Biological activity of Morita-Baylis-Hillman adduct homodimers in L. infantum and L. amazonensis: anti-Leishmania activity and cytotoxicity.
Juliana da Câmara RochaKlinger Antonio da Franca RodriguesPatrícia Lima do Nascimento NérisLarisse Virgolino da SilvaFernanda Silva AlmeidaViviane Silva LimaRephany Fonseca PeixotoJuliene da Câmara RochaFátima de Lourdes Assunção Araújo de AzevedoRobson Cavalcanti VerasIsac Almeida de MedeirosWagner André Vieira da SilvaClaudio G Lima-JuniorMário Luiz Araújo de Almeida VasconcellosIan Porto Gurgel do AmaralMárcia Rosa de OliveiraTatjana de Souza Lima KeesenPublished in: Parasitology research (2019)
This study is a report on the anti-Leishmania activity of Morita-Baylis-Hillman (MBH) homodimers adducts against the promastigote and axenic amastigote forms of Leishmania (Leishmania) infantum and Leishmania (Leishmania) amazonensis and on the cytotoxicity of these adducts to human blood cells. Both studied homodimers, MBH 1 and MBH 2, showed activity against the promastigote forms of L. infantum and L. amazonensis, which are responsible for visceral and cutaneous leishmaniasis, respectively. Additionally, the homodimers presented biological activity against the axenic amastigote forms of these two Leishmania species. The adducts exhibited no hemolytic activity to human peripheral blood mononuclear cells or erythrocytes at the tested concentrations and achieved higher selectivity indices than amphotericin B. Evaluation of cell death by apoptosis revealed that the homodimers had better apoptosis/necrosis profiles than amphotericin B in the promastigote forms of both L. infantum and L. amazonensis. In conclusion, these Morita-Baylis-Hillman adducts had anti-Leishmania activity in an in vitro model and may thus be promising molecules in the search for new drugs to treat leishmaniasis.