WS75624 A and B, New Endothelin Converting Enzyme Inhibitors Isolated from Saccharothrix sp. No. 75624 I. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Biological Activities
Novel endothelin converting enzyme (ECE) inhibitors, WS75624 A and B, have been isolated from the fermentation broth of Saccharothrix sp. No. 75624. These inhibitors were purified from an acetone extract of whole culture broth followed by HP-20 column chromatography, silica gel column chromatography...
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Published in | Journal of antibiotics Vol. 48; no. 10; pp. 1066 - 1072 |
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Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
Published |
Tokyo
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
1995
Japan Antibiotics Research Association |
Subjects | |
Online Access | Get full text |
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Summary: | Novel endothelin converting enzyme (ECE) inhibitors, WS75624 A and B, have been isolated from the fermentation broth of Saccharothrix sp. No. 75624. These inhibitors were purified from an acetone extract of whole culture broth followed by HP-20 column chromatography, silica gel column chromatography and HPLC. WS75624 A and B showed highly potent ECE inhibitory activity, and both had IC50 values of 0.03μg/ml. WS75624 A and B also showed other metalloprotease (collagenase and neutral endopeptidase) inhibitory activity with IC50 values of 1 μg/ml. Since large amount of WS75624 B was isolated, we tried in vivo evaluation using WS75624 B. WS75624 B inhibited big endothelin-induced pressor effect when administered to SD rat intravenously with big ET-1. |
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Bibliography: | ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 content type line 23 ObjectType-Article-1 ObjectType-Feature-2 |
ISSN: | 0021-8820 1881-1469 |
DOI: | 10.7164/antibiotics.48.1066 |