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.

中文翻译：

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脂肪链的延长提高了 2-羟基-3,4,6-三甲氧基苯基查耳酮对克氏锥虫的选择性。


目的：我们的目的是研究查耳酮 (2E,4E)-1-(2-羟基-3,4,6-三甲氧基苯基)-5-苯基五-2,4-二烯-1-酮 (CPNC) 的杀锥虫效果）。材料和方法：通过MTT法评估对LLC-MK2宿主细胞的细胞毒性，并通过计数评估对克氏锥虫生命体（表鞭毛体、锥鞭毛体和无鞭毛体）的影响。进行流式细胞术分析以评估可能的作用机制。最后，进行分子对接模拟来评估 CPNC 和 T. cruzi 酶之间的相互作用。结果：CPNC 对克氏锥虫的上鞭毛体、锥鞭毛体和无鞭毛体生命形式表现出活性，诱导细胞膜损伤、细胞质活性氧增加和线粒体功能障碍。关于分子对接，CPNC 与锥硫酮还原酶和 TcCr 酶相互作用。结论：CPNC具有杀锥虫作用，其作用与氧化应激、线粒体损伤和坏死有关。