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

被引:38
|
作者
Feng, Yunjiang [1 ]
Davis, Rohan A. [1 ]
Sykes, Melissa [1 ]
Avery, Vicky M. [1 ]
Camp, David [1 ]
Quinn, Ronald J. [1 ]
机构
[1] Griffith Univ, Eskitis Inst, Brisbane, Qld 4111, Australia
来源
JOURNAL OF NATURAL PRODUCTS | 2010年 / 73卷 / 04期
关键词
TRYPANOSOMA-BRUCEI; SLEEPING SICKNESS; DIOL ANALOGS; INHIBITORS; HALICHONDRIOIDES; EFLORNITHINE; METABOLITES; DISCOVERY; SIMPLEX; TBCATB;
D O I
10.1021/np900535z
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
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.
引用
收藏
页码:716 / 719
页数:4
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