These authors contributed equally to this work.
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Novel activity of acriflavine against colorectal cancer tumor cells
Article first published online: 12 OCT 2011
DOI: 10.1111/j.1349-7006.2011.02097.x
© 2011 Japanese Cancer Association
Additional Information
How to Cite
Hassan, S., Laryea, D., Mahteme, H., Felth, J., Fryknäs, M., Fayad, W., Linder, S., Rickardson, L., Gullbo, J., Graf, W., Påhlman, L., Glimelius, B., Larsson, R. and Nygren, P. (2011), Novel activity of acriflavine against colorectal cancer tumor cells. Cancer Science, 102: 2206–2213. doi: 10.1111/j.1349-7006.2011.02097.x
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These authors contributed equally to this work.
Publication History
- Issue published online: 20 NOV 2011
- Article first published online: 12 OCT 2011
- Accepted manuscript online: 12 SEP 2011 03:58PM EST
- (Received July 8, 2011/Revised August 13, 2011/Accepted August 18, 2011/Accepted manuscript online September 12, 2011)
A high-throughput screen of the cytotoxic activity of 2000 molecules from a commercial library in three human colon cancer cell lines and two normal cell types identified the acridine acriflavin to be a colorectal cancer (CRC) active drug. Acriflavine was active in cell spheroids, indicating good drug penetration and activity against hypoxic cells. In a validation step based on primary cultures of patient tumor cells, acriflavine was found to be more active against CRC than ovarian cancer and chronic lymphocytic leukemia. This contrasted to the activity pattern of the CRC active standard drugs 5-fluorouracil, irinotecan and oxaliplatin. Mechanistic studies indicated acriflavine to be a dual topoisomerase I and II inhibitor. In conclusion, the strategy used seems promising for identification of new diagnosis-specific cancer drugs. (Cancer Sci 2011; 102: 2206–2213)