F-12509A, a new sphingosine kinase inhibitor, produced by a discomycete

Citation
K. Kono et al., F-12509A, a new sphingosine kinase inhibitor, produced by a discomycete, J ANTIBIOT, 53(5), 2000, pp. 459-466
Citations number
26
Categorie Soggetti
Microbiology
Journal title
JOURNAL OF ANTIBIOTICS
ISSN journal
00218820 → ACNP
Volume
53
Issue
5
Year of publication
2000
Pages
459 - 466
Database
ISI
SICI code
0021-8820(200005)53:5<459:FANSKI>2.0.ZU;2-O
Abstract
In the course of our screening for inhibitors of sphingosine kinase, we fou nd an active compound from a culture broth of a discomycete, Trichopezizell a barbata SANK 25395. The structure of the compound, named F-12509A, was el ucidated by a combination of spectroscopic analyses, to be a new sesquiterp ene quinone consisting of a drimane moiety and a dihydroxybenzoquinone. Enz yme kinetic analyses showed that F-12509A inhibits sphingosine kinase activ ity in a competitive manner with respect to sphingosine, with a K-i value o f 18 mu M.