Details

Autor(en) / Beteiligte

• Ribeiro, Lyanna Rodrigues
• Magalhães, Emanuel Paula
• Barroso Gomes, Naiara Dutra
• Cavalcante, John Washington
• Gomes Maia, Marcelo Morais
• Marinho, Márcia Machado
• Dos Santos, Hélcio Silva
• Marinho, Emmanuel Silva
• Sampaio, Tiago Lima
• Costa Martins, Alice Maria
• Paula Pessoa Bezerra de Menezes, Ramon Róseo

Titel

Elongation on aliphatic chain improves selectivity of 2-hydroxy-3,4,6-trimethoxyphenyl chalcone on Trypanosoma cruzi

Ist Teil von

• Future medicinal chemistry, 2024-01, Vol.16 (1), p.11-26

Ort / Verlag

England

Erscheinungsjahr

2024

Quelle

MEDLINE

Beschreibungen/Notizen

• Our objective was to investigate the trypanocidal effect of the chalcone (2 ,4 )-1-(2-hydroxy-3,4,6-trimethoxyphenyl)-5-phenylpenta-2,4-dien-1-one (CPNC). Cytotoxicity toward LLC-MK2 host cells was assessed by MTT assay, and the effect on 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 enzymes. CPNC showed activity against epimastigote, trypomastigote and amastigote life forms, induced membrane damage, increased cytoplasmic reactive oxygen species and mitochondrial dysfunction on . Regarding molecular docking, CPNC interacted with both trypanothione reductase and TcCr enzymes. CPNC presented a trypanocidal effect, and its effect is related to oxidative stress, mitochondrial impairment and necrosis.