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

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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.

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Authors and Affiliations

  1. Programa de Pós-Graduação em Produtos Naturais e Sintéticos Bioativos, Centro de Ciências da Saúde, Universidade Federal da Paraíba, João Pessoa, PB, 58051-970, Brazil

    Juliana da Câmara Rocha & Patrícia Lima do Nascimento Néris

  2. Laboratório de Imunologia de Doenças Infecciosas. Departamento de Biologia Celular e Molecular, Universidade Federal da Paraíba, João Pessoa, PB, 58059-900, Brazil

    Juliana da Câmara Rocha, Larisse Virgolino da Silva, Viviane Silva Lima, Rephany Fonseca Peixoto, Ian Porto Gurgel do Amaral & Tatjana de Souza Lima Keesen

  3. Coordenação do curso de Medicina, Campus Ministro Reis Velloso, Universidade Federal do Piauí, Teresina, PI, 65202-020, Brazil

    Klinger Antonio da Franca Rodrigues

  4. Programa de Pós-Graduação em Ciências Farmacêuticas, Centro de Ciências Biológicas e da Saúde, Universidade Estadual da Paraíba, Campina Grande, PB, 58429-500, Brazil

    Fernanda Silva Almeida

  5. Programa de Pós-Graduação em Engenharia Química, Departamento de Engenharia Química, Centro de Tecnologia, Universidade Federal do Rio Grande do Norte, Natal, RN, 59078-970, Brazil

    Juliene da Câmara Rocha

  6. Instituto de Pesquisa de Medicamentos e Medicamentos da Universidade Federal da Paraíba, João Pessoa, PB, 58059-900, Brazil

    Fátima de Lourdes Assunção Araújo de Azevedo, Robson Cavalcanti Veras & Isac Almeida de Medeiros

  7. Laboratório de Síntese Orgânica Medicinal da Paraíba, Departamento de Química, Universidade Federal da Paraíba Campus I, João Pessoa, Paraíba, 58059-900, Brazil

    Wagner André Vieira da Silva, Claudio G. Lima-Junior & Mário Luiz Araújo de Almeida Vasconcellos

  8. Laboratório de Leishmanioses do Departamento de Biologia Molecular, Centro de Ciências Exatas e da Natureza, Universidade Federal da Paraíba, João Pessoa, PB, 58059-900, Brazil

    Márcia Rosa de Oliveira

Authors
  1. Juliana da Câmara Rocha
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  2. Klinger Antonio da Franca Rodrigues
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  3. Patrícia Lima do Nascimento Néris
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  8. Juliene da Câmara Rocha
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  12. Wagner André Vieira da Silva
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  13. Claudio G. Lima-Junior
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  14. Mário Luiz Araújo de Almeida Vasconcellos
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  17. Tatjana de Souza Lima Keesen
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Correspondence to Tatjana de Souza Lima Keesen.

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da Câmara Rocha, J., da Franca Rodrigues, K.A., do Nascimento Néris, P.L. et al. Biological activity of Morita-Baylis-Hillman adduct homodimers in L. infantum and L. amazonensis: anti-Leishmania activity and cytotoxicity. Parasitol Res 118, 3067–3076 (2019). https://doi.org/10.1007/s00436-019-06403-w

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