Antileishmanial activity of MDL 28170, a potent calpain inhibitor
| Autor: | Fernanda A. Marinho, Claudia M. d’Avila-Levy, Marta H. Branquinha, Juliana L. Martins, Lívia O. Santos, André L.S. Santos |
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| Jazyk: | angličtina |
| Rok vydání: | 2006 |
| Předmět: |
Microbiology (medical)
Cell Biology Cysteine Proteinase Inhibitors Median lethal dose Article Parasitic Sensitivity Tests medicine Chemotherapy Animals Pharmacology (medical) Glycoproteins chemistry.chemical_classification Leishmania Calpain Kinetoplastida General Medicine Dipeptides biology.organism_classification In vitro Blot Peptidase inhibitor Infectious Diseases Enzyme medicine.anatomical_structure chemistry Biochemistry Microscopy Fluorescence biology.protein |
| Zdroj: | International Journal of Antimicrobial Agents |
| ISSN: | 1872-7913 0924-8579 |
| Popis: | Several calpain inhibitors are under development and some are useful agents against important human pathogens. We therefore investigated the effect of MDL 28170, a potent calpain inhibitor, on the growth of Leishmania amazonensis . After 48h of treatment, the inhibitor exhibited a dose-dependent antileishmanial activity, with a 50% lethal dose (LD 50 ) of 23.3μM. The inhibitor promoted cellular alterations, such as the parasites becoming short and round. A calpain-like protein migrating at 80kDa was identified by Western blotting. In addition, the calpain-like molecules were identified on the cell surface of the flagellate. These results add new in vitro insights into the exploitation of calpain inhibitors in treating parasitic infections and add this family of peptidases to the list of potential targets for development of more potent and specific inhibitors against trypanosomatids. |
| Databáze: | OpenAIRE |
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