The Marine Microbial Alkaloid (R)‐Salsolinol is Effective Against Trypanosoma cruzi

Chagas disease is a parasitic disease with approximately 8 million people infected worldwide, presenting a limited and toxic treatment. Comprising a vast chemodiversity, microbial metabolites are among the most important sources of FDA‐approved anti‐infectives. In this work, the bioactivity‐guided fractionation from an extract obtained from the bacterium Bacillus altitudinis , isolated from a red seaweed, afforded an antitrypanosomal alkaloid which was characterized as ( R )‐salsolinol by 1 H NMR and HR‐ESIMS analysis. ( R )‐Salsolinol showed a trypanocidal effect against the trypomastigotes (EC 50 = 14 µg/mL) and a selective activity against the intracellular amastigotes (EC 50 = 19 µg/mL), with no mammalian cytotoxicity in human monocytic cells THP‐1 (CC 50 > 36 µg/mL). In silico studies predicted a high permeability into cell membranes, as well as a high gastrointestinal absorption, with acceptable parameters in pharmaceutical filters, as well as cruzipain as a possible target protein, suggesting that ( R )‐salsolinol can be used as a prototype for drug design studies in Chagas disease.