WS009 A and B, new endothelin receptor antagonists isolated from Streptomyces sp. no. 89009. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
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.
Miyata
S
S
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
Ohhata
N
N
Murai
H
H
Masui
Y
Y
Ezaki
M
M
Takase
S
S
Nishikawa
M
M
Kiyoto
S
S
Okuhara
M
M
Kohsaka
M
M
D000880:Anthraquinones / Q000737:chemistry / Q000145:classification / Q000302:isolation & purification*; D016232:Endothelins / Q000378:metabolism*; D005285:Fermentation; D009682:Magnetic Resonance Spectroscopy; D008722:Methods; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors*; D017466:Receptors, Endothelin; D013302:Streptomyces / Q000378:metabolism*
D000880:Anthraquinones; D016232:Endothelins; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; C076466:WS 009A; C076467:WS 009B