Peloruside E（22-Norpeloruside A），一种来自新西兰海洋海绵 Mycale hentscheli 的 Pelorusane 大环内酯，保留微管稳定特性。
Peloruside E (22-Norpeloruside A), a Pelorusane Macrolide from the New Zealand Marine Sponge Mycale hentscheli, Retains Microtubule-Stabilizing Properties.
机构信息
School of Chemical and Physical Sciences , Victoria University of Wellington , Wellington 6012 , New Zealand.
Centre for Biodiscovery , Victoria University of Wellington , Wellington 6012 , New Zealand.
出版信息
J Nat Prod. 2018 Sep 28;81(9):2125-2128. doi: 10.1021/acs.jnatprod.8b00557. Epub 2018 Sep 6.
A new peloruside congener, peloruside E (5), has been isolated in sub-milligram quantities from a specimen of the New Zealand marine sponge Mycale hentscheli. The structure of 5 differs from the parent compound peloruside A (1) by replacement of the C-10 gem-dimethyl moiety with a monomethyl substituent and represents the first structural deviation in the pelorusane scaffold. Peloruside E (5) is potently antiproliferative (HL-60, IC 90 nM, cf. 1, 19 nM) and polymerizes purified tubulin, albeit at a rate lower than that of 1.
从新西兰海洋海绵 Mycale hentscheli 的标本中以亚毫克级的量分离出了一种新的 peloruside 同系物，peloruside E（5）。结构 5 与母体化合物 peloruside A（1）不同，C-10 位的双甲基取代基被一个单甲基取代基取代，代表了 pelorusane 支架的第一个结构偏差。Peloruside E（5）具有很强的抗增殖活性（HL-60，IC 90 nM，与 1 相比，19 nM），并且聚合纯化的微管蛋白，尽管速度低于 1。
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