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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http://dx.doi.org/10.1007/s00436-019-06403-w | DOI Listing |
Zoonoses Public Health
December 2024
Department of Animal Production and Preventive Veterinary Medicine, São Paulo State University, Botucatu, Brazil.
Aims: Leishmaniasis is an endemic disease in several regions of Brazil, a tropical country that presents specific environmental conditions that contribute to the development of phlebotomine vectors. This study aimed to detect Leishmania species in naturally infected bats from 17 municipalities in the São Paulo state.
Methods And Results: Spleen and liver samples from 203 bats were analysed by real-time PCR and confirmed by conventional PCR followed by gene sequencing.
Parasitol Res
November 2024
Laboratório de Doenças Parasitárias (LADOPAR), Programa de Pós-Graduação Em Medicina Veterinária, Universidade Federal de Santa Maria, Santa Maria, Rio Grande Do Sul, Brasil.
Acta Trop
December 2024
Departamento de Parasitologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais 31270-901, Brasil. Electronic address:
Leishmaniasis is a diverse group of clinical diseases caused by protozoan parasites of the Leishmania genus. Species-specific identification of Leishmania spp. is challenging due to the high number of different pathogenic species that sometimes co-circulate in the same foci, hampering efforts to effectively control the disease.
View Article and Find Full Text PDFInt J Mol Sci
October 2024
Instituto de Química Médica del Consejo Superior de Investigaciones Científicas de España, Juan de la Cierva 3, 28006 Madrid, Spain.
Indazoles have previously been identified as molecules with antiprotozoal activity. In this study, we evaluate the in vitro activity of thirteen 3-alkoxy-1-benzyl-5-nitroindazole derivatives (series D) against , and . In vitro, cytotoxicity against mouse peritoneal macrophages and growth inhibitory activity in promastigotes were evaluated for all compounds, and those showing adequate activity and selectivity were tested against intracellular amastigotes.
View Article and Find Full Text PDFPLoS Negl Trop Dis
October 2024
Laboratório de Doenças Parasitárias, Instituto Oswaldo Cruz/FIOCRUZ, Rio de Janeiro, Rio de Janeiro, Brazil.
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