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Effect of Trichomonacide 6-Nitro-1H-benzimidazole Derivative Compounds on Expression Level of Metabolic Genes in Trichomonas vaginalis

Authors :
Jocelyn Yamin Gutiérrez-Cardona
Ernesto Calderón-Jaimes
Daniel Ortega-Cuellar
Adrián Sánchez-Carrillo
Rosa Angélica Castillo-Rodríguez
Luis Miguel Canseco-Ávila
Luz María Rocha-Ramírez
Víctor Martínez-Rosas
Saúl Gómez-Manzo
Beatriz Hernández-Ochoa
Source :
International Journal of Molecular Sciences, Vol 25, Iss 8, p 4568 (2024)
Publication Year :
2024
Publisher :
MDPI AG, 2024.

Abstract

The parasite Trichomonas vaginalis 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 O2N-BZM7 and O2N-BZM9 (1H-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 T. vaginalis. The results show that genes involved in redox balance (NADHOX, G6PD::6PGL) are overexpressed, as well as the gene that participates in the first reaction of glycolysis (CK); on the other hand, structural genes such as ACT and TUB are decreased in expression in trophozoites treated with the compound O2N-BZM9, which would probably affect its morphology, motility and virulence. These results align with the trichomonacidal activity of the compounds, with benzimidazole O2N-BZM9 being the most potent, with an IC50 value of 4.8 μM. These results are promising for potential future therapeutic applications.

Details

Language :
English
ISSN :
14220067 and 16616596
Volume :
25
Issue :
8
Database :
Directory of Open Access Journals
Journal :
International Journal of Molecular Sciences
Publication Type :
Academic Journal
Accession number :
edsdoj.8723ee9193bc422499dc56c1b6b2a0ca
Document Type :
article
Full Text :
https://doi.org/10.3390/ijms25084568