Department of Parasitology, University of Granada, Granada, Spain.
Am J Trop Med Hyg. 2012 Sep;87(3):481-8. doi: 10.4269/ajtmh.2012.11-0471. Epub 2012 Jul 16.
Four terpenoid derivatives were examined for their activity against Trypanosoma cruzi. Our results show that two compounds were very active in vitro against both extra- and intracellular forms. These compounds, non-toxic for the host cells, are more effective than the reference drug benznidazole. The capacity to infect cells was negatively affected and the number of amastigotes and trypomastigotes was reduced. A wide range of ultrastructural alterations was found in the epimastigote forms treated with these compounds. Some metabolic changes occurred presumably at the level of succinate and acetate production, perhaps caused by the disturbance of the enzymes involved in sugar metabolism inside the mitochondria. In vivo results were consistent with those observed in vitro. The parasitic load was significantly lower than in the control assay with benznidazole. The effects of these products showed the reduction of the anti-T. cruzi antibodies level during the chronic stage.
四种萜类衍生物的抗 Trypanosoma cruzi 活性研究。我们的结果表明，两种化合物对细胞内外形式的活性都非常高。这些化合物对宿主细胞无毒，比参考药物苯并咪唑更有效。感染细胞的能力受到负面影响，并且阿米巴和锥虫数量减少。在用这些化合物处理的epimastigote 形式中发现了广泛的超微结构改变。一些代谢变化可能发生在琥珀酸和醋酸盐产生水平上，可能是由于线粒体中参与糖代谢的酶受到干扰所致。体内结果与体外观察结果一致。寄生虫负荷明显低于苯并咪唑对照试验。这些产物的作用显示出在慢性阶段降低了抗 T. cruzi 抗体的水平。
