Abstract
The Latin American plant Tabernaemontana longipes was studied in this work as a potential source of antiparasitic agents. The chloroform extract of T. longipes leaves was separated into several fractions, and tested for antitrypanosomal activity. One of the fractions displayed significant growth inhibitory activity against Trypanosoma brucei. The active principle in the fraction was isolated, purified, and characterized by NMR and mass spectrometry. The antitrypanosomal agent in the CHCl3 extract of T. longipes leaves is the pentacyclic triterpenoid bauerenol acetate. A metabolite profiling assay suggest that the triterpenoid influences cholesterol metabolism. The molecular target(s) of bauerenol and its acetate, like many other antiparasitic pentacyclic triterpenoids is/are unknown, but they present privileged structural scaffolds that can be explored for structure-based activity optimization studies using phenotypic assays.
Highlights
African sleeping sickness (Human African Trypanosomiasis) caused by protozoan Trypanosoma brucei gambiense/rhodesiense is still a public health problem in rural and remote regions of the continent, especially in the Democratic Republic of the Congo
T. longipes is a tropical plant found in several Latin American countries, including Nicaragua, Colombia, Ecuador, and Costa Rica
The leaves of T. longipes were obtained from several mature trees growing in Costa Rica in
Summary
African sleeping sickness (Human African Trypanosomiasis) caused by protozoan Trypanosoma brucei gambiense/rhodesiense is still a public health problem in rural and remote regions of the continent, especially in the Democratic Republic of the Congo. Despite a gradual decrease in the number of reported cases in the past few years, the lack of effective and safe medicines, the unavailability of adequate and rapid diagnostic tools, especially in rural and remote places, and the possibility of continuous transmission of the parasite from animal reservoirs to humans, make the disease a continuous threat to millions of people [1,2,3,4]. In our on-going exploration of tropical plants as potential sources of new antitrypanosomal agents, Tabernaemontana longipes Donn. (Apocynaceae) was studied as a potential source of antitrypanosomal phytochemicals.
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