Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 15, Pages 3537-3540Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.05.054
Keywords
Callyspongia sp.; Bromotyrosine derivatives; Bastadin; ApoE modulation activity
Categories
Funding
- Queensland Government Smart Futures NIRAP Program
- Australian Research Council for NMR and MS equipment [LE0668477, LE0237908]
- Alzheimer's Drug Discovery Foundation
- Centre for Drug Research and Development (Vancouver, Canada)
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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 mu M. (C) 2014 The Authors. Published by Elsevier Ltd.
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