Anti-Trichomonas vaginalis activity of chalcone and amino-analogues
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1007/s00436-018-6164-4 http://hdl.handle.net/11449/187150 |
Resumo: | 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. |
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Anti-Trichomonas vaginalis activity of chalcone and amino-analoguesAntiparasiticAntiprotozoalChalconeTrichomonas vaginalisTrichomoniasisTrichomoniasis 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.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Laboratório de Pesquisa em Parasitologia Faculdade de Farmácia Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752Laboratory of Antibiotics and Chemotherapeutics Institute of Biosciences Humanities and Exact Sciences (Ibilce) São Paulo State University (Unesp), Rua Cristóvão Colombo 2265Departamento de Ciências Básicas da Saúde Universidade Federal de Ciências da Saúde de Porto AlegreLaboratório de Biofilmes e Diversidade Microbiana Faculdade de Farmácia Universidade do Rio Grande do Sul, Av. Ipiranga 2752Laboratory of Antibiotics and Chemotherapeutics Institute of Biosciences Humanities and Exact Sciences (Ibilce) São Paulo State University (Unesp), Rua Cristóvão Colombo 2265CNPq: 408578/2013-0CNPq: 443150/2014-1Universidade Federal do Rio Grande do SulUniversidade Estadual Paulista (Unesp)Universidade Federal de Ciências da Saúde de Porto AlegreUniversidade do Rio Grande do SulTrein, Márcia RodriguesRodrigues e Oliveira, Lígia [UNESP]Rigo, Graziela VargasGarcia, Mayara Aparecida Rocha [UNESP]Petro-Silveira, Brendada Silva Trentin, DanielleMacedo, Alexandre JoséRegasini, Luis Octávio [UNESP]Tasca, Tiana2019-10-06T15:27:03Z2019-10-06T15:27:03Z2019-02-14info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article607-615http://dx.doi.org/10.1007/s00436-018-6164-4Parasitology Research, v. 118, n. 2, p. 607-615, 2019.1432-19550932-0113http://hdl.handle.net/11449/18715010.1007/s00436-018-6164-42-s2.0-850580667290992736452764550Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengParasitology Researchinfo:eu-repo/semantics/openAccess2021-10-23T19:02:08Zoai:repositorio.unesp.br:11449/187150Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462021-10-23T19:02:08Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
title |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
spellingShingle |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues Trein, Márcia Rodrigues Antiparasitic Antiprotozoal Chalcone Trichomonas vaginalis Trichomoniasis |
title_short |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
title_full |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
title_fullStr |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
title_full_unstemmed |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
title_sort |
Anti-Trichomonas vaginalis activity of chalcone and amino-analogues |
author |
Trein, Márcia Rodrigues |
author_facet |
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 |
author_role |
author |
author2 |
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 |
author2_role |
author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Federal do Rio Grande do Sul Universidade Estadual Paulista (Unesp) Universidade Federal de Ciências da Saúde de Porto Alegre Universidade do Rio Grande do Sul |
dc.contributor.author.fl_str_mv |
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 |
dc.subject.por.fl_str_mv |
Antiparasitic Antiprotozoal Chalcone Trichomonas vaginalis Trichomoniasis |
topic |
Antiparasitic Antiprotozoal Chalcone Trichomonas vaginalis Trichomoniasis |
description |
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. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019-10-06T15:27:03Z 2019-10-06T15:27:03Z 2019-02-14 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1007/s00436-018-6164-4 Parasitology Research, v. 118, n. 2, p. 607-615, 2019. 1432-1955 0932-0113 http://hdl.handle.net/11449/187150 10.1007/s00436-018-6164-4 2-s2.0-85058066729 0992736452764550 |
url |
http://dx.doi.org/10.1007/s00436-018-6164-4 http://hdl.handle.net/11449/187150 |
identifier_str_mv |
Parasitology Research, v. 118, n. 2, p. 607-615, 2019. 1432-1955 0932-0113 10.1007/s00436-018-6164-4 2-s2.0-85058066729 0992736452764550 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Parasitology Research |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
607-615 |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1799964551615086592 |