Gliotoxin Analogues from a Marine-Derived Fungus, Penicillium sp., and Their Cytotoxic and Histone Methyltransferase Inhibitory Activities
Gliotoxin Analogues from a Marine-Derived Fungus, Penicillium sp., and Their Cytotoxic and Histone Methyltransferase Inhibitory Activities
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DOI：
10.1021/np200740e
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发表时间：
2012-01-01
影响因子：
5.1
通讯作者：
Matsunaga, Shigeki
中科院分区：
文献类型：
--
作者：
Sun, Yi;Takada, Kentaro;Matsunaga, Shigeki
从日本骏河湾深海沉积物中分离到7种胶粘毒素相关化合物。其中包括两种新的代谢产物，双（脱硫基）-10 α-甲硫基-3 α-脱氧-3，3 α-二脱氢胶霉毒素（1）和6-脱氧-5 α，6-二脱氢胶霉毒素（2），以及五种已知代谢产物（3-7）。新化合物的结构通过光谱数据分析和应用改进的Mosher分析进行了鉴定。所有的化合物都表现出细胞毒活性，而含有二硫键的化合物显示出对组蛋白甲基转移酶（HMT）G9 a的有效抑制活性。它们都没有抑制HMT SET 7/9。
Seven gliotoxin-related compounds were isolated from the fungus Penicillium sp. strain JMF034, obtained from deep sea sediments of Suruga Bay, Japan. These included two new metabolites, bis(dethio)-10a-methylthio-3a-deoxy-3,3a-didehydrogliotoxin (1) and 6-deoxy-5a,6-didehydrogliotoxin (2), and five known metabolites (3-7). The structures of the new compounds were elucidated by analysis of spectroscopic data and the application of the modified Mosher's analysis. All of the compounds exhibited cytotoxic activity, whereas compounds containing a disulfide bond showed potent inhibitory activity against histone methyltransferase (HMT) G9a. None of them inhibited HMT SET7/9.