Title:Flavonoid-derived Privileged Scaffolds in anti-Trypanosoma brucei Drug Discovery
Volume: 20
Issue: 12
Author(s): Pone Kamdem Boniface*Ferreira Igne Elizabeth
Affiliation:
- Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Sao Paulo,Brazil
Keywords:
Human african trypanosomiasis, flavonoids, molecular targets, drug discovery, neglected tropical diseases, Trypanosoma
brucei gambiense.
Abstract:
Background: Human African Trypanosomiasis (HAT), also known as sleeping sickness is
one of the 20 neglected tropical diseases listed by the World Health Organization, which lead to death
if left untreated. This disease is caused by Trypanosoma brucei gambiense, which is the chronic form
of the disease present in western and central Africa, and by T. brucei rhodesiense, which is the
acute form of the disease located in eastern and southern Africa. Many reports have highlighted the
effectiveness of flavonoid-based compounds against T. brucei.
Objective: The present review summarizes the current standings and perspectives for the use of flavonoids
as lead compounds for the potential treatment of HAT.
Methods: A literature search was conducted for naturally occurring and synthetic anti-T brucei flavonoids
by referencing textbooks and scientific databases (SciFinder, PubMed, Science Direct,
Wiley, ACS, SciELO, Google Scholar, Springer, among others) from their inception until February
2019.
Results: Flavonoids isolated from different parts of plants and species were reported to exhibit moderate
to high in vitro antitrypanosomal activity against T. brucei. In addition, synthetic flavonoids revealed
anti-T. brucei activity. Molecular interactions of bioactive flavonoids with T. brucei protein
targets showed promising results.
Conclusion: According to in vitro anti-T brucei studies, there is evidence that flavonoids might be
lead compounds for the potential treatment of HAT. However, toxicological studies, as well as the
mechanism of action of the in vitro active flavonoids are needed to support their use as potential leads
for the treatment of HAT.