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Arisugacins A and B, Novel and Selective Acetylcholinesterase Inhibitors from Penicillium sp. FO-4259. I. Screening, Taxonomy, Fermentation, Isolation and Biological Activity.
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- KUNO FUMIYOSHI
- Research Center for Biological Function, The Kitasato Institute
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- OTOGURO KAZUHIKO
- Research Center for Biological Function, The Kitasato Institute
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- SHIOMI KAZURO
- Research Center for Biological Function, The Kitasato Institute
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- IWAI YUZURU
- Research Center for Biological Function, The Kitasato Institute
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- OMURA SATOSHI
- Research Center for Biological Function, The Kitasato Institute
Bibliographic Information
- Other Title
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- I. Screening, Taxonomy, Fermentation, Isolation and Biological Activity
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Description
An in vitro screening method for selective acetylcholinesterase (AChE) inhibitors was established. Inhibitory activity of AChE and butyrylcholinesterase (BuChE) was measured and the culture broths of microorganisms that showed selective inhibition against AChE were characterized.<br>By using this method, a strain producing the novel and selective inhibitors of AChE, arisugacins A and B, was picked out among over seven thousand microorganisms tested. Arisugacins were obtained as white powders from the culture broth together with three known compounds, territrems B and C and cyclopenin that also showed selective inhibition against AChE. Arisugacins and territrems are members of the meroterpenoid compounds. They showed potent inhibitory activities against AChE with IC50 values in range of 1.0-25.8nM. Furthermore, they showed greater than 2, 000-fold more potent inhibition against AChE than BuChE.
Journal
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- The Journal of Antibiotics
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The Journal of Antibiotics 49 (8), 742-747, 1996
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
