Biological activity of Morita-Baylis-Hillman adduct homodimers in L. infantum and L. amazonensis: anti-Leishmania activity and cytotoxicity
| Autor: | Juliene da Câmara Rocha, Patrícia Lima do Nascimento Néris, Tatjana Souza Lima Keesen, Rephany Fonseca Peixoto, Juliana da Câmara Rocha, Claudio G. Lima-Junior, Wagner André Vieira da Silva, Robson Cavalcanti Veras, Ian P.G. Amaral, Márcia Rosa de Oliveira, Fátima de Lourdes Assunção Araújo de Azevedo, Mário L. A. A. Vasconcellos, Isac Almeida de Medeiros, Fernanda Silva Almeida, Viviane Silva Lima, Larisse Virgolino da Silva, Klinger Antonio da Franca Rodrigues |
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| Rok vydání: | 2019 |
| Předmět: |
030231 tropical medicine
Antiprotozoal Agents Drug Evaluation Preclinical Apoptosis Hemolysis Peripheral blood mononuclear cell 030308 mycology & parasitology 03 medical and health sciences 0302 clinical medicine Cutaneous leishmaniasis Amphotericin B parasitic diseases medicine Animals Humans Amastigote Cytotoxicity Leishmania 0303 health sciences General Veterinary biology Leishmaniasis Biological activity General Medicine medicine.disease biology.organism_classification Molecular biology Infectious Diseases Insect Science Parasitology Dimerization |
| Zdroj: | Parasitology Research. 118:3067-3076 |
| ISSN: | 1432-1955 0932-0113 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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