Antitrypanosomal Cyclic Polyketide Peroxides from the Australian Marine Sponge Plakortis sp.
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Davis, Rohan A
Sykes, Melissa
Avery, Vicky M
Camp, David
Quinn, Ronald J
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Abstract
Bioassay-guided fractionation of the crude extract from the Australian marine sponge Plakortis sp. led to the isolation of two new cyclic polyketide peroxides, 11,12-didehydro-13-oxo-plakortide Q (1) and 10-carboxy-11,12,13,14-tetranor-plakortide Q (2). Antitrypanosomal studies showed that compound 1 had an IC50 value of 49 nM against Trypanosoma brucei brucei, and compound 2, where a carboxylic acid is present in the side chain, had a 20-fold reduction of activity. 11,12-Didehydro-13-oxo-plakortide Q (1) is the most active peroxide isolated so far against T. b. brucei, and it indicates the potential therapeutic value of this class of compounds.
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Journal of Natural Products
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73
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4
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Chemical sciences
Biologically active molecules
Biological sciences
Biomedical and clinical sciences
Traditional, complementary and integrative medicine