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

摘要: Herein, we evaluated in vitro the anti-leishmanial activity of betulin derivatives Venezuelan isolates Leishmania amazonensis, isolated from patients with therapeutic failure. Methods: We analyzed promastigote susceptibility as well cytotoxicity and selectivity compounds. Additionally, selected compounds was determined intracellular amastigotes. Finally, to gain hints on their potential mechanism action, effect most promising plasma mitochondrial membrane potential, nitric oxide superoxide production by infected macrophages determined. Results: From tested 28 compounds, those numbered 18 22 were chosen for additional studies. Both active (GI50 ≤ 2 µM, cytotoxic CC50 > 45 SI 20) reference strain LTB0016 patient isolates. The results suggest that significantly depolarized (p < 0.05) when compared untreated cells. Although neither nor induced macrophages, macrophages. Conclusion: Our due efficacy against parasites mechanisms underlying leishmanicidal effect, could be used tools designing new chemotherapies leishmaniasis.