Thiodiketopiperazines Produced by the Endophytic Fungus Epicoccum nigrum
Thiodiketopiperazines Produced by the Endophytic Fungus Epicoccum nigrum
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DOI：
10.1021/np1000895
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发表时间：
2010-07-01
影响因子：
5.1
通讯作者：
Du, Dan
中科院分区：
文献类型：
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作者：
Wang, Jia-Ming;Ding, Guang-Zhi;Du, Dan
从内生真菌Epicoccum nigram中分离得到13个新的硫代二酮哌嗪类化合物epicoccin I（1）、ent-epicoccin G（2）和epicoccin J-T（3-13），以及6个已知的二酮哌嗪类化合物Epicoccum nigram（14-19）。化合物1、2和10的结构经X射线晶体学确证，化合物2、4、6和8的绝对构型用Moshers方法确定。化合物2、6、12和17在体外对血小板活化因子诱导的大鼠多形核白细胞中β-葡萄糖醛酸酶的释放显示出有效的活性，IC 50值分别为3.07、4.16、4.95和1.98 μ M。在MTT试验中，19种化合物中没有一种对六种肿瘤细胞系（A549、Bc-17402、BGC-823、HCT-116和A2780）表现出可检测的细胞毒活性。
Thirteen new thiodiketopiperazines, epicoccin I (1), ent-epicoccin G (2), and epicoccins J-T (3-13), together with six known diketopiperazines (14-19), have been isolated from the endophytic fungus Epicoccum nigram. The structures of 1, 2, and 10 were confirmed by X-ray crystallography, and the absolute configurations of 2, 4, 6, and 8 were assigned using Moshers' method. Compounds 2, 6, 12, and 17 showed potent activities in vitro against the release of beta-glucuronidase in rat polymorphonuclear leukocytes induced by platelet-activating factor, with IC50 values of 3.07, 4.16, 4.95, and 1.98 mu M, respectively. None of the 19 compounds exhibited detectable cytotoxic activities toward six tumor cell lines (A549, Bc-17402, BGC-823, HCT-116, and A2780) in the MTT assay.