bcrp - publications

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1. J Nat Prod. 2012 Feb 23. [Epub ahead of print]

Asperjinone, a Nor-Neolignan, and Terrein, a Suppressor of ABCG2-Expressing
Breast Cancer Cells, from Thermophilic Aspergillus terreus.

Liao WY, Shen CN, Lin LH, Yang YL, Han HY, Chen JW, Kuo SC, Wu SH, Liaw CC.

Graduate Institute of Pharmaceutical Chemistry, China Medical University ,
Taichung 402, Taiwan, Republic of China.

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 the Akt
signaling pathway, which led to a decrease in ABCG2-expressing cells and a
reduction in the side-population phenotype.

PMID: 22360613 [PubMed - as supplied by publisher]