Gutiérrez-Cardona Jocelyn Yamin, Calderón-Jaimes Ernesto, Ortega-Cuellar Daniel, Sánchez-Carrillo Adrián, Castillo-Rodríguez Rosa Angélica, Canseco-Ávila Luis Miguel, Rocha-Ramírez Luz María, Martínez-Rosas Víctor, Gómez-Manzo Saúl, Hernández-Ochoa Beatriz
Laboratorio de Inmunoquímica, Hospital Infantil de México Federico Gómez, Secretaría de Salud, Mexico City 06720, Mexico.
Laboratorio de Nutrición Experimental, Instituto Nacional de Pediatría, Secretaría de Salud, Mexico City 04530, Mexico.
Int J Mol Sci. 2024 Apr 22;25(8):4568. doi: 10.3390/ijms25084568.
The parasite is the etiologic agent of trichomoniasis, the most common non-viral sexually transmitted disease worldwide. This infection often remains asymptomatic and is related to several health complications. The traditional treatment for trichomoniasis is the use of drugs of the 5-nitroimidazole family, such as metronidazole; however, scientific reports indicate an increasing number of drug-resistant strains. Benzimidazole derivatives could offer an alternative in the search for new anti-trichomonas drugs. In this sense, two attractive candidates are the compounds and (1-benzimidazole derivatives), since, through in vitro tests, they have shown a higher trichomonacide activity. In this study, we determined the effect on the expression level of metabolic genes in . The results show that genes involved in redox balance (, ) are overexpressed, as well as the gene that participates in the first reaction of glycolysis (); on the other hand, structural genes such as and are decreased in expression in trophozoites treated with the compound , which would probably affect its morphology, motility and virulence. These results align with the trichomonacidal activity of the compounds, with benzimidazole being the most potent, with an IC value of 4.8 μM. These results are promising for potential future therapeutic applications.
这种寄生虫是滴虫病的病原体，滴虫病是全球最常见的非病毒性性传播疾病。这种感染通常没有症状，并与多种健康并发症相关。滴虫病的传统治疗方法是使用5-硝基咪唑类药物，如甲硝唑；然而，科学报告显示耐药菌株的数量在增加。苯并咪唑衍生物可能为寻找新的抗滴虫药物提供一种替代方案。从这个意义上说，两种有吸引力的候选化合物是化合物 和 （1-苯并咪唑衍生物），因为通过体外试验，它们显示出更高的杀滴虫活性。在这项研究中，我们确定了 对代谢基因表达水平的影响。结果表明，参与氧化还原平衡的基因（ 、 ）以及参与糖酵解第一步反应的基因（ ）过度表达；另一方面，在用化合物 处理的滋养体中，诸如 和 等结构基因的表达降低，这可能会影响其形态、运动性和毒力。这些结果与化合物的杀滴虫活性一致，其中苯并咪唑 最有效，IC值为4.8 μM。这些结果对未来潜在的治疗应用很有前景。
