Literature DB >> 31392413

Biological activity of Morita-Baylis-Hillman adduct homodimers in L. infantum and L. amazonensis: anti-Leishmania activity and cytotoxicity.

Juliana da Câmara Rocha1,2, Klinger Antonio da Franca Rodrigues3, Patrícia Lima do Nascimento Néris1, Larisse Virgolino da Silva2, Fernanda Silva Almeida4, Viviane Silva Lima2, Rephany Fonseca Peixoto2, Juliene da Câmara Rocha5, Fátima de Lourdes Assunção Araújo de Azevedo6, Robson Cavalcanti Veras6, Isac Almeida de Medeiros6, Wagner André Vieira da Silva7, Claudio G Lima-Junior7, Mário Luiz Araújo de Almeida Vasconcellos7, Ian Porto Gurgel do Amaral2, Márcia Rosa de Oliveira8, Tatjana de Souza Lima Keesen9.   

Abstract

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.

Entities:  

Keywords:  Anti-Leishmania activity; Leishmania spp.; Morita-Baylis-Hillman; Treatments

Mesh:

Substances:

Year:  2019        PMID: 31392413     DOI: 10.1007/s00436-019-06403-w

Source DB:  PubMed          Journal:  Parasitol Res        ISSN: 0932-0113            Impact factor:   2.289


  29 in total

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