3466-3476 Chromomycins a2and a3from marine actinomycetes with TRAIL resistance-overcoming and wnt signal inhibitory activities

Kazufumi Toume, Kentaro Tsukahara, Hanako Ito, Midori A. Arai, Masami Ishibashi

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19 Citations (Scopus)


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 (IC 50 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.

Original languageEnglish
Pages (from-to)3466-3476
Number of pages11
JournalMarine Drugs
Issue number6
Publication statusPublished - 2014 Jun
Externally publishedYes


  • Actinomycetes
  • Wnt

ASJC Scopus subject areas

  • Drug Discovery


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