Epohelmins A and B, novel lanosterol synthase inhibitors from a fungal strain FKI-0929.
Epohelmins A and B, novel lanosterol synthase inhibitors from a fungal strain FKI-0929.
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DOI：
10.7164/antibiotics.57.564
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发表时间：
2004-09
期刊：
影响因子：
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通讯作者：
Y. Sakano;M. Shibuya;Y. Yamaguchi;R. Masuma;H. Tomoda;S. Ōmura;Y. Ebizuka
中科院分区：
文献类型：
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作者：
Y. Sakano;M. Shibuya;Y. Yamaguchi;R. Masuma;H. Tomoda;S. Ōmura;Y. Ebizuka
从真菌菌株 FKI-0929 中分离出两种化合物，命名为 epohelmins A 和 B，作为新的天然产物，对重组人羊毛甾醇合酶具有抑制活性。通过硅胶柱色谱和HPLC对该菌株的全肉汤的粗提物进行分级，得到两种分离的抑制剂。详细的光谱分析确定了它们的结构。它们是4,5-环氧-2-(4'-oxoundec-(5'E)-烯基)-七亚甲基胺的非对映异构体，并且其相对立体化学构型对于依波黑明A确定为(2R，4R，5R)或(2S，4S，5S)，对于依波黑明B确定为(2R，4S，5R)或(2S，4R，5S)，分别。这些化合物抑制重组人羊毛甾醇合酶，IC50 值分别为 10 和 6.0 microM。
From a fungal strain FKI-0929, two compounds designated epohelmins A and B, were isolated as new natural products with inhibitory activity against recombinant human lanosterol synthase. The crude extract from the whole broth of this strain was fractionated by silica gel column chromatography and HPLC to afford two isolated inhibitors. Detailed spectroscopic analyses led to the identification of their structures. They are diastereomers of 4,5-epoxy-2-(4'-oxoundec-(5'E)-enyl)-heptamethylenamines, and their relative stereochemical configurations were determined as (2R, 4R, 5R) or (2S, 4S, 5S) for epohelmin A, and (2R, 4S, 5R) or (2S, 4R, 5S) for epohelmin B, respectively. These compounds inhibited recombinant human lanosterol synthase with IC50 values of 10 and 6.0 microM, respectively.