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WS79089A、B和C,从玫瑰链霉菌79089号菌株中分离出的新型内皮素转化酶抑制剂。分类学、发酵、分离、理化性质及生物活性

WS79089A, B and C, new endothelin converting enzyme inhibitors isolated from Streptosporangium roseum. No. 79089. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.

作者信息

Tsurumi Y, Ohhata N, Iwamoto T, Shigematsu N, Sakamoto K, Nishikawa M, Kiyoto S, Okuhara M

机构信息

Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.

出版信息

J Antibiot (Tokyo). 1994 Jun;47(6):619-30. doi: 10.7164/antibiotics.47.619.

Abstract

WS79089A, B and C, which are novel endothelin converting enzyme (ECE) inhibitors have been isolated from the fermentation broth of Streptosporangium roseum No. 79089. These inhibitors were purified from an acetone extract of whole culture broth followed by Silicar CC-4 column chromatography and HPLC. WS79089A, B and C showed highly selective ECE inhibition activity with IC50 values of 0.73 microM 0.14 microM and 3.42 microM, respectively. On the basis of spectroscopic and chemical evidence, the tentative structures of WS79089A, B and C have been proposed, they have benzo[a]naphtacen chromophores.

摘要

WS79089A、B和C是新型内皮素转化酶(ECE)抑制剂,它们是从玫瑰孢链霉菌79089号的发酵液中分离得到的。这些抑制剂是从全培养液的丙酮提取物中纯化出来的,随后进行硅胶CC - 4柱色谱法和高效液相色谱法。WS79089A、B和C表现出高度选择性的ECE抑制活性,其IC50值分别为0.73微摩尔、0.14微摩尔和3.42微摩尔。基于光谱和化学证据,已提出WS79089A、B和C的初步结构,它们具有苯并[a]萘并四苯发色团。

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