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首页> 外文期刊>The Journal of Antibiotics: An International Journal >F-12509A,a New Sphingosine Kinase Inhibitor, Produced by a Discomycete
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F-12509A,a New Sphingosine Kinase Inhibitor, Produced by a Discomycete

机译:F-12509A,一种新的鞘氨醇激酶抑制剂,由Discomycete生产

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摘要

In the course of our screening for inhibitors of sphingosine kinase, we found an active compound from a culture broth of a discomycete, Trichopezizella barbata SANK 25395. The structure of the compound, named F-12509A, was elucidated by a combination of spectroscopic analyses, to be a new sesquiterpene quinone consisting of a drimane moiety and a dihydroxybenzoquinone. Enzyme kinetic analyses showed that F-12509A inhibits sphingosine kinase activity in a competitive manner with respect to sphingosine, with a K_i value of 18 #mu#M.
机译:在筛选鞘氨醇激酶抑制剂的过程中,我们从圆盘菌Tribatpezizella barbata SANK 25395的培养液中发现了一种活性化合物。该化合物的结构F-12509A通过光谱分析的组合得以阐明,成为一种新的倍半萜醌,它由drimane部分和二羟基苯醌组成。酶动力学分析表明,F-12509A以相对于鞘氨醇竞争的方式抑制鞘氨醇激酶活性,K_i值为18#mu#M。

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