Title:Overview of Natural Antiplasmodials from the Last Decade to Inspire Medicinal Chemistry
Volume: 28
Issue: 30
Author(s): Gilles Degotte , Bernard Pirotte, Pierre Francotte and Michel Frédérich*
Affiliation:
- Laboratory of Pharmacognosy, Faculty of Medicine, University of Liege, Liege,Belgium
Keywords:
Malaria, Plasmodium, natural products, antiplasmodial, marine products, fungi, bacteria.
Abstract:
Background: Despite major advances in the fight against this parasitic disease,
malaria remained a major cause of concern in 2021. This infection, mainly due to Plasmodium
falciparum, causes more than 200 million cases every year and hundreds of thousands
deaths in the developing regions, mostly in Africa. The last statistics show an increase
in the cases for the third consecutive year; from 211 million in 2015, it has reached
229 million in 2019. This trend could be partially explained by the appearance of resistance
to all the used antimalarials, including artemisinin. Thus, the design of new anti-
Plasmodium compounds is an urgent need. For thousands of years, nature has offered
humans medicines to cure their diseases or the inspiration for the development of new active
principles. It then seems logical to explore the natural sources to find new molecules
to treat this parasitosis.
Methods: Therefore, this review reports and analyzes the extracts (plants, bacteria,
sponges, fungi) and the corresponding isolated compounds, showing antiplasmodial properties
between 2013 and 2019.
Results and Conclusion: Nature remains a major source of active compounds. Indeed,
648 molecules from various origins, mostly plants, have been reported for their inhibitory
effect on Plasmodium falciparum. Among them, 188 scaffolds were defined as highly active
with IC50 ≤ 5 μM, and have been reported here in detail. Moreover, the most active
compounds showed a large variety of structures, such as flavonoids, triterpenes, and alkaloids.
Therefore, these compounds could be an interesting source of inspiration for medicinal
chemists; several of these molecules could become the next leads for malaria treatment.
