Eurystatins A and B, new prolyl endopeptidase inhibitors. I. Taxonomy, production, isolation and biological activities

S Toda; Y Obi; K Numata; Y Hamagishi; K Tomita; N Komiyama; C Kotake; T Furumai; T Oki

doi:10.7164/antibiotics.45.1573

Eurystatins A and B, new prolyl endopeptidase inhibitors. I. Taxonomy, production, isolation and biological activities

J Antibiot (Tokyo). 1992 Oct;45(10):1573-9. doi: 10.7164/antibiotics.45.1573.

Authors

S Toda¹, Y Obi, K Numata, Y Hamagishi, K Tomita, N Komiyama, C Kotake, T Furumai, T Oki

Affiliation

¹ Bristol-Myers Squibb Research Institute, Tokyo, Japan.

PMID: 1473984
DOI: 10.7164/antibiotics.45.1573

Abstract

Eurystatins A and B, were isolated from the cultured broth of Streptomyces eurythermus R353-21. They showed specific and potent inhibitory activity against prolyl endopeptidase and did not show antimicrobial activity. No lethal toxicity was observed for the two compounds after ip administration in mice at 200 mg/kg.

MeSH terms

Animals
Brain / drug effects
Brain / enzymology
Chromatography, Gel
Chromatography, High Pressure Liquid
Flavobacterium / drug effects
Flavobacterium / enzymology
Male
Mice
Mice, Inbred ICR
Microbial Sensitivity Tests
Microbiological Techniques
Peptides, Cyclic / chemistry
Peptides, Cyclic / isolation & purification
Peptides, Cyclic / pharmacology*
Prolyl Oligopeptidases
Rabbits
Serine Endopeptidases / chemistry
Serine Endopeptidases / isolation & purification
Serine Endopeptidases / metabolism*
Serine Proteinase Inhibitors / chemistry
Serine Proteinase Inhibitors / isolation & purification
Serine Proteinase Inhibitors / metabolism*
Streptomyces* / chemistry
Streptomyces* / classification

Substances

Peptides, Cyclic
Serine Proteinase Inhibitors
eurystatin A
eurystatin B
Serine Endopeptidases
Prolyl Oligopeptidases