Interactions between 4-aminoquinoline and heme: Promising mechanism against Trypanosoma cruzi
| Autor: | Maria Cristina M. Motta, Alice M. R. Bernardino, Julio C. Borges, Samara Braga do Nascimento, Humberto Pinheiro de Araújo, Aline Araujo Zuma, Guilherme C. Lechuga, Claudia M. Calvet, Mirian Claudia de Souza Pereira, Saulo Cabral Bourguignon |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Chagas disease Cell Survival Trypanosoma cruzi Quinoline Heme lcsh:Infectious and parasitic diseases Inhibitory Concentration 50 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Microscopy Electron Transmission medicine Chemotherapy lcsh:RC109-216 Pharmacology (medical) Amastigote Pharmacology biology Regular Article biology.organism_classification medicine.disease Trypanocidal Agents Mitochondria 030104 developmental biology Infectious Diseases Biochemistry Mechanism of action chemistry Benznidazole 030220 oncology & carcinogenesis 4-Aminoquinoline Aminoquinolines Parasitology medicine.symptom Hemin medicine.drug |
| Zdroj: | International Journal for Parasitology: Drugs and Drug Resistance International Journal for Parasitology: Drugs and Drug Resistance, Vol 6, Iss 3, Pp 154-164 (2016) |
| ISSN: | 2211-3207 |
| Popis: | Chagas disease is a neglected tropical disease caused by the flagellated protozoan Trypanosoma cruzi. The current drugs used to treat this disease have limited efficacy and produce severe side effects. Quinolines, nitrogen heterocycle compounds that form complexes with heme, have a broad spectrum of antiprotozoal activity and are a promising class of new compounds for Chagas disease chemotherapy. In this study, we evaluated the activity of a series of 4-arylaminoquinoline-3-carbonitrile derivatives against all forms of Trypanosoma cruzi in vitro. Compound 1g showed promising activity against epimastigote forms when combined with hemin (IC50 Graphical abstract Highlights • 4-arylaminoquinoline-3-carbonitrile derivatives were active against Trypanosoma cruzi. • Hemin increased quinoline activity against trypomastigotes and epimastigotes. • Combination therapy did not affected mammalian cells. • Peroxidation of heme were inhibit by addition of quinoline derivative. • Quinoline-heme interactions are proposed as new trypanocidal mechanism. |
| Databáze: | OpenAIRE |
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