Dicationic compounds, which are derivatives of pentamidine, are being developed for use as antiprotozoal drugs. These compounds bind to the minor groove of DNA and are thought to inhibit DNA-dependent enzymes and thereby prevent cellular replication by protozoans. The objective of this study was to test the ability of a group of these compounds to inhibit the intracellular and extracellular reproduction of Trypanosoma cruzi in vitro. At present, there are few drugs in use capable of inhibiting the intracellular stages of this parasite, and therefore compounds with this ability would be of value. Cultures of mouse fibroblasts were infected and treated with doses of dicationic compounds, and the numbers of parasites released at the end of the 5- to 7-day growth cycle were determined. Five of the compounds tested were found to be effective at inhibiting T. cruzi growth at doses that were not toxic to the host cells. The compound found most effective (DB709) inhibited parasite release at the low concentration of 0.8 ng/ml, justifying further study. These results suggest that dicationic compounds may have potential as chemotherapy against T. cruzi infection.
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October 2003
RESEARCH NOTES|
October 01 2003
Inhibition of In Vitro Intracellular Growth of Trypanosoma cruzi by Dicationic Compounds
Edwin C. Rowland;
Edwin C. Rowland
aBiomedical Sciences Department, College of Osteopathic Medicine, Ohio University, Athens, Ohio 45701
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Deborah Moore-Lai;
Deborah Moore-Lai
aBiomedical Sciences Department, College of Osteopathic Medicine, Ohio University, Athens, Ohio 45701
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John R. Seed;
John R. Seed
bDepartment of Epidemiology, School of Public Health, University of North Carolina, Chapel Hill, North Carolina 27599
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Chad E. Stephens;
Chad E. Stephens
cDepartment of Chemistry, Georgia State University, Atlanta, Georgia 30303. rowland@ohiou.edu
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David W. Boykin
David W. Boykin
cDepartment of Chemistry, Georgia State University, Atlanta, Georgia 30303. rowland@ohiou.edu
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J Parasitol (2003) 89 (5): 1078–1080.
Citation
Edwin C. Rowland, Deborah Moore-Lai, John R. Seed, Chad E. Stephens, David W. Boykin; Inhibition of In Vitro Intracellular Growth of Trypanosoma cruzi by Dicationic Compounds. J Parasitol 1 October 2003; 89 (5): 1078–1080. doi: https://doi.org/10.1645/GE-53R
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