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海绵素 J,一种来自海洋海绵 Theonella swinhoei 的有效细胞毒素。

Swinholide J, a potent cytotoxin from the marine sponge Theonella swinhoei.

机构信息

Department of Chemistry of Natural Compounds, University of Naples, "Federico II", via D. Montesano 49, 80131 Napoli, Italy.

Natural Substances Institute, la Terrasse Street, 91198 Gif sur Yvette Cedex, France.

出版信息

Mar Drugs. 2011;9(6):1133-1141. doi: 10.3390/md9061133. Epub 2011 Jun 22.

Abstract

In our ongoing search for new pharmacologically active leads from Solomon organisms, we have examined the sponge Theonella swinhoei. Herein we report the isolation and structure elucidation of swinholide A (1) and one new macrolide, swinholide J (2). Swinholide J is an unprecedented asymmetric 44-membered dilactone with an epoxide functionality in half of the molecule. The structural determination was based on extensive interpretation of high-field NMR spectra and HRESIMS data. Swinholide J displayed potent in vitro cytotoxicity against KB cells (human nasopharynx cancer) with an IC(50) value of 6 nM.

摘要

在我们不断从 Solomon 生物体中寻找新的具有药理活性的先导化合物的过程中,我们研究了海绵 Theonella swinhoei。本文报道了 swinholide A(1)和一种新的大环内酯化合物 swinholide J(2)的分离和结构阐明。Swinholide J 是一种前所未有的不对称 44 元二内酯,分子的一半具有环氧化物官能团。结构测定是基于对高场 NMR 谱和 HRESIMS 数据的广泛解释。Swinholide J 对 KB 细胞(人鼻咽癌细胞)表现出很强的体外细胞毒性,IC50 值为 6 nM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b3/3131564/777bf91414ce/marinedrugs-09-01133f1.jpg

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