Elongation on aliphatic chain improves selectivity of 2-hydroxy-3,4,6-trimethoxyphenyl chalcone on Trypanosoma cruzi.
Future Med Chem
; 16(1): 11-26, 2024 Jan.
Article
en En
| MEDLINE
| ID: mdl-38084595
ABSTRACT
Aim:
Our objective was to investigate the trypanocidal effect of the chalcone (2E,4E)-1-(2-hydroxy-3,4,6-trimethoxyphenyl)-5-phenylpenta-2,4-dien-1-one (CPNC). Material &methods:
Cytotoxicity toward LLC-MK2 host cells was assessed by MTT assay, and the effect on Trypanosoma cruzi life forms (epimastigotes, trypomastigotes and amastigotes) was evaluated by counting. Flow cytometry analysis was performed to evaluate the possible mechanisms of action. Finally, molecular docking simulations were performed to evaluate interactions between CPNC and T. cruzi enzymes.Results:
CPNC showed activity against epimastigote, trypomastigote and amastigote life forms, induced membrane damage, increased cytoplasmic reactive oxygen species and mitochondrial dysfunction on T. cruzi. Regarding molecular docking, CPNC interacted with both trypanothione reductase and TcCr enzymes.Conclusion:
CPNC presented a trypanocidal effect, and its effect is related to oxidative stress, mitochondrial impairment and necrosis.Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Tripanocidas
/
Trypanosoma cruzi
/
Enfermedad de Chagas
/
Chalconas
Límite:
Humans
Idioma:
En
Revista:
Future Med Chem
Año:
2024
Tipo del documento:
Article
País de afiliación:
Brasil