Herraez 2021 Pharmaceutics: Difference between revisions
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|diseases=Infectious | |diseases=Infectious | ||
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|preparations=Intact cells | |preparations=Intact cells | ||
|couplingstates=ROUTINE | |couplingstates=ROUTINE |
Latest revision as of 19:19, 16 February 2022
Herraez R, Quesada R, Dahdah N, Vinas M, Vinuesa T (2021) Tambjamines and prodiginines: Biocidal activity against Trypanosoma cruzi. Pharmaceutics 13:705. |
Herraez Rocio, Quesada Roberto, Dahdah Norma, Vinas Miguel, Vinuesa Teresa (2021) Pharmaceutics
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 ยตM for epimastigotes and 1.9, 0.57, and 0.1 ยตM 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 ยฝ 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. โข Keywords: Trypanosoma cruzi, Anti-chagasic agents, Cytotoxicity, Mitochondria, Obatoclax, Prodigiosin, Tambjamines, Targets โข Bioblast editor: Reiswig R โข O2k-Network Lab: ES Barcelona Garcia-Roves PM
Labels: MiParea: Respiration, Pharmacology;toxicology
Pathology: Infectious
Organism: Protists
Preparation: Intact cells
Coupling state: ROUTINE
Pathway: ROX
HRR: Oxygraph-2k
2021-08