Protective effect of eurystatins A and B, new prolyl endopeptidase inhibitors, on scopolamine-induced amnesia in rats.

Abstract

Eurystatins A and B, which are produced by Streptomyces eurythermus R353-21, potently inhibited Flavobacterium prolyl endopeptidase (PED) with IC50 values of 0.004 and 0.002 micrograms/ml, respectively, while no inhibition was observed against another 5 proteases, even at 100 micrograms/ml. The protective effect of eurystatins A and B against scopolamine (3 mg/kg, i.p.)-induced amnesia in rats was evaluated by the step-through one-trial passive avoidance method. When administered i.p. 30 min prior to the acquisition trial, both eurystatins A, at 2-8 mg/kg, and B, at 4-8 mg/kg, significantly protected rats from the amnesic effect of scopolamine without behavioral side effects.

• Authors: H Kamei, T Ueki, Y Obi, Y Fukagawa, T Oki
• Journal: Japanese journal of pharmacology (Jpn J Pharmacol) Vol. 60 Issue 4 Pg. 377-80 (Dec 1992) ISSN: 0021-5198 [Print] Japan
• PMID: 1287273 (Publication Type: Journal Article)

Chemical References

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

Topics

• Amino Acid Sequence
• Amnesia (chemically induced)
• Animals
• Avoidance Learning (drug effects)
• Dose-Response Relationship, Drug
• Flavobacterium (drug effects, enzymology)
• Molecular Sequence Data
• Peptides, Cyclic (pharmacology)
• Prolyl Oligopeptidases
• Rats
• Scopolamine (antagonists & inhibitors, pharmacology)
• Serine Endopeptidases (metabolism)
• Serine Proteinase Inhibitors (pharmacology)