Cytotoxic Polyketide Derivatives from the South China Sea Sponge Plakortis simplex

• DOI: 10.1021/np300771p
• Publication Date: 2013-03-25T18:06:30Z
• Authors: Jinrong Zhang; Xuli Tang; Jing Li; Peifeng Li; Nicole J. de Voogd; Xiaoqin Ni; Xiaojie Jin; Xiaojun Yao; Pinglin Li; Guoqiang Li
• Keywords: HeLa; Moiety; Butenolide; Sponge

Five new polyketides, plakortoxides A (1) and B (2), simplextones C (3) D (4), plakorsin (5), together with six known analogues (6–11) were isolated from the South China Sea sponge Plakortis simplex. Their structures identified by spectroscopic chemical methods, including NMR, MS, IR. Experimental calculated ECD spectra modified Mosher's method used to determine absolute configurations. Structurally, both feature a butenolide coupled an epoxide moiety, while consist of γ-butyrolactone cyclopentane moieties, is furan acetic acid polyketide. The cytotoxic activities isolates tested, compounds 8, 10, 11 showed potent cytotoxicity against K562 HeLa tumor cell lines IC50 values ranging 0.8 5.3 μM. Compound 3 significant inhibitory activity c-Met kinase.