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 activi...

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Published in:Journal of antibiotics 1992/07/25, Vol.45(7), pp.1029-1040
Main Authors: MIYATA, SUSUMU, OHHATA, NOBUTAKA, MURAI, HIDETUGU, MASUI, YUKO, EZAKI, MASAMI, TAKASE, SHIGEHIRO, NISHIKAWA, MOTOAKI, KIYOTO, SUMIO, OKUHARA, MASAKUNI, KOHSAKA, MASANOBU
Format: Article
Language:English
Subjects:
Anthraquinones - chemistry
Anthraquinones - classification
Anthraquinones - isolation & purification
Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents
Applied microbiology
Biological and medical sciences
Chemotherapic agents
Endothelins - metabolism
Fermentation
Fundamental and applied biological sciences. Psychology
Magnetic Resonance Spectroscopy
Methods
Microbiology
Receptors, Cell Surface - antagonists & inhibitors
Receptors, Endothelin
Streptomyces
Streptomyces - metabolism
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Summary: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 × 10-6M and 6.7 × 10-7M, 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.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.45.1029