Herraez 2021 Pharmaceutics

From Bioblast
Publications in the MiPMap
Herraez R, Quesada R, Dahdah N, Vinas M, Vinuesa T (2021) Tambjamines and prodiginines: Biocidal activity against Trypanosoma cruzi. Pharmaceutics 13:705.

Β» PMID: 34065993 Open Access

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 Β΅M for epimastigotes and 1.9, 0.57, and 0.1 Β΅M 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 Β½ 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. β€’ Keywords: Trypanosoma cruzi, Anti-chagasic agents, Cytotoxicity, Mitochondria, Obatoclax, Prodigiosin, Tambjamines, Targets β€’ Bioblast editor: Reiswig R β€’ 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 


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