Arisugacins A and B, Novel and Selective Acetylcholinesterase Inhibitors from Penicillium sp. FO-4259. I. Screening, Taxonomy, Fermentation, Isolation and Biological Activity.

KUNO FUMIYOSHI, OTOGURO KAZUHIKO, SHIOMI KAZURO, IWAI YUZURU, OMURA SATOSHI

doi:10.7164/antibiotics.49.742

Arisugacins A and B, Novel and Selective Acetylcholinesterase Inhibitors from Penicillium sp. FO-4259. I. Screening, Taxonomy, Fermentation, Isolation and Biological Activity.

DOI PubMed 被引用文献3件

KUNO FUMIYOSHI

Research Center for Biological Function, The Kitasato Institute
OTOGURO KAZUHIKO

Research Center for Biological Function, The Kitasato Institute
SHIOMI KAZURO

Research Center for Biological Function, The Kitasato Institute
IWAI YUZURU

Research Center for Biological Function, The Kitasato Institute
OMURA SATOSHI

Research Center for Biological Function, The Kitasato Institute

書誌事項

タイトル別名

I. Screening, Taxonomy, Fermentation, Isolation and Biological Activity

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説明

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.