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Chromomycins A2 and A3 from Marine Actinomycetes with TRAIL Resistance-Overcoming and Wnt Signal Inhibitory Activities

Department of Natural Products Chemistry, Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan
Author to whom correspondence should be addressed.
Mar. Drugs 2014, 12(6), 3466-3476;
Received: 12 March 2014 / Revised: 5 April 2014 / Accepted: 9 April 2014 / Published: 5 June 2014
(This article belongs to the Special Issue Advances and New Perspectives in Marine Biotechnology)
A biological screening study of an actinomycetes strain assembly was conducted using a cell-based cytotoxicity assay. The CKK1019 strain was isolated from a sea sand sample. Cytotoxicity-guided fractionation of the CKK1019 strain culture broth, which exhibited cytotoxicity, led to the isolation of chromomycins A2 (1) and A3 (2). 1 and 2 showed potent cytotoxicity against the human gastric adenocarcinoma (AGS) cell line (IC50 1; 1.7 and 2; 22.1 nM), as well as strong inhibitory effects against TCF/β-catenin transcription (IC50 1; 1.8 and 2; 15.9 nM). 2 showed the ability to overcome tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) resistance. To the best of our knowledge, the effects of chromomycins A2 (1) and A3 (2) on TRAIL resistance-overcoming activity, and on the Wnt signaling pathway, have not been reported previously. Thus, 1 and 2 warrant potential drug lead studies in relation to TRAIL-resistant and Wnt signal-related diseases and offer potentially useful chemical probes for investigating TRAIL resistance and the Wnt signaling pathway. View Full-Text
Keywords: chromomycin A2; chromomycin A3; actinomycetes; TRAIL; Wnt chromomycin A2; chromomycin A3; actinomycetes; TRAIL; Wnt
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Toume, K.; Tsukahara, K.; Ito, H.; Arai, M.A.; Ishibashi, M. Chromomycins A2 and A3 from Marine Actinomycetes with TRAIL Resistance-Overcoming and Wnt Signal Inhibitory Activities. Mar. Drugs 2014, 12, 3466-3476.

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