WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
WS-7338 A, B, C and D, novel endothelin receptor antagonists, have been isolated from fermentation broth of Streptomyces sp. No. 7338. These antagonists were purified from the culture mycelium by extraction with acetone, followed by carbon column chromatography and HPLC. Among them, WS-7338 B showed good activity in an endothelin receptor binding assay with an IC50 of 2.7 x 10(-7) M.
Miyata
S
S
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
Hashimoto
M
M
Masui
Y
Y
Ezaki
M
M
Takase
S
S
Nishikawa
M
M
Kiyoto
S
S
Okuhara
M
M
Kohsaka
M
M
D000595:Amino Acid Sequence; D000818:Animals; D001011:Aorta; D001419:Bacteria / Q000187:drug effects; D002845:Chromatography; D016232:Endothelins / Q000378:metabolism*; D004730:Endothelium, Vascular / Q000378:metabolism*; D005285:Fermentation; D005658:Fungi / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D009682:Magnetic Resonance Spectroscopy; D008855:Microscopy, Electron, Scanning; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic / Q000096:biosynthesis / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors*; D017466:Receptors, Endothelin; D012995:Solubility; D013302:Streptomyces / Q000145:classification / Q000378:metabolism* / Q000648:ultrastructure; D013552:Swine
D016232:Endothelins; D010456:Peptides, Cyclic; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; C072732:cyclo(valyl-leucyl-tryptophyl-glutamyl-alanyl); C069764:cyclo(glutamyl-alanyl-isoleucyl-leucyl-tryptophyl); C073559:cyclo(leucyl-leucyl-tryptophyl-glutamyl-alanyl); C073560:cyclo(valyl-valyl-tryptophyl-glutamyl-alanyl)