Abstract
Constant efforts to discover new antileishmanial agents are important because there are only a few available drugs for the treatment of leishmaniasis, which present several drawbacks including high toxicity and difficult route of administration. In this scenario, different sources of natural products have been explored regarding their potential to treat infectious diseases. Following this initiative, our research team has been analyzing the bioactive potential of Himantothallus grandifolius, an endemic macroalga of the Antarctic region, with the hypothesis that the hostile environment imposed on these organisms has shaped its arsenal of chemical constituents, thus consequently bringing new opportunities to discover bioactive compounds that might be useful against leishmaniasis. Herein, we report the antileishmanial property of the fatty acid 13E-docosenamide, identified during the fractionation of the hexanic extract of H. grandifolius after semipreparative high performance liquid chromatography separation and ultrafast liquid chromatography coupled with mass spectrometry analyses to track its antileishmanial constituents. 13E-docosenamide was found in HSG11and HSG12 fractions, presented promising antileishmanial activity (IC50 = 9.6 μg ml−1) and is 10 times more selective to the parasite rather than to the host cells (SI > 10.4).
Highlights
The food industries consume a wide range of algae, which are well known to have high contents of polysaccharides, fatty acids, sterols, fiber, minerals, vitamins, and a large number of antioxidants (Gambato et al, 2014; Pereira et al, 2012)
Our research team has been analyzing the bioactive potential of Himantothallus grandifolius, an endemic macroalga of the Antarctic region, with the hypothesis that the hostile environment imposed on these organisms has shaped its arsenal of chemical constituents, bringing new opportunities to discover bioactive compounds that might be useful against leishmaniasis
We report the antileishmanial property of the fatty acid 13E-docosenamide, identified during the fractionation of the hexanic extract of H. grandifolius after semipreparative high performance liquid chromatography separation and ultrafast liquid chromatography coupled with mass spectrometry analyses to track its antileishmanial constituents. 13E-docosenamide was found in HSG11and HSG12 fractions, presented promising antileishmanial activity (IC50 = 9.6 μg ml−1) and is 10 times more selective to the parasite rather than to the host cells (SI > 10.4)
Summary
The food industries consume a wide range of algae, which are well known to have high contents of polysaccharides, fatty acids, sterols, fiber, minerals, vitamins, and a large number of antioxidants (Gambato et al, 2014; Pereira et al, 2012). Clementino et al / Journal of Applied Pharmaceutical Science 10 (12); 2020: 098-103 investigates the potential of H. grandifolius secondary metabolites against leishmaniasis. This parasitic disease endangers more than one billion people in endemic areas throughout the world and if left untreated it can lead to 20,000–30,000 deaths annually (Molyneux et al, 2016). There are few therapeutic options for the treatment of leishmaniasis including pentavalent antimony, amphotericin B, miltefosine, and paromomycin, which present several drawbacks such as high toxicity and low efficacy (Sundar and Chakravarty, 2015), which makes the discovery of new therapeutic alternatives urgent. The aim of this study was to evaluate the antileishmanial activity of extracts and fractions of the Antarctic alga H. grandifolius against Leishmania amazonensis, the etiologic agent of cutaneous leishmaniasis, followed by UPLC-MS analyses revealing for the first time the antileishmanial properties of 13E-docosenamide
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