thalifendine and protoberberine

Chemical investigation of the stem of Thalictrum foliolosum resulted in the isolation of two new bisbenzylisoquinoline alkaloids (1 and 2) along with known protoberberine group of isoquinoline alkaloids thalifendine (3) and berberine (4). The structures of the new compounds were established by detailed 2D NMR spectral analysis with their configurations determined from their optical rotation values and confirmed using circular dichroism. Inhibitory activities of these four compounds against DNA topoisomerase IB of Leishmania donovani were evaluated. Compound 2 exhibited almost complete inhibition of the enzyme activity at 50 μM concentration and it was found to be effective in killing both wild type as well as SAG resistant promastigotes of the parasite.

Topics: Alkaloids; Animals; Antiprotozoal Agents; Berberine; Berberine Alkaloids; Cells, Cultured; DNA Topoisomerases, Type I; Isoquinolines; Leishmania donovani; Macrophages, Peritoneal; Mice, Inbred BALB C; Molecular Structure; Thalictrum; Topoisomerase I Inhibitors