Marquez, N., Sancho, R., Ballero, M., Bremner, P., Appendino, G., Fiebich, B.L., Heinrich, M. and Munoz, E. (2004) Imperatorin inhibits T-cell proliferation by targeting the transcription factor NFAT. Planta Medica, 70 (11). pp. 1016-1021. 10.1055/s-2004-832640.
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In our ongoing research into anti-inflammatory compounds from medicinal plants in the Mediterranean area, we have isolated several furanocoumarins from the roots of Oppopanax chironium (L.), and have evaluated them for activity related to T-cell functionality. Heraclenin (1) and imperatorin (2) significantly inhibited T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner. In transient transfection experiments with a plasmid containing the IL-2 promoter we found that imperatorin is a potent inhibitor of IL-2 gene transcription. To further characterize the inhibitory mechanisms of imperatorin at the transcriptional level, we examined the DNA-binding and transcriptional activities of NF-kappaB, NFAT, and AP-1 transcription factors in Jurkat T cells. We found that imperatorin inhibited both the NFAT binding to DNA and transcriptional activities, without affecting significantly the activation of the NF-kappaB and AP-1 transcription factors. These findings provide new insights into the molecular mechanisms involved in the immunomodulatory and anti-inflammatory activities of natural furanocoumarins.
|Additional Information:||Full text available in print in the School of Pharmacy Library.|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Centre for Pharmacognosy and Phytotherapy|
|Journal or Publication Title:||Planta Medica|
|Deposited By:||Library Staff|
|Deposited On:||23 Nov 2006|
|Last Modified:||07 Oct 2011 11:18|
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