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Suppression of NRF2/ARE by Convallatoxin Sensitises A549 Cells to 5-FU-mediated Apoptosis

Suppression of NRF2/ARE by Convallatoxin Sensitises A549 Cells to 5-FU-mediated Apoptosis

June Lee, Jong-Su Kang, Le Ba Nam, Ok-Kyung Yoo, Young-Sam Keum

Free Radic Res. 2018 Dec;52(11-12):1416-1423.

PMID: 29902094

Abstract:

NF-E2-related factor 2 (NRF2) regulates transcription of phase II cytoprotective enzymes to protect normal cells against oxidative stress. However, a high level of NRF2 offers a growth advantage, chemoresistance, and radioresistance in cancer. In the present study, we have identified convallatoxin as a novel inhibitor of NRF2/ARE. Suppression of NRF2 by convallatoxin was not transcriptionally mediated, but regulated at the level of proteolysis. Convallatoxin activated GSK-3β and suppression of NRF2 by convallatoxin required the Neh6 domain. Convallatoxin sensitised A549 cells to 5-fluorouracil-mediated cell death by promoting apoptosis. Together, our results provide evidence that convallatoxin might be useful as a chemotherapeutic adjuvant due to its ability to suppress NRF2/ARE.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP508758	Convallatoxin		508-75-8	Price

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