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Research Project: Health-Promoting Bioactives and Biobased Pesticides from Medicinal and Herbal Crops

Location: Natural Products Utilization Research

Title: Antimalarial and antileishmanial activities of phytophenolics and their synthetic analogues

Author
item Morimoto, Masanori - Kinki University
item Cantrell, Charles
item Khan, Shabana - University Of Mississippi
item Tekwani, Babu - University Of Mississippi
item Duke, Stephen

Submitted to: Chemistry and Biodiversity
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 10/3/2017
Publication Date: 12/5/2017
Citation: Morimoto, M., Cantrell, C.L., Khan, S., Tekwani, B.L., Duke, S.O. 2017. Antimalarial and antileishmanial activities of phytophenolics and their synthetic analogues. Chemistry and Biodiversity. DOI: 10.1002/cbdv.201700324.
DOI: https://doi.org/10.1002/cbdv.201700324

Interpretive Summary: Plants produce various phenolics for protection from natural enemies, such as phytophagous insects, and environmental stresses such as severe sun light. The system is physiologically called a chemical defense system. In our research, the phytophenolic mono-/bi-benzene analogues were evaluated against protozoa causing the diseases leishmaniasis and malaria. Thirty-seven phytophenolics and their synthetic analogues were evaluated for activity against these two protozoal pathogens. 4,6-Dimethoxyaurone demonstrated the highest activity against protozoa causing the diseases leishmaniasis and malaria without undesired cytotoxicity. There was no correlation between antiprotozoal activities and previously evaluated insect antifeedant activity against common cutworms.

Technical Abstract: Thirty-seven phytophenolics and their synthetic analogues were evaluated for activity against two protozoal pathogens, Leishmania donovani and Plasmodium falciparum (D6 and W2 clone), respectively. 4,6-Dimethoxyaurone demonstrated the highest activity with IC50 values of 13.2 uM and 16.9 uM 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 coumaranes 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, pterocarpanes, and lignans, structural analogues of coumaranes, are abundant in fruits and vegetables, so these phytophenolics may act as natural antiprotozoal agents in humans.