Antiproliferative activity on<i>Trypanosoma cruzi</i>(Y strain) of the triterpene 3β,6β,16β-trihidroxilup-20 (29)-ene isolated from<i>Combretum leprosum</i>

Aim: Our objective was to investigate the trypanocidal effect of the chalcone (2 E,4 E)-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.

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Antiproliferative activity onTrypanosoma cruzi(Y strain) of the triterpene 3β,6β,16β-trihidroxilup-20 (29)-ene isolated fromCombretum leprosum

Cited by 3 publications

References 71 publications

A review on the secretory structures, bioactive compounds and biological activities of selected Combretum species

A review on the secretory structures, bioactive compounds and biological activities of selected Combretum species

Quantum mechanical, molecular docking, molecular dynamics, ADMET and antiproliferative activity onTrypanosoma cruzi(Y strain) of chalcone (E)-1-(2-hydroxy-3,4,6-trimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one derived from a natural product

Elongation on Aliphatic Chain Improves Selectivity of 2-Hydroxy-3,4,6-Trimethoxyphenyl Chalcone on Trypanosoma Cruzi

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