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

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...

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Veröffentlicht in:	Journal of antibiotics 2001/05/25, Vol.54(5), pp.415-420
Hauptverfasser:	KONO, KEITA, TANAKA, MASAHIRO, ONO, YASUNORI, HOSOYA, TSUYOSHI, OGITA, TAKESHI, KOHAMA, TAKAFUMI
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics (antibacterial agents, antifungal agents) Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents Applied microbiology Biological and medical sciences Blood Platelets - drug effects Blood Platelets - enzymology Cell-Free System Enzyme Inhibitors - chemistry Enzyme Inhibitors - isolation & purification Enzyme Inhibitors - pharmacology Fermentation Fundamental and applied biological sciences. Psychology Humans Hydrogenation Magnetic Resonance Spectroscopy Microbiology Mitosporic Fungi - chemistry Mitosporic Fungi - growth & development Mitosporic Fungi - metabolism Phosphotransferases (Alcohol Group Acceptor) - antagonists & inhibitors Spectrometry, Mass, Fast Atom Bombardment Sphingosine - analogs & derivatives Sphingosine - chemistry Sphingosine - isolation & purification Sphingosine - pharmacology Substrate Specificity
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Zusammenfassung:	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.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.54.415