Leishmanicidal Activity of Betulin Derivatives in Leishmania amazonensis; Effect on Plasma and Mitochondrial Membrane Potential, and Macrophage Nitric Oxide and Superoxide Production.

ABSTRACT: Herein, we evaluated in vitro the anti-leishmanial activity of betulin derivatives in Venezuelan isolates of Leishmania amazonensis, isolated from patients with therapeutic failure.

Methods

We analyzed promastigote in vitro susceptibility as well as the cytotoxicity and selectivity of the evaluated compounds. Additionally, the activity of selected compounds was determined in intracellular amastigotes. Finally, to gain hints on their potential mechanism of action, the effect of the most promising compounds on plasma and mitochondrial membrane potential, and nitric oxide and superoxide production by infected macrophages was determined.

Results

From the tested 28 compounds, those numbered 18 and 22 were chosen for additional studies. Both 18 and 22

SUBMITTER: Alcazar W 

PROVIDER: S-EPMC7913927 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature