Parasitology research · 2019
Biological activity of Morita-Baylis-Hillman adduct homodimers in L. infantum and L. amazonensis: anti-Leishmania activity and cytotoxicity.
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da Câmara Rocha Juliana, da Franca Rodrigues Klinger Antonio, do Nascimento Néris Patrícia Lima, da Silva Larisse Virgolino, Almeida Fernanda Silva, Lima Viviane Silva, Peixoto Rephany Fonseca, da Câmara Rocha Juliene, de Azevedo Fátima de Lourdes Assunção Araújo, Veras Robson Cavalcanti, de Medeiros Isac Almeida, da Silva Wagner André Vieira, Lima-Junior Claudio G, de Almeida Vasconcellos Mário Luiz Araújo, do Amaral Ian Porto Gurgel, de Oliveira Márcia Rosa, de Souza Lima Keesen Tatjana
Аннотация
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.