Arisugacins C and D, novel acetylcholinesterase inhibitors and their related novel metabolites produced by Penicilium sp. FO-4259-11

J Antibiot (Tokyo). 2000 Jan;53(1):50-7. doi: 10.7164/antibiotics.53.50.

Abstract

The mutant of Penicillium sp. FO-4259, an arisugacins A and B producing strain, was found to produce a series of metabolites, designated arisugacins C, D, E, F, G and H, which were structurally related to arisugacins A and B. These compounds were isolated from the culture broth and the physico-chemical and biological properties were examined. The IC50 values of arisugacins C and D against acetylcholinesterase (AChE) were 2.5 microM and 3.5 microM, respectively. However arisugacins E, F, G and H did not inhibit AChE at 100 microM. Though they showed only weak or no activity against AChE compared with arisugacins A and B, they may be useful for the study of the structure-activity relationship.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cholinesterase Inhibitors / chemistry*
  • Cholinesterase Inhibitors / isolation & purification*
  • Cholinesterase Inhibitors / metabolism
  • Humans
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Penicillium
  • Pyrans / chemistry
  • Pyrans / isolation & purification
  • Pyrans / pharmacology*
  • Structure-Activity Relationship

Substances

  • Cholinesterase Inhibitors
  • Pyrans
  • arisugacin
  • territrem B