Abstract

The aim of the present study was to evaluate the anti-leishmanial activity of Betula utilis D. Don ethanolic extract, isolated betulin (VA1), its semisynthetic derivative (VA2) against Leishmania donovani. The ethanolic extract was obtained by Soxhlet extraction, and betulin was isolated by column chromatography. In-silico studies identified potential interaction sites between amphotericin B (standard drug), betulin, its semisynthetic derivative, and the active sites of pteridine reductase (PTR1). VA2 exhibited important interactions with amino acid residues compared to betulin. Anti-promastigote activity and cytotoxicity tests were conducted using the MTT cell viability method on modified THP-1 cells infected with L. donovani. Promastigotes were treated with varying concentrations of VA1, VA2 and EEBU for 72 hours. In-vitro studies showed that EEBU, VA1 and VA2 significantly reduced viable L. donovani promastigotes, with IC50 values of (58.26 µM) EEBU, (58.39µM) VA1, and (25.50 µM) VA2. They also inhibited amastigote forms with low macrophage cytotoxicity. The significant anti-leishmanial activity exhibited by VA2 suggested it could serve as a lead agent against leishmaniasis.

Key words: Betula utilis, betulin, cytotoxicity, leishmania