FR-901367

WS009 A and B novel endothelin receptor antagonists, have been isolated from the fermentation broth of Streptomyces sp. No. 89009. These antagonists were purified from the culture filtrate followed by Diaion SP-207, DEAE Toyopearl column chromatography and HPLC. WS009 A and B showed selective activity in an endothelin receptor binding assay with IC50 of 5.8 x 10(-6) M and 6.7 x 10(-7) M, respectively. On the basis of spectroscopic and chemical evidence, the structures of WS009 A and B have been established as 1 and 3, and are highly hydroxylated benz[a]anthraquinone chromophores.

A review.With the development of mol. biol., enzymol., pharmacol. and immunol., and the diversification of mol. screening, the research on searching for receptor antagonists from the secondary-metabolites of microorganisms has been gradually advanced since 1990s.The studies on seventeen kinds of receptor antagonists from microorganisms, including those affecting blood pressure, formation of thrombus, secretion of sex hormone, occurrence of inflammation, function of neural system etc. are summarized.The structures, sources and main bioactivities of endothelin receptor antagonists from microorganisms are particularly reviewed with 21 references