine sponge, stabilizes microtubules and blocks cells in G(2)/M of the cell cycle. Zampanolide is cytotoxic in the low nanomolar range and induces microtubule bundles in cells. It leads to tubulin assembly in cells and in purified tubulin preparations and is not a substrate for the P-glycoprotein drug efflux pump. Zampanolide, with only four stereogenic centers, may be amenable to large-scale synthetic preparation.
扎马内酯(1)是一种从汤加海洋海绵中提取的20元大环内酯类化合物,它能稳定微管并使细胞周期停滞于G(2)/M期。扎马内酯在低纳摩尔浓度范围内具有细胞毒性,并能在细胞中诱导微管束形成。它能导致细胞内和纯化微管蛋白制剂中的微管蛋白组装,且不是P-糖蛋白药物外排泵的底物。扎马内酯仅含有四个手性中心,或许适合大规模合成制备。