Arisugacins, selective acetylcholinesterase inhibitors of microbial origin.

Abstract

Synthetic inhibitors of acetylcholinesterase (AChE) recently have attracted particular attention for treatment of Alzheimer's disease. By systematic screening of microbial metabolites, we were able to discover the new AChE inhibitors, named arisugacins A and B, from the culture broth of Penicillium sp. FO-4259. The structures of arisugacins are members of the meroterpenoid compounds. Arisugacin A is a potent and highly selective inhibitor of AChE but does not inhibit butyrylcholinesterase in vitro. Arisugacin A is a good candidate as an excellent potential drug for treatment of Alzheimer's disease. Also reviewed is the current status of development of antidementia drugs.

• Authors: K Otoguro, F Kuno, S Omura
• Journal: Pharmacology & therapeutics (Pharmacol Ther) 1997 Oct-Dec Vol. 76 Issue 1-3 Pg. 45-54 ISSN: 0163-7258 [Print] England
• PMID: 9535168 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Antipsychotic Agents
• Cholinesterase Inhibitors
• Pyrans
• arisugacin
• Acetylcholinesterase

Topics

• Acetylcholinesterase (drug effects)
• Alzheimer Disease (drug therapy, prevention & control)
• Animals
• Antipsychotic Agents (therapeutic use)
• Cholinesterase Inhibitors (chemistry, isolation & purification, therapeutic use)
• Drug Evaluation
• Drug Evaluation, Preclinical
• Humans
• Penicillium (chemistry)
• Pyrans (chemistry, isolation & purification, therapeutic use)
• Structure-Activity Relationship