Mechanisms of 1-hydroxy-2-hydroxymethylanthraquinone from Coptosapelta flavescens as an anti-giardial activity

Thai medicinal plants represent a rich source of potential anti-parasitic compounds. 1-hydroxy-2-hydroxymethylanthraquinone (CFQ) purified from Coptosapelta flavescens, a plant commonly used to expel intestinal worms, indicated potential anti-giardial agent as shown in a previous study. This study aims to investigate its mechanism of action. We assessed whether CFQ was involved as an inducer of apoptosis as well as having effects on the fine structure of Giardia intestinalis trophozoites. We observed the consequences of exposing G. intestinalis trophozoites to CFQ and metronidazole, both had an IC50 of 0.42 mu g/ml, after 6, 12 and 24h exposure. An apoptosis in trophozoite was confirmed by the AnnexinV-FITC assay and as viewed by flow cytometry. CFQ at its IC50 induced apoptosis as early as 6 h after incubation while metronidazole produced little or no apoptosis at its IC50 value. Ultrastructural analyzes at 24 h demonstrated that both CFQ and metronidazole induced several physical alterations, including the appearance of wrinkled and rounded cells, membrane blebbing, ventral disc damage, electron dense precipitates in the nuclei, all of which were indicative of cell death. However, membrane rupture was found only in G. intestinalis exposed to CFQ and this proved the induction of apoptosis. Taken together, we have provided a mechanistic explanation of the action of CFQ against G. intestinalis trophozoites. These results have provided further evidence that CFQ is a new compound that has the potential for use to treat infections from G. intestinalis. (C) 2015 Elsevier B.V. All rights reserved.