title: Arisugacins C and D, novel acetylcholinesterase inhibitors and their related novel metabolites produced by Penicilium sp. FO-4259-11.
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.
authors.affiliation: Research Center for Biological Function, The Kitasato Institute, Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Otoguro
authors.forename: K
authors.initials: K
authors.lastname: Shiomi
authors.forename: Y
authors.initials: Y
authors.lastname: Yamaguchi
authors.forename: N
authors.initials: N
authors.lastname: Arai
authors.forename: T
authors.initials: T
authors.lastname: Sunazuka
authors.forename: R
authors.initials: R
authors.lastname: Masuma
authors.forename: Y
authors.initials: Y
authors.lastname: Iwai
authors.forename: S
authors.initials: S
authors.lastname: Omura
mesh_terms: D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000302:isolation & purification* / Q000378:metabolism; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010407:Penicillium; D011714:Pyrans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002800:Cholinesterase Inhibitors; D011714:Pyrans; C095353:arisugacin; C040405:territrem B