WS009 A和B，从链霉菌属89009号菌株中分离出的新型内皮素受体拮抗剂。I. 分类学、发酵、分离、理化性质及生物活性。
WS009 A and B, new endothelin receptor antagonists isolated from Streptomyces sp. no. 89009. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
作者信息
Miyata S, Ohhata N, Murai H, Masui Y, Ezaki M, Takase S, Nishikawa M, Kiyoto S, Okuhara M, Kohsaka M
机构信息
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
出版信息
J Antibiot (Tokyo). 1992 Jul;45(7):1029-40. doi: 10.7164/antibiotics.45.1029.
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.
新型内皮素受体拮抗剂WS009 A和B是从链霉菌属89009号菌株的发酵液中分离得到的。这些拮抗剂先通过Diaion SP - 207、DEAE Toyopearl柱色谱法以及高效液相色谱法从培养滤液中进行纯化。在一项内皮素受体结合试验中，WS009 A和B表现出选择性活性，其半数抑制浓度（IC50）分别为5.8×10⁻⁶ M和6.7×10⁻⁷ M。基于光谱和化学证据，WS009 A和B的结构已确定为1和3，且为高度羟基化的苯并[a]蒽醌发色团。
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