Abstract

Leishmaniasis remains a major world health problem, and in particular, Algeria ranks second for the incidence of cutaneous leishmaniasis. Pulicaria inuloides is a well-known Arabian Peninsula medicinal plant. In the present study, the chloroform, ethyl acetate and n-butanol extracts from the roots of Pulicaria inuloides were analyzed for antioxidant activity and its correlation with the total phenolic and flavonoid contents. The highest antioxidant activity using a DPPH assay was showed by the ethyl acetate extract (IC50 4.08 µg/mL), which also had the highest total phenolic content (307.12 µgAGE). Furthermore, P. inuloides root extracts were evaluated against Leishmania amazonensis and Leishmania donovani. The results highlighted the chloroform extract as the most active one against both tested Leishmania strains. A bioguided fractionation of the chloroform extract led to the isolation of (8R:8S)-(75:25 er)-10-isobutyryloxy-8,9-epoxy-thymol isobutyrate as the main bioactive component, showing a potent leishmanicidal activity on L. amazonensis promatigote and amastigote stages (IC50 5.03 and 2.87 µM, respectively) and a good selectivity index on murine macrophages (CC50 19.37 µM). This study provides the first report of the antioxidant and leishmanicidal activities of P. inuloides root extracts and the results point to this species as a source of potential bioactive agents.

Highlights

  • Leishmaniasis, a neglected tropical disease caused by protozoan parasites belonging to the genusLeishmania, remains a major world health problem [1]

  • Administration of exogenous antioxidants is a promising way of combating the undesirable effects of reactive oxygen species (ROS) induced oxidative damage

  • The results of the antioxidant activity (Table 1, Figure 1) by the DPPH radical scavenging assay of three extracts from the roots of P. inuloides indicated strong ability of the ethyl acetate extract to act as DPPH scavenger, with an IC50 value of 4.08 μg/mL, followed by the n-butanol and chloroform extracts (8.76 and 12.85 μg/mL, respectively)

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Summary

Introduction

Leishmania, remains a major world health problem [1]. CL, called “Biskra boil” in the local language, is a serious public health problem because the country has the second largest focus in the Pathogens 2019, 8, 201; doi:10.3390/pathogens8040201 www.mdpi.com/journal/pathogens. It is reported to be endemic in 328 third sub-national administrative levels with 10 million populations at risk, rising 13106 numbers of cases reported in 2017 [3]. The Leishmaniasis National Control Program (LNCP) in Algeria was established in 2006, with a vector control program based on pyrethroids as insecticides, but without reservoir host control program [5]. The treatment of the population is provided free of charge in the public sector, with the following antileishmanial medicines included in the national List of Essential Medicines: amphotericin

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