Abstract
With an estimated annual incidence of one million cases, leishmaniasis is one of the top five vector-borne diseases. Currently available medical treatments involve side effects, including toxicity, non-specific targeting, and resistance development. Thus, new antileishmanial chemical entities are of the utmost interest to fight against this disease. The aim of this study was to obtain potential antileishmanial natural products from Psidium guajava leaves using a metabolomic workflow. Several crude extracts from P. guajava leaves harvested from different locations in the Lao People’s Democratic Republic (Lao PDR) were profiled by liquid chromatography coupled to high-resolution mass spectrometry, and subsequently evaluated for their antileishmanial activities. The putative active compounds were highlighted by multivariate correlation analysis between the antileishmanial response and chromatographic profiles of P. guajava mixtures. The results showed that the pooled apolar fractions from P. guajava were the most active (IC50 = 1.96 ± 0.47 µg/mL). Multivariate data analysis of the apolar fractions highlighted a family of triterpenoid compounds, including jacoumaric acid (IC50 = 1.318 ± 0.59 µg/mL) and corosolic acid (IC50 = 1.01 ± 0.06 µg/mL). Our approach allowed the identification of antileishmanial compounds from the crude extracts in only a small number of steps and can be easily adapted for use in the discovery workflows of several other natural products.
Highlights
Leishmaniasis is in the top five of vector-bone diseases identified in the Global Health Estimates2016 summary table of the World Health Organization (WHO)
Antileishmanial activities of the nine crude extracts and fractions from P. guajava leaves collected in different areas of Lao People’s Democratic Republic (Lao PDR) were tested on the promastigote and amastigote forms of L. infantum at concentrations of 25 and 50 μg/mL
The results indicated that crude extracts, and polar and apolar fractions were not active on promastigote forms, whereas crude extracts and apolar fractions inhibited over 50% of L. infantum amastigotes at 25 μg/mL (Figure 1A)
Summary
Leishmaniasis is in the top five of vector-bone diseases identified in the Global Health Estimates. 2016 summary table of the World Health Organization (WHO). It is one of 20 neglected tropical diseases that infect one billion people in low socioeconomic populations in 149 countries [1]. Leishmaniasis is caused by the genus Leishmania spp., which includes 29 species. Leishmania donovani and Leishmania infantum cause visceral leishmaniasis, the lethal form of the disease [2]. The epidemiology of leishmaniasis depends on a variety of factors including the between host, reservoir and vector (human, animal and sandfly), the local ecological characteristics of the transmission sites such as alterations in temperature and water storage, irrigation habits, deforestation, climate changes, exposure
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