title: Acetylcholinesterase inhibitors from a marine fungus Talaromyces sp. strain LF458.
abstract: Two new oxaphenalenone dimers, talaromycesone A (1) and talaromycesone B (2), and a new isopentenyl xanthenone, talaroxanthenone (3), together with six known diphenyl ether derivatives, e.g., Δ(1',3'),-1'-dehydroxypenicillide (4), 1',2'-dehydropenicillide (5), vermixocin A (6), vermixocin B (7), 3'-methoxy-1'2'-dehydropenicillide (8), and AS-186c (9), were isolated from the culture broth and mycelia of a marine fungus Talaromyces sp. strain LF458. Compound 2 represents the first example of 1-nor oxaphenalenone dimer carbon skeleton. All isolated compounds were subjected to bioactivity assays. Compounds 1, 2, and 9 exhibited potent antibacterial activities with IC50 3.70, 17.36, and 1.34 μM, respectively, against human pathogenic Staphylococcus strains. Compounds 1, 3, and 9 displayed potent acetylcholinesterase inhibitory activities with IC50 7.49, 1.61, and 2.60 μM, respectively. Interestingly, phosphodiesterase PDE-4B2 was inhibited by compounds 3 (IC50 7.25 μM) and 9 (IC50 2.63 μM).
authors.affiliation: Wirkstoff-Zentrum am GEOMAR Helmholtz-Zentrum für Ozeanforschung Kiel, Kiel, 24105, Germany.
authors.forename: Bin
authors.initials: B
authors.lastname: Wu
authors.forename: Birgit
authors.initials: B
authors.lastname: Ohlendorf
authors.forename: Vanessa
authors.initials: V
authors.lastname: Oesker
authors.forename: Jutta
authors.initials: J
authors.lastname: Wiese
authors.forename: Susann
authors.initials: S
authors.lastname: Malien
authors.forename: Rolf
authors.initials: R
authors.lastname: Schmaljohann
authors.forename: Johannes F
authors.initials: JF
authors.lastname: Imhoff
mesh_terms: D000900:Anti-Bacterial Agents / Q000032:analysis / Q000302:isolation & purification* / Q000494:pharmacology; D002800:Cholinesterase Inhibitors / Q000032:analysis / Q000302:isolation & purification*; D002851:Chromatography, High Pressure Liquid; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D058988:Phosphodiesterase 4 Inhibitors; D013055:Spectrophotometry, Infrared; D013210:Staphylococcus / Q000187:drug effects; D032901:Talaromyces / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D002800:Cholinesterase Inhibitors; D058988:Phosphodiesterase 4 Inhibitors
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