Abstract

Schistosomiasis is a neglected tropical disease that affects million people worldwide, mostly in developing countries. Ruta graveolens (Rutaceae) is a plant used in folk medicine to treat several diseases, including parasitic infections. In this study, we reported the in vitro schistosomicidal activity of the R. graveolens extract (Rg) and its active fraction (Rg-FAE). Also, the characterization of Rg-FAE by UPLC-ESI-QTOF-MS analysis and its in vitro antileishmanial activity against Leishmania braziliensis were also performed. In vitro schistosomicidal assays were assessed against adult worms of S. mansoni, while cell viability against peritoneal macrophages was measured by MTT assay. Rg (100 μg/mL) exhibited noticeable schistosomicidal activity, causing 100% mortality and decreasing motor activity of all adult male and female schistosomes, but with low activity against L. braziliensis. After chromatographic fractionation of Rg, fraction Rg-FAE was obtained, showing high activity against adult schistosomes. UPLC-ESI-QTOF-MS analysis of Rg-FAE revealed the presence of eleven alkaloids and one furanocoumarin. No significant antileishmanial activity was found for Rg, while Rg-FAE exhibited activity against L. braziliensis promastigotes. We demonstrated, for the first time, that the R. graveolens extract (Rg) and its alkaloid-rich fraction (Rg-FAE) are active against adult worms of S. mansoni, with no significant cytotoxicity on macrophages. Our findings open the route to further antiparasitic studies with the active fraction of R. graveolens and its identified compounds, especially alkaloids.

Highlights

  • Schistosomiasis is a neglected tropical disease (NTD) caused by Schistosoma parasites, mainly S. mansoni, that is associated with long-term undernutrition, anaemia, organ scarring, and fibrosis, resulting in disabling patient symptoms [1]

  • Results and Discussion e demand for new therapeutic alternatives against the 20 groups of the so-called NTDs is a worldwide need since the few drugs available are often associated with severe side effects and high toxicity [1, 6, 15]

  • Considering the promising antiparasitic potential of Rutaceae species, in this work, we have highlighted the antischistosomal activity of an alkaloid-rich fraction from the R. graveolens extract

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Summary

Introduction

Schistosomiasis is a neglected tropical disease (NTD) caused by Schistosoma parasites, mainly S. mansoni, that is associated with long-term undernutrition, anaemia, organ scarring, and fibrosis, resulting in disabling patient symptoms [1]. Some antileishmanial compounds have been registered as medications, such as amphotericin B, pentamidine, and miltefosine, none of the available drugs can be considered perfect because of their high toxicity, long duration of treatment, and severe adverse reactions, which often lead to treatment abandonment [5]. In this scenario, there is an urgent need for new and better antileishmanial drugs [5, 6]

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