S-15183a and b, New Sphingosine Kinase Inhibitors, Produced by a Fungus.

DOI PubMed 被引用文献2件 参考文献30件
  • KONO KEITA
    Pharmacology and Molecular Biology Research Laboratories, Research Institute, Sankyo Co., Ltd.
  • TANAKA MASAHIRO
    Exploratory Chemistry Research Laboratories, Research Institute, Sankyo Co., Ltd.
  • ONO YASUNORI
    Lead Discovery Research Laboratories, Research Institute, Sankyo Co., Ltd.
  • HOSOYA TSUYOSHI
    Lead Discovery Research Laboratories, Research Institute, Sankyo Co., Ltd.
  • OGITA TAKESHI
    Drug Metabolism and Pharmacokinetics Research Laboratories, Research Institute, Sankyo Co., Ltd.
  • KOHAMA TAKAFUMI
    Pharmacology and Molecular Biology Research Laboratories, Research Institute, Sankyo Co., Ltd.

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In the course of our screening for inhibitors of sphingosine kinase, we found two active compounds in a culture broth of a fungus, Zopfiella inermis SANK 15183. The structures of the compounds, named S-15183a and b, were elucidated by a combination of spectroscopic analyses to be new azaphilone-type metabolites. S-15183a and b inhibited sphingosine kinase from rat liver with IC50 values of 2.5 and 1.6μM, respectively. S-15183a also inhibited endogenous SPH kinase activity in intact platelets.

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