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http://hdl.handle.net/2445/181172
Title: | Tambjamines and prodiginines: biocidal activity against trypanosoma cruzi |
Author: | Herráez, Rocio Quesada, Roberto Dahdah, Norma Viñas, Miquel Vinuesa Aumedes, Teresa |
Keywords: | Tripanosoma Mitocondris Malaltia de Chagas Trypanosoma Mitochondria Chagas' disease |
Issue Date: | 12-May-2021 |
Publisher: | MDPI |
Abstract: | 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. |
Note: | Reproducció del document publicat a: https://doi.org/10.3390/pharmaceutics13050705 |
It is part of: | Pharmaceutics, 2021, vol. 13, num. 5, p. 705 |
URI: | http://hdl.handle.net/2445/181172 |
Related resource: | https://doi.org/10.3390/pharmaceutics13050705 |
ISSN: | 1999-4923 |
Appears in Collections: | Articles publicats en revistes (Fonaments Clínics) Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL)) Articles publicats en revistes (Ciències Fisiològiques) Articles publicats en revistes (Patologia i Terapèutica Experimental) |
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