摘要
The organometallic compounds triphenyltinsalicylate (TPTS) and triphenylsiliconsalicylate (TPSS) were found to be trypanocidal against culture forms of Trypanosoma congolense. Both compounds at 0.4–5 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 2–10 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 2–10 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.
摘要译文
该有机金属化合物triphenyltinsalicylate（TPT类）和triphenylsiliconsalicylate（TPSS）被发现是杀锥虫针对锥虫congolense的培养形式。两种化合物在0。4-51 / SUP TPT类杀寄生虫种群，相差显微镜下观察其之前有一个簇效应的至少50％。此外，3.51 / SUP TPSS被要求杀死T. congolense细胞的50％。在2-10的低剂量它是监测该有机金属化合物的作用的效果和模式是可行的。有中合成胆固醇的量的减少在6存在下50％毫升SUPcongolense具有K i的值3.61 / SUP 4天。 TPSS是，然而，在体内的完全失活。在trypanocides的设计中使用的有机金属化合物的讨论。版权
Andrew J. Nok[1,*]; Ishaya H. Nock[2] and Josiah J. Bonire[3];. The cholesterol pathway of Trypanosoma congolense could be a target for triphenyltinsalicylate and triphenylsiliconsalicylate inhibition[J]. Applied Organometallic Chemistry, 2003,17(1): 17-22