Author(s): Trein, Márcia Rodrigues ; Rodrigues e Oliveira, Lígia [UNESP] ; Rigo, Graziela Vargas ; Garcia, Mayara Aparecida Rocha [UNESP] ; Petro-Silveira, Brenda ; da Silva Trentin, Danielle ; Macedo, Alexandre José ; Regasini, Luis Octávio [UNESP] ; Tasca, Tiana
Date: 2019
Persistent ID: http://hdl.handle.net/11449/187150
Origin: Oasisbr
Subject(s): Antiparasitic; Antiprotozoal; Chalcone; Trichomonas vaginalis; Trichomoniasis
Made available in DSpace on 2019-10-06T15:27:03Z (GMT). No. of bitstreams: 0 Previous issue date: 2019-02-14
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Trichomoniasis is the most common non-viral sexually transmitted disease worldwide and can lead to serious consequences in reproductive health, cancer, and HIV acquisition. The current approved treatment present adverse effects and drug resistance data on this neglected parasitic infection is underestimated. Chalcones are a family of molecules that present biological applications, such as activity against many pathogenic organisms including protozoan pathogens. Chalcone (1) and three amino-analogues (2–4) were synthesized by Claisen–Schmidt condensation reaction and had their activity evaluated against the parasitic protozoan Trichomonas vaginalis. This bioassay indicated the presence and position of the amino group on ring A was crucial for anti-T. vaginalis activity. Among these, 3′-aminochalcone (3) presented the most potent effect and showed high cytotoxicity against human vaginal cells. On the other hand, 3 was not able to exhibit toxicity against Galleria mellonella larvae, as well as the hemolytic effect on human erythrocytes. Trophozoites of T. vaginalis were treated with 3, and did not present significant reactive oxygen species (ROS) accumulation, but induced a significantly higher ROS accumulation in human neutrophils after co-incubation. T. vaginalis pyruvate:ferredoxin oxidoreductase (PFOR) and β-tubulin gene expression was not affected by 3.
Laboratório de Pesquisa em Parasitologia Faculdade de Farmácia Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752
Laboratory of Antibiotics and Chemotherapeutics Institute of Biosciences Humanities and Exact Sciences (Ibilce) São Paulo State University (Unesp), Rua Cristóvão Colombo 2265
Departamento de Ciências Básicas da Saúde Universidade Federal de Ciências da Saúde de Porto Alegre
Laboratório de Biofilmes e Diversidade Microbiana Faculdade de Farmácia Universidade do Rio Grande do Sul, Av. Ipiranga 2752
Laboratory of Antibiotics and Chemotherapeutics Institute of Biosciences Humanities and Exact Sciences (Ibilce) São Paulo State University (Unesp), Rua Cristóvão Colombo 2265
CNPq: 408578/2013-0
CNPq: 443150/2014-1
