Institute of Pharmacology and Toxicology, Department of Biomedical Sciences, University of Veterinary Medicine Vienna, Vienna, Austria.
Department of Parasitology, Institute of Tropical Medicine "Pedro Kourí", Havana, Cuba.
Phytother Res. 2018 Sep;32(9):1729-1740. doi: 10.1002/ptr.6097. Epub 2018 Apr 19.
The antileishmanial activity of the essential oil (EO) from Chenopodium ambrosioides L. has been demonstrated in vitro and in animal models, attributed to the major components of the EO. This study focused on the effects of the three major EO compounds carvacrol, caryophyllene oxide (Caryo), and the antileishmanial endoperoxide ascaridole (Asc) on mitochondrial functions in Leishmania tarentolae promastigotes (LtP). EO and Caryo were able to partially inhibit the leishmanial electron transport chain, whereas other components failed to demonstrate a direct immediate effect. Caryo demonstrated inhibition of complex III activity in LtP and in isolated complex III from other species. The formation of superoxide radicals was studied in Leishmania by electron spin resonance spectroscopy in the presence of iron chelators wherein selected compounds failed to trigger a significant immediate additional superoxide production in LtP. However, upon prolonged incubation of Leishmania with Asc and especially in the absence of iron chelators (allowing the activation of Asc), an increased superoxide radical production and significant impairment of mitochondrial coupling in Leishmania was observed. Prolonged incubation with all EO components resulted in thiol depletion. Taken together, the major components of EO mediate their leishmanicidal activity via different mitochondrial targets and time profiles. Further studies are required to elucidate possible synergistic effects of carvacrol and Asc and the influence of minor compounds.
从Chenopodium ambrosioides L.中提取的精油(EO)已被证明具有抗利什曼原虫活性,这种活性归因于 EO 的主要成分。本研究主要关注三种主要 EO 化合物香芹酚、石竹烯氧化物(Caryo)和抗利什曼原虫过氧化物ascaridole(Asc)对 Leishmania tarentolae 前鞭毛体(LtP)线粒体功能的影响。EO 和 Caryo 能够部分抑制利什曼原虫的电子传递链,而其他成分则未能显示出直接的即时影响。Caryo 显示出对 LtP 和其他物种分离的复合物 III 活性的抑制作用。通过电子自旋共振光谱法在存在铁螯合剂的情况下研究了利什曼原虫中超氧自由基的形成,其中选择的化合物未能在 LtP 中引发明显的即时额外超氧自由基产生。然而,当 Asc 与利什曼原虫孵育时间延长,特别是在没有铁螯合剂的情况下(允许 Asc 激活),观察到超氧自由基产生增加和利什曼原虫线粒体偶联严重受损。与所有 EO 成分的长时间孵育都会导致硫醇耗竭。综上所述,EO 的主要成分通过不同的线粒体靶标和时间谱介导其杀利什曼原虫活性。需要进一步研究以阐明香芹酚和 Asc 的可能协同作用以及微量化合物的影响。