BIOMAT Database Logo BIOMAT Database Logo

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. 1995

Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.

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 0.03 microgram/ml. WS75624 A and B also showed other metalloprotease (collagenase and neutral endopeptidase) inhibitory activity with IC50 values of 1 microgram/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.

UI MeSH Term Description Entries
D008297 Male Males
D008666 Metalloendopeptidases ENDOPEPTIDASES which use a metal such as ZINC in the catalytic mechanism. Metallo-Endoproteinases,Metalloendopeptidase
D008826 Microbial Sensitivity Tests Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D011725 Pyridines Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
D002417 Cattle Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor. Beef Cow,Bos grunniens,Bos indicus,Bos indicus Cattle,Bos taurus,Cow,Cow, Domestic,Dairy Cow,Holstein Cow,Indicine Cattle,Taurine Cattle,Taurus Cattle,Yak,Zebu,Beef Cows,Bos indicus Cattles,Cattle, Bos indicus,Cattle, Indicine,Cattle, Taurine,Cattle, Taurus,Cattles, Bos indicus,Cattles, Indicine,Cattles, Taurine,Cattles, Taurus,Cow, Beef,Cow, Dairy,Cow, Holstein,Cows,Dairy Cows,Domestic Cow,Domestic Cows,Indicine Cattles,Taurine Cattles,Taurus Cattles,Yaks,Zebus
D005285 Fermentation Anaerobic degradation of GLUCOSE or other organic nutrients to gain energy in the form of ATP. End products vary depending on organisms, substrates, and enzymatic pathways. Common fermentation products include ETHANOL and LACTIC ACID. Fermentations
D000072396 Endothelin-Converting Enzymes Metalloendopeptidases which convert BIG ENDOTHELIN to ENDOTHELIN-1. ECE-1beta,Endothelin Converting Enzyme,Endothelin Converting Enzyme-1a,Endothelin-Converting Enzyme,Endothelin-Converting Enzyme 1,Endothelin-Converting Enzyme 2,Endothelin-Converting Enzyme II,Endothelin-Converting Enzyme-1b,Endothelin-Converting Metalloprotease 2,Metalloprotease ECE-2,ECE-2, Metalloprotease,Endothelin Converting Enzyme 1,Endothelin Converting Enzyme 1a,Endothelin Converting Enzyme 1b,Endothelin Converting Enzyme 2,Endothelin Converting Enzyme II,Endothelin Converting Enzymes,Endothelin Converting Metalloprotease 2,Metalloprotease ECE 2
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013552 Swine Any of various animals that constitute the family Suidae and comprise stout-bodied, short-legged omnivorous mammals with thick skin, usually covered with coarse bristles, a rather long mobile snout, and small tail. Included are the genera Babyrousa, Phacochoerus (wart hogs), and Sus, the latter containing the domestic pig (see SUS SCROFA). Phacochoerus,Pigs,Suidae,Warthogs,Wart Hogs,Hog, Wart,Hogs, Wart,Wart Hog
D013844 Thiazoles Heterocyclic compounds where the ring system is composed of three CARBON atoms, a SULFUR and NITROGEN atoms. Thiazole

Related Publications

Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
WS79089A, B and C, new endothelin converting enzyme inhibitors isolated from Streptosporangium roseum. No. 79089. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
June 1994, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
WS009 A and B, new endothelin receptor antagonists isolated from Streptomyces sp. no. 89009. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
July 1992, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
January 1992, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
New dithiolopyrrolone antibiotics from Saccharothrix sp. SA 233. I. Taxonomy, fermentation, isolation and biological activities.
August 2002, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
WS-7528, a new isoflavanone with estrogen activity isolated from Streptomyces sp. No. 7528. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
November 1990, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
A new antimitotic substance, FR182877. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
February 2000, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
Micacocidin A, B and C, novel antimycoplasma agents from Pseudomonas sp. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
March 1998, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
WS9326A, a novel tachykinin antagonist isolated from Streptomyces violaceusniger no. 9326. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
July 1992, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
Studies on new antibiotics SF2415. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
June 1987, The Journal of antibiotics,
Y Tsurumi, and H Ueda, and K Hayashi, and S Takase, and M Nishikawa, and S Kiyoto, and M Okuhara
YM-47141 and 47142, new elastase inhibitors produced by Flexibacter sp. Q17897. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.
December 1995, The Journal of antibiotics,
Copied contents to your clipboard!