Tambjamines and Prodiginines: Biocidal Activity against Trypanosoma cruzi
| Autor: | Teresa Vinuesa, Miguel Viñas, Norma Dahdah, Rocío Herráez, Roberto Quesada |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
anti-chagasic agents
Chagas disease Trypanosoma Trypanosoma cruzi 030231 tropical medicine Pharmaceutical Science Tripanosoma Mitocondris Article Prodigiosin 03 medical and health sciences chemistry.chemical_compound Pharmacy and materia medica 0302 clinical medicine Malaltia de Chagas medicine Mode of action Amastigote IC50 030304 developmental biology 0303 health sciences biology Chemistry obatoclax biology.organism_classification medicine.disease Mitochondria Chagas' disease RS1-441 mitochondria tambjamines prodigiosin Biochemistry Benznidazole cytotoxicity targets Tambjamine medicine.drug |
| Zdroj: | Pharmaceutics Volume 13 Issue 5 Pharmaceutics, Vol 13, Iss 705, p 705 (2021) Dipòsit Digital de la UB Universidad de Barcelona |
| ISSN: | 1999-4923 |
| DOI: | 10.3390/pharmaceutics13050705 |
| Popis: | The aim of this work was to explore new therapeutic options against Chagas disease by the in vitro analysis of the biocidal activities of several tambjamine and prodiginine derivatives, against the Trypanosoma cruzi CLB strain (DTU TcVI). The compounds were initially screened against epimastigotes. The five more active compounds were assayed in intracellular forms. The tambjamine MM3 and both synthetic and natural prodigiosins displayed the highest trypanocidal profiles, with IC50 values of 4.52, 0.46, and 0.54 µM for epimastigotes and 1.9, 0.57, and 0.1 µM for trypomastigotes/amastigotes, respectively. Moreover, the combination treatment of these molecules with benznidazole showed no synergism. Finally, oxygen consumption inhibition determinations performed using high-resolution respirometry, revealed a potent effect of prodigiosin on parasite respiration (73% of inhibition at ½ IC50), suggesting that its mode of action involves the mitochondria. Moreover, its promising selectivity index (50) pointed out an interesting trypanocidal potential and highlighted the value of prodigiosin as a new candidate to fight Chagas disease. |
| Databáze: | OpenAIRE |
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