ArticleParasitology research2018
Susceptibility of promastigotes and intracellular amastigotes from distinct Leishmania species to the calpain inhibitor MDL28170.
Article in Parasitology research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Susceptibility ofTropical medicine and infectious disease · 2024Article
- Assessing proteases and enzymes of the trypanothione system in subpopulations of Leishmania (Viannia) braziliensis Thor strain during macrophage infection.Memorias do Instituto Oswaldo Cruz · 2024Article
- Antibacterial, Antiparasitic, and Cytotoxic Activities of Chemical Characterized Essential Oil ofPharmaceuticals (Basel, Switzerland) · 2022Article
- Antileishmanial Efficacy of the Calpain Inhibitor MDL28170 in Combination with Amphotericin B.Tropical medicine and infectious disease · 2022Article
- Proteolytic inhibitors as alternative medicines to treat trypanosomatid-caused diseases: experience with calpain inhibitors.Memorias do Instituto Oswaldo Cruz · 2022Article
- Challenges and Tools for In VitroPathogens (Basel, Switzerland) · 2021Review
- Effects of functionally diverse calpain system on immune cells.Immunologic research · 2021Review
- The Diverse Calpain Family in Trypanosomatidae: Functional Proteins Devoid of Proteolytic Activity?Cells · 2021Review
- β-Cyclodextrin/Isopentyl Caffeate Inclusion Complex: Synthesis, Characterization and Antileishmanial Activity.Molecules (Basel, Switzerland) · 2020Article
- A Novel Anti-Microbial Peptide from Pseudomonas, REDLK Induced Growth Inhibition of Leishmania tarentolae Promastigote In Vitro.The Korean journal of parasitology · 2020Article
- Expression and cellular localisation of Trypanosoma cruzi calpains.Memorias do Instituto Oswaldo Cruz · 2020Article
- Calpains of Leishmania braziliensis: genome analysis, differential expression, and functional analysis.Memorias do Instituto Oswaldo Cruz · 2019Article
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Despite the available drug options, leishmaniasis treatment remains unsatisfactory. The repurposing of calpain inhibitors originally developed for human diseases became an interesting alternative, since Leishmania cells express calpain-related proteins. The susceptibility of six Leishmania species (L. amazonensis, L. braziliensis, L. major, L. mexicana, L. chagasi, and L. donovani) to the calpain inhibitor MDL28170 was determined. Promastigote and intracellular amastigote viability in the presence of MDL28170 was evaluated. MDL28170 was able to reduce promastigote proliferation in a dose-dependent manner for all the parasites. A significant reduction on the general parasite metabolism was detected, as judged by resazurin assay, as well as induced important morphological alterations, including rounding promastigotes and loss of the flagellum. MDL28170 was also able to reduce the number of intracellular amastigotes in RAW macrophages. The susceptibility of both parasite stages (promastigotes and amastigotes) to MDL28170 was similar for all Leishmania species tested. MDL28170 showed a much higher toxicity to Leishmania amastigotes when compared with mammalian macrophages, displaying selectivity index values varying from 13.1 to 39.8. These results suggest that the development of calpain inhibitors may represent an interesting alternative in the treatment of leishmaniasis.
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