Arisugacins C and D, novel acetylcholinesterase inhibitors and their related novel metabolites produced by Penicillium sp FO-4259-11
Arisugacins C and D, novel acetylcholinesterase inhibitors and their related novel metabolites produced by Penicillium sp FO-4259-11
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DOI：
10.7164/antibiotics.53.50
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发表时间：
2000-01-01
影响因子：
3.3
通讯作者：
Omura, S
中科院分区：
文献类型：
--
作者：
Otoguro, K;Shiomi, K;Omura, S
从青霉菌突变株FO-4259中分离出一系列代谢产物，分别命名为亚芥子素A、B的代谢物C、D、E、E、G和H，与亚芥子素A、B具有结构上的相似性。对乙酰胆碱酯酶（AChE）的IC50值分别为2.5 μ M和3.5 μ M。而亚芥子素El F、G和H在I OD μ m下对AChE没有抑制作用，虽然与亚芥子素A和B相比，它们对AChE的抑制作用较弱或无抑制作用，但它们可能为研究其构效关系提供了有益的依据。
The mutant of Penicillium sp. FO-4259, an arisugacins A and B producing strain, was found to produce a series of metabolites, designated arisugacins C, D, E, E G and H, which were structurally related to arisugacins A and B. These compounds were isolated from the culture broth and the physico-chemical and biological properties were examined. The IC50 values of arisugacins C and D against acetylcholinesterase (AChE) were 2.5 mu M and 3.5 mu M, respectively. However arisugacins El F, G and H did not inhibit AChE at I OD mu M. Though they showed only weak or no activity against AChE compared with arisugacins A and B, they may be useful for the study of the structure-activity relationship.