Antitrypanosomal Cyclic Polyketide Peroxides from the Australian Marine Sponge Plakortis sp.

作者：Feng Yunjiang; Davis Rohan A; Sykes Melissa; Avery Vicky M; Camp David; Quinn Ronald J^*

来源：Journal of Natural Products, 2010, 73(4): 716-719.

DOI：10.1021/np900535z

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-didephydro-13-oxo-plakortide Q(1) and 10-carboxy-11,12,13,14-tetranor-plakortide Q(2). Antitrypanosomal studies showed that compound 1 had an IC(50) 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.

• 出版日期2010-4