Planta Med 2012; 78 - PI81
DOI: 10.1055/s-0032-1320768

Asperjinone, a norneolignan, and terrein, a suppressor of ABCG2-expressing breast cancer cells, from Aspergillus terreus

WY Liao 1, 2, CN Shen 2, LH Lin 3, YL Yang 4, HY Han 2, JW Chen 1, SC Kuo 1, SH Wu 3, 5, CC Liaw 6
  • 1Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung 402, Taiwan
  • 2Genomics Research Center, Academia Sinica, Taipei 115, Taiwan
  • 3Graduate Institute of Biochemical Science, National Taiwan University, Taipei 106, Taiwan
  • 4Agricultural Biotechnology Research Center, Academia Sinica, Taipei 115, Taiwan
  • 5Institute of Biological Chemistry, Academia Sinica, Taipei 115, Taiwan
  • 6Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung 804, Taiwan

Breast cancer cells express ABCG2 transporters, which mediate multidrug resistance. Discovering a novel compound that can suppress ABCG2 expression and restore drug sensitivity could be the key to improving breast cancer therapeutics. In the current work, one new nor-neolignan, asperjinone (1), as well as 12 other known compounds, was isolated from Aspergillus terreus. The structure of the new isolate was determined by spectroscopic methods. Among these isolates, terrein (2) displayed strong cytotoxicity against breast cancer MCF-7 cells. Treatment with terrein (2) significantly suppressed growth of ABCG2-expressing breast cancer cells. This suppressive effect was achieved by inducing apoptosis via activating the caspase-7 pathway and inhibiting Akt signaling pathway, which led to a decrease in ABCG2-expressing cells and reduction in the side-population phenotype.