title: ApoE secretion modulating bromotyrosine derivative from the Australian marine sponge Callyspongia sp.
abstract: High throughput screening of a pre-fractionated natural product library identified 11 active fractions showing ApoE modulation activity. Mass-directed fractionation of one active crude extract from the Australian marine sponge Callyspongia sp. resulted in the isolation of 13 metabolites, including three new bromotyrosine derivatives, callyspongic acid (1), 3,5-dibromo-4-methoxyphenylpyruvic acid (2), N-acetyl-3-bromo-4-hydroxylphenylethamine (3), and ten known compounds (4-13). The structure elucidation of compounds 1-3 was based on their 1D and 2D NMR and MS spectroscopic data. 3,5-Dibromo-4-methoxyphenylpyruvic acid (2) showed weak activity in increasing the apolipoprotein E secretion from human CCF-STTG1 cells at the concentration of 40 μM.
authors.affiliation: Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Li-Wen
authors.initials: LW
authors.lastname: Tian
authors.affiliation: Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Yunjiang
authors.initials: Y
authors.lastname: Feng
authors.affiliation: Centre for Drug Research and Development, Vancouver, BC V6T 1Z3, Canada.
authors.forename: Yoko
authors.initials: Y
authors.lastname: Shimizu
authors.affiliation: Centre for Drug Research and Development, Vancouver, BC V6T 1Z3, Canada.
authors.forename: Tom A
authors.initials: TA
authors.lastname: Pfeifer
authors.affiliation: Department of Pathology and Laboratory Medicine, University of British Columbia, Vancouver, BC V6T 1Z4, Canada.
authors.forename: Cheryl
authors.initials: C
authors.lastname: Wellington
authors.affiliation: Queensland Museum, South Brisbane, QLD 4101, Australia.
authors.forename: John N A
authors.initials: JN
authors.lastname: Hooper
authors.affiliation: Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia. Electronic address: r.quinn@griffith.edu.au.
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Quinn
mesh_terms: D000818:Animals; D001057:Apolipoproteins E / Q000378:metabolism*; D001315:Australia; D047128:Callyspongia / Q000737:chemistry* / Q000378:metabolism; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
chemical_list: D001057:Apolipoproteins E; C475724:bromotyrosine; D014443:Tyrosine
keywords: ApoE modulation activity; Bastadin; Bromotyrosine derivatives; Callyspongia sp.