Cell screening assay for identifying inhibitors of eosinophil proliferation
Version of Record online: 4 FEB 2011
© 2011 Wiley-Liss, Inc.
Drug Development Research
Volume 72, Issue 4, pages 353–360, June 2011
How to Cite
Kempe-Dustin, J. J., Aboul-Fadl, T., Christensen, C., Palais, R., Parsawar, K., Gleich, G. J. and Wagner, L. A. (2011), Cell screening assay for identifying inhibitors of eosinophil proliferation. Drug Dev. Res., 72: 353–360. doi: 10.1002/ddr.20438
- Issue online: 20 JUN 2011
- Version of Record online: 4 FEB 2011
- Manuscript Accepted: 27 DEC 2010
- Manuscript Received: 18 JUN 2010
- University of Utah Foundation
- University of Utah Biology Undergraduate Research Program
The purpose of this study was to develop a cell-based screening assay for identification of small molecules for the treatment of asthma. Eosinophils are leukocytes that contribute to the pathology of asthma. Lidocaine inhibits interleukin-5 (IL-5)-mediated survival and activation of human eosinophils, and it is able to replace inhaled glucocorticoids for the treatment of asthma; however, lidocaine has many side effects, including anesthesia. Therefore, a collection of commercial and novel, synthesized lidocaine analogues were investigated for inhibitory activity of the IL-5-stimulated proliferation of TF-1 cells, a CD34+, cytokine-dependent, erythroleukemic cell line model for eosinophil growth. Among 74 investigated compounds, 10 were more potent inhibitors of cell proliferation than lidocaine (average IC50 = 223 µM), with IC50 values ranging within 1–119 µM. This cell-based assay is an effective method for screening chemical compounds and has revealed promising lead compounds for the treatment of asthma. Drug Dev Res 72: 353–360, 2011. © 2011 Wiley-Liss, Inc.