| Autor: |
Nok, Andrew J., Nock, Ishaya H., Bonire, Josiah J. |
| Zdroj: |
Applied Organometallic Chemistry; January 2003, Vol. 17 Issue: 1 p17-22, 6p |
| Abstrakt: |
The organometallic compounds triphenyltinsalicylate (TPTS) and triphenylsiliconsalicylate (TPSS) were found to be trypanocidal against culture forms of Trypanosoma congolense. Both compounds at 0.45 µmol ml−1 completely killed the parasites in vitro within 3-8 min after incubation. A dosage of 1.5 µmol ml−1 TPTS killed at least 50% of the parasite population, which was preceded by a cluster effect as observed under phase contrast microscopy. Also, 3.5 µg ml−1 of TPSS was required to kill 50% of the T. congolense cells. At a low dosage of 210 µg ml−1, it was feasible to monitor the effect and mode of action of the organometallic compounds. There was a 50% reduction in the amount of synthesized cholesterols in the presence of 6 µg ml−1 and 10 µg ml−1 of TPTS and TPSS respectively. TPTS and TPSS also non-competitively inhibited pyrophosphatase from lysed T. congolense with Ki values of 3.6 µM and 8.5 µM respectively. In the in vivo experiments, TPTS cured T. congolense infected mice at a dosage of 210 mg kg day−1 for 4 days. TPSS was, however, completely inactive in vivo. The use of organometallic compounds in the design of trypanocides is discussed. Copyright © 2002 John Wiley & Sons, Ltd. |
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