Antimalarial and Antileishmanial Activities of Phytophenolics and Their Synthetic Analogues |
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Authors: | Masanori Morimoto Charles L. Cantrell Shabana Khan Babu L. Tekwani Stephen O. Duke |
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Affiliation: | 1. USDA‐ARS, Natural Products Utilization Research Unit, Thad Cochran Center, University, MS, USA;2. Department of Applied Chemistry, Graduated School of Agriculture, Kindai University, Nara City, Nara, Japan;3. National Center for Natural Products Research, School of Pharmacy, University of Mississippi, MS, USA |
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Abstract: | Thirty‐seven phytophenolics and their synthetic analogues were evaluated for activity against two protozoal pathogens, Leishmania donovani and Plasmodium falciparum (D6 and W2 clones), respectively. 4,6‐Dimethoxyaurone demonstrated the highest activity with IC50 values of 13.2 and 16.9 μm against L. donovani and P. falciparum (W2 clone), respectively, without undesired cytotoxicity against VERO cells. The moiety having two benzene rings was critical to maintain the antiprotozoal activities based on the observation that both coumaranones and chromones were inactive while other test compounds, including coumarans and aurones, remained active. There was no correlation between antiprotozoal activities and previously evaluated insect antifeedant activity against common cutworms (Spodoptera litura). Flavonoids, including aurones, pterocarpans, and lignan like dihydrobenzofurans, structural analogues of coumarans, are abundant in fruits and vegetables, so these phytophenolics may act as natural antiprotozoal agents in humans. |
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Keywords: |
Leishmania donovani
Plasmodium falciparum
Phytophenolics Antiprotozoal activity Aurones |
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