Santos Tamiris A C, Silva Kleiton P, Souza Gabriella B, Alves Péricles B, Menna-Barreto Rubem F S, Scher Ricardo, Fernandes Roberta P M
Laboratório de Enzimologia, Departamento de Fisiologia, Universidade Federal de Sergipe, São Cristóvão 49100-000, SE, Brazil.
Programa de Pós-Graduação em Agricultura e Biodiversidade, Universidade Federal de Sergipe, São Cristóvão 49100-000, SE, Brazil.
Pathogens. 2023 Mar 7;12(3):423. doi: 10.3390/pathogens12030423.
is a trypanosomatid phytoparasite, found in a great variety of species, including tomato plants. It is a significant problem for agriculture, causing high economic loss. In order to reduce the vegetal infections, different strategies have been used. The biological activity of molecules obtained from natural sources has been widely investigated to treat trypanosomatids infections. Among these compounds, chalcones have been shown to have anti-parasitic and anti-inflammatory effects, being described as having a remarkable activity on trypanosomatids, especially in species. Here, we evaluated the antiprotozoal activity of the chalcone derivative (NaF) on promastigotes, while also assessing its mechanism of action. The results showed that treatment with the derivative NaF for 24 h promotes an important reduction in the parasite proliferation (IC/24 h = 23.6 ± 4.6 µM). At IC/24 h concentration, the compound induced an increase in reactive oxygen species (ROS) production and a shortening of the unique flagellum of the parasites. Electron microscopy evaluation reinforced the flagellar phenotype in treated promastigotes, and a dilated flagellar pocket was frequently observed. The treatment also promoted a prominent autophagic phenotype. An increased number of autophagosomes were detected, presenting different levels of cargo degradation, endoplasmic reticulum profiles surrounding different cellular structures, and the presence of concentric membranar structures inside the mitochondrion. Chalcone derivatives may present an opportunity to develop a treatment for the infection, as they are easy to synthesize and are low in cost. In order to develop a new product, further studies are still necessary.
是一种锥虫属植物寄生虫，存在于多种物种中，包括番茄植株。它是农业上的一个重大问题，会造成巨大的经济损失。为了减少植物感染，人们采用了不同的策略。从天然来源获得的分子的生物活性已被广泛研究用于治疗锥虫感染。在这些化合物中，查耳酮已被证明具有抗寄生虫和抗炎作用，被描述为对锥虫具有显著活性，尤其是在[具体物种]中。在此，我们评估了查耳酮衍生物（NaF）对[某种锥虫]前鞭毛体的抗原虫活性，同时也评估了其作用机制。结果表明，用衍生物NaF处理24小时可显著降低寄生虫增殖（IC₅₀/24小时 = 23.6 ± 4.6 μM）。在IC₅₀/24小时浓度下，该化合物诱导活性氧（ROS）产生增加，并使寄生虫的唯一鞭毛缩短。电子显微镜评估强化了处理过的前鞭毛体中的鞭毛表型，并且经常观察到鞭毛囊扩张。该处理还促进了显著的自噬表型。检测到自噬体数量增加，呈现出不同程度的货物降解、围绕不同细胞结构的内质网轮廓以及线粒体内同心膜状结构的存在。查耳酮衍生物可能为开发治疗[该寄生虫名称]感染的药物提供机会，因为它们易于合成且成本低廉。为了开发新产品，仍有必要进行进一步研究。
